著名经济学家曼斯菲尔德曾研究分析得出结论，如果没有专利保护，60%的新药就不会被发明出来，这充分说明了专利保护对药物研发的重要意义。在新药的4中知识产权保护中，也只有专利保护是国家以法律形式确定的保护，且具有独占性、力度强、范围广、保护时间长等特点，是最全面、最高级别的保护。为此，浮米网收集了并总结了上周（2014.5.10-2014.5.14）内，在全球新公布的药物专利，呈现给各位。本周公开了17项专利。其中罗氏/基因泰克公开2篇mGluR5受体拮抗剂专利、3篇TRPA1拮抗剂专利及1篇ERK抑制剂专利。拜耳公开2篇CDK9/cyclin T1抑制剂专利。默克公开2篇IRAK-4抑制剂专利。
1. WO 2014060398标题: Ethynyl derivatives as modulators of mGluR5 receptor activity
申请人: 罗氏
优先权日期及相关专利公开号: 2012 EP 188940
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: 焦虑、孤独症、抑郁、脆性X综合症、胃食管反流、疼痛、帕金森综合症、
专利摘要: The present invention relates to ethynyl derivatives of formula (I) wherein Y is N or CH R1 is fluoro or chloro R2 is hydrogen or methyl or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. It has now surprisingly been found that the compounds of general formula I are metabotropic glutamate receptor antagonists (negative allosteric modulators) for use in the treatment of anxiety and pain, depression, Fragile-X syndrom, autism spectrum disorders, Parkinson’s disease, and gastroesophageal reflux disease (GERD).
备注: mGluR5受体拮抗剂可以用于治疗焦虑、疼痛、抑郁、脆性X综合征、自闭、帕金森综合征、胃食管反流病等。本发明一个示例性的化合物可以抑制[3H]-MPEP与mGluR5a受体的结合，在EBNA细胞中，对mGluR5a的Ki值为19 nM.
2. WO 2014060394标题: Ethynyl derivatives as modulators of mGluR5 receptor activity
申请人: 罗氏
优先权日期及相关专利公开号: 2012 EP 189015
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: 焦虑、孤独症、抑郁、脆性X综合症、胃食管反流、疼痛、帕金森综合症、
专利摘要: The present invention relates to ethynyl derivatives of formula (I) or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. It has now surprisingly been found that the compounds of general formula (I) are metabotropic glutamate receptor antagonists (negative allosteric modulators) for use in the treatment of anxiety and pain, depression, Fragile-X syndrom, autism spectrum disorders, Parkinson’s disease, and gastroesophageal reflux disease (GERD).
备注: mGluR5受体拮抗剂可以用于治疗焦虑、疼痛、抑郁、脆性X综合征、自闭、帕金森综合征、胃食管反流病等。本发明一个示例性的化合物可以抑制[3H]-MPEP与mGluR5a受体的结合，在EBNA细胞中，对mGluR5a的Ki值为15 nM.
3. WO 2014060384标题: Ethynyl derivatives as modulators of mGluR5 receptor activity
申请人: 罗氏
优先权日期及相关专利公开号: 2012 EP 188943
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: 焦虑、孤独症、抑郁、脆性X综合症、胃食管反流、疼痛、帕金森综合症、
专利摘要: The present invention relates to ethynyl derivatives of formula (I) wherein Y is N or CH R1 is fluoro or chloro or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. It has now surprisingly been found that the compounds of general formula (I) are metabotropic glutamate receptor antagonists (negative allosteric modulators) for use in the treatment of anxiety and pain, depression, Fragile-X syndrom, autism spectrum disorders, Parkinson’s disease, and gastroesophageal reflux disease (GERD)
备注: mGluR5受体拮抗剂可以用于治疗焦虑、疼痛、抑郁、脆性X综合征、自闭、帕金森综合征、胃食管反流病等。本发明一个示例性的化合物可以抑制[3H]-MPEP与mGluR5a受体的结合，在EBNA细胞中，对mGluR5a的Ki值为24 nM.
4. WO 2014056958标题: Substituted phenylcarbamate compounds
申请人: 罗氏
优先权日期及相关专利公开号: 2012 US 712836
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、、慢性阻塞性肺病、鼻炎、
专利摘要: The invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein Y, R1, R2 and R3 are defined in the detailed description and claims. 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、鼻炎和支气管痉挛等。本发明的示例化合物在CHO细胞中，对TRPA1的IC50为0.0049125 mcM.
