本周共有16篇专利。罗氏公开4篇药物专利；诺华公开1篇用于治疗肺结核的药物专利，1篇治疗多囊性肾病专利；拜耳公开2篇用于Brd4抑制剂专利；国内的恒瑞医药公开1篇PI3Kalpha抑制剂专利。1. WO 2014095774标题: BET-protein-inhibiting dihydropyridopyrazinones
申请人: 拜耳
优先权日期及相关专利公开号: 2013 EP 182252
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，病毒感染，神经退行性疾病，炎症，动脉粥样硬化和男性避孕
专利摘要: The invention concerns BET-protein-inhibiting, in particular BRD4-inhibiting, dihydropyridopyrazinones of general formula (I), in which A, X, R1, R2, R3, R4, R5, R6, R7 and n have the meanings given in the description, intermediates for producing the compounds according to the invention, pharmaceutical agents containing the compounds according to the invention, and their prophylactic and therapeutic use in hyperproliferative diseases, in particular tumour diseases. The invention further concerns the use of BET-protein-inhibitors in viral infections, neurodegenerative diseases, inflammatory illnesses, atherosclerotic diseases, and in male fertility control.
备注: Brd4抑制剂可以治疗增殖性疾病（包括癌症），病毒感染，神经退行性疾病，炎症，动脉粥样硬化和男性避孕等。本发明的化合物可以抑制Brd4和乙酰化组蛋白H4的结合（IC50 = 194 nM）,对AML细胞MOLM-13的IC50为51 nM。
2. WO 2014095775标题: BET-protein-inhibiting dihydroquinoxalinones
申请人: 拜耳
优先权日期及相关专利公开号: 2013 EP 187778
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，病毒感染，神经退行性疾病，炎症，动脉粥样硬化和男性避孕
专利摘要: The invention concerns BET-protein-inhibiting, in particular BRD4-inhibiting, dihydroquinoxalinones of general formula (I), in which A, X, R1, R2, R3, R4, R5, R6, R7 and n have the meanings given in the description, intermediates for producing the compounds according to the invention, pharmaceutical agents containing the compounds according to the invention, and their prophylactic and therapeutic use in hyperproliferative diseases, in particular tumour diseases. The invention further concerns the use of BET-protein-inhibitors in viral infections, neurodegenerative diseases, inflammatory illnesses, atherosclerotic diseases, and male fertility control.
备注: Brd4抑制剂可以治疗增殖性疾病（包括癌症），病毒感染，神经退行性疾病，炎症，动脉粥样硬化和男性避孕等。本发明的化合物可以抑制乙酰化组蛋白H4肽与Brd4 domain 1（IC50 = 156）和Brd4 domain 2的结合(IC50 =47 nM)。可以抑制MOLM-13（IC50 = 300 nM）,B16-F10（IC50 =179 nM）, MOLP-8（IC50 =98 Nm)。
3. WO 2014091446标题: Pyrimido[4,5-b]quinoline-4,5(3H,10H)-diones as nonsense mutation suppressors
申请人: 诺华
优先权日期及相关专利公开号: 2012 US 736748
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: 血友病A型、血友病B型、囊胞纤维化、黏多糖症、杜氏营养不良症、p53和APC缺失引起的癌症
专利摘要: The invention relates to compound of the formula (I); or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.
备注: 无义突变的抑制剂可以用于治疗血友病A型、血友病B型、囊胞纤维化、黏多糖症、杜氏营养不良症、p53和APC缺失引起的癌症等疾病。本发明的化合物可以抑制CFTR蛋白的络氨酸(Y122X)的无义突变(AC50 = 2.5 mcM，10 mcM时Amax = 67%)；也可以抑制b型血友病患者的凝血因子IX R29X突变(AC50 = 1.9 mcM，10 mcM时Amax = 167%)。可以抑制来自Hurler综合症患者的艾杜糖苷酶的Q70X和W402X无义突变(AC50 = 1.7和2.9 mcM; Amax = 438和300%)。
4. WO 2014093606标题: Pyridone derivatives and uses thereof in the treatment of tuberculosis
申请人: 诺华
优先权日期及相关专利公开号: 2012 US 736921
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: 肺结核
专利摘要: A compound of Formula (I) is provided that has been shown to be useful for treating a disease, disorder or syndrome that is mediated by the inhibition of mycolic acid biosynthesis through inhibition of M. tuberculosis EnoyI Acyl Carrier Protein Reductase enzyme (InhA): wherein R1, R2, R3, R4 and R5 are as defined herein.
