BR112014011173A2 - carboxamidas heterocíclicas úteis como inibidores de fosfodiesterase tipo 10a - Google Patents

carboxamidas heterocíclicas úteis como inibidores de fosfodiesterase tipo 10a

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Publication number
BR112014011173A2
BR112014011173A2 BR112014011173A BR112014011173A BR112014011173A2 BR 112014011173 A2 BR112014011173 A2 BR 112014011173A2 BR 112014011173 A BR112014011173 A BR 112014011173A BR 112014011173 A BR112014011173 A BR 112014011173A BR 112014011173 A2 BR112014011173 A2 BR 112014011173A2
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Brazil
Prior art keywords
alkyl
cycloalkyl
disorders
fluoroalkyl
inter alia
Prior art date
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BR112014011173A
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English (en)
Inventor
Jakob Clarissa
Geneste Hervé
Dinges Jürgen
Drescher Karla
Ochse Michael
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Abbvie Deutschland
Abbvie Inc
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Application filed by Abbvie Deutschland, Abbvie Inc filed Critical Abbvie Deutschland
Publication of BR112014011173A2 publication Critical patent/BR112014011173A2/pt

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
    • C07D217/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • 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
    • A61P25/18—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
    • A61P25/22—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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
    • C07D217/24—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
    • C07D237/30—Phthalazines
    • C07D237/32—Phthalazines with oxygen atoms directly attached to carbon atoms of the nitrogen-containing ring
    • 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
    • C07D401/02—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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D401/02—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/08—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing alicyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D413/06—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 only aliphatic carbon atoms
    • 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
    • C07D417/06—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
    • 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
    • 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

resumo “carboxamidas heterocíclicas úteis como inibidores de fosfodiesterase tipo 10ª” a presente invenção refere-se a compostos que são inibidores da fosfodiesterase tipo 10a e a seu uso para a fabricação de um medicamento e que, portanto, são adequados para o tratamento ou controle de distúrbios médicos selecionados a partir de distúrbios neurológicos e distúrbios psiquiátricos, para melhorar os sintomas associados com tais distúrbios e para reduzir o risco de tais distúrbios. . em que x1 é ch ou n, x2 é c-r5 ou n, y é o ou s, r1 é inter alia c2-c8-alquil, c2-c8-alquenil, c1-c4-fluoroalquil, c3-c8-cicloalquil, c5-c8-cicloalquil transportando um anel de benzeno fundido, ou uma fração z1-ar1; r2 é um radical de fórmula cr21r22r23 ou fenil ou hetaril de 5- ou 6- membros tendo 1, 2 ou 3 heteroátomos como membros do anel que são selecionados a partir de o, s e n, em que o fenil e o hetaril monocíclico são não substituídos ou podem transportar 1, 2 ou 3 substituintes idênticos ou diferentes ra, r3 é inter alia hidrogênio, c1-c8-alquil, c2-c8-alquenil, c1-c4-fluoroalquil, c3-c8-cicloalquil, etc, ou r2 e r3 juntamente com o átomo de nitrogênio, ao qual eles estão ligados formam um anel heterocíclico de 5- a 7- membros saturado opcionalmente substituído que, além do átomo de nitrogênio, pode ter 1 ou 2 heteroátomos adicionais ou grupos contendo heteroátomos selecionados a partir do grupo de o, n, s, so e so2; r4 é inter alia c1-c4-alquil, c1-c4-fluoroalquil, c3-c6-cicloalquil, c3-c6-cicloalquil-c1-c4-alquil ou z4-ar4; r5 é inter alia hidrogênio, halogênio, c1-c4-alquil, c1-c4-fluoroalquil, c1-c4-alcóxi, c1-c4-fluoro-alcóxi, -z5-ar5,-o-z5-ar5, etc; em que z1 a z5, ar1 a ar5, ra, r21, r22 e r23 são como definidos nas reivindicações.
BR112014011173A 2011-11-09 2012-11-08 carboxamidas heterocíclicas úteis como inibidores de fosfodiesterase tipo 10a BR112014011173A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161557878P 2011-11-09 2011-11-09
PCT/EP2012/072175 WO2013068489A1 (en) 2011-11-09 2012-11-08 Heterocyclic carboxamides useful as inhibitors of phosphodiesterase type 10a

Publications (1)

Publication Number Publication Date
BR112014011173A2 true BR112014011173A2 (pt) 2017-05-09

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US (3) US20130116229A1 (pt)
EP (1) EP2780324B1 (pt)
JP (1) JP2014532747A (pt)
KR (1) KR20140090665A (pt)
CN (1) CN104203919A (pt)
AU (1) AU2012334011A1 (pt)
BR (1) BR112014011173A2 (pt)
CA (1) CA2852820A1 (pt)
HK (1) HK1201523A1 (pt)
IL (1) IL232170A0 (pt)
MX (1) MX2014005705A (pt)
RU (1) RU2014123352A (pt)
SG (1) SG11201402134VA (pt)
WO (1) WO2013068489A1 (pt)

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WO2015060368A1 (ja) * 2013-10-23 2015-04-30 武田薬品工業株式会社 複素環化合物
JP2019508496A (ja) 2016-02-15 2019-03-28 チェム−フォルシュングスツェントルン フュル モレクラーレ メディツィン ゲゼルシャフト ミット ベシュレンクテル ハフツング 癌の治療法のためのｔａｆ１阻害剤
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CN109432428A (zh) * 2018-11-02 2019-03-08 浙江大学 一种pde10a抑制剂在制备成纤维细胞活性抑制药物中的应用

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HK1201523A1 (en) 2015-09-04
US20130116229A1 (en) 2013-05-09
CN104203919A (zh) 2014-12-10
EP2780324B1 (en) 2017-05-17
EP2780324A1 (en) 2014-09-24
IL232170A0 (en) 2014-06-30
AU2012334011A1 (en) 2014-05-15
RU2014123352A (ru) 2015-12-20
MX2014005705A (es) 2014-09-04
US20180099936A1 (en) 2018-04-12
US9856220B2 (en) 2018-01-02
WO2013068489A1 (en) 2013-05-16
JP2014532747A (ja) 2014-12-08
CA2852820A1 (en) 2013-05-16
KR20140090665A (ko) 2014-07-17
US10308610B2 (en) 2019-06-04
SG11201402134VA (en) 2014-06-27
US20160318871A1 (en) 2016-11-03
NZ624124A (en) 2016-05-27

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