AR087771A1 - Moduladores de la pde10 - Google Patents

Moduladores de la pde10

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Publication number
AR087771A1
AR087771A1 ARP120103252A ARP120103252A AR087771A1 AR 087771 A1 AR087771 A1 AR 087771A1 AR P120103252 A ARP120103252 A AR P120103252A AR P120103252 A ARP120103252 A AR P120103252A AR 087771 A1 AR087771 A1 AR 087771A1
Authority
AR
Argentina
Prior art keywords
alkyl
haloalkyl
heteroaryl
aryl
halogen
Prior art date
Application number
ARP120103252A
Other languages
English (en)
Inventor
Bachmann Stephan
Flohr Alexander
Groebke Zbinden Katrin
Koerner Matthias
Kuhn Bernd
Peters Jens
Uwe-Rudolph Markus
Original Assignee
Hoffmann La Roche
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR087771A1 publication Critical patent/AR087771A1/es

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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
    • C07D471/04—Ortho-condensed systems
    • 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
    • A61P25/14—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
    • 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
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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 ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members 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 ring carbon atoms
    • C07D233/90—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—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
    • C07D403/12—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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—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 three or more hetero rings
    • 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
    • C07D413/12—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 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
    • C07D413/14—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
    • 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
    • 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
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Psychiatry (AREA)
  • Diabetes (AREA)
  • Psychology (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Addiction (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La presente se refiere a compuestos de la fórmula (1) que actúan como moduladores de la PDE10A. Estos compuestos inhiben la PDE10A y pueden utilizarse como medicamentos en trastornos psicóticos como por ejemplo la esquizofrenia, pánico, Alzheimer, etc.. Reivindicación 1: Un compuesto de la fórmula (1) en la que: X y X¹ son con independencia CR⁴ o N; Y e Y¹ son con independencia C o N; Z y Z¹ son con independencia CR⁶, NR⁷, N, O ó S; R¹ y R² se eligen con independencia entre hidrógeno, alquilo C₁₋₇, cicloalquilo C₃₋₈, haloalquilo C₁₋₇, (alcoxi C₁₋₇)-alquilo C₁₋₇, heterocicloalquilo o alquilo C₁₋₇ opcionalmente sustituido por arilo o heteroarilo o R¹ y R², junto con el átomo de nitrógeno al que están unidos, forman un sistema de anillo bicíclico o un heterocicloalquilo, que puede estar sustituido por 1 - 3 sustituyentes elegidos con independencia entre el grupo formado por hidroxilo, halógeno, alquilo C₁₋₇, alcoxi C₁₋₇, haloalquilo C₁₋₇ y oxo; R³ es hidrógeno o alquilo C₁₋₇; R⁴ es hidrógeno, alquilo C₁₋₇, cicloalquilo C₃₋₈, haloalquilo C₁₋₇ o halógeno; R⁵ es arilo o heteroarilo, ambos grupos están opcionalmente sustituidos por alquilo C₁₋₇, cicloalquilo C₃₋₈, halógeno, haloalquilo C₁₋₇, alcoxi C₁₋₇, hidroxilo, hidroxialquilo C₁₋₇, alcoxialquilo C₁₋₇, acetilo, ciano, amino opcionalmente sustituido por uno o dos grupos alquilo C₁₋₇; R⁶ es hidrógeno, halógeno, alquilo C₁₋₇, cicloalquilo C₃₋₈, alcoxi C₁₋₇, haloalquilo C₁₋₇, alcoxialquilo C₁₋₇, heterocicloalquilo, arilo, heteroarilo o alquilo C₁₋₇ opcionalmente sustituido por arilo, heteroarilo, heterocicloalquilo, cicloalquilo o R⁵ y R⁶, junto con los grupos Y¹ y Z a los que están unidos, forman un arilo o heteroarilo, ambos grupos están opcionalmente sustituidos por alquilo C₁₋₇, halógeno, alcoxi C₁₋₇, haloalquilo C₁₋₇; R⁷ es hidrógeno, halógeno, alquilo C₁₋₇, cicloalquilo C₃₋₈, alcoxi C₁₋₇, haloalquilo C₁₋₇, alcoxialquilo C₁₋₇, heterocicloalquilo, arilo, heteroarilo o alquilo C₁₋₇ opcionalmente sustituido por arilo, heteroarilo, heterocicloalquilo, cicloalquilo o R⁵ y R⁷, junto con los grupos Y¹ y Z a los que están unidos, forman un arilo o heteroarilo, ambos grupos están opcionalmente sustituidos por alquilo C₁₋₇, halógeno, alcoxi C₁₋₇, haloalquilo C₁₋₇; W se elige entre etileno y etenileno, ambos están opcionalmente sustituidos por alquilo C₁₋₇ o halógeno o W es -N=CH-.
ARP120103252A 2011-09-06 2012-09-04 Moduladores de la pde10 AR087771A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP11180135A EP2574607A1 (en) 2011-09-06 2011-09-06 PDE10 modulators