备注: 吡啶酮衍生物可以通过抑制结核杆菌还原酶的活性，调节霉菌酸的生物合成，达到治疗肺结核的作用。本发明的化合物可以抑制结核杆菌H37Rv（MIC50 =0.02 mcM)。
5. US 2014171417标题: Tricyclic compounds for inhibiting the CFTR channel
申请人: 诺华
优先权日期及相关专利公开号: 2012 US 739335
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: 多囊性肾病、腹泻
专利摘要: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
备注: CFTR离子通道抑制剂可以治疗多囊性肾病和腹泻。本发明的化合物可以抑制CFTR离子通道的表达（IC50=0.05 mcM。
6. US 2014163110标题: Benzyl sulfonamide derivatives as RORc modulators
申请人: 罗氏
优先权日期及相关专利公开号: 2012 US 735364
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: 关节炎
专利摘要: Compounds of the formula Ia or Ib, or pharmaceutically acceptable salts thereof, wherein m, n, r, A, X1, X2, X3, X4, Y, Z, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
备注: 维甲酸RORgamma受体调控剂可以治疗关节炎。本发明的化合物可以抑制25-[3H]-hydroxycholesterol与维甲酸RORgamma 受体的结合（IC50=0.0111 mcM)。
7. US 2014163024标题: Benzyl sulfonamide derivatives as RORc modulators
申请人: 罗氏
优先权日期及相关专利公开号: 2012 US 735360
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: 关节炎
专利摘要: Compounds of the formula Ia or Ib, or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, A, X1, X2, X3, X4, Y, Z, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
备注: 维甲酸RORgamma受体调控剂可以治疗关节炎。本发明的化合物可以抑制25-[3H]-hydroxycholesterol与维甲酸RORgamma 受体的结合(IC50 = 0.006 mcM).
8. WO 2014090692标题: Novel bi-ring phenyl-pyridines/pyrazines for the treatment of cancer
申请人: 罗氏
优先权日期及相关专利公开号: 2012 CN 86275
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: 胃癌、结直肠癌
专利摘要: The invention provides novel compounds having the general formula: wherein R1, R2 and R3 are as described herein, compositions including the compounds and methods of using the compounds.
备注: CDK8/cyclin C复合物抑制剂可以治疗癌症，尤其是胃癌和结直肠癌。本发明的化合物可以抑制CDK8/cyclin C酶的活性 (IC50 = 0.0002 mcM)，同时对结直肠癌细胞 HCT 116, SW-837和胃癌细胞AGS癌细胞有抑制作用，IC50分别为0.037mcM, 0.091mcM和0.033 mcM。
9. WO 2014090715标题: Thiazole derivatives as inhibitors of Bruton’s tyrosine kinase
申请人: 罗氏
优先权日期及相关专利公开号: 2012 US 736631
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、炎症
专利摘要: This application discloses compounds according to generic Formula I: wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.
备注: BTK抑制剂可以治疗自身免疫和炎症等疾病。本发明的化合物对BTK的IC50值为0.2543 mcM。
10. WO 2014093230标题: Compositions and methods for the production of pyrimidine and pyridine compounds with BTK inhibitory activity
申请人: 默克
优先权日期及相关专利公开号: 2012 US 735186
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、类风湿性关节炎和系统红斑狼疮
专利摘要: The present invention provides novel pyrimidine and pyridine compounds which are attached to a warhead, and the manufacture and use for the treatment of hyperproliferative diseases including, but not limited to, cancer, lupus, allergic disorders, Sjogren’s disease and rheumatoid arthritis. The invention also describes kinase inhibitors including, but not limited to, inhibitors of Bruton’s tyrosine kinase.
