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: 5252581Abstract: This application relates to compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, m and n are as defined in the specification which are useful as modulators of neurotransmitter function 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 disorders. Certain of the compounds are also useful as glycine partial agonists.Type: GrantFiled: July 20, 1992Date of Patent: October 12, 1993Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Richard C. Effland, Joseph T. Klein, Lawrence L. Martin
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Patent number: 5246947Abstract: This invention relates to substituted pyridinylamino-1H-indoles, 1H-indazoles, 2H-indazoles, benzo[b]thiophenes and 1,2-benzisothiazoles of the formula ##STR1## wherein Q is S, N or NR.sub.2 ;Y is CH, N or NR.sub.2 ;R.sub.1 is hydrogen, loweralkyl, loweralkynyl, loweralkenyl, arylloweralkyl, loweralkoxycarbonylaminoloweralkylcarbonyl, arylloweralkoxycarbonylaminoloweralkylcarbonyl, aminoloweralkylcarbonyl, loweralkoxycarbonyl or acyl;R.sub.2 is hydrogen or loweralkyl;R.sub.3 is hydrogen or loweralkyl;X is hydrogen, loweralkyl, halogen; andn is 0 or 1; or a pharmaceutically acceptable acid addition salt thereof.The compounds of this invention are useful in the treatment of memory dysfunctions characterized by a cholinergic deficit such as the type associated with Alzheimer's disease and other memory disorders.Type: GrantFiled: August 7, 1992Date of Patent: September 21, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Richard C. Effland, Joseph T. Klein, Lawrence L. Martin
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Patent number: 5229417Abstract: Novel 2-(3-phenylpropyl)hydrazines, intermediates in and processes for the preparation thereof, and a method of treating personality disorders utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: December 5, 1991Date of Patent: July 20, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Richard C. Effland, Joseph T. Klein
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Patent number: 5229401Abstract: This invention relates to substituted pyridinylamino-1H-indoles, 1H-indazoles, 2H-indazoles, benzo[b]thiophenes and 1,2-benzisothiazoles of the formula ##STR1## wherein Q is S, N or NR.sub.2 ;Y is CH, N or NR.sub.2 ;R.sub.1 is hydrogen, loweralkyl, loweralkynyl, loweralkenyl, arylloweralkyl, loweralkoxycarbonylaminoloweralkylcarbonyl, arylloweralkoxycarbonylaminoloweralkylcarbonyl, aminoloweralkylcarbonyl, loweralkoxycarbonyl or acyl;R.sub.2 is hydrogen or loweralkyl;R.sub.3 is hydrogen or loweralkyl;X is hydrogen, loweralkyl, halogen; andn is 0 or 1; or a pharmaceutically acceptable acid addition salt thereof.The compounds of this invention are useful in the treatment of memory dysfunctions characterized by a cholinergic deficit such as the type associated with Alzhemier's disease and other memory disorders.Type: GrantFiled: August 7, 1992Date of Patent: July 20, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Richard C. Effland, Joseph T. Klein, Lawrence L. Martin
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Patent number: 5227388Abstract: Novel naphtho[2,3-b]thiophen-9(4H)-ones of the formula ##STR1## wherein R is loweralkyl or arylloweralkyl; X and Y are independently hydrogen, loweralkyl, halogen, loweralkoxy, or trifluoromethyl; W is CH.sub.2, CHOH, or C.dbd.O; n is 1 or 2; an optical isomer or pharmaceutically acceptable salt thereof, processes for the preparation thereof, and methods of alleviating pain utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: January 30, 1991Date of Patent: July 13, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Richard C. Effland, David G. Wettlaufer
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Patent number: 5221682Abstract: There are described compounds of the formula ##STR1## where n is 0 or 1;X is O or NR.sub.2, R.sub.2 being hydrogen, loweralkyl or loweralkylcarbonyl;R is hydrogen, loweralkyl, arylloweralkyl or loweralkylcarbonyl; andR.sub.1 is ##STR2## wherein R.sub.3 is hydrogen, loweralkyl or loweralkylcarbonyl; m is 1 or 2; each R.sub.4 is independently hydrogen or loweralkyl; and Y is hydrogen, halogen, loweralkyl, loweralkoxy or trifluoromethyl;which compounds are useful as topical antiinflammatory agents for the treatment of various dematoses.Type: GrantFiled: May 3, 1991Date of Patent: June 22, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Richard C. Effland, Joseph T. Klein, Gordon E. Olsen, Larry Davis, Russell R. L. Hamer, Brian S. Freed
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Patent number: 5216164Abstract: Novel 5-amino-5,6,7,8-tetrahydroquinolines and related compounds, intermediates and processes for the preparation thereof, and methods for relieving memory dysfunction utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: February 10, 1992Date of Patent: June 1, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Richard C. Effland, David Fink
