Cytotoxic compounds and their use 机翻标题: 暂无翻译,请尝试点击翻译按钮。

公开号/公开日
US2003171338 A1 2003-09-11 [US20030171338]US6699851 B2 2004-03-02 [US6699851] / 2003-09-112004-03-02
申请号/申请日
2001US-10332745 / 2001-07-05
发明人
STRELCHENOK OLEG;
申请人
ARDENIA INVESTMENTS;
主分类号
IPC分类号
A61K-031/661C07F-009/09C07F-009/12C07F-009/165
摘要
(US6699851) Novel amides of polyunsaturated fatty acids with cysteamine-S-phosphate have been synthesized.  Combinations of the all-trans-retinoic acid and/or amides of the 13-cis-retinoic acid with O-phospho-L-tyrosine, and N-docosahexaenoyl-cysteamine-S-phosphate, N-eicosapentaenoyl-cysteamine-S-phosphatee, N-arachidonoyl-cysteamine-S-phosphate, N-alpha-linolenoyl-cysteamine-S-phosphate, and N-gamma-linolenoyl-cysteamine-S-phosphate and their analogues N-docosahexaenoyl-O-phospho-2-aminoethanol, N-eicosapentaenoyl-O-phospho-2-aminoethanol, N-arachidonoyl-O-phospho-2-aminoethanol, N-alpha-linolenoyl-O-phospho-2-aminoethanol, N-gamma-linolenoyl-O-phospho-2-aminoethanol in different compositions exhibit a marked cell-growth inhibiting effect and display anti-tumor activity.
机翻摘要
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地址
代理人
代理机构
;
优先权号
2000SE-0002629 2000-07-12 2000US-60217810 2000-07-12 2001WO-SE01559 2001-07-05 2003US-10332745 2003-05-06
主权利要求
(US6699851) 1. A method for treating a patient suffering from cancer, said method comprising the step of administering to the patient an effective amount of a compound selected from the group consisting of N-docosahexaenoyl-cysteamine-S-phosphate, N-eicosapentaenoyl-cysteamine-S-phosphate, N-arachidonoyl-cysteamine-S-phosphate, N-alpha -linolenoyl-cysteamine-S-phosphate, and N-gamma -linolenoyl-cysteamine-S-phosphate. What is claimed is: 2.  A method for treating a patient suffering from cancer, said method comprising the step of administering to the patient an effective amount of a compound selected from the group consisting of N-docosahexaenoyl-cysteamine-S-phosphate, N-eicosapentaenoyl-cysteamine-S-phosphate, N-arachidonoyl-cysteamine-S-phosphate, N-alpha -linolenoyl-cysteamine-S-phosphate, and N-gamma -linolenoyl-cysteamine-S-phosphate in admixture or simultaneously with N-(all-trans-retinoyl)-O-phospho-L-tyrosine. 3. A method for treating a patient suffering from cancer, said method comprising the step of administering to the patient an effective amount of a compound selected from the group consisting of N-docosahexaenoyl-cysteamine-S-phosphate, N-eicosapentaenoyl-cysteamine-S-phosphate, N-arachidonoyl-cysteamine-S-phosphate, N-alpha -linolenoyl-cysteamine-S-phosphate, and N-gamma -linolenoyl-cysteamine-S-phosphate in admixture or simultaneously with N-(13-cis-retinoyl)-O-phospho-L-tyrosine. 4. A substantially pure compound selected from the group consisting of N-docosahexaenoyl-cysteamine-S-phosphate, N-eicosapentaenoyl-cysteamine-S-phosphate, N-arachidonoyl-cysteamine-S-phosphate, N-alpha -linolenoyl-cysteamine-S-phosphate, and N-gamma -linolenoyl-cysteamine-S-phosphate. 5. A pharmaceutical preparation, characterized in that it comprises a therapeutically effective amount of a compound according to claim 1. 6. A pharmaceutical preparation, characterized in that it comprises a therapeutically effective amount of a compound according to claim 1 in micellar form. 7. A pharmaceutical preparation, characterized in that it comprises a therapeutically effective amount of a compound selected from the group consisting of N-docosahexaenoyl-O-phospho-2-aminoethanol, N --  eicosapentaenoyl O-phospho-2-aminoethanol, N-arachidonoyl O-phospho-2-aminoethanol, N-alpha -linolenoyl O-phospho-2-aminoethanol, and N-gamma -linolenoyl O-phospho-2-aminoethanol. 8. A pharmaceutical preparation according to claim 4, characterized in that it comprises the therapeutically effective amount of the selected compound in micellar form. 9. A pharmaceutical preparation, characterized in that it comprises a therapeutically effective amount of a compound according to claim 1 in combination with a therapeutically effective amount of N-(all-trans-retinoyl)-O-phospho-L-tyrosine. 10. A pharmaceutical preparation, characterized in that it comprises a therapeutically effective amount of a compound according to claim 1 in combination with a therapeutically effective amount of N-(13-cis-retinoyl)-O-phospho-L-tyrosine. 11. A pharmaceutical preparation, characterized in that it comprises a therapeutically effective amount of a compound selected from the group consisting of N-docosahexaenoyl-O-phospho-2-aminoethanol, N-eicosapentaenoyl O-phospho-2-aminoethanol, N-arachidonoyl O-phospho-2-aminoethanol, N-alpha -linolenoyl O-phospho-2-aminoethanol, and N-gamma -linolenoyl O-phospho-2-aminoethanol in combination with a therapeutically effective amount of N-(all-trans-retinoyl)-O-phospho-L-tyrosine. 12. A pharmaceutical preparation, characterized in that it comprises a therapeutically effective amount of a compound selected from the group consisting of N-docosahexaenoyl-O-phospho-2-aminoethanol, N-eicosapentaenoyl O-phospho-2-aminoethanol, N-arachidonoyl O-phospho-2-aminoethanol, N-alpha -linolenoyl O-phospho-2-aminoethanol, and N-gamma -linolenoyl O-phospho-2-aminoethanol in combination with a therapeutically effective amount of N-(13-cis-retinoyl)-O-phospho-L-tyrosine. 13. A pharmaceutical preparation, characterized in that it comprises a therapeutically effective amount of N-docosahexaenoyl-cysteamine-S-phosphate and one of N-(all-trans-retinoyl)-O-phospho-L-tyrosine or N-(13-cis-retinoyl)-O-phospho-L-tyrosine. 14. A pharmaceutical preparation, characterized in that it comprises a therapeutically effective amount of N-eicosapentaenoyl-cysteamine-S-phosphate and one of N-(all-trans-retinoyl)-O-phospho-L-tyrosine or N-(13-cis-retinoyl)-O-phospho-L-tyrosine. 15. A pharmaceutical preparation, characterized in that it comprises a therapeutically effective amount of N-arachidonoyl-cysteamine-S-phosphate and one of N-(all-trans-retinoyl)-O-phospho-L-tyrosine or N-(13-cis-retinoyl)-O-phospho-L-tyrosine. 16. A pharmaceutical preparation, characterized in that it comprises a therapeutically effective amount of N-alpha -linolenoyl-cysteamine-S-phosphate and one of N-(all-trans-retinoyl)-O-phospho-L-tyrosine or N-(13-cis-retinoyl)-O-phospho-L-tyrosine. 17. A pharmaceutical preparation, characterized in that it comprises a therapeutically effective amount of N-gamma -linolenoyl-cysteamine-S-phosphate and one of N-(all-trans-retinoyl)-O-phospho-L-tyrosine or N-(13-cis-retinoyl)-O-phospho-L-tyrosine. 18. Use of a compound according to claim 1 for the manufacture of a pharmaceutical preparation. 19. Use of a compound according to claim 1 for the manufacture of a pharmaceutical preparation for the treatment of cancer. 20. Use of a compound for the manufacture of a pharmaceutical preparation, said compound being selected from the group consisting of N-docosahexaenoyl-O-phospho-2-aminoethanol, N-eicosapentaenoyl O-phospho-2-aminoethanol, N-arachidonoyl O-phospho-2-aminoethanol, N-alpha -linolenoyl O-phospho-2-aminoethanol, and N-gamma -linolenoyl O-phospho-2-aminoethanol. 21. Use of a compound for the manufacture of a pharmaceutical preparation for the treatment of cancer, said compound being selected from the group consisting of N-docosahexaenoyl-O-phospho-2-aminoethanol, N --  eicosapentaenoyl O-phospho-2-aminoethanol, N-arachidonoyl O-phospho-2-aminoethanol, N-alpha -linolenoyl O-phospho-2-aminoethanol, and N-gamma -linolenoyl O-phospho-2-aminoethanol. 22. A method for treating a patient suffering from cancer, said method comprising the step of administering to the patient an effective amount of a compound according to claim 7, in admixture with or substantially simultaneously with a cytotoxic agent. 23. A method for treating a patient suffering from cancer, said method comprising the step of administering to the patient an effective amount of a compound according to claim 11, in admixture with or substantially simultaneously with a cytotoxic agent. 24. A method for treating a patient suffering from cancer, said method comprising the step of administering to the patient an effective amount of a compound according to claim 8, in admixture with or substantially simultaneously with a cytotoxic agent. 25. A method for treating a patient suffering from cancer, said method comprising the step of administering to the patient an effective amount of a compound according to claim 12, in admixture with or substantially simultaneously with a cytotoxic agent. 26. The method of claim 22 wherein said cytotoxic agent is doxorubicin. 27. The method of claim 23 wherein said cytotoxic agent is doxorubicin. 28. The method of claim 24 wherein said cytotoxic agent is doxorubicin. 29. The method of claim 25 wherein said cytotoxic agent is doxorubicin.
法律状态
(US6699851) LEGAL DETAILS FOR US2003171338  Actual or expected expiration date=2021-07-05    Legal state=ALIVE    Status=GRANTED     Event publication date=2003-05-06  Event code=US/APP  Event indicator=Pos  Event type=Examination events  Application details  Application country=US US10332745  Application date=2003-05-06  Standardized application number=2001US-10332745     Event publication date=2003-04-17  Event code=US/M905  Event type=Examination events  Event type=OAO  Notice of DO/EO Missing Requirements Mailed    Event publication date=2003-05-06  Event code=US/EXMR  Event type=Administrative notifications  USPTO Examiner Name Primary Examiner: CARR, DEBORAH D    Event publication date=2003-05-06  Event code=US/ART  Event type=Administrative notifications  USPTO Art Group  ART=1621     Event publication date=2003-05-06  Event code=US/DK  Event type=Examination events  Attorney Docket Number Docket Nbr: 506112000800    Event publication date=2003-05-06  Event code=US/SMALL  Event type=Administrative notifications  Appl Has Filed a Verified Statement of Micro to Small Entity Status Business Entity Status: SMALL    Event publication date=2003-05-06  Event code=US/AIA  Event type=Administrative notifications  First Inventor File Indicated:  AIA=No     Event publication date=2003-05-06  Event code=US/APE  Event type=Corrections  Preliminary amendments    Event publication date=2003-05-06  Event code=US/IDS  Event type=Examination events  Event type=OAI  Information Disclosure Statement Filed    Event publication date=2003-05-16  Event code=US/M903  Event indicator=Pos  Event type=Examination events  Event type=OAO  Notice of DO/EO Acceptance Mailed    Event publication date=2003-09-11  Event code=US/A1  Event type=Examination events  Application published  Publication country=US  Publication number=US2003171338  Publication stage Code=A1  Publication date=2003-09-11  Standardized publication number=US20030171338     Event publication date=2003-09-23  Event code=US/DOCK  Event indicator=Pos  Event type=Examination events  Case Docketed to Examiner    Event publication date=2003-09-29  Event code=US/DOCK  Event indicator=Pos  Event type=Examination events  Case Docketed to Examiner    Event publication date=2003-10-01  Event code=US/NOAM  Event indicator=Pos  Event type=Examination events  Event type=OAO  Mail Notice of Allowance    Event publication date=2003-10-29  Event code=US/AS  Event type=Change of name or address  Event type=Reassignment  Assignment  Effective date of the event=2003-09-30  ASSIGNMENT OF ASSIGNORS INTEREST ASSIGNOR:STRELCHENOK, OLEG REEL/FRAME:014089/0085     Event publication date=2004-01-26  Event code=US/APRDY  Event indicator=Pos  Event type=Examination events  Application Is Considered Ready for Issue    Event publication date=2004-02-12  Event code=US/PAT  Event indicator=Pos  Event type=Event indicating In Force  Patented Case    Event publication date=2004-02-12  Event code=US/ISSM  Event indicator=Pos  Event type=Examination events  Event type=OAO  Event type=Restitution or restoration  Issue Notification Mailed    Event publication date=2004-03-02  Event code=US/B2  Event indicator=Pos  Event type=Event indicating In Force  Granted patent as second publication  Publication country=US  Publication number=US6699851  Publication stage Code=B2  Publication date=2004-03-02  Standardized publication number=US6699851     Event publication date=2004-03-02  Event code=US/354  Event indicator=Pos  Event type=Extension of term of duration of protection  Patent term extended under  35 U.S.C 154(b) until/for Delays (A,B,C): 0  Overlap Delays: 0  Non Overlap Delays: 0   PTO Office Delays: 0  Applicant Delays: 0  Adjustment total:  Number of days of extension=0    Event publication date=2005-10-25  Event code=US/CC  Event type=Corrections  Event type=Restitution or restoration  Certificate of Correction - Post Issue Communication    Event publication date=2007-03-13  Event code=US/NMFP  Event type=Payment or non-payment notifications  Publication of First Notice of Maintenance Fees Payable. PAYMENT NOTICE YEAR:  Year of payment of annual fees=3     Event publication date=2007-07-31  Event code=US/FPAY  Event indicator=Pos  Event type=Event indicating In Force  Event type=Payment or non-payment notifications  Fee payment recorded   Annual fees payment date=2007-07-31     Year of payment of annual fees=4     Event publication date=2011-03-15  Event code=US/NMFP  Event type=Payment or non-payment notifications  Publication of First Notice of Maintenance Fees Payable. PAYMENT NOTICE YEAR:  Year of payment of annual fees=7     Event publication date=2011-08-09  Event code=US/FPAY  Event indicator=Pos  Event type=Event indicating In Force  Event type=Payment or non-payment notifications  Fee payment recorded   Annual fees payment date=2011-08-09     Year of payment of annual fees=8     Event publication date=2015-03-17  Event code=US/NMFP  Event type=Payment or non-payment notifications  Publication of First Notice of Maintenance Fees Payable. 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专利类型码
A1B2
国别省市代码
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