马上注册，结交更多好友，享用更多功能，让你轻松玩转社区
您需要 登录 才可以下载或查看，没有帐号？立即注册 
x
行业 作者：浮米网 来源：浮米网 2015-06-08 0评论
1. WO 2015071393 标题: Tetrahydro-benzodiazepinones 申请人: 罗氏 优先权日期及相关专利公开号: 2013 US 905448 相关候选药物类型: 药物 相关候选药物化学结构: 适应症: 癌症 专利摘要: Disclosed are compounds of Formula I, or pharmaceutically acceptable salts thereof, wherein W, X, Y, Z, R1, R2, R3, R4 and R5 are as described in this application, and methods of using said compounds in the treatment of cancer. 备注: XIAP抑制剂对治疗癌症有效。示例化合物对XIAP的BIR2和BIR3结合域的抑制活性在TR-FRET实验中分别为：IC50 0.001 和 3.479 mcM
2. WO 2015071780 标题: Alkylidine substituted heterocyclyl derivatives as anti-bacterial agents 申请人: Aurigene Discovery Technologies Ltd. & UM Pharmauji Sdn. Bhd. 优先权日期及相关专利公开号: 2013 IN 5133 相关候选药物类型: 药物 相关候选药物化学结构: 适应症: 细菌感染 专利摘要: The present invention relates to alkylidine substituted heterocyclyl derivatives of formula (1) which may be therapeutically useful as as anti-bacterial agents, more particulalrly FabI inhibitors; I in which P, Q, Ri, R2, R3 and “n” have the same meanings given in the specification, and pharmaceutically acceptable salts or pharmaceutically acceptable stereoisomers thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage in inhibiting Enoyl-ACP reductase enzyme (FABI) activity. The present invention also provides methods for synthesizing and administering the FabI inhibitory compounds. The present invention also provides pharmaceutical formulations comprising at least one of the FabI inhibitory compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor. 备注: 烯酰-酰基载体蛋白还原酶Fab1抑制剂对治疗细菌感染有效。示例化合物对金黄色葡萄球菌Fab1的酶活性抑制为IC50 = 0.3 mcM；对甲氧西林敏感金黄色葡萄球菌（MSSA）、甲氧西林耐药的金黄色葡萄球菌（MRSA）以及甲氧西林耐药的表皮葡萄球菌的最低抑菌浓度为0.12 mcg/ml。
3. WO 2015073547 标题: Disubstituted phenoxy azetidine derivatives as sphingosine-1-phosphate (S1P) receptor modulators 申请人: Allergan 优先权日期及相关专利公开号: 2013 US 903630 相关候选药物类型: 药物 相关候选药物化学结构: 适应症: 过敏、自身免疫疾病、癌症、眼部疾病、免疫抑制、炎症、皮肤损害、疼痛 专利摘要: The present invention relates to disubstituted phenoxy azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. 备注: S1P1受体的配体可用于治疗过敏、自身免疫疾病、癌症、眼部疾病、免疫抑制、炎症、皮肤损害、疼痛等。示例化合物对人S1P1受体的EC50为2.77 nM。
4. WO 2015073344 标题: Compounds inhibiting leucine-rich repeat kinase enzyme activity 申请人: 默克 优先权日期及相关专利公开号: 2013 US 904260 相关候选药物类型: 药物 相关候选药物化学结构: 适应症: 帕金森综合症 专利摘要: The present invention is directed to substituted indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson’s Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved. 备注: 富亮氨酸重复受体激酶2(LRRK2)抑制剂可用于治疗帕金森综合症。示例化合物对人LRRK2的酶活性为IC50 = 8.2 nM。
5. WO 2015073763 标题: Substituted 4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazine derivatives as casein kinase 1 delta/epsilon 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 904116/2014 US 65594 相关候选药物类型: 药物 相关候选药物化学结构: 适应症: 癌症、昼夜节律紊乱、神经退行性变 专利摘要: The invention provides compounds of Formula (I): and pharmaceutically acceptable salts thereof. The compounds of Formula (I) inhibit protein kinase activity thereby making them useful as anticancer agents. 备注: 酪蛋白激酶-1抑制剂对治疗癌症、昼夜节律紊乱和神经退行性变有效。示例化合物对CK-1δ和CK-1ε的酶活性分别为IC50 0.0003和0.0001 mcM。
