AR079840A2 - Receptor nicotinico de acetilcolina, subtipo selectivo de amidas de diazabicicloalcanos - Google Patents
Receptor nicotinico de acetilcolina, subtipo selectivo de amidas de diazabicicloalcanosInfo
- Publication number
- AR079840A2 AR079840A2 ARP110100026A ARP110100026A AR079840A2 AR 079840 A2 AR079840 A2 AR 079840A2 AR P110100026 A ARP110100026 A AR P110100026A AR P110100026 A ARP110100026 A AR P110100026A AR 079840 A2 AR079840 A2 AR 079840A2
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- substituted
- aryl
- heteroaryl
- compounds
- Prior art date
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Classifications
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- 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
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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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- 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
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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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
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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
- A61P25/18—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
- A61P25/26—Psychostimulants, e.g. nicotine, cocaine
-
- 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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- 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
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- 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
-
- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- 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
- C07D471/08—Bridged systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Psychology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Se revelan compuestos, composiciones farmacéuticas que incluyen los compuestos y métodos de preparacion y el uso de los mismos. Los compuestos son compuestos amida que pueden prepararse desde ciertos ácidos carboxílicos heteroarilos y ciertos diazabicicloalcanos. Los compuestos exhiben selectividad para los receptores nicotínicos neuronales del subtipo alfa4beta2 en el sistema nervioso central (SNC) y se unen con alta afinidad. Los compuestos y composiciones pueden ser utilizados para tratar y/o prevenir una gran variedad de males y enfermedades, particularmente del Sistema Nervioso Central. Los compuestos pueden: (i) alterar el numero de receptores colinérgicos nicotínicos del cerebro del paciente, (ii) exhibir efectos neuroprotectores, y (iii) cuando se utilizan en cantidades efectivas, no dan como resultado efectos colaterales adversos (por ejemplo, efectos colaterales como presion sanguínea y frecuencia cardiaca, efectos negativos importantes en el tracto gastrointestinal y efectos importantes en el musculo oseo). Reivindicacion 1: Un compuesto representado por formula (1) caracterizado porque n tiene el valor de 0 o 1, y Cy es un grupo heteroarilo elegido del grupo de 2-furanilo, 3-furanilo, 2-oxazolilo, 4-oxazolilo, 5-oxazolilo, 3-isoxazolilo, 4-isoxazolilo, 5-isoxazolilo, 1,3,4-oxadiazol-2-ilo, 1,2,4-oxadiazol-3-ilo, 1,2,4-oxadiazol-5-ilo, 2-tiazolilo, 4-tiazolilo, 5-tiazolilo, 3-isotiazolilo, 4-isotiazolilo, 5-isotiazolilo, 1,3,4-tiadiazol-2-ilo, 1,2,4-tiadiazol-3-ilo, 1,2,4-tiadiazol-5-ilo y 4-piridinilo, cuyos grupos heteroarilo son sustituidos opcionalmente con hasta tres sustituyentes no hidrogeno independientemente seleccionados de alquilo C1-6, alquilo C1-6 sustituido, alquenilo C2-6, alquenilo C2-6 