Compounds of formula (I), wherein R1 to R8 A, B, Z1 and Z2 are as defined in the claims and pharmaceutically acceptable salts and esters thereof are disclosed. The compounds of formula (I) possess utility as androgen receptor antagonists (inhibitors) and/or cytochrome P450 monooxygenase 17a-hydroxylase/17,20-lyase (...

A compound of formula (I), wherein R1 to R5, A, B, Z, Z1 and Z2 are as defined in the claims, and pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (I) possess utility as FGFR inhibitors and are useful in the treatment of a condition, where FGFR kinase inhibition is desired, such as c...

The present invention relates to novel prodrugs of MPV-2426, to methods for preparing said pradrug forms, to pharmaceutical compositions containing such prodrug forms, and to methods for using the prodrug forms. A compound of general formula (1), or pharmaceutically acceptable salts or hydrates thereo...

The present invention relates to E-2-[4-(4-chloro-1,2-dipheny1-but-1-eny1)phenpxy] ethanol useful in lowering serum cholesterol and to pharmaceutical compositions thereof . A method of lowering of lowering serum cholesterol and a method and a method for the prevention or treatment of anther sclerosis is also disclos...

The present invention relaes to a pyndazinyl derivative (I) and use as a reference compound in the Jetermination of potentially genotoxic impurities in levosimendan samples. The invention also relates to an analytic method for the determintion of potentially genotoxic impurities in levosimendan samples wherein (I) ...

Compounds of formula (I), wherein R1-R4, X, Y and Z are as defined in claims, exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors.

34A compound of formula (I) wherein R R G B M and Z are as defined in the claims and pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (I) possess utility as FGFR inhibitors and are useful in the treatment of a condition where FGFR kinase inhibition is desired such as cancer. ...

Compounds of formula I, wherein A, B, X, Z and R1-R6, are as defined in the claims, exhibit TRPA 1 activity and are thus useful as TRPA1 modulators.

The present invention provides novel spiro[cyclobutane-1,3"-indolin]-2"-one derivatives of formula (I) in which Cy,R1, R2, L and "m" are have the meaning given in the specification, and pharmaceutically acceptable salts thereof. The compounds of formula (I) are useful as bromodomain inhibitors in the treatmen...

A compound of formula (I) wherein R1 to R5, A, B, Z, Z1 and Z2 are as defined in the claims, and pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (I) possess utility as FGFR inhibitors and are useful in the treatment of a condition, where FGFR kinase inhibition is desired, suc...

12341212The present invention provides bicyclic heterocyclic derivatives of formula (I) which may be therapeutically useful more particularly as bromodomain inhibitors; (I) in which R R R R L L Cy Cy X n and dotted line are have the same meaning given in the specification and pharmaceutically acceptable...

Compounds of formula (I) or (II) wherein Rx, Rz, R9, R10, R14, R14", R15, R15", A and B are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds possess utility as tissue-selective androgen receptor modulators (SARM) and are particularly useful as med...

Compounds of formula (I), wherein X, Z, A, B, D, E,R1-R4 and m are as defined in the claims, exhibit alpha2C an- tagonistic activity and are thus useful as alpha2C antagonists.

The invention relates to novel bicyclic heterocycle derivatives of formula (I) wherein Cy1, Cy2, R1, R2 and L1 have the meaning given in the specification, and pharmaceutically acceptable salts thereof. The compounds of formula (I) are useful as bromodomain inhibitors in the treatment or prevention of diseases...

Compounds of formula (I), wherein X and R 1-R , are as defined in the claims, exhibit alpha2 agonistic activity and thus useful as alpha2 agonists, especially as alpha2A agonists. Methods of use of said compounds are also provided.

The present invention relates to an improved process for the preparation of carboxamide structured androgen receptor (AR) antagonists such as N ((S) 1 (3 (3 chloro 4 cyanophenyl) 1H pyrazol 1 yl) propan 2 yl) 5 (1 hydroxyethyl) 1H pyrazole 3 carboxamide (1A) and key intermediates thereof such as 2 chloro 4 (IH pyraz...

A compound of formula (I) wherein R1 to R15, P1, P2, A, B and Q are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as matriptase inhibitors and are useful in the treatment of matriptase dependent conditions, particularl...

Compounds of formula (I) wherein Rx, Rz, R9, R10, R14, R14", R15, R15", A and B are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds possess utility as tissue-selective androgen receptor modulators (SARM) and are particularly useful as medicaments in the...

A compound of formula (I) wherein R1 to R5, A, B and Z are as defined in the claims and pharmaceutically acceptable salts thereof, are disclosed. The compounds of formula (I) possess utility as FGFR inhibitors and are useful in the treatment of a condition, where FGFR kinase inhibition is desired, such as can...

The invention provides a compound of formula I, wherein X, Z, R1 to R10, R15, R16, m, n, r and t are as defined in claim 1, or a pharmaceutically acceptable salt or ester thereof, useful as an alpha-2 antagonist. The compounds of formula I can be used for the treatment of diseases or conditions where antagonists of ...

