TWI305528B - 9-substituted minocycline compounds - Google Patents

9-substituted minocycline compounds Download PDF

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Publication number
TWI305528B
TWI305528B TW093140806A TW93140806A TWI305528B TW I305528 B TWI305528 B TW I305528B TW 093140806 A TW093140806 A TW 093140806A TW 93140806 A TW93140806 A TW 93140806A TW I305528 B TWI305528 B TW I305528B
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Taiwan
Prior art keywords
group
substituted
pharmaceutically acceptable
acceptable salt
alkyl
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TW093140806A
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English (en)
Chinese (zh)
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TW200519070A (en
Inventor
L Nelson Mark
Frechette Roger
Viski Peter
Ismail Mohamed
Bowser Todd
Dumornay Jimmie
Rennie Glen
Liu Gui
Koza Darrell
Sheahan Paul
Stapleton Karen
Hawkins Paul
Bhatia Beena
Verma Atul
Mcintyre Laura
Warchol Tadeusz
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Tufts College
Paratek Pharm Innc
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    • A—HUMAN NECESSITIES
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • C07C237/26—Carboxylic 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
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    • C07C255/59—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton the carbon skeleton being further substituted by singly-bound oxygen atoms
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    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
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    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
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TW093140806A 2000-07-07 2001-07-06 9-substituted minocycline compounds TWI305528B (en)

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US21665900P 2000-07-07 2000-07-07
US27562101P 2001-03-13 2001-03-13

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TW200519070A TW200519070A (en) 2005-06-16
TWI305528B true TWI305528B (en) 2009-01-21

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Families Citing this family (80)

* 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
WO1999037306A1 (en) * 1998-01-23 1999-07-29 Trustees Of Tufts College Pharmaceutically active compounds and methods of use thereof
US8106225B2 (en) * 1999-09-14 2012-01-31 Trustees Of Tufts College Methods of preparing substituted tetracyclines with transition metal-based chemistries
EP1666454B1 (en) * 1999-09-14 2011-09-07 Trustees Of Tufts College Methods of preparing substituted tetracyclines with transition metal-based chemistries
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
ATE264295T1 (de) * 2000-05-15 2004-04-15 Paratek Pharm Innc 7-substituierte kondensierte ring-tetrazyclin- verbindungen
AU2001268475A1 (en) * 2000-06-16 2002-01-02 Trustees Of Tufts College 7-phenyl-substituted tetracycline compounds
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
EA201000496A1 (ru) * 2000-07-07 2010-10-29 Трастис Оф Тафтс Коллидж Замещенное соединение миноциклина, способ получения замещенных соединений миноциклина (варианты)
US7094806B2 (en) * 2000-07-07 2006-08-22 Trustees Of Tufts College 7, 8 and 9-substituted tetracycline compounds
AU2002250331A1 (en) * 2001-03-13 2002-09-24 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
HRP20030743A2 (en) * 2001-03-13 2005-06-30 Paratek Pharmaceuticals 7,9-substituted tetracycline compounds
