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Attorney: North; Robert J., Winokur; Melvin


Number of patents: 82
Last date: June 27, 2000

1      
NumberTitleIssue Date
6080745Fused tricyclic heteroaromatic derivatives as dopamine receptor subtype ligands
A class of fused tricyclic heteroaromatic compounds of formula (I) as defined in claim 1 or a salt thereof or a prodrug thereof, containing a fused pyrazole, oxazole or pyrimidine ring are ligands for dopamine receptor subtypes within the body and are the...
06/27/2000
5717104Process for preparing indole derivatives containing a 1,2,4-triazol-1-yl substituent
A process for preparing tryptamine derivatives and related compounds having a 1,2,4-triazol-1-yl moiety within the molecule comprises reacting 4-amino-1,2,4-triazol with a nitrobenzene derivative containing a readily displaceable group; deaminating the am...
02/10/1998
5714498Benzimidazole derivatives
The invention is directed to substituted benzimidazole compounds which are ligands for dopamine receptor subtypes used in the treatment of the dopamine system....
02/03/1998
5712285Pyrrolo-pyridine derivatives
A class of pyrrolo›2,3 -b!pyridine derivatives, linked via the 3-position thereof by a methylene group to a tetrahydropyridinyl moiety, the latter moiety being substituted in turn by an aryl- or heteroaryl-substituted divalent monocyclic radical, are lig...
01/27/1998
5710161Triazole derivatives and their use as therapeutic agents
The present invention relates to compounds of the formula (I): ##STR1## wherein Ar1 represents optionally substituted phenyl; Ar2 represents aryl; benzhydryl; or benzyl; wherein each aryl and heteroaryl and each phenyl moiety of...
01/20/1998
5710015cDNA cloning of inositol monophosphatase
The present invention relates to the cloning of novel cDNA sequences encoding human and rat inositol monophosphatase (IMP); to the preparation of IMP enzyme by incorporation of the cDNAs into an expression vector and the expression thereof in recombinant ...
01/20/1998
5700941Octahydronaphthyridine derivatives
A class of substituted 1,2,3,4,5,6,7,8-octahydronaphthyridine derivatives are ligands for dopamine receptor subtypes within the body, in particular the D4 subtype, and are therefore useful in the treatment and/or prevention of disorders of the ...
12/23/1997
5700802Furopyridine derivatives
A class of substituted furo›2,3-b!pyridine derivatives are ligands for dopamine receptor subtypes within the body, in particular the D4 subtype, and are therefore useful in the treatment and/or prevention of disorders of the dopamine system, i...
12/23/1997
5700809Pyrrolo-pyridine derivatives
Compounds of formula I are ligands for dopamine receptor subtypes within the body and are therefore useful in the treatment and/or prevention of disorders of the dopamine system, in particular schizophrenia. ##STR1## wherein Q is ##STR2##...
12/23/1997
5698573Imidazolone and oxazolone derivatives as dopamine antagonists
A class of imidazolone and oxazolone derivatives of Structure I, ##STR1## wherein X represents oxygen or N--R1 ; Q represents a substituted five-, six- or seven-membered monocyclic heteroaliphatic ring which contains one nitrogen atom as the so...
12/16/1997
5693640Pyridazino-indole derivatives
A class of pyridazino›4,5-b!indole-1,4-dione derivatives, substituted in the 2-position by an optionally substituted phenyl moiety, are selective non-competitive antagonists of NMDA receptors and/or are antagonists of AMPA receptors, and are therefore of...
12/02/1997
5686480Fused tricyclic heteroaromatic derivatives as dopamine receptor subtype ligands
A class of fused tricyclic heteroaromatic compounds of formula (I), or a salt thereof or a prodrug thereof containing a fused pyrazole ring are ligands for dopamine receptor subtypes within the body and are therefore of use in the treatment and/or prevent...
