CN113348168A - 杂环衍生物 - Google Patents

杂环衍生物 Download PDF

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Publication number
CN113348168A
CN113348168A CN202080010269.1A CN202080010269A CN113348168A CN 113348168 A CN113348168 A CN 113348168A CN 202080010269 A CN202080010269 A CN 202080010269A CN 113348168 A CN113348168 A CN 113348168A
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CN
China
Prior art keywords
compound
mixture
het
nmr
pharmaceutically acceptable
Prior art date
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Pending
Application number
CN202080010269.1A
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English (en)
Chinese (zh)
Inventor
蒂莫·海因里希
莎拉·沃罗德
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Merck Patent GmbH
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Merck Patent GmbH
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Publication of CN113348168A publication Critical patent/CN113348168A/zh
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    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non 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
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non 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
    • 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
    • A61P17/00—Drugs for dermatological 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
    • A61P27/00—Drugs for disorders of the senses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic 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
    • C07D407/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/10—Spiro-condensed systems
    • 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
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • 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)
CN202080010269.1A 2019-01-22 2020-01-20 杂环衍生物 Pending CN113348168A (zh)

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 (1)

Publication Number Publication Date
CN113348168A true CN113348168A (zh) 2021-09-03

Family

ID=65199328

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202080010269.1A Pending CN113348168A (zh) 2019-01-22 2020-01-20 杂环衍生物

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)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116854604A (zh) * 2023-06-27 2023-10-10 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

Families Citing this family (5)

* 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

Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20020068063A1 (en) * 2000-09-08 2002-06-06 Deshaies Raymond J. Proteolysis targeting chimeric pharmaceutical
US20110281859A1 (en) * 2009-01-20 2011-11-17 Merck Patent Gesellschaft Mit Beschrankter Haftung Novel heterocyclic compounds as metap-2 inhibitors
WO2012048775A1 (de) * 2010-10-13 2012-04-19 Merck Patent Gmbh Pyrrolidinone als metap-2 inhibitoren
WO2013149704A1 (de) * 2012-04-04 2013-10-10 Merck Patent Gmbh Cyclische amide als metap-2 inhibitoren
WO2016020031A1 (en) * 2014-08-04 2016-02-11 Merck Patent Gmbh Pyrrolidinone derivatives as metap-2 inhibitors
EP2994471A1 (en) * 2013-05-06 2016-03-16 Merck Patent GmbH Macrocycles as kinase inhibitors
CN107540608A (zh) * 2017-07-17 2018-01-05 大连理工大学 4‑取代萘酰亚胺类化合物及其应用
WO2018033556A1 (en) * 2016-08-18 2018-02-22 Glaxosmithkline Intellectual Property Development Limited Novel compounds
US20180228907A1 (en) * 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
KR20180132861A (ko) * 2016-04-12 2018-12-12 더 리젠츠 오브 더 유니버시티 오브 미시간 Bet 단백질 분해제

Patent Citations (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20020068063A1 (en) * 2000-09-08 2002-06-06 Deshaies Raymond J. Proteolysis targeting chimeric pharmaceutical
US20110281859A1 (en) * 2009-01-20 2011-11-17 Merck Patent Gesellschaft Mit Beschrankter Haftung Novel heterocyclic compounds as metap-2 inhibitors
CN102292339A (zh) * 2009-01-20 2011-12-21 默克专利有限公司 作为MetAP-2抑制剂的新杂环化合物
WO2012048775A1 (de) * 2010-10-13 2012-04-19 Merck Patent Gmbh Pyrrolidinone als metap-2 inhibitoren
US20130296274A1 (en) * 2010-10-13 2013-11-07 Merck Patent Gmbh Pyrrolidinones as metap-2 inhibitors
WO2013149704A1 (de) * 2012-04-04 2013-10-10 Merck Patent Gmbh Cyclische amide als metap-2 inhibitoren
CN104245675A (zh) * 2012-04-04 2014-12-24 默克专利股份公司 作为MetAP-2抑制剂的环酰胺
EP2994471A1 (en) * 2013-05-06 2016-03-16 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
WO2016020031A1 (en) * 2014-08-04 2016-02-11 Merck Patent Gmbh Pyrrolidinone derivatives as metap-2 inhibitors
WO2018033556A1 (en) * 2016-08-18 2018-02-22 Glaxosmithkline Intellectual Property Development Limited Novel compounds
CN107540608A (zh) * 2017-07-17 2018-01-05 大连理工大学 4‑取代萘酰亚胺类化合物及其应用

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
PHILIPP OTTIS等: "Proteolysis-Targeting Chimeras: Induced Protein Degradation as a Therapeutic Strategy", ACS CHEM. BIOL., vol. 12, pages 892 - 898, XP055819452, DOI: 10.1021/acschembio.6b01068 *

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116854604A (zh) * 2023-06-27 2023-10-10 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
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

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
AU2020211684A1 (en) 2021-09-09
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
US20220062258A1 (en) 2022-03-03
BR112021014220A2 (pt) 2022-01-18

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