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1. 发明申请

WO2008024922A2 8-HYDROXYQUINOLINE COMPOUNDS AND METHODS THEREOF 审中-公开
标题翻译： 8-羟基喹啉化合物及其方法
公开(公告)号：WO2008024922A2
公开(公告)日：2008-02-28
申请号：PCT/US2007/076661
申请日：2007-08-23
申请人： WYETH , BURSAVICH, Matthew, G. , LOMBARDI, Sabrina , GILBERT, Adam, M. , LAAKSO, Leif, Mark , KHAFIZOVA, Gulnaz , HOW, David, Brian , SABATINI, Joshua, James , SUM, Phaik-Eng , CLEMENS, Jeremy, J.
发明人： BURSAVICH, Matthew, G. , LOMBARDI, Sabrina , GILBERT, Adam, M. , LAAKSO, Leif, Mark , KHAFIZOVA, Gulnaz , HOW, David, Brian , SABATINI, Joshua, James , SUM, Phaik-Eng , CLEMENS, Jeremy, J.
IPC分类号： A61K31/4709
CPC分类号： C07D215/28 , C07D215/26 , C07D401/06 , C07D401/12 , C07D405/06 , C07D409/10 , C07D417/10
摘要： The present invention relates to 8-Hydroxyquinoline Compounds; compositions comprising an 8-Hydroxyquinoline Compound; and methods for treating or preventing a metalloproteinase-related disorder, such as, an arthritic disorder, osteoarthritis, malignant neoplasm, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, atherosclerosis, age-related macular degeneration, myocardial infarction, a corneal ulceration, an ocular surface disease, hepatitis, an aortic aneurysm, tendonitis, a central nervous system disorder, abnormal wound healing, angiogenesis, restenosis, cirrhosis, multiple sclerosis, glomerulonephritis, graft versus host disease, diabetes, an inflammatory bowel disease, shock, invertebral disc degeneration, stroke, osteopenia or a periodontal disease or comprising administering an effective dose of an 8-Hydroxyquinoline Compound to a mammal in need thereof.
摘要翻译：本发明涉及8-羟基喹啉化合物; 包含8-羟基喹啉化合物的组合物; 和治疗或预防与金属蛋白酶相关的病症例如关节炎病症，骨关节炎，恶性肿瘤，类风湿性关节炎，哮喘，慢性阻塞性肺病，动脉粥样硬化，年龄相关性黄斑变性，心肌梗塞，角膜溃疡，角膜溃疡眼球表面疾病，肝炎，主动脉瘤，腱炎，中枢神经系统疾病，伤口愈合异常，血管生成，再狭窄，肝硬化，多发性硬化症，肾小球肾炎，移植物抗宿主疾病，糖尿病，炎症性肠病，休克，椎间盘退变，中风，骨质减少或牙周病或包括将有效剂量的8-羟基喹啉化合物给予有需要的哺乳动物。

2. 发明申请

WO2007008994A2 GLUTAMATE AGGRECANASE INHIBITORS 审中-公开
标题翻译：谷氨酸AGGRECANASE抑制剂
公开(公告)号：WO2007008994A2
公开(公告)日：2007-01-18
申请号：PCT/US2006/027066
申请日：2006-07-11
申请人： WYETH , SUM, Phaik-Eng , HOW, David, Brian , SABATINI, Joshua, James , XIANG, Jason, Shaoyun , IPEK, Manus , FEYFANT, Eric
发明人： SUM, Phaik-Eng , HOW, David, Brian , SABATINI, Joshua, James , XIANG, Jason, Shaoyun , IPEK, Manus , FEYFANT, Eric
CPC分类号： C07D213/82 , C07B2200/07 , C07C231/16 , C07C233/83 , C07C235/84 , C07C237/22 , C07C237/42 , C07C259/06 , C07C323/32 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/08 , C07C2603/18 , C07C2603/74 , C07D213/38 , C07D239/26 , C07D239/42 , C07D277/30 , C07D307/52 , C07D307/68 , C07D307/79 , C07D307/85 , C07D317/58 , C07D333/20 , C07D333/22 , C07D333/28 , C07D333/38 , C07D409/04
摘要： The present invention relates to modulators of metalloproteinase activity.
摘要翻译：本发明涉及金属蛋白酶活性的调节剂。

