Patents by Inventor Richard C. Effland
Richard C. Effland 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: 4900742Abstract: 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: June 1, 1988Date of Patent: February 13, 1990Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Richard C. Effland, Joseph T. Klein, Kevin J. Kapples
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Patent number: 4894461Abstract: 3-(.gamma.-chloropropyl)-6-fluoro-1,2-benzisoxazole is a compound useful in preparing compounds having a neuroleptic utility.Type: GrantFiled: February 27, 1986Date of Patent: January 16, 1990Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Larry Davis, Richard C. Effland
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Patent number: 4883794Abstract: There are described pyrrolo[1,2-b] cinnolines having formula ##STR1## where R.sub.1 when present is hydrogen, loweralky, arylloweralkyl or --CH.sub.2 CO.sub.2 C.sub.2 H.sub.5 ; 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, flourine, 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 demetia's such as Alzheimer's disease characterized by diminished cholinergic function.Type: GrantFiled: December 19, 1988Date of Patent: November 28, 1989Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: R. Russell L. Hamer, Richard C. Effland, Joseph T. Klein
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Patent number: 4880822Abstract: There are disclosed compounds of the formula ##STR1## where m, n, p, R, R.sub.1, R.sub.2 and R.sub.3 are as defined in the specification which compounds are useful for enhancing memory and also as analgesic and antidepressant agents.Type: GrantFiled: April 4, 1988Date of Patent: November 14, 1989Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Richard C. Effland, Joseph T. Klein
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Patent number: 4879382Abstract: Pyrido[3,4-f]pyrrolo[1,2-b][1,2]triazepines and methods for treating depression, alleviating pain and inflammation, and enhancing memory utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: July 25, 1988Date of Patent: November 7, 1989Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Richard C. Effland, Larry Davis, Kevin J. Kapples, Gordon E. Olsen
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Patent number: 4868190Abstract: There are described compounds of the formula: ##STR1## where, X is hydrogen, loweralkyl, loweralkoxy or halogen;Y is hydrogen, loweralkyl or halogen;Z is hydrogen, loweralkyl or halogen;R is hydrogen, loweralkyl, loweralkenyl, loweralkylcarbonyl, dimethylaminoloweralkyl or ##STR2## m being an integer of 1 to 6, with the proviso that when R is loweralkenyl the double bond is not alpha to the nitrogen atom;which compounds are useful analgesic, anticonvulsant and antidepressant agents, and for treating various memory dysfunctions characterized by decreased cholinergic function such as Alzheimer's disease.Type: GrantFiled: December 27, 1988Date of Patent: September 19, 1989Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Richard C. Effland, Joseph T. Klein, Larry Davis, Gordon E. Olsen
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Patent number: 4865764Abstract: 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, ##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: October 11, 1988Date of Patent: September 12, 1989Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Richard C. Effland, Kevin J. Kapples
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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: 4840972Abstract: 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 for enhancing memory and for treating Alzheimer's disease.Type: GrantFiled: November 14, 1988Date of Patent: June 20, 1989Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Richard C. Effland, Joseph T. Effland
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Spiro((piperidine-pyrrolidine- or hexahydroazepinyl substituted) pyrrolo(2,1-C) (1,4)benzoxazepines)
Patent number: 4812450Abstract: This invention relates to spiro-[(piperidine-, pyrrolidine-, or -hexahyroazepinyl 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## wherein 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: July 30, 1987Date of Patent: March 14, 1989Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Richard C. Effland, Larry Davis, Kevin J. Kapples -
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: 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: 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: 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
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Patent number: 4681879Abstract: There are described novel 11-substituted 5H,11H-pyrrolo[2,1-c][1,4]benzoxazepines of the general formula ##STR1## where m and n are each independently 0, 1 or 2 and m+n is 1 or 2, X and Y are each independently hydrogen, loweralkyl or halogen, and R is hydrogen, cyano, --C(NH.sub.2)NOH, ##STR2## unsubstituted loweralkyl, or substituted loweralkyl having one to three substituents each of which being independently cyano, hydroxy, cycloalkyl of 3-6 carbon atoms, furyl, thienyl, ##STR3## k being 1, 2 or 3, W being each indepentently hydrogen, halogen, hydroxy, loweralkyl, trifluoromethyl, loweralkoxy, nitro, amino, diloweralkylamino, phenoxy, or benzyloxy, and Z being hydrogen, loweralkyl or halogen, which are useful as antipsychotic and analgesic agents; novel intermediate compounds therefor; and methods of synthesizing the foregoing compounds.Type: GrantFiled: March 20, 1985Date of Patent: July 21, 1987Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Richard C. Effland, Larry Davis, Kevin J. Kapples
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Patent number: 4667039Abstract: There are described to novel 11-substituted 5H,11H-pyrrolo[2,1-c][1,4]benzoxazepines of the general formula ##STR1## where m and n are each independently 0, 1 or 2 and m+n is 1 or 2, X and Y are each independently hydrogen, loweralkyl or halogen, and R is hydrogen, cyano, --C(NH.sub.2)NOH, ##STR2## unsubstituted loweralkyl, or substituted loweralkyl having one to three substituents each of which being independently cyano, hydroxy, cyclohexyl, furyl, thienyl, ##STR3## k being 1, 2 or 3, W being each independently hydrogen, halogen, hydroxy, loweralkyl, trifluoromethyl, loweralkoxy, nitro, amino, diloweralkylamino, phenoxy, or benzyloxy, and Z being hydrogen, loweralkyl or halogen, which are useful as antipsychotic and analgesic agents; novel intermediate compounds therefor; and methods of synthesizing the foregoing compounds.Type: GrantFiled: December 19, 1985Date of Patent: May 19, 1987Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Richard C. Effland, Larry Davis, Kevin J. Kapples
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Patent number: 4608374Abstract: There are described to novel 11-substituted 5H,11H-pyrrolo[2,1-c][1,4]benzoxazepines of the general formula ##STR1## where m and n are each independently 0, 1 or 2 and m+n is 1 or 2, X and Y are each independently hydrogen, loweralkyl or halogen, and R is hydrogen, cyano, --C(NH.sub.2)NOH, ##STR2## unsubstituted loweralkyl, or substituted loweralkyl having one to three substituents each of which being independently cyano, hydroxy, cyclohexyl, furyl, thienyl, ##STR3## k being 1, 2 or 3, W being each independently hydrogen, halogen, hydroxy, loweralkyl, trifluoromethyl, loweralkoxy, nitro, amino, diloweralkylamino, phenoxy, or benzyloxy, and Z being hydrogen, loweralkyl or halogen, which are useful as antipsychotic and analgesic agents; novel intermediate compounds therefor; and methods of synthesizing the foregoing compounds.Type: GrantFiled: November 7, 1983Date of Patent: August 26, 1986Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Richard C. Effland, Larry Davis, Kevin J. Kapples