Vitae Pharmaceuticals, Inc.

Boehringer Ingelheim International Gmbh

Robert Simpson

David A Claremon

Suresh B Singh

Colin M Tice

Wei Zhao

Zhenrong Xu

Salvacion Cacatian

John J Baldwin

Lawrence Wayne Dillard

Jing Yuan

Gerard McGeehan

Alexey V Ishchenko

Patrick Flaherty

Lanqi Jia

Yuanjie Ye

Linghang Zhuang

Wei He

Jean-Pierre Wery

Nathan K Yee

Xudong Wei

Rogelio Perez Frutos

Nizar Haddad

Fabrice Gallou

Thomas Nicola

Juergen Schnaubelt

Joerg Brandenburg

Dirk Kemmer

Dieter Gutheil

Jutta Kroeber

Yibo Xu

Michael Schul

Robert Hagenkoetter

Kai Oliver Donsbach

Eric Winter

Hans-Dieter Ecker

This invention relates to novel compounds of the Formula (I*), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11&#x3b2;-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell. 

Inhibitors of 11&#x3b2;-hydroxysteroid dehydrogenase type 1

This invention relates to novel compounds of the Formula (I), (I*), (Ia), (Ib), (Ic), (Id), (Ie), (If), (If*), (Ig), (Ih), (Ij), (Ik), (ll1-3 ), (Im1-3), (In1-3), (lo1-2), (Ip1-9), (Iq1-9), (Ir1-9) and (Is1-3) pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11&#x3b2;-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell. (I) 

Lactam inhibitors of 11-&#x3b2;-hydroxysteroid dehydrogenase 1

This invention relates to novel compounds of the Formula (I), any of the formulas I-I1a-1jor pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11&#x3b2;-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell. 

Cycloalkyl lactame derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1

The present invention is directed to aspartic protease inhibitors represented by the following structural formula: or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the aspartic protease inhibitors of Structural Formula (I). Methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using these aspartic protease inhibitors are also disclosed.

Piperidine renin inhibitors

The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors. 

Piperidinyl carbamate intermediates for the synthesis of aspartic protease inhibitors

Diaminoalkanes of below Formula I have now been found which are orally active and bind to aspartic proteases to inhibit their activity: They are useful in the treatment or amelioration of diseases associated with elevated levels of aspartic protease activity. The invention also relates to a method for the use of the compounds of Formula I in ameliorating or treating aspartic protease related disorders in a subject in need thereof comprising administering to said subject an effective amount of a compound of Formula I.

Diaminoalkane aspartic protease inhibitors

This invention relates to novel compounds of the Formulae I or II and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 &#x3b2;-HSD 1 in mammals. Formula (I). 

Mucic acid salts of a compound represented by the following structural formula: are disclosed. In particular, single crystalline mucic acid salts of the compound represented by structural formula (I) are characterized by a variety of properties and physical measurements. Methods of producing the mucic acid salts, using the salts to antagonize one or more aspartic proteases, and methods of treating a number of aspartic protease mediated disorders using the salts are described herein.

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The present invention is directed to aspartic protease inhibitors represented by the following structural formula (I), or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the aspartic protease inhibitors of Structural Formula (I). Methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using these aspartic protease inhibitors are also disclosed. 

The present invention is directed to aspartic protease inhibitors. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.

Renin inhibitors

Described are diaminopropanols of which are orally active and bind to renin to inhibit its activity. They are useful in the treatment or amelioration of diseases associated with elevated. levels of renin activity or in the treatment of aspartic protease mediated disorders. Also described is a method for the use of the diaminopropanols in ameliorating or treating renin related disorders in a subject in need thereof. 

Diaminopropanol renin inhibitors

Described are compounds which are orally active and bind to renin to inhibit its activity. They are useful in the treatment or amelioration of diseases associated with renin activity. Also described are methods of use of these compounds for treating or ameliorating a renin mediated disorder in a subject.

Piperidine and morpholine renin inhibitors

Diaminoalkanes of Formula I have now been found which are orally active and bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with elevated levels of aspartic protease activity. The invention also relates to a method for the use of the compounds of Formula I in ameliorating or treating aspartic protease related disorders in a subject in need thereof comprising administering to said subject an effective amount of a compound of Formula I. 

Disclosed is a process for preparing a macrocyclic compound of the formula (I): which is carried out using an intermediate of the formula (II): wherein W, Rthrough R, D, A and Rare as defined herein. The compounds of formula (I) are potent active agents for the treatment of hepatitis C virus (HCV) infection.

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Wilmington, DE, United States of America

Robert Simpson