JP5010089B2 - Ｃｃ−１０６５およびデュオカルマイシンのアキラルアナログの組成物およびその使用方法 - Google Patents

Ｃｃ−１０６５およびデュオカルマイシンのアキラルアナログの組成物およびその使用方法 Download PDF

Info

Publication number
JP5010089B2
JP5010089B2 JP2002534280A JP2002534280A JP5010089B2 JP 5010089 B2 JP5010089 B2 JP 5010089B2 JP 2002534280 A JP2002534280 A JP 2002534280A JP 2002534280 A JP2002534280 A JP 2002534280A JP 5010089 B2 JP5010089 B2 JP 5010089B2
Authority
JP
Japan
Prior art keywords
chloroethyl
carboxamide
mmol
phenol
added
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
JP2002534280A
Other languages
English (en)
Japanese (ja)
Other versions
JP2004511466A5 (https=
JP2004511466A (ja
Inventor
モーゼス リー
Original Assignee
スピロジェン リミテッド
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 スピロジェン リミテッド filed Critical スピロジェン リミテッド
Publication of JP2004511466A publication Critical patent/JP2004511466A/ja
Publication of JP2004511466A5 publication Critical patent/JP2004511466A5/ja
Application granted granted Critical
Publication of JP5010089B2 publication Critical patent/JP5010089B2/ja
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members 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 ring carbon atoms
    • C07D207/36—Oxygen or sulfur atoms
    • C07D207/40—2,5-Pyrrolidine-diones
    • C07D207/416—2,5-Pyrrolidine-diones 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 other ring carbon atoms
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/74—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton
    • C07C215/76—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton of the same non-condensed six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/32—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
    • C07C235/38—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/26—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring
    • C07C271/28—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring to a carbon atom of a non-condensed six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/26—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring
    • C07C271/30—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring to a carbon atom of a six-membered aromatic ring being part of a condensed ring system
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D209/02—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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 ring carbon atoms
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/64—One oxygen atom attached in position 2 or 6
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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 ring carbon atoms
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/69—Two or more oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Polysaccharides And Polysaccharide Derivatives (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2002534280A 2000-09-19 2001-09-19 Ｃｃ−１０６５およびデュオカルマイシンのアキラルアナログの組成物およびその使用方法 Expired - Fee Related JP5010089B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US66616000A 2000-09-19 2000-09-19
US09/666,160 2000-09-19
PCT/US2001/029160 WO2002030894A2 (en) 2000-09-19 2001-09-19 Compositions and methods of the use thereof achiral analogues of cc-1065 and the duocarmycins

Publications (3)

Publication Number Publication Date
JP2004511466A JP2004511466A (ja) 2004-04-15
JP2004511466A5 JP2004511466A5 (https=) 2008-11-13
JP5010089B2 true JP5010089B2 (ja) 2012-08-29

Family

ID=24673061

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2002534280A Expired - Fee Related JP5010089B2 (ja) 2000-09-19 2001-09-19 Ｃｃ−１０６５およびデュオカルマイシンのアキラルアナログの組成物およびその使用方法

Country Status (9)

Country Link
US (1) US6660742B2 (https=)
EP (1) EP1320522B8 (https=)
JP (1) JP5010089B2 (https=)
CN (1) CN1315805C (https=)
AT (1) ATE310724T1 (https=)
DE (1) DE60115265T2 (https=)
DK (1) DK1320522T3 (https=)
ES (1) ES2254492T3 (https=)
WO (1) WO2002030894A2 (https=)

