JP2020525475A - N−[1−(5−シアノ−ピリジン−2−イルメチル)−1h−ピラゾール−3−イル]−2−[4−(1−トリフルオロメチル−シクロプロピル)−フェニル]−アセタミドの結晶形 - Google Patents

N−[1−(5−シアノ−ピリジン−2−イルメチル)−1h−ピラゾール−3−イル]−2−[4−(1−トリフルオロメチル−シクロプロピル)−フェニル]−アセタミドの結晶形 Download PDF

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JP2020525475A
JP2020525475A JP2019572102A JP2019572102A JP2020525475A JP 2020525475 A JP2020525475 A JP 2020525475A JP 2019572102 A JP2019572102 A JP 2019572102A JP 2019572102 A JP2019572102 A JP 2019572102A JP 2020525475 A JP2020525475 A JP 2020525475A
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trifluoromethyl
pyrazol
phenyl
ylmethyl
cyano
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JP2020525475A5 (enExample
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ハイドマン ビビア
ハイドマン ビビア
フォン ラウマー マルクス
フォン ラウマー マルクス
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Idorsia Pharmaceuticals Ltd
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Idorsia Pharmaceuticals Ltd
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Priority to JP2023104050A priority Critical patent/JP2023123679A/ja
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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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non 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
    • 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
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2019572102A 2017-07-05 2018-07-04 N−[1−(5−シアノ−ピリジン−2−イルメチル)−1h−ピラゾール−3−イル]−2−[4−(1−トリフルオロメチル−シクロプロピル)−フェニル]−アセタミドの結晶形 Pending JP2020525475A (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2023104050A JP2023123679A (ja) 2017-07-05 2023-06-26 N-[1-(5-シアノ-ピリジン-2-イルメチル)-1h-ピラゾール-3-イル]-2-[4-(1-トリフルオロメチル-シクロプロピル)-フェニル]-アセタミドの結晶形

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP2017066806 2017-07-05
EPPCT/EP2017/066806 2017-07-05
PCT/EP2018/068087 WO2019008034A1 (en) 2017-07-05 2018-07-04 CRYSTALLINE FORM OF N- [1- (5-CYANO-PYRIDIN-2-YLMETHYL) -1H-PYRAZOL-3-YL] -2- [4- (1-TRIFLUOROMETHYL-CYCLOPROPYL) -PHENYL] -ACETAMIDE

Related Child Applications (1)

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JP2023104050A Division JP2023123679A (ja) 2017-07-05 2023-06-26 N-[1-(5-シアノ-ピリジン-2-イルメチル)-1h-ピラゾール-3-イル]-2-[4-(1-トリフルオロメチル-シクロプロピル)-フェニル]-アセタミドの結晶形

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JP2020525475A true JP2020525475A (ja) 2020-08-27
JP2020525475A5 JP2020525475A5 (enExample) 2021-08-12

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JP2019572102A Pending JP2020525475A (ja) 2017-07-05 2018-07-04 N−[1−(5−シアノ−ピリジン−2−イルメチル)−1h−ピラゾール−3−イル]−2−[4−(1−トリフルオロメチル−シクロプロピル)−フェニル]−アセタミドの結晶形
JP2023104050A Pending JP2023123679A (ja) 2017-07-05 2023-06-26 N-[1-(5-シアノ-ピリジン-2-イルメチル)-1h-ピラゾール-3-イル]-2-[4-(1-トリフルオロメチル-シクロプロピル)-フェニル]-アセタミドの結晶形

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JP2023104050A Pending JP2023123679A (ja) 2017-07-05 2023-06-26 N-[1-(5-シアノ-ピリジン-2-イルメチル)-1h-ピラゾール-3-イル]-2-[4-(1-トリフルオロメチル-シクロプロピル)-フェニル]-アセタミドの結晶形

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US (2) US11059803B2 (enExample)
EP (1) EP3649117B1 (enExample)
JP (2) JP2020525475A (enExample)
KR (1) KR102645911B1 (enExample)
CN (1) CN110831932A (enExample)
AU (1) AU2018296423B2 (enExample)
BR (1) BR112020000099A2 (enExample)
CA (1) CA3067489A1 (enExample)
CL (1) CL2020000002A1 (enExample)
EA (1) EA202090193A1 (enExample)
IL (1) IL271764B2 (enExample)
MA (1) MA50972A (enExample)
MY (1) MY206357A (enExample)
PH (1) PH12020500040A1 (enExample)
SG (1) SG11201912881SA (enExample)
UA (1) UA126582C2 (enExample)
WO (1) WO2019008034A1 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2024531363A (ja) * 2021-08-17 2024-08-29 コリア アドバンスト インスティテュート オブ サイエンス アンド テクノロジー Cav3.1遺伝子を標的とするアンチセンスオリゴヌクレオチド及びその使用

