Selected CGRP antagonists, methods for the production thereof and their use as medicaments

摘要

Piperidine-1-carboxylic acid derivatives (I) are new. Piperidine-1-carboxylic acid derivatives of formula (I) and their tautomers, isomers, hydrates and salts are new. A, X : O or S; D, E : CH or N; G : CRa or N; M : CRb or N; Q : CRc or N, Ra, Rb, Rc : e.g. Halogen, 1-6C-Alkyl, Cyano, Hydroxy, Hydroxy-1-6C-alkyl, Hydroxy-3-6C-alkenyl, 1-6C-Alkoxy; R 1> : e.g. a saturated or mono- or diunsaturated aza, triaza, oxaza, thiaza, thiadiaza or S,S-dioxido thiadiaza heterocycle bonded to the piperidine ring through a C or N atom or spirocyclically through a C atom and C, N, O or S atom; R 2> : benzyl; optionally omega -substituted 2-7C-alkyl; or phenyl or pyridyl; where phenyl, pyridyl and diazinyl groups are optionally substituted; R 3> : H, phenyl(C1-3)alkyl or pyridyl(C1-3)alkyl, where the alkyl group can form a 4- to 7-membered ring with R 2>; R 2>+R 3> : (CR 8>R 9>) q-CR 6>R 7>-Y 1>R 4>R 5>-CR 6>R 7>-(CR 8>R 9>) r; Y 1> : C or N; q, r : 0-2 when Y 1> is C or 1-2 when Y 1> is N; R 4> : H, Amino-, 1-4C-Alkylamino-, Di-(1-4C-alkyl)alkylamino-, 1-6C-Alkyl-, optionally Hydroxycarbonyl; R 5> : H or OH; optionally substituted 1-4C-Alkyl; or is absent when Y 1> is N; or is F when Y 1> is C; or is linked to R 4> to form a 4- to 7-membered cycloaliphatic Ring, in which a CH 2 group can be replaced by -NH-, -N(1-4C-Alkyl)-, -N(3-4C-Alkenyl)-, -N(3-4C-Alkynyl)-, -N(Cyclo-3-7C-alkyl)-, -N(3-7C-Cycloalkyl-1-3C-alkyl)-, -N(Hydroxycarbonyl-1-3C-alkyl)- or -N(1-6C-Alkoxycarbonyl-1-3C-alkyl)-; R 6>, R 7> : H, 1-4C-Alkyl or, when Y 1> is C, also F, Amino, 1-4C-Alkylamino- or Di-(1-4C-alkyl)amino, where the two 1-4C-Alkyl groups can be joined to form a ring; R 8>, R 9> : H or 1-3C-Alkyl; Full definitions are given in the Definitions Field (Full Definitions). An independent claim is also included for a process for preparing (I). [Image] ACTIVITY : Analgesic; Antimigraine; Antidiabetic; Vasotropic; Antidiarrheic; Dermatological; Antiinflammatory; Antiarthritic; Antiallergic; Anmtiasthmatic; Antibacterial; Immunosuppressive. No biological data given. MECHANISM OF ACTION : Calcitonin gene related peptide (CGRP) antagonist.