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浮米每周专利快讯：2014年4月（一）已有1人参与
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1. WO 2014032188 标题: Glycosidase inhibitors and uses thereof 申请人: 默克，Alectos Therapeutics Inc. 优先权日期及相关专利公开号: 2012 US 695987 相关候选药物类型: 适应症: 肿瘤，心血管系统疾病，神经退行性疾病 专利摘要: The invention provides compounds for inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc. 备注: N-乙酰-B-D氨基葡萄糖苷酶 (O-GlcNAcase)抑制剂可以用于治疗肿瘤、神经退行性疾病及心血管系统等多种疾病。本专利提供的示例化合物对O-GlcNAcase的Ki值为16 nM. 2.WO 2014032187 标题: Glycosidase inhibitors and uses thereof 申请人: 默克，Alectos Therapeutics Inc. 优先权日期及相关专利公开号: 2012 US 696003 相关候选药物类型: 适应症: 肿瘤，心血管系统疾病，神经退行性疾病 专利摘要: The invention provides compounds of Formula (I) for inhibiting gh cosidases, prodrugs of the compounds, and pharmaceutical compositions comprising the compounds or prodrugs of the compounds. The invention also provides method of treating diseases and disorders related to deficiency or over-expression of O-gh coprotein 2-acetamido-2- deoxy-ß-D-giucopyranosidase (O-GlcNAcase), accumulation or deficiency of 2-acetamido-2-deoxy-ß-D- glucopyranoside (O-GlcNAc). 备注: N-乙酰-B-D氨基葡萄糖苷酶 (O-GlcNAcase)抑制剂可以用于治疗肿瘤、神经退行性疾病及心血管系统等多种疾病。本专利提供的示例化合物对O-GlcNAcase的Ki值为2578 nM. 3. WO 2014032185 标题: Glycosidase inhibitors and uses thereof 申请人: 默克，Alectos Therapeutics Inc. 优先权日期及相关专利公开号: 2012 US 696026 相关候选药物类型: 适应症: 肿瘤，心血管系统疾病，神经退行性疾病 专利摘要: The invention provides compounds for inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc. 备注: N-乙酰-B-D氨基葡萄糖苷酶 (O-GlcNAcase)抑制剂可以用于治疗肿瘤、神经退行性疾病及心血管系统等多种疾病。本专利提供的示例化合物对O-GlcNAcase的Ki值为16.5mcM. 4.WO 2014032184 标题: Glycosidase inhibitors and uses thereof 申请人: 默克，Alectos Therapeutics Inc. 优先权日期及相关专利公开号: 2012 US 695939 相关候选药物类型: 适应症: 肿瘤，心血管系统疾病，神经退行性疾病 专利摘要: The invention provides compounds for inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc. 备注: N-乙酰-B-D氨基葡萄糖苷酶 (O-GlcNAcase)抑制剂可以用于治疗肿瘤、神经退行性疾病及心血管系统等多种疾病。本专利提供的示例化合物对O-GlcNAcase的Ki值为16.5mcM.9.4 nM. 5. WO 2014034898 标题: Pyridine derivative and medicine 申请人: Nippon Shinyaku Co., Ltd. 优先权日期及相关专利公开号: 2012 JP 190548，2012 JP 215947 相关候选药物类型: 适应症: 胃食管反流病(GERD)，下尿路症状(LUTS)，疼痛 专利摘要: The main purpose of the invention is to provide a novel pyridine derivative or a pharmaceutically acceptable salt thereof. Examples of the invention include a pyridine derivative represented by general formula [1], and a pharmaceutically acceptable salt thereof. This compound or a pharmaceutically acceptable salt thereof exhibits mGluR5 inhibitory activity, and can therefore be used as an agent for the prevention or treatment of, e.g., pain (for example, acute pain, chronic pain, inflammatory pain, neuropathic pain, hyperalgesia, thermal hyperalgesia, allodynia, pain due to noxious thermal stimulation, pain due to noxious mechanical stimulation, pain in the lower urinary tract or reproductive organs, or migraine), pruritus, lower urinary tract symptoms or lower urinary tract disorders, gastroesophageal reflux disease (GERD), gastroesophageal reflux associated with transient lower esophageal sphincter relaxation (TLESR), and diseases of the central nervous system. 备注: mGluR5拮抗剂可以治疗疼痛、胃食管反流病(GERD) 、下尿路症状(LUTS)、X染色体易损综合征和中枢神经系统疾病。本发明提供了一系列mGluR5拮抗剂。