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2. 发明申请

WO03010140A3 HEPATITIS C VIRUS POLYMERASE INHIBITORS WITH HETEROBICYCLIC STRUCTURE 审中-公开
标题翻译：具有异构结构的丙型肝炎病毒聚合酶抑制剂
公开(公告)号：WO03010140A3
公开(公告)日：2003-07-10
申请号：PCT/CA0201127
申请日：2002-07-18
申请人： BOEHRINGER INGELHEIM CA LTD , BEAULIEU PIERRE LOUIS , FAZAL GULREZ , KUKOLJ GEORGE , JOLICOEUR ERIC , GILLARD JAMES , POUPART MARC-ANDRE , RANCOURT JEAN
发明人： BEAULIEU PIERRE LOUIS , FAZAL GULREZ , KUKOLJ GEORGE , JOLICOEUR ERIC , GILLARD JAMES , POUPART MARC-ANDRE , RANCOURT JEAN
IPC分类号： A61K31/13 , A61K31/381 , A61K31/404 , A61K31/405 , A61K31/4184 , A61K31/422 , A61K31/427 , A61K31/428 , A61K31/437 , A61K31/443 , A61K31/4436 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/497 , A61K31/506 , A61K31/53 , A61K31/5377 , A61K31/7052 , A61K38/21 , A61K45/00 , A61P31/12 , A61P31/14 , A61P37/02 , A61P43/00 , C07D20060101 , C07D209/08 , C07D209/14 , C07D209/20 , C07D209/30 , C07D209/42 , C07D333/62 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/02 , C07D471/04 , C07D491/02 , C07D498/02 , C07H19/056 , A61K31/4402
CPC分类号： C07D333/62 , C07D209/08 , C07D209/30 , C07D209/42 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07D471/04
摘要： An isomer, enantiomer, diastereoisomer, or tautomer of a compound, represented by formula (I) wherein: A is O, S, NR1, or CR1, wherein R1 is defined herein; represents either a single or a double bond;R2 is selected from: H, halogen, R21, OR21, SR21, COOR21, SO2N(R22)2, N(R22)2, CON(R22)2, NR22C(O)R22 or NR22C(O)NR22 wherein R21 and each R22 is defined herein;B is NR3 or CR3, with the proviso that one of A or B is either CR1 or CR3, wherein R3 is defined herein;K is N or CR4, wherein R4 is defined herein;L is N or CR5, wherein R5 has the same definition as R4 defined above;M is N or CR7, wherein R7 has the same definition as R4 defined above;Y1 is O or S;Z is N(R6a)R6 or OR6, wherein R6a is H or alkyl or NR61R62 wherein R61 and R62 are defined herein;a salt or a derivative thereof, as an inhibitor of HCV NS5B polymerase.
摘要翻译：由式（I）表示的化合物的异构体，对映异构体，非对映异构体或互变异构体，其中：A是O，S，NR 1或CR 1，其中R 1在本文中定义; 代表单键或双键; R2选自：H，卤素，R21，OR21，SR21，COOR21，SO2N（R22）2，N（R22）2，CON（R22）2，NR22C（O） NR 22 C（O）NR 22，其中R 21和每个R 22如本文所定义; B是NR 3或CR 3，条件是A或B中的一个是CR 1或CR 3，其中R 3在本文中定义; K是N或CR 4，其中R 4是 L是N或CR5，其中R5具有与上述定义的R4相同的定义; M是N或CR7，其中R7具有与上述定义的R4相同的定义; Y1是O或S; Z是N（R6a）R6 或OR 6，其中R 6a是H或烷基或NR 61 R 62，其中R 61和R 62在本文中定义;其盐或其衍生物，作为HCV NS5B聚合酶的抑制剂。

