Back to results
US 2026/0125347 A1Published application
l,2-SUBSTITUTED 3-OXOPYRAZOLIDINE DERIVATIVES AS PROSTAGLANDIN E2 RECEPTOR 4 (EP4) AGONISTS FOR THE TREATMENT OF GASTROINTESTINAL AND PULMONARY DISEASES
AssigneeNxera Pharma UK Limited
InventorsNigel Alan SWAIN, Benjamin WHITEHURST, Miles Stuart CONGREVE, Giles Albert BROWN
Life of this patent
Estimating the term…
Abstract
The present invention relates to compounds of formula I as prostaglandin E2 receptor 4 (EP4) agonists for use in methods of treatment of gastrointestinal and pulmonary dis-cases or disorders. An exemplary compound is e.g. 4-(2-(2-(3-hydroxy-3-(4′-hydroxy-2′-methyl-[1,1′-biphenyl]-3-yl) propyl)-5-oxopyrazolidin-1-yl)ethyl)benzoic acid (Example 1) Pharmacological data is provided, e.g.
Claims24
A compound of the Formula I:
- or a pharmaceutically acceptable salt solvate, hydrate, tautomer or optical isomer thereof, wherein;
- A is OR′, C(O)R′, CO2R′, C(O)N(R′)2, C(O)N(R′)S(O)2R3, S(O)2R′, S(O)2OR′, SO2N(R′)2, C1-8 alkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl;
- X is halo, OR′, COOR′, or C1-6 alkyl;
- L and L′are each independently a C2-4 alkylene;
- R1 is H, halo, CN, NO2, OR′, SR′, COOR′, C1-6 alkoxy, or C1-6 alkyl;
- R2 is OR′, OC(O)R3, OC(O)OR3, CO2R′, CON(R′)2, SO2N(R′)2, SO2R3, OSO2R3, or OSO2N(R′)2;
- R3 is C1-6 alkyl, C3-6 cycloalkyl, or a phenyl;
- R′ is H, C1-6 alkyl, or C3-6 cycloalkyl;
- and
- n is 0, 1, 2, or 3;
- wherein at each occurrence, alkyl, alkylene, alkoxy, and cycloalkyl are each optionally and independently substituted with up to 3 instances of OH, SH, CN, NO2, COOH, halo, or COOC1-4 alkyl;
- wherein at each occurrence, heterocycloalkyl, aryl, and heteroaryl are each optionally and independently substituted with up to 3 instances of OR′, SR′, CN, NO2, CO2R′, halo, C1-4 alkyl, or oxo.
9 more elements
(canceled)
Dependencies are inferred from the claim text.