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MX367774B - N-ACIL-5,6,7, (8-SUSTITUIDO)-TETRAHIDRO- [1,2,4] TRIAZOLO [4,3-a] PIRAZINAS QUIRALES, NOVEDOSAS, COMO ANTAGONISTAS SELECTIVOS DE RECEPTOR DE NK-3; COMPOSICIÓN FARMACÉUTICA, MÉTODOS PARA USO EN TRASTORNOS MEDIADOS POR RECEPTOR DE NK-3 Y SU SÍNTESIS QUIRAL. - Google Patents

N-ACIL-5,6,7, (8-SUSTITUIDO)-TETRAHIDRO- [1,2,4] TRIAZOLO [4,3-a] PIRAZINAS QUIRALES, NOVEDOSAS, COMO ANTAGONISTAS SELECTIVOS DE RECEPTOR DE NK-3; COMPOSICIÓN FARMACÉUTICA, MÉTODOS PARA USO EN TRASTORNOS MEDIADOS POR RECEPTOR DE NK-3 Y SU SÍNTESIS QUIRAL.

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Publication number
MX367774B
MX367774B MX2014004057A MX2014004057A MX367774B MX 367774 B MX367774 B MX 367774B MX 2014004057 A MX2014004057 A MX 2014004057A MX 2014004057 A MX2014004057 A MX 2014004057A MX 367774 B MX367774 B MX 367774B
Authority
MX
Mexico
Prior art keywords
chiral
pyrazines
tetrahydro
substituted
acyl
Prior art date
Application number
MX2014004057A
Other languages
English (en)
Other versions
MX2014004057A (es
Inventor
Hoveyda Hamid
Dutheuil Guillaume
Fraser Graeme
Roy Marie-Odile
El Bousmaqui Mohamed
Batt Frédéric
Original Assignee
Ogeda S A
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 Ogeda S A filed Critical Ogeda S A
Publication of MX2014004057A publication Critical patent/MX2014004057A/es
Publication of MX367774B publication Critical patent/MX367774B/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/14—Antitussive agents
    • 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
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    • 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
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    • 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
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
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    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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    • A—HUMAN NECESSITIES
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    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
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    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/26—Androgens
    • 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
    • A61P5/28—Antiandrogens
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    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
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    • 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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
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  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
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  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Gynecology & Obstetrics (AREA)
  • Oncology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Rheumatology (AREA)
  • Emergency Medicine (AREA)
  • Otolaryngology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La presente invención se refiere a compuestos novedosos de la fórmula I: (ver Fórmula) y su uso en tratamientos terapéuticos. La invención se refiere además a una síntesis quiral novedosa de 5,6,7, (8- sustituido)-tetrahidro-[1,2,4]triazolo[4,3-a]pirazinas usando grupos protectores N-sp3. La invención provee también intermediarios para uso en la síntesis de compuestos de la fórmula I.
MX2014004057A 2011-10-03 2012-10-03 N-ACIL-5,6,7, (8-SUSTITUIDO)-TETRAHIDRO- [1,2,4] TRIAZOLO [4,3-a] PIRAZINAS QUIRALES, NOVEDOSAS, COMO ANTAGONISTAS SELECTIVOS DE RECEPTOR DE NK-3; COMPOSICIÓN FARMACÉUTICA, MÉTODOS PARA USO EN TRASTORNOS MEDIADOS POR RECEPTOR DE NK-3 Y SU SÍNTESIS QUIRAL. MX367774B (es)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
EP11183678 2011-10-03
EP11183679 2011-10-03
EP11183681 2011-10-03
EP11183692 2011-10-03
US201161543611P 2011-10-05 2011-10-05
PCT/EP2012/069546 WO2013050424A1 (en) 2011-10-03 2012-10-03 NOVEL CHIRAL N-ACYL-5,6,7,(8-SUBSTITUTED)-TETRAHYDRO-[1,2,4]TRIAZOLO[4,3-a]PYRAZINES AS SELECTIVE NK-3 RECEPTOR ANTAGONISTS, PHARMACEUTICAL COMPOSITION, METHODS FOR USE IN NK-3 RECEPTOR MEDIATED DISORDERS AND CHIRAL SYNTHESIS THEREOF

Publications (2)

Publication Number Publication Date
MX2014004057A MX2014004057A (es) 2014-08-22
MX367774B true MX367774B (es) 2019-09-04

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Family Applications (1)

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MX2014004057A MX367774B (es) 2011-10-03 2012-10-03 N-ACIL-5,6,7, (8-SUSTITUIDO)-TETRAHIDRO- [1,2,4] TRIAZOLO [4,3-a] PIRAZINAS QUIRALES, NOVEDOSAS, COMO ANTAGONISTAS SELECTIVOS DE RECEPTOR DE NK-3; COMPOSICIÓN FARMACÉUTICA, MÉTODOS PARA USO EN TRASTORNOS MEDIADOS POR RECEPTOR DE NK-3 Y SU SÍNTESIS QUIRAL.

Country Status (20)

Country Link
US (4) US9475814B2 (es)
EP (2) EP3029042A1 (es)
JP (2) JP6023814B2 (es)
KR (1) KR102049534B1 (es)
CN (2) CN103906750B9 (es)
AU (1) AU2012320568C1 (es)
BR (1) BR112014007652B1 (es)
CA (1) CA2849751C (es)
CY (1) CY1117773T1 (es)
DK (1) DK2763992T3 (es)
EA (2) EA029340B1 (es)
ES (1) ES2572604T3 (es)
HR (1) HRP20160396T1 (es)
HU (1) HUE028858T2 (es)
MX (1) MX367774B (es)
PL (1) PL2763992T3 (es)
RS (1) RS54833B1 (es)
SI (1) SI2763992T1 (es)
SM (1) SMT201600164B (es)
WO (1) WO2013050424A1 (es)

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* Cited by examiner, † Cited by third party
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EP3176171A1 (en) 2010-04-02 2017-06-07 Ogeda Sa Novel nk-3 receptor selective antagonist compounds, pharmaceutical composition and methods for use in nk-3 receptors mediated disorders
US10065960B2 (en) 2010-04-02 2018-09-04 Ogeda Sa NK-3 receptor selective antagonist compounds, pharmaceutical composition and methods for use in NK-3 receptors mediated disorders
AU2012320568C1 (en) 2011-10-03 2018-07-19 Ogeda S.A. Novel chiral N-acyl-5,6,7,(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines as selective NK-3 receptor antagonists, pharmaceutical composition, methods for use in NK-3 receptor mediated disorders and chiral synthesis thereof
PL2948455T3 (pl) 2013-03-29 2018-01-31 Ogeda S A N-acyl-(3-podstawiony)-(8-podstawiony)-5,6-dihydro- [1,2,4]triazolo[4,3-a]pyrazyny jako wybrani antagoniści receptora nk-3, kompozycja farmaceutyczna, sposoby używania w zakresie zaburzeń receptora nk-3
AU2014242908B2 (en) 2013-03-29 2018-07-19 Ogeda Sa Novel N-acyl-(3-substituted)-(8-methyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazines as selective NK-3 receptor antagonists, pharmaceutical composition, methods for use in NK-3 receptor-mediated disorders
WO2014154896A1 (en) 2013-03-29 2014-10-02 Euroscreen Sa NOVEL N-ACYL-(3-SUBSTITUTED)-5,6,7,8-TETRAHYDRO-[1,2,4]TRIAZOLO[4,3-a]PYRAZINES AS SELECTIVE NK-3 RECEPTOR ANTAGONISTS, PHARMACEUTICAL COMPOSITION, METHODS FOR USE IN NK-3 RECEPTOR-MEDIATED DISORDERS
US10183948B2 (en) 2013-03-29 2019-01-22 Ogeda Sa N-acyl-(3-substituted)-(8-substituted)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazines as selective NK-3 receptor antagonists
GB201315846D0 (en) 2013-09-05 2013-10-23 Imp Innovations Ltd Method for treating or preventing hot flushes
PT3197876T (pt) * 2014-09-25 2019-02-21 Ogeda Sa Nova síntese quiral de n-acyl-(3-substituído)-(8-substituído)-5,6-di-hidro-[1,2,4]triazolo[4,3-a]pirazinas
RS65039B1 (sr) 2015-03-16 2024-02-29 Ogeda N V Antagonisti nk-3 receptora za terapijski ili kozmetički tretman viška telesne masti
JP2021014404A (ja) * 2017-10-13 2021-02-12 アステラス製薬株式会社 トリアゾロピラジン誘導体の塩及び結晶
CA3123757A1 (en) 2018-12-21 2020-06-25 Ogeda Sa Synthesis of 3-methyl-1,2,4-thiadiazole-5-carbohydrazide or of the methyl-d3 deuterated form thereof
CN111499640A (zh) * 2019-01-31 2020-08-07 上海医药工业研究院 哌嗪并三唑类衍生物的手性拆分方法
WO2020211798A1 (zh) * 2019-04-16 2020-10-22 上海翰森生物医药科技有限公司 含二并环类衍生物抑制剂、其制备方法和应用
KR20220075386A (ko) * 2019-09-30 2022-06-08 얀센 파마슈티카 엔.브이. 방사성 표지된 mgl pet 리간드
CN113527307B (zh) * 2020-04-20 2024-10-11 上海翰森生物医药科技有限公司 含三唑基的并环类衍生物抑制剂、其制备方法和应用
CN113549074A (zh) * 2020-04-26 2021-10-26 上海翰森生物医药科技有限公司 含三唑基的并环类衍生物抑制剂、其制备方法和应用
AU2021317809A1 (en) * 2020-07-30 2023-02-16 Jiangsu Hansoh Pharmaceutical Group Co., Ltd. Nitrogen-containing fused ring derivative inhibitor, preparation method therefor and use thereof
CN117177974A (zh) * 2021-04-21 2023-12-05 长春金赛药业有限责任公司 含咪唑稠环类衍生物、其制备方法及其在医药上的应用
WO2024188143A1 (zh) * 2023-03-10 2024-09-19 山东绿叶制药有限公司 Nk-3受体拮抗剂化合物、药物组合物、其制备方法和应用
WO2025009477A1 (ja) * 2023-07-03 2025-01-09 Ａｇｃ株式会社 ３－メチル－１，２，４－チアジアゾール－５－カルボヒドラジドの新規製造方法
TW202508570A (zh) * 2023-07-03 2025-03-01 日商Ａｇｃ股份有限公司 3-甲基-1,2,4-噻二唑-5-卡肼之新穎製造方法
CN118290429B (zh) * 2024-06-06 2024-10-11 山东百诺医药股份有限公司 非唑奈坦中间体及非唑奈坦的制备方法
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