- AMINOPYRAZINE DERIVATIVE AND MEDICINE
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The present invention relates to a compound represented by general formula [1] satisfying the following (I) or (II), or a pharmaceutical acceptable salt of the compound. (I) X is CH or N; R1 is a halogen atom,; and R2 is H, a halogen atom, CN, [2], [3], [8], [9], an —O-alkyl, an —O-(saturated ring), etc. [2]: —C(RC)(RD)(RE) (RC to RE each are H, an alkyl, etc.) [3]: —N(RF)(RG) (RF and RG each are H, OH, amino, a (hetero)aryl, etc.) [8]: —C(═O)RL (RL is an alkyl, OH, an alkoxy, amino, etc.) [9]: a (substituted)phenyl; (II) X is >C—C(—O)R3 (R3 is a (substituted)amino, an alkoxy, OH, etc.); R1 is a halogen atom; R2 is H; R3 is H or OH; and R3 and R4 each are H or an alkyl.
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Page/Page column 40
(2011/12/12)
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- METHOD FOR THE PRODUCTION OF BORONIC ACIDS CARRYING CYANOALKYL, CARBOXYL AND AMINOCARBONYL GROUPS AND THEIR DERIVATIVES
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A process for the manufacture of aminocarbonyl boronic acids of formula (IV) by converting the compounds of formula (III) with a Br?nsted base Y(OH)n in a solvent or a solvent mixture, in which Z represents an optionally substituted arylene, heteroarylene, alkene, heteroalkene, alkylidene, heteroalkylidene, alkenylidene, heteroalkenylidene, alkynylidene, arylalkylene, heteroarylalkylene, arylheteroalkylene, heteroarylheteroalkylene, alkylheteroarylene, heteroalkylheteroarylene, or alkylarylene group; Y represents a metal or ammonium cation of valence n with 0n5; and B represents boronic acid, boronic acid ester, or a borate, or a boronic acid anhydride. The aminocarbonyl boronic acids of formula (IV) can be further hydrolyzed to form the carboxy boronic acid of formula (V).
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Page/Page column 5
(2009/12/05)
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- Substituted phenyl derivatives, their preparation and use
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The present invention discloses compounds having the formula wherein the substituents are defined in the application. The compounds are useful as chloride channel blockers.
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- DIARYLUREA DERIVATIVES AND THEIR USE AS CHLORIDE CHANNEL BLOCKERS
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The present invention relates to novel diarylurea derivatives useful as chloride channel blockers. In other aspects the invention relates to the use of these compounds in a method for therapy, such as for the treatment of bone metabolic diseases, diseases responsive to modulation of the mast cell or basophil activity, diseases responsive to inhibition of angiogenesis, or sickle cell anaemia, and to pharmaceutical compositions comprising the compounds of the invention.
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- Substituted phenyl derivatives, their preparation and use
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The present invention discloses compounds having the formula wherein the substituents are defined in the application. The compounds are useful as chloride channel blockers.
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- Substituted phenyl derivatives, their preparation and use
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A compound having the formula (I) or a pharmaceutically acceptable salt thereof where the variables are defined in the specification are useful in the treatment of sickle-cell anemia.
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