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305 条记录 (耗时 0.021 秒)

    TRI-SUBSTITUTED PHENYL DERIVATIVES USEFUL AS PDE IV INHIBITORS
    91.
    发明公开
    TRI-SUBSTITUTED PHENYL DERIVATIVES USEFUL AS PDE IV INHIBITORS 失效
    用作PDE IV抑制剂三取代苯基衍生物

    公开(公告)号：EP0766670A1

    公开(公告)日：1997-04-09

    申请号：EP95922640.0

    申请日：1995-06-22

    申请人： CELLTECH THERAPEUTICS LIMITED

    发明人： HEAD, John, Clifford ,  WARRELLOW, Graham, John ,  ALEXANDER, Rikki, Peter

    IPC分类号： A61K31 ,  A61P11 ,  A61P29 ,  A61P43 ,  C07C43 ,  C07C57 ,  C07C69 ,  C07C205 ,  C07C227 ,  C07C229 ,  C07C233 ,  C07C327 ,  C07D213

    CPC分类号： C07D213/30 ,  C07D213/32 ,  C07D213/38

    摘要： Compounds of general formula (1) are described wherein =W- is (1) =C(Y)- where Y is a halogen atom, or an alkyl or -XRa group where X is -O-, -S(O)¿m?-[where m is zero or an integer of value 1 or 2], or -N(R?b¿)- where Rb is a hydrogen atom or an optionally substituted alkyl group or, (2) =N; L is a -XR, [where R is an optionally substituted alkyl, alkenyl, cycloalkyl or cycloalkenyl group], -C(R?11)=C(R1)(R2¿) or [-CH(R11)]nCH(R1)(R2) group where R11 is a hydrogen or a fluorine atom or a methyl group, and R?1 and R2¿, which may be the same or different, is each a hydrogen or fluorine atom or an optionally substituted alkyl, alkenyl, alkynyl, alkoxy, alkylthio, -CO¿2 R?8, [where R8 is a hydrogen atom or an optionally substituted alkyl, aralkyl, or aryl group], -CONR9R10 [where R?9 and R10¿, which may be the same or different are as defined for R8], -CSNR9R10, -CN or -NO¿2?group, or R?1 and R2¿ together with the C atom to which they are attached are linked to form an optionally substituted cycloalkyl or cycloalkenyl group and n is zero or the integer 1; Z is (1) a group -C(R?3)(R4)C(R5)(R6)(R7) or -C(R?4)=C(R5)(R6¿) where R3 is a hydrogen or a fluorine atom or an optionally substituted straight or branched alkyl group; R4 is a group selected from -XaL1R12 [where Xa is as defined above for X, L1 is a linker group and R12 is a hydrogen atom or a cycloaliphatic, heterocycloaliphatic, or monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms], -Alk1R12 [where Alk1 is an optionally substituted straight or branched alkenyl or alkynyl chain optionally containing one or more -O- or -S- atoms or -N(Rb)-, carbocyclic or heteroatom-containing groups], -CH¿2L?1R12a [where R12a is as defined for R12 but is not a hydrogen atom]; -XaR12a; or -C(Xb)R12a [where Xb is an oxygen or sulphur atom]; R5 is a -(CH¿2?)pAr group where p is zero or an integer 1, 2 or 3 and Ar is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms; R?6¿ is a hydrogen or a fluorine atom or an optionally substituted alkyl group; R7 is a hydrogen or a fluorine atom or an ORc group where Rc is a hydrogen atom or an optionally substituted alkyl or alkenyl group, or an alkoxyalkyl, alkanoyl, formyl, carboxamido or thiocarboxamido group; or Z is (2) a group -C(R?4)C(R5)(R6)(R7¿) where R4 is a group =CH¿2?, or =CH(L?1)¿n-R12; and the salts, solvates, hydrates, prodrugs and N-oxides thereof. Compounds according to the invention are phosphodiesterase type IV inhibitors and are useful in the prophylaxis and treatment of disease such as asthma where an unwanted inflammatory response or muscular spasm is present.

