公开(公告)号：US11708336B2

公开(公告)日：2023-07-25

申请号：US17066702

申请日：2020-10-09

申请人： MediBeacon Inc.

发明人： Thomas E. Rogers

IPC分类号： C07D487/14 ,  C07D241/28

CPC分类号： C07D241/28 ,  C07D487/14

摘要： A process for preparing pyrimido[4,5-g]pteridine-2,4,7,9-tetraol, or a salt thereof, is provided. A process for the preparation of 3,6-diaminopyrazine-2,5-dicarboxylic acid, or a salt thereof, from pyrimido[4,5-g]pteridine-2,4,7,9-tetraol, or a salt thereof, is further provided. A process for preparing a substituted pteridine compound, or a salt thereof, is further provided. A process for the preparation of a N-substituted 3,6-diaminopyrazine-2,5-dicarboxylic acid from a substituted pteridine compound, or a salt thereof, is further provided.

公开(公告)号：US20230192628A1

公开(公告)日：2023-06-22

申请号：US17614053

申请日：2020-05-27

申请人： SYNGENTA CROP PROTECTION AG

发明人： Mattia Riccardo MONACO ,  Stefano RENDINE ,  Mathias BLUM ,  Andrew EDMUNDS

IPC分类号： C07D241/28 ,  C07D403/12 ,  C07D401/12 ,  C07D417/12 ,  C07D405/12 ,  C07D471/04 ,  C07D401/14 ,  A01P3/00 ,  A01N43/60 ,  A01N47/00 ,  A01N43/80 ,  A01N43/90 ,  C07D417/14

CPC分类号： C07D241/28 ,  A01N43/60 ,  A01N43/80 ,  A01N43/90 ,  A01N47/00 ,  A01P3/00 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

摘要： Compounds of the formula (I) wherein the substituents are as defined in claim 1, useful as pesticides, and especially fungicides.

公开(公告)号：US11655214B2

公开(公告)日：2023-05-23

申请号：US16606410

申请日：2018-04-11

申请人： ELI LILLY AND COMPANY

发明人： Marta Maria Cifuentes-Garcia ,  Maria Cristina Garcia Paredes

IPC分类号： A61K31/167 ,  C07C233/01 ,  C07D213/82 ,  A61P35/00 ,  C07D241/28 ,  C07D487/04

CPC分类号： C07D213/82 ,  A61P35/00 ,  C07D241/28 ,  C07D487/04

摘要： The present invention provides phenyl-2-hydroxy-acetylamino-2-methyl-phenyl compounds, such as compounds of formula I:




pharmaceutical compositions comprising the compounds, and methods of using the compounds to treat physiological disorders such as pancreatic cancer.

公开(公告)号：US20180170922A1

公开(公告)日：2018-06-21

申请号：US15608630

申请日：2017-05-30

申请人： Vertex Pharmaceuticals Incorporated

发明人： Jean-Damien Charrier ,  Steven Durrant ,  David Kay ,  Ronald Knegtel ,  Somhairle MacCormick ,  Michael Mortimore ,  Michael O'Donnell ,  Joanne Pinder ,  Alistair Rutherford ,  Anisa Nizarali Virani ,  Stephen Young ,  Philip Michael Reaper

IPC分类号： C07D413/14 ,  C07D471/04 ,  C07D241/28 ,  C07D417/12 ,  C07D417/04 ,  C07D413/12 ,  C07D409/14 ,  C07D409/04 ,  C07D405/14 ,  C07D405/12 ,  C07D405/04 ,  C07D403/14 ,  C07D403/12 ,  C07D403/10 ,  C07D403/04 ,  C07D401/14 ,  C07D401/10 ,  C07D401/04 ,  C07D417/14

CPC分类号： C07D413/14 ,  A61P35/00 ,  C07D241/28 ,  C07D401/04 ,  C07D401/10 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

摘要： The present invention relates to pyrazine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.The compounds of this invention have formula I: wherein the variables are as defined herein.

