EA024106B1 - Производные 2-(1,2,3-триазол-2-ил)бензамида и 3-(1,2,3-триазол-2-ил)пиколинамида - Google Patents

Производные 2-(1,2,3-триазол-2-ил)бензамида и 3-(1,2,3-триазол-2-ил)пиколинамида Download PDF

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Publication number
EA024106B1
EA024106B1 EA201400553A EA201400553A EA024106B1 EA 024106 B1 EA024106 B1 EA 024106B1 EA 201400553 A EA201400553 A EA 201400553A EA 201400553 A EA201400553 A EA 201400553A EA 024106 B1 EA024106 B1 EA 024106B1
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EA
Eurasian Patent Office
Prior art keywords
triazol
benzyl
methanone
phenyl
morpholin
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EA201400553A
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English (en)
Russian (ru)
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EA201400553A1 (ru
Inventor
Мартин Болли
Кристоф Босс
Кристине Брочи
Бибия Хайдманн
Тьерри Зифферлен
Джоди Т. Уилльямс
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Актелион Фармасьютиклз Лтд.
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Application filed by Актелион Фармасьютиклз Лтд. filed Critical Актелион Фармасьютиклз Лтд.
Publication of EA201400553A1 publication Critical patent/EA201400553A1/ru
Publication of EA024106B1 publication Critical patent/EA024106B1/ru

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    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • 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
    • A61P25/26Psychostimulants, e.g. nicotine, cocaine
    • 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
    • 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
    • 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
    • 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
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Addiction (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
EA201400553A 2011-11-08 2012-11-07 Производные 2-(1,2,3-триазол-2-ил)бензамида и 3-(1,2,3-триазол-2-ил)пиколинамида EA024106B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IB2011054976 2011-11-08
PCT/IB2012/056218 WO2013068935A1 (en) 2011-11-08 2012-11-07 2-(1,2,3-triazol-2-yl)benzamide and 3-(1,2,3-triazol-2-yl)picolinamide derivatives as orexin receptor antagonists

Publications (2)

Publication Number Publication Date
EA201400553A1 EA201400553A1 (ru) 2014-10-30
EA024106B1 true EA024106B1 (ru) 2016-08-31

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EA201400553A EA024106B1 (ru) 2011-11-08 2012-11-07 Производные 2-(1,2,3-триазол-2-ил)бензамида и 3-(1,2,3-триазол-2-ил)пиколинамида

Country Status (28)

Country Link
US (1) US9150566B2 (enExample)
EP (1) EP2776430B1 (enExample)
JP (1) JP5718535B2 (enExample)
KR (1) KR101676930B1 (enExample)
CN (1) CN103917538B (enExample)
AR (1) AR088692A1 (enExample)
AU (1) AU2012335194B2 (enExample)
BR (1) BR112014010617B1 (enExample)
CA (1) CA2846568C (enExample)
CL (1) CL2014000659A1 (enExample)
CY (1) CY1117638T1 (enExample)
DK (1) DK2776430T3 (enExample)
EA (1) EA024106B1 (enExample)
ES (1) ES2572703T3 (enExample)
HR (1) HRP20160678T1 (enExample)
HU (1) HUE029239T2 (enExample)
IL (1) IL232462A (enExample)
IN (1) IN2014CN04127A (enExample)
MX (1) MX343837B (enExample)
MY (1) MY167791A (enExample)
PH (1) PH12014500852A1 (enExample)
PL (1) PL2776430T3 (enExample)
SG (1) SG11201401665WA (enExample)
SI (1) SI2776430T1 (enExample)
TW (2) TWI565703B (enExample)
UA (1) UA112317C2 (enExample)
WO (1) WO2013068935A1 (enExample)
ZA (1) ZA201404189B (enExample)

