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1. 发明授权

US4466969A 7-Oxoprostacyclin derivatives and their use as hypotensives and bronchodilators 失效
标题翻译： 7-氧前列环素衍生物及其作为假药和支气管扩张剂的用途
公开(公告)号：US4466969A
公开(公告)日：1984-08-21
申请号：US385414
申请日：1982-05-17
申请人： Robert C. Nikolson , Helmut Vorbruggen , Jorge Casals-Stenzel , Gerda Mannesmann
发明人： Robert C. Nikolson , Helmut Vorbruggen , Jorge Casals-Stenzel , Gerda Mannesmann
IPC分类号： A61K31/34 , A61K31/557 , A61P43/00 , C07C17/08 , C07C21/14 , C07C57/03 , C07C57/13 , C07C57/52 , C07C69/593 , C07C69/606 , C07D307/935 , C07D307/937 , C07D407/12 , C07F9/40 , C07F9/48 , C07F9/535 , C07F9/54
CPC分类号： C07D307/935 , C07C17/08 , C07C57/03 , C07C57/13 , C07C57/52 , C07D307/937 , C07F9/4015 , C07F9/5352
摘要： Prostacyclin, although having a useful dilating effect on blood vessels, is not sufficiently stable to ensure successful use as a hypotensive agent.A 7-oxo prostacyclin derivative of the general formula ##STR1## in which R.sub.1 represents the radical OR.sub.3 whereinR.sub.3 represents hydrogen, a straight-chain or branched optionally substituted, (C.sub.1 -C.sub.10)alkyl, optionally substituted aryl, optionally substituted cycloalkyl, optionally substituted heterocyclic,orR.sub.1 represents the radical NHR.sub.4 whereinR.sub.4 represents hydrogen, or a group derived from an unsaturated or saturated, unsubstituted or substituted, (C.sub.1 -C.sub.15)organic carboxylic or sulphonic acid,A represents --CH.sub.2 --CH.sub.2 --, cis--CH.dbd.CH-- or trans--CH.dbd.CH--,W represents ##STR2## either having a free or functionally modified hydroxy group which may be in the .alpha.- or .beta.-position,D and E together represent a direct bond, orD represents a straight-chain or branched, unsaturated or saturated, optionally substituted (C.sub.1 -C.sub.10)alkylene, andE represents oxygen or a direct bond,R.sub.2 represents a straight-chain or branched optionally substituted, (C.sub.1 -C.sub.10)alkyl, a straight-chain or branched optionally substituted, (C.sub.2 -C.sub.10)alkenyl, or, where D and E together represent a direct bond, a straight-chain or branched optionally substituted (C.sub.2 -C.sub.6)alkynyl,andR.sub.5 represents a free or functionally modified hydroxy group,has proved to have not only a hypotensive and bronchodilative action, for example, but also an increased stability over prostacyclin. Advantages in medicinal use over other prostaglandins have also been found.
摘要翻译： PCT No.PCT / EP81 / 00148 Sec。 371日期1982年5月17日 102（e）日期1982年5月17日PCT提交1981年9月17日PCT公布。出版物WO82 / 01002 日期：1982年4月1日。前列环素尽管对血管具有有用的扩张作用，但不能保证成功地用作血压降低剂。（I）的7-氧代前列环素衍生物，其中R 1表示基团OR 3，其中R 3表示氢，直链或支链任选取代的（C 1 -C 10）烷基，任选取代的芳基，任选取代的环烷基，任选取代的杂环基，或R 1表示基团NHR 4，其中R 4表示氢，或衍生自不饱和或饱和，未取代或取代的（C1-C15）有机羧酸或磺酸的基团，A表示-CH2-CH2-，顺式-CH = CH-或反式-CH = CH-，W表示具有游离或功能改性的羟基，其可以是α或β位，D和E一起代表直接键，或 D表示直链或支链，不饱和或饱和的任选取代的（C 1 -C 10）亚烷基，E表示氧或直接键，R 2表示直链或支链任选取代的（C 1 -C 10）烷基，直链或支链取代的（C 2 -C 10）烯基，或其中D和E一起代表直接键，直链或支链任选取代的（C 2 -C 6）炔基，R 5表示游离或官能改性的羟基，不仅具有低血压和支气管扩张作用，而且比前列环素具有更高的稳定性。也发现药物使用优于其他前列腺素的优点。

