Abstract: Provided is a stereoselective synthesis of an intermediate for the preparation of the heterocyclic derivative as a Cap-dependent endonuclease inhibitor. The synthesis process has the advantages of simple operation, higher yield and relatively controllable steroselectivity, such that it is suitable for large-scale production.

Abstract: Provided is a stereoselective synthesis of an intermediate for the preparation of the heterocyclic derivative as a Cap-dependent endonuclease inhibitor. The synthesis process has the advantages of simple operation, higher yield and relatively controllable steroselectivity, such that it is suitable for large-scale production.

Abstract: A trans-isomeric compound of formula (I) below or a pharmaceutically acceptable salt thereof: in which R1 is C1-C5 alkyl or C3-C5 cycloalkyl and the trans-isomeric compound has a trans:cis ratio of at least 70:30. Further disclosed is a method for preparing the trans-isomeric compound.

Abstract: A trans-isomeric compound of formula (I) below or a pharmaceutically acceptable salt thereof: in which R1 is C1-C5 alkyl or C3-C5 cycloalkyl and the trans-isomeric compound has a trans:cis ratio of at least 70:30. Further disclosed is a method for preparing the trans-isomeric compound.

Abstract: This invention relates to a malic acid salt of (3S,5R)-7-[3-amino-5-methyl-piperidinyl]-1-cyclopropyl-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid. Also disclosed is a method of treating bacterial infection by an effective amount of this salt.

Abstract: This invention relates to dialdehyde or dinitrile compounds, which are useful for stereoselective synthesis of piperidine, pyrrolidine, and azepane derivatives.

Abstract: A method for synthesis of C2-symmetric diamino diol mediated by titanium complexes is provided. A substituted-L-phenylalaninal undergoes pinacol coupling to yield the corresponding C2-symmetric (1S,2R,3R,4S)-1,4-diamino 2,3-diol in the presence of Cp2TiCl2/ZnCl2 and zinc metal, mediated in good yield and highly selective. This titanium-catalyzed reaction yields diaminodiol, offering a convenient alternative method to the synthesis of C2-symmetric peptidic protease inhibitors. Consequently, the method allows to synthesize TL-3 via titanium complex in moderate yield.

Abstract: This invention relates to treating diabetes mellitus with certain 4-hydroxyfuroic acid derivatives. These derivates are of formula (I) below. Each variable is defined in the specification.

Abstract: This invention relates to a method of treating liver cancer, comprising administering to a subject in need thereof an effective amount of a compound of formula (I): In formula (I), each of R1 and R2, independently, is H, C1-C10 alkyl, C3-C20 cycloalkyl, C3-C20 heterocycloalkyl, aryl, heteroaryl, or C(O)Ra; X is Se, S, O, or NRb; and each of R3, R4, R5, and R6, independently, is H, C1-C10 alkyl, C3-C20 cycloalkyl, C3-C20 heterocycloalkyl, aryl, or heteroaryl; in which each of Ra and Rb, independently, is H or C1-C10 alkyl.

Abstract: Disclosed are novel 1,2,4-triazin-5-one biphenyl derivatives having structural formula (I) useful as non-peptide antagonists of angiotensin II receptor: ##STR1## where R.sub.1 represents alkyl, cycloalkyl, or substituted or unsubstituted aryl;R.sub.2 represents alkyl, substituted or unsubstituted aryl, or arylalkyl;A and D independently represent C--R.sub.3, N, NH or C.dbd.O, wherein when A and D independently denote C--R.sub.3 or N, b and c are independently a double bond, and when A and D independently denote NH or C.dbd.O, b and c are independently a single bond; provided that b and c are not both double bonds; andR.sub.3 is hydrogen, dialkylphosphonate or halogen;and pharmaceutically acceptable salts thereof.Also disclosed is the use of the compounds of formula (I) as non-peptide antagonists of angiotensin II receptor, in the treatment of cardiovascular diseases, in particular hypertension and congestive heart failure.

Abstract: A compound of formula I, ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.1 ', R.sub.2 ', and R.sub.3 ' are independently the same or different and each represent hydrogen, hydroxy, or lower alkoxy, or any vicinal two of R.sub.1, R.sub.2, R.sub.3, R.sub.1 ', R.sub.2 ', and R.sub.3 ' combined together represent --O--(CH.sub.2).sub.n --O--, wherein n=1 or 2; R.sub.4 represents methylene or halomethyl; and X.sub.1, X.sub.2, X.sub.3, and X.sub.4 are independently the same or different and each represent hydrogen or halogen; or a pharmaceutically acceptable salt thereof. Also disclosed are a pharmaceutical composition that contains an effective amount of a compound of formula I together with a pharmaceutically acceptable excipient, and a method of treating cancer that involves the administration of an effective amount of the compound of formula I to a patient in need thereof.

Abstract: A series of novel polyamine-linked acridine dimers and derivatives thereof are described. The polyamine-linked acridine dimers and derivatives are potential anti-cancer agents.

Abstract: A process of preparing 2-cyano-3,5-dimethyl-4-methoxypyridine. The process includes the steps of: acylating 2-methyl-1-penten-1-alkoxy-3-one to obtain 2-alkoxycarbonyl-3,5-dimethyl-4-pyrone; ammonolyzing 2-alkoxycarbonyl-3,5-dimethyl-4-pyrone to obtain 2-carboxamido-3,5-dimethyl-4(1H)-pyridone; methylating 2-carboxamido-3,5-dimethyl-4(1H)-pyridone to obtain 2-carboxamido-3,5-dimethyl-4-methoxypyridine; and dehydrating said 2-carboxamido-3,5-dimethyl-4-methoxypyridone to obtain 2-cyano-3,5-dimethyl-4-methoxypyridine.

Abstract: A process of preparing 2-hydroxymethyl-3,5-dimethyl-4-methoxypyridine including the steps of acylating 2-methyl-1-penten-1-alkoxy-3-one to obtain 2-alkoxycarbonyl-3,5-dimethyl-4-pyrone; ammonolyzing 2-alkoxycarbonyl-3,5-dimethyl-4-pyrone to obtain 2-alkoxycarbonyl-3,5-dimethyl-4(1H)-pyridone; halogenating 2-alkoxycarbonyl-3,5-dimethyl-4(1H)-pyridone to obtain 2-alkoxycarbonyl-4-halo-3,5-dimethylpyridine; methoxylating 2-alkoxycarbonyl-4-halo-3,5-dimethylpyridine to obtain 2-methoxycarbonyl-3,5-dimethyl-4-methoxypyridine; and reducing 2-methoxycarbonyl-3,5-dimethyl-4-methoxypyridine to obtain 2-hydroxymethyl-3,5-dimethyl-4-methoxypyridine.