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1. 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。

2. 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。

3. 发明申请

WO2011153310A1 DIHYDROFOLATE REDUCTASE INHIBITORS 审中-公开
标题翻译：二氢叶酸还原酶抑制剂
公开(公告)号：WO2011153310A1
公开(公告)日：2011-12-08
申请号：PCT/US2011/038871
申请日：2011-06-02
申请人： TRIUS THERAPEUTICS , CHEN, Zhiyong , CREIGHTON, Chris , CUNNINGHAM, Mark , FINN, John , HILGERS, Mark , JUNG, Michael , KOHNEN, Lucy, Aguirre , LAM, Thanh , LI, Xiaoming , STIDHAM, Mark , TARI, Les , TRZOSS, Michael , ZHANG, Junhu
发明人： CHEN, Zhiyong , CREIGHTON, Chris , CUNNINGHAM, Mark , FINN, John , HILGERS, Mark , JUNG, Michael , KOHNEN, Lucy, Aguirre , LAM, Thanh , LI, Xiaoming , STIDHAM, Mark , TARI, Les , TRZOSS, Michael , ZHANG, Junhu
IPC分类号： A01N43/54 , C07D239/42 , C07D401/04
CPC分类号： C07D401/14 , C07D239/95 , C07D417/14
摘要： The present disclosure provides compounds of Formula I: (I) or a pharmaceutically acceptable salt thereof, wherein R 5 , R 6 and Z are as described herein. The disclosure also provides pharmaceutical compositions thereof; and methods for inhibiting DHFR activity; and methods for treating cell proliferative diseases, autoimmune disease, inflammatory disease or bacterial, fungal or parasitic infection by administering a compound of Formula I.
摘要翻译：本公开提供式I化合物：（I）或其药学上可接受的盐，其中R 5，R 6和Z如本文所述。本公开还提供其药物组合物; 和抑制DHFR活性的方法; 以及通过给予式I化合物治疗细胞增殖性疾病，自身免疫疾病，炎性疾病或细菌，真菌或寄生虫感染的方法。

4. 发明公开

EP2686320A1 TRICYCLIC GYRASE INHIBITORS 有权转让
标题翻译：三环旋转酶抑制剂
公开(公告)号：EP2686320A1
公开(公告)日：2014-01-22
申请号：EP12710633.4
申请日：2012-03-14
申请人： Trius Therapeutics, Inc. , Lawrence Livermore National Security, LLC
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： Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.

5. 发明申请

WO2010138649A1 OXAZOLIDINONE CONTAINING DIMER COMPOUNDS, COMPOSITIONS AND METHODS TO MAKE AND USE 审中-公开
标题翻译：含有二异氰酸酯的化合物，组合物和方法制备和使用
公开(公告)号：WO2010138649A1
公开(公告)日：2010-12-02
申请号：PCT/US2010/036283
申请日：2010-05-27
申请人： TRIUS THERAPEUTICS, INC. , HESTER, D., Keith , DUGUID, Robert, J. , FINN, John
发明人： HESTER, D., Keith , DUGUID, Robert, J. , FINN, John
IPC分类号： A61K31/675 , C07D413/14 , A61P31/04
CPC分类号： C07F9/65583 , A61K31/675
摘要： Dosage forms or pharmaceutical compositions comprise a compound having the structure of Formula (IV) wherein n is a non-negative integer; wherein each Z is an oxazolidinone-containing moiety having antibiotic activity in vivo upon cleaving, wherein M is independently OR 1 or NR 1 R 2 ; wherein R 1 and R 2 are independently selected from the group consisting of H, an optionally-substituted hydrocarbyl residue or a pharmaceutically acceptable cation; wherein the compound in the dosage form or a pharmaceutical composition is present in an amount effective for treating or preventing an antibacterial infection in a mammalian subject. Methods of preparing and using these dosage forms or pharmaceutical compositions are also disclosed.
摘要翻译：剂型或药物组合物包含具有式（IV）结构的化合物，其中n是非负整数; 其中每个Z是在裂解时在体内具有抗生素活性的含恶唑烷酮的部分，其中M独立地为OR 1或NR 1 R 2; 其中R1和R2独立地选自H，任选取代的烃基残基或药学上可接受的阳离子; 其中剂型中的化合物或药物组合物以有效治疗或预防哺乳动物受试者的抗菌感染的量存在。还公开了制备和使用这些剂型或药物组合物的方法。

6. 发明授权

EP2686320B1 TRICYCLIC GYRASE INHIBITORS 有权转让
标题翻译：三环旋转酶抑制剂
公开(公告)号：EP2686320B1
公开(公告)日：2016-05-18
申请号：EP12710633.4
申请日：2012-03-14
申请人： Merck Sharp & Dohme Corp. , Lawrence Livermore National Security, LLC
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： Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.

7. 发明公开

EP3044225A1 TRICYCLIC GYRASE INHIBITORS 审中-实审转让
标题翻译： TRICYCLIC GYRASE抑制剂
公开(公告)号：EP3044225A1
公开(公告)日：2016-07-20
申请号：EP14844214.8
申请日：2014-09-10
申请人： Merck Sharp & Dohme Corp. , Lawrence Livermore National Security, LLC
发明人： FINN, John , TARI, Leslie William , CHEN, Zhiyong , ZHANG, Junhu , PHILLIPSON, Douglas , LEE, Suk Joong , TRZOSS, Michael , BENSEN, Daniel , LI, Xiaoming , TENG, Min , ONG, Voon , BORCHARDT, Allen John , LAM, Thanh To , LIGHTSTONE, Felice, C. , WONG, Sergio, E. , NGUYEN, Toan, B.
IPC分类号： C07D487/04 , C07D487/16 , C07D487/22 , C07D515/22 , A61P31/04 , A61K31/519
CPC分类号： C07D487/04 , C07D491/147
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促旋酶抑制剂。也考虑了相关的药物组合物，用途以及制备这些化合物的方法。

8. 发明公开

EP2475666A2 GYRASE INHIBITORS 审中-公开
标题翻译： GYRASE抑制剂
公开(公告)号：EP2475666A2
公开(公告)日：2012-07-18
申请号：EP10760175.9
申请日：2010-09-10
申请人： Trius Therapeutics, Inc.
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 , 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）化合物：式（I），其中Y是N或CH; Z是N或CR 5; R 5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），或者是无机残基; L是O，S，NR 7或CR 8 R 9; R 7是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; R 2是H，含有0-10个选自O，S和N的杂原子的烃基残基（1-40C），其任选地被无机残基取代; R 4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（1-30C），其中R 5和R 4一起可以连接形成稠环且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，卤代C 2-5烯基，卤代C 2-5炔基，C 1-5羟烷基，C 1-5烷基氯，C 2-5链烯基氯和C 2-5炔基氯; 或其药学上可接受的盐，酯或前药。

9. 发明申请

WO2015038661A1 TRICYCLIC GYRASE INHIBITORS 审中-公开
公开(公告)号：WO2015038661A1
公开(公告)日：2015-03-19
申请号：PCT/US2014/055019
申请日：2014-09-10
申请人： TRIUS THERAPEUTICS, INC.
发明人： FINN, John , TARI, Leslie, William , CHEN, Zhiyong , ZHANG, Junhu , PHILLIPSON, Douglas , LEE, Suk, Joong , TRZOSS, Michael , BENSEN, Daniel , LI, Xiaoming , TENG, Min , ONG, Voon , BORCHARDT, Allen, John , LAM, Thanh, To
IPC分类号： C07D487/04 , C07D487/16 , C07D487/22 , C07D515/22 , A61P31/04 , A61K31/519
CPC分类号： C07D487/04 , C07D491/147
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。

10. 发明申请

WO2007014126A3 PARTIAL PRESSURE SWING ADSORPTION SYSTEM FOR PROVIDING HYDROGEN TO A VEHICLE FUEL CELL 审中-公开
公开(公告)号：WO2007014126A3
公开(公告)日：2007-02-01
申请号：PCT/US2006/028612
申请日：2006-07-24
申请人： BLOOM ENERGY CORPORATION , MCELROY, James , FINN, John , LEVAN, M., Douglas , VENKATARAMAN, Swaminathan , MITLITSKY, Fred
发明人： MCELROY, James , FINN, John , LEVAN, M., Douglas , VENKATARAMAN, Swaminathan , MITLITSKY, Fred
IPC分类号： B01D53/02
摘要： A method of operating a fuel cell system includes providing a fuel inlet stream into a fuel cell stack, operating the fuel cell stack to generate electricity and a hydrogen containing fuel exhaust stream, separating at least a portion of hydrogen contained in the fuel exhaust stream using partial pressure swing adsorption, and providing the hydrogen separated from the fuel exhaust stream to a hydrogen storage vessel or to a hydrogen using device.

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