利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

28 条记录 (耗时 0.057 秒)

    Substituted diamino-1,3,5-triazine derivatives
    21.
    发明授权
    Substituted diamino-1,3,5-triazine derivatives 失效
    取代的二氨基-1,3,5-三嗪衍生物

    公开(公告)号：US06858609B2

    公开(公告)日：2005-02-22

    申请号：US10002456

    申请日：2001-11-15

    申请人： Paul A. J. Janssen ,  Jan Heeres ,  Henri E. L. Moereels ,  Michael Joseph Kukla ,  Donald W. Ludovici

    发明人： Paul A. J. Janssen ,  Jan Heeres ,  Henri E. L. Moereels ,  Michael Joseph Kukla ,  Donald W. Ludovici

    IPC分类号： A61K31/53 ,  A61P31/12 ,  A61P31/18 ,  A61P37/04 ,  C07D251/18 ,  C07D251/22 ,  C07D403/06 ,  C07D405/12 ,  C07D409/12 ,  C07D251/42

    CPC分类号： C07D403/06 ,  C07D251/18 ,  C07D251/48 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12

    摘要： This invention concerns the compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R1 and R2 are each independently selected from hydrogen; hydroxy; amino; optionally substituted C1-6alkyl; C1-6alkyloxy; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; Ar1; mono- or di(C1-6alkyl)amino; mono- or di(C1-6alkyl)-aminocarbonyl; dihydro-2(3H7)-furanone; or R1 and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-6alkyl)amino-C1-4alkylidene; R3 is hydrogen, Ar1, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxy-carbonyl, C1-6alkyl substituted with C1-6alkyloxycarbonyl; and R4, R5, R6, R7 and R8 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl or trihalomethyloxy; L is optionally substituted C1-10alkyl; C3-10alkenyl; C3-10alkynyl; C3-7cycloalkyl; Ar1 is optionally substituted phenyl; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection. It further relates to new compounds being a subgroup of the compounds of formula (I), their preparation and compositions comprising them.

    摘要翻译： 本发明涉及配制药学上可接受的酸加成盐及其立体化学异构形式的化合物，其中R 1和R 2各自独立地选自氢; 羟基; 氨基; 任选取代的C 1-6烷基; C 1-6烷氧基; C 1-6烷基羰基; C 1-6烷氧基羰基; Ar <1>; 单或二（C 1-6烷基）氨基; 单或二（C 1-6烷基） - 氨基羰基; 二氢-2（3H7） - 呋喃酮; 或R 1和R 2一起可以形成吡咯烷基，哌啶基，吗啉基，叠氮基或单或二（C 1-6烷基）氨基-C 1-4亚烷基; R 3是氢，Ar 1，C 1-6烷基羰基，C 1-6烷基，C 1-6烷氧基羰基，被C 1-6烷氧基羰基取代的C 1-6烷基; R 4，R 5，R 6，R 7和R 8各自独立地选自氢，卤素，C 1-6烷基，C 1-6烷氧基，氰基，氨基羰基，硝基，氨基， 三卤甲基或三卤代甲氧基; L是任选取代的C 1-10烷基; C3-10烯基; C3-10炔基; C 3-7环烷基; Ar 1是任选取代的苯基; 用于制造用于治疗患有HIV（人类免疫缺陷病毒）感染的受试者的药物。 它还涉及作为式（I）化合物的亚组的新化合物，其制备方法和包含它们的组合物。

    Substituted diamino-1,3,5-triazine derivatives
    22.
    发明授权
    Substituted diamino-1,3,5-triazine derivatives 失效
    取代的二氨基-1,3,5-三嗪衍生物

    公开(公告)号：US06380194B1

    公开(公告)日：2002-04-30

    申请号：US08938602

    申请日：1997-09-26

    申请人： Paul A. J. Janssen ,  Jan Heeres ,  Henri E. L. Moereels ,  Michael Joseph Kukla ,  Donald W. Ludovici

    发明人： Paul A. J. Janssen ,  Jan Heeres ,  Henri E. L. Moereels ,  Michael Joseph Kukla ,  Donald W. Ludovici

    IPC分类号： C07D25150

    CPC分类号： C07D403/06 ,  C07D251/18 ,  C07D251/48 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12

    摘要： This invention concerns the compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R1 and R2 are each independently selected from hydrogen; hydroxy; amino; optionally substituted C1-6alkyl; C1-6alkyloxy; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; Ar1; mono- or di(C1-6alkyl)amino; mono- or di(C1-6alkyl)-aminocarbonyl; dihydro-2(3H)-furanone; or R1and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-6alkyl)amino-C1-4alkylidene; R3 is hydrogen, Ar1, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, C1-6alkyl substituted with C1-6alkyloxycarbonyl; and R4, R5, R6, R7 and R8 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl or trihalomethyloxy; L is optionally substituted C1-10alkyl; C3-10alkenyl; C3-10alkynyl; C3-7cycloalkyl; Ar1is optionally substituted phenyl; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection. It further relates to new compounds being a subgroup of the compounds of formula (I), their preparation and compositions comprising them.

