CAS: 14152-28-4; Prostaglandin A1

上下游产品

rac-(15S)-11β,15-dihydroxy-9-oxo-prost-13t-en-1-oic acidrac-(15S)-11β,15-dihydroxy-9-oxo-prost-13t-en-1-oic acid rac-(15R)-11β,15-dihydroxy-9-oxo-prost-13t-en-1-oic acidrac-(15R)-11β,15-dihydroxy-9-oxo-prost-13t-en-1-oic acid(1)-p-phenylbenzylesterProstaglandin A(1)-p-phenylbenzylester 7-[(1R,2S)-2-((E)-(S)-3-Hydroxy-°Ct-1-enyl)-5-oxo-cyclopent-3-enyl]-heptanoic acid biphenyl-4-yloxycarbonylmethyl ester (1)-p-bromphenacylesterProstaglandin A(1)-p-bromphenacylester

📜前列地尔置于14-Phenyl-11α,15R-Dihydroxy-9-Oxoprost-10,13E-Dien-1-Oic,乙醚,甲苯,苯乙醇体系中,用 Acetic Acid Monohydrate 用作溶剂,化学反应 48.0H,以to Yield 102 Mg Of The Pga1 Analogue的收率获得前列腺素 A1
参考文献:C.Sub.14 Phenyl-Substituted Derivatives Of Prostaglandin Analogues
标题:C.Sub.14 Phenyl-Substituted Derivatives Of Prostaglandin Analogues
摘要:本发明揭示了连接到c.Sub.14碳原子上的苯基基团的前列腺素a,E和f的类似物.还揭示了制备类似物和起始材料的方法.化合物的结构式为:##str1## 其中j是亚甲基,R或s-羟甲基或亚甲基;L是亚甲基或亚甲基,当j为亚甲基时,L只能是亚甲基;M是羰基,R或s-羟甲基;Q是乙烯基,Z-乙烯基或间苯基;T是具有2到3个碳原子的低碳基的烷氧基羰基,或羧基;B是1到5个碳原子的低碳基.本发明的前列腺素类似物表现出药理活性的分离.类似物可用于血小板聚集(methyl 14-Phenyl-11.Alpha.,15S-Dihydroxy-9-Oxoprost-13E-En-1-Oate可用于拮抗平滑肌刺激),而不会伴随着天然前列腺素的不良副作用,例如潮红,头痛,腹部痉挛和恶心.

专利信息

专利号:US-3992439-A
优先权日:1972-04-17
标 题:Synthesis of prostaglandins of the 'one'-series
发明人：SCHAAF THOMAS K; COREY ELIAS J
权利人:PFIZER
摘要:In the synthesis of prostaglandins of the 'one' -series an alteration in the conventional reaction sequence avoids side reactions and provides an improved synthesis via a series of novel intermediates. In this improved synthesis the side chain at the 8 position is attached to the five membered ring before the side chain at the 12 position is attached.

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-5905091-A
优先权日:1996-07-03
标 题 :Enhancement of skin pigmentation by prostaglandins
发明人：FULLER BRYAN B
权利人:UNIV OKLAHOMA
摘要:A composition comprising a carrier and prostaglandin effective in stimulating synthesis of melanin in a human melanocyte thereby enhancing pigmentation of the human skin and optionally comprising a lysosomotropic agent, a phosphodiesterase inhibitor, and/or methylxanthines, and a method of use of the composition. Use of this composition promotes tanning of the human skin and increases photoprotection from ultraviolet radiation.

专利号:US-4331688-A
优先权日:1978-02-23
标题 :Therapeutic method for inhibiting gastric secretion by administration of 15-deoxy-16-hydroxy prostaglandins
发明人：KLUENDER HAROLD C; WOESSNER WARREN D; BIDDLECOM WILLIAM G
权利人:MILES LAB
摘要:Analogues of PGE 1 having the structural formula, ##STR1## in which J is R-hydroxymethylene or S-hydroxymethylene; R 1 is hydrogen; R 2 is hydrogen or together with R 4 is a methylene chain of 2 to 3 carbon atoms such that a cycloalkyl of 5 to 6 carbon atoms inclusive is formed; R 3 is hydrogen or methyl, or together with R 4 is a methylene or a lower alkylated methylene chain of 2 to 5 carbon atoms such that a cycloalkyl or a lower alkylated cycloalkyl of 4 to 7 carbon atoms inclusive is formed, or together with R 4 is bicycloalkyl or bicycloalkenyl moiety having the formula: ##STR2## such that a bicycloalkyl or bicycloalkenyl compound is formed, wherein m and n are integers having a value from 0 to 3, p is an integer having a value from 0 to 4 and q is an integer having a value of from 1 to 4 and wherein the double bond of such bicycloalkenyl is in the m, n, p, or q bridge; R 4 is hydrogen or methyl or together with R 2 or R 3 forms a cycloalkyl or bicycloalkyl or bicycloalkenyl as defined above, or together with R 5 is a methylene chain of 3 to 5 carbon atoms such that a cycloalkyl of 4 to 6 carbon atoms inclusive is formed; R 5 is selected from the group consisting of hydrogen, straight-chain alkyl having from 1 to 3 carbon atoms or together with R 4 forms a cycloalkyl as defined above; and R 6 is hydrogen or straight-chain alkyl having from 1 to 3 carbon atoms are disclosed. n PGE 1 ester analogues of the above formula, limited to the structures wherein two of R 2 , R 3 R 4 and R 5 form a cycloalkyl, lower alkylated cycloalkyl, bicycloalkyl or bicycloalkenyl are also disclosed. n The prostaglandin analogues selectively produce bronchodilation and decrease gastric secretion in vivo. n Methods of preparing the analogues and starting materials required in the synthesis of the analogues are also disclosed.

专利号:US-7772278-B2
优先权日:1999-03-01
标 题:Nitrosated and nitrosylated prostaglandins, compositions and methods of use
发明人：GARVEY DAVID S; GASTON RICKY D; LETTS L GORDON; DE TEJADA INIGO SAENZ; TAM SANG WILLIAM; WORCEL MANUEL
权利人:NITROMED INC
摘要:The invention describes novel nitrosated and/or nitrosylated prostaglandins, and novel compositions comprising at least one nitrosated and/or nitrosylated prostaglandin, 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 invention also provides novel compositions comprising at least one prostaglandin and at least one S-nitrosothiol compound, and, optionally, at least one vasoactive agent. The prostaglandin is preferably a prostaglandin E 1 compound, more preferably alprostadil, and the S-nitrosothiol compound is preferably S-nitrosoglutathione. The invention also provides methods for treating or preventing sexual dysfunctions in males and females, for enhancing sexual responses in males and females, and for treating or preventing cerebrovascular disorders, cardiovascular disorders, benign prostatic hyperplasia (BPH), glaucoma, peptic ulcers or for inducing abortions.

专利号:US-2004110228-A1
优先权日:2002-04-01
标 题:Combinatorial organic synthesis of unique biologically active compounds
发明人：MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M
摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.