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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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (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 (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)

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

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2008545661A (ja) * 2005-05-19 2008-12-18 ジェネンテック・インコーポレーテッド 線維芽細胞活性化タンパク質阻害剤化合物および
EP1760076A1 (en) * 2005-09-02 2007-03-07 Ferring B.V. FAP Inhibitors
US7442830B1 (en) 2007-08-06 2008-10-28 Millenium Pharmaceuticals, Inc. Proteasome inhibitors
EP2527347A1 (en) 2007-08-06 2012-11-28 Millennium Pharmaceuticals, Inc. Proteasome inhibitors
JP5600595B2 (ja) * 2007-10-16 2014-10-01 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 プロテアソーム阻害剤
US7838673B2 (en) 2007-10-16 2010-11-23 Millennium Pharmaceuticals, Inc. Proteasome inhibitors
AU2009260778B2 (en) 2008-06-17 2014-08-28 Takeda Pharmaceutical Company Limited 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.
CA2794334C (en) 2010-03-31 2018-06-12 Millennium Pharmaceuticals, Inc. Derivatives of 1-amino-2-cyclopropylethylboronic acid
CN108383893A (zh) * 2011-08-30 2018-08-10 塔夫茨大学信托人 用于治疗实体瘤的fap-活化的蛋白酶体抑制剂
HK1201871A1 (en) 2011-11-22 2015-09-11 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
TWI746422B (zh) 2014-05-20 2021-11-21 美商千禧製藥公司 用於癌症治療的方法
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
CN110291401B (zh) 2016-12-14 2023-04-11 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
MX2022011842A (es) * 2020-03-24 2022-10-20 Tufts College Agentes de imagen y radiofarmacos dirigidos a fap, y usos relacionados con los mismos.
JP2024511054A (ja) * 2021-03-24 2024-03-12 トラスティーズ オブ タフツ カレッジ ボロン酸化合物、組成物および方法
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

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
JP4412586B2 (ja) * 2002-01-08 2010-02-10 エーザイ・アール・アンド・ディー・マネジメント株式会社 エポネマイシンおよびエポキソマイシン類似物およびそれらの用途
CA2484551A1 (en) * 2002-04-30 2003-11-13 Trustees Of Tufts College Smart pro-drugs of serine protease inhibitors
EP1578362A4 (en) * 2002-07-09 2008-11-05 Point Therapeutics Inc COMBINATION THERAPY WITH A BOROPROLINE COMPOUND
AU2003297612A1 (en) * 2002-12-02 2004-06-23 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
US7674913B2 (en) * 2003-11-12 2010-03-09 Phenomix Corporation Heterocyclic boronic acid compounds
JP2008545661A (ja) 2005-05-19 2008-12-18 ジェネンテック・インコーポレーテッド 線維芽細胞活性化タンパク質阻害剤化合物および

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

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