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2391 条记录 (耗时 0.046 秒)

    Transmetalations from zirconium to copper intermediates
    52.
    发明授权
    Transmetalations from zirconium to copper intermediates 失效
    从锆到铜中间体的转化

    公开(公告)号：US5286889A

    公开(公告)日：1994-02-15

    申请号：US20492

    申请日：1993-02-22

    申请人： Bruce H. Lipshutz ,  Edmund L. Ellsworth

    发明人： Bruce H. Lipshutz ,  Edmund L. Ellsworth

    IPC分类号： C07C405/00 ,  C07F1/08 ,  C07D309/00

    CPC分类号： C07F1/08 ,  C07C405/00

    摘要： Higher order cuprate complexes are prepared by means of a transmetalation from a corresponding zirconate intermediate. This process is particularly valuable with respect to the preparation of vinylic side chains such as are present in prostaglandins, as it is possible in accordance with the present invention to proceed directly from the acetylenic precursors via the reactive cuprates to the desired final products in a one-pot operation without isolation of intermediates and in high yields. Sequential additions to zirconium intermediates of components which together comprise the cuprate involved in transmetalation with the zirconium intermediate are disclosed as alternative procedures.

    摘要翻译： 通过来自相应锆酸盐中间体的转化金属制备高级铜酸盐络合物。 该方法对于制备乙烯基侧链（例如存在于前列腺素中）是特别有价值的，因为根据本发明可能通过反应性铜酸盐从炔属前体直接进行到所需的最终产物 - 不分离中间体并以高产率进行操作。 作为替代方法公开了一起组合的锆中间体的顺序添加，其一起包括与锆中间体转铁合金的铜盐。

    Prostaglandins E and anti ulcers containing same
    54.
    发明授权
    Prostaglandins E and anti ulcers containing same 失效
    前列腺素E和含有相同的抗溃疡

    公开(公告)号：US5225439A

    公开(公告)日：1993-07-06

    申请号：US681031

    申请日：1991-04-05

    申请人： Ryuzo Ueno ,  Ryuji Ueno ,  Ichie Kato ,  Tomio Oda

    发明人： Ryuzo Ueno ,  Ryuji Ueno ,  Ichie Kato ,  Tomio Oda

    IPC分类号： C07C405/00

    CPC分类号： C07C405/00

    摘要： The novel 13, 14-dihydro-15-keto prostaglandins E of the invention have remarkable preventive effects against ulcers. Further, the novel 13,14-dihydro-15-keto-prostaglandins E of the invention have an advatage that they have none of side effects which prostaglandin E intrinsically has, or can remarakably reduce such effects of the prostaglandin E. Therefore, the novel 13, 14-dihydro-15-keto prostaglandins E of the invention are effective for animal and human use for treatment and prevention of ulcers, such as duodenal ulcer and gastric ulcer.

    摘要翻译： 本发明的新型13,14-二氢-15-酮前列腺素E对溃疡具有显着的预防作用。 此外，本发明的新型13,14-二氢-15-酮前列腺素E具有前列腺素E本身具有的副作用，或者可以再度降低前列腺素E的作用的优点。因此，该小说 本发明的13,14-二氢-15-酮基前列腺素E对于动物和人类用于治疗和预防溃疡如十二指肠溃疡和胃溃疡是有效的。

    Pharmaceutically active 9-chloroprostaglandins
    56.
    发明授权
    Pharmaceutically active 9-chloroprostaglandins 失效
    药用活性9-氯前列腺素

    公开(公告)号：US5204371A

    公开(公告)日：1993-04-20

    申请号：US792574

    申请日：1991-11-15

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

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

    IPC分类号： C07C405/00

    CPC分类号： C07C405/0041 ,  C07C405/00

    摘要： Compounds of the formula ##STR1## wherein the 9-chlorine atom can be in the .alpha.-or .beta.-position,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 --CH.tbd.C--, W is hydroxymethylene orD and E together represent a direct bond orD is a straight-chain or branched alkylene group of 1-10 carbon atoms, optionally substituted by fluorine, andE is oxygen or sulfur or a direct bond, andR.sub.4 is hydroxy or hydroxy etherified or esterified as defined for W above;R.sub.5 is a C.sub.1-10 hydrocarbon aliphatic group; a C.sub.1-10 hydrocarbon aliphatic group substituted by aryl, a substituted aryl as defined for R.sub.2 above, or halogen; or cycloalkyl, substituted cycloalkyl, aryl, substituted aryl or aromatic heterocyclic, all as defined for R.sub.2 above;or a physiologically acceptable salt thereof with a base when R.sub.1 is OH,have valuable pharmacologoical properties.

    摘要翻译： 其中9-氯原子可以是α-或β-位的式为“IMAGE”的化合物，A为-CH 2 -CH 2 - 或顺式-CH = CH-，B为-CH 2 -CH 2， - ， CH = CH-或-CH 3 B - ，W是羟基亚甲基或D和E一起代表直接键，或D是1-10个碳原子的直链或支链亚烷基，任选被氟取代，E是 氧或硫或直接键，并且R4是如上定义的羟基或羟基醚化或酯化; R5是C1-10烃脂族基团; 被芳基取代的C1-10烃脂族基，对上述R2定义的取代芳基或卤素; 或环烷基，取代的环烷基，芳基，取代的芳基或芳族杂环，全部如上述R2所定义; 或其生理上可接受的盐，当R1为OH时，具有有价值的药理学性质。

    20-alkyl-7-oxoprostacyclin derivatives useful as pharmaceuticals
    57.
    发明授权
    20-alkyl-7-oxoprostacyclin derivatives useful as pharmaceuticals 失效
    可用作药物的20-烷基-7-氧代前列环素衍生物

