[Problems] A compound, which is useful as an active ingredient for a pharmaceutical composition, for example a pharmaceutical composition for treating constipation-type irritable bowel syndrome, atonic constipation and/or functional gastrointestinal disorder, is provided. [Means for Solution] The present inventors ...

[Problem]To provide an anti human IL 23R antibody that has excellent activity and/or species cross reactivity as compared to conventional anti human IL 23R antibodies and to provide means using the antibody for preventing or treating various types of diseases in which human IL 23R is involved in pathogenesis. [Solut...

The present invention addresses the problem of providing a method for acquiring and producing kidney progenitor cells having a high degree of purity from a cell population obtained by inducing differentiation of pluripotent stem cells into kidney progenitor cells by identifying a kidney progenitor specific cell surf...

333[Problem] To provide a compound useful as an active ingredient of a pharmacological composition for the treatment of urinary storage symptoms dysuria lower urinary tract diseases and the like. [Solution] The inventors perfected the present invention after discovering that thiazole derivatives substituted at posit...

The present invention provides anti-CD28 antibodies which are defective in mitogenic activity (silenced anti-CD28 antibodies), methods of producing, compositions containing the antibody and methods of immunosuppression, inducing T-cell tolerance and treating organ and/or tissue transplant rejections. ...

A stable oral solid drug composition of ramosetron or a pharrnaceutically acceptable salt thereof, which is characterized by containing one or two or more members selected from the group consisting of the following (i) to (vi); (i) an aliphatic carboxylic acid selected from the group consisting of maleic acid, malo...

To provide novel crystals useful as an ingredient for the production of a diabetes remedy. The invention is concerned with α-form crystal and ß-form crystal of (R)-2-(2-aminothiazol-4-yl)-4"-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide. The α-form crystal does not exhibit hygroscopicity and has a stability s...

A quick-disintegrating tablet in the bucccal cavity comprising a drug; a diluent; a saccharide of the kind such as herein described characterized in that said tablet comprising a saccharide with a relatively lower melting point than said drug and said diluent; and a binder; wherein the amount of saccharide with a lo...

[Problems] A useful compound which can be used as a pharmaceutical, in particular, an agent for treating peripheral arterial occlusive disease is provided. [Means for Solution] The present inventors have conducted extensive studies on EP4 receptor agonists, and as a result, have found that a novel pyridone ...

TITLE: 2-ACYLAMINOTHIAZOLE DERIVATIVE OR SALT THEREOF. A 2-acylaminothiazole derivative or a pharmaceutically acceptable salt thereof having an excellent effect of proliferating human c-mpl-Ba/F3 cells and an activity of increasing platelets based on the effect of promoting the formation of megakaryocytic colon...

A pharmaceutical composition for improving chronic pelvic cavity pain syndrome due to urinary dysfunction where said composition contains tamsulosin or pharmaceutically acceptable salts thereof.

Provided is a compound useful as an inhibitor against the kinase activity of EML4- ALK fusion protein. As a result of intensive and extensive studies on compounds having inhibitory activity against the kinase activity of EML4-ALK fusion protein, the present inventors found that the diamino heterocyclic carboxamid...

There is provided a compound having a capsaicin receptor VRl inhibitory activity and useful as a therapeutic agent for various pains including inflammatory pain and neurogenic pain, migraine, cluster headache, bladder diseases including overactive bladder, and the like. A benzamide derivative or a salt thereof wher...

Abstract [Abstract] [Problem] Provided is a compound which is useful as a dopamine Dl receptor positive allosteric modulator (Dl PAM). [Means for Solution] The present inventors have studied a compound which has a positive allosteric modulating action (PAM action) on a dopamine Dl receptor and which can be used ...

This invention relates to a bicyclic nitrogen containing aromatic heterocyclic amide compound of formula (I) or a salt thereof which has excellent Complex 1 inhibitory effect and AMPK activating effect and which is useful as a therapeutic drug for breast cancer. This compound has a cell growth inhibitory effect on a...

[Problem] To provide an anti human Tie2 antibody which prevents or treats diabetic macular edema diabetic retinopathy or critical limb ischaemia by binding to human Tie2 and activating human Tie2. [Solution] The inventors of the present invention studied anti human Tie2 antibodies and have provided an anti human Tie...

[Problem] To provide an anti human Igß antibody in which BCR and Fc?RIIb are crosslinked and which has a more enhanced immunosuppressive function compared to conventional antibodies. [Solution] An anti human Igß antibody including: a heavy chain variable region that includes a CDR 1 comprising an amino acid sequence...

[Object]A compound which is useful as an EP1 receptor antagonist is provided. [Means for Solution] The present inventors investigated EP1 receptor antagonists, and confirmed that a compound having a sulfonamide structure, in which the nitrogen atom of the sulfonamide structure is substituted with 2-fluoropropyl gro...

[Problem] To provide a compound that can be used as an MC4 receptor agonist. [Solution] The inventors studied MC4 receptor agonists confirmed that a piperazine derivative has an action and perfected the present invention. Specifically this piperazine derivative has an MC4 receptor agonist action and can be used as a...

A compound, which can be used for preventing or treating diseases, in which 11ß-hydroxysteroid dehydrogenase type 1(11ß-HSD1) is concerned, in particular, diabetes, insulin resistance, dementia, schizophrenia and depression, is provided. [Means for Solution] It was found that a triazole derivative, in which one of ...

[Problem] To provide a compound which has a positive allosteric modulating effect (PAM effect) for an ??7 nicotinic acetylcholine receptor (??7 nACh receptor). [Solution] The inventors have achieved the present invention by making studies on PAM effects for an ??7 nACh receptor and confirming that a tetrahydrooxepi...

[Problems] A compound which is useful as an active ingredient of a pharmaceutical composition for treating neuropathic pain is provided. [Means for Solution] The present inventors have made extensive studies on compounds having an FAAH inhibitory activity, and as a result, have found that an azole compound substi...

The present invention provides a pharmaceutical composition whose active ingredients are (R)-5-(2-{[2-(2-ethoxyphenoxy)ethyl]amino}propyl-2-methoxybenzene-1-sulfonamide (tamsulosin), or its pharmaceutically acceptable salt, and (1S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylic acid (3R)-quinuclidin-3-yl este...

Provided is a novel and excellent method for treating and/or preventing benign prostatic hyperplasia, prostate cancer, and the like based on selective inhibitory activity against 17βHSD type 5.  It was found that an indole or benzimidazole derivative, where a nitrogen atom of the indole ring or benzimidazole ring is...

The present invention provides a compound which is useful as an inhibitor against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. As a result of extensive and intensive studies on compounds having an inhibitory effect against the kinase activity of EML4-ALK fusion proteins and mutant EGFR ...

[Problem] To provide a compound useful as the active ingredient in a drug composition for treating diseases to which 11ß hydroxysteroid dehydrogenase type 1 contributes such as dementia schizophrenia depression pain (particularly neuropathic pain and fibromyalgia) diabetes (particularly type 2 diabetes) and insulin ...

[Problem] To provide a compound which is useful as a novel and excellent prophylactic and/or therapeutic agent for rejection in various types of organ transplantation allergic diseases autoimmune diseases and blood tumors and which acts in a manner relying on a PI3Kd selective inhibitory activity and/or an IL 2 pr...

The objective of the present invention is to provide a compound having inhibitory activity against an intestinal phosphate transporter (NPT IIb) and useful as an active ingredient in a hyperphosphatemia therapeutic agent and/or preventive. A thiophene compound represented by formula (I) may be used as a hyperphospha...

As a result of studies on compounds having a selective inhibitory activity against l7βHSD type 5, the present inventors have confirmed that a {1-[(indol-2-yl)carbonyl]piperidyl}alkanol derivative has a potent selective inhibitory- activity against 17βHSD type 5.  The invention has been completed based on these findi...

