Patents Represented by Attorney, Agent or Law Firm Tatsuya Ikeda
  • Patent number: 4751223
    Abstract: There are disclosed compounds of the formula ##STR1## where X and Y are independently hydrogen, loweralkyl, trifluoromethyl or halogen; Z is --CH.sub.2 CH.sub.2 --, --CH.dbd.CH-- or --CH.sub.2 CH.sub.2 CH.sub.2 --; n is 1, 2 or 3; R.sub.1 is hydrogen, loweralkanoyl, aroyl, ethoxycarbonyl, phenoxycarbonyl, loweralkylaminocarbonyl, arylaminocarbonyl, loweralkyl or arylmethyl; R.sub.2 is hydrogen or loweralkyl; R.sub.3 is hydrogen, loweralkyl, ethoxycarbonyl, loweralkanoyl or arylloweralkyl, or R.sub.2 and R.sub.3 taken together is isopropylidene; with the proviso that when n is 3, X, Y and R.sub.1 are all hydrogen and Z is --CH.sub.2 CH.sub.2 --, R.sub.2 and R.sub.3 can not both be methyl. These compounds display antiinflammatory and analgesic activities.
    Type: Grant
    Filed: October 14, 1986
    Date of Patent: June 14, 1988
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang, Frederick J. Ehrgott, Jr.
  • Patent number: 4743601
    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: July 13, 1987
    Date of Patent: May 10, 1988
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Karl Schonafinger, Helen H. Ong
  • Patent number: 4742171
    Abstract: There is described a method of synthesizing 1,4-dihydro-benzo[c]-1,5-naphthyridin-2(3H)-ones having the formula ##STR1## where X is hydrogen, halogen, loweralkyl, loweralkoxy, trifluoromethyl or hydroxy, which method consists essentially of the aromatization and rearrangement of 1,10a-dihydropyrrolo[1,2-b]isoquinoline-3,10(2H,5H)-dione oximes of the formula below: ##STR2##
    Type: Grant
    Filed: November 4, 1986
    Date of Patent: May 3, 1988
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Lawrence L. Martin, Linda L. Setescak, Susan J. Scott
  • Patent number: 4742061
    Abstract: There are disclosed novel compounds of the formula ##STR1## where m is 1 or 2; each X is independently H, halogen, loweralkyl, loweralkoxy, --CF.sub.3, or --OH; R is H, loweralkyl, chloroloweralkyl, bromoloweralkyl, iodoloweralkyl, aminoloweralkyl, loweralkylaminoloweralkyl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, thienylloweralkyl, furylloweralkyl, loweralkanoyl, chloroloweralkanoyl, bromoloweralkanoyl, iodoloweralkanoyl, aminoloweralkanoyl, loweralkylaminoloweralkanoyl, diloweralkylaminoloweralkanoyl, aroyl, arylloweralkanoyl or diarylloweralkanoyl, thienylloweralkanoyl, furylloweralkanoyl; and R.sub.1 is .dbd.O, ##STR2## or --NR.sub.2 R.sub.3, R.sub.2 and R.sub.3 being independently H or loweralkyl, or taken together with the nitrogen atom to which they are attached constituting ##STR3## R.sub.4 in turn being H, loweralkyl, hydroxyloweralkyl, aryl, arylloweralkyl or diarylloweralkyl, with the proviso that when R.sub.1 is --NR.sub.2 R.sub.3, R is nonexistent, that when R.sub.1 is .
    Type: Grant
    Filed: June 4, 1986
    Date of Patent: May 3, 1988
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Lawrence L. Martin, Linda L. Setescak, Susan J. Scott
  • Patent number: 4734513
    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.beta.-tetra hydrolabd-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: March 31, 1986
    Date of Patent: March 29, 1988
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventor: Nicholas J. Hrib
  • Patent number: 4728651
    Abstract: There are described compounds of the formula ##STR1## where X is O or NR, R being hydrogen or loweralkyl; R.sub.1 is hydrogen; and R.sub.2 is loweralkyl, arylloweralkyl, aryloxyloweralkyl or loweralkyl substituted with ##STR2## or alternatively --NR.sub.1 R.sub.2 taken together is ##STR3## R.sub.3 being arylloweralkyl or a pharmaceutically acceptable acid addition salt thereof, which are useful as ocular or systemic antihypertensive agents.
