Patents Represented by Attorney, Agent or Law Firm Janelle D. Strode
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Patent number: 5840747Abstract: A method for antagonizing or blocking calcium channels in vascular tissue, comprising administering to an animal in need thereof a pharmaceutically-effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, C.sub.1 -C.sub.4 alkyl, --CO--(C.sub.1 -C.sub.6 alkyl), or --CH.sub.2 Ar, --CO--Ar, wherein Ar is phenyl or substituted phenyl;R.sup.2 is selected from the group consisting of pyrrolidine, hexamethylenemino, and piperidino; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: June 7, 1995Date of Patent: November 24, 1998Assignee: Eli Lilly and CompanyInventor: Marlene L. Cohen
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Patent number: 5834488Abstract: The invention provides dihydrobenzo?b!indenothiophene compounds, intermediates, processes, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, cardiovascular-related pathological conditions including hyperlipidemia and related cardiovascular pathologies, and estrogen-dependent cancer.Type: GrantFiled: September 19, 1997Date of Patent: November 10, 1998Assignee: Eli Lilly and CompanyInventors: Michael Gregory Bell, Brian Stephen Muehl, Mark Alan Winter
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Patent number: 5821253Abstract: The invention provides tetrahydrobenzo?a!fluorene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions, including hyperlipidemia.Type: GrantFiled: September 24, 1997Date of Patent: October 13, 1998Assignee: Eli Lilly and CompanyInventors: Henry Uhlman Bryant, George Joseph Cullinan
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Patent number: 5811421Abstract: The present invention provides compounds of formula ##STR1## wherein R.sup.1 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), or --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl);R.sup.2 is C.sub.1 -C.sub.6 alkyl or C.sub.5 -C.sub.7 cycloalkyl which is optionally substituted with 1 to 3 substitutents selected from the group consisting of C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, hydroxy, amino, nitro, and halo;X is --CH(OH)-- or --CH.sub.2 --;M is --CH.sub.2 CH.sub.2 -- or --CH.dbd.CH--;n is 2 or 3; andR.sup.3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino; or a pharmaceutically acceptable salt thereof. Also provided are methods of using the compounds of the present invention for the treatment of various medical indications associated with post-menopausal syndrome, uterine fibroid disease, endometriosis, and aortal smooth muscle cell proliferation.Type: GrantFiled: July 16, 1996Date of Patent: September 22, 1998Assignee: Eli Lilly and CompanyInventors: Jeffrey Alan Dodge, Kennan Joseph Fahey, Charles David Jones, Charles Willis Lugar, III
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Patent number: 5808061Abstract: The present invention provides a novel process for preparing a compound of formula I ##STR1## wherein R.sup.1 and R.sup.2 combine to form C.sub.4 -C.sub.6 polymethylene, --CH.sub.2 CH(CH.sub.3)CH.sub.2 CH.sub.2 --, --CH.sub.2 C(CH.sub.3).sub.2 CH.sub.2 CH.sub.2 --, or --CH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 --; or a pharmaceutically acceptable salt or solvate thereof.Also provided intermediates of formulae II and IV ##STR2## wherein Z is a leaving group.Type: GrantFiled: July 17, 1995Date of Patent: September 15, 1998Assignee: Eli Lilly and CompanyInventors: Jeffrey A. Dodge, Mark G. Stocksdale
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Patent number: 5792762Abstract: The invention provides dihydronaphthofluorene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions.Type: GrantFiled: September 19, 1997Date of Patent: August 11, 1998Assignee: Eli Lilly and CompanyInventors: Henry Uhlman Bryant, Thomas Alan Crowell, Charles David Jones
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Patent number: 5792797Abstract: A pharmaceutical compound of the formula ##STR1## in which R is hydrogen, halo or F.sub.2 HCO--;or a salt, amide or ester thereof.Type: GrantFiled: February 25, 1997Date of Patent: August 11, 1998Assignee: Lilly Industries LimitedInventors: Peter Thaddeus Gallagher, William Martin Owton, Andrew Caerwyn Williams
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Patent number: 5792798Abstract: Methods of inhibiting plasminogen activator inhibitor 1 comprising administering to a human in need thereof an effective amount of a compound having the formula I: ##STR1## wherein R.sup.1 and R.sup.2 are, independently, --H, --C.sub.1 -C.sub.4 alkyl, or taken together with the nitrogen to which they are attached form a pyrrolidine, piperidine, or hexamethyleneimino ring;or a pharmaceutically acceptable salt or solvate thereof.Type: GrantFiled: July 15, 1997Date of Patent: August 11, 1998Assignee: Eli Lilly and CompanyInventors: David Thompson Berg, George Joseph Cullinan, Brian William Grinnell, Mark Alan Richardson