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI808952B (zh) 2016-12-16 2023-07-21 瑞士商愛杜西亞製藥有限公司 包含t型鈣通道阻斷劑之醫藥組合
CN110234622B (zh) 2017-02-06 2023-07-04 爱杜西亚药品有限公司 用于合成1-芳基-1-三氟甲基环丙烷的新颖方法
KR102645911B1 (ko) * 2017-07-05 2024-03-08 이도르시아 파마슈티컬스 리미티드 N-[1-(5-시아노-피리딘-2-일메틸)-1h-피라졸-3-일]-2-[4-(1-트리플루오로메틸-시클로프로필)-페닐]-아세타미드의 결정질 형태
US20230047102A1 (en) 2019-12-20 2023-02-16 Idorsia Pharmaceuticals Ltd Pharmaceutical compositions comprising n-[1-(5-cyano-pyridin-2-ylmethyl)-1h-pyrazol-3-yl]-2-[4-(1-trifluoromethyl-cyclopropyl)-phenyl]-acetamide
WO2023240205A1 (en) 2022-06-10 2023-12-14 Neurocrine Biosciences, Inc. Deuterated compounds

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017516830A (ja) * 2014-06-03 2017-06-22 アクテリオン ファーマシューティカルズ リミテッドActelion Pharmaceuticals Ltd ピラゾール化合物及びt型カルシウムチャンネルブロッカーとしてのそれらの使用

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Publication number Priority date Publication date Assignee Title
JP6500092B2 (ja) 2014-09-15 2019-04-10 イドーシア ファーマシューティカルズ リミテッドIdorsia Pharmaceuticals Ltd T型カルシウムチャンネルブロッカーとしてのトリアゾール化合物
TWI808952B (zh) 2016-12-16 2023-07-21 瑞士商愛杜西亞製藥有限公司 包含t型鈣通道阻斷劑之醫藥組合
CN110234622B (zh) 2017-02-06 2023-07-04 爱杜西亚药品有限公司 用于合成1-芳基-1-三氟甲基环丙烷的新颖方法
KR102645911B1 (ko) * 2017-07-05 2024-03-08 이도르시아 파마슈티컬스 리미티드 N-[1-(5-시아노-피리딘-2-일메틸)-1h-피라졸-3-일]-2-[4-(1-트리플루오로메틸-시클로프로필)-페닐]-아세타미드의 결정질 형태

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017516830A (ja) * 2014-06-03 2017-06-22 アクテリオン ファーマシューティカルズ リミテッドActelion Pharmaceuticals Ltd ピラゾール化合物及びt型カルシウムチャンネルブロッカーとしてのそれらの使用

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STAHLY,P.: "医薬品の塩選択,結晶多形のスクリーニングの重要性について", 薬剤学, vol. 66, no. 6, JPN6015024142, 2006, pages 435 - 439, ISSN: 0005000426 *
平山令明, 有機化合物結晶作製ハンドブック −原理とノウハウ−, JPN6011053065, 25 July 2008 (2008-07-25), pages 57 - 84, ISSN: 0005000428 *
芦澤一英: "塩・結晶形の最適化と結晶化技術", PHARM TECH JAPAN, vol. 18, no. 10, JPN6013060608, 2002, pages 81 - 96, ISSN: 0005000429 *
長瀬博監訳, 最新 創薬化学 下巻, JPN6008054607, 25 September 1999 (1999-09-25), pages 347 - 365, ISSN: 0005000425 *
高田則幸: "創薬段階における原薬Formスクリーニングと選択", PHARM STAGE, vol. 6, no. 10, JPN6009053755, 15 January 2007 (2007-01-15), pages 20 - 25, ISSN: 0005000427 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2024531363A (ja) * 2021-08-17 2024-08-29 コリア アドバンスト インスティテュート オブ サイエンス アンド テクノロジー Cav3.1遺伝子を標的とするアンチセンスオリゴヌクレオチド及びその使用

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US11555025B2 (en) 2023-01-17
UA126582C2 (uk) 2022-11-02
BR112020000099A2 (pt) 2020-07-07
WO2019008034A1 (en) 2019-01-10
SG11201912881SA (en) 2020-01-30
EA202090193A1 (ru) 2020-06-03
JP2023123679A (ja) 2023-09-05
MA50972A (fr) 2020-10-14
US20200165221A1 (en) 2020-05-28
US11059803B2 (en) 2021-07-13
MY206357A (en) 2024-12-12
CN110831932A (zh) 2020-02-21
IL271764B1 (en) 2023-06-01
IL271764A (en) 2020-02-27
EP3649117B1 (en) 2024-10-09
CA3067489A1 (en) 2019-01-10
KR102645911B1 (ko) 2024-03-08
CL2020000002A1 (es) 2020-07-31
US20210300894A1 (en) 2021-09-30
KR20200018698A (ko) 2020-02-19
PH12020500040A1 (en) 2020-10-12
IL271764B2 (en) 2023-10-01
AU2018296423A1 (en) 2020-02-20
AU2018296423B2 (en) 2022-07-28
EP3649117A1 (en) 2020-05-13

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