IP Library Granted Patent US 10,385,052
Granted Patent B2
US 10,385,052 · App. 15/841,002 · Granted Aug 20, 2019

Tricyclic compound and JAK inhibitor

Inventors: Tsuneo Watanabe (Funabashi, JP); Keiji Takahashi (Funabashi, JP); Keishi Hayashi (Funabashi, JP); Takanori Nakamura (Shiraoka, JP); Masataka Minami (Funabashi, JP); Kazunori Kurihara (Funabashi, JP); Akio Yamamoto (Funabashi, JP); Takuya Nishimura (Funabashi, JP); Miyuki Uni (Funabashi, JP); Toshihiko Kamiyama (Funabashi, JP); Shunsuke Iwamoto (Funabashi, JP)
Assignee: Nissan Chemical Corporation
C07D471/14A61K31/4375A61K31/519Y02P20/55
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Quick Facts
Patent No.
US 10,385,052
App. No.
15/841,002
Granted
Aug 20, 2019
Kind
B2
Abstract

Novel tricyclic compounds which have JAK inhibitory activities are useful for prevention, treatment or improvement of autoimmune diseases, inflammatory diseases and allergic diseases are provided. Novel tricyclic compound represented by the formula (I), the formula (II) or the formula (III) (wherein: each of A 1 , A 2 and A 3 is a cyclohexane-1,4-diyl group or the like; each of L 1 , L 2 and L 3 is a methylene group or the like; each of X 1 and X 3 is O or NH; each of R 1 and R 3 is a cyano C 1-6 haloalkyl group or the like; and R 2 is an aromatic heterocyclic group), a tautomer or pharmaceutically acceptable salt of the compound or a solvate thereof.

Claims (18)

1. A compound represented by the formula (I):

wherein A 1 is a C 3-7 cycloalkylene group,

L 1 is a C 1-6 alkylene group,

X 1 is O or NH, and

when X 1 is O, R 1 is a C 1-6 haloalkyl group, a cyano C 1-6 haloalkyl group or a cyano C 1-6 alkyl group, and

when X 1 is NH, R 1 is a cyano C 1-6 haloalkyl group,

or a tautomer or pharmaceutically acceptable salt of the compound.

2. The compound, tautomer, or pharmaceutically acceptable salt according to claim 1 , wherein L 1 is a methylene group.

3. The compound, tautomer, or pharmaceutically acceptable salt according to claim 1 , wherein A 1 is a cyclohexanediyl group.

4. The compound, tautomer, or pharmaceutically acceptable salt according to claim 1 , wherein X 1 is O.

5. The compound, tautomer, or pharmaceutically acceptable salt according to claim 4 , wherein R 1 is a C 1-4 haloalkyl group.

6. The compound, tautomer, or pharmaceutically acceptable salt according to claim 1 , wherein X 1 is NH.

7. The compound, tautomer, or pharmaceutically acceptable salt according to claim 6 , wherein R 1 is a cyano C 2-4 haloalkyl group.

8. A JAK inhibitor containing the compound, tautomer, or pharmaceutically acceptable salt according to claim 1 , as an active ingredient.

9. A therapeutic or improving agent for diseases against which inhibition of JAK is effective, which contains the compound, tautomer, or pharmaceutically acceptable salt according to claim 1 , as an active ingredient.

10. A therapeutic agent for rheumatoid arthritis, which contains the compound, tautomer, or pharmaceutically acceptable salt as according to claim 1 , as an active ingredient.

11. A composition comprising the compound, tautomer, or pharmaceutically acceptable salt according to claim 1 as an active ingredient, and one or more inactive ingredients.

12. The composition according to claim 11 , wherein the one or more inactive ingredients comprise at least one selected from the group consisting of lactose, corn starch, low-viscosity hydroxypropylcellulose, magnesium stearate, microcrystalline cellulose, carboxymethylcellulose sodium salt, and saturated fatty acid glyceride.

Assignments (1)
CHANGE OF NAME Recorded Oct 18, 2018
From: NISSAN CHEMICAL INDUSTRIES, LTD.
To: NISSAN CHEMICAL CORPORATION
Reel/Frame 047261/0146 →
Priority Claims (1)
JP 2014-100712 · May 14, 2014 · national
Continuity (2)
Division 15307036
Related Publication 20180099966A1 · Apr 12, 2018