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RU2014136339A (ru) 2012-02-07 2016-03-27 Иолас Терапьютикс, Инк. Замещенные пролины/пиперидины как антагонисты орексиновых рецепторов
KR101995683B1 (ko) 2012-06-04 2019-07-02 이도르시아 파마슈티컬스 리미티드 벤즈이미다졸-프롤린 유도체
EP2970241A1 (en) 2013-03-12 2016-01-20 Actelion Pharmaceuticals Ltd. Azetidine amide derivatives as orexin receptor antagonists
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
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
HK1225734B (en) 2013-12-04 2017-09-15 Idorsia Pharmaceuticals Ltd Use of benzimidazole-proline derivatives
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JP2017024990A (ja) * 2013-12-13 2017-02-02 大正製薬株式会社 オキサゾリジン及びオキサジナン誘導体
WO2015174532A1 (ja) * 2014-05-16 2015-11-19 国立大学法人 東京大学 うつ治療剤
TW201613902A (en) 2014-08-13 2016-04-16 Eolas Therapeutics Inc Difluoropyrrolidines as orexin receptor modulators
WO2016095205A1 (en) 2014-12-19 2016-06-23 Merck Sharp & Dohme Corp. Heteroaryl orexin receptor antagonists
CN104557744B (zh) * 2014-12-23 2017-04-12 广东东阳光药业有限公司 一种三氮唑化合物的制备方法
US10370380B2 (en) 2015-11-23 2019-08-06 Sunshine Lake Pharma Co., Ltd. Octahydropyrrolo[3,4-c]pyrrole derivatives and uses thereof
CN109219606B (zh) 2016-02-12 2021-10-01 阿斯利康(瑞典)有限公司 食欲素受体调节剂的卤素取代的哌啶
KR102582197B1 (ko) 2017-05-03 2023-09-22 이도르시아 파마슈티컬스 리미티드 2-([1,2,3]트리아졸-2-일)-벤조산 유도체의 제조
WO2020099511A1 (en) * 2018-11-14 2020-05-22 Idorsia Pharmaceuticals Ltd Benzimidazole-2-methyl-morpholine derivatives
GB201901142D0 (en) 2019-01-28 2019-03-20 Heptares Therapeutics Ltd OX1 Antagonists
WO2022167330A1 (en) 2021-02-02 2022-08-11 Idorsia Pharmaceuticals Ltd A crystalline form of (4-methyl-2-[1,2,3]triazol-2-yl-phenyl)-[(r)-3-(3-[1,2,3]triazol-2-yl-benzyl)-morpholin-4-yl]-methanone
TW202400149A (zh) * 2022-05-13 2024-01-01 瑞士商愛杜西亞製藥有限公司 經噻唑并芳基-甲基取代之環狀肼-n-甲醯胺衍生物
CN115947697A (zh) * 2022-12-28 2023-04-11 苏州汉德创宏生化科技有限公司 一种3-氧代吗啉-4-羧酸叔丁酯的合成方法
WO2024214321A1 (ja) * 2023-04-10 2024-10-17 三菱瓦斯化学株式会社 化合物、組成物、増感効果を発現する方法および製造方法
GB202311280D0 (en) 2023-07-21 2023-09-06 Bial Portela & Ca Sa Orexin receptor antagonists
GB202311281D0 (en) 2023-07-21 2023-09-06 Bial Portela & Ca Sa Orexin receptor antagonists

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WO2003002559A2 (en) * 2001-06-28 2003-01-09 Smithkline Beecham P.L.C. Piperidine compounds for use as orexin receptor antagonist
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WO2003032991A1 (en) * 2001-10-11 2003-04-24 Smithkline Beecham Plc N-aroyl piperazine derivatives as orexin receptor antagonists
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WO2010048013A1 (en) * 2008-10-21 2010-04-29 Merck Sharp & Dohme Corp. 2,5-disubstituted morpholine orexin receptor antagonists
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Publication number Priority date Publication date Assignee Title
WO2002089800A2 (en) * 2001-05-05 2002-11-14 Smithkline Beecham P.L.C. N-aroyl cyclic amine derivatives as orexin receptor antagonists
WO2003002559A2 (en) * 2001-06-28 2003-01-09 Smithkline Beecham P.L.C. Piperidine compounds for use as orexin receptor antagonist
WO2003002561A1 (en) * 2001-06-28 2003-01-09 Smithkline Beecham P.L.C. N-aroyl cyclic amine derivatives as orexin receptor antagonists
WO2003032991A1 (en) * 2001-10-11 2003-04-24 Smithkline Beecham Plc N-aroyl piperazine derivatives as orexin receptor antagonists
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Also Published As

Publication number Publication date
WO2013068935A1 (en) 2013-05-16
IN2014CN04127A (enExample) 2015-07-10
CA2846568A1 (en) 2013-05-16
MX2014005635A (es) 2014-06-23
UA112317C2 (uk) 2016-08-25
JP2014532753A (ja) 2014-12-08
AU2012335194B2 (en) 2017-05-25
SI2776430T1 (sl) 2016-06-30
TWI565703B (zh) 2017-01-11
EP2776430B1 (en) 2016-03-16
EP2776430A1 (en) 2014-09-17
BR112014010617A8 (pt) 2017-12-26
AU2012335194A1 (en) 2014-07-03
SG11201401665WA (en) 2014-09-26
BR112014010617B1 (pt) 2021-12-14
CL2014000659A1 (es) 2014-08-18
CA2846568C (en) 2020-01-14
CY1117638T1 (el) 2017-04-26
CN103917538B (zh) 2016-08-24
KR20140096338A (ko) 2014-08-05
NZ625896A (en) 2016-04-29
KR101676930B1 (ko) 2016-11-16
TW201323421A (zh) 2013-06-16
IL232462A0 (en) 2014-06-30
JP5718535B2 (ja) 2015-05-13
TWI555747B (zh) 2016-11-01
US9150566B2 (en) 2015-10-06
IL232462A (en) 2016-11-30
HK1199022A1 (zh) 2015-06-19
ZA201404189B (en) 2017-08-30
TW201632517A (zh) 2016-09-16
MY167791A (en) 2018-09-26
PH12014500852A1 (en) 2016-03-02
HUE029239T2 (en) 2017-02-28
DK2776430T3 (en) 2016-05-09
BR112014010617A2 (pt) 2017-04-25
CN103917538A (zh) 2014-07-09
ES2572703T3 (es) 2016-06-01
MX343837B (es) 2016-11-24
AR088692A1 (es) 2014-06-25
US20150158855A1 (en) 2015-06-11
HRP20160678T1 (hr) 2016-07-15
EA201400553A1 (ru) 2014-10-30
PL2776430T3 (pl) 2016-09-30

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