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1. 发明授权

US07511032B2 Pyrrolobenzodiazepine derivatives, compositions comprising the same and methods related thereto 失效
标题翻译：吡咯并苯并二氮杂衍生物，包含其的组合物及其相关方法
公开(公告)号：US07511032B2
公开(公告)日：2009-03-31
申请号：US10576689
申请日：2004-10-22
申请人： Paul S Liu , B. Rao Vishnuvajjala , Kenneth M Snader , David E Thurston , Philip W Howard , Luke Y Hsiao , Gregory Turner
发明人： Paul S Liu , B. Rao Vishnuvajjala , Kenneth M Snader , David E Thurston , Philip W Howard , Luke Y Hsiao , Gregory Turner
IPC分类号： C07D487/04 , A61K31/551 , A61P31/00
CPC分类号： C07D487/04
摘要： Disclosed are compounds of Formula (I) wherein X, Y, Ri-R7, T1, T2, Z, and p are as described herein; a pharmaceutical composition comprising a compound of Formula (I) and a carrier; a method of inhibiting growth of a cell, which method comprises administering in an amount effective to inhibit growth a compound of Formula (I); a method of treating cancer in a mammal, which method comprises administering in an amount effective to treat cancer a compound of Formula (I); a method of treating a viral, parasitic, or bacterial infection of a cell, which method comprises administering in an amount effective to treat a viral, parasitic, or bacterial infection a compound of Formula (I); and a method of preparing a compound of Formula (I) as described herein.
摘要翻译：公开了式（I）的化合物，其中X，Y，R 1 -R 7，T 1，T 2，Z和p如本文所述; 包含式（I）化合物和载体的药物组合物; 抑制细胞生长的方法，该方法包括以有效抑制生长的量施用式（I）化合物; 一种治疗哺乳动物癌症的方法，该方法包括以有效治疗癌症的量施用式（I）化合物; 治疗细胞的病毒，寄生或细菌感染的方法，所述方法包括以有效治疗病毒，寄生或细菌感染的量施用式（I）化合物; 和制备本文所述的式（I）化合物的方法。

2. 发明授权

US07169819B2 Pharmaceutical compositions of fenretinide having increased bioavailability and methods of using the same 有权
标题翻译：具有增加的生物利用度的芬维A胺的药物组合物及其使用方法
公开(公告)号：US07169819B2
公开(公告)日：2007-01-30
申请号：US10010914
申请日：2001-12-05
申请人： Shanker Gupta , Barry J. Maurer , C. Patrick Reynolds , B. Rao Vishnuvajjala
发明人： Shanker Gupta , Barry J. Maurer , C. Patrick Reynolds , B. Rao Vishnuvajjala
IPC分类号： A61K31/07 , A61K47/00 , A61P35/00
CPC分类号： A61K31/16 , A61K9/107 , A61K9/1075 , A61K31/164 , A61K31/167 , A61K47/10 , A61K47/44 , Y10S514/937 , Y10S514/938 , Y10S514/975
摘要： A pharmaceutical composition for parenteral delivery, comprising a retinide such as fenretinide in combination with a solvent capable of dispersing or solubilizing the retinide. The solvent comprises an alcohol, such as ethanol, in combination with an alkoxylated castor oil, such as CREMOPHOR® EL, or comprising a retinide, such as fenretinide, in an emulsion composed of a lipoid dispersed in an aqueous phase, a stabilizing amount of a non-ionic surfactant, optionally a solvent, and optionally an isotonic agent. In addition, a method of use in the treatment of hyperproliferative disorders, such as cancers is described.
摘要翻译：一种用于胃肠外递送的药物组合物，其包含视网膜如芬维A胺与能够分散或溶解视黄酸盐的溶剂的组合。溶剂包括醇，如乙醇，与烷氧基化蓖麻油（如ELEM）组合，或在分散在水相中的脂质组成的乳液中包含视黄酸盐，如芬维A胺，稳定剂非离子表面活性剂，任选的溶剂和任选的等渗剂的量。此外，描述了用于治疗过度增殖性疾病如癌症的方法。

3. 发明授权

US06890917B2 Geldanamycin derivative and method of treating cancer using same 有权
标题翻译：格尔德霉素衍生物和使用其治疗癌症的方法
公开(公告)号：US06890917B2
公开(公告)日：2005-05-10
申请号：US10432581
申请日：2002-03-28
申请人： Kenneth M. Snader , B. Rao Vishnuvajjala , Melinda G. Hollingshead , Edward A. Sausville
发明人： Kenneth M. Snader , B. Rao Vishnuvajjala , Melinda G. Hollingshead , Edward A. Sausville
IPC分类号： A61K31/395 , A61P35/00 , A61P43/00 , C07D225/06
CPC分类号： C07D225/06
摘要： A geldanamycin derivative exhibiting significant preliminary in vivo activity, particularly significant oral in vivo activity, and a method of treating or preventing cancer in a host comprising administering a geldanamycin derivative to a host in an amount sufficient to treat or prevent cancer.
摘要翻译：表现出明显的体内活性，特别是口服体内活性的格尔德霉素衍生物，以及治疗或预防宿主中的癌症的方法，包括以足以治疗或预防癌症的量向宿主施用格尔德霉素衍生物。

4. 发明授权

US07834005B2 Pyrrolobenzodiazepine derivatives, compositions comprising the same and methods related thereto 有权
标题翻译：吡咯并苯并二氮杂衍生物，包含其的组合物及其相关方法
公开(公告)号：US07834005B2
公开(公告)日：2010-11-16
申请号：US12370856
申请日：2009-02-13
申请人： Paul S. Liu , B. Rao Vishnuvajjala , Kenneth M. Snader , David E. Thurston , Philip W. Howard , Luke Y. Hsiao , Gregory Turner
发明人： Paul S. Liu , B. Rao Vishnuvajjala , Kenneth M. Snader , David E. Thurston , Philip W. Howard , Luke Y. Hsiao , Gregory Turner
IPC分类号： C07D487/04 , A61K31/551 , A61P31/00
CPC分类号： C07D487/04
摘要： Disclosed are compounds of Formula I wherein X, Y, R1-R7, T1, T2, Z, and p are as described herein; a pharmaceutical composition comprising a compound of Formula I and a carrier; a method of inhibiting growth of a cell, which method comprises administering in an amount effective to inhibit growth a compound of Formula I; a method of treating cancer in a mammal, which method comprises administering in an amount effective to treat cancer a compound of Formula I; a method of treating a viral, parasitic, or bacterial infection of a cell, which method comprises administering in an amount effective to treat a viral, parasitic, or bacterial infection a compound of Formula I; and a method of preparing a compound of Formula I as described herein.
摘要翻译：公开了式I的化合物，其中X，Y，R 1 -R 7，T 1，T 2，Z和p如本文所述; 包含式I化合物和载体的药物组合物; 一种抑制细胞生长的方法，该方法包括以有效抑制生长式I化合物的量给药; 一种治疗哺乳动物癌症的方法，该方法包括以有效治疗癌症的剂量施用式I化合物; 治疗细胞的病毒，寄生或细菌感染的方法，该方法包括以有效治疗式I化合物的病毒，寄生或细菌感染的量施用; 以及制备如本文所述的式I化合物的方法。

5. 发明授权

US06838090B2 Water-insoluble drug delivery system 失效
标题翻译：水不溶性药物输送系统
公开(公告)号：US06838090B2
公开(公告)日：2005-01-04
申请号：US10455295
申请日：2003-06-05
申请人： S. Esmail Tabibi , Emmanuel I. Ezennia , B. Rao Vishnuvajjala , Shanker Gupta
发明人： S. Esmail Tabibi , Emmanuel I. Ezennia , B. Rao Vishnuvajjala , Shanker Gupta
IPC分类号： A61K9/107 , A61K9/127 , A61K31/33 , A61K31/4192 , A61K31/4196 , A61K47/10 , A61K47/18 , A61K47/20
CPC分类号： A61K31/4196 , A61K9/0019 , A61K9/1075 , A61K9/127 , A61K9/1278 , A61K31/33 , A61K31/4192 , A61K47/10 , A61K47/18 , A61K47/20
摘要： The present invention provides a drug delivery system comprising a water-insoluble drug, a water-miscible organic solvent for the water-insoluble drug, a surfactant, and water, as well as a process for preparing the same. This invention further provides a pharmaceutical composition comprising a pharmaceutically acceptable carrier and such a drug delivery system. In addition, the present invention provides a method of delivering a drug to a host by administering to the host the drug delivery system of the present invention.
摘要翻译：本发明提供了包含水不溶性药物，水不溶性药物的水混溶性有机溶剂，表面活性剂和水的药物递送系统及其制备方法。本发明还提供了包含药学上可接受的载体和这种药物递送系统的药物组合物。此外，本发明提供了通过向宿主施用本发明的药物递送系统来向药物递送药物的方法。