Families Citing this family (107)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MY125533A (en) * 1999-12-06 2006-08-30 Bristol Myers Squibb Co Heterocyclic dihydropyrimidine compounds
AU2002311919B8 (en) 2001-05-11 2007-03-22 Ludwig Institute For Cancer Research Ltd Specific binding proteins and uses thereof
US20100056762A1 (en) 2001-05-11 2010-03-04 Old Lloyd J Specific binding proteins and uses thereof
TW200307539A (en) * 2002-02-01 2003-12-16 Bristol Myers Squibb Co Cycloalkyl inhibitors of potassium channel function
GB0205176D0 (en) * 2002-03-06 2002-04-17 Astrazeneca Ab Chemical compounds
TW200403058A (en) * 2002-04-19 2004-03-01 Bristol Myers Squibb Co Heterocyclo inhibitors of potassium channel function
WO2004035571A1 (en) * 2002-10-15 2004-04-29 Rigel Pharmaceuticals, Inc. Substituted indoles and their use as hcv inhibitors
US7208491B2 (en) 2003-02-07 2007-04-24 Hoffmann-La Roche Inc. N-monoacylated o-phenylenediamines
US7078419B2 (en) 2003-03-10 2006-07-18 Boehringer Ingelheim Pharmaceuticals, Inc. Cytokine inhibitors
WO2005032594A2 (en) * 2003-10-03 2005-04-14 The Government Of The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Alkylators linked to polyamides as dna binding agents
KR101274524B1 (ko) * 2004-03-16 2013-06-19 온코노바 테라퓨틱스, 인코포레이티드 증식성 질병 치료용 치환 페녹시- 및 페닐티오- 유도체
WO2006055463A2 (en) * 2004-11-15 2006-05-26 Bristol-Myers Squibb Company 2-amino-3-functionalized tetralin derivatives and related glycogen phosphorylase inhibitors
WO2006053274A2 (en) * 2004-11-15 2006-05-18 Bristol-Myers Squibb Company 2-amino-1-functionalized tetralin derivatives and related glycogen phosphorylase inhibitors
US7226942B2 (en) 2004-11-15 2007-06-05 Bristol-Myers Squibb Company 2-amino-4-functionalized tetralin derivatives and related glycogen phosphorylase inhibitors
US7223786B2 (en) * 2004-11-15 2007-05-29 Bristol-Myers Squibb Company 2-aminonaphthalene derivatives and related glycogen phosphorylase inhibitors
US8782706B2 (en) 2005-12-29 2014-07-15 United Video Properties Systems and methods for providing channel groups in an interactive media guidance application
MX352516B (es) 2006-07-05 2017-04-06 Fibrotech Therapeutics Pty Ltd Compuestos terapeuticos.
GB0619325D0 (en) * 2006-09-30 2006-11-08 Univ Strathclyde New compounds
AR063311A1 (es) * 2006-10-18 2009-01-21 Novartis Ag Compuestos organicos
WO2008050140A2 (en) * 2006-10-27 2008-05-02 Spirogen Limited Compounds for treatment of parasitic infection
US9090693B2 (en) 2007-01-25 2015-07-28 Dana-Farber Cancer Institute Use of anti-EGFR antibodies in treatment of EGFR mutant mediated disease
CA2680854C (en) 2007-03-15 2017-02-14 Ludwig Institute For Cancer Research Treatment method using egfr antibodies and src inhibitors and related formulations
US9901567B2 (en) 2007-08-01 2018-02-27 Syntarga B.V. Substituted CC-1065 analogs and their conjugates
CN108424454B (zh) 2007-08-14 2022-05-31 路德维格癌症研究所有限公司 靶向egf受体的单克隆抗体175及其衍生物和用途
GB0819095D0 (en) 2008-10-17 2008-11-26 Spirogen Ltd Pyrrolobenzodiazepines
ES2647317T3 (es) 2008-11-03 2017-12-20 Syntarga B.V. Análogos de CC-1065 y sus conjugados
US20110076232A1 (en) * 2009-09-29 2011-03-31 Ludwig Institute For Cancer Research Specific binding proteins and uses thereof
CN102574843B (zh) 2009-10-22 2015-06-17 法博太科制药有限公司 抗纤维化剂的稠环类似物
JP5875083B2 (ja) 2010-04-15 2016-03-02 メディミューン リミテッド 増殖性疾患治療用ピロロベンゾジアゼピン
CA2795349C (en) 2010-04-15 2016-11-29 Seattle Genetics, Inc. Targeted pyrrolobenzodiazepine conjugates
PT3056203T (pt) 2010-04-21 2018-02-15 Syntarga Bv Conjugados de análogos de cc-1065 e ligantes bifuncionais
WO2012171020A1 (en) 2011-06-10 2012-12-13 Mersana Therapeutics, Inc. Protein-polymer-drug conjugates
SG11201400770SA (en) 2011-09-20 2014-04-28 Spirogen Sarl Pyrrolobenzodiazepines as unsymmetrical dimeric pbd compounds for inclusion in targeted conjugates
CA2850373C (en) 2011-10-14 2019-07-16 Seattle Genetics, Inc. Pyrrolobenzodiazepines and targeted conjugates
