Patents by Inventor Daniel R. Pilipauskas
Daniel R. Pilipauskas 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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Publication number: 20090149431Abstract: A novel crystalline form (Form L) of the aldosterone receptor antagonist drug eplerenone is provided having relatively high physical stability at normal temperatures of storage and use. Pharmaceutical compositions are also provided comprising Form L eplerenone, optionally accompanied by one or more other solid state forms of eplerenone, in a total unit dosage amount of eplerenone of about 10 to about 1000 mg, and further comprising one or more pharmaceutically acceptable excipients. Processes are provided for preparing Form L eplerenone and for preparing compositions comprising Form L eplerenone. A method for prophylaxis and/or treatment of an aldosterone-mediated condition or disorder is also provided, comprising administering to a subject a therapeutically effective amount of eplerenone, wherein at least a fraction of the eplerenone present is Form L eplerenone.Type: ApplicationFiled: February 18, 2009Publication date: June 11, 2009Inventors: Kathleen P. Barton, Thomas B. Borchardt, Marlow V. Carlos, Subhash Desai, Leonard J. Ferro, Henry T. Gaud, Scott S. Ganser, Clay R. Little, Partha S. Mudipalli, Mark A. Pietz, Daniel R. Pilipauskas, Yuen-Lung L. Sing, Glenn L. Stahl, Joseph J. Wieczorek, Chris Y. Yan
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Publication number: 20030083493Abstract: A novel crystalline form (Form L) of the aldosterone receptor antagonist drug eplerenone is provided having relatively high physical stability at normal temperatures of storage and use. Pharmaceutical compositions are also provided comprising Form L eplerenone, optionally accompanied by one or more other solid state forms of eplerenone, in a total unit dosage amount of eplerenone of about 10 to about 1000 mg, and further comprising one or more pharmaceutically acceptable excipients. Processes are provided for preparing Form L eplerenone and for preparing compositions comprising Form L eplerenone. A method for prophylaxis and/or treatment of an aldosterone-mediated condition or disorder is also provided, comprising administering to a subject a therapeutically effective amount of eplerenone, wherein at least a fraction of the eplerenone present is Form L eplerenone.Type: ApplicationFiled: July 9, 2002Publication date: May 1, 2003Inventors: Kathleen P. Barton, Thomas B. Borchardt, Marlon V. Carlos, Subhash Desai, Leonard J. Ferro, Henry T. Gaud, Scott S. Ganser, Clay R. Little, Partha S. Mudipalli, Mark A. Pietz, Daniel R. Pilipauskas, Yuen-Lung L. Sing, Glenn L. Stahl, Joseph J. Wieczorek, Chris Y. Yan
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Publication number: 20020045746Abstract: A novel crystalline form (Form L) of the aldosterone receptor antagonist drug eplerenone is provided having relatively high physical stability at normal temperatures of storage and use. Pharmaceutical compositions are also provided comprising Form L eplerenone, optionally accompanied by one or more other solid state forms of eplerenone, in a total unit dosage amount of eplerenone of about 10 to about 1000 mg, and further comprising one or more pharmaceutically acceptable excipients. Processes are provided for preparing Form L eplerenone and for preparing compositions comprising Form L eplerenone. A method for prophylaxis and/or treatment of an aldosterone-mediated condition or disorder is also provided, comprising administering to a subject a therapeutically effective amount of eplerenone, wherein at least a fraction of the eplerenone present is Form L eplerenone.Type: ApplicationFiled: December 7, 2000Publication date: April 18, 2002Inventors: Kathleen P. Barton, Thomas B. Borchardt, Marlon V. Carlos, Subhash Desai, Leonard J. Ferro, Henry T. Gaud, Scott S. Ganser, Clay R. Little, Partha S. Mudipalli, Mark A. Pietz, Daniel R. Pilipauskas, Yuen-Lung L. Sing, Glenn L. Stahl, Joseph J. Wieczorek, Chris Y. Yan
