05-10-2017 дата публикации
Номер: US20170283421A1
Автор:
Chough Chie Yeon,
Jeong Hyun Uk,
Jo Young Soo,
Joung Mi Suk,
KIM Jong Hoon,
Kim Kyeoung Ah,
KIM Kyoung Rak,
KIM Sung Jun,
KIM Tae Wook,
Lee Jae Min,
Lee Sun Min,
LEE Sung Il,
Moon Hong Sik,
Yi Eun Jung,
YU Se Mi
Принадлежит:
A novel substituted N-(pyrrolidin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine and a use thereof as a Janus kinase (JAK) inhibitor are provided. 2. The compound of claim 1 , wherein Ris Calkyl claim 1 , and Rand Rtaken together form —(Calkyl)-.3. The compound of claim 1 , wherein Wis absent claim 1 , or is —C(═O)— claim 1 , —C(═S)— claim 1 , —C(═O)O— claim 1 , —C(═O)NR— claim 1 , —C(═S)NR— claim 1 , or —S(═O)—;{'sup': '5', 'sub': '1-6', 'Ris H or Calkyl; and'}{'sup': 6', 'a', 'b', 'a', 'b', 'c', 'd', 'a', 'b', 'c', 'd, 'sub': 1-10', '1-6', '5-20', '1-10', '1-6', '2', '1-10', '3-7', '1-6', '1-10', '1-10', '1-10', '3', '1-10', '1-6', '1-10', '1-10', '1-10', '1-6, 'Ris Calkyl; Chaloalkyl; Caryl optionally substituted with at least one substituent selected from the group consisting of Calkyl, Chaloalkyl, halo, CN, NO, and —O—(Calkyl); Ccycloalkyl; heterocycloalkyl having 3 to 7 ring atoms, optionally substituted with —C(C═O)(Calkyl); heteroaryl having 3 to 7 ring atoms; -heteroaryl-(Calkyl) having 3 to 7 ring atoms; —(Calkyl)-CN; —(Calkyl)-N; —(Calkyl)-O—(Calkyl); —(Calkyl)-C(═O)NRR; or —(Calkyl)-NRC(═O)Ror —(Calkyl)-NRR, wherein R, R, R, and Rare each independently H or Calkyl.'}5. The compound of claim 1 , wherein the compound is(R)-N-(5-butyl-5-azaspiro[2.4]heptan-7-yl)-N-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine;(R)-N-methyl-N-(5-pentyl-5-azaspiro[2.4]heptan-7-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine;(R)-2-methyl-1-(7-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-5-azaspiro[2.4]heptan-5-yl)propan-1-one;(R)-2-azido-1-(7-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-5-azaspiro[2.4]heptan-5-yl)ethan-1-one;(R)-3-(7-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-5-azaspiro[2.4]heptan-5-yl)-3-oxopropanenitrile;(R)-3-methyl-1-(7-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-5-azaspiro[2.4]heptan-5-yl)butan-1-one;(R)-N-(2-(7-(methyl(7H-pyrrolo[2, 3-d]pyrimidin-4-yl)amino)-5-azaspiro[2.4]heptan-5-yl)-2-oxoethyl)acetamide;(R)-N-methyl-3-(7-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl ...
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