Patents Represented by Attorney, Agent or Law Firm MaCharri Vorndran-Jones
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Patent number: 8124776Abstract: The present invention provides for novel compounds of formula I wherein X is S or S(O); R1 and R2 are each independently selected from the group consisting of —CH2CH3 and phenyl; or R1 and R2 combine to form morpholino; and processes to prepare arzoxifene.Type: GrantFiled: March 3, 2008Date of Patent: February 28, 2012Assignee: Eli Lilly and CompanyInventors: Charles Arthur Alt, Douglas Patton Kjell, Tony Yantao Zhang, Fu-Yao Zhang, Jared Wade Fennell, Kevin Dale Seibert
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Patent number: 7655641Abstract: The present invention is directed to a compound of Formula (I): and pharmaceutically acceptable salts, solvates, hydrates or stereoisomers thereof, which are useful in treating or preventing disorders mediated by a peroxisome proliferator activated receptor (PPAR) such as syndrome X, type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, arteriosclerosis, and other disorders related to syndrome X and cardiovascular diseases.Type: GrantFiled: February 10, 2004Date of Patent: February 2, 2010Assignee: Eli Lilly and CompanyInventors: Scott Eugene Conner, Lynn Stacy Gossett, Jonathan Edward Green, Winton Dennis Jones, Jr., Nathan Bryan Mantlo, Donald Paul Matthews, Daniel Ray Mayhugh, Daryl Lynn Smith, Jennifer Ann Vance, Xiaodong Wang, Alan M Warshawsky, Leonard Larry Winneroski, Jr., Yanping Xu, Guoxin Zhu
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Patent number: 7608639Abstract: The present invention is directed to a compound of formula (I), or a pharmaceutically acceptable salt, solvate, hydrate or stereoisomer thereof, which is useful in treating or preventing disorders mediated by a peroxisome proliferator activated receptor (PPAR), such as syndrome X, type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, arteriosclerosis, and other disorders related to syndrome X and cardiovascular diseases.Type: GrantFiled: October 8, 2004Date of Patent: October 27, 2009Assignee: Eli Lilly and CompanyInventors: Leonard Larry Winneroski, Jr., Yanping Xu, Jeremy Schulenburg York
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Patent number: 7598266Abstract: The present invention is directed to compounds represented by the following structural formula, Formula I: wherein: (a) X is selected from the group consisting of a single bond, O, S, S(O)2 and N; (b) U is an aliphatic linker; (c) Y is selected from the group consisting of C, O, S, NH and a single bond; (d) E is C(R3)(R4)A or A and wherein (i) A is selected from the group consisting of carboxyl, tetrazole, C1-C6 alkylnitrile, carboxamide, sulfonamide and acylsulfonamide; (e) B is selected from the group consisting of S, O, C, and N; (f) Z is selected from the group consisting of N and C; with the proviso that when B is C then Z is N.Type: GrantFiled: April 9, 2008Date of Patent: October 6, 2009Assignee: Eli Lilly and CompanyInventors: Scott Eugene Conner, Nathan Bryan Mantlo, Guoxin Zhu
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Patent number: 7585977Abstract: The present invention relates to a selective estrogen receptor modulator of formula I or a pharmaceutical acid addition salt thereof; useful, e.g., for treating endometriosis and/or uterine leiomyoma/leiomyomata.Type: GrantFiled: April 9, 2008Date of Patent: September 8, 2009Assignee: Eli Lilly and CompanyInventors: Robert Dean Dally, Jeffrey Alan Dodge, Scott Alan Frank, Scott Alan Jones, Timothy Alan Shepherd, Owen Brendan Wallace, Kin Chlu Fong, Conrad Wilson Hummel, George Sal Lewis
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Patent number: 7566803Abstract: The present invention relates to novel, non-secosteroidal, diaryl compounds with vitamin D receptor (VDR) modulating activity that are less hypercalcemic than 1?,25 dihydroxy vitamin D3. These compounds are useful for treating bone disease and psoriasis.Type: GrantFiled: November 20, 2003Date of Patent: July 28, 2009Assignee: Eli Lilly and CompanyInventor: Jianliang Lu
