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JP-2026514393-A - Compositions for treating Parkinson's disease and their qualitative evaluation

JP2026514393AJP 2026514393 AJP2026514393 AJP 2026514393AJP-2026514393-A

Abstract

This disclosure provides a composition comprising compound 1, its use, and a method for producing the same.

Inventors

  • カタムラ，クライ－リト
  • シン，オンキャル・エヌ

Assignees

  • イントランス・メディカル・システムズ・インコーポレイテッド

Dates

Publication Date
20260511
Application Date
20240322
Priority Date
20230327

Claims (20)

  1. Compound 1 exceeding approximately 0.15% by weight: A composition comprising a pharmaceutically acceptable salt thereof.
  2. The composition according to claim 1, comprising approximately 50% by weight or more of compound 1.
  3. The composition according to claim 1 or 2, comprising approximately 75% by weight or more of compound 1.
  4. A composition according to any one of claims 1 to 3, comprising approximately 85% by weight or more of compound 1.
  5. A composition according to any one of claims 1 to 4, comprising approximately 90% by weight or more of compound 1.
  6. A composition according to any one of claims 1 to 5, comprising approximately 95% by weight or more of compound 1.
  7. The composition according to any one of claims 1 to 6, wherein the composition contains less than 10% by weight of an organic solvent.
  8. The composition according to any one of claims 1 to 7, wherein the composition contains less than 5% by weight of an organic solvent.
  9. The composition according to claim 7 or 8, wherein the organic solvent is selected from the group consisting of methanol, dichloromethane, acetone, ethanol, isopropanol, ethyl acetate, acetaldehyde, heptane, and acetaldehyde.
  10. The composition according to any one of claims 1 to 9, wherein the composition contains about 4% by weight or less, preferably about 3% or less, of water.
  11. The composition according to any one of claims 1 to 10, wherein the composition contains about 2% by weight or less of water.
  12. The composition according to any one of claims 1 to 11, wherein the composition contains about 1.5% by weight or less of water.
  13. The composition according to claim 10 or 12, wherein the weight of water is determined by Karl Fischer analysis.
  14. Carbidopa, entacapone, and compound 1 exceeding 0.15% by weight: A pharmaceutical composition comprising a pharmaceutically acceptable salt thereof.
  15. The pharmaceutical composition according to claim 14, further comprising levodopa.
  16. The pharmaceutical composition according to claim 14 or 15, characterized in that it is stable for 16 weeks or more when stored at approximately 5°C.
  17. The pharmaceutical composition according to claim 14 or 15, characterized in that it is stable for 16 weeks or more when stored at 5°C ± 3°C.
  18. The pharmaceutical composition according to any one of claims 14 to 17, characterized in that the pharmaceutical composition is stable for 16 hours or more at a physiological temperature (e.g., 37°C).
  19. The aforementioned pharmaceutical composition Approximately 1-15% by weight of levodopa, A pharmaceutical composition according to any one of claims 15 to 18, comprising about 0.1 to 2% by weight of carbidopa and about 1 to 7.5% by weight of entacapone.
  20. The aforementioned pharmaceutical composition Approximately 2% by weight of levodopa, A pharmaceutical composition according to any one of claims 15 to 19, comprising about 0.5% by weight of carbidopa and about 2% by weight of entacapone.

Description

Cross-reference of related applications This application claims priority to U.S. Provisional Application No. 63/492,365, filed on 27 March 2023, the contents of which are incorporated herein by reference in their entirety. Background: Parkinson's disease is a neurological disorder that causes involuntary movements of the body, including tremors, tonics, and difficulty or loss of balance and coordination. As of 2016, approximately 6.1 million people were affected by the disease. See Bloem et al., The Lancet, 397(10291):12-18 (2021). There is no cure for Parkinson's disease. People with Parkinson's disease face the continuous progression of the disease throughout their lives. Figure 1 is a plot showing the purity at 220 nm of a composition containing compound 1, measured under the indicated conditions and at the indicated time.Figure 2 is a plot showing the purity at 280 nm of a composition containing compound 1, measured under the indicated conditions and at the indicated time.Figure 3 is a plot showing the purity at 220 nm of a composition containing compound 1, measured under the indicated conditions and at the indicated time.Figure 4 is a plot showing the purity at 220 nm of a composition containing compound 1, measured under the indicated conditions and at the indicated time.Figure 5 is a plot showing the water content of a composition containing compound 1 measured under the indicated conditions and at the indicated time. Detailed Description of a Specific Embodiment This disclosure relates, in particular, to a composition comprising carbidopa and entacapone, wherein a specific by-product, for example, Compound 1: This includes the insight that such findings can be formed, and such findings are implemented herein, in particular, in novel compositions, novel methods for qualifying compositions comprising carbidopa and entacapone, and novel methods for treating patients with neurodegenerative disorders, such as Parkinson's disease. Definitions of "approximately" or "about": As used herein, the terms "approximately" or "about" applied to one or more values of interest refer to values that are similar to the reference values mentioned. Generally, a person skilled in the art familiar with the context will understand the degree of variation that "approximately" or "about" encompasses in that context. For example, in some embodiments, the terms "approximately" or "about" may encompass a range of values within 25%, 20%, 19%, 18%, 17%, 16%, 15%, 14%, 13%, 12%, 11%, 10%, 9%, 8%, 7%, 6%, 5%, 4%, 3%, 2%, 1%, or less than these values (i.e., ± these values). Administration: As used herein, the terms “administer” or “dosage” typically refer to the administration of a composition to a subject to achieve delivery of the drug, which is a composition, or a drug contained in the composition, to a target site or site to be treated. Those skilled in the art will recognize the various routes that can be used for administration to a subject, e.g., a human, in appropriate circumstances. For example, in some embodiments, administration may be intraocular, oral, parenteral, topical, etc. In some specific embodiments, administration may be bronchial (e.g., by bronchial infusion), intracheek, skin (e.g., one or more of the following, including, topical into the dermis, intradermal, interdermal, transdermal, etc.), intestinal, intraarterial, intradermal, gastric, intramedullary, intramuscular, intranasal, intraperitoneal, intrathecal, intravenous, intraventricular, intraspecific organ (e.g., intrahepatic), mucous membrane, nose, oral, rectal, subcutaneous, sublingual, topical, trachea (e.g., by intratracheal infusion), vaginal, intravitreal, etc. In some embodiments, administration may be parenteral. In some embodiments, administration may be oral. In some specific embodiments, administration may be intravenous. In some specific embodiments, administration may be subcutaneous. In some embodiments, administration may consist of only a single dose. In some embodiments, administration may consist of the application of a fixed number of doses. In some embodiments, administration may consist of intermittent dosing (e.g., multiple dosings spaced apart in time) and/or cyclical dosing (e.g., individual dosings spaced apart by a common period of time). In some embodiments, administration may consist of continuous dosing (e.g., perfusion) over at least a selected period of time. In some embodiments, administration may consist of a prime-and-boost protocol. A prime-and-boost protocol may include the administration of a first dose of a pharmaceutical composition (e.g., an immunogenic composition, e.g., a vaccine), followed by the administration of a second or subsequent dose of the pharmaceutical composition (e.g., an immunogenic composition, e.g., a vaccine) after a certain interval. In the case of immunogenic compositions, a prime-and-boost protocol can result in an increased immune response in the patient. Antagonist: As those skilled in th