6. WO 2015071178 标题: Pyrido[4,3-b]pyrazine-2-carboxamides as neurogenic agents for the treatment of neurodegenerative disorders 申请人: 罗氏 优先权日期及相关专利公开号: 2013 EP 192406 相关候选药物类型: 药物 相关候选药物化学结构: 适应症: 焦虑、阿尔兹海默痴呆、抑郁、中风 专利摘要: The present invention relates to compounds of general formula (I), wherein R1 is hydrogen; R2 is hydrogen, lower alkyl, benzyl, lower alkyl substituted by hydroxy or is cycloalkyl optionally substituted by cyano; or R1 and R2 form together with the N-atom to which they are attached a heterocycloalkyl group, optionally containing an additional N, O or S ring atom, and which is optionally substituted by hydroxy; R3 is halogen, phenyl optionally substituted by one or more halogen, cyano, lower alkyl substituted by halogen, lower alkoxy substituted by halogen or by lower alkyl substituted by hydroxy, or is heteroaryl, optionally substituted by lower alkyl or halogen, or is 3,6-dihydro-pyran-4-yl, or is piperidin-1-yl optionally substituted by one or more halogen; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to it corresponding enantiomer and/or optical isomer thereof. The compounds of formula I may be used in the treatment of schizophrenia, obsessive-compulsive personality disorder, depression, bipolar disorders, anxiety disorders, normal aging, epilepsy, retinal degeneration, traumatic brain injury, spinal cord injury, post-traumatic stress disorder, panic disorder, Parkinson’s disease, dementia, Alzheimer’s disease, cognitive impairment, chemotherapy-induced cognitive dysfunction, Down syndrome, autism spectrum disorders, hearing loss, tinnitus, spinocerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, Huntington’s disease, stroke, radiation therapy, chronic stress, abuse of neuro-active drugs, selected from alcohol, opiates, methamphetamine, phencyclidine and cocaine. 备注: 可刺激神经再生的化合物对于治疗焦虑、阿尔兹海默痴呆、抑郁、中风等有效。示例化合物在荧光细胞活性检测实验中刺激神经干细胞增殖的活性为EC150 = 0.02 mcM。
7. CN 103570727/WO 2015070766 标题: N-Benzyl tryptanthrin derivative, and preparation method and application thereof 申请人: 复旦大学 优先权日期及相关专利公开号: 2013 CN 10560572 相关候选药物类型: 药物 相关候选药物化学结构: 适应症: 焦虑、自身免疫疾病、癌症、阿尔兹海默痴呆、抑郁 专利摘要: The present invention relates to an N-benzyl tryptanthrin derivative, and preparation method and use thereof. The N-benzyl tryptanthrin derivative of the present invention is characterized in that the derivative has a structural general formula as represented by formula 1, wherein each group is defined as in the specification. The preparation method of the compound is simple, has mild conditions and high yield, and is suitable for industrial production. The N-benzyl tryptanthrin derivative has good indoleamine-2, 3-dioxygenase (IDO) inhibitory activity, and can be used for treating diseases having the pathological feature of IDO-mediated tryptophan metabolism. 备注: 吲哚胺2,3-过氧化酶（IDO）抑制剂对癌症、阿尔兹海默、自身免疫疾病、抑郁和焦虑有疗效。示例化合物显示出对人IDO的可逆非竞争性抑制作用，活性达Ki = 2.64 mcM, IC50 = 0.5 mcM。
8. WO 2015073767 标题: Substituted 4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazine derivatives as casein kinase 1 delta/epsilon 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 65599/2013 US 904116 相关候选药物类型: 药物 相关候选药物化学结构: 适应症: 癌症、昼夜节律紊乱、神经退行性变 专利摘要: The invention provides compounds of Formula (I): [INSERT CHEMICAL STRUCTURE HERE] and pharmaceutically acceptable salts thereof. The compounds of Formula (I) inhibit protein kinase activity thereby making them useful as anticancer agents. 备注: 酪蛋白激酶-1抑制剂对治疗癌症、昼夜节律紊乱和神经退行性变有效。示例化合物对CK-1δ和CK-1ε的酶活性为IC50 = 0.01-10 nM。
9. WO 2015073797 标题: Antiparasitic compounds 申请人: Scynexis 优先权日期及相关专利公开号: 2013 US 904336 相关候选药物类型: 药物 相关候选药物化学结构: 适应症: 蠕虫感染、寄生虫感染 专利摘要: The invention relates to 1,2,4 -thiadiazole derivatives and their use to treat parasites. 备注: 示例化合物显示出驱虫活性。
