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SMT201400183B - Composti antiproliferativi, loro coniugati, metodiper gli stessi e loro usi - Google Patents

Composti antiproliferativi, loro coniugati, metodiper gli stessi e loro usi

Info

Publication number
SMT201400183B
SMT201400183B SM201400183T SM201400183T SMT201400183B SM T201400183 B SMT201400183 B SM T201400183B SM 201400183 T SM201400183 T SM 201400183T SM 201400183 T SM201400183 T SM 201400183T SM T201400183 B SMT201400183 B SM T201400183B
Authority
SM
San Marino
Prior art keywords
conjugates
methods
same
antiproliferative compounds
antiproliferative
Prior art date
Application number
SM201400183T
Other languages
English (en)
Inventor
Heng Cheng
Qiang Cong
Sanjeev Gangwar
Qian Zhan
Original Assignee
Medarex Llc
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 Medarex Llc filed Critical Medarex Llc
Publication of SMT201400183B publication Critical patent/SMT201400183B/it

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/12Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04Linear peptides containing only normal peptide links
    • C07K7/06Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/06Tripeptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6801Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/6811Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6801Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/6811Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
    • A61K47/6817Toxins
    • A61K47/6829Bacterial toxins, e.g. diphteria toxins or Pseudomonas exotoxin A
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/04Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C229/06Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton
    • C07C229/10Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings
    • C07C229/14Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings to carbon atoms of carbon skeletons containing rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/04Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C229/06Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton
    • C07C229/10Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings
    • C07C229/16Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings to carbon atoms of hydrocarbon radicals substituted by amino or carboxyl groups, e.g. ethylenediamine-tetra-acetic acid, iminodiacetic acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/021Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)n-C(=0)-, n being 5 or 6; for n > 6, classification in C07K5/06 - C07K5/10, according to the moiety having normal peptide bonds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10Tetrapeptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Immunology (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Epidemiology (AREA)
  • Toxicology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicinal Preparation (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Steroid Compounds (AREA)
SM201400183T 2009-08-03 2014-12-11 Composti antiproliferativi, loro coniugati, metodiper gli stessi e loro usi SMT201400183B (it)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US23093209P 2009-08-03 2009-08-03
US23288309P 2009-08-11 2009-08-11
PCT/US2010/044078 WO2011017249A1 (en) 2009-08-03 2010-08-02 Antiproliferative compounds, conjugates thereof, methods therefor, and uses thereof

Publications (1)

Publication Number Publication Date
SMT201400183B true SMT201400183B (it) 2015-01-15

Family

ID=42782224

Family Applications (1)

Application Number Title Priority Date Filing Date
SM201400183T SMT201400183B (it) 2009-08-03 2014-12-11 Composti antiproliferativi, loro coniugati, metodiper gli stessi e loro usi

Country Status (29)

Country Link
US (6) US8394922B2 (it)
EP (1) EP2461830B1 (it)
JP (1) JP5859964B2 (it)
KR (1) KR101759359B1 (it)
CN (2) CN102725001B (it)
AR (1) AR077701A1 (it)
AU (1) AU2010279674B2 (it)
BR (1) BR112012002615A2 (it)
CA (1) CA2770042C (it)
CL (1) CL2012000302A1 (it)
CO (1) CO6501196A2 (it)
DK (1) DK2461830T3 (it)
EA (1) EA022288B1 (it)
ES (1) ES2525351T3 (it)
HK (1) HK1164751A1 (it)
HR (1) HRP20140976T1 (it)
HU (1) HUE026997T2 (it)
IL (1) IL217717A (it)
IN (1) IN2012DN00860A (it)
MX (1) MX2012001665A (it)
NZ (1) NZ597985A (it)
PE (1) PE20121087A1 (it)
PL (1) PL2461830T3 (it)
PT (1) PT2461830E (it)
SG (2) SG10201503332XA (it)
SI (1) SI2461830T1 (it)
SM (1) SMT201400183B (it)
TW (1) TWI469794B (it)
WO (1) WO2011017249A1 (it)

