CN103140227B - 制备微管蛋白细胞溶素的方法 - Google Patents

制备微管蛋白细胞溶素的方法 Download PDF

Info

Publication number
CN103140227B
CN103140227B CN201180048479.0A CN201180048479A CN103140227B CN 103140227 B CN103140227 B CN 103140227B CN 201180048479 A CN201180048479 A CN 201180048479A CN 103140227 B CN103140227 B CN 103140227B
Authority
CN
China
Prior art keywords
compound
formula
alkyl
optionally substituted
cycloalkyl
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
CN201180048479.0A
Other languages
English (en)
Chinese (zh)
Other versions
CN103140227A (zh
Inventor
I.R.弗拉霍夫
M.格罗亚宁
P.J.克莱恩德尔
H.K.R.桑塔拉普拉姆
F.尤
Y.王
L.许
K.M.斯坦福德
A.里特
C.P.利蒙
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Endocyte Inc
Original Assignee
Endocyte Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Endocyte Inc filed Critical Endocyte Inc
Publication of CN103140227A publication Critical patent/CN103140227A/zh
Application granted granted Critical
Publication of CN103140227B publication Critical patent/CN103140227B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12PFERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
    • C12P21/00Preparation of peptides or proteins
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • C07D417/02Heterocyclic 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 two hetero rings
    • C07D417/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • Zoology (AREA)
  • Engineering & Computer Science (AREA)
  • Wood Science & Technology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Microbiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CN201180048479.0A 2010-08-06 2011-08-05 制备微管蛋白细胞溶素的方法 Expired - Fee Related CN103140227B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US37143310P 2010-08-06 2010-08-06
US61/371433 2010-08-06
PCT/US2011/046797 WO2012019123A1 (en) 2010-08-06 2011-08-05 Processes for preparing tubulysins

Publications (2)

Publication Number Publication Date
CN103140227A CN103140227A (zh) 2013-06-05
CN103140227B true CN103140227B (zh) 2016-01-20

Family

ID=45559842

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201180048479.0A Expired - Fee Related CN103140227B (zh) 2010-08-06 2011-08-05 制备微管蛋白细胞溶素的方法

Country Status (12)

