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首页> 外国专利> Novel antagonist derivatives of vitronectin receptors, processes for their preparation, their use as medicaments and pharmaceutical compositions containing them

Novel antagonist derivatives of vitronectin receptors, processes for their preparation, their use as medicaments and pharmaceutical compositions containing them

机译：玻璃粘连蛋白受体的新型拮抗剂衍生物，其制备方法，其在药物中的用途以及含有它们的药物组合物

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4-(N-(2-Amino-2-carboxyethyl)-amino)-6-(4-substituted 1-piperidinyl)-4-pyrimidine derivatives (I) are new. Pyrimidine derivatives of formula (I) (including isomers and isomer mixtures) and their salts are new. [Image] G : R 7R 8N-C(=NR 6)-NHCO-, Het-NHCO-, Het-NHCH 2- or Het-; Het : mono- or polycyclic ring system, in which each ring is 4-10 membered and aromatic or non-aromatic and at least one ring contains 1-4 N heteroatoms, optionally substituted (os) by one or more groups R 9; R 1H, aryl, arylalkyl or amino (os by 1 or 2 of alkyl and/or 1-4C acyl); R 2H, halo, NO 2, alkyl, amino (os by 1 or 2 of alkyl and/or 1-4C acyl), -Q-COOR 5 or -Q-OR 5; Q : direct bond, CH 2 or CH 2CH 2; R 3COOR 5 or SO 2R 5; or a mono- or polycyclic ring system, in which each ring is 4-10 membered and aromatic or non-aromatic and at least one ring contains 1-4 N, O and/or S heteroatoms, os by one or more groups R 9; R 4OH, 1-8C alkoxy, 5-14C aryloxy, arylalkoxy, cycloalkoxy, cycloalkylalkoxy, (1-8C) alkylcarbonyloxyalkoxy, aryl-(1-8C) alkylcarbonyloxyalkoxy, di-(1-8C alkyl)-aminocarbonylmethoxy or aryl-dialkylaminocarbonylmethoxy; amino (os by 1 or 2 of alkyl, aryl, arylalkyl and/or 1-5C acyl); or a D- or L-aminoacid residue; R 51-8C alkyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, bicycloalkylalkyl or cycloalkylalkyl, where aryl, alkyl, cycloalkyl, bicycloalkylalkyl and tricycloalkyl moieties are os by one or more groups R 9; R 6H, OH, NO 2, (1-6C) alkoxycarbonyl or (1-6C) alkoxycarbonyloxy; R 7, R 8H or 1-6C alkyl (os by R 9); R 9halo, NH 2, NO 2, OH, alkoxy, alkylthio, COOH, alkoxycarbonyl, or 1-8C alkyl (os by one or more of halo, aryl or arylalkyl); unless specified otherwise alkyl moieties have 1-4C, aryl moieties 5-14C and cycloalkyl moieties 5-14C. Independent claims are also included for the preparation of (I). ACTIVITY : Osteopathic; Cytostatic; Antiinflammatory; Cardiant; Vasotropic; Antiarteriosclerotic; Nephrotropic; Ophthalmological; Antiarthritic; Antirheumatic. MECHANISM OF ACTION : Vitronectin receptor antagonist. 3-((5-Ethyl-6-(4-(1,2,3,4-tetrahydro-1,8-naphthyridin-7-yl)-1-piperidinyl)-4-pyrimidinyl)-amino)-N-((phenylmethoxy)-carbonyl)-alanine (Ia) had IC 5 0 3 nM in a vitronectin (alpha vbeta 3) receptor binding assay in vitro.
机译：4-（N-（2-氨基-2-羧乙基）-氨基）-6-（4-取代的1-哌啶基）-4-嘧啶衍生物（I）是新的。式（I）的嘧啶衍生物（包括异构体和异构体混合物）及其盐是新的。 [图像] G：R 7＞ R 8＞ N-C（＝ NR 6＞）-NHCO-，Het-NHCO-，Het-NHCH 2-或Het-; Het：单环或多环系统，其中每个环为4-10元且为芳族或非芳族，并且至少一个环包含1-4个N杂原子，任选被一个或多个基团R 9取代（os）。 R 1> H，芳基，芳基烷基或氨基（由烷基和/或1-4C酰基的1或2所取代）; R 2> H，卤素，NO 2，烷基，氨基（烷基和/或1-4C酰基的1或2个os），-Q-COOR 5>或-Q-OR 5>; Q：直接键，CH 2或CH 2CH 2; R 3> COOR 5>或SO 2R 5>;或单环或多环系统，其中每个环为4-10元且为芳族或非芳族，并且至少一个环包含1-4个N，O和/或S杂原子，其中一个或多个基团为R 9 >; R 4> OH，1-8C烷氧基，5-14C芳氧基，芳基烷氧基，环烷氧基，环烷基烷氧基，（1-8C）烷基羰氧基烷氧基，芳基-（1-8C）烷基羰氧基烷氧基，二-（1-8C烷基）-氨基羰基甲氧基或芳基-二烷基氨基羰基甲氧基;氨基（烷基，芳基，芳基烷基和/或1-5C酰基的1或2个基团）; D-或L-氨基酸残基;或R 5> 1-8C烷基，芳基，芳基烷基，环烷基，环烷基烷基，双环烷基烷基或环烷基烷基，其中芳基，烷基，环烷基，双环烷基烷基和三环烷基部分被一个或多个基团R 9所取代。 R 6＞ H，OH，NO 2，（1-6C）烷氧羰基氧基或（1-6C）烷氧羰基氧基; R 7＞，R 8＞ H或1-6C烷基（R 9＞ os）; R 9＞卤代，NH 2，NO 2，OH，烷氧基，烷硫基，COOH，烷氧羰基或1-8C烷基（由卤代，芳基或芳基烷基中的一个或多个所取代）;除非另有说明，否则烷基部分具有1-4C，芳基部分5-14C和环烷基部分5-14C。独立权利要求也包括用于制备（I）。活动：整骨疗法;细胞抑制消炎（药;卡迪恩变压性抗动脉硬化;嗜肾眼科抗关节炎抗风湿。作用机理：玻连蛋白受体拮抗剂。 3-（（5-乙基-6-（4-（1,2,3,4-四氢-1,8-萘啶-7-基）-1-哌啶基）-4-嘧啶基）-氨基）-N- （（苯基甲氧基）-羰基）-丙氨酸（Ia）在体外玻连蛋白（αvbeta 3）受体结合试验中的IC 5 0 3 nM。

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