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    Pyrazolopyridine derivatives as selective cox-2 inhibitors
    61.
    发明授权
    Pyrazolopyridine derivatives as selective cox-2 inhibitors 失效
    吡唑并吡啶衍生物作为选择性cox-2抑制剂

    公开(公告)号：US07223772B1

    公开(公告)日：2007-05-29

    申请号：US09830836

    申请日：1999-11-01

    申请人： Ian Baxter Campbell ,  Alan Naylor

    发明人： Ian Baxter Campbell ,  Alan Naylor

    IPC分类号： A61K31/415 ,  A61K31/44 ,  C07D231/56 ,  C07D471/02

    CPC分类号： C07D471/04

    摘要： The invention provides the compounds of formula (I) and pharmaceutically acceptable derivatives thereof wherein: R0 and R1 are independently selected from the group consisting of H, halogen, C1-6alkyl, C1-6alkoxy, and C1-6alkoxy substituted by one or more fluorine atoms; R2 is selected from the group consisting of H, C1-6alkyl, C1-6alkyl substituted by one or more fluorine atoms, C1-6alkoxy, C1-6hydroxyalkyl, SC1-6alkyl, C(O)H, C(O)C1-6alkyl, C1-6alkylsulphonyl, and C1-6alkoxy substituted by one or more fluorine atoms; and R3 is C1-6alkyl or NH2. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever, inflammation of a variety of conditions and diseases.

    摘要翻译： 本发明提供式（I）化合物及其药学上可接受的衍生物，其中：R 0和R 1独立地选自H，卤素， C 1-6烷基，C 1-6烷氧基和被一个或多个氟原子取代的C 1-6烷氧基; R 2选自H，C 1-6烷基，被一个或多个氟原子取代的C 1-6烷基 ，C 1-6烷氧基，C 1-6 1-6烷基，C 1-6烷基，C（O）H，C（O） C 1-6烷基，C 1-6烷基磺酰基和被一个或多个氟原子取代的C 1-6烷氧基; R 3是C 1-6烷基或NH 2。 式（I）化合物是COX-2的有效和选择性抑制剂，可用于治疗疼痛，发热，各种病症和疾病的炎症。

    2,3-diaryl-pyrazolo[1,5-b]pyridazines derivatives, their preparation and their use as cyclooxygenase 2 (COX-2) inhibitors
    64.
    发明授权
    2,3-diaryl-pyrazolo[1,5-b]pyridazines derivatives, their preparation and their use as cyclooxygenase 2 (COX-2) inhibitors 失效
    2,3-二芳基 - 吡唑并[1,5-b]哒嗪衍生物，其制备及其作为环加氧酶2（COX-2）抑制剂的用途

    公开(公告)号：US06861429B2

    公开(公告)日：2005-03-01

    申请号：US10212513

    申请日：2002-08-05

    申请人： Paul John Beswick ,  Charanjit Bountra ,  Ian Baxter Campbell ,  Neil Matthews ,  Alan Naylor

    发明人： Paul John Beswick ,  Charanjit Bountra ,  Ian Baxter Campbell ,  Neil Matthews ,  Alan Naylor

    IPC分类号： A61K31/00 ,  A61K31/50 ,  A61K31/5025 ,  A61P1/04 ,  A61P3/10 ,  A61P7/06 ,  A61P9/00 ,  A61P11/00 ,  A61P11/06 ,  A61P17/00 ,  A61P17/02 ,  A61P19/02 ,  A61P19/06 ,  A61P25/06 ,  A61P25/16 ,  A61P25/28 ,  A61P27/02 ,  A61P27/16 ,  A61P29/00 ,  A61P35/00 ,  C07D487/04 ,  A61K31/4985

    CPC分类号： C07D487/04 ,  A61K31/50 ,  Y02P20/55

    摘要： The invention provides a pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable salt, solvate, ester or salt or solvate of such ester, of a compound of formula (I) in which: R0 is halogen, C1-6alkyl, C1-6alkoxy, C1-6alkoxy substituted by one or more fluorine atoms, or O(CH2)nNR4R5; R1 and R2 are independently selected from H, C1-6alkyl, C1-6alkyl substituted by one or more fluorine atoms, C1-6alkoxy, C1-6hydroxyalkyl, SC1-6alkyl, C(O)H, C(O)C1-6alkyl, C1-6alkylsulphonyl, C1-6alkoxy substituted by one or more fluorine atoms, O(CH2)nCO2C1-6alkyl, O(CH2)nSC1-6alkyl, (CH2)nNR4R5, (CH2)nSC1-6alkyl or C(O)NR4R5; with the proviso that when R0 is at the 4-position and is halogen, at least one of R1 and R2 is C1-6alkylsulphonyl, C1-6alkoxy substituted by one or more fluorine atoms, O(CH2)nCO2C1-6alkyl, O(CH2)nSC1-6alkyl, (CH2)nNR4R5 or (CH2)nSC1-6alkyl, C(O)NR4R5; R3 is C1-6alkyl or NH2; R4 and R5 are independently selected from H and C1-6alkyl or, together with the nitrogen atom to which they are attached, form a 4-8 membered saturated ring; and n is 1-4; and a sodium channel inhibitor.

    摘要翻译： 本发明提供包含式（I）化合物或其药学上可接受的盐，溶剂化物，酯或盐或溶剂合物的药物组合物，其中：R 0是卤素，C1 1-6烷基，C 1-6烷氧基，被一个或多个氟原子取代的C 1-6烷氧基，或O（CH 2）n NR 4 R 5; R 1和R 2独立地选自H，C 1-6烷基 被一个或多个氟原子取代的C 1-6烷基，C 1-6烷氧基，C 1-6羟烷基，SC 1-6烷基，C（O）H，C（O）C 1-6烷基，C 1-6烷基磺酰基，被一个或多个 氟原子，O（CH 2）n CO 2 C 1-6烷基，O（CH 2）nSC 1-6烷基，（CH 2）n NR 4 R 5，（CH 2）nSC 1-6烷基或C（O）NR 4 R 5 ; 条件是当R 0在4-位且是卤素时，R 1和R 2中的至少一个是C 1-6烷基磺酰基，被一个或多个氟原子取代的C 1-6烷氧基，O（ O（CH 2）n C 1-6烷基，（CH 2）n NR 4 R 5或（CH 2）nSC 1-6烷基，C（O）NR 4 R 5; R 3， 是C 1-6烷基或NH 2; R 4和R 5独立地选自H和C 1-6烷基，或与它们所连接的氮原子一起形成4-8元饱和环; 和n为1-4;和钠通道抑制剂。

    Chemical compounds
    66.
    发明授权
    Chemical compounds 失效
    化学化合物

    公开(公告)号：US5116842A

    公开(公告)日：1992-05-26

    申请号：US524441

    申请日：1990-05-17

    申请人： Alan Naylor ,  Duncan B. Judd

    发明人： Alan Naylor ,  Duncan B. Judd

    IPC分类号： C07D241/04 ,  A61K31/495 ,  A61P25/04 ,  C07D403/06

    CPC分类号： C07D403/06

    摘要： Compounds are disclosed of formula (I) ##STR1## wherein R.sub.1 represents --COR.sub.4, --CO.sub.2 R.sub.4, --COCO.sub.2 R.sub.4 or --CONR.sub.4 R.sub.5 (where R.sub.4 and R.sub.5 may be the same or different and represent a hydrogen atom or a C.sub.1-3 alkyl group);R.sub.2 represents a hydrogen atom or a hydroxy or oxo group, with the proviso that when R.sub.1 is --COR.sub.4, --CO.sub.2 R.sub.4 or --COCO.sub.2 R.sub.4, R.sub.2 is not a hydrogen atom;R.sub.3 represents a hydrogen atom or a hydroxy group;X represents a direct bond, --CH.sub.2 -- or --CH.sub.2 O--;Ar represents a substituted phenyl moiety; and physiologically acceptable salts thereof.The compounds are indicated as useful in the treatment of pain.Processes for their preparation and pharmaceutical compositions containing them are also disclosed.

    Phenethanolamine derivatives
    67.
    发明授权
    Phenethanolamine derivatives 失效

    公开(公告)号：US5099068A

    公开(公告)日：1992-03-24

    申请号：US622549

    申请日：1990-12-05

    申请人： William L. Mitchell ,  Ian F. Skidmore ,  Lawrence H. C. Lunts ,  Harry Finch ,  Alan Naylor ,  David Hartley

    发明人： William L. Mitchell ,  Ian F. Skidmore ,  Lawrence H. C. Lunts ,  Harry Finch ,  Alan Naylor ,  David Hartley

    IPC分类号： C07C307/10 ,  C07C65/11 ,  C07C217/08 ,  C07C231/12 ,  C07C233/43 ,  C07C275/34 ,  C07C311/08 ,  C07C323/12 ,  C07C323/16 ,  C07C323/25

    CPC分类号： C07C65/11 ,  Y10S514/819 ,  Y10S514/826 ,  Y10S514/886 ,  Y10S514/887 ,  Y10S514/913 ,  Y10S514/925 ,  Y10S514/927