sustituido, alquinilo C2-6, alquinilo C2-6 sustituido, heterociclilo de 3 a 8 miembros, heterociclilo de 3 a 8 miembros sustituido, cicloalquilo C3-8, cicloalquilo C3-8 sustituido, arilo C5-10, heteroarilo de 5 a 10 miembros, arilo C5-10 sustituido, heteroarilo de 5 a 10 miembros sustituido, alquilo C1-6-arilo C5-10, alquil C1-6-heteroarilo de 5 a 10 miembros, alquilo C1-6-arilo C5-10 sustituido, alquilo C1-6-heteroarilo de 5 a 10 miembros sustituido, arilo C5-10-alquilo C1-6, heteroarilo de 5 a 10 miembros-alquilo C1-6, arilo C5-10-alquilo C1-6 sustituido, heteroarilo de 5 a 10 miembros-alquilo C1-6 sustituido, halo, -OR', -NR'Rö, -CF3, -CN, -NO2, -C2R', -SR', -N3, -C(=O)NR'Rö, -NR'C(=O)Rö, -C(=O)R', -C(=O)OR', -OC(=O)R', -OC(=O)NR'Rö, -NR'C(=O)ORö, -SO2R', -SO2NR'Rö, y -NR'SO2Rö, donde R' y Rö se seleccionan independientemente del hidrogeno, alquilo C1-6, cicloalquilo C3-8, heterociclilo de 3 a 8 miembros, arilo C5-10, heteroarilo de 5 a 10 miembros y arilo C5-10-alquilo C1-6, o R' y Rö junto con los átomos a los cuales se unen pueden formar un anillo heterocíclico de 3 a 8 miembros, en donde el término ôsustituidoö aplicado a alquilo, alquenilo, alquinilo, heterociclilo, cicloalquilo, arilo, heteroarilo, alquilarilo, alquilheteroarilo, arilalquilo y heteroarilalquilo, se refiere a una sustitucion por uno o mas grupos alquilo, arilo, heteroarilo, halo, -OR' y -NR'Rö, o sales farmacéuticamente aceptables de los mismos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US85607906P | 2006-11-02 | 2006-11-02 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR079840A2 true AR079840A2 (es) | 2012-02-22 |
Family
ID=39233054
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP070104876A AR063451A1 (es) | 2006-11-02 | 2007-11-01 | Diazabiciclo alcanos como receptores nicotinicos de acetilcolina. composiciones farmaceuticas. |
| ARP110100026A AR079840A2 (es) | 2006-11-02 | 2011-01-05 | Receptor nicotinico de acetilcolina, subtipo selectivo de amidas de diazabicicloalcanos |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP070104876A AR063451A1 (es) | 2006-11-02 | 2007-11-01 | Diazabiciclo alcanos como receptores nicotinicos de acetilcolina. composiciones farmaceuticas. |
Country Status (33)
| Country | Link |
|---|---|
| US (6) | US8114889B2 (es) |
| EP (2) | EP2094703B1 (es) |
| JP (2) | JP5539723B2 (es) |
| KR (2) | KR20100124356A (es) |
| CN (4) | CN102942569B (es) |
| AR (2) | AR063451A1 (es) |
| AT (2) | ATE545646T1 (es) |
| AU (2) | AU2007317433B2 (es) |
| BR (2) | BRPI0722387A2 (es) |
| CA (1) | CA2663925C (es) |
| CL (1) | CL2007003155A1 (es) |
| CO (1) | CO6180435A2 (es) |
| CY (1) | CY1112374T1 (es) |
| DK (1) | DK2094703T3 (es) |
| ES (2) | ES2395157T3 (es) |
| HK (2) | HK1133260A1 (es) |
| HR (1) | HRP20110570T1 (es) |
| IL (2) | IL197618A (es) |
| MX (1) | MX2009004801A (es) |
| MY (2) | MY156730A (es) |
| NO (1) | NO20091251L (es) |
| NZ (2) | NZ575557A (es) |
| PE (2) | PE20110671A1 (es) |
| PL (1) | PL2094703T3 (es) |
| PT (1) | PT2094703E (es) |
| RS (1) | RS51834B (es) |
| RU (2) | RU2448969C2 (es) |
| SA (1) | SA07280584B1 (es) |
| SI (1) | SI2094703T1 (es) |
| TW (3) | TWI454262B (es) |
| UA (2) | UA106718C2 (es) |
| UY (1) | UY30686A1 (es) |
| WO (1) | WO2008057938A1 (es) |
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| TWI454262B (zh) * | 2006-11-02 | 2014-10-01 | Targacept Inc | 菸鹼乙醯膽鹼受體亞型選擇性之二氮雜雙環烷類醯胺 |
| RU2010140613A (ru) * | 2008-03-05 | 2012-04-10 | Таргасепт, Инк. (Us) | Амиды диазабициклоалканов, селективные в отношении подтипа никотиновых ацетилхолиновых рецепторов |