[Problem] To provide a pharmaceutical product especially a pharmaceutical composition which is useful for the treatment of pain. [Solution] The inventors have intensively studied using pain model animals for the purpose of providing a therapeutic agent for pain. As the results of the intensive studies the inventors...

Abstract Provided is a novel potent pharmaceutical composition for treating nociceptive pain. The present invention relates to a pharmaceutical composition for treating nociceptive pain, containing a morpholine derivative or a pharmaceutically acceptable salt thereof, as an active ingredient. The present inventio...

The present invention provides a substituted amide compound such as a compound represented by formula AA which is useful as an active ingredient of a pharmaceutical composition especially as an active ingredient of a pharmaceutical composition for the treatment of diseases that are caused by lysophosphatidic acid (L...

As a result of extensive studies on NAD(P)H oxidase inhibitors, the present inventors found that a quinolone derivative having, at the 2-position, an alkyl group substituted with a heteroatom or the like has an excellent NAD(P)H oxidase inhibitory activity, and accomplished the present invention.  The compound of th...

[Problem] To provide a compound that is useful as an inhibitor of EGFR T790M mutation kinase activity. [Solution] The inventors studied compounds having an inhibiting effect against EGFR T790M mutation kinase and perfected the invention upon confirming that a pyrazine carboxamide compound has an inhibiting effect ag...

The present invention provides a substituted amide compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for treating diseases caused by lysophosphatidic acid (LPA). (wherein A is aryl which may be substituted, etc, B is a 5-membered aro...

To provide a therapeutic and/or prophylactic agent for urinary frequency, urinary urgency, and urinary incontinence associated with various lower urinary tract diseases including overactive bladder, various lower urinary tract diseases accompanied by lower urinary tract pain, such as interstitial cystitis, chronic p...

[Problem] To provide: an anti human CTGF antibody having a superior binding activity and/or a superior neutralization activity compared with those of conventional anti human CTGF antibodies; and a means for preventing or treating various diseases in which human CTGF is involved in the formation of clinical condition...

A pharmaceutical agent having GPR40 receptor agonistic action, particularly a compound which is useful as an insulin secretagogue or an agent for preventing and/or treating diabetes mellitus. The present inventors have examined a compound having GPR40 receptor agonistic action, confirmed that an oxadiazolidinedione ...

Problems] A compound useful as an active ingredient for a pharmaceutical composition for treating FAAH-related diseases is provided. [Means for Solution] The present inventors have made extensive studies on compounds having an FAAH inhibitory activity, and as a result, have found that a piperazine-l-carboxylate c...

The present invention provides a solid pharmaceutical composition comprising a cocrystal of (1S)-1,5-anhydro-1-[3-(1-benzothien-2-ylmethyl)-4-fluorophenyl]-D-glucitol and L-proline, in combination with crystalline cellulose, and also provides a method for producing the composition.

Provided is a compound which has an excellent S1 P1 agonist action, and is useful particularly as an active ingredient for an agent for preventing and/or treating a disease induced by undesirable lymphocyte infiltration or a disease induced by abnormal proliferation or accumulation of cells. [Means for Solution] ...

The present invention addresses the problem of providing a pharmaceutical composition particularly a compound suitable for the treatment of nocturia. Extensive and intensive studies have been made on compounds capable of inhibiting placental leucineaminopeptidase (P LAP) in the anticipation that an antidiuretic act...

5A5A[Problem] To provide an exceptional agent for preventing or treating dementia and schizophrenia the agent being based on a serotonin 5 HT receptor regulating action. [Solution] The inventors perfected the invention upon discovering that a tetrahydroisoquinoline derivative characterized by having a structure in w...

The purpose of the present invention is to provide a new process for producing an enzalutamide crystal form which is reduced in the contents of 2 propanol and B form crystals the process including obtaining wet crystals of enzalutamide in a crystallization step during the production of the enzalutamide crystal form ...

[Problem] To provide a medicinal composition for treating cancer in which at least one kinase selected from among BTK JAK3 and ITK participates. [Solution] As the results of studies on compounds having BTK inhibiting effect JAK3 inhibiting effect and ITK inhibiting effect the present inventors confirmed that specifi...

The present invention addresses the problem of providing a medicinal composition and in particular a compound suitable for treating nocturia. Under the expectation that nocturnal urinary frequency could be reduced via an antidiuretic action said antidiuretic action being induced by inhibiting placental leucine amino...

[Abstract] [Object] A novel and excellent method for preventing or treating rejection in the transplantation of various organs, allergy diseases, autoimmune diseases, hematologic tumor, or the like, based on a PDK5-selective inhibitory action and/or an IL-2 production inhibitory action, and/or ...

A compound useful as an antifungal agent, particularly a therapeutic agent for deep-seated mycoses, is provided. A fungus Acremonium persicinum was collected, and cyclic compounds were isolated from culture liquids thereof. The present inventors confirmed that the cyclic compounds or salts thereof have a potent anti...

[Object]  To provide an excellent pharmaceutical composition for preventing and/or treating vascular diseases. [Means for Solution]  Useful to provide a pharmaceutical composition for preventing and/or treating vascular diseases, which comprises 1) a COX-1 selective inhibitor and 2) clopidogrel or a pharmaceuticall...

[Problem] To provide an excellent therapeutic or prophylactic agent for cardiovascular diseases on the basis of cGMP production increasing activity attributed to soluble guanylate cyclase activating activity. [Solution] It was discovered that an imidazopyridine compound having a carbamoyl group at the 3 position of...

Disclosed is a compound which has an intestinal phosphate transporter (NPT IIb) inhibition activity and is useful as an active ingredient for a therapeutic agent and/or a prophylactic agent for hyperphosphatemia. A tetrahydrobenzothiophene compound represented by formula (I) has an NPT IIb inhibition activity and c...

The present invention provides a condensed pyrrolopyridine derivative which is useful as an active ingredient for a pharmaceutical composition, in particular, a pharmaceutical composition for preventing or treating diseases caused by undesirable cytokine signal transduction or diseases caused by abnormal cytokine si...

A miciro organisim which produces compounds useful as an antifungal agent, particularly a therapeutic agent for deep-seated mycoses, such as mycotic sinusitis, is provided. The present inventors have conducted intensive studies on naturally-occurring microorganisms as a research for antifungal compounds, and found a...

[Object]  Disclosed is a compound useful as an active ingredient for a pharmaceutical composition having an a-amylase inhibitory activity, particularly a pharmaceutical composition for the treatment of diabetes. [Solution]  An investigation has been made on a compound having an α-amylase inhibitory activity among t...

Provided is a compound which is useful as an agent for treating or preventing 5-HT2C receptor-related diseases, particularly incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like,...

Provided is a novel and excellent method for preventing and/or treating diseases j related to a cannabinoid type 2 receptor, based on an agonistic action on a cannabinoid type 2 receptor. [Means for Solution] It was found that a hetero ring derivative mainly having two substituents, for example, a pyrimidine...

The present invention has an object to provide a compound having a GPR40 agonistic activity, which is useful as a pharmaceutical composition, an insulin secretion promoter, or an agent for preventing/treating diabetes. [Means for Solution] The present inventors have extensively studied a compound having a GPR40 agon...

[Problem] A compound which is useful as an anti-obesity agent is provided. [Means for Solution] The present inventors have investigated a compound having a DGAT1 inhibitory action, which is promising as an active ingredient of a pharmaceutical composition for treating obesity, type II diabetes mellitus, fatt...

[Problem] Provided is a compound which has a PDE9-inhibiting action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, and bladder/urethral diseases, and the like. [Means for Solution] The present inventors have investigated a compoun...

