Patents Assigned to Hoechst-Roussel Pharmaceutical Incorporated
  • Patent number: 5264587
    Abstract: 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, furanyl, 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: Grant
    Filed: August 10, 1992
    Date of Patent: November 23, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventor: Denise M. Flanagan
  • Patent number: 5264442
    Abstract: This invention relates to compounds of the formula ##STR1## where R.sub.1 -R.sub.6, X and Y are as defined in the specification, which are useful for the treatment of various memory dysfunctions characterized by a cholinergic deficit and thus may be indicated in the treatment of Alzheimer's disease.
    Type: Grant
    Filed: February 14, 1992
    Date of Patent: November 23, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Richard C. Effland, Larry Davis, Gordon E. Olsen
  • Patent number: 5264576
    Abstract: There are disclosed novel pyrazolo[4,3-c]pyridines of the formula ##STR1## where Ar and R.sub.1 are as defined in the specification, which are useful as serotonin reuptake inhibitors and as such may be useful for the treatment of depression, obsessive-compulsive disorders, stuttering and trichotillomania.
    Type: Grant
    Filed: October 22, 1992
    Date of Patent: November 23, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Gregory M. Shutske, Kevin J. Kapples, John D. Tomer, IV
  • Patent number: 5260319
    Abstract: Novel thienobenzoxepins and naphthothiophenes, intermediates and processes for the preparation thereof, and methods of alleviating pain utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: March 19, 1993
    Date of Patent: November 9, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Richard C. Effland, David G. Wettlaufer
  • Patent number: 5260339
    Abstract: Novel 4-phenyl-1,3-benzodiazepines and 2-amino-.alpha.-phenylphenethylamines, novel intermediates thereof, and methods of preparing same are described. These benzodiazepines are useful as antidepressants, analgetics and anticonvulsants. The 2-amino-.alpha.-phenylphenethylamines are useful as anticonvulsant and neuroprotective agents.
    Type: Grant
    Filed: October 8, 1992
    Date of Patent: November 9, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Lawrence L. Martin, Manfred Worm, Charles A. Crichlow
  • Patent number: 5256672
    Abstract: 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, pyrtolidinyl, morpholinyl, imidazol-1-yl, 1-piperazinyl, said substituents being hydrogen or loweralkyl; 4-substituted-1-piperazinyl of the formula where R.sub.
    Type: Grant
    Filed: December 13, 1992
    Date of Patent: October 26, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: David G. Wettlaufer, Gregory M. Shutske, Peter A. Nemoto
  • Patent number: 5246947
    Abstract: 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: Grant
    Filed: August 7, 1992
    Date of Patent: September 21, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Richard C. Effland, Joseph T. Klein, Lawrence L. Martin
  • Patent number: 5247097
    Abstract: Novel oxolabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: May 28, 1992
    Date of Patent: September 21, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventor: Nicholas J. Hrib
  • Patent number: 5240927
    Abstract: There are disclosed various compounds of the formula depicted below, ##STR1## where the parameters m, n, p, q, X and R are as defined in the specification, as being useful as antipsychotic agents.
    Type: Grant
    Filed: May 19, 1992
    Date of Patent: August 31, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Nicholas J. Hrib, John G. Jurcak
  • Patent number: 5234941
    Abstract: There are disclosed various compounds of the formula below, ##STR1## where the parameters R.sub.1 and R.sub.2 are as defined in the specification, which compounds are useful for alleviating various memory dysfunctions characterized by a cholinergic deficit such as Alzheimer's disease.
    Type: Grant
    Filed: August 5, 1992
    Date of Patent: August 10, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Denise M. Flanagan, Lawrence L. Martin
  • Patent number: 5234931
    Abstract: This invention relates to compounds of the formula ##STR1## where X is --O--, --S-- or --NH--;Y is hydrogen, halogen and loweralkoxy;p is 1 or 2;n is 2, 3 or 4;R is hydrogen, loweralkyl, loweralkoxy, hydroxy, halogen, amino, loweralkylamino, nitro, loweralkylthio, trifluoromethoxy, cyano, trifluoromethyl, ##STR2## R.sub.1 is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, carboxyl, loweralkylamino, nitro, loweralkylthio, cyano, and trifluoromethyl;m is 1 or 2; a pharmaceutically acceptable acid addition salt thereof and, where applicable the geometric and optical isomers and racemic mixtures thereof.The compounds and compositions of this invention are useful as antipsychotic agents, as 5-HT.sub.3 receptor antagonists and as inhibitors of the reuptake of serotonin.
