BRPI0507971A - composto, composição farmacêutica, uso de um composto,método para inibir a atividade proteolìtica de uma enzima de clivagem pós-prolina e remédio empacotado - Google Patents

composto, composição farmacêutica, uso de um composto,método para inibir a atividade proteolìtica de uma enzima de clivagem pós-prolina e remédio empacotado

Info

Publication number
BRPI0507971A
BRPI0507971A BRPI0507971-3A BRPI0507971A BRPI0507971A BR PI0507971 A BRPI0507971 A BR PI0507971A BR PI0507971 A BRPI0507971 A BR PI0507971A BR PI0507971 A BRPI0507971 A BR PI0507971A
Authority
BR
Brazil
Prior art keywords
compound
inhibitors
pharmaceutical composition
proteolytic activity
inhibit
Prior art date
Application number
BRPI0507971-3A
Other languages
English (en)
Inventor
William W Bachovchin
Hung-Sen Lai
Wengen Wu
Original Assignee
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 Tufts College filed Critical Tufts College
Publication of BRPI0507971A publication Critical patent/BRPI0507971A/pt

Links

Classifications

    • 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
    • C07D207/18—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 one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—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 one double bond between ring members or between a ring member and a non-ring member 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/273—2-Pyrrolidones 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 other ring carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10—Spiro-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Diabetes (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyrrole Compounds (AREA)

Abstract

COMPOSTO, COMPOSIçãO FARMACêUTICA, USO DE UM COMPOSTO, MéTODO PARA INIBIR A ATIVIDADE PROTEOLìTICA DE UMA EMZIMA DE CLIVAGEM PóS-PROLINA E REMéDIO EMPACOTADO A presente invenção se refere a inibidores de emzima de clivagem pós-prolina, tais como inibidores de dipeptidilpeptidase iv, assim como suas composições farmacêuticas, e métodos para usar tais inibidores. Em particular, os inibidores da presente invenção incorporam um anel de lactama na estrutura principal dos inibidores. Os compostos da presente invenção podem ter um melhor índice terapêutico, devido em parte à toxicidade reduzida e/ou especificidade melhorada para a protease alvo.
BRPI0507971-3A 2004-02-23 2005-02-23 composto, composição farmacêutica, uso de um composto,método para inibir a atividade proteolìtica de uma enzima de clivagem pós-prolina e remédio empacotado BRPI0507971A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US54722604P 2004-02-23 2004-02-23
PCT/US2005/006127 WO2005082849A1 (en) 2004-02-23 2005-02-23 Lactams as conformationally constrained peptidomimetic inhibitors

Publications (1)

Publication Number Publication Date
BRPI0507971A true BRPI0507971A (pt) 2007-07-24

Family

ID=34910873

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0507971-3A BRPI0507971A (pt) 2004-02-23 2005-02-23 composto, composição farmacêutica, uso de um composto,método para inibir a atividade proteolìtica de uma enzima de clivagem pós-prolina e remédio empacotado

Country Status (11)

