公开(公告)号：US20080015200A1

公开(公告)日：2008-01-17

申请号：US11827354

申请日：2007-07-10

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: A61K31/519 ,  A61K31/4985 ,  A61P1/00 ,  A61P17/00 ,  A61P27/00 ,  A61P37/00 ,  A61P5/00 ,  A61P9/00 ,  C07D239/70 ,  C07D403/14

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.

Abstract translation: 描述了苯并呋喃和苯并噻吩并嘧啶化合物，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：US07253203B2

公开(公告)日：2007-08-07

申请号：US11378851

申请日：2006-03-17

Applicant: Andrew Fensome ,  Lori L. Miller ,  John W. Ullrich ,  Reinhold H. W. Bender ,  Puwen Zhang ,  Jay E. Wrobel ,  Lin Zhi ,  Todd K. Jones ,  James P. Edwards ,  Christopher M. Tegley

Inventor： Andrew Fensome ,  Lori L. Miller ,  John W. Ullrich ,  Reinhold H. W. Bender ,  Puwen Zhang ,  Jay E. Wrobel ,  Lin Zhi ,  Todd K. Jones ,  James P. Edwards ,  Christopher M. Tegley

IPC: C07D401/02 ,  C07D403/02 ,  A61K31/404 ,  A61K31/4439

CPC classification number: C07D209/34 ,  C07D209/96 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D491/10

Abstract: This invention relates to substituted indoline derivative compounds which are antagonists of the progesterone receptor, their preparation and pharmaceutical utility, particularly including contraception and treatment of benign or malignant neoplastic diseases, having the general structure: wherein R1 and R2 may be single substituents or fused to form spirocyclic rings.

Abstract translation: 本发明涉及作为孕酮受体拮抗剂的取代二氢吲哚衍生物化合物，其制备方法和药物应用，特别是包括具有以下一般结构的良性或恶性肿瘤疾病的避孕和治疗：其中R 1和 R 2可以是单个取代基或稠合形成螺环。

公开(公告)号：US07091234B2

公开(公告)日：2006-08-15

申请号：US10969531

申请日：2004-10-20

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: 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，其具有以下通式结构：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，以及使用这些化合物的方法 诱导避孕或治疗孕激素相关的癌和腺癌。

公开(公告)号：US06949540B2

公开(公告)日：2005-09-27

申请号：US10401486

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 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06

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.

Abstract translation: 描述了取代的吡唑，其制备方法，含有它们的组合物，以及使用它们来治疗例如由组织蛋白酶S介导的自身免疫性疾病的方法。

公开(公告)号：US06936603B2

公开(公告)日：2005-08-30

申请号：US10402694

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 ,  A61K31/4985 ,  A61K31/5025 ,  A61K31/519

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：US06759408B2

公开(公告)日：2004-07-06

申请号：US10141792

申请日：2002-05-09

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

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

IPC: A61K31535

CPC classification number: A61K31/535 ,  A61K31/56 ,  Y10S514/843 ,  A61K2300/00

Abstract: This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds which are antagonists of the progesterone receptor having the general structure: wherein R1 and R2 may be single substituents or fused; R3 is H, OH, NH2, C1 to C6 alkyl, CORC, or optionally substituted C1 to C6 alkyl, C3 to C6 alkenyl, or alkynyl; RC is H, or optionally substituted C1 to C3 alkyl, aryl, C1 to C3 alkoxy, or C1 to C3 aminoalkyl; R4 is H, halogen, CN, NO2, or optionally substituted C1 to C6 alkyl, alkynyl, C1 to C6 alkoxy, amino, or C1 to C6 aminoalkyl; and R5 is a benzene ring, a five or six membered heterocyclic ring; or pharmaceutically acceptable salt thereof. Methods of treatment include contraception, secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, carcinomas, adenocarcinomas minimization of side effects, or food intake stimulation.

