本周共有14篇专利。罗氏公开分别用于治疗癌症和炎症的3篇药物专利；诺华公开1篇用于治疗黄斑变性的抗体专利，1篇治疗登革热的前药专利；拜耳公开1篇用于治疗血友病的抗体专利；国内的广东东阳光公开4篇专利，包括ALK，c-MET，NS5A抑制剂等专利；此外杭州海盛医药化工公开1篇mTOR抑制剂专利；南京圣和公开1篇激酶抑制剂专利。
1. WO 2014082889、US 2014148443标题: Novel imidazolines as dual inhibitors of MDM2 and MDMX
申请人: 罗氏
优先权日期及相关专利公开号: 2012 US 730638
相关候选药物化学结构:
适应症: 癌症
专利摘要: Disclosed are compounds of Formula I or pharmaceutically acceptable salts thereof, wherein X1, X2, X3, R1, R2 and R3 are as described in this application, methods for making said compounds as well as methods of using them in the treatment of cancer.
备注: MDM2抑制剂可以治疗癌症。本发明的化合物可以抑制p53和MDM2的相互作用(IC50 = 0.0042 mcM)，且对p53和MDM4的相互作用具有选择性(IC50 = 0.9735 mcM)。
2. WO 2014086667标题: Substituted isoxazole amine compounds as inhibitors of SCD1
申请人: 罗氏
优先权日期及相关专利公开号: 2012 US 732463
相关候选药物化学结构:
适应症: 癌症
专利摘要: The invention is concerned with a compound of formula (I) wherein R1 to R3 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
备注: SCD1抑制剂可以用于治疗癌症。本发明的化合物对SCD1的IC50为40 nM。
3. WO 2014086697标题: Substituted thiazole compounds
申请人: 罗氏
优先权日期及相关专利公开号: 2012 US 733980
相关候选药物化学结构:
适应症: 类风湿性关节炎、红斑狼疮和炎症性肠病
专利摘要: The invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and using the compounds of formula (I) as well as pharmaceutical compositions containing such compounds. The compounds of formula (I) are LMP7 inhibitors and may be useful in treating associated inflammatory diseases and disorders such as, for example, rheumatoid arthritis, lupus and irritable bowel disease.
备注: LPM7抑制剂可以治疗类风湿性关节炎、红斑狼疮和炎症性肠病。 本发明的化合物可抑制proteasome beta 5i（IC50 = 0.247mcM）。
4. WO 2014089111标题: Compositions and methods for antibodies targeting EPO
申请人: 诺华
优先权日期及相关专利公开号: 2012 US 733566
相关候选药物类型: 抗体
相关候选药物化学结构:
适应症: 黄斑变性、
专利摘要: The present invention relates to compositions and methods for the inhibition of EPO. The invention provides antibodies and antigen binding fragments thereof that bind to EPO and are able to inhibit EPO-dependent cell proliferation and/or EPO-dependent cell signaling.
备注:
5. WO 2014082935标题: Cyclic nucleoside derivatives and uses thereof
申请人: 诺华
优先权日期及相关专利公开号: 2012 SG 8891
相关候选药物类型: 前药
相关候选药物化学结构:
适应症: 登革热
专利摘要: A compound of Formula (I) is provided that has been shown to be useful for treating a disease caused by a viral infection wherein R1, R2 and R3 are as defined herein.
备注: 2′-deoxy-2′(R)-fluoro-2′-methylguanosine triphosphate (NTP) 的磷酸盐前药可以治疗病毒性感染疾病，尤其是登革热。本发明的化合物在外周血单核细胞中，可以抑制登革热空斑形成(EC50 = 0.23 mcM)。在人肝脏S9细胞和肝微粒体中的半衰期分别为76和47分钟。
6. WO 2014085208标题: 2-Pyridylamino-4-nitrile-piperidinyl orexin receptor antagonists
申请人: 默克
优先权日期及相关专利公开号: 2012 US 730144
相关候选药物类型: 小分子药物
相关候选药物化学结构:
适应症: 睡眠障碍、肥胖
专利摘要: The present invention is directed to 2-pyridylamino-4-nitrile-piperidinyl compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridylamino-4-nitrile-piperidinyl compounds described herein in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
备注: Orexin OX-2受体拮抗剂可以治疗失眠等睡眠障碍和肥胖。本发明的化合物可以抑制人源OX-2受体(IC50 = 7 nM)，且对OX-1受体具有选择性(IC50 = 1149 nM)。
7. WO 2014085211标题: Spirocyclic sulfones as gamma secretase inhibitors
申请人: 默克
优先权日期及相关专利公开号: 2012 US 731025
相关候选药物类型: 小分子药物
相关候选药物化学结构:
适应症: 阿尔兹海默、唐氏综合症、中风等
专利摘要: Disclosed herein are compounds of Formula (I), wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and use of the compound in the treatment of neurodegenerative diseases or conditions such as Alzheimer’s disease.
