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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)
  • 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)

Families Citing this family (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1389209B1 (en) * 2001-04-24 2009-04-08 Purdue Research Foundation Folate mimetics and folate-receptor binding conjugates thereof
JP4814520B2 (ja) * 2002-05-15 2011-11-16 エンドサイト，インコーポレイテッド ビタミン−マイトマイシン結合体
TWI492750B (zh) 2003-01-27 2015-07-21 安德賽特公司 維生素-受體結合性藥物輸送共軛物、醫藥組合物、用途及製備方法
JP5149620B2 (ja) 2004-07-23 2013-02-20 エンドサイト，インコーポレイテッド ２価リンカーおよびその結合体
EP1863816B1 (en) 2005-03-16 2014-06-25 Endocyte, Inc. Synthesis and purification of pteroic acid and conjugates thereof
EP2382995A3 (en) * 2005-08-19 2013-09-25 Endocyte, Inc. Ligand conjugates of Vinca alkaloids, analogs and derivatives
AU2006279304A1 (en) 2005-08-19 2007-02-22 Endocyte, Inc. Multi-drug ligand conjugates
US20100104626A1 (en) * 2007-02-16 2010-04-29 Endocyte, Inc. Methods and compositions for treating and diagnosing kidney disease
AU2008224988A1 (en) * 2007-03-14 2008-09-18 Endocyte, Inc. Binding ligand linked drug delivery conjugates of tubulysins
JP2010528115A (ja) * 2007-05-25 2010-08-19 ブリストル−マイヤーズ スクイブ カンパニー エポチロン化合物およびアナログの製造方法
US9877965B2 (en) 2007-06-25 2018-01-30 Endocyte, Inc. Vitamin receptor drug delivery conjugates for treating inflammation
BRPI0812970A2 (pt) * 2007-06-25 2019-09-24 Endocyte Inc conjugados contendo espaçadores hidrofílicos
CN101909441B (zh) 2007-10-25 2015-05-13 恩多塞特公司 微管蛋白抑制剂及其制备方法
EP2744487B1 (en) * 2011-08-15 2016-10-05 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
CN104869998A (zh) 2012-10-16 2015-08-26 恩多塞特公司 含有非天然氨基酸的药物递送缀合物以及其使用方法
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
CN109316605B (zh) * 2014-01-20 2023-07-14 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
EP3647322B1 (en) 2014-03-20 2021-10-20 Bristol-Myers Squibb Company Stabilized fibronectin based scaffold molecules
SMT202000579T1 (it) 2014-11-21 2020-11-10 Bristol Myers Squibb Co Anticorpi comprendenti regioni costanti pesanti modificate
MX383868B (es) 2014-11-21 2025-03-14 Bristol Myers Squibb Co Anticuerpos contra cd73 y sus usos.
EP3702367B1 (en) 2014-11-25 2024-05-15 Bristol-Myers Squibb Company Novel pd-l1 binding polypeptides for imaging
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
HRP20230060T1 (hr) 2015-05-29 2023-03-17 Bristol-Myers Squibb Company Antitijela protiv ox40 i njihova primjena
US10584160B2 (en) 2015-09-23 2020-03-10 Bristol-Myers Squibb Company Glypican-3-binding fibronectin based scaffold molecules
CN108430996A (zh) * 2015-10-16 2018-08-21 威廉马歇莱思大学 埃博霉素类似物、合成方法、治疗方法及其药物缀合物
CN108431034A (zh) 2015-12-21 2018-08-21 百时美施贵宝公司 用于位点-特异性缀合的变体抗体
JP2019514844A (ja) 2016-03-04 2019-06-06 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ 抗ｃｄ７３抗体を用いた併用療法
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
EP4098662A1 (en) 2017-05-25 2022-12-07 Bristol-Myers Squibb Company Antibodies comprising modified heavy constant regions
EP3887397A1 (en) 2018-11-28 2021-10-06 Bristol-Myers Squibb Company Antibodies comprising modified heavy constant regions
PL3886914T3 (pl) 2018-11-30 2023-05-08 Bristol-Myers Squibb Company Przeciwciało zawierające c-końcowe rozszerzenie łańcucha lekkiego zawierające glutaminę, jego koniugaty oraz metody i zastosowania
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
WO2021055306A1 (en) 2019-09-16 2021-03-25 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

Family Cites Families (9)

* 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
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
IL166039A0 (en) * 2002-07-31 2006-01-15 Schering Ag New effector conjugates process for their production and their pharmaceutical use
TWI492750B (zh) * 2003-01-27 2015-07-21 安德賽特公司 維生素-受體結合性藥物輸送共軛物、醫藥組合物、用途及製備方法
US20090004118A1 (en) * 2004-10-07 2009-01-01 Shuming Nie Multifunctional Nanoparticle Conjugates And Their Use

Also Published As

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

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