US2018221348A1PendingUtilityA1
Modulators of pharmacokinetic properties of therapeutics
Est. expiryJul 7, 2026(expired)· nominal 20-yr term from priority
A61P 43/00A61P 7/00A61P 31/12A61P 31/00A61P 31/18A61P 31/14C07D 417/14C07C 227/16C07D 277/24C07C 315/04C07C 227/18C07C 209/78C07D 277/28A61K 45/00A61K 31/426C07K 5/06052C07D 417/12C07K 5/06A61K 31/5377A61K 31/496A61K 31/47A61K 38/05A61K 45/06C07D 277/30A61K 31/4402A61K 31/427A61K 38/005C07K 5/06034A61K 31/4535C07K 5/06026
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Claims
Abstract
or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods and include the administration of such compounds with at least one additional therapeutic agent.
Claims
exact text as granted — not AI-modified1 - 20 . (canceled)
21 . An in vivo metabolic product of Compound P prepared according to the process of Scheme 18 at page 211.
22 . The metabolic product of claim 21 which is substantially isolated.
23 . A method of preparing the in vivo metabolic product of claim 21 comprising contacting Compound P prepared according to the process of Scheme 18 at page 211 with a mammal for a period of time sufficient to yield the in vivo metabolic product.
24 . The method of claim 23 wherein the mammal is a rat, mouse, guinea pig, monkey, or human.
25 . The method of claim 23 wherein Compound P prepared according to the process of Scheme 18 at page 211 is orally administered to the mammal.
26 . The method of claim 23 wherein Compound P prepared according to the process of Scheme 18 at page 211 is radiolabeled.
27 . The method of claim 26 wherein the radiolabel comprises C 14 or H 3 .
28 . A method of determining the optimal therapeutic dose of Compound P prepared according to the process of Scheme 18 at page 211 in a mammal comprising measuring the quantity of the in vivo metabolic product of claim 21 produced upon contacting the mammal with a radiolabeled Compound P and correlating the measured quantity of the in vivo metabolic product with therapeutic effectiveness of Compound P.
29 . A prodrug of Compound P prepared according to the process of Scheme 18 at page 211.
30 . A pharmaceutical composition comprising the prodrug of claim 29 , or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier or excipient.
31 . A method of improving the pharmacokinetics of a drug, comprising administering to a patient treated with said drug, a therapeutically effective amount of a prodrug of claim 29 , or a pharmaceutically acceptable salt thereof.
32 . A solvate of Compound P prepared according to the process of Scheme 18 at page 211.
33 . A pharmaceutical composition comprising the solvate of claim 32 , or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier or excipient.
34 . A method of improving the pharmacokinetics of a drug, comprising administering to a patient treated with said drug, a therapeutically effective amount of a solvate of claim 32 , or a pharmaceutically acceptable salt thereof.
35 . A kit comprising Compound P prepared according to the process of Scheme 18 at page 211, wherein the kit is useful for improving the pharmacokinetics of a drug.Join the waitlist — get patent alerts
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