Warner-lambert Company

British Technology Group Limited

Other

Warner Lambert LLC

British Tech. Group

Howard D Showalter

William Alexander Denny

Anthony Denver Sercel

James Marino Hamby

Andrew Mark Thompson

Vladimir Genukh Beylin

Ian J Stratford

Gerald E Adams

Edward M Fielden

Matthew A Naylor

Gordon William Rewcastle

Brian Desmond Palmer

Ellen Myra Dobrusin

Annette M Doherty

Mel C Schroeder

Edward Faith Elslager

Leslie M Werbel

Moana Tercel

Clifton J Blankley

Roy Thomas Winters

Cleo Connolly

Robert Lee Panek

Alexander James Bridges

James Bernard Kramer

Diane H Boschelli

Om Prakash Goel

Annette Marian Doherty

James C French

David W Fry

Daniel Fred Ortwine

Mark Robert Barvian

Robert Frederick Meyer

Alan Kraker

David B Capps

Donald F Worth

Ellen M Berman

Sonya Shah Khatana

Vlad E Gregor

Zhipei Wu

Judith L Johnson

Colin R Edmunds

Peter McDonnell

Vladimir G Beylin

Anthony D Sercel

Naphthyridinones for inhibiting protein tyrosine kinase and cell cycle

Benzimidazoles of Formula I below are inhibitors of protein tyrosine kinases, and are useful in treating cellular proliferation. ##STR1## The compounds are especially useful in treating cancer, atherosclerosis, restenosis, and psoriasis.

Benzimidazoles for inhibiting protein tyrosine kinase mediated cellular

6-Aryl naphthyridines are inhibitors of protein tyrosine kinase, and are thus useful in treating cellular proliferation mediated thereby. The compounds are especially useful in treating atherosclerosis, restenosis, psoriasis, as well as bacterial infections.

6-aryl naphthyridines for inhibiting protein tyrosine kinase mediated

6-Aryl pyrido�2,3-d!pyrimidines and naphthyridines are inhibitors of protein tyrosine kinase, and are thus useful in treating cellular proliferation mediated thereby. The compounds are especially useful in treating atherosclerosis, restenosis, psoriasis, as well as bacterial infections.

6-Aryl pyrido�2,3-d! pyrimidines and naphthyridines for inhibiting

Novel 4-substituted amino benzothieno�3,2-d!pyrimidine and 4-substituted amino�2,3-d!pyrimidine inhibitors of epidermal growth factor receptor family of tyrosine kinases are described, as well as pharmaceutical compositions of the same, which are useful in treating proliferative diseases such as cancer, synovial pannus invasion in arthritis, psoriasis, vascular restenosis and angiogenesis and additionally useful in the treatment of pancreatitis and kidney disease as well as a contraceptive agent.

Tricyclic compounds capable of inhibiting tyrosine kinases of the

Chiral compounds useful as radiosensitizers or chemosensitizers having the formula ##STR1## wherein X is halogen or ##STR2## intermediates used to prepare these compounds, and a novel process to prepare these compounds are described.

Chiral [[(2-bromoethyl)-amino]methyl]-2-nitro-1H-imidazol-1-ethanol and

2-Thioindoles (2-selenoindoles) and analogous 2-indolinethione (2-indolineselenone) and polysulfide (selenide) compounds, salts thereof, methods of production, intermediates in their production, pharmaceutical compositions containing said compounds, and methods for inhibiting protein kinase dependent disease in a mammal or treating aberrant cell growth in a mammal, using said compositions, are disclosed.

2-thioindoles (selenoindoles) and related disulfides (selenides) which

Process for preparing chiral

A process for purifying pentostatin from a crude fermentation beer comprising the steps of 1) applying the fermentation beer to a strong cation exchange resin; 2) eluting with ammonium hydroxide; 3) concentrating the eluate; 4) applying the concentrated eluate to a strongly basic anion exchange resin charged with borate ion; 5) eluting with water; 6) applying this eluate to styrene-divinylbenzene beads prewashed with ethanol; 7) eluting the beads with water; and 8) recrysllyzing the pentostatin from water and methanol to yield a product that is greater than 99.7% pure.

Process for purifying pentostatin

This invention concerns novel dihydro- and tetrahydronaphthyridines useful for enhancing the lethal effects on tumor cells to treatment causing DNA-damaging activity as with ionizing radiation or with a chemotherapeutic agent.

Dihydro- and tetrahydronaphthyridines

Preparation of 4-bromo-4'-demethylepipodophyllotoxin by reacting podophyllotoxin with hydrogen bromide at about -20.degree. C. New antitumor compounds of the formula: ##STR1## wherein R is A--(CH.sub.2).sub.n [A(CH.sub.2).sub.n ].sub.m (CHAH).sub.p --Q or ##STR2## each A, independently, is O, S, SO or SO.sub.2 ; n is an integer from 1 to 6, except when n and p, taken together, are zero, then n is 2 to 6; n is 0, 1, or 2; p is 0, 1, or 2; Q is H, alkyl from 1 to 6 carbon atoms which may be substituted with an NR.sub.1 R.sub.2 group wherein each R.sub.1 and R.sub.2, independently, is selected from the group of H, alkyl containing 1 to 6 carbon atoms which may be substituted with OH, alkanoyl containing 1 to 6 carbon atoms, or R.sub.1 and R.sub.2 are interconnected and together with the N to which they are connected form an N heterocyclic ring of 5 to 6 carbon atoms; R.sub.3 is hydrogen, and R.sub.4 is an alkyl, alkenyl, cycloalkyl, 2-furyl, 2-thienyl, aryl, aralkyl, and aralkenyl, wherein the aromatic ring may optionally be substituted, preferentially by one or more of hydroxyl, alkyl, alkoxy, nitro, or halogen radicals. R.sub.3 and R.sub.4 together with the carbon atom to which they are attached may form a saturated cycloaliphatic ring having 5 or 6 carbon atoms; each X and Y, individually, is OH or NR.sub.6 R.sub.7 wherein R.sub.6 and R.sub.7, independently, is H, alkyl containing 1 to 6 carbon atoms or one of R.sub.6 and R.sub.7 is acyl; and Z is ##STR3## Novel process for the preparation of the novel compounds or analogs thereof having advantageous stereoselection using alkyltin thiolates, preferably with selected solvents.

4-bromo-4'-demethylepipodophyllotoxin derivatives

Improved processes for producing substituted benzo(chalcogeno)[4,3,2-cd] indazoles. The processes produce compounds in higher yields and of greater purity by using a novel sequence of acylation chemistry and easily removed protecting groups. The compounds produced have antibacterial, antifungal, antileukemic, and antitumor activity.

Processes for the preparation of benzo(chalcogeno)(4,3,2-cd)indazoles

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Ann Arbor, MI, United States of America

Howard D Showalter