本周专利共13篇。百时美施贵宝公开4篇NS3/NS4A抑制剂专利， 用于治疗丙肝；Zafgen, Inc.公开2篇MetAP2抑制剂，用于治疗肥胖症；Allergan, Inc.公开2篇S1P1受体的配体专利，用于治疗过敏、自身免疫疾病等；此外，罗氏，默克，辉瑞等公司，分别有1篇专利公开。
1. WO 2014071007标题: Hepatitis C virus inhibitors
申请人: 百时美施贵宝
优先权日期及相关专利公开号: 2012 US 721565
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: 丙肝
专利摘要: Hepatitis C virus inhibitors having the general formula (I) [PLEASE INSERT CHEMICAL STRUCTURE HERE], are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
备注: NS3 NS4A蛋白酶抑制剂被证明对HCV感染有治疗效果。本发明提供的化合物可以抑制基因1a和1b型HCV,相应的IC50分别为0.46 nM和0.40 nM.
2. WO 2014071032标题: Hepatitis C virus inhibitors
申请人: 百时美施贵宝
优先权日期及相关专利公开号: 2012 US 721560
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: 丙肝
专利摘要: Hepatitis C virus inhibitors having the general formula (I), are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
备注: NS3 NS4A蛋白酶抑制剂被证明对HCV感染有治疗效果。本发明提供的化合物可以抑制基因1a和1b型HCV,相应的IC50分别为0.85 nM和0.89 nM.
3. WO 2014070974标题: Hepatitis C virus inhibitors
申请人: 百时美施贵宝
优先权日期及相关专利公开号: 2012 US 722317
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: 丙肝
专利摘要: Hepatitis C virus inhibitors having the general formula (I) are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
备注: NS3 NS4A蛋白酶抑制剂被证明对HCV感染有治疗效果。本发明提供的化合物可以抑制基因1a和1b型HCV,相应的EC50分别为0.96 nM和0.33 nM.
4. WO 2014070964标题: Hepatitis C virus inhibitors
申请人: 百时美施贵宝
优先权日期及相关专利公开号: 2012 US 721564
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: 丙肝
专利摘要: Hepatitis C virus inhibitors having the general formula (I) are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
备注: NS3 NS4A蛋白酶抑制剂被证明对HCV感染有治疗效果。本发明提供的化合物可以抑制基因1a和1b型HCV,相应的IC50分别为0.41 nM和0.28 nM.
5. WO 2014071369标题: Tricyclic compounds for use in the treatment and/or control of obesity
申请人: Zafgen, Inc.
优先权日期及相关专利公开号: 2012 US 722449
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: 肥胖
专利摘要: The invention provides tricyclic compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.
备注: MetAP2 抑制剂被用于治疗肥胖。本发明提供的化合物对MetAP2 的IC50小于0.05 mcM.
6. WO 2014071363
标题: Tricyclic compounds and methods of making and using same
申请人: Zafgen, Inc.
优先权日期及相关专利公开号: 2012 US 722455
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: 肥胖
专利摘要: The invention provides tricyclic compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.
备注: MetAP2 抑制剂被用于治疗肥胖。本发明提供的化合物对MetAP2 的IC50小于0.05 mcM.
7. WO 2014071355标题: 1,3,4-Oxadiazoles-2-thio azetidine derivatives as sphingosine-1 phosphate receptors modulators
申请人: Allergan, Inc.
优先权日期及相关专利公开号: 2013 US 70725
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: 过敏症、自身免疫疾病、癌症、眼疾、炎症、疼痛和糖尿病视网膜病变
专利摘要: The present invention relates to substituted 1,3,4-oxadiazoles-2-thio azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
备注: S1P1受体的配体可以用于治疗过敏症、自身免疫疾病、癌症、眼疾、炎症、疼痛和糖尿病视网膜病变、肺气肿、骨关节炎等疾病。本发明提供的化合物对S1P1的EC50=22.9 nM 。
8. WO 2014071342标题: 1,3,4-Oxadiazoles-2-thio derivatives as sphingosine-1 phosphate receptors modulators
申请人: Allergan, Inc.
