CN100545151C - 四环素类的恶唑衍生物 - Google Patents

四环素类的恶唑衍生物 Download PDF

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Publication number
CN100545151C
CN100545151C CNB2004800364939A CN200480036493A CN100545151C CN 100545151 C CN100545151 C CN 100545151C CN B2004800364939 A CNB2004800364939 A CN B2004800364939A CN 200480036493 A CN200480036493 A CN 200480036493A CN 100545151 C CN100545151 C CN 100545151C
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CN
China
Prior art keywords
dimethylamino
dioxo
oxazole
trihydroxy
methane amide
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
CNB2004800364939A
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English (en)
Chinese (zh)
Other versions
CN1890226A (zh
Inventor
费尔克-恩格·萨姆
戴维·布赖恩·豪
达林·威廉·霍珀
马修·道格拉斯·威拉
乔舒亚·詹姆斯·萨巴蒂尼
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Wyeth LLC
Original Assignee
Wyeth 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
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34681543&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CN100545151(C) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Wyeth LLC filed Critical Wyeth LLC
Publication of CN1890226A publication Critical patent/CN1890226A/zh
Application granted granted Critical
Publication of CN100545151C publication Critical patent/CN100545151C/zh
Anticipated expiration legal-status Critical
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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/62—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems having two or more ring systems containing condensed 1,3-oxazole rings
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/65—Tetracyclines
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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)
  • 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)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
CNB2004800364939A 2003-12-08 2004-12-07 四环素类的恶唑衍生物 Expired - Fee Related CN100545151C (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US52792803P 2003-12-08 2003-12-08
US60/527,928 2003-12-08
US58482304P 2004-07-01 2004-07-01
US60/584,823 2004-07-01

Publications (2)

Publication Number Publication Date
CN1890226A CN1890226A (zh) 2007-01-03
CN100545151C true CN100545151C (zh) 2009-09-30

Family

ID=34681543

Family Applications (1)

Application Number Title Priority Date Filing Date
CNB2004800364939A Expired - Fee Related CN100545151C (zh) 2003-12-08 2004-12-07 四环素类的恶唑衍生物

Country Status (25)

Country Link
US (3) US7176225B2 (enExample)
EP (2) EP2157085B1 (enExample)
JP (1) JP4848287B2 (enExample)
KR (1) KR101164262B1 (enExample)
CN (1) CN100545151C (enExample)
AR (1) AR047274A1 (enExample)
AT (2) ATE525365T1 (enExample)
AU (1) AU2004297243B2 (enExample)
BR (1) BRPI0417421A (enExample)
CA (1) CA2546895A1 (enExample)
CO (1) CO5700818A2 (enExample)
CR (1) CR8437A (enExample)
DE (1) DE602004023417D1 (enExample)
EC (1) ECSP066605A (enExample)
ES (2) ES2372635T3 (enExample)
IL (2) IL176162A (enExample)
MY (1) MY146098A (enExample)
NO (1) NO20062629L (enExample)
PA (1) PA8619601A1 (enExample)
PE (1) PE20050995A1 (enExample)
RU (1) RU2415844C2 (enExample)
SG (1) SG148216A1 (enExample)
TW (1) TW200528437A (enExample)
UA (2) UA83266C2 (enExample)
WO (1) WO2005056538A1 (enExample)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL1753713T3 (pl) * 2004-05-21 2017-02-28 President And Fellows Of Harvard College Synteza tetracyklin oraz ich analogów
CA2585418A1 (en) 2004-10-25 2006-05-04 Paratek Pharmaceuticals, Inc. 4-aminotetracyclines and methods of use thereof
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
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
CA2648668C (en) 2006-04-07 2015-06-23 The President And Fellows Of Harvard College Synthesis of tetracyclines and analogues thereof
US8440646B1 (en) 2006-10-11 2013-05-14 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds for treatment of Bacillus anthracis infections
EP2487160B1 (en) 2006-10-11 2016-02-03 President and Fellows of Harvard College Synthesis of Enone Intermediate
US8121767B2 (en) * 2007-11-02 2012-02-21 GM Global Technology Operations LLC Predicted and immediate output torque control architecture for a hybrid powertrain system
US8252946B2 (en) 2007-11-14 2012-08-28 Sandoz Ag Crystalline forms of tigecycline hydrochloride
CA2730377C (en) * 2008-07-11 2017-09-19 Neumedics Tetracycline derivatives with reduced antibiotic activity and neuroprotective benefits
EP2376433B1 (en) 2008-12-18 2014-10-29 Sandoz AG Crystalline form c of tigecycline dihydrochloride and methods for its preparation
US9073829B2 (en) 2009-04-30 2015-07-07 President And Fellows Of Harvard College Synthesis of tetracyclines and intermediates thereto

