JP2017525677A - 治療用化合物及びその使用方法 - Google Patents

治療用化合物及びその使用方法 Download PDF

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JP2017525677A
JP2017525677A JP2017501012A JP2017501012A JP2017525677A JP 2017525677 A JP2017525677 A JP 2017525677A JP 2017501012 A JP2017501012 A JP 2017501012A JP 2017501012 A JP2017501012 A JP 2017501012A JP 2017525677 A JP2017525677 A JP 2017525677A
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alkyl
group
haloalkyl
compound
pain
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JP2017525677A5 (enExample
Inventor
ジーン−クリストフ アンドレス，
ジーン−クリストフ アンドレス，
フィリップ バージェロン，
フィリップ バージェロン，
ポール ロバート ビッヒラー，
ポール ロバート ビッヒラー，
スルタン チョウドリー，
スルタン チョウドリー，
クリストフ マーティン デーンハルト，
クリストフ マーティン デーンハルト，
ティーロ フォッケン，
ティーロ フォッケン，
ウェイ ゴン，
ウェイ ゴン，
マイケル エドワード グリムウッド，
マイケル エドワード グリムウッド，
アビド ハサン，
アビド ハサン，
アイバン ウィリアム ヘメオン，
アイバン ウィリアム ヘメオン，
チー ジア，
チー ジア，
ブライアン サフィナ，
ブライアン サフィナ，
シャオイ サン，
シャオイ サン，
マイケル スコット ウィルソン，
マイケル スコット ウィルソン，
アラ ユレブナ ゼノバ，
アラ ユレブナ ゼノバ，
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Xenon Pharmaceuticals Inc
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Xenon Pharmaceuticals Inc
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Publication of JP2017525677A publication Critical patent/JP2017525677A/ja
Publication of JP2017525677A5 publication Critical patent/JP2017525677A5/ja
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Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017525677A (ja) 2014-07-07 2017-09-07 ジェネンテック， インコーポレイテッド 治療用化合物及びその使用方法
MA42118A (fr) * 2015-05-22 2018-03-28 Genentech Inc Benzamides substitués et leurs méthodes d'utilisation
RU2760373C2 (ru) 2015-09-18 2021-11-24 Какен Фармасьютикал Ко., Лтд. Биарильное производное и содержащее его лекарственное средство
WO2017091592A1 (en) 2015-11-25 2017-06-01 Genentech, Inc. Substituted benzamides useful as sodium channel blockers
JP6572392B2 (ja) 2015-12-18 2019-09-11 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． 電位作動型ナトリウムチャネルにおいて選択的活性を有する、ヒドロキシアルキルアミンおよびヒドロキシシクロアルキルアミンで置換されたジアミン−アリールスルホンアミド化合物
EP3436432B1 (en) 2016-03-30 2021-01-27 Genentech, Inc. Substituted benzamides and methods of use thereof
JP6938545B2 (ja) * 2016-05-20 2021-09-22 ゼノン・ファーマシューティカルズ・インコーポレイテッドＸｅｎｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃ． ベンゼンスルホンアミド化合物および治療剤としてのそれらの使用
EP3601273B1 (en) 2017-03-24 2021-12-01 Genentech, Inc. 4-piperidin-n-(pyrimidin-4-yl)chroman-7-sulfonamide derivatives as sodium channel inhibitors
BR112020003725A2 (pt) 2017-10-06 2020-11-03 Forma Therapeutics, Inc. inibição da peptidase 30 específica de ubiquitina
AR114263A1 (es) 2018-02-26 2020-08-12 Genentech Inc Compuestos terapéuticos y métodos para utilizarlos
JP2021519788A (ja) 2018-03-30 2021-08-12 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ ナトリウムチャネル阻害剤としての縮合環ヒドロピリド化合物
CN112513036B (zh) 2018-05-17 2024-05-24 福马治疗有限公司 用作泛素特异性肽酶30抑制剂的稠合双环化合物
