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    Benzospiroalkene compounds
    2.
    发明授权
    Benzospiroalkene compounds 失效
    苯并噻唑烯化合物

    公开(公告)号：US5648374A

    公开(公告)日：1997-07-15

    申请号：US420064

    申请日：1995-04-11

    申请人： Alex Cordi ,  Jean-Michel Lacoste ,  Michel Laubie ,  Tony Verbeuren ,  Jean-Jacques Descombes ,  Mark Millan

    发明人： Alex Cordi ,  Jean-Michel Lacoste ,  Michel Laubie ,  Tony Verbeuren ,  Jean-Jacques Descombes ,  Mark Millan

    IPC分类号： C07D277/60 ,  A61K31/415 ,  A61K31/4162 ,  A61K31/4184 ,  A61K31/4188 ,  A61K31/42 ,  A61K31/423 ,  A61K31/424 ,  A61K31/425 ,  A61K31/428 ,  A61K31/429 ,  A61P9/00 ,  A61P9/04 ,  A61P9/12 ,  A61P9/14 ,  A61P23/00 ,  A61P23/02 ,  A61P25/02 ,  A61P25/04 ,  A61P25/20 ,  A61P25/30 ,  A61P43/00 ,  C07D235/02 ,  C07D263/52 ,  C07D491/107 ,  C07D493/10 ,  C07D495/10 ,  C07D498/10 ,  C07D513/10 ,  C07D263/28

    CPC分类号： C07D235/02 ,  C07D263/52

    摘要： Compounds of formula (I): ##STR1## in which: X represents --CH.sub.2 --, --(CH.sub.2).sub.2 --, --CH.dbd.CH--, --O--CH.sub.2 --, --S--CH.sub.2 --, --SO--CH.sub.2 -- or --SO.sub.2 --CH.sub.2 --,Y represents oxygen or sulfur or --NR.sub.5 --,R.sub.1 represents halogen, linear or branched (C.sub.1 -C.sub.6) alkyl (unsubstituted or substituted), hydroxyl or linear or branched (C.sub.1 -C.sub.6) alkoxy,R.sub.2 represents hydrogen or halogen, linear or branched (C.sub.1 -C.sub.6) alkyl (unsubstituted or substituted), hydroxyl, linear or branched (C.sub.1 -C.sub.6) alkoxy or linear or branched (C.sub.1 -C.sub.6) alkylthio,R.sub.3 represents hydrogen or halogen, linear or branched (C.sub.1 -C.sub.6) alkyl (unsubstituted or substituted), hydroxyl, linear or branched (C.sub.1 -C.sub.6) alkoxy or linear or branched (C.sub.1 -C.sub.6) alkylthio,R.sub.4 represents hydrogen or amino (unsubstituted or substituted)R.sub.5 represents hydrogen or linear or branched (C.sub.1 -C.sub.6) alkyl, or alternativelyR.sub.1 and R.sub.2 form, together with the carbon atoms which bear them, a benzenic ring, on condition that, in this case, X represents --CH.sub.2 -- or --(CH.sub.2).sub.2 --, their isomers and their addition salts with a pharmaceutically acceptable acid, and medicinal product containing the same are useful as .alpha.2-adrenergic agonist.

    摘要翻译： 式（I）化合物：其中：X表示-CH 2 - ， - （CH 2）2 - ， - CH = CH - ， - O-CH 2 - ， - S-CH 2 - ，-SO- CH 2 - 或-SO 2 -CH 2 - ，Y表示氧或硫或-NR 5 - ，R 1表示卤素，直链或支链（C 1 -C 6）烷基（未取代或取代的），羟基或直链或支链（C 1 -C 6）烷氧基， 直链或支链（C1-C6）烷基（未取代或取代的），羟基，直链或支链（C1-C6）烷氧基或直链或支链（C1-C6）烷硫基，R3代表氢或卤素， 或支链（C1-C6）烷基（未取代或取代的），羟基，直链或支链（C1-C6）烷氧基或直链或支链（C1-C6）烷硫基，R4代表氢或氨基（未取代或取代的） 直链或支链（C1-C6）烷基，或者R1和R2与带有它们的碳原子一起形成苯环，条件是在这种情况下，X表示-CH 2 - 或 - （CH 2）2 - ，它们的异构体及其加成盐 一种药学上可接受的酸，以及含有该酸的药物可用作α2-肾上腺素能激动剂。

