JP5718535B2 - オレキシン受容体アンタゴニストとしての２−（１，２，３−トリアゾール−２−イル）ベンズアミド及び３−（１，２，３−トリアゾール−２−イル）ピコリンアミド誘導体 - Google Patents
オレキシン受容体アンタゴニストとしての２−（１，２，３−トリアゾール−２−イル）ベンズアミド及び３−（１，２，３−トリアゾール−２−イル）ピコリンアミド誘導体 Download PDFInfo
- Publication number
- JP5718535B2 JP5718535B2 JP2014540606A JP2014540606A JP5718535B2 JP 5718535 B2 JP5718535 B2 JP 5718535B2 JP 2014540606 A JP2014540606 A JP 2014540606A JP 2014540606 A JP2014540606 A JP 2014540606A JP 5718535 B2 JP5718535 B2 JP 5718535B2
- Authority
- JP
- Japan
- Prior art keywords
- triazol
- benzyl
- phenyl
- methanone
- morpholin
- 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.)
- Active
Links
- XSRLTWBCMOYCSY-MLWJPKLSSA-N CCC(COC1)N(C)[C@@H]1I Chemical compound CCC(COC1)N(C)[C@@H]1I XSRLTWBCMOYCSY-MLWJPKLSSA-N 0.000 description 1
- IEKBTRIPIOGCEZ-CZEFRNQJSA-N CCC1N(C)C[C@@]2(C(CC3O[C@@H](C)CN(C)[C@@H]3C)C2)OC1 Chemical compound CCC1N(C)C[C@@]2(C(CC3O[C@@H](C)CN(C)[C@@H]3C)C2)OC1 IEKBTRIPIOGCEZ-CZEFRNQJSA-N 0.000 description 1
Classifications
-
- 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
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic 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
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
-
- 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
- A61P25/26—Psychostimulants, e.g. nicotine, cocaine
-
- 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
-
- 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
-
- 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
-
- 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
- C07D413/14—Heterocyclic 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
-
- 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)
- 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)
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)
| Publication Number | Publication Date |
|---|---|
| JP2014532753A JP2014532753A (ja) | 2014-12-08 |
| JP5718535B2 true JP5718535B2 (ja) | 2015-05-13 |
Family
ID=47258050
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014540606A Active JP5718535B2 (ja) | 2011-11-08 | 2012-11-07 | オレキシン受容体アンタゴニストとしての２−（１，２，３−トリアゾール−２−イル）ベンズアミド及び３−（１，２，３−トリアゾール−２−イル）ピコリンアミド誘導体 |
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) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5130432A (en) | 1990-12-21 | 1992-07-14 | Syntex (U.S.A.) Inc. | Process for preparing cyclic amines and intermediate products thereof |
| JPH06509069A (ja) | 1991-06-27 | 1994-10-13 | バージニア・コモンウェルス・ユニバーシティ | シグマレセプターリガンドおよびその用途 |
| WO2002089800A2 (en) * | 2001-05-05 | 2002-11-14 | Smithkline Beecham P.L.C. | N-aroyl cyclic amine derivatives as orexin receptor antagonists |
| WO2003002561A1 (en) * | 2001-06-28 | 2003-01-09 | Smithkline Beecham P.L.C. | N-aroyl cyclic amine derivatives as orexin receptor antagonists |
| GB0115862D0 (en) * | 2001-06-28 | 2001-08-22 | Smithkline Beecham Plc | Compounds |
| GB0124463D0 (en) * | 2001-10-11 | 2001-12-05 | Smithkline Beecham Plc | Compounds |
| GB0130335D0 (en) * | 2001-12-19 | 2002-02-06 | Smithkline Beecham Plc | Compounds |
| 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 |
| EP1998774A1 (en) | 2006-03-15 | 2008-12-10 | Actelion Pharmaceuticals Ltd. | Tetrahydroisoquinoline derivatives to enhance memory function |
| EP2049110B1 (en) | 2006-07-14 | 2014-08-20 | Merck Sharp & Dohme Corp. | Bridged diazepan orexin receptor antagonists |
| GB0620818D0 (en) | 2006-10-19 | 2006-11-29 | Ucb Sa | Therapeutic agents |
| PE20081229A1 (es) | 2006-12-01 | 2008-08-28 | Merck & Co Inc | Antagonistas de receptor de orexina de diazepam sustituido |
| 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 |
| CA2739915A1 (en) | 2008-10-21 | 2010-04-29 | Merck Sharp & Dohme Corp. | 2,5-disubstituted piperidine orexin receptor antagonists |
| AU2009307916A1 (en) * | 2008-10-21 | 2010-04-29 | Merck Sharp & Dohme Corp. | 2,5-disubstituted morpholine orexin receptor antagonists |
| JP2012506375A (ja) | 2008-10-21 | 2012-03-15 | メルク・シャープ・エンド・ドーム・コーポレイション | ２，５−二置換ピペリジンオレキシン受容体アンタゴニスト |
| CA2745433A1 (en) | 2008-12-02 | 2010-06-10 | Glaxo Group Ltd. | N-{[(ir,4s,6r-3-(2-pyridinylcarbonyl)-3-azabicyclo [4.1.0]hept-4-yl] methyl}-2-heteroarylamine derivatives and uses thereof |
| TW201031407A (en) | 2008-12-02 | 2010-09-01 | Glaxo Group Ltd | Novel compounds |
| ES2585806T3 (es) | 2009-10-23 | 2016-10-10 | Janssen Pharmaceutica N.V. | Octahidropirrolo [3,4-c] pirroles disustituidos como moduladores de receptores de orexina |
| WO2011050202A1 (en) | 2009-10-23 | 2011-04-28 | Janssen Pharmaceutica Nv | Fused heterocyclic compounds as orexin receptor modulators |
| EP2491034B1 (en) | 2009-10-23 | 2013-12-18 | Janssen Pharmaceutica, N.V. | Fused heterocyclic compounds as orexin receptor modulators |
-
2012
- 2012-11-07 DK DK12791862.1T patent/DK2776430T3/en active
- 2012-11-07 UA UAA201402001A patent/UA112317C2/uk unknown
- 2012-11-07 AU AU2012335194A patent/AU2012335194B2/en not_active Ceased
- 2012-11-07 IN IN4127CHN2014 patent/IN2014CN04127A/en unknown
- 2012-11-07 PL PL12791862.1T patent/PL2776430T3/pl unknown
- 2012-11-07 SI SI201230556A patent/SI2776430T1/sl unknown
- 2012-11-07 KR KR1020147014960A patent/KR101676930B1/ko not_active Expired - Fee Related
- 2012-11-07 EA EA201400553A patent/EA024106B1/ru not_active IP Right Cessation
- 2012-11-07 ES ES12791862.1T patent/ES2572703T3/es active Active
- 2012-11-07 AR ARP120104193A patent/AR088692A1/es active IP Right Grant
- 2012-11-07 MY MYPI2014701155A patent/MY167791A/en unknown
- 2012-11-07 JP JP2014540606A patent/JP5718535B2/ja active Active
- 2012-11-07 CN CN201280054325.7A patent/CN103917538B/zh not_active Expired - Fee Related
- 2012-11-07 CA CA2846568A patent/CA2846568C/en active Active
- 2012-11-07 HU HUE12791862A patent/HUE029239T2/en unknown
- 2012-11-07 MX MX2014005635A patent/MX343837B/es active IP Right Grant
- 2012-11-07 TW TW105118634A patent/TWI565703B/zh not_active IP Right Cessation
- 2012-11-07 PH PH1/2014/500852A patent/PH12014500852A1/en unknown
- 2012-11-07 US US14/357,159 patent/US9150566B2/en active Active
- 2012-11-07 EP EP12791862.1A patent/EP2776430B1/en active Active
- 2012-11-07 WO PCT/IB2012/056218 patent/WO2013068935A1/en not_active Ceased
- 2012-11-07 TW TW101141421A patent/TWI555747B/zh not_active IP Right Cessation
- 2012-11-07 HR HRP20160678TT patent/HRP20160678T1/hr unknown
- 2012-11-07 SG SG11201401665WA patent/SG11201401665WA/en unknown
- 2012-11-07 BR BR112014010617-7A patent/BR112014010617B1/pt not_active IP Right Cessation
-
2014
- 2014-03-18 CL CL2014000659A patent/CL2014000659A1/es unknown
- 2014-05-05 IL IL232462A patent/IL232462A/en active IP Right Grant
- 2014-06-06 ZA ZA2014/04189A patent/ZA201404189B/en unknown
-
2016
- 2016-06-15 CY CY20161100527T patent/CY1117638T1/el unknown
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