1. WO 2014121883标题: Substituted acetylene derivatives and their use as positive allosteric modulators of mGluR4
申请人: 默克
优先权日期及相关专利公开号: 2013 US 762000
相关候选药物类型: 小分子药物
适应症: 精神疾病、2型糖尿病、胃食管反流病、肠炎、黄斑变性、药物滥用和依赖
专利摘要: The present invention relates to novel acetylene derivatives as positive allosteric modulators for modulating metabotropic glutamate receptor subtype 4 (mGluR4) and/or altering glutamate level or glutamatergic signalling.
备注: mGluR4受体正向变构调控剂可以治疗精神疾病（如注意力缺陷、多动症、焦虑和情绪异常）、神经退行性疾病（如帕金森症）、2型糖尿病、胃食管反流病、肠炎、黄斑变性、药物滥用和依赖。本发明的的化合物对mGluR4受体的EC50 1 mcM。
2. WO 2014117920标题: Spiro-quinazolinone derivatives useful for the treatment of neurological diseases and conditions
申请人: 默克
优先权日期及相关专利公开号: 2013 US 760367
相关候选药物类型: 小分子药物
适应症: 精神疾病、2型糖尿病、胃食管反流病、肠炎、黄斑变性、药物滥用和依赖
专利摘要: The present invention relates to novel spiro-quinazolinone derivatives as positive allosteric modulators for modulating metabotropic glutamate receptor subtype 4 (mGluR4) and/or altering glutamate level or glutamatergic signalling
备注: mGluR4受体正向变构调控剂可以治疗精神疾病（如注意力缺陷、多动症、焦虑和情绪异常）、神经退行性疾病（如帕金森症）、2型糖尿病、胃食管反流病、肠炎、黄斑变性、药物滥用和依赖。本发明的的化合物对mGluR4受体的EC50 1 mcM。
3. WO 2014120346标题: Factor IXa inhibitors
申请人: 默克
优先权日期及相关专利公开号: 2012 US 739266
相关候选药物类型: 小分子药物
适应症: 血栓
专利摘要: The present invention provides a compound of Formula (I) (structurally represented) wherein R1 is H or C1-6 alkyl, R2 is H or C1-6 alkyl or CH20H, R3 is H or C1-6 alkyl, and R4 is H or C1-6 alkyl, provided that when R1, R2, and R3 are H, R4 is C1-6 alkyl, and when R1, R2, and R4 are H, then R3 is C1-6 alkyl, and when R1, R3, and R4 are H, R2 is C1-6 alkyl or-CH20H, and when R2, R3, and R4 are H, then R1 is C 1-6 alkyl; A is 1 ) a 9-10 membered bicyclic heterocycle having 1-3 heteroatoms independently selected from N, S and 0, which 9-10 membered bicyclic heterocycle is unsubstituted or substituted with R5 and unsubstituted or substituted with R6 and unsubstituted or substituted with NH2, or 2) a 6-9 membered monocyclic or bicyclic carbocyclic ring system unsubstituted or substituted with R5, unsubstituted or substituted with R6, and unsubstituted or substituted with -CH2NH2; and B is 1) a 5- or 6-membered monocyclic heterocycle having 1 or 2 heteroatoms independently selected from N, S or 0, which is unsubstituted or substituted on a carbon or nitrogen atom with R7, unsubstituted or substituted on a carbon or nitrogen atom with R8, and unsubstituted or substituted on a carbon or nitrogen atom with R9, or 2) an 8- or 9-membered fused bicyclic heterocycle having 1, 2 or 3 nitrogen atoms which is unsubstituted or substituted on a carbon or nitrogen atom with R7, and unsubstituted or substituted on a carbon or nitrogen atom with R8; and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses.
备注: 凝血因子IXa抑制剂可以治疗血栓。本发明的化合物可以抑制凝血因子Ixa的活性，其IC50为1.345 nM.。
4. WO 2014121062标题: Selective HDAC3 inhibitors
申请人: Acetylon Pharmaceuticals, Inc.
