AU2002314067B2 - Dipeptide derivatives having a n-terminal 2-thioacyl group as vasopeptidase inhibitors - Google Patents

Dipeptide derivatives having a n-terminal 2-thioacyl group as vasopeptidase inhibitors Download PDF

Info

Publication number
AU2002314067B2
AU2002314067B2 AU2002314067A AU2002314067A AU2002314067B2 AU 2002314067 B2 AU2002314067 B2 AU 2002314067B2 AU 2002314067 A AU2002314067 A AU 2002314067A AU 2002314067 A AU2002314067 A AU 2002314067A AU 2002314067 B2 AU2002314067 B2 AU 2002314067B2
Authority
AU
Australia
Prior art keywords
lower alkyl
hydrogen
represent
carbocyclic
compound
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.)
Ceased
Application number
AU2002314067A
Other languages
English (en)
Other versions
AU2002314067A1 (en
Inventor
Cynthia Anne Fink
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.)
Novartis AG
Original Assignee
Novartis AG
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 Novartis AG filed Critical Novartis AG
Publication of AU2002314067A1 publication Critical patent/AU2002314067A1/en
Application granted granted Critical
Publication of AU2002314067B2 publication Critical patent/AU2002314067B2/en
Anticipated expiration legal-status Critical
Ceased 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
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/235Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/05Dipeptides
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/12Drugs for disorders of the metabolism for electrolyte homeostasis
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • 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
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • 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
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Emergency Medicine (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
AU2002314067A 2001-05-15 2002-05-14 Dipeptide derivatives having a n-terminal 2-thioacyl group as vasopeptidase inhibitors Ceased AU2002314067B2 (en)

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
AU2002314067A1 AU2002314067A1 (en) 2003-05-01
AU2002314067B2 true AU2002314067B2 (en) 2006-03-16

Family

ID=26966569

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2002314067A Ceased AU2002314067B2 (en) 2001-05-15 2002-05-14 Dipeptide derivatives having a n-terminal 2-thioacyl group as vasopeptidase inhibitors

Country Status (23)

Country Link
US (3) US6777443B2 (enExample)
EP (2) EP1392720A2 (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)

Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6777443B2 (en) * 2001-05-15 2004-08-17 Novartis Ag Dipeptide derivatives
WO2003004456A1 (en) * 2001-07-06 2003-01-16 Teva Pharmaceutical Industries Ltd. Process for the preparation of 7-amino syn 3,5-dihydroxy heptanoic acid derivatives via 6-cyano syn 3,5-dihydroxy hexanoic acid derivatives
WO2003027091A1 (en) * 2001-09-21 2003-04-03 Novartis Ag Pyrane derivatives as both ace- and nep- inhibitors
DE60315795T2 (de) * 2002-01-17 2008-06-05 Novartis Ag Pharmazeutische zusammensetzung enthaltend valsartan und nep-inhibitoren
US7468390B2 (en) 2002-01-17 2008-12-23 Novartis Ag Methods of treatment and pharmaceutical composition
ATE409476T1 (de) * 2002-06-13 2008-10-15 Novartis Pharma Gmbh Calciumsalze von statinen aus indol
ATE493973T1 (de) 2004-06-04 2011-01-15 Teva Pharma Irbesartan enthaltende pharmazeutische zusammensetzung
CA2590278A1 (en) * 2004-12-15 2006-06-22 Solvay Pharmaceuticals Gmbh Pharmaceutical compositions comprising nep-inhibitors, inhibitors of the endogenous endothelin producing system and hmg coa reductase inhibitors
WO2006097570A1 (en) * 2005-03-14 2006-09-21 Orion Corporation A combination treatment for enhancing diuresis
US7390789B2 (en) * 2005-09-13 2008-06-24 William H Simmons Thio-containing inhibitors of aminopeptidase P, and compositions thereof
US7400236B2 (en) 2005-10-21 2008-07-15 Gm Global Technology Operations, Inc. Vehicular lane monitoring system utilizing front and rear cameras
AR057882A1 (es) 2005-11-09 2007-12-26 Novartis Ag Compuestos de accion doble de bloqueadores del receptor de angiotensina e inhibidores de endopeptidasa neutra
US20120157387A1 (en) * 2006-11-28 2012-06-21 Apotex Technologies Inc. Orally bioavailable d-gamma-glutamyl-d-tryptophan
TW200838501A (en) * 2007-02-02 2008-10-01 Theravance Inc Dual-acting antihypertensive agents
TWI448284B (zh) 2007-04-24 2014-08-11 Theravance Inc 雙效抗高血壓劑
TWI406850B (zh) 2007-06-05 2013-09-01 Theravance Inc 雙效苯并咪唑抗高血壓劑
WO2009035543A1 (en) 2007-09-07 2009-03-19 Theravance, Inc. Dual-acting antihypertensive agents
EP2225210B1 (en) 2007-12-11 2012-04-25 Theravance, Inc. Dual-acting benzoimidazole derivative and their use as antihypertensive agents
EP2297113A1 (en) 2008-04-29 2011-03-23 Theravance, Inc. Dual-acting antihypertensive agents
WO2010011821A2 (en) 2008-07-24 2010-01-28 Theravance, Inc. Dual-acting antihypertensive agents
JP5833000B2 (ja) 2009-07-07 2015-12-16 セラヴァンス バイオファーマ アール&ディー アイピー, エルエルシー 二重に作用するピラゾール抗高血圧症薬
WO2011011232A1 (en) 2009-07-22 2011-01-27 Theravance, Inc. Dual-acting oxazole antihypertensive agents
EP2526095A1 (en) * 2010-01-19 2012-11-28 Theravance, Inc. Dual-acting thiophene, pyrrole, thiazole and furan antihypertensive agents
EA201391421A1 (ru) * 2011-03-31 2014-02-28 Апотекс Текнолоджиз Инк. Пролекарства d-гамма-глутамил-d-триптофана и d-гамма-глутамил-l-триптофана
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
CN121039147A (zh) * 2023-05-05 2025-11-28 上海济煜医药科技股份有限公司 一种短肽类化合物及其制备方法和医药应用

