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1. 发明申请

WO2022063153A1 BENZOTHIAZOLE AND QUINOLINE DERIVATIVES AND THEIR USE 审中-公开
公开(公告)号：WO2022063153A1
公开(公告)日：2022-03-31
申请号：PCT/CN2021/119802
申请日：2021-09-23
申请人： SHANGHAI YAO YUAN BIOTECHNOLOGY CO., LTD.
发明人： LIU, Danyang , XU, Cong , MELVIN, Lawrence S., Jr. , WEI, Xiong , LI, Tongruei Raymond , FAN, Jieqing , PAN, Yanfang , DANG, Huaixin , LICHENSTEIN, Henri , XU, Tian
IPC分类号： C07D277/82 , C07D417/02 , C07D215/38 , C07D401/12 , C07D217/06 , A61K31/428 , A61K31/47 , A61P35/00 , A61P37/00 , A61P25/00
摘要： Provided are compounds of Formula (I) or (II) and related compositions and methods for their use as inhibitors of alpha-kinase 1 (ALPK1).

2. 发明申请

WO2022036080A1 CONDENSED AZACYCLES AS SIGMA LIGAND COMPOUNDS AND USES THEREOF 审中-公开
公开(公告)号：WO2022036080A1
公开(公告)日：2022-02-17
申请号：PCT/US2021/045720
申请日：2021-08-12
申请人： MINERVA NEUROSCIENCES, INC.
发明人： LUTHRINGER, Remy , NOEL, Nadine , SCHMITT, Florent , WERNER, Sandra , MAAG, Hans , SAOUD, Jay
IPC分类号： A61P25/00 , A61P31/00 , C07D217/06 , C07D217/08 , C07D223/16 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D405/06 , C07D405/12 , C07D405/14 , C07D417/14 , A61K31/47
摘要： The present disclosure relates to compounds of Formula (I) and their prodrugs, solvates, pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods of their preparation. The compounds disclosed herein are useful for modulating Sigma receptors and have antiviral activity, and may also be useful in the treatment and/or prevention of pain disorders, neurological disorders (e.g., Parkinson's disease and Alzheimer's disease), and cancer.

3. 发明申请

WO2021245426A1 N-(PHENYLAMINOCARBONYL) TETRAHYDRO-ISOQUINOLINES AND RELATED COMPOUNDS AS MODULATORS OF GPR65 审中-公开
公开(公告)号：WO2021245426A1
公开(公告)日：2021-12-09
申请号：PCT/GB2021/051396
申请日：2021-06-04
申请人： PATHIOS THERAPEUTICS LIMITED
发明人： MCCARTHY, Tom , MILNE, Gavin , MOECHEL, Tobias , NAYLOR, Alan
IPC分类号： A61P9/10 , A61P11/06 , A61P35/00 , A61P37/02 , C07D217/02 , C07D217/24 , C07D413/04 , C07D471/04 , C07D487/04 , C07D487/14 , C07D498/04 , A61K31/47 , A61K31/5365 , A61K31/4738 , C07D217/06 , C07D409/04 , C07D471/14
摘要： The present invention relates to a compound of formula (Ia), or a pharmaceutically acceptable salt or solvate thereof, (I) wherein: ring A is a 5- or 6-membered monocyclic aromatic or heteroaromatic ring, or a 9- or 10-membered bicyclic aromatic or heteroaromatic ring, each of which is optionally substituted with one or more substituents selected from F, Cl, Br, I, CN, alkoxy, NR11R11', OH, SO2-alkyl, CO2-alkyl, alkyl, haloalkyl, aralkyl, aryl, and heteroaryl, and wherein said aryl and heteroaryl substituents are in turn optionally substituted with one or more substituents each independently selected from F, Cl, Br, I, CN, alkoxy, NR11R11', OH, alkyl, haloalkyl, and aralkyl; Y and Z are each independently CR10R10', wherein R10 and R10' are each independently selected from H, F, alkyl, and haloalkyl; R1, R4, and R5 are each independently selected from H, F, Cl, Br, I and haloalkyl; R2 and R3 are each independently selected from H, F, Cl, Br, I, CN, and haloalkyl; wherein at least two of R2, R3 and R4 are other than H; and R11 and R11' are each independently selected from H, alkyl, haloalkyl, COR12, and SO2R13, wherein R12 and R13 are both alkyl; wherein the compound is other than: N-(3,4-Dichlorophenyl)-7,8-dihydropyrido[4,3-d]pyrimidine-6(5H)-carboxamide; N-(3,4-Dichlorophenyl)-5,8-dihydropyrido[3,4-d]pyrimidine-7(6H)-carboxamide; N-(4-Chloro-3-(trifluoromethyl)phenyl)-3,4-dihydroisoquinoline-2(1H)-carboxamide; N-(3,4-dichlorophenyl)-3,4-dihydroisoquinoline-2(1H)-carboxamide; N-(3,4-Dichlorophenyl)-6,7-dihydroisoxazolo[4,5-c]pyridine-5(4H)-carboxamide; and N-(3,4-Dichlorophenyl)-4-methyl-6,7-dihydrothieno[3,2-c]pyridine-5(4H)-carboxamide. Further aspects of the invention relate to such compounds for use in the field of immunooncology, immunology, and related applications.

