AU2020288559C1 - Pyrazole and imidazole derivatives, compositions and methods as orexin antagonists - Google Patents

Pyrazole and imidazole derivatives, compositions and methods as orexin antagonists

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Publication number
AU2020288559C1
AU2020288559C1 AU2020288559A AU2020288559A AU2020288559C1 AU 2020288559 C1 AU2020288559 C1 AU 2020288559C1 AU 2020288559 A AU2020288559 A AU 2020288559A AU 2020288559 A AU2020288559 A AU 2020288559A AU 2020288559 C1 AU2020288559 C1 AU 2020288559C1
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AU
Australia
Prior art keywords
alkyl
compound
iii
substituted
group
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.)
Expired - Fee Related
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AU2020288559A
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English (en)
Other versions
AU2020288559B2 (en
AU2020288559A1 (en
AU2020288559A8 (en
Inventor
Belew Mekonnen
Hemantbhai Patel
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.)
Hager Biosciences LLC
Original Assignee
Hager Biosciences LLC
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 Hager Biosciences LLC filed Critical Hager Biosciences LLC
Publication of AU2020288559A1 publication Critical patent/AU2020288559A1/en
Publication of AU2020288559A8 publication Critical patent/AU2020288559A8/en
Publication of AU2020288559B2 publication Critical patent/AU2020288559B2/en
Application granted granted Critical
Publication of AU2020288559C1 publication Critical patent/AU2020288559C1/en
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

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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
    • A61K31/435—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
    • A61K31/437—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 containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim 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
    • A61K31/535—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
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • 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
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
AU2020288559A 2019-06-04 2020-06-03 Pyrazole and imidazole derivatives, compositions and methods as orexin antagonists Expired - Fee Related AU2020288559C1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962856822P 2019-06-04 2019-06-04
US62/856,822 2019-06-04
PCT/US2020/035851 WO2020247447A1 (en) 2019-06-04 2020-06-03 Pyrazole and imidazole derivatives, compositions and methods as orexin antagonists

Publications (4)

Publication Number Publication Date
AU2020288559A1 AU2020288559A1 (en) 2022-01-20
AU2020288559A8 AU2020288559A8 (en) 2022-02-03
AU2020288559B2 AU2020288559B2 (en) 2025-04-17
AU2020288559C1 true AU2020288559C1 (en) 2025-07-24

Family

ID=73651984

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2020288559A Expired - Fee Related AU2020288559C1 (en) 2019-06-04 2020-06-03 Pyrazole and imidazole derivatives, compositions and methods as orexin antagonists

Country Status (9)

Country Link
US (2) US20220315602A1 (enExample)
EP (1) EP3972587A4 (enExample)
JP (1) JP7837120B2 (enExample)
KR (1) KR20220016919A (enExample)
CN (1) CN114340616A (enExample)
AU (1) AU2020288559C1 (enExample)
CA (1) CA3140173A1 (enExample)
SG (1) SG11202112828SA (enExample)
WO (1) WO2020247447A1 (enExample)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2022534704A (ja) 2019-06-04 2022-08-03 ヘイガー バイオサイエンシズ，エルエルシー オレキシンアンタゴニストとしてのイミダゾロ誘導体、組成物、及び方法
KR20220119653A (ko) 2019-12-20 2022-08-30 테나야 테라퓨틱스, 인코포레이티드 플루오로알킬-옥사디아졸 및 이의 용도
US20240252502A1 (en) 2021-05-04 2024-08-01 Tenaya Therapeutics, Inc. Hdac6 inhibitors for treatment of metabolic disease and hfpef
JP2025530768A (ja) * 2022-09-01 2025-09-17 ヘイガー バイオサイエンシズ，エルエルシー 神経疾患および精神疾患の治療のための、オレキシン受容体およびカッパオピオイド受容体に対する二重調節剤としてのピラゾール誘導体およびイミダゾール誘導体、組成物、ならびに治療法
EP4471034A4 (en) * 2022-11-23 2025-06-18 Jiangsu NHWA Pharmaceutical Co., Ltd DISUBSTITUTED OCTAHYDROPYRROLO[3,4-C PYRROL METHYL KETONE DERIVATIVE AND ITS USE
GB202311281D0 (en) 2023-07-21 2023-09-06 Bial Portela & Ca Sa Orexin receptor antagonists
GB202311280D0 (en) 2023-07-21 2023-09-06 Bial Portela & Ca Sa Orexin receptor antagonists
CN117169393B (zh) * 2023-11-03 2024-03-19 杭州湃肽生化科技有限公司 一种植物组织中环肽的检测方法

