CO5380019A1 - Azalidas de 13 miembros utiles como agentes antibioticos - Google Patents

Azalidas de 13 miembros utiles como agentes antibioticos

Info

Publication number
CO5380019A1
CO5380019A1 CO99072704A CO99072704A CO5380019A1 CO 5380019 A1 CO5380019 A1 CO 5380019A1 CO 99072704 A CO99072704 A CO 99072704A CO 99072704 A CO99072704 A CO 99072704A CO 5380019 A1 CO5380019 A1 CO 5380019A1
Authority
CO
Colombia
Prior art keywords
alkyl
alkynyl
alkenyl
hydrogen
aryl
Prior art date
Application number
CO99072704A
Other languages
English (en)
Inventor
Robert John Rafka
Barry James Morton
Ragan Colman Brendan
Peter Bertinato
John Philip Dirlam
Alan Elwood Blize
Carl Bernard Ziegler
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=22327457&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CO5380019(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Pfizer Prod Inc filed Critical Pfizer Prod Inc
Publication of CO5380019A1 publication Critical patent/CO5380019A1/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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Biochemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biotechnology (AREA)
  • Public Health (AREA)
  • Genetics & Genomics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyrane Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Pyridine Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

Un compuesto de fórmula 2 <EMI FILE="99072704_1" ID="1" IMF=JPEG >o una sal farmacéuticamente aceptable del mismo, en el que:X es -C(O)- o -CH(OR7); yR2 es hidrógeno o alquilo C1-C4;cada R7 es independientemente hidrógeno, alquilo C1-C20, alquenilo C2-C20, alquinilo C2-C20, -C(O)alquilo C1-C20, -C(O)alquenilo C2-C20, -C(O)alquinilo C2-C20, -C(O)N(H)alquilo C1-C10, -C(O)N(H)alquenilo C2-C20, -C(O)N(H)alquinilo C2-C20, -SO2(O)alquilo C1-C20, -SO2(O)alquenilo C2-C20, -SO2(O)alquinilo C2-C20 o -PO42-;R8 es hidrógeno o metilo: <EMI FILE="99072704_2" ID="2" IMF=JPEG >R9 es 2 o 4"-oxacladinosilo; yR5 es hidrógeno, alquilo C1-C10, alquenilo C2-C10, alquinilo C2-C10, ciano, -CH2S(O)p alquilo C1-C10, -CH2S(O)p alquenilo C2-C10, -CH2S(O)p alquinilo C2-C10, en los que p es un número entero que varía de 0 a 2, -CH2O(alquilo C1-C10), -CH2O(alquenilo C2-C10), -CH2O(alquinilo C2-C10), -CH2N(hidrógeno, alquilo C1-C10, alquenilo C2-C10 o alquinilo C2-C10)(hidrógeno, alquilo C1-C10, alquenilo C2-C10 o aIquinilo C2-C10), -(CH2)m(arilo C6-C10) o -(CH2)m(heteroarilo de 5-10 miembros), en los que m es un número entero que varía de 0 a 4 y en los que los restos alquilo, alquenilo, alquinilo, arilo y heteroarilo de los grupos anteriores están opcionalmente sustituidos con 1 a 3 sustituyentes seleccionados independientemente entre halo, ciano, nitro, trifluorometilo, azido, -C(O)alquilo C1-C10, -C(O)alquenilo C2-C10, -C(O)alquinilo C2-C10, -OC(O)alquilo C1-C10, -OC(O)alquenilo C2-C10, -OC(O)alquinilo C2-C10, -N(hidrógeno, alquilo C1-C10, alquenilo C2-C10 o alquinilo C2-C10)C(O)(alquilo C1-C10, alquenilo C2-C10 o alquinilo C2-C10), -C(O)N(hidrógeno, alquilo C1-C10, alquenilo C2-C10 o alquinilo C2-C10)(hidrógeno, alquilo C1-C10, alquenilo C2-C10 o alquinilo C2-C10), -N(hidrógeno, alquilo C1-C10, alquenilo C2-C10 o alquinilo C2-C10)(hidrógeno, alquilo C1-C10, alquenilo C2-C10 o alquinilo C2-C10), alcoxi C1-C10, arilo C6-C10 y heterociclo de 5-10 miembros, hidroxi, alquilo C1-C6, alcoxi C1-C6, arilo C6-C10 y heteroarilo de 5-10 miembros.
CO99072704A 1998-11-20 1999-11-18 Azalidas de 13 miembros utiles como agentes antibioticos CO5380019A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US10939998P 1998-11-20 1998-11-20