Country Link
US (3) US8889880B2 (enExample)
EP (1) EP2600866A4 (enExample)
JP (1) JP2013535220A (enExample)
KR (1) KR20130096712A (enExample)
CN (1) CN103140227B (enExample)
AU (1) AU2011285532B2 (enExample)
BR (1) BR112013003004A2 (enExample)
CA (1) CA2807511A1 (enExample)
EA (1) EA025471B1 (enExample)
MX (1) MX2013001402A (enExample)
SG (1) SG187728A1 (enExample)
WO (1) WO2012019123A1 (enExample)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101098854B (zh) 2004-07-23 2012-12-05 恩多塞特公司 二价连接体及其轭合物
WO2008101231A2 (en) 2007-02-16 2008-08-21 Endocyte, Inc. Methods and compositions for treating and diagnosing kidney disease
NZ599239A (en) 2007-03-14 2013-10-25 Endocyte Inc Binding ligand linked drug delivery conjugates of tubulysins
US9877965B2 (en) 2007-06-25 2018-01-30 Endocyte, Inc. Vitamin receptor drug delivery conjugates for treating inflammation
US9138484B2 (en) 2007-06-25 2015-09-22 Endocyte, Inc. Conjugates containing hydrophilic spacer linkers
US9187521B2 (en) 2007-10-25 2015-11-17 Endocyte, Inc. Tubulysins and processes for preparing
CA2807511A1 (en) 2010-08-06 2012-02-09 Endocyte, Inc. Processes for preparing tubulysins
WO2013126797A1 (en) 2012-02-24 2013-08-29 Purdue Research Foundation Cholecystokinin b receptor targeting for imaging and therapy
US20140080175A1 (en) * 2012-03-29 2014-03-20 Endocyte, Inc. Processes for preparing tubulysin derivatives and conjugates thereof
US9662402B2 (en) 2012-10-16 2017-05-30 Endocyte, Inc. Drug delivery conjugates containing unnatural amino acids and methods for using
KR102575825B1 (ko) 2012-11-15 2023-09-06 엔도사이트, 인코포레이티드 Psma 발현 세포에 의해 야기되는 질병을 치료하기 위한 컨쥬게이트
US20140249315A1 (en) 2013-03-01 2014-09-04 Endocyte, Inc. Processes for preparing tubulysins
JP6664329B2 (ja) * 2014-01-28 2020-03-13 トゥーベ・ファルマシューティカルズ・ゲー・エム・ベー・ハー コンジュゲーションのための新規な細胞毒性チューブリシン化合物
HK1232127A1 (zh) 2014-04-11 2018-01-05 Medimmune, Llc 双特异性her2抗体
EP3200829B1 (en) 2014-10-01 2023-12-06 Medimmune, LLC Method of conjugating a polypeptide
JP2018509404A (ja) 2015-02-25 2018-04-05 ウィリアム マーシュ ライス ユニバーシティWilliam Marsh Rice University デスアセトキシツブリシンhおよびその類似体
ES2959663T3 (es) 2015-11-10 2024-02-27 Medimmune Llc Moléculas de unión específicas para ASCT2 y usos de las mismas
US11229708B2 (en) 2015-12-04 2022-01-25 Seagen Inc. Conjugates of quaternized tubulysin compounds
US11793880B2 (en) 2015-12-04 2023-10-24 Seagen Inc. Conjugates of quaternized tubulysin compounds
CN108495653A (zh) 2016-01-27 2018-09-04 免疫医疗有限责任公司 用于制备具有定义的糖基化模式抗体的方法
US10961311B2 (en) 2016-04-15 2021-03-30 Macrogenics, Inc. B7-H3 binding molecules, antibody drug conjugates thereof and methods of use thereof
AR111963A1 (es) 2017-05-26 2019-09-04 Univ California Método y moléculas
SG11202000499RA (en) 2017-08-01 2020-02-27 Medimmune Llc Bcma monoclonal antibody-drug conjugate
US11274124B2 (en) 2017-11-29 2022-03-15 William Marsh Rice University Tubulysin analogues as anticancer agents and payloads for antibody-drug conjugates and methods of treatment therewith
WO2022053650A1 (en) 2020-09-11 2022-03-17 Medimmune Limited Therapeutic b7-h4 binding molecules
US11807685B2 (en) 2021-08-05 2023-11-07 The Uab Research Foundation Anti-CD47 antibody and uses thereof
AU2022384597A1 (en) 2021-11-10 2024-06-13 Astrazeneca Ab Antibody molecules and conjugates
GB202117928D0 (en) 2021-12-11 2022-01-26 Cancer Research Tech Ltd Immunotherapy for cancer
MX2024010956A (es) 2022-03-09 2024-09-17 Astrazeneca Ab Moleculas de union contra fra.
IL317733A (en) 2022-06-27 2025-02-01 Astrazeneca Ab Combinations involving epidermal growth factor receptor tyrosine kinase inhibitors for cancer treatment
WO2024170660A1 (en) 2023-02-16 2024-08-22 Astrazeneca Ab Combination therapies for treatment of cancer with therapeutic binding molecules