Family Cites Families (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3432307A1 (de) * 1984-09-03 1986-04-10 Boehringer Ingelheim KG, 6507 Ingelheim Aminosaeurederivate, verfahren zu ihrer herstellung und pharmazeutische zusammensetzungen
ES2074257T3 (es) 1989-11-27 1995-09-01 Santen Pharmaceutical Co Ltd Derivados de aminoacidos.
FR2679564A1 (fr) 1991-07-23 1993-01-29 Inst Nat Sante Rech Med Nouveaux acylmercaptoalcanoldipeptides, leur preparation et les compositions qui les contiennent.
ATE159515T1 (de) 1992-07-21 1997-11-15 Ciba Geigy Ag Oxamidsäure-derivate als hypocholesterämische mittel
US5432186A (en) * 1993-11-16 1995-07-11 Ciba-Geigy Corporation Cyclic amino acid derivatives
US5508266A (en) 1994-06-22 1996-04-16 Ciba-Geigy Corporation Gem-disubstituted amino acid derivatives
AU5122196A (en) 1995-03-31 1996-10-16 Takeda Chemical Industries Ltd. Cysteine protease inhibitor
US6147114A (en) * 1995-04-25 2000-11-14 Fuji Yakuhin Kogyo Kabushiki Kaisha Highly water-soluble metalloproteinase inhibitors
DE69627483T2 (de) 1995-05-10 2004-04-01 Darwin Discovery Ltd., Slough Peptidartige stoffe, die metalloproteinasen und die tnf-freisetzung hemmen, und ihre therapeutische verwendung
JPH11507352A (ja) * 1995-06-07 1999-06-29 ジンタ・インコーポレイテッド 新規カルバメート基本カチオン性脂質
US6245809B1 (en) * 1996-12-09 2001-06-12 Cor Therapeutics Inc. Integrin antagonists
US6492421B1 (en) * 1997-07-31 2002-12-10 Athena Neurosciences, Inc. Substituted phenylalanine type compounds which inhibit leukocyte adhesion mediated by VLA-4
DE19745151A1 (de) 1997-10-14 1999-04-15 Basf Ag Neue Verbindungen zur Behandlung von Krankheiten, die mit der biologischen Wirkung von Endothelin assoziiert sind
FR2770844A1 (fr) 1997-11-10 1999-05-14 Inst Nat Sante Rech Med Inhibiteurs de toxines clostridiales et compositions pharmaceutiques les contenant
US6576766B1 (en) * 1997-11-12 2003-06-10 Ariad Pharmaceuticals, Inc. Signal transduction inhibitors, compositions containing them
AU750048B2 (en) 1998-04-23 2002-07-11 Novartis Ag Certain heteroaryl substituted thiol inhibitors of endothelin-converting enzyme
ID26822A (id) 1998-04-23 2001-02-15 Novartis Ag Inhibitor tiol tertentu dari enzim pengubah endotelin
EP1140984B1 (en) 1998-12-31 2003-02-12 Aventis Pharmaceuticals Inc. Selective inhibitors of mmp-12
FR2788526B1 (fr) 1999-01-20 2002-07-05 Inst Nat Sante Rech Med Composes tripeptidiques utiles a titre d'hinhibiteurs selectifs de l'aminopeptidase a et compositions pharmaceutiques correspondantes
CO5160290A1 (es) 1999-03-29 2002-05-30 Novartis Ag Derivados de acido fenoxifeniloxamico sustituido .
US6503949B1 (en) * 1999-05-17 2003-01-07 Noro Nordisk A/S Glucagon antagonists/inverse agonists
GB9917909D0 (en) * 1999-07-31 1999-09-29 Synphar Lab Inc Cysteine protease inhibitors
CA2383002A1 (en) * 1999-08-27 2001-03-08 Cytovia, Inc. Substituted .alpha.-hydroxy acid caspase inhibitors and the use thereof
US6803383B2 (en) * 2000-03-27 2004-10-12 The Scripps Research Institute Inhibition of angiogenesis and tumor growth
AU2001287289A1 (en) 2000-04-03 2001-10-15 Bristol-Myers Squibb Company Vasopeptidase inhibitors to treat isolated systolic hypertensions
HUP0301335A3 (en) 2000-04-12 2006-02-28 Novartis Ag Combination of organic compounds
US20020013307A1 (en) 2000-05-23 2002-01-31 Pablo Lapuerta Use of vasopeptidase inhibitors to treat or slow the progression of cognitive dysfunction and to treat and/or prevent dementia
US6777443B2 (en) * 2001-05-15 2004-08-17 Novartis Ag Dipeptide derivatives

