发明名称 Benzofuran-2-sulfonamides pyridine derivatives as chemokine receptor modulators
摘要 The present invention relates to novel benzofuran-2-sulfonamide pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
申请公布号 US9416120(B2) 申请公布日期 2016.08.16
申请号 US201414334145 申请日期 2014.07.17
申请人 Allergan, Inc. 发明人 Yuan Haiqing;Beard Richard L.;Garst Michael E.;Liu Xiaoxia;Donello John E.;Viswanath Veena
分类号 A61K31/44;A01N43/40;C07D307/78;C07D405/12;C07D307/82;C07D405/14 主分类号 A61K31/44
代理机构 代理人 Bass Jonathan York
主权项 1. A method of treating a disorder associated with chemokine receptor modulation, which comprises administering to a mammal in need thereof, a pharmaceutical composition comprising a therapeutically effective amount of at least one compound of Formula Iwherein: R1 is hydrogen, halogen, CN, substituted or unsubstituted C1-6 alkyl, OR12, NR13R14, or COR15; R2 is hydrogen, halogen, CN, substituted or unsubstituted C1-6 alkyl, OR12, NR13R14, or COR15; R3 is hydrogen, halogen, CN, substituted or unsubstituted C1-6 alkyl, OR12, NR13R14, or COR15; R4 is hydrogen, halogen, CN, substituted or unsubstituted C1-6 alkyl, OR12, NR13R14, or COR15; R5 is hydrogen, halogen, CN, substituted or unsubstituted C1-6 alkyl, OR12, NR13R14, or COR15; R6 is hydrogen, halogen, CN, substituted or unsubstituted C1-6 alkyl, OR12, NR13R14, or COR15; R7 is hydrogen, halogen, CN, substituted or unsubstituted C1-6 alkyl, OR12, NR13R14, or COR15; R8 is hydrogen, halogen, CN, substituted or unsubstituted C1-6 alkyl, OR12, NR13R14, or COR15; R9 is O, C(O), S, S(O), S(O)2, —C(═NOR16)—; a is 0 or 1; R11 is hydrogen, CN, substituted or unsubstituted C1-6 alkyl, CF3, OR12, NR13R14, substituted or unsubstituted C6-10 aryl, substituted or unsubstituted heterocycle, substituted or unsubstituted C3-8 cycloalkyl, substituted or unsubstituted C2-6 alkyne, substituted or unsubstituted C2-6 alkene or COR15; R12 is hydrogen or substituted or unsubstituted C1-6 alkyl; R13 is hydrogen or substituted or unsubstituted C1-6 alkyl or can from an optionally substituted heterocycle with R14; R14 is hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted heterocycle or substituted or unsubstituted C6-10 aryl or can from an optionally substituted heterocycle with R13; R15 is hydrogen, hydroxyl, substituted or unsubstituted heterocycle, substituted or unsubstituted C6-10 aryl or substituted or unsubstituted C1-6 alkyl; R16 is hydrogen or substituted or unsubstituted C1-6 alkyl; and R18 is hydrogen or substituted or unsubstituted C1-6 alkyl;wherein the disorder associated with chemokine receptor modulation is: an ocular inflammatory disease selected from: uveitis, retinal degenerative conditions, angiogenesis, dry eve, Keratitis, allergic eve disease, conditions affecting the posterior part of the eye, retinal degeneration, non-exudative age related macular degeneration, exudative age related macular degeneration, choroidal neovascularization, diabetic retinopathy, acute macular neuroretinopathy, central serous chorioretinopathy, cystoid macular edema, and diabetic macular edema, retinitis, acute multifocal placoid pigment epitheliopathy, Behcet's disease, birdshot retinochoroidopathy, multifocal choroiditis, multiple evanescent white dot syndrome, ocular sarcoidosis, posterior scleritis, serpiginous choroiditis, subretinal fibrosis and Vogt-Koyanagi-and Harada syndrome; or a skin inflammatory disease selected from: rosacea , sunburn, chronic sun damage, discreet erythemas, psoriasis, atopic dermatitis, menopause-associated hot flashes, hot flashes resulting from orchiectomvatopic dermatitis, photoaging, seborrheic dermatitis, acne, allergic dermatitis, irritant dermatitis, telangiectasia of the face, rhinophyma , red bulbous nose, acne-like skin eruptions, burning or stinging sensation of the face, cutaneous hyperactivity with dilation of blood vessels of the skin, Lyell's syndrome, Stevens-Johnson syndrome, erythema multiforme minor, erythema multiforme, actinic keratoses, arsenic keratoses, inflammatory acne, non inflammatory acne, eczema and wound healing.
地址 Irvine CA US