10. WO 2015067650 标题: Substituted 1,2,4-triazine-3,5-diones and the use thereof as chymase inhibitors 申请人: 拜耳 优先权日期及相关专利公开号: 2013 EP 192182 相关候选药物类型: 药物 相关候选药物化学结构: 适应症: 哮喘、COPD、纤维变性、心衰、肺动脉高血压、肾病、肾衰竭 专利摘要: The invention relates to novel substituted 1,2,4-triazine-3,5-dione deratives, to a method for the production thereof, to the use thereof either alone or in combination for the treatment and/or prophylaxis of diseases, and to the use thereof for producing medicaments for the treatment and/or prophylaxis of diseases. 备注: 糜蛋白酶抑制剂对治疗哮喘、COPD、纤维变性、心衰、肺动脉高血压、肾病、肾衰竭等有效。示例化合物对仓鼠糜蛋白酶的抑制活性为IC50 = 0.0043 mcM。
11. WO 2015067755 标题: Novel methods and antibodies for treating coagulapathy 申请人: 诺和诺德 优先权日期及相关专利公开号: 2014 EP 175858/2013 US 901496/2013 EP 191940 相关候选药物类型: 药物、抗体 适应症: 第八凝血因子缺乏(血友病A)、凝血障碍 专利摘要: The present invention relates to pro-coagulant human Protein S inhibitors, such as antibodies or antigen-binding fragments thereof that can be administered subcutaneously as prophylactic treatment for haemophilia patients regardless of inhibitor status and without interfering with non-coagulant functions of Protein S. 备注: 抗体特异性结合到S蛋白EGF样区。示例单抗IgG1对S蛋白EGF样区域1-4特异性结合，对兔子血友病模型以1.18 micro liter/kg的剂量使用示例化合物显著降低血红蛋白水平。
12. WO 2015069593 标题: Substituted pyridine derivatives useful as GSK-3 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 900547 相关候选药物类型: 药物 相关候选药物化学结构: 适应症: 阿尔兹海默痴呆 专利摘要: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, antagonists of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system. 备注: GSK-3抑制剂对治疗阿尔兹海默病有效。示例化合物对GSK-3β和GSK-3α的抑制活性分别为IC50 = 0.06 及 0.07 nM，对微管相关蛋白tau磷酸化抑制作用为IC50 = 2.0 nM。
13. US 2015133395/WO 2015069939 标题: Pyrrolo[1,2,f][1,2,4]triazines useful for treating respiratory syncitial virus infections 申请人: 吉利德 优先权日期及相关专利公开号: 2014 US 534715/2013 US 902544 相关候选药物类型: 药物 相关候选药物化学结构: 适应症: 呼吸道合胞体病毒感染、肺炎 专利摘要: Provided herein are formulations, methods and substituted tetrahydrofuranyl- pyrrolo[1,2-f][1,2,4]triazine-4-amine compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of tetrahydrofuranyl-pyrrolo[1,2-fj[i,2,4]triazine-4-amine compounds. 备注: 示例化合物在人肝脏Hep2细胞中对RSV核糖核蛋白转录酶的抑制活性为IC50=0.022 mcM。
14. US 2015133447/WO 2015067770 标题: Triazolopyrazine derivatives as BRD4 inhibitors 申请人: 勃林格殷格翰 优先权日期及相关专利公开号: 2013 EP 192002 相关候选药物类型: 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 R3, X3 to X6 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: 溴区包含蛋白（Brd4，HUNK1）抑制剂可用于治疗癌症。示例化合物抑制四乙酰组蛋白H4多肽与GST-Brd4-BD1溴区的活性为IC50 = 9 nM。
15. WO 2015069594 标题: GSK-3 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 900465 相关候选药物类型: 药物 相关候选药物化学结构: 适应症: 阿尔兹海默痴呆 专利摘要: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds to treat disorders associated with GSK-3. 备注: GSK-3抑制剂对治疗阿尔兹海默病有效。示例化合物对GSK-3β和GSK-3α的抑制活性分别为IC50 = 0.04 及 0.17 nM，对微管相关蛋白tau磷酸化抑制作用为IC50 = 6.6 nM
16. US 2015133451/WO 2015068856 标题: Pyrazole for the treatment autoimmune disorders 申请人: 武田制药 优先权日期及相关专利公开号: 2014 JP 128562/2013 JP 232571 相关候选药物类型: 药物 相关候选药物化学结构: 适应症: 痛风、多发性硬化、过敏性鼻炎、系统性红斑狼疮 专利摘要: The present invention provides a heterocyclic compound having an IRAK-4 inhibitory action, which is useful for the prophylaxis or treatment of inflammatory disease, autoimmune disease, osteoarticular degenerative disease, neoplastic disease and the like, and a medicament containing thereof. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof. 备注: 白介素-受体相关激酶4（IRAK-4）和TNF-alpha生成抑制剂可用于治疗痛风、多发性硬化、过敏性鼻炎、系统性红斑狼疮。示例化合物1 mcM在LANCE试验中对IRAK-4的抑制为100 %。
| 
|手机版|药群论坛
( 蜀ICP备15007902号 )
收藏
支持
反对