AR068658A1 - Derivados de tiazol - Google Patents

Derivados de tiazol

Info

Publication number
AR068658A1
AR068658A1 ARP080104329A ARP080104329A AR068658A1 AR 068658 A1 AR068658 A1 AR 068658A1 AR P080104329 A ARP080104329 A AR P080104329A AR P080104329 A ARP080104329 A AR P080104329A AR 068658 A1 AR068658 A1 AR 068658A1
Authority
AR
Argentina
Prior art keywords
nnr2
atoms
hal
nhet
nhet1
Prior art date
Application number
ARP080104329A
Other languages
English (en)
Inventor
Melanie Schultz
Ingo Kober
Wolfgang Staehle
Kai Schiemann
Andree Blaukat
Original Assignee
Merck Patent Gmbh
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 Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR068658A1 publication Critical patent/AR068658A1/es

Links

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
    • C07D417/02Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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
    • C07D417/14Heterocyclic 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

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Los compuestos de formula (1) en donde R1 es un heterociclo insaturado o aromático bicíclico con 1 a 4 átomos de N, O y/o S, que puede no estar sustituido o que puede estar mono-, di- o trisustituido con A, Ar, SR, NR2, Hal, NO2, CN, (CR2)n[X(CR2)n)]p-Y, CONR2, OR5 y/u =O (oxígeno del carbonilo); R2 y R3 son en cada caso, de modo independiente entre sí, H, A, Ar, OR, SR, NR2, Hal, NO2, CN o (CR2)n[X(CR2)n)]p-Y; R4 es H, Hal, A, OR, NR2 o (CR2)n[X(CR2)n)]p-Y; X es O, NR o CR2; Y es OR o NR2; R5 es H o alquilo no ramificado o ramificado con 1, 2, 3, 4, 5 o 6 átomos de C, en donde 1-7 átomos de H pueden estar reemplazados por F y/o Cl; K es C=O, CR2CO, o CR2; E es COO(CR2)n, CO(CR2)mO, CONH(CR2)n, S(O)q(CR2)n, CO(CR2)n, (CR2)n, CO(CR2)mO(CR2)p, CO(CR2)mNH(CR2)p o C(=S)O(CR2)n; R es H o alquilo no ramificado o ramificado con 1, 2, 3, 4, 5 o 6 átomos de C; W es Ar o Het; G es CH o N; Ar es fenilo, naftilo o bifenilo no sustituido o mono-, di-, tri-, tetra- o pentasustituido con Hal, A, (CR2)nOR, (CR2)nNR2, SR, NO2, CN, COOR, CONR2, NRCOA, NRSO2A, SO2NR2, S(O)qA, CO-Het, (CR2)nHet, O(CR2)nNR2, O(CR2)nHet, NHCOOA, NHCONR2, NHCOO(CR2)nNR2, NHCOO(CR2)nHet, NHCONH(CR2)nNR2, NHCONH(CR2)nHet, OCONH(CR2)nNR2, OCONH(CR2)nHet, CONR(CR2)nNR2, CONR(CR2)nHet y/o COA; Het es un heterociclo saturado, insaturado o aromático mono-, di- o tricíclico con 1 a 4 átomos de N, O y/o S, que puede no estar sustituido o que puede estar mono-, di- o trisustituido con Hal, A, (CR2)nOR, (CR2)nNR2, SR, NO2, CN, COOR, CONR2, NRCOA, NRSO2A, SO2NR2, S(O)qA, CO-Het1, (CR2)nHet1, O(CR2)nNR2, O(CR2)nHet1, NHCOOA, NHCONR2, NHCOO(CR2)nNR2, NHCOO(CR2)nHet1, NHCONH(CR2)NR2, NHCONH(CR2)nHet1, OCONH(CR2)nNR2, OCONH(CR2)nHet1, CO-Het1, CHO, COA, =S, =NH, =NA y/u =O (oxígeno del carbonilo); Het1 es un heterociclo saturado monocíclico con 1 a 2 N y/o átomos de O, que puede estar mono- o disustituido con A, OA, OH, Hal y/u =O (oxígeno del carbonilo); A es alquilo no ramificado o ramificado con 1-10 átomos de C, en donde 1-7 átomos de H pueden estar reemplazados por OR, CN, NR2, F y/o Cl y/o en donde uno o dos grupos CH2 no adyacentes pueden estar reemplazados por O, NH, S, SO, SO2 y/o por grupos CH=CH, o alquilo cíclico con 3-7 átomos de C; m es 1, 2, 3, 4, 5 o 6; n es 0, 1, 2, 3, 4, 5, 6, 7 u 8, p es 0, 1, 2, 3, 4, 5 o 6; q es 0, 1 o 2; Hal es F, Cl, Br o I; así como sus derivados, solvatos, tautomeros, sales y estereoisomeros de utilidad farmacéutica, incluyendo sus mezclas en todas las proporciones. Se pueden utilizar para el tratamiento de tumores. También se reivindica medicamento y proceso.
ARP080104329A 2007-10-05 2008-10-03 Derivados de tiazol AR068658A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102007047735A DE102007047735A1 (de) 2007-10-05 2007-10-05 Thiazolderivate

