- Triazolo pyridine compound and preparation method, medicinal composition and application thereof
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The invention discloses a triazolo pyridine compound as well as a preparation method, a medicinal composition and application thereof. The compound is selected from a compound shown in a general formula I, or a tautomer, an enantiomer, a diastereoisomer,
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Paragraph 0046; 0059-0061
(2020/05/08)
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- Discovery of triazolo [1,5-a] pyridine derivatives as novel JAK1/2 inhibitors
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Small molecule JAK inhibitors have been demonstrated efficacy in rheumatoid arthritis, inflammatory bowel disease, and psoriasis with the approval of several drugs. Aiming to develop potent JAK1/2 inhibitors, two series of triazolo [1,5-a] pyridine derivatives were designed and synthesized by various strategies. The pharmacological results identified the optimized compounds J-4 and J-6, which exerted high potency against JAK1/2, and selectivity over JAK3 in enzyme assays. Furthermore, J-4 and J-6 effectively suppressed proliferation of JAK1/2 high-expression BaF3 cells accompanied with acceptable metabolic stability in liver microsomes. Therefore, J-4 and J-6 might serve as promising JAK1/2 inhibitors for further investigation.
- Chen, Dawei,Jiang, Yuyang,Li, Anqi,Liu, Zijian,Lu, Kuan,Wu, Weibin,Xiao, Boren,Yuan, Zigao,Zhai, Xin,Zhang, Cunlong
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- COMPOUND AS SELECTIVE JAK INHIBITOR, AND SALT AND THERAPEUTIC USE THEREOF
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Disclosed are a compound as a selective JAK inhibitor, and an isomer, a solvate or a pharmaceutically acceptable salt thereof, wherein: the definitions of (A), R, R1 and n are described in detail in the specification. In addition, also disclose
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Paragraph 0040
(2019/06/12)
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- 1,2,4-Triazolo-[1,5-a]pyridine HIF Prolylhydroxylase Domain-1 (PHD-1) Inhibitors with a Novel Monodentate Binding Interaction
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Herein we describe the identification of 4-{[1,2,4]triazolo[1,5-a]pyridin-5-yl}benzonitrile-based inhibitors of the hypoxia-inducible factor prolylhydroxylase domain-1 (PHD-1) enzyme. These inhibitors were shown to possess a novel binding mode by X-ray crystallography, in which the triazolo N1 atom coordinates in a hitherto unreported monodentate interaction with the active site Fe2+ ion, while the benzonitrile group accepts a hydrogen-bonding interaction from the side chain residue of Asn315. Further optimization led to potent PHD-1 inhibitors with good physicochemical and pharmacokinetic properties.
- Ahmed, Saleh,Ayscough, Andrew,Barker, Greg R.,Canning, Hannah E.,Davenport, Richard,Downham, Robert,Harrison, David,Jenkins, Kerry,Kinsella, Natasha,Livermore, David G.,Wright, Susanne,Ivetac, Anthony D.,Skene, Robert,Wilkens, Steven J.,Webster, Natalie A.,Hendrick, Alan G.
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supporting information
p. 5663 - 5672
(2017/07/22)
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- METHODS FOR THE TREATMENT OF CARDIOVASCULAR DISORDERS
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The present invention discloses compounds according to Formula (I): or a pharmaceutically acceptable salt thereof, or a solvate or the salt of a solvate thereof, pharmaceutical compositions comprising the same, and methods of treatment using the same, for
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Paragraph 0163-0164
(2016/11/02)
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- PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF INFLAMMATORY DISORDERS
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The present invention discloses pharmaceutical compositions comprising: a compound according to Formula I: useful in the prophylaxis and/or treatment of inflammatory conditions, autoimmune diseases, proliferative diseases, allergy, transplant rejection, d
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Paragraph 0275
(2015/09/22)
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- NOVEL SALTS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF INFLAMMATORY DISORDERS
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The present invention discloses salts of a Compound 1: useful in the prophylaxis and/or treatment of inflammatory conditions, autoimmune diseases, proliferative diseases, allergy, transplant rejection, diseases involving degradation and/or disruption of
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Paragraph 0266; 0267
(2015/09/22)
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- FILGOTINIB: Tyrosine-protein kinase JAK1 inhibitor, treatment of rheumatoid arthritis, treatment of crohn's disease
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Rheumatoid arthritis (RA), a chronic autoimmune inflammatory disease, is associated with pain, progressive disability, systemic comorbidities and early death. Filgotinib (GLPG-0634), a new selective tyrosine-protein kinase (JAK1) inhibitor, is currently i
- Gras
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p. 547 - 551
(2014/12/11)
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- Triazolopyridines as selective JAK1 inhibitors: From hit identification to GLPG0634
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Janus kinases (JAK1, JAK2, JAK3, and TYK2) are involved in the signaling of multiple cytokines important in cellular function. Blockade of the JAK-STAT pathway with a small molecule has been shown to provide therapeutic immunomodulation. Having identified
- Menet, Christel J.,Fletcher, Stephen R.,Van Lommen, Guy,Geney, Raphael,Blanc, Javier,Smits, Koen,Jouannigot, Nolwenn,Deprez, Pierre,Van Der Aar, Ellen M.,Clement-Lacroix, Philippe,Lepescheux, Liên,Galien, René,Vayssiere, Béatrice,Nelles, Luc,Christophe, Thierry,Brys, Reginald,Uhring, Muriel,Ciesielski, Fabrice,Van Rompaey, Luc
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p. 9323 - 9342
(2015/01/09)
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- 2-Amino-[1,2,4]triazolo[1,5-a]pyridines as JAK2 inhibitors
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The advancement of a series of ligand efficient 2-amino-[1,2,4]triazolo[1, 5-a]pyridines, initially identified from high-throughput screening, to a JAK2 inhibitor with pharmacodynamic activity in a mouse xenograft model is disclosed.