    Benzospiroalkenes
    3.
    发明授权
    Benzospiroalkenes 失效
    苯并噻唑烯

    公开(公告)号：US5486532A

    公开(公告)日：1996-01-23

    申请号：US276910

    申请日：1994-07-19

    申请人： Alex Cordi ,  Jean-Michel Lacoste ,  Michel Laubie ,  Tony Verbeuren ,  Jean-Jacques Descombes ,  Mark Millan

    发明人： Alex Cordi ,  Jean-Michel Lacoste ,  Michel Laubie ,  Tony Verbeuren ,  Jean-Jacques Descombes ,  Mark Millan

    IPC分类号： C07D277/60 ,  A61K31/415 ,  A61K31/4162 ,  A61K31/4184 ,  A61K31/4188 ,  A61K31/42 ,  A61K31/423 ,  A61K31/424 ,  A61K31/425 ,  A61K31/428 ,  A61K31/429 ,  A61P9/00 ,  A61P9/04 ,  A61P9/12 ,  A61P9/14 ,  A61P23/00 ,  A61P23/02 ,  A61P25/02 ,  A61P25/04 ,  A61P25/20 ,  A61P25/30 ,  A61P43/00 ,  C07D235/02 ,  C07D263/52 ,  C07D491/107 ,  C07D493/10 ,  C07D495/10 ,  C07D498/10 ,  C07D513/10 ,  C07D263/28

    CPC分类号： C07D235/02 ,  C07D263/52

    摘要： Compounds of formula (I): ##STR1## in which: X represents --CH.sub.2 --, --(CH.sub.2).sub.2 --, --CH.dbd.CH--, --O--CH.sub.2 --, --S--CH.sub.2 --, --SO--CH.sub.2 -- or --SO.sub.2 --CH.sub.2 --,Y represents oxygen or sulfur or --NR.sub.5 --,R.sub.1 represents halogen, linear or branched (C.sub.1 -C.sub.6) alkyl (unsubstituted or substituted), hydroxyl or linear or branched (C.sub.1 -C.sub.6) alkoxy,R.sub.2 represents hydrogen or halogen, linear or branched (C.sub.1 -C.sub.6) alkyl (unsubstituted or substituted), hydroxyl, linear or branched (C.sub.1 -C.sub.6) alkoxy or linear or branched (C.sub.1 -C.sub.6) alkylthio,R.sub.3 represents hydrogen or halogen, linear or branched (C.sub.1 -C.sub.6) alkyl (unsubstituted or substituted), hydroxyl, linear or branched (C.sub.1 -C.sub.6) alkoxy or linear or branched (C.sub.1 -C.sub.6) alkylthio,R.sub.4 represents hydrogen or amino (unsubstituted or substituted)R.sub.5 represents hydrogen or linear or branched (C.sub.1 -C.sub.6) alkyl,or alternativelyR.sub.1 and R.sub.2 form, together with the carbon atoms which bear them, a benzenic ring, on condition that, in this case, X represents --CH.sub.2 -- or --(CH.sub.2).sub.2 --, their isomers and their addition salts with a pharmaceutically acceptable acid, and medicinal product containing the same are useful as .alpha.2-adrenergic agonist.

    摘要翻译： 式（I）化合物：其中：X表示-CH 2 - ， - （CH 2）2 - ， - CH = CH - ， - O-CH 2 - ， - S-CH 2 - ，-SO- CH 2 - 或-SO 2 -CH 2 - ，Y表示氧或硫或-NR 5 - ，R 1表示卤素，直链或支链（C 1 -C 6）烷基（未取代或取代的），羟基或直链或支链（C 1 -C 6）烷氧基， 直链或支链（C1-C6）烷基（未取代或取代的），羟基，直链或支链（C1-C6）烷氧基或直链或支链（C1-C6）烷硫基，R3代表氢或卤素， 或支链（C1-C6）烷基（未取代或取代的），羟基，直链或支链（C1-C6）烷氧基或直链或支链（C1-C6）烷硫基，R4代表氢或氨基（未取代或取代的） 直链或支链（C1-C6）烷基，或者R1和R2与带有它们的碳原子一起形成苯环，条件是在这种情况下，X表示-CH 2 - 或 - （CH 2）2 - ，它们的异构体及其加成盐 一种药学上可接受的酸，以及含有该酸的药物可用作α2-肾上腺素能激动剂。

    Benzospiroalkene heterocyclic compounds
    4.
    发明授权
    Benzospiroalkene heterocyclic compounds 失效
    苯并四氢烯烃杂环化合物

