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58 条记录 (耗时 0.021 秒)

    Carboxylic and hydroxamic acid compounds inhibiting metalloproteases, method for preparing same and pharmaceutical compositions containing them
    5.
    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。

    Dihydrofuro[3,4-b]quinolin-1-one compounds
    7.
    发明授权
    Dihydrofuro[3,4-b]quinolin-1-one compounds 失效
    二氢呋喃并[3,4-b]喹啉-1-酮化合物

    公开(公告)号：US06548515B1

    公开(公告)日：2003-04-15

    申请号：US09718917

    申请日：2000-11-22

    申请人： Henri-Philippe Husson ,  Sylviane Giorgi-Renault ,  Christophe Tratrat ,  Ghanem Atassi ,  Alain Pierre ,  Pierre Renard ,  Bruno Pfeiffer

    发明人： Henri-Philippe Husson ,  Sylviane Giorgi-Renault ,  Christophe Tratrat ,  Ghanem Atassi ,  Alain Pierre ,  Pierre Renard ,  Bruno Pfeiffer

    IPC分类号： A61K314741

    CPC分类号： C07D491/04 ,  C07D219/06 ,  C07D221/16 ,  C07D221/18 ,  C07D491/14 ,  C07D495/04

    摘要： The invention relates to compound of formula (I): wherein: represents a single or double bond, R0 represents hydrogen or hydroxy or alkoxy, R1 and R2, which are identical or different, each represents hydrogen or halogen or alkyl, alkoxy, hydroxy, polyhaloalkyl, nitro or optionally substituted amino or  wherein m represents an integer such that 1≦m≦4, or form together with the carbon atoms carrying them an aromatic or non-aromatic, mono- or bi-cyclic group having from 5 to 12 ring members and optionally containing 1 or 2 hetero atoms selected from O, S and N, R3 represents hydrogen or aryl, heteroaryl, cycloalkyl, optionally substituted alkyl or a group of formula COR7 wherein R7 represents aryl, optionally substituted alkyl, optionally substituted amino or OR10 wherein R10 represents aryl or optionally substituted alkyl, X represents oxygen or sulphur or —CH2— or —CH2—CH2—, Ar represents aryl, heteroaryl or arylalkyl, its optical isomers, its hydrates, solvates, and also its addition salts with a pharmaceutically acceptable acid. Medicinal products containing the same are useful in the treatment of cancer.

    摘要翻译： 本发明涉及式（I）的化合物：其中：表示单键或双键，R 0表示氢或羟基或烷氧基，R 1和R 2相同或不同，各自表示氢或卤素或烷基，烷氧基，羟基，多卤代烷基，硝基或任选取代的氨基或 其中m表示1≤= m = 4的整数，或与带有带有5至12个环成员的芳族或非芳族单环或双环基团的碳原子一起形成，并且任选地含有1或 2个选自O，S和N的杂原子，R 3表示氢或芳基，杂芳基，环烷基，任选取代的烷基或式COR7基团，其中R7表示芳基，任选取代的烷基，任选取代的氨基或OR 10，其中R 10表示芳基或任选地 取代的烷基，X表示氧或硫或-CH 2 - 或-CH 2-CH 2 - ，Ar表示芳基，杂芳基或芳基烷基，其光学异构体，其水合物，溶剂合物，以及其与药学上可接受的酸的加成盐。含有它们的医药产品可用于治疗癌症。

    12,13-(pyranosyl)-indolo[2,3-a]pyrrolo[3,4-c]carbazole and 12,13-(pyranosyl)-furo[3,4-c]indolo[2,3-a]carbazoles
    9.
    发明授权
    12,13-(pyranosyl)-indolo[2,3-a]pyrrolo[3,4-c]carbazole and 12,13-(pyranosyl)-furo[3,4-c]indolo[2,3-a]carbazoles 失效
    12,13-（吡喃糖基） - 吲哚并[2,3-a]吡咯并[3,4-c]咔唑和12,13-（吡喃糖基） - 呋喃并[3,4-c]吲哚并[2,3-a] 咔唑

    公开(公告)号：US06569858B2

    公开(公告)日：2003-05-27

    申请号：US10010379

    申请日：2001-11-05

    申请人： Michelle Prudhomme ,  Pascale Moreau ,  Fabrice Anizon ,  Christelle Marminon ,  Ghanem Atassi ,  Alain Pierre ,  Bruno Pfeiffer ,  Pierre Renard

