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CO4940506A1 - DERIVATIVES OF 9-OXYME ERYTHROMYCIN - Google Patents

DERIVATIVES OF 9-OXYME ERYTHROMYCIN

Info

Publication number
CO4940506A1
CO4940506A1 CO98033538A CO98033538A CO4940506A1 CO 4940506 A1 CO4940506 A1 CO 4940506A1 CO 98033538 A CO98033538 A CO 98033538A CO 98033538 A CO98033538 A CO 98033538A CO 4940506 A1 CO4940506 A1 CO 4940506A1
Authority
CO
Colombia
Prior art keywords
alkyl
integer
optionally substituted
formula xvi
ring
Prior art date
Application number
CO98033538A
Other languages
Spanish (es)
Inventor
Wu Tong-Jin
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 CO4940506A1 publication Critical patent/CO4940506A1/en

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7048Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C07H17/04Heterocyclic radicals containing only oxygen as ring hetero atoms
    • C07H17/08Hetero rings containing eight or more ring members, e.g. erythromycins

Landscapes

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

Abstract

Un compuesto de la fórmula 1 o una sal farmacéuticamenteaceptable del mismo, en la que X es -CR7 R8 -o-NR7 -; o X es junto con R2 forma N=CR4 R5 ; o X y R2 juntos forman un anillo heterocíclico de fórmula XVI:En la que dicho anillo de fórmula XVI, r y p son cada uno de ellos independientemente un número entero de 1 a 3, q es O ó 1 y X1 es -CH2 -, O, -C(O)-, -C(S)-, -CH=CH-, CH(OH)CH(OH)-, o -NH-; y donde las partes (CH2 )r y (CH2 )p de dicho anillo de fórmula XVI están opcionalmente sustituidas con 1 a 4 sustituyentes y el átomo de nitrógeno cuando X1 es -NH- está opcionalmente sustituido con 1 sustituyente, estando dichos sustituyentes opcionales independientemente seleccionados entre el grupo constituido por -C(O) o (alquilo C1 -C10 ), alcoxi C1 -C10 , alcanoílo C1 -C10 , halógeno, nitro, ciano, heterociclilo de 5-10 elementos, alquilo C1 -C10 , -NR7 R8 , arilo C6 -C10 , -S(O)n (alquilo C1 -C10 ) donde n es un número entero de 0 a 2, y -SO2 NR7 R8 ; R1 es H o alquilo C1 -C10 , donde 1 a 3 carbonos de dicho alquilo están opcionalmente remplazados por un hetero+atomo seleccionado entre O, S y N, estando dicho alquilo opcionalmente sustituido con 1 a 3 sustituyentes seleccionados independientemente entre el grupo constituido por -C(O) O (alquilo C1 -C10 ), alcoxi C1 -C10 , alcanoílo C1 -C10 , halógeno, nitro, ciano, heterociclilo de 5-10 elementos, alquilo C1 -C10 , -NR7 R8 , arilo C1 -C10 , -S(O)n (alquilo C1 -C10 ) donde n es un número entero de 0 a 2 , y -SO2 NR7 R8 ; R2 es (y) H; R4 , -C(=)R4 , -C(O)OR4 , o -(CR7 R8 )m R3 cuando X es -NR7 -, o (II) H, R4 , o -CR7 R8 -, donde para ambos (i) y (ii) m es un número entero de 0 a 6 y tanto R7 como R8 pueden variar en cada caso en que m sea mayor que 1;...A compound of formula 1 or a pharmaceutically acceptable salt thereof, wherein X is -CR7 R8 -o-NR7 -; or X is together with R2 form N = CR4 R5; or X and R2 together form a heterocyclic ring of formula XVI: Wherein said ring of formula XVI, r and p are each independently an integer from 1 to 3, q is O or 1 and X1 is -CH2 -, O , -C (O) -, -C (S) -, -CH = CH-, CH (OH) CH (OH) -, or -NH-; and where the (CH2) r and (CH2) p parts of said ring of formula XVI are optionally substituted with 1 to 4 substituents and the nitrogen atom when X1 is -NH- is optionally substituted with 1 substituent, said optional substituents being independently selected between the group consisting of -C (O) or (C1-C10 alkyl), C1-C10 alkoxy, C1-C10 alkanoyl, halogen, nitro, cyano, 5-10-membered heterocyclyl, C1-C10 alkyl, -NR7 R8, C6 -C10 aryl, -S (O) n (C1-C10 alkyl) where n is an integer from 0 to 2, and -SO2 NR7 R8; R1 is H or C1-C10 alkyl, where 1 to 3 carbons of said alkyl are optionally replaced by a hetero + atom selected from O, S and N, said alkyl being optionally substituted with 1 to 3 substituents independently selected from the group consisting of -C (O) O (C1-C10 alkyl), C1-C10 alkoxy, C1-C10 alkanoyl, halogen, nitro, cyano, 5-10 membered heterocyclyl, C1-C10 alkyl, -NR7 R8, C1-C10 aryl, -S (O) n (C1-C10 alkyl) where n is an integer from 0 to 2, and -SO2 NR7 R8; R2 is (y) H; R4, -C (=) R4, -C (O) OR4, or - (CR7 R8) m R3 when X is -NR7 -, or (II) H, R4, or -CR7 R8 -, where for both (i ) and (ii) m is an integer from 0 to 6 and both R7 and R8 may vary in each case where m is greater than 1; ...

