746630-34-2Relevant articles and documents
P2X3 MODULATORS
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Paragraph 00256, (2021/08/20)
Provided herein are P2X3 modulators and methods of utilizing P2X3 modulators in the treatment of diseases, disorders, or conditions. Also described herein are pharmaceutical compositions containing such compounds.
PHENYL SUBSTITUTED PYRAZOLES AS MODULATORS OF RORgT
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Paragraph 0546-0547, (2020/01/09)
The present invention comprises compounds of Formula I. wherein: R1, R3, R4, R5, R6, R7, R8, and Q are defined in the specification. The invention also comprises a method of treating or ameliorating a ROR-γ-t mediated syndrome, disorder or disease, including wherein the syndrome, disorder or disease is selected from the group consisting of rheumatoid arthritis, psoriatic arthritis, and psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.
BIARYL DERIVATIVE AS GPR120 AGONIST
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Paragraph 0140, (2017/11/17)
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.
Indazole-6-phenylcyclopropylcarboxylic Acids as Selective GPR120 Agonists with in Vivo Efficacy
McCoull, William,Bailey, Andrew,Barton, Peter,Birch, Alan M.,Brown, Alastair J. H.,Butler, Hayley S.,Boyd, Scott,Butlin, Roger J.,Chappell, Ben,Clarkson, Paul,Collins, Shelley,Davies, Robert M. D.,Ertan, Anne,Hammond, Clare D.,Holmes, Jane L.,Lenaghan, Carol,Midha, Anita,Morentin-Gutierrez, Pablo,Moore, Jane E.,Raubo, Piotr,Robb, Graeme
supporting information, p. 3187 - 3197 (2017/04/19)
GPR120 agonists have therapeutic potential for the treatment of diabetes, but few selective agonists have been reported. We identified an indazole-6-phenylcyclopropylcarboxylic acid series of GPR120 agonists and conducted SAR studies to optimize GPR120 potency. Furthermore, we identified a (S,S)-cyclopropylcarboxylic acid structural motif which gave selectivity against GPR40. Good oral exposure was obtained with some compounds displaying unexpected high CNS penetration. Increased MDCK efflux was utilized to identify compounds such as 33 with lower CNS penetration, and activity in oral glucose tolerance studies was demonstrated. Differential activity was observed in GPR120 null and wild-type mice indicating that this effect operates through a mechanism involving GPR120 agonism.
PYRAZOLYL-SUBSTITUTED HETEROARYLS AND THEIR USE AS MEDICAMENTS
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Page/Page column 48, (2017/03/28)
The invention relates to new substituted heteroaryls of formula 1 or of formula 1' wherein A is either N or CH, wherein R2 is selected from the group consisting of -C1-3-alkyl, -C1-3-haloalkyl, F, Br, CI, wherein Y is selected from -O- or -CH2-, and wherein R3 is defined as in claim 1, and the pharmaceutically acceptable salts thereof, and the use of these aforementioned compounds for the treatment of diseases such as asthma, COPD, allergic rhinitis, allergic dermatitis, lupus erythematodes, lupus nephritis and rheumatoid arthritis.
ANTIPROLIFERATIVE 2-(SULFO-PHENYL)-AMINOTHIAZOLE DERIVATIVES
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Page 100-101, (2010/02/08)
Aminothiazole compounds substituted with sulfur-containing groups are represented by the Formula (I), and their pharmaceutically acceptable salts, prodrugs, active metabolites, and pharmaceutically acceptable salts of said metabolites are described. These agents modulate and/or inhibit the cell proliferation and activity of protein kinases and are useful as pharmaceuticals for treating malignancies and other disorders.