Phenylalanine Enamide Derivatives
    1.
    发明申请
    Phenylalanine Enamide Derivatives 失效
    苯丙氨酸酰胺衍生物

    公开(公告)号:US20090105291A1

    公开(公告)日:2009-04-23

    申请号:US12327311

    申请日:2008-12-03

    摘要: Phenylalanine enamide derivatives of formula (1) are described: wherein R1 is a group Ar1 L2Ar2Alk- in which: Ar1 is an optionally substituted aromatic or heteroaromatic group; L2 is a covalent bond or a linker atom or group; Ar2 is an optionally substituted arylene or heteroarylene group; and Alk is a chain —CH2—CH(R)—, —CH═C(R)— or in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; X is an —O— or —S— atom or —N(R2)— group in which: Rx, Ry and Rz which may be the same or different is each a hydrogen atom or an optional substituent; or Rz is an atom or group as previously defined and Rx and Ry are joined together to form an optionally substituted spiro linked cycloaliphatic or heterocycloaliphatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immuno or inflammatory disorders or disorders involving the inappropriate growth or migration of cells.

    摘要翻译: 描述了式(1)的苯丙氨酸烯酰胺衍生物:其中R1是基团Ar1 L2Ar2Alk-,其中:Ar1是任选取代的芳族或杂芳族基团; L2是共价键或连接体原子或基团; Ar 2是任选取代的亚芳基或亚杂芳基; 并且Alk是链-CH 2 -CH(R) - , - CH-C(R) - 或其中R是羧酸(-CO 2 H)或其衍生物或生物试剂; X是-O-或-S-原子或-N(R 2) - 基团,其中:可以相同或不同的R x,R y和R z各自为氢原子或任选的取代基; 或R z是如先前定义的原子或基团,并且R x和R y连接在一起以形成任选取代的螺环连接的脂环族或杂环脂族基团; 及其盐,溶剂合物,水合物和N-氧化物。 该化合物能够抑制整联蛋白与其配体的结合,并且可用于预防和治疗涉及细胞不适当生长或迁移的免疫或炎性疾病或病症。

    Phenylalanine enamide derivatives
    2.
    发明授权
    Phenylalanine enamide derivatives 失效
    苯丙氨酸烯酰胺衍生物

    公开(公告)号:US07501437B2

    公开(公告)日:2009-03-10

    申请号:US11692612

    申请日:2007-03-28

    IPC分类号: C07D471/04 A61K31/4375

    摘要: Phenylalanine enamide derivatives of formula (1) are described: wherein R1 is a group Ar1L2Ar2Alk—in which: Ar1 is an optionally substituted aromatic or heteroaromatic group; L2 is a covalent bond or a linker atom or group; Ar2 is an optionally substituted arylene or heteroarylene group; and Alk is a chain in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; X is an —O— or —S— atom or —N(R2)— group in which: Rx, Ry and Rz which may be the same or different is each a hydrogen atom or an optional substituent; or Rz is an atom or group as previously defined and Rx and Ry are joined together to form an optionally substituted spiro linked cycloaliphatic or heterocycloaliphatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immuno or inflammatory disorders or disorders involving the inappropriate growth or migration of cells.

    摘要翻译: 描述式(1)的苯丙氨酸烯酰胺衍生物:其中R1是Ar1L2Ar2Alk基团,其中:Ar1是任选取代的芳族或杂芳族基团; L2是共价键或连接原子或基团; Ar 2是任选取代的亚芳基或亚杂芳基; 并且Alk是其中R是羧酸(-CO 2 H)或其衍生物或生物试剂的链; X是-O-或-S-原子或-N(R 2) - 基团,其中:可以相同或不同的R x,R y和R z各自为氢原子或任选的取代基; 或R z是如先前定义的原子或基团,并且R x和R y连接在一起以形成任选取代的螺环连接的脂环族或杂环脂族基团; 及其盐,溶剂合物,水合物和N-氧化物。 该化合物能够抑制整联蛋白与其配体的结合,并且可用于预防和治疗涉及细胞不适当生长或迁移的免疫或炎性疾病或病症。

    Carboxylic and hydroxamic acid compounds inhibiting metalloproteases, method for preparing same and pharmaceutical compositions containing them
    3.
    发明授权
    Carboxylic and hydroxamic acid compounds inhibiting metalloproteases, method for preparing same and pharmaceutical compositions containing them 失效
    抑制金属蛋白酶的羧酸和异羟肟酸化合物,其制备方法和含有它们的药物组合物

