KR101676930B1 - 오렉신 수용체 길항제로서의 ２-(１,２,３-트리아졸-２-일)벤즈아미드 및 ３-(１,２,３-트리아졸-２-일)피콜린아미드 유도체 - Google Patents
오렉신 수용체 길항제로서의 ２-(１,２,３-트리아졸-２-일)벤즈아미드 및 ３-(１,２,３-트리아졸-２-일)피콜린아미드 유도체 Download PDFInfo
- Publication number
- KR101676930B1 KR101676930B1 KR1020147014960A KR20147014960A KR101676930B1 KR 101676930 B1 KR101676930 B1 KR 101676930B1 KR 1020147014960 A KR1020147014960 A KR 1020147014960A KR 20147014960 A KR20147014960 A KR 20147014960A KR 101676930 B1 KR101676930 B1 KR 101676930B1
- Authority
- KR
- South Korea
- Prior art keywords
- morpholin
- methanone
- benzyl
- triazol
- phenyl
- 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
- PEDODSOFPMWUMO-SSDOTTSWSA-N CC[C@H]1N(C)CCOC1 Chemical compound CC[C@H]1N(C)CCOC1 PEDODSOFPMWUMO-SSDOTTSWSA-N 0.000 description 2
- BCECPPZTDSOTCO-HTQZYQBOSA-N CC[C@H]1N(C)C[C@@H](C)OC1 Chemical compound CC[C@H]1N(C)C[C@@H](C)OC1 BCECPPZTDSOTCO-HTQZYQBOSA-N 0.000 description 2
- AVPHREXUHKIHQW-MRVPVSSYSA-N CC[C@@]1(C)N(C)CCOC1 Chemical compound CC[C@@]1(C)N(C)CCOC1 AVPHREXUHKIHQW-MRVPVSSYSA-N 0.000 description 1
- YABJQYZJFDJJSK-SSDOTTSWSA-N CC[C@H](COC)N(C)C Chemical compound CC[C@H](COC)N(C)C YABJQYZJFDJJSK-SSDOTTSWSA-N 0.000 description 1
- NRYFXJRIRCQGSS-WHHARQNVSA-N CC[C@H]1N(C)C(CCC2N(C)C[C@H](C)OC2)[C@@H](CC)OC1 Chemical compound CC[C@H]1N(C)C(CCC2N(C)C[C@H](C)OC2)[C@@H](CC)OC1 NRYFXJRIRCQGSS-WHHARQNVSA-N 0.000 description 1
- BFCAISJBETWESU-GZNJTBKBSA-N CC[C@H]1N(C)C(CC[C@H]2N(C)CCO[C@H]2C)CO[C@@H]1C Chemical compound CC[C@H]1N(C)C(CC[C@H]2N(C)CCO[C@H]2C)CO[C@@H]1C BFCAISJBETWESU-GZNJTBKBSA-N 0.000 description 1
- HRSGPCLVYDTFSK-JGVFFNPUSA-N CC[C@H]1N(C)[C@@H](C)COC1 Chemical compound CC[C@H]1N(C)[C@@H](C)COC1 HRSGPCLVYDTFSK-JGVFFNPUSA-N 0.000 description 1
- HRSGPCLVYDTFSK-HTQZYQBOSA-N CC[C@H]1N(C)[C@H](C)COC1 Chemical compound CC[C@H]1N(C)[C@H](C)COC1 HRSGPCLVYDTFSK-HTQZYQBOSA-N 0.000 description 1
Classifications
-
- 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
-
- 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
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 |
|---|---|---|---|
| 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 |
|---|---|
| KR20140096338A KR20140096338A (ko) | 2014-08-05 |
| KR101676930B1 true KR101676930B1 (ko) | 2016-11-16 |
Family
ID=47258050
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020147014960A Expired - Fee Related KR101676930B1 (ko) | 2011-11-08 | 2012-11-07 | 오렉신 수용체 길항제로서의 ２-(１,２,３-트리아졸-２-일)벤즈아미드 및 ３-(１,２,３-트리아졸-２-일)피콜린아미드 유도체 |
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 |
|---|---|---|---|---|
| US9440982B2 (en) | 2012-02-07 | 2016-09-13 | Eolas Therapeutics, Inc. | Substituted prolines/piperidines as orexin receptor antagonists |
| ES2672732T3 (es) | 2012-02-07 | 2018-06-15 | Eolas Therapeutics Inc. | Prolinas/piperidinas sustituidas como antagonistas del receptor de orexina |
| KR101689093B1 (ko) | 2012-06-04 | 2016-12-22 | 액테리온 파마슈티칼 리미티드 | 벤즈이미다졸-프롤린 유도체 |
| CA2902135A1 (en) | 2013-03-12 | 2014-09-18 | Actelion Pharmaceuticals Ltd | Azetidine amide derivatives 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 |
| HK1225731B (en) | 2013-12-03 | 2017-09-15 | 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 |
| HRP20181710T1 (hr) | 2013-12-04 | 2018-12-28 | Idorsia Pharmaceuticals Ltd | Uporaba derivata benzimidazol-prolina |
| 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 |
| 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 |
| EP3143999A4 (en) | 2014-05-16 | 2017-12-20 | The University of Tokyo | Depression treatment agent |
| JP6663909B2 (ja) | 2014-08-13 | 2020-03-13 | 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モジュレーターとしてのジフルオロピロリジン |
| 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 |
| WO2017088759A1 (en) | 2015-11-23 | 2017-06-01 | Sunshine Lake Pharma Co., Ltd. | OCTAHYDROPYRROLO [3, 4-c] PYRROLE DERIVATIVES AND USES THEREOF |
| MX2018009656A (es) | 2016-02-12 | 2019-02-20 | Astrazeneca Ab | Piperidinas halo-sustituidas como moduladores de los receptores de orexinas. |
| HRP20211304T1 (hr) | 2017-05-03 | 2021-11-12 | Idorsia Pharmaceuticals Ltd | Pripravljanje derivata 2-([1,2,3]triazol-2-il)-benzojeve kiseline |
| 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 |
| EP4288432A1 (en) * | 2021-02-02 | 2023-12-13 | 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 |
| 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 | ||
| 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 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003002559A2 (en) * | 2001-06-28 | 2003-01-09 | Smithkline Beecham P.L.C. | Piperidine compounds for use as orexin receptor antagonist |
Family Cites Families (21)
| 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 |
| WO1993000313A2 (en) | 1991-06-27 | 1993-01-07 | 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 |
| BR0210609A (pt) * | 2001-06-28 | 2004-07-20 | Smithkline Beecham Plc | Derivados de amina cìclica n-aroila como antagonistas do receptor da orexina |
| GB0124463D0 (en) * | 2001-10-11 | 2001-12-05 | Smithkline Beecham Plc | Compounds |
| GB0130335D0 (en) * | 2001-12-19 | 2002-02-06 | Smithkline Beecham Plc | Compounds |
| PT1751111E (pt) | 2004-03-01 | 2015-04-01 | Actelion Pharmaceuticals Ltd | Derivados de 1,2,3,4-tetrahidroisoquinolina substituída |
| US20090082394A1 (en) | 2006-03-15 | 2009-03-26 | Actelion Pharmaceuticals, Ltd. | Tetrahydroisoquinoline Derivatives to Enhance Memory Function |
| CA2657623A1 (en) | 2006-07-14 | 2008-01-17 | Merck & Co., Inc. | 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 |
| WO2009040730A2 (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 |
| AU2009307916A1 (en) * | 2008-10-21 | 2010-04-29 | Merck Sharp & Dohme Corp. | 2,5-disubstituted morpholine orexin receptor antagonists |
| EP2349269A4 (en) | 2008-10-21 | 2012-04-25 | Merck Sharp & Dohme | 2,5-DISUBSTITUTED PIPERIDINOREXINE RECEPTOR ANTAGONISTS |
| AU2009307913A1 (en) * | 2008-10-21 | 2010-04-29 | Merck Sharp & Dohme Corp. | 2,5-disubstituted piperidine orexin receptor antagonists |
| JP2012510494A (ja) | 2008-12-02 | 2012-05-10 | グラクソ グループ リミテッド | Ｎ−｛［（ｉｒ、４ｓ、６ｒ）−３−（２−ピリジニルカルボニル）−３−アザビシクロ［４．１．０］ヘプタ−４−イル］メチル｝−２−ヘテロアリールアミン誘導体およびその使用 |
| AR074426A1 (es) | 2008-12-02 | 2011-01-19 | Glaxo Group Ltd | Compuesto de n-(((1s,4s,6s)-3-(2-piridinilcarbonil)3-azabiciclo (4,1.0)hept-4-il) metil)-2-heteroarilamina, su uso para la prepracion de un medicamento para el tratamiento de una enfermedad que requiere un antagonista de un receptor de orexina humana y composicion farmaceutica que lo comprende |
| 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 |
| WO2011050200A1 (en) | 2009-10-23 | 2011-04-28 | Janssen Pharmaceutica Nv | Fused heterocyclic compounds as orexin receptor modulators |
-
2012
- 2012-11-07 TW TW105118634A patent/TWI565703B/zh not_active IP Right Cessation
- 2012-11-07 JP JP2014540606A patent/JP5718535B2/ja active Active
- 2012-11-07 BR BR112014010617-7A patent/BR112014010617B1/pt not_active IP Right Cessation
- 2012-11-07 MX MX2014005635A patent/MX343837B/es active IP Right Grant
- 2012-11-07 HU HUE12791862A patent/HUE029239T2/en unknown
- 2012-11-07 SI SI201230556A patent/SI2776430T1/sl unknown
- 2012-11-07 IN IN4127CHN2014 patent/IN2014CN04127A/en unknown
- 2012-11-07 SG SG11201401665WA patent/SG11201401665WA/en unknown
- 2012-11-07 US US14/357,159 patent/US9150566B2/en active Active
- 2012-11-07 HR HRP20160678TT patent/HRP20160678T1/hr unknown
- 2012-11-07 MY MYPI2014701155A patent/MY167791A/en 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 KR KR1020147014960A patent/KR101676930B1/ko not_active Expired - Fee Related
- 2012-11-07 ES ES12791862.1T patent/ES2572703T3/es active Active
- 2012-11-07 PH PH1/2014/500852A patent/PH12014500852A1/en unknown
- 2012-11-07 UA UAA201402001A patent/UA112317C2/uk unknown
- 2012-11-07 PL PL12791862.1T patent/PL2776430T3/pl 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 AR ARP120104193A patent/AR088692A1/es active IP Right Grant
- 2012-11-07 CN CN201280054325.7A patent/CN103917538B/zh not_active Expired - Fee Related
- 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 DK DK12791862.1T patent/DK2776430T3/en active
-
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 (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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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