US2022112157A1PendingUtilityA1
Myc-max inhibitor compound therapeutics for cancer treatment, methods and uses associated therewith
Est. expirySep 5, 2038(~12.1 yrs left)· nominal 20-yr term from priority
Inventors:Artem TcherkassovPaul S. RennieFuqiang BanEric J. J. LeblancLavinia A. CarabetNada LallousKriti SinghHelene MorinAnh-Tien Ton
A61P 35/00C07D 241/24C07D 403/12C07D 403/06C07C 255/66C07D 271/12C07C 381/00C07C 233/56C07C 311/18C07C 335/18C07D 239/42C07D 261/08C07K 5/06026C07C 2603/74C07D 333/20C07D 417/12C07C 237/42C07C 237/22C07D 413/12C07D 213/40C07C 335/16C07C 271/22C07D 417/06C07C 323/60C07D 211/42C07C 237/12C07C 233/43C07D 213/61C07D 311/16C07D 307/14C07D 265/36C07D 405/12C07D 471/04C07D 409/06C07D 249/08C07D 213/75C07D 235/02C07C 275/30C07D 231/14C07C 275/24C07K 7/06C07D 265/30C07C 311/39C07D 333/38C07C 335/12C07D 277/36C07C 335/22C07C 311/19C07C 275/10C07C 2601/16C07C 235/20C07C 335/20C07C 2601/08
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Claims
Abstract
Provided herein are Myc-Max inhibitory compounds having the structure of Formula (I) and compositions thereof for use in the treatment of cancer. In particular, the Myc-Max inhibitory compounds may be useful for the treatment of cancers selected from one or more of: prostate cancer, breast cancer, colon cancer, cervical cancer, small-cell lung carcinomas, neuroblastomas, osteosarcomas, glioblastomas, melanoma and myeloid leukaemia.
Claims
exact text as granted — not AI-modifiedWhat is claimed is:
1 . A compound, the compound having the structure of Formula I:
wherein,
M 1 is selected from:
M 2 is selected from:
CH 3 or NH 2 ;
A 1 is selected from CH 2 , CH(CH 3 ), CH(CH 2 CH 3 ), CH(CH(CH 3 ) 2 ), or CHX;
A 2 is CH 2 or CH(CH 3 );
T 1 is H or CH 3 ;
T2 is H or CH 3 ;
D 1 is O or S;
n 1 is 0-3, wherein if n 1 is 2 or 3, each A 1 may be independently selected from CH 2 , CH(CH 3 ), CH(CH 2 CH 3 ), CH(CH(CH 3 ) 2 ), or CHX;
n 2 is 0-1;
n 3 is 1 or 2, wherein if n 3 is 2, each D 1 may be independently selected from O or S;
n 4 is 0-3, wherein if n 4 is 2 or 3, each T 2 may be independently selected from H or CH 3 ;
n 5 is 0-3, wherein if n 5 is 2 or 3, each A 2 may be independently selected from CH 2 , CH(CH 3 ), CH(CH 2 CH 3 ), CH(CH(CH 3 ) 2 ), or CHX;
X is
E 1 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, CF 3 , OCF 3 , OCF 2 , S(═O) 2 (NH 2 ), OCH 2 C(CH 3 )(CH 2 ),
E 2 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, CF 3 , OCF 3 , OCF 2 , S(═O) 2 (NH 2 ), OCH 2 C(CH 3 )(CH 2 ),
E 3 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, CF 3 , OCF 3 , OCF 2 , S(═O) 2 (NH 2 ), OCH 2 C(CH 3 )(CH 2 ),
E 4 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, CF 3 , OCF 3 , OCF 2 , S(═O) 2 (NH 2 ), OCH 2 C(CH 3 )CH 2 )
E 5 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, CF 3 , OCF 3 , OCF 2 , S(═O) 2 (NH 2 ), OCH 2 C(CH 3 (CH 2 ),
E 6 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, CF 3 , OCF 3 , OCF 2 , S(═O) 2 (NH 2 ), OCH 2 C(CH 3 )(CH 2 ),
E 7 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, CF 3 , OCF 3 , OCF 2 , S(═O) 2 (NH 2 ), OCH 2 C(CH 3 )(CH 2 ),
G 1 is H, OCH 3 , CH 2 CH 3 , F, Cl, Br, CF 3 , OCF 3 , OCF 2 , S(═O) 2 (NH 2 ) or OCH 2 C(CH 3 )(CH 2 );
L 1 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, CF 3 , OCF 3 , OCF 2 , S(═O) 2 (NH 2 ), OCH 2 C(CH 3 )(CH 2 ),
L 2 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, CF 3 , OCF 3 , OCF 2 , S(═O) 2 (NH 2 ), OCH 2 C(CH 3 )(CH 2 ),
L 3 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, CF 3 , OCF 3 , OCF 2 , S(═O) 2 (NH 2 ), OCH 2 C(CH 3 )(CH 2 ),
L 4 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, CF 3 , OCF 3 , OCF 2 , S(═O) 2 (NH 2 ), OCH 2 C(CH 3 )(CH 2 ),
L 5 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, CF 3 , OCF 3 , OCF 2 , S(═O) 2 (NH 2 ), OCH 2 C(CH 3 )(CH 2 ),
L 6 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, CF 3 , OCF 3 , OCF 2 , S(═O) 2 (NH 2 ), OCH 2 C(CH 3 )(CH 2 ),
L 7 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, CF 3 , OCF 3 , OCF 2 , S(═O) 2 (NH 2 ), OCH 2 C(CH 3 )(CH 2 ),
and
provided that when M 1 is
and G 1 is H, then n 3 is 1;
wherein the compound is for use in the treatment of one or more of the following: prostate cancer; breast cancer; colon cancer; cervical cancer; small-cell lung carcinoma; neuroblastomas; osteosarcoma; glioblastoma; melanoma; and myeloid leukaemia.
