Patents by Inventor Gregory M. Shutske

Gregory M. Shutske has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 5428169
    Abstract: There are disclosed novel pyrazolo[4,3-c]pyridines of the formula ##STR1## where Ar and R.sub.1 are as defined in the specification, which are useful as serotonin reuptake inhibitors and as such may be useful for the treatment of depression, obsessive-compulsive disorders, stuttering and trichotillomania.
    Type: Grant
    Filed: September 15, 1994
    Date of Patent: June 27, 1995
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Gregory M. Shutske, Kevin J. Kapples, John D. Tomer, IV
  • 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: 5382594
    Abstract: Novel 9-aminotetrahydroacridines and related compounds, intermediates and processes for the preparation thereof, and a method of relieving memory dysfunction are disclosed.
    Type: Grant
    Filed: March 1, 1993
    Date of Patent: January 17, 1995
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Gregory M. Shutske, Kevin J. Kapples, John D. Tomer
  • Patent number: 5380847
    Abstract: There are disclosed novel pyrazolo[4,3-c]pyridines of the formula ##STR1## where Ar and R.sub.1 are as defined in the specification, which are useful as serotonin reuptake inhibitors and as such may be useful for the treatment of depression, obsessive-compulsive disorders, stuttering and trichotillomania.
    Type: Grant
    Filed: January 12, 1994
    Date of Patent: January 10, 1995
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Gregory M. Shutske, Kevin J. Kapples, John D. Tomer, IV
  • Patent number: 5330986
    Abstract: This invention relates to indole-7-carboxamide derivatives of the formula ##STR1## where R.sub.1 through R.sub.6 are independently H, loweralkyl, aryl, and aralkyl; and in addition R.sub.3 and R.sub.5 can be joined together to form a piperazine ring of the formula ##STR2## where R.sub.7 is H, loweralkyl, aryl, arylloweralkyl, pyrimidyl; and R.sub.4 and R.sub.5 can be joined together to form a pyrrolidine ring of the formula ##STR3## where R.sub.8 is H, loweralkyl, aryl, arylloweralkyl; X is H, loweralkyl, halogen, NO.sub.2, CF.sub.3, NH.sub.2, and OR.sub.9 ; where R.sub.9 is loweralkyl, arylloweralkyl and n is an integer of 1 to 3; and the pharmaceutically acceptable acid addition salts thereof and the optical isomers thereof where such isomers exist.
    Type: Grant
    Filed: November 24, 1992
    Date of Patent: July 19, 1994
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventor: Gregory M. Shutske
  • 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: 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: 5296491
    Abstract: There are disclosed novel pyrazolo[4,3-c]pyridines of the formula ##STR1## where Ar and R.sub.1 are as defined in the specification, which are useful as serotonin reuptake inhibitors and as such may be useful for the treatment of depression, obsessive-compulsive disorders, stuttering and trichotillomania.
    Type: Grant
    Filed: August 17, 1993
    Date of Patent: March 22, 1994
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Gregory M. Shutske, Kevin J. Kapples, John D. Tomer, IV
  • Patent number: 5264576
    Abstract: There are disclosed novel pyrazolo[4,3-c]pyridines of the formula ##STR1## where Ar and R.sub.1 are as defined in the specification, which are useful as serotonin reuptake inhibitors and as such may be useful for the treatment of depression, obsessive-compulsive disorders, stuttering and trichotillomania.
    Type: Grant
    Filed: October 22, 1992
    Date of Patent: November 23, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Gregory M. Shutske, Kevin J. Kapples, John D. Tomer, IV
  • Patent number: 5256672
    Abstract: This invention relates to 6,7-dihydro-3-phenyl-1,2-benzisoxazol-4(5H)-ones and -ols of the formula ##STR1## wherein X is ##STR2## or loweralkyl; Y is hydrogen, halogen, loweralkyl, loweralkoxy, trifluoromethyl, nitro or amino; R is H when the bond between the oxygen atom and the carbon atom in question is a single bond; otherwise the dotted line signifies part of a double bond to the oxygen atom; R.sub.1 is hydrogen, loweralkyl or arylloweralkyl; R.sub.2 and R.sub.3 are independently hydrogen, loweralkyl or arylloweralkyl, or R.sub.2 and R.sub.3 taken together with the nitrogen atom form an optionally substituted heterocycle selected from the group consisting of piperidinyl, pyrtolidinyl, morpholinyl, imidazol-1-yl, 1-piperazinyl, said substituents being hydrogen or loweralkyl; 4-substituted-1-piperazinyl of the formula where R.sub.
    Type: Grant
    Filed: December 13, 1992
    Date of Patent: October 26, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: David G. Wettlaufer, Gregory M. Shutske, Peter A. Nemoto
  • Patent number: 5232927
    Abstract: There are disclosed novel compounds having the formula, ##STR1## wherein, m is an integer of 0-3;n is an integer of 1-4;R.sub.1 is hydrogen, alkyl, cycloalkyl, arylloweralkyl, aryl, naphthyl, furyl, thienyl, pyridinyl or pyrrolyl;each R.sub.2 and R.sub.3 are independently hydrogen, loweralkyl or aryllowralkyl, or alternatively R.sub.2 and R.sub.3 taken together form a methylene or ethylene bridge;X is hydrogen, loweralkyl, cycloalkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, formyl, loweralkoxycarbonyl, 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 CH.sub.2, CH.dbd.CH, O, S or NR.sub.7, R.sub.7 being hydrogen, loweralkyl or arylloweralkyl;with the proviso that the number of said methylene or ethylene bridge shall not exceed 1 and that when Y is CH.sub.2, one and only one combination of R.sub.2 and R.sub.
