JP6088443B2 - イオンチャネルのモジュレーターとしてのモルホリン−スピロ環式ピペリジンアミド - Google Patents

イオンチャネルのモジュレーターとしてのモルホリン−スピロ環式ピペリジンアミド Download PDF

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JP6088443B2
JP6088443B2 JP2013558104A JP2013558104A JP6088443B2 JP 6088443 B2 JP6088443 B2 JP 6088443B2 JP 2013558104 A JP2013558104 A JP 2013558104A JP 2013558104 A JP2013558104 A JP 2013558104A JP 6088443 B2 JP6088443 B2 JP 6088443B2
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pain
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substituted
compound
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JP2014508169A5 (OSRAM
JP2014508169A (ja
Inventor
サラ サビーナ ハディダ−ルア,
サラ サビーナ ハディダ−ルア,
ヘイリー マリー ビンチ,
ヘイリー マリー ビンチ,
マイケル ポール デニノ,
マイケル ポール デニノ,
レブ タイラー デュイー ファニング,
レブ タイラー デュイー ファニング,
ブライアン エー. フリーマン,
ブライアン エー. フリーマン,
ピーター ディーデリック ジャン グルーテンフイ,
ピーター ディーデリック ジャン グルーテンフイ,
ニコール ヒルグラフ,
ニコール ヒルグラフ,
プラモド ジョシ,
プラモド ジョシ,
エドワード アダム カレル,
エドワード アダム カレル,
ジョセフ ポンティーロ,
ジョセフ ポンティーロ,
アリーナ セリーナ,
アリーナ セリーナ,
アービー ジャグディシュバイ セス,
アービー ジャグディシュバイ セス,
デニス ジェイムズ ハーリー,
デニス ジェイムズ ハーリー,
ヴィジャヤラクスミ アルムガム,
ヴィジャヤラクスミ アルムガム,
マーク トーマス ミラー,
マーク トーマス ミラー,
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/10Spiro-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
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    • A61P11/00Drugs for disorders of the respiratory system
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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Emergency Medicine (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Obesity (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Otolaryngology (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2013558104A 2011-03-14 2012-03-13 イオンチャネルのモジュレーターとしてのモルホリン−スピロ環式ピペリジンアミド Expired - Fee Related JP6088443B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201161452538P 2011-03-14 2011-03-14
US61/452,538 2011-03-14
US201161567809P 2011-12-07 2011-12-07
US61/567,809 2011-12-07
PCT/US2012/028882 WO2012125613A1 (en) 2011-03-14 2012-03-13 Morpholine-spirocyclic piperidine amides as modulators of ion channels

Publications (3)

Publication Number Publication Date
JP2014508169A JP2014508169A (ja) 2014-04-03
JP2014508169A5 JP2014508169A5 (OSRAM) 2015-04-30
JP6088443B2 true JP6088443B2 (ja) 2017-03-01

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JP2013558104A Expired - Fee Related JP6088443B2 (ja) 2011-03-14 2012-03-13 イオンチャネルのモジュレーターとしてのモルホリン−スピロ環式ピペリジンアミド

Country Status (9)

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US (2) US8828996B2 (OSRAM)
EP (1) EP2686325B1 (OSRAM)
JP (1) JP6088443B2 (OSRAM)
CN (1) CN103517910B (OSRAM)
AU (1) AU2012229187B2 (OSRAM)
CA (1) CA2829803A1 (OSRAM)
ES (1) ES2618929T3 (OSRAM)
MX (1) MX347982B (OSRAM)
WO (1) WO2012125613A1 (OSRAM)

