Patents Represented by Attorney, Agent or Law Firm Tatsuya Ikeda
  • Patent number: 4608374
    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: November 7, 1983
    Date of Patent: August 26, 1986
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Effland, Larry Davis, Kevin J. Kapples
  • Patent number: 4602035
    Abstract: There are described compounds of the formula ##STR1## where n is 2 or 3, X and Y are each independently hydrogen, loweralkyl, or halogen, and R.sub.1 and R.sub.2 are each independently hydrogen, loweralkyl, cyano, beta,beta,beta-trichloroethyoxycarbonyl, cyclopropylmethyl, phenethyl, or cyanoethyl, but at least one of the two is loweralkyl, which are useful as antidepressant and analgesic agents; novel intermediate compounds for preparing said compounds; and methods for synthesizing the foregoing compounds.
    Type: Grant
    Filed: December 7, 1983
    Date of Patent: July 22, 1986
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: John J. Tegeler, Craig J. Diamond, Grover C. Helsley
  • Patent number: 4588727
    Abstract: There are described novel pyrrolo[1,2-b][1,2,5]triazepines of the general formula ##STR1## where R is hydrogen, loweralkyl, loweralkylaminoloweralkyl or diloweralkylaminoloweralkyl; X is hydrogen, halogen (fluorine, chlorine, bromine or iodine), trifluoromethyl or nitro; and Y is hydrogen, halogen or loweralkyl. Also described are derivatives of 1-amino-2-benzoylpyrrole having the general formula ##STR2## where R, X and Y are as defined above, and R.sub.1 is hydrogen, ##STR3##Compounds I and II are useful as analgesic, anxiolytic and/or anticonvulsant agents, and many of Compounds II are useful as intermediates for synthesizing Compounds I.
    Type: Grant
    Filed: February 4, 1985
    Date of Patent: May 13, 1986
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Effland, Joseph T. Klein, R. Richard L. Hamer
  • Patent number: 4585779
    Abstract: cis-4a-Aryl-1,2,3,4,4a,9b-hexahydro-benzofuro[3,2-c]pyridines and methods of preparing same are described. On the nitrogen atom there may be a substituent including loweralkyl, loweralkenyl, phenylloweralkyl, hydrogen cyanoloweralkyl, phenylcarbonylloweralkyl, phenoxyloweralkyl and cycloalkylloweralkyl. The 4a-aryl group may be a phenyl, mono-halogen substituted phenyl, tolyl, methoxyphenyl, hydroxyphenyl, or furyl. These compounds are useful as analgesic and anticonvulsant agents.3-o-Fluorophenyl-1-methyl-4-aryl-4-piperidinols which are useful as intermediates for preparing the aforementioned compounds and methods for preparing same are also described.
    Type: Grant
    Filed: December 21, 1984
    Date of Patent: April 29, 1986
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventor: Solomon S. Klioze
  • Patent number: 4562186
    Abstract: There are disclosed novel compounds having the formula ##STR1## where X is hydrogen, halogen (F, Cl, Br or I), loweralkyl or loweralkoxy; and R is --CH, --CONH.sub.2, --COOCH(CH.sub.3).sub.2, --COOH, --COO(CH.sub.2).sub.4 Cl, ##STR2## R.sub.1 and R.sub.2 being independently hydrogen or lower alkyl and R.sub.3 being ##STR3## an optical antipode thereof or a pharmaceutically acceptable acid addition salt thereof, which are useful as antihypertensive, analgesic and antiinflammatory agents, methods for synthesizing them, and pharmaceutical compositions comprising an effective amount of such a compound.
    Type: Grant
    Filed: January 22, 1985
    Date of Patent: December 31, 1985
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: John J. Tegeler, Craig J. Diamond
  • Patent number: 4562187
    Abstract: There are disclosed novel compounds having the formula ##STR1## where each X is independently hydrogen, halogen (F, Cl, Br or I), loweralkyl or loweralkoxy; m is 1 or 2; R' is hydrogen or loweralkyl; and R is ##STR2## n being 1, 2 or 3, each of R.sub.1 and R.sub.2 being independently hydrogen or loweralkyl and R.sub.3 being ##STR3## an optical antipode thereof or a pharmaceutically acceptable acid addition salt thereof, which are useful as antihypertensive, analgesic and antiinflammatory agents, methods for synthesizing them, and pharmaceutical compositions comprising an effective amount of such a compound.
    Type: Grant
    Filed: January 22, 1985
    Date of Patent: December 31, 1985
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: John J. Tegeler, Craig J. Diamond
  • Patent number: 4544745
    Abstract: Cis-4a-aryl, 1, 2, 3, 4, 4A, 9B-hexahydro-benzofuro-[3,2-C]- pyridines, useful as analgesic and anticonvulsant agents are described.
