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    Novel prostacyclin derivatives and a process for the preparation thereof
    1.
    发明授权
    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.

    5-Cyano-prostacyclin derivatives
    2.
    发明授权
    5-Cyano-prostacyclin derivatives 失效
    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。

    Certain pyrrole analogs of prostacyclin derivatives
    3.
    发明授权
    Certain pyrrole analogs of prostacyclin derivatives 失效
    某些前列环素衍生物的吡咯类似物

    公开(公告)号：US4315013A

    公开(公告)日：1982-02-09

    申请号：US122794

    申请日：1980-02-19

    申请人： Werner Skuballa ,  Bernd Raduechel ,  Helmut Vorbrueggen ,  Gerda Mannesmann ,  Wolfgang Losert ,  Jorge Casals

    发明人： Werner Skuballa ,  Bernd Raduechel ,  Helmut Vorbrueggen ,  Gerda Mannesmann ,  Wolfgang Losert ,  Jorge Casals

    IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K31/557 ,  A61K31/5585 ,  A61P7/02 ,  A61P9/12 ,  A61P11/08 ,  A61P43/00 ,  C07C405/00 ,  C07D209/52 ,  A61K31/435 ,  C07D401/12 ,  C07D405/12

    CPC分类号： C07D209/52 ,  C07C405/00 ,  C07C405/0041

    摘要： Prostane derivatives 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;W is hydroxymethylene or RO-methylene; or ##STR2## wherein OH or OR is in the .alpha.-position and R is an in vivo hydrolyzable and physiologically acceptable ether or acyl group which is conventional for modifying OH groups in prostaglandins;R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are each independently hydrogen or alkyl of 1-5 carbon atoms,R.sub.2 is OH or OR, R being as defined above,or, when R.sub.1 is H, a physiologically compatible salt thereof with a base.

    摘要翻译： 其中R 1为（a）氢，（b）C 1-10烷基，（c）被卤素取代的C 1-10烷基; C 1-4烷氧基; C6-10芳基; 被1-3个卤素原子取代的C 6-10芳基，苯基，1-3个C 1-4烷基或氯甲基，氟甲基，三氟甲基，羧基，羟基或C 1-4烷氧基; 二-C 1-4 - 烷基氨基; 或三-C 1-4烷基铵; （d）C 4-10环烷基，（e）被C 1-4烷基取代的C 4-10环烷基，（f）C 6-10芳基，（g）被1-3个卤素原子取代的C 6-10芳基，苯基， -3 C 1-4烷基或氯甲基，氟甲基，三氟甲基，羧基，羟基或C 1-4烷氧基，或（h）5或6个环原子的芳族杂环，其中一个为O，N或S; W是羟基亚甲基或RO-亚甲基; 或其中OH或OR位于α位且R是体内可水解和生理上可接受的醚或酰基，其是常规用于改变前列腺素中的OH基团; R 3，R 4，R 5和R 6各自独立地是氢或1-5个碳原子的烷基，R 2是OH或OR，R如上定义，或者当R 1是H时，其与碱的生理上相容的盐。

    Crystalline prostanoic acid esters
    5.
    发明授权
    Crystalline prostanoic acid esters 失效
    结晶前列腺酸酯

    公开(公告)号：US4154953A

    公开(公告)日：1979-05-15

    申请号：US826908

    申请日：1977-08-19

    申请人： Werner Skuballa ,  Bernd Raduchel ,  Helmut Vorbruggen ,  Walter Elger ,  Olaf Loge ,  Wolfgang Losert

    发明人： Werner Skuballa ,  Bernd Raduchel ,  Helmut Vorbruggen ,  Walter Elger ,  Olaf Loge ,  Wolfgang Losert

    IPC分类号： C07C405/00 ,  C07C177/00

    CPC分类号： C07C405/00

    摘要： Prostanoic acid esters of the formulaPG-- CH.sub.2 -- X-- Ywherein PG is the prostanoyloxy radical of a prostaglandin, X is a carbon-carbon single bond, carbonyl or carbonyloxy, and Y is substituted phenyl are easily crystallized compounds at least as active as the unesterified prostanoic acid and useful for the purification of the parent prostaglandin are prepared by reacting, in the presence of an agent which splits off hydrogen halide, the unesterified prostaglandin with a halide of the formula Hal--CH.sub.2 --X--Y, wherein Hal is a halogen atom and X and Y have the values given above.

