摘要:
Disclosed is to prevent generation of byproducts or a deterioration in the physical properties of a polythiol composition that may be caused by active oxygen during storage thereof by way of controlling the content of active oxygen in the polythiol composition after the synthesis of the polythiol. As a result, it is possible to enhance the long-term storage stability of a polythiol composition after it has been synthesized until it is used in the polymerization reaction.
摘要:
The present disclosure features a strain-promoted [2+2+2] reaction that can be carried out under physiological conditions. In general, the reaction involves reacting a pi-electrophile with a low lying LUMO with a quadricyclane on a biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provides for its application in vivo and in vitro. The reaction is compatible with modification of living cells. In certain embodiments, the pi-electrophile can comprise a molecule of interest that is desired for delivery to a quadricyclane-containing biomolecule via [2+2+2] reaction.
摘要:
The present invention discloses cysteine prodrugs having the general formula: cystine dimers of the cysteine prodrugs having the general formula: protected cysteine analogs having the general formula: and dimers of the protected cysteine analogs having the general formula: The invention further encompasses pharmaceutical compositions containing the disclosed prodrugs, dimers, and analogs, and methods of using such compounds for treatment of schizophrenia and drug addiction.
摘要:
A method and a composition for treating or reducing and/or controlling intraocular pressure comprising administering an effective amount of a renin inhibiting compound of the formula: ##STR1## wherein A is a substituent; W is CO or CHOH and U is CH.sub.2 or NR.sub.2 wherein R.sub.2 is hydrogen or loweralkyl; with the proviso that when W is CHOH then U is CH.sub.2 ; R.sub.1 is loweralkyl, cycloalkyl, benzyl, (alpha, alpha)-dimethylbenzyl, 4-hydroxybenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, phenethyl, 1-benzyloxyethyl, phenoxy, thiophenoxy or anilino; R.sub.3 is loweralkyl, loweralkenyl, ((alkoxy)alkoxy)alkyl, carboxyalkyl, (thioalkoxy)alkyl, benzyl or heterocyclic ring substituted methyl; and R.sub.4 is a substituted amino group; or pharmaceutically acceptable salts or esters thereof.Also disclosed are compositions, methods and kits for treating glaucoma or reducing and/or controlling intraocular pressure wherein the renin inhibiting compound is administered in combination with a beta-adrenergic antagonist, a steroidal antiinflammatory agent or an angiotensin converting enzyme inhibiting compound.
摘要:
The present invention relates to a polythiol composition that includes (a) a polythiol compound (A) having at least two thiol groups; and (b) a nitrogen-containing compound (B) represented by the following Formula (I), In Formula (I), —S—R is a residue of the polythiol compound (A). A peak area of the nitrogen-containing compound (B) is equal to or less than 3.0, with respect to a peak area of 100 of the polythiol compound (A). Each peak area for compounds (A) and (B) is determined by high performance liquid chromatography analysis. The present invention also relates to a polymerizable composition that includes the polythiol composition, and polymerizates thereof.
摘要:
2-Aroylcyclohexanediones I ##STR1## (A is C.sub.1 -C.sub.6 -alkylene; R.sup.1 is substituted phenyl or hetaryl which may furthermore carry a fused ring; R.sup.2 -R.sup.5 are each hydrogen or C.sub.1 -C.sub.4 -alkyl; R.sup.6 is H, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkoxycarbonyl and R.sup.7 is C.sub.1 -C.sub.4 -alkyl,with the proviso that R.sup.1 is not mono- or dihalophenyl)and the agriculturally useful salts thereof and the esters of I with C.sub.1 -C.sub.10 -carboxylic acids or inorganic acids.The 2-aroylcyclohexanediones I are suitable as herbicides and plant growth regulators.
摘要翻译:2-芳酰基环己烷二酮I(A是C 1 -C 6 - 亚烷基; R 1是取代的苯基或杂芳基,其还可以带有稠环; R 2 -R 5各自是氢或C 1 -C 4 - 烷基; R 6是H, C4-烷基或C1-C4-烷氧基羰基,R7为C1-C4-烷基,条件是R1不是单 - 或二卤代苯基)及其农业上有用的盐和I与C1-C10-羧酸或无机 酸。 2-芳酰基环己烷二酮I适用作除草剂和植物生长调节剂。
摘要:
Bicyclic derivatives of the formula ##STR1## wherein X.sup.1, X.sup.2, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7a, R.sup.7b, and R.sup.8 are as defined in the specification. These compounds are antimicrobially active.
摘要:
Unsymmetrical organic disulfide sulfinate compounds, useful as an antiradiation agents, having the general formula: ##STR1## wherein A is one or of the following polar groups, OH, COOH, SO.sub.3 Na, --C(O)--, or derivatives such as esters and nonamino nitrogen derivatives such as amides or nitriles; k is an integer of one to eight; Y is a straight or substituted aliphatic chain haivng from two to eight carbon atoms which may have one or more S--S groups interposed therebetween; m signifies the number of carbon atoms in an aliphatic chain Y containing 2 to 8 carbon stoms which may have S--S interposed; aliphatic chain Y, substituted with one or more polar groups of the number k is attached to one of the two sulfur atoms shown. The second sulfur atom is attached through an aliphatic chain of 2 to 5 carbon atoms to the sulfinate function SO.sub.2 M wherein R.sup.1 and R.sup.2 may be hydrogen, aryl, cycloalkyl or various polar groups such as OH, COOH, SO.sub.3 Na, --C(O)--, or derivatives such as esters and nonamino derivatives such as amides or nitriles. The system ##STR2## also may comprise an aromatic ring; n may be the integers 2 through 6; M of the sulfinate function is hydrogen, a metallic element selected from group 1 A of the Periodic Table such as Li, Na, or K, or the equivalent R.sub.4 N+; or an organic group such as a straight or substituted aliphatic chain having up to 4 carbon atoms, designed to promote stability. The synthesis of the compounds occurs by subjecting 1,1-dioxides of cyclic disulfidesto the action of a thiolate ion, whereby cleavage is effected between the sulfur and sulfonyl units.
摘要:
Fungicidal and plant growth-regulsting azolylmethylcyclopropyl derivatives of the formula ##STR1## in which R represents halogen, alkyl or optionally substituted phenyl, or represents the groupings --Y--R.sup.2,whereinY represents oxygen, sulphur, SO or SO.sub.2 andR.sup.2 represents optionally substituted phenyl,R.sup.1 represents hydrogen, alkyl or acyl,X represents nitrogen or a CH group,Z represents halogen, alkyl with 1 to 4 carbon atoms, alkoxy with 1 to 4 carbon atoms, alkylthio with 1 to 4 carbon atoms, halogenoalkyl with 1 or 2 carbon atoms and 1 to 5 halogen atoms, halogenoalkoxy with 1 or 2 carbon atoms and 1 to 5 halogen atoms, halogenoalkylthio with 1 or 2 carbon atoms and 1 to 5 halogen atoms or phenyl which is optionally substituted by aklyl with 1 or 2 carbon atoms and/or halogen, or represents phenoxy which is optionally substituted by alkyl with 1 or 2 carbon atoms and/or halogen andm represents the number 0, 1, 2 or 3,and addition products thereof with acids and metal salts. Intermediates therefor of the formulas ##STR2## are also new.
摘要:
The invention relates to methods of treating cell proliferative disorders. The invention further relates to pharmaceutical compositions for treating cell proliferative disorders, especially cancer.