公开(公告)号：US20090325927A1

公开(公告)日：2009-12-31

申请号：US12496932

申请日：2009-07-02

Applicant: Frank Chavez ,  Michael P. Curtis ,  James P. Edwards ,  Laurent Gomez ,  Cheryl A. Grice ,  Aaron M. Kearney ,  Brad M. Savall

Inventor： Frank Chavez ,  Michael P. Curtis ,  James P. Edwards ,  Laurent Gomez ,  Cheryl A. Grice ,  Aaron M. Kearney ,  Brad M. Savall

IPC: A61K31/496 ,  C07D491/048 ,  C07D405/14 ,  A61K31/551 ,  A61K31/397 ,  A61P37/00

CPC classification number: C07D491/048 ,  C07D491/147 ,  C07D495/04 ,  C07D519/00

Abstract: Benzofuro- and benzothienopyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.

公开(公告)号：US20090118274A1

公开(公告)日：2009-05-07

申请号：US12031579

申请日：2008-02-14

Applicant: Darin Allen ,  Michael K. Ameriks ,  Frank U. Axe ,  Matthew Burdett ,  Hui Cai ,  Ingrid Choong ,  James P. Edwards ,  Willard Lew ,  Steven P. Meduna

Inventor： Darin Allen ,  Michael K. Ameriks ,  Frank U. Axe ,  Matthew Burdett ,  Hui Cai ,  Ingrid Choong ,  James P. Edwards ,  Willard Lew ,  Steven P. Meduna

IPC: A61K31/5377 ,  C07D471/04 ,  A61K31/496 ,  A61K31/4375 ,  A61P29/00 ,  A61P25/00 ,  A61P35/00 ,  A61P1/00 ,  A61P37/00 ,  A61K31/4545 ,  C07D471/10

CPC classification number: C07D471/04

Abstract: Monocyclic aminopropyl tetrahydro-pyrazolo-pyridine compounds are described, which are useful as cathepsin S modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by cathepsin S activity, such as psoriasis, pain, multiple sclerosis, atherosclerosis, and rheumatoid arthritis.

Abstract translation: 描述了单环氨基丙基四氢 - 吡唑并吡啶化合物，其可用作组织蛋白酶S调节剂。 这些化合物可用于治疗由组织蛋白酶S活性介导的疾病状态，病症和病症的药物组合物和方法，例如银屑病，疼痛，多发性硬化，动脉粥样硬化和类风湿性关节炎。

公开(公告)号：US20090111802A1

公开(公告)日：2009-04-30

申请号：US12326385

申请日：2008-12-02

Applicant: Puwen Zhang ,  Eugene A. Terefenko ,  Andrew Fensome ,  Jay E. Wrobel ,  Horace Fletcher, III ,  Lin Zhi ,  Todd K. Jones ,  James P. Edwards ,  Christopher M. Tegley

Inventor： Puwen Zhang ,  Eugene A. Terefenko ,  Andrew Fensome ,  Jay E. Wrobel ,  Horace Fletcher, III ,  Lin Zhi ,  Todd K. Jones ,  James P. Edwards ,  Christopher M. Tegley

IPC: A61K31/536

CPC classification number: C07D265/18 ,  C07D413/04 ,  C07D413/10 ,  C07D417/04

Abstract: This invention provides compounds of Formula (I): wherein R1 and R2 are independent substituents or are fused to form spirocyclic rings; R3, RC, and R4 are as defined herein; and R5 is a substituted benzene ring or a substituted five or six membered heterocyclic ring having in its backbone 1, 2, or 3 heteroatoms including O, S, SO, SO2 or NR6; or pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods using the compounds as antagonists of the progesterone receptor.

