JP5847830B2 - オレキシン受容体拮抗薬として有用なラクタム誘導体 - Google Patents

オレキシン受容体拮抗薬として有用なラクタム誘導体 Download PDF

Info

Publication number
JP5847830B2
JP5847830B2 JP2013538312A JP2013538312A JP5847830B2 JP 5847830 B2 JP5847830 B2 JP 5847830B2 JP 2013538312 A JP2013538312 A JP 2013538312A JP 2013538312 A JP2013538312 A JP 2013538312A JP 5847830 B2 JP5847830 B2 JP 5847830B2
Authority
JP
Japan
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.)
Expired - Fee Related
Application number
JP2013538312A
Other languages
English (en)
Japanese (ja)
Other versions
JP2013545744A (ja
JP2013545744A5 (enExample
Inventor
アイサオウイ ハメッド
アイサオウイ ハメッド
クリストフ ボス
ボス クリストフ
ブロッチ クリスティーン
ブロッチ クリスティーン
ハイドマン ビビア
ハイドマン ビビア
シファーレン ティエリー
シファーレン ティエリー
ティー ウィリアムズ ジョディ
ティー ウィリアムズ ジョディ
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.)
Actelion 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 JP2013545744A publication Critical patent/JP2013545744A/ja
Publication of JP2013545744A5 publication Critical patent/JP2013545744A5/ja
Application granted granted Critical
Publication of JP5847830B2 publication Critical patent/JP5847830B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • 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
    • C07D207/24Oxygen or sulfur atoms
    • C07D207/262-Pyrrolidones
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • 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
    • C07D207/24Oxygen or sulfur atoms
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • 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
    • C07D211/72Heterocyclic 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
    • C07D211/74Oxygen atoms
    • C07D211/76Oxygen atoms attached in position 2 or 6
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic 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
    • C07D215/04Heterocyclic 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
    • C07D215/08Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic 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
    • C07D215/12Heterocyclic 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
    • C07D215/14Radicals substituted by oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D223/00Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/02Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings
    • 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
    • C07D223/08Oxygen atoms
    • C07D223/10Oxygen atoms attached in position 2
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/10Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D407/00Heterocyclic 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
    • C07D407/02Heterocyclic 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
    • C07D407/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • 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
    • C07D413/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/10Heterocyclic 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 aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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 three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Anesthesiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Diabetes (AREA)
  • Addiction (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (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)
JP2013538312A 2010-11-10 2011-11-09 オレキシン受容体拮抗薬として有用なラクタム誘導体 Expired - Fee Related JP5847830B2 (ja)

Applications Claiming Priority (3)

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

Publications (3)

Publication Number Publication Date
JP2013545744A JP2013545744A (ja) 2013-12-26
JP2013545744A5 JP2013545744A5 (enExample) 2014-12-11
JP5847830B2 true JP5847830B2 (ja) 2016-01-27

Family

ID=45757741

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2013538312A Expired - Fee Related JP5847830B2 (ja) 2010-11-10 2011-11-09 オレキシン受容体拮抗薬として有用なラクタム誘導体

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)

Families Citing this family (44)

* 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
TWI570120B (zh) 2012-06-04 2017-02-11 艾克泰聯製藥有限公司 苯并咪唑脯胺酸衍生物
LT3495367T (lt) 2012-06-13 2021-02-25 Incyte Holdings Corporation Pakeistieji tricikliniai junginiai, kaip fgfr inhibitoriai
HUE031885T2 (en) * 2012-07-19 2017-08-28 Cayman Chemical Co Inc Difluoro lactam preparations for EP4-mediated osteo-related diseases and conditions
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
WO2014089364A1 (en) 2012-12-06 2014-06-12 Quanticel Pharmaceuticals, Inc Histone demethylase inhibitors
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
US9676712B2 (en) 2013-03-15 2017-06-13 Cayman Chemical Company, Inc. Lactam compounds as EP4 receptor-selective agonists for use in the treatment of EP4-mediated diseases and conditions
WO2014144500A2 (en) 2013-03-15 2014-09-18 Cayman Chemical Company, Inc. Methods of synthesizing a difluorolactam analog
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
LT2986610T (lt) 2013-04-19 2018-04-10 Incyte Holdings Corporation Bicikliniai heterociklai, kaip fgfr inhibitoriai
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
KR20160048054A (ko) 2013-07-19 2016-05-03 카이맨 케미칼 컴파니 인코포레이티드 골 성장의 촉진을 위한 방법, 시스템 및 조성물
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
JP6496733B2 (ja) 2013-12-03 2019-04-03 イドーシア ファーマシューティカルズ リミテッドIdorsia Pharmaceuticals Ltd (s)−(2−(6−クロロ−7−メチル−1h−ベンゾ[d]イミダゾール−2−イル)−2−メチルピロリジン−1−イル)(5−メトキシ−2−(2h−1,2,3−トリアゾール−2−イル)フェニル)メタノンの結晶形及びオレキシン受容体アンタゴニストとしてのその使用
KR102330133B1 (ko) 2013-12-04 2021-11-23 이도르시아 파마슈티컬스 리미티드 벤즈이미다졸-프롤린 유도체의 용도
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
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
SG11201706287PA (en) 2015-02-20 2017-09-28 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
CA3027500A1 (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
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
ES3061844T3 (en) 2018-05-04 2026-04-07 Incyte Corp Salts of an fgfr inhibitor
MX2020011718A (es) 2018-05-04 2021-02-15 Incyte Corp Formas solidas de un inhibidor de receptores del factor de crecimiento de fibroblastos (fgfr) y procesos para prepararlas.
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
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
US12122767B2 (en) 2019-10-01 2024-10-22 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
TWI891666B (zh) 2019-10-14 2025-08-01 美商英塞特公司 作為fgfr抑制劑之雙環雜環
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2021113462A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Derivatives of an fgfr inhibitor
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
TW202304459A (zh) 2021-04-12 2023-02-01 美商英塞特公司 包含fgfr抑制劑及nectin-4靶向劑之組合療法
EP4352060A1 (en) 2021-06-09 2024-04-17 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
JP2024522189A (ja) 2021-06-09 2024-06-11 インサイト・コーポレイション Fgfr阻害剤としての三環式ヘテロ環
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
US7211580B2 (en) * 2002-07-23 2007-05-01 Cytokinetics, Incorporated Compounds, compositions, and methods
JP4094050B2 (ja) 2004-03-01 2008-06-04 アクテリオン ファーマシューティカルズ リミテッド 置換1,2,3,4−テトラヒドロイソキノリン誘導体
EP1888563A1 (en) * 2005-05-23 2008-02-20 Merck & Co., Inc. Proline bis-amide orexin receptor antagonists
EP1998774A1 (en) 2006-03-15 2008-12-10 Actelion Pharmaceuticals Ltd. Tetrahydroisoquinoline derivatives to enhance memory function
CA2659299A1 (en) * 2006-08-15 2008-02-21 Actelion Pharmaceuticals Ltd Azetidine compounds
CL2007002809A1 (es) * 2006-09-29 2008-04-18 Actelion Pharmaceuticals Ltd Compuestos derivados de 3-aza biciclo [3.1.0]hexano; y su uso en el tratamiento de enfermedades tales como desordenes psicoticos y de ansiedad, desordenes del sueno, uso y abuso de sustancias psicoactivas, demencia y deterioro de funciones cognitivas
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.
TW200911242A (en) * 2007-07-03 2009-03-16 Glaxo Group Ltd Novel compounds
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
CA2699328A1 (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
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
AU2009307918A1 (en) * 2008-10-21 2010-04-29 Merck Sharp & Dohme Corp. 2,4-disubstituted pyrrolidine orexin receptor antagonists
US20120088759A1 (en) 2009-05-12 2012-04-12 Hamed Aissaoui Thiazolidin-4-one and [1,3]-thiazinan-4-one compounds as orexin receptor antagonists
CA2758675A1 (en) 2009-05-12 2010-11-18 Actelion Pharmaceuticals Ltd Oxazolidinone derivatives

