AR042583A1 - Macrolidos - Google Patents

Macrolidos

Info

Publication number
AR042583A1
AR042583A1 ARP010105997A ARP010105997A AR042583A1 AR 042583 A1 AR042583 A1 AR 042583A1 AR P010105997 A ARP010105997 A AR P010105997A AR P010105997 A ARP010105997 A AR P010105997A AR 042583 A1 AR042583 A1 AR 042583A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
nitrogen
alkyl
elements
oxygen
Prior art date
Application number
ARP010105997A
Other languages
English (en)
Original Assignee
Glaxo Group Ltd
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
Priority claimed from GB0031309A external-priority patent/GB0031309D0/en
Priority claimed from GB0126277A external-priority patent/GB0126277D0/en
Priority claimed from GB0126276A external-priority patent/GB0126276D0/en
Application filed by Glaxo Group Ltd filed Critical Glaxo Group Ltd
Publication of AR042583A1 publication Critical patent/AR042583A1/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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • 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

Abstract

La presente se refiere a cetólidos de 11, 12-gama lactona de la fórmula (1), en donde: R es hidrógeno, ciano, (CH2)nA-X-R4 o (CH2)nR5; A es un grupo seleccionado de -N(R6)-, -N[C(O)R6]-, -N(R6)C(O)-, -N(R6)S(O)2- , -N(R6)C(O)O-, N=C(R6) o N(R6)C(Y)N(R7)-; R1 es alquilo C1-6 o alquenilo C3-6; R2 es hidrógeno o un grupo protector hidroxilo; R3 es hidrógeno o halógeno; X es un enlace, un alquenilo C1-10, un alquinileno C2-10 o una cadena alquinileno C2-10 en donde dicha cadena está: i) interrumpida opcionalmente por un grupo radical bivalente seleccionado de -O-, -N(R8)-, -C(O)-, -N(R8)C(Y)N(R9)-, -S(O)m-, -N(R8)C(O)-, -C(O)N(R8)-, -N(R8)C(O)C(O)-, -C(O)O- o -C(NOR6)- y/o ii) sustituida opcionalmente por uno o dos grupos seleccionados de: alquilo C1-4, oxo, alcoxi C1-4, halógeno, ciano, fenoxi, hidroxi, NR8R9, N(R8)C(O)R9, =NOR6, NR8C(Y)NR9 o fenilo opcionalmente sustituido; R4 se selecciona de: hidrógeno, fenilo opcionalmente sustituido, cicloalquilo C3-7 opcionalmente sustituido, carbocíclico bicíclico fusionado de 9 a 10 elementos opcionalmente sustituido, heteroarilo de 5 ó 6 elementos opcionalmente sustituido en el cual el heteroarilo de 5 elementos contiene al menos un heteroátomos seleccionado de oxígeno, azufre o nitrógeno y el grupo heteroarilo de 6 elementos contiene de 1 a 3 átomos de nitrógeno, heterocíclico de 5 ó 6 elementos opcionalmente sustituido, o R4 es un heterocíclico bicíclico fusionado 9 ó 10 elementos opcionalmente sustituido que tiene al menos un heteroátomo seleccionado de oxígeno, azufre o nitrógeno; R5 es un heterocíclico de 5 ó 6 elementos que contiene al menos un nitrógeno, opcionalmente sustituido, por uno o dos grupos seleccionados de oxo o heterocíclico bicíclico fusionado de 9 a 10 elementos que tiene al menos un heteroátomo seleccionado de oxígeno, azufre o nitrógeno; R6 y R7 son independientemente hidrógeno, alquilo C1-4 o fenilo el cual opcionalmente sustituido por uno o dos grupos alquilo C1-4; R8 y R9 son independientemente hidrógeno, fenilo (el cual puede estar sustituido por uno o dos alquilo C1-4) o R8 y R9 son independientemente alquilo C1-4 el cual es opcionalmente sustituido por 1 ó 2 grupos seleccionados de: fenilo, alcoxi C1-4, ciano, heteroarilo de 5 elementos que contiene 1 ó 2 heteroátomos seleccionados de oxígeno, azufre o nitrógeno o el grupo heteroarilo de 6 elementos de 1 ó 3 átomos de nitrógeno, hidroxi, oxo, carboxi; Y es un oxígeno o un átomo de azufre, n es 0 o un entero de 1 a 3; , es 0, 1 ó 2; y sales y solvatos del mismo farmacéuticamente aceptables, a procesos para su preparación y su uso en la terapia o profilaxis de infecciones bacterianas sistémicas o tópicas en un cuerpo humano o animal.
ARP010105997A 2000-12-21 2001-12-21 Macrolidos AR042583A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB0031309A GB0031309D0 (en) 2000-12-21 2000-12-21 Macrolides
GB0126277A GB0126277D0 (en) 2001-11-01 2001-11-01 Macrolides
GB0126276A GB0126276D0 (en) 2001-11-01 2001-11-01 Macolides

Publications (1)

Publication Number Publication Date
AR042583A1 true AR042583A1 (es) 2005-06-29

Family

ID=27256023

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP010105997A AR042583A1 (es) 2000-12-21 2001-12-21 Macrolidos

Country Status (20)

Country Link
US (3) US20040077557A1 (es)
EP (1) EP1363925B8 (es)
JP (1) JP2004531471A (es)
KR (1) KR20030068189A (es)
CN (1) CN1492874A (es)
AR (1) AR042583A1 (es)
AT (1) ATE345350T1 (es)
AU (2) AU1727702A (es)
BR (1) BR0116431A (es)
CA (1) CA2432429A1 (es)
CZ (1) CZ20031751A3 (es)
DE (1) DE60124594T2 (es)
ES (1) ES2275621T3 (es)
HU (1) HUP0302526A2 (es)
IL (1) IL156561A0 (es)
MX (1) MXPA03005668A (es)
NO (1) NO20032846L (es)
NZ (1) NZ526450A (es)
PL (1) PL365012A1 (es)
WO (1) WO2002050091A1 (es)

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Also Published As

Publication number Publication date
WO2002050091A1 (en) 2002-06-27
EP1363925B8 (en) 2007-04-25
AU1727702A (en) 2002-07-01
ES2275621T3 (es) 2007-06-16
US20060211636A1 (en) 2006-09-21
EP1363925A1 (en) 2003-11-26
EP1363925B1 (en) 2006-11-15
ATE345350T1 (de) 2006-12-15
CN1492874A (zh) 2004-04-28
PL365012A1 (en) 2004-12-27
MXPA03005668A (es) 2004-12-03
KR20030068189A (ko) 2003-08-19
AU2002217277B2 (en) 2005-06-16
BR0116431A (pt) 2004-06-22
DE60124594D1 (de) 2006-12-28
NZ526450A (en) 2005-04-29
HUP0302526A2 (hu) 2003-11-28
NO20032846L (no) 2003-08-20
CZ20031751A3 (cs) 2004-03-17
CA2432429A1 (en) 2002-06-27
NO20032846D0 (no) 2003-06-20
IL156561A0 (en) 2004-01-04
DE60124594T2 (de) 2007-10-04
US20050215495A1 (en) 2005-09-29
JP2004531471A (ja) 2004-10-14
US20040077557A1 (en) 2004-04-22

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