Richardson; Peter C., Ginsburg; Paul H. - US Patent Attorneys and Agents

Attorney: Richardson; Peter C., Ginsburg; Paul H.

Number of patents: 62
Last date: September 10, 2002

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Number	Title	Issue Date
6448265	Pyrazoles and pyrazolopyrimidines having CRF antagonistic activity The pyrazoles and pyrazolopyrimidines of the formula ##STR1## wherein R1, R2, R3, R4 and A are as defined herein, have corticotropin releasing factor (CRF) antagonist activity. As such, they are effective in the...	09/10/2002
6441018	Pyrazoles and pyrazolopyrimidines having CRF antagonistic activity The pyrazoles and pyrazolopyrimidines of the formula ##STR1## wherein R1, R2, R3, R4 and A are as defined herein, have corticotropin releasing factor (CRF) antagonist activity. As such, they are effective in the...	08/27/2002
6417194	Quinolines and quinazolines useful in therapy Compounds of formula I, ##STR1## wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 and R3 independently represent H or C1-6 alkoxy (which is optionally substit...	07/09/2002
6388127	Process for preparing cyclic thioamides The present invention relates to a process for preparing a compound of the formula ##STR1## wherein b, Y and R3 are defined as above, useful for preparing novel aralkyl and aralkylidene heterocyclic lactams and imides which are selective a...	05/14/2002
6387904	Method of treating glaucoma and ischemic retinopathy A method for treating glaucoma and ischemic retinopathy in a mammal, comprising administering to said mammal a therapeutically effective amount of a compound of the formula ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein n, X...	05/14/2002
6372736	Heterocyclic compounds as inhibitors of rotamase enzymes Compounds of the formula (I): ##STR1## wherein A, Y, R, X, R1, R2, R3 and R4 are as defined above are inhibitors of rotamase enzymes in particular FKBP-12 and FKBP-52. The compounds therefore moderate neuronal r...	04/16/2002
6100240	Macrolide derivatives The invention relates to compounds of the formula I ##STR1## and to pharmaceutically acceptable salts thereof, wherein R1, R2, R3, Q, X, Y and Z are as defined herein. The invention also relates to pharmaceutical comp...	08/08/2000
6083943	Substituted azaheterocyclecarboxylic acid A compound of the chemical formula (I) and its pharmaceutically acceptable salt: ##STR1## wherein Y is C2 -C4 alkylene; Z is a valence bond or C1 -C6 alkylene; R1 is substituted or unsubstituted ...	07/04/2000
6060479	Quinazoline-4-one AMPA antagonists The present invention relates to novel quinazolin-4-one derivatives of the formula I, as defined in the specification, pharmaceutical compositions containing such compounds the use of such compounds to treat neurodegenerative, psychotropic, and drug and a...	05/09/2000
6048864	Quinolines and quinazolines useful in therapy Compounds of formula I, ##STR1## wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 and R3 independently represent H or C1-6 alkoxy (which is optionally su...	04/11/2000
6034082	5-azabicyclo(3.1.0)hexylalkyl-2-piperiodones and --glutarimides as neurokinin receptor antagonists Compounds of formula (I) ##STR1## and salts thereof, wherein: R1 is C1 -C6 alkyl, C3 -C7 cycloalkyl, C3 -C7 cycloalkyl(C1 -C4)alky aryl or aryl(C1...	03/07/2000
5972962	Treatment of pruritus The use of certain known 1,3,4 trisubstituted 4-aryl-piperidines for the treatment of pruritus in humans and animals is disclosed....	10/26/1999
5939550	Process for preparing derivatives of azabicyclo naphthyridine carboxylic acid comprising a dipeptide A multi-step process for preparing a dipeptide derivative of 7-(6-amino-3-azabicyclo3.1.0.!hex-3-yl)-6-fluoro-1-(2,4-difluorophenyl)-1 ,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid, in the form of a pharmaceutically acceptable acid addition salt i...	08/17/1999
