Pharmacopeia Drug Discovery, Inc.

Berlex Laboratories, Inc.

Other

Pharmacopeia Inc.

Columbia University

Cold Spring Harbor Laboratory

Berlax Laboratories, Inc.

Michael H J Ohlmeyer

John J Baldwin

Roland Ellwood Dolle

Shawn David Erickson

Vidyadhar Madhav Paradkar

Gonghua Pan

Gary Bruce Phillips

Michael M Morrissey

David D Davey

Zuchun Zhao

James J Devlin

Damian O Arnaiz

Bin Ye

John V Parkinson

Kirk McMillan

Lawrence Wayne Dillard

Michael H Wigler

W Clark Still

John C Reader

Koc-Kan Ho

Dirk Leysen

Jaap Van Der Louw

Jeffrey John Letourneau

Steven G Kultgen

Christopher Mark Riviello

James Inglese

Adolph C Bohnstedt

Jorge Quintero

Paolo Giovanni Martino Conti

Angela Wong

Roland E Dolle, Iii

Yaing Rong

Vidyahar Paradkar

Nitrogen heterocycle biaryls having a carboxylate terminus are useful for treating endometriosis, osteoporosis, restenosis following angioplasty, rheumatoid arthritis, cancer, macular degeneration and obesity. Compounds of formula: are disclosed. A representative example is 

Nitrogen heterocycle biaryls for osteoporosis and other diseases

Compounds containing the pyrimidine nucleus and their use to treat diseases and conditions related to inappropriate Interleukin-8 receptor activity are disclosed. The compounds are of the formula IIn these compounds, Q is preferably unsubstituted and substituted heterocyclyl; U is usually hydrogen or fluorine; and V is preferably hydrogen, halogen, alkyl, &#x2014;O&#x2014;alkyl or &#x2014;S-alkyl. A representative example is:

Pyrimidine derivatives as IL-8 receptor antagonists

Encoded combinatorial chemistry is provided, where sequential synthetic schemes are recorded using organic molecules, which define choice of reactant, and stage, as the same or different bit of information. Various products can be produced in the multi-stage synthesis, such as oligomers and synthetic non-repetitive organic molecules. Conveniently, nested families of compounds can be employed as identifiers, where number and/or position of a substituent define the choice. Alternatively, detectable functionalities may be employed, such as radioisotopes, fluorescers, halogens, and the like, where presence and ratios of two different groups can be used to define stage or choice. Particularly, pluralities of identifiers may be used to provide a binary or higher code, so as to define a plurality of choices with only a few detachable tags. The particles may be screened for a characteristic of interest, particularly binding affinity, where the products may be detachable from the particle or retained on the particle. The reaction history of the particles which are positive for the characteristic can be determined by the release of the tags and analysis to define the reaction history of the particle.

Complex combinatorial chemical libraries encoded with tags

Bradykinin B-receptor antagonists of formulaare disclosed. The compounds are useful for treating diseases associated with inappropriate bradykinin receptor activity, such as diabetic vasculopathy, inflammation, pain, hyperalgesia, asthma, rhinitis, septic shock, atherosclerosis and multiple sclerosis. Pyrimidines, triazines, and anilines in which Q is imidazolyl or pyrrolyl are particularly preferred.

Bradykinin B1 receptor antagonists

N-Heterocyclic derivatives of the formula (I):are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.

N-heterocyclic derivatives as NOS inhibitors

N-heterocyclic derivatives as nos inhibitors

Encoded combinatorial chemistry is provided, where sequential synthetic schemes are recorded using organic molecules, which define choice of reactant, and stage, as the same or different bit of information. Various products can be produced in the multi-stage synthesis, such as oligomers and synthetic non-repetitive organic molecules. Conveniently, nested families of compounds can be employed as identifiers, where number and/or position of a substituent define the choice. Alternatively, detectable functionalities may be employed, such as radioisotopes, fluorescers, halogens, and the like, where presence and ratios of two different groups can be used to define stage or choice. Particularly, pluralities of identifiers may be used to provide a binary or higher code, so as to define a plurality of choices with only a few detachable tags. The particles may be screened for a characteristic of interest, particularly binding affinity, where the products may be detached from the particle or retained on the particle. The reaction history of the particles which are positive for the characteristic can be determined by the release of the tags and analysis to define the reaction history of the particle.

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Plainsboro, NJ, United States of America

Michael H J Ohlmeyer