Also Published As

Publication number Publication date
NO20035084D0 (no) 2003-11-14
US6777443B2 (en) 2004-08-17
WO2002092622A3 (en) 2003-04-10
PE20030042A1 (es) 2003-02-28
US6992105B2 (en) 2006-01-31
CZ20033077A3 (cs) 2004-02-18
US20060058242A1 (en) 2006-03-16
PL366786A1 (en) 2005-02-07
KR20030096401A (ko) 2003-12-24
EP1392720A2 (en) 2004-03-03
MXPA03010403A (es) 2004-03-09
CA2449292A1 (en) 2002-11-21
IL158772A0 (en) 2004-05-12
EP2239268A1 (en) 2010-10-13
SK14032003A3 (sk) 2004-06-08
US20020183260A1 (en) 2002-12-05
WO2002092622A2 (en) 2002-11-21
AR035890A1 (es) 2004-07-21
HUP0304084A2 (hu) 2004-12-28
BR0209652A (pt) 2004-07-13
NZ529438A (en) 2005-07-29
MY127495A (en) 2006-12-29
HUP0304084A3 (en) 2010-10-28
RU2003134153A (ru) 2005-06-10
KR100908152B1 (ko) 2009-07-16
US20040235754A1 (en) 2004-11-25
RU2298559C2 (ru) 2007-05-10
CN1649893A (zh) 2005-08-03
JP2005504011A (ja) 2005-02-10
WO2002092622A8 (en) 2004-01-22
NO20035084L (no) 2004-01-15
TWI295996B (en) 2008-04-21
JP4390458B2 (ja) 2009-12-24
CO5540347A2 (es) 2005-07-29

Similar Documents

Publication Publication Date Title
AU2002314067B2 (en) Dipeptide derivatives having a n-terminal 2-thioacyl group as vasopeptidase inhibitors
AU2002314067A1 (en) Dipeptide derivatives having a n-terminal 2-thioacyl group as vasopeptidase inhibitors
US5508266A (en) Gem-disubstituted amino acid derivatives
EP0655461B1 (en) Cyclic amino acid derivatives having ACE and NEP inhibiting activity
JP4263095B2 (ja) Aceおよびnepの両阻害剤としてのピラン誘導体
US5506244A (en) Cyclic amino acid derivatives
WO1999055726A1 (en) Certain thiol inhibitors of endothelin-converting enzyme
EP1080104B1 (en) Certain heteroaryl substituted thiol inhibitors of endothelin-converting enzyme
US6689801B2 (en) Certain heteroaryl substituted thiol inhibitors of endothelin-converting enzyme
ZA200308590B (en) Dipeptide derivatives having a n-terminal 2-thiocyl group as vasopeptidase inhibitors.
HK1068332B (en) Pyrane derivatives as both ace- and nep-inhibitors
WO2001077095A2 (en) Derivatives of alpha-mercaptoacetamide

Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired