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US 2016/0184274 A1Published application
Methods for inhibiting mesenchymal phenotype after epithelial-to-mesenchymal transition
OwnerJuan Saus, Fernando Revert +7inventors
InventorsJuan Saus, Fernando Revert, Aida Artigot, Francisco Revert-Ros, Ernesto Lopez-Pascual, Raul Blasco, Nuria Roda, Juan F. Sanz-Cervera, Roberto Gozalbo-Rovira
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Abstract
Methods of using inhibitors of Goodpasture Antigen Binding Protein for inhibiting mesenchymal phenotype after epithelial-to-mesenchymal transition (EMT), treating an invasive tumor, and detecting EMT in a tissue are described.
Claims21
A method for inhibiting mesenchymal phenotype after epithelial-to-mesenchymal transition (EMT), or for treating an invasive tumor, comprising administering to a subject in need thereof an amount effective to inhibit mesenchymal phenotype after EMT, or to treat an invasive tumor, of an antibody selective for Goodpasture Antigen Binding Protein (GPBP), or a compound of formula:
- or a pharmaceutically acceptable salt thereof, wherein:
- R is selected from N and CR5;
- R5 is selected from the group consisting of hydrogen, halogen, cyano, nitro, hydroxy, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo(C1-C6 alkyl), C1-C6 alkoxy, halo(C1-C6 alkoxy), amino, (C1-C6 alkyl)amino, di(C1-C6 alkyl)amino, hydroxy(C1-C6 alkyl), (C1-C6 alkoxy)C1-C6 alkyl, amino(C1-C6 alkyl), sulfanyl(C1-C6 alkyl), (C1-C6 alkyl)sulfanyl(C1-C6 alkyl), —(CH2)1-5—C(O)(C1-C6 alkoxy), —(CH2)1-5—C(O)NH2, (aryl)C2-C6 alkyl, and (heteroaryl)C1-C6 alkyl;
- R1 is hydrogen, halogen, hydroxy, C1-C6 alkyl, halo(C1-C6 alkyl), C1-C6 alkoxy, halo(C1-C6 alkoxy), hydroxy(C1-C6 alkyl), (C1-C6 alkoxy)C1-C6 alkyl, amino(C1-C6 alkyl), sulfanyl(C1-C6 alkyl), or (C1-C6 alkyl)sulfanyl(C1-C6 alkyl);
- R2 is C1-C6 alkyl, halo(C1-C6 alkyl), C1-C6 alkoxy, halo(C1-C6 alkoxy), hydroxy(C1-C6 alkyl), (C1-C6 alkoxy)C1-C6 alkyl, formyl(C0-C6 alkyl), amino(C1-C6 alkyl), sulfanyl(C1-C6 alkyl), (C1-C6 alkyl)sulfanyl(C1-C6 alkyl), —(CH2)1-5—C(O)OH, —(CH2)1-5—C(O)(C1-C6 alkoxy), —(CH2)1-5—C(O)NH2, (aryl)C1-C6 alkyl, or (heteroaryl)C1-C6 alkyl;
- R3 is C1-C6 alkyl, halo(C1-C6 alkyl), C1-C6 alkoxy, halo(C1-C6 alkoxy), hydroxy(C1-C6 alkyl), (C1-C6 alkoxy)C1-C6 alkyl, formyl(C1-C6 alkyl), amino(C1-C6 alkyl), sulfanyl(C1-C6 alkyl), (C1-C6 alkyl)sulfanyl(C1-C6 alkyl), —(CH2)1-5—C(O)OH, —(CH2)1-5—C(O)(C1-C6 alkoxy), —(CH2)1-5—C(O)NH2, —(CH2)1-5—C(O)NH(C1-C6 alkyl), —(CH2)1-5—C(O)N(C1-C6 alkyl)2, —CH═CH—C(O)OH, —CH═CH—C(O)(C1-C6 alkoxy), (aryl)C1-C6 alkyl, or (heteroaryl)C1-C6 alkyl;
- and
- R4 is hydroxy, halogen, C1-C6 alkyl, C1-C6 alkoxy, halo(C1-C6 alkoxy), benzyloxy, —(CH2)1-5—C(O)OH, —(CH2)1-5—C(O)(C1-C6 alkoxy), —(CH2)1-5—C(O)NH2, —(CH2)1-5—C(O)NH(C1-C6 alkyl), —(CH2)1-5—C(O)N(C1-C6 alkyl)2, —CH═CH—C(O)OH, —CH═CH—C(O)(C1-C6 alkoxy), —O(CH2)1-5—C(O)OH, —O(CH2)1-5—C(O)(C1-C6 alkoxy), (aryl)C1-C6 alkyl, or (heteroaryl)C1-C6 alkyl.
