JP7780440B2 - Kv1.3カリウムシェーカーチャネル遮断薬としてのアリール複素二環式化合物 - Google Patents
Kv1.3カリウムシェーカーチャネル遮断薬としてのアリール複素二環式化合物Info
- Publication number
- JP7780440B2 JP7780440B2 JP2022546592A JP2022546592A JP7780440B2 JP 7780440 B2 JP7780440 B2 JP 7780440B2 JP 2022546592 A JP2022546592 A JP 2022546592A JP 2022546592 A JP2022546592 A JP 2022546592A JP 7780440 B2 JP7780440 B2 JP 7780440B2
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- compound
- mmol
- dichloro
- group
- 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.)
- Active
Links
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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
- A61K31/535—Heterocyclic 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
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
-
- 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
-
- 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
-
- 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
-
- 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
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Diabetes (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Obesity (AREA)
- Hospice & Palliative Care (AREA)
- Hematology (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychiatry (AREA)
- Cardiology (AREA)
- Transplantation (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Pyridine Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962911648P | 2019-10-07 | 2019-10-07 | |
| US62/911,648 | 2019-10-07 | ||
| PCT/US2020/054393 WO2021071832A1 (en) | 2019-10-07 | 2020-10-06 | Aryl heterobicyclic compounds as kv1.3 potassium shaker channel blockers |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2022551199A JP2022551199A (ja) | 2022-12-07 |
| JP2022551199A5 JP2022551199A5 (https=) | 2024-05-20 |
| JP7780440B2 true JP7780440B2 (ja) | 2025-12-04 |
Family
ID=75438321
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022546592A Active JP7780440B2 (ja) | 2019-10-07 | 2020-10-06 | Kv1.3カリウムシェーカーチャネル遮断薬としてのアリール複素二環式化合物 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US20230049231A1 (https=) |
| EP (1) | EP4041405A4 (https=) |
| JP (1) | JP7780440B2 (https=) |
| KR (1) | KR20220079878A (https=) |
| AU (1) | AU2020362118A1 (https=) |
| BR (1) | BR112022006292A2 (https=) |
| CA (1) | CA3157020A1 (https=) |
| IL (1) | IL291866A (https=) |
| MX (1) | MX2022004178A (https=) |
| WO (1) | WO2021071832A1 (https=) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2023003841A (es) | 2020-10-06 | 2023-06-23 | De Shaw Res Llc | Compuestos lactámicos como bloqueadores del canal agitador de potasio kv1.3. |
| TW202521512A (zh) | 2023-07-31 | 2025-06-01 | 美商美國禮來大藥廠 | Kv1.3鉀shaker通道阻斷劑之固體形式及其使用方法 |
| WO2025161144A1 (zh) * | 2024-01-29 | 2025-08-07 | 上海深势唯思科技有限责任公司 | 芳基杂环类Kv1.3抑制剂及其制备方法和用途 |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2004511516A (ja) | 2000-10-17 | 2004-04-15 | ワイス | 膀胱の機能を調節する方法 |
| JP2006512378A (ja) | 2002-12-23 | 2006-04-13 | ブリストル−マイヤーズ スクイブ カンパニー | 3−置換−4−アリールキノリン−2−オン誘導体のアトロプ異性体 |
| JP2007506749A (ja) | 2003-09-23 | 2007-03-22 | メルク エンド カムパニー インコーポレーテッド | イソキノリンカリウムチャネル阻害剤 |
| WO2011073273A1 (en) | 2009-12-16 | 2011-06-23 | Evotec Ag | Benzoxazine aryl sulfonamide derivatives as kv1.3 modulators |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3854480A (en) | 1969-04-01 | 1974-12-17 | Alza Corp | Drug-delivery system |
| US4675189A (en) | 1980-11-18 | 1987-06-23 | Syntex (U.S.A.) Inc. | Microencapsulation of water soluble active polypeptides |
| US4452775A (en) | 1982-12-03 | 1984-06-05 | Syntex (U.S.A.) Inc. | Cholesterol matrix delivery system for sustained release of macromolecules |
| US5075109A (en) | 1986-10-24 | 1991-12-24 | Southern Research Institute | Method of potentiating an immune response |
| US5133974A (en) | 1989-05-05 | 1992-07-28 | Kv Pharmaceutical Company | Extended release pharmaceutical formulations |
| US5407686A (en) | 1991-11-27 | 1995-04-18 | Sidmak Laboratories, Inc. | Sustained release composition for oral administration of active ingredient |
| US5736152A (en) | 1995-10-27 | 1998-04-07 | Atrix Laboratories, Inc. | Non-polymeric sustained release delivery system |
| JP4377231B2 (ja) * | 2001-11-05 | 2009-12-02 | 大日本住友製薬株式会社 | 新規なカルバペネム化合物 |
| US7538110B2 (en) * | 2005-10-27 | 2009-05-26 | Adolor Corporation | Opioid antagonists |
| TWI370130B (en) * | 2005-11-24 | 2012-08-11 | Eisai R&D Man Co Ltd | Two cyclic cinnamide compound |
-
2020
- 2020-10-06 KR KR1020227013487A patent/KR20220079878A/ko not_active Withdrawn
- 2020-10-06 IL IL291866A patent/IL291866A/en unknown
- 2020-10-06 AU AU2020362118A patent/AU2020362118A1/en not_active Abandoned
- 2020-10-06 EP EP20873621.5A patent/EP4041405A4/en active Pending
- 2020-10-06 JP JP2022546592A patent/JP7780440B2/ja active Active
- 2020-10-06 MX MX2022004178A patent/MX2022004178A/es unknown
- 2020-10-06 BR BR112022006292A patent/BR112022006292A2/pt not_active IP Right Cessation
- 2020-10-06 CA CA3157020A patent/CA3157020A1/en active Pending
- 2020-10-06 WO PCT/US2020/054393 patent/WO2021071832A1/en not_active Ceased
- 2020-10-06 US US17/766,834 patent/US20230049231A1/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2004511516A (ja) | 2000-10-17 | 2004-04-15 | ワイス | 膀胱の機能を調節する方法 |
| JP2006512378A (ja) | 2002-12-23 | 2006-04-13 | ブリストル−マイヤーズ スクイブ カンパニー | 3−置換−4−アリールキノリン−2−オン誘導体のアトロプ異性体 |
| JP2007506749A (ja) | 2003-09-23 | 2007-03-22 | メルク エンド カムパニー インコーポレーテッド | イソキノリンカリウムチャネル阻害剤 |
| WO2011073273A1 (en) | 2009-12-16 | 2011-06-23 | Evotec Ag | Benzoxazine aryl sulfonamide derivatives as kv1.3 modulators |
Also Published As
| Publication number | Publication date |
|---|---|
| KR20220079878A (ko) | 2022-06-14 |
| JP2022551199A (ja) | 2022-12-07 |
| EP4041405A4 (en) | 2023-10-18 |
| US20230049231A1 (en) | 2023-02-16 |
| WO2021071832A1 (en) | 2021-04-15 |
| AU2020362118A1 (en) | 2022-04-21 |
| IL291866A (en) | 2022-06-01 |
| MX2022004178A (es) | 2022-06-16 |
| CA3157020A1 (en) | 2021-04-15 |
| BR112022006292A2 (pt) | 2022-06-28 |
| CN114828963A (zh) | 2022-07-29 |
| EP4041405A1 (en) | 2022-08-17 |
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