公开(公告)号：US07456203B2

公开(公告)日：2008-11-25

申请号：US10425368

申请日：2003-04-29

Applicant: James Aggen ,  John H. Griffin ,  Mathai Mammen ,  Daniel Marquess ,  Edmund J. Moran ,  David Oare

Inventor： James Aggen ,  John H. Griffin ,  Mathai Mammen ,  Daniel Marquess ,  Edmund J. Moran ,  David Oare

IPC: A01N43/40 ,  A61K31/445

CPC classification number: A61K31/40 ,  C07C211/32 ,  C07C2603/32 ,  C07D207/08 ,  C07D209/48 ,  C07D211/46 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D519/00 ,  G01N33/566

Abstract: Disclosed are multibinding compounds which are muscarinic receptor antagonists. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is, independently of each other, a muscarinic receptor antagonist or an allosteric modulator provided that at least one of said ligand is a muscarinic receptor antagonist. The multibinding compounds of this invention are useful in the treatment and prevention of diseases such as chronic obstructive pulmonary disease, chronic bronchitis, irritable bowel syndrome, urinary incontinence, and the like.

Abstract translation: 公开了作为毒蕈碱受体拮抗剂的多重联结化合物。 含有2-10个配体的本发明的多相结合化合物共价连接到一个或多个接头上。 每个配体彼此独立地是毒蕈碱受体拮抗剂或变构调节剂，只要至少一种所述配体是毒蕈碱受体拮抗剂即可。 本发明的多重联结化合物可用于治疗和预防慢性阻塞性肺疾病，慢性支气管炎，肠易激综合征，尿失禁等疾病。

公开(公告)号：US20070244148A1

公开(公告)日：2007-10-18

申请号：US10583814

申请日：2004-12-21

Applicant: Steven Bondy ,  Eric Dowdy ,  Choung Kim ,  David Oare ,  Johan Neyts ,  Vahid Zia ,  Gerhard Purstinger

Inventor： Steven Bondy ,  Eric Dowdy ,  Choung Kim ,  David Oare ,  Johan Neyts ,  Vahid Zia ,  Gerhard Purstinger

IPC: C07D471/04 ,  A61K31/437

CPC classification number: C07D471/04

Abstract: The present invention relates to a pharmaceutical composition for the treatment or prevention of viral infections comprising as an active principle at least one imidazo[4,5-c]pyridine prodrug having the general formula (Z): The invention also relates to processes for the preparation of compounds according to the invention having above mentioned general formula and their use as a medicine or to treat or prevent viral infections.

Abstract translation: 本发明涉及用于治疗或预防病毒感染的药物组合物，其包含作为活性成分的具有通式（Z）的至少一种咪唑并[4,5-c]吡啶前药：本发明还涉及 制备具有上述通式的本发明化合物及其作为药物的用途或用于治疗或预防病毒感染。

公开(公告)号：US20060079478A1

公开(公告)日：2006-04-13

申请号：US10833293

申请日：2004-04-26

Applicant: Constantine Boojamra ,  Carina Cannizzaro ,  James Chen ,  Xiaowu Chen ,  Aesop Cho ,  Lee Chong ,  Maria Fardis ,  Alan Huang ,  Choung Kim ,  Thorsten Kirschberg ,  Steven Krawczyk ,  Christopher Lee ,  Kuei-Ying Lin ,  Richard Mackman ,  David Markevitch ,  Peter Nelson ,  David Oare ,  Vidya Prasad ,  Hyung-Jung Pyun ,  Adrian Ray ,  Sundaramoorthi Swaminathan ,  William Watkins ,  Jennifer Zhang ,  Lijun Zhang

