Patents Assigned to Hoechst-Roussel Pharmaceutical Incorporated
  • Patent number: 5521320
    Abstract: This invention relates to a process of obtaining optically pure enantiomers of an alkylated oxindole selected from ##STR1## where R is methyl, ethyl or benzyl.
    Type: Grant
    Filed: May 27, 1993
    Date of Patent: May 28, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Thomas B. K. Lee, George S. K. Wong
  • Patent number: 5514700
    Abstract: There are disclosed various compounds of the formula below, ##STR1## where n, X and R.sub.1 through R.sub.4 are as defined in the specification, which are useful for alleviating various memory dysfunctions characterized by a cholinergic deficit such as Alzheimer's disease.Compounds of this invention also inhibit monoamine oxidase and/or act at central .alpha..sub.2 -adrenergic receptors, and hence are useful as antidepressants.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: May 7, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Helen H. Ong, Gerard J. O'Malley, Michael C. Merriman, Mark G. Palermo
  • Patent number: 5498726
    Abstract: This application relates to a new process for the preparation of a product of the formula ##STR1## wherein R, R.sup.1, R.sup.2, X and m are as defined within, which process comprises preparing treating a compound such as physostigmine to form eseroline which is then treated with an appropriate compound or its equivalent. Acetic acid is added to the reaction mixture after the formation of eseroline.
    Type: Grant
    Filed: March 22, 1994
    Date of Patent: March 12, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: George E. Lee, Thomas B. K. Lee, Donna M. Borek
  • Patent number: 5494908
    Abstract: This application relates to compounds of the formula ##STR1## wherein R.sup.1, X, Y and n are as defined in the specification; and pharmaceutically acceptable addition salts thereof and optical and geometric isomers or racemic mixtures thereof; which compounds are useful for the treatment of various memory dysfunctions characterized by a decreased cholinergic function such as Alzheimer's disease. Compounds of this invention also inhibit monoamine oxidase and hence are useful as antidepressants.
    Type: Grant
    Filed: November 12, 1993
    Date of Patent: February 27, 1996
    Assignee: Hoechst-Roussel Pharmaceutical Incorporated
    Inventors: Gerard J. O'Malley, Mark G. Palermo
  • Patent number: 5475107
    Abstract: Process for obtaining 3,7-dialkylxanthines from 3-alkyl-xanthines3,7-Dialkylxanthines are obtained from the corresponding 3-alkylxanthines using an alkylating agent in the presence of quaternary ammonium and/or phosphonium compounds and, where appropriate, of additional polyethers in a two-phase mixture.
    Type: Grant
    Filed: November 9, 1993
    Date of Patent: December 12, 1995
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Gerhard Korb, Hans-Wolfram Flemming
  • Patent number: 5472975
    Abstract: There are disclosed various compounds of the formula below, ##STR1## where n, X and R.sub.1 through R.sub.4 are as defined in the specification, which are useful for alleviating various memory dysfunctions characterized by a cholinergic deficit such as Alzheimer's disease.Compounds of this invention also inhibit monoamine oxidase and/or act at central .alpha..sub.2 -adrenergic receptors, and hence are useful as antidepressants.
    Type: Grant
    Filed: January 4, 1994
    Date of Patent: December 5, 1995
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Helen H. Ong, Gerard J. O'Malley, Michael C. Merriman, Mark G. Palermo
  • 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: 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: 5360811
    Abstract: Novel 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols of the formulaRCH(OR.sup.1)CH(NR.sup.2 R.sup.3)R.sup.4 or RCH.sub.2 CR.sup.35 (NR.sup.2 R.sup.3)R.sup.4wherein R is ##STR1## wherein R.sup.5 is CH.sub.3 (CH.sub.2).sub.m C.tbd.C, CH.sub.3 (CH.sub.2).sub.m CH.dbd.CH,CH.sub.3 (CH.sub.2).sub.m CH.sub.2 CH.sub.2, ##STR2## wherein m is 3 to 15, n is 0 to 12, and W and X are independently hydrogen, hydroxy, alkyl, alkoxy, halogen, or trifluoromethyl, ##STR3## wherein R.sup.23 loweralkyl; Z is S, O, or C.dbd.O; and A is S or O; R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.35 and R.sup.40 are as defined in the specification, the optical isomers thereof, or the pharmaceutically acceptable salts thereof, intermediates and processes for the preparation thereof, and methods of reducing inflammation and cell proliferation, and relieving memory dysfunction, and inhibiting bacterial and fungal growth are disclosed.
    Type: Grant
    Filed: September 10, 1992
    Date of Patent: November 1, 1994
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: John J. Tegeler, Barbara S. Rauckman, Russell R. L. Hamer, Brian S. Freed, Gregory H. Merriman
  • Patent number: 5350762
    Abstract: There are disclosed various compounds of the formula below, ##STR1## where the various parameters R.sub.1, R.sub.2, R.sub.3, R.sub.4, X, m and n are as defined in the specification, which show activities as a monoamine oxidase inhibitor demonstrating a utility for the treatment of depression, and activities as a cholinesterase inhibitor demonstrating a utility for the treatment of various memory dysfunctions such as Alzheimer's disease.
