AU2011285532B2 - Processes for preparing tubulysins - Google Patents

Processes for preparing tubulysins Download PDF

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Publication number
AU2011285532B2
AU2011285532B2 AU2011285532A AU2011285532A AU2011285532B2 AU 2011285532 B2 AU2011285532 B2 AU 2011285532B2 AU 2011285532 A AU2011285532 A AU 2011285532A AU 2011285532 A AU2011285532 A AU 2011285532A AU 2011285532 B2 AU2011285532 B2 AU 2011285532B2
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AU
Australia
Prior art keywords
compound
formula
optionally substituted
alkyl
treating
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.)
Ceased
Application number
AU2011285532A
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English (en)
Other versions
AU2011285532A1 (en
Inventor
Michael Groaning
Paul Joseph Kleindl
Christopher Paul Leamon
Allen Ritter
Hari Krishna R. Santhapuram
Katheryn Marie Stanford
Iontcho Radoslavov Vlahov
Yu Wang
Le-Cun Xu
Fei You
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 AU2011285532A1 publication Critical patent/AU2011285532A1/en
Priority to AU2013203491A priority Critical patent/AU2013203491A1/en
Application granted granted Critical
Publication of AU2011285532B2 publication Critical patent/AU2011285532B2/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12P—FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
    • C12P21/00—Preparation of peptides or proteins
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K31/435—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
    • 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
    • A61K31/435—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
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/021—Peptides 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)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (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)
  • Biotechnology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Engineering & Computer Science (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)
AU2011285532A 2010-08-06 2011-08-05 Processes for preparing tubulysins Ceased AU2011285532B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2013203491A AU2013203491A1 (en) 2010-08-06 2013-04-10 Processes for preparing tubulysins

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US37143310P 2010-08-06 2010-08-06
US61/371,433 2010-08-06
PCT/US2011/046797 WO2012019123A1 (en) 2010-08-06 2011-08-05 Processes for preparing tubulysins

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2013203491A Division AU2013203491A1 (en) 2010-08-06 2013-04-10 Processes for preparing tubulysins

Publications (2)

Publication Number Publication Date
AU2011285532A1 AU2011285532A1 (en) 2013-02-21
AU2011285532B2 true AU2011285532B2 (en) 2015-09-10

Family

ID=45559842

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2011285532A Ceased AU2011285532B2 (en) 2010-08-06 2011-08-05 Processes for preparing tubulysins

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
JP5149620B2 (ja) 2004-07-23 2013-02-20 エンドサイト，インコーポレイテッド ２価リンカーおよびその結合体
US20100104626A1 (en) 2007-02-16 2010-04-29 Endocyte, Inc. Methods and compositions for treating and diagnosing kidney disease
NZ580132A (en) 2007-03-14 2012-11-30 Endocyte Inc Binding ligand linked drug delivery conjugates of tubulysins to vitamins
US9877965B2 (en) 2007-06-25 2018-01-30 Endocyte, Inc. Vitamin receptor drug delivery conjugates for treating inflammation
CN104383553A (zh) 2007-06-25 2015-03-04 恩多塞特公司 含有亲水性间隔区接头的共轭物
WO2009055562A1 (en) 2007-10-25 2009-04-30 Endocyte, Inc. Tubulysins and processes for preparing
MX2013001402A (es) 2010-08-06 2013-08-29 Endocyte Inc Proceso para preparar tubulisinas.
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
JP2015536323A (ja) 2012-10-16 2015-12-21 エンドサイト・インコーポレイテッドＥｎｄｏｃｙｔｅ， Ｉｎｃ． 非天然アミノ酸を含む薬物送達結合体および使用方法
AU2013344778C1 (en) 2012-11-15 2024-06-27 Endocyte, Inc. Conjugates for treating diseases caused by PSMA expressing cells
US20140249315A1 (en) * 2013-03-01 2014-09-04 Endocyte, Inc. Processes for preparing tubulysins
ES2843537T3 (es) 2014-01-28 2021-07-19 Tube Pharmaceuticals Gmbh Compuestos citotóxicos de tubulisina y conjugados de los mismos
SG11201608192SA (en) 2014-04-11 2016-10-28 Medimmune Llc Bispecific her2 antibodies
US20170304460A1 (en) 2014-10-01 2017-10-26 Medimmune, Llc Method of conjugating a polypeptide
EA201791896A1 (ru) 2015-02-25 2018-02-28 Уильям Марш Райс Юниверсити Дезацетокситубулизин н и его аналоги
LT3374398T (lt) 2015-11-10 2020-09-10 Medimmune, Llc Asct2 atžvilgiu specifinės surišančios molekulės ir jų panaudojimai
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
US11414477B2 (en) 2016-01-27 2022-08-16 Medimmune, Llc Methods for preparing antibodies with a defined glycosylation pattern
CA3020864A1 (en) 2016-04-15 2017-10-19 Macrogenics, Inc. Novel 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
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
CA3193594A1 (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
WO2023083846A1 (en) 2021-11-10 2023-05-19 Astrazeneca Ab Antibody molecules and conjugates
GB202117928D0 (en) 2021-12-11 2022-01-26 Cancer Research Tech Ltd Immunotherapy for cancer
AU2023229884A1 (en) 2022-03-09 2024-10-10 Astrazeneca Ab BINDING MOLECULES AGAINST FRα
IL317733A (en) 2022-06-27 2025-02-01 Astrazeneca Ab Combinations involving epidermal growth factor receptor tyrosine kinase inhibitors for cancer treatment
JP2026506049A (ja) 2023-02-16 2026-02-20 アストラゼネカ・アクチエボラーグ 治療用結合分子を用いた癌の治療のための併用療法

