AR074238A1 - Compuesto de n-{[(1r,4s,6r)-3-(2-piridinilcarbonil)-3-azabiciclo[4,1.0]hept-4-il]metil}-2-heteroarilamina, su uso para la preparacion de un medicamento util para el tratamiento de una enfermedad que requiere un antagonista del receptor de orexina humano y composicion farmaceutica que lo comprende - Google Patents
Compuesto de n-{[(1r,4s,6r)-3-(2-piridinilcarbonil)-3-azabiciclo[4,1.0]hept-4-il]metil}-2-heteroarilamina, su uso para la preparacion de un medicamento util para el tratamiento de una enfermedad que requiere un antagonista del receptor de orexina humano y composicion farmaceutica que lo comprendeInfo
- Publication number
- AR074238A1 AR074238A1 ARP090104606A ARP090104606A AR074238A1 AR 074238 A1 AR074238 A1 AR 074238A1 AR P090104606 A ARP090104606 A AR P090104606A AR P090104606 A ARP090104606 A AR P090104606A AR 074238 A1 AR074238 A1 AR 074238A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- haloalkoxy
- haloalkyl
- halo
- cyano
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory 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
-
- 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
- A61P25/20—Hypnotics; Sedatives
-
- 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
- A61P25/24—Antidepressants
-
- 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
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
Abstract
Compuesto de N-{[(1R,4S,6R)-3-(2-piridinilcarbonil)-3-azabiciclo[4.1.0]hept-4-il]metil}-2-heteroarilamina, de formula (1), donde Het es un grupo heteroarilo seleccionado entre el grupo que consiste en piridinilo, pirimidinilo, piridazinilo o pirazinilo, estando dicho grupo heteroarilo opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados independientemente entre el grupo que consiste en alquilo C1-4, halo, alcoxi C1-4, haloalquilo C1-4, haloalcoxi C1-4, y ciano; R1 es alquilo C1-4, halo, alcoxi C1-4, haloalquilo C1-4, haloalcoxi C1-4, ciano, alquil C1-4-SO2, cicloalquil C3-8-SO2, cicloalquil C3-8-CH2SO2, fenilo o un grupo heterociclilo de 5 o 6 miembros que contiene 1, 2 o 3 átomos seleccionados entre N, O o S, donde el grupo fenilo o heterociclilo está opcionalmente sustituido con alquilo C1-4, halo, alcoxi C1-4, haloalquilo C1-4, haloalcoxi C1-4, o ciano; R2 es alquilo C1-4, halo, alcoxi C1-4, haloalquilo C1-4, haloalcoxi C1-4, ciano, fenilo o un grupo heterociclilo de 5 o 6 miembros que contiene 1, 2 o 3 átomos seleccionados entre N, O o S, donde el grupo fenilo o heterociclilo está opcionalmente sustituido con alquilo C1-4, halo, alcoxi C1-4, haloalquilo C1-4, haloalcoxi C1-4 o ciano; R3 es alquilo C1-4, halo, alcoxi C1-4, haloalquilo C1-4, haloalcoxi C1-4 o ciano; m es 0 o 1; y n es 0 o 1; o una sal farmacéuticamente aceptable del mismo. Uso de dicho compuesto para la preparacion de un medicamento util para el tratamiento de una enfermedad o trastorno en el que se requiere un antagonista del receptor de orexina humano y composicion farmacéutica que lo comprende.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US11912608P | 2008-12-02 | 2008-12-02 | |
US18531609P | 2009-06-09 | 2009-06-09 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR074238A1 true AR074238A1 (es) | 2010-12-29 |
Family
ID=41528698
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP090104606A AR074238A1 (es) | 2008-12-02 | 2009-11-30 | Compuesto de n-{[(1r,4s,6r)-3-(2-piridinilcarbonil)-3-azabiciclo[4,1.0]hept-4-il]metil}-2-heteroarilamina, su uso para la preparacion de un medicamento util para el tratamiento de una enfermedad que requiere un antagonista del receptor de orexina humano y composicion farmaceutica que lo comprende |
Country Status (15)
Country | Link |
---|---|
US (1) | US20100144760A1 (es) |
