Patents Represented by Attorney, Agent or Law Firm Tatsuya Ikeda
  • Patent number: 4880818
    Abstract: There are disclosed compounds of the formula ##STR1## where X,Y are each independently hydrogen, loweralkyl, loweralkoxy, hydroxy, halogen, trifluoromethyl or nitro; R.sub.1 is hydrogen or loweralkyl; R.sub.2 ' is hydrogen or loweralkyl and R.sub.4 is hydrogen, loweralkyl or aryl, which are useful as hypotensive agents and as intermediates.
    Type: Grant
    Filed: July 12, 1988
    Date of Patent: November 14, 1989
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Karl Schonafinger, Helen Hu Ong
  • Patent number: 4879382
    Abstract: Pyrido[3,4-f]pyrrolo[1,2-b][1,2]triazepines and methods for treating depression, alleviating pain and inflammation, and enhancing memory utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: July 25, 1988
    Date of Patent: November 7, 1989
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Richard C. Effland, Larry Davis, Kevin J. Kapples, Gordon E. Olsen
  • Patent number: 4873239
    Abstract: There are described compounds of the formula ##STR1## where n is 0, 1 or 2; X and Y are independently hydrogen, loweralkyl, loweralkoxy, arylloweralkyl, aryloxy, halogen, --CF.sub.3, --NO.sub.2, --OH, --OCOR.sub.1, ##STR2## where R.sub.1 is loweralkyl, arylloweralkyl, aryl or loweralkoxy, R.sub.2 is hydrogen, loweralkyl or loweralkylcarbonyl, R.sub.3 is hydrogen or loweralkyl, or the group --NR.sub.2 R.sub.3 as a whole is ##STR3## m is 0, 1 or 2, and R.sub.4 is hydrogen, loweralkyl or aryl; and Z is (R.sub.5,R.sub.6), ##STR4## where R.sub.5 and R.sub.6 are each independently hydrogen or loweralkyl, R.sub.7 is loweralkyl, R.sub.8 is hydrogen, loweralkyl or aryl, R.sub.9 and R.sub.10 are each independently loweralkyl or the group --NR.sub.9 R.sub.10 as a whole is ##STR5## R.sub.12 being hydrogen, loweralkyl or aryl, and R.sub.11 is hydrogen, loweralkyl or aryl; which are useful for the treatment of glaucoma.
    Type: Grant
    Filed: May 3, 1988
    Date of Patent: October 10, 1989
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: John J. Tegeler, Kirk D. Shoger
  • Patent number: 4871764
    Abstract: Novel 12-halogenated forskolin derivatives, intermediates and processes for their preparation, and methods for reducing intraocular pressure utilizing the compounds or compositions are disclosed.
    Type: Grant
    Filed: November 20, 1986
    Date of Patent: October 3, 1989
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventor: Gregory M. Shutske
  • Patent number: 4868190
    Abstract: There are described compounds of the formula: ##STR1## where, X is hydrogen, loweralkyl, loweralkoxy or halogen;Y is hydrogen, loweralkyl or halogen;Z is hydrogen, loweralkyl or halogen;R is hydrogen, loweralkyl, loweralkenyl, loweralkylcarbonyl, dimethylaminoloweralkyl or ##STR2## m being an integer of 1 to 6, with the proviso that when R is loweralkenyl the double bond is not alpha to the nitrogen atom;which compounds are useful analgesic, anticonvulsant and antidepressant agents, and for treating various memory dysfunctions characterized by decreased cholinergic function such as Alzheimer's disease.
    Type: Grant
    Filed: December 27, 1988
    Date of Patent: September 19, 1989
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Richard C. Effland, Joseph T. Klein, Larry Davis, Gordon E. Olsen
  • Patent number: 4868177
    Abstract: There are disclosed compounds having the formula ##STR1## where n is 1, 2 or 3;X is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, nitro or trifluoromethylR.sub.1 and R.sub.2 are each independently hydrogen, lower alkyl or arylloweralkyl, but both may not be arylloweralkyl simultaneously;R.sub.3 and R.sub.4 are each independently hydrogen, lower alkyl, arylloweralkyl, formyl or lower alkylcarbonyl, or alternatively the group --NR.sub.3 R.sub.4 taken as a whole constitutes ##STR2## stereo isomers thereof and pharmaceutically acceptable acid addition salts thereof, which are useful for the treatment of various memory dysfunctions characterized by decreased cholinergic function, such as Alzheimer's disease.
    Type: Grant
    Filed: November 29, 1988
    Date of Patent: September 19, 1989
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Gregory M. Shutske, Kevin J. Kapples
  • Patent number: 4868188
    Abstract: Novel 4-(benzisothiazol-3-yl)phenoxyacetic acid 1',1'-dioxides of the formula ##STR1## where X is hydrogen, halogen or loweralkyl; R.sub.1 is hydrogen or loweralkyl; R.sub.2 and R.sub.3 are each independently Cl, Br or CH.sub.3, and related compounds, methods for preparing same and methods of treatment by administering compositions containing such a compound are described. These compounds are useful as diuretics.
