CN101175757B - 蝶酸及其缀合物的合成和纯化 - Google Patents

蝶酸及其缀合物的合成和纯化 Download PDF

Info

Publication number
CN101175757B
CN101175757B CN2006800162870A CN200680016287A CN101175757B CN 101175757 B CN101175757 B CN 101175757B CN 2006800162870 A CN2006800162870 A CN 2006800162870A CN 200680016287 A CN200680016287 A CN 200680016287A CN 101175757 B CN101175757 B CN 101175757B
Authority
CN
China
Prior art keywords
acid
resorcinolphthalein
conjugate
pteroic
compound
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
CN2006800162870A
Other languages
English (en)
Chinese (zh)
Other versions
CN101175757A (zh
Inventor
许乐村
I·R·弗拉霍夫
C·P·利蒙
H·K·桑塔普拉姆
李春红
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 CN101175757A publication Critical patent/CN101175757A/zh
Application granted granted Critical
Publication of CN101175757B publication Critical patent/CN101175757B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D475/00—Heterocyclic compounds containing pteridine ring systems
    • C07D475/06—Heterocyclic compounds containing pteridine ring systems with a nitrogen atom directly attached in position 4
    • C07D475/08—Heterocyclic compounds containing pteridine ring systems with a nitrogen atom directly attached in position 4 with a nitrogen atom directly attached in position 2
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/10—Anthelmintics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/10—Anthelmintics
    • A61P33/12—Schistosomicides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/14—Ectoparasiticides, e.g. scabicides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CN2006800162870A 2005-03-16 2006-03-14 蝶酸及其缀合物的合成和纯化 Expired - Fee Related CN101175757B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US66227705P 2005-03-16 2005-03-16
US60/662,277 2005-03-16
PCT/US2006/009153 WO2006101845A2 (en) 2005-03-16 2006-03-14 Synthesis and purification of pteroic acid and conjugates thereof

Publications (2)

Publication Number Publication Date
CN101175757A CN101175757A (zh) 2008-05-07
CN101175757B true CN101175757B (zh) 2012-11-14

Family

ID=36699050

Family Applications (1)

Application Number Title Priority Date Filing Date
CN2006800162870A Expired - Fee Related CN101175757B (zh) 2005-03-16 2006-03-14 蝶酸及其缀合物的合成和纯化

Country Status (5)

Country Link
US (1) US8044200B2 (cg-RX-API-DMAC7.html)
EP (1) EP1863816B1 (cg-RX-API-DMAC7.html)
JP (1) JP5289935B2 (cg-RX-API-DMAC7.html)
CN (1) CN101175757B (cg-RX-API-DMAC7.html)
WO (1) WO2006101845A2 (cg-RX-API-DMAC7.html)

