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1. 发明授权

US06344570B1 Substituted urea derivatives as cell adhesion inhibitors 失效
标题翻译：取代的脲衍生物作为细胞粘附抑制剂
公开(公告)号：US06344570B1
公开(公告)日：2002-02-05
申请号：US09554224
申请日：2000-07-11
申请人： David R Brittain , Craig Johnstone
发明人： David R Brittain , Craig Johnstone
IPC分类号： C07D31748
CPC分类号： C07D405/12 , C07C275/34 , C07D317/12 , C07D407/12 , C07D413/12 , C07D417/12
摘要： Compounds of formula (II) where R1 is in the para or meta position and is (A); R2 and R3 are each independently selected from hydrogen, nitro, C1-6alkyl, C3-6cycloalkyl, C2-6alkenyl, C2-6alkynyl, C1-4alkoxyl, C1-6alkylamino, C1-6dialkylamino, C1-6akylC1-4alkoxyl, C1-6alkylaminoC1-6alkyl, amino, cyano, halogeno, trifluoromethyl, —CO2R12 and —CONR12R13, where R12 and R13 are independently selected from hydrogen or C1-6alkyl, or R2 and R3 together with the phenyl to which they are attached form a 9 or 10 membered bicyclic ring system; R4 is C1-4alkyl; R5 is selected from hydrogen and C1-4alkyl; R6 is selected from C1-6alkyl, C1-4alkyl(C4-6)cycloalkyl, C1-6alkyl(C1-6)alkoxyl, C1-6alkylS(C1-6)alkyl, C1-4alkylsulphonyl(C1-4)alkyl; (B) where q is an integer from 1 to 6 and R14 is halogeno; R7 is selected from C1-6alkyl, C1-8alkoxylcarbonyl, C2-6alkenyl, 1,3-benzodioxol-5-yl and aryl each optionally substituted by one or more substituents selected from C1-4alkoxy, C1-6alkyl, cyano, halogeno, and trifluoromethyl; R8 is aryl, heteroaryl, a bicyclic heteroaryl ring system linked to the nitrogen via a ring carbon or a 9 or 10 membered bicyclic ring system linked to the nitrogen via a ring carbon and each ring is optionally substituted with up to two substituents, which may be the same or different, and are selected from C1-6alkyl, C1-4alkoxy, C1-4alkylthio, C1-6alkylC1-4alkoxyl, C1-6alkylaminoC1-6alkyl, hydroxy, —CO2H, —(CH2)pOH where p is 1 or 2, cyano, halogeno, and trifluoromethyl; R9 and R10 are each independently selected from hydrogen and C1-4alkyl or R8 and R9 together with the nitrogen to which they are attached form a dihydroindolyl, or a dihidroquinolinyl group; R11 is selected from carboxyl, tetrazolyl, alkyl sulphonylcarbamyl, sulfo and sulfino; Y is oxygen, sulphur or sulfonyl; m is 0 or 1; and n is 0 or an integer from 1 to 4 with the proviso that when m and n cannot both be 0 and when m is 1, n is 0; or a pharmaceutically acceptable salt or in vivo hydrolyzable ester thereof. The compounds inhibit the interaction of vascular cell-adhesion molecule-1 and fibronectin with integrin very late antigen 4 (&agr;4&bgr;1). They have therapeutic applications such as in multiple sclerosis, rheumatoid arthritis, asthma, coronary artery disease and psoriasis.
摘要翻译：其中R1为对位或间位且为（A）的式（II）化合物; R 2和R 3各自独立地选自氢，硝基，C 1-6烷基，C 3-6环烷基，C 2-6烯基，C 2-6炔基，C 1-4烷氧基，C 1-6烷基氨基，C 1-6二烷基氨基，C 1-6烷基C 1-4烷氧基，C 1-6烷基氨基C 1- 6烷基，氨基，氰基，卤代，三氟甲基，-CO 2 R 12和-CONR 12 R 13，其中R 12和R 13独立地选自氢或C 1-6烷基，或者R 2和R 3与它们所连接的苯基一起形成9或10元双环环系; R4是C1-4烷基; R5选自氢和C 1-4烷基; R 6选自C 1-6烷基，C 1-4烷基（C 4-6）环烷基，C 1-6烷基（C 1-6）烷氧基，C 1-6烷基S（C 1-6）烷基，C 1-4烷基磺酰基（C 1-4）烷基; （B）其中q是1至6的整数，R 14是卤素; R 7选自C 1-6烷基，C 1-8烷氧基羰基，C 2-6烯基，1,3-苯并间二氧杂环戊烯-5-基和各自任选被一个或多个选自C 1-4烷氧基，C 1-6烷基，氰基，卤代和三氟甲基 R 8是芳基，杂芳基，通过环碳与氮连接的双环杂芳基环系统，或通过环碳与氮连接的9或10元双环体系，并且每个环任选被至多两个取代基取代，选自C 1-6烷基，C 1-4烷氧基，C 1-4烷硫基，C 1-6烷基C 1-4烷氧基，C 1-6烷基氨基C 1-6烷基，羟基，-CO 2 H， - （CH 2）p OH，其中p为1或2 ，氰基，卤代和三氟甲基; R9和R

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