本周知名制药巨头申请的主要新药专利共22件。肿瘤、中枢神经系统、感染类疾病是新药专利申请的主要领域。罗氏本周公开的专利均是mGluR5调控剂，用于治疗中枢神经系统疾病。礼来公开了一项靶向SGLT-1小分子抑制剂专利,用于治疗糖尿病。Allergan申请了3项关于S1P1受体的配体的专利。Dana-Farber Cancer Institute公开了一项PDL-1抗体的专利。详情如下：
1. WO 2014057436标题: Anticancer conjugate
申请人: Adamed Ltd.
优先权日期及相关专利公开号: 2012 PL 401144
相关候选药物类型: 融合蛋白
相关候选药物化学结构:
适应症: 癌症
专利摘要: A conjugate comprises a fusion protein comprising domain (a), which is the functional fragment of a hTRAIL protein sequence, said fragment beginning with an amino acid at a position not lower than hTRAIL95, or a homolog of said functional fragment having at least 70% sequence identity; and domain (b) which is the sequence of an immunostimulating effector peptide; and the molecule of a chemical compound Z with antiblastic activity, which is linked to the fusion protein directly or by means ofa conjugation linker L. the conjugate is useful in the treatment of cancer diseases.
备注: 包含人类肿瘤坏死因子相关的凋亡诱导配体（hTRAL）和人类干扰素γ的融合蛋白有望治疗癌症。本发明提供的示例性融合蛋白（在人类干扰素γ的N端融合hTRAL）在小鼠动物模型中展现了非常好的有效性，且并未导致严重的副作用.
2. WO 2014056401,CN 103709227标题: Double-bond substituted tripterygium wilfordii lactone derivative and preparation method and use thereof
申请人: Shanghai Huilun Life Science & Technology Co., Ltd.
优先权日期及相关专利公开号: 2012 CN 10380144
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: Disclosed are a double-bond substituted tripterygium wilfordii lactone derivative as represented by formula (I), or pharmaceutically acceptable salt or hydrate thereof, or optical isomer thereof, wherein R1=OH, R2=H, or R1=H, R2=OH. Also disclosed are a preparation method and uses thereof in the preparation of drugs for treating cancers and cancer-related diseases.
备注: 雷公藤甲素衍生物有望治疗包括乳腺癌、肺癌、结直肠癌、前列腺癌和卵巢癌在内的多种癌症。本发明提供的示例性化合物在接种SK-OV-3癌症细胞的动物模型中的IC50为390 nM。
3. WO 2014056953标题: Pyrrolo[3,2-d]pyrimidine derivatives for the treatment of viral infections and other diseases
申请人: Janssen R&D Ireland
优先权日期及相关专利公开号: 2012 EP 187994
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: 免疫疾病,病毒感染
专利摘要: This invention concerns pyrrolo[3,2-d]pyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treatment and /or therapy of diseases.
备注: Toll样受体TLR7及TLR8受体激动剂可以治疗病毒感染、免疫类疾病和炎症。本发明的示例化合物对TLR7和TLR8的最低有效浓度（LEC）值分别为0.0004和0.5577 mcM.
4. EP 2719685,WO 2014057103标题: Inhibitors of viral replication, their process of preparation and their therapeutical uses
申请人: Laboratoire Biodim
优先权日期及相关专利公开号: 2012 US 712674,2012 EP 306244
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: HIV感染
专利摘要: Inhibitors of viral replication of formula (I), their process of preparation and their therapeutical uses. The present invention relates to compounds, their use in the treatment or the prevention of viral disorders, including HIV.
备注: 本发明提供的化合物可以抑制NL43株HIV复制，EC50为0.067mcM。
5. CN 103724269,WO 2014056446
标题: Phenyl 1,2-isoxazolyl or phenyl 1,2-pyrazole compound and application thereof
申请人: Shanghai Institute Materia Medica (SIMM)
优先权日期及相关专利公开号: 2012 CN 10384862
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: Disclosed is an application of a phenyl 1,2-isoxazolyl or 1,2-pyrazole compound of the following structure formula (I). It is proved through a biological activity test, the compound has an obvious activity of inhibiting the heat shock protein 90. Therefore, the phenyl 1,2-isoxazolyl or 1,2-pyrazole compound of the present invention can be used as an inhibitor of the heat shock protein 90 for curing cancers.
备注: 热休克蛋白90（HSP90）抑制剂可以治疗癌症。本发明提供的示例化合物可以抑制BODIPY标记的格尔德霉素与hsp90蛋白结合（IC50为0.023mcM）。对A549细胞的IC50小于0.01mcM。
6. WO 2014056710标题: Arylethynyl derivatives
申请人: F. Hoffmann-La Roche AG
优先权日期及相关专利公开号: 2012 EP 186265
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: 孤独症,认知障碍,脆性X综合征,精神分裂症
专利摘要: The present invention relates to ethynyl derivatives of formula (I) wherein • R is phenyl, 3-fluorophenyl, 4-fluorophenyl or 2,5-di-fluorophenyl; • or to a pharmaceutically acceptable acid addition salt, in enantiomerically pure form with the absolute configuration as shown in formula (I). It has now surprisingly been found that the compounds of general formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5) whic are useful for he treatment of schizophrenia, cognitive disorders, fragile X sydrome or autism and which show advantageous biochemical-, physicochemical- and pharmacodynamic- properties compared to compounds of prior art.
备注: mGluR5调控剂可以治疗精神分裂症、孤独症、认知障碍、脆性X综合征等。本发明的示例性化合物在HEK-293中调控mGluR5，EC50=10nM.
7. WO 2014057435标题: Orexin receptor antagonists which are [ortho bi(hetero)aryl]-[2-(meta bi(hetero)aryl)-pyrrolidin-1-yl]-methanone derivatives
申请人: Actelion Pharmaceuticals Ltd.
优先权日期及相关专利公开号: 2013 EP 157809,2012 EP 188019
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,认知障碍,饮食失调,情感障碍,失眠,物质滥用
专利摘要: The present invention relates to [ortho bi-(hetero-)aryl]-[2-(meta bi-(hetero-)aryl)-pyrrolidin-1-yl]- methanone derivatives of formula (I) wherein R, and the rings A1 A2 and A3 are as described in the description, to pharmaceutically acceptable salts thereof, to their preparation, to pharmaceutical compositions containing one or more compounds of formula (I), and to their use as pharmaceuticals, especially to their use as orexin receptor antagonists.
备注: 阿立新OX-1和OX-2受体拮抗剂可以治疗失眠、焦虑、物质滥用、认知障碍和饮食失调等疾病。本发明示例性化合物在CHO细胞中，对OX-1和OX-2的IC50分别为5nM和6nM.
8. WO 2014055297,US 2014100179
标题: Novel urea compounds
申请人: Eli Lilly and Company
优先权日期及相关专利公开号: 2012 US 710123,2013 US 35997
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: 糖尿病
专利摘要: The present invention provides a compound of Formula I:, or a pharmaceutically acceptable salt thereof.
备注: SGLT-1抑制剂可以治疗糖尿病。本发明的示例化合物对鼠源和人源SGLT-1的IC50分别为7.3nM和17.3nM.且对人源SGLT-2的IC50为171 nM.
9. WO 2014054635标题: Imidazole derivative
申请人: Dainippon Sumitomo Pharma Co., Ltd.
优先权日期及相关专利公开号: 2012 JP 219934
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: 注意缺陷/多动障碍(ADHD）,脑缺血,认知障碍,唐氏综合症
专利摘要: Provided is a therapeutic agent for diseases associated with a cholinergic property of the central nervous system (CNS) and/or the peripheral nervous system (PNS), diseases associated with the contraction of smooth muscle, incretion diseases, diseases associated with neuronal degeneration and the like, said therapeutic agent comprising a compound represented by formula (I) [wherein X-Y-Z represents N-CO-NR4AR4B or the like; R1 represents a phenyl group or the like; R2A and R2B may be the same as or different from each other and independently represent a hydrogen atom or the like; R3A to R3D and R6 may be the same as or different from one another and independently represent a hydrogen atom or the like; R4A and R4B may be the same as or different from each other and independently represent an aryl group or the like; and n represents 1 or 2] or a pharmaceutically acceptable salt thereof and having a potent activity of regulating an a7 nicotinic acetylcholine receptor (an a7 nAChR).
备注: 烟碱alpha7乙酰胆碱受体变构调控剂可以治疗精神分裂症相关的认知障碍，阿尔兹海默，唐氏综合症等中枢神经疾病。本发明提供的示例化合物在GH4C1细胞中，浓度为10mcM时，活性为836%.
