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) | CN104877001B (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 |
|---|---|---|---|---|
| KR20130100142A (ko) | 2010-08-26 | 2013-09-09 | 바이엘 인텔렉쳐 프로퍼티 게엠베하 | 5-요오도트리아졸 유도체 |
| SMT202200202T1 (it) | 2015-01-19 | 2022-07-21 | Scynexis Inc | Sali e polimorfi innovativi di scy-078 |
| CA3059225A1 (en) * | 2017-04-10 | 2018-10-18 | Scynexis, Inc. | Antifungal agents used in combination |
| CN111093655A (zh) | 2017-08-04 | 2020-05-01 | 西尼克斯公司 | 在酸性ph值下具有经增强活性的抗真菌剂 |
| MX2020006992A (es) * | 2018-01-02 | 2020-09-09 | Scynexis Inc | Composiciones inyectables de antifungicos triterpenoides encapsulados en liposomas. |
| US12053486B2 (en) | 2018-03-09 | 2024-08-06 | Therazure LLC | Compositions for the treatment of infections in feet |
| JP7562542B2 (ja) * | 2019-01-30 | 2024-10-07 | サイネクシス，インコーポレーテッド | 真菌性骨－関節感染症を治療するためのトリテルペノイド系抗真菌薬 |
| US20230149376A1 (en) | 2019-02-27 | 2023-05-18 | Scynexis, Inc. | Triterpenoid antifungals for the treatment or prevention of pneumocystis spp. pneumonia |
| MX2021013899A (es) | 2019-05-16 | 2022-02-10 | Scynexis Inc | Agentes antifungicos para la descolinizacion de candida auris. |
| WO2021092349A1 (en) | 2019-11-08 | 2021-05-14 | Scynexis, Inc. | Lipid-based formulations of scy-078 salts |
| US20220409651A1 (en) * | 2019-11-15 | 2022-12-29 | 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 |
| WO1997027860A1 (en) | 1996-01-31 | 1997-08-07 | Merck & Co., Inc. | Antifungal agent |
| 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 |
| WO2003086271A2 (en) | 2002-04-17 | 2003-10-23 | Ranbaxy Laboratories Limited | Azole derivatives as antifungal agents |
| JP5245057B2 (ja) | 2006-04-03 | 2013-07-24 | メルク・シャープ・アンド・ドーム・コーポレーション | 抗真菌剤 |
-
2009
- 2009-08-07 CN CN201510182454.XA patent/CN104877001B/zh active Active
- 2009-08-07 US US12/461,318 patent/US8188085B2/en active Active
- 2009-08-07 EP EP09806945A patent/EP2326181A4/en not_active Withdrawn
- 2009-08-07 CN CN200980140485.1A patent/CN102176827B/zh active Active
- 2009-08-07 WO PCT/US2009/004560 patent/WO2010019204A1/en not_active Ceased
- 2009-08-07 AU AU2009282474A patent/AU2009282474B2/en active Active
- 2009-08-07 JP JP2011522975A patent/JP5548875B2/ja active Active
- 2009-08-07 CA CA2731941A patent/CA2731941C/en active Active
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