BR112020008893A2 - derivados de pirrolopirazina como inibidores de alfa v integrina - Google Patents

Info

Publication number

BR112020008893A2

BR112020008893A2 BR112020008893-5A BR112020008893A BR112020008893A2 BR 112020008893 A2 BR112020008893 A2 BR 112020008893A2 BR 112020008893 A BR112020008893 A BR 112020008893A BR 112020008893 A2 BR112020008893 A2 BR 112020008893A2

Authority

BR

Brazil

Prior art keywords

amino

hydrogen

mmol

lcms

nmr

Prior art date

2017-11-07

Links

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• 102000006495 integrins Human genes 0.000 title abstract description 28
• 108010044426 integrins Proteins 0.000 title abstract description 28
• 239000003112 inhibitor Substances 0.000 title description 17
• LJWZSXDLNMOUIP-UHFFFAOYSA-N N1C=CN=C2N=CC=C21 Chemical class N1C=CN=C2N=CC=C21 LJWZSXDLNMOUIP-UHFFFAOYSA-N 0.000 title description 2
• 238000000034 method Methods 0.000 claims abstract description 140
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• 206010052779 Transplant rejections Diseases 0.000 claims abstract description 3
• -1 guanidinyl Chemical group 0.000 claims description 203
• 229910052739 hydrogen Inorganic materials 0.000 claims description 33
• 239000001257 hydrogen Substances 0.000 claims description 33
• 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 32
• 125000000217 alkyl group Chemical group 0.000 claims description 23
• 125000003545 alkoxy group Chemical group 0.000 claims description 13
• 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims description 13
• 150000003839 salts Chemical class 0.000 claims description 12
• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 10
• VSWICNJIUPRZIK-UHFFFAOYSA-N 2-piperideine Chemical compound C1CNC=CC1 VSWICNJIUPRZIK-UHFFFAOYSA-N 0.000 claims description 9
• 208000027866 inflammatory disease Diseases 0.000 claims description 9
• 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims description 9
• 125000001424 substituent group Chemical group 0.000 claims description 9
• 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 8
• 125000004076 pyridyl group Chemical group 0.000 claims description 8
• 125000000753 cycloalkyl group Chemical group 0.000 claims description 7
• 125000004438 haloalkoxy group Chemical group 0.000 claims description 7
• 125000001188 haloalkyl group Chemical group 0.000 claims description 7
• 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 6
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• 125000000714 pyrimidinyl group Chemical group 0.000 claims description 6
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• 125000003373 pyrazinyl group Chemical group 0.000 claims description 4
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