公开(公告)号：US07615566B2

公开(公告)日：2009-11-10

申请号：US12011939

申请日：2008-01-30

Applicant: Mathai Mammen ,  Adam Hughes ,  Yu-hua Ji ,  Li Li ,  Weijiang Zhang

Inventor： Mathai Mammen ,  Adam Hughes ,  Yu-hua Ji ,  Li Li ,  Weijiang Zhang

IPC: A61K31/445 ,  A61K31/40 ,  C07D207/04 ,  C07D211/06

CPC classification number: C07D207/08 ,  A61K31/40 ,  C07D207/09 ,  C07D207/16 ,  C07D211/34

Abstract: This invention is directed to compounds of formula I: wherein R1-R5 and a-e are as defined in the specification; or pharmaceutically-acceptable salt or solvate or stereoisomer thereof. The invention also directed to pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors using such compounds.

Abstract translation: 本发明涉及式I化合物：其中R1-R5和a-e如说明书中所定义; 或其药学上可接受的盐或溶剂合物或立体异构体。 本发明还涉及含有这些化合物的药物组合物; 用于制备这些化合物的方法和中间体; 以及使用这些化合物治疗由毒蕈碱受体介导的疾病状况的方法。

公开(公告)号：US20090176833A1

公开(公告)日：2009-07-09

申请号：US12406283

申请日：2009-03-18

Applicant: Pierre-Jean Colson ,  Adam D. Hughes ,  Craig Husfeld ,  Mathai Mammen ,  Miroslav Rapta

Inventor： Pierre-Jean Colson ,  Adam D. Hughes ,  Craig Husfeld ,  Mathai Mammen ,  Miroslav Rapta

IPC: A61K31/445 ,  A61P11/06

CPC classification number: C07D211/46

Abstract: This invention relates to compounds of formula I: wherein R1 and R2 are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention also relates to pharmaceutical compositions and combinations comprising such compounds, processes and intermediates for preparing such compounds, and methods of using such compound to, for example, treat pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.

Abstract translation: 本发明涉及式I化合物：其中R1和R2如本说明书中所定义，或其药学上可接受的盐或溶剂合物或立体异构体。 本发明还涉及包含这些化合物的药物组合物和组合物，用于制备这些化合物的方法和中间体，以及使用该化合物例如治疗慢性阻塞性肺疾病和哮喘等肺病的方法。

公开(公告)号：US07557126B2

公开(公告)日：2009-07-07

申请号：US11820153

申请日：2007-06-18

Applicant: Mathai Mammen ,  Yu-Hua Ji ,  Yan Chen ,  Craig Husfeld

Inventor： Mathai Mammen ,  Yu-Hua Ji ,  Yan Chen ,  Craig Husfeld

IPC: A61K31/40 ,  C07D207/09

CPC classification number: C07D207/08 ,  C07D409/06

Abstract: This invention provides compounds of formula I: wherein a, b, c, e, m, n, Ar1, R1, R2, R3, R4a, R4b, R5 and R6 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.

Abstract translation: 本发明提供式I化合物：其中a，b，c，e，m，n，Ar1，R1，R2，R3，R4a，R4b，R5和R6如说明书中所定义。 式I化合物是毒蕈碱受体拮抗剂。 本发明还提供含有这些化合物的药物组合物，用于制备这些化合物的方法和中间体以及使用这些化合物治疗肺部疾病的方法。

公开(公告)号：US20090048299A1

公开(公告)日：2009-02-19

申请号：US12286914

申请日：2008-10-03

Applicant: Mathai Mammen ,  Yu-Hua Ji ,  YongQi Mu ,  Trevor Mischki ,  Viengkham Malathong

Inventor： Mathai Mammen ,  Yu-Hua Ji ,  YongQi Mu ,  Trevor Mischki ,  Viengkham Malathong

IPC: A61K31/4545 ,  C07D401/02

CPC classification number: C07D211/46

Abstract: This invention provides compounds of formula I: wherein a, b, c, m, p, s, t, W, Ar1, X1, R1, R2, R3, R4, R6, and R7 areas defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.

Abstract translation: 本发明提供式I化合物：其中在说明书中定义的其中a，b，c，m，p，s，t，W，Ar1，X1，R1，R2，R3，R4，R6和R7区域。 式I化合物是毒蕈碱受体拮抗剂。 本发明还提供含有这些化合物的药物组合物，用于制备这些化合物的方法和中间体以及使用这些化合物治疗肺部疾病的方法。

公开(公告)号：US07479562B2

公开(公告)日：2009-01-20

申请号：US11372251

申请日：2006-03-09

Applicant: Yu-Hua Ji ,  Craig Husfeld ,  Mathai Mammen ,  YongQi Mu ,  Eric L. Stangeland

Inventor： Yu-Hua Ji ,  Craig Husfeld ,  Mathai Mammen ,  YongQi Mu ,  Eric L. Stangeland

IPC: C07D211/00 ,  C07D409/00 ,  C07D405/00

CPC classification number: C07D211/58 ,  C07D211/46 ,  C07D211/62 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D487/08 ,  C07D487/10

Abstract: The invention provides compounds of formula I: wherein a, b, c, d, f, W, Q, Y, R1, R2, and R3 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.

