BRPI0510501A - antagonistas do receptor 3 de histamina - Google Patents
antagonistas do receptor 3 de histaminaInfo
- Publication number
- BRPI0510501A BRPI0510501A BRPI0510501-3A BRPI0510501A BRPI0510501A BR PI0510501 A BRPI0510501 A BR PI0510501A BR PI0510501 A BRPI0510501 A BR PI0510501A BR PI0510501 A BRPI0510501 A BR PI0510501A
- Authority
- BR
- Brazil
- Prior art keywords
- disorder
- disease
- compound
- formula
- congestion
- Prior art date
Links
- 102000000543 Histamine Receptors Human genes 0.000 title abstract 2
- 108010002059 Histamine Receptors Proteins 0.000 title abstract 2
- 239000005557 antagonist Substances 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 4
- 238000000034 method Methods 0.000 abstract 4
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 abstract 3
- 208000026935 allergic disease Diseases 0.000 abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 3
- 210000001035 gastrointestinal tract Anatomy 0.000 abstract 3
- 208000036864 Attention deficit/hyperactivity disease Diseases 0.000 abstract 2
- 206010020751 Hypersensitivity Diseases 0.000 abstract 2
- 241000124008 Mammalia Species 0.000 abstract 2
- 230000007815 allergy Effects 0.000 abstract 2
- 208000015802 attention deficit-hyperactivity disease Diseases 0.000 abstract 2
- 208000027744 congestion Diseases 0.000 abstract 2
- 208000035475 disorder Diseases 0.000 abstract 2
- 208000035231 inattentive type attention deficit hyperactivity disease Diseases 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 208000019901 Anxiety disease Diseases 0.000 abstract 1
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- 102000004384 Histamine H3 receptors Human genes 0.000 abstract 1
- 108090000981 Histamine H3 receptors Proteins 0.000 abstract 1
- 208000001953 Hypotension Diseases 0.000 abstract 1
- 208000019022 Mood disease Diseases 0.000 abstract 1
- 206010028735 Nasal congestion Diseases 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 208000028017 Psychotic disease Diseases 0.000 abstract 1
- 208000012886 Vertigo Diseases 0.000 abstract 1
- 230000002378 acidificating effect Effects 0.000 abstract 1
- 230000008369 airway response Effects 0.000 abstract 1
- 230000000172 allergic effect Effects 0.000 abstract 1
- 230000003042 antagnostic effect Effects 0.000 abstract 1
- 208000010668 atopic eczema Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 206010015037 epilepsy Diseases 0.000 abstract 1
- 230000036543 hypotension Effects 0.000 abstract 1
- 201000003152 motion sickness Diseases 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 208000023504 respiratory system disease Diseases 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 201000000980 schizophrenia Diseases 0.000 abstract 1
- 230000028327 secretion Effects 0.000 abstract 1
- 208000019116 sleep disease Diseases 0.000 abstract 1
- 208000020685 sleep-wake disease Diseases 0.000 abstract 1
- 231100000889 vertigo Toxicity 0.000 abstract 1
Classifications
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/36—Radicals substituted by singly-bound nitrogen atoms
- C07D213/38—Radicals substituted by singly-bound nitrogen atoms having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom
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- 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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- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- C07C215/02—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C215/22—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated
- C07C215/28—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing six-membered aromatic rings
- C07C215/30—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing six-membered aromatic rings containing hydroxy groups and carbon atoms of six-membered aromatic rings bound to the same carbon atom of the carbon skeleton
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- C07C233/42—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
- C07C233/43—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of a saturated carbon skeleton
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- C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/37—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
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- C07C317/32—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
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- C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
- C07C323/23—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
- C07C323/31—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton
- C07C323/32—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton having at least one of the nitrogen atoms bound to an acyclic carbon atom of the carbon skeleton
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- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
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- C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
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- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
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- C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D211/26—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
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Abstract
ANTAGONISTAS DO RECEPTOR 3 DE HISTAMINA. A presente invenção refere-se a um composto de fórmula (I), conforme aqui definido ou um sal farmaceuticamente aceitável do mesmo, uma composição farmacêutica contendo um composto de fórmula (I), um método de tratamento de um distúrbio ou uma condição doentia que podem ser tratados através da antagonização dos receptores H3 de histamina, o método compreendendo a administração a um mamífero com necessidade de tal tratamento de um composto de fórmula (I), conforme descrito acima, e um método de tratamento de um distúrbio ou uma condição doentia selecionada do grupo que consiste em depressão, distúrbios do humor, esquizofrenia, distúrbios de ansiedade, doença de Alzheimer, distúrbio por déficit de atenção (ADD), distúrbio de hiperatividade por déficit de atenção (ADHD), distúrbios psicóticos, distúrbios do sono, obesidade, vertigens, epilepsia, doença do movimento, doenças respiratórias, alergia, resposta das vias aéreas induzida por alergia, rinite alérgica, congestão nasal, congestão alérgica, congestão, hipotensão, doença cardiovascular, doenças do trato gastrointestinal (GI), hiper e hipomobilidade e secreção acídica do trato gastrointestinal, o método compreendendo a administração a um mamífero com necessidade de tal tratamento de um composto de fórmula (I), conforme descrito acima.
