JP2011530593A5 - - Google Patents
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- Publication number
- JP2011530593A5 JP2011530593A5 JP2011522975A JP2011522975A JP2011530593A5 JP 2011530593 A5 JP2011530593 A5 JP 2011530593A5 JP 2011522975 A JP2011522975 A JP 2011522975A JP 2011522975 A JP2011522975 A JP 2011522975A JP 2011530593 A5 JP2011530593 A5 JP 2011530593A5
- Authority
- JP
- Japan
- Prior art keywords
- pyran
- dimethylpropyl
- phenanthro
- propano
- dodecahydro
- Prior art date
- 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
- -1 Unsaturated Chemical group 0.000 claims 90
- 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 claims 86
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 57
- 150000001875 compounds Chemical class 0.000 claims 54
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 44
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 41
- 239000002253 acid Substances 0.000 claims 34
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 34
- 229910052799 carbon Inorganic materials 0.000 claims 26
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 23
- 125000001424 substituent group Chemical group 0.000 claims 23
- 125000003118 aryl group Chemical group 0.000 claims 22
- 229910052757 nitrogen Inorganic materials 0.000 claims 22
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 21
- 229910052736 halogen Inorganic materials 0.000 claims 20
- 229910052760 oxygen Inorganic materials 0.000 claims 20
- 150000001735 carboxylic acids Chemical class 0.000 claims 19
- 150000002367 halogens Chemical class 0.000 claims 19
- 125000001072 heteroaryl group Chemical group 0.000 claims 19
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 18
- 239000005973 Carvone Substances 0.000 claims 17
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims 17
- 229910052739 hydrogen Inorganic materials 0.000 claims 16
- 125000000623 heterocyclic group Chemical group 0.000 claims 15
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 14
- MGADZUXDNSDTHW-UHFFFAOYSA-N 2H-pyran Chemical compound C1OC=CC=C1 MGADZUXDNSDTHW-UHFFFAOYSA-N 0.000 claims 13
- 125000005842 heteroatom Chemical group 0.000 claims 13
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 11
- 125000000217 alkyl group Chemical group 0.000 claims 10
- 125000000031 ethylamino group Chemical group [H]C([H])([H])C([H])([H])N([H])[*] 0.000 claims 10
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 10
- 229920006395 saturated elastomer Polymers 0.000 claims 10
- 229910052717 sulfur Inorganic materials 0.000 claims 9
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 7
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 7
- 125000004043 oxo group Chemical group O=* 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 7
- 125000006308 propyl amino group Chemical group 0.000 claims 6
- 206010017533 Fungal infection Diseases 0.000 claims 5
- 208000031888 Mycoses Diseases 0.000 claims 5
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 5
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 5
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 5
- 125000001624 naphthyl group Chemical group 0.000 claims 5
- 125000006432 1-methyl cyclopropyl group Chemical group [H]C([H])([H])C1(*)C([H])([H])C1([H])[H] 0.000 claims 4
