CA2468192A1 - Peptidomimetic inhibitors of post-proline cleaving enzymes - Google Patents

Peptidomimetic inhibitors of post-proline cleaving enzymes Download PDF

Info

Publication number
CA2468192A1
CA2468192A1 CA002468192A CA2468192A CA2468192A1 CA 2468192 A1 CA2468192 A1 CA 2468192A1 CA 002468192 A CA002468192 A CA 002468192A CA 2468192 A CA2468192 A CA 2468192A CA 2468192 A1 CA2468192 A1 CA 2468192A1
Authority
CA
Canada
Prior art keywords
hydrogen
inhibitor
alkyl
alkenyl
cycloalkyl
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.)
Abandoned
Application number
CA002468192A
Other languages
English (en)
French (fr)
Inventor
William W. Bachovchin
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Tufts University
Original Assignee
Individual
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 Individual filed Critical Individual
Priority to CA2837936A priority Critical patent/CA2837936A1/en
Publication of CA2468192A1 publication Critical patent/CA2468192A1/en
Abandoned legal-status Critical Current

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
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22Hormones
    • A61K38/28Insulins
    • 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
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic 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
    • C07D207/04Heterocyclic 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
    • C07D207/10Heterocyclic 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
    • C07D207/16Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02Boron compounds
    • C07F5/025Boronic and borinic acid compounds

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Zoology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Immunology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Emergency Medicine (AREA)
  • Dermatology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CA002468192A 2001-11-26 2002-11-26 Peptidomimetic inhibitors of post-proline cleaving enzymes Abandoned CA2468192A1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CA2837936A CA2837936A1 (en) 2001-11-26 2002-11-26 Peptidomimetic inhibitors of post-proline cleaving enzymes

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US33351901P 2001-11-26 2001-11-26
US60/333,519 2001-11-26
US40553002P 2002-08-23 2002-08-23
US60/405,530 2002-08-23
PCT/US2002/038053 WO2003045977A2 (en) 2001-11-26 2002-11-26 Peptidomimetic Inhibitors of Post-Proline Cleaving Enzymes

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CA2837936A Division CA2837936A1 (en) 2001-11-26 2002-11-26 Peptidomimetic inhibitors of post-proline cleaving enzymes

Publications (1)

Publication Number Publication Date
CA2468192A1 true CA2468192A1 (en) 2003-06-05

Family

ID=26988769

Family Applications (2)

Application Number Title Priority Date Filing Date
CA002468192A Abandoned CA2468192A1 (en) 2001-11-26 2002-11-26 Peptidomimetic inhibitors of post-proline cleaving enzymes
CA2837936A Abandoned CA2837936A1 (en) 2001-11-26 2002-11-26 Peptidomimetic inhibitors of post-proline cleaving enzymes

Family Applications After (1)

Application Number Title Priority Date Filing Date
CA2837936A Abandoned CA2837936A1 (en) 2001-11-26 2002-11-26 Peptidomimetic inhibitors of post-proline cleaving enzymes

Country Status (6)

Country Link
US (4) US7727964B2 (enExample)
EP (2) EP2316470A3 (enExample)
JP (3) JP4771661B2 (enExample)
AU (1) AU2002357767C1 (enExample)
CA (2) CA2468192A1 (enExample)
WO (1) WO2003045977A2 (enExample)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7674913B2 (en) 2003-11-12 2010-03-09 Phenomix Corporation Heterocyclic boronic acid compounds
US7767828B2 (en) 2003-11-12 2010-08-03 Phenomix Corporation Methyl and ethyl substituted pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV
US7884217B2 (en) 2003-11-12 2011-02-08 Phenomix Corporation Pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV

Families Citing this family (85)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2304206A1 (en) * 1997-09-29 1999-04-08 Point Therapeutics, Inc. Stimulation of hematopoietic cells in vitro
EP2823812A1 (en) * 1998-02-02 2015-01-14 Trustees Of Tufts College Dipeptidylpeptidase IV inhibitors for use in the treatment of Type II diabetes
US6979697B1 (en) * 1998-08-21 2005-12-27 Point Therapeutics, Inc. Regulation of substrate activity
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
EP2316470A3 (en) * 2001-11-26 2011-08-24 Trustees Of Tufts College Peptidomimetic inhibitors of post-proline cleaving enzymes
CA2484551A1 (en) * 2002-04-30 2003-11-13 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
CA2518465A1 (en) 2003-03-25 2004-10-14 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
JP4806628B2 (ja) 2003-05-05 2011-11-02 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤
US7638638B2 (en) 2003-05-14 2009-12-29 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
US7678909B1 (en) 2003-08-13 2010-03-16 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
KR20060041309A (ko) 2003-08-13 2006-05-11 다케다 야쿠힌 고교 가부시키가이샤 4-피리미돈 유도체 및 펩티딜 펩티다제 저해제로서의 그의용도
US7169926B1 (en) 2003-08-13 2007-01-30 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
JP2007505121A (ja) 2003-09-08 2007-03-08 武田薬品工業株式会社 ジペプチジルぺプチダーゼ阻害剤
AR046330A1 (es) * 2003-09-09 2005-12-07 Japan Tobacco Inc Inhibidor de dipeptidilpeptidasa iv
DE10348044A1 (de) 2003-10-15 2005-05-19 Imtm Gmbh Duale Alanyl-Aminopeptidase- und Dipeptidylpeptidase IV-Inhibitoren zur funktionellen Beeinflussung unterschiedlicher Zellen und zur Behandlung immunologischer, entzündlicher, neuronaler und anderer Erkrankungen
DE10348022A1 (de) * 2003-10-15 2005-05-25 Imtm Gmbh Neue Dipeptidylpeptidase IV-Inhibitoren zur funktionellen Beeinflussung unterschiedlicher Zellen und zur Behandlung immunologischer, entzündlicher, neuronaler und anderer Erkrankungen
DE10348023A1 (de) * 2003-10-15 2005-05-19 Imtm Gmbh Neue Alanyl-Aminopeptidasen-Inhibitoren zur funktionellen Beeinflussung unterschiedlicher Zellen und zur Behandlung immunologischer, entzündlicher, neuronaler und anderer Erkrankungen
WO2005049027A2 (en) 2003-11-03 2005-06-02 Probiodrug Ag Combinations useful for the treatment of neuronal disorders
US7576121B2 (en) 2003-11-12 2009-08-18 Phenomix Corporation Pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV
AU2007201757A1 (en) * 2003-11-12 2007-05-17 Phenomix Corporation Heterocyclic boronic acid compounds
KR101099206B1 (ko) 2004-02-05 2011-12-27 프로비오드룩 아게 신규한 글루타미닐 시클라제 저해제
KR101292707B1 (ko) * 2004-02-23 2013-08-02 트러스티즈 오브 터프츠 칼리지 디펩티딜펩티다아제 ⅳ의 억제제
EA013427B1 (ru) 2004-03-15 2010-04-30 Такеда Фармасьютикал Компани Лимитед Ингибиторы дипептидилпептидазы
JP2008501714A (ja) 2004-06-04 2008-01-24 武田薬品工業株式会社 ジペプチジルペプチダーゼインヒビター
WO2006019965A2 (en) 2004-07-16 2006-02-23 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
WO2006012395A2 (en) 2004-07-23 2006-02-02 Susan Marie Royalty Peptidase inhibitors
US20060063719A1 (en) * 2004-09-21 2006-03-23 Point Therapeutics, Inc. Methods for treating diabetes
TW200630337A (en) 2004-10-14 2006-09-01 Euro Celtique Sa Piperidinyl compounds and the use thereof
EP1828192B1 (en) 2004-12-21 2014-12-03 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
DOP2006000008A (es) 2005-01-10 2006-08-31 Arena Pharm Inc Terapia combinada para el tratamiento de la diabetes y afecciones relacionadas y para el tratamiento de afecciones que mejoran mediante un incremento de la concentración sanguínea de glp-1
CN101277949A (zh) 2005-04-22 2008-10-01 阿兰托斯制药控股公司 二肽基肽酶-ⅳ抑制剂
US7825139B2 (en) 2005-05-25 2010-11-02 Forest Laboratories Holdings Limited (BM) Compounds and methods for selective inhibition of dipeptidyl peptidase-IV
AU2006290205B2 (en) 2005-09-14 2012-12-13 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors for treating diabetes
CA2622642C (en) 2005-09-16 2013-12-31 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
WO2007078726A2 (en) 2005-12-16 2007-07-12 Merck & Co., Inc. Pharmaceutical compositions of combinations of dipeptidyl peptidase-4 inhibitors with metformin
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
US8247442B2 (en) 2006-03-29 2012-08-21 Purdue Pharma L.P. Benzenesulfonamide compounds and their use
PE20071221A1 (es) 2006-04-11 2007-12-14 Arena Pharm Inc Agonistas del receptor gpr119 en metodos para aumentar la masa osea y para tratar la osteoporosis y otras afecciones caracterizadas por masa osea baja, y la terapia combinada relacionada a estos agonistas
ES2354390T3 (es) 2006-04-11 2011-03-14 Arena Pharmaceuticals, Inc. Procedimientos de uso del receptor gpr119 para identificar compuestos útiles para aumentar la masa ósea en un individuo.
BRPI0709984A2 (pt) 2006-04-12 2011-08-02 Probiodrug Ag inibidores de enzima
