EA200201046A1 - 7- или 9-замещенные соединения тетрациклина, способ их получения (варианты), фармацевтическая композиция, способ лечения состояния, чувствительного к действию тетрациклина, у млекопитающего и реакционноспособное промежуточное производное - Google Patents

7- или 9-замещенные соединения тетрациклина, способ их получения (варианты), фармацевтическая композиция, способ лечения состояния, чувствительного к действию тетрациклина, у млекопитающего и реакционноспособное промежуточное производное

Info

Publication number
EA200201046A1
EA200201046A1 EA200201046A EA200201046A EA200201046A1 EA 200201046 A1 EA200201046 A1 EA 200201046A1 EA 200201046 A EA200201046 A EA 200201046A EA 200201046 A EA200201046 A EA 200201046A EA 200201046 A1 EA200201046 A1 EA 200201046A1
Authority
EA
Eurasian Patent Office
Prior art keywords
applications
treatment
methods
substituted
conditions
Prior art date
Application number
EA200201046A
Other languages
English (en)
Inventor
Тодд Е. Баузер
Мохамед И. Измаил
Стюарт Б. Леви
Марк Л. Нельсон
Роджер Фречетт
Original Assignee
Трастис Оф Тафтс Коллидж
Пэрэтек Фамэсьютикэлс, Инк.
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Трастис Оф Тафтс Коллидж, Пэрэтек Фамэсьютикэлс, Инк. filed Critical Трастис Оф Тафтс Коллидж
Publication of EA200201046A1 publication Critical patent/EA200201046A1/ru

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/24Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton
    • C07C237/26Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton of a ring being part of a condensed ring system formed by at least four rings, e.g. tetracycline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06Esters of carbamic acids
    • C07C271/08Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/26Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring
    • C07C271/30Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring to a carbon atom of a six-membered aromatic ring being part of a condensed ring system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06Esters of carbamic acids
    • C07C271/40Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings
    • C07C271/58Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/28Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C275/42Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by carboxyl groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/50Compounds containing any of the groups, X being a hetero atom, Y being any atom
    • C07C311/52Y being a hetero atom
    • C07C311/54Y being a hetero atom either X or Y, but not both, being nitrogen atoms, e.g. N-sulfonylurea
    • C07C311/57Y being a hetero atom either X or Y, but not both, being nitrogen atoms, e.g. N-sulfonylurea having sulfur atoms of the sulfonylurea groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/60Y being a hetero atom either X or Y, but not both, being nitrogen atoms, e.g. N-sulfonylurea having sulfur atoms of the sulfonylurea groups bound to carbon atoms of six-membered aromatic rings having nitrogen atoms of the sulfonylurea groups bound to carbon atoms of six-membered aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C333/00Derivatives of thiocarbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C333/02Monothiocarbamic acids; Derivatives thereof
    • C07C333/08Monothiocarbamic acids; Derivatives thereof having nitrogen atoms of thiocarbamic groups bound to carbon atoms of six-membered aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C335/00Thioureas, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C335/04Derivatives of thiourea
    • C07C335/16Derivatives of thiourea having nitrogen atoms of thiourea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C335/20Derivatives of thiourea having nitrogen atoms of thiourea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by nitrogen atoms, not being part of nitro or nitroso groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/38Nitrogen atoms
    • C07D277/42Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/56Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0055Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of at least three carbon atoms which may or may not be branched, e.g. cholane or cholestane derivatives, optionally cyclised, e.g. 17-beta-phenyl or 17-beta-furyl derivatives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00Systems containing at least three condensed rings
    • C07C2603/02Ortho- or ortho- and peri-condensed systems
    • C07C2603/04Ortho- or ortho- and peri-condensed systems containing three rings
    • C07C2603/06Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members
    • C07C2603/10Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings
    • C07C2603/12Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings only one five-membered ring
    • C07C2603/18Fluorenes; Hydrogenated fluorenes
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00Systems containing at least three condensed rings
    • C07C2603/02Ortho- or ortho- and peri-condensed systems
    • C07C2603/40Ortho- or ortho- and peri-condensed systems containing four condensed rings
    • C07C2603/42Ortho- or ortho- and peri-condensed systems containing four condensed rings containing only six-membered rings
    • C07C2603/44Naphthacenes; Hydrogenated naphthacenes
    • C07C2603/461,4,4a,5,5a,6,11,12a- Octahydronaphthacenes, e.g. tetracyclines

