BR9912327B1 - Inibidores da uroquinase - Google Patents
Inibidores da uroquinaseInfo
- Publication number
- BR9912327B1 BR9912327B1 BRPI9912327-4B1A BR9912327A BR9912327B1 BR 9912327 B1 BR9912327 B1 BR 9912327B1 BR 9912327 A BR9912327 A BR 9912327A BR 9912327 B1 BR9912327 B1 BR 9912327B1
- Authority
- BR
- Brazil
- Prior art keywords
- optionally
- alkyl
- substituted
- aryl
- ring
- Prior art date
Links
- 239000002797 plasminogen activator inhibitor Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 10
- 102000003990 Urokinase-type plasminogen activator Human genes 0.000 abstract 6
- 108090000435 Urokinase-type plasminogen activator Proteins 0.000 abstract 6
- 125000003118 aryl group Chemical group 0.000 abstract 6
- 229960005356 urokinase Drugs 0.000 abstract 6
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 3
- 125000001072 heteroaryl group Chemical group 0.000 abstract 3
- 125000005842 heteroatom Chemical group 0.000 abstract 3
- 150000003839 salts Chemical class 0.000 abstract 3
- 101100440695 Dictyostelium discoideum corB gene Proteins 0.000 abstract 2
- -1 Sulfonyl-substituted 3-amidino-phenylalanine Chemical class 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 238000003745 diagnosis Methods 0.000 abstract 2
- 230000006806 disease prevention Effects 0.000 abstract 2
- 210000002751 lymph Anatomy 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 2
- 230000008685 targeting Effects 0.000 abstract 2
- 238000002560 therapeutic procedure Methods 0.000 abstract 2
- IVWWFWFVSWOTLP-YVZVNANGSA-N (3'as,4r,7'as)-2,2,2',2'-tetramethylspiro[1,3-dioxolane-4,6'-4,7a-dihydro-3ah-[1,3]dioxolo[4,5-c]pyran]-7'-one Chemical compound C([C@@H]1OC(O[C@@H]1C1=O)(C)C)O[C@]21COC(C)(C)O2 IVWWFWFVSWOTLP-YVZVNANGSA-N 0.000 abstract 1
- DSSGKVAUNCQJTG-UHFFFAOYSA-N C(C)OC(=O)N1CCN(CC1)C(C(N)(CC1=CC(=CC=C1)C(N)=N)S(=O)(=O)C1=C(C=C(C=C1C(C)C)C(C)C)C(C)C)=O Chemical compound C(C)OC(=O)N1CCN(CC1)C(C(N)(CC1=CC(=CC=C1)C(N)=N)S(=O)(=O)C1=C(C=C(C=C1C(C)C)C(C)C)C(C)C)=O DSSGKVAUNCQJTG-UHFFFAOYSA-N 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 150000001409 amidines Chemical class 0.000 abstract 1
- 125000004104 aryloxy group Chemical group 0.000 abstract 1
- 125000001584 benzyloxycarbonyl group Chemical group C(=O)(OCC1=CC=CC=C1)* 0.000 abstract 1
- 125000001589 carboacyl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000005553 heteroaryloxy group Chemical group 0.000 abstract 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 125000006678 phenoxycarbonyl group Chemical group 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- UYWQUFXKFGHYNT-UHFFFAOYSA-N phenylmethyl ester of formic acid Natural products O=COCC1=CC=CC=C1 UYWQUFXKFGHYNT-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
- A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
- A61K51/04—Organic compounds
- A61K51/0404—Lipids, e.g. triglycerides; Polycationic carriers
- A61K51/0406—Amines, polyamines, e.g. spermine, spermidine, amino acids, (bis)guanidines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
- A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
- A61K51/04—Organic compounds
- A61K51/041—Heterocyclic compounds
- A61K51/044—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
- A61K51/0455—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
- A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
- A61K51/04—Organic compounds
- A61K51/041—Heterocyclic compounds
- A61K51/044—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
- A61K51/0459—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07D295/20—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 carbonic acid, or sulfur or nitrogen analogues thereof
- C07D295/205—Radicals derived from carbonic acid
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- Optics & Photonics (AREA)
- Physics & Mathematics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Molecular Biology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biophysics (AREA)
- Engineering & Computer Science (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Hydrogenated Pyridines (AREA)
- Enzymes And Modification Thereof (AREA)
- Medicinal Preparation (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
- Medicines Containing Plant Substances (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP98113519 | 1998-07-20 | ||
