CA2815179A1 - Lactam derivatives useful as orexin receptor antagonists - Google Patents

Lactam derivatives useful as orexin receptor antagonists Download PDF

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Publication number
CA2815179A1
CA2815179A1 CA2815179A CA2815179A CA2815179A1 CA 2815179 A1 CA2815179 A1 CA 2815179A1 CA 2815179 A CA2815179 A CA 2815179A CA 2815179 A CA2815179 A CA 2815179A CA 2815179 A1 CA2815179 A1 CA 2815179A1
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Canada
Prior art keywords
dimethoxyphenyl
benzyl
methyl
piperidin
pyrrolidin
Prior art date
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Abandoned
Application number
CA2815179A
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English (en)
French (fr)
Inventor
Hamed Aissaoui
Christoph Boss
Christine Brotschi
Bibia Heidmann
Thierry Sifferlen
Jodi T. Williams
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Idorsia Pharmaceuticals Ltd
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Actelion Pharmaceuticals Ltd
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Publication date
Application filed by Actelion Pharmaceuticals Ltd filed Critical Actelion Pharmaceuticals Ltd
Publication of CA2815179A1 publication Critical patent/CA2815179A1/en
Abandoned legal-status Critical Current

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    • C07ORGANIC CHEMISTRY
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    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/10Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365Lactones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D207/262-Pyrrolidones
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    • C07D207/262-Pyrrolidones
    • C07D207/2732-Pyrrolidones with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
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    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
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    • C07D211/68Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
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    • C07D223/06Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D401/06Heterocyclic 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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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  • Chemical & Material Sciences (AREA)
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  • Animal Behavior & Ethology (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
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  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Addiction (AREA)
  • Child & Adolescent Psychology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Anesthesiology (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pyrrole Compounds (AREA)
CA2815179A 2010-11-10 2011-11-09 Lactam derivatives useful as orexin receptor antagonists Abandoned CA2815179A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
IB2010055105 2010-11-10
IBPCT/IB2010/055105 2010-11-10
PCT/IB2011/054993 WO2012063207A1 (en) 2010-11-10 2011-11-09 Lactam derivatives useful as orexin receptor antagonists

Publications (1)

Publication Number Publication Date
CA2815179A1 true CA2815179A1 (en) 2012-05-18

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CA2815179A Abandoned CA2815179A1 (en) 2010-11-10 2011-11-09 Lactam derivatives useful as orexin receptor antagonists

Country Status (6)

Country Link
US (1) US9242970B2 (OSRAM)
EP (1) EP2638008B1 (OSRAM)
JP (1) JP5847830B2 (OSRAM)
CN (1) CN103201261A (OSRAM)
CA (1) CA2815179A1 (OSRAM)
WO (1) WO2012063207A1 (OSRAM)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110563565A (zh) * 2019-09-02 2019-12-13 南通大学 一种3-溴-6-氟-2-甲氧基苯甲醛的合成方法

