AR052768A1 - Derivados de aza-azucar, inhibidores de heparanasas y las composiciones que los contienen - Google Patents
Derivados de aza-azucar, inhibidores de heparanasas y las composiciones que los contienenInfo
- Publication number
- AR052768A1 AR052768A1 ARP050103039A ARP050103039A AR052768A1 AR 052768 A1 AR052768 A1 AR 052768A1 AR P050103039 A ARP050103039 A AR P050103039A AR P050103039 A ARP050103039 A AR P050103039A AR 052768 A1 AR052768 A1 AR 052768A1
- Authority
- AR
- Argentina
- Prior art keywords
- radical
- formula
- alkyl
- hydroxyl
- aralkyl
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H5/00—Compounds containing saccharide radicals in which the hetero bonds to oxygen have been replaced by the same number of hetero bonds to halogen, nitrogen, sulfur, selenium, or tellurium
- C07H5/04—Compounds containing saccharide radicals in which the hetero bonds to oxygen have been replaced by the same number of hetero bonds to halogen, nitrogen, sulfur, selenium, or tellurium to nitrogen
- C07H5/06—Aminosugars
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- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7008—Compounds having an amino group directly attached to a carbon atom of the saccharide radical, e.g. D-galactosamine, ranimustine
-
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/702—Oligosaccharides, i.e. having three to five saccharide radicals attached to each other by glycosidic linkages
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- 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
-
- 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
- A61P9/08—Vasodilators for multiple indications
-
- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H3/00—Compounds containing only hydrogen atoms and saccharide radicals having only carbon, hydrogen, and oxygen atoms
- C07H3/06—Oligosaccharides, i.e. having three to five saccharide radicals attached to each other by glycosidic linkages
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biotechnology (AREA)
- Biochemistry (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Urology & Nephrology (AREA)
- Oncology (AREA)
- Rheumatology (AREA)
- Ophthalmology & Optometry (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Dermatology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Pain & Pain Management (AREA)
- Vascular Medicine (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
Abstract
La presente se refiere a los compuestos inhibidores de heparanasas, que responden a la formula general (1). Estos compuestos son utiles en el carcinoma de pulmon, mama, prostata y esofago y de enfermedades cardiovasculares como la aterosclerosis y las retenosis post angioplastia y enfermedades inflamatorios cronicas. Reivindicacion 1: Compuestos de formula general (1), donde: R representa un átomo de hidrogeno, un radical hidroxilo, un radical -OSO3-, un radical -O-alquiloC1-5 o un radical - O-aralquilo; Z representa un radical COO- o un radical hidroxilo; X representa un radical hidroxilo o una unidad sacarídica de formula (2); donde: R1 representa un átomo de oxígeno, que permite a la formula (2) ligarse a la unidad aza-azucar o a otra unidad sacarídica; R2 representa un radical -NH2, un radical -NHCOalquiloC1-5, un radical -NHCOarilo, un radical -NHSO3-, un radical hidroxilo, un radical -O-alquiloC1-5, un radical -O-aralquilo o un radical -OSO3-; R3 representa un radical hidroxilo, un radical -OSO3-, un radical -O-alquiloC1-5 o un radical -O-aralquilo; R4 representa un radical hidroxilo, un