CN116615427B - 被取代的大环化合物及相关治疗方法 - Google Patents

被取代的大环化合物及相关治疗方法 Download PDF

Info

Publication number
CN116615427B
CN116615427B CN202180080848.8A CN202180080848A CN116615427B CN 116615427 B CN116615427 B CN 116615427B CN 202180080848 A CN202180080848 A CN 202180080848A CN 116615427 B CN116615427 B CN 116615427B
Authority
CN
China
Prior art keywords
formula
another embodiment
ring
alkyl
alkylene
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.)
Active
Application number
CN202180080848.8A
Other languages
English (en)
Chinese (zh)
Other versions
CN116615427A (zh
Inventor
刘易斯·D·彭宁顿
崔永吉
黄霍安
布莱恩·M·阿奎拉
英戈·安德里亚斯·马格
胡元
詹姆斯·R·伍兹
布莱恩·肯尼斯·雷默
乔治·马丁·本齐恩
乔纳森·沃德·莱曼
迈克尔·R·霍尔
斯里尼瓦斯·卡拉
罗曼·A·瓦利林
达尔吉特·马塔鲁
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.)
Alkermes Inc
Original Assignee
Alkermes Inc
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 Alkermes Inc filed Critical Alkermes Inc
Publication of CN116615427A publication Critical patent/CN116615427A/zh
Application granted granted Critical
Publication of CN116615427B publication Critical patent/CN116615427B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A61P25/10—Antiepileptics; Anticonvulsants for petit-mal
    • 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
    • C07D498/12—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 three hetero rings
    • C07D498/14—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
CN202180080848.8A 2020-12-21 2021-12-21 被取代的大环化合物及相关治疗方法 Active CN116615427B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US202063128404P 2020-12-21 2020-12-21
US63/128,404 2020-12-21
US202163190937P 2021-05-20 2021-05-20
US63/190,937 2021-05-20
PCT/US2021/064483 WO2022140316A1 (en) 2020-12-21 2021-12-21 Substituted macrocyclic compounds and related methods of treatment

Publications (2)

Publication Number Publication Date
CN116615427A CN116615427A (zh) 2023-08-18
CN116615427B true CN116615427B (zh) 2025-07-04

Family

ID=80050560

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202180080848.8A Active CN116615427B (zh) 2020-12-21 2021-12-21 被取代的大环化合物及相关治疗方法

Country Status (10)

Country Link
US (2) US12006330B2 (https=)
EP (1) EP4263555A1 (https=)
JP (1) JP2024501641A (https=)
KR (1) KR20230127254A (https=)
CN (1) CN116615427B (https=)
AU (1) AU2021409403A1 (https=)
CA (1) CA3172841A1 (https=)
IL (1) IL303848A (https=)
MX (1) MX2023005338A (https=)
WO (1) WO2022140316A1 (https=)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FI4065585T3 (fi) 2019-11-25 2025-09-26 Alkermes Inc Substituoituja makrosyklisiä yhdisteitä ja niihin liittyviä hoitomenetelmiä
WO2022109117A1 (en) * 2020-11-23 2022-05-27 Merck Sharp & Dohme Corp. 3-amino pyrrolidine and piperidine macrocyclic orexin receptor agonists
US12006330B2 (en) * 2020-12-21 2024-06-11 Alkermes, Inc. Substituted macrocyclic compounds and related methods of treatment
US11760747B2 (en) 2020-12-21 2023-09-19 Alkermes, Inc. Substituted piperidino compounds and related methods of treatment
WO2022232025A1 (en) * 2021-04-26 2022-11-03 Alkermes, Inc. Substituted amide macrocyclic compounds with orexin-2 receptor agonist activity
WO2022251304A1 (en) * 2021-05-26 2022-12-01 Alkerme, Inc. Substituted carbamate macrocyclic compounds and related methods of treatment
EP4347046A1 (en) * 2021-05-26 2024-04-10 Alkermes, Inc. Substituted fused bicyclic macrocyclic compounds and related methods of treatment
EP4622712A1 (en) * 2022-11-23 2025-10-01 Vertex Pharmaceuticals Incorporated Substituted macrocyclic amine modulators of orexin receptor 2
EP4658660A1 (en) * 2023-01-31 2025-12-10 Jazz Pharmaceuticals Ireland Limited Macrocyclic orexin receptor agonists and uses thereof
KR20250155550A (ko) * 2023-03-16 2025-10-30 다케다 야쿠힌 고교 가부시키가이샤 매크로시클릭 헤테로시클 화합물 및 이의 용도
US20240425521A1 (en) 2023-06-01 2024-12-26 H. Lundbeck A/S Spiromacrocyclic orexin 2 receptor agonists
WO2025096445A1 (en) * 2023-10-30 2025-05-08 Alkermes, Inc. Synthesis of intermediates for the preparation of macrocyclic compounds
WO2025124698A1 (en) 2023-12-12 2025-06-19 Idorsia Pharmaceuticals Ltd Aryl sulfone and sulfanone derivatives as orexin receptor modulators
TW202542165A (zh) 2023-12-19 2025-11-01 瑞士商愛杜西亞製藥有限公司 大環食慾素激動劑
WO2026017128A1 (zh) * 2024-07-17 2026-01-22 江苏恩华药业股份有限公司 作为食欲素受体激动剂的环烯烃衍生物及其组合物和用途
WO2026064378A1 (en) * 2024-09-18 2026-03-26 Vertex Pharmaceuticals Incorporated Macrocyclic sulfonamide modulators

