Patents Represented by Attorney, Agent or Law Firm Elliott Korsen
-
Patent number: 5185350Abstract: This invention relates to substituted pyridinylamino-1H-indoles, 1H-indazoles, 2H-indazoles, benzo[b]thiophenes and 1,2-benzisothiazoles of the formula ##STR1## wherein Q is S, N or NR.sub.2 ;Y is CH, N or NR.sub.2 ;R.sub.1 is hydrogen, loweralkyl, loweralkynyl, loweralkenyl, arylloweralkyl, loweralkoxycarbonylaminoloweralkylcarbonyl, arylloweralkoxycarbonylaminoloweralkylcarbonyl, aminoloweralkylcarbonyl, loweralkoxycarbonyl or acyl;R.sub.2 is hydrogen or loweralkyl;R.sub.3 is hydrogen or loweralkyl;X is hydrogen, loweralkyl, halogen; andn is 0 or 1; or a pharmaceutically acceptable acid addition salt thereof.The compounds of this invention are useful in the treatment of memory dysfunctions characterized by a cholinergic deficit such as the type associated with Alzheimer's disease and other memory disorders.Type: GrantFiled: September 23, 1991Date of Patent: February 9, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Richard C. Effland, Joseph T. Klein, Lawrence L. Martin
-
Patent number: 5180834Abstract: This invention relates to 6,7-dihydro-3-phenyl-1,2-benzisoxazol-4(5H)-ones and -ols of the formula ##STR1## wherein X is ##STR2## or loweralkyl; Y is hydrogen, halogen, loweralkyl, loweralkoxy, trifluoromethyl, nitro or amino; R is H when the bond between the oxygen atom and the carbon atom in question is a single bond; otherwise the dotted line signifies part of a double bond to the oxygen atom; R.sub.1 is hydrogen, loweralkyl or arylloweralkyl; R.sub.2 and R.sub.3 are independently hydrogen, loweralkyl or arylloweralkyl, or R.sub.2 and R.sub.3 taken together with the nitrogen atom form an optionally substituted heterocycle selected from the group consisting of piperidinyl, pyrrolidinyl, morpholinyl, imidazol-1-yl, 1-piperazinyl, said substituents being hydrogen or loweralkyl;4-substituted-1-piperazinyl of the formula ##STR3## R.sub.8 is hydrogen or --OH; R.sub.Type: GrantFiled: February 28, 1992Date of Patent: January 19, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: David G. Wettlaufer, Gregory M. Shutske, Peter A. Nemoto
-
Patent number: 5179099Abstract: This invention relates to 2,3-dihydro-1-(pyridinylamino)-indoles of the formula ##STR1## wherein R.sub.1 is hydrogen, loweralkyl, aryl, arylloweralkyl, alkenyl, alkynyl or heteroarylloweralkyl selected from the group consisting of pyridinylmethyl, pyridinylethyl, thienylmethyl, thienylethyl; R.sub.2 and R.sub.3 and independently hydrogen, loweralkyl, aryl, arylloweralkyl or heteroarylloweralkyl selected from the group consisting of pyridinylmethyl, pyridinylethyl, thienylmethyl, thienylethyl; or R.sub.2 and R.sub.3 together form a cycloalkane ring of 4 to 6 carbons or a spiro-fused aryl or heteroaryl; the term heteroaryl signifying a group selected from pyridine or thiophene; X and Y are independently hydrogen, halogen, hydroxy, loweralkyl, loweralkoxy, nitro, amino or trifluoromethyl; m and n are independently integers of 1 to 3, or a pharmaceutically acceptable acid addition salt thereof or where appropriate, an optical, geometrical or stereoisomer or racemic mixture thereof.Type: GrantFiled: May 24, 1991Date of Patent: January 12, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Richard C. Effland, David G. Wettlaufer, Joseph T. Klein
-
Patent number: 5179119Abstract: This invention relates to 1,3-dihydro-1-(pyridinylamino)-2H-indol-2-ones of the formula ##STR1## where R.sub.1, R.sub.2 and R.sub.3 are independently hydrogen, loweralkyl, aryl, arylloweralkyl or heteroarylloweralkyl selected from the group consisting of pyridinylmethyl, pyridinylethyl, thienylmethyl, thienylethyl; or R.sub.2 and R.sub.3 together form a cycloalkane ring of 4 to 6 carbons or a spiro-fused aryl cycloalkane or heterocycloalkyl selected from the group consisting of piperidine and tetrahydropyran; X and Y are independently hydrogen, halogen, hydroxy, loweralkyl, loweralkoxy, nitro, amino or trifluoromethyl; m and n are independently integers of 1 to 3, the pharmaceutically acceptable acid addition salts thereof and, where applicable the optical, geometrical and stereoisomers and racemic mixtures thereof. The compounds of this invention display utility as analgesics, anticonvulsants, for enhancing memory and for the treatment of Alzheimer's disease.Type: GrantFiled: July 26, 1991Date of Patent: January 12, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Richard C. Effland, David G. Wettlaufer
