KR100908152B1 - 바소펩티다제 억제제로서 ｎ-말단 2-티오아실기를 갖는디펩티드 유도체 - Google Patents

바소펩티다제 억제제로서 ｎ-말단 2-티오아실기를 갖는디펩티드 유도체 Download PDF

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KR100908152B1
KR100908152B1 KR1020037014849A KR20037014849A KR100908152B1 KR 100908152 B1 KR100908152 B1 KR 100908152B1 KR 1020037014849 A KR1020037014849 A KR 1020037014849A KR 20037014849 A KR20037014849 A KR 20037014849A KR 100908152 B1 KR100908152 B1 KR 100908152B1
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alkyl
compound
carbocyclic aryl
hydrogen
represent
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KR20030096401A (ko
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신시아 앤 핑크
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노파르티스 아게
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    • 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
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/235—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
    • 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
    • A61K38/05—Dipeptides
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • 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
    • 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
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • 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
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Emergency Medicine (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
KR1020037014849A 2001-05-15 2002-05-14 바소펩티다제 억제제로서 ｎ-말단 2-티오아실기를 갖는디펩티드 유도체 Expired - Fee Related KR100908152B1 (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US29108801P 2001-05-15 2001-05-15
US60/291,088 2001-05-15
US33957501P 2001-12-11 2001-12-11
US60/339,575 2001-12-11
PCT/EP2002/005293 WO2002092622A2 (en) 2001-05-15 2002-05-14 Dipeptide derivatives having a n-terminal 2-thioacyl group as vasopeptidase inhibitors

Publications (2)

Publication Number Publication Date
KR20030096401A KR20030096401A (ko) 2003-12-24
KR100908152B1 true KR100908152B1 (ko) 2009-07-16

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Country Status (23)

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US (3) US6777443B2 (enExample)
EP (2) EP2239268A1 (enExample)
JP (1) JP4390458B2 (enExample)
KR (1) KR100908152B1 (enExample)
CN (1) CN1649893A (enExample)
AR (1) AR035890A1 (enExample)
AU (1) AU2002314067B2 (enExample)
BR (1) BR0209652A (enExample)
CA (1) CA2449292A1 (enExample)
CO (1) CO5540347A2 (enExample)
CZ (1) CZ20033077A3 (enExample)
HU (1) HUP0304084A3 (enExample)
IL (1) IL158772A0 (enExample)
MX (1) MXPA03010403A (enExample)
MY (1) MY127495A (enExample)
NO (1) NO20035084L (enExample)
NZ (1) NZ529438A (enExample)
PE (1) PE20030042A1 (enExample)
PL (1) PL366786A1 (enExample)
RU (1) RU2298559C2 (enExample)
SK (1) SK14032003A3 (enExample)
TW (1) TWI295996B (enExample)
WO (1) WO2002092622A2 (enExample)