TW202003490A (zh) 2018-05-22 2020-01-16 瑞士商赫孚孟拉羅股份公司 治療性化合物及其使用方法
AU2019301628C1 (en) 2018-07-09 2025-02-06 Lieber Institute, Inc. Pyridine carboxamide compounds for inhibiting NaV1.8
AU2019302534B2 (en) 2018-07-09 2024-10-03 Lieber Institute, Inc. Pyridazine compounds for inhibiting NaV1.8
CA3110113A1 (en) 2018-10-05 2020-04-09 Forma Therapeutics, Inc. Fused pyrrolines which act as ubiquitin-specific protease 30 (usp30) inhibitors
WO2020094539A1 (de) * 2018-11-05 2020-05-14 Merck Patent Gmbh In einer organischen elektronischen vorrichtung einsetzbare verbindungen
CN115215787A (zh) * 2021-04-19 2022-10-21 中国科学院上海药物研究所 生长抑素受体5拮抗剂及其用途

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012007836A1 (en) * 2010-07-16 2012-01-19 Purdue Pharma .Lp. Pyridine compounds as sodium channel blockers
WO2013092674A1 (en) * 2011-12-20 2013-06-27 Boehringer Ingelheim International Gmbh Heterocyclic compounds, medicaments containing said compounds, use thereof and processes for the preparation thereof
WO2013161308A1 (en) * 2012-04-25 2013-10-31 Raqualia Pharma Inc. Amide derivatives as ttx-s blockers

Family Cites Families (114)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3705185A (en) 1969-04-14 1972-12-05 Minnesota Mining & Mfg N-aroyl sulfonamides
US3773919A (en) 1969-10-23 1973-11-20 Du Pont Polylactide-drug mixtures
US4485045A (en) 1981-07-06 1984-11-27 Research Corporation Synthetic phosphatidyl cholines useful in forming liposomes
EP0102324A3 (de) 1982-07-29 1984-11-07 Ciba-Geigy Ag Lipide und Tenside in wässriger Phase
US4544545A (en) 1983-06-20 1985-10-01 Trustees University Of Massachusetts Liposomes containing modified cholesterol for organ targeting
HUT35524A (en) 1983-08-02 1985-07-29 Hoechst Ag Process for preparing pharmaceutical compositions containing regulatory /regulative/ peptides providing for the retarded release of the active substance
GB8524157D0 (en) 1984-10-19 1985-11-06 Ici America Inc Heterocyclic amides
US5004697A (en) 1987-08-17 1991-04-02 Univ. Of Ca Cationized antibodies for delivery through the blood-brain barrier
DK24089D0 (da) 1989-01-20 1989-01-20 Hans Bundgaard Novel prodrug derivatives of biologically active agents containing hydroxyl groups or nh-acidic groups
GB8911854D0 (en) 1989-05-23 1989-07-12 Ici Plc Heterocyclic compounds
US5268164A (en) 1990-04-23 1993-12-07 Alkermes, Inc. Increasing blood-brain barrier permeability with permeabilizer peptides
US5112596A (en) 1990-04-23 1992-05-12 Alkermes, Inc. Method for increasing blood-brain barrier permeability by administering a bradykinin agonist of blood-brain barrier permeability
IL101860A0 (en) 1991-05-31 1992-12-30 Ici Plc Heterocyclic derivatives
JPH07509250A (ja) 1992-07-27 1995-10-12 アメリカ合衆国 血液脳バリヤーへのリポソームの標的化