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021108628A1 (en) * 2019-11-25 2021-06-03 Alkermes, Inc. Substituted macrocyclic compounds and related methods of treatment
WO2022109117A1 (en) * 2020-11-23 2022-05-27 Merck Sharp & Dohme Corp. 3-amino pyrrolidine and piperidine macrocyclic orexin receptor agonists

Family Cites Families (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8258163B2 (en) 2008-06-04 2012-09-04 Board Of Regents, The University Of Texas System Small-molecule agonists for type-2 orexin receptor
EP2694472B1 (en) 2011-04-05 2020-03-11 Takeda Pharmaceutical Company Limited Sulfonamide derivative and use thereof
US10017481B2 (en) 2012-03-17 2018-07-10 Polyphor Ag Conformationally constrained, fully synthetic macrocyclic compounds
WO2014198880A1 (en) 2013-06-14 2014-12-18 Ferrer Internacional, S.A. 2-(2-aminophenoxy)-3-chloronaphthalene-1,4-dione compounds having orexin 2 receptor agonist activity
US20160250224A1 (en) 2013-09-24 2016-09-01 The Board Of Regents Of The University Of Texas System Orexin-control of bone formation and loss
CA2930693A1 (en) 2013-11-15 2015-05-21 The Board Of Trustees Of The Leland Stanford Junior Unversity Methods of treating heart failure with agonists of hypocretin receptor 2
PE20161064A1 (es) 2013-12-12 2016-10-28 Univ Tsukuba Derivado de sulfonamida o sales de adicion de acido farmaceuticamente aceptables del mismo
WO2015147240A1 (ja) 2014-03-28 2015-10-01 国立大学法人筑波大学 敗血症の予防治療剤
KR102455043B1 (ko) 2014-09-11 2022-10-13 얀센 파마슈티카 엔.브이. 치환된 2-아자바이사이클 및 오렉신 수용체 조절제로서의 이의 용도
WO2016133160A1 (ja) 2015-02-19 2016-08-25 国立大学法人筑波大学 スルホンアミド誘導体またはその薬学的に許容される酸付加塩
WO2016199906A1 (ja) 2015-06-12 2016-12-15 国立大学法人筑波大学 スルホンアミド誘導体またはその薬学的に許容される酸付加塩
PL3411358T3 (pl) 2016-02-04 2022-02-28 Takeda Pharmaceutical Company Limited Podstawiony związek piperydynowy i jego zastosowanie
WO2018164191A1 (ja) 2017-03-08 2018-09-13 武田薬品工業株式会社 置換ピロリジン化合物およびその用途
US11034700B2 (en) 2017-03-08 2021-06-15 Takeda Pharmaceutical Company Limited Substituted pyrrolidine compound and use thereof
US20200207734A1 (en) 2017-08-03 2020-07-02 Takeda Pharmaceutical Company Limited Heterocyclic compound and use thereof
US11319286B2 (en) 2017-08-03 2022-05-03 Takeda Pharmaceutical Company Limited Heterocyclic compound and application thereof
CN111132975B (zh) 2017-09-28 2023-05-23 勃林格殷格翰国际有限公司 N-(2,2-二氟乙基)-n-[(嘧啶基氨基)丙基]芳基甲酰胺
WO2019117148A1 (ja) 2017-12-12 2019-06-20 国立大学法人 筑波大学 スルホンアミド誘導体またはその薬学的に許容される酸付加塩
MX2020010155A (es) 2018-03-27 2021-03-25 Univ Texas Compuestos de ox2r.
JP7413261B2 (ja) 2018-06-29 2024-01-15 武田薬品工業株式会社 複素環化合物およびその用途
US12077522B2 (en) 2018-06-29 2024-09-03 Takeda Pharmaceutical Company Limited Heterocyclic compound and application thereof
EP3896060B1 (en) 2018-12-12 2023-08-16 Takeda Pharmaceutical Company Limited Heterocyclic compound
JP7379374B2 (ja) 2018-12-12 2023-11-14 武田薬品工業株式会社 複素環化合物
SG11202106791XA (en) 2019-01-31 2021-07-29 Takeda Pharmaceuticals Co Heterocyclic compound and use thereof
US11098029B2 (en) 2019-02-13 2021-08-24 Merck Sharp & Dohme Corp. 5-alkyl pyrrolidine orexin receptor agonists
