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    Analgesic oxazolopyridine compounds
    1.
    发明授权
    Analgesic oxazolopyridine compounds 失效
    镇痛恶唑吡啶化合物

    公开(公告)号：US5061713A

    公开(公告)日：1991-10-29

    申请号：US564033

    申请日：1990-08-07

    申请人： Gerald Guillaumet ,  Christine Flouzat ,  Jacqueline Bonnet

    发明人： Gerald Guillaumet ,  Christine Flouzat ,  Jacqueline Bonnet

    IPC分类号： A61K31/44 ,  A61K31/50 ,  A61K31/505 ,  A61K31/53 ,  A61P25/04 ,  C07D498/04

    CPC分类号： C07D498/04

    摘要： Compound of general formula (I): ##STR1## in which: X, Y, Z and T each represent, independently of one another, a nitrogen atom, a --CH.dbd. group or a group CW, in which W represents a halogen atom or a lower alkyl or alkoxy group optionally substituted with one or more halogen atoms, such as a trifluoromethyl group, on condition that only one of them represents a nitrogen atom,Ra, Rb, Rc, Rd and Re represent, independently of one another, a hydrogen atom, a halogen atom or a lower alkyl or alkoxy group optionally substituted with one or more halogen atoms, such as a trifluoromethyl group,B represents a hydrogen atom and D a hydroxyl group, or B and D simultaneously represent an oxygen atom,n represents 1 or 2, andR.sub.1 represents a hydrogen atom, a linear or branched lower alkyl, linear or branched lower alkenyl, aryl or lower arylalkyl group or a cycloalkyl group having 3 to 7 carbon atoms, it being possible for each of the lower alkyl, lower alkenyl, aryl, lower arylalkyl and cycloalkyl groups to be substituted with one or more halogen atoms or a lower alkyl or alkoxy group optionally substituted with one or more halogen atoms, such as a trifluoromethyl group,their isomers, epimers and diastereoisomers, and addition salts with a pharmaceutically acceptable acidare useful in the treatment of pain.

    摘要翻译： 通式（I）的化合物：其中：X，Y，Z和T​​各自独立地表示氮原子，-CH =基团或基团CW，其中W表示 卤素原子或任选被一个或多个卤素原子取代的低级烷基或烷氧基，例如三氟甲基，条件是只有一个表示氮原子，Ra，Rb，Rc，Rd和Re独立地表示 另一方面，氢原子，卤原子或任选被一个或多个卤素原子取代的低级烷基或烷氧基，例如三氟甲基，B表示氢原子，D表示羟基，或者B和D同时表示 氧原子，n表示1或2，R1表示氢原子，直链或支链的低级烷基，直链或支链的低级烯基，芳基或低级芳基烷基或具有3至7个碳原子的环烷基，每种 的低级烷基，低级烯基，芳基，低级芳基烷基和环亚烷基 被一个或多个卤素原子取代的烷基或任选被一个或多个卤素原子取代的低级烷基或烷氧基，例如三氟甲基，它们的异构体，差向异构体和非对映异构体，以及与药学上可接受的酸的加成盐是有用的 在治疗疼痛。

    Oxazolopyridine compounds
    2.
    发明授权
    Oxazolopyridine compounds 失效
    氧杂环丁烯化合物

    公开(公告)号：US5084456A

    公开(公告)日：1992-01-28

    申请号：US564035

    申请日：1990-08-07

    申请人： Gerald Guillaumet ,  Christine Flouzat ,  Jacqueline Bonnet

    发明人： Gerald Guillaumet ,  Christine Flouzat ,  Jacqueline Bonnet

    IPC分类号： A61K31/44 ,  A61K31/4412 ,  A61K31/4418 ,  A61K31/4427 ,  A61K31/495 ,  A61P25/04 ,  C07D213/74 ,  C07D401/12 ,  C07D417/12 ,  C07D498/04

    CPC分类号： C07D213/74

    摘要： Compounds of general formula (I): ##STR1## in which: R.sub.1 and R.sub.2 each represent a hydrogen atom or, with the oxygen and nitrogen, form an --O--CO--N-- linkage,W represents a halogen atom or a lower alkyl or alkoxy group optionally substituted with one or more halogen atoms, such as trifluoromethyl, and m being between 0 and 3,A represents a linear or branched lower alkylene group, andAr represents an aryl or heteroaryl group optionally substituted with one or more halogen atoms or with one or more lower alkyl, hydroxy, hydroxysulfonyloxy, lower alkoxy or aryloxy groups optionally substituted with one or more halogen atoms, such as a trifluoromethyl group,on the understanding that lower alkyl or lower alkyloxy radical is understood to mean a linear or branched alkyl group comprising from 1 to 6 carbon atom, their isomers, epimers and diastereoisomers. Medicinal products useful in the treatment of pain.

