169328-26-1Relevant articles and documents
Acyliminothiadiazoline derivatives: New, highly potent, and orally active angiotensin II receptor antagonists
Hirata, Terukage,Nomiyama, Jun,Sakae, Nobuya,Nishimura, Kouji,Yokomoto, Masaharu,Inoue, Satoshi,Tamura, Koichi,Okuhira, Masayasu,Amano, Hirotaka,Nagao, Yoshimitsu
, p. 1469 - 1474 (1996)
Syntheses and pharmacological properties of a new series of acyliminothiadiazoline derivatives 1 are described. These compounds exhibited angiotensin II receptor antagonistic activities in vitro and in vivo. Among them, the compound 1g (KRH-594) showed the strongest antihypertensive action in renal hypertensive rats after oral administration, and its oral bioavailability in dogs was also found to be high (73%).
Process for producing tetrazolylated biphenylmethane derivatives
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, (2008/06/13)
The present invention relates to a process for producing a tetrazolylated biphenylmethane derivatives (6) or salts thereof in accordance with the below-described reaction scheme wherein R 1 represents an alkyl; R 2 represents H, etc.; Z represents a halogen, etc.; and A represents a cycloalkene, etc. According to the above process, a tetrazolylated biphenylmethane derivative can be industrially and advantageously produced with short steps.
POTASSIUM SALT OF BIPHENYLMETHANE DERIVATIVE AND MEDICINE CONTAINING THE SAME
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, (2008/06/13)
The present invention relates to mono or dipotassium 2-[[5-ethyl-3-[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl-1,3,4-thiadiazolin-2-yliden]aminocarbonyl]-1-cyclopentenecarboxylate, a pharmaceutical composition containing the compound, use of the compound for pharmaceuticals, and a therapeutic method of circulatory diseases by administering the compound. The mono or dipotassium salt of the compound has a potent angiotensin II antagonist activity and anti-hypertensive effect and also has high bioavailability when administered orally so that it is useful as a pharmaceutical.