Antifolate compounds for the treatment of melanoma
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A01N-043/16
A61K-031/35
A61K-031/353
출원번호
US-0809713
(2008-12-18)
등록번호
US-9060997
(2015-06-23)
우선권정보
GB-0725077.2 (2007-12-21)
국제출원번호
PCT/IB2008/003727
(2008-12-18)
§371/§102 date
20100621
(20100621)
국제공개번호
WO2009/081275
(2009-07-02)
발명자
/ 주소
Rodriguez-Lopez, Jose Neptuno
Del Campo Ferrer, Luis Sanchez
Cabezas-Herrera, Juan
Tomas, Alberto Tarraga
Saez Ayala, Magali Maria
출원인 / 주소
UNIVERSIDAD DE MURCIA
대리인 / 주소
Vedder Price P.C.
인용정보
피인용 횟수 :
0인용 특허 :
2
초록▼
This invention relates to compounds of the formula X) or Xl) (X) (XI) wherein: each —R1, —R2 and —R3 is independently -Q1, —OH or —H, where at least one of —R1, —R2 and —R3 is not —H or —OH; each —R4 and —R5 is independently -Q2 or —H; each -Q1 is independently selected from: —F, —Cl, —RA, —ORA, —SH
This invention relates to compounds of the formula X) or Xl) (X) (XI) wherein: each —R1, —R2 and —R3 is independently -Q1, —OH or —H, where at least one of —R1, —R2 and —R3 is not —H or —OH; each —R4 and —R5 is independently -Q2 or —H; each -Q1 is independently selected from: —F, —Cl, —RA, —ORA, —SH, —SRA, where each —RA is independently selected from methyl and ethyl, which may substituted by one or more fluoro or chloro groups; and each -Q2 is selected from: —F, —Cl, —RB, —ORB, —SH, —SRB, where each —RB is independently selected from methyl and ethyl, which may substituted by one or more fluoro or chloro groups; which are useful in the treatment of melanoma.
대표청구항▼
1. A method of treating melanoma comprising administering to an individual in need thereof a therapeutically effective dose of a compound of formula (XI) at neutral pH: wherein:each —R1, —R2 and —R3 is independently -Q1, —OH or —H, where at least one of —R1, —R2 and —R3 is not a substituent selected
1. A method of treating melanoma comprising administering to an individual in need thereof a therapeutically effective dose of a compound of formula (XI) at neutral pH: wherein:each —R1, —R2 and —R3 is independently -Q1, —OH or —H, where at least one of —R1, —R2 and —R3 is not a substituent selected from the group consisting of —H and —OH;each —R4 and —R5 is independently —H;each -Q1 is independently selected from the group consisting of: —F, —Cl,—RA,—ORA,—SH, and —SRA,where each —RA is independently selected from the group consisting of: methyl and ethyl, each of which may substituted by one or more fluoro or chloro groups;wherein optionally one or more of the hydroxyl groups in the compound of formula (XI) are esterified to an —O—C(═O)—RC group, wherein RC is selected from the group consisting of: methyl and ethyl;or an isomer, salt or solvate thereof. 2. A method according to claim 1 wherein —R1, —R2, and —R3 are the same. 3. A method according to claim 1 wherein —R1 and —R3 are the same. 4. A method according to claim 1 wherein, each of —R2 and —R3 is independently selected from the group consisting of: —H, —F, —Cl, —Br, —I, and —ORA. 5. A method according to claim 1 wherein each of —R1, —R2 and —R3 is independently —ORA. 6. A method according to claim 1 wherein each —RA is independently methyl, optionally substituted by one or more fluoro or chloro groups. 7. A method according to claim 1 wherein the compound is of formula (XIa): or Formula (XIb): wherein optionally one of more of the hydroxyl groups in the compound of formula (XIa) or formula (XIb) are esterified to an —O—C(═O)—Rc group, where Rc is selected from the group consisting of methyl and ethyl;or an isomer, salt, or solvate thereof. 8. A method according to claim 7 wherein Rc is methyl. 9. A method according to claim 1 wherein the compound of formula (XI) is one of: wherein optionally one or more of the hydroxyl groups in the compound are esterified to an —O—C(═O)—RC group, where RC is selected from the group consisting of: methyl and ethyl;or an isomer, salt, or solvate thereof. 10. A method according to claim 1 wherein the compound is 3,4,5-trimethoxy-epicatechin-3-gallate, or an isomer, salt, solvate, chemically protected form thereof. 11. A method according to claim 1 wherein the compound is administered in combination with; a cytotoxic FRα ligand selected from the group consisting of 2-[4-[2-(4-amino-2-oxo-3,5,7-triazabicyclo[4.3.0]nona-3,8,10-trien-9-yl)ethyl]benzoyl]aminopentanedioic acid, BGC945 and BGC638;an anti-androgen selected from the group consisting of flutamide, nilutamide, bicalutamide, finasteride and dutasteride;a methionine cycle inhibitor selected from the group consisting of s-adenosylmethionine, 5′-methylthioadenosine, 5-azacytidine and 5-aza-2′-deoxycytidine, adenosine, dipirydamole, pirydamole and difluoromethylornithine; or,a thymidylate synthase (TS) inhibitor selected from the group consisting of 5-fluorouracil, fluorodeoxyuridine, raltitrexed, and nolatrexed.
연구과제 타임라인
LOADING...
LOADING...
LOADING...
LOADING...
LOADING...
이 특허에 인용된 특허 (2)
Cheng Shu Jun,JPX ; Wang De Chang,JPX ; Zhen Yong Su,JPX ; Nishino Hoyoku,JPX ; Hara Yukihiko,JPX, Method of increasing the effectiveness of anti-metabolites.
Netke,Shrirang; Niedzwiecki,Aleksandra; Rath,Matthias; Roomi,Waheed M., Nutrient pharmaceutical formulation comprising polyphenols and use in treatment of cancer.
※ AI-Helper는 부적절한 답변을 할 수 있습니다.