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    Certain indole derivatives useful as leukotriene antagonists
    1.
    发明授权
    Certain indole derivatives useful as leukotriene antagonists 失效
    某些吲哚衍生物可用作白三烯拮抗剂

    公开(公告)号：US5281593A

    公开(公告)日：1994-01-25

    申请号：US54914

    申请日：1993-04-29

    Applicant: Jeremy Gilmore ,  Alec Todd

    Inventor： Jeremy Gilmore ,  Alec Todd

    IPC: C07D401/10 ,  C07D401/14 ,  C07D417/14 ,  A61K31/47 ,  C07D401/12

    CPC classification number: C07D401/14 ,  C07D401/10 ,  C07D417/14

    Abstract: A compound of the formula ##STR1## in which R.sup.1 is hydrogen, halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, nitrile, optionally protected carboxy, optionally protected tetrazolyl, trihalomethyl, hydroxy-C.sub.1-4 alkyl, aldehydo, --CH.sub.2 Z, --CH.dbd.CH--Z or --CH.sub.2 CH.sub.2 Z where Z is optionally protected carboxy or optionally protected tetrazolyl; R.sup.2 is halo, nitrile, an optionally protected acid group or --CONR.sup.7 R.sup.8 where R.sup.7 and R.sup.8 are each hydrogen or C.sub.1-4 alkyl; R.sup.3 and R.sup.4 are each hydrogen, C.sub.1-4 alkyl, optionally substituted phenyl, or C.sub.1-4 alkyl substituted by --CONR.sup.7 R.sup.8 or an optionally protected acid group; R.sup.5 is ##STR2## where W is --CH.dbd.CH--, --CH.dbd.N--, --N.dbd.CH--, --O-- or --S--, R.sup.9 is hydrogen, halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or trihalomethyl, and R.sup.10 is hydrogen, C.sub.1-4 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.1-4 alkyl-C.sub.3-6 cycloalkyl; R.sup.6 is hydrogen or C.sub.1-4 alkyl; X is --O--(CH.sub.2).sub.n CR.sup.11 R.sup.12, --CR.sup.11 R.sup.12 --, --CR.sup.11 R.sup.12.(CH.sub.2).sub.n.CR.sup.13 R.sup.14 -- or --CR.sup.11 .dbd.CR.sup.12 -- where R.sup.11, R.sup.12, R.sup.13 and R.sup.14 are each hydrogen or C.sub.1-4 alkyl, and n is 0, 1 or 2; and Y is --O--CR.sup.15 R.sup.16 --, --CR.sup.15 .dbd.CR.sup.16 -- or --CR.sup.15 R.sup.16.CR.sup.17 R.sup.18 -- where R.sup.15, R.sup.16, R.sup.17 and R.sup.18 are each hydrogen or C.sub. 1-4 alkyl; or a salt thereof. The compounds in unprotected form are active as leukotriene antagonists.

    Abstract translation: 其中R 1为氢，卤素，C 1-4烷基，C 1-4烷氧基，腈，任意保护的羧基，任意保护的四唑基，三卤代甲基，羟基-C 1-4烷基，醛，-CH 2 Z， -CH = CH-Z或-CH 2 CH 2 Z，其中Z为任选保护的羧基或任选保护的四唑基; R 2是卤素，腈，任意保护的酸基或-CONR 7 R 8，其中R 7和R 8各自是氢或C 1-4烷基; R 3和R 4各自为氢，C 1-4烷基，任选取代的苯基或被-CONR 7 R 8或任选保护的酸基取代的C 1-4烷基; R5是 其中W是-CH = CH-，-CH = N-，-N = CH-，-O-或-S-，R9是氢，卤素，C1-4烷基，C1- 4烷氧基或三卤甲基，R 10是氢，C 1-4烷基，C 2-6烯基，C 3-6环烷基或C 1-4烷基-C 3-6环烷基; R6是氢或C1-4烷基; X是-O-（CH 2）n CR 11 R 12，-CR 11 R 12 - ， - CR 11 R 12。（CH 2）n CR 1 R 14 - 或-CR 11 = CR 12 - ，其中R 11，R 12，R 13和R 14各自是氢或C 1-4烷基，n是 0，1或2; 并且Y是-O-CR 15 R 16 - ， - CR 15 = CR 16 - 或-CR 15 R 16 CR 17 R 18 - ，其中R 15，R 16，R 17和R 18各自是氢或C 1-4烷基; 或其盐。 未保护形式的化合物作为白三烯拮抗剂是活性的。

    Dimeric oxazole derivatives
    2.
    发明授权
    Dimeric oxazole derivatives 失效
    二聚恶唑衍生物

    公开(公告)号：US4216219A

    公开(公告)日：1980-08-05

    申请号：US10185

    申请日：1979-02-07

    Applicant: William J. Ross ,  Alec Todd

    Inventor： William J. Ross ,  Alec Todd

    IPC: C07D263/48 ,  A61K31/42

    CPC classification number: C07D263/48

    Abstract: Novel compounds are described of the formula ##STR1## where R is C.sub.2-6 alkyl, R.sup.1 and R.sup.2 are hydrogen or C.sub.1-4 alkyl and n is 3 to 6. The compounds are useful in the prophylactic treatment of immediate hypersensitivity diseases including asthma.

