CN103917538B - 2-(1,2,3-三唑-2-基)苯甲酰胺及3-(1,2,3-三唑-2-基)吡啶酰胺衍生物 - Google Patents
2-(1,2,3-三唑-2-基)苯甲酰胺及3-(1,2,3-三唑-2-基)吡啶酰胺衍生物 Download PDFInfo
- Publication number
- CN103917538B CN103917538B CN201280054325.7A CN201280054325A CN103917538B CN 103917538 B CN103917538 B CN 103917538B CN 201280054325 A CN201280054325 A CN 201280054325A CN 103917538 B CN103917538 B CN 103917538B
- Authority
- CN
- China
- 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.)
- Expired - Fee Related
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
- A61K31/395—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
- C07D413/14—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)
- 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)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Psychiatry (AREA)
- Obesity (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)
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 |
|---|---|
| CN103917538A CN103917538A (zh) | 2014-07-09 |
| CN103917538B true CN103917538B (zh) | 2016-08-24 |
Family
ID=47258050
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201280054325.7A Expired - Fee Related CN103917538B (zh) | 2011-11-08 | 2012-11-07 | 2-(1,2,3-三唑-2-基)苯甲酰胺及3-(1,2,3-三唑-2-基)吡啶酰胺衍生物 |
Country Status (28)
| Country | Link |
|---|---|
| US (1) | US9150566B2 (https=) |
| EP (1) | EP2776430B1 (https=) |
| JP (1) | JP5718535B2 (https=) |
| KR (1) | KR101676930B1 (https=) |
| CN (1) | CN103917538B (https=) |
| AR (1) | AR088692A1 (https=) |
| AU (1) | AU2012335194B2 (https=) |
| BR (1) | BR112014010617B1 (https=) |
| CA (1) | CA2846568C (https=) |
| CL (1) | CL2014000659A1 (https=) |
| CY (1) | CY1117638T1 (https=) |
| DK (1) | DK2776430T3 (https=) |
| EA (1) | EA024106B1 (https=) |
| ES (1) | ES2572703T3 (https=) |
| HR (1) | HRP20160678T1 (https=) |
| HU (1) | HUE029239T2 (https=) |
| IL (1) | IL232462A (https=) |
| IN (1) | IN2014CN04127A (https=) |
| MX (1) | MX343837B (https=) |
| MY (1) | MY167791A (https=) |
| PH (1) | PH12014500852A1 (https=) |
| PL (1) | PL2776430T3 (https=) |
| SG (1) | SG11201401665WA (https=) |
| SI (1) | SI2776430T1 (https=) |
| TW (2) | TWI565703B (https=) |
| UA (1) | UA112317C2 (https=) |
| WO (1) | WO2013068935A1 (https=) |
| ZA (1) | ZA201404189B (https=) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2863413A1 (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 |
| ES2617863T3 (es) | 2012-06-04 | 2017-06-20 | Actelion Pharmaceuticals Ltd. | Derivados de bencimidazol-prolina |
| CA2902135A1 (en) | 2013-03-12 | 2014-09-18 | Actelion Pharmaceuticals Ltd | Azetidine amide derivatives as orexin receptor antagonists |
| MY179862A (en) | 2013-12-03 | 2020-11-18 | 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 |
| SI3077391T1 (sl) | 2013-12-04 | 2018-11-30 | Idorsia Pharmaceuticals Ltd | Uporaba benzimidazol-prolinskih derivatov |
| WO2015087853A1 (ja) * | 2013-12-13 | 2015-06-18 | 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 |
| WO2015174532A1 (ja) * | 2014-05-16 | 2015-11-19 | 国立大学法人 東京大学 | うつ治療剤 |
| UY36272A (es) | 2014-08-13 | 2016-02-29 | Eolas Therapeutics Inc | Difluoropirrolidinas como moduladores de los receptores de orexinas |
| 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 |
| AU2016360245B2 (en) | 2015-11-23 | 2020-07-09 | Sunshine Lake Pharma Co., Ltd. | Octahydropyrrolo [3, 4-c] pyrrole derivatives and uses thereof |
| AU2017217931B2 (en) | 2016-02-12 | 2020-10-22 | Astrazeneca Ab | Halo-substituted piperidines as orexin receptor modulators |
| LT3619199T (lt) | 2017-05-03 | 2021-09-27 | Idorsia Pharmaceuticals Ltd | 2-([1,2,3]triazol-2-il)-benzenkarboksirūgšties darinių gamyba |
| 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 |
| AR129309A1 (es) * | 2022-05-13 | 2024-08-07 | Idorsia Pharmaceuticals Ltd | Derivados de hidrazina-n-carboxamida cíclica sustituida con tiazoloaril-metilo |
| 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 |
| JPWO2024214321A1 (https=) * | 2023-04-10 | 2024-10-17 | ||
| 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 |
Citations (7)
| 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 |
| WO2003032991A1 (en) * | 2001-10-11 | 2003-04-24 | Smithkline Beecham Plc | N-aroyl piperazine derivatives as orexin receptor antagonists |
| WO2003051368A1 (en) * | 2001-12-19 | 2003-06-26 | Smithkline Beecham Plc | N-aroyl cyclic amine derivatives as orexin receptor antagonists |
| CN1549816A (zh) * | 2001-06-28 | 2004-11-24 | ʷ | 作为阿立新受体拮抗药的n-芳酰基环胺衍生物 |
