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1. 发明申请

WO2012125746A9 TRICYCLIC GYRASE INHIBITORS 审中-公开
公开(公告)号：WO2012125746A9
公开(公告)日：2013-10-24
申请号：PCT/US2012029104
申请日：2012-03-14
申请人： TRIUS THERAPEUTICS INC , L LIVERMORE NAT SECURITY LLC , BENSEN DANIEL , FINN JOHN , LEE SUK JOONG , CHEN ZHIYONG , LAM THANH TO , LI XIAOMING , TRZOSS MICHAEL , JUNG MICHAEL , NGUYEN TOAN B , LIGHTSTONE FELICE , TARI LESLIE WILLIAM , ZHANG JUNHU , ARISTOFF PAUL , PHILLIPSON DOUGLAS W , WONG SERGIO E
发明人： BENSEN DANIEL , FINN JOHN , LEE SUK JOONG , CHEN ZHIYONG , LAM THANH TO , LI XIAOMING , TRZOSS MICHAEL , JUNG MICHAEL , NGUYEN TOAN B , LIGHTSTONE FELICE , TARI LESLIE WILLIAM , ZHANG JUNHU , ARISTOFF PAUL , PHILLIPSON DOUGLAS W , WONG SERGIO E
IPC分类号： C07D487/04 , A61K31/495 , A61P31/04 , C07D487/14
CPC分类号： C07D487/04 , C07D487/14
摘要： Disclosed herein are compounds having the structure of Formula I and pharmaceutically suitable salts, esters, and prodrugs thereof that are useful as antibacterially effective tricyclic gyrase inhibitors. Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.
摘要翻译：本文公开了具有式I结构的化合物及其药学上合适的盐，酯和前药，其可用作抗菌有效的三环类回旋酶抑制剂。还考虑了相关的药物组合物，用途和制备化合物的方法。

2. 发明申请

WO2007072153A8 CARBONYLAMINO PYRROLOPYRAZOLES, POTENT KINASE INHIBITORS 审中-公开
标题翻译：亚磷酸吡咯烷酮，磷酸激酶抑制剂
公开(公告)号：WO2007072153A8
公开(公告)日：2008-08-14
申请号：PCT/IB2006003646
申请日：2006-12-12
申请人： PFIZER PROD INC , DONG LIMING , GUO CHUANGXING , HONG YUFENG , JOHNSON MARY CATHERINE , KEPHART SUSAN ELIZABETH , LI HAITAO , MCALPINE INDRAWAN JAMES , TIKHE JAYASHREE GIRISH , YANG ANLE , ZHANG JUNHU
发明人： DONG LIMING , GUO CHUANGXING , HONG YUFENG , JOHNSON MARY CATHERINE , KEPHART SUSAN ELIZABETH , LI HAITAO , MCALPINE INDRAWAN JAMES , TIKHE JAYASHREE GIRISH , YANG ANLE , ZHANG JUNHU
IPC分类号： C07D487/04 , A61K31/4162 , A61P35/00
CPC分类号： C07D487/04
摘要： Carbonylamino Pyrrolopyrazole compounds of formula (I), compositions including these compounds and methods of their use are provided. Preferred compounds of formula (I) have activity as protein kinase inhibitors, including as inhibitors of PAK4.
摘要翻译：羰基氨基吡咯并吡唑式（I）化合物，包括这些化合物的组合物及其使用方法。优选的式（I）化合物具有作为蛋白激酶抑制剂的活性，包括作为PAK4的抑制剂。

3. 发明申请

WO2007072153A3 CARBONYLAMINO PYRROLOPYRAZOLES, POTENT KINASE INHIBITORS 审中-公开
标题翻译：亚磷酸吡咯烷酮，磷酸激酶抑制剂
公开(公告)号：WO2007072153A3
公开(公告)日：2007-10-25
申请号：PCT/IB2006003646
申请日：2006-12-12
申请人： PFIZER PROD INC , DONG LIMING , GUO CHANGXING , HONG YUFENG , JOHNSON MARY CATHERINE , KEPHART SUSAN ELIZABETH , LI HAITAO , MCALPINE INDRAWN JAMES , TIKHE JAYASHREE GIRISH , YANG ANLE , ZHANG JUNHU
发明人： DONG LIMING , GUO CHANGXING , HONG YUFENG , JOHNSON MARY CATHERINE , KEPHART SUSAN ELIZABETH , LI HAITAO , MCALPINE INDRAWN JAMES , TIKHE JAYASHREE GIRISH , YANG ANLE , ZHANG JUNHU
IPC分类号： C07D487/04 , A61K31/4162 , A61P35/00
CPC分类号： C07D487/04
摘要： Carbonylamino Pyrrolopyrazole compounds of formula (I), compositions including these compounds and methods of their use are provided. Preferred compounds of formula (I) have activity as protein kinase inhibitors, including as inhibitors of PAK4.
摘要翻译：羰基氨基吡咯并吡唑式（I）化合物，包括这些化合物的组合物及其使用方法。优选的式（I）化合物具有作为蛋白激酶抑制剂的活性，包括作为PAK4的抑制剂。