EP2751111B1 (en) 2011-10-14 2017-04-26 MedImmune Limited Asymmetrical bis-(5H-Pyrrolo[2,1-c][1,4]benzodiazepin-5-one) derivatives for the treatment of proliferative or autoimmune diseases
AU2012322932B2 (en) 2011-10-14 2016-11-10 Medimmune Limited Pyrrolobenzodiazepines
CN103997893B (zh) 2011-10-14 2019-04-12 西雅图基因公司 吡咯并苯并二氮杂卓和靶向结合物
CN102827061A (zh) * 2012-09-19 2012-12-19 兰州大学 5,6,7-三甲氧基吲哚类衍生物、制备方法及用途
HRP20190366T1 (hr) 2012-10-12 2019-04-19 Medimmune Limited Pirolobenzodiazepini i njihovi konjugati
EP2906249B1 (en) 2012-10-12 2018-06-27 MedImmune Limited Synthesis and intermediates of pyrrolobenzodiazepine derivatives for conjugation
JP6392765B2 (ja) 2012-10-12 2018-09-19 エイディーシー・セラピューティクス・エス・アーＡｄｃ Ｔｈｅｒａｐｅｕｔｉｃｓ Ｓａ ピロロベンゾジアゼピン−抗体結合体
EP2906297B1 (en) 2012-10-12 2017-12-06 ADC Therapeutics SA Pyrrolobenzodiazepine-antibody conjugates
EP2906296B1 (en) 2012-10-12 2018-03-21 ADC Therapeutics SA Pyrrolobenzodiazepine-antibody conjugates
MX338711B (es) 2012-10-12 2016-04-28 Medimmune Ltd Pirrolobenzodiazepinas y conjugados de las mismas.
ES2680153T3 (es) 2012-10-12 2018-09-04 Adc Therapeutics Sa Conjugados de anticuerpos anti-PSMA-pirrolobenzodiazepinas
RS57694B1 (sr) 2012-10-12 2018-11-30 Adc Therapeutics Sa Pirolobenzodiazepin - anti-psma konjugati antitela
HRP20182129T1 (hr) 2012-10-12 2019-02-08 Adc Therapeutics Sa Konjugati protutijelo - pirolobenzodiazepin
CA2892863C (en) 2012-12-10 2022-03-15 Mersana Therapeutics, Inc. Polymeric scaffold based on phf for targeted drug delivery
WO2014093640A1 (en) 2012-12-12 2014-06-19 Mersana Therapeutics,Inc. Hydroxy-polmer-drug-protein conjugates
CN105189507A (zh) 2012-12-21 2015-12-23 斯皮罗根有限公司 吡咯并苯并二氮杂卓及其结合物
CN110627797A (zh) 2012-12-21 2019-12-31 麦迪穆有限责任公司 用于治疗增殖性和自身免疫疾病的非对称吡咯并苯并二氮杂卓二聚物
AU2014229529B2 (en) 2013-03-13 2018-02-15 Medimmune Limited Pyrrolobenzodiazepines and conjugates thereof
TWI680766B (zh) 2013-03-13 2020-01-01 英商梅迪繆思有限公司 吡咯并苯并二氮呯及其共軛物
KR102087850B1 (ko) 2013-10-11 2020-03-12 메르사나 테라퓨틱스, 인코포레이티드 단백질-고분자-약물 접합체
WO2015052535A1 (en) 2013-10-11 2015-04-16 Spirogen Sàrl Pyrrolobenzodiazepine-antibody conjugates
EP3054983B1 (en) 2013-10-11 2019-03-20 Medimmune Limited Pyrrolobenzodiazepine-antibody conjugates
GB201317982D0 (en) 2013-10-11 2013-11-27 Spirogen Sarl Pyrrolobenzodiazepines and conjugates thereof
WO2015052534A1 (en) 2013-10-11 2015-04-16 Spirogen Sàrl Pyrrolobenzodiazepine-antibody conjugates
GB201317981D0 (en) 2013-10-11 2013-11-27 Spirogen Sarl Pyrrolobenzodiazepines and conjugates thereof
ES2754397T3 (es) 2013-10-11 2020-04-17 Asana Biosciences Llc Conjugados de proteína-polímero-fármaco
RU2686085C2 (ru) 2014-01-10 2019-04-24 Синтон Байофармасьютикалс Б. В. Конъюгаты антитело-лекарственное средство (adc) с дуокармицином, применяемые для лечения рака эндометрия
CA2935433C (en) 2014-01-10 2019-04-02 Synthon Biopharmaceuticals B.V. Duocarmycin anti-her2 antibody drug conjucates with activity against her2 expressing malignancies
RU2680404C2 (ru) 2014-01-10 2019-02-21 Синтон Байофармасьютикалс Б. В. Способ очистки cys-связанных конъюгатов антитело-лекарственное средство
GB201416112D0 (en) 2014-09-12 2014-10-29 Medimmune Ltd Pyrrolobenzodiazepines and conjugates thereof
CN107148285B (zh) 2014-11-25 2022-01-04 Adc治疗股份有限公司 吡咯并苯并二氮杂䓬-抗体缀合物
GB201506411D0 (en) 2015-04-15 2015-05-27 Bergenbio As Humanized anti-axl antibodies
GB201506402D0 (en) 2015-04-15 2015-05-27 Berkel Patricius H C Van And Howard Philip W Site-specific antibody-drug conjugates
DE102016105449A1 (de) * 2015-10-29 2017-05-04 Georg-August-Universität Göttingen Stiftung Öffentlichen Rechts Bifunktionale Prodrugs
GB201601431D0 (en) 2016-01-26 2016-03-09 Medimmune Ltd Pyrrolobenzodiazepines
GB201602359D0 (en) 2016-02-10 2016-03-23 Medimmune Ltd Pyrrolobenzodiazepine Conjugates
GB201602356D0 (en) 2016-02-10 2016-03-23 Medimmune Ltd Pyrrolobenzodiazepine Conjugates
GB201607478D0 (en) 2016-04-29 2016-06-15 Medimmune Ltd Pyrrolobenzodiazepine Conjugates
