BR0101674A - Antagonistas e agonistas de somatostatina queatuam no receptor sst subtipo 2 - Google Patents

Antagonistas e agonistas de somatostatina queatuam no receptor sst subtipo 2

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Publication number
BR0101674A
BR0101674A BR0101674-1A BR0101674A BR0101674A BR 0101674 A BR0101674 A BR 0101674A BR 0101674 A BR0101674 A BR 0101674A BR 0101674 A BR0101674 A BR 0101674A
Authority
BR
Brazil
Prior art keywords
heteroaryl
aryl
receptor
carbonyl
sst
Prior art date
Application number
BR0101674-1A
Other languages
English (en)
Inventor
Bridget Mccarthy Cole
Bruce Allan Hay
Anthony Paul Ricketts
Original Assignee
Pfizer Prod Inc
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 Pfizer Prod Inc filed Critical Pfizer Prod Inc
Publication of BR0101674A publication Critical patent/BR0101674A/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
    • C07K5/08Tripeptides
    • 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
    • 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
    • A61P17/00Drugs for dermatological disorders
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/04Immunostimulants
    • 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
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/02Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/06Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/06Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
    • A61P5/08Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH for decreasing, blocking or antagonising the activity of the anterior pituitary hormones
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/021Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)n-C(=0)-, n being 5 or 6; for n > 6, classification in C07K5/06 - C07K5/10, according to the moiety having normal peptide bonds
    • 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
    • C07K5/06Dipeptides
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
    • C07K5/06156Dipeptides with the first amino acid being heterocyclic and Trp-amino acid; Derivatives thereof
    • 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
    • C07K5/06191Dipeptides containing heteroatoms different from O, S, or N
    • 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)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Immunology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Dermatology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

Patente de Invenção: "ANTAGONISTAS E AGONISTAS DESOMATOSTATINA QUE ATUAM NO RECEPTOR SST SUBTIPO2". Compostos de acordo com a fórmula (I) A-G-Z-W e seus saisfarmaceuticamente aceitáveis, solvatos ou hidratos; em que, A éarila (C~ 6~-C~ 10~), aril(C~ 6~-C~ 10~)-SO~ 2~, aril (C~ 6~-C~10~)-CH~ 2~, aril (C~ 6~-C~ 10~)carbonila, heteroarila (C~ 1~-C~9~), heteroaril(C~ 1~-C~ 9~)-SO~ 2-~, heteroaril(C~ 1~-C~9~)-CH~ 2-~ ou heteroaril(C~ 1~-C~ 9~)-carbonila; G éselecionado do grupo consistindo por: onde B é arila (C~ 6~-C~10~) ou heteroarila (C~ 1~-C~ 9~), e X é CH~ 2~, SO~ 2~ oucarbonila; onde X é CH~ 2~, SO~ 2~ ou carbonila; e R^ 1^ e R^1<39>^ são cada um independentemente selecionados de entreH, CN, alquila (C~ 1~-C~ 8-~) e fenila(CH~ 2~)-, em que osreferidos grupos alquila e fenila são facultativamente substituídas;e onde Z e W são conforme definidos na presente Descrição; ecomposições farmacêuticas e métodos úteis para aumentar asecreção de hormónio do crescimento (GH) a partir da pituitáriaanterior de mamíferos, incluindo em uma base de libertaçãosustentada.
BR0101674-1A 2000-04-28 2001-04-27 Antagonistas e agonistas de somatostatina queatuam no receptor sst subtipo 2 BR0101674A (pt)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US20031900P 2000-04-28 2000-04-28

Publications (1)

Publication Number Publication Date
BR0101674A true BR0101674A (pt) 2001-12-04

Family

ID=22741214

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0101674-1A BR0101674A (pt) 2000-04-28 2001-04-27 Antagonistas e agonistas de somatostatina queatuam no receptor sst subtipo 2

Country Status (5)

