BR9814499A - Peptìdeo amida opióide sintético ou um sal farmaceuticamente aceitável do mesmo, composição farmacêutica, e, processo para tratamento compreendendo a administração de uma quantidade da mesma - Google Patents

Peptìdeo amida opióide sintético ou um sal farmaceuticamente aceitável do mesmo, composição farmacêutica, e, processo para tratamento compreendendo a administração de uma quantidade da mesma

Info

Publication number
BR9814499A
BR9814499A BR9814499-5A BR9814499A BR9814499A BR 9814499 A BR9814499 A BR 9814499A BR 9814499 A BR9814499 A BR 9814499A BR 9814499 A BR9814499 A BR 9814499A
Authority
BR
Brazil
Prior art keywords
phe
nle
arg
morpholinyl
pharmaceutically acceptable
Prior art date
Application number
BR9814499-5A
Other languages
English (en)
Other versions
BR9814499B1 (pt
Inventor
Jean Louis Junien
Pierre J M Riviere
Claudio D Schteingart
Javier Sueiras Diaz
Jerzy A Trojnar
Todd W Vanderah
Original Assignee
Ferring Bv
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 Ferring Bv filed Critical Ferring Bv
Publication of BR9814499A publication Critical patent/BR9814499A/pt
Publication of BR9814499B1 publication Critical patent/BR9814499B1/pt

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    • 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
    • C07K5/1027Tetrapeptides containing heteroatoms different from O, S, or N
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • 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
    • 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
    • C07K5/1024Tetrapeptides with the first amino acid being heterocyclic
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Biochemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Molecular Biology (AREA)
  • Veterinary Medicine (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Nutrition Science (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

"PEPTìDEO AMIDA OPIóIDE SINTéTICO OU UM SAL FARMACEUTICAMENTE ACEITáVEL DO MESMO, COMPOSIçãO FARMACêUTICA, E, PROCESSO PARA TRATAMENTO COMPREENDENDO A ADMINISTRAçãO DE UMA QUANTIDADE DA MESMA". Peptídeos que demonstram alta seletividade para o receptor opióide kappa (KOR) e longa duração de ação periférica sem entrada significante no cerébro são criados que são seq³ências de quatro resíduos de aminoácidos D-isómero tendo um C-término que é uma amida mono- ou disubstituída. Os compostos representativos, que tem uma afinidade para o KOR de pelo menos 1000 vezes sua afinidade para o receptor opióide mu e um ED~ 50~ não maior que cerca de 0,5 mg/kg, incluem H-D-Phe-D-Phe-D-Nle-D-Arg-NHEt, H-D-Phe-D-Phe-D-Nle-D-Arg-morfolinila, H-D-Phe-D-Phe-D-Nle-D-Arg-Nh-4-picolila, H-D-Phe-D-Phe-D-Nle-D-Arg-NHPr,H-D-Phe-D-Phe-D-Nle-D-Arg-tio morfolinila, H-D-Phe-D-Phe-D-Nle-D-Arg-Net~ 2~, H-D-Phe-D-Phe-D-Nle-D-Arg-NHMe, H-D-Phe-D-Phe-D-Nle-D-Orn-morfolinila, H-D-4Fpa-D-Phe-D-Nle-D-Arg-NH-4-picolila, H-D-Phe-D-Phe-D-Nle-D-Arg-NH-ciclopropila, H-D-Ala(2Thi)D-3,4-Cpa-D-Leu-D-Arg-morfolinila, H-D-Phe-D-Phe-D-Nle-D-Gmf-morfolinila, H-D-Phe-D-Phe-D-Leu-D-Orn-NH (Aeb), H-D-Phe-D-Phe-D-Leu-D-Lys-morfolinila, H-D-Phe-D-Phe-D-Nle-D-Arg-piperazinila, e H-D-Phe-D-Phe-D-Nle-D-Arg-NH(Hoh).
BRPI9814499-5A 1997-12-23 1998-12-22 Peptídeo amida opióide sintético ou um sal farmaceuticamente aceitavel do mesmo, e, composição farmacêutica BR9814499B1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US08/997208 1997-12-23
US08/997,208 US5965701A (en) 1997-12-23 1997-12-23 Kappa receptor opioid peptides
PCT/US1998/027282 WO1999032510A1 (en) 1997-12-23 1998-12-22 Kappa receptor opioid peptides

Publications (2)

Publication Number Publication Date
BR9814499A true BR9814499A (pt) 2000-10-10
BR9814499B1 BR9814499B1 (pt) 2014-10-21

Family

ID=25543752

Family Applications (2)

Application Number Title Priority Date Filing Date
BRPI9814499A BRPI9814499B8 (pt) 1997-12-23 1998-12-22 Peptídeo amida opióide sintético ou um sal farmaceuticamente aceitavel do mesmo, e, composição farmacêutica
BRPI9814499-5A BR9814499B1 (pt) 1997-12-23 1998-12-22 Peptídeo amida opióide sintético ou um sal farmaceuticamente aceitavel do mesmo, e, composição farmacêutica

Family Applications Before (1)

Application Number Title Priority Date Filing Date
BRPI9814499A BRPI9814499B8 (pt) 1997-12-23 1998-12-22 Peptídeo amida opióide sintético ou um sal farmaceuticamente aceitavel do mesmo, e, composição farmacêutica

Country Status (33)

Country Link
US (1) US5965701A (pt)
EP (1) EP1042359B1 (pt)
JP (1) JP4275852B2 (pt)
KR (1) KR100629548B1 (pt)
CN (1) CN1154655C (pt)
AR (1) AR014167A1 (pt)
AT (1) ATE301670T1 (pt)
AU (1) AU747806B2 (pt)
BR (2) BRPI9814499B8 (pt)
CA (1) CA2315878C (pt)
CR (1) CR5936A (pt)
CZ (1) CZ297281B6 (pt)
DE (1) DE69831176T2 (pt)
DK (1) DK1042359T3 (pt)
EE (1) EE04440B1 (pt)
ES (1) ES2247735T3 (pt)
HK (1) HK1029349A1 (pt)
HR (1) HRP20000415B1 (pt)
HU (1) HU227640B1 (pt)
IL (3) IL136742A0 (pt)
MY (1) MY117542A (pt)
NO (1) NO327080B1 (pt)
NZ (1) NZ505183A (pt)
PL (1) PL195842B1 (pt)
PT (1) PT1042359E (pt)
RU (1) RU2217437C2 (pt)
SK (1) SK286135B6 (pt)
TR (1) TR200001985T2 (pt)
TW (1) TW580502B (pt)
UA (1) UA68366C2 (pt)
UY (1) UY25327A1 (pt)
WO (1) WO1999032510A1 (pt)
ZA (1) ZA9811801B (pt)

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US7713937B2 (en) * 2006-11-10 2010-05-11 Cara Therapeutics, Inc. Synthetic peptide amides and dimeric forms thereof
US8906859B2 (en) * 2006-11-10 2014-12-09 Cera Therapeutics, Inc. Uses of kappa opioid synthetic peptide amides
WO2008077194A1 (en) * 2006-12-22 2008-07-03 Xenome Ltd Receptor agonists
US8485180B2 (en) 2008-06-13 2013-07-16 Mannkind Corporation Dry powder drug delivery system
AR072114A1 (es) 2008-06-13 2010-08-04 Mannkind Corp Un inhalador de polvo seco y sistema para suministro de farmacos
BRPI0914308B8 (pt) 2008-06-20 2021-06-22 Mannkind Corp sistema de inalação
TWI614024B (zh) 2008-08-11 2018-02-11 曼凱公司 超快起作用胰島素之用途
US8314106B2 (en) 2008-12-29 2012-11-20 Mannkind Corporation Substituted diketopiperazine analogs for use as drug delivery agents
CA2754595C (en) 2009-03-11 2017-06-27 Mannkind Corporation Apparatus, system and method for measuring resistance of an inhaler
KR101875969B1 (ko) 2009-06-12 2018-07-06 맨카인드 코포레이션 한정된 비표면적을 갖는 디케토피페라진 마이크로입자
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JP6018640B2 (ja) 2011-10-24 2016-11-02 マンカインド コーポレイション 疼痛を緩和するのに有効な鎮痛組成物並びに当該組成物を含む乾燥粉末及び乾燥粉末薬剤輸送システム
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Also Published As

Publication number Publication date
IL136742A (en) 2006-12-31
HRP20000415A2 (en) 2000-12-31
HUP0100626A3 (en) 2001-12-28
BR9814499B1 (pt) 2014-10-21
CA2315878A1 (en) 1999-07-01
CN1283201A (zh) 2001-02-07
PT1042359E (pt) 2005-11-30
NO20003245D0 (no) 2000-06-21
NO327080B1 (no) 2009-04-20
DK1042359T3 (da) 2005-11-28
ATE301670T1 (de) 2005-08-15
IL178471A0 (en) 2007-02-11
PL195842B1 (pl) 2007-10-31
PL341308A1 (en) 2001-04-09
CR5936A (es) 2006-08-18
TR200001985T2 (tr) 2000-11-21
SK286135B6 (sk) 2008-04-07
UA68366C2 (en) 2004-08-16
KR100629548B1 (ko) 2006-09-27
UY25327A1 (es) 2000-12-29
MY117542A (en) 2004-07-31
WO1999032510A9 (en) 1999-09-23
ES2247735T3 (es) 2006-03-01
HU227640B1 (en) 2011-10-28
CA2315878C (en) 2010-11-16
SK9602000A3 (en) 2001-01-18
BRPI9814499B8 (pt) 2021-11-09
BRPI9814499B1 (pt) 2014-10-21
HRP20000415B1 (en) 2004-06-30
CZ20002382A3 (cs) 2000-12-13
RU2217437C2 (ru) 2003-11-27
JP4275852B2 (ja) 2009-06-10
US5965701A (en) 1999-10-12
JP2001526295A (ja) 2001-12-18
ZA9811801B (en) 1999-06-22
TW580502B (en) 2004-03-21
EP1042359B1 (en) 2005-08-10
KR20010033450A (ko) 2001-04-25
AR014167A1 (es) 2001-02-07
DE69831176T2 (de) 2006-04-20
BRPI9814499A (pt) 2000-10-10
DE69831176D1 (de) 2005-09-15
EP1042359A1 (en) 2000-10-11
EE200000370A (et) 2001-10-15
AU747806B2 (en) 2002-05-23
WO1999032510A1 (en) 1999-07-01
IL136742A0 (en) 2001-06-14
CN1154655C (zh) 2004-06-23
NO20003245L (no) 2000-08-23
AU1940299A (en) 1999-07-12
CZ297281B6 (cs) 2006-10-11
HUP0100626A2 (hu) 2001-08-28
HK1029349A1 (en) 2001-03-30
NZ505183A (en) 2001-09-28
EE04440B1 (et) 2005-02-15

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