Patents Represented by Attorney, Agent or Law Firm Tatsuya Ikeda
  • Patent number: 5100891
    Abstract: 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.Compound of this invention also inhibit monoamine oxidase and/or act at central .alpha..sub.2 -adrenergic receptors, and hence are useful as antidepressants.
    Type: Grant
    Filed: January 18, 1991
    Date of Patent: March 31, 1992
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Helen H. Ong, Gerard J. O'Malley, Michael C. Merriman, Mark G. Palermo
  • Patent number: 5095019
    Abstract: There are described compounds of the formula ##STR1## where R.sub.1 is hydrogen, loweralkyl, arylloweralkyl or aryl;R.sub.2 when present is hydrogen, loweralkyl, arylloweralkyl; andR.sub.3 is hydrogen, loweralkyl, cycloalkyl or aryl;which compounds are useful as analgesics and topical antiinflammatory agents for the treatment of skin disorders.
    Type: Grant
    Filed: August 5, 1991
    Date of Patent: March 10, 1992
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Effland, Joseph T. Klein
  • Patent number: 5091541
    Abstract: There are disclosed various compounds of the formula below, ##STR1## where X is O, S, NH, N-loweralkyl, or N-arylloweralkyl;Y is hydrogen, fluorine, chlorine, bromine, nitro, loweralkyl, loweralkoxy, or triloweralkylsilyl;R.sub.1 is loweralkyl, halogen-substituted loweralkyl, aryl, arylloweralkyl, cycloalkyl, heteroaryl or heteroarylloweralkyl;R.sub.2 is hydrogen, loweralkyl or arylloweralkyl;R.sub.3 is loweralkyl or arylloweralkyl;R.sub.4 is hydrogen, loweralkyl, loweralkenyl, loweralkynyl, arylloweralkyl, formyl, loweralkylcarbonyl, arylloweralkylcarbonyl or loweralkoxycarbonyl;R.sub.5 is hydrogen or loweralkyl; andm is 0 or 1, with the proviso that when m is O, R.sub.1 may also be hydrogen.which compounds are useful for alleviating various memory dysfunctions characterized by a cholinergic deficit such as Alzheimer's disease.
    Type: Grant
    Filed: October 24, 1990
    Date of Patent: February 25, 1992
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Gerard J. O'Malley, Richard C. Allen, John I. White
  • Patent number: 5089615
    Abstract: There are described compounds of the formula ##STR1## where X is hydrogen, loweralkyl, loweralkoxy or halogen;R when present is hydrogen, loweralkyl or aryloweralkyl;R.sub.1 is hydrogen, loweralkyl or arylloweralkyl; andR.sub.2 when present is hydrogen or loweralkyl;which compounds are useful for alleviating various memory dysfunctions characterized by a decreased cholinergic function such Alzheimer's disease.
    Type: Grant
    Filed: January 11, 1991
    Date of Patent: February 18, 1992
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Lawrence L. Martin, Joseph F. Payack, Helen H. Ong
  • Patent number: 5077289
    Abstract: 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: Grant
    Filed: November 30, 1989
    Date of Patent: December 31, 1991
    Assignee: Hoechst Roussel Pharmaceuticals Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang, Russell R. L. Hamer
  • Patent number: 5070209
    Abstract: Novel 12-halogenated forskolin derivatives, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: April 12, 1991
    Date of Patent: December 3, 1991
    Assignee: Hoechst Roussel Pharmaceuticals Inc.
    Inventor: Gregory M. Shutske
  • Patent number: 5059602
    Abstract: There are described compounds of the formula ##STR1## where R.sub.1 is hydrogen, loweralkyl, arylloweralkyl or aryl;R.sub.2 when present is hydrogen, loweralkyl, arylloweralkyl; andR.sub.3 is hydrogen, loweralkyl, cycloalkyl or aryl;which compounds are useful as analgesics and topical antiinflammatory agents for the treatment of skin disorders.
