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PE20080102A1 - Conjugados de analogos de aziridinil-epotilona y composiciones farmaceuticas que comprenden los mismos - Google Patents

Conjugados de analogos de aziridinil-epotilona y composiciones farmaceuticas que comprenden los mismos

Info

Publication number
PE20080102A1
PE20080102A1 PE2007000649A PE2007000649A PE20080102A1 PE 20080102 A1 PE20080102 A1 PE 20080102A1 PE 2007000649 A PE2007000649 A PE 2007000649A PE 2007000649 A PE2007000649 A PE 2007000649A PE 20080102 A1 PE20080102 A1 PE 20080102A1
Authority
PE
Peru
Prior art keywords
alkyl
carboxi
ilamino
cycloalkyl
epotilone
Prior art date
Application number
PE2007000649A
Other languages
English (en)
Inventor
Gregory D Vite
Francis Y Lee
Christopher P Leamon
Iontcho Vlahov
Original Assignee
Bristol Myers Squibb Co
Endocyte Inc
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, Endocyte Inc filed Critical Bristol Myers Squibb Co
Publication of PE20080102A1 publication Critical patent/PE20080102A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)

Abstract

SE REFIERE A COMPUESTOS CONJUGADOS DE ANALOGOS DE AZIRIDINIL-EPOTILONA DE FORMULA (I) DONDE V ES UN FOLATO; Q ES O, S O NR7; M ES UN LIGADOR QUE SE LIBERA; K ES O, S O NR7a; A ES -(CR8R9)-(CH2)m-Z- EN DONDE Z ES -(CHR10)-, C(=O), SO2, ENTRE OTROS, DONDE R7a, R7, R8, R9 Y R10 SON CADA UNO H, ALQUILO(C1-C10), CICLOALQUILO(C3-C7), ENTRE OTROS; m ES DE 0 A 6; B1 ES OH O CN; R1 ES H O R1 Y B1 SE TOMAN JUNTOS PARA FORMAR UN DOBLE ENLACE; R2, R3 Y R5 SON CADA UNO H, ALQUILO(C1-C10), ARILO, ENTRE OTROS; R4 ES H, ALQUILO(C1-C10), ENTRE OTROS; R6 ES H O ALQUILO(C1-C10); R12 ES H, HALOGENO O ALQUILO(C1-C10); R13 ES ARILO O HETEROARILO; T ES UN COMPUESTO DE FORMULA (i) DONDE R14 ES H, ALQUILO(C1-C10), CICLOALQUILO(C3-C7), ENTRE OTROS; q ES DE 1 A 10; R15, R16 Y R17 SON CADA UNO H, ALQUILO(C1-C4) OPCIONALMENTE SUSTITUIDO O R16 Y R17 SE TOMAN JUNTOS PARA FORMAR UN CICLOALQUILO(C3-C7). ES UN COMPUESTO PREFERIDO EL ACIDO (S)-2-(4-((2-AMINO-4-OXO-3,4-DIHIDROPTERIDIN-6-IL)METILAMINO)BENZAMIDO)-5-((S)-3-CARBOXI-1-((S)-1-((S)-3-CARBOXI-1-((R)-1-CARBOXI-2-(2-(2-((2-((1S,3S,7S,10R,11S,12S,16R)-7,11-DIHIDROXI-8,8,10,12-TETRAMETIL-3-((E)-1-(2-METILTIAZOL-4-IL)PROP-1-EN-2-IL)-5,9-DIOXO-4-OXA-17-AZA-BICICLO[14.1.0]HEPTADECAN-17-IL)ETOXI)CARBONILOXI)ETIL)DISULFANIL)ETILAMINO)-1-OXOPROPAN-2-ILAMINO)-5-GUANIDINO-1-OXOPENTAN-2-ILAMINO)-1-OXOPROPAN-2-ILAMINO)-5-OXOPENTANOICO. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON UTILES EN EL TRATAMIENTO DE CANCER
PE2007000649A 2006-05-25 2007-05-24 Conjugados de analogos de aziridinil-epotilona y composiciones farmaceuticas que comprenden los mismos PE20080102A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US80836706P 2006-05-25 2006-05-25

