每周专利快讯：2014年9月（三）
本周共公开12篇专利。包括辉瑞公开2篇BACE1的专利；Allergan公开2篇S1P1受体的配体专利；拜耳公开用于治疗癌症的MNK1抑制剂专利；诺华公开了环前列腺素受体激动剂专利。1. WO 2014128093标题: Substituted-imidazopyridazines as MKNK1 inhibitors申请人: 拜耳优先权日期及相关专利公开号: 2013 EP 157935相关候选药物类型: 小分子药物相关候选药物化学结构:http://www.hfoom.com/file/uploads/2014/09/WO-2014128093.jpg适应症: 癌症专利摘要: The present invention relates to amido-substituted imidazopyridazine compounds of general formula (I): (Ia) (Ib) (Ic) (Id) in which A, Y, R1, R2, R3, R4 and n are as defined in the claims, 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。本发明的化合物可以抑制 MNK1 的活性( IC50=0.4~0.1 nM)。 2. WO 2014126746标题: Phenoxyethoxy compounds申请人: 礼来优先权日期及相关专利公开号: 2013 US 765057相关候选药物类型: 小分子药物相关候选药物化学结构:http://www.hfoom.com/file/uploads/2014/09/WO-2014126746.jpg适应症: 类风湿性关节炎、骨关节炎专利摘要: The present invention provides a compound of the Formula I: or a pharmaceutically acceptable salt thereof.备注: 前列腺素EP4受体拮抗剂可以治疗类风湿性关节炎、骨关节炎及与类风湿性关节炎和骨关节炎相关的疼痛。本发明的化合物可以 -PGE2与 EP4受体的结合(Ki = 0.45 nM)，同时对hEP1、hEP2 、hEP3受体具有选择性 (Ki > 17400, 261和> 12700 nM)。 3. US 2014228344标题: Alkene azetidine derivatives as sphingosine 1-phosphate (S1P) receptor modulators申请人: Allergan, Inc.优先权日期及相关专利公开号: 2014 US 174050相关候选药物类型: 小分子药物相关候选药物化学结构:http://www.hfoom.com/file/uploads/2014/09/US-2014228344.jpg适应症: 疼痛、眼疾、免疫疾病、过敏、炎症和癌症专利摘要: The present invention relates to alkene 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受体的配体可以用于治疗疼痛、眼疾、免疫疾病、过敏、炎症和癌症等疾病。本发明的化合物对S1P1的EC50为4.21 nM。 4. US 2014228445标题: Alkyne derivatives as sphingosine 1-phosphate (S1P) receptor modulators申请人: Allergan, Inc.优先权日期及相关专利公开号: 2013 US 763628相关候选药物类型: 小分子药物相关候选药物化学结构:http://www.hfoom.com/file/uploads/2014/09/US-2014228445.jpg适应症: 疼痛、眼疾、免疫疾病、过敏、炎症和癌症专利摘要: The present invention relates to alkyne derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.备注: S1P1受体的配体可以用于治疗疼痛、眼疾、免疫疾病、过敏、炎症和癌症等疾病。本发明的化合物对S1P1的EC50为3.27 nM。 5. WO 2014125426标题: Trisubstituted heterocyclic derivatives as ROR gamma modulators申请人: Aurigene Discovery Technologies Ltd.优先权日期及相关专利公开号: 2013 IN 674相关候选药物类型: 小分子药物相关候选药物化学结构:http://www.hfoom.com/file/uploads/2014/09/WO-2014125426.jpg适应症: 炎症和类风湿性关节炎、哮喘、慢性阻塞性肺病、1型糖尿病、多发性硬化症、肠炎、银屑病、系统红斑狼疮专利摘要: The present invention provides trisubstituted heterocyclic derivatives of formula (I), which may be therapeutically useful, more particularly as ROR? modulators; (I) in which R1, R2, R3, Ra, X, L, m and ring A have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorder, in particular their use in diseases or disorder where there is an advantage in modulating ROR? receptor. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the trisubstituted heterocyclic derivatives of formula (I) together with a pharmaceutically acceptable carrier, diluent or excipient therefor.备注: 维甲酸RORgamma受体的配体可以治疗炎症和类风湿性关节炎、哮喘、慢性阻塞性肺病、1型糖尿病、多发性硬化症、肠炎、银屑病、系统红斑狼疮等疾病。本发明的化合物可以抑制25--hydroxycholesterol与retinoid ROR gamma-LBD的结合(IC50 = 100.01-250 nM)。 6. US 2014228356标题: Heteroaryl-substituted hexahydropyranothiazin-2-amine compounds申请人: 辉瑞优先权日期及相关专利公开号: 2013 US 764185相关候选药物类型: 小分子药物相关候选药物化学结构:http://www.hfoom.com/file/uploads/2014/09/US-2014228356.jpg适应症: 阿尔兹海默型痴呆、2型糖尿病专利摘要: The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, and the variables R1 and R2 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.备注: BACE1抑制剂可作为Abeta产物的抑制剂，因此可以用于治疗阿尔兹海默和2型糖尿病。本发明的化合物可以抑制BACE1的活性（ IC50=0.0379 mcM）。 