radical -OSO3-, un radical -O-alquiloC1-5, un radical -O-aralquilo o una unidad sacarídica de formula (3), donde: R6 representa un átomo de oxígeno, que permite a la formula (3) ligarse a otra unidad sacarídica de formula (2); R7 y R8 tienen la misma definicion que R3 tal como se definio anteriormente; R9 representa un grupo hidroxilo, un radical -OSO3-, un radical -O- alquiloC1-5, un radical -O-aralquilo o una unidad sacarídica de formula (2) como se definio anteriormente; R5 tiene la misma definicion que R3 tal como se definio anteriormente; Y representa un átomo de hidrogeno, un radical alquilo C1-5 o una unidad sacarídica de formula (4), donde: R10, R12 y R13 tienen, respectivamente, las mismas definiciones que R5, R3 y R2 tal como se definieron anteriormente; R11 representa: un radical alquileno C1-3 que permite a la formula (4) unirse a la unidad aza-sucre; o un átomo de oxígeno que permite a la formula (4) unirse a otra unidad sacarísica; R14 representa un radical -O-alquiloC1-5 o un radical de formula -O-E, en donde E representa un radical de formula (5), donde: R15 representa un radical - O-alquiloC1-5, un radical -O-aralquilo o una unidad sacarídica de formula (4) en donde R11 representa un átomo de oxígeno; R16 y R17 tienen la misma definicion que R3 tal como se definio anteriormente; con la condicion, sin embargo, de que cuando X y R representan cada uno un radical hidroxilo, Y no represente un átomo de hidrogeno; y entendiéndose que el numero de unidades sacarídicas contenidas por el compuesto de formulas (1) se encuentra entre 1 y 10; en forma libre o en forma de sales formadas con una base o un ácido farmacéuticamente aceptables, como así también en forma de solventes o de hidratos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR0408160A FR2873377B1 (fr) | 2004-07-23 | 2004-07-23 | Derives d'azasucre, inhibiteurs d'heparanases, leur procede de preparation, les compositions en contenant et leur utilisation |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR052768A1 true AR052768A1 (es) | 2007-04-04 |
Family
ID=34949814
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP050103039A AR052768A1 (es) | 2004-07-23 | 2005-07-22 | Derivados de aza-azucar, inhibidores de heparanasas y las composiciones que los contienen |
Country Status (18)
| Country | Link |
|---|---|
| US (2) | US20070270354A1 (es) |
| EP (1) | EP1773854B1 (es) |
| JP (1) | JP2008507496A (es) |
| KR (1) | KR20070034996A (es) |
| CN (1) | CN1956991A (es) |
| AR (1) | AR052768A1 (es) |
| AT (1) | ATE525382T1 (es) |
| AU (1) | AU2005276351A1 (es) |
| BR (1) | BRPI0511480A (es) |
| CA (1) | CA2564224A1 (es) |
| FR (1) | FR2873377B1 (es) |
| IL (1) | IL179076A (es) |
| NZ (1) | NZ552708A (es) |
| PE (1) | PE20060571A1 (es) |
| RU (1) | RU2007106880A (es) |
| TW (1) | TW200617018A (es) |
| UY (1) | UY29030A1 (es) |
| WO (1) | WO2006021653A2 (es) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0816613A2 (pt) | 2007-10-16 | 2018-10-23 | Progen Pharmaceuticals Ltd | novos derivados de oligossacarideos sulfatados |
| AU2010234779A1 (en) | 2009-03-30 | 2011-10-20 | University Of Georgia Research Foundation, Inc. | Heparan sulfate synthesis |
| FR2949114B1 (fr) * | 2009-08-14 | 2011-08-26 | Sanofi Aventis | OCTASACCHARIDES N-ACYLES ACTIVATEURS DES RECEPTEURS DES FGFs, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE |
| FR2949115B1 (fr) | 2009-08-14 | 2012-11-02 | Sanofi Aventis | OLIGOSACCHARIDES N-SULFATES ACTIVATEURS DES RECEPTEURS DES FGFs, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE |
| CN102655863B (zh) * | 2009-09-30 | 2013-11-20 | 株式会社资生堂 | 乙酰肝素酶活性抑制剂 |
| CN101704812B (zh) * | 2009-11-09 | 2014-03-05 | 北京大学 | 氮杂糖类化合物及其制备方法和应用 |
| US10469224B2 (en) * | 2016-09-30 | 2019-11-05 | Qualcomm Incorporated | Joint transmission of precoded and unprecoded sounding reference signals in uplink |
| US11787783B2 (en) | 2016-12-13 | 2023-10-17 | Beta Therapeutics Pty Ltd | Heparanase inhibitors and use thereof |
| CN110291073A (zh) | 2016-12-13 | 2019-09-27 | 贝塔医疗私人有限公司 | 乙酰肝素酶抑制剂及其用途 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5378829A (en) * | 1990-04-23 | 1995-01-03 | Akzo N.V. | Sulfated glycosaminoglycanoid derivatives of the heparin and heparan sulfate type |
| KR970001164B1 (ko) * | 1993-06-09 | 1997-01-29 | 한국과학기술연구원 | 세팔로스포린계 항생제 및 그의 제조방법 |
| US6190875B1 (en) * | 1997-09-02 | 2001-02-20 | Insight Strategy & Marketing Ltd. | Method of screening for potential anti-metastatic and anti-inflammatory agents using mammalian heparanase as a probe |
| US6274597B1 (en) * | 1998-06-01 | 2001-08-14 | Mount Sinai School Of Medicine Of New York University | Method of enhancing lysosomal α-Galactosidase A |
-
2004
- 2004-07-23 FR FR0408160A patent/FR2873377B1/fr not_active Expired - Fee Related
-
2005
- 2005-07-20 CA CA002564224A patent/CA2564224A1/fr not_active Abandoned
- 2005-07-20 CN CNA2005800165037A patent/CN1956991A/zh active Pending
- 2005-07-20 RU RU2007106880/04A patent/RU2007106880A/ru not_active Application Discontinuation
- 2005-07-20 JP JP2007521986A patent/JP2008507496A/ja active Pending
- 2005-07-20 EP EP05790838A patent/EP1773854B1/fr active Active
- 2005-07-20 WO PCT/FR2005/001851 patent/WO2006021653A2/fr active Application Filing
- 2005-07-20 AT AT05790838T patent/ATE525382T1/de not_active IP Right Cessation
- 2005-07-20 AU AU2005276351A patent/AU2005276351A1/en not_active Abandoned
- 2005-07-20 NZ NZ552708A patent/NZ552708A/en not_active IP Right Cessation
- 2005-07-20 KR KR1020067024508A patent/KR20070034996A/ko not_active Application Discontinuation
- 2005-07-20 BR BRPI0511480-2A patent/BRPI0511480A/pt not_active IP Right Cessation
- 2005-07-21 PE PE2005000849A patent/PE20060571A1/es not_active Application Discontinuation
- 2005-07-22 UY UY29030A patent/UY29030A1/es not_active Application Discontinuation
- 2005-07-22 TW TW094125039A patent/TW200617018A/zh unknown
- 2005-07-22 AR ARP050103039A patent/AR052768A1/es not_active Application Discontinuation
-
2006
- 2006-11-06 IL IL179076A patent/IL179076A/en not_active IP Right Cessation
-
2007
- 2007-01-23 US US11/625,994 patent/US20070270354A1/en not_active Abandoned
-
2011
- 2011-09-08 US US13/227,922 patent/US20120065153A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| UY29030A1 (es) | 2006-02-24 |
| WO2006021653A2 (fr) | 2006-03-02 |
| ATE525382T1 (de) | 2011-10-15 |
| PE20060571A1 (es) | 2006-07-22 |
| BRPI0511480A (pt) | 2007-12-26 |
| EP1773854B1 (fr) | 2011-09-21 |
| FR2873377B1 (fr) | 2006-10-13 |
| RU2007106880A (ru) | 2008-09-10 |
| CN1956991A (zh) | 2007-05-02 |
| US20070270354A1 (en) | 2007-11-22 |
| CA2564224A1 (fr) | 2006-03-02 |
| AU2005276351A1 (en) | 2006-03-02 |
| IL179076A0 (en) | 2007-03-08 |
| NZ552708A (en) | 2010-07-30 |
| KR20070034996A (ko) | 2007-03-29 |
| IL179076A (en) | 2011-10-31 |
| EP1773854A2 (fr) | 2007-04-18 |
| WO2006021653A3 (fr) | 2006-08-10 |
| US20120065153A1 (en) | 2012-03-15 |
| TW200617018A (en) | 2006-06-01 |
| FR2873377A1 (fr) | 2006-01-27 |
| JP2008507496A (ja) | 2008-03-13 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |