Abstract: The invention relates to a novel process for the preparation of the optically pure 2S- or 2R-indolinecarboxylic acid of the formula ##STR1## and salts thereof. The process comprises forming the heterocyclic 5-membered ring in formula I from an open chain precursor by diastereoselective cyclization.
Abstract: Compounds of formula (I), and pharmaceutically acceptable salts thereof: ##STR1## wherein: X is CH.sub.2, O, S or NR.sub.4 wherein R.sub.4 is hydrogen or C.sub.1-4 alkyl;one of Y and Z is NR.sub.5 and the other is CR.sub.6 R.sub.7 wherein R.sub.5 is hydrogen, C.sub.1-4 alkyl or C.sub.1-4 acyl and R.sub.6 and R.sub.7 are either both hydrogen or together form an oxo group;R.sub.1 is hydrogen, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.4-7 cycloalkenyl or C.sub.1-4 alkyl substituted by C.sub.2-7 alkenyl, C.sub.2-7 alkynyl, C.sub.3-7 cycloalkyl, amino optionally substituted by one or two C.sub.1-4 alkyl or by C.sub.4-6 polymethylene optionally containing an oxygen atom or by phenyl C.sub.1-4 alkyl optionally substituted in the phenyl ring by C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or trifluoromethyl; andR.sub.2 and R.sub.3 are the same or different and are hydrogen, halogen, hydroxy, C.sub.1-4 alkyl C.sub.
Abstract: Antibiotic substance named saframycin S having antibacterial activities and produced by decyanating antibiotic saframycin A or cultivating Streptomyces lavendulae strain No. 314 and recovering saframycin S from a cultured broth.
Type:
Grant
Filed:
September 23, 1980
Date of Patent:
February 8, 1983
Assignee:
Tadashi Arai
Inventors:
Tadashi Arai, Katsuhiro Takahashi, Kimiko Ishiguro, Koji Yokoyama
Abstract: New heterocyclylcarboxylic acid derivatives which are acylated in the nucleus, especially benz-acyl-benzimidazole-2-carboxylic acid derivatives of the formula ##STR1## in which R is a free, esterified or amidated carboxyl group or a free, etherified or esterified hydroxymethyl group, R.sub.1 is an aliphatic, cycloaliphatic, aromatic, araliphatic, heterocyclic or heterocyclic-aliphatic radical, R.sub.2 is hydrogen or an aliphatic radical and Ph is a 1,2-phenylene group containing the radical R.sub.1 --C(.dbd.O)--, with the proviso that R.sub.1 contains at least 2 carbon atoms if Ph is otherwise unsubstituted, R.sub.2 is ethyl and R is acetoxymethyl, and salts of such compounds having salt-forming properties, are useful as anti-allergic agents.
Type:
Grant
Filed:
August 18, 1977
Date of Patent:
February 27, 1979
Assignee:
Ciba-Geigy Corporation
Inventors:
Ernst Habicht, Pier G. Ferrini, Alfred Sallmann