本周知名制药巨头申请的主要新药专利共16件。肿瘤、中枢神经系统、感染和代谢类疾病依旧是新药专利申请的主要领域。辉瑞本周公开的3项专利均是TRKA抑制剂，用于治疗肿瘤及疼痛。赛诺菲公开了一项靶向pim激酶的小分子抑制剂专利，pim抑制剂可以用于治疗肿瘤。罗氏本周公开的专利显示，苯并咪唑类化合物可用于中枢神经系统疾病的治疗。Laboratoire Biodim申请了两项关于HIV病毒复制抑制剂的专利。详情如下：
1. WO 2014053968标题: Pyrrolo[3,2-c]pyridine tropomyosin-related kinase inhibitors
申请人: 辉瑞
优先权日期及相关专利公开号: 2012 US 709497
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、疼痛
专利摘要: The present invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as Trk antagonists.
备注: TRKA抑制剂可以治疗癌症和疼痛。本发明的示例化合物对TRKA的IC50为2.87 nM。
2. WO 2014053965标题: Tropomyosin-related kinase inhibitors
申请人: 辉瑞
优先权日期及相关专利公开号: 2012 US 709513
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、疼痛
专利摘要: The present invention relates to compounds of Formula (IA) and (IB) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as Trk antagonists.
备注: TRKA抑制剂可以治疗癌症和疼痛。本发明的示例化合物对TRKA的IC50为16.6 nM.
3. WO 2014053967标题: Pyrrolo[2,3-d]pyrimidine tropomyosin-related kinase inhibitors
申请人: 辉瑞
优先权日期及相关专利公开号: 2012 US 709482
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、疼痛
专利摘要: The present invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as Trk antagonists.
备注: TRKA抑制剂可以用于治疗疼痛和癌症。本发明的示例化合物对TRKA的IC50为4.24 nM.
4. WO 2014053595标题: Acylaminopyrimidine derivatives for the treatment of viral infections and further diseases
申请人: 杨森
优先权日期及相关专利公开号: 2012 EP 187519
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、免疫疾病、病毒感染
专利摘要: This invention relates to acylaminopyrimidine derivatives of formula (I), processes for their preparation, pharmaceutical compositions, and their use in therapy.
备注: 作为干扰素诱导物的化合物可以用于治疗癌症，病毒感染和免疫类疾病。本发明的示例化合物可以诱导内生性干扰素-alpha的产生以及上调CXCL 10 mRNA的表达水平。
5. WO 2014053568标题: Indolyldihydroimidazopyrimidinone derivatives, preparation thereof and therapeutic use thereof
申请人: 赛诺菲
优先权日期及相关专利公开号: 2012 US 740244、2012 FR 59315
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 invention relates to the novel products of formula (I): in which R1 represents H, Alk or cycloalkyl optionally substituted with one or more Hal; R2 represents H or Hal; and R3 represents H; Hal, OH; NO2; C2-C6 alkenyl; C2-C6 alkynyl; -Y-alkyl; R; OR; -CO2H; -CO2R; -NRxRy, -CONRxRy or -CO2NRxRy, all optionally substituted; where Y represents S, SO or SO2; NRxRy is such that either Rx represents H, alk or cycloalkyl and Ry represents H, alk, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, COR or SO2R, all optionally substituted; or Rx and Ry form, with N, an optionally substituted cyclic radical; R represents alk, cycloalkyl, heterocycloalkyl, aryl or heteroaryl, all optionally substituted; with one or more H representing a deuterium atom; these products being in any of the isomer forms, and the salts, as medicaments, in particular as anticancer agents.
备注: pim激酶抑制及可以治疗癌症。本发明的示例化合物对pim-1，pim-2的IC50分别为0.69 和25.9 nM.
6. WO 2014053409标题: Benzimidazoles as CNS active agents
申请人: 罗氏
优先权日期及相关专利公开号: 2012 EP 186784
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、阿尔兹海默性痴呆、抑郁、中风
专利摘要: The present invention relates to compounds of general formula wherein R1 hydrogen, lower alkyl, halogen or lower alkyl substituted by halogen; R2 is hydrogen or halogen; X1 is N or CH; X2 is N or CH; with the proviso that only one of X1 or X2 is N; X3 is C(R) or N; and R is hydrogen, lower alkyl, halogen, lower alkyl substituted by halogen, lower alkoxy or SO2-lower alkyl; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof. The compounds may be used for the treatment of schizophrenia, obsessive-compulsive personality disorder, major 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, mild 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, such as alcohol, opiates, methamphetamine, phencyclidine and cocaine.
备注: 苯并咪唑可以刺激神经干细胞形成神经元，因此可以用于治疗阿尔兹海默，抑郁，焦虑，中风，精神分裂症，帕金森症，唐氏综合症，多发性硬化症等疾病。本发明提供的化合物对胚胎干细胞的EC50达到0.008 mcM。
7. WO 2014048869标题: Substituted indazol-pyrrolopyrimidines useful in the treatment of hyperproliferative diseases
申请人: 拜耳
优先权日期及相关专利公开号: 2012 EP 186032、2013 EP 154193
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 substituted indazol-pyrrolopyrimidine compounds of general formula (I):in which R1a, R1b, R1c, R1d, R2a and R2b are 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等增生性疾病。本专利提供的示例化合物对GST标签的MNK1的IC50小于1 nM.
8. WO 2014053491标题: Inhibitors of histone demethylases
申请人: EpiTherapeutics ApS
优先权日期及相关专利公开号: 2013 DK 70112
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 application discloses compounds capable of modulating the activity of histone demethylases (HDMEs), which are useful for prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, such as e.g. cancer. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament. The compounds take the form (I).
