- Photochemical Ring Contraction of Dihydro-1,4-benzothiazines
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The pheomelanin precursors 1a and the related dihydro-1,4-benzothiazines 1b-f undergo ring contraction upon irradiation with pyrex-filtered UV light to give 2-methylbenzothiazoles 2a-f in good yields.
- Costantini, Claudio,Testa, Gennaro,Crescenzi, Orlando,d'Ischia, Marco
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- HYDROXYQUINOXALINECARBOXAMIDE DERIVATIVE
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The present invention provides a novel hydroxyquinoxaline carboxamide derivative that is useful for preventing and/or treating blood coagulation disorders. A compound represented by formula (i), or a pharmacologically acceptable salt thereof: wherein, each of R1 and R2 independently represents a group such as a hydrogen atom or a halogen atom; R3 represents a group such as a hydrogen atom; each of R4 and R5 independently represents a group such as a hydrogen atom, a halogen atom or a C1-4 alkyl group; each of R6 and R7 independently represents a hydrogen atom or a C1-4 alkyl group; X represents a group such as a C3-10 cycloalkyl group, C6-10 aryl group or a 5- to 10-membered heterocyclic group, which may be substituted with substituent(s) selected from substituent group α; Y represents a group such as -CO-, -O- or -NRa-, and Ra represents a group such as a hydrogen atom or a C1-4 alkyl group.
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Page/Page column 117
(2010/12/29)
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- Processes and intermediates for the preparation of N4-phenyl-quinazoline-4-amine derivatives
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This invention provides compounds of Formula (I), wherein B, G, A, E, R1, R2, R3, m and n are as defined herein, which are useful as type I receptor tyrosine kinase inhibitors, and methods of use thereof in the treatment of hyperproliferative disorders in mammals.
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Page/Page column 51-52
(2009/09/05)
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- Searching for new cures for tuberculosis: Design, synthesis, and biological evaluation of 2-methylbenzothiazoles
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The actual development and clinical use of new therapeutics for tuberculosis (TB) have remained stagnant for years because of the complexity of the disease process, the treatment of which at present requires the administration of drug combinations over a 6month period. There is thus an urgent need for the discovery and development of novel, more active, and less toxic anti-TB agents. In this study, we report on the chemistry and biology of a series of potent 5-(2-methylbenzothiazol-5-yloxymethyl) isoxazole-3-carboxamide derivatives, which proved to be active against replicating Mycobacterium tuberculosis (Mtb) H37Rv. The most potent compounds 7j and 7s were found to inhibit Mtb growth at micromolar concentrations, with MICvalues of 1.4 and 1.9 μM, respectively. Impressively, all active compounds were nontoxic toward Vero cells (IC50 > 128 μM). Moreover, the best of these compounds were also tested against protozoan parasites, and some of these compounds were found to show activity, especially against Plasmodium falciparum. These studies thus suggest that certain 2-methylbenzothiazole based compounds may serve as promising lead scaffolds for further elaboration as anti-TB drugs and as possible antimalaria drugs. 2009 American Chemical Society.
- Huang, Qingqing,Mao, Jialin,Wan, Baojie,Wang, Yuehong,Brun, Reto,Franzblau, Scott G.,Kozikowski, Alan P.
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supporting information; experimental part
p. 6757 - 6767
(2010/04/24)
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- High-yielding cleavage of (aryloxy)acetates
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A reliable and high-yielding one-pot sequence for the removal of O-carboxymethyl moieties from phenols is presented. When diethylphosphoryl azide is employed as the azide transfer reagent in the Curtius rearrangement and glycerol in the subsequent hydrolytic workup, the protocol can be reliably applied to a very broad scope of substrates. Wiley-VCH Verlag GmbH & Co. KGaA, 2008.
- Spurg, Anke,Waldvogel, Siegfried R.
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p. 337 - 342
(2008/09/18)
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- CYANOISOQUINOLINE COMPOUNDS AND METHODS OF USE THEREOF
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The present invention relates to cyanoisoquinoline compounds suitable for use in treating hypoxia inducible factor-mediated and/or erythropoietin-associated conditions. The cyanoisoquinoline compounds of the invention have the following structure: Formula (I).
