KR20220051207A - 효소 저해제 - Google Patents

효소 저해제 Download PDF

Info

Publication number
KR20220051207A
KR20220051207A KR1020227008821A KR20227008821A KR20220051207A KR 20220051207 A KR20220051207 A KR 20220051207A KR 1020227008821 A KR1020227008821 A KR 1020227008821A KR 20227008821 A KR20227008821 A KR 20227008821A KR 20220051207 A KR20220051207 A KR 20220051207A
Authority
KR
South Korea
Prior art keywords
pharmaceutically acceptable
solvates
racemic
diastereomers
compound
Prior art date
Legal status (The legal status 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 status listed.)
Withdrawn
Application number
KR1020227008821A
Other languages
English (en)
Korean (ko)
Inventor
한나 조이 에드워즈
데이비드 마이클 에반스
알레산드로 마자카니
알리샤 스텔라 오바라
데이비드 에드워드 클라크
엠마누엘라 간치아
레이첼 피타웨이
조셉 윌리엄 리글스워스
Original Assignee
칼비스타 파마슈티컬즈 리미티드
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.)
Filing date
Publication date
Application filed by 칼비스타 파마슈티컬즈 리미티드 filed Critical 칼비스타 파마슈티컬즈 리미티드
Publication of KR20220051207A publication Critical patent/KR20220051207A/ko
Withdrawn legal-status Critical Current

Links

Classifications

    • 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)
KR1020227008821A 2019-08-21 2020-02-13 효소 저해제 Withdrawn KR20220051207A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
PCT/GB2019/052359 WO2021032936A1 (en) 2019-08-21 2019-08-21 Enzyme inhibitors
GBPCT/GB2019/052359 2019-08-21
PCT/GB2020/050332 WO2021032937A1 (en) 2019-08-21 2020-02-13 Enzyme inhibitors

Publications (1)

Publication Number Publication Date
KR20220051207A true KR20220051207A (ko) 2022-04-26

Family

ID=67777359

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020227008821A Withdrawn KR20220051207A (ko) 2019-08-21 2020-02-13 효소 저해제

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
US20220363668A1 (en) 2022-11-17
TW202115033A (zh) 2021-04-16
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

Similar Documents

Publication Publication Date Title
JP7566870B2 (ja) 酵素阻害剤
US10336741B2 (en) Substituted pyrrolidines as factor XIa inhibitors for the treatment thromboembolic diseases
KR102424709B1 (ko) 혈장 칼리크레인 저해제로서 피라졸 유도체
KR20220050944A (ko) 효소 저해제
KR20220050942A (ko) 효소 저해제
KR20220050925A (ko) 효소 저해제
KR20230128413A (ko) 효소 저해제
CN116745278A (zh) 酶抑制剂
CN116829547A (zh) 因子XIIa抑制剂

Legal Events

Date Code Title Description
PA0105 International application

St.27 status event code: A-0-1-A10-A15-nap-PA0105

PG1501 Laying open of application

St.27 status event code: A-1-1-Q10-Q12-nap-PG1501

PC1203 Withdrawal of no request for examination

St.27 status event code: N-1-6-B10-B12-nap-PC1203