Disclosed is a prophylactic or therapeutic agent for diseases associated with pains in urinary organs. It is confirmed that a pyridyl non aromatic nitrogenated heterocyclic 1 carboxylate compound or a salt thereof has an effective bladder capacity increasing activity and also has an analgesic activity on pains in t...

The invention relates to compound of the formula (!) or its salt, wherein -R1 -R2, -R3; R4 -R5, -M-, -X- and -Y= are as defined in the description, their use of as medicament, the process for their preparation and use for the treatment of JAK3 mediated diseases.

Disclosed is a pharmaceutical composition which contains: a composite of solifenacin or a pharmaceutically acceptable salt thereof and an ion exchange resin; and an acrylic acid polymer.

The l-(2-methoxyethyl)-2-melthyl-4, 9-dioxo-3-(pyrazin-2-ylmethyl)-4, 9-dihydro-lH-naphtho [2 , 3-d] imidazol-3-ium bromide of the invention and its crystals, particularly α-and ß-form Crystals, have no hygroscopic property, have excellent stability and therefore are useful as production materials of medicines. Part...

It is intended to provide novel a compound useful in drugs, in particular, in drugs for various diseases caused by infection with viruses belonging to the family Herpesviridae, i.e., in preventing or treating infections with various herpesviruses, more specifically speaking, chicken pox (varicella) caused by the inf...

2-Acylaminothiazole derivatives or salts thereof which have a platelet increasing activity based on an excellent human c-mpl-Ba/F3 cell growth function and a function of accelerating formation of megakaryocytic colonies and which are useful for treating thrombocytopenia are provided.

The piperidine derivative of the present invention in which the 4-position of the piperidine ring is bonded, via vinylene, to a mono-substituted (-R1) or unsubstituted benzene ring and the 1-position of the piperidine ring has an acyl group [-C(=O)-R4], or a pharmaceutically acceptable salt thereof has an excellent ...

A platelet aggregation inhibitor comprising a quinolone derivative or a pharmaceutically acceptable salt thereof as an active ingredient, and a novel quinolone derivative or a pharmaceutically acceptable salt thereof useful as a platelet aggregation inhibitor.

This invention relates to novel amide derivatives and salts thereof. More particularly, it relates to novel amide derivatives and salts thereof which act as a ROCK inhibitor, to a pharmaceutical composition comprising the same and to a method of using the same therapeutically in the treatment and/or prevention of RO...

[Problem] There is provided a compound which can be used for therapy of diseases in which l ip-hydroxysteroid dehydrogenase type l (l 1(3-HSD1) participates, in particular diabetes, insulin resistance. [Means for Solution] It has been found that a triazole derivative wherein the triazole ring is substituted wi...

The present invention relates to a compound of the formula [I]: wherein (a), in which -Y6 area R5 each as defined in the description, etc., R1 is hydrogen, halogen, lower alkyl, hydroxy, etc., R2 is hydrogen, lower alkyl or hydroxy(lower)alkyl, R3 is hydrogen or an amino protective group, 20 R7 is hydrogen, lower al...

Disclosed is an orally disintegrating tablet comprising a pharmacologically active substance, a modified starch having a degree of gelatinization of 30 to 60%, and a saccharide. Also disclosed is a process for producing an orally disintegrating tablet, which comprises the steps of mixing a pharmacologically active s...

The present invention relates to a new cyclic peptide compound or a salt thereofr which has anti-hepatitis C virus activities based on -inhibitory activity against the RNA replication of hepatitis C virus replicon, to a process for preparation thereof comprising a rearrangement reaction under a mild acidic conditi...

There are provided newpyrimidine derivatives condensed with a non-aromatic ring selected from dihydrothiophene', dihydrofuran, cycloalkane moiety, and the like or phairaaceutically acceptable salts thereof; and a pharmaceutical composition comprising said compound as an active ingredient. These compounds exhibit ...

It is intended to provide an agent for treating or preventing hyperuricemia, gout, inflammatory bowel disease, diabetic nephropathy, diabetic retinopathy and so on which has a non-nucleic acid structure and exerts an excellent xanthine oxidase inhibiting action and a hypouricemic effect. It has been confirmed tha...

(R)-2-(2-aminothiazol-4-yl)-4" -[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide or its salt shows a potent bladder relaxation effect in "isolated rat bladder smooth muscle relaxation test", dose-dependently lowers the contraction frequency of rhythmic bladder contractions in "rat rhythmic bladder contra...

It is an object of the present invention to provide a novel therapeutic agent for glioblastoma. In accordance with the present invention, it was found that compounds having an antagonistic action against AMPA receptor are useful as therapeutic agents for glioblastoma, particularly primary glioblastoma de nova with a...

The present invention relates to a compound of the formula [I]: wherein R1 is lower alkyl or hydroxy (lower) alkyl, and R2 is hydrogen or amino protecting group, or R1 and R2 are bonded together and form lower alkylene; R3 is - A-R6 wherein A is bond, -NHCO-(CH2CO)n-, lower alkylene, -NH-CO-CO- or the like, and R6 i...

A pharmaceutical composition for controlled release comprises (a) a drug of the kind such as herein described, wherein the amount of the drug is from 0.02 wt% to 85 wt% per unit of the pharmaceutical preparation, (b) polyethylene oxide wherein the amount of polyethylene oxide is 10 to 95 wt% per unit of the pharmace...

A pharmaceutical composition for therapy of diarrhea irritable bowel syndrome in male and female patients, containing from 0.001 to 0.05 mg of ramosetron hydrochloride as a daily dose or an equivalent molar amount of ramosetron or its pharmaceutically acceptable other salt as an active ingredient. ...

To provide a novel and excellent agent for treating or preventing nociceptive pain, neuropathic pain, cancer pain, headache, bladder function disorder and the like, based on the inhibitory action on the capsaicin receptor VRl activation. The present invention was accomplished by confirming that a benzamide derivati...

The present invention relates to a novel compound or a salt thereof, which is useful as a CRT.H2 antagonist, especially as a medicament for disorder that participates eosinophil, for example, allergic disorder such as asthma, allergic rhinitis, allergic dermatitis, conjunctival inflammation, hives, eosinophilic bron...

A non-immnunosuppressive pipecolic acid derivative having an affinity for FKBP-type immunophilins is provided for inducing chondrogenic differentiation. Composition containing such compounds is also disclosed.

ABSTRACT The present invention provides a compound having excellent JAK3 inhibitory activity and being useful as an active ingredient of an agent for treating and/or preventing various immune diseases including autoimmune diseases, inflammatory diseases, and allergic diseases. As a result of investigations with re...

Macrolide compound (I) is provided for treating or preventing erectile dysfunction, which is, for example, induced by or secondary to diseases, alcoholism, aging, arterial insufficiency, venous leakage, hormonal insufficiency, drug use, surgery, chemotherapy or radiation, particularly, for preventing or treating an ...

The present invention provides a novel formulation for improving chronic pelvic cavity pain syndrome due to urinary dysfunction and/or hypogastric/perineal pain due to a state of decreased urine production. The invention also provides a process for preparing such composition.

The present invention relates to an agent for preventing and/or treating diabetic neuropathy comprising a 2-[(substituted-inden-7-yloxy)methyl)morpholine of the formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient. The invention is useful for Providing an excellent agent for preventing a...

The present invention relates to an agent for preventing and/or treating neuropathic pain comprising a 2-[ (substitutecl-inden-7-yloxy) methyl)morpholine of the formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient. The invention is useful for providing an excellent agent for preventing a...

[Problems] To provide a novel process for producing ramosetron or its salt that is useful as a pharmaceutical, especially as a therapeutic and/or preventive agent for digestive symptoms caused by administration of an anti- malignant tumor agent, diarrheal-type irritable bowel syndrome, diarrheal symptoms of irr...