2. 发明授权

US4191694A Prostaglandin-I.sub.2 derivatives 失效
标题翻译：前列腺素I2衍生物
公开(公告)号：US4191694A
公开(公告)日：1980-03-04
申请号：US928126
申请日：1978-07-26
申请人： Werner Skuballa , Bernd Raduchel , Norbert Schwarz , Helmut Vorbruggen , Bernd Muller , Gerda Mannesmann , Olaf Loge , Ekkehardt Schillinger , Jorge Casals-Stenzel
发明人： Werner Skuballa , Bernd Raduchel , Norbert Schwarz , Helmut Vorbruggen , Bernd Muller , Gerda Mannesmann , Olaf Loge , Ekkehardt Schillinger , Jorge Casals-Stenzel
IPC分类号： A61K31/557 , A61K31/34 , A61K31/343 , A61K31/5575 , A61P7/02 , A61P7/10 , A61P9/06 , A61P9/12 , A61P43/00 , C07C405/00 , C07D307/935 , C07D307/937 , C07D307/93
CPC分类号： C07D307/937 , C07C405/00 , Y10S514/821 , Y10S514/822 , Y10S514/869
摘要： Prostane derivatives of the formula ##STR1## wherein R.sub.1 is OR.sub.2 or NHR.sub.3 ;R.sub.2 is hydrogen, C.sub.1-10 alkyl, C.sub.4-10 cycloalkyl, C.sub.6-10 aryl, or a 5 or 6 membered heterocyclic ring having 1-3 hetero atoms selected from O, N and S;R.sub.3 is the residue of a hydrocarbon carboxylic or sulfonic acid of 1-15 carbon atoms;W is (a) an OH-substituted methylene group, (b) a ##STR2## wherein the OH-groups in (a) or (b) can be in the .alpha.- or .beta.-position, or (c) such a group wherein the H atom of the OH group is replaced by the residue of a hydrocarbon carboxylic or sulfonic acid of 1-15 carbon atoms or by a conventional etherifying OH-blocking group;R.sub.4 is OH or hydroxy whose H atom is replaced as defined for W; andR.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10 and R.sub.11 each independently is hydrogen or alkyl of 1-5 carbon atoms; or R.sub.9 and R.sub.10 together represent a direct bond; and, when R.sub.11 is alkyl, R.sub.10 can also be chlorine;and, for a derivative wherein R.sub.2 is hydrogen, the salts thereof with physiologically compatible bases,have improved prostaglandin activity.
摘要翻译：其中R1为OR2或NHR3的式（Ⅰ）所示的前驱体衍生物; R2是氢，C1-10烷基，C4-10环烷基，C6-10芳基或具有1-3个选自O，N和S的杂原子的5或6元杂环; R3是1-15个碳原子的烃羧酸或磺酸的残基; W是（a）OH-取代的亚甲基，（b）其中（a）或（b）中的OH基可以是α或β-位，或（c）这样的基团其中OH基团的H原子被1-15个碳原子的烃羧酸或磺酸的残基或通过常规的醚化OH-封闭基团取代; R4是OH或羟基，其H原子被替换为W定义; R 5，R 6，R 7，R 8，R 9，R 10和R 11各自独立地为氢或1-5个碳原子的烷基; 或R 9和R 10一起代表直接键; 当R 11为烷基时，R 10也可为氯; 并且对于其中R 2是氢的衍生物，其与生理上相容的碱的盐具有改善的前列腺素活性。

