Eli Lilly and Company

Nathan Bryan Mantlo

Guoxin Zhu

Xiaodong Wang

Scott Eugene Conner

Daniel Ray Mayhugh

Yanping Xu

Alan M Warshawsky

Leonard Larry Winneroski, Jr

Richard Craig Thompson

Richard Duane Johnston

Michael Gregory Bell

Robert Jason Herr

Tianwei Ma

Ana Maria Escribano

Jeffrey Michael Schkeryantz

Peter Ambrose Lander

James Allen Knobelsdorf

Douglas Linn Gernert

Maria Carmen Fernandez

Ashraf Saeed

Ana Isabel Mateo Herranz

Todd Fields

Eva Maria Martin De La Nava

Guoqing Cao

James R McCarthy

Donald Paul Matthews

Robert J Ardecky

Christopher J Rito

Christopher Cioffi

Samuel James Dominianni

John S Tyhonas

Winton Dennis Jones, Jr

Alexander Glenn Godfrey

Daryl Lynn Smith

Lynn Stacy Gossett

Quanrong Shen

Ryan Edward Stites

Sean Richard Dinn

Dawn Alisa Brooks

Lance Allen Pfeifer

Jonathan Edward Green

Lindsay Stelzer

Xinchao Chen

Christopher Randall Schmid

Michael James Genin

Fucheng Qu

Robert Anthony Doti

Jason Matthew Ochoada

Sarah Beth Jones

Jennifer Ann Vance

Antonio Navarro

Tracey Ann Gibson

Pierre Yves Michellys

Garret Jay Etgen

Matthew Scott Dowling

Scott Eugene Connor

Saravanan Parthasarathy

Christopher Lawrence Cioffi

Lindsay Scott Stelzer

Ana Isabel Mateo-Herranz

The present invention provides a compound of Formula II:  or a pharmaceutically acceptable salt thereof.

Pyrazole compounds

Compounds of formula (I) wherein variables are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and related diseases. 

Compounds and methods for modulating FXR

Compounds of formula I wherein n, m, p, q, Y, RR, R, R, R, R, and Rare as defined herein and their pharmaceutical compositions and methods of use are disclosed.

Compounds and method for treating dyslipidemia

Compounds of formula I wherein n, m, p, q, y, RR, R, R, R, and Rare as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating artherosclerosis and its sequelae.

Compounds and methods for treating dislipidemia

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. 

Sulfonamide derivatives as PPAR modulators

The present invention is directed to compounds represented by the following structural formula, Formula I: wherein:

Fused heterocyclic derivatives as PPAR modulators

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 C-Calkyl and C-heteroalkyl; (b) X is selected from the group consisting of a single bond, O, S, S(O)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.

Bicyclic derivatives as PPAR modulators

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 C-Calkyl, aryl-C-alkyl, heteroaryl-C-alkyl, C-Ccycloalkylaryl-C-alkyl, and &#x2014;CH&#x2014;C(O)&#x2014;R17-R18, wherein R17 is O or NH and R18 is optionally substituted benzyl; (b) R2 is selected from the group consisting of C-Calkyl, C-Calkenyl, aryl-C-alkyl, heteroaryl-C-alkyl, C-Calkyl sulfonamide, C-Calkyl amide, OR10 and C-Ccycloalkyl; (c) W is O or S; (d) X is an optionally substituted C-Calkylene 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 (CH)n COOR19. 

Peroxisome proliferator activated receptor agonists

The present invention is directed to a method of treatment by modulating a peroxisome proliferator activated receptor by employing a compound of Structural Formula (I). The variables in I are defined herein. Also included are compounds, methods of making compounds, and pharmaceutical compositions. The compounds of the present invention are believed to be effective in treating and preventing Syndrome X, Type H diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, atherosclerosis, and other disorders related to Syndrome X and cardiovascular diseases.

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)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, C-Calkylnitrile, 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.

Triazole PPAR modulators

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.

Thiophene derivative PPAR modulators

The present invention discloses compounds of formula (I) wherein A, n, q, K, W, X, Y; Z, R, R, R, R, R, and Rare as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and its sequelae.

Compounds and methods for treating dyslipidemia

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.

Pyrazole derivative as PPAR modulator

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)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, C-Calkylnitrile, 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.

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 C-Calkyl, aryl-C-alkyl, heteroaryl-C-alkyl, C-Ccycloalkylaryl-C-alkyl or phenyl. W is O or S. R2 is H or a substituted or unsubstituted group selected from C-Calkyl, C-Ccycloalkyl and heteroaryl. X is a C-Calkylene 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 (CH)COOH, 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 C-Calkyl, C-Calkoxy. Additionally, R4 is H, halo, a substituted or unsubstituted group selected from C-Calkyl, C-Calkoxy, C-Ccycloalkyl, arylC-Calkyl and phenyl, or R3 and R4 are combined to form a C-Ccycloalkyl.

Peroxisome proliferator activated receptor alpha agonists

Growing community of inventors

Brownsburg, IN, United States of America

Nathan Bryan Mantlo