BRPI0410663B8 - compostos de hidroxiamidina e hidroxiguanidina e seus usos - Google Patents
compostos de hidroxiamidina e hidroxiguanidina e seus usosInfo
- Publication number
- BRPI0410663B8 BRPI0410663B8 BRPI0410663A BRPI0410663A BRPI0410663B8 BR PI0410663 B8 BRPI0410663 B8 BR PI0410663B8 BR PI0410663 A BRPI0410663 A BR PI0410663A BR PI0410663 A BRPI0410663 A BR PI0410663A BR PI0410663 B8 BRPI0410663 B8 BR PI0410663B8
- Authority
- BR
- Brazil
- Prior art keywords
- compounds
- hydroxyamidine
- urokinase
- hydroxyguanidine
- relates
- Prior art date
Links
- WFBHRSAKANVBKH-UHFFFAOYSA-N N-hydroxyguanidine Chemical class NC(=N)NO WFBHRSAKANVBKH-UHFFFAOYSA-N 0.000 title abstract 3
- 102000003990 Urokinase-type plasminogen activator Human genes 0.000 abstract 3
- 108090000435 Urokinase-type plasminogen activator Proteins 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 229960005356 urokinase Drugs 0.000 abstract 2
- 206010027476 Metastases Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 230000009401 metastasis Effects 0.000 abstract 1
- 239000002797 plasminogen activator inhibitor Substances 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
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)
- Genetics & Genomics (AREA)
- Biochemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (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)
- Medicinal Preparation (AREA)
- Peptides Or Proteins (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.
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 BRPI0410663A (pt) | 2006-06-20 |
| BRPI0410663B1 BRPI0410663B1 (pt) | 2019-05-21 |
| BRPI0410663B8 true 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) | EP1628965B1 (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)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2003219039A1 (en) * | 2002-03-11 | 2003-09-22 | Curacyte Ag | Urokinase inhibitors, production and use thereof |
| 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 |
| WO2006136419A2 (en) | 2005-06-24 | 2006-12-28 | 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 |
| DE102008007381A1 (de) | 2008-02-01 | 2009-08-13 | Dritte Patentportfolio Beteiligungsgesellschaft Mbh & Co.Kg | Amidine und Guanidine und deren Derivate zur Behandlung von Krankheiten |
| US9662308B2 (en) | 2008-02-01 | 2017-05-30 | Dritte Patentportfolio Beteiligungsgesellschaft Mbh & Co. Kg | Orally bioavailable pentamidine prodrugs for the treatment of diseases |
| 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 |
| EP3359255A4 (en) | 2015-10-06 | 2019-06-12 | Redhill Biopharma Ltd. | POLYTHERAPIES FOR THE TREATMENT OF CANCER |
| SG11201912043QA (en) * | 2017-07-21 | 2020-02-27 | Redhill Biopharma Ltd | Use of wx-uk1 and its prodrug, wx-671, for the treatment of non-cancerous medical conditions |
| CN117695284A (zh) | 2020-03-10 | 2024-03-15 | 红山生物医药有限公司 | 冠状病毒感染的治疗 |
| 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)
| 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 |
| ES2189455T3 (es) | 1998-07-20 | 2003-07-01 | Wilex Ag | Nuevos agentes inhibidores de la urocinasa. |
| US7745441B1 (en) * | 1998-09-18 | 2010-06-29 | Wilex Ag | Urokinase inhibitors |
| DE10029014A1 (de) | 2000-06-15 | 2001-12-20 | Univ Schiller Jena | Urokinase-Hemmstoffe |
| US6410005B1 (en) * | 2000-06-15 | 2002-06-25 | Pmd Holdings Corp. | Branched/block copolymers for treatment of keratinous substrates |
| US20030125233A1 (en) | 2000-06-27 | 2003-07-03 | Peter Carmeliet | Use of urokinase inhibitors for the treatment and/or prevention of pulmonary hypertension and/or cardiac remodelling |
| CA2387002A1 (en) | 2000-08-11 | 2002-02-21 | Corvas International, Inc. | Non-covalent inhibitors of urokinase and blood vessel formation |
| ES2285989T3 (es) * | 2000-08-11 | 2007-12-01 | Wilex Ag | Inhibidores no covalentes de la uroquinasa y de la formacion de vasos sanguineos. |
| EP1332131A2 (en) * | 2000-11-07 | 2003-08-06 | Bristol-Myers Squibb Company | Acid derivatives useful as serine protease inhibitors |
| WO2002063303A1 (en) * | 2001-02-07 | 2002-08-15 | Graffinity Pharmaceuticals Ag | Screening method using solid supports modified with self-assembled monolayers |
| JP4414652B2 (ja) * | 2001-03-21 | 2010-02-10 | ヴィレックス アクチェンゲゼルシャフト | ウロキナーゼ阻害剤 |
| 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 |
-
2003
- 2003-05-26 DE DE10323898A patent/DE10323898A1/de not_active Ceased
-
2004
- 2004-05-26 EP EP04734821.4A patent/EP1628965B1/de not_active Expired - Lifetime
- 2004-05-26 AU AU2004240771A patent/AU2004240771B2/en not_active Ceased
- 2004-05-26 PT PT47348214T patent/PT1628965E/pt unknown
- 2004-05-26 CN CN2004800145217A patent/CN1795183B/zh not_active Expired - Fee Related
- 2004-05-26 MX MXPA05012675A patent/MXPA05012675A/es active IP Right Grant
- 2004-05-26 BR BRPI0410663A patent/BRPI0410663B8/pt not_active IP Right Cessation
- 2004-05-26 CN CN201010143428A patent/CN101791394A/zh active Pending
- 2004-05-26 ES ES04734821.4T patent/ES2550611T3/es not_active Expired - Lifetime
- 2004-05-26 CA CA2526989A patent/CA2526989C/en not_active Expired - Lifetime
- 2004-05-26 DK DK04734821.4T patent/DK1628965T3/en active
- 2004-05-26 HU HUE04734821A patent/HUE025940T2/en unknown
- 2004-05-26 WO PCT/EP2004/005682 patent/WO2004103984A1/de active Application Filing
- 2004-05-26 EP EP10163579A patent/EP2243774A1/de not_active Withdrawn
- 2004-05-26 PL PL04734821T patent/PL1628965T3/pl unknown
- 2004-05-26 JP JP2006529927A patent/JP4621676B2/ja not_active Expired - Lifetime
-
2005
- 2005-11-28 US US11/287,480 patent/US7608623B2/en active Active
-
2008
- 2008-04-18 US US12/105,975 patent/US7807681B2/en not_active Expired - Lifetime
-
2009
- 2009-05-06 AU AU2009201816A patent/AU2009201816A1/en not_active Abandoned
- 2009-09-14 US US12/558,790 patent/US20100068272A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| CN1795183B (zh) | 2010-04-28 |
| US20080261998A1 (en) | 2008-10-23 |
| AU2009201816A1 (en) | 2009-05-28 |
| DK1628965T3 (en) | 2015-11-02 |
| BRPI0410663A (pt) | 2006-06-20 |
| DE10323898A1 (de) | 2004-12-23 |
| EP2243774A1 (de) | 2010-10-27 |
| AU2004240771A1 (en) | 2004-12-02 |
| PT1628965E (pt) | 2015-11-04 |
| US20060142305A1 (en) | 2006-06-29 |
| MXPA05012675A (es) | 2006-02-22 |
| CN1795183A (zh) | 2006-06-28 |
| EP1628965A1 (de) | 2006-03-01 |
| CA2526989C (en) | 2012-12-04 |
| US7807681B2 (en) | 2010-10-05 |
| US7608623B2 (en) | 2009-10-27 |
| CN101791394A (zh) | 2010-08-04 |
| PL1628965T3 (pl) | 2016-02-29 |
| AU2004240771B2 (en) | 2009-02-19 |
| WO2004103984A1 (de) | 2004-12-02 |
| US20100068272A1 (en) | 2010-03-18 |
| HUE025940T2 (en) | 2016-05-30 |
| JP4621676B2 (ja) | 2011-01-26 |
| ES2550611T3 (es) | 2015-11-11 |
| JP2007513062A (ja) | 2007-05-24 |
| CA2526989A1 (en) | 2004-12-02 |
| BRPI0410663B1 (pt) | 2019-05-21 |
| EP1628965B1 (de) | 2015-07-22 |
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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. |