AR091185A1 - Derivados de 1,2,4-triazol - Google Patents

Derivados de 1,2,4-triazol

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Publication number
AR091185A1
AR091185A1 ARP130101863A AR091185A1 AR 091185 A1 AR091185 A1 AR 091185A1 AR P130101863 A ARP130101863 A AR P130101863A AR 091185 A1 AR091185 A1 AR 091185A1
Authority
AR
Argentina
Prior art keywords
alkyl
cycloalkyl
optionally substituted
heterocycloalkyl
haloalkyl
Prior art date
Application number
Other languages
English (en)
Inventor
Schaffhauser Herve
Groebke Zbinden Katrin
Kuhn Bernd
Lerner Christian
Flohr Alexander
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=48534382&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR091185(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR091185A1 publication Critical patent/AR091185A1/es

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Classifications

    • 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
    • C07D403/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • 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
    • C07D403/04—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

Landscapes

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

Abstract

Estos compuestos inhiben la PDE10A y pueden utilizarse como medicamentos. Reivindicación 1: Un compuesto de la fórmula (1) ó (2) en las que: B es alquileno C₁₋₄, alquenileno C₂₋₄, alquinileno C₂₋₄, cicloalquilo C₃₋₅; R¹ y R² se eligen con independencia entre hidrógeno, alquilo C₁₋₇ opcionalmente sustituido por cicloalquilo C₃₋₅; hidroxialquilo C₁₋₇, alcoxialquilo C₁₋₇, haloalquilo C₁₋₇, cicloalquilo C₃₋₅, R¹ y R² junto con el átomo de nitrógeno, al que están unidos, forman un azaespirocicloalquilo, un anillo bicíclico o un heterocicloalquilo que pueden estar sustituidos de 1 a 3 veces por sustituyentes elegidos con independencia entre el grupo formado por halógeno, alquilo C₁₋₇, alcoxialquilo C₁₋₇; hidroxi-alquilo C₁₋₇, alcoxi C₁₋₇, haloalquilo C₁₋₇, hidroxilo, -NR⁹R¹⁰ y oxo; R³ se elige entre hidrógeno, cicloalquilo C₃₋₅, alcoxialquilo C₁₋₇, haloalquilo C₁₋₇, heterocicloalquilo, -(CH₂)₀,₁,₂-arilo opcionalmente sustituido por alcoxi C₁₋₇ y alquilo C₁₋₇ opcionalmente sustituido por cicloalquilo C₃₋₅; R⁴ se elige entre heteroarilo opcionalmente sustituido de 1 a 3 veces por sustituyentes elegidos entre halógeno, alquilo C₁₋₇, hidroxialquilo C₁₋₇, haloalcoxi C₁₋₇, halo-alquilo C₁₋₇, cicloalquilo C₃₋₅, ciano, amino, nitro, -O-R⁶-C(O)-R⁷, -SO₂R⁸, alcoxi C₁₋₂ opcionalmente sustituido por alcoxi C₁₋₂, heterocicloalquilo; R⁶ y R⁸ se eligen entre alquilo C₁₋₇; R⁷ se elige entre heterocicloalquilo; R⁹ y R¹⁰ se eligen con independencia entre hidrógeno, alquilo C₁₋₇, -C(O)-O-alquilo C₁₋₇.
ARP130101863 2012-05-30 2013-05-29 Derivados de 1,2,4-triazol AR091185A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP12169954 2012-05-30

Publications (1)

Publication Number Publication Date
AR091185A1 true AR091185A1 (es) 2015-01-14

Family

ID=48534382

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP130101863 AR091185A1 (es) 2012-05-30 2013-05-29 Derivados de 1,2,4-triazol

Country Status (21)

