CO5261612A1 - Inhibidores de girasa y usos de esta - Google Patents

Inhibidores de girasa y usos de esta

Info

Publication number
CO5261612A1
CO5261612A1 CO01003497A CO01003497A CO5261612A1 CO 5261612 A1 CO5261612 A1 CO 5261612A1 CO 01003497 A CO01003497 A CO 01003497A CO 01003497 A CO01003497 A CO 01003497A CO 5261612 A1 CO5261612 A1 CO 5261612A1
Authority
CO
Colombia
Prior art keywords
aliphatic
ring
optionally substituted
hydrogen
heteroaryl
Prior art date
Application number
CO01003497A
Other languages
English (en)
Inventor
Paul S Charifson
Dean Stamos
Michael Badia
Anne-Laure Grillot
Steven Ronkin
Martin Trudeau
Original Assignee
Vertex Pharma
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 Vertex Pharma filed Critical Vertex Pharma
Publication of CO5261612A1 publication Critical patent/CO5261612A1/es

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/41551,2-Diazoles non condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42Oxazoles
    • A61K31/4211,3-Oxazoles, e.g. pemoline, trimethadione
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42Oxazoles
    • A61K31/422Oxazoles not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • A61P31/06Antibacterial agents for tuberculosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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 three or more hetero rings
    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Communicable Diseases (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Un método para tratar una infección bacterial en un mamífero en necesidad de ello, comprende la etapa de administrar a dicho mamífero una cantidad terapéuticamente efectiva de un compuesto que tiene la fórmula: <EMI FILE="01003497_1" ID="1" IMF=JPEG >O una sal farmacéuticamente aceptable de la misma, en donde R1 es un grupo opcionalmente sustituido seleccionado a partir de un grupo alifático con 1 a 6 átomos de carbono, -C(R4)2(CH2)Nnrcor, -C(R4)=N-OR, -C(R4)=N-OC(=O) (C1-6 alifático), C(R4)=NNRCRO, -C(R4)=NN( R )2, -(R4)2(CH2)nNRCO2 (C1-6 alifático), -CO2(C1-6 alifático), -CON(R)2, C(R4)2(CH2)nCON(R)2(CH2)nSO2N(R)2, -C(R4)2(CH2)nSO2N(R)2, -CONH-OR, SO2N(R)2 o -C(R4)2NRSO2(C1-6 alifático), n es cero o uno cada R es independientemente seleccionado de hidrógeno o un grupo alifático C1-6 opcionalmente sustituido; R2 se selecciona de hidrógeno o, cuando R1 es -CO2(C1-3 alifático), R2 se selecciona además de -halo -CN, - C1-4 alifático, un heterocíclico de 3 a 5 miembros, o un heteroarilo de 5 miembros; El anillo A es un anillo de heteroarilo seleccionado de tiazol, oxazol, imidazol o pirazol, en donde dicho imidazol esta opcionalmente unido a un puente C1-3 de un nitrógeno de anillo de imidazol a Ar para formar un anillo fusionado de 5 a 7 miembros; Z es C-R3 o N-R3; R3 es -(CH2)pN(R5)2 o un grupo opcionalmente sustituido seleccionado de C1-6 alifático, heterocíclico, heterocicloalquilo, arilo, aralquilo, heteroarilo o heteroaralquilo; Cada R4 es independientemente seleccionado de hidrógeno, Un grupo alifático C1-6 opcionalmente sustituido, o dos R4 tomados juntos con el carbono al cual ellos están unidos para formar un anillo alifático de 3 a 6 miembros; Cada R5 es independientemente seleccionado de hidrógeno, un grupo alifático C1-4, o dos R5 tomados junto con el nitrógeno al cual ellos están unidos para formar un anillo heterocíclico de 5 a 6 miembros; P es un entero de cero a 4 cuando z es C-R3 o un entero de 1 a 4 cuando z es N-R3; yAr es anillo de arilo heteroarilo, o heterocíclico opcionalmente sustituido.
CO01003497A 2000-01-18 2001-01-18 Inhibidores de girasa y usos de esta CO5261612A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US17667100P 2000-01-18 2000-01-18
US25433100P 2000-12-08 2000-12-08

Publications (1)

Publication Number Publication Date
CO5261612A1 true CO5261612A1 (es) 2003-03-31

Family

ID=26872470

Family Applications (1)

Application Number Title Priority Date Filing Date
CO01003497A CO5261612A1 (es) 2000-01-18 2001-01-18 Inhibidores de girasa y usos de esta

Country Status (23)

Country Link
US (2) US6608087B1 (es)
EP (1) EP1251848B1 (es)
JP (1) JP2003520233A (es)
CN (1) CN1230166C (es)
AR (1) AR027518A1 (es)
AT (1) ATE269701T1 (es)
AU (1) AU782883B2 (es)
BR (1) BR0107713A (es)
CA (1) CA2397686A1 (es)
CO (1) CO5261612A1 (es)
DE (1) DE60103974T2 (es)
DK (1) DK1251848T3 (es)
EA (1) EA005680B1 (es)
ES (1) ES2222336T3 (es)
HK (1) HK1053984B (es)
MX (1) MXPA02007134A (es)
MY (1) MY133572A (es)
NZ (1) NZ520628A (es)
PT (1) PT1251848E (es)
SI (1) SI1251848T1 (es)
TR (1) TR200401735T4 (es)
TW (1) TWI287449B (es)
WO (1) WO2001052845A1 (es)

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US20080234132A1 (en) * 2004-11-19 2008-09-25 Laurence Coquin Microcin B17 Analogs And Methods For Their Preparation And Use
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JP5581219B2 (ja) 2008-01-25 2014-08-27 ミレニアム ファーマシューティカルズ, インコーポレイテッド チオフェンおよびホスファチジルイノシトール3−キナーゼ(pi3k)阻害薬としてのその使用
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Also Published As

Publication number Publication date
US6608087B1 (en) 2003-08-19
DE60103974T2 (de) 2005-06-30
DK1251848T3 (da) 2004-10-18
PT1251848E (pt) 2004-10-29
CN1400898A (zh) 2003-03-05
BR0107713A (pt) 2002-11-19
EP1251848B1 (en) 2004-06-23
JP2003520233A (ja) 2003-07-02
SI1251848T1 (en) 2004-12-31
EA200200769A1 (ru) 2002-12-26
NZ520628A (en) 2004-05-28
HK1053984B (zh) 2006-07-28
CA2397686A1 (en) 2001-07-26
TR200401735T4 (tr) 2004-08-23
WO2001052845A1 (en) 2001-07-26
DE60103974D1 (de) 2004-07-29
EA005680B1 (ru) 2005-04-28
AU782883B2 (en) 2005-09-08
MY133572A (en) 2007-11-30
EP1251848A1 (en) 2002-10-30
ATE269701T1 (de) 2004-07-15
US6930116B2 (en) 2005-08-16
HK1053984A1 (en) 2003-11-14
TWI287449B (en) 2007-10-01
AU3094001A (en) 2001-07-31
AR027518A1 (es) 2003-04-02
ES2222336T3 (es) 2005-02-01
CN1230166C (zh) 2005-12-07
US20040024030A1 (en) 2004-02-05
MXPA02007134A (es) 2003-03-27

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