公开(公告)号：US20180162838A1

公开(公告)日：2018-06-14

申请号：US15840339

申请日：2017-12-13

申请人： AstraZeneca AB

发明人： Susanne Elisabeth BERGLUND ,  Stephen CONNOLLY ,  Martin HEMMERLING ,  Nafizal HOSSAIN ,  Anna KRISTOFFERSSON ,  Johan Rune Michael LUNDKVIST ,  Grigorios NIKITIDIS ,  Lena Elisabeth RIPA ,  Igor SHAMOVSKY

IPC分类号： C07D401/12 ,  A61K31/4965 ,  A61K45/06 ,  C07D241/26 ,  A61K31/497

CPC分类号： C07D401/12 ,  A61K31/4965 ,  A61K31/497 ,  A61K45/06 ,  C07D241/26 ,  C07D241/28 ,  C07D405/14

摘要： The present invention provides a compound of a formula (I): or a pharmaceutically acceptable salt thereof; a process for preparing such a compound; and to the use of such a compound in the treatment of an ENaC mediated disease state (such as asthma, CF or COPD).

公开(公告)号：US20170253596A2

公开(公告)日：2017-09-07

申请号：US14772737

申请日：2014-02-27

申请人： Aquinox Pharmaceuticals (Canada) Inc.

发明人： Lloyd F. Mackenzie ,  Curtis Harwig ,  David Bogucki ,  Jeffery R. Raymond ,  Jeremy D. Pettigrew

IPC分类号： C07D473/34 ,  C07C215/42 ,  C07C233/23 ,  C07D207/335 ,  C07C311/04 ,  C07C225/10 ,  C07D207/06 ,  C07D213/38 ,  C07C233/74 ,  C07D231/12 ,  C07D249/08 ,  C07D233/60 ,  C07D209/08 ,  C07D317/46 ,  C07D295/096 ,  C07D213/64 ,  C07D239/34 ,  C07D241/18 ,  C07C255/31 ,  C07C275/24 ,  C07C279/08

CPC分类号： C07D473/34 ,  C07C35/21 ,  C07C35/32 ,  C07C59/46 ,  C07C62/32 ,  C07C215/42 ,  C07C215/50 ,  C07C215/52 ,  C07C225/10 ,  C07C233/18 ,  C07C233/23 ,  C07C233/60 ,  C07C233/74 ,  C07C235/30 ,  C07C235/44 ,  C07C235/46 ,  C07C235/48 ,  C07C255/31 ,  C07C261/04 ,  C07C275/10 ,  C07C275/24 ,  C07C275/34 ,  C07C279/08 ,  C07C291/04 ,  C07C311/04 ,  C07C335/10 ,  C07C2602/24 ,  C07C2603/14 ,  C07D207/06 ,  C07D207/08 ,  C07D207/335 ,  C07D207/416 ,  C07D209/08 ,  C07D213/04 ,  C07D213/30 ,  C07D213/36 ,  C07D213/38 ,  C07D213/64 ,  C07D213/81 ,  C07D213/82 ,  C07D231/12 ,  C07D233/60 ,  C07D233/72 ,  C07D235/06 ,  C07D235/14 ,  C07D239/34 ,  C07D241/18 ,  C07D241/28 ,  C07D249/08 ,  C07D295/096 ,  C07D307/68 ,  C07D317/46 ,  C07D317/58

摘要： Compounds of formula (I): where R1, R2, R3, R4a, R4b, R5, R6 and R7 are defined herein, or stereoisomers or pharmaceutically acceptable salts thereof, are described herein. Such compounds have activity as SHIP1 modulators, and thus may be used to treat any of a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of formula (I) in combination with a pharmaceutically acceptable carrier or diluent are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.

公开(公告)号：US20170174659A1

公开(公告)日：2017-06-22

申请号：US15118461

申请日：2015-02-13

申请人： Mark E. Adams ,  Jason W. Brown ,  Stephen Hitchcock ,  Maria Hopkins ,  Shota Kikuchi ,  Betty Lam ,  Holger Monenschein ,  Holly Reichard ,  Huikai Sun

发明人： Mark E. Adams ,  Jason W. Brown ,  Stephen Hitchcock ,  Maria Hopkins ,  Shota Kikuchi ,  Betty Lam ,  Holger Monenschein ,  Holly Reichard ,  Huikai Sun

IPC分类号： C07D401/14 ,  C07D401/04 ,  C07D241/28

CPC分类号： C07D401/14 ,  C07D241/26 ,  C07D241/28 ,  C07D401/04

摘要： The present invention provides compounds of formula I: which are useful as modulators of GPR6, pharmaceutical compositions thereof, methods for treatment of conditions associated with GPR6, processes for making the compounds and intermediates thereof.