    Type: Grant
    Filed: March 8, 1993
    Date of Patent: September 27, 1994
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Lawrence L. Martin, Larry Davis
  • Patent number: 5328920
    Abstract: There are disclosed various compounds of the formula below, ##STR1## where R, R.sub.1, W, X, Y and Z are as defined in the specification; which are useful for alleviating various memory dysfunctions such as Alzheimer's disease, as modulators of neurotransmitter functions 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 disorder.
    Type: Grant
    Filed: October 21, 1992
    Date of Patent: July 12, 1994
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Richard C. Effland, Joseph T. Klein, Lawrence L. Martin, Gregory M. Shutske, Kevin J. Kapples, John D. Tomer, IV
  • Patent number: 5310914
    Abstract: Novel 5-amino-5,6,7,8-tetrahydroquinolines and related compounds, intermediates and processes for the preparation thereof, and methods for relieving memory dysfunction utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: March 19, 1993
    Date of Patent: May 10, 1994
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Richard C. Effland, David Fink
  • 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: 5300498
    Abstract: There are disclosed various compounds of the formula below, ##STR1## where the parameters n, R.sub.1, R.sub.2 and X are as defined in the specification which are selective inhibitors of the reuptake of the serotonin and as such are useful for the treatment of depression and obsessive compulsive disorder.
    Type: Grant
    Filed: June 4, 1993
    Date of Patent: April 5, 1994
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventor: Gregory M. Shutske
  • Patent number: 5300527
    Abstract: This invention relates to alkylamino and alkyl amino alkyl diarylketones of the formula ##STR1## where Ar is aryl of the formula ##STR2## where V is hydrogen, halogen, loweralkyl, loweralkoxy, CF.sub.3, NO.sub.2 and u is an integer of 1 to 3; X and Y are independently CH.sub.2 --, --CF.sub.2 -- or --CHF--; Z and W are independently --CH.sub.2 --, --O--, --CHOH--, or --CHF--; m, n, p, q and t are integers which are independently 0 or 1; R.sub.1 is H or loweralkyl; R.sub.2 and R.sub.3 are loweralkyl; and the pharmaceutically acceptable acid addition salts thereof and where applicable the geometric and optical isomers and racemic mixtures thereof. The compounds of this invention display utility as analgesic agents and as agents for alleviating various memory dysfunctions, characterized by a decreased cholinergic function, such as Alzheimer's disease.
    Type: Grant
    Filed: October 13, 1992
    Date of Patent: April 5, 1994
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: R. Richard L. Hamer, Brian Freed, Richard C. Allen
  • Patent number: 5298626
    Abstract: There are disclosed various compounds of the formula below, ##STR1## wherein n, X and R.sub.1 through R.sub.4 are as defined in the specification, which are useful for alleviating various memory dysfunctions characterized by a cholinergic deficit such as Alzheimer's disease.Compounds of this invention also inhibit monoamine oxidase and/or act at central .alpha..sub.2 -adrenergic receptors, and hence are useful as antidepressants.
    Type: Grant
    Filed: November 13, 1992
    Date of Patent: March 29, 1994
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Helen H. Ong, Gerard J. O'Malley, Michael C. Merriman, Mark G. Palermo
  • Patent number: 5292883
    Abstract: A compound of the formula ##STR1## wherein R.sup.1 is hydrogen, loweralkyl, phenyl, phenyl substituted by one or more loweralkyl, loweralkoxy, halogen, or trifluoromethyl groups, phenylloweralkyl or phenylloweralkyl in which the phenyl group is substituted by one or more loweralkyl, loweralkoxy, halogen, or trifluoromethyl groups; R.sup.2 is loweralkyl, furanylloweralkyl, thienylloweralkyl, pyrrolylloweralkyl, pyridinylloweralkyl, phenylloweralkyl, or phenylloweralkyl in which the phenyl group is substituted by one or more loweralkyl, loweralkoxy, halogen, or trifluoromethyl groups; X is hydrogen, loweralkyl, loweralkoxy, halogen, or trifluoromethyl; m is 0, 1 or 2; n is 1 or 2; an optical isomer thereof or a salt thereof.
    Type: Grant
    Filed: May 27, 1993
    Date of Patent: March 8, 1994
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Lawrence L. Martin, Denise M. Flanagan, Joseph F. Payack
  • Patent number: 5276156
    Abstract: This invention relates to 1-(pyrido[3,4-b]-1,4-oxazinyl-4-yl)-1H-indoles of the formula ##STR1## where R.sub.1 -R.sub.3 are as defined herein which are useful for alleviation of depression and various memory dysfunction characterized by a cholinergic or adrenergic deficit. This invention also relates to intermediate compounds of the formula ##STR2## where R.sub.1, R.sub.2, R.sub.3, R.sub.7 and X are as defined herein.
    Type: Grant
    Filed: November 16, 1992
    Date of Patent: January 4, 1994
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Richard C. Effland, Larry Davis, Gordon E. Olsen
  • Patent number: 5272148
    Abstract: Novel heteroarenylpiperazines, intermediates and processes for the preparation thereof, and methods for treating psychoses utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: September 9, 1992
    Date of Patent: December 21, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Nicholas J. Hrib, John G. Jurcak
  • Patent number: 5268468
    Abstract: Novel 2-(3-phenylpropyl)hydrazines, intermediates in and processes for the preparation thereof, and a method of treating personality disorders utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: May 24, 1993
    Date of Patent: December 7, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Richard C. Effland, Joseph T. Klein