Abstract:
The invention provides a screening assay for selecting inhibitors of NFAT:Transcription factor interactions. The invention also provides compositions and methods for inhibiting immune response in a subject.
Abstract:
The invention relates to novel compounds and methods of treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.
Abstract:
The present invention relates to a diketohydrazine derivative of formula (I) and a pharmaceutically acceptable salt thereof (the symbols in the formula have the same meaning as described in the specification). The compound of formula (I) has an inhibitory activity against cysteine protease, and it is useful for the treatment of inflammatory diseases, immune diseases, ischemic diseases, respiratory diseases, circulatory diseases, blood diseases, neuronal diseases, hepatic or biliary diseases, osseous or articular diseases, metabolic diseases, etc. And the compound has inhibitory activity against elastase and it is also useful for the treatment of COPD (chronic obstacle pulmonary diseases).
Abstract:
This invention relates to a novel organophotoreceptor that includes: (a) a charge transport material comprising a fluorenone hydrazone having a) least two fluorenone alkylsulfonylphenylhydrazone groups, b) at least two fluorenone pyrrolylhydrazone groups, c) at least two fluorenone benzotriazolylhydrazone groups, d) at least two fluorenone sulfolanylhydrazone groups, e) at least two fluorenone pyrazolylhydrazone groups, f) at least two fluorenone naphthylhydrazone groups, g) at least two fluorenone tetrazolylhydrazone groups, h) at least two fluorenone stilbenylhydrazone groups, or i) at least two fluorenone(9H-fluoren-9-ylidene)benzylhydrazone groups. Some of these fluoreneones may be represented by the formula where n is an integer between 2 and 6, inclusive; R1 is hydrogen, alkyl, or aryl; R2 is alkylsulfonylphenyl or one of its derivatives; X is a linking group having the formula —(CH2)m—, branched or linear. The compounds may form electrostatic imaging systems in combination with (b) a charge generating compound; and (c) an electrically conductive substrate.
Abstract translation:本发明涉及一种新型有机光感受器,其包括:(a)电荷传输材料,其包含芴酮腙,其具有a)至少两个芴酮烷基磺酰基苯腙基团,b)至少两个芴酮吡咯基腙基团,c)至少两个芴酮苯并三唑基腙基团,d) 至少两个芴酮砜基腙基团,e)至少两个芴酮吡唑基腙基团,f)至少两个芴酮萘基腙基团,g)至少两个芴酮四唑腙基团,h)至少两个芴酮茋基腙基团,或i)至少两个芴酮 (9H-芴-9-亚基)苄腙基团。 这些芴酮中的一些可以由下式表示:其中n是2和6之间的整数,包括端值在内; R 1是氢,烷基或芳基; R 2是烷基磺酰基苯基或其衍生物之一; X是具有下式的连接基团 - (CH 2 CH 2)m - 支链或直链。 所述化合物可以与(b)产生电荷的化合物组合形成静电成像系统; 和(c)导电基板。
Abstract:
Improved organophotoreceptor comprises an electrically conductive substrate and a photoconductive element on the electrically conductive substrate, the photoconductive element comprising: (a) a charge transport material having the formula where n is an integer between 2 and 6, inclusive; R1 and R2 are, independently, an alkyl group, an alkaryl group, or an aryl group with the proviso that neither R1 nor R2 is a naphthyl group, a stilbenyl group, alkylsulfonylphenyl group or a (9H-fluoren-9-ylidene)benzyl group; R3 and R4 are, independently, H, halogen, carboxyl, hydroxyl, thiol, cyano, nitro, aldehyde group, ketone group, an ether group, an ester group, a carbonyl group, an alkyl group, an alkaryl group, or an aryl group; X is a linking group having the formula —(CH2)m—, branched or linear, where m is an integer between 0 and 20, inclusive, and one or more of the methylene groups can be optionally replaced by O, S, C═O, O=S=O, a heterocyclic group, an aromatic group, urethane, urea, an ester group, a NR5 group, a CHR6 group, or a CR7R8 group where R5, R6, R7, and R8 are, independently, H, an alkyl group, an alkaryl group, a heterocyclic group, or an aryl group; and Y comprises a bond, C, N, O, S, a branched or linear —(CH2)p— group where p is an integer between 0 and 10, an aromatic group, a cycloalkyl group, a heterocyclic group, or a NR9 group where R9 is hydrogen atom, an alkyl group, or aryl group, wherein Y has a structure selected to form n bonds with the corresponding X groups; and (b) a charge generating compound. Corresponding electrophotographic apparatuses and imaging methods are described.
