公开(公告)号：US20100063118A1

公开(公告)日：2010-03-11

申请号：US12501133

申请日：2009-07-10

申请人： Matthew W. Olson ,  Martin Di Grandi ,  Amarnauth Prashad

发明人： Matthew W. Olson ,  Martin Di Grandi ,  Amarnauth Prashad

IPC分类号： A61K31/4164 ,  C07D233/72 ,  C12N9/99 ,  A61P31/12 ,  A61P31/18 ,  A61P35/00 ,  C12Q1/68 ,  C07D471/10 ,  C07D471/04

CPC分类号： C07D233/76 ,  C07D471/10

摘要： The present invention relates to hydantoin derivatives having RNase H, polymerase and/or HIV reverse transcriptase modulatory, and particularly, inhibitory activity. Included in the invention are the hydantoin derivatives, compositions containing the derivatives, methods of synthesis of the derivatives, screening methods to identify the derivatives, and methods of treatment using the hydantoin derivatives, including the treatment of HIV, AIDS and retrovirus-associated cancer.

摘要翻译： 本发明涉及具有RNA酶H，聚合酶和/或HIV逆转录酶调节的乙内酰脲衍生物，特别是抑制活性。 本发明包括乙内酰脲衍生物，含有衍生物的组合物，衍生物的合成方法，鉴定衍生物的筛选方法以及使用乙内酰脲衍生物的治疗方法，包括治疗HIV，AIDS和逆转录病毒相关癌症。

公开(公告)号：US07553967B2

公开(公告)日：2009-06-30

申请号：US11076936

申请日：2005-03-11

申请人： Matthew Olson ,  Martin Di Grandi ,  Amarnauth Prashad

发明人： Matthew Olson ,  Martin Di Grandi ,  Amarnauth Prashad

IPC分类号： C07D215/38

CPC分类号： C07D215/48 ,  C07D215/08

摘要： The present invention is directed to compound of formula (A): wherein R1 is selected from (a) alkyl, alkenyl, alkynyl, cycloalkyl, aryl, and heteroaryl, or (b) CN and —C(NR10R11)═N—R12, R2 is selected from the group consisting of alkyl, alkenyl, alkynyl, cycloalkyl, aryl and heteroaryl, R3-R12 are as described within the specification, and A is O, NR9 or S, or a prodrug, a pharmaceutically acceptable salt or a pharmaceutically active metabolite thereof, provided that R1 is not alkyl when R2 is pyridine, provided that at least one of R3-R8 is not H or F when A is O, R1 is (b) and R2 is a phenyl ring, a phenyl ring substituted at the para position with halo, —CN, —OCH3, —CF3 or —CO2CH3, a quinoline or an ethylene substituted with a phenyl ring or a 3,4-methylenedioxyphenyl moiety, provided that R4 is not methyl when R3 and R5-R8 are H, A is O, R1 is (b) and R2 is 4-chlorophenyl, and provided that R6 is not Cl when R3-R5 and R7-R8 are H, R1 is CN and R2 is phenyl. This invention is also directed to methods of using the same for treating HIV infections, or AIDS, or preventing replication.

摘要翻译： 本发明涉及式（A）的化合物：其中R1选自（a）烷基，烯基，炔基，环烷基，芳基和杂芳基，或（b）CN和-C（NR10R11）-N-R12， R 2选自烷基，烯基，炔基，环烷基，芳基和杂芳基，R 3 -R 12如说明书中所述，A是O，NR 9或S，或前药，药学上可接受的盐或药学上可接受的盐 条件是当R 2为吡啶时R 1不为烷基，条件是当A为O时，R 3 -R 8中的至少一个不为H或F，R 1为（b）且R 2为苯环，苯环取代 在具有卤素的对位，-CN，-OCH 3，-CF 3或-CO 2 CH 3，喹啉或被苯环或3,4-亚甲二氧基苯基部分取代的亚乙基，条件是当R 3和R 5 -R 8 是H，A是O，R 1是（b），R 2是4-氯苯基，条件是当R 3 -R 5和R 7 -R 8是H时，R 6不是Cl，R 1是CN，R 2是苯基。 本发明还涉及使用该方法治疗HIV感染或AIDS或预防复制的方法。

公开(公告)号：US20070244140A1

公开(公告)日：2007-10-18

申请号：US11786380

申请日：2007-04-10

申请人： Yongbo Hu ,  Fuk-Wah Sum ,  Martin Di Grandi ,  Emily Norton

发明人： Yongbo Hu ,  Fuk-Wah Sum ,  Martin Di Grandi ,  Emily Norton

IPC分类号： A61K31/506 ,  C07D403/02 ,  A61K31/505 ,  C07D239/32

CPC分类号： C07D409/12 ,  C07D239/42 ,  C07D409/04 ,  C07D409/14

摘要： The present invention relates to compounds of formula III: wherein R2, R3, R5 and R6 are as defined herein.

