HUP0203899A2 - Alfavbéta3 vagy alfavbéta5 integrin antagonistát és citosztatikumot tartalmazó konjugátumok, eljárás előállításukra és ilyen konjugátumokat tartalmazó gyógyászati készítmények - Google Patents
Alfavbéta3 vagy alfavbéta5 integrin antagonistát és citosztatikumot tartalmazó konjugátumok, eljárás előállításukra és ilyen konjugátumokat tartalmazó gyógyászati készítményekInfo
- Publication number
- HUP0203899A2 HUP0203899A2 HU0203899A HUP0203899A HUP0203899A2 HU P0203899 A2 HUP0203899 A2 HU P0203899A2 HU 0203899 A HU0203899 A HU 0203899A HU P0203899 A HUP0203899 A HU P0203899A HU P0203899 A2 HUP0203899 A2 HU P0203899A2
- Authority
- HU
- Hungary
- Prior art keywords
- cytostatic
- symbol
- conjugates
- integrin
- group
- Prior art date
Links
- 239000000824 cytostatic agent Substances 0.000 title abstract 9
- 230000001085 cytostatic effect Effects 0.000 title abstract 9
- 229940123038 Integrin antagonist Drugs 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 238000002360 preparation method Methods 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 230000008878 coupling Effects 0.000 abstract 3
- 238000010168 coupling process Methods 0.000 abstract 3
- 238000005859 coupling reaction Methods 0.000 abstract 3
- 102000006495 integrins Human genes 0.000 abstract 2
- 108010044426 integrins Proteins 0.000 abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 238000003776 cleavage reaction Methods 0.000 abstract 1
- 231100000433 cytotoxic Toxicity 0.000 abstract 1
- 230000001472 cytotoxic effect Effects 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 230000002255 enzymatic effect Effects 0.000 abstract 1
- 230000003301 hydrolyzing effect Effects 0.000 abstract 1
- 230000003834 intracellular effect Effects 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 108090000765 processed proteins & peptides Proteins 0.000 abstract 1
- 230000007017 scission Effects 0.000 abstract 1
- 210000002966 serum Anatomy 0.000 abstract 1
- 230000008685 targeting Effects 0.000 abstract 1
- 210000004881 tumor cell Anatomy 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/55—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicinal Preparation (AREA)
- Plural Heterocyclic Compounds (AREA)
- Indole Compounds (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
- Peptides Or Proteins (AREA)
Abstract
A találmány konjugátumra vonatkozik, amely tartalmaz a) egya<$]Symbol><>vb3 vagy <><>a<><>v<><>b<$]Symbol><>5 integrinreceptorokat célzó nem peptid részt; b) egy kapcsolóegységet, amelyenzimatikusan vagy hidrolitikusan hasítható a citotoxikus csoport vagyegy citosztatikum vagy egy citosztatikus származék csoportjafelszabadulásával és c) egy citosztatikus csoportot vagy egycitosztatikumból vagy egy citosztatikus származékból leszármaztatottcsoportot. A fenti citosztatikumok daganatspecifikus hatássalrendelkeznek azáltal, hogy <><><>a<$]Symbol><>v<><><>b<$]Symbol><>3integrin antagonistákhoz kapcsolódnak előnyös kapcsolóegységekkel. Azelőnyös kapcsolóegységek biztosítják a citosztatikum és az<><>a<$]Symbol><>v<><><>b<$]Symbol><>3 integrin antagonistakonjugátumának szérumstabilitását, és ugyanakkor az enzimatikus vagyhidrolitikus hasíthatóságuk révén a citosztatikum felszabadulásávalbiztosítják a kívánt intracelluláris hatást a daganatsejtekben. Atalálmány tárgya továbbá eljárás a konjugátumok előállítására,valamint a konjugátumokat tartalmazó gyógyászati készítmények. Ó
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US39216799A | 1999-09-08 | 1999-09-08 | |
| US60677200A | 2000-06-29 | 2000-06-29 | |
