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

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

Info

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
Authority
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
Other languages
English (en)
French (fr)
Other versions
CA2079703A1 (en
Inventor
Joseph J. Hlavka
Phaik-Eng Sum
Yakov Gluzman
Ving J. Lee
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Wyeth Holdings LLC
Original Assignee
Wyeth Holdings LLC
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 Wyeth Holdings LLC filed Critical Wyeth Holdings LLC
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

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/24—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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/02—Ortho- or ortho- and peri-condensed systems
    • C07C2603/40—Ortho- or ortho- and peri-condensed systems containing four condensed rings
    • C07C2603/42—Ortho- or ortho- and peri-condensed systems containing four condensed rings containing only six-membered rings
    • C07C2603/44—Naphthacenes; Hydrogenated naphthacenes
    • C07C2603/46—1,4,4a,5,5a,6,11,12a- Octahydronaphthacenes, e.g. tetracyclines

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (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)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Luminescent Compositions (AREA)
  • Peptides Or Proteins (AREA)
  • Quinoline Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Moulding By Coating Moulds (AREA)
  • Tires In General (AREA)
  • Spinning Or Twisting Of Yarns (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 1991-10-04
US07/771,697 US5281628A (en) 1991-10-04 1991-10-04 9-amino-7-(substituted)-6-demethyl-6-deoxytetracyclines

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 (25)

Country Link
US (3) US5281628A (cg-RX-API-DMAC10.html)
EP (1) EP0535346B1 (cg-RX-API-DMAC10.html)
JP (1) JP3183729B2 (cg-RX-API-DMAC10.html)
KR (1) KR100261528B1 (cg-RX-API-DMAC10.html)
CN (1) CN1053182C (cg-RX-API-DMAC10.html)
AT (1) ATE129697T1 (cg-RX-API-DMAC10.html)
AU (1) AU651734B2 (cg-RX-API-DMAC10.html)
CA (1) CA2079703C (cg-RX-API-DMAC10.html)
CZ (1) CZ285015B6 (cg-RX-API-DMAC10.html)
DE (1) DE69205792T2 (cg-RX-API-DMAC10.html)
DK (1) DK0535346T3 (cg-RX-API-DMAC10.html)
ES (1) ES2081005T3 (cg-RX-API-DMAC10.html)
FI (1) FI111716B (cg-RX-API-DMAC10.html)
GR (1) GR3017978T3 (cg-RX-API-DMAC10.html)
HK (1) HK1000319A1 (cg-RX-API-DMAC10.html)
HU (2) HU211214B (cg-RX-API-DMAC10.html)
IL (1) IL103319A (cg-RX-API-DMAC10.html)
MX (1) MX9205573A (cg-RX-API-DMAC10.html)
NO (1) NO300129B1 (cg-RX-API-DMAC10.html)
NZ (1) NZ244556A (cg-RX-API-DMAC10.html)
PH (1) PH30343A (cg-RX-API-DMAC10.html)
PL (2) PL170933B1 (cg-RX-API-DMAC10.html)
SK (1) SK281113B6 (cg-RX-API-DMAC10.html)
TW (1) TW222616B (cg-RX-API-DMAC10.html)
ZA (1) ZA927608B (cg-RX-API-DMAC10.html)

