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Cyclic Depsipeptide Compound And Use Thereof

Abstract: [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 actions of naturally fermented materials, and as a result, they have found that a cyclic depsipeptide compound derived from a soil bacterium belonging to the genus Chromobacterium which is collected in Okutama-machi, Tokyo has both an inhibitory action on airway contraction and an inhibitory action on airway inflammation, and thus, is useful as an agent for preventing or treating COPD or asthma, thereby completing the present invention.  That is, the present invention relates to a pharmaceutical composition for preventing and/or treating chronic obstructive pulmonary disease (COPD) or asthma, which contains a cyclic depsipeptide compound or a salt thereof as an active ingredient and is intended to be administered by intratracheal administration, nasal drop administration, or inhalation administration. [Selected Figure] Nil

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Notices, Deadlines & Correspondence

Patent Information

Application #
Filing Date
24 May 2011
Publication Number
36/2012
Publication Type
INA
Invention Field
CHEMICAL
Status
Email
patent@depenning.com
Parent Application

Applicants

ASTELLAS PHARMA INC.
3-11, NIHONBASHI-HONCHO 2-CHOME, CHUO-KU, TOKYO 103-8411

Inventors

1. TSUJIMOTO, SUSUMU
C/O ASTELLAS PHARMA INC., 3-11, NIHONBASHI-HONCHO 2-CHOME, CHUO-KU, TOKYO 103-8411
2. TANIGUCHI, MASATOSHI
C/O ASTELLAS PHARMA INC., 3-11, NIHONBASHI-HONCHO 2-CHOME, CHUO-KU, TOKYO 103-8411
3. HIRAYAMA, YOSHITAKA
C/O ASTELLAS PHARMA INC., 3-11, NIHONBASHI-HONCHO 2-CHOME, CHUO-KU, TOKYO 103-8411
4. TAKASAKI, JUN
C/O ASTELLAS PHARMA INC., 3-11, NIHONBASHI-HONCHO 2-CHOME, CHUO-KU, TOKYO 103-8411
5. KAWASAKI, TOMIHISA
C/O ASTELLAS PHARMA INC., 3-11, NIHONBASHI-HONCHO 2-CHOME, CHUO-KU, TOKYO 103-8411
6. SAKAMOTO, KAZUTOSHI
C/O ASTELLAS PHARMA INC., 3-11, NIHONBASHI-HONCHO 2-CHOME, CHUO-KU, TOKYO 103-8411
7. NISHIWAKI, SHINYA
C/O ASTELLAS PHARMA INC., 3-11, NIHONBASHI-HONCHO 2-CHOME, CHUO-KU, TOKYO 103-8411
8. KITANAGA, YUKIHIRO
C/O ASTELLAS PHARMA INC., 3-11, NIHONBASHI-HONCHO 2-CHOME, CHUO-KU, TOKYO 103-8411

Specification

DESCRIPTION Title of Invention: CYCLIC DEPSIPEPTIDE COMPOUND AND USE THEREOF Technical Field [0001] The present invention relates to a cyclic depsipeptide compound useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for treating chronic obstructive pulmonary disease (COPD) or asthma, and its use for treating COPD or asthma. Background Art [0002] COPD and asthma are both diseases involving limited airflow in the airway. [0003] COPD is a disease in which coughing accompanying exertional dyspnea and sputum is a main symptom. When the disease condition worsens, coughing, wheezing, and dyspnea increase, accompanied by increased sputum which has a changed purulent nature. The airway symptoms such as coughing and wheezing are caused by airway contraction and airway inflammation, and airway hypersecretion accompanied therewith. The disease is characterized in that airflow limitation is not completely reversible. The airflow limitation is usually progressive and occurs with an abnormal inflammatory response of the lung to noxious particles or gases (the Global Initiative for Chronic Obstructive Lung Disease in 2006, which will be hereinafter referred to as GOLD). Most sufferers are smokers. It is estimated that COPD will be the third largest cause of mortality in the world in 2020 (Lancet, 349, pp. 1498-1504,1997). In a survey conducted in 12 countries of adults over the age of 40, it was estimated that COPD prevalence was 10.1% (Lancet, 370, pp. 741-750, 2007). It is estimated that the COPD prevalence in people of the age of 40 or more in Japan is 10.9% (Respiology, 9, pp. 458-465,2004). [0004] Asthma is a disease characterized by airway hyperresponsiveness and chronic inflammation, and is also a chronic inflammatory disease of the airway showing reversible airway obstruction improved with therapy and having repeatedly occurring airflow limitation due to airway mucosal edema. It shows symptoms such as paroxysmal dyspnea, coughing, and wheezing. Asthma is one type of chronic respiratory disease and occurs in all age groups ranging from children to the elderly. In addition the number of sufferers, regardless of whether in developed countries or developing countries, is tending to increase and the prevalence thereof in Japan is reported to be 4.2% for infants, 4.0% for children, and 1.7% for adults (Health and Welfare Long-Term Chronic Disease Comprehensive Research Project in Heisei 8). The number of people who have died of asthma in Japan is tending to decrease and was 2778 in 2006, which is still high. [0005] In diagnosing COPD and asthma, a volume in one second indicating a degree of airway obstruction (FEVi: Forced Expiratory Volume in 1 Second) is presented as an indicator. The "volume in one second" is defined as "a volume of exhaled breath during the first one second when a deep breath is exhaled as quickly as possible after inhalation". Typical disease stage classification of COPD is stipulated in GOLD and the stages are classified into the following four stages according to FEV1: Stage I (mild): FEV1>80% predicted value, II (moderate): 50%80% (less than 20% variation), Step 2 (mild persistent type) FEV1, PEF>80% (20% to 30% variation), Step 3 (moderate persistent type) 60% or -CH2SCH3, R22 is -CH(CH3)2 or -CH2SCH3, R3 and R4 are tile same as or different from each other, and represent -H or -CH3, or R3 arid R4 are combined to form =CH2, and R, R and R are the same as or different from each other, and represent -H or -F]. [Claim 5] A method for preventing or treating COPD or asthma, comprising administering to a patient in need thereof an effective amount of the cyclic depsipeptide compound of the formula (II) or a salt thereof by any one process of intratracheal administration, nasal drop administration, and inhalation administration: [Chem. 11] [wherein R1 is -H or -CH3, R2 is -H or a group represented by the formula (III): [Chem. 12] R21 is -CH3, -CH2CH3, -CH2CH2CH3, or -CH2SCH3, R22 is-CH(CH3)2 or-CH2SCH3, R3andR4 are the same as or different from each other, and represent -H or -CH3, or R3 and R4 are combined to form, =CH2, and R5, R6 and R7 are the same as or different from each other, and represent -H or -F].

