KR20080030079A - 섬유아세포 활성 단백질 알파의 억제제 - Google Patents

섬유아세포 활성 단백질 알파의 억제제 Download PDF

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Publication number
KR20080030079A
KR20080030079A KR1020087002781A KR20087002781A KR20080030079A KR 20080030079 A KR20080030079 A KR 20080030079A KR 1020087002781 A KR1020087002781 A KR 1020087002781A KR 20087002781 A KR20087002781 A KR 20087002781A KR 20080030079 A KR20080030079 A KR 20080030079A
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KR
South Korea
Prior art keywords
compound
alkyl
group
cancer
aralkyl
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Ceased
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KR1020087002781A
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English (en)
Korean (ko)
Inventor
윌리엄 더블유. 바쵸브친
헝-센 라이
Original Assignee
트러스티즈 오브 터프츠 칼리지
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Application filed by 트러스티즈 오브 터프츠 칼리지 filed Critical 트러스티즈 오브 터프츠 칼리지
Publication of KR20080030079A publication Critical patent/KR20080030079A/ko
Ceased legal-status Critical Current

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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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (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)
KR1020087002781A 2005-07-05 2006-07-05 섬유아세포 활성 단백질 알파의 억제제 Ceased KR20080030079A (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US69677205P 2005-07-05 2005-07-05
US60/696,772 2005-07-05

Publications (1)

Publication Number Publication Date
KR20080030079A true KR20080030079A (ko) 2008-04-03

Family

ID=37604810

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020087002781A Ceased KR20080030079A (ko) 2005-07-05 2006-07-05 섬유아세포 활성 단백질 알파의 억제제

Country Status (12)

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

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016171446A1 (ko) * 2015-04-20 2016-10-27 동아에스티 주식회사 펩타이드 붕소산 화합물을 함유하는 안정화 약학 제제

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US7399869B2 (en) * 2005-05-19 2008-07-15 Genentech, Inc. Fibroblast activation protein inhibitor compounds and methods
EP1760076A1 (en) * 2005-09-02 2007-03-07 Ferring B.V. FAP Inhibitors
PL2178888T3 (pl) 2007-08-06 2012-11-30 Millennium Pharm Inc Inhibitory proteasomów
US7442830B1 (en) 2007-08-06 2008-10-28 Millenium Pharmaceuticals, Inc. Proteasome inhibitors
WO2009051581A1 (en) * 2007-10-16 2009-04-23 Millennium Pharmaceuticals, Inc. Proteasome inhibitors
US7838673B2 (en) 2007-10-16 2010-11-23 Millennium Pharmaceuticals, Inc. Proteasome inhibitors
EP2730579A1 (en) 2008-06-17 2014-05-14 Millennium Pharmaceuticals, Inc. Boronate ester compounds and pharmaceutical compositions thereof
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.
MX2012011298A (es) 2010-03-31 2012-11-06 Millennium Pharm Inc Derivados del acido 1-amino-2-ciclopropiletilboronico.
PL2753334T3 (pl) * 2011-08-30 2022-12-12 Trustees Of Tufts College Aktywowane przez fap inhibitory proteasomu do leczenia guzów litych
WO2013078059A1 (en) * 2011-11-22 2013-05-30 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
MA39964A (fr) 2014-05-20 2015-11-26 Millennium Pharm Inc Inhibiteurs du protéasome contenant du bore destinés à être utilisés après une thérapie contre le cancer primaire
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
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
CN116474108A (zh) 2016-12-14 2023-07-25 普渡研究基金会 成纤维细胞活化蛋白(fap)-靶向成像和治疗
US11613785B2 (en) 2017-01-09 2023-03-28 Onkosxcel Therapeutics, Llc 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
EP4126053A4 (en) * 2020-03-24 2024-11-20 Trustees Of Tufts College IMAGING AGENTS AND RADIOPHARMACEUTICALS TARGETING FAP, AND USES THEREOF
TW202304469A (zh) * 2021-03-24 2023-02-01 美商杜夫特學院信託管理公司 酸化合物、組合物及方法
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

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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
US5159060A (en) * 1988-05-27 1992-10-27 Mayo Foundation For Medical Education And Research Cytotoxic boronic acid peptide analogs
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
AU2003219652A1 (en) * 2002-01-08 2003-07-30 Eisai Co. Ltd. Eponemycin and epoxomicin analogs and uses thereof
US7691967B2 (en) * 2002-04-30 2010-04-06 Trustees Of Tufts College Smart pro-drugs of serine protease inhibitors
WO2004004661A2 (en) * 2002-07-09 2004-01-15 Point Therapeutics, Inc. Boroproline compound combination therapy
EP1581496A4 (en) * 2002-12-02 2008-04-23 Gilead Sciences Inc 2-SUBSTITUTED 3-PROPENAMIDE DERIVATIVES AND PROCESS FOR THEIR PREPARATION
US7576206B2 (en) * 2003-08-14 2009-08-18 Cephalon, Inc. Proteasome inhibitors and methods of using the same
SG134333A1 (en) * 2003-11-12 2007-08-29 Phenomix Corp Heterocyclic boronic acid compounds
US7399869B2 (en) * 2005-05-19 2008-07-15 Genentech, Inc. Fibroblast activation protein inhibitor compounds and methods

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016171446A1 (ko) * 2015-04-20 2016-10-27 동아에스티 주식회사 펩타이드 붕소산 화합물을 함유하는 안정화 약학 제제

Also Published As

Publication number Publication date
US20090221818A1 (en) 2009-09-03
IL188327A0 (en) 2008-04-13
EP1898899A4 (en) 2009-07-29
US20120077779A1 (en) 2012-03-29
AU2006264305B2 (en) 2012-07-05
CN101247799B (zh) 2013-03-27
NO20080626L (no) 2008-04-02
MX2008000318A (es) 2008-03-11
JP5229897B2 (ja) 2013-07-03
CA2613795A1 (en) 2007-01-11
CN101247799A (zh) 2008-08-20
AU2006264305A1 (en) 2007-01-11
US7998997B2 (en) 2011-08-16
IL217579A (en) 2013-04-30
JP2012140439A (ja) 2012-07-26
EP1898899A1 (en) 2008-03-19
WO2007005991A1 (en) 2007-01-11
BRPI0612607A2 (pt) 2010-12-07
JP2009500423A (ja) 2009-01-08

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