本周共有13篇专利，1、:勃林格殷格翰的的BRD4抑制剂，可以治疗多种癌症。本发明的化合物可以抑制BRD4-BD1和四乙酰化组蛋白H4相互作用，IC50=1 nM. 2、 杨森的备注: TLR7/TLR8受体激动剂可以治疗病毒感染，免疫疾病和炎症。本发明的化合物可以激活TLR7受体，其最低有效浓度（LEC）为0.047mcM,对TLR8受体具有选择性（LEC=1.94mcM）等1. WO 2014076237标题: Triazolopyrazine
申请人: 勃林格殷格翰
优先权日期及相关专利公开号: 2012 EP 192987
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 encompasses compounds of general formula (I) wherein the groups R1 to R 3 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.
备注: BRD4抑制剂可以治疗多种癌症。本发明的化合物可以抑制BRD4-BD1和四乙酰化组蛋白H4相互作用，IC50=1 nM.
2. WO 2014076221标题: Heterocyclic substituted 2-amino-quinazoline derivatives for the treatment of viral infections
申请人: 杨森
优先权日期及相关专利公开号: 2012 EP 192970
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: 病毒感染，免疫疾病和炎症
专利摘要: This invention relates to heterocyclic substituted 2-amino-quinazoline derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.
备注: TLR7/TLR8受体激动剂可以治疗病毒感染，免疫疾病和炎症。本发明的化合物可以激活TLR7受体，其最低有效浓度（LEC）为0.047mcM,对TLR8受体具有选择性（LEC=1.94mcM）.
3. WO 2014075754标题: 3-Aminocyclopentane carboxamide derivatives
申请人: Merck Patent GmbH
优先权日期及相关专利公开号: 2012 EP 7759
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，多发性硬化症，炎症，脑损伤，心血管疾病
专利摘要: Compounds of the formula (I) in which R1, R4, R, X1, X2, X3, X4, q and W have the meanings indicated in Claim 1, are inhibitors of fatty acid synthase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.
备注: 脂肪酸合成酶（FAS）抑制剂可以治疗癌症，多发性硬化症，炎症，脑损伤，心血管疾病（包括动脉粥样硬化，术后再狭窄，心肌梗死和痛风）等疾病。本发明中的化合物对FAS酶的I50小于0.3mcM.
4. WO 2014075318标题: Pyrimidine compounds and use thereof
申请人: 先声制药
优先权日期及相关专利公开号: 2012 CN 84846
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: 慢性髓性白血病，过敏症，哮喘，自身免疫疾病
专利摘要: Disclosed in the present invention are compounds of general formula (I) and pharmaceutically acceptable equivalents or salts thereof, and the use of the compounds as a Janus kinase inhibitor for application in a variety of medicinal uses.
备注: JAK抑制剂可以用于治疗红细胞增多，骨髓纤维化（如慢性特发性骨髓纤维化），慢性髓性白血病，过敏症，哮喘，自身免疫疾病等疾病。本发明中的化合物对JAK2和JAK3的IC50小于500 nM.
5. WO 2014078214标题: Azetidine benzimidazoles as PDE10 inhibitors
申请人: 默克
优先权日期及相关专利公开号: 2012 US 726645
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: 情绪疾病，认知和神经退行性疾病，亨廷顿症，精神错乱
专利摘要: The present invention is directed to substituted azetidine benzimidazole compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington’s disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
备注: PDE10A抑制剂可以治疗情绪疾病，认知和神经退行性疾病，亨廷顿症，精神错乱（包括妄想症，精神错乱）等疾病。本发明的化合物可以抑制PDE10A,其IC50达到0.11 nM.
6. WO 2014074670标题: Alkyl amide-substituted pyrimidine compounds useful in the modulation of IL-12, IL-23 and/or IFNalpha
申请人: 百时美施贵宝
优先权日期及相关专利公开号: 2012 US 723827
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: 自身免疫疾病和炎症
专利摘要: Compounds having the following formula (I): or a stereoisomer or pharmaceutically-acceptable salt thereof, where R1, R2, R3, R4, and R5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNa by acting on Tyk-2 to cause signal transduction inhibition.
备注: Tyk2抑制剂可以治疗自身免疫疾病和炎症。本发明的化合物对Tyk2的EC50=0.03 mcM.
7. WO 2014074661标题: Amide-substituted heterocyclic compounds useful as modulators of IL-12, IL-23 and/or IFNalpha responses
申请人: 百时美施贵宝
优先权日期及相关专利公开号: 2012 US 723840
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: 自身免疫疾病和炎症
专利摘要: Compounds having the following formula I: or a stereoisomer or pharmaceutically-acceptable salt thereof, where R1, R2, R3, R4, and R5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNa, by acting on Tyk-2 to cause signal transduction inhibition.