    Abstract translation: 描述了新颖的化合物，其中R为C 2-6烷基，R 1和R 2为氢或C 1-4烷基，n为3至6.式的化合物。该化合物可用于预防性治疗包括哮喘在内的立即超敏反应疾病。

    SRS-A antagonists
    5.
    发明授权
    SRS-A antagonists 失效
    SRS-A拮抗剂

    公开(公告)号：US4513005A

    公开(公告)日：1985-04-23

    申请号：US386570

    申请日：1982-06-09

    Applicant: Stephen R. Baker ,  William B. Jamieson ,  William J. Ross ,  Alec Todd

    Inventor： Stephen R. Baker ,  William B. Jamieson ,  William J. Ross ,  Alec Todd

    IPC: C07B45/04 ,  C07C317/46 ,  C07C323/22 ,  C07C323/56 ,  C07C323/58 ,  C07D303/40 ,  C07D303/42 ,  C07D307/38 ,  C07D309/12 ,  C07D309/30 ,  C07D313/04 ,  C07F9/53 ,  C07K5/06 ,  C07C149/20 ,  A61K31/23 ,  A61K31/335

    CPC classification number: C07D307/38 ,  C07B45/04 ,  C07C317/46 ,  C07C323/22 ,  C07C323/56 ,  C07C323/58 ,  C07D303/40 ,  C07D303/42 ,  C07D309/12 ,  C07D309/30 ,  C07D313/04 ,  C07F9/5304 ,  C07F9/5325 ,  C07K5/06034

    Abstract: There are described pharmacologically active compounds, useful in the treatment of allergic/inflammatory disorders involving SRS-A as causal mediator and which, in free acid form, are of formula I, ##STR1## in which R.sub.1 is (i) an aliphatic, saturated or unsaturated hydrocarbyl radical of up to 20 carbon atoms, unsubstituted or substituted by at least one substituent selected from halogen, hydroxy, C.sub.3-6 alkoxy, C.sub.3-6 cycloalkyl, aryl or heteroaryl, the cycloalkyl, aryl or heteroaryl being unsubstituted or substituted by at least one substituent selected from hydroxy, halogen and alkyl, alkenyl or alkynyl of up to 10 carbon atoms,(ii) cycloalkyl of 3 to 8 carbon atoms unsubstituted or substituted by alkyl, alkenyl or alkynyl of up to 16 carbon atoms, or(iii) aryl or heteroaryl, unsubstituted or substituted by hydroxyl, C.sub.1-4 alkoxy, halogen or alkyl, alkenyl or alkynyl of up to 16 carbon atoms; and R.sub.2 is(i) alkyl, cycloalkyl or alkenyl of up to 10 carbon atoms, unsubstituted or substituted by one or more substituents selected from aryl, cycloalkyl, halogen, hydroxy, NHR.sub.3 and COX, where R.sub.3 is H, C.sub.1-4 alkyl, aryl or an amino acid residue or COX, and X is OH, C.sub.1-4 alkyl, NH.sub.2 or an amino acid residue, or(ii) aryl or heteroaryl, unsubstituted or substituted by one or more substituents selected from C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.2-5 acyl, halogen, hydroxy, carboxy, nitro, trihalomethyl, phenyl, C.sub.1-4 acylamino and NHR.sub.4, where R.sub.4 is hydrogen or C.sub.1-4 alkyl; and Y is --S--, --SO-- or --SO.sub.2 --,with the proviso that when --YR.sub.2 is glutathionyl, cysteinyl or cysteinylglycinyl, then R.sub.1 is other than an unsubstituted alkatetraenyl or alkapentaenyl radical of 12 to 16 carbon atoms.

