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134 条记录 (耗时 0.042 秒)

    Prostaglandins and prostacyclins, process for their preparation and their use as medicaments
    52.
    发明授权
    Prostaglandins and prostacyclins, process for their preparation and their use as medicaments 失效
    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。

    .DELTA..sup.8,9 -Prostaglandin derivatives, their preparation and use as medicinal agents
    53.
    发明授权
    .DELTA..sup.8,9 -Prostaglandin derivatives, their preparation and use as medicinal agents 失效
    DELTA 8,9-前列腺素衍生物，其制备和用作药物

    公开(公告)号：US4560786A

    公开(公告)日：1985-12-24

    申请号：US391734

    申请日：1982-06-24

    申请人： Werner Skuballa ,  Bernd Raduechel ,  Norbert Schwarz ,  Helmut Vorbrueggen ,  Walter Elger ,  Olaf Loge ,  Michael-Harold Town

    发明人： Werner Skuballa ,  Bernd Raduechel ,  Norbert Schwarz ,  Helmut Vorbrueggen ,  Walter Elger ,  Olaf Loge ,  Michael-Harold Town

    IPC分类号： A61K31/045 ,  A61K31/557 ,  A61K31/5575 ,  A61P25/04 ,  C07C67/00 ,  C07C401/00 ,  C07C405/00 ,  C07C177/00

    CPC分类号： C07C405/0016 ,  C07C405/00 ,  C07C405/0041

    摘要： .DELTA..sup.8,9 -Prostane derivatives of Formula I ##STR1## wherein R.sub.1 is CH.sub.2 OH or ##STR2## wherein R.sub.2 is hydrogen, alkyl, cycloalkyl, aryl, or a heterocyclic residue; or R.sub.1 is ##STR3## wherein R.sub.3 is an acid residue or R.sub.2 ; A is --CH.sub.2 --CH.sub.2 -- or cis--CH.dbd.CH;B 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 ##STR4## wherein the OH--group can be in the .alpha.-- or .beta.-- position; D and E jointly are a direct bond orD is straight chain or branched alkylene or alkenylene of 1-10 carbon atoms which can optionally be substituted by fluorine atoms, and E is oxygen, sulfur, a direct bond, --C.tbd.C-- or --CR.sub.6 .dbd.CR.sub.7 --, wherein R.sub.6 and R.sub.7 differ from each other and each is hydrogen, chlorine or alkyl;R.sub.4 is free or functionally modified hydroxy andR.sub.5 is an optionally substituted aliphatic group, cycloalkyl, optionally substituted aryl, or a heterocyclic group, and when R.sub.2 is hydrogen, physiologically compatible salts thereof with bases,have valuable pharmacological properties, e.g. luteolytic and abortifacient activities.

    摘要翻译： DELTA 8,9-式I的前驱体衍生物其中R 1是CH 2 OH或其中R 2是氢，烷基，环烷基，芳基或杂环残基; 或R 1为，其中R 3为酸残基或R 2; A是-CH 2 -CH 2 - 或顺式-CH = CH; B是-CH 2 -CH 2 - ，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“IMAGE”，其中OH-基团可以是α或β - 位置 D和E共同是直接键合，或D是可以任选被氟原子取代的1-10个碳原子的直链或支链亚烷基或亚烯基，并且E是氧，硫，直接键，-C 3 D或 -CR 6 = CR 7 - ，其中R 6和R 7彼此不同，各自为氢，氯或烷基; R4是游离的或官能改性的羟基，R 5是任选取代的脂族基，环烷基，任选取代的芳基或杂环基，当R 2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。 luteolytic和流产活动。

    9-Fluoroprostaglandin derivatives, and use as medicinal agents
    54.
    发明授权
    9-Fluoroprostaglandin derivatives, and use as medicinal agents 失效
    9-氟前列腺素衍生物，用作药物

    公开(公告)号：US4454339A

    公开(公告)日：1984-06-12

    申请号：US395448

    申请日：1982-07-06

    申请人： Werner Skuballa ,  Bernd Raduechel ,  Norbert Schwarz ,  Helmut Vorbrueggen ,  Walter Elger ,  Olaf Loge ,  Michael-Harold Town