    Naphthoic acid derivative
    92.
    发明公开
    Naphthoic acid derivative 失效
    Naphtoesäure - 衍生金融工具。

    公开(公告)号：EP0492178A2

    公开(公告)日：1992-07-01

    申请号：EP91120553.2

    申请日：1991-11-29

    申请人： FUJIREBIO INC.

    发明人： Sekine, Yasuo ,  Yamaura, Tetsuaki ,  Nishimura, Masato, Fuji Rebio Hachiojiryo ,  Kojima, Eri ,  Emoto, Yasuko ,  Higashide, Yasushi

    IPC分类号： C07D333/18 ,  C07D207/12 ,  C07D295/12 ,  C07D213/32 ,  C07D213/38 ,  C07D211/46 ,  C07D213/30 ,  C07D307/38 ,  C07D401/12 ,  A61K31/38 ,  A61K31/40

    CPC分类号： C07D213/30 ,  C07D211/46 ,  C07D211/54 ,  C07D213/32 ,  C07D213/38 ,  C07D295/13 ,  C07D307/38 ,  C07D317/56 ,  C07D333/18 ,  C07D333/28 ,  C07D401/12

    摘要： A naphthoic acid derivative represented by the following general formula or a salt thereof:
    wherein R i , R 2 and R 3 are each independently a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group, a lower alkoxy group, a lower alkanoyloxy group, a hydroxy-lower alkyl group, a lower alkoxy-lower alkyl group, a lower alkanoyloxy-lower alkyl group or an aralkyloxy group;

    R 4 is a hydrogen atom or a lower alkyl group;
    R 5 is a substituted or unsubstituted aryl group or a substituted or unsubstituted heteroaromatic group;
    X is a group

    a cycloalkylene group, a bivalent nitrogen-containing heterocyclic group, or a group


    -R 8 - NH- or -NH-R 8 , where R 6 and R 7 are each a hydrogen atom or a lower alkyl group and R 8 is a cycloalkylene group, or R 6 and R 7 , together with R 4 , may form an alkylene group of 1-3 carbon atoms;
    Y is -S(O)p-, -(CH 2 ) n - or -0-;
    Z is a substituted or unsubstituted alkylene group or a single bond;
    ℓ is an integer of 0-4;
    m is an integer of 0-8;
    n is 0 or 1;
    p is an integer of 0-2; and
    g is 0 or 1.
    The compound is useful as an antiallergic agent.

    摘要翻译： 由以下通式表示的萘甲酸衍生物或其盐：其中R 1，R 2和R 3各自独立地为氢原子，卤素原子，羟基，低级烷基，低级烷氧基， 低级烷酰氧基，羟基低级烷基，低级烷氧基 - 低级烷基，低级烷酰氧基 - 低级烷基或芳烷氧基; R4是氢原子或低级烷基; R5是取代或未取代的芳基或取代或未取代的杂芳基; X为环状亚烷基，二价含氮杂环基，或基团 -R8-NH-或-NH-R8，其中R6和R7各自为氢原子或低级烷基 并且R 8为亚环烷基，或者R 6和R 7与R 4一起可以形成1-3个碳原子的亚烷基; Y是-S（O）对 - ， - （CH 2）n - 或-O-; Z是取代或未取代的亚烷基或单键; l是0-4的整数; m为0-8的整数; n为0或1; p是0-2的整数; 并且g为0或1.该化合物可用作抗过敏剂。

    Ethanolamine derivates, processes for their preparation and pharmaceutical compositions containing them
    95.
    发明公开
    Ethanolamine derivates, processes for their preparation and pharmaceutical compositions containing them 失效
    乙酰胺衍生物，其制备方法和含有它们的药物组合物

    公开(公告)号：EP0286242A3

    公开(公告)日：1989-08-09

    申请号：EP88302151.1

    申请日：1988-03-11

    申请人： GLAXO GROUP LIMITED

    发明人： Skidmore, Ian Frederick ,  Finch, Harry ,  Mitchell, William Leonard ,  Naylor, Alan ,  Lunts, Lawrence Henry ,  Hartley, David

    IPC分类号： C07C93/08 ,  C07C149/32 ,  C07C143/75 ,  C07C127/17 ,  C07C103/76 ,  C07D213/65 ,  C07D215/52 ,  A61K31/10 ,  A61K31/135 ,  A61K31/165