The present invention relates to a process for preparing a pharmaceutical composition for the therapy of overactive bladder wherein said composition contains 0.1 to 2.0 mg of tamsulosin or its salt and 1 to 100 mg of quinuclidin-3 '-yl l-phenyl-l,2,3,4,-tetrahydroisoquinoline-2-carboxylate or its salt. ...

It is intended to provide a compound having an excellent effect of inhibiting dipeptidylpeptidase IV, and an excellent remedy for insulin-dependent diabetes (type 1 diabetes), in particular, insulin-independent diabetes (type 2 diabetes), insulin resistance disease and obesity based on the above effect. ...

The present invention relates to a pharmaceutical composition for improving adsorption of a drug on the gastrointestinal mucous layers. Further, the invention relates to use of an ethylene oxide derivative for producing a drug adsorptivity improving agent. Specifically, it relates to use of one or more members selec...

Provided is a compound that is an NMDA receptor antagonist having a broader safety margin, and is useful as an agent for treating or preventing Alzheimer"s disease, cerebrovascular dementia, Parkinson"s disease, ischemic apoplexy, or pain. A novel compound or a salt thereof, which is characterized in that it has ...

The present invention relates to the crystal of 4, 6- dimethyl - 4' - [3 , 5 - bis (trifluoromethyl)-lH-pyrazol-l-yl] nicotinanilide having excellent activity of inhibiting Ca2+ release-activated Ca2+ channel and suppressing 1L-2 production to find that the compound includes the presence of two types of polymorphic ...

A process for producing an azulene derivative useful as a Na+-glucose cotransporter inhibitor, which is high in yield, is simple in operation, is low in cost, is suited for environmental protection, and is advantageous industrially, the process being characterized by reducing and deprotecting at least one compound s...

[Problems]  To provide a pharmaceutical, in particular a compound which can be used as a therapeutic agent for irritable bowel syndrome (IBS). [Means for Solving Problems]  It was found that a tetrahydroisoquinolin-l-one derivative having an amide group at the 4-position or a pharmaceutically acceptable salt thereo...

[Solving Means]  The present inventors have conducted extensive studies on an EP4 receptor agonist, and as a result, found that a novel pyridone compound characterized in that the 1-position in the pyridone ring is substituted with a group having an acidic group such as a carboxyl group and the 6-position is bonded ...

Abstract The present invention provides a humanized anti-human osteopontin antibody having better activities (antigen binding activity, leukocyte migration inhibitory activity and the like) and/or stability (resistance to heat, low-pH conditions, denaturants and the like) than those of conventional anti-human osteo...

A choline salt crystal of (1S)-1,5-anhydro-1-[5-(azulen-2-ylmethyl)-2-hydroxyphenyl]- D-glucitol which shows an endothermic peak at 194 to 198°C as measured by differential scanning calorimetry (DSC analysis) and shows main peaks at about 2?(°) 5.58, 14.72, 16.80, 17.82, 21.02 and 22.46 as measured by powder X ray d...

[Problem] To provide a compound which can be used in the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly in the treatment of irritable bowel syndrome (IBS) and/or prevention of migraine. [Means for Resolution] It was found that an acylguanidine derivati...

[Problem] To provide a compound which is useful as a GK activator. [Means for Resolution] As a result of an extensive study on thiazole derivatives, the present inventors have found that a compound having an oxamoyl group, a glycol group or the like on a thiazole ring and a compound having an acetamide group substit...

A pyridazinone derivative compound shown by the following formula (I): wherein R1 is selected from hydrogen, etc.; R2 is selected from substituted or unsubstituted aryl, etc.; R3 is hydrogen, etc.;p is 0,1 or 2; R4 and R5 are each hydrogen, etc.; R6 and R7 are taken together to form a group of the formula: wherei...

ABSTRACT Problem: To provide compounds which have an anticoagulation effect based on their ability to inhibit the activated blood coagulation factor X and are useful as coagulation inhibitors or agents for prevention or treatment for diseases caused by thrombi or emboli. Means for Solution: Benzene derivatives o...

[Problem] To provide a pharmaceutical, particularly a compound which can be used as an insulin secretion promoter or a preventive or therapeutic agent for diabetes mellitus and the like diseases in which GPR40 is concerned. [Means for resolution] It was found that novel carboxylic acid derivatives or salts there...

The present invention provides a method for producing a C-glycoside derivative, which can produce the C-glycoside derivative at a high yield and at a low cost, which conforms to environmental protection, and which is applicable industrially. The C-glycoside derivative is useful for treating and preventing diabetes ...

112 ABSTRACT A compound having the following formula (I): wherein R1 is hydrogen, optionally substituted lower alJcyl, cyclo(lower)alkyl, cyclo(higher)alkyl, optionally substituted aryl, optionally substituted heterocyclyl, or aryl-fused cyclo(lower)alkyl, R1 is hydrogen or halogen, 2 is CH or N, R1 is ...

There is provided a pharmaceutical drug, particularly a novel compound useful for prophylaxis or a therapeutic treatment of various diseases involving infections with viruses of the herpesvirus family, specifically various herpesvirus infections such as varicella (chicken pox) via varicella zoster virus, varicella ...

It is intended to provide a novel agent for promoting the recovery from dysfunction after the onset of a central neurological disease or an agent for enhancing and/or promoting the effect of rehabilitation for functional recovery. Namely, an agent for promoting the recovery from dysfunction after the onset of a cent...

A novel process for the production of isoquinoline derivatives having inhibitory activity against current If; novel benzamide derivatives or salts thereof which are to be used in the process; and a process for the production of the bcnzamidc derivatives or the salts.

There is provided a novel pyrrolidine derivative represented by the formula (I) or a salt thereof having an excellent DPP-IV inhibitory activity and an excellent pharmacokinetic.  On the basis of the action as such, the compound of the present invention is useful for treatment and/or prevention of insulin-dependent ...

The present invention provides marked results in that it is possible to present by a simple method a dry powder inhalation for pulmonary delivery that is made from a biologically active substance in crystal from and a biocompatible, electrostatic aggregation-inhibiting substance and that has excellent safety, stabil...

The present invention relates to enteric sustained-release fine particles of tamsulosin or its salt that can be contained in tablets that disintegrate in the buccal cavity and a manufacturing method thereof. In further detail, the present invention relates to enteric sustained-release fine particles for tablets that...

The present invention relates to a. novel 2-phenylpyridine derivative or a salt thereof, wherein the pyridine ring is substituted with a carboxyl group or the like and the benzene ring has an electron-withdrawing group such as a cyano group and an electron-donating group such as a substituted alfcoxy group at the sa...

The present invention provides a compound having an excellent JAK3 inhibition activity and being useful as an active ingredient of an agent for treating and/or preventing various immune diseases including autoimmune diseases inflammatory diseases, and allergic diseases. As a result of studies on a novel condensed...

This invention relates to novel N-hydroxyacrylamide compounds and pharmaceutically acceptable salts thereof. More particularly, it relates to novel N-hydroxyacrylamide compounds and pharmaceutically acceptable salts thereof which act as a HDAC inhibitor, to a pharmaceutical composition comprising the same and to a m...

Crystal of 4, 6-dimethyl-4'-[3, 5-bis (trifluoromethyl)-] H-pyrazol-1 -yl]nicotinanilide having an excellent calcium release-dependent calcium channel inhibitory effect and an excellent IL-2 production inhibitory activity are obtained. It is found out that this compound occurs in two crystal polymorphisms both ...

[Problem] To provide a compound which may be used in treating diseases in which 11 p-hydroxysteroid dehydrogenase type 1 (1 lp-HSDl) is concerned, especially diabetes and insulin resistance. [Means for Solution] It was found that a triazole derivative or a pharmaceutically acceptable salt thereof, in which th...

