AR104882A1 - DERIVADOS DE 2-(1-HETEROARILPIPERAZIN-4-IL)METIL-1,4-BENZODIOXANO COMO ANTAGONISTAS DE a2C - Google Patents
DERIVADOS DE 2-(1-HETEROARILPIPERAZIN-4-IL)METIL-1,4-BENZODIOXANO COMO ANTAGONISTAS DE a2CInfo
- Publication number
- AR104882A1 AR104882A1 ARP160101636A ARP160101636A AR104882A1 AR 104882 A1 AR104882 A1 AR 104882A1 AR P160101636 A ARP160101636 A AR P160101636A AR P160101636 A ARP160101636 A AR P160101636A AR 104882 A1 AR104882 A1 AR 104882A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- alkoxy
- heterocyclic ring
- substituted
- heterocyclyl
- Prior art date
Links
- 239000005557 antagonist Substances 0.000 title abstract 3
- MJCYUVOCINOVJH-UHFFFAOYSA-N 3-methyl-2,3-dihydro-1,4-benzodioxine Chemical compound C1=CC=C2OC(C)COC2=C1 MJCYUVOCINOVJH-UHFFFAOYSA-N 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 11
- 125000000623 heterocyclic group Chemical group 0.000 abstract 9
- 125000001424 substituent group Chemical group 0.000 abstract 5
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- -1 1,2,3-oxadiazol-3-ium-3-yl Chemical group 0.000 abstract 1
- 208000015114 central nervous system disease Diseases 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 125000004043 oxo group Chemical group O=* 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000006413 ring segment Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- 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
- C07D405/14—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 three or more hetero 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- 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
- A61P25/24—Antidepressants
-
- 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
- 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
- C07D405/12—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 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
- C07D413/02—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
- C07D413/12—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 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
- C07D417/02—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
- 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
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Epidemiology (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
La presente solicitud para compuestos con actividad antagonista de a2C y por lo tanto son útiles como antagonistas de a2C en el tratamiento de enfermedades del SNC. Reivindicación 1: Un compuesto caracterizado porque es de fórmula (1), donde A es un anillo heterocíclico insaturado de cinco miembros que contiene 1, 2 ó 3 heteroátomo/s en el anillo cada uno seleccionado en forma independiente entre N, O y S, donde dicho anillo heterocíclico no está sustituido, o dicho anillo heterocíclico está sustituido con 1 sustituyente R¹, o dicho anillo heterocíclico está sustituido con 2 sustituyentes R¹ y R², o dicho anillo heterocíclico está sustituido con 3 sustituyentes R¹, R², y R³, o dicho anillo heterocíclico está sustituido con 4 sustituyentes R¹, R², R³, y R⁴; R¹ es C₁₋₆ alquilo, C₁₋₆ alcoxi, hidroxi-C₁₋₆ alquilo, C₁₋₆ alcoxi-C₁₋₆ alquilo, C₁₋₆ alcoxi-(C=O)-, CN, C₁₋₆ alquil-(C=O)-, R⁵R⁶N-, R⁵R⁶N-(C=O)-, R⁶(C=O)-R⁵N-, heterociclilo, heterociclil-N-, o fenil-N-, donde dicho heterociclilo o fenilo está opcionalmente sustituido con 1, 2, 3, ó 4 sustituyente/s donde cada uno es en forma independiente C₁₋₆ alquilo, C₁₋₆ alcoxi, oxo, o fenil-C₁₋₆ alcoxi; R² es C₁₋₆ alquilo, C₁₋₆ alcoxi, o C₁₋₆ alcoxi-C₁₋₆ alquilo; R³ es C₁₋₆ alquilo, C₁₋₆ alcoxi, o C₁₋₆ alcoxi-C₁₋₆ alquilo; R⁴ es C₁₋₆ alquilo; R⁵ es H, o C₁₋₆ alquilo; y R⁶ es H, o C₁₋₆ alquilo; o R¹ y R² forman, junto con los átomos del anillo a los cuales están unidos, un anillo heterocíclico insaturado de 6 miembros condensado, que contiene 1 ó 2 heteroátomo(s) que son N; o una sal aceptable farmacéuticamente o éster de los mismos; con la condición de que A no es 1,2,3-oxadiazol-3-ium-3-ilo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FI20150169 | 2015-06-05 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR104882A1 true AR104882A1 (es) | 2017-08-23 |
Family
ID=56132965
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP160101636A AR104882A1 (es) | 2015-06-05 | 2016-06-02 | DERIVADOS DE 2-(1-HETEROARILPIPERAZIN-4-IL)METIL-1,4-BENZODIOXANO COMO ANTAGONISTAS DE a2C |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US10774074B2 (es) |
| EP (1) | EP3303327B1 (es) |
| JP (1) | JP6806711B2 (es) |