-
Patent number: 5179204Abstract: This invention relates to N-heteroaryl-4-pyrimidinamines of the formula ##STR1## where R.sub.1 is hydrogen, loweralkyl, aryl, or arylloweralkyl; R.sub.2 and R.sub.3 are independently hydrogen or loweralkyl, or R.sub.2 and R.sub.3 taken together are aryl; R.sub.4 and R.sub.5 are independently hydrogen or loweralkyl, or R.sub.4 and R.sub.5 taken together are aryl; X is hydrogen, halogen, cyano, nitro, amino, loweralkyl, loweralkoxy, trifluoromethyl or ##STR2## where Y is hydrogen, halogen or loweralkyl; m is an integer of 1 to 3; and the pharmaceutically acceptable acid addition salts thereof and where applicable the geometrical and optical isomers and racemic mixtures thereof. The compounds of this invention display utility as memory enhancing agents and as analgesic agents.Type: GrantFiled: September 18, 1990Date of Patent: January 12, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Richard C. Effland, Joseph T. Klein, Larry Davis, Gordon E. Olsen
-
Patent number: 5173497Abstract: This invention relates to compounds of the formula ##STR1## where X is --NH, oxygen, N-loweralkyl, or N-arylloweralkyl; R.sub.1 is hydrogen, loweralkyl, cycloalkyl, aryl, arylloweralkyl, loweralkylene, haloloweralkyl, heteroaryl selected from the group consisting of thienyl, furnayl, pyrrolyl and pyridinyl; heteroarylloweralkyl, heterocyclic selected from piperidinyl, piperazinyl, pyrrolidinyl; or heterocyclicloweralkyl; R.sub.2 is hydrogen or loweralkyl; R.sub.3 is loweralkyl or arylloweralkyl; R.sub.4 is hydrogen, loweralkyl, loweralkenyl, loweralkynyl, arylloweralkyl, formyl, loweralkylcarbonyl, arylloweralkylcarbonyl or loweralkoxycarbonyl; Y is hydrogen, loweralkyl or loweralkoxy, and the pharmaceutically acceptable acid addition salts thereof, and where applicable, the geometric and optical isomers and racemic mixtures thereof.Type: GrantFiled: September 26, 1991Date of Patent: December 22, 1992Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventor: Denise M. Flanagan
-
Patent number: 5166436Abstract: A process for preparing N-ethylhydroxylamine hydrochloride which comprises reacting hydroxylamine hydrochloride with di-t-butyl dicarbonate in the presence of a base selected from sodium carbonate, potassium carbonate, sodium bicarbonate, potassium bicarbonate, sodium or potassium hydroxide or triethylamine, in a non-reactive solvent, alkylating said reaction product with an alkyl halide and then cleaving with a strong acid the tert-butyloxycarbonyl (BOC) portion of the alkylated product.Type: GrantFiled: September 23, 1991Date of Patent: November 24, 1992Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventor: George E. Lee
-
Patent number: 5166163Abstract: This invention relates to 3-(1H-indazol-3-yl)-4-pyridinamines of the formula ##STR1## where R.sub.1 is hydrogen, loweralkyl, arylalkyl or acyl; R.sub.2 is hydrogen, loweralkyl or arylalkyl; R.sub.3 is hydrogen, loweralkyl or aryl and X is hydrogen, halogen, nitro or amino or the pharmaceutically acceptable addition salts thereof, and where applicable, the geometric and optical isomers and racemic mixtures thereof. The compounds of this invention are useful as analgesics and as topical antiinflammatory agents for the treatment of various dermatoses.Type: GrantFiled: May 6, 1991Date of Patent: November 24, 1992Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Richard C. Effland, Joseph T. Klein
-
Patent number: 5155226Abstract: A method of preparing 9-amino-1,2,3,4-tetrahydroacridine by the reaction of 2-aminobenzonitrile and cyclohexanone with p-toluenesulfonic acid monohydrate in xylenes is disclosed.Type: GrantFiled: February 19, 1991Date of Patent: October 13, 1992Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Thomas B. K. Lee, Keith E. Goehring
