CA2550350C - 2-(hetero)aryl-substituted tetrahydroquinoline derivatives - Google Patents

2-(hetero)aryl-substituted tetrahydroquinoline derivatives Download PDF

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Publication number
CA2550350C
CA2550350C CA2550350A CA2550350A CA2550350C CA 2550350 C CA2550350 C CA 2550350C CA 2550350 A CA2550350 A CA 2550350A CA 2550350 A CA2550350 A CA 2550350A CA 2550350 C CA2550350 C CA 2550350C
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CA
Canada
Prior art keywords
compound
mixture
salt
formula
tumour
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
CA2550350A
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English (en)
French (fr)
Other versions
CA2550350A1 (en
Inventor
Kai Schiemann
Ulrich Emde
Dirk Finsinger
Johannes Gleitz
Helmut Reubold
Frank Zenke
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Merck Patent GmbH
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
Priority claimed from DE10360154A external-priority patent/DE10360154A1/de
Priority claimed from DE102004026026A external-priority patent/DE102004026026A1/de
Application filed by Merck Patent GmbH filed Critical Merck Patent GmbH
Publication of CA2550350A1 publication Critical patent/CA2550350A1/en
Application granted granted Critical
Publication of CA2550350C publication Critical patent/CA2550350C/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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Classifications

    • 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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/47064-Aminoquinolines; 8-Aminoquinolines, e.g. chloroquine, primaquine
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4738Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/052Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/14Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Saccharide Compounds (AREA)
CA2550350A 2003-12-20 2004-12-14 2-(hetero)aryl-substituted tetrahydroquinoline derivatives Expired - Fee Related CA2550350C (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
DE10360154A DE10360154A1 (de) 2003-12-20 2003-12-20 Tetrahydrochinoline
DE10360154.6 2003-12-20
US53996104P 2004-01-30 2004-01-30
US60/539,961 2004-01-30
DE102004026026A DE102004026026A1 (de) 2004-05-27 2004-05-27 Tetrahydrochinoline
DE102004026026.5 2004-05-27
PCT/EP2004/014205 WO2005063735A1 (de) 2003-12-20 2004-12-14 2- (hetero) -arylsubstituierte tetrahydrochinolinderivate

Publications (2)

Publication Number Publication Date
CA2550350A1 CA2550350A1 (en) 2005-07-14
CA2550350C true CA2550350C (en) 2013-03-12

Family

ID=43969203

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2550350A Expired - Fee Related CA2550350C (en) 2003-12-20 2004-12-14 2-(hetero)aryl-substituted tetrahydroquinoline derivatives

Country Status (14)

