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Dosage forms and regimens of amino acid compounds
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A dosage form, carrier technology, applied in the field of delaying the onset of fibrotic diseases in individuals, can solve problems such as low therapeutic effect
Pending Publication Date: 2022-03-11
PLIANT THERAPEUTICS INC
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Problems solved by technology
In the treatment of IPF, pirfenidone and nintedanib have been used, but showed less than expected therapeutic effects, while also exhibiting many side effects
Method used
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Embodiment 1
[0668] Embodiment 1. A kind of compound of formula (I)
[0669]
[0670] or a salt thereof, where:
[0671] R 1 for C 6 -C 14 Aryl or 5- to 10-membered heteroaryl, wherein the C 6 -C 14 Aryl and 5- to 10-membered heteroaryl are optionally R 1a replace;
[0672] R 2 for optionally R 2a substituted C 1 -C 6 Alkyl; optionally by R 2b substituted C 3 -C 6 Alkyl; optionally by R 2c Substituted 3- to 12-membered heterocyclyl; or -S(O) 2 R 2d ;
[0673] each R 1a independently for C 1 -C 6 Alkyl, C 2 -C 6 Alkenyl, C 2 -C 6 Alkynyl, C 3 -C 8 Cycloalkyl, C 4 -C 8 Cycloalkenyl, 3- to 12-membered heterocyclyl, 5- to 10-membered heteroaryl, C 6 -C 14 Aryl, Deuterium, Halogen, -CN, -OR 3 , -SR 3 , -NR 4 R 5 , -NO 2 , -C=NH(OR 3 ), -C(O)R 3 , -OC(O)R 3 , -C(O)OR 3 , -C(O)NR 4 R 5 , -NR 3 C(O)R 4 , -NR 3 C(O)OR 4 , -NR 3 C(O)NR 4 R 5 , -S(O)R 3 , -S(O) 2 R 3 , -NR 3 S(O)R 4 , -NR 3 S(O) 2 R 4 , -S(O)NR 4 R 5 , -S(O) 2 NR 4 R 5 or...
Embodiment 2
[0687] Embodiment 2. The compound or salt thereof according to Embodiment 1, wherein R 1a , R 2a , R 2b , R 2c , R 2e , R 2f , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 , R 12 , R 13 or R 14 At least one of them is deuterium.
Embodiment 3
[0688] Embodiment 3. The compound or salt thereof according to Embodiment 1, wherein R 10 , R 11 , R 12 , R 13 and R 14 is hydrogen; p is 3; and is represented by a compound of formula (II):
[0689]
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Abstract
The present invention relates to dosage forms for daily administration of compounds of formula (A) and compounds of formula (I): or salts thereof, wherein R1, R2, R10, R11, R12, R13, R14, R15, R16, q and p are as described herein. Compounds of formula (A), compounds of formula (I), and pharmaceutical compositions thereof are alpha v beta 6 integrin inhibitors that are useful in the treatment of fibrosis, such as idiopathic pulmonary fibrosis (IPF) and non-specific interstitial pneumonia (NSIP).
Description
[0001] CROSS-REFERENCE TO RELATED APPLICATIONS [0002] This application claims US Provisional Patent Application No. 62 / 831,060, filed on April 8, 2019, US Provisional Patent Application No. 62 / 850,530, filed on May 20, 2019, and filed on September 11, 2019 Priority of US Provisional Patent Application No. 62 / 899,071. The entire contents of these patent applications are incorporated herein by reference. Background technique [0003] Fibrosis is a pathological feature of many diseases and results from malfunctioning of the body's natural ability to repair damaged tissue. Left untreated, fibrosis can lead to scarring of vital organs, causing irreparable damage and eventual organ failure. [0004] Patients with nonalcoholic fatty liver disease (NAFLD) may progress from simple steatosis to nonalcoholic steatohepatitis (NASH) followed by fibrosis. Although liver fibrosis is reversible in its initial stages, progressive liver fibrosis can lead to cirrhosis. [0005] Renal fibr...
Claims
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Application Information
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