Purinone derivative hydrochloride

Patent metadata

Field	Value
Publication number	US-2016264576-A1
Application number	US-201615158993-A
Country	US
Kind code	A1
Filing date	May 19, 2016
Priority date	Nov 29, 2011
Publication date	Sep 15, 2016
Grant date	—

Abstract

The purinone derivative 6-amino-9-[(3R)-1-(2-butynoyl)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one hydrochloride has Btk-selective inhibitory activity and, in addition to having excellent metabolic stability, it is a compound that exhibits a high level of solubility and absorption with respect to the free base and can be crystallized, hence it can serve as a therapeutic agent for diseases involving B cells and mast cells.

First claim

1 - 2 . (canceled)

3 . A crystal of 6-amino-9-[(3R)-1-(2-butynoyl)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one hydrochloride, having at least 2 or more peaks at angle 2θ selected from approximately 8.11, 8.43, 11.57, 12.73, 13.85, 14.20, 14.67, 14.91, 15.94, 16.64, 18.06, 19.74, 20.42, 21.05, 22.57, 23.21, 23.85, and 24.70 degrees in a powder x-ray diffraction spectrum.

4 . The crystal according to claim 3 , having peaks at angle 2θ of approximately 8.11, 8.43, 14.20, 14.67, 14.91 and 23.21 degrees in a powder x-ray diffraction spectrum.

5 . The crystal according to claim 3 , having peaks at angle 2θ selected from approximately 8.11, 8.43, 11.57, 12.73, 13.85, 14.20, 14.67, 14.91, 15.94, 16.64, 18.06, 19.74, 20.42, 21.05, 22.57, 23.21, 23.85, and 24.70 degrees in a powder x-ray diffraction spectrum.

6 . The crystal according to claim 3 , which is characterized by the powder x-ray diffraction spectral chart in FIG. 3 .

7 . The crystal according to claim 3 , having an endothermic peak at a peak temperature of 216° C. in differential scanning calorimetry.

8 . The crystal according to claim 3 , which is characterized by the differential scanning calorimetry chart in FIG. 4 .

9 . A pharmaceutical composition comprising 6-amino-9-[(3R)-1-(2-butynoyl)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one hydrochloride.

10 . The pharmaceutical composition according to claim 9 , which is a Btk inhibitor.

11 . The pharmaceutical composition according to claim 10 , which is an agent for the prevention and/or treatment of a Btk-related disease.

12 . The pharmaceutical composition according to claim 11 , wherein the Btk-related disease is an allergic disease, an autoimmune disease, an inflammatory disease, a thromboembolic disease, a bone-related disease, or cancer.

13 . The pharmaceutical composition according to claim 12 , wherein the cancer is non-Hodgkin's lymphoma.

Assignees

• Ono Pharmaceutical Co

Inventors

• Yamamoto Shingo
• Yoshizawa Toshio

Classifications

• A61P35/00

  Antineoplastic agents · CPC title

• A61P7/02

  Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors · CPC title

• A61P35/02

  specific for leukemia · CPC title

• A61P37/08

  Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14) · CPC title

• A61P7/00

  Drugs for disorders of the blood or the extracellular fluid · CPC title