AR099640A1 - Derivados de pirrolopiridina o pirazolopiridina - Google Patents
Derivados de pirrolopiridina o pirazolopiridinaInfo
- Publication number
- AR099640A1 AR099640A1 ARP140103205A ARP140103205A AR099640A1 AR 099640 A1 AR099640 A1 AR 099640A1 AR P140103205 A ARP140103205 A AR P140103205A AR P140103205 A ARP140103205 A AR P140103205A AR 099640 A1 AR099640 A1 AR 099640A1
- Authority
- AR
- Argentina
- Prior art keywords
- lower alkyl
- hydroxy
- substituted
- optionally substituted
- halogen
- Prior art date
Links
- 125000000217 alkyl group Chemical group 0.000 abstract 9
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 8
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 102000014415 Muscarinic acetylcholine receptor Human genes 0.000 abstract 2
- 108050003473 Muscarinic acetylcholine receptor Proteins 0.000 abstract 2
- 239000002253 acid Substances 0.000 abstract 2
- -1 cyano, phenyl Chemical group 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- 230000003287 optical effect Effects 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 208000002193 Pain Diseases 0.000 abstract 1
- DHXVGJBLRPWPCS-UHFFFAOYSA-N Tetrahydropyran Chemical group C1CCOCC1 DHXVGJBLRPWPCS-UHFFFAOYSA-N 0.000 abstract 1
- 230000003281 allosteric effect Effects 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 208000010877 cognitive disease Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- CBOIHMRHGLHBPB-UHFFFAOYSA-N hydroxymethyl Chemical compound O[CH2] CBOIHMRHGLHBPB-UHFFFAOYSA-N 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 201000000980 schizophrenia Diseases 0.000 abstract 1
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
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
- A61P25/20—Hypnotics; Sedatives
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Rheumatology (AREA)
- Anesthesiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Epidemiology (AREA)
Abstract
La presente hace referencia a compuestos y a su sal de adición ácida farmacéuticamente aceptable, a una mezcla racémica o a su enantiómero correspondiente y/o los isómeros ópticos de los mismos. Los compuestos son moduladores alostéricos positivos del receptor muscarínico M1 (PAM) y por consiguiente son útiles en el tratamiento de enfermedades mediadas por el receptor muscarínico M1, tales como la enfermedad de Alzheimer, la disfunción cognitiva, la esquizofrenia, el dolor o los trastornos del sueño. Reivindicación 1: Un compuesto con la fórmula (1) en la que R¹ es un halógeno, un alquilo inferior, un alcoxi inferior, ciano, fenilo, C(O)NHCH₃, C(O)NH₂, un alquilo inferior sustituido con un halógeno o sus un grupo heteroarilo de cinco miembros, sustituido de manera opcional con un alquilo inferior; Y¹ es N o CH; Y² es CH; y si Y¹ es CH, Y¹ e Y² pueden formar en conjunto un anillo con, los átomos de C a los que están unidos, e incluyen -CH=N-N(CH₃)-, -CH=N-N(H)-; X es CH o N; R es (CH₂)ₘ-cicloalquilo, sustituido de manera opcional con un hidroxi, un alcoxi inferior o un alquilo inferior, o es tetrahidropirano, sustituido de manera opcional con un hidroxi, o es un alcoxi inferior, sustituido con un hidroxi, o es un alquilo inferior sustituido con uno o dos hidroxi, o es (CH₂)ₘ-piridinilo, sustituido de manera