11/11/1997
5686463Oxadiazoles useful in the treatment of senile dementia
A class of novel oxadiazoles, substituted on one of the ring carbon atoms with a non-aromatic azacyclic or azabicyclic ring, and substituted on the other ring carbon atom with a substituent of low lipophilicity; are potent muscarinic agonists, and have go...
11/11/1997
5684006Isoxazole and pyrazole derivatives as dopamine receptor subtype ligands
A class of substituted isoxazole and pyrazole derivatives of formula (I), or a salt thereof of or a prodrug thereof, wherein the broken circle represents two non-adjacent double bonds whereby the five-membered ring containing X and Y is aromatic; one of X...
11/04/1997
5681836Methanesulfonate salts of antipsychotic benzofuran derivatives
The methanesulfonate salt of a class of antipsychotic compounds comprising a benzo›b!furan moiety and a substituted heterocyclic moiety, linked via the 3-position of the benzo›b!furan moiety by a methylene group, which are antagonists of dopamine recept...
10/28/1997
5681833Benzodiazepine derivatives
Compounds of Formula (I), and salts and prodrugs thereof, wherein said formula, R1 represents certain optionally substituted alkyl or C3-7 cycloalkyl; R2 represents (II) or (III), where m is 0, 1, 2 or 3; R9 is ...
10/28/1997
5681959Chemical synthesis of azaindoles
The present invention relates to a process for the preparation of azaindole derivatives of the formula ##STR1## wherein Q is hydrogen, C1-6 alkyl, C2-6 alkenyl, C1-6 alkoxy, hydroxy, aryl or arylC1-4 alkyl;...
10/28/1997
5674889Aromatic compounds, compositions containing them and their use in therapy
The present invention relates to compounds of formula (I) and salts and prodrugs thereof, wherein Q1 represents a phenyl group substituted by one or more halo optionally substituted naphthyl, optionally substituted indolyl, optionally substitut...
10/07/1997
5668153Piperidine derivatives and their use as therapeutic agents
Compounds of formula (I) ##STR1## exemplified by formulae (Ia) and (Ib) ##STR2## are tachykinin receptor antagonists useful in the treatment of disorders associated with the presence of an excess of tachykinins such as pain, inflammation, m...
09/16/1997
5665732Indazole derivatives
A class of chemical compounds comprising a 1-H-indazole moiety and a substituted heterocyclic moiety, linked via the 3-position of the indazole moiety by a methylene group, are ligands for dopamine receptor subtypes within the body and are therefore usefu...
09/09/1997
5665722Benzofuran derivatives as D4 receptor antagonists
A class of chemical compounds comprising a benzo [b] furan moiety and a substituted heterocyclic moiety, linked via the 3-position of the benzo [b] furan moiety by a methylene group, are antagonists of dopamine receptor subtypes within the brain, being ex...
09/09/1997
5641787Indole derivatives as dopamine D4 antagonists
The present invention accordingly provides the use of a compound of formula I, or a pharmaceutically acceptable salt thereof or a prodrug thereof: ##STR1## wherein R1 represents hydrogen or C1-6 alkyl; Z represents --CH2 -...
06/24/1997
56332813,3-diphenyl prop-2-yl amino acid derivatives and their use as tachykinin antagonists
Compounds of formula (I), or a salt or prodrug thereof, wherein R1 represents H, C1-4 alkyl or CH2 COOH; R2 represents H or C1-4 alkyl, with the proviso that R1 and R2 are not both H;...
05/27/1997
5629336Use of glycine/NMDA receptor ligands for the treatment of drug dependence and withdrawal
Compounds capable of interacting with the strychnine-insensitive glycine modulatory site of the N-methyl-D-aspartate (NMDA) receptor are active in preventing or reducing dependence on dependence-inducing agents such as morphine, but lack the undesirable s...
05/13/1997
5629347Aromatic compounds, pharmaceutical compositions containing them and their use in therapy
Compounds of formula (I), and salts and prodrugs thereof, wherein Q is R9 CR10 R11 or CH2 R9 CR10 R11 where R9 is H or OH and R10 and R11 are optional...
