JP6430398B2 - ベンジルアミン誘導体 - Google Patents

ベンジルアミン誘導体 Download PDF

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JP6430398B2
JP6430398B2 JP2015551223A JP2015551223A JP6430398B2 JP 6430398 B2 JP6430398 B2 JP 6430398B2 JP 2015551223 A JP2015551223 A JP 2015551223A JP 2015551223 A JP2015551223 A JP 2015551223A JP 6430398 B2 JP6430398 B2 JP 6430398B2
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ylmethyl
carboxylic acid
aryl
benzyl
aminomethyl
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JP2016504378A5 (enExample
JP2016504378A (ja
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アラン,クリスティン・エリザベス
バット,アンジェイ・ロマン
デイビー,レベッカ・ルイーズ
エドワーズ,ハンナ・ジョイ
エバンス,デイビッド・マイケル
ペテン,スティーブン・ジョン
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カルビスタ・ファーマシューティカルズ・リミテッド
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • A61K31/33—Heterocyclic compounds
    • 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
    • A61K31/4025—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 not condensed and containing further heterocyclic rings, e.g. cromakalim
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    • 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
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
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    • 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
    • A61K31/425—Thiazoles
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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
    • A61K31/4436—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
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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
    • 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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    • A61K31/47—Quinolines; Isoquinolines
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    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
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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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    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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  • Chemical & Material Sciences (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pulmonology (AREA)
  • Emergency Medicine (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Vascular Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyrrole Compounds (AREA)
JP2015551223A 2013-01-08 2014-01-08 ベンジルアミン誘導体 Expired - Fee Related JP6430398B2 (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201361750074P 2013-01-08 2013-01-08
GBGB1300304.1A GB201300304D0 (en) 2013-01-08 2013-01-08 Benzylamine derivatives
GB1300304.1 2013-01-08
US61/750,074 2013-01-08
US201361865732P 2013-08-14 2013-08-14
US61/865,732 2013-08-14
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Families Citing this family (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
LT2766346T (lt) 2011-10-14 2017-06-12 Bristol-Myers Squibb Company Pakeistieji tetrahidroizochinolino junginiai, kaip faktoriaus xia inhibitoriai
EP2906552B1 (en) 2012-10-12 2017-11-22 Bristol-Myers Squibb Company Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
HRP20180465T1 (hr) 2012-10-12 2018-05-04 Bristol-Myers Squibb Company Kristalni oblici inhibitora faktora xia
US9403774B2 (en) 2012-10-12 2016-08-02 Bristol-Myers Squibb Company Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
JP6479763B2 (ja) 2013-03-25 2019-03-06 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company 第xia因子阻害剤としての置換アゾール含有のテトラヒドロイソキノリン
GB2517908A (en) 2013-08-14 2015-03-11 Kalvista Pharmaceuticals Ltd Bicyclic inhibitors
HUE14755117T2 (hu) * 2013-08-14 2018-12-28 Kalvista Pharmaceuticals Ltd Plazma-kallikrein inhibitorok
TWI636047B (zh) 2013-08-14 2018-09-21 英商卡爾維斯塔製藥有限公司 雜環衍生物
NO2760821T3 (enExample) 2014-01-31 2018-03-10
JP6505727B2 (ja) 2014-01-31 2019-04-24 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company ヘテロ環式p2’基を有する第xia因子阻害剤としてのマクロ環