Publications (1)

Publication Number Publication Date
CO5380019A1 true CO5380019A1 (es) 2004-03-31

Family

ID=22327457

Family Applications (1)

Application Number Title Priority Date Filing Date
CO99072704A CO5380019A1 (es) 1998-11-20 1999-11-18 Azalidas de 13 miembros utiles como agentes antibioticos

Country Status (46)

Country Link
US (1) US6329345B1 (es)
EP (1) EP1131331B1 (es)
JP (1) JP3842973B2 (es)
KR (1) KR100477774B1 (es)
CN (2) CN1326460A (es)
AP (1) AP2001002142A0 (es)
AR (3) AR019496A1 (es)
AT (1) ATE260927T1 (es)
AU (1) AU766106B2 (es)
BG (1) BG65107B1 (es)
BR (2) BRPI9915480B8 (es)
CA (1) CA2351429C (es)
CO (1) CO5380019A1 (es)
CZ (1) CZ303099B6 (es)
DE (1) DE69915336T2 (es)
DK (1) DK1131331T3 (es)
DZ (1) DZ2944A1 (es)
EA (2) EA009729B1 (es)
EG (1) EG23823A (es)
ES (1) ES2216581T3 (es)
GT (1) GT199900198A (es)
HK (1) HK1041269A1 (es)
HR (1) HRP20010374B1 (es)
HU (1) HU229008B1 (es)
ID (1) ID28548A (es)
IL (3) IL142631A0 (es)
IS (1) IS2350B (es)
MA (1) MA26707A1 (es)
ME (1) ME00467B (es)
MY (1) MY122353A (es)
NO (3) NO319796B1 (es)
NZ (1) NZ511199A (es)
OA (1) OA11713A (es)
PA (1) PA8485601A1 (es)
PE (1) PE20001378A1 (es)
PL (1) PL198580B1 (es)
PT (1) PT1131331E (es)
RS (1) RS50302B (es)
SI (1) SI1131331T1 (es)
SK (1) SK284607B6 (es)
TN (1) TNSN99214A1 (es)
TW (2) TWI243825B (es)
UA (1) UA70972C2 (es)
UY (1) UY25805A1 (es)
WO (1) WO2000031097A1 (es)
ZA (1) ZA200104019B (es)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HN1998000086A (es) 1997-06-11 1999-03-08 Pfizer Prod Inc Derivados de 9 - desofo - 9 aza - 9a - homoeritromicina a - c - 4 sustituidos.
AP9801420A0 (en) * 1998-01-02 1998-12-31 Pfizer Prod Inc Novel macrolides.
UA70972C2 (uk) * 1998-11-20 2004-11-15 Пфайзер Продактс Інк. 13-членні азаліди і їх застосування як антибіотиків
AP2001002302A0 (en) * 1999-05-24 2001-10-25 Pfizer Prod Inc 13-Methyl erythromycin derivatives.
US6465437B1 (en) * 1999-06-30 2002-10-15 Pfizer Inc. Diphosphate salt of a 4″-substituted-9-deoxo-9A-AZA-9A- homoerythromycin derivative and its pharmaceutical composition
OA12257A (en) * 2000-04-27 2003-11-06 Pfizer Prod Inc the use of azalide antibiotic compositions for treating or preventing a bacterial or protozoal infection in mammals.
WO2002088158A1 (en) * 2001-04-27 2002-11-07 Pfizer Products Inc. Process for preparing 4'-substituted-9-deoxo-9a-aza-9a-homoerythromycin a derivatives
JP4311203B2 (ja) * 2001-08-08 2009-08-12 大正製薬株式会社 １１ａ−アザライド化合物及びその製造方法
ES2552682T3 (es) * 2003-03-10 2015-12-01 Merck Sharp & Dohme Corp. Agentes antibacterianos novedosos
WO2004108744A2 (en) * 2003-05-19 2004-12-16 Prasad K Deshpande Azalides and azaketolides having antimicrobial activity
CN1882360A (zh) * 2003-11-21 2006-12-20 辉瑞产品公司 抗生素作为疫苗佐剂的用途
WO2007091393A1 (ja) * 2006-02-07 2007-08-16 Taisho Pharmaceutical Co., Ltd. １０ａ－アザライド化合物
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
US8299035B2 (en) 2008-05-15 2012-10-30 Taisho Pharmaceutucal Co., Ltd. 10a-azalide compound having 4-membered ring structure
US8940880B2 (en) 2010-09-20 2015-01-27 Novartis Ag Process for the preparation of 9-deoxo-9a-homoerythromycin A, modified in the C-4″ of the cladinose ring by an epoxide group
CN102295672B (zh) * 2011-07-13 2014-06-04 武汉回盛生物科技有限公司 一种泰拉菌素的合成方法
EP2736915A1 (en) 2011-07-27 2014-06-04 Farma GRS, d.o.o. New crystalline forms of tulathromycin
CN102786569B (zh) * 2012-09-07 2016-12-07 安徽中升药业有限公司 泰拉霉素中间体及其制备方法与泰拉霉素的制备方法
WO2015014907A1 (en) * 2013-07-31 2015-02-05 Farma Grs, D.O.O. Process for preparation of tulathromycin
CN109748942A (zh) * 2014-05-16 2019-05-14 普莱柯生物工程股份有限公司 一种大环内酯类化合物
CN104725446B (zh) * 2015-03-26 2017-10-27 宁夏泰瑞制药股份有限公司 一种从泰拉霉素粗品中分离泰拉霉素a和泰拉霉素b的方法
SG11202105227QA (en) * 2018-11-19 2021-06-29 Zikani Therapeutics Inc C10-alkylene substituted 13-membered macrolides and uses thereof
CN113646319A (zh) * 2018-11-19 2021-11-12 齐卡尼治疗股份有限公司 C11-环取代的13元大环内酯及其用途

