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公开(公告)号：US20070178574A1
公开(公告)日：2007-08-02
申请号：US11467135
申请日：2006-08-24
Applicant: Lydia Mosyak , Thomas Rush , Xiaotian Zhong , Thomas McDonagh , Katy Georgiadis , Phaik-Eng Sum , Edward LaVallie , Lisa Collins-Racie , Christopher Corcoran , Ravindra Kumar , Tracy Hebert , Stephane Olland , Stewart Mackie
Inventor： Lydia Mosyak , Thomas Rush , Xiaotian Zhong , Thomas McDonagh , Katy Georgiadis , Phaik-Eng Sum , Edward LaVallie , Lisa Collins-Racie , Christopher Corcoran , Ravindra Kumar , Tracy Hebert , Stephane Olland , Stewart Mackie
CPC classification number: C12N9/6421 , C07K2299/00 , C07K2319/00
Abstract: 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.
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公开(公告)号：US20050153944A1
公开(公告)日：2005-07-14
申请号：US11007621
申请日：2004-12-08
Applicant: Phaik-Eng Sum , David How , Darrin Hopper , Matthew Vera , Joshua Sabatini
Inventor： Phaik-Eng Sum , David How , Darrin Hopper , Matthew Vera , Joshua Sabatini
IPC: A61K31/423 , A61K31/65 , C07C237/26 , C07D263/52 , C07D413/04 , C07D413/06 , C07D417/04
CPC classification number: C07C237/26 , A61K31/65 , C07C2603/46 , C07D263/52 , C07D413/04 , C07D413/06 , C07D417/04
Abstract: This invention provides compounds of the formula: wherein A″, X and Y are defined in the specification. These compounds are useful as antibacterial agents.
Abstract translation: 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。
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3.发明授权Methods for inhibiting angiogenesis proliferation of endothelial or tumor cells and tumor growth 失效抑制内皮细胞和肿瘤细胞血管生成增殖的方法及肿瘤生长
公开(公告)号：US5574026A
公开(公告)日：1996-11-12
申请号：US355392
申请日：1994-12-13
Applicant: Joseph M. Backer , Peter Bohlen , Phaik-Eng Sum
Inventor： Joseph M. Backer , Peter Bohlen , Phaik-Eng Sum
IPC: A61K31/165 , A61K31/167 , A61K31/40 , A61K31/4453 , A61K31/65 , A61K31/025
CPC classification number: A61K31/4453 , A61K31/165 , A61K31/167 , A61K31/40
Abstract: The invention relates to a method for inhibiting angiogenesis and proliferation of endothelial cells by administering an inhibitory amount of a 7-halogen-9-[hydrogen or [(substituted glycyl)amido]]-6-demethyl-6-deoxytetracycline of Formula I: ##STR1## wherein X and W are as defined in the specification. The invention also relates to a method for inhibiting proliferation of tumor cells and tumor growth by administering an inhibitory amount of a compound of Formula I in combination with a chemotherapeutic agent or radiation therapy. The invention also relates to compositions containing an effective inhibitory amount of a compound of Formula I in a pharmaceutically acceptable carrier.
Abstract translation: 本发明涉及通过给予抑制量的式I的7-卤-9- [氢或[（取代的甘氨酰基）酰胺基]] - 脱甲基-6-脱氧四环素来抑制内皮细胞的血管生成和增殖的方法。 其中X和W如说明书中所定义。 本发明还涉及通过与化疗剂或放射治疗组合施用抑制量的式I化合物来抑制肿瘤细胞增殖和肿瘤生长的方法。 本发明还涉及在药学上可接受的载体中含有有效抑制量的式I化合物的组合物。
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4.发明授权Process for the production of 7-(substituted)-9-[(substituted glycyl)amido]-6-demethyl-6-deoxytetracyclines 失效制备7-（取代的）-9 - [（取代的甘氨酰）酰氨基] -6-脱甲基-6-脱氧四环素的方法
公开(公告)号：US5495031A
公开(公告)日：1996-02-27
申请号：US304913
申请日：1994-09-13
Applicant: Phaik-Eng Sum , Ving J. Lee , Raymond T. Testa
Inventor： Phaik-Eng Sum , Ving J. Lee , Raymond T. Testa
IPC: A61K31/16 , A61K31/40 , A61K31/403 , A61K31/425 , A61K31/428 , A61K31/65 , A61P31/04 , C07C20060101 , C07C231/12 , C07C237/26 , C07C255/50 , C07C255/52 , C07C317/28 , C07D207/16 , C07D209/02 , C07D211/14 , C07D211/22 , C07D211/26 , C07D213/36 , C07D213/38 , C07D233/56 , C07D233/64 , C07D237/26 , C07D249/04 , C07D249/08 , C07D261/08 , C07D265/30 , C07D277/64 , C07D293/00 , C07D295/12 , C07D295/13 , C07D295/14 , C07D295/15 , C07D295/22 , C07D295/30 , C07D307/32 , C07D207/18
CPC classification number: C07D295/30 , C07C237/26 , C07D207/16 , C07D213/38 , C07D295/13 , C07D295/15 , C07C2101/02 , C07C2103/46
Abstract: The invention provides a process for the production of compounds of the formula: ##STR1## wherein R, R.sup.3, R.sup.4 and W are defined in the specification in which a compound of the following formula: ##STR2## is reacted with a nucleophile of the formula WH in an inert atmosphere in the presence of a polar aprotic solvent. The resulting compounds are useful as antibiotics.