EP1241160A1 (en) * 2001-03-13 2002-09-18 Glaxo Group Limited Tetracycline derivatives and their use as antibiotic agents
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
EP2332549A1 (en) 2001-07-13 2011-06-15 Paratek Pharmaceuticals, Inc. Novel tetracyclines and their use in medicine
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
US7056902B2 (en) * 2002-01-08 2006-06-06 Paratek Pharmaceuticals, Inc. 4-dedimethylamino tetracycline compounds
EP2316450A1 (en) 2002-03-08 2011-05-04 Paratek Pharmaceuticals, Inc. Amino-methyl substituted tetracycline compounds
KR101083498B1 (ko) * 2002-03-21 2011-11-16 파라테크 파마슈티컬스, 인크. 치환된 테트라시클린 화합물
WO2003079983A2 (en) * 2002-03-21 2003-10-02 Trustees Of Tufts College Methods of preparing substituted tetracyclines with transition metal-based chemistries
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
US8173624B2 (en) * 2002-10-24 2012-05-08 Paratek Pharmaceuticals, Inc. Methods of using substituted tetracycline compounds to modulate RNA
JP2006503898A (ja) * 2002-10-24 2006-02-02 パラテック ファーマシューティカルズ， インク． マラリア治療のための置換テトラサイクリン化合物
WO2004091513A2 (en) * 2003-04-10 2004-10-28 Paratek Pharmaceuticals, Inc. 9-aminomethyl substituted minocycline compounds
US20060287283A1 (en) * 2003-07-09 2006-12-21 Paratek Pharmaceuticals, Inc. Prodrugs of 9-aminomethyl tetracycline compounds
CN1845897A (zh) * 2003-07-09 2006-10-11 帕拉特克药品公司 取代的四环素化合物
EP1656341A1 (en) * 2003-07-09 2006-05-17 Paratek Pharmaceuticals, Inc. Prodrugs of 9-aminomethyl tetracycline compounds
US8691258B2 (en) * 2003-12-12 2014-04-08 Medtronic, Inc. Anti-infective medical device
EP2332904A3 (en) 2004-01-15 2012-04-11 Paratek Pharmaceuticals, Inc. Derivatives of tetracycline compounds
BRPI0510113B1 (pt) * 2004-05-21 2022-09-27 President And Fellows Of Harvard College Compostos de tetraciclinas e análogos das mesmas
TWI261038B (en) * 2004-08-11 2006-09-01 Bo-Cheng Chen Bicycle gear-shifting handgrip
EP2284151A3 (en) 2004-10-25 2011-09-21 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds
EP2301916A3 (en) 2004-10-25 2011-09-28 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
AR057032A1 (es) * 2005-05-27 2007-11-14 Wyeth Corp Tigeciclina y metodos de preparacion
AR057033A1 (es) * 2005-05-27 2007-11-14 Wyeth Corp Tigeciclina y metodos para preparar 9-nitrominociclina
AR057324A1 (es) * 2005-05-27 2007-11-28 Wyeth Corp Tigeciclina y metodos para preparar 9-aminominociclina
CA2616224A1 (en) * 2005-07-21 2007-02-01 Paratek Pharmaceuticals, Inc. 10-substituted tetracyclines and methods of use thereof
AU2006331685A1 (en) * 2005-12-22 2007-07-05 Wyeth Methods of treating gastrointestinal tract infections with tigecycline
EP1965770A2 (en) * 2005-12-22 2008-09-10 Wyeth a Corporation of the State of Delaware Oral formulations comprising tigecycline
WO2007087416A2 (en) 2006-01-24 2007-08-02 Paratek Pharaceuticals, Inc. Methods of increasing oral bioavailability of tetracyclines
EP2016044B1 (en) * 2006-04-07 2020-06-10 President and Fellows of Harvard College Pentacycline derivatives for the treatment of infections
CA2652346A1 (en) * 2006-05-15 2007-11-22 Paratek Pharmaceuticals, Inc. Methods of regulating expression of genes or of gene products using substituted tetracycline compounds
US7763735B2 (en) 2006-10-11 2010-07-27 President And Fellows Of Harvard College Synthesis of enone intermediate
WO2008045507A2 (en) 2006-10-11 2008-04-17 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds for treatment of bacillus anthracis infections
