KR20120105449A - 오렉신 수용체 조절제로서의 이치환된 옥타하이드로피롤로［3,4-ｃ］피롤 - Google Patents

오렉신 수용체 조절제로서의 이치환된 옥타하이드로피롤로［3,4-ｃ］피롤 Download PDF

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KR20120105449A
KR20120105449A KR1020127013101A KR20127013101A KR20120105449A KR 20120105449 A KR20120105449 A KR 20120105449A KR 1020127013101 A KR1020127013101 A KR 1020127013101A KR 20127013101 A KR20127013101 A KR 20127013101A KR 20120105449 A KR20120105449 A KR 20120105449A
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South Korea
Prior art keywords
pyrrole
phenyl
triazol
carbonyl
fluoro
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Korean (ko)
Inventor
웨닝 차이
마이클 에이. 레타빅
키브 에스. 라이
다니엘 제이. 피펠
데일 에이. 루돌프
캐슬린 씨. 스트로더
브래드 엠. 사발
챈드라바댄 알. 샤
브락 티. 셔먼
아키놀라 소요데-존슨
에밀리 엠. 스톡킹
데빈 엠. 스완슨
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얀센 파마슈티카 엔.브이.
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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
    • C07D487/04—Ortho-condensed systems
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
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KR1020127013101A 2009-10-23 2010-10-21 오렉신 수용체 조절제로서의 이치환된 옥타하이드로피롤로［3,4-ｃ］피롤 Withdrawn KR20120105449A (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US25450909P 2009-10-23 2009-10-23
US61/254,509 2009-10-23

Related Child Applications (2)

Application Number Title Priority Date Filing Date
KR1020177034281A Division KR101859409B1 (ko) 2009-10-23 2010-10-21 오렉신 수용체 조절제로서의 이치환된 옥타하이드로피롤로［3,4-ｃ］피롤
KR1020177034279A Division KR101859400B1 (ko) 2009-10-23 2010-10-21 오렉신 수용체 조절제로서의 이치환된 옥타하이드로피롤로［3,4-ｃ］피롤

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KR20120105449A true KR20120105449A (ko) 2012-09-25

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KR1020127013101A Withdrawn KR20120105449A (ko) 2009-10-23 2010-10-21 오렉신 수용체 조절제로서의 이치환된 옥타하이드로피롤로［3,4-ｃ］피롤
KR1020177034281A Active KR101859409B1 (ko) 2009-10-23 2010-10-21 오렉신 수용체 조절제로서의 이치환된 옥타하이드로피롤로［3,4-ｃ］피롤
KR1020177034279A Active KR101859400B1 (ko) 2009-10-23 2010-10-21 오렉신 수용체 조절제로서의 이치환된 옥타하이드로피롤로［3,4-ｃ］피롤

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KR1020177034281A Active KR101859409B1 (ko) 2009-10-23 2010-10-21 오렉신 수용체 조절제로서의 이치환된 옥타하이드로피롤로［3,4-ｃ］피롤
KR1020177034279A Active KR101859400B1 (ko) 2009-10-23 2010-10-21 오렉신 수용체 조절제로서의 이치환된 옥타하이드로피롤로［3,4-ｃ］피롤

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20220136475A (ko) * 2016-03-10 2022-10-07 얀센 파마슈티카 엔.브이. 오렉신-2 수용체 길항제를 사용한 우울증의 치료 방법
US12378254B2 (en) 2009-10-23 2025-08-05 Janssen Pharmaceutica Nv Disubstituted octahydropyrrolo[3,4-c]pyrroles as orexin receptor modulators

Families Citing this family (64)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9586962B2 (en) 2011-04-20 2017-03-07 Janssen Pharmaceutica Nv Disubstituted octahydropyrrolo [3,4-C] pyrroles as orexin receptor modulators
US8501768B2 (en) * 2011-05-17 2013-08-06 Hoffmann-La Roche Inc. Hexahydrocyclopentapyrrolone, hexahydropyrrolopyrrolone, octahydropyrrolopyridinone and octahydropyridinone compounds
ES2572703T3 (es) 2011-11-08 2016-06-01 Actelion Pharmaceuticals Ltd. Derivados de 2-(1,2,3-triazol-2-il)benzamida y 3-(1,2,3-triazol-2-il)picolinamida como antagonistas del receptor de orexina
US9440982B2 (en) 2012-02-07 2016-09-13 Eolas Therapeutics, Inc. Substituted prolines/piperidines as orexin receptor antagonists
CA2863413A1 (en) 2012-02-07 2013-08-15 Eolas Therapeutics, Inc. Substituted prolines / piperidines as orexin receptor antagonists
CN104334544B (zh) 2012-06-04 2016-10-19 埃科特莱茵药品有限公司 苯并咪唑脯氨酸衍生物
DK2884978T3 (da) * 2012-08-16 2019-09-30 Scripps Research Inst Nye Kappa-opioidligander
MX2015004638A (es) 2012-10-10 2015-07-14 Actelion Pharmaceuticals Ltd Antagonistas de receptores de orexina los cuales son derivados de [orto bi-(hetero-) aril]-[2-meta bi-(hetero-) aril)-pirrolidin-1-il]-metanona.