- 125000004076 pyridyl group Chemical group 0.000 claims 4
- 125000004429 atom Chemical group 0.000 claims 3
- 125000006317 cyclopropyl amino group Chemical group 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- BODYFEUFKHPRCK-ZCZMVWJSSA-N ibrexafungerp Chemical compound N1([C@@H]2C[C@@]34COC[C@]([C@H]2OC[C@](C)(N)C(C)(C)C)(C)[C@@H]3CC[C@@H]2[C@@]3(C)CC[C@]([C@H]([C@]3(C)CC=C24)C(O)=O)(C)[C@H](C)C(C)C)N=CN=C1C1=CC=NC=C1 BODYFEUFKHPRCK-ZCZMVWJSSA-N 0.000 claims 3
- 125000001841 imino group Chemical group [H]N=* 0.000 claims 3
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- KPCZJLGGXRGYIE-UHFFFAOYSA-N [C]1=CC=CN=C1 Chemical group [C]1=CC=CN=C1 KPCZJLGGXRGYIE-UHFFFAOYSA-N 0.000 claims 2
- 239000002671 adjuvant Substances 0.000 claims 2
- 125000004202 aminomethyl group Chemical group [H]N([H])C([H])([H])* 0.000 claims 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 125000004106 butoxy group Chemical group [*]OC([H])([H])C([H])([H])C(C([H])([H])[H])([H])[H] 0.000 claims 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 claims 2
- 125000006574 non-aromatic ring group Chemical group 0.000 claims 2
- 239000001301 oxygen Substances 0.000 claims 2
- 125000004430 oxygen atom Chemical group O* 0.000 claims 2
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 claims 2
- 125000004528 pyrimidin-5-yl group Chemical group N1=CN=CC(=C1)* 0.000 claims 2
- 125000004434 sulfur atom Chemical group 0.000 claims 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- 239000003981 vehicle Substances 0.000 claims 2
- 125000006645 (C3-C4) cycloalkyl group Chemical group 0.000 claims 1
- 125000001607 1,2,3-triazol-1-yl group Chemical group [*]N1N=NC([H])=C1[H] 0.000 claims 1
- XTFIVUDBNACUBN-UHFFFAOYSA-N 1,3,5-trinitro-1,3,5-triazinane Chemical compound [O-][N+](=O)N1CN([N+]([O-])=O)CN([N+]([O-])=O)C1 XTFIVUDBNACUBN-UHFFFAOYSA-N 0.000 claims 1
- 125000006018 1-methyl-ethenyl group Chemical group 0.000 claims 1
- 125000004206 2,2,2-trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims 1
- 125000004778 2,2-difluoroethyl group Chemical group [H]C([H])(*)C([H])(F)F 0.000 claims 1
- 125000000022 2-aminoethyl group Chemical group [H]C([*])([H])C([H])([H])N([H])[H] 0.000 claims 1
- 125000004777 2-fluoroethyl group Chemical group [H]C([H])(F)C([H])([H])* 0.000 claims 1
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 1
- 125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims 1
- 125000000094 2-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 claims 1
- KEJIWSCZZLLOCC-CPDFAIAISA-N 20-(3-cyano-1,2,4-triazol-4-yl)-5,7,10,15-tetramethyl-7-[(2R)-3-methylbutan-2-yl]-17-oxapentacyclo[13.3.3.01,14.02,11.05,10]henicos-2-ene-6-carboxylic acid Chemical compound C12=CCC3(C)C(C(O)=O)C([C@H](C)C(C)C)(C)CCC3(C)C2CCC2C(C3)(C)COCC21CC3N1C=NN=C1C#N KEJIWSCZZLLOCC-CPDFAIAISA-N 0.000 claims 1
- JJJCTBNRYRDSRX-CPDFAIAISA-N 20-(5-cyano-1,2,4-triazol-1-yl)-5,7,10,15-tetramethyl-7-[(2R)-3-methylbutan-2-yl]-17-oxapentacyclo[13.3.3.01,14.02,11.05,10]henicos-2-ene-6-carboxylic acid Chemical compound C12=CCC3(C)C(C(O)=O)C([C@H](C)C(C)C)(C)CCC3(C)C2CCC2C(C3)(C)COCC21CC3N1N=CN=C1C#N JJJCTBNRYRDSRX-CPDFAIAISA-N 0.000 claims 1
- 125000004179 3-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(Cl)=C1[H] 0.000 claims 1
