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1. 发明申请

WO02076982A3 NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS 审中-公开
标题翻译：非核苷酸逆转录酶抑制剂
公开(公告)号：WO02076982A3
公开(公告)日：2002-12-12
申请号：PCT/CA0200385
申请日：2002-03-21
申请人： BOEHRINGER INGELHEIM CA LTD , OGILVIE WILLIAM W , DEZIEL ROBERT , NAUD JULIE , O'MEARA JEFFREY
发明人： OGILVIE WILLIAM W , DEZIEL ROBERT , NAUD JULIE , O'MEARA JEFFREY
IPC分类号： A61K31/551 , A61P31/14 , A61P31/18 , A61P43/00 , C07D471/14 , A61K31/55
CPC分类号： C07D471/14
摘要： A compound of formula (I) wherein A is a connecting chain of (C1-3) alkyl; B is O or S; R is H, (C1-6) alkyl, halo, CF3, or OR wherein R is H or (C1-6)alkyl; R is H or Me; R is H or Me; R is H, (C1-4) alkyl, (C3-4) cycloalkyl and (C1-4)alkyl(C3-7)cycloalkyl; W is selected form formula (i), (ii) or (iii) wherein, a) one of Y is SO2 and the other Y is NR , provided that both are not the same, wherein R is H, (C1-6)alkyl,(C3-6) cycloalkyl, the alkyl being substituted, COR , COOR or CONR R ; and each R is H, (C1-4) alkyl, (C3-6) cycloalkyl, or (C1-4) alkyl-(C3-6) cycloalkyl; or b) E is CR R wherein R and R is H, or alkyl and J is CH2; or J is CR R and E is CH2, and the dotted line represents a single bond; or c) E is C(O) and J is CR R or J is C(O) and E is CR R and the dotted line represents a single bond; or d) E and J are CR R and the dotted line represents a double bond. Compounds of formula I have activity against HIV WT and double mutant strains.
摘要翻译：式（I）的化合物，其中A是（C 1-3）烷基的连接链; B是O或S; R 1是H，（C 1-6）烷基，卤素，CF 3或OR 1a，其中R 1a是H或（C 1-6）烷基; R 2是H或Me; R 3是H或Me; R 4是H，（C 1-4）烷基，（C 3-8）环烷基和（C 1-4）烷基（C 3-7）环烷基; W选自式（i），（ii）或（iii），其中a）Y中的一个是SO 2，另一个Y是NR 5，条件是两者不同，其中R 5是H ，（C 1-6）烷基，（C 3-6）环烷基，取代的烷基，COR 50，COOR 5或CONR 5 R 5; 并且每个R 8是H，（C 1-4）烷基，（C 3-6）环烷基或（C 1-4）烷基 - （C 3-6）环烷基; 或b）E是CR 8a R 8b，其中R 8a和R 8b是H，或烷基，J是CH 2; 或J为CR 8a R 8b且E为CH 2，虚线表示单键; 或c）E是C（O），J是CR 8a R 8b或J是C（O），E是CR 8a R 8b，虚线代表单键; 或d）E和J是CR 8a R 8b，虚线表示双键。式I化合物具有抗HIV WT和双突变株的活性。