    Type: Grant
    Filed: October 24, 1985
    Date of Patent: March 1, 1988
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Helen H. Ong, Christine M. Yasenchak
  • Patent number: 4720553
    Abstract: There is described an improved method for synthesizing N-aminophthalimide from phthalimide and hydrazine wherein the reaction is conducted in a medium consisting essentially of water and alcohol at a volume ratio within the range of from 80:20 to 20:80 at a temperature within the range of from -5.degree. C. to 35.degree. C., said alcohol being methanol, ethanol, n-propanol, iso-propanol or a mixture thereof.
    Type: Grant
    Filed: April 14, 1986
    Date of Patent: January 19, 1988
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: George E. Lee, Robert J. Heffner
  • Patent number: 4710573
    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: March 19, 1987
    Date of Patent: December 1, 1987
    Assignee: Hoechst Roussel Pharmaceuticals, Inc.
    Inventor: Joseph T. Strupczewski
  • Patent number: 4695573
    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: October 1, 1985
    Date of Patent: September 22, 1987
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Gregory M. Shutske, Frank A. Pierrat
  • Patent number: 4681879
    Abstract: There are described novel 11-substituted 5H,11H-pyrrolo[2,1-c][1,4]benzoxazepines of the general formula ##STR1## where m and n are each independently 0, 1 or 2 and m+n is 1 or 2, X and Y are each independently hydrogen, loweralkyl or halogen, and R is hydrogen, cyano, --C(NH.sub.2)NOH, ##STR2## unsubstituted loweralkyl, or substituted loweralkyl having one to three substituents each of which being independently cyano, hydroxy, cycloalkyl of 3-6 carbon atoms, furyl, thienyl, ##STR3## k being 1, 2 or 3, W being each indepentently hydrogen, halogen, hydroxy, loweralkyl, trifluoromethyl, loweralkoxy, nitro, amino, diloweralkylamino, phenoxy, or benzyloxy, and Z being hydrogen, loweralkyl or halogen, which are useful as antipsychotic and analgesic agents; novel intermediate compounds therefor; and methods of synthesizing the foregoing compounds.
    Type: Grant
    Filed: March 20, 1985
    Date of Patent: July 21, 1987
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Effland, Larry Davis, Kevin J. Kapples
  • Patent number: 4670562
    Abstract: There is disclosed novel compounds of the formula ##STR1## where X is H, halogen, loweralkyl, loweralkoxy, -CF.sub.3, or -OH; R is H, loweralkyl, arylloweralkyl, diarylloweralkyl, loweralkanoyl, arylloweralkanoyl or diarylloweralkanoyl; and R.sub.1 is H.sub.2, O or --NR.sub.2 R.sub.3, R.sub.2 and R.sub.3 being independently H or loweralkyl, or taken together with the nitrogen atom to which they are attached constitute ##STR2## R.sub.4 in turn being H, loweralkyl, hydroxyloweralkyl, aryl, arylloweralkyl or diarylloweralkyl or pharmaceutically acceptable acid addition salts thereof, which are useful for enchancing memory.
    Type: Grant
    Filed: November 4, 1986
    Date of Patent: June 2, 1987
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Lawrence L. Martin, Linda L. Setescak, Susan J. Scott
  • Patent number: 4667039
    Abstract: There are described to novel 11-substituted 5H,11H-pyrrolo[2,1-c][1,4]benzoxazepines of the general formula ##STR1## where m and n are each independently 0, 1 or 2 and m+n is 1 or 2, X and Y are each independently hydrogen, loweralkyl or halogen, and R is hydrogen, cyano, --C(NH.sub.2)NOH, ##STR2## unsubstituted loweralkyl, or substituted loweralkyl having one to three substituents each of which being independently cyano, hydroxy, cyclohexyl, furyl, thienyl, ##STR3## k being 1, 2 or 3, W being each independently hydrogen, halogen, hydroxy, loweralkyl, trifluoromethyl, loweralkoxy, nitro, amino, diloweralkylamino, phenoxy, or benzyloxy, and Z being hydrogen, loweralkyl or halogen, which are useful as antipsychotic and analgesic agents; novel intermediate compounds therefor; and methods of synthesizing the foregoing compounds.
