187722-18-5Relevant articles and documents
Synthesis of β-dimethylsulfonium- and β-methylthio-substituted vinyl triflates by reaction of acetylenes with dimethyl sulfide ditriflate
Nenajdenko, Valentine G.,Vertelezkij, Pavel V.,Balenkova, Elizabeth S.
, p. 351 - 355 (1997)
A one-pot synthesis of β-dimethylsulfonium-substituted vinyl triflates by the reaction of dimethyl sulfide ditriflate with acetylenes is described. β-Dimethylsulfonium-substituted vinyl triflates were found to exhibit unusual reactivity towards nucleophil
SULFINIC ACID COMPOUNDS AS FREE FATTY ACID RECEPTOR AGONISTS
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Page/Page column 99, (2021/02/19)
The present invention relates to certain compounds, their use in therapy, as well as to pharmaceutical compositions including said compounds. Specifically, the invention relates to certain compounds and pharmaceutical compositions including these compounds for the treatment of metabolic disorders including, for example, diabetes, obesity, metabolic syndrome, fatty liver disease, and bone disorders.
SYNTHESIS OF 3-({5-CHLORO-1-[3-(METHYLSULFONYL)PROPYL]-1H-INDOL-2 YL} METHYL)-1-(2,2,2-TRIFLUOROETHYL)-1,3-DIHYDRO-2H-IMIDAZO[4,5-C]PYRIDIN-2-ONE
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Paragraph 0017, (2021/05/07)
The present invention relates to a chemical synthesis route for preparing the RSV inhibiting compound 3-({5-chloro-1-[3-(methylsulfonyl)propyl]-1H-indol-2-yl}methyl)-1-(2,2,2-trifluoroethyl)-10 1,3-dihydro-2H-imidazo[4,5-c]pyridin-2-one, and to new compounds used as intermediate compounds in the multistep process.
4-diphenylcarboxylic acid compound and preparing method and application thereof
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Paragraph 0117; 0118; 0019; 0120, (2018/06/21)
The invention relates to a 4-diphenylcarboxylic acid compound and a preparing method and application thereof, and belongs to the field of medicines. The 4-diphenylcarboxylic acid compound is shown inthe formula I. The 4-diphenylcarboxylic acid compound ex
Ex Situ Formation of Methanethiol: Application in the Gold(I)-Promoted Anti-Markovnikov Hydrothiolation of Olefins
Kristensen, Steffan K.,Laursen, Simon L. R.,Taarning, Esben,Skrydstrup, Troels
supporting information, p. 13887 - 13891 (2018/10/02)
A protocol for the Au-promoted anti-Markovnikov hydrothiolation of olefins using ex situ generated methanethiol is reported. The use of S-methylisothiourea hemisulfate salt as a solid precursor for methanethiol generation ensures a safe and reliable deliverance of a stoichiometric amount of this thiol. The procedure was shown to work for a broad range of olefins providing the corresponding hydrothiolated adduct in good to excellent yields. Mechanistic evaluations suggest that thiyl radicals are generated and that gold acts as an efficient but stable radical initiator.
GPR40 AGONISTS IN ANTI-DIABETIC DRUG COMBINATIONS
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Paragraph 0472, (2017/10/27)
Disclosed are compositions comprising (a) a GPR40 agonist and (b) an SGLT2 inhibitor, and methods for treating of disorders that are affected by the modulation of the GPR40 receptor and SGLT2 transporter. Such GPR40 compounds are represented by Formula (I) as follows: wherein ring W, R1, R2, R3, R5, R6, A, and Z, are defined herein.
SUBSTITUTED BENZOTHIOPHENYL DERIVATIVES AS GPR40 AGONISTS FOR THE TREATMENT OF TYPE II DIABETES
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Paragraph 0471, (2017/11/01)
Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR40 receptor. Such compounds are represented by Formula (I) as follows: wherein U1, U2, U3, R1, R2, Z, and W are defined herein.
Discovery of methylsulfonyl indazoles as potent and orally active respiratory syncytial Virus(RSV) fusion inhibitors
Feng, Song,Li, Chao,Chen, Dongdong,Zheng, Xiufang,Yun, Hongying,Gao, Lu,Shen, Hong C.
supporting information, p. 1147 - 1157 (2017/08/02)
Recently we described a novel class of imidazopyridine compounds that showed exceptional anti-RSV potency in cell culture. However, unfavorable pharmacokinetic (PK) properties and glutathione (GSH) adduct liabilities impeded their further development. In a bid to address the PK and early safety concerns, a small compound library consisting of dozens of scaffold-hopping analogues was designed and synthesized for RSV CPE assay screening, which led to the identification of a new chemical starting point: methylsulfonyl indole compound 8. In this paper, we report the discovery and optimization of a series of methylsulfonyl indazoles as potent RSV fusion inhibitors. In particular, compound 47 was orally efficacious in a RSV mouse model, with 1.6 log unit viral load reduction at 25 mg/kg BID upon oral dosing. The results may have broad implications for the design of new RSV fusion inhibitors, and demonstrate the potential for developing novel therapies for RSV infection.
COMPOSITE PREPARATION, CONTAINING NOVEL 3-(4-(BENZYLOXY)PHENYL)HEX-4-INOIC ACID DERIVATIVE AND ANOTHER ACTIVE INGREDIENT, FOR PREVENTING OR TREATING METABOLIC DISEASES
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Paragraph 0177-0179, (2017/09/04)
The present invention relates to a pharmaceutical composition for preventing or treating metabolic diseases, in which a novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative and at least another active ingredient, which is selected from the group consisting of dipeptidyl peptidase-4 (DPPIV) inhibitor-based, sulfonylurea-based, thiazolidinedione (TZD)-based, biguanide-based, and sodium/glucose cotransporter 2 (SGLT2) inhibitor-based drugs, may be administered in combination or in the form of a composite preparation. The use of the composition of the present invention can provide a remarkably excellent blood sugar reducing effect in various animal diabetic disease models, and the composition of the present invention can be favorably used as a pharmaceutical composition for preventing or treating metabolic diseases, such as obesity, diabetes type I, diabetes type II, glucose intolerance symptoms, insulin resistance symptoms, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, dyslipidemia, and syndrome X.
SUBSTITUTED BENZOTHIOPHENYL DERIVATIVES AS GPR40 AGONISTS FOR THE TREATMENT OF TYPE II DIABETES
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Page/Page column 96-97, (2016/05/02)
Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR40 receptor. Such compounds are represented by Formula (I) wherein R1, R2, R3, R5, R6, W, and A are defined herein.