4. 发明申请

WO2021026179A1 AGONISTS OF ROR GAMMAt 审中-公开
公开(公告)号：WO2021026179A1
公开(公告)日：2021-02-11
申请号：PCT/US2020/044918
申请日：2020-08-05
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： HARIKRISHNAN, Lalgudi S. , PARK, Peter Kinam , RUAN, Zheming , WEI, Donna D. , O'MALLEY, Daniel , WAN, Honghe , PURANDARE, Ashok Vinayak , FINK, Brian E.
IPC分类号： C07D211/52 , A61K31/445 , A61P35/00 , C07D205/04 , C07D207/27 , C07D211/18 , C07D211/26 , C07D211/34 , C07D211/42 , C07D211/46 , C07D211/54 , C07D211/56 , C07D211/88 , C07D211/96 , C07D213/12 , C07D213/56 , C07D213/61 , C07D213/69 , C07D213/71 , C07D213/75 , C07D213/82 , C07D217/02 , C07D217/04 , C07D217/06 , C07D231/12 , C07D231/18 , C07D233/60 , C07D233/61 , C07D233/64 , C07D235/18 , C07D239/26 , C07D241/12 , C07D241/16 , C07D241/24 , C07D249/08 , C07D261/08 , C07D263/20 , C07D263/24 , C07D277/64 , C07D295/125 , C07D295/145 , C07D295/15 , C07D295/192 , C07D295/215 , C07D295/26 , C07D309/04 , C07D335/02 , C07D401/06 , C07D401/12 , C07D471/04 , C07D471/10 , C07D487/10
摘要： The present invention is directed to compounds of the formula (I) wherein all substituents are defined herein, as well as pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.

5. 发明申请

WO2019053607A1 PROCESS FOR PREPARATION OF LIFITEGRAST 审中-公开
公开(公告)号：WO2019053607A1
公开(公告)日：2019-03-21
申请号：PCT/IB2018/056959
申请日：2018-09-12
申请人： GLENMARK PHARMACEUTICALS LIMITED
发明人： NAIK, Samir , MISHRA, Sushanta , NARAYANAN, Suresh Babu , NAYKODI, Sachin Bhagwan , PARDESHI, Abhijit Ajaysinh , BHIRUD, Shekhar Bhaskar , NIMONKAR, Abhay Dhondiram
IPC分类号： C07D217/06 , C07D405/06
CPC分类号： C07D405/06 , C07D217/06
摘要： The present invention relates to a process for the preparation of lifitegrast, a compound of formula I, the process comprising deprotecting a compound of formula III using a Lewis acid. The present invention also relates to lifitegrast organic amine salt, a compound of formula II, process for its preparation and conversion thereof to lifitegrast.

6. 发明申请

WO2018167269A1 COMPOUNDS USEFUL IN THE TREATMENT OR PREVENTION OF A PRMT5-MEDIATED DISORDER 审中-公开
公开(公告)号：WO2018167269A1
公开(公告)日：2018-09-20
申请号：PCT/EP2018/056663
申请日：2018-03-16
申请人： ARGONAUT THERAPEUTICS LIMITED
发明人： MORLEY, Andrew , MILLER, Rebecca , LA THANGUE, Nicholas
IPC分类号： C07D401/14 , C07D405/14 , C07D217/04 , C07D217/06 , C07D401/12 , C07D409/12 , C07D409/14 , C07D417/12 , C07D491/18 , C07D495/04 , A61P35/00 , A61K31/4725 , A61K31/4365
摘要： The present disclosure relates to compounds suitable for the inhibition of protein arginine methyl-transferase (PRMT), in particular PRMT5. These compounds may be for use as therapeutic agents, in particular, agents for use in the treatment and/or prevention of proliferative diseases, such as cancer.

7. 发明申请

WO2016174496A1 P-GP RADIOTRACERS FOR IMAGING AS BIOMARKER INVOLVED IN ONSET OF NEURODEGENERATIVE DISEASES 审中-公开
标题翻译：用于成像生物标记物的P-GP放射线照相机参与神经干细胞移植疾病
公开(公告)号：WO2016174496A1
公开(公告)日：2016-11-03
申请号：PCT/IB2015/053046
申请日：2015-04-27
申请人： BIOFORDRUG S.R.L.
发明人： GHAFIR EL IDRISSI, Imane , CANTORE, Mariangela , BERARDI, Francesco , LEOPOLDO, Marcello , PERRONE, Roberto , COLABUFO, Nicola Antonio
IPC分类号： C07D217/04 , C07D217/06 , A61K31/472 , A61P25/28
CPC分类号： C07D217/04 , C07D217/06
摘要： The invention includes a new class of radiolabeled compounds of formula I able to bind P-glycoprotein with high affinity and selectivity. The protein prevents accumulation in the brain of a wide range of drugs and, changes in P-gp expression and function, are also believed to occur in several neurological disorder, such as Alzheimer's disease (AD). Indeed, it is widely reported that decreased expression of P- gp and/or activity at the BBB level could cause accumulation of I3- amyloid plaques, the main hallmark of AD onset. 13-amyloid is a P-gp substrate, and these results support the importance of P-gp in the clearance of 13-amyloid peptide from brain parenchyma. For this reason, P-gp can be considered a useful biomarker for the early diagnosis of neurodegeneration. There is considerable interest in the development of P-gp PET radiotracers for imaging expression and function of P-gp. Formula I wherein the compound is labeled with an isotope selected from H, 11 C 14 C, 13 N, 150 18 F 19 F, 75 Br, 76 Br, 79 Br.
摘要翻译：本发明包括能够以高亲和力和选择性结合P-糖蛋白的新一类式I的放射性标记化合物。蛋白质可以预防大量药物的脑部积聚，并且P-gp表达和功能的变化也被认为发生在几种神经障碍，如阿尔茨海默病（AD）。事实上，广泛报道的是，BBB水平的P- gp和/或活性的降低可能导致I3淀粉样斑块的积累，这是AD发病的主要标志。 13-淀粉样蛋白是P-gp底物，这些结果支持P-gp在来自脑实质的13-淀粉样蛋白肽清除中的重要性。因此，P-gp可被认为是神经退行性早期诊断的有用生物标志物。对P-gp PET放射性示踪剂的发展有相当的兴趣，用于成像表达和P-gp的功能。式I化合物用选自H，11C 14 C，13 N，150 18 F 19 F，75 Br，76 Br，79 Br的同位素标记。

