PE20171318A1 - Ciclopropabenzofuranil-piridopirazindionas novedosas - Google Patents

Ciclopropabenzofuranil-piridopirazindionas novedosas

Info

Publication number
PE20171318A1
PE20171318A1 PE2017001310A PE2017001310A PE20171318A1 PE 20171318 A1 PE20171318 A1 PE 20171318A1 PE 2017001310 A PE2017001310 A PE 2017001310A PE 2017001310 A PE2017001310 A PE 2017001310A PE 20171318 A1 PE20171318 A1 PE 20171318A1
Authority
PE
Peru
Prior art keywords
halogen
methyl
hydrogen
dihydro
cyano
Prior art date
Application number
PE2017001310A
Other languages
English (en)
Inventor
Martin Youngjin Pettersson
Ende Christopher William Am
Douglas Scott Johnson
Gregory Wayne Kauffman
Antonia Friederike Stepan
Patrick Robert Verhoest
Original Assignee
Pfizer
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 Pfizer filed Critical Pfizer
Publication of PE20171318A1 publication Critical patent/PE20171318A1/es

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Classifications

    • 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
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Se refiere a un compuesto de formula I, donde: X es un heteroarilo de 5 a 14 miembros que contiene 1 a 3 heteroatomos; R1 es hidrogeno, halogeno, entre otros; R2a y R2b son hidrogeno, halogeno, ciano, entre otros; R4a y R4b son hidrogeno, halogeno, oxo, entre otros; R5a y R5b son hidrogeno, halogeno, SF5, entre otros; R6 y R7 son hidrogeno, halogeno, entre otros; R10 es halogeno, ciano, entre otros; R11 es halogeno, ciano, entre otros; y es un numero entero de 1, 2, 3 o 4. Son compuestos preferidos: 2-{[(1aS, 6bR)-4-fluoro-1a-metil-5-(trifluorometoxi)-1,1a-dihidro-6bH-ciclopropa[b][1]benzofuran-6b-il]metil}-7-(4-metil-1H-imidazol-1-il)-3,4-dihidro-2H-pirido[1,2-a]pirazin-1,6-diona; 2-{[(1aS, 6bR)-3-fluoro-1a-metil-5-(trifluorometoxi)-1,1a-dihidro-6bH-ciclopropa[b][1]benzofuran-6b-il]metil}-7-(4-metil-1H-imidazol-1-il)-3,4-dihidro-2H-pirido[1,2-a]pirazin-1,6-diona; entre otros. Tambien se refiere a una composicion farmaceutica. Dichos compuestos son moduladores de gamma-secretasa, siendo utiles en el tratamiento de trastornos neurodegenerativos y neurologicos, tales como la enfermedad de Alzheimer y sindrome de Down.
PE2017001310A 2015-02-03 2016-01-26 Ciclopropabenzofuranil-piridopirazindionas novedosas PE20171318A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201562111222P 2015-02-03 2015-02-03

Publications (1)

Publication Number Publication Date
PE20171318A1 true PE20171318A1 (es) 2017-09-07

Family

ID=55299692

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2017001310A PE20171318A1 (es) 2015-02-03 2016-01-26 Ciclopropabenzofuranil-piridopirazindionas novedosas

Country Status (22)

Country Link
US (2) US20160222007A1 (es)
EP (1) EP3253755B1 (es)
JP (1) JP6628805B2 (es)
KR (1) KR102000382B1 (es)
CN (1) CN107406445B (es)
AR (1) AR103582A1 (es)
AU (1) AU2016214102B2 (es)
BR (1) BR112017015693A2 (es)
CA (1) CA2919338A1 (es)
DK (1) DK3253755T3 (es)
EA (1) EA033423B1 (es)
EC (1) ECSP17050310A (es)
ES (1) ES2818806T3 (es)
IL (1) IL253635A0 (es)
MX (1) MX368391B (es)
PE (1) PE20171318A1 (es)
PH (1) PH12017501369A1 (es)
SG (1) SG11201705780PA (es)
TN (1) TN2017000342A1 (es)
TW (1) TWI616445B (es)
UY (1) UY36546A (es)
WO (1) WO2016125048A1 (es)

Families Citing this family (6)

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Publication number Priority date Publication date Assignee Title
US20210393621A1 (en) 2018-10-26 2021-12-23 The Research Foundation For The State University Of New York Combination serotonin specific reuptake inhibitor and serotonin 1a receptor partial agonist for reducing l-dopa-induced dyskinesia
KR102271305B1 (ko) 2020-05-21 2021-06-30 주식회사 아리바이오 치매 예방 및 치료용 조성물
CN111978324A (zh) * 2020-08-28 2020-11-24 开封康诺药业有限公司 一种多索茶碱的晶型及其制备方法
KR102272907B1 (ko) 2020-11-05 2021-07-05 주식회사 아리바이오 치매 예방 및 치료용 조성물
KR102272910B1 (ko) 2021-01-28 2021-07-06 주식회사 아리바이오 당뇨병을 동반한 치매 예방 및 치료용 조성물
KR102311224B1 (ko) * 2021-04-23 2021-10-13 주식회사 아리바이오 Pde5 억제제와 글루코코르티코이드 수용체 길항제 병용투여를 통한 치매 예방 및 치료용 조성물

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