专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

11. 发明专利

MX2009000160A INHIBIDORES DE PROTEASA DE VIRUS DE INMUNODEFICIENCIA HUMANA DE 2-(AMINO-SUSTITUIDO)-BENZOTIAZOL SULFONAMIDA. 未知
公开(公告)号：MX2009000160A
公开(公告)日：2009-01-23
申请号：MX2009000160
申请日：2007-06-22
申请人： TIBOTEC PHARM LTD
发明人： DIERYNCK INGE , JONCKERS TIM HUGO MARIA , LAST STEFAAN JULIEN , BOONANTS PAUL JOZEF GABRIEL MARIA , DE KOCK HERMAN , BAUMEISTER JUDITH EVA , T KLOOSTER GERBEN ALBERT ELEUTHERIUS VAN
IPC分类号： C07D493/04 , A61K31/34 , A61P31/18
摘要： La presente invención se relaciona con compuestos de 2-(amino-sustituido)-benzotiazol sulfonamida y derivados; con su uso como inhibidores de proteasa, en particular, como inhibidores de proteasa de HIV de amplio espectro; con procesos para su preparación; y con composiciones farmacéuticas y equipos de diagnóstico que los comprenden. La presente invención además se relaciona con combinaciones de los presentes compuestos de 2-(amino-sustituido)-benzotiazol sulfonamida y derivados, con otro agente antirretroviral. Se relaciona asimismo con su uso en ensayos, como compuestos de referencia o como reactivos.

12. 发明专利

BG108309A BROADSPECTRUM 2-AMINO-BENZOXAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS 未知
公开(公告)号：BG108309A
公开(公告)日：2004-12-30
申请号：BG10830903
申请日：2003-11-03
申请人： TIBOTEC PHARM LTD
发明人： SURLERAUX DOMINIQUE , VENDEVILLE SANDRINE , VERSCHUEREN WIM , DE BETHUNE MARIE-PIERRE , DE KOCK HERMAN , TAHRI ABDELLAH
IPC分类号： A61K31/423 , A61K31/424 , A61K31/427 , A61K31/429 , A61K31/4439 , A61K31/5383 , A61P31/14 , A61P31/18 , A61P43/00 , C07D263/58 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D491/04 , C07D493/04 , C07D498/04 , C07D513/04
摘要： The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7cycloalkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9-; t is 0, 1 or 2; R2 is H or C1 6alkyl; L is -C(=O)-, -O-C(=O)-, -NR8-C(=O)-, -O-C1-6alkanedyl-C(=O)-NR8-C1-6alkanediyl-C(=O)-, -S(=O)2-, -O-S(=O)2-, -NR8--S(=O)2; R3 is C1-6alkyl, aryl, C3-7cycxloalkyl, C3-7cyclkoalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC(=O), carboxyl, aminoC(=O), mono- or di(C1-4alkyl)aminoC(=O), C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; R5 and R6 are H or C1-6alkyl. It further relates to their use as broad spectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with another anti-retroviral agent, and to their use in assays as reference compounds or as reagents.

13. 发明专利

BG66371B1 BROADSPECTRUM 2-(SUBSTITUTED-AMINO)-BENZOXAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS 未知
公开(公告)号：BG66371B1
公开(公告)日：2013-10-31
申请号：BG10821803
申请日：2003-10-01
申请人： TIBOTEC PHARM LTD
发明人： SURLERAUX DOMINIQUE , VENDEVILLE SANDRINE , VERSCHUEREN WIM , DE BETHUNE MARIE-PIERRE , DE KOCK HERMAN , TAHRI ABDELLAH , ERRA SOLA MONSTERRAT
IPC分类号： C07D263/58 , A61K31/423 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/496 , A61P31/18 , A61P35/00 , A61P43/00 , C07D413/04 , C07D417/12 , C07D417/14 , C07D493/04
摘要： The invention relates to compounds with the formula wherein the substitutes R1, R2, R3, R4, R5, R6, H, L, A are given in the description, to their N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters or metabolites. The invention also relates to their use as broadspectrum HIV protease inhibitors, processes for their preparation and to pharmaceutical compositions and diagnostic kits comprising them, to their combinations thereof with another anti-retroviral agent and to their use in assays as reference compounds or as reagents.

