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Assignee: A. H. Robins Company, Inc.


Location: Richmond, VA
No. of patents: 86

1      
NumberTitleIssue Date
50632354-[(diaryl)hydromethyl]-1-piperidinealkanols and esters and carbamates thereof useful in the treatment of allergic disorders
Novel compounds of the formula: ##STR1## are disclosed wherein Ar and Ar1 are phenyl, sustituted phenyl or pyridinyl, "alk" is a C1 -C12 straight or branched hydrocarbon chain, and R is H, loweralkylcarbonyl, arylcarb...
11/05/1991
5061720Substituted-4-thiazolidinone derivatives
Disclosed are novel substituted 4-thiazolidinone derivatives having cyclooxygenase and 5-lipoxygenase inhibiting properties and which are topical antiinflammatory agents for inflammed conditions of the skin having the formula: ##STR1## wherein R...
10/29/1991
4960896Process for the preparation of 5-chloro and 5-bromo-2-hydroxynicotinic acids
A process for the preparation of 5-halo-2-hydroxynicotinic acids having the formula: ##STR1## wherein X is chlorine or bromine, Y and Z are selected from hydrogen, loweralkyl or loweralkyl, is described wherein a corresponding 2-hydroxynicotinic...
10/02/1990
49607764-aryl-N-(alkylaminoalkyl, heterocyclicamino and heterocyclicamino)alkyl)-1-piperazinecarboxamides
Novel 4-aryl-N-[2-(dialkylamino and heterocyclicamino)alkyl]-1-piperazinecarboxamides of the formula: ##STR1## wherein B is oxygen or sulfur; Ar is selected from ##STR2## or 2, 3 or 4-pyridyl; X is selected from hydrogen, halogen, loweralkyl, ...
10/02/1990
49563593-aryloxy and 3-arylthioazetidinecarboxamides as anticonvulsants and antiepileptics
Novel 3-aryloxy and 3-arylthioazetidinecarboxamides having utility in a method of treating convulsions and epilepsy and compositions therefor are disclosed having the formula: ##STR1## wherein Z is oxygen or sulfur; B is oxygen or sulfur; Ar is pyrid...
09/11/1990
4898874Acetic acid derivatives of 3-aryl-2,1-benzisoxazole and esters and amides thereof
3-Aryl-2,1-benzisoxazole compounds having the formula: ##STR1## wherein R1 and R2 are hydrogen or methyl; R3 and R4 are hydroxyl, loweralkoxy, amino or --OM wherein M is a pharmaceutically acceptable cation; X i...
02/06/1990
4808404Live vaccine for coccidiosis utilizing coccidial sporozoites
Methods and compositions are disclosed for vaccinating warm-blooded animals against coccidiosis utilizing suspensions of excysted coccidial sporozoites in physiologically balanced medium containing water-soluble polymeric stabilizers selected from gels, g...
02/28/1989
4772600Fused imidazoheterocyclic compounds and pharmaceutical compositions
Imidazoheterocyclic compounds having the formula: ##STR1## wherein the A ring is pyridine in any of its four positions; B is carbonyl, thioxomethyl or hydroxymethylene; Z is hydrogen, halogen, loweralkyl, hydroxy, loweralkoxy, diloweralkylamino or ni...
09/20/1988
4727152Intermediates useful in the preparation of fused aromatic oxazepinones, thiazepinones, diazepinones and sulfur analogs thereof
Chemical intermediates having the formula: ##STR1## wherein A represents an aromatic or heterocyclic ring system selected from benzene, a naphthalene, a quinoline or a pyridine in any of its four positions, any of the rings systems are optionally sub...