    摘要翻译： 本发明涉及配制药学上可接受的酸加成盐及其立体化学异构形式的化合物，其中R 1和R 2各自独立地选自氢; 羟基; 氨基; 任选取代的C 1-6烷基; C 1-6烷氧基; C 1-6烷基羰基; C 1-6烷氧基羰基; Ar1; 单或二（C 1-6烷基）氨基; 单或二（C 1-6烷基） - 氨基羰基; 二氢-2（3H） - 呋喃酮; 或R 1和R 2一起可以形成吡咯烷基，哌啶基，吗啉基，叠氮基或单或二（C 1-6烷基）氨基-C 1-4亚烷基; R3是氢，Ar1，C1-6烷基羰基，C1-6烷基，C1-6烷氧基羰基，被C1-6烷氧基羰基取代的C1-6烷基; 并且R 4，R 5，R 6，R 7和R 8各自独立地选自氢，卤素，C 1-6烷基，C 1-6烷氧基，氰基，氨基羰基，硝基，氨基，三卤甲基或三卤代甲氧基。 L是任选取代的C 1-10烷基; C3-10烯基; C3-10炔基; C 3-7环烷基; 任选取代的苯基; 用于制造用于治疗患有HIV（人类免疫缺陷病毒）感染的受试者的药物。 它还涉及作为式（I）化合物的亚组的新化合物，其制备方法和包含它们的组合物。

    Tripeptidyl peptidase inhibitors
    23.
    发明授权
    Tripeptidyl peptidase inhibitors 有权
    三肽基肽酶抑制剂

    公开(公告)号：US07947713B2

    公开(公告)日：2011-05-24

    申请号：US11928273

    申请日：2007-10-30

    申请人： Henry Joseph Breslin ,  Hans Louis Jos De Winter ,  Michael Joseph Kukla

    发明人： Henry Joseph Breslin ,  Hans Louis Jos De Winter ,  Michael Joseph Kukla

    IPC分类号： A61K31/4025 ,  A61K31/403 ,  A61K31/4196 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/422 ,  C07D403/04 ,  C07D401/04 ,  C07D413/04 ,  C07D417/04

    CPC分类号： C07D401/04 ,  C07D403/04 ,  C07D403/12 ,  C07D413/04 ,  C07D417/04

    摘要： The present invention is concerned with novel compounds of formula (I) which are inhibitors of a membrane tripeptidyl peptidase responsible for the inactivation of endogenous neuropeptides such as cholecystokinis (CCKs). The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds. wherein n is an integer 0 or 1; X represents O; S; or —(CR4R5)m— wherein m is an integer 1 or 2; R4 and R5 are each independently from each other hydrogen or C1-4alkyl; R1 is C1-6alkylcarbonyl optionally substituted with hydroxy; C1-6alkyloxycarbonyl; aminoC1-6alkylcarbonyl wherein the C1-6alkyl group is optionally substituted with C3-6cycloalkyl; mono- and di(C1-4alkyl)aminoC1-6alkylcarbonyl; aminocarbonyl substituted with aryl; C1-6alkylcarbonyloxyC1-6alkylcarbonyl; C1-6alkyloxycarbonylaminoC1-6alkylcarbonyl wherein the amino group is optionally substituted with C1-4alkyl; an amino acid; C1-6alkyl substituted with amino; or arylcarbonyl; R2 is an optionally substituted 5-membered heterocycle, or R2 is optionally substituted benzimidazole; R3 is a bivalent radical —CH2CH2— optionally substituted with halo or phenylmethyl; or R3 is a bivalent radical of formula.

    摘要翻译： 本发明涉及新型的式（I）化合物，其是负责灭活内源性神经肽如缩胆囊肿（CCKs）的膜三肽基肽酶的抑制剂。 本发明还涉及制备这些化合物的方法，包含所述化合物的药物组合物以及用作所述化合物的药物。 其中n为整数0或1; X表示O; S; 或 - （CR 4 R 5）m - ，其中m是整数1或2; R 4和R 5各自独立地为氢或C 1-4烷基; R1是任选被羟基取代的C 1-6烷基羰基; C 1-6烷氧基羰基; 氨基C 1-6烷基羰基，其中C 1-6烷基任选被C 3-6环烷基取代; 单和二（C 1-4烷基）氨基C 1-6烷基羰基; 被芳基取代的氨基羰基; C 1-6烷基羰氧基C 1-6烷基羰基; C 1-6烷氧基羰基氨基C 1-6烷基羰基，其中氨基任选被C 1-4烷基取代; 氨基酸; 被氨基取代的C1-6烷基; 或芳基羰基; R2是任选取代的5元杂环，或R 2是任选取代的苯并咪唑; R3是任选被卤素或苯基甲基取代的二价基团-CH 2 CH 2; 或R 3是式的二价基团。

