JP2011517697A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2011517697A5 JP2011517697A5 JP2011505019A JP2011505019A JP2011517697A5 JP 2011517697 A5 JP2011517697 A5 JP 2011517697A5 JP 2011505019 A JP2011505019 A JP 2011505019A JP 2011505019 A JP2011505019 A JP 2011505019A JP 2011517697 A5 JP2011517697 A5 JP 2011517697A5
- Authority
- JP
- Japan
- Prior art keywords
- aryl
- alkyl
- carbonyl
- heterocycle
- sulfinyl
- 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.)
- Pending
Links
- -1 tetracycline compound Chemical class 0.000 claims description 80
- 125000003118 aryl group Chemical group 0.000 claims description 68
- 125000000217 alkyl group Chemical group 0.000 claims description 66
- 229910052739 hydrogen Inorganic materials 0.000 claims description 66
- 239000001257 hydrogen Substances 0.000 claims description 66
- 125000000623 heterocyclic group Chemical group 0.000 claims description 64
- 150000002431 hydrogen Chemical group 0.000 claims description 64
- 125000002252 acyl group Chemical group 0.000 claims description 62
- 125000003342 alkenyl group Chemical group 0.000 claims description 62
- 125000003545 alkoxy group Chemical group 0.000 claims description 62
- 125000000304 alkynyl group Chemical group 0.000 claims description 62
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 62
- 229910052736 halogen Inorganic materials 0.000 claims description 62
- 150000002367 halogens Chemical group 0.000 claims description 62
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 62
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 62
- 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 claims description 62
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims description 62
- 150000003568 thioethers Chemical group 0.000 claims description 62
- 208000035143 Bacterial infection Diseases 0.000 claims description 20
- 208000022362 bacterial infectious disease Diseases 0.000 claims description 20
- 239000008194 pharmaceutical composition Substances 0.000 claims description 20
- 239000000651 prodrug Chemical group 0.000 claims description 20
- 229940002612 prodrug Drugs 0.000 claims description 20
- 239000004098 Tetracycline Substances 0.000 claims description 18
- 229960002180 tetracycline Drugs 0.000 claims description 18
- 229930101283 tetracycline Natural products 0.000 claims description 18
- 235000019364 tetracycline Nutrition 0.000 claims description 18
- 208000015181 infectious disease Diseases 0.000 claims description 10
- 150000002148 esters Chemical class 0.000 claims description 8
- 150000003839 salts Chemical class 0.000 claims description 8
- 239000003814 drug Substances 0.000 claims description 6
- 230000000813 microbial effect Effects 0.000 claims description 5
- 244000005700 microbiome Species 0.000 claims description 5
- 229910052760 oxygen Inorganic materials 0.000 claims description 5
- 229910052717 sulfur Inorganic materials 0.000 claims description 5
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims description 4
- 241000588724 Escherichia coli Species 0.000 claims description 4
- 239000003937 drug carrier Substances 0.000 claims description 4
- 229940072172 tetracycline antibiotic Drugs 0.000 claims description 4
