CN101247799B - 成纤维细胞活化蛋白α的抑制剂 - Google Patents

成纤维细胞活化蛋白α的抑制剂 Download PDF

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Publication number
CN101247799B
CN101247799B CN2006800307719A CN200680030771A CN101247799B CN 101247799 B CN101247799 B CN 101247799B CN 2006800307719 A CN2006800307719 A CN 2006800307719A CN 200680030771 A CN200680030771 A CN 200680030771A CN 101247799 B CN101247799 B CN 101247799B
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cancer
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CN101247799A (zh
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W·W·巴乔夫钦
H·赖
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Tufts University
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Tufts University
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/04—Esters of boric acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/025—Boronic and borinic acid compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • C07D207/09—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/04—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D277/06—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
CN2006800307719A 2005-07-05 2006-07-05 成纤维细胞活化蛋白α的抑制剂 Expired - Fee Related CN101247799B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US69677205P 2005-07-05 2005-07-05
US60/696,772 2005-07-05
PCT/US2006/026258 WO2007005991A1 (en) 2005-07-05 2006-07-05 Inhibitors of fibroblast activation protein alpha

Publications (2)

Publication Number Publication Date
CN101247799A CN101247799A (zh) 2008-08-20
CN101247799B true CN101247799B (zh) 2013-03-27

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CN2006800307719A Expired - Fee Related CN101247799B (zh) 2005-07-05 2006-07-05 成纤维细胞活化蛋白α的抑制剂

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Country Link
US (2) US7998997B2 (enExample)
EP (1) EP1898899A4 (enExample)
JP (2) JP5229897B2 (enExample)
KR (1) KR20080030079A (enExample)
CN (1) CN101247799B (enExample)
AU (1) AU2006264305B2 (enExample)
BR (1) BRPI0612607A2 (enExample)
CA (1) CA2613795A1 (enExample)
IL (2) IL188327A0 (enExample)
MX (1) MX2008000318A (enExample)
NO (1) NO20080626L (enExample)
WO (1) WO2007005991A1 (enExample)

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CA2606785A1 (en) * 2005-05-19 2006-11-23 Genentech, Inc. Fibroblast activation protein inhibitor compounds and methods
EP1760076A1 (en) * 2005-09-02 2007-03-07 Ferring B.V. FAP Inhibitors
KR20140042933A (ko) 2007-08-06 2014-04-07 밀레니엄 파머슈티컬스 인코퍼레이티드 프로테아좀 억제제
US7442830B1 (en) 2007-08-06 2008-10-28 Millenium Pharmaceuticals, Inc. Proteasome inhibitors
US7838673B2 (en) 2007-10-16 2010-11-23 Millennium Pharmaceuticals, Inc. Proteasome inhibitors
EP2212334B1 (en) * 2007-10-16 2012-08-15 Millennium Pharmaceuticals, Inc. Proteasome inhibitors
SI2318419T2 (sl) 2008-06-17 2025-10-30 Takeda Pharmaceutical Company Limited Spojine boronat estra in njihovi farmacevtski sestavki
AR075090A1 (es) 2008-09-29 2011-03-09 Millennium Pharm Inc Derivados de acido 1-amino-2-ciclobutiletilboronico inhibidores de proteosoma,utiles como agentes anticancerigenos, y composiciones farmaceuticas que los comprenden.
AU2011235227B2 (en) 2010-03-31 2016-09-08 Millennium Pharmaceuticals, Inc. Derivatives of 1-amino-2-cyclopropylethylboronic acid
EP4706663A3 (en) * 2011-08-30 2026-05-20 Trustees Of Tufts College FAP-ACTIVATED PROTEASOME INHIBITORS USED TO TREAT SOLID TUMORS
US9284337B2 (en) * 2011-11-22 2016-03-15 Trustees Of Tufts College Small molecule enhancer for dendritic cell cancer vaccines
WO2014022636A1 (en) * 2012-08-02 2014-02-06 Trustees Of Tufts College Broad spectrum inhibitors of the post proline cleaving enzymes for treatment of hepatitis c virus infections
UA121389C2 (uk) 2014-05-20 2020-05-25 Мілленніум Фармасьютікалз, Інк. Борвмісні інгібітори протеасом для застосування після первинної протиракової терапії
CZ2014527A3 (cs) * 2014-08-05 2016-02-17 Ústav Organické Chemie A Biochemie Akademie Věd Čr, V.V.I. Způsob detekce aktivní formy analytů ve vzorku a stanovení schopnosti dalších látek vázat se do aktivních míst těchto analytů
MA41505A (fr) 2015-02-11 2017-12-19 Millennium Pharm Inc Nouvelle forme cristalline d'un inhibiteur de protéasome
WO2016171446A1 (ko) * 2015-04-20 2016-10-27 동아에스티 주식회사 펩타이드 붕소산 화합물을 함유하는 안정화 약학 제제
CN106588965A (zh) 2015-10-15 2017-04-26 北京大学 脲拟肽硼酸化合物及其药物组合物、制备方法和用途
JP6223508B2 (ja) * 2016-06-27 2017-11-01 ミレニアム ファーマシューティカルズ， インコーポレイテッドＭｉｌｌｅｎｎｉｕｍ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． プロテアソーム阻害剤
JP7162592B2 (ja) 2016-12-14 2022-10-28 パーデュー・リサーチ・ファウンデイション 線維芽細胞活性化タンパク質（ｆａｐ）標的イメージングおよび治療
WO2018129497A1 (en) 2017-01-09 2018-07-12 Bioxcel Therapeutics, Inc. Predictive and diagnostic methods for prostate cancer
CN108929340B (zh) * 2017-05-22 2019-12-13 北京大学 脯氨酸硼酸类化合物及其制备方法和用途
WO2019154859A1 (en) * 2018-02-06 2019-08-15 Universität Heidelberg Fap inhibitor
MX2022011842A (es) * 2020-03-24 2022-10-20 Tufts College Agentes de imagen y radiofarmacos dirigidos a fap, y usos relacionados con los mismos.
EP4313033A4 (en) * 2021-03-24 2025-04-23 Trustees Of Tufts College BORONIC ACID COMPOUNDS, COMPOSITIONS AND METHODS
CN118955616B (zh) * 2024-05-01 2025-09-02 杭州景嘉航生物医药科技有限公司 一种靶向结合成纤维细胞活化蛋白化合物及应用
CN119390720B (zh) * 2024-12-31 2025-04-01 杭州景嘉航生物医药科技有限公司 一种靶向结合成纤维细胞活化蛋白的双环[1.1.1]戊烷类化合物及其应用
WO2026007968A1 (zh) * 2024-07-01 2026-01-08 杭州景嘉航生物医药科技有限公司 一种靶向结合成纤维细胞活化蛋白的化合物及应用

