AR074608A1 - Derivados de 2-(piperidin-1-il)-4-heterociclil-tiazol-5-carboxilico para infecciones bacterianas - Google Patents

Derivados de 2-(piperidin-1-il)-4-heterociclil-tiazol-5-carboxilico para infecciones bacterianas

Info

Publication number
AR074608A1
AR074608A1 ARP090104826A ARP090104826A AR074608A1 AR 074608 A1 AR074608 A1 AR 074608A1 AR P090104826 A ARP090104826 A AR P090104826A AR P090104826 A ARP090104826 A AR P090104826A AR 074608 A1 AR074608 A1 AR 074608A1
Authority
AR
Argentina
Prior art keywords
alkyl
heterocycle
amino
independently selected
optionally substituted
Prior art date
Application number
ARP090104826A
Other languages
English (en)
Inventor
Gregory Steven Basarab
Pamela Hill
Fei Zhou
Brian Sherer
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 AR074608A1 publication Critical patent/AR074608A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic 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
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Otolaryngology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

También se describen procesos para su preparación, composiciones farmacéuticas que los contienen, su uso como medicamentos y uso en el tratamiento de infecciones bacterianas. Reivindicación 1: Un compuesto caracterizado porque es de fórmula (1): una sal farmacéuticamente aceptable del mismo, en donde: R1 es cloro o ciano; R2 es hidrógeno, cloro o ciano; R3 es halo, alquiloC1-4, alcoxiC1-4 o aliloxi; R4 es hidrógeno o alquiloC1-4; el Anillo A se selecciona de la fórmula (2), (3) o (4); en donde: "*" es el punto de unión al anillo de tiazolilo; X es CH, CR o N; R5 es H, un alquiloC1-4 o alcoxiC1-4alquiloC1-4; R6, en cada oportunidad, se selecciona independientemente de halo, -NR7R8, -OR8 y heterociclo en donde dicho heterociclo comprende al menos un miembro nitrógeno del anillo y está opcionalmente sustituido en uno o más átomos de carbono por uno o más R9 y está opcionalmente sustituido en uno o más nitrógenos del anillo por R10; R6 es hidrógeno o R6; R7 y R8 cada uno, independientemente, se selecciona del grupo que consiste en hidrógeno y un aIquiIoC1-6, en donde dicho alquilo está opcionalmerte sustituido por uno o más independientemente seleccionados de -OH, N,N-di(alquilC1-4)amino, un alcoxiC1-6 un alcoxiC1-6aIcoxiC1-6 y heterociclo, en donde dicho heterociclo está opcionalmente sustituido en uno o más átomos de carbono por uno o más independientemente seleccionados de halo, alquiloC1-6 y alcoxiC1-6 y en donde si dicho heterociclilo contiene un resto -NH- dicho nitrógeno puede sustituirse opcionalmente por un alquiloC1-4; R9, en cada oportunidad, se selecciona independientemente de un alquiloC1-4, halo, hidroxi, alcoxiC1-4, amino, N-(alquilC1-4)amino y N,N-di(alquilC1-4)amino; R10, en cada oportunidad, se selecciona independientemente de un alquiloC1-4 opcionalmente sustituido por N,N-di(alquilC1-4)amino, -OH, heterociclo y cicloalquiloC3-6, en donde el heterociclo puede sustituirse opcionalmente por alquilo C1-4; y n es 0, 1, 2 ó 3.
ARP090104826A 2008-12-12 2009-12-11 Derivados de 2-(piperidin-1-il)-4-heterociclil-tiazol-5-carboxilico para infecciones bacterianas AR074608A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US12195308P 2008-12-12 2008-12-12

Publications (1)

Publication Number Publication Date
AR074608A1 true AR074608A1 (es) 2011-01-26

Family

ID=41818426

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP090104826A AR074608A1 (es) 2008-12-12 2009-12-11 Derivados de 2-(piperidin-1-il)-4-heterociclil-tiazol-5-carboxilico para infecciones bacterianas

Country Status (13)

