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2. 发明专利

TW201425314A 三環旋轉酶抑制劑审中-公开
简体标题：三环旋转酶抑制剂
公开(公告)号：TW201425314A
公开(公告)日：2014-07-01
申请号：TW102132841
申请日：2013-09-11
申请人：特留斯治療學有限公司 , TRIUS THERAPEUTICS INC. , 勞倫斯利弗莫爾國家安全有限公司 , LAWRENCE LIVERMORE NATIONAL SECURITY, LLC
发明人：班森丹尼爾 , BENSEN, DANIEL , 柏查德艾倫 , BORCHARDT, ALLEN , 陳志勇 , CHEN, ZHIYONG , 芬恩約翰M , FINN, JOHN M. , 萊姆坦圖 , LAM, THANH TO , 李錫中 , LEE, SUK JOONG , 李曉明 , LI, XIAOMING , 塔瑞雷斯利威廉 , TARI, LESLIE WILLIAM , 唐明 , TENG, MIN , 翠佐斯麥可 , TRZOSS, MICHAEL , 張君夫 , ZHANG, JUNHU , 君恩麥可E , JUNG, MICHAEL E. , 萊斯頓菲利斯C , LIGHTSTONE, FELICE C. , 汪恩西瑞格爾E , WONG, SERGIO E. , 奈吉彥圖恩B , NGUYEN, TOAN B.
IPC分类号： C07D487/04 , A61K31/519 , A61P31/04
CPC分类号： C07D519/00 , C07D487/04 , C07D487/16 , C07D487/22 , C07D498/22 , C07D515/22
摘要：本文揭示具有式I結構的化合物及其醫藥學上適合之鹽、酯及前藥，可用作抗細菌有效之三環旋轉酶抑制劑。另外，本文亦揭示三環旋轉酶抑制劑化合物之種類。亦涵蓋相關醫藥組合物、用途及製造該等化合物之方法。
简体摘要：本文揭示具有式I结构的化合物及其医药学上适合之盐、酯及前药，可用作抗细菌有效之三环旋转酶抑制剂。另外，本文亦揭示三环旋转酶抑制剂化合物之种类。亦涵盖相关医药组合物、用途及制造该等化合物之方法。

3. 发明申请

US20140057874A1 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：US20140057874A1
公开(公告)日：2014-02-27
申请号：US14068450
申请日：2013-10-31
申请人： TRIUS THERAPEUTICS, INC.
发明人： David Keith Hester, II , Robert J. Duguid , John Finn
IPC分类号： C07F9/6558
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 OR1 or NR1R2; wherein R1 and R2 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。

4. 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。

5. 发明申请

US20140206878A1 METHODS FOR PREPARING OXAZOLIDINONES AND COMPOSITIONS CONTAINING THEM 有权
标题翻译：制备含有它们的奥昔洛芬及其组合物的方法
公开(公告)号：US20140206878A1
公开(公告)日：2014-07-24
申请号：US14089050
申请日：2013-11-25
申请人： TRIUS THERAPEUTICS, INC.
发明人： Carrie A. Costello , Jacqueline A. Ware , Robert J. Duguid
IPC分类号： C07F5/02 , C07D401/04
CPC分类号： C07D401/04 , C07D403/10 , C07F5/025 , C07F9/65583
摘要： Methods of preparing a class of oxazolidinones useful to impede bacterial growth are disclosed.
摘要翻译：公开了制备一类可用于阻碍细菌生长的恶唑烷酮的方法。

6. 发明授权

US08461188B2 Therapeutic combination of daptomycin and protein synthesis inhibitor antibiotic, and methods of use 有权
标题翻译：达托霉素和蛋白质合成抑制剂抗生素的治疗组合及使用方法
公开(公告)号：US08461188B2
公开(公告)日：2013-06-11
申请号：US13655704
申请日：2012-10-19
申请人： Trius Therapeutics, Inc.
发明人： Kenneth F Bartizal , Jeffrey B Locke , Karen Joy Shaw , Philippe G Prokocimer
IPC分类号： A61K31/4439 , A61K38/12 , C07D413/14
CPC分类号： A61K31/4439 , A61K31/675 , A61K38/12 , A61K45/06 , C07D413/14 , C07F9/65583 , A61K2300/00
摘要： A therapeutic combination comprises an antibacterially effective amount of daptomycin, and an amount of protein synthesis inhibitor antibiotic effective to prevent the development of daptomycin non-susceptibility in bacteria. Related combination therapies and methods are also included.
摘要翻译：治疗组合包含抗菌有效量的达托霉素和一定量的蛋白质合成抑制剂抗生素，其有效地防止达托霉素在细菌中的非易感性发展。还包括相关组合疗法和方法。

7. 发明申请

WO2013059610A9 THERAPEUTIC COMBINATION OF DAPTOMYCIN AND PROTEIN SYNTHESIS INHIBITOR ANTIBIOTIC, AND METHODS OF USE 审中-公开
公开(公告)号：WO2013059610A9
公开(公告)日：2013-04-25
申请号：PCT/US2012/061048
申请日：2012-10-19
申请人： TRIUS THERAPEUTICS, INC.
发明人： BARTIZAL, Kenneth, F. , LOCKE, Jeffrey, B. , SHAW, Karen, Joy , PROKOCIMER, Philippe, G.
IPC分类号： A61K38/12 , A61K31/4439
摘要： A therapeutic combination comprises an antibacterially effective amount of daptomycin, and an amount of protein synthesis inhibitor antibiotic effective to prevent the development of daptomycin non-susceptibility in bacteria. Related combination therapies and methods are also included.

8. 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。

9. 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。

10. 发明申请

US20150246934A1 TRICYCLIC GYRASE INHIBITORS 审中-公开
公开(公告)号：US20150246934A1
公开(公告)日：2015-09-03
申请号：US14427611
申请日：2013-09-11
申请人： TRIUS THERAPEUTICS INC. , LAWRENCE LIVERMORE NATIONAL SECURITY, LLC
发明人： Daniel Bensen , Allen Borchardt , Zhiyong Chen , John M. Finn , Thanh To Lam , Suk Joong Lee , Xiaoming Li , Leslie William Tari , Min Teng , Michael Trzoss , Junhu Zhang , Michael E. Jung , Felice C. Lightstone , Sergio E. Wong , Toan B. Nguyen
IPC分类号： C07D519/00 , C07D487/04
CPC分类号： C07D519/00 , C07D487/04 , C07D487/16 , C07D487/22 , C07D498/22 , C07D515/22
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. In addition, species of tricyclic gyrase inhibitors compounds are also disclosed herein.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。此外，本文还公开了三环类回旋激酶抑制剂化合物的种类。还考虑了相关的药物组合物，用途和制备化合物的方法。

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