Bristol-myers Squibb Compnay

Bristol Meyers Squibb Company

Lawrence R Marcin

John E Macor

Mendi A Higgins

Joanne J Bronson

Andrew Charles Good

Yong-Jin Wu

Michael Frederick Parker

Jianliang Shi

Lorin A Thompson, Iii

Carl P Bergstrom

Yonghua Gai

Robert A Mate

Richard Eric Olson

Ronald J Mattson

Pratik Devasthale

Kenneth M Boy

Guohua Zhao

Dalton King

Manoranjan Panda

Kumaravel Selvakumar

Jonathan L Ditta

Suresh Dhanusu

Derek John Denhart

Fang Moore

Susan Nicole Pieniazek

Katharine E McElhone

Stephen T Wrobleski

John E Starrett, Jr

Min Ding

Bang-Chi Chen

Kevin W Gillman

Ramkumar Rajamani

John D Catt

Yunhui Zhang

F Christopher Zusi

Jason M Guernon

Zhaoxing Meng

Nenghui Wang

James R Epperson

Dmitry S Zuev

Huiping Zhang

Tg Murali Dhar

Jeffrey A Deskus

Katharin E McElhone

TG Murali Dhar

Lorin A Iii Thompson

The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds are antagonists to &#x3b1;v-containing integrins. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with dysregulation of &#x3b1;-containing integrins, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.

Cyclobutanes- and azetidine-containing mono and spirocyclic compounds as &#x3b1;V integrin inhibitors

The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds are antagonists to &#x3b1;v-containing integrins. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with dysregulation of av-containing integrins, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions. 

Cyclobutane- and azetidine-containing mono and spirocyclic compounds as &#x3b1;V integrin inhibitors

Disclosed are compounds of Formula (I) or a salt thereof, wherein: X is CRor N; W is: (i) &#x2014;(CRR)&#x2014; or (ii) &#x2014;(CRR)x-Y&#x2014;(CRR)y-; and Y, R, R, R, R, R, R, x, and y are define herein. Also disclosed are methods of using such compounds as modulators of TNF&#x3b1;, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases. 

Heterocyclic compounds useful as inhibitors of TNF

The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds modulate the mGluR2 receptor and may be useful for the treatment of various disorders of the central nervous system. 

Triazolopyridine ether derivatives and their use in neurological and pyschiatric disorders

Compounds of formula (I), including pharmaceutically acceptable salts thereof, are set forth herein: 

Compounds for the reduction of beta-amyloid production

There is provided a series of novel &#x3b1;-(N-sulfonamido)acetamide compounds of the Formula (I) wherein R, R, Rand Rare defined herein, which are inhibitors of &#x3b2;-amyloid peptide (&#x3b2;-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by anti-amyloid activity.

&#x3b1;-(N-sulfonamido)acetamide derivatives as &#x3b2;-amyloid inhibitors

The present invention provides a novel alpha-(N-sulfonamido)acetamide compound, its pharmaceutical composition, processes thereof and a method for the treatment of Alzheimer's disease and other conditions associated with &#x3b2;-amyloid peptide.

Alpha-(N-sulfonamido)acetamide compound as an inhibitor of beta amyloid peptide production

The present disclosure provides a series of compounds of the formula (I) which reduce &#x3b2;-amyloid peptide (&#x3b2;-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by &#x3b2;-amyloid peptide (&#x3b2;-AP) production.

Bicyclic compounds for the reduction of beta-amyloid production

There is provided a series of tetrahydroisoquinoline diaminopropane compounds of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R, Rand Rare as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by &#x3b2;-secretase and, more specifically, inhibit the production of A&#x3b2;-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to &#x3b2;-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.

Substituted tetrahydroisoquinolines as &#x3b2;-secretase inhibitors

There is provided a series of macrocyclic diaminopropanes of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R, R, R, m, n, W, X, Y, Z and L as defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by &#x3b2;-secretase and, more specifically, inhibit the production of A&#x3b2;-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to &#x3b2;-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.

Diaminopropane derived macrocycles as inhibitors of &#x3b2; amyloid production

There is provided a series of novel macrocyclic diaminopropanes of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R, R, R, R, n, L, Z, and as defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by &#x3b2;-secretase and, more specifically, inhibit the production of A&#x3b2;-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to &#x3b2;-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.

Macrocyclic diaminopropanes as beta-secretase inhibitors

The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salts or solvates thereof and pharmaceutically acceptable formulations comprising said compounds useful for the treatment of premature ejaculation, depression, attention deficit hyperactivity disorder, obsessive-compulsive disorder, post-traumatic stress disorder and substance abuse disorders.

Compounds for the treatment of premature ejaculation

A series of N-cycloalkylcarboxamide derivatives of N-benzyl benzenesulfonamides of Formula I are described.  The compounds inhibit &#x3b2;-amyloid peptide (&#x3b2;-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions characterized by aberrant extracellular deposition of &#x3b2;-amyloid. Pharmaceutical compositions and methods of treatment using these compounds are also disclosed.

Antiamyloid phenylsulfonamides: N-cycloalkylcarboxamides derivatives

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Bethany, CT, United States of America

Lawrence R Marcin