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US 2020/0345860 A1Published application
Compounds and compositions for immunotherapy
AssigneeBirdie Biopharmaceuticals, Inc.
InventorLixin Li
Life of this patent
Estimating the term…
Abstract
The present invention relates to compounds for targeted immunotherapy, as well as compositions comprising the same. Further, the present invention relates to the use of the compounds in the treatment of diseases such as cancer.
Claims28
A compound having the structure of Formula (Ib):
- TM-L-AM (Ib),
- wherein TM is a targeting moiety that comprises an immunoglobulin that specifically binds to an antigen that is expressed on a tumor cell that is able to inhibit cell growth or proliferation, or induce apoptosis, directly or indirectly;
- L is a linker;
- and AM is a radical of an activating moiety that is represented by structure of formula (I) or (II):
- wherein dashed line represents a bond or absence of the bond, is the point to be connected to the linker;
- X is S or —NR1, R1 is —W0-W1-W2-W3-W4,
- W0 is a bond, alkyl, alkenyl, alkynyl, alkoxy, or -alkyl-S-alkyl-,
- W1 is a bond, —O—, or —NR2—, wherein R2 is hydrogen, alkyl or alkenyl,
- W2 is a bond, —O—, —C(O)—, —C(S)—, or —S(O)2—,
- W3 is a bond, —NR3—, wherein R3 is hydrogen, alkyl or alkenyl,
- W4 is hydrogen, alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, aryl, aryloxy, heteroaryl, or heterocyclyl, each of which is optionally substituted by one or more substituents selected from the group consisting of hydroxyl, alkoxy, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, heterocyclyl, —NH2, nitro, -alkyl-hydroxyl, -alkyl-aryl, -alkyl-heteroaryl, -alkyl-heterocyclyl, —O—R4, —O-alkyl-R4, -alkyl-O—R4, —C(O)—R4, -alkyl-C(O)—R4, -alkyl-C(O)—O—R4, —C(O)—O—R4, —S—R4, —S(O)2—R4, —NH—S(O)2—R4, -alkyl-S—R4, -alkyl-S(O)2—R4, —NHR4, —NR4R4, —NH-alkyl-R4, halogen, —CN, —NO2, and —SH, wherein R4 is independently hydrogen, alkyl, alkenyl, -alkyl-hydroxyl, aryl, heteroaryl, heterocyclyl, or haloalkyl;
- Z is hydrogen, alkyl, alkenyl, alkynyl, alkoxy, aryl, haloalkyl, heteroaryl, heterocyclyl, each of which can be optionally substituted by one or more substituents selected from the group consisting of hydroxyl, alkoxy, alkyl, alkenyl, alkynyl, aryl, heteroaryl, heterocyclyl, halogen, cyano, nitro, —N(R5)2, -alkoxy-alkyl, -alkoxy-alkenyl, —C(O)-alkyl, —C(O)—O-alkyl, —O—C(O)-alkyl, —C(O)—N(R5)2, aryl, heteroaryl, —CO-aryl, and —CO-heteroaryl, wherein each R5 is independently hydrogen, alkyl, haloalkyl, -alkyl-aryl, or -alkyl-heteroaryl;
- R is hydrogen, alkyl, alkoxy, haloalkyl, halogen, aryl, heteroaryl, heterocyclyl, each of which is optionally substituted by one or more substituents selected from the group consisting of hydroxyl, alkoxy, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, heterocyclyl, —NH2, nitro, -alkyl-hydroxyl, -alkyl-aryl, -alkyl-heteroaryl, -alkyl-heterocyclyl, —O—R4, —O-alkyl-R4, -alkyl-O—R4, —C(O)—R4, —C(O)—NH—R4, —C(O)—NR4R4, -alkyl-C(O)—R4, -alkyl-C(O)—O—R4, —C(O)—O—R4, —O—C(O)—R4, —S—R4, —C(O)—S—R4, —S—C(O)—R4, —S(O)2—R4, —NH—S(O)2—R4, -alkyl-S—R4, -alkyl-S(O)2—R4, —NHR4, —NR4R4, —NH-alkyl-R4, halogen, —CN, and —SH, wherein R4 is independently hydrogen, alkyl, alkenyl, alkoxy, -alkyl-hydroxyl, aryl, heteroaryl, or haloalkyl;
- n is 0, 1, 2, 3, or 4;
- Y is —NR6R7, —CR6R7R, or -alkyl-NH2, each of which can be optionally substituted by one or more substituents selected from the group consisting of hydroxyl, alkoxy, alkyl, alkenyl, alkynyl, —NH2, halogen, —N(R5)2, -alkoxy-alkyl, -alkoxy-alkenyl, —C(O)-alkyl, —C(O)—O-alkyl, —C(O)—N(R5)2, aryl, heteroaryl, —CO-aryl, and —CO-heteroaryl,
- wherein R6, R7 and R8 are independently hydrogen, alkyl, alkenyl, alkoxy, alkylamino, dialkylamino, alkylthio, arylthio, -alkyl-hydroxyl, -alkyl-C(O)—O—R9, -alkyl-C(O)—R9, or -alkyl-O—C(O)—R9, wherein each R5 is independently hydrogen, alkyl, haloalkyl, -alkyl-aryl, or -alkyl-heteroaryl, wherein R9 is hydrogen, alkyl, alkenyl, halogen, or haloalkyl;
- X and Z taken together may optionally form a (5-9)-membered ring;
- or a pharmaceutically acceptable salt or solvate thereof.
15 more elements
Dependencies are inferred from the claim text.