JP2024508903A - Ｔ型カルシウムチャネルアンタゴニストおよびその使用 - Google Patents

Ｔ型カルシウムチャネルアンタゴニストおよびその使用 Download PDF

Info

Publication number
JP2024508903A
JP2024508903A JP2023553432A JP2023553432A JP2024508903A JP 2024508903 A JP2024508903 A JP 2024508903A JP 2023553432 A JP2023553432 A JP 2023553432A JP 2023553432 A JP2023553432 A JP 2023553432A JP 2024508903 A JP2024508903 A JP 2024508903A
Authority
JP
Japan
Prior art keywords
miro1
alkyl
haloalkyl
cycloalkyl
pyrazolo
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.)
Pending
Application number
JP2023553432A
Other languages
English (en)
Japanese (ja)
Other versions
JP2024508903A5 (https=
Inventor
ワン シンナン
バンホーウェルト ローランド
ザーラー ロバート
バーラト ビニータ
グエン デイビッド
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Leland Stanford Junior University
Original Assignee
Leland Stanford Junior University
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 Leland Stanford Junior University filed Critical Leland Stanford Junior University
Publication of JP2024508903A publication Critical patent/JP2024508903A/ja
Publication of JP2024508903A5 publication Critical patent/JP2024508903A5/ja
Pending legal-status Critical Current

Links

Images

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61P25/28—Drugs 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/65—One oxygen atom attached in position 3 or 5
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/056—Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/68—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids
    • G01N33/6893—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids related to diseases not provided for elsewhere
    • G01N33/6896—Neurological disorders, e.g. Alzheimer's disease
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/90—Enzymes; Proenzymes
    • G01N2333/914—Hydrolases (3)
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2800/00—Detection or diagnosis of diseases
    • G01N2800/50—Determining the risk of developing a disease

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Neurosurgery (AREA)
  • Public Health (AREA)
  • Neurology (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hematology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Cell Biology (AREA)
  • Microbiology (AREA)
  • General Physics & Mathematics (AREA)
  • Biochemistry (AREA)
  • Analytical Chemistry (AREA)
  • Physics & Mathematics (AREA)
  • Food Science & Technology (AREA)
  • Pathology (AREA)
  • Biotechnology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
JP2023553432A 2021-03-04 2022-03-03 Ｔ型カルシウムチャネルアンタゴニストおよびその使用 Pending JP2024508903A (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US202163156806P 2021-03-04 2021-03-04
US63/156,806 2021-03-04
US202163228505P 2021-08-02 2021-08-02
US63/228,505 2021-08-02
PCT/US2022/018682 WO2022216386A2 (en) 2021-03-04 2022-03-03 T-type calcium channel antagonists and uses thereof

Publications (2)

Publication Number Publication Date
JP2024508903A true JP2024508903A (ja) 2024-02-28
JP2024508903A5 JP2024508903A5 (https=) 2025-03-11

Family

ID=83545681

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2023553432A Pending JP2024508903A (ja) 2021-03-04 2022-03-03 Ｔ型カルシウムチャネルアンタゴニストおよびその使用

Country Status (10)

Country Link
US (1) US20240190865A1 (https=)
EP (1) EP4301759A4 (https=)
JP (1) JP2024508903A (https=)
KR (1) KR20230167035A (https=)
AU (1) AU2022255225A1 (https=)
BR (1) BR112023016601A2 (https=)
CA (1) CA3208202A1 (https=)
IL (1) IL305381A (https=)
MX (1) MX2023010175A (https=)
WO (1) WO2022216386A2 (https=)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2024081653A2 (en) * 2022-10-12 2024-04-18 Acurex Biosciences Corporation Methods of lowering miro2 to treat neurodegenerative diseases
EP4611744A1 (en) * 2022-10-31 2025-09-10 Acurex Biosciences Corporation Methods of reducing miro1 or phosphorylated alpha-synuclein
CN116813444A (zh) * 2023-06-28 2023-09-29 福建凯昕药业有限公司 一种1-溴-4-(1-(三氟甲基)环丙基)苯的制备方法
WO2025257786A1 (en) * 2024-06-13 2025-12-18 Iama Therapeutics S.R.L. Benzoimidazole derivatives as nkcc1 inhibitors

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009534320A (ja) * 2006-04-12 2009-09-24 メルク エンド カムパニー インコーポレーテッド ピリジルアミドｔ型カルシウムチャンネルアンタゴニスト
JP2011500809A (ja) * 2007-10-24 2011-01-06 メルク・シャープ・エンド・ドーム・コーポレイション 複素環フェニルアミドｔ型カルシウムチャネルアンタゴニスト
JP2011500808A (ja) * 2007-10-24 2011-01-06 メルク・シャープ・エンド・ドーム・コーポレイション 複素環アミドｔ型カルシウムチャネルアンタゴニスト
WO2011053542A1 (en) * 2009-10-30 2011-05-05 Merck Sharp & Dohme Corp. Heterocycle amide t-type calcium channel antagonists
JP2022546604A (ja) * 2019-09-05 2022-11-04 ザ ボード オブ トラスティーズ オブ ザ レランド スタンフォード ジュニア ユニバーシティー ミトコンドリア機能を修飾する方法および化合物

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6610701B2 (en) * 2001-02-09 2003-08-26 Merck & Co., Inc. Thrombin inhibitors

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009534320A (ja) * 2006-04-12 2009-09-24 メルク エンド カムパニー インコーポレーテッド ピリジルアミドｔ型カルシウムチャンネルアンタゴニスト
JP2011500809A (ja) * 2007-10-24 2011-01-06 メルク・シャープ・エンド・ドーム・コーポレイション 複素環フェニルアミドｔ型カルシウムチャネルアンタゴニスト
JP2011500808A (ja) * 2007-10-24 2011-01-06 メルク・シャープ・エンド・ドーム・コーポレイション 複素環アミドｔ型カルシウムチャネルアンタゴニスト
WO2011053542A1 (en) * 2009-10-30 2011-05-05 Merck Sharp & Dohme Corp. Heterocycle amide t-type calcium channel antagonists
JP2022546604A (ja) * 2019-09-05 2022-11-04 ザ ボード オブ トラスティーズ オブ ザ レランド スタンフォード ジュニア ユニバーシティー ミトコンドリア機能を修飾する方法および化合物

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
ZHANG, CHEN ET AL.: ""Discovery of novel PDE9A inhibitors with antioxidant activities for treatment of Alzheimer’s dise", JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol. 33, no. 1, JPN6025050428, 22 December 2017 (2017-12-22), pages 260 - 270, ISSN: 0005749294 *

Also Published As

Publication number Publication date
MX2023010175A (es) 2023-09-07
WO2022216386A9 (en) 2022-12-01
CA3208202A1 (en) 2022-10-13
BR112023016601A2 (pt) 2023-12-12
EP4301759A2 (en) 2024-01-10
WO2022216386A2 (en) 2022-10-13
WO2022216386A3 (en) 2023-01-12
IL305381A (en) 2023-10-01
US20240190865A1 (en) 2024-06-13
KR20230167035A (ko) 2023-12-07
AU2022255225A1 (en) 2023-09-21
EP4301759A4 (en) 2025-09-24

Similar Documents

Publication Publication Date Title
JP2024508903A (ja) Ｔ型カルシウムチャネルアンタゴニストおよびその使用
CA2887701C (en) Gsk3 inhibitors and methods of use thereof
US9434734B2 (en) Substituted pyrazoloquinazolinones and pyrroloquinazolinones as allosteric modulators of group II metabotropic glutamate receptors
KR101762981B1 (ko) 기분 장해 치료제
KR20170103838A (ko) 염증 및 암의 치료를 위한 헤테로시클릭 itk 저해제
JP2017503815A (ja) がんまたは炎症性疾患を処置するための置換されたピロロピリジンおよびピロロピラジン
KR20190087622A (ko) 질환 치료를 위한 이중 류신 지퍼 (dlk) 키나아제의 바이시클로[1.1.1]펜탄 억제제
KR20180110132A (ko) 무스카린성 아세틸콜린 수용체 m1의 양성 알로스테릭 조절제
US20180346468A1 (en) Substituted tricyclic 1,4-benzodiazepinone derivatives as allosteric modulators of group ii metabotropic glutamate receptors
KR20190112022A (ko) 단백질 응집의 조절제로서의 바이사이클릭 비스-헤테로아릴 유도체
JP2021520340A (ja) 化合物およびｐｄｅ４活性剤としてのそれらの使用
TW202421130A (zh) 作為pi3k抑制劑的異喹啉酮
TW201720829A (zh) 哌喃并二吡啶化合物
JP6116761B2 (ja) 代謝型グルタミン酸受容体アンタゴニストとしてのエチニル誘導体
WO2024081653A2 (en) Methods of lowering miro2 to treat neurodegenerative diseases
US20190152979A1 (en) Substituted pyrazoloquinazolinones and pyrroloquinazolinones as allosteric modulators of group ii metabotropic glutamate receptors
KR20160127826A (ko) 비장 티로신 키나제 억제제로서 치환된 옥사졸 유도체
WO2024097632A1 (en) Methods of reducing miro1 or phosphorylated alpha-synuclein
US11472806B2 (en) Substituted heterocyclic compounds as allosteric modulators of group II metabotropic glutamate receptors
CN116917289A (zh) T型钙通道拮抗剂及其用途
TW202438051A (zh) 用於選擇性降解工程化蛋白質的化合物及組合物
HK1255833A1 (en) Hpk1 inhibitors and methods of using same
HK1260037B (zh) 取代的三环杂环化合物及其用途
HK1255833B (en) Hpk1 inhibitors and methods of using same
HK1159947A (en) Triazolopyridine jak inhibitor compounds and methods

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20250303

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20250303

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20251120

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20251209

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20260309