US8513223B2 (en) 2006-12-21 2013-08-20 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds for treatment of inflammatory skin disorders
ES2463457T3 (es) * 2006-12-21 2014-05-28 Paratek Pharmaceuticals, Inc. Derivados de la tetraciclina para el tratamiento de infecciones bacterianas, virales y parasitarias
JP2010523684A (ja) * 2007-04-12 2010-07-15 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を用いる、脊髄筋委縮症を治療するための方法
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
US9522872B2 (en) * 2007-07-06 2016-12-20 Paratek Pharmaceuticals, Inc. Methods for synthesizing substituted tetracycline compounds
CN101868469B (zh) 2007-11-29 2014-04-02 埃科特莱茵药品有限公司 膦酸衍生物及其作为p2y12受体拮抗剂
CA2717703A1 (en) 2008-03-05 2009-09-11 Paratek Pharmaceuticals, Inc. Minocycline compounds and methods of use thereof
PT2271348T (pt) * 2008-03-28 2018-04-16 Paratek Pharm Innc Formulação de comprimido oral de composto de tetraciclina
US20100022483A1 (en) * 2008-04-14 2010-01-28 Paratek Pharmaceuticals, Inc. Substituted Tetracycline Compounds
TW202216656A (zh) * 2008-05-19 2022-05-01 美商Ｐｒｔｋ Ｓｐｖ２公司 四環素化合物之甲苯磺酸鹽及同素異形體
HRP20130928T1 (hr) * 2008-08-08 2013-11-22 Tetraphase Pharmaceuticals, Inc. C7-fluor supstituirani spojevi tetraciklina
JP5443720B2 (ja) * 2008-09-05 2014-03-19 住友化学株式会社 組成物、光学フィルム及びその製造方法、光学部材ならびに表示装置
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
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
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
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
BRPI0918050A2 (pt) * 2008-09-19 2015-09-22 Paratek Pharm Innc compostos de tetraciclina para o tratamento de artrite reumatoide e metodos relacionados de tratamento
WO2010126607A2 (en) 2009-04-30 2010-11-04 President And Fellows Of Harvard College Synthesis of tetracyclines and intermediates thereto
US9315451B2 (en) 2009-05-08 2016-04-19 Tetraphase Pharmaceuticals, Inc. Tetracycline compounds
DK2470500T3 (en) 2009-08-28 2018-01-08 Tetraphase Pharmaceuticals Inc tetracycline
EP2738156B1 (en) 2011-07-26 2018-01-03 Kbp Biosciences Usa Inc. 9-aminomethyl substituted tetracycline compounds
EP2872146A4 (en) * 2012-07-13 2016-01-06 Paratek Pharm Innc TETRACYCLIN COMPOUNDS FOR THE TREATMENT OF NEURODEEGENERATIVE DISEASES
CN108329312B (zh) 2012-08-31 2021-12-31 四相制药公司 四环素化合物
TWI641372B (zh) 2013-03-15 2018-11-21 美商梅琳塔有限責任公司 使用抗生素治療超重和肥胖患者感染的方法
ES2954860T3 (es) * 2014-10-24 2023-11-27 Launx Biomedical Co Ltd Uso de azelnidipina en la preparación de una composición medicinal para el tratamiento de cánceres
AU2016235151A1 (en) 2015-03-24 2017-10-12 Paratek Pharmaceuticals, Inc. Minocycline compounds for biodefense
CN119454720A (zh) * 2016-03-24 2025-02-18 帕拉特克Spv2有限责任公司 用于治疗和预防艰难梭菌感染的方法
HUE066360T2 (hu) 2016-10-19 2024-07-28 Tetraphase Pharmaceuticals Inc Eravaciklin kristályformái
RU2019113715A (ru) 2016-11-01 2020-12-03 Паратек Фармасьютикалс, Инк. 9-аминометилминоциклиновые соединения и их применение для лечениия внебольничной бактериальной пневмонии(вбп)
BR112021004057A2 (pt) * 2018-09-04 2021-05-25 Paratek Pharmaceuticals, Inc. métodos de tratar ou prevenir uma infecção micobacteriana, de tratar ou prevenir, de controlar ou reduzir o avanço, severidade ou efeitos de uma doença micobacteriana, tuberculose, lepra, bronquiectasia, doença pulmonar cavitária, linfadenite, uma doença de tecido mole, granuloma de aquário, úlcera de buruli, uma doença ocular e doença óssea em um indivíduo em necessidade dos mesmos, e, métodos de tratar um indivíduo com uma doença pulmonar e de tratar um indivíduo com uma condição imunossuprimida.