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI7910768A8 (en) 1979-04-02 1996-06-30 Pliva Pharm & Chem Works Process for pripering 11-aza-4-0-cladinosyl-6-0-desosaminyl-15-ethyl- 7,13,14-trihydroxy-3,5,7,9,12,14-hexamethyl- oxacyclopentadecane-2-one and their derivatives
SI8110592A8 (en) * 1981-03-06 1996-06-30 Pliva Pharm & Chem Works Process for preparing of n-methyl-11-aza-10-deoxo-10-dihydroerythromycine a and derivatives thereof
US4474768A (en) * 1982-07-19 1984-10-02 Pfizer Inc. N-Methyl 11-aza-10-deoxo-10-dihydro-erytromycin A, intermediates therefor
YU44599B (en) * 1986-09-12 1990-10-31 Pliva Pharm & Chem Works Process for preparing complex of n-methyl-11-aza-10-deoxo-10-dihydroeritromicine a and 11-aza-10-deoxo-10-dihydroeritromicine a with metals
US5106961A (en) 1987-05-26 1992-04-21 Eli Lilly And Company Erythromycin ring-contracted derivatives
SI9011409A (en) 1990-07-18 1995-10-31 Pliva Pharm & Chem Works O-methyl azitromycin derivates, methods and intermediates for their preparation and methods for preparation of pharmaceuticals products which comprise them
HRP931480B1 (en) * 1993-12-08 1997-08-31 Sour Pliva 9a-N-(N'-CARBAMONYL) and 9a-N-(N'-THIOCARBAMONYL) DERIVATES OF 9-DEOXO-9a-HOMOERYTHROMYCIN A
GB2327084A (en) * 1997-07-08 1999-01-13 Merck & Co Inc 9a-Aza-3-ketolide antibiotics
UA70972C2 (uk) * 1998-11-20 2004-11-15 Пфайзер Продактс Інк. 13-членні азаліди і їх застосування як антибіотиків

Also Published As

Publication number Publication date
GT199900198A (es) 2001-05-11
WO2000031097A1 (en) 2000-06-02
NO20012464L (no) 2001-07-17
NO20050904L (no) 2001-07-17
CZ303099B6 (cs) 2012-04-04
JP3842973B2 (ja) 2006-11-08
PE20001378A1 (es) 2000-12-14
NO329629B1 (no) 2010-11-22
CA2351429A1 (en) 2000-06-02
DE69915336T2 (de) 2005-01-13
HUP0104313A2 (hu) 2002-02-28
PA8485601A1 (es) 2000-09-29
PL198580B1 (pl) 2008-06-30
IL189430A (en) 2010-05-31
HRP20010374B1 (en) 2006-09-30
CA2351429C (en) 2005-07-12
NO20012464D0 (no) 2001-05-18
OA11713A (en) 2005-01-25
ES2216581T3 (es) 2004-10-16
EA005156B1 (ru) 2004-12-30
NO330249B1 (no) 2011-03-14
TWI243824B (en) 2005-11-21
HK1041269A1 (zh) 2002-07-05
MY122353A (en) 2006-04-29
KR20010086043A (ko) 2001-09-07
KR100477774B1 (ko) 2005-03-21
ID28548A (id) 2001-05-31
DZ2944A1 (fr) 2004-03-15
JP2002530422A (ja) 2002-09-17
HUP0104313A3 (en) 2003-12-29
CN1326460A (zh) 2001-12-12
YU33401A (sh) 2004-05-12
EP1131331B1 (en) 2004-03-03
BRPI9915480B8 (pt) 2022-05-10
ME00467B (me) 2011-10-10
BR9915480A (pt) 2001-07-31
TW200404077A (en) 2004-03-16
SK284607B6 (sk) 2005-07-01
UA70972C2 (uk) 2004-11-15
US6329345B1 (en) 2001-12-11
BRPI9915480B1 (pt) 2015-12-29
CZ20011754A3 (cs) 2002-03-13
EG23823A (en) 2007-09-19
TNSN99214A1 (fr) 2005-11-10
ZA200104019B (en) 2002-06-17
EA200100416A1 (ru) 2001-10-22
EP1131331A1 (en) 2001-09-12
ATE260927T1 (de) 2004-03-15
IS5918A (is) 2001-04-17
IL142631A0 (en) 2002-03-10
PT1131331E (pt) 2004-06-30
HRP20010374A2 (en) 2002-06-30
IL189430A0 (en) 2008-06-05
AP2001002142A0 (en) 2001-05-09
IL142631A (en) 2010-05-31
CN101367853A (zh) 2009-02-18
EA200400701A1 (ru) 2004-12-30
PL347784A1 (en) 2002-04-22
UY25805A1 (es) 2001-08-27
SI1131331T1 (en) 2004-08-31
NZ511199A (en) 2003-08-29
DE69915336D1 (de) 2004-04-08
MA26707A1 (fr) 2004-12-20
RS50302B (sr) 2009-09-08
AU1068600A (en) 2000-06-13
BG105600A (en) 2001-12-29
NO20050893L (no) 2001-07-17
IS2350B (is) 2008-04-15
AR059523A2 (es) 2008-04-09
AR059524A2 (es) 2008-04-09
EA009729B1 (ru) 2008-02-28
NO319796B1 (no) 2005-09-19
SK6632001A3 (en) 2002-07-02
DK1131331T3 (da) 2004-06-14
BG65107B1 (bg) 2007-02-28
AR019496A1 (es) 2002-02-20
AU766106B2 (en) 2003-10-09
HU229008B1 (en) 2013-07-29
TWI243825B (en) 2005-11-21

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