| WO2010048010A1 (en) * | 2008-10-21 | 2010-04-29 | Merck Sharp & Dohme Corp. | 2,5-disubstituted piperidine orexin receptor antagonists |
| WO2010048013A1 (en) * | 2008-10-21 | 2010-04-29 | Merck Sharp & Dohme Corp. | 2,5-disubstituted morpholine orexin receptor antagonists |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
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| 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 |
| CA2557163C (en) | 2004-03-01 | 2011-08-16 | Idorsia Pharmaceuticals Ltd | Substituted 1,2,3,4-tetrahydroisoquinoline derivatives |
| AU2007226203A1 (en) | 2006-03-15 | 2007-09-20 | 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 |
| JP2010540429A (ja) | 2007-09-24 | 2010-12-24 | アクテリオン ファーマシューティカルズ リミテッド | オレキシン受容体拮抗薬としてのピロリジン類及びピペリジン類 |
| PE20091010A1 (es) | 2007-10-10 | 2009-08-08 | Actelion Pharmaceuticals Ltd | Derivados de tetrahidroquinolina |
| US8710076B2 (en) | 2008-10-21 | 2014-04-29 | Merck Sharp & Dohme Corp. | 2,5-disubstituted piperidine orexin receptor antagonists |
| US20100144760A1 (en) | 2008-12-02 | 2010-06-10 | Giuseppe Alvaro | Novel compounds |
| AU2009324238A1 (en) | 2008-12-02 | 2010-06-10 | Glaxo Group Limited | N-{[(IR,4S,6R-3-(2-pyridinylcarbonyl)-3-azabicyclo [4.1.0] hept-4-yl] methyl}-2-heteroarylamine derivatives and uses thereof |
| JP5847087B2 (ja) | 2009-10-23 | 2016-01-20 | ヤンセン ファーマシューティカ エヌ．ベー． | オレキシン受容体調節因子としての縮合複素環式化合物 |
| WO2011050202A1 (en) | 2009-10-23 | 2011-04-28 | Janssen Pharmaceutica Nv | 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 |
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2012
- 2012-11-07 ES ES12791862.1T patent/ES2572703T3/es active Active
- 2012-11-07 JP JP2014540606A patent/JP5718535B2/ja active Active
- 2012-11-07 UA UAA201402001A patent/UA112317C2/uk unknown
- 2012-11-07 CN CN201280054325.7A patent/CN103917538B/zh not_active Expired - Fee Related
- 2012-11-07 TW TW105118634A patent/TWI565703B/zh not_active IP Right Cessation
- 2012-11-07 SG SG11201401665WA patent/SG11201401665WA/en unknown
- 2012-11-07 TW TW101141421A patent/TWI555747B/zh not_active IP Right Cessation
- 2012-11-07 EA EA201400553A patent/EA024106B1/ru not_active IP Right Cessation
- 2012-11-07 MY MYPI2014701155A patent/MY167791A/en unknown
- 2012-11-07 AU AU2012335194A patent/AU2012335194B2/en not_active Ceased
- 2012-11-07 HU HUE12791862A patent/HUE029239T2/en unknown
- 2012-11-07 SI SI201230556A patent/SI2776430T1/sl unknown
- 2012-11-07 HR HRP20160678TT patent/HRP20160678T1/hr unknown
- 2012-11-07 US US14/357,159 patent/US9150566B2/en active Active
- 2012-11-07 MX MX2014005635A patent/MX343837B/es active IP Right Grant
- 2012-11-07 DK DK12791862.1T patent/DK2776430T3/en active
- 2012-11-07 CA CA2846568A patent/CA2846568C/en active Active
- 2012-11-07 IN IN4127CHN2014 patent/IN2014CN04127A/en unknown
- 2012-11-07 EP EP12791862.1A patent/EP2776430B1/en active Active
- 2012-11-07 KR KR1020147014960A patent/KR101676930B1/ko not_active Expired - Fee Related
- 2012-11-07 BR BR112014010617-7A patent/BR112014010617B1/pt not_active IP Right Cessation
- 2012-11-07 WO PCT/IB2012/056218 patent/WO2013068935A1/en not_active Ceased
- 2012-11-07 PH PH1/2014/500852A patent/PH12014500852A1/en unknown
- 2012-11-07 AR ARP120104193A patent/AR088692A1/es active IP Right Grant
- 2012-11-07 PL PL12791862.1T patent/PL2776430T3/pl unknown
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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
Patent Citations (7)
| 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 |
| CN1549816A (zh) * | 2001-06-28 | 2004-11-24 | ʷ | 作为阿立新受体拮抗药的n-芳酰基环胺衍生物 |
| WO2003032991A1 (en) * | 2001-10-11 | 2003-04-24 | Smithkline Beecham Plc | N-aroyl piperazine derivatives as orexin receptor antagonists |
| WO2003051368A1 (en) * | 2001-12-19 | 2003-06-26 | Smithkline Beecham Plc | N-aroyl cyclic amine derivatives as orexin receptor antagonists |
| WO2010048010A1 (en) * | 2008-10-21 | 2010-04-29 | Merck Sharp & Dohme Corp. | 2,5-disubstituted piperidine orexin receptor antagonists |
| WO2010048013A1 (en) * | 2008-10-21 | 2010-04-29 | Merck Sharp & Dohme Corp. | 2,5-disubstituted morpholine orexin receptor antagonists |
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Effective date of registration: 20171109 Address after: Swiss A Skei Weil Patentee after: ACTELION PHARMACEUTICALS LTD. Address before: Swiss A Skei Weil Patentee before: Actelion Pharmaceuticals Ltd. |
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