Patents Represented by Attorney, Agent or Law Firm Tatsuya Ikeda
  • Patent number: 5013741
    Abstract: There are disclosed compounds having the formula ##STR1## wherein n is 1-4; R.sub.1 is hydrogen, alkyl, aryl, arylloweralkyl, naphthyl, furyl, thienyl, pyridinyl or pyrrolyl; X is hydrogen, loweralkyl, cycloalkyl, loweralkoxy, halogen, hydroxy nitro, trifluoromethyl, formyl, loweralkylcarbonyl, arylcarbonyl, --SH, loweralkylthio, --NHCOR.sub.2 or --NR.sub.3 R.sub.4 where R.sub.2 is hydrogen or loweralkyl, and R.sub.3 and R.sub.4 are independently hydrogen, loweralkyl or cycloalkyl; stereo, optical and geometrical isomers thereof, and pharmaceutically acceptable acid addition salts thereof, which are useful for enhancing memory and pharmaceutical compositions comprising an effective memory enhancing amount of such a compound.
    Type: Grant
    Filed: July 25, 1988
    Date of Patent: May 7, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventor: Gregory M. Shutske
  • Patent number: 5008264
    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## R.sub.6 being aryl, arylloweralkyl, diarylloweralkyl, ##STR3## 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: October 9, 1990
    Date of Patent: April 16, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventor: Larry Davis
  • Patent number: 5008407
    Abstract: A method of regioselectively and stereoselectively synthesizing forskolin (8,13-epoxy-1.alpha.,6.beta.,7.beta.,9.alpha.-tetrahydroxylabd-14-en-11-on e) from 9-deoxyforskolin (8,13-epoxy-1.alpha.,6.beta.,7.beta.-trihydroxylabd-14-en-11-one) with a good yield is described. In a preferred embodiment, it comprises an enol ether formation from 8,13-epoxy-1.alpha.,6.beta.,7.beta.-trihydroxylabd-14-en-11-one-6,7-carbon ate, oxidation of the enol ether with a suitable peroxy acid to obtain 11,12-dehydro-8,13-epoxy-11-methoxy-1.alpha.,6.beta.,7.beta.,9.alpha.-tetr ahydrolabd-14-ene-6,7-carbonate and hydrolysis of the latter under an acidic condition to obtain 8,13-epoxy-1.alpha.,6.beta.,7.beta.,9.alpha.-tetrahydroxylabd-14-en-11-one -6,7-carbonate. As an alternative way of protecting the two hydroxy groups at carbon-6 and carbon-7, they may also be converted to dimethyl acetal during the synthetic sequence. Four compounds produced in the synthetic scheme as intermediates, namely, 9,11-dehydro-8,13-epoxy-11-methoxy-1.
    Type: Grant
    Filed: November 24, 1989
    Date of Patent: April 16, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventor: Nicholas J. Hrib
  • Patent number: 5006531
    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 loweralkythio;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: July 10, 1989
    Date of Patent: April 9, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Grover C. Helsley, John J. Tegeler, Kirk D. Shoger
  • Patent number: 5002955
    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: April 13, 1989
    Date of Patent: March 26, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Gregory M. Shutske, Richard C. Effland
  • Patent number: 4999358
    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: June 26, 1989
    Date of Patent: March 12, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Lawrence L. Martin, Joseph F. Payack, Helen H. Ong
  • Patent number: 4996205
    Abstract: Pyrido[3,4-f]pyrrolo[1,2-b][1,2,5]triazepines and methods for treating depression, alleviating pain and inflammation, and enhancing memory utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: January 19, 1990
    Date of Patent: February 26, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Effland, Larry Davis, Kevin J. Kapples, Gordon E. Olsen
  • Patent number: 4992448
    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: October 24, 1989
    Date of Patent: February 12, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Effland, Joseph T. Klein, Gordon E. Olsen, Larry Davis
  • Patent number: 4983616
    Abstract: There are disclosed various compounds of the formula below, ##STR1## where X is O, S, NH, H-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: February 1, 1990
    Date of Patent: January 8, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Gerard J. O'Malley, Richard C. Allen, John I. White
  • Patent number: 4983615
    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 dermatoses.
