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Attorney: Stein; Bruce


Number of patents: 170
Last date: December 07, 2004

1          
NumberTitleIssue Date
6828120Process to prepare 11β, 17α,21-trihydroxy-6α-methylpregna-1,4-diene-3,20-dione 21-acetate
The present invention is a novel process for the transformation of 17α-hydroxy-6α-methylpregn-4-ene-3,20-dione 17-acetate (I) to 11β,17α,21-trihydroxy-6α-methylpregna-1,4-diene-3,20-dione 21-acetate (VI)
12/07/2004
6796975Container for linezolid intravenous solution
The present invention is a container for an IV aqueous solution of a Gram-positive oxazolidinone agent, such as linezolid a the compound of formula: which comprises having the container-solution contact surface material ...
09/28/2004
6509491Aminohydroxylation of olefins in the presence of acetamide
The present invention is a process to prepare on of a phenylisoserine ester of the formula (II) $c;--CH(NH--CO--CH3)--CH(OH)--CO--O--R1 with reduced amount of diol by-product by the use of a compound of the formula R2 --CO--...
01/21/2003
64689991,2,3,4,5,6,-hexahydroazepino [4,5-b]indoles containing arylsulfones at the 9-position
The present invention are substituted 9-arylsulfone-1,2,3,4,5,6-hexahydroazepino[4,5-b]indoles (X) and unsubstituted 9-arylsulfone-1,2,3,4,5,6-hexahydroazepino[4,5-b]indoles (XI) such as the compound of EXAMPLE 13 ##STR1## which are useful in treatin...
10/22/2002
6462234Process to prepare (2S)-2-(dipropylamino)-6-ethoxy-2, 3-dihydro-1H-indene-5-carboxamide
The present invention is a process, including intermediates, to produce (2S)-2-dipropylamino)-6-ethoxy-2,3-dihydro-1H-indene-5-carboxamide ##STR1## which is a useful pharmaceutical agent....
10/08/2002
6455564Method of treating sexual disturbances
The present invention is a method of treating sexual disturbances in humans and inducing mating in non-human mammals using the compounds of formula (A) ##STR1## in a dosage range where the sexually therapeutic amount is from about 0.2 thru 8 mg/perso...
09/24/2002
6452007Crystal forms of 1-[5-methanesulfonamidoindolyl-2-carbonyl]-4-[3-(1-methylethylamino)-2-pyr idinyl]piperazine
The present invention relates to two novel crystal forms of a known compound, 1-[5-Methanesulfonamidoindolyl-2-carbonyl]-4-[3-(1-methylethylamino)-2-pyr idinyl] piperazine monomethanesulfonate salt, which are useful for treating humans who are HIV pos...
09/17/2002
6444813Linezolid-crystal form II
The invention is a process to produce a compound, linezolid ##STR1## which is useful as an antibacterial agent....
09/03/2002
6410760Process to prepare androst-4-en-17-carboxylic acid
The process of the present invention transforms a steroidal ketone of formula (III) ##STR1## to androst-4-en-17ଲ-carboxylic acid (IV) ##STR2## by reaction with K2 SO5.KHSO.sub.4.K.sub.2 SO4....
06/25/2002
6355802Process to prepare (5R)-(methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]-quinolin-2(1h)-one
The present invention is an improved prosess to prepare (5R)-(methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one the compound of formula (VII)....
03/12/2002
6307064Process to prepare taxol
The present invention includes processes to prepare commercially important taxols (X) ##STR1## from substituted amino-3-phenyl (2R,3S) isoserinates (II). In addition processes to prepare the substituted amino-3-phenyl (2R,3S) isoserinates (II) as wel...
10/23/2001
6265604(R)-3-hydroxy-3-(2-phenylethyl)-hexanoic acid derivatives
The compound of the present invention (R)-3-hydroxy-3-(2-phenylethyl)-hexanoic acid ##STR1## is an intermediate in the preparation of the anti-AIDS compound, [R-(R*,R*)]-N-[3-[1-5,6-dihydro-4-hydroxy-2-oxo-6-(2-phenylethyl)-6-propyl -2H-pyran-3-yl]pro...
07/24/2001
6239283Process to prepare cyclic-sulfur fluorine containing oxazolidinones
The invention is a process for the preparation of cyclic-sulfur fluorine containing oxazolidinone antibacterial agents which utilizes the important tetrahydrothiopyran-o-fluorinated carbamate of formula (IV) ##STR1##...