Abstract translation: 本发明提供式I化合物：其中a，b，c，d，f，W，Q，Y，R 1，R 2和R 3如说明书中所定义。 式I化合物是毒蕈碱受体拮抗剂。 本发明还提供含有这些化合物的药物组合物，用于制备这些化合物的方法和中间体以及使用这些化合物治疗肺部疾病的方法。

公开(公告)号：US07456203B2

公开(公告)日：2008-11-25

申请号：US10425368

申请日：2003-04-29

Applicant: James Aggen ,  John H. Griffin ,  Mathai Mammen ,  Daniel Marquess ,  Edmund J. Moran ,  David Oare

Inventor： James Aggen ,  John H. Griffin ,  Mathai Mammen ,  Daniel Marquess ,  Edmund J. Moran ,  David Oare

IPC: A01N43/40 ,  A61K31/445

CPC classification number: A61K31/40 ,  C07C211/32 ,  C07C2603/32 ,  C07D207/08 ,  C07D209/48 ,  C07D211/46 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D519/00 ,  G01N33/566

Abstract: Disclosed are multibinding compounds which are muscarinic receptor antagonists. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is, independently of each other, a muscarinic receptor antagonist or an allosteric modulator provided that at least one of said ligand is a muscarinic receptor antagonist. The multibinding compounds of this invention are useful in the treatment and prevention of diseases such as chronic obstructive pulmonary disease, chronic bronchitis, irritable bowel syndrome, urinary incontinence, and the like.

Abstract translation: 公开了作为毒蕈碱受体拮抗剂的多重联结化合物。 含有2-10个配体的本发明的多相结合化合物共价连接到一个或多个接头上。 每个配体彼此独立地是毒蕈碱受体拮抗剂或变构调节剂，只要至少一种所述配体是毒蕈碱受体拮抗剂即可。 本发明的多重联结化合物可用于治疗和预防慢性阻塞性肺疾病，慢性支气管炎，肠易激综合征，尿失禁等疾病。

公开(公告)号：US07355046B2

公开(公告)日：2008-04-08

申请号：US11448294

申请日：2006-06-07

Applicant: Mathai Mammen ,  Adam Hughes ,  Yan Chen

Inventor： Mathai Mammen ,  Adam Hughes ,  Yan Chen

IPC: C07D221/02

CPC classification number: C07D211/46 ,  A61K31/445 ,  A61K31/452 ,  C07D211/48 ,  C07D211/58 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12 ,  C07D453/02 ,  C07D471/08 ,  G01N33/9433

Abstract: This invention provides biphenyl derivatives of formula I: wherein R1, R2, R3, R4, R5, R6, R7, W, a, b and c are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The biphenyl derivatives of this invention possess both β2 adrenergic receptor agonist and muscarinic receptor antagonist activity and therefore, such biphenyl derivatives are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.

Abstract translation: 本发明提供式I的联苯衍生物：其中R 1，R 2，R 3，R 4， R 5，R 6，R 7，W，a，b和c如本说明书中所定义，或其药学上可接受的盐或 其溶剂合物或立体异构体。 本发明的联苯衍生物具有β2N2肾上腺素能受体激动剂和毒蕈碱受体拮抗剂活性，因此，这种联苯衍生物可用于治疗肺部疾病，如慢性阻塞性肺病和哮喘。

公开(公告)号：US07345175B2

公开(公告)日：2008-03-18

申请号：US11448293

申请日：2006-06-07

Applicant: Mathai Mammen ,  Adam Hughes ,  Yan Chen

Inventor： Mathai Mammen ,  Adam Hughes ,  Yan Chen

IPC: C07D211/00

CPC classification number: C07D211/46 ,  A61K31/445 ,  A61K31/452 ,  C07D211/48 ,  C07D211/58 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12 ,  C07D453/02 ,  C07D471/08 ,  G01N33/9433

Abstract: This invention provides biphenyl derivatives of formula I: wherein R1, R2, R3, R4, R5, R6, R7, W, a, b and c are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The biphenyl derivatives of this invention possess both β2 adrenergic receptor agonist and muscarinic receptor antagonist activity and therefore, such biphenyl derivatives are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.

公开(公告)号：US20070254943A1

公开(公告)日：2007-11-01

申请号：US11820153

申请日：2007-06-18

Applicant: Mathai Mammen ,  Yu-Hua Ji ,  Yan Chen ,  Craig Husfeld

Inventor： Mathai Mammen ,  Yu-Hua Ji ,  Yan Chen ,  Craig Husfeld

IPC: A61K31/4025 ,  A61P9/00 ,  C07D207/00

CPC classification number: C07D207/08 ,  C07D409/06

Abstract: This invention provides compounds of formula I: wherein a, b, c, e, m, n, Ar1, R1, R2, R3, R4a, R4b, R5 and R6 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.

公开(公告)号：US07288657B2

公开(公告)日：2007-10-30

申请号：US11077433

申请日：2005-03-10

Applicant: Mathai Mammen ,  Yu-Hua Ji ,  YongQi Mu ,  Craig Husfeld ,  Li Li

Inventor： Mathai Mammen ,  Yu-Hua Ji ,  YongQi Mu ,  Craig Husfeld ,  Li Li

IPC: C07D211/00 ,  C07D405/00 ,  C07D409/00

CPC classification number: C07D211/62 ,  A61K9/124 ,  A61K9/1623 ,  A61K9/1652 ,  A61K31/4545 ,  A61K45/06 ,  C07D401/12

Abstract: This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, s, t, W, Ar1, R1, R2, R3, R4, R6, R7, and R8 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.

Abstract translation: 本发明提供式I化合物：其中a，b，c，d，m，n，p，s，t，W，Ar 1，R 1，R R 2，R 3，R 4，R 6，R 7和/或R 4， R 8如本说明书中所定义。 式I的化合物是毒蕈碱受体拮抗剂。 本发明还提供含有这些化合物的药物组合物，用于制备这些化合物的方法和中间体以及使用这些化合物治疗肺部疾病的方法。