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CAS号141-30-0 3,6-二氯哒嗪 | CAS号17284-97-8 3-氯-6-肼基哒嗪 | CAS号14959-31-0 N-(6-氯-3-哒嗪基)乙酰胺 | CAS号108-98-5 硫酚 | CAS号80-32-0 磺胺氯哒嗪 | CAS号5096-76-4 3-氯-6-(1H-吡咯-1-基)哒嗪 | CAS号39614-78-3 6-乙氧基哒嗪-3-胺 | CAS号5469-70-5 3-氨基哒嗪 | CAS号35053-55-5 [2-(6-氯-3-吡嗪)-2... | CAS号58059-47-5 3-氨基-6-(4-氯苯基)哒嗪 | CAS号14714-18-2 6-氯-2-甲基-咪唑并[2,... | CAS号14959-31-0 N-(6-氯-3-哒嗪基)乙酰胺 | CAS号147362-88-7 N-(6-氯哒嗪-3-基)新戊酰胺 | CAS号4776-87-8 6-(4-甲氧基苯基)哒嗪-3-胺 | CAS号446273-59-2 3-氨基-4-溴-6-氯哒嗪3-氯-6-肼基哒嗪置于镍 氢气体系中,用 甲醇 作为反应溶剂,20.0 °C,101.32 Kpa 条件下,反应生成 3-氨基-6-氯哒嗪
参考文献:一系列作为选择性gaba-A拮抗剂的γ-氨基丁酸氨基哒嗪衍生物的合成与构效关系.
标题:一系列作为选择性gaba-A拮抗剂的γ-氨基丁酸氨基哒嗪衍生物的合成与构效关系.
摘要:我们最近发现,Gaba的芳基氨基哒嗪衍生物sr 95103 [2-(3-羧丙基)-3-氨基-4-甲基-6-苯基吡啶并鎓氯化物]是一种选择性和竞争性的gaba-A受体拮抗剂.为了进一步探索对gaba受体亲和力的结构要求,我们通过将各种哒嗪结构连接到gaba或gaba样侧链上,合成了38种化合物.大多数化合物从大鼠脑膜中取代了[3H] Gaba.所有活性化合物都拮抗了gaba引起的[3H]地西p结合的增强,强烈表明所有这些化合物都是gaba-A受体拮抗剂.从大鼠脑膜置换[3H] Gaba的化合物均未与其他gaba识别位点(gaba-B受体,Gaba吸收结合位点,谷氨酸脱羧酶,Gaba转氨酶)相互作用.它们不与与gaba-A受体相关的cl-离子载体相互作用,也不与苯并二氮杂str,士的宁和谷氨酸结合位点相互作用.因此,这些化合物似乎是特异性的gaba-A受体拮抗剂.就结构活性而言,可以得出结论,
DOI:10.1021/jm00385A003
专利信息
专利号:US-9370515-B2
优先权日:2013-03-07
标题 :Mixed lineage kinase inhibitors and method of treatments
发明人:GOODFELLOW VAL S; NGUYEN THONG X; RAVULA SATHEESH B; GELBARD HARRIS A
权利人:CALIFIA BIO INC; UNIV ROCHESTER
摘要:Provided herein are imidazopyridine compounds having an inhibitory effect on mixed lineage kinases (MLKs), methods of their synthesis, and methods of their therapeutic. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and pharmaceutical compositions.
专利号:US-8372971-B2
优先权日:2004-08-25
标 题:Heterocyclic compounds and methods of use
发明人:WRASIDLO WOLFGANG; DNEPROVSKAIA ELENA
权利人:TARGEGEN INC; WRASIDLO WOLFGANG; DNEPROVSKAIA ELENA
摘要:Heterocyclic compounds derived from benzotriazine, triazines, triazoles and oxadiazoles are disclosed. The methods of synthesis and of use of such heterocyclic compounds are also provided.
专利号:US-11685761-B2
优先权日:2017-12-20
标 题:Cyclic di-nucleotide compounds as sting agonists
发明人:ANDRESEN BRIAN M; BENNETT FRANK; CHANG WONSUK; CHILDERS MATTHEW LLOYD; CUMMING JARED N; LIM JONGWON; LU MIN; TROTTER BENJAMIN WESLEY; WU WEN-LIAN
权利人:MERCK SHARP & DOHME; ANDRESEN BRIAN M; BENNETT FRANK; CHANG WONSUK; CHILDERS MATTHEW LLOYD; CUMMING JARED N; LIM JONGWON; LU MIN; TROTTER BENJAMIN WESLEY; WU WEN LIAN; MERCK SHARP & DOHME LLC
摘要:A class of polycyclic compounds of general formula (I), wherein Base1, Base2, Y, Za, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3, R4, R4a, R5, R6, R6a, R7, R7a, R8, R8a, and R9 are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds.
专利号:US-2013072495-A1
优先权日:2010-05-14
标 题 :Fused bicyclic kinase inhibitors
发明人:LI AN-HU; MULVIHILL MARK J; STEINIG ARNO G
权利人:LI AN-HU; MULVIHILL MARK J; STEINIG ARNO G; OSI PHARMACEUTICALS LLC
摘要:Compounds of Formula I, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as but not limited to tumors driven at least in part by at least one of RON, MET, IR, IGF-1R, or ALK. This Abstract is not limiting of the invention.
专利号:US-10227344-B2
优先权日:2016-06-24
标题 :CK2 inhibitors, compositions and methods thereof
发明人:WEBBER STEPHEN E; TAO XUELIANG; BRIN ELENA
权利人:POLARIS PHARMACEUTICALS INC
摘要:The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula (I), or a stereoisomer, a tautomer or a pharmaceutically acceptable salt thereof. n nFor Formula (I) compounds R 1 , R 2 , R 3 , Ar and Z are as defined in the specification. The inventive Formula (I) compounds are inhibitors of CK2 and find utility in any number of therapeutic applications, including but not limited to treatment of proliferative disorders such as cancer, inflammation and immunological disorders.
专利号:US-8937072-B2
优先权日:2011-06-17
标题:Substituted cyanoaniline compounds, preparation and use thereof
发明人:LIU CHANGLING; HUANG GUANG; LAN JIE; HAO SHULIN; LI ZHINIAN; LI HUICHAO; GUAN AIYING; JIANG AIRU; XU YING
权利人:LIU CHANGLING; HUANG GUANG; LAN JIE; HAO SHULIN; LI ZHINIAN; LI HUICHAO; GUAN AIYING; JIANG AIRU; XU YING; SINOCHEM CORP; SHENYANG RES INST CHEMICAL IND
摘要:Disclosed is a substituted cyanoaniline compound or a salt thereof, wherein the compound has a structure represented by General Formula I. The compound of General Formula I has broad-spectrum fungicidal activity in the field of agriculture and effectively prevents against a variety of pathogens such as cucumber downy mildew, wheat powdery mildew, maize rust disease, rice blast and cucumber gray mold. In particular, even at a low dose, the compound effectively prevents and treats rice blast, cucumber gray mold, maize rust disease and cucumber downy mildew. Moreover, the raw materials for preparing the compounds are widely available and the synthesis method therefor is simple and convenient.