DK2753334T3 - Fap-aktiverede proteasomhæmmere til behandling af solide tumorer - Google Patents

Fap-aktiverede proteasomhæmmere til behandling af solide tumorer Download PDF

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Publication number
DK2753334T3
DK2753334T3 DK12827686.2T DK12827686T DK2753334T3 DK 2753334 T3 DK2753334 T3 DK 2753334T3 DK 12827686 T DK12827686 T DK 12827686T DK 2753334 T3 DK2753334 T3 DK 2753334T3
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fap
treatment
solid tumors
proteasome inhibitors
activated proteasome
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DK12827686.2T
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English (en)
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Hung-Sen Lai
Sarah E Poplawski
William W Bachovchin
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Tufts College
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/69—Boron compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal 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
    • A61K47/51—Medicinal 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
    • A61K47/62—Medicinal 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
    • A61K47/64—Drug-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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/07—Tetrapeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal 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
    • A61K47/51—Medicinal 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
    • A61K47/54—Medicinal 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0808—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/081—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing O or S as heteroatoms, e.g. Cys, Ser
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0821—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
    • C07K5/1016—Tetrapeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/574—Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Gastroenterology & Hepatology (AREA)
  • General Physics & Mathematics (AREA)
  • Analytical Chemistry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pathology (AREA)
  • Biotechnology (AREA)
  • Cell Biology (AREA)
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  • Microbiology (AREA)
  • Food Science & Technology (AREA)
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  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Vascular Medicine (AREA)
DK12827686.2T 2011-08-30 2012-08-30 Fap-aktiverede proteasomhæmmere til behandling af solide tumorer DK2753334T3 (da)

Applications Claiming Priority (2)

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

Publications (1)

Publication Number Publication Date
DK2753334T3 true DK2753334T3 (da) 2022-11-07

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DK12827686.2T DK2753334T3 (da) 2011-08-30 2012-08-30 Fap-aktiverede proteasomhæmmere til behandling af solide tumorer

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US (5) US9597410B2 (da)
EP (2) EP4144354A1 (da)
JP (2) JP6207509B2 (da)
CN (2) CN103945856A (da)
AU (2) AU2012301810B2 (da)
CA (1) CA2846852C (da)
DK (1) DK2753334T3 (da)
ES (1) ES2929179T3 (da)
HR (1) HRP20221320T1 (da)
HU (1) HUE060305T2 (da)
PL (1) PL2753334T3 (da)
PT (1) PT2753334T (da)
SI (1) SI2753334T1 (da)
WO (1) WO2013033396A2 (da)