    Type: Grant
    Filed: November 3, 1982
    Date of Patent: September 19, 1989
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventor: Gregory M. Shutske
  • Patent number: 4865764
    Abstract: There are disclosed compounds of the formula, ##STR1## where X and Y are each independently hydrogen, loweralkyl, halogen or trifluoromethyl; Z is hydrogen or 2- or 3-Cl, Br, I, CHO or CH.dbd.CR.sub.1 R.sub.2 where R.sub.1 and R.sub.2 are each independently hydrogen or loweralkyl; R is hydrogen, ##STR2## where n is 1, 2 or 3, R.sub.3 is loweralkyl, and R.sub.4 is hydrogen or loweralkyl, or alternatively the group --NR.sub.3 R.sub.4 as a whole is ##STR3## where R.sub.6 is loweralkyl, ##STR4## and R.sub.7 is loweralkyl or ##STR5## R.sub.8 being hydrogen, loweralkyl, halogen, trifluoromethyl or methoxy; and R.sub.5 is hydrogen, loweralkyl or arylloweralkyl.
    Type: Grant
    Filed: October 11, 1988
    Date of Patent: September 12, 1989
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Richard C. Effland, Kevin J. Kapples
  • Patent number: 4855479
    Abstract: There are disclosed compounds having the formula ##STR1## wherein m is 1 or 2; n is 1 or 2; p is 1-5; 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; R is hydrogen, loweralkyl or loweralkylcarbonyl; and R.sub.1 is hydrogen, loweralkyl, loweralkylcarbonyl, aryl, diloweralkylaminolowralkyl, arylloweralkyl, diarylloweralkyl, oxygen-bridged arylloweralkyl or oxygen-bridged diarylloweralkyl; stereo, optical and geometrical isomers thereof, and pharmaceutically acceptable acid addition salts thereof, which are useful for enhancing memory.
    Type: Grant
    Filed: November 21, 1988
    Date of Patent: August 8, 1989
    Inventor: Gregory M. Shutske
  • Patent number: 4853470
    Abstract: Novel 3-(piperidinyl)- and 3-(pyrrolidinyl)-1H-indazoles, intermediates and processes for the preparation thereof, and methods for treating psychoses, treating depression, alleviating pain, treating convulsions and treating hypertension utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: December 23, 1988
    Date of Patent: August 1, 1989
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventor: Joseph T. Strupczewski
  • Patent number: 4847414
    Abstract: 2'-substituted-spiro[benzofuran-2(3H),1'-cyclohexanes] and methods of preparing same are described. On the aromatic portion of the benzofuran ring, there may be a substituent or substituents including halogen, amino, lower-alkyl-substituted amino, lower alkyl, lower alkoxy, hydroxy and nitro. The substituents at the 2-position of the cyclohexane ring are --(CH.sub.2).sub.n NR.sup.1 R.sup.2 where n is 0, 1 or 2 and R.sup.1 and R.sup.2 are each independently hydrogen and alkyl of 1-3 carbons. These compounds are useful as antidepressants and analgesics.Various other compounds which are useful as intermediates for preparing the aforementioned compounds and methods for preparing same are also described.
    Type: Grant
    Filed: March 2, 1983
    Date of Patent: July 11, 1989
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Edward J. Glamkowski, Michael C. Jones
  • Patent number: 4843079
    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-bridge 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.6 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 4, 1988
    Date of Patent: June 27, 1989
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Gregory M. Shutske, Richard C. Effland
  • Patent number: 4840972
    Abstract: There are described compounds of the formula ##STR1## where X is hydrogen, halogen, loweralkyl, loweralkoxy or trifluoromethyl; R is ##STR2## R.sub.4 being loweralkyl; R.sub.1 is hydrogen, loweralkyl or arylloweralkyl; R.sub.2 is hydrogen, loweralkyl or arylloweralkyl; and R.sub.3 is loweralkyl, with the proviso that when R is acetyl, R.sub.3 is methyl and X is hydrogen, R.sub.1 and R.sub.2 are not both hydrogen, or pharmaceutically acceptable acid addition salts thereof, which are useful for enhancing memory and for treating Alzheimer's disease.
    Type: Grant
    Filed: November 14, 1988
    Date of Patent: June 20, 1989
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Richard C. Effland, Joseph T. Effland
  • Patent number: 4840947
    Abstract: There are disclosed compounds of the formula ##STR1## where X and Y are independently hydrogen, loweralkyl, halogen or trifluoromethyl; Z is --CH.sub.2 CH.sub.2 --, --CH.dbd.CH-- or --CH.sub.2 CH.sub.2 CH.sub.2 --; R is ##STR2## R.sub.2 being hydrogen, loweralkyl, ethoxycarbonyl, 2,2,2-trichloroethoxycarbonyl or phenoxycarbonyl; and R.sub.1 is hydrogen, loweralkanoyl, loweralkyl, ethoxycarbonyl, 2,2,2-trichloroethoxycarbonyl or phenoxycarbonyl; the dotted line within the seven-membered ring and the dotted line between R.sub.1 and the ring nitrogen being optional bonds such that the former is absent and the latter present when R is ##STR3## whereas the former is present and the latter absent when R is ##STR4## These compounds display antiinflammatory activities and analgesic activities.