Abstract

Предложены замещенные соединения тетрациклина, способы их синтеза и применения. Описаны также тетрациклины, пригодные для лечения чувствительных к тетрациклину нарушений. Включены также промежуточные соединения, используемые для синтеза других соединений тетрациклина.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA200201046A 2000-03-31 2001-03-30 7- или 9-замещенные соединения тетрациклина, способ их получения (варианты), фармацевтическая композиция, способ лечения состояния, чувствительного к действию тетрациклина, у млекопитающего и реакционноспособное промежуточное производное EA200201046A1 (ru)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US19387900P 2000-03-31 2000-03-31
US19397200P 2000-03-31 2000-03-31
US28036701P 2001-03-29 2001-03-29
PCT/US2001/010342 WO2001074761A1 (en) 2000-03-31 2001-03-30 7-and 9-carbamate, urea, thiourea, thiocarbamate, and heteroaryl-amino substituted tetracycline compounds

Publications (1)

Publication Number Publication Date
EA200201046A1 true EA200201046A1 (ru) 2003-04-24

Family

ID=27393263

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200201046A EA200201046A1 (ru) 2000-03-31 2001-03-30 7- или 9-замещенные соединения тетрациклина, способ их получения (варианты), фармацевтическая композиция, способ лечения состояния, чувствительного к действию тетрациклина, у млекопитающего и реакционноспособное промежуточное производное

Country Status (18)

Country Link
US (3) US6818634B2 (ru)
EP (1) EP1272459B1 (ru)
JP (1) JP2004505012A (ru)
KR (1) KR20030007489A (ru)
CN (1) CN1430600A (ru)
AR (1) AR033361A1 (ru)
AT (1) ATE365710T1 (ru)
AU (1) AU2001251157A1 (ru)
BR (1) BR0109725A (ru)
CA (1) CA2404628A1 (ru)
CZ (1) CZ20023581A3 (ru)
DE (1) DE60129116T2 (ru)
EA (1) EA200201046A1 (ru)
ES (1) ES2288945T3 (ru)
HU (1) HUP0300082A2 (ru)
IL (1) IL151971A0 (ru)
MX (1) MXPA02009482A (ru)
WO (1) WO2001074761A1 (ru)

