BR112014015832A8 - derivados heterocíclicos como receptores associados com aminas vistigiais (taars) - Google Patents

derivados heterocíclicos como receptores associados com aminas vistigiais (taars)

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Publication number
BR112014015832A8
BR112014015832A8 BR112014015832A BR112014015832A BR112014015832A8 BR 112014015832 A8 BR112014015832 A8 BR 112014015832A8 BR 112014015832 A BR112014015832 A BR 112014015832A BR 112014015832 A BR112014015832 A BR 112014015832A BR 112014015832 A8 BR112014015832 A8 BR 112014015832A8
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Brazil
Prior art keywords
halogen
disorders
hydrogen
formula
optionally substituted
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BR112014015832A
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English (en)
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BR112014015832A2 (pt
Inventor
Goergler Annick
Galley Guido
Pflieger Philippe
Norcross Roger
Original Assignee
Hoffmann La Roche
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Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of BR112014015832A2 publication Critical patent/BR112014015832A2/pt
Publication of BR112014015832A8 publication Critical patent/BR112014015832A8/pt

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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
    • C07D413/02—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
    • C07D413/10—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 carbon chain containing aromatic 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • 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
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    • 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
    • A61P25/22—Anxiolytics
    • 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
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • 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
    • 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
    • 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

Abstract

resumo patente de invenção: "derivados heterocíclicos como receptores associados com aminas vistigiais (taars)". a presente invenção refere-se aos compostos da fórmula i, em que r1 é um grupo heteroarila de um ou dois membros, selecionado do grupo que consiste na fórmula (a), (b), (c), (d), (e), (f), (g), (h), (i) ou (j); r2 é hidrogênio ou halogênio; ou r1 e r2 podem formar junto com os átomos de carbono aos quais estão ligados os seguintes anéis da fórmula (k), (l), (m), (n) ou (o); r3 é hidrogênio, halogênio ou alquila inferior; n é 1 ou 2; r4 é fenila, opcionalmente substituída por um ou dois substituintes, selecionados de halogênio ou ciano, ou é piridinila, opcionalmente substituída por halogênio, ou é tetra-hidropirano, ou é -nh-c(o)-fenila, opcionalmente substituída por halogênio; r5 é hidrogênio ou halogênio; r6 - r13 são fenila, opcionalmente substituída por halogênio; r14 é -nh-c(o)-fenila, substituída por halogênio; r15 é hidrogênio, alquila inferior substituída por halogênio ou é halogênio; r16 é hidrogênio ou alcóxi inferior; r17 é piridinila, opcionalmente substituída por alcóxi inferior ou alquila inferior substituída por halogênio; ou a um sal farmaceuticamente de adição de ácido adequado dos mesmos, a todas as misturas racêmicas, a todos seus enantiômeros e/ou isômeros ópticos correspondentes e a todas formas tautoméricas dos compostos da fórmula i. os compostos da fórmula i têm uma afinidade boa pelos receptores associados a aminas vistigiais (taars), especialmente para taar1. os compostos podem ser usados para o tratamento de depressão, distúrbios de ansiedade, distúrbio bipolar, distúrbio de déficit de atenção-hiperatividade (adhd), distúrbios relacionados ao estresse, distúrbios psicóticos tais como esquizofrenia, doenças neurológicas tais como doença de parkinson, distúrbios neurodegenerativos tais como doença de alzheimer, epilepsia, enxaqueca, hipertensão, abuso de substância e distúrbios metabólicos tais como distúrbios alimentares, diabetes, complicações diabéticas, obesidade, dislipidemia, distúrbios de consumo e assimilação de energia, distúrbios e mau funcionamento da homeóstase da temperatura corporal, distúrbios do sono e ritmo circadiano, e distúrbios cardiovasculares.
BR112014015832A 2012-01-12 2013-01-08 derivados heterocíclicos como receptores associados com aminas vistigiais (taars) BR112014015832A8 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP12150876 2012-01-12
PCT/EP2013/050170 WO2013104591A1 (en) 2012-01-12 2013-01-08 Heterocyclic derivatives as trace amine associated receptors (taars)

Publications (2)

Publication Number Publication Date
BR112014015832A2 BR112014015832A2 (pt) 2017-06-13
BR112014015832A8 true BR112014015832A8 (pt) 2017-07-04

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
BR112014015832A BR112014015832A8 (pt) 2012-01-12 2013-01-08 derivados heterocíclicos como receptores associados com aminas vistigiais (taars)

Country Status (14)

Country Link
US (1) US9181230B2 (pt)
EP (1) EP2802578B1 (pt)
JP (1) JP5872069B2 (pt)
KR (1) KR101631003B1 (pt)
CN (1) CN104024250B (pt)
AR (1) AR089691A1 (pt)
BR (1) BR112014015832A8 (pt)
CA (1) CA2856204A1 (pt)
ES (1) ES2554843T3 (pt)
HK (1) HK1196357A1 (pt)
MX (1) MX354815B (pt)
RU (1) RU2621050C2 (pt)
TW (1) TW201332998A (pt)
WO (1) WO2013104591A1 (pt)

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TWI652014B (zh) 2013-09-13 2019-03-01 美商艾佛艾姆希公司 雜環取代之雙環唑殺蟲劑
JP2015131783A (ja) * 2014-01-14 2015-07-23 株式会社日本ファインケム アリール−１，２，４−トリアゾール誘導体の製造方法
JP2019514960A (ja) * 2016-05-04 2019-06-06 パーデュー ファーマ エルピー オキサゾリンシュードダイマー、医薬組成物及びその使用
KR102161787B1 (ko) * 2018-07-02 2020-10-06 한국기초과학지원연구원 수면 장애의 예방 또는 치료용 약학적 조성물
WO2023033680A1 (en) 2021-09-01 2023-03-09 Limited Liability Company «Excellena Research And Development» (Llc «Excellena») Substituted 2,3,4,5-tetrahydrobenzo[ f][1,4]oxazepines as modulators of trace amine-associated receptor 1 (taar1)
WO2023033681A1 (en) 2021-09-01 2023-03-09 Limited Liability Company «Excellena Research And Development» (Llc «Excellena») Substituted 2-(5-aryl-4 h-1,2,4-triazol-3-yl)ethanamines as modulators of trace amine-associated receptor 1 (taar1)
WO2023033679A1 (en) 2021-09-01 2023-03-09 Limited Liability Company «Excellena Research And Development» (Llc «Excellena») (azacycloalkyl)methoxy-substituted benzamides as modulators of trace amine-associated receptor 1 (taar1)
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Also Published As

Publication number Publication date
US9181230B2 (en) 2015-11-10
CN104024250B (zh) 2016-01-27
US20150045359A1 (en) 2015-02-12
RU2621050C2 (ru) 2017-05-31
JP5872069B2 (ja) 2016-03-01
AR089691A1 (es) 2014-09-10
ES2554843T3 (es) 2015-12-23
MX354815B (es) 2018-03-22
CN104024250A (zh) 2014-09-03
KR101631003B1 (ko) 2016-06-15
JP2015503600A (ja) 2015-02-02
WO2013104591A1 (en) 2013-07-18
CA2856204A1 (en) 2013-07-18
RU2014132044A (ru) 2016-03-10
KR20140116920A (ko) 2014-10-06
MX2014008402A (es) 2014-08-22
BR112014015832A2 (pt) 2017-06-13
HK1196357A1 (zh) 2014-12-12
TW201332998A (zh) 2013-08-16
EP2802578B1 (en) 2015-10-07
EP2802578A1 (en) 2014-11-19

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