05/29/2001
6211386Process for asymmetric hydrogenation
The present invention is a process for the preparation of a compound of the formula: ##STR1## where R3, R4 and n are defined in the specification which comprises hydrogenating a compound of the formula: ##STR2## the E-geometrical isomer th...
04/03/2001
6197339Sustained release tablet formulation to treat Parkinson's disease
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)-...
03/06/2001
6177101Delavirdine high strength tablet formulation
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 ...
01/23/2001
6177573Process to prepare taxol
The invention is an oxazolidine ester of silylated baccatin III of formula (VII) ##STR1## which is a useful intermediate to produce pharmaceutically useful anti-cancer compounds....
01/23/2001
6133446Heterocyclic compounds for the treatment of CNS and cardiovascular disorders
Novel aromatic bicyclic amines of formula (I) ##STR1## are useful in treating central nervous system disorders and cardiac arrhythmias and cardiac fibrillation....
10/17/2000
6107519Process to produce oxazolidinones
The present invention includes a number of novel intermediates such as the (S)-secondary alcohol of formula (VIIIA) X2 --CH2 --C*H(OH)--CH2 --NH--CO--RN (VIIIA) and processes for production of pharmacologically useful o...
08/22/2000
6077963Process to produce a protease inhibitor
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...
06/20/2000
6057452Process to prepare taxol
The invention is novel intermediates useful in producing taxol. These include the oxazolidine ester (III) ##STR1## the oxazolidine acid (IV) ##STR2## and the oxazolidine (XI) ##STR3##...
05/02/2000
6040306Method of treating psoriasis, arthritis and reducing the toxicity of cancer chemotherapy
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)-...
03/21/2000
5942614Process to produce midazolam
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....
08/24/1999
5935970Use of imidazo›1,5-a!quinolones as neuroprotective agents
The imidazo›1,5-a!quinolines (I) are useful in treating neurological diseases/conditions or chronic neurodegenerative diseases/conditions....
08/10/1999
5932728Pharmaceutically active tricyclic amines
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....
08/03/1999
5929248Substituted heteroarylphenyloxazolidinones
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 ox...
07/27/1999
5922892Process to produce midazolam
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....
07/13/1999
5922914Process to prepare tolterodine
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....
07/13/1999
5912349Process for the preparation of roquinimex
The present invention is an improved process to prepare roquinimex (IV) which comprises: (1) contacting N-methyl-N-phenyl-଱-carbomethoxyamide (V) with from about one to about two equivalents of base and (2) contacting the mixture of step (1) with N-methy...
06/15/1999
588618025-methylene and 24-25 -epoxy marcfortines and paraherquamides
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 ...
03/23/1999
5877317Heterocyclic compounds for the treatment of CNS and cardiovascular disorders
Novel aromatic bicyclic amines of formula (I) ##STR1## are useful in treating central nervous system disorders and cardiac arrhythmias and cardiac fibrillation....
03/02/1999
5866589Alkyl substituted piperadinyl and piperazinyl anti-AIDS compounds
Anti-AIDS compounds of formula (I) ##STR1## wherein R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification and R8 is alkyl of substituted alkyl....
02/02/1999
5858999Cosolvent parenteral formulation of tirilazad
The invention is a cosolvent parenteral pharmaceutical formulation of a lazaroid and its pharmaceutically acceptable salts....
01/12/1999
5837870Process to prepare oxazolidinones
The present invention includes processes for producing 5-hydroxymethyl substituted oxazolidinone alcohols (III) from carbamates (IIA) or a trifluoroacetamide (IIB) using a dihydroxy compound (I) or glycidol (IV) starting material and for the transformatio...
11/17/1998
5831089Process to produce midazolam
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....
11/03/1998
5801246Substituted heteroarylphenyloxazolidinones
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 ox...
09/01/1998
5795986Pyrimido›4,5-B!indoles
The pyrimido›4,5-b!indoles (I) ##STR1## and lactams (XIII) of the invention are useful as pharmaceutical agents for a number of different indications....
08/18/1998
5756732Substituted heteroarylphenyloxazolidinones
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 ox...
05/26/1998
5750695Antiparasitic paraherquamides
The present invention includes various substituted and paraherquamides, exemplified by the 14-hydroxy-2-deoxoparaherquamide B of formula (XXV) which are useful as antiparasitic agents....
05/12/1998
5707634Finely divided solid crystalline powders via precipitation into an anti-solvent
The present invention is a process for producing a finely divided solid which comprises (1) dissolving the solid to be finely divided in a liquid carrier solvent to form an injection solution and (2) adding the injection solution of step (1) to a volume of ant...
01/13/1998
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