JP2011517697A5 - - Google Patents
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- 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 (cg-RX-API-DMAC7.html) | 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 (cg-RX-API-DMAC7.html) |
| EP (1) | EP2276342A4 (cg-RX-API-DMAC7.html) |
| JP (1) | JP2011517697A (cg-RX-API-DMAC7.html) |
| AU (1) | AU2009236631A1 (cg-RX-API-DMAC7.html) |
| CA (1) | CA2721399A1 (cg-RX-API-DMAC7.html) |
| PE (1) | PE20110069A1 (cg-RX-API-DMAC7.html) |
| WO (1) | WO2009128913A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103040773A (zh) | 2003-07-25 | 2013-04-17 | 沃纳奇尔科特有限责任公司 | 多西环素金属络合物固体剂型 |
| NZ556582A (en) * | 2005-01-21 | 2010-12-24 | Warner Chilcott Co Llc | A tetracycline metal complex in a solid dosage form |
| US20090253660A1 (en) | 2008-03-05 | 2009-10-08 | Paratek Pharmaceuticals, Inc. | Minocycline Compounds and Methods of Use Thereof |
| CN105367440A (zh) | 2008-08-08 | 2016-03-02 | 四相制药公司 | C7-氟取代的四环素化合物 |
| CA2761241C (en) | 2009-05-08 | 2018-02-27 | Tetraphase Pharmaceuticals, Inc. | Tetracycline compounds |
| WO2011025982A2 (en) | 2009-08-28 | 2011-03-03 | Tetraphase Pharmaceuticals, Inc. | Tetracycline compounds |
| CA2874640A1 (en) * | 2012-05-30 | 2013-12-05 | Paratek Pharmaceuticals, Inc. | 7-disubstituted-phenyl tetracycline derivatives |
| DK2890673T3 (en) | 2012-08-31 | 2019-03-18 | Tetraphase Pharmaceuticals Inc | tetracycline |
| DK3529236T3 (da) | 2016-10-19 | 2024-05-13 | Tetraphase Pharmaceuticals Inc | Krystalformer af eravacyclin |
| MX2019005070A (es) | 2016-11-01 | 2019-09-23 | Paratek Pharm Innc | Compuestos de 9-aminometil minociclina y su uso en el tratamiento de neumonía bacteriana adquirida en la comunidad (cabp). |
| 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 (cg-RX-API-DMAC7.html) * | 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 |
| US5064821A (en) * | 1982-11-18 | 1991-11-12 | Trustees Of Tufts College | Method and compositions for overcoming tetracycline resistance within living cells |
| US5589470A (en) * | 1990-02-26 | 1996-12-31 | Trustees Of Tufts College | Reducing tetracycline resistance in 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 |
| IL137445A0 (en) * | 1998-01-23 | 2001-07-24 | Tufts College | Pharmaceutically active compounds and methods of use thereof |
| 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 |
| US6500812B2 (en) * | 1999-09-14 | 2002-12-31 | Paratek Pharmaceuticals, Inc. | 13-substituted methacycline compounds |
| US6849615B2 (en) * | 1999-09-14 | 2005-02-01 | Paratek Pharmaceuticals, Inc. | 13-substituted methacycline compounds |
| CZ301835B6 (cs) * | 1999-09-14 | 2010-07-07 | Trustees Of Tufts College | Zpusob prípravy 7-, 9- nebo 13- substituované tetracyklinové slouceniny, reaktivní tetracyklinový chemický komplex a tetracyklinová sloucenina substituovaná v poloze 7 nebo 9 |
| CA2397863A1 (en) * | 2000-01-24 | 2001-07-26 | Trustees Of Tufts College | Tetracycline compounds for treatment of cryptosporidium parvum related disorders |
| KR20030007489A (ko) * | 2000-03-31 | 2003-01-23 | 트러스티즈 오브 터프츠 칼리지 | 7- 및 9-카르바메이트, 우레아, 티오우레아,티오카르바메이트 및 헤테로아릴-아미노 치환된테트라사이클린 화합물 |
| EP2308863A1 (en) * | 2000-05-15 | 2011-04-13 | Paratek Pharmaceuticals, Inc. | 7-substituted fused ring 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 |
| US20040224927A1 (en) * | 2000-06-16 | 2004-11-11 | Trustees Of Tufts College | 7-N-substituted phenyl tetracycline compounds |
| US7094806B2 (en) * | 2000-07-07 | 2006-08-22 | Trustees Of Tufts College | 7, 8 and 9-substituted tetracycline compounds |
| JP4963771B2 (ja) * | 2000-07-07 | 2012-06-27 | トラスティーズ・オブ・タフツ・カレッジ | ７、８および９−置換テトラサイクリン化合物 |
| CN1690047B (zh) * | 2000-07-07 | 2010-10-06 | 塔夫茨大学信托人 | 9-取代的二甲胺四环素化合物 |
| US20050143353A1 (en) * | 2000-07-07 | 2005-06-30 | Paratek Pharmaceuticals, Inc. | 13-Substituted methacycline compounds |
