CAS: 58584-94-4; 2,6-Dichloro-3-Methylpyridine

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18368-76-8 72093-12-0 18368-64-4

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CAS号2402-78-0 2,6-二氯吡啶 | CAS号74-88-4 碘甲烷 | CAS号20173-49-3 2-氯-5-甲基吡啶-N-氧化物 | CAS号88-95-9 邻苯二甲酰氯 | CAS号125849-94-7 3,5-二氯-6-甲基-1,4... | CAS号74-86-2 乙炔 | CAS号91668-83-6 2-氯-3-甲基吡啶-N-氮氧化物 | CAS号29553-51-3 3-甲基哌啶-2,6-二酮 | CAS号18368-76-8 2-氯-3-甲基吡啶 | CAS号4553-62-2 2-甲基戊二腈

3-甲基环戊烷-1,2-二胺置于硫酸,溶剂黄146体系中,化学反应 3.0H,反应生成 2,6-二氯-3-甲基吡啶
参考文献:Synthesis And Biological Evaluation Of Aroylguanidines Related To Amiloride As Inhibitors Of The Human Platelet Na+/h+ Exchanger
标题:Synthesis And Biological Evaluation Of Aroylguanidines Related To Amiloride As Inhibitors Of The Human Platelet Na+/h+ Exchanger
摘要:Pyridine And Benzene Bioisosteres Of Amiloride Were Synthesized And Evaluated For Their Inhibitory Potency Against The Sodium-Hydrogen Exchanger (Nhe) Involved In Intracellular Ph Regulation. The Inhibition Of Nhe Was Determined By Using The Platelet Swelling Assay (Psa) In Which The Swelling Of Human Platelets Was Induced By Their Incubation In An Acid Buffer (Ph 6.7). Additionally,The Inhibitory Potency Of The Most Active Compounds Was Assessed By Measuring The Inhibition Of The Eipa-Sensitive Na-22 (+) Uptake (Uia) By Human Platelets After Intracellular Acidosis. The Results Indicated That Several Benzene Derivatives And Compounds Bearing An Carbonylguanidine Moiety In The Meta Position Of The Pyridine Nitrogen Were Much More Potent Than Amiloride (Psa:Ic50 = 43.5 Mum,Uia:Ic50 = 100.1 Mum),But Less Than Eipa,A Pyrazine Nhe Inhibitor (Psa:Ic50=0.08 Mum,Uia: Ic50-0.5 Mum). In Both Biological Assays (2-Amino-5-Bromo-Pyridine-3-Carbonyl)Guanidine (32) Was The Most Active Molecule (Psa: Ic50 = 0.8 Mum,Uia : Ic50 = 0.8 Mum). Our Investigations Demonstrated That The Replacement Of The Pyrazine Ring Of Amiloride E By A Pyridine Ora Phenyl Ring Improved The Nhe Inhibitory Potency (Phenyl >Pyridine >Pyrazine). (C) 2002 Elsevier Science Ltd. All Rights Reserved.
DOI:10.1016/s0968-0896(02)00022-6

专利信息

专利号:WO-2014158302-A1
优先权日:2013-03-25
标 题:Novel sphingosine 1-phosphate receptor antagonists
发明人：SWENSON ROLF ERIC
权利人:SWENSON ROLF ERIC
摘要:The present invention relates to sphingosine-1 -phosphate (S1 P) receptors and compounds of the general formula (1), that are useful in the treatment and prevention of conditions associated with such receptors. More specifically, the present invention relates to the synthesis and use of sphingosine 1 -phosphate receptor 2 (S1 P2) antagonists that are useful in the treatment of cancer, atherosclerosis, diabetic retinopathy, and other inflammatory diseases. Among these inflammatory diseases that could be treated with these S1 P2 antagonist are those characterized by fibrosis including chronic lung disease, chronic kidney and liver disease, chronic heart disease, and skin diseases such as sclerosis/scleroderma. The S1 P2 antagonists can also be used in the treatment of glioblastoma multiforme (brain cancer), pediatric neuroblastoma, and other cancers.

专利号:US-9663511-B2
优先权日:2012-03-26
标题:Sphingosine 1-phosphate receptor antagonists
发明人：SWENSON ROLF E
权利人:ARROYO BIOSCIENCES LLC
摘要:The present invention relates to sphingosine-1-phosphate (S1P) receptors and compounds of the general formula: n nthat are useful in the treatment and prevention of conditions associated with such receptors. More specifically, the present invention relates to the synthesis and use of sphingosine 1-phosphate receptor 2 (S1P 2 ) antagonists that are useful in the treatment of cancer, atherosclerosis, diabetic retinopathy, and other inflammatory diseases. Among these inflammatory diseases that could be treated with these S1P 2 antagonist are those characterized by fibrosis including chronic lung disease, chronic kidney and liver disease, chronic heart disease, and skin diseases such as sclerosis/scleroderma. The S1P 2 antagonists can also be used in the treatment of glioblastoma multiforme (brain cancer), pediatric neuroblastoma, and other cancers.