[go: up one dir, main page]

AR061181A1 - Compuestos de aziridinil-epotilona - Google Patents

Compuestos de aziridinil-epotilona

Info

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
Application number
ARP070102263A
Other languages
English (en)
Inventor
Gregory D Vite
Christopher P Leamon
Iontcho Viahov
Soong-Hoon Kim
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 AR061181A1 publication Critical patent/AR061181A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/396Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having three-membered rings, e.g. aziridine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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
    • A61K47/55Medicinal 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
    • A61K47/551Medicinal 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/62Medicinal 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
    • A61K47/65Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic 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.
ARP070102263A 2006-05-25 2007-05-24 Compuestos de aziridinil-epotilona AR061181A1 (es)

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)

* Cited by examiner, † Cited by third party
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)

* 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
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

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

Similar Documents

Publication Publication Date Title
AR061181A1 (es) Compuestos de aziridinil-epotilona
PA8783601A1 (es) Derivados de piperidina/piperazina
CY1119049T1 (el) Υποκατεστημενα πυρρολιδινο-2-καρβοξαμιδια
CY1114932T1 (el) Αντιπαρασιτικοι παραγοντες
AR076171A1 (es) Pirazolopirimidinonas 1,6-disustituidas, composiciones farmaceuticas que las contienen y uso de las mismas para el tratamiento del alzheimer, epilepsia y otras enfermedades del sistema nervioso central.
HRP20120323T1 (en) Diarylhydantoin compounds
CO6160237A2 (es) Pirazinonas y pirazinoles sustituidos y composiciones que los comprenden
CY1108744T1 (el) 2-οξο-1,2,4,5-τετραϋδρo-1,3-βενζοδιαζεπιν-3-υλ-πιπεριδινες ως ανταγωνιστες της cgrp
AR109958A1 (es) Lactamas bicíclicas de piridona y sus métodos de uso
ECSP055974A (es) Síntesis de cloruros de 4 amino-2-butenoil y su uso en la preparación de 3-ciano quinolinas
PE20130375A1 (es) Compuestos de triazolopiridinas y triazolopirazinas inhibidores de c-met y composiciones de los mismos
AR061739A1 (es) Nuevos derivados naftalenicos, su procedimiento de preparacion y las composiciones farmaceuticas que los contienen
CY1113395T1 (el) Σταθερη φαρμακευτικη συνθεση που περιεχει πυριμιδινη-σουλφαμιδη
PE20080102A1 (es) Conjugados de analogos de aziridinil-epotilona y composiciones farmaceuticas que comprenden los mismos
CY1109441T1 (el) Ενδιαμεσα προϊοντα για την παραγωγη διοξανιου-2-αλκυλκαρβαμικου
AR069796A1 (es) Derivados de bencimidazol, sustituido por carboxilo o por hidroxilo, proceso para prepararlos y composiciones farmaceuticas que los contienen
ECSP12012161A (es) Compuestos en calidad de antagonistas de Bradiquinina-b1
AR045805A1 (es) Quinolonas y naftridonas 7- amino alquidenil - heterociclicas
ATE478054T1 (de) Benzimidazolderivate
UY28848A1 (es) Antagonistas de cgrp seleccionados, procedimientos para su preparación, y su empleo como medicamentos
CO5601021A2 (es) Derivados de quinazolinona, composiciones farmaceuticas que los contienen y su proceso de preparacion y su uso como antagonistas cb
UY29169A1 (es) Derivados de 2-amido-4 feniltiazol, su preparacion y su aplicacion en terapeutica
AR056025A1 (es) Compuestos de imidazol sustituidos como inhibidores de ksp
AR064306A1 (es) Antagonistas del receptor de angiotensina ii
AR075586A1 (es) Proceso, purificacion y cristalizacion de 1-(4-{[4-(dimetilamino)piperidin-1-il]carbonil}fenil)-3-[4-(4,6-dimorfolin-4-il-1,3,5-triazin-2-il)fenil]urea, inhibidor de pi3k/mtor

Legal Events

Date Code Title Description
FG Grant, registration
FD Application declared void or lapsed, e.g., due to non-payment of fee