Patents Represented by Attorney, Agent or Law Firm Tatsuya Ikeda
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Patent number: 4806554Abstract: There are described compounds of the formula ##STR1## where n is 0 or 1; R.sub.1 is independently hydrogen, loweralkyl, loweralkenyl, loweralkynyl, loweralkoxycarbonylloweralkyl, loweralkylaminocarbonylloweralkyl, aminocarbonylloweralkyl, arylloweralkyl, phenyl, nitrophenyl, cyanophenyl, trifluoromethylphenyl, aminophenyl, loweralkanoylaminophenyl, loweralkoxycarbonyl, arylloweralkoxycarbonyl, aryloxycarbonyl, loweralkylaminocarbonyl, arylloweralkylaminocarbonyl, arylaminocarbonyl, alkanoyl, arylloweralkanoyl, aroyl, alkenoyl, alkynoyl or --R.sub.5 --NR'R" where R.sub.5 is loweralkylene, loweralkenylene or loweralkynylene and R' and R" are each independently loweralkyl or alternatively the group --NR'R" as a whole is 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 4-loweralkyl-1-piperazinyl or 4-aryl-1-piperazinyl;R.sub.2 is hydrogen or loweralkyl;R.sub.3 and R.sub.4 are each independently hydrogen or loweralkyl, or alternatively R.sub.3 and R.sub.4 taken together form --CH.dbd.CH--CH.dbd.Type: GrantFiled: January 11, 1988Date of Patent: February 21, 1989Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Richard C. Effland, Joseph T. Klein
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Patent number: 4806649Abstract: Novel 3-(piperidinyl)- and 3-(pyrrolidinyl)-1H-indazoles, intermediates and processes for the preparation thereof, and methods for treating psychoses, treating depression, alleviating pain, treating convulsions and treating hypertension utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: August 4, 1988Date of Patent: February 21, 1989Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventor: Joseph T. Strupczewski
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Patent number: 4806646Abstract: 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, diloweralkylaminoloweralkyl, 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: May 9, 1988Date of Patent: February 21, 1989Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventor: Gregory M. Shutske
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Patent number: 4800203Abstract: There are described pyrrolo[1,2-b]cinnolines having the formula ##STR1## where R.sub.1 when present is hydrogen, loweralkyl, arylloweralkyl or --CH.sub.2 CO.sub.2 C.sub.2 H.sub.5 ; R.sub.2 is hydrogen, loweralkyl, arylloweralkyl, chlorine, bromine, iodine, formyl, nitro, --Ch.dbd.CR.sub.3 R.sub.4 or --CH.sub.2 CHR.sub.3 R.sub.4, R.sub.3 and R.sub.4 being independently hydrogen, loweralkyl, aryl or arylloweralkyl; X is oxygen, amino, loweralkylamino, arylloweralkylamino or methoxy; and Y is hydrogen, fluorine, chlorine, bromine, iodine, trifluoromethyl or nitro, and pharmaceutically acceptable acid addition salts thereof which are useful as analgesic agents and as enhancers of cholinergic function and hence for the treatment of memory dysfunctions and senile dementia's such as Alzheimer's disease characterized by diminished cholinergic function.Type: GrantFiled: September 24, 1987Date of Patent: January 24, 1989Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: R. Russell Hamer, Richard C. Effland, Joseph T. Klein
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Patent number: 4794181Abstract: The invention relates to 1-aryloxy-2,3,4,5-tetrahydro-3-benzazepines of the formula ##STR1## wherein Y is the same of different and is hydrogen and lower alkoxy; X is hydrogen, halogen, lower alkyl, lower alkoxy, CF.sub.3, NO.sub.2, CN and NH.sub.2 ; R is hydrogen, lower alkyl, cycloalkyllower alkyl, ##STR2## Ar lower alkyl of the formula ##STR3## where Z is hydrogen, lower alkyl, lower alkoxy, halogen CF.sub.3, NO.sub.2 and NH.sub.2 ; Aryloxy lower alkyl of the formula ##STR4## where Z is as previously defined; and an alkylene amine of the formula ##STR5## where R.sub.1 and R.sub.2 are the same or different and are hydrogen and lower alkyl, n is an integer of 1 or 2; and the pharmaceutically acceptable acid addition salts thereof.Type: GrantFiled: January 16, 1986Date of Patent: December 27, 1988Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Richard C. Effland, Joseph T. Klein, Larry Davis