6. 发明授权

US06812246B2 Aminoflavone compounds, compositions, and methods of use thereof 失效
标题翻译：氨基黄酮化合物，组合物及其使用方法
公开(公告)号：US06812246B2
公开(公告)日：2004-11-02
申请号：US10240883
申请日：2003-06-12
申请人： Kenneth M. Snader , B. Rao Vishnuvajjala , Tsutomu Akama
发明人： Kenneth M. Snader , B. Rao Vishnuvajjala , Tsutomu Akama
IPC分类号： A61K3135
CPC分类号： C07D311/30
摘要： The invention provides an aminoflavone having formula (I), wherein each of R1 and R2 is H, COCH2—R7, wherein R7 is amino alkylamino, dialkylamino, or alkyl- or dialkylaminoalkyl, or an &agr;-amino acid residue, provided that at least one of R1 or R2 is other than H, and R3 is H, branched or straight-chain alkyl, hydroxyalkyl, alkanoyloxyalkyl, alkanoyloxy, alkoxy, or alkoxyalkyl, or pharmaceutically acceptable salts thereof. The present invention also provides a pharmaceutical composition comprising an aminoflavone as described above, and a method of inhibiting the growth of a tumor in a host by administering a tumor growth-inhibiting amount of an aminoflavone compound having the formula as described above.
摘要翻译：本发明提供具有式（I）的氨基黄酮，其中R 1和R 2各自为H，COCH 2 -R 7，其中R 7为氨基烷基氨基，二烷基氨基或烷基 - 或二烷基氨基烷基，或α-氨基酸残基，条件是R 1或R 2中的至少一个不是H，R 3是H，支链或直链烷基，羟烷基，烷酰氧基烷基，烷酰氧基，烷氧基，或烷氧基烷基，或其药学上可接受的盐。本发明还提供了包含如上所述的氨基黄酮的药物组合物，以及通过施用具有抑制肿瘤生长抑制量的具有上述通式的氨基黄酮化合物来抑制宿主中肿瘤生长的方法。

7. 发明授权

US5696154A Brefeldin A derivatives and their utility in the treatment of cancer 失效
标题翻译： Brefeldin A衍生物及其在治疗癌症中的应用
公开(公告)号：US5696154A
公开(公告)日：1997-12-09
申请号：US267525
申请日：1994-06-29
申请人： Louis Malspeis , B. Rao Vishnuvajjala , Jeffrey G. Supko , Charles Theodore Kane, Jr.
发明人： Louis Malspeis , B. Rao Vishnuvajjala , Jeffrey G. Supko , Charles Theodore Kane, Jr.
IPC分类号： A61K31/365 , A61P35/02 , C07D313/00 , C07D405/12 , C07D413/12
CPC分类号： C07D313/00
摘要： Provided are brefeldin A derivatives of the formula: ##STR1## wherein one of R.sub.1 and R.sub.2 is H and the other of R.sub.1 and R.sub.2 is a substituent group having 1 to 12 carbon atoms containing a basic nitrogen atom or a quaternary ammonium group, or a salt thereof. These derivatives exhibit good antitumor activity, and are administrable to human patients without the problems associated with brefeldin A.
摘要翻译：本发明提供了下列式的布雷菲尔德A衍生物：其中R 1和R 2之一为H且R 1和R 2中的另一个为含有碱性氮原子或季铵基团的具有1至12个碳原子的取代基，或其盐。这些衍生物表现出良好的抗肿瘤活性，并且可以对人类患者施用，而没有与布雷菲德菌素A相关的问题。

