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EA201170741A1 - Производные n-{[(1r,4s,6r)-3-(2-пиридинилкарбонил)-3-азабицикло[4.1.0]гепт-4-ил]метил}-2-гетероариламина и их применения - Google Patents

Производные n-{[(1r,4s,6r)-3-(2-пиридинилкарбонил)-3-азабицикло[4.1.0]гепт-4-ил]метил}-2-гетероариламина и их применения

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Publication number
EA201170741A1
EA201170741A1 EA201170741A EA201170741A EA201170741A1 EA 201170741 A1 EA201170741 A1 EA 201170741A1 EA 201170741 A EA201170741 A EA 201170741A EA 201170741 A EA201170741 A EA 201170741A EA 201170741 A1 EA201170741 A1 EA 201170741A1
Authority
EA
Eurasian Patent Office
Prior art keywords
heteroarylamine
azabicyclo
hept
derivatives
methyl
Prior art date
Application number
EA201170741A
Other languages
English (en)
Inventor
Джузеппе Альваро
Давид Амантини
Эмилиано Кастильони
Романо Ди Фабио
Франческа Павоне
Original Assignee
Глэксо Груп Лимитед
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Глэксо Груп Лимитед filed Critical Глэксо Груп Лимитед
Publication of EA201170741A1 publication Critical patent/EA201170741A1/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/06Heterocyclic 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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/26Psychostimulants, e.g. nicotine, cocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Anesthesiology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Это изобретение относится к производным N-{[(1S,4S,6S)-3-(2-пиридинилкарбонил)-3-азабицикло[4.1.0]гепт-4-ил]метил}-2-гетероариламина и к их применению в качестве фармацевтических средств.
EA201170741A 2008-12-02 2009-11-30 Производные n-{[(1r,4s,6r)-3-(2-пиридинилкарбонил)-3-азабицикло[4.1.0]гепт-4-ил]метил}-2-гетероариламина и их применения EA201170741A1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US11911808P 2008-12-02 2008-12-02
US23630209P 2009-08-24 2009-08-24
PCT/EP2009/066016 WO2010063662A1 (en) 2008-12-02 2009-11-30 N-{[(ir,4s,6r-3-(2-pyridinylcarbonyl)-3-azabicyclo [4.1.0] hept-4-yl] methyl}-2-heteroarylamine derivatives and uses thereof

Publications (1)

Publication Number Publication Date
EA201170741A1 true EA201170741A1 (ru) 2011-12-30

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Family Applications (1)

Application Number Title Priority Date Filing Date
EA201170741A EA201170741A1 (ru) 2008-12-02 2009-11-30 Производные n-{[(1r,4s,6r)-3-(2-пиридинилкарбонил)-3-азабицикло[4.1.0]гепт-4-ил]метил}-2-гетероариламина и их применения

Country Status (16)

Country Link
US (1) US8133908B2 (ru)
EP (1) EP2370427A1 (ru)
JP (1) JP2012510493A (ru)
KR (1) KR20110091581A (ru)
CN (1) CN102300858A (ru)
AR (1) AR074426A1 (ru)
AU (1) AU2009324238A1 (ru)
BR (1) BRPI0922353A2 (ru)
CA (1) CA2745420A1 (ru)
EA (1) EA201170741A1 (ru)
IL (1) IL212925A0 (ru)
MX (1) MX2011005799A (ru)
TW (1) TW201031407A (ru)
UY (1) UY32276A (ru)
WO (1) WO2010063662A1 (ru)
ZA (1) ZA201103482B (ru)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010063663A1 (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
EP2470525A1 (en) * 2009-08-24 2012-07-04 Glaxo Group Limited Piperidine derivatives used as orexin antagonists
US8653263B2 (en) 2009-10-23 2014-02-18 Janssen Pharmaceutica Disubstituted octahydropyrrolo[3,4-c]pyrroles as orexin receptor modulators
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
JP5848251B2 (ja) 2009-10-23 2016-01-27 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
WO2012085852A1 (en) 2010-12-22 2012-06-28 Actelion Pharmaceuticals Ltd 3,8-diaza-bicyclo[4.2.0]oct-8-yl amides
WO2012089606A1 (en) * 2010-12-28 2012-07-05 Glaxo Group Limited Azabicyclo [4.1.0] hept - 4 - yl derivatives as human orexin receptor antagonists
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
US9586962B2 (en) 2011-04-20 2017-03-07 Janssen Pharmaceutica Nv Disubstituted octahydropyrrolo [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
SG11201401665WA (en) 2011-11-08 2014-09-26 Actelion Pharmaceuticals Ltd 2-(1,2,3-triazol-2-yl)benzamide and 3-(1,2,3-triazol-2-yl)picolinamide derivatives as orexin receptor antagonists
US9440982B2 (en) 2012-02-07 2016-09-13 Eolas Therapeutics, Inc. Substituted prolines/piperidines as orexin receptor antagonists
RU2014136339A (ru) 2012-02-07 2016-03-27 Иолас Терапьютикс, Инк. Замещенные пролины/пиперидины как антагонисты орексиновых рецепторов
US9416109B2 (en) 2012-02-17 2016-08-16 Eisai R&D Management Co., Ltd. Methods and compounds useful in the synthesis of orexin-2 receptor antagonists
ITMI20120424A1 (it) * 2012-03-19 2013-09-20 Rottapharm Spa Composti chimici
TWI510481B (zh) 2012-06-04 2015-12-01 Actelion Pharmaceuticals Ltd 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
EP2970241A1 (en) 2013-03-12 2016-01-20 Actelion Pharmaceuticals Ltd. Azetidine amide derivatives as orexin receptor antagonists
ES2651475T3 (es) 2013-12-03 2018-01-26 Idorsia Pharmaceuticals Ltd Forma cristalina de (S)-(2-(6-cloro-7-metil-1H-benzo[d]imidazol-2-il)-2-metilpirrolidin-1-il)(5-metoxi-2-(2H-1,2,3-triazol-2-il)fenil)metanona y su uso como antagonistas del receptor de orexina
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
AU2014358766B2 (en) 2013-12-04 2019-01-17 Idorsia Pharmaceuticals Ltd Use of benzimidazole-proline derivatives
AR101558A1 (es) 2014-08-13 2016-12-28 Eolas Therapeutics Inc Difluoropirrolidinas como moduladores del receptor de orexina
RS63471B1 (sr) 2016-02-12 2022-08-31 Astrazeneca Ab Halo-supstituisani piperidini kao modulatori receptora oreksina
NZ785827A (en) 2016-03-10 2025-05-02 Janssen Pharmaceutica Nv Methods of treating depression using orexin-2 receptor antagonists
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
EP3661928B1 (en) * 2017-07-31 2021-06-16 Boehringer Ingelheim International GmbH N-[(pyrimidinylamino)propanyl]-, n-[(pyridylamino)propanyl]- and n-[(pyrazinylamino)propanyl]arylcarboxamides
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
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