Families Citing this family (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1389209B1 (en) * 2001-04-24 2009-04-08 Purdue Research Foundation Folate mimetics and folate-receptor binding conjugates thereof
MXPA03010035A (es) 2001-05-02 2004-06-30 Purdue Research Foundation Tratamiento y diagnostico de enfermedades mediadas por macrofagos.
US8043602B2 (en) 2002-02-07 2011-10-25 Endocyte, Inc. Folate targeted enhanced tumor and folate receptor positive tissue optical imaging technology
US8043603B2 (en) 2002-02-07 2011-10-25 Endocyte, Inc. Folate targeted enhanced tumor and folate receptor positive tissue optical imaging technology
EP2517729A3 (en) 2003-01-27 2013-01-02 Endocyte, Inc. Vitamin receptor binding drug delivery conjugates
JP4680185B2 (ja) 2003-05-30 2011-05-11 パーデュー・リサーチ・ファウンデーション アテローム性動脈硬化症の診断法
EP1789391B1 (en) 2004-07-23 2017-06-28 Endocyte, Inc. Bivalent linkers and conjugates thereof
CN101175757B (zh) 2005-03-16 2012-11-14 恩多塞特公司 蝶酸及其缀合物的合成和纯化
EP1904183B1 (en) 2005-07-05 2014-10-15 Purdue Research Foundation Pharmaceutical composition for the treatment of osteoarthritis
US8465724B2 (en) * 2005-08-19 2013-06-18 Endocyte, Inc. Multi-drug ligand conjugates
US20080280937A1 (en) * 2005-08-19 2008-11-13 Christopher Paul Leamon Ligand Conjugates of Vinca Alkaloids, Analogs, and Derivatives
WO2007038346A2 (en) 2005-09-23 2007-04-05 Purdue Research Foundation Multiphoton in vivo flow cytometry method and device
EP2087337A4 (en) 2006-11-03 2010-09-08 Purdue Research Foundation METHOD AND DEVICE FOR EX-VIVO FLOW CYTOMETRY
EP2109466B1 (en) 2007-02-07 2014-11-12 Purdue Research Foundation Positron emission tomography imaging method
US20100104626A1 (en) * 2007-02-16 2010-04-29 Endocyte, Inc. Methods and compositions for treating and diagnosing kidney disease
CA2680535C (en) * 2007-03-14 2016-09-20 Endocyte, Inc. Binding ligand linked drug delivery conjugates of tubulysins
CN101646639A (zh) 2007-04-11 2010-02-10 默克阿泼洛发股份公司 18f-标记的叶酸
US8961926B2 (en) 2007-05-25 2015-02-24 Purdue Research Foundation Method of imaging localized infections
CA2690943A1 (en) 2007-06-25 2008-12-31 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
WO2009055562A1 (en) 2007-10-25 2009-04-30 Endocyte, Inc. Tubulysins and processes for preparing
PL2349274T3 (pl) 2008-09-17 2025-09-22 Endocyte, Inc. Koniugaty antyfolianów wiążące się z receptorem folianów
IN2012DN01708A (cg-RX-API-DMAC7.html) * 2009-07-31 2015-06-05 Endocyte Inc
WO2011027786A1 (ja) * 2009-09-07 2011-03-10 ニプロパッチ株式会社 経皮吸収型製剤
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
IN2015DN04147A (cg-RX-API-DMAC7.html) 2012-10-16 2015-10-16 Endocyte Inc
US9333270B2 (en) * 2013-03-15 2016-05-10 Purdue Research Foundation Synthesis and composition of amino acid linking groups conjugated to compounds used for the targeted imaging of tumors
EP3071971B1 (en) 2013-11-19 2019-04-24 Purdue Research Foundation Patient selection method for inflammation
US20180036312A1 (en) * 2016-08-02 2018-02-08 ISI Life Sciences Inc. Novel Scaffolds for Intracellular Compound Delivery for the Detection of Cancer Cells
US10239891B2 (en) * 2017-05-15 2019-03-26 Indicator Systems International, Inc. Compositions to detect remnant cancer cells
WO2018026965A1 (en) 2016-08-02 2018-02-08 Isi Life Sciences, Inc. Compositions and methods for detecting cancer cells in a tissue sample
CN106420394B (zh) * 2016-10-21 2019-05-10 江南大学 一种增强叶酸光稳定性的方法
US10753942B2 (en) 2017-05-15 2020-08-25 Indicator Systems International, Inc. Methods to detect remnant cancer cells
CN109734717B (zh) * 2019-01-24 2022-03-22 苏州华健瑞达医药技术有限公司 蝶酸新晶型及其制备方法
US20240165250A1 (en) * 2021-01-08 2024-05-23 Lycia Therapeutics, Inc. Bifunctional Folate Receptor Binding Compounds
CN116218513A (zh) * 2023-03-03 2023-06-06 杭州谱康医学科技有限公司 Fitc标记的荧光微球、制备方法及应用
CN116621838A (zh) * 2023-04-17 2023-08-22 武汉翱飞科技有限公司 一种蝶酸活性酯及其合成方法

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4337339A (en) * 1979-04-30 1982-06-29 Baker Instruments Corp. Process for preparation of folic acid derivatives