7. WO 2014125397标题: Substituted phenyl hexahydropyranothiazin-2-amine compounds申请人: 辉瑞优先权日期及相关专利公开号: 2013 US 765283相关候选药物类型: 小分子药物相关候选药物化学结构:http://www.hfoom.com/file/uploads/2014/09/WO-2014125397.jpg适应症: 阿尔兹海默型痴呆、2型糖尿病专利摘要: The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula (I), and the variables R1 and R2 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.备注: BACE1抑制剂可作为Abeta产物的抑制剂，因此可以用于治疗阿尔兹海默和2型糖尿病。本发明的化合物可以抑制BACE1的活性（ IC50=0.028 mcM）。 8. US 2014235634标题: Therapeutic compounds and uses thereof申请人: Kala Pharmaceuticals, Inc.优先权日期及相关专利公开号: 2013 US 765487相关候选药物类型: 小分子药物相关候选药物化学结构:http://www.hfoom.com/file/uploads/2014/09/US-2014235634.jpg适应症: 癌症、青光眼、视网膜病和黄斑变性专利摘要: Described herein are compounds of Formula (I) or Formula (VI), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I) or Formula (VI) and pharmaceutical compositions thereof that are mucus penetrating. Methods of using the compounds or pharmaceutical compositions hereof for treating diseases are also provided.备注: VEGFR-2 抑制剂可以治疗癌症、青光眼、视网膜病和黄斑变性。本发明的化合物可以抑制VEGFR-2。此外也具有良好的药代动力学性质： Cmax (retina) = 110 nM, Cmax (choroid) = 693 nM, AUC(0-last) (retina) = 915 h·nM and AUC(0-last) (choroid) = 5400 h·nM.。 9. WO 2014124757标题: Pyrrolotriazine derivatives as PI3K inhibitors申请人: Almirall, SA优先权日期及相关专利公开号: 2013 EP 382046相关候选药物类型: 小分子药物相关候选药物化学结构:http://www.hfoom.com/file/uploads/2014/09/WO-2014124757.jpg适应症: 癌症、自身免疫疾病、心血管疾病、神经系统疾病、过敏、炎症、病毒感染、疼痛、移植排异专利摘要: New pyrrolotriazine 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抑制剂可以治疗癌症、自身免疫疾病、心血管疾病、神经系统疾病、过敏、炎症、病毒感染、疼痛、移植排异等疾病。本发明的化合物可以抑制 PI3Kdelta的活性（IC50 =0.1 nM ）。 10. WO 2014125413标题: IP receptor agonist heterocyclic compounds申请人: 诺华优先权日期及相关专利公开号: 2013 US 764308相关候选药物类型: 小分子药物相关候选药物化学结构:http://www.hfoom.com/file/uploads/2014/09/WO-2014125413.jpg适应症: 肺动脉高压、哮喘、动脉粥样硬化、慢性阻塞性肺病、高血糖、高血压和炎症专利摘要: The present invention provides heterocyclic derivatives which activate the IP receptor. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients. Pharmaceutical compositions comprising such derivatives are also encompassed.备注: 环前列腺素受体激动剂可以治疗肺动脉高压、哮喘、动脉粥样硬化、慢性阻塞性肺病、纤维化、高血糖、高血压和炎症、血栓等疾病。本发明的化合物可以激活环前列腺素受体活性（EC50=0.000455 mcM）。 11. WO 2014125410标题: N-Substituted heterocyclic 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 599相关候选药物类型: 小分子药物相关候选药物化学结构:http://www.hfoom.com/file/uploads/2014/09/WO-2014125410.jpg适应症: 自身免疫疾病、癌症、炎症专利摘要: The present invention provides N-substituted novel heterocyclic derivatives of formula (I) as protein kinase inhibitors, in which R1, R2 and ‘n’ have the same 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、多种炎症，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BTK的活性（IC502 mcM ) 12. WO 2014124560标题: mGluR regulators申请人: Hua Medicine Ltd.优先权日期及相关专利公开号: 2013 CN 71644相关候选药物类型: 小分子药物相关候选药物化学结构:http://www.hfoom.com/file/uploads/2014/09/WO-2014124560.jpg适应症: 认知障碍、神经系统疾病、疼痛专利摘要: Provided herein are compounds of the formula I: (I), as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment or prevention of mGluR5 mediated disorders, such as acute and/or chronic neurological disorders, cognitive disorders and memory deficits, as well as acute and chronic pain.备注: mgluR5拮抗剂可以治疗神经系统疾病和疼痛。本发明的化合物可以拮抗mGluR5的活性 (IC50 = 500 nM）。我比较感兴趣的是专利11， BTK抑制剂，把这个作为本月作为调研的目标，不知道有没有愿意参与的~~ 非常好的东西！支持丁丁。
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