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1. 发明申请

WO2003097644A3 NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS 审中-公开
公开(公告)号：WO2003097644A3
公开(公告)日：2003-11-27
申请号：PCT/CA2003/000718
申请日：2003-05-14
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , SIMONEAU, Bruno , LANDRY, Serge , MALENFANT, Éric , NAUD, Julie , O'MEARA, Jeffrey , THAVONEKHAM, Bounkham , YOAKIM, Christiane
发明人： SIMONEAU, Bruno , LANDRY, Serge , MALENFANT, Éric , NAUD, Julie , O'MEARA, Jeffrey , THAVONEKHAM, Bounkham , YOAKIM, Christiane
IPC分类号： C07D471/14
摘要： Compounds represented by formula (I), wherein R 2 is selected from the group consisting of H, (C 1-4 )alkyl, halo, haloalkyl, OH, (C 1-6 )alkoxy, NH(C 1-4 alkyl) or N(C 1-4 alkyl) 2 ; R 4 is H or Me; R 5 is H or Me; R 11 is H, (C 1-4 )alkyl, (C 3-4 )cycloalkyl and (C 1-4 )alkyl-(C 3-4 )cycloalkyl; A is a connecting chain of (C 1-3 )alkyl; B is O or S; n is 0 or 1; wherein when n is 0: Ring C is 6- or 10-membered aryl or 5- or 6-membered heterocycle having from 1 to 4 heteroatoms selected from the group consisting of O, N, and S, said aryl and said heterocycle being optionally substituted; and E is CONR 12 R 13 ; CONHNR 14 R 15 ; NR 16 COR 17 ; NR 18 SO 2 (C 1-6 )alkyl; SO 2 NR 19 R 20 ; or SO 2 R 21 ; or when n is 1: Ring C is as defined above and E is a single bond or a connecting group; and Ring D is 6- or 10-membered aryl or 5- or 6-membered heterocycle having from 1 to 4 heteroatoms selected from the group consisting of O, N, and S, said aryl and said heterocycle being optionally substituted with from 1 to 5 substituents; or a salt or a prodrug thereof are provided as inhibitors of HIV reverse transcriptase.

2. 发明申请

WO2003097644A2 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：WO2003097644A2
公开(公告)日：2003-11-27
申请号：PCT/CA2003/000718
申请日：2003-05-14
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , SIMONEAU, Bruno , LANDRY, Serge , MALENFANT, Éric , NAUD, Julie , O'MEARA, Jeffrey , THAVONEKHAM, Bounkham , YOAKIM, Christiane
发明人： SIMONEAU, Bruno , LANDRY, Serge , MALENFANT, Éric , NAUD, Julie , O'MEARA, Jeffrey , THAVONEKHAM, Bounkham , YOAKIM, Christiane
IPC分类号： C07D471/14
CPC分类号： C07D471/14
摘要： Compounds represented by formula (I), wherein R 2 is selected from the group consisting of H, (C 1-4 )alkyl, halo, haloalkyl, OH, (C 1-6 )alkoxy, NH(C 1-4 alkyl) or N(C 1-4 alkyl) 2 ; R 4 is H or Me; R 5 is H or Me; R 11 is H, (C 1-4 )alkyl, (C 3-4 )cycloalkyl and (C 1-4 )alkyl-(C 3-4 )cycloalkyl; A is a connecting chain of (C 1-3 )alkyl; B is O or S; n is 0 or 1; wherein when n is 0: Ring C is 6- or 10-membered aryl or 5- or 6-membered heterocycle having from 1 to 4 heteroatoms selected from the group consisting of O, N, and S, said aryl and said heterocycle being optionally substituted; and E is CONR 12 R 13 ; CONHNR 14 R 15 ; NR 16 COR 17 ; NR 18 SO 2 (C 1-6 )alkyl; SO 2 NR 19 R 20 ; or SO 2 R 21 ; or when n is 1: Ring C is as defined above and E is a single bond or a connecting group; and Ring D is 6- or 10-membered aryl or 5- or 6-membered heterocycle having from 1 to 4 heteroatoms selected from the group consisting of O, N, and S, said aryl and said heterocycle being optionally substituted with from 1 to 5 substituents; or a salt or a prodrug thereof are provided as inhibitors of HIV reverse transcriptase.
摘要翻译：由式（I）表示的化合物，其中R 2选自H，（C 1-4）烷基，卤素，卤代烷基，OH，（C 1-6）烷氧基，NH（C 1-4烷基）或N （C 1-4烷基）2; R 4是H或Me; R 5是H或Me; R 11是H，（C 1-4）烷基，（C 3-4）环烷基和（C 1-4）烷基 - （C 3-4）环烷基; A是（C 1-3）烷基的连接链; B是O或S; n为0或1; 其中当n为0时：环C为具有1至4个选自O，N和S的杂原子的6-元或10元芳基或5-或6-元杂环，所述芳基和所述杂环任选地取代; 并且E是CONR 12 R 13; CONHNR <14> - [R <15>; NR <16> COR <17>; NR <18> SO 2（C 1-6）烷基; SO 2 NR <19> - [R <20>; 或SO2R 21; 或当n为1时：环C如上定义，E为单键或连接基团; 环D是具有1至4个选自O，N和S的杂原子的6-或10-元芳基或5-或6-元杂环，所述芳基和所述杂环任选被1至 5个取代基; 或其盐或前药作为HIV逆转录酶的抑制剂。

