16732-64-2Relevant articles and documents
4 - bromo - 2 - hydroxy indole synthesis method (by machine translation)
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Paragraph 0062; 0069, (2017/04/27)
The present invention provides 4 - bromo - 2 - hydroxy indole synthesis method, its steps are as follows: (1) the aluminum powder and zirconium oxide grinding ball into the ball mill pot ball grinding pre-processing aluminum powder; (2) hydrogenation the sodium uses pentane is pretreated pre-processing sodium hydride; (3) the pre-processing of aluminum powder and pretreatment sodium hydride, zirconium oxide grinding ball, to join the ball rubs the pot ball grindingnitric acid titanium, products of sodium aluminum hydride; (4) there will be aluminum nitrate, nitrate by the sol - gel process compound indium catalyst; (5) the α - (N, N - dimethylamino) - 2 - bromo - 6 nitrobenzene ethylene for the cyclization catalyst reduction compound indium prepared 4 - bromo indole; (6) the 4 - bromo indole with oxalyl, methanol prepared through the reaction of 4 - bromo indole - 2 - carboxylic acid; (7) will be 4 - bromo indole - 2 - carboxylic acid is sodium aluminum hydride reduction to obtain the target product. The invention of high yield, low cost. (by machine translation)
Integrin expression inhibitors
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, (2008/06/13)
The present invention provides an integrin expression inhibitor, and an agent for treating arterial sclerosis, psoriasis, cancer, retinal angiogenesis, diabetic retinopathy or inflammatory diseases, an anticoagulant, or a cancer metastasis suppressor on the basis of an integrin inhibitory action. Namely, it provides an integrin expression inhibitor comprising, as an active ingredient, a sulfonamide compound represented by the following formula (I), a pharmacologically acceptable salt thereof or a hydrate of them. In the formula, B means a C6-C10 aryl ring or 6- to 10-membered heteroaryl ring which may have a substituent and in which a part of the ring may be saturated; K means a single bond, —CH═CH— or —(CR4bR5b)mb— (wherein R4b and R5b are the same as or different from each other and each means hydrogen atom or a C1-C4 alkyl group; and mb means an integer of 1 or 2); R1 means hydrogen atom or a C1-C6 alkyl group; Z means a single bond or —CO—NH—; and R means a C6-C10 aryl ring or 6- to 10-membered heteroaryl ring which may have a substituent and in which a part of the ring may be saturated, respectively.
The first potent and selective non-imidazole human histamine H4 receptor antagonists
Jablonowski, Jill A.,Grice, Cheryl A.,Chai, Wenying,Dvorak, Curt A.,Venable, Jennifer D.,Kwok, Annette K.,Ly, Kiev S.,Wei, Jianmei,Baker, Sherry M.,Desai, Pragnya J.,Jiang, Wen,Wilson, Sandy J.,Thurmond, Robin L.,Karlsson, Lars,Edwards, James P.,Lovenberg, Timothy W.,Carruthers, Nicholas I.
, p. 3957 - 3960 (2007/10/03)
Following the discovery of the human histamine H4 receptor, a high throughput screen of our corporate compound collection identified compound 6 as a potential lead. Investigation of the SAR resulted in the discovery of novel compounds 10e and 10l, which are the first potent and selective histamine H4 receptor antagonists to be described.
INTEGRIN EXPRESSION INHIBITORS
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, (2008/06/13)
The present invention provides an integrin expression inhibitor, and an agent for treating arterial sclerosis, psoriasis, cancer, retinal angiogenesis, diabetic retinopathy or inflammatory diseases, an anticoagulant, or a cancer metastasis suppressor on the basis of an integrin inhibitory action. Namely, it provides an integrin expression inhibitor comprising, as an active ingredient, a sulfonamide compound represented by the following formula (I), a pharmacologically acceptable salt thereof or a hydrate of them. In the formula, B means a C6-C10 aryl ring or 6- to 10-membered heteroaryl ring which may have a substituent and in which a part of the ring may be saturated; K means a single bond, -CH=CH- or - (CR4bR5b)mb- (wherein R4b and R5b are the same as or different from each other and each means hydrogen atom or a C1-C4 alkyl group; and mb means an integer of 1 or 2); R1 means hydrogen atom or a C1-C6 alkyl group; Z means a single bond or -CO-NH-; and R means a C6-C10 aryl ring or 6- to 10-membered heteroaryl ring which may have a substituent and in which a part of the ring may be saturated, respectively.
Indoline Analogues of Idazoxan: Potent α2-Antagonists and α1-Agonists
Fagan, Gay P.,Chapleo, Christopher B.,Lane, Anthony C.,Myers, Malcolm,Roach, Alan G.,et al
, p. 944 - 948 (2007/10/02)
The synthesis and α-adrenergic activity of a series of substituted 2-imidazolinylindolines are described.Substitution in the indoline ring generated compounds with a spectrum of adrenoceptor antagonist/agonist profiles that proved sensitive to both the nature and position of the substituent.Many of the derivatives possess greater presynaptic antagonist potency that the corresponding benzodioxan 1, dihydrobenzofuran 2, and indan 3 analogues; however, this α2-antagonism is often accompanied by α1-agonist activity.It was not possible to separate α2-antagonist from α1-agonist properties in this series.Compounds of most interest proved to be the N-ethyl 6, 5-chloro-N-methyl 18 and 5-chloro-N-ethyl 23 derivatives, all being potent α2-antagonists and α1-agonists.Substitution at the 4- and 7-position of the indoline ring generally gave compounds with nonselective agonist properties.