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5627165A (en) 1990-06-13 1997-05-06 Drug Innovation & Design, Inc. Phosphorous prodrugs and therapeutic delivery systems using same
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
DE10254439A1 (de) 2002-11-21 2004-06-03 GESELLSCHAFT FüR BIOTECHNOLOGISCHE FORSCHUNG MBH (GBF) Tubulysine, Herstellungsverfahren und Tubulysin-Mittel
AR042942A1 (es) 2003-01-27 2005-07-06 Endocyte Inc Conjugados de administracion de drogas de union de receptores de vitaminas
NZ599239A (en) 2007-03-14 2013-10-25 Endocyte Inc Binding ligand linked drug delivery conjugates of tubulysins
DE102009032972A1 (de) 2009-07-14 2011-01-20 Erbe Elektromedizin Gmbh Vorrichtung zur Herstellung von Anastomosen
WO2011069116A1 (en) 2009-12-04 2011-06-09 Endocyte, Inc. Binding ligand linked drug delivery conjugates of tubulysins
US20120322741A1 (en) 2010-02-25 2012-12-20 Purdue Research Foundation Psma binding ligand-linker conjugates and methods for using
CA2807511A1 (en) 2010-08-06 2012-02-09 Endocyte, Inc. Processes for preparing tubulysins

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
The Total Synthesis of Tubulysin D;Hillary M. Peltier, et al;《J. AM. CHEM. SOC.》;20061201;第128卷;16018-16019 *

Also Published As

Publication number Publication date
CA2807511A1 (en) 2012-02-09
JP2013535220A (ja) 2013-09-12
AU2011285532A1 (en) 2013-02-21
AU2011285532B2 (en) 2015-09-10
WO2012019123A1 (en) 2012-02-09
US9499849B2 (en) 2016-11-22
CN103140227A (zh) 2013-06-05
EA025471B1 (ru) 2016-12-30
BR112013003004A2 (pt) 2016-06-14
US9273091B2 (en) 2016-03-01
MX2013001402A (es) 2013-08-29
EP2600866A4 (en) 2013-12-11
US8889880B2 (en) 2014-11-18
KR20130096712A (ko) 2013-08-30
EA201390203A1 (ru) 2013-08-30
US20150225447A1 (en) 2015-08-13
HK1185558A1 (zh) 2014-02-21
EP2600866A1 (en) 2013-06-12
US20130137139A1 (en) 2013-05-30
SG187728A1 (en) 2013-03-28
US20160177363A1 (en) 2016-06-23

Similar Documents

Publication Publication Date Title
CN103140227B (zh) 制备微管蛋白细胞溶素的方法
US9771391B2 (en) Process for preparing tubulysins
EP2831059B1 (en) Processes for preparing tubulysin derivatives and conjugates thereof
Dahiya Synthesis, characterization and antimicrobial studies on some newer imidazole analogs
CN110117293B (zh) 多氟取代的Largazole类似物、其制备方法和用途
JP2006527173A (ja) コルヒチン類似体
US7365055B2 (en) Derivatives of morphine-6-glucuronide, pharmaceutical compositions containing them, their preparation method and their uses
HK1185558B (en) Processes for preparing tubulysins
US5151521A (en) 1-aminoethyl phosphonic acid derivatives
JPS59199693A (ja) インドリルグリシルセフアロスポリン誘導体
JP6570034B2 (ja) 新規なグルタミン酸誘導体およびその用途
AU2013203491A1 (en) Processes for preparing tubulysins
KR970004044B1 (ko) 약물동력학적으로 개선된 세팔로스포린 유도체, 그의 제조방법, 그를 함유하는 약제학적 조성물 및 합성 중간체
KR100450607B1 (ko) 가라민 유도체의 제조방법
JP2023084946A (ja) 生理活性を有する新規化合物
WO2025169980A1 (ja) テストステロンの産生/分泌を調節するための環状ペプチド誘導体組成物
WO1999021867A1 (fr) Derives d'erythromycine a
JPWO1999021867A1 (ja) エリスロマイシンa誘導体
IT8422036A1 (it) Derivati dell'1,3-diossano, procedimento per la loro preparazione composizioni farmaceutiche

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1185558

Country of ref document: HK

C14 Grant of patent or utility model
GR01 Patent grant
REG Reference to a national code

Ref country code: HK

Ref legal event code: GR

Ref document number: 1185558

Country of ref document: HK

CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20160120

Termination date: 20170805

CF01 Termination of patent right due to non-payment of annual fee