化合物对 mGluR5 的 IC50 值为36 nM。 6.WO 2014034719 标题: Quinoline derivative having TLR inhibitory activity 申请人: Kowa Co., Ltd. 优先权日期及相关专利公开号: 2012 JP 188968，2012 JP 232798 相关候选药物类型: 适应症: 过敏症，哮喘，自身免疫疾病，移植物抗宿主反应，炎症，败血症，移植排斥 专利摘要: A compound represented by general formula (1), a salt of the compound, or a solvate of the compound or the salt, which can inhibit TLR3, 7 and/or 9 and has an excellent prophylactic and/or therapeutic effect on autoimmune diseases, inflammations, allergies, asthma, graft rejection, GvHD or cardiomyopathy associated with sepsis. A: a (substituted) 5- to 6-membered saturated nitrogen-containing heterocyclic ring; Y: a bond or a phenylene group; Z: a bond, a C1-6 alkylene group, N-R7 or O; R1, R3 and R5 to R8: H, a C1-3 alkyl group or the like; R7: H, a C1-6 alkyl group or a 2-nitrobenzenesulfonyl group; and R2 and R4: one represents R8 and the other represents a group represented by formula (2) (wherein B: a (substituted) carbocyclic/heterocyclic ring, W: a C2-6 alkenylene group or the like, X, V: a bond, C(O)NH, NHC(O) or the like, and U: a bond or a C1-6 alkylene group; wherein a case in which each of X, V and U is a bond is excluded). 备注: Toll样受体拮抗剂，尤其是TLR7和TLR9拮抗剂可以用于治疗等疾病。本发明中的示例性 化合物可以抑制TLR7和TLR9，IC50分别为543nM和15 nM. 7. WO 2014033631 标题: N-(3-Pyridyl) biarylamides as kinase inhibitors 申请人: 诺华 优先权日期及相关专利公开号: 2012 US 695602 相关候选药物类型: 适应症: 肿瘤，肠炎，类风湿性关节炎 专利摘要: The present invention provides a compound of formula (I): as described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula (I), and pharmaceutical compositions comprising such compounds. 备注: Pim（包括Pim-1、2 、 3 ）抑制剂可以用于肿瘤、自身免疫疾病、肠炎等疾病。本发明中化合物对pim1,pim2，pim3的IC50分别为0.00002, 0.00053和0.0004 mcM。 8. WO 2014035140 标题: Compounds and compositions for modulating histone methyltransferase activity 申请人: Kainos Medicine, Inc. 优先权日期及相关专利公开号: 2012 US 694892 相关候选药物类型: 适应症: 肿瘤 专利摘要: The invention provides DOT1L inhibitors, and also methods and use of the compounds of the invention, by themselves or in combination with other therapies, for treating a disease, disorder, or condition. 备注: DOT1L抑制剂可以作为抗肿瘤药的候选。本发明中提供了高选择性的抑制剂，其对 DOT1L的IC50为0.4 nM，且对 EZH1, EZH2, G9a, PRMT4, 和SET7的IC50均大于10 mcM. 9. WO 2014033196，US 2014065136 标题: Dioxino- and oxazin-[2,3-d]pyrimidine PI3K inhibitor compounds and methods of use 申请人: 基因泰克 优先权日期及相关专利公开号: 2013 US 13256，2012 US 694898 相关候选药物类型: 适应症: 肿瘤 专利摘要: Dioxino- and oxazin-[2,3-d]pyrimidine PI3K inhibitor compounds of Formula I with anti-cancer activity, anti-inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions. 备注: PI3K抑制剂可以用于治疗肿瘤。本发明中的化合物对MDA-MB-361.1和PC-3的EC50分别为0.544和0.489 mcM。 10. WO 2014033446 标题: Kinase inhibitors 申请人: RespiVert Ltd.，Topivert Pharma Ltd. 优先权日期及相关专利公开号: 2012 GB 15370，2013 GB 4780 相关候选药物类型: 适应症: 哮喘，慢性阻塞性肺病，肠炎 专利摘要: There are provided compounds of formula (I), (Formula (I)) wherein R1 to R5, X1, X2, Ar, L, A, A1, E and G have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines. 备注: MAPK14（MAPK p38 alpha）抑制剂，Src抑制剂，Syk抑制剂可用于治疗哮喘、COPD、肠炎、肺动脉高压等疾病。本发明所示的化合物对MAPK p38 alpha、Src、Syk的IC50分别为71nM、2nM、8nM。同时对GSK3alpha具有选择性（IC50=1096 nM）。 11. WO 2014033447 标题: Kinase inhibitors 申请人: RespiVert Ltd.，Topivert Pharma Ltd. 