-
Patent number: 5149866Abstract: The present inventon pertains to a process for the preparation of omega-arylalkanoic acids of the genral formulaR--Ar--R.sup.1 --COOHwherein R is hydrogen, hydroxy, C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 alkoxy, or aryl; wherein R.sup.1 is C.sub.1 -C.sub.4 alkyl; and wherein Ar is an aryl group which can be further substituted with at least one of hydroxy, C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 alkoxy, aryl, halide, amino, or acetamido. The omega arylalkanoic acids of the given formula are prepared using catalysts which provide an improvement over the known Willgerodt-Kindler reaction.The present invention also pertains to methods for removing sulfur during the above-described process for the preparation of the omega-arylalkanoic acids.Type: GrantFiled: August 14, 1991Date of Patent: September 22, 1992Assignee: Hoechst Celanese CorporationInventors: Huh-Sun Chiou, Mark R. Rubino, Susan W. Jahoda, Daniel Lindley, John R. Battler
-
Patent number: 5145844Abstract: Novel hydroxy-,alkoxy-and benzyloxy-substituted phospholipids, a process for the preparation thereof, and methods for treating pain, phospholipase A.sub.2 mediated inflammation and similar conditions utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: March 5, 1991Date of Patent: September 8, 1992Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: John J. Tegeler, Kirk D. Shoger
-
Patent number: 5145866Abstract: A method of treating anxiety with the aid of R(+)-3-amino-1-hydroxypyrrolidin-2-one of the formula ##STR1## is disclosed.Type: GrantFiled: April 22, 1991Date of Patent: September 8, 1992Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Robert W. Dunn, Roy Corbett
-
Patent number: 5145965Abstract: Novel 2,6-methanopyrrolo-3-benzazocines, intermediates, processes for the preparation thereof, and methods for alleviating pain utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: March 11, 1991Date of Patent: September 8, 1992Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Richard C. Allen, David G. Wettlaufer
-
Patent number: 5114936Abstract: This invention relates to 6,7-dihydro-3-phenyl-1,2-benzisoxazol-4(5H)-ones and -ols of the formula ##STR1## wherein X is (Y) ##STR2## or loweralkyl; Y is hydrogen, halogen, loweralkyl, loweralkoxy, trifluoromethyl, nitro or amino; R is H when the bond between the oxygen atom and the carbon atom in question is a single bond; otherwise the dotted line signifies part of a double bond to the oxygen atom; R.sub.1 is hydrogen, loweralkyl or arylloweralkyl; R.sub.2 and R.sub.3 are independently hydrogen, lower alkyl or arylloweralkyl, or R.sub.2 and R.sub.3 taken together with the nitogen atom form an optionally substituted heterocycle selected from the group consisting of piperidinyl, pyrrolidinyl, morpholinyl, imidazol-1-yl, 1-piperazinyl, said substituents being hydrogen or loweralkyl; 4-substituted-1-piperazinyl of the formula ##STR3## where R.sub.Type: GrantFiled: April 26, 1991Date of Patent: May 19, 1992Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: David G. Wettlaufer, Gregory M. Shutske, Peter A. Nemoto
-
Patent number: 5109011Abstract: This invention relates to p-acylaminophenoxycarbamates having the formula ##STR1## where R.sub.1 and R.sub.2 are each independently hydrogen, loweralkyl, aryl and arylloweralkyl; R.sub.3 is hydrogen, loweralkyl, aryllowerallkyl; R.sub.4 is hydrogen, loweralkyl, formyl, alkylcarbonyl, arylloweralkyl, phenylcarbonyl, arylloweralkylcarbonyl, substituted phenylcarbonyl, pyridylcarbonyl, and substituted pyridylcarbonyl with the proviso that if R.sub.4 contains a carbonyl group directly attached to the oxygen of the N-O moiety, R.sub.3 cannot by hydrogen; or R.sub.3 and R.sub.4 taken together form a heterocyclic ring selected from the group consisting of imidazole or loweralkylimidazole; X is hydrogen, halogen, hydroxy, loweralkyl, loweralkoxy, nitro, amino or trifluoromethyl; and p is an integer selected from 0 and 1; the pharmaceutically acceptable acid addition salts thereof, and where applicable, the geometric and stereoisomers and racemic mixtures thereof.Type: GrantFiled: July 30, 1990Date of Patent: April 28, 1992Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Richard C. Allen, Raymond W. Kosley, Jr., Bettina Spahl
-
Patent number: 5097033Abstract: Novel 2,6-methano-1,3-benzodiazocines, intermediates, processes for the preparation thereof, and methods for alleviating pain and for alleviating various memory dysfunctions characterized by a decreased cholinergic function, such as Alzheimer's disease, utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: January 9, 1991Date of Patent: March 17, 1992Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Richard C. Allen, Marc N. Agnew, David M. Fink
-
Patent number: 5081117Abstract: This invention relates to 4- and 6-carbamates related to physostigmine of the formula ##STR1## where R.sub.1 is alkyl, cycloalkyl, bicycloalkyl, aryl or arylloweralkyl; R.sub.2 is hydrogen or alkyl or the group --NR.sub.1 R.sub.2 taken together forms a monocyclic or bicyclic ring of 5 to 12 carbons; m is 0,1, or 2; each X is independently hydrogen, halogen, loweralkyl, nitro or amino; and the pharmaceutically acceptable acid addition salts thereof, and where applicable, the geometric and optical isomers and racemic mixtures thereof. This invention also relates to novel intermediates useful in the preparation of the 4- and 6-carbamates. The compounds of this invention display utility for alleviating various memory dysfunctions characterized by a decreased cholinergic function, such as Alzheimer's disease.Type: GrantFiled: November 3, 1989Date of Patent: January 14, 1992Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Edward J. Glamkowski, Barbara E. Kurys
-
Patent number: 5078280Abstract: An improvement in a mechanic's creeper whereby a Z-shaped shelf member with a powerful magnet is attached to an edge of the creeper. The shelf member with its magnet holds tools in such a way that the tools can be readily accessible to the mechanic.Type: GrantFiled: March 22, 1991Date of Patent: January 7, 1992Assignee: Hoechst-Roussel Pharmaceutical IncorporatedInventor: Ryan C. Nordeen
-
Patent number: 5077405Abstract: This invention relates to 3-(1-substituted-4-piperazinyl)-1H-indazoles having the following formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, arylloweralkyl, acyl, cycloalkylloweralkylene, and phenylsulfonyl; and R.sub.2 is hydrogen, lower alkyl, hydroxyloweralkyl of the formula -(loweralkylene)-OH, arylloweralkyl, acyl, cycloalkylloweralkylene, ##STR2## where Z is selected from hydrogen, halogen, loweralkoxy, CF.sub.3, NO.sub.2, and NH.sub.2 ; ##STR3## where Z is as defined above; ##STR4## where Z is as defined above; ##STR5## where R.sub.3 and R.sub.4 are each independently hydrogen and loweralkyl; ##STR6## where Z is as defined above; ##STR7## where R' and R" are each independently hydrogen and loweralkyl; X is hydrogen, loweralkyl, hydroxyl, halogen, loweralkoxy, CF.sub.3, NO.sub.2 and amino; n is an integer of 1 to 4, with the further proviso that R.sub.2 is not loweralkyl when R.sub.Type: GrantFiled: May 21, 1990Date of Patent: December 31, 1991Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Joseph T. Strupczewski, Kenneth J. Bordeau
-
Patent number: 5055476Abstract: This invention relates to 3-(1,2-benzisoxazol-3-yl)-4-pyridinamines of the formula ##STR1## where R.sub.1 is hydrogen, loweralkyl, arylalkyl or acyl; R.sub.2 is hydrogen, loweralkyl or arylalkyl, X is hydrogen, halogen, nitro or amino; or the pharmaceutically acceptable addition salts thereof, and where applicable, the geometric and optical isomers and racemic mixtures thereof. The compounds of this invention are useful as analgesics, for alleviating various memory dysfunctions characterized by a decreased cholinergic function, as cognition enhancers in the treatment of senile dementia such as Alzheimer's disease and as topical antiinflammatory agents for the treatment of various dermatoses.Type: GrantFiled: August 13, 1990Date of Patent: October 8, 1991Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Richard C. Effland, Joseph T. Klein