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Patent number: 5770612Abstract: The present invention provides a method of alleviating one or more menstrual symptoms in a woman comprising administering to said woman in need of treatment an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, --CH.sub.3, --CO--(C.sub.1 -C.sub.6 alkyl), or --CO--Ar in which Ar is optionally substituted phenyl; andR.sup.2 is selected from the group consisting of pyrrolidino, hexamethyleneimino and piperidino; or a pharmaceutically acceptable salt or solvate thereof.The present invention also provides the aforementioned method and further comprises administering to said woman an effective amount of at least one pharmaceutical agent selected from the group consisting of an analgesic, a diuretic, and an antihistamine, and compositions therefore.Type: GrantFiled: May 16, 1995Date of Patent: June 23, 1998Assignee: Eli Lilly and CompanyInventor: Steven A. Fontana
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Patent number: 5760030Abstract: The instant invention provides novel benzothiophene compounds, pharmaceutical formulations, and methods of use.Type: GrantFiled: June 30, 1997Date of Patent: June 2, 1998Assignee: Eli Lilly and CompanyInventors: Henry Uhlman Bryant, George Joseph Cullinan, Kennan Joseph Fahey
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Patent number: 5760061Abstract: The present invention provides a method of alleviating one or more menstrual symptoms in a woman comprising administering to said woman in need of treatment an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, --CH.sub.3, --CO--(C.sub.1 -C.sub.6 alkyl), or --CO--Ar in which Ar is optionally substituted phenyl; andR.sup.2 is selected from the group consisting of pyrrolidino, hexamethyleneimino and piperidino; or a pharmaceutically acceptable salt or solvate thereof.The present invention also provides the aforementioned method and further comprises administering to said woman an effective amount of at least one pharmaceutical agent selected from the group consisting of an analgesic, a diuretic, and an antihistamine, and compositions therefore.Type: GrantFiled: May 16, 1995Date of Patent: June 2, 1998Assignee: Eli Lilly and CompanyInventor: Steven A. Fontana
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Process for preparing benzoic acid derivative intermediates and benzothiophene pharmaceutical agents
Patent number: 5750688Abstract: Novel processes are provided for producing compounds of formula II ##STR1## wherein R.sup.1 and R.sup.2 each are independently C.sub.1 -C.sub.4 alkyl, or combine to form piperidinyl, pyrrolidinyl, methylpyrrolidinyl, dimethylpyrrolidinyl, morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino;R.sup.3 and R.sup.4 each are H or a hydroxy protecting group; andn is 2 or 3;or a pharmaceutically acceptable salt thereof by reacting a haloalkylamine with a phenolic ester in the presence of an alkylacetate solvent and a base.Type: GrantFiled: April 9, 1996Date of Patent: May 12, 1998Assignee: Eli Lilly and CompanyInventors: Douglas P. Kjell, Fred M. Perry -
Patent number: 5750708Abstract: The present invention is directed to compounds of Formula I: ##STR1## wherein: n is 2 or 3;R is dimethylamino, diethylamino, 1-piperidinyl, 1-pyrrolidinyl, 4-morpholinyl, or 1-hexamethyleneimino;R.sup.1 is hydrogen, loweralkyl of C.sub.1 -C.sub.4, phenyl, or mono or di-substituted phenyl wherein each substituent is independently halo, methyl, hydroxy, C.sub.1 -C.sub.6 -alkoxy, benzyloxy, C.sub.1 -C.sub.6 -alkanoyloxy, benzoyloxy, substituted benzoyloxy bearing 1 to 3 substituents each of which is independently halo, C.sub.1 -C.sub.4 -loweralkyl, or C.sub.1 -C.sub.4 -loweralkoxy, C.sub.1 -C.sub.5 -alkoxycarbonyloxy, or C.sub.4 -C.sub.6 -alkylsulfonyloxy;R.sup.2 is hydrogen, hydroxy, C.sub.1 -C.sub.6 -alkoxy, benzyloxy, C.sub.1 -C.sub.6 -alkanoyloxy, benzoyloxy, substituted benzoyloxy bearing 1 to 3 substituents each of which is independently halo, C.sub.1 -C.sub.4 -loweralkyl, or C.sub.1 -C.sub.4 -loweralkoxy, C.sub.1 -C.sub.5 -alkoxycarbonyloxy, or C.sub.4 -C.sub.Type: GrantFiled: April 15, 1997Date of Patent: May 12, 1998Assignee: Eli Lilly and CompanyInventors: Henry Uhlman Bryant, Don Richard Finley, Ken Matsumoto
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Process for preparing benzoic acid derivative intermediates and benzothiophene pharmaceutical agents
