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NO20084742L - Aziridinyl-epotilonforbindelser - Google Patents

Aziridinyl-epotilonforbindelser

Info

Publication number
NO20084742L
NO20084742L NO20084742A NO20084742A NO20084742L NO 20084742 L NO20084742 L NO 20084742L NO 20084742 A NO20084742 A NO 20084742A NO 20084742 A NO20084742 A NO 20084742A NO 20084742 L NO20084742 L NO 20084742L
Authority
NO
Norway
Prior art keywords
substituted
aryl
alkyl
heteroaryl
hydrogen
Prior art date
Application number
NO20084742A
Other languages
English (en)
Inventor
Gregory D Vite
Soong-Hoon Kim
Christopher P Leamon
Iontcho R Vlahov
Original Assignee
Bristol Myers Squibb Co
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of NO20084742L publication Critical patent/NO20084742L/no

Links

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)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (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

Foreliggende oppfinnelse angår aziridinyl-epotilon-forbindelser som ytterligere beskrevet her og/eller farmasøytisk akseptable salter og/eller solvater derav som har formel (X), hvor K er -O-, -S- eller -NR7-; A er -(CR8R9)-(CH2)m-Z- hvor Z er -(CHR10)-, -C(=O)-, -C(=O)-C(=O)-, -OC(=O)-, -N(R11)C(=O)-, -SO2- eller -N(R11)SO2-; B1 er hydroksyl eller cyano og R1 er hydrogen eller B1 og R1 er tatt sammen for å danne en dobbeltbinding; R2, R3 og R5 er uavhengig hydrogen, alkyl, substituert alkyl, aryl eller substituert aryl; eller R2 og R3 kan være tatt sammen med karbonet som de er bundet til for å danne eventuelt substituert cykloalkyl; R4 er hydrogen, alkyl, alkenyl, substituert alkyl, substituert alkenyl, aryl eller substituert aryl; R6 er hydrogen, alkyl eller substituert alkyl; R7, R8, R9, R10, R11 og R12 er uavhengig hydrogen, alkyl, substituert alkyl, cykloalkyl, substituert cykloalkyl, aryl, substituert aryl, heterocykloalkyl, substituert heterocykloalkyl, heteroaryl eller substituert heteroaryl; og R13 er aryl, substituert aryl, heteroaryl eller substituert heteroaryl.
NO20084742A 2006-05-25 2008-11-10 Aziridinyl-epotilonforbindelser NO20084742L (no)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US80836606P 2006-05-25 2006-05-25
PCT/US2007/069736 WO2007140297A2 (en) 2006-05-25 2007-05-25 Aziridinyl-epothilone compounds

Publications (1)

Publication Number Publication Date
NO20084742L true NO20084742L (no) 2008-12-16

Family

ID=38561739

Family Applications (1)

Application Number Title Priority Date Filing Date
NO20084742A NO20084742L (no) 2006-05-25 2008-11-10 Aziridinyl-epotilonforbindelser

Country Status (20)