    Type: Grant
    Filed: April 18, 1991
    Date of Patent: August 3, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Gregory M. Shutske, Kevin J. Kapples
  • Patent number: 5210087
    Abstract: Novel 9-aminotetrahydroacridines and related compounds, intermediates and processes for the preparation thereof, and a method of relieving memory dysfunction are disclosed.
    Type: Grant
    Filed: February 13, 1991
    Date of Patent: May 11, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Gregory M. Shutske, Kevin J. Kapples, John D. Tomer
  • Patent number: 5208330
    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: February 25, 1992
    Date of Patent: May 4, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Gregory M. Shutske, Richard C. Effland
  • Patent number: 5206387
    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 of (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: October 19, 1992
    Date of Patent: April 27, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Gregory M. Shutske, Richard C. Effland
  • Patent number: 5180834
    Abstract: This invention relates to 6,7-dihydro-3-phenyl-1,2-benzisoxazol-4(5H)-ones and -ols of the formula ##STR1## wherein X is ##STR2## or loweralkyl; Y is hydrogen, halogen, loweralkyl, loweralkoxy, trifluoromethyl, nitro or amino; R is H when the bond between the oxygen atom and the carbon atom in question is a single bond; otherwise the dotted line signifies part of a double bond to the oxygen atom; R.sub.1 is hydrogen, loweralkyl or arylloweralkyl; R.sub.2 and R.sub.3 are independently hydrogen, loweralkyl or arylloweralkyl, or R.sub.2 and R.sub.3 taken together with the nitrogen atom form an optionally substituted heterocycle selected from the group consisting of piperidinyl, pyrrolidinyl, morpholinyl, imidazol-1-yl, 1-piperazinyl, said substituents being hydrogen or loweralkyl;4-substituted-1-piperazinyl of the formula ##STR3## R.sub.8 is hydrogen or --OH; R.sub.
    Type: Grant
    Filed: February 28, 1992
    Date of Patent: January 19, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: David G. Wettlaufer, Gregory M. Shutske, Peter A. Nemoto
  • Patent number: 5179100
    Abstract: There are disclosed various compounds of the formula below, ##STR1## where the parameters R.sub.1, R.sub.2 and R.sub.3 are as defined in the specification, which compounds are useful as analgesic agents.
    Type: Grant
    Filed: March 9, 1992
    Date of Patent: January 12, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals inc.
    Inventors: Gregory M. Shutske, John D. Tomer, IV
  • Patent number: 5114936
    Abstract: This invention relates to 6,7-dihydro-3-phenyl-1,2-benzisoxazol-4(5H)-ones and -ols of the formula ##STR1## wherein X is (Y) ##STR2## or loweralkyl; Y is hydrogen, halogen, loweralkyl, loweralkoxy, trifluoromethyl, nitro or amino; R is H when the bond between the oxygen atom and the carbon atom in question is a single bond; otherwise the dotted line signifies part of a double bond to the oxygen atom; R.sub.1 is hydrogen, loweralkyl or arylloweralkyl; R.sub.2 and R.sub.3 are independently hydrogen, lower alkyl or arylloweralkyl, or R.sub.2 and R.sub.3 taken together with the nitogen atom form an optionally substituted heterocycle selected from the group consisting of piperidinyl, pyrrolidinyl, morpholinyl, imidazol-1-yl, 1-piperazinyl, said substituents being hydrogen or loweralkyl; 4-substituted-1-piperazinyl of the formula ##STR3## where R.sub.
    Type: Grant
    Filed: April 26, 1991
    Date of Patent: May 19, 1992
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: David G. Wettlaufer, Gregory M. Shutske, Peter A. Nemoto
  • Patent number: 5112829
    Abstract: Novel 9-amino-1,2,3,4-tetrahydroacridines and related compounds of the formula ##STR1## wherein R.sup.1 is H, loweralkyl, or benzyl; R.sup.3 is H, loweralkyl, a group of the formula CH.sub.2 CHR.sup.2 Hal wherein R.sup.2 is hydrogen, loweralkyl, or phenyl and Hal is chloro, bromo, or iodo, or a group of the formula CHR.sup.2 CO.sub.2 R.sup.5 wherein R.sup.2 is as above and R.sup.5 is H or loweralkyl; Z is O or S; X is H, halogen, loweralkoxy, loweralkyl, or trifluoromethyl; n is 1, 2, or 3; the group ZR.sup.3 is bound to either the A- or B-position of the heteroaromatic nucleus; the pharmaceutically acceptable salts thereof; and the optical isomers thereof, useful as intermediates for the preparation of memory dysfunction relieving hexahydro-1H-quino[4,3,2-ef][1,4]benzoxazepines are related compounds and for relieving memory dysfunction are disclosed.
    Type: Grant
    Filed: August 6, 1990
    Date of Patent: May 12, 1992
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Gregory M. Shutske, Kevin J. Kapples, John D. Tomer, IV