126832-81-3Relevant academic research and scientific papers
Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation
Wang, Zhengyu,Shi, Xiaofan,Zhang, Huan,Yu, Liang,Cheng, Yanhua,Zhang, Hefeng,Zhang, Huibin,Zhou, Jinpei,Chen, Jing,Shen, Xu,Duan, Wenhu
, p. 128 - 152 (2017/08/10)
Glucokinase (GK) activators are being developed for the treatment of type 2 diabetes mellitus (T2DM). However, existing GK activators have risks of hypoglycemia caused by over-activation of GK in islet cells and dyslipidemia caused by over-activation of intrahepatic GK. In the effort to mitigate risks of hypoglycemia and dyslipidemia while maintaining the promising efficacy of GK activator, we investigated a series of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific partial GK activators, which led to the identification of compound 72 that showed a good balance between in vitro potency and enzyme kinetic parameters, and protected β-cells from streptozotocin-induced apoptosis. Chronic treatment of compound 72 demonstrated its potent activity in regulation of glucose homeostasis and low risk of dyslipidemia with diabetic db/db mice in oral glucose tolerance test (OGTT). Moreover, acute treatment of compound 72 did not induce hypoglycemia in C57BL/6J mice even at 200 mg/kg via oral administration.
Substituted Benzamide Compounds
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, (2012/04/04)
Substituted benzamide compounds corresponding to formula (I) in which R5, R6, R7, R8, a, b, c, d, t, D and X have defined meanings, a process for their preparation, pharmaceutical compositions comprising such compounds, and a method of using such compounds to treat pain and other conditions mediated at least in part via the bradykinin 1 receptor.
PIPERIDIN-4-YLPIPERAZINE COMPOUNDS FOR THE TREATMENT OF HCV INFECTION
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Page/Page column 17, (2010/08/08)
The invention relates to new piperazine-pieridine compounds having anti-viral activity and particularly anti-HCV activity. The invention further relates to pharmaceutical compositions comprising compounds according to the invention.
An improved synthesis of N-aryl and N-heteroaryl substituted piperidones
Sch?n, Uwe,Messinger, Josef,Buckendahl,Prabhu,Konda
, p. 2519 - 2525 (2008/02/02)
An efficient Pd(0)-catalyzed protocol for the rapid and efficient preparation of N-aryl and N-heteroaryl substituted piperidones is described. The two step syntheses proceed with an overall yield of 50-70% using X-Phos as optimal ligand for the Pd(0)-cata
Synthesis and structure-activity relationships of novel selective factor Xa inhibitors with a tetrahydroisoquinoline ring
Ueno, Hiroshi,Yokota, Katsuyuki,Hoshi, Jun-Ichi,Yasue, Katsutaka,Hayashi, Mikio,Hase, Yasunori,Uchida, Itsuo,Aisaka, Kazuo,Katoh, Susumu,Cho, Hidetsura
, p. 3586 - 3604 (2007/10/03)
A series of novel 2,7-disubstituted tetrahydroisoquinoline derivatives were designed and synthesized. Among these derivatives, compounds 1 and 2 exhibited potent inhibitory activity against factor Xa (FXa) and good selectivity with respect to other serine
Amino alcohol derivatives, process for their production and pharmaceutical preparations and reagents containing these compounds
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Page 7, (2008/06/13)
The present invention concerns new amino alcohol derivatives, a process for their production as well as pharmaceutical preparations and reagents which contain these substances. The invention concerns pharmaceutical agents of the general formula I in which A denotes hydrogen, a group NR1R2, a group NR1(CH2)pNR3R4, a group (C═NH)NH2 or a pyridinyl residue, B and D are the same or different and each denotes a bond, a C1 to C6 alkylene residue or a group NR5—C2 to C6-alkylene, C denotes piperidinediyl or piperazinediyl, W and X are the same or different and each denotes a bond or a carbonyl group, Y and Z are the same or different and each denotes a saturated or unsaturated hydrocarbon residue with 7 to 24 carbon atoms, R1 to R5are the same or different and each represents hydrogen or a C1 to C6 alkyl residue, m is an integer 0, 1 or 2 and if m equals 2 C can also independently of one another be piperidinediyl or piperazinediyl, n and o are the same or different and each denotes the integers 2, 3 or 4 and p denotes an integer from 2 to 6 as well as physiologically tolerated salts thereof, provided that hydrazine derivatives are not included and that m cannot be 0 if A denotes hydrogen or a group (C═NH)NH2 and B and D being the same or different represent a bond or an alkylene residue.
Amidine compounds
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, (2008/06/13)
A compound of the formula [I] wherein R1, R2and R3are the same or different and each is hydrogen atom, wherein each symbol is as defined in the specification, a salt thereof or a prodrug thereof. The compound of the presen
ACYLHYDRAZINE DERIVATIVES, PROCESS FOR PREPARING THE SAME AND USE THEREOF
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Page 45, (2010/11/30)
Novel acylhydrazine derivatives exhibiting an inhibitory activity against activated blood coagulation factor X, which are compounds of general formula (I)or salts thereof, wherein R is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; R1and R2are each hydrogen or optionally substituted hydrocarbyl, or alternatively R1and R2or the substituent of X1and R2may be united to form an optionally substituted ring; X1and X2are each free valency, optionally substituted alkylene, or optionally substituted imino; D is oxygen or sulfur; A is -N(R3)-Y- or -N=Y-, R3is hydrogen, optionally substituted hydrocarbyl, or acyl; Y is an optionally substituted chain hydrocarbon group or an optionally substituted cyclic group; and Z is (1) optionally substituted amino, (2) optionally substituted imidoyl, or (3) an optionally substituted nitrogenous heterocycle group.
Sulfonamide derivatives, processes for producing the same and utilization thereof
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, (2008/06/13)
The present invention is to provide a compound or a salt thereof represented by the formula: wherein R1is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, the ring A is an optionally substituted divalent nitrogen-containing heterocyclic group, X′ is an optionally substituted alkylene chain, Y is an optionally substituted divalent cyclic group, X is a chemical bond or an optionally substituted alkylene chain, and Z is (1) an optionally substituted amino group, (2) an optionally substituted imidoyl group or (3) an optionally substituted nitrogen-containing heterocyclic group, or a pro-drug thereof, which have activated coagulation factor X inhibitory activity and which are useful as anti-coagulants.
Oxazolidinone derivatives, processes for the production thereof and pharmaceutical agents containing these compounds
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, (2008/06/13)
The present invention concerns new oxazolidinone derivatives, processes for their production as well as pharmaceutical agents containing these substances. The present invention concerns compounds of the general formula I STR1 in which the symbols have the meanings as listed in the claims.