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0582788A1 (en) * 1992-08-13 1994-02-16 American Cyanamid Company 7-(Substituted)-9- (substituted glycyl)-amido)-6-demethyl-6-deoxytetracyclines
US5494903A (en) * 1991-10-04 1996-02-27 American Cyanamid Company 7-substituted-9-substituted amino-6-demethyl-6-deoxytetracyclines

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US26253A (en) * 1859-11-29 Vegetable-cutter
US2482055A (en) 1948-02-11 1949-09-13 American Cyanamid Co Aureomycin and preparation of same
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 (enExample) 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
US3341585A (en) 1966-05-06 1967-09-12 American Cyanamid Co Substituted 7-and/or 9-amino-6-deoxytetracyclines
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
US4806529A (en) 1982-11-18 1989-02-21 Trustees Of Tufts College, Tufts University Tetracycline activity enhancement
DE69232302T4 (de) * 1991-10-04 2003-02-13 American Cyanamid Co., Wayne 7-Substituierte-9-substituierte Amino-6-Demethyl-6-Deoxy-Tetracycline
CA2378990A1 (en) * 1999-08-10 2001-02-15 Siegfried B. Christensen, Iv 1,4-substituted 4,4-diaryl cyclohexanes
AU2002318238A1 (en) * 2001-07-13 2003-01-29 Paratek Pharmaceuticals, Inc. Tetracycline compounds having target therapeutic activities

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5494903A (en) * 1991-10-04 1996-02-27 American Cyanamid Company 7-substituted-9-substituted amino-6-demethyl-6-deoxytetracyclines
EP0582788A1 (en) * 1992-08-13 1994-02-16 American Cyanamid Company 7-(Substituted)-9- (substituted glycyl)-amido)-6-demethyl-6-deoxytetracyclines

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Glycylcyclines. 1. A new generation of potent antibacterialagents through modification of 9-aminotetracyclines.. Phaik-Eng Sum, et al.J.Med.Chem.,Vol.37 No.1. 1994 *

Also Published As

Publication number Publication date
TW200528437A (en) 2005-09-01
US20080177080A1 (en) 2008-07-24
AU2004297243A1 (en) 2005-06-23
US20080064667A1 (en) 2008-03-13
KR101164262B1 (ko) 2012-07-09
BRPI0417421A (pt) 2007-03-13
PA8619601A1 (es) 2006-03-24
SG148216A1 (en) 2008-12-31
EP1692117A1 (en) 2006-08-23
ATE525365T1 (de) 2011-10-15
WO2005056538A1 (en) 2005-06-23
CR8437A (es) 2006-10-06
AU2004297243B2 (en) 2011-02-17
EP2157085B1 (en) 2011-09-21
UA83268C2 (en) 2008-06-25
CA2546895A1 (en) 2005-06-23
US7365087B2 (en) 2008-04-29
AR047274A1 (es) 2006-01-11
KR20060105047A (ko) 2006-10-09
JP4848287B2 (ja) 2011-12-28
US20050153944A1 (en) 2005-07-14
PE20050995A1 (es) 2006-01-11
JP2007515411A (ja) 2007-06-14
US7176225B2 (en) 2007-02-13
RU2006118367A (ru) 2008-01-20
IL176162A (en) 2011-09-27
UA83266C2 (en) 2008-06-25
IL206050A (en) 2013-01-31
IL176162A0 (en) 2006-10-05
EP2157085A1 (en) 2010-02-24
NO20062629L (no) 2006-09-06
IL206050A0 (en) 2010-11-30
RU2415844C2 (ru) 2011-04-10
EP1692117B1 (en) 2009-09-30
ATE444290T1 (de) 2009-10-15
MY146098A (en) 2012-06-29
CO5700818A2 (es) 2006-11-30
ES2372635T3 (es) 2012-01-25
DE602004023417D1 (de) 2009-11-12
ECSP066605A (es) 2006-10-25
ES2331574T3 (es) 2010-01-08
CN1890226A (zh) 2007-01-03

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Granted publication date: 20090930

Termination date: 20131207