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Patent number: 7544812Abstract: The present invention is directed to compounds represented by the following structural Formula (I), (a) R1 is selected from the group consisting of hydrogen, substituted or unsubstituted group selected from C1-C8 alkyl, aryl-C0-4-alkyl, heteroaryl-C0-4-alkyl, C3-C6 cycloalkylaryl-C0-2-alkyl, and —CH2—C(O)—R17-R18, wherein R17 is O or NH and R18 is optionally substituted benzyl; (b) R2 is selected from the group consisting of C1-C6 alkyl, C1-C6 alkenyl, aryl-C0-4-alkyl, heteroaryl-C0-4-alkyl, C1-C4 alkyl sulfonamide, C1-C4 alkyl amide, OR10 and C3-C6 cycloalkyl; (c) W is O or S; (d) X is an optionally substituted C1-C5 alkylene linker wherein one carbon atom of the linker may optionally be replaced with O, NH, S, and optionally two carbons together may form a double bond; (e) Y is selected from the group consisting of C, O, S, NH and a single bond; and (f) E is selected from the group consisting of C(R3)(R4)A, A, and a substituted or unsubstituted group selected from the group consisting of (CH2)n COOR19.Type: GrantFiled: November 26, 2002Date of Patent: June 9, 2009Assignee: Eli Lilly and CompanyInventors: Tracey Ann Gibson, Richard Duane Johnston, Nathan Bryan Mantlo, Richard Craig Thompson, Leonard Larry Winneroski, Yanping Xu, Xiaodong Wang
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Patent number: 7544707Abstract: The present invention is directed to compounds represented by the following structural formula, Formula (I), and stereoisomers, pharmaceutically acceptable salts, solvates and hydrates thereof, wherein: (a) R2 is selected from the group consisting of C0-C8 alkyl and C1-4-heteroalkyl; (b) X is selected from the group consisting of a single bond, O, S, S(O)2 and N; (c) U is an aliphatic linker wherein one carbon atom of the aliphatic linker is optionally replaced with O, NH or S, and wherein such aliphatic linker is optionally substituted with from one to four substituents each independently selected from R30; (d) Y is selected from the group consisting of C, O, S, NH and a single bond; and (e) E is C(R3)(R4)A or A.Type: GrantFiled: December 16, 2004Date of Patent: June 9, 2009Assignee: Eli Lilly and CompanyInventors: Scott Eugene Connor, Nathan Bryan Mantlo, Guoxin Zhu, Robert Jason Herr
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Patent number: 7507832Abstract: The present invention is directed to compounds represented by the following structural formula, Formula (I): wherein: (a) X is selected from the group consisting of a single bond, O, S, S(O)2 and N; (b) U is an aliphatic linker; (c) Y is selected from the group consisting of O, C, S, NH and a single bond; (d) W is N, O or S; (e) E is C(R3)(R4)A or A and wherein; (f) A is selected from the group consisting of carboxyl, tetrazole, C1-C6 alkylnitrile, carboxamide, sulfonamide and acylsufonamide. The other substituents are defined in the claims; the compounds are modulators of peroxisome proleferator activated receptors (PPARs) and are useful for the treatment of diabetes and other metabolic disorders.Type: GrantFiled: December 21, 2004Date of Patent: March 24, 2009Assignee: Eli Lilly and CompanyInventors: Nathan Bryan Mantlo, Antonio Navarro, Ashraf Saeed, Douglas Linn Gernert, Tianwei Ma, Lance Allen Pfeifer
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Patent number: 7504433Abstract: The present invention is directed to compounds represented by the following structural formula, Formula I: and stereoisomers, pharmaceutically acceptable salts, solvates and hydrates thereof, wherein: (a) X is selected from the group consisting of O, S, S(O)2, N, and a bond; (b) U is an aliphatic linker wherein one carbon atom of the aliphatic linker may be replaced with O, NH or S, and wherein such aliphatic linker is optionally substituted with R30; (c) Y is selected from the group consisting of C, O, S, NH and a single bond; and (d) E is C(R3)(R4)A or A.Type: GrantFiled: December 31, 2003Date of Patent: March 17, 2009Assignee: Eli Lilly and CompanyInventors: Nathan Bryan Mantlo, Xiaodong Wang, Guoxin Zhu