Families Citing this family (52)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011140425A1 (en) 2010-05-06 2011-11-10 Vertex Pharmaceuticals Incorporated Heterocyclic chromene-spirocyclic piperidine amides as modulators of ion channels
RU2634900C2 (ru) 2011-02-02 2017-11-08 Вертекс Фармасьютикалз Инкорпорейтед Спироциклические пирролопиразин(пиперидин)амиды в качестве модуляторов ионных каналов
JP5940562B2 (ja) 2011-02-18 2016-06-29 バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated イオンチャネルのモジュレーターとしてのクロマン−スピロ環式ピペリジンアミド
US9403839B2 (en) 2012-01-16 2016-08-02 Vertex Pharmaceuticals Incorporated Pyran-spirocyclic piperidine amides as modulators of ion channels
RS56015B1 (sr) 2013-01-31 2017-09-29 Vertex Pharma Piridon amidi kao modulatori natrijumovih kanala
AR095192A1 (es) 2013-01-31 2015-09-30 Vertex Pharma Quinolina y quinazolinamidas como modulares de canales de sodio
CN105683157B (zh) 2013-07-19 2019-07-19 沃泰克斯药物股份有限公司 用作钠通道调节剂的磺酰胺类
JP6483666B2 (ja) 2013-10-14 2019-03-13 エーザイ・アール・アンド・ディー・マネジメント株式会社 選択的に置換されたキノリン化合物
WO2015057659A1 (en) 2013-10-14 2015-04-23 Eisai R&D Management Co., Ltd. Selectively substituted quinoline compounds
SI3080134T1 (sl) 2013-12-13 2018-11-30 Vertex Pharmaceuticals Incorporated Predzdravila piridon amidov uporabna kot modulatorji natrijevih kanalov
TW201615642A (zh) * 2014-06-02 2016-05-01 伊史帝夫博士實驗室股份有限公司 具有多重模式抗疼痛活性的1-氧雜-4,9-二氮雜螺十一烷化合物之醯胺衍生物
TW201615643A (zh) * 2014-06-02 2016-05-01 伊史帝夫博士實驗室股份有限公司 具有多重模式抗疼痛活性之1-氧雜-4,9-二氮雜螺十一烷化合物之烷基與芳基衍生物
TWI685497B (zh) * 2014-06-02 2020-02-21 西班牙商伊史帝夫製藥公司 具有多重模式抗疼痛活性的1-氧雜-4,9-二氮雜螺十一烷化合物之烷基衍生物
CN107849017B (zh) 2015-07-31 2021-03-30 辉瑞公司 作为magl抑制剂的1,1,1-三氟-3-羟基丙-2-基氨基甲酸酯衍生物及1,1,1-三氟-4-羟基丁-2-基氨基甲酸酯衍生物
AU2016343551A1 (en) * 2015-10-23 2018-04-19 Esteve Pharmaceuticals, S.A. Oxa-diazaspiro compounds having activity against pain
EP3365345B1 (en) * 2015-10-23 2020-02-26 Esteve Pharmaceuticals, S.A. Oxa-azaspiro compounds having activity against pain
JP6844822B2 (ja) * 2015-10-23 2021-03-17 エステベ ファーマシューティカルズ, ソシエダッド アノニマEsteve Pharmaceuticals, S.A. 疼痛に対して活性を有する置換モルホリン誘導体
HRP20221343T1 (hr) 2015-11-16 2022-12-23 Esteve Pharmaceuticals, S.A. Oksadiazaspiro spojevi za liječenje zlouporabe droga i ovisnosti
EA036086B1 (ru) * 2016-03-17 2020-09-24 Фмк Корпорейшн Способ превращения s-энантиомера в его рацемическую форму
AU2018208846A1 (en) 2017-01-20 2019-07-25 Pfizer Inc. 1,1,1-trifluoro-3-hydroxypropan-2-yl carbamate derivatives as magl inhibitors
WO2018134698A1 (en) 2017-01-23 2018-07-26 Pfizer Inc. Heterocyclic spiro compounds as magl inhibitors
US11358977B2 (en) 2017-05-16 2022-06-14 Vertex Pharmaceuticals Incorporated Deuterated pyridone amides and prodrugs thereof as modulators of sodium channels
JP7277431B2 (ja) 2017-07-11 2023-05-19 バーテックス ファーマシューティカルズ インコーポレイテッド ナトリウムチャネルのモジュレーターとしてのカルボキサミド
US11236110B2 (en) 2017-10-17 2022-02-01 Esteve Pharmaceuticals, S.A. Salts of (R)-9-(2,5-difluorophenethyl)-4-ethyl-2-methyl-1-oxa-4,9-diazaspiro[5.5]undecan-3-one
US11529337B2 (en) 2018-02-12 2022-12-20 Vertex Pharmaceuticals Incorporated Method of treating pain
SG11202100130QA (en) 2018-07-09 2021-02-25 Lieber Institute Inc Pyridine carboxamide compounds for inhibiting nav1.8
KR102840599B1 (ko) 2018-07-09 2025-07-29 리버 인스티튜트, 아이엔씨 Nav1.8을 억제하기 위한 피리다진(PYRIDAZINE) 화합물
US12440481B2 (en) 2019-01-10 2025-10-14 Vertex Pharmaceuticals Incorporated Esters and carbamates as modulators of sodium channels
US12441703B2 (en) 2019-01-10 2025-10-14 Vertex Pharmaceuticals Incorporated Carboxamides as modulators of sodium channels
WO2020176763A1 (en) 2019-02-27 2020-09-03 Vertex Pharmaceuticals Incorporated Dosage form comprising prodrug of na 1.8 sodium channel inhibitor
WO2020219867A1 (en) 2019-04-25 2020-10-29 Vertex Pharmaceuticals Incorporated Pyridone amide co-crystal compositions for the treatment of pain
CN110452183B (zh) * 2019-09-04 2023-03-14 中国科学院上海有机化学研究所 一种手性杂环化合物的制备方法
MX2022006865A (es) 2019-12-06 2022-07-11 Vertex Pharma Tetrahidrofuranos sustituidos como moduladores de canales de sodio.
WO2021130723A1 (en) * 2019-12-24 2021-07-01 Cadila Healthcare Limited Novel compounds suitable for the treatment of dyslipidemia
CN113278021B (zh) * 2021-05-29 2022-09-23 天津全和诚科技有限责任公司 1,7-二氮杂螺[3.5]壬烷-7-甲酸叔丁酯及其草酸盐的制备方法
BR112023025264A2 (pt) 2021-06-04 2024-02-20 Vertex Pharma Formas farmacêuticas sólidas e regimes posológicos compreendendo (2r,3s,4s,5r)-4-[[3- (3,4-difluoro-2-metóxi-fenil)-4,5-dimetil-5-(trifluorometil) tetra-hidrofuran-2-carbonil]amino ]piridina-2-carboxamida
US20240400544A1 (en) 2021-06-04 2024-12-05 Vertex Pharmaceuticals Incorporated N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamide analogs as modulators of sodium channels
JP2024520648A (ja) 2021-06-04 2024-05-24 バーテックス ファーマシューティカルズ インコーポレイテッド ナトリウムチャネルの調節因子としての置換テトラヒドロフラン-2-カルボキサミド
DK4347031T3 (da) 2021-06-04 2025-12-01 Vertex Pharma N-(hydroxyalkyl-(hetero)aryl)-tetrahydrofuran-carboxamider som modulatorer af natriumkanaler
WO2022256676A1 (en) 2021-06-04 2022-12-08 Vertex Pharmaceuticals Incorporated Substituted tetrahydrofuran analogs as modulators of sodium channels
WO2022256842A1 (en) 2021-06-04 2022-12-08 Vertex Pharmaceuticals Incorporated Hydroxy and (halo)alkoxy substituted tetrahydrofurans as modulators of sodium channels
KR20240102969A (ko) * 2021-10-13 2024-07-03 밴쿠아 바이오, 인크. 글루코세레브로시다제 활성의 소분자 조절제 및 이의 용도
EP4511117A1 (en) 2022-04-22 2025-02-26 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
JP2025513454A (ja) 2022-04-22 2025-04-24 バーテックス ファーマシューティカルズ インコーポレイテッド 疼痛の治療のためのヘテロアリール化合物
