Patents by Inventor Kevin J. Kapples
Kevin J. Kapples 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).
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Patent number: 6022880Abstract: 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, antienmtics, and for the treatment of personality disorders such as obsessive compulsive disorder.Type: GrantFiled: July 28, 1997Date of Patent: February 8, 2000Assignee: Hoechst Marion Roussel, Inc.Inventors: Richard Charles Effland, Joseph Thomas Klein, Lawrence Leo Martin, Gregory M. Shutske, Kevin J. Kapples, John D. Tomer, IV
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Patent number: 5567718Abstract: 2,3-dihydro-1H-isoindole derivatives of the formula ##STR1## where R.sub.1 -R.sub.5 and X are defined herein which are useful as serotonin reuptake inhibitors are disclosed. As such, these compounds may be useful for the treatment of depression, obsessive-compulsive disorders, stuttering and trichotillomania.Type: GrantFiled: August 11, 1994Date of Patent: October 22, 1996Assignee: Hoechst Marion Roussel Inc.Inventors: Gregory M. Shutske, Kevin J. Kapples
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Patent number: 5502203Abstract: Novel 9-aminotetrahydroacridines and related compounds, intermediates and processes for the preparation thereof, and a method of relieving memory dysfunction are disclosed.Type: GrantFiled: May 31, 1995Date of Patent: March 26, 1996Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Gregory M. Shutske, Kevin J. Kapples, John D. Tomer
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Patent number: 5428169Abstract: 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: GrantFiled: September 15, 1994Date of Patent: June 27, 1995Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Gregory M. Shutske, Kevin J. Kapples, John D. Tomer, IV
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Patent number: 5401749Abstract: 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: GrantFiled: July 8, 1988Date of Patent: March 28, 1995Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Gregory M. Shutske, Kevin J. Kapples
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Patent number: 5391553Abstract: 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: GrantFiled: September 14, 1988Date of Patent: February 21, 1995Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Gregory M. Shutske, Grover C. Helsley, Kevin J. Kapples
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Patent number: 5382594Abstract: Novel 9-aminotetrahydroacridines and related compounds, intermediates and processes for the preparation thereof, and a method of relieving memory dysfunction are disclosed.Type: GrantFiled: March 1, 1993Date of Patent: January 17, 1995Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Gregory M. Shutske, Kevin J. Kapples, John D. Tomer
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Patent number: 5380847Abstract: 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: GrantFiled: January 12, 1994Date of Patent: January 10, 1995Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Gregory M. Shutske, Kevin J. Kapples, John D. Tomer, IV
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Patent number: 5328920Abstract: 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: GrantFiled: October 21, 1992Date of Patent: July 12, 1994Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Richard C. Effland, Joseph T. Klein, Lawrence L. Martin, Gregory M. Shutske, Kevin J. Kapples, John D. Tomer, IV
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Patent number: 5296491Abstract: 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: GrantFiled: August 17, 1993Date of Patent: March 22, 1994Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Gregory M. Shutske, Kevin J. Kapples, John D. Tomer, IV
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Patent number: 5264576Abstract: 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: GrantFiled: October 22, 1992Date of Patent: November 23, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Gregory M. Shutske, Kevin J. Kapples, John D. Tomer, IV
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Patent number: 5232927Abstract: 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: GrantFiled: April 18, 1991Date of Patent: August 3, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Gregory M. Shutske, Kevin J. Kapples
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Patent number: 5215984Abstract: This invention relates to spiro-](piperidine-, pyrrolidine-, or -hexahydroazepinyl substituted) pyrrolo[2,1-c][1,4]-benzoxazepines] having the following formula ##STR1## wherein R is hydrogen, lower alkyl, arylloweralkyl, acyl, lower alkenyl, lower alkynyl, and loweralkylbenzisoxazole; X is hydrogen, halogen, loweralkoxy, and trifluoromethyl; Y is hydrogen; 2' or 3' acyl, formyl, carbinol of the formula ##STR2## where R.sub.1 and R.sub.2 are the same or different and are independently hydrogen, loweralkyl, arylloweralkyl, aryl, loweralkenyl, lower alkynyl and lower alkylbenzisoxazole; loweralkyl, loweralkenyl and halogen; and n is an integer of 1 to 3. The compounds of this invention display utility as analgesic and antihypertensive agents.Type: GrantFiled: November 24, 1989Date of Patent: June 1, 1993Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Richard C. Effland, Larry Davis, Kevin J. Kapples