    发明人： Werner Skuballa ,  Bernd Raduechel ,  Norbert Schwarz ,  Helmut Vorbrueggen ,  Walter Elger ,  Olaf Loge ,  Michael-Harold Town

    IPC分类号： A61K31/557 ,  A61K31/5575 ,  A61P43/00 ,  C07C67/00 ,  C07C401/00 ,  C07C405/00 ,  C07C177/00

    CPC分类号： C07C405/00 ,  C07C405/0016 ,  C07C405/0041

    摘要： 9-Fluoroprostane derivatives of Formula I ##STR1## wherein R.sub.1 is CH.sub.2 OH or ##STR2## wherein R.sub.2 is hydrogen, alkyl, cycloalkyl, aryl, or a heterocyclic residue; or R.sub.1 is the residue ##STR3## wherein R.sub.3 is an acid residue or R.sub.2 and A is --CH.sub.2 --CH.sub.2 -- or cis--CH.dbd.CH--,B is --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH-- or --C.tbd.C,W is a free or functionally modified hydroxymethylene group wherein the OH-group can be in the .alpha.- or .beta.-position,D and E jointly are a direct bond orD is straight-chain or branched alkylene or alkenylene of 1-10 carbon atoms which can optionally be substituted by fluorine atoms, and E is oxygen or sulfur, a direct bond, --C.tbd.C-- or --CR.sub.6 .dbd.CR.sub.7 -- wherein R.sub.6 and R.sub.7 differ from each other and each is hydrogen, chlorine, or alkyl,R.sub.4 is a free or functionally modified hydroxy group, andR.sub.5 is hydrogen, an optionally substituted aliphatic group, e.g., alkyl or halosubstituted alkyl, cycloalkyl, optionally substituted aryl or a heterocyclic group, and, when R.sub.2 is H, physiologically compatible salts thereof with bases,have valuable pharmacological properties, e.g., as luteolytics or abortifacients.

    摘要翻译： 其中R 1是CH 2 OH或其中R 2是氢，烷基，环烷基，芳基或杂环残基的式I的1-氟代衍生物（Ⅰ） 或R1是残基，其中R3是酸残基或R2和A是-CH2-CH2-或顺式-CH = CH-，B是-CH2-CH2-，反式-CH = CH-或-C3BOND C，W是游离的或官能改性的羟基亚甲基，其中OH基可以是α-或β-位，D和E共同是直接键，或D是1-10的直链或支链亚烷基或亚烯基 可以任选被氟原子取代的碳原子，E是氧或硫，直接键，-C 3 D或-CR 6 = CR 7 - ，其中R 6和R 7彼此不同，各自是氢，氯或烷基 R4是游离的或官能改性的羟基，R5是氢，任意取代的脂族基团，例如烷基或卤代取代的烷基，环烷基，任选取代的芳基或杂环基，当R 2是H时，其生理上相容的盐 具有碱性，具有有价值的药理学性质，例如作为纤溶素或流产。

    Novel 1,3-benzodioxaneprostanoic acid derivatives and process for the preparation thereof
    56.
    发明授权
    Novel 1,3-benzodioxaneprostanoic acid derivatives and process for the preparation thereof 失效
    新型1,3-苯并二恶烷庚酸衍生物及其制备方法

