ACRYLIC-CONTAINING NUCLEAR TRANSPORT MODULATORS AND APPLICATION THEREOF Russian patent published in 2025 - IPC C07D403/12 C07D401/12 C07D413/12 C07D471/10 C07D487/10 C07D498/10 C07D491/107 A61K31/4196 A61K31/397 A61K31/45 A61K31/496 A61K31/501 A61K31/513 A61K31/55 A61K31/4985 A61P35/00 

Abstract RU 2838463 C2

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formulas (1C):

(1C) or a pharmaceutically acceptable salt thereof, where: n is equal to 1; Y is selected from a group consisting of a bond, -CH2-, -CO-, -SO2-, and -COCON(R8)-; wherein R8 is H, or C1-C3 alkyl; and R7 is selected from the group consisting of H, C1-C3 alkyl, C3 cycloalkyl, and 6-member heteroaryl containing 1-2 N heteroatoms, optionally substituted with a halogen;

(1AA) or a pharmaceutically acceptable salt thereof, where: m is equal to 0, 1, 2 or 3; Ra, Rb, Rc and Rd are independently selected from a group consisting of H, halogen, OCH2CF3, OH, NMe2, R3 and OR3; wherein R3 is C1-C3 alkyl group or C3 cycloalkyl group; or Ra and Rb together with a carbon atom bonded thereto, form a C3 cycloalkyl group or 4–6-membered non-aromatic heterocycle containing 1 N heteroatom, optionally substituted CH3 or COCH3; or Rc and Rd together with a carbon atom bonded to them, form a C3-C6 cycloalkyl group or 4–6-membered non-aromatic heterocycle containing 1 N or O heteroatom, optionally substituted CH3 or COCH3; or Ra (or Rb) and Rc (or Rd) together with the C-C bond bonded thereto, form C3-C6 cycloalkyl;

(1AB) or a pharmaceutically acceptable salt thereof, where: n is 1 or 2; Re and Rf are independently selected from a group consisting of H, OCH2CF3, OCH2CH2OCH3, O-CD3, R3 and OR3; wherein R3 is C1-C3 alkyl, or C3 cycloalkyl;

(1AC) or a pharmaceutically acceptable salt thereof, where: M is -O-, -NR3- or -CO-, wherein R3 is C1-C3 alkyl or COCH3; Rg, Rh, Ri and Rj are H; or Rg and Rh together represent a -CO- group; or Ri and Rj together represent a -CO- group, or Ri and Rj together with the carbon atom bonded thereto form C3 cycloalkyl;

(1BA) or a pharmaceutically acceptable salt thereof, where: n is 1 or 2; Q is -CH2- or -CO-; R9 is selected from the group consisting of H, C1-C3 alkyl, deuterated C1-C3 alkyl, C3-C6 cycloalkyl, amino-substituted C1-C3 alkylamino, C1-substituted C1-C3 alkyl, C3 substituted C1-C3 alkyl, 6-member heteroaryl and 5–7-member non-aromatic heterocycle containing 1 heteroatom N, optionally substituted with CH3.

EFFECT: novel compounds which can be used to treat or prevent diseases associated with physiological conditions associated with the CRM1 protein are obtained.

7 cl, 2 dwg, 7 tbl, 108 ex

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RU 2 838 463 C2

Authors

Fan, Houxing

Xie, Yuli

Dates

2025-04-16Published

2020-02-25Filed