Abstract translation: 本发明提供了一种制备下式的化合物的方法：其中R，R 3，R 4和W在本说明书中定义，其中下式的化合物与下式的亲核试剂反应： WH在极性非质子溶剂存在下在惰性气氛中。 所得化合物可用作抗生素。
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5.发明授权7-(substituted)-9-[(substituted glycyl)amido]-6-demethyl-6-deoxytetracyclines 失效7-（取代的）-9 - [（取代的甘氨酰基）酰胺基] -6-脱甲基-6-脱氧四环素
公开(公告)号：US5466684A
公开(公告)日：1995-11-14
申请号：US304731
申请日：1994-09-12
Applicant: Phaik-Eng Sum , Ving J. Lee , Raymond T. Testa
Inventor： Phaik-Eng Sum , Ving J. Lee , Raymond T. Testa
IPC: A61K31/16 , A61K31/40 , A61K31/403 , A61K31/425 , A61K31/428 , A61K31/65 , A61P31/04 , C07C20060101 , C07C231/12 , C07C237/26 , C07C255/50 , C07C255/52 , C07C317/28 , C07D207/16 , C07D209/02 , C07D211/14 , C07D211/22 , C07D211/26 , C07D213/36 , C07D213/38 , C07D233/56 , C07D233/64 , C07D237/26 , C07D249/04 , C07D249/08 , C07D261/08 , C07D265/30 , C07D277/64 , C07D293/00 , C07D295/12 , C07D295/13 , C07D295/14 , C07D295/15 , C07D295/22 , C07D295/30 , C07D307/32
CPC classification number: C07D295/30 , C07C237/26 , C07D207/16 , C07D213/38 , C07D295/13 , C07D295/15 , C07C2101/02 , C07C2103/46
Abstract: The invention provides compounds of the formula: ##STR1## wherein R, R.sup.3, R.sup.4 and W are defined in the specification. These compounds are useful as antibiotic agents.
Abstract translation: 本发明提供下式的化合物：其中R，R 3，R 4和W在说明书中定义。 这些化合物可用作抗生素。
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Patent Agency Ranking6.发明授权
公开(公告)号：US5442059A
公开(公告)日：1995-08-15
申请号：US928590
申请日：1992-08-13
Applicant: Phaik-Eng Sum , Ving J. Lee , Raymond T. Testa
Inventor： Phaik-Eng Sum , Ving J. Lee , Raymond T. Testa
IPC: A61K31/65 , A61P31/00 , A61P31/04 , C07C20060101 , C07C237/26 , C07C239/18 , C07C239/20 , C07C255/50 , C07C271/22 , C07C323/29 , C07D207/06 , C07D207/14 , C07D207/16 , C07D207/30 , C07D209/02 , C07D211/14 , C07D211/56 , C07D213/40 , C07D213/74 , C07D221/22 , C07D231/12 , C07D231/14 , C07D241/04 , C07D241/14 , C07D249/02 , C07D249/04 , C07D249/08 , C07D265/28 , C07D279/04 , C07D295/14 , C07D295/15 , C07D295/215 , C07D295/24 , C07D307/33 , C07D333/20 , C07D333/36 , C07F15/00 , C07C231/12 , C07C233/64
CPC classification number: C07D213/40 , C07C237/26 , C07C239/18 , C07C239/20 , C07C271/22 , C07D295/15 , C07D295/215 , C07D295/24 , C07D333/20 , C07C2103/46
Abstract: The invention provides compounds of the formula: ##STR1## wherein R, and R.sup.1 and W are defined in the specification. These compounds are useful as antibiotic agents.