Families Citing this family (86)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1789391B1 (en) 2004-07-23 2017-06-28 Endocyte, Inc. Bivalent linkers and conjugates thereof
NZ599239A (en) 2007-03-14 2013-10-25 Endocyte Inc Binding ligand linked drug delivery conjugates of tubulysins
EP2176293B1 (en) 2007-06-25 2019-04-03 Endocyte, Inc. Conjugates containing hydrophilic spacer linkers
US9877965B2 (en) 2007-06-25 2018-01-30 Endocyte, Inc. Vitamin receptor drug delivery conjugates for treating inflammation
NZ583931A (en) 2007-08-17 2012-06-29 Purdue Research Foundation Psma binding ligand-linker conjugates and methods for using
IT1394860B1 (it) * 2009-07-22 2012-07-20 Kemotech S R L Composti farmaceutici
US8394922B2 (en) 2009-08-03 2013-03-12 Medarex, Inc. Antiproliferative compounds, conjugates thereof, methods therefor, and uses thereof
US9951324B2 (en) 2010-02-25 2018-04-24 Purdue Research Foundation PSMA binding ligand-linker conjugates and methods for using
MX336540B (es) 2010-06-08 2016-01-22 Genentech Inc Conjugados y anticuerpos manipulados geneticamente con cisteina.
ES2865449T3 (es) * 2011-03-16 2021-10-15 Hoffmann La Roche Cromatografía de intercambio iónico con selectividad mejorada para la separación de monómeros, agregados y fragmentos polipeptídicos por modulación de la fase móvil
DK2717916T3 (en) 2011-06-10 2017-04-24 Mersana Therapeutics Inc PROTEIN POLYMER-drug conjugates
US10080805B2 (en) 2012-02-24 2018-09-25 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
JP6280103B2 (ja) * 2012-05-15 2018-02-14 ソレント・セラピューティクス・インコーポレイテッドSorrento Therapeutics, Inc. 薬物コンジュゲート、コンジュゲーション方法およびその使用
LT3210627T (lt) * 2012-07-12 2023-04-11 Hangzhou Dac Biotech Co., Ltd Ląsteles surišančiųjų molekulių konjugatai su citotoksinėmis medžiagomis
US11873281B2 (en) 2012-07-12 2024-01-16 Hangzhou Dac Biotech Co., Ltd. Conjugates of cell binding molecules with cytotoxic agents
EP2708243A1 (en) 2012-09-17 2014-03-19 OntoChem GmbH Receptor ligand linked cytotoxic molecules
EA201590622A1 (ru) 2012-10-16 2015-10-30 Эндосайт, Инк. Конъюгаты для доставки лекарственного средства, содержащие не встречающиеся в природе аминокислоты, и способы применения
KR102318999B1 (ko) 2012-11-15 2021-10-29 엔도사이트, 인코포레이티드 Psma 발현 세포에 의해 야기되는 질병을 치료하기 위한 컨쥬게이트
WO2014080251A1 (en) 2012-11-24 2014-05-30 Hangzhou Dac Biotech Co., Ltd. Hydrophilic linkers and their uses for conjugation of drugs to cell binding molecules
WO2014093394A1 (en) 2012-12-10 2014-06-19 Mersana Therapeutics, Inc. Protein-polymer-drug conjugates
EP2931316B1 (en) 2012-12-12 2019-02-20 Mersana Therapeutics, Inc. Hydroxyl-polymer-drug-protein conjugates
RS56169B1 (sr) 2013-02-14 2017-11-30 Bristol Myers Squibb Co Jedinjenja tubulisina, metode pripreme i primena
US20140249315A1 (en) 2013-03-01 2014-09-04 Endocyte, Inc. Processes for preparing tubulysins
CA2906784C (en) 2013-03-15 2023-02-28 The Centre For Drug Research And Development Cytotoxic and anti-mitotic compounds, and methods of using the same
JP6171435B2 (ja) * 2013-03-18 2017-08-02 富士通株式会社 半導体装置及びその製造方法、電源装置、高周波増幅器
US10781259B2 (en) 2013-06-06 2020-09-22 Magenta Therapeutics, Inc. Modified antibodies and related compounds, compositions, and methods of use
WO2015057585A1 (en) * 2013-10-14 2015-04-23 Regents Of The University Of Minnesota Therapeutic compounds
FI4095130T3 (fi) 2013-10-18 2024-04-25 Novartis Ag Prostataspesifisen membraaniantigeenin (psma) leimattuja estäjiä, niiden käyttö kuvantamisaineina ja farmaseuttisia aineita eturauhassyövän hoitoon
WO2015074792A1 (en) 2013-11-25 2015-05-28 Ontochem Gmbh Method for diagnosing g-protein coupled receptor-related diseases
SG11201605260VA (en) 2013-12-27 2016-07-28 Zymeworks Inc Var2csa-drug conjugates
JP6560681B2 (ja) 2013-12-27 2019-08-14 ザイムワークス インコーポレイティド 薬物結合体のためのスルホンアミド含有連結系
CA2940311C (en) * 2014-01-28 2022-12-13 Tube Pharmaceuticals Gmbh Cytotoxic tubulysin compounds for conjugation
WO2015127685A1 (en) 2014-02-28 2015-09-03 Hangzhou Dac Biotech Co., Ltd Charged linkers and their uses for conjugation
WO2015135659A1 (en) 2014-03-14 2015-09-17 Ontochem Gmbh Receptor ligand linked cytotoxic molecules
ES2750563T3 (es) 2014-03-20 2020-03-26 Bristol Myers Squibb Co Moléculas con una estructura basada en fibronectina estabilizada
CN106458942A (zh) * 2014-04-11 2017-02-22 麦迪穆有限责任公司 微管溶素衍生物
JP6539729B2 (ja) * 2014-06-03 2019-07-03 ジアリー・ファーマシューティカルズ・インコーポレイテッドJiaray Pharmaceuticals, Inc. ペプチド−薬物複合体
CN104262455B (zh) * 2014-08-22 2017-05-03 亚飞(上海)生物医药科技有限公司 肿瘤微环境靶向激活的紫杉醇衍生物及其制备和用途
EP3184540A4 (en) 2014-08-22 2018-03-21 Yafei Shanghai Biolog Medicine Science& Technology Specifically activated micromolecular target coupling body in tumor microenvironment and use thereof
CA2959424C (en) * 2014-09-11 2023-10-31 Seattle Genetics, Inc. Targeted delivery of tertiary amine-containing drug substances
AU2015314826A1 (en) 2014-09-12 2017-03-02 Genentech, Inc. Cysteine engineered antibodies and conjugates
CN113416229A (zh) 2014-09-17 2021-09-21 酵活有限公司 细胞毒性和抗有丝分裂化合物、及其使用方法
US10077287B2 (en) 2014-11-10 2018-09-18 Bristol-Myers Squibb Company Tubulysin analogs and methods of making and use
EP3789399A1 (en) 2014-11-21 2021-03-10 Bristol-Myers Squibb Company Antibodies comprising modified heavy constant regions
ES2807182T3 (es) 2014-11-21 2021-02-22 Bristol Myers Squibb Co Anticuerpos frente a CD73 y sus usos
WO2016086021A1 (en) 2014-11-25 2016-06-02 Bristol-Myers Squibb Company Novel pd-l1 binding polypeptides for imaging
US10188759B2 (en) 2015-01-07 2019-01-29 Endocyte, Inc. Conjugates for imaging
AU2016222575A1 (en) 2015-02-25 2017-09-07 William Marsh Rice University Desacetoxytubulysin H and analogs thereof
US10676773B2 (en) 2015-03-10 2020-06-09 Bristol-Myers Squibb Company Antibodies conjugatable by transglutaminase and conjugates made therefrom
SG10202008304TA (en) 2015-05-29 2020-10-29 Bristol Myers Squibb Co Antibodies against ox40 and uses thereof
WO2015151081A2 (en) 2015-07-12 2015-10-08 Suzhou M-Conj Biotech Co., Ltd Bridge linkers for conjugation of a cell-binding molecule
US9839687B2 (en) 2015-07-15 2017-12-12 Suzhou M-Conj Biotech Co., Ltd. Acetylenedicarboxyl linkers and their uses in specific conjugation of a cell-binding molecule
KR20180057657A (ko) 2015-09-23 2018-05-30 브리스톨-마이어스 스큅 컴퍼니 글리피칸-3-결합 피브로넥틴 기반 스캐폴드 분자
KR101897872B1 (ko) * 2015-09-24 2018-09-12 주식회사 엘지화학 화합물 및 이를 포함하는 유기 발광 소자
JP6412906B2 (ja) 2015-11-03 2018-10-24 財團法人工業技術研究院Industrial Technology Research Institute 化合物、リンカー−薬物およびリガンド−薬物複合体
US11793880B2 (en) 2015-12-04 2023-10-24 Seagen Inc. Conjugates of quaternized tubulysin compounds
TWI852735B (zh) 2015-12-04 2024-08-11 美商思進公司 四級胺化妥布賴森(tubulysin)化合物之結合物