2. 发明申请

WO0250082A3 INHIBITORS OF PAPILLOMA VIRUS 审中-公开
标题翻译： PAPILLOMA病毒的抑制剂
公开(公告)号：WO0250082A3
公开(公告)日：2002-12-19
申请号：PCT/CA0101800
申请日：2001-12-14
申请人： BOEHRINGER INGELHEIM CA LTD , YOAKIM CHRISTIANE , HACHE BRUNO , OGILVIE WILLIAM W , O'MEARA JEFFREY , WHITE PETER , GOUDREAU NATHALIE
发明人： YOAKIM CHRISTIANE , HACHE BRUNO , OGILVIE WILLIAM W , O'MEARA JEFFREY , WHITE PETER , GOUDREAU NATHALIE
IPC分类号： A61K31/34 , A61K31/343 , A61K31/36 , A61K31/381 , A61K31/407 , A61K31/4245 , A61K31/428 , A61K31/4725 , A61K31/5377 , A61P31/12 , A61P31/20 , C07D307/94 , C07D405/12 , C07D407/10 , C07D407/12 , C07D407/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D491/04 , C07D491/107 , C07D493/04 , C07D493/10 , C07D495/10 , C07D495/12 , C07D495/14 , C07D495/20
CPC分类号： C07D405/12 , C07D307/94 , C07D407/12 , C07D407/14 , C07D413/12 , C07D417/12 , C07D491/04 , C07D493/04 , C07D493/10 , C07D495/12
摘要： A compound of formula (I) or its enantiomers or diastereoisomers thereof:wherein: A is a 5- or 6-membered homocyclic ring, or a 5- or 6-membered heterocyclic ring containing 1 or more heteroatoms; X is H and W is OH; or X and W together form a carbonyl group or an epoxide; R1 is H; or one or two substituents; Y is phenyl optionally mono- or di-substituted, said phenyl ring being optionally fused with a saturated or unsaturated 4 to 6-membered ring optionally containing a heteroatom; or Y is a heterocycle (Het) containing one or more heteroatoms, said Het optionally mono- or di-substituted, said Het being optionally fused with a saturated or unsaturated 4 to 6-membered ring optionally containing a heteroatom; or Y is ethylene-phenyl, said ethylene moiety being optionally mono-substituted, wherein said phenyl ring is optionally mono- or di-substituted, said phenyl ring being optionally fused with a saturated or unsaturated 4 to 6-membered ring optionally containing a heteroatom; or Y is ethylene-Het, said ethylene moiety being optionally mono-substituted, wherein Het is optionally mono- or di-substituted; said Het being optionally fused with a saturated or unsaturated 4 to 6-membered ring optionally containing a heteroatom; R3 is selected from the group consisting of: lower alkyl, lower cycloalkyl, lower alkylene, aryl or lower aralkyl, all of which optionally mono- or di-substituted, said lower cycloalkyl, aryl, lower aralkyl or Het being optionally fused with a saturated or unsaturated 4 to 6-membered ring optionally containing a heteroatom; and R4 is a carboxylic acid, a salt or an ester thereof.The compounds of the invention may be used as inhibitors of the papilloma virus E1-E2-DNA complex. The invention further provides a method of treating or preventing human papilloma virus infection.
摘要翻译：式（I）化合物或其对映异构体或非对映异构体：其中：A为5-或6-元级环，或含有1个或多个杂原子的5或6元杂环; X是H，W是OH; 或X和W一起形成羰基或环氧化物; R1是H; 或一个或两个取代基; Y是任选被一或二取代的苯基，所述苯环任选地与任选地含有杂原子的饱和或不饱和的4至6元环稠合; 或Y是含有一个或多个杂原子的杂环（Het），所述Het任选地被单取代或二取代，所述Het任选地与任选地含有杂原子的饱和或不饱和的4至6元环稠合; 或Y是乙烯 - 苯基，所述乙烯部分任选被单取代，其中所述苯环任选被一或二取代，所述苯环任选与饱和或不饱和的4至6元环稠合，任选地含有杂原子 ; 或Y是乙烯-Het，所述乙烯部分任选是单取代的，其中Het任选被一或二取代; 所述Het任选地与任选地含有杂原子的饱和或不饱和的4至6元环稠合; R 3选自：低级烷基，低级环烷基，低级亚烷基，芳基或低级芳烷基，所有这些可任选被一或二取代，所述低级环烷基，芳基，低级芳烷基或Het任选地与饱和的或任选含有杂原子的不饱和4至6元环; 并且R 4是羧酸，其盐或酯。本发明的化合物可以用作乳头瘤病毒E1-E2-DNA复合物的抑制剂。本发明还提供了治疗或预防人乳头状瘤病毒感染的方法。

