专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO0174768A3 INHIBITORS OF SERINE PROTEASES, PARTICULARLY HEPATITIS C VIRUS NS3 PROTEASE 审中-公开
标题翻译：丝氨酸蛋白酶抑制剂，特异性丙型肝炎病毒NS3蛋白
公开(公告)号：WO0174768A3
公开(公告)日：2002-06-06
申请号：PCT/US0110367
申请日：2001-03-29
申请人： VERTEX PHARMA , PERNI ROBERT , COURT JOHN , MALLEY ETHAN O , BHISETTI GOVINDA RAO
发明人： PERNI ROBERT , COURT JOHN , O'MALLEY ETHAN , BHISETTI GOVINDA RAO
IPC分类号： C12N9/99 , A61K31/13 , A61K31/7052 , A61K38/00 , A61K38/21 , A61K45/00 , A61P31/14 , C07K5/103 , C07K7/06 , C07K5/117 , A61K38/07 , A61L2/16
CPC分类号： C07K7/06 , A61K38/00 , C07K5/101
摘要： The present invention relates to compounds that are useful as protease inhibitors, particularly as serine protease inhibitors, and more particularly as hepatitis C NS3 protease inhibitors. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HCV NS3 protease activity and consequently, may be advantageously used as therapeutic agents against the hepatitis C virus and other viruses that are dependent upon a serine protease for proliferation. This invention also relates to methods for inhibiting the activity of proteases, including hepatitis C virus NS3 protease and other serine proteases, using the compounds of this invention and related compounds.
摘要翻译：本发明涉及可用作蛋白酶抑制剂的化合物，特别是作为丝氨酸蛋白酶抑制剂，特别是作为丙型肝炎NS3蛋白酶抑制剂。因此，它们通过干扰丙型肝炎病毒的生命周期起作用，也可用作抗病毒剂。本发明还涉及包含这些化合物的药物组合物。本发明的化合物和药物组合物特别适用于抑制HCV NS3蛋白酶活性，因此可有利地用作针对依赖于丝氨酸蛋白酶增殖的丙型肝炎病毒和其它病毒的治疗剂。本发明还涉及使用本发明化合物和相关化合物来抑制蛋白酶（包括丙型肝炎病毒NS3蛋白酶和其它丝氨酸蛋白酶）的活性的方法。

2. 发明申请

WO2008106151A3 CO-CRYSTALS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME 审中-公开
标题翻译：包括其的CO晶体和药物组合物
公开(公告)号：WO2008106151A3
公开(公告)日：2008-11-06
申请号：PCT/US2008002568
申请日：2008-02-27
申请人： VERTEX PHARMA , CONNELLY PATRICK R , KADIYALA IRINA , STAVROPOLUS KATHY , ZHANG YUEGANG , JOHNSTON STEVE , BHISETTI GOVINDA RAO , JURKAUSKAS VALDAS , ROSE PETER
发明人： CONNELLY PATRICK R , KADIYALA IRINA , STAVROPOLUS KATHY , ZHANG YUEGANG , JOHNSTON STEVE , BHISETTI GOVINDA RAO , JURKAUSKAS VALDAS , ROSE PETER
IPC分类号： C07D403/12 , A61K31/497 , A61K38/07 , C07K5/10
CPC分类号： C07K5/0812 , C07D403/12
摘要： The invention relates to compositions and co-crystals each comprising VX-950 and a co-crystal former selected from the group consisting of 4-hydroxybenzoic acid, 4-amino salicylic acid, phenylalanine, threonline, tartaric acid, adipic acid, succinic acetate, proline, methyl 4-hydroxybenzoate, anthranilic acid, and d-Biotin. Also within the scope of this invention are methods of making and using the same.
摘要翻译：本发明涉及各自包含VX-950和选自4-羟基苯甲酸，4-氨基水杨酸，苯丙氨酸，苏氨酸，酒石酸，己二酸，琥珀酸乙酯，脯氨酸，4-羟基苯甲酸甲酯，邻氨基苯甲酸和d-生物素。在本发明的范围内也是制造和使用本发明的方法。

