Methods for treatment of diseases related to activated lymphocytes
AssigneeImmune Control, Inc.
InventorsStephen Roth, Clayton Buck, Christopher Self, Gary Olson
Life of this patent
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Abstract
The present invention relates to inhibiting proliferation and inducing apoptosis in activated lymphocytes, including T cells and B cells. The invention also provides compositions and methods for inhibiting proliferation and inducing apoptosis in activated lymphocytes, as well methods for treating diseases associated with activated lymphocytes by administering 5-HT receptor antagonists.
Claims11
A method of inducing apoptosis in an immune cell, the method comprising contacting the immune cell with a compound of formula I:
- or a pharmaceutically acceptable salt thereof, wherein:
- R1 is independently selected at each occurrence from hydrogen, halogen, (C1-C6)alkyl;
- (C1-C6)alkenyl;
- (C1-C6)alkoxy;
- OH;
- NO2;
- C≡N;
- C(═O)OR7;
- C(═O)NR72;
- NR72;
- NR7C(═O)(C1-C6)alkyl;
- NR7C(═O)O(C1-C6)alkyl;
- NR7C(═O)NR72;
- NR7SO2(C1-C6)alkyl;
- SO2NR72;
- OC(═O)(C1-C6)alkyl;
- O(C2-C6)alkylene-NR72;
- (C2-C6)alkylene-OR7;
- and (C1-C3)perfluoroalkyl;
- R2 is independently selected at each occurrence from hydrogen, halogen, (C1-C6)alkyl;
- (C1-C6)alkenyl;
- (C1-C6)alkoxy;
- OH;
- NO2;
- C≡N;
- C(═O)OR7;
- C(═O)NR72;
- NR72;
- NR7C(═O)(C1-C6)alkyl;
- NR7C(═O)O(C1-C6)alkyl;
- NR7C(═O)NR72;
- NR7SO2(C1-C6)alkyl;
- SO2NR72;
- OC(═O)(C1-C6)alkyl;
- O(C2-C6)alkylene-NR72;
- (C2-C6)alkylene-OR7;
- and (C1-C3)perfluoroalkyl;
- R3 is hydrogen, C(═O)OR7, or C(═O)NR72;
- A1 is CH2 or NR4;
- A2 is CH or N;
- provided that if A1 is CH2, then A2 is N, and if A2 is CH, then A1 is NR4;
- R4 is (CH2)pNHC(O)R5;
- (CH2)pO(CH2)pOR7;
- (CH2)pO(CH2)pNR72;
- (CH2)pNR4(CH2)pNR72;
- (CH2)pO(CH2)pNHC(O)R5;
- (CH2)pNR7(CH2)pNHC(O)R5;
- (CH2)qC(═O)OR7;
- (CH2)qC(═O)NR72;
- (CH2)pO(CH2)qC(═O)OR7;
- (CH2)pO(CH2)qC(═O)NR72;
- (CH2)pNR7(CH2)qC(═O)OR7;
- or (CH2)pNR7(CH2)qC(═O)NR72;
- R5 is (C1-C6)alkyl;
- NR7C(═O)(C1-C6)alkyl;
- NR7C(═O)O(C1-C6)alkyl;
- NR7C(═O)NR72;
- CH(R6)NR72;
- CH(R6)NR7C(═O)(C1-C6)alkyl;
- or CH(R6)NR7C(═O)O(C1-C6)alkyl;
- R6 is H, (C1-C6)alkyl;
- (C2-C6)alkylene-OR7;
- (CH2)qC(═O)OR7;
- or (CH2)qC(═O)NR72;
- R7 is independently selected at each occurrence from the group consisting of hydrogen and (C1-C6)alkyl;
- m is independently at each occurrence 1, 2, or 3;
- n is 0, 1, or 2;
- p is independently at each occurrence 2 or 3;
- and
- q is independently at each occurrence 1 or 2.
A method of inducing apoptosis in a lymphocyte, the method comprising contacting the lymphocyte with a compound of formula I.
A method of inhibiting proliferation of a lymphocyte, the method comprising contacting the lymphocyte with a compound of formula I.
Dependencies are inferred from the claim text.