1. WO 2014110065标题: (Thieno[2,3-b][1,5]benzoxazepin-4-yl)piperazin-1-yl compounds as dual activity H1 inverse agonists/5-HT2A antagonists
申请人: 礼来
优先权日期及相关专利公开号: 2013 US 752203
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: 失眠
专利摘要: A dual H1 inverse agonist/5-HT2A receptor antagonist of the formula: [Formula I], its uses, and methods for its preparation are described.
备注: 组胺H1受体反义激动剂和/或5-HT2A受体拮抗剂可以用于治疗失眠。本发明的化合物可以抑制[3H]-嘧啶胺和重组的人源H1受体结合，Ki = 43.2 nM。
2. WO 2014110000标题: Pyrido- or pyrrolo-fused pyrimidine derivatives as autotaxin inhibitors for treating pain
申请人: 礼来
优先权日期及相关专利公开号: 2013 US 777201
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: 疼痛
专利摘要: The present invention provides compounds of the Formula I: [Formula should be inserted here] wherein X is a bond or CH2; R is selected from the group consisting of [Formula should be inserted here] R1 and R2 are each independently selected from the group consisting of CH and N; R3 is H or CH3; R4 is H or CH3; L is selected from the group consisting of -0(CH2)3-, -C(0)NH(CH2)2-, -CH2C(0)NH(CH2)2-, -(CH2)3N(C(0)CH3)CH2-, -(CH2)2N(C(0)CH3)CH2-, -(CH2)3NH-, (CH2)2OCH2-, -(CH2)4-, -(CH2)2NHCH2-, -(CH2)30-, and -CH20(CH2)2-; pharmaceutically acceptable salt thereof. Compounds of this invention are autotaxin inhibitors.
备注: ENPP2（autotaxin)抑制剂可以治疗疼痛。本发明的化合物可以抑制重组的人源autotaxin，IC50小于1.7 nM。。
3. WO 2014110298标题: 5-Membered heteroaryls and their use as antiviral agents
申请人: 吉利德
优先权日期及相关专利公开号: 2013 US 750762
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: Compounds of formula (I): or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.
备注: 本发明的化合物可以治疗HIV感染，其对HIV-IIIb感染的T细胞MT-4展示了良好的抗病毒活性，在6mcM时，抑制率达到121%，同时对MT-4细胞也未显示毒性(CC50 > 47114 nM)。
4. WO 2014110296标题: Therapeutic compounds for the treatment of viral infections
申请人: 吉利德
优先权日期及相关专利公开号: 2013 US 750759
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: Compounds of formula I or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.
备注: 本发明的化合物可以治疗HIV感染，其对HIV-IIIb感染的T细胞MT-4展示了良好的抗病毒活性，在2mcM时，抑制率达到102.9%，同时对MT-4细胞也未显示毒性(CC50 > 50.3 mcM)。
5. WO 2014110297标题: (Hetero) arylacetamide derivatives as antiretroviral agents
申请人: 吉利德
优先权日期及相关专利公开号: 2013 US 750763
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: Compounds of formula (I): or pharmaceutically acceptable salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.
备注: 本发明的化合物可以治疗HIV感染，其对HIV-IIIb感染的T细胞MT-4展示了良好的抗病毒活性，在3 mcM时，抑制率达到91%，同时对MT-4细胞也未显示毒性(CC50 > 49982 nM)。
6. WO 2014108168标题: Piperidinylcarbazole as antimalarial
申请人: 默克
优先权日期及相关专利公开号: 2013 EP 150827
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: 疟疾
专利摘要: The present invention provides compounds of Formula (I) for the treatment of parasitic diseases including malaria, as well as neurodegenerative diseases. Formula (I) wherein R3, R4, X and Y have the meaning given in claim 1.
备注: 本发明的化合物可以治疗寄生虫感染，如疟疾，且可以治疗神经退行性疾病、癫痫、贫血、心血管障碍和肝炎。该化合物可以抑制恶性疟原虫K1和NF54的增殖，IC50 分别为10和40.16 nM。
7. WO 2014108452标题: Proteolysis targeting chimeras (PROTACs) directed to the modulation of the estrogen receptor
申请人: 葛兰素史克
优先权日期及相关专利公开号: 2013 US 751290
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: 乳腺癌
专利摘要: A compound of formula (I): or a pharmaceutically acceptable salt thereof, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of the estrogen receptor, including degrading the estrogen receptor, the treatment of diseases and conditions mediated by the estrogen receptor.
备注: PROTAC分子可以作为雌激素受体alpha调控剂和泛素蛋白配体E3诱导剂，因此可以用于治疗癌症，尤其是乳腺癌。1 mcM该化合物可以降解ER alpha。
8. WO 2014108858标题: Fatty acid synthase inhibitors
申请人: 葛兰素史克
优先权日期及相关专利公开号: 2013 US 750872
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: This invention relates to triazolones and triazolones for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of triazolones in the treatment of cancer.
