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    LEUKOTRIEN-B 4?-DERIVATE, INSBESONDERE 7-METHYLCYCLOHEXYL-LTB 4?-ANTAGONISTEN
    2.
    发明公开
    LEUKOTRIEN-B 4?-DERIVATE, INSBESONDERE 7-METHYLCYCLOHEXYL-LTB 4?-ANTAGONISTEN 失效
    白三烯B 4？衍生物尤其是7-甲基环己基LTB4？拮抗剂

    公开(公告)号：EP0983234A1

    公开(公告)日：2000-03-08

    申请号：EP98928323.9

    申请日：1998-05-22

    申请人： Schering Aktiengesellschaft

    发明人： BUCHMANN, Bernd ,  FRÖHLICH, Wolfgang ,  GIESEN, Claudia ,  HENNEKES, Hartwig ,  JAROCH, Stefan ,  SKUBALLA, Werner

    IPC分类号： C07C405/00

    CPC分类号： C07C405/0066 ,  C07C405/00

    摘要： The invention relates to leukotriene B4 derivatives of general formula (I) in which R1 stands for CH2OH, CH3, CF3, COOR4, CONR5R6; R2 stands for H or an organic acid radical with 1-15 C atoms; R3 stands for H; R4 is hydrogen, C1-C10-alkyl, C3-C10-cycloalkyl, a C6-C10-aryl radical optionally substituted by 1-3 halogen, phenyl, C1-C4-alkyl, C1-C4-alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carboxyl or hydroxy, or CH2-CO-(C6-C10) aryl, or a 5-6 link ring with at least 1 heteroatom; A is a trans-, trans-CH=CH-CH=CH, a -CH2CH2-CH=CH- or a tetramethylene group; B is a C1-C10 linear or branched-chain aklylene group or the group (a) or (b); D is a direct bonding, oxygen, sulphur, -C C-, -CH=CR7, or a direct bonding with B. The invention also relates to salts thereof, having physiologically compatible bases and their cyclodextrin clathrates. The inventive substances can be used as pharmaceutical preparations.

    Prostaglandins
    6.
    发明公开
    Prostaglandins 失效
    前列腺素。

    公开(公告)号：EP0043292A2

    公开(公告)日：1982-01-06

    申请号：EP81303000.4

    申请日：1981-07-01

    申请人： NATIONAL RESEARCH DEVELOPMENT CORPORATION

    发明人： Jones, Robert Leslie ,  Wilson, Norman Happer

    IPC分类号： C07C177/00 ,  C07D493/08 ,  C07C175/00 ,  C07C109/12 ,  C07C109/14 ,  C07C109/16 ,  C07C133/02 ,  C07C159/00 ,  C07C143/825 ,  C07C131/00 ,  A61K31/557

    CPC分类号： C07D493/08 ,  C07C45/305 ,  C07C45/44 ,  C07C47/225 ,  C07C47/47 ,  C07C57/26 ,  C07C251/72 ,  C07C403/20 ,  C07C405/0041 ,  C07C405/0066 ,  C07C405/0091 ,  C07C2601/16 ,  C07C47/198