    Type: Grant
    Filed: December 21, 1984
    Date of Patent: October 1, 1985
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventor: Solomon S. Klioze
  • Patent number: 4528292
    Abstract: There are described novel antihypertensive 1,2-benzisothiazole piperidines of the formula ##STR1## where X is hydrogen, halogen, loweralkoxy, loweralkyl, nitro, amino or trifluoromethyl; and R is ##STR2## R.sub.1 being loweralkyl, aryl, aralkyl, cycloalkylloweralkyl or a loweralkyl substituted with an amino, loweralkylamino or diloweralkylamino, and R.sub.2 being hydrogen, loweralkyl or aryl; antihypertensive compositions comprising said compounds or pharmaceutically acceptable acid addition salts thereof; and methods for synthesizing the same.
    Type: Grant
    Filed: April 23, 1984
    Date of Patent: July 9, 1985
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventor: Joseph T. Strupczewski
  • Patent number: 4521214
    Abstract: There is described a process for producing, in a continuous manner, a gradient dyeing across the width of a long strip of a plastic sheet and an apparatus used therefor. In a preferred embodiment of the invention, the orientation of the plastic strip is maintained substantially constant during the passage through a dye bath, and the dye liquid level is repetitively varied by use of a liquid level control means. This invention is particularly useful for making gradient-dyed plastic sheets which in turn are used for making sunglass lenses.
    Type: Grant
    Filed: January 9, 1984
    Date of Patent: June 4, 1985
    Assignee: American Hoechst Corporation
    Inventor: Robert Weis
  • Patent number: 4518713
    Abstract: There are described analgesic substituted-1-aminoalkylamino-4-aryloxypiperidines of the formula ##STR1## where X is hydrogen, loweralkyl, CF.sub.3, acetyl or halogen; n is 1 or 2; R.sub.1 is H.sub.2 or oxygen; R.sub.2 is H, loweralkyl or benzyl; and R.sub.3 is oxygen or --OCH.sub.2 CH.sub.2 O--, which are useful as analgesic agents and intermediate compounds therefor.
    Type: Grant
    Filed: April 13, 1984
    Date of Patent: May 21, 1985
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Raymond W. Kosley, Jr., Richard C. Allen
  • Patent number: 4517195
    Abstract: There are described novel pyrrolo[1,2-b][1,2,5]triazepines of the general formula ##STR1## where R is hydrogen, loweralkyl, loweralkylaminoloweralkyl or diloweralkylaminoloweralkyl; X is hydrogen, halogen (fluorine, chlorine, bromine or iodine), trifluoromethyl or nitro; and Y is hydrogen, halogen or loweralkyl. Also described are derivatives of 1-amino-2-benzoylpyrrole having the general formula ##STR2## where R, X and Y are as defined above, and R.sub.1 is hydrogen, ##STR3## Compounds I and II are useful as analgesic, anxiolytic and/or anticonvulsant agents, and many of Compounds II are useful as intermediates for synthesizing Compounds I.
    Type: Grant
    Filed: July 2, 1984
    Date of Patent: May 14, 1985
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Effland, Joseph T. Klein, R. Richard L. Hamer
  • Patent number: 4507306
    Abstract: cis-4a-Aryl-1,2,3,4,4a,9b-hexahydro-benzofuro[3,2-c]pyridines and methods of preparing same are described. On the nitrogen atom there may be a substituent including loweralkyl, loweralkenyl, phenylloweralkyl, hydrogen, cyanoloweralkyl, phenylcarbonylloweralkyl, phenoxyloweralkyl and cycloalkylloweralkyl. The 4a-aryl group may be a phenyl, mono-halogen substituted phenyl, tolyl, methoxyphenyl, hydroxyphenyl, or furyl. These compounds are useful as analgesic and anticonvulsant agents.3-o-Fluorophenyl-1-methyl-4-aryl-4-piperidinols which are useful as intermediates for preparing the aforementioned compounds and methods for preparing same are also described.
    Type: Grant
    Filed: July 22, 1982
    Date of Patent: March 26, 1985
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventor: Solomon S. Klioze
  • Patent number: 4503126
    Abstract: There is disclosed a method for providing an improved abrasion resistant coating on solid substrates such as plastic articles and solid articles prepared thereby having on the surface such abrasion resistant coating. A solid substrate is coated with an organosilanol-type coating liquid comprising organosilanol molecules, or a precursor thereof or a partial condensation product thereof. At least 90 mole percent of said organosilanol molecules are trifunctional silanol molecules of the formula RSi(OH).sub.3, R being a hydrocarbon radical, and at least 50 mole percent of said trisilanols being an alkyl trisilanols of 1-3 carbon atoms or phenyl trisilanol. Preferably, at least 70 mole percent of the trisilanol is methyltrisilanol. After the coating is cured by a conventional means, it is post-treated by an electron beam irradiation to afford an abrasion resistance far superior to that obtained from organosilanol coating liquids without electron beam irradiation post-treatment.
