Salts of 2-amino-1-hydroxyethyl-8-hydroxyquinolin-2(1H)-one derivatives having both β2 adrenergic receptor agonist and M3 muscarinic receptor antagonist activities
US-9562039-B2 · Feb 7, 2017 · US
Pharmaceutical formulations and uses thereof
US12064516B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-12064516-B2 |
| Application number | US-202117333528-A |
| Country | US |
| Kind code | B2 |
| Filing date | May 28, 2021 |
| Priority date | May 13, 2020 |
| Publication date | Aug 20, 2024 |
| Grant date | Aug 20, 2024 |
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- Title
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Abstract
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The present invention relates to pharmaceutical compositions and unit dosage forms comprising a quinoline compound, or a pharmaceutically acceptable salt thereof, which are useful for treatment of a disease, disorder, or condition such as inflammatory diseases, respiratory diseases, organ diseases, viral infections, and sequelae and associated conditions such as acute respiratory distress syndrome.
First claim
Opening claim text (preview).
We claim: 1. A pharmaceutical composition comprising: a) compound I-1: or a pharmaceutically acceptable salt thereof, as about 15% to about 60% by weight of the composition; b) one or more fillers comprising at least one of microcrystalline cellulose, mannitol, and lactose monohydrate, as about 1% to 20% w/w by weight of the composition; c) one or more binders comprising vinylpyrrolidone-vinyl acetate copolymer, as about 2% to about 18% w/w by weight of the composition; d) one or more disintegrants comprising at least one of croscarmellose sodium and crospovidone, as about 1% to 20% w/w by weight of the composition; e) one or more glidants comprising fumed silica, as about 0.05% to about 2.0% w/w by weight of the composition; f) one or more lubricants comprising magnesium stearate, as about 0.05% to about 2.0% w/w by weight of the composition; g) optionally, one or more surfactants comprising lauryl sulfate, as about 0.05% to 2.0% w/w by weight of the composition; and h) optionally, one or more effervescent components comprising sodium bicarbonate and an organic acid selected from citric acid or tartaric acid, as about 0.05% to 2.0% w/w by weight of the composition, wherein the pharmaceutical composition is in a unit dosage form for oral administration to a subject in need thereof, in the form of a capsule or tablet; wherein the subject is a human and upon oral administration to the human subject, the unit dosage form provides an oral bioavailability of at least 70% of the administered dose of I-1, or a pharmaceutically acceptable salt thereof. 2. The pharmaceutical composition of claim 1 , wherein compound I-1 or a pharmaceutically acceptable salt thereof is present in the pharmaceutical composition as a spray-dried solid comprising a copolymer of methacrylate and acrylate. 3. The pharmaceutical composition of claim 2 , wherein compound I-1 or a pharmaceutically acceptable salt thereof is provided as a spray-dried solid mixed with the copolymer of methacrylate and acrylate; and about 0.9 mg to about 3.6 mg of the copolymer of methacrylate and acrylate is mixed with each 1 mg of I-1 or pharmaceutically acceptable salt thereof. 4. The pharmaceutical composition of claim 1 , wherein the capsule or tablet comprises about 5 mg to about 500 mg I-1, or a pharmaceutically acceptable salt thereof. 5. The pharmaceutical composition of claim 1 , wherein, upon oral administration to a human subject in a daily dose of 20 mg, 50 mg, 100 mg, 200 mg, 400 mg, 700 mg or 1200 mg, the unit dosage form provides a pharmacokinetic result shown below: 20 50 100 200 400 700 1200 mg mg mg mg mg mg mg C max about about about about about about about (ng/mL) 26.4 56.7 140 459 869 2020 4220 AUC inf about about about about about about about (ng * h/mL) 50.0 156 433 1140 2730 6710 14500 t 1/2 (h) about about about about about 3.52 6.04 6.15 7.33 7.69. 6. The pharmaceutical composition of claim 1 , wherein, upon oral administration to a human subject in a dose of about 50 mg BID, about 150 mg BID, about 350 mg BID, or about 600 mg BID, the unit dosage form provides a pharmacokinetic result shown below: Mean Mean C max AUC 0-12 Mean Day Dose (ng/mL) (h * ng/mL) t 1/2 (h) 1 about 50 mg BID about 70.2 about 148 about 3.49 about 150 mg BID about 343 about 809 about 4.86 about 350 mg BID about 1190 about 2950 about 5.67 about 600 mg BID about 2230 about 6450 about 4.15 10 about 50 mg BID about 85.9 about 252 about 5.25 about 150 mg BID about 320 about 1170 about 6.34 about 350 mg BID about 1230 about 4340 about 6.83
Assignees
Inventors
Classifications
Quinolines; Isoquinolines · CPC title
Preparations in capsules, e.g. of gelatin, of chocolate {(A61K9/0004 takes precedence; bite capsules A61K9/0056)} · CPC title
Pills, tablets, {discs, rods (A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095)} · CPC title
Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin (homeopathic globules A61K9/1623) · CPC title
obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates · CPC title
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Frequently asked questions
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- What does patent US12064516B2 cover?
- The present invention relates to pharmaceutical compositions and unit dosage forms comprising a quinoline compound, or a pharmaceutically acceptable salt thereof, which are useful for treatment of a disease, disorder, or condition such as inflammatory diseases, respiratory diseases, organ diseases, viral infections, and sequelae and associated conditions such as acute respiratory distress syndr…
- Who is the assignee on this patent?
- Aldeyra Therapeutics Inc
- What technology area does this patent fall under?
- Primary CPC classification A61K9/1623. Mapped technology areas include Human Necessities.
- When was this patent published?
- Publication date Tue Aug 20 2024 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
- What related patents are in patentsdb?
- We list 12 related publications on this page (citations in our corpus or others sharing the same primary CPC).