A new process for manufacturing entacapone comprising reacting 3,4-dihydroxy-5-nitrobenzaIdehyde with N,N-di- ethyl-2-cyanoacetamide in the presence of a catalyst in a C 4 to 8 alcohol at reduced pressure and at a temperature of at least 70 °C, cooling i.he mixture to a temperature of 30 °C or below, seeding the m...

A compound of formula (I) wherein R1 to R15, P1, P2, A, B and Q are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as matriptase inhibitors and are useful in the treatment of matriptase dependent conditions, particularly...

Compounds of formula (I), wherein X, Z, R1-R4, and m are as defined in the claims, exhibit alpha2C antagonistic activity and are thus useful for the treatment of diseases and conditions of the peripheric system and the central nervous system (CNS).

N/A

The present invention relates to an oral compacted composition comprising entacapone, nitecapone, or a pharmaceutically acceptable salt thereof and a cross-linked cellulose derivative. The composition is premised on the discovery that the cross-linked cellulose derivative increases the release rate of entacapone or ...

The invention relates to levosimendan solutions for pharmaceutical use, and particularly for intravenous administration. The solutions of the invention have enhanced stability and they are particularly useful as infusion or injection solutions or infusion concentrates. Levosimendan is useful in the treatment of co...

Compounds of formula (I), wherein R1 is as defined in the claims, exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors.

Compounds of formula (I) wherein R1 to R16, A. B and E are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as tissue-selective androgen receptor modulators (SARM) and are particularly useful as medicaments in the treatmen...

The present invention relates to E-2-[4-(4-chloro-1,2-diphenyl-but-1-enyl)phenoxy]ethanol useful in lowering serum cholesteroland to pharmaceutical compositions thereof. A method of lowering serum cholesterol and a method for the prevention or treatment ofatherosclerosis is also disclosed. ...

Therapeutically active compounds of formula (I) in which R1 to R4 means hydrogen, alkyl, alkenyl, aryl, arylalkyl, carboxyalkyl, hydroxyalkyl or halogenalkyl, or R2 and R3 form a ring of 5-7 carbon atoms, R5 to R9 means hydrogen, alkyl, alkenyl, aryl, arylalkyl, acyl, hydroxy, alkoxy, alkoxycarbonyl, amino, ...

The present invention relates to a medical product comprising,separately or together, as active ingredients a thrombolytic agent and levosimendanor a pharmaceutically acceptable salt thereof as a combined preparation. Thecombination synergistically reduces mortality of patients with acute m...

The invention provides a compoundof formula I, wherein X, Z, R1 to R10, R15, R16, m, n,r and t are as defined in claim 1, or a pharmaceuticallyacceptable salt or ester thereof, useful as an alpha-2antagonist. The compounds of formula I can be used forthe treatment of diseases or...

There is disclosed a novel bioreversible ester prodrug of general formula I, or pharmaceutically acceptable salts or hydrates thereof, wherein R representsunsubstituted or substituted lower alkyl, unsubstituted or substituted aryl,unsubstituted or substituted cycloalkyl, unsubstituted...

Therapeuticallyactive compounds of formula (I)or (II) wherein X is -O-, -CH2-or -C(O)-; Z is -CHR12- or avalence bond; Y is -CH2-, -C(O)-,CH(OR13)-, -O-, -S-; provided thatin case Z is a valence bond, Y is notC(O); the dashed line representingan optional double...

The invention discloses prolyl oligopeptidase inhibitor compounds of formula (I)wherein in X is C; the dotted line represents a double bond; R1, R2, R3 and X are as defined inthe specification and pharmaceutical composition comprising them.

Compounds of formula I (formula I) wherein A is an optionally substituted five membered unsaturated heterocyclic ring containing 1 2 or 3 N O or S ring heteroatom(s) exhibit alpha2C antagonistic activity and are thus useful for the treatment of diseases or conditions of the peripheric or central nervous system. ...

Compounds of formula (I) wherein R1 R2R3R4R5R23R24L A and Bare as defined in claim 1 or pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (I) possess utility as cytochrome P450 monooxygenase 11A1(CYP11A1) inhibitors. The compounds are useful as medicaments in the treatment of steroidr...

The present invention relates to an improved process for the preparation of a sulfonamide structured kinase inhibitor namely N-(2"4"-difluoro-5-(5-(1-methyl-1H- pyrazol-4-yl)-1H-benzo[d]imidazol-1-yl)-[11"-biphenyl]-3-yl)cyclopropanesulfon- amide (1A) and pharmaceutically acceptable salts thereof. Compound of formul...

The present disclosure relates to an improved process for the preparation of isochroman structured alpha2A adrenoceptor agonist, namely 2-(5-methoxyisochroman-1-yl)-4,5- dihydro-1H-imidazole of formula (I) and a pharmaceutically acceptable salts thereof, such as 2-(5-methoxyisochroman-1-yl)-4,5-dihydro-1H-imidazole ...

