BR112014019426A8 - Prolinas/ piperidinas substituídas como antagonistas do receptor de orexina - Google Patents
Prolinas/ piperidinas substituídas como antagonistas do receptor de orexinaInfo
- Publication number
- BR112014019426A8 BR112014019426A8 BR112014019426A BR112014019426A BR112014019426A8 BR 112014019426 A8 BR112014019426 A8 BR 112014019426A8 BR 112014019426 A BR112014019426 A BR 112014019426A BR 112014019426 A BR112014019426 A BR 112014019426A BR 112014019426 A8 BR112014019426 A8 BR 112014019426A8
- Authority
- BR
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- Prior art keywords
- disorder
- orexin receptor
- disorders
- compounds
- disease
- Prior art date
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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
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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
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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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A—HUMAN NECESSITIES
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- A61P25/08—Antiepileptics; Anticonvulsants
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- A—HUMAN NECESSITIES
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- 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
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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
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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
- C07D413/14—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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- 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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- 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
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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
- C07D417/14—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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Addiction (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Psychology (AREA)
- Endocrinology (AREA)
- Heart & Thoracic Surgery (AREA)
- Child & Adolescent Psychology (AREA)
- Hematology (AREA)
- Anesthesiology (AREA)
- Obesity (AREA)
- Hospice & Palliative Care (AREA)
- Cardiology (AREA)
- Reproductive Health (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
Abstract
PROLINAS/ PIPERIDINAS SUBSTITUÍDAS COMO ANTAGONISTAS DO RECEPTOR DE OREXINA, SEUS USOS E COMPOSIÇÃO FARMACÊUTICA. A presente invenção refere-se a compostos que podem modular a bioatividade de um receptor de orexina tal como OX1 ou OX2, ou ambos; as composições farmacêuticas e combinações compreendendo um composto da invenção; a métodos de tratamento de disfunções em pacientes nas quais a modulação de um receptor de orexina é uma indicação médica; e a métodos de preparação dos compostos da invenção. Por exemplo, os compostos moduladores do receptor de orexina da presente invenção podem ser usados no tratamento de um distúrbio alimentar, obesidade, alcoolismo ou um distúrbio relacionado com álcool, abuso ou adicção a fármacos incluindo adicção à cocaína, opiáceos, anfetaminas, ou nitocina, um distúrbio do sono, uma disfunção cognitiva em um transtorno psiquiátrico ou neurológico, depressão, ansiedade, distúrbio do pânico, esquizofrenia, mal de Alzheimer, mal de Parkinson, coreia de Huntington, cefaleia, enxaqueca, dor, doenças gastrointestinais, epilepsia, inflamações, doenças imunológicas, doenças endócrinas, câncer, hipertensão, distúrbio de comportamento, distúrbio do humor, depressão maníaca, demência, distúrbio sexual, distúrbio psicossexual, ou doença renal.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201261596062P | 2012-02-07 | 2012-02-07 | |
PCT/US2013/024903 WO2013119639A1 (en) | 2012-02-07 | 2013-02-06 | Substituted prolines / piperidines as orexin receptor antagonists |
Publications (2)
Publication Number | Publication Date |
---|---|
BR112014019426A2 BR112014019426A2 (pt) | 2017-06-20 |
BR112014019426A8 true BR112014019426A8 (pt) | 2017-07-11 |
Family
ID=48947950
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR112014019426A BR112014019426A8 (pt) | 2012-02-07 | 2013-02-06 | Prolinas/ piperidinas substituídas como antagonistas do receptor de orexina |
Country Status (18)
Country | Link |
---|---|
US (2) | US9499517B2 (pt) |
EP (1) | EP2811997B1 (pt) |
JP (1) | JP6346862B2 (pt) |
KR (1) | KR20140124398A (pt) |
CN (1) | CN104220065A (pt) |
AR (1) | AR099466A1 (pt) |
AU (1) | AU2013217323A1 (pt) |
BR (1) | BR112014019426A8 (pt) |
CA (1) | CA2863413A1 (pt) |
ES (1) | ES2672732T3 (pt) |
HK (1) | HK1204955A1 (pt) |
IL (1) | IL234025A0 (pt) |
MX (1) | MX2014009281A (pt) |
NZ (1) | NZ628491A (pt) |
PH (1) | PH12014501784A1 (pt) |
RU (1) | RU2014136339A (pt) |
SG (1) | SG11201404738QA (pt) |
WO (1) | WO2013119639A1 (pt) |