摘要翻译： 本发明涉及式III化合物：其中R 2，R 3，R 5和R 6， 如本文所定义。

公开(公告)号：US07563905B2

公开(公告)日：2009-07-21

申请号：US11076960

申请日：2005-03-11

申请人： Matthew Olson ,  Martin Di Grandi

发明人： Matthew Olson ,  Martin Di Grandi

IPC分类号： C07D249/08

CPC分类号： C07D409/04 ,  C07D249/12 ,  C07D401/04 ,  C07D405/04

摘要： The present invention is directed to compounds of formula (I): wherein R1, R2 and R3 are independently selected from the group consisting of alkyl, alkenyl, alkynyl, cycloalkyl, aryl and heteroaryl and X1 and X2 are independently a bond or an linker group of 1 to 6 atoms and may be optional substituted or oxidized, or a prodrug, a pharmaceutically acceptable salt or a pharmaceutically active metabolite thereof. The invention is also directed to methods of using the same for treating HIV infections, or AIDs or preventing viral replication.

摘要翻译： 本发明涉及式（I）化合物：其中R 1，R 2和R 3独立地选自烷基，烯基，炔基，环烷基，芳基和杂芳基，X 1和X 2独立地是键或连接基团 1至6个原子，并且可以是任选的取代或氧化的，或其前药，药学上可接受的盐或其药物活性代谢物。 本发明还涉及使用该方法治疗HIV感染或AID或预防病毒复制的方法。

公开(公告)号：US20050203129A1

公开(公告)日：2005-09-15

申请号：US11076936

申请日：2005-03-11

申请人： Matthew Olson ,  Martin Di Grandi ,  Amarnauth Prashad

发明人： Matthew Olson ,  Martin Di Grandi ,  Amarnauth Prashad

IPC分类号： A61K31/4709 ,  C07D215/08 ,  C07D215/16 ,  C07D215/48

CPC分类号： C07D215/48 ,  C07D215/08

摘要： The present invention is directed to compound of formula (A): wherein R1 is selected from (a) alkyl, alkenyl, alkynyl, cycloalkyl, aryl, and heteroaryl, or (b) CN and —C(NR10R11)═N—R12, R2 is selected from the group consisting of alkyl, alkenyl, alkynyl, cycloalkyl, aryl and heteroaryl, R3-R12 are as described within the specification, and A is O, NR9 or S, or a prodrug, a pharmaceutically acceptable salt or a pharmaceutically active metabolite thereof, provided that R1 is not alkyl when R2 is pyridine, provided that at least one of R3-R8 is not H or F when A is O, R1 is (b) and R2 is a phenyl ring, a phenyl ring substituted at the para position with halo, —CN, —OCH3, —CF3 or —CO2CH3, a quinoline or an ethylene substituted with a phenyl ring or a 3,4-methylenedioxyphenyl moiety, provided that R4 is not methyl when R3 and R5-R8 are H, A is O, R1 is (b) and R2 is 4-chlorophenyl, and provided that R6 is not Cl when R3-R5 and R7-R8 are H, R1 is CN and R2 is phenyl. This invention is also directed to methods of using the same for treating HIV infections, or AIDS, or preventing replication.

摘要翻译： 本发明涉及式（A）的化合物：其中R 1选自（a）烷基，烯基，炔基，环烷基，芳基和杂芳基，或（b）CN和-C （NR 10 R 11） - NR 12，R 2选自烷基，烯基（C 1 -C 6） ，炔基，环烷基，芳基和杂芳基，R 3 -R 12如说明书中所述，A是O，NR 9或 S或其前药，药学上可接受的盐或其药学活性代谢物，条件是当R 2为吡啶时，R 1不为烷基，条件是至少一个 当A是O时，R 3 - R 8不是H或F，R 1是（b）和R 2， SUB>是苯环，在对位具有卤素，-CN，-OCH 3，-CF 3或-CO 2的苯环， 喹啉或被苯环或3,4-亚甲二氧基苯基部分取代的亚乙基，提供于 当R 3和R 5 -R 8为H时，R 4不为甲基，A为O， R 1是（b），R 2是4-氯苯基，并且条件是R 3不是Cl，当R 3' R 5和R 7 -R 8是H，R 1是CN，R 1是H， SUB> 2是苯基。 本发明还涉及使用该方法治疗HIV感染或AIDS或预防复制的方法。

公开(公告)号：US20050209287A1

公开(公告)日：2005-09-22

申请号：US11076960

申请日：2005-03-11

申请人： Matthew Olson ,  Martin Di Grandi

发明人： Matthew Olson ,  Martin Di Grandi

IPC分类号： A61K31/4196 ,  A61K31/4439 ,  C07D249/12 ,  C07D401/04 ,  C07D401/14 ,  C07D405/04 ,  C07D409/04 ,  C07D409/14 ,  C07D49/02

CPC分类号： C07D409/04 ,  C07D249/12 ,  C07D401/04 ,  C07D405/04

摘要： The present invention is directed to compounds of formula (I): wherein R1, R2 and R3 are independently selected from the group consisting of alkyl, alkenyl, alkynyl, cycloalkyl, aryl and heteroaryl and X1 and X2 are independently a bond or an linker group of 1 to 6 atoms and may be optional substituted or oxidized, or a prodrug, a pharmaceutically acceptable salt or a pharmaceutically active metabolite thereof. The invention is also directed to methods of using the same for treating HIV infections, or AIDs or preventing viral replication.

摘要翻译： 本发明涉及式（I）的化合物：其中R 1，R 2和R 3 3独立地选自 的烷基，烯基，炔基，环烷基，芳基和杂芳基，X 1和X 2独立地是1至6个原子的键或连接基团，并且可以是任选取代的 或氧化的，或其前药，药学上可接受的盐或其药物活性代谢物。 本发明还涉及使用该方法治疗HIV感染或AID或预防病毒复制的方法。