105772-13-2Relevant academic research and scientific papers
The Discovery of 3-((4-Chloro-3-methoxyphenyl)amino)-1-((3R,4S)-4-cyanotetrahydro-2H-pyran-3-yl)-1H-pyrazole-4-carboxamide, a Highly Ligand Efficient and Efficacious Janus Kinase 1 Selective Inhibitor with Favorable Pharmacokinetic Properties
Siu, Tony,Brubaker, Jason,Fuller, Peter,Torres, Luis,Zeng, Hongbo,Close, Joshua,Mampreian, Dawn M.,Shi, Feng,Liu, Duan,Fradera, Xavier,Johnson, Kevin,Bays, Nathan,Kadic, Elma,He, Fang,Goldenblatt, Peter,Shaffer, Lynsey,Patel, Sangita B.,Lesburg, Charles A.,Alpert, Carla,Dorosh, Lauren,Deshmukh, Sujal V.,Yu, Hongshi,Klappenbach, Joel,Elwood, Fiona,Dinsmore, Christopher J.,Fernandez, Rafael,Moy, Lily,Young, Jonathan R.
, p. 9676 - 9690 (2017)
The discovery of a potent selective low dose Janus kinase 1 (JAK1) inhibitor suitable for clinical evaluation is described. As part of an overall goal to minimize dose, we pursued a medicinal chemistry strategy focused on optimization of key parameters th
PROCESS FOR PREPARING 1-[(3R,4S)-4-CYANOTETRAHYDROPYRAN-3-YL]-3-[(2-FLUORO-6-METHOXY-4-PYRIDYL)AMINO]P YRAZOLE-4-CARBOXAMIDE
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Page/Page column 21-22, (2020/07/07)
The application relates to processes for the preparation of 1-[(3R,4S) -4-cyanotetrahydropyran-3-yl]-3-[(2-fluoro-6-methoxy-4-pyridyl) amino]pyrazole-4-carboxamide (I) which include (i) a synthesis for bromo and iodo pyridine intermediates, (ii) a synthesis of a pyrazole ester intermediate which can be obtained in enantiopure form and (iii) the combination of these intermediates into compound (I).
FACTOR XIIA INHIBITORS
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Paragraph 00339; 00340, (2019/10/19)
This invention relates to compoundsof formula (I)and methods of treatment using the compounds. The invention also relates to processes and methods for producing the compounds of the invention. The compounds of the invention are modulators of Factor XII (e.g. Factor XIIa). In particular, the compounds are inhibitors of Factor XIIa and may be useful as anticoagulants.
AMINOPYRAZOLES AS SELECTIVE JANUS KINASE INHIBITORS
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Page/Page column 20, (2018/07/05)
The instant invention provides compounds of formula I which are selective JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as atopic dermatitis, arthritis, and cancer.
AMINOPYRAZOLES AS JANUS KINASE INHIBITORS
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Page/Page column 21, (2018/07/05)
The instant invention provides compounds which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
N-(2-CYANO HETEROCYCLYL)PYRAZOLO PYRIDONES AS JANUS KINASE INHIBITORS
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Page/Page column 40, (2014/10/03)
Provided are compounds of Formula I, a JAK inhibitor, and use thereof for the treatment of JAK-mediated diseases by the application.
Facile entry to an efficient and practical enantioselective synthesis of a polycyclic cholesteryl ester transfer protein inhibitor
Han, Zhengxu S.,Xu, Yibo,Fandrick, Daniel R.,Rodriguez, Sonia,Li, Zhibin,Qu, Bo,Gonnella, Nina C.,Sanyal, Sanjit,Reeves, Jonathan T.,Ma, Shengli,Grinberg, Nelu,Haddad, Nizar,Krishnamurthy, Dhileep,Song, Jinhua J.,Yee, Nathan K.,Pfrengle, Waldemar,Ostermeier, Markus,Schnaubelt, Juergen,Leuter, Zeno,Steigmiller, Sonja,Daeubler, Juergen,Stehle, Emanuel,Neumann, Lukas,Trieselmann, Thomas,Tielmann, Patrick,Buba, Annette,Hamm, Rainer,Koch, Gunter,Renner, Svenja,Dehli, Juan R.,Schmelcher, Florian,Stange, Christian,MacK, Juergen,Soyka, Rainer,Senanayake, Chris H.
supporting information, p. 4142 - 4145 (2014/10/15)
An efficient enantioselective synthesis of the chiral polycyclic cholesteryl ester transfer protein (CETP) inhibitor 1 has been developed. The synthesis was rendered practical for large scale via the development of a modified Hantzsch-type reaction to prepare the sterically hindered pyridine ring, enantioselective hydrogenation of hindered ketone 6 utilizing novel BIBOP-amino-pyridine derived Ru complex, efficient ICl promoted lactone formation, and a BF3 mediated hydrogenation process for diastereoselective lactol reduction. This efficient route was successfully scaled to produce multikilogram quantities of challenging CETP drug candidate 1.
Highly enantioselective quinoline synthesis via ene-type cyclization of 1,7-enynes catalyzed by a cationic BINAP-palladium(II) complex
Hatano, Manabu,Mikami, Koichi
, p. 4704 - 4705 (2007/10/03)
The first highly enantioselective synthesis of a six-membered ring quinoline catalyzed by a cationic BINAP-palladium(II) complex is shown to afford the quinoline products having a quaternary carbon center or a spiro-ring in quantitative yield and >99% ee.
