CA2079703C - Novel 9-amino-7-substituted-6-demethyl-6-deoxytetracyclines - Google Patents

Novel 9-amino-7-substituted-6-demethyl-6-deoxytetracyclines Download PDF

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Publication number
CA2079703C
CA2079703C CA002079703A CA2079703A CA2079703C CA 2079703 C CA2079703 C CA 2079703C CA 002079703 A CA002079703 A CA 002079703A CA 2079703 A CA2079703 A CA 2079703A CA 2079703 C CA2079703 C CA 2079703C
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CA
Canada
Prior art keywords
methylpropyl
ethyl
amino
propyl
alkyl
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.)
Expired - Fee Related
Application number
CA002079703A
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English (en)
French (fr)
Other versions
CA2079703A1 (en
Inventor
Joseph J. Hlavka
Phaik-Eng Sum
Yakov Gluzman
Ving J. Lee
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Wyeth Holdings LLC
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Wyeth Holdings LLC
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Publication date
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Publication of CA2079703A1 publication Critical patent/CA2079703A1/en
Application granted granted Critical
Publication of CA2079703C publication Critical patent/CA2079703C/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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    • 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Oncology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Communicable Diseases (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Seasonings (AREA)
  • Peptides Or Proteins (AREA)
  • Quinoline Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Luminescent Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Spinning Or Twisting Of Yarns (AREA)
  • Moulding By Coating Moulds (AREA)
  • Tires In General (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CA002079703A 1991-10-04 1992-10-02 Novel 9-amino-7-substituted-6-demethyl-6-deoxytetracyclines Expired - Fee Related CA2079703C (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US07/771,697 US5281628A (en) 1991-10-04 1991-10-04 9-amino-7-(substituted)-6-demethyl-6-deoxytetracyclines
US07/771,697 1991-10-04

Publications (2)

Publication Number Publication Date
CA2079703A1 CA2079703A1 (en) 1993-04-05
CA2079703C true CA2079703C (en) 2004-07-20

Family

ID=25092681

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002079703A Expired - Fee Related CA2079703C (en) 1991-10-04 1992-10-02 Novel 9-amino-7-substituted-6-demethyl-6-deoxytetracyclines

Country Status (24)

Country Link
US (3) US5281628A (show.php)
EP (1) EP0535346B1 (show.php)
JP (1) JP3183729B2 (show.php)
KR (1) KR100261528B1 (show.php)
CN (1) CN1053182C (show.php)
AT (1) ATE129697T1 (show.php)
AU (1) AU651734B2 (show.php)
CA (1) CA2079703C (show.php)
CZ (1) CZ285015B6 (show.php)
DE (1) DE69205792T2 (show.php)
DK (1) DK0535346T3 (show.php)
ES (1) ES2081005T3 (show.php)
FI (1) FI111716B (show.php)
GR (1) GR3017978T3 (show.php)
HU (2) HU211214B (show.php)
IL (1) IL103319A (show.php)
MX (1) MX9205573A (show.php)
NO (1) NO300129B1 (show.php)
NZ (1) NZ244556A (show.php)
PH (1) PH30343A (show.php)
PL (2) PL170933B1 (show.php)
SK (1) SK281113B6 (show.php)
TW (1) TW222616B (show.php)
ZA (1) ZA927608B (show.php)