    摘要： Novel compounds have a formula (I)
    wherein
    represents a bicyclo (2,2,1) hept-2Z-ene, bicyclo (2,2,1) heptane, 7-oxabicyclo (2,2,1) hept-2Z-ene, 7-oxabicyclo (2,2,1) heptane, bicyclo (2,2,2) oct-2Z-ene or bicyclo (2,2,2) octane substituted at the 5-position by the group R 1 and at the 6-position by the group C(R 2 )=NR, a 6,6-dimethyl-bicyclo (3,1,1) heptane substituted at the 5- position by the group R' and at the 6-position by the group C(R 2 )=NR or at the 5-position by the group C(R 2 )=NR and at the 6-position by the group R 1 , a cyclohex-1-ene or cyclohexane substituted at the 4-position by the group R 1 and at the 5-position by the group C(R 2 )=NR, or a 1-hydroxycyclopentane substituted at the 2-position by the group R 1 and at the 2-position by the group C(R 2 )=NR, R 1 is a 6-carboxyhex-2-enyl group or a modification thereof as defined herein, R 2 is hydrogen, an aliphatic hydrocarbon group or an aliphatic hydrocarbon group substituted directly or through an oxygen or sulphur atom by an aromatic group, and R is a group -OR 3 , -OR 4 , -A-R 3 or -N=R 5 in which A is -NH-, -NH.CO-, -NH.CO.CH 2 N(R 6 )-, -NH.SO 2 -, -NH.CO.NH or -NH.CS.NH- and wherein R 3 is an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted directly or through an oxygen or sulphur atom by an aromatic group, R 4 is an aliphatic hydrocarbon group which is substituted through an oxygen atom by an aliphatic hydrocarbon group which is itself substituted by an aromatic group, R 5 is an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted directly or through an oxygen or sulphur atom by an aromatic group, and R 6 is hydrogen, an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted directly or through an oxygen or sulphur atom by an aromatic group, with the proviso that when R is a group -OR 3 , -NH.COR 3 or-NH.CO.NHR3 then
    excludes bicyclo (2,2,1) hept-2Z-enes and bicyclo (2,2,1) heptanes. The compounds are of value for use in phar. maceutical compositions particularly in the context of the inhibition of thromboxane activity.

    摘要翻译： 新化合物具有式（I）表示双环[2,2,1]庚-2Z-烯，双环[2,2,1]庚烷，7-氧杂双环[2,2,1]庚-2 - 烯基，7-氧杂二环[2,2,1]庚烷，双环[2,2,2]辛-2Z-烯或在5位被基团R 1取代的双环[2,2,2]辛烷 并且在C（R 2）= NR基团的6位上，在5位被基团R 1取代的6,6-二甲基 - 双环[3,1,1]庚烷和 在C（R 2）= NR的6位上或在C（R 2）= NR的5位，在6位被基团R 1取代， 环己-1-烯或环基在4-位上被基团R 1取代，在5-位被C（R 2）= NR取代，或在2-位取代的1-羟基环戊烷 通过基团R 1和基团C（R 2）= NR的2-位，R 1是如本文所定义的6-羧基己-2-烯基或其修饰， 2>是氢，脂族烃基或直接取代或通过氧或者-SO取代的脂族烃基 R为-OR 3，-OR 4，-AR 3或-N = R 5的基团，其中A为-NH-，-CH .CO- ，-NH.CO.CH 2 N（R 6） - ， - NHSO 2 - ， - NH.CO.NH或-NH.CS.NH-，并且其中R 3是脂族烃基，芳族基团 或通过芳族基团直接或通过氧或硫原子取代的脂族烃基，R 4是被本身被芳基取代的脂族烃基通过氧原子取代的脂族烃基，R 5是由芳基直接取代或通过氧或硫原子取代的脂肪族烃基，芳香族基团或脂肪族烃基，R 6是氢，脂肪族烃基，芳香族基团或脂肪族烃基 烃基直接或通过芳族基团通过氧或硫原子取代，条件是当R为基团-OR 3，-NHCOR 3或-NH.CO.NHR 3时， CHEM>不包括双环[2,2,1]庚-2Z-en es和双环[2,2,1]庚烷。 这些化合物在药物组合物中是有用的，特别是在抑制血栓素活性的情况下。

    Prostaglandin intermediates
    8.
    发明公开
    Prostaglandin intermediates 失效
    前列腺素Zwischenprodukte

    公开(公告)号：EP0111955A1

    公开(公告)日：1984-06-27

    申请号：EP83201692.7

    申请日：1981-07-01

    申请人： NATIONAL RESEARCH DEVELOPMENT CORPORATION

    发明人： Jones, Robert Leslie ,  Wilson, Norman Happer

    IPC分类号： C07C69/738 ,  C07C69/732 ,  C07C59/80 ,  C07C59/74 ,  C07C59/46 ,  C07C59/205 ,  C07C59/147 ,  C07C59/11 ,  C07D493/08

