公开(公告)号：US07320992B2

公开(公告)日：2008-01-22

申请号：US10926238

申请日：2004-08-24

Applicant: Christopher Tegley ,  Jeffrey A. Adams ,  Benny C. Askew, Jr. ,  Michael Croghan ,  Daniel Elbaum ,  Julie Germain ,  Gregory J. Habgood ,  Scott Harried ,  Aiwen Li ,  Nobuko Nishimura ,  Rana Nomak ,  Andrew Tasker ,  Kevin Yang

Inventor： Christopher Tegley ,  Jeffrey A. Adams ,  Benny C. Askew, Jr. ,  Michael Croghan ,  Daniel Elbaum ,  Julie Germain ,  Gregory J. Habgood ,  Scott Harried ,  Aiwen Li ,  Nobuko Nishimura ,  Rana Nomak ,  Andrew Tasker ,  Kevin Yang

IPC: A61K31/4439 ,  C07D401/12

CPC classification number: C04B35/632 ,  C07D401/12 ,  C07D401/14

Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract translation: 所选化合物对于预防和治疗诸如血管生成介导的疾病等疾病是有效的。 本发明包括新颖的化合物，类似物，前药和药学上可接受的盐，用于预防和治疗疾病和其它疾病或涉及癌症等的病症的药物组合物和方法。 本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。

公开(公告)号：US20070259944A1

公开(公告)日：2007-11-08

申请号：US11821384

申请日：2007-06-22

Applicant: Andrew Fensome ,  Lori Miller ,  John Ullrich ,  Reinhold Bender ,  Puwen Zhang ,  Jay Wrobel ,  Lin Zhi ,  Todd Jones ,  James Edwards ,  Christopher Tegley

Inventor： Andrew Fensome ,  Lori Miller ,  John Ullrich ,  Reinhold Bender ,  Puwen Zhang ,  Jay Wrobel ,  Lin Zhi ,  Todd Jones ,  James Edwards ,  Christopher Tegley

IPC: A61K31/404 ,  C07D209/04

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.

公开(公告)号：US20070197598A1

公开(公告)日：2007-08-23

申请号：US11598238

申请日：2006-11-13

Applicant: Martin Henriksson ,  Evert Homan ,  Lars Johansson ,  Jerk Vallgarda ,  Meredith Williams ,  Eric Bercot ,  Christopher Fotsch ,  Aiwen Li ,  Guolin Cai ,  Randall Hungate ,  Chester Yuan ,  Christopher Tegley ,  David Jean ,  Nianhe Han ,  Qi Huang ,  Qingyian Liu ,  Michael Bartberger ,  George Moniz ,  Matthew Frizzle ,  Teresa Marshall

Inventor： Martin Henriksson ,  Evert Homan ,  Lars Johansson ,  Jerk Vallgarda ,  Meredith Williams ,  Eric Bercot ,  Christopher Fotsch ,  Aiwen Li ,  Guolin Cai ,  Randall Hungate ,  Chester Yuan ,  Christopher Tegley ,  David Jean ,  Nianhe Han ,  Qi Huang ,  Qingyian Liu ,  Michael Bartberger ,  George Moniz ,  Matthew Frizzle ,  Teresa Marshall

IPC: A61K31/454 ,  A61K31/4439 ,  A61K31/426 ,  C07D417/02 ,  C07D277/34

CPC classification number: C07D277/54 ,  C07D277/60 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14

Abstract: The present invention relates to thiazolinones and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-β-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.

Abstract translation: 本发明涉及噻唑啉酮以及包含该化合物的药物组合物，以及该化合物用于治疗与人类11-β-羟基类固醇脱氢酶1型酶有关的病症的用途的方法以及用于制备作用于 人类11-β-羟基类固醇脱氢酶1型酶。

公开(公告)号：US20060160882A1

公开(公告)日：2006-07-20

申请号：US11378851

申请日：2006-03-17

Applicant: Andrew Fensome ,  Lori Miller ,  John Ullrich ,  Reinhold Bender ,  Puwen Zhang ,  Jay Wrobel ,  Lin Zhi ,  Todd Jones ,  James Edwards ,  Christopher Tegley

Inventor： Andrew Fensome ,  Lori Miller ,  John Ullrich ,  Reinhold Bender ,  Puwen Zhang ,  Jay Wrobel ,  Lin Zhi ,  Todd Jones ,  James Edwards ,  Christopher Tegley

