AMIDE DERIVATIVES OF N-CARBAMIDE-SUBSTITUTED AMINO ACIDS AS MODULATORS OF FORMYLPEPTIDE RECEPTOR-1 (FPRL-1) Russian patent published in 2021 - IPC C07C275/28 C07C275/30 C07C317/42 C07C317/50 C07C323/44 C07C323/60 C07D209/20 C07D233/64 C07K5/06 A61K31/17 A61K31/197 A61K31/216 A61K31/4045 A61K31/417 A61P27/00 A61P29/00 

Abstract RU 2744577 C2

FIELD: biochemistry.

SUBSTANCE: invention relates to the use of a compound represented by formula II, enantiomers thereof, diastereoisomers or pharmaceutically acceptable salts in the treatment of a disorder associated with the modulation of the N-formylpeptide receptor 1 (FPRL-1). In formula II, a is equal to 1 and b is equal to 0; a is equal to 0 and b is equal to 1; a is equal to 1 and b is equal to 1; R1 is a C1-8 alkyl, not necessarily substituted by hydroxyl, -NR11R12 or -OR13; R2 is a C1-8 alkyl, not necessarily substituted by C6-10 aryl, amide or heterocycle, the heterocycle is in the form of a 3-10-member aromatic ring containing at least one heteroatom selected from N; one methyl alkyl group can be replaced by sulphur or sulfonyl; R3 is in the form of hydrogen or halogen; R4 is in the form of hydrogen; R5 is a halogen, either -CF3 or -S(O)nR14; n is 0, 1 or 2; R6 is hydrogen; R7 is hydrogen or halogen; R8 is hydrogen or C1-8 alkyl; R9 is hydrogen, C1-8 alkyl, not necessarily substituted for hydroxyl, or C6-10 aryl; R10 is hydrogen, C1-8 alkyl, not necessarily substituted by hydroxyl, or C6-10 aryl; R9a is hydrogen or C1-8 alkyl, not necessarily substituted by hydroxyl; R10a is hydrogen or C1-8 alkyl, not necessarily substituted by hydroxyl; R11 is hydrogen or C1-8 alkyl; R12 is hydrogen or C1-8 alkyl; R13 is hydrogen or C1-8 alkyl; R14 is CF3 or C1-8 alkyl. Furthermore, the disorder associated with the modulation of the N-formylpeptide receptor 1 is selected from a group consisting of inflammatory eye diseases, including, but not limited to, uveitis, dryness of the eye, keratitis, allergic eye disease, infectious keratitis, herpetic keratitis, corneal angiogenesis, lyfangiogenesis, retinitis, chorioiditis, acute multifocal placoid pigment epithelial disease, Behçet's disease, postoperative retinal healing, wet and dry age-related macular degeneration (ARMD); systemic inflammatory diseases; pain; immunological disorders; healing of skin wounds; burns; pink acne; atopic dermatitis; acne; psoriasis; seborrhea dermatitis; actic keratosis; common warts; photoaging; rheumatoid arthritis and related inflammatory disorders.

EFFECT: invention enables effective treatment of a disorder associated with the modulation of the N-formylpeptide receptor 1 (FPRL-1).

Formula II

39 cl, 5 tbl, 4 ex

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RU 2 744 577 C2

Authors

Bird Richard L.

Duong Ten T.

Donello Dzhon E.

Visvanat Veena

Garst Majkl E.

Dates

2021-03-11Published

2012-10-23Filed