Inventor： Constantine Boojamra ,  Carina Cannizzaro ,  James Chen ,  Xiaowu Chen ,  Aesop Cho ,  Lee Chong ,  Maria Fardis ,  Alan Huang ,  Choung Kim ,  Thorsten Kirschberg ,  Steven Krawczyk ,  Christopher Lee ,  Kuei-Ying Lin ,  Richard Mackman ,  David Markevitch ,  Peter Nelson ,  David Oare ,  Vidya Prasad ,  Hyung-Jung Pyun ,  Adrian Ray ,  Sundaramoorthi Swaminathan ,  William Watkins ,  Jennifer Zhang ,  Lijun Zhang

IPC: A61K31/7076 ,  A61K31/7072 ,  C07H19/04 ,  A61K31/675

CPC classification number: A61K31/7076 ,  A61K31/675 ,  A61K31/7072 ,  A61K47/548 ,  C07H19/04

Abstract: The invention is related to phosphorus substituted anti-cancer compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract translation: 本发明涉及磷取代的抗癌化合物，含有这些化合物的组合物和包括施用这些化合物的治疗方法以及可用于制备这些化合物的方法和中间体。

公开(公告)号：US20050261237A1

公开(公告)日：2005-11-24

申请号：US10832810

申请日：2004-04-26

Applicant: Constantine Boojamra ,  James Chen ,  Xiaowu Chen ,  Aesop Cho ,  Lee Chong ,  Maria Fardis ,  Alan Huang ,  Choung Kim ,  Thorsten Kirschberg ,  Christopher Lee ,  David Oare ,  Vidya Prasad ,  Adrian Ray ,  Sundaramoorthi Swaminathan ,  William Watkins

Inventor： Constantine Boojamra ,  James Chen ,  Xiaowu Chen ,  Aesop Cho ,  Lee Chong ,  Maria Fardis ,  Alan Huang ,  Choung Kim ,  Thorsten Kirschberg ,  Christopher Lee ,  David Oare ,  Vidya Prasad ,  Adrian Ray ,  Sundaramoorthi Swaminathan ,  William Watkins

IPC: A61K31/675 ,  A61K31/7072 ,  A61K31/7076

CPC classification number: C07F9/65616 ,  C07F9/65586 ,  C07F9/6561 ,  C07H7/04 ,  C07H19/056 ,  C07H19/06 ,  C07H19/14 ,  C07H19/173

Abstract: The invention is related to phosphorus substituted nucleoside compounds and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract translation: 本发明涉及磷取代的核苷化合物和包括施用这些化合物的治疗方法以及可用于制备这些化合物的方法和中间体。

公开(公告)号：US06693202B1

公开(公告)日：2004-02-17

申请号：US09645609

申请日：2000-08-25

Applicant: James Aggen ,  John H. Griffin ,  Mathai Mammen ,  Daniel Marquess ,  Edmund J. Moran ,  David Oare

Inventor： James Aggen ,  John H. Griffin ,  Mathai Mammen ,  Daniel Marquess ,  Edmund J. Moran ,  David Oare

IPC: C07D20700

CPC classification number: A61K31/40 ,  C07C211/32 ,  C07C2603/32 ,  C07D207/08 ,  C07D209/48 ,  C07D211/46 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D519/00 ,  G01N33/566

Abstract: Disclosed are multibinding compounds which are muscarinic receptor antagonists. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is, independently of each other, a muscarinic receptor antagonist or an allosteric modulator provided that at least one of said ligand is a muscarinic receptor antagonist. The multibinding compounds of this invention are useful in the treatment and prevention of diseases such as chronic obstructive pulmonary disease, chronic bronchitis, irritable bowel syndrome, urinary incontinence, and the like.

