189333-18-4Relevant academic research and scientific papers
Solid dispersions containing an apoptosis-inducing agent
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Page/Page column 190, (2019/03/15)
A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound of Formula I as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises dissolving the compound, the polymeric carrier and the surfactant in a suitable solvent, and removing the solvent to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.
Aryl substituted aminotetrahydropyran compound and use thereof
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Paragraph 0250; 0252; 0253; 0254, (2019/07/04)
The invention relates to an aryl substituted aminotetrahydropyran compound and use thereof, and further relates to a pharmaceutical composition comprising the compound. The compound or pharmaceuticalcomposition provided by the invention can be used as a dipeptidyl peptidase-IV (DPP-IV) inhibitor.
Design, synthesis, and evaluation of novel and selective G-protein coupled receptor 120 (GPR120) spirocyclic agonists
Cox, Jason M.,Chu, Hong D.,Chelliah, Mariappan V.,Debenham, John S.,Eagen, Keith,Lan, Ping,Lombardo, Matthew,London, Clare,Plotkin, Michael A.,Shah, Unmesh,Sun, Zhongxiang,Vaccaro, Henry M.,Venkatraman, Srikanth,Suzuki, Takao,Wang, Nengxue,Ashley, Eric R.,Crespo, Alejandro,Madeira, Maria,Leung, Dennis H.,Alleyne, Candice,Ogawa, Aimie M.,Souza, Sarah,Thomas-Fowlkes, Brande,Di Salvo, Jerry,Weinglass, Adam,Kirkland, Melissa,Pachanski, Michele,Powles, Mary Ann,Tozzo, Effie,Akiyama, Taro E.,Ujjainwalla, Feroze,Tata, James R.,Sinz, Christopher J.
supporting information, p. 49 - 54 (2017/12/12)
Type 2 diabetes mellitus (T2DM) is an ever increasing worldwide epidemic, and the identification of safe and effective insulin sensitizers, absent of weight gain, has been a long-standing goal of diabetes research. G-protein coupled receptor 120 (GPR120) has recently emerged as a potential therapeutic target for treating T2DM. Natural occurring, and more recently, synthetic agonists have been associated with insulin sensitizing, anti-inflammatory, and fat metabolism effects. Herein we describe the design, synthesis, and evaluation of a novel spirocyclic GPR120 agonist series, which culminated in the discovery of potent and selective agonist 14. Furthermore, compound 14 was evaluated in vivo and demonstrated acute glucose lowering in an oral glucose tolerance test (oGTT), as well as improvements in homeostatic measurement assessment of insulin resistance (HOMA-IR; a surrogate marker for insulin sensitization) and an increase in glucose infusion rate (GIR) during a hyperinsulinemic euglycemic clamp in diet-induced obese (DIO) mice.
SUBSTITUTED SPIROPIPERIDINYL COMPOUNDS USEFUL AS GPR120 AGONISTS
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Page/Page column 36; 39, (2014/05/07)
The present invention relates to a compound represented by formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing diabetes, hyperlipidemia, obesity, inflammation related disorders, and related diseases and conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR120. Pharmaceutical compositions and methods of treatment are also included.
TETRAHYDROPYRAZOLOPYRIMIDINE COMPOUNDS
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Paragraph 0499, (2014/01/07)
Embodiments of the disclosure relate to tetrahydropyrazolopyrimidine compounds that act as antagonists or inhibitors for Toll-like receptors 7 and/or 8, and their use in pharmaceutical compositions effective for treatment of systemic lupus erythematosus (SLE) and lupus nephritis
SUBSTITUTED ACETYL-COA CARBOXYLASE INHIBITORS
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Page/Page column 17-18, (2012/11/07)
The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof; wherein G is R1, R2 and R3 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.
Synthesis of 7-oxo-dihydrospiro[indazole-5,4′-piperidine] acetyl-CoA carboxylase inhibitors
Bagley, Scott W.,Southers, James A.,Cabral, Shawn,Rose, Colin R.,Bernhardson, David J.,Edmonds, David J.,Polivkova, Jana,Yang, Xiaojing,Kung, Daniel W.,Griffith, David A.,Bader, Scott J.
experimental part, p. 1497 - 1506 (2012/03/26)
Synthesis of oxo-dihydrospiroindazole-based acetyl-CoA carboxylase (ACC) inhibitors is reported. The dihydrospiroindazoles were assembled in a regioselective manner in six steps from substituted hydrazines and protected 4-formylpiperidine. Enhanced regios
N1-PYRAZOLOSPIROKETONE ACETYL-COA CARBOXYLASE INHIBITORS
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Page/Page column 21; 22, (2011/05/16)
The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3 and R4 are as described herein; pharmaceutical compositions there-of; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl- CoA carboxylase enzyme(s) in an animal
N2-PYRAZOLOSPIROKETONE ACETYL-COA CARBOXYLASE INHIBITORS
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Page/Page column 42; 43, (2011/06/16)
The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of said compound, wherein R1, R2, R3 and R4 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl- CoA carboxylase enzyme(s) in an animal.
Substituted Disulfonamide Compounds
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Page/Page column 31, (2010/06/22)
Substituted disulfonamide compounds corresponding to formula I: In which R1, R2, R3, R4a, R4b, R5a, R5b, R8, R9a, R9b, R10, R11, a, b, s, t and A have defined meanings, pharmaceutical compositions containing one or more such compounds, processes for preparing such compounds, and a method of using such compounds for the treatment or inhibition of pain and/or other conditions mediated by the bradykinin receptor 1 (BR1).
