Howard Isaac Tjiong - Holland MI, US Roy Thomas Winters - Pinckney MI, US
Assignee:
Warner-Lamber Company - Morris Plains NJ
International Classification:
C07D471/04 C07D239/47
US Classification:
544279, 544317
Abstract:
A process for preparing a 2-(pyridin-4-ylamino)-pyrido[2,3-d]pyrimidine of Formula II comprising reacting a 4-aminopyridine of the formula with an alkali metal amide or hydride and a 2-alkylsulfanyl-pyrido[2,3-d]pyrimidine of Formula I wherein R, R, R′ and R″, and aryl are as defined in the specification.
Quinazolines And Their Use For Inhibiting Cyclin-Dependent Kinase Enzymes
Mark Robert Barvian - Ann Arbor MI, US Ellen Myra Dobrusin - Ann Arbor MI, US James Stanley Kaltenbronn - Ann Arbor MI, US Peter L. Toogood - Ann Arbor MI, US Roy Thomas Winters - Pinckney MI, US Inderjit S. Sidhu - Edmonton, CA Rajeshwar Singh - Edmonton, CA Yadagiri Bathini - Alberta, CA Ronald George Micetich - Sherwood Park, CA
This invention provides quinazolines that are useful for treating cell proliferative diseases and disorders, such as cardiovascular diseases, infections, cancers, autoimmune diseases, gout, kidney disease, and neurodegenerative diseases and disorders such as Alzheimer's disease. We have now discovered a group of 2-arylamino-7-(alkyl)oxy-8-alkylquinazolines and 8-alkyl-2-arylamino-quinazoline 2,7-diamines that are potent inhibitors of cyclin-dependent kinases (cdks). The compounds are readily synthesized and can be administered by a variety of routes, including orally, and have sufficient bioavailability. This invention also provides pharmaceutical formulations comprising at least one of the quinazoline compounds together with a pharmaceutically acceptable carrier, diluent, or excipient therefor. The invention further provide useful intermediates generated during the production of the quinazoline compounds.
Stephen Alan Fakhoury - Saline MI, US Helen Tsenwhei Lee - Ann Arbor MI, US Jessica Elizabeth Reed - Ann Arbor MI, US Kevin Matthew Schlosser - Ann Arbor MI, US Karen Elaine Sexton - Chelsea MI, US Haile Tecle - Ann Arbor MI, US Roy Thomas Winters - Pinckney MI, US
Assignee:
Warner-Lambert Company LLC - Morris Plains NJ
International Classification:
A61K 31/517 C07D 239/94 C07D 413/12
US Classification:
51426621, 5142662, 544119, 544284, 544293, 540600
Abstract:
This invention provides quinazoline compounds of the formula:.
Stephen Alan Fakhoury - Saline MI, US Helen Tsenwhei Lee - Ann Arbor MI, US Jessica Elizabeth Reed - Ann Arbor MI, US Kevin Matthew Schlosser - Ann Arbor MI, US Karen Elaine Sexton - Chelsea MI, US Haile Tecle - Ann Arbor MI, US Roy Thomas Winters - Pinckney MI, US
Assignee:
Warner-Lambert Company LLC - Morris Plains NJ
International Classification:
A61K 31/517 A01N 43/90 C07D 239/72
US Classification:
51426621, 544284, 544293
Abstract:
This invention provides quinazoline compounds of the formula:.
Helen Tsenwhei Lee - Ann Arbor MI, US Jessica Elizabeth Reed - Ann Arbor MI, US Kevin Matthew Schlosser - North Wales PA, US Karen Elaine Sexton - Kent, GB Haile Tecle - Ann Arbor MI, US Roy Thomas Winters - Pinckney MI, US
Assignee:
Warner-Lambert Company LLC - Morris Plains NJ
International Classification:
A01N 43/54 A61K 31/519 C07D 239/72 C07D 401/00
US Classification:
5142662, 5142661, 544283, 544284
Abstract:
This invention provides quinazoline compounds of the formula:.
Hubert Barth - Emmendingen, DE Alexander Bridges - Saline MI, US Ronald Heemstra - Pinckney MI, US Nicole Horne - Muskegon MI, US Robert Hughes - Grand Haven MI, US Thomas Jacks - Holland MI, US Dennis McNamara - Ann Arbor MI, US Simon Schneider - Merzhausen, DE Klaus Steiner - Emmendingen, DE Peter Toogood - Ann Arbor MI, US Roy Winters - Pinckney MI, US
International Classification:
C 07D 4 3/02
US Classification:
544/284000, 544/293000, 544/244000
Abstract:
Methods and materials for preparing irreversible inhibitors of tyrosine kinases of general Formula 1 are disclosed. Such inhibitors, which include N-[4-(3-chloro-4-floro-phenylamino)-7-(3-morpholin-4-yl-propoxy)-quinazolin-6-yl]-acrylamide, are useful for treating cancer, restenosis, atherosclerosis, endometriosis and psoriasis. The disclosed methods employ protecting schemes to minimize undesirable diacryloylamino-quinazoline side products.
Pyrazole Derivatives As Anti-Platelet And Anti-Thrombotic Agents
Liguo Chi - Ann Arbor MI, US Chulho Choi - Mystic CT, US Andrew G. Geyer - Chicago IL, US Robert M. Kennedy - Ann Arbor MI, US Jeffery A. Pfefferkorn - Mystic CT, US Roy T. Winters - Pinckney MI, US
This invention relates to novel compounds of formula (I)or stereoisomers or pharmaceutically acceptable salts thereof wherein Y, Rthrough R, and Xthrough Xare as defined in the specification, pharmaceutical compositions containing said compounds useful as P2Yantagonists, and to methods of treating thromboembolic disorders.
Process For Preparing 4,6-Disubstituted Pyrido[3,4-D]Pyrimidines
H. D. H. Showalter - Ann Arbor MI Roy T. Winters - Ann Arbor MI Gordon W. Rewcastle - Manurewa, NZ William A. Denny - Pakuranga, NZ
Assignee:
Warner-Lambert Company - Morris Plains MI
International Classification:
C07D47104
US Classification:
544277
Abstract:
An improved process for the preparation of 4,6-disubstituted pyrido[3,4-d]pyrimidines is described where 5-amino-2-fluoropyridine is converted in seven operations to the desired products, as well as other valuable intermediates used in the process.
T Dorrell, Cynthia Hedrick, Dorothy Loyd, Dave Dale, Kenneth Idol, Rick Matthias, Leanda Windmeyer, Jean Ball, Barry Boos, Larry Hamman, Charles Waggoner