JP2020506899A - Magl阻害薬としての1,1,1−トリフルオロ−3−ヒドロキシプロパン−2−イルカルバマート誘導体 - Google Patents

Magl阻害薬としての1,1,1−トリフルオロ−3−ヒドロキシプロパン−2−イルカルバマート誘導体 Download PDF

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JP2020506899A
JP2020506899A JP2019538407A JP2019538407A JP2020506899A JP 2020506899 A JP2020506899 A JP 2020506899A JP 2019538407 A JP2019538407 A JP 2019538407A JP 2019538407 A JP2019538407 A JP 2019538407A JP 2020506899 A JP2020506899 A JP 2020506899A
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compound
formula
pharmaceutically acceptable
acceptable salt
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アーロン ブロドニー マイケル
アーロン ブロドニー マイケル
ライアン バトラー クリストファー
ライアン バトラー クリストファー
アン マカリスター ローラ
アン マカリスター ローラ
ジョン ヘラール クリストファー
ジョン ヘラール クリストファー
ヴィクター オニール スティーブン
ヴィクター オニール スティーブン
ロバート ヴァーホスト パトリック
ロバート ヴァーホスト パトリック
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ファイザー・インク
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JP2019538407A 2017-01-20 2018-01-08 Magl阻害薬としての1,1,1−トリフルオロ−3−ヒドロキシプロパン−2−イルカルバマート誘導体 Withdrawn JP2020506899A (ja)

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2023519367A (ja) * 2020-03-26 2023-05-10 ヤンセン ファーマシューティカ エヌ.ベー. モノアシルグリセロールリパーゼ調節因子としてのアザスピロ環化合物
JP2023542512A (ja) * 2020-09-22 2023-10-10 ヤンセン ファーマシューティカ エヌ.ベー. シクロブチルアミドモノアシルグリセロールリパーゼ調節因子

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TN2017000544A1 (en) 2015-07-31 2019-04-12 Pfizer 1,1,1-trifluoro-3-hydroxypropan-2-yl carbamate derivatives and 1,1,1-trifluoro-4-hydroxybutan-2-yl carbamate derivatives as magl inhibitors
RU2720203C1 (ru) 2017-01-20 2020-04-27 Пфайзер Инк. 1,1,1-трифтор-3-гидроксипропан-2-илкарбаматные производные как ингибиторы magl
US10662159B2 (en) * 2017-11-22 2020-05-26 Makscientific, Llc ABHD6 and dual ABHD6/MGL inhibitors and their uses
BR112021014389A2 (pt) * 2019-01-25 2021-09-28 NodThera Limited Derivados de carbamato e usos dos mesmos
MX2022015706A (es) * 2020-06-09 2023-01-24 Pfizer Antagonistas del receptor de melanocortina 4 y usos de estos.
JP2023541601A (ja) 2020-09-10 2023-10-03 プレシリックス・ナームローゼ・ベンノートシヤープ Fapに対する抗体フラグメント
WO2022135462A1 (zh) * 2020-12-22 2022-06-30 鲁南制药集团股份有限公司 Magl抑制剂的医药用途
CA3242372A1 (en) 2021-12-29 2023-07-06 Psy Therapeutics, Inc. Inhibiting monoacylglycerol lipase (magl)
WO2023203135A1 (en) 2022-04-22 2023-10-26 Precirix N.V. Improved radiolabelled antibody
CA3251753A1 (en) 2022-05-02 2023-11-09 Precirix N.V. PRE-TARGETTING
EP4665718A1 (en) 2023-02-13 2025-12-24 Apogee Pharmaceuticals, Inc. Small molecules as monoacylglycerol lipase (magl) inhibitors, compositions and use thereof
CN116621792B (zh) * 2023-05-16 2025-02-25 常州大学 一种制备n-正丁基-1,2-苯并异噻唑啉-3-酮-1-氧化物的方法
CN118191332B (zh) * 2024-03-19 2024-10-29 暨南大学 一种用于诊断术后认知功能障碍的血浆生物标志物及其应用