Country Link
US (1) US20090209491A1 (pt)
EP (1) EP1732885A1 (pt)
JP (1) JP2007526255A (pt)
CN (1) CN101090885A (pt)
AU (1) AU2005217642B2 (pt)
BR (1) BRPI0507971A (pt)
CA (1) CA2555961A1 (pt)
IL (1) IL177643A (pt)
MX (1) MXPA06009588A (pt)
NO (1) NO20064306L (pt)
WO (1) WO2005082849A1 (pt)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
TWI357902B (en) * 2005-04-01 2012-02-11 Lg Life Science Ltd Dipeptidyl peptidase-iv inhibiting compounds, meth
CA2622579C (en) * 2005-09-20 2013-12-31 Novartis Ag Use of a dpp-iv inhibitor to reduce hypoglycemic events
CN101365432B (zh) * 2005-12-16 2011-06-22 默沙东公司 二肽基肽酶-4抑制剂与二甲双胍的组合的药物组合物
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
EP2108960A1 (en) 2008-04-07 2009-10-14 Arena Pharmaceuticals, Inc. Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditons modulated by PYY
CA2793683A1 (en) * 2009-03-20 2010-09-23 Centre Hospitalier Universitaire Sainte-Justine Peptidomimetics for modulating interleukin-1 receptor
AR077642A1 (es) 2009-07-09 2011-09-14 Arena Pharm Inc Moduladores del metabolismo y el tratamiento de trastornos relacionados con el mismo
AU2011237775A1 (en) 2010-04-06 2012-11-22 Arena Pharmaceuticals, Inc. Modulators of the GPR119 receptor and the treatment of disorders related thereto
AU2011256455A1 (en) 2010-05-17 2013-01-10 Array Biopharma Inc. Piperidinyl-substituted lactams as GPR119 modulators
PH12013500547A1 (en) 2010-09-22 2013-06-10 Arena Pharm Inc Modulators of the gpr119 receptor and the treatment of disorders related thereto
US20140018371A1 (en) 2011-04-01 2014-01-16 Arena Pharmaceuticals, Inc. Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto
US20140066369A1 (en) 2011-04-19 2014-03-06 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
WO2012145604A1 (en) 2011-04-22 2012-10-26 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
WO2013055910A1 (en) 2011-10-12 2013-04-18 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
US20140256756A1 (en) * 2011-11-03 2014-09-11 Array Biopharma Inc. Piperidinyl-substituted lactams as gpr119 modulators
WO2014074668A1 (en) 2012-11-08 2014-05-15 Arena Pharmaceuticals, Inc. Modulators of gpr119 and the treatment of disorders related thereto
EA201791982A1 (ru) 2015-03-09 2020-02-17 Интекрин Терапьютикс, Инк. Способы лечения неалкогольной жировой болезни печени и/или липодистрофии
AU2018249822A1 (en) 2017-04-03 2019-10-31 Coherus Biosciences Inc. PPArgamma agonist for treatment of progressive supranuclear palsy
CN112986065B (zh) * 2021-02-08 2021-08-31 杭州同创医学检验实验室有限公司 一种用于血细胞分析仪的全血质控品及其制备方法

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IT1247698B (it) * 1990-06-21 1994-12-30 Sigma Tau Ind Farmaceuti 1-alchil-3-(acilammino)-e-caprolattami quali attivatori dei processi di apprendimento e della memoria e composizioni farmaceutiche comprendenti tali composti
WO1998054208A1 (en) * 1997-05-28 1998-12-03 Cadus Pharmaceutical Corporation CONFORMATIONALLY CONSTRAINED PEPTIDOMIMETICS AS β-TURN TEMPLATES AND MODULATORS OF SH3 DOMAINS
DE19841895A1 (de) * 1998-09-11 2000-03-23 Degussa Neues Verfahren zur Herstellung von 3-Amino-2-oxo-pyrrolidinen, neue Zwischenprodukte und deren Verwendung
US6344450B1 (en) * 1999-02-09 2002-02-05 Bristol-Myers Squibb Company Lactam compounds and their use as inhibitors of serine proteases and method
US7122627B2 (en) * 1999-07-26 2006-10-17 Bristol-Myers Squibb Company Lactam inhibitors of Hepatitis C virus NS3 protease
US6541467B1 (en) * 2000-04-14 2003-04-01 Corvas International, Inc. Thrombin inhibitors having a lactam at P3
US6511973B2 (en) * 2000-08-02 2003-01-28 Bristol-Myers Squibb Co. Lactam inhibitors of FXa and method
WO2002083130A1 (en) * 2001-04-16 2002-10-24 Bristol-Myers Squibb Company Enantiomers of n-[[2'-[[(4,5-dimethyl-3-isoxazolyl) amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]-2-yl]methyl]-n,3,3-trimethylbutanamide
GB0114004D0 (en) * 2001-06-08 2001-08-01 Glaxo Group Ltd Chemical compounds
DE60221983T2 (de) * 2001-06-27 2008-05-15 Smithkline Beecham Corp. Fluorpyrrolidine als dipeptidyl-peptidase inhibitoren
JP4266092B2 (ja) * 2001-10-09 2009-05-20 第一三共株式会社 ジアミン誘導体
GB0130285D0 (en) * 2001-12-19 2002-02-06 Astrazeneca Ab Chemical process
WO2003080633A1 (fr) * 2002-03-25 2003-10-02 Nippon Kayaku Kabushiki Kaisha Nouveau derive d'$g(a)-amino-n-(diaminophosphinyl)lactame
US7057046B2 (en) * 2002-05-20 2006-06-06 Bristol-Myers Squibb Company Lactam glycogen phosphorylase inhibitors and method of use
WO2004022536A1 (en) * 2002-09-04 2004-03-18 Glenmark Pharmaceuticals Limited New heterocyclic amide compounds useful for the treatment of inflammatory and allergic disorders: process for their preparation and pharmaceutical compositions containing them
US7112702B2 (en) * 2002-12-12 2006-09-26 General Electric Company Process for the synthesis of bisphenol
JO2355B1 (en) * 2003-04-15 2006-12-12 ميرك شارب اند دوم كوربوريشن Hereditary calcitonin polypeptide receptor antagonists

