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)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Peptides Or Proteins (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (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 (21)
| 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) |
| HK (1) | HK1124335A1 (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 |
| EP3119803B1 (en) | 2014-03-20 | 2019-09-11 | Bristol-Myers Squibb Company | Stabilized fibronectin based scaffold molecules |
| DK3221346T3 (da) | 2014-11-21 | 2020-10-12 | Bristol Myers Squibb Co | Antistoffer omfattende modificerede konstante områder af tungkæden |
| HUE050596T2 (hu) | 2014-11-21 | 2020-12-28 | Bristol Myers Squibb Co | Antitestek CD73 ellen és azok felhasználásai |
| 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 |
| TWI732760B (zh) | 2015-05-29 | 2021-07-11 | 美商必治妥美雅史谷比公司 | 抗ｏｘ４０抗體及其用途 |
| WO2017053619A1 (en) | 2015-09-23 | 2017-03-30 | Bristrol-Myers Squibb Company | Glypican-3binding fibronectin based scafflold molecules |
| EP3371176A4 (en) * | 2015-10-16 | 2019-09-04 | William Marsh Rice University | EPOTHILON ANALOGUE, SYNTHESIS METHOD, TREATMENT METHOD AND MEDICAMENT CONJUGATE THEREFOR |
| US20180362619A1 (en) | 2015-12-21 | 2018-12-20 | Bristol-Myers Squibb Company | Variant antibodies for site-specific conjugation |
| 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 |
| US20190218294A1 (en) | 2016-09-09 | 2019-07-18 | 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 |
| WO2018218056A1 (en) | 2017-05-25 | 2018-11-29 | Birstol-Myers Squibb Company | Antibodies comprising modified heavy constant regions |
| US20220106400A1 (en) | 2018-11-28 | 2022-04-07 | Bristol-Myers Squibb Company | Antibodies comprising modified heavy constant regions |
| SI3886914T1 (sl) | 2018-11-30 | 2023-06-30 | Bristol-Myers Squibb Company | Protitelo, ki vsebuje C-terminalni podaljšek lahke verige, ki vsebuje glutamin, njegove konjugate ter metode in uporabe |
| KR20210102334A (ko) | 2018-12-12 | 2021-08-19 | 브리스톨-마이어스 스큅 컴퍼니 | 트랜스글루타미나제 접합을 위해 변형된 항체, 그의 접합체, 및 방법 및 용도 |
| 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 |
| US20240377413A1 (en) | 2019-09-16 | 2024-11-14 | Bristol-Myers Squibb Company | Dual capture method for analysis of antibody-drug conjugates |
| EP4178982A1 (en) | 2020-07-13 | 2023-05-17 | 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 |
| CN119584994A (zh) | 2022-05-02 | 2025-03-07 | 普雷西里克斯公司 | 预靶向 |
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 |
| MXPA03010909A (es) * | 2001-06-01 | 2004-02-17 | Bristol Myers Squibb Co | Derivados de epotilona. |
| WO2004012735A2 (en) | 2002-07-31 | 2004-02-12 | Schering Ag | New effector conjugates, process for their production and their pharmaceutical use |
| AU2003288467A1 (en) | 2002-12-13 | 2004-07-09 | Immunomedics, Inc. | Immunoconjugates with an intracellularly-cleavable linkage |
| EP2517730A3 (en) * | 2003-01-27 | 2013-01-02 | Endocyte, Inc. | Vitamin receptor binding drug delivery conjugates |
| DE602005003453T2 (de) | 2004-01-30 | 2008-09-25 | Bayer Schering Pharma Aktiengesellschaft | Neue effektor-konjugate, verfahren zu ihrer herstellung und ihre pharmazeutische verwendung |
| WO2006042146A2 (en) | 2004-10-07 | 2006-04-20 | Emory University | Multifunctional nanoparticles 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 AT AT07762325T patent/ATE524477T1/de not_active IP Right Cessation
- 2007-05-25 JP JP2009512317A patent/JP5249929B2/ja not_active Expired - Fee Related
- 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 US US11/753,785 patent/US7872145B2/en not_active Ceased
- 2007-05-25 ES ES07762325T patent/ES2371111T3/es active Active
- 2007-05-25 EP EP07762325A patent/EP2041140B1/en active Active
- 2007-05-25 MX MX2008014735A patent/MX2008014735A/es active IP Right Grant
- 2007-05-25 EA EA200802389A patent/EA014872B1/ru not_active IP Right Cessation
- 2007-05-25 AU AU2007267535A patent/AU2007267535B2/en not_active Ceased
- 2007-05-25 CN CN200780028309XA patent/CN101495482B/zh not_active Expired - Fee Related
- 2007-05-25 BR BRPI0712167-9A patent/BRPI0712167A2/pt not_active IP Right Cessation
- 2007-05-25 KR KR1020087031405A patent/KR101413955B1/ko not_active Expired - Fee Related
- 2007-05-25 WO PCT/US2007/069736 patent/WO2007140297A2/en active Application Filing
- 2007-05-25 CA CA2655668A patent/CA2655668C/en not_active Expired - Fee Related
-
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
-
2009
- 2009-04-23 HK HK09103805.0A patent/HK1124335A1/xx not_active IP Right Cessation
-
2011
- 2011-04-18 US US13/089,067 patent/USRE42930E1/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| AR061181A1 (es) | 2008-08-13 |
| JP2009538349A (ja) | 2009-11-05 |
| AU2007267535B2 (en) | 2012-07-05 |
| KR20090025266A (ko) | 2009-03-10 |
| USRE42930E1 (en) | 2011-11-15 |
| ATE524477T1 (de) | 2011-09-15 |
| IL195236A0 (en) | 2009-08-03 |
| EA200802389A1 (ru) | 2009-06-30 |
| US20070276018A1 (en) | 2007-11-29 |
| US7872145B2 (en) | 2011-01-18 |
| AU2007267535A1 (en) | 2007-12-06 |
| NO20084742L (no) | 2008-12-16 |
| CN101495482A (zh) | 2009-07-29 |
| TWI383985B (zh) | 2013-02-01 |
| CA2655668C (en) | 2013-02-26 |
| WO2007140297A3 (en) | 2008-01-31 |
| KR101413955B1 (ko) | 2014-07-01 |
| HK1124335A1 (en) | 2009-07-10 |
| EA014872B1 (ru) | 2011-02-28 |
| ZA200810022B (en) | 2011-05-25 |
| JP5249929B2 (ja) | 2013-07-31 |
| NZ572763A (en) | 2010-08-27 |
| AU2007267535A8 (en) | 2011-06-09 |
| CN101495482B (zh) | 2012-05-02 |
| IL195236A (en) | 2012-12-31 |
| TW200815452A (en) | 2008-04-01 |
| BRPI0712167A2 (pt) | 2012-08-28 |
| MX2008014735A (es) | 2009-02-12 |
| CA2655668A1 (en) | 2007-12-06 |
| EP2041140A2 (en) | 2009-04-01 |
| EP2041140B1 (en) | 2011-09-14 |
| WO2007140297A2 (en) | 2007-12-06 |
| ES2371111T3 (es) | 2011-12-27 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration | ||
| FD | Application declared void or lapsed |