Country Link
US (2) US8071605B2 (es)
EP (1) EP2376488A1 (es)
JP (1) JP2012511561A (es)
KR (1) KR20110097825A (es)
CN (1) CN102317286A (es)
AR (1) AR074608A1 (es)
AU (1) AU2009326141A1 (es)
BR (1) BRPI0923326A2 (es)
CA (1) CA2745063A1 (es)
MX (1) MX2011005909A (es)
TW (1) TW201026695A (es)
UY (1) UY32315A (es)
WO (1) WO2010067123A1 (es)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI0607756A2 (pt) * 2005-02-18 2010-05-18 Astrazeneca Ab composto ou um sal farmaceuticamente aceitável do mesmo, composição farmacêutica, método para inibição de dna girase bacteriana e/ou topoisomerase iv em um animal de sangue quente, uso de um composto ou um sal farmaceuticamente aceitável do mesmo, e, processo para preparar compostos ou sais farmaceuticamente aceitáveis dos mesmos
TW201026694A (en) * 2008-12-12 2010-07-16 Astrazeneca Ab Compound 468
RU2012136451A (ru) 2010-01-28 2014-03-10 Президент Энд Феллоуз Оф Гарвард Колледж Композиции и способы улучшения активности протеасомы
DK2707101T3 (da) 2011-05-12 2019-05-13 Proteostasis Therapeutics Inc Proteostaseregulatorer
US9849135B2 (en) 2013-01-25 2017-12-26 President And Fellows Of Harvard College USP14 inhibitors for treating or preventing viral infections
WO2015073528A1 (en) 2013-11-12 2015-05-21 Proteostasis Therapeutics, Inc. Proteasome activity enhancing compounds
BR112016016289B1 (pt) 2014-01-14 2023-02-07 Takeda Pharmaceutical Company Limited Heteroaris e usos dos mesmos
WO2015108881A1 (en) 2014-01-14 2015-07-23 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
US9839363B2 (en) * 2015-05-13 2017-12-12 Alivecor, Inc. Discordance monitoring
CN105067814A (zh) * 2015-07-24 2015-11-18 中国科学院成都生物研究所 解旋酶水解atp活性测定方法
US10399968B2 (en) 2015-09-30 2019-09-03 Daiichi Sankyo Company, Limited Hydroxyalkyl thiadiazole derivatives
US11857352B2 (en) 2016-09-06 2024-01-02 The Research Foundation For The State University Of New York Positron imaging tomography imaging agent composition and method for bacterial infection
TW201840322A (zh) 2017-03-14 2018-11-16 日商第一三共股份有限公司 羥烷基噻二唑衍生物之ｎ－膦醯基氧基甲基前驅藥
RU2019133662A (ru) 2017-03-24 2021-04-26 Тайсо Фармасьютикал Ко., Лтд. Производное 2(1h)-хинолинона
WO2020048949A1 (en) 2018-09-03 2020-03-12 Univerza V Ljubljani New class of dna gyrase and/or topoisomerase iv inhibitors with activity against gram-positive and gram-negative bacteria
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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FR2735475B1 (fr) 1995-06-13 1997-07-11 Synthelabo Derives de n-((1,4-diazabicyclo(2.2.2)oct-2-yl)methyl) benzamide, leur preparation et leur application en therapeutique
TW538046B (en) 1998-01-08 2003-06-21 Hoechst Marion Roussel Inc Aromatic amides having antiobiotic activities and the preparation processes, intermediates and pharmaceutical composition thereof
JP2003520233A (ja) 2000-01-18 2003-07-02 バーテックス ファーマシューティカルズ インコーポレイテッド ジャイレースインヒビターおよびそれらの使用
SI1341769T1 (sl) 2000-12-15 2008-02-29 Vertex Pharma Inhibitorji bakterijske giraze in njihove uporabe
MXPA04006136A (es) 2001-12-21 2004-11-01 Anormed Inc Compuestos heterociclicos que se unen a receptor de quimiocina con eficacia incrementada.
TW200526626A (en) 2003-09-13 2005-08-16 Astrazeneca Ab Chemical compounds
BRPI0607756A2 (pt) * 2005-02-18 2010-05-18 Astrazeneca Ab composto ou um sal farmaceuticamente aceitável do mesmo, composição farmacêutica, método para inibição de dna girase bacteriana e/ou topoisomerase iv em um animal de sangue quente, uso de um composto ou um sal farmaceuticamente aceitável do mesmo, e, processo para preparar compostos ou sais farmaceuticamente aceitáveis dos mesmos
EP1856103A2 (en) 2005-02-18 2007-11-21 AstraZeneca AB Pyrrole derivatives as dna gyrase and topoisomerase inhibitors
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Also Published As

Publication number Publication date
BRPI0923326A2 (pt) 2017-07-11
JP2012511561A (ja) 2012-05-24
US20120028979A1 (en) 2012-02-02
US20100173909A1 (en) 2010-07-08
CN102317286A (zh) 2012-01-11
AU2009326141A1 (en) 2011-06-30
EP2376488A1 (en) 2011-10-19
UY32315A (es) 2010-07-30
MX2011005909A (es) 2011-06-20
TW201026695A (en) 2010-07-16
CA2745063A1 (en) 2010-06-17
WO2010067123A1 (en) 2010-06-17
KR20110097825A (ko) 2011-08-31
US8071605B2 (en) 2011-12-06

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