Therapeutic agents
AssigneeThe Trustees of the University of Pennsylvania
InventorsHarvey Rubin, Takahiro Yano, Sacha Kassovska-Bratinova, Norman Schechter, Jiah Shin Teh, Jeffrey Winkler
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Abstract
The present invention includes a method of treating or preventing a disease or disorder such as a mycobacterial infection, a Gram-positive bacterium infection, a yeast infection, an inflammatory condition, an auto-immune disorder and/or a proliferative disorder in a subject in need thereof. The method comprises administering to the subject a therapeutically effective amount of at least one compound of the invention, which includes clofazimine derivatives.
Claims11
A compound of formula (I), or a salt or solvate thereof:
- wherein:
- each occurrence of R1 and R2 is independently selected from the group consisting of F, Cl, Br, I, CN, NO2, OR5, SR5, S(═O)R6, S(═O)2R6, NHS(═O)2R6, C(═O)R5, OC(═O)R5, CO2R5, OCO2R6, N(R5)2, C(═O)N(R5)2, OC(═O)N(R5)2, NHC(═O)NH(R5), NHC(═O)R5, NHC(═O)OR5, C1-C6 alkyl, C1-C6 fluoroalkyl and C1-C6 heteroalkyl;
- each occurrence of R3 is independently selected from the group consisting of N(R5), CH2N(R5), O, and CH2O;
- R4 is selected from the group consisting of (CH2)mOR5, and (CH2)mN(R5)2;
- each occurrence of R5 is independently selected from the group consisting of H, C1-C6 alkyl, C1-C6 fluoroalkyl, C1-C6 heteroalkyl, C3-C10 cycloalkyl, C2-C10 heterocycloalkyl, aryl, heteroaryl, C1-C4 alkyl-(C3-C10 cycloalkyl), C1-C4 alkyl-(C2-C10 heterocycloalkyl), C1-C4 alkyl-(aryl), and C1-C4 alkyl-(heteroaryl);
- each occurrence of R6 is independently selected from the group consisting of C1-C6 alkyl, C1-C6 fluoroalkyl, C1-C6 heteroalkyl, C3-C10 cycloalkyl, C2-C10 heterocycloalkyl, aryl, heteroaryl, C1-C4 alkyl-(C3-C10 cycloalkyl), C1-C4 alkyl-(C2-C10 heterocycloalkyl), C1-C4 alkyl-(aryl), and C1-C4 alkyl-(heteroaryl);
- each occurrence of x and y is independently selected from the group consisting of 0, 1, 2, and 3;
- n is an integer ranging from 2 to 4;
- and m is an integer ranging from 0 to 3.
A compound of formula (I), or a salt or solvate thereof:
- wherein:
- each occurrence of R1 and R2 is independently selected from the group consisting of F, Cl, Br, I, CN, NO2, OR5, SR5, S(═O)R6, S(═O)2R6, NHS(═O)2R6, C(═O)R5, OC(═O)R5, CO2R5, OCO2R6, N(R5)2, C(═O)N(R5)2, OC(═O)N(R5)2, NHC(═O)NH(R5), NHC(═O)R5, NHC(═O)OR5, C1-C6 alkyl, C1-C6 fluoroalkyl and C1-C6 heteroalkyl;
- each occurrence of R3 is independently selected from the group consisting of N(R5), CH2N(R5), O, and CH2O;
- R4 is (CH2)mNR5(C═NR5)N(R5)2;
- each occurrence of R5 is independently selected from the group consisting of H, C1-C6 alkyl, C1-C6 fluoroalkyl, C1-C6 heteroalkyl, C3-C10 cycloalkyl, C2-C10 heterocycloalkyl, aryl, heteroaryl, C1-C4 alkyl-(C3-C10 cycloalkyl), C1-C4 alkyl-(C2-C10 heterocycloalkyl), C1-C4 alkyl-(aryl), and C1-C4 alkyl-(heteroaryl);
- each occurrence of R6 is independently selected from the group consisting of C1-C6 alkyl, C1-C6 fluoroalkyl, C1-C6 heteroalkyl, C3-C10 cycloalkyl, C2-C10 heterocycloalkyl, aryl, heteroaryl, C1-C4 alkyl-(C3-C10 cycloalkyl), C1-C4 alkyl-(C2-C10 heterocycloalkyl), C1-C4 alkyl-(aryl), and C1-C4 alkyl-(heteroaryl);
- each occurrence of x and y is independently selected from the group consisting of 0, 1, 2, and 3;
- n is an integer ranging from 0 to 4;
- and
- m is an integer ranging from 0 to 3.
Dependencies are inferred from the claim text.