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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CA
Canada
Prior art keywords
dimethoxyphenyl
benzyl
methyl
piperidin
pyrrolidin
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.)
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
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.)
Idorsia Pharmaceuticals Ltd
Original Assignee
Actelion Pharmaceuticals Ltd
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 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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    • 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
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365—Lactones
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic 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
    • C07D207/18—Heterocyclic 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
    • C07D207/22—Heterocyclic 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic 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
    • C07D207/18—Heterocyclic 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
    • C07D207/22—Heterocyclic 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/273—2-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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68—Heterocyclic 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
    • C07D211/72—Heterocyclic 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 with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D211/74—Oxygen atoms
    • C07D211/76—Oxygen atoms attached in position 2 or 6
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/04—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms
    • C07D215/08—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms with acylated ring nitrogen atom
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    • C07D215/12—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D215/14—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/02—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D223/06—Heterocyclic 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
    • C07D223/08—Oxygen atoms
    • C07D223/10—Oxygen atoms attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/06—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members
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    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/10—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 two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • 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
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
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    • 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
    • C07D407/02—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 two hetero rings
    • C07D407/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
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    • C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
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  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Addiction (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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ID=45757741

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Application Number Title Priority Date Filing Date
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 (enExample)
EP (1) EP2638008B1 (enExample)
JP (1) JP5847830B2 (enExample)
CN (1) CN103201261A (enExample)
CA (1) CA2815179A1 (enExample)
WO (1) WO2012063207A1 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
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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
HUE042374T2 (hu) 2012-06-13 2019-06-28 Incyte Holdings Corp Szubsztituált triciklusos vegyületek mint FGFR inhibitorok
CN107802623B (zh) * 2012-07-19 2020-10-30 开曼化学股份有限公司 用于ep4介导的骨相关疾病和病症的二氟内酰胺组合物
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
EP3763367A1 (en) 2012-12-06 2021-01-13 Celgene Quanticel Research, Inc. Pyridine-pyrazole derivatives as histone demethylase inhibitors
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
BR112015023080A2 (pt) 2013-03-15 2017-07-18 Cayman Chemical Co Inc composto, composição farmacêutica, e, método para tratamento de doenças
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
JP6368351B2 (ja) 2013-03-15 2018-08-01 ケイマン ケミカル カンパニー， インコーポレーテッド ジフルオロラクタムアナログを合成する方法
HUE036571T2 (hu) 2013-04-19 2018-07-30 Incyte Holdings Corp Biciklusos heterociklusok mint FGFR inhibitorok
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
WO2015009991A2 (en) 2013-07-19 2015-01-22 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
US9914720B2 (en) 2013-12-03 2018-03-13 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
HK1225734B (en) 2013-12-04 2017-09-15 Idorsia Pharmaceuticals Ltd Use of benzimidazole-proline derivatives
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
MX388991B (es) 2015-02-20 2025-03-20 Incyte Corp Heterociclos biciclicos como inhibidores de receptores del factor de crecimiento fibroblastico (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
WO2017223243A1 (en) * 2016-06-21 2017-12-28 X4 Pharmaceuticals, Inc. Cxcr4 inhibitors and uses thereof
JP7054529B2 (ja) 2016-06-21 2022-04-14 エックス４ ファーマシューティカルズ， インコーポレイテッド Ｃｘｃｒ４阻害剤およびその使用
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
ES2912657T3 (es) * 2017-08-02 2022-05-26 Vertex Pharma Procesos para preparar compuestos de pirrolidina
EP3788047B1 (en) 2018-05-04 2024-09-04 Incyte Corporation Solid forms of an fgfr inhibitor and processes for preparing the same
BR112020022373A2 (pt) 2018-05-04 2021-02-02 Incyte Corporation sais de um inibidor de fgfr
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
KR20220100879A (ko) 2019-10-14 2022-07-18 인사이트 코포레이션 Fgfr 저해제로서의 이환식 헤테로사이클
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021113479A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
KR20220131900A (ko) 2019-12-04 2022-09-29 인사이트 코포레이션 Fgfr 억제제의 유도체
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2022221170A1 (en) 2021-04-12 2022-10-20 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
TW202313611A (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
EP4352060A1 (en) 2021-06-09 2024-04-17 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
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
JP2006501201A (ja) * 2002-07-23 2006-01-12 サイトキネティクス・インコーポレーテッド 化合物、組成物および方法
CA2557163C (en) 2004-03-01 2011-08-16 Actelion Pharmaceuticals Ltd Substituted 1,2,3,4-tetrahydroisoquinoline derivatives
JP2008542276A (ja) * 2005-05-23 2008-11-27 メルク エンド カムパニー インコーポレーテッド プロリンビスアミドオレキシン受容体アンタゴニスト
KR101065239B1 (ko) 2006-03-15 2011-09-16 액테리온 파마슈티칼 리미티드 기억 기능을 증진하는 테트라히드로이소퀴놀린 유도체
CA2659299A1 (en) * 2006-08-15 2008-02-21 Actelion Pharmaceuticals Ltd Azetidine compounds
DE602007009284D1 (de) * 2006-09-29 2010-10-28 Actelion Pharmaceuticals Ltd 3-aza-bicycloä3.1.0ühexanderivate
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.
EP2176258A1 (en) * 2007-07-03 2010-04-21 Glaxo Group Limited Piperidine derivatives useful as orexin receptor antagonists
RU2010109455A (ru) * 2007-08-15 2011-09-20 Актелион Фармасьютиклз Лтд (Ch) Производные 1,2-диамидоэтилена в качестве антагонистов орексина
CN101874030B (zh) * 2007-09-24 2012-11-14 埃科特莱茵药品有限公司 用作食欲素受体拮抗剂的吡咯烷和哌啶
PE20091010A1 (es) 2007-10-10 2009-08-08 Actelion Pharmaceuticals Ltd Derivados de tetrahidroquinolina
CN102015645B (zh) * 2008-04-30 2012-11-14 埃科特莱茵药品有限公司 哌啶和吡咯烷化合物
JP2011522878A (ja) * 2008-06-11 2011-08-04 アクテリオン ファーマシューティカルズ リミテッド オレキシン受容体拮抗薬としてのテトラゾール化合物
JP2012506377A (ja) * 2008-10-21 2012-03-15 メルク・シャープ・エンド・ドーム・コーポレイション ２，４−二置換フェニルカルボキサミド・オレキシン受容体アンタゴニスト
EP2429523A1 (en) 2009-05-12 2012-03-21 Actelion Pharmaceuticals Ltd. Thiazolidin-4-one and [1,3]-thiazinan-4-one compounds as orexin receptor antagonists
EP2430004B1 (en) 2009-05-12 2013-07-17 Actelion Pharmaceuticals Ltd. Novel oxazolidinone derivatives and their use 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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