CO98033538A 1997-06-11 1998-06-11 DERIVATIVES OF 9-OXYME ERYTHROMYCIN CO4940506A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US4934997P 1997-06-11 1997-06-11

Publications (1)

Publication Number Publication Date
CO4940506A1 true CO4940506A1 (en) 2000-07-24

Family

ID=21959341

Family Applications (1)

Application Number Title Priority Date Filing Date
CO98033538A CO4940506A1 (en) 1997-06-11 1998-06-11 DERIVATIVES OF 9-OXYME ERYTHROMYCIN

Country Status (31)

Country Link
EP (1) EP0988308A1 (en)
JP (1) JP2000513026A (en)
KR (1) KR20010013660A (en)
CN (1) CN1259135A (en)
AP (1) AP9801253A0 (en)
AR (1) AR012244A1 (en)
AU (1) AU7226798A (en)
BG (1) BG103947A (en)
BR (1) BR9810021A (en)
CA (1) CA2293335A1 (en)
CO (1) CO4940506A1 (en)
CZ (1) CZ9904388A3 (en)
EA (1) EA199901016A1 (en)
GT (1) GT199800074A (en)
HN (1) HN1998000073A (en)
HR (1) HRP980316A2 (en)
HU (1) HUP0002252A3 (en)
ID (1) ID24529A (en)
IL (1) IL132767A0 (en)
IS (1) IS5251A (en)
MA (1) MA26505A1 (en)
NO (1) NO996108L (en)
OA (1) OA11225A (en)
PA (1) PA8451801A1 (en)
PE (1) PE79899A1 (en)
PL (1) PL337606A1 (en)
TN (1) TNSN98083A1 (en)
TR (1) TR199902995T2 (en)
TW (1) TW448174B (en)
WO (1) WO1998056800A1 (en)
ZA (1) ZA985018B (en)

Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HN1998000159A (en) * 1997-10-29 1999-02-09 Monsanto Co DERIVATIVES OF 9- AMINO - 3 CETO ERITROMICINA
ES2243066T3 (en) * 1998-09-22 2005-11-16 Pfizer Products Inc. CARBAMATE AND CETOLID CARBAZATE ANTIBIOTICS.
FR2786188B1 (en) * 1998-11-24 2002-10-31 Hoechst Marion Roussel Inc NOVEL ERYTHROMYCIN DERIVATIVES, THEIR PREPARATION PROCESS AND THEIR APPLICATION AS MEDICAMENTS
US6258785B1 (en) 1998-12-02 2001-07-10 Pfizer Inc. Crystalline 9-E-(O-methyl)oxime of 11, 12-dideoxy-3-de(2,6-dideoxy-3-C-methyl-3-O-methyl-α-L-ribohexopyranosyloxy)-6-O-methyl-12,11-(iminocarbonyl-(2-(3-(4-(3-pyridinyl)1H-imadazol-1-yl)propyl)hydrazono))-3-oxoerythromycin
EP1298138B1 (en) * 1998-12-10 2006-11-02 Pfizer Products Inc. Carbamate and Carbazate Ketolide Antibiotics
US6284732B1 (en) * 1998-12-18 2001-09-04 Bio-Rad Laboratories, Inc. Peptides and peptide analogues designed from HFE protein and their uses in the treatment of iron overload diseases
ATE340183T1 (en) * 1999-04-16 2006-10-15 Kosan Biosciences Inc ANTINIFECTIVE MACROLIDE DERIVATIVES
HK1045523A1 (en) 1999-05-24 2002-11-29 辉瑞产品公司 13-methyl erythromycin derivatives
DK1181300T3 (en) * 1999-06-07 2004-01-26 Abbott Lab 6-O-carbamate ketolide derivatives
ID27331A (en) * 1999-09-29 2001-03-29 Pfizer Prod Inc MAKING ANTIBIOTIC-ANTIBIOTIC KETOLIDA CARBAMATE
EP1114826A3 (en) * 1999-12-29 2001-10-31 Pfizer Products Inc. Novel antibacterial and prokinetic macrolides
EP1439186A3 (en) * 1999-12-29 2004-11-03 Pfizer Products Inc. Intermediates for novel antibacterial and prokinetic macrolides
US6946446B2 (en) 2000-02-24 2005-09-20 Abbott Laboratories Anti-infective agents useful against multidrug-resistant strains of bacteria
US6403776B1 (en) 2000-07-05 2002-06-11 Pfizer Inc. Synthesis of carbamate ketolide antibiotics
WO2003090761A1 (en) * 2002-04-25 2003-11-06 Abbott Laboratories 9-oxime macrolide antibacterials
US7091196B2 (en) 2002-09-26 2006-08-15 Rib-X Pharmaceuticals, Inc. Bifunctional heterocyclic compounds and methods of making and using same
EP1638549A4 (en) * 2003-03-10 2011-06-15 Optimer Pharmaceuticals Inc NEW ANTIBACTERIAL AGENTS
EP1723159B1 (en) 2004-02-27 2019-06-12 Melinta Therapeutics, Inc. Macrocyclic compounds and methods of making and using the same
US9453042B2 (en) 2007-10-25 2016-09-27 Cempra Pharmaceuticals, Inc. Process for the preparation of macrolide antibacterial agents
HRP20160222T1 (en) 2008-10-24 2016-04-08 Cempra Pharmaceuticals, Inc. BE PROTECTED BY USING TRIAZOLE CONTROLLED MACROLIDE
US9937194B1 (en) 2009-06-12 2018-04-10 Cempra Pharmaceuticals, Inc. Compounds and methods for treating inflammatory diseases
EP2475253B1 (en) 2009-09-10 2016-10-26 Cempra Pharmaceuticals, Inc. Methods for treating malaria, tuberculosis and mac diseases
CN102146085B (en) * 2010-02-09 2014-03-26 北京理工大学 9-oxime-ether ketolide derivative, and preparation method and medical composite thereof
JP5711352B2 (en) 2010-03-22 2015-04-30 センプラ ファーマシューティカルズ,インコーポレイテッド Macrolide crystal forms and their use
CN102917708B (en) 2010-05-20 2015-11-25 森普拉制药公司 Process for preparing macrolides and ketolides and intermediates thereof
US9815863B2 (en) 2010-09-10 2017-11-14 Cempra Pharmaceuticals, Inc. Hydrogen bond forming fluoro ketolides for treating diseases
IN2014DN08939A (en) 2012-03-27 2015-05-22 Cempra Pharmaceuticals Inc
CA2905975A1 (en) 2013-03-14 2014-09-25 Cempra Pharmaceuticals, Inc. Methods for treating respiratory diseases and formulations therefor
EP2968384A4 (en) 2013-03-15 2017-02-15 Cempra Pharmaceuticals, Inc. Convergent processes for preparing macrolide antibacterial agents

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL114589A (en) * 1990-11-21 1999-12-22 Roussel Uclaf Intermediates for the preparation of erythromycin derivatives
US5527780A (en) * 1992-11-05 1996-06-18 Roussel Uclaf Erythromycin derivatives
FR2718450B1 (en) * 1994-04-08 1997-01-10 Roussel Uclaf New erythromycin derivatives, their preparation process and their use as drugs.

Also Published As

Publication number Publication date
HRP980316A2 (en) 1999-04-30
NO996108D0 (en) 1999-12-10
IL132767A0 (en) 2001-03-19
NO996108L (en) 2000-02-10
TR199902995T2 (en) 2000-02-21
KR20010013660A (en) 2001-02-26
CZ9904388A3 (en) 2002-10-16
HUP0002252A2 (en) 2000-12-28
WO1998056800A1 (en) 1998-12-17
ID24529A (en) 2000-07-20
CA2293335A1 (en) 1998-12-17
AP9801253A0 (en) 1999-12-04
JP2000513026A (en) 2000-10-03
BR9810021A (en) 2000-09-19
CN1259135A (en) 2000-07-05
IS5251A (en) 1999-11-16
TNSN98083A1 (en) 2005-03-15
MA26505A1 (en) 2004-12-20
BG103947A (en) 2000-07-31
PA8451801A1 (en) 2000-05-24
EA199901016A1 (en) 2000-06-26
ZA985018B (en) 1999-12-10
PE79899A1 (en) 1999-08-25
GT199800074A (en) 1999-11-27
TW448174B (en) 2001-08-01
HN1998000073A (en) 1999-01-08
PL337606A1 (en) 2000-08-28
EP0988308A1 (en) 2000-03-29
HUP0002252A3 (en) 2002-01-28
AU7226798A (en) 1998-12-30
OA11225A (en) 2003-07-17
AR012244A1 (en) 2000-09-27

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