    公开(公告)号:US06605604B1

    公开(公告)日:2003-08-12

    申请号:US09720850

    申请日:2000-12-26

    IPC分类号: C07D20948

    摘要: The invention concerns a compound of formula (I) wherein: n is equal to 0 or 1; R1, R2, R3, R4 represent a hydrogen or an alkyl group, or R1 and R3 together form a cycloalkyl group; R5 represents a hydrogen, an alkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl, hetereoalkylalkyl, hetereocycloalkyl, hetereocycloalkylalkyl group (all optionally substituted), or a —CO—R6 group; and R6 represents R7 or OR7 or NR7R8, with R7 representing an aryl, arylalkyl, heteroaryl or heteroarylalkyl, heterocycloalkyl, heterocycloalkylalkyl group (all optionally substituted), and R8 representing an alkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl (all optionally substituted); or R5 and R6 form with the nitrogen atom and the Z group bearing them a saturated monocyclic, bicyclic or tricyclic group, partially unsaturated or unsaturated, with 5 to 16 chain links containing 1 to 7 heteroatoms and optionally substituted; R10 represents a hydrogen atom or a hydroxy group, and in the latter case R1, R2, R3, R4 are independently selected among hydrogen and alkyl; Z represents a hydroxy, alkoxy, alkenyloxy, benzyloxy group or a NH—OR group; X represents a sulphur, a SO, SO2 group (in those cases where R3 and R4 are different from an alkyl) or a group —CO—O— (in which case R1 and R3 form a cycloalkyl group), or X represents an oxygen atom; W represents a W1—(A)p or W1—B—W2—(A)p group wherein W1 and W2 represent an aryl or heteroaryl group, A is a standard substituent of aromatic cycles, B a bond, an oxygen or an alkylene, alkenylene, alkynylene group, and p is an integer ranging between 0 and 5; T1 and T2 represent a bond or an alkylene, alkenylene, or alkynylene group. The invention is useful for preparing medicines.

    摘要翻译: 本发明涉及式(I)的化合物,其中:n等于0或1; R1,R2,R3,R4表示氢或烷基,或R1和R3一起形成环烷基; R5代表氢,烷基,环烷基,环烷基烷基,芳基,芳烷基,杂芳基,杂芳烷基烷基,杂三环烷基,杂三环烷基烷基(全部任意取代)或-CO-R 6基团; 并且R 6表示R 7或OR 7或NR 7 R 8,其中R 7表示芳基,芳基烷基,杂芳基或杂芳基烷基,杂环烷基,杂环烷基烷基(全部被取代),R 8表示烷基,芳基,芳基烷基,杂芳基或杂芳基烷基(全部被取代) 或R 5和R 6与氮原子一起形成,Z基团带有饱和的单环,双环或三环基团,部分不饱和或不饱和的,具有5至16个含有1至7个杂原子和任选取代的链节; R 10表示氢原子或羟基,在后一种情况下,R 1,R 2,R 3,R 4独立地选自氢和烷基; Z表示羟基,烷氧基,烯氧基,苄氧基或NH-OR基; X表示硫,SO,SO 2基(在那些R3和R4不同于烷基的情况下)或基团-CO-O-(在这种情况下,R1和R3形成环烷基),或X表示氧 原子; W表示W1-(A)p或W1-B-W2-(A)p基团,其中W1和W2表示芳基或杂芳基,A是芳族环的标准取代基,B a键,氧或亚烷基 亚烯基,亚炔基,p为0〜5的整数。 T1和T2表示键或亚烷基,亚烯基或亚炔基。 本发明可用于制备药物。

    Phenylalanine enamide derivatives
    6.
    发明授权
    Phenylalanine enamide derivatives 失效
    苯丙氨酸烯酰胺衍生物

    公开(公告)号:US07645770B2

    公开(公告)日:2010-01-12

    申请号:US12327311

    申请日:2008-12-03

    IPC分类号: C07D471/04 A61K31/4375

    摘要: Phenylalanine enamide derivatives of formula (1) are described: wherein R1 is a group Ar1L2Ar2Alk- in which: Ar1 is an optionally substituted aromatic or heteroaromatic group; L2 is a covalent bond or a linker atom or group; Ar2 is an optionally substituted arylene or heteroarylene group; and Alk is a chain —CH2—CH(R)—, —CH═C(R)— or in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; X is an —O— or —S— atom or —N(R2)— group in which: Rx, Ry and Rz which may be the same or different is each a hydrogen atom or an optional substituent; or Rz is an atom or group as previously defined and Rx and Ry are joined together to form an optionally substituted spiro linked cycloaliphatic or heterocycloaliphatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immuno or inflammatory disorders or disorders involving the inappropriate growth or migration of cells.

