On August 3, 2006, Sekiguchi, Yoshinori; Kuwada, Takeshi; Hayashi, Masato; Nozawa, Dai; Amada, Yuri; Shibata, Tsuyoshi; Yamamoto, Shuji; Ohta, Hiroshi; Okubo, Taketoshi; Koami, Takeshi published a patent.Related Products of 141940-37-6 The title of the patent was Preparation of 1,3-dihydro-2H-indol-2-one compounds and pyrrolidin-2-one compound fused with aromatic heterocycle as antagonists of arginine-vasopressin V1b receptor. And the patent contained the following:
The title compounds [I; ring A = each (un)substituted C6-14 aryl or aromatic heterocyclyl; P = a single bond, C1-5 alkylene; Q = each (un)substituted C6-14 aryl or aromatic heterocyclyl, Q1; RD and RE at 2 and 3 or 3 and 4 positions together form (un)substituted C1-3 alkylenedioxy, (CH2)m-O, N-(un)substituted (CH2)m-NH or NH-(CH2)m, (CH2)m-S, O-(CH2)m-S, or S-(CH2)m-S (m = 2-4); R5 = Q2, Q3, etc.; R6 = H, halo, (un)substituted HO; R7 = H, halo, (un)substituted SH; or R6 and R7 together represent oxo; R9 = each (un)substituted OH, SH or NH2; R33 = H, (un)substituted C1-5 alkyl, C3-8 cycloalkyl, C1-5 alkoxycarbonyl, C6-14 aryl, heterocyclyl; RA, RB, RC = H, halo, NO2, NH2, hydroxyamino, C1-5 alkyl, C1-5 alkoxy, C1-5 alkylthio, etc.] or pharmacol. acceptable salts thereof are prepared These compounds are highly selectively antagonistic to arginine-vasopressin V1b receptor over arginine-vasopressin V1a receptor and arginine-vasopressin V2 receptor, have high metabolic stabilities and show favorable migration into the brain and high concentrations in the plasma. They provide drugs which are efficacious against pathol. conditions relating to arginine-vasopressin V1b receptor. More particularly speaking, they provide drugs which have a therapeutic or preventive effect on depression, anxiety, Alzheimer’s disease, Parkinson’s disease, Huntington’s chorea, eating disorders, hypertension, digestive diseases, drug addiction, epilepsy, brain infarction, brain ischemia, brain edema, head injury, inflammation, immune diseases, alopecia and so on. Thus, reductive amination of (4R)-1-((3R)-5-Chloro-3-[2-methoxy-5-(2-oxoethyl)phenyl]-1-([4-methoxy-2-(trifluoromethoxy)phenyl]sulfonyl)-2-oxo-2,3-dihydro-1H-indol-3-yl)-4-hydroxy-N,N-dimethyl-L-prolinamide with piperidine using sodium triacetoxyborohydride in the presence of acetic acid din a mixture of THF and CHCl3 gave (+)-(4R)-1-[5-Chloro-3-[5-[2-(dimethylamino)ethyl]-2-methoxyphenyl]-1-[[4-methoxy-2-(trifluoromethoxy)phenyl]sulfonyl]-2-oxo-2,3-dihydro-1H-indol-3-yl]-4-hydroxy-N,N-dimethyl-L-prolinamide (II). II inhibited the binding of [3H](Arg8)vasopressin to human arginine vasopressin V1b, V1a, and V2 receptor with IC50 of 0.32, 102, and 5,050, nM, resp. The experimental process involved the reaction of tert-Butyl (4-(trifluoromethyl)phenyl)carbamate(cas: 141940-37-6).Related Products of 141940-37-6
The Article related to phenylsulfonylindolylprolinamide preparation antagonist arginine vasopressin v1b receptor, dihydroindolone preparation antagonist arginine vasopressin v1b receptor, pyrrolidinone fused heterocycle preparation antagonist arginine vasopressin v1b receptor, depression anxiety alzheimer disease treatment dihydroindolone preparation and other aspects.Related Products of 141940-37-6
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