10. WO 2014049133标题: New positive allosteric modulators of nicotinic acetylcholine receptor
申请人: H. Lundbeck A/S
优先权日期及相关专利公开号: 2012 DK 588
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: 注意缺陷/多动障碍(ADHD），痴呆，阿尔兹海默，糖尿病，炎症，疼痛，精神错乱，脑外伤
专利摘要: The present invention relates to indole derivatives useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said com- pounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine a7 receptor.
备注: 烟碱alpha7乙酰胆碱受体变构调控剂可以治疗精神分裂症相关的认知障碍，阿尔兹海默，唐氏综合症等中枢神经疾病。本发明提供的示例化合物在GH4C1细胞中，EC50 = 800 nM.
11. WO 2014054634标题: Pyrimidine derivative
申请人: Dainippon Sumitomo Pharma Co., Ltd.
优先权日期及相关专利公开号: 2012 JP 220577
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: 注意缺陷/多动障碍(ADHD）,脑缺血,认知障碍,唐氏综合症
专利摘要: Provided is a therapeutic agent for diseases associated with a cholinergic property of the central nervous system (CNS) and/or the peripheral nervous system (PNS), diseases associated with the contraction of smooth muscle, incretion diseases, diseases associated with neuronal degeneration and the like, said therapeutic agent comprising a compound represented by formula (I) [wherein X-Y-Z represents NR6-N=C or the like; A represents CR1D or the like; B1 represents a nitrogen atom or the like; B2 represents a single bond or the like; R1A to R1D may be the same as or different from one another and independently represent a hydrogen atom or the like; R2A to R2E may be the same as or different from one another and independently represent a hydrogen atom or the like; and R3, R4 and R5 may be the same as or different from one another and independently represent a hydrogen atom or the like] or a pharmaceutically acceptable salt thereof and having a potent activity of regulating an a7 nicotinic acetylcholine receptor (an a7 nAChR).
备注: 烟碱alpha7乙酰胆碱受体变构调控剂可以治疗精神分裂症相关的认知障碍，阿尔兹海默，唐氏综合症等中枢神经疾病。本发明提供的示例化合物在GH4C1细胞中，浓度为10mcM时，活性为1748%.
12. WO 2014055595标题: Indoline compounds as aldosterone synthase inhibitiors related applications
申请人: ElexoPharm GmbH,Merck & Co., Inc.
优先权日期及相关专利公开号: 2012 US 710197
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: 心力衰竭,高血压
专利摘要: This invention relates to indo line compounds of the structural formula I, or their pharmaceutically acceptable salts, wherein the variables are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatmen amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthase.
备注: 细胞色素P450 11B2抑制剂可以治疗高血压、心力衰竭、冠心病、肝病、低钾症、心肌梗塞和肾衰竭等疾病。本发明的示例化合物可以抑制CYP11B2（IC50=0.2 nM）,且对CYP11B1具有选择性（IC50=68 nM）.
13. WO 2014055461标题: IAP antagonists
申请人: Bristol-Myers Squibb Co.
优先权日期及相关专利公开号: 2012 US 708828
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: There are disclosed compounds that modulate the activity of inhibitors of apoptosis (IAPs), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.
备注: XIAP抑制剂可以治疗癌症。本发明一个示例性化合物可以抑制XIAP的BIR3域和BIR2域，IC50分别为0.06和0.03mcM。
14. WO 2014055311标题: Substituted isoquinolines as CRTH2 receptor modulators
申请人: Merck & Co., Inc.
优先权日期及相关专利公开号: 2012 US 708327
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(COPD)
专利摘要: The invention provides certain substituted isoquinolines of the Formula (I), and their pharmaceutically acceptable salts and esters. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.
备注: CRTH2受体拮抗剂可以治疗哮喘、鼻炎和慢性阻塞性肺疾病。本发明的一个示例性化合物可以抑制[3H]-PGD2与CRTH2受体的结合（Ki=5.519nM）.
15. WO 2014055934标题: Substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase BTK inhibitors
申请人: University of Utah
优先权日期及相关专利公开号: 2012 US 709534
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,炎症
专利摘要: In one aspect, the invention relates to substituted N-(3-(pyrimidin-4- yl)phenyl)acrylamide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the BTK kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the BTK kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
备注: BTK抑制剂可以治疗癌症和炎症。本发明的一个示例化合物对BTK的IC50=0.004mcM.