02/23/1988
47175632-alkoxy-N-(1-azabicyclo(2.2.2)oct-3-yl) benzamides and thiobenzamides in a method for alleviating emesis caused by non-platinum anticancer drugs
A method of controlling emesis caused by non-platinum anti-cancer drugs with 2-alkoxy-N-(1-azabicyclo[2.2.2]oct-3-yl)benzamides and thiobenzamides having the formula ##STR1## wherein X is oxygen or sulfur; R1 is loweralkyl; and R2
01/05/1988
4705853Fused aromatic oxazepinones, thiazepinones, diazepinones and sulfur analogs thereof
Aromatic azepinones and thiones having the formula ##STR1## wherein; A is benzene, naphthalene, quinoline or pyridine; B is oxygen or sulfur; E is oxygen, sulfur or ##STR2## n is 1, 2 or 3; Z is an amino or a heterocyclic nitrogen-containing rad...
11/10/1987
4698430Nitro, amino and aroylamino-n-phenylpyridinamines
Nitro, amino and aroylamino-N-phenylpyridinamines as chemical intermediates and/or having antidepressant activity having the formula ##STR1## wherein R3 is nitro, amino or aroylamino, and Q is hydrogen, --NR1 R2 or ha...
10/06/1987
4610819Process for the preparation of aromatic-1,4-oxazepinones and thiones
A process for the preparation of 1,4-oxazepinones and thiones having the formula: ##STR1## wherein A is an aromatic ring selected from benzene, naphthalene, quinoline or pyridine; n is 1 to 3; Z is an amino radical; R is hydrogen, loweralkyl, cy...
09/09/1986
4609735Certain aryloxy-4-chloro-2-butanol intermediates
Novel 1-aryloxy-4-amino-2-butanols of the formula wherein AR is 1-naphythyl, 2-naphthyl, indene-4(or 5-)yl, 3-(or 5-)chloro-2-pyridyl, phenyl, monosubstituted phenyl or di-substituted phenyl, R1 is lower alkyl, phenyl, phenylalkyl, 2-hydroxymet...
09/02/1986
4605550Delayed release formulations and processes for making them
There is disclosed a granular composition having particles of average particle size as determined by sieving in the range 70 to 500 microns, the said particles comprising up to 55% of active ingredient e.g. ferrous sulphate having primary particles the ma...
08/12/1986
4605652Method of enhancing memory or correcting memory deficiency with arylamido (and arylthioamido)-azabicycloalkanes
A pharmaceutical method for improving memory or correcting memory deficiency is disclosed, utilizing compounds having the formula: ##STR1## wherein n1, n2, n3, and n4 =0 to 3; R1, R2, ...
08/12/1986
4604404Antiviral sulfonated naphthalene formaldehyde condensation polymers
A method is disclosed for combating Herpes simplex viruses, Types I and II, which comprises topically applying and antiviral arylsulfonic acid polymer to the animal tissue under attack. Bacterial infections are also affectively treated....
08/05/1986
4594189Process for preparing 3-phenoxy-1-azetidines and carboxamide derivatives
An improved process is disclosed for preparing 3-phenoxyazetidines which utilizes a phase transfer catalyst to add the phenoxy group to azetidine blocked in the 1-position by a diphenylmethane group and utilizes a stabilizing tertiary amine base to preven...
06/10/1986
4592866Fused aromatic oxazepinones, thiazepinones, diazepinones and sulfur analogs thereof
Aromatic azepinones and thiones having the formula ##STR1## wherein; A is benzene, naphthalene, quinoline or pyridine; B is oxygen or sulfur; E is oxygen, sulfur or ##STR2## n is 1, 2 or 3; Z is an amino or a heterocyclic nitrogen containing rad...
06/03/1986
45930342-alkoxy-N-(1-azabicyclo[2.2.2]oct-3-yl)benzamides and thiobenzamides
2-Alkoxy-N-(1-azabicyclo[2.2.2]oct-3-yl)benzamides and thiobenzamides having the formula ##STR1## wherein X is oxygen or sulfur; R1 is loweralkyl; and R2 is selected from the group consisting of hydrogen, halo, 4,5-benzo, alkoxy...