3. 发明申请

WO2011009084A2 BENZIMIDAZOLE ANALOGUES FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS 审中-公开
标题翻译：苯并咪唑类似物用于治疗或预防黄病毒感染
公开(公告)号：WO2011009084A2
公开(公告)日：2011-01-20
申请号：PCT/US2010042340
申请日：2010-07-16
申请人： VERTEX PHARMA , HENDERSON JAMES A , MAXWELL JOHN , VAILLANCOURT LOUIS , MORRIS MARK , GREY JR RONALD , GIROUX SIMON , KONG LAVAL CHAN CHUN , DAS SANJOY KUMAR , LIU BINGCAN , POISSON CARL , CADILHAC CAROLINE , BUBENIK MONICA , REDDY T JAGADEESWAR , FALARDEAU GUY , YANNOPOULOS CONSTANTIN , WANG JIAN , PEREIRA OSWY Z , BENNANI YOUSSEF L , PIERCE ALBERT C , BHISETTI GOVINDA RAO , COTTRELL KEVIN M , MARONE VALERIE
发明人： HENDERSON JAMES A , MAXWELL JOHN , VAILLANCOURT LOUIS , MORRIS MARK , GREY JR RONALD , GIROUX SIMON , KONG LAVAL CHAN CHUN , DAS SANJOY KUMAR , LIU BINGCAN , POISSON CARL , CADILHAC CAROLINE , BUBENIK MONICA , REDDY T JAGADEESWAR , FALARDEAU GUY , YANNOPOULOS CONSTANTIN , WANG JIAN , PEREIRA OSWY Z , BENNANI YOUSSEF L , PIERCE ALBERT C , BHISETTI GOVINDA RAO , COTTRELL KEVIN M , MARONE VALERIE
IPC分类号： C07D403/14 , A61K31/506
CPC分类号： C07K5/06052 , C07D401/14 , C07D403/14 , C07D405/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D495/04
摘要： Compounds represented by formula (I) or pharmaceutically acceptable salts and solvates thereof, wherein A, B, B', X, Y, R1, R1 ', R2, R2', R3, R3', R5, R5', R6, m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.
摘要翻译：其中A，B，B'，X，Y，R1，R1'，R2，R2'，R3，R3'，R5，R5'，R6，m ，n或p如本文所定义，可用于治疗黄病毒科病毒感染。