优先权日期及相关专利公开号: 2012 US 722650
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: 过敏症、自身免疫疾病、癌症、眼疾、炎症、疼痛和糖尿病视网膜病变
专利摘要: The present invention relates to substituted 1,3,4-oxadiazoles-2-thio derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
备注: S1P1受体的配体可以用于治疗过敏症、自身免疫疾病、癌症、眼疾、炎症、疼痛和糖尿病视网膜病变、肺气肿、骨关节炎等疾病。本发明提供的化合物对S1P1的EC50=8.4 nM 。
9. WO 2014072257标题: Pyrazine derivatives
申请人: 罗氏
优先权日期及相关专利公开号: 2012 EP 191529
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: 抑郁、神经错乱、癫痫、焦虑、糖尿病、阿尔兹海默和帕金森症
专利摘要: The present invention relates to compounds of formula (I), wherein R1R2 are hydrogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, cycloalkyl, OCH2-cycloalkyl or heterocycloalkyl which is optionally substituted by halogen, with the proviso that one of R1 and R2 is hydrogen, or R1 and R2 form together with the carbon atom to which they are attach a phenyl ring, which may be optionally substituted by lower alkyl; R3/R4 are hydrogen, halogen or cyano; with the proviso that one of R3 and R4 is hydrogen; or to a pharmaceutically suitable acid addition salt thereof, to all racemic mixtures, all their corresponding enantiomers and/or optical isomers, which may be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson’s disease, neurodegenerative disorders, Alzheimer’s disease, epilepsy, migraine, hypertension, substance abuse, metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
备注: TAAR1配体可用于治疗抑郁、神经错乱、癫痫、焦虑、糖尿病、阿尔兹海默和帕金森症。本发明所提供的化合物对鼠源的TAAR1的Ki值为0.0037~0.0053 mcM.
10. WO 2014074422
标题: Amino-pyridine-containing spleen tyrosine kinase (Syk) inhibitors
申请人: 默克
优先权日期及相关专利公开号: 2012 US 723575
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: 哮喘和慢性阻塞性肺疾病
专利摘要: The invention provides certain amino-pyridine-containing compounds of the Formula (I) (I) or pharmaceutically acceptable salts thereof, wherein R3, R4, R5, R6, and the subscript n are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
备注: SYK激酶抑制剂可用于治疗哮喘和慢性阻塞性肺疾病。本发明所提供的化合物对SYK的IC50约为0.002 nM.
11. WO 2014072881标题: Heteroaromatic compounds and their use as dopamine D1 ligands
申请人: 辉瑞
优先权日期及相关专利公开号: 2013 US 881218
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: 焦虑、疼痛、精神错乱、药物滥用和成瘾、心血管疾病、肾衰竭、肥胖和糖尿病
专利摘要: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof and N-oxides thereof; processes and intermediates for preparation of; and compositions and uses thereof. The present invention further provides D1 agonists with reduced D1R desensitization, D1 agonists with a reduced ß- arrestin recruitment activity relative to Dopamine, D1 agonists interacting significantly with the Ser188 but not significantly with the Ser202 of a D1R when binding to the D1R, D1 agonists interacting less strongly with the Asp103 and interacting less strongly with the Ser198 of a D1R when binding to the D1R, and their uses.
备注: 多巴胺D1受体激动剂可用于治疗焦虑、疼痛、精神错乱、药物滥用和成瘾、心血管疾病、肾衰竭、肥胖和糖尿病等疾病。本发明提供的化合物可以抑制[3H]-SCH-23390与D1受体的结合（Ki=5.76 nM）。对D1的EC50=0.037nM.此外，化合物也展示了对野生型和S188I,S202A,S198A,D103A突变的D1受体具有部分激动效应。
12. WO 2014071044
标题: Substituted 6,7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (PDE10A)
申请人: Allergan, Inc.、Diaxonhit SA
优先权日期及相关专利公开号: 2012 US 721260
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: 焦虑、肥胖、糖尿病、疼痛、帕金森综合症、亨廷顿症、阿尔兹海默、运动障碍、糖尿病症
专利摘要: The invention relates to compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R’, R1 through R7 and Ar are as defined herein. These compounds are useful as inhibitors of phosphodiesterase 10 (PDE10A) which are useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type II diabetes, metabolic syndrome, glucose intolerance, pain and ophthalmic diseases.
备注: PDE10A可用于治疗焦虑、肥胖、糖尿病、疼痛、帕金森综合症、亨廷顿症、阿尔兹海默、运动障碍、糖尿病症等疾病。本发明中提供的化合物对PDE10A的IC50=0.18 nM 。
13. WO 2014070979标题: Inhibitors of cytomegalovirus
申请人: 勃林格殷格翰
优先权日期及相关专利公开号: 2012 US 722152
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: 巨细胞病毒感染
专利摘要: Compounds of Formula (I) wherein n, R1, R1A, R2, R4 and Z are defined herein, are useful for the treatment of cytomegalovirus disease and/or infection.
备注: 巨细胞病毒CMV DNA聚合酶抑制剂可以治疗巨细胞病毒感染。本发明中的化合物可以抑制巨细胞病毒CMV的活性，其EC50=180 nM.
(by 浮米网)