Families Citing this family (55)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
DK0643775T3 (da) * 1992-05-28 2004-09-06 Ct For Molecular Biology And M Quinonderivater til forbedring af cellebioenergi
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
US5442059A (en) * 1992-08-13 1995-08-15 American Cyanamid Company 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
WO1999037307A1 (en) * 1998-01-23 1999-07-29 Trustees Of Tufts College Pharmaceutically active compounds and methods of use thereof
JP5093953B2 (ja) * 1999-09-14 2012-12-12 トラスティーズ オブ タフツ カレッジ 遷移金属を用いた化学反応による置換テトラサイクリンの調製方法
US8106225B2 (en) * 1999-09-14 2012-01-31 Trustees Of Tufts College Methods of preparing substituted tetracyclines with transition metal-based chemistries
US6686365B2 (en) * 2000-02-04 2004-02-03 Eli Lilly And Company Pharmaceutical composition
US20020128238A1 (en) * 2000-06-16 2002-09-12 Nelson Mark L. 7-phenyl-substituted tetracycline compounds
US20020132798A1 (en) * 2000-06-16 2002-09-19 Nelson Mark L. 7-phenyl-substituted tetracycline compounds
US7094806B2 (en) 2000-07-07 2006-08-22 Trustees Of Tufts College 7, 8 and 9-substituted tetracycline compounds
CZ2003343A3 (cs) * 2000-07-07 2003-05-14 Trustees Of Tufts College 7-Substituované tetracyklinové sloučeniny
EA013908B1 (ru) 2000-07-07 2010-08-30 Трастис Оф Тафтс Коллидж Замещенные соединения миноциклина (варианты), фармацевтическая композиция и способ лечения чувствительного к тетрациклину состояния млекопитающего
EP2298732A1 (en) * 2001-03-13 2011-03-23 Paratek Pharmaceuticals, Inc. 7,9-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
EP1241160A1 (en) * 2001-03-13 2002-09-18 Glaxo Group Limited Tetracycline derivatives and their use as antibiotic agents
US20060194773A1 (en) * 2001-07-13 2006-08-31 Paratek Pharmaceuticals, Inc. Tetracyline compounds having target therapeutic activities
WO2003005971A2 (en) 2001-07-13 2003-01-23 Paratek Pharmaceuticals, Inc. Tetracycline 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
JP2005526754A (ja) * 2002-03-08 2005-09-08 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 アミノメチル置換されたテトラサイクリン化合物
CN1653037A (zh) 2002-03-21 2005-08-10 帕拉特克药品公司 取代的四环素化合物
EA200900540A1 (ru) 2002-07-12 2009-12-30 Пэрэтек Фамэсьютикэлс, Инк. Замещённые соединения тетрациклина, фармацевтическая композиция и способ лечения чувствительного к тетрациклину состояния у субъекта
WO2004060425A2 (en) * 2002-12-27 2004-07-22 Angiotech International Ag Compositions and methods of using collagen and mmpi
US20060287283A1 (en) * 2003-07-09 2006-12-21 Paratek Pharmaceuticals, Inc. Prodrugs of 9-aminomethyl tetracycline compounds
EP2295404A3 (en) 2003-07-09 2011-05-11 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds
WO2005070878A1 (en) * 2004-01-15 2005-08-04 Paratek Pharmaceuticals, Inc. Aromatic a-ring derivatives of tetracycline compounds
AU2005299294B2 (en) 2004-10-25 2012-06-07 Paratek Pharmaceuticals, Inc. 4-aminotetracyclines and methods of use thereof
EP2284151A3 (en) 2004-10-25 2011-09-21 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds
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
AR057034A1 (es) * 2005-05-27 2007-11-14 Wyeth Corp Metodos para purificar tigeciclina
AR057033A1 (es) * 2005-05-27 2007-11-14 Wyeth Corp Tigeciclina y metodos para preparar 9-nitrominociclina
AR057032A1 (es) * 2005-05-27 2007-11-14 Wyeth Corp Tigeciclina y metodos de preparacion
JP2009502809A (ja) * 2005-07-21 2009-01-29 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 １０−置換テトラサイクリンおよびその使用方法
CA2632213A1 (en) * 2005-12-22 2007-07-05 Wyeth 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
US20070244335A1 (en) * 2006-04-17 2007-10-18 Teva Pharmaceutical Industries Ltd. Isolation of tetracycline derivatives
DE202007019460U1 (de) * 2006-04-24 2012-10-24 Teva Pharmaceutical Industries Ltd. Kristalline Tigecyclin-Formen
US8198470B2 (en) * 2006-04-24 2012-06-12 Teva Pharmaceutical Industries Ltd. Crystalline form II of tigecycline and processes for preparation thereof
CA2649660A1 (en) * 2006-05-10 2007-11-22 Teva Pharmaceutical Industries Ltd. Methods for reducing 7/9-nitrotetracycline derivatives
WO2007133797A2 (en) 2006-05-15 2007-11-22 Paratek Pharmaceuticals, Inc. Methods of regulating expression of genes or of gene products using substituted tetracycline compounds
US8198469B2 (en) 2006-11-29 2012-06-12 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
WO2008106234A1 (en) * 2007-03-01 2008-09-04 Teva Pharmaceutical Industries Ltd. Processes for purification of tigecycline
US8518912B2 (en) 2007-11-29 2013-08-27 Actelion Pharmaceuticals Ltd. Phosphonic acid derivates and their use as P2Y12 receptor antagonists
WO2010032219A1 (en) * 2008-09-18 2010-03-25 Ranbaxy Laboratories Limited Process for the preparation of tigecycline
CA2751238A1 (en) * 2009-03-12 2010-10-07 Wyeth Llc Nitration of tetracyclines
ES2469829T3 (es) * 2009-11-26 2014-06-20 Sandoz Ag Reacción de compuestos orgánicos con bajas cantidades de hidrógeno

