Fatty acid analogues for the treatment of cancer
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-031/22
A61K-031/21
A61K-031/23
A61K-031/20
A61K-031/185
출원번호
US-0312901
(2001-07-13)
등록번호
US-7378443
(2008-05-27)
우선권정보
NO-20003591(2000-07-13)
국제출원번호
PCT/NO01/000301
(2001-07-13)
§371/§102 date
20030102
(20030102)
국제공개번호
WO02/003983
(2002-01-17)
발명자
/ 주소
Berge,Rolf
출원인 / 주소
Thia Medica, AS
대리인 / 주소
Reed Smith LLP
인용정보
피인용 횟수 :
12인용 특허 :
4
초록▼
A fatty acid analogue of the general formula: R1-[xi-CH2]n--COOR2, wherein R1 is: a C2-C24 alkene with one or more double bonds and/or with one or more triple bonds, and/or a C2-C24 alkyne, and/or a C1-C24 alkyl, or a C1-C24 alkyl substituted in one or several positions with one or more compounds se
A fatty acid analogue of the general formula: R1-[xi-CH2]n--COOR2, wherein R1 is: a C2-C24 alkene with one or more double bonds and/or with one or more triple bonds, and/or a C2-C24 alkyne, and/or a C1-C24 alkyl, or a C1-C24 alkyl substituted in one or several positions with one or more compounds selected from the group comprising fluoride, chloride, hydroxy, C1-C4 alkoxy, C1-C4 alkylthio, C2-C5 acyloxy or C1-C4 alkyl, and wherein R2 represents hydrogen or C1-C4 alkyl, and wherein n is an integer from 1 to 12, and wherein i is an odd number and indicates the position relative to COOR2, and wherein Xi independent of each other are selected from the group comprising O, S, SO, SO2, Se and CH2, and with the proviso that at least one of the Xi is not CH2, and or a salt, prodrug or complex thereof is used in the treatment and/or prevention of primary and secondary metastatic neoplasms.
대표청구항▼
The invention claimed is: 1. A method of inhibiting the metastasis of metastatic neoplasms comprising the administration to a mammal in need thereof an effective amount of a fatty acid analogue having the following formula description="In-line Formulae" end="lead"R1-[xi-CH2]n--COOR2 description="
The invention claimed is: 1. A method of inhibiting the metastasis of metastatic neoplasms comprising the administration to a mammal in need thereof an effective amount of a fatty acid analogue having the following formula description="In-line Formulae" end="lead"R1-[xi-CH2]n--COOR2 description="In-line Formulae" end="tail" wherein R1 is; a C2-C24 alkene with one or more double bonds and/or with one or more triple bonds; and/or a C2-C24 alkyne, and/or a C1-C24 alkyl, or a C1-C24 alkyl substituted in one or several positions with one a more compounds selected from the group comprising fluoride, chloride, hydroxy, C1-C4 alkoxy, C1-C4 alkylthio, C2-C5 acyloxy or C1-C4 alkyl, and wherein R2 represents hydrogen or C1-C4 alkyl, and wherein n is an integer from 2-12, and wherein i is an odd number and indicates the position relative to COOR2, and wherein xi are independently selected from the group consisting of O, S, SO, SO2, Se and CH2, and with the proviso that at least one of the xi is not CH2; and with the proviso that if R1 is an alkyl, then xi=3 is not Se or S; a salt, prodrug or complex thereof, wherein said metastatic neoplasms are sensitive to the effects of said fatty acid analogue. 2. A method as set forth in claim 1, wherein the method is effective to inhibit the invasion of a primary tumor into connective tissue. 3. A method as set forth in claim 1, wherein the method is effective to inhibit the formation of a secondary tumor. 4. A method as set forth in claim 1, wherein the method is effective to increase the survival of a mammal with a tumor due to decrease in the survival-threatening effects of the tumor. 5. A method as set forth in claim 1, wherein the method is effective to maintain a therapeutically effective concentration substantially continuously in the blood of the mammal during the period of administration. 6. A method as set forth in claim 1, wherein the fatty acid analogue is administered in unit dosage forms. 