AR076460A1 - Antagonistas del receptor cxcr3 - Google Patents

Antagonistas del receptor cxcr3

Info

Publication number
AR076460A1
AR076460A1 ARP100101401A ARP100101401A AR076460A1 AR 076460 A1 AR076460 A1 AR 076460A1 AR P100101401 A ARP100101401 A AR P100101401A AR P100101401 A ARP100101401 A AR P100101401A AR 076460 A1 AR076460 A1 AR 076460A1
Authority
AR
Argentina
Prior art keywords
alkyl
alkoxy
cycloalkyl
nr9r10
heteroaryl
Prior art date
Application number
ARP100101401A
Other languages
English (en)
Inventor
Frank Wu
Sabine Schlyer
John David Ginn
Daniel Richard Marshall
Anthony S Prokopowicz
Michael Robert Turner
Robert Sibley
Di Wu
Original Assignee
Boehringer Ingelheim Int
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 Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of AR076460A1 publication Critical patent/AR076460A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D417/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Biomedical Technology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Y sales farmacéuticamente aceptables de Ios mismos, en la que R1 a R6, A, B, X, Y y n son como se definen en la presente. Composiciones farmacéuticas que comprenden estos compuestos, a métodos para usar estos compuestos en el tratamiento de diversas enfermedades y trastornos. Reivindicacion 1: Un compuesto caracterizado porque tiene la formula (1): en la que: A es C o N; B es C o N; X es -NHC(O)-, -N(CH3)C(O)-, -NH- o está ausente; Y es -C(O)NH- o -NHC(O)-; R1 es H, -CN, halogeno, -CF3, -OCF3, alquilo C1-3, alcoxi C1-3, -S(O)mCH3, amino, mono- o dimetilamino, -NHC(O)alquilo C1-3, -NO2 -C(O)NH2, -C(O)NHalquilo C1-3 o -C(O)alquilo C1-3; R2 es arilo, heteroarilo o cicloalquilo C3-10, cada uno opcionalmente sustituido con de uno a tres R7; R3 es heteroarilo, heterociclilo, arilo o cicloalquilo C3-10, cada uno opcionalmente sustituido con de uno a tres R8; R4 es H o alquilo C1-6; cada uno de R5 y R6 se selecciona independientemente entre H, alquilo C1-2 y fenilo; o R5 y R6 pueden unirse para formar un puente etilo; R7 es -OH, oxo, hidroxialquilo C1-6, halogeno, -(CH2)m-CN, nitro, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-10, alcoxi C1-6, fenoxi, heteroariloxi, alcoxicarbonilo C1-6, carboxilo, -C(O)alquilo C1-6, -(CH2)m-NR9R10, -S(O)malquilo C1-6, -NHS(O)2alquhlo C1-6, NR9C(O)alquilo C1-6, -S(O)2NR9R10, -C(O)NR9R10 heterociclilo, heteroarilo, fenilo o bencilo, donde cada alquilo, alquenilo, alquinilo o alcoxi está opcionalmente parcial o totalmente halogenado y cada heterociclo, heteroarilo, fenilo o bencilo de dicho R7 está opcionalmente sustituido con de uno a tres alquilo C1-6, alcoxi C1-6(CH2)m, halogeno, -CN, -CF3, acilo C1-6, -NR9R10, -C(O)NR9R10, -OH, hidroxialquilo C1-6 o -S(O)malquilo C1-6; R8 es alquilo C1-6, alquenilo C2-6, alquinilo C2-6, carboxilo, cicloalquilo C3-10, alcoxi C1-6, halogeno, oxo o fenilo, donde cada alquilo, alquenilo, alquinilo, cicloalquilo o alcoxi está opcionalmente parcial o totalmente halogenado; R9 y R10 se seleccionan independientemente entre hidrogeno, alquilo C1-6, acilo C1-6, cicloalquilo C3-10, hidroxialquilo C1-6, alquil C1-6-alcoxi C1-6, alquilsulfonilo C1-6 y alcoxicarbonilo C1-6; m es 0-2; n es 1 o 2; -------- es un enlace sencillo si A es N o un enlace sencillo o doble enlace si A es C; o una sal farmacéuticamente aceptable del mismo.
ARP100101401A 2009-04-27 2010-04-26 Antagonistas del receptor cxcr3 AR076460A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US17286909P 2009-04-27 2009-04-27
US31735110P 2010-03-25 2010-03-25

Publications (1)

Publication Number Publication Date
AR076460A1 true AR076460A1 (es) 2011-06-15

Family

ID=42272001

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100101401A AR076460A1 (es) 2009-04-27 2010-04-26 Antagonistas del receptor cxcr3

Country Status (7)

Country Link
US (1) US8362249B2 (es)
EP (1) EP2424858B1 (es)
JP (1) JP5741574B2 (es)
AR (1) AR076460A1 (es)
TW (1) TW201103933A (es)
UY (1) UY32574A (es)
WO (1) WO2010126851A1 (es)