备注: gamma-Secretase抑制剂可以治疗阿尔兹海默和神经退行性疾病。 本发明的化合物可以抑制Abeta40产生（IC50=5.4 nM）。
8. WO 2014085527标题: Humanized monoclonal antibodies against activated protein C and uses thereof
申请人: 拜耳
优先权日期及相关专利公开号: 2012 US 731368
相关候选药物类型: 抗体
相关候选药物化学结构:
适应症: 血友病、败血症
专利摘要: Provided are humanized antibodies that selectively bind to and inhibit activated protein C without binding to or inhibiting unactivated protein C. Methods of treatment employing these antibodies are described herein.
备注: 本发明的人源单克隆IgG kappa抗体可以用于治疗血友病和败血症。其可以抑制活化的C蛋白（APC）， ka值为1.46E+06 M-1.s-1, kd值为0.005538 s-1，KD 值为3.80E-06M。
9. WO 2014089324标题: Substituted cyclic compounds and methods of use
申请人: Calitor Sciences, 广东东阳光药业有限公司
优先权日期及相关专利公开号: 2012 US 734903
相关候选药物类型: 小分子药物
相关候选药物化学结构:
适应症: 癌症、骨髓增生性疾病、动脉粥样硬化、肺纤维化
专利摘要: The present invention provides novel substituted alkynyl compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans
备注: ALK 和/或HGFR (MET; c-Met)抑制剂可以治疗增殖性疾病，如癌症、骨髓增生性疾病、动脉粥样硬化和肺纤维化等。 本发明中的化合物对ALK和c-MET的IC50分别为 8 nM和1 nM。在大鼠和人肝脏microsomes稳定性实验中的半衰期和清除率分别为14.5分钟和171.29 ml/min/kg（大鼠）、 33.7 分钟和 51.58 ml/min/kg（肝脏microsomes稳定性实验）。
10. WO 2014089280标题: Alkynyl compounds and methods of use
申请人: Calitor Sciences, 广东东阳光药业有限公司
优先权日期及相关专利公开号: 2012 US 734897
相关候选药物类型: 小分子药物
相关候选药物化学结构:
适应症: 癌症、骨髓增生性疾病、动脉粥样硬化、肺纤维化
专利摘要: The present invention provides novel substituted alkynyl compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
备注: ALK 和/或HGFR (MET; c-Met)抑制剂可以治疗增殖性疾病，如癌症、骨髓增生性疾病、动脉粥样硬化和肺纤维化等。 本发明中的化合物对ALK的IC50为58 nM。在大鼠和人肝脏microsomes稳定性实验中的半衰期和清除率分别为716.1分钟和3.5 ml/min/kg（大鼠）、 418分钟和4.2 ml/min/kg（肝脏microsomes稳定性实验）。
11. WO 2014082379标题: Spiro ring compound as hepatitis C virus (HCV) inhibitor and uses thereof field of the invention
申请人: 广东东阳光药业有限公司
优先权日期及相关专利公开号: 2012 CN 10495665、2013 CN 10116312
相关候选药物化学结构:
适应症: Hepatitis C (HCV)
专利摘要: A compound of formula (I) or a stereoisomer, a geometric isomer. a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof is provided, which can be used for treating HCV infection or a HCV disorder. Also a pharmaceutical composition comprising the compound and the use of the compound and the pharmaceutical composition thereof are provided, which can also be used for treating HCV infection or a HCV disorder.
