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).
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Patent number: 5112830Abstract: 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: GrantFiled: January 10, 1991Date of Patent: May 12, 1992Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Gregory M. Shutske, Richard C. Effland
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Patent number: 5070209Abstract: Novel 12-halogenated forskolin derivatives, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: April 12, 1991Date of Patent: December 3, 1991Assignee: Hoechst Roussel Pharmaceuticals Inc.Inventor: Gregory M. Shutske
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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: 5023344Abstract: Novel 12-halogenated forskolin derivatives, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: May 14, 1990Date of Patent: June 11, 1991Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventor: Gregory M. Shutske
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Patent number: 5013741Abstract: There are disclosed compounds having the formula ##STR1## wherein n is 1-4; R.sub.1 is hydrogen, alkyl, aryl, arylloweralkyl, naphthyl, furyl, thienyl, pyridinyl or pyrrolyl; X is hydrogen, loweralkyl, cycloalkyl, loweralkoxy, halogen, hydroxy nitro, trifluoromethyl, formyl, loweralkylcarbonyl, arylcarbonyl, --SH, loweralkylthio, --NHCOR.sub.2 or --NR.sub.3 R.sub.4 where R.sub.2 is hydrogen or loweralkyl, and R.sub.3 and R.sub.4 are independently hydrogen, loweralkyl or cycloalkyl; stereo, optical and geometrical isomers thereof, and pharmaceutically acceptable acid addition salts thereof, which are useful for enhancing memory and pharmaceutical compositions comprising an effective memory enhancing amount of such a compound.Type: GrantFiled: July 25, 1988Date of Patent: May 7, 1991Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventor: Gregory M. Shutske
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Patent number: 5002955Abstract: 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: GrantFiled: April 13, 1989Date of Patent: March 26, 1991Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Gregory M. Shutske, Richard C. Effland
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Patent number: 4994452Abstract: Novel hexahydro-1H-quino[4,3,2-ef][1,4]benzoxazepines and related compounds, intermediates for the preparation thereof, and a method for relieving memory dysfunction, utilizing the compounds are disclosed.Type: GrantFiled: November 28, 1989Date of Patent: February 19, 1991Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Gregory M. Shutske, Kevin J. Kapples, John D. Tomer, IV
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Patent number: 4978678Abstract: Novel 12-halogenated forskolin derivatives, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: August 7, 1989Date of Patent: December 18, 1990Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventor: Gregory M. Shutske
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Patent number: 4960767Abstract: This invention relates to isoxazolobenzoxazepines having the following formula ##STR1## wherein X.sub.1 is H; X.sub.2 is H or OH; or X.sub.1 and X.sub.2 taken together are carbonyl oxygen or ##STR2## R is (1) H, (2) loweralkyl, (3) arylloweralkyl, (4) loweralkynyl, (5) loweralkenyl, (6) ##STR3## where R.sub.1 and R.sub.2 are independently (a) H, (b) lower alkyl, (c) arylloweralkyl, (d) ##STR4## where Z is H, halogen, loweralkyl, loweralkoxy, CF.sub.3, nitro or amino and n' is an integer of 1 to 3; (e) ##STR5## where n" is an integer of 1 to 3; or (f) R.sub.1 and R.sub.2 taken together with the nitrogen atom are substituted or unsubstituted piperidino or pyrrolidino of the formula ##STR6## where R.sub.3 is H, loweralkyl or aryl, and m is an integer of 1 or 2; (7) ##STR7## where R.sub.4 is H or loweralkyl and m' is an integer of 3 or 4; (8) ##STR8## where Z and n' are as previously defined; (9) ##STR9## where m'" is an integer of 1, 2, or 3 (10) ##STR10## where R.sub.5 and R.sub.Type: GrantFiled: January 30, 1989Date of Patent: October 2, 1990Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Gregory M. Shutske, Kevin J. Kapples