CA2149918A1 (en) 1992-11-23 1994-06-09 Mark G. Palermo Substituted 3-(aminoalkylamino)-1,2-benzisoxazoles and related compounds
US5573653A (en) 1994-07-11 1996-11-12 Sandoz Ltd. Electrochemical process for thiocyanating aminobenzene compounds
CN1098843C (zh) 1994-08-30 2003-01-15 三共株式会社 异噁唑衍生物
US5753653A (en) 1995-12-08 1998-05-19 Agouron Pharmaceuticals, Inc. Metalloproteinase inhibitors, pharmaceutical compositions containing them and their pharmaceutical uses
GB9828442D0 (en) 1998-12-24 1999-02-17 Karobio Ab Novel thyroid receptor ligands and method II
US6514221B2 (en) 2000-07-27 2003-02-04 Brigham And Women's Hospital, Inc. Blood-brain barrier opening
US20020065259A1 (en) 2000-08-30 2002-05-30 Schatzberg Alan F. Glucocorticoid blocking agents for increasing blood-brain barrier permeability
US7034036B2 (en) 2000-10-30 2006-04-25 Pain Therapeutics, Inc. Inhibitors of ABC drug transporters at the blood-brain barrier
DE10121982B4 (de) 2001-05-05 2008-01-24 Lts Lohmann Therapie-Systeme Ag Nanopartikel aus Protein mit gekoppeltem Apolipoprotein E zur Überwindung der Blut-Hirn-Schranke und Verfahren zu ihrer Herstellung
JP4202250B2 (ja) 2001-07-25 2008-12-24 バイオマリン ファーマシューティカル インコーポレイテッド 血液脳関門輸送を調節するための組成物および方法
KR100789567B1 (ko) 2001-11-06 2007-12-28 동화약품공업주식회사 3-아미도-1,2-벤조이소옥사졸 유도체, 그 염, 제조방법 및 용도
DE10201550A1 (de) 2002-01-17 2003-07-31 Merck Patent Gmbh Phenoxy-Piperidine
US20030162695A1 (en) 2002-02-27 2003-08-28 Schatzberg Alan F. Glucocorticoid blocking agents for increasing blood-brain barrier permeability
CA2494028A1 (en) 2002-08-08 2004-02-19 Memory Pharmaceuticals Corporation Derivatives of 2-trifluormethyl-6-aminopurine as phosphodiesterase 4 inhibitors
CA2791165C (en) 2002-12-03 2015-02-24 Blanchette Rockefeller Neurosciences Institute A conjugate comprising cholesterol linked to tetracycline
US7132425B2 (en) 2002-12-12 2006-11-07 Hoffmann-La Roche Inc. 5-substituted-six-membered heteroaromatic glucokinase activators
EA200501462A1 (ru) 2003-04-15 2006-04-28 Пфайзер Инк. Альфа-замещенные карбоновые кислоты в качестве модуляторов ppar
KR20060073930A (ko) 2003-08-08 2006-06-29 버텍스 파마슈티칼스 인코포레이티드 통증 치료시 나트륨 또는 칼슘 채널 차단제로서 유용한헤테로아릴아미노설포닐페닐 유도체
ZA200601942B (en) 2003-08-08 2007-05-30 Vertex Pharma Heteroarylaminosulfonylphenyl derivatives for use as sodium or calcium channel blockers in the treatment of pain
US20050089473A1 (en) 2003-09-10 2005-04-28 Cedars-Sinai Medical Center Potassium channel mediated delivery of agents through the blood-brain barrier
CA2540214A1 (en) 2003-10-03 2005-04-14 Portola Pharmaceuticals, Inc. 2,4-dioxo-3-quinazolinylaryl sulfonylureas
US7081539B2 (en) 2004-03-25 2006-07-25 Dainippon Sumitomo Pharma Co., Ltd. One-pot process for the preparation of 1,2-benzisoxazole-3-methanesulfonamide
EP1773792A1 (en) 2004-07-30 2007-04-18 Merck & Co., Inc. Indanone potentiators of metabotropic glutamate receptors
WO2006020830A2 (en) 2004-08-12 2006-02-23 Amgen Inc. Bisaryl-sulfonamides
EP1812429A4 (en) 2004-09-29 2010-07-21 Portola Pharm Inc SUBSTITUTED 2H-1,3-BENZOXAZIN-4 (3H) -ONE
JP2008189549A (ja) 2005-05-12 2008-08-21 Astellas Pharma Inc カルボン酸誘導体またはその塩
DE102005038947A1 (de) 2005-05-18 2006-11-30 Grünenthal GmbH Substituierte Benzo[d]isoxazol-3-yl-amin-Verbindungen und deren Verwendung in Arzneimitteln
US7632837B2 (en) 2005-06-17 2009-12-15 Bristol-Myers Squibb Company Bicyclic heterocycles as cannabinoid-1 receptor modulators
WO2007030582A2 (en) 2005-09-09 2007-03-15 Bristol-Myers Squibb Company Acyclic ikur inhibitors
RU2008119412A (ru) 2005-10-19 2009-11-27 Ф.Хоффманн-Ля Рош Аг (Ch) N-фенил-фенилацетамидные ненуклеозидные ингибиторы обратной транскриптазы
CA2630234A1 (en) 2005-11-23 2007-05-31 Ligand Pharmaceuticals Inc. Thrombopoietin activity modulating compounds and methods
AR058296A1 (es) 2005-12-09 2008-01-30 Kalypsys Inc Inhibidores de histona desacetilasa y composicion farmaceutica
WO2007120647A2 (en) 2006-04-11 2007-10-25 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of voltage-gated sodium channels
WO2008045393A2 (en) 2006-10-11 2008-04-17 Amgen Inc. Imidazo- and triazolo-pyridine compounds and methods of use therof
US20110281821A9 (en) 2007-01-30 2011-11-17 Biogen Idec Ma Inc. Modulators of Mitotic Kinases
AU2008213836A1 (en) 2007-02-05 2008-08-14 Xenon Pharmaceuticals Inc. Pyridopyrimidinone compounds useful in treating sodium channel-mediated diseases or conditions
WO2008118758A1 (en) 2007-03-23 2008-10-02 Icagen, Inc. Inhibitors of ion channels
AU2008256937A1 (en) 2007-05-25 2008-12-04 Vertex Pharmaceuticals Incorporated Ion channel modulators and methods of use
KR20100031725A (ko) 2007-06-07 2010-03-24 아스텔라스세이야쿠 가부시키가이샤 피리돈 화합물
US20090012103A1 (en) 2007-07-05 2009-01-08 Matthew Abelman Substituted heterocyclic compounds
WO2009010784A1 (en) 2007-07-13 2009-01-22 Astrazeneca Ab New compounds 955
JP5460589B2 (ja) 2007-07-13 2014-04-02 アイカジェン， インコーポレイテッド ナトリウムチャネル阻害物質
US20110092703A1 (en) 2007-08-10 2011-04-21 Nippon Chemiphar Co., Ltd. P2x4 receptor antagonist
GB0720390D0 (en) 2007-10-18 2007-11-28 Prosidion Ltd G-Protein coupled receptor agonists
JP2011507910A (ja) 2007-12-21 2011-03-10 ユニバーシティー オブ ロチェスター 真核生物の寿命を変更するための方法
RU2481329C2 (ru) 2008-06-23 2013-05-10 Астеллас Фарма Инк. Сульфонамидные соединения или их соли
WO2010022055A2 (en) 2008-08-20 2010-02-25 Amgen Inc. Inhibitors of voltage-gated sodium channels
CA2747419C (en) 2009-01-12 2014-07-08 Icagen, Inc. Sulfonamide derivatives
HRP20171454T8 (hr) 2009-07-27 2018-01-12 Gilead Sciences, Inc. Fuzionirani heterociklični spojevi kao modulatori ionskih kanala
US8809380B2 (en) 2009-08-04 2014-08-19 Raqualia Pharma Inc. Picolinamide derivatives as TTX-S blockers
BR112012006686B8 (pt) 2009-09-25 2021-05-25 Astellas Pharma Inc compostos de amida substituída, composições farmacêuticas contendo os ditos compostos, e uso dos mesmos para prevenir e/ou tratar doenças causadas pelo lpa
WO2011059042A1 (ja) 2009-11-12 2011-05-19 武田薬品工業株式会社 芳香環化合物
US8471034B2 (en) 2009-11-18 2013-06-25 Concert Pharmaceuticals, Inc. Niacin prodrugs and deuterated versions thereof
TW201139406A (en) 2010-01-14 2011-11-16 Glaxo Group Ltd Voltage-gated sodium channel blockers
SI2533638T1 (sl) 2010-02-12 2016-05-31 Nivalis Therapeutics, Inc. Novi inhibitorji S-nitrozoglutation reduktaze
WO2011153588A1 (en) 2010-06-10 2011-12-15 Biota Scientific Management Pty Ltd Viral polymerase inhibitors
EP2588186A1 (en) 2010-06-30 2013-05-08 Cardiac Pacemakers, Inc. Lead having coil electrode with preferential bending region
US9279003B2 (en) 2010-07-07 2016-03-08 Purdue Pharma L.P. Analogs of sodium channel peptide toxin
ES2532356T3 (es) * 2010-07-09 2015-03-26 Pfizer Limited N-sulfonilbenzamidas como inhibidores de los canales de sodio dependientes de voltaje
ES2533065T3 (es) 2010-07-09 2015-04-07 Pfizer Limited Bencenosulfonamidas útiles como inhibidores de los canales de sodio
JP5860045B2 (ja) 2010-07-09 2016-02-16 ファイザー・リミテッドＰｆｉｚｅｒ Ｌｉｍｉｔｅｄ 化合物
CA2804351A1 (en) 2010-07-12 2012-01-19 Pfizer Limited Chemical compounds
CA2804877A1 (en) 2010-07-12 2012-01-19 Pfizer Limited Sulfonamide derivatives as nav1.7 inhibitors for the treatment of pain
JP2013532184A (ja) 2010-07-12 2013-08-15 ファイザー・リミテッド 電位開口型ナトリウムチャネル阻害剤として有用なｎ−スルホニルベンズアミド誘導体
ES2526981T3 (es) 2010-07-12 2015-01-19 Pfizer Limited N-sulfonilbenzamidas como inhibidores de canales de sodio dependientes de voltaje
US9096500B2 (en) 2010-07-12 2015-08-04 Pfizer Limited Acyl sulfonamide compounds
HRP20160094T1 (hr) 2010-09-13 2016-02-26 Novartis Ag Triazin-oksadiazoli
WO2012039657A1 (en) 2010-09-22 2012-03-29 Astrazeneca Ab Novel chromane compound for the treatment of pain disorders
JP2014500303A (ja) 2010-12-22 2014-01-09 パーデュー、ファーマ、リミテッド、パートナーシップ ナトリウムチャネル遮断剤としての置換ピリジン
WO2012095781A1 (en) 2011-01-13 2012-07-19 Pfizer Limited Indazole derivatives as sodium channel inhibitors
ES2573497T3 (es) 2011-02-02 2016-06-08 Vertex Pharmaceuticals Incorporated Pirrolopirazin-amidas de piperidina espirocíclicas como moduladores de canales iónicos
US9079902B2 (en) 2011-08-17 2015-07-14 Amgen Inc. Heteroaryl sodium channel inhibitors
US20140235676A1 (en) 2011-10-13 2014-08-21 Case Western Reserve University Rxr agonist compounds and methods
JP2014532660A (ja) 2011-10-28 2014-12-08 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． 電位作動型ナトリウムチャネルにおける選択活性を有するベンゾオキサゾリノン化合物
ES2586213T3 (es) 2011-10-31 2016-10-13 Xenon Pharmaceuticals Inc. Compuestos de bencenosulfonamida y su uso como agentes terapéuticos
EP2773641B1 (en) 2011-10-31 2017-09-27 Xenon Pharmaceuticals Inc. Biaryl ether sulfonamides and their use as therapeutic agents