06/03/1986
4593102N-[(amino)alkyl]-1-pyrrolidine, 1-piperidine and 1-homopiperidinecarboxamides (and thiocarboxamides) with sulfur linked substitution in the 2, 3 or 4-position
Novel pyrrolidine, piperidine and homopiperidinecarboxamide and thiocarboxamide compounds having the formula: ##STR1## wherein X is --S--, --S(O)-- or --S(O)2 --; A is a loweralkalene chain and A1 and A2 are alkalene ...
06/03/1986
4585785Cis and trans-3-aryloxy-4-hydroxypyrrolidines used as anti-arrhythmics
Cis and trans-3-aryloxy-4-hydroxypyrrolidines and derivatives thereof having the formula: ##STR1## are disclosed wherein R1 is hydrogen, loweralkyl, benzyloxycarbonyl and N-loweralkylcarbamoyl; R2 is hydrogen, lower alkyl, cyclo...
04/29/1986
45380011-Aryloxy-4-amino-2-butanols
Novel 1-aryloxy-4-amino-2-butanols of the formula wherein Ar is 1-naphthyl, 2-naphthyl, indene-4(or 5-)yl, 3-(or 5-)chloro-2-pyridyl, phenyl, monosubstituted phenyl or di-substituted phenyl, R1 is lower alkyl, phenyl, phenyl-alkyl, 2-hydroxymet...
08/27/1985
4536386Method of controlling emesis caused by cisplatin in cancer chemotherapy
High dosages of metoclopramide or a pharmaceutical salt thereof is administered intravenously to human cancer patients undergoing cisplatin chemotherapy to prevent emesis....
08/20/1985
4518603[2-[(Nitropyridinyl)amino]phenyl]arylmethanones in a process for preparing pyrido[1,4]benzodiazepines
[2-[(Nitropyridinyl)amino]phenyl]arylmethanones as chemical intermediates and/or having antidepressant activity having the formula: ##STR1## wherein; B is carbonyl, thioxomethyl, ketal or thioketal, R is hydrogen or --alk1 -Q, Q is hydrogen, --...
05/21/1985
4508724Aryloxymethylpyrrolidinols and piperidinols having antidepressant, antiarrhythmic or hypotensive activity
Novel aryloxymethylpyrrolidinols and piperidinols are provided of the formula: ##STR1## wherein R1 is hydrogen, loweralkyl and phenylloweralkyl; R2 is hydrogen, loweralkyl and acyl; R3 is phenyl, naphthyl, 4-indanyl a...
04/02/1985
4505907N-Formyl and N-hydroxymethyl-3-phenoxy-1-azetidinecarboxamides
N-Formyl and N-hydroxymethyl-3-phenoxy-1-azetidinecarboxamides having the formula: ##STR1## wherein R is selected from formyl and hydroxymethyl and R1 is selected from hydrogen, fluoro, loweralkyl, loweralkoxy, trifluoromethyl, acetyl...
03/19/1985
4480100[2-[(Nitropyridinyl)amino]phenyl]arymethanones
[2-[(Nitropyridinyl)amino]phenyl]arylmethanones as chemical intermediates and/or having antidepressant activity having the formula: ##STR1## wherein: B is carbonyl, thioxomethyl, ketal or thioketal, R is hydrogen or -alk1 -Q, Q is hydrogen, --N...
10/30/1984
44631901-Aryloxy-4-amino-2-butanols
Novel 1-aryloxy-4-amino-2-butanols of the formula wherein Ar is 1-naphthyl, 2-naphthyl, indene-4(or 5-)yl, 3-(or 5-)chloro-2-pyridyl, phenyl, monosubstituted phenyl or di-substituted phenyl, R1 is lower alkyl, phenyl, phenylalkyl, 2-hydroxymeth...
