摘要:
Compounds of formula (I): ##STR1## [wherein R.sup.1 represents a group of formula (II) or (III): ##STR2## R.sup.2 is alkyl, alkenyl or alkynyl; R.sup.3 and R.sup.4 are each hydrogen, alkyl, alkenyl or alkynyl; R.sup.5 is hydrogen or a carboxy-protecting group; R.sup.a is hydrogen or a group of formula and --OR.sup.6 ; R.sup.6, R.sup.6a and R.sup.6b are each hydrogen, a hydroxy-protecting group, alkyl, alkanesulfonyl, halogenated alkanesulfonyl or arylsulfonyl] and their salts and esters have the ability to inhibit the synthesis of cholesterol, and can thus be used for the treatment and prophylaxis of hypercholesterolemia and of various cardiac disorders.
摘要翻译:式(I)化合物:其中R 1表示式(II)或(III)的基团:烯基或炔基; R3和R4各自为氢,烷基,烯基或炔基; R5是氢或羧基保护基; R a是氢或式-OR 6基团; R6,R6a和R6b各自为氢,羟基保护基,烷基,烷基磺酰基,卤代烷磺酰基或芳基磺酰基),其盐和酯具有抑制胆固醇合成的能力,因此可用于治疗和预防 高胆固醇血症和各种心脏疾病。
摘要:
Polyurethane foams having improved retention of insulative properties can be prepared using one or more of two novel polyols. One of the polyols is a polyether prepared by reacting a monoepoxide with a compound having the general formula: ##STR1## wherein X is H, Li, Na, K; A is N, S or O; L is a covalent bond or a connecting group having from 1 to 10 carbons; M is any group capable of reacting with an ethylene oxide molecule in the presence of a basic catalyst; and J is an integer from 2 to 8. The other polyol is prepared by (1) admixing ethylene carbonate and one or more hydroxyl functional compounds under reaction conditions sufficient to react the ethylene carbonate and the hydroxyl functional compounds to produce a polyol precursor, and (2) admixing the polyol precursor with diethylene glycol and an anhydride, a dicarboxylic acid, a tricarboxylic acid or mixtures thereof, optionally in the presence of a catalyst.
摘要:
Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof have been found to possess activity as cell-selective HMG-CoA reductase inhibitors, thus making them useful as antihypercholesterolemic agents. In the above formula, ##STR2## R.sup.1 is hydrogen, alkyl, cycloalkyl, aryl or arylalkyl; and R.sup.2 is hydrogen, alkyl, ammonium, or alkali metal.
摘要:
A method of treating hyperproliferative skin diseases, such as psoriasis, using a compound of formula ##STR1## wherein R.sub.1 is hydrogen when R.sub.2 is hydroxy, and R.sub.1 is methyl when R.sub.2 is hydrogen; and A is alkyl; cycloalkyl; alkenyl; alkyl substituted with trifluoromethyl; phenyl; halophenyl; phenyl-C.sub.1-3 alkyl; phenyl-C.sub.1-3 alkyl substituted on the phenyl with 1 to 3 substituents selected from the group consisting of halo, C.sub.1-3 alkyl, and C.sub.1-3 alkoxy; orA is ##STR2## wherein R.sub.3 is hydrogen or ##STR3## R.sub.4 is hydrogen or methyl, and n is 1 to 5, or the corresponding hydroxy acid of formula ##STR4## or a pharmaceutically acceptable salt of said acid, an alkyl ester of said acid, an acetylamino-substituted-C.sub.1-4 alkyl ester of said acid, a phenyl-dimethylamino ester of said acid or a .alpha.-monoglyceride of said acid.
摘要:
Bicyclic decanedioic acids corresponding to the following general formula ##STR1## in which R represents a C.sub.1 -C.sub.22 alkyl radical, a C.sub.2 -C.sub.34 alkylcarbonyl radical, or a residue of a polyalkoxylated C.sub.2 -C.sub.22 fatty alcohol, represent a new class of dicarboxylic acids which are useful as flotation aids in the flotation of non-sulfidic ores.
摘要:
Novel antiandrogenic compositions comprising an antiandrogenically effective amount of at least one compound of the formula ##STR1## wherein R is alkyl of 1 to 4 carbon atoms, R.sub.1 is alkyl of 1 to 2 carbon atoms, R.sub.2 is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms optionally interrupted with a heteroatom, alkenyl and alkynyl of 2 to 8 carbon atoms optionally interrupted with a heteroatom, formyl and acyl of an organic carboxylic acid of 2 to 18 carbon atoms, R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms, R.sub.4 is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, the dotted lines indicate optional presence of a double bond between the 4(5) and 5a(6) carbons and the wavy line indicates that R.sub.4 may be in the .alpha.- or .beta.-position and a non-toxic, pharmaceutical carrier or excipient and a method of treating hyperandrogenic conditions in warm-blooded animals.