    公开(公告)号：US5190973A

    公开(公告)日：1993-03-02

    申请号：US599916

    申请日：1990-10-19

    申请人： Robert Nickolson ,  Helmut Vorbrueggen ,  Claus S. Stuerzebecher ,  Martin Haberey

    发明人： Robert Nickolson ,  Helmut Vorbrueggen ,  Claus S. Stuerzebecher ,  Martin Haberey

    IPC分类号： C07C405/00 ,  C07D307/935 ,  C07D307/937

    CPC分类号： C07D307/935 ,  C07C405/00 ,  C07D307/937

    摘要： The invention concerns 20-alkyl-7-oxoprostacyclin derivatives of general Formula I ##STR1## wherein R.sub.1 is the residue OR.sub.3 where R.sub.3 means hydrogen or alkyl of 1-10 carbon atoms optionally substituted by halogen, phenyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.4 -dialkylamino; cycloalkyl, aryl or a heterocyclic residue, or the residue NHR.sub.4 where R.sub.4 means hydrogen or an alkanoyl or alkanesulfonyl residue of respectively 1-10 carbon atoms,n is 1 or 2,A is a CH.sub.2 --CH.sub.2 --, cis--CH.dbd.CH-- or trans--CH.dbd.CH--group,W is a ##STR2## or a ##STR3## wherein the OH-group can respectively be esterified with a benzoyl or alkanoic acid residue of 1-4 carbon atoms, or etherified with a tetrahydropyranol, tetrahydrofuranyl, alkoxyalkyl or trialkylsilyl residue, wherein the free or esterified OH-group can be in the .alpha.- or .beta.-position,R.sub.2 is a straight-chain or branched-chain alkyl group of 1-6 carbon atoms,R.sub.5 is a hydroxy group which can be esterified with an alkanoic acid residue of 1-4 carbon atoms or etherified with a tetrahydropyranyl, tetrahydrofuranyl, alkoxyalkyl or trialkylsilyl residue,R.sub.6 and R.sub.7 are hydrogen or a straight-chain or branched-chain alkyl group of 1-4 carbon atoms, or R.sub.6 and R.sub.7 jointly represent a trimethylene group,R.sub.8 and R.sub.9 jointly represent a linkage or hydrogen or a straight-chain or branched-chain alkyl group of 1-4 carbon atoms,and, if R.sub.3 is hydrogen, the salts thereof with physiologically compatible bases; their production; and their use as medicinal agents.

    摘要翻译： 本发明涉及通式I（I）的20-烷基-7-氧代前列环素衍生物，其中R 1是残基OR 3，其中R 3表示氢或1-10个碳原子的任选被卤素，苯基，C 1 -C 4 - 烷氧基或C 1 -C 4 - 二烷基氨基; 环烷基，芳基或杂环残基，或残基NHR4，其中R4表示氢或分别为1-10个碳原子的烷酰基或烷磺酰基，n为1或2，A为CH2-CH2-，顺式-CH = CH- 或反式-CH = CH-基团，W为“IMAGE”或“IMAGE”，其中OH基团可分别用1-4个碳原子的苯甲酰基或链烷酸残基酯化，或用四氢吡喃醇醚化，四氢呋喃基 ，烷氧基烷基或三烷基甲硅烷基残基，其中游离或酯化的OH基可以是α或β-位，R2是1-6个碳原子的直链或支链烷基，R5是羟基， 可以用1-4个碳原子的链烷酸残基酯化，或与四氢吡喃基，四氢呋喃基，烷氧基烷基或三烷基甲硅烷基残基醚化，R6和R7是氢或1-4个碳原子的直链或支链烷基， 或R6和R7共同表示三亚甲基，R8和R9共同表示键或 氢或1-4个碳原子的直链或支链烷基，如果R 3是氢，则其与生理上相容的碱的盐; 他们的生产; 并将其用作药剂。

    5-fluorocarbacyclins, their preparation and pharmaceutical use
    58.
    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。

    Transmetalations from zirconium to copper intermediates
    59.
    发明授权
    Transmetalations from zirconium to copper intermediates 失效
    从锆到铜中间体的转化

    公开(公告)号：US5166382A

    公开(公告)日：1992-11-24

    申请号：US747772

    申请日：1991-08-20

    申请人： Bruce Howard ,  Edmund L. Ellsworth

    发明人： Bruce Howard ,  Edmund L. Ellsworth

    IPC分类号： C07C405/00 ,  C07F1/08

    CPC分类号： C07C405/00 ,  C07F1/08

    摘要： Higher order cuprate complexes are prepared by means of a transmetalation from a corresponding zirconate intermediate. This process is particularly valuable with respect to the preparation of vinylic side chains such as are present in prostaglandins, as it is possible in accordance with the present invention to proceed directly from the acetylenic precursors via the reactive cuprates to the desired final products in a one-pot operation without isolation of intermediates and in high yields. Sequential additions to zirconium intermediates of components which together comprise the cuprate involved in transmetalation with the zirconium intermediate are disclosed as alternative procedures.

    摘要翻译： 通过来自相应锆酸盐中间体的转化金属制备高级铜酸盐络合物。 该方法对于制备乙烯基侧链（例如存在于前列腺素中）是特别有价值的，因为根据本发明可能通过反应性铜酸盐从炔属前体直接进行到所需的最终产物 - 不分离中间体并以高产率进行操作。 作为替代方法公开了一起组合的锆中间体的顺序添加，其一起包括与锆中间体转铁合金的铜盐。