4. 发明专利

ES2351970T3 SULFONAMIDAS INHIBIDORES DE ASPARTIL PROTEASA QUE CONTIENEN HETEROCICLOS OXIGENADOS. 未知
公开(公告)号：ES2351970T3
公开(公告)日：2011-02-14
申请号：ES05028389
申请日：1996-04-18
申请人： VERTEX PHARMA
发明人： BHISETTI GOVINDA RAO , TUNG ROGER D
IPC分类号： C07D319/06 , A61K31/335 , A61K31/34 , A61K31/341 , A61K31/35 , A61K31/357 , A61P31/12 , A61P43/00 , C07D307/20 , C07D309/12 , C07D317/24 , C07D493/04
摘要： Un compuesto de formula I: **Fórmula** en la que: cada R1 se elige independientemente entre el grupo que consiste en -C(O)-, -S(O)2-, - C(O)-C(O)-, -O-C(O)-, -O-S(O)2, -NR2-S(O)2-, -NR2-C(O)- y -NR2-C(O)-C(O)-; cada A es tetrahidropiranil; cada Het se elige independientemente entre el grupo que consiste en carbociclo C3-C7; arilo C6-C10; fenilo fusionado con heterociclo; y heterociclo; en el que cualquier miembro de dicho Het puede estar opcionalmente sustituido con uno o mas sustituyentes elegidos entre el grupo que consiste en oxo, -OR2, -R2, -N(R2)(R2), - NHOH, -R2-OH, -CN, -CO2R2, -C(O)-N(R2)(R2), -S(O)2-N(R2)(R2), -N(R2)-C(O)-R2, - C(O)-R2, -S(O)n-R2, -OCF3, -S(O)n-R6, -N(R2)-S(O)2-(R2), halo, -CF3, -NO2, -R6 y -O-R6; cada R2 se elige independientemente entre el grupo que consiste en H y alquilo C1-C3 opcionalmente sustituido con R6; cada R3 se elige independientemente entre el grupo que consiste en H, Het, alquilo C1-C6 y alquenilo C2-C6 en el que cualquier miembro de dicho R3 , excepto H, puede estar opcionalmente sustituido con uno o mas sustituyentes elegidos entre el grupo que consiste en -OR2, -C(O)-NH-R2, -S(O)n-N(R2)(R2), Het, -CN, -SR2, -CO2R2, - N(R2)-C(O)-R2; cada n es independientemente 1 o 2; cada D y D'' se eligen independientemente entre el grupo que consiste R6; alquilo C1-C5 , que puede estar opcionalmente sustituido con uno o mas grupos elegidos entre el grupo que consiste en -OR2, -R3, -S-R6 -O-R6 y R6; alquenilo C2-C4, que puede estar opcionalmente sustituido con uno o mas grupos elegidos entre el grupo que consiste en -OR2, -R3, -O-R6 y R6, y carbociclo C3-C6, que puede estar opcionalmente sustituido o fusionado con R6; cada E se elige independientemente entre el grupo que consiste en Het; -OHet; Het-Het; -O-R3; -NR2R3; alquilo C1-C6, que puede estar opcionalmente sustituido con uno o mas grupos elegidos entre el grupo que consiste en R4 y Het; alquenilo C2- C6, que puede estar opcionalmente sustituido con uno o mas grupos elegidos entre el grupo que consiste en R4 y Het; y fenilo fusionado con un heterociclo o carbociclo de 5-7 miembros; cada R4 se elige independientemente entre el grupo que consiste en -OR2, - C(O)-NHR2, -S(O)2-NHR2, halo, -NHR2- C(O)- R2, y -CN; cada R5 se elige independientemente entre el grupo que consiste en H y alquilo C1-C4 opcionalmente sustituido con arilo; y cada R6 se elige independientemente entre el grupo que consiste en arilo, carbociclo y heterociclo , en el que dicho arilo, carbociclo o heterociclo puede estar opcionalmente sustituido con uno o mas grupos elegidos entre el grupo que consiste en oxo, -OR5, -R5, -N(R5)(R5), -N(R5)-C(O)-R5, -R5-OH, -CN, -CO2R5, -C(O)-N(R5)(R5), halo, y -CF3, donde "arilo" se refiere a un radical aromatico carbociclico que contiene el numero de atomos de carbono especificado; "carbociclo" se refiere a un radical de anillo de carbono estable no aromatico de 3 a 8 miembros tal como se ha designado, mono-insaturado o poli-insaturado; y "heterociclo" se refiere a un anillo heterociclico monociclico estable de 3-7 miembros, tal como se ha designado, o un anillo heterociclico biciclico de 8-11 miembros que esta o bien saturado o insaturado, opcionalmente benzofusionado si es monociclico, y consiste en uno o mas atomos de carbono y de uno a cuatro heteroatomos elegidos entre el grupo que consiste en nitrogeno, oxigeno y azufre.

5. 发明专利

DE60329326D1 未知
公开(公告)号：DE60329326D1
公开(公告)日：2009-10-29
申请号：DE60329326
申请日：2003-12-19
申请人： VERTEX PHARMA
发明人： BANDARAGE UPUL , COME JON H , PEROLA EMANUELE , BHISETTI GOVINDA RAO , SAUNDERS JEFFREY O , WANG TIANSHENG
IPC分类号： C07D207/12 , A61K31/40 , A61P35/00 , C07C323/65 , C07D205/04 , C07D261/04 , C07D401/12 , C07D403/12 , C07D413/12
摘要： The present invention relates to compounds that inhibit TACE, compositions thereof, and methods of using those compounds and compositions for treating diseases.

6. 发明专利

MX2009009182A CO-CRISTALES Y COMPOSICIONES FARMACEUTICAS QUE LOS COMPRENDEN. 未知
公开(公告)号：MX2009009182A
公开(公告)日：2009-09-04
申请号：MX2009009182
申请日：2008-02-27
申请人： VERTEX PHARMA
发明人： CONNELLY PATRICK R , KADIYALA IRINA , STAVROPOLUS KATHY , ZHANG YUEGANG , JOHNSTON STEVE , BHISETTI GOVINDA RAO , JURKAUSKAS VALDAS , ROSE PETER
IPC分类号： A61K31/497 , C07D403/12 , A61K38/07 , C07K5/10
摘要： La invención se refiere a composiciones y co-cristales cada uno comprendiendo VX-950 y formador de co-cristal seleccionado del grupo que consiste de ácido 4-hidroxibenzoico, ácido 4-aminosalicílico, feriilalanina, treonlina, ácido tartárico, ácido adípico, acetato succínico, prolina, 4-hidroxobenzoato de metilo, ácido antranílico y d-Biotina. También dentro del alcance de esta invención están los métodos para hacer y utilizar los mismos.