The present invention provides a pharmaceutical composition useful as a therapeutic agent for fatty liver disease. A pharmaceutical composition, which comprises (1S)-1,5- anhydro-1-[5-(azulen-2-ylmethyl)-2-hydroxyphenyl]-D-glucitol or a pharmaceutically acceptable salt thereof, (1S)-1,5-anhydro-1-[3-(1-benzothiop...

A pharmaceutical composition for use in solid formulation, the composition containing crystalline and amorphous solifenacin or a crystalline and amorphous salt thereof, together with an inhibitor of amorphous preparation.

ABSTRACT To provide a useful compound as an active ingredient for a preventing and/or treating agent for rejection in the transplantation of an organ, bone marrow, or a tissue, an autoimmune disease, or the like, which has an excellent SIP1 agonist activity. [Means for solving] Since the compound of the invention ...

ABSTRACT Provided is an agent for treating or preventing urinary frequency, urinary urgency and urinary, incontinence which are associated with overactive bladder, a lower urinary tract disease such as interstitial cystitis and chronic prostatitis accompanied by lower urinary tract pain, and various diseases accomp...

ABSTRACT [Abstract] [Problem] A compound which can be used as a pharmaceutical, particularly a insulin secretion promoter or a agent for preventing/treating disease in which GPR40 is concerned such as diabetes or the like is provided. [Means for resolution] It was found that an oxadiazolidinedione compound which i...

[Problems]  A compound, which is useful as an active ingredient of a pharmaceutical composition, for example, a pharmaceutical composition for treating chronic renal failure and/or diabetic nephropathy, is provided. [Solving Means]  The present inventors have conducted extensive studies on a compound having an EP4 ...

Abstract An object of the present invention is to provide an agent for treating or preventing digestive ulcer that is effective even to ulcer of small intestine and others, for which gastric acid secretion inhibitors such as proton pump inhibitors are ineffective, and is superior to allopurinol in the efficaciousne...

{R)-2-(2-aminothiazol-4-yl}-4' -[2-((2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide or its salt shows a potent bladder relaxation effect in "isolated rat bladder smooth muscle relaxation test", dose-dependently lowers the contraction frequency of rhythmic bladder contractions in "rat rhythmic bladder contra...

ABSTRACT [Abstract] [Problem] To provide a compound which can be used for the prevention and/or treatment of diseases in which 5-HT2B receptor and S-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS). [Means for Resolution] It was found that an amide derivative characte...

To provide a novel and excellent method for treating and/or preventing prostatic cancer, benign prostatic hyperplasia, acne, seborrhea, hirsutism, baldness, alopecia, precocious puberty, adrenal hypertrophy, polycystic ovary syndrome, breast cancer, lung cancer, endometriosis, leiomyoma and the like based on selecti...

To provide a compound which is useful as an NMDA receptor antagonist. [Means for solution]  The present inventors have studied a compound having an NMDA receptor antagonistic action, and confirmed that the fused indane compound of the present invention has an excellent NMDA receptor antagonistic action, thereby ...

A pharmaceutical composition for oral administration, comprising 3-hydroxy-N1- ( 4-methoxybenzoyl) -N2- [4- (4-methyl- 1, 4-diazepan-l-yl) benzoyl]-1, 2-phenylenediami.ne or a pharmaceutically acceptable salt thereof, and hydroxypropyl cellulose having a viscosity of approximately 6 mPa-S (inclusive) to approximatel...

ABSTRACT [Abstract] [Problem] To provide a compound which may be used for the prevention and/or treatment of diseases in which S-HT2b receptor and 5-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS). [Means for Resolution] It was found that a pyrrole derivative characteriz...

To provide a compound having an excellent inhibitory effect on platelet aggregation. [MEANS FOR SOLVING PROBLEMS] Disclosed is a quinolone derivative having a lower alkyl, a cycloalkyl or the like at the 1-position; -N(R0)C(O)-lower alkylene-CO2R0, a lower alkylene-CO2R0, a lower alkenylene-CO2R0, -O-lower alkenylen...

A cocrystal of (1S)-1, 5-anhydro-1-[3-(1-benzothien-2-ylmethyl)-4-fluorophenyl]-D-glucitol and L-proline. It is a cocrystal of known compound A, which has a constant quality, is superior in storage stability, has no moisture absorptivity, and is suitable as a crystal of a drug substance used for preparing pharmace...

The present invention is useful for providing an excellent pharmaceutical composition for prevention and/or treatment of schizophrenia, containing a BEC1 potassium channel inhibitor or a pharmaceutically acceptable salt thereof as an active ingredient, and is particularly useful for providing a pharmaceutical c...

The present invention relates to a pharmaceutical composition for oral administration comprising a modified release portion containing tamsulosin or a pharmaceutically acceptable salt thereof, and an immediate release portion containing solifenacin or a pharmaceutically acceptable salt thereof and a hydrophilic subs...

A compound represented by the formula (I): wherein R1 is lower alkyl, cycloalkyl or aromatic hydrocarbon ring, each of which is optionally substituted with one or more substituents; R2 is hydrogen atom, halogen atom, lower alkyl, halo(lower)alkyl or lower alkoxy; and R3 is (1) a group represented by the for...

Provided is a compound useful as an N-type Ca2+ channel blocker. As a result of intensive studies of compounds having an action of blocking N-type Ca2+ channels, the present inventors found that a tetrahydroisoquinoline compound of the present invention having a substituent at the 1 -position has an action of bloc...

The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases. [Means for Solution] The present inventors have conducted intensive studies on a compound having...

Provided are compounds which are an NMDA antagonist having a broad safety margin and are useful as a treating agent or a preventing agent for Alzheimer"s disease, cerebrovascular dementia, Parkinson"s disease, ischemic apoplexy, pain, etc. Concretely provided are an amine derivative or its salt characterized in that...

A compound of the formula (I): wherein R1 is hydrogen or lower alkyl; R2 is lower alkyl, etc.; R3 is lower alkoxy, etc.; R4 is hydroxy, etc.; X is 0, S, etc.; Y is CH or N; Z is lower alkylene or lower alkenylene; anc m is 0 or 1; or salts thereof, which are useful as a medicament. ...

The 1-(2-methoxyethyl)-2-methyl-4,9-dioxo-3-(pyrazin-2-ylmethyl)-4,9-dihydro-lH-naphtho[2,3-d] imidazol-3-ium bromide of the invention and its crystals, particularly a-and p-form Crystals, have no hygroscopic property, have excellent stability and therefore are useful as production materials of medicines. Particular...

This invention relates to a novel fluorene derivative having a characteristic structure in which guanidino group or the like functional group is linked to the fluorene structure via carbonyl group, or a salt thereof. The compound of the invention has an advantage in that it has high affinity for serotonin receptor...

The present invention relates to an antibacterial agent for Propionibacterium acnes containing, as an active ingredient, a peptide represented by the formula [I]: or a pharmaceutically acceptable salt thereof.

The pyrazine compound (I) and a salt thereof of the present invention are adenosine antagonists and are useful for the prevention and/or treatment of depression, dementia (e.g. Alzheimer"s disease, cerebrovascular dementia, dementia accompanying Parkinson"s disease,, etc.), Parkinson"s disease, anxiety, pain, cerebr...

This invention relates to a method for preventing and/or treating bone diseases which comprises administering a potentiator of TGF-beta activity such as the compound of the formula 11 ] or pharmaceutically acceptable salts thereof to human being or animals. wherein RJ is hydrogen, etc., R2 is optionally substitut...

The present invention relates to a compound formula (I): wherein (II) is (III) or (IV), X is bond, -CH2-, -O- or -NH-, R1 and R12 are each independently hydrogen, halogen, lower alkyl, etc., R2 is hydrogen or optionally substituted lower alkyl, R3 is hydrogen or an amino protective group, R4, R5 and R6 are each inde...

