摘要:
The invention relates to aryl substituted heterocyclyl sulfones as voltage gated calcium channel blockers, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
摘要:
The present invention provides catalysts, methods, and reactor systems for converting oxygenated hydrocarbons to oxygenated compounds. The invention includes methods for producing cyclic ethers, monooxygenates, dioxygenates, ketones, aldehydes, carboxylic acids, and alcohols from oxygenated hydrocarbons, such as carbohydrates, sugars, sugar alcohols, sugar degradation products, and the like, using catalysts containing palladium, molybdenum, tin, and tungsten. The oxygenated compounds produced are useful in the production of liquid fuels, chemicals, and other products.
摘要:
The present invention relates to dielectrically positive liquid-crystalline media comprising in each case one or more compounds of the formula I in which the parameters have the respective meanings indicated in the specification, and optionally one or more further dielectrically positive compounds and optionally one or more further dielectrically neutral compounds, and to liquid-crystal displays containing these media, especially to active-matrix displays and in particular to TN, IPS and FFS displays.
摘要:
The present invention is directed to ester derivatives of levulinic acid that are useful as plasticizers and/or coalescent solvents in polymer compositions, compositions comprising the ester derivatives, methods of making the derivatives and the compositions, and the use of the derivatives as additives in polymer compositions.
摘要:
Novel benzenedicarboxamides of the formula (I) wherein X represents hydrogen, halogen atom, nitro, C1-6alkylsulfonyloxy, C1-6alkylsulfinyl, C1-6alkylsulfenyl or C1-6alkylsulfonyl, R1 represents C1-6alkyl, C1-6alkylthio-C1-6alkyl, or C1-6alkyl, m represents 0 or 1, A represents O, S, SO, SO2, CH2 or CH(CH3), and Q represents a 5- or 6-membered heterocyclic group that contains at least one hetero atom selected from the group consisting of N, O and S and can be optionally substituted; processes for their preparation, their intermediates and their use as insecticides.
摘要:
The invention relates to quinazoline derivatives of formula (1) wherein m is an integer from 1 to 2; R1 represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, C1-3alkyl, C1-3alkoxy, C1-3alkylthio, or —NR5R6 (wherein R5 and R6, which may be the same or different, each represents hydrogen or C1-3alkyl); R2 represents hydrogen, hydroxy, halogeno, methoxy, amino or nitro; R3 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; X1 represents —O—, —CH2—, —S—, —SO—, —SO2—, —NR7CO—, —CONR8—, —SO2NR9—, —NR10SO2— or —NR11— (wherein R7, R8, R9, R10 and R11 each independently represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl); R4 represents an optionally substituted 5 or 6 membered saturated carbocyclic or heterocyclic group or a group which is alkenyl, alkynyl or optionally substituted alkyl, which alkyl group may contain a heteroatom linking group, which alkenyl, alkynyl or alkyl group may carry a terminal optionally substituted group selected from alkyl and a 5 or 6 membered saturated carbocyclic or heterocyclic group, and salts thereof; processes for their preparation, pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as active ingredient. The compounds of formula (I) and pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.
摘要:
Novel chemical compounds that can be used to synthesize halichondrin B and norhalichondrin B, and related derivatives, are described. The synthesis of halichondrin B and norhalichondrin B from these compounds also is described.
摘要:
A process for the manufacture of .beta.-bromoalkylsulfones and .beta.-bromoalkenylsulfones by addition reaction of sulfonic acid bromides with olefins or acetylenes in the presence of hydroperoxide and, optionally, of metal salts. Starting materials for further syntheses and for biologically active compounds may be obtained by subsequent dehydrobromination of the addition products.
(2-HAL,4-(R-OOC-Z-)PHENYL)-CH WHEREIN X IS SELECTED FROM THE GROUP CONSISTING OF OXYGEN, SULFUR, SO AND SO2, R IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, ANION OF A NON-TOXIC; THERAPEUTICALLY ACCEPTABLE ORGANIC OR MINERAL BASE AND RESIDUE OF AN ALCOHOL, AN Z IS SELCETED FROM THE GROUP CONSISTING OF -CHR1- AND >C=R2 WHEREIN R1 IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND STRAINGT OR BRANCHED ALKYL OF 1 TO 4 CARBON ATOMS, AND R2 IS A STRAIGHT OR BRANCHED ALKYLIDENE OF 1 TO 4 CARBON ATOMS AND HAL IS SELECTED FROM THE GROUP CONSISTING OF FLUORINE, BROMINE AND CHLORINE, WHICH COMPOUNDS WHICH CONTAIN AT LEAST ONE ASYMMETRIC CARBON ATOM CAN BE IN RACEMIC OR OPTICALLY ACTIVE GORM, AND THEIR PREPARATION WHICH COMPOUNDS HAVE ANALGESIC AND ANTIINFLAMMATORY ACTIVITY.
摘要:
Methods, compounds, and compositions of conjugating anthracyclines to a carbohydrate polymer backbone via click chemistry are provided. The conjugation of anthracyclines utilizing a reaction between a hydrazone azide moiety and alkyne moiety provide for compositions with less crosslinking, and thereby increasing the efficacy of targeted drug delivery. The methods further provide for controlled loading of anthracycline to a carbohydrate polymer backbone.