| WO2009113950A1 (en) * | 2008-03-10 | 2009-09-17 | Astrazeneca Ab | Therapeutic combinations of (a) an antipsychotic and (b) an alpha-4/beta-2 (a4b2)-neuronal nicotinic receptor agonist |
| US8536169B2 (en) | 2008-06-05 | 2013-09-17 | Glaxo Group Limited | Compounds |
| ES2445199T3 (es) | 2008-06-05 | 2014-02-28 | Glaxo Group Limited | Derivados de benzpirazol como inhibidores de PI3-quinasas |
| WO2009147190A1 (en) | 2008-06-05 | 2009-12-10 | Glaxo Group Limited | Novel compounds |
| WO2010028011A1 (en) * | 2008-09-05 | 2010-03-11 | Targacept, Inc. | Amides of diazabicyclononanes and uses thereof |
| EP2344496A1 (en) * | 2008-09-05 | 2011-07-20 | Targacept Inc. | Amides of diazabicyclooctanes and uses thereof |
| WO2010080757A2 (en) | 2009-01-07 | 2010-07-15 | Astrazeneca Ab | Combinations with an alpha-4beta-2 nicotinic agonist |
| ES2542551T3 (es) | 2009-03-09 | 2015-08-06 | Glaxo Group Limited | 4-Oxadiazol-2-il-indazoles como inhibidores de PI3 cinasas |
| SI2899191T1 (sl) | 2009-04-30 | 2017-11-30 | Glaxo Group Limited | Z oksazolom substituirani indazoli kot PI3-kinazni inhibitorji |
| RU2417082C2 (ru) * | 2009-07-14 | 2011-04-27 | Учреждение Российской Академии Наук Институт Физиологически Активных Веществ Ран (Ифав Ран) | Средство для восстановления утраченной памяти в норме и патологии у пациентов всех возрастных групп на основе n, n'-замещенных 3, 7-диазабицикло[3.3.1]нонанов, фармацевтическая композиция на его основе и способ ее применения |
| HUE033352T2 (en) | 2009-11-18 | 2017-11-28 | Suven Life Sciences Ltd | Bicyclic compounds as alpha4-beta2 nicotinic acetylcholine receptor ligands |
| KR101410903B1 (ko) | 2009-12-29 | 2014-06-23 | 수벤 라이프 사이언시스 리미티드 | α４β２ 신경 니코틴성 아세틸콜린 수용체 리간드 |
| GB201018124D0 (en) | 2010-10-27 | 2010-12-08 | Glaxo Group Ltd | Polymorphs and salts |
| AR095079A1 (es) | 2013-03-12 | 2015-09-16 | Hoffmann La Roche | Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo |
| UA118201C2 (uk) | 2013-11-26 | 2018-12-10 | Ф. Хоффманн-Ля Рош Аг | НОВИЙ ОКТАГІДРОЦИКЛОБУТА[1,2-c;3,4-c']ДИПІРОЛ-2-ІЛ |
| EA037928B1 (ru) | 2014-03-26 | 2021-06-08 | Ф. Хоффманн-Ля Рош Аг | Бициклические соединения в качестве ингибиторов продукции аутотаксина (atx) и лизофосфатидиловой кислоты (lpa) |
| SG10202011669PA (en) | 2014-10-20 | 2020-12-30 | Oyster Point Pharma Inc | Methods of treating ocular conditions |
| MX2020004504A (es) | 2015-09-04 | 2021-11-10 | Hoffmann La Roche | Derivados de fenoximetilo. |
| MA42918A (fr) | 2015-09-24 | 2018-08-01 | Hoffmann La Roche | Composés bicycliques utilisés en tant qu'inhibiteurs d'atx |
| MA42919A (fr) | 2015-09-24 | 2018-08-01 | Hoffmann La Roche | Composés bicycliques utilisés en tant qu'inhibiteurs d'atx |
| EP3353181B1 (en) | 2015-09-24 | 2021-08-11 | F. Hoffmann-La Roche AG | Bicyclic compounds as dual atx/ca inhibitors |
| PE20180552A1 (es) | 2015-09-24 | 2018-04-02 | Hoffmann La Roche | Nuevos compuestos biciclicos como inhibidores duales de atx/ca |
| KR102485299B1 (ko) | 2016-04-07 | 2023-01-06 | 오이스터 포인트 파마 인코포레이티드 | 안구 장애의 치료 방법 |
| EP3596060B1 (en) | 2017-03-16 | 2023-09-20 | F. Hoffmann-La Roche AG | New bicyclic compounds as atx inhibitors |
| RU2019132254A (ru) | 2017-03-16 | 2021-04-16 | Ф. Хоффманн-Ля Рош Аг | Гетероциклические соединения, пригодные в качестве дуальных ингибиторов atx/ca |
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| BR112021005188A2 (pt) | 2018-09-19 | 2021-06-08 | Forma Therapeutics, Inc. | tratamento de anemia falciforme com um composto de ativação de piruvato cinase r |
| JP7450610B2 (ja) | 2018-09-19 | 2024-03-15 | ノヴォ・ノルディスク・ヘルス・ケア・アーゲー | ピルビン酸キナーゼｒの活性化 |
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