备注: 脂肪酸合成酶FAS抑制剂可以治疗癌症。本发明的化合物可以抑制FAS的活性（IC50 20 nM），其在小鼠和大鼠的相关实验中，该化合物的清除率小于17 ml/min/kg 。
9. WO 2014110344标题: Meglumine salt forms of 2-((1R,4R)-4-(4-(5-(benzoxazol-2-ylamino)pyridin-2-yl)phenyl)cyclohexyl) acetic acid and their use as DGAT1 inhibitors
申请人: 诺华
优先权日期及相关专利公开号: 2013 US 751443
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，肥胖，血脂异常和乳糜微粒血
专利摘要: The present invention relates to novel crystalline forms of meglumine salts of 2-((1 R,4R)-4-(4-(5-(benzo[d]oxazol-2-ylamino)pyridin-2-yl) phenyl)cyclohexyl)acetic acid :Formule(I) and their use in the treatment or prevention of a condition or a disorder associated with DGATl activity in animals, particularly humans.
备注: DGAT-1抑制剂可以治疗II型糖尿病，肥胖，血脂异常和乳糜微粒血。一个修饰的葡甲胺盐在30 mg/kg p.o.时展示了17.3%的良好的口服生物利用度。
10. WO 2014110066标题: Macrocyclic benzofuran and azabenzofuran 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: 2013 US 750967
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: Compounds of formula I, including their salts, as well as compositions and methods of using the compounds are set forth. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
备注: NS5B抑制剂可以治疗HCV感染。本发明的化合物可以基因1b型的重组（EC50=0.0477 mcM）。
11. WO 2014110574标题: Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors
申请人: Incyte Corp.
优先权日期及相关专利公开号: 2013 US 791275
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 disclosure describes bicyclic aromatic carboxamide derivatives of formula (I), as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.
备注: Pim激酶抑制剂可以用于治疗癌症和免疫性疾病。本发明的化合物可以抑制Pim-1, Pim-2和Pim-3的活性（IC50小于100 nM)。
12. WO 2014108021标题: Fluorocyclobutanylimidazole compounds
申请人: TerraBay Pharmaceuticals, Inc.
优先权日期及相关专利公开号: 2013 CN 10006964
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: Provided are fluorocyclobutanylimidazole compounds of formula (I) and N-oxides, pharmaceutically acceptable salt or prodrugs thereof. Also provided are the preparation method thereof and intermediates useful in the preparation of the compounds. Also provided are a pharmaceutical composition containing the compounds and optionally at least one pharmaceutically acceptable excipient and the use thereof in the preparation of drugs for treating diseases relating to tyrosine kinase pathway disorders, especially cancers, wherein R1, R2, R3, R4, R5, R6, R7, m and n are as defined in the description.
备注: Abl抑制剂可以用于治疗癌症。本发明的化合物TEB-415可抑制Abl的活性，IC50=0.01003 mcM,且对EGFR, Jak2, PDGFR alpha和beta, Akt1和C-KIT具有选择性(IC50分别为= >100, 7.325, 0.1999, 19.90, 18.05 and 0.5118 mcM)。
13. WO 2014110103标题: Biphenyl-ethyl-pyrrolidine derivatives as histamine H3 receptor modulators for the treatment of cognitive disorders
申请人: Arena Pharmaceuticals, Inc.
优先权日期及相关专利公开号: 2013 US 750475
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: 瘙痒、过敏性鼻炎、认知障碍
专利摘要: The present invention relates to compounds of Formula (Ia) and pharmaceutically acceptable salts, solvates, and hydrates thereof, that modulate the activity of the histamine H3 receptor (Ia). Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of histamine H3-associated disorders.
备注: 组胺H3受体拮抗剂可以治疗瘙痒、过敏性鼻炎、认知障碍、抑郁、肥胖、睡眠障碍、精神障碍、疼痛、癫痫、脑损伤和注意力障碍等疾病。本发明的化合物对人源H3受体的IC50=2.5 nM。
14. WO 2014108820标题: Substituted 2-pyrazinone derivatives as kinase inhibitors
申请人: Aurigene Discovery Technologies Ltd.
优先权日期及相关专利公开号: 2013 IN 123
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、自身免疫疾病、炎症
专利摘要: The present invention provides novel substituted 2-pyrazinone derivatives of formula (1) as protein kinase inhibitors, in which R1; R2, R3, R4, R5, R6, R7 and ‘p’ have the meanings given in the specification, and pharmaceutically acceptable salts 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 kinase enzyme, more particularly BTK enzyme. The present invention also provides methods for synthesizing and administering the kinase inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the kinase inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
备注: BTK抑制剂可以治疗癌症、自身免疫疾病、炎症，如多发性硬化症、类风湿性关节炎等。本发明的化合物可以抑制重组的人源BTK活性，IC50小于等于0.7 mcM。
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