05/13/1997
5624947Phenyl derivatives useful as tachykinin antagonists
Compounds of formula (I), or a salt or prodrug thereof are tachykinin antagonists....
04/29/1997
5622950Pyrrolo-pyridine derivatives
A class of pyrrolo[2,3-b]pyridine derivatives, substituted at the 3-position by a substituted piperazinylmethyl moiety, are antagonists of dopamine receptor subtypes within the brain, having a selective affinity for the dopamine D4 receptor sub...
04/22/1997
5620972Substituted benzene derivatives
Benzapines of the formula (I) ##STR1## and salts and prodrugs thereof useful as CCK antagonists....
04/15/1997
5618812Benzodiazepine derivatives
Compounds of Formula (I), and salts and prodrugs thereof, wherein R1 represents H, optionally substituted C1-6 alkyl or C3-7 cycloalkyl; R2 is NHR12 or (CH2)s R13 where 5 i...
04/08/1997
5614532Quinolone derivatives
A class of 2-(1H)-quinolone derivatives, substituted at the 3-position by an optionally substituted aryl substituent, are selective non-competitive antagonists of NMDA receptors and/or are antagonists of AMPA receptors, and are therefore of utility in the...
03/25/1997
5614518Morpholine derivatives as dopamine receptor subtype ligands
A class of substituted morpholine derivatives of formula ##STR1## wherein Y represents an optionally substituted bicyclic heteroaromatic ring system containing one or two nitrogen atoms, the ring system comprising a six-membered aromatic or heteroaro...
03/25/1997
5614524Piperazine derivatives as 5-HT1 Agonists
A class of substituted piperazine derivatives of formula I ##STR1## are selective agonists of 5-HT1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated conditions, for whi...
03/25/1997
5612362Imidazolinone derivatives as tachykinin receptor antagonists
Compounds of formula (I) and salts and prodrugs wherein Q1 is a specified aryl group, the dotted line is an optional double bond, Z is O or NR3, R1 and R3 are H or specified optionally substituted alkyl or other...
03/18/1997
5612336Heterocyclic amide derivatives as tachykinin antagonists
Compounds of formula (I), and salts and prodrugs thereof, wherein Q1 is phenyl substituted by one or more halo; optionally substituted naphthyl, indolyl, benzothiophenyl, benzofuranyl, benzyl or fluorenyl; the dotted line represents an optional...
03/18/1997
5610183Phenylglycine derivatives pharmaceutical compositions containing them and their use in therapy
Compounds of Formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein Q is optionally substituted phenyl or naphthyl; X and Y are each H, C1-6 alkyl, C2-6 alkenyl or X and Y are together .dbd.O; Z is O or S; R...
03/11/1997
5607957Imidazole, triazole and tetrazole derivatives
A class of substituted imidazole, triazole and tetrazole derivatives are selective agonists of 5-HT1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a ...
03/04/1997
5607946Quinolone derivatives as dopamine D4 ligands
A class of chemical compounds comprising a 2(1H)-quinolone moiety and a substituted heterocyclic moiety, linked via the 3-position of the 2(1H)-quinolone moiety by a methylene group, are antagonists of dopamine receptor subtypes within the brain, having a...
03/04/1997
5604240Pyrrolo-pyridine derivatives
A class of substituted pyrrolo[2,3-c]pyridine derivatives are selective agonists of 5-HT1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective a...
02/18/1997
5602162Imidazole, triazole and tetrazole derivatives
A class of substituted imidazole, triazole and tetrazole derivatives are selective agonists of 5-HT1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a ...
02/11/1997
5602125Thienodiazepine derivatives as cholecystokinin and gastrin antagonists
Thienodiazepine compounds of formula (1) wherein: R1 represents H, optionally substituted C1-6 alkyl or C3-7 cycloalkyl; R2 represents optionally substituted phenyl; or R2 represents a group (a) where...
02/11/1997
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