EA201890152A1 - Производные 2,3-дигидро-4h-1,3-бензоксазин-4-онов в качестве модуляторов холинергического мускаринового m1 рецептора - Google Patents
Производные 2,3-дигидро-4h-1,3-бензоксазин-4-онов в качестве модуляторов холинергического мускаринового m1 рецептораInfo
- Publication number
- EA201890152A1 EA201890152A1 EA201890152A EA201890152A EA201890152A1 EA 201890152 A1 EA201890152 A1 EA 201890152A1 EA 201890152 A EA201890152 A EA 201890152A EA 201890152 A EA201890152 A EA 201890152A EA 201890152 A1 EA201890152 A1 EA 201890152A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- cholinergic
- muscarin
- benzoxazin
- dihydro
- derivatives
- Prior art date
Links
- 230000001713 cholinergic effect Effects 0.000 title abstract 2
- YBYIZRPBXCCDQW-UHFFFAOYSA-N 2,3-dihydro-1,3-benzoxazin-4-one Chemical class C1=CC=C2C(=O)NCOC2=C1 YBYIZRPBXCCDQW-UHFFFAOYSA-N 0.000 title 1
- UQOFGTXDASPNLL-XHNCKOQMSA-N Muscarine Chemical compound C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O UQOFGTXDASPNLL-XHNCKOQMSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 206010012289 Dementia Diseases 0.000 abstract 1
- 102000007207 Muscarinic M1 Receptor Human genes 0.000 abstract 1
- 108010008406 Muscarinic M1 Receptor Proteins 0.000 abstract 1
- 208000002193 Pain Diseases 0.000 abstract 1
- 208000018737 Parkinson disease Diseases 0.000 abstract 1
- 244000309466 calf Species 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 229940126027 positive allosteric modulator Drugs 0.000 abstract 1
- 230000000069 prophylactic effect Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 201000000980 schizophrenia Diseases 0.000 abstract 1
- 208000019116 sleep disease Diseases 0.000 abstract 1
- 229940124597 therapeutic agent Drugs 0.000 abstract 1
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- 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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- 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
- A61K31/536—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 ortho- or peri-condensed with carbocyclic ring systems
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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
- A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/541—Non-condensed thiazines containing further heterocyclic rings
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- 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
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- 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
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D265/04—1,3-Oxazines; Hydrogenated 1,3-oxazines
- C07D265/12—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems
- C07D265/14—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring
- C07D265/20—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring with hetero atoms directly attached in position 4
- C07D265/22—Oxygen atoms
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- 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
- C07D413/04—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 directly linked by a ring-member-to-ring-member bond
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- 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
- C07D413/06—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 carbon chain containing only aliphatic carbon atoms
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- 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
- C07D413/10—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 carbon chain containing aromatic rings
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- 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
- C07D417/06—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 carbon chain containing only aliphatic carbon atoms
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- 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
- C07D417/10—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 carbon chain containing aromatic rings
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- 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
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- 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
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
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- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/0803—Compounds with Si-C or Si-Si linkages
- C07F7/081—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
- C07F7/0812—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring
- C07F7/0814—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring said ring is substituted at a C ring atom by Si
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- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
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- Biomedical Technology (AREA)
- Neurology (AREA)
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- Veterinary Medicine (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)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
Настоящее изобретение обеспечивает соединение, обладающее активностью положительного аллостерического модулятора холинергического мускаринового M1 рецептора, которое может быть полезным в качестве профилактического или терапевтического средства от болезни Альцгеймера, шизофрении, боли, расстройства сна, деменции при болезни Паркинсона, деменции с тельцами Леви и т.п. Настоящее изобретение относится к соединению, представленному формулой (I), или его соли:где каждый символ имеет значение, определенное в прилагаемом описании.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2015129043 | 2015-06-26 | ||
JP2015206797 | 2015-10-20 | ||
PCT/JP2016/069189 WO2016208775A1 (en) | 2015-06-26 | 2016-06-23 | 2,3-dihydro-4h-1,3-benzoxazin-4-one derivatives as modulators of cholinergic muscarinic m1 receptor |
Publications (1)
Publication Number | Publication Date |
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EA201890152A1 true EA201890152A1 (ru) | 2018-08-31 |
Family
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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EA201890152A EA201890152A1 (ru) | 2015-06-26 | 2016-06-23 | Производные 2,3-дигидро-4h-1,3-бензоксазин-4-онов в качестве модуляторов холинергического мускаринового m1 рецептора |
Country Status (23)
Country | Link |
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US (5) | US9878989B2 (ru) |
EP (1) | EP3313836B1 (ru) |
JP (1) | JP6745824B2 (ru) |
KR (1) | KR20180019234A (ru) |
CN (1) | CN107922403A (ru) |
AU (1) | AU2016284654B9 (ru) |
CA (1) | CA2988572A1 (ru) |
CL (1) | CL2017003127A1 (ru) |
CO (1) | CO2017012859A2 (ru) |
CR (1) | CR20170568A (ru) |
DO (1) | DOP2017000309A (ru) |
EA (1) | EA201890152A1 (ru) |
HK (1) | HK1248698A1 (ru) |
IL (1) | IL256059A (ru) |
MX (1) | MX2017016875A (ru) |
PE (1) | PE20180500A1 (ru) |
PH (1) | PH12017502351A1 (ru) |
TN (1) | TN2017000508A1 (ru) |
TW (1) | TW201710255A (ru) |
UA (1) | UA121503C2 (ru) |
UY (1) | UY36750A (ru) |
WO (1) | WO2016208775A1 (ru) |
ZA (1) | ZA201708387B (ru) |
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JP6745824B2 (ja) * | 2015-06-26 | 2020-08-26 | 武田薬品工業株式会社 | 複素環化合物 |
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JP6787913B2 (ja) | 2015-10-20 | 2020-11-18 | 武田薬品工業株式会社 | 複素環化合物 |
US10548877B2 (en) | 2016-03-11 | 2020-02-04 | Takeda Pharmaceutical Company Limited | Aromatic ring compound |
CA3054773A1 (en) * | 2017-02-28 | 2018-09-07 | Takeda Pharmaceutical Company Limited | Method for producing heterocyclic compound |
EP3612527B1 (en) | 2017-04-18 | 2022-07-20 | Takeda Pharmaceutical Company Limited | Heterocyclic compounds useful as modulators of acetylcholine receptors |
JP7197472B2 (ja) | 2017-05-19 | 2022-12-27 | 武田薬品工業株式会社 | スクリーニング方法 |
CA3068209A1 (en) | 2017-06-20 | 2018-12-27 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
HUE063823T2 (hu) | 2017-06-20 | 2024-02-28 | Heterociklusos vegyület és annak alkalmazása a kolinerg muszkarin M1 receptor pozitív alloszterikus modulátoraként | |
WO2020067456A1 (ja) | 2018-09-28 | 2020-04-02 | 武田薬品工業株式会社 | 複素環化合物 |
US20220041581A1 (en) | 2018-09-28 | 2022-02-10 | Takeda Pharmaceutical Company Limited | Condensed-cyclic compound |
BR112021005759A2 (pt) | 2018-09-28 | 2021-07-06 | Takeda Pharmaceuticals Co | composto, medicamento, métodos de modulação alostérica positiva e para a profilaxia ou o tratamento de constipação, e, uso do composto ou de um sal do mesmo |
KR102288434B1 (ko) * | 2018-10-18 | 2021-08-12 | 에이치케이이노엔 주식회사 | 신규한 (이소프로필-트리아졸릴)피리디닐 치환된 벤조옥사지논 또는 벤조티아지논 유도체 및 이의 용도 |
EP3870173A4 (en) | 2018-10-24 | 2022-06-22 | Vanderbilt University | WDR5 MODULATORS AND INHIBITORS |
WO2020247679A1 (en) * | 2019-06-04 | 2020-12-10 | Vanderbilt University | Wdr5 inhibitors and modulators |
CN114539035B (zh) * | 2021-03-10 | 2023-08-18 | 山东新时代药业有限公司 | 一种七氟烷的合成方法 |
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