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Publication number: 20020038021Abstract: A novel crystalline form (Form H) of the aldosterone receptor antagonist drug eplerenone is provided having a relatively rapid dissolution rate in aqueous media. Also provided are novel solvated crystalline forms of eplerenone that, when desolvated, can yield Form H eplerenone. Also provided is amorphous eplerenone. Pharmaceutical compositions are provided comprising Form H eplerenone, optionally accompanied by one or more other solid state forms of eplerenone, in a total unit dosage amount of eplerenone of about 10 to about 1000 mg, and further comprising one or more pharmaceutically acceptable excipients. Processes are provided for preparing Form H eplerenone and for preparing compositions comprising Form H eplerenone. A method for prophylaxis and/or treatment of an aldosterone-mediated condition or disorder is also provided, comprising administering to a subject a therapeutically effective amount of eplerenone, wherein at least a fraction of the eplerenone present is Form H eplerenone.Type: ApplicationFiled: December 7, 2000Publication date: March 28, 2002Inventors: Kathleen P. Barton, Thomas B. Borchardt, Marlon V. Carlos, Subhash Desai, Leonard J. Ferro, Henry T. Gaud, Scott S. Ganser, Clay R. Little, Partha S. Mudipalli, Mark A. Pietz, Daniel R. Pilipauskas, Yuen-Lung L. Sing, Glenn L. Stahl, Joseph J. Wieczorek, Chris Y. Yan
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Patent number: 5631399Abstract: The present invention relates to a novel process for the preparation of ethyl 3S-[[4-[[4-(aminoiminomethyl)phenyl]amino]-1,4-dioxobutyl]amino]-4-pentyno ate and pharmaceutically acceptable acid addition salt thereof.Type: GrantFiled: May 14, 1996Date of Patent: May 20, 1997Assignee: G. D. Searle & Co.Inventors: Kevin A. Babiak, Srinivasan Babu, James R. Behling, Mark L. Boys, Kimberly J. Cain-Janicki, Wendel W. Doubleday, Payman Farid, Timothy J. Hagen, E. A. Hallinan, Donald W. Hansen, Jr., Donald E. Korte, Kathleen T. Mc Laughlin, John R. Medich, Sean T. Nugent, Vlasdislav Orlovski, Jung M. Park, Karen B. Peterson, Daniel R. Pilipauskas, Barnett S. Pitzele, Sofya Tsymbalov, Glenn L. Stahl
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Patent number: 5536869Abstract: The present invention relates to a novel process for the preparation of ethyl 3S-[[4-[[4-(aminoiminomethyl)phenyl]amino]-1,4-dioxobutyl]amino]-4-pentyno ate and pharmaceutically acceptable acid addition salt thereof which comprises treating (trimethylsilyl)acetylene sequentially with n-butyllithium and 4-formylmorpholine followed by acid hydrolysis to give 3-(trimethylsilyl)-2-propynal; treating 3-(trimethylsilyl)-2-propynal with lithium bis(trimethylsilyl)amide to give in situ N,3-bis(trimethylsilyl)-2-propyn-1-imine; condensation of N,3-bis(trimethylsilyl)-2-propyn-1-imine with lithium t-butyl acetate to give (.+-.)1,1-dimethylethyl 3-amino-5-(trimethylsilyl)-4-pentynoate; treating (.+-.)1,1-dimethylethyl 3-amino-5-(trimethylsilyl)-4-pentynoate- with p-toluenesulfonic acid to give (.+-.)1,1-dimethylethyl 3-amino-5-(trimethylsilyl)-4-pentynoate, mono p-toluenesulfonic acid salt, treatment of resulting salt with ethanol in the presence of p-toluenesulfonic acid to give (.+-.Type: GrantFiled: July 14, 1995Date of Patent: July 16, 1996Assignee: G. D. Searle & Co.Inventors: Kevin A. Babiak, Srinivasan Babu, James R. Behling, Mark L. Boys, Kimberly J. Cain-Janicki, Wendel W. Doubleday, Payman Farid, Timothy J. Hagen, E. Ann Hallinan, Donald W. Hansen, Jr., Donald E. Korte, Kathleen T. McLaughlin, John R. Medich, Sean T. Nugent, Vlasdislav Orlovski, Jung M. Park, Karen B. Peterson, Daniel R. Pilipauskas, Barnett S. Pitzele, Sofya Tsymbalov, Glenn L. Stahl
