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    5 Amino-2-carbonylthiophene derivatives for use as p38 map kinase inhibitors in the treatment of inflammatory diseases
    1.
    发明申请
    5 Amino-2-carbonylthiophene derivatives for use as p38 map kinase inhibitors in the treatment of inflammatory diseases 审中-公开

    公开(公告)号：US20070082898A1

    公开(公告)日：2007-04-12

    申请号：US10553361

    申请日：2004-04-13

    申请人： Adrian Gill ,  Steven Woodhead ,  Maria Carr

    发明人： Adrian Gill ,  Steven Woodhead ,  Maria Carr

    IPC分类号： A61K31/538 ,  A61K31/522 ,  A61K31/52 ,  A61K31/517 ,  A61K31/496 ,  A61K31/4745 ,  A61K31/4709 ,  A61K31/4178 ,  A61K31/416 ,  C07D417/02 ,  C07D413/02 ,  C07D409/02

    CPC分类号： C07D409/12 ,  C07D333/38 ,  C07D409/14 ,  C07D417/12 ,  C07D417/14

    摘要： The invention provides the use of a compound for the manufacture of a medicament for the prophylaxis or treatment of a disease state or condition mediated by a p38 MAP kinase; the compound being defined by formula (I): wherein: R1 and R2 are the same or different and each is selected from hydrogen, C1-4 hydrocarbyl, halogen and cyano; X is selected from C═O, C═S, C(═O)NH, C(═S)NH, C(═O)O, C(═O)S, C(═S)O and C(═S)S; R3 is selected from aryl and hetcroaryl groups each having from 5 to 12 ring members, the aryl and heteroaryl groups each being unsubstituted or substituted by one or more substituent groups R7 selected from halogen, hydroxy, trifluoromethyl, cyano, nitro, carboxy, amino, carbocyclic and heterocyclic groups having from 3 to 12 ring members; a group Ra—Rb wherein Ra is a bond, 0, CO, X1C(X2), C(X2)X1, X1C(X2)X1, S, SO, SO2, NRc, SO2NRc or NRcSO2; and Rb is selected from hydrogen, carbocyclic and heterocyclic groups having from 3 to 7 ring members, and a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from hydroxy, oxo, halogen, cyano, nitro, amino, mono- or di-C1-4 hydrocarbylamino, carbocyclic and heterocyclic groups having from 3 to 12 ring members and wherein one or more carbon atoms of the C1-8 hydrocarbyl group may optionally be replaced by O, S, SO, SO2, NRc, X1C(X2), C(X2)X1 or X1C(X2)X1; X1 is O, S or NRc and X2 is ═O, ═S or ═NRc; Rc is hydrogen or C1-4 hydrocarbyl; R4 is a group YR5 or a group R6; Y is is NH, O or S; R5 is selected from (a) carbocyclic and heterocyclic groups having from 3 to 12 ring members; and (b) C1-8 hydrocarbyl groups optionally substituted by one or more substituents selected from hydroxy, oxo, halogen, cyano, amino, mono- or di- C1-4 hydrocarbylamino, and carbocyclic and heterocyclic groups having from 3 to 12 ring members, wherein one or more carbon atoms of the C1-8 hydrocarbyl group may optionally be replaced by O, S, SO, SO2, NRc, X1C(X2), C(X2)X1 or X1C(X2)X1, provided that when Y is O, a carbon atom adjacent to the group Y is not replaced by O; and R6 is a heterocyclic group having from 4 to 12 ring members and containing at least one ring nitrogen atom through which R6 is linked to the adjacent carbonyl group; wherein the carbocyclic and heterocyclic groups of substituents R5 and R6 are each unsubstituted or substituted by one or more substituent groups R7 as hereinbefore defined. Also provided are novel compounds, pharmaceutical compositions containing the compounds and methods for their preparation.