3. 发明申请

WO03010141A3 HEPATITIS C VIRUS POLYMERASE INHIBITORS WITH A HETEROBICYCLIC STRUCTURE 审中-公开
标题翻译：具有异构结构的丙型肝炎病毒聚合酶抑制剂
公开(公告)号：WO03010141A3
公开(公告)日：2003-05-30
申请号：PCT/CA0201128
申请日：2002-07-18
申请人： BOEHRINGER INGELHEIM CA LTD , BEAULIEU PIERRE LOUIS , FAZAL GULREZ , GOULET SYLVIE , KUKOLJ GEORGE , POIRIER MARTIN , TSANTRIZOS YOULA S , JOLICOEUR ERIC , GILLARD JAMES , POUPART MARC-ANDRE , RANCOURT JEAN
发明人： BEAULIEU PIERRE LOUIS , FAZAL GULREZ , GOULET SYLVIE , KUKOLJ GEORGE , POIRIER MARTIN , TSANTRIZOS YOULA S , JOLICOEUR ERIC , GILLARD JAMES , POUPART MARC-ANDRE , RANCOURT JEAN
IPC分类号： A61K31/13 , A61K31/381 , A61K31/404 , A61K31/405 , A61K31/4184 , A61K31/422 , A61K31/427 , A61K31/428 , A61K31/437 , A61K31/443 , A61K31/4436 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/497 , A61K31/506 , A61K31/53 , A61K31/5377 , A61K31/7052 , A61K38/21 , A61K45/00 , A61P31/12 , A61P31/14 , A61P37/02 , A61P43/00 , C07D20060101 , C07D209/08 , C07D209/14 , C07D209/20 , C07D209/30 , C07D209/42 , C07D333/62 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/02 , C07D471/04 , C07D491/02 , C07D498/02 , C07H19/056 , C07D403/12
CPC分类号： C07D333/62 , C07D209/08 , C07D209/30 , C07D209/42 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07D471/04
摘要： An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein: A is O, S, NR , or CR , wherein R is defined herein; represents either a single or a double bond;R is selected from: H, halogen, R , OR , SR , COOR ,SO2N(R )2, N(R )2, , CON(R )2,NR C(O)R or NR C(O)NR wherein R and each R is defined herein; B is NR or CR , with the proviso that one of A or B is either CR or CR , wherein R is defined herein; K is N or CR , wherein R is defined herein; L is N or CR , wherein R has the same definition as R ; M is N or CR , wherein R has the same definition as R ; Y is O or S; Z is N(R )R or OR , wherein R is H or alkyl or NR R wherein R and R are defined herein; and R is H, alkyl, cycloalkyl, alkenyl, Het, alkyl-aryl, alkyl-Het;or R is wherein R and R and Q are as defined herein; Y is O or S; R is H, (C1-6 alkyl), (C3-7)cycloalkyl or (C1-6)alkyl-(C3-7)cycloalkyl, aryl, Het, (C1-6)alkyl-aryl or (C1-6)alkyl-Het, all of which optionally substituted with R ; or R is covalently bonded to either of R or R to form a 5- or 6-membered heterocycle; a salt or a derivative thereof, as an inhibitor of HCV NS5B polymerase.
摘要翻译：由式I表示的化合物的异构体，对映异构体，非对映异构体或互变异构体：其中：A是O，S，NR 1或CR 1，其中R 1在本文中定义; 表示单键或双键; R 2选自：H，卤素，R 21，OR 21，SR 21，COOR 21，SO 2 N（R 22）2， N（R 22）2，CON（R 22）2，NR 22 C（O）R 22或NR 22 C（O）NR 22其中R 21和每个R 22在本文中定义; B是NR 3或CR 3，条件是A或B中的一个是CR 1或CR 3，其中R 3在本文中定义; K是N或CR 4，其中R 4在本文中定义; L是N或CR 5，其中R 5具有与R 4相同的定义; M是N或CR 7，其中R 7具有与R 4相同的定义; Y 1是O或S; Z是N（R 6a）R 6或OR 6，其中R 6a是H或烷基或NR 61 R 62，其中R 61和R 62定义在本文中 ; 且R 6为H，烷基，环烷基，烯基，Het，烷基 - 芳基，烷基-Het;或R 6为其中R 7和R 8和Q如本文所定义; Y 2为O或S; R 9是H，（C 1-6烷基），（C 3-7）环烷基或（C 1-6）烷基 - （C 3-7）环烷基，芳基，Het，（C 1-6）烷基 - 芳基或（C 1 -6）烷基-Het，它们全部被R 90取代; 或R 9与R 7或R 8中的任一个共价键合以形成5-或6-元杂环; 其盐或其衍生物，作为HCV NS5B聚合酶的抑制剂。