    公开(公告)号：US5436261A

    公开(公告)日：1995-07-25

    申请号：US276918

    申请日：1994-07-19

    申请人： Alex Cordi ,  Jean-Michel Lacoste ,  Michel Laubie ,  Tony Verbeuren ,  Jean-Jacques Descombes

    发明人： Alex Cordi ,  Jean-Michel Lacoste ,  Michel Laubie ,  Tony Verbeuren ,  Jean-Jacques Descombes

    IPC分类号： A61K31/415 ,  A61K31/4162 ,  A61K31/4184 ,  A61K31/4188 ,  A61K31/42 ,  A61K31/423 ,  A61K31/424 ,  A61K31/425 ,  A61K31/429 ,  A61P25/02 ,  A61P25/04 ,  A61P25/06 ,  A61P43/00 ,  C07D235/02 ,  C07D263/52 ,  C07D491/10 ,  C07D491/107 ,  C07D495/10 ,  C07D498/10 ,  C07D513/10

    CPC分类号： C07D235/02 ,  C07D263/52 ,  C07D491/10 ,  C07D495/10

    摘要： Compounds of formula (I): ##STR1## in which: X represents --CH.sub.2 --, --(CH.sub.2).sub.2 --, --CH.dbd.CH--, --O--CH.sub.2 --, --S--CH.sub.2 --, --SO--CH.sub.2 -- or --SO.sub.2 --CH.sub.2 --,Y represents oxygen or sulfur or --NR.sub.6 --,R.sub.1 represents hydrogen or linear or branched (C.sub.1 -C.sub.6) alkyl,R.sub.2 represents hydrogen or halogen, linear or branched (C.sub.1 -C.sub.6) alkyl, (substituted or unsubstituted), hydroxyl, linear or branched (C.sub.1 -C.sub.6) alkoxy or linear or branched (C.sub.1 -C.sub.6) alkylthio,R.sub.3 represents hydrogen or halogen, linear or branched (C.sub.1 -C.sub.6) alkyl (substituted or unsubstituted), hydroxyl, linear or branched (C.sub.1 -C.sub.6) alkoxy or linear or branched (C.sub.1 -C.sub.6)alkylthio,R.sub.4 represents hydrogen (on condition that, in this case, R.sub.1 represents hydrogen), halogen, linear or branched (C.sub.1 -C.sub.6) alkyl (substituted or unsubstituted) or hydroxyl, or alternativelyR.sub.1 and R.sub.2, R.sub.2 and R.sub.3, R.sub.3 and R.sub.4 or R.sub.4 and X, together with the carbon atoms which bear them, form a benzene ring, on condition that, in the case where R.sub.1 and R.sub.2 form a benzene ring, X is other than --CH.sub.2 -- or --(CH.sub.2).sub.2 --,R.sub.5 represents hydrogen or amino (substituted or unsubstituted),R.sub.6 has the same meaning as R.sub.1,their isomers and also their. addition salts with a pharmaceutically acceptable acid and medicinal product containing the sarne are useful as partial .alpha..sub.1 and .alpha..sub.2 adrenergic agonist in the treatment of venous disease and migraine.

    摘要翻译： 式（I）化合物：其中：X表示-CH 2 - ， - （CH 2）2 - ， - CH = CH - ， - O-CH 2 - ， - S-CH 2 - ，-SO- CH2-或-SO2-CH2-，Y表示氧或硫或-NR6-，R1表示氢或直链或支链（C1-C6）烷基，R2表示氢或卤素，直链或支链（C1-C6）烷基，（ 取代或未取代的），羟基，直链或支链（C1-C6）烷氧基或直链或支链（C1-C6）烷硫基，R3表示氢或卤素，直链或支链（C1-C6）烷基（取代或未取代的） 直链或支链（C1-C6）烷氧基或直链或支链（C1-C6）烷硫基，R4代表氢（在这种情况下，R1表示氢），卤素，直链或支链（C1-C6）烷基 或未取代的）或羟基，或者R1和R2，R2和R3，R3和R4或R4和X与它们携带的碳原子一起形成苯环，条件是在R1和R2形成 苯环，X不是-CH 2 - 或 - （CH 2）2 - ， R5代表氢或氨基（取代或未取代的），R6具有与R1相同的含义，它们的异构体以及它们的含义。 与药学上可接受的酸和含有缬氨酸的药物的加成盐可用作治疗静脉疾病和偏头痛的部分α1和α2肾上腺素能激动剂。

