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浮米每周专利快讯：2015年4月（一） 作者：浮米网 来源：浮米网 2015-04-01
1. WO 2015033303 标题: Cyclic peptidomimetic compounds as immunomodulators 申请人: Aurigene Discovery Technologies Ltd. 优先权日期及相关专利公开号: 2013 IN 4010 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、真菌感染 专利摘要: The present invention relates to cyclic peptidomimetic compounds as therapeutic agents capable of inhibiting the programmed cell death 1 (PD1) signalling pathway. The invention also relates to derivatives of the therapeutic agents. The invention also encompasses the use of the said therapeutic agents and derivatives for treatment of disorders via immunopotentiation comprising inhibition of immunosuppressive signal induced due to PD-1, PD-L1, or PD-L2 and therapies using them. 备注: PD-1(CD279) 抑制剂可用于治疗癌症、细菌、病毒和真菌感染。本发明的化合物在100 nM的CFSE中对PDL-1的抑制率为93%。 2. WO 2015036927 标题: Immunomodulating peptidomimetic derivatives 申请人: Aurigene Discovery Technologies Ltd. 优先权日期及相关专利公开号: 2013 IN 4044 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、细菌、病毒、真菌感染 专利摘要: The present invention relates to immunomodulating peptidomimetic derivatives as therapeutic agents capable of inhibiting the programmed cell death 1 (PD1) signalling pathway. The invention also refers to derivatives of the therapeutic agents. The invention also encompasses the use of the said therapeutic agents and derivatives for treatment of disorders via immunopotentiation comprising inhibition of immunosuppressive signal induced due to PD-1, PD-L1, or PD-L2 and therapies using them. 备注: PD-1(CD279) 抑制剂可用于治疗癌症、细菌、病毒和真菌感染。本发明的化合物在100 nM的CFSE中对PDL-1的抑制率为87%。 3. WO 2015032286 标题: Triazolopyridine compounds, compositions and methods of use thereof 申请人: 罗氏 优先权日期及相关专利公开号: 2013 US 874038 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 专利摘要: Compounds of Formula 0, Formula I and Formula II and methods of use as Janus kinase inhibitors are described herein. 备注: Jak抑制剂，尤其是Jak1和Jak2,可用于治疗哮喘。本发明的化合物对Jak1和Jak2的Ki分别为 0.00121和0.00056 mcM。 4. WO 2015035223 标题: Aryl ethers and uses thereof 申请人: Peloton Therapeutics, Inc. 优先权日期及相关专利公开号: 2014 US 978421 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: 肾癌 专利摘要: The present disclosure relates to HIF-2a inhibitors and methods of making and using them for treating cancer. Certain compounds were potent in HIF-2a scintillation proximity assay, luciferase assay, and VEGF ELISA assay, and led to tumor size reduction and regression in 786-O xenograft bearing mice in vivo. 备注: HIF-2alpha抑制剂可用于治疗肾癌。本发明的化合物对HIF-2alpha的IC50 = 0.008 mcM。 5. WO 2015034420 标题: HCV polymerase inhibitors 申请人: Medivir AB 优先权日期及相关专利公开号: 2013 SE 51169 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: The invention provides compounds of the formula I) wherein B is a nucleobase selected from the groups (a) to (d) and the other variables are as defined in the claims, which are of use in the treatment or prophylaxis of hepatitis C virus infection, and related aspects. 备注: NS5B抑制剂可用于治疗丙肝。本发明的化合物HCV的重组，其EC50 = 0.055 mcM。 6. WO 2015038446 标题: C5-spiro iminothiazine dioxides as BACE inhibitors, compositions, and their use 申请人: Merck & Co., Inc. 优先权日期及相关专利公开号: 2013 US 877440 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 专利摘要: In its many embodiments, the present invention provides certain C5-spiro iminothiadiazine dioxide compounds, including compounds Formula (I): or a tautomers and/or stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomers and said stereoisomers, wherein RL, X, Y, R1A, R1B, R2, R3, m, and RA are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer’s disease, are also disclosed. 