opcional con un hidroxi, un alquilo inferior o un alquilo inferior sustituido con un hidroxi, o es L-fenilo, sustituido de manera opcional con un hidroxi, un alquilo inferior o un alquilo inferior sustituido con un hidroxi, y L es un enlace, -CH(CH₂OH)- o -CH₂CH(OH)-; n es 0, 1 ó 2; m es 0 ó 1; o una sal de adición ácida farmacéuticamente aceptable una mezcla racémica o su enantiómero correspondiente y/o isómeros ópticos de los mismos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13182351 | 2013-08-30 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR099640A1 true AR099640A1 (es) | 2016-08-10 |
Family
ID=49036519
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP140103205A AR099640A1 (es) | 2013-08-30 | 2014-08-27 | Derivados de pirrolopiridina o pirazolopiridina |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US9932335B2 (es) |
| EP (1) | EP3039024A1 (es) |
| JP (1) | JP6434516B2 (es) |
| KR (1) | KR20160035068A (es) |
| CN (2) | CN105358559A (es) |
| AR (1) | AR099640A1 (es) |
| BR (1) | BR112015032637A2 (es) |
| CA (1) | CA2915952A1 (es) |
| HK (1) | HK1215575A1 (es) |
| MX (1) | MX2015017343A (es) |
| RU (1) | RU2016110483A (es) |
| TW (1) | TW201512197A (es) |
| WO (1) | WO2015028483A1 (es) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201317363D0 (en) * | 2013-10-01 | 2013-11-13 | Eisai Ltd | Novel compounds |
| PL3134386T3 (pl) | 2014-04-23 | 2020-11-16 | Takeda Pharmaceutical Company Limited | Pochodne izoindolin-1-onu jako dodatnia aktywność allosterycznego modulatora cholinergicznego receptora muskarynowego m1 do leczenia choroby alzheimera |
| EP3144308B1 (en) | 2014-05-16 | 2020-06-24 | Takeda Pharmaceutical Company Limited | Nitrogen-containing heterocyclic compound |
| ES2719626T3 (es) * | 2015-06-08 | 2019-07-11 | Suven Life Sciences Ltd | Moduladores alostéricos positivos al receptor M1 muscarínico |
| AU2016320645B2 (en) | 2015-09-10 | 2019-02-28 | Suven Life Sciences Limited | Fluoroindole derivatives as muscarinic M1 receptor positive allosteric modulators |
| JP2019504901A (ja) | 2016-02-16 | 2019-02-21 | ヴァンダービルト ユニバーシティー | ムスカリン性アセチルコリン受容体ｍ１のポジティブアロステリックモジュレーター |
| ES2824495T3 (es) * | 2016-09-02 | 2021-05-12 | Suven Life Sciences Ltd | Moduladores alostéricos positivos del receptor muscarínico M1 |
| WO2018063552A1 (en) | 2016-09-30 | 2018-04-05 | Vanderbilt University | Positive allosteric modulators of the muscarinic acetylcholine receptor m1 |
| WO2019000237A1 (en) | 2017-06-27 | 2019-01-03 | Merck Sharp & Dohme Corp. | ALLOSTERIC MODULATORS OF 3- (1H-PYRAZOL-4-YL) PYRIDINE FROM THE M4 ACETYLCHOLINE MUSCARINIC RECEPTOR |
| WO2019000236A1 (en) * | 2017-06-27 | 2019-01-03 | Merck Sharp & Dohme Corp. | ALLOSTERIC MODULATORS OF 3- (1H-PYRAZOL-4-YL) PYRIDINE FROM THE M4 ACETYLCHOLINE MUSCARINIC RECEPTOR |
| WO2019000238A1 (en) | 2017-06-27 | 2019-01-03 | Merck Sharp & Dohme Corp. | 5- (PYRIDIN-3-YL) OXAZOLE ALLOSTERIC MODULATORS OF M4 ACETYLCHOLINE MUSCARINIC RECEPTOR |
| KR102438588B1 (ko) * | 2017-10-18 | 2022-08-31 | 수벤 라이프 사이언시스 리미티드 | 무스카린 m1 수용체 양성 알로스테릭 조절제로서 헤테로아릴 화합물 |
| MA50464A (fr) | 2017-10-27 | 2021-06-02 | Suven Life Sciences Ltd | Amides polycycliques utilisés en tant que modulateurs allostériques positifs du récepteur muscarinique m1 |