Publications (1)

Publication Number Publication Date
AR068658A1 true AR068658A1 (es) 2009-11-25

Family

ID=40418145

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP080104329A AR068658A1 (es) 2007-10-05 2008-10-03 Derivados de tiazol

Country Status (16)

Country Link
US (1) US8557824B2 (es)
EP (1) EP2209777B1 (es)
JP (2) JP2010540580A (es)
KR (1) KR20100080836A (es)
CN (1) CN101815714A (es)
AR (1) AR068658A1 (es)
AU (1) AU2008310068B2 (es)
BR (1) BRPI0817579A2 (es)
CA (1) CA2701525C (es)
DE (1) DE102007047735A1 (es)
EA (1) EA201000550A1 (es)
ES (1) ES2548525T3 (es)
IL (1) IL204563A (es)
MX (1) MX2010003365A (es)
WO (1) WO2009046842A2 (es)
ZA (1) ZA201003123B (es)

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JP5337711B2 (ja) * 2007-01-25 2013-11-06 イー・アイ・デュポン・ドウ・ヌムール・アンド・カンパニー 殺菌性アミド
DE102009049211A1 (de) * 2009-10-13 2011-04-28 Merck Patent Gmbh Sulfoxide
US9353113B2 (en) 2011-03-18 2016-05-31 Ono Pharmaceutical Co., Ltd. Tetrahydrocarboline derivative
MY182095A (en) 2013-11-22 2021-01-18 Sabre Therapeutics Llc Autotaxin inhibitor compounds
US9051320B1 (en) 2014-08-18 2015-06-09 Pharmakea, Inc. Methods for the treatment of metabolic disorders by a selective small molecule autotaxin inhibitor
GB201501870D0 (en) 2015-02-04 2015-03-18 Cancer Rec Tech Ltd Autotaxin inhibitors
GB201502020D0 (en) 2015-02-06 2015-03-25 Cancer Rec Tech Ltd Autotaxin inhibitory compounds
MX2017015225A (es) 2015-05-27 2018-02-19 Pharmakea Inc Inhibidores de la autotaxina y sus usos.
EP3302465A1 (en) 2015-06-05 2018-04-11 Vertex Pharmaceuticals Incorporated Triazoles for the treatment of demyelinating diseases
WO2018106643A1 (en) 2016-12-06 2018-06-14 Vertex Pharmaceuticals Incorporated Heterocyclic azoles for the treatment of demyelinating diseases
WO2018106641A1 (en) 2016-12-06 2018-06-14 Vertex Pharmaceuticals Incorporated Pyrazoles for the treatment of demyelinating diseases
WO2018106646A1 (en) 2016-12-06 2018-06-14 Vertex Pharmaceuticals Incorporated Aminotriazoles for the treatment of demyelinating diseases
TW202110831A (zh) * 2019-06-04 2021-03-16 大陸商江蘇恆瑞醫藥股份有限公司 吡啶酮類衍生物、其製備方法及其在醫藥上的應用
TW202116754A (zh) 2019-07-11 2021-05-01 美商E 斯蓋普生物股份有限公司 作為lrrk2抑制劑之吲唑及氮雜吲唑
CN113493453B (zh) * 2020-04-07 2023-06-16 江苏恒瑞医药股份有限公司 稠合芳香环类衍生物、其制备方法及其在医药上的应用

