Patent application number | Description | Published |
20090018103 | Diaminoalkane Aspartic Protease 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. | 01-15-2009 |
20090186884 | Diaminopropanol 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. | 07-23-2009 |
20090264428 | Renin Inhibitors - Described are compounds of the formula (I) 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 aspartic protease activity. Also described are methods of use of the compounds described herein in ameliorating or treating aspartic protease related disorders in a subject in need thereof. | 10-22-2009 |
20090264432 | Piperidine and Morpholine 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. | 10-22-2009 |
20090275581 | RENIN INHIBITORS - Disclosed are compounds according to Formula I: | 11-05-2009 |
20090312369 | Renin Inhibitors - 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. | 12-17-2009 |
20090318501 | Piperidine derivatives as renin inhibitors - 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. | 12-24-2009 |
20100041637 | 1,3-Oxazepan-2-one and 1,3-diazepan-2-one inhibitors of 11 -hydroxysteroid dehydrogenase 1 - This invention relates to novel compounds of the Formula (I), (I*), (I**), I, Ia, Ib, Ic, Id, Ie, If, Ig, Il | 02-18-2010 |
20100048636 | Aspartic Protease 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. | 02-25-2010 |
20100130471 | Renin Inhibitors - Described are compounds which bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also described are methods of use of the compounds described herein in ameliorating or treating aspartic protease related disorders in a subject in need thereof. | 05-27-2010 |
20100144825 | Renin Inhibitors - 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. | 06-10-2010 |
20100160424 | RENIN INHIBITORS - Described are compounds that bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also described are methods of use of the compounds described herein in ameliorating or treating aspartic protease related disorders in a subject in need thereof. | 06-24-2010 |
20100168243 | Renin Inhibitors - 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. | 07-01-2010 |
20100179109 | RENIN INHIBITORS - Disclosed are compounds of Formula (I) wherein the R, R | 07-15-2010 |
20100184805 | RENIN INHIBITORS - Disclosed are aspartic protease inhibitors represented by the following structural formula: and pharmaceutically acceptable salts thereof. These compounds are orally active and bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with aspartic protease activity. The present invention is also directed to pharmaceutical compositions comprising a compound described herein or enantiomers, diastereomers, or salts thereof and a pharmaceutically acceptable carrier or excipient. | 07-22-2010 |
20100190829 | RENIN INHIBITORS - Described are compounds that bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also described are methods of use of the compounds described herein in ameliorating or treating aspartic protease related disorders in a subject in need thereof. | 07-29-2010 |
20100197675 | CYCLIC UREA AND CARBAMATE INHIBITORS OF 11 BETA-HYDROXYSTEROID DEHYDROGENASE 1 - 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 β-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. | 08-05-2010 |
20100280005 | Renin Inhibitors - Disclosed are compounds of Formula I, wherein the R, R | 11-04-2010 |
20100317697 | Renin Inhibitors - Disclosed are compounds having the formula (I): wherein the R | 12-16-2010 |
20100324045 | CYCLIC UREA INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE 1 - This invention relates to novel compounds of the Formula (I), (Ia), (Ib), (Ic), (Id), (Ie), (If), (Ig), (Ih)1 (Ij), (Ik), (Il | 12-23-2010 |
20110015157 | CYCLIC INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE 1 - This invention relates to novel compounds of the Formula (I), (Ia), (Ib), (Ic), (Id), (Ie), (If), (Ig), (Ih); (Ii); (Ij), (Ik), (II) 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 β-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. | 01-20-2011 |
20110021512 | Cyclic Inhibitors Of 11Beta-Hydroxysteroid Dehydrogenase 1 - This invention relates to novel compounds of the Formula Ik, Im | 01-27-2011 |
20110034455 | INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 - 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 11β-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. | 02-10-2011 |
20110053943 | CARBAMATE AND UREA INHIBITORS OF 11 -HYDROXYSTEROID DEHYDROGENASE 1 - This invention relates to novel compounds of the invention pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-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. | 03-03-2011 |
20110071126 | INHIBITORS OF BETA-SECRETASE - The present invention is directed to a compound represented by the following structural formula | 03-24-2011 |
20110071139 | Cycloalkyl Lactame Derivatives As Inhibitors Of 11-Beta-Hydroxysteroid Dehydrogenase 1 - This invention relates to novel compounds of the Formula (I), any of the formulas I | 03-24-2011 |
20110098320 | Lactam Inhibitors Of 11-Beta-Hydroxysteroid Dehydrogenase 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 11β-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. | 04-28-2011 |
20110105504 | Inhibitors Of 11beta-Hydroxysteroid Dehydrogenase Type 1 - This invention relates to novel compounds of the Formula (I) 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 11β-HSD1 in mammals. | 05-05-2011 |
20110105506 | Diaminoalkane aspartic protease 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. | 05-05-2011 |
20110112062 | Carbamate And Urea Inhibitors Of 11Beta-Hydroxysteroid Dehydrogenase 1 - This invention relates to novel compounds of the Formula I, II, III, IHa, NIb, IV, IVa, IVb, IVc, IVd, IVe, V, Va, Vb1 V1, V1a, VIb, VII, Vi1a, VIIb, VIII, V111a, VIIIb, IX, IXa, X, and Xa, 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 β-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. | 05-12-2011 |
