公开(公告)号：US08618131B2

公开(公告)日：2013-12-31

申请号：US13545523

申请日：2012-07-10

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

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

IPC: A61K31/47 ,  C07D215/00

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 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：US07879879B2

公开(公告)日：2011-02-01

申请号：US11448317

申请日：2006-06-07

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

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

IPC: A61K31/445 ,  C07D211/54 ,  C07D211/56

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：US20050113417A1

公开(公告)日：2005-05-26

申请号：US10992927

申请日：2004-11-19

Applicant: Mathai Mammen ,  Sarah Dunham

Inventor： Mathai Mammen ,  Sarah Dunham

IPC: A61K31/405 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  A61K31/454 ,  C07D277/68 ,  C07D417/12

CPC classification number: C07D417/12 ,  A61K31/439 ,  A61K31/445 ,  A61K31/4545 ,  C07D277/68

Abstract: The invention is directed to compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7a, R7b, W, G1, G2, a, b, c, d and m are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

Abstract translation: 本发明涉及式I化合物：其中R 1，R 2，R 3，R 4， R 5，R 6，R 7a，R 7b，W，G 1， A，B，C，D和m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。 本发明还涉及包含这些化合物的药物组合物; 使用这些化合物的方法; 以及制备这些化合物的方法和中间体。

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：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：US07842704B2

公开(公告)日：2010-11-30

申请号：US12001362

申请日：2007-12-11

Applicant: Mathai Mammen ,  Sarah Dunham

Inventor： Mathai Mammen ,  Sarah Dunham

IPC: A61K31/455 ,  C07D409/00

CPC classification number: C07D417/12 ,  A61K31/439 ,  A61K31/445 ,  A61K31/4545 ,  C07D277/68

Abstract: The invention is directed to compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7a, R7b, W, G1, G2, a, b, c, d and m are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

Abstract translation: 本发明涉及式I化合物：其中R1，R2，R3，R4，R5，R6，R7a，R7b，W，G1，G2，a，b，c，d和m如说明书中所定义， 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; 使用这些化合物的方法; 以及制备这些化合物的方法和中间体。

公开(公告)号：US07728144B2

公开(公告)日：2010-06-01

申请号：US11451179

申请日：2006-06-12

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

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

IPC: C07D211/08 ,  A61K31/44

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。

公开(公告)号：US20080096911A1

公开(公告)日：2008-04-24

申请号：US12001363

申请日：2007-12-11

Applicant: Mathai Mammen ,  Sarah Dunham

Inventor： Mathai Mammen ,  Sarah Dunham

IPC: A61K31/445 ,  A61K31/439 ,  A61K31/4545 ,  A61P11/00

CPC classification number: C07D417/12 ,  A61K31/439 ,  A61K31/445 ,  A61K31/4545 ,  C07D277/68

Abstract: The invention is directed to compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7a, R7b, W, G1, G2, a, b, c, d and m are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.