CAS: 75680-92-1; Ethyl 6-Chloro-3-Pyridazinecarboxylate

相似化合物

5096-73-1 303085-53-2 1011487-94-7

上下游产品

CAS号1211587-01-7 5-氯哒嗪-3-羧酸 | CAS号63001-31-0 3-哒嗪酮-6-甲酸乙酯 | CAS号37972-69-3 6-羟基-3-哒嗪甲酸 | CAS号13327-27-0 6-甲基-3(2H)-哒嗪酮 | CAS号303085-53-2 6-氯哒嗪-3-甲醛 | CAS号98548-01-7 6-氨基哒嗪-3-甲酸乙酯 | CAS号66346-83-6 6-氯哒嗪-3-甲酰胺 | CAS号77407-73-9 ethyl 6-morphol...

Alpha-酮戊二酸置于盐酸,溴,溶剂黄146,Sodium Hydroxide,硫酸肼,三氯氧磷体系中,用 水 作为反应溶剂,化学反应 16.0H,反应生成 6-氯哒嗪3-羧酸乙酯
参考文献:开发哒嗪-3-羧酰胺作为cb2激动剂:设计,合成,结构-活性关系和对接研究
标题:开发哒嗪-3-羧酰胺作为cb2激动剂:设计,合成,结构-活性关系和对接研究
摘要:在这里,我们描述了通过支架跳跃和生物等排策略的组合,将一系列哒嗪-3-羧酰胺设计和合成为cb2选择性激动剂.通过钙动员测定法对化合物的潜在活性进行评估.在测试的衍生物中,这些化合物中超过一半的化合物表现出中等至有效的cb2激动剂活性.六种化合物的ec 50值低于35 Nm,几种衍生物在cb2受体上的效力和选择性也大大高于cb1受体.具体而言,化合物26显示出最高的cb2激动剂活性(ec 50 = 3.665+/-0.553Nm)和对cb1的显着选择性(选择性指数＞ 2729).此外,与gw842166X相比,一些代表性化合物的logps被测量为显示出明显降低的值.此外,进行了对接仿真以解释该系列的交互模式.
DOI:10.1016/j.Ejmech.2017.05.060

专利信息

专利号:WO-0107416-A1
优先权日:1999-07-28
标题 :Method of producing pyridazine carboxylic acid derivatives
发明人：BESSARD YVES; CRETTAZ ROGER; EGGEL MICHAEL
权利人:LONZA AG; BESSARD YVES; CRETTAZ ROGER; EGGEL MICHAEL
摘要:The invention relates to a method of producing pyridazine carboxylic acid derivatives of the general formulae (Ia) or (Ib), wherein R<1> represents a group of the formula -OR<3> or -NR<4>R<5>, R<2> represents hydrogen, chlorine, a group of the formula -OR<6> or a group of the formula -NR<7>R<8>, R<3> represents C1-10 alkyl, C3-8 cycloalkyl or aryl-C1-4-alkyl, R<4> represents C1-10 alkyl, C3-8 cycloalkyl, optionally substituted aryl or aryl-C1-4-alkyl, R<5> represents hydrogen, C1-10 alkyl, C3-8 cycloalkyl, optionally substituted aryl or aryl-C1-4-alkyl and R<6> represents C1-10 alkyl, C3-8 cycloalkyl, aryl-C1-4-alkyl or an optionally substituted aromatic or heteroaromatic rest and R<7> and R<8> represent independently C1-10 alkyl, C3-8 cycloalkyl or aryl-C1-4-alkyl or together with the nitrogen atom form a saturated or aromatic heterocyclic ring. The inventive derivatives are obtained by reacting the corresponding 3-chloropyridazines or 3,6-dichloropyridazine with carbon monoxide and alcohols or amines H-R<1> in the presence of palladium-phosphin complexes and bases. The pyridazine carboxylic acid derivatives (Ia, Ib) are the intermediates for the synthesis of pharmaceutically active substances.

专利号:US-2009069334-A1
优先权日:2007-08-18
标题:Pyridazine based alpha-helix mimetics
发明人：REBEK JR JULIUS; BIROS SHANNON; MOISAN LIONEL; VOLONTERIO ALESSANDRO; MANN ENRIQUE; DALE TREVOR
权利人:SCRIPPS RESEARCH INST
摘要:The synthesis of new α-helix scaffolds mimicking i, i+3 or i+4, i+7 residues, was accomplished. The common pyridazine heterocycle originates from the easily available building block, 6. These scaffolds may be thought of as synthetic counterparts of amphiphilic α-helices having a “wet faceâ€? along one side and a hydrophobic face along the other side of the helix.

专利号:US-8344010-B2
优先权日:2008-12-26
标 题 :Fused imidazole derivatives as TRPV3 antagonist
发明人：LINGAM V S PRASADARAO; THOMAS ABRAHAM; PHATANGARE SHANTARAM KASHINATH; MINDHE AJIT SHANKAR; KHATIK JAVED YUSUF; KHAIRATKAR-JOSHI NEELIMA; KATTIGE VIDYA GANAPATI
权利人:GLENMARK PHARMACEUTICALS SA; LINGAM V S PRASADARAO; THOMAS ABRAHAM; PHATANGARE SHANTARAM KASHINATH; MINDHE AJIT SHANKAR; KHATIK JAVED YUSUF; KHAIRATKAR-JOSHI NEELIMA; KATTIGE VIDYA GANAPATI
摘要:The present invention provides transient receptor potential vanilloid (TRPV) modulators of formula (I). In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.