- Diruthenium complexes with a 1,8-Naphthyridine-based Bis(silyl) supporting ligand: Synthesis and structures of complexes containing RuII2(μ-H)2 and RuI2 cores
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We designed a novel naphthyridine-based supporting ligand involving two silyl coordinating moieties at 2,7-positions, t-BuNBSi, for the synthesis of dinuclear metal complexes. Reaction of a ligand precursor t-BuNBSi(H)2 (1) with Ru3(CO)12 gave a di-μ-hydridodiruthenium(II,II) complex (t-BuNBSi)Ru2(μ-H)2(CO)4 (2). Photoirradiation to 2 resulted in the formation of a diruthenium(I,I) complex (t-BuNBSi)Ru2(CO)6 (3). The SiRuRuSi linkage of 2 takes a zigzag arrangement, whereas that of 3 adopts a roughly linear one.
- Kusuma, Indra,Komuro, Takashi,Tobita, Hiromi
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p. 400 - 403
(2018/03/27)
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- Method for preparing 2-amino-3-hydroxymethylpyridine
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The invention discloses a method for preparing 2-amino-3-hydroxymethylpyridine, and belongs to the field of chemical synthesis. 2-aminopyridine and pivaloyl chloride are used as initial reactants to form intermediate product 2-pivalamidopyridine under the action of triethylamine, after hydrogen extraction by use of n-butyllithium, dimethylformamide is added for hydroformylation, and target product2-amino-3-hydroxymethylpyridine can be obtained by reduction with sodium borohydride. Raw materials used in the method are low in cost, and the method is simple in operation, short in synthesis process, mild in reaction conditions, high in yield, and suitable for large-scale industrial production.
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- HETEROCYCLIC CGRP RECEPTOR ANTAGONISTS
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The present invention is directed to heterocyclic compounds which are antagonists of CGRP receptors and may be useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
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Page/Page column 87
(2016/05/19)
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- RING-FUSED 2-PYRIDONE DERIVATIVES AND HERBICIDES
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Provided are 2-pyridone derivatives which have excellent herbicidal activity and exhibit high safety to useful crops and so on; salts thereof; and herbicides containing same. In more detail, 2-pyridone derivatives represented by general formula [I] or agrochemically acceptable salts thereof, and herbicides containing these compounds are provided. In general formula [I], X1 is an oxygen atom or a sulfur atom; X2, X3, and X4 are to each CH or N(O)m; m is an integer of 0 or 1; R1 is a hydrogen atom, a C1-12 alkyl group, or the like; R2 is a halogen atom, a cyano group, or the like; n is an integer of 0 to 4; R3 is a hydroxyl group, a halogen atom, or the like; A1 is C(R11R12); A2 is C(R13R14) or C═O; A3 is C(R15R16); and R11, R12, R13, R14, R15, and R16 are each independently a hydrogen atom or a C1-6 alkyl group.
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Page/Page column 68
(2011/12/12)
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- NOVEL ANTIMALARIA AGENT CONTAINING HETEROCYCLIC COMPOUND
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Disclosed is an antimalarial agent containing a compound represented by the formula: [wherein A1 represents a 3-pyridyl group that may have a substituent, a 6-quinolyl group that may have a substituent, or the like; X1 represents a group represented by the formula -C(=O)-NH- or the like; E represents a furyl group, a thienyl group or a phenyl group; with the proviso that A1 may have one to three substituents, and E has one of two substituents] or a salt thereof or hydrates thereof.
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Page/Page column 59
(2008/06/13)
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- CONSTRAINED COMPOUNDS AS CGRP-RECEPTOR ANTAGONISTS
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The invention encompasses constrained bicyclic and tricyclic CGRP-receptor antagonists, methods for identifying them, pharmaceutical compositions comprising them, and methods for their use in therapy for treatment of migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.
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Page/Page column 85
(2008/06/13)
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- CGRP antagonists
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The present invention encompasses compounds of Formula I which are antagonists of calcitonin gene-related peptide receptors (“CGRP-receptor”), pharmaceutical compositions comprising them, methods for identifying them, methods of treatment using them and t
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Page/Page column 10-11
(2010/11/26)
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- NOVEL ANTIFUNGAL AGENT COMPRISING HETEROCYCLIC COMPOUND
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The present invention provides an antifungal agent represented by the formula: [wherein A1 represents a 3-pyridyl group which may have a substituent, a quinolyl group which may have a substituent, or the like; X1 represents a group represented by the formula -NH-C(=O)-, a group represented by the formula -C(=O)-NH-, or the like; E represents a furyl group, a thienyl group, a pyrrolyl group, a phenyl group, a pyridyl group, a tetrazolyl group, a thiazolyl group or a pyrazolyl group; with the proviso that A1 may have 1 to 3 substituents, and E has one or two substituents].