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR016817A1 (es) 1997-08-14 2001-08-01 Smithkline Beecham Plc Derivados de fenilurea o feniltiourea, procedimiento para su preparacion, coleccion de compuestos, compuestos intermediarios, composicion farmaceutica,metodo de tratamiento y uso de dichos compuestos para la manufactura de un medicamento
US6372757B1 (en) 1998-05-08 2002-04-16 Smithkline Beecham P.L.C. Phenylurea and phenylthio urea derivatives
WO2000047576A1 (en) 1999-02-12 2000-08-17 Smithkline Beecham Plc Cinnamide derivatives as orexin-1 receptors antagonists
ES2226785T3 (es) 1999-02-12 2005-04-01 Smithkline Beecham Plc Derivados de fenilurea como antagonistas de los receptores de orexina.
JP2002536447A (ja) 1999-02-12 2002-10-29 スミスクライン・ビーチャム・パブリック・リミテッド・カンパニー フェニル尿素およびフェニルチオ尿素誘導体
EP1289955B1 (en) 2000-06-16 2005-04-13 Smithkline Beecham Plc Piperidines for use as orexin receptor antagonists
AU2002224885A1 (en) 2000-11-28 2002-06-11 Smithkline Beecham Plc Morpholine derivatives as antagonists of orexin receptors
WO2002089800A2 (en) 2001-05-05 2002-11-14 Smithkline Beecham P.L.C. N-aroyl cyclic amine derivatives as orexin receptor antagonists
ES2299567T3 (es) * 2001-05-05 2008-06-01 Smithkline Beecham Plc N-aroilaminas ciclicas.
GB0115862D0 (en) 2001-06-28 2001-08-22 Smithkline Beecham Plc Compounds
CA2451464A1 (en) 2001-06-28 2003-01-09 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
GB0126292D0 (en) 2001-11-01 2002-01-02 Smithkline Beecham Plc Compounds
GB0127145D0 (en) 2001-11-10 2002-01-02 Smithkline Beecham Compounds
AU2003262516A1 (en) * 2002-09-18 2004-04-08 Glaxo Group Limited N-aroyl cyclic amines as orexin receptor antagonists
GB0225884D0 (en) * 2002-11-06 2002-12-11 Glaxo Group Ltd Novel compounds
SI1751111T1 (sl) 2004-03-01 2015-04-30 Actelion Pharmaceuticals Ltd. Substituirani 1,2,3,4-tetrahidroizokinolinski derivati
TW200823227A (en) 2006-09-29 2008-06-01 Actelion Pharmaceuticals Ltd 3-aza-bicyclo[3.1.0]hexane derivatives
US20120095034A1 (en) 2007-07-03 2012-04-19 Giuseppe Alvaro Piperidine derivatives useful as orexin receptor antagonists
GB0712888D0 (en) 2007-07-03 2007-08-15 Glaxo Group Ltd Novel compounds
GB0806536D0 (en) 2008-04-10 2008-05-14 Glaxo Group Ltd Novel compounds
WO2010063663A1 (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

Also Published As

Publication number Publication date
KR20110091581A (ko) 2011-08-11
US20100168131A1 (en) 2010-07-01
CN102300858A (zh) 2011-12-28
WO2010063662A1 (en) 2010-06-10
EP2370427A1 (en) 2011-10-05
US8133908B2 (en) 2012-03-13
MX2011005799A (es) 2011-06-20
AU2009324238A1 (en) 2010-06-10
TW201031407A (en) 2010-09-01
UY32276A (es) 2010-05-31
BRPI0922353A2 (pt) 2018-06-05
AR074426A1 (es) 2011-01-19
CA2745420A1 (en) 2010-06-10
JP2012510493A (ja) 2012-05-10
IL212925A0 (en) 2011-07-31
ZA201103482B (en) 2012-01-25

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