Family Cites Families (118)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2515483A (en) * 1946-08-10 1950-07-18 Merck & Co Inc Diacylated pteroic acid and process for preparing same
US2816110A (en) 1956-11-23 1957-12-10 Merck & Co Inc Methods for the production of substituted pteridines
US3392173A (en) * 1964-03-09 1968-07-09 Lilly Co Eli Novel acyl derivatives of desacetyl-vincaleukoblastine and processes for their preparation
US3387001A (en) * 1964-10-19 1968-06-04 Lilly Co Eli Novel aminoacyl esters of desacetyl vincaleukoblastine
US4203898A (en) * 1977-08-29 1980-05-20 Eli Lilly And Company Amide derivatives of VLB, leurosidine, leurocristine and related dimeric alkaloids
US4166810A (en) * 1978-04-20 1979-09-04 Eli Lilly And Company Derivatives of 4-desacetyl VLB C-3 carboxyhydrazide
US4639456A (en) 1980-06-10 1987-01-27 Omnichem S.A. Vinblastin-23-oyl amino acid derivatives
US4316885A (en) * 1980-08-25 1982-02-23 Ayerst, Mckenna And Harrison, Inc. Acyl derivatives of rapamycin
US4713249A (en) 1981-11-12 1987-12-15 Schroeder Ulf Crystallized carbohydrate matrix for biologically active substances, a process of preparing said matrix, and the use thereof
US5140104A (en) * 1982-03-09 1992-08-18 Cytogen Corporation Amine derivatives of folic acid analogs
DE116208T1 (de) 1982-12-07 1985-02-28 Kyowa Hakko Kogyo Co., Ltd., Tokio/Tokyo Mitomycin-analoge.
US4866180A (en) * 1984-02-24 1989-09-12 Bristol-Myers Company Amino disulfide thiol exchange products
JPS60255789A (ja) 1984-06-01 1985-12-17 Kyowa Hakko Kogyo Co Ltd マイトマイシン誘導体，その製造法および抗腫瘍剤
US5266333A (en) * 1985-03-06 1993-11-30 American Cyanamid Company Water dispersible and water soluble carbohydrate polymer compositions for parenteral administration of growth hormone
US4650803A (en) * 1985-12-06 1987-03-17 University Of Kansas Prodrugs of rapamycin
US4801688A (en) * 1986-05-27 1989-01-31 Eli Lilly And Company Hydrazone immunoglobulin conjugates
IL82579A0 (en) 1986-05-27 1987-11-30 Lilly Co Eli Immunoglobulin conjugates
EP0280741B1 (en) 1986-08-29 1994-12-07 Kyowa Hakko Kogyo Kabushiki Kaisha Mitomycin derivatives
US5006652A (en) * 1988-08-08 1991-04-09 Eli Lilly And Company Intermediates for antibody-vinca drug conjugates
US5094849A (en) * 1988-08-08 1992-03-10 Eli Lilly And Company Cytotoxic antibody conjugates of hydrazide derivatized vinca analogs via simple organic linkers
US5108921A (en) 1989-04-03 1992-04-28 Purdue Research Foundation Method for enhanced transmembrane transport of exogenous molecules
US5688488A (en) * 1989-04-03 1997-11-18 Purdue Research Foundation Composition and method for tumor imaging
US5627165A (en) * 1990-06-13 1997-05-06 Drug Innovation & Design, Inc. Phosphorous prodrugs and therapeutic delivery systems using same
US5998603A (en) 1994-09-29 1999-12-07 Isis Pharmaceuticals, Inc. 4'-desmethyl nucleoside analogs, and oligomers thereof
CA2090105A1 (en) * 1990-08-29 1992-03-01 Jean-Paul Soulillou Protein polyligands joined to a stable protein core
US5221670A (en) * 1990-09-19 1993-06-22 American Home Products Corporation Rapamycin esters
US5378696A (en) * 1990-09-19 1995-01-03 American Home Products Corporation Rapamycin esters
US5130307A (en) * 1990-09-28 1992-07-14 American Home Products Corporation Aminoesters of rapamycin
US5233036A (en) * 1990-10-16 1993-08-03 American Home Products Corporation Rapamycin alkoxyesters
