ZA200509890B - Substitution diketopiperazines and their use as oxytocin antagonists - Google Patents

Substitution diketopiperazines and their use as oxytocin antagonists Download PDF

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Publication number
ZA200509890B
ZA200509890B ZA200509890A ZA200509890A ZA200509890B ZA 200509890 B ZA200509890 B ZA 200509890B ZA 200509890 A ZA200509890 A ZA 200509890A ZA 200509890 A ZA200509890 A ZA 200509890A ZA 200509890 B ZA200509890 B ZA 200509890B
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ZA
South Africa
Prior art keywords
compound
formula
methyl
oxytocin
exemplified
Prior art date
Application number
ZA200509890A
Other languages
English (en)
Inventor
John Liddle
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
Publication of ZA200509890B publication Critical patent/ZA200509890B/en

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    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • 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
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • 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
    • A61P5/10Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/10Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH
    • A61P5/12Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH for decreasing, blocking or antagonising the activity of the posterior pituitary hormones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/36Antigestagens
    • 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
    • A61P9/12Antihypertensives
    • 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
    • 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
    • C07D413/06Heterocyclic 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
    • 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
    • C07D413/14Heterocyclic 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Neurosurgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Reproductive Health (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
ZA200509890A 2003-06-24 2005-12-06 Substitution diketopiperazines and their use as oxytocin antagonists ZA200509890B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GB0314738A GB0314738D0 (en) 2003-06-24 2003-06-24 Novel compounds

Publications (1)

Publication Number Publication Date
ZA200509890B true ZA200509890B (en) 2006-07-26

Family

ID=27637257

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA200509890A ZA200509890B (en) 2003-06-24 2005-12-06 Substitution diketopiperazines and their use as oxytocin antagonists

Country Status (31)

Country Link
US (6) US8071594B2 (ja)
EP (1) EP1641787B1 (ja)
JP (1) JP5128126B2 (ja)
KR (1) KR101131378B1 (ja)
CN (2) CN101597282A (ja)
AR (1) AR044869A1 (ja)
AT (1) ATE361295T1 (ja)
AU (1) AU2004251868B2 (ja)
BR (1) BRPI0411729A (ja)
CA (1) CA2530310C (ja)
CY (1) CY1107703T1 (ja)
DE (1) DE602004006268T2 (ja)
DK (1) DK1641787T3 (ja)
EG (1) EG24929A (ja)
ES (1) ES2285474T3 (ja)
GB (1) GB0314738D0 (ja)
HK (1) HK1088910A1 (ja)
HR (1) HRP20070286T3 (ja)
IL (1) IL172529A (ja)
IS (1) IS2463B (ja)
MA (1) MA27887A1 (ja)
MX (1) MXPA05014068A (ja)
MY (1) MY140653A (ja)
NO (1) NO332677B1 (ja)
NZ (1) NZ544006A (ja)
PL (1) PL1641787T3 (ja)
PT (1) PT1641787E (ja)
RU (1) RU2343152C2 (ja)
TW (1) TWI340745B (ja)
WO (1) WO2005000840A1 (ja)
ZA (1) ZA200509890B (ja)

Families Citing this family (12)

* 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
GB0314738D0 (en) * 2003-06-24 2003-07-30 Glaxo Group Ltd Novel compounds
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
GB0428235D0 (en) * 2004-12-23 2005-01-26 Glaxo Group Ltd Novel compounds
JP2013509391A (ja) 2009-10-30 2013-03-14 グラクソ グループ リミテッド (3r,6r)−3−(2,3−ジヒドロ−1h−インデン−2−イル)−1−[(1r)−1−(2,6−ジメチル−3−ピリジニル)−2−(4−モルホリニル)−2−オキソエチル]−6−[(1s)−1−メチルプロピル]−2,5−ピペラジンジオンの新規結晶性形態
RU2017100906A (ru) 2014-06-16 2018-07-16 Глэксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед Ретосибан для лечения преждевременных родов
AU2017205670B2 (en) 2016-01-04 2021-05-20 Merck Serono S.A. L-valinate of hydroxypropylthiazolidine carboxamide derivative and salt form, crystal polymorph thereof
CA3031252A1 (en) 2016-07-21 2018-01-25 ObsEva S.A. Oxytocin antagonist dosing regimens for promoting embryo implantation and preventing miscarriage
CN106674031A (zh) * 2016-11-18 2017-05-17 浙江工业大学 R‑2‑二氢茚氨酸的制备方法
EP4025207A1 (en) 2019-09-03 2022-07-13 ObsEva S.A. Oxytocin antagonist dosing regimens for promoting embryo implantation and preventing miscarriage
US20230102503A1 (en) 2020-02-10 2023-03-30 ObsEva S.A. Biomarkers for oxytocin receptor antagonist therapy