JP6526796B2 (ja) 2014-09-04 2019-06-05 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company Fxia阻害剤であるジアミドマクロ環
US9453018B2 (en) 2014-10-01 2016-09-27 Bristol-Myers Squibb Company Pyrimidinones as factor XIa inhibitors
GB201421085D0 (en) * 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd New enzyme inhibitors
GB201421088D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd New enzyme inhibitors
GB201421083D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd Enzyme inhibitors
FI4019022T3 (fi) 2015-10-01 2024-04-19 Biocryst Pharm Inc Ihmisen plasman kallikreiinin estäjiä
GB201609519D0 (en) * 2016-05-31 2016-07-13 Kalvista Pharmaceuticals Ltd Polymorphs of n-[(2,6-difluoro-3-methoxyphenyl)methyl]-3-(methoxymethyl)-1-({4-[(2-oxopyr idin-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide
ME03794B (me) * 2016-05-31 2021-04-20 Kalvista Pharmaceuticals Ltd Derivati pirazola kao inhibitori kalikreina plazme
GB201609603D0 (en) 2016-06-01 2016-07-13 Kalvista Pharmaceuticals Ltd Polymorphs of N-[(6-cyano-2-fluoro-3-methoxyphenyl)Methyl]-3-(methoxymethyl)-1-({4-[(2-ox opyridin-1-YL)Methyl]phenyl}methyl)pyrazole-4-carboxamide
GB201609607D0 (en) 2016-06-01 2016-07-13 Kalvista Pharmaceuticals Ltd Polymorphs of N-(3-Fluoro-4-methoxypyridin-2-yl)methyl)-3-(methoxymethyl)-1-({4-((2-oxopy ridin-1-yl)methyl)phenyl}methyl)pyrazole-4-carboxamide and salts
WO2018200674A1 (en) * 2017-04-26 2018-11-01 Mitobridge, Inc. Dynamin-1-like protein inhibitors
GB201719882D0 (en) * 2017-11-29 2018-01-10 Kalvista Pharmaceuticals Ltd Solid forms of a plasma kallikrein inhibitor and salts thereof
GB201719881D0 (en) 2017-11-29 2018-01-10 Kalvista Pharmaceuticals Ltd Solid forms of plasma kallikrein inhibitor and salts thereof
PL3716952T3 (pl) 2017-11-29 2022-05-02 Kalvista Pharmaceuticals Limited Postacie dawkowania zawierające inhibitor kalikreiny osoczowej
AU2019387370A1 (en) 2018-11-30 2021-06-10 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
GB201910125D0 (en) 2019-07-15 2019-08-28 Kalvista Pharmaceuticals Ltd Treatments of angioedema
GB201910116D0 (en) 2019-07-15 2019-08-28 Kalvista Pharmaceuticals Ltd Treatments of hereditary angioedema
WO2021028645A1 (en) 2019-08-09 2021-02-18 Kalvista Pharmaceuticals Limited Plasma kallikrein inhibitors
US20220298141A1 (en) 2019-08-21 2022-09-22 Kalvista Pharmaceuticals Limited Enzyme inhibitors
EP4017850A1 (en) 2019-08-21 2022-06-29 Kalvista Pharmaceuticals Limited Enzyme inhibitors
GB201918994D0 (en) 2019-12-20 2020-02-05 Kalvista Pharmaceuticals Ltd Treatments of diabetic macular edema and impaired visual acuity
GB2591730A (en) 2019-12-09 2021-08-11 Kalvista Pharmaceuticals Ltd New polymorphs
RU2734970C1 (ru) * 2019-12-10 2020-10-26 Общество С Ограниченной Ответственностью "Научно-Производственная Компания "Фармасофт" Система доставки 2-этил-6-метил-3-гидроксипиридина сукцината для перорального применения в форме гастроретентивной таблетки
WO2021138540A1 (en) 2020-01-03 2021-07-08 Berg Llc Polycyclic amides as ube2k modulators for treating cancer
TWI873290B (zh) 2020-02-13 2025-02-21 德商百靈佳殷格翰國際股份有限公司 作為血漿激肽釋放酶抑制劑之雜芳族甲醯胺衍生物
EP4178620B1 (en) 2020-07-10 2026-04-01 Merck Sharp & Dohme LLC Plasma kallikrein inhibitors
TW202228686A (zh) 2020-10-15 2022-08-01 英商卡爾維斯塔製藥有限公司 血管性水腫之治療
WO2022084693A1 (en) 2020-10-23 2022-04-28 Kalvista Pharmaceuticals Limited Treatments of angioedema
JP2024505596A (ja) 2021-02-09 2024-02-06 カルビスタ・ファーマシューティカルズ・リミテッド 遺伝性血管性浮腫の治療
CN115073429A (zh) * 2021-03-15 2022-09-20 昆药集团股份有限公司 一种1,2,4-三嗪-3,5-二酮类化合物的盐型、晶型及其制备方法
WO2023002219A1 (en) 2021-07-23 2023-01-26 Kalvista Pharmaceuticals Limited Treatments of hereditary angioedema
WO2023185634A1 (zh) * 2022-03-30 2023-10-05 南京明德新药研发有限公司 作为血浆激肽释放酶抑制剂的杂环类化合物
US20250281397A1 (en) 2022-04-27 2025-09-11 Kalvista Pharmaceuticals Limited Formulations of a plasma kallikrein inhibitor
EP4673437A1 (en) 2023-02-27 2026-01-07 Kalvista Pharmaceuticals Limited New solid form of a plasma kallikrein inhibitor
WO2025153806A1 (en) 2024-01-15 2025-07-24 Kalvista Pharmaceuticals Limited Methods for determining amidolytic activity