    摘要翻译： 通式（I）的化合物：其中：R1和R2各自表示氢原子，或者与氧和氮形成-O-CO-N-键，W表示卤原子或 任选被一个或多个卤素原子取代的低级烷基或烷氧基，例如三氟甲基，m在0和3之间，A代表直链或支链的低级亚烷基，Ar表示任选被一个或多个 更多的卤素原子或与一个或多个低级烷基，羟基，羟基磺酰氧基，任选被一个或多个卤素原子取代的低级烷氧基或芳氧基，例如三氟甲基，因为低级烷基或低级烷氧基被理解为是指 包含1至6个碳原子的直链或支链烷基，它们的异构体，差向异构体和非对映异构体。 用于治疗疼痛的药用产品。

    Metalloproteinase inhibitors
    3.
    发明授权
    Metalloproteinase inhibitors 失效
    金属蛋白酶抑制剂

    公开(公告)号：US6066633A

    公开(公告)日：2000-05-23

    申请号：US191323

    申请日：1998-11-13

    申请人： Guillaume De Nanteuil ,  Georges Remond ,  Joseph Paladino ,  Ghanem Atassi ,  Alain Pierre ,  Gordon Tucker ,  Jacqueline Bonnet ,  Massimo Sabatini

    发明人： Guillaume De Nanteuil ,  Georges Remond ,  Joseph Paladino ,  Ghanem Atassi ,  Alain Pierre ,  Gordon Tucker ,  Jacqueline Bonnet ,  Massimo Sabatini

    IPC分类号： A61K31/00 ,  A61K31/435 ,  A61K31/4353 ,  A61K31/437 ,  A61P9/00 ,  A61P9/10 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D471/04 ,  A61K31/5377 ,  A61K31/4523 ,  C07D487/44

    CPC分类号： C07D471/04

    摘要： Compound of formula (I): ##STR1## in which: m represents an integer from 1 to 4 inclusive, and n and p an integer from 0 to 4 inclusive,X represents O, S or a single bond,R.sub.1 represent hydrogen or halogen, or alkyl, alkoxy, hydroxy, trihaloalkyl or trihaloalkoxy,R.sub.2, R.sub.3 and R.sub.4, which may be same or different, each represents hydrogen or alkyl,R.sub.5 represents hydrogen or halogen, or alkoxy, aryloxy or heteroaryloxy,R.sub.6, R.sub.7 and R.sub.8, which may be same or different, each represents hydrogen or alkyl, or together form, with the atoms carrying them respectively, an optionally substituted heterocycle,R.sub.9 represents SO.sub.3 H, --CO.sub.2 R.sub.10, --CO--NR.sub.11 R.sub.12, or --NR.sub.13 R.sub.14, wherein R.sub.10, R.sub.11, R.sub.12, R.sub.13 and R.sub.14 each represents hydrogen or alkyl or together (R.sub.11 /R.sub.12 ; R.sub.13 /R.sub.14) form, with nitrogen carrying them, heterocycle,isomers thereof, and addition salts thereof with a pharmaceutically-acceptable acid or base.

    摘要翻译： 式（I）的化合物：其中：m表示1〜4的整数，n和p为0〜4的整数，X表示O，S或单键，R 1表示氢或卤素，或烷基 ，烷氧基，羟基，三卤代烷基或三卤代烷氧基，可以相同或不同的R 2，R 3和R 4各自表示氢或烷基，R 5表示氢或卤素，或烷氧基，芳氧基或杂芳氧基，R 6，R 7和R 8，其可以是 相同或不同，各自表示氢或烷基，或与分别携带它们的原子一起形成任选取代的杂环，R 9表示SO 3 H，-CO 2 R 10，-CO-NR 11 R 12或-NR 13 R 14，其中R 10，R 11，R 12，R 13 和R 14各自表示氢或烷基或一起（R 11 / R 12; R 13 / R 14），带有氮的杂环，杂环，异构体及其与药学上可接受的酸或碱的加成盐。