TW200812963A (en) 2006-04-13 2008-03-16 Euro Celtique Sa Benzenesulfonamide compounds and the use thereof
TW200815353A (en) 2006-04-13 2008-04-01 Euro Celtique Sa Benzenesulfonamide compounds and their use
US8324383B2 (en) 2006-09-13 2012-12-04 Takeda Pharmaceutical Company Limited Methods of making polymorphs of benzoate salt of 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile
US8278345B2 (en) 2006-11-09 2012-10-02 Probiodrug Ag Inhibitors of glutaminyl cyclase
TW200838536A (en) 2006-11-29 2008-10-01 Takeda Pharmaceutical Polymorphs of succinate salt of 2-[6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethy]-4-fluor-benzonitrile and methods of use therefor
JP5523107B2 (ja) 2006-11-30 2014-06-18 プロビオドルグ エージー グルタミニルシクラーゼの新規阻害剤
US8093236B2 (en) 2007-03-13 2012-01-10 Takeda Pharmaceuticals Company Limited Weekly administration of dipeptidyl peptidase inhibitors
US20100105629A1 (en) * 2007-03-23 2010-04-29 Bachovchin William W N-Substituted Peptidomimetic Inhibitors of Dipeptidylpeptidase IV
US8399486B2 (en) 2007-04-09 2013-03-19 Purdue Pharma L.P. Benzenesulfonyl compounds and the use thereof
WO2008128985A1 (en) 2007-04-18 2008-10-30 Probiodrug Ag Thiourea derivatives as glutaminyl cyclase inhibitors
US8765736B2 (en) 2007-09-28 2014-07-01 Purdue Pharma L.P. Benzenesulfonamide compounds and the use thereof
EP2146210A1 (en) 2008-04-07 2010-01-20 Arena Pharmaceuticals, Inc. Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditions modulated by PYY
WO2010054326A2 (en) 2008-11-07 2010-05-14 The General Hospital Corporation C-terminal fragments of glucagon-like peptide-1 (glp-1)
AR077642A1 (es) 2009-07-09 2011-09-14 Arena Pharm Inc Moduladores del metabolismo y el tratamiento de trastornos relacionados con el mismo
MX2012002993A (es) 2009-09-11 2012-04-19 Probiodrug Ag Derivados heterociclicos como inhibidores de ciclasa glutaminilo.
JP6026284B2 (ja) 2010-03-03 2016-11-16 プロビオドルグ エージー グルタミニルシクラーゼの阻害剤
US8269019B2 (en) 2010-03-10 2012-09-18 Probiodrug Ag Inhibitors
MX2012011631A (es) 2010-04-06 2013-01-18 Arena Pharm Inc Moduladores del receptor gpr119 y el tratamiento de trastornos relacionados con el mismo.
WO2011131748A2 (en) 2010-04-21 2011-10-27 Probiodrug Ag Novel inhibitors
MX2013003184A (es) 2010-09-22 2013-06-07 Arena Pharm Inc Moduladores del receptor gpr119 y el tratamiento de transtornos relacionados con el mismo.
US9040481B2 (en) 2010-11-02 2015-05-26 The General Hospital Corporation Methods for treating steatotic disease
ES2570167T3 (es) 2011-03-16 2016-05-17 Probiodrug Ag Derivados de benzimidazol como inhibidores de glutaminil ciclasa
WO2012135570A1 (en) 2011-04-01 2012-10-04 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2012145361A1 (en) 2011-04-19 2012-10-26 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
US20140051714A1 (en) 2011-04-22 2014-02-20 Arena Pharmaceuticals, Inc. Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto
US20140038889A1 (en) 2011-04-22 2014-02-06 Arena Pharmaceuticals, Inc. Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto
WO2012170702A1 (en) 2011-06-08 2012-12-13 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
EP2729157B1 (en) 2011-07-06 2019-01-16 The General Hospital Corporation A pentapeptide derived from the c-terminus of glucagon-like peptide 1 (glp-1) for use in treatment
EP2753334B1 (en) 2011-08-30 2022-10-19 Trustees Of Tufts College Fap-activated proteasome inhibitors for treating solid tumors
WO2013055910A1 (en) 2011-10-12 2013-04-18 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2014074668A1 (en) 2012-11-08 2014-05-15 Arena Pharmaceuticals, Inc. Modulators of gpr119 and the treatment of disorders related thereto
CN105399700A (zh) * 2013-01-06 2016-03-16 天津市汉康医药生物技术有限公司 噻唑烷衍生物、其制备方法和用途
WO2015117136A1 (en) * 2014-02-03 2015-08-06 Ohio State Innovation Foundation Boronic acid esters and pharmaceutical formulations thereof
BR112016023723B1 (pt) 2014-04-24 2023-01-17 Hyundai Motor Company Sistema de exibição
HK1249847A1 (zh) 2015-03-09 2018-11-16 Intekrin Therapeutics, Inc. 用於治疗非酒精性脂肪肝疾病和/或脂肪营养不良的方法
WO2016144654A1 (en) 2015-03-09 2016-09-15 Washington University Inhibitors of growth factor activation enzymes
MX388602B (es) 2016-04-04 2025-03-20 Res Triangle Inst Agonistas de receptor de neuropéptido s (npsr).
CN109906082A (zh) * 2016-09-07 2019-06-18 塔夫茨大学信托人 使用免疫dash抑制剂和pge2拮抗剂的组合治疗
KR20200036808A (ko) 2017-04-03 2020-04-07 코히러스 바이오사이언시스, 인크. 진행성 핵상 마비 치료를 위한 PPARγ 작용제
US11559537B2 (en) 2017-04-07 2023-01-24 Trustees Of Tufts College Combination therapies using caspase-1 dependent anticancer agents and PGE2 antagonists
PL3461819T3 (pl) 2017-09-29 2020-11-30 Probiodrug Ag Inhibitory cyklazy glutaminylowej
CN108309964B (zh) * 2018-04-04 2020-06-30 军事科学院军事医学研究院环境医学与作业医学研究所 二甲双胍在制备噪声性听力损失防治产品中的应用
CN117379409B (zh) * 2023-11-29 2025-10-31 郑州大学 油酰乙醇胺的新用途