Abstract translation: 本发明涉及使用具有通式结构的孕酮受体的拮抗剂的取代的二氢吲哚衍生物化合物的环状组合疗法和方案：其中R 1和R 2可以是单个取代基或稠合的; R 3是H，OH，NH 2，C 1 -C 6烷基，COR C或任选取代的C 1 -C 6烷基，C 3至C 6烯基或炔基; R C是H或任选取代的C 1至C 3烷基，芳基，C 1至C 3烷氧基或C 1至C 3氨基烷基; R 4是H，卤素，CN，NO 2或任选取代的C 1至C 6烷基，炔基，C 1至C 6烷氧基，氨基或C 1至C 6氨基烷基; 和R 5为苯环，五或六元杂环; 或其药学上可接受的盐。 治疗方法包括避孕，继发性闭经，功能障碍性出血，子宫平滑肌瘤，子宫内膜异位症，多囊卵巢综合征，癌，腺癌最小化副作用或食物摄取刺激。

公开(公告)号：US06579896B2

公开(公告)日：2003-06-17

申请号：US09946713

申请日：2001-09-05

Applicant: Hui Cai ,  James P. Edwards ,  Yin Gu ,  Lars Karlsson ,  Steven P. Meduna ,  Barbara A. Pio ,  Siquan Sun ,  Robin L. Thurmond ,  Jianmei Wei

Inventor： Hui Cai ,  James P. Edwards ,  Yin Gu ,  Lars Karlsson ,  Steven P. Meduna ,  Barbara A. Pio ,  Siquan Sun ,  Robin L. Thurmond ,  Jianmei Wei

IPC: A61K31415

CPC classification number: A61K31/4745 ,  A61K31/00 ,  A61K31/13 ,  A61K31/275 ,  A61K31/4155 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/495 ,  A61K31/496 ,  A61K31/519 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55

Abstract: A method for the treatment of an allergic condition, including an an atopic allergic conditions, using substituted pyrazoles.

公开(公告)号：US06506766B1

公开(公告)日：2003-01-14

申请号：US09610638

申请日：2000-07-05

Applicant: Michael J. Coghlan ,  James P. Edwards ,  Steven W. Elmore ,  Todd K. Jones ,  Michael E. Kort ,  Philip R. Kym ,  Jimmie L. Moore ,  John K. Pratt ,  Alan X. Wang

Inventor： Michael J. Coghlan ,  James P. Edwards ,  Steven W. Elmore ,  Todd K. Jones ,  Michael E. Kort ,  Philip R. Kym ,  Jimmie L. Moore ,  John K. Pratt ,  Alan X. Wang

IPC: A61K314741

CPC classification number: C07D491/04

Abstract: Compounds having Formula I are useful for partially or fully antagonizing, repressing, agonizing, or modulating the glucocorticoid receptor and treating immune, autoimmune and inflammatory diseases in a mammal. Also disclosed are pharmaceutical compositions comprising compounds of Formula I and methods of inhibiting immune or autoimmune diseases in a mammal.

Abstract translation: 具有式I的化合物可用于部分或完全拮抗，抑制，激动或调节糖皮质激素受体并在哺乳动物中治疗免疫，自身免疫和炎性疾病。 还公开了包含式I化合物的药物组合物和在哺乳动物中抑制免疫或自身免疫性疾病的方法。

公开(公告)号：US06448405B1

公开(公告)日：2002-09-10

申请号：US08947428

申请日：1997-10-08

Applicant: Todd K. Jones ,  Lin Zhi ,  James P. Edwards ,  Christopher M. Tegley ,  Sarah J. West

Inventor： Todd K. Jones ,  Lin Zhi ,  James P. Edwards ,  Christopher M. Tegley ,  Sarah J. West

IPC: C07D491052

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：US06391907B1

公开(公告)日：2002-05-21

申请号：US09552632

申请日：2000-04-19

Applicant: Andrew Fensome ,  Lori L. Miller ,  John W. Ullrich ,  Reinhold H. W. Bender ,  Puwen Zhang ,  Jay E. Wrobel ,  Lin Zhi ,  Todd K. Jones ,  James P. Edwards ,  Christopher M. Tegley

Inventor： Andrew Fensome ,  Lori L. Miller ,  John W. Ullrich ,  Reinhold H. W. Bender ,  Puwen Zhang ,  Jay E. Wrobel ,  Lin Zhi ,  Todd K. Jones ,  James P. Edwards ,  Christopher M. Tegley

IPC: A61K314015

CPC classification number: C07D209/34 ,  C07D209/96 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D491/10

Abstract: This invention relates to substituted indoline derivative compounds which are antagonists of the progesterone receptor, their preparation and pharmaceutical utility, particularly including contraception and treatment of benign or malignant neoplastic diseases, having the general structure: wherein R1 and R2 may be single substituents or fused to form spirocyclic rings.

Abstract translation: 本发明涉及作为孕酮受体拮抗剂的取代二氢吲哚衍生物，其制备和药物应用，特别是包括具有以下通式结构的良性或恶性肿瘤性疾病的避孕和治疗：其中R1和R2可以是单取代基或与 形成螺环。