首页> 外国专利> Biphenyl compounds useful as Muscarinic Receptor Antagonists, Process for their preparation, Pharmaceutical compositions containing them, their use in the manufacture of a Medicament for the treatment of pulmonary diseases and a method to study a Biological Sample than the C

Biphenyl compounds useful as Muscarinic Receptor Antagonists, Process for their preparation, Pharmaceutical compositions containing them, their use in the manufacture of a Medicament for the treatment of pulmonary diseases and a method to study a Biological Sample than the C

机译:用作毒蕈碱受体拮抗剂的联苯化合物,其制备方法,包含它们的药物组合物,其在制备用于治疗肺部疾病的药物中的用途以及研究比C生物学样品的方法

摘要

Formula compound (1) is the opposite of muscle receptor. Drug synthesis containing such compounds, processes and intermediates, and methods of using these compounds for the treatment of lung diseases. Item 1: a formula compound (1)where: a is 0 or an integer between 1 and 5; each R1 is independently selected from C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, C3-6 cycloalkyl, cyano, halo, - OR1a, -C (O) OR1b, -SR1c, -S (O) R1d, -S (O) 2R1e and -NR1fR1g; where each of R1a, R1b, R1c, R1d, R1e, R1f and R1g is independently hydrogen, C1-4 alkyl or phenyl-C1-4alkyl; b is 0 or an integer between 1 and 4; each R2 is independently selected from C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, C3-6 cycloalkyl, cyano, halo, -OR2a, -C (O) OR2b, -SR2c, -S (O) R2d, -S (O) 2R2e and -NR2fR2g; where each of R2a, R2b, R2c, R2d, R2e, R2f and R2g is independently hydrogen, C1-4 alkyl or phenyl-C1-4alkyl;W stands for O NWA, where Wa is hydrogen or C1-4 tar; C is an integer of 0 or 1 to 5; each R3 stands for a separate combination of C1-4 or 2 R3 to form c1-3 tar, C2-3 alquinile or oxran-2.3-dilo; m is 0 or 1; R4 is hydrogen gene or C1-4 tar; s is 0, 1 or 2; AR1 refers to a group of phenyl compounds or c3-5 heteromorphic atoms containing 1 or 2 heteromorphic atoms independently selected between oxygen, nitro or sulfur; in this group, the phenyl or heteromorphic ring is replaced by (R5) Q, q is 0 or 1 to 4 integers, and each R5 is in halogen, hydroxy, C1-4 tar or C1-4 alcoxi; t is 0, 1 or 2; n is 0,1 or 2: D is an integer of 0 or 1 to 4; each R6 represents an independent fluorine insect or C1-4 tar; P is 0 or 1; R7 and R8 are independent hydrogen or C1-4 tar; each group of R1, r1a-1g, R2, r2a-2g, R3, R5, R6, R7 or R8 asphalt and alcox is replaced by a fluorine substitute of 1 to 5, or a salt or a solution. Or acceptable stereoisomers for pharmaceutical use Requirement No. 18: a process for preparing a process consisting of any one of 1 and 14 requirements, characterized by (a) reacting a compound of a formula (2),Or salt, a formula compound (3),Z1 represents a factory group, or (b) separates a compound (4) from the formula,Containing a formula compound (5),Or a reaction derivative; or (c) a formula compound (6) reacts,Z2 represents an outgoing group, consisting of a formula (7);(d) Reacting a formula compound (2) with a formula compound (8),In the presence of a reducing agent; or (E) reacting a formula compound (9),In the presence of a reducing agent, a formula compound (7) reacts; or (f) reacts a formula compound (10),R'es h, CH3 o-ch2ch3, which contains a formula compound: nhr7r8, indicating a formula compound (1). Labor requirement 21: a method of studying a biological system or sample, characterized by its inclusion of a muscle receptor, including: (a) linking the biological system or sample to compounds in labor requirements 1 to 14; and (b) determining the effect of a compound on the biological system or sample.
机译:式(1)化合物与肌肉受体相反。包含此类化合物,方法和中间体的药物合成,以及使用这些化合物治疗肺部疾病的方法。第1项:式(1)的化合物,其中:a为0或1至5之间的整数;每个R1独立地选自C1-4烷基,C2-4烯基,C2-4炔基,C3-6环烷基,氰基,卤素,-OR1a,-C(O)OR1b,-SR1c,-S(O)R1d, -S(O)2R1e和-NR1fR1g;其中R1a,R1b,R1c,R1d,R1e,R1f和R1g各自独立地是氢,C1-4烷基或苯基-C1-4烷基; b为0或1至4之间的整数;每个R 2独立地选自C 1-4烷基,C 2-4烯基,C 2-4炔基,C 3-6环烷基,氰基,卤素,-OR 2a,-C(O)OR 2b,-SR 2c,-S(O)R 2d, -S(O)2R2e和-NR2fR2g;其中R 2a,R 2b,R 2c,R 2d,R 2e,R 2f和R 2g各自独立地是氢,C 1-4烷基或苯基-C 1-4烷基; W代表O NWA,其中W a是氢或C 1-4焦油; C为0或1至5的整数;每个R 3代表C 1-4或2个R 3的单独组合以形成c 1-3焦油,C 2-3炔基或oxran-2.3 dilo。 m为0或1; R4是氢基因或C1-4焦油; s是0、1或2; AR1是指含有1或2个独立地选自氧,硝基或硫之间的杂原子的苯基化合物或c3-5个杂原子。在该组中,苯基或杂环被(R5)Q取代,q是0或1-4个整数,并且每个R5在卤素,羟基,C1-4焦油或C1-4醇中。 t是0、1或2; n是0,1或2:D是0或1到4的整数;每个R 6代表独立的氟昆虫或C 1-4焦油; P为0或1; R7和R8是独立的氢或C1-4焦油; R1,r1a-1g,R2,r2a-2g,R3,R5,R6,R7或R8沥青和醇中的每组均被1-5的氟代用品或盐或溶液代替。或药学上可接受的立体异构体第18号要求:一种用于制备由1和14中任一项要求组成的方法的方法,其特征在于(a)使式(2)的化合物或盐,式化合物(3)反应),Z1代表工厂基团,或(b)从式中分离化合物(4),包含式化合物(5),或反应衍生物;或(c)使式(6)的化合物反应,Z 2代表由式(7)组成的输出基团;(d)使式(2)与式(8)反应,在还原剂存在下代理商(E)使式(9)的化合物在还原剂的存在下反应。或(f)使包含式化合物:nhr7r8的式(10)的R 3,h,CH 3 o-ch2ch3反应,表示式(1)。劳动要求21:一种研究生物系统或样品的方法,其特征在于它包含肌肉受体,包括:(a)将生物系统或样品与劳动要求1至14中的化合物联系起来; (b)确定化合物对生物系统或样品的作用。

著录项

  • 公开/公告号AR048032A1

    专利类型

  • 公开/公告日2006-03-22

    原文格式PDF

  • 申请/专利权人 THERAVANCE INC.;

    申请/专利号AR2005P100927

  • 申请日2005-03-10

  • 分类号C07D401/12;A61K31/4545;A61P11/00;A61P11/06;G01N33/567;C07D211/62;C07D401/12;C07D211/46;C07D211/60;

  • 国家 AR

  • 入库时间 2022-08-21 21:40:28

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