Abstract translation: 本发明提供式（I）的化合物：其中R 1和R 2是独立的取代基或稠合形成螺环; R3，RC和R4如本文所定义; 并且R5是取代的苯环或其主链1,2或3个杂原子包括O，S，SO，SO 2或NR 6的取代的五元或六元杂环; 或其药学上可接受的盐，以及使用该化合物作为孕酮受体的拮抗剂的药物组合物和方法。

公开(公告)号：US07432378B2

公开(公告)日：2008-10-07

申请号：US10952989

申请日：2004-09-29

Applicant: James P. Edwards ,  Michael D. Hack ,  David E. Kindrachuk ,  Jennifer D. Venable

Inventor： James P. Edwards ,  Michael D. Hack ,  David E. Kindrachuk ,  Jennifer D. Venable

IPC: C07D211/68 ,  C07D211/80 ,  C07D213/02

CPC classification number: C07D235/18 ,  C04B35/632 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07K16/00 ,  C07K2317/50 ,  C07K2317/53 ,  C07K2318/10

Abstract: Benzoimidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.

Abstract translation: 苯并咪唑化合物，组合物及其在白细胞募集抑制中的用途，调节H4受体以及治疗诸如炎症，H 4受体介导的病症的病症， 和相关条件。

公开(公告)号：US20070238771A1

公开(公告)日：2007-10-11

申请号：US11731047

申请日：2007-03-30

Applicant: James P. Edwards ,  Brad M. Savall ,  Chandravadan R. Shah

Inventor： James P. Edwards ,  Brad M. Savall ,  Chandravadan R. Shah

IPC: A61K31/4184 ,  A61K31/405 ,  C07D403/14

CPC classification number: C07D403/14 ,  C07D403/06 ,  C07D471/04 ,  C07D487/08

Abstract: Benzoimidazole and indole compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.

Abstract translation: 描述了苯并咪唑和吲哚化合物，其可用作H 4 S 5受体调节剂。 这样的化合物可以用于治疗由H 4 S受体活性介导的疾病状态，病症和病症的药物组合物和方法，例如过敏，哮喘，自身免疫疾病和瘙痒症。

公开(公告)号：US06951851B2

公开(公告)日：2005-10-04

申请号：US10402696

申请日：2003-03-28

Applicant: Hui Cai ,  James P. Edwards ,  Steven P. Meduna ,  Barbara A. Pio ,  Jianmei Wei

Inventor： Hui Cai ,  James P. Edwards ,  Steven P. Meduna ,  Barbara A. Pio ,  Jianmei Wei

IPC: A61K31/275 ,  A61K31/4155 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/495 ,  A61K31/55 ,  A61P11/06 ,  A61P19/02 ,  A61P29/00 ,  A61P37/06 ,  C07D413/14 ,  C07D471/04 ,  C07D471/14 ,  C07D519/00 ,  C07D487/04 ,  A61K31/53

CPC classification number: C07D413/14 ,  A61K31/275 ,  A61K31/4155 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/495 ,  A61K31/55 ,  C07D401/14 ,  C07D409/14 ,  C07D471/04 ,  C07D471/14

Abstract: Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S are described.

公开(公告)号：US06841568B2

公开(公告)日：2005-01-11

申请号：US10420276

申请日：2003-04-22

Applicant: Andrew Fensome ,  Puwen Zhang ,  Marci C. Koko ,  Jay E. Wrobel ,  Edward G. Melenski ,  Lin Zhi ,  Todd K. Jones ,  Christopher M. Tegley ,  James P. Edwards

Inventor： Andrew Fensome ,  Puwen Zhang ,  Marci C. Koko ,  Jay E. Wrobel ,  Edward G. Melenski ,  Lin Zhi ,  Todd K. Jones ,  Christopher M. Tegley ,  James P. Edwards

IPC: C07D409/10 ,  A61K31/404 ,  A61P1/00 ,  A61P5/34 ,  A61P5/36 ,  A61P7/00 ,  A61P7/04 ,  A61P13/08 ,  A61P15/00 ,  A61P35/00 ,  A61P43/00 ,  C07D209/08 ,  C07D209/30 ,  C07D209/40 ,  C07D209/96 ,  A61K31/405 ,  C07D209/04

CPC classification number: C07D209/40 ,  C07D209/08 ,  C07D209/30

Abstract: This invention relates to compounds which are agonists of the progesterone receptor which have the general structure: wherein: R1, R2, R3, R4, R5 and Q1 are as defined herein, or a pharmaceutically acceptable salt thereof, as well as methods of using these compounds to induce contraception or treat progesterone-related carcinomas and adenocarcinomas.