WO2020167701A1 (en) 2019-02-13 2020-08-20 Merck Sharp & Dohme Corp. Pyrrolidine orexin receptor agonists
WO2021026047A1 (en) 2019-08-08 2021-02-11 Merck Sharp & Dohme Corp. Heteroaryl pyrrolidine and piperidine orexin receptor agonists
BR112022004576A2 (pt) 2019-09-13 2022-06-14 Takeda Pharmaceuticals Co Métodos para diminuir ou tratar sonolência excessiva, tratar narcolepsia tipo 2 ou hipersonia idiopática, tratar distúrbio de trabalho de turno, aumentar latência de sono em manutenção de teste de insônia, melhorar classificação de escaça de sonolência de karolinska, diminuir ou melhorar sonolência subjetiva, aumentar insônia ou diminuir sonolência excessiva, melhorar classificação de escala de sonolência epworth, tratar narcolepsia tipo 2, diminuir ou tratar sonolência diurna excessiva, e, composição farmacêutica
WO2021106975A1 (ja) 2019-11-27 2021-06-03 武田薬品工業株式会社 複素環化合物
US11352357B2 (en) 2019-11-27 2022-06-07 Sumitomo Dainippon Pharma Co., Ltd. Cycloalkylurea derivative
MX2022008392A (es) 2020-01-10 2022-08-08 Takeda Pharmaceuticals Co Metodo para mejorar la farmacocinetica o aumentar la concentracion de plasma de 3-((metilsulfonil)amino)-2-(((4-fenilci clohexil)oxi)metil)piperidina-1-carboxilato de metilo o una sal del mismo con un inhibidor de citocromo p450.
KR20230040953A (ko) 2020-07-17 2023-03-23 에자이 알앤드디 매니지먼트 가부시키가이샤 치환된 피페리딘 화합물 및 이의 적용례
BR112023002957A2 (pt) 2020-08-18 2023-04-04 Merck Sharp & Dohme Llc Composto, composição farmacêutica, e, métodos para tratar narcolepsia e para tratar hipersonia em um sujeito mamífero
EP4199925A4 (en) 2020-08-18 2024-08-28 Merck Sharp & Dohme LLC CYCLOPENTAPYRROLE OREXIN RECEPTOR AGONISTS
US12503475B2 (en) 2020-09-03 2025-12-23 Centessa Pharmaceuticals (Uk) Limited Bicyclic-heterocycle derivatives and their uses as orexin-2 receptor agonists
WO2022051583A1 (en) 2020-09-03 2022-03-10 Orexia Therapeutics Limited Medium- or macro-cyclic benzyl-substituted heterocycle derivatives and their uses as orexin-2 receptor agonists
JP2022064180A (ja) 2020-10-13 2022-04-25 武田薬品工業株式会社 複素環化合物
EP4236938A4 (en) 2020-11-02 2024-10-16 Merck Sharp & Dohme LLC MACROCYCLIC UREA-OREX RECEPTOR AGONISTS
EP4255429A4 (en) 2020-12-03 2024-12-11 Merck Sharp & Dohme LLC 3-heteroaryl pyrrolidine and piperidine orexin receptor agonists
US20240101555A1 (en) 2020-12-16 2024-03-28 Merck Sharp & Dohme Llc Urea orexin receptor agonists
US12006330B2 (en) * 2020-12-21 2024-06-11 Alkermes, Inc. Substituted macrocyclic compounds and related methods of treatment
US20240174605A1 (en) 2021-03-03 2024-05-30 Research Triangle Institute Arylsulfonamides as orexin receptor agonists
WO2022207935A1 (en) 2021-04-02 2022-10-06 Orexia Therapeutics Limited 2-(3-ethynylbenzyl)-substituted heterocycle derivatives as orexin-2 agonists
KR20240004802A (ko) 2021-05-03 2024-01-11 재즈 파마슈티칼즈 아일랜드 리미티드 오렉신 수용체 효능제 및 그의 용도
CA3219888A1 (en) 2021-05-26 2022-12-01 Masafumi KOMIYA Phenyl urea derivative
EP4359387A1 (en) 2021-06-25 2024-05-01 Jazz Pharmaceuticals Ireland Limited Sulfonamide orexin receptor agonists and uses thereof
WO2023017180A1 (en) 2021-08-13 2023-02-16 Orexia Therapeutics Limited Peptide derivatives and related uses as orexin agonists