Documents

Application Documents

# Name Date
1 3542-CHENP-2011 FORM-3 07-12-2011.pdf 2011-12-07
1 3542-CHENP-2011 PCT 24-05-2011.pdf 2011-05-24
2 3542-CHENP-2011 FORM-5 24-05-2011.pdf 2011-05-24
2 3542-CHENP-2011 CORRESPONDENCE OTHERS 07-12-2011.pdf 2011-12-07
3 3542-CHENP-2011 FORM-3 24-05-2011.pdf 2011-05-24
3 3542-CHENP-2011 CORRESPONDENCE OTHERS 14-11-2011.pdf 2011-11-14
4 3542-CHENP-2011 FORM-2 24-05-2011.pdf 2011-05-24
4 3542-CHENP-2011 FORM-3 14-11-2011.pdf 2011-11-14
5 3542-CHENP-2011 FORM-1 24-05-2011.pdf 2011-05-24
5 3542-CHENP-2011 POWER OF ATTORNEY 24-05-2011.pdf 2011-05-24
6 3542-CHENP-2011 CORRESPONDENCE OTHERS 24-05-2011.pdf 2011-05-24
6 3542-CHENP-2011 ABSTRACT 24-05-2011.pdf 2011-05-24
7 3542-CHENP-2011 DRAWINGS 24-05-2011.pdf 2011-05-24
7 3542-CHENP-2011 CLAIMS 24-05-2011.pdf 2011-05-24
8 3542-CHENP-2011 DESCRIPTION(COMPLETE) 24-05-2011.pdf 2011-05-24
9 3542-CHENP-2011 DRAWINGS 24-05-2011.pdf 2011-05-24
9 3542-CHENP-2011 CLAIMS 24-05-2011.pdf 2011-05-24
10 3542-CHENP-2011 ABSTRACT 24-05-2011.pdf 2011-05-24
10 3542-CHENP-2011 CORRESPONDENCE OTHERS 24-05-2011.pdf 2011-05-24
11 3542-CHENP-2011 FORM-1 24-05-2011.pdf 2011-05-24
11 3542-CHENP-2011 POWER OF ATTORNEY 24-05-2011.pdf 2011-05-24
12 3542-CHENP-2011 FORM-2 24-05-2011.pdf 2011-05-24
12 3542-CHENP-2011 FORM-3 14-11-2011.pdf 2011-11-14
13 3542-CHENP-2011 FORM-3 24-05-2011.pdf 2011-05-24
13 3542-CHENP-2011 CORRESPONDENCE OTHERS 14-11-2011.pdf 2011-11-14
14 3542-CHENP-2011 FORM-5 24-05-2011.pdf 2011-05-24
14 3542-CHENP-2011 CORRESPONDENCE OTHERS 07-12-2011.pdf 2011-12-07
15 3542-CHENP-2011 PCT 24-05-2011.pdf 2011-05-24
15 3542-CHENP-2011 FORM-3 07-12-2011.pdf 2011-12-07