5. WO 2014060328
标题: 6-Aminoindole derivatives as TRP channel antagonists
申请人: 罗氏
优先权日期及相关专利公开号: 2012 US 714957
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、慢性阻塞性肺病、鼻炎、
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) can be used as medicament.
备注: TRPA1拮抗剂可以治疗哮喘、慢性阻塞性肺疾病、鼻炎和支气管痉挛等。本发明的示例化合物在CHO细胞中，对TRPA1的IC50为0.46mcM.
6. WO 2014060341标题: Substituted carbamate compounds and their use as transient receptor potential (TRP) channel antagonists
申请人: 罗氏
优先权日期及相关专利公开号: 2012 US 714266
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、慢性阻塞性肺病、鼻炎、
专利摘要: The invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein Y, R1 and R3 are defined in the detailed description and claims. 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、鼻炎和支气管痉挛等。本发明的示例化合物在CHO细胞中，对TRPA1的IC50为0.0104mcM.
7. WO 2014060395
标题: Serine/threonine kinase inhibitors
申请人: 基因泰克
优先权日期及相关专利公开号: 2012 US 714558
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: Compounds having the formula (I) wherein R1and R2 are as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders.
备注: ERK抑制剂，尤其是ERK2抑制剂可以用于肿瘤疾病的治疗。本发明的示例化合物对ERK2的IC50=0.0015mcM.在HepG2细胞中，可以抑制PMA诱导的P90RSK的磷酸化作用（IC50=0.0972mcM）.
8. WO 2014060376标题: 4-(Ortho)-fluorophenyl-5-fluoropyrimidin-2-yl amines containing a sulfone group
申请人: 拜耳
优先权日期及相关专利公开号: 2012 EP 189137
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: 心脏动脉瘤、心律失常、动脉疾病、癌症、心脏病、病毒感染、
专利摘要: The present invention relates to 4-(ortho)-fluorophenyl-5-fluoropyrimidin-2-yl amine derivatives of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).
备注: CDK9/cyclin T1抑制剂可以治疗肿瘤和心绞痛、心肌衰弱等心血管等疾病及病毒感染等疾病。本发明示例性的化合物可以抑制HIS标记的重组人类CDK9/cyclin T1蛋白，IC50分别为14nM;抑制GST标记的CDK2/cyclin E的IC50=1760nM.
9. WO 2014060375标题: 5-Fluoro-N-(pyridin-2-yl)pyridin-2-amine derivatives containing a sulfone group
申请人: 拜耳
优先权日期及相关专利公开号: 2012 EP 189134
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 5-fluoro-N-(pyridin-2-yl)pyridin-2-amine derivatives containing a sulfone group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).
备注: CDK9/cyclin T1抑制剂可以治疗肿瘤和心绞痛、心肌衰弱等心血管等疾病及病毒感染等疾病。本发明示例性的化合物可以抑制HIS标记的重组人类CDK9/cyclin T1蛋白，IC50分别为2 nM;抑制GST标记的CDK2/cyclin E的IC50=2180nM.
10. WO 2014062938标题: RORy modulators
申请人: Exelixis, Inc.、百时美施贵宝
优先权日期及相关专利公开号: 2012 US 716233、2012 US 716244
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: 过敏、哮喘、自身免疫疾病、癌症、代谢疾病、
专利摘要: Described are RORy modulators of the formula (I), and N-oxides thereof, and pharmaceutically acceptable salts thereof, and solvates and hydrates thereof, wherein R1, R2, R3, R4, R5, R6, Ra, x, y, L, G, Z, the bond denoted by “q”, the ring system denoted by “A” and the ring system denoted by “B” are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORy activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORy activity, for example, autoimmune and/or inflammatory disorders.
备注: 类维生素ROR gamma受体调控剂可以治疗自身免疫疾病，哮喘，鼻炎，代谢类疾病和肿瘤。本发明的示例化合物可以抑制[3H]-25-hydroxycholesterol与RORgamma的结合，IC50=1.7 nM.
11. WO 2014062636标题: Compounds for the treatment of hepatitis C
申请人: 百时美施贵宝
优先权日期及相关专利公开号: 2012 US 715734
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: 丙肝
专利摘要: The disclosure provides compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
备注: 本发明提供了一系列可用于治疗丙肝的化合物。一个示例化合物在Huh7细胞中，抑制HCV基因1a型的复制，其IC50为0.1055 nM.