- 238000004519 manufacturing process Methods 0.000 claims description 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 2
- 241000193998 Streptococcus pneumoniae Species 0.000 claims description 2
- 125000001931 aliphatic group Chemical group 0.000 claims description 2
- 229910052799 carbon Inorganic materials 0.000 claims description 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 2
- 125000002541 furyl group Chemical group 0.000 claims description 2
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
- 229910052757 nitrogen Inorganic materials 0.000 claims description 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 2
- 125000004193 piperazinyl group Chemical group 0.000 claims description 2
- 125000003386 piperidinyl group Chemical group 0.000 claims description 2
- 125000004076 pyridyl group Chemical group 0.000 claims description 2
- 125000000168 pyrrolyl group Chemical group 0.000 claims description 2
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims description 2
- 238000000034 method Methods 0.000 description 18
- 0 *C(*)(C(*c1c(*)c(*)c(*)c(O*)c1C1=O)C1=C1*)C(C(*)(*)C(O*)=C(C(*)=O)C2=O)[C@]12O Chemical compound *C(*)(C(*c1c(*)c(*)c(*)c(O*)c1C1=O)C1=C1*)C(C(*)(*)C(O*)=C(C(*)=O)C2=O)[C@]12O 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- FXXMAATYZFRICG-AFJXRHPYSA-N CN(C)CCNC(c1cccc(-c(cc2)c(CC(CC([C@H](C(O)=C(C(N)=O)C3=O)N(C)C)[C@@]33O)C(C4=O)=C3O)c4c2O)c1)=O Chemical compound CN(C)CCNC(c1cccc(-c(cc2)c(CC(CC([C@H](C(O)=C(C(N)=O)C3=O)N(C)C)[C@@]33O)C(C4=O)=C3O)c4c2O)c1)=O FXXMAATYZFRICG-AFJXRHPYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US4477308P | 2008-04-14 | 2008-04-14 | |
| US61/044,773 | 2008-04-14 | ||
| PCT/US2009/002344 WO2009128913A1 (en) | 2008-04-14 | 2009-04-14 | Substituted tetracycline compounds |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2011517697A JP2011517697A (ja) | 2011-06-16 |
| JP2011517697A5 true JP2011517697A5 (OSRAM) | 2013-05-23 |
Family
ID=41199392
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011505019A Pending JP2011517697A (ja) | 2008-04-14 | 2009-04-14 | 置換テトラサイクリン化合物 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US20100022483A1 (OSRAM) |
| EP (1) | EP2276342A4 (OSRAM) |
| JP (1) | JP2011517697A (OSRAM) |
| AU (1) | AU2009236631A1 (OSRAM) |
| CA (1) | CA2721399A1 (OSRAM) |
| PE (1) | PE20110069A1 (OSRAM) |
| WO (1) | WO2009128913A1 (OSRAM) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2004261143B2 (en) | 2003-07-25 | 2009-11-05 | Allergan Pharmaceuticals International Limited | A doxycycline metal complex in a solid dosage form |
| EP1855690B1 (en) * | 2005-01-21 | 2016-06-01 | Warner Chilcott Company, LLC | A tetracycline metal complex in a solid dosage form |
| WO2009111064A2 (en) | 2008-03-05 | 2009-09-11 | Paratek Pharmaceuticals, Inc. | Minocycline compounds and methods of use thereof |
| ES2655911T3 (es) | 2008-08-08 | 2018-02-22 | Tetraphase Pharmaceuticals, Inc. | Compuestos de tetraciclina sustituidos con C7-fluoro |
| ES2627772T3 (es) | 2009-05-08 | 2017-07-31 | Tetraphase Pharmaceuticals, Inc. | Compuestos de tetraciclina |
| 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 |
| HK1209030A1 (en) * | 2012-05-30 | 2016-03-24 | Paratek Pharmaceuticals, Inc. | 7-disubstituted-phenyl tetracycline derivatives |