US5120842A (en) * 1991-04-01 1992-06-09 American Home Products Corporation Silyl ethers of rapamycin
US5100883A (en) * 1991-04-08 1992-03-31 American Home Products Corporation Fluorinated esters of rapamycin
US5194447A (en) * 1992-02-18 1993-03-16 American Home Products Corporation Sulfonylcarbamates of rapamycin
US5118678A (en) * 1991-04-17 1992-06-02 American Home Products Corporation Carbamates of rapamycin
US5138051A (en) * 1991-08-07 1992-08-11 American Home Products Corporation Rapamycin analogs as immunosuppressants and antifungals
US5118677A (en) * 1991-05-20 1992-06-02 American Home Products Corporation Amide esters of rapamycin
US5169851A (en) 1991-08-07 1992-12-08 American Home Products Corporation Rapamycin analog as immunosuppressants and antifungals
US6335434B1 (en) * 1998-06-16 2002-01-01 Isis Pharmaceuticals, Inc., Nucleosidic and non-nucleosidic folate conjugates
US5151413A (en) * 1991-11-06 1992-09-29 American Home Products Corporation Rapamycin acetals as immunosuppressant and antifungal agents
US5159079A (en) * 1991-12-20 1992-10-27 Eli Lilly And Company 2-piperidones as intermediates for 5-deaza-10-oxo- and 5-deaza-10-thio-5,6,7,8-tetrahydrofolic acids
US6004555A (en) 1992-03-05 1999-12-21 Board Of Regents, The University Of Texas System Methods for the specific coagulation of vasculature
US5302584A (en) * 1992-10-13 1994-04-12 American Home Products Corporation Carbamates of rapamycin
US5258389A (en) * 1992-11-09 1993-11-02 Merck & Co., Inc. O-aryl, O-alkyl, O-alkenyl and O-alkynylrapamycin derivatives
US5260300A (en) * 1992-11-19 1993-11-09 American Home Products Corporation Rapamycin carbonate esters as immuno-suppressant agents
JPH08509499A (ja) * 1993-04-23 1996-10-08 アボツト・ラボラトリーズ ラパマイシン結合体及び抗体
US5391730A (en) * 1993-10-08 1995-02-21 American Home Products Corporation Phosphorylcarbamates of rapamycin and oxime derivatives thereof
US5385908A (en) * 1993-11-22 1995-01-31 American Home Products Corporation Hindered esters of rapamycin
US5385910A (en) * 1993-11-22 1995-01-31 American Home Products Corporation Gem-distributed esters of rapamycin
US5385909A (en) * 1993-11-22 1995-01-31 American Home Products Corporation Heterocyclic esters of rapamycin
US5389639A (en) * 1993-12-29 1995-02-14 American Home Products Company Amino alkanoic esters of rapamycin
US5417982A (en) * 1994-02-17 1995-05-23 Modi; Pankaj Controlled release of drugs or hormones in biodegradable polymer microspheres
IL112873A (en) * 1994-03-08 2005-03-20 Wyeth Corp Rapamycin-fkbp12 binding proteins, their isolation and their use
US6171859B1 (en) * 1994-03-30 2001-01-09 Mitokor Method of targeting conjugate molecules to mitochondria
US5362718A (en) * 1994-04-18 1994-11-08 American Home Products Corporation Rapamycin hydroxyesters
US5463048A (en) * 1994-06-14 1995-10-31 American Home Products Corporation Rapamycin amidino carbamates
US5491231A (en) * 1994-11-28 1996-02-13 American Home Products Corporation Hindered N-oxide esters of rapamycin
US5547668A (en) * 1995-05-05 1996-08-20 The Board Of Trustees Of The University Of Illinois Conjugates of folate anti-effector cell antibodies
US6207157B1 (en) * 1996-04-23 2001-03-27 The United States Of America As Represented By The Department Of Health And Human Services Conjugate vaccine for nontypeable Haemophilus influenzae
US6030941A (en) * 1996-05-01 2000-02-29 Avi Biopharma, Inc. Polymer composition for delivering substances in living organisms
