公开(公告)号：EP1833978B1

公开(公告)日：2008-10-08

申请号：EP06717426.8

申请日：2006-01-04

申请人： TELIK, INC.

发明人： AURRECOECHEA, Natalia ,  KELSON, Andrew, B. ,  MACSATA, Robert, W. ,  ROBINSON, Louise ,  SANCHEZ, Anthony, J. ,  SANTIAGO, Nicholas, M. ,  SCHOW, Steven, R. ,  SIMON, Reyna, J.

IPC分类号： C12P21/02 ,  C07K5/08 ,  A61K38/06 ,  A61P31/00

CPC分类号： C07K5/0215 ,  A61K38/00

摘要： Tripeptide and tetrapeptide thioethers, pharmaceutical compositions containing them, their pharmaceutical use, and their preparation. The compounds are useful in potentiating the cytotoxic effects of chemotherapeutic agents in tumor cells, selectively exerting toxicity in tumor cells, elevating the production of GM progenitors in bone marrow, stimulating the differentiation of bone marrow, mitigating the myelosuppressive effects of chemotherapeutic agents, and modulating hematopoiesis in bone marrow.

公开(公告)号：EP1355698A2

公开(公告)日：2003-10-29

申请号：EP01980019.2

申请日：2001-10-10

申请人： TELIK, INC.

发明人： MANCHEM, Prasad V. V. S. V. ,  LUM, Robert, T. ,  SCHOW, Steven, R.

IPC分类号： A61P3/10 ,  A61P5/50 ,  A61K31/655 ,  A61K31/195 ,  A61K31/185

CPC分类号： A61K31/19 ,  A61K31/17 ,  A61K31/18 ,  A61K31/185 ,  A61K31/195 ,  A61K31/655

摘要： The present invention comprises the use of insulin receptor activating compounds, optionally in conjunction with insulin, for the treatment of HIV protease inhibitor-induced metabolic disorders. Any insulin receptor activating compounds is suitable for the practice of the invention. In addition, preferred compounds are disclosed. Methods of treating a person suffering from HIV protease inhibitor-induced metabolic disorders such as lipodystrophy, hypertriglyceridemia, insulin resistance, hyperglycemia, diabetes and ketoacidosis are also provided.

公开(公告)号：EP1278759B1

公开(公告)日：2005-12-21

申请号：EP01935025.5

申请日：2001-05-02

申请人： TELIK, INC.

发明人： HERR, Jason, R. ,  LUM, Robert, T. ,  SCHOW, Steven, R. ,  MENG, Fanying ,  KOZLOWSKI, Michael, R. ,  ZHICHKIN, Pavel

IPC分类号： C07F9/24 ,  A61K31/664 ,  A61P35/04

CPC分类号： C07F9/2458 ,  C07F9/2408

摘要： The present invention relates to chemical compounds, methods of treatment, pharmaceutical compositions, and processes for their preparation. The compounds possess anti-tumor activities or are capable of being modified to have anti-tumor activities, and therefore, this invention particularly relates to the use of the compounds in methods for the treatment of tumors and especially for the treatment of cancer, as well as to the processes for their preparation.

公开(公告)号：EP1278759A1

公开(公告)日：2003-01-29

申请号：EP01935025.5

申请日：2001-05-02

申请人： TELIK, INC.

发明人： HERR, Jason, R. ,  LUM, Robert, T. ,  SCHOW, Steven, R. ,  MENG, Fanying ,  KOZLOWSKI, Michael, R. ,  ZHICHKIN, Pavel

IPC分类号： C07F9/24 ,  A61K31/664 ,  A61P35/04

CPC分类号： C07F9/2458 ,  C07F9/2408

摘要： The present invention relates to chemical compounds, methods of treatment, pharmaceutical compositions, and processes for their preparation. The compounds possess anti-tumor activities or are capable of being modified to have anti-tumor activities, and therefore, this invention particularly relates to the use of the compounds in methods for the treatment of tumors and especially for the treatment of cancer, as well as to the processes for their preparation.

公开(公告)号：EP1200396A1

公开(公告)日：2002-05-02

申请号：EP00952351.5

申请日：2000-07-28

申请人： TELIK, INC.

发明人： SPEVAK, Wayne, R. ,  SONGYUAN, Shi ,  PRASAD, V., V., S., V., Manchem ,  KOZLOWSKI, Michael, R. ,  SCHOW, Steven, R. ,  LUM, Robert, T. ,  ROBINSON, Louise ,  PARK, Jeong, Weong

IPC分类号： C07C309/51 ,  C07C309/59 ,  C07D213/81 ,  C07D213/82 ,  C07D307/85 ,  C07C311/21 ,  C07C311/29 ,  C07C311/13 ,  C07C237/42 ,  A61K31/16 ,  A61K31/18 ,  A61K31/33

CPC分类号： C07D241/44 ,  C07C237/42 ,  C07C309/51 ,  C07C309/59 ,  C07C311/13 ,  C07C311/21 ,  C07C311/29 ,  C07D213/81 ,  C07D213/82 ,  C07D215/48 ,  C07D307/68 ,  C07D307/85

摘要： Methods for treating conditions associated with hyperglycemia, especially Type II diabetes, with novel naphthylsulfonic acids and related compounds are provided. Compounds of formula (1) where: R?1 and R2¿ are, independently, hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, R3 is a substituent on the B ring; and is -SO¿2OR?6, -C(O)OR6, -SO2NR62-C(O)NR62 or tetrazolyl; the linker -WY- between the naphthyl and phenyl intersects the A ring of the naphthyl and is, independently, -C(O)NR?7-, -NR7¿C(O)-, -C(O)O-, -OC(O)-, -CH=CH-, -NR7CH2-, -CH2NR?7-, -NR7C(O)NR7- -NR7¿C(O)O-, -OC(O)NR?7-, -NR7SO¿2O-, -OSO2NR7-, -OC(O)O-, -SO¿2?NR?7-, -NR7SO¿2-, -OSO2-, or -SO2O-; each R?6 and R7¿ is, independently, hydrogen or lower alkyl; optionally in the form of single stereoisomers or mixtures of stereoisomers, or the pharmaceutically acceptable salts thereof; are useful in methods of stimulating the kinase activity of the insulin receptor, enhancing the activation of the insulin receptor by insulin, and stimulating the uptake of glucose into cells. A variety of antidiabetic compounds and pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.

公开(公告)号：EP2576590A1

公开(公告)日：2013-04-10

申请号：EP11707986.3

申请日：2011-03-04

申请人： Telik, Inc.

发明人： PARENT, Stephan, D. ,  SCHOW, Steven, R.

IPC分类号： C07K5/02 ,  A61K38/06 ,  A61P35/00

CPC分类号： C07K5/0215 ,  A61K38/00

摘要： Crystalline ezatiostat hydrochloride ansolvate form D is more stable and/or more soluble than various solvated crystalline polymorphic forms of ezatiostat hydrochloride.

公开(公告)号：EP1791549A2

公开(公告)日：2007-06-06

申请号：EP05804834.9

申请日：2005-05-20

申请人： TELIK, INC.

发明人： ALLEN, David, R. ,  MA, Wenli ,  PETERSON, Brian, T. ,  ROBINSON, Louise ,  SCHOW, Steven, R. ,  SHI, Songyuan ,  SIMON, Reyna, J. ,  WEBER, Kevin, T. ,  WICK, Michael, M.

IPC分类号： A61K31/664

CPC分类号： C07F9/2458 ,  C07F9/2408 ,  C07F9/5721 ,  C07F9/581 ,  C07F9/582 ,  C07F9/591 ,  C07F9/598 ,  C07F9/650958 ,  C07F9/6533 ,  C07F9/65515 ,  C07F9/655345 ,  C07F9/65616

摘要： Sulfonylethyl and thioethyl phosphorodiamidates, their preparation and intermediates in their preparation, formulations containing them, and their pharmaceutical use. The compounds are useful for treating cancer, alone and in combination with other anticancer therapies.

公开(公告)号：EP2785689A1

公开(公告)日：2014-10-08

申请号：EP12853218.1

申请日：2012-11-30

申请人： Telik, Inc.

发明人： SCHOW, Steven, R.

IPC分类号： C07C321/20 ,  A61K31/19 ,  A61P35/00

CPC分类号： C07K5/06078 ,  A61K31/216 ,  C07B2200/07 ,  C07C323/60

摘要： Provided herein is an amorphous form of a pharmaceutically acceptable salt of ezatiostat, for example, ezatiostat hydrochloride, compositions, uses and methods of preparation thereof.

摘要翻译： 本文提供的是ezatiostat的药学上可接受的盐的无定形形式，例如ezatiostat盐酸盐，组合物，用途及其制备方法。

公开(公告)号：EP1833978A1

公开(公告)日：2007-09-19

申请号：EP06717426.8

申请日：2006-01-04

申请人： TELIK, INC.

发明人： AURRECOECHEA, Natalia ,  KELSON, Andrew, B. ,  MACSATA, Robert, W. ,  ROBINSON, Louise ,  SANCHEZ, Anthony, J. ,  SANTIAGO, Nicholas, M. ,  SCHOW, Steven, R. ,  SIMON, Reyna, J.

IPC分类号： C12P21/02 ,  C07K5/08 ,  A61K38/06 ,  A61P31/00

CPC分类号： C07K5/0215 ,  A61K38/00

摘要： Tripeptide and tetrapeptide thioethers, pharmaceutical compositions containing them, their pharmaceutical use, and their preparation. The compounds are useful in potentiating the cytotoxic effects of chemotherapeutic agents in tumor cells, selectively exerting toxicity in tumor cells, elevating the production of GM progenitors in bone marrow, stimulating the differentiation of bone marrow, mitigating the myelosuppressive effects of chemotherapeutic agents, and modulating hematopoiesis in bone marrow.

公开(公告)号：EP1562564A2

公开(公告)日：2005-08-17

申请号：EP03783388.6

申请日：2003-11-14

申请人： TELIK, INC.

发明人： XU, Hua ,  BROWN, Gail, L. ,  SCHOW, Steven, R. ,  KECK, James, G.

IPC分类号： A61K31/00

CPC分类号： A61K45/06 ,  A61K31/282 ,  A61K31/337 ,  A61K31/475 ,  A61K31/5377 ,  A61K31/70 ,  A61K38/05 ,  A61K2300/00

摘要： A method of combination cancer therapy in a mammal, especially a human, by administering a therapeutically effective amount of a GST-activated anticancer compound and a therapeutically effective dose of another anticancer therapy. Pharmaceutical compositions, products, and kits for the method. The use of a GST-activated anticancer compound in the manufacture of a medicament for the method. A method of potentiating an anticancer therapy in a mammal, especially a human, comprising administering a therapeutically effective amount of a GST-activated anticancer compound to the mammal being treated with the anticancer therapy. The use of a GST-activated anticancer compound in the manufacture of a medicament for the method. The GST-activated anticancer compound is preferably a compound of US Patent No. 5,556,942, and more preferably TLK286, especially as the hydrochloride salt.