- Copper-Catalyzed Monoorganylation of Trialkyl Borates with Functionalized Organozinc Pivalates
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Organozinc pivalates, a recently developed air- and moisture-stable organozinc species, were found for the first time as excellent organometallic species in the monoorganylation of trialkyl borates whereby boronic acids were prepared in high yields. The significant advantage of organozinc pivalates over another previously employed organometallic reagents, e. g., organolithium reagents, Grignard reagents and organozinc halides, is that the generation of multiorganylation byproducts such as borinic acids and trialkylboranes were completely suppressed. Additionally, the in situ generated boronates could be directly arranged into Suzuki-Miyaura type cross-coupling reactions to produce biaryls in high yields.
- Fu, Ying,Gou, Bei-Lei,Shi, Chun-Zhao,Du, Zhengyin,Shen, Tong
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p. 4253 - 4257
(2018/09/18)
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- Stabilization of zwitterionic aryltrifluoroborates against hydrolysis
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The presence of a proximal cationic group in zwitterionic aryltrifluoroborates such as o-(Ph2MeP)C6H 4(BF3) stabilizes these compounds against hydrolysis.
- Wade, Casey R.,Zhao, Haiyan,Gabba?, Franois P.
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supporting information; experimental part
p. 6380 - 6381
(2010/10/18)
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- NITROGEN CONTAINING HETEROAROMATICS AS FACTOR Xa INHIBITORS
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The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula (I) or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and D may be C(=NH)NH2, which are useful as inhibitors of factor Xa.
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Page/Page column 60
(2009/10/01)
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- PREVENTIVE OR THERAPEUTIC AGENT FOR KIDNEY DISEASE
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The present invention relates to an agent for the prevention or treatment of a renal disease comprising as an active ingredient a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is a hydrogen atom or an optionally substituted alkyl group; R2 is a dialkylamino group, an alkyl group, a cycloalkyl group, an optionally substituted aryl group etc.; T is an oxygen atom, a sulfur atom etc.; Q is a hydrogen atom or an optionally substituted alkyl group; and Z is a hydrogen atom, a hydroxy group etc., or a pharmaceutically acceptable salt thereof which has an inhibitory effect on mesangial cell proliferation and a decreasing effect on protein excretion in urine, and are useful for preventing or treating of various renal diseases such as IgA nephropathy, diabetic nephropathy, nephritic syndrome and the like.
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- 5-AMIDINO-2-HYDROXYBENZENESULFONAMIDE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AND INTERMEDIATES FOR THEIR PREPARATION
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The present invention relates to a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is a hydrogen atom or an optionally substituted lower alkyl group; R2 is a di(lower alkyl)amino group,
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- OXYGEN OR SULFUR CONTAINING 5-MEMBERED HETEROAROMATICS AS FACTOR Xa INHIBITORS
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The present application describes oxygen and sulfur containing heteroaromatics and derivatives thereof of formula (I), or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is O or S and D may be C(=NH)NH2, which are useful as inhibitors of factor Xa.
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- Factor xa inhibitors with aryl-amidines and derivatives, and prodrugs thereof
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The present invention relates to a compound with aryl-amidines, particularly amidinoaryl-cyclopropanes, amidinoarylmethyl-pyrroles, amidinoaryl-benzenes, amidinoaryl-pyridines, or amindonoaryl-alanines, represented by formula (1), a pharmaceutically acceptable salt, a prodrug, a hydrate, a solvate or an isomer thereof, which are inhibitors of coagulation enzyme, factor Xa (FXa). The present invention also relates to a pharmaceutical composition containing the compound, and a method of using the same as an anticoagulant agent for treatment and prevention of thrombosis disorders.
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- Phenyl-isoxazoles as factor XA Inhibitors
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The present application describes oxygen and sulfur containing heteroaromatics and derivatives thereof of formula or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is O or S and D may be C(=NH)NH2, which are useful as inhibitors of factor Xa.
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- Nitrogen containing heteroaromatics as factor Xa inhibitors
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The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and D may be C(=NH)NH2, which are useful as inhibitors of factor Xa.
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- INHIBITORS OF FACTOR XA WITH A NEUTRAL P1 SPECIFICITY GROUP
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The present application describes inhibitors of factor Xa with a neutral P1 specificity group of formula I: STR1 or pharmaceutically acceptable salt forms thereof, wherein R and E may be groups such as methoxy and halo.
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