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Patent number: 7396850Abstract: The present invention is directed to a compound, {2-Methyl-4-[3-methyl-1-(4-trifluoromethyl-phenyl)-1H-pyrazol-4-ylmethylsulfanyl]-phenoxy}-acetic acid and pharmaceutical uses thereof.Type: GrantFiled: December 31, 2003Date of Patent: July 8, 2008Assignee: Eli Lilly and CompanyInventors: Scott Eugene Conner, Nathan Bryan Mantlo, Daniel Ray Mayhugh, Guoxin Zhu
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Patent number: 7384965Abstract: The present invention is directed to compounds represented by the following structural formula, Formula I: wherein (a) X is selected from the group consisting of a single bond, O, S, S(O)2 and N; (b) U ia an aliphatic linker; (c) Y is selected from the group consisting of C, O, S, NH and a single bond; (d) E is C(R3) (R4) A or A and wherein (i) A is selected from the group consisting of carboxyl, tetrazole, C1-C6 alkylnitrile, carboxamidek, sulfonamide and acylsulfonamide; (e) B is selected from the group consisting of S, O, C, and N; (f) Z is selected from the group consisting of N and C; with the proviso that when B is C then Z is N.Type: GrantFiled: December 31, 2003Date of Patent: June 10, 2008Assignee: Eli Lilly and CompanyInventors: Scott Eugene Conner, Nathan Bryan Mantlo, Guoxin Zhu
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Patent number: 7351728Abstract: Compounds represented by the following structural formula (I), and pharmaceutically acceptable salts, solvates and hydrates thereof, wherein R1 is an unsubstituted or substituted aryl, heteroaryl, cycloalkyl, aryl-alkyl, heteroaryl-alkyl or cycloalkyl-alkyl, R2 is H, alkyl or haloalkyl, the polymethylene chain (II), is saturated or may contain a carbon-carbon double bond, while n is 2, 3, 4, W is O or S, Y is an unsubstituted phenylene, naphthylene or 1, 2, 3, 4 tetrahydronaphthylene, R3 is II, alkyl or haloalkyl, R4 is II, alkyl, haloalkyl or a substituted or unsubstituted benzyl, are useful for modulating a peroxisome proliferator activated receptor, particularly in the treatment of diabetes mellitus.Type: GrantFiled: July 14, 2005Date of Patent: April 1, 2008Assignee: Eli Lilly and CompanyInventors: Dawn Alisa Brooks, Scott Eugene Conner, Samuel James Dominianni, Alexander Glenn Godfrey, Lynn Stacy Gossett, Christopher John Rito, Allie Edward Tripp, Alan M. Warshawsky, Leonard Larry Winneroski, Jr., Guoxin Zhu
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Patent number: 7345070Abstract: Compounds represented by the following structural formula (I), and pharmaceutically acceptable salts, solvates and hydrates thereof, wherein: n is 2, 3, or 4 and W is CH2, CH(OH), C(O) or O; R1 is an unsubstituted or substituted aryl, heteroaryl, cycloalkyl, heterocycloalkyl, aryl-alkyl, heteroaryl-alkyl, cycloalkyl-alkyl, or t-butyl; R2 is H, alkyl, haloalkyl or phenyl; Y is an unsubstituted or substituted thiophen-2,5-diyl or phenylene; R3 is alkyl or haloalkyl; R4 is a substituted or unsubstituted phenyl, naphthyl, 1,2,3,4-tetrahydronaphthyl, quinolyl, pyridyl or benzo[1,3]dioxol-5-yl group; and R5 is H, alkyl, or aminoalkyl; are useful for modulating a peroxisome proliferator activated receptor, particularly in the treatment of diabetes mellitus.Type: GrantFiled: February 9, 2005Date of Patent: March 18, 2008Assignee: Eli Lilly and CompanyInventors: Dawn Alisa Brooks, Alexander Glenn Godfrey, Sarah Beth Jones, James Ray McCarthy, Christopher John Rito, Leonard Larry Winneroski, Yanping Xu
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Patent number: 7321056Abstract: The present invention is directed to a novel compound, its composition and use of a compound having a structural formula (I), or a pharmaceutically acceptable salt, solvate, hydrate or stereoisomers thereof, which is useful in treating or preventing disorders mediated by a peroxisome proliferator activated receptor (PPAR) such as syndrome X, type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, arteriosclerosis, and other disorders related to syndrome X and cardiovascular diseasesType: GrantFiled: December 8, 2004Date of Patent: January 22, 2008Assignee: Eli Lilly and CompanyInventors: Rafael Ferritto Crespo, Maria Dolores Martin-Ortega Finger