The present disclosure relates to a process for the preparation of 4,5-dihydroxy-2-(4-methylbenzyl)isophthalonitrile, to use of a compound which is 2-methoxy-5-(4-methylbenzyl)phenol, (3-hydroxy-4-methoxyphenyl)(p-tolyl)methanone, 2-methoxy-5-(4-methylbenzoyl)phenyl 2-chloroacetate, 4-methylbenzoyl chloride, 2-metho...

Therapeutically activecompounds of formula (I): wherein Xis -O-, -CH2- or -C(O); Z is -CHR9-or valence bond; Y is -CH2-, -C(O)-,CH(OR10)-. -CH(NR11R12)-, -O-,-S-, -S(O)- or S(O2)-, provided thatin case Z is a valence bond, Y is notC(O); the dashed line represents an<...

Compounds of formula (I) wherein R1 to R4, X and A are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as tissue-selective androgen receptor modulators (SARM) and are useful in hormonal therapy, e.g. in the treatme...

Compounds of formula (I): wherein Ra and Rb are as defined in the claims, exhibit alpha2C antagonistic activity and are thus useful as alpha2C antagonists.

The present invention relates to an improved process for the preparation of a sulfonamide structured kinase inhibitor, namely N-(2',4'-difluoro-5-(5-(1-methyl-1H- pyrazol-4-yl)-1H-benzo[d]imidazol-1-yl)-[1,1'-biphenyl]-3-yl)cyclopropanesulfon- amide (1A) and pharmaceutically acceptable salts thereof. Compound of for...

The invention relates to the use of an activating AR gene alteration as a biomarker for identifying prostate cancer patients who have a higher probability to be responsive to the treatment with a CYP11A1 inhibitor. The invention also relates to a method for treating prostate cancer comprising a) obtaining or having ...

The present invention relates to an improved process for the preparation of 2-chloro-4-(1-(tetrahydro-2H-pyran-2-yl)-1H-pyrazol-5-yl)benzonitrile (III) which is useful as an intermediate in the preparation of carboxamide structured androgen receptor antagonists. The process comprises preparation of compound (III) us...

The present invention relates to novel salts, particularly crystalline salts, of 2-(isoindolin-2-ylmethyl)-5-((1-(methylsulfonyl)piperidin-4-yl)methoxy)-4H-pyran-4-one (I) which are particularly suitable for use in the manufacture of pharmaceutical 5 compositions. Furthermore, the invention relates to pharmaceutical...

The present invention relates to compounds of formula (I) wherein A is a 3-10 membered carbocyclyl or a 4-12 membered heterocyclyl containing 1-4 heteroatoms selected from O, N or S; B is any of the following groups (1) (2) or (3 ); C is any of the following groups (1') (2') (3") or (4') G1 is CH2, NH or O; G2 and G...

The present invention relates to an improved process for the preparation of 4H-pyranone structured CYP11A1 inhibitors such as 2-(isoindolin-2-ylmethyl)-5- (( 1 -(methylsulfonyl)piperidin-4-y l)methoxy)-4H-pyran-4-one (1A) and key intermediates thereof such as 2-(chloromethyl)-5-hydroxy-4H-pyran-4-one (II), 5- hydrox...

The present invention relates to a compound of formula (I) wherein A, Z, L, R1, R2, R3, R4, R5 and R33 are as defined in claim 1, or a pharmaceutically acceptable salt thereof. The compounds of formula (I) possess utility as inhibitors of TEAD. The compounds are useful as medicaments in the treatment of diseases or ...

The present disclosure relates to a pharmaceutical composition in the form of an orally deliverable liquid composition comprising tasipimidine, or a pharmaceutically acceptable salt thereof, as an active ingredient and to the use thereof in the treatment and prevention of a disorder, condition or disease where an al...

The present invention relates to an improved process for the preparation of 4H-pyranone structured CYP11A1 inhibitors such as 5-((1-(methylsulfonyl)-piperidin-4-yl)methoxy)-2-((5-(trifluoromethyl)isoindolin-2-yl)methyl)-4H-pyran-4-one (1A) and key intermediates thereof including 5-(trifluoromethyl)isoindoline (V) an...

The present invention relates to a pharmaceutical composition for oral administration, particularly in the form of a tablet or a powder suitable to be filled into a capsule shell, comprising 2-(isoindolin-2-ylmethyl)-5-((1-(methylsulfonyl)-piperidin-4-yl)methoxy)-4H-pyran-4-one (I) or a pharmaceutically acceptable s...

The invention relates to co administration a CYP2D6 inhibitor with tasipimidine or a pharmaceutically acceptable salt thereof in order to improve the pharmacokinetic profile of tasipimidine by decreasing its clearance and inter individual variation. The invention also relates to a combination of tasipimidine or a...