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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: 5214058Abstract: This invention relates to compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, loweralkyl, arylloweralkyl, loweralkenyl or loweralkynyl;R.sub.2 is hydrogen, loweralkyl, loweralkenyl, formyl or cyano;X is hydrogen, halogen, nitro, amino, loweralkyl, loweralkoxy or hydroxy;Y is hydrogen, loweralkyl, loweralkoxy, arylloweralkoxy, hydroxy, halogen, nitro or amino, with the proviso that when Y is hydrogen or loweralkyl, R.sub.1 is not hydrogen and R.sub.2 is not formyl; a pharmaceutically acceptable acid addition salt thereof, or where applicable, a geometric or optical isomer or racemic mixture thereof. The compounds of the invention are useful for the treatment of various memory dysfunctions characterized by a decreased cholinergic function, such as found in Alzheimer's disease and other senile dementia.Type: GrantFiled: June 27, 1991Date of Patent: May 25, 1993Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Richard C. Effland, Larry Davis, Gordon E. Olsen
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Patent number: 5214038Abstract: This invention relates to compounds of the formula ##STR1##whereinR.sub.1 is hydrogen or loweralkyl;R.sub.2 is hydrogen or loweralkyl; andR.sub.3 is hydrogen, loweralkyl, halogen, nitro, amino, hydroxy, loweralkoxy, benzyloxy or ##STR2##where R.sub.4 is hydrogen or loweralkyl and R.sub.5 is loweralkyl, aryl or arylloweralkyl, or R.sub.4 and R.sub.5 taken together form a heterocyclic ring selected from the group consisting of ##STR3##whereinR.sub.6 is hydrogen, loweralkyl, aryl or arylloweralkyl or a pharmaceutically acceptable acid addition salt thereof.The compounds of this invention are useful for alleviating depression and various memory dysfunctions characterized by a cholinergic or adrenergic deficit, such as Alzheimer's Disease.Type: GrantFiled: April 15, 1991Date of Patent: May 25, 1993Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Richard C. Effland, Larry Davis, Gordon E. Olsen
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Patent number: 5208330Abstract: 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: February 25, 1992Date of Patent: May 4, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Gregory M. Shutske, Richard C. Effland
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Patent number: 5206387Abstract: 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: GrantFiled: October 19, 1992Date of Patent: April 27, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Gregory M. Shutske, Richard C. Effland
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Patent number: 5204480Abstract: There are described compounds of the formula ##STR1## where n is 1, 2 or 3;R.sub.1 is hydrogen, formyl, loweralkylcarbonyl, arylloweralkylcarbonyl, loweralkyl, arylloweralkyl, ##STR2## R.sub.5 and R.sub.6 being independently loweralkyl or alternatively the group ##STR3## taken as a whole is ##STR4## R.sub.2 is hydrogen, loweralkyl, loweralkenyl, arylloweralkyl, --CH.sub.2 C.tbd.CH, ##STR5## R.sub.7 and R.sub.8 being independently loweralkyl or alternatively the group ##STR6## taken as a whole is ##STR7## R.sub.3 is hydrogen is loweralkyl; and R.sub.4 is hydrogen or loweralkyl;which compounds are useful as analgesic agents and also for treating various memory dysfunctions.Type: GrantFiled: February 21, 1992Date of Patent: April 20, 1993Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Richard C. Effland, David M. Fink
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Patent number: 5202319Abstract: There are disclosed various compounds of the formula below, ##STR1## where n is 1 or 2;m is 1 or 2;each X is independently hydrogen or loweralkoxy;Y is hydrogen, halogen or trifluoromethyl;R.sub.1 is hydrogen, loweralkyl, arylloweralkyl, heteroarylloweralkyl, pyridinyl, loweralkylcarbonyl, arylloweralkylcarbonyl, heteroarylloweralkylcarbonyl, trifluoromethylcarbonyl or arylcarbonyl; andR.sub.2 is hydrogen, loweralkyl, loweralkoxycarbonyl, aminoloweralkylcarbonyl, loweralkylaminoloweralkylcarbonyl or diloweralkylaminoloweralkylcarbonyl;which are useful as modulators of neurotransmitter function such as serotonergic and adrenergic, and as such are useful as antidepressants and for the treatment of personality disorders such as obsessive compulsive disorders.Type: GrantFiled: September 23, 1991Date of Patent: April 13, 1993Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Richard C. Effland, Joseph T. Klein