4. 发明申请

WO2006027694A1 INHIBITORS OF THE HIV INTEGRASE ENZYME 审中-公开
标题翻译： HIV整合酶抑制剂
公开(公告)号：WO2006027694A1
公开(公告)日：2006-03-16
申请号：PCT/IB2005/002967
申请日：2005-08-26
申请人： PFIZER INC. , DRESS, Klaus , KUEHLER, Jon, Edward , PLEWE, Michael, Bruno , YANG, Anle , ZHANG, Junhu
发明人： DRESS, Klaus , KUEHLER, Jon, Edward , PLEWE, Michael, Bruno , YANG, Anle , ZHANG, Junhu
IPC分类号： C07D471/04 , A61K31/437 , A61P31/18
CPC分类号： C07D471/04
摘要： The present invention relates to compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, pharmaceutical compositions comprisingm compounds of formula (I), and their methods of use in treating HIV-infected mammals.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐或溶剂合物，其包含式（I）化合物及其用于治疗HIV感染哺乳动物的方法的药物组合物。

5. 发明申请

WO2004039803A3 HIV-INTEGRASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS FOR THEIR USE 审中-公开
标题翻译： HIV-INTEGRASE INHIBITORS，PHARMACEUTICAL COMPOSITIONS及其使用方法
公开(公告)号：WO2004039803A3
公开(公告)日：2004-09-16
申请号：PCT/IB0304735
申请日：2003-10-27
申请人： PFIZER , HU QIYUE , KUKI ATSUO , NOWLIN DAWN MARIE , PLEWE MICHAEL BRUNO , WANG HAI , ZHANG JUNHU
发明人： HU QIYUE , KUKI ATSUO , NOWLIN DAWN MARIE , PLEWE MICHAEL BRUNO , WANG HAI , ZHANG JUNHU
IPC分类号： A61K31/435 , A61P31/18 , C07D471/04 , C07D471/12 , C07D471/14
CPC分类号： C07D471/04 , C07D471/12 , C07D471/14
摘要： Bicyclic hydroxamate compounds represented by the Formula I are described. The bicyclic hydroxamate compounds and compositions containing those compounds may be used to inhibit or modulate an enzyme activity of HIV Integrase and to treat HIV mediated diseases and conditions.
摘要翻译：描述由式I表示的双环氧肟酸盐化合物。双环异羟肟酸酯化合物和含有这些化合物的组合物可用于抑制或调节HIV整合酶的酶活性并治疗HIV介导的疾病和病症。

6. 发明申请

WO2004067531A1 HIV-INTEGRASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS FOR THEIR USE 审中-公开
标题翻译： HIV-INTEGRASE INHIBITORS，PHARMACEUTICAL COMPOSITIONS及其使用方法
公开(公告)号：WO2004067531A1
公开(公告)日：2004-08-12
申请号：PCT/IB2004/000259
申请日：2004-01-23
申请人： PFIZER INC. , KUKI, Atsuo , LI, Xinqiang , PLEWE, Michael, Bruno , WANG, Hai , ZHANG, Junhu
发明人： KUKI, Atsuo , LI, Xinqiang , PLEWE, Michael, Bruno , WANG, Hai , ZHANG, Junhu
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： Beta-carboline hydroxamic acid compounds represented by formula (I) and formula (lb) are described, wherein: R 1, R 2 , R 3 , R 4 , R 5 , and R 6 are independently selected from hydrogen, halogen, C 1 _C 6 alkyl, aikoxy C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, -OR c , -NO 2 , and -N(R c ) 2 , each R c is Independently selected from hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, and C 2 -C a alkynyl; R 7 Is C 1 -C 6 alkyl, C 2 -C 6 alkenyl, or C 2 -C 6 alkynyl, all of which are optionally substituted by one or more substituents independently selected from halogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl; C 2 -C 6 alkynyl, aryl, cycloalkyl, heterocycioalkyl, and heteroaryl, wherein said aryl, cydoalkyi, and heterocycloalkyl are optionally substituted with one or more substituents independently selected from halogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, and C 2 -C 6 alkynyl; R 8 and R 9 are independently selected from hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, and C 2 -C 6 aikynyl, wherein said alkyl, alkenyl, and alkynyl are optionally substituted with one or more substituents independently selected from halogen, aryl, cycloalkyl, heterocycloalkyl, and heteroaryl group, wherein said aryl, cycloalkyl, and heterocycloalkyl are optionally substituted with one or more substituents independently selected from halogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, and C 2 -C 6 alkynyl. The beta-carboline hydroxamic acid compounds and compositions containing those compounds may be used to inhibit or modulate the activity of HIV integrase enzyme and to treat HIV integrase-mediated diseases and conditions.
摘要翻译：描述了由式（I）和式（Ib）表示的β-咔啉异羟肟酸化合物，其中：R1，R2，R3，R4，R5和R6独立地选自氢，卤素，C1-C6烷基，烷氧基C1-C6烷基，C 2 -C 6烯基，C 2 -C 6炔基，-OR c，-NO 2和-N（R c）2，每个R c独立地选自氢，C 1 -C 6烷基，C 2 -C 6烯基和C 2 -C 5炔基; R 7是C 1 -C 6烷基，C 2 -C 6烯基或C 2 -C 6炔基，它们全部被一个或多个独立地选自卤素，C 1 -C 6烷基，C 2 -C 6烯基， C 2 -C 6炔基，芳基，环烷基，杂环烷基和杂芳基，其中所述芳基，环烷基和杂环烷基任选被一个或多个独立地选自卤素，C 1 -C 6烷基，C 2 -C 6烯基和C 2 -C 6炔基的取代基取代 ; R 8和R 9独立地选自氢，C 1 -C 6烷基，C 2 -C 6烯基和C 2 -C 6炔基，其中所述烷基，烯基和炔基任选地被一个或多个独立地选自卤素，芳基，环烷基，杂环烷基和杂芳基，其中所述芳基，环烷基和杂环烷基任选地被一个或多个独立地选自卤素，C 1 -C 6烷基，C 2 -C 6烯基和C 2 -C 6炔基的取代基取代。含有这些化合物的β-咔啉异羟肟酸化合物和组合物可用于抑制或调节HIV整合酶的活性并且用于治疗HIV整合酶介导的疾病和病症。

7. 发明申请

WO2012125746A1 TRICYCLIC GYRASE INHIBITORS 审中-公开
公开(公告)号：WO2012125746A1
公开(公告)日：2012-09-20
申请号：PCT/US2012/029104
申请日：2012-03-14
申请人： TRIUS THERAPEUTICS INC. , LAWRENCE LIVERMORE NATIONAL SECURITY, LLC , BENSEN, Daniel , FINN, John , LEE, Suk, Joong , CHEN, Zhiyong , LAM, Thanh, To , LI, Xiaoming , TRZOSS, Michael , JUNG, Michael , NGUYEN, Toan, B. , LIGHTSTONE, Felice , TARI, Leslie, William , ZHANG, Junhu , ARISTOFF, Paul , PHILLIPSON, Douglas, W. , WONG, Sergio, E.
发明人： BENSEN, Daniel , FINN, John , LEE, Suk, Joong , CHEN, Zhiyong , LAM, Thanh, To , LI, Xiaoming , TRZOSS, Michael , JUNG, Michael , NGUYEN, Toan, B. , LIGHTSTONE, Felice , TARI, Leslie, William , ZHANG, Junhu , ARISTOFF, Paul , PHILLIPSON, Douglas, W. , WONG, Sergio, E.
IPC分类号： C07D487/04 , C07D487/14 , A61K31/495 , A61P31/04
CPC分类号： C07D487/04 , C07D487/14
摘要： Disclosed herein are compounds having the structure of Formula I and pharmaceutically suitable salts, esters, and prodrugs thereof that are useful as antibacterially effective tricyclic gyrase inhibitors. Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.
摘要翻译：本文公开了具有式I结构的化合物及其药学上合适的盐，酯和前药，其可用作抗菌三环类回旋酶抑制剂。还考虑了相关的药物组合物，用途和制备化合物的方法。