Family Cites Families (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0273659A1 (en) 1986-12-27 1988-07-06 Takeda Chemical Industries, Ltd. Azaspiro compounds, their production and use
KR0166088B1 (ko) 1990-01-23 1999-01-15 . 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도
US5376645A (en) 1990-01-23 1994-12-27 University Of Kansas Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof
JPH10503768A (ja) 1994-08-02 1998-04-07 メルク シヤープ エンド ドーム リミテツド アゼチジン、ピロリジンおよびピペリジン誘導体
GB9518953D0 (en) 1995-09-15 1995-11-15 Pfizer Ltd Pharmaceutical formulations
WO2000035298A1 (en) 1996-11-27 2000-06-22 Wm. Wrigley Jr. Company Chewing gum containing medicament active agents
GB9711643D0 (en) 1997-06-05 1997-07-30 Janssen Pharmaceutica Nv Glass thermoplastic systems
EP1182193A4 (en) 1999-04-09 2002-09-11 Mochida Pharm Co Ltd REMEDIES FOR NEUROGENIC PAIN
JP2003506468A (ja) 1999-08-13 2003-02-18 アベンティス・クロップサイエンス・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング 農薬としての複素環式スピロ化合物
US20020151712A1 (en) 1999-09-14 2002-10-17 Nan-Horng Lin 3-pyrrolidinyloxy-3'-pyridyl ether compounds useful for controlling chemical synaptic transmission
DE60125980T2 (de) 2000-11-20 2007-10-25 Scios Inc., Sunnyvale P38kinase-inhibitoren vom piperidin/piperazin-typ
CN1264847C (zh) 2001-05-14 2006-07-19 弗·哈夫曼-拉罗切有限公司 1-氧杂-3,9-二氮杂-螺[5.5]十一-2-酮衍生物及其作为神经激肽受体拮抗剂的用途
JP2007504123A (ja) 2003-08-29 2007-03-01 ランバクシー ラボラトリーズ リミテッド Iv型ホスホジエステラーゼの阻害剤
SE0302811D0 (sv) 2003-10-23 2003-10-23 Astrazeneca Ab Novel compounds
AR046756A1 (es) 2003-12-12 2005-12-21 Solvay Pharm Gmbh Derivados de hidronopol como agonistas de receptores orl-1 humanos.
JP3912400B2 (ja) 2004-03-30 2007-05-09 株式会社デンソー 圧力センサ
ES2370788T3 (es) 2005-02-07 2011-12-22 Aerocrine Ab Controlar flujo de aliento exhalado durante análisis.
UA90720C2 (en) 2005-05-25 2010-05-25 Басф Акциенгезелльшафт Heteroaroyl-substituted serine amides
CN101228116A (zh) 2005-05-25 2008-07-23 巴斯福股份公司 苯甲酰基取代的丝氨酸酰胺
EP1910290A2 (en) 2005-06-30 2008-04-16 Prosidion Limited Gpcr agonists
AR055395A1 (es) 2005-08-26 2007-08-22 Vertex Pharma Compuestos inhibidores de la actividad de la serina proteasa ns3-ns4a del virus de la hepatitis c
EP2102208B1 (en) 2006-12-05 2014-04-23 Janssen Pharmaceutica NV Novel substituted diaza spiro pyridinone derivatives for use in mch-1 mediated diseases
FR2915198B1 (fr) 2007-04-18 2009-12-18 Sanofi Aventis Derives de triazolopyridine-carboxamides et triazolopyridine -carboxamides, leur preparation et leur application en therapeutique.
JP2010524940A (ja) 2007-04-20 2010-07-22 シェーリング コーポレイション ピリミジノン誘導体およびそれらの使用方法
EP2058306A1 (en) 2007-11-08 2009-05-13 Schwarz Pharma Ag Heteroaryl-substituted 2-pyridinyl-methylamine derivatives
US8822480B2 (en) 2008-07-16 2014-09-02 Merck Sharp & Dohme Corp. Bicyclic heterocycle derivatives and use thereof as GPR119 modulators
JP2012506883A (ja) 2008-10-29 2012-03-22 グリュネンタール・ゲゼルシャフト・ミト・ベシュレンクテル・ハフツング 置換されたスピロアミン