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Patent number: 4794110Abstract: There are disclosed compounds of the formula, ##STR1## where X and Y are each independently hydrogen, loweralkyl, halogen or trifluoromethyl; Z is hydrogen or 2- or 3-Cl, Br, I, CHO or CH.dbd.CR.sub.1 R.sub.2 where R.sub.1 and R.sub.2 are each independently hydrogen or loweralkyl; R is hydrogen, --(CH.sub.2).sub.n NR.sub.3 R.sub.4 or ##STR2## where n is 1, 2 or 3, R.sub.3 is loweralkyl, and R.sub.4 is hydrogen or loweralkyl, or alternatively the group --NR.sub.3 R.sub.4 as a whole is ##STR3## where R.sub.6 is loweralkyl, ##STR4## and R.sub.7 is loweralkyl or ##STR5## R.sub.8 being hydrogen, loweralkyl, halogen, trifluoromethyl or methoxy; and R.sub.5 is hydrogen, loweralkyl or arylloweralkyl.Type: GrantFiled: July 20, 1987Date of Patent: December 27, 1988Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Richard C. Effland, Kevin J. Kapples
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Patent number: 4792562Abstract: 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## --CH.sub.2 CHR.sub.6 R.sub.7, --CH.sub.2 CH.sub.2 CN, --CH.sub.2 CH.sub.2 OCH.sub.3, --CH.sub.2 CH.sub.2 CO.sub.2 C.sub.2 H.sub.5, ##STR3## 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.Type: GrantFiled: November 12, 1986Date of Patent: December 20, 1988Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Richard C. Effland, Joseph T. Klein, Kevin J. Kapples
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Patent number: 4791107Abstract: There are described compounds of the formula ##STR1## where (a) X is O or S;(b) R is H, loweralkyl, ##STR2## where Y is O or S; R.sub.2 is alkyl, cycloalkyl, bicycloalkyl, cycloalkenyl, aryl, arylloweralkyl, heteroaryl or heteroarylloweralkyl, R.sub.3 is H or alkyl, or the group --NR.sub.2 R.sub.3 taken as a whole is 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 4-thiomorpholinyl, 1-piperazinyl, 4-methyl-1-piperazinyl or 2-(2,6-dichlorophenylimino)-1-imidazolidinyl) and R.sub.4 is hydrogen, loweralkyl, arylloweralkyl, diarylloweralkyl, aryl or heteroaryl,(c) m is 1 or 2;(d) each Z is independently H, loweralkyl, halogen, nitro, --NH.sub.2, loweralkylcarbonylamino, arylcarbonylamino, loweralkoxycarbonylamino or loweralkylamino, and(e) R.sub.1 is H, loweralkyl, arylloweralkyl, heteroarylloweralkyl, cycloalkylmethyl or loweralkenylmethyl, with the proviso that when X is O, m is 1, Z is H and R.sub.1 is methyl, R is not --CONHCH.sub.3, --CONHC.sub.6 H.sub.Type: GrantFiled: May 15, 1987Date of Patent: December 13, 1988Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: R. Richard L. Hamer, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang
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Patent number: 4789678Abstract: There are described compounds of the formula ##STR1## where X is hydrogen, halogen, loweralkyl, loweralkoxy or trifluoromethyl; R is ##STR2## R.sub.4 being loweralkyl; R.sub.1 is hydrogen, loweralkyl or arylloweralkyl; R.sub.2 is hydrogen, loweralkyl or arylloweralkyl; and R.sub.3 is loweralkyl, with the proviso that when R is acetyl, R.sub.3 is methyl and X is hydrogen, R.sub.1 and R.sub.2 are not both hydrogen, or pharmaceutically acceptable acid addition salts thereof, which are useful in the treatment of various memory dysfunctions characterized by decreased cholinergic function.Type: GrantFiled: August 25, 1986Date of Patent: December 6, 1988Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Richard C. Effland, Joseph T. Klein