3. 发明申请

WO2005118575A1 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：WO2005118575A1
公开(公告)日：2005-12-15
申请号：PCT/CA2005/000907
申请日：2005-05-30
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GmbH , BOEHRINGER INGELHEIM PHARMA GmbH & CO KG , DEROY, Patrick , FAUCHER, Anne-Marie , GAGNON, Alexandre , LANDRY, Serge , MORIN, Sébastien , O'MEARA, Jeffrey , SIMONEAU, Bruno , THAVONEKHAM, Bounkham , YOAKIM, Christiane
发明人： DEROY, Patrick , FAUCHER, Anne-Marie , GAGNON, Alexandre , LANDRY, Serge , MORIN, Sébastien , O'MEARA, Jeffrey , SIMONEAU, Bruno , THAVONEKHAM, Bounkham , YOAKIM, Christiane
IPC分类号： C07D403/12
CPC分类号： C07D257/04 , A61K31/41 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/495 , A61K31/5377 , A61K31/541 , C07D231/18 , C07D233/84 , C07D249/08 , C07D249/12 , C07D277/36 , C07D285/06 , C07D285/125 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12
摘要： The invention relates to compounds of formula (I) wherein Ar, X, R 1 , R 2 , R 3 and R 4 are as defined herein and pharmaceutical compositions thereof useful, either alone or in combination with other therapeutic agents as reverse transcriptase inhibitors against wild type and single or double mutant strains of HIV for the treatment or prophylaxis of HIV infection.
摘要翻译：本发明涉及其中Ar，X，R 1，R 2，R 3和R 4如本文所定义的式（I）化合物及其药物组合物，其单独使用或与作为用于治疗或预防HIV感染的针对野生型和单或双突变株的HIV的逆转录酶抑制剂的其它治疗剂。