WO2010056309A2 (en) 2008-11-14 2010-05-20 The Scripps Research Institute Methods and compositions related to targeting monoacylglycerol lipase
JP5657566B2 (ja) * 2008-12-24 2015-01-21 バイアル ポルテラ アンド シーエイ エス エイBIAL−Portela & Ca, S.A. 医薬品
US8435977B2 (en) 2009-04-22 2013-05-07 Janssen Pharmaceutica, Nv Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitors
US8455476B2 (en) 2009-04-22 2013-06-04 Janssen Pharmaceutica, Nv Azetidinyl diamides as monoacylglycerol lipase inhibitors
FR2945531A1 (fr) * 2009-05-12 2010-11-19 Sanofi Aventis Derives de 7-aza-spiro°3,5!nonane-7-carboxylates, leur preparation et leur application en therapeutique
WO2011142359A1 (ja) 2010-05-10 2011-11-17 日産化学工業株式会社 スピロ化合物及びアディポネクチン受容体活性化薬
FR2960875B1 (fr) 2010-06-04 2012-12-28 Sanofi Aventis Derives de carbamates d'hexafluoroisopropyle, leur preparation et leur application en therapeutique
JP2013537920A (ja) 2010-09-27 2013-10-07 ヤンセン ファーマシューティカ エヌ.ベー. モノアシルグリセロールリパーゼ阻害剤としてのオキソピペラジン−アゼチジンアミド及びオキソジアゼピン−アゼチジンアミド
JP2013540160A (ja) 2010-10-22 2013-10-31 ヤンセン ファーマシューティカ エヌ.ベー. モノアシルグリセロールリパーゼ阻害剤としてのアミノ−ピロリジン−アゼチジンジアミド
US8513423B2 (en) 2010-10-22 2013-08-20 Janssen Pharmaceutica, Nv Piperidin-4-yl-azetidine diamides as monoacylglycerol lipase inhibitors
MX347982B (es) 2011-03-14 2017-05-22 Vertex Pharma Morfolina-piperidina espirociclica-amidas como moduladores de canales ionicos.
JP2014159376A (ja) 2011-06-17 2014-09-04 Taisho Pharmaceutical Co Ltd アザスピロアルカン化合物
PE20141702A1 (es) 2012-01-06 2014-11-19 Abide Therapeutics Inc Compuestos de carbamato y preparacion y uso de los mismos
WO2013131010A2 (en) 2012-03-02 2013-09-06 Icahn School Of Medicine At Mount Sinai Function of chemokine receptor ccr8 in melanoma metastasis
JP6566867B2 (ja) 2012-07-13 2019-08-28 ペイン セラピューティクス インコーポレイテッド 生きている患者でのアルツハイマー病アッセイ
WO2014074715A1 (en) * 2012-11-07 2014-05-15 Genentech, Inc. Cyclopropyl amide derivatives
JP6647592B2 (ja) * 2013-07-03 2020-02-14 ルンドベック ラ ホーヤ リサーチ センター,インク. ピロロピロールカルバメート、および関連する有機化合物、医薬組成物、ならびにその医学的使用
JP2018513119A (ja) * 2015-03-18 2018-05-24 アビデ セラピューティクス,インク. ピペラジンカルバメート、およびピペラジンカルバメートを製造ならびに使用する方法
TN2017000544A1 (en) * 2015-07-31 2019-04-12 Pfizer 1,1,1-trifluoro-3-hydroxypropan-2-yl carbamate derivatives and 1,1,1-trifluoro-4-hydroxybutan-2-yl carbamate derivatives as magl inhibitors
RU2720203C1 (ru) 2017-01-20 2020-04-27 Пфайзер Инк. 1,1,1-трифтор-3-гидроксипропан-2-илкарбаматные производные как ингибиторы magl
CN110198944A (zh) * 2017-01-23 2019-09-03 辉瑞大药厂 作为单酰基甘油脂肪酶抑制剂的杂环螺环化合物

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2023519367A (ja) * 2020-03-26 2023-05-10 ヤンセン ファーマシューティカ エヌ.ベー. モノアシルグリセロールリパーゼ調節因子としてのアザスピロ環化合物
JP7777083B2 (ja) 2020-03-26 2025-11-27 ヤンセン ファーマシューティカ エヌ.ベー. モノアシルグリセロールリパーゼ調節因子としてのアザスピロ環化合物
JP2023542512A (ja) * 2020-09-22 2023-10-10 ヤンセン ファーマシューティカ エヌ.ベー. シクロブチルアミドモノアシルグリセロールリパーゼ調節因子

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