Ornithine derivatives of the formula (I): wherein X is -CO- or -(CH2) k- (wherein k is 1, 2 or 3); Y is Z-(CH2) n-, and the like; {wherein Z is R1-CO-NR4-, and the like, (wherein R1 is aryl, and the like; and R4 is hydrogen, or lower alkyl); and n is 1, 2, 3, 4, 5 or 6}; R2 is aryl-(lower alkyl), and the l...

Novel tetrahydroisoquinoline derivative compounds are disclosed herein that may be used as an active ingredient for a pharmaceutical composition and in particular for a pharmaceutical composition useful for preventing or treating a disease or condition responsive to modulation of the contractility of the skeletal sa...

Tablets quickly disintegrating in the oral cavity which contain a drug, a diluent and a saccharide having a melting point lower than the melting points of the drug and the diluent, wherein the low-melting saccharide is uniformly dispersed in the tablets and crosslinkage of the low-melting saccharide, which has been ...

A solid pharmaceutical preparation of solifenacin or a salt thereof, the preparation being stable and inhibited from decomposing with time when supplied to clinical fields. In a pharmaceutical preparation containing solifenacin or a salt thereof, the compound in an amorphous form was revealed to be causative of card...

An antiobesity agent, an antidiabetic agent, and/or a hypolipidemic agent comprising an angiopoietin-related growth factor (AGF) or a polynucleotide encoding the same as an active ingredient a polypeptide are disclosed. Further, a functional food or a health food for alleviating obesity, diabetes, and/or hyperlipemi...

The invention relates to a compound useful as remedies or preventives fot lKK2-related inflammatory diseases or autoimmune diseases, or that is, a 2-aminopyrimidine derivative having a 2-hydroxyphenyl group at the 6-position thereof and having a saturated cyclic group that contains one nitrogen atom, such as piperid...

[Problem] To provide compounds useful as GnRH receptor antagonists. [Means for Resolution] The inventors have further examined propane-1,3-dione derivatives and confirmed as a result that a propane-1,3-dione having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene), or a compound having 2-(1,3-dihydro-...

A particle size-controlling substance containing a ding, polyethylene oxide having a molecular weight of 2,000,000 or more and a particle size-controlling agent (a substance having appropriate plasticizing properties and binding force) for the polyethylene oxide wherein at least the particle size-controlling agent ...

A compound of the formula (I) or a pharmaceutically acceptable salt thereof: [wherein X1 and X2 each is independently lower alkylene; X3 is =CH2, =CHF or =CF2; R1 is substituent, R2 and R3 each is independently H or lower alkyl; n is 0, 1, 2, 3 or 4.] having the activity inhibiting DPP-IV activity. They are therefor...

An agent for treating eye and mouth dryness, which does not accompanies undesirable actions is provided. [Means for Resolution] Administration of the compound A made it possible to accelerate tear and salivary fluid secretion without administration enabled acceleration of lacrimal gland and salivary gland cell...

ABSTRACT [Abstract] [Object] A compound that can be used as an agent for treating a disease associated with an EP1 receptor, in particular, a lower urinary tract symptom. [Means for Solution] It was confirmed that a sulfonamide compound having an amide structure and characterized by a chemical structure i...

[Problem] A compound useful for the prevention and/or treatment of chronic obstructive pulmonary disease (COPD) or asthma, and a pharmaceutical composition containing the compound as an active ingredient are provided. [Means for Solution] The present inventors have made extensive studies on the pharmacological a...

Provided is a compound which is useful as a therapeutic agent for chronic rena insufficiency and a therapeutic agent for diabetic nephropathy. The present inventors have made extensive studies on an ornithine derivative having an antagonistic action against an EP4 receptor, and as a result, they have found that by ...

A compound of the formula (I): wherein R1 is cycloalkyl, etc; R2 is (lower)alkoxy, etc; R3 is (lower)alkylene, etc; R4 is (lower)alkylene, etc; R5 is hydroxy, etc; X is '0', 'S', 'SO', or 'S02'; Y is 'CH' or 'N'; n is 0 or 1; or pharmaceutically acceptable salts thereof, which are useful as a medicament. ...

2[Problem] There have been demands for a therapeutic method that increases the medicinal effects of taxane based antitumor agents on various tumors. [Solution] As a result of researches for a method for enhancing the antitumor effects of taxane based antitumor agents the inventors have achieved the present inventio...

The present invention relates to a new cyclic peptide compound or a salt thereof, which has anti-hepatitis C virus activities based on inhibitory activity against the RNA replication of hepatitis C virus replicon, a process for preparation thereof, a pharmaceutical composition comprising the same, and a method for p...

[Problem] To provide: an anti human NGF antibody which is reduced in the influence on fetuses and the risk of adverse side effects including thrombosis while keeping a high neutralizing activity and which has excellent safety or an antigen binding fragment thereof; and a means for preventing or treating various dise...

To provide novel crystals useful as an ingredient for the production of a diabetes remedy. The invention is concerned with α-form crystal and β-form crystal of (R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenyleth- yl)amino]ethyl]acetanilide. The α-form crystal does not exhibit hygroscopicity and has stabil...

An object of the present invention is to provide a novel and excellent agent for treating or preventing dementia, schizophrenia and the like, based on the 5-HT5A receptor modulating action.  It was confirmed that a compound characterized by a structure that a tricyclic hetero ring having a pyrrole ring at the center...

[Problems]  To provide an antibacterial agent, particularly a novel polypeptide compound having an antifungal action. [Means for Solution] As a result of an extensive study on a novel antifungal agent, the inventors have found that an excellent anti-deep-fungal activity is exhibited by introducing a cyclohexylmethy...

The invention relates to compound of the formula (I) or its salt, in which R1, R2, R3 and R4 are as defined in the description, their use of as medicament, the process for their preparation and use for the treatment of PDE-IV or TNF-a mediated diseases.

The present invention relates to the provision of a stable particulate pharmaceutical composition of solifenacin or a salt thereof, which is in a spherical shape suitable for coating and in which degradation with time can be inhibited when a pharmaceutical preparation of solifenacin or a salt thereof is supplie...

[Problem] To provide a labeled fatty acid derivative for imaging diagnosis that enables quantification of fatty acid metabolic activity in the heart muscle. [Solution] As the results of intensive studies on a method enabling quantification of fatty acid metabolic activity, the present inventors found that a labeled ...

[Problem] To provide a pharmaceutical composition for treating FGFR4 related cancer FGF19 related cancer or FGF19 gene amplification positive liver cancer. [Solution] The inventors perfected the present invention through study of compounds having FGFR4 inhibitory effect verifying that specific pyrimidine compounds h...

[Problem] To provide an anti human TSLP receptor antibody for specifically bonding to the human TSLP receptor and blocking the effect of human TSLP receptor mediated human TSLP. [Solution] The present inventors studied the anti human TSLP receptor antibody and have provided an anti human TSLP receptor antibody that ...

A novel 4,4-difluoro-l,2,3,4-tetrahydro-5H-l-benzazepine derivative or a pharmaceutically acceptable salt thereof, which is useful as an agent for treating or preventing nocturia and/or diabetes insipidus, is provided.

The present invention relates to compound of the formula (I) or its salt, in which R1 R2, R3 and R4 are as defined in the description, and to the process for their preparation.

1234YL[Problem] To provide a compound useful as a pharmaceutical composition for prevention and/or treatment of diseases such as schizophrenia. [Solution] The inventors developed the present invention upon investigating a pharmaceutical composition having effects as a GABAB positive allosteric modulator (effects as ...

The inventors perfected the present invention as a result of a study into IK1 channel activators and a confirmation that a benzothiophene compound exhibits efficacy against visceral pain inflammatory pain osteoarthritic pain neuropathic pain or fibromyalgia. This compound represented by formula (I) has IK1 channel a...

