摘要:
Bicyclic fused benzenoid compounds of the formula ##STR1## and pharmaceutically acceptable cationic and acid addition salts thereof, where M is O, CH.sub.2 or NR.sub.6 ; R.sub.6 is hydrogen, formyl, carbobenzyloxy or certain carboalkoxyalkyl, alkanoyl, alkyl, aralkyl or aralkylcarbonyl groups;A' is:(1) A where one of A and B is hydrogen such that when A is hydrogen, B is C(R.sub.2 R.sub.3)(CH.sub.2).sub.f Q and f is 1 or 2; when B is hydrogen, A is C(R.sub.2 R.sub.3)(CH.sub.2).sub.f Q and f is 0 or 1, when taken together A and OR.sub.1 form a lactone or certain derivatives thereof;(2) A' is ##STR2## (3) A' is Q.sub.3 ; Q is CO.sub.2 R.sub.7, COR.sub.8, C(OH)R.sub.8 R.sub.9, CN, CONR.sub.12 R.sub.13, CH.sub.2 NR.sub.12 R.sub.13, CH.sub.2 NHCOR.sub.14, CH.sub.2 NHSO.sub.2 R.sub.17 or 5-tetrazoyl;Q.sub.3 is ##STR3## 5-tetrazolyl, CH.sub.2 CONHCOR.sub.7, COOH or certain ester, amide, carboximido or sulfonimido derivatives thereof, CONHOH, CONHCONH.sub.2, or COCH.sub.2 Q.sub.4 where Q.sub.4 is CN or COOH or certain esters thereof;R.sub.1 is hydrogen, benzyl or certain acyl groups; R.sub.4 is hydrogen, certain alkyl or certain aralkyl groups; R.sub.5 is hydrogen or certain alkyl groups; Z is (C.sub.1 -C.sub.9)alkylene, optionally interrupted by O, S, SO or SO.sub.2 ; and W is hydrogen, methyl, certain aryl or cycloalkyl groups; useful in mammals as analgesics, tranquilizers, anteimetic agents, diuretics, anticonvulsants, antidiarrheals, antitussives, in treatment of glaucoma, and intermediates therefore.
摘要翻译:式(I')的双环稠合苯并噻唑类化合物及其药学上可接受的阳离子和酸加成盐,其中M为O,CH 2或NR 6; R6是氢,甲酰基,苄氧羰基或某些烷氧基烷基,烷酰基,烷基,芳烷基或芳烷基羰基; A'为:(1)其中A和B之一为氢,使得当A为氢时,B为C(R2R3)(CH2)fQ且f为1或2; 当B为氢时,A为C(R2R3)(CH2)fQ,f为0或1,当A和OR1一起形成内酯或其某些衍生物时; (2)A'是(3)A'是Q3; Q是CO 2 R 7,COR 8,C(OH)R 8 R 9,CN,CONR 12 R 13,CH 2 NR 12 R 13,CH 2 NHCOR 14,CH 2 NHSO 2 R 17或5-四唑基; Q 4是CN或COOH或其某些酯; Q 3是CN,COOH或其某些酯;其中Q 4是CN或COOH或其某些酯; R1是氢,苄基或某些酰基; R4是氢,某些烷基或某些芳烷基; R5是氢或某些烷基; Z是(C1-C9)亚烷基,任选地被O,S,SO或SO 2中断; W是氢,甲基,某些芳基或环烷基; 因此在哺乳动物中作为止痛剂,止痛剂,促炎剂,利尿剂,抗惊厥药,止泻药,镇咳药,治疗青光眼有用。
摘要:
Compounds having the formula ##STR1## R.sub.1 is hydrogen, benzyl or alkanoyl, X is C.sub.2-4 alkylene; andZ-W is alkyl, phenylalkyl or pyridylalkyl which can have an oxygen atom as part of the alkyl chain and their use as CNS agents, antidiarrheals and antiemetics. Processes for their preparation and intermediates therefor are described.
摘要:
Compounds useful for treating inflammation, swelling and associated pain, represented by the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein: a is an integer of 0-3;b is an integer of 0-2;n is an integer of 3-12;each X and each Y are independently -halo, --R.sup.1, -alkoxy, or -phenyl; andB is selected from the group consisting of:--NR.sup.1 R.sup.2, --NR.sup.1 (CH.sub.2 CH.sub.2 OH), ##STR2## in which R.sup.1 and R.sup.2 are independently H, alkyl or cycloalkyl;R.sup.3 is H, alkyl or --CH.sub.2 CH.sub.2 OH; andm is an integer of 3-8.Novel compounds are those wherein n is at least 6 if both a and b are 0.
摘要:
Herbicidal mixtures comprising (1) a diphenyl ether of the formula: ##STR1## or a salt thereof, wherein R.sup.1 is, for example, alkyl; R.sup.2 is hydrogen, halogen or nitro; R.sup.3 is hydrogen, halogen, alkyl, trifluoromethyl or cyano; R.sup.4 is hydrogen, halogen or trifluoromethyl; R.sup.5 is hydrogen, halogen or trifluoromethyl and R.sup.6 is hydrogen or alkyl of 1 to 6 carbons and (2) another herbicide not of formula (I). Intermediates for preparing the formula (I) compounds and processes for using these compounds are also disclosed.