    TRIPEPTIDYL PEPTIDASE INHIBITORS
    25.
    发明申请
    TRIPEPTIDYL PEPTIDASE INHIBITORS 有权
    TRIPEPTIDYL肽抑制剂

    公开(公告)号：US20110224255A1

    公开(公告)日：2011-09-15

    申请号：US13111010

    申请日：2011-05-19

    申请人： Henry Joseph Breslin ,  Hans Louis Jos De Winter ,  Michael Joseph Kukla

    发明人： Henry Joseph Breslin ,  Hans Louis Jos De Winter ,  Michael Joseph Kukla

    IPC分类号： A61K31/4709 ,  C07D401/04 ,  C07D233/54 ,  C07D271/08 ,  A61K31/4178 ,  A61K31/422 ,  A61P25/00

    CPC分类号： C07D401/04 ,  C07D403/04 ,  C07D403/12 ,  C07D413/04 ,  C07D417/04

    摘要： The present invention is concerned with novel compounds of formula (I) which are inhibitors of a membrane tripeptidyl peptidase responsible for the inactivation of endogenous neuropeptides such as cholecystokinis (CCKs). The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds. wherein n is an integer 0 or 1; X represents O; S; or —(CR4R5)m— wherein m is an integer 1 or 2; R4 and R5 are each independently from each other hydrogen or C1-4alkyl; R1 is C1-6alkylcarbonyl optionally substituted with hydroxy; C1-6alkyloxycarbonyl; aminoC1-6alkylcarbonyl wherein the C1-6alkyl group is optionally substituted with C3-6cycloalkyl; mono- and di(C1-4alkyl)aminoC1-6alkylcarbonyl; aminocarbonyl substituted with aryl; C1-6alkylcarbonyloxyC1-6alkylcarbonyl; C1-6alkyloxycarbonylaminoC1-6alkylcarbonyl wherein the amino group is optionally substituted with C1-4alkyl; an amino acid; C1-6alkyl substituted with amino; or arylcarbonyl; R2 is an optionally substituted 5-membered heterocycle, or R2 is optionally substituted benzimidazole; R3 is a bivalent radical —CH2CH2— optionally substituted with halo or phenylmethyl; or R3 is a bivalent radical of formula

    摘要翻译： 本发明涉及新型的式（I）化合物，其是负责灭活内源性神经肽如缩胆囊肿（CCKs）的膜三肽基肽酶的抑制剂。 本发明还涉及制备这些化合物的方法，包含所述化合物的药物组合物以及用作所述化合物的药物。 其中n为整数0或1; X表示O; S; 或 - （CR 4 R 5）m - ，其中m是整数1或2; R 4和R 5各自独立地为氢或C 1-4烷基; R1是任选被羟基取代的C 1-6烷基羰基; C 1-6烷氧基羰基; 氨基C 1-6烷基羰基，其中C 1-6烷基任选被C 3-6环烷基取代; 单和二（C 1-4烷基）氨基C 1-6烷基羰基; 被芳基取代的氨基羰基; C 1-6烷基羰氧基C 1-6烷基羰基; C 1-6烷氧基羰基氨基C 1-6烷基羰基，其中氨基任选被C 1-4烷基取代; 氨基酸; 被氨基取代的C1-6烷基; 或芳基羰基; R2是任选取代的5元杂环，或R 2是任选取代的苯并咪唑; R3是任选被卤素或苯基甲基取代的二价基团-CH 2 CH 2; 或R 3是式的二价基团

    Tripeptidyl peptidase inhibitors
    27.
    发明授权
    Tripeptidyl peptidase inhibitors 有权

    公开(公告)号：US07125891B2

    公开(公告)日：2006-10-24

    申请号：US10415623

    申请日：2001-10-24

    申请人： Henry Joseph Breslin ,  Hans Louis Jos De Winter ,  Michael Joseph Kukla

    发明人： Henry Joseph Breslin ,  Hans Louis Jos De Winter ,  Michael Joseph Kukla

    IPC分类号： A61K31/4725 ,  C07D217/08 ,  C07D217/22

    CPC分类号： C07D401/04 ,  C07D403/04 ,  C07D403/12 ,  C07D413/04 ,  C07D417/04

    摘要： The present invention is concerned with novel compounds of formula (I) which are inhibitors of a membrane tripeptidyl peptidase responsible for the inactivation of endogenous neuropeptides such as cholecystokinis (CCKs). The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds. wherein n is an integer 0 or 1; X represents O; S; or —(CR4R5)m— wherein m is an integer 1 or 2; R4 and R5 are each independently from each other hydrogen or C1-4alkyl; R1 is C1-6alkylcarbonyl optionally substituted with hydroxy; C1-6alkyloxycarbonyl; aminoC1-6alkylcarbonyl wherein the C1-6alkyl group is optionally substituted with C3-6cycloalkyl; mono- and di(C1-4alkyl)aminoC1-6alkylcarbonyl; aminocarbonyl substituted with aryl; C1-6alkylcarbonyloxyC1-6alkylcarbonyl; C1-6alkyloxycarbonylaminoC1-6alkylcarbonyl wherein the amino group is optionally substituted with C1-4alkyl; an amino acid; C1-6alkyl substituted with amino; or arylcarbonyl; R2 is an optionally substituted 5-membered heterocycle, or R2 is optionally substituted benzimidazole; R3 is a bivalent radical —CH2CH2— optionally substituted with halo or phenylmethyl; or R3 is a bivalent radical of formula