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ES2659222T3 - 7-azabicíclicos sustituidos y su uso para moduladores de receptores de orexina - Google Patents

7-azabicíclicos sustituidos y su uso para moduladores de receptores de orexina Download PDF

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Publication number
ES2659222T3
ES2659222T3 ES14717297.7T ES14717297T ES2659222T3 ES 2659222 T3 ES2659222 T3 ES 2659222T3 ES 14717297 T ES14717297 T ES 14717297T ES 2659222 T3 ES2659222 T3 ES 2659222T3
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alkyl
pyrazolyl
pyridyl
alkoxy
group
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Inventor
Heather R. COATE
Curt A. Dvorak
Anne E. Fitzgerald
Terry P. LEBOLD
Cathy PREVILLE
Brock T. Shireman
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Janssen Pharmaceutica NV
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Janssen Pharmaceutica NV
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems
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    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
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    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • 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
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Abstract

Un compuesto de fórmula I: **Fórmula** o un enantiómero o diastereómero, tautómero o variante isotópica del mismo; o una sal o solvato farmacéuticamente aceptable del mismo; donde el anillo A es fenilo, naftalenilo, piridilo, quinolinilo, isoquinolinilo, imidazopiridilo, furanilo, tiazolilo, isoxazolilo, pirazolilo, imidazotiazolilo, bencimidazolilo o indazolilo; R1 es H, alquilo, alcoxi, hidroxialquileno, OH, halo, fenilo, triazolilo, oxazolilo, isoxazolilo, piridilo, pirimidinilo, pirazinilo, piridazinilo, piperazinilo, pirazolilo, oxadiazolilo, pirrolidinilo, tiofenilo, morfolinilo o dialquilamino, en donde fenilo, triazolilo, oxazolilo, isoxazolilo, piridilo, pirimidinilo, pirazinilo, piridazinilo, piperazinilo, pirazolilo, oxadiazolilo, pirrolidinilo, tiofenilo o morfolinilo están opcionalmente sustituidos con hasta dos sustituyentes seleccionados del grupo que consiste en halo y alquilo; R2 es H, alquilo, alcoxi, hidroxialquileno o halo; Z es NH, N-alquilo u O; R5 es piridilo, pirimidinilo, pirazinilo, piridazinilo, quinazolinilo, quinoxalinilo, pirazolilo, tiazolilo, tiadiazolilo, benzoxazolilo, imidazopirazinilo o triazolopirazinilo, opcionalmente sustituido con uno o dos sustituyentes seleccionados independientemente del grupo que consiste en alquilo, ciano, alquilo carboxilato, alcoxi y halo; y n es 0 o 1, donde "alquilo" es un grupo alquilo de cadena lineal o ramificada que tiene de 1 a 12 átomos de carbono en la cadena o un grupo hidrocarburo no aromático monocíclico que tiene de 3 a 7 átomos de carbono y está opcionalmente sustituido con uno o más átomos de halógeno .
ES14717297.7T 2013-03-13 2014-03-12 7-azabicíclicos sustituidos y su uso para moduladores de receptores de orexina Active ES2659222T3 (es)

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US201361780428P 2013-03-13 2013-03-13
US201361780428P 2013-03-13
PCT/US2014/024322 WO2014159591A1 (en) 2013-03-13 2014-03-12 Substituted 7-azabicycles and their use as orexin receptor modulators

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Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
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
EP3115362B1 (en) * 2014-03-06 2019-06-12 Shanghai Haiyan Pharmaceutical Technology Co. Ltd. Piperidine derivatives as orexin receptor antagonist
MX364612B (es) 2014-06-27 2019-05-02 Anvil Int Llc Abrazadera ajustable y cubo para soporte de manguera flexible.
GB201415569D0 (en) 2014-09-03 2014-10-15 C4X Discovery Ltd Therapeutic Compounds
US9611262B2 (en) 2014-09-11 2017-04-04 Janssen Pharmaceutica Nv Substituted 2-azabicycles and their use as orexin receptor modulators
US10196383B2 (en) 2015-07-17 2019-02-05 Sunshine Lake Pharma Co., Ltd. Substituted quinazoline compounds and preparation and uses thereof
US10668066B2 (en) 2015-08-14 2020-06-02 Shanghai Haiyan Pharmaceutical Technology Co., Ltd. Crystal form of orexin receptor antagonist compound, and preparation method and application thereof
CA2997543C (en) * 2015-09-04 2022-07-19 Janssen Pharmaceutica Nv Therapeutic compounds for pain and synthesis thereof
GB201601703D0 (en) * 2016-01-29 2016-03-16 C4X Discovery Ltd Therapeutic compounds
CA3059394C (en) * 2017-05-03 2023-09-12 Idorsia Pharmaceuticals Ltd Preparation of 2-([1,2,3]triazol-2-yl)-benzoic acid derivatives
PH12020500236B1 (en) * 2017-08-03 2023-12-06 Takeda Pharmaceuticals Co Heterocyclic compound and use thereof
CN107573294A (zh) * 2017-09-19 2018-01-12 四川大学 5‑甲基‑2‑(2h‑1,2,3‑三唑‑2‑基)苯甲酸的合成方法
GB201906914D0 (en) 2019-05-16 2019-07-03 Ucl Business Plc Substituted naphtahlene diimdes and their use
CA3140170A1 (en) * 2019-06-04 2020-12-10 Belew Mekonnen Imidazolo derivatives, compositions and methods as orexin antagonists
CN115379830A (zh) * 2020-04-17 2022-11-22 上海海雁医药科技有限公司 固体药物制剂及其制备方法和用途
AR122973A1 (es) * 2020-07-17 2022-10-19 Eisai R&D Man Co Ltd Compuestos de piperidina sustituida y su uso
US20250051322A1 (en) * 2022-01-14 2025-02-13 Eisai R&D Management Co., Ltd. Crystal of substituted piperidine compound, salts of substituted piperidine compound, and crystals thereof
JP7591592B2 (ja) * 2022-01-14 2024-11-28 エーザイ・アール・アンド・ディー・マネジメント株式会社 置換ピペリジン化合物を含有する医薬
ES3038762A1 (es) * 2024-04-12 2025-10-14 Moehs Iberica Sl Procedimiento de síntesis de ácido 5-metoxi-2-(2H-1,2,3-triazol-2yl)benzoico, sal sódica de dicho ácido como intermedio de síntesis y uso del ácido o de su sal en la preparación de daridorexant y ciertos intermedios en la síntesis del mismo

Family Cites Families (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3674793A (en) 1967-03-29 1972-07-04 Sterling Drug Inc 6-hydroxy-2-azabicyclo(2.2.2)octan-3-ones and 2-azabicyclo(2.2.2.)octane-3,6-diones
US6505492B2 (en) 2001-04-11 2003-01-14 Bethlehem Steel Corporation Method and apparatus for forming deep-drawn articles
EP1396488A1 (en) 2001-05-23 2004-03-10 Mitsubishi Pharma Corporation Fused heterocyclic compound and medicinal use thereof
EP1594852A1 (en) 2003-02-07 2005-11-16 Ranbaxy Laboratories, Ltd. Oxazolidinone derivatives as antimicrobials
MXPA05008108A (es) 2003-02-21 2005-09-21 Pharmacia & Upjohn Co Llc Exo-(2r)(+))-2-amino-7-azabiciclo[2.2.1]heptan-7-carboxilato de terc-butilo, compuestos intermedios y procedimiento para prepararlos y aislarlos.
KR20080076962A (ko) 2005-12-20 2008-08-20 노파르티스 아게 대사성 글루타메이트 수용체 조절제로서의 니코틴산 유도체
EP2272509A1 (en) 2006-09-11 2011-01-12 Novartis AG New Uses of metabotropic glutamate receptors
WO2008065626A2 (en) 2006-12-01 2008-06-05 Actelion Pharmaceuticals Ltd 3-heteroaryl (amino or amido)-1- (biphenyl or phenylthiazolyl) carbonylpiperidine derivativesas orexin receptor inhibitors
AR064561A1 (es) 2006-12-28 2009-04-08 Actelion Pharmaceuticals Ltd Derivados de 2-aza-biciclo[3.1.0]hexano y su uso en la preparacion de un medicamento para el tratamiento de enfermedades relacionadas con disfunciones generales del sistema de la orexina.
WO2008150364A1 (en) * 2007-05-23 2008-12-11 Merck & Co., Inc. Cyclopropyl pyrrolidine orexin receptor antagonists
JP5301539B2 (ja) 2007-07-17 2013-09-25 ブリストル−マイヤーズ スクイブ カンパニー Ｇｐｒ１１９ｇタンパク質共役受容体の調節方法および選択された化合物
BRPI0821141A2 (pt) 2007-12-21 2015-06-16 Hoffmann La Roche Derivados de heteroarila como antagonistas do receptor de orexina
RU2010138640A (ru) * 2008-02-21 2012-03-27 Актелион Фармасьютиклз Лтд (Ch) Производные 2-аза-бицикло [2.2.1] гептана
KR20100135962A (ko) 2008-04-30 2010-12-27 액테리온 파마슈티칼 리미티드 피페리딘 및 피롤리딘 화합물
WO2010009195A1 (en) 2008-07-16 2010-01-21 Schering Corporation Bicyclic heterocycle derivatives and use thereof as gpr119 modulators
US8710076B2 (en) 2008-10-21 2014-04-29 Merck Sharp & Dohme Corp. 2,5-disubstituted piperidine orexin receptor antagonists
EP2350061B1 (en) 2008-10-21 2013-08-14 Merck Sharp & Dohme Corp. 2,3-disubstituted piperidine orexin receptor antagonists
TW201033190A (en) 2008-12-02 2010-09-16 Glaxo Group Ltd Novel compounds
DE102009015516A1 (de) 2009-04-02 2010-10-07 Mediri Gmbh Verfahren und Vorrichtung zur Ermittlung von T2 und T2* mittels Magnet- Resonanz-Tomographie
AR076024A1 (es) 2009-04-03 2011-05-11 Schering Corp Derivados de heterociclos biciclicos puenteados y metodos de uso de los mismos
KR20120007061A (ko) 2009-04-24 2012-01-19 글락소 그룹 리미티드 오렉신 길항제로서 사용되는 3-아자비시클로［4.1.0］헵탄
WO2011050200A1 (en) 2009-10-23 2011-04-28 Janssen Pharmaceutica Nv Fused heterocyclic compounds as orexin receptor modulators
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
ES2735411T3 (es) 2009-10-23 2019-12-18 Janssen Pharmaceutica Nv Octahidropirrolo[3,4-c]pirroles disustituidos como moduladores del receptor de orexina
CA2778684A1 (en) 2009-10-29 2011-05-05 Schering Corporation Bridged bicyclic piperidine derivatives and methods of use thereof
WO2011066137A1 (en) 2009-11-24 2011-06-03 Schering Corporation Substituted biaryl derivatives and methods of use thereof
CA2781390A1 (en) 2009-12-14 2011-06-23 Inspire Pharmaceuticals, Inc. Bridged bicyclic rho kinase inhibitor compounds, composition and use
WO2011087812A1 (en) 2009-12-21 2011-07-21 Vanderbilt University Alkyl 3-((2-amidoethyl)amino)-8-azabicyclo[3.2.1]octane-8-carboxylate analogs as selective m1 agonists and methods of making and using same
WO2011093365A1 (ja) 2010-01-27 2011-08-04 協和発酵キリン株式会社 含窒素複素環化合物
UY33227A (es) 2010-02-19 2011-09-30 Novartis Ag Compuestos de pirrolopirimidina como inhibidores de la cdk4/6
US20130096141A1 (en) 2010-06-18 2013-04-18 Bernard R. Neustadt Bicyclic heterocycle derivatives and methods of use thereof
WO2012089606A1 (en) 2010-12-28 2012-07-05 Glaxo Group Limited Azabicyclo [4.1.0] hept - 4 - yl derivatives as human orexin receptor antagonists
US9586962B2 (en) 2011-04-20 2017-03-07 Janssen Pharmaceutica Nv Disubstituted octahydropyrrolo [3,4-C] pyrroles as orexin receptor modulators
AR088352A1 (es) 2011-10-19 2014-05-28 Merck Sharp & Dohme Antagonistas del receptor de 2-piridiloxi-4-nitrilo orexina
EP2911675A4 (en) 2012-10-23 2016-06-01 Merck Sharp & Dohme 2-PYRIDYLOXY-3-SUBSTITUTED 4-NITRIL-OREXINE RECEPTOR ANTAGONISTS
CN104918939B (zh) * 2012-11-16 2018-08-28 默沙东公司 人磷脂酰肌醇3-激酶δ的嘌呤抑制剂
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
KR20160118345A (ko) 2014-02-06 2016-10-11 애브비 인코포레이티드 6-헤테로아릴옥시- 및 6-아릴옥시-퀴놀린-2-카복사미드 및 이의 용도
US9611262B2 (en) 2014-09-11 2017-04-04 Janssen Pharmaceutica Nv Substituted 2-azabicycles and their use as orexin receptor modulators

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WO2014159591A1 (en) 2014-10-02
HK1219726A1 (en) 2017-04-13
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AU2014240388A1 (en) 2015-08-27
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