Schering Corporation

Intervet Inc.

Intervet International B.v.

Jay Weinstein

Adriano Afonso

Margaret J Gentles

Stuart B Rosenblum

Joseph Michael Kelly

Ronald L Wolin

David J Cooper

Jay A Waitz

Mae Counelis

William J Greenlee

Viyyoor Moopil Girijavallabhan

Andrew William Stamford

Michael W Miller

Jack D Scott

Eric J Gilbert

Ashit K Ganguly

Ronald J Doll

Arthur G Taveras

Timothy J Guzi

Alan K Mallams

John W Clader

Stuart W McCombie

Alan B Cooper

Dinanath F Rane

Carmen S Alvarez

Harry R Davis

Jagdish A Desai

Jianping Chao

Tarik Lalwani

James J-s Wang

Cynthia J Aki

Johan A Ferreira

Deborra E Mullins

[object Object]

Compounds of Formula (I):  or pharmaceutically acceptable salts, solvates, or esters thereof, are useful in treating diseases or conditions mediated by CBreceptors, such as metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, addiction (e.g., smoking cessation), gastrointestinal disorders, and cardiovascular conditions.

Substituted piperazines as CB1 antagonists

Farnesyl protein transferase inhibitors

Novel phenyl-substituted 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 halo-N-substituted urea compound to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammals such as a human.

Phenyl-substituted tricyclic inhibitors of farnesyl-protein transferase

Compounds of Formula I: ##STR1## wherein: X.sup.1 is hydrogen, halogen, CF.sub.3, nitro, NH.sub.2 or lower alkyl; each X.sup.2 is independently selected from the group consisting of hydrogen, halogen, lower alkoxy and lower alkyl; n is 1 or 2; Y is selected from the group consisting of S(O).sub.p, O, and NR.sup.5, wherein p is 0, 1 or 2, and R.sup.5 is hydrogen, alkyl, aryl, cycloalkyl, loweralkoxycarbonyl, aminocarbonyl or acyl; R.sup.1 and R.sup.2, which may be the same or different, are selected from the group consisting of hydrogen and lower alkyl groups, or taken together can form an oxygen atom when Y is NR.sup.5 ; A . . . is C=, CH-- or N--; R is --CZ--Y.sup.1 --Y.sup.2 --R.sup.3, wherein: Z is O, =CH--CN, or =N--CN; one of Y.sup.1 and Y.sup.2 is a bond, --CO--, O, S, or --NR.sup.4 --, and the other is (CH.sub.2).sub.m, where m is 0 or an integer of 1 to 4, and R.sup.4 is H or alkyl, with the proviso that when Z is O and m is 0 then Y.sup.1 or Y.sup.2 is selected from --CO--, O, S, or --NR.sup.4 ; R.sup.3 is aryl, heteroaryl or heterocycloalkyl, with the proviso that R.sup.3 can also be lower alkyl when Z is =N--CN; and their pharmaceutically acceptable acid addition salts; have activity as Ras-FPT inhibitors. They can be used, e.g., in pharmaceutical compositions, for inhibiting the abnormal growth of cells and for inhibiting proliferative diseases. Processes for their preparation, and useful intermediates, are also disclosed.

Tricyclic compounds having activity as RAS-FPT inhibitors

Compounds useful as antihypertensive agents and useful as antiviral agents against DNA-containing viruses, such as herpes group viruses, are disclosed. The compounds are represented by Formula 1.0: ##STR1## and their pharmaceutically acceptable salts and solvates. Pharmaceutical compositions containing compounds represented by Formula 1.0 are disclosed. Methods of treating a viral infection using compounds represented by Formula 1.0 are disclosed. Also disclosed are methods of treating hypertension using compounds of Formula 1.0 wherein R is selected from the group consisting of H, halogen and --C(O)OR.sup.6 ; and R.sup.1 is selected from the group consisting of --OR.sup.14, --O(CH.sub.2).sub.a C(H).sub.3-i Z.sub.i and --O(CH.sub.2).sub.h N(R.sup.15).sub.2.

Antiviral compounds and antihypertensive compounds

Ester and alkoxy substituted benzopyrans

Alkyl and acyl substituted quinolines

Acyl and alkoxy substituted quinolines

A method of inhibiting the binding of PDGF using compounds of the formula I ##STR1## useful in the treatment of atherosclerosis, cancer, retinal detachment, pulmonary fibrosis, arthritis, psoriasis and glomerulonephritis, and restenosis following angioplasty or vascular surgery is disclosed. Also disclosed are pharmaceutical compositions and novel PDGF inhibitory compounds of the formula ##STR2## or a pharmaceutically acceptable addition salt thereof, useful in the treatment of atherosclerosis, cancer, retinal detachment, pulmonary fibrosis, arthritis, psoriasis and glomerulonephritis, and restenosis following angioplasty or vascular surgery.

Inhibitors of platelet-derived growth factor

Compounds useful as antiviral agents against DNA containing viruses, such as herpes group viruses, are disclosed. The compounds are selected from the group consisting of: ##STR1## and their pharmaceutically acceptable salts and solvates. Pharmaceutical compositions containing compounds represented by Formula 1.00 are disclosed. Also disclosed are methods of treating a viral infection using compounds represented by Formula 1.00 The compounds of Formula 1.00 are also useful as intermediates to compounds of: ##STR2## Compounds of Formula 1.0 are useful as antiviral agents against the same viruses that the compounds of Formula 1.00 are useful against.

Certain N-substituted 3-oximino-2,4-dioxoquinolin-2,4-(1H)diones useful

Compounds useful as antiviral agents against DNA containing viruses, such as herpes group viruses, are disclosed. The compounds are selected from the group consisting of: ##STR1## and their pharmaceutically acceptable salts and solvates. Pharmaceutical compositions containing compounds represented by Formula 1.0 are disclosed. Also disclosed are methods of treating a viral infection using compounds represented by Formula 1.0. A process for making compounds of Formula 1.0 from the appropriate 3-oximino-quinolin-2,4(1H)-dione (Formula 2.5) is also disclosed. The process comprises reductively hydrolyzing an appropriate 3-oximino-quinolin-2,4(1H)-dione (Formula 2.5) in a mixture with a hydrogenation catalyst and an acidic solvent mixture.

Antiviral quinolinone compounds

Compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein, R is H, halogen, (C.sub.1 -C.sub.6) alkyl, N(C.sub.1 -C.sub.6 alkyl/aryl).sub.2, OH, O--(C.sub.1 -C.sub.6) alkyl/aryl, CH.sub.2 OH, COOH, COO-alkyl/aryl, SO.sub.2 NH.sub.2, or SO.sub.2 NH (C.sub.1 -C.sub.6 alkyl/aryl);

Quinoline-diones

Compounds useful as antihypertensive agents, or antiviral agents against DNA containing viruses, such as herpes group viruses, are disclosed. The compounds are represented by Formula 1.0: ##STR1## and their pharmaceutically acceptable salts and solvates. Pharmaceutical compositions containing compounds represented by Formula 1.0 are disclosed. Also disclosed are methods of treating hypertension or a viral infection using compounds represented by Formulas 1.0. Also disclosed is a compound of Structure B ##STR2## useful as an intermediate in producing compounds of Formula 1.0. A process for preparing the compounds of Formula 1.0 is also disclosed. In the process a compound of Structure B ##STR3## is reacted with an alkoxide R.sub.1 O.sup.- M.sup.+ in a solvent comprising the corresponding alcohol R.sub.1 OH of the alkoxide. Optionally, an organic cosolvent may be used with the solvent.

Growing community of inventors

Upper Montclair, NJ, United States of America

Jay Weinstein