12. WO 2014059902标题: 2′-Disubstituted substituted nucleoside derivatives and methods of use thereof for treatment of viral diseases
申请人: 默克
优先权日期及相关专利公开号: 2012 US 715017
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: 丙肝
专利摘要: 2′-disubstituted substituted nucleoside derivatives of formula (I) and pharmaceutically acceptable salts thereof are disclosed
1), wherein A is N3 or NH2 and X, Y, R1, R2, R3, R4,R5 and R18 are as defined herein. Compositions comprising at least one 2′-disubstituted nucleoside derivative, and methods of using the 2′-disubstituted nucleoside derivatives for treating or preventing HCV infection in a patient are disclosed.
备注: NS5B抑制剂可以治疗丙型肝炎。本发明的实例化合物可以抑制HCV基因1b型，IC50=1.3mcM.
13. WO 2014058691标题: Inhibitors of IRAK4 activity
申请人: 默克
优先权日期及相关专利公开号: 2012 US 710958
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、肠炎、类风湿性关节炎、
专利摘要: The present invention relates to inhibitors of IRAK4 of Formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
备注: IRAK-4抑制剂可以用于治疗肿瘤、类风湿性关节炎和肠炎。本发明的示例化合物可以抑制IRAK-4，IC50=32nM.
14. WO 2014058685标题: Inhibitors of IRAK4 activity
申请人: 默克
优先权日期及相关专利公开号: 2012 US 710951
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、肠炎、类风湿性关节炎、
专利摘要: The present invention relates to compounds which modulate interleukin-l (IL-1 ) receptor-associated kinase 4 (IRAK4) and are useful in the prevention or treatment of inflammatory, cell proliferative and immune-related conditions and diseases. Specifically, provided herein are inhibitors of IRAK4 of Formula I and pharmaceutical compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
备注: IRAK-4抑制剂可以用于治疗肿瘤、类风湿性关节炎和肠炎。本发明的示例化合物可以抑制IRAK-4，IC50=-0.2 nM.
15. WO 2014058538
标题: Substituted pyrrolidine thrombin inhibitors
申请人: 默克、Albany Molecular Research, Inc. (AMRI)
优先权日期及相关专利公开号: 2012 US 693376
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:静脉血栓、肺栓塞、深静脉血栓
专利摘要: 4-Substituted pyrrolidine carboxamide compounds are useful in inhibiting thrombin and associated thrombus formation for treating or preventing venous thromboembolisms.
备注: 凝血酶抑制剂可用于治疗静脉血栓、肺栓塞、深静脉血栓等。本发明的示例化合物可以抑制凝血酶，Ki=0.93 nM。
16. WO 2014060431标题: Pyrrolotriazinone derivatives as PI3K inhibitors
申请人: Almirall, SA
优先权日期及相关专利公开号: 2012 US 718787、2012 EP 382398
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: 过敏、自身免疫疾病、癌症、心血管疾病、病毒感染、炎症、代谢疾病、神经退行疾病、
专利摘要: New pyrrolotriazinone derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Phosphoinositide 3-Kinases (PI3Ks).
备注: PI3Kdelta抑制剂可以治疗过敏、自身免疫疾病、癌症、心血管疾病、病毒感染、炎症、代谢疾病、神经退行疾病等疾病。本发明的示例化合物对 PI3Kdelta的IC50 为1 nM.
17. WO 2014060113标题: Novel kinase inhibitors
申请人: Origenis GmbH
优先权日期及相关专利公开号: 2012 US 795571
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: 过敏、自身免疫疾病、眼疾、炎症 、
专利摘要: The present invention relates to novel compounds of formula (I) that are capable of inhibiting one or more kinases, especially SYK (Spleen Tyrosine Kinase), LRRK2 (Leucine-rich repeat kinase 2) and/or MYLK (Myosin light chain kinase) or mutants thereof. The compounds find applications in the treatment of a variety of diseases. These diseases include autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, alzheimer’s disease, parkinson’s disease, skin disorders, eye diseases, infectious diseases and hormone-related diseases.
备注: SYK、LRRK2、MYLK的抑制剂可用于治疗过敏、自身免疫、炎症、眼疾等疾病。本发明的示例化合物对SYK、LRRK2的IC50小于10 nM。
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