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1. 发明授权

US4520207A Synthesis of thiophene-containing prostaglandin endoperoxide analogs 失效
标题翻译：含噻吩的前列腺素内过氧化物类似物的合成
公开(公告)号：US4520207A
公开(公告)日：1985-05-28
申请号：US423789
申请日：1982-09-27
申请人： Richard C. Larock
发明人： Richard C. Larock
IPC分类号： C07C405/00 , C07D333/24 , C07F1/02 , C07F3/14 , C07F15/00
CPC分类号： C07F3/14 , C07C405/0091 , C07D333/24 , C07F1/02 , C07F15/006
摘要： New organopalladium reactions involving the addition of thienylpalladium compounds to strained bicyclic alkenes, and subsequent chain extension reactions employing the chemistry of organopalladium compounds are disclosed. By these techniques a large number of bicyclic prostaglandin analogs are prepared, which are useful as inhibitors of arachidonic acid induced blood platelet aggregation, and are specific inhibitors of thromboxane synthetase.
摘要翻译：公开了涉及将噻吩基钯化合物加入到应变双环烯烃中的新的有机钯反应，以及使用有机钯化合物化学的随后的链延伸反应。通过这些技术，制备了大量的双环前列腺素类似物，其可用作花生四烯酸诱导的血小板聚集的抑制剂，并且是凝血恶烷合成酶的特异性抑制剂。

2. 发明授权

US4436934A Bicyclic prostaglandin analogs and method of synthesis 失效
标题翻译：双环前列腺素类似物和合成方法
公开(公告)号：US4436934A
公开(公告)日：1984-03-13
申请号：US334750
申请日：1981-12-28
申请人： Richard C. Larock
发明人： Richard C. Larock
IPC分类号： C07C405/00 , C07C177/00
CPC分类号： C07C405/0091
摘要： New organopalladium reactions involving the addition of pi-allylpalladium compounds to strained bicyclic alkenes, and subsequent chain extension reactions employing the chemistry of organopalladium compounds are disclosed. By these techniques a large number of bicyclic prostaglandin analogs are prepared, which are useful as inhibitors of arachidonic acid induced platelet aggregation, and are specific inhibitors of thromboxane synthetase.
摘要翻译：公开了涉及将π-烯丙基钯化合物加入到应变双环烯烃中的新的有机钯反应，以及使用有机钯化合物化学的随后的链延伸反应。通过这些技术，制备了大量的双环前列腺素类似物，其可用作花生四烯酸诱导的血小板聚集的抑制剂，并且是凝血恶烷合成酶的特异性抑制剂。

3. 发明授权

US4424374A Bicycloheptane derivatives 失效
标题翻译：双环庚烷衍生物
公开(公告)号：US4424374A
公开(公告)日：1984-01-03
申请号：US243567
申请日：1981-03-13
申请人： Michael P. L. Caton , Keith A. J. Stuttle
发明人： Michael P. L. Caton , Keith A. J. Stuttle
IPC分类号： C07C69/73 , A61K31/19 , A61K31/215 , A61P9/08 , A61P9/10 , A61P15/04 , A61P43/00 , C07C45/67 , C07C51/00 , C07C59/42 , C07C59/46 , C07C59/80 , C07C67/00 , C07C405/00 , C07D307/20 , C07D309/12 , C07C61/38
CPC分类号： C07D309/12 , C07C405/0091 , C07C45/67 , C07C45/673 , C07C59/46 , C07C59/80
摘要： Compounds of the general formula: ##STR1## wherein R.sup.1 represents a straight- or branched-chain alkyl group containing from 1 to 6 carbon atoms or a phenoxy or benzyl group, and pharmaceutically acceptable salts and esters thereof, possess pharmacological properties of use in the fields of mammalian reproduction and cardiovascular disease.
摘要翻译：通式为：其中R 1表示含有1至6个碳原子的直链或支链烷基或苯氧基或苄基的化合物及其药学上可接受的盐和酯，具有用于哺乳动物繁殖和心血管疾病的领域。

5. 发明授权

US4992581A Novel methods of manufacturing thromboxane A.sub.2 antagonists 失效
标题翻译：制备血栓素A2拮抗剂的新方法
公开(公告)号：US4992581A
公开(公告)日：1991-02-12
申请号：US283675
申请日：1988-12-13
申请人： Robert B. Garland , Masateru Miyano
发明人： Robert B. Garland , Masateru Miyano
IPC分类号： C07D311/94 , A61K31/19 , A61K31/557 , A61P7/02 , C07C1/207 , C07C1/32 , C07C13/61 , C07C49/447 , C07C59/46 , C07C59/80 , C07C337/08 , C07C405/00
CPC分类号： C07C337/08 , C07C405/0091 , C07C2102/42
摘要： This invention relates to several novel methods of manufacturing thromboxane A.sub.2 inhibiting 7-[3-.alpha.-[1-[[(phenylamino)-thioxomethyl]hydrazono]ethyl]-bicyclo[2.2.1]-heptenoic acids.

