Patents by Inventor Alan D. Palkowitz
Alan D. Palkowitz 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: 6391901Abstract: This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula I, and the use of defined compounds of formula I as thrombin inhibitors.Type: GrantFiled: January 21, 2000Date of Patent: May 21, 2002Assignee: Eli Lilly and CompanyInventors: Nickolay Y Chirgadze, Michael L Denney, Matthew J Fisher, Robert J Foglesong, Richard W Harper, Mary G Johnson, Ho-Shen Lin, Michael P Lynch, Jefferson R McCowan, Shawn C Miller, Alan D Palkowitz, Michael E Richett, Daniel J Sall, Gerald F Smith, Kumiko Takeuchi, Minsheng Zhang
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Patent number: 6355632Abstract: The present invention provides pharmaceutically active compounds formula I wherein R1 is —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), or —OSO2(C2-C6 alkyl); R2 is —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), —OSO2(C2-C6 alkyl), or halo; R3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; and n is 2 or 3; and or a pharmaceutically acceptable salt thereof. Also provided are compounds of formula II wherein R1a is —H or —OR5 in which R5 is a hydroxy protecting group. R2a is —H, halo, or —OR6 in which R6 is a hydroxy protecting group; and R4 is —OH or —CHO; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: May 3, 2000Date of Patent: March 12, 2002Assignee: Eli Lilly and CompanyInventor: Alan D. Palkowitz
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Patent number: 6350774Abstract: This application relates to novel compounds of formula (I) (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula (I), and the use of the compounds of formula (I) as thrombin inhibitors.Type: GrantFiled: January 24, 2000Date of Patent: February 26, 2002Assignee: Eli Lilly And CompanyInventors: Nicholas J Bach, Jolie A. Bastian, Nickolay Y Chirgadze, Michael L Denney, Robert J. Foglesong, Richard W Harper, Mary G Johnson, Ho-Shen Lin, Michael P Lynch, Jefferson R McCowan, Alan D Palkowitz, Daniel J Sall, Gerald F Smith, Kumiko Takeuchi, Minsheng Zhang
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Patent number: 6329342Abstract: The present invention is directed to methods for the modulation of cardiac function which comprise the administration of certain compounds, as defined herein, having growth hormone secretagogue activity.Type: GrantFiled: February 18, 2000Date of Patent: December 11, 2001Assignee: Eli Lilly and CompanyInventors: Raymond F. Kauffman, Alan D. Palkowitz
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Patent number: 6288105Abstract: This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula I, and the use of the compounds of formula I as thrombin inhibitors.Type: GrantFiled: February 3, 2000Date of Patent: September 11, 2001Assignee: Eli Lilly and CompanyInventors: Nickolay Y Chirgadze, Matthew J Fisher, Richard W Harper, Ho-Shen Lin, Jefferson R McCowan, Alan D Palkowitz, Daniel J Sall, Gerald F Smith, Kumiko Takeuchi, Minsheng Zhang
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Patent number: 6284756Abstract: This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula I, and the use of the compounds of formula I as thrombin inhibitors.Type: GrantFiled: January 21, 2000Date of Patent: September 4, 2001Assignee: Eli Lilly and CompanyInventors: Nickolay Y Chirgadze, Richard W Harper, Todd J Kohn, Ho-Shen Lin, Jefferson R McCowan, Alan D Palkowitz, Daniel J Sall, Gerald F Smith, Kumiko Takeuchi, Michael R Wiley, Minsheng Zhang
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Patent number: 6271227Abstract: This application relates to novel compounds of formula (I) (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula (I), and the use of the compounds of formula (I) as thrombin inhibitors.Type: GrantFiled: January 24, 2000Date of Patent: August 7, 2001Assignee: Eli Lilly and CompanyInventors: Nickolay Y Chirgadze, Matthew J Fisher, Richard W Harper, Ho-Shen Lin, Jefferson R McCowan, Alan D Palkowitz, Michael E Richett, Daniel J Sall, Gerald F Smith, Kumiko Takeuchi, Minsheng Zhang
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Patent number: 6268361Abstract: The present invention is related to methods for treating pathological conditions resulting from an estrogen deficiency, such as cardiovascular disease and osteoporosis, and is further related to methods for treating estrogen-dependent cancer, such as breast and uterine cancer, employing compounds of formula IType: GrantFiled: June 6, 1995Date of Patent: July 31, 2001Inventor: Alan D. Palkowitz
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Patent number: 5998401Abstract: A class of substituted phenoxy naphthalene compounds of the structure: ##STR1## where n is 2 or 3; R.sup.1 is hydrogen, hydroxy, C.sub.1 -C.sub.4 alkoxy, phenoxycarbonyl, C.sub.1 -C.sub.6 alkoxycarbonyl, or C.sub.2 -C.sub.6 alkoxy-sulfonyl; R.sup.2 is is hydrogen, hydroxy, C.sub.1 -C.sub.4 alkoxy, phenoxycarbonyl, C.sub.1 -C.sub.6 alkoxycarbonyl, or C.sub.2 -C.sub.6 alkoxy-sulfonyl, or halo; and R.sup.3 is 1-piperidinyl, 1-pyrollidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; are useful in the treatment of pathological conditions associated with post-menopause including osteoporosis, endometriosis, uterine fibroid disease, cardiovascular disease (particularly hyperlipidemia), and hormonally-dependent cancers (particularly breast and uterine cancer).Type: GrantFiled: February 28, 1995Date of Patent: December 7, 1999Assignee: Eli Lilly and CompanyInventor: Alan D. Palkowitz
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Patent number: 5712390Abstract: The present invention provides processes for preparing compounds of formula I ##STR1## and for preparing compounds of formula VII ##STR2## Also provided are processes for preparing compounds of formula VII in addition to intermediates of formula IX ##STR3## wherein R.sup.1' is --OH, or --OR.sup.3, in which R.sup.3 is a hydroxy protecting group; andZ is bromo, iodo, triflate, or --B(OH).sub.2.Type: GrantFiled: October 27, 1995Date of Patent: January 27, 1998Assignee: Eli Lilly and CompanyInventors: Kenneth L. Hauser, Alan D. Palkowitz, Daniel J. Sall, Kenneth J. Thrasher
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Patent number: 5710285Abstract: The present invention provides useful intermediates for preparing 2-(substituted phenyl)benzothiophenes compounds said intermediates having the structure ##STR1## wherein R.sup.1 ' is --OH, or --OR.sup.3, in which R.sup.3 is a hydroxy protecting group; andZ is bromo, iodo, triflate, or --B(OH).sub.2 with the proviso that when Z is bromo or iodo, R1' is not alkoxy.Type: GrantFiled: October 27, 1995Date of Patent: January 20, 1998Assignee: Eli Lilly and CompanyInventors: Kenneth L. Hauser, Alan D. Palkowitz, Daniel J. Sall, Kenneth J. Thrasher
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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: 5614639Abstract: The present invention provides processes for preparing 2-substituted benzo[b]thiophene compounds, some of which are useful as intermediates for preparing pharmaceutically-active compounds and others which are useful, inter alia, for the treatment of osteoporosis in postmenopausal women.Type: GrantFiled: March 31, 1995Date of Patent: March 25, 1997Assignee: Eli Lilly and CompanyInventors: Kenneth L. Hauser, Alan D. Palkowitz, Daniel J. Sall, Kenneth J. Thrasher
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Patent number: 5612360Abstract: This invention provides novel heterocyclic derivatives, their pharmaceutical formulations, and their use for antagonizing angiotensin II receptors in mammals.Type: GrantFiled: April 20, 1993Date of Patent: March 18, 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: 5604236Abstract: Selected acid functional beta-carboline type derivatives effective as thromboxane synthase inhibitors having the formula: ##STR1## where R.sub.1 and R.sub.2 are monovalent radicals, --(L.sub.a)-- is a linking group of 4 to 8 chain atoms, and A is an acidic group.Type: GrantFiled: May 5, 1995Date of Patent: February 18, 1997Assignee: Eli Lilly and CompanyInventors: Joseph A. Jakubowski, Alan D. Palkowitz
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Patent number: 5574190Abstract: The present invention provides pharmaceutically active compounds formula I ##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.2 -C.sub.6 alkyl);R.sup.2 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), --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl), or halo;R.sup.3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; andn is 2 or 3; and or a pharmaceutically acceptable salt thereof.Also provided are compounds of formula II ##STR2## wherein R.sup.1a is --H or --OR.sup.5 in which R.sup.5 is a hydroxy protecting group.R.sup.2a is --H, halo, or --OR.sup.6 in which R.sup.6 is a hydroxy protecting group; andR.sup.4 is --OH or --CHO;or a pharmaceutically acceptable salt thereof.Type: GrantFiled: June 6, 1995Date of Patent: November 12, 1996Assignee: Eli Lilly and CompanyInventor: Alan D. Palkowitz
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Patent number: 5569768Abstract: This invention provides novel heterocyclic derivatives, their pharmaceutical formulations, and their use for antagonizing angiotensin II receptors in mammals.Type: GrantFiled: May 31, 1995Date of Patent: October 29, 1996Assignee: 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: 5567712Abstract: The present invention provides pharmaceutically active compounds formula I ##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.2 -C.sub.6 alkyl);R.sup.2 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), --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl), or halo;R.sup.3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; andn is 2 or 3; andor a pharmaceutically acceptable salt thereof.Also provided are compounds of formula II ##STR2## wherein R.sup.1a is --H or --OR.sup.5 in which R.sup.5 is a hydroxy protecting group.R.sup.2a is --H, halo, or --OR.sup.6 in which R.sup.6 is a hydroxy protecting group; andR.sup.4 is --OH or --CHO;or a pharmaceutically acceptable salt thereof.Type: GrantFiled: June 6, 1995Date of Patent: October 22, 1996Assignee: Eli Lilly and CompanyInventor: Alan D. Palkowitz
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Patent number: 5556981Abstract: 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: September 17, 1996Assignee: 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, Venkatraghaven Vasudevan, Celia A. Whitesitt
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Patent number: 5550118Abstract: Selected acid functional polyhydronorharman type derivatives effective as thromboxane synthase inhibitors having the formula: ##STR1## where R.sub.1 and R.sub.2 are monovalent radicals, --(L.sub.a)-- is a linking group of 4 to 8 chain atoms, and A is an acidic group.Type: GrantFiled: January 31, 1994Date of Patent: August 27, 1996Assignee: Eli Lilly and CompanyInventors: Joseph A. Jakubowski, Alan D. Palkowitz, Sandra K. Sigmund