CN105683179B - 血浆激肽释放酶的抑制剂 - Google Patents

血浆激肽释放酶的抑制剂 Download PDF

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Publication number
CN105683179B
CN105683179B CN201480055925.4A CN201480055925A CN105683179B CN 105683179 B CN105683179 B CN 105683179B CN 201480055925 A CN201480055925 A CN 201480055925A CN 105683179 B CN105683179 B CN 105683179B
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methyl
pyridine
aminoisoquinolin
formula
alkyl
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CN105683179A (zh
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汉娜·乔伊·爱德华兹
戴维·米歇尔·埃万斯
普雷姆吉·梅根尼
安德鲁·理查德·诺瓦克
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Kalvista Pharmaceuticals Ltd
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    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • A—HUMAN NECESSITIES
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/455—Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
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    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
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    • C07D471/04—Ortho-condensed systems

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  • Veterinary Medicine (AREA)
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  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Immunology (AREA)
  • Rheumatology (AREA)
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  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Obesity (AREA)
  • Ophthalmology & Optometry (AREA)
  • Endocrinology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN201480055925.4A 2013-08-14 2014-08-14 血浆激肽释放酶的抑制剂 Expired - Fee Related CN105683179B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201361865732P 2013-08-14 2013-08-14
US201361865756P 2013-08-14 2013-08-14
US61/865,732 2013-08-14
US61/865,756 2013-08-14
PCT/GB2014/052510 WO2015022546A1 (en) 2013-08-14 2014-08-14 Inhibitors of plasma kallikrein

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CN105683179A CN105683179A (zh) 2016-06-15
CN105683179B true CN105683179B (zh) 2018-10-26

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US (1) US10221161B2 (enExample)
EP (1) EP3033336B1 (enExample)
JP (1) JP6527147B2 (enExample)
CN (1) CN105683179B (enExample)
CA (1) CA2920815C (enExample)
ES (1) ES2674088T3 (enExample)
HU (1) HUE14755117T2 (enExample)
MX (1) MX366498B (enExample)
PL (1) PL3033336T3 (enExample)
RU (1) RU2674028C2 (enExample)
WO (1) WO2015022546A1 (enExample)

Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO2015103317A1 (en) * 2013-12-30 2015-07-09 Lifesci Pharmaceuticals, Inc. Therapeutic inhibitory compounds
US9611252B2 (en) 2013-12-30 2017-04-04 Lifesci Pharmaceuticals, Inc. Therapeutic inhibitory compounds
MX381342B (es) * 2014-07-16 2025-03-12 Lifesci Pharmaceuticals Inc Compuestos terapeuticos inhibidores.
US9463201B2 (en) 2014-10-19 2016-10-11 M.G. Therapeutics Ltd Compositions and methods for the treatment of meibomian gland dysfunction
GB201421085D0 (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
WO2016201052A1 (en) 2015-06-12 2016-12-15 Global Blood Therapeutics, Inc. Bridged bicyclic kallikrein inhibitors
EP3317241A4 (en) * 2015-07-01 2019-01-23 Lifesci Pharmaceuticals, Inc. THERAPEUTIC INHIBITING COMPOUNDS
CA2991171A1 (en) 2015-07-01 2017-01-05 Lifesci Pharmaceuticals, Inc. Therapeutic inhibitory compounds
CN108472312A (zh) 2015-09-28 2018-08-31 阿祖拉眼科有限公司 用于增加睑板腺脂质分泌物的含硫醇及二硫化物的药剂
MA44676A (fr) 2016-04-14 2019-02-20 Azura Ophthalmics Ltd Compositions de disulfure de sélénium destinées à être utilisées dans le traitement du dysfonctionnement de la glande de meibomius
RS60600B1 (sr) 2016-05-31 2020-08-31 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
WO2018011628A1 (en) 2016-07-11 2018-01-18 Lifesci Pharmaceuticals, Inc. Therapeutic inhibitory compounds
GB201719881D0 (en) 2017-11-29 2018-01-10 Kalvista Pharmaceuticals Ltd Solid forms of plasma kallikrein inhibitor and salts thereof
GB201721515D0 (en) * 2017-12-21 2018-02-07 Kalvista Pharmaceuticals Ltd Dosage forms comprising a plasma kallikrein inhibtor
IL274557B2 (en) 2017-11-29 2024-09-01 Kalvista Pharmaceuticals Ltd Dosage forms comprising a plasma kallikrein inhibitor
JP2021515761A (ja) * 2018-02-28 2021-06-24 ライフサイ ファーマシューティカルズ，インク． 遺伝性血管浮腫の治療
KR20200143376A (ko) 2018-03-13 2020-12-23 샤이어 휴먼 지네틱 테라피즈 인크. 혈장 칼리크레인 억제제로서의 치환된 이미다조피리딘 및 이의 용도
CN113039181B (zh) * 2018-08-16 2024-08-13 勃林格殷格翰国际有限公司 作为血浆激肽释放酶抑制剂的杂芳族甲酰胺衍生物
CN114206852A (zh) 2019-08-09 2022-03-18 卡尔维斯塔制药有限公司 血浆激肽释放酶抑制剂
ES2987744T3 (es) 2019-09-18 2024-11-18 Takeda Pharmaceuticals Co Inhibidores de calicreína plasmática y usos de los mismos
WO2021055589A1 (en) 2019-09-18 2021-03-25 Shire Human Genetic Therapies, Inc. Heteroaryl plasma kallikrein inhibitors
CN113004286B (zh) * 2019-12-20 2022-08-12 成都康弘药业集团股份有限公司 作为血浆激肽释放酶抑制剂的三环类化合物及其用途
US11091447B2 (en) 2020-01-03 2021-08-17 Berg Llc UBE2K modulators and methods for their use
EP4087655A4 (en) 2020-01-10 2024-02-21 Azura Ophthalmics Ltd INSTRUCTIONS FOR COMPOSITION AND SENSITIVITY
CN120712252A (zh) * 2023-02-16 2025-09-26 治纳辅医药科技有限公司 包含sos1抑制剂和抗癌药物的用于治疗癌症的药物组合物
WO2025153806A1 (en) 2024-01-15 2025-07-24 Kalvista Pharmaceuticals Limited Methods for determining amidolytic activity

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003035076A1 (en) * 2001-10-26 2003-05-01 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa Dihydroxypyrimidine carboxamide inhibitors of hiv integrase
WO2004069792A2 (en) * 2003-02-03 2004-08-19 Janssen Pharmaceutica N.V. Quinoline-derived amide modulators of vanilloid vr1 receptor
WO2005079800A1 (en) * 2004-02-12 2005-09-01 Vernalis (R & D) Ltd. Pyrimidine compounds as purine receptor antagonist
WO2005123680A1 (en) * 2004-06-15 2005-12-29 Bristol-Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
WO2008121670A1 (en) * 2007-03-30 2008-10-09 Sanofi-Aventis Pyrimidine hydrazide compounds as pgds inhibitors
WO2009083553A1 (en) * 2007-12-31 2009-07-09 Rheoscience A/S Azine compounds as glucokinase activators
WO2013111108A1 (en) * 2012-01-27 2013-08-01 Novartis Ag 5-membered heteroarylcarboxamide derivatives as plasma kallikrein inhibitors

Family Cites Families (27)

* 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
GB0205527D0 (en) 2002-03-08 2002-04-24 Ferring Bv Inhibitors
AU2004268614C1 (en) 2003-08-27 2010-10-28 Ophthotech Corporation Combination therapy for the treatment of ocular neovascular disorders
US7417063B2 (en) * 2004-04-13 2008-08-26 Bristol-Myers Squibb Company Bicyclic heterocycles useful as serine protease inhibitors
US20070254894A1 (en) 2006-01-10 2007-11-01 Kane John L Jr Novel small molecules with selective cytotoxicity against human microvascular endothelial cell proliferation
AU2007281220B2 (en) * 2006-07-31 2013-08-15 Activesite Pharmaceuticals, Inc. Inhibitors of plasma kallikrein
DE102006050672A1 (de) 2006-10-24 2008-04-30 Curacyte Discovery Gmbh Hemmstoffe des Plasmins und des Plasmakallikreins
PT2439205E (pt) 2006-12-29 2015-07-16 Abbvie Deutschland Compostos de carboxamida e seus usos como inibidores de calpaína
CA2680173A1 (en) 2007-03-07 2008-09-12 Alantos Pharmaceuticals Holding, Inc. Metalloprotease inhibitors containing a heterocyclic moiety
US8324385B2 (en) 2008-10-30 2012-12-04 Madrigal Pharmaceuticals, Inc. Diacylglycerol acyltransferase inhibitors
GB0910003D0 (en) 2009-06-11 2009-07-22 Univ Leuven Kath Novel compounds for the treatment of neurodegenerative diseases
JP2013515000A (ja) 2009-12-18 2013-05-02 アクティベサイト ファーマシューティカルズ インコーポレイティッド 血漿カリクレインの阻害薬のプロドラッグ
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
EP2458315B1 (de) 2010-11-25 2017-01-04 Balcke-Dürr GmbH Regenerativer Wärmetauscher mit zwangsgeführter Rotordichtung
US8691861B2 (en) * 2011-04-13 2014-04-08 Activesite Pharmaceuticals, Inc. Prodrugs of inhibitors of plasma kallikrein
EP2807156A1 (en) 2012-01-27 2014-12-03 Novartis AG Aminopyridine derivatives as plasma kallikrein inhibitors
GB201300304D0 (en) * 2013-01-08 2013-02-20 Kalvista Pharmaceuticals Ltd Benzylamine derivatives
HUE034829T2 (en) * 2013-05-23 2018-03-28 Kalvista Pharmaceuticals Ltd Heterocyclic derivatives
WO2015103317A1 (en) 2013-12-30 2015-07-09 Lifesci Pharmaceuticals, Inc. Therapeutic inhibitory compounds
WO2015171526A2 (en) 2014-05-05 2015-11-12 Global Blood Therapeutics, Inc. Tricyclic pyrazolopyridine compounds
WO2015171527A1 (en) 2014-05-05 2015-11-12 Global Blood Therapeutics, Inc. Pyrazolopyridine pyrazolopyrimidine and related compounds
MX381342B (es) 2014-07-16 2025-03-12 Lifesci Pharmaceuticals Inc Compuestos terapeuticos inhibidores.

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003035076A1 (en) * 2001-10-26 2003-05-01 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa Dihydroxypyrimidine carboxamide inhibitors of hiv integrase
WO2004069792A2 (en) * 2003-02-03 2004-08-19 Janssen Pharmaceutica N.V. Quinoline-derived amide modulators of vanilloid vr1 receptor
WO2005079800A1 (en) * 2004-02-12 2005-09-01 Vernalis (R & D) Ltd. Pyrimidine compounds as purine receptor antagonist
WO2005123680A1 (en) * 2004-06-15 2005-12-29 Bristol-Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
WO2008121670A1 (en) * 2007-03-30 2008-10-09 Sanofi-Aventis Pyrimidine hydrazide compounds as pgds inhibitors
WO2009083553A1 (en) * 2007-12-31 2009-07-09 Rheoscience A/S Azine compounds as glucokinase activators
WO2013111108A1 (en) * 2012-01-27 2013-08-01 Novartis Ag 5-membered heteroarylcarboxamide derivatives as plasma kallikrein inhibitors

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CA2920815A1 (en) 2015-02-19
HUE14755117T2 (hu) 2018-12-28
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MX366498B (es) 2019-07-11
US10221161B2 (en) 2019-03-05
WO2015022546A1 (en) 2015-02-19
EP3033336B1 (en) 2018-05-30
RU2016108753A (ru) 2017-09-19
RU2674028C2 (ru) 2018-12-04
CA2920815C (en) 2021-09-21
CN105683179A (zh) 2016-06-15
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