HRP20221320T1 - Fap-aktivirani inhibitori proteasoma za liječenje solidnih tumora - Google Patents

Fap-aktivirani inhibitori proteasoma za liječenje solidnih tumora Download PDF

Info

Publication number
HRP20221320T1
HRP20221320T1 HRP20221320TT HRP20221320T HRP20221320T1 HR P20221320 T1 HRP20221320 T1 HR P20221320T1 HR P20221320T T HRP20221320T T HR P20221320TT HR P20221320 T HRP20221320 T HR P20221320T HR P20221320 T1 HRP20221320 T1 HR P20221320T1
Authority
HR
Croatia
Prior art keywords
alkyl
compound
image
group
aryl
Prior art date
Application number
HRP20221320TT
Other languages
English (en)
Croatian (hr)
Inventor
William W. Bachovchin
Hung-Sen Lai
Sarah E. Poplawski
Original Assignee
Trustees Of Tufts College
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 Trustees Of Tufts College filed Critical Trustees Of Tufts College
Publication of HRP20221320T1 publication Critical patent/HRP20221320T1/hr

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/69Boron compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/64Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/07Tetrapeptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06078Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0808Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/081Tripeptides with the first amino acid being neutral and aliphatic the side chain containing O or S as heteroatoms, e.g. Cys, Ser
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0812Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0821Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10Tetrapeptides
    • C07K5/1002Tetrapeptides with the first amino acid being neutral
    • C07K5/1016Tetrapeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/574Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Gastroenterology & Hepatology (AREA)
  • General Physics & Mathematics (AREA)
  • Physics & Mathematics (AREA)
  • Analytical Chemistry (AREA)
  • Cell Biology (AREA)
  • Pathology (AREA)
  • Food Science & Technology (AREA)
  • Oncology (AREA)
  • Hospice & Palliative Care (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
HRP20221320TT 2011-08-30 2012-08-30 Fap-aktivirani inhibitori proteasoma za liječenje solidnih tumora HRP20221320T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161528824P 2011-08-30 2011-08-30
PCT/US2012/053140 WO2013033396A2 (en) 2011-08-30 2012-08-30 Fap-activated proteasome inhibitors for treating solid tumors
EP12827686.2A EP2753334B1 (en) 2011-08-30 2012-08-30 Fap-activated proteasome inhibitors for treating solid tumors

Publications (1)

Publication Number Publication Date
HRP20221320T1 true HRP20221320T1 (hr) 2023-01-06

Family

ID=47757170

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20221320TT HRP20221320T1 (hr) 2011-08-30 2012-08-30 Fap-aktivirani inhibitori proteasoma za liječenje solidnih tumora

Country Status (14)

Country Link
US (6) US9597410B2 (enExample)
EP (2) EP4144354B1 (enExample)
JP (2) JP6207509B2 (enExample)
CN (2) CN108383893A (enExample)
AU (2) AU2012301810B2 (enExample)
CA (1) CA2846852C (enExample)
DK (1) DK2753334T3 (enExample)
ES (1) ES2929179T3 (enExample)
HR (1) HRP20221320T1 (enExample)
HU (1) HUE060305T2 (enExample)
PL (1) PL2753334T3 (enExample)
PT (1) PT2753334T (enExample)
SI (1) SI2753334T1 (enExample)
WO (1) WO2013033396A2 (enExample)