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
USRE26271E (en) * 1967-09-26 Reductive alkylation process
US2482055A (en) * 1948-02-11 1949-09-13 American Cyanamid Co Aureomycin and preparation of same
US2997471A (en) * 1958-08-18 1961-08-22 Bristol Myers Co Tetracycline derivatives
US3007965A (en) * 1959-02-13 1961-11-07 American Cyanamid Co New tetracyclines produced by streptomyces aureofaciens
US3043875A (en) * 1959-10-22 1962-07-10 Pfizer & Co C Halogenated tetracycline derivatives and processes for their preparation
FR1430859A (cg-RX-API-DMAC10.html) * 1960-05-23 1966-05-25
US3338963A (en) * 1960-10-28 1967-08-29 American Cyanamid Co Tetracycline compounds
US3148212A (en) 1961-12-22 1964-09-08 American Cyanamid Co Reductive alkylation process
US3360557A (en) * 1963-05-10 1967-12-26 American Cyanamid Co 9-hydroxytetracyclines and a process of preparing same
USRE26253E (en) * 1963-05-17 1967-08-15 And z-alkylamino-g-deoxytetracycline
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
US3373198A (en) * 1967-04-27 1968-03-12 American Cyanamid Co Substituted 5a, 11a-dehydro-6-epitetracyclines
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
NL158172B (nl) * 1972-09-18 1978-10-16 Farmaceutici Italia Werkwijze voor het bereiden van tetracyclinederivaten met een substituent op de 7-plaats.
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
US5202449A (en) * 1987-07-28 1993-04-13 Nippon Kayaku Kabushiki Kaisha Process for purifying 7-dimethylamino-6-demethyl-6-deoxytetracycline
JPH04295458A (ja) * 1991-03-22 1992-10-20 Fuji Photo Film Co Ltd 光照射により酸を発生する化合物
US5141960A (en) * 1991-06-25 1992-08-25 G. D. Searle & Co. Tricyclic glycinamide derivatives as anti-convulsants
US5258398A (en) * 1991-12-16 1993-11-02 Rhone-Poulenc Rorer Pharmaceuticals Inc. Antithrombotic diaminoalkanoic acid derivatives

Also Published As

Publication number Publication date
CN1071415A (zh) 1993-04-28
ES2081005T3 (es) 1996-02-16
JP3183729B2 (ja) 2001-07-09
FI111716B (fi) 2003-09-15
EP0535346B1 (en) 1995-11-02
CZ285015B6 (cs) 1999-05-12
TW222616B (cg-RX-API-DMAC10.html) 1994-04-21
ZA927608B (en) 1993-04-13
HUT64298A (en) 1993-12-28
PL296140A1 (en) 1993-11-02
CZ297292A3 (en) 1993-04-14
IL103319A (en) 1996-07-23
PH30343A (en) 1997-04-02
GR3017978T3 (en) 1996-02-29
MX9205573A (es) 1993-05-01
NO300129B1 (no) 1997-04-14
PL170939B1 (pl) 1997-02-28
US5326759A (en) 1994-07-05
US5401863A (en) 1995-03-28
KR100261528B1 (ko) 2000-07-15
HU9203143D0 (en) 1992-12-28
DE69205792T2 (de) 1996-06-20
HU211922A9 (en) 1996-01-29
SK281113B6 (sk) 2000-12-11
IL103319A0 (en) 1993-03-15
NZ244556A (en) 1994-06-27
JPH05239006A (ja) 1993-09-17
HU211214B (en) 1995-11-28
NO923856D0 (no) 1992-10-02
SK297292A3 (en) 1994-12-07
AU2618292A (en) 1993-04-08
NO923856L (no) 1993-04-05
HK1000319A1 (en) 1998-02-27
EP0535346A1 (en) 1993-04-07
US5281628A (en) 1994-01-25
PL170933B1 (pl) 1997-02-28
AU651734B2 (en) 1994-07-28
CA2079703A1 (en) 1993-04-05
FI924453L (fi) 1993-04-05
ATE129697T1 (de) 1995-11-15
DK0535346T3 (da) 1995-12-04
KR930007895A (ko) 1993-05-20
CN1053182C (zh) 2000-06-07
FI924453A0 (fi) 1992-10-02
DE69205792D1 (de) 1995-12-07

Similar Documents

Publication Publication Date Title
CA2079703C (en) Novel 9-amino-7-substituted-6-demethyl-6-deoxytetracyclines
HK1000319B (en) 9-amino-7-substituted-6-demethyl-6-deoxytetracyclines
CA2383364C (en) Methods of preparing substituted tetracyclines with transition metal-based chemistries
CA2462572C (en) Tetracycline derivatives and methods of use thereof
EP0536515B1 (en) Novel 7-substituted-9-substituted amino-6-demethyl-6-deoxytetracyclines
US20130029943A1 (en) Methods of Preparing Substituted Tetracyclines with Transition Metal-Based Chemistries
WO1999037307A1 (en) Pharmaceutically active compounds and methods of use thereof
US7812008B2 (en) 9-substituted tetracyclines
HK1011348B (en) Novel 7-substituted-9-substituted amino-6-demethyl-6-deoxytetracyclines

Legal Events

Date Code Title Description
EEER Examination request
MKLA Lapsed