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Patent number: 5210087Abstract: Novel 9-aminotetrahydroacridines and related compounds, intermediates and processes for the preparation thereof, and a method of relieving memory dysfunction are disclosed.Type: GrantFiled: February 13, 1991Date of Patent: May 11, 1993Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Gregory M. Shutske, Kevin J. Kapples, John D. Tomer
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Patent number: 5194618Abstract: There are disclosed compounds of the formula ##STR1## where n is 0 or 1; R is hydrogen or loweralkyl; R.sub.1 is hydrogen, loweralkyl, halogen, --CH(OH)R.sub.4, --C(OH)R.sub.4 R.sub.5 or --CH.sub.2 OR.sub.5, R.sub.4 being hydrogen, loweralkyl, arylloweralkyl or aryl, R.sub.5 being loweralkyl, aryl or arylloweralkyl, R.sub.6 being hydrogen or loweralkyl and R.sub.7 being hydrogen, loweralkyl or aryl; R.sub.2 is hydrogen, loweralkyl, loweralkenyl, loweralkynyl, --CH.sub.2 CO.sub.2 C.sub.2 H.sub.5, arylloweralkyl, phenyl, nitrophenyl, cyanophenyl, trifluoromethylphenyl, aminophenyl, loweralkanoylaminophenyl, loweralkoxycarbonyl, arylloweralkoxycarbonyl, aryloxycarbonyl, loweralkylaminocarbonyl, arylloweralkylaminocarbonyl, arylaminocarbonyl, alkanoyl, arylloweralkanoyl, aroyl, alkenoyl, alkynoyl, --CH.sub.2 C.tbd.CCH.sub.2 --NR'R", --CH.sub.2 CH=CHCH.sub.2 --NR'R" or --CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 --NR'R", R' and R" being independently loweralkyl or --NR'R" taken as a whole being ##STR2## and R.sub.Type: GrantFiled: May 23, 1991Date of Patent: March 16, 1993Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Richard C. Effland, Joseph T. Klein, Kevin J. Kapples
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Patent number: 5112829Abstract: 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: GrantFiled: August 6, 1990Date of Patent: May 12, 1992Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Gregory M. Shutske, Kevin J. Kapples, John D. Tomer, IV
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Patent number: 5039687Abstract: There are disclosed novel compounds of the formula ##STR1## where R is H, loweralkyl, halogen, cyano, loweralkanoyl, arylloweralkanoyl, aroyl, --CH(OH)r.sub.1, --C(OH)r.sub.1 r.sub.2 or --CH.sub.2 Or.sub.2, where r.sub.1 is H, loweralkyl, arylloweralkyl or aryl and r.sub.2 is loweralkyl; R.sub.1 H, loweralkyl, arylloweralkyl, phenyl, nitrophenyl, cyanophenyl, trifluoromethylphenyl, aminophenyl, loweralkanoylaminophenyl, loweralkoxycarbonyl, arylloweralkylkoxycarbonyl, aryloxycarbonyl, loweralkylaminocarbonyl, arylloweralkylaminocarbonyl, arylaminocarbonyl, alkanoyl, arylloweralkanoyl, aroyl, alkenoyl or alkynoyl; and R.sub.2 is H, NO.sub.2, NH.sub.2, halogen, loweralkanoylamino, arylloweralkanoylamino, aroylamino or loweralkyl, or R.sub.Type: GrantFiled: February 9, 1990Date of Patent: August 13, 1991Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Richard C. Effland, Joseph T. Klein, Kevin J. Kapples
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Patent number: 5037833Abstract: 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 arylloweralkyl, 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: GrantFiled: February 15, 1990Date of Patent: August 6, 1991Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Gregory M. Shutske, Kevin J. Kapples
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Patent number: 5032599Abstract: There are disclosed novel compounds of the formula ##STR1## where n is 0 or 1; R is hydrogen or loweralkyl; R.sub.1 is hydrogen, loweralkyl, halogen, cyano, loweralkanoyl, arylloweralkanoyl, aroyl, --CH(OH)R.sub.4, --C(OH)R.sub.4 R.sub.5 or --CH.sub.2 OR.sub.5, --CH.dbd.CR.sub.6 R.sub.7, --CH.dbd.CHCN, --CH.dbd.CHOCH.sub.3, --CH.dbd.CHCO.sub.2 C.sub.2 H.sub.5, ##STR2## R.sub.4 being hydrogen, loweralkyl, arylloweralkyl or aryl, R.sub.5 being loweralkyl, aryl or arylloweralkyl, R.sub.6 being hydrogen or loweralkyl and R.sub.7 being hydrogen, loweralkyl or aryl; R.sub.2 is hydrogen, loweralkyl, loweralkenyl, loweralkynyl, --CH.sub.2 CO.sub.2 C.sub.2 H.sub.5, arylloweralkyl, phenyl, nitrophenyl, cyanophenyl, trifluoromethylphenyl, aminophenyl, loweralkanoylaminophenyl, loweralkoxycarbonyl, arylloweralkoxycarbonyl, aryloxycarbonyl, loweralkylaminocarbonyl, arylloweralkylaminocarbonyl, arylaminocarbonyl, alkanoyl, arylloweralkanoyl, aroyl, alkenoyl, alkynoyl, --CH.sub.2 C.tbd.CCH.sub.2 --NR'R", --CH.sub.2 CH.dbd.Type: GrantFiled: September 16, 1988Date of Patent: July 16, 1991Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Richard C. Effland, Joseph T. Klein, Kevin J. Kapples
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Patent number: 4996205Abstract: Pyrido[3,4-f]pyrrolo[1,2-b][1,2,5]triazepines and methods for treating depression, alleviating pain and inflammation, and enhancing memory utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: January 19, 1990Date of Patent: February 26, 1991Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Richard C. Effland, Larry Davis, Kevin J. Kapples, Gordon E. Olsen