Families Citing this family (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4144354B1 (en) 2011-08-30 2025-11-26 Trustees Of Tufts College Fap-activated proteasome inhibitors for treating solid tumors
CA2893239A1 (en) * 2012-12-03 2014-06-12 F. Hoffmann-La Roche Ag Substituted triazole and imidazole compounds
WO2014200969A2 (en) * 2013-06-10 2014-12-18 Millennium Pharmaceuticals, Inc. Methods of treatment of cancer
WO2015076359A1 (ja) * 2013-11-21 2015-05-28 国立大学法人北海道大学 プロテアソーム阻害性化合物
WO2015192124A1 (en) 2014-06-13 2015-12-17 Trustees Of Tufts College Fap-activated therapeutic agents, and uses related thereto
HUE063194T2 (hu) * 2014-06-13 2024-01-28 Bach Biosciences Llc FAP-aktivált terápiás szerek és az azokkal kapcsolatos felhasználások
ES2785551T3 (es) 2014-06-30 2020-10-07 Glykos Finland Oy Derivado de sacárido de una carga útil tóxica y sus conjugados con anticuerpos
JP6608442B2 (ja) 2014-07-14 2019-11-20 セントラックス インターナショナル,インコーポレイテッド 酵素阻害に用いられるエポキシケトン化合物
CN104231047B (zh) * 2014-08-22 2017-06-16 亚飞(上海)生物医药科技有限公司 水溶性靶向激活的紫杉醇衍生物及其制备和用途
EP3184540A4 (en) * 2014-08-22 2018-03-21 Yafei Shanghai Biolog Medicine Science& Technology Specifically activated micromolecular target coupling body in tumor microenvironment and use thereof
WO2016210054A1 (en) * 2015-06-23 2016-12-29 The Board Of Trustees Of The Leland Stanford Junior University Novel rhodol fluorophores for near-infrared imaging
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
CN105938123B (zh) * 2015-12-18 2018-09-14 重庆两江药物研发中心有限公司 一种卡非佐米中间体中杂质的检测方法
EP3426674A4 (en) 2016-03-09 2019-08-14 Blade Therapeutics, Inc. CYCLIC KETO AMID COMPOUNDS AS CALPAIN MODULATORS AND METHOD FOR THE PRODUCTION AND USE THEREOF
JP7164521B2 (ja) 2016-06-21 2022-11-01 オリオン・オフサルモロジー・エルエルシー 炭素環式プロリンアミド誘導体
UA124672C2 (uk) 2016-06-21 2021-10-27 Оріон Офтальмолоджі Ллс Гетероциклічні похідні пролінаміду
AU2017292646A1 (en) 2016-07-05 2019-02-07 Blade Therapeutics, Inc. Calpain modulators and therapeutic uses thereof
KR20190063473A (ko) 2016-09-28 2019-06-07 블레이드 테라퓨틱스, 인크. 칼페인 조정자 및 그 치료학적 용도
US20200237936A1 (en) 2016-12-14 2020-07-30 Purdue Research Foundation Fibroblast activation protein (fap)-targeted imaging and therapy
MA47215A (fr) 2017-01-09 2019-11-13 Bioxcel Therapeutics Inc Procédés prédictifs et diagnostiques pour le cancer de la prostate
JP7022145B2 (ja) * 2017-04-04 2022-02-17 ジェネンテック, インコーポレイテッド 線維芽細胞活性化タンパク質(fap)によって認識される基質とその使用方法
GB201710973D0 (en) 2017-07-07 2017-08-23 Avacta Life Sciences Ltd Scaffold proteins
KR102005030B1 (ko) * 2017-10-31 2019-07-29 충북대학교 산학협력단 프로테아좀 억제제를 유효성분으로 포함하는 신경퇴행성 질환의 예방 또는 치료용 약학적 조성물
CN108191957B (zh) * 2017-12-30 2021-05-04 浙江大学 三肽大环衍生物及其制备方法和应用
EP3746065A4 (en) 2018-01-29 2022-02-16 Cognos Therapeutics Inc. INTRATUMORAL ADMINISTRATION OF BORTEZOMIB
KR102794330B1 (ko) * 2018-02-06 2025-04-11 우니베르시타트 하이델베르크 Fap 억제제
WO2020025037A1 (zh) * 2018-08-02 2020-02-06 正大天晴药业集团股份有限公司 氮杂环丁烷衍生物的硼酸酯
EP3833374B1 (en) 2018-08-06 2024-12-25 University Of Kentucky Research Foundation Proteasome inhibitors
GB201820320D0 (en) * 2018-12-13 2019-01-30 Bicyclerd Ltd Bicyclic peptide ligands specific for FAPalpha
WO2021072212A1 (en) * 2019-10-11 2021-04-15 Mayo Foundation For Medical Education And Research Proteasome inhibitors
CN111235221B (zh) * 2020-01-22 2022-08-05 北京大学第一医院 一种fap抑制剂的活性检测方法
CZ309380B6 (cs) * 2020-03-30 2022-10-26 Ústav organické chemie a biochemie AV ČR v. v. i Sloučeniny pro inhibici fibroblastového aktivačního proteinu
JP2023532199A (ja) 2020-06-17 2023-07-27 ユニヴァーシティー オブ ユタ リサーチ ファウンデーション プロテアソーム阻害剤治療のためのバイオマーカーに基づく患者選択
UY39569A (es) 2020-12-17 2022-07-29 Astrazeneca Ab N-(2-(4-cianotiazolidin-3-il)-2-oxoetil)- quinolin-4-carboxamidas
CN116981479A (zh) * 2020-12-17 2023-10-31 塔夫茨大学信托人 Fap激活的放射治疗诊断法以及与之相关的用途
KR20230158005A (ko) 2021-03-18 2023-11-17 씨젠 인크. 생물학적 활성 화합물의 내재화된 접합체로부터의 선택적 약물 방출
US11806405B1 (en) 2021-07-19 2023-11-07 Zeno Management, Inc. Immunoconjugates and methods
TWI869142B (zh) * 2022-12-27 2025-01-01 大陸商上海美悦生物科技發展有限公司 三肽環氧酮化合物、藥物組合物及其製備方法和用途
WO2025159301A1 (ko) * 2024-01-24 2025-07-31 서울대학교산학협력단 섬유아세포 활성화 단백질에 의해 활성화되는 프로드러그 화합물