7. 发明授权

US4430345A Prostaglandins 失效
标题翻译：前列腺素
公开(公告)号：US4430345A
公开(公告)日：1984-02-07
申请号：US431554
申请日：1982-09-30
申请人： Robert L. Jones , Norman H. Wilson
发明人： Robert L. Jones , Norman H. Wilson
IPC分类号： B29C47/04 , A61K31/19 , A61K31/557 , A61P7/02 , A61P11/00 , B65D33/25 , C07C41/48 , C07C43/315 , C07C45/44 , C07C59/11 , C07C59/13 , C07C59/147 , C07C59/205 , C07C59/31 , C07C59/325 , C07C59/46 , C07C59/54 , C07C59/62 , C07C59/74 , C07C59/80 , C07C59/86 , C07C67/00 , C07C69/608 , C07C69/675 , C07C69/716 , C07C69/732 , C07C69/738 , C07C231/00 , C07C233/08 , C07C235/30 , C07C235/78 , C07C251/42 , C07C251/50 , C07C251/52 , C07C251/54 , C07C253/00 , C07C255/31 , C07C301/00 , C07C311/51 , C07C323/12 , C07C405/00 , C07D213/63 , C07D307/60 , C07D307/93 , C07C131/02 , C07C131/08
CPC分类号： C07C255/00 , C07C405/0091 , C07C41/48 , C07C43/315 , C07C45/44 , C07C59/13 , C07C59/147 , C07C59/31 , C07C59/325 , C07C59/46 , C07C59/54 , C07C59/62 , C07C59/74 , C07C59/80 , C07C59/86 , C07D307/60 , C07D307/93 , C07B2200/07 , C07C2102/42 , Y10S514/826
摘要： Novel bicyclo [2,2,1] heptanes and hept-2Z-enes are substituted at the 5-position by a 6-carboxyhex-2-enyl group or a modification thereof, and at the 6-position by an aldoxime or ketoxime group which is O-substituted by an aliphatic hydrocarbon residue, an aromatic residue, or an aliphatic hydrocarbon residue substituted directly or through an oxygen or sulphur atom by an aromatic residue. Such compounds may be prepared by the action of an oximating agent on an intermediate which is substituted at the 6-position by an aldehydic or ketonic carbonyl group. The compounds are of value for use in pharmaceutical compositions particularly in the context of the inhibition of thromboxane activity.

8. 发明授权

US4389413A 9,11-Methano-13-aza-11a-carbathrombanoic acid analogues 失效
公开(公告)号：US4389413A
公开(公告)日：1983-06-21
申请号：US285723
申请日：1981-07-22
申请人： Nobuyuki Hamanaka , Shinsuke Hashimoto , Masaki Hayashi
发明人： Nobuyuki Hamanaka , Shinsuke Hashimoto , Masaki Hayashi
IPC分类号： C07C33/14 , C07C405/00 , C07D309/12 , A61K31/557 , C07C101/14
CPC分类号： C07C33/14 , C07C405/0091 , C07D309/12 , Y10S514/826
摘要： The 9,11-methano-13-aza-11a-carbathrombanoic acid analogues of the general formula: ##STR1## [wherein A represents ##STR2## (in which m is an integer of 1 to 6, the double bond between the carbon atoms in positions 5 and 6 in (iv) is in cis or trans-configuration or a mixture thereof and the phenylene group in (iv) represents o-, m- or p-phenylene), R.sup.1 represents a hydrogen atom or a straight- or branched-chain alkyl group of 1 to 12 carbon atoms, two R.sup.2 both represent hydrogen atoms or methyl groups, R.sup.3 represents a hydrogen atom or a hydroxy group, R.sup.4 represents a single bond or a straight- or branched-chain alkylene group of 1 to 5 carbon atoms, R.sup.5 represents(i) a straight- or branched-chain alkyl, alkoxy or alkylthio group of 1 to 8 carbon atoms,(ii) a cycloalkyl or cycloalkyloxy group of 4 to 7 carbon atoms being unsubstituted or substituted by at least one straight- or branched-chain alkyl group of 1 to 8 carbon atoms or ##STR3## in which Z represents a single bond, an oxygen atom or a sulfur atom and R.sup.6 may occupy any of the free positions on the phenyl ring and represents a hydrogen atom, a halogen atom, a hydroxy group, a straight- or branched-chain alkyl or alkoxy group of 1 to 5 carbon atoms, a trihalomethyl group, an amino group or a mono- or dialkyl-amino group of 1 to 5 carbon atoms)and the wavy line attached to the carbon atom in position 15 represents .alpha.- or .beta.-configuration or a mixture thereof, provided that, when R.sup.3 represents a hydroxy group and R.sup.4 represents a single bond, R.sup.5 does not represent an alkoxy group, an alkylthio group, a cycloalkyloxy group, a phenoxy group and a phenylthio group],and cyclodextrin clathrates thereof, and when R.sup.1 represents a hydrogen atom, non-toxic salts thereof, possess strong inhibitory activities on platelet aggregation and on aorta contraction, and are useful for prevention and treatment of diseases which are induced by thromboxane A.sub.2.