8. 发明申请

WO2011032050A3 GYRASE INHIBITORS 审中-公开
标题翻译： GYRASE抑制剂
公开(公告)号：WO2011032050A3
公开(公告)日：2012-04-05
申请号：PCT/US2010048538
申请日：2010-09-10
申请人： TRIUS THERAPEUTICS INC , CREIGHTON CHRIS , TARI LES , CHEN ZHIYONG , HILGERS MARK , LAM THANH , LI XIAOMING , TRZOSS MICHAEL , ZHANG JUNHU , FINN JOHN , BENSEN DANIEL
发明人： CREIGHTON CHRIS , TARI LES , CHEN ZHIYONG , HILGERS MARK , LAM THANH , LI XIAOMING , TRZOSS MICHAEL , ZHANG JUNHU , FINN JOHN , BENSEN DANIEL
IPC分类号： C07D487/04 , A61K31/519 , A61P31/00 , A61P31/04 , C07D519/00
CPC分类号： C07D519/00 , C07D471/04 , C07D471/16 , C07D487/04 , C07D487/16 , C07D491/048 , C07D513/04
摘要： Novel gyrase inhibitors and related compositions and methods are useful for impeding bacterial growth. Compounds of Formula (I), are disclosed: Formula (I), wherein Y is N or CH; Z is N or CR5; R5 is H, a substituted or unsubstituted hydrocarbyl residue (1-3C) containing 0-2 heteroatoms selected from O, S and N, or is an inorganic residue; L is O, S, NR7, or CR8R9; R7 is H or C1-3 alkyl; R8 and R9 are each independently H or C1-3 alkyl; R2 is H, a hydrocarbyl residue (1-40C) containing 0-10 heteroatoms selected from O, S and N optionally substituted with an inorganic residue; R4 is H, an inorganic residue, or a hydrocarbyl residue (1-30C) containing 0- 12 heteroatoms selected from O, S and N and containing 0-10 inorganic residues, wherein R5 and R4 together may join to form a fused ring; and R6 is selected from the group consisting of H, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, halo C1-5 alkyl, halo C2-5 alkenyl, halo C2-5 alkynyl, C1-5 hydroxyalkyl, C1-5 alkyl chloride, C2-5 alkenyl chloride, and C2-5 alkynyl chloride; or a pharmaceutically-acceptable salt, ester, or prodrug thereof.
摘要翻译：新型促旋酶抑制剂和相关组合物和方法可用于阻止细菌生长。公开了式（I）的化合物：式（I），其中Y是N或CH; Z是N或CR5; R5是H，取代或未取代的含0-2个选自O，S和N的杂原子的烃基残基（1-3C），或是无机残基; L是O，S，NR7或CR8R9; R 7为H或C 1-3烷基; R 8和R 9各自独立地为H或C 1-3烷基; R2是H，含有0-10个选自O，S和N的杂原子的烃基残基（1-40℃），任选被无机残基取代; R4是H，无机残基，或含有0-12个选自O，S和N的杂原子且含有0-10个无机残基的烃基残基（1-30℃），其中R 5和R 4可以连接形成稠环; 并且R 6选自H，C 1-5烷基，C 2-5烯基，C 2-5炔基，卤代C 1-5烷基，卤素C 2-5烯基，卤代C 2-5炔基，C 1-5羟基烷基，C 1 -5烷基氯，C2-5烯基氯和C2-5炔基氯; 或其药学上可接受的盐，酯或前药。