Abstract translation: 本发明涉及作为孕酮受体激动剂的化合物，其具有以下通式：其中：R 1，R 2，R 3，R 4，R 5和Q 1如本文所定义，或其药学上可接受的盐，以及方法 使用这些化合物诱导避孕或治疗孕酮相关的癌和腺癌。

公开(公告)号：US06696459B1

公开(公告)日：2004-02-24

申请号：US08950032

申请日：1997-10-14

Applicant: Todd K. Jones ,  Mark E. Goldman ,  Charlotte L. F. Pooley ,  David T. Winn ,  James P. Edwards ,  Sarah J. West ,  Christopher M. Tegley ,  Lin Zhi ,  Lawrence G. Hamann ,  Luc J. Farmer ,  Robert L. Davis

Inventor： Todd K. Jones ,  Mark E. Goldman ,  Charlotte L. F. Pooley ,  David T. Winn ,  James P. Edwards ,  Sarah J. West ,  Christopher M. Tegley ,  Lin Zhi ,  Lawrence G. Hamann ,  Luc J. Farmer ,  Robert L. Davis

IPC: A61K314353

CPC classification number: C07D401/04 ,  C07D215/06 ,  C07D221/18 ,  C07D311/80 ,  C07D413/04 ,  C07D417/04 ,  C07D471/04 ,  C07D491/04

Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.

Abstract translation: 公开了用于类固醇受体的高亲和力，高选择性调节剂的非甾体化合物。 还公开了掺入这种化合物的药物组合物，使用所公开的化合物的方法和用于治疗需要类固醇受体激动剂或拮抗剂治疗的患者的组合物，可用于制备化合物的中间体和用于制备类固醇受体调节剂化合物的方法。

公开(公告)号：US06635633B2

公开(公告)日：2003-10-21

申请号：US09927188

申请日：2001-08-10

Applicant: Hui Cai ,  James P. Edwards ,  Steven P. Meduna ,  Barbara A. Pio ,  Jianmei Wei

Inventor： Hui Cai ,  James P. Edwards ,  Steven P. Meduna ,  Barbara A. Pio ,  Jianmei Wei

IPC: C07D48704

CPC classification number: C07D413/14 ,  A61K31/275 ,  A61K31/4155 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/495 ,  A61K31/55 ,  C07D401/14 ,  C07D409/14 ,  C07D471/04 ,  C07D471/14

Abstract: Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S are described.

公开(公告)号：US06583145B1

公开(公告)日：2003-06-24

申请号：US10253380

申请日：2002-09-24

Applicant: Andrew Fensome ,  Puwen Zhang ,  Marci C. Koko ,  Lin Zhi ,  Todd K. Jones ,  Jay E. Wrobel ,  Christopher M. Tegley ,  James P. Edwards ,  Edward G. Melenski

Inventor： Andrew Fensome ,  Puwen Zhang ,  Marci C. Koko ,  Lin Zhi ,  Todd K. Jones ,  Jay E. Wrobel ,  Christopher M. Tegley ,  James P. Edwards ,  Edward G. Melenski

IPC: A61K31404

CPC classification number: C07D209/40 ,  C07D209/08 ,  C07D209/30

Abstract: This invention relates to compounds which are agonists of the progesterone receptor which have the general structure: wherein: R1, R2, R3, R4, R5 and Q1 are as defined herein, or a pharmaceutically acceptable salt thereof, as well as methods of using these compounds to induce contraception or treat progesterone-related carcinomas and adenocarcinomas.

Abstract translation: 本发明涉及作为孕酮受体的激动剂的具有以下通式结构的化合物：其中：R1，R2，R3，R4，R5和Q1如本文所定义，或其药学上可接受的盐，以及使用它们的方法 化合物诱导避孕或治疗孕激素相关的癌和腺癌。