3. 发明授权

US4708963A Novel carbacyclins, their preparation and use 失效
标题翻译：新型碳霉素，其制备和用途
公开(公告)号：US4708963A
公开(公告)日：1987-11-24
申请号：US738545
申请日：1985-05-28
申请人： Werner Skuballa , Bernd Raduchel , Norbert Schwarz , Helmut Vorbruggen , Jorge Casals-Stenzel , Ekkehard Schillinger , Michael H. Town
发明人： Werner Skuballa , Bernd Raduchel , Norbert Schwarz , Helmut Vorbruggen , Jorge Casals-Stenzel , Ekkehard Schillinger , Michael H. Town
IPC分类号： C07C69/708 , A61K31/16 , A61K31/19 , A61K31/20 , A61K31/23 , A61K31/557 , A61P1/04 , A61P7/02 , A61P9/00 , A61P9/12 , A61P11/08 , C07C51/00 , C07C51/367 , C07C59/125 , C07C67/00 , C07C231/00 , C07C231/02 , C07C235/06 , C07C235/88 , C07C301/00 , C07C303/40 , C07C311/51 , C07C405/00 , C07D309/12 , C07D317/72 , C07F9/40 , C07C177/00
CPC分类号： C07D317/72 , C07C405/0083 , C07D309/12 , C07F9/4015 , Y10S514/927
摘要： Carbacyclin derivatives of Formula I ##STR1## wherein R.sub.1 is OR.sub.2, wherein R.sub.2 is hydrogen, alkyl, cycloalkyl, aryl, a heterocyclic residue, or NHR.sub.3, wherein R.sub.3 is an acid residue or hydrogen;X is oxygen;A is --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH--, or --C.tbd.C--;W is free or functionally modified hydroxymethylene or free or functionally modified ##STR2## wherein the OH-group can be in the .alpha.- or .beta.-position; D is a straight-chain or branched, saturated or unsaturated aliphatic group of 1-10 carbon atoms, which can optionally be substituted by fluorine atoms, 1,2-methylene, 1,1-trimethylene;E is --C.tbd.C-- or --CR.sub.6 .dbd.CH.sub.7 -- wherein R.sub.6 and R.sub.7 are hydrogen or alkyl of 1-5 carbon atoms;R.sub.4 is an aliphatic group, cycloalkyl, optionally substituted aryl, or a heterocyclic group;R.sub.5 is free or functionally modified hydroxy and,when R.sub.2 is hydrogen, the physiologically compatible salts thereof with bases, have valuable pharmacological properties.
摘要翻译：式I的卡巴环素衍生物其中R 1是OR 2，其中R 2是氢，烷基，环烷基，芳基，杂环残基或NHR 3，其中R 3是酸残基或氢; X是氧; A是-CH 2 -CH 2 - ，反式-CH = CH-或-C 3位C; W是游离的或官能改性的羟基亚甲基或游离或功能改性的“IMAGE”，其中OH-基团可以是α-或β-位; D是1-10个碳原子的直链或支链，饱和或不饱和的脂族基团，其可任选被氟原子取代，1,2-亚甲基，1,1-三亚甲基; E是-C 3 C或-CR 6 = CH 7 - ，其中R 6和R 7是氢或1-5个碳原子的烷基; R4是脂族基团，环烷基，任选取代的芳基或杂环基; R5是游离的或官能改性的羟基，当R2是氢时，其与碱的生理上相容的盐具有有价值的药理学性质。