WO2017112624A1 (en) 2015-12-21 2017-06-29 Bristol-Myers Squibb Company Variant antibodies for site-specific conjugation
EP3411371A1 (en) 2016-02-01 2018-12-12 Pfizer Inc Tubulysin analogs and methods for their preparation
SG10201913033UA (en) 2016-03-04 2020-03-30 Bristol Myers Squibb Co Combination therapy with anti-cd73 antibodies
CN109620949A (zh) * 2016-03-13 2019-04-16 曹帅 一种用于治疗骨癌的药物组合物
EP3454909A1 (en) 2016-05-10 2019-03-20 Bristol-Myers Squibb Company Antibody-drug conjugates of tubulysin analogs with enhanced stability
US20170326249A1 (en) * 2016-05-10 2017-11-16 Bristol-Myers Squibb Company Antibody-drug conjugate of an anti-glypican-3 antibody and a tubulysin analog, preparation and uses
US10106560B2 (en) 2016-06-16 2018-10-23 Bristol-Myers Squibb Company Process and intermediates for making tubulysin analogs
WO2018035391A1 (en) 2016-08-19 2018-02-22 Bristol-Myers Squibb Company Seco-cyclopropapyrroloindole compounds, antibody-drug conjugates thereof, and methods of making and use
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
US10517958B2 (en) 2016-10-04 2019-12-31 Zymeworks Inc. Compositions and methods for the treatment of platinum-drug resistant cancer
US10398783B2 (en) 2016-10-20 2019-09-03 Bristol-Myers Squibb Company Antiproliferative compounds and conjugates made therefrom
KR20220147720A (ko) 2016-11-14 2022-11-03 항저우 디에이씨 바이오테크 씨오, 엘티디 결합 링커, 그러한 결합 링커를 함유하는 세포 결합 분자-약물 결합체, 링커를 갖는 그러한 결합체의 제조 및 사용
JP6585650B2 (ja) * 2017-03-23 2019-10-02 ハンヂョウ ディーエイシー バイオテック カンパニー リミテッド 細胞毒性剤と細胞結合受容体との共役体
SG10201913206RA (en) 2017-05-25 2020-02-27 Bristol Myers Squibb Co Antibodies comprising modified heavy constant regions
WO2019108685A1 (en) * 2017-11-29 2019-06-06 William March Rice University Tubulysin analogues as anticancer agents and payloads for antibody-drug conjugates and methods of treatment therewith
WO2019209811A1 (en) 2018-04-24 2019-10-31 Bristol-Myers Squibb Company Macrocyclic toll-like receptor 7 (tlr7) agonists
CN112188902A (zh) 2018-05-29 2021-01-05 百时美施贵宝公司 用于前药和缀合物的经修饰的自消灭部分以及使用和制造方法
US11020490B2 (en) 2018-06-22 2021-06-01 Bristol-Myers Squibb Company Antibody-drug conjugate with a tubulysin analog warhead having a stabilized acetate group in the TUV subunit
WO2020112781A1 (en) 2018-11-28 2020-06-04 Bristol-Myers Squibb Company Antibodies comprising modified heavy constant regions
ES2943474T3 (es) 2018-11-30 2023-06-13 Bristol Myers Squibb Co Anticuerpo que comprende una extensión carboxiterminal de una cadena ligera que contiene glutamina, conjugados del mismo, y métodos y usos
US20220031860A1 (en) 2018-12-12 2022-02-03 Bristol-Myers Squibb Company Antibodies modified for transglutaminase conjugation, conjugates thereof, and methods and uses
CN113454097B (zh) 2018-12-21 2024-08-30 里珍纳龙药品有限公司 微管溶素及蛋白质-微管溶素偶联物
JP6842127B2 (ja) * 2019-05-22 2021-03-17 ハンヂョウ ディーエイシー バイオテック カンパニー リミテッド 細胞毒性剤と細胞結合受容体との共役体
CN114040778A (zh) 2019-06-29 2022-02-11 杭州多禧生物科技有限公司 一种细胞结合分子-Tubulysin衍生物偶联物及其制备方法
WO2021055306A1 (en) 2019-09-16 2021-03-25 Bristol-Myers Squibb Company Dual capture method for analysis of antibody-drug conjugates
CN113387829B (zh) * 2020-03-13 2023-04-07 凯特立斯(深圳)科技有限公司 一种沙库必曲的制备方法
WO2021262910A2 (en) * 2020-06-24 2021-12-30 Regeneron Pharmaceuticals, Inc. Tubulysins and protein-tubulysin conjugates
JP7044419B2 (ja) * 2021-02-04 2022-03-30 ハンヂョウ ディーエイシー バイオテック カンパニー リミテッド 細胞毒性剤と細胞結合受容体との共役体

