4-chloro-6,8-dihydro-5H-pyrido[3,4-d]pyrimidine-7-carboxylic acid

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶并嘧啶类
• 英文名称: 4-chloro-6,8-dihydro-5H-pyrido[3,4-d]pyrimidine-7-carboxylic acid
• 化学式: C₈H₈ClN₃O₂
• 分子量: 213.62
• InChiKey: IADXUPHVLCMZFX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  14
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  66.3
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• [EN] KRAS G12C INHIBITORS<br/>[FR] INHIBITEURS DE KRAS G12C
  申请人：MIRATI THERAPEUTICS INC

  公开号：WO2017201161A1

  公开（公告）日：2017-11-23

  The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.

  本发明涉及抑制KRas G12C的化合物。特别是，本发明涉及不可逆地抑制KRas G12C活性的化合物，包括含有这些化合物的药物组合物及其使用方法。
• KRAS G12C INHIBITORS
  申请人：Mirati Therapeutics, Inc.

  公开号：US20190144444A1

  公开（公告）日：2019-05-16

  The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.

  本发明涉及抑制KRas G12C的化合物。特别地，本发明涉及不可逆抑制KRas G12C活性的化合物、包含这些化合物的药物组合物及其使用方法。
• [EN] SUBSTITUTED FURANOPYRIMIDINE COMPOUNDS AS PDE1 INHIBITORS<br/>[FR] COMPOSÉS FURANOPYRIMIDINE SUBSTITUÉS UTILISÉS EN TANT QU'INHIBITEURS DE PDE1
  申请人：DART NEUROSCIENCE LLC

  公开号：WO2019104285A1

  公开（公告）日：2019-05-31

  Substituted furanopyrimidine chemical entities of Formula (I): wherein Ra has any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive therapies; modulating and treating disorders mediated by PDE1 activity or dopaminergic signaling; treating neurological disorders, CNS disorders, dementia, neurodegenerative diseases, and trauma-dependent losses of function; treating stroke, including cognitive and motor deficits during stroke rehabilitation; facilitating neuroprotection and neurorecovery; enhancing the efficiency of cognitive and motor training, including animal skill training protocols; and treating peripheral disorders, including cardiovascular, renal, hematological, gastroenterological, liver, cancer, fertility, and metabolic disorders.

  化学实体的呋喃嘧啶替代物的化学结构如下（I）：其中Ra具有以下所述的任何值，并含有此类化学实体的组合物；制备它们的方法；以及它们在广泛应用中的使用，包括代谢和反应动力学研究；检测和成像技术；放射性治疗；调节和治疗由PDE1活性或多巴胺信号传导介导的疾病；治疗神经系统疾病，中枢神经系统疾病，痴呆症，神经退行性疾病和依赖创伤的功能丧失；治疗中风，包括中风康复期间的认知和运动缺陷；促进神经保护和神经恢复；增强认知和运动训练的效率，包括动物技能训练方案；以及治疗周围疾病，包括心血管，肾脏，血液，胃肠，肝脏，癌症，生育和代谢性疾病。
• P2X7 MODULATORS
  申请人：ALCAZAR VACA Manuel Jesus

  公开号：US20160024082A1

  公开（公告）日：2016-01-28

  The present invention is directed to a compound of Formula (I) or (Ia) The invention also relates to pharmaceutical compositions comprising compounds of Formula (I) or (Ia) and methods comprising administering of compounds of Formula (I) or (Ia) for treating 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.

  本发明涉及一种公式（I）或（Ia）的化合物。本发明还涉及包含公式（I）或（Ia）化合物的药物组合物以及包括施用公式（I）或（Ia）化合物治疗类风湿性关节炎、骨关节炎、牛皮癣、败血症性休克、过敏性皮炎、哮喘、过敏性哮喘、轻度至重度哮喘、类固醇抵抗性哮喘、特发性肺纤维化、过敏性鼻炎、慢性阻塞性肺疾病、气道高反应性、神经和神经免疫系统疾病、神经病理性疼痛、炎性疼痛、自发性疼痛、阿片类药物引起的疼痛、糖尿病神经病变、带状疱疹性神经痛、腰痛、化疗引起的神经病理性疼痛、纤维肌痛、中枢神经系统有或无神经炎症的疾病、情绪障碍、重度抑郁症、治疗难度大的抑郁症、躁郁症、焦虑抑郁症、焦虑、认知、睡眠障碍、多发性硬化症、癫痫、帕金森病、精神分裂症、阿尔茨海默病、亨廷顿病、自闭症、脊髓损伤和脑缺血/创伤性脑损伤、与压力相关的疾病、心血管、代谢、消化和泌尿系统疾病，如糖尿病、糖尿病、血栓形成、肠易激综合征、克罗恩病、缺血性心脏病、缺血、高血压、心血管疾病、心肌梗死，以及下尿路功能障碍，如失禁、下尿路综合征、多囊肾病、肾小球肾炎、骨骼疾病、骨质疏松症、骨化不全症和青光眼、间质性膀胱炎、咳嗽、输尿管梗阻、败血症、肌萎缩性侧索硬化症、查加氏病、沙眼衣原体感染、神经母细胞瘤、结核病和偏头痛的方法。
• KRas G12C inhibitors
  申请人：Mirati Therapeutics, Inc.

  公开号：US10125134B2

  公开（公告）日：2018-11-13

  The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.

  本发明涉及抑制 KRas G12C 的化合物。特别是，本发明涉及不可逆地抑制 KRas G12C 活性的化合物、包含该化合物的药物组合物及其使用方法。