Patents Represented by Attorney, Agent or Law Firm Tatsuya Ikeda
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Patent number: 4751223Abstract: 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: GrantFiled: October 14, 1986Date of Patent: June 14, 1988Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang, Frederick J. Ehrgott, Jr.
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Patent number: 4743601Abstract: 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: GrantFiled: July 13, 1987Date of Patent: May 10, 1988Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Karl Schonafinger, Helen H. Ong
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Patent number: 4742171Abstract: 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: GrantFiled: November 4, 1986Date of Patent: May 3, 1988Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Lawrence L. Martin, Linda L. Setescak, Susan J. Scott
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Patent number: 4742061Abstract: 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: GrantFiled: June 4, 1986Date of Patent: May 3, 1988Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Lawrence L. Martin, Linda L. Setescak, Susan J. Scott
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Patent number: 4734513Abstract: 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: GrantFiled: March 31, 1986Date of Patent: March 29, 1988Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventor: Nicholas J. Hrib
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Patent number: 4728651Abstract: 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: GrantFiled: October 24, 1985Date of Patent: March 1, 1988Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Helen H. Ong, Christine M. Yasenchak
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Patent number: 4720553Abstract: 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: GrantFiled: April 14, 1986Date of Patent: January 19, 1988Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: George E. Lee, Robert J. Heffner
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Patent number: 4710573Abstract: 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: GrantFiled: March 19, 1987Date of Patent: December 1, 1987Assignee: Hoechst Roussel Pharmaceuticals, Inc.Inventor: Joseph T. Strupczewski
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Patent number: 4695573Abstract: 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: GrantFiled: October 1, 1985Date of Patent: September 22, 1987Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Gregory M. Shutske, Frank A. Pierrat
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Patent number: 4681879Abstract: 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: GrantFiled: March 20, 1985Date of Patent: July 21, 1987Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Richard C. Effland, Larry Davis, Kevin J. Kapples
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Patent number: 4670562Abstract: 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: GrantFiled: November 4, 1986Date of Patent: June 2, 1987Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Lawrence L. Martin, Linda L. Setescak, Susan J. Scott
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Patent number: 4667039Abstract: 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: GrantFiled: December 19, 1985Date of Patent: May 19, 1987Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Richard C. Effland, Larry Davis, Kevin J. Kapples
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Patent number: 4659112Abstract: 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: GrantFiled: December 3, 1984Date of Patent: April 21, 1987Assignee: Optical Devices, IncorporatedInventors: Daniel T. Reiner, Lawrence Bolt, Philip W. Morlan, Jr., Ali Tavasolian
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Patent number: 4658029Abstract: 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: GrantFiled: August 15, 1986Date of Patent: April 14, 1987Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventor: Gregory M. Shutske
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Patent number: 4652567Abstract: 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: GrantFiled: March 13, 1985Date of Patent: March 24, 1987Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Lawrence L. Martin, Linda L. Setescak, Susan J. Scott
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Patent number: 4631286Abstract: 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: GrantFiled: October 25, 1984Date of Patent: December 23, 1986Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Gregory M. Shutske, Frank A. Pierrat
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Patent number: 4624955Abstract: 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: GrantFiled: December 23, 1985Date of Patent: November 25, 1986Assignee: Hoechst-Roussel PharmaceuticalsInventor: Gregory M. Shutske
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Patent number: 4623657Abstract: 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: GrantFiled: September 5, 1985Date of Patent: November 18, 1986Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Edward J. Glamkowski, Frederick J. Ehrgott, Jr.
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Patent number: 4622326Abstract: 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: GrantFiled: December 23, 1985Date of Patent: November 11, 1986Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventor: Gregory M. Shutske
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Patent number: 4614272Abstract: 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: GrantFiled: May 3, 1984Date of Patent: September 30, 1986Assignee: Foster Grant CorporationInventors: Robert N. Shelton, Gail S. Mowrer