JP5229897B2 - 線維芽細胞活性化タンパクα阻害剤 - Google Patents

線維芽細胞活性化タンパクα阻害剤 Download PDF

Info

Publication number
JP5229897B2
JP5229897B2 JP2008520373A JP2008520373A JP5229897B2 JP 5229897 B2 JP5229897 B2 JP 5229897B2 JP 2008520373 A JP2008520373 A JP 2008520373A JP 2008520373 A JP2008520373 A JP 2008520373A JP 5229897 B2 JP5229897 B2 JP 5229897B2
Authority
JP
Japan
Prior art keywords
compound
compound according
group
alkyl
cancer
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
JP2008520373A
Other languages
English (en)
Japanese (ja)
Other versions
JP2009500423A5 (OSRAM
JP2009500423A (ja
Inventor
ダブリュ バチョフチン，ウィリアム
ライ，フン−セン
Original Assignee
タフツ ユニバーシティー／トラスティーズ オブ タフツ カレッジ
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 タフツ ユニバーシティー／トラスティーズ オブ タフツ カレッジ filed Critical タフツ ユニバーシティー／トラスティーズ オブ タフツ カレッジ
Publication of JP2009500423A publication Critical patent/JP2009500423A/ja
Publication of JP2009500423A5 publication Critical patent/JP2009500423A5/ja
Application granted granted Critical
Publication of JP5229897B2 publication Critical patent/JP5229897B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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

Landscapes

  • 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)
JP2008520373A 2005-07-05 2006-07-05 線維芽細胞活性化タンパクα阻害剤 Expired - Fee Related JP5229897B2 (ja)

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

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2012033777A Division JP2012140439A (ja) 2005-07-05 2012-02-20 線維芽細胞活性化タンパクα阻害剤

Publications (3)

Publication Number Publication Date
JP2009500423A JP2009500423A (ja) 2009-01-08
JP2009500423A5 JP2009500423A5 (OSRAM) 2010-08-26
JP5229897B2 true JP5229897B2 (ja) 2013-07-03

Family

ID=37604810

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2008520373A Expired - Fee Related JP5229897B2 (ja) 2005-07-05 2006-07-05 線維芽細胞活性化タンパクα阻害剤
JP2012033777A Pending JP2012140439A (ja) 2005-07-05 2012-02-20 線維芽細胞活性化タンパクα阻害剤

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2012033777A Pending JP2012140439A (ja) 2005-07-05 2012-02-20 線維芽細胞活性化タンパクα阻害剤

Country Status (12)

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

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006125227A2 (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
KR20150010802A (ko) 2007-08-06 2015-01-28 밀레니엄 파머슈티컬스 인코퍼레이티드 프로테아좀 억제제
US7442830B1 (en) 2007-08-06 2008-10-28 Millenium 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
US20090325903A1 (en) 2008-06-17 2009-12-31 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.
US8513218B2 (en) 2010-03-31 2013-08-20 Millennium Pharmaceuticals, Inc. Derivatives of 1-amino-2-cyclopropylethylboronic acid
HUE060305T2 (hu) * 2011-08-30 2023-02-28 Tufts College FAP-aktivált proteaszóma inhibitorok a szolid tumorok kezelésére
CN106075450A (zh) * 2011-11-22 2016-11-09 塔夫茨大学信托人 用于树突状细胞癌症疫苗的小分子增强剂
US20150202218A1 (en) * 2012-08-02 2015-07-23 Trustees Of Tufts College Broad Spectrum Inhibitors of the Post Proline Cleaving Enzymes for Treatment of Hepatitis C Virus Infections
WO2015179443A1 (en) 2014-05-20 2015-11-26 Millennium Pharmaceuticals. Inc. Boron-containing proteasome inhibitors for use after primary cancer therapy
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
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
TW202202150A (zh) * 2020-03-24 2022-01-16 美商杜夫特學院信託管理公司 靶向fap之放射性藥品及造影劑，與其相關用途
CA3212974A1 (en) * 2021-03-24 2022-09-29 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