Families Citing this family (68)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US20050281821A1 (en) * 1999-01-06 2005-12-22 Flavia Pernasetti Method and composition for angiogenesis inhibition
DK1240133T3 (da) * 1999-09-14 2006-08-21 Tufts College Fremgangsmåde til fremstilling af substituerede tetracycliner med overgangsmetalbaserede kemiske metoder
US8106225B2 (en) * 1999-09-14 2012-01-31 Trustees Of Tufts College Methods of preparing substituted tetracyclines with transition metal-based chemistries
AU3105801A (en) * 2000-01-24 2001-07-31 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
DE60102815D1 (de) * 2000-05-15 2004-05-19 Paratek Pharm Innc 7-substituierte kondensierte ring-tetrazyclin- verbindungen
US20040224927A1 (en) * 2000-06-16 2004-11-11 Trustees Of Tufts College 7-N-substituted phenyl tetracycline compounds
US20020132798A1 (en) 2000-06-16 2002-09-19 Nelson Mark L. 7-phenyl-substituted tetracycline compounds
AU2001268475A1 (en) 2000-06-16 2002-01-02 Trustees Of Tufts College 7-phenyl-substituted tetracycline compounds
SI1301467T1 (sl) 2000-07-07 2007-02-28 Tufts College 9-substituirane minociklinske spojine
BR0112265A (pt) 2000-07-07 2003-06-24 Tufts College Compostos de tetraciclina substituìda, e de sanciclina 7-substituìda, método para tratar um estado responsivo à tetraciclina em um indivìduo, e, composição farmacêutica
US7094806B2 (en) 2000-07-07 2006-08-22 Trustees Of Tufts College 7, 8 and 9-substituted tetracycline compounds
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
WO2002072506A2 (en) * 2001-03-13 2002-09-19 Paratek Pharmaceuticals, Inc. 7-pyrollyl tetracycline compounds and methods of use thereof
MXPA03008165A (es) * 2001-03-13 2003-12-12 Paratek Pharm Innc Compuestos tetraciclina sustituidos en la posicion 7,9.
US7045507B2 (en) 2001-03-14 2006-05-16 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds as synergistic 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
EP1408987B1 (en) 2001-07-13 2013-04-10 Paratek Pharmaceuticals, Inc. Tetracycline compounds having target therapeutic activities
WO2003055441A2 (en) 2001-08-02 2003-07-10 Paratek Pharmaceuticals, Inc. Medicaments
MY133403A (en) * 2001-10-05 2007-11-30 Tetragenex Pharmaceuticals Inc Tetracycline derivatives and methods of use thereof
AU2003235759A1 (en) 2002-01-08 2003-07-24 Paratek Pharmaceuticals, Inc. 4-dedimethylamino tetracycline compounds
KR101163937B1 (ko) * 2002-03-08 2012-07-09 파라테크 파마슈티컬스, 인크. 아미노-메틸 치환된 테트라시클린 화합물
EP1503981A4 (en) * 2002-03-21 2007-08-15 Paratek Pharm Innc SUBSTITUTED TETRACYCLINE COMPOUNDS
CN1700922A (zh) * 2002-07-12 2005-11-23 帕拉特克药品公司 3、10或12a位取代的四环素化合物
CA2503446C (en) * 2002-10-24 2012-12-18 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
WO2005009943A2 (en) 2003-07-09 2005-02-03 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds
EP2332904A3 (en) 2004-01-15 2012-04-11 Paratek Pharmaceuticals, Inc. Derivatives of tetracycline compounds
US20070216872A1 (en) * 2004-03-26 2007-09-20 Hall Estill T Jr Two- Stage Projector Architecture
LT1753713T (lt) * 2004-05-21 2016-11-25 President And Fellows Of Harvard College Tetraciklinų ir jų analogų sintezė
TWI261038B (en) * 2004-08-11 2006-09-01 Bo-Cheng Chen Bicycle gear-shifting handgrip
EP2284164A3 (en) 2004-10-25 2011-09-21 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds
US7858601B2 (en) * 2004-10-25 2010-12-28 Paratek Pharmaceuticals, Inc. 4-substituted tetracyclines and methods of use thereof