- 125000004207 3-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(OC([H])([H])[H])=C1[H] 0.000 claims 1
- 125000004800 4-bromophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Br 0.000 claims 1
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 1
- 125000006164 6-membered heteroaryl group Chemical group 0.000 claims 1
- 241000228212 Aspergillus Species 0.000 claims 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 1
- MAYKXZKDQCOLOD-UHFFFAOYSA-N CC1CCC2(C3CCC4C5(CCCC4(C3=CCC2(C1C(=O)O)C)COC5N6C(=CC=N6)C7=CC=CC=C7)C)C Chemical compound CC1CCC2(C3CCC4C5(CCCC4(C3=CCC2(C1C(=O)O)C)COC5N6C(=CC=N6)C7=CC=CC=C7)C)C MAYKXZKDQCOLOD-UHFFFAOYSA-N 0.000 claims 1
- 241000222120 Candida <Saccharomycetales> Species 0.000 claims 1
- 241001337994 Cryptococcus <scale insect> Species 0.000 claims 1
- 241000233866 Fungi Species 0.000 claims 1
- 229920001503 Glucan Polymers 0.000 claims 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 1
- 125000002619 bicyclic group Chemical group 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 125000006309 butyl amino group Chemical group 0.000 claims 1
- 125000001951 carbamoylamino group Chemical group C(N)(=O)N* 0.000 claims 1
- ZJBYOJIEOKSZJY-CTDFECGVSA-N chembl2165732 Chemical compound O([C@H]1[C@@H](C[C@@]23COC[C@]1(C)[C@@H]2CC[C@@H]1[C@@]2(C)CC[C@]([C@H]([C@]2(C)CC=C13)C(O)=O)(C)[C@H](C)C(C)C)N1C(=NC=N1)C=1C=CN=CC=1)C[C@@H]1CCCN1C ZJBYOJIEOKSZJY-CTDFECGVSA-N 0.000 claims 1
- GQGZKTYWGITQBN-CUINCDKWSA-N chembl2165733 Chemical compound O([C@H]1[C@@H](C[C@@]23COC[C@]1(C)[C@@H]2CC[C@@H]1[C@@]2(C)CC[C@]([C@H]([C@]2(C)CC=C13)C(O)=O)(C)[C@H](C)C(C)C)N1C(=NC=N1)C=1C=CN=CC=1)C[C@@H]1CCCN1 GQGZKTYWGITQBN-CUINCDKWSA-N 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 125000006311 cyclobutyl amino group Chemical group [H]N(*)C1([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- UKJLNMAFNRKWGR-UHFFFAOYSA-N cyclohexatrienamine Chemical group NC1=CC=C=C[CH]1 UKJLNMAFNRKWGR-UHFFFAOYSA-N 0.000 claims 1
- 125000001664 diethylamino group Chemical group [H]C([H])([H])C([H])([H])N(*)C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000003754 ethoxycarbonyl group Chemical group C(=O)(OCC)* 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- DXASQZJWWGZNSF-UHFFFAOYSA-N n,n-dimethylmethanamine;sulfur trioxide Chemical group CN(C)C.O=S(=O)=O DXASQZJWWGZNSF-UHFFFAOYSA-N 0.000 claims 1
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 238000002360 preparation method Methods 0.000 claims 1
- 230000000069 prophylactic effect Effects 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 239000011593 sulfur Substances 0.000 claims 1
- 238000003786 synthesis reaction Methods 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- 0 CC1C(*)(*)N(*)CC1 Chemical compound CC1C(*)(*)N(*)CC1 0.000 description 2
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US13610108P | 2008-08-12 | 2008-08-12 | |
| US61/136,101 | 2008-08-12 | ||
| PCT/US2009/004560 WO2010019204A1 (en) | 2008-08-12 | 2009-08-07 | Antifungal agents |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011530593A JP2011530593A (ja) | 2011-12-22 |
| JP2011530593A5 true JP2011530593A5 (enExample) | 2012-12-20 |
| JP5548875B2 JP5548875B2 (ja) | 2014-07-16 |
Family
ID=41669133
