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
    • 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 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)
  • Medicinal Preparation (AREA)
  • Peptides Or Proteins (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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ATE427948T1 (de) * 2001-04-24 2009-04-15 Purdue Research Foundation Folat-mimetika und deren folatrezeptorbindende konjugate
EP1504010B1 (en) * 2002-05-15 2009-03-25 Endocyte, Inc. Vitamin-mitomycin conjugates
EP2517730A3 (en) 2003-01-27 2013-01-02 Endocyte, Inc. Vitamin receptor binding drug delivery conjugates
US8288557B2 (en) * 2004-07-23 2012-10-16 Endocyte, Inc. Bivalent linkers and conjugates thereof
JP5289935B2 (ja) 2005-03-16 2013-09-11 エンドサイト，インコーポレイテッド プテロイン酸およびその結合体の合成と精製
US8465724B2 (en) 2005-08-19 2013-06-18 Endocyte, Inc. Multi-drug ligand conjugates
EP2382995A3 (en) * 2005-08-19 2013-09-25 Endocyte, Inc. Ligand conjugates of Vinca alkaloids, analogs and derivatives
US20100104626A1 (en) * 2007-02-16 2010-04-29 Endocyte, Inc. Methods and compositions for treating and diagnosing kidney disease
CN101678124A (zh) 2007-03-14 2010-03-24 恩多塞特公司 结合配体连接的微管溶素递药缀合物
CN101754969A (zh) * 2007-05-25 2010-06-23 百时美施贵宝公司 制备埃坡霉素化合物和类似物的方法
CN101784565B (zh) 2007-06-25 2014-12-10 恩多塞特公司 含有亲水性间隔区接头的共轭物
US9877965B2 (en) 2007-06-25 2018-01-30 Endocyte, Inc. Vitamin receptor drug delivery conjugates for treating inflammation
CA2703491C (en) 2007-10-25 2017-06-13 Endocyte, Inc. Tubulysins and processes for preparing
AU2012296624B2 (en) * 2011-08-15 2017-08-31 Research Foundation Of The City University Of New York NO- and H2S- releasing compounds
WO2013126797A1 (en) 2012-02-24 2013-08-29 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
AU2013331440A1 (en) 2012-10-16 2015-04-30 Endocyte, Inc. Drug delivery conjugates containing unnatural amino acids and methods for using
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
CN115322253A (zh) 2014-03-20 2022-11-11 百时美施贵宝公司 稳定化的基于纤连蛋白的支架分子
LT3221346T (lt) 2014-11-21 2020-11-10 Bristol-Myers Squibb Company Antikūnai, apimantys modifikuotas sunkiosios grandinės pastoviąsias sritis
HUE050596T2 (hu) 2014-11-21 2020-12-28 Bristol Myers Squibb Co Antitestek CD73 ellen és azok felhasználásai
ES2822990T3 (es) 2014-11-25 2021-05-05 Bristol Myers Squibb Co Novedosos polipéptidos de unión a PD-L1 para obtención de imágenes
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
UY36687A (es) 2015-05-29 2016-11-30 Bristol Myers Squibb Company Una Corporación Del Estado De Delaware Anticuerpos contra ox40 y sus usos
ES2809125T3 (es) 2015-09-23 2021-03-03 Bristol Myers Squibb Co Moléculas de armazón a base de fibronectina de unión a glipicano-3
EP3371176A4 (en) * 2015-10-16 2019-09-04 William Marsh Rice University EPOTHILON ANALOGUE, SYNTHESIS METHOD, TREATMENT METHOD AND MEDICAMENT CONJUGATE THEREFOR
JP2019505575A (ja) 2015-12-21 2019-02-28 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ 部位特異的な結合のための変異型抗体
IL295230A (en) 2016-03-04 2022-10-01 Bristol Myers Squibb Co Combination therapy with anti-cd73 antibodies
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
MX2019013132A (es) 2017-05-25 2020-01-27 Bristol Myers Squibb Co Anticuerpos que comprenden regiones constantes pesadas modificadas.
US20220106400A1 (en) 2018-11-28 2022-04-07 Bristol-Myers Squibb Company Antibodies comprising modified heavy constant regions
BR112021010060B1 (pt) 2018-11-30 2024-03-12 Bristol-Myers Squibb Company Anticorpo que compreende uma extensão c-terminal de cadeia leve que contém glutamina, conjugados do mesmo, e método de preparação de conjugados
WO2020123425A2 (en) 2018-12-12 2020-06-18 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
EP4359414A4 (en) * 2021-06-24 2026-01-21 Lycia Therapeutics Inc BIFOCTIONAL FOLATE RECEPTOR-BINDING COMPOUNDS

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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
WO2004012735A2 (en) * 2002-07-31 2004-02-12 Schering Ag New effector conjugates, process for their production and their pharmaceutical use
EP2517730A3 (en) * 2003-01-27 2013-01-02 Endocyte, Inc. Vitamin receptor binding drug delivery conjugates
JP2008515915A (ja) * 2004-10-07 2008-05-15 エモリー ユニバーシティー 多機能性ナノ粒子結合体およびそれらの使用

Also Published As

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

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