摘要:
The invention provides novel compounds of the formula: ##STR1## wherein n is 0 to 4, R.sub.1 and R.sub.2, which can be the same or different are H, OH, alkoxy of 1 to 4 carbon atoms, benzyloxy or methoxymethoxy; R.sub.3 is H, OH, halogen, alkoxy of 1 to 4 carbon atoms, benzyloxy, methoxymethoxy, 2,3-dihydroxypropoxy or ##STR2## wherein m is 1 or 2, R.sub.6 and R.sub.7, which can be the same or different are H or an alkyl group of 1 to 4 carbon atoms, or ##STR3## can form an N-containing three-, four-, five- or six-membered heterocyclic ring; R.sub.4 is OH, F, Cl, Br, I, mesyloxy, tosyloxy, alkylcarbonyloxy of 1 to 4 C-atoms, formyloxy or CH.sub.2 R.sub.4 is replaced by CHO; R.sub.5 is H or OH; or R.sub.4 and R.sub.5 together form an --O-- bridge between the carbon atoms to which they are attached, and their non-toxic pharmaceutically acceptable salts and esters and mixtures thereof. Processes for the preparation of these compounds are described, and also novel pharmaceutical compositions containing them. These compounds exhibit valuable pharmacological properties as estrogenic, anti-estrogenic, and progestanic agents. They are also effective against oestrogen-dependent tumors. Certain compounds are useful as chemical intermediates for the preparation of pharmacologically active compounds of the invention.
摘要翻译:本发明提供新的下式化合物:其中n为0至4,可以相同或不同的是H,OH,1至4的烷氧基,其中n为0至4, 碳原子,苄氧基或甲氧基甲氧基; R 3是H,OH,卤素,1至4个碳原子的烷氧基,苄氧基,甲氧基甲氧基,2,3-二羟基丙氧基或其中m是1或2,R6和R7可以相同或不同,是H或 1至4个碳原子的烷基或者可以形成含N的三,四,五或六元杂环; R4是OH,F,Cl,Br,I,甲磺酰氧基,甲苯磺酰氧基,1至4个C原子的烷基羰基氧基,甲酰氧基或CH 2 R 4被CHO取代; R5是H或OH; 或R4和R5一起在它们所连接的碳原子之间形成-O-桥,以及它们的无毒的药学上可接受的盐和酯及其混合物。 本发明描述了制备这些化合物的方法,以及含有它们的新型药物组合物。 这些化合物表现出有价值的药理学性质,如雌激素,抗雌激素和孕激素。 它们也有效抵抗雌激素依赖性肿瘤。 某些化合物可用作制备本发明的药理活性化合物的化学中间体。
摘要:
Triphenylalkene derivatives, in particular 1-(p-.beta.-dimethylaminoethyoxyphenyl)-1,2-diphenylbut-1-ene, which possess utility as anti-oestrogens.
摘要:
The invention relates to new 4-hydroxy-benzhydrols of the formula (I) ##STR1## wherein R.sub.1 and R.sub.2 independently represent hydrogen, halogen, trihalomethyl, alkyl having from one to 4 carbon atoms or alkoxy having from one to 4 carbon atoms, with the proviso that if R.sub.1 is hydrogen, R.sub.2 is other than hydrogen or a 3-trifluoromethyl group, or if R.sub.1 is a 2-methyl group, R.sub.2 is other than a 5-methyl group.According to another aspect of the invention there are provided processes for the preparation of these compounds.The compounds of the formula (I) are pharmacologically active. In particular, they are suitable for the treatment of acute ethanolic intoxication. Pharmaceutical compositions containing them as active ingredients are also within the scope of the invention.
摘要:
Conversion, e.g. dehydration of aliphatic organic oxygenates having up to about 6 carbon atoms by contact with a crystalline aluminosilicate zeolite, preferably ZSM-5, having a silica to alumina ratio substantially greater than 10, at a temperature of about 70.degree. to 1400.degree. F., depending upon the exact nature of the reactant and product.
摘要:
At least one of the other functions comprising an aryl-aliphatic ether, e.g., veratrol, is catalytically hydrolyzed with water, e.g., to guaiacol, in the presence of a catalytically effective amount of a salt of a carboxylic acid.
摘要:
A process for producing 4,4'-dihydroxydiphenyl which comprises subjecting to alkali fusion 1 mol of 4,4'-diphenyldisulfonic acid and/or potassium 4,4'-diphenyldisulfonate together with 4 to 10 mol of potassium hydroxide and 0.1 to 2 mol of potassium sulfate. Alternatively, the process may comprise subjecting to alkali fusion 4,4'-diphenyldisulfonic acid in the presence of potassium hydroxide, controlling to 20 to 25% the potassium hydroxide concentration in the reaction mixture, and separating dipotassium salt of 4,4'-dihydroxydiphenyl.