| KR20210021042A (ko) * | 2018-06-15 | 2021-02-24 | 카딜라 핼쓰캐어 리미티드 | 포유동물 감염 치료를 위한 신규한 화합물 |
| WO2020086864A1 (en) | 2018-10-24 | 2020-04-30 | Vanderbilt University | Positive allosteric modulators of the muscarinic acetylcholine receptor m1 |
| CN116102549B (zh) * | 2021-11-09 | 2025-02-11 | 暨南大学 | 5-醛基杂环酰胺类化合物及其应用 |
| WO2023082044A1 (zh) * | 2021-11-09 | 2023-05-19 | 暨南大学 | 5-醛基杂环酰胺类化合物及其应用 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5461067A (en) * | 1993-02-25 | 1995-10-24 | Abbott Laboratories | Retroviral protease inhibiting compounds |
| US8012992B2 (en) * | 2008-06-30 | 2011-09-06 | Allergan, Inc. | Aza-indoles and related compounds having sphingosine-1-phosphate (S1P) receptor antagonist biological activity |
| WO2010019391A1 (en) * | 2008-08-12 | 2010-02-18 | Merck Sharp & Dohme Corp. | N-heterocyclic m1 receptor positive allosteric modulators |
| EP2483275B1 (en) * | 2009-10-01 | 2014-10-15 | Merck Sharp & Dohme Corp. | HETEROCYCLIC-FUSED PYRAZOLO[4,3-c]PYRIDIN-3-ONE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS |
| EP2512243B1 (en) * | 2009-12-17 | 2016-04-06 | Merck Sharp & Dohme Corp. | Quinoline amide m1 receptor positive allosteric modulators |
| US8883850B2 (en) * | 2010-05-28 | 2014-11-11 | Merck Sharp & Dohme Corp. | Naphthalene carboxamide M1 receptor positive allosteric modulators |
| US9012445B2 (en) * | 2012-01-12 | 2015-04-21 | Vanderbilt University | Substituted 4-(1H-pyrazol-4-yl)benzyl analogues as positive allosteric modulators of mAChR M1 receptors |
| CN105636646B (zh) * | 2013-07-17 | 2017-12-19 | 全球结核病药物研发联盟 | 氮杂吲哚化合物、其合成及其使用方法 |
-
2014
- 2014-08-26 TW TW103129408A patent/TW201512197A/zh unknown
- 2014-08-27 EP EP14755820.9A patent/EP3039024A1/en not_active Withdrawn
- 2014-08-27 RU RU2016110483A patent/RU2016110483A/ru unknown
- 2014-08-27 KR KR1020167005141A patent/KR20160035068A/ko not_active Abandoned
- 2014-08-27 AR ARP140103205A patent/AR099640A1/es unknown
- 2014-08-27 WO PCT/EP2014/068114 patent/WO2015028483A1/en not_active Ceased
- 2014-08-27 MX MX2015017343A patent/MX2015017343A/es unknown
- 2014-08-27 BR BR112015032637A patent/BR112015032637A2/pt not_active Application Discontinuation
- 2014-08-27 HK HK16103515.2A patent/HK1215575A1/zh unknown
- 2014-08-27 CN CN201480038043.7A patent/CN105358559A/zh active Pending
- 2014-08-27 CA CA2915952A patent/CA2915952A1/en not_active Abandoned
- 2014-08-27 CN CN201810375657.4A patent/CN108558867A/zh active Pending
- 2014-08-27 JP JP2016537274A patent/JP6434516B2/ja not_active Expired - Fee Related
-
2016
- 2016-03-11 US US15/068,096 patent/US9932335B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| HK1215575A1 (zh) | 2016-09-02 |
| JP2016529268A (ja) | 2016-09-23 |
| WO2015028483A1 (en) | 2015-03-05 |
| BR112015032637A2 (pt) | 2017-07-25 |
| US9932335B2 (en) | 2018-04-03 |
| KR20160035068A (ko) | 2016-03-30 |
| MX2015017343A (es) | 2016-04-06 |
| CA2915952A1 (en) | 2015-03-05 |
| CN108558867A (zh) | 2018-09-21 |
| EP3039024A1 (en) | 2016-07-06 |
| RU2016110483A (ru) | 2017-10-04 |
| CN105358559A (zh) | 2016-02-24 |
| TW201512197A (zh) | 2015-04-01 |
| US20160194321A1 (en) | 2016-07-07 |
| JP6434516B2 (ja) | 2018-12-05 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |