３位において二置換されているインドール−２−オン誘導体、これらの調製およびこれらの治療上の使用

Title:

３位において二置換されているインドール−２−オン誘導体、これらの調製およびこれらの治療上の使用

Document Type and Number:

Japanese Patent JP5685440

Kind Code:

B2

Abstract:

Indol-2-one derivatives (I) and their acid or base addition salts, hydrates or solvates are new. Indol-2-one derivatives of formula (I) and their acid or base addition salts, hydrates or solvates are new. dotted line : simple or double bond; X : CH, N or C; Y1 : N or CH; Ar : aryl or heteroaryl (optionally substituted by one or more substituents comprising halo, alkoxy, aryl, perhaloalkyl or alkyl); R1 : H or -C(=O)alkyl, -C(=O)aryl or alkyl; R2-R4 : H, halo, alkyl, perhaloalkyl, CN, aryl, heteroaryl, OH, alkoxy, perhaloalkoxy, aminocarbonyl, alkylaminocarbonyl or dialkylaminocarbonyl; R5 : alkyl; and n : 1 or 2. Provided that at least one of: X, Y1 is N; and R2-R4 are H. Independent claims are included for: (1) the preparations of (I); (2) a halo substituted indol-2-one compound of formula (III); (3) alkyl substituted 1,3-dihydro-indol-2-one compound of formula (XXVIII); and (4) a halo substituted indol-2-one compound of formula (XXIX). Hal, Hal2 : halo; and Alk : alkyl. [Image] [Image] ACTIVITY : Anorectic; Antidiabetic; Anorectic. MECHANISM OF ACTION : Growth hormone secretagogue receptor-1a antagonist. The ability of (I) to antagonize growth hormone secretagogue receptor-1a was tested in rats. The result showed that (+)N-[4,6-dichloro-3-(4-trifluoromethyl-phenyl)-2-oxo-2,3-dihydro-1H-indol-3-yl]-2-(4-ethyl-piperidin-1-yl)-acetamide exhibited an IC 5 0value of 1x 10 -> 9>M.

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Inventors:

バローニ，マルコ
プレオ，レテイーツイア

Application Number:

JP2010520610A

Publication Date:

March 18, 2015

Filing Date:

August 14, 2008

Export Citation:

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Assignee:

サノフイ

International Classes:

C07D209/40; A61K31/404; A61K31/4439; A61K31/454; A61K31/4545; A61K31/496; A61K31/551; A61K45/00; A61P3/04; A61P3/10; A61P43/00; C07D295/14; C07D401/04; C07D401/12; C07D403/12; C07D405/04; C07D405/14; C07D409/04; C07D409/14; C07D417/04

Attorney, Agent or Firm:

In the patent business corporation Kawaguchi 國 case, it is a patent firm.
Chihiro Watanabe
Osaki Katsuma
Michiaki Tsubokura

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