5859011	Dihydropyridine derivatives as bradykinin antagonist Compound of formula (1) and their pharmaceutically acceptable salts wherein A1,A2,R1, R2,R3,R4,X are as defined in the specification have excellent bradykinin antagonistic activity. ##STR1##...	01/12/1999
5852016	Quinoxaline derivatives useful in therapy Compounds of formula (I), wherein A represents N or CH; R1 and R2 independently represent C1-4 alkyl, halo or CF3 ; R3 represents C1-4 alkyl (optionally substituted), C3-7 cycloalkyl,...	12/22/1998
5837717	Hydroxamic acid anesthetic compounds A compound of the following formula: ##STR1## and its pharmaceutically acceptable salt thereof, wherein R1 and R2 are independently hydrogen, C1-4 alkyl, C3-7 cycloalkyl, C2-4 alkenyl, C1-4	11/17/1998
5837720	N-2-(pyrrolidinyl-1)-1-phenethyl) acetamides as kappa receptor antagonists A compound of formula (I): ##STR1## and its pharmaceutically acceptable salt, wherein R is hydrogen or hydroxy; Ar is unsubstituted or substituted phenyl; X is unsubstituted or substituted phenyl or heterocyclic, mono-, di- or trihalomethyl, cyano, o...	11/17/1998
5834478	Morphinan hydroxamic acid compounds This invention provides a compound of the following formula: ##STR1## and the pharmaceutically acceptable salts thereof, wherein R is hydrogen, C1 -C5 alkyl or an O-protecting group; B is a dircet bond, C1 -C5	11/10/1998
5783572	Quinoxalinedione NMDA receptor antagonists Compounds of formula (I): ##STR1## and their pharmaceutically acceptable salts, wherein R1 and R2 are each independently Cl, Br, CH3, CH2 CH3 or CF3 ; R3 is H, CH3	07/21/1998
5604241	Substituted benzylaminoquinuclidines as substance P antagonists Compounds useful in the treatment of inflammatory disorders, central nervous system disorders and other disorders of the formula I ##STR1## and the pharmaceutically-acceptable salts thereof, wherein Ar1 and Ar2 are each independ...	02/18/1997
5466880	Process for preparing ketone enantiomer A novel multi-step process for preparing the (4S)-enantiomer of 4-(3,4 -dichlorophenyl)-3,4-1(2H)- naphthalenone in a highly-optically pure form is disclosed. The process involved starts from the known 4-(3,4-dichlorophenyl)-4-ketobutanoic acid and procee...	11/14/1995
5463126	Process for preparing sertraline The invention provides the substantially geometrically pure cis-stereoisomeric form of a compound of formula (I) and the substantially geometrically and optically pure cis-stereoisomeric form of a compound of formula (II): ##STR1## wherein R	10/31/1995
5442116	Process for preparing sertraline intermediates The invention provides the substantially geometrically and optically pure trans-stereoisomeric form of a compound of formula (I): ##STR1## wherein R1 is H or C1 -C4 alkyl, together with processes for its preparation. ...	08/15/1995
5373003	1-azabicyclo[3.2.2]nonan-3-amine derivatives The present invention relates to novel 1-azabicyclo[3.2.2]nonan-3-amine derivatives of the formula ##STR1## wherein R1, R2, R3, R4, R5 are each independently selected from hydrogen, fluorine, chl...	12/13/1994
5362902	N-(1-(2-carboxyethyl35cloalkylcarbonyl)-beta-alanine derivatives for pharmaceutical use Compounds of formula (I) are diuretic agents for treating various cardiovascular diseases including hypertension, heart failure and renal insufficiency....	11/08/1994
5362743	Aminoquinoline derivatives Certain novel 3-acyl-4-amino-8-alkoxyquinoline compounds have been prepared, including their pharmaceutically-acceptable salts. These compounds are useful for inhibiting gastric acid secretion in mammals and therefore, are of value in therapy as anti-ulce...	11/08/1994
5304557	Substituted oxoophthalazinyl acetic acids and analogs thereof A compound of the formula ##STR1## wherein A1 and A2 are independently N or CH; B is a covalent bond or C.dbd. O; R1 is hydrogen or C1 -C6 alkyl; R2 is hydrogen, fluorine, chlorine, bromine, tri...	04/19/1994
5300516	Muscarinic receptor antagonists Musacarinic receptor antagonists, particularly useful in the treatment of irritable bowel syndrome, of formula (I), or a pharmaceutically acceptable salt thereof, where m is 1 or 2; R1 and R2 are each independently H or C1...	04/05/1994
