Patents Represented by Attorney, Agent or Law Firm Tatsuya Ikeda
  • Fused heteroalkylene quinolinamines
    Patent number: 5208330
    Abstract: 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: Grant
    Filed: February 25, 1992
    Date of Patent: May 4, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Gregory M. Shutske, Richard C. Effland
  • Fused heteroalkylene quinolinamines
    Patent number: 5206387
    Abstract: 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: Grant
    Filed: October 19, 1992
    Date of Patent: April 27, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Gregory M. Shutske, Richard C. Effland
  • 5-(1-hydroxylcycloalkyl)-2-methoxy pyridine compounds
    Patent number: 5204480
    Abstract: There are described compounds of the formula ##STR1## where n is 1, 2 or 3;R.sub.1 is hydrogen, formyl, loweralkylcarbonyl, arylloweralkylcarbonyl, loweralkyl, arylloweralkyl, ##STR2## R.sub.5 and R.sub.6 being independently loweralkyl or alternatively the group ##STR3## taken as a whole is ##STR4## R.sub.2 is hydrogen, loweralkyl, loweralkenyl, arylloweralkyl, --CH.sub.2 C.tbd.CH, ##STR5## R.sub.7 and R.sub.8 being independently loweralkyl or alternatively the group ##STR6## taken as a whole is ##STR7## R.sub.3 is hydrogen is loweralkyl; and R.sub.4 is hydrogen or loweralkyl;which compounds are useful as analgesic agents and also for treating various memory dysfunctions.
    Type: Grant
    Filed: February 21, 1992
    Date of Patent: April 20, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Effland, David M. Fink
  • Substituted 3-amino-2,3,4,5-tetrahydro-1-aryloxy-3-benzazepines
    Patent number: 5202319
    Abstract: There are disclosed various compounds of the formula below, ##STR1## where n is 1 or 2;m is 1 or 2;each X is independently hydrogen or loweralkoxy;Y is hydrogen, halogen or trifluoromethyl;R.sub.1 is hydrogen, loweralkyl, arylloweralkyl, heteroarylloweralkyl, pyridinyl, loweralkylcarbonyl, arylloweralkylcarbonyl, heteroarylloweralkylcarbonyl, trifluoromethylcarbonyl or arylcarbonyl; andR.sub.2 is hydrogen, loweralkyl, loweralkoxycarbonyl, aminoloweralkylcarbonyl, loweralkylaminoloweralkylcarbonyl or diloweralkylaminoloweralkylcarbonyl;which are useful as modulators of neurotransmitter function such as serotonergic and adrenergic, and as such are useful as antidepressants and for the treatment of personality disorders such as obsessive compulsive disorders.
    Type: Grant
    Filed: September 23, 1991
    Date of Patent: April 13, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Effland, Joseph T. Klein
  • N-(pyrrol-1-yl)pyridinamines
    Patent number: 5194618
    Abstract: There are disclosed compounds of the formula ##STR1## where n is 0 or 1; R is hydrogen or loweralkyl; R.sub.1 is hydrogen, loweralkyl, halogen, --CH(OH)R.sub.4, --C(OH)R.sub.4 R.sub.5 or --CH.sub.2 OR.sub.5, 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=CHCH.sub.2 --NR'R" or --CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 --NR'R", R' and R" being independently loweralkyl or --NR'R" taken as a whole being ##STR2## and R.sub.
    Type: Grant
    Filed: May 23, 1991
    Date of Patent: March 16, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Effland, Joseph T. Klein, Kevin J. Kapples
  • Substituted 1,2,3,4-tetrahydrocyclopent[b]indoles, 1,2,3,3a,4,8a-hexahydrocyclopent[b]indoles and related compounds
    Patent number: 5192789
    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.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: Grant
    Filed: January 9, 1992
    Date of Patent: March 9, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Helen H. Ong, Gerard J. O'Malley, Michael C. Merriman, Mark G. Palermo
  • Memory enhancing and analgesic 1,2,3a,8,8a-hexahydro-3a,8(and 1,3a,8)-di(and tri)methylpyrrolo[2,3-b]indoles
    Patent number: 5187165
    Abstract: There are disclosed various derivatives of eseroline and related compounds of the formula below ##STR1## where R,R.sub.1, X,Z and m are as defined in the specification, which compounds being useful for enhancing cholinergic function, as antidepressant agents and as analgesic agents.
    Type: Grant
    Filed: September 22, 1988
    Date of Patent: February 16, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Russell R. L. Hamer, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Brian S. Freed, Barbara E. Kurys
  • Dihydro-4(hydroxyalkyeneamino)quinolines
    Patent number: 5182275
    Abstract: 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: Grant
    Filed: May 10, 1990
    Date of Patent: January 26, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Karl Schonafinger, Helen H. Ong
  • 4,5-dihydropyrazolo[3,4-a]acridines
    Patent number: 5179100
    Abstract: There are disclosed various compounds of the formula below, ##STR1## where the parameters R.sub.1, R.sub.2 and R.sub.3 are as defined in the specification, which compounds are useful as analgesic agents.
    Type: Grant
    Filed: March 9, 1992
    Date of Patent: January 12, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals inc.
