CAS: 89667-40-3; (E)-7-Phenyl-7-(Pyridin-3-yl)Hept-6-Enoic Acid

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CAS号89668-28-0 methyl 7-phenyl...

📜Ethyl (E)-7-(3-Pyridyl)-7-Phenylhept-6-Enoate置于sodium Hydroxide体系中,用 乙醇 作为反应溶剂,化学反应 1.0H,反应生成 伊波格雷
参考文献:Thromboxane Synthetase Inhibitors (Txsi). Design,Synthesis,And Evaluation Of A Novel Series Of .Omega.-Pyridylalkenoic Acids
标题:Thromboxane Synthetase Inhibitors (Txsi). Design,Synthesis,And Evaluation Of A Novel Series Of .Omega.-Pyridylalkenoic Acids
摘要:A Novel Series Of Omega-Pyridylalkenoic Acids Has Been Prepared By Applying The Wittig Reaction. Modifications Were Made In The Omega-Aryl Moiety,The Alkylene Chain Length,The Alpha-Methylene Group Adjacent To The Carbonyl Group,And The Carboxyl Group Of The Molecule. The Compounds Were Tested As Inhibitors Of Thromboxane Synthetase In An In Vitro Assay And In Ex Vivo Experiments With The Rat. Most Members Of This New Class Of Thromboxane Synthetase Inhibitors (Txsi) Showed Good Activity In Both Assay Systems. (E)-7-Phenyl-7-(3-Pyridyl)-6-Heptenoic Acid (9C; Cv-4151) Was One Of The Most Potent Compounds In In Vitro Enzyme Inhibition (Ic50 = 2.6 X 10(-8) M) And,When Orally Administered,The Most Potent And Long Acting In The Inhibition Of Blood Thromboxane A2 Production In The Rat. New Conceptual Models I-Iii For The Enzyme-Substrate (Prostaglandin H2,Pgh2) And The Enzyme-Txsi Interactions Are Proposed For Understanding The Molecular Design And Structure-Activity Relations.
DOI:10.1021/jm00381A005

专利信息

专利号:US-2003050305-A1
优先权日:2000-05-22
标题:Thromboxane inhibitors, compositions and methods of use
发明人：TEJADA INIGO SAENZ DE
摘要:The present invention describes methods for treating or preventing sexual dysfunctions in males and females, and for enhancing sexual responses in males and females by administering a therapeutically effective amount of at least one thromboxane inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase, and/or at least one vasoactive agent. The male or female may preferably be diabetic. The present invention also provides novel compositions comprising at least one thromboxane inhibitor, and, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase, and, optionally, at least one therapeutic agent, such as, vasoactive agents, nonsteroidal antiinflanmmatory compounds (NSAIDs), selective cyclooxygenase-2 (COX-2) inhibitors, anticoagulants, angiotensin converting enzymes (ACE) inhibitors, angiotensin II receptor antagonists, renin inhibitors, and mixtures thereof. The present invention also provides methods for treating or preventing ischemic heart disorders, myocardial infarction, angina pectoris, stroke, migraine, cerebral hemorrhage, cardiac fatalities, transient ischaemic attacks, complications following organ transplants, coronary artery bypasses, angioplasty, endarterectomy, atherosclerosis, pulmonary embolism, bronchial asthma, bronchitis, pneumonia, circulatory shock of various organs, nephritis, graft rejection, cancerous metastases, pregnancy-induced hypertension, preeclampsia, eclampsia, thrombotic and thromboembolic disorders, intrauterine growth, gastrointestinal disorders, renal diseases and disorders, disorders resulting from elevated uric acid levels and dysmenorrhea, and for inhibiting platelet aggregation or platelet adhesion or relaxing smooth muscles.