    CPC分类号： C07D493/08 ,  C07C45/305 ,  C07C45/44 ,  C07C47/225 ,  C07C47/47 ,  C07C57/26 ,  C07C251/72 ,  C07C403/20 ,  C07C405/0041 ,  C07C405/0066 ,  C07C405/0091 ,  C07C2601/16 ,  C07C47/198

    摘要： Novel compounds have a formula (I)
    wherein
    represents a bicyclo [2,2,1] hept-2Z-ene, bicyclo [2,2,1] heptane, 7-oxabicyclo [2,2,1] hept-2Z-ene, 7-oxabicyclo [2,2,1] heptane, bicyclo [2,2,2] oct-2Z-ene or bicyclo [2,2,2] octane substituted at the 5-position by the group R' and at the 6-position by the group C(R 2 )=NR, a 6,6-dimethyl-bicyclo [3,1,1] heptane substituted at the 5-position by the group R' and at the 6-position by the group C(R 2 )=NR or at the 5-position by the group C(R 2 )=NR and at the 6-position by the group R', a cyclohex-1-ene or cyclohexane substituted at the 4-position by the group R 1 and at the 5-position by the group C(R 2 )=NR, or a 1-hydroxycyclopentane substituted at the 2-position by the group R 1 and at the 2-position by the group C(R 2 )=NR, R 1 is a 6-carboxyhex-2-enyl group or a modification thereof as defined herein, R 2 is hydrogen, an aliphatic hydrocarbon group or an aliphatic hydrocarbon group substituted directly or through an oxygen or sulphur atom by an aromatic group, and R is a group -OR 3 , -OR 4 , -A-R 3 or -N=R 5 in which A is -NH-, -CH.CO-, -NH.CO.CH 2 N(R 6 )-, -NH.S0 2 -, -NH.CO.NH or -NH.CS.NH-and wherein R 3 is an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted directly or through an oxygen or sulphur atom by an aromatic group, R 4 is an aliphatic hydrocarbon group which is substituted through an oxygen atom by an aliphatic hydrocarbon group which is itself substituted by an aromatic group, R 5 is an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted directly or through an oxygen or sulphur atom by an aromatic group, and R 6 is hydrogen, an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted directly or through an oxygen or sulphur atom by an aromatic group, with the proviso that when R is a group -OR 3 , - NH.COR 3 or -NH.CO.NHR 3 then
    excludes bicyclo [2,2,1] hept-2Z-enes and bicyclo [2,2,1] heptanes. The compounds are of value for use in pharmaceutical compositions particularly in the context of the inhibition of thromboxane activity.

    摘要翻译： 新化合物具有式（I）表示双环[2,2,1]庚-2Z-烯，双环[2,2,1]庚烷，7-氧杂双环[2,2,1]庚-2 - 烯基，7-氧杂二环[2,2,1]庚烷，双环[2,2,2]辛-2Z-烯或在5位被基团R 1取代的双环[2,2,2]辛烷 并且在C（R 2）= NR基团的6位上，在5位被基团R 1取代的6,6-二甲基 - 双环[3,1,1]庚烷和 在C（R 2）= NR的6位上或在C（R 2）= NR的5位，在6位被基团R 1取代， 环己-1-烯或环基在4-位上被基团R 1取代，在5-位被C（R 2）= NR取代，或在2-位取代的1-羟基环戊烷 通过基团R 1和基团C（R 2）= NR的2-位，R 1是如本文所定义的6-羧基己-2-烯基或其修饰， 2>是氢，脂族烃基或直接取代或通过氧或者-SO取代的脂族烃基 R为-OR 3，-OR 4，-AR 3或-N = R 5的基团，其中A为-NH-，-CH .CO- ，-NH.CO.CH 2 N（R 6） - ， - NHSO 2 - ， - NH.CO.NH或-NH.CS.NH-，并且其中R 3是脂族烃基，芳族基团 或通过芳族基团直接或通过氧或硫原子取代的脂族烃基，R 4是被本身被芳基取代的脂族烃基通过氧原子取代的脂族烃基，R 5是由芳基直接取代或通过氧或硫原子取代的脂肪族烃基，芳香族基团或脂肪族烃基，R 6是氢，脂肪族烃基，芳香族基团或脂肪族烃基 烃基直接或通过芳族基团通过氧或硫原子取代，条件是当R为基团-OR 3，-NHCOR 3或-NH.CO.NHR 3时， CHEM>不包括双环[2,2,1]庚-2Z-en es和双环[2,2,1]庚烷。 这些化合物在药物组合物中是有用的，特别是在抑制血栓素活性的情况下。

