Pharmacopeia Inc.

Columbia University

Cold Spring Harbor Laboratory

Schering Corporation

Other

Pharmacopeia Drug Discovery, Inc.

John C Reader

Lawrence Wayne Dillard

John J Baldwin

Ge Li

Michael H Wigler

W Clark Still

Michael H Ohlmeyer

Ronald J Doll

Alan K Mallams

Wenguang Zeng

F George Njoroge

Adriano Afonso

Randall R Rossman

Dinanath F Rane

Michael H J Ohlmeyer

Viyyoor Moopil Girijavallabhan

Arthur G Taveras

Alan B Cooper

Ian Henderson

Jonathan J Burbaum

George F Njoroge

Dinanth F Rane

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

Combinatorial dihydrobenzopyran library

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.

Tricyclic compounds useful for inhibition of G-protein function and for treatment of proliferative diseases

Combinatorial libraries are disclosed which are represented by Formula I: ##STR1## wherein: ##STR2## is a solid support; T'--L-- is an identifier residue; and --L'--II' is a ligand/linker residue. These libraries contain dihydrobenzopyrans of the formula ##STR3## which interact (i.e., as agonists or antagonists) with .alpha. adrenergic receptors, dopamine receptors, .sigma.-opiate receptors, and K.sup.+ channels and are inhibitors of carbonic anhydrase isozymes. They are useful in the treatment of ocular diseases such as glaucoma.

Supports and combinatorial chemical libraries thereof encoded by

Methods for recording the reaction history of a solid support

Novel tricyclic compounds and pharmaceutical compositions are disclosed which are inhibitors of the enzyme, farnesyl protein transferase. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering the novel tricyclic compound to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human.

Tricyclic piperidinyl compounds useful as inhibitors of farnesyl-protein

Novel carbonyl piperazinyl and piperidinyl compounds and pharmaceutical compositions are disclosed. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering the novel carbonyl piperazinyl or piperidinyl compound to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being.

Carbonyl piperazinyl and piperidinyl compounds

A solid phase synthesis reaction vessel includes a vessel with a first inlet, a second inlet, and an outlet. A first stopcock is disposed within the first inlet and a second stopcock is disposed within the outlet. Solid phase material is prevented from escaping the reaction vessel via the outlet while allowing fluid to flow through the outlet by a frit. In one embodiment, the reaction vessel includes an outer hollow shell surrounding the vessel to allow cooling or heating fluid to flow therein for controlling the temperature in the interior reaction volume. The solid phase synthesis reaction vessel provides for the independent opening and closing of each of the inlets and outlet to provide for various ways of draining the vessel, varying the conditions within the vessel, and/or adding additional materials into the vessel.

Solid phase synthesis reaction vessel and method of using the same

Combinatorial libraries are disclosed which are represented by Formula I:

Novel compounds of Formula ##STR1## are disclosed. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering a compound of the above formula to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being.

Tricyclic compounds useful for inhibition of G-protein function and for

Methods of determining the structure of a compound encoded by

Process for preparing intermediates for a combinatorial

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Princeton, NJ, United States of America

John C Reader