Patents Represented by Attorney, Agent or Law Firm Barbara V. Maurer
  • Patent number: 5455354
    Abstract: This invention relates to a process for the preparation of a product of the formula ##STR1## wherein R, R.sup.1, R.sup.2, X and m are defined within which process comprises(a) contacting a compound of Formula II ##STR2## wherein R.sup.3 is loweralkyl, with a reagent selective from the group consisting of aluminum chloride, hydrobromic acid and boron tribromide followed by tartaric acid to afford a compound of Formula III ##STR3## wherein R, X and m are as defined above; (b) contacting the reaction mixture containing compound of Formula IV ##STR4## wherein R.sup.4 is hydrogen or loweralkyl in the presence of a carboxylic acid of the formulaR.sup.5 COOHwherein R.sup.5 is loweralkyl to afford a compound of formula V ##STR5## wherein R, R.sup.4, X and m are as above; contacting the reaction mixture containing the compound of Formula V obtained in step(b) with a compound of the formulaR.sup.1 R.sup.2 NHwherein R.sup.1 and R.sup.2 are as above; and isolating the product of Formula I.
    Type: Grant
    Filed: February 17, 1994
    Date of Patent: October 3, 1995
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: George S. K. Wong, Thomas B. K. Lee, Franz J. Weiberth
  • Patent number: 5430110
    Abstract: Polyvinylamine derivatives having hydrophilic centers, processes for their preparation and the use of the compounds as a medicament, active compound carrier and foodstuff auxiliary.Polyvinylamine derivatives containing hydrophilic centers, of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, X, w, x, y and z have the meanings given, and a process for their preparation, and the use of these compounds as medicaments, active compound carriers and foodstuff auxiliaries are described. Highly pure polyvinylamines having the recurring unit of the formula Ia ##STR2## the preparation of which is likewise described, are used in particular as starting substances for the preparation.
    Type: Grant
    Filed: July 21, 1993
    Date of Patent: July 4, 1995
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Michael Ahlers, Heiner Glombik, Susanne Grabley, Ernold Granzer, Stefan Mullner, Axel Walch, Guan-Yu Xu
  • Patent number: 5428112
    Abstract: Crosslinked, nitrogen-containing vinyl copolymers having units of the formula I ##STR1## and physiologically tolerated salts thereof, in which, in formula I, A1, A2, R, w, x, y and z have the meanings given, a process for their preparation and the use of the compounds as medicaments, active compound carriers and foodstuff auxiliaries are described.
    Type: Grant
    Filed: July 21, 1993
    Date of Patent: June 27, 1995
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Michael Ahlers, Heiner Glombik, Stefan Mullner, Axel Walch
  • Patent number: 5424322
    Abstract: This invention relates to compositions of substituted pyridinylamino-1H-indoles of the formula ##STR1## wherein Q is N or NR.sub.2 ;Y is CHR.sub.1 is hydrogen, loweralkyl, loweralkynyl, loweralkenyl, arylloweralkyl, loweralkoxycarbonylaminoloweralkylcarbonyl, arylloweralkoxycarbonylaminoloweralkylcarbonyl, aminoloweralkylcarbonyl, loweralkoxycarbonyl or acyl;R.sub.2 is hydrogen or loweralkyl;R.sub.3 is hydrogen or loweralkyl;X is hydrogen, loweralkyl, halogen; andn is 0 or 1 with utility in the treatment of personality disorders as obsessive compulsive disorders.
    Type: Grant
    Filed: March 25, 1993
    Date of Patent: June 13, 1995
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Effland, Joseph T. Klein, Lawrence L. Martin
  • Patent number: 5405856
    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;eachR.sub.4 is independently hydrogen or loweralkyl; andY is hydrogen, halogen, loweralkyl, loweralkoxy or trifluoromethyl;which compounds are useful as topical antiinflammatory agents for the treatment of various dermatoses.