    摘要翻译： 式PG-CH2-X-Y的前列腺酸，其中PG是前列腺素的前烷氧基自由基，X是碳 - 碳单键，羰基或羰氧基，Y是取代的苯基，容易结晶化合物至少与 通过使未分解的前列腺素与式Hal-CH2-XY的卤化物反应，其中Hal是卤素，其中Hal是卤素 原子，X和Y具有上面给出的值。

    Novel prostanoic acid derivatives and process for the preparation thereof
    7.
    发明授权
    Novel prostanoic acid derivatives and process for the preparation thereof 失效
    新型前列腺酸衍生物及其制备方法

    公开(公告)号：US4004020A

    公开(公告)日：1977-01-18

    申请号：US534483

    申请日：1974-12-19

    申请人： Werner Skuballa ,  Bernd Raduchel ,  Helmut Vorbruggen ,  Walter Elger ,  Wolfgang Losert ,  Olaf Loge

    发明人： Werner Skuballa ,  Bernd Raduchel ,  Helmut Vorbruggen ,  Walter Elger ,  Wolfgang Losert ,  Olaf Loge

    IPC分类号： C07D317/14 ,  C07D317/46 ,  C07D317/70 ,  C07D319/06 ,  C07D319/08 ,  C07F9/40 ,  C07F9/54 ,  A01N9/28 ,  A61K31/335

    CPC分类号： C07F9/4006 ,  C07D317/46 ,  C07D317/70 ,  C07D319/06 ,  C07F9/5407

    摘要： Prostaglandins of the formula ##STR1## wherein R.sub.1 is hydroxymethyl, carboxy, aryloxycarbonyl, alkoxycarbonyl of 1-8 carbon atoms in the alkoxy group, or the group -COO-CH.sub.2 -U-V wherein U is a direct C-C bond, carbonyl or carbonyloxy and V is phenyl substituted by phenyl, alkoxy of 1-2 carbon atoms or halogen; R.sub.2 is hydroxy and R.sub.3 is a hydrogen atom or R.sub.2 and R.sub.3 collectively are an oxygen atom; A is -CH.sub.2 -CH.sub.2 or trans-CH=CH; B is -CH.sub.2 -CH.sub.2 or CH=CH; one of R.sub.4 and R.sub.5 is hydroxy and the other is a hydrogen atom; R.sub.6 and R.sub.7 each are alkyl of 1-10 carbon atoms or collectively are alkylene of up to 7 carbon atoms and with 2-3 carbon atoms in the chain, phenylene or naphthylene; R.sub.8 is a hydrogen atom or alkyl of 1-5 carbon atoms; ##STR2## when R.sub.2 is hydroxy and R.sub.3 is a hydrogen atom or is ##STR3## or -CH=CH- when R.sub.2 and R.sub.3 collectively are an oxygen atom; or, when R.sub.1 is carboxy, a physiologically acceptable salt thereof with a base, possess the activity of the corresponding natural prostaglandins, including a luteolytic effect, and are useful in triggering abortions and syncronizing the conception cycle of mammals.

    摘要翻译： 其中R1是羟甲基，羧基，芳氧基羰基，烷氧基中1-8个碳原子的烷氧基羰基或基团-COO-CH2-UV，其中U是直接的CC键，羰基或羰基氧基和V 是被苯基，1-2个碳原子的烷氧基或卤素取代的苯基; R2是羟基，R3是氢原子，R2和R3一起是氧原子; A是-CH 2 -CH 2或反式-CH = CH; B是-CH 2 -CH 2或CH = CH; R4和R5之一是羟基，另一个是氢原子; R6和R7各自为1-10个碳原子的烷基，或者统称为至多7个碳原子的亚烷基，链中有2-3个碳原子，亚苯基或亚萘基; R8是氢原子或1-5个碳原子的烷基; 当R2和R3共同为氧原子时，当R 2为羟基且R 3为氢原子或者为或者-CH = CH-时， 或者，当R 1为羧基时，其与碱的生理上可接受的盐具有相应的天然前列腺素的活性，包括溶血性作用，并且可用于触发哺乳动物的受孕循环的流产和同步化。