    Type: Grant
    Filed: February 4, 1992
    Date of Patent: August 10, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Edward J. Glamkowski, David M. Fink, Barbara E. Kurys, Yulin Chiang
  • Patent number: 5232927
    Abstract: There are disclosed novel compounds having the formula, ##STR1## wherein, m is an integer of 0-3;n is an integer of 1-4;R.sub.1 is hydrogen, alkyl, cycloalkyl, arylloweralkyl, aryl, naphthyl, furyl, thienyl, pyridinyl or pyrrolyl;each R.sub.2 and R.sub.3 are independently hydrogen, loweralkyl or aryllowralkyl, or alternatively R.sub.2 and R.sub.3 taken together form a methylene or ethylene bridge;X is hydrogen, loweralkyl, cycloalkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, formyl, loweralkoxycarbonyl, 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 CH.sub.2, CH.dbd.CH, O, S or NR.sub.7, R.sub.7 being hydrogen, loweralkyl or arylloweralkyl;with the proviso that the number of said methylene or ethylene bridge shall not exceed 1 and that when Y is CH.sub.2, one and only one combination of R.sub.2 and R.sub.
    Type: Grant
    Filed: April 18, 1991
    Date of Patent: August 3, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Gregory M. Shutske, Kevin J. Kapples
  • Patent number: 5231093
    Abstract: There are disclosed various compounds of the formula below, ##STR1## where the parameters R.sub.1 and R.sub.2 are as defined in the specification, which compounds are useful for alleviating various memory dysfunctions characterized by a cholinergic deficit such as Alzheimer's disease.
    Type: Grant
    Filed: August 5, 1992
    Date of Patent: July 27, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Denise M. Flanagan, Lawrence L. Martin
  • Patent number: 5229517
    Abstract: Novel 2-(4-piperidinyl)-1H-pyrido[4,3-b]indol-1-ones and related compounds, intermediates and processes for the preparation thereof, and methods of treating psychoses employing compounds and compositions thereof are disclosed.
    Type: Grant
    Filed: January 15, 1992
    Date of Patent: July 20, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Lawrence L. Martin, Denise M. Flanagan, Joseph F. Payack
  • Patent number: 5229417
    Abstract: Novel 2-(3-phenylpropyl)hydrazines, intermediates in and processes for the preparation thereof, and a method of treating personality disorders utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: December 5, 1991
    Date of Patent: July 20, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Richard C. Effland, Joseph T. Klein
  • Patent number: 5229388
    Abstract: There are disclosed compounds of the formula, ##STR1## where n is 0, 1 or 2; A is ##STR2## where X in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, loweralkoxy, amino, cyano, trifluoromethyl or methylthio; Y in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, loweralkoxy, amino, cyano, trifluoromethyl or methylthio; m is 1 or 2; k is 1 or 2; R.sub.1 and R.sub.2 are independently hydrogen, loweralkyl, ##STR3## or aryl except that when R.sub.1 is ##STR4## or aryl, R.sub.2 is hydrogen, or alternatively R.sub.1 +R.sub.2 taken together with the carbon atom to which they are attached form a cyclopentane, cyclohexane, cycloheptane, pyran, thiopyran, indan or piperidine ring; R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl, or alternatively R.sub.3 +R.sub.
    Type: Grant
    Filed: November 21, 1991
    Date of Patent: July 20, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Nicholas J. Hrib, John G. Jurcak
  • Patent number: 5229401
    Abstract: 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 Alzhemier's disease and other memory disorders.
    Type: Grant
    Filed: August 7, 1992
    Date of Patent: July 20, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Richard C. Effland, Joseph T. Klein, Lawrence L. Martin
  • Patent number: 5227388
    Abstract: Novel naphtho[2,3-b]thiophen-9(4H)-ones of the formula ##STR1## wherein R is loweralkyl or arylloweralkyl; X and Y are independently hydrogen, loweralkyl, halogen, loweralkoxy, or trifluoromethyl; W is CH.sub.2, CHOH, or C.dbd.O; n is 1 or 2; an optical isomer or pharmaceutically acceptable salt thereof, processes for the preparation thereof, and methods of alleviating pain utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: January 30, 1991
    Date of Patent: July 13, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Richard C. Effland, David G. Wettlaufer
  • Patent number: 5225412
    Abstract: Novel benzisothiazole- and benzisoxazole-3-carboxamides, processes and intermediates for the preparation thereof, and methods of treating psychoses utilizing compounds and compositions thereof are disclosed.
    Type: Grant
    Filed: June 16, 1992
    Date of Patent: July 6, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Nicholas J. Hrib, John G. Jurcak
  • Patent number: 5221682
    Abstract: There are described compounds of the formula ##STR1## where n is 0 or 1;X is O or NR.sub.2, R.sub.2 being hydrogen, loweralkyl or loweralkylcarbonyl;R is hydrogen, loweralkyl, arylloweralkyl or loweralkylcarbonyl; andR.sub.1 is ##STR2## wherein R.sub.3 is hydrogen, loweralkyl or loweralkylcarbonyl; m is 1 or 2; each R.sub.4 is independently hydrogen or loweralkyl; and Y is hydrogen, halogen, loweralkyl, loweralkoxy or trifluoromethyl;which compounds are useful as topical antiinflammatory agents for the treatment of various dematoses.
    Type: Grant
    Filed: May 3, 1991
    Date of Patent: June 22, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Richard C. Effland, Joseph T. Klein, Gordon E. Olsen, Larry Davis, Russell R. L. Hamer, Brian S. Freed