AR115015A1 - Derivados de azaespiro piperazina - Google Patents
Derivados de azaespiro piperazinaInfo
- Publication number
- AR115015A1 AR115015A1 ARP190100746A ARP190100746A AR115015A1 AR 115015 A1 AR115015 A1 AR 115015A1 AR P190100746 A ARP190100746 A AR P190100746A AR P190100746 A ARP190100746 A AR P190100746A AR 115015 A1 AR115015 A1 AR 115015A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- alkoxy
- members
- heterocycloalkyl
- heteroaryl
- Prior art date
Links
Classifications
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- 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
- C07D401/14—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 three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- 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
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
- A61P25/10—Antiepileptics; Anticonvulsants for petit-mal
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- 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
- C07D401/08—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 carbon chain containing alicyclic rings
-
- 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
-
- 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
- C07D413/14—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
-
- 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
- C07D417/14—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 three or more hetero rings
-
- 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
-
- 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
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Pulmonology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Urology & Nephrology (AREA)
- Addiction (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Cosmetics (AREA)
Abstract
La presente proporciona, en parte, compuestos de fórmula (1), o un N-óxido del mismo, o una sal farmacéuticamente aceptable del compuesto o el N-óxido, en donde: X¹, X², R¹, R², m y n son como se describe en la presente; procesos para la preparación de; intermediarios usados en la preparación de; y composiciones que contienen dichos compuestos, N-óxidos o sales, y sus usos para tratar trastornos mediados por M4 (o asociados con M4) que incluyen, por ejemplo, enfermedad de Alzheimer, enfermedad de Parkinson, esquizofrenia (por ejemplo, sus síntomas cognitivos y negativos), dolor, adicción y un trastorno del sueño. Reivindicación 1: Un compuesto de fórmula (1), o un N-óxido del mismo, o una sal farmacéuticamente aceptable del compuesto o el N-óxido, en donde: X¹ y X² son cada uno independientemente CH o nitrógeno, siempre y cuando X¹ y X² no sean ambos CH; R¹ se selecciona del grupo que consiste en halógeno, ciano, hidroxi, -SF₅, nitro, -N(R⁶)(R⁷), C₁₋₆ alquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, C₁₋₆ alquiltio, C₁₋₆ alcoxi, C₃₋₆ cicloalquilo, -O-heterocicloalquilo (4 a 6 miembros), C₆₋₁₀ arilo, heteroarilo (5 a 10 miembros) y heterocicloalquilo (4 a 8 miembros), en donde dicho C₁₋₆ alquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, C₁₋₆ alquiltio, C₁₋₆ alcoxi, C₃₋₆ cicloalquilo, -O-heterocicloalquilo (4 a 6 miembros), C₆₋₁₀ arilo, heteroarilo (5 a 10 miembros) y heterocicloalquilo (4 a 8 miembros) están opcionalmente sustituidos con 1 a 3 sustituyentes seleccionados del grupo que consiste en halógeno, ciano, hidroxi, -N(R⁶)(R⁷), C₁₋₆ alquilo, C₁₋₆ alcoxi, C₃₋₆ cicloalquilo, y heteroarilo (5 a 6 miembros), en donde dicho C₁₋₆ alquilo, C₁₋₆ alcoxi, y heteroarilo (5 a 6 miembros) están opcionalmente sustituidos con 1 a 3 sustituyentes seleccionados del grupo que consiste en halógeno, ciano, hidroxi, C₁₋₆ alquilo y C₁₋₆ alcoxi; R² se selecciona del grupo que consiste en hidrógeno, halógeno, ciano, hidroxi, -SF₅, nitro, -N(R⁶)(R⁷), C₁₋₆ alquilo, y C₁₋₆ alcoxi, en donde dicho C₁₋₆ alquilo y C₁₋₆ alcoxi están opcionalmente sustituidos con 1 a 3 halógenos; R⁶ y R⁷ se seleccionan, cada uno independientemente, de hidrógeno, C₁₋₆ alquilo o C(O)-CH₃; m es 1 ó 2; y n es 1 ó 2.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201862647106P | 2018-03-23 | 2018-03-23 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR115015A1 true AR115015A1 (es) | 2020-11-18 |