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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: 5185350Abstract: This invention relates to substituted pyridinylamino-1H-indoles, 1H-indazoles, 2H-indazoles, benzo[b]thiophenes and 1,2-benzisothiazoles of the formula ##STR1## wherein Q is S, N or NR.sub.2 ;Y is CH, N or NR.sub.2 ;R.sub.1 is hydrogen, loweralkyl, loweralkynyl, loweralkenyl, arylloweralkyl, loweralkoxycarbonylaminoloweralkylcarbonyl, arylloweralkoxycarbonylaminoloweralkylcarbonyl, aminoloweralkylcarbonyl, loweralkoxycarbonyl or acyl;R.sub.2 is hydrogen or loweralkyl;R.sub.3 is hydrogen or loweralkyl;X is hydrogen, loweralkyl, halogen; andn is 0 or 1; or a pharmaceutically acceptable acid addition salt thereof.The compounds of this invention are useful in the treatment of memory dysfunctions characterized by a cholinergic deficit such as the type associated with Alzheimer's disease and other memory disorders.Type: GrantFiled: September 23, 1991Date of Patent: February 9, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Richard C. Effland, Joseph T. Klein, Lawrence L. Martin
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Patent number: 5179204Abstract: This invention relates to N-heteroaryl-4-pyrimidinamines of the formula ##STR1## where R.sub.1 is hydrogen, loweralkyl, aryl, or arylloweralkyl; R.sub.2 and R.sub.3 are independently hydrogen or loweralkyl, or R.sub.2 and R.sub.3 taken together are aryl; R.sub.4 and R.sub.5 are independently hydrogen or loweralkyl, or R.sub.4 and R.sub.5 taken together are aryl; X is hydrogen, halogen, cyano, nitro, amino, loweralkyl, loweralkoxy, trifluoromethyl or ##STR2## where Y is hydrogen, halogen or loweralkyl; m is an integer of 1 to 3; and the pharmaceutically acceptable acid addition salts thereof and where applicable the geometrical and optical isomers and racemic mixtures thereof. The compounds of this invention display utility as memory enhancing agents and as analgesic agents.Type: GrantFiled: September 18, 1990Date of Patent: January 12, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Richard C. Effland, Joseph T. Klein, Larry Davis, Gordon E. Olsen
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Patent number: 5179119Abstract: This invention relates to 1,3-dihydro-1-(pyridinylamino)-2H-indol-2-ones of the formula ##STR1## where R.sub.1, R.sub.2 and R.sub.3 are independently hydrogen, loweralkyl, aryl, arylloweralkyl or heteroarylloweralkyl selected from the group consisting of pyridinylmethyl, pyridinylethyl, thienylmethyl, thienylethyl; or R.sub.2 and R.sub.3 together form a cycloalkane ring of 4 to 6 carbons or a spiro-fused aryl cycloalkane or heterocycloalkyl selected from the group consisting of piperidine and tetrahydropyran; X and Y are independently hydrogen, halogen, hydroxy, loweralkyl, loweralkoxy, nitro, amino or trifluoromethyl; m and n are independently integers of 1 to 3, the pharmaceutically acceptable acid addition salts thereof and, where applicable the optical, geometrical and stereoisomers and racemic mixtures thereof. The compounds of this invention display utility as analgesics, anticonvulsants, for enhancing memory and for the treatment of Alzheimer's disease.Type: GrantFiled: July 26, 1991Date of Patent: January 12, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Richard C. Effland, David G. Wettlaufer
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Patent number: 5179099Abstract: This invention relates to 2,3-dihydro-1-(pyridinylamino)-indoles of the formula ##STR1## wherein R.sub.1 is hydrogen, loweralkyl, aryl, arylloweralkyl, alkenyl, alkynyl or heteroarylloweralkyl selected from the group consisting of pyridinylmethyl, pyridinylethyl, thienylmethyl, thienylethyl; R.sub.2 and R.sub.3 and independently hydrogen, loweralkyl, aryl, arylloweralkyl or heteroarylloweralkyl selected from the group consisting of pyridinylmethyl, pyridinylethyl, thienylmethyl, thienylethyl; or R.sub.2 and R.sub.3 together form a cycloalkane ring of 4 to 6 carbons or a spiro-fused aryl or heteroaryl; the term heteroaryl signifying a group selected from pyridine or thiophene; X and Y are independently hydrogen, halogen, hydroxy, loweralkyl, loweralkoxy, nitro, amino or trifluoromethyl; m and n are independently integers of 1 to 3, or a pharmaceutically acceptable acid addition salt thereof or where appropriate, an optical, geometrical or stereoisomer or racemic mixture thereof.Type: GrantFiled: May 24, 1991Date of Patent: January 12, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Richard C. Effland, David G. Wettlaufer, Joseph T. Klein
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Patent number: 5177088Abstract: There are disclosed various compounds of the formula below, ##STR1## where 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 function 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 disorders.Type: GrantFiled: April 17, 1991Date of Patent: January 5, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Richard C. Effland, Joseph T. Klein, Lawrence L. Martin