3. 发明专利

ES2268499T3 INHIBIDORES NO NUCLEOSIDOS DE TRANSCRIPTASA INVERESA. 未知
公开(公告)号：ES2268499T3
公开(公告)日：2007-03-16
申请号：ES03816107
申请日：2003-09-15
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： YOAKIM CHRISTIANE , MALENFANT ERIC , THAVONEKHAM BOUNKHAM , OGILVIE WILLIAM W , DEZIEL ROBERT
IPC分类号： C07D471/14 , A61K31/55 , A61P31/18 , C07D221/00 , C07D243/00
摘要： Un compuesto representado por la fórmula I: en la que R1 se elige entre el grupo formado por H, halógeno, alquilo C1-4, O-alquilo C1-6 y haloalquilo; R2 es H o alquilo C1-4; R3 es H o alquilo C1-4; R4 es alquilo C1-4, (alquil C1-4)-cicloalquilo C3-7 o ciclo- alquilo C3-7 y Q es un heterociclo saturado de 5 ó 6 eslabones, fusionado con un fenilo, que tiene uno o dos heteroátomos elegidos entre O y N, dicho Q se elige entre el grupo formado por: a) en el que uno de E y G es C(O) y el otro es NR5, en el que R5 se elige entre el grupo formado por H, hidroxi y alquilo C1-4 sin sustituir o sustituido por piridinilmetilo, (N-óxido de piridinil)metilo o C(O)OR6, en el que R6 es H o alquilo C1-4; y cada R7 con independencia de su aparición es H, Me o Et; o b) en el que E es NR8, en el que R8 es H, alquilo C1-4 sin sus- tituir o sustituido por C(O)OR9, en el que R9 es H o alquilo C1-4; o c) en el que D y G son NR10, en el que cada R10 con independencia de su aparición es H o alquilo C1-4 sin sustituir o sustituir por C(O)OR11, en el que R11 es H o alquilo C1-4; o d) en el que uno de L, M, Y y Z es NR12, en el que R12 es H, alquilo C1-4 sin sustituir o sustituido por C(O)OR12x, en el que R12x es H o alquilo C1-4; una de las posiciones restantes de L, M, Y y Z contiguas a NR12 es C(O); y las dos posiciones restantes son en cada caso CR13R13, en el que cada R13 con independencia de su aparición es H, Me o Et; o e) en el que tres posiciones contiguas de L, M, Y y Z (a saber: L-M-Y o M-Y-Z) significan NR14-C(O)-O- o -NR15-C(O)-NR16-, en los que R14, R15 y R16 significan en cada caso H o alquilo C1-4 sin sustituir o sustituido por C(O)OR17, en el que R17 es H o alquilo C1-4; y la posición restante de L o de Z es CR18R18, en el que cada R18 es H, Me o Et; o una sal farmacéuticamente aceptable o un profármaco del mismo.

4. 发明专利

AT331716T 未知
公开(公告)号：AT331716T
公开(公告)日：2006-07-15
申请号：AT03816107
申请日：2003-09-15
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： YOAKIM CHRISTIANE , MALENFANT ERIC , THAVONEKHAM BOUNKHAM , OGILVIE WILLIAM W , DEZIEL ROBERT
IPC分类号： A61P31/18 , C07D471/14 , A61K31/55 , C07D243/00 , C07D221/00
摘要： Compounds represented by formula I: wherein R 1 is H, halogen, (C 1-4 )alkyl, O(C 1-4 )alkyl, and haloalkyl; R 2 is H or (C 1-4 )alkyl; R 3 is H or (C 1-4 )alkyl; R 4 is (C 1-4 )alkyl, (C 1-4 )alkyl(C 3-7 )cycloalkyl, or (C 3-7 )cycloalkyl; and Q is a fused phenyl-5 or 6-membered saturated heterocycle having one to two heteroatoms selected from O and N, said Q being optionally substituted with hydroxy, or (C 1-4 )alkyl which in turn maybe optionally substituted with pyridinyl-N-oxide or C(O)OR wherein R is H or (C 1-4 )alkyl; or a salt thereof. The compounds have inhibitory activity against Wild Type, and single and double mutants strains, of HIV.

5. 发明专利

AT288434T 未知
公开(公告)号：AT288434T
公开(公告)日：2005-02-15
申请号：AT02716563
申请日：2002-03-21
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： OGILVIE WILLIAM W , D ZIEL ROBERT , NAUD JULIE , O'MEARA JEFFREY , DALE R CAMERON
IPC分类号： A61K31/551 , A61P31/14 , A61P31/18 , A61P43/00 , C07D471/14
摘要： A compound of formula I: wherein A is a connecting chain of (C1-3) alkyl; B is O or S; R is H, (C1-6) alkyl, halo, CF3, or OR wherein R is H or (C1-6)alkyl; R is H or Me; R is H or Me; R is H, (C1-4) alkyl, (C3-4) cycloalkyl and (C1-4)alkyl(C3-7)cycloalkyl; W is selected from wherein, a) one of Y is SO2 and the other Y is NR , provided that both are not the same, wherein R is H, (C1-6)alkyl,(C3-6) cycloalkyl, the alkyl being substituted, COR , COOR or CONR PR ; and each R is H, (C1-4) alkyl, (C3-6) cycloalkyl, or (C1-4) alkyl-(C3-6) cycloalkyl; or b) E is CR R wherein R and R is H, or alkyl and J is CH2; or J is CR R and E is CH2, and the dotted line represents a single bond; or c) E is C(O) and J is CR R or J is C(O) and E is CR R and the dotted line represents a single bond; or d) E and J are CR R and the dotted line represents a double bond. Compounds of formula I have activity against HIV WT and double mutant strains.