Publications (1)

Publication Number Publication Date
PE20080102A1 true PE20080102A1 (es) 2008-02-11

Family

ID=38461157

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2007000649A PE20080102A1 (es) 2006-05-25 2007-05-24 Conjugados de analogos de aziridinil-epotilona y composiciones farmaceuticas que comprenden los mismos

Country Status (16)

Country Link
US (1) US20070275904A1 (es)
EP (1) EP2023960A1 (es)
JP (1) JP2009538350A (es)
KR (1) KR20090025267A (es)
CN (1) CN101495154A (es)
AR (1) AR062448A1 (es)
AU (1) AU2007267536A1 (es)
BR (1) BRPI0712165A2 (es)
CA (1) CA2657276A1 (es)
EA (1) EA200802390A1 (es)
IL (1) IL195237A0 (es)
MX (1) MX2008014788A (es)
NO (1) NO20084752L (es)
PE (1) PE20080102A1 (es)
TW (1) TW200813065A (es)
WO (1) WO2007140298A1 (es)

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EP1389209B1 (en) * 2001-04-24 2009-04-08 Purdue Research Foundation Folate mimetics and folate-receptor binding conjugates thereof
US7910594B2 (en) * 2002-05-15 2011-03-22 Endocyte, Inc. Vitamin-mitomycin conjugates
TWI405573B (zh) 2003-01-27 2013-08-21 Endocyte Inc 維生素-受體結合性藥物輸送共軛物中間物及製備方法
EP1789391B1 (en) 2004-07-23 2017-06-28 Endocyte, Inc. Bivalent linkers and conjugates thereof
US8044200B2 (en) 2005-03-16 2011-10-25 Endocyte, Inc. Synthesis and purification of pteroic acid and conjugates thereof
CN103893779A (zh) 2005-08-19 2014-07-02 恩多塞特公司 多药物配体缀合物
WO2007022493A2 (en) * 2005-08-19 2007-02-22 Endocyte, Inc. Ligand conjugates of vinca alkaloids, analogs, and derivatives
WO2008101231A2 (en) * 2007-02-16 2008-08-21 Endocyte, Inc. Methods and compositions for treating and diagnosing kidney disease
EP2139523B1 (en) * 2007-03-14 2014-10-22 Endocyte, Inc. Conjugates of folate and tubulysin for targeted drug delivery
US8143415B2 (en) * 2007-05-25 2012-03-27 Bristol-Myers Squibb Company Processes for making epothilone compounds and analogs
RU2523909C2 (ru) * 2007-06-25 2014-07-27 Эндосайт, Инк. Конъюгаты, содержащие гидрофильные спейсеры линкеров
US9877965B2 (en) 2007-06-25 2018-01-30 Endocyte, Inc. Vitamin receptor drug delivery conjugates for treating inflammation
WO2009055562A1 (en) 2007-10-25 2009-04-30 Endocyte, Inc. Tubulysins and processes for preparing
BR112013026680A2 (pt) * 2011-08-15 2016-12-27 Univ City New York Res Found composto, método de tratamento de uma doença inflamatória e composição farmacêutica
US10080805B2 (en) 2012-02-24 2018-09-25 Purdue Research Foundation Cholecystokinin B receptor targeting for imaging and therapy
US20140080175A1 (en) 2012-03-29 2014-03-20 Endocyte, Inc. Processes for preparing tubulysin derivatives and conjugates thereof
JP2015536323A (ja) 2012-10-16 2015-12-21 エンドサイト・インコーポレイテッドＥｎｄｏｃｙｔｅ， Ｉｎｃ． 非天然アミノ酸を含む薬物送達結合体および使用方法
US20140154702A1 (en) * 2012-11-30 2014-06-05 Endocyte, Inc. Methods For Treating Cancer Using Combination Therapies
WO2014101134A1 (zh) * 2012-12-28 2014-07-03 Yan Wenguang 叶酸衍生物及其制备方法和应用
CN104784699B (zh) * 2014-01-20 2019-05-03 博瑞生物医药（苏州）股份有限公司 叶酸受体结合配体-药物偶联物
EA201691589A1 (ru) 2014-03-20 2017-02-28 Бристол-Маерс Сквибб Компани Стабилизированные основанные на фибронектине каркасные молекулы
HUE052526T2 (hu) 2014-11-21 2021-05-28 Bristol Myers Squibb Co Antitestek, amelyek tartalmaznak módosított nehéz konstans régiókat
TN2017000203A1 (en) 2014-11-21 2018-10-19 Bristol Myers Squibb Co Antibodies against cd73 and uses thereof
MX383917B (es) 2014-11-25 2025-03-14 Bristol Myers Squibb Co Nuevos péptidos que se unen al ligando-1 de muerte programada (pd-l1) para formación de imagen.
JP2018510864A (ja) 2015-03-10 2018-04-19 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ トランスグルタミナーゼによって結合可能な抗体およびそれによって製造される結合体
KR20180010264A (ko) 2015-05-29 2018-01-30 브리스톨-마이어스 스큅 컴퍼니 Ox40에 대한 항체 및 그의 용도
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
CA3008678A1 (en) 2015-12-21 2017-06-29 Bristol-Myers Squibb Company Variant antibodies for site-specific conjugation
BR112018067368A2 (pt) 2016-03-04 2019-01-15 Bristol-Myers Squibb Company terapia de combinação com anticorpos anti-cd73
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
CN116333129A (zh) 2017-05-25 2023-06-27 百时美施贵宝公司 包含经修饰的重链恒定区的抗体
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
FI3886914T3 (fi) 2018-11-30 2023-05-26 Bristol Myers Squibb Co Glutamiinin sisältävän kevytketjun c-terminaalisen jatkeen käsittävä vasta-aine, sen konjugaatteja, ja menetelmiä ja käyttöjä
US20220031860A1 (en) 2018-12-12 2022-02-03 Bristol-Myers Squibb Company Antibodies modified for transglutaminase conjugation, conjugates thereof, and methods and uses
US20240377413A1 (en) 2019-09-16 2024-11-14 Bristol-Myers Squibb Company Dual capture method for analysis of antibody-drug conjugates

