CAS: 49609-84-9; 2-Chloronicotinoyl Chloride

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2-氯烟酸置于氯化亚砜体系中,化学反应 12.0H,反应生成 2-氯烟酰氯
参考文献:发现和优化chromeno [2,3-C] Pyrrol-9(2 H)-作为新型选择性和口服生物利用磷酸二酯酶5抑制剂治疗肺动脉高压
标题:发现和优化chromeno [2,3-C] Pyrrol-9(2 H)-作为新型选择性和口服生物利用磷酸二酯酶5抑制剂治疗肺动脉高压
摘要:磷酸二酯酶5(pde5)抑制剂已用作治疗勃起功能障碍和肺动脉高压(pah)的临床药物.在本文中,我们详细介绍一系列新的色烯的发现[2,3-C ^]吡咯9(2 ħ)-酮衍生物作为选择性和口服生物可利用的抑制剂对磷酸二酯酶5药物化学优化导致了2,其表现出理想的抑制力为5.6 Nm,具有显着的选择性以及出色的药代动力学特性和63.4%的口服生物利用度.另外,口服2与10.0 Mg / Kg的柠檬酸西地那非相比,以5.0 Mg / Kg的剂量对mpap(平均肺动脉压)和rvhi(右心室肥大指数)的药效学效果更好.这些活性及其合理的类药物特性,例如人肝微粒体稳定性,细胞色素抑制作用,Herg抑制作用和药理安全性,表明2是治疗pah的潜在候选者.
DOI:10.1021/acs.Jmedchem.7B00523

专利信息

专利号:US-2013338369-A1
优先权日:2011-03-07
标 题 :Process for the Synthesis of Aminobiphenylene
发明人：HEINRICH MARKUS; PRATSCH GERALD
权利人:HEINRICH MARKUS; PRATSCH GERALD; BASF SE
摘要:The present invention relates to a process for the synthesis of 2-aminobiphenylene and derivatives thereof by reacting a benzene diazonium salt with an aniline compound under basic reaction conditions.

专利号:US-7244753-B2
优先权日:2002-07-29
标 题:Cyclooxygenase-2 selective inhibitors, compositions and methods of use
发明人：GARVEY DAVID S; KHANAPURE SUBHASH P; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D
权利人:NITROMED INC
摘要:The invention describes novel cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and/or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and/or preventing renal and/or respiratory toxicity; for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.

专利号:WO-2012120003-A1
优先权日:2011-03-07
标 题 :Process for the synthesis of aminobiphenylene

专利号:EP-2683682-A1
优先权日:2011-03-07
标题 :Process for the synthesis of aminobiphenylene

专利号:EP-2822924-B1
优先权日:2012-03-07
标题:Process for the synthesis of aminobiphenyls using arylhydrazines
发明人：HEINRICH MARKUS; JASCH HANNELORE; HÖFLING SARAH
权利人:BASF SE

专利号:CN-108997210-A
优先权日:2018-06-11
标 题 :A kind of Boscalid synthesis technology