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US 2014/0235581 A1Published application
Composition for preventing and treating non-small cell lung cancer, containing pyrazino-triazine derivatives
AssigneeJw Pharmaceutical Corporation
InventorsJoo-Young Cha, Kwan-Hoo Lee, Ji-Eun Jung
Life of this patent
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Abstract
Disclosed is a composition comprising a pyrazino-triazine derivative, an isomer thereof or a pharmaceutically acceptable salt thereof. It is very effective for preventing and treating NSCLC.
Claims14
1-14. (canceled)
15:
- A method for preventing or treating NSCLC (non-small cell lung cancer), comprising administering a therapeutically effective amount of a compound represented by the following Chemical Formula 1, an isomer thereof, and a pharmaceutically acceptable salt thereof to a subject in need thereof:
- wherein,
- R1 is substituted or unsubstituted C3-C10 aryl or substituted or unsubstituted C3-C10 heteroaryl with at least one nitrogen (N) atom;
- R3 is hydrogen, C1˜C6 alkyl, C2˜C6 alkenyl, C2˜C6 alkynyl, C3˜C6 aryl, C3˜C10 heteroaryl with at least one N atom, C3˜C10 arylalkyl or C3˜C10 heteroarylalkyl with at least one N atom;
- A is hydrogen or C1˜C6 alkyl;
- B is hydrogen or C1˜C6 alkyl;
- X is —O—PO3H2 or —OH;
- and
- Y is hydrogen, C3˜C10 aryl, C3˜C10 heteroaryl with at least one N atom or C1˜C6 alkyl.
6 more elements
16:
- The method of claim 15, wherein the substituted C3˜C10 aryl or the substituted C3˜C10 heteroaryl with at least one N atom has at least one substituent selected from the group consisting of C1˜C6 alkyl,
- wherein Ra and Rb may be independently hydrogen, C1˜C6 alkyl, pyridinyl or amino-substituted pyridinyl, and may be condensed together to form a ring.
17:
- The method of claim 15, wherein,
- R1 is naphthyl, quinolinyl, indolyl, substituted naphthyl, substituted quinolinyl or substituted indolyl,
- wherein the substituted naphthyl, the substituted quinolinyl and the substituted indolyl have at least one substituent selected from C1˜C6 alkyl,
- wherein Ra and Rb may be independently hydrogen, C1˜C6 alkyl, pyridinyl or amino-substituted pyridinyl and may be condensed together to form a ring;
- R3 is methyl or propenyl;
- either or both of A and B is hydrogen;
- X is —O—PO3H2 or —OH;
- and
- Y is hydrogen.
6 more elements
18:
- The method of claim 17, wherein the substituted naphthyl, the substituted quinolinyl or the substituted indolyl has at least one substituent selected from
19:
- The method of claim 15, wherein,
- R1 is
- R3 is
- or methyl;
- either or both of A and B is hydrogen;
- X is —O—PO3H2 or —OH;
- and
- Y is hydrogen.
5 more elements
20:
- The method of claim 15, wherein the compound of Chemical Formula 1 is selected from the group consisting of the compound represented by one of the following Chemical Formulas 2 to 11, an isomer thereof, and a pharmaceutically acceptable salt thereof:
- No.
- Chemical Formula
- 2
- 3
- 4
- 5
- 6
- 7
- 8
- 9
- 10
- 11
10 more elements
21:
- The method of claim 15, wherein the compound of Chemical Formula 1 is selected from the group consisting of the compound represented by following Chemical Formulas 1-1 or 1-1P, an isomer thereof, and a pharmaceutically acceptable salt thereof:
22:
- The method of claim 15, wherein the compound of Chemical Formula 1 is selected from the group consisting of the compound represented by one of the following Chemical Formulas 1-2 to 1-7, an isomer thereof, and a pharmaceutically acceptable salt thereof:
- No.
- Chemical Formula
- 1-2
- 1-3
- 1-4
- 1-5
- 1-6
- 1-7
6 more elements
23:
- The method of claim 15, wherein the compound of Chemical Formula 1 is selected from the group consisting of the compound represented by one of the following Chemical Formulas 2-1 to 2-8, an isomer thereof, and a pharmaceutically acceptable salt thereof:
- No.
- Chemical Formula
- 2-1
- 2-2
- 2-3
- 2-4
- 2-5
- 2-6
- 2-7
- 2-8
8 more elements
24:
- The method of claim 15, wherein the NSCLC is cancer occurring in a patient having wild-type EGFR (epithelial growth factor receptor) or an active mutation on EGFR.
25:
- The method of claim 15, wherein the NSCLC is EGFR TKI (Epidermal Growth Factor Receptor tyrosine kinase inhibitor)-resistant cancer.
26:
- The method of claim 25, wherein the EGFR TKI-resistant cancer is cancer occurring in a patient having mutant EGFR.
27:
- The method of claim 26, wherein the mutant EGFR has a double mutation of L858R and T790M.