    15-Ethylenedioxy-prostanoic acid derivatives and esters thereof and intermediates thereof
    8.
    发明授权
    15-Ethylenedioxy-prostanoic acid derivatives and esters thereof and intermediates thereof 失效
    15-亚乙二氧基 - 前列腺酸衍生物及其酯及其中间体

    公开(公告)号：US4088775A

    公开(公告)日：1978-05-09

    申请号：US595015

    申请日：1975-07-11

    申请人： Werner Skuballa ,  Bernd Raduchel ,  Helmut Vorbruggen ,  Walter Elger ,  Wolfgang Losert ,  Olaf Loge

    发明人： Werner Skuballa ,  Bernd Raduchel ,  Helmut Vorbruggen ,  Walter Elger ,  Wolfgang Losert ,  Olaf Loge

    IPC分类号： C07D407/04 ,  A61K31/557 ,  A61K31/5575 ,  A61P43/00 ,  C07C67/00 ,  C07C401/00 ,  C07C405/00 ,  C07D317/00 ,  C07D317/30 ,  C07D317/46 ,  C07F9/535 ,  C07F9/655 ,  A61K31/335 ,  A61K31/36

    CPC分类号： C07C405/00 ,  C07D317/30

    摘要： Prostanoic acid derivatives of the formula ##STR1## wherein R.sub.1 is a hydrogen atom, alkyl of 1-10 carbon atoms, aryl or --CH.sub.2 --U--V wherein U is a direct bond, carbonyl, or carbonyloxy and V is phenyl or substituted phenyl, e.g. substituted by at least one of phenyl, alkoxy of 1-2 carbon atoms or a halogen atom; one of R.sub.2 and R.sub.3 is hydroxy and the other is a hydrogen atom or R.sub.2 and R.sub.3 collectively are an oxygen atom; A is --CH.sub.2 --CH.sub.2 -- or trans--CH.dbd.CH; B is --CH.sub.2 --CH.sub.2 -- or cis--CH.dbd.CH; D and E collectively are a direct bond, or D is alkylene or 1-5 carbon atoms and E is an oxygen or sulfur atom; R.sub.4 is alkyl of 1-10 carbon atoms, alkyl of 1-5 carbon atoms substituted by unsubstituted or substituted aryl, unsubstituted or substituted aryl, or benzodioxol-2-yl-; X--Y is ##STR2## when one of R.sub.2 and R.sub.3 is a hydroxy group and the other is a hydrogen atom or X--Y is ##STR3## or --CH.dbd.CH-- when R.sub.2 and R.sub.3 collectively are an oxygen atom; and when R.sub.1 is a hydrogen atom, the physiologically acceptable salts thereof with bases, have an activity spectrum similar to but stronger and longer lasting activity than the corresponding natural prostaglandins.

    摘要翻译： 其中R1是氢原子，1-10个碳原子的烷基，芳基或-CH2-U-V，其中U是直接键，羰基或羰氧基，V​​是苯基或取代的苯基，例如， 被苯基，1-2个碳原子的烷氧基或卤素原子中的至少一个取代; R2和R3之一是羟基，另一个是氢原子，R2和R3共同是氧原子; A是-CH 2 -CH 2 - 或反-CH = CH; B是-CH 2 -CH 2 - 或顺式-CH = CH; D和E共同是直接键合，或D是亚烷基或1-5个碳原子，E是氧或硫原子; R4是1-10个碳原子的烷基，1-5个碳原子的烷基被未取代或取代的芳基，未取代或取代的芳基或苯并间二氧杂环戊烯-2-基取代; 当R2和R3中的一个是氧原子时，当R 2和R 3中的一个是羟基，另一个是氢原子或X-Y是<或>时，X-Y是 当R1是氢原子时，其与碱的生理上可接受的盐具有与相应的天然前列腺素相似但更强和更持久的活性的活性谱。