| PCT/EP2000/008361 WO2001017563A2 (en) | 1999-09-08 | 2000-08-28 | Integrin-mediated drug targeting |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HUP0203899A2 true HUP0203899A2 (hu) | 2003-02-28 |
| HUP0203899A3 HUP0203899A3 (en) | 2004-09-28 |
Family
ID=27013781
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0203899A HUP0203899A3 (en) | 1999-09-08 | 2000-08-28 | Conjugates containing alphavbetha3 or alphavbetha5 integrin antagonist and cytostatic, process for their preparation and pharmaceutical compositions containing the same |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US20060189544A1 (hu) |
| EP (1) | EP1235595B8 (hu) |
| JP (1) | JP2003508497A (hu) |
| CN (1) | CN1402643A (hu) |
| AT (1) | ATE438413T1 (hu) |
| AU (1) | AU773781B2 (hu) |
| BR (1) | BR0013883A (hu) |
| CA (1) | CA2383981A1 (hu) |
| DE (1) | DE60042700D1 (hu) |
| ES (1) | ES2330079T3 (hu) |
| HU (1) | HUP0203899A3 (hu) |
| MX (1) | MXPA02002488A (hu) |
| NZ (1) | NZ517620A (hu) |
| PL (1) | PL354268A1 (hu) |
| RU (1) | RU2002109215A (hu) |
| WO (1) | WO2001017563A2 (hu) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1219305A1 (en) * | 2000-12-27 | 2002-07-03 | Bayer Aktiengesellschaft | Conjugates of integrin receptor antagonists and a cytostatic agent having specifically cleavable linking units |
| EP1238678A1 (en) * | 2001-03-08 | 2002-09-11 | Bayer Aktiengesellschaft | Enzyme-activated cytostatic conjugates with integrin ligands |
| ITRM20040240A1 (it) * | 2004-05-13 | 2004-08-13 | Ist Naz Stud Cura Dei Tumori | Camptotecine coniugate in posizione 7 con antagonisti delle integrine. |
| ITRM20040241A1 (it) * | 2004-05-13 | 2004-08-13 | Ist Naz Stud Cura Dei Tumori | Camptotecine coniugate in posizione 20 con antagonisti delle integrine. |
| CN105566338B (zh) * | 2014-10-08 | 2017-11-21 | 兰州大学 | 一种喜树碱类化合物及其制备方法和用途 |
| CN108456154A (zh) * | 2018-04-13 | 2018-08-28 | 昆明理工大学 | 一种n-叔丁氧羰基烃基胍的制备方法 |
| EP4412656A1 (en) * | 2021-10-04 | 2024-08-14 | Vincerx Pharma GmbH | Compounds, pharmaceutical compositions, and methods for the treatment, prevention, or management of hyperproliferative disorders |
| WO2023057813A1 (en) * | 2021-10-04 | 2023-04-13 | Vincerx Pharma Gmbh | Compounds, pharmaceutical compositions, and methods for the treatment, prevention, or management of hyperproliferative disorders |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2132091C (en) * | 1992-04-03 | 2008-09-16 | Kyung J. Kim | Antibodies to alphavbeta3 integrin |
| WO1997039021A1 (en) * | 1995-12-21 | 1997-10-23 | The Scripps Research Institute | Targeted therapeutic or diagnostic agents and methods of making and using same |
-
2000
- 2000-08-28 CA CA002383981A patent/CA2383981A1/en not_active Abandoned
- 2000-08-28 CN CN00814704A patent/CN1402643A/zh active Pending
- 2000-08-28 ES ES00965901T patent/ES2330079T3/es not_active Expired - Lifetime
- 2000-08-28 HU HU0203899A patent/HUP0203899A3/hu unknown
- 2000-08-28 EP EP00965901A patent/EP1235595B8/en not_active Expired - Lifetime
- 2000-08-28 AT AT00965901T patent/ATE438413T1/de not_active IP Right Cessation
- 2000-08-28 MX MXPA02002488A patent/MXPA02002488A/es unknown
- 2000-08-28 NZ NZ517620A patent/NZ517620A/en unknown
- 2000-08-28 WO PCT/EP2000/008361 patent/WO2001017563A2/en active Search and Examination
- 2000-08-28 BR BR0013883-5A patent/BR0013883A/pt not_active IP Right Cessation
- 2000-08-28 RU RU2002109215/15A patent/RU2002109215A/ru not_active Application Discontinuation
- 2000-08-28 AU AU76487/00A patent/AU773781B2/en not_active Ceased
- 2000-08-28 JP JP2001521351A patent/JP2003508497A/ja active Pending
- 2000-08-28 PL PL00354268A patent/PL354268A1/xx not_active Application Discontinuation
- 2000-08-28 DE DE60042700T patent/DE60042700D1/de not_active Expired - Lifetime