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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
WO2002098868A1 (en) * 2001-06-01 2002-12-12 Bristol-Myers Squibb Company Epothilone derivatives
NZ537870A (en) * 2002-07-31 2007-03-30 Schering Ag New effector conjugates, process for their production and their pharmaceutical use
TWI405573B (zh) * 2003-01-27 2013-08-21 Endocyte Inc 維生素-受體結合性藥物輸送共軛物中間物及製備方法
US20090004118A1 (en) * 2004-10-07 2009-01-01 Shuming Nie Multifunctional Nanoparticle Conjugates And Their Use

Also Published As

Publication number Publication date
JP2009538350A (ja) 2009-11-05
EP2023960A1 (en) 2009-02-18
BRPI0712165A2 (pt) 2012-02-14
WO2007140298A1 (en) 2007-12-06
AU2007267536A1 (en) 2007-12-06
AR062448A1 (es) 2008-11-12
NO20084752L (no) 2008-12-17
MX2008014788A (es) 2008-12-02
KR20090025267A (ko) 2009-03-10
TW200813065A (en) 2008-03-16
IL195237A0 (en) 2009-08-03
EA200802390A1 (ru) 2009-06-30
CA2657276A1 (en) 2007-12-06
CN101495154A (zh) 2009-07-29
US20070275904A1 (en) 2007-11-29

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