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
EP1463719A2 (en) * 2002-01-08 2004-10-06 Eisai Co., Ltd Eponemycin and epoxomicin analogs and uses thereof
EP2204181A3 (en) * 2002-04-30 2010-09-22 Trustees Of Tufts College Protease inhibitors
WO2004004661A2 (en) * 2002-07-09 2004-01-15 Point Therapeutics, Inc. Boroproline compound combination therapy
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
US7674913B2 (en) * 2003-11-12 2010-03-09 Phenomix Corporation Heterocyclic boronic acid compounds
WO2006125227A2 (en) * 2005-05-19 2006-11-23 Genentech, Inc. Fibroblast activation protein inhibitor compounds and methods

Also Published As

Publication number Publication date
IL188327A0 (en) 2008-04-13
CA2613795A1 (en) 2007-01-11
AU2006264305B2 (en) 2012-07-05
CN101247799B (zh) 2013-03-27
IL217579A (en) 2013-04-30
BRPI0612607A2 (pt) 2010-12-07
WO2007005991A1 (en) 2007-01-11
US7998997B2 (en) 2011-08-16
AU2006264305A1 (en) 2007-01-11
JP2012140439A (ja) 2012-07-26
KR20080030079A (ko) 2008-04-03
EP1898899A4 (en) 2009-07-29
CN101247799A (zh) 2008-08-20
NO20080626L (no) 2008-04-02
US20120077779A1 (en) 2012-03-29
EP1898899A1 (en) 2008-03-19
JP2009500423A (ja) 2009-01-08
US20090221818A1 (en) 2009-09-03
MX2008000318A (es) 2008-03-11

Similar Documents

Publication Publication Date Title
JP5229897B2 (ja) 線維芽細胞活性化タンパクα阻害剤
JP4771661B2 (ja) Ｐｏｓｔ−プロリン開裂酵素の擬ペプチド性阻害剤
JP4966659B2 (ja) 異なる細胞に機能的に影響を及ぼし、免疫性疾患、炎症性疾患、神経疾患、およびその他の疾患を治療するための二重のアラニルアミノペプチダーゼおよびジペプチジルペプチダーゼｉｖの阻害剤
EP1228061A1 (en) Dipeptidyl peptidase iv inhibitors and methods of making and using dipeptidyl peptidase iv inhibitors
ES2268327T3 (es) Uso de un selectivo de un receptor de ep4 para el tratamiento de enfermedades.
US20040152745A1 (en) Dipeptidyl peptidase IV inhibitors and methods of making and using dipeptidyl peptidase IV inhibitors
US6632830B1 (en) ACE-2 inhibiting compounds and methods of use thereof
CA2761489C (en) High penetration prodrug compositions of peptides and peptide-related compounds
CA2349575A1 (en) Nitrosated and nitrosylated h2 receptor antagonist compounds, compositions and methods of use
JP2003520849A (ja) 酵素ｄｐｐ−ｉｖの阻害剤であるｎ−置換２−シアノピロールおよび−ピロリン
JP4954864B2 (ja) イオンチャネル調節化合物のプロドラッグおよびその使用
JP2001520674A (ja) ペプチジル−２−アミノ−１−ヒドロキシアルカンスルホン酸システインプロテアーゼインヒビター
EP0201057A2 (en) Bone targeted inhibitors of carbonic anhydrase
JP5300485B2 (ja) 炎症性疾患および他の疾患の治療のためのプロドラッグとしての新規なペプチダーゼ二重阻害剤
AU2008339610A1 (en) Methods of peptide modification
CN101538311B (zh) α-氨基酰环酰亚胺类肽金属蛋白酶抑制剂及其应用
WO2010065461A1 (en) Tri-peptide inhibitors of serine elastases
JP2012519187A (ja) ソフトプロテアーゼ阻害剤およびそのプロソフト型
AU2011265405A1 (en) Proteasome inhibitors and methods of using the same

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20090706

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20090706

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20100618

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20111018

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20120117

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20120124

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20120220

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20120410

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20120703

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20130212

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20130314

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20160329

Year of fee payment: 3

R150 Certificate of patent or registration of utility model

Free format text: JAPANESE INTERMEDIATE CODE: R150

LAPS Cancellation because of no payment of annual fees