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Page/Page column 67
(2010/11/08)
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- Constrained compounds as CGRP-receptor antagonists
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The invention encompasses constrained bicyclic and tricyclic CGRP-receptor antagonists, methods for identifying them, pharmaceutical compositions comprising them, and methods for their use in therapy for treatment of migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.
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Page/Page column 49
(2008/06/13)
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- VITRONECTIN RECEPTOR ANTAGONISTS
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Compounds of formula (I) are disclosed which are vitronectin receptor antagonists and are useful in the treatment of osteoporosis wherein R is Het- or Ar; R is formula (a) or formula (b); or a pharmaceutically acceptable salt thereof.
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- Alpha v integrin receptor antagonists
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The present invention relates to novel chain-fluorinated alkanoic acid derivatives thereof, their synthesis, and their use as αv integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin recep
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- αv integrin receptor antagonists
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The present invention relates to novel nonanoic acid derivatives, their synthesis, and their use as αv integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors αvβ3 and αvβ5 and are
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- Modified aminoacids, pharmaceuticals containing these compounds and method for their production
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The present invention relates to modified amino acids of general formula wherein A, Z, X, n, m, R, R2, R3, R4and R11are defined as in claims 1 to 5, their tautomers, their diastereomers, their enantiomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them as well as their use for the production and purification of antibodies and as labelled compounds in RIA- and ELISA assays and as diagnostic or analytical aids in neurotransmitter research.
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Page column 130-131
(2008/06/13)
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- Highly efficient synthesis of 2-amino-3-pyridinecarboxaldehyde
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2-Amino-3-pyridinecarboxaldehyde is synthesized in a highly efficient process via ortho-lithiation of 2-(pivaloyl-amino)pyridine and reaction with DMF, followed by acid hydrolysis. Major impurities were identified and were cleanly eliminated through careful choice of base and solvent.
- Rivera,Hsiao,Cowen,McWilliams,Armstrong,Yasuda,Hughes
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p. 1573 - 1579
(2007/10/03)
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- Modified amino acids, pharmaceuticals containing these compounds and method for their production
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The present invention relates to modified amino acids of general formula wherein A, Z, X, n, m, R, R2, R3, R4 and R11 are defined as in claims 1 to 5, their tautomers, their diastereomers, their enantiomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them as well as their use for the production and purification of antibodies and as labelled compounds in RIA- and ELISA assays and as diagnostic or analytical aids in neurotransmitter research.
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- Pyridazinone and pyrazolone compounds, cardiotonic compositions including same, and their uses
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This invention relates to substituted pyridooxazinone and naphtheridone pyridazinone and pyrazolone compounds which are useful as cardiotonic agents for the treatment of congestive heart failure, to methods for increasing cardiac contractility using said
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- Naphtheridinone- and pyridooxazinone-pyridone compounds, cardiotonic compositions including same, and their uses
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This invention relates to substituted pyridooxazinone and naphtheridone pyridones which are useful as cardiotonic agents for the treatment of congestive heart failure, to methods for increasing cardiac contractility using said compounds, and pharmaceutical compositions including the same.
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- Regiospecific Electrophilic Substitution of Aminopyridines: Ortho Lithiation of 2-, 3-, and 4-(Pivaloylamino)pyridines
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2- and 4-(pivaloylamino)pyridines have been shown to undergo metalation exclusively at C-3 and these smoothly react with a variety of electrophiles to produce 2,3- and 3,4-disubstituted pyridines, respectively.Removal of the pivaloyl protecting group results in overall electrophilic substitution of an aminopyridine.Utilization of this method is exemplified by efficient syntheses of 2- and 4-aminonicotinaldehydes.Minor modifications of the reaction conditions permitted exclusive ortho metalation of 2-(pivaloylamino)pyridines additionally functionalized by chloro, fluoro, or methyl groups.Although the major product from reaction of 3-(pivaloylamino)pyridine by this method was metalation at C-4, the reaction was complicated by substantial quantities of product derived from nucleophilic attack by n-butyllithium on the pyridine nucleus.
- Turner, James A.
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p. 3401 - 3408
(2007/10/02)
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