cas 116815-03-3, 8-CHLORO-1,2,3,4-TETRAHYDRO-BENZO[B]AZEPIN-5-ONE | Articles data ｜lookchem

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116815-03-3

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COMPOUNDS AND METHODS FOR TREATING DYSLIPIDEMIA
Compounds of formula I wherein n, m, p, q, Y, R1 R2, R3, R4, R5, and R6 are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating artherosclerosis and its sequelae.
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Page/Page column 142

(2008/06/13)

Synthesis and diuretic activity of bicyclic fused heterocycles containing oxime-O-sulfonic acid moiety
In order to investigate the origin of the loop-type diuretic activity of M17055 (1), several variants (3-9) were designed and synthesized by modifying the quinolinone skeleton, and their diuretic activities were compared with the lead 1 and furosemide in dogs. It was found that the negative charge distribution pattern afforded by the dispositional arrangement of the 4- oxime-O-sulfonic acid and 1-N-acyl carbonyl moiety attached to the tetrahydropyridine ring system is inevitable for the development of the activity, which strongly supports the previously proposed model for the active site of the Na+-K+-2Cl- cotransporter. Also reported is the first synthesis of the dihydrothieno[3,2-b]pyridine-7(4H)-one ring system required in the synthesis of compound 9. (C) 2000 Editions scientifiques et medicales Elsevier SAS.
Nishijima, Kazumi,Nishida, Hidemitsu,Yamashita, Yoshiaki,Ito, Manabu,Onuki, Yoshiaki,Mizota, Masahiro,Miyano, Sotaro
p. 227 - 240
(2007/10/03)

7-Chloro-5-hydroxy-1-[2-methyl-4-(2-methylbenzoylamino)benzoyl]-2,3,4,5- tetrahydro-1H-1-benzazepine (OPC-41061): A potent, orally active nonpeptide arginine vasopressin V2 receptor antagonist
We previously reported a series of benzazepine derivatives as orally active nonpeptide arginine vasopressin (AVP) V2 receptor antagonists. After the lead structure OPC-31260 was structurally evaluated and optimized, the introduction of the 7-Cl moiety on the benzazepine and 2-CH3 on the aminobenzoyl moiety enhanced its oral activity. The new AVP-V2 selective antagonist OPC-41061 was determined to be a potent and orally active agent. Copyright (C) 1999 Elsevier Science Ltd.
Kondo, Kazumi,Ogawa, Hidenori,Yamashita, Hiroshi,Miyamoto, Hisashi,Tanaka, Michinori,Nakaya, Kenji,Kitano, Kazuyoshi,Yamamura, Yoshitaka,Nakamura, Shigeki,Onogawa, Toshiyuki,Mori, Toyoki,Tominaga, Michiaki
p. 1743 - 1754
(2007/10/03)

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Chemical Properties

Melting Point: 104 °C
Boiling Point: 352.635 °C at 760 mmHg
Flash Point:167.068 °C
Density: 1.235 g/cm³
Storage Temp.:2-8°C(protect from light)
Vapor Pressure: 0mmHg at 25°C
Refractive Index: 1.562
PKA: 2.18±0.20(Predicted)
PSA: 29.10000
LogP: 2.86640

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