IPC: A61K31/404 ,  C07D409/02 ,  C07D405/02 ,  C07D403/02

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：US20060142357A1

公开(公告)日：2006-06-29

申请号：US11135662

申请日：2005-05-24

Applicant: Martin Henriksson ,  Evert Homan ,  Lars Johansson ,  Jerk Vallgarda ,  Meredith Williams ,  Eric Bercot ,  Christopher Fotsch ,  Aiwen Li ,  Guolin Cai ,  Randall Hungate ,  Chester Yuan ,  Christopher Tegley ,  David Jean ,  Nianhe Han ,  Qi Huang ,  Qingyian Liu ,  Michael Bartberger ,  George Moniz ,  Matthew Frizzle

Inventor： Martin Henriksson ,  Evert Homan ,  Lars Johansson ,  Jerk Vallgarda ,  Meredith Williams ,  Eric Bercot ,  Christopher Fotsch ,  Aiwen Li ,  Guolin Cai ,  Randall Hungate ,  Chester Yuan ,  Christopher Tegley ,  David Jean ,  Nianhe Han ,  Qi Huang ,  Qingyian Liu ,  Michael Bartberger ,  George Moniz ,  Matthew Frizzle

IPC: A61K31/426 ,  A61K31/421 ,  C07D277/04 ,  C07D263/04

CPC classification number: C07D417/06 ,  C07D263/34 ,  C07D263/48 ,  C07D275/03 ,  C07D277/42 ,  C07D277/54 ,  C07D277/60 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D513/10 ,  C07F7/1804

Abstract: The present invention relates to compounds with the formula (I), (II), (III) or (IV): wherein R1, R2, R3, R4, R5, R6, R7, X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-β-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.

Abstract translation: 本发明涉及具有式（I），（II），（III）或（IV）的化合物：其中R 1，R 2，R 2， 3，R 4，R 5，R 6，R 7，X和Z分别为 以及包含该化合物的药物组合物的使用方法，以及该化合物用于治疗与人类11-β-羟基类固醇脱氢酶1型酶相关的病症和用于制备作用于人的药物的方法 11-β-羟基类固醇脱氢酶1型酶。

公开(公告)号：US20050054711A1

公开(公告)日：2005-03-10

申请号：US10969531

申请日：2004-10-20

Applicant: Andrew Fensome ,  Puwen Zhang ,  Marci Koko ,  Lin Zhi ,  Todd Jones ,  Jay Wrobel ,  Christopher Tegley ,  James Edwards ,  Edward Melenski

Inventor： Andrew Fensome ,  Puwen Zhang ,  Marci Koko ,  Lin Zhi ,  Todd Jones ,  Jay Wrobel ,  Christopher Tegley ,  James Edwards ,  Edward Melenski

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 ,  C07D209/36 ,  C07D43/02

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：US08686011B2

公开(公告)日：2014-04-01

申请号：US13233699

申请日：2011-09-15

Applicant: Martin Henriksson ,  Evert Homan ,  Lars Johansson ,  Jerk Vallgarda ,  Meredith Williams ,  Eric A. Bercot ,  Christopher H. Fotsch ,  Aiwen Li ,  Guolin Cai ,  Randall W. Hungate ,  Chester Chenguang Yuan ,  Christopher Tegley ,  David J. St. Jean, Jr. ,  Nianhe Han ,  Qi Huang ,  Qingyian Liu ,  Michael D. Bartberger ,  George A. Moniz ,  Matthew J. Frizzle

Inventor： Martin Henriksson ,  Evert Homan ,  Lars Johansson ,  Jerk Vallgarda ,  Meredith Williams ,  Eric A. Bercot ,  Christopher H. Fotsch ,  Aiwen Li ,  Guolin Cai ,  Randall W. Hungate ,  Chester Chenguang Yuan ,  Christopher Tegley ,  David J. St. Jean, Jr. ,  Nianhe Han ,  Qi Huang ,  Qingyian Liu ,  Michael D. Bartberger ,  George A. Moniz ,  Matthew J. Frizzle

IPC: A61K31/427 ,  C07D277/34 ,  C07D277/38 ,  C07D277/42

CPC classification number: C07D277/54 ,  C07D263/34 ,  C07D275/03 ,  C07D277/60 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D513/10

Abstract: The present invention relates to compounds with the formula (I), (II), (III) or (IV): wherein R1, R2, R3, R4, R5, R6, R7, X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-β-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.

