227029-27-8Relevant articles and documents
Synthesis of JTT-501 and its metabolite JTP-20604 labelled with 13C
Pignatti,Giribone,Felicini,Fontana
, p. 605 - 611 (2003)
JTT-501 specifically labelled with 13C was obtained via a four-step synthesis at an isotopic enrichment level of 99% and in 14% overall chemical yield starting from 4-hydroxy-[ring-U-13C6]benzaldehyde (3). The hydrogenatio
Convenient Continuous Flow Synthesis of N-Methyl Secondary Amines from Alkyl Mesylates and Epoxides
Lebel, Hélène,Mathieu, Gary,Patel, Heena
supporting information, p. 2157 - 2168 (2020/11/23)
The first continuous flow process was developed to synthesize N-methyl secondary amines from alkyl mesylates and epoxides via a nucleophilic substitution using aqueous methylamine. A variety of N-methyl secondary amines were produced in good to excellent yields, including a number of bioactive compounds or their precursors. Up to 10.6 g (88% yield) of an N-methyl secondary amine was produced in 140 min process time. The amination procedure included an in-line workup, and the starting mesylate material was also produced in continuous flow from the corresponding alcohol. Finally, an in-line process combining the mesylate synthesis and nucleophilic substitution was developed.
METHODS OF TREATING OR PREVENTING COGNITIVE IMPAIRMENT USING INDANE ACETIC ACID DERIVATIVES BASED ON APOE4 GENOTYPE
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Paragraph 0427-0429, (2018/06/15)
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.
METHODS OF DOSE ADMINISTRATION FOR TREATING OR PREVENTING COGNITIVE IMPAIRMENT USING INDANE ACETIC ACID DERIVATIVES
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Paragraph 0430; 0431, (2018/06/15)
The present invention provides indane acetic acid and their derivatives and methods for the treating and/or preventing of cognitive disorders.
Design and synthesis of Oxime ethers of β-oxo-γ-phenylbutanoic acids as PPAR a and -γ dual agonists
Han, Hee Oon,Koh, Jong Sung,Kim, Seung Hae,Park, Ok Ku,Kim, Kyoung-Hee,Jeon, Sang Kweon,Hur, Gwong-Cheung,Yim, Hyeon Joo,Kim, Geun Tae
, p. 1979 - 1982 (2012/08/14)
Oxime ethers of p-oxo-y-phenylbutanoic acids were prepared to develop more effective PPAR a and y dual agonists. Among them, compound 11k exhibited potent in vitro activities with EC50 of 2.5 nM and 3.3 nM in PPAR a and y, respectively. It showed better g
Synthesis and antimicrobial evaluation of 3-methanone-6-substituted- benzofuran derivatives
Liu, Jingbao,Jiang, Faqin,Jiang, Xizhen,Zhang, Wei,Liu, Jingjing,Liu, Wenlu,Fu, Lei
, p. 879 - 886 (2012/09/10)
Seventeen benzofuran derivatives were synthesized and screened for their antibacterial activities against Escherichia coli, Staphylococcus aureus, Methicillin-resistant S. aureus, Bacillus subtilis, and Pseudomonas aeruginosa. Seven of them have showed excellent antibacterial activities compared to the positive controls (Cefotaxime and Sodium Penicillin). The substitutions at C-6 and C-3 positions of these derivatives were found to greatly impact on the antibacterial activity and strains specificity, respectively. Specifically, compounds bearing a hydroxyl group at C-6 (5a, 5b, 5c and 12) offered excellent antibacterial activities against all five above-mentioned strains (MIC 80 = 0.78-12.5 ug/mL), and those with imine (15) and (3, 4, 5-trimethoxyphenyl) methanone (7e), respectively, at C-3 position showed selective activity against S. aureus among five tested strains with great MIC80 values (3.12-12.5 ug/mL).
In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: Trends across multiple chemical series
Nersesian, Diana L.,Black, Lawrence A.,Miller, Thomas R.,Vortherms, Timothy A.,Esbenshade, Timothy A.,Hancock, Arthur A.,Cowart, Marlon D.
, p. 355 - 359 (2008/04/03)
Structure-activity relationships (SAR) were analyzed within a library of diverse yet simple compounds prepared as histamine H3 antagonists. The libraries were constructed with a variety of low molecular weight pyrrolidines, selected from (R)-2-methylpyrrolidine, (S)-2-methylpyrrolidine, and pyrrolidine.
Design and synthesis of oxime ethers of α-acyl-β-phenylpropanoic acids as PPAR dual agonists
Oon Han, Hee,Hae Kim, Seung,Kim, Kyoung-Hee,Hur, Gwong-Cheung,Joo Yim, Hyeon,Chung, Hee-Kyung,Ho Woo, Sung,Dong Koo, Ki,Lee, Chang-Seok,Sung Koh, Jong,Tae Kim, Geun
, p. 937 - 941 (2007/10/03)
Oxime ethers of α-acyl-β-phenylpropanoic acids were prepared to apply as PPARα and γ dual agonists. Among them, compound 11l proved to exhibit potent in vitro activities with EC50 of 19 and 13 nM in PPARα and γ, respectively. It showed better g
Design and synthesis of N-[(4-methoxyphenoxy)carbonyl]-N-[[4-[2-(5-methyl- 2-phenyl-4-oxazolyl)ethoxy]phenyl]methyl]glycine [muraglitazar/BMS-298585], a novel peroxisome proliferator-activated receptor α/γ dual agonist with efficacious glucose and lipid-l
Devasthale, Pratik V.,Chen, Sean,Jeon, Yoon,Qu, Fucheng,Shao, Chunning,Wang, Wei,Zhang, Hao,Cap, Michael,Farrelly, Dennis,Golla, Rajasree,Grover, Gary,Harrity, Thomas,Ma, Zhengping,Moore, Lisa,Ren, Jimmy,Seethala, Ramakrishna,Cheng, Lin,Sleph, Paul,Sun, Wei,Tieman, Aaron,Wetterau, John R.,Doweyko, Arthur,Chandrasena, Gamini,Chang, Shu Y.,Humphreys, W. Griffith,Sasseville, Vito G.,Biller, Scott A.,Ryono, Denis E.,Selan, Fred,Hariharan, Narayanan,Cheng, Peter T. W.
, p. 2248 - 2250 (2007/10/03)
Muraglitazar/BMS-298585 (2) has been identified as a non-thiazolidinedione PPAR α/γ dual agonist that shows potent activity in vitro at human PPARα (EC50 = 320 nM) and PPARγ (EC50 = 110 nM). Compound 2 shows excellent efficacy for lo
ORGANIC COMPOUNDS
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Page 48, (2010/02/11)
Compounds of the formula (I) provide pharmacological agents which bind to Peroxisome Proliferator-Activated Receptors (PPARs). Accordingly, the compounds of the present invention are useful for the treatment of conditions mediated by the PPAR receptor activity in mammals. Such conditions include dyslipidemia, hyperlipidemia, hypercholesteremia, atherosclerosis, hypertriglyceridemia, heart failure, myocardial infarction, vascular diseases, cardiovascular diseases, hypertension, obesity, inflammation, arthritis, cancer, Alzheimer's disease, skin disorders, respiratory diseases, ophthalmic disorders, inflammatory bowel diseases (IBDs), ulcerative colitis and Crohn's disease. The compounds of the present invention are particularly useful in mammals as hypoglycemic agents for the treatment and prevention of conditions in which impaired glucose tolerance, hyperglycemia and insulin resistance are implicated, such as type-1 and type-2 diabetes, and Syndrome X.