4. 发明授权

US4423067A Carbacyclins, their preparation and use 失效
标题翻译：卡巴菌素，其制备和用途
公开(公告)号：US4423067A
公开(公告)日：1983-12-27
申请号：US333099
申请日：1981-12-21
申请人： Werner Skuballa , Bernd Raduchel , Norbert Schwarz , Helmut Vorbruggen , Jorge Casals-Stenzel , Ekkehard Schillinger , Michael H. Town
发明人： Werner Skuballa , Bernd Raduchel , Norbert Schwarz , Helmut Vorbruggen , Jorge Casals-Stenzel , Ekkehard Schillinger , Michael H. Town
IPC分类号： C07C69/708 , A61K31/16 , A61K31/19 , A61K31/20 , A61K31/23 , A61K31/557 , A61P1/04 , A61P7/02 , A61P9/00 , A61P9/12 , A61P11/08 , C07C51/00 , C07C51/367 , C07C59/125 , C07C67/00 , C07C231/00 , C07C231/02 , C07C235/06 , C07C235/88 , C07C301/00 , C07C303/40 , C07C311/51 , C07C405/00 , C07D309/12 , C07D317/72 , C07F9/40 , C07C177/00
CPC分类号： C07D317/72 , C07C405/0083 , C07D309/12 , C07F9/4015 , Y10S514/927
摘要： Carbacyclin derivatives of Formula I ##STR1## wherein R.sub.1 is OR.sub.2, wherein R.sub.2 is hydrogen, alkyl, cycloalkyl, aryl, a heterocyclic residue, or NHR.sub.3, wherein R.sub.3 is an acid residue or hydrogen;X is oxygen;A is --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH--, or --C.tbd.C--;W is free or functionally modified hydroxymethylene or free or functionally modified ##STR2## wherein the OH-group can be in the .alpha.- or .beta.-position; D is a straight-chain or branched, saturated or unsaturated aliphatic group of 1-10 carbon atoms, which can optionally be substituted by fluorine atoms, 1,2-methylene, 1,1-trimethylene;E is --C.tbd.C-- or --CR.sub.6 .dbd.CR.sub.7 -- wherein R.sub.6 and R.sub.7 are hydrogen or alkyl of 1-5 carbon atoms;R.sub.4 is an aliphatic group, cycloalkyl, optionally substituted aryl, or a heterocyclic group;R.sub.5 is free or functionally modified hydroxy and,when R.sub.2 is hydrogen, the physiologically compatible salts thereof with bases, have valuable pharmacological properties.
摘要翻译：式I的卡巴环素衍生物其中R 1是OR 2，其中R 2是氢，烷基，环烷基，芳基，杂环残基或NHR 3，其中R 3是酸残基或氢; X是氧; A是-CH 2 -CH 2 - ，反式-CH = CH-或-C 3位C; W是游离的或官能改性的羟基亚甲基或游离或功能改性的“IMAGE”，其中OH-基团可以是α-或β-位; D是1-10个碳原子的直链或支链，饱和或不饱和的脂族基团，其可任选被氟原子取代，1,2-亚甲基，1,1-三亚甲基; E是-C 3 C或-CR 6 = CR 7 - ，其中R 6和R 7是氢或1-5个碳原子的烷基; R4是脂族基团，环烷基，任选取代的芳基或杂环基; R5是游离的或官能改性的羟基，当R2是氢时，其与碱的生理上相容的盐具有有价值的药理学性质。

