Patents Assigned to Hoechst Roussel Pharmaceuticals Incorporated
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Patent number: 5216178Abstract: Novel aminoalkylthiodibenzoxepins, physiologically tolerable acid addition salts thereof, a method of preparing same, pharmaceutical and veterinary preparations including same and methods of treating by administering same are disclosed. These compounds are useful as analgesic, antidepressant and anticonvulsant agents. A process for selectively reducing olefins by alkaline earth metals in loweralkanols is also disclosed.Type: GrantFiled: August 15, 1991Date of Patent: June 1, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Helen H. Ong, Vernon B. Anderson, James A. Profitt
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Patent number: 5216017Abstract: This invention relates to pyrrolo[2,3-b]indole ketones of the formula ##STR1## where R.sub.1 is loweralkyl, aryl or arylloweralkyl; R.sub.2 is hydrogen, halogen or loweralkyl; R.sub.3 is hydrogen or loweralkyl; R.sub.4 is loweralkyl or arylloweralkyl; R.sub.5 is hydrogen, loweralkyl, loweralkenyl, loweralkynyl, arylloweralkyl, formyl, loweralkylcarbonyl, arylloweralkylcarbonyl or loweralkoxycarbonyl; Y is hydrogen, loweralkyl or loweralkoxy; 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 in the treatment of memory impairment characterized by a cholinergic deficit such as that associated with electroshock-induced amnesia and Alzheimer's disease and other senile dementia.Type: GrantFiled: September 26, 1991Date of Patent: June 1, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Richard C. Allen, Denise M. Flanagan
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Patent number: 5216164Abstract: Novel 5-amino-5,6,7,8-tetrahydroquinolines and related compounds, intermediates and processes for the preparation thereof, and methods for relieving memory dysfunction utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: February 10, 1992Date of Patent: June 1, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Richard C. Effland, David Fink
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Patent number: 5214059Abstract: There are described compounds of the formula ##STR1## where A is CH or N;X is hydrogen, loweralkyl, halogen, trifluromethyl, loweralkoxy, arylloweralkoxy, hydroxy or phenylamino;Y is hydrogen, loweralkyl, halogen, loweralkoxy, arylloweralkoxy or hydroxy;R.sub.1 is hydrogen or loweralkyl;R.sub.2 is hydrogen, loweralkyl, formyl, alkylcarbonyl, arylloweralkylcarbonyl, arylcarbonyl, alkoxycarbonyl, arylloweralkoxycarbonyl or aryloxycarbonyl;R.sub.3 is hydrogen, alkyl, alkylcarbonyl, arylloweralkylcarbonyl, arylcarbonyl, alkoxycarbonyl, arylloweralkoxycarbonyl, aryloxycarbonyl or --CH.sub.2 CO.sub.2 C.sub.2 H.sub.5 ;which compounds are useful as topical antiinflammatory agents for the treatment of skin disorders.Type: GrantFiled: August 10, 1992Date of Patent: May 25, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: John J. Tegeler, Eileen M. Gardenhire, Grover C. Helsley
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Patent number: 5208330Abstract: There are disclosed compounds having the formula ##STR1## wherein n is 1-4; R is hydrogen, loweralkyl or loweralkylcarbonyl; R.sub.1 is hydrogen, loweralkyl, loweralkylcarbonyl, aryl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, oxygen-bridged arylloweralkyl, or oxygen-bridged diaryllowerallyl; A is a direct bond or (CHR.sub.3).sub.m, m being 1-3; X is hydrogen, loweralkyl, cycloalkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, formyl, loweralkylcarbonyl, arylcarbonyl, --SH, loweralkylthio, --NHCOR.sub.4 or --NR.sub.5 R.sub.6, R.sub.4 being hydrogen or loweralkyl, and R.sub.5 and R.sub.6 being independently hydrogen, loweralkyl or cycloalkyl; Y is O, S or NR.sub.7 ; and each R.sub.2, each R.sub.3 and R.sub.Type: GrantFiled: February 25, 1992Date of Patent: May 4, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Gregory M. Shutske, Richard C. Effland
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Patent number: 5206387Abstract: There are disclosed compounds having the formula ##STR1## wherein n is 1-4; R is hydrogen, loweralkyl or loweralkylcarbonyl; R.sub.1 is hydrogen, loweralkyl, loweralkylcarbonyl, aryl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, oxygen-bridged arylloweralkyl, or oxygen-bridged diaryllowerallyl; A is a direct bond of (CHR.sub.3).sub.m, m being 1-3; X is hydrogen, loweralkyl, cycloalkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, formyl, loweralkylcarbonyl, arylcarbonyl, --SH, loweralkylthio, --NHCOR.sub.4 or --NR.sub.5 R.sub.6, R.sub.4 being hydrogen or loweralkyl, and R.sub.5 and R.sub.6 being independently hydrogen, loweralkyl or cycloalkyl; Y is O, S or NR.sub.7 ; and each R.sub.2, each R.sub.3 and R.sub.Type: GrantFiled: October 19, 1992Date of Patent: April 27, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Gregory M. Shutske, Richard C. Effland