备注: NS5A抑制剂可以治疗丙肝。本发明的化合物可以抑制基因1a（EC50 = 0.023nM）和基因1b型HCV重组(EC50 = 0.006 nM）。
12. WO 2014082380标题: Fused ring compounds as hepatitis C virus inhibitors, pharmaceutical compositions and uses thereof
申请人: 广东东阳光药业有限公司
优先权日期及相关专利公开号: 2013 CN 10116819、2012 CN 10497565
相关候选药物类型: 小分子药物
相关候选药物化学结构:
适应症: Hepatitis C (HCV)
专利摘要: Provided are fused tricyclic compounds effective to inhibit the function of the NS5A protein of formula (I), wherein X, X’, Y, Y’, A, A’,Q1, Q2, R1-R4, X4, R5a, f and W are defined as in the description. Also provided herein are pharmaceutical compositions thereof, and uses in the manufacture of a medicament for treating HCV infection or a HCV disorder thereof.
备注: NS5A抑制剂可以治疗丙肝。本发明的化合物可以抑制基因1a（EC50 = 0.003nM）和基因1b型HCV重组(EC50 = 0.001nM）。
13. WO 2014082286标题: Rafamycin analogs and methods for making same
申请人: 杭州海盛医药化工有限公司
优先权日期及相关专利公开号: 2012 CN 85631
相关候选药物类型: 小分子药物
相关候选药物化学结构:
适应症: 癌症、自身免疫疾病
专利摘要: A semi-synthetic rapamycin analog with a triazole moiety or a pharmaceutically acceptable salt or prodrug thereof, is a broad-spectrum cytostatic agent and a m TOR inhibitor, and is useful in the treatment of various cancers, or tumors in organs such as kidney, liver, breast, head and neck, lung, prostate, and restenosis in coronary arteries, peripheral arteries, and arteries in the brain, immune and autoimmune diseases. Also disclosed are fungal growth-, restenosis-, post- transplant tissue rejection- and immune- and autoimmune disease- inhibiting compositions and a method of inhibiting cancer, fungal growth, restenosois, post-transplant tissue rejection, and immune and autoimmune disease in a mammal. One particular preferred application of such triazole-moiety containing rapamycin analog is in treating renal carcinoma, lung cancer, colon cancer, and breast cancers wherein potency of the drug, its half-life, tissue distribution properties, and its pharmacokinetic properties including bioavailability through oral and intravenous routes are essential to the clinical outcomes.
备注: mTOR抑制剂可以治疗癌症和免疫性疾病（如类风湿性关节炎、系统性红斑狼疮,移植排斥反应,桥本甲状腺炎、多发性硬化症、重症肌无力、葡萄膜炎、移植物抗宿主病,脑脊髓炎和过敏等）。本发明的化合物对mTOR的IC50为23.77 nM。
14. WO 2014082578
标题: Heteroaryl alkyne compound and application thereof
申请人: 南京圣和药业有限公司
优先权日期及相关专利公开号: 2012 CN 10493364
相关候选药物类型: 小分子药物
相关候选药物化学结构:
适应症: 癌症
专利摘要: The present invention relates to the field of the chemical medicines, and in particular, to a compound with a Heteroaryl alkyne structure shown in formula I or pharmaceutically acceptable salts, isomers, solvate, crystal or prodrug thereof, pharmaceutical compositions containing there compounds and applications of these compounds or compositions in the medicine preparation. The compound of the present invention has a strong inhibiting effect on BCR-ABL kinase, and can be used for treating, for example, neoplastic diseases.
备注: 蛋白激酶抑制剂可以治疗癌症。本发明的化合物在SD鼠中展示了良好的药代动力学性质（在15 mg/kg i.g.给药时，半衰期为4.1小时,Tmax =7.33小时, Cmax = 375.77 ng/ml, AUC (0-t) = 5367.4 h·ng/ml , AUC(0-inf) = 5224.2 h·ng/ml; and at 3 mg/kg i.v.: t1/2 4.93 h, Cmax = 1265.1 ng/ml, AUC (0-t) = 3297.84 h·ng/ml ，AUC(0-inf) = 3380.39 h·ng/ml，生物利用度F = 32.6 %）。
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