- An efficient synthesis of 5-chloro-2, 3, 4-trifluorobenzoic acid
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5-Chloro-2, 3, 4-trifluorobenzoic acid, a key intermediate for preparing quinolone-3-carboxylic acid derivatives, was synthesised from the commercially available 2, 3, 4, 5-trifluorobenzoic acid in excellent yield by a reaction sequence involving nitration, selective reduction, diazotisation and chlorination.
- Yu, Shuitao,Zhou, Weiyou,Xia, Zhengjun,Lin, Song,Chen, Zaixin
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- FORMS OF BINIMETINIB AND PROCESS FOR PREPARATION THEREOF
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Amorphous forms of Binimetinib and processes for the preparation thereof.
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Page/Page column 22; 26
(2021/06/22)
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- Substituted benzimidazole compound and composition with compound
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The invention provides a substituted benzimidazole compound and a composition with the compound. The substituted benzimidazole compound is a compound of formula (I) as shown in the specification, or apharmaceutically acceptable salt, prodrug, aquo-complex or solvent compound, polycrystalline type compound, stereisomer or isotope variant of the compound. The compound provided by the invention canbe adopted to treat and/or prevent related diseases caused by MEK (Methyl Ethyl Ketone), such as excessive proliferative diseases, pancreatitis, kidney illness, blastocyte cell transplantation and angiogenesis or angiopoiesis related diseases.
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Paragraph 0100-0105
(2019/03/31)
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- COMBINATION THERAPY
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The present invention relates to a pharmaceutical combination comprising a MEK inhibitor compound 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxyethyoxy)- amide or a pharmaceutically acceptable salt thereof and the IGFIR inhibitor ANTIBODY A, a pharmaceutical composition comprising such combination, methods for treating cancer comprising administration of a therapeutically effective amount of such combination to a subject in need thereof, and uses of such combination for the treatment of cancer.
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Page/Page column 21
(2013/10/08)
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- INHIBITORS OF MEK
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This invention concerns to N-(2-aylamino) aryl sulfonamides, which are inhibitors of MEK, methods of using such compounds in the treatment of hyperproliferative diseases, and to pharmaceutical compositions containing such compounds.
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Page/Page column 42
(2008/12/07)
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- NOVEL HYDROGEN SULFATE SALT
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The present invention relates to Compound 1 hydrogen sulfate salt and solvates, crystalline forms and amorphous forms thereof, and to processes for their preparation. Compound I
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Page/Page column 18
(2008/06/13)
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- SNAr PROCESS FOR PREPARING BENZIMIDAZOLE COMPOUNDS
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Provided are methods for the synthesis of heterocyclic compounds such as benzimidazole carboxylic acid core structures having Formula Ia-2 and their synthetic intermediates: wherein X1, X2, X5, R1, R2 and R4 are as defined herein. Compounds of Formula Ia-2 and their synthetic intermediates can be used to prepare heterocyclic derivatives such as benzimidazole derivatives.
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Page/Page column 49-50
(2010/11/25)
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- PROCESS FOR PREPARING BENZIMIDAZOLE COMPOUNDS
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Provided are methods for the synthesis of heterocyclic compounds such as benzimidazole carboxylic acid core structures having Formula Ia-1 and their synthetic intermediates: wherein Z, X1, X2, X5, R2 and R10 are as defined herein. Compounds of Formula Ia-1 and their synthetic intermediates can be used to prepare heterocyclic derivatives such as benzimidazole derivatives.
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Page/Page column 2; 63
(2010/11/25)
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- N-METHYL-SUBSTITUTED BENZAMIDZOLES
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The present invention relates to N-methyl-substituted benzamidazole derivatives of formula (I), as defined in the specification; pharmaceutical compositions and mehtod of use thereof.
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Page/Page column 51-52
(2008/06/13)
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- N3 alkylated benzimidazole derivatives as MEK inhibitors
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Disclosed are compounds of the formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein W, R1, R2, R7, R8, R9 and R10 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.