Family Cites Families (90)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US53711A (en) * 1866-04-03 Improvement in the construction of pulleys
USRE26271E (en) 1967-09-26 Reductive alkylation process
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
US3007965A (en) * 1959-02-13 1961-11-07 American Cyanamid Co New tetracyclines produced by streptomyces aureofaciens
GB921252A (en) * 1960-03-09 1963-03-20 Erba Carlo Spa New tetracycline derivatives
US3338963A (en) * 1960-10-28 1967-08-29 American Cyanamid Co Tetracycline compounds
US3219671A (en) * 1961-04-14 1965-11-23 American Cyanamid Co Substituted 6-deoxytetracyclines and 6-demethyl-6-deoxytetracyclines
GB955766A (en) 1961-06-14 1964-04-22 Ciba Ltd New thioethers and process for their manufacture
US3165531A (en) 1962-03-08 1965-01-12 Pfizer & Co C 13-substituted-6-deoxytetracyclines and process utilizing the same
USRE26253E (en) 1963-05-17 1967-08-15 And z-alkylamino-g-deoxytetracycline
US3373193A (en) * 1963-11-13 1968-03-12 Olin Mathieson Dimeric halophospha (iii)-carboranes and their production
ES302929A1 (es) 1964-08-07 1964-12-01 Viladot Oliva Francisco Procedimiento para la obtenciën de compuestos antibiëticos derivados de tetraciclina-penicilina
US3454697A (en) 1965-06-08 1969-07-08 American Cyanamid Co Tetracycline antibiotic compositions for oral use
US3397230A (en) * 1966-03-14 1968-08-13 American Cyanamid Co Nitration of tetracyclines
US3341585A (en) 1966-05-06 1967-09-12 American Cyanamid Co Substituted 7-and/or 9-amino-6-deoxytetracyclines
NL6607516A (enExample) 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
US3360561A (en) * 1967-06-19 1967-12-26 American Cyanamid Co Nitration of tetracyclines
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
NL158172B (nl) * 1972-09-18 1978-10-16 Farmaceutici Italia Werkwijze voor het bereiden van tetracyclinederivaten met een substituent op de 7-plaats.
US3957980A (en) 1972-10-26 1976-05-18 Pfizer Inc. Doxycycline parenteral compositions
DE2527568A1 (de) 1974-06-25 1976-01-15 Farmaceutici Italia Verfahren zur herstellung von alkyltetracyclinen und neue tetracyclinderivate
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
US5064821A (en) * 1982-11-18 1991-11-12 Trustees Of Tufts College Method and compositions for overcoming tetracycline resistance within living cells
US4806529A (en) * 1982-11-18 1989-02-21 Trustees Of Tufts College, Tufts University Tetracycline activity enhancement
JP3009942B2 (ja) * 1991-06-27 2000-02-14 マツダ株式会社 車両の制御装置
US5494903A (en) * 1991-10-04 1996-02-27 American Cyanamid Company 7-substituted-9-substituted amino-6-demethyl-6-deoxytetracyclines
DE122006000058I2 (de) * 1991-10-04 2007-09-13 Wyeth Corp 7-Substituierte-9-substituierte Amino-6-Demethyl-6-Deoxy-Tetracycline
US5281628A (en) * 1991-10-04 1994-01-25 American Cyanamid Company 9-amino-7-(substituted)-6-demethyl-6-deoxytetracyclines
US5442059A (en) * 1992-08-13 1995-08-15 American Cyanamid Company 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
US5284963A (en) * 1992-08-13 1994-02-08 American Cyanamid Company Method of producing 7-(substituted)-9-[(substituted glycyl)-amidol]-6-demethyl-6-deoxytetra-cyclines
US5328902A (en) * 1992-08-13 1994-07-12 American Cyanamid Co. 7-(substituted)-9-[(substituted glycyl)amido]-6-demethyl-6-deoxytetracyclines
