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

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.

3. 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.

4. 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.

5. 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.

6. 发明专利

AT231124T 未知
公开(公告)号：AT231124T
公开(公告)日：2003-02-15
申请号：AT98947257
申请日：1998-10-06
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： YOAKIM CHRISTIANE , CHABOT CATHERINE , DEZIEL ROBERT , KAWAI STEPHEN , OGILVIE WILLIAN W , O'MEARA JEFFREY
IPC分类号： A61K31/397 , A61K31/41 , A61K31/4178 , A61K31/423 , A61K31/428 , A61K31/437 , A61K31/4427 , A61K31/443 , A61K31/4523 , A61K31/506 , A61P31/22 , C07D205/08 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D413/12 , C07D417/12 , C07D513/04 , A61K31/395

7. 发明专利

DE69426337T2 未知
公开(公告)号：DE69426337T2
公开(公告)日：2001-05-31
申请号：DE69426337
申请日：1994-02-23
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： DEZIEL ROBERT , MOSS NEIL
IPC分类号： C12N9/99 , A61K31/52 , A61K31/70 , A61K38/00 , A61P31/12 , A61P31/22 , C07K1/02 , C07K5/103 , C07K7/06 , C07K14/035 , A61K38/07 , A61K38/08 , A61K7/48
摘要： Disclosed herein are peptide derivatives of the formula A-B-D-NHCH{CH2C(O)R }C(O)-NHCH{CR (R )-COOH}C(O)-E wherein A is a lower alkanoyl bearing two substituents, each substituent selected independently from phenyl or a monosubstituted phenyl wherein the monosubstituent is alkyl, halo, hydroxy or alkoxy; B is a N-methyl amino acid residue; D is an amino acid residue; R is alkyl, cycloalkyl, a monosubstituted amino or a disubstituted amino; R is hydrogen or alkyl and R is alkyl, or R and R are joined to form a cycloalkyl; and E is a terminal unit, for example, an alkylamino or a monovalent amino acid radical such as NHCH(alkyl)C(O)OH. The derivatives are useful for treating herpes infections.

8. 发明专利

ES2152269T3 未知
公开(公告)号：ES2152269T3
公开(公告)日：2001-02-01
申请号：ES94102680
申请日：1994-02-23
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： DEZIEL ROBERT , MOSS NEIL
IPC分类号： C12N9/99 , A61K31/52 , A61K31/70 , A61K38/00 , A61P31/12 , A61P31/22 , C07K1/02 , C07K5/103 , C07K7/06 , C07K14/035 , A61K38/07 , A61K38/08 , A61K7/48
摘要： Disclosed herein are peptide derivatives of the formula A-B-D-NHCH{CH2C(O)R }C(O)-NHCH{CR (R )-COOH}C(O)-E wherein A is a lower alkanoyl bearing two substituents, each substituent selected independently from phenyl or a monosubstituted phenyl wherein the monosubstituent is alkyl, halo, hydroxy or alkoxy; B is a N-methyl amino acid residue; D is an amino acid residue; R is alkyl, cycloalkyl, a monosubstituted amino or a disubstituted amino; R is hydrogen or alkyl and R is alkyl, or R and R are joined to form a cycloalkyl; and E is a terminal unit, for example, an alkylamino or a monovalent amino acid radical such as NHCH(alkyl)C(O)OH. The derivatives are useful for treating herpes infections.

9. 发明专利

DE69426337D1 未知
公开(公告)号：DE69426337D1
公开(公告)日：2001-01-04
申请号：DE69426337
申请日：1994-02-23
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： DEZIEL ROBERT , MOSS NEIL
IPC分类号： C12N9/99 , A61K31/52 , A61K31/70 , A61K38/00 , A61P31/12 , A61P31/22 , C07K1/02 , C07K5/103 , C07K7/06 , C07K14/035 , A61K38/07 , A61K38/08 , A61K7/48
摘要： Disclosed herein are peptide derivatives of the formula A-B-D-NHCH{CH2C(O)R }C(O)-NHCH{CR (R )-COOH}C(O)-E wherein A is a lower alkanoyl bearing two substituents, each substituent selected independently from phenyl or a monosubstituted phenyl wherein the monosubstituent is alkyl, halo, hydroxy or alkoxy; B is a N-methyl amino acid residue; D is an amino acid residue; R is alkyl, cycloalkyl, a monosubstituted amino or a disubstituted amino; R is hydrogen or alkyl and R is alkyl, or R and R are joined to form a cycloalkyl; and E is a terminal unit, for example, an alkylamino or a monovalent amino acid radical such as NHCH(alkyl)C(O)OH. The derivatives are useful for treating herpes infections.

10. 发明专利

DE69319266T2 未知
公开(公告)号：DE69319266T2
公开(公告)日：1998-11-26
申请号：DE69319266
申请日：1993-03-09
申请人： BOEHRINGER INGELHEIM CA LTD
发明人： DEZIEL ROBERT , MOSS NEIL , PLANTE RAYMOND
IPC分类号： A61K8/30 , A61K8/00 , A61K8/49 , A61K8/64 , A61K31/70 , A61K38/00 , A61K38/55 , A61P31/12 , A61P31/22 , C07K1/113 , C07K5/06 , C07K5/08 , C07K5/083 , C07K5/087 , C07K5/093 , C07K5/10 , C07K5/103 , C07K5/107 , A61K38/06 , A61K38/07

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