FI114911B - Menetelmä uusien terapeuttisesti käyttökelpoisten 7-substituoitu-9-(substituoitu amino)-6-demetyyli-6-deoksitetrasykliinien valmistamiseksi sekä menetelmässä käytettävät välituotteet - Google Patents

Menetelmä uusien terapeuttisesti käyttökelpoisten 7-substituoitu-9-(substituoitu amino)-6-demetyyli-6-deoksitetrasykliinien valmistamiseksi sekä menetelmässä käytettävät välituotteet Download PDF

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Publication number
FI114911B
FI114911B FI924454A FI924454A FI114911B FI 114911 B FI114911 B FI 114911B FI 924454 A FI924454 A FI 924454A FI 924454 A FI924454 A FI 924454A FI 114911 B FI114911 B FI 114911B
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FI
Finland
Prior art keywords
amino
dimethylamino
group
dioxo
bis
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FI924454A
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English (en)
Finnish (fi)
Swedish (sv)
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FI924454A0 (fi
FI924454A (fi
Inventor
Phaik-Eng Sum
Ving J Lee
Joseph J Hlavka
Yakov Gluzman
Adma A Ross
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Wyeth Corp
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Publication of FI924454A0 publication Critical patent/FI924454A0/fi
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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
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • 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
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D205/00Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • 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
    • C07D277/44Acylated amino or imino radicals
    • C07D277/46Acylated amino or imino radicals by carboxylic acids, or sulfur or nitrogen analogues thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/56Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom 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
    • C07D307/68Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/06Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
    • C07D333/24Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom 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
    • C07D333/30Hetero atoms other than halogen
    • C07D333/34Sulfur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom 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
    • C07D333/38Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Oncology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Communicable Diseases (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Moulding By Coating Moulds (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Furan Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Transition And Organic Metals Composition Catalysts For Addition Polymerization (AREA)
  • Hydrogenated Pyridines (AREA)
  • Saccharide Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
FI924454A 1991-10-04 1992-10-02 Menetelmä uusien terapeuttisesti käyttökelpoisten 7-substituoitu-9-(substituoitu amino)-6-demetyyli-6-deoksitetrasykliinien valmistamiseksi sekä menetelmässä käytettävät välituotteet FI114911B (fi)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US77157691A 1991-10-04 1991-10-04
US77157691 1991-10-04

Publications (3)

Publication Number Publication Date
FI924454A0 FI924454A0 (fi) 1992-10-02
FI924454A FI924454A (fi) 1993-04-05
FI114911B true FI114911B (fi) 2005-01-31

Family

ID=25092264

Family Applications (1)

Application Number Title Priority Date Filing Date
FI924454A FI114911B (fi) 1991-10-04 1992-10-02 Menetelmä uusien terapeuttisesti käyttökelpoisten 7-substituoitu-9-(substituoitu amino)-6-demetyyli-6-deoksitetrasykliinien valmistamiseksi sekä menetelmässä käytettävät välituotteet

Country Status (28)

Country Link
EP (1) EP0536515B1 (cs)
JP (1) JP3186863B2 (cs)
KR (1) KR100269072B1 (cs)
CN (1) CN1048240C (cs)
AT (1) ATE211128T1 (cs)
AU (1) AU654049B2 (cs)
BR (1) BR1100853A (cs)
CA (1) CA2079692C (cs)
CL (1) CL2004001623A1 (cs)
CZ (2) CZ284159B6 (cs)
DE (4) DE69232302D1 (cs)
DK (1) DK0536515T3 (cs)
ES (1) ES2168254T3 (cs)
FI (1) FI114911B (cs)
HK (1) HK1011348A1 (cs)
HU (2) HU219973B (cs)
IL (3) IL119590A (cs)
LU (1) LU91279I2 (cs)
MX (1) MX9205532A (cs)
NL (1) NL300244I2 (cs)
NO (3) NO301472B1 (cs)
NZ (1) NZ244585A (cs)
PL (4) PL175957B1 (cs)
PT (1) PT536515E (cs)
SG (1) SG52361A1 (cs)
SK (2) SK284826B6 (cs)
TW (1) TW275616B (cs)
ZA (1) ZA927607B (cs)

Families Citing this family (39)

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US5420272A (en) * 1992-08-13 1995-05-30 American Cyanamid Company 7-(substituted)-8-(substituted)-9-](substituted glycyl)amido]-6-demethyl-6-deoxytetracyclines
US5328902A (en) * 1992-08-13 1994-07-12 American Cyanamid Co. 7-(substituted)-9-[(substituted glycyl)amido]-6-demethyl-6-deoxytetracyclines
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
US5834450A (en) * 1994-02-17 1998-11-10 Pfizer Inc. 9- (substituted amino) -alpha-6-deoxy-5-oxy tetracycline derivatives, their preparation and their use as antibiotics
US8106225B2 (en) 1999-09-14 2012-01-31 Trustees Of Tufts College Methods of preparing substituted tetracyclines with transition metal-based chemistries
CA2672722C (en) 1999-09-14 2013-11-05 Trustees Of Tufts College Methods of preparing substituted tetracyclines with transition metal-based chemistries
CN1430600A (zh) * 2000-03-31 2003-07-16 塔夫茨大学信托人 7-和9-氨基甲酸酯、脲、硫脲、硫代氨基甲酸酯,和杂芳基-氨基取代的四环素化合物
DE60102815D1 (de) * 2000-05-15 2004-05-19 Paratek Pharm Innc 7-substituierte kondensierte ring-tetrazyclin- verbindungen
KR100674047B1 (ko) * 2000-07-07 2007-01-25 트러스티즈 오브 터프츠 칼리지 9-치환된 미노사이클린 화합물
US7094806B2 (en) 2000-07-07 2006-08-22 Trustees Of Tufts College 7, 8 and 9-substituted tetracycline compounds
IL157860A0 (en) 2001-03-13 2004-03-28 Paratek Pharm Innc 7,9-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
ATE455092T1 (de) * 2001-04-24 2010-01-15 Paratek Pharm Innc Substituierte tetracyclin-verbindungen zur behandlung von malaria
EP2301915A1 (en) 2001-07-13 2011-03-30 Paratek Pharmaceuticals, Inc. 7-(diethylamino)methyl substituted tetracycline having target therapeutic activities
WO2003055441A2 (en) 2001-08-02 2003-07-10 Paratek Pharmaceuticals, Inc. Medicaments
EP2311797A1 (en) 2002-01-08 2011-04-20 Paratek Pharmaceuticals, Inc. 4-dedimethylamino tetracycline compounds
CN102531948A (zh) * 2002-03-08 2012-07-04 帕拉特克药品公司 氨基-甲基取代的四环素类化合物
EP2298323A3 (en) 2003-07-09 2011-05-11 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds
UA83266C2 (en) * 2003-12-08 2008-06-25 Уайет Oxazole derivatives of tetracyclines
AU2005244988C1 (en) * 2004-05-21 2012-06-28 President And Fellows Of Harvard College Synthesis of tetracyclines and analogues thereof
US7534766B2 (en) 2004-11-05 2009-05-19 Wyeth Glucuronide metabolites and epimers thereof of tigecycline
AR057649A1 (es) 2005-05-27 2007-12-12 Wyeth Corp Formas solidas cristalinas de tigeciclina y metodos para preparar las mismas
KR20080041722A (ko) * 2005-08-31 2008-05-13 와이어쓰 글리실사이클린의 9-아미노카르보닐 치환된 유도체
JP2009543544A (ja) 2006-05-15 2009-12-10 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 置換されたテトラサイクリン化合物を用いて、遺伝子または遺伝子産物の発現を調節する方法
ES2388958T3 (es) 2007-11-29 2012-10-22 Actelion Pharmaceuticals Ltd. Derivados de acido fosfonico y su uso como antagonista del receptor P2Y12
PT2271348T (pt) 2008-03-28 2018-04-16 Paratek Pharm Innc Formulação de comprimido oral de composto de tetraciclina
ITMI20080807A1 (it) 2008-05-05 2009-11-06 Antibioticos Spa Procedimento per la preparazione di tigeciclina in forma amorfa
TW202332671A (zh) 2008-05-23 2023-08-16 美商Prtk Spv2公司 四環素化合物之甲苯磺酸鹽及同素異形體
NZ603568A (en) * 2008-08-08 2014-05-30 Tetraphase Pharmaceuticals Inc C7-fluoro substituted tetracycline compounds
EP2424834B1 (en) 2009-04-30 2018-07-11 President and Fellows of Harvard College Synthesis of tetracyclines and intermediates thereof
DK2427425T3 (en) 2009-05-08 2017-06-12 Tetraphase Pharmaceuticals Inc tetracycline
CN102596898B (zh) 2009-08-28 2016-01-27 四相制药公司 四环素类化合物
WO2011143503A2 (en) 2010-05-12 2011-11-17 Rempex Pharmaceuticals, Inc. Tetracycline compositions
CN103635456B (zh) * 2011-07-26 2016-03-09 山东亨利医药科技有限责任公司 替加环素衍生物
NZ705849A (en) 2012-08-31 2018-06-29 Tetraphase Pharmaceuticals Inc Tetracycline compounds
US20160143925A1 (en) 2013-11-12 2016-05-26 Galenicum Health S.L. Stable pharmaceutical compositions
DK3529236T3 (da) 2016-10-19 2024-05-13 Tetraphase Pharmaceuticals Inc Krystalformer af eravacyclin