16. WO 2014055928标题: Substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase BTK inhibitors
申请人: University of Utah
优先权日期及相关专利公开号: 2012 US 709519
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,炎症
专利摘要: In one aspect, the invention relates to substituted N-(3-(pyrimidin-4- yl)phenyl)acrylamide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the BTK kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the BTK kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
备注: BTK抑制剂可以治疗癌症和炎症。本发明的一个示例化合物对BTK的IC50=0.008mcM.
17. WO 2014055921标题: 1,2,4-Oxadiazoles azetidine derivatives as sphingosine-1 phosphate receptors modulators
申请人: Allergan, Inc.
优先权日期及相关专利公开号: 2013 US 41465
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: 过敏症,自身免疫病,癌症,眼疾,免疫抑制,炎症,疼痛
专利摘要: The present invention relates to 1,2,4-oxadiazoles 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受体的配体可以治疗疼痛，眼疾，自身免疫疾病，过敏，炎症和癌症等疾病。本发明一个示例性化合物对S1P1的EC50为483.13 nM。
18. US 2014100199标题: Substituted aryl-1,2,4-oxadiazole derivatives useful for the treatment of interalia ocular or inflammatory diseases
申请人: Allergan, Inc.
优先权日期及相关专利公开号: 2013 US 41539
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: 过敏症,自身免疫病,癌症,眼疾,免疫抑制,炎症,疼痛
专利摘要: The present invention relates to substituted aryl 1,2,4-oxadiazoles derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
备注: S1P1受体的配体可以治疗疼痛，眼疾，自身免疫疾病，过敏，炎症和癌症等疾病。本发明一个示例性化合物对S1P1的EC50为16.9 nM.
19. WO 2014055911标题: Bicyclic 1,2,4-oxadiazoles derivatives as sphingosine-1 phosphate receptors modulators
申请人: Allergan, Inc.
优先权日期及相关专利公开号: 2012 US 709854
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: 过敏症,自身免疫病,癌症,眼疾,免疫抑制,炎症,疼痛
专利摘要: The present invention relates to bicyclic aryl 1,2,4-oxadiazoles derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
备注: S1P1受体的配体可以治疗疼痛，眼疾，自身免疫疾病，过敏，炎症和癌症等疾病。本发明一个示例性化合物对S1P1的EC50为3.52 nM.
20. WO 2014055897标题: Human monoclonal anti-PD-L1 antibodies and methods of use
申请人: Dana-Farber Cancer Institute, Inc.
优先权日期及相关专利公开号: 2013 US 779969,2012 US 709731
相关候选药物类型: 抗体
相关候选药物化学结构:
适应症: 癌症,HIV感染
专利摘要: The present invention comprises human monoclonal antibodies that bind to PD-L1 (also known as programmed death ligand 1 or B7H1). Binding of the invented antibody to PD-L1 inhibits binding to its receptor, PD1 (programmed death 1), and ligand-mediated activities and can be used to treat cancer and chronic viral infections.
备注: PDL-1抗体可以治疗癌症和慢性病毒感染。本发明提供了修饰的人源lgG抗体可以靶向PDL-1，抑制PD-1与PDL-1的结合。
21. WO 2014048072，CN 103709151标题: Spiro ring compounds as hepatitis C virus (HCV) inhibitors
申请人: Sunshine Lake Pharma Co., Ltd.
优先权日期及相关专利公开号: 2013 CN 10117051，2012 CN 10366536
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: HCV感染
专利摘要: A compound of formula (I) or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof is provided, which can be used for treating HCV infection or a HCV disorder. Also a pharmaceutical composition comprising the compound and the use of the compound and the pharmaceutical composition thereof are provided, which can also be used for treating HCV infection or a HCV disorder.
备注: NS5A抑制剂可以治疗HCV感染。本发明一个示例性化合物可以抑制HCV基因1a型和1b型（EC50=0.008nM和0.005nM）.
22. WO 2014051653标题: Bicyclic dihydropyridone kinase inhibitors
申请人: Portola Pharmaceuticals, Inc.
优先权日期及相关专利公开号: 2012 US 706681
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: 自身免疫病，癌症，心血管疾病，炎症
专利摘要: Provided are bicyclic dihydropyridone compounds for inhibiting of JAK/Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting JAK/Syk kinase activity, and methods for treating conditions mediated at least in part by JAK/Syk kinase activity.
备注: Syk抑制剂可以治疗癌症、自身免疫疾病、炎症和心血管疾病。本发明提供了一系列IC50小于100nM的Syk抑制剂。
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