优先权日期及相关专利公开号: 2014 US 923023
相关候选药物类型: 小分子药物
适应症: 癌症、2型糖尿病、神经退行性疾病、镰状细胞贫血、地中海贫血症
专利摘要: Provided herein are HDAC3 inhibitors, as well as methods of treatment comprising administering these compounds to a subject in need thereof.
备注: HDAC3抑制剂可以治疗癌症、2型糖尿病、神经退行性疾病、镰状细胞贫血、地中海贫血症。本发明的化合物可以抑制HDAC3 (IC50 = 30 nM)，且对HDAC1 和HDAC2 具有选择性(IC50 分别等于462 和228 nM)。
5. WO 2014117947标题: 4-Amino substituted condensed pyrimidine compounds as PDE4 inhibitors
申请人: Gruenenthal GmbH
优先权日期及相关专利公开号: 2013 EP 565
相关候选药物类型: 小分子药物
适应症: 哮喘、过敏性鼻炎、类风湿性关节炎、银屑病、肠炎、慢性阻塞性肺病、癌症
专利摘要: The invention relates to novel substituted condensed pyrimidine compounds of general formula (I) in which the chemical groupings, substituents and indices are as defined in the description, and to their use as medicaments, in particular as medicaments for the treatment of conditions and diseases that can be treated by inhibition of the PDE4 enzyme.
备注: PDE4B抑制剂可以治疗哮喘、过敏性鼻炎、类风湿性关节炎、银屑病、肠炎、慢性阻塞性肺病、癌症、痛风、葡萄膜炎、阿尔兹海默等多种疾病。本发明的化合物可以抑制PDE4B1活性(IC50 = 0.07 mcM) ，且对PDE4D2具有50倍的选择性。
6. WO 2014117948标题: Novel substituted condensed pyrimidine compounds
申请人: Gruenenthal GmbH
优先权日期及相关专利公开号: 2013 EP 550
相关候选药物类型: 小分子药物
适应症: 哮喘、过敏性鼻炎、类风湿性关节炎、银屑病、肠炎、慢性阻塞性肺病、癌症
专利摘要: The invention relates to novel substituted condensed pyrimidine compounds of general formula (I) in which the chemical groupings, substituents and indices are as defined in the description, and to their use as medicaments, in particular as medicaments for the treatment of conditions and diseases that can be treated by inhibition of the PDE4 enzyme.
备注: PDE4B抑制剂可以治疗哮喘、过敏性鼻炎、类风湿性关节炎、银屑病、肠炎、慢性阻塞性肺病、癌症、痛风、葡萄膜炎、阿尔兹海默等多种疾病。本发明的化合物可以抑制PDE4B1活性IC500.1 mcM 。
7. WO 2014117676标题: N- and S-containing heterocyclic compound having DHODH inhibiting activity and preparation and use thereof
申请人: East China University of Science and Technology (ECUST)
优先权日期及相关专利公开号: 2013 CN 10039793
相关候选药物类型: 小分子药物
适应症: 癌症、自身免疫类疾病、类风湿性关节炎、红斑狼疮
专利摘要: The present invention relates to an N- and S-containing heterocyclic compound having DHODH inhibiting activity and a preparation and use thereof. In particular, disclosed in the present invention are a compound of general formula (I), or an optical isomer, a cis-trans isomer or a pharmaceutically acceptable salt thereof, and the preparation method thereof. This compound has excellent dihydroorotate dehydrogenase inhibiting activity, thereby being used for treating or preventing diseases such as inflammatory diseases, for example, autoimmune diseases, rheumatoid arthritis and lupus erythematosus, destructive bone disorders, malignant nephrosclerosis disease, vascular diseases and infectious diseases.
备注: DHODH抑制剂可以治疗癌症、自身免疫类疾病、类风湿性关节炎、红斑狼疮等疾病。本发明的化合物可以抑制DHODH 的活性(IC50 = 0.12 mcM)。
8. WO 2014117718标题: Substituted 2-aminopyridine protein kinase inhibitor
申请人: Centaurus BioPharma Co., Ltd.