    Type: Grant
    Filed: March 21, 1990
    Date of Patent: January 8, 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: 4980365
    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## R.sub.6 being aryl, arylloweralkyl, diarylloweralkyl, ##STR3## 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: July 13, 1987
    Date of Patent: December 25, 1990
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventor: Larry Davis
  • Patent number: 4978663
    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, R.sub.7 and R.sub.8 being independently loweralkyl or alternatively the group ##STR5## taken as a whole is ##STR6## 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: August 16, 1989
    Date of Patent: December 18, 1990
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Effland, David M. Fink
  • Patent number: 4978678
    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: August 7, 1989
    Date of Patent: December 18, 1990
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventor: Gregory M. Shutske
  • Patent number: 4970219
    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; and R.sub.1 is ##STR2## wherein R.sub.3 is hydrogen, loweralkyl or loweralkylcarbonyl; which compounds are useful as topical antiinflammatory agents for the treatment of various dermatoses.
    Type: Grant
    Filed: June 28, 1989
    Date of Patent: November 13, 1990
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Effland, Joseph T. Klein, Gordon E. Olsen, Larry Davis
  • Patent number: 4970218
    Abstract: There are disclosed compounds of the formula, ##STR1## where 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: September 11, 1989
    Date of Patent: November 13, 1990
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Effland, Joseph T. Klein, Larry Davis, Gordon E. Olsen
  • Patent number: 4959377
    Abstract: There are described compounds of the formula ##STR1## where n is 0 or 1;X is hydrogen, loweralkyl, loweralkoxy, halogen, formyl, loweralkylcarbonyl, loweralkyoxycarbonyl, loweralkoxycarbonylloweralkyl or hydroxymethyl;Y is hydrogen or halogen;andR is hydrogen, loweralkyl arylloweralkyl or loweralkylcarbonyl,which compounds are useful as topical antiinflammatory agents for the treatment of various dermatoses.
    Type: Grant
    Filed: June 29, 1989
    Date of Patent: September 25, 1990
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Effland, Joseph T. Klein, Gordon E. Olsen, Larry Davis
  • Patent number: 4959378
    Abstract: There are described compounds of the formula ##STR1## where R is hydrogen, loweralkyl, arylloweralkyl or loweralkylcarbonyl;R.sub.1 is hydrogen, loweralkyl or loweralkylcarbonyl; andn is 0 or 1;which compounds are useful as topical antiinflammatory agents for the treatment of various dermatoses.
    Type: Grant
    Filed: October 24, 1989
    Date of Patent: September 25, 1990
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Allen, Joseph T. Klein, Richard C. Effland
  • Patent number: 4942168
    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: March 7, 1988
    Date of Patent: July 17, 1990
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Karl Schonafinger, Helen H. Ong
  • Patent number: 4942237
    Abstract: There are disclosed compounds having the formula ##STR1## where X is hydrogen, loweralkyl, loweralkoxy, halogen or trifluoromethyl, andR when present is hydrogen, loweralkyl, allyl, arylloweralkyl, ##STR2## wherein R.sub.1 is loweralkyl, --CH.sub.2 C.tbd.CH, ##STR3## n being 2, 3 or 4 and R.sub.2 and R.sub.3 being independently loweralkyl, or the group ##STR4## taken as a whole constituting ##STR5## which compounds are useful as analgesic agents and also for the treatment of various memory dysfunctions characterized by a decreased cholinergic function such as Alzheimer's disease.
    Type: Grant
    Filed: February 12, 1990
    Date of Patent: July 17, 1990
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventor: Gregory M. Shutske
  • Patent number: 4937341
    Abstract: There are disclosed various derivatives of physostigmine and related compounds of the formula below, ##STR1## where X, R.sub.1, R.sub.2 and R.sub.3 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: November 24, 1989
    Date of Patent: June 26, 1990
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventor: Edward J. Glamkowski