UY25041A1 - Derivados de macrolidos c-4" sustituidos - Google Patents

Derivados de macrolidos c-4" sustituidos

Info

Publication number
UY25041A1
UY25041A1 UY25041A UY25041A UY25041A1 UY 25041 A1 UY25041 A1 UY 25041A1 UY 25041 A UY25041 A UY 25041A UY 25041 A UY25041 A UY 25041A UY 25041 A1 UY25041 A1 UY 25041A1
Authority
UY
Uruguay
Prior art keywords
infections
groups
formula
compounds
hydroxy
Prior art date
Application number
UY25041A
Other languages
English (en)
Inventor
Bingwei Vera Yang
Hengmiao Cheng
Edward Alan Glazer
Brian Scott Bronk
Michael Anthony Letavic
Takushi Kaneko
Original Assignee
Pfizer Prod Inc
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 Pfizer Prod Inc filed Critical Pfizer Prod Inc
Publication of UY25041A1 publication Critical patent/UY25041A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C07H17/04—Heterocyclic radicals containing only oxygen as ring hetero atoms
    • C07H17/08—Hetero rings containing eight or more ring members, e.g. erythromycins
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • Biochemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Biotechnology (AREA)
  • Molecular Biology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Esta invención se refiere a los nuevos derivados de macrólidos C-4" sustituidos que son útiles como agentes antibacterianos y antiprotozoos en mamíferos, incluyendo al hombre. Tales antibióticos macrólidos incluyen varios derivados de la eritromicina A como la azitromicina. Esta invención refiere a los compuestos macrólidos, de fórmula (I), y sus sales farmacéuticamente aceptables. Dichos compuestos son potentes agentes antibacterianos que pueden usarse para tratar diversas infecciones bacterianas y trastornos relacionados con las mismas. La invención también refiere las composiciones farmacéuticas que los contienen y a los métodos para el tratamiento de las infecciones bacterianas mediante la administración de los mismos. También refiere los métodos para la preparación y los productos intermedios útiles para dicha preparación. Compuestos de fórmula (I), en la que: X es CH(NR9R10), C(O), C(=NOR9), CH2NR9 ó N-alquilo-CH2 en los que la primera línea de cada uno de los anteriores grupos X está unida la carbono C10 y la última línea de cada grupo está unida al carbono C8 del compuesto de fórmula (I); R1 es H, hidroxi o metoxi; R2 es hidroxi; R3 es alquilo, alquenilo, alquinilo, ciano, CH2S(O)nR8, en el que n es un número entero entre 0 y 2, CH2OR8, CH2N(OR9)R8, CH2NR8R15, (CH2)m-arilo, ó (CH2)m-heteroarilo, en el que m es un número entero entre 0 y 4 y en los que los anteriores grupos R3 están opcionalmente sustituidos en 1 a 3 grupos R16; ó R2 y R3 están unidos formando un anillo oxazolilo; R4 es H, C(O)R9, C(O)OR9, C(O)NR9R10 ó un grupo protector de hidroxi. Útiles para trastornos relacionados con dichas infecciones que incluyen: neumonía, otitis media, sinusitis, bronquitis, tonsilitis y mastoiditis; faringitis, fiebre reumática y glomerulonefritis; infecciones del tracto respiratorio; infecciones de la piel y del tejido blando, abscesos y osteomielitis y fiebre puerperal; infecciones del tracto urinario agudas sin complicaciones; uretritis y cervicitis, y enfermedades de trasmisión sexual, entre otras.
UY25041A 1997-06-11 1998-06-11 Derivados de macrolidos c-4" sustituidos UY25041A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US4998097P 1997-06-11 1997-06-11

Publications (1)

Publication Number Publication Date
UY25041A1 true UY25041A1 (es) 2000-09-29

Family

ID=21962765

Family Applications (1)

Application Number Title Priority Date Filing Date
UY25041A UY25041A1 (es) 1997-06-11 1998-06-11 Derivados de macrolidos c-4" sustituidos

Country Status (40)

