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    Cycloheptene compounds
    3.
    发明授权
    Cycloheptene compounds 失效
    环庚烯化合物

    公开(公告)号：US06638962B2

    公开(公告)日：2003-10-28

    申请号：US10050666

    申请日：2002-01-16

    申请人： Patrick Casara ,  Thierry Le Diguarher ,  Gilbert Dorey ,  John Hickman ,  Alain Pierre ,  Gordon Tucker ,  Nicolas Guilbaud

    发明人： Patrick Casara ,  Thierry Le Diguarher ,  Gilbert Dorey ,  John Hickman ,  Alain Pierre ,  Gordon Tucker ,  Nicolas Guilbaud

    IPC分类号： A61K314174

    CPC分类号： C07D233/64 ,  A61K31/4164 ,  C07D213/38 ,  C07D401/06

    摘要： Compound of formula (I): wherein: X represents a bond or alkylene, CO, S(O)n, —S(O)n—A1—, —CO—A1—, —A—S(O)n—A′1— or —A1—CO—A′1—, Y represents aryl, heteroaryl, cycloalkyl or heterocycloalkyl, each unsubstituted or substituted, R1, R2, R3 and R4 each independently of the others represent hydrogen or aryl, heteroaryl, cycloalkyl or heterocycloalkyl, each unsubstituted or substituted, or R1, R2, R3 and R4, taken in pairs, together form a bond, or form a fused benzene ring or a fused aromatic or partially unsaturated heterocycle, T represents —CH(R5)—, —N(R5)— or —N(R5)CO—, V represents hydrogen or unsubstituted or substituted aryl or heteroaryl, A2 represents [C(R6)(R′6)]p, R7 and R8 are as defined in the description, their isomers and addition salts thereof with a pharmaceutically acceptable acid or base and medicinal products containing the same are useful as farnesyl transferase inhibitors.

    摘要翻译： 式（I）的化合物：其中：X表示键或亚烷基，CO，S（O）n，-S（O）n -A1，-CO-A1-，-AS（O）n-A'1 - 或-A1-CO-A'1-，Y表示芳基，杂芳基，环烷基或杂环烷基，每个未取代或取代的，R 1，R 2，R 3和R 4各自独立地表示氢或芳基，杂芳基，环烷基或杂环烷基， 每个未取代或取代的或R 1，R 2，R 3和R 4成对取代，一起形成键，或形成稠合苯环或稠合芳族或部分不饱和杂环，T表示-CH（R 5） - ， - N（ R5） - 或-N（R5）CO-，V表示氢或未取代或取代的芳基或杂芳基，A2表示[C（R6）（R'6）] p，R7和R8如说明书中所定义， 并且其与药学上可接受的酸或碱的加成盐和含有它们的药物可用作法呢基转移酶抑制剂。

    Carboxylic and hydroxamic acid compounds inhibiting metalloproteases, method for preparing same and pharmaceutical compositions containing them
    4.
    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

    申请人： Patrick Casara ,  Anne Marie Chollet ,  Thierry Le Diguarher ,  Ghanem Atassi ,  Jacqueline Bonnet ,  Alain Pierre ,  Massimo Sabatini ,  Gordon Tucker ,  Nicolas Guilbaud

    发明人： Patrick Casara ,  Anne Marie Chollet ,  Thierry Le Diguarher ,  Ghanem Atassi ,  Jacqueline Bonnet ,  Alain Pierre ,  Massimo Sabatini ,  Gordon Tucker ,  Nicolas Guilbaud

    IPC分类号： C07D20948

    CPC分类号： C07D209/48 ,  C07C233/82 ,  C07C259/10 ,  C07C311/29 ,  C07D231/22 ,  C07D237/32 ,  C07D239/96 ,  C07D253/08 ,  C07D275/06 ,  C07D403/12 ,  C07D409/12 ,  C07D471/04

    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。