    5-Morpholinylmethylthiophenyl Pharmaceutical Compounds As P38 MAP Kinase Modulators
    3.
    发明申请
    5-Morpholinylmethylthiophenyl Pharmaceutical Compounds As P38 MAP Kinase Modulators 审中-公开
    5-吗啉基甲硫基苯基药物化合物为P38

    公开(公告)号：US20070208015A1

    公开(公告)日：2007-09-06

    申请号：US10599931

    申请日：2005-04-13

    申请人： Adrian Gill ,  Maria Carr ,  John Lyons ,  Neil Thompson ,  David Rees

    发明人： Adrian Gill ,  Maria Carr ,  John Lyons ,  Neil Thompson ,  David Rees

    IPC分类号： A61K31/5377 ,  C07D413/14

    CPC分类号： C07D333/36 ,  C07D409/12 ,  C07D417/12

    摘要： The invention provides compounds of the formula (I) or a salt, solvate or N-oxide thereof, wherein: R1 and R2 are the same or different and each is selected from hydrogen, saturated C1-3 hydrocarbyl, halogen and cyano; X is selected from C═O, C═S, C(═O)NH, C(═S)NH, C(═O)O, C(═O)S, C(═S)O and C(═S)S; R3 is selected from aryl and heteroaryl groups each having from 5 to 12 ring members and being unsubstituted or substituted by one or more substituent groups R10 as defined in the claims; R4 and R5 are the same or different and are selected from hydrogen and methyl; or one of R4 and R5 is selected from hydroxymethyl and ethyl and the other is hydrogen; and R6 and R7 are the same or different and are selected from hydrogen and methyl. The compounds of the formula (I) hayed activity as p38 MAP kinase and Taf kinase inhibitors.

    摘要翻译： 本发明提供式（I）化合物或其盐，溶剂合物或N-氧化物，其中：R 1和R 2相同或不同，各自为 选自氢，饱和C 1-3烃基，卤素和氰基; X选自C-O，C-S，C（-O）NH，C（-S）NH，C（-O）O，C（-O）S，C（-S）O和C（-S） R 3选自具有5至12个环成员的芳基和杂芳基，并且未被取代或被权利要求中所定义的一个或多个取代基R 10取代; R 4和R 5相同或不同，并且选自氢和甲基; 或者R 4和R 5中的一个选自羟甲基和乙基，另一个是氢; 和R 6和R 7相同或不同，并且选自氢和甲基。 式（I）化合物具有作为p38 MAP激酶和Taf激酶抑制剂的活性。

    3,4-Disubstituted Pyrazoles as Cyclin Dependent Kinases (Cdk) or Aurora Kinase or Glycogen Synthase 3 (Gsk-3) Inhibitors
    6.
    发明申请
    3,4-Disubstituted Pyrazoles as Cyclin Dependent Kinases (Cdk) or Aurora Kinase or Glycogen Synthase 3 (Gsk-3) Inhibitors 审中-公开
    作为细胞周期蛋白依赖性激酶（Cdk）或极光激酶或糖原合酶3（Gsk-3）抑制剂的3,4-二取代吡唑类

    公开(公告)号：US20080004270A1

    公开(公告)日：2008-01-03

    申请号：US11571713

    申请日：2005-07-05

    申请人： Adrian Gill ,  Maria Carr ,  Michael O'Brien ,  Paul Wyatt ,  Valerio Berdini

    发明人： Adrian Gill ,  Maria Carr ,  Michael O'Brien ,  Paul Wyatt ,  Valerio Berdini

    IPC分类号： A61K31/5377 ,  A61K31/4188 ,  A61P25/28 ,  A61P35/00 ,  C07D235/02 ,  C07D471/02 ,  C07D265/34 ,  A61P37/00 ,  A61P31/12 ,  A61K31/47

    CPC分类号： C07D471/04 ,  C07D487/04 ,  C07D495/04

    摘要： The invention provides compounds of the formula (I); or salts or solvates or N-oxides thereof; wherein: Rq is selected from groups (a), (b) and (c); the asterisk denoting the point of attachment to the pyrazole ring; X is N or CR5; X″ is NR4; O, S or S(O); A is a bond or —(CH2)m—(B)n—; B is C═O, NRg(C═O) or O(C═O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; m is 0, 1 or 2; n is 0 or 1; R0 is hydrogen or, together with NRg when present, forms a group —(CH2)p— wherein p is 2 to 4; and R1 to R6b are as defined in the description. Compounds of the formula (I) have activity as inhibitors of CDK, aurora and GSK-3 kinases are useful in treating or preventing diseases such as cancers that are mediated by the said kinases.

