Synthesis of naturally occurring ecteinascidins and related compounds
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A01N-043/00
A61K-031/33
C07D-487/00
C07D-491/00
C07D-513/00
출원번호
UP-0503106
(2003-02-04)
등록번호
US-7767659
(2010-08-24)
우선권정보
GB-0202544.3(2002-02-04)
국제출원번호
PCT/GB2003/000481
(2003-02-04)
§371/§102 date
20050608
(20050608)
국제공개번호
WO03/066638
(2003-08-14)
발명자
/ 주소
Barrasa, Valentin Martinez
Gallego, Pilar
Cuevas, Carmen
Munt, Simon
Manzanares, Ignacio
Menchaca, Roberto
Rodriguez, Natividad
Rodriguez, Alberto
출원인 / 주소
Pharma Mar, S.A.
대리인 / 주소
Sonnenfeld, Kenneth H.
인용정보
피인용 횟수 :
2인용 특허 :
29
초록
Ecteinascidin compounds with a quinone ring for ring E are active as anti-cancer agents. Related processes and compounds are provided.
대표청구항▼
The invention claimed is: 1. A compound of the formula (Ab): wherein Ra and Rb together with the carbon to which they are attached form a group: —C(═O)—; —CHOX1 or —CHNX1X2 where each X1 and X2 is independently selected from hydrogen, substituted or unsubstitut
The invention claimed is: 1. A compound of the formula (Ab): wherein Ra and Rb together with the carbon to which they are attached form a group: —C(═O)—; —CHOX1 or —CHNX1X2 where each X1 and X2 is independently selected from hydrogen, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstituted aryl, protecting group, and —C(═O)R′ wherein R′ is selected from hydrogen, OH, NO2, NH2, SH, CN, halogen, C1-C6 alkyl, alkenyl, alkynyl, aryl, aralkyl and heterocyclic; or a group of formula: wherein Rd and X1 are independently selected from hydrogen, substituted or unsubstituted R′, OR′, —C(═O)R′, substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, and substituted or unsubstituted aralkyl, wherein R′ is selected from hydrogen, OH, NO2, NH2, SH, CN, halogen, C(═O)H, C(═O)CH3, CO2H, CO2CH3, C1-C6 alkyl, alkenyl, alkynyl, aryl, aralkyl and heterocyclic; X is —O— or —NH—; R5 is OX1 wherein X1 is hydrogen, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstituted aryl, or —C(═O)R′ wherein R′ is selected from of hydrogen, OH, NO2, NH2, SH, CN, halogen, C1-C6 alkyl, alkenyl, alkynyl, aryl, aralkyl and heterocyclic; R7 is —OCH3 and R8 is —OH, or R7 and R8 together form a group —O—CH2—O—; R12b is hydrogen, substituted or unsubstituted alkyl, haloalkyl, alkoxyalkyl, haloalkoxyalkyl, arylalkylene, haloalkylarylalkylene, acyl, haloacyl, carbonate, carbamate, arylalkyl, alkenyl and amino acid; and R21 is —H, —OH or —CN. 2. A compound according to claim 1 wherein R5 is —OH or —OC(═O)R′ wherein R′ is selected from of hydrogen, OH, NO2, NH2, SH, CN, halogen, C1-C6 alkyl, alkenyl, alkynyl, aryl, aralkyl and heterocyclic. 3. A compound according to claim 2 wherein R5 is —OAc. 4. A compound according to claim 1, wherein R7 and R8 together form a group —O—CH2—O—. 5. A compound according to claim 1, wherein R12b is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, amino acid or acyl. 6. A compound according to claim 5 wherein R12b is methyl. 7. A compound according to claim 1, wherein R12b is —OH or —CN. 8. A compound according to claim 1, wherein X is —0—. 9. A compound according to claim 1 of formula: 10. A compound according to claim 1 of formula: 11. A compound according to claim 1 of formula: 12. A compound according to claim 1 of formula: 13. A compound according to claim 1 of formula: 14. A compound according to claim 1 of formula: 15. A pharmaceutical composition comprising a compound according to claim 1, and a pharmaceutical carrier. 16. A method for the treatment of a cancer selected from chronic myelogenous leukaemia, lung cancer, colon cancer, kidney cancer, malignant melanoma, prostate cancer, ovarian cancer, breast cancer, pancreatic epitheloid carcinoma, and cervix epitheloid carcinoma in a mammal affected by such cancer, the method comprising administering to the mammal a therapeutically effective amount of a compound of claim 1 or a pharmaceutical composition thereof.
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이 특허에 인용된 특허 (29)
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