4. 发明公开

EP1682547A4 RSV POLYMERASE INHIBITORS 有权
标题翻译：抑制剂RSV聚合酶
公开(公告)号：EP1682547A4
公开(公告)日：2008-12-31
申请号：EP04789793
申请日：2004-10-28
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： SIMONEAU BRUNO , BORDELEAU JOSEE , FAZAL GULREZ , LANDRY SERGE , MASON STEVE , RANCOURT JEAN
IPC分类号： C07D471/04 , A61K31/437 , A61K31/4745 , A61P11/00 , A61P31/12 , C07D471/02
CPC分类号： C07D471/04 , A61K31/4353 , A61K31/437

5. 发明专利

CY1107355T1 ΑΝΑΣΤΟΛΕΙΣ ΠΟΛΥΜΕΡΑΣΗΣ ΙΟΥ ΗΠΑΤΙΤΙΔΑΣ C ΜΕ ΜΙΑ ΕΤΕΡΟΔΙΚΥΚΛΙΚΗ ΔΟΜΗ 未知
公开(公告)号：CY1107355T1
公开(公告)日：2012-12-19
申请号：CY081100332
申请日：2008-03-21
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： BEAULIEU PIERRE LOUIS , FAZAL GULREZ , GOULET SYLVIE , KUKOLJ GEORGE , POIRIER MARTIN , TSANTRIZOS YOULA S , JOLICOEUR ERIC , GILLARD JAMES , POUPART MARC-ANDRE , RANCOURT JEAN
IPC分类号： C07D209/00 , A61K31/13 , A61K31/381 , A61K31/404 , A61K31/405 , A61K31/4184 , A61K31/422 , A61K31/427 , A61K31/428 , A61K31/437 , A61K31/443 , A61K31/4436 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/497 , A61K31/506 , A61K31/53 , A61K31/5377 , A61K31/7052 , A61K38/21 , A61K45/00 , A61P31/12 , A61P31/14 , A61P37/02 , A61P43/00 , C07D20060101 , C07D209/08 , C07D209/14 , C07D209/20 , C07D209/30 , C07D209/42 , C07D333/62 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/02 , C07D471/04 , C07D491/02 , C07D498/02 , C07H19/056
摘要： Έναισομερές, εναντιομερές, διαστερεοϊσομερέςή ταυτομερέςμιαςένωσης, πουαναπαρίσταταιμέσωτουχημικούτύπου I: στονοποίον: τοΑ είναιταΟ, S, NR1, ή CR1, στοοποίοτο R1 ορίζεταισύμφωναμετοπαρόν · αναπαριστάδεείτεένανμονόή ένανδιπλόδεσμό· το R2 επιλέγεταιαπότα: Η, αλογόνο, R21, OR21, SR21, COOR21, SO2N(R22), N(R22)2, CON(R22)2, NR22C(O)NR22, ή NR22C(O)NR22, σταοποίατο R21 καιτοκαθένα R22 καθορίζονταισύμφωναμετοπαρόν· τοΒ είναιτα NR3 ή CR3, μετηνπροϋπόθεσηότιέναεκτωνΑ ήΒ είναιείτετο CR1 ή CR3, στοοποίοτο R3 ορίζεταισύμφωναμετοπαρόν· τοΚ είναιταΝ ή CR4, στοοποίοτο R4 ορίζεταισύμφωναμετοπαρόν· το L είναιτοΝ ή CR5, στονοποίοτο R5 έχειτονίδιοορισμόωςτο R4· τοΜ είναιταΝ ή CR7, στοοποίοτο R7 έχειτονίδιοορισμόωςτο R4· τοΥ1 είναιταΟ ή S· τοΖ είναιτα N(R6a)R6 ή OR6, στονοποίοτο R6a είναιτοΗ ήτοαλκύλιοή το NR61R62 στοοποίοτα R61 και R62 καθορίζονταισύμφωναμετοπαρόν· καιτο R6 είναιταΗ, αλκύλιο, κυκλοαλκύλιο, αλκενύλιο, Het, αλκυλ-αρύλιο, αλκυλ-Het· ήτο R6 στοοποίοτα R7 και R8 και Q καθορίζονταισύμφωναμετοπαρόν· τοΥ2 είναιταΟ ή S· το R9 είναιταΗ, (C1-6 αλκύλιο), (C3-7)κυκλοαλκύλιοή (C1-6)αλκύλιο-(C3-7)κυκλοαλκύλιο, αρύλιο, Het, (C1-6)αλκυλ-αρύλιοή (C1-6)αλκύλ-Ηet, όλαεκτωνοποίωνυποκαθίστανταιπροαιρετικώςμε R90 · ήτο R9 συνδέεταιομοιοπολικώςστοόποιοεκτων R7 ή R8 γιατονσχηματισμόενός 5- ή 6-μελούςετερόκυκλου· έναάλαςή έναπαράγωγοεξαυτών, ωςέναςαναστολέαςτηςπολυμεράσης NS5B του HCV.