Family Cites Families (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4499082A (en) 1983-12-05 1985-02-12 E. I. Du Pont De Nemours And Company α-Aminoboronic acid peptides
AU600226B2 (en) 1985-02-04 1990-08-09 Merrell Pharmaceuticals Inc. Novel peptidase inhibitors
US4935493A (en) 1987-10-06 1990-06-19 E. I. Du Pont De Nemours And Company Protease inhibitors
US5462928A (en) 1990-04-14 1995-10-31 New England Medical Center Hospitals, Inc. Inhibitors of dipeptidyl-aminopeptidase type IV
US6825169B1 (en) 1991-10-22 2004-11-30 Trustees Of Tufts College Inhibitors of dipeptidyl-aminopeptidase type IV
EP0760059B1 (en) 1994-03-11 2006-05-31 Wilson Greatbatch Ltd. Low power electromagnetic pump
US5580979A (en) 1994-03-15 1996-12-03 Trustees Of Tufts University Phosphotyrosine peptidomimetics for inhibiting SH2 domain interactions
US6083903A (en) * 1994-10-28 2000-07-04 Leukosite, Inc. Boronic ester and acid compounds, synthesis and uses
US6180402B1 (en) 1996-11-20 2001-01-30 Qlt Inc. Method for inhibiting apoptosis induced by photodynamic therapy using a cysteine or serine protease inhibitor
WO1999016864A1 (en) 1997-09-29 1999-04-08 Point Therapeutics, Inc. Stimulation of hematopoietic cells in vitro
AU766219B2 (en) 1998-02-02 2003-10-09 1149336 Ontario Inc. Method of regulating glucose metabolism, and reagents related thereto
JP2002513762A (ja) 1998-05-04 2002-05-14 ポイント セラピューティクス, インコーポレイテッド 造血刺激
EP1084129B1 (en) 1998-06-05 2003-01-22 Point Therapeutics, Inc. Cyclic boroproline compounds
US6979697B1 (en) 1998-08-21 2005-12-27 Point Therapeutics, Inc. Regulation of substrate activity
WO2000048302A1 (en) 1999-02-11 2000-08-17 Battelle Memorial Institute Power supply
US6890904B1 (en) 1999-05-25 2005-05-10 Point Therapeutics, Inc. Anti-tumor agents
AU2002360453C1 (en) 2001-11-26 2009-06-18 The Brigham And Women's Hospital, Inc. Methods for treating autoimmune disorders, and reagents related thereto
JP4771661B2 (ja) 2001-11-26 2011-09-14 トラスティーズ オブ タフツ カレッジ Post−プロリン開裂酵素の擬ペプチド性阻害剤
JP2005531540A (ja) * 2002-04-30 2005-10-20 トラスティーズ・オブ・タフツ・カレッジ セリンプロテアーゼ阻害剤のスマートプロドラッグ
JP2006507352A (ja) 2002-07-09 2006-03-02 ポイント セラピューティクス, インコーポレイテッド イソロイシンのボロプロリン化合物に関する方法および組成物
WO2004103390A2 (en) 2003-05-15 2004-12-02 Trustees Of Tufts College Stable analogs of peptide and polypeptide therapeutics
US20050203027A1 (en) 2004-02-23 2005-09-15 Trustees Of Tufts College Inhibitors of dipeptidylpeptidase IV
US20060063719A1 (en) 2004-09-21 2006-03-23 Point Therapeutics, Inc. Methods for treating diabetes
CA2606785A1 (en) 2005-05-19 2006-11-23 Genentech, Inc. Fibroblast activation protein inhibitor compounds and methods
WO2007005991A1 (en) * 2005-07-05 2007-01-11 Trustees Of Tufts College Inhibitors of fibroblast activation protein alpha
AU2006201635A1 (en) * 2005-10-20 2007-05-10 Ludwig Institute For Cancer Research Novel inhibitors and methods for their preparation
WO2007100374A2 (en) * 2005-12-19 2007-09-07 Trustees Of Tufts College Soft protease inhibitors and pro-soft forms thereof
CA2656393A1 (en) * 2006-06-30 2008-01-10 Schering Corporation Method of using substituted piperidines that increase p53 activity
JP2010523477A (ja) * 2007-03-20 2010-07-15 トラスティーズ オブ タフツ カレッジ 線維芽細胞活性化タンパク質の阻害剤、およびそれを使用する方法
WO2008116053A2 (en) * 2007-03-20 2008-09-25 Trustees Of Tufts College Fap-activated chemotherapeutic compounds, and methods of use thereof
WO2009006473A2 (en) * 2007-07-05 2009-01-08 Trustees Of Tufts College Pro-soft polypeptide proteasome inhibitors, and methods of use thereof
ES2390606T3 (es) * 2007-08-06 2012-11-14 Millennium Pharmaceuticals, Inc. Inhibidores de proteasomas
WO2009024542A2 (en) * 2007-08-17 2009-02-26 Boehringer Ingelheim International Gmbh Purin derivatives for use in the treatment of fab-related diseases
MX2010009766A (es) * 2008-03-03 2010-09-28 Univ Kansas State Ensayo de proteasa.
JP5801585B2 (ja) 2011-03-30 2015-10-28 株式会社ケーヒン 燃料噴射制御システム
EP4144354B1 (en) * 2011-08-30 2025-11-26 Trustees Of Tufts College Fap-activated proteasome inhibitors for treating solid tumors

