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US 2024/0254113 A1Published application
Compounds and their uses as cd38 inhibitors
OwnerJianbei Xi, Guohuang Fan +2inventors
InventorsJianbei Xi, Guohuang Fan, Jianfei Wang, Kin Chiu Fong
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Abstract
Provided are compounds of Formula I which can be used as CD38 inhibitors; methods for the production of the compounds; pharmaceutical compositions comprising the compounds; as well as uses and methods for treating a disease mediated by CD38 by administering the compounds.
Claims22
A compound of formula I:
- wherein
- A1 is halogen;
- or 5 or 6 membered unsaturated monocyclic heterocycle containing 1 to 3 heteroatoms selected from the group consisting of N, O and S, and optionally substituted with one or two C1-6 alkyl optionally substituted with 1, 2 or 3 halogen;
- A2 is
- optionally having one or two carbon atoms replaced with nitrogen;
- wherein A2 is optionally substituted with 0 or 1 —OH;
- —CN;
- halogen;
- C1-6 alkyl optionally substituted with 1, 2 or 3 halogen;
- C2-6 alkynyl;
- 6 alkoxy;
- C3-6 cycloalkoxy, in which the cycloalkyl optionally has one carbon atom replaced with O or S:
- —NR1R2, in which each of R1 and R2 independently is H, C1-6 alkyl, —C(O)C1-6 alkyl;
- in which
- is a 5 or 6 membered saturated or unsaturated heterocycle containing 1 to 3 heteroatoms selected from the group consisting of N, O and S, and optionally substituted with 1-2 C1-6 alkyl;
- A3 is selected from the group consisting of
- C1-6 alkyl;
- —(CHR3)n—C3-8 cycloalkyl, in which the C3-8 cycloalkyl optionally has one or two carbon atoms replaced with N, O or S, n is 0, 1 or 2, and R3 is H or C1-6 alkyl;
- or
- in which the phenyl optionally has one or two carbon atoms replaced with N, k is 0, 1 or 2;
- wherein A3 is optionally substituted with 0, 1 or 2 substituents independently selected from the group consisting of —OH;
- —CN;
- —OCH2CH2OCH3;
- —CO—C1-6 alkyl;
- halogen;
- C1-6 alkyl optionally substituted with 1-3 halogen, methoxy or hydroxy;
- C1-6 alkoxy optionally substituted with NH2, dimethylamino, hydroxy or carboxy;
- C3-6 cycloalkoxy;
- or C3-8 cycloalkyl, in which the C3-8 cycloalkyl optionally has one or two carbon atoms replaced with N, O or S amd is optionally substituted with 1-3 halogen, C1-6 alkyl, C1-6 alkyl or hydroxy;
- R is H or C1-6 alkyl;
- or a pharmaceutically acceptable salt, ester, stereoisomer, tautomer, solvate, prodrug, or combination thereof.
28 more elements
Dependencies are inferred from the claim text.