Publications (1)

Publication Number Publication Date
AR087771A1 true AR087771A1 (es) 2014-04-16

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ID=46832363

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ARP120103252A AR087771A1 (es) 2011-09-06 2012-09-04 Moduladores de la pde10

Country Status (14)

Country Link
US (1) US8772510B2 (es)
EP (2) EP2574607A1 (es)
JP (1) JP5973576B2 (es)
KR (1) KR101611106B1 (es)
CN (1) CN103781768B (es)
AR (1) AR087771A1 (es)
BR (1) BR112014004522A2 (es)
CA (1) CA2844652C (es)
ES (1) ES2550201T3 (es)
HK (1) HK1195767A1 (es)
MX (1) MX340607B (es)
RU (1) RU2567396C1 (es)
TW (1) TWI434687B (es)
WO (1) WO2013034506A1 (es)

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WO2015172196A1 (en) * 2014-05-13 2015-11-19 Monash University Heterocyclic compounds and use of same
JP2021522181A (ja) * 2018-04-20 2021-08-30 バイエル・アクチエンゲゼルシヤフト 殺有害生物剤としてのヘテロアリール−トリアゾール化合物及びヘテロアリール−テトラゾール化合物
CN110903245B (zh) * 2018-09-17 2022-11-22 南京药石科技股份有限公司 一种合成1-烷基-2-三氟甲基-5-氨基-1h-咪唑的关键中间体及其制备方法
BR112020013697A2 (pt) 2018-11-06 2020-12-01 H. Lundbeck A/S compostos para tratamento de sintomas negativos e comprometimentos cognitivos
BR112020013820A2 (pt) 2018-11-06 2021-06-01 H. Lundbeck A/S inibidores de pde10a para tratamento de sintomas negativos e comprometimentos cognitivos em um paciente sofrendo de esquizofrenia
CN110759902B (zh) * 2019-11-01 2022-04-22 海南一龄医疗产业发展有限公司 Set8赖氨酸甲基转移酶抑制剂及其制备方法和用途
CN114989103A (zh) * 2022-06-09 2022-09-02 杭州科巢生物科技有限公司 一种2-甲氧基-3-(1-甲基-1h-1,2,4-三唑-3-基)苯胺的制备方法

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CA2534432A1 (en) 2003-07-31 2005-02-10 Bayer Pharmaceuticals Corporation Methods for treating diabetes and related disorders using pde10a inhibitors
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JP2010504980A (ja) * 2006-09-28 2010-02-18 エグゼリクシス， インコーポレイテッド Ｊａｋ−２モジュレーターおよび使用方法
KR101324329B1 (ko) * 2008-09-04 2013-10-31 미쓰비시 타나베 파마 코퍼레이션 삼치환된 피리미딘 화합물 및 ｐｄｅ10 억제제로서의 그의 용도
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JP5629322B2 (ja) 2009-09-24 2014-11-19 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ ホスホジエステラーゼ１０ａ阻害剤としてのイミダゾピリジンまたはイミダゾピリミジン誘導体
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Also Published As

Publication number Publication date
EP2574607A1 (en) 2013-04-03
EP2753604B1 (en) 2015-08-19
US20130059833A1 (en) 2013-03-07
ES2550201T3 (es) 2015-11-05
HK1195767A1 (zh) 2014-11-21
CN103781768B (zh) 2016-08-17
TW201317227A (zh) 2013-05-01
EP2753604A1 (en) 2014-07-16
MX2014002682A (es) 2014-04-14
JP5973576B2 (ja) 2016-08-23
CN103781768A (zh) 2014-05-07
JP2014525467A (ja) 2014-09-29
TWI434687B (zh) 2014-04-21
KR101611106B1 (ko) 2016-04-08
CA2844652C (en) 2016-11-01
US8772510B2 (en) 2014-07-08
BR112014004522A2 (pt) 2017-06-13
MX340607B (es) 2016-07-18
RU2567396C1 (ru) 2015-11-10
CA2844652A1 (en) 2013-03-14
KR20140069088A (ko) 2014-06-09
WO2013034506A1 (en) 2013-03-14

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