| PCT/EP1999/005145 WO2000004954A2 (de) | 1998-07-20 | 1999-07-20 | Neue urokinase-inhibitoren |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| BR9912327A BR9912327A (pt) | 2001-05-02 |
| BR9912327B1 true BR9912327B1 (pt) | 2013-11-12 |
Family
ID=8232314
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI9912327-4B1A BR9912327B1 (pt) | 1998-07-20 | 1999-07-20 | Inibidores da uroquinase |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US6624169B1 (pt) |
| EP (2) | EP1264828B1 (pt) |
| JP (1) | JP4603162B2 (pt) |
| AT (2) | ATE230599T1 (pt) |
| AU (1) | AU754958B2 (pt) |
| BR (1) | BR9912327B1 (pt) |
| CA (1) | CA2338073C (pt) |
| DE (2) | DE59909210D1 (pt) |
| ES (2) | ES2219607T3 (pt) |
| MX (1) | MXPA01000553A (pt) |
| PT (1) | PT1264828E (pt) |
| WO (1) | WO2000004954A2 (pt) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1114024B1 (de) * | 1998-09-18 | 2002-11-27 | Pentapharm A.G. | Urokinase-inhibitoren |
| DE10013715A1 (de) * | 2000-03-20 | 2001-09-27 | Wilex Biotechnology Gmbh | Hochselektive Inhibitoren des Urokinase-Plasminogenaktivators |
| DE10029014A1 (de) * | 2000-06-15 | 2001-12-20 | Univ Schiller Jena | Urokinase-Hemmstoffe |
| ATE386029T1 (de) | 2001-03-21 | 2008-03-15 | Wilex Ag | Urokinase-inhibitoren |
| DE50310038D1 (de) * | 2002-03-11 | 2008-08-07 | Curacyte Ag | Hemmstoffe der urokinase, ihre herstellung und verwendung |
| DE10225876A1 (de) | 2002-06-11 | 2003-12-24 | Wilex Ag | Guanidinophenylalaninverbindungen als Urokinase-Inhibitoren |
| DE10233632A1 (de) * | 2002-07-24 | 2004-02-05 | Wilex Ag | Formulierungen von Phenylalanin-Derivaten |
| DE10238048A1 (de) * | 2002-07-25 | 2004-02-05 | Wilex Ag | Verfahren zur Herstellung von Phenylalanin-Derivaten |
| EP1525195A2 (de) * | 2002-07-25 | 2005-04-27 | Wilex AG | Verfahren zur herstellung von phenylalanin-derivaten |
| DE10301300B4 (de) * | 2003-01-15 | 2009-07-16 | Curacyte Chemistry Gmbh | Verwendung von acylierten 4-Amidino- und 4-Guanidinobenzylaminen zur Inhibierung von Plasmakallikrein |
| DE10322191B4 (de) * | 2003-05-16 | 2014-02-27 | The Medicines Company (Leipzig) Gmbh | N-sulfonylierte Aminosäurederivate, Verfahren zu ihrer Herstellung und ihre Verwendung |
| DE10323898A1 (de) | 2003-05-26 | 2004-12-23 | Wilex Ag | Hydroxyamidin- und Hydroxyguanidin-Verbindungen als Urokinase-Hemmstoffe |
| DE10342108A1 (de) * | 2003-09-11 | 2005-04-14 | Curacyte Chemistry Gmbh | Basisch-substituierte Benzylaminanaloga als Inhibitoren des Gerinnungsfaktors Xa, ihre Herstellung und Verwendung |
| 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 |
| DE102004045720A1 (de) * | 2004-09-21 | 2006-03-23 | Wilex Ag | Stabile Dosierungsform von Phenylalanin-Derivaten |
| ATE442842T1 (de) | 2005-06-24 | 2009-10-15 | Wilex Ag | Verwendung von urokinase-inhibitoren zur behandlung und/oder vorbeugung von amyotrophischer lateralsklerose (als) |
| DE102006050672A1 (de) | 2006-10-24 | 2008-04-30 | Curacyte Discovery Gmbh | Hemmstoffe des Plasmins und des Plasmakallikreins |
| CA2800684A1 (en) * | 2010-05-26 | 2011-12-01 | Expression Pathology, Inc. | Urokinase-type plasminogen activator protein/plasminogen activator inhibitor type-1 protein selected reaction monitoring assay |
| EP2590945B1 (en) | 2010-07-07 | 2014-04-30 | The Medicines Company (Leipzig) GmbH | Serine protease inhibitors |
| EP3247376B1 (en) | 2015-03-30 | 2021-07-14 | Sunnybrook Research Institute | Treating prostate cancer |
| US10573824B2 (en) * | 2015-09-24 | 2020-02-25 | Lg Chem, Ltd. | Compound and organic electronic element comprising same |
| RU2727474C2 (ru) * | 2015-10-06 | 2020-07-21 | Редхилл Байофарма Лтд. | Виды комбинированной терапии для лечения рака |
| KR20220151613A (ko) | 2020-03-10 | 2022-11-15 | 레드힐 바이오파마 엘티디 | 코로나바이러스 감염의 치료 |
| 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 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU541738B2 (en) * | 1979-09-20 | 1985-01-17 | Nippon Chemiphar Co. Ltd. | Cyclohexane carboxylic acid derivatives |
| DE3577700D1 (de) * | 1984-11-30 | 1990-06-21 | Shosuke Okamoto | Lysinderivat und proteinase-inhibitor. |
| CA2073776A1 (en) * | 1990-11-15 | 1992-05-16 | Joerg Stuerzebecher | Meta-substituted phenyl alanine derivatives |