Family Cites Families (73)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1981001145A1 (en) 1979-10-18 1981-04-30 Univ Illinois Hydrolytic enzyme-activatible pro-drugs
US4475196A (en) 1981-03-06 1984-10-02 Zor Clair G Instrument for locating faults in aircraft passenger reading light and attendant call control system
US4447233A (en) 1981-04-10 1984-05-08 Parker-Hannifin Corporation Medication infusion pump
US5144011A (en) 1981-06-26 1992-09-01 Boston University Acidity-sensitive spacer molecule to control the release of pharmaceuticals from molecular carriers
US4631190A (en) 1981-06-26 1986-12-23 Shen Wei C Acidity-sensitive spacer molecule to control the release of pharmaceuticals from molecular carriers
US4439196A (en) 1982-03-18 1984-03-27 Merck & Co., Inc. Osmotic drug delivery system
US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
US4447224A (en) 1982-09-20 1984-05-08 Infusaid Corporation Variable flow implantable infusion apparatus
US4487603A (en) 1982-11-26 1984-12-11 Cordis Corporation Implantable microinfusion pump system
US4486194A (en) 1983-06-08 1984-12-04 James Ferrara Therapeutic device for administering medicaments through the skin
US4698420A (en) 1985-02-25 1987-10-06 Xoma Corporation Antibody hybrid molecules and process for their preparation
US4596556A (en) 1985-03-25 1986-06-24 Bioject, Inc. Hypodermic injection apparatus
US5374548A (en) 1986-05-02 1994-12-20 Genentech, Inc. Methods and compositions for the attachment of proteins to liposomes using a glycophospholipid anchor
MX9203291A (es) 1985-06-26 1992-08-01 Liposome Co Inc Metodo para acoplamiento de liposomas.
US4941880A (en) 1987-06-19 1990-07-17 Bioject, Inc. Pre-filled ampule and non-invasive hypodermic injection device assembly
US4790824A (en) 1987-06-19 1988-12-13 Bioject, Inc. Non-invasive hypodermic injection device
US5108921A (en) 1989-04-03 1992-04-28 Purdue Research Foundation Method for enhanced transmembrane transport of exogenous molecules
US5064413A (en) 1989-11-09 1991-11-12 Bioject, Inc. Needleless hypodermic injection device
US5312335A (en) 1989-11-09 1994-05-17 Bioject Inc. Needleless hypodermic injection device
US5383851A (en) 1992-07-24 1995-01-24 Bioject Inc. Needleless hypodermic injection device
US6214345B1 (en) 1993-05-14 2001-04-10 Bristol-Myers Squibb Co. Lysosomal enzyme-cleavable antitumor drug conjugates
TW420681B (en) 1995-12-08 2001-02-01 Lederle Japan Ltd Carbapenem-3-carboxylic acid ester derivatives
DE19638870B4 (de) 1996-09-23 2009-05-14 Helmholtz-Zentrum für Infektionsforschung GmbH Tubulysine, Verfahren zu ihrer Gewinnung und sie enthaltende Mittel
US7214487B2 (en) 1998-06-26 2007-05-08 Sunesis Pharmaceuticals, Inc. Methods for identifying compounds that modulate enzymatic activities by employing covalently bonded target-extender complexes with ligand candidates