US5420272A (en) 1992-08-13 1995-05-30 American Cyanamid Company 7-(substituted)-8-(substituted)-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
JPH06256280A (ja) 1992-11-17 1994-09-13 Univ New York State 糖尿病における過度のコラーゲン架橋結合を阻害する非抗菌性化学修飾テトラサイクリンを含むテトラサイクリン
US5371076A (en) * 1993-04-02 1994-12-06 American Cyanamid Company 9-[(substituted glycyl)amido]-6-(substituted)-5-hydroxy-6-deoxytetracyclines
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
US5675030A (en) * 1994-11-16 1997-10-07 American Cyanamid Company Method for selective extracting a 7-(hydrogen or substituted amino)-9- (substituted glycyl) amido!-6-demethyl-6-deoxytetracycline compound
EP0823893A1 (en) 1995-05-03 1998-02-18 Pfizer Inc. Novel tetracycline derivatives
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
WO1999037306A1 (en) 1998-01-23 1999-07-29 Trustees Of Tufts College Pharmaceutically active compounds and methods of use thereof
DE69932846T2 (de) * 1998-11-18 2007-03-15 Collagenex Pharmaceuticals, Inc. Neue 4-dedimethylaminotetracyclinderivate
US6506740B1 (en) * 1998-11-18 2003-01-14 Robert A. Ashley 4-dedimethylaminotetracycline derivatives
WO2000030958A1 (en) * 1998-11-25 2000-06-02 Henkel Corporation Resealable package containing an organic solvent or solution
EP1666454B1 (en) * 1999-09-14 2011-09-07 Trustees Of Tufts College Methods of preparing substituted tetracyclines with transition metal-based chemistries
US8106225B2 (en) * 1999-09-14 2012-01-31 Trustees Of Tufts College Methods of preparing substituted tetracyclines with transition metal-based chemistries
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
US7202035B2 (en) * 1999-09-30 2007-04-10 University Of Guelph Genetic markers for skatole metabolism
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
ATE264295T1 (de) 2000-05-15 2004-04-15 Paratek Pharm Innc 7-substituierte kondensierte ring-tetrazyclin- verbindungen
US20020128237A1 (en) 2000-06-16 2002-09-12 Nelson Mark L. 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
EA201000496A1 (ru) * 2000-07-07 2010-10-29 Трастис Оф Тафтс Коллидж Замещенное соединение миноциклина, способ получения замещенных соединений миноциклина (варианты)
CZ2003343A3 (cs) 2000-07-07 2003-05-14 Trustees Of Tufts College 7-Substituované tetracyklinové sloučeniny
EP1303479B1 (en) * 2000-07-07 2011-04-06 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
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
AU2002250331A1 (en) 2001-03-13 2002-09-24 Paratek Pharmaceuticals, Inc. 7-pyrollyl tetracycline compounds and methods of use thereof
HRP20030743A2 (en) * 2001-03-13 2005-06-30 Paratek Pharmaceuticals 7,9-substituted tetracycline compounds
US7045507B2 (en) * 2001-03-14 2006-05-16 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds as synergistic antifungal agents
JP2004530661A (ja) * 2001-03-14 2004-10-07 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 抗真菌剤としての置換テトラサイクリン化合物
US8088820B2 (en) 2001-04-24 2012-01-03 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds for the treatment of malaria
ATE455092T1 (de) 2001-04-24 2010-01-15 Paratek Pharm Innc Substituierte tetracyclin-verbindungen zur behandlung von malaria
EP2332549A1 (en) 2001-07-13 2011-06-15 Paratek Pharmaceuticals, Inc. Novel tetracyclines and their use in medicine
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
