KR102217524B1 - 이온 통로 억제 화합물, 제제 및 용도 - Google Patents

이온 통로 억제 화합물, 제제 및 용도 Download PDF

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KR102217524B1
KR102217524B1 KR1020187013376A KR20187013376A KR102217524B1 KR 102217524 B1 KR102217524 B1 KR 102217524B1 KR 1020187013376 A KR1020187013376 A KR 1020187013376A KR 20187013376 A KR20187013376 A KR 20187013376A KR 102217524 B1 KR102217524 B1 KR 102217524B1
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compound
substituted
unsubstituted
pharmaceutically acceptable
azaspiro
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KR20180074705A (ko
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신민 시에
프랭크 카이셔
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아파싸이, 인코포레이티드
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/26—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4453—Non condensed piperidines, e.g. piperocaine only substituted in position 1, e.g. propipocaine, diperodon
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4747—Quinolines; Isoquinolines spiro-condensed
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
    • C07D211/56—Nitrogen atoms
    • C07D211/58—Nitrogen atoms attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/20—Spiro-condensed ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/02—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 two hetero rings
    • C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
KR1020187013376A 2015-11-12 2016-11-14 이온 통로 억제 화합물, 제제 및 용도 Active KR102217524B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562254564P 2015-11-12 2015-11-12
US62/254,564 2015-11-12
PCT/US2016/061918 WO2017083867A1 (en) 2015-11-12 2016-11-14 Ion channel inhibitory compounds, pharmaceutical formulations and uses

Publications (2)

Publication Number Publication Date
KR20180074705A KR20180074705A (ko) 2018-07-03
KR102217524B1 true KR102217524B1 (ko) 2021-02-19

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KR1020187013376A Active KR102217524B1 (ko) 2015-11-12 2016-11-14 이온 통로 억제 화합물, 제제 및 용도

Country Status (16)

Country Link
US (1) US10562857B2 (enExample)
EP (1) EP3340988B1 (enExample)
JP (1) JP6790094B2 (enExample)
KR (1) KR102217524B1 (enExample)
CN (1) CN108289886B (enExample)
AU (1) AU2016353446B2 (enExample)
BR (1) BR112018009439B1 (enExample)
CA (1) CA3004448A1 (enExample)
IL (1) IL259199B (enExample)
MX (1) MX383833B (enExample)
NZ (1) NZ742033A (enExample)
PH (1) PH12018501000A1 (enExample)
RU (1) RU2746188C2 (enExample)
SG (1) SG11201803475YA (enExample)
WO (1) WO2017083867A1 (enExample)
ZA (1) ZA201803739B (enExample)

Families Citing this family (13)

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KR20200027992A (ko) * 2017-07-12 2020-03-13 반더빌트유니버시티 무스카린성 아세틸콜린 수용체 m4의 길항제
JP2020537667A (ja) 2017-10-17 2020-12-24 ヴァンダービルト ユニバーシティー ムスカリン性アセチルコリン受容体ｍ４のアンタゴニスト
WO2019126559A1 (en) 2017-12-20 2019-06-27 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor m4
CN110294717B (zh) * 2018-03-21 2021-01-19 湖南加法检测有限公司 农药全组分中2,2-二取代环丁酮杂质及其衍生物、制备方法与应用
CN108658933A (zh) * 2018-07-13 2018-10-16 南京大学 一种二芳基并噻吩型或二芳基硫醚型氘代烷基的制备方法
US11744825B2 (en) * 2018-08-28 2023-09-05 Afasci, Inc. Methods of treating hypersensitive cough or itching using ion channel inhibitory compounds
WO2020223136A1 (en) 2019-05-02 2020-11-05 Merck Sharp & Dohme Corp. Spiropiperidine allosteric modulators of nicotinic acetylcholine receptors
JP2022540253A (ja) * 2019-07-11 2022-09-14 プラクシス プレシジョン メディシンズ， インコーポレイテッド Ｔ型カルシウムチャネル調節因子の製剤およびその使用方法
BR112022021946A2 (pt) * 2020-04-29 2023-01-17 Praxis Prec Medicines Inc Métodos de uso de moduladores do canal de cálcio do tipo t
CN112574085A (zh) * 2020-12-18 2021-03-30 南通药明康德医药科技有限公司 一种5-氨基-2-氮杂螺[3.4]辛烷-2-羧酸叔丁酯的制备方法
JP2025505578A (ja) * 2022-02-03 2025-02-28 プラクシス プレシジョン メディシンズ， インコーポレイテッド Ｔ型カルシウムチャネル調節因子を使用した治療方法
AU2024230662A1 (en) * 2023-03-02 2025-09-11 Praxis Precision Medicines, Inc. High strength single unit dose formulations and methods of use thereof
AU2024229800A1 (en) * 2023-03-02 2025-09-11 Praxis Precision Medicines, Inc. Methods of treating essential tremor

