DE102007040336A1 - Neue Inhibitoren der 5-Lipoxygenase und deren Verwendungen - Google Patents

Neue Inhibitoren der 5-Lipoxygenase und deren Verwendungen Download PDF

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Publication number
DE102007040336A1
DE102007040336A1 DE102007040336A DE102007040336A DE102007040336A1 DE 102007040336 A1 DE102007040336 A1 DE 102007040336A1 DE 102007040336 A DE102007040336 A DE 102007040336A DE 102007040336 A DE102007040336 A DE 102007040336A DE 102007040336 A1 DE102007040336 A1 DE 102007040336A1
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Prior art keywords
methyl
compound
formula
diseases
hydrogen
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DE102007040336A
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German (de)
English (en)
Inventor
Gisbert Schneider
Dieter Steinhilber
Lutz Franke
Bettina Hofmann
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Goethe Universitaet Frankfurt am Main
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Goethe Universitaet Frankfurt am Main
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Priority to DE102007040336A priority Critical patent/DE102007040336A1/de
Priority to PCT/EP2008/007014 priority patent/WO2009027077A2/fr
Publication of DE102007040336A1 publication Critical patent/DE102007040336A1/de
Withdrawn legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/34—Oxygen atoms
    • 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/38—Nitrogen atoms
    • C07D277/42—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Immunology (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
DE102007040336A 2007-08-27 2007-08-27 Neue Inhibitoren der 5-Lipoxygenase und deren Verwendungen Withdrawn DE102007040336A1 (de)

Priority Applications (2)

Application Number Priority Date Filing Date Title
DE102007040336A DE102007040336A1 (de) 2007-08-27 2007-08-27 Neue Inhibitoren der 5-Lipoxygenase und deren Verwendungen
PCT/EP2008/007014 WO2009027077A2 (fr) 2007-08-27 2008-08-27 Nouveaux inhibiteurs de la 5-lipoxygénase et utilisations de ceux-ci

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102007040336A DE102007040336A1 (de) 2007-08-27 2007-08-27 Neue Inhibitoren der 5-Lipoxygenase und deren Verwendungen

Publications (1)

Publication Number Publication Date
DE102007040336A1 true DE102007040336A1 (de) 2009-03-05

Family

ID=40298809

Family Applications (1)

Application Number Title Priority Date Filing Date
DE102007040336A Withdrawn DE102007040336A1 (de) 2007-08-27 2007-08-27 Neue Inhibitoren der 5-Lipoxygenase und deren Verwendungen

Country Status (2)

Country Link
DE (1) DE102007040336A1 (fr)
WO (1) WO2009027077A2 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103140488A (zh) * 2010-08-03 2013-06-05 加利福尼亚大学董事会 缓和组织损伤和坏死的化合物和组合物

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20120214840A1 (en) * 2009-09-23 2012-08-23 Panmira Pharmaceuticals, Llc Indolizine inhibitors of 5-lipoxygenase
JP2013515677A (ja) * 2009-09-23 2013-05-09 アミラ ファーマシューティカルズ，インク． ５−リポキシゲナーゼのインドリジンインヒビター
US9029389B2 (en) * 2011-04-21 2015-05-12 Institut Pasteur Korea Anti-inflammation compounds
EP2881394B1 (fr) 2012-07-31 2018-03-21 Kyowa Hakko Kirin Co., Ltd. Composé hétérocyclique à cycles condensés
CN108689960B (zh) * 2018-06-07 2022-03-04 济南大学 5-苯亚甲基-2-苯基噻唑酮类化合物及其制备和应用