    Type: Grant
    Filed: August 27, 1990
    Date of Patent: October 22, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Effland, Joseph T. Klein
  • Patent number: 5059688
    Abstract: The invention relates to 1-aryloxy-2,3,4,5-tetrahydro-3-benzazepines of the formula ##STR1## wherein Y is the same or different and is hydrogen and lower alkoxy; X is hydrogen, halogen, lower alkyl, lower alkoxy, CF.sub.3, No.sub.2, CN and NH.sub.2 ; R is hydrogen, lower alkyl, cycloalkyllower alkyl, ##STR2## Ar lower alkyl of the formula ##STR3## where Z is hydrogen, lower alkyl, lower alkoxy, halogen CF.sub.3, NO.sub.2 and NH.sub.2 ; Aryloxy lower alkyl of the formula ##STR4## where Z is as previously defined; and an alkylene amine of the formula ##STR5## where R.sub.1 and R.sub.2 are the same or different and are hydrogen and lower alkyl, n is an integer of 1 or 2; and the pharmaceutically acceptable acid addition salts thereof.
    Type: Grant
    Filed: April 23, 1990
    Date of Patent: October 22, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Effland, Joseph T. Klein, Larry Davis
  • Patent number: 5045539
    Abstract: There are disclosed compounds having the formula ##STR1## where n is 0, 1, or 2;p and q are each independently 1, 2 or 3;each X and each Y are independently hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, nitro, amino, loweralkylamino, diloweralkylamino, trifluoromethyl or loweralkylthio;R.sub.1 and R.sub.2 are each independently hydrogen or loweralkyl; andR.sub.3 is hydrogen, loweralkyl, loweralkylcarbonyl, arylloweralkyl or aminocarbonyl;which are useful as analgesic, antipsychotic and anticonvulsant agents.
    Type: Grant
    Filed: February 6, 1991
    Date of Patent: September 3, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Grover C. Helsley, John J. Tegeler, Kirk D. Shoger
  • Patent number: 5039809
    Abstract: A compound of the formula: ##STR1## where n is 1, 2, or 3;R.sub.3 is hydrogen or loweralkyl;R.sub.4 is hydrogen or loweralkyl; andAr is a phenyl group optionally mono-substituted with a loweralkoxy, halogen or trifluoromethyl group which are useful as intermediates.
    Type: Grant
    Filed: October 9, 1990
    Date of Patent: August 13, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Effland, David M. Fink
  • Patent number: 5039687
    Abstract: There are disclosed novel compounds of the formula ##STR1## where R is H, loweralkyl, halogen, cyano, loweralkanoyl, arylloweralkanoyl, aroyl, --CH(OH)r.sub.1, --C(OH)r.sub.1 r.sub.2 or --CH.sub.2 Or.sub.2, where r.sub.1 is H, loweralkyl, arylloweralkyl or aryl and r.sub.2 is loweralkyl; R.sub.1 H, loweralkyl, arylloweralkyl, phenyl, nitrophenyl, cyanophenyl, trifluoromethylphenyl, aminophenyl, loweralkanoylaminophenyl, loweralkoxycarbonyl, arylloweralkylkoxycarbonyl, aryloxycarbonyl, loweralkylaminocarbonyl, arylloweralkylaminocarbonyl, arylaminocarbonyl, alkanoyl, arylloweralkanoyl, aroyl, alkenoyl or alkynoyl; and R.sub.2 is H, NO.sub.2, NH.sub.2, halogen, loweralkanoylamino, arylloweralkanoylamino, aroylamino or loweralkyl, or R.sub.
    Type: Grant
    Filed: February 9, 1990
    Date of Patent: August 13, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Effland, Joseph T. Klein, Kevin J. Kapples
  • Patent number: 5039811
    Abstract: There are disclosed compounds of the formula, ##STR1## wherein m, n, p, R, R.sub.1, R.sub.2 and R.sub.3 are as defined in the specification; which compounds are useful for enhancing memory and also as analgesic and antidepressant agents.
    Type: Grant
    Filed: August 23, 1990
    Date of Patent: August 13, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Effland, Joseph T. Klein, Larry Davis, Gordon E. Olsen
  • Patent number: 5037984
    Abstract: There are disclosed compounds of the formula ##STR1## where n is 0 or 1; 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: March 2, 1990
    Date of Patent: August 6, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Nicholas J. Hrib, John G. Jurcak
  • Patent number: 5037835
    Abstract: There are described compounds of the formula, ##STR1## where R is hydrogen, loweralkyl, arylloweralkyl or loweralkylcarbonyl;k is 0 or 1;m is 1, 2 or 3;k+m is 2 or 3; andn is 0 or 1;which compounds are useful as topical antiinflammatory agents for the treatment of various dermatoses.
