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)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Diabetes (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 |
|---|---|---|---|
| IBPCT/IB2011/054976 | 2011-11-08 | ||
| 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 |
|---|---|
| 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) | TWI555747B (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 |
|---|---|---|---|---|
| US9440982B2 (en) | 2012-02-07 | 2016-09-13 | Eolas Therapeutics, Inc. | Substituted prolines/piperidines as orexin receptor antagonists |
| JP6346862B2 (ja) | 2012-02-07 | 2018-06-20 | エオラス セラピューティクス， インコーポレイテッド | オレキシンレセプターアンタゴニストとしての置換プロリン／ピペリジン |
| DK2855453T3 (en) | 2012-06-04 | 2017-02-06 | Actelion Pharmaceuticals Ltd | Benzimidazol-proline derivatives |
| 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 |
| 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 |
| 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 |
| SI3077391T1 (sl) | 2013-12-04 | 2018-11-30 | Idorsia Pharmaceuticals Ltd | Uporaba benzimidazol-prolinskih derivatov |
| JP5907310B2 (ja) * | 2013-12-13 | 2016-04-26 | 大正製薬株式会社 | オキサジナン化合物の結晶形及びその製造方法 |
| 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 |
| US9968624B2 (en) | 2014-05-16 | 2018-05-15 | The University Of Tokyo | Depression treatment agent |
| 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 |
| US10894789B2 (en) | 2016-02-12 | 2021-01-19 | Astrazeneca Ab | Halo-substituted piperidines as orexin receptor modulators |
| MX392154B (es) | 2017-05-03 | 2025-03-21 | Idorsia Pharmaceuticals Ltd | Preparacion de derivados de acido 2-([1,2,3]triazol-2-il)-benzoico. |
| 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 |
| WO2023218023A1 (en) * | 2022-05-13 | 2023-11-16 | Idorsia Pharmaceuticals Ltd | Thiazoloaryl-methyl substituted cyclic hydrazine-n-carboxamide derivatives |
| 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 |
| CN121057722A (zh) * | 2023-04-10 | 2025-12-02 | 三菱瓦斯化学株式会社 | 化合物、组合物、显现增敏效果的方法和制造方法 |
| GB202311281D0 (en) | 2023-07-21 | 2023-09-06 | Bial Portela & Ca Sa | Orexin receptor antagonists |
| GB202311280D0 (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 |
| AU676993B2 (en) | 1991-06-27 | 1997-04-10 | Virginia Commonwealth University | Sigma receptor ligands and the use thereof |
| US20040192673A1 (en) | 2001-05-05 | 2004-09-30 | Pascale Gaillard | N-aroyl cyclic amine derivatives as orexin receptor antagonists |
| GB0115862D0 (en) * | 2001-06-28 | 2001-08-22 | Smithkline Beecham Plc | Compounds |
| US7470710B2 (en) * | 2001-06-28 | 2008-12-30 | Smithkline Beecham P.L.C. | N-aroyl cyclic amine derivatives as orexin receptor antagonists |
| GB0124463D0 (en) * | 2001-10-11 | 2001-12-05 | Smithkline Beecham Plc | Compounds |
| GB0130335D0 (en) * | 2001-12-19 | 2002-02-06 | Smithkline Beecham Plc | Compounds |
| 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 |
| 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 |
| US8288411B2 (en) | 2007-09-24 | 2012-10-16 | Actelion Pharmaceuticals Ltd. | Pyrrolidines and piperidines as orexin receptor antagonists |
| PE20091010A1 (es) | 2007-10-10 | 2009-08-08 | Actelion Pharmaceuticals Ltd | Derivados de tetrahidroquinolina |
| JP2012506374A (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 |
| WO2010048013A1 (en) * | 2008-10-21 | 2010-04-29 | Merck Sharp & Dohme Corp. | 2,5-disubstituted morpholine orexin receptor antagonists |
| AU2009307915A1 (en) | 2008-10-21 | 2010-04-29 | Merck Sharp & Dohme Corp. | 2,5-disubstituted piperidine orexin receptor antagonists |
| 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 |
| KR20110091581A (ko) | 2008-12-02 | 2011-08-11 | 글락소 그룹 리미티드 | Ｎ-｛［1ｒ,4ｓ,6ｒ-3-(2-피리디닐카르보닐)-3-아자비시클로［4.1.0］헵트-4-일］메틸｝-2-헤테로아릴아민 유도체 및 그의 용도 |
| EP2491034B1 (en) | 2009-10-23 | 2013-12-18 | Janssen Pharmaceutica, N.V. | Fused heterocyclic compounds as orexin receptor modulators |
| ME03452B (me) | 2009-10-23 | 2020-01-20 | Janssen Pharmaceutica Nv | Disupstituisani oktahi-dropirolo[3,4-c]piroli kao modulatori oreksin receptora |
| EP2491031B1 (en) | 2009-10-23 | 2013-08-07 | Janssen Pharmaceutica N.V. | Fused heterocyclic compounds as orexin receptor modulators |
-
2012
- 2012-11-07 SI SI201230556A patent/SI2776430T1/sl unknown
- 2012-11-07 PL PL12791862.1T patent/PL2776430T3/pl unknown
- 2012-11-07 KR KR1020147014960A patent/KR101676930B1/ko not_active Expired - Fee Related
- 2012-11-07 IN IN4127CHN2014 patent/IN2014CN04127A/en unknown
- 2012-11-07 MX MX2014005635A patent/MX343837B/es active IP Right Grant
- 2012-11-07 BR BR112014010617-7A patent/BR112014010617B1/pt not_active IP Right Cessation
- 2012-11-07 JP JP2014540606A patent/JP5718535B2/ja active Active
- 2012-11-07 UA UAA201402001A patent/UA112317C2/uk unknown
- 2012-11-07 AU AU2012335194A patent/AU2012335194B2/en not_active Ceased
- 2012-11-07 CA CA2846568A patent/CA2846568C/en active Active
- 2012-11-07 PH PH1/2014/500852A patent/PH12014500852A1/en unknown
- 2012-11-07 EA EA201400553A patent/EA024106B1/ru not_active IP Right Cessation
- 2012-11-07 TW TW101141421A patent/TWI555747B/zh not_active IP Right Cessation
- 2012-11-07 CN CN201280054325.7A patent/CN103917538B/zh not_active Expired - Fee Related
- 2012-11-07 HU HUE12791862A patent/HUE029239T2/en unknown
- 2012-11-07 DK DK12791862.1T patent/DK2776430T3/en active
- 2012-11-07 WO PCT/IB2012/056218 patent/WO2013068935A1/en not_active Ceased
- 2012-11-07 ES ES12791862.1T patent/ES2572703T3/es active Active
- 2012-11-07 US US14/357,159 patent/US9150566B2/en active Active
- 2012-11-07 AR ARP120104193A patent/AR088692A1/es active IP Right Grant
- 2012-11-07 EP EP12791862.1A patent/EP2776430B1/en active Active
- 2012-11-07 TW TW105118634A patent/TWI565703B/zh not_active IP Right Cessation
- 2012-11-07 MY MYPI2014701155A patent/MY167791A/en unknown
- 2012-11-07 HR HRP20160678TT patent/HRP20160678T1/hr unknown
- 2012-11-07 SG SG11201401665WA patent/SG11201401665WA/en unknown
-
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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| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |