20010-99-5Relevant articles and documents
Targeted structural modification of spin crossover complexes: pyridine vs pyrazine
Feltham, Humphrey L. C.,Cowan, Matthew G.,Kitchen, Jonathan A.,Jameson, Guy N. L.,Brooker, Sally
, p. 296 - 304 (2018)
2-(Aminomethyl)pyrazine has been prepared in five steps from 2-pyrazine carboxylic acid. From this key amine, two new bis-terdentate triazole-based ligands which feature pendant pyrazine groups, PZMAT and PZMPT (4-amino- and 4-pyrrolyl-3,5-bis{[(2-pyrazylmethyl)amino]methyl}-4H-1,2,4-triazole, respectively), and two dinuclear complexes of them, [FeII 2(PZMAT)2](BF4)4?MeOH?2H2O (1?MeOH?2H2O) and [FeII 2(PZMPT)2](BF4)4?3H2O (2?3H2O), have been prepared. A structure determination at 100?K on 2?3.5MeCN confirmed that the ligands adopt the expected binding mode, providing all twelve donors to the two iron(II) centres and two N1,N2-triazole bridges between them. Both undergo gradual incomplete spin transitions: at room temperature 1?MeOH?2H2O and 2?3H2O are approximately two-thirds to three-quarters [HS-HS], dropping to mostly ‘[HS-LS]’ at 50?K. The structure determination and M?ssbauer spectroscopy of 2 qualitatively support this. These findings are consistent with the pendant pyrazines providing a somewhat higher field strength than the pendant pyridines do in the analogous PMRT complexes.
Compound with nitrogen-containing bridge ring, spiro or fused ring structure and application thereof
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Paragraph 0168-0170, (2020/08/12)
The invention discloses a compound with a nitrogen-containing bridge ring, spiro or fused ring structure and application of the compound. The compound has an obvious inhibition effect on the activityof protein kinase, can be used as a BTK inhibitor for preparing drugs for treating BTK-mediated diseases including, but not limited to, autoimmune diseases, malignant tumors and the like, and has a wide application prospect.
MANUFACTURING METHOD OF OPTICAL ACTIVE SECONDARY ALCOHOL
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Paragraph 0099, (2019/03/20)
PROBLEM TO BE SOLVED: To provide a method for manufacturing optical active secondary alcohol with high optical purity by hydrogenating a substrate carbonyl compound using a ruthenium complex with a specific optical active diphosphine compound and an amine compound of which synthesis is easy as ligands as a catalyst. SOLUTION: The manufacturing method of optical active secondary alcohol including reacting a substrate carbonyl compound (excluding 3-quinuclidinone, a 3-quinuclidinone derivative having a substituent, and ketone having an aromatic hydrocarbon group and a heterocycle) with hydrogen and/or a hydrogen-donating compound in a presence of a ruthenium complex selected from a compound represented by the following general formula (1) RuXYAB (1) [X and Y are same or different, represent a hydrogen atom or an anionic group, A represents optical active diphosphine represented by the general formula (2), and B represents an amine compound represented by the following general formula (3)]. SELECTED DRAWING: None COPYRIGHT: (C)2019,JPO&INPIT
BRUTON'S TYROSINE KINASE INHIBITORS
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Page/Page column 21, (2018/10/19)
Bruton's tyrosine kinase (Btk) inhibitors have the following Formula (I).
TETRAHYDRO-IMIDAZO[1,5-A]PYRAZINE DERIVATIVES SALTS, PREPARATION PROCESS AND PHARMACEUTICAL USE THEREOF
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Page/Page column 15; 18, (2016/10/08)
The present invention relates to (R)-7-[3-Amino-4-(2,4,5-trifluoro-phenyl)-butyryl]-3-trifluoromethyl-5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine-1-carboxylic acid pharmaceutical salts, methods for their preparation, pharmaceutical compositions containing the same and their use as a therapeutic agent, especially as a dipeptidyl peptidase IV inhibitor.
PROCESS FOR PRODUCING OPTICALLY ACTIVE SECONDARY ALCOHOL
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Paragraph 0150; 0151; 0152, (2015/02/19)
[Object] The object of this invention is to provide a method for producing an optically active secondary alcohol at a high optical purity by hydrogenating a substrate carbonyl compound at a high efficiency using as a catalyst a ruthenium complex bearing as a ligand certain optically active diphosphine compound and a readily synthesized amine compound. [Solution] The method of producing an optically active secondary alcohol according to the present invention is characterized in that a substrate carbonyl compound (provided that 3-quinuclidinone, 3-quinuclidinone derivative having a substituent, and a ketone having an aromatic hydrocarbon group and a heterocycle are excluded) is reacted with hydrogen and/or a hydrogen donating compound in the presence of a ruthenium complex selected from the compounds expressed by following general formula (1) RuXYAB (1) [in the general formula (1), X and Y are the same or different from each other and denote a hydrogen atom or an anionic group, A denotes an optically active diphosphine expressed by the general formula (2), B denotes an amine compound expressed by following general formula (3)].
BIARYL ETHER SULFONAMIDES AND THEIR USE AS THERAPEUTIC AGENTS
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, (2013/05/22)
This invention is directed to biaryl ether sulfonamides, or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.
SALTS OF TETRAHYDROIMIDAZO Y1,5-A¨PYRAZINE DERIVATIVES, PREPARATION METHODS AND PHARMACEUTICAL USE THEREOF
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Page/Page column 9, (2012/02/04)
Pharmaceutical salts of (R)-7-[3-amino-4-(2,4,5-trifluorophenyl)-butyryl]-3-trifluoromethyl-5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine-1-formic acid, their preparation methods, compositions containing the said pharmaceutical salts and their use as medicaments, especially as dipeptidyl peptidase IV (DPP-IV) inhibitors are disclosed.
TETRAHYDRO-IMIDAZO[1,5-a]PYRAZINE DERIVATIVES SALTS, PREPARATION METHODS AND MEDICINAL USE THEREOF
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Page/Page column 9, (2012/03/27)
Pharmaceutically acceptable salts of (R)-7-[3-amino-4-(2,4,5-trifluorophenyl)-butyryl]-3-trifluoromethyl-5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine-1-formic acid, their preparation methods, compositions containing the said pharmaceutical salts and their use as medicaments, especially as dipeptidyl peptidase IV (DPP-IV) inhibitors are disclosed.
TETRAHYDRO-IMIDAZOY1,5-A¨PYRAZINE DERIVATIVES, PREPARATION METHODS AND MEDICAL USES THEREOF
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Page/Page column 18, (2010/10/03)
Tetrahydro-imidazo[1,5-a]pyrazine derivatives of formula ( I ), their preparation methods, pharmaceutical compositions containing the derivatives and uses thereof as medicaments, especially as dipeptidyl peptidase IV inhibitor, wherein the substituents of formula ( I ) are defined as same as the description.