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Patent number: 4780466Abstract: There are disclosed compounds of the formula ##STR1## wherein the group A is ##STR2## where R.sub.1 and R.sub.2 are each independently hydrogen or loweralkyl, or R.sub.1 +R.sub.2 =(CH.sub.2).sub.m, m being 2 to 6, p is 1 or 2, and each X is independently hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, nitro, amino, loweralkylamino, diloweralkylamino, trifluoromethyl or loweralkylthio; W is O, H.sub.2 or [H, OH]; n is 2, 3 or 4; and R.sub.3 is ##STR3## where q is 1 or 2 and each Y is independently hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, nitro, amino, loweralkylamino, diloweralkylamino, trifluoromethyl or loweralkylthio, which are useful as antipsychotic, anxiolytic and analgesic agents.Type: GrantFiled: March 17, 1988Date of Patent: October 25, 1988Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Nicholas J. Hrib, John G. Jurcak
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Patent number: 4775761Abstract: Novel 3-(piperidinyl)- and 3-(pyrrolidinyl)-1H-indazoles, intermediates and processes for the preparation thereof, and methods for treating psychoses, treating depression, alleviating pain, treating convulsions and treating hypertension utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: April 15, 1988Date of Patent: October 4, 1988Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventor: Joseph T. Strupczewski
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5-Substituted 1-(4-(1-pyrrolidinyl)-2-butynyl)-2-pyrrolidinones, pharmaceutical compositions and use
Patent number: 4772601Abstract: There are disclosed compounds of the formula ##STR1## where R.sub.1 is loweralkoxycarbonyl, --CH.sub.2 OH or --CONR.sub.3 R.sub.4, R.sub.3 and R.sub.4 being independently hydrogen, loweralkyl or arylloweralkyl; and R.sub.2 is --CH.sub.2 CH.dbd.CH.sub.2, ##STR2## R.sub.5 and R.sub.6 being independently loweralkyl or alternatively the group --NR.sub.5 R.sub.6 as a whole being ##STR3## R.sub.7 being hydrogen, loweralkyl or arylloweralkyl; which are useful for enhancing cholinergic activity in mammals and hence for the treatment of various memory dysfunctions characterized by decreased cholinergic function such as Alzheimer's disease.Type: GrantFiled: January 25, 1988Date of Patent: September 20, 1988Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventor: Lawrence L. Martin -
Patent number: 4771052Abstract: There are disclosed compounds of the formula ##STR1## where X and Y are independently hydrogen, loweralkyl, loweralkoxy, hydroxy, halogen, trifluoromethyl or nitro; R.sub.1 is hydrogen or loweralkyl; R.sub.2 is hydrogen, loweralkyl, loweralkylcarbonyl or arylcarbonyl; and R.sub.3 is hydrogen, loweralkyl, arylloweralkyl, ##STR2## loweralkylcarbonyl or arylcarbonyl, n being an interger of 1 to 6 inclusive and Z being hydrogen, loweralkyl, loweralkoxy, hydroxy or halogen; which are useful as hypotensive agents.Type: GrantFiled: February 5, 1987Date of Patent: September 13, 1988Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Karl Schonafinger, Helen H. Ong
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Patent number: 4769472Abstract: There are described compounds of the formula ##STR1## where X is O or NR, R being hydrogen or loweralkyl; R.sub.1 is hydrogen; and R.sub.2 is loweralkyl, arylloweralkyl, aryloxyloweralkyl or loweralkyl substituted with ##STR2## or alternatively--NR.sub.1 R.sub.2 taken together is ##STR3## R.sub.3 being arylloweralkyl or a pharmaceutically acceptable acid addition salt thereof, which are useful as ocular or systemic antihypertensive agents.There are also described intermediate compounds having the formula ##STR4## where X is oxygen or NR, R being hydrogen or loweralkyl; and Y is --OCH.sub.3, --OH or ##STR5## as well as intermediate compounds of the formula ##STR6## where Z is oxygen, NOH or NNHR.sub.4, R.sub.4 being hydrogen or loweralkyl.Type: GrantFiled: November 25, 1987Date of Patent: September 6, 1988Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Helen H. Ong, Christine M. Yasenchak