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Page/Page column 83
(2008/06/13)
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- Heteroaryl alkyl piperazine derivatives
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Novel compounds of the general formula: and pharmaceutically acceptable acid addition salts thereof, wherein the compounds are useful in therapy to protect skeletal muscles against damage resulting from trauma or to protect skeletal muscles subsequent to muscle or systemic diseases such as intermittent claudication, to treat shock conditions, to preserve donor tissue and organs used in transplants, in the treatment of diabetes, in the treatment of cardiovascular diseases including atrial and ventricular arrhythmias, Prinzmetal's (variant) angina, stable angina, and exercise induced angina, congestive heart disease, and myocardial infarction.
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- Compound
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There is provided a compound of Formula I 1 wherein each T is independently selected from H, hydrocarbyl, —F—R, and a bond with one of D, E, P or Q, or together with one of P and Q forms a ring; Z is a suitable atom the valency of which is m; D, E and F are each independently of each other an optional linker group, wherein when Z is nitrogen E is other than CH2 and C═O; P, Q and R are independently of each other a ring system; and at least Q comprises a sulphamate group.
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Page/Page column 66
(2008/06/13)
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- N-ALKYNYL-2-HETEROARYLOXYALKYLAMIDES FOR USE AS FUNGICIDES
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Compounds of the general formula (I) are useful as fungicides wherein Het is a 5- or 6- linked group of the formula (a) or (b), and the variables are as defined in the claims.
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- Heteroaryl alkyl piperazine derivatives
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Novel compounds of the general formula: and pharmaceutically acceptable acid addition salts thereof, wherein the compounds are useful in therapy to protect skeletal muscles against damage resulting from trauma or to protect skeletal muscles subsequent to muscle or systemic diseases such as intermittent claudication, to treat shock conditions, to preserve donor tissue and organs used in transplants, in the treatment of cardiovascular diseases including atrial and ventricular arrhythmias, Prinzmetal's (variant) angina, stable angina, and exercise induced angina, congestive heart disease, and myocardial infarction.
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- Heteroaryl alkyl piperazine derivatives
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Novel compounds of the general formula: and pharmaceutically acceptable acid addition salts thereof, wherein the compounds are useful in therapy to protect skeletal muscles against damage resulting from trauma or to protect skeletal muscles subsequent to muscle or systemic diseases such as intermittent claudication, to treat shock conditions, to preserve donor tissue and organs used in transplants, in the treatment of diabetes, in the treatment of cardiovascular diseases including atrial and ventricular arrhythmias, Prinzmetal's (variant) angina, stable angina, and exercise induced angina, congestive heart disease, and myocardial infarction.
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- Synthesis and Photochromic Characteristics of 1,3-Dihydrospiropyrimidobenzoxazines> and 1,3-Dihydrospirothiazolobenzoxazines>
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Two new series of 1,3-dihydrospiro derivatives were synthesized, the 1,3-dihydrospiropyrimidobenzoxazines> 4-10 and the 1,3-dihydrospirothiazolobenzoxazines> 11-17.These series extend the available range of photochromic properties (rate constant of thermal bleaching, UV/VIS spectrum of the opened coloured form, and photocoloration yield), an interesting feature of variable-transmission materials.The synthesis of these compounds (Scheme 1) required the preliminary synthesis of intermediate β-hydroxy-α-nitrosoheterocycles 18 and 19 (Scheme 2).Important amounts of a coloured, non-photochromic, stable secondary product (see 20) were formed in the condensation in the spiro series.The photochromic characteristics of the new derivatives were determined using a flash-photolysis apparatus coupled to a fast-scanning spectrometer.The role of the heteroatoms in the oxazine moiety and the role of substituents in the indole moiety were investigated quantitatively through the study of the photochromic properties and the solvent effects.The presence of an S-atom gives rise to interesting properties which open up new prospects for synthesis and applications.
- Tardieu, Pascale,Dubest, Roger,Aubard, Jean,Kellmann, Arlette,Tfibel, Francis,et al.
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p. 1185 - 1197
(2007/10/02)
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