- Targeted structural modification of spin crossover complexes: pyridine vs pyrazine
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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.
- Feltham, Humphrey L. C.,Cowan, Matthew G.,Kitchen, Jonathan A.,Jameson, Guy N. L.,Brooker, Sally
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Read Online
- Compound with nitrogen-containing bridge ring, spiro or fused ring structure and application thereof
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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.
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Paragraph 0168-0170
(2020/08/12)
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- MANUFACTURING METHOD OF OPTICAL ACTIVE SECONDARY ALCOHOL
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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
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Paragraph 0099
(2019/03/20)
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- BRUTON'S TYROSINE KINASE INHIBITORS
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Bruton's tyrosine kinase (Btk) inhibitors have the following Formula (I).
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Page/Page column 21
(2018/10/19)
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- TETRAHYDRO-IMIDAZO[1,5-A]PYRAZINE DERIVATIVES SALTS, PREPARATION PROCESS AND PHARMACEUTICAL USE THEREOF
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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.
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Page/Page column 15; 18
(2016/10/08)
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- PROCESS FOR PRODUCING OPTICALLY ACTIVE SECONDARY ALCOHOL
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[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)].
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Paragraph 0150; 0151; 0152
(2015/02/19)
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- BIARYL ETHER SULFONAMIDES AND THEIR USE AS THERAPEUTIC AGENTS
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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.
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- SALTS OF TETRAHYDROIMIDAZO Y1,5-A¨PYRAZINE DERIVATIVES, PREPARATION METHODS AND PHARMACEUTICAL USE THEREOF
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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.
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Page/Page column 9
(2012/02/04)
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- TETRAHYDRO-IMIDAZO[1,5-a]PYRAZINE DERIVATIVES SALTS, PREPARATION METHODS AND MEDICINAL USE THEREOF
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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.
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Page/Page column 9
(2012/03/27)
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- TETRAHYDRO-IMIDAZOY1,5-A¨PYRAZINE DERIVATIVES, PREPARATION METHODS AND MEDICAL USES THEREOF
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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.
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Page/Page column 18
(2010/10/03)
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- 7-Substituted Purine Derivatives for Immunosuppression
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The present invention provides novel purinone and related derivatives useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection. The compounds are of the general formula III:
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Page/Page column 10
(2008/12/05)
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- 7-SUBSTITUTED PURINE DERIVATIVES FOR IMMUNOSUPPRESSION
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The present invention provides novel purinone and related derivatives useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection. The compounds are of the general formula (III).
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Page/Page column 29
(2008/12/05)
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- ORGANIC COMPOUNDS
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The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.
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Page/Page column 103
(2008/12/08)
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- PURINE AND IMIDAZOPYRIDINE DERIVATIVES FOR IMMUNOSUPPRESSION
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The present invention provides novel purine and imidazopyridine derivatives useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection. The compounds are of the general formulas ( I ) and ( II ).
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Page/Page column 30
(2010/11/24)
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- CB1 MODULATOR COMPOUNDS
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Novel compounds of structural formula (I) are disclosed. As modulators of the Cannabinoid-1 (CB1) receptor, these compounds are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. As such, compounds of the present invention are useful as in the treatment, prevention and suppression of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders (e.g., multiple sclerosis, Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis), cerebral vascular accidents, head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, particularly to opiates, alcohol, and nicotine. The compounds are also useful for the treatment of obesity or eating disorders associated with excessive food intake and complications associated therewith.
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Page/Page column 61-62
(2008/06/13)
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- SUBSTITUTED QUINAZOLINE DERIVATIVES AND THEIR USE AS INHIBITORS
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The use of a compound of formula (I) 1 or a salt, ester or amide thereof; where X is O, or S, S(O) or S(O)2, or NR6 where R6 is hydrogen or C1-6 alkyl,; R5 is an optionally substituted 5-membered heteroaromatic ring, R1, R2 ,R3, R4 are independently selected from various specified moieties, in the preparation of a medicament for use in the inhibition of aurora 2 kinase. Certain compounds are novel and these, together with pharmaceutical compositions containing them are also described and claimed
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- Supported nickel-catalyzed hydrogenation of aromatic nitriles under low pressure conditions
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Hydrogenation of aromatic nitriles takes place under the mild conditions using supported nickel catalysts to afford amino-methyl-substituted aromatics in good yields.
- Takamizawa,Wakasa,Fuchikami
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p. 1623 - 1625
(2007/10/03)
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- N-substituted ergoline- and 9,10-didehydro-ergoline-8-carboxamide-and-8-aminomethyl-derivatives, their production and their pharmaceutical composition
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Novel N-substituted ergoline- and 9,10-didehydro-8-carboxamide- and -8-aminomethyl-derivatives for the treatment of vascular headaches, especially migraine, and of orthostatic hypotension.
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