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20060135447A1 (en) * 2004-12-21 2006-06-22 Chupak Louis S Macrolides
WO2013062858A1 (en) * 2011-10-25 2013-05-02 Merck Sharp & Dohme Corp. Isoxazolopyridine orexin receptor antagonists
US20130217727A1 (en) * 2010-10-21 2013-08-22 Jurgen Benting 1-(heterocyclic carbonyl)-2-substituted pyrrolidines
EP2730573A1 (en) * 2011-07-05 2014-05-14 Taisho Pharmaceutical Co., Ltd. Methylpiperidine derivative
US20180222896A1 (en) * 2014-08-26 2018-08-09 Takeda Pharmaceutical Company Limited Heterocyclic compound

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4925849A (en) * 1987-06-15 1990-05-15 Fujisawa Pharmaceutical Company, Ltd. Pharmaceutically useful pyrazolopyridines
AR067665A1 (es) * 2007-07-27 2009-10-21 Actelion Pharmaceuticals Ltd Derivados de trans-3- aza-biciclo ( 3.1.0) hexano
JP6346862B2 (ja) * 2012-02-07 2018-06-20 エオラス セラピューティクス， インコーポレイテッド オレキシンレセプターアンタゴニストとしての置換プロリン／ピペリジン
MA53721A (fr) * 2018-09-28 2021-09-15 Janssen Pharmaceutica Nv Modulateurs de la monoacylglycérol lipase
JP2022534704A (ja) * 2019-06-04 2022-08-03 ヘイガー バイオサイエンシズ，エルエルシー オレキシンアンタゴニストとしてのイミダゾロ誘導体、組成物、及び方法

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20060135447A1 (en) * 2004-12-21 2006-06-22 Chupak Louis S Macrolides
US20130217727A1 (en) * 2010-10-21 2013-08-22 Jurgen Benting 1-(heterocyclic carbonyl)-2-substituted pyrrolidines
EP2730573A1 (en) * 2011-07-05 2014-05-14 Taisho Pharmaceutical Co., Ltd. Methylpiperidine derivative
WO2013062858A1 (en) * 2011-10-25 2013-05-02 Merck Sharp & Dohme Corp. Isoxazolopyridine orexin receptor antagonists
US20180222896A1 (en) * 2014-08-26 2018-08-09 Takeda Pharmaceutical Company Limited Heterocyclic compound

Also Published As

Publication number Publication date
EP3972587A1 (en) 2022-03-30
JP7837120B2 (ja) 2026-03-30
KR20220016919A (ko) 2022-02-10
AU2020288559B2 (en) 2025-04-17
SG11202112828SA (en) 2021-12-30
AU2020288559A1 (en) 2022-01-20
US20220315602A1 (en) 2022-10-06
WO2020247447A1 (en) 2020-12-10
CA3140173A1 (en) 2020-12-10
EP3972587A4 (en) 2023-01-18
CN114340616A (zh) 2022-04-12
US20240400580A1 (en) 2024-12-05
US12275744B2 (en) 2025-04-15
JP2022534709A (ja) 2022-08-03
AU2020288559A8 (en) 2022-02-03

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Legal Events

Date Code Title Description
TH Corrigenda

Free format text: IN VOL 36 , NO 3 , PAGE(S) 317 UNDER THE HEADING PCT APPLICATIONS THAT HAVE ENTERED THE NATIONAL PHASE - NAME INDEX UNDER THE NAME HAGER BIOSCIENCES, LLC, APPLICATION NO. 2020288559, UNDER INID (72) CORRECT THE CO-INVENTOR TO MEKONNEN, BELEW

DA2 Applications for amendment section 104

Free format text: THE NATURE OF THE AMENDMENT IS AS SHOWN IN THE STATEMENT(S) FILED 14 APR 2025

DA3 Amendments made section 104

Free format text: THE NATURE OF THE AMENDMENT IS AS SHOWN IN THE STATEMENT FILED 14 APR 2025

MK25 Application lapsed reg. 22.2i(2) - failure to pay acceptance fee