会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 4. 发明授权
    • Heteroaryl-cyclic acetals
    • 杂芳基环缩醛
    • US07479501B2
    • 2009-01-20
    • US09871564
    • 2001-05-31
    • Alan CollisFrank HalleyIain McLay
    • Alan CollisFrank HalleyIain McLay
    • A61K31/4439C07D405/14
    • C07D409/14C07D405/14C07D413/14
    • Compounds of formula (I) are described in which Het is a five or six membered heteroaromatic ring of the formula in which one of R1 and R2 is optionally substituted heteroaryl and the other is optionally substituted heteroaryl or optionally substituted aryl; X1 is a bond, X3 and X4 are each independently N or C and X2 and X5 are independently CH, N, NH, O or S; or X3 and X4 are C, one of X1, X2 and X5 is N and the others are N or CH; but excluding compounds in which X1 is a bond, one of X2 and X5 is N and the other is NH and X3 and X4 are both C; R3 represents a group -L1-R6; R4 represents hydrogen, alkyl or hydroxyalkyl; or R3 and R4, when attached to the same carbon atom, may form with the said carbon atom a cycloalkyl, cycloalkenyl or heterocycloalkyl ring or a group C═CH2; R5 represents hydrogen or alkyl; and m is zero or an integer 1 or 2; and N-oxides thereof, and their prodrugs; and pharmaceutically acceptable salts and solvates of compounds of formula (I) and N-oxides thereof, and their prodrugs. The compounds are TNF inhibitors and are useful as pharmaceuticals.
    • 描述式(I)的化合物,其中Het是下式的五或六元杂芳族环,其中R 1和R 2中的一个是任选取代的杂芳基,另一个是任选取代的杂芳基或任选取代的芳基; X1是键,X3和X4各自独立地是N或C,X2和X5独立地是CH,N,NH,O或S; 或X3和X4为C,X1,X2和X5之一为N,其余为N或CH; 但不包括X1为键的化合物,X2和X5之一为N,另一个为NH,X3和X4均为C; R3表示基团-L1-R6; R4表示氢,烷基或羟烷基; 或者R 3和R 4在连接到相同的碳原子时可与所述碳原子一起形成环烷基,环烯基或杂环烷基环或基团C-CH 2; R5代表氢或烷基; m为零或整数1或2; 和N-氧化物及其前药; 和式(I)化合物及其N-氧化物的药学上可接受的盐和溶剂合物及其前药。 这些化合物是TNF抑制剂,可用作药物。
    • 5. 发明申请
    • Heteroaryl-cyclic acetals
    • 杂芳基环缩醛
    • US20050090501A1
    • 2005-04-28
    • US09871564
    • 2001-05-31
    • Alan CollisFrank HalleyIain McLay
    • Alan CollisFrank HalleyIain McLay
    • A61K31/4439A61K31/497A61K31/501A61K31/506A61K31/5377A61P3/04A61P3/10A61P9/10A61P11/06A61P19/02A61P27/02A61P35/00A61P43/00C07D405/14C07D409/14C07D413/14C07D45/04
    • C07D409/14C07D405/14C07D413/14
    • Compounds of formula (I) are described in which Het is a five or six membered heteroaromatic ring of the formula in which one of R1 and R2 is optionally substituted heteroaryl and the other is optionally substituted heteroaryl or optionally substituted aryl; X1 is a bond, X3 and X4 are each independently N or C and X2 and X5 are independently CH, N, NH, O or S; or X3 and X4 are C, one of X1, X2 and X5 is N and the others are N or CH; but excluding compounds in which X1 is a bond, one of X2 and X5 is N and the other is NH and X3 and X4 are both C; R3 represents a group -L1-R6; R4 represents hydrogen, alkyl or hydroxyalkyl; or R3 and R4, when attached to the same carbon atom, may form with the said carbon atom a cycloalkyl, cycloalkenyl or heterocycloalkyl ring or a group C═CH2; R5 represents hydrogen or alkyl; and m is zero or an integer 1 or 2; and N-oxides thereof, and their prodrugs; and pharmaceutically acceptable salts and solvates of compounds of formula (I) and N-oxides thereof, and their prodrugs. The compounds are TNF inhibitors and are useful as pharmaceuticals.
