Patent classifications
C07D487/18
FAK inhibitor and drug combination thereof
A deuterated compound as represented by formula (I) or an optical isomer, a tautomer, a pharmaceutically acceptable salt, a prodrug, a hydrate, or a solvate thereof are presented. Compared with a compound before deuteration, the deuterated compound shows better pharmacokinetics, higher maximum plasma drug concentration, higher exposure, and longer half-life, and has more excellent metabolic performance. The deuterated compound can effectively inhibit FAK activity, and has good application prospect in preparation of FAK inhibitors and/or drugs for treating cancer. In addition, the use of the deuterated compound in combination with an anti-cancer drug (such as a PD-1 inhibitor) can achieve a synergistic effect, thereby significantly improving the tumor suppression effect, and providing a better choice for clinical cancer treatment.
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Macrocyclic compounds for treatment of medical disorders
Macrocyclic Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, Formula IV, Formula V, Formula VI, Formula VII, and Formula VIII or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.
Macrocyclic compounds for treatment of medical disorders
Macrocyclic Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, Formula IV, Formula V, Formula VI, Formula VII, and Formula VIII or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.
2-AMINO-N-PHENYL-NICOTINAMIDES AS NAV1.8 INHIBITORS
Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of Na.sub.v1.8 channel activity and may be useful in the treatment, prevention, management, amelioration, control and suppression of diseases mediated by Na.sub.v1.8 channel activity. The compounds of the present invention may be useful in the treatment, prevention or management of pain disorders, cough disorders, acute itch disorders, and chronic itch disorders.
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2-AMINO-N-PHENYL-NICOTINAMIDES AS NAV1.8 INHIBITORS
Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of Na.sub.v1.8 channel activity and may be useful in the treatment, prevention, management, amelioration, control and suppression of diseases mediated by Na.sub.v1.8 channel activity. The compounds of the present invention may be useful in the treatment, prevention or management of pain disorders, cough disorders, acute itch disorders, and chronic itch disorders.
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Complexes and Ligands
The present application provides ligands and fluorescent or luminescent complexes comprising these ligands.
Complexes and Ligands
The present application provides ligands and fluorescent or luminescent complexes comprising these ligands.
Fused Pentacyclic Imidazole Derivatives as Modulators of TNF Activity
A compound of formula (I) as defined herein, or a pharmaceutically acceptable salt thereof, being potent modulators of human TNF a activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
FUSED PYRROLINES WHICH ACT AS UBIQUITIN-SPECIFIC PROTEASE 30 (USP30) INHIBITORS
The disclosure relates to USP30 Inhibitor Compounds I, pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising same, and medical uses involving same. (I)
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FUSED PYRROLINES WHICH ACT AS UBIQUITIN-SPECIFIC PROTEASE 30 (USP30) INHIBITORS
The disclosure relates to USP30 Inhibitor Compounds I, pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising same, and medical uses involving same. (I)
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