JP2009533346A5 - - Google Patents
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- Publication number
- JP2009533346A5 JP2009533346A5 JP2009504327A JP2009504327A JP2009533346A5 JP 2009533346 A5 JP2009533346 A5 JP 2009533346A5 JP 2009504327 A JP2009504327 A JP 2009504327A JP 2009504327 A JP2009504327 A JP 2009504327A JP 2009533346 A5 JP2009533346 A5 JP 2009533346A5
- Authority
- JP
- Japan
- Prior art keywords
- unsubstituted
- substituted
- moiety
- branched
- unbranched
- 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
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- 150000001875 compounds Chemical class 0.000 claims description 257
- 229910052739 hydrogen Inorganic materials 0.000 claims description 250
- 239000001257 hydrogen Substances 0.000 claims description 250
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 160
- 125000002252 acyl group Chemical group 0.000 claims description 154
- 125000001072 heteroaryl group Chemical group 0.000 claims description 149
- 125000003118 aryl group Chemical group 0.000 claims description 147
- 125000001931 aliphatic group Chemical group 0.000 claims description 145
- 125000002015 acyclic group Chemical group 0.000 claims description 126
- 125000004122 cyclic group Chemical group 0.000 claims description 126
- 150000002431 hydrogen Chemical group 0.000 claims description 90
- 125000006239 protecting group Chemical group 0.000 claims description 82
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 70
- 229910052736 halogen Inorganic materials 0.000 claims description 69
- 150000002367 halogens Chemical class 0.000 claims description 69
- 125000004104 aryloxy group Chemical group 0.000 claims description 68
- 125000004663 dialkyl amino group Chemical group 0.000 claims description 67
- 125000004414 alkyl thio group Chemical group 0.000 claims description 66
- 125000005110 aryl thio group Chemical group 0.000 claims description 66
- 125000003545 alkoxy group Chemical group 0.000 claims description 65
- 125000005368 heteroarylthio group Chemical group 0.000 claims description 65
- 125000005553 heteroaryloxy group Chemical group 0.000 claims description 61
- 125000003282 alkyl amino group Chemical group 0.000 claims description 57
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 35
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 31
- 238000000034 method Methods 0.000 claims description 29
- 125000000217 alkyl group Chemical group 0.000 claims description 13
- 239000000651 prodrug Substances 0.000 claims description 13
- 229940002612 prodrug Drugs 0.000 claims description 13
- 150000003839 salts Chemical class 0.000 claims description 13
- 241000894006 Bacteria Species 0.000 claims description 10
- 208000015181 infectious disease Diseases 0.000 claims description 10
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 7
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims description 6
- 239000004098 Tetracycline Substances 0.000 claims description 4
- 125000000623 heterocyclic group Chemical group 0.000 claims description 4
- 235000019364 tetracycline Nutrition 0.000 claims description 4
- 150000003522 tetracyclines Chemical class 0.000 claims description 4
- -1 —CHO Chemical group 0.000 claims description 4
- 229960002180 tetracycline Drugs 0.000 claims description 3
- 229930101283 tetracycline Natural products 0.000 claims description 3
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims description 2
- 241000606161 Chlamydia Species 0.000 claims description 2
- RJQXTJLFIWVMTO-TYNCELHUSA-N Methicillin Chemical compound COC1=CC=CC(OC)=C1C(=O)N[C@@H]1C(=O)N2[C@@H](C(O)=O)C(C)(C)S[C@@H]21 RJQXTJLFIWVMTO-TYNCELHUSA-N 0.000 claims description 2
- 241000606701 Rickettsia Species 0.000 claims description 2
- 125000004202 aminomethyl group Chemical group [H]N([H])C([H])([H])* 0.000 claims description 2
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims description 2
- 229910052794 bromium Inorganic materials 0.000 claims description 2
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims description 2
- 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 claims description 2
- 229960003085 meticillin Drugs 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 125000001769 aryl amino group Chemical group 0.000 claims 10
- 241000192125 Firmicutes Species 0.000 claims 1
- 241000202934 Mycoplasma pneumoniae Species 0.000 claims 1
- 108010059993 Vancomycin Proteins 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 229960003165 vancomycin Drugs 0.000 claims 1
- MYPYJXKWCTUITO-UHFFFAOYSA-N vancomycin Natural products O1C(C(=C2)Cl)=CC=C2C(O)C(C(NC(C2=CC(O)=CC(O)=C2C=2C(O)=CC=C3C=2)C(O)=O)=O)NC(=O)C3NC(=O)C2NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(CC(C)C)NC)C(O)C(C=C3Cl)=CC=C3OC3=CC2=CC1=C3OC1OC(CO)C(O)C(O)C1OC1CC(C)(N)C(O)C(C)O1 MYPYJXKWCTUITO-UHFFFAOYSA-N 0.000 claims 1
- MYPYJXKWCTUITO-LYRMYLQWSA-O vancomycin(1+) Chemical compound O([C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1OC1=C2C=C3C=C1OC1=CC=C(C=C1Cl)[C@@H](O)[C@H](C(N[C@@H](CC(N)=O)C(=O)N[C@H]3C(=O)N[C@H]1C(=O)N[C@H](C(N[C@@H](C3=CC(O)=CC(O)=C3C=3C(O)=CC=C1C=3)C([O-])=O)=O)[C@H](O)C1=CC=C(C(=C1)Cl)O2)=O)NC(=O)[C@@H](CC(C)C)[NH2+]C)[C@H]1C[C@](C)([NH3+])[C@H](O)[C@H](C)O1 MYPYJXKWCTUITO-LYRMYLQWSA-O 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 12
- 239000003153 chemical reaction reagent Substances 0.000 description 9
- 229910052751 metal Inorganic materials 0.000 description 6
- 239000002184 metal Substances 0.000 description 6
- 125000005842 heteroatom Chemical group 0.000 description 4
- WHXSMMKQMYFTQS-UHFFFAOYSA-N Lithium Chemical group [Li] WHXSMMKQMYFTQS-UHFFFAOYSA-N 0.000 description 2
- MZRVEZGGRBJDDB-UHFFFAOYSA-N N-Butyllithium Chemical compound [Li]CCCC MZRVEZGGRBJDDB-UHFFFAOYSA-N 0.000 description 2
- 238000013459 approach Methods 0.000 description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 2
- 229910052744 lithium Inorganic materials 0.000 description 2
- ZWLPBLYKEWSWPD-UHFFFAOYSA-N o-toluic acid Chemical compound CC1=CC=CC=C1C(O)=O ZWLPBLYKEWSWPD-UHFFFAOYSA-N 0.000 description 2
- 230000002194 synthesizing effect Effects 0.000 description 2
- SGKRLCUYIXIAHR-AKNGSSGZSA-N (4s,4ar,5s,5ar,6r,12ar)-4-(dimethylamino)-1,5,10,11,12a-pentahydroxy-6-methyl-3,12-dioxo-4a,5,5a,6-tetrahydro-4h-tetracene-2-carboxamide Chemical compound C1=CC=C2[C@H](C)[C@@H]([C@H](O)[C@@H]3[C@](C(O)=C(C(N)=O)C(=O)[C@H]3N(C)C)(O)C3=O)C3=C(O)C2=C1O SGKRLCUYIXIAHR-AKNGSSGZSA-N 0.000 description 1
- FFTVPQUHLQBXQZ-KVUCHLLUSA-N (4s,4as,5ar,12ar)-4,7-bis(dimethylamino)-1,10,11,12a-tetrahydroxy-3,12-dioxo-4a,5,5a,6-tetrahydro-4h-tetracene-2-carboxamide Chemical compound C1C2=C(N(C)C)C=CC(O)=C2C(O)=C2[C@@H]1C[C@H]1[C@H](N(C)C)C(=O)C(C(N)=O)=C(O)[C@@]1(O)C2=O FFTVPQUHLQBXQZ-KVUCHLLUSA-N 0.000 description 1
- SOVUOXKZCCAWOJ-HJYUBDRYSA-N (4s,4as,5ar,12ar)-9-[[2-(tert-butylamino)acetyl]amino]-4,7-bis(dimethylamino)-1,10,11,12a-tetrahydroxy-3,12-dioxo-4a,5,5a,6-tetrahydro-4h-tetracene-2-carboxamide Chemical compound C1C2=C(N(C)C)C=C(NC(=O)CNC(C)(C)C)C(O)=C2C(O)=C2[C@@H]1C[C@H]1[C@H](N(C)C)C(=O)C(C(N)=O)=C(O)[C@@]1(O)C2=O SOVUOXKZCCAWOJ-HJYUBDRYSA-N 0.000 description 1
- 239000007818 Grignard reagent Substances 0.000 description 1
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical group [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 description 1
- 241000204031 Mycoplasma Species 0.000 description 1
- 206010035664 Pneumonia Diseases 0.000 description 1
- HCHKCACWOHOZIP-UHFFFAOYSA-N Zinc Chemical group [Zn] HCHKCACWOHOZIP-UHFFFAOYSA-N 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 150000007513 acids Chemical class 0.000 description 1
- MYPYJXKWCTUITO-KIIOPKALSA-N chembl3301825 Chemical compound O([C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1OC1=C2C=C3C=C1OC1=CC=C(C=C1Cl)[C@@H](O)[C@H](C(N[C@@H](CC(N)=O)C(=O)N[C@H]3C(=O)N[C@H]1C(=O)N[C@H](C(N[C@H](C3=CC(O)=CC(O)=C3C=3C(O)=CC=C1C=3)C(O)=O)=O)[C@H](O)C1=CC=C(C(=C1)Cl)O2)=O)NC(=O)[C@@H](CC(C)C)NC)[C@H]1C[C@](C)(N)C(O)[C@H](C)O1 MYPYJXKWCTUITO-KIIOPKALSA-N 0.000 description 1
- 229960003722 doxycycline Drugs 0.000 description 1
- 150000004795 grignard reagents Chemical class 0.000 description 1
- RQLKAKQYERUOJD-UHFFFAOYSA-N lithium;1,3,5-trimethylbenzene-6-ide Chemical compound [Li+].CC1=CC(C)=[C-]C(C)=C1 RQLKAKQYERUOJD-UHFFFAOYSA-N 0.000 description 1
- UBJFKNSINUCEAL-UHFFFAOYSA-N lithium;2-methylpropane Chemical compound [Li+].C[C-](C)C UBJFKNSINUCEAL-UHFFFAOYSA-N 0.000 description 1
- GPSDUZXPYCFOSQ-UHFFFAOYSA-N m-toluic acid Chemical compound CC1=CC=CC(C(O)=O)=C1 GPSDUZXPYCFOSQ-UHFFFAOYSA-N 0.000 description 1
- 229910052749 magnesium Inorganic materials 0.000 description 1
- 239000011777 magnesium Substances 0.000 description 1
- 229960004023 minocycline Drugs 0.000 description 1
- NHKJPPKXDNZFBJ-UHFFFAOYSA-N phenyllithium Chemical compound [Li]C1=CC=CC=C1 NHKJPPKXDNZFBJ-UHFFFAOYSA-N 0.000 description 1
- 229940040944 tetracyclines Drugs 0.000 description 1
- 229960004089 tigecycline Drugs 0.000 description 1
- 229910052725 zinc Inorganic materials 0.000 description 1
- 239000011701 zinc Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US79041306P | 2006-04-07 | 2006-04-07 | |
| US60/790,413 | 2006-04-07 | ||
| PCT/US2007/008647 WO2007117639A2 (en) | 2006-04-07 | 2007-04-06 | Synthesis of tetracyclines and analogues thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012282759A Division JP2013082730A (ja) | 2006-04-07 | 2012-12-26 | テトラサイクリンおよびその類似体の合成 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2009533346A JP2009533346A (ja) | 2009-09-17 |
| JP2009533346A5 true JP2009533346A5 (enExample) | 2010-05-27 |
| JP5335664B2 JP5335664B2 (ja) | 2013-11-06 |
Family
ID=38581662
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009504327A Active JP5335664B2 (ja) | 2006-04-07 | 2007-04-06 | テトラサイクリンおよびその類似体の合成 |