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DE10050663A1 (de) * 2000-10-13 2002-04-18 Gruenenthal Gmbh Verwendung von substituierten Imidazo[1,2-a]pyridin-, -pyrimidin- und pyrazin-3-yl-amin-Derivaten zur Herstellung von Medikamenten zur NOS-Inhibierung
US20030022914A1 (en) * 1999-10-08 2003-01-30 Gruenenthal Gmbh . Tert.-butyl-(7-menthyl-imidazol [1,2-A] pyridin-3-yl)-amine derivatives
US20040137472A1 (en) * 2002-09-27 2004-07-15 Ryszard Kole Methods and compositions for modification of splicing of pre-mRNA
WO2005007141A2 (fr) * 2003-07-11 2005-01-27 Proteologics, Inc. Inhibiteurs de l'ubiquitine ligase et methodes associees
JP2005063833A (ja) 2003-08-13 2005-03-10 Mitsubishi Paper Mills Ltd 光電変換材料、半導体電極並びにそれを用いた光電変換素子
WO2005082363A1 (fr) * 2004-02-20 2005-09-09 Board Of Regents, The University Of Texas System Composes de thiazolone permettant de traiter le cancer
WO2006101455A1 (fr) 2005-03-21 2006-09-28 S*Bio Pte Ltd Derives imidazo[1,2-a]pyridine : preparation et applications pharmaceutiques
WO2006114263A1 (fr) 2005-04-25 2006-11-02 Novartis Ag Derives de imidazo [1, 2-a] pyridine utilises en tant qu'inhibiteurs de peptide deformylase (pdf)
WO2007012464A1 (fr) 2005-07-26 2007-02-01 Merckle Gmbh Conjugues macrolides de composes de pyrrolizine et d'indolizine comme inhibiteurs de la 5-lipooxygenase et de la cyclooxygenase
WO2007067711A2 (fr) * 2005-12-08 2007-06-14 Amphora Discovery Corporation Certains types d'entites chimiques, compositions et methode de modulation de trpv1
WO2007103754A2 (fr) * 2006-03-02 2007-09-13 Smithkline Beecham Corporation Thiazolones utilisés en tant qu'inhibiteurs de p13-kinases

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DE3874257T2 (de) * 1987-03-11 1993-02-11 Kanegafuchi Chemical Ind Hydroxystyren-derivate.
WO2002090911A1 (fr) * 2001-05-07 2002-11-14 Flir Systems Ab Camera infrarouge a main
WO2005016227A2 (fr) * 2003-08-14 2005-02-24 Insight Biopharmaceuticals Ltd. Methodes et compositions pharmaceutiques servant a moduler l'activation d'heparanase et leurs utilisations
DE102004021716A1 (de) * 2004-04-30 2005-12-01 Grünenthal GmbH Substituierte Imidazo[1,2-a]pyridin-Verbindungen und Arzneimittel enthaltend substituierte Imidazo[1,2-a]pyridin-Verbindungen
DE102005024012A1 (de) * 2005-05-20 2006-11-23 Grünenthal GmbH Verwendung von 2,5-disubstituierten Thiazol-4-on-Derivaten in Arzneimitteln
US7592461B2 (en) * 2005-12-21 2009-09-22 Bristol-Myers Squibb Company Indane modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof

Patent Citations (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030022914A1 (en) * 1999-10-08 2003-01-30 Gruenenthal Gmbh . Tert.-butyl-(7-menthyl-imidazol [1,2-A] pyridin-3-yl)-amine derivatives
DE10050663A1 (de) * 2000-10-13 2002-04-18 Gruenenthal Gmbh Verwendung von substituierten Imidazo[1,2-a]pyridin-, -pyrimidin- und pyrazin-3-yl-amin-Derivaten zur Herstellung von Medikamenten zur NOS-Inhibierung
US20040137472A1 (en) * 2002-09-27 2004-07-15 Ryszard Kole Methods and compositions for modification of splicing of pre-mRNA
WO2005007141A2 (fr) * 2003-07-11 2005-01-27 Proteologics, Inc. Inhibiteurs de l'ubiquitine ligase et methodes associees
JP2005063833A (ja) 2003-08-13 2005-03-10 Mitsubishi Paper Mills Ltd 光電変換材料、半導体電極並びにそれを用いた光電変換素子
WO2005082363A1 (fr) * 2004-02-20 2005-09-09 Board Of Regents, The University Of Texas System Composes de thiazolone permettant de traiter le cancer
WO2006101455A1 (fr) 2005-03-21 2006-09-28 S*Bio Pte Ltd Derives imidazo[1,2-a]pyridine : preparation et applications pharmaceutiques
WO2006114263A1 (fr) 2005-04-25 2006-11-02 Novartis Ag Derives de imidazo [1, 2-a] pyridine utilises en tant qu'inhibiteurs de peptide deformylase (pdf)
WO2007012464A1 (fr) 2005-07-26 2007-02-01 Merckle Gmbh Conjugues macrolides de composes de pyrrolizine et d'indolizine comme inhibiteurs de la 5-lipooxygenase et de la cyclooxygenase
WO2007067711A2 (fr) * 2005-12-08 2007-06-14 Amphora Discovery Corporation Certains types d'entites chimiques, compositions et methode de modulation de trpv1
WO2007103754A2 (fr) * 2006-03-02 2007-09-13 Smithkline Beecham Corporation Thiazolones utilisés en tant qu'inhibiteurs de p13-kinases