2 . The compound of claim 1 , wherein M 1 is selected from:
and wherein M 2 is selected from:
CH 3 or NH 2 .
3 . The compound of claim 1 or 2 , wherein A 1 is selected from CH 2 , CH(CH 3 ) or CH(CH 2 CH 3 ); wherein A 2 is CH 2 or CH(CH 3 ); and wherein G 1 is H, OCH 3 , CH 2 CH 3 , F, Cl, Br, CF 3 , OCF 3 , OCF 2 or S(═O) 2 (NH 2 ).
4 . The compound of claim 1 , 2 or 3 , wherein E 1 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, CF 3 , OCF 3 , OCF 2 , S(═O) 2 (NH 2 ), OCH 2 C(CH 3 )(CH 2 ),
E 2 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, CF 3 , OCF 3 , OCF 2 , S(═O) 2 (NH 2 ), OCH 2 C(CH 3 )(CH 2 ),
E 3 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, CF 3 , OCF 3 , OCF 2 , S(═O) 2 (NH 2 ), OCH 2 C(CH 3 )(CH 2 ),
E 4 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, CF 3 , OCF 3 , OCF 2 , S(═O) 2 (NH 2 ), OCH 2 C(CH 3 )(CH 2 ),
E 5 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, CF 3 , OCF 3 , OCF 2 , S(═O) 2 (NH 2 ), OCH 2 C(CH 3 )(CH 2 ),
E 6 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, CF 3 , OCF 3 , OCF 2 , S(═O) 2 (NH 2 ), OCH 2 C(CH 3 )(CH 2 ),
E 7 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, CF 3 , OCF 3 , OCF 2 , S(═O) 2 (NH 2 ), OCH 2 C(CH 3 )(CH 2 ),
L 1 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, CF 3 , OCF 3 , OCF 2 , S(═O) 2 (NH 2 ), OCH 2 C(CH 3 )(CH 2 ),
L 2 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, CF 3 , OCF 3 , OCF 2 , S(═O) 2 (NH 2 ), OCH 2 C(CH 3 )(CH 2 ),
L 3 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, CF 3 , OCF 3 , OCF 2 , S(═O) 2 (NH 2 ), OCH 2 C(CH 3 )(CH 2 ),
L 4 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, CF 3 , OCF 3 , OCF 2 , S(═O) 2 (NH 2 ), OCH 2 C(CH 3 )(CH 2 ),
L 5 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, CF 3 , OCF 3 , OCF 2 , S(═O) 2 (NH 2 ), OCH 2 C(CH 3 )(CH 2 ),
L 6 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, CF 3 , OCF 3 , OCF 2 , S(═O) 2 (NH 2 ), OCH 2 C(CH 3 )(CH 2 ),
and
L 7 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, CF 3 , OCF 3 , OCF 2 , S(═O) 2 (NH 2 ), OCH 2 C(CH 3 )(CH 2 ),
5 . The compound of any one of claims 1 - 4 , wherein the compound has the structure of Formula II:
6 . The compound of any one of claims 1 - 5 , wherein the compound has the structure of Formula III:
7 . The compound of claim 1 , wherein the compounds is selected from TABLE 3.