| JP2012282759A Withdrawn JP2013082730A (ja) | 2006-04-07 | 2012-12-26 | テトラサイクリンおよびその類似体の合成 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012282759A Withdrawn JP2013082730A (ja) | 2006-04-07 | 2012-12-26 | テトラサイクリンおよびその類似体の合成 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US8486921B2 (enExample) |
| EP (1) | EP2016044B1 (enExample) |
| JP (2) | JP5335664B2 (enExample) |
| AU (1) | AU2007235279B2 (enExample) |
| CA (1) | CA2648668C (enExample) |
| WO (1) | WO2007117639A2 (enExample) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101027279B (zh) | 2004-05-21 | 2013-03-27 | 哈佛大学校长及研究员协会 | 四环素及其类似物的合成 |
| AU2007235279B2 (en) | 2006-04-07 | 2012-12-06 | President And Fellows Of Harvard College | Synthesis of tetracyclines and analogues thereof |
| US8440646B1 (en) * | 2006-10-11 | 2013-05-14 | Paratek Pharmaceuticals, Inc. | Substituted tetracycline compounds for treatment of Bacillus anthracis infections |
| US7763735B2 (en) | 2006-10-11 | 2010-07-27 | President And Fellows Of Harvard College | Synthesis of enone intermediate |
| DE102007034259A1 (de) * | 2007-07-20 | 2009-01-22 | Otto-Von-Guericke-Universität Magdeburg Medizinische Fakultät | Verfahren zur Synthese von A-Ring-aromatisierten Acetyl-Minocyclinen |
| ES2655911T3 (es) | 2008-08-08 | 2018-02-22 | Tetraphase Pharmaceuticals, Inc. | Compuestos de tetraciclina sustituidos con C7-fluoro |
| WO2010126607A2 (en) | 2009-04-30 | 2010-11-04 | President And Fellows Of Harvard College | Synthesis of tetracyclines and intermediates thereto |
| ES2627772T3 (es) | 2009-05-08 | 2017-07-31 | Tetraphase Pharmaceuticals, Inc. | Compuestos de tetraciclina |
| WO2010132670A2 (en) * | 2009-05-13 | 2010-11-18 | Tetraphase Pharmaceuticals, Inc. | Pentacycline compounds |
| JP5944825B2 (ja) | 2009-08-28 | 2016-07-05 | テトラフェース ファーマシューティカルズ，インコーポレイテッド | テトラサイクリン化合物 |
| JP5820462B2 (ja) * | 2010-03-31 | 2015-11-24 | テトラフェース ファーマシューティカルズ，インコーポレイテッド | 多環式テトラサイクリン化合物 |
| WO2012047907A1 (en) | 2010-10-04 | 2012-04-12 | President And Fellows Of Harvard College | Synthesis of c5-substituted tetracyclines, uses thereof, and intermediates thereto |
| WO2012065028A2 (en) | 2010-11-11 | 2012-05-18 | Concert Pharmaceuticals Inc. | Substituted tetracyclines |
| JP2013123450A (ja) * | 2011-12-13 | 2013-06-24 | Akihiro Sato | 金属錯体イオン液を応用した塵肺の療養方法、および、咽頭・気管・気管支の療養方法 |
| BR112015004523B1 (pt) * | 2012-08-31 | 2020-08-04 | Tetraphase Pharmaceuticals, Inc | Compostos de tetraciclina, composições farmacêuticas e seus usos |
| CN102993043B (zh) * | 2012-12-04 | 2015-03-04 | 天津大学 | 一种制备高纯度盐酸四环素的方法 |
| KR20170134514A (ko) | 2015-03-23 | 2017-12-06 | 바이오팜엑스 인코포레이티드 | 피부과 사용을 위한 약학 테트라사이클린 조성물 |
| ES2978198T3 (es) | 2016-10-19 | 2024-09-06 | Tetraphase Pharmaceuticals Inc | Formas cristalinas de eravaciclina |
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-
2007
- 2007-04-06 AU AU2007235279A patent/AU2007235279B2/en active Active
- 2007-04-06 JP JP2009504327A patent/JP5335664B2/ja active Active
- 2007-04-06 EP EP07774919.0A patent/EP2016044B1/en active Active
- 2007-04-06 CA CA2648668A patent/CA2648668C/en active Active
- 2007-04-06 US US12/296,223 patent/US8486921B2/en active Active
- 2007-04-06 WO PCT/US2007/008647 patent/WO2007117639A2/en not_active Ceased
-
2012
- 2012-12-26 JP JP2012282759A patent/JP2013082730A/ja not_active Withdrawn
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