Families Citing this family (20)

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CA2735593C (en) 2008-09-03 2017-08-15 Repligen Corporation Compositions including 6-aminohexanoic acid derivatives as hdac inhibitors
EP2424840B1 (en) * 2009-04-27 2014-08-06 Boehringer Ingelheim International GmbH Cxcr3 receptor antagonists
JP2011057661A (ja) * 2009-08-14 2011-03-24 Bayer Cropscience Ag 殺虫性カルボキサミド類
WO2011084985A1 (en) * 2010-01-07 2011-07-14 Boehringer Ingelheim International Gmbh Cxcr3 receptor antagonists
EP3524324A1 (en) 2011-02-28 2019-08-14 BioMarin Pharmaceutical Inc. Histone deacetylase inhibitors
US10059723B2 (en) 2011-02-28 2018-08-28 Biomarin Pharmaceutical Inc. Histone deacetylase inhibitors
US8957066B2 (en) 2011-02-28 2015-02-17 Biomarin Pharmaceutical Inc. Histone deacetylase inhibitors
EP2508511A1 (en) * 2011-04-07 2012-10-10 Laboratoire Biodim Inhibitors of viral replication, their process of preparation and their therapeutical uses
CA2861020C (en) 2012-02-02 2018-07-17 Actelion Pharmaceuticals Ltd 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives and their use as cxcr3 receptor modulators
KR20150132345A (ko) 2013-03-15 2015-11-25 바이오마린 파머수티컬 인크. Hdac 저해제
WO2014182688A1 (en) * 2013-05-07 2014-11-13 Arena Pharmaceuticals, Inc. Modulators of the g protein-coupled mas receptor and the treatment of disorders related thereto
WO2014182673A1 (en) * 2013-05-07 2014-11-13 Arena Pharmaceuticals, Inc. Modulators of the g protein-coupled mas receptor and the treatment of disorders related thereto
US9663529B2 (en) 2013-07-02 2017-05-30 Bristol-Myers Squibb Company Tricyclic pyrido-carboxamide derivatives as rock inhibitors
JP6434968B2 (ja) 2013-07-02 2018-12-05 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company Rock阻害剤としての三環式ピリド−カルボキサミド誘導体
ES2671323T3 (es) 2013-07-22 2018-06-06 Idorsia Pharmaceuticals Ltd Derivados 1¿(piperazin¿1¿il)¿2¿([1,2,4]triazol¿1¿il)¿etanona
AR099789A1 (es) * 2014-03-24 2016-08-17 Actelion Pharmaceuticals Ltd Derivados de 8-(piperazin-1-il)-1,2,3,4-tetrahidro-isoquinolina
MY187540A (en) * 2014-08-01 2021-09-28 Nuevolution As Compounds active towards bromodomains
TWI689497B (zh) * 2014-09-04 2020-04-01 南北兄弟藥業投資有限公司 芳雜環類衍生物及其在藥物中的應用
PL3245203T3 (pl) 2015-01-15 2019-05-31 Idorsia Pharmaceuticals Ltd Pochodne hydroksyalkilopiperazyny jako modulatory receptora cxcr3
AR103399A1 (es) * 2015-01-15 2017-05-10 Actelion Pharmaceuticals Ltd Derivados de (r)-2-metil-piperazina como moduladores del receptor cxcr3

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JP4723242B2 (ja) * 2002-06-12 2011-07-13 ケモセントリックス インコーポレーティッド 炎症および免疫障害治療用ccr1アンタゴニストとして使用するための1−アリール−4−置換ピペラジン誘導体
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US20040192728A1 (en) * 2003-02-03 2004-09-30 Ellen Codd Quinoline-derived amide modulators of vanilloid VR1 receptor
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US20090030012A1 (en) * 2006-02-23 2009-01-29 Adams Alan D Pyridine, Pyrimidine and Pyrazine Derivatives as Cxcr3 Receptor Modulators
JP5286646B2 (ja) * 2006-04-19 2013-09-11 トヨタ自動車株式会社 スルホン基含有モノマーの重合方法
EP2009005A4 (en) * 2006-04-19 2010-06-02 Astellas Pharma Inc AZOLECARBOXAMIDE DERIVATIVE
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EP2424840B1 (en) * 2009-04-27 2014-08-06 Boehringer Ingelheim International GmbH Cxcr3 receptor antagonists

Also Published As

Publication number Publication date
JP2012525335A (ja) 2012-10-22
US20100273781A1 (en) 2010-10-28
UY32574A (es) 2010-11-30
WO2010126851A1 (en) 2010-11-04
EP2424858B1 (en) 2014-05-14
TW201103933A (en) 2011-02-01
EP2424858A1 (en) 2012-03-07
JP5741574B2 (ja) 2015-07-01
US8362249B2 (en) 2013-01-29

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