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Bird, T. G. C., Bruneau, P., Crawley, P. C., Edwards, M. P., Foster, S. J., Girodeau, J-M., Kingston, J. F. and McMillan, R. M. (1991) (Methoxyalkyl)thiazoles: a new series of potent, selective, and orally active 5-lipoxygenase inhibitors displaying high enantioselectivity. J. Med. Chem. 34(7), 2176-2186
Fechner, U., Franke, L., Renner, S., Schneider, P., Schneider, G. (2003) Comparison of correlation vector methods for ligand-based similarity searching. J. Comput. Aided Mol. Des. 17, 687-698
McMillan et al., 1991
McMillan, R. M., Bird, T. G., Crawley, G. C., Edwards, M. P., Girodeau, J. M., Kingston, J. F., Foster, S. J. (1991) Methoxyalkyl thiazoles: a novel series of potent, orally active and enantioselective inhibitors of 5-lipoxygenase. Agents Action. 34(1-2), 110-112
Mehrabian, M., Allayee, H. (2003) 5-lipoxygenase and atherosclerosis. Curr Opin Lipidol 14, 447-457
Miller, D. K., Gillard, J. W., Vickers, P. J., Sadowski, S., Léveillé, C., Mancini, J. A., Charleson, P., Dixon, R. A. F., Ford-Hutchinson, A. W., Fortin, R., Gauthier, J. Y., Rodkey, J., Rosen, R., Rouzer, C., Sigal, I. S., Strader, C. D., Evans, J. F. (1990) Identification and isolation of a membrane protein necessary for leukotriene production. Nature 343, 278-281
Rådmark, O., Samuelsson, B. (2005) Regulation of 5-lipoxygenase enzyme activity. Biochem. Biophys. Res. Commun. 338, 102-110
Schneider, G., Neidhart, W., Giller, T., Schmid, G. (1999) "Scaffold-Hopping" by topological pharmacophore search: A contribution to virtual screening. Angew. Chemie 111, 3068-3070, Angew. Chemie Int. Ed. 38, 2894-2896
Schneider, P., Schneider, G. (2003) Collection of bioactive reference compounds for focused library design. QSAR Comb. Sci. 22, 713-718
Werz, O., Bürkert, E., Fischer, L., Szellas, D., Dishart, D., Samuelsson, B., Rådmark, O., Steinhilber, D. (2002) Extracellular signal-regulated kinases phosphorylate 5-lipoxygenase and stimulate 5-lipoxygenase product formation in leukocytes. FASEB J. 16, 1441-1443
Werz, O., Bürkert, E., Rådmark, O., Steinhilber, D. (2002) Activation of 5-lipoxygenase by cell stress is calcium independent in human polymorphonuclear leukocytes. Blood 99, 1044-1052
Werz, O., Klemm, J., Samuelsson, B., Rådmark, 0. (2000) 5-lipoxygenase is phosphorylated by p38 kinase-dependent MAPKAP kinases. Proc. Natl. Acad. Sci. USA 97, 5261-5266
Werz, O., Steinhilber, D. (2005) Development of 5-lipoxygenase inhibitors - lessons from cellular enzyme regulation. Biochem. Pharmacol. 70, 327-333
Werz, O., Steinhilber, D. (2006) Therapeutic options for 5-lipoxygenase inhibitors. Pharmacol. Ther. 112, 701-718
Werz, O., Szellas, D., Steinhilber, D., Rådmark, O. (2002) Arachidonic acid promotes phosphorylation of 5-lipoxygenase at Ser-271 by MAPK-activated protein kinase 2 (MK2). J. Biol. Chem. 277, 14793-14800

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103140488A (zh) * 2010-08-03 2013-06-05 加利福尼亚大学董事会 缓和组织损伤和坏死的化合物和组合物
EP2601191A2 (fr) * 2010-08-03 2013-06-12 The Regents of the University of California Composés et compositions pour l'atténuation de dommage et de létalité tissulaire
EP2601191A4 (fr) * 2010-08-03 2013-07-31 Univ California Composés et compositions pour l'atténuation de dommage et de létalité tissulaire
US9045474B2 (en) 2010-08-03 2015-06-02 The Regents Of The University Of California Compounds and compositions for mitigating tissue damage and lethality

Also Published As

Publication number Publication date
WO2009027077A2 (fr) 2009-03-05
WO2009027077A8 (fr) 2009-04-30
WO2009027077A3 (fr) 2009-09-24

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Effective date: 20120301