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Patent number: 4942237Abstract: There are disclosed compounds having the formula ##STR1## where X is hydrogen, loweralkyl, loweralkoxy, halogen or trifluoromethyl, andR when present is hydrogen, loweralkyl, allyl, arylloweralkyl, ##STR2## wherein R.sub.1 is loweralkyl, --CH.sub.2 C.tbd.CH, ##STR3## n being 2, 3 or 4 and R.sub.2 and R.sub.3 being independently loweralkyl, or the group ##STR4## taken as a whole constituting ##STR5## which compounds are useful as analgesic agents and also for the treatment of various memory dysfunctions characterized by a decreased cholinergic function such as Alzheimer's disease.Type: GrantFiled: February 12, 1990Date of Patent: July 17, 1990Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventor: Gregory M. Shutske
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Patent number: 4927820Abstract: There are disclosed compounds having the formula ##STR1## where R.sub.1 is hydrogen, loweralkyl or arylloweralkyl;Z is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, nitro or trifluoromethyl;Y is O or NR.sub.2, R.sub.2 being hydrogen, loweralkyl or arylloweralkyl; andX is CR.sub.3, CHR.sub.3, C.dbd.O, C.dbd.S or CHN(CH.sub.3).sub.2, R.sub.3 being hydrogen, loweralkyl or aryl;stereo isomers thereof and pharmaceutically acceptable acid addition salts thereof, which are useful for the treatment of various memory dysfunctions characterized by decreased cholinergic function, such as Alzheimer's disease.Type: GrantFiled: November 25, 1988Date of Patent: May 22, 1990Assignee: Hoechst Roussel Pharmaceuticals Inc.Inventors: Gregory M. Shutske, Kevin J. Kapples
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Patent number: 4920117Abstract: There are disclosed compounds having the formula ##STR1## where X is hydrogen, loweralkyl, loweralkoxy, halogen or trifluoromethyl, andR when present is hydrogen, loweralkyl, allyl, arylloweralkyl, ##STR2## wherein R.sub.1 is loweralkyl, --CH.sub.2 C.tbd.CH, ##STR3## n being 2, 3 or 4 and R.sub.2 and R.sub.3 being independently loweralkyl, or the group ##STR4## taken as a whole constituting ##STR5## which compounds are useful as analgesic agents and also for the treatment of various memory dysfunctions characterized by a decreased cholinergic function such as Alzheimer's disease.Type: GrantFiled: June 9, 1989Date of Patent: April 24, 1990Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventor: Gregory M. Shutske
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Patent number: 4897400Abstract: 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.sup.6 where R.sup.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 P and Q are independently CR.sub.7 'R.sub.8 ', CR.sub.7 'R.sub.8 '-CR.sub.9 'R.sub.10 ' 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.10 ' is independently H or CH.Type: GrantFiled: February 13, 1987Date of Patent: January 30, 1990Assignee: Hoeschst-Roussel Pharmaceuticals, Inc.Inventor: Gregory M. Shutske
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Patent number: 4873234Abstract: This invention relates to isoxazolobenzoxazepines having the following formula ##STR1## wherein X.sub.1 is H; X.sub.2 is H or OH; or X.sub.1 and X.sub.2 taken together are carbonyl oxygen or ##STR2## R is (1) H, (2) loweralkyl, (3) arylloweralkyl, (4) loweralkynyl, (5) loweralkenyl, ##STR3## where R.sub.1 and R.sub.2 are independently (a) H, (b) lower alkyl, (c) arylloweralkyl, (d) lower alkylene ##STR4## where Z is H, halogen, loweralkyl, loweralkoxy, CF.sub.3, nitro or amino and n is a integer of 1 to 3; ##STR5## where n" is an integer of 1 to 3; or (f) R.sub.1 and R.sub.2 taken together with the nitrogen atom are substituted or unsubstituted piperidino or pyrrolidino of the formula ##STR6## where R.sub.3 is H, loweralkyl or aryl, and m is an integer of 1 to 2; ##STR7## wherein R.sub.4 is H or loweralkyl and m' is an integer of 3 to 4; ##STR8## where Z and n are as previously defined; ##STR9## where m'" is an integer of 1,2 or 3 ##STR10## where R.sub.5 and R.sub.Type: GrantFiled: August 1, 1988Date of Patent: October 10, 1989Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Gregory M. Shutske, Kevin J. Kapples