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021108628A1 (en) * 2019-11-25 2021-06-03 Alkermes, Inc. Substituted macrocyclic compounds and related methods of treatment
WO2022109117A1 (en) * 2020-11-23 2022-05-27 Merck Sharp & Dohme Corp. 3-amino pyrrolidine and piperidine macrocyclic orexin receptor agonists

Also Published As

Publication number Publication date
JP2024501641A (ja) 2024-01-15
US20240368182A1 (en) 2024-11-07
MX2023005338A (es) 2023-05-22
KR20230127254A (ko) 2023-08-31
CN116615427A (zh) 2023-08-18
US12006330B2 (en) 2024-06-11
EP4263555A1 (en) 2023-10-25
IL303848A (en) 2023-08-01
AU2021409403A9 (en) 2025-03-20
US20220194958A1 (en) 2022-06-23
WO2022140316A1 (en) 2022-06-30
AU2021409403A1 (en) 2023-05-25
CA3172841A1 (en) 2022-06-30

Similar Documents

Publication Publication Date Title
CN116615427B (zh) 被取代的大环化合物及相关治疗方法
JP7787812B2 (ja) 置換大環状化合物および関連する治療方法
EP4329877B1 (en) Substituted amide macrocyclic compounds with orexin-2 receptor agonist activity
CN116670124A (zh) 被取代的哌啶类化合物及相关治疗方法
JP2024520395A (ja) 置換される縮合二環式大環状化合物および関連のある治療方法
EP4347604B1 (en) Substituted carbamate macrocyclic compounds and related methods of treatment
WO2022093849A1 (en) Pyrimidine derivatives as modulators of the 5-ht2a serotonin receptor useful for the treatment of disorders related thereto
JP2026503035A (ja) 新規な可逆性ｄｐｐ１阻害剤及びその用途
EA007335B1 (ru) Новые соединения и композиции как ингибиторы катепсина
JP2025521503A (ja) 置換ピロリジニル及びピペリジニル化合物並びに関連する治療方法
JP2025521508A (ja) 置換ピロリジニル及びピペリジニル化合物並びに関連する治療方法
CA3199269A1 (en) Isoxazole derivatives as modulators of the 5-ht2a serotonin receptor useful for the treatment of disorders related thereto
EA049565B1 (ru) Замещенные макроциклические соединения, обладающие активностью агониста рецептора орексина-2, и их применение
HK40129946A (en) Substituted macrocyclic compounds and related methods of treatment
HK40079289B (en) Substituted macrocyclic compounds and related methods of treatment
HK40079289A (en) Substituted macrocyclic compounds and related methods of treatment

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
CB02 Change of applicant information
CB02 Change of applicant information

Address after: 900 Winter Street, Waltham, Massachusetts, United States

Applicant after: Alkermes, Inc.

Address before: 852 winter street, Waltham, Massachusetts, USA

Applicant before: Alkermes, Inc.

GR01 Patent grant
GR01 Patent grant