Family Cites Families (20)

* 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
US5091387A (en) * 1990-03-02 1992-02-25 Merck & Co., Inc. Spirocyclic oxytocin antagonists
GB9217331D0 (en) 1992-08-14 1992-09-30 Xenova Ltd Pharmaceutical compounds
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
US5968938A (en) * 1997-06-18 1999-10-19 Merck & Co., Inc. Piperazine oxytocin receptor antagonists
KR20010034442A (ko) 1998-01-27 2001-04-25 아벤티스 파마슈티칼즈 프로덕츠 인코포레이티드 치환된 옥소아자헤테로사이클릴 인자 Xa 억제제
EA003061B1 (ru) 1998-01-29 2002-12-26 Авентис Фармасьютикалз Инк. Способ получения n-[(алифатическая или ароматическая группа) карбонил]-2- аминоацетамидов и циклических соединений
AU3087099A (en) * 1998-03-16 1999-10-11 Ontogen Corporation Piperazines as inhibitors of fructose-1,6-bisphosphatase (FBPase)
GB2372740A (en) 2001-01-17 2002-09-04 Xenova Ltd Diketopiperazines
GB0130677D0 (en) 2001-12-21 2002-02-06 Glaxo Group Ltd Medicaments and novel compounds
US20030229001A1 (en) 2002-01-31 2003-12-11 Pfizer Inc. Treatment of male sexual dysfunction
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
US9757424B2 (en) 2011-09-27 2017-09-12 Biomed Valley Discoveries, Inc. Compositions and methods of treating gliomas

Also Published As

Publication number Publication date
DE602004006268D1 (de) 2007-06-14
IS2463B (is) 2008-11-15
US20150105387A1 (en) 2015-04-16
JP5128126B2 (ja) 2013-01-23
US9452169B2 (en) 2016-09-27
EP1641787B1 (en) 2007-05-02
US8357685B2 (en) 2013-01-22
CN100404532C (zh) 2008-07-23
TWI340745B (en) 2011-04-21
HK1088910A1 (en) 2006-11-17
US20140058105A1 (en) 2014-02-27
NO20060383L (no) 2006-01-24
DK1641787T3 (da) 2007-09-17
JP2009513484A (ja) 2009-04-02
RU2343152C2 (ru) 2009-01-10
IL172529A (en) 2011-06-30
AU2004251868A1 (en) 2005-01-06
US8937179B2 (en) 2015-01-20
IS8248A (is) 2006-01-20
CN101597282A (zh) 2009-12-09
PT1641787E (pt) 2007-08-01
GB0314738D0 (en) 2003-07-30
WO2005000840A8 (en) 2005-05-19
AR044869A1 (es) 2005-10-05
KR101131378B1 (ko) 2012-04-04
WO2005000840A1 (en) 2005-01-06
EP1641787A1 (en) 2006-04-05
RU2006101859A (ru) 2006-06-10
US20160074413A1 (en) 2016-03-17
KR20060024440A (ko) 2006-03-16
ES2285474T3 (es) 2007-11-16
AU2004251868B2 (en) 2009-01-22
DE602004006268T2 (de) 2008-01-10
US20120004229A1 (en) 2012-01-05
CA2530310C (en) 2012-01-03
CN1812987A (zh) 2006-08-02
EG24929A (en) 2011-01-05
US8071594B2 (en) 2011-12-06
BRPI0411729A (pt) 2006-08-08
MY140653A (en) 2010-01-15
ATE361295T1 (de) 2007-05-15
NO332677B1 (no) 2012-12-03
CY1107703T1 (el) 2013-04-18
HRP20070286T3 (en) 2007-08-31
IL172529A0 (en) 2006-04-10
MA27887A1 (fr) 2006-05-02
TW200524917A (en) 2005-08-01
MXPA05014068A (es) 2006-03-02
US20070149524A1 (en) 2007-06-28
CA2530310A1 (en) 2005-01-06
NZ544006A (en) 2008-12-24
US20130102783A1 (en) 2013-04-25
PL1641787T3 (pl) 2007-08-31

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