WO2025172692A1 (en) 2024-02-13 2025-08-21 Kalvista Pharmaceuticals Limited Oral sebetralstat for the treatment of an attack of hereditary angioedema
WO2025172693A1 (en) 2024-02-13 2025-08-21 Kalvista Pharmaceuticals Limited Oral sebetralstat for the treatment of an attack of hereditary angioedema

Family Cites Families (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5187157A (en) 1987-06-05 1993-02-16 Du Pont Merck Pharmaceutical Company Peptide boronic acid inhibitors of trypsin-like proteases
GB9019558D0 (en) 1990-09-07 1990-10-24 Szelke Michael Enzyme inhibitors
SE9301911D0 (sv) 1993-06-03 1993-06-03 Ab Astra New peptide derivatives
US5589467A (en) 1993-09-17 1996-12-31 Novo Nordisk A/S 2,5',N6-trisubstituted adenosine derivatives
AU759310B2 (en) * 1998-08-20 2003-04-10 Agouron Pharmaceuticals, Inc. Non-peptide GnRH agents, methods and intermediates for their preparation
US7101878B1 (en) * 1998-08-20 2006-09-05 Agouron Pharmaceuticals, Inc. Non-peptide GNRH agents, methods and intermediates for their preparation
GB0205527D0 (en) 2002-03-08 2002-04-24 Ferring Bv Inhibitors
DE10301300B4 (de) 2003-01-15 2009-07-16 Curacyte Chemistry Gmbh Verwendung von acylierten 4-Amidino- und 4-Guanidinobenzylaminen zur Inhibierung von Plasmakallikrein
US7247654B2 (en) * 2003-06-04 2007-07-24 Bristol-Myers Squibb Company 3,4-disubstituted benzamidines and benzylamines, and analogues thereof, useful as serine protease inhibitors
NZ592039A (en) 2003-08-27 2013-03-28 Ophthotech Corp Combination therapy for the treatment of ocular neovascular disorders
EP1568698A1 (en) 2004-02-27 2005-08-31 Aventis Pharma Deutschland GmbH Pyrrole-derivatives as factor Xa inhibitors
US7429604B2 (en) 2004-06-15 2008-09-30 Bristol Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
GB0508472D0 (en) 2005-04-26 2005-06-01 Glaxo Group Ltd Compounds
JP5225098B2 (ja) * 2005-12-14 2013-07-03 ブリストル−マイヤーズ スクイブ カンパニー 第XIa因子インヒビターとしてのアリールプロピオンアミド、アリールアクリルアミド、アリールプロピンアミド、またはアリールメチルウレアアナログ
AU2006325746A1 (en) * 2005-12-14 2007-06-21 Bristol-Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
EP2051707B1 (en) * 2006-07-31 2013-07-17 Activesite Pharmaceuticals, Inc. Inhibitors of plasma kallikrein
DE102006050672A1 (de) 2006-10-24 2008-04-30 Curacyte Discovery Gmbh Hemmstoffe des Plasmins und des Plasmakallikreins
US8658685B2 (en) 2008-01-31 2014-02-25 Activesite Pharmaceuticals, Inc. Methods for treatment of kallikrein-related disorders
WO2009106980A2 (en) 2008-02-29 2009-09-03 Pfizer Inc. Indazole derivatives
CN102026996B (zh) * 2008-03-13 2015-01-07 百时美施贵宝公司 作为凝血因子xia抑制剂的哒嗪衍生物
US8609866B2 (en) * 2009-12-18 2013-12-17 Activesite Pharmaceuticals, Inc. Prodrugs of inhibitors of plasma kallikrein
WO2011094496A2 (en) 2010-01-28 2011-08-04 The Medicines Company Trypsin-like serine protease inhibitors, and their preparation and use
JP2013121919A (ja) 2010-03-25 2013-06-20 Astellas Pharma Inc 血漿カリクレイン阻害剤
ES2483802T3 (es) 2010-07-07 2014-08-07 The Medicines Company (Leipzig) Gmbh Inhibidores de serina proteasa
US9290485B2 (en) * 2010-08-04 2016-03-22 Novartis Ag N-((6-amino-pyridin-3-yl)methyl)-heteroaryl-carboxamides
WO2012142080A1 (en) * 2011-04-12 2012-10-18 Bristol-Myers Squibb Company Thioamide, amidoxime and amidrazone derivatives as hiv attachment inhibitors
EP2697196A1 (en) * 2011-04-13 2014-02-19 Activesite Pharmaceuticals, Inc. Prodrugs of inhibitors of plasma kallikrein
US9133128B2 (en) 2011-06-17 2015-09-15 Research Triangle Institute Pyrazole derivatives as cannabinoid receptor 1 antagonists
US20140378474A1 (en) * 2012-01-27 2014-12-25 Novartis Ag 5-membered heteroarylcarboxamide derivatives as plasma kallikrein inhibitors
US20140350034A1 (en) 2012-01-27 2014-11-27 Novartis Ag Aminopyridine derivatives as plasma kallikrein inhibitors
EA201591291A1 (ru) 2013-01-08 2015-12-30 Савира Фармасьютикалз Гмбх Производные пиримидона и их применение в лечении, облегчении или профилактике вирусного заболевания

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