AR078471A1 - COMPUESTOS MAITANSINOIDES Y EL USO DE ESTOS PARA PREPARAR CONJUGADOS CON UN ANTICUERPO LOS CUALES SE UTILIZAN COMO AGENTES ANTICANCERIGENOS Y EL PROCEDIMIENTO DE PREPARACIoN DE ESTOS CONJUGADOS - Google Patents
COMPUESTOS MAITANSINOIDES Y EL USO DE ESTOS PARA PREPARAR CONJUGADOS CON UN ANTICUERPO LOS CUALES SE UTILIZAN COMO AGENTES ANTICANCERIGENOS Y EL PROCEDIMIENTO DE PREPARACIoN DE ESTOS CONJUGADOSInfo
- Publication number
- AR078471A1 AR078471A1 ARP100103531A ARP100103531A AR078471A1 AR 078471 A1 AR078471 A1 AR 078471A1 AR P100103531 A ARP100103531 A AR P100103531A AR P100103531 A ARP100103531 A AR P100103531A AR 078471 A1 AR078471 A1 AR 078471A1
- Authority
- AR
- Argentina
- Prior art keywords
- conjugates
- maitansinoid
- antibody
- compounds
- preparation procedure
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 abstract 1
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 1
- 238000002835 absorbance Methods 0.000 abstract 1
- 230000001093 anti-cancer Effects 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/18—Bridged 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
-
- 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
- A61K47/68—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
- A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
- A61K47/68033—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a maytansine
-
- 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
- A61K47/68—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6835—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
- A61K47/6849—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a receptor, a cell surface antigen or a cell surface determinant
-
- 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
- C07K—PEPTIDES
- C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
- C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
- C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
- C07K16/30—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Immunology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Cell Biology (AREA)
- Biophysics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- General Chemical & Material Sciences (AREA)
- Biochemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Peptides Or Proteins (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Medicinal Preparation (AREA)
- Other Investigation Or Analysis Of Materials By Electrical Means (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
Abstract
Compuesto de la formula (1), en donde: ALK es un grupo alquileno C1-6; X1 y X2 son cada uno independientemente uno de los grupos siguientes -CH=CH-, -CO-, -CONR-, -NRCO-, -COO-, -OCO-, -OCONR-, -NRCOO-, -NRCONR'-, -NR-, -S(O)n (n = 0, 1 o 2) o -O-; R y R' son independientemente H o un grupo alquilo C1-6; i es un numero entero de 1 a 40, preferiblemente de 1 a 20, y más preferiblemente de 1 a 10; j es un numero entero que corresponde a 1 cuando X2 es -CH=CH- y 2 cuando X2 no es -CH=CH-; Zb es un enlace sencillo, -O- o -NH- y Rb es H o un grupo alquilo C1-6, cicloalquilo C3-7, arilo, heteroarilo o heterocicloalquilo C3-7; o Zb es un enlace sencillo y Rb es Hal. Su uso como anticancerígeno. Reivindicacion 17: Conjugado segun la reivindicacion 