7. A method of treating the metastasis of metastatic neoplasms comprising the administration to a mammal in need thereof an effective amount of a fatty acid analogue having the following formula description="In-line Formulae" end="lead"R1-[xi-CH2]n--COOR2 description="In-line Formulae" end="tail" wherein R1 is; a C2-C24 alkene with one or more double bonds and/or with one a more triple bonds, end/or C2-C24 alkyne, and/or C1-C24 alkyl, or a C1-C24 alkyl substituted in one or several positions with one or more compounds selected from the group comprising fluoride, chloride, hydroxy, C1-C4 alkoxy, C2-C4 alkyltliio, C2-C5 acyloxy or C1-C4 alkyl, and wherein R2 represents hydrogen or C1-C4 alkyl, and wherein n is an integer from 1-12, and wherein i is an odd number and indicates the position relative to COOR2, and wherein xi are independently selected from the group consisting of O , S, SO, SO2, Se and CH2, and with the proviso that at least one of the x1 is not CR2; a salt, prodrug or complex thereof, wherein said metastatic neoplasms are sensitive to the effects of said fatty acid analogue. 8. A method as set forth in claim 7, wherein the fatty acid analogue is tetradecylthioacetic acid. 9. A method as set forth in claim 7, wherein the fatty acid analogue is tetradecylselenoacetic acid. 10. A method as set forth in claim 7, wherein the treatment is effective to inhibit the invasion of a primary tumor into connective tissue. 11. A method as set forth in claim 7, herein the treatment is effective to inhibit the formation of a secondary tumor. 12. A method as set forth in claim 7, wherein the treatment is effective to increase the survival of a mammal with a tumor due to decrease in the survival-threatening effects of the tumor. 13. A method as set forth in claim 7, wherein the treatment is effective to maintain a therapeutically effective concentration substantially continuously in the blood of the mammal during the period of administration. 14. A method as set forth in claim 7, wherein the fatty acid analogue is administered in unit dosage forms. 15. A method of inhibiting the metastasis of metastatic neoplasms comprising the administration to a mammal in need thereof an effective amount of a fatty acid analogue having the following formula description="In-line Formulae" end="lead"R1-x-CH2--COOR2 description="In-line Formulae" end="tail" wherein R1 is; a C1-C24 alkyl, and wherein R2 represents hydrogen or C1-C4 alkyl, and wherein x is independently selected from the group consisting of S and Se; a salt, prodrug or complex thereof, wherein said metastatic neoplasms are sensitive to the effects of said fatty acid analogue. 16. The method as set forth in claim 15, wherein the fatty acid analogue is tetradecylthioacetic acid. 17. The method as set forth in claim 15, wherein the fatty acid analogue is tetradecylselenoacetic acid. 18. The method as set forth in claim 15, wherein the method is effective to inhibit the invasion of a primary tumor into connective tissue. 19. The method as set forth in claim 15, wherein the method is effective to inhibit the formation of a secondary tumor. 20. The method as set forth in claim 15, wherein the method is effective to increase the survival of a mammal with a tumor due to decrease in the survival-threatening effects of the tumor. 21. The method as set forth in claim 15, wherein the method is effective to maintain a therapeutically effective concentration substantially continuously in the blood of the mammal during the period of administration. 22. The method as set forth in claim 15, wherein the fatty acid analogue is administered in unit dosage forms.
DiPerna, Paul M.; Brown, David; Rosinko, Mike; Kincade, Dan; Michaud, Michael; Nadworny, John; Kruse, Geoffrey A.; Ulrich, Thomas R., Infusion pump system with disposable cartridge having pressure venting and pressure feedback.
DiPerna, Paul M.; Brown, David; Rosinko, Mike; Kincade, Dan; Michaud, Michael; Nadworny, John; Kruse, Geoffrey A.; Ulrich, Thomas R., Infusion pump system with disposable cartridge having pressure venting and pressure feedback.
Verhoef, Erik T.; DiPerna, Paul M.; Rosinko, Mike; Williamson, Mark; Kruse, Geoffrey A.; Ulrich, Thomas R.; Lamb, Phil; Saint, Sean; Michaud, Michael; Trevaskis, William, Infusion pump system with disposable cartridge having pressure venting and pressure feedback.
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