| BR112015004523B1 (pt) | 2012-08-31 | 2020-08-04 | Tetraphase Pharmaceuticals, Inc | Compostos de tetraciclina, composições farmacêuticas e seus usos |
| ES2978198T3 (es) | 2016-10-19 | 2024-09-06 | Tetraphase Pharmaceuticals Inc | Formas cristalinas de eravaciclina |
| CN110087655A (zh) | 2016-11-01 | 2019-08-02 | 帕拉特克药品公司 | 9-氨基甲基米诺环素化合物及其在治疗社区获得性细菌性肺炎(cabp)中的用途 |
| US20230113011A1 (en) * | 2020-03-13 | 2023-04-13 | Cmtx Biotech Inc. | Methods of treating illnesses caused by coronavirus, swine flu and avian flu |
Family Cites Families (62)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2990331A (en) * | 1956-11-23 | 1961-06-27 | Pfizer & Co C | Stable solutions of salts of tetracyclines for parenteral administration |
| US2980584A (en) * | 1957-10-29 | 1961-04-18 | Pfizer & Co C | Parenteral magnesium oxytetracycline acetic or lactic acid carboxamide vehicle preparation |
| US3062717A (en) * | 1958-12-11 | 1962-11-06 | Pfizer & Co C | Intramuscular calcium tetracycline acetic or lactic acid carboxamide vehicle preparation |
| US3165531A (en) * | 1962-03-08 | 1965-01-12 | Pfizer & Co C | 13-substituted-6-deoxytetracyclines and process utilizing the same |
| US3454697A (en) * | 1965-06-08 | 1969-07-08 | American Cyanamid Co | Tetracycline antibiotic compositions for oral use |
| NL6607516A (OSRAM) * | 1966-05-31 | 1967-12-01 | ||
| DE1767891C3 (de) * | 1968-06-28 | 1980-10-30 | Pfizer | Verfahren zur Herstellung von wäßrigen arzneilichen Lösungen für die parenterale, perorale und lokale Anwendung mit einem Gehalt an einem Tetracyclinderivat |
| US3957980A (en) * | 1972-10-26 | 1976-05-18 | Pfizer Inc. | Doxycycline parenteral compositions |
| DE2442829A1 (de) * | 1974-09-06 | 1976-03-18 | Merck Patent Gmbh | Tetracyclische verbindungen und verfahren zu ihrer herstellung |
| US4018889A (en) * | 1976-01-02 | 1977-04-19 | Pfizer Inc. | Oxytetracycline compositions |
| US4126680A (en) * | 1977-04-27 | 1978-11-21 | Pfizer Inc. | Tetracycline antibiotic compositions |
| US4806529A (en) * | 1982-11-18 | 1989-02-21 | Trustees Of Tufts College, Tufts University | Tetracycline activity enhancement |
| US5589470A (en) * | 1990-02-26 | 1996-12-31 | Trustees Of Tufts College | Reducing tetracycline resistance in living cells |
| US5064821A (en) * | 1982-11-18 | 1991-11-12 | Trustees Of Tufts College | Method and compositions for overcoming tetracycline resistance within living cells |
| US4806372A (en) * | 1985-02-15 | 1989-02-21 | Georgia Oil & Gas Co., Inc. | Nitrite-free-curing of bacon and product thereof |
| US6756365B2 (en) * | 1991-11-06 | 2004-06-29 | Trustees Of Tufts College | Reducing tetracycline resistance in living cells |
| JP2002501026A (ja) * | 1998-01-23 | 2002-01-15 | トルスティーズ オブ トゥフツ カレッジ | 薬学的に活性の化合物及びその利用法 |
| US6256365B1 (en) * | 1999-08-16 | 2001-07-03 | Analogic Corporation | Apparatus and method for reconstruction of images in a computed tomography system using oblique slices |
| US6849615B2 (en) * | 1999-09-14 | 2005-02-01 | Paratek Pharmaceuticals, Inc. | 13-substituted methacycline compounds |
| PT1240133E (pt) * | 1999-09-14 | 2006-07-31 | Tufts College | Processos para preparar tetraciclinas substituidas com quimicas baseadas em metais de transicao |