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011522975A Active JP5548875B2 (ja) | 2008-08-12 | 2009-08-07 | 抗真菌剤 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US8188085B2 (enExample) |
| EP (1) | EP2326181A4 (enExample) |
| JP (1) | JP5548875B2 (enExample) |
| CN (2) | CN102176827B (enExample) |
| AU (1) | AU2009282474B2 (enExample) |
| CA (1) | CA2731941C (enExample) |
| WO (1) | WO2010019204A1 (enExample) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103180301B (zh) | 2010-08-26 | 2015-11-25 | 拜耳知识产权有限责任公司 | 5-碘代三唑衍生物 |
| PT3247711T (pt) * | 2015-01-19 | 2022-05-16 | Scynexis Inc | Novos sais e polimorfos de scy-078 |
| JP7263313B2 (ja) * | 2017-04-10 | 2023-04-24 | サイネクシス，インコーポレーテッド | 併用される抗真菌剤 |
| PL3661503T3 (pl) | 2017-08-04 | 2023-01-09 | Scynexis, Inc. | Środki przeciwgrzybicze o zwiększonej aktywności przy kwasowym odczynie ph |
| JP7378401B2 (ja) * | 2018-01-02 | 2023-11-13 | サイネクシス，インコーポレーテッド | リポソームの中にカプセル化されたトリテルペノイド抗真菌薬の注射可能な組成物 |
| US12053486B2 (en) | 2018-03-09 | 2024-08-06 | Therazure LLC | Compositions for the treatment of infections in feet |
| MA54866A (fr) * | 2019-01-30 | 2022-05-04 | Scynexis Inc | Antifongiques triterpénoïdes pour le traitement d'infections ostéoarticulaires fongiques |
| AU2020228036B2 (en) | 2019-02-27 | 2025-08-07 | Scynexis, Inc. | Triterpenoid antifungals for the treatment or prevention of Pneumocystis spp. pneumonia |
| AU2020276595B2 (en) | 2019-05-16 | 2025-12-04 | Scynexis, Inc. | Antifungal Agents for Candida Auris Decolonization |
| WO2021092349A1 (en) | 2019-11-08 | 2021-05-14 | Scynexis, Inc. | Lipid-based formulations of scy-078 salts |
| WO2021097411A1 (en) * | 2019-11-15 | 2021-05-20 | The Research Foundation For The State University Of New York | Anti-fungal compositions and methods for using same |
| CN118724779B (zh) * | 2024-06-05 | 2025-09-23 | 浙江瑞博制药有限公司 | 一种醛基化合物的制备方法 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5756472A (en) * | 1996-01-31 | 1998-05-26 | Merck & Co., Inc. | Antifungal agent obtained from hormonema |
| DE69718141T2 (de) | 1996-01-31 | 2003-08-21 | Merck & Co., Inc. | Fungizid |
| HUP0303249A3 (en) * | 2001-02-22 | 2007-03-28 | Sankyo Co | Water-soluble triazole fungicide compounds and pharmaceutical compositions containing them |
| FR2824324B1 (fr) * | 2001-05-04 | 2003-08-15 | Aventis Pharma Sa | Nouveaux derives d'azole ou de triazole, leur procede de preparation et leur application comme medicaments anti-fongiques |
| AU2002253456A1 (en) | 2002-04-17 | 2003-10-27 | Ranbaxy Laboratories Limited | Azole derivatives as antifungal agents |
| ES2402659T3 (es) | 2006-04-03 | 2013-05-07 | Merck Sharp & Dohme Corp. | Derivados de enfumafungina como agentes antifúngicos |
-
2009
- 2009-08-07 WO PCT/US2009/004560 patent/WO2010019204A1/en not_active Ceased
- 2009-08-07 JP JP2011522975A patent/JP5548875B2/ja active Active
- 2009-08-07 EP EP09806945A patent/EP2326181A4/en not_active Withdrawn
- 2009-08-07 CA CA2731941A patent/CA2731941C/en active Active
- 2009-08-07 AU AU2009282474A patent/AU2009282474B2/en active Active
- 2009-08-07 CN CN200980140485.1A patent/CN102176827B/zh active Active
- 2009-08-07 CN CN201510182454.XA patent/CN104877001B/zh active Active
- 2009-08-07 US US12/461,318 patent/US8188085B2/en active Active
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