CO6311102A2 - Derivados carboxílicos y alcoxi de 4-sustituido-2-[4-({(5-metil-1h-pirrol -2-il) carbonil} amino)- piperidin sustituido -1-il]-1,3-tiazol como inhibidores de dna girasa y/o topoisomerasa iv y composiciones farmacéuticas de los mismos - Google Patents

Derivados carboxílicos y alcoxi de 4-sustituido-2-[4-({(5-metil-1h-pirrol -2-il) carbonil} amino)- piperidin sustituido -1-il]-1,3-tiazol como inhibidores de dna girasa y/o topoisomerasa iv y composiciones farmacéuticas de los mismos

Info

Publication number
CO6311102A2
CO6311102A2 CO10001889A CO10001889A CO6311102A2 CO 6311102 A2 CO6311102 A2 CO 6311102A2 CO 10001889 A CO10001889 A CO 10001889A CO 10001889 A CO10001889 A CO 10001889A CO 6311102 A2 CO6311102 A2 CO 6311102A2
Authority
CO
Colombia
Prior art keywords
4alkyl
methyl
amino
carbamoyl
girasa
Prior art date
Application number
CO10001889A
Other languages
English (en)
Inventor
Gregory Basarab
Pamela Hill
Fei Zhou
Original Assignee
Astrazeneca Ab
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 Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of CO6311102A2 publication Critical patent/CO6311102A2/es

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Classifications

    • 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
    • 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
    • A61P31/12Antivirals
    • 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

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

1.- Un compuesto de fórmula (Ia):R1 es cloro o ciano;R2E es hidrógeno, cloro, ciano o metilo;R3 es fluoro, metilo, metoxi, etoxi, propoxi, aliloxi y benciloxi;R4 es hidrógeno o C1-4alquilo;El anillo A es carbociclilo o heterociclilo; donde si dicho heterociclilo contiene un resto -NH-, dicho nitrógeno puede estar opcionalmente sustituido por un grupo seleccionado de R6; y donde si dicho heterociclilo contiene un resto -N=, dicho nitrógeno puede formar un compuesto cuaternario con un grupo metilo;R5 es un sustituyente de un carbono y se selecciona entre halo, nitro, ciano, hidroxi, amino, carboxi, carbamoílo, mercapto, sulfamoílo, sulfo, formilo, ureido, hidroxiiminometilo, N-hidroxiformamido, hidrazinocarbonilo, N-hidroxietanimidoílo, amino(hidroxiimino)metilo,C1-4alquilo, C2-4alquenilo, C2-4alquinilo, C1-4aIcoxi, C1-4alcanoílo, C1-4alcanoiloxi,N-(C1-4alquil)amino, N,N-(C1-4alquil)2amino, C1-4alcanoilamino, N-(C1-4alquil)carbamoílo,N,N-(C1-4alquil)2carbamoílo, N-(C1-4alcoxi)carbamoílo, NE-(C1-4alquil)ureido,NE,NE-(C1-4alquil)2ureido, N-(C1-4alquil)-N-(C1- 4alcoxi)carbamoílo, C1-4alquilS(O)a donde a es 0-2, C1- 4alcoxicarbonilo, C1-4alcoxicarbonilamino, N-(C1- 4alquil)sulfamoílo, N,N-(C1-4alquil)2sulfamoílo, C1-4alquilsulfonilamino, C1-4alquilsulfonilaminocarbonilo, NE-(C1-4alquil)hidrazinocarbonilo, NE,NE-(C1-4alquil)2hidrazinocarbonilo, carbociclil-R7- o heterociclil-R8-; donde R5 puede estar opcionalmente sustituido en un carbono por uno o más R9; y donde si dicho heterociclilo contiene un resto -NH-, dicho nitrógeno puede estar opcionalmente sustituido por un grupo seleccionado de R10; n es 0, 1, 2 ó 3; ...
CO10001889A 2007-06-12 2010-01-08 Derivados carboxílicos y alcoxi de 4-sustituido-2-[4-({(5-metil-1h-pirrol -2-il) carbonil} amino)- piperidin sustituido -1-il]-1,3-tiazol como inhibidores de dna girasa y/o topoisomerasa iv y composiciones farmacéuticas de los mismos CO6311102A2 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US94344007P 2007-06-12 2007-06-12

Publications (1)

Publication Number Publication Date
CO6311102A2 true CO6311102A2 (es) 2011-08-22

Family

ID=39673349

Family Applications (1)

Application Number Title Priority Date Filing Date
CO10001889A CO6311102A2 (es) 2007-06-12 2010-01-08 Derivados carboxílicos y alcoxi de 4-sustituido-2-[4-({(5-metil-1h-pirrol -2-il) carbonil} amino)- piperidin sustituido -1-il]-1,3-tiazol como inhibidores de dna girasa y/o topoisomerasa iv y composiciones farmacéuticas de los mismos

Country Status (30)

Country Link
US (1) US20080312255A1 (es)
EP (1) EP2158199B1 (es)
JP (1) JP2010529184A (es)
KR (1) KR20100038095A (es)
CN (1) CN102648199A (es)
AR (1) AR066977A1 (es)
AT (1) ATE488514T1 (es)
AU (1) AU2008263580A1 (es)
BR (1) BRPI0812473A2 (es)
CA (1) CA2689076A1 (es)
CL (1) CL2008001740A1 (es)
CO (1) CO6311102A2 (es)
CY (1) CY1111442T1 (es)
DE (1) DE602008003575D1 (es)
DK (1) DK2158199T3 (es)
ES (1) ES2354647T3 (es)
HK (1) HK1140198A1 (es)
HR (1) HRP20110048T1 (es)
IL (1) IL202367A0 (es)
MX (1) MX2009013501A (es)
NZ (1) NZ582516A (es)
PE (1) PE20090555A1 (es)
PL (1) PL2158199T3 (es)
PT (1) PT2158199E (es)
RU (1) RU2010100352A (es)
SA (1) SA08290357B1 (es)
SI (1) SI2158199T1 (es)
TW (1) TW200906412A (es)
UY (1) UY31141A1 (es)
WO (1) WO2008152418A1 (es)

