919363-09-0Relevant articles and documents
Development of a Scalable and Practical Synthesis of AB928, a Dual A2a/A2bReceptor Antagonist
Debien, Laurent P. P.,Jeffrey, Jenna L.,Leleti, Manmohan R.,Miles, Dillon H.,Powers, Jay P.,Rosen, Brandon R.,Sharif, Ehesan U.
, p. 1254 - 1261 (2020/08/14)
AB928 is a potent and selective dual antagonist of the A2a and A2b receptors, which is currently in clinical trials. Here, we report the development of two scalable and practical syntheses of AB928. The first-generation synthesis was used to successfully
PROCESSES FOR PREPARING AMINOPYRIMIDINE COMPOUNDS
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Paragraph 0079, (2020/12/29)
Provided herein are improved processes for preparing aminopyrimidine compounds of Formula (I). The disclosed processes advantageously proceed through a β-diketoester intermediate of Formula (A) and avoid the direct linking of a pyrimidine and phenyl moiet
As opioid receptor antagonists or inverse agonists of the novel compounds
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Paragraph 0335-0337; 0338-0340, (2016/10/08)
Novel compounds which are antagonists or inverse agonists at one or more of the opioid receptors, pharmaceutical compositions containing them, to processes for their preparation.
DIFLUOROMETHYLENE COMPOUND
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Paragraph 0505-0507, (2015/06/16)
The present invention relates to a compound having an URAT1 inhibitory activity, and to an URAT1 inhibitor, a blood uric acid level-reducing agent and a pharmaceutical composition containing the compound. More specifically, the present invention relates to a compound represented by the formula (I): wherein R1 is -Q1-A1 or the like; R2 is a hydrogen atom, a halogen atom, a lower alkyl group or the like; W1, W2, W3 and W4 are each independently a nitrogen atom or a methine group optionally having substituents, or the like; X and Y are each a single bond, an oxygen atom or the like; Z is a hydroxyl group or COOR3 or the like.
NOVEL PKC INHIBITORS
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Page/Page column 46, (2012/12/13)
The present invention relates to new kinase inhibitors, more specifically PKCθ inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular,
Synthesis and structure-activity relationships of novel benzoxaboroles as a new class of antimalarial agents
Zhang, Yong-Kang,Plattner, Jacob J.,Freund, Yvonne R.,Easom, Eric E.,Zhou, Yasheen,Gut, Jiri,Rosenthal, Philip J.,Waterson, David,Gamo, Francisco-Javier,Angulo-Barturen, Inigo,Ge, Min,Li, Zhiya,Li, Lingchao,Jian, Yong,Cui, Han,Wang, Hailong,Yang, Jian
, p. 644 - 651 (2011/03/18)
A series of boron-containing benzoxaborole compounds was designed and synthesized for a structure-activity relationship investigation surrounding 7-(HOOCCH2CH2)-1,3-dihydro-1-hydroxy-2,1-benzoxaborole (1) with the goal of discovering
DUAL PHARMACOPHORES - PDE4-MUSCARINIC ANTAGONISTICS
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, (2009/10/09)
The present invention is directed to novel compounds of Formula's (I) - (VI), and pharmaceutically acceptable salts thereof, pharmaceutical compositions and their use in therapy, for example as inhibitors of phosphodiesterase type IV (PDE4) and as antagonists of muscarinic acetylcholine receptors (mAChRs), in the treatment of and/or prophylaxis of respiratory diseases, including inflammatory and/or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rhinitis (e.g. allergic rhinitis), atopic dermatitis or psoriasis.
Dual Pharmacophores - PDE4-Muscarinic Antagonistics
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Page/Page column 50, (2009/08/18)
The present invention is directed to novel compounds of Formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions and their use as dual chromaphores having inhibitory activity against PDE4 and muscarinic acetylcholine receptors (mAChRs), and thus being useful for treating respiratory diseases.
Dual Pharmacophores - PDE4-Muscarinic Antagonistics
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Page/Page column 52, (2009/08/16)
The present invention is directed to novel compounds of Formula (I), pharmaceutical compositions and their use in therapy, for example as inhibitors of phosphodiesterase type IV (PDE4) and as antagonists of muscarinic acetylcholine receptors (mAChRs), in the treatment of/and or prophylaxis of respiratory diseases, including antiinflammatory and/or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rhinitis (e.g. allergic rhinitis), atopic dermatitis or psoriasis.
Dual Pharmacophores - PDE4-Muscarinic Antagonistics
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Page/Page column 53, (2009/08/18)
The present invention relates to novel compounds of Formula (I) and their use in the treatment of respiratory diseases, including anti-inflammatory and allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rhinitis (e.g. allergic rhinitis), atopic dermatitis or psoriasis.