1.WO 2014053612

标题：Immunogenic composition

申请人：诺华

优先权日期及相关专利公开号：2013 US 799123 / 2012 US 744880 / 2013 EP 70656

疫苗

适应症：菌血症、脑膜炎、骨髓炎、肺炎、败血症

专利摘要：

The invention provides an immunogenic composition comprising: a) a conjugate that is a capsular saccharide from GBS serotype Ia conjugated to a carrier protein; b) a conjugate that is a capsular saccharide from GBS serotype Ib conjugated to a carrier protein; c) a conjugate that is a capsular saccharide from GBS serotype III conjugated to a carrier protein; d) a conjugate that is a capsular saccharide from GBS serotype II conjugated to a carrier protein; and e) a conjugate that is a capsular saccharide from GBS serotype V conjugated to a carrier protein.

备注：

专利提供的疫苗组成为来自B型链球菌血清V的糖荚膜与载体蛋白偶联。

2. WO 2014049488

标题：Benzamide and heterobenzamide compounds

申请人：辉瑞

优先权日期及相关专利公开号：2012 US 707447

适应症：癌症

专利摘要：

This invention relates to compounds of general formula (I), in which R1, R2, R6, U, V, W, X, Y and Z are as defined herein, and the pharmaceutically acceptable salts thereof, pharmaceutical compositions containing such compounds and salts, and to methods of using such compounds, salts and compositions.

备注：

组氨酸-赖氨酸N-甲基转移酶EZH2抑制剂已被证实对癌症有效。专利提供的示例化合物对野生型EZH2抑制活性为IC50 = 0.015 mcM

3. WO 2014048547

标题：alpha Hydroxy amides

申请人：默克

优先权日期及相关专利公开号：2012 EP 185835

适应症：溃疡性结肠炎

专利摘要：

The present invention relates to alpha hydroxy amides including compounds of formula (I) and related compounds and their use in the prophylaxis and treatment of inflammatory disorders and diseases, wherein T1, T2, W and Rw has the meaning given in claim 1.

备注：

血管非炎症分子1(vanin-1)抑制剂可用于治疗炎性疾病，如炎症性肠病，特别是溃疡性结肠炎。专利示例化合物对重组人类vanin-1分子的抑制活性为IC50 < 0.01 mcM。此外，对人类胰腺SUIT-2细胞中表达的vanin-1分子的抑制活性IC50 < 0.01 mcM。

4. WO 2014048532

标题：Quinazolinone derivatives as PARP inhibitors

申请人：默克

优先权日期及相关专利公开号：2012 EP 6707

适应症：动脉粥样硬化、癌症、炎症、大脑损伤、多发性硬化、关节炎、动脉再狭窄

专利摘要：

Compounds of the formula (I) in which R1, R2, R3, X1, X2 and Y have the meanings indicated in Claim 1, are inhibitors of Tankyrase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.

备注：

PARP-1、TNKS1和TNKS2抑制剂可用于治疗癌症、多发性硬化、心血管疾病、中枢神经系统损伤和炎症。本专利示例化合物对TNKS1、TNKS2、PARP-1的抑制活性均为IC50 < 0.3 mcM。

5. WO 2014048065

标题：Triazolyl derivatives as Syk inhibitors

申请人：默克弗罗斯特加拿大有限公司 & 默克

优先权日期及相关专利公开号：2012 US 707246

适应症：哮喘、癌症、慢性阻塞性肺病、风湿性关节炎

专利摘要：

Provided are triazole derivatives of Formula I which are potent inhibitors of spleen tyrosine kinase and pharmaceutical composition. The triazole derivatives are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.

备注：

SYK抑制剂可以用来治疗哮喘、慢性阻塞性肺病、癌症和风湿性关节炎。本专利示例化合物对SYK抑制活性达到IC50 = 0.1 nM。

6. WO 2014052566

标题：Novel compounds that are ERK inhibitors

申请人：默克

优先权日期及相关专利公开号：2012 US 707091

适应症：癌症

专利摘要：

Disclosed are the ERK inhibitors of formula (1.0), having a pyrazolopyridine base structure, and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds offormula (1.0).

备注：

ERK2抑制剂对癌症有效，特别是黑色素瘤和结直肠癌。本专利示例化合物对ERK2激酶抑制活性为IC50 = 0.3 nM。

7. WO 2014052563

标题：Novel compounds that are ERK inhibitors

申请人：默克

优先权日期及相关专利公开号：2012 US 707081

适应症：癌症

专利摘要：

Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1).

备注：

本专利示例化合物对ERK2激酶抑制活性为IC50 = 0.2 nM。

8. WO 2014052379

标题：Substituted cyclopropyl compounds

申请人：默克

优先权日期及相关专利公开号：2012 US 705850

适应症：糖尿病、肥胖

专利摘要：

Substituted cyclopropyl piperidinyl compounds and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-1 19. Pharmaceutical compositions and methods of treatment are also included.