Country Link
US (1) US9394311B2 (es)
EP (1) EP2855455B1 (es)
JP (1) JP5992096B2 (es)
KR (1) KR101666293B1 (es)
CN (1) CN104364249B (es)
AR (1) AR091185A1 (es)
AU (1) AU2013269800A1 (es)
BR (1) BR112014026828A2 (es)
CA (1) CA2868240A1 (es)
CL (1) CL2014002847A1 (es)
CO (1) CO7091174A2 (es)
CR (1) CR20140481A (es)
EA (1) EA201492069A1 (es)
IL (1) IL235829A0 (es)
MX (1) MX2014014468A (es)
PE (1) PE20142366A1 (es)
PH (1) PH12014502294A1 (es)
SG (1) SG11201406890YA (es)
TW (1) TW201402564A (es)
WO (1) WO2013178572A1 (es)
ZA (1) ZA201407695B (es)

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* Cited by examiner, † Cited by third party
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CA2888324A1 (en) * 2012-11-07 2014-05-15 Alexander Flohr Triazolo compounds
EA201991095A1 (ru) 2016-11-03 2019-09-30 Бристол-Маерс Сквибб Компани Замещенные азотсодержащие соединения
CN111875583B (zh) * 2017-10-17 2021-06-15 中国科学院上海药物研究所 三氮唑衍生物及其制备方法和用途
US20190292188A1 (en) 2018-02-27 2019-09-26 Incyte Corporation Imidazopyrimidines and triazolopyrimidines as a2a / a2b inhibitors
WO2019222677A1 (en) 2018-05-18 2019-11-21 Incyte Corporation Fused pyrimidine derivatives as a2a / a2b inhibitors
PE20211807A1 (es) 2018-07-05 2021-09-14 Incyte Corp Derivados de pirazina fusionados como inhibidores de a2a/a2b
BR112020013697A2 (pt) 2018-11-06 2020-12-01 H. Lundbeck A/S compostos para tratamento de sintomas negativos e comprometimentos cognitivos
WO2020094591A1 (en) 2018-11-06 2020-05-14 H. Lundbeck A/S Pde10a inhibitors for treating negative symptoms and cognitive impairments in a patient suffering from schizophrenia
TWI829857B (zh) 2019-01-29 2024-01-21 美商英塞特公司 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶
WO2021059220A1 (en) * 2019-09-25 2021-04-01 Oncoarendi Therapeutics S.A. Process for the production of 5-(4-((2 s,5 s)-5-(4-chlorobenzyl)-2-methylmorpholino)piperidin-1-yl)-1 h-1,2,4-triazol-3-amine
CN113929634A (zh) * 2021-11-22 2022-01-14 山西永津集团有限公司 一种2,3-二溴喹喔啉的合成方法

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AR022229A1 (es) * 1999-01-12 2002-09-04 Abbott Gmbh & Co Kg Compuestos de triazol, composicion farmaceutica que los comprende y uso de los mismos para preparar dicha composicion
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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
JP2008540633A (ja) * 2005-05-18 2008-11-20 ファイザー・リミテッド バソプレッシン拮抗薬としての１，２，４−トリアゾール誘導体
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WO2012054366A2 (en) * 2010-10-21 2012-04-26 Merck Sharp & Dohme Corp. Substituted amino-triazolyl pde10 inhibitors

Also Published As

Publication number Publication date
CL2014002847A1 (es) 2015-01-30
BR112014026828A2 (pt) 2017-06-27
JP2015518018A (ja) 2015-06-25
PE20142366A1 (es) 2015-01-10
JP5992096B2 (ja) 2016-09-14
EP2855455A1 (en) 2015-04-08
CN104364249B (zh) 2018-04-17
EA201492069A1 (ru) 2015-03-31
CO7091174A2 (es) 2014-10-21
TW201402564A (zh) 2014-01-16
CR20140481A (es) 2014-11-17
EP2855455B1 (en) 2017-11-08
MX2014014468A (es) 2015-02-12
KR101666293B1 (ko) 2016-10-13
CA2868240A1 (en) 2013-12-05
KR20150027143A (ko) 2015-03-11
PH12014502294A1 (en) 2014-12-15
CN104364249A (zh) 2015-02-18
SG11201406890YA (en) 2014-11-27
US20150148332A1 (en) 2015-05-28
ZA201407695B (en) 2016-08-31
US9394311B2 (en) 2016-07-19
IL235829A0 (en) 2015-02-01
AU2013269800A1 (en) 2014-10-09
WO2013178572A1 (en) 2013-12-05

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