EP (1) | EP2370426A1 (es) |
JP (1) | JP2012510494A (es) |
KR (1) | KR20110091582A (es) |
CN (1) | CN102300857A (es) |
AR (1) | AR074238A1 (es) |
AU (1) | AU2009324239A1 (es) |
CA (1) | CA2745433A1 (es) |
EA (1) | EA201170742A1 (es) |
IL (1) | IL212920A0 (es) |
MX (1) | MX2011005800A (es) |
TW (1) | TW201033190A (es) |
UY (1) | UY32277A (es) |
WO (1) | WO2010063663A1 (es) |
ZA (1) | ZA201103481B (es) |
Families Citing this family (39)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8133908B2 (en) | 2008-12-02 | 2012-03-13 | Glaxo Group Limited | Heteroaryl derivatives of N-{[(1S,4S,6S)-3-(2-pyridinylcarbonyl)-3-azabicyclo[4.1.0]hept-4-yl]methyl}-2-amine |
WO2011023585A1 (en) * | 2009-08-24 | 2011-03-03 | Glaxo Group Limited | Piperidine derivatives used as orexin antagonists |
CN102781942B (zh) | 2009-10-23 | 2015-09-23 | 詹森药业有限公司 | 用作食欲肽受体调节剂的二取代八氢吡咯并[3,4-c]吡咯 |
EP2491034B1 (en) | 2009-10-23 | 2013-12-18 | Janssen Pharmaceutica, N.V. | Fused heterocyclic compounds as orexin receptor modulators |
WO2011050202A1 (en) | 2009-10-23 | 2011-04-28 | Janssen Pharmaceutica Nv | Fused heterocyclic compounds as orexin receptor modulators |
RS54101B1 (en) * | 2010-09-22 | 2015-10-30 | Eisai R&D Management Co. Ltd. | A CYCLOPROPAN UNIT |
WO2012085852A1 (en) | 2010-12-22 | 2012-06-28 | Actelion Pharmaceuticals Ltd | 3,8-diaza-bicyclo[4.2.0]oct-8-yl amides |
WO2012089607A1 (en) * | 2010-12-28 | 2012-07-05 | Glaxo Group Limited | Novel compounds with a 3a-azabicyclo [4.1.0] heptane core acting on orexin receptors |
WO2012145581A1 (en) | 2011-04-20 | 2012-10-26 | Janssen Pharmaceutica Nv | Disubstituted octahy-dropyrrolo [3,4-c] pyrroles as orexin receptor modulators |
WO2013050938A1 (en) | 2011-10-04 | 2013-04-11 | Actelion Pharmaceuticals Ltd | 3,7-diazabicyclo[3.3.1]nonane and 9-oxa-3,7-diazabicyclo[3.3.1]nonane derivatives |
HUE029239T2 (en) | 2011-11-08 | 2017-02-28 | Actelion Pharmaceuticals Ltd | 2- (1,2,3-Triazol-2-yl) benzamide and 3- (1,2,3-triazol-2-yl) picolinamide derivatives such as orexin receptor antagonists |
ITMI20112329A1 (it) * | 2011-12-21 | 2013-06-22 | Rottapharm Spa | Nuovi derivati spiro amminici |
US9440982B2 (en) | 2012-02-07 | 2016-09-13 | Eolas Therapeutics, Inc. | Substituted prolines/piperidines as orexin receptor antagonists |
WO2013119639A1 (en) | 2012-02-07 | 2013-08-15 | Eolas Therapeutics, Inc. | Substituted prolines / piperidines as orexin receptor antagonists |
ITMI20120322A1 (it) | 2012-03-01 | 2013-09-02 | Rottapharm Spa | Composti di 4,4-difluoro piperidina |
ITMI20120424A1 (it) | 2012-03-19 | 2013-09-20 | Rottapharm Spa | Composti chimici |
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 |
EA201500399A1 (ru) | 2012-10-10 | 2015-09-30 | Актелион Фармасьютиклз Лтд. | Антагонисты рецептора орексина, которые представляют собой производные [орто-би-(гетеро)арил]-[2-(мета-би-(гетеро)арил)пирролидин-1-ил]метанона |
KR20150130413A (ko) | 2013-03-12 | 2015-11-23 | 액테리온 파마슈티칼 리미티드 | 오렉신 수용체 길항제로서의 아제티딘 아미드 유도체 |
TW201444849A (zh) | 2013-03-13 | 2014-12-01 | Janssen Pharmaceutica Nv | 經取代的7-氮雜雙環類及其作為食慾激素受體調節劑之用途 |
TWI621618B (zh) | 2013-03-13 | 2018-04-21 | 比利時商健生藥品公司 | 經取代2-氮雜雙環類及其作為食慾素受體調控劑之用途 |
TW201444821A (zh) | 2013-03-13 | 2014-12-01 | Janssen Pharmaceutica Nv | 經取代之哌啶化合物及其作為食慾素受體調節劑之用途 |
KR102361418B1 (ko) | 2013-12-03 | 2022-02-09 | 이도르시아 파마슈티컬스 리미티드 | (S)-(2-(6-클로로-7-메틸-1H-벤조[d]이미다졸-2-일)-2-메틸피롤리딘-1- 일)(5-메톡시-2-(2H-1,2,3-트리아졸-2-일)페닐)메타논의 결정형 및 오렉신 수용체 길항제로서의 그 용도 |
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 |
UY36272A (es) | 2014-08-13 | 2016-02-29 | Eolas Therapeutics Inc | Difluoropirrolidinas como moduladores de los receptores de orexinas |
US9611262B2 (en) | 2014-09-11 | 2017-04-04 | Janssen Pharmaceutica Nv | Substituted 2-azabicycles and their use as orexin receptor modulators |