    摘要翻译: 描述式(1)的苯丙氨酸烯酰胺衍生物:其中R1是Ar1L2Ar2Alk-基团,其中:Ar1是任选取代的芳族或杂芳族基团; L2是共价键或连接原子或基团; Ar 2是任选取代的亚芳基或亚杂芳基; 并且Alk是链-CH 2 -CH(R) - , - CH-C(R) - 或其中R是羧酸(-CO 2 H)或其衍生物或生物试剂; X是-O-或-S-原子或-N(R 2) - 基团,其中:可以相同或不同的R x,R y和R z各自为氢原子或任选的取代基; 或R z是如先前定义的原子或基团,并且R x和R y连接在一起以形成任选取代的螺环连接的脂环族或杂环脂族基团; 及其盐,溶剂合物,水合物和N-氧化物。 该化合物能够抑制整联蛋白与其配体的结合,并且可用于预防和治疗涉及细胞不适当生长或迁移的免疫或炎性疾病或病症。

    Phenylalanine Enamide Derivatives
    7.
    发明申请
    Phenylalanine Enamide Derivatives 失效
    苯丙氨酸酰胺衍生物

    公开(公告)号:US20070167483A1

    公开(公告)日:2007-07-19

    申请号:US11692612

    申请日:2007-03-28

    IPC分类号: A61K31/44

    摘要: Phenylalanine enamide derivatives of formula (1) are described: wherein R1 is a group Ar1L2Ar2Alk- in which: Ar1 is an optionally substituted aromatic or heteroaromatic group; L2 is a covalent bond or a linker atom or group; Ar2 is an optionally substituted arylene or heteroarylene group; and Alk is a chain in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; X is an —O— or —S— atom or —N(R2)— group in which: Rx, Ry and Rz which may be the same or different is each a hydrogen atom or an optional substituent; or Rz is an atom or group as previously defined and Rx and Ry are joined together to form an optionally substituted spiro linked cycloaliphatic or heterocycloaliphatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immuno or inflammatory disorders or disorders involving the inappropriate growth or migration of cells.

    摘要翻译: 描述了式(1)的苯丙氨酸烯酰胺衍生物:其中R 1是基团Ar 1,L 2,Ar 2, > Alk-其中:Ar 1是任选取代的芳族或杂芳族基团; L 2是共价键或连接原子或基团; Ar 2是任选取代的亚芳基或杂亚芳基; 和Alk是其中R是羧酸(-CO 2 H 2 H)或其衍生物或生物固体的链; X是-O-或-S-原子或-N(R 2)基团,其中:R x,R y和 R“可以相同或不同,各自为氢原子或任选的取代基; 或R z是如前所定义的原子或基团,并且R x和R y连接在一起形成任选取代的螺环连接的脂环族或 杂环脂族基团 及其盐,溶剂合物,水合物和N-氧化物。 该化合物能够抑制整联蛋白与其配体的结合,并且可用于预防和治疗涉及细胞不适当生长或迁移的免疫或炎性疾病或病症。

    Phenylalanine Enamide Derivatives
    8.
    发明申请
    Phenylalanine Enamide Derivatives 失效
    苯丙氨酸酰胺衍生物

    公开(公告)号:US20070027174A1

    公开(公告)日:2007-02-01

    申请号:US11533117

    申请日:2006-09-19

    摘要: Phenylalanine enamide derivatives of formula (1) are described: wherein R1 is a group Ar1L2Ar2Alk— in which: Ar1 is an optionally substituted aromatic or heteroaromatic group; L2 is a covalent bond or a linker atom or group; Ar2 is an optionally substituted arylene or heteroarylene group; and Alk is a chain —CH2—CH(R)—, —CH═C(R)— or in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; X is an —0— or —S— atom or —N(R2)— group in which: Rx, Ry and Rz which may be the same or different is each a hydrogen atom or an optional substituent; or Rz is an atom or group as previously defined and Rx and Ry are joined together to form an optionally substituted spiro linked cycloaliphatic or heterocycloaliphatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immuno or inflammatory disorders or disorders involving the inappropriate growth or migration of cells.

    摘要翻译: 描述了式(1)的苯丙氨酸烯酰胺衍生物:其中R 1是基团Ar 1,L 2,Ar 2, > Alk-其中:Ar 1是任选取代的芳族或杂芳族基团; L 2是共价键或连接原子或基团; Ar 2是任选取代的亚芳基或杂亚芳基; 并且Alk是一个链<?in-line-formula description =“In-line Formulas”end =“lead”?> CH 2 - (CH 2)-CH(R) - , - CH-C ) - 或<?in-line-formula description =“In-line Formulas”end =“tail”?>其中R是羧酸(-CO 2 H 2 H)或衍生物或生物体 的; X是-O-或-S-原子或-N(R 2 O) - 基团,其中:R x,R y和/或 R“可以相同或不同,各自为氢原子或任选的取代基; 或R z是如前所定义的原子或基团,并且R x和R y连接在一起形成任选取代的螺环连接的脂环族或 杂环脂族基团 及其盐,溶剂合物,水合物和N-氧化物。 该化合物能够抑制整联蛋白与其配体的结合,并且可用于预防和治疗涉及细胞不适当生长或迁移的免疫或炎性疾病或病症。