8. 发明授权

US07244724B2 Pyrrolobenzodiazepines 有权
标题翻译：吡咯并苯并二氮杂卓
公开(公告)号：US07244724B2
公开(公告)日：2007-07-17
申请号：US11129207
申请日：2005-05-13
申请人： Paul S. Liu , B. Rao Vishnuvajjala , Kenneth M. Snader , David E. Thurston , Philip Howard , Stephen Gregson
发明人： Paul S. Liu , B. Rao Vishnuvajjala , Kenneth M. Snader , David E. Thurston , Philip Howard , Stephen Gregson
IPC分类号： C07D403/12 , A61K31/5517
CPC分类号： C07D487/04
摘要： A compound of formula I: or solvate thereof, wherein n is 1 to 10, and M and M′ are independently selected from monovalent pharmaceutically acceptable cations, or together represent a divalent pharmaceutically acceptable cation.
摘要翻译：式I化合物或其溶剂化物，其中n为1-10，M和M'独立地选自一价药学上可接受的阳离子，或一起代表二价药学上可接受的阳离子。

9. 发明授权

US5824674A Brefeldin A derivatives and their utility in the treatment of cancer 失效
标题翻译： Brefeldin A衍生物及其在治疗癌症中的应用
公开(公告)号：US5824674A
公开(公告)日：1998-10-20
申请号：US974902
申请日：1997-11-20
申请人： Louis Malspeis , B. Rao Vishnuvajjala , Jeffrey G. Supko , Charles Theodore Kane, Jr.
发明人： Louis Malspeis , B. Rao Vishnuvajjala , Jeffrey G. Supko , Charles Theodore Kane, Jr.
IPC分类号： A61K31/365 , A61P35/02 , C07D313/00 , A61K31/55
CPC分类号： C07D313/00
摘要： Provided are brefeldin A derivatives of the formula: ##STR1## wherein one of R.sub.1 and R.sub.2 is H and the other of R.sub.1 and R.sub.2 is a substituent group having 1 to 12 carbon atoms containing a basic nitrogen atom or a quaternary ammonium group, or a salt thereof. These derivatives exhibit good antitumor activity, and are administrable to human patients without the problems associated with brefeldin A.
摘要翻译：本发明提供了下列式的布雷菲尔德A衍生物：其中R 1和R 2之一为H且R 1和R 2中的另一个为含有碱性氮原子或季铵基团的具有1至12个碳原子的取代基，或其盐。这些衍生物表现出良好的抗肿瘤活性，并且可以对人类患者施用，而没有与布雷菲德菌素A相关的问题。

10. 发明申请

US20090149449A1 PYRROLOBENZODIAZEPINE DERIVATIVES, COMPOSITIONS COMPRISING THE SAME AND METHODS RELATED THERETO 有权
标题翻译：吡咯烷酮衍生物，包含该衍生物的组合物及其相关方法
公开(公告)号：US20090149449A1
公开(公告)日：2009-06-11
申请号：US12370856
申请日：2009-02-13
申请人： Paul S. Liu , B. Rao Vishnuvajjala , Kenneth M. Snader , David E. Thurston , Philip W. Howard , Luke Y. Hsiao , Gregory Turner
发明人： Paul S. Liu , B. Rao Vishnuvajjala , Kenneth M. Snader , David E. Thurston , Philip W. Howard , Luke Y. Hsiao , Gregory Turner
IPC分类号： A61K31/551 , C07D487/04 , C12N5/06 , A61P31/04
CPC分类号： C07D487/04
摘要： Disclosed are compounds of Formula I wherein X, Y, R1-R7, T1, T2, Z, and p are as described herein; a pharmaceutical composition comprising a compound of Formula I and a carrier; a method of inhibiting growth of a cell, which method comprises administering in an amount effective to inhibit growth a compound of Formula I; a method of treating cancer in a mammal, which method comprises administering in an amount effective to treat cancer a compound of Formula I; a method of treating a viral, parasitic, or bacterial infection of a cell, which method comprises administering in an amount effective to treat a viral, parasitic, or bacterial infection a compound of Formula I; and a method of preparing a compound of Formula I as described herein.
摘要翻译：公开了式I的化合物，其中X，Y，R 1 -R 7，T 1，T 2，Z和p如本文所述; 包含式I化合物和载体的药物组合物; 一种抑制细胞生长的方法，该方法包括以有效抑制生长式I化合物的量给药; 一种治疗哺乳动物癌症的方法，该方法包括以有效治疗癌症的剂量施用式I化合物; 治疗细胞的病毒，寄生或细菌感染的方法，该方法包括以有效治疗式I化合物的病毒，寄生或细菌感染的量施用; 以及制备如本文所述的式I化合物的方法。

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