Inhibitors of IKK-beta serine-threonine protein kinase
    5.
    发明授权
    Inhibitors of IKK-beta serine-threonine protein kinase 失效
    IKK-β丝氨酸 - 苏氨酸蛋白激酶抑制剂

    公开(公告)号:US08106091B2

    公开(公告)日:2012-01-31

    申请号:US12447271

    申请日:2007-10-29

    CPC classification number: C07D333/38

    Abstract: Compounds of formula (IA) or (IB) are inhibitors of IkB kinase (IKK) activity, and are useful in the treatment of autoimmune and inflammatory diseases: wherein R7 is hydrogen or optionally substituted (C1-C6)alkyl; ring A is an optionally substituted aryl or heteroaryl ring of 5-13 ring atoms; Z is a radical of formula R-L1-Y1—(CH2)z—, wherein: z is 0 or 1; R is a radical of formula (X) or (Y) R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; R6 is hydrogen, or optionally substituted C1-C6 alkyl, C3-C7 cycloalkyl, aryl or heteroaryl or —(C═O)R3, —(C═O)OR3, or —(C═O)NR3 wherein R3 is hydrogen or optionally substituted (C1-C6)alkyl; Y1 is a bond, —(C═O)—, —S(O2)—, —C(═O)O—, —OC(═O)—, —(C═O)NR3—, —NR3(C═O)—, —S(O2)NR3—, —NR3S(O2)—, or —NR3(C═O)NR4—, wherein R3 and R4 are independently hydrogen or optionally substituted (C1-C6)alkyl, L1 is a divalent linker radical of formula -(Alk1)m(Q)n(Alk2)p- wherein m, n, p, Q, Alk1 and Alk2 are as defined in the claims.

    Abstract translation: 式(IA)或(IB)的化合物是IkB激酶(IKK)活性的抑制剂,可用于治疗自身免疫性和炎性疾病:其中R 7为氢或任选取代的(C 1 -C 6)烷基; 环A是任选取代的5-13个环原子的芳基或杂芳基环; Z是式R-L1-Y1-(CH2)z-的基团,其中:z是0或1; R是式(X)或(Y)的基团,R 1是羧酸基团(-COOH)或可被一个或多个细胞内酯酶水解成羧酸基团的酯基; R 6是氢或任选取代的C 1 -C 6烷基,C 3 -C 7环烷基,芳基或杂芳基或 - (C = O)R 3, - (C = O)OR 3或 - (C = O)NR 3,其中R 3是氢或 任选取代的(C 1 -C 6)烷基; Y1是一个键, - (C = O) - , - S(O 2) - , - C(= O)O-,-OC(= O) - , - (C = O)NR 3 - , - NR 3 (O) - , - S(O 2)NR 3 - , - NR 3 S(O 2) - 或-NR 3(C = O)NR 4 - ,其中R 3和R 4独立地是氢或任选取代的(C 1 -C 6) 式 - (Alk1)m(Q)n(Alk2)p的二价连接基团其中m,n,p,Q,Alk1和Alk2如权利要求中所定义。

    INHIBITORS OF IKK-BETA SERINE-THERONINE PROTEIN KINASE
    6.
    发明申请
    INHIBITORS OF IKK-BETA SERINE-THERONINE PROTEIN KINASE 审中-公开
    IKK-BETA丝氨酸蛋白激酶激酶的抑制剂

    公开(公告)号:US20110039920A1

    公开(公告)日:2011-02-17

    申请号:US12989022

    申请日:2008-04-23

    CPC classification number: C07D333/38

    Abstract: Cyclopentyl(2S,4E)-2-amino-5-{3-[4-carbamoyl-5(carbamoylamino)-2-thienyl]phenyl}pent-4-enoate; Cyclopentyl 5-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]phenyl}-L-norvalinate; Cyclopentyl(2S,4E)-2-amino-5-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]-5-methylphenyl}pent-4-enoate; Cyclopentyl(25,4E)-2-amino-5-{5-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]-2-methylphenyl}pent-4-enoate; Cyclopentyl O-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]phenyl}-L-homoserinate; Cyclopentyl O-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]phenyl}-L-homoserinate; Cyclopentyl N-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]benzyl}-L-alaninate; and tert-Butyl N-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]benzyl}-L-alaninate are hydrolysed to the corresponding carboxylic acids by intracellular carboxylesterases, and are useful for the inhibition of IKKβ activity.

    Abstract translation: (2S,4E)-2-氨基-5- {3- [4-氨基甲酰基-5(氨基甲酰基氨基)-2-噻吩基]苯基}戊-4-烯酸酯; 5- {3- [4-氨甲酰基-5-(氨基甲酰基氨基)-2-噻吩基]苯基} -L-降冰片烯环戊酯; (2S,4E)-2-氨基-5- {3- [4-氨基甲酰基-5-(氨基甲酰基氨基)-2-噻吩基] -5-甲基苯基}戊-4-烯酸酯; 环戊基(25,4E)-2-氨基-5- {5- [4-氨基甲酰基-5-(氨基甲酰基氨基)-2-噻吩基] -2-甲基苯基}戊-4-烯酸酯; 环戊基O- {3- [4-氨基甲酰基-5-(氨基甲酰基氨基)-2-噻吩基]苯基} -L-高丝氨酸酯; 环戊基O- {3- [4-氨基甲酰基-5-(氨基甲酰基氨基)-2-噻吩基]苯基} -L-高丝氨酸酯; N- {3- [4-氨基甲酰基-5-(氨基甲酰基氨基)-2-噻吩基]苄基} -L-丙氨酸酯的环戊基酯; 和N- {3- [4-氨基甲酰基-5-(氨基甲酰基氨基)-2-噻吩基]苄基} -L-丙氨酸叔丁酯通过细胞内羧酸酯酶水解成相应的羧酸,并且可用于抑制IKK和bgr; 活动。

    Bushing for processing molten glass
    9.
    发明授权
    Bushing for processing molten glass 失效
    用于加工熔融玻璃的衬套

    公开(公告)号:US4099948A

    公开(公告)日:1978-07-11

    申请号:US822257

    申请日:1977-08-05

    CPC classification number: C03B37/091 Y10S65/04 Y10T29/49988

    Abstract: This invention relates to a bushing for processing molten glass. The bushing has a bottom wall provided with orifices to deliver downwardly flowing streams of molten glass, side walls and end walls. The bushing is provided with oppositely arranged terminals to receive electrical conductors for heating the bushing. The end walls of the bushing and the terminal means are moulded integrally from rhodium or platinum/rhodium alloy.

    Abstract translation: 本发明涉及一种用于加工熔融玻璃的衬套。 衬套具有设置有孔口的底壁,以向下流动的熔融玻璃,侧壁和端壁流。 衬套设置有相对布置的端子,以接收用于加热衬套的电导体。 衬套和端子装置的端壁由铑或铂/铑合金一体成型。

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