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Patent number: 4762841Abstract: 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, diloweralkylaminoloweralkyl, 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: March 30, 1987Date of Patent: August 9, 1988Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventor: Gregory M. Shutske
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Patent number: 4758578Abstract: There are described compounds of the formula ##STR1## where n is 0, 1 or 2; X and Y are independently hydrogen, loweralkyl, loweralkoxy, arylloweralkyl, aryloxy, halogen, --CF.sub.3, --NO.sub.2, --OH, --OCOR.sub.1, ##STR2## where R.sub.1 is loweralkyl, arylloweralkyl, aryl or loweralkoxy, R.sub.2 is hydrogen, loweralkyl or loweralkylcarbonyl, R.sub.3 is hydrogen or loweralkyl, or the group --NR.sub.2 R.sub.3 as a whole is ##STR3## m is 0, 1 or 2, and R.sub.4 is hydrogen, loweralkyl or aryl; and Z is (R.sub.5,R.sub.6), ##STR4## where R.sub.5 and R.sub.6 are each independently hydrogen or loweralkyl, R.sub.7 is loweralkyl, R.sub.8 is hydrogen, loweralkyl or aryl, R.sub.9 and R.sub.10 are each independently loweralkyl or the group --NR.sub.9 R.sub.10 as a whole is ##STR5## R.sub.12 being hydrogen, loweralkyl or aryl, and R.sub.11 is hydrogen, loweralkyl or aryl; which are useful for the treatment of glaucoma.Type: GrantFiled: January 29, 1987Date of Patent: July 19, 1988Assignee: Hoechst Roussel Pharmaceuticals, Inc.Inventors: John J. Tegeler, Kirk D. Shoger
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Patent number: 4758668Abstract: Novel 3-(piperidinyl)- and 3-(pyrrolidinyl)-1H-indazoles, intermediates and processes for the preparation thereof, and methods for treating pyschoses, treating depression, alleviating pain, treating convulsions and treating hypertension utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: September 30, 1987Date of Patent: July 19, 1988Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventor: Joseph T. Strupczewski
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Patent number: 4753950Abstract: There are disclosed compounds of the formula ##STR1## where .dbd.X--Y-- is ##STR2## R.sub.4 being loweralkyl and R.sub.5 being hydrogen or loweralkyl, --Z-- is ##STR3## n is 1, 2 or 3, R.sub.1 and R.sub.2 are each independently hydrogen, loweralkyl or arylloweralkyl, and R.sub.3 is hydrogen or loweralkyl, with the proviso that when .dbd.X--Y-- is ##STR4## n is 2 or 3, R.sub.1 is hydrogen and R.sub.2 is hydrogen or loweralkyl, Z is not ##STR5## which compounds are useful for enhancing memory and for treating Alzheimer's disease.Type: GrantFiled: November 24, 1986Date of Patent: June 28, 1988Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Gregory M. Shutske, Kevin J. Kapples
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Patent number: 4754050Abstract: 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: November 25, 1987Date of Patent: June 28, 1988Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Gregory M. Shutske, Frank A. Pierrat
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Patent number: 4752610Abstract: 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 is H, loweralkyl, arylloweralkyl, phenyl, nitrophenyl, cyanophenyl, trifluoromethylphenyl, aminophenyl, loweralkanoylaminophenyl, loweralkoxycarbonyl, arylloweralkoxycarbonyl, 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: December 4, 1985Date of Patent: June 21, 1988Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Richard C. Effland, Joseph T. Klein, Kevin J. Kapples