AR061181A1 - Compuestos de aziridinil-epotilona - Google Patents
Compuestos de aziridinil-epotilonaInfo
- Publication number
- AR061181A1 AR061181A1 ARP070102263A ARP070102263A AR061181A1 AR 061181 A1 AR061181 A1 AR 061181A1 AR P070102263 A ARP070102263 A AR P070102263A AR P070102263 A ARP070102263 A AR P070102263A AR 061181 A1 AR061181 A1 AR 061181A1
- Authority
- AR
- Argentina
- Prior art keywords
- substituted
- alkyl
- aryl
- hydrogen
- heteroaryl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 5
- 125000003118 aryl group Chemical group 0.000 abstract 4
- 125000001072 heteroaryl group Chemical group 0.000 abstract 4
- 150000002431 hydrogen Chemical class 0.000 abstract 4
- 125000003107 substituted aryl group Chemical group 0.000 abstract 4
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 2
- 125000005346 substituted cycloalkyl group Chemical group 0.000 abstract 2
- 101100495911 Arabidopsis thaliana CHR10 gene Proteins 0.000 abstract 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000005017 substituted alkenyl group Chemical group 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)
- 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
Reivindicacion 1: Un compuesto caracterizado porque tiene la Formula (1) o sales farmacéuticamente aceptables de los mismos, en donde: K es -O-, -S-, o -NR7-; A es -(CR8R9)-(CH2)m-Z- en donde Z es -(CHR10)-, -C(=O)-, -C(=O)-C(=O)-, -OC(=O)-, - N(R11)C(=O)-, -SO2-, o -N(R11)SO2-; B1 es hidroxilo o ciano, y R1 es hidrogeno o B1 y R1 son tomados juntos para formar un enlace doble; R2, R3 y R5 son, independientemente, hidrogeno, alquilo, alquilo substituido, arilo o arilo substituido; o R2 y R3 pueden ser tomados juntos con el carbono al cual se enlazan para formar un cicloalquilo opcionalmente substituido; R4 es hidrogeno, alquilo, alquenilo, alquilo substituido, alquenilo substituido, arilo, o arilo substituido; R6 es hidrogeno, alquilo o alquilo substituido; R7, R8, R9, R10 y R11 son independientemente hidrogeno, alquilo, alquilo substituido, cicloalquilo, cicloalquilo substituido, arilo, arilo substituido, heterocicloalquilo, heterocicloalquilo substituido, heteroarilo, o heteroarilo substituido; R12 es H, alquilo, alquilo substituido, o halogeno; R13 es arilo, arilo substituido, heteroarilo o heteroarilo substituido; y m es 0 hasta 6.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US80836606P | 2006-05-25 | 2006-05-25 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR061181A1 true AR061181A1 (es) | 2008-08-13 |
Family
ID=38561739
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP070102263A AR061181A1 (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 |
|---|---|---|---|---|
| EP2152717A1 (en) | 2007-05-25 | 2010-02-17 | Bristol-Myers Squibb Company | Processes for making epothilone compounds and analogs |
| EP2571525A4 (en) | 2010-05-18 | 2016-04-27 | Cerulean Pharma Inc | Compositions and methods for treating autoimmune and other diseases |
| ES2898273T3 (es) | 2014-03-20 | 2022-03-04 | Bristol Myers Squibb Co | Moléculas con una estructura a base de fibronectina estabilizada |
| DK3221363T3 (da) | 2014-11-21 | 2020-08-10 | Bristol Myers Squibb Co | Antistoffer mod cd73 og anvendelser deraf |
| DK3221346T3 (da) | 2014-11-21 | 2020-10-12 | Bristol Myers Squibb Co | Antistoffer omfattende modificerede konstante områder af tungkæden |
| CA2969067A1 (en) | 2014-11-25 | 2016-06-02 | Bristol-Myers Squibb Company | Novel pd-l1 binding polypeptides for imaging |
| EP3268048B1 (en) | 2015-03-10 | 2019-05-08 | Bristol-Myers Squibb Company | Antibodies conjugatable by transglutaminase and conjugates made therefrom |
| DK3303396T5 (da) | 2015-05-29 | 2024-10-07 | Bristol Myers Squibb Co | Antistoffer mod ox40 og anvendelser deraf |
| CN108884147B (zh) | 2015-09-23 | 2024-02-27 | 百时美施贵宝公司 | 结合磷脂酰肌醇蛋白聚糖3的基于纤连蛋白的支架分子 |
| MA43178A (fr) * | 2015-10-16 | 2018-09-12 | Univ Rice William M | Analogues d'épothilone, procédés de synthèse, procédés de traitement, et conjugués médicamenteux de ceux-ci |
| EA201891482A1 (ru) | 2015-12-21 | 2018-12-28 | Бристол-Маерс Сквибб Компани | Модифицированные антитела для сайт-специфической конъюгации |
| IL295230A (en) | 2016-03-04 | 2022-10-01 | Bristol Myers Squibb Co | Combination therapy with anti-cd73 antibodies |
| 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 |
| CN110719915A (zh) | 2017-05-25 | 2020-01-21 | 百时美施贵宝公司 | 包含经修饰的重链恒定区的抗体 |
| CN113348177A (zh) | 2018-11-28 | 2021-09-03 | 百时美施贵宝公司 | 包含经修饰的重链恒定区的抗体 |
| ES2943474T3 (es) | 2018-11-30 | 2023-06-13 | Bristol Myers Squibb Co | Anticuerpo que comprende una extensión carboxiterminal de una cadena ligera que contiene glutamina, conjugados del mismo, y métodos y usos |
| CN113544155A (zh) | 2018-12-12 | 2021-10-22 | 百时美施贵宝公司 | 经修饰用于转谷氨酰胺酶缀合的抗体、其缀合物以及方法和用途 |
| 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 |
| 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 |
| WO2023213801A1 (en) | 2022-05-02 | 2023-11-09 | 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 |
| EP1392664A4 (en) * | 2001-06-01 | 2005-01-26 | Bristol Myers Squibb Co | EPOTHILONE DERIVATIVES |
| US7585491B2 (en) | 2002-12-13 | 2009-09-08 | Immunomedics, Inc. | Immunoconjugates with an intracellularly-cleavable linkage |
| PL374528A1 (en) | 2002-07-31 | 2005-10-31 | Schering Aktiengesellschaft | New effector conjugates, process for their production and their pharmaceutical use |
| CA2512867C (en) * | 2003-01-27 | 2014-08-26 | Endocyte, Inc. | Vitamin receptor binding drug delivery conjugates |
| PL1718340T3 (pl) | 2004-01-30 | 2008-04-30 | Bayer Schering Pharma Ag | Nowe koniugaty efektorowe, sposób ich wytwarzania i ich zastosowanie farmaceutyczne |
| CA2583389A1 (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 AU AU2007267535A patent/AU2007267535B2/en not_active Ceased
- 2007-05-25 NZ NZ572763A patent/NZ572763A/en not_active IP Right Cessation
- 2007-05-25 EP EP07762325A patent/EP2041140B1/en active Active
- 2007-05-25 CN CN200780028309XA patent/CN101495482B/zh not_active Expired - Fee Related
- 2007-05-25 MX MX2008014735A patent/MX2008014735A/es active IP Right Grant
- 2007-05-25 CA CA2655668A patent/CA2655668C/en not_active Expired - Fee Related
- 2007-05-25 TW TW096118882A patent/TWI383985B/zh not_active IP Right Cessation
- 2007-05-25 AT AT07762325T patent/ATE524477T1/de not_active IP Right Cessation
- 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 KR KR1020087031405A patent/KR101413955B1/ko not_active Expired - Fee Related
- 2007-05-25 US US11/753,785 patent/US7872145B2/en not_active Ceased
- 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 BR BRPI0712167-9A patent/BRPI0712167A2/pt not_active IP Right Cessation
-
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 |
|---|---|
| AU2007267535B2 (en) | 2012-07-05 |
| MX2008014735A (es) | 2009-02-12 |
| CA2655668C (en) | 2013-02-26 |
| IL195236A (en) | 2012-12-31 |
| EP2041140A2 (en) | 2009-04-01 |
| NO20084742L (no) | 2008-12-16 |
| WO2007140297A3 (en) | 2008-01-31 |
| CN101495482B (zh) | 2012-05-02 |
| TW200815452A (en) | 2008-04-01 |
| TWI383985B (zh) | 2013-02-01 |
| NZ572763A (en) | 2010-08-27 |
| AU2007267535A1 (en) | 2007-12-06 |
| PE20080316A1 (es) | 2008-04-10 |
| USRE42930E1 (en) | 2011-11-15 |
| KR20090025266A (ko) | 2009-03-10 |
| ES2371111T3 (es) | 2011-12-27 |
| EA200802389A1 (ru) | 2009-06-30 |
| CN101495482A (zh) | 2009-07-29 |
| IL195236A0 (en) | 2009-08-03 |
| AU2007267535A8 (en) | 2011-06-09 |
| US7872145B2 (en) | 2011-01-18 |
| ZA200810022B (en) | 2011-05-25 |
| US20070276018A1 (en) | 2007-11-29 |
| JP2009538349A (ja) | 2009-11-05 |
| CA2655668A1 (en) | 2007-12-06 |
| JP5249929B2 (ja) | 2013-07-31 |
| ATE524477T1 (de) | 2011-09-15 |
| EA014872B1 (ru) | 2011-02-28 |
| EP2041140B1 (en) | 2011-09-14 |
| WO2007140297A2 (en) | 2007-12-06 |
| KR101413955B1 (ko) | 2014-07-01 |
| BRPI0712167A2 (pt) | 2012-08-28 |
| HK1124335A1 (en) | 2009-07-10 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration | ||
| FD | Application declared void or lapsed, e.g., due to non-payment of fee |