JP2008530023A (ja) 2005-02-04 2008-08-07 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 テトラサイクリン化合物の11a,12−誘導体
AR057032A1 (es) * 2005-05-27 2007-11-14 Wyeth Corp Tigeciclina y metodos de preparacion
AR057324A1 (es) * 2005-05-27 2007-11-28 Wyeth Corp Tigeciclina y metodos para preparar 9-aminominociclina
AR057033A1 (es) * 2005-05-27 2007-11-14 Wyeth Corp Tigeciclina y metodos para preparar 9-nitrominociclina
US20070093455A1 (en) * 2005-07-21 2007-04-26 Paul Abato 10-substituted tetracyclines and methods of use thereof
US20070048325A1 (en) * 2005-08-24 2007-03-01 Dennis Van Epps Combination therapies for inhibiting integrin-extracellular matrix interactions
CA2620600A1 (en) 2005-08-31 2007-03-08 Wyeth 9-aminocarbonylsubstituted derivatives of glycylcyclines
BRPI0620646A2 (pt) * 2005-12-22 2011-11-22 Wyeth Corp composição farmacêutica compreendendo tigeciclina e seu uso
RU2008121238A (ru) * 2005-12-22 2010-01-27 Вайет (Us) Способы лечения инфекций желудочно-кишечного тракта с применением тайгециклина
WO2007117639A2 (en) * 2006-04-07 2007-10-18 The President And Fellows Of Harvard College Synthesis of tetracyclines and analogues thereof
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
WO2008045507A2 (en) 2006-10-11 2008-04-17 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds for treatment of bacillus anthracis infections
EP2076133B1 (en) * 2006-10-11 2012-12-12 President and Fellows of Harvard College Synthesis of enone intermediate
EP2109602B1 (en) * 2006-12-21 2014-02-12 Paratek Pharmaceuticals, Inc. Tetracycline derivatives for the treatment of bacterial, viral and parasitic infections
CA2892739A1 (en) 2006-12-21 2008-07-03 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds for treatment of inflammatory skin disorders
WO2008085913A1 (en) * 2007-01-04 2008-07-17 Rib-X Pharmaceuticals, Inc. Methods for treating, preventing, or reducing the risk of opthalmic, otic, and nasal infections
US7935687B2 (en) * 2007-04-12 2011-05-03 Paratek Pharmaceuticals, Inc. Methods for treating spinal muscular atrophy using tetracycline compounds
CA2688662A1 (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
KR101007026B1 (ko) 2007-07-19 2011-01-12 삼성전자주식회사 광대역 무선접속 시스템의 서킷모드 자원할당 장치 및 방법
CA2706475C (en) 2007-11-29 2016-05-03 Actelion Pharmaceuticals Ltd Phosphonic acid derivates and their use as p2y12 receptor antagonists
WO2009111064A2 (en) 2008-03-05 2009-09-11 Paratek Pharmaceuticals, Inc. Minocycline compounds and methods of use thereof
AU2009236631A1 (en) * 2008-04-14 2009-10-22 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds
CN101759598B (zh) * 2008-09-12 2011-11-09 山东轩竹医药科技有限公司 具有氨基烷基脒的四环素化合物
CN101684080B (zh) * 2008-09-16 2011-12-14 山东轩竹医药科技有限公司 含有甲酰肼基的四环素化合物
CN101684083B (zh) * 2008-09-16 2011-10-05 山东轩竹医药科技有限公司 胍基烷酰胺基取代的四环素衍生物
CN101759599B (zh) * 2008-09-17 2012-05-30 山东轩竹医药科技有限公司 具有氨基肟基的四环素类化合物
JP2012503017A (ja) * 2008-09-19 2012-02-02 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 関節リウマチの治療用のテトラサイクリン化合物および関連する治療方法
US9073829B2 (en) 2009-04-30 2015-07-07 President And Fellows Of Harvard College Synthesis of tetracyclines and intermediates thereto
SG10201913599RA (en) 2016-11-01 2020-02-27 Paratek Pharm Innc 9-aminomethyl minocycline compounds and use thereof in treating community-acquired bacterial pneumonia (cabp)
CN110156624B (zh) * 2019-05-29 2022-03-08 河北冀衡药业股份有限公司 一种米诺环素及其衍生物的合成方法