6. 发明专利

MEP59608A HEPATITIS C VIRUS POLYMERASE INHIBITORS WITH HETEROBICYCLIC STRUCTURE 未知
公开(公告)号：MEP59608A
公开(公告)日：2011-05-10
申请号：MEP59608
申请日：2002-07-18
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： BEAULIEU PIERRE LOUIS , FAZAL GULREZ , KUKOLJ GEORGE , JOLICOEUR ERIC , GILLARD JAMES , POUPART MARC-ANDRE , RANCOURT JEAN
IPC分类号： A61K31/13 , A61K31/381 , A61K31/404 , A61K31/405 , A61K31/4184 , A61K31/422 , A61K31/427 , A61K31/428 , A61K31/437 , A61K31/4402 , A61K31/443 , A61K31/4436 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/497 , A61K31/506 , A61K31/53 , A61K31/5377 , A61K31/7052 , A61K38/21 , A61K45/00 , A61P31/12 , A61P31/14 , A61P37/02 , A61P43/00 , C07D20060101 , C07D209/08 , C07D209/14 , C07D209/20 , C07D209/30 , C07D209/42 , C07D333/62 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/02 , C07D471/04 , C07D491/02 , C07D498/02 , C07H19/056
摘要： An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein: A is O, S, N R 1 , or C R 1 , wherein R 1 is defined herein; ----- represents either a single or a double bond; R 2 is selected from: H, halogen, R 21 , O R 21 , S R 21 , COO R 21 , SO 2 N( R 22 ) 2 , N( R 22 ) 2 , , CON( R 22 ) 2 , N R 22 C(O) R 22 or N R 22 C(O)N R 22 wherein R 21 and each R 22 is defined herein; B is N R 3 or C R 3 , with the proviso that one of A or B is either C R 1 or C R 3 , wherein R 3 is defined herein; K is N or C R 4 , wherein R 4 is defined herein; L is N or C R 5 , wherein R 5 has the same definition as R 4 ; M is N or C R 7 , wherein R 7 has the same definition as R 4 ; Y 1 is O or S; Z is N( R 6a ) R 6 or O R 6 , wherein R 6a is H or alkyl or N R 61 R 62 wherein R 61 and R 62 are defined herein; and R 6 is H, alkyl, cycloalkyl, alkenyl, Het , alkyl-aryl, alkyl- Het ; or R 6 is wherein R 7 and R 8 and Q are as defined herein; Y 2 is O or S; R 9 is H, (C 1-6 alkyl), (C 3-7 )cycloalkyl or (C 1-6 )alkyl-(C 3-7 )cycloalkyl, aryl, Het , (C 1-6 )alkyl-aryl or (C 1-6 )alkyl- Het , all of which optionally substituted with R 90 ; or R 9 is covalently bonded to either of R 7 or R 8 to form a 5- or 6-membered heterocycle; a salt or a derivative thereof, as an inhibitor of HCV NS5B polymerase.

7. 发明专利

HRP20090668A2 VIRAL POLYMERASE INHIBITORS 未知
公开(公告)号：HRP20090668A2
公开(公告)日：2010-07-31
申请号：HRP20090668
申请日：2009-12-14
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： BEAULIEU PIERRE LOUIS , FAZAL GULREZ , GILLARD JAMES , GOULET SYLVIE , JOLICOEUR ERIC , POIRIER MARTIN , POUPART MARC-ANDRE , RANCOURT JEAN , TSANTRIZOS YOULA S , KUKOLJ GEORGE
IPC分类号： A61K31/404 , A61K31/13 , A61K31/381 , A61K31/405 , A61K31/4184 , A61K31/422 , A61K31/427 , A61K31/428 , A61K31/437 , A61K31/443 , A61K31/4436 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/497 , A61K31/506 , A61K31/53 , A61K31/5377 , A61K31/7052 , A61K38/21 , A61K45/00 , A61P31/12 , A61P31/14 , A61P37/02 , A61P43/00 , C07D20060101 , C07D209/08 , C07D209/14 , C07D209/20 , C07D209/30 , C07D209/42 , C07D333/62 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/02 , C07D471/04 , C07D491/02 , C07D498/02 , C07H19/056
摘要： An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein: A is O, S, N R 1 , or C R 1 , wherein R 1 is defined herein; ----- represents either a single or a double bond; R 2 is selected from: H, halogen, R 21 , O R 21 , S R 21 , COO R 21 , SO 2 N( R 22 ) 2 , N( R 22 ) 2 , , CON( R 22 ) 2 , N R 22 C(O) R 22 or N R 22 C(O)N R 22 wherein R 21 and each R 22 is defined herein; B is N R 3 or C R 3 , with the proviso that one of A or B is either C R 1 or C R 3 , wherein R 3 is defined herein; K is N or C R 4 , wherein R 4 is defined herein; L is N or C R 5 , wherein R 5 has the same definition as R 4 ; M is N or C R 7 , wherein R 7 has the same definition as R 4 ; Y 1 is O or S; Z is N( R 6a ) R 6 or O R 6 , wherein R 6a is H or alkyl or N R 61 R 62 wherein R 61 and R 62 are defined herein; and R 6 is H, alkyl, cycloalkyl, alkenyl, Het , alkyl-aryl, alkyl- Het ; or R 6 is wherein R 7 and R 8 and Q are as defined herein; Y 2 is O or S; R 9 is H, (C 1-6 alkyl), (C 3-7 )cycloalkyl or (C 1-6 )alkyl-(C 3-7 )cycloalkyl, aryl, Het , (C 1-6 )alkyl-aryl or (C 1-6 )alkyl- Het , all of which optionally substituted with R 90 ; or R 9 is covalently bonded to either of R 7 or R 8 to form a 5- or 6-membered heterocycle; a salt or a derivative thereof, as an inhibitor of HCV NS5B polymerase.