5. 发明授权

US4364950A 5-Cyano-prostacyclin derivatives and use as medicines 失效
标题翻译： 5-Cyano-prostacyclin衍生物用作药物
公开(公告)号：US4364950A
公开(公告)日：1982-12-21
申请号：US317621
申请日：1981-11-02
申请人： Werner Skuballa , Helmut Vorbruggen , Bernd Raduchel , Jorge Casals-Stenzel , Ekkehard Schillinger , Michael H. Town
发明人： Werner Skuballa , Helmut Vorbruggen , Bernd Raduchel , Jorge Casals-Stenzel , Ekkehard Schillinger , Michael H. Town
IPC分类号： A61K31/557 , A61P7/02 , A61P9/12 , A61P11/08 , A61P43/00 , C07D307/935 , C07D307/937 , C07F7/18 , C07F9/40
CPC分类号： C07D307/935 , C07D307/937 , C07F7/1856 , C07F9/4015
摘要： 5-cyano-prostacyclins of the formula ##STR1## wherein R.sub.1 is OR.sub.2 or NHR.sub.3 ; R.sub.2 and R.sub.3 each independently is (a) H, (b) C.sub.1-10 -alkyl, (c) C.sub.1-10 -alkyl substituted by halo, C.sub.1-4 -alkoxy or phenyl, 1-naphthyl or 2-naphthyl, each optionally substituted as defined below, (d) C.sub.4-10 -cycloalkyl, (e) C.sub.4-10 -cycloalkyl substituted by C.sub.1-4 -alkyl, (f) phenyl, 1-naphthyl or 2-naphthyl, (g) phenyl, 1-naphthyl or 2-naphthyl substituted by 1-3 halogen atoms, phenyl, 1-3 alkyl groups of 1-4 C atoms each, or a chloromethyl-, fluoromethyl-, trifluoromethyl-, carboxyl-, hydroxy- or alkoxy-group of 1-4 C atoms, or (h) an aromatic, 5- or 6-membered heterocyclic ring containing one hetero atom which is O, N or S, the remaining atoms being carbon; R.sub.3 also possibly being an acyl group of a C.sub.1-15 -hydrocarbon carboxylic or sulfonic acid;B is straight chain or branched alkylene of 2-10 C atoms;W is hydroxymethylene or ##STR2## wherein the OH group may be in the alpha or beta position, and is optionally modified by replacement of the H atom of the OH with an ether or acyl group which is conventional for such replacements in prostaglandins and which is readily cleavable at physiological pH's;R.sub.4 is hydroxy, optionally modified as described for W above;R.sub.5, R.sub.6, R.sub.7 and R.sub.8 each independently is hydrogen, alkyl of 1-5 C atoms or methoxy; andR.sub.9 is alkyl of 1-5 C atoms orfor compounds wherein R.sub.2 is H, the salts thereof with physiologically compatible bases have valuable pharmacalogical properties, e.g., hypertonic and bronchodilatory activities.
摘要翻译：其中R1是OR2或NHR3的式“IMAGE”的5-氰基 - 前列环素; R 2和R 3各自独立地为（a）H，（b）C 1-10 - 烷基，（c）被卤素，C 1-4 - 烷氧基或苯基，1-萘基或2-萘基取代的C 1-10 - 烷基，（d）C 4-10 - 环烷基，（e）被C 1-4 - 烷基取代的C 4-10 - 环烷基，（f）苯基，1-萘基或2-萘基，（g）苯基，萘基或被1-3个卤素原子取代的2-萘基，苯基，1-4个C原子的1-3个烷基，或1个氯甲基 - ，氟甲基 - ，三氟甲基 - ，羧基 - ，羟基或烷氧基 -4个C原子，或（h）含有一个杂原子的芳族的5或6元杂环，它是O，N或S，其余的原子是碳; R3也可能是C1-15-烃羧酸或磺酸的酰基; B是2-10个C原子的直链或支链亚烷基; W是羟基亚甲基或其中OH基团可以在α或β位置，并且任选地通过用在前列腺素中这种替代物常规的醚或酰基取代OH的H原子来任意修饰，并且其是在生理pH值下易于切割; R4是羟基，任选地按照上述W所述进行改性; R5，R6，R7和R8各自独立地为氢，1-5个C原子的烷基或甲氧基; 并且R 9为1-5个C原子的烷基，或对于其中R 2为H的化合物，其与生理上相容的碱的盐具有有价值的药理学性质，例如高渗和支气管扩张活性。