14. 发明专利

BG66301B1 BROADSPECTRUM 2-(SUBSTITUTED-AMINO)-BENZOTHIAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS 未知
公开(公告)号：BG66301B1
公开(公告)日：2013-03-29
申请号：BG10814303
申请日：2003-09-01
申请人： TIBOTEC PHARM LTD
发明人： SURLERAUX DOMINIQUE , WIGERINCK PIET , GETMAN DANIEL , VERSCHUEREN WIM , VENDEVILLE SANDRINE , DE BETHUNE MARIE-PIERRE , DE KERPEL JAN , MOORS SAMUEL , DE KOCK HERMAN , VOETS MARIEKE
IPC分类号： C07D277/82 , A61K31/428 , A61K31/4439 , A61K31/496 , A61K31/5377 , A61P31/14 , A61P31/18 , A61P43/00 , C07D417/12 , C07D493/04
摘要： The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6 alkyl, C2-6 alkenyl, C3-7 cycloalkyl, aryl, Het1, Het2 R1 may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9-;@T is 0, 1 or 2 R2 is H or C1-6 alkyl L is -C(=O)-, -O-C(=O)-, -NR8-C(=O)-, O-C1-6 alkanediyl-C(=O)-, -NR8-C1-6 alkanediyl-C(=O)-, -S(=O)2-, -O-S(=0)2-NR8-S(=O)2 R3 is C1-6 alkyl, aryl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-4 alkyl, or arylC 1-4 alkyl R4 isH, C1-4 alkyl OC(=O), carboxyl, amino C(=O), mono or di(C1-4 alkyl) amino C(=O), C3-7 cycloalkyl, C2-6 alkenyl, C2-6 alkynyl or optionally substituted C1-6 alkyl A is C1-6 alkanediyl, -C(=O)-, -C(=S)-, (S=0)2-C1-6 alkanediyl-C(=O)-, C1-6 alkanediyl-C(=S)- or C1-6 alkanediyl-S(=O)2- R5 is H, OH, C1-6 alkyl, Het1C1-6alkyl, Het2C1-6alkyl, optionally substituted amino C1-6 alkyl R6 is C1-6 alkylO, Het1, Het1O, Het2, Het2O, aryl, arylO, C1-6 alkyloxycarbonylamino or amino and in case -A- is other than C1-6 alkanediyl then R6 may also be C1-6 alkyl, Het1C1-4 alkyl, Het1OC 1-4 alkyl, Het2 C1-4alkyl, Het2OC 1-4 alkyl, arylC 1-4 alkyl, arylOC 1-4 alkyl or aminoC 1-4 alkyl whereby each of the amino groups in the definition of R6 may be optionally be substituted R5 and -A-R6 taken together with the nitrogen atom to which they attached may also form Het1 or Het2. It further relates to their use as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with another anti-retroviral agent, and to their use in assays as reference compounds or as reagents. 51 claims@

15. 发明专利

AT429431T 未知
公开(公告)号：AT429431T
公开(公告)日：2009-05-15
申请号：AT02735354
申请日：2002-05-10
申请人： TIBOTEC PHARM LTD
发明人： SURLERAUX DOMINIQUE , VENDEVILLE SANDRINE , VERSCHUEREN WIM , DE BETHUNE MARIE-PIERRE , DE KOCK HERMAN , TAHRI ABDELLAH
IPC分类号： C07D413/12 , A61K31/423 , A61K31/424 , A61K31/427 , A61K31/429 , A61K31/4439 , A61K31/5383 , A61P31/14 , A61P31/18 , A61P43/00 , C07D263/58 , C07D413/14 , C07D417/12 , C07D417/14 , C07D491/04 , C07D493/04 , C07D498/04 , C07D513/04
摘要： The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7cycloalkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9—; t is 0, 1 or 2; R2 is H or C1-6alkyl; L is —C(═O)—, —O—C(═O)—, —NR8—C(═O)—, —O—C1-6alkanediyl-C(═O)—, —NR8—C1-6alkanediyl-C(═O)—, —S(═O)2—, —O—S(═O)2—, —NR8—S(═O)2; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC(═O), carboxyl, aminoC(═O), mono- or di(C1-4alkyl)aminoC(═O), C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; R5 and R6 are H or C1-6alkyl. It further relates to their use as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with another anti-retroviral agent, and to their use in assays as reference compounds or as reagents.