Country Link
EP (1) EP0988309B1 (es)
JP (1) JP3262806B2 (es)
KR (1) KR100369959B1 (es)
CN (1) CN1145636C (es)
AP (1) AP1189A (es)
AR (1) AR013085A1 (es)
AT (1) ATE310742T1 (es)
AU (1) AU745006C (es)
BG (1) BG64357B1 (es)
BR (1) BR9810097A (es)
CA (1) CA2293397C (es)
CO (1) CO4950584A1 (es)
DE (1) DE69832486T2 (es)
DZ (1) DZ2515A1 (es)
EA (1) EA002440B1 (es)
ES (1) ES2251081T3 (es)
GT (1) GT199800075A (es)
HK (1) HK1025974A1 (es)
HN (1) HN1998000074A (es)
HR (1) HRP980315A2 (es)
HU (1) HUP0004076A3 (es)
ID (1) ID24530A (es)
IL (1) IL132808A (es)
IS (1) IS1979B (es)
MA (1) MA24563A1 (es)
MY (1) MY133027A (es)
NO (1) NO315560B1 (es)
NZ (1) NZ500652A (es)
OA (1) OA11226A (es)
PA (1) PA8452001A1 (es)
PE (1) PE79999A1 (es)
PL (1) PL337497A1 (es)
SK (1) SK168299A3 (es)
TN (1) TNSN98084A1 (es)
TW (2) TWI224106B (es)
UA (1) UA70298A (es)
UY (1) UY25041A1 (es)
WO (1) WO1998056801A1 (es)
YU (1) YU62999A (es)
ZA (1) ZA985016B (es)

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US6339063B1 (en) 1997-09-10 2002-01-15 Merck & Co., Inc. 9a-azalides as veterinary antimicrobial agents
EP1779853A3 (en) * 1997-09-10 2010-01-27 Merial Ltd. 9a-azalides as veterinary antimicrobial agents
DE69837007T2 (de) * 1997-09-10 2007-11-22 Merial Ltd. Verwendung von 9a-azaliden als antimikrobielle mittel für tiere
AP9801420A0 (en) * 1998-01-02 1998-12-31 Pfizer Prod Inc Novel macrolides.
EP1437360A3 (en) * 1998-08-19 2005-04-06 Pfizer Products Inc. C11 Carbamates of macrolide antibacterials
US6043227A (en) * 1998-08-19 2000-03-28 Pfizer Inc. C11 carbamates of macrolide antibacterials
US6100240A (en) * 1998-10-09 2000-08-08 Pfizer Inc Macrolide derivatives
HUP0104192A3 (en) 1998-11-03 2003-12-29 Pfizer Prod Inc Novel macrolide antibiotics
CA2292359C (en) * 1999-01-28 2004-09-28 Pfizer Products Inc. Novel azalides and methods of making same
DK1206476T3 (da) * 1999-08-24 2006-05-15 Abbott Lab 9a-azalider med antibakteriel virkning
US6764996B1 (en) 1999-08-24 2004-07-20 Abbott Laboratories 9a-azalides with antibacterial activity
PT1250343E (pt) 2000-01-27 2003-11-28 Pfizer Prod Inc Composicoes de antibioticos de azalida
CA2445306C (en) * 2001-04-27 2008-02-12 Pfizer Products Inc. Process for preparing 4"-substituted-9-deoxo-9a-aza-9a-homoerythromycin a derivatives
JP2003040782A (ja) * 2001-05-31 2003-02-13 Pfizer Prod Inc アザリド抗生物質組成物
WO2004005313A2 (en) 2002-07-08 2004-01-15 Pliva - Istrazivacki Institut D.O.O. Hybrid molecules of macrolides with steroid/non-steroid anti-inflammatory, antineoplastic and antiviral active molecules
EP1521763A2 (en) * 2002-07-08 2005-04-13 Pliva - Istrazivacki Institut d.o.o. Novel nonsteroidal anti-inflammatory substances, compositions and methods for their use
WO2004005310A2 (en) 2002-07-08 2004-01-15 Pliva-Istrazivacki Institut D.O.O. New compounds, compositions and methods for treatment of inflammatory diseases and conditions
AR043050A1 (es) 2002-09-26 2005-07-13 Rib X Pharmaceuticals Inc Compuestos heterociclicos bifuncionales y metodos para preparar y usar los mismos
US7601695B2 (en) * 2003-03-10 2009-10-13 Optimer Pharmaceuticals, Inc. Antibacterial agents
US7276487B2 (en) 2003-09-23 2007-10-02 Enanta Pharmaceuticals, Inc. 9a, 11-3C-bicyclic 9a-azalide derivatives
CN102816194A (zh) 2004-02-27 2012-12-12 瑞伯-X医药品有限公司 大环化合物以及其制作和使用方法
JPWO2009019868A1 (ja) 2007-08-06 2010-10-28 大正製薬株式会社 １０ａ、１２位架橋型１０ａ−アザライド化合物
CA2703475A1 (en) 2007-10-25 2009-04-30 Cempra Pharmaceuticals, Inc. Process for the preparation of macrolide antibacterial agents
US8299035B2 (en) 2008-05-15 2012-10-30 Taisho Pharmaceutucal Co., Ltd. 10a-azalide compound having 4-membered ring structure
CN102245195B (zh) 2008-10-24 2016-01-13 森普拉制药公司 使用含三唑的大环内酯的生物防御
US9937194B1 (en) 2009-06-12 2018-04-10 Cempra Pharmaceuticals, Inc. Compounds and methods for treating inflammatory diseases
JP5908479B2 (ja) * 2010-09-20 2016-04-26 ノバルティス ティーアゲズントハイト アーゲー クラジノース環のＣ−４”をエポキシド基で修飾した９−デオキソ−９ａ−アザ−９ａ−ホモエリスロマイシンＡの新規製造方法
AR085286A1 (es) 2011-02-21 2013-09-18 Taisho Pharmaceutical Co Ltd Derivado de macrolido sustituido en la posicion c-4
EP2830632A4 (en) 2012-03-27 2015-10-21 Cempra Pharmaceuticals Inc PARENTERAL FORMULATIONS FOR THE ADMINISTRATION OF MACROLIDE ANTIBIOTICS
JP5857008B2 (ja) * 2012-08-20 2016-02-10 大正製薬株式会社 Ｃ−４”位置換マクロライド誘導体を含有する医薬
CN105246334A (zh) 2013-04-04 2016-01-13 哈佛大学的校长及成员们 大环内酯及其制备和使用方法
CN105669798B (zh) * 2013-08-23 2019-07-26 普莱柯生物工程股份有限公司 一种大环内酯类化合物
CN103965273B (zh) 2013-08-23 2016-05-25 普莱柯生物工程股份有限公司 一种大环内酯类化合物
AR102810A1 (es) 2014-08-18 2017-03-29 Taisho Pharmaceutical Co Ltd Derivado de macrólido sustituido en la posición c-4
US10633407B2 (en) 2014-10-08 2020-04-28 President And Fellows Of Harvard College 14-membered ketolides and methods of their preparation and use
JP2018509452A (ja) 2015-03-25 2018-04-05 プレジデント アンド フェローズ オブ ハーバード カレッジ 修飾デソサミン糖をもつマクロライドおよびその使用
CN108003207B (zh) 2017-12-19 2019-05-10 海门慧聚药业有限公司 制备泰拉霉素的方法

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CA2064634C (en) * 1991-04-04 1998-08-04 James V. Heck 9-deoxo-8a-aza-8a-homoerythromycin a derivatives modified at the 4"- and8a-positions
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US5412982A (en) * 1994-03-10 1995-05-09 Potts; James K. Windsock support

Also Published As

Publication number Publication date
NO996107L (no) 2000-02-10
DZ2515A1 (fr) 2003-02-01
CA2293397A1 (en) 1998-12-17
MA24563A1 (fr) 1998-12-31
GT199800075A (es) 1999-11-30
TNSN98084A1 (fr) 2005-03-15
IS1979B (is) 2005-01-14
AU745006C (en) 2006-02-23
DE69832486T2 (de) 2006-07-27
NO996107D0 (no) 1999-12-10
AR013085A1 (es) 2000-12-13
MY133027A (en) 2007-10-31
OA11226A (en) 2003-07-16
IL132808A0 (en) 2001-03-19
IL132808A (en) 2004-08-31
AU7228198A (en) 1998-12-30
CA2293397C (en) 2004-08-31
HUP0004076A3 (en) 2003-05-28
TW200418871A (en) 2004-10-01
PA8452001A1 (es) 2000-05-24
UA70298C2 (uk) 2004-10-15
BG103969A (en) 2000-07-31
JP2000514097A (ja) 2000-10-24
EA002440B1 (ru) 2002-04-25
BR9810097A (pt) 2000-08-08
AU745006B2 (en) 2002-03-07
CN1259955A (zh) 2000-07-12
EP0988309A1 (en) 2000-03-29
EP0988309B1 (en) 2005-11-23
KR20010013633A (ko) 2001-02-26
UA70298A (uk) 2004-10-15
CO4950584A1 (es) 2000-09-01
HRP980315A2 (en) 1999-04-30
JP3262806B2 (ja) 2002-03-04
PL337497A1 (en) 2000-08-28
NZ500652A (en) 2001-10-26
AP9801254A0 (en) 1998-06-30
WO1998056801A1 (en) 1998-12-17
IS5250A (is) 1999-11-16
CN1145636C (zh) 2004-04-14
HN1998000074A (es) 1999-01-08
AP1189A (en) 2003-07-16
DE69832486D1 (de) 2005-12-29
HK1025974A1 (en) 2000-12-01
BG64357B1 (bg) 2004-11-30
ID24530A (id) 2000-07-20
NO315560B1 (no) 2003-09-22
HUP0004076A2 (hu) 2001-04-28
ZA985016B (en) 1999-12-10
EA199901014A1 (ru) 2000-06-26
PE79999A1 (es) 1999-08-25
ATE310742T1 (de) 2005-12-15
TWI224106B (en) 2004-11-21
ES2251081T3 (es) 2006-04-16
KR100369959B1 (ko) 2003-02-12
SK168299A3 (en) 2000-09-12
YU62999A (sh) 2002-10-18

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