CN103201261A - 用作为食欲素受体拮抗剂的内酰胺衍生物 - Google Patents

用作为食欲素受体拮抗剂的内酰胺衍生物 Download PDF

Info

Publication number
CN103201261A
CN103201261A CN2011800543642A CN201180054364A CN103201261A CN 103201261 A CN103201261 A CN 103201261A CN 2011800543642 A CN2011800543642 A CN 2011800543642A CN 201180054364 A CN201180054364 A CN 201180054364A CN 103201261 A CN103201261 A CN 103201261A
Authority
CN
China
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.)
Pending
Application number
CN2011800543642A
Other languages
English (en)
Chinese (zh)
Inventor
哈马德·艾斯奥维
克里斯多夫·博斯
克莉丝汀·普罗奇
比比安·海德曼
蒂埃里·西弗朗
约迪·T·威廉斯
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 CN103201261A publication Critical patent/CN103201261A/zh
Pending legal-status Critical Current

Links

Classifications

    • 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
    • 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
    • C07D215/12—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
    • C—CHEMISTRY; METALLURGY
    • 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
    • C—CHEMISTRY; METALLURGY
    • 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
    • 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
    • C07D401/14—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
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—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
    • 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
    • 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
    • C07D413/06—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 only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/06—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/10—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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)
  • General Health & Medical Sciences (AREA)
  • 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)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Child & Adolescent Psychology (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)
CN2011800543642A 2010-11-10 2011-11-09 用作为食欲素受体拮抗剂的内酰胺衍生物 Pending CN103201261A (zh)

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 (1)

Publication Number Publication Date
CN103201261A true CN103201261A (zh) 2013-07-10

Family

ID=45757741

Family Applications (1)

Application Number Title Priority Date Filing Date
CN2011800543642A Pending CN103201261A (zh) 2010-11-10 2011-11-09 用作为食欲素受体拮抗剂的内酰胺衍生物

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
Publication number Priority date Publication date Assignee Title
CN115047127A (zh) * 2022-04-25 2022-09-13 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

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
DK2855453T3 (en) 2012-06-04 2017-02-06 Actelion Pharmaceuticals Ltd Benzimidazol-proline derivatives
CA2876689C (en) 2012-06-13 2022-04-26 Incyte Corporation Substituted tricyclic compounds as fgfr inhibitors
EP2875022B1 (en) * 2012-07-19 2016-10-12 Cayman Chemical Company, Incorporated Difluorolactam compounds as ep4 receptor-selective agonists for use in the treatment of ep4-mediated disease and conditions
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
US8987461B2 (en) 2012-12-06 2015-03-24 Quanticel Pharmaceuticals, Inc. Histone demethylase inhibitors
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
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
WO2014144500A2 (en) 2013-03-15 2014-09-18 Cayman Chemical Company, Inc. Methods of synthesizing a difluorolactam analog
PT2989098T (pt) 2013-03-15 2017-08-16 Cayman Chemical Co Inc Compostos de lactama como agonistas selectivos do receptor ep4 para uso no tratamento de doenças e condições mediadas por ep4
PH12015502383B1 (en) 2013-04-19 2023-02-03 Incyte Holdings Corp Bicyclic heterocycles as fgfr inhibitors
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
CN105392505A (zh) 2013-07-19 2016-03-09 开曼化学股份有限公司 用于促进骨生长的方法、系统和组合物
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
CN105793257B (zh) 2013-12-03 2018-11-13 爱杜西亚药品有限公司 苯并咪唑环化合物的晶形及其用途
SI3077391T1 (sl) 2013-12-04 2018-11-30 Idorsia Pharmaceuticals Ltd Uporaba benzimidazol-prolinskih derivatov
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
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
CA2976790C (en) 2015-02-20 2024-02-27 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
EP3808748B1 (en) 2016-06-21 2026-05-20 X4 Pharmaceuticals, Inc. Substituted piperidines as cxcr4-inhibitors
JP6994767B2 (ja) * 2016-06-21 2022-01-14 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
MA49752A (fr) * 2017-08-02 2021-04-21 Vertex Pharma Procédés de préparation de composés de pyrrolidine
RS66310B1 (sr) 2018-05-04 2025-01-31 Incyte Corp Čvrsti oblici inhibitora fgfr i procesi za njegovu pripremu
KR102956194B1 (ko) 2018-05-04 2026-04-23 인사이트 코포레이션 Fgfr 억제제의 염
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
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
GEP20247679B (en) 2019-10-14 2024-10-10 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
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
MX2022006691A (es) 2019-12-04 2022-09-19 Incyte Corp Derivados de un inhibidor de receptores del factor de crecimiento de fibroblastos (fgfr).
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
EP4323405A1 (en) 2021-04-12 2024-02-21 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
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
CA3220274A1 (en) 2021-06-09 2022-12-15 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
TW202409023A (zh) 2022-07-14 2024-03-01 美商富曼西公司 除草苯并𠯤
AU2024387082A1 (en) 2023-11-21 2026-06-04 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

Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006127550A1 (en) * 2005-05-23 2006-11-30 Merck & Co., Inc. Proline bis-amide orexin receptor antagonists
CN101506199A (zh) * 2006-08-15 2009-08-12 埃科特莱茵药品有限公司 用作食欲素受体拮抗剂的氮杂环丁烷化合物
CN101522618A (zh) * 2006-09-29 2009-09-02 埃科特莱茵药品有限公司 3-氮杂-双环[3.1.0]己烷衍生物
WO2009133522A1 (en) * 2008-04-30 2009-11-05 Actelion Pharmaceuticals Ltd Piperidine and pyrrolidine compounds
WO2009150614A1 (en) * 2008-06-11 2009-12-17 Actelion Pharmaceuticals Ltd Tetrazole compounds as orexin receptor antagonists
CN101641342A (zh) * 2007-03-26 2010-02-03 埃科特莱茵药品有限公司 作为食欲素受体拮抗剂的四氢噻唑衍生物
CN101778846A (zh) * 2007-08-15 2010-07-14 埃科特莱茵药品有限公司 作为食欲素拮抗剂的1,2-二酰氨基-乙烯衍生物
CN101796053A (zh) * 2007-07-03 2010-08-04 葛兰素集团有限公司 用作食欲素受体拮抗剂的哌啶衍生物
CN101874030A (zh) * 2007-09-24 2010-10-27 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
WO2010131192A2 (en) * 2009-05-12 2010-11-18 Actelion Pharmaceuticals Ltd Novel oxazolidinone derivatives

Family Cites Families (7)

* 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
WO2004009036A2 (en) * 2002-07-23 2004-01-29 Cytokinetics, Inc. Compounds compositions and methods
RU2378257C2 (ru) 2004-03-01 2010-01-10 Актелион Фармасьютиклз Лтд Замещенные производные 1,2,3,4-тетрагидроизохинолина
EA015256B1 (ru) 2006-03-15 2011-06-30 Актелион Фармасьютикалз Лтд. Производные тетрагидроизохинолина для повышения функции памяти
PE20091010A1 (es) 2007-10-10 2009-08-08 Actelion Pharmaceuticals Ltd Derivados de tetrahidroquinolina
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

Patent Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006127550A1 (en) * 2005-05-23 2006-11-30 Merck & Co., Inc. Proline bis-amide orexin receptor antagonists
CN101506199A (zh) * 2006-08-15 2009-08-12 埃科特莱茵药品有限公司 用作食欲素受体拮抗剂的氮杂环丁烷化合物
CN101522618A (zh) * 2006-09-29 2009-09-02 埃科特莱茵药品有限公司 3-氮杂-双环[3.1.0]己烷衍生物
CN101641342A (zh) * 2007-03-26 2010-02-03 埃科特莱茵药品有限公司 作为食欲素受体拮抗剂的四氢噻唑衍生物
CN101796053A (zh) * 2007-07-03 2010-08-04 葛兰素集团有限公司 用作食欲素受体拮抗剂的哌啶衍生物
CN101778846A (zh) * 2007-08-15 2010-07-14 埃科特莱茵药品有限公司 作为食欲素拮抗剂的1,2-二酰氨基-乙烯衍生物
CN101874030A (zh) * 2007-09-24 2010-10-27 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
WO2009133522A1 (en) * 2008-04-30 2009-11-05 Actelion Pharmaceuticals Ltd Piperidine and pyrrolidine compounds
WO2009150614A1 (en) * 2008-06-11 2009-12-17 Actelion Pharmaceuticals Ltd Tetrazole compounds as orexin receptor antagonists
WO2010131192A2 (en) * 2009-05-12 2010-11-18 Actelion Pharmaceuticals Ltd Novel oxazolidinone derivatives

Non-Patent Citations (11)

