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浮米每周专利快讯：2014年10月（二） 作者：浮米网 来源：浮米网 2014-10-09
1. WO 2014133134 标题: Novel tetrahydropyridopyrimidinone derivative 申请人: Ajinomoto Co., Inc. 优先权日期及相关专利公开号: 2013 JP 39540 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: 血脂障碍、肥胖 专利摘要: Provided is a novel compound having a higher MGAT2-inhibiting activity than those of conventional compounds. A compound represented by general formula (I) or a pharmaceutically acceptable salt thereof. 备注: MGAT2抑制剂可以治疗肥胖和血脂障碍。本发明的化合物可以抑制重组MGAT2的活性（IC50=0.64 nM）。
2. WO 2014134267 标题: Carbazole compounds useful as bromodomain inhibitors 申请人: 百时美施贵宝 优先权日期及相关专利公开号: 2013 US 770021 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 is directed to carbazole compounds, pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders. 备注: Brd4抑制剂可以治疗癌症。本发明的化合物可以抑制组蛋白多肽与Brd4的结合 (IC50 0.05 mcM)。
3. US 2014256700 标题: Carbazole compounds useful as bromodomain inhibitors 申请人: 百时美施贵宝 优先权日期及相关专利公开号: 2014 US 190477 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 is directed to carbazole compounds, pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders. 备注: Brd4抑制剂可以治疗癌症。本发明的化合物可以抑制biotinylated组蛋白多肽与Brd4的结合(IC50 50 nM)。
4. WO 2014128655 标题: Substituted imidazo[4,5-c]quinoline derivatives as bromodomain inhibitors 申请人: Aurigene Discovery Technologies Ltd. 优先权日期及相关专利公开号: 2013 IN 802 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: 自身免疫疾病、癌症、炎症 专利摘要: The present invention provides novel substituted imidazo[4,5-c]quinoline derivatives of formula (1), which may be therapeutically useful, more particularly as Bromodomain inhibitors; (1) in which Cyi, Cy2, R1, R2, R3, R4 and R5 have the same meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorder, in particular their use in diseases or disorder associated as bromodomain inhibitors. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted imidazo[4,5-C]quinoline compounds of formula (1) together with a pharmaceutically acceptable carrier, diluent or excipient therefor. 备注: BET蛋白抑制剂，尤其是Brd2、Brd3、Brd4可用于治疗癌症、炎症和自身免疫疾病。本发明的化合物可以抑制BET的活性（IC50200 nM）。
5. US 2014243287 标题: Pyrazole derivatives as sphingosine 1-phosphate (S1P) receptor modulators 申请人: Allergan, Inc. 优先权日期及相关专利公开号: 2014 US 187586 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、眼疾、免疫疾病、过敏症、自身免疫疾病、炎症、癌症 专利摘要: The present invention relates to pyrazole derivatives of formula (I), processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-l-phosphate receptors. 备注: S1P1受体配体可以治疗疼痛、眼疾、免疫疾病、过敏症、自身免疫疾病、炎症和癌症。本发明的化合物对S1P1受体的EC50=262 nM。
6. WO 2014133046 标题: Novel pyrazole derivative 申请人: Mochida Pharmaceutical Co., Ltd. 优先权日期及相关专利公开号: 2013 JP 38030 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: 精神疾病；双相障碍症；帕金森综合症；亨廷顿症；神经退行性疾病 专利摘要: There has been a demand for a pharmaceutical composition which is used for a prophylactic and/or therapeutic agent for various diseases associated with PDE10 (for example, mental disorder, neurodegenerative disorder and the like). The present invention provides: a compound having a PDE10 inhibitory effect, in particular, a compound which is represented by formula (I) and is characterized by having a 4-heteroarylpyrazole-5-carboxylic acid amide structure, a pharmaceutically acceptable salt thereof, and a solvate of the compound or the salt; a pharmaceutical composition which is characterized by containing, as an active ingredient, the compound, a pharmaceutically acceptable salt of the compound, or a solvate of the compound or the salt; and a pharmaceutical use of the compound, a pharmaceutically acceptable salt of the compound, or a solvate of the compound or the salt. 备注: PDE10选择性抑制剂可以治疗精神疾病（如精神分裂症、抑郁、焦虑）；双相障碍症；帕金森综合症；亨廷顿症；神经退行性疾病；注意力缺陷或认知障碍；肥胖；物质滥用与依赖。本发明的化合物对PDE10的IC50小于5 nM。
