公开(公告)号：US09045443B2

公开(公告)日：2015-06-02

申请号：US13905338

申请日：2013-05-30

Applicant: Mathai Mammen ,  Adam D. Hughes

Inventor： Mathai Mammen ,  Adam D. Hughes

IPC: C07D261/18 ,  C07D413/12 ,  C07D271/08 ,  C07C235/80 ,  A61K31/42 ,  A61K31/4245 ,  A61K31/216 ,  C07C233/56 ,  A61K45/06 ,  C07D271/04 ,  C07C243/28

CPC classification number: C07D271/08 ,  A61K31/216 ,  A61K31/42 ,  A61K31/4245 ,  A61K45/06 ,  C07C233/56 ,  C07C235/80 ,  C07C243/28 ,  C07D261/18 ,  C07D271/04 ,  C07D413/12

Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, R7, R8, Z, X, b, and c are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds are nitric oxide donors and have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

Abstract translation: 一方面，本发明涉及具有下式的化合物：其中R1，R2，R3，R7，R8，Z，X，b和c如说明书中所定义，或其药学上可接受的盐。 这些化合物是一氧化氮供体并且具有去甲肾上腺素抑制活性。 另一方面，本发明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：US20140235864A1

公开(公告)日：2014-08-21

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

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：US20130172301A1

公开(公告)日：2013-07-04

申请号：US13592713

申请日：2012-08-23

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: C07D211/62 ,  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.

公开(公告)号：US08247564B2

公开(公告)日：2012-08-21

申请号：US12903365

申请日：2010-10-13

Applicant: Mathai Mammen ,  Sarah Dunham

Inventor： Mathai Mammen ,  Sarah Dunham

IPC: 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：US20120190657A1

公开(公告)日：2012-07-26

申请号：US13438105

申请日：2012-04-03

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: A61K31/4545 ,  A61P11/00 ,  A61K31/56

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：US08173815B2

公开(公告)日：2012-05-08

申请号：US13226677

申请日：2011-09-07

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

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

IPC: C07D211/00

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，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：US08124627B2

公开(公告)日：2012-02-28

申请号：US12605854

申请日：2009-10-26

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

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

IPC: A61K31/45 ,  A61K31/454 ,  A61K31/4545 ,  C07D401/10 ,  C07D295/08

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, 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：US07858795B2

公开(公告)日：2010-12-28

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: C07D227/08 ,  A61K31/445

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：US07829728B2

公开(公告)日：2010-11-09

申请号：US11983963

申请日：2007-11-13

Applicant: Mathai Mammen ,  Adam Hughes

Inventor： Mathai Mammen ,  Adam Hughes

IPC: C07D207/30

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。

公开(公告)号：US20100249421A1

公开(公告)日：2010-09-30

申请号：US12814629

申请日：2010-06-14

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.

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。