| US6500812B2 (en) * | 1999-09-14 | 2002-12-31 | Paratek Pharmaceuticals, Inc. | 13-substituted methacycline compounds |
| EP1263442A1 (en) * | 2000-01-24 | 2002-12-11 | Trustees Of Tufts College | TETRACYCLINE COMPOUNDS FOR TREATMENT OF i CRYPTOSPORIDIUM PARVUM /i RELATED DISORDERS |
| DE60129116T2 (de) * | 2000-03-31 | 2008-03-13 | Trustees Of Tufts College, Medford | 7- und 9-carbamat, harnstoff, thioharnstoff, thiocarbamat und heteroaryl-amino substituierte tetracyclinverbindungen |
| EP1286954B1 (en) * | 2000-05-15 | 2004-04-14 | Paratek Pharmaceuticals, Inc. | 7-substituted fused ring tetracycline compounds |
| US20040224927A1 (en) * | 2000-06-16 | 2004-11-11 | Trustees Of Tufts College | 7-N-substituted phenyl tetracycline compounds |
| AU2001268475A1 (en) * | 2000-06-16 | 2002-01-02 | Trustees Of Tufts College | 7-phenyl-substituted tetracycline compounds |
| US20020132798A1 (en) * | 2000-06-16 | 2002-09-19 | Nelson Mark L. | 7-phenyl-substituted tetracycline compounds |
| MXPA03000055A (es) * | 2000-07-07 | 2003-07-14 | Tufts College | Compuestos de monociclina sustituidos en posicion 9.. |
| DE60144375D1 (de) * | 2000-07-07 | 2011-05-19 | Trustees Of Tufts College Medford | 7-, 8- und 9-substitutierte tetracyclinverbindungen |
| US7094806B2 (en) * | 2000-07-07 | 2006-08-22 | Trustees Of Tufts College | 7, 8 and 9-substituted tetracycline compounds |
| US20050143353A1 (en) * | 2000-07-07 | 2005-06-30 | Paratek Pharmaceuticals, Inc. | 13-Substituted methacycline compounds |
| KR100997596B1 (ko) * | 2000-07-07 | 2010-11-30 | 파라테크 파마슈티컬스, 인크. | 7-치환 테트라사이클린 화합물 |
| EP1241160A1 (en) * | 2001-03-13 | 2002-09-18 | Glaxo Group Limited | Tetracycline derivatives and their use as antibiotic agents |
| US7553828B2 (en) * | 2001-03-13 | 2009-06-30 | Paratek Pharmaceuticals, Inc. | 9-aminomethyl substituted minocycline compounds |
| EP2298732A1 (en) * | 2001-03-13 | 2011-03-23 | Paratek Pharmaceuticals, Inc. | 7,9-Substituted tetracycline compounds |
| WO2002072506A2 (en) * | 2001-03-13 | 2002-09-19 | Paratek Pharmaceuticals, Inc. | 7-pyrollyl tetracycline compounds and methods of use thereof |
| EP1381372A2 (en) * | 2001-03-14 | 2004-01-21 | Paratek Pharmaceuticals, Inc. | Substituted tetracycline compounds as synergistic antifungal agents |
| US6841546B2 (en) * | 2001-03-14 | 2005-01-11 | Paratek Pharmaceuticals, Inc. | Substituted tetracycline compounds as antifungal agents |
| US8088820B2 (en) * | 2001-04-24 | 2012-01-03 | Paratek Pharmaceuticals, Inc. | Substituted tetracycline compounds for the treatment of malaria |
| US20060194773A1 (en) * | 2001-07-13 | 2006-08-31 | Paratek Pharmaceuticals, Inc. | Tetracyline compounds having target therapeutic activities |
| WO2003055441A2 (en) * | 2001-08-02 | 2003-07-10 | Paratek Pharmaceuticals, Inc. | Medicaments |
| AU2002323688A1 (en) * | 2001-09-10 | 2003-03-24 | Paratek Pharmaceuticals, Inc. | Computational method for determining oral bioavailability |
| EP2311797A1 (en) * | 2002-01-08 | 2011-04-20 | Paratek Pharmaceuticals, Inc. | 4-dedimethylamino tetracycline compounds |
| EA201000491A1 (ru) * | 2002-03-08 | 2010-08-30 | Паратек Фармасьютикалс, Инк. | Аминометилзамещенные тетрациклиновые соединения |