    Inventors: Gregory M. Shutske, John D. Tomer, IV
  • Substituted 3-(pyridinylamino)-indoles
    Patent number: 5177088
    Abstract: 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: Grant
    Filed: April 17, 1991
    Date of Patent: January 5, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Richard C. Effland, Joseph T. Klein, Lawrence L. Martin
  • Memory enhancing and analgesic aminocarbonylcarbamates related to physostigmine
    Patent number: 5177101
    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: August 23, 1991
    Date of Patent: January 5, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Edward J. Glamkowski, Yulin Chiang, Russell R. L. Hamer
  • 2-(aminoaryl) indoles and indolines as topical antiinflammatory agents for the treatment of skin disorders
    Patent number: 5166170
    Abstract: 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: Grant
    Filed: July 3, 1989
    Date of Patent: November 24, 1992
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: John J. Tegeler, Eileen M. Gardenhire, Grover C. Helsley
  • Carbamate derivatives of 4-amino-3-isoxazolidinones, 3-amino-1-hydroxypyrrolidin-2-ones and 1-amino-1-cyclopropanecarboxylic acid analogs
    Patent number: 5153193
    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: October 1, 1991
    Date of Patent: October 6, 1992
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Denise M. Flanagan, Lawrence L. Martin
  • Process for (1,2,3,4-tetrahydro-9-acridinimino)cyclohexane carboxylic acid and related compounds
    Patent number: 5149813
    Abstract: There are described compounds of the formula, ##STR1## where X is hydrogen, loweralkyl, loweralkoxy or halogen;R when present is hydrogen, loweralkyl or arylloweralkyl;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: March 27, 1992
    Date of Patent: September 22, 1992
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Lawrence L. Martin, Joseph F. Payack, Helen H. Ong
  • 3-(4-substituted-4-piperazinyl)butyl-4-thiazolidinone and related compounds
    Patent number: 5136037
    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, lower alkyl, ##STR3## 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: June 7, 1991
    Date of Patent: August 4, 1992
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Nicholas J. Hrib, John G. Jurcak
  • (1,2,3,4-Tetrahydro-9-acridinimino)cyclohexane carboxylic acid and related compounds
    Patent number: 5126449
    Abstract: There are described compounds of the formula, ##STR1## where X is hydrogen, loweralkyl, loweralkoxy or halogen;R when present is hydrogen, loweralkyl or arylloweralkyl;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: November 5, 1991
    Date of Patent: June 30, 1992
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Lawrence L. Martin, Joseph F. Payack, Helen H. Ong
  • 5-(1-aminocyclohexyl)-2(1H)-pyridinone and related compounds
    Patent number: 5112981
    Abstract: There are described compounds of the formula ##STR1## where n is 1, 2 or 3;R.sub.1 is hydrogen, formyl, loweralkylcarbonyl, arylloweralkylcarbonyl, loweralkyl, arylloweralkyl, ##STR2## R.sub.5 and R.sub.6 being independently loweralkyl or alternatively the group ##STR3## taken as a whole is ##STR4## R.sub.2 is hydrogen, loweralkyl, loweralkenyl, arylloweralkyl, --CH.sub.2 C.tbd.CH, ##STR5## R.sub.7 and R.sub.8 being independently loweralkyl or alternatively the group ##STR6## taken as a whole is ##STR7## R.sub.3 is hydrogen or loweralkyl; and R.sub.4 is hydrogen or loweralkyl;which compounds are useful as analgesic agents and also for treating various memory dysfunctions.
    Type: Grant
    Filed: June 5, 1991
    Date of Patent: May 12, 1992
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Effland, David M. Fink
  • Fused heteroalkylene quinolinamines
    Patent number: 5112830
    Abstract: 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: Grant
    Filed: January 10, 1991
    Date of Patent: May 12, 1992
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Gregory M. Shutske, Richard C. Effland
  • [(Arylalkylpiperidin-4-yl)methyl]-2a,3,4,5-tetrahydro- 1(2H)-acenaphthylen-1-ones and related compounds
    Patent number: 5106856
    Abstract: There are disclosed various compounds of the formula below, ##STR1## where X is hydrogen, loweralkyl, loweralkoxy, hydroxy or nitro;Y is hydrogen or loweralkoxy; or alternatively, X and Y combined together form the group --OCH.sub.2 O-- in which case the positions of X and Y on the benzene ring moiety must be adjacent to each other;and Z is hydrogen, loweralkyl, loweralkoxy, hydroxy, halogen or nitro;which compounds are useful for alleviating various memory dysfunctions characterized by a cholinergic deficit such as Alzheimer's disease.
    Type: Grant
    Filed: June 7, 1991
    Date of Patent: April 21, 1992
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Raymond W. Kosley, Jr., Bettina Spahl
  • 1-(substituted pyridinylamino)-1H-indol-5-yl substituted carbamates
    Patent number: 5102891
    Abstract: There are disclosed various compounds of the formula below, ##STR1## where n is 0 or 1;X is hydrogen, halogen, nitro, amino, trifluoromethyl, loweralkyl, or loweralkoxy;Y is hydrogen, halogen, nitro, amino, trifluoromethyl, loweralkyl, or loweralkoxy;R.sub.1 is hydrogen, loweralkyl, arylloweralkyl, loweralkenyl, loweralkynyl, loweralkanoyl, arylloweralkanoyl, heteroarylloweralkyl or heteroarylloweralkanoyl;R.sub.2 is hydrogen, loweralkyl, formyl or cyano;R.sub.3 is hydrogen or loweralkyl;R.sub.4 is loweralkyl, arylloweralkyl, cycloalkyl, aryl or heteroaryl; or alternatively, --NR.sub.3 R.sub.4 taken together constitutes ##STR2## R.sub.5 being hydrogen, loweralkyl, aryl, arylloweralkyl, heteroaryl or heteroarylloweralkyl,which compounds are useful for the treatment of various memory dysfunctions characterized by a cholinergic deficit such as Alzheimer's disease.
    Type: Grant
    Filed: July 23, 1990
    Date of Patent: April 7, 1992
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Effland, Larry Davis, Gordon E. Olsen, Joseph T. Klein, David G. Wettlaufer, Peter A. Nemoto