    Type: Grant
    Filed: January 13, 1984
    Date of Patent: March 5, 1985
    Assignee: Foster Grant Corporation
    Inventors: Richard A. Phillips, Theodore A. Haddad
  • Patent number: 4496582
    Abstract: There are described analgesic dibenz[b,f]oxepins having the general formula ##STR1## wherein n is an odd integer 1-7 inclusive; R is --CO.sub.2 R.sub.1 or --CH.sub.2 OR.sub.2 where R.sub.1 is H, C.sub.1-5 lower alkyl, aralkyl, ##STR2## R.sub.3 being C.sub.1-5 lower alkyl; X and Y are each independently hydrogen, halogen, trifluoromethyl, C.sub.1-5 lower alkoxy, C.sub.1-5 lower alkyl, C.sub.1-5 lower alkylthio, or hydroxy; and the dotted line may be a bond or nothing.
    Type: Grant
    Filed: December 12, 1983
    Date of Patent: January 29, 1985
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Helen H. Ong, Matthew J. Flynn
  • Patent number: 4496732
    Abstract: A stereoselective reduction of 2- or 3-substituted 4-piperidones of the formula ##STR1## where R.sub.1 is hydrogen, loweralkyl or benzyl and R.sub.2 is methyl or ethyl, to the di-equatorial isomer of the corresponding 4-piperidinol is described. Said reduction is conducted by use of sodium borohydride in a protic solvent medium at a temperature substantially lower than ambient temperature in the presence of an effective amount of an inorganic acid. Under favorable reaction conditions, the stereoselectivity of the reduction is so high that simple crystallization of the reaction product affords the pure isomer in a commercially acceptable and advantageous process.
    Type: Grant
    Filed: March 14, 1983
    Date of Patent: January 29, 1985
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: George E. Lee, Thomas B. K. Lee
  • Patent number: 4492733
    Abstract: There is disclosed a method for providing an improved abrasion resistant coating on solid substrates such as plastic articles and solid articles prepared thereby having on the surface such abrasion resistant coating. A solid substrate is coated with an organosilanol-type coating liquid comprising organosilanol molecules or a partial condensation product thereof. At least 90 mole percent of said organosilanol molecules are trifunctional silanol molecules of the formula RSi(OH).sub.3, R being a hydrocarbon radical, and at least 50 mole percent of said trisilanols being an alkyl trisilanols of 1-3 carbon atoms or phenyl trisilanol. Preferably, at least 70 mole percent of the trisilanol is methyltrisilanol. After the coating is cured by a conventional means, it is post-treated by a glow discharge to afford an abrasion resistance far superior to those obtained from organosilanol coating liquids without glow discharge post-treatment.
    Type: Grant
    Filed: January 23, 1984
    Date of Patent: January 8, 1985
    Assignee: Foster Grant Corporation
    Inventors: Richard A. Phillips, Theodore A. Haddad
  • Patent number: 4472414
    Abstract: There are described spiro[indolo[1,7-ab][1,5]benzodiazepine-2,4'-piperidines]of the formula ##STR1## wherein p is 1 or 0, R.sub.1 is hydrogen or methyl and R is hydrogen or --CO(CH.sub.2).sub.n NR.sub.2 R.sub.3, R.sub.2 and R.sub.3 being each hydrogen or methyl but at least one of the two being methyl, and n being 1 or 2, which are useful as analgesic agents; intermediate compounds therefor; and methods for synthesizing the foregoing compounds.
    Type: Grant
    Filed: May 18, 1983
    Date of Patent: September 18, 1984
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Edward J. Glamkowski, James M. Fortunato, Richard C. Allen
  • Patent number: 4452802
    Abstract: There are described antihypertensive spiro[benzofuran-azalkanes] of the formula ##STR1## where X is hydrogen or halogen (F, Cl, Br, or I); m and n are each 0, 1 or 2 but m plus n is 1 or 2; and R is ##STR2## k being 2 or 3 and Y being hydrogen or halogen, which are useful as antihypertensive agents and methods for synthesizing the same.
    Type: Grant
    Filed: August 25, 1983
    Date of Patent: June 5, 1984
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Raymond W. Kosley, Jr., Robert J. Cherill
  • Patent number: D275160
    Type: Grant
    Filed: May 15, 1980
    Date of Patent: August 21, 1984
    Assignee: Foster Grant Corporation
    Inventor: Robert N. Shelton
  • Patent number: D275161
    Type: Grant
    Filed: May 14, 1980
    Date of Patent: August 21, 1984
    Assignee: Foster Grant Corporation
    Inventor: Robert N. Shelton