摘要:
A compound of the formula ##STR1## wherein R is halogen, C.sub.1 -C.sub.2 alkyl, C.sub.1 -C.sub.2 alkoxy, nitro; cyano; C.sub.1 -C.sub.2 haloalkyl, or R.sup.a SO.sub.m -wherein m is 0 or 2 and R.sup.a is C.sub.1 -C.sub.2 alkyl; R.sup.1 is hydrogen or C.sub.1 -C.sub.2 alkyl; R.sup.2 is hydrogen or C.sub.1 -C.sub.4 alkyl; or R.sup.1 and R.sup.2 together are alkylene having 2 to 5 carbon atoms; R.sup.3 is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sup.4 is hydrogen or C.sub.1 -C.sub.4 alkyl; or R.sup.3 and R.sup.4 together are oxo; R.sup.5 is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sup.6 is hydrogen or C.sub.1 -C.sub.4 alkyl; or R.sup.5 and R.sup.6 together are alkylene having 2 to 5 carbon atoms; R.sup.7 and R.sup.8 independently are (1) hydrogen; (2) halogen; (3) C.sub.1 -C.sub.4 alkyl; (4) C.sub.1 - C.sub.4 alkoxy; (5) trifluoromethoxy; (6) cyano; (7) nitro; (8) C.sub.1 -C.sub.4 haloalkyl; (9) R.sup.b SO.sub.n -wherein n is the integer 0, 1 or 2; and R.sup.b is (a) C.sub.1 -C.sub.4 alkyl; (b) C.sub.1 -C.sub.4 alkyl substituted with halogen or cyano; (c) phenyl; or (d) benzyl; (10) -NR.sup.c R.sup.d wherein R.sup.c and R.sup.d independently are hydrogen or C.sub.1 -C.sub.4 alkyl; (11) R.sup.e C(O)- wherein R.sup.e is C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy; (12) SO.sub.2 NR.sup.c R.sup.d wherein R.sup.c and R.sup.d are as defined; or (13) -N(R.sup.c)C(O)R.sup.d wherein R.sup.c and R.sup.d are as defined; and R.sup.9 is (a) C.sub.1 -C.sub.6 alkyl; (b) C.sub.4 -C.sub.6 cycloalkyl; (c) substituted C.sub.1 -C.sub.6 alkyl; (d) phenyl-SO.sub.2 -; (e) substituted phenyl-SO.sub.2 -; (f) C.sub.1 -C.sub.6 -alkyl-SO.sub.2 -, optionally substituted; (g) C.sub.1 -C.sub.6 alkyl-C(O)-, optionally substituted; (h) phenyl-C(O)-, optionally substituted; (i) benzyl; or (h) C.sub.3 -C.sub.6 alkenyl.
摘要:
A process for the preparation of ethyl trifluoroacetate, in which:in a first stage, trifluoroacetic acid is brought into contact with a slight excess of ethanol in the presence of concentrated sulfuric acid and a solvent, the solvent having a boiling point higher than that of trifluoroacetic acid and specific gravity relative to water less than 1 and which solvent does not form an azeotrope with ethyl trifluoroacetate, and then carrying out a phase separation and removing the sulfuric layer, followed, if required, by an additional stage in which concentrated sulfuric acid is added to complete the esterification;in a second stage, an additional quantity of sulfuric acid and trifluoroacetic acid is introduced and a phase separation is then carried out to remove the sulfuric layer; andin a third stage, the mixture obtained in the second stage is distilled to recover ethyl trifluoroacetate.
摘要:
New bicyclohexylethanes of formula IR1--Cy--Cy--CH2CH2--A--(Cy)n--R2 (I)wherein R1 is alkyl; R2 is alkyl, in which one or two non-adjacent CH.sub.2 groups can be replaced by 0 atoms, or is F, Cl, Br, CN, --COOalkyl or --O--CO--alkyl; or one of the radicals R.sup.1 and R.sup.2 can also be H; A is Cy, or 1,4-phenylene which is unsubstituted or substituted by one or two F and/or Cl atoms and/or CH.sub.3 groups or by a CN group; Cy is 1,4-cyclohexylene and n is 0 or 1; the alkyl groups in each case containing 1-10 C atoms, with the proviso that n is 1 if A is Cy and R2 is CN, can be used as constituents of dielectrics for electrooptical display elements.