Abstract translation: 公开了作为毒蕈碱受体拮抗剂的多重联结化合物。 含有2-10个配体的本发明的多相结合化合物共价连接到一个或多个接头上。 每个配体彼此独立地是毒蕈碱受体拮抗剂或变构调节剂，只要至少一种所述配体是毒蕈碱受体拮抗剂即可。 本发明的多重联结化合物可用于治疗和预防慢性阻塞性肺疾病，慢性支气管炎，肠易激综合征，尿失禁等疾病。

公开(公告)号：US20090306134A1

公开(公告)日：2009-12-10

申请号：US12286528

申请日：2008-09-30

Applicant: James Aggen ,  John H. Griffin ,  Mathai Mammen ,  Daniel Marquess ,  Edmund J. Moran ,  David Oare

Inventor： James Aggen ,  John H. Griffin ,  Mathai Mammen ,  Daniel Marquess ,  Edmund J. Moran ,  David Oare

IPC: A61K31/4545 ,  A61K31/54 ,  A61K31/5377 ,  A61K31/495 ,  A61K31/445 ,  C07D413/12 ,  C07D403/06 ,  C07D401/06 ,  C07D211/00

CPC classification number: A61K31/40 ,  C07C211/32 ,  C07C2603/32 ,  C07D207/08 ,  C07D209/48 ,  C07D211/46 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D519/00 ,  G01N33/566

Abstract: Disclosed are multibinding compounds which are muscarinic receptor antagonists. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is, independently of each other, a muscarinic receptor antagonist or an allosteric modulator provided that at least one of said ligand is a muscarinic receptor antagonist. The multibinding compounds of this invention are useful in the treatment and prevention of diseases such as chronic obstructive pulmonary disease, chronic bronchitis, irritable bowel syndrome, urinary incontinence, and the like.

Abstract translation: 公开了作为毒蕈碱受体拮抗剂的多重联结化合物。 含有2-10个配体的本发明的多相结合化合物共价连接到一个或多个接头上。 每个配体彼此独立地是毒蕈碱受体拮抗剂或变构调节剂，只要至少一种所述配体是毒蕈碱受体拮抗剂即可。 本发明的多重联结化合物可用于治疗和预防慢性阻塞性肺疾病，慢性支气管炎，肠易激综合征，尿失禁等疾病。

公开(公告)号：US07368463B2

公开(公告)日：2008-05-06

申请号：US10888855

申请日：2004-07-09

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 ,  C07D401/12

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：US20060264404A1

公开(公告)日：2006-11-23

申请号：US11258621

申请日：2005-10-25

Applicant: Constantine Boojamra ,  Carina Cannizzaro ,  James Chen ,  Xiaowu Chen ,  Aesop Cho ,  Lee Chong ,  Manoj Desai ,  Maria Fardis ,  Craig Gibbs ,  Ralph Hirschmann ,  Alan Huang ,  Haolun Jin ,  Choung Kim ,  Thorsten Kirschberg ,  Steven Krawczyk ,  Christopher Lee ,  William Lee ,  Kuei-Ying Lin ,  Richard Mackman ,  David Markevitch ,  Peter Nelson ,  David Oare ,  Vidya Prasad ,  Hyung-Jung Pyun ,  Adrian Ray ,  Rosemarie Sherlock ,  Sundaramoorthi Swaminathan ,  William Watkins ,  Jennifer Zhang ,  Lijun Zhang

Inventor： Constantine Boojamra ,  Carina Cannizzaro ,  James Chen ,  Xiaowu Chen ,  Aesop Cho ,  Lee Chong ,  Manoj Desai ,  Maria Fardis ,  Craig Gibbs ,  Ralph Hirschmann ,  Alan Huang ,  Haolun Jin ,  Choung Kim ,  Thorsten Kirschberg ,  Steven Krawczyk ,  Christopher Lee ,  William Lee ,  Kuei-Ying Lin ,  Richard Mackman ,  David Markevitch ,  Peter Nelson ,  David Oare ,  Vidya Prasad ,  Hyung-Jung Pyun ,  Adrian Ray ,  Rosemarie Sherlock ,  Sundaramoorthi Swaminathan ,  William Watkins ,  Jennifer Zhang ,  Lijun Zhang

IPC: A61K31/675 ,  C07F9/6512

CPC classification number: C07F9/65616 ,  C07F9/4006 ,  C07F9/4465 ,  C07F9/5304 ,  C07F9/650952 ,  C07F9/653 ,  C07F9/65507 ,  C07F9/65515 ,  C07F9/65517 ,  C07F9/65583 ,  C07F9/65586 ,  C07F9/6561

Abstract: The invention is related to phosphorus substituted therapeutic agents, compositions containing such phosphorus substituted agents, and therapeutic methods that include the administration of such phosphorus substituted agents, as well as to processes and intermediates useful for preparing such agents.