9. 发明申请

WO2005103003A2 INHIBITORS OF THE HIV INTEGRASE ENZYME 审中-公开
标题翻译： HIV整合酶抑制剂
公开(公告)号：WO2005103003A2
公开(公告)日：2005-11-03
申请号：PCT/IB2005/001029
申请日：2005-04-14
申请人： PFIZER INC. , DRESS, Klaus, Ruprecht , HU, Qiyue , JOHNSON, Ted, William , PLEWE, Michael, Bruno , TANIS, Steven, Paul , WANG, Hai , YANG, Anle , YIN, Chunfeng , ZHANG, Junhu
发明人： DRESS, Klaus, Ruprecht , HU, Qiyue , JOHNSON, Ted, William , PLEWE, Michael, Bruno , TANIS, Steven, Paul , WANG, Hai , YANG, Anle , YIN, Chunfeng , ZHANG, Junhu
IPC分类号： C07D213/00
CPC分类号： C07D471/04
摘要： The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts and solvates thereof, their synthesis, and their use as modulators or inhibitors of the human immunodeficiency virus (“HIV”) integrase enzyme.
摘要翻译：本发明涉及式（I）化合物及其药学上可接受的盐和溶剂合物，它们的合成及其作为人免疫缺陷病毒（“HIV”）整合酶的调节剂或抑制剂的用途。

10. 发明申请

WO2011032050A2 GYRASE INHIBITORS 审中-公开
标题翻译： GYRASE抑制剂
公开(公告)号：WO2011032050A2
公开(公告)日：2011-03-17
申请号：PCT/US2010/048538
申请日：2010-09-10
申请人： TRIUS THERAPEUTICS, INC. , CREIGHTON, Chris , TARI, Les , CHEN, Zhiyong , HILGERS, Mark , LAM, Thanh , LI, Xiaoming , TRZOSS, Michael , ZHANG, Junhu , FINN, John
发明人： CREIGHTON, Chris , TARI, Les , CHEN, Zhiyong , HILGERS, Mark , LAM, Thanh , LI, Xiaoming , TRZOSS, Michael , ZHANG, Junhu , FINN, John
IPC分类号： C07D487/04 , C07D519/00 , A61K31/519 , A61P31/00
CPC分类号： C07D519/00 , C07D471/04 , C07D471/16 , C07D487/04 , C07D487/16 , C07D491/048 , C07D513/04
摘要： Novel gyrase inhibitors and related compositions and methods are useful for impeding bacterial growth. Compounds of Formula (I), are disclosed: Formula (I), wherein Y is N or CH; Z is N or CR 5 ; R 5 is H, a substituted or unsubstituted hydrocarbyl residue (1-3C) containing 0-2 heteroatoms selected from O, S and N, or is an inorganic residue; L is O, S, NR 7 , or CR 8 R 9 ; R 7 is H or C 1-3 alkyl; R 8 and R 9 are each independently H or C 1-3 alkyl; R 2 is H, a hydrocarbyl residue (1-40C) containing 0-10 heteroatoms selected from O, S and N optionally substituted with an inorganic residue; R 4 is H, an inorganic residue, or a hydrocarbyl residue (1-30C) containing 0- 12 heteroatoms selected from O, S and N and containing 0-10 inorganic residues, wherein R 5 and R 4 together may join to form a fused ring; and R 6 is selected from the group consisting of H, C 1-5 alkyl, C 2-5 alkenyl, C 2-5 alkynyl, halo C 1-5 alkyl, halo C 2-5 alkenyl, halo C 2-5 alkynyl, C 1-5 hydroxyalkyl, C 1-5 alkyl chloride, C 2-5 alkenyl chloride, and C 2-5 alkynyl chloride; or a pharmaceutically-acceptable salt, ester, or prodrug thereof.
摘要翻译：新型促旋酶抑制剂和相关组合物和方法可用于阻止细菌生长。公开了式（I）的化合物：式（I），其中Y是N或CH; Z为N或CR5; R5是H，含有0-2个选自O，S和N的杂原子的取代或未取代的烃基残基（1-3C），或是无机残基; L是O，S，NR7或CR8R9; R7是H或C1-3烷基; R 8和R 9各自独立地为H或C 1-3烷基; R2是H，含有0-10个选自O，S和N的杂原子的烃基残基（1-40℃），任选被无机残基取代; R4是H，无机残基，或含有0-12个选自O，S和N的杂原子并含有0-10个无机残基的烃基残基（1-30℃），其中R 5和R 4可以连接形成稠环; 并且R 6选自H，C 1-5烷基，C 2-5烯基，C 2-5炔基，卤代C 1-5烷基，卤素C 2-5烯基，卤代C 2-5炔基，C 1-5羟基烷基，C 1 -5烷基氯，C2-5烯基氯和C2-5炔基氯; 或其药学上可接受的盐，酯或前药。

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