7. 发明专利

AT314360T 未知
公开(公告)号：AT314360T
公开(公告)日：2006-01-15
申请号：AT01113575
申请日：1996-04-18
申请人： VERTEX PHARMA
发明人： TUNG ROGER D , BHISETTI GOVINDA RAO
IPC分类号： A61K31/335 , A61K31/34 , A61K31/341 , A61K31/357 , A61P31/12 , A61P43/00 , C07D307/20 , C07D309/12 , C07D317/24 , C07D319/06 , C07D493/04 , A61K31/35
摘要： The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention.

8. 发明专利

AT297946T 未知
公开(公告)号：AT297946T
公开(公告)日：2005-07-15
申请号：AT01924516
申请日：2001-03-29
申请人： VERTEX PHARMA
发明人： PERNI ROBERT , COURT JOHN , O'MALLEY ETHAN , BHISETTI GOVINDA RAO
IPC分类号： C12N9/99 , A61K31/13 , A61K31/7052 , A61K38/00 , A61K38/21 , A61K45/00 , A61P31/14 , C07K5/103 , C07K7/06 , C07K5/117 , A61K38/07 , A61L2/16
摘要： The present invention relates to compounds that are useful as protease inhibitors, particularly as serine protease inhibitors, and more particularly as hepatitis C NS3 protease inhibitors. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HCV NS3 protease activity and consequently, may be advantageously used as therapeutic agents against the hepatitis C virus and other viruses that are dependent upon a serine protease for proliferation. This invention also relates to methods for inhibiting the activity of proteases, including hepatitis C virus NS3 protease and other serine proteases, using the compounds of this invention and related compounds.

9. 发明专利

DE69333012D1 未知
公开(公告)号：DE69333012D1
公开(公告)日：2003-07-03
申请号：DE69333012
申请日：1993-09-07
申请人： VERTEX PHARMA
发明人： TUNG ROGER D , MURCKO MARK A , BHISETTI GOVINDA RAO
IPC分类号： G01N33/53 , A61K31/16 , A61K31/165 , A61K31/17 , A61K31/18 , A61K31/255 , A61K31/27 , A61K31/325 , A61K31/34 , A61K31/341 , A61K31/343 , A61K31/35 , A61K31/40 , A61K31/4015 , A61K31/403 , A61K31/404 , A61K31/41 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/4245 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4418 , A61K31/4433 , A61K31/445 , A61K31/47 , A61K31/495 , A61K31/496 , A61K31/505 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61K31/63 , A61K38/00 , A61K38/55 , A61P31/12 , A61P31/18 , C07C307/02 , C07C307/06 , C07C311/13 , C07C311/18 , C07C311/29 , C07C311/39 , C07C311/41 , C07C311/46 , C07D207/12 , C07D207/26 , C07D207/27 , C07D207/28 , C07D209/08 , C07D209/10 , C07D213/30 , C07D215/48 , C07D231/14 , C07D239/22 , C07D239/54 , C07D263/24 , C07D271/08 , C07D277/20 , C07D277/36 , C07D295/12 , C07D305/12 , C07D307/12 , C07D307/14 , C07D307/20 , C07D307/52 , C07D307/64 , C07D307/79 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D419/14 , C07G99/00 , C07K5/078 , G01N33/569
摘要： The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors, of formula (I). In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as antiviral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.

10. 发明专利

ES2169880T3 未知
公开(公告)号：ES2169880T3
公开(公告)日：2002-07-16
申请号：ES97946273
申请日：1997-10-17
申请人： VERTEX PHARMA
发明人： TUNG ROGER D , HARBESON SCOTT L , DEININGER DAVID D , MURCKO MARK A , BHISETTI GOVINDA RAO , FARMER LUC J
IPC分类号： A61K38/00 , A61K38/08 , C07K5/02 , C07K5/10 , C07K5/117 , C07K7/02 , C07K7/06 , A61K38/55
摘要： The present invention relates to compounds, methods and pharmaceutical compositions for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases. The compounds, and the compositions and methods that utilize them, can be used, either alone or in combination to inhibit viruses, particularly HCV virus.

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