    Type: Grant
    Filed: October 14, 1986
    Date of Patent: June 20, 1989
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang, Frederick J. Ehrgott, Jr.
  • Patent number: 4839364
    Abstract: There are disclosed compounds having the formula ##STR1## wherein n is 1, 2 or 3; X is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, NHCOR.sub.2 where R.sub.2 is loweralkyl, or NR.sub.3 R.sub.4 where R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl; R is hydrogen or loweralkyl; R.sub.1 is hydrogen, loweralkyl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, furylloweralkyl, thienylloweralkyl, oxygen-bridged arylloweralkyl, oxygen-bridged diarylloweralkyl, oxygen-bridged furylloweralkyl or oxygen-bridged thienylloweralkyl; Y is C.dbd.O or CR.sub.5 OH where R.sub.5 is hydrogen or loweralkyl; Z is CH.sub.2 or C.dbd.CR.sub.6 R.sub.7 where R.sub.6 and R.sub.7 are independently hydrogen or loweralkyl; or Y and Z taken together is CR.sub.5 .dbd.Ch where CR.sub.
    Type: Grant
    Filed: January 28, 1987
    Date of Patent: June 13, 1989
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Gregory M. Shutske, Frank A. Pierrat
  • Patent number: 4835275
    Abstract: There are disclosed compounds having the formula ##STR1## wherein n is 1, 2 or 3; X is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, NHCOR.sub.2 where R.sub.2 is loweralkyl, or NR.sub.3 R.sub.4 where R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl; R is hydrogen or loweralkyl; R.sub.1 is hydrogen, loweralkyl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, furylloweralkyl, thienylloweralkyl, oxygen-bridged arylloweralkyl, oxygen-bridged diarylloweralkyl, oxygen-bridged furylloweralkyl or oxygen-bridged thienylloweralkyl; Y is C.dbd.O or CR.sub.5 OH where R.sub.5 is hydrogen or loweralkyl; Z is CH.sub.2 or C.dbd.CR.sub.6 R.sub.7 where R.sub.6 and R.sub.7 are independently hydrogen or loweralkyl; or Y and Z taken together is CR.sub.5 .dbd.CH where CR.sub.
    Type: Grant
    Filed: November 25, 1987
    Date of Patent: May 30, 1989
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Gregory M. Shutske, Frank A. Pierrat
  • Patent number: 4833139
    Abstract: There are disclosed compounds of the formula ##STR1## where R.sub.1 is loweralkoxycarbonyl, --CH.sub.2 OH or --CONR.sub.3 R.sub.4, R.sub.3 and R.sub.4 being independently hydrogen, loweralkyl or arylloweralkyl; and R.sub.2 is --CH.sub.2 CH.dbd.CH.sub.2, ##STR2## R.sub.5 and R.sub.6 being independently loweralkyl or alternatively the group -NR.sub.5 R.sub.6 as a whole being ##STR3## R.sub.7 being hydrogen, loweralkyl or arylloweralkyl; which are useful for enhancing cholinergic activity in mammals and hence for the treatment of various memory dysfunctions characterized by decreased cholinergic function such as Alzheimer's disease.
    Type: Grant
    Filed: July 5, 1988
    Date of Patent: May 23, 1989
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventor: Lawrence L. Martin
  • Patent number: 4826846
    Abstract: There are disclosed compounds of the formula ##STR1## wherein the group A is ##STR2## where R.sub.1 and R.sub.2 are each independently or loweralkyl, or R.sub.1 +R.sub.2 =(CH.sub.2).sub.m, m being 2 to 6, p is 1 or 2, and each X is independently hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, nitro, amino, loweralkylamino, diloweralkylamino, trifluoromethyl or loweralkylthio; W is O, H.sub.2 or [H, OH]; n is 2, 3 or 4; and R.sub.3 is ##STR3## where q is 1 or 2 and each Y is independently hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, nitro, amino, loweralkylamino, diloweralkylamino, triflouromethyl or loweralkylthio, which are useful as antipsychotic, anxiolytic and analgesic agents.
    Type: Grant
    Filed: July 18, 1988
    Date of Patent: May 2, 1989
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Nicholas J. Hrib, John G. Jurcak
  • Patent number: 4822896
    Abstract: A method of regioselectively and stereoselectively synthesizing forskolin (8,13-epoxy-1.alpha.,6.beta.,7.beta.,9.alpha.-tetrahydroxy-labd-14-en-11-o ne) 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: January 25, 1988
    Date of Patent: April 18, 1989
    Assignee: Hoechst Roussel Pharmaceuticals, Inc.
    Inventor: Nicholas J. Hrib
  • Patent number: 4820826
    Abstract: A method of regioselectively and stereoselectively synthesizing forskolin (8,13-epoxy-1.alpha., 6.beta., 7.beta., 9.alpha.-tetrahydroxylabd-14-en-11-one) 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-carbonate, 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.-tetrahydrolabd-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.
    Type: Grant
    Filed: January 25, 1988
    Date of Patent: April 11, 1989
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventor: Nicholas J. Hrib