16. 发明专利

CA2651659A1 LYSINE RELATED DERIVATIVES AS HIV ASPARTYL PROTEASE INHIBITORS 未知
公开(公告)号：CA2651659A1
公开(公告)日：2007-12-06
申请号：CA2651659
申请日：2007-05-30
申请人： TIBOTEC PHARM LTD
发明人： DE KOCK HERMAN , LAST STEFAAN JULIEN , JONCKERS TIM HUGO MARIA , DIERYNCK INGE
IPC分类号： C07C311/37 , A61K31/18 , A61K31/197 , C07C311/40
摘要： The present invention concerns lysine related derivatives, their use as p rotease inhibitors, in particular as HIV aspartyl protease inhibitors, proce sses for their preparation as well as pharmaceutical compositions and diagno stic kits comprising them. The present invention also concerns combinations of the present lysine related derivatives with another anti-retroviral agent . It further relates to their use in assays as reference compounds or as rea gents.

17. 发明专利

CA2653233C 2-(SUBSTITUTED-AMINO)-BENZOTHIAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS 未知
公开(公告)号：CA2653233C
公开(公告)日：2015-09-29
申请号：CA2653233
申请日：2007-06-22
申请人： TIBOTEC PHARM LTD
发明人： DE KOCK HERMAN , JONCKERS TIM HUGO MARIA , BOONANTS PAUL JOZEF GABRIEL MARIA , LAST STEFAAN JULIEN , DIERYNCK INGE , BAUMEISTER JUDITH EVA , VAN T KLOOSTER GERBEN ALBERT ELEUTHERIUS
IPC分类号： C07D493/04 , A61K31/454 , A61P31/18
摘要： The present invention relates to 2-(substituted-amino)-benzothiazole sulfonamide compounds and derivatives, their use as protease inhibitors, in particular as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. The present invention also concerns combinations of the present 2-(substituted-amino)-benzothiazole sulfonamide compounds and derivatives with another anti-retroviral agent. It further relates to their use in assays as reference compounds or as reagents.

18. 发明专利

AT544769T 未知
公开(公告)号：AT544769T
公开(公告)日：2012-02-15
申请号：AT07765554
申请日：2007-06-22
申请人： TIBOTEC PHARM LTD
发明人： DE KOCK HERMAN , JONCKERS TIM HUGO MARIA , BOONANTS PAUL JOZEF GABRIEL MARIA , LAST STEFAAN JULIEN , DIERYNCK INGE , BAUMEISTER JUDITH EVA , VAN T KLOOSTER GERBEN ALBERT ELEUTHE
IPC分类号： C07D493/04 , A61K31/34 , A61P31/18
摘要： The present invention relates to 2-(substituted-amino)-benzothiazole sulfonamide compounds and derivatives, their use as protease inhibitors, in particular as broad-spectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. The present invention also concerns combinations of the present 2-(substituted-amino)-benzothiazole sulfonamide compounds and derivatives with another anti-retroviral agent. It further relates to their use in assays as reference compounds or as reagents.

