AMINOPYRIDINE DERIVATIVES AND THEIR USE AS SELECTIVE ALK-2 INHIBITORS Russian patent published in 2021 - IPC C07D401/10 C07D401/12 C07D401/14 C07D405/14 C07D409/14 C07D411/14 C07D413/10 A61K31/4427 A61P19/00 

Abstract RU 2747318 C2

FIELD: pharmacology.

SUBSTANCE: invention relates to a compound of Formula (I) in free form or in the form of a pharmacologically acceptable salt

(I),

wherein L represents a relationship, (CH2)n, –CH(CH3)–, –O–(CH2)n–, –C(O)–, –C(O)–NH–(CH2)n–; n equals 1, 2 or 3; R1 is C3–C7cycloalkyl, optionally substituted once or more than once by a substituent independently selected from hydroxyl, halogen, C1–C3alkyl; or bridged C5–C10cycloalkyl, optionally substituted once or more than once by a substituent independently selected from hydroxyl and hydroxyC1–C3alkyl; R2 and R3 are independently selected from H, halogen and C1–C3alkyl; R4 is an N-containing heterocyclic non-aromatic ring, optionally containing one or more additional heteroatoms selected from N, O or S, where the specified ring is optionally substituted once or more than once by R7; each R7 is independently selected from C1–C3alkyl, hydroxyC1–C3alkyl, halogenC1–C3alkyl, C1–C3alkoxyC1–C3alkyl, halogenC1–C3alkoxyC1–C3alkyl, C2–C4alkynyl, cyanoC1–C3alkyl and (CH2)m–R8; m equals 0, 1, 2 or 3; R8 is selected from: 4–, 5– or 6-membered saturated or unsaturated non-aromatic heterocyclic ring containing one or more heteroatoms selected from N, O, or S, with the specified ring not necessarily replaced once or more than once by a substitute, independently selected from oxo SO2C1–C3alkyl and halogenC1–C3alkyl; or C3–C6cycloalkyl, optionally substituted once or more than once by halogen, which is used to suppress the activity of ALK–2 receptor; as well as to pharmaceutical compositions containing this compound, and the use of this compound in the treatment of heterotopic ossification and progressive ossifying fibrodysplasia.

EFFECT: this invention can be used in the treatment of heterotopic ossification and progressive ossifying fibrodysplasia.

18 cl, 19 dwg, 12 tbl, 93 ex

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RU 2 747 318 C2

Authors

Li, Jialiang

Arista, Luca

Babu, Sreehari

Bian, Jianwei

Cui, Kai

Dillon, Michael Patrick

Lattmann, Rene

Liao, Lv

Lizos, Dimitrios

Ramos, Rita

Stiefl, Nikolaus Johannes

Ullrich, Thomas

Usselmann, Peggy

Wang, Xiaoyang

Waykole, Liladhar Murlidhar

Weiler, Sven

Zhang, Yubo

Zhou, Yizong

Zhu, Tingying

Dates

2021-05-04Published

2017-07-18Filed