Families Citing this family (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL2753334T3 (pl) * 2011-08-30 2022-12-12 Trustees Of Tufts College Aktywowane przez fap inhibitory proteasomu do leczenia guzów litych
BR112015012885A2 (pt) * 2012-12-03 2017-07-11 Hoffmann La Roche composições triazol e imidazol substituídas
US20170035917A1 (en) * 2013-06-10 2017-02-09 Millennium Pharmaceuticals, Inc. Methods of treatment of cancer
JP6468562B2 (ja) * 2013-11-21 2019-02-13 国立大学法人北海道大学 プロテアソーム阻害性化合物
US10245248B2 (en) 2014-06-13 2019-04-02 Bach Biosciences, Llc FAP-activated therapeutic agents, and uses related thereto
US9737556B2 (en) 2014-06-13 2017-08-22 Trustees Of Tufts College FAP-activated therapeutic agents, and uses related thereto
AU2015282627B2 (en) 2014-06-30 2020-04-02 Glykos Finland Oy Saccharide derivative of a toxic payload and antibody conjugates thereof
PT3166933T (pt) 2014-07-14 2018-12-06 Centrax Int Inc Compostos de epoxicetona para inibição de enzimas
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
US10682371B2 (en) 2014-08-22 2020-06-16 Yafei Shanghai Biolog Medicine Science & Technology Co. Ltd. Small molecule conjugates specifically activated in tumor microenvironment for targeting and use thereof
US10675364B2 (en) * 2015-06-23 2020-06-09 The Board Of Trustees Of The Leland Stanford Junior University 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
CN109476637B (zh) 2016-06-21 2022-02-01 奥瑞恩眼科有限责任公司 杂环脯氨酰胺衍生物
US10526315B2 (en) 2016-06-21 2020-01-07 Orion Ophthalmology LLC Carbocyclic prolinamide derivatives
AU2017292646A1 (en) 2016-07-05 2019-02-07 Blade Therapeutics, Inc. Calpain modulators and therapeutic uses thereof
SG10201912574WA (en) 2016-09-28 2020-02-27 Blade Therapeutics Inc Calpain modulators and therapeutic uses thereof
WO2018111989A1 (en) 2016-12-14 2018-06-21 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
EP3606939A4 (en) * 2017-04-04 2021-01-20 F. Hoffmann-La Roche AG SUBSTRATES RECOGNIZED BY FIBROBLAST ACTIVATION PROTEIN (FAP) AND METHOD OF USING THEM
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
CN111867573A (zh) 2018-01-29 2020-10-30 科诺斯治疗学公司 硼替佐米的瘤内递送
IL276594B2 (en) * 2018-02-06 2023-11-01 Univ Heidelberg FAP inhibitors
BR112021001963B1 (pt) 2018-08-02 2024-02-15 Chia Tai Tianqing Pharmaceutical Group Co., Ltd Compostos de borato de um derivado de azetidina, composição farmacêutica que compreende os ditos compostos e uso dos mesmos para prevenção ou tratamento de mieloma múltiplo
EP3833374A4 (en) * 2018-08-06 2022-04-27 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
CN115968411A (zh) * 2020-06-17 2023-04-14 犹他大学研究基金会 基于生物标记的用于蛋白酶体抑制剂治疗的患者选择
JP2023554396A (ja) * 2020-12-17 2023-12-27 トラスティーズ オブ タフツ カレッジ Ｆａｐ活性化ラジオセラノスティクスおよび関連する使用
US20240101549A1 (en) 2020-12-17 2024-03-28 Astrazeneca Ab N-(2-(4-cyanothiazolidin-3-yl)-2-oxoethyl)-quinoline-4-carboxamides
US11806405B1 (en) 2021-07-19 2023-11-07 Zeno Management, Inc. Immunoconjugates and methods