Family Cites Families (55)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IT1164225B (it) 1983-05-13 1987-04-08 Anic Spa Analoghi retro-invertiti del pentapeptide potenziante la bradichina bpp5a e metodi per la loro preparazione
US4499082A (en) * 1983-12-05 1985-02-12 E. I. Du Pont De Nemours And Company α-Aminoboronic acid peptides
US4698327A (en) * 1985-04-25 1987-10-06 Eli Lilly And Company Novel glycopeptide derivatives
US4935493A (en) 1987-10-06 1990-06-19 E. I. Du Pont De Nemours And Company Protease inhibitors
US4963655A (en) * 1988-05-27 1990-10-16 Mayo Foundation For Medical Education And Research Boron analogs of amino acid/peptide protease inhibitors
IT1227907B (it) 1988-12-23 1991-05-14 Eniricerche S P A Milano Sclav Procedimento per la sintesi di peptidi retro-inversi e nuovi intermediin tale procedimento
US5462928A (en) 1990-04-14 1995-10-31 New England Medical Center Hospitals, Inc. Inhibitors of dipeptidyl-aminopeptidase type IV
ATE140449T1 (de) * 1991-10-07 1996-08-15 Hoechst Ag Verfahren zur diastereoselektiven reduktiven pinakol-kupplung von homochiralen alpha- aminoaldehyden
US6825169B1 (en) 1991-10-22 2004-11-30 Trustees Of Tufts College Inhibitors of dipeptidyl-aminopeptidase type IV
DK0610317T3 (da) * 1991-10-22 2001-02-19 New England Medical Center Inc Inhibitorer af dipeptidyl-aminopeptidase type IV
DK36392D0 (da) 1992-03-19 1992-03-19 Novo Nordisk As Anvendelse af kemisk forbindelse
WO1994028014A2 (en) * 1993-05-28 1994-12-08 Chiron Corporation Peptide inhibitors of urokinase receptor activity
FR2707085B1 (fr) 1993-06-30 1995-08-18 Adir Nouveaux dérivés d'alpha amino acides, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent.
WO1995011689A1 (en) * 1993-10-29 1995-05-04 Trustees Of Tufts College Use of inhibitors of dipeptidyl-aminopeptidase to block entry of hiv into cells
IL111785A0 (en) 1993-12-03 1995-01-24 Ferring Bv Dp-iv inhibitors and pharmaceutical compositions containing them
US5580979A (en) 1994-03-15 1996-12-03 Trustees Of Tufts University Phosphotyrosine peptidomimetics for inhibiting SH2 domain interactions
US5543396A (en) * 1994-04-28 1996-08-06 Georgia Tech Research Corp. Proline phosphonate derivatives
AU2790895A (en) * 1994-06-10 1996-01-05 Universitaire Instelling Antwerpen Purification of serine protease and synthetic inhibitors thereof
US5574017A (en) * 1994-07-05 1996-11-12 Gutheil; William G. Antibacterial agents
US5614649A (en) 1994-11-14 1997-03-25 Cephalon, Inc. Multicatalytic protease inhibitors
US5834428A (en) 1995-04-14 1998-11-10 1149336 Ontario Inc. Glucagon-like peptide-2 and its therapeutic use
FI974437A0 (fi) 1995-06-06 1997-12-05 Pfizer Substituoituja N-(indoli-2-karbonyyli)amideja ja johdannaisia glykogeenifosforylaasi-inhibiittoreina
US5721214A (en) * 1995-06-07 1998-02-24 Cor Therapeutics, Inc. Inhibitors of factor Xa
DE122010000020I1 (de) 1996-04-25 2010-07-08 Prosidion Ltd Verfahren zur Senkung des Blutglukosespiegels in Säugern