备注: BTK抑制剂可以治疗癌症、类风湿性关节炎和系统红斑狼疮等疾病。本发明的化合物对BTK的IC50小于100 nM。
11. WO 2014093190标题: BACE inhibitors of iminothiadiazine dioxides
申请人: 默克
优先权日期及相关专利公开号: 2012 US 737209
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 C2-ring-substituted iminothiadiazine compounds, or a tautomers thereof, and pharmaceutically acceptable salts of said compounds and said tautomers. The novel compounds of the invention are 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: BACE抑制剂可以治疗阿尔兹海默疾病。本发明的化合物对BACE1 和BACE2的Ki值分别为3nM和4 nM。
12. WO 2014092100标题: Heterocyclic compound
申请人: 武田
优先权日期及相关专利公开号: 2013 JP 210439、2012 JP 270445
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: 痴呆、阿尔兹海默、帕金森症、亨廷顿症
专利摘要: The purpose of the invention is to provide a compound or salt thereof that is useful as an agent for the prevention or treatment of epilepsy, neurodegenerative disease, and the like. The invention pertains to compounds represented by formula (I) (in the formula, each symbol is as defined in the specification) or salts thereof.
备注: CH24H抑制剂可以治疗癫痫、神经退行性疾病（如帕金森、阿尔兹海默、和亨廷顿症）。本发明的化合物可以抑制CH24H（1 mcM时抑制率达到97%）。
13. WO 2014089904标题: Triazinone compounds
申请人: 艾伯维
优先权日期及相关专利公开号: 2012 CN 86292
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、骨关节炎，哮喘，慢性阻塞性肺病，银屑病，肠炎，系统红斑狼疮、移植排异、糖尿病
专利摘要: The invention provides a compound of Formula (I), pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
备注: 蛋白激酶C抑制剂可以治疗自身免疫疾病（如类风湿性关节炎，骨关节炎，哮喘，慢性阻塞性肺病，银屑病，肠炎，系统红斑狼疮），移植排异和糖尿病。本发明的化合物可以抑制PKC alpha 和PKC thetaIC50、EC50均小于0.25 mcM
14. WO 2014090731标题: New positive allosteric modulators of nicotinic acetylcholine receptor
申请人: 灵北
优先权日期及相关专利公开号: 2012 US 735077
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: 注意力缺陷、多动症、糖尿病、疼痛、阿尔兹海默、精神错乱、脑损伤、炎症
专利摘要: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine a7 receptor.
备注: 烟碱alpha7阳性变构调控剂可以治疗注意力缺陷、多动症、糖尿病、疼痛、阿尔兹海默、精神错乱、脑损伤、炎症等。 本发明的化合物可以抑制烟碱alpha7受体(EC50 = 33 nM)。
15. WO 2014090147标题: Pyrimidine derivatives and salts thereof, preparation method and pharmaceutical use thereof
申请人: 恒瑞
优先权日期及相关专利公开号: 2012 CN 10544453
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 pyrimidine derivatives and salts thereof, preparation method and pharmaceutical use thereof. Specifically, the present invention relates to pyrimidine derivatives of general formula(I), pharmaceutically acceptable salts thereof, and the preparation methods thereof, as well as their use as a cancer therapeutic agent, especially their use as a P13K kinase inhibitor, wherein each substitute of general formula(I) is defined as the specification.
备注: PI3Kalpha抑制剂可以治疗癌症。本发明的化合物可以抑制PI3Kalpha (IC50 = 20 nM)，且对PI3Kbeta, PI3Kdelta, PI3Kgamma和mTOR具有选择性 (IC50分别为 1381nM, 963nM, 164nM和4008 nM)。
16. WO 2014096212标题: Novel tricyclic 3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-dione derivatives as gamma secretase modulators
申请人: 杨森
优先权日期及相关专利公开号: 2012 EP 198403
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: The present invention is concerned with novel tricyclic 3,4-dihydro-2H-pyrido[l,2-a]pyrazine-l,6-dione derivatives of Formula (I) wherein R1, R2, R3, R4, L, Y, Z and X have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament for the treatment of i.a. Alzheimer’s disease.
备注: gamma-Secretase调控剂可以抑制Abeta的产生，可用于治疗阿尔兹海默，脑外伤，认知功能障碍，痴呆，唐氏综合症等疾病。 本发明的化合物可以通过降低Abeta42（(IC50 = 0.05 mcM）和Abetatotal肽（IC50=10 mcM）。
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