    Type: Grant
    Filed: April 2, 1993
    Date of Patent: April 11, 1995
    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: 5401749
    Abstract: There are disclosed compounds having the formula ##STR1## wherein R is hydrogen, loweralkyl or loweralkylcarbonyl; R.sub.1 is hydrogen, loweralkyl, loweralkylcarbonyl, aryl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, oxygen-bridged arylloweralkyl or oxygen-bridged diarylloweralkyl; R.sub.2 and R.sub.3 are independently H or CH.sub.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 where R.sub.4 is hydrogen or loweralkyl, and R.sub.5 and R.sub.6 are independently hydrogen, loweralkyl or cycloalkyl; Y and Z are independently a direct bond, CR.sub.7 R.sub.8 or CR.sub.7 R.sub.8 --CR.sub.9 R.sub.10 ; and L and Q are independently CR'.sub.7 R'.sub.8, CR'.sub.7 R'.sub.8 --CR'.sub.9 R'.sub.10, CR'.sub.7 .dbd.CR'.sub.9 or CR'.sub.7 R'.sub.8 --CR'.sub.9 R'.sub.10 --CR.sub.11 R.sub.12, where each of R.sub.7 through R.sub.12 and R'.sub.7 through R'.sub.
    Type: Grant
    Filed: July 8, 1988
    Date of Patent: March 28, 1995
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Gregory M. Shutske, Kevin J. Kapples
  • Patent number: 5391553
    Abstract: There are disclosed compounds having the formula ##STR1## wherein n is 1-4; X is alkyl of 3-18 carbon atoms, cycloalkyl of 3-7 carbon atoms or cycloalkylloweralkyl; R is hydrogen, loweralkyl or loweralkylcarbonyl; R.sub.1 is hydrogen, loweralkyl, loweralkylcarbonyl, aryl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, oxygen-bridged arylloweralkyl or oxygen-bridged diarylloweralkyl; stereo isomers thereof and pharmaceutically acceptable acid addition salts thereof, which are useful for enhancing memory, methods for synthesizing them, and pharmaceutical compositions comprising an effective memory enhancing amount of such a compound.
    Type: Grant
    Filed: September 14, 1988
    Date of Patent: February 21, 1995
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Gregory M. Shutske, Grover C. Helsley, Kevin J. Kapples
  • Patent number: 5389629
    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: January 10, 1991
    Date of Patent: February 14, 1995
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Gregory M. Shutske, Richard C. Effland
  • Patent number: 5371087
    Abstract: There are disclosed compounds of the formula, ##STR1## where n is 0, 1 or 2; A is ##STR2## where X in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, loweralkoxy, amino, cyano, trifluoromethyl or methylthio; Y in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, loweralkoxy, amino cyano, trifluoromethyl or methylthio; m is 1 or 2; k is 1 or 2; R.sub.1 and R.sub.2 are independently hydrogen, loweralkyl, ##STR3## or aryl except that when R.sub.1 is ##STR4## or aryl, R.sub.2 is hydrogen, or alternatively R.sub.1 +R.sub.2 taken together with the carbon atom to which they are attached form a cyclopentane, cyclohexane, cycloheptane, pyran, thiopyran, indan or piperidine ring; R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl, or alternatively R.sub.3 +R.sub.
    Type: Grant
    Filed: June 29, 1993
    Date of Patent: December 6, 1994
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Nicholas J. Hrib, John G. Jurcak
  • Patent number: 5340936
    Abstract: This invention relates to compounds of the formula ##STR1## where X is --0--, --S--or --NH--;Y is hydrogen, halogen and loweralkoxy;p is 1 or 2;n is 2, 3 or 4;R is hydrogen, loweralkyl, loweralkoxy, hydroxy, halogen, amino, loweralkylamino, nitro, loweralkylthio, trifiuoromethoxy, cyano, trifluoromethyl, ##STR2## where aryl is ##STR3## R.sub.1 is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, carboxyl, loweralkylamino, nitro, loweralkylthio, cyano, and trifluoromethyl;m is 1 or 2; a pharmaceutically acceptable acid addition salt thereof and, where applicable the geometric and optical isomers and racemic mixtures thereof.The compounds and compositions of this invention are useful as antipsychotic agent, as 5-HT.sub.3 receptor antagonists and as inhibitors of the reuptake of serotonin.