4. 发明申请

WO2004050643A2 NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS 审中-公开
标题翻译：非核苷反义转录酶抑制剂
公开(公告)号：WO2004050643A2
公开(公告)日：2004-06-17
申请号：PCT/CA2003/001870
申请日：2003-12-01
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , SIMONEAU, Bruno , THAVONEKHAM, Bounkham , LANDRY, Serge , O'MEARA, Jeffrey , YOAKIM, Christiane , FAUCHER, Anne-Marie
发明人： SIMONEAU, Bruno , THAVONEKHAM, Bounkham , LANDRY, Serge , O'MEARA, Jeffrey , YOAKIM, Christiane , FAUCHER, Anne-Marie
IPC分类号： C07D257/00
CPC分类号： C07D257/04 , A61K31/167 , A61K31/41 , A61K31/4164 , A61K31/4178 , A61K31/4184 , A61K31/4192 , A61K31/4439 , C07D233/84 , C07D235/28 , C07D249/12 , C07D257/06 , C07D307/54 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要： Disclosed herein are compounds of formula Ar 1 -X-W-Ar 2 wherein Ar 1 and Ar 2 represent aryl groups characterized generally as aromatic heterocycles (e.g. imidazolyl or tetrazolyl) or carbocycles (e.g. phenyl or naphthalenyl); the aryl groups are optionally substituted or fused with other heterocycles or carbocycles; the aryl groups can bear substituents such as alkyl, halo or O-alkyl. X is a heteroatom, a valence bond or an optionally substituted divalent methylene, and W represents a spacer; typical spacers include divalent alkylene or alkylene-amido, -amido or -oxy radicals, which may optionally be substituted (e.g. hydroxyl or oxo). A typical compound is a derivative of 2-(N-napthalenyltetrazolylthio)- N-(2-nitrophenyl)acetamide. The compounds have inhibitory activity against Wild Type and single or double mutant strains of HIV.
摘要翻译：本文公开的是式Ar 1 -XW-Ar 2 2的化合物，其中Ar 1和Ar 2分别为氢， 2表示通常表征为芳族杂环（例如咪唑基或四唑基）或碳环（例如苯基或萘基）的芳基; 芳基任选被取代或与其它杂环或碳环稠合; 芳基可以带有取代基如烷基，卤素或O-烷基。 X是杂原子，价键或任选取代的二价亚甲基，并且W代表间隔基; 典型的间隔基包括可任选被取代的二价亚烷基或亚烷基 - 酰胺基， - 酰胺基或 - 氧基（例如羟基或氧代）。典型的化合物是2-（N-萘基四唑基硫基）-N-（2-硝基苯基）乙酰胺的衍生物。该化合物对野生型和HIV的单或双突变株具有抑制活性。

5. 发明申请

WO2006034583A1 ALKYNYL BASED DERVATIVES OF BENZOPHENONE AS NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS 审中-公开
标题翻译：苯丙酮碱作为非核苷酸逆转录酶抑制剂的基于碱基的催化剂
公开(公告)号：WO2006034583A1
公开(公告)日：2006-04-06
申请号：PCT/CA2005/001480
申请日：2005-09-27
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH & CO KG , BOEHRINGER INGELHEIM PHARMA GMBH & CO KG , BONNEAU, Pierre , DEROY, Patrick , GAGNON, Alexandre , O'MEARA, Jeffrey , SIMONEAU, Bruno , YOAKIM, Christiane
发明人： BONNEAU, Pierre , DEROY, Patrick , GAGNON, Alexandre , O'MEARA, Jeffrey , SIMONEAU, Bruno , YOAKIM, Christiane
IPC分类号： C07D307/33
CPC分类号： C07C235/24 , C07C235/84 , C07C237/10 , C07C237/24 , C07C255/56 , C07C2601/02 , C07C2601/04 , C07D205/04 , C07D207/10 , C07D207/16 , C07D211/62 , C07D213/75 , C07D213/81 , C07D213/82 , C07D213/89 , C07D295/088 , C07D295/15 , C07D295/32 , C07D307/33
摘要： Compounds of formula (I) wherein Q, R 1 , R 2 , R 3 , R 4 , R 6 and R 7 are as defined herein. The compounds are useful as reverse transcriptase inhibitors against HIV. In particular, the compounds are active against wild type and single or double mutant strains of HIV.
摘要翻译：其中Q，R 1，R 2，R 3，R 4，R 4，R 4，R 4， 6和7和R 7如本文所定义。这些化合物可用作抗HIV的逆转录酶抑制剂。特别地，这些化合物对HIV的野生型和单突变或双突变株具有活性。

6. 发明申请

WO2006012733A1 BENZOIC ACID DERIVATIVES AS NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS 审中-公开
标题翻译：作为非核苷酸逆转录酶抑制剂的苯甲酸衍生物
公开(公告)号：WO2006012733A1
公开(公告)日：2006-02-09
申请号：PCT/CA2005/001179
申请日：2005-07-28
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GmbH , BOEHRINGER INGELHEIM PHARMA GmbH & CO KG , SIMONEAU, Bruno , O'MEARA, Jeffrey , YOAKIM, Christiane
发明人： SIMONEAU, Bruno , O'MEARA, Jeffrey , YOAKIM, Christiane
IPC分类号： C07C255/57
CPC分类号： C07C235/68 , C07C235/24 , C07C255/56
摘要： Compounds of formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as defined herein. The compounds are useful as reverse transcriptase inhibitors against HIV. In particular, the compounds are active against wild type and single or double mutant strains of HIV.
摘要翻译：式（I）的化合物：其中R

7. 发明申请

WO2003080612A1 DIPYRIDODIAZEPINONES AS REVERSE TRANSCRIPTASE INHIBITORS 审中-公开
标题翻译： DIPYRIDODIAZEPINONES作为反向转录酶抑制剂
公开(公告)号：WO2003080612A1
公开(公告)日：2003-10-02
申请号：PCT/CA2003/000418
申请日：2003-03-24
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , O'MEARA, Jeffrey , SIMONEAU, Bruno , YOAKIM, Christiane , DÉZIEL, Robert , OGILVIE, William, W.
发明人： O'MEARA, Jeffrey , SIMONEAU, Bruno , YOAKIM, Christiane , DÉZIEL, Robert , OGILVIE, William, W.
IPC分类号： C07D471/14
CPC分类号： A61K31/55 , C07D471/14
摘要： Disclosed are compounds of formula I:whereinR2 is H, halogen, (C1-4)alkyl, O(C1-4)alkyl, NH(C1-4alkyl) or N(C1-4alkyl)2;R4 is H or CH3;R5 is H or CH3;R12 is H, halogen, (C1-4)alkyl, CF3, or NO2; R13 is H, (C1-4)alkyl, halogen, OH, or NH2, with the proviso that R12 and R13 are not both H; andR14 is COOR14a wherein R14a is H or (C1-6)alkyl; or R14 is (C2-4)alkenyl-COOR14a wherein R14a is as defined herein; or R14 is (C1-4)alkyl-COOR14a wherein R14a is as defined above;or a salt or a prodrug thereof, useful as inhibitors of HIV reverse transcriptase.
摘要翻译：公开了式I的化合物：其中R2是H，卤素，（C1-4）烷基，O（C1-4）烷基，NH（C1-4烷基）或N（C1-4烷基）2; R4是H或CH3; R5 是H或CH 3; R 12是H，卤素，（C 1-4）烷基，CF 3或NO 2; R 13是H，（C 1-4）烷基，卤素，OH或NH 2，条件是R 12和R 13不同时为H; R14是COOR14a，其中R14a是H或（C1-6）烷基; 或R 14为（C 2-4）烯基-COOR 14a，其中R 14a如本文所定义; 或R14是（C 1-4）烷基-COOR14a，其中R14a如上定义;或其盐或其前药，可用作HIV逆转录酶的抑制剂。

8. 发明申请

WO2010130034A1 INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION 审中-公开
标题翻译：人类免疫缺陷病毒复制的抑制剂
公开(公告)号：WO2010130034A1
公开(公告)日：2010-11-18
申请号：PCT/CA2010/000707
申请日：2010-05-13
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , YOAKIM, Christiane , BAILEY, Murray, D . , BILODEAU, Francois , CARSON, Rebekah, J . , FADER , Lee , KAWAI, Stephen , LAPLANTE, Steven , SIMONEAU, Bruno , SURPRENANT, Simon , THIBEAULT , Carl , TSANTRIZOS, Youla, S .
发明人： YOAKIM, Christiane , BAILEY, Murray, D . , BILODEAU, Francois , CARSON, Rebekah, J . , FADER , Lee , KAWAI, Stephen , LAPLANTE, Steven , SIMONEAU, Bruno , SURPRENANT, Simon , THIBEAULT , Carl , TSANTRIZOS, Youla, S .
IPC分类号： C07D213/55 , A61K31/44 , A61K31/5375 , A61K31/54 , A61P31/18 , C07D213/60 , C07D401/00 , C07D405/00 , C07D413/00 , C07D417/00 , C07D471/04 , C07D491/06 , C07D498/06
CPC分类号： C07D213/81 , A61K31/4375 , A61K31/44 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4709 , A61K31/4741 , A61K31/501 , A61K31/506 , A61K31/538 , A61K31/5383 , A61K45/06 , C07D213/55 , C07D401/12 , C07D405/10 , C07D405/14 , C07D411/10 , C07D413/10 , C07D413/14 , C07D417/10 , C07D471/04 , C07D491/06 , C07D498/06
摘要： Compounds of formula I wherein a, R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are defined herein, are useful as inhibitors of HIV replication.
摘要翻译：其中a，R 1，R 2，R 3，R 4，R 5和R 6在本文中定义的式I化合物可用作HIV复制的抑制剂。