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
WO2004005326A2 (de) 2002-07-09 2004-01-15 Morphochem Aktiengellschaft Fu Tubulysinkonjugate
DK1523493T3 (da) 2002-07-09 2013-12-02 Alexander Doemling Nye tubulysinanaloge
DE10254439A1 (de) 2002-11-21 2004-06-03 GESELLSCHAFT FüR BIOTECHNOLOGISCHE FORSCHUNG MBH (GBF) Tubulysine, Herstellungsverfahren und Tubulysin-Mittel
JP5576007B2 (ja) 2003-01-27 2014-08-20 エンドサイト・インコーポレイテッド ビタミン受容体結合性薬剤送達結合体
NZ580132A (en) 2007-03-14 2012-11-30 Endocyte Inc Binding ligand linked drug delivery conjugates of tubulysins to vitamins
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
WO2011106639A1 (en) 2010-02-25 2011-09-01 Purdue Research Foundation Psma binding ligand-linker conjugates and methods for using
MX2013001402A (es) * 2010-08-06 2013-08-29 Endocyte Inc Proceso para preparar tubulisinas.

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
PELTIER, H.M. et al. "The Total Synthesis of Tubulysin D" Journal of the American Chemical Society (2006) Vol 128 pages 16018 to 16019 *
WU, S.-H. et al. "Enhancing the Enantioselectivity of Candida Lipase Catalyzed Ester Hydrolysis via Noncovalent Enzyme Modification" Journal of the American Chemical Society (1990) Vol.112 pages 1990 to 1995 *

Also Published As

Publication number Publication date
EP2600866A4 (en) 2013-12-11
CN103140227A (zh) 2013-06-05
US20150225447A1 (en) 2015-08-13
JP2013535220A (ja) 2013-09-12
AU2011285532A1 (en) 2013-02-21
US9499849B2 (en) 2016-11-22
MX2013001402A (es) 2013-08-29
CN103140227B (zh) 2016-01-20
EA025471B1 (ru) 2016-12-30
US9273091B2 (en) 2016-03-01
BR112013003004A2 (pt) 2016-06-14
US8889880B2 (en) 2014-11-18
EP2600866A1 (en) 2013-06-12
US20130137139A1 (en) 2013-05-30
KR20130096712A (ko) 2013-08-30
EA201390203A1 (ru) 2013-08-30
SG187728A1 (en) 2013-03-28
US20160177363A1 (en) 2016-06-23
HK1185558A1 (zh) 2014-02-21
CA2807511A1 (en) 2012-02-09
WO2012019123A1 (en) 2012-02-09

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FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired