ATE399011T1 - Substituierte diketopiperazine als oxytocin- antagonisten - Google Patents

Substituierte diketopiperazine als oxytocin- antagonisten

Info

Publication number
ATE399011T1
ATE399011T1 AT02799077T AT02799077T ATE399011T1 AT E399011 T1 ATE399011 T1 AT E399011T1 AT 02799077 T AT02799077 T AT 02799077T AT 02799077 T AT02799077 T AT 02799077T AT E399011 T1 ATE399011 T1 AT E399011T1
Authority
AT
Austria
Prior art keywords
oxytocin antagonists
substituted diketopiperazine
oxytocin
diketopiperazine
substituted
Prior art date
Application number
AT02799077T
Other languages
English (en)
Inventor
Alan Borthwick
Richard Hatley
Deirdre HICKEY
John Liddle
David Livermore
Andrew Mason
Neil Miller
Fabrizio Nerozzi
Steven Sollis
Anna Szardenings
Paul Wyatt
Original Assignee
Glaxo Group Ltd
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 Glaxo Group Ltd filed Critical Glaxo Group Ltd
Application granted granted Critical
Publication of ATE399011T1 publication Critical patent/ATE399011T1/de

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/06Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members
    • C07D241/08Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members with oxygen atoms directly attached to ring carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/06Antiabortive agents; Labour repressants
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/10Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic 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
    • C07K5/06008Dipeptides 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
    • C07K5/06191Dipeptides 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)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Epidemiology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AT02799077T 2001-12-21 2002-12-20 Substituierte diketopiperazine als oxytocin- antagonisten ATE399011T1 (de)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB0130677.8A GB0130677D0 (en) 2001-12-21 2001-12-21 Medicaments and novel compounds

Publications (1)

Publication Number Publication Date
ATE399011T1 true ATE399011T1 (de) 2008-07-15

Family

ID=9928187

Family Applications (1)

Application Number Title Priority Date Filing Date
AT02799077T ATE399011T1 (de) 2001-12-21 2002-12-20 Substituierte diketopiperazine als oxytocin- antagonisten

Country Status (27)

Country Link
US (3) US7514437B2 (de)
EP (1) EP1458393B1 (de)
JP (1) JP4638149B2 (de)
KR (2) KR20100060012A (de)
CN (1) CN100374115C (de)
AT (1) ATE399011T1 (de)
AU (1) AU2002364304B2 (de)
BR (1) BRPI0215277B1 (de)
CA (1) CA2471355C (de)
CO (1) CO5590916A2 (de)
CY (1) CY1108334T1 (de)
DE (1) DE60227283D1 (de)
DK (1) DK1458393T3 (de)
ES (1) ES2307827T3 (de)
GB (1) GB0130677D0 (de)
HU (1) HU229708B1 (de)
IL (2) IL162515A0 (de)
IS (1) IS2613B (de)
MX (1) MXPA04006033A (de)
NO (1) NO329543B1 (de)
NZ (1) NZ533218A (de)
PL (1) PL215826B1 (de)
PT (1) PT1458393E (de)
RU (1) RU2303032C2 (de)
SI (1) SI1458393T1 (de)
WO (1) WO2003053443A1 (de)
ZA (1) ZA200404326B (de)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0314738D0 (en) * 2003-06-24 2003-07-30 Glaxo Group Ltd Novel compounds
GB0314733D0 (en) * 2003-06-24 2003-07-30 Glaxo Group Ltd Medicaments
GB0414092D0 (en) * 2004-06-23 2004-07-28 Glaxo Group Ltd Novel compounds
GB0414100D0 (en) * 2004-06-23 2004-07-28 Glaxo Group Ltd Novel compounds
GB0414093D0 (en) * 2004-06-23 2004-07-28 Glaxo Group Ltd Novel compounds
GB0428235D0 (en) * 2004-12-23 2005-01-26 Glaxo Group Ltd Novel compounds
AP2007004047A0 (en) 2005-01-20 2007-06-30 Pfizer Ltd Substituted triazole derivatives as oxtocin antagonists
RU2318818C1 (ru) * 2006-04-12 2008-03-10 Общество С Ограниченной Ответственностью "Исследовательский Институт Химического Разнообразия" Азагетероциклы, комбинаторная библиотека, фокусированная библиотека, фармацевтическая композиция и способ получения (варианты)
US9403789B2 (en) 2008-02-21 2016-08-02 Sequoia Pharmaceuticals, Inc. Benzofuran-containing amino acid inhibitors of cytochrome P450
ES2593859T3 (es) * 2008-08-22 2016-12-13 British Columbia Cancer Agency Branch Moléculas pequeñas inhibidoras de la activación del extremo N del receptor de andrógenos
EP2493874A1 (de) 2009-10-30 2012-09-05 Glaxo Group Limited Neue kristalline formen von (3r,6r) -3- (2, 3 -dihydro- 1h- inden- 2 -yl) - 1 - [ (1r) - 1 - (2, 6 - dimethyl - 3 - pyridinyl) - 2 - (4 -morpholinyl) -2-oxoethyl]-6- [(1s) - 1 -methylpropyl]-2,5- piperazinedion
JP5579939B2 (ja) * 2010-10-29 2014-08-27 ロンザ リミテッド ジケトピペラジン形成ジペプチジルリンカー
CN103242246A (zh) * 2013-05-21 2013-08-14 苏州科捷生物医药有限公司 3-位取代的n-甲基哌嗪的合成方法
CN105061317B (zh) * 2015-08-26 2017-08-25 浙江大果生物医药科技有限公司 一类吲唑盐类化合物及其制备方法和应用
LT3400217T (lt) 2016-01-04 2022-06-27 Merck Serono S.A. Hidroksipropiltiazolidino karboksamido l-valinato darinys, jo druska ir jo kristalinė forma
WO2018015497A2 (en) 2016-07-21 2018-01-25 ObsEva S.A. Oxytocin antagonist dosing regimens for promoting embryo implantation and preventing miscarriage
CN109305969B (zh) * 2017-07-27 2023-03-10 江苏恒瑞医药股份有限公司 哌嗪-2,5-二酮类衍生物、其制备方法及其在医药上的应用
CN109485598A (zh) * 2018-11-29 2019-03-19 河南师范大学 一种去除氨基上喹啉保护基的新方法
AU2020340670A1 (en) 2019-09-03 2022-04-07 ObsEva S.A. Oxytocin antagonist dosing regimens for promoting embryo implantation and preventing miscarriage
WO2021160597A1 (en) 2020-02-10 2021-08-19 ObsEva S.A. Biomarkers for oxytocin receptor antagonist therapy