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UA94901C2 (ru) 2005-02-18 2011-06-25 Астразенека Аб Антибактериальные производные пиперидина
TW201026695A (en) * 2008-12-12 2010-07-16 Astrazeneca Ab Piperidine compounds and uses thereof-596
TW201026694A (en) * 2008-12-12 2010-07-16 Astrazeneca Ab Compound 468
WO2011024004A1 (en) 2009-08-26 2011-03-03 Astrazeneca Ab Heterocyclic urea derivatives useful for treatment of bacterial infection
US20150174034A1 (en) 2013-03-13 2015-06-25 Avon Products, Inc. Tyrosinase inhibitors
WO2014164195A1 (en) * 2013-03-13 2014-10-09 Avon Products, Inc Tyrosinase inhibitors
CN108137574B (zh) 2015-09-30 2021-12-28 第一三共株式会社 羟烷基噻二唑衍生物
JP2020511457A (ja) 2017-03-14 2020-04-16 第一三共株式会社 ヒドロキシアルキルチアジアゾール誘導体のn−ホスホノキシメチルプロドラッグ
JPWO2018174288A1 (ja) 2017-03-24 2020-01-23 大正製薬株式会社 2(1h)−キノリノン誘導体
US20210323957A1 (en) 2018-09-03 2021-10-21 Univerza V Ljubljani New class of dna gyrase and/or topoisomerase iv inhibitors with activity against gram-positive and gram-negative bacteria
CN110172435B (zh) * 2019-06-06 2020-12-29 江南大学 一种催化合成2,5-二甲基吡嗪的重组菌
WO2022129327A1 (en) 2020-12-17 2022-06-23 Univerza V Ljubljani New n-phenylpyrrolamide inhibitors of dna gyrase and topoisomerase iv with antibacterial activity
CN115466246B (zh) * 2021-06-11 2024-02-06 中国医学科学院药物研究所 吡咯酰哌啶胺类化合物及其用途

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US3963480A (en) * 1973-04-11 1976-06-15 Sterling Drug Inc. Herbicidal pyrrole-2-carboxamides
US4046775A (en) * 1973-04-11 1977-09-06 Sterling Drug Inc. 4,5-Dihalopyrrole-2-carboxamides
US4791112A (en) * 1987-02-02 1988-12-13 The Boc Group, Inc. N-heterocyclic-N-(4-piperidyl)amides and pharmaceutical compositions and methods employing such compounds
US4912109A (en) * 1987-02-02 1990-03-27 Boc, Inc. N-heterocyclic-N-(4-piperidinyl) amides and pharmaceutical compositions and methods employing such compounds
US5739135A (en) * 1993-09-03 1998-04-14 Bristol-Myers Squibb Company Inhibitors of microsomal triglyceride transfer protein and method
BR0107713A (pt) * 2000-01-18 2002-11-19 Vertex Pharma Inibidores de girase e usos dos mesmos
DE60309701T2 (de) * 2002-06-13 2007-09-06 Vertex Pharmaceuticals Inc., Cambridge 2-ureido-6-heteroaryl-3h-benzoimidazol-4-carbonsäurederivate und verwandte verbindungen als gyrase und/oder topoisomerase iv inhibitoren zur behandlung von bakteriellen infektionen
TW200526626A (en) * 2003-09-13 2005-08-16 Astrazeneca Ab Chemical compounds
GB0321509D0 (en) * 2003-09-13 2003-10-15 Astrazeneca Ab Chemical compounds
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Also Published As

Publication number Publication date
DK2158199T3 (da) 2011-02-07
US20080312255A1 (en) 2008-12-18
CN102648199A (zh) 2012-08-22
MX2009013501A (es) 2010-01-18
IL202367A0 (en) 2010-06-30
UY31141A1 (es) 2009-01-30
PT2158199E (pt) 2011-01-19
ES2354647T3 (es) 2011-03-16
BRPI0812473A2 (pt) 2014-12-02
RU2010100352A (ru) 2011-07-20
JP2010529184A (ja) 2010-08-26
WO2008152418A1 (en) 2008-12-18
AR066977A1 (es) 2009-09-23
PE20090555A1 (es) 2009-06-04
DE602008003575D1 (de) 2010-12-30
EP2158199B1 (en) 2010-11-17
EP2158199A1 (en) 2010-03-03
SI2158199T1 (sl) 2011-02-28
SA08290357B1 (ar) 2011-06-22
PL2158199T3 (pl) 2011-04-29
AU2008263580A1 (en) 2008-12-18
TW200906412A (en) 2009-02-16
HK1140198A1 (en) 2010-10-08
CA2689076A1 (en) 2008-12-18
NZ582516A (en) 2012-03-30
ATE488514T1 (de) 2010-12-15
CY1111442T1 (el) 2015-08-05
KR20100038095A (ko) 2010-04-12
CL2008001740A1 (es) 2009-07-17
HRP20110048T1 (hr) 2011-03-31

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