    Type: Grant
    Filed: December 19, 1985
    Date of Patent: May 19, 1987
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Effland, Larry Davis, Kevin J. Kapples
  • Patent number: 4659112
    Abstract: There is disclosed a tamper-free identification system, such as an ID card, comprising an information-bearing substrate made of a flexible but substantially rigid material, a partial light reflector superposed over said substrate which produces a substantially nondepolarizing light reflection, and a substantially transparent 90.degree. retarder superposed over said reflector. Said identification card can be manufactured at low cost using techniques known in the art, and with the aid of a simple and inexpensive analyzer such as a linear light polarizer, fraudulent alternations of the identification card can readily be detected.
    Type: Grant
    Filed: December 3, 1984
    Date of Patent: April 21, 1987
    Assignee: Optical Devices, Incorporated
    Inventors: Daniel T. Reiner, Lawrence Bolt, Philip W. Morlan, Jr., Ali Tavasolian
  • Patent number: 4658029
    Abstract: This invention claims compounds having the formulae ##STR1## where R.sub.1 is hydrogen, loweralkyl, arylloweralkyl, aryl or heteroaryl; R.sub.2 is hydrogen or loweralkyl; R.sub.3 is loweralkyl, loweralkoxyloweralkyl, cycloalkyl, arylloweralkyl or heteroarylmethyl; R.sub.4 is hydrogen or loweralkyl; and Z is O, S, NR.sub.5 or CH.dbd.N, R.sub.5 being loweralkyl, phenylloweralkyl or benzensulfonyl. These compounds are useful as intermediates for synthesizing 6H-isoxazolo[5,4-d]pyrazolo[3,4-b]pyridines which in turn are useful as analgesic and hypotensive agents.
    Type: Grant
    Filed: August 15, 1986
    Date of Patent: April 14, 1987
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventor: Gregory M. Shutske
  • Patent number: 4652567
    Abstract: There are disclosed novel compounds of the formula ##STR1## where X is H, halogen, loweralkyl, loweralkoxy, --CF.sub.3, or --OH; R is H, loweralkyl, arylloweralkyl, diarylloweralkyl, loweralkanoyl, arylloweralkanoyl or diarylloweralkanoyl; and R.sub.1 is H.sub.2, O or --NR.sub.2 R.sub.3, R.sub.2 and R.sub.3 being independently H or loweralkyl, or taken together with the nitrogen atom to which they are attached constitute ##STR2## R.sub.4 in turn being H, loweralkyl, hydroxyloweralkyl, aryl, arylloweralkyl or diarylloweralkyl or pharmaceutically acceptable acid addition salts thereof, which are useful for enhancing memory.
    Type: Grant
    Filed: March 13, 1985
    Date of Patent: March 24, 1987
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Lawrence L. Martin, Linda L. Setescak, Susan J. Scott
  • Patent number: 4631286
    Abstract: There are disclosed compounds having the formula ##STR1## wherein X is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, nitro, NHCOR.sub.2 wherein R.sub.2 is loweralkyl, or a group of the formula NR.sub.3 R.sub.4 wherein R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl; R and R.sub.1 are independently hydrogen, loweralkyl, phenylloweralkyl, phenylloweralkyl in which the phenyl group is substituted by one or more loweralkyl, loweralkoxy, halogen, hydroxy or trifluoromethyl, diphenylloweralkyl or diphenylloweralkyl in which one or both phenyl groups are substituted by one or more loweralkyl, loweralkoxy, halogen, hydroxy or trifluoromethyl; Y is C.dbd.O or CR.sub.5 OH wherein R.sub.5 is hydrogen or loweralkyl; Z is CH.sub.2 or C.dbd.CR.sub.6 R.sub.7 wherein R.sub.6 and R.sub.7 are independently hydrogen or loweralkyl; or Y and Z taken together is CR.sub.5 .dbd.CH wherein CR.sub.
