Abstract: The present invention is a process for the preparation of a compound of the formula: where R3, R4 and n are defined in the specification which comprises hydrogenating a compound of the formula: the E-geometrical isomer thereof or a mixture of the Z- and E-isomers in the presence of catalyst containing Rh, a chiral ligand with at least one phosphorous atom where the hydrogenation is conducted in the presence of a base.

Abstract: The sustained release tablet of (R)-5,6-dihydro-5-(methylamino)-4H-imidazo[4,5-ij]-quinolin-2(1H)-one (Z)-2-butenedioate (1:1) which is disclosed permits twice daily administration of (R)-5,6-dihydro-5-(methylamino)-4H-imidazo[4,5-ij]-quinolin-2(1H)-one (Z)-2-butenedioate (1:1) to treat humans with Parkinson's disease.

Abstract: Disclosed is a non-sustained release pharmaceutical tablet composition which comprises a rapidly precipitating drug in an amount from about 5 to about 60% and at least one member selected from the group consisting of a binder in an amount of from about 2 to about 25% and a superdisintegrant in an amount from about 6 to about 40% where the rapidly precipitating drug, “binder” and superdisintegrant are mixed and compressed into a tablet without heating, solvent or grinding.

Abstract: The invention is an oxazolidine ester of silylated baccatin III of formula (VII) which is a useful intermediate to produce pharmaceutically useful anti-cancer compounds.

Abstract: Novel aromatic bicyclic amines of formula (I) ##STR1## are useful in treating central nervous system disorders and cardiac arrhythmias and cardiac fibrillation.

Abstract: The present invention includes a number of novel intermediates such as the (S)-secondary alcohol of formula (VIIIA)X.sub.2 --CH.sub.2 --C*H(OH)--CH.sub.2 --NH--CO--R.sub.N (VIIIA)and processes for production of pharmacologically useful oxazolidinones.

Abstract: Compounds and their pharmaceutically acceptable salts suitable for treating central nervous system disorders associated with the dopamine D3 receptor activity of structural Formula I: ##STR1##

Abstract: Disclosed is a novel process and novel intermediates to prepare [R-(R*,R*)]-N-[3-[1-[5,6-dihydro-4-hydroxy-2-oxo-6-(2-phenylethyl)-6-propy l-2H-pyran-3-yl]propyl]phenyl]-5-(trifluoromethyl)-2-pyridinesulfonamide (XIX) ##STR1## which is a protease inhibitor useful in treating humans infected with the HIV virus.

Abstract: The invention is novel intermediates useful in producing taxol.

Abstract: The present invention is a method of treating a person who has psoriasis or arthritis or reducing the toxicity of cancer chemotherapy which comprises administering to the patient an anti-psoriasis effective amount of an oxazolidinone, preferably (S)-N-[[3-[3-fluoro-4-(4-morpholinyl)phenyl]-2-oxo-5-oxazolidinyl]methyl]a cetamide.

Abstract: The present invention discloses new processes in the preparation of midazolam (VII), ##STR1## a commercially important pharmaceutical, as well a new intermediates in those processes from a known benzophenone (I) starting material.

Abstract: Compounds and their pharmaceutically acceptable salts suitable for treating central nervous system disorders associated with the dopamine D3 receptor activity of Formula I: wherein R.sub.1 and R.sub.2 are independently H, C.sub.1-8 alkyl or C.sub.1-8 alkylAryl; X is CH.sub.2 R.sub.3 or NHSO.sub.2 R.sub.4 ; Y is hydrogen, CH.sub.2 R.sub.3, NHSO.sub.2 R.sub.4, CONR.sub.1 R.sub.2, SO.sub.2 NR.sub.1 R.sub.2, SO.sub.2 CH.sub.3, halogen, OSO.sub.2 CF.sub.3, SCH.sub.3 or OCH.sub.3 ; R.sub.3 is NHSO.sub.2 R.sub.4, SO.sub.2 R.sub.4, CONR.sub.1 R.sub.2 or Aryl; and R.sub.4 is NR.sub.1 R.sub.2, C.sub.1 -C.sub.8 alkyl, Aryl or C.sub.1 -C.sub.8 alkylAryl.

Abstract: The imidazo?1,5-a!quinolines (I) are useful in treating neurological diseases/conditions or chronic neurodegenerative diseases/conditions.

Abstract: Pyrimido?4,5-b!indoles (IV) ##STR1## and pyrimido?4,5-b!indole salts (V) useful in treating asthma are disclosed as well as process for their preparation.

Abstract: The present invention discloses novel substituted aryl- and heteroarylphenyloxazolidinones which are useful as anti-bacterial agents. More specifically, the substituted aryl- and heteroarylphenyloxazolidinones of the invention are characterized by oxazolidinones having an aryl or heteroaryl group at the p-position of the 3-phenyl ring and additional substitutions at the m-position(s) of the 3-phenyl ring. A compound representative of this new class of oxazolidinones is (.+-.)-5-(acetamidomethyl)-3-?4-(3-pyridyl)-3,5-difluorophenyl!-2-oxazolid inone.

Abstract: Disclosed is a novel intermediate, 3,4-dihydro-6-methyl-4-phenyl-2H-benzopyran-2-ol (IV) ##STR1## and an improved process for the preparation of tolterodine.

Abstract: The present invention discloses new processes in the preparation of midazolam (VII), ##STR1## a commercially important pharmaceutical, as well a new intermediates in those processes from a known benzophenone (I) starting material.

Abstract: The present invention is an improved process to prepare roquinimex (IV) which comprises:(1) contacting N-methyl-N-phenyl-.alpha.-carbomethoxyamide (V) with from about one to about two equivalents of base and(2) contacting the mixture of step (1) with N-methylisatoic anhydride (I).

Abstract: The present invention are marefortines and paraherquamides where the 7-member oxygenated ring has been modified to produce 25-methylene compounds (VII) and 24,25-epoxy compounds (VIII) all of which are useful as antiparasitic agents against endo and ecto parasites, particularly helminths and arthropods.

Abstract: Novel aromatic bicyclic amines of formula (I) ##STR1## are useful in treating central nervous system disorders and cardiac arrhythmias and cardiac fibrillation.