Invention Grant
- Patent Title: Pharmacophores, compounds and methods having application in the treatment of cancer through inhibition of CYP17A1 and CYP19A1
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Application No.: US15769824Application Date: 2016-10-22
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Publication No.: US11548860B2Publication Date: 2023-01-10
- Inventor: Njabulo Joyfull Gumede
- Applicant: MANGOSUTHU UNIVERSITY OF TECHNOLOGY
- Applicant Address: ZA Durban
- Assignee: MANGOSUTHU UNIVERSITY OF TECHNOLOGY
- Current Assignee: MANGOSUTHU UNIVERSITY OF TECHNOLOGY
- Current Assignee Address: ZA Durban
- Agency: Grossman, Tucker, Perreault & Pfleger, PLLC
- Priority: ZA2015/07849 20151022
- International Application: PCT/ZA2016/050041 WO 20161022
- International Announcement: WO2017/070718 WO 20170427
- Main IPC: C07D265/36
- IPC: C07D265/36 ; C07D413/12 ; C07D231/56 ; C07C311/29 ; C07D417/12 ; C07D405/14 ; C07D309/34 ; C07C233/43 ; G16B50/30 ; G16B50/10 ; G16B50/20 ; C07C237/22 ; C07D417/02

Abstract:
The invention provides compounds for use as medicaments, which act by inhibiting CYP17A1 and CYP19A1 enzymes. The compounds have particular application in the treatment of cancer especially prostate cancer and breast cancer. The compounds have the formula: [Chem. 1] wherein: R is independently selected from the group consisting of optionally substituted arylamide; optionally substituted alkylarylamide; optionally substituted aryl carboxamide; optionally substituted cyanopiperidine; optionally substituted oxopiperidine; optionally substituted N-(pyridin-3-yl); optionally substituted pyridin-3-yl; optionally substituted pyrazole-4-carboxamide; optionally substituted pyrimidin-4-ylcarboxamide; optionally substituted pyrimidin-4-ylcarboxamide; optionally substituted 1H-pyrrol-2-ylcarboxamide; optionally substituted morpholin carboxamide; optionally substituted 1H-indazol-3-ylcarboxamide; optionally substituted 5-cyanopiperidin-3-ylcarboxamide; optionally substituted quinolin-7-yl; optionally substituted pyrazin-2-ylcarboxamide; optionally substituted 1H-1,3-benzodiazole-6-carboxamide; and optionally substituted 3-oxo-3,4-dihydro-2H-1,4-benzoxazin-7-ylcarboxamide; Each R1, R2, R3, R4, R5 is independently selected from the group consisting of H; OH; a halogen atom; OCH3; and NH2; and X is independently selected from the group consisting of O, H and OH. Some of the compounds are claimed per se and the invention also encompasses pharmaceutically acceptable salts, solvates, hydrates, primary metabolites and prodrugs thereof.
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