[Problem] To provide a compound which is useful as an active ingredient of a pharmaceutical composition especially of a pharmaceutical composition for the prophylaxis and/or treatment of VAP 1 associated diseases. [Solution] As a result of intensive studies on a compound having VAP 1 inhibitory activity the invento...

The present invention provides a combination therapy comprising an anti-Claudin (CLDN) 18.2 antibody and an immune checkpoint inhibitor for effectively treating and/or preventing diseases associated with cells expressing CLDN18.2, including cancer diseases such as gastric cancer, esophageal cancer, pancreatic cancer...

Polynucleotides comprising the following base sequences: (a) a base sequence encoding a fusion protein of a nuclease-deficient CRISPR effector protein and a transcriptional repressor, and (b) a base sequence encoding a guide RNA targeting a continuous region of 18 to 24 nucleotides in length in a region set forth in...

A sustained-release formulation comprising a solid dispersion composition, wherein the solid dispersion composition comprises tacrolimus or its hydrate, in a mixture comprising a water-soluble polymer and a water-insoluble polymer, and an excipient.

This invention relates to a compound of the formula;

The invention relates to implants, in particular intracavernous or intravascular, preferably for the treatment or prophylaxis of coronary or peripheral vascular constrictions or vascular occlusions, in particular of constrictions and stenoses or restenoses, preferably for the prophylaxis of restenosis, which...

4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepine derivatives, whichhave excellent arginine vasopressin V2 activity and are useful for a drug forthe treatment of central diabetes insipidus and/or nocturia.

The present invention provides marked results in that it is possible to present by asimple method a dry powder inhalation for pulmonary delivery that is made from abiologically active substance in crystal form and a biocompatible, electrostaticaggregation-inhibiting substance and that has e...

A 2-acylaminothiazole derivative or a pharmaceutically acceptable salt thereof having an excellent effect of proliferating human c-mpl-Ba/F3 cells and an activity of increasing platelets based on the effect of promoting the formation of megakaryocytic colonies. A compound or a pharmaceutically acceptable sal...

A 2,4,6-triamine-1,3,5-triazine represented by formula (II) or apharmaceutically acceptable salt thereof (symbols in the formula are as followsR1:HR2: a hydrocarbon radical which is lower alkyl, and which may besubstituted with substituents from a hetero ring which is a gr...

A pharmaceutical composition for the treatment of glioblastoma comprising 2-[N-(4-chlorophenyl)-N-methylamino]-4H-pyrido[3,2-e]-1,3-thiazin-4-one or 7-Acetyl-5-(4-aminophenyl)-8(R)-methyl-8,9-dihydro-7H-1,3:dioxolo[4,5-h][2,3]benzodiazepine(Talampanel).

The present invention provides an azulene derivative anda salt thereof, wherein an azulene ring is bonded to a benzenering directly or via a lower alkylene which may be substitutedwith a halogen atom and the benzene ring is directly bonded tothe glucose residue, and it is usable as a ...

There are provided novel crystals of (-)-N-{2-[(R)-3-(6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline-2-carbonyl) piperidino]ethyl}-4-fluorobenzamide monophosphate.

The invention provides a novel nitrogen-containing heterocyclic derivativehaving 2,6-disubstituted styryl and a pharmaceutically acceptable salt thereof, and apharmaceutical composition comprising the nitrogen-containing heterocyclicderivative and a pharmaceutically acceptable salt thereof,...

The present invention provides C-glycoside derivatives andsalts thereof, wherein B ring is bonded to A ring via -X- and A ringis directly bonded to the glucose residue, and it is usable as aand/or preventive agent for diabetes such as insulin-dependentdiabetes), as well as diabetes re...

A compound having the following formula (I): wherein R 1< is N-containing heterocyclic ring optionally substituted with one or more suitable substituent(s), R 2? is hydroxyamino, R 3? is hydrogen or a suitable substituent, L 1? is -(CH?2#191)?n#191- (wherein n is an integer of 0 to 6) optionally substituted with one...

The present invention is to provide a therapeutic agent for attention deficit/hyperactivity disorder having a novel mechanism of action which is different from conventional psychostimulants. The present invention is useful for providing an excellent pharmaceutical composition for prevention and/or treatment of at...

Disclosed is a compound useful as an active ingredient for medicines having PDE4B inhibiting activity in particular therapeutic or preventive medicinal compositions for schizophrenia Alzheimer s disease dementia depression and the like. Specifically the present inventors examined compounds having PDE4B inhibiting ac...

[Problem] To provide: a novel method for producing a pyrazine carboxamide compound as a production material of pharmaceutical products etc.; and a synthetic intermediate that is useful in said production method. [Solution] As a result of diligent research on production methods in industrially producing a pyrazine ca...

[Problem] To provide a compound useful as a cathepsin S inhibitor. [Solution] The present inventors have studied on a compound which has a cathepsin S-inhibiting activity and can be used as an active ingredient for a pharmaceutical composition for preventing and/or treating an autoimmune disease such as systemic lu...

[Problem] To provide an anti-human MUC1 antibody Fab fragment which is expected to be useful for the diagnosis and/or treatment of cancer particularly the diagnosis and/or treatment of breast cancer or bladder cancer and a diagnosis means and/or a therapeutic means using a complex containing the Fab fragment. [Solut...

[Problem] To provide a compound that is useful as an active ingredient of a pharmaceutical composition for the treatment of lung cancer. [Solution] The present inventors examined compounds that are useful as an active ingredient of a pharmaceutical composition for the treatment of lung cancer and found that a quinaz...

The purpose of the present invention is to provide: an anti-human CEACAM5 antibody Fab fragment which is expected as useful in diagnosing cancer, in particular, colon cancer, breast cancer, lung cancer, thyroid cancer or cancer metastasized therefrom; and a diagnostic means wherein a conjugate comprising the Fab fra...

The invention relates to antibodies directed against an epitope located within the C-terminal portion of CLDN6 which are useful, for example, in diagnosing cancer and/or in determining whether cancer cells express CLDN6.

[Problem] To provide a nucleic acid expected to be useful in treating crustacean allergy. [Solution] Provided is a nucleic acid including, in the following order: a base sequence that encodes a signal peptide; a base sequence that encodes a LAMP intra-organelle stabilizing domain; a base sequence that encodes an all...

[Problem] To provide an anti-human Fn14 antibody that binds to human Fn14 and blocks action mediated through human Fn14 to prevent or treat cancer cachexia. [Solution] The present inventors conducted research on anti-human Fn14 antibodies, and have provided an anti-human Fn14 antibody including a heavy chain having ...

[Problem] To provide a complex comprising a ligand, spacer, and peptide linker useful in internal diagnostics and internal radiation therapy that uses an anti-human MUC1 antibody Fab fragment the binding activity of which is not weakened even by labeling by a metal, fluorescent dye, or the like. [Solution] A complex...

[Problem] To provide a complex comprising a ligand, a spacer, and a peptide linker useful in internal diagnostics and internal radiation therapy, that uses an anti-human CEACAM5 antibody Fab fragment the binding activity of which is not weakened even by labeling with a metal, fluorescent dye, or the like. [Solution]...

The present invention provides pharmaceutical compositions comprising an oncolytic vaccinia virus and methods of using such pharmaceutical compositions for treating a subject having a cancer.

Provided is a method for treating or preventing cancer safely and effectively using aAVC. Suitable ranges for the dose of a-GalCer loaded on the surface of aAVC cells preferred from the viewpoint of ensuring safety and efficacy in the treatment and prevention of cancer using aAVC and the amount of a-GalCer loaded on...

The present invention addresses the problem of providing an aAVC-NY-ESO-1 cell, which stably expresses NY-ESO-1 and is clinically applicable, in order to use the aAVC-NY-ESO-1 cell to treat a patient with NY-ESO-1 expressing cancer. The present invention provides a human-derived cell including, for example, a polynu...

