TW202115033A - 酵素抑制劑 - Google Patents

酵素抑制劑 Download PDF

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Publication number
TW202115033A
TW202115033A TW109104437A TW109104437A TW202115033A TW 202115033 A TW202115033 A TW 202115033A TW 109104437 A TW109104437 A TW 109104437A TW 109104437 A TW109104437 A TW 109104437A TW 202115033 A TW202115033 A TW 202115033A
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TW
Taiwan
Prior art keywords
pharmaceutically acceptable
compound
racemic
diastereomers
enantiomers
Prior art date
Application number
TW109104437A
Other languages
English (en)
Chinese (zh)
Inventor
漢娜 喬伊 愛德華茲
大衛 麥可 伊凡斯
亞歷山卓 馬札卡尼
艾莉西亞 史黛拉 歐巴拉
大衛 愛德華 克拉克
艾瑪努亞拉 甘西亞
瑞秋 皮塔威
約瑟夫 威廉 芮格史沃斯
Original Assignee
英商卡爾維斯塔製藥有限公司
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Publication date
Application filed by 英商卡爾維斯塔製藥有限公司 filed Critical 英商卡爾維斯塔製藥有限公司
Publication of TW202115033A publication Critical patent/TW202115033A/zh

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
TW109104437A 2019-08-21 2020-02-13 酵素抑制劑 TW202115033A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
PCT/GB2019/052359 WO2021032936A1 (en) 2019-08-21 2019-08-21 Enzyme inhibitors
WOPCT/GB2019/052359 2019-08-21

Publications (1)

Publication Number Publication Date
TW202115033A true TW202115033A (zh) 2021-04-16

Family

ID=67777359

Family Applications (1)

Application Number Title Priority Date Filing Date
TW109104437A TW202115033A (zh) 2019-08-21 2020-02-13 酵素抑制劑

Country Status (15)

Country Link
US (1) US20220363668A1 (https=)
EP (1) EP4017587A1 (https=)
JP (1) JP7566870B2 (https=)
KR (1) KR20220051207A (https=)
CN (1) CN114269430A (https=)
AR (1) AR118085A1 (https=)
AU (1) AU2020333222A1 (https=)
BR (1) BR112022000936A2 (https=)
CA (1) CA3147228A1 (https=)
CO (1) CO2022000266A2 (https=)
IL (1) IL289783A (https=)
MX (1) MX2022002069A (https=)
PH (1) PH12022550078A1 (https=)
TW (1) TW202115033A (https=)
WO (2) WO2021032936A1 (https=)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
GB201719881D0 (en) 2017-11-29 2018-01-10 Kalvista Pharmaceuticals Ltd Solid forms of plasma kallikrein inhibitor and salts thereof
WO2021028645A1 (en) 2019-08-09 2021-02-18 Kalvista Pharmaceuticals Limited Plasma kallikrein inhibitors
WO2021032935A1 (en) * 2019-08-21 2021-02-25 Kalvista Pharmaceuticals Limited Enzyme inhibitors
WO2025153806A1 (en) * 2024-01-15 2025-07-24 Kalvista Pharmaceuticals Limited Methods for determining amidolytic activity

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ592039A (en) 2003-08-27 2013-03-28 Ophthotech Corp Combination therapy for the treatment of ocular neovascular disorders
CN103415301A (zh) * 2011-03-09 2013-11-27 德国杰特贝林生物制品有限公司 用于与包括与人造表面接触的医疗操作一起施用的fxii抑制剂
GB2517908A (en) * 2013-08-14 2015-03-11 Kalvista Pharmaceuticals Ltd Bicyclic inhibitors
WO2015171527A1 (en) * 2014-05-05 2015-11-12 Global Blood Therapeutics, Inc. Pyrazolopyridine pyrazolopyrimidine and related compounds
GB201421088D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd New enzyme inhibitors
WO2017123518A1 (en) 2016-01-11 2017-07-20 The Rockefeller University Aminotriazole immunomodulators for treating autoimmune diseases
AU2017269256B2 (en) 2016-05-23 2021-02-25 The Rockefeller University Aminoacylindazole immunomodulators for treatment of autoimmune diseases
WO2018093695A1 (en) 2016-11-18 2018-05-24 Merck Sharp & Dohme Corp. FACTOR XIIa INHIBITORS
EP3541381B1 (en) 2016-11-18 2022-12-28 Merck Sharp & Dohme LLC Inhibitors of factor xiia
JP2021504490A (ja) 2017-11-29 2021-02-15 ザ ロックフェラー ユニバーシティーThe Rockefeller University 自己免疫疾患治療用ピラノピラゾールおよびピラゾロピリジン免疫調節薬
WO2021032935A1 (en) * 2019-08-21 2021-02-25 Kalvista Pharmaceuticals Limited Enzyme inhibitors

Also Published As

Publication number Publication date
EP4017587A1 (en) 2022-06-29
AR118085A1 (es) 2021-09-15
MX2022002069A (es) 2022-03-17
IL289783A (en) 2022-03-01
PH12022550078A1 (en) 2022-11-21
CO2022000266A2 (es) 2022-01-28
CA3147228A1 (en) 2021-02-25
KR20220051207A (ko) 2022-04-26
US20220363668A1 (en) 2022-11-17
AU2020333222A1 (en) 2022-02-24
JP2022545158A (ja) 2022-10-26
WO2021032936A1 (en) 2021-02-25
CN114269430A (zh) 2022-04-01
WO2021032937A1 (en) 2021-02-25
JP7566870B2 (ja) 2024-10-15
BR112022000936A2 (pt) 2022-03-08

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