    公开(公告)号：US4217360A

    公开(公告)日：1980-08-12

    申请号：US2268

    申请日：1979-01-10

    申请人： Helmut Vorbrueggen ,  Norbert Schwarz ,  Olaf Loge ,  Walter Elger

    发明人： Helmut Vorbrueggen ,  Norbert Schwarz ,  Olaf Loge ,  Walter Elger

    IPC分类号： C07C37/62 ,  C07C37/66 ,  C07D319/08 ,  C07F9/655

    CPC分类号： C07D319/08 ,  C07C37/62 ,  C07C37/66 ,  C07F9/65522

    摘要： 1,3-Benzodioxaneprostanoic acid compound of the formula ##STR1## wherein R.sub.1 is hydroxy, alkoxy of 1-10 carbon atoms, methylsulfamido, substituted or unsubstituted aryloxy, or O--CH.sub.2 --U--V wherein U is a direct bond, carbonyl, or carbonyloxy, and V is phenyl or phenyl substituted, e.g. by one or more of phenyl, phenoxy, alkoxy of 1-2 carbon atoms, and halogen; A is --CH.sub.2 --CH.sub.2 -- or trans --CH.dbd.CH--; B is --CH.sub.2 --CH.sub.2 -- or cis- or trans--CH.dbd.CH--; Z is hydroxymethylene or carbonyl; X Y, if Z is hydroxymethylene, is ##STR2## or, if Z is carbonyl, is ##STR3## or --CH.dbd.CH--; R.sub.2 is hydrogen or alkyl of 1-5 carbon atoms; R.sub.3 and R.sub.4 each are H, F, Cl, Br, I or CF.sub.3, CH.sub.3 or alkoxy of 1-2 carbon atoms or R.sub.3 and R.sub.4 in 6-,7-position is methylendioxy; and if R.sub.1 is hydroxy, salts thereof with pharmaceutically acceptable bases, are agents for inducing menstruation, interrupting pregnancy, inducing labor and synchronizing the sexual cycle in female mammals.

    摘要翻译： 其中R1是羟基，1-10个碳原子的烷氧基，甲基亚磺酰氨基，取代或未取代的芳氧基或O-CH2-UV，其中U是直接键，羰基或羰基氧基的1,3-苯并二恶烷庚酸化合物 ，和V是苯基或苯基取代的，例如 苯基，苯氧基，1-2个碳原子的烷氧基和一个或多个卤素; A是-CH 2 -CH 2 - 或反-CH = CH-; B是-CH 2 -CH 2 - 或顺式 - 或反式-CH = CH-; Z是羟基亚甲基或羰基; 如果Z是羟基亚甲基，X Y是或者如果Z是羰基，则是Y或CH = CH-; R2是氢或1-5个碳原子的烷基; R3和R4各自为H，F，Cl，Br，I或CF3，CH3或1-2个碳原子的烷氧基或6-7位的R3和R4是甲氧基; 并且如果R 1是羟基，则其盐与药学上可接受的碱，是诱导雌性哺乳动物诱发月经，中断怀孕，诱导劳动和同步性循环的药剂。

    Novel acetylenic prostaglandin analogs
    57.
    发明授权
    Novel acetylenic prostaglandin analogs 失效
    新型炔类前列腺素类似物

    公开(公告)号：US4073934A

    公开(公告)日：1978-02-14

    申请号：US677861

    申请日：1976-04-16

    申请人： Werner Skuballa ,  Bernd Raduechel ,  Helmut Vorbrueggen ,  Walter Elger ,  Olaf Loge ,  Eckehard Schillinger

    发明人： Werner Skuballa ,  Bernd Raduechel ,  Helmut Vorbrueggen ,  Walter Elger ,  Olaf Loge ,  Eckehard Schillinger

    IPC分类号： A61K31/23 ,  C07C67/00 ,  C07C401/00 ,  C07C405/00 ,  C07D213/30 ,  C07D213/55 ,  C07D307/38 ,  C07D307/54 ,  C07D307/935 ,  C07D333/06 ,  C07C177/00 ,  A61K31/19 ,  A61K31/215

