BRPI0410663A - compostos de hidroxiamidina e hidroxiguanidina como inibidores de uroquinase - Google Patents

compostos de hidroxiamidina e hidroxiguanidina como inibidores de uroquinase

Info

Publication number
BRPI0410663A
BRPI0410663A BRPI0410663-6A BRPI0410663A BRPI0410663A BR PI0410663 A BRPI0410663 A BR PI0410663A BR PI0410663 A BRPI0410663 A BR PI0410663A BR PI0410663 A BRPI0410663 A BR PI0410663A
Authority
BR
Brazil
Prior art keywords
compounds
hydroxyamidine
urokinase
hydroxyguuanidine
urokinase inhibitors
Prior art date
Application number
BRPI0410663-6A
Other languages
English (en)
Inventor
Stefan Sperl
Markus Buergle
Wolfgang Schmalix
Katja Wosikowski
Bernd Clement
Original Assignee
Wilex Ag
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 Wilex Ag filed Critical Wilex Ag
Publication of BRPI0410663A publication Critical patent/BRPI0410663A/pt
Publication of BRPI0410663B1 publication Critical patent/BRPI0410663B1/pt
Publication of BRPI0410663B8 publication Critical patent/BRPI0410663B8/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/185—Radicals derived from carboxylic acids from aliphatic carboxylic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)

Abstract

"COMPOSTOS DE HIDROXIAMIDINA E HIDROXIGUANIDINA COMO INIBIDORES DE UROQUINASE". A presente invenção refere-se a novos compostos para inibição do ativador de plasminogênio uroquinase (uPA), que apresentam alta biodisponibilidade e administrabilidade oral, e também ao uso dos mesmos como compostos terapêuticos ativos para o tratamento de distúrbios associados à uroquinase ou/e receptores de uroquinase tais como, por exemplo, tumores e metastatização. A invenção refere-se em particular a compostos que contêm grupos hidroxiamidina ou hidroxiguanidina.
BRPI0410663A 2003-05-26 2004-05-26 compostos de hidroxiamidina e hidroxiguanidina e seus usos BRPI0410663B8 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE10323898A DE10323898A1 (de) 2003-05-26 2003-05-26 Hydroxyamidin- und Hydroxyguanidin-Verbindungen als Urokinase-Hemmstoffe
DE10323898.0 2003-05-26
PCT/EP2004/005682 WO2004103984A1 (de) 2003-05-26 2004-05-26 Hydroxyamidin- und hydroxyguanidin-verbindungen als urokinase-hemmstoffe

Publications (3)

Publication Number Publication Date
BRPI0410663A true BRPI0410663A (pt) 2006-06-20
BRPI0410663B1 BRPI0410663B1 (pt) 2019-05-21
BRPI0410663B8 BRPI0410663B8 (pt) 2021-05-25

Family

ID=33461890

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0410663A BRPI0410663B8 (pt) 2003-05-26 2004-05-26 compostos de hidroxiamidina e hidroxiguanidina e seus usos

Country Status (15)