备注: BACE1和BACE2抑制剂可用于治疗阿尔茨海默、唐氏综合症、帕金森氏症、中风、青光眼、2型糖尿病和克雅氏病等疾病。本发明的化合物对BACE1 和BACE2的Ki分别为3和1 nM。 7. WO 2015034213 标题: Protein kinase inhibitor containing pyrrolopyridazine derivative 申请人: CJ CheilJedang Corp. 优先权日期及相关专利公开号: 2013 KR 106063 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: 症、牛皮癣、风湿性关节炎、炎症性肠病和慢性阻塞性肺疾病(COPD) 专利摘要: The present invention relates to a pyrrolopyridazine derivative represented by chemical formula 1 of the detailed description, or a pharmaceutically acceptable salt thereof. According to the present invention, a compound and a pharmaceutically acceptable salt thereof inhibit the activity of a protein kinase, and thus are useful for preventing or treating diseases related thereto. 备注: c-Met抑制剂可用于治疗癌症、牛皮癣、风湿性关节炎、炎症性肠病和慢性阻塞性肺疾病(COPD)等疾病。本发明的化合物对c-Met的IC50 40 nM。 8. WO 2015035278 标题: RORgamma modulators 申请人: 百时美施贵宝 优先权日期及相关专利公开号: 2013 US 875220 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: 自身免疫性疾病、哮喘、过敏、代谢疾病、癌症 专利摘要: Described are ROR? modulators of the formula (I), or pharmaceutically acceptable salts thereof, wherein all substituents are defined herein. The invention includes stereoisomeric forms of the compounds of formula I, including stereoisomerically-pure, scalemic and racemic form, as well as tautomers thereof. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating ROR? activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of ROR? activity, for example, autoimmune and/or inflammatory disorders. 备注: 维甲酸RORgamma受体调控剂可用于治疗自身免疫性疾病、哮喘、过敏、代谢疾病和癌症。本发明的化合物对RORgamma受体的IC50 = 10.04 nM。 9. WO 2015035015 标题: Liver X receptor (LXR) modulators 申请人: Alexar Therapeutics, Inc. 优先权日期及相关专利公开号: 2013 US 873755 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、老年痴呆症、帕金森疾病、糖尿病、代谢综合征、动脉粥样硬化、感染、炎症、认知障碍 专利摘要: Described herein are liver X receptor (LXR) modulators and methods of utilizing LXR modulators in the treatment of LXR-associated diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds. 备注: LXRbeta配体可以用于治疗癌症、老年痴呆症、帕金森疾病、糖尿病、代谢综合征、动脉粥样硬化、感染、炎症和认知障碍等疾病。本发明的化合物对LXRbeta配体的EC50小于1 mcM。 10. WO 2015024878 标题: Novel neurokinin 1 receptor antagonist compounds II 申请人: Leo Pharma A/S 优先权日期及相关专利公开号: 2013 CN 81889 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: 皮炎 专利摘要: The invention relates novel NK1 receptor antagonists represented in formula A, wherein R1 and R2 independently are selected from the group consisting of (C1-4)alkyl, (C1-4)haloalkyl, (C1-4)alkoxy, CD3 or halogen; R3 is selected from the group consisting of hydrogen, (C1-4)alkyl, (C1-4)haloalkyl and (C1-4)hydroxyalkyl; R4 is selected from the group consisting of phenyl, 5-membered heteroaryl and 6-membered heteroaryl; R5 and R6 are independently selected from the group consisting of hydrogen, (C1-4)alkyl, (C1-4)hydroxyalkyl and (C1-4)haloalkyl and X and Y are independently selected from the group consisting of CH and N. The invention furthermore relates to intermediates for the preparation of said compounds, to their use in therapy, and to pharmaceutical compositions comprising said compounds. 备注: 速激肽NK1拮抗剂可治疗皮炎、湿疹、痒疹、皮肤萎缩等皮肤疾病。本发明的化合物对NK1受体的 IC50为0.02 nM。
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