DE69737867T2 (de) * 1996-05-03 2007-10-18 Immunomedics, Inc. Zielgerichtete kombinations-immuntherapie für krebs
DE19621133A1 (de) * 1996-05-24 1997-11-27 Boehringer Mannheim Gmbh Bestimmungsverfahren mit oligomerisierten Rezeptoren
WO1998010651A1 (en) 1996-09-12 1998-03-19 Merck & Co., Inc. Conjugates useful in the treatment of prostate cancer
US6056973A (en) * 1996-10-11 2000-05-02 Sequus Pharmaceuticals, Inc. Therapeutic liposome composition and method of preparation
US6177404B1 (en) * 1996-10-15 2001-01-23 Merck & Co., Inc. Conjugates useful in the treatment of benign prostatic hyperplasia
US6071532A (en) * 1996-10-15 2000-06-06 Emory University Synthesis of glycophospholipid and peptide-phospholipid conjugates and uses thereof
US6291673B1 (en) 1997-10-17 2001-09-18 Purdue Research Foundation Folic acid derivatives
GB9723669D0 (en) * 1997-11-07 1998-01-07 Univ Aberdeen Skin penetration enhancing components
US6380395B1 (en) 1998-04-21 2002-04-30 Bristol-Myers Squibb Company 12, 13-cyclopropane epothilone derivatives
US6093382A (en) * 1998-05-16 2000-07-25 Bracco Research Usa Inc. Metal complexes derivatized with folate for use in diagnostic and therapeutic applications
US6291684B1 (en) 1999-03-29 2001-09-18 Bristol-Myers Squibb Company Process for the preparation of aziridinyl epothilones from oxiranyl epothilones
HUP0201425A3 (en) * 1999-04-23 2006-07-28 Hadasit Med Res Service Conjugate having a cleavable linkage for use in a liposome
AUPQ014799A0 (en) 1999-05-04 1999-05-27 Access Pharmaceuticals Australia Pty Limited Amplification of folate-mediated targeting to tumor cells using polymers
AUPQ071299A0 (en) 1999-06-02 1999-06-24 Access Pharmaceuticals Australia Pty Limited Vitamin directed dual targeting therapy
KR20020059618A (ko) * 1999-10-15 2002-07-13 메이오 파운데이션 포 메디칼 에쥬케이션 앤드 리써치 이미지화제 및 항종양제로서 유용한 코발라민 콘쥬게이트
US7067111B1 (en) * 1999-10-25 2006-06-27 Board Of Regents, University Of Texas System Ethylenedicysteine (EC)-drug conjugates, compositions and methods for tissue specific disease imaging
PL211872B1 (pl) * 2000-03-31 2012-07-31 Purdue Research Foundation Kompozycja farmaceutyczna
US6670355B2 (en) 2000-06-16 2003-12-30 Wyeth Method of treating cardiovascular disease
PT1318837E (pt) * 2000-08-11 2004-12-31 Wyeth Corp Metodo de tratamenton de carcinoma positivo a receptor de estrogenio
MXPA03002258A (es) * 2000-09-19 2003-06-24 Wyeth Corp Esteres de rapamicina solubles en agua.
US6399625B1 (en) * 2000-09-27 2002-06-04 Wyeth 1-oxorapamycins
US6399626B1 (en) * 2000-10-02 2002-06-04 Wyeth Hydroxyesters of 7-desmethylrapamycin
US6440991B1 (en) * 2000-10-02 2002-08-27 Wyeth Ethers of 7-desmethlrapamycin
JP2004526425A (ja) 2000-11-28 2004-09-02 ワイス 前立腺癌の診断および治療に有用なｆｋｂｐ核酸およびポリペプチドの発現分析
AR036993A1 (es) * 2001-04-02 2004-10-20 Wyeth Corp Uso de agentes que modulan la interaccion entre pd-1 y sus ligandos en la submodulacion de respuestas inmunologicas
US7105328B2 (en) * 2001-04-02 2006-09-12 Dana-Farber Cancer Institute Methods for screening for compounds that modulate pd-1 signaling
EP1389209B1 (en) * 2001-04-24 2009-04-08 Purdue Research Foundation Folate mimetics and folate-receptor binding conjugates thereof
US7109165B2 (en) * 2001-05-18 2006-09-19 Sirna Therapeutics, Inc. Conjugates and compositions for cellular delivery
MXPA03010909A (es) 2001-06-01 2004-02-17 Bristol Myers Squibb Co Derivados de epotilona.