Patent number: 5731436Abstract: Processes for producing benzothiophenes employing ethylene carbonate or propylene carbonate are provided.Type: GrantFiled: August 31, 1994Date of Patent: March 24, 1998Assignee: Eli Lilly and CompanyInventor: Douglas P. Kjell -
Patent number: 5726186Abstract: The present invention provides compounds of formula I: ##STR1## wherein X is --O-- or --S--,Y is --O--, --S--, --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, or --NR.sup.5 --;R.sup.1, R.sup.2, and R.sup.3 are each independently --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl), --OSO.sub.2 CF.sub.3, Cl, or F;n is 1 or 2;W is CH.sub.2 or C.dbd.O;R.sup.4 is 1-piperidinyl, 2-oxo-1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 2-oxo-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino;R.sup.5 is C.sub.1 -C.sub.3 alkyl, --COC.sub.6 H.sub.5, --CO(C.sub.1 -C.sub.6 alkyl), --C(O)OC.sub.6 H.sub.5, --C(O)O(C.sub.1 -C.sub.6 alkyl), --SO.sub.2 (C.sub.1 -C.sub.6 alkyl), --SO.sub.2 C.sub.6 H.sub.5, or --SO.sub.2 CF.sub.3 ;or a pharmaceutically acceptable salt or solvate thereof.Type: GrantFiled: August 13, 1996Date of Patent: March 10, 1998Assignee: Eli Lilly and CompanyInventor: Timothy Alan Grese
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Patent number: 5705507Abstract: This invention relates to the fields of pharmaceutical and organic chemistry and provides novel 3-benzyl-benzofurans which are .alpha.-substituted with ether, thioether, amino, hydrazino, cyano or halo that are useful for the treatment of the various medical indications associated with post-menopausal syndrome, as well as estrogen dependent diseases including cancer of the breast, uterus and cervix. The present invention further relates to intermediate compounds and processes useful for preparing the pharmaceutically active compounds of the present invention, and pharmaceutical compositions.Type: GrantFiled: September 29, 1995Date of Patent: January 6, 1998Assignee: Eli Lilly and CompanyInventor: Brian S. Muehl
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Patent number: 5693633Abstract: This invention provides novel heterocyclic derivatives, their pharmaceutical formulations, and their use for antagonizing angiotensin II receptors in mammals.Type: GrantFiled: May 30, 1995Date of Patent: December 2, 1997Assignee: Eli Lilly and CompanyInventors: Donald B. Boyd, Sherryl L. Lifer, Winston S. Marshall, Alan D. Palkowitz, William Pfeifer, Jon K. Reel, Richard L. Simon, Mitchell I. Steinberg, K. Jeff Thrasher, Venkatraghavan Vasudevan, Celia A. Whitesitt
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Patent number: 5674887Abstract: The administration of a xanthine oxidase inhibitor is effective for the treatment or prevention of the excessive resorption of bone in conditions such as osteoporosis and the like.Type: GrantFiled: February 22, 1995Date of Patent: October 7, 1997Assignees: Eli Lilly and Company, London Hospital Medical College, St. George's Hospital Medical SchoolInventors: David R. Blake, Jill A. Panetta, Mone Zaidi
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Patent number: 5672609Abstract: The present invention is directed to compounds of Formula I: ##STR1## wherein: n is 2 or 3;R is dimethylamino, diethylamino, 1-piperidinyl, 1-pyrrolidinyl, 4-morpholinyl, or 1-hexamethyleneimino;R.sup.1 is hydrogen, loweralkyl of C.sub.1 -C.sub.4, phenyl, or mono or di-substituted phenyl wherein each substituent is independently halo, methyl, hydroxy, C.sub.1 -C.sub.6 -alkoxy, benzyloxy, C.sub.1 -C.sub.6 -alkanoyloxy, benzoyloxy, substituted benzoyloxy bearing 1 to 3 substituents each of which is independently halo, C.sub.1 -C.sub.4 -loweralkyl, or C.sub.1 -C.sub.4 -loweralkoxy, C.sub.1 -C.sub.5 -alkoxycarbonyloxy, or C.sub.4 -C.sub.6 -alkylsulfonyloxy;R.sup.2 is hydrogen, hydroxy, C.sub.1 -C.sub.6 -alkoxy, benzyloxy, C.sub.1 -C.sub.6 -alkanoyloxy, benzoyloxy, substituted benzoyloxy bearing 1 to 3 substituents each of which is independently halo, C.sub.1 -C.sub.4 -loweralkyl, or C.sub.1 -C.sub.4 -loweralkoxy, C.sub.1 -C.sub.5 -alkoxycarbonyloxy, or C.sub.4 -C.sub.Type: GrantFiled: July 18, 1996Date of Patent: September 30, 1997Assignee: Eli Lilly and CompanyInventors: Henry Uhlman Bryant, Don Richard Finley, Ken Matsumoto
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Patent number: 5668172Abstract: A pharmaceutical compound of the formula ##STR1## in which R is hydrogen, halo or F.sub.2 HCO--; or a salt, amide or ester thereof, useful in the treatment of skeletal diseases.Type: GrantFiled: August 23, 1995Date of Patent: September 16, 1997Assignee: Lilly Industries LimitedInventors: Peter Thaddeus Gallagher, William Martin Owton, Andrew Caerwyn Williams