    Prostaglandins
    9.
    发明公开
    Prostaglandins 失效
    前列腺素

    公开(公告)号：EP0043292A3

    公开(公告)日：1982-12-15

    申请号：EP81303000

    申请日：1981-07-01

    申请人： NATIONAL RESEARCH DEVELOPMENT CORPORATION

    发明人： Jones, Robert Leslie ,  Wilson, Norman Happer

    IPC分类号： C07C177/00 ,  C07D493/08 ,  C07C175/00 ,  C07C109/12 ,  C07C109/14 ,  C07C109/16 ,  C07C133/02 ,  C07C159/00 ,  C07C143/825 ,  C07C131/00 ,  A61K31/557

    CPC分类号： C07D493/08 ,  C07C45/305 ,  C07C45/44 ,  C07C47/225 ,  C07C47/47 ,  C07C57/26 ,  C07C251/72 ,  C07C403/20 ,  C07C405/0041 ,  C07C405/0066 ,  C07C405/0091 ,  C07C2601/16 ,  C07C47/198

    摘要： Novel compounds have a formula (I)
    wherein
    represents a bicyclo (2,2,1) hept-2Z-ene, bicyclo (2,2,1) heptane, 7-oxabicyclo (2,2,1) hept-2Z-ene, 7-oxabicyclo (2,2,1) heptane, bicyclo (2,2,2) oct-2Z-ene or bicyclo (2,2,2) octane substituted at the 5-position by the group R 1 and at the 6-position by the group C(R 2 )=NR, a 6,6-dimethyl-bicyclo (3,1,1) heptane substituted at the 5- position by the group R' and at the 6-position by the group C(R 2 )=NR or at the 5-position by the group C(R 2 )=NR and at the 6-position by the group R 1 , a cyclohex-1-ene or cyclohexane substituted at the 4-position by the group R 1 and at the 5-position by the group C(R 2 )=NR, or a 1-hydroxycyclopentane substituted at the 2-position by the group R 1 and at the 2-position by the group C(R 2 )=NR, R 1 is a 6-carboxyhex-2-enyl group or a modification thereof as defined herein, R 2 is hydrogen, an aliphatic hydrocarbon group or an aliphatic hydrocarbon group substituted directly or through an oxygen or sulphur atom by an aromatic group, and R is a group -OR 3 , -OR 4 , -A-R 3 or -N=R 5 in which A is -NH-, -NH.CO-, -NH.CO.CH 2 N(R 6 )-, -NH.SO 2 -, -NH.CO.NH or -NH.CS.NH- and wherein R 3 is an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted directly or through an oxygen or sulphur atom by an aromatic group, R 4 is an aliphatic hydrocarbon group which is substituted through an oxygen atom by an aliphatic hydrocarbon group which is itself substituted by an aromatic group, R 5 is an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted directly or through an oxygen or sulphur atom by an aromatic group, and R 6 is hydrogen, an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted directly or through an oxygen or sulphur atom by an aromatic group, with the proviso that when R is a group -OR 3 , -NH.COR 3 or-NH.CO.NHR3 then excludes bicyclo (2,2,1) hept-2Z-enes and bicyclo (2,2,1) heptanes. The compounds are of value for use in phar. maceutical compositions particularly in the context of the inhibition of thromboxane activity.