- Siu, Michael,Pastor, Richard,Liu, Wendy,Barrett, Kathy,Berry, Megan,Blair, Wade S.,Chang, Christine,Chen, Jacob Z.,Eigenbrot, Charles,Ghilardi, Nico,Gibbons, Paul,He, Haiying,Hurley, Christopher A.,Kenny, Jane R.,Cyrus Khojasteh,Le, Hoa,Lee, Leslie,Lyssikatos, Joseph P.,Magnuson, Steve,Pulk, Rebecca,Tsui, Vickie,Ultsch, Mark,Xiao, Yisong,Zhu, Bing-Yan,Sampath, Deepak
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p. 5014 - 5021
(2013/09/02)
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- AMINOTRIAZOLOPYRIDINE FOR USE IN THE TREATMENT OF INFLAMMATION, AND PHARMACEUTICAL COMPOSITIONS THEREOF
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The present invention relates to the novel medical use of the compound according to Formula I, in particular in the treatment of inflammatory conditions, autoimmune diseases, proliferative diseases, allergy, transplant rejection, diseases involving impair
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Paragraph 00156; 00157
(2014/01/09)
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- TRIAZOLOPYRIDINES AS TYK2 INHIBITORS
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The present invention relates to compounds of Formula (I), wherein R1 to R6 have the meaning as cited in the description and the claims. Said compounds are useful as TYK2 inhibitors for the treatment or prophylaxis of immunological,
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Page/Page column 30
(2012/01/14)
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- NOVEL COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES
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[1,2,4]Triazolo[1,5-a]pyridine compounds are disclosed that have a Formula (I), represented by the following: These compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, diseases involving cartilage degradation, bone and/or joint degradation, for example osteoarthritis; and/or conditions involving inflammation or immune responses, such as Crohn's disease, rheumatoid arthritis, psoriasis, allergic airways disease (e.g. asthma, rhinitis), juvenile idiopathic arthritis, colitis, inflammatory bowel diseases, endotoxin-driven disease states (e.g. complications after bypass surgery or chronic endotoxin states contributing to e.g. chronic cardiac failure), diseases involving impairment of cartilage turnover (e.g. diseases involving the anabolic stimulation of chondrocytes), congenital cartilage malformations, diseases associated with hypersecretion of IL6 and transplantation rejection (e.g. organ transplant rejection) and proliferative diseases.
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Page/Page column 47; 48
(2010/04/03)
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- NOVEL COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES
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A novel [1,2,4]triazolo[1,5-a]pyridine compound is disclosed that has a formula represented by the following: This compound may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, diseases involving cartilage degradation, bone and/or joint degradation, for example osteoarthritis; and/or conditions involving inflammation or immune responses, such as Crohn''s disease, rheumatoid arthritis, psoriasis, allergic airways disease (e.g. asthma, rhinitis), juvenile idiopathic arthritis, colitis, inflammatory bowel diseases, endotoxin-driven disease states (e.g. complications after bypass surgery or chronic endotoxin states contributing to e.g. chronic cardiac failure), diseases involving impairment of cartilage turnover (e.g. diseases involving the anabolic stimulation of chondrocytes), congenital cartilage malformations, diseases associated with hypersecretion of IL6 and transplantation rejection (e.g. organ transplant rejection) and proliferative diseases.
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Page/Page column 21-22
(2010/03/02)
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- PREPARATION AND USES OF 1,2,4-TRIAZOLO [1,5a] PYRIDINE DERIVATIVES
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This application relates to compounds of the general Formula I and salts thereof, wherein X, R1A, R1B, R2, R3, R4, and R5 are as defined herein. The application also relates to compositions and methods of treatment of hyperproliferative diseases or disorders.
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Page/Page column 182
(2010/12/29)
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- NOVEL COMPOUND USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES
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A novel compound able to inhibit JAK is disclosed, this compound may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting exa
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Page/Page column 10
(2011/01/05)
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- INHIBITORS OF JAK2 KINASE
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Compounds inhibiting the bioactivity of the protein tyrosine kinase JAK2 are provided, along with methods of using the compounds in the treatment of malconditions wherein inhibition of JAK2 is medically indicated. Methods of preparation are also provided
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Page/Page column 27-28
(2009/03/07)
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- TRIAZOLOPYRIDINE JAK INHIBITOR COMPOUNDS AND METHODS
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A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined herein, are useful as JAK kinase inhibitors. A ph
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Page/Page column 92
(2010/01/12)
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- TRIAZOLOPYRIDINE COMPOUNDS AND THEIR USE AS ASK INHIBITORS
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The present invention relates to triazolopyridine compounds according to Formula (I), their use as medicament, for treating autoimmune disorders, inflammatorydiseases, cardiovascular disceases and/or neurodegenerative diseases and a process for their preparation.
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Page/Page column 55-56
(2009/04/25)
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