CAS: 6326-79-0; 6-Bromoindoline-2,3-Dione

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CAS号65971-74-6 N-(3-bromopheny... | CAS号303743-53-5 | CAS号591-19-5 3-溴苯胺 | CAS号195526-38-6 N,N'-bis-(3-bro... | CAS号302-17-0 水合氯醛 | CAS号885278-42-2 6-溴-1H-吲唑-3-甲酸甲酯 | CAS号20776-50-5 2-氨基-4-溴苯甲酸 | CAS号99365-40-9 6-溴-1,3-二氢-2H-吲哚-2-酮 | CAS号885272-94-6 6-溴-1H-吲唑-3-羧酸乙酯 | CAS号959237-68-4 2,4-二氯-7-溴喹唑啉 | CAS号660823-36-9 6-溴吲唑-3-羧酸 | CAS号76561-16-5 4-溴靛红酸酐 | CAS号139582-54-0 6-MONOBROMOINDIGO | CAS号114703-12-7 7-溴喹唑啉-2,4-二酮 | CAS号31009-04-8 7-溴喹啉-4-羧酸

N-(3-Bromophenyl)-2-Hydroxyiminacetamide置于硫酸体系中,用32%的收率获得产物6-溴靛红
参考文献:Gsk2193874的发现:瞬态潜在电位香草醛的口服活性,有效和选择性阻滞剂4.
标题:Gsk2193874的发现:瞬态潜在电位香草醛的口服活性,有效和选择性阻滞剂4.
摘要:瞬时受体电位vanilloid 4(trpv4)是阳离子通道的瞬时受体电位(trp)超家族的成员.trpv4在肺部的血管内皮中表达,并调节肺泡间隔屏障的完整性.升高的肺血管压力会引起trpv4依赖性肺水肿,因此,抑制trpv4代表了一种新的方法来治疗与充血性心力衰竭等疾病相关的肺水肿.在这里,我们报告发现了口服活性,有效和选择性trpv4阻滞剂3-(1,4'-Bipiperidin-1'-Ylmethyl)-7-Bromo-N-(1-苯基环丙基)-2-[3-(三氟甲基)苯基]-4-喹啉羧酰胺(gsk2193874,28)解决了从体内研究中观测到的意外脱靶心血管不良反应.
DOI:10.1021/acsmedchemlett.7B00094

专利信息

专利号:US-9073900-B2
优先权日:2013-10-02
标题:Dihydroquinone derivatives of piperidine and piperazine
发明人：ULLAH NISAR
权利人:UNIV KING FAHD PET & MINERALS; KING ABDULAZIZ CITY SCI & TECH
摘要:The dihydroquinone derivatives of piperidine and piperazine are 7-piperazinyl and 7-piperadinyl-3,4-dihydroquinazolin-2(1H)-ones that exhibit D 2 and 5-HT 1A receptor binding affinities, making them suitable for use as the active ingredient of pharmaceuticals for the treatment of schizophrenia. The derivatives have the general formula: n nwhere X is carbon or nitrogen and R is a group selected from a through f having the formula:n n nor a pharmaceutically acceptable salt thereof. The piperazine compounds are prepared by condensing 4-bromo-2-nitro-benzonitrile with 1-Boc-piperazine (1-tert-butoxycarbonyl-piperazine) to form an intermediate that is converted to a piperazinyl-3,4-dihydroquinazolin-2(1H)-one. Subsequent reductive amination with the biarylaldehydes a through f completes the synthesis of the 7-piperadinyl-3,4-dihydroquinazolin-2(1H)-ones. The piperadinyl compounds are prepared from tert-butyl-4-(2-oxo-1,2,3,4-tetradihydroquinazolin-7-yl)piperidine-1-carboxylate, which is converted to 7-(piperidin-4-yl)-3,4-dihyroquinazolin-2(1H)-one. Subsequent reductive amination with the biarylaldehydes a through f completes the synthesis of the 7-piperidinyl-3,4-dihydroquinazolin-2(1H)-ones.

专利号:WO-2011050245-A1
优先权日:2009-10-23
标 题:Bicyclic heteroaryls as kinase inhibitors
发明人：FENG YANGBO; CHEN YEN TING; SESSIONS HAMPTON; MISHRA JITENDRA K; CHOWDHURY SARWAT; YIN YAN; LOGRASSO PHILIP; LUO JUN-LI; BANNISTER THOMAS; SCHROETER THOMAS
权利人:FENG YANGBO; CHEN YEN TING; SESSIONS HAMPTON; MISHRA JITENDRA K; CHOWDHURY SARWAT; YIN YAN; LOGRASSO PHILIP; LUO JUN-LI; BANNISTER THOMAS; SCHROETER THOMAS
摘要:The invention is directed to heteroaryl compounds useful as inhibitors of various kinase enzymes. In various embodiments, the invention provides a heteroaryl compound having inhibitory bioactivity with respect to a Rho kinase, an AKT kinase, a p70S6K kinase, a LIM kinase, an IKK kinase, a Flt kinase, an Aurora kinase, or a Src kinase, or any combination thereof. Compounds of the invention include bicyclic heteroaryl compounds of formula (I), which can contain a bridging nitrogen atom at a ring junction. The invention further provides methods of synthesis of compounds of the invention, pharmaceutical compositions, pharmaceutical combinations, and methods of treatment of malconditions using compounds of the invention.

专利号:US-11840537-B2
优先权日:2020-11-03
标 题:Preparation and application of a 5-bromoquinazoline derivative
发明人：LUO MEI
权利人:LUO MEI; UNIV HEFEI TECHNOLOGY
摘要:A 5-bromoquinazoline derivative (I), structural formula thereof is as follows:the synthesis method thereof comprises weighing 1.18 g of 5-bromoisatin, 2.5503 g of ammonium formate and 100 ml of absolute methanol in a 250 mL round-bottom flask, heating, stirring and refluxing for 48 h, stopping reaction, rotating to obtain 1.6033 g of filter residue crude product, carrying out column chromatography separation by using dichloromethane and absolute methanol according to a volume ratio of 1:1, and obtaining a target crystal compound I; the application of the 5-bromoquinazoline derivative compound crystal (I), as a catalyst has a good catalytic effect in nitrile silicification reaction of benzaldehyde and auto-polymerization reaction of benzophenone hydrazone, the conversion rates thereof respectively reach 39% and 76%, and the crystal (I) can be used as an anti-cancer reagent which has certain anti-cancer activity of breast cancer, liver cancer and lung cancer.

专利号:US-8952042-B2
优先权日:2009-08-19
标 题 :FXR (NR1H4) binding and activity modulating compounds
发明人：KREMOSER CLAUS; ABEL ULRICH; STEENECK CHRISTOPH; KINZEL OLAF
权利人:KREMOSER CLAUS; ABEL ULRICH; STEENECK CHRISTOPH; KINZEL OLAF; PHENEX PHARMACEUTICALS AG
摘要:The present invention relates to compounds of formula (1): n nwhere R, A, Q and Z are defined herein, or an enantiomer, diastereomer, tautomer, solvate, prodrug or pharmaceutical acceptable salt thereof. These compounds bind to the NR1H4 receptor (FXR) and act as agonists of the NR1H4 receptor (FXR). The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds, and to a process for the synthesis of said compounds.

专利号:CN-111187233-B
优先权日:2020-01-18
标 题:A kind of multi-substituted benzothiazole and its derivatives and its synthesis method

专利号:CN-112500341-B
优先权日:2020-11-16
标题 :Synthesis method of 7-hydroxyquinoline-4-carboxylic acid