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)
  • 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

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 (21)

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)
HK (1) HK1124335A1 (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
WO2008147941A1 (en) * 2007-05-25 2008-12-04 Bristol-Myers Squibb Company Processes for making epothilone compounds and analogs
EP3566719A1 (en) 2010-05-18 2019-11-13 Cerulean Pharma Inc. Compositions and methods for treatment of autoimmune and other diseases
AU2015231210B2 (en) 2014-03-20 2019-09-12 Bristol-Myers Squibb Company Stabilized fibronectin based scaffold molecules
ME03806B (me) 2014-11-21 2021-04-20 Bristol Myers Squibb Co Antitela protiv cd73 i njihova upotreba
CN107250157B (zh) 2014-11-21 2021-06-29 百时美施贵宝公司 包含修饰的重链恒定区的抗体
ES2822990T3 (es) 2014-11-25 2021-05-05 Bristol Myers Squibb Co Novedosos polipéptidos de unión a PD-L1 para obtención de imágenes
US10676773B2 (en) 2015-03-10 2020-06-09 Bristol-Myers Squibb Company Antibodies conjugatable by transglutaminase and conjugates made therefrom
US9644032B2 (en) 2015-05-29 2017-05-09 Bristol-Myers Squibb Company Antibodies against OX40 and uses thereof
KR20180057657A (ko) 2015-09-23 2018-05-30 브리스톨-마이어스 스큅 컴퍼니 글리피칸-3-결합 피브로넥틴 기반 스캐폴드 분자
EP3371176A4 (en) * 2015-10-16 2019-09-04 William Marsh Rice University EPOTHILONE ANALOGS, METHODS OF SYNTHESIS, METHODS OF TREATMENT, AND MEDICAMENT CONJUGATES THEREOF
BR112018012524A2 (pt) 2015-12-21 2018-12-11 Bristol Myers Squibb Co anticorpos variantes para conjugação sítio-específica
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
MX2019013132A (es) 2017-05-25 2020-01-27 Bristol Myers Squibb Co Anticuerpos que comprenden regiones constantes pesadas modificadas.
JP2022513653A (ja) 2018-11-28 2022-02-09 ブリストル－マイヤーズ スクイブ カンパニー 修飾された重鎖定常領域を含む抗体
EP3886914B1 (en) 2018-11-30 2023-03-29 Bristol-Myers Squibb Company Antibody comprising a glutamine-containing light chain c-terminal extension, conjugates thereof, and methods and uses
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
CA3185968A1 (en) 2020-07-13 2022-01-20 Tony Lahoutte 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)

* 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
AU1095799A (en) 1997-10-17 1999-05-10 Philip L. Fuchs 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
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
JP2006505627A (ja) 2002-07-31 2006-02-16 シエーリング アクチエンゲゼルシャフト 新規エフェクター接合体、それらの生成方法及びそれらの医薬使用
WO2004054622A1 (en) 2002-12-13 2004-07-01 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
AU2005294214A1 (en) 2004-10-07 2006-04-20 Emory University Multifunctional nanoparticles conjugates and their use

Also Published As

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

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