Citations (2)

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WO2003092605A2 (en) * 2002-04-30 2003-11-13 Trustees Of Tufts College Protease inhibitors
US20050084490A1 (en) * 2002-07-09 2005-04-21 Point Therapeutics, Inc. Boroproline compound combination therapy

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US497A (en) * 1837-12-01 Improvement in the machine for preparing ice for shipping and storing
US4935493A (en) * 1987-10-06 1990-06-19 E. I. Du Pont De Nemours And Company Protease inhibitors
US5106948A (en) 1988-05-27 1992-04-21 Mao Foundation For Medical Education And Research Cytotoxic boronic acid peptide analogs
US4963655A (en) 1988-05-27 1990-10-16 Mayo Foundation For Medical Education And Research Boron analogs of amino acid/peptide protease inhibitors
US5159060A (en) * 1988-05-27 1992-10-27 Mayo Foundation For Medical Education And Research Cytotoxic boronic acid peptide analogs
EP1463719A2 (en) * 2002-01-08 2004-10-06 Eisai Co., Ltd Eponemycin and epoxomicin analogs and uses thereof
WO2004050613A2 (en) * 2002-12-02 2004-06-17 Gilead Sciences, Inc. 2-substituted-3-propenamide derivatives and methods of using the same
US7576206B2 (en) * 2003-08-14 2009-08-18 Cephalon, Inc. Proteasome inhibitors and methods of using the same
AU2004288831B2 (en) * 2003-11-12 2010-08-26 Phenomix Corporation Heterocyclic boronic acid compounds
CA2606785A1 (en) * 2005-05-19 2006-11-23 Genentech, Inc. Fibroblast activation protein inhibitor compounds and methods

Patent Citations (2)

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WO2003092605A2 (en) * 2002-04-30 2003-11-13 Trustees Of Tufts College Protease inhibitors
US20050084490A1 (en) * 2002-07-09 2005-04-21 Point Therapeutics, Inc. Boroproline compound combination therapy

Also Published As

Publication number Publication date
AU2006264305B2 (en) 2012-07-05
CN101247799A (zh) 2008-08-20
IL217579A (en) 2013-04-30
EP1898899A1 (en) 2008-03-19
JP2009500423A (ja) 2009-01-08
IL188327A0 (en) 2008-04-13
AU2006264305A1 (en) 2007-01-11
NO20080626L (no) 2008-04-02
JP5229897B2 (ja) 2013-07-03
EP1898899A4 (en) 2009-07-29
MX2008000318A (es) 2008-03-11
JP2012140439A (ja) 2012-07-26
BRPI0612607A2 (pt) 2010-12-07
CA2613795A1 (en) 2007-01-11
US7998997B2 (en) 2011-08-16
US20090221818A1 (en) 2009-09-03
WO2007005991A1 (en) 2007-01-11
US20120077779A1 (en) 2012-03-29
KR20080030079A (ko) 2008-04-03

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