* Cited by examiner, † Cited by third party
Title
AMAT,MERCEDES,等: "Preparation of enantiopure 6-(3-indolyl)-2-piperidones and conjugate additions to a 3,4-didehydro derivative", 《TETRAHEDRON》, vol. 53, no. 2, 13 January 1997 (1997-01-13), XP004105174, DOI: doi:10.1016/S0040-4020(96)01014-9 *
AUBE,JEFFREY,等: "Syntheses and rearrangements of spirocyclic oxaziridines derived from unsymmetrical ketones", 《JOURNAL OF ORGANIC CHEMISTRY》, vol. 56, no. 2, 31 January 1991 (1991-01-31), pages 504 - 32 *
BAENS,NICOLE P,等: "Synthesis of 2,5-substituted piperidines: transposition of 1,4-substitution pattern for the analgesic drug R6582", 《TETRAHEDRON》, vol. 49, no. 15, 9 April 1993 (1993-04-09), pages 3194 - 6 *
BAXTER,ELLEN W，等: "Reductive aminations of carbonyl compounds with borohydride and borane reducing agents", 《ORGANIC REACTIONS》, no. 59, 31 December 2008 (2008-12-31) *
CLE´MENT DENHEZ,等: "Asymmetric synthesis of di- and trisubstituted pyrrolidinones via zirconium-mediated intramolecular coupling of N-3-alkenyl carbamates", 《TETRAHEDRON: ASYMMETRY》, vol. 18, no. 3, 21 February 2007 (2007-02-21), pages 424 - 434, XP005922572, DOI: doi:10.1016/j.tetasy.2007.01.026 *
FUWA,HARUHIKO,等: "Concise and short synthesis of functionalized 5,6-dihydropyridin-2-ones by means of palladium(0)-catalyzed cross-coupling of ketene aminal phosphates", 《HETEROCYCLES》, vol. 70, 29 September 2006 (2006-09-29), pages 101 - 106 *
PETERSON, EMILY A,等: "Enantioselective, thiourea-catalyzed intermolecular addition of indoles to cyclic N-acyl iminium ions", 《ANGEWANDTE CHEMIE, INTERNATIONAL EDITION》, vol. 48, no. 34, 16 July 2009 (2009-07-16), pages 6328 - 6331 *
TROISI, LUIGINO,等: "Palladium-catalyzed cyclocarbonylation of unsaturated amines. Chemo- and stereoselective synthesis of N-heteroaryl γ- and δ-lactams", 《ARKIVOC》, no. 6, 31 December 2006 (2006-12-31), XP002527075 *
初晓娜,等: "食欲素(Orexin)的研究进展", 《江西饲料》, no. 02, 28 April 2005 (2005-04-28), pages 1 - 3 *
崔志英,等: "食欲素(Orexin)及其受体(OXR)的特点及功能", 《饲料博览》, no. 03, 25 March 2004 (2004-03-25), pages 7 - 9 *
黄培强,等: "一种基于酰胺α-烷基化反应制备1,5-二取代-2-吡咯烷酮的方法", 《厦门大学学报(自然科学版)》, vol. 36, no. 02, 31 March 1997 (1997-03-31), pages 254 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115047127A (zh) * 2022-04-25 2022-09-13 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
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

Also Published As

Publication number Publication date
JP2013545744A (ja) 2013-12-26
US20130237525A1 (en) 2013-09-12
WO2012063207A1 (en) 2012-05-18
EP2638008A1 (en) 2013-09-18
CA2815179A1 (en) 2012-05-18
US9242970B2 (en) 2016-01-26
JP5847830B2 (ja) 2016-01-27
EP2638008B1 (en) 2015-07-01

Similar Documents

Publication Publication Date Title
JP5847830B2 (ja) オレキシン受容体拮抗薬として有用なラクタム誘導体
KR101247840B1 (ko) 아밀로이드 베타 조절제
US8703934B2 (en) Substituted 4-amino-3,5-dicyano-2-thiopyridines and use thereof
JP4719745B2 (ja) カリウムチャンネル阻害剤
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
CN102498107A (zh) 作为激酶抑制剂的杂芳基化合物
WO2002032872A1 (fr) Composes a noyau aromatique azote
CN109071526A (zh) 哌嗪衍生物的酸加成盐
TW201414727A (zh) 其係［鄰雙（雜）芳基］－［２－（間雙（雜）芳基）吡咯啶－１－基］甲酮衍生物之食慾素受體拮抗劑
CN102993084A (zh) 作为促代谢谷氨酸受体的调节剂的新型炔基衍生物
JP2009523795A (ja) 炎症性障害の処置のためのヒダントイン化合物
JP2011519849A (ja) ピペリジン及びピロリジン化合物
JP2004521072A (ja) 尿素化合物および使用法
KR20110082189A (ko) 아밀로이드 베타의 조절제
CA2044828A1 (en) Inhibitors of hiv reverse transcriptase
EP2001875A2 (en) Glucokinase activators
KR20020016795A (ko) 신규 화합물, 이의 용도 및 이의 제조 방법
CN103781776A (zh) 用作端锚聚合酶抑制剂的新的2-哌啶-1-基-乙酰胺化合物
CN101511796A (zh) 咪唑衍生物
CN102471310A (zh) 用于治疗增生性疾病的联吡啶化合物
US20110021487A1 (en) Cycloalkoxy-substituted 4-phenyl-3,5-dicyanopyridines and their use
CN102482265A (zh) 用于治疗增殖性疾病的吡嗪基吡啶化合物
TW201427968A (zh) 芳香環化合物
TW201625581A (zh) 側氧雜環衍生物
JP2012523380A (ja) Ｈｉｖ複製の阻害薬

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C02 Deemed withdrawal of patent application after publication (patent law 2001)
WD01 Invention patent application deemed withdrawn after publication

Application publication date: 20130710