    摘要翻译： 本发明提供式（I）化合物; 或其盐或溶剂合物或N-氧化物; 其中：R q选自（a），（b）和（c）组; 星号表示与吡唑环的连接点; X是N或CR 5; X“是NR 4; O，S或S（O）; A是键或 - （CH 2）m - （B）n - B为CO，NR（CO）或O（CO），其中R为氢或任选被羟基取代的C 1-4烷基烃基 或C 1-4烷氧基; m为0,1或2; n为0或1; 当存在时，R 0是氢或与NR a一起形成基团 - （CH 2 CH 2）n - - 其中p为2至4; 和R 1至R 6b如说明书中所定义。 式（I）化合物具有作为CDK抑制剂的活性，极光和GSK-3激酶可用于治疗或预防诸如由所述激酶介导的癌症的疾病。

    Imidazo[4,5-B]Pyridin-2-One and Oxazolo[4,5-B]Pyridin-2-One Compounds and Analogs Thereof as Therapeutic Compounds
    7.
    发明申请
    Imidazo[4,5-B]Pyridin-2-One and Oxazolo[4,5-B]Pyridin-2-One Compounds and Analogs Thereof as Therapeutic Compounds 有权

    公开(公告)号：US20070287838A1

    公开(公告)日：2007-12-13

    申请号：US11665640

    申请日：2005-10-21

    申请人： Dan Niculescu-Duvaz ,  Caroline Springer ,  Adrian Gill ,  Richard Taylor ,  Richard Marais ,  Hermen Dijkstra ,  Catherine Gaulon ,  Delphine Menard ,  Esteban Roman Vela

    发明人： Dan Niculescu-Duvaz ,  Caroline Springer ,  Adrian Gill ,  Richard Taylor ,  Richard Marais ,  Hermen Dijkstra ,  Catherine Gaulon ,  Delphine Menard ,  Esteban Roman Vela

    IPC分类号： C07D471/04

    CPC分类号： C07D471/04

    摘要： The present invention pertains to certain imidazo[4,5-b]pyridin-2-one and oxazolo[4,5-b]pyridin-2-one compounds and analogs thereof, which, inter alia, inhibit RAF (e.g., B-RAF) activity, inhibit cell proliferation, treat cancer, etc., and more particularly to compounds of the formula (I): wherein: J is independently —O— or —NRN1—; RN1, if present, is independently —H or a substituent; RN2 is independently —H or a substituent; Y is independently —CH═ or —N═; Q is independently —(CH2)j-M-(CH2)k— wherein: j is independently 0, 1 or 2; k is independently 0, 1, or 2; j+k is 0, 1, or 2; M is independently —O—, —S—, —NH—, —NMe—, or —CH2—; each of RP1, RP2, RP3, and RP4 is independently —H or a substituent; and additionally RP1 and RP2 taken together may be —CH═CH—CH═CH—; L is independently: a linker group formed by a chain of 2, 3, or 4 linker moieties; each linker moiety is independently —CH2—, —NRN—, —C(═X)—, or —S(═O)2—; exactly one linker moiety is —NRN—, or: exactly two linker moieties are —NRN—; exactly one linker moiety is —C(═X)—, and no linker moiety is —S(═O)2—; or: exactly one linker moiety is —S(═O)2—, and no linker moiety is —C(═X)—; no two adjacent linker moieties are —NRN—; X is independently ═O or ═S; each RN is independently —H or a substituent; A is independently: C6-14carboaryl, C5-14heteroaryl, C3-12carbocyclic, C3-12heterocyclic; and is independently unsubstituted or substituted; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, N-oxides, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., B-RAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and conditions that are ameliorated by the inhibition of RAF, RTK, etc., proliferative conditions such as cancer (e.g., colorectal cancer, melanoma), etc.

