EA032844B1 - Трициклические соединения бензоксаборола и их применение - Google Patents

Info

Publication number

EA032844B1

EA032844B1 EA201690135A EA201690135A EA032844B1 EA 032844 B1 EA032844 B1 EA 032844B1 EA 201690135 A EA201690135 A EA 201690135A EA 201690135 A EA201690135 A EA 201690135A EA 032844 B1 EA032844 B1 EA 032844B1

Authority

EA

Eurasian Patent Office

Prior art keywords

mycobacterium

compound

tuberculosis

pharmaceutically acceptable

dihydro

Prior art date

2013-08-09

Links

• Espacenet
• Global Dossier
• Discuss

• GDMJXXLVTYSBBE-UHFFFAOYSA-N 1,2-benzoxaborole Chemical class C1=CC=C2OB=CC2=C1 GDMJXXLVTYSBBE-UHFFFAOYSA-N 0.000 title description 73
• 150000001875 compounds Chemical class 0.000 claims abstract description 239
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• 239000003814 drug Substances 0.000 claims abstract description 78
• 150000003839 salts Chemical class 0.000 claims abstract description 76
• 229940124597 therapeutic agent Drugs 0.000 claims abstract description 56
• 238000000034 method Methods 0.000 claims abstract description 48
• 125000001246 bromo group Chemical group Br* 0.000 claims abstract description 46
• 238000011282 treatment Methods 0.000 claims abstract description 46
• 125000001309 chloro group Chemical group Cl* 0.000 claims abstract description 43
• 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 40
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• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 32
• 208000027531 mycobacterial infectious disease Diseases 0.000 claims abstract description 28
• 206010062207 Mycobacterial infection Diseases 0.000 claims abstract description 26
• 241000124008 Mammalia Species 0.000 claims abstract description 20
• 230000002401 inhibitory effect Effects 0.000 claims abstract description 19
• 230000010076 replication Effects 0.000 claims abstract description 15
• 230000002147 killing effect Effects 0.000 claims abstract description 7
• 230000000798 anti-retroviral effect Effects 0.000 claims abstract description 5
• QRXWMOHMRWLFEY-UHFFFAOYSA-N isoniazide Chemical compound NNC(=O)C1=CC=NC=C1 QRXWMOHMRWLFEY-UHFFFAOYSA-N 0.000 claims description 114
• 229960003350 isoniazid Drugs 0.000 claims description 112
• -1 Sch-D Chemical compound 0.000 claims description 99
• 125000003112 azulen-2-yl group Chemical group [H]C1=C2C([H])=C([H])C([H])=C([H])C([H])=C2C([H])=C1* 0.000 claims description 58
• 241000186359 Mycobacterium Species 0.000 claims description 49
• JQXXHWHPUNPDRT-WLSIYKJHSA-N rifampicin Chemical compound O([C@](C1=O)(C)O/C=C/[C@@H]([C@H]([C@@H](OC(C)=O)[C@H](C)[C@H](O)[C@H](C)[C@@H](O)[C@@H](C)\C=C\C=C(C)/C(=O)NC=2C(O)=C3C([O-])=C4C)C)OC)C4=C1C3=C(O)C=2\C=N\N1CC[NH+](C)CC1 JQXXHWHPUNPDRT-WLSIYKJHSA-N 0.000 claims description 37
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• AEUTYOVWOVBAKS-UWVGGRQHSA-N ethambutol Chemical compound CC[C@@H](CO)NCCN[C@@H](CC)CO AEUTYOVWOVBAKS-UWVGGRQHSA-N 0.000 claims description 21
• 241001465754 Metazoa Species 0.000 claims description 20
• BAVYZALUXZFZLV-UHFFFAOYSA-N Methylamine Chemical compound NC BAVYZALUXZFZLV-UHFFFAOYSA-N 0.000 claims description 17
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