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Patent number: 7304062Abstract: The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts, solvates and hydrates thereof, R1 is a substituted or unsubstituted group selected from C1-C8 alkyl, aryl-C0-2-alkyl, heteroaryl-C0-2-alkyl, C3-C6 cycloalkylaryl-C0-2-alkyl or phenyl. W is O or S. R2 is H or a substituted or unsubstituted group selected from C1-C6 alkyl, C3-C6 cycloalkyl and heteroaryl. X is a C2-C5 alkylene linker wherein one carbon atom of the linker may be replaced with O, NH or S. Y is C, O, S, NH or a single bond. Furthermore, E is (CH2)nCOOH, wherein n is 0, 1, 2 or 3, or C(R3)(R4)A, wherein A is an acidic functional group such as carboxyl, carboxamide substituted or unsubstituted sulfonamide, or substituted or unsubstituted tetrazole. R3 is H, saturated or unsaturated C1-C5 alkyl, C1-C5 alkoxy.Type: GrantFiled: November 9, 2001Date of Patent: December 4, 2007Assignee: Eli Lilly and CompanyInventors: Samuel James Dominianni, Garret Jay Etgen, Richard Duane Johnston, Nathan Bryan Mantlo, Daniel Ray Mayhugh, Ashraf Saeed, Richard Craig Thompson, Xiaodong Wang, Christopher Randall Schmid, Yanping Xu
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Patent number: 7282501Abstract: The present invention is directed to a compound of formula I, and pharmaceutically acceptable salts, solvates, hydrates or stereoisomer thereof, which are useful in treating Syndrome X, Type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, arteriosclerosis, and other disorders related to Syndrome X as well as cardiovascular diseases.Type: GrantFiled: May 24, 2002Date of Patent: October 16, 2007Assignee: Eli Lilly and CompanyInventors: Lynn Stacy Gossett, Jonathan Edward Green, James Robert Henry, Winton Dennis Jones, Donald Paul Matthews, Quanrong Shen, Daryl Lynn Smith, Jennifer Ann Vance, Alan M. Warshawsky
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Patent number: 7220880Abstract: The present invention is directed to compounds, compositions, and use of compounds the structural Formula (I)Type: GrantFiled: June 11, 2003Date of Patent: May 22, 2007Assignee: Eli Lilly and CompanyInventors: Rafael Ferritto Crespo, Jose Alfredo Martin, Maria Dolores Martin-Ortega Finger, Isabel Rojo Garcia, Quanrong Shen, Alan M Warshawsky, Yanping Xu
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Patent number: 7205321Abstract: The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts, solvates and hydrates thereof, R1 is selected from the group consisting of hydrogen, substituted or unsubstituted group selected from C1–C8 alkyl, aryl-C0-4-alkyl, heteroaryl-C0-4-alkyl, and C3–C6 cycloalkylaryl-C0-2-alkyl; W is O or S; X is an optionally substituted C1–C5 alkylene linker wherein one carbon atom of the linker may be replaced with O, NH or S; Y is C, O, S, NH or a single bond; E is C(R3)(R4)A or AType: GrantFiled: November 13, 2002Date of Patent: April 17, 2007Assignee: Eli Lilly and CompanyInventors: Richard Duane Johnston, Nathan Bryan Mantlo, Richard Craig Thompson
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Patent number: 7176224Abstract: Novel compounds that are modulators of PPAR receptors, and pharmaceutically acceptable salts, solvates and hydrates thereof, processes for making the compounds, pharmaceutical compositions containing the compounds, or pharmaceutically acceptable salts, solvates and hydrates thereofType: GrantFiled: August 23, 2001Date of Patent: February 13, 2007Assignee: Eli Lilly and CompanyInventors: Robert J Ardecky, Dawn Alisa Brooks, Alexander Glenn Godfrey, Sarah Beth Jones, Nathan Bryan Mantlo, James Ray McCarthy, Pierre Yves Michellys, Christopher John Rito, John S Tyhonas, Leonard Larry Winneroski, Yanping Xu