公开(公告)号：US20060116398A1

公开(公告)日：2006-06-01

申请号：US11204066

申请日：2005-08-15

Applicant: Mathai Mammen ,  Trevor Mischki

Inventor： Mathai Mammen ,  Trevor Mischki

IPC: A61K31/445 ,  A61K31/40 ,  A61K31/381 ,  A61K31/34 ,  A61K31/325 ,  A61K31/17 ,  C07D207/12 ,  C07D211/22 ,  C07D307/14

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 b 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. 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：其中R 1，R 2，R 3，R 4，R 4， R 5，R 6，R 7，R 8a，R 8b，W 8， ，a和b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β2 N 2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：US20060035933A1

公开(公告)日：2006-02-16

申请号：US11204263

申请日：2005-08-15

Applicant: Mathai Mammen ,  Trevor Mischki ,  Adam Hughes ,  Yu-Hua Ji

Inventor： Mathai Mammen ,  Trevor Mischki ,  Adam Hughes ,  Yu-Hua Ji

IPC: A61K31/4545 ,  A61K31/454 ,  C07D401/02

CPC classification number: C07D401/12 ,  C07D401/14 ,  C07D409/14 ,  C07D417/14

Abstract: This invention provides compounds of formula I: wherein R1, R2, R4, R5, R6, R7, R8a, R8b, W, a, b, c and m 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. 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: 本发明提供式I化合物：其中R 1，R 2，R 4，R 5，R 5， R 6，R 7，R 8a，R 8b，W，a，b，c和m分别为 在本说明书中定义，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。 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：US20050203139A1

公开(公告)日：2005-09-15

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: A61K31/445 ,  C07D211/26 ,  C07D211/46

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：US06656694B2

公开(公告)日：2003-12-02

申请号：US09758916

申请日：2001-01-11

Applicant: Mathai Mammen

Inventor： Mathai Mammen

IPC: G01N3353

CPC classification number: C07D211/58 ,  G01N33/60 ,  G01N2500/04 ,  Y10S530/807

Abstract: A method of identifying a ligand for a second binding site (5) on a biological substrate (1) is disclosed. The method comprises determining the effect of a candidate compound (9) on the binding of a probe compound (2) which binds to a first binding site (3) on the biological substrate in the presence of a first multibinding compound (4) which binds to the first (3) and second (5) binding sites on the biological substrate (1).

公开(公告)号：US08969571B2

公开(公告)日：2015-03-03

申请号：US14087404

申请日：2013-11-22

Applicant: Mathai Mammen ,  Adam Hughes ,  Yan Chen

Inventor： Mathai Mammen ,  Adam Hughes ,  Yan Chen

IPC: 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 ,  G01N33/94

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R1，R2，R3，R4，R5，R6，R7，W，a，b和c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。 本发明的联苯衍生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，因此，这种联苯衍生物可用于治疗肺部疾病，如慢性阻塞性肺疾病和哮喘。

公开(公告)号：US08912334B2

公开(公告)日：2014-12-16

申请号：US14023794

申请日：2013-09-11

Applicant: Mathai Mammen ,  YuHua Ji ,  YongQi Mu ,  Craig Husfeld ,  Li Li

Inventor： Mathai Mammen ,  YuHua Ji ,  YongQi Mu ,  Craig Husfeld ,  Li Li

IPC: C07D401/00 ,  A61K31/44 ,  C07D211/62 ,  C07D401/12 ,  A61K45/06 ,  A61K31/4545

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，Ar1，R1，R2，R3，R4，R6，R7和R8如 规范。 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：US20140171397A1

公开(公告)日：2014-06-19

申请号：US14023794

申请日：2013-09-11

Applicant: Mathai Mammen ,  YuHua Ji ,  YongQi Mu ,  Craig Husfeld ,  Li Li

Inventor： Mathai Mammen ,  YuHua Ji ,  YongQi Mu ,  Craig Husfeld ,  Li Li

IPC: C07D401/12 ,  A61K45/06 ,  A61K31/4545

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，Ar1，R1，R2，R3，R4，R6，R7和R8如 规范。 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：US20130274288A1

公开(公告)日：2013-10-17

申请号：US13915004

申请日：2013-06-11

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

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

IPC: C07D401/12 ,  C07D405/12

CPC classification number: C07D401/12 ,  C07D211/46 ,  C07D211/62 ,  C07D401/14 ,  C07D405/12 ,  C07D409/12

Abstract: The invention provides compounds of formula I: wherein a, b, c, m, n, q, r, W, Z1, Ar1, Z2, 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，m，n，q，r，w，Z1，Ar1，Z2，Y，R1，R2和R3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：US08211915B2

公开(公告)日：2012-07-03

申请号：US12880752

申请日：2010-09-13

Applicant: Mathai Mammen ,  YuHua Ji ,  YongQi Mu

Inventor： Mathai Mammen ,  YuHua Ji ,  YongQi Mu

IPC: A61K31/4465 ,  A61K31/40 ,  C07D401/10 ,  C07D401/12

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 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，Ar1，R1，R2，R3，R4，R6，R7，R8和W如 规范。 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：US20120122926A1

公开(公告)日：2012-05-17

申请号：US13357891

申请日：2012-01-25

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

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

IPC: A61K31/4545 ,  C07D405/12 ,  C07D401/12 ,  C07D405/14 ,  A61K31/4535 ,  A61K31/4525 ,  A61P11/00 ,  C07D409/14 ,  C07D409/12 ,  C07D401/14

CPC classification number: C07D211/46 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12

Abstract: The invention provides compounds of formula I: wherein a, b, c, m, n, q, r, W, Z1, Ar1, Z2, 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，m，n，q，r，w，Z1，Ar1，Z2，Y，R1，R2和R3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。