    CPC分类号： C07D307/935 ,  C07C405/00

    摘要： Optically active and racemic prostaglandin derivatives of the formula ##STR1## wherein R.sub.1 is --OR.sub.5 ; --NHSO.sub.2 CH.sub.3 ; or --O--CH.sub.2 --U--V; R.sub.5 is hydrogen, alkyl, aryl, or a heterocyclic group; U is a direct bond, carbonyl or carbonyloxy; and V is phenyl substituted by 1-3 phenyl, alkoxy of 1-2 carbon atoms, or halogen, preferably bromine;R.sub.2 is hydrogen or alkyl of 1-5 carbon atoms;R.sub.3 is alkyl, substituted or unsubstituted cycloalkyl, straight-chain or branched alkyl of 1-5 carbon atoms substituted by aryl or substituted aryl, when R.sub.1 is as above; or R.sub.3 is aryl or substituted aryl group when R.sub.1 is --OR.sub.5 ', --NHSO.sub.2 CH.sub.3, or --O--CH.sub.2 --U--V and R.sub.5 ' is aryl or a heterocyclic group and U and V are as above;R.sub.4 is hydrogen or an ether or acyl residue;A is --CH.sub.2 --CH.sub.2 -- or cis--CH.dbd.CH--;B is --CH.sub.2 --CH.sub.2 -- or trans--CH.dbd.CH--;D is a direct bond, oxygen, or sulfur;Z is carbonyl or >CH OR.sub.4 wherein OR.sub.4 is in the .alpha.- or .beta.-position; andX y is ##STR2## when Z is >CH OR.sub.4 --, or ##STR3## or --CH.dbd.CH-- when Z is carbonyl; AND, WHEN R.sub.1 is hydroxy, the physiologically compatible salts thereof with bases, have more prolonged activity than naturally-occurring prostaglandins.

    摘要翻译： 式（Ⅰ）的光学活性和外消旋前列腺素衍生物，其中R1为-OR5; -NHSO 2 CH 3; 或-O-CH 2 -U-V; R5是氢，烷基，芳基或杂环基; U是直接键，羰基或羰氧基; 并且V是被1-3个苯基，1-2个碳原子的烷氧基或卤素，优选溴取代的苯基; R2是氢或1-5个碳原子的烷基; R 3为烷基，取代或未取代的环烷基，被芳基或取代芳基取代的1-5个碳原子的直链或支链烷基，当R 1如上所述时; 或当R 1为-OR 5'，-NHSO 2 CH 3或-O-CH 2 -U-V且R 5'为芳基或杂环基时，R 3为芳基或取代的芳基，U和V如上所述; R4是氢或醚或酰基残基; A是-CH 2 -CH 2 - 或顺式-CH = CH-; B是-CH 2 -CH 2 - 或反式-CH = CH-; D是直接键合，氧或硫; Z是羰基或> CH OR 4，其中OR 4在α或β-位; 当Z为羰基时Z为> CH OR4-或或-CH = CH-时，X Y为 当R1是羟基时，其与碱的生理上相容的盐比天然存在的前列腺素具有更长的活性。

    Mesoprogrestins (progesterone receptor modulations) as a component of compositions for hormone replacement therapy (HRT)
    60.
    发明授权
    Mesoprogrestins (progesterone receptor modulations) as a component of compositions for hormone replacement therapy (HRT) 有权
    作为激素替代疗法（HRT）组合物组分的Mesoprogrestins（孕酮受体调节）

    公开(公告)号：US07629334B1

    公开(公告)日：2009-12-08

    申请号：US10433984

    申请日：2000-08-31

    申请人： Kristof Chwalisz ,  Walter Elger ,  Gerd Schubert

    发明人： Kristof Chwalisz ,  Walter Elger ,  Gerd Schubert

    IPC分类号： A61K31/56 ,  C07J1/00 ,  C07J6/00

    CPC分类号： A61K31/56

    摘要： The use of mesoprogestins as pharmaceutical components for the manufacture of a medicament for hormone replacement therapy (HRT) and as components for the combined use together with an estrogen for the manufacture of a medicament for HRT as well as in respective HRT-methods and methods of treating hormone deficiency and hormone irregularity symptoms. Mesoprogestins are defined as compounds possessing both agonistic and antagonistic activities at the progesterone receptor (PR) in vivo. They stabilize the function of PR at an intermediate level of agonistic and antagonistic. Corresponding functional states cannot be achieved with progestins or antiprogestins. J867, J912, J956 and J1042 are the mesoprogestins preferred herein.

    摘要翻译： 使用中孕烯素作为药物组分用于制造用于激素替代疗法（HRT）的药物，以及作为与雌激素联合使用以用于制备用于HRT的药物的组合以及相应的HRT方法和方法 治疗激素缺乏和激素不规则症状。 中孕烯孕素被定义为在体内孕酮受体（PR）具有激动作用和拮抗活性的化合物。 他们将PR的功能稳定在激进和对抗的中间水平。 孕激素或抗孕激素不能达到相应的功能状态。 J867，J912，J956和J1042是本文优选的中孕酮。