    发明人： Michelle Prudhomme ,  Pascale Moreau ,  Fabrice Anizon ,  Christelle Marminon ,  Ghanem Atassi ,  Alain Pierre ,  Bruno Pfeiffer ,  Pierre Renard

    IPC分类号： C07D49044

    CPC分类号： C07H19/23

    摘要： A compound selected from those of formula (I): wherein: R1 and R2, which may be identical or different, represent a group of formula U-V wherein U represents single bond, or alkylene which is optionally substituted and/or unsaturated, and V is as defined in the description, G represents oxygen, or NR3 wherein R3 is as defined in the description, X represents hydrogen, hydroxy, alkoxy, mercapto or alkylthio, Y represents hydrogen, or X+Y represents carbonyl, X1 represents hydrogen, hydroxy, alkoxy, mercapto or alkylthio, Y1 represents hydrogen, or X1+Y1 represents carbonyl, R4, R5, and R6 are as defined in the description, its isomers, and pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same are useful in the treatment of cancer.

    摘要翻译： 选自式（I）的化合物：其中：R 1和R 2可以相同或不同，表示其中U表示单键的式UV基团，或任选被取代和/或不饱和的亚烷基，V是 G表示氧或NR 3，其中R3如说明书中所定义，X表示氢，羟基，烷氧基，巯基或烷硫基，Y表示氢，或X + Y表示羰基，X1表示氢，羟基， 烷氧基，巯基或烷硫基，Y1表示氢，或X1 + Y1表示羰基，R4，R5和R6如说明书中所定义，其异构体及其药学上可接受的酸或碱加成盐，以及含有它们的药物 可用于治疗癌症。

    Camptothecin analogue compounds
    10.
    发明授权
    Camptothecin analogue compounds 失效
    喜树碱类似物

    公开(公告)号：US06509345B2

    公开(公告)日：2003-01-21

    申请号：US10010380

    申请日：2001-11-05

    申请人： Gilbert Lavielle ,  Patrick Hautefaye ,  Alain Pierre ,  Ghanem Atassi ,  John Hickman ,  Bernard Cimetiere

    发明人： Gilbert Lavielle ,  Patrick Hautefaye ,  Alain Pierre ,  Ghanem Atassi ,  John Hickman ,  Bernard Cimetiere

    IPC分类号： C07D47114

    CPC分类号： C07D471/14 ,  A61K31/4745 ,  Y02P20/55

    摘要： Compound of formula (I): wherein: n is 0, 1 or 2, R1, R2, R3, R4 and R5 are selected from hydrogen, halogen, alkyl, alkenyl, alkynyl, perhaloalkyl, cycloalkyl, cycloalkylalkyl, hydroxy, hydroxyalkyl, alkoxy, alkoxyalkyl, alkoxycarbonyl, acyloxy, carboxy, nitro, cyano, aminocarbonyl (optionally substituted), and the groups (CH2)p—NRaRb and —O—C(O)—N—RaRb, with p, Ra and Rb being as defined in the description, or two adjacent groups R2, R3, R4 and R5 together form a group —O—(CH2)t—O, t being an integer from 1 to 3, R60, R70n, R80 and R90 represent a hydrogen atom, a hydroxy group, an alkoxy group, or an O—(CO)—X or O—(CO)—NXW group as defined in the description, R61, R71n, R81 and R91 represent a hydrogen atom, alkyl, alkenyl or alkynyl, or taken in pairs together form a bond or an oxirane group, or two groups together form an oxo group. and medicinal products containing the same are useful for the treatment of cancerous diseases.

    摘要翻译： 式（I）化合物：其中：n为0,1或2，R1，R2，R3，R4和R5选自氢，卤素，烷基，烯基，炔基，全卤代烷基，环烷基，环烷基烷基，羟基，羟烷基，烷氧基 ，烷氧基烷基，烷氧基羰基，酰氧基，羧基，硝基，氰基，氨基羰基（任选取代的）和基团（CH 2）p -NR a R b和-OC（O）-NR a R b，其中p，R a和R b如 描述或两个相邻基团R 2，R 3，R 4和R 5一起形成基团-O-（CH 2）t O，t为1至3的整数，R 60，R 70n，R 80和R 90表示氢原子，羟基， 烷氧基或描述中定义的O-（CO）-X或O-（CO）-NXW基团，R61，R71n，R81和R91表示氢原子，烷基，烯基或炔基，或成对取代 一起形成键或环氧乙烷基团，或两个基团一起形成氧代基，并且含有该氧基的药物可用于治疗癌性疾病。