Country Link
US (2) US6495589B2 (pt)
EP (1) EP1149842A3 (pt)
JP (1) JP2002003498A (pt)
BR (1) BR0101674A (pt)
CA (1) CA2345569A1 (pt)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6495589B2 (en) * 2000-04-28 2002-12-17 Pfizer Inc. Somatostatin antagonists and agonists that act at the SST subtype 2 receptor
US6555581B1 (en) 2001-02-15 2003-04-29 Jones Pharma, Inc. Levothyroxine compositions and methods
US20060127442A1 (en) * 2004-12-09 2006-06-15 Helmus Michael N Use of supercritical fluids to incorporate biologically active agents into nanoporous medical articles
JP2008524427A (ja) * 2004-12-21 2008-07-10 ハーキュリーズ・インコーポレーテッド 亜硫酸イオンを含む製紙系において乾燥および湿潤紙力増強剤として使用するための反応性を有するカチオン性樹脂
US20080014152A1 (en) * 2006-07-13 2008-01-17 Di Mauro Thomas M Intranasal delivery of clenbuterol across the cribriform plate and into the brain
WO2008095063A1 (en) 2007-01-31 2008-08-07 Dana-Farber Cancer Institute, Inc. Stabilized p53 peptides and uses thereof
US7862825B2 (en) * 2007-02-21 2011-01-04 Mladen Vranic Method of controlling tight blood glucose by somatostatin receptor antagonists
EP2508531B1 (en) 2007-03-28 2016-10-19 President and Fellows of Harvard College Stitched polypeptides
WO2008134538A2 (en) * 2007-04-25 2008-11-06 Verto Institute Antibodies to human somatostatin receptor and methods of use
GB0903496D0 (en) * 2009-02-27 2009-04-08 Cambridge Entpr Ltd Methods for identification
SI2603600T1 (sl) 2010-08-13 2019-04-30 Aileron Therapeutics, Inc. Peptidomimetični makrocikli
AU2012326026B2 (en) 2011-10-18 2017-04-13 Aileron Therapeutics, Inc. Peptidomimetic macrocyles
CN112500466B (zh) 2012-02-15 2022-05-03 艾瑞朗医疗公司 拟肽大环化合物
WO2013123267A1 (en) 2012-02-15 2013-08-22 Aileron Therapeutics, Inc. Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles
AU2013337388B2 (en) 2012-11-01 2018-08-02 Aileron Therapeutics, Inc. Disubstituted amino acids and methods of preparation and use thereof
BR112017005598A2 (pt) 2014-09-24 2017-12-12 Aileron Therapeutics Inc macrociclos peptidomiméticos e usos dos mesmos
KR20170129879A (ko) 2015-03-20 2017-11-27 에일러론 테라퓨틱스 인코포레이티드 펩티드모방 거대고리 및 이의 용도
US10849955B2 (en) 2016-09-28 2020-12-01 City Of Hope Methods of treating pancreatic cancer using GPCR antagonists
WO2022000071A1 (en) * 2020-06-29 2022-01-06 Brandon University Matrix metalloproteinase inhibitors (mmpis)

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5270302A (en) * 1988-12-21 1993-12-14 Abbott Laboratories Derivatives of tetrapeptides as CCK agonists
DE4338015A1 (de) * 1993-11-08 1995-05-11 Asta Medica Ag Verwendung von D-glucopyranuronsäuren und deren Derivaten zum Einbau in pharmakologisch wirksame Peptide und deren Salze
US5936089A (en) 1995-05-29 1999-08-10 Pfizer Inc Dipeptides which promote release of growth hormone
US6025372A (en) 1997-04-04 2000-02-15 Merck & Co., Inc. Somatostatin agonists
US6063796A (en) 1997-04-04 2000-05-16 Merck & Co., Inc. Somatostatin agonists
US6057338A (en) * 1997-04-04 2000-05-02 Merck & Co., Inc. Somatostatin agonists
WO1999022735A1 (en) 1997-10-30 1999-05-14 Merck & Co., Inc. Somatostatin agonists
CZ20004580A3 (cs) 1998-06-12 2001-12-12 Societe De Conseils De Recherches Et D'application Beta-karbolinové sloučeniny
PT1086086E (pt) 1998-06-12 2005-02-28 Sod Conseils Rech Applic Derivados imidazolilo e sua utilizacao como ligandos de receptores da somatostatina
EP1086947A1 (en) * 1999-09-01 2001-03-28 Pfizer Products Inc. Somatostatin antagonists and agonists that act at the SST subtype 2 receptor
US6495589B2 (en) * 2000-04-28 2002-12-17 Pfizer Inc. Somatostatin antagonists and agonists that act at the SST subtype 2 receptor

Also Published As

Publication number Publication date
JP2002003498A (ja) 2002-01-09
EP1149842A3 (en) 2002-07-31
US20050054581A1 (en) 2005-03-10
US20010047030A1 (en) 2001-11-29
US6495589B2 (en) 2002-12-17
CA2345569A1 (en) 2001-10-28
EP1149842A2 (en) 2001-10-31

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Legal Events

Date Code Title Description
B08F Application fees: application dismissed [chapter 8.6 patent gazette]

Free format text: REFERENTE A 3A, 4A, 5A, 6A E 7A ANUIDADES.

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 PUBLICADO NA RPI 1963 DE 19.08.2008.