CN110770214B - 杂环p2x7拮抗剂 - Google Patents

杂环p2x7拮抗剂 Download PDF

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Publication number
CN110770214B
CN110770214B CN201880027662.4A CN201880027662A CN110770214B CN 110770214 B CN110770214 B CN 110770214B CN 201880027662 A CN201880027662 A CN 201880027662A CN 110770214 B CN110770214 B CN 110770214B
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Prior art keywords
diazole
ones
dihydro
methyl
fluorophenyl
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Chinese (zh)
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CN110770214A (zh
Inventor
P·佩瓦雷洛
M·索达诺
E·塞维里
R·维他酮
R·托马斯
V·库萨诺
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Breyer Therapy Co ltd
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Breyer Therapy Co ltd
AXXAM SpA
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/06—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
    • C07D271/07—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
    • 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
    • A61K31/4245—Oxadiazoles
    • 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
    • A61K31/41—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
    • A61K31/433—Thidiazoles
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4365—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine 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
    • A61K31/535—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
    • A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring 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
    • 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
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • 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
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/08—1,2,4-Thiadiazoles; Hydrogenated 1,2,4-thiadiazoles
    • 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
    • C07D413/02—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
    • C07D413/10—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 aromatic 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
    • C07D417/02—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 two hetero rings
    • C07D417/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (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)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
CN201880027662.4A 2017-05-03 2018-05-02 杂环p2x7拮抗剂 Active CN110770214B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP17169277.5 2017-05-03
EP17169277.5A EP3398941A1 (en) 2017-05-03 2017-05-03 Heterocyclic p2x7 antagonists
PCT/EP2018/061180 WO2018202694A1 (en) 2017-05-03 2018-05-02 Heterocyclic p2x7 antagonists

Publications (2)

Publication Number Publication Date
CN110770214A CN110770214A (zh) 2020-02-07
CN110770214B true CN110770214B (zh) 2024-03-29

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US (1) US11623919B2 (enExample)
EP (2) EP3398941A1 (enExample)
JP (1) JP7227916B2 (enExample)
CN (1) CN110770214B (enExample)
CA (1) CA3059525A1 (enExample)
DK (1) DK3619200T3 (enExample)
ES (1) ES2911049T3 (enExample)
IL (1) IL270275B2 (enExample)
RU (1) RU2768865C2 (enExample)
WO (1) WO2018202694A1 (enExample)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116782901A (zh) 2020-11-30 2023-09-19 旭化成制药株式会社 用于使神经病理性疼痛缓和的药物
US20240368092A1 (en) 2021-09-03 2024-11-07 Breye Therapeutics Aps 2,4-Dihydro-3H-1,2,4-Triazol-3-One P2X7 Antagonists
WO2025057074A1 (en) 2023-09-13 2025-03-20 Suven Life Sciences Limited N-aryl benzamide derivatives as p2x7 receptor antagonists
WO2026041663A1 (en) 2024-08-22 2026-02-26 Breye Therapeutics Aps P2x7 receptor antagonists

Citations (5)

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JPS61106575A (ja) * 1984-10-31 1986-05-24 Nippon Soda Co Ltd １，２，４−チアジアゾ−ル−５−オン誘導体及び製造方法
US5066662A (en) * 1990-05-21 1991-11-19 Warner-Lambert Company Substituted oxazolidin-2-ones and 1,2,4-oxadiazolin-5-ones and derivatives thereof acting at muscarinic receptors
CN1419539A (zh) * 2000-03-24 2003-05-21 法马西亚公司 用作一氧化氮合酶抑制剂的脒基化合物及其盐
CN1474804A (zh) * 2000-09-15 2004-02-11 2-氨基-2-烷基-4-己烯酸和己炔酸衍生物用作氧化氮合酶抑制剂
PL389815A1 (pl) * 2009-12-08 2011-06-20 Uniwersytet Medyczny W Lublinie Nowe zastosowanie pochodnych semikarbazydowych oraz 1, 2, 4-triazolino-5-onu posiadających układ 1-metylopirolu

