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US 2019/0167701 A1Published application
Methods of Treating Eye Pain With Aminophosphinic Derivatives
AssigneePharmaleads
InventorsHervé PORAS, Michel WURM, Stéphane MELIK PARSADANIANTZ, Annabelle REAUX-LE GOAZIGO
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Abstract
The disclosure relates to a method of treating or preventing eye pain in a subject in need thereof. The method includes administering a compound of formula (I), R1—NH—CH(R2)—P(═O)(OH)—CH2—C(R3)(R4)—CONH—C(R5)(R6)—COOR7, to the subject.
Claims20
A method for treating or preventing eye pain in a subject in need thereof, the method comprising:
- administering a compound having formula (I) to the subject, the compound having formula (I) being:
- R1—NH—CH(R2)—P(═O)(OH)—CH2—C(R3)(R4)—CONH—C(R5)(R6)—COOR7
- wherein:
- R1 is:
- a hydrogen
- an (acyloxy)alkyl carbamate group —C(═O)—O—C(R)(R′)—OC(═O)—R″ wherein R and R′ are each independently a hydrogen, an alkyl group and R″ is an alkyl group;
- R2 is:
- a linear or branched, saturated or unsaturated hydrocarbon chain having from 1 to 6 carbon atoms;
- R3 and R4 are each independently:
- a hydrogen
- a phenyl or benzyl group, optionally substituted on the phenyl ring by:
- 1 to 5 halogen atoms;
- an OH, SH, OR″ or SR″ radical, R″ is an alkyl group;
- an amino group optionally mono- or di-substituted by a cyclic or linear aliphatic group having from 1 to 6 carbon atoms;
- a trifluoromethyl group;
- an aromatic or heteroaromatic group having 5 or 6 atoms;
- a heteroaromatic group having 5 or 6 atoms, containing 1 or 2 heteroatom(s) selected from oxygen, nitrogen or sulphur, wherein the sulphur and nitrogen atoms may be oxidized in S-oxide or N-oxide form;
- a methylene substituted by an aromatic or saturated heterocycle having 5 or 6 atoms, the heteroatom being an oxygen, a nitrogen or a sulphur, wherein the nitrogen and sulphur atoms may be oxidized in N-oxide or S-oxide form;
- R3 and R4 are not simultaneously a hydrogen atom;
- R5 and R6 are each independently:
- a hydrogen atom;
- a linear or branched, saturated or unsaturated hydrocarbon chain having from 1 to 6 carbon atoms;
- R7 is:
- a hydrogen;
- a CH2COOR′″ or CH(CH3)COOR′″ radical, R′″ being:
- a saturated hydrocarbon chain having from 1 to 6 carbon atoms, optionally substituted by a C1 to C3 alkoxy group;
- a C5 to C8 cycloalkyl group;
- a phenyl, benzyl or alkyl group;
- a CH(R)O—C(O)OR′ or CH(R)OC(O)R′ group wherein R and R′ are each independently a hydrogen or an alkyl group;
- or a pharmaceutically acceptable salt thereof.
27 more elements
Dependencies are inferred from the claim text.