    CPC分类号： C07D213/30 ,  C07D213/32 ,  C07D213/63

    摘要： This invention relates to compounds of the general formula (I)
    and physiologically acceptable salts and solvates thereof where Ar represents
    where
    R 3 is a bond or a straight or branched C 1 2 alkylene group, R 4 is a hydroxy group or a group R 5 NH-where R 5 represents a group CH 3 SO 2 -, HCO-or NH 2 CO-,
    where R 6 is a chlorine atom or the group F 3 C-,
    k represents an integer from 1 to 8, m represents zero or an integer from 2 to 7 and n represents an integer from 2 to 7 with the proviso that the sum total of k. m and n is 4 to 12; R 1 and R 2 each represents a hydrogen atom or a methyl or ethyl group with the proviso that the sum total of carbon atoms in R 1 and R 2 is not more than 2; R 30 represents hydrogen or C 12 alkyl; X represents an oxygen or sulphur atom: and Y and Q may each represent a bond or an oxygen or sulphur atom with the provisos that at least one of Y and Q represents an oxygen or sulphur atom and when Y is a bond m is zero, or when Y represents an oxygen or sulphur atom m is an integer from 2 to 7: P represents a phenyl group otionally substituted by one or more substituents selected from halogen atoms, or the groups C 1 3 alkyl, C 1 3 alkoxy, hydroxy, -CH 2 OH-, -(CH 2 ) 2 OH, -CO 2 H. -CO 2 CH 3 , ·CO 2 (CH 2 )- 2 CH 3 , -R 7 , COR 7 , -NHCOR s and ·NR 9 SO 2 R 10 ; where R 7 represents an amino, aminoC 1 3 alkyl, aminoC, 3 dialkyl, pyrrolidino. piperidino. hexamethyleneimino, piperazino, N-methylpiperazino or morpholino group; R 8 represents a hydrogen atom or a C, 4 alkyl, C, 4 alkoxy, phenyl or amino group; R 9 represents a hydrogen atom or a methyl group; R 10 represents a methyl, phenyl, amino or dimethylamino group;
    or P represents a pyridyl group optionally substituted by one or two substitutents selected from halogen atoms or hydroxy, C, 3 alkyl and C 1 3 alkoxy groups. The compounds have a stimulant action at β 2 -adrenoreceptors and are useful, in particular, in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.

    Process for preparing intermediate products and their use for preparing cephem compounds
    99.
    发明公开
    Process for preparing intermediate products and their use for preparing cephem compounds 失效
    一种用于中间化合物的制备方法以及它们用于生产头孢烯化合物的使用过程中。

    公开(公告)号：EP0231475A1

    公开(公告)日：1987-08-12

    申请号：EP86116828.4

    申请日：1982-09-13

    申请人： FUJISAWA PHARMACEUTICAL CO., LTD.

    发明人： Teraji, Tsutomu ,  Sakane, Kazuo ,  Goto, Jiro

    IPC分类号： C07D285/00 ,  C07D501/20

    CPC分类号： C07D213/30 ,  C07D213/32 ,  C07D213/68 ,  C07D213/70 ,  C07D213/74 ,  C07D285/08 ,  C07D401/12 ,  Y02P20/55

    摘要： A process for preparing a compound of the formula :
    wherein

    R 2 is lower aliphatic hydrocarbon group which may be substituted with suitable substituent(s), cyclo(lower)alkyl or cyclo(lower)alkenyl; or a salt thereof, which comprises reacting a compound of the formula :

    wherein

    R 2 is as defined above and
    Y is halogen,
    or a salt thereof, with a salt of HSCN.
    The obtained compounds are intermediates which can be used for preparing cephem compounds.

    摘要翻译： 一种制备下式化合物的方法： worinř<2>是可以substituiertem与合适的取代基（多个），环（低级）烷基或环（低级）链烯基的低级脂族烃基; 或其盐，该方法包括使下式的化合物：卤素worinř<2>如上所定义，Y是，或它们的盐，与HSCN的盐。 将所得到的化合物是可用于制备头孢烯化合物的中间体。