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| US56684904P | 2004-04-30 | 2004-04-30 | |
| PCT/IB2005/001038 WO2005105744A1 (en) | 2004-04-30 | 2005-04-18 | Histamine-3 receptor antagonists |
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| US20060014733A1 (en) * | 2004-07-19 | 2006-01-19 | Pfizer Inc | Histamine-3 agonists and antagonists |
| WO2007076140A2 (en) * | 2005-12-23 | 2007-07-05 | University Of Cincinnati | Treatment methods employing histamine h3 receptor antagonists, including betahistine |
| US8242148B2 (en) * | 2005-12-23 | 2012-08-14 | Nelson Erik B | Treatment methods employing histamine H3 receptor antagonists, including betahistine |
| US7728031B2 (en) * | 2006-02-24 | 2010-06-01 | Abbott Laboratories | Octahydro-pyrrolo[3,4-b]pyrrole derivatives |
| CN101522614B (zh) | 2006-08-09 | 2014-06-25 | 史密丝克莱恩比彻姆公司 | 作为阿片样物质受体的拮抗剂或反向激动剂的化合物 |
| JP4944122B2 (ja) * | 2006-09-29 | 2012-05-30 | パナソニック株式会社 | 記録装置、記録方法およびコンピュータプログラム |
| TW200823204A (en) * | 2006-10-17 | 2008-06-01 | Arena Pharm Inc | Biphenyl sulfonyl and phenyl-heteroaryl sulfonyl modulators of the histamine H3-receptor useful for the treatment of disorders related thereto |
| JP2010509392A (ja) | 2006-11-13 | 2010-03-25 | ファイザー・プロダクツ・インク | ジアリール、ジピリジニルおよびアリール−ピリジニル誘導体ならびにその使用 |
| WO2009036132A1 (en) * | 2007-09-11 | 2009-03-19 | Abbott Laboratories | Octahydro-pyrrolo[3,4-b]pyrrole n-oxides |
| AU2008319310A1 (en) * | 2007-10-30 | 2009-05-07 | Arena Pharmaceuticals, Inc. | Biphenyl derivatives as modulators of the histamine-H3 receptor useful for the treatment of disorders related thereto |
| US20100113512A1 (en) * | 2008-10-30 | 2010-05-06 | Diane Michele Ignar | Method of treatment using novel antagonists or inverse agonists at opioid receptors |
| PH12013501136A1 (en) | 2010-12-07 | 2013-07-08 | Amira Pharmaceuticals Inc | Lysophosphatidic acid receptor antagonists and uses thereof |
| JP6440625B2 (ja) | 2012-11-14 | 2018-12-19 | ザ・ジョンズ・ホプキンス・ユニバーシティー | 精神分裂病を処置するための方法および組成物 |
| ES2886914T3 (es) * | 2013-01-09 | 2021-12-21 | Arena Pharm Inc | Acido (R)-3-(4'-(2-(2-metilpirrolidin-1-il)etil)-bifenil-4-il)propanoico como moduladores del receptor de histamina H3 para el tratamiento de trastornos cognitivos |
| TWI644899B (zh) | 2013-02-04 | 2018-12-21 | 健生藥品公司 | Flap調節劑 |
| US9079866B2 (en) | 2013-02-04 | 2015-07-14 | Janssen Pharmaceutica Nv | Flap modulators |
| ES2804304T3 (es) | 2013-09-04 | 2021-02-05 | Ellora Therapeutics Inc | Moduladores del receptor X hepático (LXR) |
| CN105646452B (zh) * | 2015-12-24 | 2018-05-01 | 北京康立生医药技术开发有限公司 | 一种蛋白激酶抑制剂的合成方法 |
| CN107011921A (zh) * | 2016-12-19 | 2017-08-04 | 西安近代化学研究所 | 一种氯代氮杂环液晶化合物及其液晶组合物 |
| CN116396243B (zh) * | 2023-04-17 | 2024-10-18 | 贵州民族大学 | 一种芳烃的多氟芳基化的方法 |
| IL311338A (en) * | 2024-03-07 | 2025-10-01 | Ariel Scient Innovations Ltd | Using hyaluronic acid to treat mental disorders |
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|---|---|---|---|---|
| EP0978512A1 (en) * | 1998-07-29 | 2000-02-09 | Societe Civile Bioprojet | Non-imidazole aryloxy (or arylthio) alkylamines as histamine H3-receptor antagonists and their therapeutic applications |
| US6316475B1 (en) * | 2000-11-17 | 2001-11-13 | Abbott Laboratories | Aminoalkoxybiphenylcarboxamides as histamine-3 receptor ligands and their therapeutic applications |
| US6919343B2 (en) * | 2002-02-08 | 2005-07-19 | Merck & Co., Inc. | N-biphenyl(substituted methyl) aminocycloalkane-carboxamide derivatives |
| US20060014733A1 (en) * | 2004-07-19 | 2006-01-19 | Pfizer Inc | Histamine-3 agonists and antagonists |
| BRPI0513444A (pt) * | 2004-07-21 | 2008-05-06 | Pfizer Prod Inc | antagonistas do receptor da histamina 3 |
-
2005
- 2005-04-15 US US11/107,457 patent/US20050245543A1/en not_active Abandoned
- 2005-04-18 WO PCT/IB2005/001038 patent/WO2005105744A1/en not_active Ceased
- 2005-04-18 EP EP05718479A patent/EP1756058A1/en not_active Withdrawn
- 2005-04-18 MX MXPA06012506A patent/MXPA06012506A/es unknown
- 2005-04-18 JP JP2007510141A patent/JP2007535528A/ja active Pending
- 2005-04-18 BR BRPI0510501-3A patent/BRPI0510501A/pt not_active IP Right Cessation
- 2005-04-18 CA CA002564258A patent/CA2564258A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| MXPA06012506A (es) | 2006-12-15 |
| WO2005105744A1 (en) | 2005-11-10 |
| JP2007535528A (ja) | 2007-12-06 |
| CA2564258A1 (en) | 2005-11-10 |
| EP1756058A1 (en) | 2007-02-28 |
| US20050245543A1 (en) | 2005-11-03 |
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