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    Alkenoic acid derivatives
    1.
    发明授权
    Alkenoic acid derivatives 失效
    烯酸衍生物

    公开(公告)号：US5221760A

    公开(公告)日：1993-06-22

    申请号：US891629

    申请日：1992-06-01

    申请人： Ulrich Rosentreter ,  Harold C. Kluender ,  Trevor S. Abram ,  Peter Norman ,  Steven R. Tudhope

    发明人： Ulrich Rosentreter ,  Harold C. Kluender ,  Trevor S. Abram ,  Peter Norman ,  Steven R. Tudhope

    IPC分类号： C07C43/225 ,  C07C43/23 ,  C07C63/14 ,  C07C65/24 ,  C07C309/73 ,  C07C323/56 ,  C07F7/18 ,  C07F9/54

    CPC分类号： C07F9/5456 ,  C07C309/73 ,  C07C323/56 ,  C07C43/225 ,  C07C43/23 ,  C07C63/14 ,  C07C65/24 ,  C07F7/1852 ,  C07F9/5407

    摘要： An alkenoic acid derivative of the formula ##STR1## in which X and Y are identical or different and represent sulfur, sulfoxide, sulfone, an alkylene chain, --SCH.sub.2 --, or oxygen or a direct bond,W represents --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --,o represents a number 1 to 5,A and B are identical or different and represent carboxyl, carboxymethylene, tetrazolyl or tetrazolylmethylene, or --CO.sub.2 R.sup.9 or --CH.sub.2 CO.sub.2 R.sup.9 or --CONR.sup.10 R.sup.11 or nitrilen represents a number 1 to 10,m represents a number 0 to 7,T and Z are identical or different and represent oxygen or a direct bond andR.sup.2, R.sup.3, R.sup.8 are identical or different and represent hydrogen, alkyl, alkoxy, halogen, trifluoromethyl, trifluoromethoxy, cyano or nitro andR.sup.9 is lower alkyl and R.sup.10 and R.sup.11 are hydrogen, lower alkyl, alkylsulfonyl or arylsulfonyl or together are an alkylene chain to form a ringand pharmaceutically acceptable salts thereof. Such alkenoic acid derivatives are useful as leucotriene disease antagonists.

    摘要翻译： 其中X和Y相同或不同并表示硫，亚砜，砜，亚烷基链，-SCH 2 - 或氧或直接键的式（I）的链烯酸衍生物，W表示-CH = CH-或-CH 2 -CH 2 - ，o表示数1至5，A和B相同或不同，表示羧基，羧基亚甲基，四唑基或四唑基亚甲基，或-CO 2 R 9或-CH 2 CO 2 R 9或-CONR 10 R 11或腈n表示1 至10，m表示0至7的数，T和Z相同或不同，表示氧或直接键，R2，R3，R8相同或不同，表示氢，烷基，烷氧基，卤素，三氟甲基，三氟甲氧基，氰基 或硝基，R 9为低级烷基，R 10和R 11为氢，低级烷基，烷基磺酰基或芳基磺酰基，或一起为形成环的亚烷基链及其药学上可接受的盐。 这样的链烯酸衍生物可用作白三烯类疾病拮抗剂。

    15-Deoxy-16-hydroxy prostaglandins for producing bronchodilation
    4.
    发明授权
    15-Deoxy-16-hydroxy prostaglandins for producing bronchodilation 失效
    用于产生支气管扩张的15-脱氧-16-羟基前列腺素

    公开(公告)号：US4415592A

    公开(公告)日：1983-11-15

    申请号：US357428

    申请日：1982-03-12

    申请人： Harold C. Kluender ,  Warren D. Woessner ,  William G. Biddlecom

    发明人： Harold C. Kluender ,  Warren D. Woessner ,  William G. Biddlecom

    IPC分类号： C07C29/09 ,  C07C29/147 ,  C07C29/36 ,  C07C29/42 ,  C07C29/62 ,  C07C45/45 ,  C07C45/62 ,  C07C47/293 ,  C07C47/30 ,  C07C49/293 ,  C07C49/433 ,  C07C49/443 ,  C07C51/09 ,  C07C51/353 ,  C07C51/38 ,  C07C61/04 ,  C07C61/08 ,  C07C405/00 ,  C07F1/08 ,  A61K31/12