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- A novel antibacterial 8-chloroquinolone with a distorted orientation of the N1-(5-amino-2,4-difluorophenyl) group
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Fluoroquinolones represent a major class of antibacterial agents with great therapeutic potential. In this study, we designed m-aminophenyl groups as novel N-1 substituents of naphthyridones and quinolones. Among newly synthesized compounds, 7-(3-aminoazetidin-1-yl)-1-(5-amino-2,4-difluorophenyl)-8-chloro-6- fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (4) has extremely potent antibacterial activities against Gram (+) as well as Gram (-) bacteria. This compound is significantly more potent than trovafloxacin against clinical isolates: 30 times against Streptococcus pneumoniae and 128 times against methicillin resistant Staphylococcus aureus. The structure-activity relationship (SAR) study revealed that a limited combination of 1-(5-amino-2,4-difluorophenyl) group, 7-(azetidin-1-yl) group, and 8-Cl atom (or Br atom or Me group) gave potent antibacterial activity. An X-ray crystallographic study of a 7-(3-ethylaminoazetidin-1-yl)-8-chloro derivative demonstrated that the N-1 aromatic group was remarkably distorted out of the core quinolone plane by steric repulsion between the C-8 Cl atom and the N-1 substituent. Furthermore, a molecular modeling study of 4 and its analogues demonstrated that a highly distorted orientation was induced by a steric hindrance of the C-8 substituent, such as Cl, Br, or a methyl group. Thus, their highly strained conformation should be a key factor for the potent antibacterial activity.
- Kuramoto, Yasuhiro,Ohshita, Yoshihiro,Yoshida, Jiro,Yazaki, Akira,Shiro, Motoo,Koike, Tohru
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p. 1905 - 1917
(2007/10/03)
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- 4-Arylamino, 4-aryloxy, and 4-arylthio diarylamines and derivatives thereof as selective MEK inhibitors
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The invention provides compounds of formula (II), wherein Ar, R3, R4, R5, R6, R7, R8and W have the meanings given in the description. They are selective MEK inhibitors.
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- METHOD FOR TREATING CHRONIC PAIN USING MEK INHIBITORS
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The invention features a method for treating chronic pain using a compound selected from formulae (I), (II)A, (I)B and (I)C.
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- N3 alkylated benzimidazole derivatives as MEK inhibitors
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Disclosed are compounds of the formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein W, t, R1, R2, R7, R9, R10, R11 and R12 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.
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- Benzoheterocycles and their uses as MEK inhibitors
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The invention provides compounds having formula (I), wherein W is OH, or derivatives of the carboxylic acid, and Q is a heterocyclo-condensed ortho-phenylene residue. These compounds are useful as MEK inhibitors, particularly in the treatment of proliferative diseases such as cancer.
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- Trifluoro-substituted benzoic acid, esters thereof, and process for producing the same
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The present invention is to provide a trifluoro-substituted benzoic acid, an ester thereof, particularly 2,3,4-trifluoro-5-iodobenzoic acid, 2,3,4-trifluoro-5-trifluoromethylbenzoic acid, esters thereof, which are useful as a starting material for synthesizing a quinolonecarboxylic acid compound useful as a medicine, an anti-bacterial agent or an antiviral agent, and processes for preparing these compounds and 2,4,5-trifluoro-3-iodobenzoic acid, 2,4,5-trifluoro-3-trifluoromethylbenzoic acid and esters thereof.
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- Pyridonecarboxylic acid derivatives or salts thereof and drugs containing the same as the active ingredient
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PCT No. PCT/JP97/04326 Sec. 371 Date May 28, 1999 Sec. 102(e) Date May 28, 1999 PCT Filed Nov. 27, 1997 PCT Pub. No. WO98/23592 PCT Pub. Date Jun. 4, 1998The invention relates to pyridonecarboxylic acid derivatives represented by the general formula (1): wherein R1 is -OH, a carboxy-protecting group or (alkyl)amino group, R2 is H, or -NO2, (protected) amino, (protected) hydroxyl, lower alkyl or lower alkoxyl group, R3 is a halogen atom, H, or -NO2, lower alkyl, lower alkoxyl or amino group, R4 is an azido, (substituted) hydrazino, (substituted) amino, lower alkoxyl or hydroxyl group, R5, R6 and R7 are independently H, -NO2, halogen atom or lower alkyl group, R8 is a -NO2, (substituted) amino, -OH or lower alkoxyl group, A is N or C-R12, in which R12 is H, halogen atom, or (substituted) lower alkyl, lower alkenyl, lower alkynyl, lower alkoxyl, lower alkylthio or nitro group, and B is N or C-R13, in which R13 is H or halogen atom, or salts thereof, and medicine comprising such a compound as an active ingredient. The derivatives or the salts thereof exhibit excellent antibacterial action and peroral absorbability, scarcely cause side effects, and are easy of synthesis.
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- Phenylenediamines and process for preparing the same
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Phenylenediamines represented by general formula (1): STR1 wherein R represents an alkyl group or an optionally substituted aralkyl group, X1 represents a hydrogen atom or a halogen atom, and X2 represents a halogen atom; salts thereof, and a process for preparing the same. The compounds are useful as intermediates for synthesis of pyridonecarboxylic acid derivatives useful as antibacterial agents.
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