[미국특허]
Pharmaceutical compositions comprising estetrol derivatives for use in cancer therapy
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-031/565
A61K-045/06
출원번호
US-0621267
(2015-02-12)
등록번호
US-9561238
(2017-02-07)
우선권정보
EP-02079414 (2002-10-23)
발명자
/ 주소
Coelingh Bennink, Herman Jan Tijmen
Bunschoten, Evert Johannes
출원인 / 주소
Donesta Bioscience B.V.
대리인 / 주소
Foley & Lardner LLP
인용정보
피인용 횟수 :
0인용 특허 :
21
초록▼
The present invention relates to a method of treating or preventing estrogen-suppressed tumors in a mammal, said method comprising the administration of a therapeutically effective amount of an estrogenic component to said mammal, wherein the estrogenic component is selected from the group consistin
The present invention relates to a method of treating or preventing estrogen-suppressed tumors in a mammal, said method comprising the administration of a therapeutically effective amount of an estrogenic component to said mammal, wherein the estrogenic component is selected from the group consisting of: substances represented by the following formula in which formula R1, R2, R3, R4 independently are a hydrogen atom, a hydroxyl group or an alkoxy group with 1-5 carbon atoms; precursors capable of liberating a substance according to the aforementioned formula when used in the present method; and mixtures of one or more of the aforementioned substances and/or precursors. The estrogenic component according to the invention is particularly useful in the treatment or prevention of colorectal and prostate cancer and, unlike commonly used estrogens, does not simultaneously enhance the risk of estrogen-stimulated cancers such as breast cancer.
대표청구항▼
1. A method of treating colorectal and/or prostate tumours in a human subject, comprising parenterally administering to the subject at least 0.1 mg per day of an estrogenic component selected from the group consisting of estetrol, precursors capable of liberating estetrol, and mixtures thereof, wher
1. A method of treating colorectal and/or prostate tumours in a human subject, comprising parenterally administering to the subject at least 0.1 mg per day of an estrogenic component selected from the group consisting of estetrol, precursors capable of liberating estetrol, and mixtures thereof, wherein the precursors capable of liberating estetrol are derivatives of estetrol wherein the hydrogen atom of at least one of the hydroxyl groups of estetrol is substituted by sulfamic acid or sulfonic acid of 1-25 carbon atoms, tetrahydrofuranyl, tetrahydropyranyl, a straight or branched chain glycosidic residue containing 1-20 glycosidic units per residue, or an acyl radical of a hydrocarbon carboxylic. 2. The method according to claim 1, wherein the estrogenic component consists of estetrol. 3. The method according to claim 1, wherein 0.1 mg to 20 mg per day of the estrogenic component is administered. 4. The method according to claim 3, wherein the estrogenic component consists of estetrol. 5. The method according to claim 1, wherein the estrogenic component is administered daily for at least 5 days. 6. The method according to claim 1, wherein the tumours are malignant tumours. 7. The method according to claim 1, wherein the tumours are colorectal tumours. 8. The method according to claim 1, wherein the subject is a female. 9. The method according to claim 1, further comprising co-administering a progestogen. 10. The method according to claim 9, wherein the progestogen is selected from the group consisting of progesterone, desogestrel, etonogestrel, gestodene, dienogest, levonorgestrel, norgestimate, norethisterone, drospirenone, trimegestone, and dydrogesterone. 11. A method of treating colorectal and/or prostate tumours in a human subject, comprising administering to the subject between 0.1 and 20 mg per day of estetrol. 12. The method according to claim 11, wherein the estetrol is administered daily for at least 5 days. 13. The method according to claim 11, wherein the tumours are malignant tumours. 14. The method according to claim 11, wherein the tumours are colorectal tumours. 15. The method according to claim 11, wherein the subject is a female. 16. The method according to claim 11, further comprising co-administering a progestogen selected from the group consisting of progesterone, desogestrel, etonogestrel, gestodene, dienogest, levonorgestrel, norgestimate, norethisterone, drospirenone, trimegestone, and dydrogesterone.
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