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JP4263095B2 (ja) * 2001-09-21 2009-05-13 ノバルティス アクチエンゲゼルシャフト Ａｃｅおよびｎｅｐの両阻害剤としてのピラン誘導体
US7468390B2 (en) 2002-01-17 2008-12-23 Novartis Ag Methods of treatment and pharmaceutical composition
DE60315795T2 (de) * 2002-01-17 2008-06-05 Novartis Ag Pharmazeutische zusammensetzung enthaltend valsartan und nep-inhibitoren
ES2315510T3 (es) * 2002-06-13 2009-04-01 Novartis Ag Sales de calcio de estatinas derivadas del indol.
WO2005118166A2 (en) 2004-06-04 2005-12-15 Teva Pharmaceutical Industries, Ltd. Pharmaceutical composition containing irbesartan
US7816347B2 (en) * 2004-12-15 2010-10-19 Solvay Pharmaceuticals Gmbh Pharmaceutical compositions comprising NEP-inhibitors, inhibitors of the endogenous endothelin producing system and HMG CoA reductase inhibitors
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US7390789B2 (en) * 2005-09-13 2008-06-24 William H Simmons Thio-containing inhibitors of aminopeptidase P, and compositions thereof
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US20120157387A1 (en) * 2006-11-28 2012-06-21 Apotex Technologies Inc. Orally bioavailable d-gamma-glutamyl-d-tryptophan
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JP2010538071A (ja) * 2007-09-07 2010-12-09 セラヴァンス， インコーポレーテッド 二重作用性降圧剤
EP2225210B1 (en) 2007-12-11 2012-04-25 Theravance, Inc. Dual-acting benzoimidazole derivative and their use as antihypertensive agents
JP2011518884A (ja) 2008-04-29 2011-06-30 セラヴァンス， インコーポレーテッド 二重活性抗高血圧剤
US7863309B2 (en) 2008-07-24 2011-01-04 Theravance, Inc. Dual-acting antihypertensive agents
US7956054B2 (en) 2009-07-07 2011-06-07 Theravance, Inc. Dual-acting pyrazole antihypertensive agents
EP2456762B1 (en) 2009-07-22 2013-10-16 Theravance, Inc. Dual-acting oxazole antihypertensive agents
WO2011090929A1 (en) 2010-01-19 2011-07-28 Theravance, Inc. Dual-acting thiophene, pyrrole, thiazole and furan antihypertensive agents
CA2831429A1 (en) * 2011-03-31 2012-10-04 Apotex Technologies Inc. Prodrugs of d-gamma-glutamyl-d-tryptophan and d-gamma- glutamyl-l-tryptophan
US9212206B1 (en) * 2014-11-24 2015-12-15 William H Simmons 4-Fluoro-Thio-containing inhibitors of APP2, compositions thereof and method of use
WO2018002673A1 (en) 2016-07-01 2018-01-04 N4 Pharma Uk Limited Novel formulations of angiotensin ii receptor antagonists
UY38072A (es) 2018-02-07 2019-10-01 Novartis Ag Compuestos derivados de éster butanoico sustituido con bisfenilo como inhibidores de nep, composiciones y combinaciones de los mismos
US11396497B2 (en) 2018-05-04 2022-07-26 New Mexico Tech University Research Park Corporation Proteasome inhibitors
CN113956183B (zh) * 2021-10-28 2023-06-20 成都市科隆化学品有限公司 一种Boc-Ser(Bzl)-OH及其制备方法
WO2024230583A1 (zh) * 2023-05-05 2024-11-14 上海济煜医药科技有限公司 一种短肽类化合物及其制备方法和医药应用

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Also Published As

Publication number Publication date
AU2002314067B2 (en) 2006-03-16
TWI295996B (en) 2008-04-21
JP4390458B2 (ja) 2009-12-24
PL366786A1 (en) 2005-02-07
EP1392720A2 (en) 2004-03-03
RU2003134153A (ru) 2005-06-10
WO2002092622A8 (en) 2004-01-22
SK14032003A3 (sk) 2004-06-08
PE20030042A1 (es) 2003-02-28
EP2239268A1 (en) 2010-10-13
MY127495A (en) 2006-12-29
CN1649893A (zh) 2005-08-03
BR0209652A (pt) 2004-07-13
US20020183260A1 (en) 2002-12-05
MXPA03010403A (es) 2004-03-09
CO5540347A2 (es) 2005-07-29
AR035890A1 (es) 2004-07-21
US6992105B2 (en) 2006-01-31
WO2002092622A2 (en) 2002-11-21
NO20035084D0 (no) 2003-11-14
US6777443B2 (en) 2004-08-17
WO2002092622A3 (en) 2003-04-10
US20040235754A1 (en) 2004-11-25
HUP0304084A3 (en) 2010-10-28
US20060058242A1 (en) 2006-03-16
CZ20033077A3 (cs) 2004-02-18
KR20030096401A (ko) 2003-12-24
IL158772A0 (en) 2004-05-12
NZ529438A (en) 2005-07-29
HUP0304084A2 (hu) 2004-12-28
RU2298559C2 (ru) 2007-05-10
CA2449292A1 (en) 2002-11-21
JP2005504011A (ja) 2005-02-10
NO20035084L (no) 2004-01-15

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