    CPC分类号： C07F1/08 ,  C07C29/095 ,  C07C29/147 ,  C07C29/36 ,  C07C29/42 ,  C07C29/62 ,  C07C405/0025 ,  C07C45/45 ,  C07C45/62 ,  C07C47/293 ,  C07C47/30 ,  C07C49/293 ,  C07C49/433 ,  C07C49/443 ,  C07C51/09 ,  C07C51/353 ,  C07C51/38 ,  C07C61/04 ,  C07C61/08 ,  C07B2200/07 ,  C07B2200/09 ,  C07C2101/04 ,  C07C2101/08 ,  C07C2101/14 ,  C07C2101/20 ,  C07C2102/20 ,  C07C2102/22

    摘要： Analogues of PGE.sub.1 having the structural formula, ##STR1## in which J is R-hydroxymethylene or S-hydroxymethylene; R.sub.1 is hydrogen; R.sub.2 is hydrogen or together with R.sub.4 is a methylene chain of 2 to 3 carbon atoms such that a cycloalkyl of 5 to 6 carbon atoms inclusive is formed; R.sub.3 is hydrogen or methyl, or together with R.sub.4 is a methylene or a lower alkylated methylene chain of 2 to 5 carbon atoms such that a cycloalkyl or a lower alkylated cycloalkyl of 4 to 7 carbon atoms inclusive is formed, or together with R.sub.4 is bicycloalkyl or bicycloalkenyl moiety having the formula: ##STR2## such that a bicycloalkyl or bicycloalkenyl compound is formed, wherein m and n are integers having a value from 0 to 3, p is an integer having a value from 0 to 4 and q is an integer having a value of from 1 to 4 and wherein the double bond of such bicycloalkenyl is in the m, n, p, or q bridge; R.sub.4 is hydrogen or methyl or together with R.sub.2 or R.sub.3 forms a cycloalkyl or bicycloalkyl or bicycloalkenyl as defined above, or together with R.sub.5 is a methylene chain of 3 to 5 carbon atoms such that a cycloalkyl of 4 to 6 carbon atoms inclusive is formed; R.sub.5 is selected from the group consisting of hydrogen, straight-chain alkyl having from 1 to 3 carbon atoms or together with R.sub.4 forms a cycloalkyl as defined above; and R.sub.6 is hydrogen or straight-chain alkyl having from 1 to 3 carbon atoms are disclosed.PGE.sub.1 ester analogues of the above formula, limited to the structures wherein two of R.sub.2, R.sub.3, R.sub.4 and R.sub.5 form a cycloalkyl, lower alkylated cycloalkyl, bicycloalkyl or bicycloalkenyl are also disclosed.The prostaglandin analogues selectively produce bronchodilation and decrease gastric secretion in vivo.Methods of preparing the analogues and starting materials required in the synthesis of the analogues are also disclosed.

    摘要翻译： 具有结构式的PGE1的类似物，其中J是R-羟基亚甲基或S-羟基亚甲基; R1是氢; R2是氢或与R4一起是具有2至3个碳原子的亚甲基链，使得形成包含5至6个碳原子的环烷基; R 3为氢或甲基，或与R 4一起为亚甲基或2至5个碳原子的低级烷基化亚甲基链，使得形成包含4-7个碳原子的环烷基或低级烷基化环烷基，或与R4一起形成双环烷基 或具有下式的双环烯基部分：，使得形成双环烷基或双环烯基化合物，其中m和n是0-3的整数，p是0-4的整数，q是整数 具有1至4的值，并且其中双环烯基的双键位于m，n，p或q桥中; R4是氢或甲基，或与R2或R3一起形成如上定义的环烷基或双环烷基或双环烯基，或与R5一起形成3至5个碳原子的亚甲基链，使得形成包含4至6个碳原子的环烷基; R5选自氢，具有1至3个碳原子的直链烷基或与R 4一起形成如上定义的环烷基; 并且R6是氢或具有1至3个碳原子的直链烷基。 还公开了上述式的PGE1酯类似物，限于其中R2，R3，R4和R5中两个形成环烷基，低级烷基化环烷基，双环烷基或双环烯基的结构。 前列腺素类似物选择性地产生支气管扩张并减少体内胃分泌。 还公开了合成类似物所需的类似物和起始材料的方法。