    摘要翻译： 新化合物具有式（I）表示双环[2,2,1]庚-2Z-烯，双环[2,2,1]庚烷，7-氧杂双环[2,2,1]庚-2 - 烯基，7-氧杂二环[2,2,1]庚烷，双环[2,2,2]辛-2Z-烯或在5位被基团R 1取代的双环[2,2,2]辛烷 并且在C（R 2）= NR基团的6位上，在5位被基团R 1取代的6,6-二甲基 - 双环[3,1,1]庚烷和 在C（R 2）= NR基的6-位上或在C（R 2）= NR基的5位，在6位由基团R 1取代，a 环己-1-烯或环己基在4-位被基团R 1取代，在5-位被C（R 2）= NR取代，或在2-位取代的1-羟基环戊烷 通过基团R 1和基团C（R 2）= NR的2-位，R 1是如本文所定义的6-羧基己-2-烯基或其修饰， 2>是氢，脂族烃基或脂族烃基直接或通过氧或磺取代 R 1是-OR 3，-OR 4，-AR 3或-N = R 5，其中A是-NH-，-CH.CO- ，-NH.CO.CH 2 N（R 6） - ， - NHS 2 - ， - NH.CO.NH或-NH.CS.NH-，并且其中R 3是脂族烃基，芳族基团 或通过芳族基团直接或通过氧或硫原子取代的脂族烃基，R 4是脂族烃基，其被本身被芳基取代的脂族烃基经氧原子取代，R 5是脂肪族烃基，芳香族基团或脂肪族烃基，其被芳基直接或者被氧原子或硫原子取代，R 6是氢，脂肪族烃基，芳香族基团或脂肪族烃基 烃基直接或通过芳族基团通过氧或硫原子取代，条件是当R为基团-OR 3，-NHCOR 3或-NH.CO.NHR 3时， CHEM>不包括双环[2,2,1]庚-2Z-en es和双环[2,2,1]庚烷。 这些化合物在药物组合物中是有用的，特别是在抑制血栓素活性的情况下。

    Phenylalkan(en)oic acids with leukotriene B4 antagonistic activity
    10.
    发明公开
    Phenylalkan(en)oic acids with leukotriene B4 antagonistic activity 失效
    苯基（en）-Sauren mit白三烯B4拮抗剂Wirkung。

    公开(公告)号：EP0652208A1

    公开(公告)日：1995-05-10

    申请号：EP94118144.8

    申请日：1990-05-16

    申请人： ONO PHARMACEUTICAL CO., LTD.

    发明人： Konno, Mitoshi, Ono Pharmaceutical Co.,Ltd. ,  Nakae, Takahiko, Ono Pharmaceutical Co.,Ltd. ,  Hamanaka, Nobuyuki, Ono Pharmaceutical Co.,Ltd.

    IPC分类号： C07C233/54 ,  A61K31/16 ,  C07D209/08 ,  C07D277/42 ,  C07C323/19 ,  C07C235/16 ,  C07C311/21 ,  C07C235/20 ,  C07C235/34 ,  C07C235/78 ,  C07C59/68

    CPC分类号： C07C69/734 ,  C07C59/52 ,  C07C59/64 ,  C07C59/68 ,  C07C59/90 ,  C07C205/34 ,  C07C205/56 ,  C07C233/47 ,  C07C233/54 ,  C07C233/81 ,  C07C235/16 ,  C07C235/20 ,  C07C235/34 ,  C07C235/42 ,  C07C235/78 ,  C07C311/08 ,  C07C311/13 ,  C07C311/21 ,  C07C311/51 ,  C07C323/19 ,  C07C405/0066 ,  C07C2601/14 ,  C07D207/27 ,  C07D209/08 ,  C07D209/48 ,  C07D275/03 ,  C07D277/42 ,  C07D277/46 ,  C07D279/02 ,  C07D295/185