DK1212422T3 (da) * 1999-08-24 2007-07-02 Medarex Inc Humane CTLA-4-antistoffer og anvendelserne deraf
DE10008089A1 (de) 2000-02-22 2001-10-31 Biotechnolog Forschung Gmbh Syntheseverfahren zur Herstellung von Tubulysinen
PE20020908A1 (es) * 2001-03-21 2002-10-26 Cell Therapeutics Inc Produccion recombinante de polimeros polianionicos y uso de de los mismos
US7087600B2 (en) * 2001-05-31 2006-08-08 Medarex, Inc. Peptidyl prodrugs and linkers and stabilizers useful therefor
US7091186B2 (en) 2001-09-24 2006-08-15 Seattle Genetics, Inc. p-Amidobenzylethers in drug delivery agents
NZ534174A (en) * 2002-01-09 2007-03-30 Medarex Inc An isolated human monoclonal antibody which binds to human CD30
AU2003253048A1 (en) * 2002-07-09 2004-01-23 Morphochem Aktiengellschaft Fur Kombinatorische Chemie Tubulysin conjugates
AU2003266233A1 (en) * 2002-07-09 2004-01-23 Morphochem Aktiengesellschaft Fur Kombinatorische Chemie Novel tubulysin analogues
DE10241152A1 (de) * 2002-09-05 2004-03-18 GESELLSCHAFT FüR BIOTECHNOLOGISCHE FORSCHUNG MBH (GBF) Tubulysin-Biosynthese-Gene
FR2845630B1 (fr) * 2002-10-09 2005-09-30 Helitest Ags Dispositif de demasticage, notamment pour la refection de joints dans des structures de reservoirs d'aeronefs et container d'intervention
DE10254439A1 (de) * 2002-11-21 2004-06-03 GESELLSCHAFT FüR BIOTECHNOLOGISCHE FORSCHUNG MBH (GBF) Tubulysine, Herstellungsverfahren und Tubulysin-Mittel
ES2340494T3 (es) 2003-04-15 2010-06-04 Glaxosmithkline Llc Mutantes de sustitucion de il-18 humana y sus conjugados.
NZ544911A (en) * 2003-07-22 2008-12-24 Schering Ag RG1 antibodies and uses thereof
CA2556752C (en) 2004-02-23 2016-02-02 Genentech, Inc. Heterocyclic self-immolative linkers and conjugates
RU2402548C2 (ru) * 2004-05-19 2010-10-27 Медарекс, Инк. Химические линкеры и их конъюгаты
MXPA06013413A (es) * 2004-05-19 2007-01-23 Medarex Inc Enlazadores quimicos y conjugados de los mismos.
US7541330B2 (en) 2004-06-15 2009-06-02 Kosan Biosciences Incorporated Conjugates with reduced adverse systemic effects
DE102004030227A1 (de) 2004-06-23 2006-01-26 Dömling, Alexander, Dr. Wirkstoffe mit antiangiogenetischen Eigenschaften
KR101270829B1 (ko) 2004-09-23 2013-06-07 제넨테크, 인크. 시스테인 유전자조작 항체 및 접합체
AU2006214031A1 (en) * 2005-02-18 2006-08-24 Medarex, Inc. Human monoclonal antibodies to prostate specific membrane antigen (PSMA)
US7714016B2 (en) * 2005-04-08 2010-05-11 Medarex, Inc. Cytotoxic compounds and conjugates with cleavable substrates
CA3151350A1 (en) 2005-05-09 2006-11-16 E. R. Squibb & Sons, L.L.C. Human monoclonal antibodies to programmed death 1 (pd-1) and methods for treating cancer using anti-pd-1 antibodies alone or in combination with other immunotherapeutics
EP1899379B1 (en) * 2005-06-20 2018-04-11 E. R. Squibb & Sons, L.L.C. Cd19 antibodies and their uses
