MX344770B - Derivados de 6-cicloalquil-1,5-dihidro-pirazolo (3,4-d) pirimidin-4-onas y su uso como inhibidores de pde9a. - Google Patents

Derivados de 6-cicloalquil-1,5-dihidro-pirazolo (3,4-d) pirimidin-4-onas y su uso como inhibidores de pde9a.

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Publication number
MX344770B
MX344770B MX2013001335A MX2013001335A MX344770B MX 344770 B MX344770 B MX 344770B MX 2013001335 A MX2013001335 A MX 2013001335A MX 2013001335 A MX2013001335 A MX 2013001335A MX 344770 B MX344770 B MX 344770B
Authority
MX
Mexico
Prior art keywords
medicaments
cycloalkyl
pyrazolo
pyrimidin
dihydro
Prior art date
Application number
MX2013001335A
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English (en)
Other versions
MX2013001335A (es
Inventor
Eickmeier Christian
Schaenzle Gerhard
Heine Niklas
Rosenbrock Holger
Giovannini Riccardo
Ferrara Marco
Original Assignee
Boehringer Ingelheim Int Gmbh *
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 Boehringer Ingelheim Int Gmbh * filed Critical Boehringer Ingelheim Int Gmbh *
Publication of MX2013001335A publication Critical patent/MX2013001335A/es
Publication of MX344770B publication Critical patent/MX344770B/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
    • 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
    • A61K31/495—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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
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    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
    • 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
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    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic 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
    • 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
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    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Virology (AREA)
  • Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Ophthalmology & Optometry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Oncology (AREA)
  • Anesthesiology (AREA)
  • Communicable Diseases (AREA)
  • AIDS & HIV (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)

Abstract

La invención se refiere a nuevas 6-cicloalquil-pirazolopirimidinon as según la fórmula (I). (ver fórmula) en donde R1 es un grupo heteroarilo aromático de 5 o 6 eslabones, R2 es un sustituyente opcional, D es ciclopentilo, ciclohexilo, tetrahidrofuranilo, tetrahidropiranilo o 2-, 3- o 4-piridilo, opcionalmente sustituidos, m = 1 o 2 y n es 0, 1 o 2. Los nuevos compuestos son para usar como la entidad activa de medicamentos o para la fabricación de medicamentos respectivamente, en particular medicamentos para el tratamiento de estados relacionados con déficits en la percepción, concentración, aprendizaje o memoria. Tales estados pueden por ejemplo estar asociados con la enfermedad de Alzheimer, esquizofrenia y otras enfermedades. Los nuevos compuestos son también por ejemplo para la fabricación de medicamentos y/o para uso en el tratamiento de estas enfermedades, en particular para el impedimento cognitivo asociado con dicha enfermedad. El compuesto de la invención muestra propiedades inhibitorias de PDE9.
MX2013001335A 2010-08-12 2011-08-09 Derivados de 6-cicloalquil-1,5-dihidro-pirazolo (3,4-d) pirimidin-4-onas y su uso como inhibidores de pde9a. MX344770B (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP10172597 2010-08-12
EP11154397 2011-02-14
PCT/EP2011/063705 WO2012020022A1 (en) 2010-08-12 2011-08-09 6-cycloalkyl-1, 5-dihydro-pyrazolo [3, 4-d] pyrimidin-4-one derivatives and their use as pde9a inhibitors

Publications (2)

Publication Number Publication Date
MX2013001335A MX2013001335A (es) 2013-03-22
MX344770B true MX344770B (es) 2017-01-06

Family

ID=45567392

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2013001335A MX344770B (es) 2010-08-12 2011-08-09 Derivados de 6-cicloalquil-1,5-dihidro-pirazolo (3,4-d) pirimidin-4-onas y su uso como inhibidores de pde9a.

Country Status (30)

Country Link
US (2) US8912201B2 (es)
EP (2) EP2603511B1 (es)
JP (1) JP5756176B2 (es)
KR (1) KR101918909B1 (es)
CN (2) CN105541849B (es)
AP (1) AP2012006631A0 (es)
AR (1) AR082667A1 (es)
AU (1) AU2011288503C1 (es)
BR (1) BR112013003097B1 (es)
CA (1) CA2807687C (es)
CL (1) CL2013000368A1 (es)
CO (1) CO6670591A2 (es)
DK (1) DK2603511T3 (es)
EA (1) EA024984B1 (es)
ES (1) ES2626006T3 (es)
GE (1) GEP20156217B (es)
HK (1) HK1178539A1 (es)
HU (1) HUE033378T2 (es)
IL (1) IL223347A (es)
MX (1) MX344770B (es)
MY (1) MY170189A (es)
NZ (1) NZ603725A (es)
PE (1) PE20130602A1 (es)
PL (1) PL2603511T3 (es)
SG (1) SG187081A1 (es)
TN (1) TN2013000051A1 (es)
TW (1) TWI510490B (es)
UA (1) UA110347C2 (es)
UY (1) UY33556A (es)
WO (1) WO2012020022A1 (es)

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CN116585316A (zh) 2017-06-01 2023-08-15 卫材R&D管理有限公司 包含pde9抑制剂的药物组合物
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SG10202113198TA (en) 2017-06-01 2021-12-30 Eisai R&D Man Co Ltd Dementia therapeutic agent combining pyrazoloquinoline derivative and donepezil
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CN110627795A (zh) * 2018-06-21 2019-12-31 南京药捷安康生物科技有限公司 磷酸二酯酶抑制剂及其用途
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