07/31/1984
4452809Trans-4-(2-chlorophenoxy)-1-ethyl-3-pyrrolidinol and anti-depressant use thereof
Cis and trans-3-aryloxy-4-hydroxypyrrolidines and derivatives thereof having the formula: ##STR1## are disclosed wherein R1 is hydrogen, loweralkyl, benzyloxycarbonyl and N-loweralkylcarbamoyl; R2 is hydrogen, lower alkyl, cyclo...
06/05/1984
4447361Aryl substituted pyrido[1,4]benzodiazepines
Pyrido[1,4]benzodiazepines having antidepressant activity of the formula ##STR1## wherein Ar is 2, 3 and 4-pyridinyl, 2 or 3-thienyl, phenyl or a substituted phenyl; R is hydrogen, loweralkyl or an amine on the end of a hydrocarbon chain; Z is hydrog...
05/08/1984
4440785Methods of using 2-aminobiphenylacetic acids, esters, and metal salts thereof to treat inflammation
Novel 2-aminobiphenylacetic acids, esters and metal salts of the formula are disclosed: ##STR1## wherein R represents hydrogen, lower alkyl, sodium or potassium; R1 represents fluoro, chloro, bromo, lower-alkyl or amino; R2 repr...
04/03/1984
43791671-Aryloxy-4-amino-2-butanols and the pharmaceutical use thereof
Novel 1-aryloxy-4-amino-2-butanols of the formula wherein Ar is 1-naphthyl, 2-naphthyl, indene-4(or 5-)yl, 3-(or 5-)chloro-2-pyridyl, phenyl, monosubstituted phenyl or di-substituted phenyl, R1 is lower alkyl, phenyl, phenylalkyl, 2-hydroxymeth...
04/05/1983
43791513-Phenoxyazetidines for anorexigenic activity
3-Phenoxyazetidines having the formula: ##STR1## wherein R is hydrogen, aminocarbonyl and trifluoromethyl having anorexigenic activity are disclosed....
04/05/1983
43775822-Phenyl-4-[cis-2,5-dimethyl-4-(2-pyridinyl)-1-piperazinyl]quinazoline
Novel hypotensive agents are disclosed which are quinazolines substituted in the 2 and 4 position having the general formula: ##STR1## wherein Q is a secondary amine radical illustrated by loweralkanolylamino or a tertiary amine radical such as pyrro...
03/22/1983
4362667Optical isomers of 4-amino-N-(1-cyclohexyl-3-pyrrolidinyl)-N-methylbenzamide
The resolution of racemic 4-amino-N-(1-cyclohexyl-3-pyrrolidinyl)-N-methylbenzamide into the optically active (+) and (-) isomers is disclosed....
12/07/1982
4358599Synthesis of 4-amino-1,2-hydrocarbyl pyrazolidines via 4-nitro analogs
4-Nitro-1,2-hydrocarbyl pyrazolidines are prepared by a novel route from 1,2-disubstituted hydrazines and 1,3-di-(secondary amino)-2-nitropropanes and reduced to the corresponding 4-amino-1,2-hydrocarbyl pyrazolidines, which latter compounds are intermedi...
11/09/1982
4356209Food coloring and flavoring agent from defatted wheat germ
A process for converting defatted wheat germ to a brown cocoa-like flavoring agent for foods which can serve as a replacement of 50% or more cocoa or chocolate without deleterious effect on expectable flavor and color, but with cost reduction of better th...
10/26/1982
43438044-Amino-3-quinolinecarboxylic acids and esters-antisecretory anti-ulcer compounds
A method of reducing gastric acidity and treating peptic ulcers and pharmaceutical compositions therefor with certain 4-amino-3-quinolinecarboxylic acids and esters are disclosed. Illustrative of compounds useful in the method which relies on activity as ...
08/10/1982
43339512-Amino-6-biphenylacetic acids
Novel 2-amino-6-biphenylacetic acids, esters, and metal salts are provided of the formula: ##STR1## wherein R represents hydrogen or lower alkyl, R1 represents fluoro, chloro, bromo, lower-alkyl or amino; R2 represents lower-alk...
06/08/1982
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