PE20080316A1 - Compuestos de aziridinil-epotilona - Google Patents
Compuestos de aziridinil-epotilonaInfo
- Publication number
- PE20080316A1 PE20080316A1 PE2007000648A PE2007000648A PE20080316A1 PE 20080316 A1 PE20080316 A1 PE 20080316A1 PE 2007000648 A PE2007000648 A PE 2007000648A PE 2007000648 A PE2007000648 A PE 2007000648A PE 20080316 A1 PE20080316 A1 PE 20080316A1
- Authority
- PE
- Peru
- Prior art keywords
- rent
- epotilone
- aziridinyl
- compounds
- substitute
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 abstract 2
- 101100495911 Arabidopsis thaliana CHR10 gene Proteins 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical group [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 229940014144 folate Drugs 0.000 abstract 1
- OVBPIULPVIDEAO-LBPRGKRZSA-N folic acid Chemical compound C=1N=C2NC(N)=NC(=O)C2=NC=1CNC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 OVBPIULPVIDEAO-LBPRGKRZSA-N 0.000 abstract 1
- 235000019152 folic acid Nutrition 0.000 abstract 1
- 239000011724 folic acid Substances 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
-
- 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
- A61K31/396—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having three-membered rings, e.g. aziridine
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
-
- 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
- A61K47/551—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 one of the codrug's components being a vitamin, e.g. niacinamide, vitamin B3, cobalamin, vitamin B12, folate, vitamin A or retinoic acid
-
- 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
- A61K47/62—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 a protein, peptide or polyamino acid
- A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
-
- 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)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
Abstract
REFERIDA A UN COMPUESTO AZIRIDINIL-EPOTILONA DE FORMULA (X), DONDE K ES O, S O NR7; A ES -(CR8R9)-(CH2)m-Z-; Z ES (CHR10), C(=O), -OC(=O), ENTRE OTROS; B1 ES OH O CIANO Y R1 ES HIDROGENO O B1 Y R1 JUNTOS FORMAN UN ENLACE DOBLE; R2, R3 Y R5 SON H, ALQUILO, ARILO, ENTRE OTROS; R4 ES H, ALQUILO, ALQUENILO, ENTRE OTROS; R6 ES H, ALQUILO O ALQUILO SUSTITUIDO; R12 ES H, ALQUILO, ALQUILO SUSTITUIDO O HALOGENO; R13 ES ARILO, HETEROARILO, ENTRE OTROS; m ES UN ENTERO DE 0 A 6. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON UTILES EN EL TRATAMIENTO DE CANCERES, EN ESPECIAL AQUELLOS RELACIONADOS CON LA EXPRESION DEL RECEPTOR DE FOLATO
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US80836606P | 2006-05-25 | 2006-05-25 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20080316A1 true PE20080316A1 (es) | 2008-04-10 |
Family
ID=38561739
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2007000648A PE20080316A1 (es) | 2006-05-25 | 2007-05-24 | Compuestos de aziridinil-epotilona |
Country Status (20)
| Country | Link |
|---|---|
| US (2) | US7872145B2 (es) |
| EP (1) | EP2041140B1 (es) |
| JP (1) | JP5249929B2 (es) |
| KR (1) | KR101413955B1 (es) |
| CN (1) | CN101495482B (es) |
| AR (1) | AR061181A1 (es) |
| AT (1) | ATE524477T1 (es) |
| AU (1) | AU2007267535B2 (es) |
| BR (1) | BRPI0712167A2 (es) |
| CA (1) | CA2655668C (es) |
| EA (1) | EA014872B1 (es) |
| ES (1) | ES2371111T3 (es) |
| IL (1) | IL195236A (es) |
| MX (1) | MX2008014735A (es) |
| NO (1) | NO20084742L (es) |
| NZ (1) | NZ572763A (es) |
| PE (1) | PE20080316A1 (es) |
| TW (1) | TWI383985B (es) |
| WO (1) | WO2007140297A2 (es) |
| ZA (1) | ZA200810022B (es) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2010528115A (ja) * | 2007-05-25 | 2010-08-19 | ブリストル−マイヤーズ スクイブ カンパニー | エポチロン化合物およびアナログの製造方法 |
| EA035193B1 (ru) | 2010-05-18 | 2020-05-14 | Серулин Фарма Инк. | Композиции и способы лечения аутоиммунных и других заболеваний |
| EP3647322B1 (en) | 2014-03-20 | 2021-10-20 | Bristol-Myers Squibb Company | Stabilized fibronectin based scaffold molecules |
| SMT202000579T1 (it) | 2014-11-21 | 2020-11-10 | Bristol Myers Squibb Co | Anticorpi comprendenti regioni costanti pesanti modificate |
| MX383868B (es) | 2014-11-21 | 2025-03-14 | Bristol Myers Squibb Co | Anticuerpos contra cd73 y sus usos. |
| EP3702367B1 (en) | 2014-11-25 | 2024-05-15 | Bristol-Myers Squibb Company | Novel pd-l1 binding polypeptides for imaging |
| CN107406496A (zh) | 2015-03-10 | 2017-11-28 | 百时美施贵宝公司 | 可通过转谷氨酰胺酶缀合的抗体和由其制备的缀合物 |
| HRP20230060T1 (hr) | 2015-05-29 | 2023-03-17 | Bristol-Myers Squibb Company | Antitijela protiv ox40 i njihova primjena |
| US10584160B2 (en) | 2015-09-23 | 2020-03-10 | Bristol-Myers Squibb Company | Glypican-3-binding fibronectin based scaffold molecules |
| CN108430996A (zh) * | 2015-10-16 | 2018-08-21 | 威廉马歇莱思大学 | 埃博霉素类似物、合成方法、治疗方法及其药物缀合物 |
| CN108431034A (zh) | 2015-12-21 | 2018-08-21 | 百时美施贵宝公司 | 用于位点-特异性缀合的变体抗体 |
| JP2019514844A (ja) | 2016-03-04 | 2019-06-06 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | 抗ｃｄ７３抗体を用いた併用療法 |
| WO2018048975A1 (en) | 2016-09-09 | 2018-03-15 | Bristol-Myers Squibb Company | Use of an anti-pd-1 antibody in combination with an anti-mesothelin antibody in cancer treatment |
| KR102085798B1 (ko) | 2016-12-28 | 2020-03-06 | 주식회사 인투셀 | 베타-갈락토사이드가 도입된 자가-희생 기를 포함하는 화합물 |
| EP4098662A1 (en) | 2017-05-25 | 2022-12-07 | Bristol-Myers Squibb Company | Antibodies comprising modified heavy constant regions |
| EP3887397A1 (en) | 2018-11-28 | 2021-10-06 | Bristol-Myers Squibb Company | Antibodies comprising modified heavy constant regions |
| PL3886914T3 (pl) | 2018-11-30 | 2023-05-08 | Bristol-Myers Squibb Company | Przeciwciało zawierające c-końcowe rozszerzenie łańcucha lekkiego zawierające glutaminę, jego koniugaty oraz metody i zastosowania |
| JP7514836B2 (ja) | 2018-12-12 | 2024-07-11 | ブリストル－マイヤーズ スクイブ カンパニー | トランスグルタミナーゼによるコンジュゲーションのための改変抗体、ならびにそのコンジュゲート、方法および用途 |
| CN110563730B (zh) * | 2019-07-29 | 2022-03-25 | 江苏理工学院 | 高纯度n10-三氟乙酰蝶酸的制备方法 |
| WO2021055306A1 (en) | 2019-09-16 | 2021-03-25 | Bristol-Myers Squibb Company | Dual capture method for analysis of antibody-drug conjugates |
| WO2022013225A1 (en) | 2020-07-13 | 2022-01-20 | Precirix N.V. | Antibody fragment against folr1 |
| EP4079327A1 (en) * | 2021-04-22 | 2022-10-26 | Centaurus Polytherapeutics | Payloads for drug-conjugates and their use for treating cancer |
| WO2023203135A1 (en) | 2022-04-22 | 2023-10-26 | Precirix N.V. | Improved radiolabelled antibody |
| EP4518911A1 (en) | 2022-05-02 | 2025-03-12 | Precirix N.V. | Pre-targeting |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5108921A (en) | 1989-04-03 | 1992-04-28 | Purdue Research Foundation | Method for enhanced transmembrane transport of exogenous molecules |
| AU1095799A (en) | 1997-10-17 | 1999-05-10 | Philip L. Fuchs | Folic acid derivatives |
| US6380395B1 (en) * | 1998-04-21 | 2002-04-30 | Bristol-Myers Squibb Company | 12, 13-cyclopropane epothilone derivatives |
| US6291684B1 (en) | 1999-03-29 | 2001-09-18 | Bristol-Myers Squibb Company | Process for the preparation of aziridinyl epothilones from oxiranyl epothilones |
| AUPQ014799A0 (en) | 1999-05-04 | 1999-05-27 | Access Pharmaceuticals Australia Pty Limited | Amplification of folate-mediated targeting to tumor cells using polymers |
| JP2004532888A (ja) | 2001-06-01 | 2004-10-28 | ブリストル−マイヤーズ スクイブ カンパニー | エポチロン誘導体 |
