TWI348466B - Novel diketopiperazine derivatives as oxytocin receptor antagonists - Google Patents

Novel diketopiperazine derivatives as oxytocin receptor antagonists

Info

Publication number
TWI348466B
TWI348466B TW094120517A TW94120517A TWI348466B TW I348466 B TWI348466 B TW I348466B TW 094120517 A TW094120517 A TW 094120517A TW 94120517 A TW94120517 A TW 94120517A TW I348466 B TWI348466 B TW I348466B
Authority
TW
Taiwan
Prior art keywords
receptor antagonists
oxytocin receptor
diketopiperazine derivatives
novel
novel diketopiperazine
Prior art date
Application number
TW094120517A
Other languages
English (en)
Other versions
TW200616636A (en
Inventor
Alan David Borthwick
Deirdre Mary Bernadette Hickey
John Liddle
Andrew Mcmurtrie Mason
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=32800053&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=TWI348466(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Glaxo Group Ltd filed Critical Glaxo Group Ltd
Publication of TW200616636A publication Critical patent/TW200616636A/zh
Application granted granted Critical
Publication of TWI348466B publication Critical patent/TWI348466B/zh

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Classifications

    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/06—Antiabortive agents; Labour repressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/06—Heterocyclic 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 only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/06—Heterocyclic 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 only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Epidemiology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Cardiology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Anesthesiology (AREA)
  • Obesity (AREA)
  • Diabetes (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Nutrition Science (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
TW094120517A 2004-06-23 2005-06-21 Novel diketopiperazine derivatives as oxytocin receptor antagonists TWI348466B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB0414093.5A GB0414093D0 (en) 2004-06-23 2004-06-23 Novel compounds

Publications (2)

Publication Number Publication Date
TW200616636A TW200616636A (en) 2006-06-01
TWI348466B true TWI348466B (en) 2011-09-11

Family

ID=32800053

Family Applications (1)

Application Number Title Priority Date Filing Date
TW094120517A TWI348466B (en) 2004-06-23 2005-06-21 Novel diketopiperazine derivatives as oxytocin receptor antagonists

Country Status (30)

Country Link
US (9) US7550462B2 (zh)
EP (2) EP2918580A1 (zh)
JP (2) JP5405019B2 (zh)
KR (1) KR101186447B1 (zh)
CN (1) CN1972924B (zh)
AR (1) AR049405A1 (zh)
AU (1) AU2005256470B2 (zh)
BR (1) BRPI0512376A (zh)
CA (1) CA2571527C (zh)
CY (1) CY1116183T1 (zh)
DK (1) DK1758886T3 (zh)
ES (1) ES2537801T3 (zh)
GB (1) GB0414093D0 (zh)
HK (2) HK1208669A1 (zh)
HR (1) HRP20150401T1 (zh)
HU (1) HUE025869T2 (zh)
IL (2) IL179905A0 (zh)
MA (1) MA28675B1 (zh)
MX (1) MXPA06014545A (zh)
MY (1) MY143578A (zh)
NO (1) NO338769B1 (zh)
NZ (1) NZ551733A (zh)
PE (1) PE20060477A1 (zh)
PL (1) PL1758886T3 (zh)
PT (1) PT1758886E (zh)
RU (1) RU2382038C2 (zh)
SI (1) SI1758886T1 (zh)
TW (1) TWI348466B (zh)
WO (1) WO2006000399A1 (zh)
ZA (1) ZA200610022B (zh)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0130677D0 (en) 2001-12-21 2002-02-06 Glaxo Group Ltd Medicaments and novel compounds
DK1572950T3 (da) 2002-06-17 2013-02-04 Thrasos Inc Enkeltdomæne TDF-relaterede forbindelser og analoger deraf
GB0314738D0 (en) 2003-06-24 2003-07-30 Glaxo Group Ltd Novel compounds
AU2005265098B2 (en) 2004-06-17 2012-02-23 Thrasos Innovation, Inc. TDF-related compounds and analogs thereof
GB0414093D0 (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
EP1945258A4 (en) 2005-09-20 2011-08-17 Thrasos Therapeutics Inc FDT RELATED COMPOUNDS AND THEIR ANALOGUES
US8716286B2 (en) 2009-10-30 2014-05-06 Glaxo Group Limited Crystalline forms of (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-piperazinedione
KR20180099708A (ko) 2016-01-04 2018-09-05 메르크 세로노 에스. 에이. 하이드록시프로필티아졸리딘 카르복사미드 유도체의 알파-아미노 에스테르 및 이의 염 형태, 결정 다형체
WO2017203012A1 (en) * 2016-05-27 2017-11-30 Glaxosmithkline Intellectual Property (No.2) Limited Epelsiban for use in the treatment of adenomyosis
ES2898778T3 (es) 2016-07-21 2022-03-08 ObsEva SA Pautas posológicas de antagonistas de oxitocina para promover la implantación de embriones y prevenir aborto espontáneo
EP3805763A4 (en) * 2018-05-29 2022-03-09 Kao Corporation SHEET COMFORT EVOCATION PERFORMANCE EVALUATION METHOD AND COMFORT EVOCATION SHEET
CA3149898A1 (en) 2019-09-03 2021-03-11 Ernest Loumaye Oxytocin antagonist dosing regimens for promoting embryo implantation and preventing miscarriage
CN115380122A (zh) 2020-02-10 2022-11-22 奥布赛瓦股份公司 用于催产素受体拮抗剂疗法的生物标志物