US5965532A (en) 1996-06-28 1999-10-12 Trustees Of Tufts College Multivalent compounds for crosslinking receptors and uses thereof
US5783556A (en) 1996-08-13 1998-07-21 Genentech, Inc. Formulated insulin-containing composition
US6011155A (en) 1996-11-07 2000-01-04 Novartis Ag N-(substituted glycyl)-2-cyanopyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
TW492957B (en) 1996-11-07 2002-07-01 Novartis Ag N-substituted 2-cyanopyrrolidnes
US5952301A (en) 1996-12-10 1999-09-14 1149336 Ontario Inc. Compositions and methods for enhancing intestinal function
US6100234A (en) * 1997-05-07 2000-08-08 Tufts University Treatment of HIV
CA2304206A1 (en) 1997-09-29 1999-04-08 Point Therapeutics, Inc. Stimulation of hematopoietic cells in vitro
EP2823812A1 (en) * 1998-02-02 2015-01-14 Trustees Of Tufts College Dipeptidylpeptidase IV inhibitors for use in the treatment of Type II diabetes
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
DE19828114A1 (de) * 1998-06-24 2000-01-27 Probiodrug Ges Fuer Arzneim Produgs instabiler Inhibitoren der Dipeptidyl Peptidase IV
CA2339537A1 (en) 1998-08-21 2000-03-02 Barbara Wallner Regulation of substrate activity
US6979697B1 (en) 1998-08-21 2005-12-27 Point Therapeutics, Inc. Regulation of substrate activity
EA200100972A1 (ru) * 1999-03-15 2002-02-28 Аксис Фармасьютикалз, Инк. Новые соединения и композиции как ингибиторы протеаз
ES2219333T3 (es) * 1999-04-09 2004-12-01 Trustees Of Tufts College Metodos y reactivos para determinar la especifidad de sustratos enzimaticos y usos relacionados.
US6890904B1 (en) 1999-05-25 2005-05-10 Point Therapeutics, Inc. Anti-tumor agents
CA2373643A1 (en) * 1999-05-25 2000-11-30 Point Therapeutics, Inc. Anti-tumor comprising boroproline compounds
DE19940130A1 (de) 1999-08-24 2001-03-01 Probiodrug Ges Fuer Arzneim Neue Effektoren der Dipeptidyl Peptidase IV zur topischen Anwendung
JP4748908B2 (ja) * 1999-09-10 2011-08-17 ザ・ユニバーシティ・オブ・シドニー ジペプチジルペプチダーゼ
US6649593B1 (en) 1999-10-13 2003-11-18 Tularik Inc. Modulators of SREBP processing
AU1916401A (en) 1999-11-12 2001-06-06 Guilford Pharmaceuticals Inc. Dipeptidyl peptidase iv inhibitors and methods of making and using dipeptidyl peptidase iv inhibitors
GB0010188D0 (en) 2000-04-26 2000-06-14 Ferring Bv Inhibitors of dipeptidyl peptidase IV
DE10150203A1 (de) * 2001-10-12 2003-04-17 Probiodrug Ag Peptidylketone als Inhibitoren der DPIV
US6634939B2 (en) * 2001-08-31 2003-10-21 Thomas W. Johnson Ventilation system and method
EP1487471A4 (en) 2001-11-26 2010-03-10 Tufts College METHOD FOR TREATING AUTOIMMUNE DISEASES AND ASSOCIATED REAGENTS
EP2316470A3 (en) 2001-11-26 2011-08-24 Trustees Of Tufts College Peptidomimetic inhibitors of post-proline cleaving enzymes
CA2484551A1 (en) * 2002-04-30 2003-11-13 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
CN1822851B (zh) 2003-05-15 2011-04-13 塔夫茨大学信托人 肽和多肽药物的稳定类似物
KR101292707B1 (ko) 2004-02-23 2013-08-02 트러스티즈 오브 터프츠 칼리지 디펩티딜펩티다아제 ⅳ의 억제제
US20060063719A1 (en) 2004-09-21 2006-03-23 Point Therapeutics, Inc. Methods for treating diabetes

