发明名称 P2X7 MODULATORS
摘要 The present invention is directed to a compound of Formula (I) Formula (I) The invention also relates to pharmaceutical compositions comprising compounds of Formula (I) and methods comprising administering to a subject at least one compound selected from compounds of Formula (I) for treating diseases mediated by P2X7 receptor activity, such as rheumatoid arthritis, osteoarthritis, psoriasis, septic shock, allergic dermatitis, asthma, allergic asthma, mild to severe asthma, steroid resistant asthma, idiopathic pulmonary fibrosis, allergic rhinitis, chronic obstructive pulmonary disease; airway hyper-responsiveness, diseases of the nervous and neuro-immune system, acute and chronic pain states of neuropathic pain, inflammatory pain, spontaneous pain, opioid induced pain, diabetic neuropathy, postherpetic neuralgia, low back pain, chemotherapy-induced neuropathic pain, fibromyalgia, diseases involved with and without neuroinflammation of the central nervous system, mood disorders, major depression, major depressive disorder, treatment resistant depression, bipolar disorder, anxious depression, anxiety, cognition, sleep disorders, multiple sclerosis, epileptic seizures, Parkinson's disease, schizophrenia, Alzheimer's disease, Huntington's disease, autism, spinal cord injury and cerebral ischemia/traumatic brain injury, stress-related disorders, diseases of the cardiovascular, metabolic, gastrointestinal and urogenital systems such as diabetes, diabetes mellitus, thrombosis, irritable bowel syndrome, irritable bowel disease, Crohn's disease, ischemic heart disease, ischaemia, hypertension, cardiovascular disease, myocardial infarction, and lower urinary tract dysfunction such as incontinence, lower urinary tract syndrome, Polycystic Kidney Disease, Glomerulonephritis, skeletal disorders, osteoporosis, osteopetrosis, and glaucoma, interstitial cystitis, cough, ureteric obstruction, sepsis, Amyotrophic Lateral Sclerosis, Chaga's Disease, chlamydia, neuroblastoma, Tuberculosis, and migraine.;
申请公布号 US2016016962(A1) 申请公布日期 2016.01.21
申请号 US201414775417 申请日期 2014.03.14
申请人 JANSSEN PHARMACEUTICA NV 发明人 Ameriks Michael K.;Rech Jason C.;Savall Brad M.;WALL Jessica L.
分类号 C07D487/04;C07D487/14 主分类号 C07D487/04
代理机构 代理人
主权项 1. A compound of Formula Iwherein: each R2 is independently selected from the group consisting of H, halo, SO2CH3, C1-C3 alkyl, NO2, NH2, perhaloalkyl and perhaloalkoxy; or two R2 substituents are taken together to form: n is 0-3; X is H or C1-C3 alkyl; Y is independently selected from the group consisting of H, C1-C3alkyl and C3-C4cycloalkyl; R1 is independently selected from the group consisting of: Ra, Rc and Rg are independently H or halo; Rd is H or C1-C3 alkoxy;Re is independently selected from the group consisting of H, C1-C3 alkyl and halo;Rb, Rf, Rh, Ri, Rj, Rk, Rm, Rn, Ro are independently selected from the group consisting of H, C1-C3 alkyl and perhaloalkyl; andRp is H or C(O)OtBu; or a pharmaceutically acceptable salt of a compound of Formula (I).
地址 Beerse BE