Families Citing this family (19)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JO3267B1 (ar) | 2009-10-23 | 2018-09-16 | Janssen Pharmaceutica Nv | بيرولات [3، 4-سي] اوكتاهيدروبيرولو ثنائية الاستبدال كمعدلات لمستقبل اوريكسين |
JP6346862B2 (ja) | 2012-02-07 | 2018-06-20 | エオラス セラピューティクス, インコーポレイテッド | オレキシンレセプターアンタゴニストとしての置換プロリン/ピペリジン |
US9440982B2 (en) | 2012-02-07 | 2016-09-13 | Eolas Therapeutics, Inc. | Substituted prolines/piperidines as orexin receptor antagonists |
ITMI20120322A1 (it) * | 2012-03-01 | 2013-09-02 | Rottapharm Spa | Composti di 4,4-difluoro piperidina |
EP2925321A4 (en) * | 2012-11-27 | 2016-04-27 | Merck Sharp & Dohme | 2-pyridylamino-4-nitrile-piperidinyl orexin receptor antagonists |
WO2015018027A1 (en) * | 2013-08-08 | 2015-02-12 | Merck Sharp & Dohme Corp. | Thiazole orexin receptor antagonists |
JP2017001954A (ja) * | 2013-11-08 | 2017-01-05 | 石原産業株式会社 | 含窒素飽和複素環化合物 |
JP2017024990A (ja) * | 2013-12-13 | 2017-02-02 | 大正製薬株式会社 | オキサゾリジン及びオキサジナン誘導体 |
TW201613891A (en) * | 2014-02-12 | 2016-04-16 | Eolas Therapeutics Inc | Substituted prolines / piperidines as orexin receptor antagonists |
UY36272A (es) | 2014-08-13 | 2016-02-29 | Eolas Therapeutics Inc | Difluoropirrolidinas como moduladores de los receptores de orexinas |
US9611262B2 (en) * | 2014-09-11 | 2017-04-04 | Janssen Pharmaceutica Nv | Substituted 2-azabicycles and their use as orexin receptor modulators |
JP2018016544A (ja) * | 2014-12-03 | 2018-02-01 | 持田製薬株式会社 | 新規ジアザビシクロ[2.2.2]オクタン誘導体 |
CN104557744B (zh) * | 2014-12-23 | 2017-04-12 | 广东东阳光药业有限公司 | 一种三氮唑化合物的制备方法 |
MX2018009656A (es) * | 2016-02-12 | 2019-02-20 | Astrazeneca Ab | Piperidinas halo-sustituidas como moduladores de los receptores de orexinas. |
ES2913469T3 (es) | 2016-03-10 | 2022-06-02 | Janssen Pharmaceutica Nv | Métodos para tratar la depresión usando antagonistas del receptor de orexina-2 |
RU2738646C2 (ru) * | 2016-04-01 | 2020-12-15 | РЕКЬЮРИУМ АйПи ХОЛДИНГС, ЛЛС | Модуляторы эстрогеновых рецепторов |
AU2017264871B2 (en) * | 2016-05-12 | 2023-03-16 | Eisai R&D Management Co., Ltd. | Methods of treating circadian rhythm sleep disorders |
GB2558975B (en) * | 2017-09-01 | 2019-01-23 | Chronos Therapeutics Ltd | Substituted 2-azabicyclo[3.1.1]heptane and 2-azabicyclo[3.2.1]octane derivatives as orexin receptor antagonists |
US11660293B2 (en) | 2017-09-01 | 2023-05-30 | Chronos Therapeutics Limited | Substituted 2-azabicyclo[3.1.1]heptane and 2-azabicyclo[3.2.1]octane derivatives as orexin receptor antagonists |
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CA2331735A1 (en) | 1998-05-08 | 1999-11-18 | Smithkline Beecham P.L.C. | Phenylurea and phenylthio urea derivatives |
WO2000047577A1 (en) | 1999-02-12 | 2000-08-17 | Smithkline Beecham Plc | Phenyl urea and phenyl thiourea derivatives as orexin receptor antagonists |
WO2000047576A1 (en) | 1999-02-12 | 2000-08-17 | Smithkline Beecham Plc | Cinnamide derivatives as orexin-1 receptors antagonists |
DE60015927T2 (de) | 1999-02-12 | 2005-04-07 | Smithkline Beecham P.L.C., Brentford | Phenylharnstoff und phenylthioharnstoffderivate |
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ES2238458T3 (es) * | 2000-06-16 | 2005-09-01 | Smithkline Beecham Plc | Piperidinas para uso como antagonistas de los receptores de orexina. |
AU2002224885A1 (en) | 2000-11-28 | 2002-06-11 | Smithkline Beecham Plc | Morpholine derivatives as antagonists of orexin receptors |
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US20040192673A1 (en) | 2001-05-05 | 2004-09-30 | Pascale Gaillard | N-aroyl cyclic amine derivatives as orexin receptor antagonists |
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GB0115862D0 (en) | 2001-06-28 | 2001-08-22 | Smithkline Beecham Plc | Compounds |
GB0124463D0 (en) | 2001-10-11 | 2001-12-05 | Smithkline Beecham Plc | Compounds |
GB0126292D0 (en) | 2001-11-01 | 2002-01-02 | Smithkline Beecham Plc | Compounds |
GB0127145D0 (en) | 2001-11-10 | 2002-01-02 | Smithkline Beecham | Compounds |
GB0130341D0 (en) | 2001-12-19 | 2002-02-06 | Smithkline Beecham Plc | Compounds |
GB0130335D0 (en) | 2001-12-19 | 2002-02-06 | Smithkline Beecham Plc | Compounds |
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US20170101410A1 (en) | 2017-04-13 |
HK1204955A1 (en) | 2015-12-11 |
SG11201404738QA (en) | 2014-10-30 |
WO2013119639A1 (en) | 2013-08-15 |
CA2863413A1 (en) | 2013-08-15 |
RU2014136339A (ru) | 2016-03-27 |
MX2014009281A (es) | 2015-01-12 |
US9499517B2 (en) | 2016-11-22 |
NZ628491A (en) | 2016-06-24 |
US20140364432A1 (en) | 2014-12-11 |
AU2013217323A1 (en) | 2014-08-28 |
JP6346862B2 (ja) | 2018-06-20 |
US9896452B2 (en) | 2018-02-20 |
EP2811997A4 (en) | 2015-07-22 |
JP2015506382A (ja) | 2015-03-02 |
ES2672732T3 (es) | 2018-06-15 |
KR20140124398A (ko) | 2014-10-24 |
AR099466A1 (es) | 2016-07-27 |
IL234025A0 (en) | 2014-09-30 |
EP2811997A1 (en) | 2014-12-17 |
EP2811997B1 (en) | 2018-04-11 |
CN104220065A (zh) | 2014-12-17 |
BR112014019426A2 (pt) | 2017-06-20 |
PH12014501784A1 (en) | 2014-11-10 |
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