备注: 组蛋白赖氨酸脱甲基酶抑制剂可治疗癌症。本发明中的示例化合物对GASC-1HE PLU1的IC50分别为10-1000 nM和100 nM。
9. WO 2014055647标题: (Sulfinyl and sulfonyl benzimidazolyl) pyrimidines and triazines, pharmaceutical compositions thereof, and their use for treating proliferative diseases
申请人: MEI Pharma, Inc.
优先权日期及相关专利公开号: 2012 US 744821
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: Provided herein are (sulfmyl and sulfonyl benzimidazolyl) pyrimidines and triazines, e.g., a compound of Formula I, and their pharmaceutical compositions, and use for treating proliferative diseases.
备注: PI3K delta 抑制剂可以治疗癌症和炎症。本发明中的示例化合物对PI3K delta的IC50为8.4 nM.且对PI3K alpha，PI3Kbeta,PI3K gamma和mTOR的IC50分别为>4600，>8790，1919，>10000 nM。且在MDA-MB-453，PC-3及RAW264.7细胞的IC50分别为5820，1730，1150 nM。
10. WO 2014053694标题: N-Prop-2-ynyl carboxamide derivatives and their use as TRPA1 antagonists
申请人: Orion Corp. (FI)
优先权日期及相关专利公开号: 2012 US 708330
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、咳嗽、糖尿病、肠炎、疼痛
专利摘要: Compounds of formula I, wherein A, B, X, Z and R1-R6, are as defined in the claims, exhibit TRPA 1 activity and are thus useful as TRPA1 modulators.
备注: TRPA1拮抗剂可以治疗疼痛，哮喘，慢性阻塞性肺疾病，咳嗽，糖尿病和肠炎等疾病。本发明中的TRPA1拮抗剂的IC50达到0.1 mcM。
11. WO 2014055474、US 2014107049标题: Mannose derivatives for treating bacterial infections
申请人: Vertex Pharmaceuticals Inc.
优先权日期及相关专利公开号: 2012 US 709686
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: 尿路感染、肠炎
专利摘要: The present invention relates to compounds useful for the treatment or prevention of bacteria infections. The invention also provides pharmaceutically acceptable compositions containing the compounds and methods of using the compositions in the treatment of bacteria infections. The invention also provides processes for making the compounds of the invention. The compounds of the present invention are represented by the following structure of Formula (A); wherein the variables are as described herein.
备注: 寡糖可以作为FimH抑制剂以治疗尿路感染，肠炎等细菌感染。本发明的示例化合物展示了对FimH的良好的亲和力，其Kd值达到0.019 mcM.
12. WO 2014054053标题: Spirocyclic compounds, compositions and medicinal applications thereof
申请人: Advinus Therapeutics Pvt. Ltd.
优先权日期及相关专利公开号: 2012 IN 4129
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: II型糖尿病、HCV感染、肥胖
专利摘要: The present disclosure relates to a series of spirocyclic compounds of formula (I), their stereoisomers, tautomers, prodrugs, pharmaceutically acceptable salts, polymorphs, solvates, hydrates, N-Oxides, Co crystals and formulations thereof. The disclosure also relates to process of preparation of these spirocyclic compounds. Formula (I). These compounds are useful in the treatment, prevention, prophylaxis, management, or adjunct treatment of all medical conditions related to inhibition of acyl CoA diacyl glycerol acyltransferase 1 (DGAT1).
备注: DGAT-1抑制剂可以治疗II型糖尿病，肥胖，HCV感染，高胆固醇血症，糖尿病神经病变。胰腺炎等疾病。本发明中的示例化合物对DGAT-1的IC50为4 nM.
13. WO 2014053665、EP 2716632
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 EP 306222、2012 US 710498
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: The present invention relates to compounds of formula (I), their the treatment or the prevention of viral disorders, including HIV.
备注: HIV病毒复制抑制剂可以治疗HIV感染。本发明的示例化合物可以抑制 HIV-1 NL4.3，其EC50达到0.17 mcM。
14. WO 2014053666、EP 2716639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 710358、2012 EP 187528
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: The present invention relates to compounds, their use in the treatment or the prevention of viral disorders, including HIV.
备注: HIV病毒复制抑制剂可以治疗HIV感染。本发明的示例化合物可以抑制 HIV-1 NL4.3，其EC50达到0.04 mcM。
15. WO 2014052619标题: Piperidine derivatives and compositions as modulators of GPR119 activity
申请人: IRM, LLC
优先权日期及相关专利公开号: 2012 US 706637
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、血脂过多、肥胖
专利摘要: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119. The compounds are of Formula I: wherein the variables are as defined herein.
备注: GPR119配体可以治疗糖尿病，肥胖，高血脂等代谢类疾病。此外，也对高血压，血栓等疾病有治疗效果。本发明提供的示例化合物对CPR119的EC50达到4.6 nM。
16. WO 2014045283
标题: Restoration of the CFTR function by splicing modulation
申请人: Yissum Research Development Co.
优先权日期及相关专利公开号: 212 US 74859
相关候选药物类型: 反义药物
相关候选药物化学结构:
适应症: 囊性纤维化
专利摘要: The present provides oligonucleotides capable of binding to and modulating the splicing of the pre-mRNA of the CFTR gene, compositions comprising said oligonucleotides, kits comprising said compositions, and uses thereof. In particular, the present invention provides compositions of oligonucleotides useful in methods for suppressing exon 10 skipping optionally in combination with additional CFTR therapeutics.
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