US7056902B2 (en) 2002-01-08 2006-06-06 Paratek Pharmaceuticals, Inc. 4-dedimethylamino tetracycline compounds
EP2316450A1 (en) 2002-03-08 2011-05-04 Paratek Pharmaceuticals, Inc. Amino-methyl substituted tetracycline compounds
KR101083498B1 (ko) * 2002-03-21 2011-11-16 파라테크 파마슈티컬스, 인크. 치환된 테트라시클린 화합물
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
US8173624B2 (en) 2002-10-24 2012-05-08 Paratek Pharmaceuticals, Inc. Methods of using substituted tetracycline compounds to modulate RNA
EP1656341A1 (en) * 2003-07-09 2006-05-17 Paratek Pharmaceuticals, Inc. Prodrugs of 9-aminomethyl tetracycline compounds
CN1845897A (zh) * 2003-07-09 2006-10-11 帕拉特克药品公司 取代的四环素化合物
EP2332904A3 (en) 2004-01-15 2012-04-11 Paratek Pharmaceuticals, Inc. Derivatives of tetracycline compounds
EP2284151A3 (en) 2004-10-25 2011-09-21 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds
EP2301916A3 (en) 2004-10-25 2011-09-28 Paratek Pharmaceuticals, Inc. 4-aminotetracyclines and methods of use thereof
CA2616224A1 (en) * 2005-07-21 2007-02-01 Paratek Pharmaceuticals, Inc. 10-substituted tetracyclines and methods of use thereof

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JP5037436B2 (ja) 2012-09-26
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KR20030017610A (ko) 2003-03-03
BRPI0112269B8 (pt) 2021-05-25
AU2005201623B2 (en) 2009-02-12
EA201000496A1 (ru) 2010-10-29
US9090541B2 (en) 2015-07-28
US20030125348A1 (en) 2003-07-03
CY1107524T1 (el) 2013-03-13
HUP0301169A3 (en) 2009-08-28
DK1301467T3 (da) 2006-12-27
EP2308832B8 (en) 2019-04-24
JP2012107045A (ja) 2012-06-07
BR0112269A (pt) 2003-07-01
WO2002004406A2 (en) 2002-01-17
TW200519070A (en) 2005-06-16
MXPA03000055A (es) 2003-07-14
ATE336481T1 (de) 2006-09-15
US8258120B2 (en) 2012-09-04
BRPI0112269B1 (pt) 2016-07-05
CA2415178C (en) 2010-05-25
EP2308832A1 (en) 2011-04-13
US20150265635A1 (en) 2015-09-24
US20090325908A1 (en) 2009-12-31
HRP20030091B1 (en) 2011-10-31
PT1301467E (pt) 2006-12-29
AU8638801A (en) 2002-01-21
KR100674047B1 (ko) 2007-01-25
ZA200300749B (en) 2005-08-31
KR20060014446A (ko) 2006-02-15
CN100473644C (zh) 2009-04-01
EA200401579A1 (ru) 2005-06-30
US20120283201A1 (en) 2012-11-08
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AU2009201857B9 (en) 2012-05-10
EP3461808A1 (en) 2019-04-03
EA009175B1 (ru) 2007-12-28
EA013908B1 (ru) 2010-08-30
DE60122341D1 (de) 2006-09-28
EP2308832B1 (en) 2018-09-12
AU2005201623A1 (en) 2005-05-05
CN1690047B (zh) 2010-10-06
CZ303702B6 (cs) 2013-03-20
HUP0301169A2 (hu) 2003-08-28
ES2701599T3 (es) 2019-02-25
EP1679305B1 (en) 2012-02-08
JP4925549B2 (ja) 2012-04-25
ATE544745T1 (de) 2012-02-15
JP2004502752A (ja) 2004-01-29
HRP20030091A2 (en) 2005-02-28
EP1679305A1 (en) 2006-07-12
CN1690047A (zh) 2005-11-02
AU2001286388B2 (en) 2005-07-14
AU2009201857A1 (en) 2009-06-04
AU2009201857B2 (en) 2011-12-22
IL153639A0 (en) 2003-07-06
AU2009201857A8 (en) 2011-01-06
CZ2003344A3 (cs) 2003-05-14
CA2415178A1 (en) 2002-01-17
AU2005201623B8 (en) 2009-03-12
IL177854A0 (en) 2006-12-31
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HU229577B1 (en) 2014-02-28
CN1471509A (zh) 2004-01-28
EA200300135A1 (ru) 2003-06-26
ES2271070T3 (es) 2007-04-16
TWI299038B (en) 2008-07-21
US20040214801A1 (en) 2004-10-28
DE60122341T2 (de) 2007-08-09

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