3. 发明申请

WO2007027599A1 9-AMINOCARBONYLSUBSTITUTED DERIVATIVES OF GLYCYLCYCLINES 审中-公开
标题翻译：甘氨酸的9-氨基羰基衍生物衍生物
公开(公告)号：WO2007027599A1
公开(公告)日：2007-03-08
申请号：PCT/US2006/033516
申请日：2006-08-29
申请人： WYETH , SUM, Phaik-Eng , MANSOUR, Tarek, Suhayl , HOW, David, Brian , HOPPER, Darrin, William , VERA, Matthew, Douglas , SABATINI, Joshua, James , SHIM, Jaechul
发明人： SUM, Phaik-Eng , MANSOUR, Tarek, Suhayl , HOW, David, Brian , HOPPER, Darrin, William , VERA, Matthew, Douglas , SABATINI, Joshua, James , SHIM, Jaechul
IPC分类号： C07D237/26 , C07D209/42 , C07C271/22 , C07D333/38 , C07D213/80 , C07D215/48 , A61K31/165 , C07D319/06
CPC分类号： C07D333/38 , C07C237/26 , C07C271/22 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2603/46 , C07C2603/74 , C07D207/416 , C07D209/42 , C07D213/81 , C07D213/82 , C07D215/48 , C07D307/68 , C07D307/84 , C07D317/34
摘要： This invention provides compounds of Formula (I) having the structure where R 1 , R 2 , R 3 and A are defined in the specification or a pharmaceutically acceptable salt thereof useful as antibacterial agents. Compounds according to Formula (II): where Q, R 4 , R 5 , and R 6 and A are defined in the specification are useful as chemical intermediates.
摘要翻译：本发明提供了具有如下结构的式（I）化合物：其中R 1，R 2，R 3和A定义在说明书或其药学上可接受的盐可用作抗菌剂。根据式（II）的化合物：其中Q，R 4，R 5和R 6和A在本说明书中定义是有用的作为化学中间体。

4. 发明申请

WO2005061459A1 BIARYL SULFONAMIDES AND METHODS FOR USING SAME 审中-公开
标题翻译：二亚磺酸盐及其使用方法
公开(公告)号：WO2005061459A1
公开(公告)日：2005-07-07
申请号：PCT/US2003/041173
申请日：2003-12-22
申请人： WYETH , XIANG, Jason, Shaoyun , TAM, Steve, Yik-Kai , HU, Yonghan , SUM, Phaik-Eng , HOW, David, Brian , HOPPER, Darrin, William , VERA, Matthew, Douglas , SABATINI, Joshua, James , RUSH, Thomas, Saltmarsh, III , MORRIS, Elisabeth, Ann , GEORGIADIS, Katy, Evangelia
发明人： XIANG, Jason, Shaoyun , TAM, Steve, Yik-Kai , HU, Yonghan , SUM, Phaik-Eng , HOW, David, Brian , HOPPER, Darrin, William , VERA, Matthew, Douglas , SABATINI, Joshua, James , RUSH, Thomas, Saltmarsh, III , MORRIS, Elisabeth, Ann , GEORGIADIS, Katy, Evangelia
IPC分类号： C07D215/22
CPC分类号： C07D213/30 , A61K31/4188 , A61K31/424 , A61K31/429 , C07C311/29 , C07C311/46 , C07C2601/08 , C07C2602/10 , C07D213/64 , C07D213/643 , C07D215/14 , C07D215/227 , C07D215/233 , C07D217/18 , C07D235/12 , C07D239/34 , C07D239/60 , C07D261/14 , C07D263/22 , C07D263/58 , C07D277/64 , C07D277/68 , C07D295/096 , C07D295/192 , C07D307/79 , C07D307/80 , C07D307/82 , C07D307/84 , C07D319/18 , C07D321/10 , C07D333/20 , C07D333/36 , C07D333/66
摘要： The present invention relates to biaryl sulfonamides of the formula 1: wherein: R 1 is H or Cl-.C6 a]kyl; R 2 is H, C I -C6 alkyl, (CH 2 ) n R 2' , phenyl, or benzyl; n is 0-6; R 2' is aryl, heteroaryl, cycloalkyl, or heterocycloalkyl; R 3 is, independently with respect to each occurrence, H, halogen, OC(halogen) 3 ,C(halogen) 3 , alkoxy, or C I -C 6 alkyl; X is selected from CH 2 0, OCH 2 , C (R 3 )=(R 3 ) 2 -C(R 3 ) 2 , CH 2 NHC(=O), O(C=O)NH, O, C(=O)CH 2 , SO 2 CH 2 C(=O)NH, SO 2 NH, OC(=O), CH 2 S(O), and CH 2 S(O) 2 ; and Z is at least one aryl or heteroaryl moiety, and their use as for example metalloproteinase inhibitors.
摘要翻译：本发明涉及式1的联芳基磺酰胺：其中：R 1是H或C 1 -C 6 a] kyl; R 2是H，C 1 -C 6烷基，（CH 2）n R 2'，苯基或苄基; n为0-6; R 2是芳基，杂芳基，环烷基或杂环烷基; R 3各自独立地为H，卤素，OC（卤素）3，C（卤素）3，烷氧基或C 1 -C 6烷基; X选自CH 2 O，OCH 2，C（R 3）=（R 3）2 -C（R 3）2，CH 2 NHC（= O），O（C = O）NH，O，C （= O）CH 2，SO 2 CH 2 C（= O）NH，SO 2 NH，OC（= O），CH 2 S（O）和CH 2 S（O）并且Z是至少一个芳基或杂芳基部分，以及它们用于例如金属蛋白酶抑制剂。