8. 发明申请

WO2015064532A1 モルホリン化合物审中-公开
标题翻译：吗啉化合物
公开(公告)号：WO2015064532A1
公开(公告)日：2015-05-07
申请号：PCT/JP2014/078478
申请日：2014-10-27
申请人：第一三共株式会社
发明人：河村　明日香 , 杉山　大介 , 杉田　千絵 , 北澤　隆之 , 中村　毅
IPC分类号： C07D213/64 , A61K31/5377 , A61P7/00 , A61P13/12 , C07D217/06 , C07D231/40 , C07D237/14 , C07D239/28 , C07D239/34 , C07D239/42 , C07D241/18 , C07D263/34 , C07D277/20 , C07D277/56 , C07D401/04 , C07D401/14 , C07D471/04
CPC分类号： C07D213/64 , C07D213/65 , C07D217/06 , C07D231/40 , C07D237/14 , C07D239/28 , C07D239/34 , C07D239/42 , C07D241/18 , C07D263/34 , C07D277/56 , C07D401/04 , C07D401/14 , C07D471/04
摘要：課題は、高リン血症、又は、高リン血症に関連する疾患の予防又は治療すること。解決手段は、一般式（I）を有する化合物又はその薬理上許容される塩である。［式中、R 1 ：水素原子等、R 2 ：水素原子等、A：単結合等、E：ベンゼン環等、G：水素原子等、X：CH等、Y：-C（＝O）-等を示す。］
摘要翻译：本发明的目的是预防或治疗与高磷酸血症相关的高磷血症或疾病。为了实现这一目的，提供了具有通式（I）的化合物或其药学上可接受的盐。 [式中，R 1表示氢原子等，R 2表示氢原子等，A表示单键等，E表示苯环等，G表示氢原子等， X表示CH等，Y表示-C（= O） - 等]

9. 发明申请

WO2012117421A1 HISTONE DEACETYLASE INHIBITORS 审中-公开
标题翻译： HISTONE脱乙酰酶抑制剂
公开(公告)号：WO2012117421A1
公开(公告)日：2012-09-07
申请号：PCT/IN2012/000147
申请日：2012-03-01
申请人： ORCHID RESEARCH LABORATORIES LTD , RAJAGOPAL, Sridharan , KILAMBI, Narasimhan , KACHHADIA, Virendra , RATHINASAMY, Suresh , BALASUBRAMANIAN, Gopalan , MANI, Umamaheswari , RAJAGOPALAN, Nirmala , PUSHPARAJ, Judy Auxcilia , ROY, Anshu Mittal , VISHWAKARMA, Lolaknath Santosh , NARAYANAN, Shridhar , KALIYAMOORTHY, Vadivel , THANASEKARAN, Ponpandian , THATAVARTHY KRISHNA, Rama , KANNAN, Kalaivani , KULATHINGAL, Jayanarayan , MOOKKAN, Jeyamurugan , CHIDAMBARAM VENKATESWARAN, Srinivasan , AHAMED ALI, Fakrudeen
发明人： RAJAGOPAL, Sridharan , KILAMBI, Narasimhan , KACHHADIA, Virendra , RATHINASAMY, Suresh , BALASUBRAMANIAN, Gopalan , MANI, Umamaheswari , RAJAGOPALAN, Nirmala , PUSHPARAJ, Judy Auxcilia , ROY, Anshu Mittal , VISHWAKARMA, Lolaknath Santosh , NARAYANAN, Shridhar , KALIYAMOORTHY, Vadivel , THANASEKARAN, Ponpandian , THATAVARTHY KRISHNA, Rama , KANNAN, Kalaivani , KULATHINGAL, Jayanarayan , MOOKKAN, Jeyamurugan , CHIDAMBARAM VENKATESWARAN, Srinivasan , AHAMED ALI, Fakrudeen
IPC分类号： A61K31/404 , A61K31/435 , A61K31/436 , A61K31/4365 , A61K31/472 , A61K31/4725 , A61K31/506 , A61K31/55 , C07D217/06 , C07D495/04 , C07D401/06 , C07D209/08 , C07D223/16 , C07D409/06 , C07D491/04
CPC分类号： C07D409/06 , A61K31/404 , A61K31/435 , A61K31/436 , A61K31/4365 , A61K31/472 , A61K31/4725 , A61K31/506 , A61K31/55 , A61K45/06 , C07D209/08 , C07D217/04 , C07D217/06 , C07D223/16 , C07D401/04 , C07D401/06 , C07D403/04 , C07D405/14 , C07D409/14 , C07D495/04 , C07D498/04 , Y02A50/411 , A61K2300/00
摘要： Provided herein are isoform selective histone deacetylase inhibitors of the formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, metabolites, prodrugs, solvates, pharmaceutically acceptable salts and compositions thereof. These compounds are isoform selective inhibitors of HDACs and are useful as a therapeutic or ameliorating agent for diseases that are involved in cellular growth such as cancer, malignant tumors, autoimmune diseases, skin diseases, fungal infections, protozoal infections, HIV, inflammation and CNS disorders.
摘要翻译：本文提供式（I）的同工型选择性组蛋白脱乙酰酶抑制剂，其衍生物，类似物，互变异构形式，立体异构体，多晶型物，水合物，代谢物，前药，溶剂化物，药学上可接受的盐和组合物。这些化合物是HDAC的同种型选择性抑制剂，可用作涉及细胞生长的疾病如癌症，恶性肿瘤，自身免疫疾病，皮肤病，真菌感染，原生动物感染，HIV，炎症和CNS疾病的治疗或改善剂。