Also Published As

Publication number Publication date
WO2013033396A3 (en) 2014-05-08
AU2017204121A1 (en) 2017-07-06
JP2018016629A (ja) 2018-02-01
AU2012301810A1 (en) 2014-04-10
EP4144354B1 (en) 2025-11-26
AU2012301810B2 (en) 2017-06-01
US20250367304A1 (en) 2025-12-04
CA2846852C (en) 2021-01-12
US20160346401A1 (en) 2016-12-01
EP4144354A1 (en) 2023-03-08
CN108383893A (zh) 2018-08-10
ES2929179T3 (es) 2022-11-25
EP2753334B1 (en) 2022-10-19
JP2014527070A (ja) 2014-10-09
PL2753334T3 (pl) 2022-12-12
US20210379190A1 (en) 2021-12-09
US9956297B2 (en) 2018-05-01
US11065339B2 (en) 2021-07-20
EP2753334A4 (en) 2015-07-01
EP2753334A2 (en) 2014-07-16
WO2013033396A2 (en) 2013-03-07
CA2846852A1 (en) 2013-03-07
JP6207509B2 (ja) 2017-10-04
HUE060305T2 (hu) 2023-02-28
PT2753334T (pt) 2022-11-03
US20190054181A1 (en) 2019-02-21
US10517955B2 (en) 2019-12-31
CN103945856A (zh) 2014-07-23
US20140255300A1 (en) 2014-09-11
SI2753334T1 (sl) 2023-01-31
US12214047B2 (en) 2025-02-04
US20200323994A1 (en) 2020-10-15
DK2753334T3 (da) 2022-11-07
US9597410B2 (en) 2017-03-21

Similar Documents

Publication Publication Date Title
HRP20221320T1 (hr) Fap-aktivirani inhibitori proteasoma za liječenje solidnih tumora
RU2441869C2 (ru) Противовирусные соединения
HRP20160083T1 (hr) Makrocikliäśki inhibitori serinske proteaze virusa hepatitisa c izvedeni iz prolina
JP2018016629A5 (enExample)
ES2576497T3 (es) Compuesto de piperidina novedoso o sal del mismo
HRP20240861T1 (hr) Derivati 6-(4-amino-3-metil-2-oksa-8-azaspiro[4.5]dekan-8-il)-3-(2,3-dihlorofenil)-2-metilpirimidin-4(3h)-ona i srodni spojevi kao inhibitori ptpn11 (shp2) za liječenje raka
JP2017528498A5 (enExample)
JP2011511840A5 (enExample)
JP2009538897A5 (enExample)
JP2017528524A5 (enExample)
JP2014518546A5 (enExample)
SI2809657T1 (en) New therapeutic agents
JP2007077157A5 (enExample)
JP2012528166A5 (enExample)
HRP20150489T1 (hr) Imidazo[4,5-c]kinolini kao inhibitori dna-pk
JP2008535903A5 (enExample)
FI3307727T3 (fi) Erk1:n ja erk2:n heterosyklisiä estäjiä ja niiden käyttö syövän hoidossa
HRP20220886T1 (hr) Pripravci i postupci za proizvodnju pirimidina i spojeva piridina s btk inhibicijskom aktivnošću
HRP20230854T1 (hr) Fap-aktivirana terapeutska sredstva i s njima povezane uporabe
RU2009125441A (ru) Химические соединения
HRP20090459T1 (hr) Aminofenil derivati kao novi inhibitori histonskih deacetilaza
RU2009102252A (ru) Хиноксалинилмакроциклические ингибиторы серинпротеазы вируса гепатита с
JP2008543854A5 (enExample)
JP2011511841A5 (enExample)
JP2010031025A5 (enExample)