JP7117306B2 - Ｒｈｏキナーゼ阻害剤ＢＡ‐１０４９（Ｒ）及びその活性代謝物 - Google Patents

Ｒｈｏキナーゼ阻害剤ＢＡ‐１０４９（Ｒ）及びその活性代謝物 Download PDF

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JP7117306B2
JP7117306B2 JP2019534685A JP2019534685A JP7117306B2 JP 7117306 B2 JP7117306 B2 JP 7117306B2 JP 2019534685 A JP2019534685 A JP 2019534685A JP 2019534685 A JP2019534685 A JP 2019534685A JP 7117306 B2 JP7117306 B2 JP 7117306B2
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rock2
hydroxy
cells
mice
brain
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JP2020502248A (ja
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エム． ローゼン、ケネス
ディ． アビナンティ、マシュー
ルッシェル、イェルク
マッケラッチャー、リサ
ボンド モーリッツ、リサ
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バイオアクソン バイオサイエンシーズ インコーポレイテッド
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    • 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
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • 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
    • A61K31/495—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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/08—Vasodilators for multiple indications
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Compounds Of Unknown Constitution (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
JP2019534685A 2016-12-21 2017-05-09 Ｒｈｏキナーゼ阻害剤ＢＡ‐１０４９（Ｒ）及びその活性代謝物 Active JP7117306B2 (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2022105969A JP7461414B2 (ja) 2016-12-21 2022-06-30 Ｒｈｏキナーゼ阻害剤ＢＡ‐１０４９（Ｒ）及びその活性代謝物

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662437181P 2016-12-21 2016-12-21
US62/437,181 2016-12-21
PCT/US2017/031836 WO2018118109A1 (en) 2016-12-21 2017-05-09 Rho kinase inhibitor ba-1049 (r) and active metabolites thereof

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JP2022105969A Division JP7461414B2 (ja) 2016-12-21 2022-06-30 Ｒｈｏキナーゼ阻害剤ＢＡ‐１０４９（Ｒ）及びその活性代謝物

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JP2020502248A5 JP2020502248A5 (enExample) 2020-06-18
JP7117306B2 true JP7117306B2 (ja) 2022-08-12

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JP2022105969A Active JP7461414B2 (ja) 2016-12-21 2022-06-30 Ｒｈｏキナーゼ阻害剤ＢＡ‐１０４９（Ｒ）及びその活性代謝物

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JP (2) JP7117306B2 (enExample)
DK (1) DK3558314T3 (enExample)
ES (1) ES3002432T3 (enExample)
FI (1) FI3558314T3 (enExample)
PL (1) PL3558314T3 (enExample)
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WO (1) WO2018118109A1 (enExample)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10106525B2 (en) 2015-01-26 2018-10-23 BioAxone BioSciences, Inc. Rho kinase inhibitor BA-1049 (R) and active metabolites thereof
US10857157B2 (en) 2015-01-26 2020-12-08 BioAxone BioSciences, Inc. Treatment of cerebral cavernous malformations and cerebral aneurysms with rho kinase inhibitors
US11198680B2 (en) 2016-12-21 2021-12-14 BioAxone BioSciences, Inc. Rho kinase inhibitor BA-1049 (R) and active metabolites thereof
ES3002432T3 (en) * 2016-12-21 2025-03-06 Bioaxone Biosciences Inc Rho kinase inhibitor ba-1049 (r) and active metabolites thereof
WO2019014322A1 (en) 2017-07-11 2019-01-17 BioAxone BioSciences, Inc. KINASE INHIBITORS FOR THE TREATMENT OF DISEASES
SI3877364T1 (sl) * 2018-11-06 2025-02-28 Cervello Therapeutics, Llc Inhibitorji rock kinaze
WO2021085645A1 (ja) 2019-11-01 2021-05-06 キリンホールディングス株式会社 多成分試料における物質の構造決定方法
JP7213839B2 (ja) * 2019-11-21 2023-01-27 キリンホールディングス株式会社 結晶スポンジ法による構造解析のための結晶構造解析用試料の調製方法
EP4063839A4 (en) * 2019-11-21 2023-11-22 Kirin Holdings Kabushiki Kaisha METHOD FOR PREPARING A CRYSTAL STRUCTURAL ANALYSIS SAMPLE FOR STRUCTURAL ANALYSIS BY CRYSTAL SPONGE METHOD
CN115975940B (zh) * 2021-10-15 2025-09-02 合肥中科普瑞昇生物医药科技有限公司 胃癌原代细胞的培养基和培养方法
JPWO2023085369A1 (enExample) 2021-11-11 2023-05-19

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007523202A (ja) 2004-02-24 2007-08-16 ビオアクソン・テラプティーク・インコーポレーテッド ４置換ピペリジン誘導体
WO2008105442A1 (ja) 2007-02-28 2008-09-04 Asahi Kasei Pharma Corporation スルホンアミド誘導体
JP2011530518A (ja) 2008-08-05 2011-12-22 アボット・ラボラトリーズ タンパク質キナーゼの阻害剤として有用な化合物
US20160213664A1 (en) 2015-01-26 2016-07-28 BioAxone BioSciences, Inc. Treatment of cerebral cavernous malformations and cerebral aneurysms with rho kinase inhibitors

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US20050014783A1 (en) * 2003-05-29 2005-01-20 Schering Aktiengesellschaft Use of Rho-kinase inhibitors in the treatment of aneurysm and cardiac hypertrophy
JP4652112B2 (ja) 2005-04-26 2011-03-16 富士フイルム株式会社 投射型表示装置
US8957093B2 (en) 2011-06-06 2015-02-17 The Scripps Research Institute N-biphenylmethylindole modulators of PPARG
JP6397831B2 (ja) * 2013-03-06 2018-09-26 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｊａｋ阻害剤の製造方法及びその中間体
ES2774923T3 (es) * 2014-04-28 2020-07-23 China Resources Pharmaceutical Holdings Company Ltd Derivados de isoquinolinsulfonilo como inhibidores de RHO quinasa
US9902702B2 (en) * 2014-07-15 2018-02-27 Bristol-Myers Squibb Company Spirocycloheptanes as inhibitors of rock
ES3002432T3 (en) * 2016-12-21 2025-03-06 Bioaxone Biosciences Inc Rho kinase inhibitor ba-1049 (r) and active metabolites thereof

Patent Citations (4)

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JP2007523202A (ja) 2004-02-24 2007-08-16 ビオアクソン・テラプティーク・インコーポレーテッド ４置換ピペリジン誘導体
WO2008105442A1 (ja) 2007-02-28 2008-09-04 Asahi Kasei Pharma Corporation スルホンアミド誘導体
JP2011530518A (ja) 2008-08-05 2011-12-22 アボット・ラボラトリーズ タンパク質キナーゼの阻害剤として有用な化合物
US20160213664A1 (en) 2015-01-26 2016-07-28 BioAxone BioSciences, Inc. Treatment of cerebral cavernous malformations and cerebral aneurysms with rho kinase inhibitors

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Journal of Medicinal Chemistry，2015年，Vol. 58，pp. 5028-5037
Journal of Pharmaceutical Sciences，1977年，Vol.66, No.1，p.1-19
Kitakanto Med J，2003年，Vol. 53，pp. 99-100

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EP3558314A1 (en) 2019-10-30
PT3558314T (pt) 2024-12-19
PL3558314T3 (pl) 2025-02-24
JP2022141695A (ja) 2022-09-29
JP7461414B2 (ja) 2024-04-03
WO2018118109A1 (en) 2018-06-28
DK3558314T3 (da) 2024-11-04
EP3558314B1 (en) 2024-10-23
JP2020502248A (ja) 2020-01-23
ES3002432T3 (en) 2025-03-06
FI3558314T3 (fi) 2024-11-29
EP4509138A3 (en) 2025-04-23
EP3558314A4 (en) 2020-08-26
EP4509138A2 (en) 2025-02-19

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