Merck & Company, Inc.

Pharmacopeia Drug Discovery, Inc.

Schering Corporation

Pharmacopeia Inc.

Vitae Pharmaceuticals, Inc.

Other

Berlex Laboratories, Inc.

Bristol-myers Squibb Compnay

Merck Sharp & Dohme Corporation

Iview Therapeutics, Inc.

Nutek Pharma Ltd.

Daiichi Pharmaceutical Co., Ltd.

Pharmaceopeia, Inc.

Berlax Laboratories, Inc.

Pharmacopeia Drug Disclovery, Inc.

John J Baldwin

Gerald S Ponticello

David A Claremon

David C Remy

Harold G Selnick

Ge Li

Frederick C Novello

David E McClure

Lawrence Wayne Dillard

Shawn David Erickson

Michael H J Ohlmeyer

Roland Ellwood Dolle

Arthur G Taveras

Vidyadhar Madhav Paradkar

Gary Bruce Phillips

Michael M Morrissey

David D Davey

James J Devlin

Damian O Arnaiz

Zuchun Zhao

Bin Ye

John V Parkinson

Jing Yuan

Zhenrong Xu

Nigel J Liverton

Suresh B Singh

Colin M Tice

Wei Zhao

Younong Yu

Salvacion Cacatian

Joseph G Atkinson

Joel R Huff

Jianhua Chao

John C Reader

Robert Simpson

Purakkattle J Biju

Joseph P Vacca

Ronald J Doll

William C Lumma, Jr

Michael P Dwyer

Kenneth L Shepard

Edward McDonald

George D Hartman

Viyyoor Moopil Girijavallabhan

F George Njoroge

Alan K Mallams

Theresa M Williams

Wasyl Halczenko

Steven D Young

Marcia E Christy

Neng-Yang Shih

Richard L Tolman

Stuart B Rosenblum

Alan B Cooper

Adriano Afonso

Lanqi Jia

Dinanath F Rane

Junying Zheng

Jeffrey John Letourneau

Qingbei Zeng

Katerina Leftheris

Alaric J Dyckman

Robert G Aslanian

Walfred S Saari

Koc-Kan Ho

Stephen T Wrobleski

Kevin D McCormick

Wei Li

Michael H Ohlmeyer

Pauline C Ting

Atsushi Nakayama

Daniel M Solomon

Christopher Ronald Sarko

Robert A Horlick

Arthur F Wagner

Ashit K Ganguly

Mark G Bock

Joseph A Kozlowski

Daniel F Veber

Clarence S Rooney

Roger M Freidinger

Linghang Zhuang

Timothy J Guzi

Samuel L Graham

Ben C Askew

Tao Guo

Wensheng Yu

Bandarpalle B Shankar

Patrick A Pinto

Douglas Walsh Hobbs

Brian F McGuinness

Michael K C Wong

Seong Heon Kim

Dirk Leysen

Carmen S Alvarez

Kartik M Keertikar

Jaap Van Der Louw

Vinh D Tran

William A Bolhofer

Ray Anthony James

The present invention provides aqueous formulations containing an anti-infection agent, a biocompatible polysaccharide, an osmotic pressure regulator, a pH regulator, and water, wherein a gel containing the therapeutic agent is formed in situ upon instillation of the formulations onto the skin and a body cavity of a subject. The formulations of this invention are useful for treating infectious diseases of skin or a body cavity (e.g., eye, nose, or vagina) of a subject.

Pharmaceutical formulations that form gel in situ

The present invention provides novel slow-releasing ophthalmic compositions containing Povidone Iodine (PVP-I) and uses thereof in the treatment of acute infections of at least one eye tissue from bacterial, mycobacterial, viral, fungal, or amoebic causes and for preventing such infections in appropriate clinical settings. Each of the ophthalmic compositions contains povidone iodine, osmotic pressure regulator, suspending agent and EDTA-Na, wherein povidone iodine exists as microsphere particles formed by PVP-I and sodium alginate.

Slow-releasing ophthalmic compositions comprising povidone iodine

The present invention relates to methods and compositions for the synthesis, production, and use of pro-drug propofol analogs. This invention relates to a method for the production of a broad group of glycosylated propofol carbohydrate derivatives.

Synthesis and use of glycoside derivatives of propofol

The present invention relates to methods and compositions for the synthesis, production, and use of pro-drug analogs of the analgesic acetaminophen. This invention relates to a method for the production of a broad group of glycosides of acetaminophen derivatives.

Glycosylated acetaminophen pro-drug analogs

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

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

6-(Aminoalkyl)indazoles of formula (I) and the salts thereof have renin-inhibiting properties and can be used as antihypertensive, and renal, cardiac and vascular protecting medicinally active ingredients. 

6-(aminoalkyl)indazoles

There are disclosed compounds of the formula or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.

3,4-DI-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands

3,4-di-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands

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

The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: and the pharmaceutically acceptable salts, solvates and esters thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.

Pyrazinyl substituted piperazine-piperidines with CXCR3 antagonist activity

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

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Gwynedd Valley, PA, United States of America

John J Baldwin