Problem: Providing antisense guide RNA for editing target RNA by ADAR. Solution: Antisense guide RNA, for editing target RNA by ADAR, wherein: at least one functional region and an antisense region that is complementary to part of the target RNA and forms a double strand with the target RNA are included; and the at ...

[Problem] To provide a labeled fatty acid derivative for diagnostic imaging that enables the quantification of myocardial fatty acid metabolic activity. [Solution] The inventors, engaging in diligent research into methods that enable the quantification of fatty acid metabolic activity, discovered that a labeled fatt...

Provided is a compound that is useful as an active ingredient of a medicinal composition for treating cancer related to immunocyte activation or cancer resistant to anti-PD-1 antibody/anti-PD-L1 antibody therapy. The present inventors studied compounds being useful as an active ingredient of a medicinal composition ...

The present invention addresses the problem of providing an anti-TSPAN8-anti-CD3 bispecific antibody and an anti-TSPAN8 antibody each of which can be used for treatment or prevention in human bodies. A human-monoclonal-antibody-producing mouse is immunized with a cancer peritoneal dissemination cell isolated from a ...

Provided is a compound which is useful as an active ingredient for a pharmaceutical composition for treating cancer associated with the activation of an immunocyte or cancer having resistance to an anti-PD-1 antibody/anti-PD-L1 antibody therapy. The present inventors have studied about a compound useful as an active...

The present invention provides a polypeptide comprising a modified Fc region of an IgG, and a modified Fcy receptor that binds specifically to the polypeptide, and methods for treating or preventing a disease or a disorder in a patient using immunotherapy.

ABSTRACT"AMINOALCOHOL DERIVATIVES"3030/CHENP/2004A compound, of the formula [Ih]or a pharmaceutically acceptable salt thereof. Z is car boxy or C1-C6 alkoxycarbonyl,R1 is hydrogen, halogen or hydroxy,R2 is hydrogen,R3 is hydrogen or C1-C6 alkyl,R4 is hydr...

[PROBLEMS]  Provided is a compound which has an antagonistic action on a muscarinic M3 receptor and is useful as an active ingredient of a prophylactic and/or therapeutic agent for an inflammatory disease such as a chronic obstructive pulmonary disease (COPD), asthma and the like. [MEANS FOR SOLVING PROBLEMS]  The ...

[Problem] To provide: a medicinal composition for treating an AXL related cancer; in another embodiment a medicinal composition for treating a cancer with high expression of AXL; and in still another embodiment a medicinal composition for treating a cancer that has acquired resistance through activation of AXL ag...

To provide a superior anti-human NGF antibody Fab fragment that maintains a high neutralizing activity, and that reduces systemic side-effects arising from systemic exposure while expressing a local drug effect, and means for treating postoperative pain by using such antibody fragment An anti-human NGF antibody ...

[Technical Problem] The present invention provides a genetically recombinant vaccinia virus effective in preventing or treating cancer. [Solution to Problem]   Specifically, the present invention provides a vaccinia virus comprising two polynucleotides, a polynucleotide encoding IL-7 and a polynucleotide encoding I...

[Problem] To provide a nucleic acid expected to be useful in treating mite allergy. [Solution] Provided is a nucleic acid including, in the following order: a base sequence that encodes a signal peptide; a base sequence that encodes an LAMP intra-organelle stabilizing domain; a base sequence that encodes an allergen...

Polynucleotides comprising the following base sequences: (a) a base sequence encoding a fusion protein of a nuclease-deficient CRISPR effector protein and a transcription activator, and (b) a base sequence encoding a guide RNA targeting a continuous region of 18 to 24 nucleotides in length in a region set forth in S...

[Problem] To provide a novel method for producing nanoparticles which include metal particles containing iron oxide having at least one hydrophilic ligand coordinated thereto, and are useful as a contrast agent for magnetic resonance imaging. [Solution] The present invention provides a novel method for producing nan...

Provided are: a novel nanoparticle; a contrast agent for magnetic resonance imaging comprising the same; and a zwitterionic ligand compound to be used in the production of the nanoparticle. The contrast agent for MRI according to the present invention is appropriately usable as a contrast agent for MRI in the medica...

[Problem] To provide a compound useful as an active ingredient of a pharmaceutical composition for treating pancreatic cancer. [Solution] The present inventors have examined a compound useful as an active ingredient of a pharmaceutical composition for treating pancreatic cancer, and have found that a quinazoline com...

The present invention has an object to provide a pharmaceutical composition for treating a cancer of colorectal cancer and/or lung cancer. The present inventors have studied about a compound that is useful as an active ingredient of a pharmaceutical composition for treating a cancer, and have found that a quinazolin...

The present invention addresses the problem of providing a pharmaceutical composition, in particular, a compound suitable for preventing and/or treating inflammatory diseases and/or neurodegenerative diseases. The present inventors have conducted an intensive examination to search for a compound having an NLRP3 infl...

The present invention addresses the problem of providing an anti-CLDN4/anti-CD137 bispecific antibody that can be used in treating cancer. This anti-CLDN4/anti-CD137 bispecific antibody, which is manufactured using an anti-CLDN4 antibody that binds to CLDN4 and an anti-CD137 antibody that binds to CD137, has an agon...

The present invention provides a combination therapy for treating and/or preventing diseases associated with cells expressing CLDN18.2, including cancer diseases such as gastric cancer, esophageal cancer, pancreatic cancer, lung cancer, ovarian cancer, colon cancer, hepatic cancer, head-neck cancer, and cancer of th...

To provide a compound useful as an active ingredient of a pharmaceutical composition for treating pancreatic cancer. The present inventors have examined compounds useful as an active ingredient of a pharmaceutical composition for treating pancreatic cancer and have found that a heterocyclic compounds represented by ...

A compound which is useful as a STING inhibitor is provided. The present inventors have found aryl alkynamide derivatives having an inhibitory action on STING. The aryl alkynamide derivatives of the present invention have an inhibitory action on STING and can be used as an agent for treating an autoimmune disease, a...

Provided is a compound useful as an active ingredient in a pharmaceutical composition for treating pancreatic cancer. The present inventors carried out investigations with regard to compounds useful as an active ingredient in a pharmaceutical composition for treating pancreatic cancer and have found that a heterocyc...

The present invention relates to: a method for producing a non-human primate model of cerebral infarction, said method including administering an endothelin to the cerebral basal ganglia and thalamic area of a non-human primate and thus inducing cerebral basal ganglia damage, thalamic damage and internal capsule dam...

Provided is a compound that is effective as an active ingredient in a therapeutic pharmaceutical composition for pancreatic cancer. Having studied compounds that are effective as active ingredients in a therapeutic pharmaceutical composition for pancreatic cancer, the inventors found that the heterocyclic compound s...

There is provided herein a combination of compound of formula (I) which is a bifunctional compound with G12D mutant KRAS inhibitory activity or a pharmaceutically acceptable salt thereof and an anti cancer agent for use in the treatment of cancer wherein the compound of formula (I) and the anti cancer agent are ...

There is provided herein a combination of a compound of formula (I) or a pharmaceutically acceptable salt thereof and an anti cancer agent for use in the treatment of cancer wherein the compound of formula (I) and the anti cancer agent are as described in the description.

The present invention addresses the problem of developing an antibody-drug complex containing a TLR7/8 dual agonist compound or a salt thereof to provide a pharmaceutical composition used for the prevention or treatment of various types of cancer. The present inventors have discovered a compound having a TLR7/8 dual...

There is provided herein compounds of formula (I), (XXI), (XXII) and (XXIII) as defined herein, and salts thereof, for use in the treatment of colorectal and/or lung cancer.