备注：

葡萄糖依赖性促胰岛素受体(GDIR，GPR119)激动剂可以用于治疗糖尿病和肥胖。本专利示例化合物在LCMP测试中对HEK-293细胞转染的人类GPR119受体活性为EC50 = 0.25 nM。

9. WO 2014052188

标题：Toll-like receptor 3 antagonists for the treatment of metabolic and cardiovascular diseases

申请人：杨森生物技术

优先权日期及相关专利公开号：2012 US 628434

抗体

适应症：癌症、心血管失调、纤维变性、病毒感染、炎症、代谢性疾病、神经系统失调

专利摘要：

Toll Like Receptor 3 (TLR3) antibody antagonists, polynucleotides encoding TLR3 antibody antagonists or fragments thereof, and methods of making and using the foregoing are disclosed.

备注：

作用于TLR3的抗体或片段可用于治疗癌症、心血管失调、纤维变性、病毒感染、炎症、代谢性疾病、神经系统失调。专利提供了密码子优化的人类单克隆IgG4抗体的制备方法和表征。该抗体由突变的Fc区组成，能靶向人类TLR3。

10. WO 2014047390

标题：Tricyclic heterocyclic compounds as NOTCH inhibitors

申请人：Bristol-Myers Squibb

优先权日期及相关专利公开号：2012 US 703933

适应症：癌症

专利摘要：

Disclosed are compounds of Formula (I), wherein: X is O or -NR3; R1 is -CH2CH2CH3, -CH2CF3, -CH2CH2CF3, -CH2CF2CH3, -CH2CH2CH2CF3, -CH2CH2CF2CH3, -CH2CH(CH3)CF3, -CH2CH2CH2F, or CH2(cyclopropyl); R2 is -CH2CH2CH3, -CH2CF3, -CH2CH2CF3, -CH2CF2CH3, -CH2CH2CH2CF3, -CH2CH2CH2F, -CH2CH(CH3)CF3, CH2CH2CF2CH3, -CH2(cyclopropyl), -CH(CH3)(cyclopropyl), phenyl, fluorophenyl, chlorophenyl, trifluorophenyl, methylisoxazolyl, pyridinyl, formula (i), formula (ii), formula (iii), formula (iv) or formula (v); Ring A is phenyl or pyridinyl; and R3, Ra, Rb, Rc, y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer.

备注：

苯二氮作为Notch通路抑制剂对癌症治疗有效。示例化合物显示出对人子宫颈HeLa细胞中Notch1-CBF1和Notch3-CBF1转录活性的拮抗作用(IC50分别为10.5 nM和14.8 nM)。化合物在小鼠模型中显示出抗肿瘤活性。

11. WO 2014047374

标题：Alkyl, fluoroalkyl-1,4-benzodiazepinone compounds

申请人：Bristol-Myers Squibb

优先权日期及相关专利公开号： 2013 US 772583 / 2012 US 703917

适应症：癌症

专利摘要：

Disclosed are compounds of Formula (I) and/or salts thereof: (I) wherein: R1 is CH2CH2CF3; R2 is CH2(cyclopropyl), CH(CH3)(cyclopropyl), or CH2CH2CH3; R3 is H, CH3, or Rx; R4 is H or Ry; and Rx, Ry, Ra, Rb, Rc, y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer. The compounds of Formula (I) also include prodrugs of the Notch inhibitor compounds.

备注：

示例化合物对Notch1和Notch3的细胞活性为IC50分别为4.2 nM 和6.2 nM。化合物在动物模型中也显示出抗肿瘤活性。

12. WO 2014047370

标题：Fluoroalkyl dibenzodiazepinone compounds

申请人：Bristol-Myers Squibb

优先权日期及相关专利公开号：2012 US 703918

适应症：癌症

专利摘要：

Disclosed are compounds of Formula (I): wherein R1 is CH2CH2CF3 or CH2CH2CH3; R2 is CH2CH2CF3, CH2CH2CH3, CH2(cyclopropyl), phenyl, or; R3 is H; Ra, Rb, y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer.

备注：

示例化合物在细胞水平显示出对Notch1和Notch3的抑制活性，IC50分别为2.6nM和3.6nM。

13. US 2014088111/ WO 2014045156

标题：Novel bicyclic pyridinones

申请人：辉瑞

优先权日期及相关专利公开号：2012 US 703969/ 2013 US 31163

适应症：阿尔兹海默型老年痴呆

专利摘要：

Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

备注：

γ-分泌酶调节分子可作为β-淀粉酶(Abeta)抑制剂，对治疗神经变性的精神失调有效，例如阿尔兹海默病和C型尼曼匹克症。示例化合物在表达人类野生型APP前体蛋白的CHO细胞中能抑制Abeta(1-42)的产生，活性为IC50 = 3.34 nM。

14. WO 2014047393

标题：N-Substituted bis(fluoroalkyl)-1,4-benzodiazepinone compounds as NOTCH inhibitors

申请人：Bristol-Myers Squibb

优先权日期及相关专利公开号：2012 US 703922

适应症：癌症

专利摘要：

Disclosed are compounds of Formula (I): wherein: R1 is -CH2CH2CF3; R2 is -CH2CH2CF3, or -CH2CH2CH2CF3; R3 is -CH2CF3, -CH2CN, -CH2(cyclopropyl), pyridinyl, chloropyridinyl, or tetrahydropyranyl; Ring A is phenyl or pyridinyl; Ra, Rb, y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer.

备注：

示例化合物在表达人类Notch1和Notch3的人类宫颈HeLa细胞中的细胞活性为1.1 nM和2.6 nM。