Families Citing this family (43)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
KR101995683B1 (ko) 2012-06-04 2019-07-02 이도르시아 파마슈티컬스 리미티드 벤즈이미다졸-프롤린 유도체
ES2984771T3 (es) 2012-06-13 2024-10-31 Incyte Holdings Corp Compuestos tricíclicos sustituidos como inhibidores de FGFR
EP3176162B1 (en) * 2012-07-19 2020-05-27 Cayman Chemical Company, Inc. Difluorolactam compounds as ep4 receptor-selective agonists for use in the treatment of ep4-mediated disease and conditions
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
ES2834959T3 (es) 2012-12-06 2021-06-21 Celgene Quanticel Res Inc Inhibidores de histona desmetilasa
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
US9914725B2 (en) 2013-03-15 2018-03-13 Cayman Chemical Company, Inc. Methods of synthesizing a difluorolactam analog
WO2014144610A1 (en) 2013-03-15 2014-09-18 Cayman Chemical Company, Inc. Lactam compounds as ep4 receptor-selective agonists for use in the treatment of ep4-mediated diseases and conditions
ES2635635T3 (es) 2013-03-15 2017-10-04 Cayman Chemical Company, Incorporated Compuestos de difluorolactama como agonistas selectivos del receptor EP4 para su uso en el tratamiento de enfermedades y afecciones mediadas por EP4
EA035095B1 (ru) 2013-04-19 2020-04-27 Инсайт Холдингс Корпорейшн Бициклические гетероциклы в качестве ингибиторов fgfr
CN104133004A (zh) * 2013-05-03 2014-11-05 上海美迪西生物医药有限公司 血浆样品中2,3-吲哚醌的浓度的测定方法
AU2014290512A1 (en) 2013-07-19 2015-11-12 Cayman Chemical Company, Inc. Methods, systems, and compositions for promoting bone growth
UA119151C2 (uk) 2013-12-03 2019-05-10 Ідорсія Фармасьютікалз Лтд КРИСТАЛІЧНА СОЛЬОВА ФОРМА (S)-(2-(6-ХЛОР-7-МЕТИЛ-1H-БЕНЗО[d]ІМІДАЗОЛ-2-ІЛ)-2-МЕТИЛПІРОЛІДИН-1-ІЛ)(5-МЕТОКСИ-2-(2H-1,2,3-ТРИАЗОЛ-2-ІЛ)ФЕНІЛ)МЕТАНОНУ ЯК АНТАГОНІСТ ОРЕКСИНОВОГО РЕЦЕПТОРА
MY179862A (en) 2013-12-03 2020-11-18 Idorsia Pharmaceuticals Ltd Crystalline form of (s)-(2-(6-chloro-7-methyl-1h-benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1 -yl)(5-methoxy-2-(2h-1,2,3-triazol-2-yl)phenyl)methanone and its use as orexin receptor antagonists
UA116053C2 (uk) 2013-12-04 2018-01-25 Ідорсія Фармасьютікалз Лтд Застосування похідних бензоімідазолу-проліну
US9975876B2 (en) 2013-12-09 2018-05-22 Merck Sharp & Dohme Corp. 2-pyridyloxy-3-ester-4-ether orexin receptor antagonists
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
EA038045B1 (ru) 2015-02-20 2021-06-28 Инсайт Корпорейшн Бициклические гетероциклы в качестве ингибиторов fgfr
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
CA3027498A1 (en) 2016-06-21 2017-12-28 X4 Pharmaceuticals, Inc. Cxcr4 inhibitors and uses thereof
WO2017223243A1 (en) * 2016-06-21 2017-12-28 X4 Pharmaceuticals, Inc. Cxcr4 inhibitors and uses thereof
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
TWI799435B (zh) * 2017-08-02 2023-04-21 美商維泰克斯製藥公司 製備化合物之製程
RS66310B1 (sr) 2018-05-04 2025-01-31 Incyte Corp Čvrsti oblici inhibitora fgfr i procesi za njegovu pripremu
US11174257B2 (en) 2018-05-04 2021-11-16 Incyte Corporation Salts of an FGFR inhibitor
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
PH12022550892A1 (en) 2019-10-14 2023-05-03 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
AU2020395185A1 (en) 2019-12-04 2022-06-02 Incyte Corporation Derivatives of an FGFR inhibitor
EP4069696A1 (en) 2019-12-04 2022-10-12 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
JP2024513575A (ja) 2021-04-12 2024-03-26 インサイト・コーポレイション Fgfr阻害剤及びネクチン-4標的化剤を含む併用療法
WO2022261160A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
TW202313610A (zh) 2021-06-09 2023-04-01 美商英塞特公司 作為fgfr抑制劑之三環雜環
CN114456184B (zh) * 2022-02-21 2023-08-22 南华大学附属第一医院 一种3-芳基异喹啉衍生物及其制备与应用
CN115047127B (zh) * 2022-04-25 2024-03-08 中国检验检疫科学研究院 一种利用挥发性代谢组学技术鉴别nfc和fc橙汁的方法
TW202409023A (zh) 2022-07-14 2024-03-01 美商富曼西公司 除草苯并𠯤
WO2025111184A1 (en) 2023-11-21 2025-05-30 Fmc Corporation Substituted tetrahydroquinoline and tetrahydroquinoxaline herbicides
WO2025224168A1 (en) 2024-04-24 2025-10-30 Idorsia Pharmaceuticals Ltd Aryl sulfone and sulfanone derivatives as orexin receptor modulators