US20040018203A1 (en) * 2001-06-08 2004-01-29 Ira Pastan Pegylation of linkers improves antitumor activity and reduces toxicity of immunoconjugates
UA77200C2 (en) * 2001-08-07 2006-11-15 Wyeth Corp Antineoplastic combination of cci-779 and bkb-569
DE60206512T2 (de) * 2001-08-22 2006-06-22 Wyeth Rapamycin 29-enole
BR0211905A (pt) * 2001-08-22 2004-09-21 Wyeth Corp Dialdeìdos de rapamicina
DE60234782D1 (de) * 2001-09-28 2010-01-28 Purdue Research Foundation Behandlungsverfahren mit liganden-immunogenkonjugaten
GR1004163B (el) * 2001-11-01 2003-02-21 Πολυκυκλικα παραγωγα τροποποιησης των οπτικων ιδιοτητων και των ιδιοτητων αντοχης στο πλασμα των πολυμερων λιθογραφιας
US8043602B2 (en) * 2002-02-07 2011-10-25 Endocyte, Inc. Folate targeted enhanced tumor and folate receptor positive tissue optical imaging technology
US7000695B2 (en) * 2002-05-02 2006-02-21 Halliburton Energy Services, Inc. Expanding wellbore junction
DK2258401T3 (da) * 2002-05-06 2014-10-13 Endocyte Inc Folat-receptor targetede billeddannelsesmidler
US6596757B1 (en) * 2002-05-14 2003-07-22 Immunogen Inc. Cytotoxic agents comprising polyethylene glycol-containing taxanes and their therapeutic use
DE60326833D1 (de) * 2002-05-15 2009-05-07 Endocyte Inc Vitamin-mitomycin-konjugate
DK1523493T3 (da) * 2002-07-09 2013-12-02 Alexander Doemling Nye tubulysinanaloge
CA2501752A1 (en) 2002-10-10 2004-04-22 Wyeth Compositions, organisms and methodologies employing a novel human kinase
BR0316476A (pt) * 2002-11-21 2005-10-11 Wyeth Corp Composição e processo para tratar nefrite do lúpus
DE10254439A1 (de) * 2002-11-21 2004-06-03 GESELLSCHAFT FüR BIOTECHNOLOGISCHE FORSCHUNG MBH (GBF) Tubulysine, Herstellungsverfahren und Tubulysin-Mittel
EP2517729A3 (en) * 2003-01-27 2013-01-02 Endocyte, Inc. Vitamin receptor binding drug delivery conjugates
AR042938A1 (es) * 2003-02-06 2005-07-06 Wyeth Corp Uso del cci-779 en el tratamiento de la fibrosis hepatica
JP4597976B2 (ja) * 2003-04-17 2010-12-15 アルナイラム ファーマシューティカルズ インコーポレイテッド 修飾ｉＲＮＡ剤
WO2004101803A2 (en) * 2003-05-12 2004-11-25 Wyeth Holdings Corporation Process for producing anticancer agent ll-d45042
JP2007522091A (ja) * 2003-07-16 2007-08-09 ワイス Ｃｃｉ−７７９アイソマーｃ
AU2004265267A1 (en) 2003-08-07 2005-02-24 Wyeth Regioselective synthesis of CCI-779
EP1789391B1 (en) * 2004-07-23 2017-06-28 Endocyte, Inc. Bivalent linkers and conjugates thereof
US7582744B2 (en) * 2004-08-10 2009-09-01 Alnylam Pharmaceuticals, Inc. Chemically modified oligonucleotides
CN101175757B (zh) 2005-03-16 2012-11-14 恩多塞特公司 蝶酸及其缀合物的合成和纯化
DE602006012816D1 (de) 2005-03-30 2010-04-22 Endocyte Inc Tifizierung von zellulären folat vitamin rezeptoren
EP1904183B1 (en) 2005-07-05 2014-10-15 Purdue Research Foundation Pharmaceutical composition for the treatment of osteoarthritis
US8465724B2 (en) * 2005-08-19 2013-06-18 Endocyte, Inc. Multi-drug ligand conjugates
US20080280937A1 (en) 2005-08-19 2008-11-13 Christopher Paul Leamon Ligand Conjugates of Vinca Alkaloids, Analogs, and Derivatives
AR062448A1 (es) 2006-05-25 2008-11-12 Endocyte Inc Conjugados de analogos de aziridinil-epotilona y composiciones farmaceuticas que comprenden los mismos
US20100104626A1 (en) * 2007-02-16 2010-04-29 Endocyte, Inc. Methods and compositions for treating and diagnosing kidney disease
CA2680535C (en) * 2007-03-14 2016-09-20 Endocyte, Inc. Binding ligand linked drug delivery conjugates of tubulysins

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4337339A (en) * 1979-04-30 1982-06-29 Baker Instruments Corp. Process for preparation of folic acid derivatives

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
John M.Scott.Preparation and Purification of Pteroic Acid from Pteroylglutamic Acid(Folic Acid).《methods in enzymology》.1980,第66卷658页最后一段至660页.. *
John M.Scott.Preparation and Purification of Pteroic Acid from Pteroylglutamic Acid(Folic Acid).《methods in enzymology》.1980,第66卷658页最后一段至660页。.

Also Published As

Publication number Publication date
WO2006101845A3 (en) 2007-03-29
EP1863816A2 (en) 2007-12-12
US20080207625A1 (en) 2008-08-28
US8044200B2 (en) 2011-10-25
WO2006101845A2 (en) 2006-09-28
JP2008538743A (ja) 2008-11-06
EP1863816B1 (en) 2014-06-25
CN101175757A (zh) 2008-05-07
JP5289935B2 (ja) 2013-09-11

Similar Documents

Publication Publication Date Title
CN101175757B (zh) 蝶酸及其缀合物的合成和纯化
EP2349274B1 (en) Folate receptor binding conjugates of antifolates
AU2003217676B2 (en) Active agent delivery systems and methods for protecting and administering active agents
ES2577514T3 (es) Antagonistas de TLR
US7060708B2 (en) Active agent delivery systems and methods for protecting and administering active agents
ES2552471T3 (es) Conjugados de agonistas de TLR sintéticos y usos de los mismos
US8394813B2 (en) Active agent delivery systems and methods for protecting and administering active agents
US7427600B2 (en) Active agent delivery systems and methods for protecting and administering active agents
JP7103953B2 (ja) 薬物としてアマトキシンの誘導体を有する抗体薬物コンジュゲート
CN109316605B (zh) 叶酸受体结合配体-药物偶联物
US20240173422A1 (en) Bicyclic peptide ligand drug conjugates
CN117731798A (zh) 抗体偶联药物、其中间体、制备方法及应用
WO2021208459A1 (zh) 免疫激动剂
EP2029597A2 (en) Purine analogs
CN103893779A (zh) 多药物配体缀合物
JP5005532B2 (ja) １０−プロパルギル−１０−デアザアミノプテリンを用いるｔ細胞リンパ腫の治療
CN113941007A (zh) 一种串联的双药物链接组装单元及其应用
US20090306228A1 (en) Active agent delivery systems and methods for protecting and administering active agents
WO2021178818A2 (en) Therapeutic agents and conjugates thereof
CN1953989A (zh) 作为细胞抑制剂的在7位与环肽缀合的喜树碱
KR20240150763A (ko) 치료제에 연결된 랄티트렉시드 또는 5-mthf를 포함하는 화합물, 조성물, 및 사용 방법
CN106456796A (zh) 用于治疗耐药性癌症及用于联合治疗的药物递送缀合物
WO2015125640A1 (ja) カンプトテシン誘導体とｈｓｐ９０阻害剤の結合した高分子化合物及びその用途
WO2024263630A1 (en) Nectin-4 antibodies and antibody-drug conjugates
CN118697897A (zh) 多肽偶联药物及其制备方法和应用

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: 20121114