| DE59410179D1 (de) * | 1993-02-10 | 2002-10-10 | Pentapharm Ag Basel | Piperazide von substituierten phenylalanin-derivativen als thrombin inhibitoren |
| US5550213A (en) * | 1993-12-27 | 1996-08-27 | Rutgers, The State University Of New Jersey | Inhibitors of urokinase plasminogen activator |
| AU3107795A (en) * | 1994-08-09 | 1996-03-07 | Pentapharm Ag | Inhibitors of the benzamidine type |
| DE9418185U1 (de) * | 1994-11-12 | 1995-02-23 | Richard Wolf Gmbh, 75438 Knittlingen | Behälter für medizinische Instrumente |
| CH689611A5 (de) * | 1995-03-01 | 1999-07-15 | Pentapharm Ag | Urokinase-Inhibitoren. |
| EP1114024B1 (de) | 1998-09-18 | 2002-11-27 | Pentapharm A.G. | Urokinase-inhibitoren |
-
1999
- 1999-07-20 BR BRPI9912327-4B1A patent/BR9912327B1/pt not_active IP Right Cessation
- 1999-07-20 CA CA2338073A patent/CA2338073C/en not_active Expired - Fee Related
- 1999-07-20 EP EP02016038A patent/EP1264828B1/de not_active Expired - Lifetime
- 1999-07-20 MX MXPA01000553A patent/MXPA01000553A/es active IP Right Grant
- 1999-07-20 ES ES02016038T patent/ES2219607T3/es not_active Expired - Lifetime
- 1999-07-20 WO PCT/EP1999/005145 patent/WO2000004954A2/de active IP Right Grant
- 1999-07-20 ES ES99936570T patent/ES2189455T3/es not_active Expired - Lifetime
- 1999-07-20 DE DE59909210T patent/DE59909210D1/de not_active Expired - Lifetime
- 1999-07-20 AU AU51615/99A patent/AU754958B2/en not_active Ceased
- 1999-07-20 US US09/743,800 patent/US6624169B1/en not_active Expired - Lifetime
- 1999-07-20 AT AT99936570T patent/ATE230599T1/de active
- 1999-07-20 EP EP99936570A patent/EP1098651B1/de not_active Expired - Lifetime
- 1999-07-20 JP JP2000560945A patent/JP4603162B2/ja not_active Expired - Lifetime
- 1999-07-20 PT PT02016038T patent/PT1264828E/pt unknown
- 1999-07-20 AT AT02016038T patent/ATE264103T1/de active
- 1999-07-20 DE DE59903981T patent/DE59903981D1/de not_active Expired - Lifetime
-
2002
- 2002-07-26 US US10/202,850 patent/US6680320B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| CA2338073A1 (en) | 2000-02-03 |
| AU5161599A (en) | 2000-02-14 |
| EP1098651A2 (de) | 2001-05-16 |
| DE59903981D1 (de) | 2003-02-13 |
| ATE230599T1 (de) | 2003-01-15 |
| PT1264828E (pt) | 2004-08-31 |
| AU754958B2 (en) | 2002-11-28 |
| ES2219607T3 (es) | 2004-12-01 |
| DE59909210D1 (de) | 2004-05-19 |
| EP1098651B1 (de) | 2003-01-08 |
| CA2338073C (en) | 2010-09-21 |
| EP1264828B1 (de) | 2004-04-14 |
| JP4603162B2 (ja) | 2010-12-22 |
| ES2189455T3 (es) | 2003-07-01 |
| WO2000004954A3 (de) | 2000-06-22 |
| US20030013723A1 (en) | 2003-01-16 |
| ATE264103T1 (de) | 2004-04-15 |
| WO2000004954A2 (de) | 2000-02-03 |
| BR9912327A (pt) | 2001-05-02 |
| JP2002521348A (ja) | 2002-07-16 |
| US6624169B1 (en) | 2003-09-23 |
| MXPA01000553A (es) | 2002-04-24 |
| US6680320B2 (en) | 2004-01-20 |
| EP1264828A1 (de) | 2002-12-11 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B25D | Requested change of name of applicant approved | ||
| B07A | Application suspended after technical examination (opinion) [chapter 7.1 patent gazette] | ||
| 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. |
|
| B09B | Patent application refused [chapter 9.2 patent gazette] |
Free format text: INDEFIRO O PEDIDO DE ACORDO COM O(S) ARTIGO(S) 8O, 13 E 25 DA LPI. |
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| B12B | Appeal against refusal [chapter 12.2 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 |
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| 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 12/11/2013, OBSERVADAS AS CONDICOES LEGAIS. |
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| B16C | Correction of notification of the grant [chapter 16.3 patent gazette] |
Free format text: REFERENTE AO DESPACHO 16.1 PUBLICADO NA RPI 2236 DE 12.11.2013, QUANTO AO NOME E ENDERECO DO TITULAR |
|
| B15K | Others concerning applications: alteration of classification |
Ipc: A61K 31/495 (2006.01), A61K 51/04 (2006.0 |
|
| B21F | Lapse acc. art. 78, item iv - on non-payment of the annual fees in time |
Free format text: REFERENTE A 20A ANUIDADE. |
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| 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 2523 DE 14-05-2019 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. |