16 que tiene un DAR promedio, medido con un espectrometro UV por encima de 4, más particularmente entre 4 y 10, incluso más particularmente entre 4 y 7, estando determinado el DAR mediante la ecuacion siguiente: DAR = cD / cA con: cD = [(eA280 x A252) - (eA252 x A280)] / [(eD252 x eA280) - (eA252 x eD280)]; cA = [A280 - (cD x eD280)] / eA280; eD252 = 26.159 M-1cm-1; eD280 = 5.180 M-1cm-1; eA280 = 224.000 M-1cm-1; eA252 = 82.880 M-1cm-1; siendo A252 y A280 las absorbancias del conjugado medidas en el espectrometro UV a 252 y 280 hm respectivamente.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP09305939 | 2009-10-02 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR078471A1 true AR078471A1 (es) | 2011-11-09 |
Family
ID=41698152
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP100103531A AR078471A1 (es) | 2009-10-02 | 2010-09-29 | COMPUESTOS MAITANSINOIDES Y EL USO DE ESTOS PARA PREPARAR CONJUGADOS CON UN ANTICUERPO LOS CUALES SE UTILIZAN COMO AGENTES ANTICANCERIGENOS Y EL PROCEDIMIENTO DE PREPARACIoN DE ESTOS CONJUGADOS |
Country Status (24)
Country | Link |
---|---|
US (1) | US20120276124A1 (es) |
EP (1) | EP2483279A1 (es) |
JP (1) | JP2013506653A (es) |
KR (1) | KR20120091166A (es) |
CN (1) | CN102741260A (es) |
AR (1) | AR078471A1 (es) |
AU (1) | AU2010302247A1 (es) |
BR (1) | BR112012007305A2 (es) |
CA (1) | CA2774916A1 (es) |
CL (1) | CL2012000820A1 (es) |
CR (1) | CR20120147A (es) |
EA (1) | EA201270473A1 (es) |
EC (1) | ECSP12011756A (es) |
IL (1) | IL218740A0 (es) |
MA (1) | MA33702B1 (es) |
MX (1) | MX2012003998A (es) |
NI (1) | NI201200051A (es) |
NZ (1) | NZ599045A (es) |
PE (1) | PE20121534A1 (es) |
TN (1) | TN2012000115A1 (es) |
TW (1) | TW201117814A (es) |
UY (1) | UY32913A (es) |
WO (1) | WO2011039721A1 (es) |
ZA (1) | ZA201202328B (es) |
Families Citing this family (25)
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FR2949469A1 (fr) * | 2009-08-25 | 2011-03-04 | Sanofi Aventis | Derives anticancereux, leur preparation et leur application en therapeutique |
TW201116297A (en) * | 2009-10-02 | 2011-05-16 | Sanofi Aventis | Antibodies that specifically bind to the EphA2 receptor |
FR2963007B1 (fr) | 2010-07-26 | 2013-04-05 | Sanofi Aventis | Derives anticancereux, leur preparation et leur application therapeutique |
KR102351886B1 (ko) | 2011-03-29 | 2022-01-17 | 이뮤노젠 아이엔씨 | 일-단계 방법에 의한 메이탄시노이드 항체 접합체의 제조 |
WO2012135517A2 (en) | 2011-03-29 | 2012-10-04 | Immunogen, Inc. | Preparation of maytansinoid antibody conjugates by a one-step process |
EP2904089A4 (en) | 2012-10-04 | 2016-05-25 | Immunogen Inc | USE OF A PVDF MEMBRANE FOR PURIFYING CELL BINDING AGENT-CYTOTOXIC AGENT CONJUGATES |
NO2789793T3 (es) * | 2012-10-24 | 2018-01-27 | ||
BR112015008376A2 (pt) * | 2012-10-24 | 2017-09-26 | Polytherics Ltd | conjugados fármaco-proteína |
CN103333179B (zh) * | 2012-12-21 | 2017-06-16 | 百奥泰生物科技(广州)有限公司 | 类美登素衍生物及其制备方法和用途 |
WO2014145090A1 (en) | 2013-03-15 | 2014-09-18 | Regeneron Pharmaceuticals, Inc. | Biologically active molecules, conjugates thereof, and therapeutic uses |
US20160143914A1 (en) * | 2013-06-13 | 2016-05-26 | Emory University | Nanoparticles for Encapsulation and Delivery of Bioactive Compounds and Compositions Thereof |