    Type: Grant
    Filed: October 25, 1984
    Date of Patent: December 23, 1986
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Gregory M. Shutske, Frank A. Pierrat
  • Patent number: 4624955
    Abstract: There are disclosed compounds having the formula ##STR1## wherein R.sub.1 is hydrogen, loweralkyl, arylloweralkyl, aryl or heteroaryl; R.sub.2 is hydrogen or loweralkyl; R.sub.3 is loweralkyl, loweralkoxyloweralkyl, cycloalkyl, arylloweralkyl or heteroarylmethyl; and R.sub.4 is hydrogen or loweralkyl; or a pharmaceutically acceptable acid addition salt thereof, which are useful as anxiolytic agents, methods for synthesizing them, and pharmaceutical compositions comprising an effective amount of such a compound.
    Type: Grant
    Filed: December 23, 1985
    Date of Patent: November 25, 1986
    Assignee: Hoechst-Roussel Pharmaceuticals
    Inventor: Gregory M. Shutske
  • Patent number: 4623657
    Abstract: There are described compounds of the formula ##STR1## where each X is independently H, halogen, loweralkyl, loweralkoxy or OH; m is 1 or 2; and R is --H, .dbd.O, ##STR2## .dbd.CH(CH.sub.2).sub.n NR.sub.1 CH.sub.3, --CH.sub.2 (CH.sub.2).sub.n NR.sub.1 R.sub.2, .dbd.N--OH, .dbd.N--OCH.sub.2 (CH.sub.2).sub.n NR.sub.1 R.sub.3, ##STR3## .dbd.N--OCH.sub.2 CHOHCH.sub.2 NR.sub.1 R.sub.3, --NR.sub.2 R.sub.3, --OH or --OCH.sub.2 (CH.sub.2).sub.n NR.sub.1 R.sub.2, n being 1 or 2, R.sub.1 being loweralkyl, R.sub.2 being H, loweralkyl, loweralkanoyl, arylloweralkyl, arylloweralkanoyl, diarylloweralkyl, diarylloweralkanoyl, --CO.sub.2 C.sub.2 H.sub.5 or --CN, and R.sub.3 being H, loweralkyl, arylloweralkyl or diarylloweralkyl, or a pharmaceutically acceptable acid addition salt thereof, which are useful as antihypertensive, anticonvulsant, analgesic and antidepressant agents.
    Type: Grant
    Filed: September 5, 1985
    Date of Patent: November 18, 1986
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Edward J. Glamkowski, Frederick J. Ehrgott, Jr.
  • Patent number: 4622326
    Abstract: There are disclosed compounds having the formula ##STR1## wherein R.sub.1 is hydrogen, loweralkyl, arylloweralkyl, aryl or heteroaryl; R.sub.2 is hydrogen or loweralkyl; R.sub.3 is loweralkyl, loweralkoxyloweralkyl, cycloalkyl, arylloweralkyl or heteroarylmethyl; and R.sub.4 is hydrogen or loweralkyl; or a pharmaceutically acceptable acid addition salt thereof, which are useful for alleviating pain and lowering blood pressure, methods for synthesizing them, and pharmaceutical compositions comprising an effective amount of such a compound.
    Type: Grant
    Filed: December 23, 1985
    Date of Patent: November 11, 1986
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventor: Gregory M. Shutske
  • Patent number: 4614272
    Abstract: There is described an article of manufacture adapted to the display of small commodities such as sunglasses in a convenient and esthetic manner. The commodity display device comprises one or more two-sided columns each of which comprising a box-like outer part comprising twin parts, an S-shaped column insert adapted to be positioned inside said box-like outer part and a column support device adapted to rotatably support said one or more columns in one or more levels and reposition said one or more columns to predetermined positions at rest. In a preferred embodiment, upper and lower vertical shafts extend from the top and bottom portions of each column, each lower vertical shaft has a V-shaped profile at the end portion thereof. In a preferred embodiment a suitable number of columns, for instance six, are arranged on the same level within the supporting device and one or more levels of columns may be provided in the column support device.
    Type: Grant
    Filed: May 3, 1984
    Date of Patent: September 30, 1986
    Assignee: Foster Grant Corporation
    Inventors: Robert N. Shelton, Gail S. Mowrer