Nissan Chemical Industries Limited

Yukinori Masuda

Yoshimasa Kamikawaji

Keizo Tanikawa

Keisuke Odoi

Masayuki Sato

Tsutomu Higashiyama

Hiroo Matsumoto

Kazuhiko Ohrai

Kiyotomo Seto

Ryozo Sakoda

Toru Yamashita

Keisuke Ohdoi

Kyoko Nakayama

Taiji Furukawa

There is provided a T-type calcium channel blocker that is optically active 1,4-dihydropyridine compound, a pharmaceutically acceptable salt thereof or a solvate thereof, of formula (1) wherein Rand Rare independently of each other Calkyl group or Rand Rtogether form &#x2014;CRR&#x2014;CRR, &#x2014;CRR&#x2014;CRR&#x2014;CRR&#x2014; or &#x2014;CRR&#x2014;CRR&#x2014;CRR&#x2014;CRR&#x2014;, etc., Xand Xare independently of each other O or NR, Ar is optionally substituted phenyl group, etc., Rand Rare independently of each other Calkyl group, &#x2014;L&#x2014;NRR, CHO&#x2014;L&#x2014;NRRCN, &#x2014;L&#x2014;N(CHCH)NRor NRR, etc., Y is Calkyl group, &#x2014;L&#x2014;NRR and * is absolute configuration of R.

T-type calcium channel blocker

Medicines for cardiac insufficiency

Pyrazole compounds of formula �1! and their tautomers and salts: ##STR1## (wherein R.sup.1 is an alkyl group, etc.; R.sup.2 is a carboxyl group, etc.; R.sup.3 is a halogen atom, an alkyl group, a phenyl group, etc.; R.sup.4, R.sup.5 and R.sup.6 each are a hydrogen atom, a halogen atom, etc.; R.sup.7 is a carboxyl group, a 5-tetrazolyl group, etc.; X is a nitrogen atom, etc.; Y and Z each are CH, a nitrogen atom, etc.; A and E each are a methylene group, etc.; D is a phenyl group, etc.; G is a covalent bond, etc.). The compounds of the invention have an antagonistic effect against angiotensin II and are useful for prevention and remedy of hypertension, congestive cardiac insufficiency, chronic renal insufficiency, aldosteronism, hyper-intraocular pressure, etc.

Pyrazole derivatives

A compound of the formula (I): ##STR1## wherein X.sup.1 and X.sup.2 do not exist or represent oxygen atom; A represents OH or acyloxy group having 1 to 4 carbon atoms; B represents hydrogen atom; A and B together represent a bond; R.sup.1 and R.sup.2 represent hydrogen atom or alkyl group having 1 to 4 carbon atoms, or R.sup.1 and R.sup.2 together represent 1,2-ethylene, 1,3-propylene, 1,4-butylene or 1,5-pentylene, and these alkylene groups may be substituted by alkyl group having 1 to 4 carbon atoms; R.sup.3 represents amido group of the formula: ##STR2## wherein n, R.sup.4, R.sup.5, R.sup.6, R.sup.7. R.sup.8. R.sup.9, R.sup.10 and R.sup.11 represent specific groups, and the pharmacological acceptable salts of the compounds which can form salts have strong activity for lowering blood pressure, and process therefor and pharmaceutical use of the compounds.

Pyranobenzoxadiazole derivatives

A compounds of the formula (I): ##STR1## wherein A represents OH or OC(O)CH.sub.3-n X.sub.n, B represents hydrogen atom, or A and B together represent a bond; R.sup.1 represents hydrogen atom, R.sup.2 represents hydrogen atom, C(Z)CH.sub.3-n X.sub.n or C(Z)NHCH.sub.3-n X.sub.n or R.sup.1 and R.sup.2 together represents (CH.sub.2).sub.m, (CH.sub.2).sub.m-1 C(Z), N(R.sup.3)(CH.sub.2).sub.2 C(Z), (CH.sub.2).sub.m-2 NHC(Z) or (CH.sub.2).sub.m-2 OC(Z) in which X represents fluorine atom, chlorine atom, bromine atom, a methyl group or a methoxy group and n represents 0 or an integer of 1 to 3, Z represents oxygem atom or sulfur atom, m represents an integer of 4 or 5 and R.sup.3 represents hydrogen atom or a methyl group, and pharmacological acceptable salts of the compounds which can form salts, processes therefor and pharmaceutical use of the compounds.

Growing community of inventors

Saitama-ken, Japan

Yukinori Masuda