Country Link
US (2) US7872145B2 (no)
EP (1) EP2041140B1 (no)
JP (1) JP5249929B2 (no)
KR (1) KR101413955B1 (no)
CN (1) CN101495482B (no)
AR (1) AR061181A1 (no)
AT (1) ATE524477T1 (no)
AU (1) AU2007267535B2 (no)
BR (1) BRPI0712167A2 (no)
CA (1) CA2655668C (no)
EA (1) EA014872B1 (no)
ES (1) ES2371111T3 (no)
IL (1) IL195236A (no)
MX (1) MX2008014735A (no)
NO (1) NO20084742L (no)
NZ (1) NZ572763A (no)
PE (1) PE20080316A1 (no)
TW (1) TWI383985B (no)
WO (1) WO2007140297A2 (no)
ZA (1) ZA200810022B (no)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8143415B2 (en) 2007-05-25 2012-03-27 Bristol-Myers Squibb Company Processes for making epothilone compounds and analogs
JP5881254B2 (ja) 2010-05-18 2016-03-09 セルリアン・ファーマ・インコーポレイテッド 自己免疫疾患およびその他の疾患の治療のための組成物および方法
US10450363B2 (en) 2014-03-20 2019-10-22 Bristol-Myers Squibb Company Stabilized fibronectin based scaffold molecules
SG10201913004UA (en) 2014-11-21 2020-03-30 Bristol Myers Squibb Co Antibodies against cd73 and uses thereof
PT3221346T (pt) 2014-11-21 2020-10-23 Bristol Myers Squibb Co Anticorpos compreendendo regiões constantes de cadeia pesada modificadas
EA037590B1 (ru) 2014-11-25 2021-04-19 Бристол-Майерс Сквибб Компани Связывающиеся с pd-l1 полипептиды на основе 10fn3 домена для визуализации
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
SI3303396T1 (sl) 2015-05-29 2023-01-31 Bristol-Myers Squibb Company Protitelesa proti OX40 in njihova uporaba
EP3733698A1 (en) 2015-09-23 2020-11-04 Bristol-Myers Squibb Company Glypican-3 binding fibronectin based scafflold molecules
WO2017066606A1 (en) * 2015-10-16 2017-04-20 William Marsh Rice University Epothilone analogs, methods of synthesis, methods of treatment, and drug conjugates thereof
KR20180089433A (ko) 2015-12-21 2018-08-08 브리스톨-마이어스 스큅 컴퍼니 부위-특이적 접합을 위한 변이체 항체
KR20230038311A (ko) 2016-03-04 2023-03-17 브리스톨-마이어스 스큅 컴퍼니 항-cd73 항체와의 조합 요법
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
EP4098662A1 (en) 2017-05-25 2022-12-07 Bristol-Myers Squibb Company Antibodies comprising modified heavy constant regions
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
SG11202105565UA (en) 2018-11-30 2021-06-29 Bristol Myers Squibb Co Antibody comprising a glutamine-containing light chain c-terminal extension, conjugates thereof, and methods and uses
US12478686B2 (en) 2018-12-12 2025-11-25 Bristol-Myers Squibb Company Antibodies modified for transglutaminase conjugation, conjugates thereof, and methods and uses
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
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
KR20250034289A (ko) 2022-05-02 2025-03-11 프리시릭스 엔.브이. 사전 표적화

Family Cites Families (11)

* Cited by examiner, † Cited by third party
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
US6291673B1 (en) * 1997-10-17 2001-09-18 Purdue Research Foundation Folic acid derivatives
US6399638B1 (en) * 1998-04-21 2002-06-04 Bristol-Myers Squibb Company 12,13-modified 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
US6800653B2 (en) * 2001-06-01 2004-10-05 Bristol-Myers Squibb Compnay Epothilone derivatives
KR20050026033A (ko) 2002-07-31 2005-03-14 쉐링 악티엔게젤샤프트 신규 효과기 접합체, 그의 제조 방법 및 그의 약학적 용도
CA2508831C (en) 2002-12-13 2012-05-01 Immunomedics, Inc. Immunoconjugates with an intracellularly-cleavable linkage
WO2004069159A2 (en) * 2003-01-27 2004-08-19 Endocyte, Inc. Vitamin receptor binding drug delivery conjugates
SI1718340T1 (sl) 2004-01-30 2008-04-30 Bayer Schering Pharma Ag Novi efektorski konjugati, postopek za njihovo proizvodnjo in njihova farmacevtska uporaba
WO2006042146A2 (en) 2004-10-07 2006-04-20 Emory University Multifunctional nanoparticles conjugates and their use

Also Published As

Publication number Publication date
EA200802389A1 (ru) 2009-06-30
KR20090025266A (ko) 2009-03-10
AU2007267535A1 (en) 2007-12-06
ES2371111T3 (es) 2011-12-27
CN101495482B (zh) 2012-05-02
BRPI0712167A2 (pt) 2012-08-28
CA2655668A1 (en) 2007-12-06
KR101413955B1 (ko) 2014-07-01
ATE524477T1 (de) 2011-09-15
US7872145B2 (en) 2011-01-18
CA2655668C (en) 2013-02-26
PE20080316A1 (es) 2008-04-10
EP2041140B1 (en) 2011-09-14
EA014872B1 (ru) 2011-02-28
US20070276018A1 (en) 2007-11-29
CN101495482A (zh) 2009-07-29
ZA200810022B (en) 2011-05-25
MX2008014735A (es) 2009-02-12
AU2007267535A8 (en) 2011-06-09
JP5249929B2 (ja) 2013-07-31
HK1124335A1 (en) 2009-07-10
JP2009538349A (ja) 2009-11-05
AR061181A1 (es) 2008-08-13
NZ572763A (en) 2010-08-27
IL195236A (en) 2012-12-31
TW200815452A (en) 2008-04-01
WO2007140297A2 (en) 2007-12-06
TWI383985B (zh) 2013-02-01
IL195236A0 (en) 2009-08-03
WO2007140297A3 (en) 2008-01-31
USRE42930E1 (en) 2011-11-15
EP2041140A2 (en) 2009-04-01
AU2007267535B2 (en) 2012-07-05

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