公开(公告)号：WO1998025603A1

公开(公告)日：1998-06-18

申请号：PCT/US1997023027

申请日：1997-12-12

Applicant: ILEX ONCOLOGY, INC. ,  WEIS, Alexander ,  SHAKED, Ze'ev

Inventor： ILEX ONCOLOGY, INC.

IPC: A61K31/195

CPC classification number: A61K31/198

Abstract: Preparations comprising a single enantiomer or defined non-racemic ratio of enantiomers of alpha-difluoromethylornithine (DFMO) are provided for treating, preventing, controlling the growth of and/or reducing the risk of cancers, tumors and other related neoplastic disorders. The preparations containing a substantially pure preparation of (-)-DFMO or a defined non-racemic ratio of DFMO enantiomers will provide an enhanced pharmacological activity relative to a preparation comprising racemic DFMO.

Abstract translation: 提供包含单一对映异构体或α-二氟甲基鸟氨酸（DFMO）的对映异构体的限定非外消旋比例的制剂用于治疗，预防，控制癌症，肿瘤和其他相关的肿瘤性疾病的风险和/或降低其风险。 包含（ - ） - DFMO或DFMO对映异构体的限定非外消旋比的基本上纯的制剂的制剂相对于包含外消旋DFMO的制剂将提供增强的药理学活性。

公开(公告)号：WO1998019667A1

公开(公告)日：1998-05-14

申请号：PCT/US1997020424

申请日：1997-10-31

Applicant: ILEX ONCOLOGY, INC. ,  WEIS, Alexander ,  MCGINITY, James

Inventor： ILEX ONCOLOGY, INC.

IPC: A61K09/20

CPC classification number: A61K31/198 ,  A61K9/2081 ,  A61K9/209 ,  A61K9/5084

Abstract: 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.

Abstract translation: 提供了包含含有不同类型DFMO的核心的胶囊，片剂或其它剂型的制剂。 这些制剂能够提供直接和持续的DFMO输送到整个胃肠道或只是结肠和直肠。 含有DFMO的颗粒包括特殊配制以实现快速DFMO释放的颗粒，以及配制用于实现慢性DFMO释放和/或配制用于胃肠，肠或结肠直肠释放的颗粒的颗粒。 因此可以提供使用制剂以相对恒定水平的DFMO来淹没胃肠道的方法。 将控制颗粒中DFMO的（+）与（ - ） - 对映体形式的比例，以增强制剂相对于外消旋DFMO的药理学特性和降低毒性。 还描述了用于实现系统递送以及DFMO的直接结肠递送的制备和方法。

公开(公告)号：WO1998014188A1

公开(公告)日：1998-04-09

申请号：PCT/US1997018252

申请日：1997-10-03

Applicant: ILEX ONCOLOGY, INC. ,  WEIS, Alexander ,  LOVE, Richard ,  MANGOLD, Gina

Inventor： ILEX ONCOLOGY, INC.

IPC: A61K31/335

CPC classification number: A61K31/198 ,  A61K31/335 ,  A61K2300/00

Abstract: 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.

Abstract translation: 提供了包含单一对映异构体或定义比例的对甲氧基甲基鸟氨酸（DFMO）的制剂，用于治疗，预防和/或降低发展与雌激素无关的乳腺癌或肿瘤的风险。 含有单一DFMO对映异构体或DFMO对映异构体定义的非微量比的制剂相对于包含外消旋DFMO的制剂将提供增强的药理学活性。 还提供了治疗患有雌激素不依赖性乳腺癌的患者的方法，该方法包括单独或与紫杉醇组合施用DFMO。

公开(公告)号：WO1998003183A1

公开(公告)日：1998-01-29

申请号：PCT/US1997013102

申请日：1997-07-22

Applicant: ILEX ONCOLOGY, INC.

Inventor： ILEX ONCOLOGY, INC. ,  VON HOFF, Daniel, D. ,  IZBICKA, Elzbieta

IPC: A61K31/70

CPC classification number: A61K31/7068 ,  A61K31/165 ,  A61K31/275 ,  A61K31/70 ,  A61K38/09 ,  A61K45/06 ,  A61K2300/00

Abstract: A method for treating prostate cancer, comprising administering an effective amount of 5,6-dihydro-5-azacytidine, or a pharmaceutically acceptable salt thereof, either alone, or in combination with hormonal therapy. The invention includes a method for increasing expression of the androgen receptor in a prostate cancer cell, a method of increasing E-cadherin expression in a prostate cancer cell, and a method of inducing apoptosis in a prostate cell.

Abstract translation: 一种治疗前列腺癌的方法，包括单独施用有效量的5,6-二氢-5-氮杂胞苷或其药学上可接受的盐，或与激素治疗组合。 本发明包括增加前列腺癌细胞中雄激素受体表达的方法，增加前列腺癌细胞中E-钙粘蛋白表达的方法和诱导前列腺细胞凋亡的方法。