Family Cites Families (71)

* Cited by examiner, † Cited by third party
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
US3338963A (en) 1960-10-28 1967-08-29 American Cyanamid Co Tetracycline compounds
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
US3341585A (en) 1966-05-06 1967-09-12 American Cyanamid Co Substituted 7-and/or 9-amino-6-deoxytetracyclines
NL6607516A (ru) 1966-05-31 1967-12-01
US3345410A (en) 1966-12-01 1967-10-03 American Cyanamid Co Substituted 7- and/or 9-amino tetracyclines
US3483251A (en) 1967-03-03 1969-12-09 American Cyanamid Co Reductive alkylation process
US3373196A (en) 1967-03-21 1968-03-12 American Cyanamid Co 7-and/or 9-(lower alkyl) amino-5a, 6-anhydrotetracyclines
US3518306A (en) 1968-02-19 1970-06-30 American Cyanamid Co 7- and/or 9-(n-nitrosoalkylamino)-6-demethyl-6-deoxytetracyclines
US3579579A (en) * 1968-04-18 1971-05-18 American Cyanamid Co Substituted 7- and/or 9-amino-6-demethyl-6-deoxytetracyclines
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
USRE40183E1 (en) * 1991-10-04 2008-03-25 Wyeth Holdings Corporation 7-Substituted-9-substituted amino-6-demethyl-6-deoxytetracyclines
US5494903A (en) * 1991-10-04 1996-02-27 American Cyanamid Company 7-substituted-9-substituted amino-6-demethyl-6-deoxytetracyclines
DE122006000058I1 (de) * 1991-10-04 2007-01-18 Wyeth Corp 7-Substituierte-9-substituierte Amino-6-Demethyl-6-Deoxy-Tetracycline
US5328902A (en) 1992-08-13 1994-07-12 American Cyanamid Co. 7-(substituted)-9-[(substituted glycyl)amido]-6-demethyl-6-deoxytetracyclines
US5248797A (en) 1992-08-13 1993-09-28 American Cyanamid Company Method for the production of 9-amino-6-demethyl-6-deoxytetracycline
US5442059A (en) 1992-08-13 1995-08-15 American Cyanamid Company 9-[(substituted glycyl)amido)]-6-demethyl-6-deoxytetracyclines
SG47520A1 (en) * 1992-08-13 1998-04-17 American Cyanamid Co New method for the production of 9-amino-6-demethyl-6-deoxytetracycline
DK0599397T3 (da) 1992-11-17 1996-09-16 Univ New York State Res Found Tetracycliner, herunder non-mikrobielle, kemisk-modificerede tetracycliner, inhiberer overdreven collagentværbinding ved diabetes
AU680650B2 (en) 1993-01-06 1997-08-07 Ipsen Manufacturing Ireland Limited Ionic molecular conjugates of biodegradable polyesters and bioactive polypeptides
US5371076A (en) 1993-04-02 1994-12-06 American Cyanamid Company 9-[(substituted glycyl)amido]-6-(substituted)-5-hydroxy-6-deoxytetracyclines
US5684156A (en) 1994-02-08 1997-11-04 Pierce; David R. Process for preparation of clonidine derivatives
WO1995022529A1 (en) 1994-02-17 1995-08-24 Pfizer Inc. 9-(substituted amino)-alpha-6-deoxy-5-oxy tetracycline derivatives, their preparation and their use as antibiotics
US6165999A (en) * 1995-05-03 2000-12-26 Pfizer Inc Tetracycline derivatives
JP3567024B2 (ja) 1995-07-14 2004-09-15 三菱レイヨン株式会社 ベンジルチアゾリジン誘導体の製造方法
JPH09169748A (ja) 1995-12-20 1997-06-30 Kuraray Co Ltd 2−アミノチアゾール−5−カルボニトリル誘導体の製造方法
US5789395A (en) 1996-08-30 1998-08-04 The Research Foundation Of State University Of New York Method of using tetracycline compounds for inhibition of endogenous nitric oxide production
US5786448A (en) 1996-11-07 1998-07-28 Trega Biosciences, Inc. Combinatorial libraries of cyclic urea and cyclic thiourea derivatives and compounds therein
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
US8106225B2 (en) 1999-09-14 2012-01-31 Trustees Of Tufts College Methods of preparing substituted tetracyclines with transition metal-based chemistries