备注: Tyk2抑制剂可以治疗自身免疫疾病和炎症。本发明的化合物在IL-23细胞和Kit 225 T细胞中对Tyk2的EC50=1.52 和1.63 nM。
8. WO 2014074660标题: Alkyl-amide-substituted pyridyl compounds useful as modulators of IL-12, IL-23 and/or IFNalpha responses
申请人: 百时美施贵宝
优先权日期及相关专利公开号: 2012 US 723854
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: 自身免疫疾病和炎症
专利摘要: Compounds having the following formula (I): or a stereoisomer or pharmaceutically-acceptable salt thereof, where R1, R2, R3, R4, and R5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNa, by acting on Tyk-2 to cause signal transduction inhibition.
备注: Tyk2抑制剂可以治疗自身免疫疾病和炎症。本发明的化合物对Tyk2的EC50=0.0035 mcM.
9. WO 2014074657标题: Bicyclic heterocycle substituted pyridyl compounds useful as kinase modulators
申请人: 百时美施贵宝
优先权日期及相关专利公开号: 2012 US 723851
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:
专利摘要: Compounds having the following formula (I) or a stereoisomer or a pharmaceutically-acceptable salt thereof, wherein R2 is a bicyclic heterocycle, and R1, R3, R4, R5 and R6 are as defined herein, that are useful as kinase modulators, including IRAK-4 modulation.
备注: IRAK-4抑制剂可以用于治疗炎症和自身免疫疾病（如溃疡性结肠炎，哮喘，移植排异，牛皮癣，类风湿症）。本发明的化合物对IRAK-4的IC50=0.0018 mcM.
10. WO 2014072325标题: [3-Heteroaryl-2-trifluoromethyl-propyl]-piperidin-1-yle or -morpholin-4-yle compounds as TRPA1 antagonists for the treatment of respiratory diseases
申请人: 罗氏
优先权日期及相关专利公开号: 2012 US 723932
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，慢性阻塞性肺疾病，鼻炎和支气管痉挛
专利摘要: The invention is concerned with the compounds of formula (I) and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and using the compounds of formula (I) as well as pharmaceutical compositions containing such compounds. The compounds of formula (I) are antagonists of the TRPA1 channel and may be useful in treating inflammatory diseases and disorders associated with that channel.
备注: TRPA1拮抗剂可以治疗哮喘，慢性阻塞性肺疾病，鼻炎和支气管痉挛。本发明的化合物可以抑制TRPA1（IC50=0.0621 mcM）.
11. WO 2014074761标题: Novel compounds as diacylglycerol acyltransferase inhibitors
申请人: 葛兰素史克
优先权日期及相关专利公开号: 2012 IN 3480
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: This invention relates to novel compounds which are inhibitors of acyl coenzyme A: diacylglycerol acyltransferase 1 (DGAT-1), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination with weight management therapies or other triglyceride lowering therapy for the prevention or treatment of diseases related to DGAT-1 dysfunction or where modulation of DGAT-1 activity may have therapeutic benefit including but not limited to obesity, obesity related disorders, genetic (Type 1, Type 5 hyperlipidemia) and acquired forms of hypertriglyceridemia or hyperlipoproteinemia- related disorders, caused by but not limited to lipodystrophy, hypothyroidism, medications (beta blockers, thiazides, estrogen, glucocorticoids, transplant) and other factors (pregnancy, alcohol intake), hyperlipoproteinemia, chylomicronemia, dyslipidemia, non-alcoholic steatohepatitis, diabetes, insulin resistance, metabolic syndrome, cardiovascular outcomes, angina, excess hair growth (including syndromes associated with hirsutism), nephrotic syndrome, fibrosis such as mycocardial, renal and liver fibrosis, hepatitis C virus infection and acne or other skin disorders.
备注: DGAT-1抑制剂可以治疗肥胖症。本发明的化合物对DGAT-1的IC50小于100 nM.
12. WO 2014074421标题: Prodrug bipyridylaminopyridines as Syk inhibitors
申请人: 默克
优先权日期及相关专利公开号: 2012 US 723571
相关候选药物类型: 前药
相关候选药物化学结构:
适应症: 哮喘，系统红斑狼疮和类风湿病
专利摘要: The present invention provides compounds of Formula (I), which are prodrugs of trans-4-[(1R)-(6-{[4-(difluoromethyl)pyridin-2-yl]amino}-4-methyl-2,3′-bipyridin-6′-yl)-1-hydroxyethyl]cyclohexanecarboxylic acid, a potent inhibitor of Syk. The compounds are useful in the treatment and prevention of diseases mediated by the enzyme, such as asthma, COPD, rheumatoid arthritis and cancer.
备注: SYK抑制剂可以治疗哮喘，系统红斑狼疮和类风湿病。本发明的化合物对SYK的IC500.5 nM。
13. WO 2014074365标题: Novel benzyl sulfonamide compounds useful as MoGAT-2 inhibitors
申请人: 礼来
优先权日期及相关专利公开号: 2013 US 748935
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: 高甘油三酯血症
专利摘要: The present invention provides compounds of Formula I. Wherein Rl, L, and A are as described herein, or a pharmaceutical salt thereof, processes for preparing the compounds, and methods of treating a condition, such as hypertriglyceridemia, using the compounds.
备注: MGAT2抑制剂可以治疗高甘油三酯血症。本发明的化合物可以抑制MGAT-2，其IC50小于100 nM.
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