6. 发明授权

US4692464A Novel prostacyclin derivatives and a process for the preparation thereof 失效
公开(公告)号：US4692464A
公开(公告)日：1987-09-08
申请号：US352411
申请日：1982-02-26
申请人： Werner Skuballa , Bernd Raduchel , Helmut Vorbruggen , Gerda Mannesmann , Wolfgang Losert , Jorge Casals
发明人： Werner Skuballa , Bernd Raduchel , Helmut Vorbruggen , Gerda Mannesmann , Wolfgang Losert , Jorge Casals
IPC分类号： C07D309/12 , A61K31/557 , A61K31/5575 , A61K31/5585 , A61P7/02 , A61P25/02 , A61P43/00 , C07C45/59 , C07C45/67 , C07C45/71 , C07C51/00 , C07C51/353 , C07C59/46 , C07C62/32 , C07C67/00 , C07C67/343 , C07C69/732 , C07C401/00 , C07C405/00 , C07D317/72 , C07D319/12 , C07C177/00
CPC分类号： C07D317/72 , A61K31/557 , C07C405/0083 , C07C45/59 , C07C45/673 , C07C45/71 , C07C62/32 , C07D319/12
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is (a) hydrogen, (b) C.sub.1-10 alkyl, (c) C.sub.1-10 alkyl substituted by halogen; C.sub.1-4 alkoxy; C.sub.6-10 aryl; C.sub.6-10 aryl substituted by 1-3 halogen atoms, a phenyl group, 1-3 C.sub.1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C.sub.1-4 alkoxy group; di-C.sub.1-4 -alkylamino; or tri-C.sub.1-4 -alkylammonium, (d) C.sub.4-10 cycloalkyl, (e) C.sub.4-10 cycloalkyl substituted by C.sub.1-4 alkyl, (f) C.sub.6-10 aryl, (g) C.sub.6-10 aryl substituted by 1-3 halogen atoms, a phenyl group 1-3 C.sub.1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C.sub.1-4 alkoxy group, or (h) an aromatic heterocycle of 5 or 6 ring atoms one of which is O, N or S;A is --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH-- or --C.tbd.C--;W is hydroxymethylene, RO-methylene, CH.sub.3 or CH.sub.3, ##STR2## wherein OH or OR is in the .alpha.- or .beta.-position and R is an in vivo hydrolyzable and physiologically acceptable ether or acyl group which is conventional for modifying OH groups in prostaglandins;D and E together are a direct bond, orD is C.sub.1-10 alkylene, C.sub.1-10 alkenylene or C.sub.1-10 alkynylene or one of these groups substituted by fluorine, andE is oxygen, --C.tbd.C-- or a direct bond;R.sub.2 is (a) a C.sub.1-10 hydrocarbon aliphatic radical, (b) a C.sub.6-10 hydrocarbon aliphatic radical substituted by C.sub.6-10 aryl or by C.sub.6-10 aryl substituted by 1-3 halogen atoms, a phenyl group, 1-3 C.sub.1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C.sub.1-4 alkoxy group; (c) C.sub.4-10 cycloalkyl, (d) C.sub.4-10 cycloalkyl substituted by C.sub.1-4 alkyl, (e) C.sub.6-10 aryl, (f) C.sub.6-10 aryl substituted by 1-3 halogen atoms, a phenyl group, 1-3 C.sub.1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C.sub.1-4 alkoxy group; or (h) an aromatic heterocycle of 5 or 6 ring atoms one of which is O, N or S; andR.sub.3 is OH or OR; and, when R.sub.1 is hydrogen, the salts thereof with physiologically compatible bases, are effective as antihypertensive, bronchiodilators, thrombocyte aggregation inhibitors, inter alia.