专利号:US-4760068-A
优先权日:1982-06-14
标题:Certain pyridyl alkenoic acid derivatives which inhibit the action of thromboxane A2 synthetase
发明人：TERAO SHINJI; NISHIKAWA KOHEI
权利人:TAKEDA CHEMICAL INDUSTRIES LTD
摘要:Novel compound of the formula: ##STR1## wherein R 1 is pyridyl group, R 2 is a phenyl group, a thienyl group, a furyl group, a naphthyl group, a benzothienyl group or pyridyl group, which may optionally have a lower alkoxy group, a lower alkyl group, a halogen atom, trifluoromethyl group, a lower alkenyl group or methylenedioxy group, R 3 is hydrogen atom or a lower alkyl group, and n is an integer of 0 to 6, Y is sulphur atom, methylene group or a group of the formula: ##STR2## wherein R 4 is hydrogen atom or acetyl group, and m is 0 or 1, and their pharmaceutically acceptable salts having an inhibitory action on bio-synthesis of thromboxane A 2 (TXA 2 ) and an effect of accelerating the productivility of prostaglandin I 2 (PGI 2 ), and can be used for mammals to the prophylaxis or therapy of thrombosis caused by platelet aggregation or ischemic diseases caused by vasospasms in cardiac, cerebral and peripheral circulatory system (e.g. cardiac infarction, apoplexy, infarct of blood vessels in kidney, lung and other organs, pectic ulcer, etc.).

专利号:US-4518602-A
优先权日:1982-10-07
标题 :Vinyl carboxylic acid derivatives, their production and use as inhibitors of thromboxane synthetase
发明人：TERAO SHINJI; NISHIKAWA KOHEI
权利人:TAKEDA CHEMICAL INDUSTRIES LTD
摘要:Novel compound of the formula: wherein R1 is a pyridyl group; R2 is a phenyl, thienyl, furyl, naphthyl, benzothienyl or pyridyl group which may have as a substituent a lower alkoxy, a lower alkyl, a halogen, trifluoromethyl, a lower alkenyl or methylenedioxy; R3 is hydrogen, benzyl or a lower alkyl; one of R4 and R5 is hydrogen or a lower alkyl, and the other is an aryloxy, or lower aliphatic hydrocarbon, an alicyclic hydrocarbon having not more than 6 carbon atoms or an aromatic group which may have a substituent, or a group represented by the formula, -S(O)m-R6 (in which R6 is phenyl or a lower alkyl group; m is an integer of 0 to 2), or R4 and R5 each combine with the other to represent one alkylene group; n is an integer of 2 to 6, or a pharmaceutically acceptable salt thereof has a selective inhibitory action on bio-synthesis of thromboxane A2(TXA2) and an effect of enhancing the production of prostaglandin I2(PGI2), and can be used in mammals for to prevention and treatment of arterial thrombosis caused by platelet aggregation or ischemic diseases caused by vasospasms in cardiac, cerebral and peripheral circulatory system (e.g. cardian infarction, apoplexy, infarct of blood vessels in kidney, lung and other organs, pectic ulcer, etc.).

专利号:US-4908380-A
优先权日:1986-11-04
标题:Pharmaceutical compositions
发明人：BREWSTER ANDREW G; BROWN GEORGE R; SMITHERS MICHAEL J
权利人:ICI PLC
摘要:The invention concerns novel pharmaceutical compositions containing a 4(Z)-6-(2,4-diphenyl-1,3-dioxan-5-yl)-alkenoic acid which antagonizes one or more of the actions of thromboxane A2, together with a compound which inhibits the synthesis of thromboxane A2. The compositios are useful as medicines in treating a variety of diseases or medical conditions in which thromboxane A2 and/or other prostanoid contractile substances are involved.

专利号:US-4925869-A
优先权日:1986-11-04
标题 :Therapeutic agents
发明人：SMITHERS MICHAEL J
权利人:ICI PLC
摘要:The invention concerns novel therapeutic agents containing a (Z)-(2-alkoxyalkyl- or 2-aryloxyalkyl-4-phenyl-1,3-dioxan-5-yl)alkenoic acid, or a related tetrazole derivative, which antagonizes one or more of the actions of thromboxane A2, together with a compound which inhibits the synthesis of thromboxane A2. The compositions are useful as medicines in treating a variety of diseases or medical conditions in which thromboxane A2 and/or other prostanoid contractile substances are involved.

专利号:JP-2004500344-A
优先权日:1999-10-29
标 题 :Synthesis of endogenous nitric oxide under low oxygen partial pressure