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US5328902A (en) * 1992-08-13 1994-07-12 American Cyanamid Co. 7-(substituted)-9-[(substituted glycyl)amido]-6-demethyl-6-deoxytetracyclines
US5442059A (en) * 1992-08-13 1995-08-15 American Cyanamid Company 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
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
NZ506058A (en) * 1998-01-23 2003-04-29 Tufts College Antibacterial 9-substituted tetracyclines, and pharmaceuticals and uses thereof
US8106225B2 (en) * 1999-09-14 2012-01-31 Trustees Of Tufts College Methods of preparing substituted tetracyclines with transition metal-based chemistries
CN1399627A (zh) * 1999-09-14 2003-02-26 塔夫茨大学信托人 用基于过渡金属的化学制备取代四环素的方法
US6686365B2 (en) * 2000-02-04 2004-02-03 Eli Lilly And Company Pharmaceutical composition
US20020132798A1 (en) * 2000-06-16 2002-09-19 Nelson Mark L. 7-phenyl-substituted tetracycline compounds
WO2001098236A2 (en) * 2000-06-16 2001-12-27 Trustees Of Tufts College 7-phenyl-substituted tetracycline compounds
US7094806B2 (en) 2000-07-07 2006-08-22 Trustees Of Tufts College 7, 8 and 9-substituted tetracycline compounds
BRPI0112269B8 (pt) 2000-07-07 2021-05-25 Paratek Pharm Innc composto de minociclina 9-aminometila substituída, e, composição farmacêutica
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
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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
US7553828B2 (en) * 2001-03-13 2009-06-30 Paratek Pharmaceuticals, Inc. 9-aminomethyl substituted minocycline compounds
EP2329828A1 (en) 2001-07-13 2011-06-08 Paratek Pharmaceuticals, Inc. Tetracyclines for the treatment of ischaemia
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
US20030181371A1 (en) * 2001-12-28 2003-09-25 Angiotech Pharmaceuticals, Inc. Compositions and methods of using collajolie
EP2311798A1 (en) * 2002-01-08 2011-04-20 Paratek Pharmaceuticals, Inc. 4-dedimethylamino tetracycline compounds
EP1482926A4 (en) * 2002-03-08 2006-04-12 Paratek Pharm Innc AMINO METHYL SUBSTITUTED TETRACYCLINE COMPOUNDS
WO2003079984A2 (en) 2002-03-21 2003-10-02 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds
WO2004006850A2 (en) 2002-07-12 2004-01-22 Paratek Pharmaceuticals, Inc 3, 10, AND 12a SUBSTITUTED TETRACYCLINE COMPOUNDS
BR0317715A (pt) * 2002-12-27 2005-11-22 Angiotech Int Ag Composições e processos de uso de collajolie
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
US20060287283A1 (en) * 2003-07-09 2006-12-21 Paratek Pharmaceuticals, Inc. Prodrugs of 9-aminomethyl tetracycline compounds
EP1716101A1 (en) * 2004-01-15 2006-11-02 Paratek Pharmaceuticals, Inc. Aromatic a-ring derivatives of tetracycline compounds
US8466132B2 (en) 2004-10-25 2013-06-18 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds
WO2006047671A2 (en) 2004-10-25 2006-05-04 Paratek Pharmaceuticals, Inc. 4-aminotetracyclines and methods of use thereof
AU2006210406C1 (en) * 2005-02-04 2013-03-07 Paratek Pharmaceuticals, Inc. 11a, 12-derivatives of tetracycline compounds
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
AR057034A1 (es) * 2005-05-27 2007-11-14 Wyeth Corp Metodos para purificar tigeciclina
AR057032A1 (es) * 2005-05-27 2007-11-14 Wyeth Corp Tigeciclina y metodos de preparacion
EP1910273A2 (en) * 2005-07-21 2008-04-16 Paratek Pharmaceuticals, Inc. 10-substituted tetracyclines and methods of use thereof
EP1965770A2 (en) * 2005-12-22 2008-09-10 Wyeth a Corporation of the State of Delaware Oral formulations comprising tigecycline
JP2009521456A (ja) * 2005-12-22 2009-06-04 ワイス チゲサイクリンでの胃腸管感染症の治療法
WO2007120913A2 (en) * 2006-04-17 2007-10-25 Teva Pharmaceutical Industries Ltd. Isolation of tetracycline derivatives
SI2016045T1 (sl) * 2006-04-24 2015-03-31 Teva Pharmaceutical Industries, Ltd. 5 Basel Street Kristalinična oblika tigeciklina in postopek za njegovo pripravo
US8198470B2 (en) * 2006-04-24 2012-06-12 Teva Pharmaceutical Industries Ltd. Crystalline form II of tigecycline and processes for preparation thereof
US20080146843A1 (en) * 2006-05-10 2008-06-19 Teva Pharmaceutical Industries Ltd. Methods for reducing 7/9-nitrotetracycline derivatives
EP2431469A3 (en) 2006-05-15 2012-05-30 Paratek Pharmaceuticals, Inc. Methods of regulating expression of genes or of gene products using substituted tetracycline compounds
EP2086926A2 (en) 2006-11-29 2009-08-12 Teva Pharmaceutical Industries Ltd. Crystalline forms of tigecycline and processes for preparation thereof
BRPI0706517A2 (pt) * 2006-11-30 2011-03-29 Teva Pharma processos para preparação de f 9-haloacetamidominociclinas
EP2114865A1 (en) * 2007-03-01 2009-11-11 Teva Pharmaceutical Industries Ltd. Processes for purification of tigecycline
HRP20120735T1 (hr) 2007-11-29 2012-10-31 Actelion Pharmaceuticals Ltd. Derivati fosfonske kiseline i njihova uporaba kao antagonista p2y12 receptora
WO2010032219A1 (en) * 2008-09-18 2010-03-25 Ranbaxy Laboratories Limited Process for the preparation of tigecycline
JP2012520305A (ja) * 2009-03-12 2012-09-06 ワイス・エルエルシー テトラサイクリンのニトロ化
PL2327676T3 (pl) * 2009-11-26 2014-08-29 Sandoz Ag Reakcja związków organicznych z małymi ilościami wodoru

