摘要:
A diagnostic agent for infectious diseases which is capable of distinguishing among different kinds of bacterial species and which allows simple and non-invasive measurement and/or imaging in a short period of time is provided; and a screening method for a therapeutic agent for infectious diseases caused by microorganisms are provided.A diagnostic agent for infectious diseases caused by nitroimidazole susceptible microorganisms, containing an imidazole derivative or a fused imidazole derivative having at least one nitro group on an imidazole ring, or a labeled form thereof as an active ingredient is provided.
摘要:
Novel compounds containing a heteroatom-bearing bridge and novel complexes of these compounds with metals. The novel compounds and complexes are useful in diagnostic and therapeutic methods.
摘要:
Nitrobenzyl mustard quaternary salts of formula (I), ##STR1## and the pharmaceutically acceptable salts thereof, process for their manufacture and their chemotherapeutic use as hypoxia selective cytotoxic agents. Wherein, X represents a linker chain --CR.sub.1 R.sub.2 -- or CR.sub.1 .dbd.CR.sub.2-- (where R.sub.1 and R.sub.2 are separately H, lower alkyl, phenyl or nitrophenyl; Y is halogen or OSO.sub.2 R; Q is lower alkyl (optionaly substituted with alkyl and/or ether groups and containing up to 6 carbons) or nitrophenyl; Ar represents a mono- or bicyclic aromatic unit, R is lower alkyl optionally substituted with alkyl and/or other groups, and may contain up to eight carbon atoms. Z represents one or more of the groups NO.sub.2, SO.sub.2 R, CONHR, R, OR, SR, CF.sub.3 and aza (ring --CH.dbd.replaced by --N.dbd.); with the proviso that when H-Cl or Br, Q=Me, and X=CH.sub.2 -- then Ar.noteq.2-nitrophenyl or 4-nitrophenyl.
摘要:
Angiotensin II receptor antagonists having the formula: ##STR1## which are useful in regulating hypertension and in the treatment of congestive heart failure, renal failure, and glaucoma, pharmaceutical compositions including these antagonists, and methods of using these compounds to produce angiotensin II receptor antagonism in mammals.
摘要:
The present invention provides a thioformamide derivative represented by the following general formula (I) or a pharmacologically acceptable salt thereof, which is highly safe, easy to use, and useful as an excellent hypotensive or heart disease remedy: ##STR1## wherein Y represents ##STR2## or the like [wherein R.sup.7 represents benzyloxy or the like; R.sup.11 and R.sup.12 each represent hydrogen, hydroxyl, benzoyloxy, benzyloxy, ##STR3## (wherein R.sup.14 and R.sup.15 each represent hydrogen, benzyl or the like) or the like];Z represents --CH.sub.2 -- or the like; A represents imidazolyl or imidazopyridyl which may have one or two substituents, or the like; R.sup.1 and R.sup.2 each represent hydrogen, lower alkyl or the like; and R.sup.3 and R.sup.4 each represent hydrogen, lower alkyl or the like.
摘要翻译:PCT No.PCT / JP92 / 01297 Sec。 371日期1994年04月26日 102(e)日期1994年4月26日PCT提交1992年10月6日PCT公布。 出版物WO93 / 08168 日本1994年4月29日。本发明提供由以下通式(I)表示的硫代甲酰胺衍生物或其药理学上可接受的盐,其是高度安全,易于使用的,并且可用作优异的降压药或心脏病药物: (I)其中Y表示酰氧基等; R 11和R 12各自表示氢,羟基,苯甲酰氧基,苄氧基,苯甲酰基等)等。 Z表示-CH 2 - 等; A表示可具有一个或两个取代基的咪唑基或咪唑并吡啶等; R 1和R 2各自表示氢,低级烷基等; R 3和R 4各自表示氢,低级烷基等。
摘要:
Hydroxyalkylating agents of formula: ##STR1## in which R denotes alkyl, n is 2 or 3, R.sub.1 denotes hydrogen or alkyl and R.sub.2 denotes alkyl an unsubstituted or substituted phenyl or ##STR2## are useful inter alia for the preparation of 1-(hydroxyalkyl)imidazoles. They are made by reaction of a sulphonic acid or dimethyl sulphate with a corresponding decarboxylate ester.
摘要:
A compound of formula I ##STR1## in which formula: R.sub.1 represents hydrogen or an alkyl group;R.sub.2 -R.sub.5 represent hydrogen, alkyl aryl, aralkyl or alkaryl group; andn is 1 or 2.
摘要:
Compounds of the formula ##STR1## wherein R is hydrogen or methyl;R.sub.1 is straight or branched alkyl of 1 to 6 carbon atoms, hydroxy(alkyl of 1 to 6 carbon atoms), mono- or di-(alkoxy of 1 to 6 carbon atoms)(alkyl of 1 to 6 carbon atoms), (alkyl of 1 to 6 cabon atoms)thio(alkyl of 1 to 6 carbon atoms), cyano(alkyl of 1 to 6 carbon atoms), alkenyl, alkynyl, or cycloalkyl;R.sub.2 is hydrogen, alkyl of 1 to 3 carbon atoms, alkoxy of 1 to 3 carbon atoms or halogen; andX is pyrazol-3-yl, 1,2,4-triazol-3-yl, pyridin-2-yl, pyridin-3-yl, thiazol-4-yl, 2-methyl-thiazol-4-yl or 2-methylamino-thiazol-4-yl;tautomers thereof, and non-toxic, pharmacologiically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antiulcerogenics and gastric acid secretion inhibitors.
摘要:
Novel 0-(dialkylaminoalkyl)-1-alkyl-5-nitroimidazole-(2)-aldoximes are described as well as their manufacture and use for treating protozoal diseases. The novel compounds correspond to the general formula ##SPC1##In which R.sup.1 stand for a hydrogen atom, a methyl, ethyl or hydroxyethyl group, Z stands for a linear or branched alkylene chain of 2 to 3 carbon atoms, and R.sup.2 and R.sup.3 each stands for an identical or different lower alkyl radical having from 1 to 4 carbon atoms or the group --NR.sup.2 R.sup.3 can be part of a saturated heterocyclic ring which may contain further substituents preferably a methyl group or/and hetero atoms, such as, especially the pyrrolidine, piperidine, morpholine, thiamorpholine, tetrahydro-1,4-thiazine-1,1-dioxide and piperazine ring, and HX can be a non-toxic, physiologically acceptable acid.
摘要:
4(5)-Trifluoromethylimidazoles having optional substituents in the 1 and 2 positions are provided. The novel 4(5)trifluoromethylimidazoles are prepared by reacting a 1,1-dihalo3,3,3-trifluoroacetone compound with an appropriate carboxaldehyde and ammonia. The 4(5)-trifluoromethylimidazoles are useful as anti-gout and anti-hyperuricemic agents.