7. 发明授权

US4219479A 5-Cyano-prostacyclin derivatives 失效
标题翻译： 5-氰基前列环素衍生物
公开(公告)号：US4219479A
公开(公告)日：1980-08-26
申请号：US963240
申请日：1978-11-24
申请人： Helmut Vorbruggen , Werner Skuballa , Bernd Raduchel , Wolfgang Losert , Olaf Loge , Bernd Muller , Gerda Mannesmann
发明人： Helmut Vorbruggen , Werner Skuballa , Bernd Raduchel , Wolfgang Losert , Olaf Loge , Bernd Muller , Gerda Mannesmann
IPC分类号： A61K31/557 , A61K31/34 , A61K31/343 , A61K31/5575 , A61P1/04 , A61P7/02 , A61P9/12 , A61P11/00 , C07C405/00 , C07D307/935 , C07D307/937 , A61K31/335 , C07D307/93
CPC分类号： C07D307/937
摘要： Stabilized prostacyclins having a wide range of pharmacological activity and long duration of such activity, have the formula ##STR1## wherein R.sub.1 is (a) OR.sub.3, wherein R.sub.3 is hydrogen, alkyl, cycloalkyl, aryl or a heterocyclic residue; or (b) NHR.sub.4 wherein R.sub.4 is an acid residue;B is straight-chain or branched alkylene of 2-10 carbon atoms;A is --CH.sub.2 --CH.sub.2 --, cis--CH.dbd.CH--, trans--CH.dbd.CH-- or --C.tbd.C--,W is free or functionally modified hydroxymethylene or free or functionally modified ##STR2## wherein the OH-group can be in the .alpha.- or .beta.-position; D and E together are a direct bond; orD is straight-chain or branched alkylene of 1-5 carbon atoms; andE is oxygen or sulfur or a direct bond,R.sub.2 is alkyl, cycloalkyl, optionally substituted aryl or a heterocyclic group; andR.sub.5 is free or functionally modified hydroxy; and when R.sub.3 is hydrogen, the salts thereof with physiologically compatible bases.
摘要翻译：具有广泛的药理活性和长时间的这种活性的稳定的前列环素具有下式（IMAGE），其中R1是（a）OR3，其中R3是氢，烷基，环烷基，芳基或杂环残基; 或（b）NHR 4，其中R 4是酸残基; B是2-10个碳原子的直链或支链亚烷基; A是-CH 2 -CH 2 - ，顺式-CH = CH-，反式-CH = CH-或-C 3BOND C-，W是游离或官能改性的羟基亚甲基或游离或官能改性的，其中OH-基团可以是在alpha或beta位置; D和E一起是直接的债券; 或D是1-5个碳原子的直链或支链亚烷基; 并且E是氧或硫或直接键，R 2是烷基，环烷基，任选取代的芳基或杂环基; R5是游离或官能改性的羟基; 并且当R3是氢时，其盐与生理上相容的碱基。

8. 发明授权

US5750676A Process for preparing nucleosides with unprotected sugars 失效
标题翻译：用未保护的糖制备核苷的方法
公开(公告)号：US5750676A
公开(公告)日：1998-05-12
申请号：US817802
申请日：1997-04-04
申请人： Helmut Vorbruggen , Konrad Krolikiewicz , Barbel Bennua-Skalmowski
发明人： Helmut Vorbruggen , Konrad Krolikiewicz , Barbel Bennua-Skalmowski
IPC分类号： C07H19/02 , C07H19/056 , C07H1/00 , C07H1/06 , C07H19/067 , C07H19/167
CPC分类号： C07H19/056
摘要： A novel process for nucleoside synthesis, which process comprises reacting the free sugar with heterocyclic bases in the presence of silylating agents in an inert solvent containing a Lewis acid.
摘要翻译： PCT No.PCT / EP96 / 01472 Sec。 371日期1997年04月4日 102（e）日期1997年4月4日PCT提交1996年4月3日PCT公布。出版物WO96 / 31520 PCT 日期1996年10月10日一种用于核苷合成的新方法，该方法包括在甲硅烷基化剂存在下，在含有路易斯酸的惰性溶剂中使游离糖与杂环碱反应。

