IP Library Granted Patent US 10,174,001
Granted Patent B2
US 10,174,001 · App. 15/755,281 · Granted Jan 8, 2019

Crystals of 5-cyclopropyl-2-((1-(3-fluorobenzyl)-1H-indol-5-yl)amino)nicotinic acid

Inventors: Yusuke Okubo (Toyama, JP); Tadashi Tanaka (Toyama, JP)
Assignee: FUJIFILM Toyama Chemical Co., Ltd.
C07D401/12C07B2200/13
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Quick Facts
Patent No.
US 10,174,001
App. No.
15/755,281
Granted
Jan 8, 2019
Kind
B2
Abstract

Crystals of 5-cyclopropyl-2-((1-(3-fluorobenzyl)-1H-indol-5-yl)amino)nicotinic acid having diffraction peaks at diffraction angles (2θ) of 12.2±0.2, 17.2±0.2, 19.4±0.2, 24.1±0.2, and 27.1±0.2° or diffraction angles (2θ) of 12.9±0.2, 15.5±0.2, 21.2±0.2, 21.7±0.2, and 25.9±0.2° in powder x-ray diffraction have excellent stability, are easy to handle, and are useful as a drug substance of pharmaceuticals to be used in treatments such as the prevention or treatment of diseases involving keratinocyte hyperproliferation.

Claims (6)

1. A crystal of 5-cyclopropyl-2-((1-(3-fluorobenzyl)-1H-indol-5-yl)amino)nicotinic acid having diffraction peaks at diffraction angles (2θ) of 12.2±0.2, 17.2±0.2, 19.4±0.2, 24.1±0.2 and 27.1±0.2° in powder x-ray diffraction.

2. A crystal of 5-cyclopropyl-2-((1-(3-fluorobenzyl)-1H-indol-5-yl)amino)nicotinic acid having diffraction peaks at diffraction angles (2θ) of 12.9±0.2, 15.5±0.2, 21.2±0.2, 21.7±0.2 and 25.9±0.2° in powder x-ray diffraction.

3. A pharmaceutical composition comprising the crystal of claim 1 and a pharmaceutically acceptable adjuvant.

4. A pharmaceutical composition comprising the crystal of claim 2 and a pharmaceutically acceptable adjuvant.

5. The pharmaceutical composition of claim 3 , wherein the adjuvant is at least one selected from the group consisting of an excipient, a carrier and a diluent.

6. The pharmaceutical composition of claim 4 , wherein the adjuvant is at least one selected from the group consisting of an excipient, a carrier and a diluent.

Assignments (2)
MERGER AND CHANGE OF NAME Recorded Nov 19, 2018
From: FUJIFILM RI PHARMA CO., LTD.; TOYAMA CHEMICAL CO., LTD.
To: FUJIFILM TOYAMA CHEMICAL CO., LTD.
Reel/Frame 047536/0252 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 26, 2018
From: OKUBO, YUSUKE; TANAKA, TADASHI
To: TOYAMA CHEMICAL CO., LTD.; FUJIFILM CORPORATION
Reel/Frame 045037/0819 →
Priority Claims (1)
JP 2015-170151 · Aug 31, 2015 · national
Continuity (1)
Related Publication 20180244647A1 · Aug 30, 2018