8 . A compound, the compound having the structure of Formula IV:
wherein,
D 2 is O or S;
D 3 is O or S;
J 1 is H, CH 3 , CH 2 CH 3 ,
or is absent (+);
R 1 is
M 3 is selected from:
E 8 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, or CF 3 ;
E 9 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, or CF 3 ;
E 10 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, or CF 3 ;
E 11 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, or CF 3 ;
E 12 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, or CF 3 ;
E 13 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, or CF 3 ;
E 14 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, or CF 3 ;
L 8 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, CF 3 , OCF 3 , OCF 2 , S(═O) 2 (NH 2 ), OCH 2 C(CH 3 )(CH 2 ),
L 9 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, CF 3 , OCF 3 , OCF 2 , S(═O) 2 (NH 2 ), OCH 2 C(CH 3 )(CH 2 ),
L 10 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, CF 3 , OCF 3 , OCF 2 , S(═O) 2 (NH 2 ), OCH 2 C(CH 3 )(CH 2 ),
L 11 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, CF 3 , OCF 3 , OCF 2 , S(═O) 2 (NH 2 ), OCH 2 C(CH 3 )(CH 2 ),
L 12 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, CF 3 , OCF 3 , OCF 2 , S(═O) 2 (NH 2 ), OCH 2 C(CH 3 )(CH 2 ),
L 13 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, or CF 3 ; and
L 14 is H, CH 3 , CH 2 CH 3 , F, Cl, Br, or CF 3 ;
wherein the compound is for use in the treatment of one or more of the following: prostate cancer; breast cancer; colon cancer; cervical cancer; small-cell lung carcinoma; neuroblastomas; osteosarcoma; glioblastoma; melanoma; and myeloid leukaemia.
9 . The compound of claim 8 , wherein the compound is selected from one or more of:
10 . A compound of any one of claims 1 - 9 , for use in the treatment of cancer.
11 . The compound of claim 10 , wherein the cancer is selected from one or more of the following: prostate cancer; breast cancer; colon cancer; cervical cancer; small-cell lung carcinoma; neuroblastomas; osteosarcoma; glioblastoma; melanoma; and myeloid leukaemia.
12 . A pharmaceutical composition for treating cancer, comprising compound of any one of claims 1 - 9 and a pharmaceutically acceptable carrier.
13 . The pharmaceutical composition of claim 12 , wherein the cancer is selected from one or more of the following: prostate cancer; breast cancer; colon cancer; cervical cancer; small-cell lung carcinoma; neuroblastomas; osteosarcoma; glioblastoma; melanoma; and myeloid leukaemia.
14 . Use of compound of any one of claims 1 - 9 for treating cancer.
15 . Use of compound of any one of claims 1 - 9 in the manufacture of a medicament for treating cancer.
16 . The use of claim 14 or 15 , wherein the cancer is selected from one or more of the following: prostate cancer; breast cancer; colon cancer; cervical cancer; small-cell lung carcinoma; neuroblastomas; osteosarcoma; glioblastoma; melanoma; and myeloid leukaemia.
17 . A commercial package comprising (a) compound of any one of claims 1 - 9 and a pharmaceutically acceptable carrier; and (b) instructions for the use thereof for treating cancer.
18 . A commercial package comprising (a) a pharmaceutical composition comprising compound of any one of claims 1 - 9 and a pharmaceutically acceptable carrier; and (b) instructions for the use thereof for treating cancer.
19 . The commercial package of claim 17 or 18 , wherein the cancer is selected from one or more of the following: prostate cancer; breast cancer; colon cancer; cervical cancer; small-cell lung carcinoma; neuroblastomas; osteosarcoma; glioblastoma; melanoma; and myeloid leukaemia.
20 . A compound of any one of Formulas I-IV, provided that the compound excludes all of the compounds set out in TABLES 3 and 4.
21 . A compound having the structure
for use in the treatment of cancer.
22 . The compound of claim 21 , wherein the cancer is selected from one or more of the following: prostate cancer; breast cancer; colon cancer; cervical cancer; small-cell lung carcinoma; neuroblastomas; osteosarcoma; glioblastoma; melanoma; and myeloid leukaemia.
23 . A pharmaceutical composition for treating cancer, comprising the compound of claim 21 and a pharmaceutically acceptable carrier.
24 . The pharmaceutical composition of claim 23 , wherein the cancer is selected from one or more of the following: prostate cancer; breast cancer; colon cancer; cervical cancer; small-cell lung carcinoma; neuroblastomas; osteosarcoma; glioblastoma; melanoma; and myeloid leukaemia.
25 . Use of compound having the structure
for treating cancer.
26 . Use of compound having the structure
in the manufacture of a medicament for treating cancer.
27 . The use of claim 25 or 26 , wherein the cancer is selected from one or more of the following: prostate cancer; breast cancer; colon cancer; cervical cancer; small-cell lung carcinoma; neuroblastomas; osteosarcoma; glioblastoma; melanoma; and myeloid leukaemia.Cited by (0)
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