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0115862D0 (en) * 2001-06-28 2001-08-22 Smithkline Beecham Plc Compounds
AU2003256805A1 (en) * 2002-07-23 2004-02-09 Cytokinetics, Inc. Compounds compositions and methods
BRPI0508263B8 (pt) 2004-03-01 2021-05-25 Idorsia Pharmaceuticals Ltd derivados de 1, 2, 3, 4-tetra-hidro-isoquinolina, composição farmacêutica, e, uso de derivado de 1, 2, 3, 4-tetra-hidro-isoquinolina
WO2006127550A1 (en) * 2005-05-23 2006-11-30 Merck & Co., Inc. Proline bis-amide orexin receptor antagonists
JP4582722B2 (ja) 2006-03-15 2010-11-17 アクテリオン ファーマシューティカルズ リミテッド 記憶機能を向上させるテトラヒドロイソキノリン誘導体
JP2010500401A (ja) * 2006-08-15 2010-01-07 アクテリオン ファーマシューティカルズ リミテッド アゼチジン化合物
WO2008038251A2 (en) * 2006-09-29 2008-04-03 Actelion Pharmaceuticals Ltd 3-aza-bicyclo[3.1.0]hexane derivatives
CL2008000836A1 (es) * 2007-03-26 2008-11-07 Actelion Pharmaceuticals Ltd Compuestos derivados de tiazolidina, antagonistas del receptor de orexina; composicion farmaceutica que los comprende; y su uso en el tratamiento de neurosis emocional, depresion grave, trastornos psicoticos, alzheimer, parkinson, dolor, entre otras.
WO2009003993A1 (en) * 2007-07-03 2009-01-08 Glaxo Group Limited Piperidine derivatives useful as orexin receptor antagonists
BRPI0815079A2 (pt) * 2007-08-15 2015-02-03 Actelion Pharmaceuticals Ltd Composto dericado de 1,2-diamido-etileno, composição farmacêutica que contém e uso desse composto
WO2009040730A2 (en) * 2007-09-24 2009-04-02 Actelion Pharmaceuticals Ltd Pyrrolidines and piperidines as orexin receptor antagonists
PE20091010A1 (es) 2007-10-10 2009-08-08 Actelion Pharmaceuticals Ltd Derivados de tetrahidroquinolina
EP2318367B1 (en) * 2008-04-30 2013-03-20 Actelion Pharmaceuticals Ltd. Piperidine and pyrrolidine compounds
KR20110020906A (ko) * 2008-06-11 2011-03-03 액테리온 파마슈티칼 리미티드 오렉신 수용체 안타고니스트로서의 테트라졸 화합물
WO2010048014A1 (en) * 2008-10-21 2010-04-29 Merck Sharp & Dohme Corp. 2,4-disubstituted pyrrolidine orexin receptor antagonists
CN102414184A (zh) * 2009-05-12 2012-04-11 埃科特莱茵药品有限公司 新型的噁唑烷酮衍生物及其作为食欲素受体拮抗剂的用途
US20120088759A1 (en) 2009-05-12 2012-04-12 Hamed Aissaoui Thiazolidin-4-one and [1,3]-thiazinan-4-one compounds as orexin receptor antagonists

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110563565A (zh) * 2019-09-02 2019-12-13 南通大学 一种3-溴-6-氟-2-甲氧基苯甲醛的合成方法

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