公开(公告)号：US20160220551A1

公开(公告)日：2016-08-04

申请号：US15016528

申请日：2016-02-05

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

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

IPC: A61K31/4545 ,  A61K45/06 ,  A61K9/16

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.

公开(公告)号：US20130150404A1

公开(公告)日：2013-06-13

申请号：US13545523

申请日：2012-07-10

Applicant: Mathai Mammen ,  Sarah Dunham ,  Adam Hughes ,  Craig Husfeld ,  Eric Stangeland

Inventor： Mathai Mammen ,  Sarah Dunham ,  Adam Hughes ,  Craig Husfeld ,  Eric Stangeland

IPC: C07D401/12

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 asthmas.

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β2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：US08377966B2

公开(公告)日：2013-02-19

申请号：US13357891

申请日：2012-01-25

Applicant: YongQi Mu ,  YuHua Ji ,  Mathai Mammen ,  Viengkham Malathong

Inventor： YongQi Mu ,  YuHua Ji ,  Mathai Mammen ,  Viengkham Malathong

IPC: A61K31/4523 ,  C07D211/40 ,  C07D401/12

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.

公开(公告)号：US08329911B2

公开(公告)日：2012-12-11

申请号：US12616957

申请日：2009-11-12

Applicant: YongQi Mu ,  YuHua Ji ,  Mathai Mammen ,  Eric L. Stangeland

Inventor： YongQi Mu ,  YuHua Ji ,  Mathai Mammen ,  Eric L. Stangeland

IPC: C07D211/46 ,  A61K31/445

CPC classification number: C07D211/46 ,  C07D405/12

Abstract: The invention provides compounds of formula I: wherein a, b, c, p, W, A, X1, R1, R2, R3, 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，p，W，A，X 1，R 1，R 2，R 3，R 6，R 7和R 8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：US08242135B2

公开(公告)日：2012-08-14

申请号：US13011100

申请日：2011-01-21

Applicant: Mathai Mammen ,  Eric Stangeland

Inventor： Mathai Mammen ,  Eric Stangeland

IPC: C07D453/02 ,  A61K31/47

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：US08119796B2

公开(公告)日：2012-02-21

申请号：US13193874

申请日：2011-07-29

Applicant: YuHua Ji ,  Mathai Mammen ,  Craig Husfeld ,  Li Li ,  YongQi Mu ,  Aaron Kushner ,  Eric Stangeland ,  Trevor Mischki ,  Adam Hughes ,  Sarah Dunham

Inventor： YuHua Ji ,  Mathai Mammen ,  Craig Husfeld ,  Li Li ,  YongQi Mu ,  Aaron Kushner ,  Eric Stangeland ,  Trevor Mischki ,  Adam Hughes ,  Sarah Dunham

IPC: C07D417/14 ,  C07D265/28 ,  C07D401/14 ,  A61K31/54 ,  A61K31/5377 ,  A61K31/496

CPC classification number: C07D211/46 ,  C07D405/12 ,  C07D409/12 ,  C07D487/08

Abstract: The invention provides compounds of formula I: wherein a, b, c, m, s, t, W, Z, Ar, R1, R2, R3, 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，s，t，w，Z，Ar，R 1，R 2，R 3，R 6和R 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：US08080565B2

公开(公告)日：2011-12-20

申请号：US12074889

申请日：2008-03-06

Applicant: Mathai Mammen ,  Richard Wilson ,  Sarah Dunham ,  Adam Hughes ,  Craig Husfeld ,  Yu-Hua Ji ,  Li Li ,  Trevor Mischki ,  Ioanna Stergiades ,  David Oare

Inventor： Mathai Mammen ,  Richard Wilson ,  Sarah Dunham ,  Adam Hughes ,  Craig Husfeld ,  Yu-Hua Ji ,  Li Li ,  Trevor Mischki ,  Ioanna Stergiades ,  David Oare

IPC: A61K31/445 ,  C07D401/02

CPC classification number: C07D401/12 ,  C07D401/14 ,  C07D405/14

Abstract: This invention provides 4-amino-1-benzylpiperidine and related compounds and pharmaceutically acceptable salts thereof which are useful as muscarinic receptor antagonists. This invention also provides pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors, such as overactive bladder, irritable bowel syndrome, asthma and chronic obstructive pulmonary disease, using such compounds.

Abstract translation: 本发明提供了可用作毒蕈碱受体拮抗剂的4-氨基-1-苄基哌啶及其相关化合物及其药学上可接受的盐。 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由毒蕈碱受体介导的疾病状态如膀胱过度活动症，肠易激综合征，哮喘和慢性阻塞性肺病的方法。

公开(公告)号：US08013152B2

公开(公告)日：2011-09-06

申请号：US12759887

申请日：2010-04-14

Applicant: YuHua Ji ,  Mathai Mammen ,  Craig Husfeld ,  Li Li ,  YongQi Mu ,  Aaron Kushner ,  Eric Stangeland ,  Trevor Mischki ,  Adam Hughes ,  Sarah Dunham

Inventor： YuHua Ji ,  Mathai Mammen ,  Craig Husfeld ,  Li Li ,  YongQi Mu ,  Aaron Kushner ,  Eric Stangeland ,  Trevor Mischki ,  Adam Hughes ,  Sarah Dunham

IPC: C07D265/28 ,  C07D241/04 ,  A61K31/54 ,  A61K31/5375

CPC classification number: C07D211/46 ,  C07D405/12 ,  C07D409/12 ,  C07D487/08

Abstract: The invention provides compounds of formula I: wherein a, b, c, m, s, t, W, Z, Ar, R1, R2, R3, 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，s，t，w，Z，Ar，R 1，R 2，R 3，R 6和R 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：US07893256B2

公开(公告)日：2011-02-22

申请号：US12756694

申请日：2010-04-08

Applicant: Mathai Mammen ,  Adam Hughes

Inventor： Mathai Mammen ,  Adam Hughes

IPC: C07D221/22 ,  C07D45/02 ,  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：US20110015152A1

公开(公告)日：2011-01-20

申请号：US12891459

申请日：2010-09-27

Applicant: Mathai Mammen ,  Adam Hughes

Inventor： Mathai Mammen ,  Adam Hughes

IPC: A61K31/695 ,  C07D207/08 ,  A61K31/40 ,  C07D215/227 ,  A61K31/4704 ,  C07F7/10 ,  A61P11/00

CPC classification number: C07D401/12 ,  C07D207/04 ,  C07D207/09 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14

Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, Ar1, Ar2, E, a, b, c and z 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 and therefore, 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，R 7，Ar 1，Ar 2，E，a，b，c和z如说明书中所定义，或其药学上可接受的盐或溶剂合物 或其立体异构体。 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，因此，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。