9. 发明申请

WO2004026875A1 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：WO2004026875A1
公开(公告)日：2004-04-01
申请号：PCT/CA2003/001410
申请日：2003-09-15
申请人： BOEHRINGER INGELHEIM (CANADA) LTD. , YOAKIM, Christiane , O'MEARA, Jeffrey , SIMONEAU, Bruno , OGILVIE, William, W. , DÉZIEL, Robert
发明人： YOAKIM, Christiane , O'MEARA, Jeffrey , SIMONEAU, Bruno , OGILVIE, William, W. , DÉZIEL, Robert
IPC分类号： C07D471/22
CPC分类号： C07D471/22
摘要： Compounds represented by formula (1), wherein R 1 is H, halogen, (C 1-4 )alkyl, O(C 1-4 )alkyl, and haloalkyl; R 2 is H or methyl; R 3 is H or (C 1-4 )alkyl; R 4 is H or (C 1-4 )alkyl; R 5 is (C 1-4 )alkyl, (C 1-4 )alkyl(C 3-7 )cyclo-alkyl or (C 3-7 )cycloalkyl; and W is a fused phenyl-5 or 6-membered heterocycle having one or two heteroatoms selected from N or S; or W is phenyl, 1,1'-biphenyl, 2, 3-dihydro-1 H -indene, 1, 2, 3, 4-tetrahydronaphthyl, or naphthyl; said W being optionally substituted with (C 1-4 )alkyl, which in turn can be optionally substituted with a carboxy or (C 1-4 )alkoxycarbonyl, or a salt or ester thereof. The compounds have inhibitory activity against Wild Type, single and double mutant strains of HIV.
摘要翻译：由式（1）表示的化合物，其中R 1是H，卤素，（C 1-4）烷基，O（C 1-4）烷基和卤代烷基; R 2是H或甲基; R 3是H或（C 1-4）烷基; R 4是H或（C 1-4）烷基; R 5为（C 1-4）烷基，（C 1-4）烷基（C 3-7）环烷基或（C 3-7）环烷基; W是具有一个或两个选自N或S的杂原子的稠合苯基-5或6元杂环; 或W是苯基，1,1'-联苯基，2,3-二氢-1H-茚，1,2,3,4-四氢萘基或萘基; 所述W任选被（C 1-4）烷基取代，其又可任选地被羧基或（C 1-4）烷氧羰基或其盐或酯取代。该化合物对野生型，单突变和双突变株具有抑制活性。

10. 发明申请

WO2004085437A1 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：WO2004085437A1
公开(公告)日：2004-10-07
申请号：PCT/CA2003/001409
申请日：2003-09-15
申请人： BOEHRINGER INGELHEIM (CANADA) LTD. , YOAKIM, Christiane , MALENFANT, Eric , THAVONEKHAM, Bounkham , OGILVIE, William, W. , DEZIEL, Robert
发明人： YOAKIM, Christiane , MALENFANT, Eric , THAVONEKHAM, Bounkham , OGILVIE, William, W. , DEZIEL, Robert
IPC分类号： C07D471/14
CPC分类号： C07D471/14
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-Noxide 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.
摘要翻译：由式（I）表示的化合物：其中R 1是H，卤素，（C 1-4）烷基，O（C 1-4）烷基和卤代烷基; R 2是H或（C 1-4）烷基; R 3是H或（C 1-4）烷基; R 4是（C 1-4）烷基，（C 1-4）烷基（C 3-7）环烷基或（C 3-7）环烷基; 且Q为具有一至二个选自O和N的杂原子的稠合苯基-5或6元饱和杂环，所述Q任选被羟基取代，或（C 1-4）烷基，其又可任选被吡啶基 - 或C（O）OR，其中R是H或（C 1-4）烷基; 或其盐。该化合物对野生型具有抑制活性，并具有HIV和HIV的单和双突变株。

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