Title:
Ｎ−［（１Ｈ−ピラゾール−１−イル）アリール］−１Ｈ−インドール又は１Ｈ−インダゾール−３−カルボキサミドの誘導体、それらの製造及びＰ２Ｙ１２アンタゴニストとしてのそれらの使用
Document Type and Number:
Japanese Patent JP2014520071
Kind Code:
A
Abstract:
N-[(1H-Pyrazol-1-yl)aryl]-1H-indole or 1H-indazole-3-carboxamide derivatives (I) are new. N-[(1H-Pyrazol-1-yl)aryl]-1H-indole or 1H-indazole-3-carboxamide derivatives of formula (I) in the form of a base or addition salt to an acid or base, are new. X : -CH or N; A : aromatic bivalent group comprising phenyl group of formula (a), pyrimidine, pyrazine or pyridazine; R1 : 1-4C alkyl or 1-4C alkoxy; R2 : Alk; R3 : OH or -NR7R8; R4 : H, halo, CN, phenyl, Alk, OAlk or -NR9R10; R5 : H, halo or Alk; R6 : H, halo, CN, -COOAlk or -CONH 2; either R7 : H or 1-4C alkyl; and R8 : 3-6C heterocycloalkyl (optionally substituted by 1-4C alkyl or -COOAlk), heteroaryl (optionally substituted by 1-4C alkyl), 3-7C cycloalkyl, 3-6C heterocycloalkyl (optionally substituted by 1-4C alkyl or -COOAlk), H, OH, OAlk or -SO 2Alk; or R7R8+N : optionally saturated, mono- or poly-cyclic, condensed or bridged 4-10C heterocycle ring comprising 1-3 other nitrogen atoms or another heteroatom comprising O or S, where the heterocycle is optionally substituted by 1-3 substituents of halo, OH, -OR11, oxo, -NR9R10, -NR12COR13, -NR12COOR13, -COR13, -COOR13, -CONR14R15, 3-7C cycloalkyl (optionally substituted with OH or 1-4C alkyl), 3-6C heterocycloalkyl (optionally substituted with 1 or 2 oxo groups), phenyl (optionally substituted by one or more substituents of halo, Alk or OAlk), pyridinyl or 1-4C alkyl (optionally substituted by one or more substituents of halo, OH, -OR11, -NR9R10, -NR12COR13, -COOR13, -CONR14R15, -SO 2Alk, 3-7C cycloalkyl, 3-6C heterocycloalkyl, phenyl (optionally substituted by one or more substituents of halo, Alk or OAlk) or heteroaryl (optionally substituted by 1-4C alkyl)); R9, R10 : H or 1-4C alkyl; R11 : Alk, 1-4C alkylene-OH or 1-4C alkylene-OAlk; R12 : H or 1-4C alkyl; R13 : 1-4C alkyl; either R14, R15 : H, 1-4C alkyl or 3-7C cycloalkyl; or R14, R15+N : heterocyclic group comprising azetidin-1-yl, pyrrolidin-1-yl, piperidin-1-yl, morpholin-4-yl or piperazin-1-yl; and Alk : 1-4C alkyl (optionally substituted by F). Independent claims are included for: (1) a pyrazole compound of formula (II); and (2) the preparation of (I). Z : 1-4C alkyl. [Image] [Image] [Image] ACTIVITY : Antianginal; Cardiant; Anticoagulant; Thrombolytic; Antiarteriosclerotic; Cerebroprotective; Vasotropic; Vulnerary; Cardiovascular-Gen.; Dermatological; Hemostatic; Immunosuppressive; Gynecological; Antiinflammatory; Nephrotropic; Gastrointestinal-Gen. MECHANISM OF ACTION : Purinergic receptor P2Y G-protein coupled 12 (P2Y12) antagonist.
Inventors:
Alan バドーク
Christoff Bolu Delon
Natalie デレスク
Valery フォッセイ
Gilbert La Salle
グザヴィエ イヴォン
Christoff Bolu Delon
Natalie デレスク
Valery フォッセイ
Gilbert La Salle
グザヴィエ イヴォン
Application Number:
JP2014506776A
Publication Date:
August 21, 2014
Filing Date:
September 13, 2011
Export Citation:
Assignee:
Sanofi
International Classes:
A61K31/4155; C07D231/56; A61K31/416; A61K31/4162; A61K31/4178; A61K31/437; A61K31/497; A61K31/4985; A61K31/4995; A61K31/501; A61K31/5377; A61K31/541; A61K31/551; A61P7/02; A61P9/10; A61P13/12; A61P25/10; C07D401/14; C07D403/12; C07D403/14; C07D405/14; C07D409/14; C07D413/14; C07D471/04; C07D471/08; C07D487/04; C07D487/08
Domestic Patent References:
| JP2007518809A | 2007-07-12 | |||
| JP2012232966A | 2012-11-29 |
Foreign References:
| WO2008048981A2 | 2008-04-24 | |||
| WO2007002635A2 | 2007-01-04 |
Attorney, Agent or Firm:
Junji Yuita
Noriyuki Takebayashi
Noriyuki Takebayashi