Processes for preparing quinoline compounds and pharmaceutical compositions containing such compounds

US9717720B2 · US · B2

Patent metadata
FieldValue
Publication numberUS-9717720-B2
Application numberUS-201213984559-A
CountryUS
Kind codeB2
Filing dateFeb 10, 2012
Priority dateFeb 10, 2011
Publication dateAug 1, 2017
Grant dateAug 1, 2017

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  1. Title

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  2. Abstract

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  3. Assignees and inventors

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  4. Key dates

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  5. First independent claim

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  7. Citations and related patents

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Abstract

Official abstract text for this publication.

The present invention is directed to processes for making and compositions containing quinolines such as formula I or pharmaceutically acceptable salts thereof wherein: X1 is H, Br, CI, or X2 is H, Br, CI, or n1 is 1-2; and n2 is 1-2.

First claim

Opening claim text (preview).

The invention claimed is: 1. A capsule pharmaceutical composition: Ingredient mg ⁢ / ⁢ unit ⁢ ⁢ dose total ⁢ ⁢ fill ⁢ ⁢ weight × 100 Compound IB with 50 ppm or less 10 of 6,7-dimethoxy-quinoline-4-ol (10 percent drug load formulation) Silicified Microcrystalline Cellulose 78.7 Croscarmellose sodium 5 Sodium starch glycolate 5 Fumed Silica 0.3 Stearic acid 1 Total 100 wherein compound IB has the structure: 2. The capsule pharmaceutical composition of claim 1 , wherein the formation of 6,7-dimethoxy-quinoline-4-ol in the pharmaceutical composition is minimized to 25 ppm or less from 0 to 6 months at 25° C. and 60 percent relative humidity. 3. The capsule pharmaceutical composition of claim 1 , wherein the formation of 6,7-dimethoxy-quinoline-4-ol in the pharmaceutical composition is minimized to 15 ppm or less from 0 to 6 months at 25° C. and 60 percent relative humidity. 4. The capsule pharmaceutical composition of claim 1 , wherein the formation of 6,7-dimethoxy-quinoline-4-ol in the pharmaceutical composition is minimized to 10 ppm or less from 0 to 6 months at 25° C. and 60 percent relative humidity. 5. A capsule pharmaceutical composition: Ingredient mg ⁢ / ⁢ unit ⁢ ⁢ dose total ⁢ ⁢ fill ⁢ ⁢ weight × 100 Compound IB with 50 ppm or less 50 of 6,7-dimethoxy-quinoline-4-ol (50 percent drug load formulation) Silicified Microcrystalline Cellulose 37.7 Croscarmellose sodium 5 Sodium starch glycolate 5 Fumed Silica 0.3 Stearic acid 2 Total 100 wherein compound IB has the structure: 6. The capsule pharmaceutical composition of claim 5 , wherein the formation of 6,7-dimethoxy-quinoline-4-ol in the pharmaceutical composition is minimized to 25 ppm or less from 0 to 6 months at 25° C. and 60 percent relative humidity. 7. The capsule pharmaceutical composition of claim 5 , wherein the formation of 6,7-dimethoxy-quinoline-4-ol in the pharmaceutical composition is minimized to 15 ppm or less from 0 to 6 months at 25° C. and 60 percent relative humidity. 8. The capsule pharmaceutical composition of claim 5 , wherein the formation of 6,7-dimethoxy-quinoline-4-ol in the pharmaceutical composition is minimized to 10 ppm or less from 0 to 6 months at 25° C. and 60 percent relative humidity. 9. The capsule pharmaceutical composition of claim 1 containing 25 mg of Compound IB. 10. The capsule pharmaceutical composition of claim 9 containing:

Assignees

Inventors

Classifications

  • A61K31/47Primary

    Quinolines; Isoquinolines · CPC title

  • only one oxygen atom which is attached in position 4 · CPC title

  • A61P35/00Primary

    Antineoplastic agents · CPC title

  • attached in position 2 or 4 · CPC title

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Frequently asked questions

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What does patent US9717720B2 cover?
The present invention is directed to processes for making and compositions containing quinolines such as formula I or pharmaceutically acceptable salts thereof wherein: X1 is H, Br, CI, or X2 is H, Br, CI, or n1 is 1-2; and n2 is 1-2.
Who is the assignee on this patent?
Wilson Jo Ann, Shah Khalid, Exelixis Inc
What technology area does this patent fall under?
Primary CPC classification A61K31/47. Mapped technology areas include Human Necessities.
When was this patent published?
Publication date Tue Aug 01 2017 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 9 related publications on this page (citations in our corpus or others sharing the same primary CPC).