AU2020211684A1 - Heterocyclic derivatives - Google Patents

Heterocyclic derivatives Download PDF

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Publication number
AU2020211684A1
AU2020211684A1 AU2020211684A AU2020211684A AU2020211684A1 AU 2020211684 A1 AU2020211684 A1 AU 2020211684A1 AU 2020211684 A AU2020211684 A AU 2020211684A AU 2020211684 A AU2020211684 A AU 2020211684A AU 2020211684 A1 AU2020211684 A1 AU 2020211684A1
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AU
Australia
Prior art keywords
denotes
compound
het
mmol
mixture
Prior art date
Legal status (The legal status 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 status listed.)
Abandoned
Application number
AU2020211684A
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English (en)
Other versions
AU2020211684A2 (en
Inventor
Timo Heinrich
Sarah SCHLESIGER
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Patent GmbH
Original Assignee
Merck Patent GmbH
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 Merck Patent GmbH filed Critical Merck Patent GmbH
Publication of AU2020211684A1 publication Critical patent/AU2020211684A1/en
Publication of AU2020211684A2 publication Critical patent/AU2020211684A2/en
Abandoned legal-status Critical Current

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Classifications

    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D407/00Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero 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
    • C07D417/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10Spiro-condensed systems
    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
AU2020211684A 2019-01-22 2020-01-20 Heterocyclic derivatives Abandoned AU2020211684A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP19152928 2019-01-22
EP19152928.8 2019-01-22
PCT/EP2020/051210 WO2020152067A1 (en) 2019-01-22 2020-01-20 Heterocyclic derivatives

Publications (2)

Publication Number Publication Date
AU2020211684A1 true AU2020211684A1 (en) 2021-09-09
AU2020211684A2 AU2020211684A2 (en) 2021-09-30

Family

ID=65199328

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2020211684A Abandoned AU2020211684A1 (en) 2019-01-22 2020-01-20 Heterocyclic derivatives

Country Status (14)

Country Link
US (1) US20220062258A1 (enExample)
EP (1) EP3914590B1 (enExample)
JP (1) JP2022521453A (enExample)
KR (1) KR20210118884A (enExample)
CN (1) CN113348168A (enExample)
AU (1) AU2020211684A1 (enExample)
BR (1) BR112021014220A2 (enExample)
CA (1) CA3127268A1 (enExample)
ES (1) ES2934986T3 (enExample)
IL (1) IL285025A (enExample)
MX (1) MX2021008712A (enExample)
SG (1) SG11202107893XA (enExample)
WO (1) WO2020152067A1 (enExample)
ZA (1) ZA202106024B (enExample)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021038419A1 (en) * 2019-08-23 2021-03-04 Insilico Medicine Ip Limited Kinase inhibitors and methods of synthesis and treatment
US12293809B2 (en) 2019-08-23 2025-05-06 Insilico Medicine Ip Limited Workflow for generating compounds with biological activity against a specific biological target
CA3213624A1 (en) * 2021-03-28 2022-10-06 Canwell Biotech Limited Metap-2 inhibitors, pharmaceutical compositions and therapeutic methods thereof
US20250032625A1 (en) 2021-11-02 2025-01-30 Merck Patent Gmbh Heterobifunctional molecules as tead inhibitors
WO2023144053A1 (en) 2022-01-26 2023-08-03 Merck Patent Gmbh Heterocyclic derivatives
CN116854604B (zh) * 2023-06-27 2026-03-24 中国科学院微生物研究所 一种ω-氨基脂肪酸甲酯、长链尼龙的制备方法
CN119569617A (zh) * 2025-02-07 2025-03-07 成都普康唯新生物科技有限公司 一种磷酸酯脂肪烷酸及其中间体的合成方法

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002020740A2 (en) 2000-09-08 2002-03-14 California Institute Of Technology Proteolysis targeting chimeric pharmaceutical
JP2010531896A (ja) * 2007-06-26 2010-09-30 チルドレンズ メディカル センター コーポレーション 治療的投与のためのMetAP−2阻害剤ポリマーソーム
DE102009005193A1 (de) * 2009-01-20 2010-07-22 Merck Patent Gmbh Neue heterocyclische Verbindungen als MetAP-2 Inhibitoren
DE102010048374A1 (de) * 2010-10-13 2012-04-19 Merck Patent Gmbh Pyrrolidinone als MetAP-2 Inhibitoren
DE102012006884A1 (de) * 2012-04-04 2013-10-10 Merck Patent Gmbh Cyclische Amide als MetAP-2 Inhibitoren
WO2014180524A1 (en) * 2013-05-06 2014-11-13 Merck Patent Gmbh Macrocycles as kinase inhibitors
US20180228907A1 (en) * 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
KR102485537B1 (ko) 2014-08-04 2023-01-05 메르크 파텐트 게엠베하 Metap-2 저해제로서의 피롤리디논 유도체
KR20180132861A (ko) * 2016-04-12 2018-12-12 더 리젠츠 오브 더 유니버시티 오브 미시간 Bet 단백질 분해제
GB201614134D0 (en) * 2016-08-18 2016-10-05 Glaxosmithkline Ip Dev Ltd Novel compounds
CN107540608B (zh) 2017-07-17 2021-10-19 大连理工大学 4-取代萘酰亚胺类化合物及其应用

Also Published As

Publication number Publication date
MX2021008712A (es) 2021-08-19
AU2020211684A2 (en) 2021-09-30
SG11202107893XA (en) 2021-08-30
ES2934986T3 (es) 2023-02-28
ZA202106024B (en) 2023-03-29
CA3127268A1 (en) 2020-07-30
KR20210118884A (ko) 2021-10-01
JP2022521453A (ja) 2022-04-08
EP3914590B1 (en) 2022-09-28
WO2020152067A1 (en) 2020-07-30
EP3914590A1 (en) 2021-12-01
IL285025A (en) 2021-09-30
CN113348168A (zh) 2021-09-03
US20220062258A1 (en) 2022-03-03
BR112021014220A2 (pt) 2022-01-18

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Legal Events

Date Code Title Description
DA3 Amendments made section 104

Free format text: THE NATURE OF THE AMENDMENT IS AS SHOWN IN THE STATEMENT FILED 16 AUG 2021

MK1 Application lapsed section 142(2)(a) - no request for examination in relevant period