7. WO 2014129874 标题: Piper amide-based compound as bombesin receptor subtype 3 申请人: Seoul National University (SNU) 优先权日期及相关专利公开号: 2013 KR 20141 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 present invention relates to: a novel a,ß-unsaturated amide compound; a method for preparing a composition for preventing or treating obesity, comprising the steps of selecting a compound showing an obesity prevention or treatment effect from a compound library comprising one or more a,ß-unsaturated amide compounds, and preparing a composition for preventing or treating obesity containing the selected compound; and a composition for preventing or treating obesity, containing an a,ß-unsaturated amide compound. The a,ß-unsaturated amide compound of the present invention has a mother nucleus structure mimicking a piper amide, which is a natural substance showing various activities, and can show various pharmacological activities. In addition, a pure compound can be obtained without carrying out a purification process by column chromatography normally used since soluble by-products are generated using ß-phosphono-N-hydroxysuccinimidyl ester as an intermediate. Additionally, it is possible to screen a compound, which is a BRS-3 agonist, from a library of the compound synthesized thereby through a pharmacological activity test, and utilize the same in a composition for preventing or treating obesity. 备注: Bombesin BB3 (BRS-3)受体激动剂可以治疗肥胖。本发明的化合物可以激活CHO-K1细胞中表达的BRS-3受体。同时该化合物可以降低高脂饮食的C57BL/6J鼠的体重。
8. WO 2014133008 标题: Indole and azaindole derivatives each having AMPK-activating activity 申请人: Shionogi & Co., Ltd. 优先权日期及相关专利公开号: 2013 JP 151281 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: 糖尿病 专利摘要: Provided is a compound useful as an AMPK activator. The compound is a compound represented by the formula or a pharmaceutically acceptable salt thereof. In the formula, Y represents a substituted or unsubstituted alkyl group or the like; T represents -CR7= or -N=; U represents -CR8= or -N=; R2 represents a hydrogen atom or the like; R3 represents a halogen atom or the like; and R4, R7 and R8 independently represent a hydrogen atom or the like. 备注: AMPK激活剂可以治疗糖尿病。本发明的化合物可以激活AMPKalpha2-beta2-gamma1EC150 = 0.21 nM。
9. US 2014249120 标题: Neuroactive 13, 17-substituted steroids as modulators for gaba type-A receptors 申请人: 华盛顿大学 优先权日期及相关专利公开号: 2014 US 191740 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: 失眠症、焦虑、酒精戒断症候群、脆性X综合症、癫痫 专利摘要: The present disclosure is generally directed to neuroactive 13,17-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds. 备注: 类固醇可以作为GABA(A)受体调控剂，可作为麻醉用药，并治疗失眠症、焦虑、酒精戒断症候群、脆性X综合症、情绪疾病和癫痫。本发明的化合物XJ-99，可以抑制[35S]-TBPS与GABA(A) 受体的结合(IC50 = 43 nM)。
10. WO 2014128465 标题: 2-(Hetero)aryl-benzimidazole and imidazopyridine derivatives as inhibitors of asparagimeemethyltransferase 申请人: Cancer Therapeutics CRC Pty. Ltd. 优先权日期及相关专利公开号: 2013 GB 2927 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、血红蛋白病 专利摘要: Substituted benzimidazole and 3H-imidazo[4,5-b]pyridines or formula I: where X and Y respectively are selected from: (i) N and N; and (ii) N and CR4; A2 is selected from:, a C5 heteroarylene group, containing 2 or 3 ring heteroatoms, where the bonds to L1 and the core are ß to one another; L1 is selected from: (i)A1-O-CH2-A2; (ii)A1-CH2-O-A2; (iii)A1-C(=O)-NH-A2; (iv)A1-CH(OH)-A2; (v)A1-CH2-NH-C(=O)-A2; (vi) A1-S-CH2-A2; (vii)A1- CH2-S-A2; (viii)A1-CH2-A2; and (ix)A1-CH(CH3)-O-A2; A1 is phenyl, optionally substituted by F or CF3; their use as pharmaceuticals, and in particular, in treating cancer and hemoglobinopathies. 备注: Protein arginine N-methyltransferase 5 (PRMT5) 抑制剂可以治疗癌症和血红蛋白病。本发明的化合物可以抑制PRMT5活性(IC50 = 0.182 mcM)。
11. WO 2014130693 标题: Inhibitors of Bruton’s tyrosine kinase 申请人: Pharmacyclics, Inc. 优先权日期及相关专利公开号: 2013 US 769103 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: 自身免疫疾病、癌症 专利摘要: Disclosed herein are compounds that form covalent bonds with Bruton’s tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. 备注: Btk抑制剂可以治疗自身免疫疾病和癌症。本发明的化合物可以抑制BTK的活性，其IC50 100 nM。
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