    摘要： The invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable salts and solvates thereof, wherein AR represents the group ##STR2## where Q.sup.1 represents a straight or branched C.sub.1-3 alkylene group, ##STR3## where Q.sup.2 represents a group R.sup.3 CO--, R.sup.3 NHCO--, R.sup.3 R.sup.4 NSO.sub.2 --, or R.sup.5 SO.sub.2 --, where R.sup.3 and R.sup.4 each represent a hydrogen atom or a C.sub.1-3 alkyl group, and R.sup.5 represents a C.sub.1-3 alkyl group, ##STR4## R represents a hydrogen atom or a C.sub.1-3 alkyl group; R.sup.1 and R.sup.2 each independently represent a hydrogen atom or a methyl or ethyl group; andk represents an integer from 1 to 8;m represents zero or an integer from 2 to 7, and;n represents an integer from 1 to 7 with the proviso that the sum total of k, m and n is 4 to 12;X represents an oxygen or sulphur atom, and;Y and Z each represent a bond, or an oxygen or sulphur atom with the proviso that 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, or when Y and Z each independently represent an oxygen or sulphur atom then n is an integer from 2 to 7;Q represents a naphthalenyl group wich may optionally be substituted by one or two groups selected from C.sub.1-4 alkyl, C.sub.1-4 alkoxy, hydroxy and halogen.The compounds have a stimulant action at .beta..sub.2 -adrenoreceptors and may be used in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.

    Phenethanolamine derivatives
    68.
    发明授权
    Phenethanolamine derivatives 失效
    苯乙醇胺衍生物

    公开(公告)号：US4997986A

    公开(公告)日：1991-03-05

    申请号：US270945

    申请日：1988-11-14

    申请人： William L. Mitchell ,  Ian F. Skidmore ,  Lawrence H. C. Lunts ,  Harry Finch ,  Alan Naylor ,  David Hartley

    发明人： William L. Mitchell ,  Ian F. Skidmore ,  Lawrence H. C. Lunts ,  Harry Finch ,  Alan Naylor ,  David Hartley

    IPC分类号： C07C307/10 ,  C07C65/11 ,  C07C217/08 ,  C07C231/12 ,  C07C233/43 ,  C07C275/34 ,  C07C311/08 ,  C07C323/12 ,  C07C323/16 ,  C07C323/25

    CPC分类号： C07C65/11 ,  Y10S514/819 ,  Y10S514/826 ,  Y10S514/886 ,  Y10S514/887 ,  Y10S514/913 ,  Y10S514/925 ,  Y10S514/927

    摘要： The invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable salts and solvates thereof, wherein Ar represents the group ##STR2## where Q.sup.1 represents a straight or branched C.sub.1-3 alkylene group, ##STR3## where Q.sup.2 represents a group R.sup.3 CO--, R.sup.3 NHCO--, R.sup.3 R.sup.4 NSO.sub.2 -- or R.sup.5 SO.sub.2 --, where R.sup.3 and R.sup.4 each represent a hydrogen atom or a C.sub.1-3 alkyl group, and R.sup.5 represents a C.sub.1-3 alkyl group, ##STR4## R represents a hydrogen atom or a C.sub.1-3 alkyl group; R.sup.1 and R.sup.2 each independently represent a hydrogen atom or a methyl or ethyl group; and k represents an integer from 1 to 8; m represents zero or an integer from 2 to 7, and; n represents an integer from 1 to 7 with the proviso that the sum total of k, m and n is 4 to 12; X represents an oxygen or sulphur atom, and; Y and Z each represent a bond, or an oxygen or sulphur atom with the proviso that 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, or when Y and Z each independently represent an oxygen or sulphur atom then n is an integer from 2 to 7; Q represents a naphthalenyl group which may optionally be substituted by one or two groups selected from C.sub.1-4 alkyl, C.sub.1-4 alkoxy, hydroxy and halogen.The compounds have a stimulant action at .beta..sub.2 -adrenoreceptors and may be used in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.

    Ethanolamine derivatives
    69.
    发明授权
    Ethanolamine derivatives 失效

    公开(公告)号：US4990664A

    公开(公告)日：1991-02-05

    申请号：US230357

    申请日：1988-08-10

    申请人： Ian F. Skidmore ,  Alan Naylor ,  Harry Finch ,  Lawrence H. C. Lunts ,  Ian B. Campbell ,  Peter C. North

    发明人： Ian F. Skidmore ,  Alan Naylor ,  Harry Finch ,  Lawrence H. C. Lunts ,  Ian B. Campbell ,  Peter C. North

    IPC分类号： C07D295/18 ,  A61K31/135 ,  A61K31/165 ,  A61K31/18 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4418 ,  A61K31/47 ,  A61P5/38 ,  C07C67/00 ,  C07C231/00 ,  C07C237/30 ,  C07C301/00 ,  C07C303/34 ,  C07C309/66 ,  C07C313/00 ,  C07C323/25 ,  C07C323/27 ,  C07C323/41 ,  C07C323/42 ,  C07C323/43 ,  C07C323/44 ,  C07C323/49 ,  C07C323/60 ,  C07C323/62 ,  C07C323/65 ,  C07C325/00 ,  C07D213/32 ,  C07D213/65 ,  C07D215/26

    CPC分类号： C07C323/62 ,  C07C323/25 ,  C07D213/32

    摘要： The invention provides compounds of the general formula ##STR1## and physiologically acceptable salts and solvates thereof, wherein Z represents the group ##STR2## where A represents a group selected from HOR.sup.3 --, R.sup.6 NH(CH.sub.2)p--, R.sup.10 R.sup.11 N--, R.sup.12 OCH.sub.2 --, CH.sub.3 SO.sub.2 CH.sub.2 -- or NCCH.sub.2 --;where R.sup.3 is a C.sub.1-3 alkylene group,R.sup.6 is a group selected from R.sup.7 CO--, R.sup.7 NHCO--, R.sup.7 R.sup.8 NSO.sub.2 -- orR.sup.9 SO.sub.2 --, and p is zero or 1,R.sup.7 and R.sup.8 each represent a hydrogen atom or a C.sub.1-3 alkyl group,R.sup.9 is a C.sub.1-3 alkyl group,R.sup.10 and R.sup.11 each represent a hydrogen atom or a C.sub.1-4 alkyl group or, when R.sup.10 is a hydrogen atom, R.sup.11 may also be a C.sub.1-4 alkoxycarbonyl group, andR.sup.12 is a C.sub.1-3 alkyl group; ##STR3## where one of R.sup.4 and R.sup.5 is a hydroxy group and the other is a hydrogen or halogen atom or a hydroxy group; ##STR4## where A.sup.1 is either a chlorine atom or a --CF.sub.3 group; ##STR5## X represents a bond or a C.sub.1-7 alkenylene or C.sub.2-7 alkynylene chain, andY represents a bond, or a C.sub.1-6 alkylene, C.sub.2-6 alkenylene or C.sub.2-6 alkynylene chain, with the proviso that the sum total of carbon atoms in X and Y is 2 to 10;R represents a hydrogen atom or a C.sub.1-3 alkyl group;R.sup.1 and R.sup.2 each represents a hydrogen atom or a C.sub.1-3 alkyl group; with the proviso that the sum total of carbon atoms inR.sup.1 and R.sup.2 is not more than 4;Q represents a pyridyl group optionally substituted by one or two substituents selected from halogen atoms or hydroxy, C.sub.1-3 alkyl or C.sub.1-3 alkoxy groups, or Q represents a phenyl group optionally substituted by one or more substituents selected from halogen atoms or the groups C.sub.1-6 alkyl, nitro, --(CH.sub.2).sub.q R.sup.13 or --O(CH.sub.2).sub.r R.sup.14, or Q represents a phenyl group substituted by an alkylenedioxy group of formula --O(CH.sub.2).sub.t O--; whereR.sup.13 represents hydroxy, C.sub.1-6 alkoxy, cyano, --NR.sup.15 R.sup.16, --NR.sup.17 COR.sup.18, --NR.sup.17 SO.sub.2 R.sup.19, --COR.sup.20, --SR.sup.21, --SOR.sup.22 or --SO.sub.2 R.sup.22 ;R.sup.14 represents hydroxy or C.sub.1-4 alkoxy;R.sup.15 and R.sup.16 each represent a hydrogen atom or a C.sub.1-4 alkyl group or --NR.sup.15 R.sup.16 forms a saturated heterocyclic amino group which has 5-7 ring members and optionally contains in the ring one or more atoms selected from --O-- or --S-- or a group --NH-- or --N(CH.sub.3)--;R.sup.17 represents a hydrogen atom or a C.sub.1-4 alkyl group;R.sup.18 represents a hydrogen atom or a C.sub.1-4 alkyl, C.sub.1-4 alkoxy, phenyl or --NR.sup.15 R.sup.16 group;R.sup.19 represents C.sub.1-4 alkyl, phenyl or --NR.sup.15 R.sup.16 ;R.sup.20 represents hydroxy, C.sub.1-4 alkoxy or --NR.sup.15 R.sup.16 ;R.sup.21 represents a hydrogen atom or a C.sub.1-4 alkyl or phenyl group;R.sup.22 represents a C.sub.1-4 alkyl or phenyl group;q represents an integer from 0 to 3;r represents 2 or 3; andt represents 1 or 2.The compounds have a stimulant action at .beta..sub.2 -adrenoreceptors and may be used in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.