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GB921252A - New tetracycline derivatives - Google Patents

New tetracycline derivatives

Info

Publication number
GB921252A
GB921252A GB8743/61A GB874361A GB921252A GB 921252 A GB921252 A GB 921252A GB 8743/61 A GB8743/61 A GB 8743/61A GB 874361 A GB874361 A GB 874361A GB 921252 A GB921252 A GB 921252A
Authority
GB
United Kingdom
Prior art keywords
tetracycline
amides
hydrogen
amino acid
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
Application number
GB8743/61A
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.)
Pfizer Italia SRL
Original Assignee
Carlo Erba SpA
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 Carlo Erba SpA filed Critical Carlo Erba SpA
Publication of GB921252A publication Critical patent/GB921252A/en
Expired legal-status Critical Current

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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00Preparation of carboxylic acid amides
    • C07C231/12Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C243/00Compounds containing chains of nitrogen atoms singly-bound to each other, e.g. hydrazines, triazanes
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

The invention relates to water-soluble tetracycline derivatives of the formula: -T-CH2-NH-CH(R)-CONR1R2 where T is a radical derived from tetracycline, oxytetracycline, chlortetracycline, demethyl tetracycline or demethyl chlortetracycline by removal of a hydrogen atom and R is hydrogen, alkyl, or substituted alkyl such that the compound RCH(NH2)COOH is a known, naturally occurring amino acid and R1 and R2 may be the same or different and represent hydrogen, alkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl or dialkylaminoalkyl or R1 is hydrogen and R2 is amino, which are obtainable by the condensation of a said tetracycline with formaldehyde e.g. as formalin or trioxane and an amide of an a -amino acid of the formula:-R-CH(NH2)-CONR1R2 where R, R1 and R2 are as before. Preferably R is such that RCH(NH2)COOH is glycine, alanine, serine or lysine. Preferred a -amino acid amides are the unsubstituted amides, the N-(b -hydroxyethyl)- and N,N-di(b -hydroxyethyl)amides and the N or N,N mono or dimethyl or ethyl amides of glycine, alanine, serine or lysine. The above compounds may be formulated as pharmaceutical compositions preferably for oral or parenteral administration in association with a pharmaceutical carrier. The compositions may be prepared as tablets, pills or powders which may be encapsulated or the active ingredients may be incorporated in a syrup base or dissolved in water or physiological saline and filled into ampoules.
GB8743/61A 1960-03-09 1961-03-09 New tetracycline derivatives Expired GB921252A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
IT406560 1960-03-09

Publications (1)

Publication Number Publication Date
GB921252A true GB921252A (en) 1963-03-20

Family

ID=11112045

Family Applications (1)

Application Number Title Priority Date Filing Date
GB8743/61A Expired GB921252A (en) 1960-03-09 1961-03-09 New tetracycline derivatives

Country Status (2)

Country Link
FR (1) FR1003M (en)
GB (1) GB921252A (en)

Cited By (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2004502752A (en) * 2000-07-07 2004-01-29 トラスティーズ・オブ・タフツ・カレッジ 9-substituted minocycline compounds
WO2003075857A3 (en) * 2002-03-08 2004-02-05 Paratek Pharm Innc Amino-methyl substituted tetracycline compounds
US7208482B2 (en) 2001-03-13 2007-04-24 Paratek Pharmaceuticals, Inc. 9-aminoacyl tetracycline compounds and methods of use thereof
US7323492B2 (en) 2001-08-02 2008-01-29 Paratek Pharmaceuticals, Inc. 7-pyrollyl 9-aminoacyl tetracycline compounds and methods of use thereof
US7521437B2 (en) 2000-06-16 2009-04-21 Trustees Of Tufts College 7-phenyl-substituted tetracycline compounds
US7553828B2 (en) 2001-03-13 2009-06-30 Paratek Pharmaceuticals, Inc. 9-aminomethyl substituted minocycline compounds
US7612053B2 (en) 2000-05-15 2009-11-03 Paratek Pharmaceuticals, Inc. 7-Substituted fused ring tetracycline compounds
US7696187B2 (en) 1999-09-14 2010-04-13 Trustees Of Tufts College Methods of preparing substituted tetracyclines with transition metal-based chemistries
US7696358B2 (en) 2001-03-13 2010-04-13 Paratek Pharmaceuticals, Inc. Five-membered heterocyclyl tetracycline compounds and methods of use thereof
US7696186B2 (en) 2001-03-13 2010-04-13 Paratek Pharmaceuticals, Inc. 7,9-substituted tetracycline compounds
US7820641B2 (en) 2002-03-21 2010-10-26 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds
US8106225B2 (en) * 1999-09-14 2012-01-31 Trustees Of Tufts College Methods of preparing substituted tetracyclines with transition metal-based chemistries
US8318706B2 (en) 2006-12-21 2012-11-27 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds
US8513223B2 (en) 2006-12-21 2013-08-20 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds for treatment of inflammatory skin disorders
US8518912B2 (en) 2007-11-29 2013-08-27 Actelion Pharmaceuticals Ltd. Phosphonic acid derivates and their use as P2Y12 receptor antagonists
US9533943B2 (en) 2003-07-09 2017-01-03 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds

Cited By (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8106225B2 (en) * 1999-09-14 2012-01-31 Trustees Of Tufts College Methods of preparing substituted tetracyclines with transition metal-based chemistries
US7696187B2 (en) 1999-09-14 2010-04-13 Trustees Of Tufts College Methods of preparing substituted tetracyclines with transition metal-based chemistries
US7612053B2 (en) 2000-05-15 2009-11-03 Paratek Pharmaceuticals, Inc. 7-Substituted fused ring tetracycline compounds
US8288570B2 (en) 2000-05-15 2012-10-16 Paratek Pharmaceuticals, Inc. 7-iodo tetracyclines and related methods
US7893282B2 (en) 2000-05-15 2011-02-22 Paratek Pharmaceuticals, Inc. 7-substituted fused ring tetracycline compounds
US8168810B2 (en) 2000-06-16 2012-05-01 Trustees Of Tufts College 7-phenyl-substituted tetracycline compounds
US7851460B2 (en) 2000-06-16 2010-12-14 Trustees Of Tufts College 7-phenyl-substituted tetracycline compounds
US7521437B2 (en) 2000-06-16 2009-04-21 Trustees Of Tufts College 7-phenyl-substituted tetracycline compounds
US8258120B2 (en) 2000-07-07 2012-09-04 Paratek Pharmaceuticals, Inc. 9-substituted minocycline compounds
JP2009029785A (en) * 2000-07-07 2009-02-12 Tufts College 9-Substituted minocycline compounds
US9090541B2 (en) 2000-07-07 2015-07-28 Paratek Pharmaceuticals, Inc. 9-substituted minocycline compounds
US8048867B2 (en) 2000-07-07 2011-11-01 Trustees Of Tufts College 9-substituted minocycline compounds
JP2004502752A (en) * 2000-07-07 2004-01-29 トラスティーズ・オブ・タフツ・カレッジ 9-substituted minocycline compounds
US7553828B2 (en) 2001-03-13 2009-06-30 Paratek Pharmaceuticals, Inc. 9-aminomethyl substituted minocycline compounds
US8304445B2 (en) 2001-03-13 2012-11-06 Paratek Pharmaceuticals, Inc. 7-pyrazolyl tetracycline compounds and methods of use thereof
US7208482B2 (en) 2001-03-13 2007-04-24 Paratek Pharmaceuticals, Inc. 9-aminoacyl tetracycline compounds and methods of use thereof
US7696186B2 (en) 2001-03-13 2010-04-13 Paratek Pharmaceuticals, Inc. 7,9-substituted tetracycline compounds
US7696358B2 (en) 2001-03-13 2010-04-13 Paratek Pharmaceuticals, Inc. Five-membered heterocyclyl tetracycline compounds and methods of use thereof
US7897784B2 (en) 2001-03-13 2011-03-01 Paratek Pharmaceuticals, Inc. Process for preparing five-membered heterocyclyl tetracycline compounds and methods of use thereof
US9365500B2 (en) 2001-03-13 2016-06-14 Paratek Pharmaceuticals, Inc. 9-aminomethyl substituted minocycline compounds
US8101591B2 (en) 2001-03-13 2012-01-24 Paratek Pharmaceuticals, Inc. 9-aminoacyl tetracycline compounds and methods of use thereof
US7652002B2 (en) 2001-03-13 2010-01-26 Paratek Pharmaceuticals, Inc. 9-aminoacyl tetracycline compounds and methods of use thereof
US7323492B2 (en) 2001-08-02 2008-01-29 Paratek Pharmaceuticals, Inc. 7-pyrollyl 9-aminoacyl tetracycline compounds and methods of use thereof
US8211937B2 (en) 2001-08-02 2012-07-03 Paratek Pharmaceuticals, Inc. 7-pyrollyl 9-aminoacyl tetracycline compounds and methods of use thereof
US7326696B2 (en) 2002-03-08 2008-02-05 Paratek Pharmaceuticals, Inc. Amino-methyl substituted tetracycline compounds
WO2003075857A3 (en) * 2002-03-08 2004-02-05 Paratek Pharm Innc Amino-methyl substituted tetracycline compounds
EA013819B1 (en) * 2002-03-08 2010-08-30 Паратек Фармасьютикалс, Инк. Amino-methyl substituted tetracycline compounds
AU2003220123B2 (en) * 2002-03-08 2009-05-07 Paratek Pharmaceuticals, Inc. Amino-methyl substituted tetracycline compounds
US7820641B2 (en) 2002-03-21 2010-10-26 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds
US9533943B2 (en) 2003-07-09 2017-01-03 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds
US9012433B2 (en) 2006-12-21 2015-04-21 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds
US8513223B2 (en) 2006-12-21 2013-08-20 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds for treatment of inflammatory skin disorders
US8318706B2 (en) 2006-12-21 2012-11-27 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds
US9481639B2 (en) 2006-12-21 2016-11-01 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds for treatment of inflammatory skin disorders
US8518912B2 (en) 2007-11-29 2013-08-27 Actelion Pharmaceuticals Ltd. Phosphonic acid derivates and their use as P2Y12 receptor antagonists

Also Published As

Publication number Publication date
FR1003M (en) 1961-12-18

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