    Novel tricyclic indole compound
    7.
    发明授权
    Novel tricyclic indole compound 失效

    公开(公告)号：US5030646A

    公开(公告)日：1991-07-09

    申请号：US446034

    申请日：1989-12-05

    申请人： Charles Malen ,  Jean-Michel Lacoste ,  Michel Laubie

    发明人： Charles Malen ,  Jean-Michel Lacoste ,  Michel Laubie

    IPC分类号： A61K31/40 ,  A61P1/08 ,  A61P9/00 ,  A61P25/04 ,  A61P25/20 ,  A61P25/28 ,  A61P43/00 ,  C07D495/04

    CPC分类号： C07D495/04

    摘要： The invention relates to compounds of general formula: ##STR1## in which A, B, G, D which may be identical or different, each denote a hydrogen atom or a halogen atom, a lower alkoxy group or alternatively a lower alkyl group optionally substituted with one or more halogen atoms,X denotes a hydrogen atom, a linear or branched lower alkyl group or a group SO.sub.2 E in which E denotes a linear or branched lower alkyl group or an aryl group optionally substituted with a linear or branched lower alkyl group,T denotes a hydrogen atom or a lower alkyl group,R.sub.3 denotes a hydrogen atom or a linear or branched lower alkyl group or an aryl group optionally substituted with one or more linear or branched lower alkyl groups,n and m, which may be identical or different, each denote 0 or 1,R.sub.1 and R.sub.2, which may be identical or different, each denote a hydrogen atom or a linear or branched lower alkyl group,or alternatively,R.sup.1 and R.sup.2 form, together with the nitrogen atom to which they are linked, a saturated or unsaturated, mono- or bicyclic nitrogenous heterocyclic system, each ring being 5- or 6-membered and optionally comprising one or two other hetero atoms selected from nitrogen, oxygen or sulfur, and optionally substituted with one or more linear or branched lower alkyl or alkoxy groups or with an aryl group which is itself optionally substituted with one or more lower alkyl, lower alkoxy or trifluoromethyl groups or alternatively one or more halogen atoms,or alternatively,R.sup.1 denotes a group ##STR2## in which R.sub.4, R.sub.5 and R.sub.6, which may be identical or different, each denote a hydrogen atom or a linear or branched lower alkyl group, or alternatively R.sub.4 forms with R.sub.5 a bridge (CH.sub.2).sub.p, p being between 2 and 4, or alternatively R.sub.1 denotes a dibenzo[a,d]cyclohept-5-yl group and R.sub.2 denotes a hydrogen atom, where appropriate, their isomers and also their addition salts with a pharmaceutically acceptable acid. Medicinal products.

    Peptide compounds derived from boronic acid
    8.
    发明授权
    Peptide compounds derived from boronic acid 失效
    衍生自硼酸的肽化合物

    公开(公告)号：US5585360A

    公开(公告)日：1996-12-17

    申请号：US458504

    申请日：1995-06-02

    申请人： Guillaume de Nanteuil ,  Christine Lila ,  Philippe Gloanec ,  Michel Laubie ,  Tony Verbeuren ,  Serge Simonet ,  Alain Rupin

    发明人： Guillaume de Nanteuil ,  Christine Lila ,  Philippe Gloanec ,  Michel Laubie ,  Tony Verbeuren ,  Serge Simonet ,  Alain Rupin

    IPC分类号： A61K38/55 ,  A61K38/00 ,  A61P7/04 ,  C07K1/06 ,  C07K5/06 ,  C07K5/065 ,  C07K14/81 ,  A61K38/06 ,  C07F9/22

    CPC分类号： C07K5/06191 ,  A61K38/00

    摘要： The invention relates to the compounds of formula (I): ##STR1## in which: R.sub.1 denotes hydrogen, acyl, alkoxycarbonyl, benzyloxycarbonyl, phenoxycarbonyl or linear or branched C.sub.1 -C.sub.6 alkyl, substituted or unsubstituted, or R.sub.6 SO.sub.2 -- in which R.sub.6 denotes alkyl, naphthyl, phenyl, benzyl or morpholine,R.sub.2 denotes hydrogen or phenyl, substituted or unsubstituted benzyl, thienylmethyl, (pyridyl)methyl, diphenylmethyl, fluorenyl, naphthylmethyl, benzocyclobutyl, (dicyclopropylmethyl)methyl, indanyl or (C.sub.3 -C.sub.7 cycloalkyl)methyl,R'.sub.2 denotes hydrogen or elseR.sub.2 and R'.sub.2 together denote C.sub.6 H.sub.5 --CH.dbd.,R.sub.3 denotes any one of the groups as defined in the description, each of R.sub.4 and R.sub.5 denotes hydrogen or alkyl, or ##STR2## forms a boronic ester of pinanediol, A denotes the following group: ##STR3## in which n and A.sub.2 are as defined in the description, and medicinal products containing the same are useful as thrombin inhibitors.