5. 发明申请

WO2005056538A1 OXAZOLE DERIVATIVES OF TETRACYCLINES 审中-公开
标题翻译：四唑的氧杂衍生物
公开(公告)号：WO2005056538A1
公开(公告)日：2005-06-23
申请号：PCT/US2004/040850
申请日：2004-12-07
申请人： WYETH , SUM, Phaik-Eng , HOW, David, Brian , HOPPER, Darrin, William , VERA, Matthew, Douglas , SABATINI, Joshua, James
发明人： SUM, Phaik-Eng , HOW, David, Brian , HOPPER, Darrin, William , VERA, Matthew, Douglas , SABATINI, Joshua, James
IPC分类号： C07D263/52
CPC分类号： C07C237/26 , A61K31/65 , C07C2603/46 , C07D263/52 , C07D413/04 , C07D413/06 , C07D417/04
摘要： This invention provides compounds of the formula: wherein A", X and Y are defined in the specification. These compounds are useful as antibacterial agents.
摘要翻译：本发明提供下式的化合物：其中A“，X和Y在说明书中定义，这些化合物可用作抗菌剂。

6. 发明申请

WO2006130501A2 TIGECYCLINE AND METHODS OF PREPARING 9-NITROMINOCYCLINE 审中-公开
标题翻译：制备9-NITROMINOCYCLINE的TIGECYCLINE和方法
公开(公告)号：WO2006130501A2
公开(公告)日：2006-12-07
申请号：PCT/US2006/020540
申请日：2006-05-25
申请人： WYETH , KRISHNAN, Lalitha , SUM, Phaik-Eng , DAIGNEAULT, Sylvain , BERNATCHEZ, Michel , PILCHER, Anthony, Scott , HORNE, Jeffrey, Marshall , TUPER, Adam, Joseph , MCCAULEY, Joseph, James, III , MICHAUD, Adam, P.
发明人： KRISHNAN, Lalitha , SUM, Phaik-Eng , DAIGNEAULT, Sylvain , BERNATCHEZ, Michel , PILCHER, Anthony, Scott , HORNE, Jeffrey, Marshall , TUPER, Adam, Joseph , MCCAULEY, Joseph, James, III , MICHAUD, Adam, P.
IPC分类号： C07C231/02 , C07C237/26 , A61K31/65 , A61P31/00
CPC分类号： C07C231/02 , C07C237/26 , C07C2603/46
摘要： Methods of preparing and purifying tetracyclines, such as tigecycline, are disclosed. Also disclosed are tetracycline compositions, such as tigecycline compositions, prepared by these methods.
摘要翻译：公开了四环素如替加环素的制备和纯化方法。还公开了通过这些方法制备的四环素组合物，如替加环素组合物。