| CN102336679A (zh) * | 2000-07-07 | 2012-02-01 | 塔夫茨大学信托人 | 7-取代的四环素化合物 |
| EA201000388A1 (ru) * | 2001-03-13 | 2010-10-29 | Пэрэтек Фамэсьютикэлс, Инк. | Замещенные соединения тетрациклина (варианты), фармацевтическая композиция и способ лечения чувствительного к тетрациклину состояния субъекта |
| WO2002072506A2 (en) * | 2001-03-13 | 2002-09-19 | Paratek Pharmaceuticals, Inc. | 7-pyrollyl tetracycline compounds and methods of use thereof |
| US7553828B2 (en) * | 2001-03-13 | 2009-06-30 | Paratek Pharmaceuticals, Inc. | 9-aminomethyl substituted minocycline compounds |
| EP1241160A1 (en) * | 2001-03-13 | 2002-09-18 | Glaxo Group Limited | Tetracycline derivatives and their use as antibiotic agents |
| 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 |
| AU2002365120A1 (en) * | 2001-08-02 | 2003-07-15 | Paratek Pharmaceuticals, Inc. | Medicaments |
| WO2003023568A2 (en) * | 2001-09-10 | 2003-03-20 | Paratek Pharmaceuticals, Inc. | Computational method for determining oral bioavailability |
| EP2311799A1 (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 |
| AU2003218243B2 (en) * | 2002-03-21 | 2010-04-01 | 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 |
| JP4686189B2 (ja) * | 2002-10-24 | 2011-05-18 | パラテック ファーマシューティカルズ インコーポレイテッド | Ｒｎａを調節するための置換テトラサイクリン化合物の使用方法 |
| KR101228706B1 (ko) * | 2003-07-09 | 2013-02-01 | 파라테크 파마슈티컬스, 인크. | 치환된 테트라시클린 화합물 |
| US20060287283A1 (en) * | 2003-07-09 | 2006-12-21 | Paratek Pharmaceuticals, Inc. | Prodrugs of 9-aminomethyl tetracycline compounds |
| US7786099B2 (en) * | 2004-01-15 | 2010-08-31 | Paratek Pharmaceuticals, Inc. | Aromatic a-ring derivatives of tetracycline compounds |
| EP2284152A3 (en) * | 2004-10-25 | 2011-10-05 | Paratek Pharmaceuticals, Inc. | Substituted tetracycline compounds |
| EP2301912A3 (en) * | 2004-10-25 | 2012-07-11 | 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 |
| WO2007014154A2 (en) * | 2005-07-21 | 2007-02-01 | Paratek Pharmaceuticals, Inc. | 10-substituted tetracyclines and methods of use thereof |
| AU2007208214B2 (en) * | 2006-01-24 | 2013-02-14 | Paratek Pharmaceuticals, Inc. | Methods of increasing oral bioavailability of tetracyclines |
| AU2007249695A1 (en) * | 2006-05-15 | 2007-11-22 | Paratek Pharmaceuticals, Inc. | Methods of regulating expression of genes or of gene products using substituted tetracycline compounds |
| WO2008045507A2 (en) * | 2006-10-11 | 2008-04-17 | Paratek Pharmaceuticals, Inc. | Substituted tetracycline compounds for treatment of bacillus anthracis infections |
| ES2701725T3 (es) * | 2006-12-21 | 2019-02-25 | Paratek Pharm Innc | Compuestos de tetraciclina sustituida para el tratamiento de trastornos inflamatorios de la piel |
| ES2463457T3 (es) * | 2006-12-21 | 2014-05-28 | Paratek Pharmaceuticals, Inc. | Derivados de la tetraciclina para el tratamiento de infecciones bacterianas, virales y parasitarias |
| EP2144614A1 (en) * | 2007-04-12 | 2010-01-20 | Paratek Pharmaceuticals, Inc. | Methods for treating spinal muscular atrophy using tetracycline compounds |
| JP2010525069A (ja) * | 2007-04-27 | 2010-07-22 | パラテック ファーマシューティカルズ インコーポレイテッド | アミノアルキルテトラサイクリン化合物の合成方法および精製方法 |
| EP2176216B1 (en) * | 2007-07-06 | 2012-04-25 | Paratek Pharmaceuticals, Inc. | Methods for synthesizing 9-substituted minocycline |
-
2009
- 2009-04-14 US US12/423,718 patent/US20100022483A1/en not_active Abandoned
- 2009-04-14 WO PCT/US2009/002344 patent/WO2009128913A1/en not_active Ceased
- 2009-04-14 CA CA2721399A patent/CA2721399A1/en not_active Abandoned
- 2009-04-14 AU AU2009236631A patent/AU2009236631A1/en not_active Abandoned
- 2009-04-14 JP JP2011505019A patent/JP2011517697A/ja active Pending
- 2009-04-14 EP EP09732861A patent/EP2276342A4/en not_active Withdrawn
-
2010
- 2010-04-14 PE PE2010000229A patent/PE20110069A1/es not_active Application Discontinuation