Abstract translation: 本发明涉及具有式（I），（II），（III）或（IV）的化合物：其中R1，R2，R3，R4，R5，R6，R7，X和Z如本文所定义， 涉及包含该化合物的药物组合物，以及该化合物用于治疗与人类11-羟基类固醇脱氢酶1型酶相关的病症的用途和用于制备作用于人类11- 羟类固醇脱氢酶1型酶。

公开(公告)号：US07390820B2

公开(公告)日：2008-06-24

申请号：US10926218

申请日：2004-08-24

Applicant: Christopher Tegley

Inventor： Christopher Tegley

IPC: C07D217/22 ,  A61K31/4704

CPC classification number: C04B35/632 ,  C07D217/24 ,  C07D401/12 ,  C07D401/14 ,  C07D409/14 ,  C07D471/04 ,  C07D487/04

Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract translation: 所选化合物对于预防和治疗诸如血管生成介导的疾病等疾病是有效的。 本发明包括新颖的化合物，类似物，前药和药学上可接受的盐，用于预防和治疗疾病和其它疾病或涉及癌症等的病症的药物组合物和方法。 本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。

公开(公告)号：US20070249605A1

公开(公告)日：2007-10-25

申请号：US11635683

申请日：2006-12-08

Applicant: Jennifer Allen ,  Kaustav Biswas ,  Roland Burli ,  Jennifer Dao ,  Michael Frohn ,  Jennifer Golden ,  Randall Hungate ,  Robert Kurzeja ,  Stephanie Mercede ,  Kristine Muller ,  Susana Neira ,  Tanya Peterkin ,  Christopher Tegley ,  Violeta Yu

Inventor： Jennifer Allen ,  Kaustav Biswas ,  Roland Burli ,  Jennifer Dao ,  Michael Frohn ,  Jennifer Golden ,  Randall Hungate ,  Robert Kurzeja ,  Stephanie Mercede ,  Kristine Muller ,  Susana Neira ,  Tanya Peterkin ,  Christopher Tegley ,  Violeta Yu

IPC: A61K31/47 ,  A61K31/495 ,  A61K31/506 ,  A61K31/5377 ,  A61P35/00 ,  A61P5/00 ,  A61P7/00 ,  A61P9/00 ,  C07D215/00 ,  C07D237/02 ,  C07D239/02 ,  C07D265/30 ,  G01N33/53

CPC classification number: C07D215/22 ,  C07D215/56 ,  C07D401/04 ,  C07D405/04 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  G01N33/542

Abstract: This invention relates to new quinolone based compounds that exhibit prolyl hydroxylase inhibitory activity. This invention also relates to methods of increasing HIF levels or activity in a subject or treating a condition associated with HIF levels or activity in a subject by administering to the subject at least one quinolone based compound. This invention further involves assays for the detection of a hydroxyproline residue in a HIF molecule.

Abstract translation: 本发明涉及显示脯氨酰羟化酶抑制活性的新型喹诺酮类化合物。 本发明还涉及通过向受试者施用至少一种基于喹诺酮的化合物来增加受试者中HIF水平或活性或治疗与受试者中HIF水平或活性相关的病症的方法。 本发明还涉及用于检测HIF分子中的羟脯氨酸残基的测定法。

公开(公告)号：US07253196B2

公开(公告)日：2007-08-07

申请号：US11135662

申请日：2005-05-24

Applicant: Martin Henriksson ,  Evert Homan ,  Lars Johansson ,  Jerk Vallgarda ,  Meredith Williams ,  Eric A. Bercot ,  Christopher H. Fotsch ,  Aiwen Li ,  Guolin Cai ,  Randall W. Hungate ,  Chester Chenguang Yuan ,  Christopher Tegley ,  David J. St. Jean, Jr. ,  Nianhe Han ,  Qi Huang ,  Qingyian Liu ,  Michael D. Bartberger ,  George A. Moniz ,  Matthew J. Frizzle

Inventor： Martin Henriksson ,  Evert Homan ,  Lars Johansson ,  Jerk Vallgarda ,  Meredith Williams ,  Eric A. Bercot ,  Christopher H. Fotsch ,  Aiwen Li ,  Guolin Cai ,  Randall W. Hungate ,  Chester Chenguang Yuan ,  Christopher Tegley ,  David J. St. Jean, Jr. ,  Nianhe Han ,  Qi Huang ,  Qingyian Liu ,  Michael D. Bartberger ,  George A. Moniz ,  Matthew J. Frizzle

IPC: A61K31/426 ,  C07D279/06

CPC classification number: C07D417/06 ,  C07D263/34 ,  C07D263/48 ,  C07D275/03 ,  C07D277/42 ,  C07D277/54 ,  C07D277/60 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D513/10 ,  C07F7/1804

Abstract: The present invention relates to compounds with the formula (I), (II), (III) or (IV): wherein R1, R2, R3, R4, R5, R6, R7, X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-β-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.

Abstract translation: 本发明涉及具有式（I），（II），（III）或（IV）的化合物：其中R 1，R 2，R 2， 3，R 4，R 5，R 6，R 7，X和Z分别为 以及包含该化合物的药物组合物的使用方法，以及该化合物用于治疗与人类11-β-羟基类固醇脱氢酶1型酶相关的病症和用于制备作用于人的药物的方法 11-β-羟基类固醇脱氢酶1型酶。