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标题: 浮米每周专利快讯：2014年10月（一） [打印本页]
作者: 朵朵7 时间: 2014-10-1 07:39 PM
标题: 浮米每周专利快讯：2014年10月（一）
浮米每周专利快讯：2014年10月（一） 作者：浮米网 来源：浮米网 2014-10-01
1. WO 2014123457
标题: Alkyl [2-(2-[5-[4-(4-[2-[1-(2-methoxycarbonylamino-acetyl)-pyrrolidine-2-yl]-3H-imidazole-4-yl]-phenyl)-buta-1,3-dienyl]-1H-imidazole-2-yl]-pyrrolidine-1-yl)-2-oxo-ethyl]carbamate, pharmaceutical composition, medicinal agent and method for treatment of viral diseases
申请人: Intellektual`NY Dialog OOO
优先权日期及相关专利公开号: 2013 RU 105164
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 present invention relates to NS5A inhibitors, to a novel pharmaceutical composition, to an antiviral medicinal agent, and to a method for the prevention and treatment of viral diseases, particularly those caused by the hepatitis C (HCV) and hepatitis GBV-C viruses. Proposed are alkyl [2-(2-{5-[4-(4-{2-[1-(2-methoxycarbonylamino-acetyl)-pyrrolidine-2-yl]-3H-imidazole-4-yl}-phenyl)-buta-1,3-dienyl]-1H-imidazole-2-yl}-pyrrolidine-1-yl)-2-oxo-ethyl]carbamate of general formula 1 and their naphthalene-1,5-disulfonates of general formula 1.1, where: R1, R2, R3 and R4 independently of one another are C1-C3 alkyl; R5 and R6 independently of one another are C1-C3 alkyloxymethyl, or R3 and R5 and R4 and R6 along with the carbon atoms with which they are linked, form, independently of one another, a tetrahydrofuran cycle, where: R1, R2, R3 and R4 independently of one another are C1-C3 alkyl; R5 and R6 independently of one another are C1-C3 alkyl or C1-C3 alkyloxymethyl, or R3 and R5 and R4 and R6, along with the carbon atoms with which they are linked, form, independently of one another, a tetrahydrofuran cycle.
备注: NS5A抑制剂可以治疗HCV感染。本发明的化合物可以抑制 HCV gT1b (IC50 1 nM)、gT2a (IC50 = 9.9 to 1 nM)和 gT1a (IC50 = 9.9 to 1 nM)。
2. WO 2014123894
标题: Macrocyclic compounds as HCV entry inhibitors
申请人: Bristol-Myers Squibb Co.
优先权日期及相关专利公开号: 2013 US 761868
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: Compounds of Formula I, including pharmaceutically acceptable salts thereof, are set forth, in addition to compositions and methods of using these compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
备注: NS5B抑制剂可以治疗丙肝。本发明的化合物可以抑制基因1a型HCV复制，IC50=0.796 nM。
3. WO 2014123892
标题: Macrocyclic molecules as HCV entry inhibitors
申请人: Bristol-Myers Squibb Co.
优先权日期及相关专利公开号: 2013 US 761861
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: Compounds of Formula I, including pharmaceutically acceptable salts thereof, are set forth, in addition to compositions and methods of using these compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
备注: NS5B抑制剂可以治疗HCV感染。本发明的化合物可以抑制HCV基因1a型复制。EC50=0.109 nM。
4. WO 2014121418
标题: Tetracyclic heterocycle compounds and methods of use thereof for the treatment of hepatitis C
申请人: Merck & Co., Inc.
优先权日期及相关专利公开号: 2013 CN 130
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 present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system. I
备注: NS5B抑制剂可以治疗丙肝。本发明的化合物可以抑制基因1a和基因1b 型HCV复制，IC50 分别为1.7和1.4 nM。
5. WO 2014121416
标题: Tetracyclic heterocycle compounds and methods of use thereof for the treatment of hepatitis C
申请人: Merck & Co., Inc.
优先权日期及相关专利公开号: 2013 CN 128
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 present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
备注: NS5B抑制剂可以治疗丙肝。本发明的化合物可以抑制基因1a和基因1b 型HCV复制，IC50 分别为0.9708 和1.806 nM。
6. WO 2014121417
标题: Tetracyclic heterocycle compounds and methods of use thereof for the treatment of hepatitis C
申请人: Merck & Co., Inc.
优先权日期及相关专利公开号: 2013 CN 129
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 present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system. I
备注: NS5B抑制剂可以治疗丙肝。本发明的化合物可以抑制基因1a和基因1b 型HCV复制，IC50 分别为0.9543 和2.223 nM。
7. WO 2014121654
标题: Tetrazocyclokinase inhibitor
申请人: Shandong Xuanzhu Pharmaceutical Technology Co., Ltd.
优先权日期及相关专利公开号: 2013 CN 10045982
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 medical technologies, in particular to a tetrazocyclokinase inhibitor as represented by general formula (I), stereoisomer thereof, or pharmaceutically acceptable salt, and ester or solvate thereof, wherein A1, A2, A3, A4, R1, R2, R3, R4, R5, R6, R7, M, X, Y, Q, and n are as defined in the specification. The present invention also relates to a method for preparing the compounds, and uses of a pharmaceutical formulation and pharmaceutical composition containing the compounds, and the compounds or stereoisomers thereof, or pharmaceutically acceptable salt, ester or solvate thereof in the preparation of drugs for treating and/or preventing ALK-mediated cancer-related diseases.
备注: ALK抑制剂可以治疗癌症。本发明的化合物可以抑制ALK，IC50值为对照组的1.5。
8. WO 2014124418
标题: Modulators of methyl modifying enzymes, compositions and uses thereof
申请人: Constellation Pharmaceuticals, Inc.
优先权日期及相关专利公开号: 2013 US 25639
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: Agents having the structural Formula (II) for modulating histone methyl modifying enzymes, compositions and uses thereof for instance as anti-cancer agents are provided herein.
备注: EZH2抑制剂可以治疗癌症。本发明的化合物可以抑制EZH2和Y641N EZH2突变，IC50均小于100 nM。
9. EP 2765128
标题: Substituted benzamides with activity towards EP4 receptors
申请人: DraconisPharma SL
优先权日期及相关专利公开号: 2013 US 770096
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: 疼痛
专利摘要: The present invention belongs to the field of EP4 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP4 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP4 receptor as well as to pharmaceutical compositions comprising them.
备注: 前列腺素EP4受体拮抗剂可用于治疗疼痛。本发明的化合物可以抑制[3H]-PGE2与EP4受体的结合，在10mcM时，抑制率大于75%。
10. WO 2014123167
标题: Tricyclic pyrrolopyridine compound, and JAK inhibitor
申请人: Nissan Chemical Industry, Ltd.
优先权日期及相关专利公开号: 2013 JP 66124
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: 类风湿性关节炎
专利摘要: The present invention addresses the problem of providing a novel tricyclic pyrrolopyridine compound which has a JAK inhibitory activity, and is particularly useful for preventing, treating and/or alleviating autoimmune diseases, inflammatory diseases, or allergic diseases. Provided is a novel tricyclic pyrrolopyridine compound represented by formula (I) (the substituents in the formula are defined in detail in the description, however R1 represents a C1-6 alkyl group, or the like, R2 represents a hydrogen atom, or the like, R3 represents a hydrogen atom, or the like, ring A represents a C3-11 cycloalkane, or the like, L1 represents a C1-6 alkylene group, or the like, and R4 represents NRaRb, or the like), a tautomer of said compound or a pharmaceutically acceptable salt thereof, or a solvate of the compound, the tautomer, or the pharmaceutically acceptable salt.
备注: JAK抑制剂可以治疗类风湿性关节炎。本发明的化合物可以抑制JAK1, 2, 3和Tyk2，IC50分别为0.0022, 0.016, 0.016和0.057mcM。
11. WO 2014122184
标题: Position-specific asymmetric deuterium enriched catecholamine derivatives and medicaments comprising said compounds
申请人: CDRD Berolina AB
优先权日期及相关专利公开号: 2013 US 760738
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: 帕金森症、多动腿综合征、多系统萎缩症、肌萎缩性脊髓侧索硬化症
专利摘要: Herein described are deuterated catecholamine derivatives of the general Formula (I) wherein R1 is deuterium, R2, and R3 are independently selected from hydrogen and deuterium and wherein at least one of R2 and R3 has a deuterium enrichment in the range from 0.02 mol% to 100 mol% deuterium, and wherein the deuterium enrichment of R2 and R3 is different from each other and that the difference between the deuterium enrichment of R2 and R3 is at least 5 percentage points, R4 is hydrogen, deuterium, C1 to C6-alkyl or C5 to C6-cycloalkyl, deuterated C1 to C6-alkyl or C5 to C6-cycloalkyl, or a group that is easily hydrolytically or enzymatically cleavable under physiological conditions, as well as their physiologically acceptable salts and their stereoisomers, enantiomeres or diastereomers in optically pure form. The compounds can easily be prepared by mixing deuterated and non-deuterated compounds in a predefined ratio. The compounds show anti-Parkinson effect at lower doses and show lower side effects.
备注: 氘代左旋多巴衍生物可以治疗帕金森症、多动腿综合征、多系统萎缩症、肌萎缩性脊髓侧索硬化症。本发明的化合物提高肌动能力和降低运动障碍。
作者: 静悄悄 时间: 2014-10-1 09:21 PM
楼主辛苦，谢谢分享，好资料
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