公开(公告)号：US07151115B2

公开(公告)日：2006-12-19

申请号：US11337451

申请日：2006-01-23

Applicant: Mathai Mammen ,  Yu-Hua Ji ,  Sarah Dunham ,  Li Li

Inventor： Mathai Mammen ,  Yu-Hua Ji ,  Sarah Dunham ,  Li Li

IPC: A61K31/40 ,  A61K31/445

CPC classification number: C07D403/12 ,  A61K9/0075 ,  A61K9/0078 ,  A61K9/008 ,  A61K31/40 ,  A61K31/445 ,  C07D207/09

Abstract: This invention provides compounds of formula I: wherein a, b, c, e, m, R1, R2, R3, R4a, R4b, R5, 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：US20060205946A1

公开(公告)日：2006-09-14

申请号：US11372251

申请日：2006-03-09

Applicant: Yu-Hua Ji ,  Craig Husfeld ,  Mathai Mammen ,  YongQi Mu ,  Eric Stangeland

Inventor： Yu-Hua Ji ,  Craig Husfeld ,  Mathai Mammen ,  YongQi Mu ,  Eric Stangeland

IPC: A61K31/496 ,  A61K31/454 ,  C07D403/02

CPC classification number: C07D211/58 ,  C07D211/46 ,  C07D211/62 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D487/08 ,  C07D487/10

Abstract: The invention provides compounds of formula I: wherein a, b, c, d, f, W, Q, 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，d，f，w，Q，Y，R 1，R 2和R 2， 3 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：US20050203167A1

公开(公告)日：2005-09-15

申请号：US11077391

申请日：2005-03-10

Applicant: Mathai Mammen ,  Yu-Hua Ji ,  Yan Chen ,  Craig Husfeld

Inventor： Mathai Mammen ,  Yu-Hua Ji ,  Yan Chen ,  Craig Husfeld

IPC: A61K31/4025 ,  C07D207/08 ,  C07D207/30 ,  C07D409/06 ,  C07D49/02

CPC classification number: C07D207/08 ,  C07D409/06

Abstract: This invention provides compounds of formula I: wherein a, b, c, e, m, n, Ar1, R1, R2, R3, R4a, R4b, R5 and R6 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，e，m，n，Ar 1，R 1，R 2， R 3，R 4a，R 4b，R 5和R 6， 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：US20050203137A1

公开(公告)日：2005-09-15

申请号：US11076631

申请日：2005-03-10

Applicant: Mathai Mammen ,  Yu-Hua Ji ,  Craig Husfeld

Inventor： Mathai Mammen ,  Yu-Hua Ji ,  Craig Husfeld

IPC: A61K31/44 ,  C07D211/26 ,  C07D211/46

CPC classification number: C07D211/46

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，R 1，R 2，R 3， R 4，R 5，R 6，W和X 1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：US20050113413A1

公开(公告)日：2005-05-26

申请号：US10975657

申请日：2004-10-28

Applicant: Richard Wilson ,  Julie Congdon ,  Mathai Mammen ,  Weijiang Zhang ,  Robert Chao

Inventor： Richard Wilson ,  Julie Congdon ,  Mathai Mammen ,  Weijiang Zhang ,  Robert Chao

IPC: A61K31/444 ,  A61K31/4545 ,  C07C309/35 ,  C07D401/14 ,  C07D41/14

CPC classification number: C07C309/35 ,  C07D401/14

Abstract: This invention provides naphthalene-1,5-disulfonic acid salts of 4-{N-[7-(3-(S)-1-carbamoyl-1,1-diphenylmethyl)pyrrolidin-1-yl)hept-1-yl]-N-(isopropyl)amino}-1-(4-methoxypyrid-3-ylmethyl)piperidine, which salts are useful as muscarinic receptor antagonists. This invention is also directed to pharmaceutical compositions comprising these salt forms, methods of using these salt forms for treating medical conditions mediated by muscarinic receptors; and processes for preparing these salt forms.

Abstract translation: 本发明提供4- {N- [7-（3-（S）-1-氨甲酰基-1,1-二苯基甲基）吡咯烷-1-基）庚-1-基]萘-1,5-二磺酸盐， -N-（异丙基）氨基} -1-（4-甲氧基吡啶-3-基甲基）哌啶，其可用作毒蕈碱受体拮抗剂。 本发明还涉及包含这些盐形式的药物组合物，使用这些盐形式治疗毒蕈碱受体介导的医学病症的方法; 以及制备这些盐形式的方法。

公开(公告)号：US09452161B2

公开(公告)日：2016-09-27

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: C07D401/00 ,  A61K31/44 ,  A61K31/4545 ,  A61K9/16 ,  A61K45/06

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：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：US20130323271A1

公开(公告)日：2013-12-05

申请号：US13905338

申请日：2013-05-30

Applicant: Mathai Mammen ,  Adam D. Hughes

Inventor： Mathai Mammen ,  Adam D. Hughes

IPC: C07C233/56 ,  A61K31/42 ,  C07D271/04 ,  C07D413/12 ,  A61K31/4245 ,  A61K31/216 ,  C07D261/18 ,  A61K45/06

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：US20120122850A1

公开(公告)日：2012-05-17

申请号：US13348085

申请日：2012-01-11

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: A61K31/445 ,  C07D211/46 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D487/08 ,  A61K31/496 ,  A61K31/4525 ,  A61K31/4545 ,  A61K31/4535 ,  A61K31/5377 ,  A61K31/4995 ,  A61K31/551 ,  A61P11/00 ,  A61P11/06 ,  A61P1/00 ,  A61P1/12 ,  A61P9/06 ,  A61P25/16 ,  A61P25/28 ,  A61P25/00 ,  C07D401/12

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：US08067439B2

公开(公告)日：2011-11-29

申请号：US12938539

申请日：2010-11-03

Applicant: Mathai Mammen ,  YuHua Ji ,  YongQi Mu ,  Eric L. Stangeland ,  Aaron Kushner ,  Craig Husfeld

Inventor： Mathai Mammen ,  YuHua Ji ,  YongQi Mu ,  Eric L. Stangeland ,  Aaron Kushner ,  Craig Husfeld

IPC: C07D401/12 ,  A61K31/4465 ,  A61K31/4523

CPC classification number: C07D211/62 ,  C07D211/60

Abstract: This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, r, R1, R2, R3, R4, R5, R6, R7, 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，r，R1，R2，R3，R4，R5，R6，R7和W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。