Invention Grant
US08367692B2 Spiro (piperidine-4,2′-pyrrolidine)-1-(3,5-trifluoromethyl phenyl) methylcarboxamides as NK1 tachikynin receptor antagonists
有权
螺(哌啶-4,2'-吡咯烷)-1-(3,5-三氟甲基苯基)甲基甲酰胺作为NK1振动子受体拮抗剂
- Patent Title: Spiro (piperidine-4,2′-pyrrolidine)-1-(3,5-trifluoromethyl phenyl) methylcarboxamides as NK1 tachikynin receptor antagonists
- Patent Title (中): 螺(哌啶-4,2'-吡咯烷)-1-(3,5-三氟甲基苯基)甲基甲酰胺作为NK1振动子受体拮抗剂
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Application No.: US12989699Application Date: 2009-04-29
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Publication No.: US08367692B2Publication Date: 2013-02-05
- Inventor: Giuseppe Alvaro , Emiliano Castiglioni , Agostino Marasco
- Applicant: Giuseppe Alvaro , Emiliano Castiglioni , Agostino Marasco
- Applicant Address: SG Jurong
- Assignee: Glaxo Wellcome Manufacturing Pte Ltd
- Current Assignee: Glaxo Wellcome Manufacturing Pte Ltd
- Current Assignee Address: SG Jurong
- Agent J. Scott Young
- Priority: GB0808030.1 20080501
- International Application: PCT/EP2009/055190 WO 20090429
- International Announcement: WO2009/133135 WO 20091105
- Main IPC: A61K31/438
- IPC: A61K31/438 ; C07D401/04 ; C07D471/10

Abstract:
Compounds of formula (I) or a pharmaceutically acceptable salt thereof. wherein R is hydrogen or C1-4 alkyl; R1 is hydrogen, C1-4 alkyl, C(O)OH, C(O)NH2 or (C1-4 alkylene)R10; R2 and R3 are independently hydrogen, C1-4 alkyl or R2 together with R3 and together with the carbon atom to which they are attached form a C3-8 cycloalkyl group; R4 is C1-4 alkyl, C1-4 alkoxy or halogen; R5 and R7 are independently hydrogen, hydroxy, halogen, C(O)NH2, C(O)OH or (C1-4 alkylene)R10; R6 and R8 are independently hydrogen or halogen; R9 is hydrogen, (C1-4 alkylene)R10, C(O)NH2, C(O)OH or R9 together with R form a 6 membered heterocyclic ring optionally containing a further heteroatom selected from oxygen, sulphur or nitrogen; R10 is hydrogen, halogen, hydroxy, C(O)NH2, C(O)NH(C1-4 alkyl), C(O)N(C1-4 alkyl)2 or C(O)OH; n is 0, 1 or 2. processes for their preparation, to compositions containing them and to their use in the treatment of diseases and conditions for which antagonism of NK1 is beneficial.
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