    Type: Grant
    Filed: September 27, 1990
    Date of Patent: August 6, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Effland, Joseph T. Klein, Gordon E. Olsen, Larry Davis
  • Patent number: 5037833
    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 arylloweralkyl, 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: February 15, 1990
    Date of Patent: August 6, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Gregory M. Shutske, Kevin J. Kapples
  • Patent number: 5034403
    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, lowerallkyl 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 dermatoses.
    Type: Grant
    Filed: October 25, 1990
    Date of Patent: July 23, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Effland, Joseph T. Klein, Gordon E. Olsen, Larry Davis, Russell R. L. Hamer, Brian S. Freed
  • Patent number: 5032599
    Abstract: There are disclosed novel compounds of the formula ##STR1## where n is 0 or 1; R is hydrogen or loweralkyl; R.sub.1 is hydrogen, loweralkyl, halogen, cyano, loweralkanoyl, arylloweralkanoyl, aroyl, --CH(OH)R.sub.4, --C(OH)R.sub.4 R.sub.5 or --CH.sub.2 OR.sub.5, --CH.dbd.CR.sub.6 R.sub.7, --CH.dbd.CHCN, --CH.dbd.CHOCH.sub.3, --CH.dbd.CHCO.sub.2 C.sub.2 H.sub.5, ##STR2## R.sub.4 being hydrogen, loweralkyl, arylloweralkyl or aryl, R.sub.5 being loweralkyl, aryl or arylloweralkyl, R.sub.6 being hydrogen or loweralkyl and R.sub.7 being hydrogen, loweralkyl or aryl; R.sub.2 is hydrogen, loweralkyl, loweralkenyl, loweralkynyl, --CH.sub.2 CO.sub.2 C.sub.2 H.sub.5, arylloweralkyl, phenyl, nitrophenyl, cyanophenyl, trifluoromethylphenyl, aminophenyl, loweralkanoylaminophenyl, loweralkoxycarbonyl, arylloweralkoxycarbonyl, aryloxycarbonyl, loweralkylaminocarbonyl, arylloweralkylaminocarbonyl, arylaminocarbonyl, alkanoyl, arylloweralkanoyl, aroyl, alkenoyl, alkynoyl, --CH.sub.2 C.tbd.CCH.sub.2 --NR'R", --CH.sub.2 CH.dbd.
    Type: Grant
    Filed: September 16, 1988
    Date of Patent: July 16, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Effland, Joseph T. Klein, Kevin J. Kapples
  • Patent number: 5030639
    Abstract: There are disclosed compounds having the formula ##STR1## wherein R.sub.1 is hydrogen or loweralkyl; R.sub.2 is loweralkyl, arylloweralkyl, diarylloweralkyl or --CH.sub.2 CHOHCH.sub.2 OR.sub.5, R.sub.5 being aryl, or alternatively --NR.sub.1 R.sub.2 taken together is ##STR2## or ##STR3## R.sub.6 being aryl, arylloweralkyl, diarylloweralkyl, ##STR4## or ##STR5## and R.sub.3 and R.sub.4 are each independently methoxy or hydroxy, which compounds are useful as analgesic and hypotensive agents.
    Type: Grant
    Filed: February 4, 1991
    Date of Patent: July 9, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventor: Larry Davis
  • Patent number: 5023344
    Abstract: Novel 12-halogenated forskolin derivatives, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: May 14, 1990
    Date of Patent: June 11, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventor: Gregory M. Shutske
  • Patent number: 5015637
    Abstract: There are disclosed various compounds of the formula below, ##STR1## where X is hydrogen, halogen or loweralkyl;Y is hydrogen, halogen, loweralkyl, loweralkoxy or trifluoromethyl;R.sub.1 is hydrogen, loweralkyl, aryl, arylloweralkyl, diloweralkylaminoloweralkyl or ##STR2## R.sub.3 being hydrogen, loweralkyl or arylloweralkyl; and R.sub.2 is hydrogen, loweralkyl or arylloweralkyl;which compounds are useful as analgesic agents.
    Type: Grant
    Filed: May 25, 1990
    Date of Patent: May 14, 1991
    Assignee: Hoechst-Roussel Pharmaceutical Inc.
    Inventors: Richard C. Effland, Larry Davis