WO2018004338A1 (en) 2016-06-27 2018-01-04 Tagworks Pharmaceuticals B.V. Cleavable tetrazine used in bio-orthogonal drug activation
GB201617466D0 (en) 2016-10-14 2016-11-30 Medimmune Ltd Pyrrolobenzodiazepine conjugates
US11135307B2 (en) 2016-11-23 2021-10-05 Mersana Therapeutics, Inc. Peptide-containing linkers for antibody-drug conjugates
JP7185631B2 (ja) 2017-02-03 2022-12-07 サータ セラピューティクス プロプライエタリー リミテッド 抗線維化化合物
GB201702031D0 (en) 2017-02-08 2017-03-22 Medlmmune Ltd Pyrrolobenzodiazepine-antibody conjugates
RS61795B1 (sr) 2017-02-08 2021-06-30 Adc Therapeutics Sa Konjugati pirolobenzodiazepin antitela
CN110582505B (zh) 2017-04-18 2021-04-02 免疫医疗有限公司 吡咯并苯并二氮杂*缀合物
WO2018193102A1 (en) 2017-04-20 2018-10-25 Adc Therapeutics Sa Combination therapy with an anti-axl antibody-drug conjugate
CA3064804A1 (en) 2017-06-14 2018-12-20 Adc Therapeutics Sa Dosage regimes for the administration of an anti-cd19 adc
AU2018290330A1 (en) 2017-06-22 2020-01-02 Mersana Therapeutics, Inc. Methods of producing drug-carrying polymer scaffolds and protein-polymer-drug conjugates
KR102270107B1 (ko) 2017-08-18 2021-06-30 메디뮨 리미티드 피롤로벤조디아제핀 컨쥬게이트
GB201803342D0 (en) 2018-03-01 2018-04-18 Medimmune Ltd Methods
GB201806022D0 (en) 2018-04-12 2018-05-30 Medimmune Ltd Pyrrolobenzodiazepines and conjugates thereof
AU2019262520B2 (en) 2018-05-04 2025-07-10 Tagworks Pharmaceuticals B.V. Tetrazines for high click conjugation yield in vivo and high click release yield
CA3099421C (en) 2018-05-04 2025-05-06 Tagworks Pharmaceuticals B.V. COMPOUNDS INCLUDING A BINDER TO INCREASE TRANSCYCLOOCTENE STABILITY
CN113365664A (zh) 2018-10-29 2021-09-07 梅尔莎纳医疗公司 具有含肽接头的半胱氨酸工程化的抗体-药物缀合物
CN113631560B (zh) 2019-03-15 2025-02-18 麦迪穆有限责任公司 氮杂环丁烷并苯并二氮杂䓬二聚体和用于治疗癌症的包含它们的缀合物
DK3983363T3 (da) 2019-06-17 2024-06-24 Tagworks Pharmaceuticals B V Forbindelser til hurtig og effektiv klikfrigivelse
IL289094A (en) 2019-06-17 2022-02-01 Tagworks Pharmaceuticals B V Tetrazines for increasing the speed and yield of the "click release" reaction
WO2021040393A1 (ko) * 2019-08-26 2021-03-04 국제약품 주식회사 인돌 카복사미드 유도체 및 그를 포함하는 약제학적 조성물
US20250327057A1 (en) 2021-09-06 2025-10-23 Veraxa Biotech Gmbh Novel aminoacyl-trna synthetase variants for genetic code expansion in eukaryotes
WO2023094525A1 (en) 2021-11-25 2023-06-01 Veraxa Biotech Gmbh Improved antibody-payload conjugates (apcs) prepared by site-specific conjugation utilizing genetic code expansion
DK4186529T3 (da) 2021-11-25 2025-08-25 Veraxa Biotech Gmbh Forbedrede antistof-payload-konjugater (apc) fremstillet ved stedspecifik konjugering ved hjælp af genetisk kodeudvidelse
US20250135011A1 (en) 2021-12-08 2025-05-01 European Molecular Biology Laboratory Hydrophilic tetrazine-functionalized payloads for preparation of targeting conjugates
US20250114489A1 (en) 2022-02-15 2025-04-10 Tagworks Pharmaceuticals B.V. Masked il12 protein
CA3261603A1 (en) 2022-07-15 2024-01-18 Pheon Therapeutics Ltd ANTIBODY-DRUG CONJUGATES
WO2024080872A1 (en) 2022-10-12 2024-04-18 Tagworks Pharmaceuticals B.V. Strained bicyclononenes
WO2024153789A1 (en) 2023-01-20 2024-07-25 Basf Se Stabilized biopolymer composition, their manufacture and use
WO2024191293A1 (en) 2023-03-10 2024-09-19 Tagworks Pharmaceuticals B.V. Trans-cyclooctene with improved t-linker
KR20260046464A (ko) 2023-07-27 2026-04-07 베락사 바이오테크 게엠베하 친수성 트랜스-시클로옥텐(hyTCO) 화합물, 이를 포함하는 구조체 및 접합체
WO2025056807A1 (en) 2023-09-15 2025-03-20 Basf Se Stabilized biopolymer composition, their manufacture and use
WO2025149667A1 (en) 2024-01-12 2025-07-17 Pheon Therapeutics Ltd Antibody drug conjugates and uses thereof
WO2025174248A1 (en) 2024-02-16 2025-08-21 Tagworks Pharmaceuticals B.V. Trans-cyclooctenes with "or gate" release
WO2026043376A1 (en) 2024-08-22 2026-02-26 Tagworks Pharmaceuticals B.V. Trans-cyclooctene formulations
WO2026078060A1 (en) 2024-10-08 2026-04-16 Basf Se Tocopherol alkoxylates for biopolymer stabilization

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0888301B1 (en) * 1996-03-08 2005-08-10 The Scripps Research Institute Mcbi analogs of cc-1065 and the duocarmycins
US5843937A (en) * 1996-05-23 1998-12-01 Panorama Research, Inc. DNA-binding indole derivatives, their prodrugs and immunoconjugates as anticancer agents
EP0934269A4 (en) * 1996-05-31 2000-01-12 Scripps Research Inst ANALOGS OF CC-1065 AND DUOCARMYCINE
WO1999019298A1 (en) * 1997-10-14 1999-04-22 The Scripps Research Institute iso-CBI AND iso-CI ANALOGS OF CC-1065 AND THE DUOCARMYCINS
JP3045706B1 (ja) * 1998-09-14 2000-05-29 科学技術振興事業団 Ｄｎａの特定塩基配列をアルキル化する化合物及びその合成法

Also Published As

Publication number Publication date
EP1320522B8 (en) 2006-02-01
EP1320522A2 (en) 2003-06-25
DE60115265D1 (de) 2005-12-29
WO2002030894A2 (en) 2002-04-18
US6660742B2 (en) 2003-12-09
ES2254492T3 (es) 2006-06-16
DK1320522T3 (da) 2006-04-03
WO2002030894A3 (en) 2002-06-20
EP1320522B1 (en) 2005-11-23
US20030073731A1 (en) 2003-04-17
DE60115265T2 (de) 2006-08-10
JP2004511466A (ja) 2004-04-15
CN1461298A (zh) 2003-12-10
CN1315805C (zh) 2007-05-16
ATE310724T1 (de) 2005-12-15