    摘要： The phenylalkan(en)oic acids of the formula:

    wherein A is

    i) ―NHCO―,
    ii) ―O―
    iii) ―NHSO₂―,
    iv) ―CO―
    v) ―CH₂― or
    vi) ―CH(OH)―;
    W is C1-13 alkylene;
    R¹ is

    i) hydrogen,
    ii) C1-4 alkyl,
    iii) ―COOH,
    iv) saturated or unsaturated, 4-7 membered mono-cyclic hetero ring containing one nitrogen as a hetero atom or saturated or unsaturated, 4-7 membered mono-cyclic hetero ring containing one nitrogen as a hetero atom substituted by an oxo group,
    v)

    vi) ―CH₂OH;
    A, taken together with W and R¹, is

    i)

    ii)

    iii) ―N―(SO₂R⁶)₂,
    iv)
    or
    v)

    two R² are, same or different,

    i) hydrogen,
    ii) C1-4 alkyl or
    iii) 4-7 membered, saturated or unsaturated, mono-cyclic hetero ring containing two or three of nitrogen and sulfur in total,
    or two R², taken together with a nitrogen to which they are attached, form saturated or unsaturated

    i) 7-14 membered, bi-or tri-cyclic hetero ring containing one nitrogen as a hetero atom, or
    ii) 4-7 membered, mono-cyclic hetero ring containing two or three of nitrogen and oxygen in total ;
    Y is ethylene or vinylene;
    D is

    i) ―Z―B or
    ii)

    Z is C3-11 alkylene or alkenylene
    B is

    or
    Z, taken together with B, is C3-22 alkyl;
    R³ is

    i) hydrogen,
    ii) halogen,
    III) C1-8 alkyl, alkoxy or alkylthio, or
    iv) C2-8 alkenyl, alkenyloxy or alkenylthio;
    n is 1-3;
    R⁴ is C1-7 alkylene;
    R⁵ is

    i) C1-12 alkyl,
    ii) C2-12 alkenyl,
    iii) C5-7 cycloalkyl or
    iv) phenethyl or phenethyl wherein the ring is substituted by one C1-4 alkoxy;
    two R⁶ are, same or different,

    i) C1-7 alkyl,
    ii) benzyl or
    iii) phenyl or phenyl wherein the ring is substituted by one C1-4 alkyl; and
    Two R⁷ are, same or different, C1-4 alkyl;
    with the proviso that
       ―A―W―R¹ should bind to 4- carbon in benzene ring, and
       and non-toxic salts thereof,
    possess an antagonism on leukotriene B₄, and therefore, are useful for the prevention and treatment of several diseases induced by leukotriene B₄.

    摘要翻译： 其中A是i）-NHCO-，ii）-O-iii）-NHSO 2 - ，iv）-CO-v）-CH 2 - 或vi）-CH（ 哦）-; W是C1-13亚烷基; R 1是i）氢，ii）C 1-4烷基，iii）-COOH，iv）饱和或不饱和的含有一个氮作为杂原子或饱和或不饱和的4-7元单环杂环， 含有一个氮作为被氧基取代的杂原子的7元单环杂环，v）vii）-CH 2 OH; A与W和R 1一起是i） ii） iii）-N-（SO 2 R 6）2，iv）CHEM或v） 2）相同或不同，i）氢，ii）C1-4烷基或iii）含有总数为2或3个氮和硫的4-7元饱和或不饱和的单环杂环，或两个R' 2，与其连接的氮一起形成饱和或不饱和的i）含有一个氮作为杂原子的7-14元，双或三环杂环，或ii）4-7元，单 总共含有两个或三个氮和氧的环状杂环; Y是乙烯或亚乙烯基; D是i）-Z-B或ii） Z是C 3-11亚烷基或亚烯基B是CHEM或Z与B一起是C3-22烷基; R 3是i）氢，ii）卤素，III）C 1-8烷基，烷氧基或烷硫基，或iv）C 2-8链烯基，烯氧基或烯硫基; n为1-3; R 4是C 1-7亚烷基; R 5是i）C 1-12烷基，ii）C 2-12烯基，iii）C 5-7环烷​​基或iv）苯乙基或苯乙基，其中该环被一个C 1-4烷氧基取代; 两个R 6相同或不同，i）C 1-7烷基，ii）苄基或iii）苯基或苯基，其中该环被一个C 1-4烷基取代; 和两个R 7相同或不同，为C 1-4烷基; 条件是-AWR <1>应该与苯环中的4-碳和其无毒盐结合，对白三烯B4具有拮抗作用，因此可用于预防和治疗由白三烯诱导的几种疾病 B4。