Apigenin analogs, compositions, and methods related thereto
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
C07D-311/30
C07D-405/12
C07D-407/12
출원번호
US-0304966
(2015-04-18)
등록번호
US-9868715
(2018-01-16)
국제출원번호
PCT/US2015/026563
(2015-04-18)
국제공개번호
WO2015/161309
(2015-10-22)
발명자
/ 주소
Zhou, Jia
Hellmich, Mark
Szabo, Csaba
출원인 / 주소
THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEMS
대리인 / 주소
Norton Rose Fulbright US LLP
인용정보
피인용 횟수 :
0인용 특허 :
1
초록▼
Certain embodiments are directed to apigenin analogues or derivatives. In certain aspects, the derivatives are developed as cystathionine-beta-synthase (CBS) inhibitors. In certain aspects, the derivatives are used as anticancer or anti-inflammatory agents. Certain embodiments are directed methods o
Certain embodiments are directed to apigenin analogues or derivatives. In certain aspects, the derivatives are developed as cystathionine-beta-synthase (CBS) inhibitors. In certain aspects, the derivatives are used as anticancer or anti-inflammatory agents. Certain embodiments are directed methods of treating or compositions used to treat fibrosis and cancers. In certain aspects one or more compounds described herein can be administered to a subject to treat pancreatic fibrosis, liver fibrosis, pancreatic cancer, colon cancer, breast cancer, brain tumors, head/neck cancer, prostate and lung cancers as well as other inflammation.
대표청구항▼
1. Certain embodiments are directed to compounds having the general formula of Formula II: where X is O;n is 1, 2, 3, 4, or 5;R1, R3, and R5 are hydrogen;R2 and R4 are methoxy; andR7 is a C1-C6 hydroxyalkyl substituted by a 3 to 8 membered heterocycle, or a 3 to 8 membered heterocycle. 2. The compou
1. Certain embodiments are directed to compounds having the general formula of Formula II: where X is O;n is 1, 2, 3, 4, or 5;R1, R3, and R5 are hydrogen;R2 and R4 are methoxy; andR7 is a C1-C6 hydroxyalkyl substituted by a 3 to 8 membered heterocycle, or a 3 to 8 membered heterocycle. 2. The compound of claim 1, wherein X is at the 4′ position. 3. The compound of claim 1, wherein n is 2. 4. The compound of claim 1, wherein R7 is a 3 or 6 member heterocycle. 5. The compound of claim 4 wherein R7 is an epoxide. 6. The compound of claim 1, wherein the compound is selected from 5,7-Dimethoxy-2-[4-(2-morpholin-4-yl-ethoxy)-phenyl]-chromen-4-one (HJC-5-16), 5,7-Dimethoxy-2-[4-(2-piperidin-1-yl-ethoxy)-phenyl]-chromen-4-one (HJC-5-56), 5,7-Dimethoxy-2-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-chromen-4-one (HJC-5-57), 5,7-Dimethoxy-2-[4-(piperidin-4-yloxy)-phenyl]-chromen-4-one (HJC-5-43), 5,7-Dimethoxy-2-(4-oxiranylmethoxy-phenyl)-chromen-4-one (HJC-5-61), 2-[4-(2-Hydroxy-3-piperidin-1-yl-propoxy)-phenyl]-5,7-dimethoxy-chromen-4-one (HJC-5-100), or 2-[4-(2-Hydroxy-3-pyrrolidin-1-yl-propoxy)-phenyl]-5,7-dimethoxy-chromen-4-one (HJC-6-4).
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