- PYRAZOLYL-AMINO-SUBSTITUTED PYRAZINES AND THEIR USE FOR THE TREATMENT OF CANCER
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The present invention relates to compounds of Formula (I): and to their pharmaceutical compositions, and to their methods of use. These novel compounds provide a treatment for myeloproliferative disorders and cancer.
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Page/Page column 69
(2008/12/04)
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- Phenyl thiazolyl urea and carbamate derivatives as new inhibitors of bacterial cell-wall biosynthesis
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Over 50 phenyl thiazolyl urea and carbamate derivatives were synthesized for evaluation as new inhibitors of bacterial cell-wall biosynthesis. Many of them demonstrated good activity against MurA and MurB and gram-positive bacteria including MRSA, VRE and
- Francisco, Gerardo D.,Li, Zhong,Albright, J. Donald,Eudy, Nancy H.,Katz, Alan H.,Petersen, Peter J.,Labthavikul, Pornpen,Singh, Guy,Yang, Youjun,Rasmussen, Beth A.,Lin, Yang-I.,Mansour, Tarek S.
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p. 235 - 238
(2007/10/03)
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- Activated propenes as color couplers method for the production thereof
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The invention provides novel photographic compositions comprising a propene isomer of the formula wherein A B or E, each individually represent hydrogen, or an electron withdrawing group, selected for example from —CN, —NO2, —SO2R, —SO2NH—, —CO2R, —COR, —CONHR, —CONHAr, —CF3halogen, amino, aryl, aralkyl, alkyl, cycloalkyl, alkyl (carbonyl)oxy, aryl (carbonyl)oxy, carboxy, alkoxycarbonyl, aryloxycarbonyl, carbamomyl, acyl, alkylaminocarbonyl, arylaminocarbonyl, alkoxycarbonylamino, acylamino, ureido, alkylsulphonylamino, arylsulphonylamino, sulphamoylamino, alkylsulphonyl, arylsulphonyl, sulphamoyl, imido, alkylthio, arylthio and heterocycles; the invention also provides a propene isomer of the formula I wherein D represents a group of the formula Ar—L— wherein Ar is a phenyl group optionally substituted with one or more substituents, and —L— is a linking group incorporating a lone pair of electrons; and A, B, E and X are defined as R is above defined. The activated propenes of the above formulae are novel colour couplers which react with oxidised developer under alkaline conditions to give magenta dyes.
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- Practical preparation of (Z)-2-(5-amino-1,2,4-thiadiazol-3-yl)-2-methoxyiminoacetic acid: A side-chain of the fourth generation of cephem antibiotics
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A Z-isomer (4) of 2-(5-amino-1,2,4-thiadiazol-3-yl)-2-(methoxyimino)acetic acid, which is the common acyl moiety of clinically useful cephem antibiotics, has been prepared from the aminoisoxazoles through the skeletal rearrangement in several routes. Reaction of 3-amino-5-methoxyisoxazole (7) with alkoxycarbonyl isothiocyanates gave methyl 2-(5-alkoxycarbonylamino-1,2,4-thiadiazol-3-yl)acetates (8), which were converted into the target compound 4 through the reaction of the corresponding keto ester with O-methylhydroxylamime. Compound 4 was prepared similarly from 3-aminoisoxazole (10). Also, O-methylation of 2-hydroxyimino-2-(5-methoxycarbonylamino-1,2,4-thiazol-3-yl)acetate (15) with methyl iodide or dimethyl sulfate in the presence of barium oxide and barium hydroxide octahydrate was found to afford exclusively the desired Z-isomer (14a) of methyl 2-(5-methoxycarbonylamino-1,2,4-thiadiazol-3-yl)-2-(methoxyimino)aceta te, which was led to 4.
- Tatsuta,Miura,Gunji,Tamai,Yoshida,Inagaki,Kurita
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p. 1701 - 1707
(2007/10/02)
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- Synthesis and evaluation of antiinflammatory activities of a series of corticosteroid 17α-esters containing a functional group
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A series of 21-desoxy-21-chlorocorticosteroids that contain a functionalized ester group at 17α has been prepared and examined to separate their systemic activity from topical antiinflammatory activity. Introduction of the functionalized ester group at 17α was carried out by an acid-catalyzed formation of cyclic ortho esters with 17α,21-hydroxyl groups of corticosteroids and subsequent acid-catalyzed hydrolysis. As for the functional group, chloro, methoxy, acetoxy, cyano, cyclopropyl, or alkoxycarbonyl group was introduced at the terminal carbon atom of the 17α-alkanoate group. The topical antiinflammatory activity and systemic activity of these compounds were examined and found to be signficantly dependent on the functionalities in the 17α-esters. Among these derivatives, a series of 17α-(alkoxycarbonyl)alkanoates (17α-OCO(CH2)(n)COOR) showed an excellent separation of the systemic activity from topical activity. The effects of the number of methylene groups (n) and of the alkyl groups of the ester (R) on either topical or systemic activity of the corticosteroid derivatives were also investigated.
- Ueno,Maruyama,Miyake,Nakao,Nakao,Umezu,Nitta
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p. 2468 - 2473
(2007/10/02)
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- Thiono and Dithio Esters, 42. - Synthesis and Properties of Cyanoacetic Thionoesters
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Malononitrile (1) can be transformed into the cyanoacetic thionoesters 3 via the imidoester hydrochlorides 2 by thiolysis.The ethyl ester 3a condenses with benzylamine by H2S elimination to form the imidoester 7 and with piperidine by elimination of ethan
- Mueller, Hans-Georg,Hartke, Klaus
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p. 879 - 884
(2007/10/02)
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