Also Published As

Publication number Publication date
CA2815179A1 (en) 2012-05-18
JP2013545744A (ja) 2013-12-26
EP2638008A1 (en) 2013-09-18
US9242970B2 (en) 2016-01-26
EP2638008B1 (en) 2015-07-01
CN103201261A (zh) 2013-07-10
US20130237525A1 (en) 2013-09-12
WO2012063207A1 (en) 2012-05-18

Similar Documents

Publication Publication Date Title
US9242970B2 (en) Lactam derivatives useful as orexin receptor antagonists
KR101247840B1 (ko) 아밀로이드 베타 조절제
JP3192662B2 (ja) 6―フェニルテトラヒドロ―1,3―オキサジン―2―オン誘導体及びそれを含む医薬組成物
US8703934B2 (en) Substituted 4-amino-3,5-dicyano-2-thiopyridines and use thereof
JP2011519849A (ja) ピペリジン及びピロリジン化合物
CN100451016C (zh) 作为5-羟色胺5ht-2受体的激动剂或拮抗剂的哌嗪基嘧啶化合物
JP2010526869A (ja) 2−シクロプロピル−チアゾール誘導体
JP2002517396A (ja) 細胞接着阻害抗炎症性化合物
JP2004532806A (ja) セロトニン5ht−2レセプターのアゴニストまたはアンタゴニストとしてのピペラジニルピラジン化合物
JP2011512400A (ja) 2−アザ−ビシクロ[2.2.1]ヘプタン誘導体
CA2044828A1 (en) Inhibitors of hiv reverse transcriptase
JP6129850B2 (ja) Mch受容体拮抗剤としてのベンゾイミダゾール誘導体
US20110021487A1 (en) Cycloalkoxy-substituted 4-phenyl-3,5-dicyanopyridines and their use
JP2011168617A (ja) 神経変性疾患の治療において有用なアナバセイン誘導体
JP2006511479A (ja) 3,4−二置換ピロールおよび炎症性疾患の治療におけるこれらの使用
US8329706B2 (en) Oxazolidinone derivatives
AU2013241050B2 (en) Triazinone compound and T-type calcium channel inhibitor
TW200404067A (en) New compounds
US20130303520A1 (en) NOVEL (HETEROCYCLE/TETRAHYDROPYRIDINE)-(PIPERAZINYL)-1-ALCANONE AND (HETEROCYCLE/DIHYDROPYRROLIDINE)-(PIPERAZINYL)-1-ALCANONE DERIVATIVES, AND USE THEREOF AS p75 INHIBITORS
US20120088759A1 (en) Thiazolidin-4-one and [1,3]-thiazinan-4-one compounds as orexin receptor antagonists
MXPA04006858A (es) Oxotieno(3,2-b) piridincarboxamidas como agentes antivirales.
TW200305567A (en) Compounds and use thereof for decreasing activity of hormonesensitive lipase

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20141024

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20141024

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20150708

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20150709

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20151006

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20151111

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20151125

R150 Certificate of patent or registration of utility model

Ref document number: 5847830

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

S111 Request for change of ownership or part of ownership

Free format text: JAPANESE INTERMEDIATE CODE: R313113

R350 Written notification of registration of transfer

Free format text: JAPANESE INTERMEDIATE CODE: R350

LAPS Cancellation because of no payment of annual fees