CA3256604A1 (en) 2022-04-22 2023-10-26 Vertex Pharmaceuticals Incorporated HETEROARYL COMPOUNDS FOR PAIN RELIEF
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CN120603815A (zh) 2022-12-06 2025-09-05 沃泰克斯药物股份有限公司 钠通道的取代四氢呋喃调节剂的合成方法
TW202535867A (zh) 2023-10-23 2025-09-16 美商維泰克斯製藥公司 用於治療疼痛之鈉通道調節劑及其固體形式的製備方法
WO2025090516A1 (en) 2023-10-23 2025-05-01 Vertex Pharmaceuticals Incorporated Methods of preparing compounds for treating pain and solid forms thereof
WO2025090480A1 (en) 2023-10-23 2025-05-01 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
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US20250186419A1 (en) 2023-12-07 2025-06-12 Vertex Pharmaceuticals Incorporated Dosing regimens for treating pain

Family Cites Families (65)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3939159A (en) 1974-05-29 1976-02-17 American Hoechst Corporation Spiro(pyrrolo (1,2-A)quinoxalines)
PT67194B (en) 1976-11-02 1979-03-23 Lilly Co Eli Process for preparing 4a-aryl-octahydro-1h-2-pyrindines
PL117572B1 (en) 1977-12-27 1981-08-31 Lilly Co Eli Process for preparing novel derivatives of trans-4a-phenyl-2,3,4,4a,5,6,7,7a-octahydro-1h-2-pyrindine3,4,4a,5,6,7,7a-oktagidro-1h-2-piridina
US4353901A (en) 1981-10-19 1982-10-12 Syntex (U.S.A.) Inc. 9-(1,4-Benzodioxan-2-ylalkyl and hydroxyalkyl)-1-oxa-4,9-diazaspiro[5.5]undecan-3-ones
GB8827479D0 (en) 1988-11-24 1988-12-29 Zambeletti Spa L Novel compounds
US5206240A (en) 1989-12-08 1993-04-27 Merck & Co., Inc. Nitrogen-containing spirocycles
IL96507A0 (en) 1989-12-08 1991-08-16 Merck & Co Inc Nitrogen-containing spirocycles and pharmaceutical compositions containing them
US5304121A (en) 1990-12-28 1994-04-19 Boston Scientific Corporation Drug delivery system making use of a hydrogel polymer coating
JPH04297458A (ja) 1991-03-27 1992-10-21 Toray Ind Inc イソキノリン誘導体およびその製造方法
GB9104656D0 (en) 1991-03-05 1991-04-17 Zambeletti Spa L Pharmaceuticals
US5886026A (en) 1993-07-19 1999-03-23 Angiotech Pharmaceuticals Inc. Anti-angiogenic compositions and methods of use
DE4341403A1 (de) 1993-12-04 1995-06-08 Basf Ag N-substituierte 3-Azabicycloalkan-Derivate, ihre Herstellung und Verwendung
US6017768A (en) 1994-05-06 2000-01-25 Pharmacopeia, Inc. Combinatorial dihydrobenzopyran library
AU691296B2 (en) 1994-05-06 1998-05-14 Pharmacopeia Drug Discovery, Inc. Combinatorial dihydrobenzopyran library
US6099562A (en) 1996-06-13 2000-08-08 Schneider (Usa) Inc. Drug coating with topcoat
IT1276462B1 (it) 1995-07-03 1997-10-31 Rotta Research Lab Diamidi aromatiche acide ad attivita' antigastrinica, procedimento per la loro preparazione e loro uso farmaceutico
DE69633245T2 (de) * 1995-09-29 2005-09-08 Eli Lilly And Co., Indianapolis Spiroverbindungen als Inhibitoren der Fibrinogen-abhängigen Blutplättchenaggregation
JP4297458B2 (ja) 1999-04-16 2009-07-15 クラリオン株式会社 ナビゲーションシステム及び方法並びにナビゲーション用ソフトウェアを記録した記録媒体
US20040266802A1 (en) 1999-06-07 2004-12-30 Alain Calvet Tricyclic analgesics
US20020151712A1 (en) 1999-09-14 2002-10-17 Nan-Horng Lin 3-pyrrolidinyloxy-3'-pyridyl ether compounds useful for controlling chemical synaptic transmission
AU2001289831A1 (en) 2000-09-06 2002-03-22 Bayer Aktiengesellschaft Medicaments against viral infections
US20040014744A1 (en) 2002-04-05 2004-01-22 Fortuna Haviv Substituted pyridines having antiangiogenic activity
JPWO2003095427A1 (ja) 2002-05-10 2005-09-15 大正製薬株式会社 スピロ環化合物
WO2003104240A1 (ja) 2002-06-11 2003-12-18 三共株式会社 環状チオエーテル類の製造法及びその合成中間体
AU2003274053A1 (en) * 2002-10-22 2004-05-13 Glaxo Group Limited Aryloxyalkylamine derivates as h3 receptor ligands
CA2503520A1 (en) 2002-10-24 2004-05-06 Sankyo Company Limited Process for producing optically active sulfoxide
BR0317230A (pt) 2002-12-13 2005-10-25 Smithkline Beecham Corp Composto, composição, métodos de antagonizar uma atividade do receptor de quimiocina ccr-5, e de tratar uma infecção viral em um paciente, e, uso de um composto
CA2512886A1 (en) 2003-02-28 2004-09-10 Galderma Research & Development, S.N.C. Ligands that modulate lxr-type receptors
JPWO2004092179A1 (ja) 2003-04-14 2006-07-06 日本曹達株式会社 スピロ誘導体、製造法および抗酸化薬
FR2856685B1 (fr) 2003-06-25 2005-09-23 Merck Sante Sas Derives de thiazolylpiperidine, leurs procedes de preparation et les compositions pharmaceutiques qui les contiennent
CN101921279A (zh) 2003-10-01 2010-12-22 阿得罗公司 螺环杂环衍生物及其应用方法
EP1679069A4 (en) 2003-10-21 2009-05-13 Dainippon Sumitomo Pharma Co NEW PIPERIDINE DERIVATIVE
TWI350168B (en) 2004-05-07 2011-10-11 Incyte Corp Amido compounds and their use as pharmaceuticals
WO2005121090A1 (en) 2004-06-02 2005-12-22 Abbott Laboratories Substituted piperidines that have antiangiogenic activity
US7598261B2 (en) 2005-03-31 2009-10-06 Adolor Corporation Spirocyclic heterocyclic derivatives and methods of their use
US20090215742A1 (en) 2005-05-03 2009-08-27 Pfizer, Inc. Amide resorcinol compounds
WO2007050124A1 (en) 2005-05-19 2007-05-03 Xenon Pharmaceuticals Inc. Fused piperidine derivatives and their uses as therapeutic agents
US7935712B2 (en) 2005-07-19 2011-05-03 Merck Sharp & Dohme Corp. Spirochromanone derivatives as acetyl coenzyme A carboxylase (ACC) inhibitors
EP1931652A2 (en) 2005-09-21 2008-06-18 Incyte Corporation Amido compounds and their use as pharmaceuticals
ES2407115T3 (es) 2005-11-18 2013-06-11 Ono Pharmaceutical Co., Ltd. Compuesto que contiene un grupo básico y uso del mismo
AR057579A1 (es) 2005-11-23 2007-12-05 Merck & Co Inc Compuestos espirociclicos como inhibidores de histona de acetilasa (hdac)
US20080027072A1 (en) 2006-04-20 2008-01-31 Ampla Pharmaceuticals, Inc. Potentiation of MC4 receptor activity
US20090186901A1 (en) 2006-05-05 2009-07-23 Ulrich Reiser Chemical compounds
JP5257068B2 (ja) 2006-05-16 2013-08-07 小野薬品工業株式会社 保護されていてもよい酸性基を含有する化合物およびその用途
EP2023924B1 (en) 2006-05-18 2016-08-03 Merck Sharp & Dohme Corp. Aryl-fused spirocyclic compounds
US20090325992A1 (en) 2006-07-31 2009-12-31 Ono Pharmaceutical Co., Ltd. Compound having cyclic group bound thereto through spiro binding and use thereof
WO2008045564A2 (en) 2006-10-12 2008-04-17 Epix Delaware, Inc. Carboxamide compounds and their use as antagonists of the chemokine ccr2 receptor
AP2009004880A0 (en) 2006-11-29 2009-06-30 Pfizer Prod Inc Spiroketone acetyl-COA carboxylase inhibitors
PE20081559A1 (es) 2007-01-12 2008-11-20 Merck & Co Inc DERIVADOS DE ESPIROCROMANONA SUSTITUIDOS COMO INHIBIDORES DE ACETIL CoA CARBOXILASA
AU2008205642B2 (en) 2007-01-12 2013-06-06 Msd K.K. Spirochromanon derivatives
US20100113418A1 (en) 2007-02-20 2010-05-06 Takeda Pharmaceutical Company Limited Heterocyclic compound
EP2110377A1 (en) 2008-04-15 2009-10-21 DAC S.r.l. Spirocyclic derivatives as histone deacetylase inhibitors
US8318762B2 (en) 2008-05-28 2012-11-27 Pfizer Inc. Pyrazolospiroketone acetyl-CoA carboxylase inhibitors
US8524730B2 (en) 2008-07-04 2013-09-03 Msd K.K. Spirochromanone carboxylic acids
WO2010009195A1 (en) 2008-07-16 2010-01-21 Schering Corporation Bicyclic heterocycle derivatives and use thereof as gpr119 modulators
WO2010027567A2 (en) 2008-07-23 2010-03-11 Schering Corporation Tricyclic spirocycle derivatives and methods of use thereof
EP2488177B1 (en) 2008-10-31 2016-10-12 Pain Therapeutics, Inc. Filamin a binding anti-inflammatory and analgesic
AU2009308769B2 (en) 2008-10-31 2015-03-12 Pain Therapeutics, Inc. Filamin A-binding anti-inflammatory analgesic
US8580807B2 (en) 2009-04-03 2013-11-12 Merck Sharp & Dohme Corp. Bicyclic piperidine and piperazine derivatives as GPCR modulators for the treatment of obesity, diabetes and other metabolic disorders
WO2010151595A1 (en) * 2009-06-26 2010-12-29 Schering Corporation Pyrrolo-benzo-1,4-diazines useful as sodium channel blockers
EP2470021B1 (en) 2009-08-27 2014-10-22 Merck Sharp & Dohme Corp. Novel pyrrolidine derived beta 3 adrenergic receptor agonists
UY33199A (es) * 2010-01-26 2011-08-31 Boehringer Ingelheim Int 5-alquinil-pirimidinas.
WO2011140425A1 (en) 2010-05-06 2011-11-10 Vertex Pharmaceuticals Incorporated Heterocyclic chromene-spirocyclic piperidine amides as modulators of ion channels
RU2634900C2 (ru) 2011-02-02 2017-11-08 Вертекс Фармасьютикалз Инкорпорейтед Спироциклические пирролопиразин(пиперидин)амиды в качестве модуляторов ионных каналов
JP5940562B2 (ja) 2011-02-18 2016-06-29 バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated イオンチャネルのモジュレーターとしてのクロマン−スピロ環式ピペリジンアミド

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