公开(公告)号：US20100197922A1

公开(公告)日：2010-08-05

申请号：US12756694

申请日：2010-04-08

Applicant: Mathai Mammen ,  Adam Hughes

Inventor： Mathai Mammen ,  Adam Hughes

IPC: C07D491/08

CPC classification number: C07D451/02 ,  A61K31/46 ,  A61K31/4743 ,  C07D451/12 ,  C07D471/08

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

Abstract translation: 本发明提供式I化合物：其中R 1，R 2，R 3，R 4，R 5，R 6和R 7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。 本发明的化合物具有二肾上腺素能受体激动剂和毒蕈碱受体拮抗剂活性。 这些化合物可用于治疗肺部疾病，如慢性阻塞性肺疾病和哮喘。

公开(公告)号：US20090306134A1

公开(公告)日：2009-12-10

申请号：US12286528

申请日：2008-09-30

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: A61K31/4545 ,  A61K31/54 ,  A61K31/5377 ,  A61K31/495 ,  A61K31/445 ,  C07D413/12 ,  C07D403/06 ,  C07D401/06 ,  C07D211/00

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：US20090182010A1

公开(公告)日：2009-07-16

申请号：US12412194

申请日：2009-03-26

Applicant: Mathai Mammen ,  Trevor Mischkl

Inventor： Mathai Mammen ,  Trevor Mischkl

IPC: A61K31/4709 ,  C07D215/12 ,  A61K31/47 ,  A61P11/00

CPC classification number: C07D213/40 ,  C07C271/28 ,  C07D215/26 ,  C07D277/28 ,  C07D333/20 ,  C07D409/12

Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8a, R8b, W, a and bare as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both β2 adrenergic receptor agonist and muscarinic receptor antagonist activity. Accordingly, such compounds are expected to be useful as therapeutic agents for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.

Abstract translation: 本发明提供了式I化合物或其药学上可接受的盐或溶剂合物或立体异构体：其中R1，R2，R3，R4，R5，R6，R7，R8a，R8b， 本发明的化合物具有β2肾上腺素能受体激动剂和毒蕈碱受体拮抗剂活性。 因此，预期这些化合物可用作治疗肺部疾病如慢性阻塞性肺疾病和哮喘的治疗剂。

公开(公告)号：US07560469B2

公开(公告)日：2009-07-14

申请号：US11077436

申请日：2005-03-10

Applicant: Mathai Mammen ,  Yu-Hua Ji ,  YongQi Mu

Inventor： Mathai Mammen ,  Yu-Hua Ji ,  YongQi Mu

IPC: A61K31/45 ,  C07D211/40

CPC classification number: C07D211/62 ,  C07D409/14

Abstract: This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, s, t, Ar1, R1, R2, R3, R4, R6, R7, R8, and W are as defined in the specification. The compounds of formula I are mescaline 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，Ar1，R1，R2，R3，R4，R6，R7，R8和W如 规范。 式I化合物是麦芽糖素受体拮抗剂。 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：US20090176767A1

公开(公告)日：2009-07-09

申请号：US12402665

申请日：2009-03-12

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

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

IPC: A61K31/55 ,  C07D211/40 ,  C07D243/06 ,  A61K31/445 ,  A61P11/06

CPC classification number: C07D211/46 ,  C07D211/60 ,  C07D211/62 ,  C07D401/12 ,  C07D405/12

Abstract: This invention provides compounds of formula I: wherein a, b, c, m, p, r, R1, R2, R3, R4, R5, R6, W and X1 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，m，p，r，R1，R2，R3，R4，R5，R6，W和X1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：US07524965B2

公开(公告)日：2009-04-28

申请号：US11789300

申请日：2007-04-24

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: C07D211/40 ,  A61K31/445

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：US07456199B2

公开(公告)日：2008-11-25

申请号：US11077222

申请日：2005-03-10

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: C07D211/44 ,  A61K31/45

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 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，m，p，s，t，W，Ar 1，X 1，R 1 R 2，R 3，R 3，R 4，R 6和R 6， 7 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：US07358244B2

公开(公告)日：2008-04-15

申请号：US10854829

申请日：2004-05-27

Applicant: Mathai Mammen ,  Adam Hughes

Inventor： Mathai Mammen ,  Adam Hughes

IPC: A61K31/44 ,  A61K31/54 ,  C07D221/22 ,  C07D451/02 ,  C07D417/00

CPC classification number: C07D451/02 ,  A61K31/46 ,  A61K31/4743 ,  C07D451/12 ,  C07D471/08

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

Abstract translation: 本发明提供了式I化合物：其中R 1，R 2，R 3，R 4，R 4， 其中R 6，R 6和R 7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。 本发明的化合物具有β2 N 2肾上腺素能受体激动剂和毒蕈碱受体拮抗剂活性。 这些化合物可用于治疗肺部疾病，如慢性阻塞性肺疾病和哮喘。

公开(公告)号：US07351718B2

公开(公告)日：2008-04-01

申请号：US11602802

申请日：2006-11-21

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: A61K31/40 ,  A61K31/445 ,  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.

公开(公告)号：US20080071088A1

公开(公告)日：2008-03-20

申请号：US11899181

申请日：2007-09-05

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: C07D401/12

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.