Abstract:
The compounds of the invention which encompasses a class of compounds having the property of anti-carcinogenic activity against human myeloma r comprising 4-oxo-2-butenoic acid compounds and 3-hydrazino-2,4-dioxobutanoic acid compounds and more specifically those novel derivatives: 4-(4-Chloro-phenyl)-2-(N′-fluoren-9-ylidene-hydrazino)-4-oxo-but-2-enoic acid methyl ester (OF-07); 2-{N′-[(2-Bromo-phenyl)-phenyl-methylene]-hydrazino}-4-oxo-4-phenyl-but-2-enoic acid methyl ester (OF-09); 2-{N′-[(4-Dimethylamino-phenyl)-phenyl-methylene]-hydrazino}-4-oxo-4-phenyl-but-2-enoic acid methyl ester (OF-10) and 2-{N′-[1-(4-Chloro-phenyl)-ethylidene]-hydrazino}-4-oxo-4-phenyl-but-2-enoic acid methyl ester (OF-20) and the use of 2-(N′-Fluoren-9-ylidene-hydrazino)-5,5-dimethyl-4-oxo-hex-2-enoic acid methyl ester (OF-06); 4-(4-Ethoxy-phenyl)-2-(N′-fluoren-9-ylidene-hydrazino)-2-hydroxy-4-oxo-butyric acid methyl ester (OF-13); 4-benzoyl-3 -benzoyloxy-2-(2-oxo-2H-1,4-benzoxazin-3-yl)pyrido[2,1-c][1,4]benzoxazin-1,5-dione (1F-18), 4-Chloro-4-(4-ethoxy-phenyl)-2-(fluoren-9-ylidene-hydrazono)-but-3-enoic acid methyl ester (3F-19); and 2-(N′-Fluoren-9-ylidene-hydrazino)-4-oxo-4-phenyl-but-2-enoic acid methyl ester (1F-04) which are unique in humans as therapeutic means for the eradication human myeloma.
Abstract:
Compounds of the class of 4-oxo-butenoic acid derivatives are disclosed along with the surprising use property of these compounds as a anti-tumor agents in humans against breast carcinoma, which include: 2-(N′-Fluoren-9-ylidene-hydrazino)-5,5-dimethyl-4-oxo-hex-2-enoic acid methyl ester (OF-06), 1-(2,4-Dimethyl-phenyl)-2,4-dihydroxy-3-(4-methyl-benzoyl)-5-oxo-2,5-dihydro-1H-pyrrole-2-carboxylic acid methyl ester (1F-07), 4-(4-Methoxy-phenyl)-2,4-dioxo-3-(phenyl-hydrazono)-butyric acid (3F-10), 4-(4-Chloro-phenyl)-2,4-dioxo-3-(phenyl-hydrazono)-butyric acid ethyl ester (3F-11), 2-Hydroxy-4-oxo-4-(2,3,5,6-tetrafluoro-4-methoxy-phenyl)-but-2-enoic acid (3F-15), and 4,4-Dihydroxy-5-(4-methyl-benzoyl)-2-phenyl-2,4-dihydro-pyrazol-3-one (3F-16) as well as some novel derivatives of these compounds claimed (see Table 2). The invention also encompasses a class of the compounds with the novel property of anti-tumor activity against human breast cancer, which includes the following compounds 4-(4-Ethoxy-phenyl)-2-(N′-fluoren-9-ylidene-hydrazino)-2-hydroxy-4-oxo-butyric acid methyl ester (OF-13); 2-{N′-[1-(4-Chloro-phenyl)-ethylidene]-hydrazino}-4-oxo-4-phenyl-but-2-enoic acid methyl ester (OF-20); 2-(N′-Fluoren-9-ylidene-hydrazino)-4-oxo-4-phenyl-but-2-enoic acid methyl ester (1F-04); and 4-Chloro-4-(4-ethoxy-phenyl)-2-(fluoren-9-ylidene-hydrazono)-but-3-enoic acid methyl ester (3F-19).
Abstract:
New compounds of formula I are described: 1 The compounds have potentially valuable pharmaceutical properties in the treatment of some central and peripheral nervous system disorders.
Abstract:
A method is provided for the transition metal-catalyzed arylation, or vinylation, of hydrazines, hydrazones, and the like. Additionally, the invention provides a conceptually novel strategy, the cornerstone of which is the transition metal-catalyzed arylation or vinylation method, for the synthesis of indoles, carbazoles, and the like. The methods and strategies of the invention may be utilized in standard, parallel, and combinatorial synthetic protocols.
Abstract:
Intermediates in the synthesis of steroids having the formulas WHEREIN R and R'' are alkyl of one to three carbon atoms and may be different and R'''' is selected from the group consisting of a hydrazide, a semicarbazide, a semioxamazide, a lower alkanediol, a lower alkanedithiol and a lower alkoxycarbonyl hydrazine.