    Thiophene compounds
    4.
    发明授权
    Thiophene compounds 失效
    噻吩化合物

    公开(公告)号：US5705525A

    公开(公告)日：1998-01-06

    申请号：US605537

    申请日：1996-02-22

    申请人： Michel Wierzbicki ,  Frederic Sauveur ,  Jacqueline Bonnet ,  Charles Tordjman

    发明人： Michel Wierzbicki ,  Frederic Sauveur ,  Jacqueline Bonnet ,  Charles Tordjman

    IPC分类号： A61K31/38 ,  A61K31/381 ,  A61P1/00 ,  A61P17/00 ,  A61P29/00 ,  C07D333/24 ,  C07D333/16 ,  C07D333/20

    CPC分类号： C07D333/24

    摘要： The invention relates to thiophene compounds of formula: ##STR1## wherein: X.sub.1, X.sub.2, Y.sub.1 and Y.sub.2, which are identical or different, each represents hydrogen or halogen, (C.sub.1 -C.sub.5)-alkyl or alkoxy, or trifluoromethyl, R.sub.1 represents hydrogen or (C.sub.1 -C.sub.5)-alkyl, A represents a straight (C.sub.1 -C.sub.5)-hydrocarbon chain of which each carbon atom is optionally mono- or di-substituted by a (C.sub.1 -C.sub.5)-alkyl, and R.sub.2 represents hydrogen, (C.sub.1 -C.sub.6)-alkyl, cyclohexyl or benzyl; and their physiologically tolerable salts. The products of the invention may be used as anti-inflammatory agents.

    摘要翻译： 本发明涉及下式的噻吩化合物：其中：X 1，X 2，Y 1和Y 2相同或不同，各自表示氢或卤素，（C 1 -C 5） - 烷基或烷氧基或三氟甲基，R 1表示氢 或（C 1 -C 5） - 烷基，A表示直链（C 1 -C 5） - 烃链，其中每个碳原子任选被（C 1 -C 5） - 烷基单取代或二取代，并且R 2表示氢，（ C 1 -C 6） - 烷基，环己基或苄基; 及其生理上可耐受的盐。 本发明的产品可以用作抗炎剂。

    Carboxylic and hydroxamic acid compounds inhibiting metalloproteases, method for preparing same and pharmaceutical compositions containing them
    9.
    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。

    Thiophene compounds
    10.
    再颁专利
    Thiophene compounds 失效
    噻吩化合物

    公开(公告)号：USRE37078E1

    公开(公告)日：2001-02-27

    申请号：US09368343

    申请日：1999-08-03

    申请人： Michel Wierzbicki ,  Frédéric Sauveur ,  Jacqueline Bonnet ,  Charles Tordjman

    发明人： Michel Wierzbicki ,  Frédéric Sauveur ,  Jacqueline Bonnet ,  Charles Tordjman

    IPC分类号： A61K3138

    CPC分类号： C07D333/24

    摘要： The invention relates to thiophene compounds of formula: wherein: X1, X2, Y1 and Y2, which are identical or different, each represents hydrogen or halogen, (C1-C5)-alkyl or alkoxy, or trifluoromethyl, X1 and Y1, which are identical or different, each represents C1-C5 alkoxy, X2 and Y2 each represents hydrogen, R1 represents hydrogen or (C1-C5)-alkyl, A represents a straight (C1-C5)-hydrocarbon chain of which each carbon atom is optionally mono- or di-substituted by a (C1-C5)-alkyl, and R2 represents hydrogen, (C1-C6)-alkyl, cyclohexyl or benzyl; and their physiologically tolerable salts. The products of the invention may be used as anti-inflammatory agents.

    摘要翻译： 本发明涉及下式的噻吩化合物：其中：相同或不同的X1，X2，Y1和Y2各自表示氢或卤素，其中： X1和Y1， 它们相同或不同，各自表示C1-C5烷氧基，X2和Y2各自表示氢，R1表示氢或（C1-C5） - 烷基，A表示直链 （C 1 -C 5） - 烃链，其中每个碳原子任选被（C 1 -C 5） - 烷基单取代或二取代，R 2表示氢，（C 1 -C 6） - 烷基，环己基或苄基; 本发明的产品可以用作抗炎剂。