    METHODS OF MANUFACTURING WIND TURBINE BLADES
    8.
    发明申请
    METHODS OF MANUFACTURING WIND TURBINE BLADES 有权
    制造风力涡轮机叶片的方法

    公开(公告)号：US20120246931A1

    公开(公告)日：2012-10-04

    申请号：US13323238

    申请日：2011-12-12

    申请人： Mark Hancock ,  Anton Bech ,  Rens Christiaan Verhoef ,  Adrian Gill ,  Karl Gregory

    发明人： Mark Hancock ,  Anton Bech ,  Rens Christiaan Verhoef ,  Adrian Gill ,  Karl Gregory

    IPC分类号： B23P15/02

    CPC分类号： F03D1/0675 ,  B21D53/78 ,  B23P15/04 ,  F01D5/282 ,  F05B2230/00 ,  Y02E10/721 ,  Y02P70/523 ,  Y10T29/49336 ,  Y10T29/49337 ,  Y10T29/49947

    摘要： An elongate web is attached to the root end of a spar of a wind turbine rotor blade to provide additional support along the width of the blade. The root end is formed by a winding operation, and a recess is then cut into the surface of the spar. The recess is defined by a relatively large first, cylindrical surface, which is coaxial with the longitudinal axis of the root end, and a relatively small second, conical surface. A tapered end of the elongate web is attached within the recess of the root end using a layer of suitable adhesive and an array of pins. Resilient spacer elements are arranged within the recess so as to surround the pins. The large area of the cylindrical surface causes the tensile and compressive stresses which arise along the elongate web in use to be transmitted to the spar as shear stresses.

    摘要翻译： 细长腹板连接到风力涡轮机转子叶片的翼梁的根端以沿着叶片的宽度提供额外的支撑。 根端通过卷绕操作形成，然后将凹部切割到翼梁的表面。 凹槽由相对较大的第一圆柱形表面限定，该圆柱形表面与根端的纵向轴线同轴并且具有相对小的第二圆锥形表面。 细长腹板的锥形端部使用合适的粘合剂层和销的阵列附接在根部的凹部内。 弹性间隔元件布置在凹槽内，以便围绕销。 圆柱形表面的大面积使得沿着细长腹板产生的拉伸和压缩应力作为剪切应力传递到翼梁。

    Methods of manufacturing wind turbine blades
    10.
    发明授权
    Methods of manufacturing wind turbine blades 有权
    制造风力发电机叶片的方法

    公开(公告)号：US09032622B2

    公开(公告)日：2015-05-19

    申请号：US13323238

    申请日：2011-12-12

    申请人： Mark Hancock ,  Anton Bech ,  Rens Christiaan Verhoef ,  Adrian Gill ,  Karl Gregory

    发明人： Mark Hancock ,  Anton Bech ,  Rens Christiaan Verhoef ,  Adrian Gill ,  Karl Gregory

    IPC分类号： B21D53/78 ,  F03D1/06 ,  B23P15/04 ,  F01D5/28

    CPC分类号： F03D1/0675 ,  B21D53/78 ,  B23P15/04 ,  F01D5/282 ,  F05B2230/00 ,  Y02E10/721 ,  Y02P70/523 ,  Y10T29/49336 ,  Y10T29/49337 ,  Y10T29/49947

    摘要： An elongate web is attached to the root end of a spar of a wind turbine rotor blade to provide additional support along the width of the blade. The root end is formed by a winding operation, and a recess is then cut into the surface of the spar. The recess is defined by a relatively large first, cylindrical surface, which is coaxial with the longitudinal axis of the root end, and a relatively small second, conical surface. A tapered end of the elongate web is attached within the recess of the root end using a layer of suitable adhesive and an array of pins. Resilient spacer elements are arranged within the recess so as to surround the pins. The large area of the cylindrical surface causes the tensile and compressive stresses which arise along the elongate web in use to be transmitted to the spar as shear stresses.

    摘要翻译： 细长腹板连接到风力涡轮机转子叶片的翼梁的根端以沿着叶片的宽度提供额外的支撑。 根端通过卷绕操作形成，然后将凹部切割到翼梁的表面。 凹槽由相对较大的第一圆柱形表面限定，该圆柱形表面与根端的纵向轴线同轴并且具有相对小的第二圆锥形表面。 细长腹板的锥形端部使用合适的粘合剂层和销的阵列附接在根部的凹部内。 弹性间隔元件布置在凹槽内，以便围绕销。 圆柱形表面的大面积使得沿着细长腹板产生的拉伸和压缩应力作为剪切应力传递到翼梁。