CN103012293A (zh) * 2012-12-13 2013-04-03 同济大学 一种抗失眠药物mk-4305中间体的合成方法
CN105051040A (zh) 2013-03-12 2015-11-11 埃科特莱茵药品有限公司 作为食欲素受体拮抗剂的氮杂环丁烷酰胺衍生物
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
WO2015003002A1 (en) * 2013-07-03 2015-01-08 Abide Therapeutics, Inc. Pyrrolo-pyrrole carbamate and related organic compounds, pharmaceutical compositions, and medical uses thereof
CA2930053A1 (en) 2013-12-04 2015-06-11 Actelion Pharmaceuticals Ltd Use of benzimidazole-proline derivatives
WO2016020403A1 (en) * 2014-08-04 2016-02-11 Sandoz Ag Preparation of a benzoic acid derivative and its use for the preparation of suvorexant
EP3180332B1 (en) 2014-08-13 2021-10-27 Eolas Therapeutics Inc. Difluoropyrrolidines as orexin receptor modulators
WO2016040789A1 (en) 2014-09-11 2016-03-17 Janssen Pharmaceutica Nv Substituted 2-azabicycles and their use as orexin receptor modulators
AU2016295693B2 (en) 2015-07-17 2020-05-21 Sunshine Lake Pharma Co., Ltd. Substituted quinazoline compounds and preparation and uses thereof
JP6936224B2 (ja) * 2015-11-23 2021-09-15 サンシャイン・レイク・ファーマ・カンパニー・リミテッドＳｕｎｓｈｉｎｅ Ｌａｋｅ Ｐｈａｒｍａ Ｃｏ．，Ｌｔｄ． オクタヒドロピロロ［３，４−ｃ］ピロール誘導体およびその使用
WO2017088731A1 (zh) * 2015-11-24 2017-06-01 广东东阳光药业有限公司 八氢吡咯并[3,4-c]吡咯衍生物及其用途
EA036542B9 (ru) 2016-02-12 2020-12-22 Астразенека Аб Галоген-замещенные пиперидины в качестве модуляторов орексинового рецептора
US10030020B2 (en) 2016-05-12 2018-07-24 Abide Therapeutics, Inc. Spirocycle compounds and methods of making and using same
CN105949203B (zh) * 2016-05-24 2018-07-13 广东东阳光药业有限公司 八氢吡咯并[3,4-c]吡咯衍生物及其使用方法和用途
CN107759620B (zh) * 2016-08-16 2021-11-12 广东东阳光药业有限公司 八氢吡咯并[3,4-c]吡咯衍生物及其使用方法和用途
JOP20190107A1 (ar) 2016-11-16 2019-05-09 Lundbeck La Jolla Research Center Inc مثبطات أحادي أسيل جليسرول ليباز (magl)
CN108299437B (zh) * 2017-01-13 2022-07-08 广东东阳光药业有限公司 八氢吡咯并[3,4-c]吡咯衍生物及其用途
GB201702174D0 (en) * 2017-02-09 2017-03-29 Benevolentai Bio Ltd Orexin receptor antagonists
EP3619199B1 (en) 2017-05-03 2021-07-07 Idorsia Pharmaceuticals Ltd Preparation of 2-([1,2,3]triazol-2-yl)-benzoic acid derivatives
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
EP3675848B1 (en) 2017-08-29 2022-03-23 H. Lundbeck A/S Spirocycle compounds and methods of making and using same
EP3675847B1 (en) 2017-08-29 2023-07-12 H. Lundbeck A/S Spirocycle compounds and methods of making and using same
EP3668864B1 (en) 2017-09-28 2021-07-21 Boehringer Ingelheim International GmbH N-(2,2-difluoroethyl)-n-[(pyrimidinylamino)propanyl]arylcarboxamides
CN109988171A (zh) * 2017-12-29 2019-07-09 广东东阳光药业有限公司 八氢吡咯并[3,4-c]吡咯衍生物及其用途
CN109988169B (zh) * 2017-12-29 2022-02-01 广东东阳光药业有限公司 八氢吡咯并[3,4-c]吡咯衍生物及其用途
CN109988170B (zh) * 2017-12-29 2022-04-26 广东东阳光药业有限公司 八氢吡咯并[3,4-c]吡咯衍生物及其用途
GB201809295D0 (en) 2018-06-06 2018-07-25 Institute Of Cancer Res Royal Cancer Hospital Lox inhibitors
US20210169883A1 (en) * 2018-07-27 2021-06-10 Icahn School Of Medicine At Mount Sinai Method of treating aggression with orexin receptor antagonists
