CA3160522A1

CA3160522A1 - Compounds active towards nuclear receptors

Compounds active towards nuclear receptors Download PDF

Info

Publication number: CA3160522A1
Authority: CA; Canada
Prior art keywords: fluoro; methyl; amino; din; trifluoromethyl
Prior art date: 2019-12-20
Legal status : Pending

Application number

CA3160522A

Other languages

English (en)

French (fr)

Inventor

Sanne Schroder Glad

Ian SARVARY

Alex Haahr Gouliaev

Thomas Franch

Soren Jensby Nielsen

Luigi Piero Stasi

Current Assignee

Nuevolution AS

Original Assignee

Nuevolution AS

Priority date

2019-12-20

Filing date

2020-12-18

Publication date

2021-06-24

2020-12-18 Application filed by Nuevolution AS filed Critical Nuevolution AS

2021-06-24 Publication of CA3160522A1 publication Critical patent/CA3160522A1/en

Status Pending legal-status Critical Current

Links

150000001875 compounds Chemical class 0.000 title claims abstract description 273
108020005497 Nuclear hormone receptor Proteins 0.000 title abstract description 11
102000006255 nuclear receptors Human genes 0.000 title abstract description 11
108020004017 nuclear receptors Proteins 0.000 title abstract description 11
239000008194 pharmaceutical composition Substances 0.000 claims abstract description 46
DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims description 443
125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 336
-1 stereoisomer Chemical class 0.000 claims description 255
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 160
229910052739 hydrogen Inorganic materials 0.000 claims description 129
239000001257 hydrogen Substances 0.000 claims description 129
125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 claims description 120
125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims description 81
150000003839 salts Chemical class 0.000 claims description 81
239000000203 mixture Substances 0.000 claims description 77
150000002431 hydrogen Chemical group 0.000 claims description 73
125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 73
RWTNPBWLLIMQHL-UHFFFAOYSA-N fexofenadine Chemical group C1=CC(C(C)(C(O)=O)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 RWTNPBWLLIMQHL-UHFFFAOYSA-N 0.000 claims description 68
125000000217 alkyl group Chemical group 0.000 claims description 65
125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 57
125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 50
229910052736 halogen Inorganic materials 0.000 claims description 50
150000002367 halogens Chemical class 0.000 claims description 47
125000001153 fluoro group Chemical group F* 0.000 claims description 46
125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 43
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238000000034 method Methods 0.000 claims description 26
UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 21
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125000001188 haloalkyl group Chemical group 0.000 claims description 15
125000004438 haloalkoxy group Chemical group 0.000 claims description 14
125000002768 hydroxyalkyl group Chemical group 0.000 claims description 14
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