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Patent number: 5192789Abstract: There are disclosed various compounds of the formula below, ##STR1## where n, X and R.sub.1 through R.sub.4 are as defined in the specification, which are useful for alleviating various memory dysfunctions characterized by a cholinergic deficit such as Alzheimer's disease.Compounds of this invention also inhibit monoamine oxidase and/or act at central .alpha..sub.2 -adrenergic receptors, and hence are useful as antidepressants.Type: GrantFiled: January 9, 1992Date of Patent: March 9, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Helen H. Ong, Gerard J. O'Malley, Michael C. Merriman, Mark G. Palermo
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Patent number: 5192776Abstract: Carbonyl derivatives of 4-pentafluorophenoxypiperidines and methods for treating convulsions, depression, and hypertension utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: September 23, 1991Date of Patent: March 9, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Grover C. Helsley, Larry Davis, Gordon E. Olsen
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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
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Patent number: 5182275Abstract: There are disclosed novel compounds of the formula ##STR1## where X is hydrogen, loweralkyl, loweralkoxy, hydroxy, halogen, nitro or trifluoromethyl; R.sub.1 is hydrogen or loweralkyl; R.sub.2 is hydrogen, loweralkyl, arylloweralkyl or --(CH.sub.2).sub.m R.sub.7 wherein m is 1, 2 or 3 and R.sub.7 is cyano or amino; R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl; R.sub.5 and R.sub.6 are independently hydrogen or loweralkyl, or R.sub.5 +R.sub.6 taken together with the carbon atom to which they are attached constitute a cyclobutane, cyclopentane, cyclohexane, cycloheptane, pyrrolidine, piperidine, morpholine or thiomorpholine ring, or R.sub.5 is hydrogen and R.sub.6 is aryl or --CH.sub.2 OR.sub.8 wherein R.sub.8 is hydrogen, loweralkyl or loweralkylcarbonyl, which are useful for enhancing memory.Type: GrantFiled: May 10, 1990Date of Patent: January 26, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Karl Schonafinger, Helen H. Ong
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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
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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
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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
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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
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Patent number: 5177101Abstract: There are disclosed various derivatives related to physostigmine of the formula below, ##STR1## where Z, R.sub.1 and R.sub.2 are as defined in the specification, which compounds are useful for enhancing cholinergic function, and as analgesic agents.Type: GrantFiled: August 23, 1991Date of Patent: January 5, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Edward J. Glamkowski, Yulin Chiang, Russell R. L. Hamer
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Patent number: 5177088Abstract: There are disclosed various compounds of the formula below, ##STR1## where R.sub.1, W, X, Y and Z are as defined in the specification; which are useful for alleviating various memory dysfunctions such as Alzheimer's disease, as modulators of neurotransmitter function such as serotonergic and adrenergic, and as such are useful as antidepressants, anxiolytics, atypical antipsychotics, antiemetics, and for the treatment of personality disorders such as obsessive compulsive disorders.Type: GrantFiled: April 17, 1991Date of Patent: January 5, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Richard C. Effland, Joseph T. Klein, Lawrence L. Martin
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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
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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
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Patent number: 5166170Abstract: There are disclosed various compounds depicted by the general formula, ##STR1## where the parameters X, Y, R.sub.1, R.sub.2, and R.sub.3 are as defined in the specification. These compounds are disclosed as topical antiinflammatory agents useful for the treatment of various skin disorders including exogenous dermatitis, endogenous dermatitis, dermatitis of unknown etiology and other cutaneous disorders with an inflammatory component.Type: GrantFiled: July 3, 1989Date of Patent: November 24, 1992Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: John J. Tegeler, Eileen M. Gardenhire, Grover C. Helsley
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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