优先权日期及相关专利公开号: 2013 CN 10051822
相关候选药物类型: 小分子药物
适应症: 癌症
专利摘要: Disclosed are a 2-aminopyridine derivative having protein kinase inhibition activity, preparation method and pharmaceutical composition thereof. Also disclosed are uses of the compound and the pharmaceutical composition thereof in the preparation of drugs for treating and/or preventing protein kinase-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活性（IC50=1.96 nM），对ALK突变的L1196M和G1269S的IC50分别为35.1和61.3nM。
9. WO 2014118229标题: Substituted thienopyrimidines and pharmaceutical use thereof
申请人: 拜耳
优先权日期及相关专利公开号: 2013 EP 153619
相关候选药物类型: 小分子药物
适应症: 癌症
专利摘要: The present invention relates to substituted thienopyrimidine compounds of general formula(I)as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
备注: MNK1抑制剂可以治疗癌症。本发明的化合物可以抑制MNK1 (IC50 = 1.4 nM)。
10. WO 2014118135标题: Amidoimidazopyridazines as MKNK-1 kinase inhibitors
申请人: 拜耳
优先权日期及相关专利公开号: 2013 EP 153340
相关候选药物类型: 小分子药物
适应症: 癌症
专利摘要: The present invention relates to amido-substituted imidazopyridazine compounds of general formula (I) : in which A, R1, R2, R3, R4 and n are as defined in the claims, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper- proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
备注: MNK1抑制剂可以治疗癌症。本发明的化合物可以抑制MNK1 (IC50 = 3 ~ 11 nM 。
11. WO 2014119947标题: Biaryl- or heterocyclic biaryl-substituted cyclohexene derivative compounds as CETP inhibitors
申请人: Chong Kun Dang Holdings Corp.
优先权日期及相关专利公开号: 2013 KR 11206
相关候选药物类型: 小分子药物
适应症: 血脂异常、心绞痛、心肌梗塞、动脉硬化
专利摘要: The present invention provides biaryl- or heterocyclic biaryl-substituted cyclohexene derivative compounds, isomers thereof, or pharmaceutically acceptable salts. The compounds of the invention show a CETP inhibitory effect that increases HDL-cholesterol levels and reduces LDL-cholesterol levels. Pharmaceutical compositions comprising the compounds are useful for the prevention or treatment of dyslipidemia or dyslipidemia-related diseases.
备注: CETP抑制剂可以增加高密度脂蛋白水平，且降低低密度脂蛋白水平，因此可以治疗血脂异常及血脂异常相关疾病，如心绞痛、心肌梗塞、动脉硬化。本发明的化合物可以抑制[3H]-cholesteryl oleate至LDL（IC50=5.4 nM）。
12. WO 2014120764标题: S1P modulating agents
申请人: 百健艾迪
优先权日期及相关专利公开号: 2013 US 865846
相关候选药物类型: 小分子药物
适应症: 多发性硬化症、疼痛、类风湿性关节炎
专利摘要: Compounds of formula (I) can modulate the activity of one or more S 1P receptors. Sphingosine 1-phosphate (S IP) is a lysophospholipid mediator that evokes a variety of cellular responses by stimulation of five members of the endothelial cell differentiation gene (EDG) receptor family, namely S1P1, S1P2, S1P3, S1P4, and S1P5 (formerly EDG1, EDG5, EDG3, EDG6 and EDG8). The EDG receptors are G-protein coupled receptors (GPCRs) and on stimulation propagate second messenger signals via activation of heterotrimeric G-protein alpha (Ga.) subunits and beta-gamma (G()y) dimers.
备注: S1P5受体调控及可以治疗多发性硬化症、疼痛、类风湿性关节炎和脱髓鞘疾病、神经退行性疾病、认知障碍本发明的化合物可以拮抗S1P5受体活性(EC50 100 nM)。
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