33332-28-4Relevant articles and documents
Preparation technology of 2-bromo-3,5,6-trichloropyrazine
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Paragraph 0011-0013; 0021-0023; 0030-0032; 0040-0042; 0049, (2018/04/21)
The invention discloses a preparation technology of 2-bromo-3,5,6-trichloropyrazine. The preparation technology comprises the following steps of using 2,6-dichloropyrazine as an initiating raw material, and performing ammoniation, halogenation and Sandmeyer reaction, so as to obtain a target compound, namely 2-bromo-3,5,6-trichloropyrazine. The preparation technology has the advantages that by adopting the synthesis route, the obtaining of raw materials is easy, the cost is low, the operation is simple, the product can be easily separated, the selectivity is high, the yield is higher, the total yield can reach 62.7%, and the preparation technology is favorable for actual application.
PDE9 INHIBITORS FOR TREATMENT OF PERIPHERAL DISEASES
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Paragraph 00195; 00198-00199, (2018/09/25)
The present invention relates to PDE9 inhibitors, their synthesis, and their use for treatment of benign prostate hyperplasia, beta thalassemia, and sickle cell disease.
PDE9 INHIBITORS WITH IMIDAZO TRIAZINONE BACKBONE AND IMIDAZO PYRAZINONE BACKBONE FOR TREATMENT OF PERIPHERAL DISEASES
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Page/Page column 23; 24, (2017/02/09)
The present invention relates to PDE9 inhibitors and their use for treatment of benign prostate hyperplasia and sickle cell disease.
COMPOUNDS FOR USE IN ANTIBACTERIAL APPLICATIONS
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Paragraph 75; 133; 134, (2017/03/14)
The present invention relates to novel compounds or pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions and treatment methods or uses as antibacterials for bacterial infections.
PYRROLOTRIAZINES AS POTASSIUM ION CHANNEL INHIBITORS
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Page/Page column, (2014/09/29)
A compound of formula (I) wherein A, R1, R3, and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment of arrhythmia, maintaining normal sinus rhythm, IKur-associated disorders, and other disorders mediated by ion channel function.
5-(PYRIDIN-2-YL-AMINO)-PYRAZINE-2-CARBONITRILE COMPOUNDS AND THEIR THERAPEUTIC USE
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Page/Page column 67, 68, (2013/05/23)
The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain pyridyl-amino-pyrazine carbonitrile compounds that, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) aDNA damaging agent; (c) an antimetabolite or thymidylate synthase (TS) inhibitor; (d) a microtubule targeted agent; and (e) ionisin g radiation.
Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing
Reader, John C.,Matthews, Thomas P.,Klair, Suki,Cheung, Kwai-Ming J.,Scanlon, Jane,Proisy, Nicolas,Addison, Glynn,Ellard, John,Piton, Nelly,Taylor, Suzanne,Cherry, Michael,Fisher, Martin,Boxall, Kathy,Burns, Samantha,Walton, Michael I.,Westwood, Isaac M.,Hayes, Angela,Eve, Paul,Valenti, Melanie,De Haven Brandon, Alexis,Box, Gary,Van Montfort, Rob L. M.,Williams, David H.,Aherne, G. Wynne,Raynaud, Florence I.,Eccles, Suzanne A.,Garrett, Michelle D.,Collins, Ian
experimental part, p. 8328 - 8342 (2012/02/06)
Pyrazolopyridine inhibitors with low micromolar potency for CHK1 and good selectivity against CHK2 were previously identified by fragment-based screening. The optimization of the pyrazolopyridines to a series of potent and CHK1-selective isoquinolines demonstrates how fragment-growing and scaffold morphing strategies arising from a structure-based understanding of CHK1 inhibitor binding can be combined to successfully progress fragment-derived hit matter to compounds with activity in vivo. The challenges of improving CHK1 potency and selectivity, addressing synthetic tractability, and achieving novelty in the crowded kinase inhibitor chemical space were tackled by multiple scaffold morphing steps, which progressed through tricyclic pyrimido[2,3-b] azaindoles to N-(pyrazin-2-yl)pyrimidin-4-amines and ultimately to imidazo[4,5-c]pyridines and isoquinolines. A potent and highly selective isoquinoline CHK1 inhibitor (SAR-020106) was identified, which potentiated the efficacies of irinotecan and gemcitabine in SW620 human colon carcinoma xenografts in nude mice. (Figure presented)
PYRAZOLE COMPOUNDS
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Page/Page column 78-79, (2009/03/07)
The present invention is directed to compounds of Formula (I) and to pharmaceutically acceptable salts thereof, their synthesis, and their use as Raf inhibitors.
BICYCLYLARYL-ARYL-AMINE COMPOUNDS AND THEIR USE
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Page/Page column 88, (2009/10/18)
The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain bicyclylaryl-aryl-amines compounds of the following formula (referred to herein as BCAA compounds), which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation: (I).
Compounds derived from aryl carbamates, preparation thereof and uses of same
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Page/Page column 10-11, (2010/02/14)
The invention concerns novel compounds, preparation and uses of same, particularly therapeutic. More particularly, the invention concerns compounds derived from arylcarbamates, preparation and uses of same, particularly in the field of human or animal health. The inventive compounds are preferably ligands of serotoninergic 5-HT4 receptors, and can therefore be used in the therapeutic or prophylactic treatment of any disorder involving a 5-HT4 receptor. The invention also relates to pharmaceutical compositions comprising such compounds, preparation and uses thereof, and treatment methods using said compounds.