10. 发明申请

WO2012105588A1 テトラヒドロイソキノリン誘導体审中-公开
标题翻译：四氢喹啉衍生物
公开(公告)号：WO2012105588A1
公开(公告)日：2012-08-09
申请号：PCT/JP2012/052213
申请日：2012-02-01
申请人：アステラス製薬株式会社 , ▲はま▼口渉 , 木野山功 , 小金丸陽平 , 宮▲ざき▼ 壮宏 , 金子統 , 関岡竜一 , 鷲尾卓哉
发明人： ▲はま▼口　渉 , 木野山　功 , 小金丸　陽平 , 宮▲ざき▼　壮宏 , 金子　統 , 関岡　竜一 , 鷲尾　卓哉
IPC分类号： C07D209/44 , A61K31/4035 , A61K31/472 , A61K31/4725 , A61K31/4747 , A61K31/55 , A61P25/00 , A61P25/18 , A61P25/28 , A61P43/00 , C07D217/06 , C07D217/22 , C07D217/24 , C07D221/20 , C07D223/16 , C07D401/04
CPC分类号： C07D209/44 , A61K31/4035 , A61K31/472 , A61K31/4725 , A61K31/4747 , A61K31/55 , C07D217/06 , C07D217/22 , C07D217/24 , C07D221/20 , C07D223/16 , C07D401/04
摘要：【課題】セロトニン5-HT 5A 受容体調節作用に基づく、認知症及び統合失調症の、優れた予防または治療剤を提供すること。【解決手段】テトラヒドロイソキノリン環等のN原子にアシルグアニジノ基が結合し、不飽和の環に環基が結合した構造を特徴とするテトラヒドロイソキノリン誘導体が、強力な5-HT 5A 受容体調節作用と、これに基づく優れた薬理作用を有することを見い出し、認知症、統合失調症等の予防又は治療剤として有用であることを知見して、本発明を完成した。
摘要翻译： [问题]提供用于预防或治疗痴呆和精神分裂症的特殊药剂，所述药剂基于5-羟色胺5-HT5A受体调节作用。 [解决方案]本发明人发现，通过发现以四氢异喹啉环的N原子结合酰基胍基为结构的四氢异喹啉衍生物和环状基团与不饱和环结合的四氢异喹啉衍生物具有强大的5 -HT5A受体调节作用以及基于其的特殊药理作用; 并知道四氢异喹啉衍生物可用作预防或治疗痴呆，精神分裂症等病症的药剂。

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