CN102984943B - 用于叶酸靶向剂的改进方法 - Google Patents

用于叶酸靶向剂的改进方法 Download PDF

Info

Publication number
CN102984943B
CN102984943B CN201180035630.7A CN201180035630A CN102984943B CN 102984943 B CN102984943 B CN 102984943B CN 201180035630 A CN201180035630 A CN 201180035630A CN 102984943 B CN102984943 B CN 102984943B
Authority
CN
China
Prior art keywords
compound
formula
following formula
acetonitrile
buffer
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
CN201180035630.7A
Other languages
English (en)
Chinese (zh)
Other versions
CN102984943A (zh
Inventor
D.S.雷诺
K.M.斯坦福德
I.R.弗拉霍夫
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 CN102984943A publication Critical patent/CN102984943A/zh
Application granted granted Critical
Publication of CN102984943B publication Critical patent/CN102984943B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/02—Linear peptides containing at least one abnormal peptide link
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/55—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
    • A61K47/551—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds one of the codrug's components being a vitamin, e.g. niacinamide, vitamin B3, cobalamin, vitamin B12, folate, vitamin A or retinoic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201180035630.7A 2010-05-19 2011-05-19 用于叶酸靶向剂的改进方法 Expired - Fee Related CN102984943B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US34644410P 2010-05-19 2010-05-19
US61/346444 2010-05-19
US35102210P 2010-06-03 2010-06-03
US61/351022 2010-06-03
PCT/US2011/037134 WO2011146707A1 (en) 2010-05-19 2011-05-19 Improved process for a folate-targeted agent

Publications (2)

Publication Number Publication Date
CN102984943A CN102984943A (zh) 2013-03-20
CN102984943B true CN102984943B (zh) 2016-01-13

Family

ID=44992057

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201180035630.7A Expired - Fee Related CN102984943B (zh) 2010-05-19 2011-05-19 用于叶酸靶向剂的改进方法

Country Status (11)

Country Link
US (2) US20130065841A1 (enExample)
JP (1) JP2013526577A (enExample)
KR (1) KR20130079431A (enExample)
CN (1) CN102984943B (enExample)
BR (1) BR112012029458A2 (enExample)
CA (1) CA2799391A1 (enExample)
IL (1) IL222964A0 (enExample)
MX (1) MX2012013250A (enExample)
RU (1) RU2012154914A (enExample)
SG (1) SG185592A1 (enExample)
WO (1) WO2011146707A1 (enExample)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107847609A (zh) 2015-03-13 2018-03-27 恩多塞特公司 用于治疗疾病的缀合物
US20200323991A1 (en) * 2016-03-29 2020-10-15 Endocyte, Inc. Pbd conjugates for treating diseases
CN111918892B (zh) 2018-04-11 2023-05-05 拉迪瑟夫私人有限责任公司 形成聚合物刷的组合物

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1621092A (zh) * 2003-11-25 2005-06-01 杨正茂 叶酸受体靶向脂质体药物载体及其制备方法和应用
CN101239190A (zh) * 2003-01-27 2008-08-13 恩多塞特公司 维生素受体结合递药缀合物
US20080280937A1 (en) * 2005-08-19 2008-11-13 Christopher Paul Leamon Ligand Conjugates of Vinca Alkaloids, Analogs, and Derivatives

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101239190A (zh) * 2003-01-27 2008-08-13 恩多塞特公司 维生素受体结合递药缀合物
CN1621092A (zh) * 2003-11-25 2005-06-01 杨正茂 叶酸受体靶向脂质体药物载体及其制备方法和应用
US20080280937A1 (en) * 2005-08-19 2008-11-13 Christopher Paul Leamon Ligand Conjugates of Vinca Alkaloids, Analogs, and Derivatives

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Design and regioselective synthesis of a new generation of targeted chemotherapeutics. Part 1: EC145, a folic acid conjugate of desacetylvinblastine monohydrazide;Iontcho R. Vlahov et al;《Bioorganic & Medicinal Chemistry Letters》;20060725;第16卷;第5093-5096页 *

Also Published As

Publication number Publication date
US20140066593A1 (en) 2014-03-06
MX2012013250A (es) 2013-03-05
SG185592A1 (en) 2012-12-28
IL222964A0 (en) 2013-02-03
KR20130079431A (ko) 2013-07-10
CN102984943A (zh) 2013-03-20
RU2012154914A (ru) 2014-06-27
US20130065841A1 (en) 2013-03-14
WO2011146707A1 (en) 2011-11-24
JP2013526577A (ja) 2013-06-24
BR112012029458A2 (pt) 2015-10-20
CA2799391A1 (en) 2011-12-04

Similar Documents

Publication Publication Date Title
JP2022514618A (ja) Ｐｄ－ｌ１に特異的な二環式ペプチドリガンド
MXPA06001090A (es) Agentes de imagenologia de peptido biciclico.
AU2005328644A1 (en) Methods for preparing multivalent constructs for therapeutic and diagnostic applications
AU2020204250B2 (en) One-pot process for preparing intermediate of antibody-drug conjugate
KR20050097494A (ko) 혈관신생, 세포 이동, 세포 침투 및 증식을 저해하는펩타이드, 그것의 조성물 및 그것의 용도
CN102984943B (zh) 用于叶酸靶向剂的改进方法
CN111001012A (zh) 一种亲水碳酸酯型抗体偶联药物
Guo et al. Supramolecular nanofibers increase the efficacy of 10-hydroxycamptothecin by enhancing nuclear accumulation and depleting cellular ATP
Gonçalves et al. Design, synthesis, and evaluation of original carriers for targeting vascular endothelial growth factor receptor interactions
SA113340536B1 (ar) معضدات مستقبل v1a
WO2017152756A1 (zh) cRGD-厄洛替尼缀合物及其制备方法
CN111574592B (zh) 一类具有拮抗pd-1/pd-l1相互作用的环肽类化合物及其应用
KR100405009B1 (ko) 바이싸이클릭타치키닌길항제,그의약제,및약제학적조성물로사용하는그의용도
EP4201429A1 (en) Antibody-drug conjugate intermediate comprising sn38 and preparation method therefor
CN118634340A (zh) 一种自组装多肽偶联药物的化合物及其应用
EP4417618A1 (en) Epha2 bicyclic peptide ligand and conjugate thereof
CN116217655B (zh) 一种连接基药物偶联物的中间体的制备方法
EP3950700A1 (en) Peptide complex and production method therefor, and use of said peptide complex
CN118203646A (zh) 靶向蛋白降解嵌合体分子自组装纳米材料及制备方法与应用
EP2571362A1 (en) Improved process for a folate-targeted agent
KR20190117541A (ko) 신규 화합물 (이뮤노렐린)
SK283129B6 (sk) Deriváty peptidu, ich použitie a farmaceutický prostriedok, ktorý ich obsahuje
Cao et al. Peptide-drug conjugates with linker-dependent payload release coordinate dual antitumor efficacy: Intrinsic RGDS-mediated metastasis suppression synergizes with camptothecin cytotoxicity
TWI905962B (zh) 用於綴合之化合物、綴合物及包含其之醫藥組成物
CN118373920B (zh) 具有pd-l1靶向性和细胞穿透性的融合肽及其与紫杉醇的偶联物以及制备方法与应用

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C14 Grant of patent or utility model
GR01 Patent grant
CF01 Termination of patent right due to non-payment of annual fee
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20160113

Termination date: 20180519