- LILY OF THE VALLEY ODORANT
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The present invention concerns the use as perfuming ingredient of a compound of formula (I) in the form of any one of its stereoisomers or a mixture thereof, and wherein X represents a CHO group when R1 represents a C1-2 alkyl group
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Page/Page column 16
(2019/08/08)
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- Delta opiate receptor antagonist, application thereof and medicine composition
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The invention discloses a compound with a structure shown as a general formula (I) (the general formula is shown in the description), a pharmaceutical salt, hydrate or metabolite formed through metabolism in any form, application of the compound with the
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Paragraph 0221-0224
(2019/07/04)
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- Br?nsted Acid-Catalyzed Intramolecular Hydroarylation of β-Benzylstyrenes
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Using triphenylmethylium tetrakis(pentafluorophenyl)borate as a convenient Br?nsted acid precatalyst, β-(α,α-dimethylbenzyl)styrenes are shown to cyclize efficiently to afford a variety of new indanes that possess a benzylic quaternary center. The geminal dimethyl-containing quaternary center is proposed to be necessary to arm the substrate for cyclization through steric biasing.
- Cai, Xiao,Keshavarz, Amir,Omaque, Justin D.,Stokes, Benjamin J.
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supporting information
p. 2626 - 2629
(2017/05/24)
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- BIARYL DERIVATIVE AS GPR120 AGONIST
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The present invention relates to a biaryl derivative expressed by the chemical formula 1, a method for producing the biaryl derivative, a pharmaceutical composition comprising same, and use of same, the biaryl derivative expressed by the chemical formula 1, as a GPR120 agonist, promoting GLP-1 generation in the gastro-intestinal tract, reducing insulin resistance in the liver, muscles and the like from anti-inflammatory activity in the macrophage, pancreatic cells and the like, and allowing effective use in prevention or treatment of inflammation or metabolic diseases such as diabetes, complications from diabetes, obesity, non-alcoholic fatty liver disease, fatty liver disease, and osteoporosis.
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Paragraph 0133; 0340
(2017/11/17)
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- HETEROCYCLIC MODULATORS OF HIF ACTIVITY FOR TREATMENT OF DISEASE
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The present invention relates to compounds and methods which may be useful as inhibitors of HIF pathway activity for the treatment or prevention of cancer and other hypoxia-mediated diseases.
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Paragraph 0399
(2014/03/25)
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- INDOLE AND INDAZOLE COMPOUNDS THAT ACTIVATE AMPK
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The present invention relates to indole and indazole compounds of Formula (I) that activate 5′ adenosine monophosphate-activated protein kinase (AMPK). The invention also encompasses pharmaceutical compositions containing these compounds and methods for treating or preventing diseases, conditions, or disorders ameliorated by activation of AMPK.
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Paragraph 0842
(2013/10/22)
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- Discovery of microsomal triglyceride transfer protein (MTP) inhibitors with potential for decreased active metabolite load compared to dirlotapide
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Analogues related to dirlotapide (1), a gut-selective inhibitor of microsomal triglyceride transfer protein (MTP) were prepared with the goal of further reducing the potential for unwanted liver MTP inhibition and associated side-effects. Compounds were designed to decrease active metabolite load: reducing MTP activity of likely human metabolites and increasing metabolite clearance to reduce exposure. Introduction of 4′-alkyl and 4′-alkoxy substituents afforded compounds exhibiting improved therapeutic index in rats with respect to liver triglyceride accumulation and enzyme elevation. Likely human metabolites of select compounds were prepared and characterized for their potential to inhibit MTP in vivo. Based on preclinical efficacy and safety data and its potential for producing short-lived, weakly active metabolites, compound 13 (PF-02575799) advanced into phase 1 clinical studies.
- Robinson, Ralph P.,Bartlett, Jeremy A.,Bertinato, Peter,Bessire, Andrew J.,Cosgrove, Judith,Foley, Patrick M.,Manion, Tara B.,Minich, Martha L.,Ramos, Brenda,Reese, Matthew R.,Schmahai, Theodore J.,Swick, Andrew G.,Tess, David A.,Vaz, Alfin,Wolford, Angela
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scheme or table
p. 4150 - 4154
(2011/08/06)
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- 4-AMINO-7,8-DIHYDROPYRIDO[4,3-d]PYRIMIDIN-5(6H)-ONE DERIVATIVES
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The invention provides compounds of the general Formula (I) where R1, R2, and A are defined herein, as well as the preparation, compositions and uses thereof.
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Page/Page column 20
(2010/08/08)
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- 4-AMINO-5-OXO-7, 8-DIHYDROPYRIMIDO [5,4-F] [1,4] OXAZEPIN-6 (5H) -YL) PHENYL DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
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The invention provides compounds of Formula (I), wherein R1, R2a, R2b, R3, m and A are as defined herein, as well as compositions thereof and methods for treating a disease, condition or disorder that is modulated by the inhibition of the diacylglycerol O-acyltransferase 1 (DGAT-1) enzyme by administering the compounds of the present invention and/or compositions thereof.
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Page/Page column 50
(2010/08/09)
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- 12-ARYL PROSTAGLANDIN ANALOGS
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Compounds comprising the formula (I) are disclosed, wherein Y, A, X, R, D, and n are as described. A compound comprising a prostaglandin EP2 selective agonist wherein the ω-chain comprises a substituted phenyl, wherein at least one substituent
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Page/Page column 37
(2010/11/08)
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- 4-[[3-[α-Aminobenzyl]phenyl]methyl]morpholine and 4-[-[3-benzoylphenyl]ethyl]morpholine
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N-{2, 3- and 4-[R1 -(phenyl)-C(=X)]-phenyl-lower-alkyl}amines, useful as anti-inflammatory agents, are prepared either by reduction of 2-, 3- or 4-[R1 -(phenyl)-CO]-phenyl-lower-alkanoylamines, which are also useful as anti-inflammatory agents; by benzoylating a phenyl-lower-alkylamine; by reaction of a 2-, 3- or 4-lithiophenyl-lower-alkylamine with a R1 -(phenyl)-carboxaldehyde, a R1 -(phenyl)-lower-alkyl ketone or a R1 -(phenyl)-carbonitrile; by reaction of a 2-, 3- or 4-[R1 -(phenyl)-CO]-phenyl-lower-alkyl tosylate with an appropriate amine; or by transformations involving manipulations of a carbonyl or carbinol group.
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