- PROCESSES FOR THE PREPARATION OF FILGOTINIB
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The present invention relates to processes for the preparation of Filgotinib. The present invention relates to novel processes for the preparation of filgotinib. The present invention also relates to novel intermediates for the preparation of filgotinib.
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Paragraph 0092-0093
(2020/03/09)
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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 0081; 0082
(2019/06/12)
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- Small molecule compound
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The invention provides a small molecular compound, The small molecular compound is characterized by having a structure as shown in the following molecular general formula, wherein X1 and X2 are selected from carbon or nitrogen, G1 is a carbon ring or a heterocyclic ring with aromaticity, any one or more hydrogen atoms on the G1 ring are substituted by R1, wherein R1 is selected from nitrogen-containing groups. The small molecule compound can be used as an efficient and specific JAK kinase inhibitor, especially a Tyk2 inhibitor, and/or a JAK1 inhibitor, and/or a JAK1/Tyk2 dual inhibitor, or a Tyk2/JAK1 dual inhibitor or a Tyk2/Jak2 dual inhibitor.
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- PYRROLO-AROMATIC HETEROCYCLIC COMPOUND, PREPARATION METHOD THEREFOR, AND MEDICAL USE THEREOF
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The present invention relates to pyrrolo-aromatic heterocyclic compounds, a preparation method therefor and medical use thereof. Particularly, the present invention relates to a compound represented by formula I, a preparation method therefor, a pharmaceu
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Paragraph 0221; 0222
(2019/11/11)
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- [1,2,4]triazol[1,5-a]pyridine compound as well as preparation method and medical application thereof
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The invention relates to a [1,2,4]triazol[1,5-a] pyridine compound as well as a preparation method and medical application thereof. Particularly, the invention relates to the compound shown in a general formula I, the preparation method of the compound, a
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Paragraph 0220-0221
(2018/03/24)
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- [1,2,4]triazol[1,5-a] pyridine compound as well as preparation method and medical application thereof
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The invention relates to a [1,2,4]triazol[1,5-a] pyridine compound as well as a preparation method and medical application thereof, in particular to a compound shown in a general formula I, a preparation method thereof, a pharmaceutical composition contai
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Paragraph 0164-0167
(2018/04/26)
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- Compounds used as JAK inhibitor, and use of compounds
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The invention provides compounds used as a JAK inhibitor, and a use of the compounds, and concretely provides compounds (represented by formula (I)) with JAK inhibition activity or a stereoisomer, a geometric isomer, a tautomer, a racemate, a nitrogen oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, and a medicinal composition including the compounds. The invention also discloses a use of the compounds or the medicinal composition thereof in the preparation of medicines used for treating autoimmune diseases or proliferative diseases.
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Paragraph 0509; 0510; 0511; 0512; 0513; 0515
(2017/08/27)
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- SUBSTITUTED IMIDAZO [1, 2-A] PYRIDIN-2-YLAMINE COMPOUNDS, AND PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE THEREOF
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Provided herein are substituted imidazo [1, 2-a] pyridin-2-ylamine compounds, for example, of formula (A), and pharmaceutical compositions thereof; and methods of their use for treating, preventing, or ameliorating one or more symptoms of a Janus kinase-m
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Paragraph 00313-00314
(2016/08/23)
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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 0162
(2016/11/02)
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- Anti-Malarial Agents
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The present invention relates to a novel class of quinolone-4-carboxamide Pf3D7 inhibitors of general formula (I) (Formula (I)) wherein R1, R2, R3, R4, R5, R6, R7, R8 and X are as defined herein, to their use in medicine, and in the treatment of malaria in particular, to compositions containing them, to processes for their preparation and to intermediates used in such processes.
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- INHIBITORS OF LYSINE METHYL TRANSFERASE
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There are disclosed compounds that are inhibitors of EZH2, pharmaceutical compositions containing said compounds and methods of treating hyperproliferative, inflammatory, infectious, and immunoregulatory disorders and diseases, utilizing the compounds of
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Page/Page column 58
(2015/06/08)
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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 0273-0274
(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 0264; 0265
(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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- ANTI-MALARIAL AGENTS
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The present invention relates to a novel class of quinolone-4-carboxamide Pf3D7 inhibitors of general formula (I) (Formula (I)) wherein R1, R2, R3, R4, R5, R6, R7, R8 and X are as defined herein, to their use in medicine, and in the treatment of malaria in particular, to compositions containing them, to processes for their preparation and to intermediates used in such processes.
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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 00160
(2014/01/09)
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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 13
(2011/01/05)
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- QUINOXALINE DERIVATIVES AS INHIBITORS OF THE TYROSINE KINASE ACTIVITY OF JANUS KINASES
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The present invention relates to quinoxaline compound of the formula (I): wherein R1 is carbocyclyl or heterocyclyl, either of which is optionally substituted with 1, 2, 3, 4 or 5 R7; R2 is carbocyclyl or heterocyclyl, either of which is optionally substituted with 1, 2, 3, 4 or 5 R8; R3, R4, R5 and R6 are each independently hydrogen or R9; and R7, R8 and R9 are each independently selected from organic and inorganic substituents, their use in therapy of diseases, in particular diseases mediated by the tyrosine kinase activity of Janus kinases, including JAK-2 and JAK-3 kinases
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Page/Page column 33
(2009/01/24)
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