公开(公告)号：WO02081462A8

公开(公告)日：2004-05-27

申请号：PCT/US0111434

申请日：2001-04-06

Applicant: US GOV HEALTH & HUMAN SERV ,  KYOWA HAKKO KOGYO KK ,  SNADER KENNETH M ,  VISHNUVAJJALA B RAO ,  AKAMA TSUTOMU

Inventor： SNADER KENNETH M ,  VISHNUVAJJALA B RAO ,  AKAMA TSUTOMU

IPC: A61P35/00 ,  C07D311/30 ,  A61K31/35

CPC classification number: C07D311/30

Abstract: The invention provides an aminoflavone having formula (I), wherein each of R and R is H, COCH2-R , wherein R is amino, alkylamino, dialkylamino, or alkyl- or dialkylaminoalkyl, or an alpha -amino acid residue, provided that at least one of R or R is other than H, and R 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.

Abstract translation: 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。

公开(公告)号：WO2005040170A3

公开(公告)日：2005-06-30

申请号：PCT/US2004035050

申请日：2004-10-22

Applicant: US GOV HEALTH & HUMAN SERV ,  SPIROGEN LTD ,  STARKS ASS ,  MIDWEST RESEARCH INST ,  VISHNUVAJJALA B RAO ,  LIU PAUL S ,  SNADER KENNETH M ,  THURSTON DAVID ,  HOWARD PHILIP W ,  HSIAO LUKE Y ,  TURNER GREGORY

Inventor： VISHNUVAJJALA B RAO ,  LIU PAUL S ,  SNADER KENNETH M ,  THURSTON DAVID ,  HOWARD PHILIP W ,  TURNER GREGORY ,  HSIAO LUKE Y

IPC: C07D487/04 ,  A61K31/551 ,  A61P31/00

CPC classification number: C07D487/04

Abstract: Disclosed are compounds of Formula (I) wherein X, Y, R 1 -R 7 , T 1 , T 2 , 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.

Abstract translation: 公开了式（I）的化合物，其中X，Y，R 1 -R 7，T 1，T 2， SUP>，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。

公开(公告)号：WO2002058689A1

公开(公告)日：2002-08-01

申请号：PCT/US2001/046548

申请日：2001-12-05

Applicant: CHILDRENS HOSPITAL LOS ANGELES ,  GUPTA, Shanker ,  MAURER, Barry, James ,  REYNOLDS, C., Patrick ,  VISHNUVAJJALA, B., Rao

Inventor： GUPTA, Shanker ,  MAURER, Barry, James ,  REYNOLDS, C., Patrick ,  VISHNUVAJJALA, B., Rao

IPC: A61K31/16

CPC classification number: A61K31/16 ,  A61K9/107 ,  A61K9/1075 ,  A61K31/164 ,  A61K31/167 ,  A61K47/10 ,  A61K47/44 ,  Y10S514/937 ,  Y10S514/938 ,  Y10S514/975

Abstract: 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.

Abstract translation: 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，例如乙醇，与烷氧基化蓖麻油（例如ELEM）组合，或者在由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，稳定量的 非离子表面活性剂，任选的溶剂和任选的等渗剂。 此外，描述了用于治疗过度增殖性疾病如癌症的方法。

公开(公告)号：WO2005040170A2

公开(公告)日：2005-05-06

申请号：PCT/US2004/035050

申请日：2004-10-22

Applicant: GOVERNMENT OF THE UNITED STATES OF AMERICA, represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES ,  SPIROGEN, LTD. ,  STARKS ASSOCIATES, INC. ,  MIDWEST RESEARCH INSTITUTE ,  HSIAO, Luke, Y. ,  VISHNUVAJJALA, B., Rao ,  LIU, Paul, S. ,  SNADER, Kenneth, M. ,  THURSTON, David ,  HOWARD, Philip, W. ,  TURNER, Gregory

Inventor： VISHNUVAJJALA, B., Rao ,  LIU, Paul, S. ,  SNADER, Kenneth, M. ,  THURSTON, David ,  HOWARD, Philip, W. ,  TURNER, Gregory

IPC: C07D487/00

CPC classification number: C07D487/04

Abstract: Disclosed are compounds of Formula (I) wherein X, Y, R 1 -R 7 , T 1 , T 2 , 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.

Abstract translation: 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。

公开(公告)号：WO2002081462A1

公开(公告)日：2002-10-17

申请号：PCT/US2001/011434

申请日：2001-04-06

Applicant: THE GOVERNMENT OF THE UNITED STATES OF AMERICA, represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES ,  KYOWA HAKKO KOGYO CO., LTD. ,  SNADER, Kenneth, M. ,  VISHNUVAJJALA, B., Rao ,  AKAMA, Tsutomu

Inventor： SNADER, Kenneth, M. ,  VISHNUVAJJALA, B., Rao ,  AKAMA, Tsutomu

IPC: C07D311/30

CPC classification number: C07D311/30

Abstract: The invention provides an aminoflavone having formula (I), wherein each of R 1 and R 2 is H, COCH 2 -R 7 , wherein R 7 is amino, alkylamino, dialkylamino, or alkyl- or dialkylaminoalkyl, or an α-amino acid residue, provided that at least one of R 1 or R 2 is other than H, and R 3 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.

Abstract translation: 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。

公开(公告)号：WO2002079167A1

公开(公告)日：2002-10-10

申请号：PCT/US2002/010097

申请日：2002-03-28

Applicant: THE UNITED STATES OF AMERICA, REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES ,  SNADER, Kenneth, M. ,  VISHNUVAJJALA, B., Rao ,  HOLLINGSHEAD, Melinda, G. ,  SAUSVILLE, Edward, A.

Inventor： SNADER, Kenneth, M. ,  VISHNUVAJJALA, B., Rao ,  HOLLINGSHEAD, Melinda, G. ,  SAUSVILLE, Edward, A.

IPC: C07D225/06

CPC classification number: C07D225/06

Abstract: 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 administrering a geldanamycin derivative to a host in an amount sufficient to treat or prevent cancer.

Abstract translation: 表现出显着的初步体内活性，特别是显着的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，包括向宿主施用格尔德霉素衍生物 足以治疗或预防癌症的量。