发明名称 Organic compounds
摘要 Provided are PDE1 inhibitors of Formula I, processes for their production, their use as pharmaceuticals, and pharmaceutical compositions comprising them.
申请公布号 US9556186(B2) 申请公布日期 2017.01.31
申请号 US201514731233 申请日期 2015.06.04
申请人 INTRA-CELLULAR THERAPIES, INC. 发明人 Li Peng;Zheng Hailin;Zhao Jun;Wennogle Lawrence P.
分类号 C07D487/14;A61K31/519;A61K45/06;A61K31/5575 主分类号 C07D487/14
代理机构 Hoxie & Associates LLC 代理人 Hoxie & Associates LLC
主权项 1. A method of treating any of the following conditions: Parkinson's disease, restless leg, tremors, dyskinesias, Huntington's disease, Alzheimer's disease, drug-induced movement disorders, depression, attention deficit disorder, attention deficit hyperactivity disorder, bipolar illness, anxiety, sleep disorder, narcolepsy, cognitive impairment, e.g., cognitive impairment of schizophrenia, dementia, Tourette's syndrome, autism, fragile X syndrome, psychostimulant withdrawal, drug addiction, cerebrovascular disease, stroke, congestive heart disease, hypertension, pulmonary hypertension, sexual dysfunction, asthma, chronic obstructive pulmonary disease, allergic rhinitis, autoimmune diseases, inflammatory diseases, female sexual dysfunction, exercise amenorrhoea, anovulation, menopause, menopausal symptoms, hypothyroidism, pre-menstrual syndrome, premature labor, infertility, irregular menstrual cycles, abnormal uterine bleeding, osteoporosis, multiple sclerosis, prostate enlargement, prostate cancer, hypothyroidism, estrogen-induced endometrial hyperplasia or carcinoma, glaucoma, elevated intraocular pressure, psychosis, e.g., schizophrenia, schizoaffective disorder, schizophreniform disorder, psychotic disorder, delusional disorder, and mania, such as in acute manic episodes and bipolar disorder, traumatic brain injury, and/or any disease or condition characterized by low levels of cAMP and/or cGMP (or inhibition of cAMP and/or cGMP signaling pathways) in cells expressing PDE1, and/or by reduced dopamine D1 receptor signaling activity, and/or any disease or condition that may be ameliorated by the enhancement of progesterone signaling, comprising administering an effective amount of a compound of Formula I: wherein (i) R1 is H or C1-4 alkyl;(ii) R2 and R3 are independently H or C1-6 alkyl;(iii) R4 is H or C1-4 alkyl;(iv) R5 is aryl optionally substituted with one or more groups independently selected from —C(═O)—C1-6 alkyl and C1-6-hydroxyalkyl;(ii) R6 and R7 are independently H; aryl optionally substituted with one or more groups independently selected from C1-6 alkyl and halogen unsubstituted phenyl; phenyl substituted with one or more halogen; phenyl substituted with one or more C1-6 alkyl and one or more halogen; or phenyl substituted with one C1-6 alkyl and one halogen; and(vi) n is 1, 2, 3, or 4, in free or pharmaceutically acceptable salt form, to a patient in need thereof.
地址 New York NY US