Family
ID=66102243
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP190100746A AR115015A1 (es) | 2018-03-23 | 2019-03-25 | Derivados de azaespiro piperazina |
Country Status (14)
Country | Link |
---|---|
US (2) | US11524954B2 (es) |
EP (2) | EP3768669B1 (es) |
JP (2) | JP7497294B2 (es) |
CN (1) | CN112154145B (es) |
AR (1) | AR115015A1 (es) |
CA (1) | CA3094366A1 (es) |
DK (1) | DK3768669T3 (es) |
ES (1) | ES2942837T3 (es) |
FI (1) | FI3768669T3 (es) |
HU (1) | HUE061533T2 (es) |
PL (1) | PL3768669T3 (es) |
PT (1) | PT3768669T (es) |
TW (1) | TWI801540B (es) |
WO (1) | WO2019183636A1 (es) |
Families Citing this family (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU2020364186B2 (en) | 2019-10-09 | 2023-11-30 | Novartis Ag | 5-oxa-2-azaspiro(3.4)octane derivatives as M4 agonists |
UY38906A (es) | 2019-10-09 | 2021-05-31 | Novartis Ag | Compuestos 2- derivados de azaspiro[3,4]octano como agonistas de m4 y composiciones de los mismos |
KR20210067005A (ko) * | 2019-11-28 | 2021-06-08 | 제이투에이치바이오텍 (주) | 에다라본 전구체 약물 화합물 및 이들의 신경퇴행성 또는 운동신경 질환의 치료 또는 개선을 위한 의약 용도 |
JP2023512762A (ja) * | 2020-02-05 | 2023-03-29 | ニューロクライン バイオサイエンシーズ,インコーポレイテッド | ムスカリン性受容体4アンタゴニストおよび使用方法 |
JP2024528091A (ja) * | 2021-07-30 | 2024-07-26 | ニューロクライン バイオサイエンシーズ,インコーポレイテッド | ムスカリン性受容体4アンタゴニストおよび使用方法 |
WO2024059249A1 (en) * | 2022-09-16 | 2024-03-21 | Cerevel Therapeutics, Llc | M4 activators/modulators and uses thereof |
WO2024151833A1 (en) * | 2023-01-12 | 2024-07-18 | Cerevel Therapeutics, Llc | Spiro derivatives as m4 activators/modulators and uses thereof |
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2019
- 2019-03-25 AR ARP190100746A patent/AR115015A1/es unknown
- 2019-03-25 EP EP19716666.3A patent/EP3768669B1/en active Active
- 2019-03-25 CN CN201980033911.5A patent/CN112154145B/zh active Active
- 2019-03-25 DK DK19716666.3T patent/DK3768669T3/da active
- 2019-03-25 EP EP23151669.1A patent/EP4219464A1/en active Pending
- 2019-03-25 FI FIEP19716666.3T patent/FI3768669T3/fi active
- 2019-03-25 PL PL19716666.3T patent/PL3768669T3/pl unknown
- 2019-03-25 ES ES19716666T patent/ES2942837T3/es active Active
- 2019-03-25 US US17/040,479 patent/US11524954B2/en active Active
- 2019-03-25 HU HUE19716666A patent/HUE061533T2/hu unknown
- 2019-03-25 PT PT197166663T patent/PT3768669T/pt unknown
- 2019-03-25 TW TW108110350A patent/TWI801540B/zh active
- 2019-03-25 JP JP2020551327A patent/JP7497294B2/ja active Active
- 2019-03-25 WO PCT/US2019/023916 patent/WO2019183636A1/en active Application Filing
- 2019-03-25 CA CA3094366A patent/CA3094366A1/en active Pending
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2022
- 2022-10-19 US US17/969,479 patent/US20230192654A1/en active Pending
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2023
- 2023-12-20 JP JP2023214561A patent/JP2024037979A/ja active Pending
Also Published As
Publication number | Publication date |
---|---|
US20210024497A1 (en) | 2021-01-28 |
PT3768669T (pt) | 2023-04-24 |
PL3768669T3 (pl) | 2023-07-03 |
WO2019183636A1 (en) | 2019-09-26 |
EP4219464A1 (en) | 2023-08-02 |
JP2021519269A (ja) | 2021-08-10 |
FI3768669T3 (fi) | 2023-04-26 |
JP7497294B2 (ja) | 2024-06-10 |
CA3094366A1 (en) | 2019-09-26 |
EP3768669B1 (en) | 2023-01-25 |
DK3768669T3 (da) | 2023-04-24 |
ES2942837T3 (es) | 2023-06-07 |
CN112154145B (zh) | 2023-10-17 |
EP3768669A1 (en) | 2021-01-27 |
TW202003491A (zh) | 2020-01-16 |
CN112154145A (zh) | 2020-12-29 |
US11524954B2 (en) | 2022-12-13 |
TWI801540B (zh) | 2023-05-11 |
HUE061533T2 (hu) | 2023-07-28 |
US20230192654A1 (en) | 2023-06-22 |
JP2024037979A (ja) | 2024-03-19 |
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