ХОЭФЛИХ Клаус П.,ДЖАББ Адриан М.,КЁППЕН Хартмут,ОНГ Кристи С.
申请号：
RU2014141018
公开号：
RU2014141018A
申请日:
2013.03.13
申请国别(地区):
RU
年份:
2016
代理人:
摘要：
1. A method of treating melanoma in an individual, comprising bringing the melanoma into contact with a therapeutically effective amount of a PAK1.2 inhibitor. The method of claim 1, wherein the melanoma is melanoma with wild-type BRAF. The method of claim 1, wherein the PAK1 is overexpressed in the tumor compared to non-cancerous skin cells. The method according to claim 1, wherein PAK 1.5 is amplified in the tumor. The method of claim 4, wherein the number of copies of PAK1 in the tumor is greater than about 2.5.6. The method of claim 1, wherein the inhibitor is a small molecule, nucleic acid, or polypeptide. The method of claim 6, wherein the small molecule is PF-3758309.8. The method of claim 6, wherein the small molecule is a compound of formula VII9. The method of claim 8, wherein the small molecule is a compound of formula VII, and A is 4-indolyl, 5-indolyl, 4-indazolyl, 5-indazolyl, 4-benzimidazolyl or 5-benzimidazolyl； R, R and R are independently hydrogen or C1-6alkyl； R 1 is hydrogen or C 1-6 alkyl； R 1 is hydrogen, halogen or C 1-6 alkyl； and R 1 is cycloalkyl optionally substituted with fluorine. 10. The method of claim 1, wherein the individual is a human. The method according to any one of paragraphs. 1-10, where the PAK1 inhibitor is used in combination with a therapeutic agent. The use of a PAK1 inhibitor for the treatment of melanoma in an individual. 13. The use of claim 12, wherein the melanoma is a melanoma with wild-type BRAF. A composition comprising a PAK1 inhibitor for use in the treatment of melanoma. 15. The composition of claim 14, wherein the melanoma is a wild-type BRAF melanoma. A composition according to claim 14 or 15, further comprising a pharmaceutically acceptable excipient. The use of a PAK1 inhibitor in the manufacture of a medicament for the treatment of melanoma. 18. Application p1. Способ лечения меланомы у индивидуума, включающий приведение меланомы в контакт с терапевтически эффективным количеством ингибитора РАК1.2. Способ
