- Conformationally constrained phosphotyrosyl mimetics designed as monomeric Src homology 2 domain inhibitors
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Inhibitors of specific src homology 2 (SH2) domain binding interactions could potentially afford new therapeutic approaches toward a variety of diseases, including several cancers. To date SH2 domain inhibitors have been confined to small phosphotyrosyl (
- Burke Jr.,Barchi Jr.,George,Wolf,Shoelson,Yan
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Read Online
- Indanylacetic acids as PPAR-δ activator insulin sensitizers
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A series of indane acetic acid derivatives were prepared which show a spectrum of activity as insulin sensitizers and PPAR-α and PPAR-δ ligands. In vivo data are presented for insulin sensitizers with selectivity for PPAR-δ over PPAR-α.
- Wickens, Philip,Zhang, Chengzhi,Ma, Xin,Zhao, Qian,Amatruda, John,Bullock, William,Burns, Michael,Cantin, Louis-David,Chuang, Chih-Yuan,Claus, Thomas,Dai, Miao,Dela Cruz, Fernando,Dickson, David,Ehrgott, Frederick J.,Fan, Dongping,Heald, Sarah,Hentemann, Martin,Iwuagwu, Christiana I.,Johnson, Jeffrey S.,Kumarasinghe, Ellalahewage,Ladner, David,Lavoie, Rico,Liang, Sidney,Livingston, James N.,Lowe, Derek,Magnuson, Steve,Mannelly, Gretchen,Mugge, Ingo,Ogutu, Herbert,Pleasic-Williams, Susan,Schoenleber, Robert W.,Shapiro, Jeff,Shelekhin, Tatiana,Sweet, Laurel,Town, Christopher,Tsutsumi, Manami
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- METHODS OF TREATING OR PREVENTING COGNITIVE IMPAIRMENT USING INDANE ACETIC ACID DERIVATIVES BASED ON APOE4 GENOTYPE
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The present invention provides indane acetic acid and their derivatives and methods for the treating and/or preventing of cognitive disorders based on the ApoE4 genotype of human subjects.
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- METHODS OF DOSE ADMINISTRATION FOR TREATING OR PREVENTING COGNITIVE IMPAIRMENT USING INDANE ACETIC ACID DERIVATIVES
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The present invention provides indane acetic acid and their derivatives and methods for the treating and/or preventing of cognitive disorders.
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- Isothiazole derivatives as GPR120 agonists for the treatment of type II diabetes
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Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR120 receptor. Such compounds are represented by Formula (I) as follows: wherein R1, G, and Q are defined herein.
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- ISOTHIAZOLE DERIVATIVES AS GPR120 AGONISTS FOR THE TREATMENT OF TYPE II DIABETES
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Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR120 receptor. Such compounds are represented by Formula (I) as follows: wherein R1, G, and Q are defined herein.
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- GPR120 AGONISTS FOR THE TREATMENT OF TYPE II DIABETES
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Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR120 receptor. Such compounds are represented by Formula (I) and Formula (II) as follows: wherein Y, R1, G, and Q are defined herein; and wherein R11, R21, R41, RB1 and G1, are defined herein.
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- CYCLIC AMINE SUBSTITUTED OXAZOLIDINONE CETP INHIBITOR
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CCompounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compound of Formula I, A3 is a substitiuted phenyl group or indanyl group.Formula (I)
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Page/Page column 46; 47
(2012/05/19)
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- BRIDGED AND FUSED HETEROCYCLIC ANTIDIABETIC COMPOUNDS
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This invention provides for certain bridged and fused heterocyclic compounds of the formula (I) or a pharmaceutically acceptable salt, ester solvate or prodrug thereof wherein: L is: (II) and the other variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.
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- Indanylacetic acid derivatives carrying aryl-pyridyl and aryl-pyrimidinyl tail groups-new classes of PPAR γ/δ and PPAR α/γ/δ agonists
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Modulation of PPAR activities represents an attractive approach for the treatment of diabetes with associated cardiovascular complications. The indanylacetic acid structural motif has proven useful in the generation of potent and tunable PPAR ligands. Mod
- Cantin, Louis-David,Liang, Sidney,Ogutu, Herbert,Iwuagwu, Christiana I.,Boakye, Ken,Bullock, William H.,Burns, Michael,Clark, Roger,Claus, Thomas,delaCruz, Fernando E.,Daly, Michelle,Ehrgott, Frederick J.,Johnson, Jeffrey S.,Keiper, Christine,Livingston, James N.,Schoenleber, Robert W.,Shapiro, Jeffrey,Town, Christopher,Yang, Ling,Tsutsumi, Manami,Ma, Xin
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p. 1056 - 1061
(2007/10/03)
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- Indanylacetic acid derivatives carrying 4-thiazolyl-phenoxy tail groups, a new class of potent PPAR α/γ/δ pan agonists: Synthesis, structure-activity relationship, and in vivo efficacy
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Compounds that simultaneously activate the three peroxisome proliferator-activated receptor (PPAR) subtypes alpha, gamma, and delta hold potential to address the adverse metabolic and cardiovascular conditions associated with diabetes and the metabolic sy
- Rudolph, Joachim,Chen, Libing,Majumdar, Dyuti,Bullock, William H.,Burns, Michael,Claus, Thomas,Dela Cruz, Fernando E.,Daly, Michelle,Ehrgott, Frederick J.,Johnson, Jeffrey S.,Livingston, James N.,Schoenleber, Robert W.,Shapiro, Jeffrey,Yang, Ling,Tsutsumi, Manami,Ma, Xin
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p. 984 - 1000
(2007/10/03)
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- INDANE, DIHYDROBENZOFURAN, AND TETRAHYDRONAPHTHALENE CARBOXYLIC ACID DERIVATIVES AND THEIR USE AS ANTIDIABETICS
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This invention relates to novel indane, dihydrobenzofuran, and tetrahydronaphthalene carboxylic acid derivatives whice are useful in the treatment of diseases such sa diabetes, diabetes-related disorders, obesity, hyperlipidemia, and cardiovascular diseases. The invention also relates to intermediates useful in preparation of said carboxylic derivatives and to methods of preparation.
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- Indane acetic acid derivatives and their use as pharmaceutical agents, intermediates, and method of preparation
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This invention relates to novel indane acetic acid derivatives which are useful in the treatment of diseases such as diabetes, obesity, hyperlipidemia, and atherosclerotic diseases. The invention also relates to intermediates useful in preparation of indane acetic derivatives and to methods of preparation.
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