20110112082 | CYCLIC CARBAZATE AND SEMICARBAZIDE INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE 1 - This invention relates to novel compounds of the Formula (I), (Ia), (Ib), (Ic), (Id), (Ie),(If), (Ig), (Ih), (Ii), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-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. | 05-12-2011 |
20110124635 | Cyclic Inhibitors Of 11Beta-Hydroxysteroid Dehydrogenase 1 - This invention relates to novel compounds of the Formula (I), (II), 1u | 05-26-2011 |
20110136766 | AURORA KINASE INHIBITORS - Disclosed herein are Aurora kinase Inhibitors represented by Structural Formula (I): Values for the variables in Structural Formula (I) are defined herein. | 06-09-2011 |
20110136821 | Inhibitors Of 11Beta-Hydroxysteroid Dehydrogenase Type 1 - 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 β-HSD 1 in mammals. Formula (I). | 06-09-2011 |
20110263582 | CYCLIC UREA INHIBITORS OF 11 B-HYDROXYSTEROID DEHYDROGENASE 1 - This invention relates to novel compounds of the Formula (I), (Ia) and (Ib), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, j which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-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. | 10-27-2011 |
20110263583 | Cyclic Inhibitors Of 11Beta-Hydroxysteroid Dehydrogenase 1 - This invention relates to novel compounds of the Formula Il Ik, Im | 10-27-2011 |
20110263584 | Cyclic Inhibitors Of 11Beta-Hydroxysteroid Dehydrogenase 1 - This invention relates to novel compounds of the Formula I, Ik, Iq | 10-27-2011 |
20120040973 | DERIVATIVES OF [1,3]OXAZIN-2-ONE USEFUL FOR THE TREATMENT OF METABOLIC DISEASES SUCH AS LIPID DISORDERS - This invention relates to novel compounds of an 11 β-HSD1 inhibitor disclosed herein, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11/3-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. | 02-16-2012 |
20120178746 | CYCLIC INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE 1 - This invention relates to novel compounds of the Formula Ik, Im | 07-12-2012 |
20120208804 | CYCLIC INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE 1 BASED ON THE 1,3 -OXAZINAN- 2 -ONE STRUCTURE - This invention relates to substituted 1,3-oxazin-2-one compounds of the Formula (I), (II), (IIA), (IIB), (IIC), (II D), (IIE), (III), (III A), (III B), (IV), (IV A), (IV B), (IV C), (IV D), (V), (V A), (V B), (VI), (VI A), (VI B), (VII), (VII A), (VII B), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-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. | 08-16-2012 |
20120225906 | PIPERIDINE RENIN INHIBITORS - The present invention is directed to aspartic protease inhibitors represented by the following structural formula: | 09-06-2012 |
20120232050 | Cyclic Inhibitors of 11 beta-Hydroxysteroid Dehydrogenase 1 - This invention relates to novel compounds of the Formula (I), (II), (II-A), (II-B), (II-C), (II-D), (III). (III-A). (IIII-B). (III-C). (III-D), (III-E) (IV), (IV-A), (IV-B). (IV-C), (IV-D). (V), (V-A), (V-B), (V-C), (V-D), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-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. | 09-13-2012 |
20130244993 | SUBSTITUTED 5-,6- AND 7-MEMBERED HETEROCYCLES, MEDICAMENTS CONTAINING SUCH COMPOUNDS, AND THEIR USE - The present invention relates to compounds defined by formula I: wherein the variables A | 09-19-2013 |
20130244994 | CARBAMATE AND UREA INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE 1 - This invention relates to novel compounds of the Formula (I) | 09-19-2013 |
20130245051 | CYCLIC UREA INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE 1 - This invention relates to novel compounds of the Formula (I), (Ia) and (Ib), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, j which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 β-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. | 09-19-2013 |
20130289050 | INHIBITORS OF BETA-SECRETASE - The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the β-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of β-amyloid aggregates. | 10-31-2013 |
20140057927 | INHIBITORS OF BETA-SECRETASE - The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the β-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of β-amyloid aggregates. | 02-27-2014 |
20140200223 | INHIBITORS OF BETA-SECRETASE - The present invention is directed to a compound represented by the following structural formula | 07-17-2014 |
20150031691 | INHIBITORS OF BETA-SECRETASE - The present invention relates to compounds represented by Structural Formula (I): | 01-29-2015 |
20150051214 | LIVER X RECEPTOR MODULATORS - Provided herein are novel compounds and pharmaceutically acceptable salts thereof that are liver X receptor modulators. Also provided are compositions comprising compounds of the invention and a carrier. Additionally, use of the compounds herein and methods for treating a disease or disorder associated with the liver X receptor are further described. | 02-19-2015 |
20150065515 | LIVER X RECEPTOR MODULATORS - Provided herein are novel compounds and pharmaceutically acceptable salts thereof that are liver X receptor modulators. Also provided are compositions comprising compounds of the invention and a carrier. Additionally, use of the compounds herein and methods for treating a disease or disorder associated with the liver X receptor are further described. | 03-05-2015 |
20150080363 | SUBSTITUTED 5-,6- AND 7-MEMBERED HETEROCYCLES, MEDICAMENTS CONTAINING SUCH COMPOUNDS, AND THEIR USE - The present invention relates to compounds defined by formula I: wherein the variables A | 03-19-2015 |