AU2012335194B2 - 2-(1,2,3-triazol-2-yl)benzamide and 3-(1,2,3-triazol-2-yl)picolinamide derivatives as orexin receptor antagonists - Google Patents

2-(1,2,3-triazol-2-yl)benzamide and 3-(1,2,3-triazol-2-yl)picolinamide derivatives as orexin receptor antagonists Download PDF

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Publication number
AU2012335194B2
AU2012335194B2 AU2012335194A AU2012335194A AU2012335194B2 AU 2012335194 B2 AU2012335194 B2 AU 2012335194B2 AU 2012335194 A AU2012335194 A AU 2012335194A AU 2012335194 A AU2012335194 A AU 2012335194A AU 2012335194 B2 AU2012335194 B2 AU 2012335194B2
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Prior art keywords
triazol
benzyl
morpholin
phenyl
methanone
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AU2012335194A
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AU2012335194A1 (en
Inventor
Martin Bolli
Christoph Boss
Christine Brotschi
Bibia Heidmann
Thierry Sifferlen
Jodi T. Williams
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Idorsia Pharmaceuticals Ltd
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Idorsia Pharmaceuticals Ltd
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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)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Addiction (AREA)
  • Child & Adolescent Psychology (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)
AU2012335194A 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 Ceased AU2012335194B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
IB2011054976 2011-11-08
IBPCT/IB2011/054976 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)

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AU2012335194A1 AU2012335194A1 (en) 2014-07-03
AU2012335194B2 true AU2012335194B2 (en) 2017-05-25

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AU2012335194A Ceased AU2012335194B2 (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

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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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WO2013119639A1 (en) 2012-02-07 2013-08-15 Eolas Therapeutics, Inc. Substituted prolines / piperidines as orexin receptor antagonists
US9440982B2 (en) 2012-02-07 2016-09-13 Eolas Therapeutics, Inc. Substituted prolines/piperidines as orexin receptor antagonists
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
CN105051040A (zh) 2013-03-12 2015-11-11 埃科特莱茵药品有限公司 作为食欲素受体拮抗剂的氮杂环丁烷酰胺衍生物
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
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
KR102330133B1 (ko) 2013-12-04 2021-11-23 이도르시아 파마슈티컬스 리미티드 벤즈이미다졸-프롤린 유도체의 용도
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
CN105814042B (zh) * 2013-12-13 2018-09-28 大正制药株式会社 噁嗪烷化合物的晶形及其制造方法
JP6323886B2 (ja) 2014-05-16 2018-05-16 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
SG11201804223TA (en) 2015-11-23 2018-06-28 Sunshine Lake Pharma Co Ltd OCTAHYDROPYRROLO [3, 4-c] PYRROLE DERIVATIVES AND USES THEREOF
LT3414241T (lt) 2016-02-12 2022-08-25 Astrazeneca Ab Halogenu pakeisti piperidinai kaip oreksino receptoriaus moduliatoriai
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
CA3206675A1 (en) * 2021-02-02 2022-08-11 Markus Von Raumer 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
KR20260006548A (ko) * 2023-04-10 2026-01-13 미쯔비시 가스 케미칼 컴파니, 인코포레이티드 화합물, 조성물, 증감 효과를 발현하는 방법 및 제조방법
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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Also Published As

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TW201632517A (zh) 2016-09-16
ES2572703T3 (es) 2016-06-01
MY167791A (en) 2018-09-26
HUE029239T2 (en) 2017-02-28
TWI555747B (zh) 2016-11-01
NZ625896A (en) 2016-04-29
EP2776430A1 (en) 2014-09-17
JP5718535B2 (ja) 2015-05-13
DK2776430T3 (en) 2016-05-09
MX2014005635A (es) 2014-06-23
CY1117638T1 (el) 2017-04-26
EA201400553A1 (ru) 2014-10-30
PL2776430T3 (pl) 2016-09-30
EP2776430B1 (en) 2016-03-16
EA024106B1 (ru) 2016-08-31
UA112317C2 (uk) 2016-08-25
AU2012335194A1 (en) 2014-07-03
BR112014010617A8 (pt) 2017-12-26
PH12014500852A1 (en) 2016-03-02
KR101676930B1 (ko) 2016-11-16
KR20140096338A (ko) 2014-08-05
BR112014010617A2 (pt) 2017-04-25
IL232462A0 (en) 2014-06-30
IN2014CN04127A (enExample) 2015-07-10
CL2014000659A1 (es) 2014-08-18
HK1199022A1 (zh) 2015-06-19
IL232462A (en) 2016-11-30
CN103917538A (zh) 2014-07-09
JP2014532753A (ja) 2014-12-08
BR112014010617B1 (pt) 2021-12-14
TWI565703B (zh) 2017-01-11
US20150158855A1 (en) 2015-06-11
US9150566B2 (en) 2015-10-06
CA2846568A1 (en) 2013-05-16
MX343837B (es) 2016-11-24
AR088692A1 (es) 2014-06-25
SI2776430T1 (sl) 2016-06-30
TW201323421A (zh) 2013-06-16
CN103917538B (zh) 2016-08-24
ZA201404189B (en) 2017-08-30
WO2013068935A1 (en) 2013-05-16
SG11201401665WA (en) 2014-09-26
HRP20160678T1 (hr) 2016-07-15
CA2846568C (en) 2020-01-14

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