EA033613B1 (ru) | 2015-08-17 | 2019-11-08 | Lupin Ltd | Гетероарильные производные в качестве ингибиторов parp |
EP3414241B1 (en) | 2016-02-12 | 2022-05-04 | Astrazeneca AB | Halo-substituted piperidines as orexin receptor modulators |
CN108883110B (zh) | 2016-03-10 | 2022-05-27 | 詹森药业有限公司 | 使用食欲素-2受体拮抗剂治疗抑郁症的方法 |
GB201702174D0 (en) | 2017-02-09 | 2017-03-29 | Benevolentai Bio Ltd | Orexin receptor antagonists |
GB201707504D0 (en) | 2017-05-10 | 2017-06-21 | Benevolentai Bio Ltd | Orexin receptor antagonists |
GB201707499D0 (en) | 2017-05-10 | 2017-06-21 | Benevolentai Bio Ltd | Orexin receptor antagonists |
CN111051295B (zh) * | 2017-08-03 | 2022-09-02 | 武田药品工业株式会社 | 杂环化合物及其用途 |
WO2020007964A1 (en) | 2018-07-05 | 2020-01-09 | Idorsia Pharmaceuticals Ltd | 2-(2-azabicyclo[3.1.0]hexan-1-yl)-1h-benzimidazole derivatives |
WO2020099511A1 (en) | 2018-11-14 | 2020-05-22 | Idorsia Pharmaceuticals Ltd | Benzimidazole-2-methyl-morpholine derivatives |
CN112739689B (zh) | 2018-12-07 | 2022-06-03 | 优迈特株式会社 | 含氟嘧啶化合物及其制造方法 |
EP4155299A1 (en) | 2020-05-19 | 2023-03-29 | Unimatec Co., Ltd. | Fluoropyrimidine compound and fluoropyrimidinone compound |
WO2023218023A1 (en) | 2022-05-13 | 2023-11-16 | Idorsia Pharmaceuticals Ltd | Thiazoloaryl-methyl substituted cyclic hydrazine-n-carboxamide derivatives |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CZ20032990A3 (cs) * | 2001-05-05 | 2004-04-14 | Smithkline Beecham P. L. C. | N-aroylové cyklické aminy |
JP2006504695A (ja) * | 2002-09-18 | 2006-02-09 | グラクソ グループ リミテッド | オレキシン受容体アンタゴニストとしてのn−アロイル環状アミン |
GB0225884D0 (en) * | 2002-11-06 | 2002-12-11 | Glaxo Group Ltd | Novel compounds |
KR20090077051A (ko) * | 2006-09-29 | 2009-07-14 | 액테리온 파마슈티칼 리미티드 | 3-아자-비시클로[3.1.0]헥산 유도체 |
US8133908B2 (en) * | 2008-12-02 | 2012-03-13 | Glaxo Group Limited | Heteroaryl derivatives of N-{[(1S,4S,6S)-3-(2-pyridinylcarbonyl)-3-azabicyclo[4.1.0]hept-4-yl]methyl}-2-amine |
-
2009
- 2009-11-30 CA CA2745433A patent/CA2745433A1/en not_active Abandoned
- 2009-11-30 EP EP09759961A patent/EP2370426A1/en not_active Withdrawn
- 2009-11-30 TW TW098140727A patent/TW201033190A/zh unknown
- 2009-11-30 JP JP2011538976A patent/JP2012510494A/ja not_active Withdrawn
- 2009-11-30 UY UY0001032277A patent/UY32277A/es not_active Application Discontinuation
- 2009-11-30 KR KR1020117015256A patent/KR20110091582A/ko not_active Application Discontinuation
- 2009-11-30 EA EA201170742A patent/EA201170742A1/ru unknown
- 2009-11-30 US US12/627,134 patent/US20100144760A1/en not_active Abandoned
- 2009-11-30 CN CN2009801559231A patent/CN102300857A/zh active Pending
- 2009-11-30 AU AU2009324239A patent/AU2009324239A1/en not_active Abandoned
- 2009-11-30 AR ARP090104606A patent/AR074238A1/es not_active Application Discontinuation
- 2009-11-30 WO PCT/EP2009/066017 patent/WO2010063663A1/en active Application Filing
- 2009-11-30 MX MX2011005800A patent/MX2011005800A/es not_active Application Discontinuation
-
2011
- 2011-05-12 ZA ZA2011/03481A patent/ZA201103481B/en unknown
- 2011-05-16 IL IL212920A patent/IL212920A0/en unknown
Also Published As
Publication number | Publication date |
---|---|
US20100144760A1 (en) | 2010-06-10 |
AU2009324239A1 (en) | 2010-06-10 |
CA2745433A1 (en) | 2010-06-10 |
MX2011005800A (es) | 2011-06-20 |
KR20110091582A (ko) | 2011-08-11 |
JP2012510494A (ja) | 2012-05-10 |
UY32277A (es) | 2010-05-31 |
CN102300857A (zh) | 2011-12-28 |
EP2370426A1 (en) | 2011-10-05 |
ZA201103481B (en) | 2012-01-25 |
IL212920A0 (en) | 2011-07-31 |
EA201170742A1 (ru) | 2012-01-30 |
TW201033190A (en) | 2010-09-16 |
WO2010063663A1 (en) | 2010-06-10 |
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