发明名称 Dihydronaphthalene and naphthalene derivatives as N-formyl peptide receptor like-1 (FPRL-1) receptor modulators
摘要 The present invention relates to novel dihydronaphthalene and naphthalene derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
申请公布号 US8846760(B2) 申请公布日期 2014.09.30
申请号 US201414148377 申请日期 2014.01.06
申请人 Allergan, Inc. 发明人 Beard Richard L.;Vuligonda Vidyasagar;Donello John E.;Viswanath Veena;Garst Michael E.;Vu Thong
分类号 A61K31/195;A61K31/16;C07C235/82;C07C235/84;C07C233/59 主分类号 A61K31/195
代理机构 代理人 Ene Doina G.
主权项 1. A method of treating a disorder associated with the N-Formyl peptide receptor 2 modulation, wherein the disorder is selected from: ocular inflammatory diseases, wet age-related macular degeneration, dry age-related macular degeneration, corneal wound healing, uveitis, dry eye, Keratitis, allergic eye diseases, conditions affecting the posterior part of the eye, maculopathies, retinal degeneration, non-exudative age related macular degeneration, exudative age related macular degeneration, choroidal neovascularization, diabetic retinopathy, retinopathy of prematurity acute macular neuroretinopathy, central serous chorioretinopathy, cystoid macular edema, diabetic macular edema, infectious keratitis, herpetic keratitis, corneal angiogenesis, lymphangiogenesis, post-surgical corneal inflammation, and blepharitis, which comprises administering to a mammal in need thereof, a pharmaceutical composition comprising a therapeutically effective amount of at least one compound represented by Formula I or a pharmaceutically acceptable salt thereof:wherein: “” is a single bond or a double bond; “” is a single bond or a double bond; R1 is H, halogen, —S(O)R10, —S(O)2R11, nitro, cyano, —OC1-6 alkyl, —SC1-6 alkyl, —C1-6 alkyl, —C2-6 alkenyl, —C2-6 alkynyl, C(O)R12, NR13R14, C3-8 cycloalkyl, C3-8 cycloalkenyl or hydroxyl; R2 is H, halogen, —S(O)R10, —S(O)2R11, nitro, cyano, —OC1-6 alkyl, —SC1-6 alkyl, —C1-6 alkyl, —C2-6 alkenyl, —C2-6 alkynyl, C(O)R12, NR13R14, C3-8 cycloalkyl, C3-8 cycloalkenyl or hydroxyl; R3 is H, halogen, —S(O)R10, —S(O)2R11, nitro, cyano, —OC1-6 alkyl, —SC1-6 alkyl, —C1-6 alkyl, —C2-6 alkenyl, —C2-6 alkynyl, C(O)R12, NR13R14, C3-8 cycloalkyl, C3-8 cycloalkenyl, C6-10 aryl or hydroxyl; R4 is H or C(O)R12; R5 is H, —OC1-6 alkyl, —SC1-6 alkyl, —C1-6 alkyl, —C2-6 alkenyl or —C2-6 alkynyl; R6 is H, —OC1-6 alkyl, —SC1-6 alkyl, —C1-6 alkyl, —C2-6 alkenyl or —C2-6 alkynyl; Y is O or S; X is O, NR, or CH2; Ra is C6-10 aryl,heteroaryl, C3-8 cycloalkyl, C3-8 cycloalkenyl or H; Rb is halogen; c is 0, 1 or 2; R7 is H, halogen, —S(O)R10, —S(O)2R11, nitro, hydroxyl, cyano, —OC1-6 alkyl, —SC1-6 alkyl, —C1-6 alkyl, —C2-6 alkenyl, —C2-6 alkynyl, C(O)R12, NR13R14, C3-8 cycloalkenyl or C3-8 cycloalkyl; R8 is H, halogen, —S(O)R10, —S(O)2R11, cyano, —OC1-6 alkyl, —SC1-6 alkyl, —C1-6 alkyl, —C2-6 alkenyl, —C2-6 alkynyl, C(O)R12, NR13R14, C3-8 cycloalkenyl or C3-8 cycloalkyl; R9 is H, —S(O)2R11, —OC1-6 alkyl, —SC1-6 alkyl, —C1-6 alkyl, —C2-6 alkenyl, —C2-6 alkynyl, C(O)R12, C3-8 cycloalkenyl or C3-8 cycloalkyl; R10 is —C1-6 alkyl, C3-8 cycloalkyl, or C3-8 cycloalkenyl; R11 is H, hydroxyl, —C1-6 alkyl, C3-8 cycloalkyl or C3-8 cycloalkenyl; R12 is H, hydroxyl, —C1-6 alkyl, C3-8 cycloalkyl, C3-8 cycloalkenyl, NR13R14 or —OC1-6 alkyl; R13 is H, —C1-6 alkyl, C3-8 cycloalkyl, C3-8 cycloalkenyl SO2R11 or C(O)R15; R14 is H, —C1-6 alkyl, C3-8 cycloalkenyl, aryl, heterocycle or C3-8 cycloalkyl; R15 is H, —C1-6 alkyl, C3-8 cycloalkenyl or C3-8 cycloalkyl; and R is H, —C1-6 alkyl, C3-8 cycloalkenyl or C3-8 cycloalkyl; with the provisos when “” is a double bond then R5 and R6 are void; and the compound is not of structures
地址 Irvine CA US