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US 2020/0048220 A1Published application
Bromodomain Inhibitors
OwnerAndrew Bogdan, Steven Fidanze +3inventors
InventorsAndrew Bogdan, Steven Fidanze, Keith McDaniel, John Pratt, Le Wang
Life of this patent
Estimating the term…
Abstract
Provided are compounds of formula (I), wherein R1, Y, X1, X2, R2, R3, R4, R5, R6 and m have any of the values defined in the specification and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising compounds of formula (I).
Claims25
A compound of formula (I) or a pharmaceutically acceptable salt thereof,
- wherein
- R1 is C1-C3 alkyl;
- Y is N or C(RY) wherein RY is hydrogen or C1-C3 alkyl;
- m is 0, 1, 2, 3, or 4;
- R2 is G1A, —N(Ra)S(O)2Rb, —N(Ra)C(O)Rb, or —N(Ra)C(O)ORb;
- Ra, at each occurrence, is independently hydrogen, C1-C6 alkyl, C1-C6 haloalkyl, or —(C2-C6 alkylenyl)-ORx wherein Rx is hydrogen, C1-C6 alkyl, or C1-C6 haloalkyl;
- Rb, at each occurrence, is independently C1-C6 alkyl, C2-C6 alkenyl, C1-C6 haloalkyl, G1B, or —(C1-C6 alkylenyl)-ORj;
- G1A is formula (i)
- wherein
- Z1 is C(O) or C(Re)(Rf);
- Z2 is a bond, O, —(C(Rg)(Rh)p—C(Rm)(Rn)— wherein the left end of the moiety is attached to Z1, or N(Ri) wherein Ri is hydrogen, C1-C3 alkyl, or cyclopropyl;
- wherein the cyclopropyl is optionally substituted with 1, 2, 3, or 4 independently selected Rs groups;
- p is 0 or 1;
- Rc, Rd, Re, Rf, Rg, Rh, Rm, and Rn, are each independently hydrogen, C1-C6 alkyl, C1-C6 haloalkyl, or cyclopropyl;
- wherein the cyclopropyl, at each occurrence, is optionally substituted with 1, 2, 3, or 4 independently selected Rs groups;
- or
- Rc and Rm together with the carbon atoms to which they are attached, form a C3-C6 monocyclic cycloalkyl or a 4-6 membered monocyclic heterocycle;
- wherein the C3-C6 monocyclic cycloalkyl and the 4-6 membered monocyclic heterocycle are each optionally substituted with 1, 2, 3, or 4 independently selected Rs groups;
- or
- Rc and Ri together with the atoms to which they are attached, form a 4-6 membered monocyclic heterocycle;
- wherein the 4-6 membered monocyclic heterocycle is optionally substituted with 1, 2, 3, or 4 independently selected Rs groups;
- or
- Rc and Rd together with the carbon atoms to which they are attached, form a C3-C6 monocyclic cycloalkyl or a 4-6 membered monocyclic heterocycle;
- wherein the C3-C6 monocyclic cycloalkyl and the 4-6 membered monocyclic heterocycle are each optionally substituted with 1, 2, 3, or 4 independently selected Rs groups;
- G1B is oxetanyl, cyclopropyl, cyclobutyl, or cyclopentyl;
- wherein each G1B is optionally substituted with 1, 2, 3, or 4 Rt groups;
- wherein each Rt is independently halogen, C1-C6 alkyl, or C1-C6 haloalkyl;
- each R3 is independently C1-C3 alkyl, C1-C3 haloalkyl, halogen, —CN, —OR3a, —N(R3a)2, —C(O)R3a, cyclopropyl, or cyclobutyl;
- wherein each R3a is independently hydrogen, C1-C3 alkyl, or C1-C3 haloalkyl;
- R4 is phenyl or monocyclic heteroaryl;
- wherein each R4 is substituted with 2, 3, or 4 substituents wherein two of the substituents are independently selected from the group consisting of halogen, C1-C6 alkyl, and C1-C6 haloalkyl, and the optional substituents are independently selected from the group consisting of halogen, —CN, C1-C6 alkyl, C1-C6 haloalkyl, —S(C1-C6 alkyl), —S(O)2(C1-C6 alkyl), and —(C1-C6 alkylenyl)-OH;
- R5 is hydrogen, halogen, —CN, C1-C6 haloalkyl, or C1-C6 alkyl;
- R6 is —(C1-C3 alkylenyl)n-S(O)2—R6a or —N(R6b)—SO2—R6c;
- n is 0 or 1;
- R6a and R6c are each independently C1-C6 alkyl, C1-C6 haloalkyl, or cyclopropyl;
- wherein the cyclopropyl is optionally substituted with 1, 2, 3, or 4 substituents independently selected from the group consisting of halogen, C1-C6 alkyl, and C1-C6 haloalkyl;
- R6b is hydrogen, C1-C6 alkyl, or C1-C6 haloalkyl;
- X1 and X2 are C(R7) or
- one of X1 and X2 is N and the other is C(R7);
- R7, at each occurrence, is independently hydrogen or halogen;
- Rs, at each occurrence, is independently C1-C6 alkyl, halogen, or C1-C6 haloalkyl;
- Rj, at each occurrence, is independently hydrogen, C1-C6 alkyl, or C1-C6 haloalkyl;
- and
- Rk, at each occurrence, is independently C1-C6 alkyl or C1-C6 haloalkyl.
41 more elements
Dependencies are inferred from the claim text.