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
DE3830096A1 (de) 1988-09-03 1990-03-15 Hoechst Ag Piperazindione mit psychotroper wirkung
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
ZA99607B (en) 1998-01-27 1999-07-27 Rhone Poulenc Rorer Pharma Substituted oxoazaheterocyclyl factor xa inhibitors.
CA2318601A1 (en) 1998-01-29 1999-08-05 Aventis Pharmaceuticals Products Inc. Method for preparing an n-[(aliphatic or aromatic)carbonyl]-2-aminoacetamide compound and a cyclyzed compound
US6107274A (en) 1998-03-16 2000-08-22 Ontogen Corporation Piperazines as inhibitors of fructose-1,6-bisphosphatase (FBPase)
GB0130677D0 (en) * 2001-12-21 2002-02-06 Glaxo Group Ltd Medicaments and novel compounds
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
GB0414093D0 (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
GB0414092D0 (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
CA2571527A1 (en) 2006-01-05
RU2382038C2 (ru) 2010-02-20
SI1758886T1 (sl) 2015-06-30
HK1208669A1 (zh) 2016-03-11
ZA200610022B (en) 2008-07-30
AU2005256470B2 (en) 2012-02-02
IL237513A0 (en) 2015-04-30
US20070254888A1 (en) 2007-11-01
EP1758886B1 (en) 2015-03-04
AR049405A1 (es) 2006-07-26
BRPI0512376A (pt) 2008-03-11
MXPA06014545A (es) 2007-03-12
US7919492B2 (en) 2011-04-05
PT1758886E (pt) 2015-04-22
US7550462B2 (en) 2009-06-23
PL1758886T3 (pl) 2015-08-31
US20120202811A1 (en) 2012-08-09
US9408851B2 (en) 2016-08-09
PE20060477A1 (es) 2006-08-24
NO20070173L (no) 2007-01-22
HUE025869T2 (en) 2016-05-30
EP2918580A1 (en) 2015-09-16
TW200616636A (en) 2006-06-01
US20160030442A1 (en) 2016-02-04
ES2537801T3 (es) 2015-06-12
JP5503709B2 (ja) 2014-05-28
CA2571527C (en) 2013-02-26
MY143578A (en) 2011-05-31
US20110152262A1 (en) 2011-06-23
US20150157640A1 (en) 2015-06-11
CN1972924B (zh) 2011-07-20
JP2013010790A (ja) 2013-01-17
JP5405019B2 (ja) 2014-02-05
US20130253188A1 (en) 2013-09-26
MA28675B1 (fr) 2007-06-01
HRP20150401T1 (hr) 2015-05-08
NZ551733A (en) 2010-06-25
NO338769B1 (no) 2016-10-17
DK1758886T3 (da) 2015-04-27
US20100305127A1 (en) 2010-12-02
GB0414093D0 (en) 2004-07-28
KR20070031953A (ko) 2007-03-20
CN1972924A (zh) 2007-05-30
IL179905A0 (en) 2007-05-15
US8202864B2 (en) 2012-06-19
JP2008503534A (ja) 2008-02-07
AU2005256470A1 (en) 2006-01-05
KR101186447B1 (ko) 2012-09-27
US20090247541A1 (en) 2009-10-01
RU2007102274A (ru) 2008-07-27
US8742099B2 (en) 2014-06-03
WO2006000399A1 (en) 2006-01-05
EP1758886A1 (en) 2007-03-07
HK1106499A1 (zh) 2008-03-14
CY1116183T1 (el) 2017-02-08
US20140235639A1 (en) 2014-08-21

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