公开(公告)号：US20110118250A1

公开(公告)日：2011-05-19

申请号：US12909566

申请日：2010-10-21

Applicant: Brian K. Albrecht ,  Denise Lyn Andersen ,  Michael Bartberger ,  James Brown ,  Ryan Brown ,  Stuart C. Chaffee ,  Yuan Cheng ,  Michael Croghan ,  Russell Graceffa ,  Scott Harried ,  Stephen Hitchcock ,  Randall Hungate ,  Ted Judd ,  Matthew Kaller ,  Charles Kreiman ,  Daniel La ,  Patricia Lopez ,  Craig Masse ,  Holger Monenschein ,  Thomas Nguyen ,  Thomas Nixey ,  Vinod F. Patel ,  Lewis Pennington ,  Matthew Weiss ,  Qiufen Xue ,  Bryant Yang ,  Wenge Zhong

Inventor： Brian K. Albrecht ,  Denise Lyn Andersen ,  Michael Bartberger ,  James Brown ,  Ryan Brown ,  Stuart C. Chaffee ,  Yuan Cheng ,  Michael Croghan ,  Russell Graceffa ,  Scott Harried ,  Stephen Hitchcock ,  Randall Hungate ,  Ted Judd ,  Matthew Kaller ,  Charles Kreiman ,  Daniel La ,  Patricia Lopez ,  Craig Masse ,  Holger Monenschein ,  Thomas Nguyen ,  Thomas Nixey ,  Vinod F. Patel ,  Lewis Pennington ,  Matthew Weiss ,  Qiufen Xue ,  Bryant Yang ,  Wenge Zhong

IPC: A61K31/538 ,  C07D405/12 ,  A61K31/4433 ,  A61K31/444 ,  C07D405/14 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/497 ,  C07D413/12 ,  A61K31/5377 ,  A61K31/4178 ,  A61K31/4545 ,  A61K31/453 ,  C07D311/96 ,  A61K31/352 ,  C07D407/12 ,  A61K31/4709 ,  C07D401/12 ,  C07D409/12 ,  A61K31/422 ,  A61K31/4025 ,  C07D471/04 ,  A61K31/501 ,  A61P25/28 ,  A61P25/00 ,  A61P25/16

CPC classification number: C07D405/12 ,  C07D413/12

Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A, B, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.

Abstract translation: 本发明包括可用于调节β-分泌酶酶活性和用于治疗β-分泌酶介导的疾病（包括阿尔茨海默氏病（AD））和相关病症的新一类化合物。 在一个实施方案中，化合物具有通式I，其中A，B，R 3，R 4，R 5，i和j在本文中定义。 本发明还包括药物组合物，其包括一种或多种式I化合物，这些化合物的使用方法，包括治疗AD和相关疾病，通过给受试者施用式I化合物或包含它们的组合物。 本发明还包括式II和III的其它实施方案，可用于制备本发明化合物的中间体和方法。

公开(公告)号：US07872009B2

公开(公告)日：2011-01-18

申请号：US11600264

申请日：2006-11-14

Applicant: Brian K. Albrecht ,  Denise Lyn Andersen ,  Michael Bartberger ,  James Brown ,  Ryan Brown ,  Stuart C. Chaffee ,  Yuan Cheng ,  Michael Croghan ,  Russell Graceffa ,  Scott Harried ,  Stephen Hitchcock ,  Randall Hungate ,  Ted Judd ,  Matthew Kaller ,  Charles Kreiman ,  Daniel La ,  Patricia Lopez ,  Craig Masse ,  Holger Monenschein ,  Thomas Nguyen ,  Thomas Nixey ,  Vinod F. Patel ,  Lewis Pennington ,  Matthew Weiss ,  Qiufen Xue ,  Bryant Yang ,  Wenge Zhong

Inventor： Brian K. Albrecht ,  Denise Lyn Andersen ,  Michael Bartberger ,  James Brown ,  Ryan Brown ,  Stuart C. Chaffee ,  Yuan Cheng ,  Michael Croghan ,  Russell Graceffa ,  Scott Harried ,  Stephen Hitchcock ,  Randall Hungate ,  Ted Judd ,  Matthew Kaller ,  Charles Kreiman ,  Daniel La ,  Patricia Lopez ,  Craig Masse ,  Holger Monenschein ,  Thomas Nguyen ,  Thomas Nixey ,  Vinod F. Patel ,  Lewis Pennington ,  Matthew Weiss ,  Qiufen Xue ,  Bryant Yang ,  Wenge Zhong

IPC: A61K31/50

CPC classification number: C07D405/12 ,  C07D413/12

Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A, B, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.

Abstract translation: 本发明包括可用于调节β-分泌酶酶活性和用于治疗β-分泌酶介导的疾病（包括阿尔茨海默病（AD））和相关病症的新一类化合物。 在一个实施方案中，化合物具有通式I，其中A，B，R 3，R 4，R 5，i和j在本文中定义。 本发明还包括药物组合物，其包括一种或多种式I化合物，这些化合物的使用方法，包括治疗AD和相关疾病，通过给受试者施用式I化合物或包含它们的组合物。 本发明还包括式II和III的其它实施方案，可用于制备本发明化合物的中间体和方法。

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：US20060183755A1

公开(公告)日：2006-08-17

申请号：US10537758

申请日：2003-12-05

Applicant: Mark Fraley ,  Scott Hambaugh ,  Robert Rubino ,  Randall Hungate

Inventor： Mark Fraley ,  Scott Hambaugh ,  Robert Rubino ,  Randall Hungate

IPC: A61K31/519 ,  C07D487/04

CPC classification number: C07D487/04 ,  A61K45/06

Abstract: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, macular edema, retinal ischemia, inflammatory diseases, and the like in mammals.

Abstract translation: 本发明涉及抑制，调节和/或调节酪氨酸激酶信号转导的化合物，含有这些化合物的组合物及其用于治疗酪氨酸激酶依赖性疾病和病症如血管生成，癌症，肿瘤生长，动脉粥样硬化的方法 ，年龄相关性黄斑变性，糖尿病性视网膜病变，黄斑水肿，视网膜缺血，炎症性疾病等。

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：US20080045503A1

公开(公告)日：2008-02-21

申请号：US11819607

申请日：2007-06-28

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 St. 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 St. Jean ,  Nianhe Han ,  Qi Huang ,  Qingyian Liu ,  Michael Bartberger ,  George Moniz ,  Matthew Frizzle

IPC: C07D277/34 ,  A61K31/421 ,  A61K31/426 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/5377 ,  A61K31/55 ,  A61P25/00 ,  C07D277/62 ,  C12N9/99 ,  C07D417/00 ,  C07D413/00 ,  C07D401/00 ,  A61P3/00 ,  A61P37/00 ,  A61P9/00 ,  C07D211/06 ,  C07D221/20 ,  C07D263/36 ,  C07D263/52

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：US20070185144A1

公开(公告)日：2007-08-09

申请号：US11595187

申请日：2006-11-10

Applicant: Wenge Zhong ,  Stephen Hitchcock ,  Brian Albrecht ,  Michael Bartberger ,  James Brown ,  Ryan Brown ,  Stuart Chaffee ,  Yuan Cheng ,  Michael Croghan ,  Russell Graceffa ,  Scott Harried ,  Dean Hickman ,  Daniel Horne ,  Randall Hungate ,  Ted Judd ,  Matthew Kaller ,  Charles Kreiman ,  Daniel La ,  Patricia Lopez ,  Craig Masse ,  Holger Monenschein ,  Thomas Nguyen ,  Thomas Nixey ,  Vinod Patel ,  Lewis Pennington ,  Matthew Weiss ,  Qiufen Xue ,  Bryant Yang

Inventor： Wenge Zhong ,  Stephen Hitchcock ,  Brian Albrecht ,  Michael Bartberger ,  James Brown ,  Ryan Brown ,  Stuart Chaffee ,  Yuan Cheng ,  Michael Croghan ,  Russell Graceffa ,  Scott Harried ,  Dean Hickman ,  Daniel Horne ,  Randall Hungate ,  Ted Judd ,  Matthew Kaller ,  Charles Kreiman ,  Daniel La ,  Patricia Lopez ,  Craig Masse ,  Holger Monenschein ,  Thomas Nguyen ,  Thomas Nixey ,  Vinod Patel ,  Lewis Pennington ,  Matthew Weiss ,  Qiufen Xue ,  Bryant Yang

IPC: A61K31/4747 ,  A61K31/4743 ,  A61K31/4741 ,  A61K31/4025 ,  A61K31/353 ,  A61K31/277 ,  A61K31/165 ,  C07D491/02

CPC classification number: C07D405/12 ,  C07D311/68 ,  C07D413/12 ,  C07D491/052

Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A, B, W, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.

Abstract translation: 本发明包括可用于调节β-分泌酶酶活性和用于治疗β-分泌酶介导的疾病（包括阿尔茨海默病（AD））和相关病症的新一类化合物。 在一个实施方案中，化合物具有通式I，其中A，B，W，R 3，R 4，R 5，i和 j在本文中定义。 本发明还包括药物组合物，其包括一种或多种式I化合物，这些化合物的使用方法，包括治疗AD和相关疾病，通过给受试者施用式I化合物或包含它们的组合物。 本发明还包括式II和III的其它实施方案，可用于制备本发明化合物的中间体和方法。