DK1240133T3 (da) 1999-09-14 2006-08-21 Tufts College Fremgangsmåde til fremstilling af substituerede tetracycliner med overgangsmetalbaserede kemiske metoder
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
AU3105801A (en) 2000-01-24 2001-07-31 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
DE60102815D1 (de) 2000-05-15 2004-05-19 Paratek Pharm Innc 7-substituierte kondensierte ring-tetrazyclin- verbindungen
US20020132798A1 (en) 2000-06-16 2002-09-19 Nelson Mark L. 7-phenyl-substituted tetracycline compounds
US20020128237A1 (en) 2000-06-16 2002-09-12 Nelson Mark L. 7-N-substituted phenyl tetracycline compounds
AU2001268475A1 (en) 2000-06-16 2002-01-02 Trustees Of Tufts College 7-phenyl-substituted tetracycline compounds
SI1301467T1 (sl) 2000-07-07 2007-02-28 Tufts College 9-substituirane minociklinske spojine
US20050143353A1 (en) 2000-07-07 2005-06-30 Paratek Pharmaceuticals, Inc. 13-Substituted methacycline compounds
BR0112265A (pt) 2000-07-07 2003-06-24 Tufts College Compostos de tetraciclina substituìda, e de sanciclina 7-substituìda, método para tratar um estado responsivo à tetraciclina em um indivìduo, e, composição farmacêutica
US7094806B2 (en) 2000-07-07 2006-08-22 Trustees Of Tufts College 7, 8 and 9-substituted tetracycline compounds
CA2415086A1 (en) 2000-07-07 2002-01-17 Trustees Of Tufts College 7,8 and 9-substituted tetracycline compounds
MXPA03008165A (es) 2001-03-13 2003-12-12 Paratek Pharm Innc Compuestos tetraciclina sustituidos en la posicion 7,9.
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
US7045507B2 (en) 2001-03-14 2006-05-16 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds as synergistic antifungal agents
WO2002072022A2 (en) 2001-03-14 2002-09-19 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds as antifungal agents
ES2338994T3 (es) 2001-04-24 2010-05-14 Paratek Pharmaceuticals, Inc. Compuestos de tetraciclina sustituida para el tratamiento de la malaria.
US8088820B2 (en) 2001-04-24 2012-01-03 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds for the treatment of malaria
EP1408987B1 (en) 2001-07-13 2013-04-10 Paratek Pharmaceuticals, Inc. Tetracycline compounds having target therapeutic activities
US20060084678A1 (en) 2001-07-13 2006-04-20 Paratek Pharmaceuticals, Inc. Methods for identifying and using MarR family polypeptide binding compounds
WO2003056294A2 (en) 2001-07-13 2003-07-10 Paratek Pharmaceuticals, Inc. Methods for identifying and using marr family polypeptide binding compounds
WO2003055441A2 (en) 2001-08-02 2003-07-10 Paratek Pharmaceuticals, Inc. Medicaments
AU2003235759A1 (en) 2002-01-08 2003-07-24 Paratek Pharmaceuticals, Inc. 4-dedimethylamino tetracycline compounds
KR101163937B1 (ko) 2002-03-08 2012-07-09 파라테크 파마슈티컬스, 인크. 아미노-메틸 치환된 테트라시클린 화합물
EP1503981A4 (en) 2002-03-21 2007-08-15 Paratek Pharm Innc SUBSTITUTED TETRACYCLINE COMPOUNDS
CN1700922A (zh) 2002-07-12 2005-11-23 帕拉特克药品公司 3、10或12a位取代的四环素化合物
CA2503446C (en) 2002-10-24 2012-12-18 Paratek Pharmaceuticals, Inc. Methods of using substituted tetracycline compounds to modulate rna
WO2004062674A2 (en) 2003-01-07 2004-07-29 Paratek Pharmaceuticals, Inc. Substituted polyamines as inhibitors of bacterial efflux pumps
JP4738333B2 (ja) 2003-07-09 2011-08-03 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 9−アミノメチルテトラサイクリン化合物のプロドラッグ
WO2005009943A2 (en) 2003-07-09 2005-02-03 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds
EP2332904A3 (en) 2004-01-15 2012-04-11 Paratek Pharmaceuticals, Inc. Derivatives of tetracycline compounds

Also Published As

Publication number Publication date
EP1272459B1 (en) 2007-06-27
IL151971A0 (en) 2003-04-10
US7858600B2 (en) 2010-12-28
US20110092467A1 (en) 2011-04-21
ATE365710T1 (de) 2007-07-15
CN1430600A (zh) 2003-07-16
MXPA02009482A (es) 2004-05-14
AR033361A1 (es) 2003-12-17
US20020103171A1 (en) 2002-08-01
CA2404628A1 (en) 2001-10-11
DE60129116D1 (en) 2007-08-09
BR0109725A (pt) 2003-02-04
HUP0300082A2 (en) 2003-05-28
WO2001074761A1 (en) 2001-10-11
US6818634B2 (en) 2004-11-16
AU2001251157A1 (en) 2001-10-15
DE60129116T2 (de) 2008-03-13
JP2004505012A (ja) 2004-02-19
EP1272459A1 (en) 2003-01-08
CZ20023581A3 (cs) 2003-04-16
ES2288945T3 (es) 2008-02-01
US20040176334A1 (en) 2004-09-09
KR20030007489A (ko) 2003-01-23

Similar Documents

Publication Publication Date Title
EA200201046A1 (ru) 7- или 9-замещенные соединения тетрациклина, способ их получения (варианты), фармацевтическая композиция, способ лечения состояния, чувствительного к действию тетрациклина, у млекопитающего и реакционноспособное промежуточное производное
EA200401398A1 (ru) Замещённые фенилацетамиды и их применение в качестве активаторов глюкокиназы
EA200000920A1 (ru) Производные бициклических гидроксамовых кислот
EA200300135A1 (ru) Замещенные соединения матациклина (варианты), фармацевтическая композиция (варианты) и способ лечения чувствительного к тетрациклину состояния млекопитающего (варианты)
EA200400368A1 (ru) Новые дигидроптеридиноны, способы их получения и их применение в качестве лекарственных средств
EA200301011A1 (ru) Замещенные соединения тетрациклина (варианты), фармацевтическая композиция и способ лечения чувствительного к тетрациклину состояния субъекта
EA200300873A1 (ru) Новая соль сукцинат o-десметилвенлафаксина
EA200400815A1 (ru) Контролируемый синтез зипразидона и его композиции
ATE233274T1 (de) Oxyiminopregnancarbolactone
ATE206409T1 (de) N-(1-alkyl-5-phenyl-2,3,4,5-tetrahydro-1-h- benzo(b)(1,5)-diazepin-3-yl)-acetamide
ATE339408T1 (de) Terphenylderivate, deren herstellung und zusammensetzungen, die diese enthalten
EA200100451A1 (ru) Замещенные аналоги бензопирана для лечения воспаления
EA200500197A1 (ru) Замещенные соединения тетрациклина, фармацевтическая композиция и способ лечения чувствительного к тетрациклину состояния у субъекта
ECSP095220A (es) Derivados de n-fenil-2-pirimidin-amina
EA200401232A1 (ru) Замещенные соединения тетрациклина, фармацевтическая композиция и способ лечения чувствительного к тетрациклину состояния у субъекта
ATE396993T1 (de) Tetrahydropyranyl-cyclopentyl- tetrahydropyridopyridin-modulatoren der chemokin- rezeptor-aktivität
EA200200510A1 (ru) 4-карбоксиамино-2-этил-1,2,3,4-тетрагидрохинолин в кристаллической форме как ингибитор сетр
BR0304213A (pt) Processo para a sìntese industrial de ranelato de estrÈncio e os seus hidratos
EA200000320A1 (ru) Изохинолины в качестве ингибиторов урокиназы
ATE297903T1 (de) Substituierte phenyluracile
BR0213481A (pt) Sondas
ATE433458T1 (de) Modulatoren von ship-1
EA200501046A1 (ru) Эсциталопрамгидробромид и способ его получения
SE9903290D0 (sv) Novel compounds
EA200500517A1 (ru) Лечение синдрома х замещёнными тетралинами и инданами