AR085226A1 - 6-cicloalquil-pirazolopirimidinonas para el tratamiento de trastornos del snc - Google Patents

6-cicloalquil-pirazolopirimidinonas para el tratamiento de trastornos del snc

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Publication number
AR085226A1
AR085226A1 ARP120100483A ARP120100483A AR085226A1 AR 085226 A1 AR085226 A1 AR 085226A1 AR P120100483 A ARP120100483 A AR P120100483A AR P120100483 A ARP120100483 A AR P120100483A AR 085226 A1 AR085226 A1 AR 085226A1
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AR
Argentina
Prior art keywords
substituents
group
fluorine
alkyl
substituted
Prior art date
Application number
ARP120100483A
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English (en)
Inventor
Riccardo Giovannini
Niklas Heine
Original Assignee
Boehringer Ingelheim Int
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Publication date
Application filed by Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of AR085226A1 publication Critical patent/AR085226A1/es

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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • A61P25/08—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
    • 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
    • A61P25/20—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
    • A61P25/28—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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Psychology (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Anesthesiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Uso para la preparación de medicamentos para el tratamiento de enfermedades concernientes a insuficiencias en la percepción, concentración, aprendizaje o memoria. Dichas afecciones pueden estar asociadas por ejemplo a la enfermedad de Alzheimer, esquizofrenia y otras enfermedades. También, para la preparación de medicamentos y/o para su uso en el tratamiento de estas enfermedades, en particular para la insuficiencia cognitiva asociada a dicha enfermedad. Los compuestos presentan propiedades inhibidoras de PDE9.Reivindicación 1: Un compuesto caracterizado porque tiene la fórmula (1) en la que X es N o CRe; Ra, Rb, Rc, Re se seleccionan independientemente uno de otro del grupo consistente en H, alquilo C1-6, alquil C1-6-O-, -CF3, -CHF2, -CH2F, NC- y halógeno; en los que alquilo C1-6 y alquilo C1-6-O- opcionalmente pueden estar sustituidos con halógeno, preferentemente con flúor; Rd se selecciona del grupo consistente en flúor, NC-, -CF3, -CHF2, -CH2F y metilo; D se selecciona del grupo que consiste en ciclopentilo, ciclohexilo, tetrahidrofuranilo, tetrahidropiranilo, 2-, 3- y 4-piridilo, en los que el ciclopentilo y el ciclohexilo opcionalmente pueden estar sustituidos por 1 ó 2 sustituyentes, en los que dichos sustituyentes pueden seleccionarse independientemente uno del otro del grupo que consiste en flúor, NC-, F3C-, HF2C- y FH2C-; en los que el tetrahidrofuranilo y el tetrahidropiranilo opcionalmente pueden estar sustituidos por 1 ó 2 sustituyentes, en los que dichos sustituyentes pueden seleccionarse independientemente uno del otro del grupo que consiste en flúor, NC-, F3C-, HF2C- y FH2C-; en los que el piridilo opcionalmente puede estar sustituido por 1, 2, 3 ó 4 sustituyentes, en los que dichos sustituyentes pueden seleccionarse del grupo que consiste en flúor, cloro, bromo, NC-, F3C-, HF2C-, FH2C-, F3C-CH2-, alquilo C1-6 y cicloalquilo C3-7; m se selecciona de 1 ó 2, preferentemente 1; n se selecciona de 0, 1 ó 2, preferentemente 0 ó 1, más preferentemente 0, en el que si n = 2, los dos grupos Rd se seleccionan independientemente uno de otro; y sales, preferentemente una de sus sales farmacéuticamente aceptables, uno de sus solvatos y uno de sus solvatos de susodichas sales.
ARP120100483A 2011-02-15 2012-02-14 6-cicloalquil-pirazolopirimidinonas para el tratamiento de trastornos del snc AR085226A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP11154572 2011-02-15
EP11154858 2011-02-17

Publications (1)

Publication Number Publication Date
AR085226A1 true AR085226A1 (es) 2013-09-18

Family

ID=45569679

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP120100483A AR085226A1 (es) 2011-02-15 2012-02-14 6-cicloalquil-pirazolopirimidinonas para el tratamiento de trastornos del snc

Country Status (6)

Country Link
US (1) US8809345B2 (es)
EP (1) EP2675806B1 (es)
JP (1) JP5901659B2 (es)
AR (1) AR085226A1 (es)
UY (1) UY33910A (es)
WO (1) WO2012110441A1 (es)

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WO2012057248A1 (ja) 2010-10-29 2012-05-03 塩野義製薬株式会社 ナフチリジン誘導体
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WO2014065434A1 (en) 2012-10-24 2014-05-01 Shionogi & Co., Ltd. Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity
SI3865484T1 (sl) 2015-07-07 2024-05-31 H. Lundbeck A/S Zaviralec pde9 z imidazo pirazinonsko hrbtenico za zdravljenje perifernih bolezni
CN105669680B (zh) * 2016-03-24 2018-02-23 南京药捷安康生物科技有限公司 吡咯并[2,1‑f][1,2,4]三嗪‑4(1H)‑酮衍生物类PDE9A抑制剂
EP3632439B1 (en) * 2017-06-01 2024-03-27 Eisai R&D Management Co., Ltd. Dementia therapeutic agent combining pyrazoloquinoline derivative and donepezil
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JP2021526134A (ja) 2018-05-25 2021-09-30 イマラ インク． ６−［（３Ｓ，４Ｓ）−４−メチル−ｌ−（ピリミジン−２−イルメチル）ピロリジン−３−イル］−３−テトラヒドロピラン−４−イル−７Ｈ−イミダゾ［ｌ，５−Ａ］ピラジン−８−オンの一水和物および結晶形態
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