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
ZA86746B (en) 1985-02-04 1986-09-24 Merrell Dow Pharma 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
DE69535019T2 (de) 1994-03-11 2007-01-04 Wilson Greatbatch, Ltd. Elektromagnetische pumpe mit geringem vermögen
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
ES2285785T3 (es) 1997-09-29 2007-11-16 Point Therapeutics, Inc. Estimulacion de celulas hematopoyeticas in vitro.
CA2819705C (en) 1998-02-02 2014-07-08 Trustees Of Tufts College Method of regulating glucose metabolism, and reagents related thereto
MY132924A (en) 1998-05-04 2007-10-31 Point Therapeutics Inc Hematopoietic stimulation
WO1999062914A1 (en) 1998-06-05 1999-12-09 Point Therapeutics, Inc. Cyclic boroproline compounds
US6979697B1 (en) 1998-08-21 2005-12-27 Point Therapeutics, Inc. Regulation of substrate activity
CA2362620A1 (en) 1999-02-11 2000-08-17 Joseph A. Stets Power supply
US6890904B1 (en) 1999-05-25 2005-05-10 Point Therapeutics, Inc. Anti-tumor agents
EP1487471A4 (en) 2001-11-26 2010-03-10 Tufts College METHOD FOR TREATING AUTOIMMUNE DISEASES AND ASSOCIATED REAGENTS
CA2468192A1 (en) 2001-11-26 2003-06-05 Trustees Of Tufts College Peptidomimetic inhibitors of post-proline cleaving enzymes
AU2003228793B2 (en) 2002-04-30 2008-01-03 Trustees Of Tufts College Smart Pro-Drugs of Serine Protease Inhibitors
AU2003248921A1 (en) 2002-07-09 2004-01-23 Point Therapeutics, Inc. Boroproline compound combination therapy
CA2525574C (en) 2003-05-15 2015-06-30 Trustees Of Tufts College Stable analogs of peptide and polypeptide therapeutics
BRPI0507972A (pt) 2004-02-23 2007-07-24 Tufts College composto ,composição farmacêutica , uso de um composto, método para inibição da atividade proteolìtica de uma enzima de clivagem pós prolina e composição farmacêutica embalada
US20060063719A1 (en) 2004-09-21 2006-03-23 Point Therapeutics, Inc. Methods for treating diabetes
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
KR20080030079A (ko) * 2005-07-05 2008-04-03 트러스티즈 오브 터프츠 칼리지 섬유아세포 활성 단백질 알파의 억제제
AU2006201635A1 (en) * 2005-10-20 2007-05-10 Ludwig Institute For Cancer Research Novel inhibitors and methods for their preparation
JP5270369B2 (ja) * 2005-12-19 2013-08-21 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 ソフトプロテアーゼ抑制剤およびそのプロソフト型
US20080004286A1 (en) * 2006-06-30 2008-01-03 Schering Corporation Method of Using Substituted Piperidines that Increase P53 Activity
WO2008116053A2 (en) * 2007-03-20 2008-09-25 Trustees Of Tufts College Fap-activated chemotherapeutic compounds, and methods of use thereof
AU2008228863A1 (en) * 2007-03-20 2008-09-25 Trustees Of Tufts College Inhibitors of fibroblast activation protein, 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
MY161991A (en) * 2007-08-06 2017-05-31 Millennium Pharm Inc Proteasome inhibitors
AU2008290582B2 (en) * 2007-08-17 2014-08-14 Boehringer Ingelheim International Gmbh Purin derivatives for use in the treatment of fab-related diseases
WO2009111470A2 (en) * 2008-03-03 2009-09-11 Kansas State University Research Foundation Protease assay
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
PL2753334T3 (pl) 2011-08-30 2022-12-12 Trustees Of Tufts College Aktywowane przez fap inhibitory proteasomu do leczenia guzów litych

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HUE060305T2 (hu) 2023-02-28
SI2753334T1 (sl) 2023-01-31
US9956297B2 (en) 2018-05-01
PT2753334T (pt) 2022-11-03
CN103945856A (zh) 2014-07-23
HRP20221320T1 (hr) 2023-01-06
US11065339B2 (en) 2021-07-20
CA2846852A1 (en) 2013-03-07
US20210379190A1 (en) 2021-12-09
US20190054181A1 (en) 2019-02-21
JP2014527070A (ja) 2014-10-09
US10517955B2 (en) 2019-12-31
EP2753334B1 (en) 2022-10-19
PL2753334T3 (pl) 2022-12-12
EP4144354A1 (en) 2023-03-08
EP2753334A2 (en) 2014-07-16
ES2929179T3 (es) 2022-11-25
AU2017204121A1 (en) 2017-07-06
US9597410B2 (en) 2017-03-21
AU2012301810A1 (en) 2014-04-10
US20200323994A1 (en) 2020-10-15
CN108383893A (zh) 2018-08-10
US20160346401A1 (en) 2016-12-01
JP6207509B2 (ja) 2017-10-04
WO2013033396A3 (en) 2014-05-08
AU2012301810B2 (en) 2017-06-01
WO2013033396A2 (en) 2013-03-07
JP2018016629A (ja) 2018-02-01
EP2753334A4 (en) 2015-07-01
CA2846852C (en) 2021-01-12
US20140255300A1 (en) 2014-09-11

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