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CA2229617A1 (en) 1995-10-20 1997-05-01 Dr. Karl Thomae Gmbh 5-membered heterocycles, medicaments containing these compounds, their use and processes for their preparation
GB9904387D0 (en) 1999-02-25 1999-04-21 Pharmacia & Upjohn Spa Antitumour synergistic composition
AU4972900A (en) 1999-04-08 2000-11-14 Arch Development Corporation Use of anti-vegf antibody to enhance radiation in cancer therapy
GB0230162D0 (en) 2002-12-24 2003-02-05 Metris Therapeutics Ltd Compounds useful in inhibiting angiogenesis
FR2856685B1 (fr) * 2003-06-25 2005-09-23 Merck Sante Sas Derives de thiazolylpiperidine, leurs procedes de preparation et les compositions pharmaceutiques qui les contiennent
WO2005116653A2 (en) * 2004-04-13 2005-12-08 Arena Pharmaceuticals, Inc. Modulators of human g protein-coupled receptors for the treatment of hyperglycemia and related disorders
EP1637529A1 (en) 2004-09-20 2006-03-22 4Sc Ag Novel piperidin-4-yl-thiazole-carboxamide analogues as inhibitors of T-cell proliferation and uses thereof
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AU2006281435A1 (en) 2005-08-18 2007-02-22 F. Hoffmann-La Roche Ag Thiazolyl piperidine derivatives useful as H3 receptor modulators
CN101395107A (zh) 2006-02-28 2009-03-25 出光兴产株式会社 并四苯衍生物以及应用该衍生物的有机电致发光元件
EP1832586A1 (en) * 2006-03-10 2007-09-12 Oridis Biomed Forschungs- und Entwicklungs GmbH Thiazole-piperidine derivatives in treatment of diseases of liver and the pancreas
EP1834954A1 (en) * 2006-03-15 2007-09-19 4Sc Ag Thiazoles as NF-kB Inhibitors (proteasome inhibitors)
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Also Published As

Publication number Publication date
WO2009046842A2 (de) 2009-04-16
ZA201003123B (en) 2011-04-28
CN101815714A (zh) 2010-08-25
EA201000550A1 (ru) 2010-10-29
JP5843930B2 (ja) 2016-01-13
BRPI0817579A2 (pt) 2015-04-07
MX2010003365A (es) 2010-04-30
EP2209777B1 (de) 2015-07-29
IL204563A (en) 2017-03-30
AU2008310068A1 (en) 2009-04-16
ES2548525T3 (es) 2015-10-19
US8557824B2 (en) 2013-10-15
DE102007047735A1 (de) 2009-04-09
CA2701525C (en) 2016-06-28
JP2010540580A (ja) 2010-12-24
KR20100080836A (ko) 2010-07-12
WO2009046842A3 (de) 2009-06-25
CA2701525A1 (en) 2009-04-16
IL204563A0 (en) 2010-11-30
EP2209777A2 (de) 2010-07-28
AU2008310068B2 (en) 2014-05-01
JP2014240392A (ja) 2014-12-25
US20100240676A1 (en) 2010-09-23

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