8. 发明专利

CA2450033C VIRAL POLYMERASE INHIBITORS 未知
公开(公告)号：CA2450033C
公开(公告)日：2009-07-07
申请号：CA2450033
申请日：2002-07-18
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： BEAULIEU PIERRE LOUIS , KUKOLJ GEORGE , FAZAL GULREZ , JOLICOEUR ERIC , GILLARD JAMES , POUPART MARC-ANDRE , RANCOURT JEAN
IPC分类号： C07D401/04 , A61K31/13 , A61K31/381 , A61K31/395 , A61K31/404 , A61K31/405 , A61K31/4184 , A61K31/422 , A61K31/427 , A61K31/428 , A61K31/437 , A61K31/443 , A61K31/4436 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/497 , A61K31/506 , A61K31/53 , A61K31/5377 , A61K31/7052 , A61K38/21 , A61K45/00 , A61P31/12 , A61P31/14 , A61P37/02 , A61P43/00 , C07D20060101 , C07D209/04 , C07D209/08 , C07D209/14 , C07D209/20 , C07D209/30 , C07D209/42 , C07D333/62 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/02 , C07D471/04 , C07D491/02 , C07D498/02 , C07H19/056
摘要： An isomer, enantiomer, diastereoisomer, or tautomer of a compound, represent ed by formula (I) wherein: A is O, S, NR1, or CR1, wherein R1 is defined herein ; represents either a single or a double bond;R2 is selected from: H, halogen, R21, OR21, SR21, COOR21, SO2N(R22)2, N(R22)2, CON(R22)2, NR22C(O)R22 or NR22C(O)NR22 wherein R21 and each R22 is defined herein;B is NR3 or CR3, wit h the proviso that one of A or B is either CR1 or CR3, wherein R3 is defined herein;K is N or CR4, wherein R4 is defined herein;L is N or CR5, wherein R5 has the same definition as R4 defined above;M is N or CR7, wherein R7 has th e same definition as R4 defined above;Y1 is O or S;Z is N(R6a)R6 or OR6, where in R6a is H or alkyl or NR61R62 wherein R61 and R62 are defined herein;a salt o r a derivative thereof, as an inhibitor of HCV NS5B polymerase.

9. 发明专利

AT382348T 未知
公开(公告)号：AT382348T
公开(公告)日：2008-01-15
申请号：AT02750715
申请日：2002-07-18
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： BEAULIEU PIERRE , FAZAL GULREZ , KUKOLJ GEORGE , JOLICOEUR ERIC , GILLARD JAMES , POUPART MARC-ANDRE , RANCOURT JEAN
IPC分类号： A61K31/404 , A61K31/13 , A61K31/381 , A61K31/405 , A61K31/4184 , A61K31/422 , A61K31/427 , A61K31/428 , A61K31/437 , A61K31/4402 , A61K31/443 , A61K31/4436 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/497 , A61K31/506 , A61K31/53 , A61K31/5377 , A61K31/7052 , A61K38/21 , A61K45/00 , A61P31/12 , A61P31/14 , A61P37/02 , A61P43/00 , C07D20060101 , C07D209/08 , C07D209/14 , C07D209/20 , C07D209/30 , C07D209/42 , C07D333/62 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/02 , C07D471/04 , C07D491/02 , C07D498/02 , C07H19/056
摘要： An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein: A is O, S, N R 1 , or C R 1 , wherein R 1 is defined herein; ----- represents either a single or a double bond; R 2 is selected from: H, halogen, R 21 , O R 21 , S R 21 , COO R 21 , SO 2 N( R 22 ) 2 , N( R 22 ) 2 , , CON( R 22 ) 2 , N R 22 C(O) R 22 or N R 22 C(O)N R 22 wherein R 21 and each R 22 is defined herein; B is N R 3 or C R 3 , with the proviso that one of A or B is either C R 1 or C R 3 , wherein R 3 is defined herein; K is N or C R 4 , wherein R 4 is defined herein; L is N or C R 5 , wherein R 5 has the same definition as R 4 ; M is N or C R 7 , wherein R 7 has the same definition as R 4 ; Y 1 is O or S; Z is N( R 6a ) R 6 or O R 6 , wherein R 6a is H or alkyl or N R 61 R 62 wherein R 61 and R 62 are defined herein; and R 6 is H, alkyl, cycloalkyl, alkenyl, Het , alkyl-aryl, alkyl- Het ; or R 6 is wherein R 7 and R 8 and Q are as defined herein; Y 2 is O or S; R 9 is H, (C 1-6 alkyl), (C 3-7 )cycloalkyl or (C 1-6 )alkyl-(C 3-7 )cycloalkyl, aryl, Het , (C 1-6 )alkyl-aryl or (C 1-6 )alkyl- Het , all of which optionally substituted with R 90 ; or R 9 is covalently bonded to either of R 7 or R 8 to form a 5- or 6-membered heterocycle; a salt or a derivative thereof, as an inhibitor of HCV NS5B polymerase.