HUE066708T2 (hu) * 2018-11-14 2024-09-28 Janssen Pharmaceutica Nv Javított szintéziseljárás orexin receptor modulátor kondenzált heterociklusos vegyületek elõállítására
GB201818750D0 (en) 2018-11-16 2019-01-02 Institute Of Cancer Res Royal Cancer Hospital Lox inhibitors
CN112142713A (zh) * 2019-06-27 2020-12-29 山东润博生物科技有限公司 一种咪草烟的合成方法
BR112022002128A2 (pt) * 2019-08-07 2022-06-07 Janssen Pharmaceutica Nv Métodos sintéticos aprimorados para produção de compostos de (2h-1,2,3-triazol-2-il)fenila como moduladores do receptor de orexina
CN112876481B (zh) * 2019-11-29 2022-07-26 广东东阳光药业有限公司 八氢吡咯并[3,4-c]吡咯衍生物的晶型
CN112876479B (zh) * 2019-11-29 2022-07-26 广东东阳光药业有限公司 八氢吡咯并[3,4-c]吡咯衍生物的晶型
CN112876477B (zh) * 2019-11-29 2022-07-26 广东东阳光药业有限公司 八氢吡咯并[3,4-c]吡咯衍生物的晶型
CN112876480B (zh) * 2019-11-29 2022-07-26 广东东阳光药业有限公司 八氢吡咯并[3,4-c]吡咯衍生物的晶型
CN112876478B (zh) * 2019-11-29 2022-07-26 广东东阳光药业有限公司 八氢吡咯并[3,4-c]吡咯衍生物的晶型
WO2022122009A1 (zh) * 2020-12-11 2022-06-16 苏州晶云药物科技股份有限公司 吡咯类衍生化合物的晶型及其制备方法
KR20230159482A (ko) * 2021-03-16 2023-11-21 상하이 한서 바이오메디컬 컴퍼니 리미티드 질소-함유 헤테로사이클릭 폴리사이클릭 화합물, 이의 제조방법 및 이의 용도
CN114063673B (zh) * 2021-11-09 2023-03-03 万华化学集团股份有限公司 一种反应釜温度控制方法、系统及存储介质
CN116217593B (zh) * 2021-12-02 2025-05-09 江苏恩华药业股份有限公司 一种八氢吡咯并[3,4-c]吡咯甲基酮衍生物及其应用
EP4482838A1 (en) 2022-02-24 2025-01-01 Teva Czech Industries s.r.o Solid state forms of seltorexant
WO2023180556A1 (en) 2022-03-24 2023-09-28 Janssen Pharmaceutica Nv Methods for treating agitation in subjects with mild cognitive impairment or major neurocognition disorder
WO2024015503A1 (en) * 2022-07-15 2024-01-18 Biogen Ma Inc. Emopamil-binding protein inhibitors and uses thereof
CA3266204A1 (en) * 2022-09-14 2025-03-19 Shanghai Hansoh Biomedical Co., Ltd. FREE CRYSTALLINE BASIC FORM OF A POLYCYCLIC NITROGEN HETEROCYCLE COMPOUND AND ITS PREPARATION PROCESS
EP4471034A4 (en) * 2022-11-23 2025-06-18 Jiangsu NHWA Pharmaceutical Co., Ltd DISUBSTITUTED OCTAHYDROPYRROLO[3,4-C PYRROL METHYL KETONE DERIVATIVE AND ITS USE
TW202440545A (zh) * 2022-12-12 2024-10-16 大陸商江蘇恩華藥業股份有限公司 取代四氫環戊基〔ｃ〕吡咯衍生物、製備方法、中間體及其用途
WO2024189472A1 (en) 2023-03-14 2024-09-19 Janssen Pharmaceutica Nv Improved synthetic methods of making substituted pyrimidine intermediates for synthesis of orexin receptor modulators
WO2025003991A1 (en) 2023-06-29 2025-01-02 Janssen Pharmaceutica Nv Method of treating depression using seltorexant
WO2025162233A1 (zh) * 2024-01-29 2025-08-07 成都康弘药业集团股份有限公司 食欲素受体调节剂及其制备方法和用途
WO2025242852A1 (en) 2024-05-24 2025-11-27 Janssen Pharmaceutica Nv Seltorexant for use in treating major depressive disorder with insomnia symptoms
CN118580243B (zh) * 2024-08-07 2025-01-03 艾斯拓康生物医药(天津)有限公司 一类含氮并环化合物及其制备方法和应用
CN119039301B (zh) * 2024-10-31 2025-09-02 江苏豪森药业集团有限公司 一种含氮杂环的多环化合物晶型ⅰ的制备方法

Family Cites Families (152)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL7503310A (nl) 1975-03-20 1976-09-22 Philips Nv Verbindingen met antidepressieve werking.
GB1526331A (en) 1976-01-14 1978-09-27 Kefalas As Phthalanes
JPH11510478A (ja) 1995-06-06 1999-09-14 アボツト・ラボラトリーズ キノリジノン型化合物
GB9519563D0 (en) 1995-09-26 1995-11-29 Merck Sharp & Dohme Therapeutic agents
WO2000055143A1 (en) 1999-03-17 2000-09-21 F. Hoffmann-La Roche Ag Oxazolone derivatives and their use as alpha-1 adrenoreceptor modulators
US6375897B1 (en) 2000-02-14 2002-04-23 Ansys Technologies, Inc. Urine collection cup
US6809105B2 (en) 2000-04-27 2004-10-26 Abbott Laboratories Diazabicyclic central nervous system active agents
MY145722A (en) 2000-04-27 2012-03-30 Abbott Lab Diazabicyclic central nervous system active agents
WO2001085693A1 (en) 2000-05-11 2001-11-15 Banyu Pharmaceutical Co., Ltd. N-acyltetrahydroisoquinoline derivatives
SE0100326D0 (sv) 2001-02-02 2001-02-02 Astrazeneca Ab New compounds
WO2002070527A1 (en) 2001-03-02 2002-09-12 Akzo Nobel N.V. Mass-selective purification of organometallics
EP1368354A1 (en) 2001-03-07 2003-12-10 Pfizer Products Inc. Modulators of chemokine receptor activity
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
US6455722B1 (en) 2001-06-29 2002-09-24 Pabu Services, Inc. Process for the production of pentaerythritol phosphate alcohol
GB2383315B (en) 2001-12-18 2005-04-06 Christopher Donald Clarke Vehicle imaging system
GB0130341D0 (en) 2001-12-19 2002-02-06 Smithkline Beecham Plc Compounds
DE10226943A1 (de) 2002-06-17 2004-01-08 Bayer Ag Phenylaminopyrimidine und ihre Verwendung
MXPA04002269A (es) * 2002-07-09 2004-06-29 Actelion Pharmaceuticals Ltd Derivados de 7,8,9,10-tetrahidro-6h-azepino,6,7,8,9-tetrahidro-pirido y 2,3-dihidro-2h-pirrolo[2,1-b]-quinazolinona.
DE60335891D1 (de) 2002-10-11 2011-03-10 Actelion Pharmaceuticals Ltd Sulphonylaminoessigsaeure derivate und deren verwendung als orexin rezeptor antagoniste
GB0225944D0 (en) 2002-11-06 2002-12-11 Glaxo Group Ltd Novel compounds
AU2004224156B2 (en) 2003-03-26 2010-08-12 Actelion Pharmaceuticals Ltd. Tetrahydroisoquinolyl acetamide derivatives for use as orexin receptor antagonists
DE602004011204T2 (de) 2003-04-28 2008-12-24 Actelion Pharmaceuticals Ltd. Quinoxalin-3-on-verdindungen als orexin-rezeptor antagonisten.
US20040242641A1 (en) 2003-05-27 2004-12-02 Buckley Michael J. (1S,5S)-3-(5,6-dichloro-3-pyridinyl)-3,6-diazabicyclo[3.2.0]heptane is an effective analgesic agent
WO2005005439A1 (en) 2003-07-09 2005-01-20 Suven Life Sciences Limited Benzothiazino indoles
TW200507850A (en) 2003-07-25 2005-03-01 Kyowa Hakko Kogyo Kk Pharmaceutical composition
WO2005023231A1 (en) 2003-09-10 2005-03-17 MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. Polypyrimidine tract binding protein promotes insulin secretory granule biogenesis
US20050065178A1 (en) 2003-09-19 2005-03-24 Anwer Basha Substituted diazabicycloakane derivatives
US7399765B2 (en) 2003-09-19 2008-07-15 Abbott Laboratories Substituted diazabicycloalkane derivatives
WO2005060968A1 (en) 2003-12-11 2005-07-07 Sepracor Inc. Combination of a sedative and a neurotransmitter modulator, and methods for improving sleep quality and treating depression
HUP0400405A3 (en) 2004-02-10 2009-03-30 Sanofi Synthelabo Pyrimidine derivatives, process for producing them, their use, pharmaceutical compositions containing them and their intermediates
CN1926109B (zh) 2004-03-01 2011-04-13 埃科特莱茵药品有限公司 经取代的1,2,3,4-四氢异喹啉衍生物
JP4845873B2 (ja) 2004-03-03 2011-12-28 ケモセントリックス インコーポレーティッド 二環式および架橋した窒素複素環
US7435831B2 (en) 2004-03-03 2008-10-14 Chemocentryx, Inc. Bicyclic and bridged nitrogen heterocycles
US7226931B2 (en) 2004-07-22 2007-06-05 Cumbre Pharmaceuticals Inc. (R/S) rifamycin derivatives, their preparations and pharmaceutical compositions
WO2006012396A1 (en) 2004-07-22 2006-02-02 Glaxo Group Limited Antibacterial agents
FR2874011B1 (fr) 2004-08-03 2007-06-15 Sanofi Synthelabo Derives de sulfonamides, leur preparation et leur application en therapeutique
JP2008519078A (ja) 2004-11-04 2008-06-05 ニューロゲン コーポレイション Ｃｂ１拮抗薬としてのアリールアルキル尿素類
EP1846409A1 (en) 2004-11-24 2007-10-24 Pfizer Limited Octahydropyrrolo[3,4-c]pyrrole derivatives
DE102004061344A1 (de) 2004-12-20 2006-07-06 Siemens Ag Verfahren zur sicheren Auslegung eines Systems, zugehörige Systemkomponente und Software
WO2006124897A2 (en) 2005-05-13 2006-11-23 Lexicon Genetics Incorporated Methods and compositions for improving cognition
ZA200709626B (en) * 2005-05-13 2009-02-25 Lexicon Pharmaceuticals Inc Multicyclic compounds and methods of their use
GB0510204D0 (en) * 2005-05-19 2005-06-22 Chroma Therapeutics Ltd Enzyme inhibitors
US20080175795A1 (en) 2005-06-30 2008-07-24 Bexel Pharmaceuticals, Inc. Novel derivatives of amino acids for treatment of obesity and related disorders
GB0514018D0 (en) 2005-07-07 2005-08-17 Ionix Pharmaceuticals Ltd Chemical compounds
JP2009506061A (ja) 2005-08-26 2009-02-12 メルク エンド カムパニー インコーポレーテッド ジアザスピロデカンオレキシン受容体拮抗薬
FR2896798A1 (fr) 2006-01-27 2007-08-03 Sanofi Aventis Sa Derives de sulfonamides, leur preparation et leur application en therapeutique
FR2896799B1 (fr) 2006-02-02 2008-03-28 Sanofi Aventis Sa Derives de sulfonamides, leur preparation et leur application en therapeutique
US7553836B2 (en) 2006-02-06 2009-06-30 Bristol-Myers Squibb Company Melanin concentrating hormone receptor-1 antagonists
WO2007126935A2 (en) 2006-03-29 2007-11-08 Merck & Co., Inc. Diazepan orexin receptor antagonists
US20090105318A1 (en) 2006-03-29 2009-04-23 Coleman Paul J Amidoethylthioether Orexin Receptor Antagonists
US7834028B2 (en) 2006-04-26 2010-11-16 Actelion Pharmaceuticals Ltd. Pyrazolo-tetrahydro pyridine derivatives as orexin receptor antagonists
WO2007146761A2 (en) 2006-06-12 2007-12-21 Neurogen Corporation Diaryl pyrimidinones and related compounds
EP2049529B1 (en) 2006-07-14 2010-08-11 Merck Sharp & Dohme Corp. Substituted diazepan orexin receptor antagonists
AU2007272854B2 (en) 2006-07-14 2013-08-01 Merck Sharp & Dohme Corp. Bridged diazepan orexin receptor antagonists
JP2009543790A (ja) 2006-07-14 2009-12-10 メルク エンド カムパニー インコーポレーテッド ２−置換プロリンビス−アミドオレキシン受容体アンタゴニスト
AU2007285371A1 (en) 2006-08-15 2008-02-21 Actelion Pharmaceuticals Ltd. Azetidine compounds as orexin receptor antagonists
WO2008026149A1 (en) 2006-08-28 2008-03-06 Actelion Pharmaceuticals Ltd 1,4,5,6, 7,8-hexahydro-i^1s-triaza-azulene derivatives as orexin receptor antagonists
ATE472549T1 (de) 2006-09-18 2010-07-15 Hoffmann La Roche Octahydropyrroloä3,4-cüpyrrolderivate und ihre verwendung als antivirale mittel
US20100016401A1 (en) 2006-09-29 2010-01-21 Actelion Phamaceuticals Ltd. 3-aza-bicyclo[3.1.0]hexane derivatives
WO2008052139A2 (en) 2006-10-25 2008-05-02 Somaxon Pharmaceuticals, Inc. Ultra low dose doxepin and methods of using the same to treat sleep disorders
US20080153811A1 (en) 2006-11-07 2008-06-26 Joseph Barbosa Methods of Treating Cognitive Impairment and Dementia
PE20081229A1 (es) 2006-12-01 2008-08-28 Merck & Co Inc Antagonistas de receptor de orexina de diazepam sustituido
US20110077200A1 (en) 2006-12-06 2011-03-31 Somaxon Pharmaceuticals, Inc. Combination therapy using low-dose doxepin for the improvement of sleep
RU2009127842A (ru) 2006-12-22 2011-01-27 Актелион Фармасьютиклз Лтд (Ch) ПРОИЗВОДНЫЕ 5,6,7,8-ТЕТРАГИДРОИМИДАЗО[1.5-а]ПИРАЗИНА
CL2008000836A1 (es) 2007-03-26 2008-11-07 Actelion Pharmaceuticals Ltd Compuestos derivados de tiazolidina, antagonistas del receptor de orexina; composicion farmaceutica que los comprende; y su uso en el tratamiento de neurosis emocional, depresion grave, trastornos psicoticos, alzheimer, parkinson, dolor, entre otras.
US7851622B2 (en) 2007-04-25 2010-12-14 Bristol-Myers Squibb Company Non-basic melanin concentrating hormone receptor-1 antagonists
WO2008143856A1 (en) 2007-05-18 2008-11-27 Merck & Co., Inc. Oxo bridged diazepan orexin receptor antagonists
FR2918061B1 (fr) 2007-06-28 2010-10-22 Sanofi Aventis Derives de 6-cycloamino-3-(pyridin-4-yl)imidazo°1,2-b!- pyridazine,leur preparation et leur application en therapeutique.
EA201070091A1 (ru) 2007-07-03 2010-06-30 Глэксо Груп Лимитед Производные пиперидина, пригодные в качестве антагонистов рецептора орексина
GB0712888D0 (en) 2007-07-03 2007-08-15 Glaxo Group Ltd Novel compounds
AU2008272449A1 (en) 2007-07-03 2009-01-08 Actelion Pharmaceuticals Ltd 3-aza-bicyclo[3.3.0]octane compounds
US20090011994A1 (en) 2007-07-06 2009-01-08 Bristol-Myers Squibb Company Non-basic melanin concentrating hormone receptor-1 antagonists and methods
WO2009011775A1 (en) 2007-07-13 2009-01-22 Merck & Co., Inc. Amidoethyl alkylamino orexin receptor antagonists
FR2918986B1 (fr) * 2007-07-19 2009-09-04 Sanofi Aventis Sa Derives de 6-cycloamino-3-(pyridazin-4-yl)imidazo[1,2-b]- pyridazine, leur preparation et leur application en therapeutique
CN101874028B (zh) 2007-07-27 2012-11-14 埃科特莱茵药品有限公司 2-氮杂-二环[3.3.0]辛烷衍生物
BRPI0814767A2 (pt) 2007-08-02 2015-03-03 Hoffmann La Roche Derivados de monoamida como antagonistas do receptor de orexina
WO2009022311A2 (en) 2007-08-15 2009-02-19 Actelion Pharmaceuticals Ltd 1,2-diamido-ethylene derivatives as orexin antagonists
EP2207778A2 (en) 2007-09-24 2010-07-21 Actelion Pharmaceuticals Ltd. Pyrrolidines and piperidines as orexin receptor antagonists
CA2703904A1 (en) 2007-10-29 2009-05-07 Merck Sharp & Dohme Corp. Substituted diazepan orexin receptor antagonists
DE102007052177A1 (de) 2007-10-30 2009-05-07 Novega Produktionssysteme Gmbh Ortungsbake
EP2058001A1 (en) 2007-11-08 2009-05-13 Crossbeta Biosciences B.V. Enhancement of immunogenicity of antigens
BRPI0821676A2 (pt) 2007-12-21 2015-06-16 Astrazeneca Ab Composto, composição farmacêutica, e, processo para a preparação dos compostos.
KR101204213B1 (ko) 2007-12-21 2012-11-26 에프. 호프만-라 로슈 아게 오렉신 수용체 길항제로서의 헤테로아릴 유도체
GB0806536D0 (en) 2008-04-10 2008-05-14 Glaxo Group Ltd Novel compounds
KR20110022631A (ko) 2008-05-27 2011-03-07 인트라-셀룰라 써래피스, 인코퍼레이티드. 수면 장애 및 다른 장애를 치료하기 위한 방법 및 조성물
CA2731403C (en) 2008-07-29 2013-11-05 F. Hoffmann-La Roche Ag Pyrrolidin-3-ylmethyl-amine as orexin antagonists
AR072899A1 (es) 2008-08-07 2010-09-29 Merck Sharp & Dohme Derivados de terpiridina-carboxamida antagonistas de receptores de orexina, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento del insomnio y la obesidad.
US8129384B2 (en) 2008-10-09 2012-03-06 Glaxo Group Limited Imidazo[1,2-a]pyrazines as orexin receptor antagonists
US20100267730A1 (en) 2008-10-09 2010-10-21 Giuseppe Alvaro Novel compounds
US8093255B2 (en) 2008-10-09 2012-01-10 Glaxo Group Limited Imidazo[1,2-A]pyrimidines as orexin receptor antagonists
EP2348856B1 (en) 2008-10-21 2013-08-14 Merck Sharp & Dohme Corp. 2,4-disubstituted pyrrolidine orexin receptor antagonists
JP2012506379A (ja) 2008-10-21 2012-03-15 メルク・シャープ・エンド・ドーム・コーポレイション 二置換アゼパンオレキシン受容体アンタゴニスト
US8466281B2 (en) 2008-10-21 2013-06-18 Merck Sharp & Dohme Corp. 2,5-disubstituted morpholine orexin receptor antagonists
JP2012506378A (ja) 2008-10-21 2012-03-15 メルク・シャープ・エンド・ドーム・コーポレイション ２，３−二置換フェニルカルボキサミド・オレキシン受容体アンタゴニスト
EP2349269A4 (en) 2008-10-21 2012-04-25 Merck Sharp & Dohme 2,5-DISUBSTITUTED PIPERIDINOREXINE RECEPTOR ANTAGONISTS
US8669272B2 (en) 2008-10-21 2014-03-11 Merck Sharp & Dohme Corp. 2,5-disubstituted piperidine orexin receptor antagonists
JP2012507540A (ja) 2008-10-30 2012-03-29 メルク・シャープ・エンド・ドーム・コーポレイション ピリダジンカルボキサミド・オレキシン受容体アンタゴニスト
KR101320245B1 (ko) 2008-10-30 2013-10-30 머크 샤프 앤드 돔 코포레이션 이소니코틴아미드 오렉신 수용체 길항제
JP2012507539A (ja) 2008-10-30 2012-03-29 メルク・シャープ・エンド・ドーム・コーポレイション ２，５−二置換フェニルカルボキサミド・オレキシン受容体アンタゴニスト
WO2010060471A1 (en) 2008-11-26 2010-06-03 Glaxo Group Limited Piperidine derivatives useful as orexin receptor antagonists
EP2358711A1 (en) 2008-11-26 2011-08-24 Glaxo Group Limited Piperidine derivatives useful as orexin receptor antagonists
WO2010060472A1 (en) 2008-11-26 2010-06-03 Glaxo Group Limited Imidazopyridazine derivatives acting as orexin antagonists
AU2009324239A1 (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
TW201031407A (en) 2008-12-02 2010-09-01 Glaxo Group Ltd Novel compounds
GB0823467D0 (en) 2008-12-23 2009-01-28 Glaxo Group Ltd Novel Compounds
US20100214135A1 (en) 2009-02-26 2010-08-26 Microsoft Corporation Dynamic rear-projected user interface
CN102459229A (zh) 2009-04-24 2012-05-16 葛兰素集团有限公司 用作食欲肽拮抗剂的3-氮杂二环[4.1.0]庚烷
EP2470525A1 (en) 2009-08-24 2012-07-04 Glaxo Group Limited Piperidine derivatives used as orexin antagonists
JP2013502447A (ja) 2009-08-24 2013-01-24 グラクソ グループ リミテッド 睡眠障害の治療のためのオレキシン受容体アンタゴニストとしての５−メチル−ピペリジン誘導体
WO2011050200A1 (en) 2009-10-23 2011-04-28 Janssen Pharmaceutica Nv 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
MX2012004753A (es) 2009-10-23 2012-09-07 Janssen Pharmaceutica Nv Octahidropirrolo[3,4-c]pirrolos disustituidos como moduladores del receptor de orexina.
WO2011050199A1 (en) 2009-10-24 2011-04-28 Anantha Shekhar Methods and compositions for panic disorders
TWI410630B (zh) 2009-11-10 2013-10-01 Ct Lab Inc 一種用以治療與食慾素受體１、食慾素受體２、體抑素受體２或多巴胺ｄ２ｌ受體相關之疾病的方法和組合物
BR112012015248B1 (pt) 2009-12-23 2022-01-04 Jasco Pharmaceuticals, LLC Composto
BR112013013695A2 (pt) 2010-12-17 2016-09-13 Taisho Pharmaceutical Co Ltd derivado de pirazol
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
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
EP2708537A4 (en) 2011-05-10 2014-10-01 Taisho Pharmaceutical Co Ltd HETEROAROMATIC RING DERIVATIVE
TW201315730A (zh) 2011-07-05 2013-04-16 大正製藥股份有限公司 甲基哌啶衍生物
EP2768305A4 (en) 2011-10-21 2015-04-29 Merck Sharp & Dohme 2,5-DISUBSTITUTED THIOMORPHOLIN OREXINE RECEPTOR ANTAGONISTS
US9440982B2 (en) 2012-02-07 2016-09-13 Eolas Therapeutics, Inc. Substituted prolines/piperidines as orexin receptor antagonists
CA2863413A1 (en) 2012-02-07 2013-08-15 Eolas Therapeutics, Inc. Substituted prolines / piperidines as orexin receptor antagonists
US9493481B2 (en) 2012-02-23 2016-11-15 Vanderbilt University Substituted 5-aminothieno[2,3—C]pyridazine-6-carboxamide analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M4
JP2014015452A (ja) 2012-06-15 2014-01-30 Taisho Pharmaceutical Co Ltd ピラゾール誘導体を含有する医薬
NZ702647A (en) 2012-06-15 2016-11-25 Taisho Pharmaceutical Co Ltd Heteroaromatic methyl cyclic amine derivative
US20150166523A1 (en) 2012-06-15 2015-06-18 Taisho Pharmaceutical Co., Ltd. Branched chain alkyl heteroaromatic ring derivative
JP2014111586A (ja) 2012-11-09 2014-06-19 Taisho Pharmaceutical Co Ltd ヘテロ芳香環誘導体を含有する医薬
EP2925321A4 (en) 2012-11-27 2016-04-27 Merck Sharp & Dohme 2-pyridylamino-4-nitrile-piperidinyl orexin receptor antagonists
JP2016028017A (ja) 2012-12-13 2016-02-25 大正製薬株式会社 フッ素置換ピペリジン化合物
JP2014141480A (ja) 2012-12-28 2014-08-07 Taisho Pharmaceutical Co Ltd メチルピペリジン誘導体を含有する医薬
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
WO2015018027A1 (en) 2013-08-08 2015-02-12 Merck Sharp & Dohme Corp. Thiazole orexin receptor antagonists
DK3076967T3 (da) 2013-12-03 2021-10-25 Intra Cellular Therapies Inc Fremgangsmåder til behandling af residuelle symptomer på skizofreni
US9586934B2 (en) 2013-12-09 2017-03-07 Merck Sharp & Dohme Corp. 2-pyridyloxy-4-methyl orexin receptor antagonists
JP2015131802A (ja) 2013-12-13 2015-07-23 大正製薬株式会社 分岐鎖アルキルヘテロ芳香環誘導体を含有する医薬
JP5930010B2 (ja) 2013-12-13 2016-06-08 大正製薬株式会社 ヘテロ芳香環メチル環状アミン誘導体を含有する医薬
WO2015095108A1 (en) 2013-12-18 2015-06-25 Merck Sharp & Dohme Corp. Thioether-piperidinyl orexin receptor antagonists
TW201613891A (en) 2014-02-12 2016-04-16 Eolas Therapeutics Inc Substituted prolines / piperidines as orexin receptor antagonists
TW201613864A (en) 2014-02-20 2016-04-16 Takeda Pharmaceutical Novel compounds
JP2017100950A (ja) 2014-04-04 2017-06-08 大正製薬株式会社 オキソ複素環誘導体
JP2017100951A (ja) 2014-04-04 2017-06-08 大正製薬株式会社 オキサゾリジノン及びオキサジナノン誘導体
CN105377840B (zh) 2014-05-28 2017-12-22 杭州普晒医药科技有限公司 一种二氮杂环庚烷化合物的盐及其晶型与无定型物
EP3180332B1 (en) 2014-08-13 2021-10-27 Eolas Therapeutics Inc. Difluoropyrrolidines as orexin receptor modulators
US20160051533A1 (en) 2014-08-20 2016-02-25 Ladd Research LLC Diagnosis and pharmacological treatment of seasonal affective disorder and symptoms of seasonality
GB201415569D0 (en) 2014-09-03 2014-10-15 C4X Discovery Ltd Therapeutic Compounds
AU2016295693B2 (en) 2015-07-17 2020-05-21 Sunshine Lake Pharma Co., Ltd. Substituted quinazoline compounds and preparation and uses thereof
GB201601703D0 (en) 2016-01-29 2016-03-16 C4X Discovery Ltd Therapeutic compounds
UA125873C2 (uk) * 2016-03-10 2022-06-29 Янссен Фармацевтика Нв Спосіб лікування депресії з використанням антагоністів рецептора орексин-2
US20210169883A1 (en) 2018-07-27 2021-06-10 Icahn School Of Medicine At Mount Sinai Method of treating aggression with orexin receptor antagonists
GB201820458D0 (en) 2018-12-14 2019-01-30 Heptares Therapeutics Ltd Ox1 antagonists

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US12378254B2 (en) 2009-10-23 2025-08-05 Janssen Pharmaceutica Nv Disubstituted octahydropyrrolo[3,4-c]pyrroles as orexin receptor modulators
KR20220136475A (ko) * 2016-03-10 2022-10-07 얀센 파마슈티카 엔.브이. 오렉신-2 수용체 길항제를 사용한 우울증의 치료 방법
US12201634B2 (en) 2016-03-10 2025-01-21 Janssen Pharmaceutica Nv Methods of treating depression using orexin-2 receptor antagonists

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