Similar Documents

Publication Publication Date Title
JP5010089B2 (ja) Ｃｃ−１０６５およびデュオカルマイシンのアキラルアナログの組成物およびその使用方法
JP5057273B2 (ja) イソインドリン−１−ワン誘導体
CN107556295B (zh) 喹唑啉衍生物及其制备方法
JP5608655B2 (ja) Ｐ２ｘ３受容体活性のモジュレーター
ES2443127T3 (es) Nuevos derivados tricíclicos o sales de éstos farmacéuticamente aceptables, su procedimiento de fabricación y composiciones farmacéuticas que los contienen
US20080200524A1 (en) Amide compounds as ion channel ligands and uses thereof
JP2019518754A (ja) フッ素化２−アミノ−４−（置換アミノ）フェニルカルバメート誘導体
KR101863708B1 (ko) 고혈압 및/또는 섬유증 치료용 조성물
CA3135921C (en) Quinolyl-containing compound and pharmaceutical composition, and use thereof
KR100810453B1 (ko) 신규한 인돌 유도체 및 이를 포함하는 약제
CN112979532B (zh) 邻苯二甲酰亚胺类化合物、制备方法和应用
WO2009140928A1 (zh) 二氢吲哚酮衍生物
KR20100132553A (ko) 신규한 ｎ-(2-아미노-페닐)-아크릴아미드
JP2011526936A (ja) 癌の処理のための新規オルト−アミノアニリド
JP2011500603A5 (https=)
KR19980032504A (ko) 포유류 세포의 성장 억제 방법
JP5330377B2 (ja) ３，４−ジヒドロキナゾリン誘導体
JP7815213B2 (ja) ベンジルアミン誘導体、その調製方法およびその用途
CN106496132B (zh) N-(4-取代苯基)-2-取代乙酰胺类化合物及其作为sirt2蛋白抑制剂的用途
CN115677666A (zh) 一种吲哚联嘧啶类化合物、其中间体、制备方法及其应用
CN116987073B (zh) 一种PI3Kα/HDAC6亚型选择性双重抑制剂及其应用
RU2803116C2 (ru) Хинолинил-содержащее соединение и его фармацевтическая композиция и применение
WO2025135111A1 (ja) 新規スルホンアミド誘導体
CN121064163A (zh) 一种苯并咪唑的异羟肟酸衍生物及其制备方法和应用
CN121779351A (zh) 含环丙烷结构的化合物及其制备方法和作为pd-1/pd-l1抑制剂的用途

Legal Events

Date Code Title Description
A711 Notification of change in applicant

Free format text: JAPANESE INTERMEDIATE CODE: A711

Effective date: 20060213

RD03 Notification of appointment of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7423

Effective date: 20060213

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A821

Effective date: 20060213

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20080916

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20080916

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20110810

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20110927

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20111220

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20120508

A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20120601

R150 Certificate of patent or registration of utility model

Ref document number: 5010089

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

Free format text: JAPANESE INTERMEDIATE CODE: R150

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20150608

Year of fee payment: 3

S111 Request for change of ownership or part of ownership

Free format text: JAPANESE INTERMEDIATE CODE: R313111

Free format text: JAPANESE INTERMEDIATE CODE: R313113

R360 Written notification for declining of transfer of rights

Free format text: JAPANESE INTERMEDIATE CODE: R360

R360 Written notification for declining of transfer of rights

Free format text: JAPANESE INTERMEDIATE CODE: R360

R371 Transfer withdrawn

Free format text: JAPANESE INTERMEDIATE CODE: R371

S111 Request for change of ownership or part of ownership

Free format text: JAPANESE INTERMEDIATE CODE: R313111

Free format text: JAPANESE INTERMEDIATE CODE: R313113

R350 Written notification of registration of transfer

Free format text: JAPANESE INTERMEDIATE CODE: R350

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

S111 Request for change of ownership or part of ownership

Free format text: JAPANESE INTERMEDIATE CODE: R313113

S531 Written request for registration of change of domicile

Free format text: JAPANESE INTERMEDIATE CODE: R313531

R350 Written notification of registration of transfer

Free format text: JAPANESE INTERMEDIATE CODE: R350

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

LAPS Cancellation because of no payment of annual fees