首页> 外国专利> Piridopirimidinona AZA Derivatives, method of preparation, medicines containing them and uses as antithrombotic agents, Antidiabetic and antihyperlipidemic, among others.

Piridopirimidinona AZA Derivatives, method of preparation, medicines containing them and uses as antithrombotic agents, Antidiabetic and antihyperlipidemic, among others.

机译:Piridopirimidinona AZA衍生物,制备方法,含有它们的药物以及用作抗血栓药,抗糖尿病药和抗高血脂药等。

摘要

These compounds are resistant to hm74a and can be used as drugs. Claim 1: formula compound (1), wherein X1 is n or C (R6);X2 is n or C (R7);X3 is n or C (R8)There, at least one x1, X2 and X3 is n, and one can, O, n (R9) C (o),C (O) NR9 N (R9) C (O) O OC (O) NR9 N (R9) C (O) NR10 N (R9) SO2 o SO2N (R9)Z is a simple bond, or, if n is 1, 2, 3, 4, 5 or 6, it can also be o; R1, R2, R3 and R4, whether hydrogen, fluorine, hydrocarbyl or fluoride of lower hydrocarbyl, or R1 and R2, are all combined to form a carbon atom connected with it and - r1-r2-es (CH2) 2-6 -.R3 and R4 are combined to form a ring with the carbon atoms they are connected to, and - r3-r4-es - (CH2) 2-6 -;R5 is arilo or heteromorphic, arilo or heteromorphic substitutes are 1 to 3 independent substitutes, including halogen, tar, low oxygen, low fluoride tar, low fluoride oxygen, low fluoride oxygen, cyclopentyl, fluorine cyclopentyl, cyclopentyl oxygen, C (o) Oh, low oxygen-c (o),this is it!N (h, lower bitumen) C (o),N (lower) 2C (o),Oh, lower tar - C (o) or, NH2, n (h, lower tar),N (lower pitch) 2, lower pitch-c (o) NH, lower pitch-c (o) n,NH2SO2, N (H, lower alkyl) SO2, N (lower alkyl) 2SO2, lower alkyl-SO2-NH, lower alkyl-SO2-N (lower alkyl),cyano and phenyl which is optionally substituted with 1 to 3 substituents independently selected from the group consisting of halogen, lower alkyl, lower alkoxy and fluor-lower alkyl; R6 is hydrogen, halogen, lower alkyl, fluor-lower alkyl, lower alkoxy, fluor-lower alkoxy or cycloalkyl; R7 is hydrogen, halogen, lower alkyl, fluor-lower alkyl, lower alkoxy, fluor-lower alkoxy or cycloalkyl; R8 is hydrogen, halogen, lower alkyl, fluor-lower alkyl, lower alkoxy, fluor-lower alkoxy or cycloalkyl; R9 and R10 independently of each other are hydrogen, lower alkyl or fluor-lower alkyl; m is 0, 1,N is 0, 1, 2, 3, 4, 5, 6; m + n is = 1; but the condition is that if X1 is ch, X2 is ch, X3 is n, M + n is not 1; and salt and ester that can be accepted from drug.
机译:这些化合物对hm74a具有抗性,可用作药物。 2.权利要求1的式(1)的化合物,其中X 1为n或C(R 6); X 2为n或C(R 7); X 3为n或C(R 8)。一个罐,O,n(R9)C(o),C(O)NR9 N(R9)C(O)O OC(O)NR9 N(R9)C(O)NR10 N(R9)SO2 o SO2N( R9)Z是一个简单的键,或者,如果n为1、2、3、4、5或6,则它也可以为o; R1,R2,R3和R4(无论是氢,氟,低级烃基的氟化物还是氟化物),或R1和R2都结合在一起形成碳原子,并且-r1-r2-es(CH2)2-6- R3和R4与它们所连接的碳原子结合形成环,并且-r3-r4-es-(CH2)2-6-; R5是芳构或杂构的,芳构或杂构的取代基是1-3个独立的替代品,包括卤素,焦油,低氧,低氟焦油,低氟氧,低氟氧,环戊基,氟环戊基,环戊氧,C(o)哦,低氧-c(o),这就是N! h,低沥青)C(o),N(低)2C(o),Oh,低焦油-C(o)或NH2,n(h,低焦油),N(低沥青)2,低沥青- c(o)NH,低螺距-c(o)n,NH2SO2,N(H,低级烷基)SO2,N(低级烷基)2SO2,低级烷基-SO2-NH,低级烷基-SO2-N(低级烷基) ,氰基和苯基,它们任选地被1-3个独立地选自卤素,低级烷基,低级烷氧基和氟代低级烷基; R6是氢,卤素,低级烷基,氟代低级烷基,低级烷氧基,氟代低级烷氧基或环烷基; R7是氢,卤素,低级烷基,氟代低级烷基,低级烷氧基,氟代低级烷氧基或环烷基; R8是氢,卤素,低级烷基,氟代低级烷基,低级烷氧基,氟代低级烷氧基或环烷基; R9和R10彼此独立地是氢,低级烷基或氟代低级烷基; m为0,1,N为0,1,2,3,4,5,6; m + n是 = 1;但是条件是如果X1是ch,X2是ch,X3是n,M + n不为1;以及可以从药物中接受的盐和酯。

著录项

  • 公开/公告号AR065795A1

    专利类型

  • 公开/公告日2009-07-01

    原文格式PDF

  • 申请/专利权人 F. HOFFMANN-LA ROCHE AG.;

    申请/专利号AR2008P101143

  • 发明设计人

    申请日2008-03-19

  • 分类号C07D471/04;C07D475/04;C07D487/04;A61K31/519;A61P3/06;A61P3/10;A61P7/02;A61P9/10;A61P25/16;A61P25/18;A61P25/28;A61P11/06;A61P19/02;A61P1/12;A61P1/18;C07D471/04;C07D241/00;C07D221/00;C07D475/02;

  • 国家 AR

  • 入库时间 2022-08-21 19:28:39

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