JP2005532287A - Ｃｃ−１０６５類似体の改良プロドラッグ - Google Patents

Ｃｃ−１０６５類似体の改良プロドラッグ Download PDF

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JP2005532287A
JP2005532287A JP2003583343A JP2003583343A JP2005532287A JP 2005532287 A JP2005532287 A JP 2005532287A JP 2003583343 A JP2003583343 A JP 2003583343A JP 2003583343 A JP2003583343 A JP 2003583343A JP 2005532287 A JP2005532287 A JP 2005532287A
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prodrug
indol
indole
amino
chloromethyl
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JP2005532287A5 (https=
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チャオ，ロバート・ヨンシン
チャーリ，ラビ・ブイ・ジェイ
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イミュノジェン・インコーポレーテッド
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/82—Benzo [b] furans; Hydrogenated benzo [b] furans with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
    • C07D307/84—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D307/85—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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    • 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
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    • 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
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    • 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
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    • A61K47/548—Phosphates or phosphonates, e.g. bone-seeking
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    • A61K47/56—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/58—[b]- or [c]-condensed
    • C07D209/60—Naphtho [b] pyrroles; Hydrogenated naphtho [b] pyrroles
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
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    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
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    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
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    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Plural Heterocyclic Compounds (AREA)
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JP2003583343A 2002-04-05 2003-03-20 Ｃｃ−１０６５類似体の改良プロドラッグ Pending JP2005532287A (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US10/116,053 US6756397B2 (en) 2002-04-05 2002-04-05 Prodrugs of CC-1065 analogs
PCT/US2003/007282 WO2003086318A2 (en) 2002-04-05 2003-03-20 Improved prodrugs of cc-1065 analogs

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JP2005532287A true JP2005532287A (ja) 2005-10-27
JP2005532287A5 JP2005532287A5 (https=) 2009-08-27

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JP2003583343A Pending JP2005532287A (ja) 2002-04-05 2003-03-20 Ｃｃ−１０６５類似体の改良プロドラッグ
JP2010136274A Pending JP2010229151A (ja) 2002-04-05 2010-06-15 Ｃｃ−１０６５類似体の改良プロドラッグ

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US (7) US6756397B2 (https=)
EP (2) EP1492526B1 (https=)
JP (2) JP2005532287A (https=)
AT (1) ATE471161T1 (https=)
AU (1) AU2003218062C1 (https=)
CA (1) CA2480759A1 (https=)
DE (1) DE60333000D1 (https=)
DK (1) DK1492526T3 (https=)
ES (1) ES2347546T3 (https=)
WO (1) WO2003086318A2 (https=)

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JP2008505125A (ja) * 2004-07-02 2008-02-21 ザ ウォルター アンド エリザ ホール インスティチュート オブ メディカル リサーチ アルファヘリックス模倣体
JP2012513954A (ja) * 2008-11-03 2012-06-21 シンタルガ・ビーブイ 新規ｃｃ−１０６５類似体およびその複合体
JP2015512430A (ja) * 2012-04-05 2015-04-27 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ 癌を治療するための官能性チエノ−インドール誘導体
JP2015514101A (ja) * 2012-04-05 2015-05-18 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ 新たなアルキル化剤
US9421278B2 (en) 2014-01-10 2016-08-23 Synthon Biopharmaceuticals B.V. Duocarmycin ADCS showing improved in vivo antitumor activity
US9427480B2 (en) 2014-01-10 2016-08-30 Synthon Biopharmaceuticals B.V. Duocarmycin ADCs for use in treatment of endometrial cancer
JP2016183156A (ja) * 2010-04-21 2016-10-20 シンタルガ・ビーブイ Ｃｃ−１０６５類似体の新規の複合体および二官能性リンカー
JP2016533330A (ja) * 2013-09-25 2016-10-27 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ 新しい抗腫瘍剤としてのチエノ［２，３−ｅ］インドール誘導体
US10266606B2 (en) 2014-01-10 2019-04-23 Synthon Biopharmaceuticals B.V. Method for purifying Cys-linked antibody-drug conjugates

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US20110313230A1 (en) 2001-05-11 2011-12-22 Terrance Grant Johns Specific binding proteins and uses thereof
US20100056762A1 (en) 2001-05-11 2010-03-04 Old Lloyd J Specific binding proteins and uses thereof
AU2002311919B8 (en) 2001-05-11 2007-03-22 Ludwig Institute For Cancer Research Ltd Specific binding proteins and uses thereof
US6989452B2 (en) * 2001-05-31 2006-01-24 Medarex, Inc. Disulfide prodrugs and linkers and stabilizers useful therefor
US6756397B2 (en) * 2002-04-05 2004-06-29 Immunogen, Inc. Prodrugs of CC-1065 analogs
CN1816356A (zh) * 2003-05-14 2006-08-09 免疫原公司 药物缀合物组合物
KR20070053214A (ko) * 2004-08-26 2007-05-23 니콜라스 피라말 인디아 리미티드 신규 생분해성 링커를 함유하는 프로드럭
CA2486285C (en) * 2004-08-30 2017-03-07 Viktor S. Goldmakher Immunoconjugates targeting syndecan-1 expressing cells and use thereof
US20110166319A1 (en) * 2005-02-11 2011-07-07 Immunogen, Inc. Process for preparing purified drug conjugates
ES2503719T3 (es) 2005-02-11 2014-10-07 Immunogen, Inc. Procedimiento para preparar conjugados de anticuerpos y de maitansinoides
US7714016B2 (en) * 2005-04-08 2010-05-11 Medarex, Inc. Cytotoxic compounds and conjugates with cleavable substrates
WO2007019232A2 (en) * 2005-08-03 2007-02-15 Immunogen, Inc. Immunoconjugate formulations
CA3000520C (en) 2005-08-24 2023-04-04 Immunogen, Inc. Process for preparing antibody maytansinoid conjugates
NZ566395A (en) * 2005-09-26 2012-03-30 Medarex Inc Human monoclonal antibodies to CD70
EP2354163A3 (en) * 2005-09-26 2013-04-24 Medarex, Inc. Conjugates of duocarmycin and anti-CD70 or anti-PSMA antibodies
RS52100B (sr) * 2005-10-26 2012-06-30 Medarex, Inc. Postupci i jedinjenja za pripremu analoga cc-1065
EP1948691A1 (en) * 2005-11-17 2008-07-30 Millennium Pharmaceuticals, Inc. HUMANIZED IMMUNOGLOBULIN REACTIVE WITH a4ß7INTEGRIN
EP1806365A1 (en) 2006-01-05 2007-07-11 Boehringer Ingelheim International GmbH Antibody molecules specific for fibroblast activation protein and immunoconjugates containing them
RS52060B (sr) 2006-01-25 2012-04-30 Sanofi Citotoksični agensi koji sadrže nove derivate tomaimicina
EP1832577A1 (en) * 2006-03-07 2007-09-12 Sanofi-Aventis Improved prodrugs of CC-1065 analogs
MX2009000709A (es) * 2006-07-18 2009-02-04 Sanofi Aventis Anticuerpo antagonista contra epha2 para el tratamiento de cancer.
EP1914242A1 (en) * 2006-10-19 2008-04-23 Sanofi-Aventis Novel anti-CD38 antibodies for the treatment of cancer
MX2009006277A (es) * 2006-12-14 2009-07-24 Medarex Inc Anticuerpos humanos que se enlazan a cd70 y usos de los mismos.
TWI412367B (zh) 2006-12-28 2013-10-21 梅達雷克斯有限責任公司 化學鏈接劑與可裂解基質以及其之綴合物
US9090693B2 (en) 2007-01-25 2015-07-28 Dana-Farber Cancer Institute Use of anti-EGFR antibodies in treatment of EGFR mutant mediated disease
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