TWI340745B - Novel diketopiperazine derivatives and the processes for preparation thereof - Google Patents

Novel diketopiperazine derivatives and the processes for preparation thereof

Info

Publication number
TWI340745B
TWI340745B TW093118010A TW93118010A TWI340745B TW I340745 B TWI340745 B TW I340745B TW 093118010 A TW093118010 A TW 093118010A TW 93118010 A TW93118010 A TW 93118010A TW I340745 B TWI340745 B TW I340745B
Authority
TW
Taiwan
Prior art keywords
processes
preparation
diketopiperazine derivatives
novel
novel diketopiperazine
Prior art date
Application number
TW093118010A
Other languages
English (en)
Other versions
TW200524917A (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 TW200524917A publication Critical patent/TW200524917A/zh
Application granted granted Critical
Publication of TWI340745B publication Critical patent/TWI340745B/zh

Links

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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/10—Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/10—Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH
    • A61P5/12—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/36—Antigestagens
    • 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
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/06—Heterocyclic 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
    • C07D241/08—Heterocyclic 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
    • 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)
  • 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)
  • Reproductive Health (AREA)
  • Neurosurgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Obesity (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Child & Adolescent Psychology (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
TW093118010A 2003-06-24 2004-06-23 Novel diketopiperazine derivatives and the processes for preparation thereof TWI340745B (en)

Applications Claiming Priority (1)

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

Publications (2)

Publication Number Publication Date
TW200524917A TW200524917A (en) 2005-08-01
TWI340745B true TWI340745B (en) 2011-04-21

Family

ID=27637257

Family Applications (1)

Application Number Title Priority Date Filing Date
TW093118010A TWI340745B (en) 2003-06-24 2004-06-23 Novel diketopiperazine derivatives and the processes for preparation thereof

Country Status (31)

Country Link
US (6) US8071594B2 (zh)
EP (1) EP1641787B1 (zh)
JP (1) JP5128126B2 (zh)
KR (1) KR101131378B1 (zh)
CN (2) CN100404532C (zh)
AR (1) AR044869A1 (zh)
AT (1) ATE361295T1 (zh)
AU (1) AU2004251868B2 (zh)
BR (1) BRPI0411729A (zh)
CA (1) CA2530310C (zh)
CY (1) CY1107703T1 (zh)
DE (1) DE602004006268T2 (zh)
DK (1) DK1641787T3 (zh)
EG (1) EG24929A (zh)
ES (1) ES2285474T3 (zh)
GB (1) GB0314738D0 (zh)
HK (1) HK1088910A1 (zh)
HR (1) HRP20070286T3 (zh)
IL (1) IL172529A (zh)
IS (1) IS2463B (zh)
MA (1) MA27887A1 (zh)
MX (1) MXPA05014068A (zh)
MY (1) MY140653A (zh)
NO (1) NO332677B1 (zh)
NZ (1) NZ544006A (zh)
PL (1) PL1641787T3 (zh)
PT (1) PT1641787E (zh)
RU (1) RU2343152C2 (zh)
TW (1) TWI340745B (zh)
WO (1) WO2005000840A1 (zh)
ZA (1) ZA200509890B (zh)

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
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
CN106999497A (zh) 2014-06-16 2017-08-01 葛兰素史密斯克莱知识产权发展有限公司 用于治疗早产的瑞托西班
AU2017205254B2 (en) 2016-01-04 2021-05-20 Xoma (Us) Lcc Alpha-amino esters of hydroxypropylthiazolidine carboxamide derivative and salt form, crystal polymorph thereof
MA52548A (fr) 2016-07-21 2021-05-26 ObsEva SA Régimes posologiques d'antagonistes de l'ocytocine pour favoriser l'implantation d'embryons et prévenir les fausses couches
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
KR20220075340A (ko) 2019-09-03 2022-06-08 옵스에파 에스에이 배아 착상을 촉진하고 유산을 예방하기 위한 옥시토신 길항제 투여 요법
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 (20)

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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
US5968938A (en) * 1997-06-18 1999-10-19 Merck & Co., Inc. Piperazine oxytocin receptor antagonists
GB2326639A (en) 1997-06-18 1998-12-30 Merck & Co Inc Piperazine Oxytocin Receptor Antagonists
AU745425B2 (en) 1998-01-27 2002-03-21 Aventis Pharmaceuticals Inc. Substituted oxoazaheterocyclyl factor Xa inhibitors
SK10642000A3 (sk) 1998-01-29 2001-07-10 Aventis Pharmaceuticals Products Inc. Spôsob prípravy n-[(alifatickej alebo aromatickej)karbonyl)]-2- aminoacetamidovej zlúčeniny a cyklizovanej formy tejto zlúčeniny
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
EP2760473A1 (en) 2011-09-27 2014-08-06 Biomed Valley Discoveries, Inc. Compositions and methods of treating gliomas

Also Published As

Publication number Publication date
CY1107703T1 (el) 2013-04-18
MA27887A1 (fr) 2006-05-02
MY140653A (en) 2010-01-15
RU2006101859A (ru) 2006-06-10
CN101597282A (zh) 2009-12-09
NO20060383L (no) 2006-01-24
WO2005000840A1 (en) 2005-01-06
IL172529A0 (en) 2006-04-10
IS8248A (is) 2006-01-20
CN1812987A (zh) 2006-08-02
AR044869A1 (es) 2005-10-05
NZ544006A (en) 2008-12-24
US20160074413A1 (en) 2016-03-17
US20070149524A1 (en) 2007-06-28
ES2285474T3 (es) 2007-11-16
HRP20070286T3 (en) 2007-08-31
CA2530310A1 (en) 2005-01-06
US8357685B2 (en) 2013-01-22
JP2009513484A (ja) 2009-04-02
DE602004006268D1 (de) 2007-06-14
NO332677B1 (no) 2012-12-03
CA2530310C (en) 2012-01-03
GB0314738D0 (en) 2003-07-30
TW200524917A (en) 2005-08-01
ATE361295T1 (de) 2007-05-15
KR20060024440A (ko) 2006-03-16
US8937179B2 (en) 2015-01-20
US9452169B2 (en) 2016-09-27
AU2004251868A1 (en) 2005-01-06
US20150105387A1 (en) 2015-04-16
DK1641787T3 (da) 2007-09-17
EP1641787B1 (en) 2007-05-02
HK1088910A1 (en) 2006-11-17
EP1641787A1 (en) 2006-04-05
MXPA05014068A (es) 2006-03-02
JP5128126B2 (ja) 2013-01-23
US20130102783A1 (en) 2013-04-25
ZA200509890B (en) 2006-07-26
BRPI0411729A (pt) 2006-08-08
US8071594B2 (en) 2011-12-06
KR101131378B1 (ko) 2012-04-04
US20120004229A1 (en) 2012-01-05
PL1641787T3 (pl) 2007-08-31
WO2005000840A8 (en) 2005-05-19
CN100404532C (zh) 2008-07-23
US20140058105A1 (en) 2014-02-27
RU2343152C2 (ru) 2009-01-10
DE602004006268T2 (de) 2008-01-10
IS2463B (is) 2008-11-15
IL172529A (en) 2011-06-30
EG24929A (en) 2011-01-05
AU2004251868B2 (en) 2009-01-22
PT1641787E (pt) 2007-08-01

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MM4A Annulment or lapse of patent due to non-payment of fees