    Abstract translation: 描述了用于治疗涉及SRS-A作为因果介质的过敏性/炎症性疾病，其游离酸形式为式I的化学活性化合物，其中R 1是（i）脂族， 至少20个碳原子的饱和或不饱和烃基，未被取代或被至少一个选自卤素，羟基，C 3-6烷氧基，C 3-6环烷基，芳基或杂芳基的取代基取代，环烷基，芳基或杂芳基是未取代或取代的 至少一个选自羟基，卤素和至多10个碳原子的烷基，烯基或炔基的取代基，（ii）未被取代或被至多16个碳原子的烷基，烯基或炔基取代的3至8个碳原子的环烷基，或 （iii）未被取代或被羟基，C 1-4烷氧基，卤素或至多16个碳原子的烷基，链烯基或炔基取代的芳基或杂芳基; 并且R 2是（i）至少10个碳原子的烷基，环烷基或链烯基，未被取代或被一个或多个选自芳基，环烷基，卤素，羟基，NHR 3和COX的取代基取代，其中R 3是H，C 1-4烷基， 芳基或氨基酸残基或COX，X为OH，C 1-4烷基，NH 2或氨基酸残基，或（ii）未被取代或被一个或多个选自C 1-4烷基，C 1 -4-烷氧基，C 2-5酰基，卤素，羟基，羧基，硝基，三卤甲基，苯基，C 1-4酰基氨基和NHR 4，其中R 4是氢或C 1-4烷基; 并且Y是-S-，-SO-或-SO 2 - ，条件是当-YR 2是谷胱甘肽基，半胱氨酰基或半胱氨酰甘氨酰基时，则R 1不同于未被取代的具有12至16个碳原子的烷基四烯基或烷基五烯基。

    5-Substituted pyranone compounds and their use as pharmaceuticals to treat an immediate hypersensitivity condition
    6.
    发明授权
    5-Substituted pyranone compounds and their use as pharmaceuticals to treat an immediate hypersensitivity condition 失效
    5-取代的吡喃酮化合物及其用作药物以治疗立即超敏反应的病症

    公开(公告)号：US4364956A

    公开(公告)日：1982-12-21

    申请号：US303307

    申请日：1981-09-17

    Applicant: Barry P. Clark ,  William J. Ross ,  Alec Todd

    Inventor： Barry P. Clark ,  William J. Ross ,  Alec Todd

    IPC: A61K31/35 ,  A61K31/351 ,  A61P9/12 ,  A61P11/06 ,  A61P37/08 ,  C07D309/38 ,  C07D309/40 ,  C07D405/04 ,  C07D405/12 ,  A61K31/34 ,  C07D309/32

    CPC classification number: C07D309/38 ,  C07D309/40

    Abstract: Compounds are described of the formula ##STR1## in which R.sup.1 is COOR.sup.5, CONHR.sup.5, cyano, 5-tetrazolyl or 5-tetrazolylaminocarbonyl, where R.sup.5 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen or C.sub.1-6 alkyl; R.sup.3 is a group of the formulaR.sup.6 --(Z).sub.m --where m is O or 1, Z is O, S, SO, SO.sub.2 or CO, and R.sup.6 phenyl optionally substituted by one or more group selected from halogen, C.sub.1-4 alkyl, C.sub.3-6 cycloalkyl, C.sub.1-4 alkoxy, benzyloxy, hydroxy, nitro, C.sub.1-4 alkylthio, C.sub.1-4 alkylsulphinyl, C.sub.1-4 alkylsulphonyl, amino and NHR.sup.7 where R.sup.7 is C.sub.2-6 acyl; and R.sup.4 is hydrogen, C.sub.1-6 alkyl or halogen; and salts thereof. These compounds have pharmaceutical properties and in particular are useful in the treatment of immediate hypersensitivity conditions such as asthma.

    Abstract translation: 其中R 1是COOR 5，CONHR 5，氰基，5-四唑基或5-四唑基氨基羰基，其中R 5是氢或C 1-6烷基; R2是氢或C1-6烷基; R3是式R6-（Z）m-的基团，其中m是O或1，Z是O，S，SO，SO2或CO，R6任选地被一个或多个选自卤素，C 1-4的基团取代 烷基，C 3-6环烷基，C 1-4烷氧基，苄氧基，羟基，硝基，C 1-4烷硫基，C 1-4烷基亚磺酰基，C 1-4烷基磺酰基，氨基和NHR 7，其中R 7为C 2-6酰基; R4为氢，C1-6烷基或卤素; 及其盐。 这些化合物具有药物性质，特别是可用于治疗立即超敏反应病症如哮喘。

    6-Substituted pyranone compounds and their use as pharmaceuticals
    7.
    发明授权
    6-Substituted pyranone compounds and their use as pharmaceuticals 失效
    6-取代的吡喃酮化合物及其作为药物的用途

    公开(公告)号：US4304728A

    公开(公告)日：1981-12-08

    申请号：US134385

    申请日：1980-03-27

    Applicant: Barry P. Clark ,  William J. Ross ,  Alec Todd

    Inventor： Barry P. Clark ,  William J. Ross ,  Alec Todd

    IPC: A61K31/35 ,  A61K31/351 ,  A61P11/06 ,  A61P37/08 ,  C07D309/38 ,  C07D309/40 ,  C07D405/04 ,  C08H3/00 ,  C07C143/67 ,  C07C143/90 ,  C07C149/40

    CPC classification number: C07D309/40 ,  C07D309/38 ,  Y10S514/826

    Abstract: Compounds are described of the formula ##STR1## in which R.sup.1 is COOR.sup.5, CONHR.sup.5, cyano, 5-tetrazolyl or R.sup.6, where R.sup.5 is hydrogen or C.sub.1-8 alkyl and R.sup.6 is phenyl or naphthyl, the phenyl or naphthyl group being optionally substituted by one or more group selected from halogen, C.sub.1-6 alkyl, C.sub.1-4 alkoxy, hydroxy, benzyloxy, nitro, trifluoromethyl, carboxyl, C.sub.1-4 alkylsulphinyl, C.sub.1-4 alkylsulphonyl, N(R.sup.5).sub.2, NHCOR.sup.5 and SR.sup.5 ; R.sup.2 is R.sup.6 or --CH.dbd.CH--R.sup.6 when R.sup.1 is COOR.sup.5, CONHR.sup.5, cyano or 5-tetrazolyl, or R.sup.2 is --CH.dbd.CH--R.sup.6 when R.sup.1 is R.sup.6 ; R.sup.3 is hydrogen, C.sub.1-6 alkyl, halogen, hydroxy or --OCH.sub.2 R.sup.6 ; and R.sup.4 is hydrogen, C.sub.1-6 alkyl or halogen; and salts thereof. The compounds have pharmaceutical properties and in particular are useful in the treatment of immediate hypersensitivity conditions such as asthma.

    Abstract translation: 描述式为“IMAGE”的化合物，其中R 1为COOR 5，CONHR 5，氰基，5-四唑基或R 6，其中R 5为氢或C 1-8烷基，R 6为苯基或萘基，苯基或萘基任选被 一个或多个选自卤素，C 1-6烷基，C 1-4烷氧基，羟基，苄氧基，硝基，三氟甲基，羧基，C 1-4烷基亚磺酰基，C 1-4烷基磺酰基，N（R 5）2，NHCOR 5和SR 5; 当R1为COOR5，CONHR5，氰基或5-四唑基时，R2为R6或-CH = CH-R6，或当R1为R6时R2为-CH = CH-R6; R3是氢，C1-6烷基，卤素，羟基或-OCH2R6; R4为氢，C1-6烷基或卤素; 及其盐。 这些化合物具有药物性质，特别是可用于治疗立即超敏反应病症如哮喘。

    Compound containing tetrazolyl groups and their use for treating allergies and cardiovascular disease
    10.
    发明授权
    Compound containing tetrazolyl groups and their use for treating allergies and cardiovascular disease 失效
    含有四唑基的化合物及其用于治疗过敏和心血管疾病的用途

    公开(公告)号：US4886885A

    公开(公告)日：1989-12-12

    申请号：US262754

    申请日：1988-10-26

    Applicant: Stephen R. Baker ,  Alec Todd

    Inventor： Stephen R. Baker ,  Alec Todd

    IPC: A61K31/38 ,  A61K31/381 ,  A61K31/41 ,  A61P37/08 ,  A61P43/00 ,  C07D333/18 ,  C07D333/24 ,  C07D409/04

    CPC classification number: C07D409/04 ,  C07D333/18 ,  Y02P20/55

    Abstract: A pharmaceutical compound of the formula: ##STR1## in which R.sup.1 is C.sub.7-20 alkyl, C.sub.7-20 alkenyl or C.sub.7-20 alkynyl, the alkyl, alkenyl or alkynyl group being optionally substituted by phenyl or substituted phenyl and the alkenyl and alkynyl groups containing 1 to 3 unsaturated bonds, R.sup.2 is (i) optionally substituted phenyl, (ii) C.sub.1-10 alkyl optionally substituted by one or more substituents selected from optionally protected hydroxyl, optionally protected carboxyl, nitrile, optionally protected tetrazolyl, --COR.sup.4 where R.sup.4 is C.sub.1-14 alkyl, C.sub.1-4 alkoxy, an optionally protected amino acid residue or --NR.sub.2.sup.5 where each R.sup.5 is hydrogen or C.sub.1-4 alkyl, and --NHR.sup.6 where R.sup.6 is hydrogen, a protecting group, an optionally protected amino acid residue, C.sub.1-4 alkyl or --COR.sup.7 where R.sup.7 is C.sub.1-4 alkyl or C.sub.1-4 alkoxy, or (iii) C.sub.1-10 alkyl substituted with a group selected from ##STR2## where each R.sup.8 is hydrogen or C.sub.1-4 alkyl, and R.sup.3 is hydrogen, carboxyl, C.sub.2-5 alkoxycarbonyl, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, hydroxyl, optionally protected tetrazolyl, halo, trifluoromethyl, nitrile, nitro and --CONR.sub.2.sup.9 where each R.sup.9 is hydrogen or C.sub.1-4 alkyl; and salts thereof.

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