19. 发明专利

ES2369284T3 INHIBIDORES MACROCICLICOS DEL VIRUS DE LA HEPATITIS C. 未知
公开(公告)号：ES2369284T3
公开(公告)日：2011-11-29
申请号：ES06764264
申请日：2006-07-28
申请人： TIBOTEC PHARM LTD
发明人： RABOISSON PIERRE , DE KOCK HERMAN , VENDEVILLE SANDRINE , HU LILI , VAN DE VREKEN WIM , MC GOWAN DAVID , TAHRI ABDELLAH , SURLERAUX DOMINIQUE , SIMMEN KENNETH
IPC分类号： C07D487/04 , A61K38/05 , A61P31/14 , C07K5/06 , C07K5/078
摘要： Un compuesto que tiene la fórmula un N-óxido, sal de adición, amina cuaternaria, complejo metálico, y forma estereoquímicamente isómera del mismo, en donde la línea de trazos representa un enlace doble opcional entre los átomos C7 y C8; R1 es arilo o un sistema de anillos heterocíclico saturado, parcialmente insaturado o completamente insaturado monocíclico de 5 ó 6 miembros, o bicíclico de 9 a 12 miembros en donde dicho sistema de anillos contiene un átomo de nitrógeno, y opcionalmente 1 a 3 heteroátomos adicionales seleccionados del grupo constituido por oxígeno, azufre y nitrógeno, y en donde los miembros restantes del anillo son átomos de carbono; en donde dicho sistema de anillos puede estar sustituido opcionalmente en cualquier átomo de carbono o nitrógeno del anillo con uno, dos, tres, o cuatro sustituyentes seleccionados cada uno de modo independiente de C3-7cicloalquilo, arilo, Het, -C(=O)NR5aR5b, -C(=O)R7, -C(=O)OR6a, y C1-6alquilo sustituido opcionalmente con C3-7cicloalquilo, arilo, Het, -C(=O)NR5aR5b, -NR5aR5b, -C(=O)R7, -NR5aC(=O)R7, -NR5aSOpR8, -SOpR8, - SOpNR5aR5b, -C(=O)OR6, o -NR5aC(=O)OR6a; y en donde los sustituyentes en cualquier átomo de carbono del anillo heterocíclico pueden seleccionarse también de -OR8, -SR8, halo, polihalo-C1-6alquilo, oxo, tio, ciano,, nitro, azido, -NR5aR5b, -NR5aC(=O)R7, -NR5aSOpR8, -SOpR8, -SOpNR5aR5b, -C(=O)OH, y -NR5aC(=O)OR6a; L es un enlace directo, -O-, -O-C1-4alcanodiílo-, -O-CO-, -O-C(=O)-NR5a- u -O-C(=O)-NR5a-C1-4alcanodiílo-; R2 representa hidrógeno, -OR6, -C(=O)OR6, -C(=O)R7, -C(=O)NR5aR5b, -C(=O)NHR5c, - NR5aR5b, -NHR5c, - NHSOpNR5aR5b, -NR5aSOpR8, o -B(OR6)2; R3 y R4 son hidrógeno o C1-6alquilo; o R3 y R4 considerados juntos, pueden formar un anillo C3-7cicloalquilo; n es 3, 4, 5, ó 6; p es 1 ó 2; cada uno de R5a y R5b son, de modo independiente, hidrógeno, C3-7cicloalquilo, arilo, Het, C1-6alquilo sustituido op25 cionalmente con halo, C1-6alcoxi, ciano, polihaloC1-6alcoxi, C3-7cicloalquilo, arilo, o con Het; o R5a y R5b considerados junto con el átomo de nitrógeno al cual están unidos forman pirrolidinilo, piperidinilo, piperazinilo, 4- C1-6alquilpiperazinilo, 4-C1-6alquilcarbonil-piperazinilo, y morfolinilo; en donde los grupos morfolinilo y piperidinilo pueden estar sustituidos opcionalmente con uno o con dos radicales C1-6alquilo; R5c es C3-7cicloalquilo, arilo, Het, -O-C3-7cicloalquilo, -O-arilo, -O-Het, C1-6alquilo, o C1-6alcoxi, en donde dicho C1-6alquilo o C1-6alcoxi puede estar sustituido cada uno opcionalmente con -C(=O)OR6, C3-7cicloalquilo, arilo o Het; R6 es hidrógeno; C2-6alquenilo; Het; C3-7cicloalquilo sustituido opcionalmente con C1-6alquilo; o C1-6alquilo sustituido opcionalmente con C3-7cicloalquilo, arilo o Het; R6a es C2-6alquenilo, C3-7cicloalquilo, Het, o C1-6alquilo sustituido opcionalmente con C3-7cicloalquilo, arilo o Het; R7 es hidrógeno, C1-6alquilo, C3-7cicloalquilo, o arilo; R8 es hidrógeno, polihaloC1-6alquilo, arilo, Het, C3-7cicloalquilo sustituido opcionalmente con C1-6alquilo, o C1-6alquilo sustituido opcionalmente con C3-7cicloalquilo, arilo o Het; arilo como grupo o parte de un grupo es fenilo, naftilo, indanilo, o 1,2,3,4-tetrahidronaftilo, cada uno de los cuales puede estar sustituido opcionalmente con uno, dos o tres sustituyentes seleccionados de halo, C1-6alquilo, polihaloC1- 6alquilo, hidroxi, C1-6alcoxi, polihaloC1-6alcoxi, C1-6alcoxiC1-6alquilo, carboxilo, C1-6alquilcarbonilo , C1-6alcoxicarbonilo, ciano, nitro, amino, mono- o diC1-6alquilamino, aminocarbonilo, mono- o di- C1-6alquilaminocarbonilo, azido, mercapto, C3-7cicloalquilo, fenilo, piridilo, tiazolilo, pirazolilo, pirrolidinilo, piperidinilo, piperazinilo, 4-C1-6alquilpiperazinilo, 4-C1-6alquilcarbonil-piperazinilo, y morfolinilo; en donde los grupos morfolinilo y piperidinilo pueden estar sustituidos opcionalmente con uno o con dos radicales C1-6alquilo; y los grupos fenilo, piridinilo, tiazolilo, pirazolilo pueden estar sustituidos opcionalmente con uno, dos o tres sustituyentes seleccionados cada uno de modo independiente de C1-6alquilo, C1-6alcoxi, halo, amino, mono- o diC1-6alquilamino; Het como grupo o parte de un grupo es un anillo heterocíclico saturado, parcialmente insaturado o completamente insaturado de 5 ó 6 miembros que contiene 1 a 4 heteroátomos seleccionados cada uno de modo indepen15 diente de nitrógeno, oxígeno y azufre, estando dicho anillo heterocíclico condensado opcionalmente con un anillo de benceno, y en donde el grupo Het como un todo puede estar sustituido opcionalmente con 1, 2 ó 3 sustituyentes seleccionados cada uno de modo independiente del grupo constituido por halo, C1-6alquilo, polihaloC1- 6alquilo, hidroxi, C1-6alcoxi, polihaloC1-6alcoxi, C1-6alcoxiC1-6alquilo, carboxilo, C1-6alquilcarbonilo, C1-6alcoxicarbonilo, ciano, nitro, amino, mono- o diC1-6alquilamino, aminocarbonilo, mono- o di- C1-6alquilaminocarbonilo, C3-7cicloalquilo, fenilo, piridilo, tiazolilo, pirazolilo, pirrolidinilo, piperidinilo, piperazinilo, 4-C1-6alquilpiperazinilo, 4-C1-6alquilcarbonil-piperazinilo, y morfolinilo; en donde los grupos morfolinilo y piperidinilo pueden estar sustituidos opcionalmente con uno o con dos radicales C1-6alquilo; y los grupos fenilo, piridilo, tiazolilo, pirazolilo pueden estar sustituidos opcionalmente con 1, 2 ó 3 sustituyentes seleccionados cada uno de modo independiente de C1-6alquilo, C1-6alcoxi, halo, amino, mono- o diC1-6alquilamino.

