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BR112016024149A2 - derivados de indolin-2-ona e 1,3-di-hidro-pirrol[3,2-c]piridin-2-ona - Google Patents

derivados de indolin-2-ona e 1,3-di-hidro-pirrol[3,2-c]piridin-2-ona

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Publication number
BR112016024149A2
BR112016024149A2 BR112016024149A BR112016024149A BR112016024149A2 BR 112016024149 A2 BR112016024149 A2 BR 112016024149A2 BR 112016024149 A BR112016024149 A BR 112016024149A BR 112016024149 A BR112016024149 A BR 112016024149A BR 112016024149 A2 BR112016024149 A2 BR 112016024149A2
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BR
Brazil
Prior art keywords
lower alkyl
disorders
hydrogen
pyridinyl
pyrimidinyl
Prior art date
Application number
BR112016024149A
Other languages
English (en)
Inventor
Limberg Anja
Hilpert Hans
Kolczewski Sabine
Stoll Theodor
Original Assignee
Hoffmann La Roche
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Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of BR112016024149A2 publication Critical patent/BR112016024149A2/pt

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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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • 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
    • A61K31/4427—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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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
    • A61K31/435—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
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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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
    • A61K31/495—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
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    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond
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    • 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
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    • 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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  • Chemical & Material Sciences (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

a presente invenção refere-se a derivados de indolin-2-ona e 1,3-di-hidro-pirrol[3,2-c]piridin-2-ona de fórmula geral i onde ar1 é fenila, piridinila ou pirimidinila; ar2 é um grupo heteroarila de 5 ou 6 membros contendo 2 ou 3 heteroátomos selecio-nados de n, o ou s; r1 é hidrogênio, alquila inferior, halogênio ou alcóxi inferior; r2 é hidrogênio ou alquila inferior; r3 é hidrogênio, alquila inferior, alquila inferior substituída por hidróxi, cicloalquila, oxetan-3-ila, piridinila, imidazolila, pirazolila, pirimidinila, cujos anéis podem opcional-mente ser substituídos por alquila inferior, ou é ?(ch2)3-s(o)2-ciclopropila; x é ch ou n; n é 1 ou 2; bem como com um sal farmaceuticamente aceitável destes, com uma mistura racêmica, ou com seu enantiômero e/ou isômero ótico e/ou estereoisômero, para uso no tratamento de certos distúrbios do sistema nervoso central que são sintomas positivos (psicose) e negativos de esquizofrenia, abuso de substância, depedência de álcool e fármaco, distúrbios obsessivo-compulsivos, comprometimento cognitivo, distúrbios bipolares, distúrbios de humor, depressão maior, depressão resistente ao tratamento, distúrbios de ansiedade, doença de alzheimer, autismo, doença de parkinson, dor crônica, transtorno de personalidade bordeline, distúrbios do sono, síndrome da fadiga crônica, endurecimento, efeitos anti-inflamatórios em artrite e problemas de equilíbrio.
BR112016024149A 2014-05-22 2015-05-19 derivados de indolin-2-ona e 1,3-di-hidro-pirrol[3,2-c]piridin-2-ona BR112016024149A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP14169477 2014-05-22
PCT/EP2015/060937 WO2015177110A1 (en) 2014-05-22 2015-05-19 INDOLIN-2-ONE AND 1,3-DIHYDRO-PYRROLO[3,2-c]PYRIDIN-2-ONE DERIVATIVES

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BR112016024149A2 true BR112016024149A2 (pt) 2017-08-15

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US (2) US10112938B2 (pt)
EP (1) EP3145923B1 (pt)
JP (1) JP6445588B2 (pt)
KR (1) KR101898364B1 (pt)
CN (1) CN106232600B (pt)
AR (1) AR100532A1 (pt)
BR (1) BR112016024149A2 (pt)
CA (1) CA2943882A1 (pt)
MX (1) MX374574B (pt)
RU (1) RU2697512C2 (pt)
TW (1) TWI571463B (pt)
WO (1) WO2015177110A1 (pt)

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JP6857651B2 (ja) * 2015-11-06 2021-04-14 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ Ｃｎｓ疾患の処置に有用なインドリン−２−オン誘導体
SMT202200396T1 (it) 2017-12-13 2022-11-18 Lupin Ltd Composti eterociclici biciclici sostituiti come inibitori di prmt5

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US4721721A (en) * 1984-12-18 1988-01-26 Rorer Pharmaceutical Corporation 6-(4-thiazole) compounds, cardiotonic compositions including the same, and their uses
DE3935514A1 (de) * 1989-10-25 1991-05-02 Boehringer Mannheim Gmbh Neue bicyclo-imidazole, verfahren zu ihrer herstellung und diese verbindungen enthaltende arzneimittel
FR2780973B1 (fr) 1998-07-09 2001-10-05 Hoechst Marion Roussel Inc Procede de preparation du 4-(3-pyridinyl)-1h-imidazole, et les intermediaires mis en oeuvre
PL365441A1 (en) * 2001-04-05 2005-01-10 Torrent Pharmaceuticals Ltd. Heterocyclic compounds for aging-related and diabetic vascular complications
WO2008046083A2 (en) 2006-10-12 2008-04-17 Xenon Pharmaceuticals Inc. Use of oxindole compounds as therapeutic agents
EP2108641A1 (en) 2008-04-11 2009-10-14 Laboratorios Almirall, S.A. New substituted spiro[cycloalkyl-1,3'-indo]-2'(1'H)-one derivatives and their use as p38 mitogen-activated kinase inhibitors
GB201106817D0 (en) 2011-04-21 2011-06-01 Astex Therapeutics Ltd New compound
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CN104619701B (zh) * 2012-09-13 2016-10-19 霍夫曼-拉罗奇有限公司 用于治疗cns疾病的2-氧代-2，3-二氢-吲哚类化合物
EP3010914B1 (en) * 2013-06-19 2017-04-26 F. Hoffmann-La Roche AG Indolin-2-one or pyrrolo-pyridin/pyrimidin-2-one derivatives

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CA2943882A1 (en) 2015-11-26
EP3145923B1 (en) 2019-01-30
RU2016148902A3 (pt) 2018-12-13
US20190016719A1 (en) 2019-01-17
CN106232600A (zh) 2016-12-14
TW201607942A (zh) 2016-03-01
CN106232600B (zh) 2019-05-14
US10385050B2 (en) 2019-08-20
US20170057960A1 (en) 2017-03-02
EP3145923A1 (en) 2017-03-29
TWI571463B (zh) 2017-02-21
AR100532A1 (es) 2016-10-12
JP6445588B2 (ja) 2018-12-26
US10112938B2 (en) 2018-10-30
KR20160144493A (ko) 2016-12-16
KR101898364B1 (ko) 2018-09-12
MX2016014845A (es) 2017-02-28
MX374574B (es) 2025-03-06
RU2016148902A (ru) 2018-06-26
WO2015177110A1 (en) 2015-11-26
RU2697512C2 (ru) 2019-08-15
JP2017514870A (ja) 2017-06-08

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