| KR (1) | KR102653543B1 (es) |
| CN (1) | CN107709316B (es) |
| AR (1) | AR104882A1 (es) |
| AU (1) | AU2016272220B2 (es) |
| CA (1) | CA2985400C (es) |
| EA (1) | EA033085B1 (es) |
| ES (1) | ES2794584T3 (es) |
| IL (1) | IL255352B (es) |
| MX (1) | MX2017015572A (es) |
| TW (1) | TWI704145B (es) |
| WO (1) | WO2016193551A1 (es) |
| ZA (1) | ZA201707466B (es) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2019519582A (ja) * | 2016-06-29 | 2019-07-11 | オリオン コーポレーション | ベンゾジオキサン誘導体およびその医薬用途 |
| KR20240132345A (ko) | 2022-01-07 | 2024-09-03 | 바이엘 악티엔게젤샤프트 | 수면 무호흡의 치료를 위한 2,3-디히드로벤조[b][1,4]디옥신-2-일메틸)피페라진-1-일 유도체 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BE788052A (fr) * | 1971-08-26 | 1973-02-26 | Science Union & Cie Societe Fr | Nouveaux derives de la sydnone imine |
| US4590196A (en) * | 1984-08-23 | 1986-05-20 | Bristol-Myers Company | Analgesic 1,2-benzisothiazol-3-ylpiperazine derivatives |
| GB2167408B (en) | 1984-11-23 | 1988-05-25 | Farmos Oy | Substituted imidazole derivatives and their preparation and use |
| US5776963A (en) * | 1989-05-19 | 1998-07-07 | Hoechst Marion Roussel, Inc. | 3-(heteroaryl)-1- (2,3-dihydro-1h-isoindol-2-yl)alkyl!pyrrolidines and 3-(heteroaryl)-1- (2,3-dihydro-1h-indol-1-yl)alkyl!pyrrolidines and related compounds and their therapeutic untility |
| TWI242011B (en) * | 1997-03-31 | 2005-10-21 | Eisai Co Ltd | 1,4-substituted cyclic amine derivatives |
| FR2810979B1 (fr) * | 2000-06-29 | 2002-08-23 | Adir | Nouveaux derives de diphenyluree, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| US20040259883A1 (en) | 2001-09-14 | 2004-12-23 | Hiroshi Sakashita | Thiazolidine derivative and medicinal use thereof |
| ATE374773T1 (de) | 2002-04-03 | 2007-10-15 | Orion Corp | Polycyclische verbindungen als potenten alpha2- adrenoceptor antagonisten |
| ES2400339T3 (es) | 2002-07-15 | 2013-04-09 | Symphony Evolution, Inc. | Compuestos, composiciones farmacéuticas de los mismos y su uso en el tratamiento del cáncer |
| US8013156B2 (en) | 2003-03-19 | 2011-09-06 | Exelixis, Inc. | Tie-2 modulators and methods of use |
| TWI457122B (zh) * | 2007-07-20 | 2014-10-21 | Orion Corp | 作為用於治療周邊和中央神經系統疾病之alpha2C拮抗劑的2,3－二氫苯並[1,4]戴奧辛－2－基甲基衍生物 |
| TW201024282A (en) * | 2008-11-20 | 2010-07-01 | Orion Corp | New pharmaceutical compounds |
-
2016
- 2016-06-02 TW TW105117354A patent/TWI704145B/zh active
- 2016-06-02 AR ARP160101636A patent/AR104882A1/es active IP Right Grant
- 2016-06-03 KR KR1020187000343A patent/KR102653543B1/ko active IP Right Grant
- 2016-06-03 EA EA201792670A patent/EA033085B1/ru not_active IP Right Cessation
- 2016-06-03 CN CN201680031775.2A patent/CN107709316B/zh active Active
- 2016-06-03 ES ES16729605T patent/ES2794584T3/es active Active
- 2016-06-03 MX MX2017015572A patent/MX2017015572A/es active IP Right Grant
- 2016-06-03 CA CA2985400A patent/CA2985400C/en active Active
- 2016-06-03 JP JP2017563032A patent/JP6806711B2/ja active Active
- 2016-06-03 US US15/579,372 patent/US10774074B2/en active Active
- 2016-06-03 AU AU2016272220A patent/AU2016272220B2/en active Active
- 2016-06-03 EP EP16729605.2A patent/EP3303327B1/en active Active
- 2016-06-03 WO PCT/FI2016/050400 patent/WO2016193551A1/en active Application Filing
-
2017
- 2017-10-31 IL IL255352A patent/IL255352B/en active IP Right Grant
- 2017-11-03 ZA ZA2017/07466A patent/ZA201707466B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| TW201708208A (zh) | 2017-03-01 |
| CN107709316A (zh) | 2018-02-16 |
| US20180215739A1 (en) | 2018-08-02 |
| NZ737533A (en) | 2024-03-22 |
| IL255352B (en) | 2021-03-25 |
| EA201792670A1 (ru) | 2018-04-30 |
| MX2017015572A (es) | 2018-04-30 |
| EP3303327A1 (en) | 2018-04-11 |
| TWI704145B (zh) | 2020-09-11 |
| JP6806711B2 (ja) | 2021-01-06 |
| CN107709316B (zh) | 2021-08-17 |
| KR102653543B1 (ko) | 2024-04-03 |
| EA033085B1 (ru) | 2019-08-30 |
| CA2985400A1 (en) | 2016-12-08 |
| KR20180011316A (ko) | 2018-01-31 |
| ZA201707466B (en) | 2018-11-28 |
| WO2016193551A1 (en) | 2016-12-08 |
| US10774074B2 (en) | 2020-09-15 |
| AU2016272220A1 (en) | 2017-11-16 |
| JP2018520123A (ja) | 2018-07-26 |
| ES2794584T3 (es) | 2020-11-18 |
| CA2985400C (en) | 2023-08-29 |
| IL255352A0 (en) | 2017-12-31 |
| EP3303327B1 (en) | 2020-03-11 |
| US20190292170A9 (en) | 2019-09-26 |
| AU2016272220B2 (en) | 2020-05-21 |
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Legal Events
| Date | Code | Title | Description |
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| FG | Grant, registration |