AU2014311361B2 (en) | 2013-08-26 | 2018-11-29 | Regeneron Pharmaceuticals, Inc. | Pharmaceutical compositions comprising macrolide diastereomers, methods of their synthesis and therapeutic uses |
CN103483357B (zh) * | 2013-10-12 | 2015-11-18 | 齐鲁制药有限公司 | 一种抗体-美登素偶联物的中间体新晶型及其制备方法 |
JP6745218B2 (ja) | 2013-11-27 | 2020-08-26 | レッドウッド バイオサイエンス, インコーポレイテッド | ヒドラジニル−ピロロ化合物及び複合体を生成するための方法 |
US9562059B2 (en) * | 2013-12-02 | 2017-02-07 | Hong Kong Baptist University | Anticancer maytansinoids with two fused macrocyclic rings |
GB201416960D0 (en) * | 2014-09-25 | 2014-11-12 | Antikor Biopharma Ltd | Biological materials and uses thereof |
EP3220959A1 (en) | 2014-11-19 | 2017-09-27 | ImmunoGen, Inc. | Process for preparing cell-binding agent-cytotoxic agent conjugates |
CN106267225B (zh) | 2015-05-29 | 2020-03-06 | 上海新理念生物医药科技有限公司 | 三马来酰亚胺型连接子及其应用 |
JP6802840B2 (ja) | 2015-06-09 | 2020-12-23 | エックスディーシーエクスプローラー (シャンハイ) カンパニー リミテッド | 抗体薬物複合体、中間体、その製造方法、薬学的組成物及び応用 |
JP6638970B2 (ja) * | 2015-06-30 | 2020-02-05 | 株式会社 東北テクノアーチ | ヘテロ型単分散ポリエチレングリコール、ヘテロ型単分散ポリエチレングリコール製造用中間体の製造方法 |
US12102689B2 (en) | 2015-11-09 | 2024-10-01 | R.P. Scherer Technologies, Llc | Anti-CD22 antibody-maytansine conjugates and methods of use thereof |
US9950076B2 (en) | 2016-01-25 | 2018-04-24 | Regeneron Pharmaceuticals, Inc. | Maytansinoid derivatives, conjugates thereof, and methods of use |
TW201731532A (zh) | 2016-02-05 | 2017-09-16 | 伊繆諾金公司 | 用於製備細胞結合劑-細胞毒性劑結合物之有效方法 |
US10195283B2 (en) * | 2016-03-18 | 2019-02-05 | R.P. Scherer Technologies, Llc | Hydrazinyl-substituted heteroaryl compounds and methods for producing a conjugate |
CN107652219B (zh) | 2017-08-14 | 2021-06-08 | 上海新理念生物医药科技有限公司 | 四马来酰亚胺型连接子及其应用 |
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EP1258255A1 (en) * | 2001-05-18 | 2002-11-20 | Boehringer Ingelheim International GmbH | Conjugates of an antibody to CD44 and a maytansinoid |
US6716821B2 (en) * | 2001-12-21 | 2004-04-06 | Immunogen Inc. | Cytotoxic agents bearing a reactive polyethylene glycol moiety, cytotoxic conjugates comprising polyethylene glycol linking groups, and methods of making and using the same |
EP1578446B1 (en) | 2002-11-07 | 2015-04-08 | ImmunoGen, Inc. | Anti-cd33 antibodies and method for treatment of acute myeloid leukemia using the same |
WO2004100885A2 (en) * | 2003-05-09 | 2004-11-25 | The Trustees Of The University Of Pennsylvania | Compositions and methods for treating cancer |
CN101186613B (zh) | 2003-05-20 | 2014-09-17 | 伊缪诺金公司 | 含有新的美登素类的改进的细胞毒剂 |
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EP1669358A1 (en) | 2004-12-07 | 2006-06-14 | Aventis Pharma S.A. | Cytotoxic agents comprising new taxanes |
CA3005835C (en) | 2004-12-22 | 2023-01-31 | Ambrx, Inc. | Compositions containing, methods involving, and uses of non-natural amino acids and polypeptides |
AU2006280146B2 (en) | 2005-08-09 | 2012-06-28 | Immunogen, Inc. | Method of acylating maytansinol with chiral amino acids |
CA2893252C (en) * | 2005-08-24 | 2018-05-29 | Immunogen, Inc. | Process for preparing antibody maytansinoid conjugates |
EP1832577A1 (en) | 2006-03-07 | 2007-09-12 | Sanofi-Aventis | Improved prodrugs of CC-1065 analogs |
EP1864682A1 (en) | 2006-06-09 | 2007-12-12 | Sanofi-Aventis | Leptomycin derivatives |
EA020324B1 (ru) * | 2006-07-18 | 2014-10-30 | Санофи-Авентис | АНТИТЕЛА К РЕЦЕПТОРУ ЭФРИНА EphA2 И ИХ ПРИМЕНЕНИЕ |
EP1914242A1 (en) | 2006-10-19 | 2008-04-23 | Sanofi-Aventis | Novel anti-CD38 antibodies for the treatment of cancer |
US8865875B2 (en) | 2007-08-22 | 2014-10-21 | Medarex, L.L.C. | Site-specific attachment of drugs or other agents to engineered antibodies with C-terminal extensions |
BRPI0911442A2 (pt) * | 2008-04-30 | 2019-03-12 | Immunogen, Inc. | conjugados potentes e ligantes hidrofílicos |
TW201116297A (en) * | 2009-10-02 | 2011-05-16 | Sanofi Aventis | Antibodies that specifically bind to the EphA2 receptor |
-
2010
- 2010-09-29 AR ARP100103531A patent/AR078471A1/es not_active Application Discontinuation
- 2010-09-29 UY UY0001032913A patent/UY32913A/es not_active Application Discontinuation
- 2010-09-29 TW TW099133090A patent/TW201117814A/zh unknown
- 2010-09-30 PE PE2012000428A patent/PE20121534A1/es not_active Application Discontinuation
- 2010-09-30 EA EA201270473A patent/EA201270473A1/ru unknown
- 2010-09-30 MX MX2012003998A patent/MX2012003998A/es unknown
- 2010-09-30 JP JP2012531540A patent/JP2013506653A/ja active Pending
- 2010-09-30 AU AU2010302247A patent/AU2010302247A1/en not_active Abandoned
- 2010-09-30 CN CN2010800548853A patent/CN102741260A/zh active Pending
- 2010-09-30 BR BR112012007305A patent/BR112012007305A2/pt not_active IP Right Cessation
- 2010-09-30 EP EP10768578A patent/EP2483279A1/en not_active Withdrawn
- 2010-09-30 KR KR1020127011167A patent/KR20120091166A/ko not_active Application Discontinuation
- 2010-09-30 NZ NZ599045A patent/NZ599045A/xx not_active IP Right Cessation
- 2010-09-30 CA CA2774916A patent/CA2774916A1/en not_active Abandoned
- 2010-09-30 WO PCT/IB2010/054417 patent/WO2011039721A1/en active Application Filing
-
2012
- 2012-03-14 TN TNP2012000115A patent/TN2012000115A1/en unknown
- 2012-03-19 IL IL218740A patent/IL218740A0/en unknown
- 2012-03-26 CR CR20120147A patent/CR20120147A/es unknown
- 2012-03-26 EC ECSP12011756 patent/ECSP12011756A/es unknown
- 2012-03-29 US US13/434,363 patent/US20120276124A1/en not_active Abandoned
- 2012-03-30 ZA ZA2012/02328A patent/ZA201202328B/en unknown
- 2012-03-30 NI NI201200051A patent/NI201200051A/es unknown
- 2012-04-02 CL CL2012000820A patent/CL2012000820A1/es unknown
- 2012-04-27 MA MA34818A patent/MA33702B1/fr unknown
Also Published As
Publication number | Publication date |
---|---|
EA201270473A1 (ru) | 2013-02-28 |
KR20120091166A (ko) | 2012-08-17 |
WO2011039721A1 (en) | 2011-04-07 |
CN102741260A (zh) | 2012-10-17 |
IL218740A0 (en) | 2012-06-28 |
JP2013506653A (ja) | 2013-02-28 |
BR112012007305A2 (pt) | 2016-12-06 |
AU2010302247A1 (en) | 2012-04-26 |
CL2012000820A1 (es) | 2012-08-31 |
MA33702B1 (fr) | 2012-10-01 |
EP2483279A1 (en) | 2012-08-08 |
ECSP12011756A (es) | 2012-07-31 |
TW201117814A (en) | 2011-06-01 |
CA2774916A1 (en) | 2011-04-07 |
CR20120147A (es) | 2012-06-01 |
UY32913A (es) | 2011-04-29 |
NI201200051A (es) | 2012-08-09 |
US20120276124A1 (en) | 2012-11-01 |
MX2012003998A (es) | 2012-04-20 |
PE20121534A1 (es) | 2012-12-03 |
NZ599045A (en) | 2013-09-27 |
ZA201202328B (en) | 2014-06-25 |
TN2012000115A1 (en) | 2013-09-19 |
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