9. 发明授权

US4260806A Carbocyclic thromboxane A.sub.2 analogues 失效
标题翻译：碳环血栓素A2类似物
公开(公告)号：US4260806A
公开(公告)日：1981-04-07
申请号：US087678
申请日：1979-10-24
申请人： Kyriacos C. Nicolaou , Ronald L. Magolda , David A. Claremon
发明人： Kyriacos C. Nicolaou , Ronald L. Magolda , David A. Claremon
IPC分类号： C07C29/62 , C07C45/51 , C07C45/54 , C07C45/67 , C07C45/68 , C07C59/46 , C07C405/00 , C07C57/26 , C07C103/19
CPC分类号： C07C405/0091 , C07C29/62 , C07C45/51 , C07C45/512 , C07C45/54 , C07C45/673 , C07C45/68 , C07C59/46 , C07C2102/40 , Y10S514/822 , Y10S514/93
摘要： Stable biologically active thromboxane A.sub.2 analogues having the formula: ##STR1## wherein R.sup.1 is OR.sup.3, where R.sup.3 represents hydrogen or a pharmaceutically acceptable cation or lower alkyl group; orR.sup.1 is NR.sup.4 R.sup.5 where R.sup.4 and R.sup.5 are the same or different substituents selected from the group consisting of hydrogen and lower alkyl group; andR.sup.2 is hydrogen or an --OH group.The thromboxane analogues are potent thrombotic agents, useful in cardiovascular treatment.
摘要翻译：具有下式的稳定的生物活性凝血恶烷A2类似物：其中R1是OR3，其中R3代表氢或药学上可接受的阳离子或低级烷基; 或R 1是NR 4 R 5，其中R 4和R 5是相同或不同的选自氢和低级烷基的取代基; R2为氢或-OH基。血栓素类似物是有效的血栓形成剂，可用于心血管治疗。

10. 发明授权

US5168101A Sulfonamide derivatives 失效
标题翻译：磺酰胺衍生物
公开(公告)号：US5168101A
公开(公告)日：1992-12-01
申请号：US257369
申请日：1988-10-13
申请人： Yoshinobu Arai , Nobuyuki Hamanaka , Tohru Miyazaki
发明人： Yoshinobu Arai , Nobuyuki Hamanaka , Tohru Miyazaki
IPC分类号： C07C311/20 , C07C405/00
CPC分类号： C07C405/0091 , C07C311/20 , C07C2101/08 , C07C2102/42
摘要： A sulfonamide derivative of the general formula:Tx--R.sup.1 (I)wherein, R.sup.1 represents(i) COOR.sup.11,(ii) CH.sub.2 OR.sup.12 or(iii) CONR.sup.13 R.sup.14,Tx--represents ##STR1## X.sub.b represents(i) bond,(ii) alkylene group of from 1 to 4 carbon atoms or(iii) alkenylene group of from 2 to 4 carbon atoms (with the proviso that --CH.dbd.CHCH.sub.2 -- and --CH.sub.2 CH.dbd.CHCH.sub.2 -- are excluded),R.sup.2b represents(i) hydrogen atom,(ii) halogen atom or(iii) alkyl group of from 1 to 4 carbon atom(s), posses an antagonistic activity on TXA.sub.2.

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