5 more elements
A method for detecting EMT in a tissue, comprising
- (a) contacting a tissue in a subject with an amount effective to label the tissue of a detectably labeled compound of formula:
- or a pharmaceutically acceptable salt thereof, wherein:
- R is selected from N and CR5;
- R5 is selected from the group consisting of hydrogen, halogen, cyano, nitro, hydroxy, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo(C1-C6 alkyl), C1-C6 alkoxy, halo(C1-C6 alkoxy), amino, (C1-C6 alkyl)amino, di(C1-C6 alkyl)amino, hydroxy(C1-C6 alkyl), (C1-C6 alkoxy)C1-C6 alkyl, amino(C1-C6 alkyl), sulfanyl(C1-C6 alkyl), (C1-C6 alkyl)sulfanyl(C1-C6 alkyl), —(CH2)1-5—C(O)(C1-C6 alkoxy), —(CH2)1-5—C(O)NH2, (aryl)C2-C6 alkyl, and (heteroaryl)C1-C6 alkyl;
- R1 is hydrogen, halogen, hydroxy, C1-C6 alkyl, halo(C1-C6 alkyl), C1-C6 alkoxy, halo(C1-C6 alkoxy), hydroxy(C1-C6 alkyl), (C1-C6 alkoxy)C1-C6 alkyl, amino(C1-C6 alkyl), sulfanyl(C1-C6 alkyl), or (C1-C6 alkyl)sulfanyl(C1-C6 alkyl);
- R2 is C1-C6 alkyl, halo(C1-C6 alkyl), C1-C6 alkoxy, halo(C1-C6 alkoxy), hydroxy(C1-C6 alkyl), (C1-C6 alkoxy)C1-C6 alkyl, formyl(C0-C6 alkyl), amino(C1-C6 alkyl), sulfanyl(C1-C6 alkyl), (C1-C6 alkyl)sulfanyl(C1-C6 alkyl), —(CH2)1-5—C(O)OH, —(CH2)1-5—C(O)(C1-C6 alkoxy), —(CH2)1-5—C(O)NH2, (aryl)C1-C6 alkyl, or (heteroaryl)C1-C6 alkyl;
- R3 is C1-C6 alkyl, halo(C1-C6 alkyl), C1-C6 alkoxy, halo(C1-C6 alkoxy), hydroxy(C1-C6 alkyl), (C1-C6 alkoxy)C1-C6 alkyl, formyl(C1-C6 alkyl), amino(C1-C6 alkyl), sulfanyl(C1-C6 alkyl), (C1-C6 alkyl)sulfanyl(C1-C6 alkyl), —(CH2)1-5—C(O)OH, —(CH2)1-5—C(O)(C1-C6 alkoxy), —(CH2)1-5—C(O)NH2, —(CH2)1-5—C(O)NH(C1-C6 alkyl), —(CH2)1-5—C(O)N(C1-C6 alkyl)2, —CH═CH—C(O)OH, —CH═CH—C(O)(C1-C6 alkoxy), (aryl)C1-C6 alkyl, or (heteroaryl)C1-C6 alkyl;
- and
- R4 is hydroxy, halogen, C1-C6 alkyl, C1-C6 alkoxy, halo(C1-C6 alkoxy), benzyloxy, —(CH2)1-5—C(O)OH, —(CH2)1-5—C(O)(C1-C6 alkoxy), —(CH2)1-5—C(O)NH2, —(CH2)1-5—C(O)NH(C1-C6 alkyl), —(CH2)1-5—C(O)N(C1-C6 alkyl)2, —CH═CH—C(O)OH, —CH═CH—C(O)(C1-C6 alkoxy), —O(CH2)1-5—C(O)OH, —O(CH2)1-5—C(O)(C1-C6 alkoxy), (aryl)C1-C6 alkyl, or (heteroaryl)C1-C6 alkyl;
- for a time and under conditions suitable to promote binding of the detectably labeled compound to the tissue;
- and
- (b) detecting the detectably labeled compound bound to the tissue, thereby detecting EMT in the tissue,
9 more elements
Dependencies are inferred from the claim text.