Abstract translation: 本发明涉及磷取代的治疗剂，含有这种磷取代剂的组合物，以及包括施用这种磷取代剂的治疗方法，以及可用于制备这种药剂的方法和中间体。

公开(公告)号：US20060252791A1

公开(公告)日：2006-11-09

申请号：US11316050

申请日：2005-12-21

Applicant: Steven Bondy ,  David Oare ,  Winston Tse

Inventor： Steven Bondy ,  David Oare ,  Winston Tse

IPC: A61K31/4745 ,  C07D471/02

CPC classification number: C07D471/04

Abstract: The compound 5-((3-(2,4-trifluoromethyphenyl)isoxazol-5-yl)methyl)-2-(2-fluorophenyl)-5H-imidazo[4,5-c]pyridine, together with the salts and solvates thereof. Also provided are compositions comprising this compound and pharmaceutically acceptable carriers, as well as the use of such compositions in the treatment or prophylaxis of viral infections.

Abstract translation: 化合物5 - （（3-（2,4-三氟甲基苯基）异恶唑-5-基）甲基）-2-（2-氟苯基）-5H-咪唑并[4,5-c]吡啶与盐和溶剂合物 其中。 还提供了包含该化合物和药学上可接受的载体的组合物，以及这些组合物在治疗或预防病毒感染中的用途。

公开(公告)号：US20060199788A1

公开(公告)日：2006-09-07

申请号：US10833294

申请日：2004-04-26

Applicant: Carina Cannizzaro ,  James Chen ,  Xiaowu Chen ,  Aesop Cho ,  Lee Chong ,  Maria Fardis ,  Craig Gibbs ,  Ralph Hirschmann ,  Thorsten Kirschberg ,  Christopher Lee ,  Kuei-Ying Lin ,  Richard Mackman ,  Peter Nelson ,  David Oare ,  Hyung-Jung Pyun ,  Adrian Ray ,  Rosemarie Sherlock ,  Sundaramoorthi Swaminathan ,  William Watkins ,  Jennifer Zhang

Inventor： Carina Cannizzaro ,  James Chen ,  Xiaowu Chen ,  Aesop Cho ,  Lee Chong ,  Maria Fardis ,  Craig Gibbs ,  Ralph Hirschmann ,  Thorsten Kirschberg ,  Christopher Lee ,  Kuei-Ying Lin ,  Richard Mackman ,  Peter Nelson ,  David Oare ,  Hyung-Jung Pyun ,  Adrian Ray ,  Rosemarie Sherlock ,  Sundaramoorthi Swaminathan ,  William Watkins ,  Jennifer Zhang

IPC: A61K31/66 ,  C07F9/02

CPC classification number: C07F9/65583 ,  A61K31/60 ,  A61K47/548 ,  C07F9/4006 ,  C07F9/4021 ,  C07F9/46 ,  C07F9/572 ,  C07F9/5728 ,  C07F9/65031 ,  C07F9/65038 ,  C07F9/650905 ,  C07F9/6524 ,  C07F9/653 ,  C07F9/65515 ,  C07F9/65517 ,  C07F9/65586 ,  C07F9/6561 ,  C07F9/65616

Abstract: The invention is related to phosphorus substituted anti-inflammatory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract translation: 本发明涉及磷取代的抗炎化合物，含有这些化合物的组合物，以及包括施用这些化合物的治疗方法以及可用于制备这些化合物的方法和中间体。