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Patent number: 4871764Abstract: Novel 12-halogenated forskolin derivatives, intermediates and processes for their preparation, and methods for reducing intraocular pressure utilizing the compounds or compositions are disclosed.Type: GrantFiled: November 20, 1986Date of Patent: October 3, 1989Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventor: Gregory M. Shutske
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Patent number: 4868177Abstract: There are disclosed compounds having the formula ##STR1## where n is 1, 2 or 3;X is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, nitro or trifluoromethylR.sub.1 and R.sub.2 are each independently hydrogen, lower alkyl or arylloweralkyl, but both may not be arylloweralkyl simultaneously;R.sub.3 and R.sub.4 are each independently hydrogen, lower alkyl, arylloweralkyl, formyl or lower alkylcarbonyl, or alternatively the group --NR.sub.3 R.sub.4 taken as a whole constitutes ##STR2## stereo isomers thereof and pharmaceutically acceptable acid addition salts thereof, which are useful for the treatment of various memory dysfunctions characterized by decreased cholinergic function, such as Alzheimer's disease.Type: GrantFiled: November 29, 1988Date of Patent: September 19, 1989Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Gregory M. Shutske, Kevin J. Kapples
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Patent number: 4868188Abstract: Novel 4-(benzisothiazol-3-yl)phenoxyacetic acid 1',1'-dioxides of the formula ##STR1## where X is hydrogen, halogen or loweralkyl; R.sub.1 is hydrogen or loweralkyl; R.sub.2 and R.sub.3 are each independently Cl, Br or CH.sub.3, and related compounds, methods for preparing same and methods of treatment by administering compositions containing such a compound are described. These compounds are useful as diuretics.Type: GrantFiled: November 3, 1982Date of Patent: September 19, 1989Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventor: Gregory M. Shutske
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Patent number: 4855479Abstract: There are disclosed compounds having the formula ##STR1## wherein m is 1 or 2; n is 1 or 2; p is 1-5; X is hydrogen, loweralkyl, cycloalkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, formyl, loweralkylcarbonyl, arylcarbonyl, --SH, loweralkylthio, --NHCOR.sub.2 or --NR.sub.3 R.sub.4 where R.sub.2 is hydrogen or loweralkyl, and R.sub.3 and R.sub.4 are independently hydrogen, loweralkyl or cycloalkyl; R is hydrogen, loweralkyl or loweralkylcarbonyl; and R.sub.1 is hydrogen, loweralkyl, loweralkylcarbonyl, aryl, diloweralkylaminolowralkyl, arylloweralkyl, diarylloweralkyl, oxygen-bridged arylloweralkyl or oxygen-bridged diarylloweralkyl; stereo, optical and geometrical isomers thereof, and pharmaceutically acceptable acid addition salts thereof, which are useful for enhancing memory.Type: GrantFiled: November 21, 1988Date of Patent: August 8, 1989Inventor: Gregory M. Shutske
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Patent number: 4843079Abstract: 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-bridge 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.6 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: GrantFiled: April 4, 1988Date of Patent: June 27, 1989Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Gregory M. Shutske, Richard C. Effland
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Patent number: 4839364Abstract: There are disclosed compounds having the formula ##STR1## wherein n is 1, 2 or 3; X is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, NHCOR.sub.2 where R.sub.2 is loweralkyl, or NR.sub.3 R.sub.4 where R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl; R is hydrogen or loweralkyl; R.sub.1 is hydrogen, loweralkyl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, furylloweralkyl, thienylloweralkyl, oxygen-bridged arylloweralkyl, oxygen-bridged diarylloweralkyl, oxygen-bridged furylloweralkyl or oxygen-bridged thienylloweralkyl; Y is C.dbd.O or CR.sub.5 OH where R.sub.5 is hydrogen or loweralkyl; Z is CH.sub.2 or C.dbd.CR.sub.6 R.sub.7 where R.sub.6 and R.sub.7 are independently hydrogen or loweralkyl; or Y and Z taken together is CR.sub.5 .dbd.Ch where CR.sub.Type: GrantFiled: January 28, 1987Date of Patent: June 13, 1989Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Gregory M. Shutske, Frank A. Pierrat