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    5-fluorocarbacyclins, their preparation and pharmaceutical use
    1.
    发明授权
    5-fluorocarbacyclins, their preparation and pharmaceutical use 失效
    5-氟卡巴环素，其制备和药物用途

    公开(公告)号：US5190964A

    公开(公告)日：1993-03-02

    申请号：US480448

    申请日：1990-02-15

    申请人： Werner Skuballa ,  Bernd Raduchel ,  Helmut Vorbruggen ,  Martin Haberey ,  Claus-Steffen Sturzebecher ,  Michael-Harold Town

    发明人： Werner Skuballa ,  Bernd Raduchel ,  Helmut Vorbruggen ,  Martin Haberey ,  Claus-Steffen Sturzebecher ,  Michael-Harold Town

    IPC分类号： C07C405/00 ,  C07D263/14

    CPC分类号： C07D263/14 ,  C07C405/0083

    摘要： 5-fluorocarbacyclin derivatives of the Formula I ##STR1## wherein R.sub.1 is CH.sub.2 OH orA is --CH.sub.2 --CH.sub.2 --, trans --CH.dbd.CH-- or --C.tbd.C--,W is a free or functionally modified hydroxymethylene group or free or functionally modified ##STR2## in which the OH group can be in the .alpha.-- or .beta.-position, D is ##STR3## a C.sub.1-10 -aliphatic group (e.g., alkyl or alkenyl) which optionally can be substituted by fluorine atoms,n is 1, 2 or 3,E is a direct bond, --C.tbd.C-- or --CR.sub.6 .tbd.CR.sub.7 -- in which R.sub.6 represents a hydrogen atom or an alkyl group with 1-5 atoms and R.sub.7 represents a hydrogen atom, a halogen atom or an alkyl group with 1-5 C atoms,R.sub.4 is alkyl, cycloalkyl or optionally substituted aryl or a heterocyclic group,R.sub.5 is a free or functionally modified hydroxy groupand, when R.sub.2 is a hydrogen atom, its salts with physiologically compatible bases,have valuable pharmacological properties.

    摘要翻译： 其中R 1是CH 2 OH或A是-CH 2 -CH 2 - ，反式-CH = CH-或-CB 3 C，其中W是游离的或官能改性的羟基亚甲基，或游离或官能改性的羟基亚甲基， 官能改性的“IMAGE”，其中OH基团可以是α或β-位，D是可任选被氟原子取代的C 1-10脂族基团（例如烷基或烯基），n 是1,2或3，E是直接键，-C 3 D或-CR 6 3BOND CR 7 - ，其中R 6表示氢原子或具有1-5个原子的烷基，R 7表示氢原子，卤素原子 或具有1-5个C原子的烷基，R4是烷基，环烷基或任选取代的芳基或杂环基，R5是游离或官能改性的羟基，当R2是氢原子时，其与生理上相容的碱的盐， 具有宝贵的药理性质。

    Novel prostacyclin derivatives and a process for the preparation thereof
    2.
    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 and use as medicines
    3.
    发明授权
    5-Cyano-prostacyclin derivatives and use as medicines 失效
    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。

    Novel prostanoic acid derivatives and process for the preparation thereof
    4.
    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。

    Crystalline prostanoic acid esters
    9.
    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。

    Process for the preparation of prostaglandin F.sub.2.sub..alpha. and the analogs thereof
    10.
    发明授权
    Process for the preparation of prostaglandin F.sub.2.sub..alpha. and the analogs thereof 失效
    制备前列腺素F（HD 2 {301 {0 {B及其类似物）的方法

    公开(公告)号：US3970692A

    公开(公告)日：1976-07-20

    申请号：US472737

    申请日：1974-05-23

    申请人： Bernd Raduchel ,  Werner Skuballa ,  Helmut Vorbruggen

    发明人： Bernd Raduchel ,  Werner Skuballa ,  Helmut Vorbruggen

    IPC分类号： A01N43/832 ,  C07C67/00 ,  C07C401/00 ,  C07C405/00 ,  C07C177/00

    CPC分类号： C07C405/00

    摘要： Prostaglandin F.sub.2.sub..alpha. and analogs thereof of the formula ##SPC1##Wherein one of R.sub.1 and R.sub.2 is hydroxy and the other is H or CH.sub.3, R.sub.3 is the remainder of the lower side chain and X is the remainder of the upper side chain thereof are produced in two steps from a 3-acyloxy mono ester of a lactone of the formula ##SPC2##Wherein R.sub.1, R.sub.2 and R.sub.3 have the values given below, by reacting the lactone with excess diisobutylaluminum hydride and reacting the thus-produced ketol, in the presence of strong anhydrous base, with a Wittig reagent of the formula Ph.sub.3 P=CH--X--COOH wherein Ph is a phenyl group and X has the values given above.

    摘要翻译： 前列腺素F2α及其类似物，其中R 1和R 2的化学式为羟基，另一个为H或CH 3，R 3为下侧链的其余部分，X为上侧链的其余部分，分两步制备 由式WHEREIN R1，R2和R3的内酯的3-酰氧基单酯通过使内酯与过量的二异丁基氢化铝反应，并将如此制备的酮醇在强无水碱存在下，与 式Ph3P = CH-X-COOH的Wittig试剂，其中Ph是苯基，X具有上述给出的值。