公开(公告)号：US20170071919A1

公开(公告)日：2017-03-16

申请号：US15156528

申请日：2016-05-17

申请人： Urs BAETTIG ,  Kamlesh BALA ,  Emma BUDD ,  Lee EDWARDS ,  Catherine HOWSHAM ,  Glyn Alan HUGHES ,  Darren Mark LEGRAND ,  Katrin SPIEGEL

发明人： Urs BAETTIG ,  Kamlesh BALA ,  Emma BUDD ,  Lee EDWARDS ,  Catherine HOWSHAM ,  Glyn Alan HUGHES ,  Darren Mark LEGRAND ,  Katrin SPIEGEL

IPC分类号： A61K31/44 ,  C07D213/81 ,  C07D405/12 ,  A61K31/443 ,  A61K31/4545 ,  A61K31/5377 ,  C07D241/26 ,  A61K31/444 ,  A61K31/4439 ,  C07D413/04 ,  C07D413/12 ,  C07D403/12 ,  A61K31/497 ,  C07D401/04 ,  C07D405/04 ,  A61K45/06

CPC分类号： A61K31/44 ,  A61K31/4412 ,  A61K31/4418 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/5377 ,  A61K45/06 ,  C07D213/38 ,  C07D213/81 ,  C07D241/26 ,  C07D241/28 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D413/04 ,  C07D413/12

摘要： The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.

摘要翻译： 本发明提供吡啶和吡嗪衍生物，其恢复或增强突变和/或野生型CFTR的功能以治疗囊性纤维化，原发性纤毛运动障碍，慢性支气管炎，慢性阻塞性肺病，哮喘，呼吸道感染，肺癌，口干燥症和 角膜结膜炎或便秘（IBS，IBD，阿片样物质诱发）。 还包括包含这些衍生物的药物组合物。

公开(公告)号：US20160090376A1

公开(公告)日：2016-03-31

申请号：US14962242

申请日：2015-12-08

申请人： MediBeacon Inc.

发明人： Willliam L. Neumann ,  Raghavan Rajagopalan ,  Richard B. Dorshow

IPC分类号： C07D405/04 ,  C07D241/28 ,  C07D403/14 ,  A61K49/00 ,  C07D241/20 ,  C07D401/04 ,  C07D241/12 ,  C07D403/04 ,  C07D241/26

CPC分类号： C07D405/04 ,  A61K49/0021 ,  C07D241/12 ,  C07D241/20 ,  C07D241/24 ,  C07D241/26 ,  C07D241/28 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D409/04 ,  C07D409/06 ,  C07D409/10 ,  C07D409/14 ,  C07D413/04 ,  C07D417/04 ,  C07D473/18 ,  C07D473/34

摘要： The present invention relates to pyrazine derivatives capable of absorbing and emanating spectral energy in the visible and/or near infrared spectrum. Pyrazine derivatives of the invention may be administered to a patient in the form of a pharmaceutically acceptable composition and utilized in medical (e.g., diagnostic imaging) procedures.

摘要翻译： 本发明涉及能够吸收和发出可见光和/或近红外光谱中的光谱能量的吡嗪衍生物。 本发明的吡嗪衍生物可以以药学上可接受的组合物的形式施用于患者，并用于医学（例如，诊断成像）程序中。

公开(公告)号：US20160030424A1

公开(公告)日：2016-02-04

申请号：US14816432

申请日：2015-08-03

申请人： Vertex Pharmaceuticals Incorporated

发明人： John Robert Pollard ,  Philip Michael Reaper ,  Mohammed Asmal

IPC分类号： A61K31/496 ,  A61K31/55 ,  A61K33/24 ,  A61K45/06

CPC分类号： A61K31/496 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/55 ,  A61K33/24 ,  A61K45/06 ,  C07D241/28 ,  C07D413/04

摘要： The present invention relates to compounds useful as inhibitors of ATR protein kinase and combination therapies thereof. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.The compounds of this invention have formula I: wherein the variables are as defined herein.

摘要翻译： 本发明涉及可用作ATR蛋白激酶抑制剂的化合物及其组合疗法。 本发明还涉及包含本发明化合物的药学上可接受的组合物; 使用本发明化合物治疗各种疾病，病症和病症的方法; 制备本发明化合物的方法; 用于制备本发明化合物的中间体; 以及在体外应用中使用化合物的方法，如生物和病理现象中激酶的研究; 由这种激酶介导的细胞内信号转导途径的研究; 和新型激酶抑制剂的比较评估。 本发明的化合物具有式I：其中变量如本文所定义。