优先权日期及相关专利公开号: 2012 GB 15369，2013 GB 4777 相关候选药物类型: 适应症: 哮喘，慢性阻塞性肺病，肠炎 专利摘要: There are provided compounds of formula (I), (Formula (I)) wherein R1 to R5, X1, X2, Ar, L, E, A, A1, G and G1 have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines. 备注: MAPK14（MAPK p38 alpha）抑制剂，Src抑制剂，Syk抑制剂可用于治疗哮喘、COPD、肠炎、肺动脉高压等疾病。本发明所示的化合物对MAPK p38 alpha、Src、Syk的IC50分别为152 nM、16 nM、61 nM。同时对GSK3alpha具有选择性（IC50=6398 nM）。 12. WO 2014033448 标题: Pyrazole derivatives as p38 MAP inhibitors 申请人: RespiVert Ltd.，Topivert Pharma Ltd. 优先权日期及相关专利公开号: 2012 GB 15357 相关候选药物类型: 适应症: 哮喘，慢性阻塞性肺病 专利摘要: Compounds of formula (I) wherein R1, R2, J, Q, V, X, Y and Z are defined herein are disclosed. The compounds are inhibitors of the family of p38 mitogen-activated protein kinase enzymes (referred to herein as p38 MAP kinase inhibitors), particularly the alpha sub-type thereof, and of Syk kinase and the Src family of tyrosine kinases. The compounds may be used in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, in particular inflammatory diseases of the lung, such as asthma and COPD, as well as those of the gastrointestinal tract, such as ulcerative colitis and Crohn’s disease and of the eye, such as uveitis. 备注: MAPK14（MAPK p38 alpha）抑制剂，Src抑制剂，Syk抑制剂可用于治疗哮喘、COPD、肠炎、肺动脉高压等疾病。本发明所示的化合物对MAPK p38 alpha、Src、Syk的IC50分别为46 nM、2 nM、3 nM。同时对GSK3alpha具有选择性（IC50>13300 nM）。 13. WO 2014033449 标题: Kinase inhibitors 申请人: RespiVert Ltd.，Topivert Pharma Ltd. 优先权日期及相关专利公开号: 2012 GB 15368，2013 GB 4773 相关候选药物类型: 适应症: 哮喘，慢性阻塞性肺病，肠炎，葡萄膜炎 专利摘要: There are provided compounds of formula I, (I) wherein R1 to R5, X1, X2, Ar, L, E, A, A1, G and G1 have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines. 备注: MAPK14（MAPK p38 alpha）抑制剂，Src抑制剂，Syk抑制剂可用于治疗哮喘、COPD、肠炎、肺动脉高压等疾病。本发明所示的化合物对MAPK p38 alpha、Src、Syk的IC50分别为204 nM、17 nM、89 nM。同时对GSK3alpha具有选择性（IC50 = 11629）。 14. WO 2014033630 标题: Novel aminothiazole carboxamides as kinase inhibitors 申请人: 诺华 优先权日期及相关专利公开号: 2012 US 695618 相关候选药物类型: 适应症: 肿瘤，肠炎，类风湿性关节炎 专利摘要: The present invention provides a compound of formula (I), as described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula I, and pharmaceutical compositions comprising such compounds. 备注: Pim（包括Pim-1、2 、 3 ）抑制剂可以用于肿瘤、自身免疫疾病、肠炎等疾病。本发明中化合物对pim1,pim2，pim3的IC50分别为0.0000107, 0.00042和0.000322 mcM。 15. WO 2014029732 标题: Pyrrolo[2,3-b]pyrazines as SYK inhibitors 申请人: 罗氏 优先权日期及相关专利公开号: 2012 US 691384 相关候选药物类型: 适应症: 自身免疫疾病，肿瘤，炎症 专利摘要: The present invention relates to the use of novel pyrrolo[2,3- b]]pyrazines wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases. 备注: Syk 激酶抑制剂可以作用于治疗肿瘤、炎症和自身免疫疾病等多种疾病。本发明的示例化合物对Syk的IC50 = 0.0137 mcM. 16. WO 2014031517 标题: Novel azabenzimidazole tetrahydrofuran derivatives 申请人: 默克 优先权日期及相关专利公开号: 2012 US 692021 相关候选药物类型: 适应症: II型糖尿病 专利摘要: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension. 备注: AMPK激活剂可以治疗II型糖尿病、肥胖、高血脂、高血压等疾病。本发明中的化合物对AMPK复合物7的EC50=2 nM . 17. WO 2014031515 标题: Novel azabenzimidazole hexahydrofuro[3,2-b]furan derivatives 申请人: 默克 优先权日期及相关专利公开号: 2012 US 692018 相关候选药物类型: 适应症: II型糖尿病 专利摘要: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension. 备注: AMPK激活剂可以治疗II型糖尿病、肥胖、高血脂、高血压等疾病。本发明中的化合物对AMPK复合物7的EC50=1 nM。 |
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