    摘要翻译： 本发明涉及式（I）的化合物：其中：R1表示氢，酰基，烷氧基羰基，苄氧基羰基，苯氧基羰基或直链或支链C1-C6烷基，取代或未取代的或R6SO2-，其中R6 （吡啶基）甲基，二苯基甲基，芴基，萘基甲基，苯并环丁基，（二环丙基甲基）甲基，二氢化茚基或（C 3 -C 7环烷基） 甲基，R'2表示氢，或者R2和R'2一起表示C 6 H 5 -CH =，R 3表示说明书中定义的基团中的任一个，R 4和R 5各自表示氢或烷基，或者形成 蒎二醇的硼酸酯，A表示以下基团：其中n和A2如说明书中所定义的，含有它们的药物可用作凝血酶抑制剂。

    Peptide compounds derived from boronic acid
    9.
    发明授权
    Peptide compounds derived from boronic acid 失效
    衍生自硼酸的肽化合物

    公开(公告)号：US5444049A

    公开(公告)日：1995-08-22

    申请号：US199473

    申请日：1994-02-22

    申请人： Guillaume de Nanteuil ,  Christine Lila ,  Michel Laubie ,  Tony Verbeuren ,  Serge Simonet ,  Alain Rupin ,  Bernard Portevin

    发明人： Guillaume de Nanteuil ,  Christine Lila ,  Michel Laubie ,  Tony Verbeuren ,  Serge Simonet ,  Alain Rupin ,  Bernard Portevin

    IPC分类号： A61K38/55 ,  A61K38/00 ,  A61P7/02 ,  C07F5/02 ,  C07K1/113 ,  C07K5/06 ,  C07K5/065 ,  C07K5/078 ,  C07K14/81 ,  A61K38/06

    CPC分类号： C07K5/06191 ,  C07F5/025 ,  A61K38/00

    摘要： A compound of formula (I): ##STR1## in which: R.sub.1 represents hydrogen or acyl, alkyl, benzyl, alkoxycarbonyl, benzyloxycarbonyl, phenoxycarbonyl, 5-[(dimethyl)amino]naphthylsulfonyl, alkoxycarbonylmethyl or carboxymethyl,R.sub.2 represents hydrogen or phenyl, substituted or unsubstituted benzyl, 3-thienylmethyl, 2-pyridylmethyl, diphenylmethyl, fluorenyl, naphthylmethyl, benzocyclobutyl, (dicyclopropylmethyl)methyl, indanyl or (C.sub.3 -C.sub.7 cycloalkyl)methyl,R'.sub.2 represents hydrogen or benzylor alternativelyR.sub.2 and R'.sub.2 together represent C.sub.6 H.sub.5 --CH.dbd.,R.sub.3 represents substituted alkyl or guanidinophenyl, amidinophenyl, aminophenyl, guanidinobenzyl, amidinobenzyl, aminobenzyl or cycloalkyl,R.sub.4 and R.sub.5 each represent hydrogen or alkyl, or ##STR2## forms a boronic ester of pinanediol, A represents any one of the groups as defined in the description.Medicinal products.

    摘要翻译： 式（I）化合物：其中：R 1表示氢或酰基，烷基，苄基，烷氧基羰基，苄氧基羰基，苯氧基羰基，5 - [（二甲基）氨基]萘基磺酰基，烷氧基羰基甲基或羧甲基， 或苯基，取代或未取代的苄基，3-噻吩基甲基，2-吡啶基甲基，二苯基甲基，芴基，萘基甲基，苯并环丁基，（二环丙基甲基）甲基，茚满基或（C 3 -C 7环烷基）甲基，R 12代表氢或苄基， R 2一起代表C 6 H 5 -CH =，R 3表示取代的烷基或胍基苯基，脒基苯基，氨基苯基，胍基苄基，脒基苄基，氨基苄基或环烷基，R 4和R 5各自代表氢或烷基，或者“IMAGE”形成蒎二醇的硼酸酯 表示说明书中定义的组中的任何一个。 药用产品。