Schering Corporation

Other

Schering-plough Corporation

David R Andrews

Anantha R Sudhakar

Robert W Watkins

Bernard R Neustadt

Paul E McNamara

Federico C Gaeta

Wenxue Wu

William W Leong

Dinesh Gala

Tiruvettipuram K Thiruvengadam

Xiaoyong Fu

Timothy L McAllister

Hongbiao Liao

Gary M Lee

Martin Lawrence Schwartz

Donal Maloney

Chou-Hang Tann

Jacques Gosteli

Suhan Tang

Ingrid Mergelsberg

David J Tsai

David J S Tsai

Sami Y Kalliney

Christopher Nielsen

Frank Guenter

In an illustrative embodiment, the present invention describes the synthesis of the following compound and similar compounds, in high stereochemical purity by a novel stereoselective alkylation process: 

Stereoselective alkylation of chiral 2-methyl-4-protected piperazines

In one embodiment, the present application discloses a process for making the compound of the formula: 

Synthesis of quinoline 5-carboxamides useful for the preparation of PDE IV inhibitors

The crystalline polymorph Form I of (&#x2212;)-4-[4-[4-[4-[[(2R-cis)-5-(2,4-difluorophenyl)tetrahydro-5-(1H-1,2,4-triazol-1-ylmethyl)furan-3-yl]methoxy]phenyl]-1-piperazinyl]phenyl-2,4-dihydro-2-[(S)-1-ethyl-2(S)-hydroxylpropyl]-3H-1,2,4-triazol-3-one represented by the formula Ipharmaceutical compositions containing such a polymorph and methods of using such a polymorph to treat fungal infections in mammals are disclosed.

Crystalline antifungal polymorph

In an illustrative embodiment, the present invention describes the synthesis of the following compound and similar compounds, in high stereochemical purity by a novel stereoselective alkylation process:

Disclosed are chiral hydrazine derivatives of the formula (Ia), (Ib), (Ic) and (Id) ##STR1## wherein: R.sup.1 and R.sup.2 are independently C.sub.1 -C.sub.10 alkyl;

Chiral hydrazine derivatives

Described is a process for preparing triazolone compounds of the formula ##STR1## comprising heating a mixture of a compound of the formula ##STR2## and a hydrazine derivative of the formula R.sup.5 --NH--NH--CHO, R.sup.5 --NH--NH--C(O)OC(CH.sub.3).sub.3 or R.sup.5 --NH--NH--C(O)OCH.sub.2 C.sub.6 H.sub.5, optionally in the presence of an added base.

Process for the preparation of triazolones

Steroid intermediates and processes for their preparation

Methods and pharmaceutical compositions are disclosed for reducing intraocular pressure. The methods and compositions employ an active ingredient which comprises certain benzothiadiazinyl and quinazolinyl substituted carboxyalkyl dipeptides wherein the benzothiadiazinyl or quinazolinyl portions are joined to the dipeptide portions by an aminocarbonyl group.

Carboxyalkyl dipeptides as antiglaucoma agents

Pharmaceutical compositions and a method for reducing intraocular pressure by topically applying a carboxyalkyl dipeptide are disclosed.

Antiglaucoma agents

Antihypertensive compounds with angiotensin-converting enzyme inhibitory activity and diuretic activity are disclosed. Such compounds are useful in the treatment of cardiovascular disorders, especially hypertension and congestive heart failure, and are useful in the treatment of glaucoma.

Antihypertensive compounds

Growing community of inventors

Maplewood, NJ, United States of America

David R Andrews