Agent for treating myopia, preventing myopia and/or suppressing myopia progression

Patent metadata

Field	Value
Publication number	US-2023190766-A1
Application number	US-202118019395-A
Country	US
Kind code	A1
Filing date	Aug 3, 2021
Priority date	Aug 4, 2020
Publication date	Jun 22, 2023
Grant date	—

Abstract

The present invention relates to a pharmaceutical composition for treating myopia, preventing myopia and/or suppressing myopia progression, comprising (+)-11-[2-[2-[(diethylamino)methyl]-1-piperidinyl]acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one or a salt thereof as an active ingredient, wherein the pharmaceutical composition is substantially free of (−)-11-[2-[2-[(diethylamino)methyl]-1-piperidinyl]acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one or a salt thereof.

First claim

1 . A pharmaceutical composition for treating myopia, preventing myopia and/or suppressing myopia progression, comprising (+)-11-[2-[2-[(diethylamino)methyl]-1-piperidinyl]acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one or a salt thereof as an active ingredient, wherein the pharmaceutical composition is substantially free of (−)-11-[2-[2-[(diethylamino)methyl]-1-piperidinyl]acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one or a salt thereof.

2 . The pharmaceutical composition of claim 1 which is free of (−)-11-[2-[2-[(diethylamino)methyl]-1-piperidinyl]acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one or a salt thereof.

3 . The pharmaceutical composition of claim 1 which does not substantially have mydriatic action.

4 . The pharmaceutical composition of claim 1 , wherein the myopia is axial myopia, refractive myopia, pseudomyopia, pathological myopia, simple myopia, extreme myopia, severe myopia, high myopia, moderate myopia, low myopia, myopia complicated by glaucoma, myopia at the risk of the onset of glaucoma, or myopia with high intraocular pressure.

5 . The pharmaceutical composition of claim 1 for ocular topical administration.

6 . The pharmaceutical composition of claim 5 , wherein the ocular topical administration is ophthalmic administration, administration by an ophthalmic ointment, conjunctival sac administration, intravitreal administration, subconjunctival administration, sub-Tenon's administration, conjunctival sac injection, or application to the eyelid.

7 . The pharmaceutical composition of claim 1 which is in the form of an eye drop, an eye gel, an ophthalmic ointment, or an injection.

8 . The pharmaceutical composition of claim 1 , wherein the concentration of (+)-11-[2-[2-[(diethylamino)methyl]-1-piperidinyl]acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one or a salt thereof is 0.0001-5% (w/v).

9 . The pharmaceutical composition of claim 1 , wherein the concentration of (+)-11-[2-[2-[(diethylamino)methyl]-1-piperidinyl]acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one or a salt thereof is 0.001-1% (w/v).

10 . The pharmaceutical composition of claim 1 , wherein the concentration of (+)-11-[2-[2-[(diethylamino)methyl]-1-piperidinyl]acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one or a salt thereof is 0.001% (w/v) or more and less than 1% (w/v).

11 . The pharmaceutical composition of claim 1 , wherein the concentration of (+)-11-[2-[2-[(diethylamino)methyl]-1-piperidinyl]acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one or a salt thereof is 0.002-0.5% (w/v).

12 . The pharmaceutical composition of claim 1 , wherein the concentration of (+)-11-[2-[2-[(diethylamino)methyl]-1-piperidinyl]acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one or a salt thereof is 0.002-0.01% (w/v).

13 . The pharmaceutical composition of claim 1 , wherein the concentration of (−)-11-[2-[2-[(diethylamino)methyl]-1-piperidinyl]acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one or a salt thereof is less than 0.1% (w/v).

14 . The pharmaceutical composition of claim 1 , wherein the concentration of (−)-11-[2-[2-[(diethylamino)methyl]-1-piperidinyl]acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one or a salt thereof is 0.05 part by weight or less per part by weight of (+)-11-[2-[2-[(diethylamino)methyl]-1-piperidinyl]acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one or a salt thereof.

15 . A pharmaceutical composition for suppressing the axial length elongation, comprising (+)-11-[2-[2-[(diethylamino)methyl]-1-piperidinyl]acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one or a salt thereof as an active ingredient, wherein the pharmaceutical composition is substantially free of (−)-11-[2-[2-[(diethylamino)methyl]-1-piperidinyl]acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one or a salt thereof.

16 . A pharmaceutical composition for suppressing the refractive error, comprising (+)-11-[2-[2-[(diethylamino)methyl]-1-piperidinyl]acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one or a salt thereof as an active ingredient, wherein the pharmaceutical composition is substantially free of (−)-11-[2-[2-[(diethylamino)methyl]-1-piperidinyl]acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one or a salt thereof.

17 . Use of (+)-11-[2-[2-[(diethylamino)methyl]-1-piperidinyl]acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one or a salt thereof in the manufacture of an agent for treating and/or preventing myopia.

18 . The use of claim 17 , wherein the agent is substantially free of (−)-11-[2-[2-[(diethylamino)methyl]-1-piperidinyl]acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one or a salt thereof.

19 . Use of (+)-11-[2-[2-[(diethylamino)methyl]-1-piperidinyl]acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one or a salt thereof in the manufacture of an agent for suppressing myopia progression.

20 . The use of claim 19 , wherein the agent is substantially free of (−)-11-[2-[2-[(diethylamino)methyl]-1-piperidinyl]acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one or a salt thereof.

Assignees

• Santen Pharmaceutical Co Ltd
• Boehringer Ingelheim Int

Inventors

• Inaba Takaaki
• Kato Masatomo

Classifications

• A61K31/5513 Primary

  1,4-Benzodiazepines, e.g. diazepam {or clozapine} · CPC title

• A61P27/06

  Antiglaucoma agents or miotics · CPC title

• A61K9/0048

  Eye, e.g. artificial tears · CPC title

• A61P27/10

  for accommodation disorders, e.g. myopia · CPC title

• A61P27/02 Primary

  Ophthalmic agents · CPC title