JP2020506171A5 - - Google Patents

Info

Publication number

JP2020506171A5

JP2020506171A5 JP2019537377A JP2019537377A JP2020506171A5 JP 2020506171 A5 JP2020506171 A5 JP 2020506171A5 JP 2019537377 A JP2019537377 A JP 2019537377A JP 2019537377 A JP2019537377 A JP 2019537377A JP 2020506171 A5 JP2020506171 A5 JP 2020506171A5

Authority

JP

Japan

Prior art keywords

fluoro

indole

methylsulfonyl

phenyl

amino

Prior art date

2018-01-16

Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)

Granted

Links

• Espacenet
• Global Dossier
• Discuss

• -1 3- (2-((2-fluoro-3- (methylsulfonyl) phenyl) amino) -5-methylpyrimidine-4-yl) -1H-indole-7-yl Chemical group 0.000 claims 58
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 22
• 150000001875 compounds Chemical class 0.000 claims 17
• QLNJFJADRCOGBJ-UHFFFAOYSA-N propionamide Chemical compound CCC(N)=O QLNJFJADRCOGBJ-UHFFFAOYSA-N 0.000 claims 12
• DNSISZSEWVHGLH-UHFFFAOYSA-N butanamide Chemical compound CCCC(N)=O DNSISZSEWVHGLH-UHFFFAOYSA-N 0.000 claims 9
• 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 9
• 150000003839 salts Chemical class 0.000 claims 8
• 239000001257 hydrogen Substances 0.000 claims 6
• 229910052739 hydrogen Inorganic materials 0.000 claims 6
• 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 6
• 229910052731 fluorine Inorganic materials 0.000 claims 5
• UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
• YNRIYIURWJWHMX-UHFFFAOYSA-N 2-(4-methylpiperazin-1-yl)propanamide Chemical compound NC(=O)C(C)N1CCN(C)CC1 YNRIYIURWJWHMX-UHFFFAOYSA-N 0.000 claims 3
• ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 3
• PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 3
• 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 3
• 229910052801 chlorine Inorganic materials 0.000 claims 3
• 239000000460 chlorine Substances 0.000 claims 3
• 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 3
• 239000011737 fluorine Substances 0.000 claims 3
• 239000008194 pharmaceutical composition Substances 0.000 claims 3
• 101000997835 Homo sapiens Tyrosine-protein kinase JAK1 Proteins 0.000 claims 2
• 102100033438 Tyrosine-protein kinase JAK1 Human genes 0.000 claims 2
• 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 claims 2
• 201000010099 disease Diseases 0.000 claims 2
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
• 125000001153 fluoro group Chemical group F* 0.000 claims 2
• 150000002431 hydrogen Chemical class 0.000 claims 2
• MAZZDWBGKGDHRC-NTKDMRAZSA-N (2R)-2-[(2R)-2,4-dimethylpiperazin-1-yl]-N-[3-[2-(2-fluoro-3-methylsulfonylanilino)-5-methylpyrimidin-4-yl]-1H-indol-7-yl]-3-methoxypropanamide Chemical compound COC[C@@H](N1CCN(C)C[C@H]1C)C(=O)Nc1cccc2c(c[nH]c12)-c1nc(Nc2cccc(c2F)S(C)(=O)=O)ncc1C MAZZDWBGKGDHRC-NTKDMRAZSA-N 0.000 claims 1
• MAZZDWBGKGDHRC-DVECYGJZSA-N (2S)-2-[(2R)-2,4-dimethylpiperazin-1-yl]-N-[3-[2-(2-fluoro-3-methylsulfonylanilino)-5-methylpyrimidin-4-yl]-1H-indol-7-yl]-3-methoxypropanamide Chemical compound COC[C@H](N1CCN(C)C[C@H]1C)C(=O)Nc1cccc2c(c[nH]c12)-c1nc(Nc2cccc(c2F)S(C)(=O)=O)ncc1C MAZZDWBGKGDHRC-DVECYGJZSA-N 0.000 claims 1
• 125000004195 4-methylpiperazin-1-yl group Chemical group [H]C([H])([H])N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 1
• 206010009900 Colitis ulcerative Diseases 0.000 claims 1
• 208000011231 Crohn disease Diseases 0.000 claims 1
• 206010012438 Dermatitis atopic Diseases 0.000 claims 1
• 201000004681 Psoriasis Diseases 0.000 claims 1
• 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
• 208000025865 Ulcer Diseases 0.000 claims 1
• 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
• 208000004631 alopecia areata Diseases 0.000 claims 1
• 208000006673 asthma Diseases 0.000 claims 1
• 201000008937 atopic dermatitis Diseases 0.000 claims 1
• 208000010928 autoimmune thyroid disease Diseases 0.000 claims 1
• 239000003085 diluting agent Substances 0.000 claims 1
• 201000006417 multiple sclerosis Diseases 0.000 claims 1
• 239000000546 pharmaceutical excipient Substances 0.000 claims 1
• 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
• 231100000397 ulcer Toxicity 0.000 claims 1