Abstract translation: 本发明提供下式的化合物：说明书。 这些化合物可用作抗生素。
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7.发明授权Certain hyrdoxy-phosphinyl-oxy-phenylmethyl-imidazolium hydroxide inner salts as PAF antagonists 失效某些羟基氧膦基 - 氧 - 苯甲基 - 咪唑鎓氢氧化物内盐作为PAF拮抗剂
公开(公告)号：US5411983A
公开(公告)日：1995-05-02
申请号：US099037
申请日：1993-07-28
Applicant: Allan Wissner , Robert E. Schaub , Phaik-Eng Sum
Inventor： Allan Wissner , Robert E. Schaub , Phaik-Eng Sum
IPC: C07C43/174 , C07C43/178 , C07C59/125 , C07C309/73 , C07D213/20 , C07D215/10 , C07D277/22 , C07D521/00 , C07F9/12 , C07F9/58 , C07F9/60 , C07F9/62 , C07F9/6509 , C07F9/6539 , A61K31/415 , C07F9/6506
CPC classification number: C07D213/20 , C07C309/73 , C07C43/1745 , C07C43/1785 , C07C59/125 , C07D215/10 , C07D231/12 , C07D233/56 , C07D249/08 , C07D277/22 , C07F9/12 , C07F9/581 , C07F9/60 , C07F9/62 , C07F9/650911 , C07F9/650958 , C07F9/6539
Abstract: The invention is a compound of R or S enantiomers or racemic mixtures of compounds of the formula: ##STR1## wherein: (A) X, Y, and R.sub.3 are as defined in the specification.
Abstract translation: 本发明是R或S对映体或如说明书中定义的下式化合物的外消旋混合物的化合物。
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公开(公告)号：US5326759A
公开(公告)日：1994-07-05
申请号：US146666
申请日：1993-11-01
Applicant: Joseph J. Hlavka , Phaik-Eng Sum , Yakov Gluzman , Ving J. Lee
Inventor： Joseph J. Hlavka , Phaik-Eng Sum , Yakov Gluzman , Ving J. Lee
IPC: A61K31/165 , A61K31/47 , A61K31/65 , A61P31/04 , C07C231/12 , C07C237/26 , C07D213/74 , C07D215/38 , C07D307/66 , C07D333/36 , A61K31/54 , A61K31/535 , C07D207/00 , C07D209/18 , C07D265/30
CPC classification number: C07C237/26 , C07C2103/46
Abstract: Novel 9-amino-7-(substituted amino)-6-demethyl-6-deoxytetracyclines having activity against a wide spectrum of organisms including organisms which are resistant to tetracyclines are disclosed. Also disclosed are intermediates and methods for making the novel compounds of the present invention.
Abstract translation: 公开了具有抗四环素抗性的生物体的广谱生物体的新型9-氨基-7-（取代氨基）-6-脱甲基-6-脱氧四环素。 还公开了制备本发明新化合物的中间体和方法。
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公开(公告)号：US08101590B2
公开(公告)日：2012-01-24
申请号：US11513972
申请日：2006-08-31
Applicant: Phaik-Eng Sum , Tarek Suhayl Mansour , David Brian How , Darrin William Hopper , Matthew Douglas Vera , Joshua James Sabatini , Jaechul Shim
Inventor： Phaik-Eng Sum , Tarek Suhayl Mansour , David Brian How , Darrin William Hopper , Matthew Douglas Vera , Joshua James Sabatini , Jaechul Shim
IPC: A61K31/65 , C07C237/26
CPC classification number: 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
Abstract: This invention provides compounds of Formula I having the structure where R1, R2, R3 and A are defined in the specification or a pharmaceutically acceptable salt thereof useful as antibacterial agents. Compounds according to Formula (II): where Q, R4, R5, R6 and R10 and A are defined in the specification are useful as chemical intermediates.
Abstract translation: 本发明提供式I化合物，其具有在说明书中定义R1，R2，R3和A的结构或其药学上可接受的盐作为抗菌剂。 根据式（II）的化合物：其中Q，R 4，R 5，R 6和R 10和A在说明书中定义可用作化学中间体。
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公开(公告)号：US07998965B2
公开(公告)日：2011-08-16
申请号：US12465840
申请日：2009-05-14
Applicant: Phaik-Eng Sum , Jerauld Stanley Skotnicki , Steve Yik-Kai Tam , Tarek Suhayl Mansour , David Brian How , Joshua James Sabatini , Jason Shaoyun Xiang , Eric Feyfant
Inventor： Phaik-Eng Sum , Jerauld Stanley Skotnicki , Steve Yik-Kai Tam , Tarek Suhayl Mansour , David Brian How , Joshua James Sabatini , Jason Shaoyun Xiang , Eric Feyfant
IPC: A61K31/4965 , A61K31/16 , A61K31/34 , A61K31/44 , A61K31/38 , C07C237/00 , C07D307/87 , C07D333/02 , C07D241/02
CPC classification number: 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
Abstract: The present invention relates to modulators of metalloproteinase activity.
Abstract translation: 本发明涉及金属蛋白酶活性的调节剂。
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