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US3338963A (en) * 1960-10-28 1967-08-29 American Cyanamid Co Tetracycline compounds
US3579579A (en) * 1968-04-18 1971-05-18 American Cyanamid Co Substituted 7- and/or 9-amino-6-demethyl-6-deoxytetracyclines

Also Published As

Publication number Publication date
SK280837B6 (sk) 2000-08-14
CZ284159B6 (cs) 1998-08-12
NL300244I1 (nl) 2007-01-02
FI924454A0 (fi) 1992-10-02
CN1072172A (zh) 1993-05-19
AU654049B2 (en) 1994-10-20
HU9203110D0 (en) 1992-12-28
KR930007894A (ko) 1993-05-20
NO2017037I1 (no) 2017-08-01
BR1100853A (pt) 1999-12-07
NZ244585A (en) 1995-07-26
SK284826B6 (sk) 2005-12-01
CN1048240C (zh) 2000-01-12
JPH05255219A (ja) 1993-10-05
EP0536515B1 (en) 2001-12-19
DE122006000058I1 (de) 2007-01-18
HUT63145A (en) 1993-07-28
AU2618392A (en) 1993-04-08
PT536515E (pt) 2002-05-31
TW275616B (cs) 1996-05-11
SG52361A1 (en) 1998-09-28
DE69232302D1 (de) 2002-01-31
ATE211128T1 (de) 2002-01-15
IL119590A (en) 1999-03-12
HK1011348A1 (en) 1999-07-09
SK114999A3 (en) 2000-07-11
NO2017037I2 (no) 2017-08-01
DK0536515T3 (da) 2002-04-08
PL175957B1 (pl) 1999-03-31
KR100269072B1 (ko) 2000-10-16
PL176333B1 (pl) 1999-05-31
DE69232302T4 (de) 2003-02-13
CA2079692C (en) 2004-06-08
CZ309397A3 (cs) 1998-09-16
SK298492A3 (en) 1995-03-08
ZA927607B (en) 1993-04-13
CL2004001623A1 (es) 2005-06-03
PL172282B1 (pl) 1997-08-29
IL103320A (en) 1998-12-06
PL173311B1 (pl) 1998-02-27
NO2006015I1 (no) 2006-11-27
NO301472B1 (no) 1997-11-03
CZ298492A3 (en) 1993-05-12
CA2079692A1 (en) 1993-04-05
DE69232302T2 (de) 2002-08-14
IL103320A0 (en) 1993-03-15
NL300244I2 (nl) 2007-01-02
PL296143A1 (en) 1993-05-31
IL119590A0 (en) 1997-02-18
HU219973B (hu) 2001-10-28
MX9205532A (es) 1993-04-01
FI924454A (fi) 1993-04-05
CZ284209B6 (cs) 1998-09-16
NO923857L (no) 1993-04-05
EP0536515A1 (en) 1993-04-14
LU91279I2 (fr) 2006-12-11
NO923857D0 (no) 1992-10-02
NO2006015I2 (no) 2011-03-14
JP3186863B2 (ja) 2001-07-11
ES2168254T3 (es) 2002-06-16
DE122006000058I2 (de) 2007-09-13
HU211172A9 (en) 1995-11-28

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