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Also Published As

Publication number Publication date
AU2618292A (en) 1993-04-08
AU651734B2 (en) 1994-07-28
CA2079703A1 (en) 1993-04-05
SK297292A3 (en) 1994-12-07
HU9203143D0 (en) 1992-12-28
HK1000319A1 (en) 1998-02-27
TW222616B (show.php) 1994-04-21
CN1071415A (zh) 1993-04-28
HUT64298A (en) 1993-12-28
FI111716B (fi) 2003-09-15
HU211922A9 (en) 1996-01-29
US5326759A (en) 1994-07-05
PL170933B1 (pl) 1997-02-28
ES2081005T3 (es) 1996-02-16
CZ285015B6 (cs) 1999-05-12
FI924453L (fi) 1993-04-05
DE69205792D1 (de) 1995-12-07
HU211214B (en) 1995-11-28
IL103319A (en) 1996-07-23
EP0535346A1 (en) 1993-04-07
KR100261528B1 (ko) 2000-07-15
EP0535346B1 (en) 1995-11-02
NO923856L (no) 1993-04-05
SK281113B6 (sk) 2000-12-11
JPH05239006A (ja) 1993-09-17
PL296140A1 (en) 1993-11-02
NO923856D0 (no) 1992-10-02
GR3017978T3 (en) 1996-02-29
ATE129697T1 (de) 1995-11-15
DK0535346T3 (da) 1995-12-04
PH30343A (en) 1997-04-02
US5401863A (en) 1995-03-28
DE69205792T2 (de) 1996-06-20
NZ244556A (en) 1994-06-27
CN1053182C (zh) 2000-06-07
ZA927608B (en) 1993-04-13
CZ297292A3 (en) 1993-04-14
PL170939B1 (pl) 1997-02-28
US5281628A (en) 1994-01-25
IL103319A0 (en) 1993-03-15
KR930007895A (ko) 1993-05-20
NO300129B1 (no) 1997-04-14
MX9205573A (es) 1993-05-01
JP3183729B2 (ja) 2001-07-09
FI924453A0 (fi) 1992-10-02

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