| IL166039A0 (en) | 2002-07-31 | 2006-01-15 | Schering Ag | New effector conjugates process for their production and their pharmaceutical use |
| WO2004054622A1 (en) | 2002-12-13 | 2004-07-01 | Immunomedics, Inc. | Immunoconjugates with an intracellularly-cleavable linkage |
| TWI492750B (zh) * | 2003-01-27 | 2015-07-21 | 安德賽特公司 | 維生素-受體結合性藥物輸送共軛物、醫藥組合物、用途及製備方法 |
| DE602005003453T2 (de) | 2004-01-30 | 2008-09-25 | Bayer Schering Pharma Aktiengesellschaft | Neue effektor-konjugate, verfahren zu ihrer herstellung und ihre pharmazeutische verwendung |
| US20090004118A1 (en) | 2004-10-07 | 2009-01-01 | Shuming Nie | Multifunctional Nanoparticle Conjugates And Their Use |
-
2007
- 2007-05-24 PE PE2007000648A patent/PE20080316A1/es not_active Application Discontinuation
- 2007-05-24 AR ARP070102263A patent/AR061181A1/es not_active Application Discontinuation
- 2007-05-25 MX MX2008014735A patent/MX2008014735A/es active IP Right Grant
- 2007-05-25 NZ NZ572763A patent/NZ572763A/en not_active IP Right Cessation
- 2007-05-25 TW TW096118882A patent/TWI383985B/zh not_active IP Right Cessation
- 2007-05-25 CA CA2655668A patent/CA2655668C/en not_active Expired - Fee Related
- 2007-05-25 WO PCT/US2007/069736 patent/WO2007140297A2/en not_active Ceased
- 2007-05-25 JP JP2009512317A patent/JP5249929B2/ja not_active Expired - Fee Related
- 2007-05-25 BR BRPI0712167-9A patent/BRPI0712167A2/pt not_active IP Right Cessation
- 2007-05-25 AT AT07762325T patent/ATE524477T1/de not_active IP Right Cessation
- 2007-05-25 KR KR1020087031405A patent/KR101413955B1/ko not_active Expired - Fee Related
- 2007-05-25 EA EA200802389A patent/EA014872B1/ru not_active IP Right Cessation
- 2007-05-25 ES ES07762325T patent/ES2371111T3/es active Active
- 2007-05-25 CN CN200780028309XA patent/CN101495482B/zh not_active Expired - Fee Related
- 2007-05-25 US US11/753,785 patent/US7872145B2/en not_active Ceased
- 2007-05-25 EP EP07762325A patent/EP2041140B1/en active Active
- 2007-05-25 AU AU2007267535A patent/AU2007267535B2/en not_active Ceased
-
2008
- 2008-11-10 NO NO20084742A patent/NO20084742L/no not_active Application Discontinuation
- 2008-11-11 IL IL195236A patent/IL195236A/en not_active IP Right Cessation
- 2008-11-25 ZA ZA2008/10022A patent/ZA200810022B/en unknown
-
2011
- 2011-04-18 US US13/089,067 patent/USRE42930E1/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| KR20090025266A (ko) | 2009-03-10 |
| EP2041140B1 (en) | 2011-09-14 |
| EA014872B1 (ru) | 2011-02-28 |
| BRPI0712167A2 (pt) | 2012-08-28 |
| NO20084742L (no) | 2008-12-16 |
| JP2009538349A (ja) | 2009-11-05 |
| ES2371111T3 (es) | 2011-12-27 |
| US20070276018A1 (en) | 2007-11-29 |
| AU2007267535A8 (en) | 2011-06-09 |
| CN101495482B (zh) | 2012-05-02 |
| CA2655668A1 (en) | 2007-12-06 |
| EA200802389A1 (ru) | 2009-06-30 |
| HK1124335A1 (en) | 2009-07-10 |
| WO2007140297A2 (en) | 2007-12-06 |
| IL195236A (en) | 2012-12-31 |
| TWI383985B (zh) | 2013-02-01 |
| AR061181A1 (es) | 2008-08-13 |
| USRE42930E1 (en) | 2011-11-15 |
| JP5249929B2 (ja) | 2013-07-31 |
| KR101413955B1 (ko) | 2014-07-01 |
| CN101495482A (zh) | 2009-07-29 |
| AU2007267535B2 (en) | 2012-07-05 |
| WO2007140297A3 (en) | 2008-01-31 |
| IL195236A0 (en) | 2009-08-03 |
| MX2008014735A (es) | 2009-02-12 |
| ATE524477T1 (de) | 2011-09-15 |
| TW200815452A (en) | 2008-04-01 |
| EP2041140A2 (en) | 2009-04-01 |
| ZA200810022B (en) | 2011-05-25 |
| NZ572763A (en) | 2010-08-27 |
| CA2655668C (en) | 2013-02-26 |
| US7872145B2 (en) | 2011-01-18 |
| AU2007267535A1 (en) | 2007-12-06 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration | ||
| FD | Application declared void or lapsed |