KR101364912B1 (ko) * 2005-08-19 2014-02-21 엔도사이트, 인코포레이티드 복수-약제 리간드 공액체
US8124738B2 (en) * 2005-09-26 2012-02-28 Medarex, Inc. Human monoclonal antibodies to CD70
ES2416136T3 (es) * 2005-09-26 2013-07-30 Medarex, Inc. Conjugados de anticuerpo-fármaco y su uso
RS52100B (en) * 2005-10-26 2012-06-30 Medarex, Inc. PROCEDURES AND UNITS FOR PREPARING ANALOG CC-1065
CA2627190A1 (en) * 2005-11-10 2007-05-24 Medarex, Inc. Duocarmycin derivatives as novel cytotoxic compounds and conjugates
EP1963371A2 (en) * 2005-12-08 2008-09-03 Medarex Inc. Human monoclonal antibodies to o8e
KR101373464B1 (ko) * 2005-12-08 2014-03-14 메다렉스, 엘.엘.시. 단백질 티로신 키나제 7(ptk7)에 대한 인간 단일클론항체 및 그의 용도
CN101626782B (zh) 2006-12-01 2013-03-27 梅达雷克斯公司 结合cd22的人抗体及其用途
JP2010513306A (ja) 2006-12-14 2010-04-30 メダレックス インコーポレーティッド Cd70に結合するヒト抗体およびその使用
UY30776A1 (es) * 2006-12-21 2008-07-03 Medarex Inc Anticuerpos cd44
TWI412367B (zh) 2006-12-28 2013-10-21 Medarex Llc 化學鏈接劑與可裂解基質以及其之綴合物
JP2010516625A (ja) * 2007-01-24 2010-05-20 インサート セラピューティクス, インコーポレイテッド 制御された薬物送達のためのテザー基を有するポリマー−薬物コンジュゲート
CA2678514A1 (en) * 2007-02-21 2008-08-28 Medarex, Inc. Chemical linkers with single amino acids and conjugates thereof
US20100047841A1 (en) * 2007-02-27 2010-02-25 University Of Pittsburgh-Of The Commonwealth System Of Higher Education Synthesis of desacetoxytubulysin h and analogs thereof
NZ599239A (en) * 2007-03-14 2013-10-25 Endocyte Inc Binding ligand linked drug delivery conjugates of tubulysins
ES2463693T3 (es) 2007-05-10 2014-05-29 R & D Biopharmaceuticals Gmbh Derivados de tubulisina
EP2176293B1 (en) 2007-06-25 2019-04-03 Endocyte, Inc. Conjugates containing hydrophilic spacer linkers
US7387981B1 (en) 2007-06-28 2008-06-17 Lyondell Chemical Technology, L.P. Direct epoxidation catalyst and process
WO2009012958A2 (en) 2007-07-20 2009-01-29 Helmholtz-Zentrum für Infektionsforschung GmbH Tubulysin d analogues
NZ583931A (en) 2007-08-17 2012-06-29 Purdue Research Foundation Psma binding ligand-linker conjugates and methods for using
WO2009026274A1 (en) 2007-08-22 2009-02-26 Medarex, Inc. Site-specific attachment of drugs or other agents to engineered antibodies with c-terminal extensions
CA2700860C (en) 2007-10-01 2016-07-19 Jonathan A. Terrett Human antibodies that bind mesothelin, and uses thereof
WO2009055562A1 (en) 2007-10-25 2009-04-30 Endocyte, Inc. Tubulysins and processes for preparing
EP2174947A1 (en) 2008-09-25 2010-04-14 Universität des Saarlandes Bioactive pre-tubulysins and use thereof
US8394922B2 (en) 2009-08-03 2013-03-12 Medarex, Inc. Antiproliferative compounds, conjugates thereof, methods therefor, and uses thereof
WO2011057805A1 (en) * 2009-11-12 2011-05-19 R&D Biopharmaceuticals Gmbh Tubulin inhibitors

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