Country Link
US (3) US7608623B2 (pt)
EP (2) EP2243774A1 (pt)
JP (1) JP4621676B2 (pt)
CN (2) CN1795183B (pt)
AU (2) AU2004240771B2 (pt)
BR (1) BRPI0410663B8 (pt)
CA (1) CA2526989C (pt)
DE (1) DE10323898A1 (pt)
DK (1) DK1628965T3 (pt)
ES (1) ES2550611T3 (pt)
HU (1) HUE025940T2 (pt)
MX (1) MXPA05012675A (pt)
PL (1) PL1628965T3 (pt)
PT (1) PT1628965E (pt)
WO (1) WO2004103984A1 (pt)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1485345B1 (de) * 2002-03-11 2008-06-25 Curacyte AG Hemmstoffe der urokinase, ihre herstellung und verwendung
DE10301300B4 (de) * 2003-01-15 2009-07-16 Curacyte Chemistry Gmbh Verwendung von acylierten 4-Amidino- und 4-Guanidinobenzylaminen zur Inhibierung von Plasmakallikrein
DE10342108A1 (de) * 2003-09-11 2005-04-14 Curacyte Chemistry Gmbh Basisch-substituierte Benzylaminanaloga als Inhibitoren des Gerinnungsfaktors Xa, ihre Herstellung und Verwendung
DE102004045720A1 (de) * 2004-09-21 2006-03-23 Wilex Ag Stabile Dosierungsform von Phenylalanin-Derivaten
DE102004057195A1 (de) * 2004-11-26 2006-06-01 Wilex Ag Kristalline Modifikationen von N-Alpha-(2,4,6-Triisopropylphenylsulfonyl)-3-hydroxyamidino-(L)-phenylalanin-4-ethoxycarbonylpiperazid und/oder Salzen davon
US8093258B2 (en) 2005-06-24 2012-01-10 Wilex Ag Use of urokinase inhibitors for the treatment and/or prevention of neuropathological diseases
DE102006050672A1 (de) * 2006-10-24 2008-04-30 Curacyte Discovery Gmbh Hemmstoffe des Plasmins und des Plasmakallikreins
US20080226624A1 (en) * 2007-03-07 2008-09-18 Wolfgang Schmalix Combined treatment of cancer by urokinase inhibition and a cytostatic anti-cancer agent for enhancing the anti-metastatic effect
WO2008143342A1 (ja) * 2007-05-23 2008-11-27 Dainippon Sumitomo Pharma Co., Ltd. ３－アミノ－２，５－ジオキソピロリジン誘導体の製造方法
DE102008007440A1 (de) 2008-02-01 2009-08-13 Dritte Patentportfolio Beteiligungsgesellschaft Mbh & Co.Kg Aminosäurederivate als Arzneistoffe
US9662308B2 (en) 2008-02-01 2017-05-30 Dritte Patentportfolio Beteiligungsgesellschaft Mbh & Co. Kg Orally bioavailable pentamidine prodrugs for the treatment of diseases
DE102008007381A1 (de) 2008-02-01 2009-08-13 Dritte Patentportfolio Beteiligungsgesellschaft Mbh & Co.Kg Amidine und Guanidine und deren Derivate zur Behandlung von Krankheiten
CN102319241B (zh) * 2011-07-06 2016-02-10 中山大学 一种针对ccl18靶标的化合物在制备抗乳腺癌药物中的应用
DE102011108346A1 (de) * 2011-07-25 2013-01-31 Philipps-Universität Marburg Verwendung von Hemmstoffen der TMPRSS2 als Arzneimittel
JP6963545B2 (ja) 2015-10-06 2021-11-10 レッド ヒル バイオファーマ リミテッドRedHill Biopharma Ltd. 癌を治療するための併用療法
CA3070037A1 (en) * 2017-07-21 2019-01-24 Redhill Biopharma Ltd. Use of wx-uk1 and its prodrug, wx-671, for the treatment of non-cancerous medical conditions
AU2021235304A1 (en) 2020-03-10 2022-10-06 Redhill Biopharma Ltd. Treatment of coronavirus infection
US11471448B2 (en) 2020-12-15 2022-10-18 Redhill Biopharma Ltd. Sphingosine kinase 2 inhibitor for treating coronavirus infection in moderately severe patients with pneumonia
CN114105910B (zh) * 2021-11-02 2024-04-12 北京悦康科创医药科技股份有限公司 一种羟基脒基苯丙氨酸衍生物、药物组合物与用途

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5629327A (en) 1993-03-01 1997-05-13 Childrens Hospital Medical Center Corp. Methods and compositions for inhibition of angiogenesis
DE4321444A1 (de) 1993-06-28 1995-01-05 Bernd Prof Dr Clement Pharmazeutische Zubereitung
JP2852192B2 (ja) 1994-07-08 1999-01-27 カンセアフォースクニングスフォンデン・アフ・１９８９（フォンデン・チル・フレメ・アフ・エクスペリメンテル・カンセアフォースクニング） ｕＰＡＲのドメイン２＋３のｕＰＡ結合部位および抗体
CA2338073C (en) 1998-07-20 2010-09-21 Wilex Biotechnology Gmbh Novel urokinase inhibitors
EP1114024B1 (de) * 1998-09-18 2002-11-27 Pentapharm A.G. Urokinase-inhibitoren
US6410005B1 (en) * 2000-06-15 2002-06-25 Pmd Holdings Corp. Branched/block copolymers for treatment of keratinous substrates
DE10029014A1 (de) 2000-06-15 2001-12-20 Univ Schiller Jena Urokinase-Hemmstoffe
EP1280549A2 (en) 2000-06-27 2003-02-05 Vlaams Interuniversitair Instituut voor Biotechnologie vzw. Use of urokinase inhibitors for the treatment and/or prevention of pulmonary hypertension and/or cardiac remodelling
EP1182207B1 (en) 2000-08-11 2007-04-18 Dendreon Corporation Non-covalent inhibitors of urokinase and blood vessel formation
CA2387002A1 (en) 2000-08-11 2002-02-21 Wilex Ag Non-covalent inhibitors of urokinase and blood vessel formation
HUP0400651A2 (hu) * 2000-11-07 2004-06-28 Bristol-Myers Squibb Company Szerin proteáz inhibitorokként alkalmazható savszármazékok és ezeket tartalmazó gyógyszerkészítmények
WO2002063303A1 (en) * 2001-02-07 2002-08-15 Graffinity Pharmaceuticals Ag Screening method using solid supports modified with self-assembled monolayers
WO2002074756A2 (de) * 2001-03-21 2002-09-26 Pentapharm Ag Urokinase-inhibitoren
CH695999A5 (de) * 2002-02-28 2006-11-15 Wilex Ag Verfahren zur Herstellung von 3- Amidinophenylalanin-Derivaten.
EP1525195A2 (de) 2002-07-25 2005-04-27 Wilex AG Verfahren zur herstellung von phenylalanin-derivaten

Also Published As

Publication number Publication date
BRPI0410663B1 (pt) 2019-05-21
HUE025940T2 (en) 2016-05-30
AU2004240771A1 (en) 2004-12-02
EP2243774A1 (de) 2010-10-27
AU2004240771B2 (en) 2009-02-19
EP1628965A1 (de) 2006-03-01
MXPA05012675A (es) 2006-02-22
CN101791394A (zh) 2010-08-04
US20100068272A1 (en) 2010-03-18
EP1628965B1 (de) 2015-07-22
BRPI0410663B8 (pt) 2021-05-25
US20060142305A1 (en) 2006-06-29
CA2526989A1 (en) 2004-12-02
DE10323898A1 (de) 2004-12-23
PT1628965E (pt) 2015-11-04
AU2009201816A1 (en) 2009-05-28
DK1628965T3 (en) 2015-11-02
CN1795183B (zh) 2010-04-28
US7608623B2 (en) 2009-10-27
CN1795183A (zh) 2006-06-28
JP4621676B2 (ja) 2011-01-26
CA2526989C (en) 2012-12-04
ES2550611T3 (es) 2015-11-11
JP2007513062A (ja) 2007-05-24
WO2004103984A1 (de) 2004-12-02
US7807681B2 (en) 2010-10-05
US20080261998A1 (en) 2008-10-23
PL1628965T3 (pl) 2016-02-29

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Legal Events

Date Code Title Description
B25G Requested change of headquarter approved

Owner name: WILEX AG (DE)

Free format text: SEDE ALTERADA CONFORME SOLICITADO NA PETICAO NO 020080117818/RJ DE 08/09/2008.

B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]

Free format text: NOTIFICACAO DE ANUENCIA RELACIONADA COM O ART 229 DA LPI

B07A Application suspended after technical examination (opinion) [chapter 7.1 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

Free format text: PRAZO DE VALIDADE: 10 (DEZ) ANOS CONTADOS A PARTIR DE 21/05/2019, OBSERVADAS AS CONDICOES LEGAIS. (CO) 10 (DEZ) ANOS CONTADOS A PARTIR DE 21/05/2019, OBSERVADAS AS CONDICOES LEGAIS

B16C Correction of notification of the grant [chapter 16.3 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 26/05/2004 OBSERVADAS AS CONDICOES LEGAIS. PATENTE CONCEDIDA CONFORME ADI 5.529/DF

B21F Lapse acc. art. 78, item iv - on non-payment of the annual fees in time

Free format text: REFERENTE A 20A ANUIDADE.

B24J Lapse because of non-payment of annual fees (definitively: art 78 iv lpi, resolution 113/2013 art. 12)

Free format text: EM VIRTUDE DA EXTINCAO PUBLICADA NA RPI 2776 DE 19-03-2024 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDA A EXTINCAO DA PATENTE E SEUS CERTIFICADOS, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013.