22926-50-7Relevant articles and documents
Intramolecular nonbonded S···O interaction recognized in (acylimino)thiadiazoline derivatives as angiotensin II receptor antagonists and related compounds
Nagao, Yoshimitsu,Hirata, Terukage,Goto, Satoru,Sano, Shigeki,Kakehi, Akikazu,Iizuka, Kinji,Shiro, Motoo
, p. 3104 - 3110 (1998)
The intramolecular nonbonded 1,5-type S···O interactions are recognized in the crystalline structures of the (acylimino)thiadiazoline derivatives (1-3) as angiotensin II receptor antagonists. The relative stability of the nonbonded 1,5-type S···O interaction was investigated using the X-ray crystallographic analyses anti the ab initio MO calculations (HF/3-21G*, 6-31G*, and 6-311 +G**) of the simplified model compounds (6, 7, and 9). The concept of mimic-fused bicyclic heterocycles consisting of fairly stable nonbonded S···O interaction seems to be an efficient approach toward the design and development of various drugs.
Process for producing N-biphenylmethylthiadiazoline derivative or salt thereof and intermediate for producing the same
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, (2008/06/13)
Described is a process for producing an N-biphenyl-methylthiadiazoline derivative (7) in accordance with the reaction formula described below. According to the process of the present invention, it is possible to produce a compound (7) advantageously from the industrial viewpoint. STR1
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.
NOVEL REAGENT FOR TETRAZOLE SYNTHESIS AND PROCESS FOR PRODUCING TETRAZOLES THEREWITH
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, (2008/06/13)
Analkali metal azide and zinc chloride are used in combination as a tetrazole forming agent when producing 1H-tetrazoles of the formula (II): (where R is any substituent) from carbonitriles of the formula (I): R-CN(where R has the same meaning as defined above). The tetrazole forming agent permits many kinds of solvents to be used and can in principle be used with any carbonitriles. In addition, the use of inexpensive zinc chloride leads to cost reduction.
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.
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 (2007/10/03)
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%).