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4596819A (en) * 1984-01-23 1986-06-24 Warner-Lambert Company Modified tripeptides
HUT67287A (en) * 1991-09-13 1995-03-28 Merck & Co Inc Piperazynil camphor derivatives and pharmaceutical compositions containing them
US5464788A (en) * 1994-03-24 1995-11-07 Merck & Co., Inc. Tocolytic oxytocin receptor antagonists
US5817751A (en) * 1994-06-23 1998-10-06 Affymax Technologies N.V. Method for synthesis of diketopiperazine and diketomorpholine derivatives
GB2326639A (en) 1997-06-18 1998-12-30 Merck & Co Inc Piperazine Oxytocin Receptor Antagonists
GB9713748D0 (en) * 1997-06-27 1997-09-03 Unilever Plc Production of detergent granulates
WO1999037304A1 (en) * 1998-01-27 1999-07-29 Aventis Pharmaceuticals Products Inc. SUBSTITUTED OXOAZAHETEROCYCLYL FACTOR Xa INHIBITORS
HUP0101329A3 (en) 1998-01-29 2002-07-29 Aventis Pharmaceuticals Inc Co Method for preparing an n-[(aliphatic or aromatic)carbonyl]-2-aminoacetamide compounds and a cyclyzed compounds there from
CA2289621A1 (en) * 1998-03-16 1999-09-23 Ontogen Corporation Piperazines as inhibitors of fructose-1,6-bisphosphatase (fbpase)
GB0314738D0 (en) 2003-06-24 2003-07-30 Glaxo Group Ltd Novel compounds
GB0314733D0 (en) 2003-06-24 2003-07-30 Glaxo Group Ltd Medicaments
GB0414100D0 (en) 2004-06-23 2004-07-28 Glaxo Group Ltd Novel compounds
GB0414092D0 (en) 2004-06-23 2004-07-28 Glaxo Group Ltd Novel compounds
GB0414093D0 (en) 2004-06-23 2004-07-28 Glaxo Group Ltd Novel compounds
GB0428235D0 (en) 2004-12-23 2005-01-26 Glaxo Group Ltd Novel compounds

Also Published As

Publication number Publication date
ES2307827T3 (es) 2008-12-01
US20050148572A1 (en) 2005-07-07
GB0130677D0 (en) 2002-02-06
US7514437B2 (en) 2009-04-07
DE60227283D1 (de) 2008-08-07
AU2002364304A1 (en) 2003-07-09
CY1108334T1 (el) 2014-02-12
EP1458393A1 (de) 2004-09-22
US8541579B2 (en) 2013-09-24
NO329543B1 (no) 2010-11-08
IS7315A (is) 2004-06-16
IS2613B (is) 2010-04-15
CN100374115C (zh) 2008-03-12
BRPI0215277B1 (pt) 2016-05-03
RU2303032C2 (ru) 2007-07-20
KR20100060012A (ko) 2010-06-04
US20090186867A1 (en) 2009-07-23
IL162515A0 (en) 2005-11-20
BR0215277A (pt) 2004-12-14
CA2471355C (en) 2013-04-23
MXPA04006033A (es) 2004-09-27
NZ533218A (en) 2007-01-26
US20130131338A1 (en) 2013-05-23
ZA200404326B (en) 2005-09-28
CN1606443A (zh) 2005-04-13
KR100997856B1 (ko) 2010-12-01
HUP0500136A2 (hu) 2005-05-30
EP1458393B1 (de) 2008-06-25
PL215826B1 (pl) 2014-01-31
CO5590916A2 (es) 2005-12-30
JP4638149B2 (ja) 2011-02-23
HU229708B1 (en) 2014-05-28
DK1458393T3 (da) 2008-10-13
CA2471355A1 (en) 2003-07-03
HK1069339A1 (en) 2005-05-20
KR20040065285A (ko) 2004-07-21
JP2005517663A (ja) 2005-06-16
RU2004122392A (ru) 2005-04-20
SI1458393T1 (sl) 2008-10-31
PT1458393E (pt) 2008-09-29
AU2002364304B2 (en) 2008-04-17
PL370981A1 (en) 2005-06-13
US8367673B2 (en) 2013-02-05
NO20043115L (no) 2004-07-20
WO2003053443A1 (en) 2003-07-03
IL162515A (en) 2012-08-30

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