公开(公告)号：EP0871441B1

公开(公告)日：2003-08-13

申请号：EP97910042.7

申请日：1997-10-03

申请人： Ilex Oncology, Inc.

发明人： WEIS, Alexander ,  LOVE, Richard ,  MANGOLD, Gina

IPC分类号： A61K31/335 ,  A61K31/195 ,  A61P35/00

CPC分类号： A61K31/198 ,  A61K31/335 ,  A61K2300/00

摘要： Preparations comprising a single enantiomer or defined ratio of enantiomers of alphadifluoromethylornithine (DFMO) are provided for treating, preventing, controlling the growth of and/or reducing the risk of developing estrogen independent breast cancer or tumor. The preparations containing a single DFMO enantiomer or defined nonracemic ratio of DFMO enantiomers will provide an enhanced pharmacological activity relative to a preparation comprising racemic DFMO. Methods for treating a patient having estrogen independent breast cancer, which methods comprise administering DFMO alone or in combination with taxol, are also provided.

公开(公告)号：EP0886519A1

公开(公告)日：1998-12-30

申请号：EP97946915

申请日：1997-10-31

申请人： ILEX ONCOLOGY INC

发明人： SHAKED ZE EV ,  MCGINITY JAMES

IPC分类号： A61K9/16 ,  A61K9/20 ,  A61K9/24 ,  A61K9/26 ,  A61K9/48 ,  A61K9/50 ,  A61K31/00 ,  A61K31/195 ,  A61K31/198 ,  A61P35/00

CPC分类号： A61K31/198 ,  A61K9/2081 ,  A61K9/209 ,  A61K9/5084

摘要： Preparations comprising a capsule, tablet or other dosage form containing a core of different types of DFMO are provided. These preparations are capable of providing for the direct and constant delivery of DFMO to the entire GI tract or just the colon and rectum. The DFMO-containing granules include granules specially formulated to achieve rapid DFMO release, and granules formulated to achieve slower DFMO release and/or granules formulated for gastric, enteric or colorectal release. Methods of using the preparations to flood the GI tract with relatively constant levels of DFMO may thus be provided. The ratio of the (+) to the (-)-enantiomeric forms of DFMO in the granules will be controlled so as to enhance the pharmacological profile and reduce toxicity of the preparation relative to racemic DFMO. Preparations and methods for achieving systemic delivery as well as direct colon delivery of DFMO are also described.

公开(公告)号：EP1412369B1

公开(公告)日：2008-05-07

申请号：EP02768391.1

申请日：2002-08-01

申请人： Ilex Oncology, Inc.

发明人： BAUTA, William, E. ,  SCHULMEIER, Brian, E. ,  CANTRELL, William, R., Jr. ,  LOVETT, Dennis ,  PUENTE, Jose

IPC分类号： C07H19/00

CPC分类号： C07H19/16

摘要： The present invention provides for the preparation β-adenine nucleosides by coupling an adenine derivative containing an unprotected exocyclic amino group at the C-6 position and a blocked arabinofuranosyl derivative, in the presence of a base and solvent. The present invention also provides for the stereoselective preparation of 2-deoxy-β-D-adenine nucleosides wherein a blocked 2-deoxy-β-D-arabinofuranosyl halide is coupled with the salt of an adenine derivative. The forgoing aspects of the present invention are utilized in the preparation of a clofarabine composition wherein the ratio of β to α-anomer is at least 99:1.

公开(公告)号：EP1455826A2

公开(公告)日：2004-09-15

申请号：EP02795976.6

申请日：2002-12-19

申请人： Ilex Oncology, Inc.

发明人： SHAKED, Ze'ev ,  BRYCE, Richard, P. ,  FONG, Sonny, B.

IPC分类号： A61K39/395 ,  A61K38/21 ,  A61K38/00

CPC分类号： A61K38/21 ,  A61K38/215 ,  A61K39/39541 ,  A61K2300/00

摘要： The present invention provides for the treatment of multiple sclerosis by combination therapies of CD52 specific antibodies, such as CAMPATH-1H, with either a Type 1 interferon or coploymer-1.

公开(公告)号：EP1412369A2

公开(公告)日：2004-04-28

申请号：EP02768391.1

申请日：2002-08-01

申请人： Ilex Oncology, Inc.

发明人： BAUTA, William, E. ,  SCHULMEIER, Brian, E. ,  CANTRELL, William, R., Jr. ,  LOVETT, Dennis ,  PUENTE, Jose

IPC分类号： C07H19/00

CPC分类号： C07H19/16

摘要： The present invention provides for the preparation β-adenine nucleosides by coupling an adenine derivative containing an unprotected exocyclic amino group at the C-6 position and a blocked arabinofuranosyl derivative, in the presence of a base and solvent. The present invention also provides for the stereoselective preparation of 2-deoxy-β-D-adenine nucleosides wherein a blocked 2-deoxy-β-D-arabinofuranosyl halide is coupled with the salt of an adenine derivative. The forgoing aspects of the present invention are utilized in the preparation of a clofarabine composition wherein the ratio of β to α-anomer is at least 99:1.

公开(公告)号：EP1363667A1

公开(公告)日：2003-11-26

申请号：EP01918607.1

申请日：2001-03-13

申请人： Ilex Oncology, Inc. ,  Mercian Corporation

发明人： REIMER, Corinne ,  KUFE, Donald, W. ,  AGATA, Naoki ,  TAKEUCHI, Tomio ,  ISHIZUKA, Masaaki ,  YOSHIOKA, Takeo ,  KUMAGAI, Hiroyuki ,  WEICHSELBAUM, Ralph, R.

IPC分类号： A61K41/00

CPC分类号： A61K41/0038

摘要： A method for enhancing the efficacy of chemotherapy and/or radiation in the treatment of cancer in animals, particularly humans, is provided wherein certain isocoumarin derivatives which exhibit unique radiosensitization activity and/or chemopotentiation properties are employed in a combination treatment with ionizing radiation and/or chemotherapy.

摘要翻译： 提供了用于增强化疗和/或放射治疗动物特别是人的癌症的功效的方法，其中某些表现出独特的放射增敏活性和/或化学增强性的异香豆素衍生物用于与电离辐射和/ 或化疗。

公开(公告)号：EP1261326A1

公开(公告)日：2002-12-04

申请号：EP01914781.8

申请日：2001-03-07

申请人： Ilex Oncology, Inc.

发明人： LEVENSON, Corey ,  SHAKED, Ze'ev

IPC分类号： A61K31/00

CPC分类号： A61K31/195 ,  Y10S977/773 ,  Y10S977/775 ,  Y10S977/905 ,  Y10S977/907

摘要： The present invention concerns a method for preventing and/or treating cancer in a patient comprising administering an effective amount of substantially purified D enantiomer of difluoromethylornithine (D-DFMO) or an analog of D-DFMO to the patient. D-DFMO or an analog thereof is administered at a dose of about 0.05 to about 20.0 gm/M2/day. D-DFMO or an analog thereof may be administered more than once for the treatment and/or prevention of cancer. Methods of administration as well as compositions and formulations of substantially purified D-DFMO and analogs of D-DFMO are described.

公开(公告)号：EP1178795A1

公开(公告)日：2002-02-13

申请号：EP00936033.0

申请日：2000-05-17

申请人： Ilex Oncology, Inc.

发明人： LOVE, Richard

IPC分类号： A61K31/415 ,  A61P35/00

CPC分类号： A61K45/06 ,  A61K31/198 ,  A61K31/415 ,  A61K31/195 ,  A61K2300/00

摘要： Celecoxib, a COX-2 specific non-steroidal anti-inflammatory agent, is provided in combination with DFMO for the prevention and/or treatment of cancers. Provided with the present invention are pharmaceutically acceptable compositions that include a non-steroidal anti-inflammatory agent, celecoxib, together with an effective amount of difluoromethylornithine.

公开(公告)号：EP1003715A1

公开(公告)日：2000-05-31

申请号：EP98918385.0

申请日：1998-04-21

申请人： UNIVERSITE LAVAL ,  Ilex Oncology, Inc.

发明人： POULIN, Richard ,  AUDETTE, Marie ,  CHAREST-GAUDREALT, René

IPC分类号： C07C237/10 ,  C07C211/14 ,  C07C323/41 ,  A61K31/16 ,  A61K31/13

CPC分类号： C07C211/14 ,  C07C211/27 ,  C07C237/10 ,  C07C323/41

摘要： The present invention describes the design, synthesis and therapeutic use of a variety of novel inhibitors of polyamine transport. The main feature of this class of transport inhibitors is to incorporate a linker or side chain that prevents the uptake of polyamines and helps to conjugate polyamine analogs to form dimers with high inhibitory potency against polyamine uptake. These new compounds incorporate features that are designed to maximize their chemical and metabolic stability and their ability to bind to the polyamine transporter, and to minimize their toxicity by preventing their absorption by the cells. The purpose of such inhibitors is to prevent the uptake or salvaging of circulating polyamines by rapidly proliferating cells such as tumor cells, in order to potentiate the effect of therapeutic inhibitors of polyamine biosynthesis such as alpha-difluoromethylornithene.

公开(公告)号：EP0871441A1

公开(公告)日：1998-10-21

申请号：EP97910042.0

申请日：1997-10-03

申请人： Ilex Oncology, Inc.

发明人： WEIS, Alexander ,  LOVE, Richard ,  MANGOLD, Gina

IPC分类号： A61K31

CPC分类号： A61K31/198 ,  A61K31/335 ,  A61K2300/00

摘要： Preparations comprising a single enantiomer or defined ratio of enantiomers of alphadifluoromethylornithine (DFMO) are provided for treating, preventing, controlling the growth of and/or reducing the risk of developing estrogen independent breast cancer or tumor. The preparations containing a single DFMO enantiomer or defined nonracemic ratio of DFMO enantiomers will provide an enhanced pharmacological activity relative to a preparation comprising racemic DFMO. Methods for treating a patient having estrogen independent breast cancer, which methods comprise administering DFMO alone or in combination with taxol, are also provided.