6. 发明专利

AU2003303944A1 NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS 未知
公开(公告)号：AU2003303944A1
公开(公告)日：2004-10-18
申请号：AU2003303944
申请日：2003-09-15
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： YOAKIM CHRISTIANE , MALENFANT ERIC , THAVONEKHAM BOUNKHAM , OGILVIE WILLIAM W , DEZIEL ROBERT
IPC分类号： A61P31/18 , C07D471/14 , A61K31/55
摘要： Compounds represented by formula I: wherein R 1 is H, halogen, (C 1-4 )alkyl, O(C 1-4 )alkyl, and haloalkyl; R 2 is H or (C 1-4 )alkyl; R 3 is H or (C 1-4 )alkyl; R 4 is (C 1-4 )alkyl, (C 1-4 )alkyl(C 3-7 )cycloalkyl, or (C 3-7 )cycloalkyl; and Q is a fused phenyl-5 or 6-membered saturated heterocycle having one to two heteroatoms selected from O and N, said Q being optionally substituted with hydroxy, or (C 1-4 )alkyl which in turn maybe optionally substituted with pyridinyl-N-oxide or C(O)OR wherein R is H or (C 1-4 )alkyl; or a salt thereof. The compounds have inhibitory activity against Wild Type, and single and double mutants strains, of HIV.

7. 发明专利

PT1021404E 未知
公开(公告)号：PT1021404E
公开(公告)日：2003-04-30
申请号：PT98947255
申请日：1998-10-06
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： DEZIEL ROBERT , OGILVIE WILLIAM W , O'MEARA JEFFREY , MALENFANT ERIC
IPC分类号： A61K31/397 , A61K31/4427 , A61K45/06 , A61P31/22 , C07D205/08 , C07D205/09 , C07D401/12 , A61K31/395
摘要： A compound of formula 1:wherein Y is S or O;R1 is C1-6 alkyl; (C0-6 alkyl)aryl; (C0-6 alkyl)Het; orR1 is an amino acid analog or dipeptide analog of the formula:wherein R2 is H, C1-10 alkyl; or an amide or ester group;A is C6-10 aryl, Het or CH-R3 wherein R3 is C1-6 alkyl or (C0-4 alkyl)aryl; andZ is H, C1-6 alkyl, or an acyl;R4 is hydrogen, lower alkyl, methoxy, ethoxy, or benzyloxy; andR5 is alkyl, cycloalkyl, carboxyl group; an aryl;Het or Het(lower alkyl); or R4 and R5 together with the nitrogen atom to which they are attached form a nitrogen containing ring optionally substituted with phenyl or C(O)OCH2-phenyl, said phenyl ring optionally mono- ordi-substituted with among others C(O)OR7 wherein R7 is lower alkyl or phenyl(lower alkyl); or a therapeutically acceptable acid addition salt thereof which compounds are useful in the treatment of HCMV infections.