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7674913B2 (en) 2003-11-12 2010-03-09 Phenomix Corporation Heterocyclic boronic acid compounds
US7767828B2 (en) 2003-11-12 2010-08-03 Phenomix Corporation Methyl and ethyl substituted pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV
US7884217B2 (en) 2003-11-12 2011-02-08 Phenomix Corporation Pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV
US7906658B2 (en) 2003-11-12 2011-03-15 Phenomix Corporation Pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV
US8415295B2 (en) 2003-11-12 2013-04-09 Phenomix Corporation Heterocyclic boronic acid compounds

Also Published As

Publication number Publication date
US20170333461A1 (en) 2017-11-23
EP2316470A3 (en) 2011-08-24
WO2003045977A2 (en) 2003-06-05
WO2003045977A3 (en) 2004-05-13
US20160158260A1 (en) 2016-06-09
JP2011121989A (ja) 2011-06-23
JP2014139191A (ja) 2014-07-31
AU2002357767B2 (en) 2008-12-04
AU2002357767C1 (en) 2009-03-19
CA2837936A1 (en) 2003-06-05
EP2316470A2 (en) 2011-05-04
AU2002357767A1 (en) 2003-06-10
EP1469873A2 (en) 2004-10-27
US7727964B2 (en) 2010-06-01
JP4771661B2 (ja) 2011-09-14
EP1469873A4 (en) 2007-10-03
JP2005514377A (ja) 2005-05-19
US20110082108A1 (en) 2011-04-07
US9757400B2 (en) 2017-09-12
US20050070482A1 (en) 2005-03-31

Similar Documents

Publication Publication Date Title
US9757400B2 (en) Peptidomimetic inhibitors of post-proline cleaving enzymes
AU2005216970B2 (en) Inhibitors of dipeptidylpeptidase IV for regulating glucose metabolism
AU2005217642B2 (en) Lactams as conformationally constrained peptidomimetic inhibitors
US6803357B1 (en) Method of regulating glucose metabolism, and reagents related thereto
JP2005514377A5 (enExample)
AU2011203039B2 (en) Inhibitors of dipeptidylpeptidase IV for regulating glucose metabolism
AU2007202745A1 (en) Method of regulating glucose metabolism, and reagents related thereto
AU2016222497A1 (en) Method of regulating glucose metabolism, and reagents related thereto

Legal Events

Date Code Title Description
EEER Examination request
FZDE Dead

Effective date: 20150122