Also Published As

Publication number Publication date
JP2007526255A (ja) 2007-09-13
US20090209491A1 (en) 2009-08-20
MXPA06009588A (es) 2007-03-30
IL177643A0 (en) 2006-12-31
WO2005082849A8 (en) 2005-11-10
IL177643A (en) 2011-11-30
AU2005217642B2 (en) 2012-04-12
CN101090885A (zh) 2007-12-19
EP1732885A1 (en) 2006-12-20
AU2005217642A1 (en) 2005-09-09
CA2555961A1 (en) 2005-09-09
NO20064306L (no) 2006-11-17
WO2005082849A1 (en) 2005-09-09

Similar Documents

Publication Publication Date Title
BRPI0507971A (pt) composto, composição farmacêutica, uso de um composto,método para inibir a atividade proteolìtica de uma enzima de clivagem pós-prolina e remédio empacotado
BRPI0507972A (pt) composto ,composição farmacêutica , uso de um composto, método para inibição da atividade proteolìtica de uma enzima de clivagem pós prolina e composição farmacêutica embalada
BRPI0508085A (pt) compostos de enxofre como inibidores da ns3 serina protease do vìrus da hepatite c
BR0308081A (pt) Inibidores de histona desacetilase
BRPI0509172A (pt) pelo menos uma entidade quìmica, composição farmacêutica, métodos para tratar um paciente, para inibir pelo menos uma enzima que utiliza atp, e para tratar pelo menos uma doença, uso de pelo menos uma entidade quìmica, e, método para a fabricação de um medicamento
BR0009167A (pt) Inibidores de enzima impdh
PT966465E (pt) Inibidores do enzima imfdh
MX2007004783A (es) Inhibidores de la proteasa del virus de la hepatitis c, y composiciones y tratamientos que los usan.
EP2316470A3 (en) Peptidomimetic inhibitors of post-proline cleaving enzymes
DE60217114D1 (de) Verbrückte bizyklische serinproteaseinhibitoren
BRPI0508217A (pt) cetamidas com p4's cìclico como inibidores de ns3 serina protease de vìrus de hepatite c
WO2005007681A3 (en) Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
BRPI0414814A (pt) inibidores macrocìclicos de protease de serina ns3 de vìrus de hepatite c
BRPI0416902A (pt) inibidores de ns3/ns4a serina protease do vìrus da hepatite c
ECSP034493A (es) Inhibidores de proteasa peptidomimeticos
ATE469136T1 (de) Inhibitoren von 11-beta- hydroxysteroiddehydrogenase typ 1
NO20052690D0 (no) Fenylalaninderivater som dipeptidylpeptidaseinhibitorer for behandlingen eller profylaksen av sukkersyke.
BR0112666A (pt) Peptìdeos como inibidores de ns3-serina protease de vìrus da hepatite c
BRPI0410727A (pt) composto, composição farmacêutica, e, uso de um composto
MX2009009176A (es) Inhibidores de serina-proteasas.
BRPI0516825A (pt) inibição da protease ns3-ns4a do vìrus da hepatite c (vhc)
HU0302788D0 (en) New compounds
BRPI0519148A2 (pt) inibidores de homodimerizaÇço de myd88
Martina et al. Screening of electrophilic compounds yields an aziridinyl peptide as new active-site directed SARS-CoV main protease inhibitor
BR0306928A (pt) Composições farmacêuticas estáveis compreendendo inibidores de enzimas conversoras de angiotensina (ace)

Legal Events

Date Code Title Description
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 9A ANUIDADE.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2260 DE 29/04/2014.