公开(公告)号：US20070185103A1

公开(公告)日：2007-08-09

申请号：US11600264

申请日：2006-11-14

Applicant: Brian Albrecht ,  Denise Andersen ,  Michael Bartberger ,  James Brown ,  Ryan Brown ,  Stuart Chaffee ,  Yuan Cheng ,  Michael Croghan ,  Russell Graceffa ,  Scott Harried ,  Stephen Hitchcock ,  Randall Hungate ,  Ted Judd ,  Matthew Kaller ,  Charles Kreiman ,  Daniel La ,  Patricia Lopez ,  Craig Masse ,  Holger Monenschein ,  Thomas Nguyen ,  Thomas Nixey ,  Vinod Patel ,  Lewis Pennington ,  Matthew Weiss ,  Quifen Xue ,  Bryant Yang ,  Wenge Zhong

Inventor： Brian Albrecht ,  Denise Andersen ,  Michael Bartberger ,  James Brown ,  Ryan Brown ,  Stuart Chaffee ,  Yuan Cheng ,  Michael Croghan ,  Russell Graceffa ,  Scott Harried ,  Stephen Hitchcock ,  Randall Hungate ,  Ted Judd ,  Matthew Kaller ,  Charles Kreiman ,  Daniel La ,  Patricia Lopez ,  Craig Masse ,  Holger Monenschein ,  Thomas Nguyen ,  Thomas Nixey ,  Vinod Patel ,  Lewis Pennington ,  Matthew Weiss ,  Quifen Xue ,  Bryant Yang ,  Wenge Zhong

IPC: A61K31/538 ,  A61K31/503 ,  A61K31/4704 ,  A61K31/4745 ,  A61K31/4188 ,  A61K31/4162 ,  C07D487/02 ,  C07D471/02

CPC classification number: C07D405/12 ,  C07D413/12

Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A, B, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.

Abstract translation: 本发明包括可用于调节β-分泌酶酶活性和用于治疗β-分泌酶介导的疾病（包括阿尔茨海默病（AD））和相关病症的新一类化合物。 在一个实施方案中，化合物具有通式I，其中A，B，R 3，R 4，R 5，i和j分别为 本文定义。 本发明还包括药物组合物，其包括一种或多种式I化合物，这些化合物的使用方法，包括治疗AD和相关疾病，通过给受试者施用式I化合物或包含它们的组合物。 本发明还包括式II和III的其它实施方案，可用于制备本发明化合物的中间体和方法。

公开(公告)号：US20060199817A1

公开(公告)日：2006-09-07

申请号：US11367123

申请日：2006-03-02

Applicant: Andrew Tasker ,  Dawei Zhang ,  Guo-Qiang Cao ,  Partha Chakrabarti ,  James Falsey ,  Bradley Herberich ,  Randall Hungate ,  Liping Pettus ,  Anthony Reed ,  Robert Rzasa ,  Kelvin Sham ,  Maya Thaman ,  Shimin Xu

Inventor： Andrew Tasker ,  Dawei Zhang ,  Guo-Qiang Cao ,  Partha Chakrabarti ,  James Falsey ,  Bradley Herberich ,  Randall Hungate ,  Liping Pettus ,  Anthony Reed ,  Robert Rzasa ,  Kelvin Sham ,  Maya Thaman ,  Shimin Xu

IPC: A61K31/5377 ,  A61K31/503 ,  A61K31/53 ,  C07D487/02

CPC classification number: C07D409/04 ,  C07D237/30 ,  C07D237/32 ,  C07D237/34 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D487/08 ,  C07D491/10

Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A1, A2, B, R1, R2, R3 and R4 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of kinase mediated diseases including rheumatoid arthritis, psoriasis and other inflammation disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.

Abstract translation: 本发明包括一类新的可用于预防和治疗蛋白激酶介导的疾病，包括炎症和相关病症的化合物。 化合物具有通式I，其中A 1，A 2，B，R 1，R 2， R 3和R 4在本文中定义。 本发明还包括药物组合物，其包含一种或多种式I化合物，这些化合物和组合物用于治疗激酶介导的疾病包括类风湿性关节炎，牛皮癣和其它炎症疾病的用途，以及可用于制备 一级方程式

公开(公告)号：US20070281938A1

公开(公告)日：2007-12-06

申请号：US11596982

申请日：2005-05-24

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

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

IPC: C07D277/60 ,  A61K31/426 ,  A61K31/4436 ,  A61K31/4535 ,  A61K31/497 ,  A61K31/5377 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D417/02 ,  C07D413/02 ,  C07D401/02 ,  A61P17/02 ,  C07D211/68 ,  C07D277/02 ,  C07D277/08

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) wherein R1, R2, R3, R4, and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as to the use of the compounds in medicine 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）的化合物，其中R 1，R 2，R 3，R 4， SUP>和Z如本文所定义，并且还涉及包含该化合物的药物组合物，以及该化合物在医药中的用途以及用于制备作用于人类11-β-羟基类固醇脱氢酶1型的药物 酶。