-
2006
- 2006-04-07 US US11/399,985 patent/US20060189544A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| DE60042700D1 (de) | 2009-09-17 |
| HUP0203899A3 (en) | 2004-09-28 |
| WO2001017563A2 (en) | 2001-03-15 |
| EP1235595B1 (en) | 2009-08-05 |
| AU7648700A (en) | 2001-04-10 |
| CA2383981A1 (en) | 2001-03-15 |
| WO2001017563A3 (en) | 2002-07-11 |
| US20060189544A1 (en) | 2006-08-24 |
| BR0013883A (pt) | 2002-05-07 |
| CN1402643A (zh) | 2003-03-12 |
| ATE438413T1 (de) | 2009-08-15 |
| PL354268A1 (en) | 2003-12-29 |
| NZ517620A (en) | 2004-02-27 |
| RU2002109215A (ru) | 2003-12-10 |
| EP1235595A2 (en) | 2002-09-04 |
| ES2330079T3 (es) | 2009-12-04 |
| AU773781B2 (en) | 2004-06-03 |
| MXPA02002488A (es) | 2002-08-12 |
| EP1235595B8 (en) | 2009-10-07 |
| JP2003508497A (ja) | 2003-03-04 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| BR0011772A (pt) | Conjugado de droga-oligÈmero, composição farmacêutica, método de solubilização de uma droga em uma microemulsão, e, métodos para fornecer um conjugado de droga ativa - hidrófilo e um conjugado de droga ativa - peg a um sìtio de um indivìduo | |
| HUP0204562A2 (hu) | Poliglutaminsav-kamptotecin konjugátumok, eljárás előállításukra és ilyen konjugátumokat tartalmazó gyógyászati készítmények | |
| WO2000052015A3 (en) | Novel phosphorus-containing prodrugs | |
| AU3468900A (en) | Cyclodextrin polymers for use as drug carriers | |
| MY116287A (en) | Polymeric derivatives of camptothecins | |
| WO2001032632A3 (en) | Pharmaceutically active 4-substituted pyrimidine derivatives | |
| TR200102603T2 (tr) | Antitümör aktiviteye sahip olan kamptotesin türevleri | |
| IL161290A0 (en) | Stable composition comprising particles in a frozen aqueous matrix | |
| ATE387430T1 (de) | Verbindungen und zusammensetzungen zur abgabe aktiver wirkstoffe | |
| CA2289202A1 (en) | Solid pharmaceutical formulations containing a physical mixture of sulfoalkyl ether cyclodextrin and a therapeutic agent | |
| EP0993831A3 (en) | Compounds and compositions for delivering active agents | |
| WO2005030258A3 (en) | Small molecule compositions and methods for increasing drug efficiency using compositions thereof | |
| MXPA02001340A (es) | Compuestos novedosos 1,4-benzodiazepina y derivados de los mismos. | |
| NZ505339A (en) | Camptothecin tetracyclic derivatives useful for inhibiting topoisomerase I and/or II pyridine intermediates thereof | |
| ES2302391T3 (es) | Procedimiento de administracion de un compuesto a celulas resistentes a multi-farmacos. | |
| ES2169414T3 (es) | Amino-azucar citotoxico y derivados de azucares relacionados de indolopirrolocarbazoles. | |
| SA93140336B1 (ar) | مشتقات هيدرازين hydrazine تستخدم كمضادات للفيروسات من النوع رترو antirctroviral (رتروفيروسات) | |
| HUP0203899A2 (hu) | Alfavbéta3 vagy alfavbéta5 integrin antagonistát és citosztatikumot tartalmazó konjugátumok, eljárás előállításukra és ilyen konjugátumokat tartalmazó gyógyászati készítmények | |
| IL141236A0 (en) | New oral formulations for 5-ht4 agonists or antagonists | |
| AU7134898A (en) | Biodegradable microparticles for the sustained delivery of therapeutic drugs | |
| MY133112A (en) | 3-amino-3-arylpropan-1-ol derivatives, and their preparation and use | |
| WO2003086471A3 (en) | Lyophilized and liquid preparations comprising a polysaccharide derivative of camptothecin | |
| FR2717081B1 (fr) | Rétropeptides, anticorps dirigés contre ces derniers, et leurs utilisations pour la vaccination et le diagnostic in vitro. | |
| WO2001030391A3 (en) | Pharmaceutical composition containing midazolam | |
| KR20020057797A (ko) | 특이적으로 표적화된 촉매적 안타고니스트 및 그 용도 |