    • 描述式(I)的化合物,其中Het是下式的五或六元杂芳族环,其中R 1和R 2中的一个是任选取代的杂芳基和 另一个是任选取代的杂芳基或任选取代的芳基; X 1是一个键,X 3和X 4各自独立地是N或C和X 2和X 5个独立的是CH,N,NH,O或S; 或X 3和X 4是C,X 1,X 2和X 5之一 为N,其余为N或CH; 但不包括其中X 1是一个键的化合物,X 2和X 5之一是N,另一个是NH和X 3< 4>和< 4>都是C; R 3表示基团-L 1→6→6; R 4表示氢,烷基或羟烷基; 或R 3和R 4,当连接到相同的碳原子时,可与所述碳原子一起形成环烷基,环烯基或杂环烷基环或C-CH 3基, SUB> 2 R 5表示氢或烷基; m为零或整数1或2; 和N-氧化物及其前药; 和式(I)化合物及其N-氧化物的药学上可接受的盐和溶剂合物及其前药。 这些化合物是TNF抑制剂,可用作药物。
    • 7. 发明授权
    • Imidazolyl-cyclic acetals
    • 咪唑基 - 环状缩醛
    • US06602877B1
    • 2003-08-05
    • US09456360
    • 1999-12-08
    • Paul L. BamboroughAlan J. CollisFrank HalleyRichard A. LewisDavid J. LythgoeJeffrey M. McKennaIain M. McLayBarry PorterAndrew J. RatcliffePaul A. Wallace
    • Paul L. BamboroughAlan J. CollisFrank HalleyRichard A. LewisDavid J. LythgoeJeffrey M. McKennaIain M. McLayBarry PorterAndrew J. RatcliffePaul A. Wallace
    • C07D23354
    • C07D231/12C07D233/56C07D249/08C07D401/04C07D403/04C07D405/14C07D409/14C07D413/14C07D491/10C07D493/10
    • Compounds of formula (I) are described in which R1 is optionally substituted heteroaryl; R2 is optionally substituted aryl or optionally substituted heteroaryl; R3 is a group —L1—R7 or —L2—R8 [where L1 is an optionally substituted alkylene linkage; R7 is hydrogen, aryl, cyano, cycloalkyl, heteroaryl, heterocycloalkyl, nitro, —S(O)nR9, —NHSO2R9, —C(═Z)OR10, —C(═Z)R10, —OR10, —N(R11)—C(═Z)R9, —NY1Y2, —SO2NY1Y2, —C(═Z)—NY1Y2, —N(R11)—C(═Z)—NY1Y2, —N(OR10)—C(═Z)—NY1Y2, —N(OR10)—C(═Z)R10, —C(═NOR10)R10, —C(═Z)NR10OR12, —N(R11)—C(═NR13)—NY1Y2 or —N(R11)—C(═Z)OR11; L2 is a direct bond or a straight- or branched-carbon chain comprising from 2 to about 6 carbon atoms and contains a double or triple carbon-carbon bond; and R8 is hydrogen, aryl, cycloalkenyl, cycloalkyl, heteroaryl or heterocycloalkyl]; R4 is a group —L3—R14 [where L3 is a direct bond or an optionally substituted alkylene linkage and R14 is hydrogen, alkyl, azido, hydroxy, alkoxy, aryl, arylalkyloxy, aryloxy, carboxy (or an acid bioisostere), cycloalkyloxy, heteroaryl, heteroarylalkyloxy, heteroaryloxy, heterocycloalkyl, heterocycloalkyloxy, nitro, —NY4Y5, —N(R10)—C(═Z)—R15; —N(R10)—C(═Z)—L4—R16, —NH—C(═Z)—NH—R15, —NH—C(═Z)—NH—L4—R16, —N(R10)—SO2—R15, —N(R10)—SO2—L4—R16, —S(O)nR9, —C(═Z)—NY4Y5 or —C(═Z)—OR9]; R5 is hydrogen, alkyl or hydroxyalkyl; or R4 and R5, when attached to the same carbon atom, may form with the said carbon atom a cycloalkyl, cycloalkenyl or heterocycloalkyl ring or a group C═CH2; R6 is hydrogen or alkyl; and m is zero or an integer 1 or 2; and N-oxides thereof, and their prodrugs; and pharmaceutically acceptable salts and solvates (e.g. hydrates) of compounds of formula (I) and N-oxides thereof, and their prodrugs. The compounds are TNF inhibitors and are useful as pharmaceuticals.
    • 描述式(I)的化合物,其中R 1是任选取代的杂芳基; R2是任选取代的芳基或任选取代的杂芳基; R3是基团-L1-R7或-L2-R8 [其中L1是任选取代的亚烷基键; R 7是氢,芳基,氰基,环烷基,杂芳基,杂环烷基,硝基,-S(O)n R 9,-NHSO 2 R 9,-C(= Z)OR 10,-C(= Z)R 10,-OR 10,-N(R 11) -C(= Z)R9,-NY1Y2,-SO2NY1Y2,-C(= Z)-NY1Y2,-N(R11)-C(= Z)-NY1Y2,-N(OR10)-C(= Z)-NY1Y2 ,-N(OR 10)-C(= Z)R 10,-C(= NOR 10)R 10,-C(= Z)NR 10 OR 12,-N(R 11)-C(= NR 13)-NY 1 Y 2或-N(R 11) C(= Z)OR 11; L2是直接键或包含2至约6个碳原子并含有双或三碳 - 碳键的直链或支链碳链; 和R8是氢,芳基,环烯基,环烷基,杂芳基或杂环烷基]; R4是基团-L3-R14 [其中L3是直接键或任选取代的亚烷基键,R 14是氢,烷基,叠氮基,羟基,烷氧基,芳基,芳基烷氧基,芳氧基,羧基(或酸式生物电子等排体) 杂芳基烷氧基,杂芳氧基,杂环烷基,杂环烷氧基,硝基,-NY 4 Y 5,-N(R 10)-C(= Z)-R 15; -N(R10)-C(= Z)-L4-R