8. 发明专利

CA2430909C INHIBITORS OF PAPILLOMA VIRUS 未知
公开(公告)号：CA2430909C
公开(公告)日：2010-12-14
申请号：CA2430909
申请日：2001-12-14
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： YOAKIM CHRISTIANE , HACHE BRUNO , OGILVIE WILLIAM W , O'MEARA JEFFREY , WHITE PETER , GOUDREAU NATHALIE
IPC分类号： C07D307/94 , A61K31/34 , A61K31/343 , A61K31/36 , A61K31/381 , A61K31/395 , A61K31/407 , A61K31/4245 , A61K31/428 , A61K31/4725 , A61K31/5377 , A61P31/12 , A61P31/20 , C07D405/12 , C07D407/10 , C07D407/12 , C07D407/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D491/04 , C07D491/048 , C07D491/107 , C07D493/04 , C07D493/10 , C07D495/10 , C07D495/12 , C07D495/14 , C07D495/20
摘要： A compound of formula (I) or its enantiomers or diastereoisomers thereof: (see formula I) wherein: A is a 5- or 6-membered homocyclic ring, or a 5- or 6-membered heterocyclic ring containing 1 or more heteroatoms; X is H and W is OH; or X and W together form a carbonyl group or an epoxide; R1 is H; or one or two substituents; Y is phenyl optionally mono- or di-substituted, said phenyl ring being optionally fused with a saturated or unsaturated 4 to 6-membered ring optionally containing a heteroatom; or Y is a heterocycle (Het) containing one or more heteroatoms, said Het optionally mono-or di-substituted, said Het being optionally fused with a saturated or unsaturated 4 to 6-membered ring optionally containing a heteroatom; or Y is ethylene-phenyl, said ethylene moiety being optionally mono-substituted, wherein said phenyl ring is optionally mono- or di-substituted, said phenyl ring being optionally fused with a saturated or unsaturated 4 to 6-membered ring optionally containing a heteroatom; or Y is ethylene-Het, said ethylene moiety being optionally mono-substituted, wherein Het is optionally mono- or di-substituted; said Het being optionally fused with a saturated or unsaturated 4 to 6-membered ring optionally containing a heteroatom; R3 is selected from the group consisting of: lower alkyl, lower cycloalkyl, lower alkylene, aryl or lower aralkyl, all of which optionally mono- or di-substituted, said lower cycloalkyl, aryl, lower aralkyl or Het being optionally fused with a saturated or unsaturated 4 to 6-membered ring optionally containing a heteroatom; and R4 is a carboxylic acid, a salt or an ester thereof. The compounds of the invention may be used as inhibitors of the papilloma virus E1--E2-DNA complex. The invention further provides a method of treating or preventing human papilloma virus infection.

9. 发明专利

DE60127451T2 未知
公开(公告)号：DE60127451T2
公开(公告)日：2007-11-29
申请号：DE60127451
申请日：2001-12-14
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： YOAKIM CHRISTIANE , HACHE BRUNO , OGILVIE WILLIAM W , O'MEARA JEFFREY , WHITE PETER , GOUDREAU NATHALIE
IPC分类号： C07D493/00 , A61K31/34 , A61K31/343 , A61K31/36 , A61K31/381 , A61K31/407 , A61K31/4245 , A61K31/428 , A61K31/4725 , A61K31/5377 , A61P31/12 , A61P31/20 , C07D307/94 , C07D405/12 , C07D407/10 , C07D407/12 , C07D407/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D491/04 , C07D491/107 , C07D493/04 , C07D493/10 , C07D495/10 , C07D495/12 , C07D495/14

10. 发明专利

PT1373267E 未知
公开(公告)号：PT1373267E
公开(公告)日：2005-05-31
申请号：PT02716563
申请日：2002-03-21
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： OGILVIE WILLIAM W , ROBERT D ZIEL , JULIE NAUD , JEFFREY O MEARA , CAMERON DALE R
IPC分类号： A61K31/551 , A61P31/14 , A61P31/18 , A61P43/00 , C07D471/14
摘要： A compound of formula I: wherein A is a connecting chain of (C1-3) alkyl; B is O or S; R is H, (C1-6) alkyl, halo, CF3, or OR wherein R is H or (C1-6)alkyl; R is H or Me; R is H or Me; R is H, (C1-4) alkyl, (C3-4) cycloalkyl and (C1-4)alkyl(C3-7)cycloalkyl; W is selected from wherein, a) one of Y is SO2 and the other Y is NR , provided that both are not the same, wherein R is H, (C1-6)alkyl,(C3-6) cycloalkyl, the alkyl being substituted, COR , COOR or CONR PR ; and each R is H, (C1-4) alkyl, (C3-6) cycloalkyl, or (C1-4) alkyl-(C3-6) cycloalkyl; or b) E is CR R wherein R and R is H, or alkyl and J is CH2; or J is CR R and E is CH2, and the dotted line represents a single bond; or c) E is C(O) and J is CR R or J is C(O) and E is CR R and the dotted line represents a single bond; or d) E and J are CR R and the dotted line represents a double bond. Compounds of formula I have activity against HIV WT and double mutant strains.

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