5298629	Intermediates in the synthesis of quinoline antibiotics This invention relates to compounds of the formulae ##STR1## wherein R and X are defined as below. These compounds are useful as intermediates in the syntheses of azabicyclo quinoline carboxylic acids having antibacterial activity....	03/29/1994
5294744	Formylation process for aromatic aldehydes A novel two-step reaction process for preparing 5-substituted-2-methoxybenzaldehyde compounds is disclosed wherein the substituent group is either isopropyl or trifluoromethoxy. The process involves (1) reacting a corresponding 4-substituted phenol compou...	03/15/1994
5294619	Arylpiperidine derivatives A series of novel N-alkyl or oxyalkyl arylpiperidine derivatives have been prepared, including their pharmaceutically acceptable acid addition salts, wherein the N-alkyl or oxyalkyl side chain is further substituted by certain aryl or heterocyclic ring gr...	03/15/1994
5281601	Muscarinic receptor antagonists A series of novel 3-phenyl-3-[1-(cyclicalkyl)pyrrolidin-3-yl]glutarimide derivatives have been prepared, including their pharmaceutically acceptable salts. The cyclic moiety present in these compounds is derived from either benzene or a heteroaryl such as...	01/25/1994
5280122	Resolution of 2-benzyl-4-piperidone-succinic acid This invention relates to a process for resolving racemic or optically enriched 2-benzyl-4-piperidone-succinic acid, comprising reacting such compound with (+)-cis-N-benzyl-2-(hydroxymethyl)-cyclohexylamine, (-)-cis-N-benzyl-2-(hydroxymethyl)-cyclohexylam...	01/18/1994
5196607	Process for preparing ketone enantiomer A novel multi-step process for preparing the (4S)-enantiomer of 4-(3,4-dichlorophenyl)-3,4-dihydro-1(2H)-naphthalenone in a highly-optically pure form is disclosed. The process involves (1) first reacting 3,4-dichlorocinnamyl chloride with L-(-)-ephedrine...	03/23/1993
5192800	Glutaramide diuretic agents A series of novel spiro-substituted glutaramide derivatives have been prepared, including the pharmaceutically acceptable salts thereof and bioprecursors therefor, wherein the spiro-substituent completes a 5- or 6- membered carbocyclic ring and is located...	03/09/1993
5158964	Benzoxazole sulfonamide anti-arrhythmic agents A series of novel N-alkyl N-(alkanesulphonamidoheterocyclicmethyl)-4-alkanesulphonamidophenethylamin es have been prepared, including their pharmaceutically acceptable salts and various key novel intermediates therefor. The heterocyclic moiety present...	10/27/1992
5153206	Arylpiperidine derivatives A series of novel N-alkyl or oxyalkyl arylpiperidine derivatives have been prepared, including their pharmaceutically acceptable acid addition salts, wherein the N-alkyl or oxyalkyl side chain is further substituted by certain aryl or heterocyclic ring gr...	10/06/1992
5130334	Indane sulfonamide anti-arrhythmic agents Novel 5-alkanesulphonamido-2-[N-(alkanesulphonamidoheterocyclicmethyl)-N-methyla mino]indane compounds have been prepared, including their pharmaceutically acceptable salts and various key novel intermediates therefor. The heterocyclic moiety present ...	07/14/1992
5114952	Isoquinolinylsulfonamides as anti-arrhythmic agents A series of novel alkanesulphonamidophenyl-N-alkyl-N-(heterocyclic-alkyl)alkylamine derivatives have been prepared, including their pharmaceutically acceptable salts. These compounds are useful in therapy as anti-arrhythmic agents and therefore, are ...	05/19/1992
5082970	Process for recycling amine isomer A novel process for converting trans-isomeric N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthaleneamine to cis-isomeric N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthaleneamine is disclosed. The process involves contacting tr...	01/21/1992

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Attorney: Richardson; Peter C., Ginsburg; Paul H.