What is the GPLG0634?

GPLG0634 is , while it's Molecular Formula is C21H23N5O3S. GLPG-0634 (Filgotinib) is a potent, selective JAK1 inhibitor. Used as an anti-inflammatory agent, it reduces levels of inflammatory cytokines in the bones and tissue of mammals.

What is the CAS number for GPLG0634?

The CAS number of GPLG0634 is 1206161-97-8.

What is GPLG0634 (1206161-97-8) used for?

Filgotinib is a JAK1 inhibitor (IC50 = 10 nM). It is selective for JAK1 over JAK3 (IC50 = 810 nM) but also inhibits JAK2 and tyrosine kinase 2 (Tyk2; IC50s = 28 and 116 nM, respectively), as well as Abl, FLT1, -3, and -4, FMS, Mer, and TBK1 activity by greater than 35% in a panel of 177 tyrosine kinases at 1 μM. Filgotinib inhibits IL-6-induced phosphorylation of STAT1 in CD4+ T cells with an IC50 value of 629 nM in isolated human whole blood. It reduces hind paw macrophage and T cell infiltration and bone erosion in a rat model of collagen-induced arthritis when administered at doses ranging from 0.1 to 30 mg/kg per day for 15 days.

What is the GPLG0634?

GPLG0634 is , while it's Molecular Formula is C21H23N5O3S. GLPG-0634 (Filgotinib) is a potent, selective JAK1 inhibitor. Used as an anti-inflammatory agent, it reduces levels of inflammatory cytokines in the bones and tissue of mammals.

What is the CAS number for GPLG0634?

The CAS number of GPLG0634 is 1206161-97-8.

What is GPLG0634 (1206161-97-8) used for?

Filgotinib is a JAK1 inhibitor (IC50 = 10 nM). It is selective for JAK1 over JAK3 (IC50 = 810 nM) but also inhibits JAK2 and tyrosine kinase 2 (Tyk2; IC50s = 28 and 116 nM, respectively), as well as Abl, FLT1, -3, and -4, FMS, Mer, and TBK1 activity by greater than 35% in a panel of 177 tyrosine kinases at 1 μM. Filgotinib inhibits IL-6-induced phosphorylation of STAT1 in CD4+ T cells with an IC50 value of 629 nM in isolated human whole blood. It reduces hind paw macrophage and T cell infiltration and bone erosion in a rat model of collagen-induced arthritis when administered at doses ranging from 0.1 to 30 mg/kg per day for 15 days.

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NOVEL PROCESS FOR THE PREPARATION OF FILGOTINIB AND INTERMEDIATES THEREOF

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, (2020/10/20)

The present invention relates to a novel process for the preparation of filgotinib or a pharmaceutically acceptable salt and intermediates thereof which avoid Suzuki coupling reaction. (I)

Preparation method of filgotinib

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Paragraph 0088-0091, (2020/03/23)

A preparation method of filgotinib comprises the following steps: directly carrying out suzuki coupling on a compound of formula 1 and 4-formylphenylboronic acid, reacting the obtained reaction product with cyclopropylformylchloride to obtain a compound of formula 4, carrying out a reductive amination reaction on the compound of formula 4 and thiomorpholine 1,1-dioxide or its hydrochloride, and hydrolyzing the obtained reaction product to obtain the phenatinib product 9; or coupling the compound of formula 1 with cyclopropylformylchloride, reacting the obtained reaction product with 4-formylphenylboronic acid, and performing the reductive amination reaction on the obtained reaction product and thiomorpholine 1,1-dioxide to obtain the filgotinib product 9. The method widens the substrate range, increases the route efficiency, reduces the process cost, and achieves the effects of reducing the generation of byproducts and improving the purity of the final product by improving the crystallization property of intermediates in the route; and the route is simple to operate, the total yield is high, and the purity of the obtained product is high, so the method is suitable for large-scale production.

PROCESSES FOR THE PREPARATION OF FILGOTINIB

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, (2020/03/09)

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.

Synthesis method of JAK1 inhibitor Filgotinib

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, (2019/10/01)

The invention provides a preparing method of Filgotinib. The preparing method comprises the following steps that (1), 2-amino-6-bromopyridine reacts with a p-methylbenzene derivative to prepare a compound 1; (2), the compound 1 reacts with ethoxycarbonyl

[1,2,4]triazol[1,5-a]pyridine compound as well as preparation method and medical application thereof

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, (2018/03/24)

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

A Filgotinib synthetic method

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, (2017/08/25)

The invention discloses a filgotinib synthetic method and belongs to the technical field of chemical synthesis of medicines. 6-chloro-2-aminopyridine and di-tert-butyl dicarbonate ester are subjected to condensation reaction to obtain 6-chloro-2-tert-butyloxycarbonyl aminopyridine; hydrolysis reaction is performed; the obtained 6-chloro-2-tert-butyloxycarbonyl aminopyridine and trifluorinated methyl sulfonic anhydride are subjected to trifluoromethanesulfonic acid esterification reaction; the obtained 2-tert-butyloxycarbonylamino-6-pyridyltrifluoromethanesulfonate and [(1,1-dioxo-4-thiomorpholinyl)methyl]benzo-4-boronic acid pinacol ester are subjected to condensation reaction to obtain a tert-butyl ester derivative; the tert-butyl ester derivative is treated by trifluoroacetic acid and subjected to de-protection; the obtained intermediate and ethoxycarbonyl isothiocyanate are subjected to isothiocyanate reaction; the obtained intermediate and hydroxylamine hydrochloride are subjected to ring closing reaction; the obtained intermediate and cyclopropane carbonyl chloride are subjected to amidation reaction to obtain the finished product. Operation is simplified; reagents are available; the concept of environment friendliness and environment protection is embodied.

SOLID FORMS OF FILGOTINIB FREE BASE

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Page/Page column 29; 30, (2017/02/23)

The present invention relates to crystalline filgotinib free base, a method of its preparation and a pharmaceutical composition comprising the same.

CRYSTALLINE FILGOTINIB SULFONIC ACID ADDITION SALTS

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Page/Page column 33-34, (2017/02/09)

The present invention relates to filgotinib sulfonic acid addition salts, their polymorphs, a method of preparing the same as well as a pharmaceutical composition comprising the same.

METHODS FOR THE TREATMENT OF CARDIOVASCULAR DISORDERS

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, (2016/11/02)

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

PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF INFLAMMATORY DISORDERS

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, (2015/09/22)

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

Conditions	Yield
With 4-methyl-morpholine; In 1,4-dioxane; at 50 ℃; for 4h; Reagent/catalyst; Solvent; Temperature; Green chemistry;	91.2%
With triethylamine; at 5 - 20 ℃;

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Filgotinib | CAS 1206161-97-8

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