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WO2012047703A2 (en) * 2010-10-04 2012-04-12 Schering Corporation Cyclopropyl-spiro-piperidines useful as sodium channel blockers

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WO2007002361A2 (en) * 2005-06-23 2007-01-04 Merck & Co., Inc. 3-fluoro-piperidine t-type calcium channel antagonists
CA2611639A1 (en) * 2005-06-29 2007-01-04 Merck & Co., Inc. 4-fluoro-piperidine t-type calcium channel antagonists
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CA2689561C (en) * 2007-06-15 2015-11-17 Newron Pharmaceuticals S.P.A. Substituted 2- [2- (phenyl) ethylamino] alkaneamide derivatives and their use as sodium and/or calcium channel modulators
US8377968B2 (en) * 2008-06-02 2013-02-19 Zalicus Pharmaceuticals, Ltd. N-piperidinyl acetamide derivatives as calcium channel blockers
EP2685824A4 (en) * 2011-03-17 2014-09-10 Merck Sharp & Dohme INDUSTRIAL DERIVATIVES USED AS CCR2 ANTAGONISTS
EP3292110B1 (en) * 2011-09-22 2019-08-21 Merck Sharp & Dohme B.V. N-piperidin-4-yl derivatives
US9822129B2 (en) * 2012-03-02 2017-11-21 Genentech, Inc. Amido spirocyclic amide and sulfonamide derivatives
KR101556318B1 (ko) * 2013-05-15 2015-10-01 한국과학기술연구원 칼슘이온 채널 조절제로서 유효한 6-피라졸일아미도-3-치환된 아자바이사이클로[3.1.0]헥산 유도체
CA2912359A1 (en) * 2013-07-03 2015-01-08 F. Hoffmann-La Roche Ag Heteroaryl pyridone and aza-pyridone amide compounds
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WO2012047703A2 (en) * 2010-10-04 2012-04-12 Schering Corporation Cyclopropyl-spiro-piperidines useful as sodium channel blockers

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Publication number Publication date
AU2016353446B2 (en) 2022-05-19
NZ742033A (en) 2022-11-25
CA3004448A1 (en) 2017-05-18
EP3340988A1 (en) 2018-07-04
PH12018501000A1 (en) 2019-01-28
IL259199A (en) 2018-07-31
MX383833B (es) 2025-03-14
BR112018009439B1 (pt) 2023-12-12
SG11201803475YA (en) 2018-05-30
CN108289886A (zh) 2018-07-17
MX2018005242A (es) 2019-03-18
RU2746188C2 (ru) 2021-04-08
EP3340988A4 (en) 2019-05-15
US10562857B2 (en) 2020-02-18
AU2016353446A1 (en) 2018-05-24
RU2018121288A3 (enExample) 2020-03-27
CN108289886B (zh) 2022-01-28
EP3340988C0 (en) 2025-04-09
RU2018121288A (ru) 2019-12-16
US20180312471A1 (en) 2018-11-01
BR112018009439A2 (pt) 2018-12-04
HK1254407A1 (zh) 2019-07-19
IL259199B (en) 2022-03-01
WO2017083867A1 (en) 2017-05-18
ZA201803739B (en) 2019-04-24
KR20180074705A (ko) 2018-07-03
EP3340988B1 (en) 2025-04-09
JP2018533593A (ja) 2018-11-15
JP6790094B2 (ja) 2020-11-25

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