Amine-derivatives having NPY Y5 receptor antagonistic activity and the uses thereof

• US 8,227,618 B2
• Filed: 04/23/2010
• Issued: 07/24/2012
• Est. Priority Date: 04/23/2009
• Status: Expired due to Fees

• Current Assignee: Shionogi & Co., Ltd.
• Original Assignee: Shionogi & Co., Ltd.
• Inventors: Okuno, Takayuki, Sakagami, Masahiro
• Primary Examiner(s): Saeed, Kamal
• Assistant Examiner(s): Grazier, Nyeemah A
• Application Number:
  US12/766,458
• Publication Number:
  US 20100273841A1
• Time in Patent Office: 823 Days
• Field of Search: None
• US Class Current: 548/222
• CPC Class Codes: A61P 3/04 Anorexiants; Antiobesity agents
• CPC Class Codes: C07D 231/38 Nitrogen atoms nitro radicals C07D231/16
• CPC Class Codes: C07D 263/58 with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
• CPC Class Codes: C07D 277/82 Nitrogen atoms

Abstract

This invention provides an anorectic or anti-obesity composition comprising a compound of the formula (I):

• • formula (I):

a pharmaceutically acceptable salt or solvate thereof,
wherein

• R¹ is optionally substituted lower alkyl,
• Y is —S(O)n- wherein n is 1 or 2, or —CO—,
• R² is hydrogen or lower alkyl,
• R⁷ is hydrogen or lower alkyl,
• X is lower alkylene, lower alkenylene, arylene, cycloalkylene or the like, and
• Z is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like.

Claims

1. A compound of:

4. An anorectic or anti-obesity composition comprising a compound or pharmaceutically acceptable salt thereof according to claim 1.

5. A method for suppressing appetite, comprising administering an effective amount of a compound or pharmaceutically acceptable salt thereof according to claim 1 to a subject in need thereof.

6. A method for treating obesity, comprising administering an effective amount of a compound or pharmaceutically acceptable salt thereof according to claim 1 to a subject in need thereof.

7. A method for treating an obesity-related disorder, comprising administering an effective amount of a compound or pharmaceutically acceptable salt thereof according to claim 1 to a subject in need thereof, wherein said obesity-related disorder is overeating, hypertension, impaired glucose tolerance, diabetes, metabolic syndrome, abnormal lipid metabolism, dyslipidemia, arteriosclerosis, hyperuricemia, gout, fatty liver, endometrial, breast, prostate and colon cancer, osteoarthritis, lumbago, obstructive sleep apnea syndrome, coronary artery disease, cerebral infarction, menstrual disorder, Prader-Willi Syndrome, Frohlich'"'"'s syndrome, or pickwickian syndrome.

8. A method for weight management for obesity, comprising administering an effective amount of a compound or pharmaceutically acceptable salt thereof according to claim 1 to a subject in need thereof.

9. A method for inducing weight loss, comprising administering an effective amount of a compound or pharmaceutically acceptable salt thereof according to claim 1 to a subject in need thereof.

10. A method for accelerating weight loss, comprising administering an effective amount of a compound or pharmaceutically acceptable salt thereof according to claim 1 to a subject in need thereof.

11. A method for maintaining body weight, comprising administering an effective amount of a compound or pharmaceutically acceptable salt thereof according to claim 1 to a subject in need thereof.

12. A method for managing body weight, comprising administering an effective amount of a compound or pharmaceutically acceptable salt thereof according to claim 1 to a subject in need thereof.

2. A pharmaceutical composition, comprising a compound of:

3. A pharmaceutical composition according to claim 2, exhibiting NPY Y5 receptor antagonistic activity.