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Patent number: 4797470Abstract: This invention relates to compounds of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sup.1 is ##STR2## where X is oxygen or sulfur, Y is oxygen or nitrogen, and R.sup.11 represents straight or branched chain lower alkenyl having 2-6 carbon atoms, or phenyl, benzyl, and their equivalents such as nitro, halogen, or lower alkyl or lower alkoxy substituted phenyl or benzyl; wherein R.sup.2 and R.sup.3 may be the same or different and represent straight or branched chain lower alkyl having 1-6 carbon atoms, wherein R.sup.4 -R.sup.9 may be the same or different and represent hydrogen, or straight or branched chain lower alkyl having 1-6 carbon atoms; wherein C.sub.w is an asymmetric carbon atom when R.sup.7 and R.sup.8 are not the same and may be racemic or have the D or L configuration; and wherein C.sup.v is an asymmetric carbon atom and may be racemic or may have the D or L configuration.Type: GrantFiled: February 13, 1987Date of Patent: January 10, 1989Assignee: G. D. Searle & Co.Inventors: Barnett S. Pitzele, Donald W. Hansen, Jr., Robert W. Hamilton, Daniel R. Pilipauskas, Michael Clare
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Patent number: 4767744Abstract: This invention relates to novel substituted tyrosyl alanine dipeptide amides of the formula: ##STR1## and the pharmaceutically acceptable addition salts thereof, wherein R.sup.1 is --OH, --OCH.sub.3 or lower alkoxy of 1-6 carbon atoms; wherein R.sup.2 and R.sup.3 may be the same or different and represent straight or branched chain lower alkyl of 1-6 carbon atoms; wherein R.sup.4, R.sup.5 R.sup.9 may be the same or different and represent hydrogen or straight or branched chain lower alkyl having 1-6 carbon atoms; wherein R.sup.6 represents hydrogen, or straight or branched chain lower alkyl of 1-6 carbon atoms, or R.sup.6 may act together with N.sup.6, C.sup.w and either R.sup.7 R.sup.8 to form a cycloamine of the formula: ##STR2## such that between R.sup.7 and R.sup.8, when one acts to form said cycloamine, the other is hydrogen, or straight or branched chain lower alkyl of 1-6 carbon atoms; wherein when neither R.sup.7 nor R.sup.8 is acting to form said cycloamine, R.sup.7 R.sup.8 act together with C.sup.Type: GrantFiled: February 13, 1987Date of Patent: August 30, 1988Assignee: G. D. Searle & Co.Inventors: Donald W. Hansen, Jr., Daniel R. Pilipauskas, Michael Clare
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Patent number: 4760180Abstract: This invention encompasses compounds of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sup.1 is lower alkoxy or --O--(CH.sub.2).sub.n -phenyl where the phenyl may be optionally substituted with halogen, --NO.sub.2, --CN, --NH.sub.2 or lower alkyl wherein n is 1 to 4; R.sup.2 and R.sup.3 represent lower alkyl, halogen, lower alkoxy or one of R.sup.2 or R.sup.3 is hydrogen and the other is lower alkyl, lower alkoxy, or halogen; R.sup.4, R.sup.5, R.sup.7, R.sup.8, and R.sup.9 represent hydrogen or lower alkyl, R.sup.6 represents hydrogen, lower alkyl, lower alkenyl, or --(CH.sub.2).sub.m -cycloalkyl wherein m is 1 to 4 and the cycloalkyl has 3 to 8 carbon atoms; R.sup.10 is --(CH.sub.2).sub.p -phenyl wherein p is 1 to 4; and v represents an asymmetric carbon that may be racemic or have the D or L Configuration; w represents an asymmetric carbon when R.sup.7 and R.sup.8 are not the same that may be racemic or have the D or L configuration.Type: GrantFiled: July 14, 1986Date of Patent: July 26, 1988Assignee: G. D. Searle & Co.Inventors: Barnett S. Pitzele, Donald W. Hansen, Jr., Robert W. Hamilton, Daniel R. Pilipauskas, Michael Clare
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Patent number: 4757153Abstract: The invention relates to novel substituted tyrosyl alanine dipeptide amides of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sup.1 is hydrogen, lower alkyl, hydroxy, lower alkoxy, --O(CH.sub.2).sub.n phenyl with the phenyl optionally substituted by halogen, --NO.sub.2, --CN, --NH.sub.2 or lower alkyl wherein n is 1 to 4; R.sup.2 and R.sup.3 represent lower alkyl, halogen, or lower alkoxy, or either one of R.sup.2 or R.sup.3 is hydrogen and the other is lower alkyl, lower alkoxy or halogen; R.sup.4, R.sup.5, R.sup.6, and R.sup.9 may be the same or different and represent hydrogen, lower alkyl, cycloalkyl having 3 to 8 carbons, unsaturated lower alkyl, or --(CH.sub.2).sub.m cycloalkyl with the cycloalkyl having 3 to 8 carbons and m is 1 to 4; R.sup.10 is hydrogen or --(CH.sub.2).sub.p phenyl or with the phenyl optionally substituted with --NH.sub.2, --OH, halogen, --NO.sub.2, or lower alkyl or --(CH.sub.2).sub.p thienyl wherein p is 1 to 4; one of R.sup.7 or R.Type: GrantFiled: July 14, 1986Date of Patent: July 12, 1988Assignee: G. D. Searle & Co.Inventors: Donald W. Hansen, Jr., Daniel R. Pilipauskas, Michael Clare
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Patent number: 4727189Abstract: The invention relates to novel substituted tyrosyl alanine dipeptide amides of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sub.1 represents straight or branched lower alkyl having 1 to 4 carbons;R.sub.2 represents hydrogen, hydroxy, --OCO.sub.2 R.sub.1 substituent or lower alkyl having 1 to 4 carbons;R.sub.3 represents a hydrogen or lower alkyl having 1 to 6 carbons;R.sub.4 and R.sub.5 may be the same or different and represent hydrogen or lower alkyl having 1 to 6 carbons;n is 1 to 6;X represents a hydrogen, hydroxy or OCO.sub.2 R.sub.1 substituent;A represents a cyclohexyl, phenyl or phenyl substituted with one or more lower alkyls containing 1 to 6 carbons, one or more amino, hydroxy, halogen, nitro or lower alkoxy substituent having 1 to 6 carbons;V represents the asymmetric carbon that may be racemic or have the D or L configuration;W represents the asymmetric carbon when R.sub.4 and R.sub.Type: GrantFiled: April 14, 1986Date of Patent: February 23, 1988Assignee: G. D. Searle & Co.Inventors: Donald W. Hansen, Jr., Robert H. Mazur, Daniel R. Pilipauskas
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Patent number: 4599325Abstract: The invention relates to novel substituted tyrosyl alanine dipeptide amides of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sub.1 represents straight or branched lower alkyl having 1 to 4 carbons;R.sub.2 represents hydrogen, hydroxy, --OCO.sub.2 R.sub.1 substituent or lower alkyl having 1 to 4 carbons;R.sub.3 represents a hydrogen or lower alkyl having 1 to 6 carbons;R.sub.4 and R.sub.5 may be the same or different and represent hydrogen or lower alkyl having 1 to 6 carbons;n is 1 to 6;X represents a hydrogen, hydroxy or OCO.sub.2 R.sub.1 substituent;A represents a cyclohexyl, phenyl or phenyl substituted with one or more lower alkyls containing 1 to 6 carbons, one or more amino, hydroxy, halogen, nitro or lower alkoxy substituent having 1 to 6 carbons;V represents the asymmetric carbon that may be racemic or have the D or L configuration;W represents the asymmetric carbon when R.sub.4 and R.sub.Type: GrantFiled: January 22, 1985Date of Patent: July 8, 1986Assignee: G. D. Searle & Co.Inventors: Donald W. Hansen, Jr., Robert H. Mazur, Daniel R. Pilipauskas