| WO2003079984A2 (en) * | 2002-03-21 | 2003-10-02 | Paratek Pharmaceuticals, Inc. | Substituted tetracycline compounds |
| EA012136B1 (ru) * | 2002-07-12 | 2009-08-28 | Пэрэтек Фамэсьютикэлс, Инк. | Замещенные соединения тетрациклина, фармацевтическая композиция и способ лечения чувствительного к тетрациклину состояния у субъекта |
| WO2004038000A2 (en) * | 2002-10-24 | 2004-05-06 | Paratek Pharmaceuticals, Inc. | Methods of using substituted tetracycline compounds to modulate rna |
| US20060287283A1 (en) * | 2003-07-09 | 2006-12-21 | Paratek Pharmaceuticals, Inc. | Prodrugs of 9-aminomethyl tetracycline compounds |
| EP1648859B1 (en) * | 2003-07-09 | 2013-02-27 | Paratek Pharmaceuticals, Inc. | Substituted tetracycline compounds |
| EP2332904A3 (en) * | 2004-01-15 | 2012-04-11 | Paratek Pharmaceuticals, Inc. | Derivatives of tetracycline compounds |
| EP2284152A3 (en) * | 2004-10-25 | 2011-10-05 | Paratek Pharmaceuticals, Inc. | Substituted tetracycline compounds |
| CA2585418A1 (en) * | 2004-10-25 | 2006-05-04 | Paratek Pharmaceuticals, Inc. | 4-aminotetracyclines and methods of use thereof |
| EP1848685A1 (en) * | 2005-02-04 | 2007-10-31 | Paratek Pharmaceuticals, Inc. | 11a, 12-derivatives of tetracycline compounds |
| AU2006272698B2 (en) * | 2005-07-21 | 2012-11-01 | Paratek Pharmaceuticals, Inc. | 10-substituted tetracyclines and methods of use thereof |
| EP1991236A2 (en) * | 2006-01-24 | 2008-11-19 | Paratek Pharmaceuticals, Inc. | Methods of increasing oral bioavailability of tetracyclines |
| CA2652347A1 (en) * | 2006-05-15 | 2007-11-22 | Paratek Pharmaceuticals, Inc. | Methods of regulating expression of genes or of gene products using substituted tetracycline compounds |
| US8440646B1 (en) * | 2006-10-11 | 2013-05-14 | Paratek Pharmaceuticals, Inc. | Substituted tetracycline compounds for treatment of Bacillus anthracis infections |
| ES2548261T3 (es) * | 2006-12-21 | 2015-10-15 | Paratek Pharmaceuticals, Inc. | Derivados de tetraciclina para el tratamiento de infecciones bacterianas, virales y parasitarias |
| AU2007338681B2 (en) * | 2006-12-21 | 2013-09-26 | Paratek Pharmaceuticals, Inc. | Substituted tetracycline compounds for treatment of inflammatory skin disorders |
| US7935687B2 (en) * | 2007-04-12 | 2011-05-03 | Paratek Pharmaceuticals, Inc. | Methods for treating spinal muscular atrophy using tetracycline compounds |
| WO2008134048A2 (en) * | 2007-04-27 | 2008-11-06 | Paratek Pharmaceuticals, Inc. | Methods for synthesizing and purifying aminoalkyl tetracycline compounds |
| CN101784517A (zh) * | 2007-07-06 | 2010-07-21 | 帕拉特克药品公司 | 合成取代的四环素化合物的方法 |
-
2009
- 2009-04-14 CA CA2721399A patent/CA2721399A1/en not_active Abandoned
- 2009-04-14 WO PCT/US2009/002344 patent/WO2009128913A1/en not_active Ceased
- 2009-04-14 AU AU2009236631A patent/AU2009236631A1/en not_active Abandoned
- 2009-04-14 US US12/423,718 patent/US20100022483A1/en not_active Abandoned
- 2009-04-14 EP EP09732861A patent/EP2276342A4/en not_active Withdrawn
- 2009-04-14 JP JP2011505019A patent/JP2011517697A/ja active Pending
-
2010
- 2010-04-14 PE PE2010000229A patent/PE20110069A1/es not_active Application Discontinuation