9. 发明授权

US5716989A Bicyclo�3.3.0!octane derivatives, process for their production and their pharmaceutical use 失效
标题翻译：双环[3.3.0]辛烷衍生物，其生产工艺及其药物用途
公开(公告)号：US5716989A
公开(公告)日：1998-02-10
申请号：US777363
申请日：1991-11-27
申请人： Ulrich Klar , Hartmut Rehwinkel , Helmut Vorbruggen , Karl Heinz Thierauch , Peter Verhallen
发明人： Ulrich Klar , Hartmut Rehwinkel , Helmut Vorbruggen , Karl Heinz Thierauch , Peter Verhallen
IPC分类号： A61K31/335 , A61K31/357 , A61K31/41 , A61K31/42 , A61K31/421 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/47 , A61K31/557 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/08 , C07C251/42 , C07C281/10 , C07C311/49 , C07C335/40 , C07C405/00 , C07D257/04 , C07D263/10 , C07D263/14 , C07D263/16 , C07D263/22 , C07D319/06 , C07D401/12 , C07D405/12 , C07D413/12 , C07D493/08 , A61K31/21
CPC分类号： C07C405/0083
摘要： The invention relates to bicyclo�3.3.0!octane compounds of formula I, ##STR1## wherein the variable are defined in this specification, as well as their enantiomers, and their salts with physiologically compatible bases. .alpha.-, .beta.-, or .tau.-Cyclodextrin clathrates of the compounds and the compounds encapsulated with liposomes are also included. The invention is further directed to processes for production of the compounds and their pharmaceutical use.
摘要翻译：本发明涉及式I的双环[3.3.0]辛烷化合物，其中变体在本说明书中定义，以及它们的对映体及其与生理上相容的碱基的盐。也包括化合物和用脂质体包封的化合物的α-，β-或τ-环糊精包合物。本发明进一步涉及化合物的制备方法及其药物用途。

10. 发明授权

US4631276A Prostaglandins and prostacyclins, process for their preparation and their use as medicaments 失效
标题翻译：前列腺素和前列腺素，其制备过程及其用作药物
公开(公告)号：US4631276A
公开(公告)日：1986-12-23
申请号：US627572
申请日：1984-07-03
申请人： Helmut Vorbruggen , Walter Elger , Michael-Harold Town , Ekkehard Schillinger
发明人： Helmut Vorbruggen , Walter Elger , Michael-Harold Town , Ekkehard Schillinger
IPC分类号： C07C405/00 , C07D263/14 , C07D277/10 , C07D417/12 , C07F7/18 , C07D233/14 , A61K31/42
CPC分类号： C07D417/12 , C07C405/0041 , C07D263/14 , C07D277/10 , C07F7/1856
摘要： Compounds of Formula I ##STR1## wherein R.sub.1 is a prostaglandin or prostacyclin residue;Y is oxygen, sulfur, imino, or N-(C.sub.1 -C.sub.4 -alkyl) imino;Q is (CR.sub.6 R.sub.7).sub.p wherein p is an integer of 0 to 3;R.sub.2 is hydrogen; alkyl of 1-6 carbon atoms optionally substituted by hydroxy or amino; C.sub.1 -C.sub.4 -alkoxycarbonyl; benzyloxycarbonyl; cyano; or di-C.sub.1 -C.sub.4 -alkylamino-carbonyl;R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 each independently is hydrogen; alkyl of 1-6 carbon atoms optionally substituted by hydroxy or amino; or aryl; andR.sub.3 and R.sub.4 together form a trimethylene, tetramethylene, or 1,3-butadienylene group when R.sub.2 and R.sub.5 together represent a direct bond;have valuable pharmacological properties, e.g., as blood-pressure-lowering or abortive agents.
摘要翻译：式I的化合物其中R 1是前列腺素或前列环素残基; Y是氧，硫，亚氨基或N-（C 1 -C 4 - 烷基）亚氨基; Q是（CR 6 R 7）p，其中p是0至3的整数; R2是氢; 任选被羟基或氨基取代的1-6个碳原子的烷基; C 1 -C 4烷氧基羰基; 苄氧羰基氰基; 或二-C 1 -C 4烷基氨基 - 羰基; R3，R4，R5，R6和R7各自独立地为氢; 任选被羟基或氨基取代的1-6个碳原子的烷基; 或芳基; 当R 2和R 5一起代表直接键时，R 3和R 4一起形成三亚甲基，四亚甲基或1,3-丁二烯基; 具有有价值的药理学性质，例如作为降血压药或降血糖药。

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