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FR1529621A (fr) * 1967-01-17 1968-06-21 Dausse Lab Nouvelles oxadiazolinones basiques et leur procédé de préparation
FR1529700A (fr) * 1967-04-11 1968-06-21 Dausse Sa Lab Tertioaminoalcoyl oxadiazolinones et leur procédé de préparation
FR1575552A (enExample) * 1967-12-07 1969-07-25
GB1508210A (en) 1975-12-22 1978-04-19 Labaz Benzofuran-derived amidoximes and process for preparing the same
AR034120A1 (es) 2000-04-13 2004-02-04 Pharmacia Corp Compuesto derivado halogenado del acido 2-amino-4,5 heptenoico, composicion farmaceutica que lo comprende y el uso de dicho compuesto y dicha composicion en la fabricacion de un medicamento para inhibir o modular la sintesis de acido nitrico
TWI290130B (en) 2000-09-15 2007-11-21 Pharmacia Corp 2-Amino-2alkyl-5 heptenoic and heptynoic acid derivatives useful as nitric oxide synthase inhibitors
ES2281801T3 (es) 2003-05-12 2007-10-01 Pfizer Products Inc. Inhibidores benzamida del receptor p2x7.
GB0312609D0 (en) 2003-06-02 2003-07-09 Astrazeneca Ab Novel compounds
EP2215086B1 (en) * 2007-11-20 2011-08-24 Sumitomo Chemical Company, Limited Pyridine compound, pesticidal composition and method of controlling pest
KR100967889B1 (ko) * 2008-02-01 2010-07-06 한국화학연구원 2-이미노벤조이미다졸 유도체를 포함하는 살균제 조성물
WO2009108551A2 (en) 2008-02-25 2009-09-03 H. Lundbeck A/S Heteroaryl amide analogues
KR101598397B1 (ko) 2008-04-22 2016-02-29 얀센 파마슈티카 엔.브이. 퀴놀린 또는 이소퀴놀린 치환된 피2엑스7 안타고니스트
JP2012041325A (ja) * 2010-08-23 2012-03-01 Bayer Cropscience Ag オキサジアゾリノン誘導体およびその有害生物の防除用途
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JP6285736B2 (ja) 2014-02-04 2018-02-28 株式会社ソニー・インタラクティブエンタテインメント 情報処理装置および入力デバイスの割当方法

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS61106575A (ja) * 1984-10-31 1986-05-24 Nippon Soda Co Ltd １，２，４−チアジアゾ−ル−５−オン誘導体及び製造方法
US5066662A (en) * 1990-05-21 1991-11-19 Warner-Lambert Company Substituted oxazolidin-2-ones and 1,2,4-oxadiazolin-5-ones and derivatives thereof acting at muscarinic receptors
CN1419539A (zh) * 2000-03-24 2003-05-21 法马西亚公司 用作一氧化氮合酶抑制剂的脒基化合物及其盐
CN1474804A (zh) * 2000-09-15 2004-02-11 2-氨基-2-烷基-4-己烯酸和己炔酸衍生物用作氧化氮合酶抑制剂
PL389815A1 (pl) * 2009-12-08 2011-06-20 Uniwersytet Medyczny W Lublinie Nowe zastosowanie pochodnych semikarbazydowych oraz 1, 2, 4-triazolino-5-onu posiadających układ 1-metylopirolu

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Title
Beitrage zur Chemie von 1.2.4-Oxadiazolen mit C-5 -Heteroatom-Bindung, I;KCilmCin TakCics 等;《Chem. Ber.》;19701231;第2332页化合物4i，第2335页第2段 *
Unexpected C-C Bond Cleavage: Synthesis of 1,2,4-Oxadiazol-5-ones f rom A midoximes with Pentafluorophenyl o r T rifluoromethyl Anion Acting as Leaving Group;Thibaud Gerfaud 等;《ORGANIC LETTERS》;20111231;表2 *

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EP3619200B1 (en) 2022-03-09
EP3619200A1 (en) 2020-03-11
IL270275A (enExample) 2019-12-31
ES2911049T3 (es) 2022-05-17
RU2768865C2 (ru) 2022-03-25
US11623919B2 (en) 2023-04-11
CN110770214A (zh) 2020-02-07
CA3059525A1 (en) 2018-11-08
EP3398941A1 (en) 2018-11-07
WO2018202694A1 (en) 2018-11-08
JP2020518555A (ja) 2020-06-25
DK3619200T3 (da) 2022-04-04
JP7227916B2 (ja) 2023-02-22
IL270275B2 (en) 2023-07-01
RU2019134453A (ru) 2021-06-03
US20200055831A1 (en) 2020-02-20
IL270275B1 (en) 2023-03-01

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