    Type: Grant
    Filed: March 25, 1993
    Date of Patent: August 23, 1994
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Edward J. Glamkowski, David M. Fink, Barbara E. Kurys, Yulin Chiang
  • Patent number: 5334599
    Abstract: This invention relates to compounds of the formula ##STR1## where X is --O--, --S-- or --NH--;Y is hydrogen, halogen and loweralkoxy;p is 1 or 2;n is 2, 3 or 4;R is hydrogen, loweralkyl, loweralkoxy, hydroxy, halogen, amino, loweralkylamino, nitro, loweralkylthio, trifiuoromethoxy, cyano, trifiuoromethyl, ##STR2## R.sub.1 is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, carboxyl, loweralkylamino, nitro, loweralkylthio, cyano, and trifiuoromethyl;m is 1 or 2; a pharmaceutically acceptable acid addition salt thereof and, where applicable the geometric and optical isomers and racemic mixtures thereof.The compounds and compositions of this invention are useful as antipsychotic as 5-HT.sub.3 receptor antagonists and as inhibitors of the reuptake of serotonin.
    Type: Grant
    Filed: March 25, 1993
    Date of Patent: August 2, 1994
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Edward J. Glamkowski, David M. Fink, Barbara E. Kurys, Yulin Chiang
  • Patent number: 5328852
    Abstract: A method for determining the amount of an analyte in a sample fluid utilizing an assay element which comprises at least one reagent layer. The assay method includes the steps of optically reading a signal producing species, e.g., a fluorescent label, a first time prior to depositing the sample fluid on the assay element and a second time, at the same wavelength and in the same location within the assay element after the sample fluid has been applied to the assay element and the sample analyte has interacted with the reagent(s) present in the assay element. The first, or dry, reading is corrected for relative humidity and/or temperature variations.
    Type: Grant
    Filed: October 16, 1992
    Date of Patent: July 12, 1994
    Assignee: PB Diagnostic Systems, Inc.
    Inventors: John J. Blackwood, Shai Inbar
  • Patent number: 5319096
    Abstract: There are disclosed compounds having the formula ##STR1## wherein X is hydrogen, chloro, bromo, fluoro, hydroxy, loweralkoxy, arylloweralkoxy, acyloxy, loweralkylaminocarbonyloxy, diloweralkylaminocarbonyloxy, amino, loweralkylamino, diloweralkylamino, acylamino, loweralkyl or trifluoromethyl;Y is hydrogen, loweralkyl, chloro or bromo;Z is hydrogen, loweralkyl, loweralkoxy or halogen; or X and Z taken together can form a methylenedioxy group;R.sup.1 is hydrogen, loweralkyl, arylloweralkyl, carboxyloweralkyl, arylloweralkoxycarbonylloweralkyl or loweralkoxycarbonylloweralkyl;R.sup.2 is hydrogen, loweralkyl or hydroxyloweralkyl;R.sup.3 is hydrogen or loweralkyl; orR.sup.2 and R.sup.3 together with the carbon to which they are attached form (C.sub.3 -C.sub.7)cycloalkyl;R.sup.4 is hydrogen or loweralkyl;R.sup.5 is hydrogen, loweralkyl, aryl, arylloweralkyl, acyl, arylloweralkoxycarbonyl, loweralkoxycarbonyl or aryloxycarbonyl;R.sup.
    Type: Grant
    Filed: April 3, 1992
    Date of Patent: June 7, 1994
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Raymond W. Kosley, Jr., Denise M. Flanagan, Lawrence L. Martin, Peter A. Nemoto
  • Patent number: 5302721
    Abstract: This application relates to a new process for the preparation of a product of the formula ##STR1## wherein R is loweralkyl;R.sup.1 is hydrogen, loweralkyl, lowercycloalkyl, lowercycloalkylloweralkyl, lowerbicycloalkyl, aryl or arylloweralkyl;R.sup.2 is loweralkyl, lowercycloalkyl, lowercycloalkylloweralkyl, lowerbicycloalkyl, aryl or arylloweralkyl; orR.sup.1 and R.sup.2 taken together with the nitrogen atom to which they are attached from a 3,4-dihydro-2H(1H)-isoquinoline group;X is loweralkyl, loweralkoxy, halogen or trifluoromethyl; andm is 0, 1 or 2;which process comprises(a) contacting a compound of formula II ##STR2## wherein R, X and m are as defined above and R.sup.3 is loweralkyl, with aluminum chloride followed by tartaric acidto afford a compound of formula III ##STR3## wherein R, X and m are as defined above; (b) contacting the reaction mixture containing the compound of Formula III either(1) with an isocyanate of the formula R.sup.1 NCO and obtaining a product of the formula I wherein R.sup.
    Type: Grant
    Filed: July 21, 1992
    Date of Patent: April 12, 1994
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: George S. K. Wong, Thomas B. K. Lee, Franz J. Weiberth
  • Patent number: 5252581
    Abstract: This application relates to compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, m and n are as defined in the specification which are useful as modulators of neurotransmitter function such as serotonergic and adrenergic, and as such are useful as antidepressants, anxiolytics, atypical antipsychotics, antiemetics, and for the treatment of personality disorders such as obsessive compulsive disorders. Certain of the compounds are also useful as glycine partial agonists.
    Type: Grant
    Filed: July 20, 1992
    Date of Patent: October 12, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Effland, Joseph T. Klein, Lawrence L. Martin
  • Patent number: 5229388
    Abstract: There are disclosed compounds of the formula, ##STR1## where n is 0, 1 or 2; A is ##STR2## where X in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, loweralkoxy, amino, cyano, trifluoromethyl or methylthio; Y in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, loweralkoxy, amino, cyano, trifluoromethyl or methylthio; m is 1 or 2; k is 1 or 2; R.sub.1 and R.sub.2 are independently hydrogen, loweralkyl, ##STR3## or aryl except that when R.sub.1 is ##STR4## or aryl, R.sub.2 is hydrogen, or alternatively R.sub.1 +R.sub.2 taken together with the carbon atom to which they are attached form a cyclopentane, cyclohexane, cycloheptane, pyran, thiopyran, indan or piperidine ring; R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl, or alternatively R.sub.3 +R.sub.
    Type: Grant
    Filed: November 21, 1991
    Date of Patent: July 20, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Nicholas J. Hrib, John G. Jurcak
  • Patent number: 5214035
    Abstract: This application relates to a novel thixotropic formulation of a compound which suppresses estrus in animals, which formulation allows for convenient, accurate dosing of the animal when treated with the compound.
    Type: Grant
    Filed: April 16, 1992
    Date of Patent: May 25, 1993
    Assignee: Hoechst-Roussel Agri-Vet Company
    Inventor: James L. Veatch
  • Patent number: 5182275
    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: May 10, 1990
    Date of Patent: January 26, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Karl Schonafinger, Helen H. Ong
  • Patent number: 5091541
    Abstract: There are disclosed various compounds of the formula below, ##STR1## where X is O, S, NH, N-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: October 24, 1990
    Date of Patent: February 25, 1992
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Gerard J. O'Malley, Richard C. Allen, John I. White
  • Patent number: 5028732
    Abstract: Compounds having the formula ##STR1## wherein Q is substituted phenyl or substituted pyridyl; Y is nitro, cyano, or halogen; R is a group of the formula --(CHR.sup.1).sub.m --A--(CH.sup.2)--.sub.n --R.sup.3 wherein R.sup.1 and R.sup.2, independently of each other and in each (CHR.sup.1) and (CHR.sup.2) group, are hydrogen, unsubstituted or substituted alkyl, alkoxy, or alkylthio; A is --N(R.sup.1)--, --N(O)--, --O--, --S--, --S(O)--, --S(O).sub.2 --, --C(O)--, --C(O)B--, or --N(H)S(O).sub.2 --; B is alkylene, --O--, --S--, or --N(R.sup.4)--; R.sup.3 is cyano, halogen, or C(O)Z; R.sup.4 is hydrogen or unsubstituted or substituted alkyl; Z is hydrogen, unsubstituted or substituted alkyl, --N(R.sup.4).sub.2, --OR.sup.5, --SR.sup.5, or --N(R.sup.4)SO.sub.2 R.sup.6 ; R.sup.5 is hydrogen, unsubstituted or substituted alkyl, or an agronomically-acceptable cation; R.sup.
    Type: Grant
    Filed: March 13, 1986
    Date of Patent: July 2, 1991
    Assignee: Rohm and Haas Company
    Inventors: Ann H. Beaulieu, Roy Y. Yih