7. 发明申请

WO2006130431A1 METHODS OF PURIFYING TIGECYCLINE 审中-公开
标题翻译：净化TIGECYCLINE的方法
公开(公告)号：WO2006130431A1
公开(公告)日：2006-12-07
申请号：PCT/US2006/020270
申请日：2006-05-25
申请人： WYETH , KRISHNAN, Lalitha , SUM, Phaik-Eng , DAIGNEAULT, Sylvain , BERNATCHEZ, Michel , PILCHER, Anthony, Scott , HORNE, Jeffrey, Marshall , TUPER, Adam, Joseph , MCCAULEY, Joseph, James III , MICHAUD, Adam, P.
发明人： KRISHNAN, Lalitha , SUM, Phaik-Eng , DAIGNEAULT, Sylvain , BERNATCHEZ, Michel , PILCHER, Anthony, Scott , HORNE, Jeffrey, Marshall , TUPER, Adam, Joseph , MCCAULEY, Joseph, James III , MICHAUD, Adam, P.
IPC分类号： C07C231/24 , C07C237/26 , A61K31/65 , A61P31/00
CPC分类号： C07C231/24 , C07C2603/46 , C07C237/26
摘要： Methods of preparing and purifying tetracyclines, such as tigecycline, are disclosed. Also disclosed are tetracycline compositions, such as tigecycline compositions, prepared by these methods.
摘要翻译：公开了四环素如替加环素的制备和纯化方法。还公开了通过这些方法制备的四环素组合物，如替加环素组合物。

8. 发明申请

WO2006088720A2 9-SUBSTITUTED TETRACYCLINES 审中-公开
标题翻译： 9代替TETRACYCLINES
公开(公告)号：WO2006088720A2
公开(公告)日：2006-08-24
申请号：PCT/US2006/004562
申请日：2006-02-09
申请人： WYETH , SUM, Phaik-Eng , MANSOUR, Tarek
发明人： SUM, Phaik-Eng , MANSOUR, Tarek
IPC分类号： C07C237/26 , C07D265/06 , A61K31/65
CPC分类号： C07D265/02 , C07C237/26 , C07D267/02 , C07D409/12 , C07D413/12
摘要： This invention provides compounds of Formula (I); wherein: R 1 is a moiety selected from the group: (II) and (III) n is an integer of 1 or 2; R 2 is selected from hydrogen, amino, -NR 6 R 7 , alkyl of 1 to 12 carbon atoms optionally substituted, aryl of 6, 10 or 14 carbon atoms optionally substituted, alkenyl of 2 to 12 carbon atoms optionally substituted, alkynyl of 2 to 12 carbon atoms optionally substituted, halogen, and a 5 to 10 membered heteroaryl ring optionally substituted, having 1 to 4 heteroatoms independently selected from N, O and S; R 3 is selected from hydrogen, alkyl of 1 to 12 carbon atoms optionally substituted, aryl of 6, 10 or 14 carbon atoms optionally substituted, alkenyl of 2 to 12 carbon atoms optionally substituted, vinyl, alkynyl of 2 to 12 carbon atoms optionally substituted and halogen; R 4 is H, alkyl of 1 to 12 carbon atoms optionally substituted, cycloalkyl of 3 to 8 carbon atoms, bicycloalkyl of 5 to 10 carbon atoms or aralkyl optionally substituted; R 5 is OH or -OH 8 ; R 6 and R 7 are each independently H or alkyl of 1 to 12 carbon atoms or when optionally taken together with the nitrogen atom to which each is attached form a 3 to 8 membered saturated heterocyclyl ring; R 8 is alkyl of 1 to 12 carbon atoms optionally substituted; or a tautomer or pharmaceutically acceptable salts thereof.
摘要翻译：本发明提供式（I）化合物; 其中：R 1是选自以下的部分：（II）和（III）n是1或2的整数; R 2选自氢，氨基，-NR 6 R 7，任选取代的1至12个碳原子的烷基，6，任选取代的10或14个碳原子，任选取代的2至12个碳原子的烯基，任选取代的2至12个碳原子的炔基，卤素和任选取代的具有1至4个独立地选自N ，O和S; R 3选自氢，任选取代的1至12个碳原子的烷基，任选取代的6,10或14个碳原子的芳基，任选取代的2至12个碳原子的烯基，乙烯基， 2至12个碳原子任选取代和卤素; R 4是H，任选取代的1至12个碳原子的烷基，3至8个碳原子的环烷基，5至10个碳原子的双环烷基或任选取代的芳烷基; R 5是OH或-OH 8; R 6和R 7各自独立地为H或1至12个碳原子的烷基，或者当任选地与各自连接的氮原子一起形成3至8个元饱和杂环基; R 8是任选取代的1至12个碳原子的烷基; 或其互变异构体或其药学上可接受的盐。

9. 发明申请

WO2007025248A3 AGGRECANASE STRUCTURE 审中-公开
公开(公告)号：WO2007025248A3
公开(公告)日：2007-03-01
申请号：PCT/US2006/033498
申请日：2006-08-24
申请人： WYETH , MOSYAK, Lidia , RUSH III, Thomas Saltmarsh , ZHONG, Xiaotian , MCDONAGH, Thomas E. , GEORGIADIS, Katy E. , SUM, Phaik-Eng , LAVALLIE, Edward R. , COLLINS-RACIE, Lisa A. , CORCORAN, Christopher John , KUMAR, Ravindra , HEBERT, Tracy , OLLAND, Stephane Hubert , MACKIE, Stewart Andrews
发明人： MOSYAK, Lidia , RUSH III, Thomas Saltmarsh , ZHONG, Xiaotian , MCDONAGH, Thomas E. , GEORGIADIS, Katy E. , SUM, Phaik-Eng , LAVALLIE, Edward R. , COLLINS-RACIE, Lisa A. , CORCORAN, Christopher John , KUMAR, Ravindra , HEBERT, Tracy , OLLAND, Stephane Hubert , MACKIE, Stewart Andrews
IPC分类号： C12N9/64 , G06F19/00 , G01N23/20 , C30B7/00
摘要： This invention relates to aggrecanase polypeptides and aggrecanase polypeptide/ligand complexes, crystals of aggrecanase and aggrecanase polypeptide/ligand complexes, and related methods and software systems.

10. 发明申请

WO2006130418A1 TIGECYCLINE AND METHODS OF PREPARATION 审中-公开
标题翻译： TIGECYCLINE和制备方法
公开(公告)号：WO2006130418A1
公开(公告)日：2006-12-07
申请号：PCT/US2006/020229
申请日：2006-05-25
申请人： WYETH , KRISHNAN, Lalitha , SUM, Phaik-Eng , HORNE, Jeffrey, Marshall , TUPER, Adam, Joseph , MCCAULEY, Joseph, James, III , PILCHER, Anthony, Scott , MICHAUD, Adam, P. , DAIGNEAULT, Sylvain , BERNATCHEZ, Michel
发明人： KRISHNAN, Lalitha , SUM, Phaik-Eng , HORNE, Jeffrey, Marshall , TUPER, Adam, Joseph , MCCAULEY, Joseph, James, III , PILCHER, Anthony, Scott , MICHAUD, Adam, P. , DAIGNEAULT, Sylvain , BERNATCHEZ, Michel
IPC分类号： C07C231/02 , C07C237/26 , A61K31/65 , A61P31/00
CPC分类号： C07C237/26 , C07C231/02 , C07C2603/46
摘要： Methods of preparing and purifying tetracyclines, such as tigecycline, are disclosed. Also disclosed are tetracycline compositions, such as tigecycline compositions, prepared by these methods.
摘要翻译：公开了四环素如替加环素的制备和纯化方法。还公开了通过这些方法制备的四环素组合物，如替加环素组合物。

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