Country Link
US (1) US7868172B2 (enExample)
EP (2) EP1761515B1 (enExample)
JP (1) JP5237555B2 (enExample)
AT (2) ATE413393T1 (enExample)
AU (1) AU2004309028B9 (enExample)
BR (1) BRPI0417838A (enExample)
CA (1) CA2550350C (enExample)
DE (1) DE502004012458D1 (enExample)
DK (2) DK2033959T3 (enExample)
ES (1) ES2315727T3 (enExample)
PL (2) PL2033959T3 (enExample)
PT (2) PT1761515E (enExample)
SI (2) SI1761515T1 (enExample)
WO (1) WO2005063735A1 (enExample)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0219660D0 (en) 2002-08-23 2002-10-02 Astrazeneca Ab Therapeutic use
GB0403744D0 (en) 2004-02-20 2004-03-24 Astrazeneca Ab Chemical process
GB0425854D0 (en) * 2004-11-25 2004-12-29 Astrazeneca Ab Therapeutic treatment
DE102005027170A1 (de) * 2005-06-13 2006-12-14 Merck Patent Gmbh Substituierte Tetrahydrochinoline
WO2007019180A2 (en) * 2005-08-04 2007-02-15 Science & Technology Corporation @ Unm Compounds for binding to eralpha/beta and gpr30, methods of treating disease states and conditions mediated through these receptors and identification thereof
MX2008016071A (es) * 2006-06-19 2009-01-15 Merck Patent Gmbh Formas polimorficas y proceso.
DE102007013855A1 (de) * 2007-03-20 2008-09-25 Merck Patent Gmbh Substituierte Tetrahydrochinoline
DE102007013856A1 (de) 2007-03-20 2008-09-25 Merck Patent Gmbh Substituierte Tetrahydropyrrolochinoline
DE102007013854A1 (de) * 2007-03-20 2008-09-25 Merck Patent Gmbh Tetrahydrochinoline
DE102007021862A1 (de) * 2007-05-10 2008-11-13 Merck Patent Gmbh Wässrige pharmazeutische Zubereitung
EP2173321B1 (en) * 2007-07-19 2024-12-18 DSM IP Assets B.V. Tablettable formulations of lipophilic health ingredients
US8278454B2 (en) * 2007-12-18 2012-10-02 MERCK Patent Gesellschaft mit beschränkter Haftung Process for preparing tetrahydroquinoline derivatives
EP2291355A4 (en) * 2008-01-04 2011-08-03 Panjab University NOVEL TETRAHYDROCHINOLINE AS AN AROMATASE INHIBITOR
WO2011009523A1 (en) 2009-07-24 2011-01-27 Merck Patent Gmbh Eg5 as biomarker in rare thoracic cancer
EP2620438A1 (en) * 2012-01-24 2013-07-31 Laboratorios Del. Dr. Esteve, S.A. Substituted pyrano and furanoquinolines, their preparation and use as medicaments
EP2647638A1 (en) * 2012-04-02 2013-10-09 Almirall, S.A. Substituted tricyclic compounds with activity towards ep1 receptors
US9498540B2 (en) 2013-03-15 2016-11-22 Novartis Ag Cell proliferation inhibitors and conjugates thereof
WO2015074081A1 (en) 2013-11-18 2015-05-21 Bair Kenneth W Benzopiperazine compositions as bet bromodomain inhibitors
LT3071203T (lt) 2013-11-18 2021-05-25 Forma Therapeutics, Inc. Tetrahidrochinolino kompozicijos kaip bet bromodomeno inhibitoriai
WO2017214468A1 (en) 2016-06-09 2017-12-14 Tien Yang Der Nanodroplet compositions for the efficient delivery of anti-cancer agents
CN110684031B (zh) * 2019-08-14 2021-07-02 西北大学 一种反式-四氢呋喃/吡喃并四氢喹啉衍生手性化合物的不对称合成方法
WO2022006365A2 (en) * 2020-07-02 2022-01-06 Purdue Research Foundation Tetrahydro-3h-pyrazolo quinolone and tetrahydro-3h-pyrrolo[3,2-f]quinoline-containing compounds and uses thereof
EP4269392A4 (en) 2020-12-25 2025-01-29 Toray Industries, Inc. TETRAHYDROQUINOLINE DERIVATIVE AND MEDICAL USE THEREOF
WO2023249106A1 (ja) 2022-06-24 2023-12-28 東レ株式会社 筋萎縮性側索硬化症の治療剤又は予防剤

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH08506175A (ja) * 1992-10-01 1996-07-02 ザ・トラスティーズ・オブ・コランビア・ユニバーシティー・イン・ザ・シティー・オブ・ニューヨーク タグでコードされる複合体の組合せ化学ライブラリー
CN1154640C (zh) * 1993-10-01 2004-06-23 纽约市哥伦比亚大学理事 用标示物编码的多元组合化学库
WO2000061186A1 (en) 1999-04-08 2000-10-19 Arch Development Corporation Use of anti-vegf antibody to enhance radiation in cancer therapy
AU7558900A (en) * 1999-10-14 2001-04-23 Kaken Pharmaceutical Co., Ltd. Tetrahydroquinoline derivatives
CA2442455A1 (en) * 2001-03-29 2002-10-10 Deborah L. Roussell A method of treating proliferative diseases using eg5 inhibitors
US7250423B2 (en) 2001-09-24 2007-07-31 Chao-Jun Li Methods for synthesizing heterocycles and therapeutic use of the heterocycles for cancers
DE10236910A1 (de) * 2002-08-12 2004-03-11 Grünenthal GmbH Substituierte 1,2,3,4-Tetrahydrochinolinderivate

Also Published As

Publication number Publication date
SI2033959T1 (sl) 2011-08-31
PL2033959T3 (pl) 2011-09-30
DK2033959T3 (da) 2011-07-25
AU2004309028A1 (en) 2005-07-14
JP2007515419A (ja) 2007-06-14
ES2315727T3 (es) 2009-04-01
EP2033959B1 (de) 2011-04-27
PT2033959E (pt) 2011-07-29
CA2550350A1 (en) 2005-07-14
PL1761515T3 (pl) 2009-04-30
PT1761515E (pt) 2009-02-11
US20070203167A1 (en) 2007-08-30
ATE413393T1 (de) 2008-11-15
AU2004309028B2 (en) 2011-04-21
ATE507220T1 (de) 2011-05-15
DE502004012458D1 (de) 2011-06-09
WO2005063735A1 (de) 2005-07-14
AU2004309028B9 (en) 2011-06-16
EP1761515B1 (de) 2008-11-05
SI1761515T1 (sl) 2009-02-28
BRPI0417838A (pt) 2007-04-17
US7868172B2 (en) 2011-01-11
EP1761515A1 (de) 2007-03-14
DK1761515T3 (da) 2009-02-16
EP2033959A1 (de) 2009-03-11
JP5237555B2 (ja) 2013-07-17

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