20. 发明专利

CA2653233A1 2-(SUBSTITUTED-AMINO)-BENZOTHIAZOLE SULFONAMIDE HIV PROTEASEINHIBITORS 未知
公开(公告)号：CA2653233A1
公开(公告)日：2007-12-27
申请号：CA2653233
申请日：2007-06-22
申请人： TIBOTEC PHARM LTD
发明人： BOONANTS PAUL JOZEF GABRIEL MARIA , LAST STEFAAN JULIEN , BAUMEISTER JUDITH EVA , DIERYNCK INGE , DE KOCK HERMAN , JONCKERS TIM HUGO MARIA , VAN 'T KLOOSTER GERBEN ALBERT ELEUTHERIUS
IPC分类号： C07D493/04 , A61K31/34 , A61P31/18
摘要： The present invention relates to 2-(substituted-amino)-benzothiazole sulf onamide compounds and derivatives, their use as protease inhibitors, in part icular as broadspectrum HIV protease inhibitors, processes for their prepara tion as well as pharmaceutical compositions and diagnostic kits comprising t hem. The present invention also concerns combinations of the present 2-(subs tituted-amino)-benzothiazole sulfonamide compounds and derivatives with anot her anti-retroviral agent. It further relates to their use in assays as refe rence compounds or as reagents.

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式