    Depentyl analogues of 11-deoxy-prostaglandin E.sub.2
    8.
    发明授权
    Depentyl analogues of 11-deoxy-prostaglandin E.sub.2 失效

    公开(公告)号：US4127727A

    公开(公告)日：1978-11-28

    申请号：US787478

    申请日：1977-04-14

    申请人： Harold C. Kluender

    发明人： Harold C. Kluender

    IPC分类号： C07C405/00 ,  C07C177/00

    CPC分类号： C07C405/00

    摘要： Depentyl analogues of prostaglandins A, E, and F having no C-16 to C-20 carbon atoms. The analogues correspond to the formula ##STR1## wherein: L is methylene, ethylene, or trimethylene;K is ethylene or cis-vinylene;M is carbonyl, .alpha.-hydroxymethylene, or .beta.-hydroxymethylene;N is methylene or methine, provided that N is methine only if P is methine and M is carbonyl;P is methylene, ethylene, .alpha.-hydroxymethylene or methine, provided that P is methine only if N is methine; and,R is carboxyl; hydroxymethylene, alkoxycarbonyl, the alkyl portion of said alkoxycarbonyl being a lower alkyl, or a pharmacologically acceptable non-toxic carboxy salt.The analogues are prepared by first converting a trans-1-iodo-3-alkoxy-1-propene to the corresponding lithio compound. This lithio compound then combines with the hexamethylphosphorous triamide complex of copper (I) pentyne to give an alkenylcopper species. Reacting this alkenylcopper compound with the appropriate 2-substituted-cyclopent-2-enone or 2-substituted-cyclohex-2-enone gives the desired depentyl prostaglandins.

    Conjugate addition of organocuprates generated from copper (I) cyanide and vinyl stannanes useful in prostaglandin analog synthesis
    10.
    发明授权
    Conjugate addition of organocuprates generated from copper (I) cyanide and vinyl stannanes useful in prostaglandin analog synthesis 失效
    从用于前列腺素类似物合成的氰化铜和乙烯基锡烷产生的有机碳酸盐的共轭加成

    公开(公告)号：US4543421A

    公开(公告)日：1985-09-24

    申请号：US493709

    申请日：1983-05-11

    申请人： Paul F. Corey ,  Harold C. Kluender

    发明人： Paul F. Corey ,  Harold C. Kluender

    IPC分类号： C07C67/00 ,  C07C401/00 ,  C07C405/00 ,  C07F7/18 ,  C07F7/22 ,  C07C177/00

    CPC分类号： C07F7/2212 ,  C07C405/00 ,  C07C405/0016 ,  C07C405/0025 ,  C07F7/1852 ,  C07F7/1856

    摘要： An improved method for the preparation of prostaglandin analogs which comprises preparation of two equivalents of an alkyl or alkenyl lithium reagent in an aprotic solvent mixture such as pentane or hexane and tetrahydrofuran, conversion of said reagent by addition of 1 equivalent of copper (I) cyanide to a copper reagent, conversion of said copper reagent to the blocked prostaglandin analog by the addition of a 2-alkylcyclopent-2-en-1-one reagent and quenching of the resultant reaction mixture with aprotic media or an active acylating agent and finally optionally deblocking the resultant product is disclosed. This method is an improvement over previous methods in that more modest temperatures and less hazardous and/or less complex reagents are used and in that for some analogs the method is shorter than previous methods.

    摘要翻译： 一种用于制备前列腺素类似物的改进方法，其包括在非质子溶剂混合物如戊烷或己烷和四氢呋喃中制备两当量的烷基或烯基锂试剂，所述试剂通过加入1当量的氰化铜（I） 通过加入2-烷基环戊-2-烯-1-酮试剂将所述铜试剂转变成封闭的前列腺素类似物，并用非质子介质或活性酰化剂淬灭所得反应混合物，最后任选地 公开了解结果产物。 该方法是对以前的方法的改进，因为使用更温和的温度和更少的危险和/或较不复杂的试剂，并且对于一些类似物，该方法比先前的方法更短。