US9133131B2 (en) 2011-11-15 2015-09-15 Purdue Pharma L.P. Pyrimidine diol amides as sodium channel blockers
EP2788332A1 (en) 2011-12-07 2014-10-15 Amgen, Inc. Bicyclic aryl and heteroaryl sodium channel inhibitors
US9085517B2 (en) 2011-12-15 2015-07-21 Pfizer Limited Sulfonamide derivatives
EP2800740A1 (en) 2012-01-04 2014-11-12 Pfizer Limited N-aminosulfonyl benzamides
JP2015083542A (ja) 2012-02-08 2015-04-30 大日本住友製薬株式会社 ３位置換プロリン誘導体
US8889741B2 (en) 2012-02-09 2014-11-18 Daiichi Sankyo Company, Limited Cycloalkane derivatives
WO2013122897A1 (en) 2012-02-13 2013-08-22 Amgen Inc. Dihydrobenzoxazine and tetrahydroquinoxaline sodium channel inhibitors
WO2013134518A1 (en) 2012-03-09 2013-09-12 Amgen Inc. Sulfamide sodium channel inhibitors
WO2013146969A1 (ja) 2012-03-29 2013-10-03 第一三共株式会社 新規二置換シクロヘキサン誘導体
PE20150400A1 (es) 2012-05-22 2015-03-27 Genentech Inc Benzamidas n-sustituidas y su uso en el tratamiento del dolor
US10071957B2 (en) 2012-07-06 2018-09-11 Genentech, Inc. N-substituted benzamides and methods of use thereof
JP6220786B2 (ja) 2012-07-19 2017-10-25 大日本住友製薬株式会社 １−（シクロアルキルカルボニル）プロリン誘導体
KR20150074122A (ko) 2012-10-26 2015-07-01 머크 샤프 앤드 돔 코포레이션 전압-게이팅 나트륨 채널에서 선택적 활성을 갖는 벤족사졸리논 화합물
CN104869992A (zh) 2012-10-26 2015-08-26 默沙东公司 具有电压门控性钠通道选择性活性的n-取代的吲唑磺酰胺化合物
JP2014118368A (ja) * 2012-12-14 2014-06-30 Taisho Pharmaceutical Co Ltd アザスピロアルカン化合物を有効成分として含有する血糖低下作用薬
EP2935257B1 (en) 2012-12-20 2018-02-07 Purdue Pharma LP Cyclic sulfonamides as sodium channel blockers
EP3239134B1 (en) 2013-01-31 2020-12-23 Vertex Pharmaceuticals Incorporated Pyridone amides as modulators of sodium channels
US20140296266A1 (en) 2013-03-01 2014-10-02 Gilead Sciences, Inc. Therapeutic compounds
RU2015143906A (ru) 2013-03-14 2017-04-18 Дженентек, Инк. Замещенные триазолопиридины и способы их применения
WO2014144545A2 (en) 2013-03-15 2014-09-18 Genentech, Inc. Substituted benzoxazoles and methods of use thereof
JP6449845B2 (ja) 2013-03-15 2019-01-09 クロモセル コーポレイション 疼痛の処置のためのナトリウムチャネルモジュレーター
WO2015051043A1 (en) 2013-10-01 2015-04-09 Amgen Inc. Biaryl acyl-sulfonamide compounds as sodium channel inhibitors
CA2931732A1 (en) 2013-11-27 2015-06-04 Genentech, Inc. Substituted benzamides and methods of use thereof
JP2017525677A (ja) 2014-07-07 2017-09-07 ジェネンテック， インコーポレイテッド 治療用化合物及びその使用方法

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012007836A1 (en) * 2010-07-16 2012-01-19 Purdue Pharma .Lp. Pyridine compounds as sodium channel blockers
WO2013092674A1 (en) * 2011-12-20 2013-06-27 Boehringer Ingelheim International Gmbh Heterocyclic compounds, medicaments containing said compounds, use thereof and processes for the preparation thereof
WO2013161308A1 (en) * 2012-04-25 2013-10-31 Raqualia Pharma Inc. Amide derivatives as ttx-s blockers

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