10. 发明专利

DE60124718T2 未知
公开(公告)号：DE60124718T2
公开(公告)日：2007-09-13
申请号：DE60124718
申请日：2001-07-04
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： BEAULIEU LOUIS , FAZAL GULREZ , GILLARD JAMES , KUKOLJ GEORGE , AUSTEL VOLKHARD
IPC分类号： C07D235/18 , C12N9/99 , A61K31/4184 , A61K31/4192 , A61K31/422 , A61K31/427 , A61K31/443 , A61K31/4439 , A61K31/497 , A61P31/14 , A61P43/00 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04
摘要： A compound of the formula I: wherein: X is CH or N; Y is O or S; Z is OH, NH 2 , NMeR 3 , NHR 3 ; OR 3 or 5- or 6-membered heterocycle, having 1 to 4 heteroatoms selected from O, N and S, said heterocycle being optionally substituted with from 1 to 4 substituents; A is N, COR 7 or CR 5 , wherein R 5 is H, halogen, or (C 1-6 ) alkyl and R 7 is H or (C 1-6 alkyl), with the proviso that X and A are not both N; R 6 is H, halogen, (C 1-6 alkyl) or OR 7 , wherein R 7 is H or (C 1-6 alkyl); R 1 is selected from the group consisting of 5- or 6-membered heterocycle having 1 to 4 heteroatoms selected from O, N, and S, phenyl, phenyl(C 1-3 )alkyl, (C 2-6 )alkenyl, phenyl(C 2-6 )alkenyl, (C 3-6 )cycloalkyl, (C 1-6 )alkyl, CF 3 , 9- or 10-membered heterobicycle having 1 to 4 heteroatoms selected from O, N and S, wherein said heterocycle, phenyl, phenyl(C 2-6 )alkenyl and phenyl(C 1-3 )alkyl), alkenyl, cycloalkyl, (C 1-6 )alkyl, and heterobicycle are all optionally substituted with from 1 to 4 substituents; R 2 is selected from (C 1-6 )alkyl, (C 3-7 )cycloalkyl, (C 3-7 )cycloalkyl(C 1-3 )alkyl, (C 6-10 )bicycloalkyl, adamantyl, phenyl, and pyridyl, all of which is optionally substituted with from 1 to 4 substituents; R 3 is selected from H, (C 1-6 )alkyl, (C 3-6 )cycloalkyl, (C 3-6 )cycloalkyl(C 1-6 )alkyl, (C 6-10 )aryl, (C 6-10 )aryl(C 1-6 )alkyl, (C 2-6 )alkenyl, (C 3-6 )cycloalkyl(C 2-6 )alkenyl, (C 6-10 )aryl(C 2-6 )alkenyl, N{(C 1-6 )alkyl} 2 , NHCOO(C 1-6 )alkyl(C 6-10 )aryl, NHCO(C 6-10 )aryl, (C 1-6 )alkyl-5- or 10-atom heterocycle, having 1 to 4 heteroatoms selected from O, N and S, and 5- or 10-atom heterocycle having 1 to 4 heteroatoms selected from O, N and S; wherein said alkyl, cycloalkyl, aryl, alkenyl and heterocycle are all optionally substituted with from 1 to 4 substituents; n is zero or 1; or a detectable derivative or salt thereof. The compounds of the invention may be used as inhibitors of hepatitis C virus replication. The invention further provides a method for treating or preventing hepatitis C virus infection.

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