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PE20180357A1 - Derivados de etinilo - Google Patents

Derivados de etinilo

Info

Publication number
PE20180357A1
PE20180357A1 PE2017002405A PE2017002405A PE20180357A1 PE 20180357 A1 PE20180357 A1 PE 20180357A1 PE 2017002405 A PE2017002405 A PE 2017002405A PE 2017002405 A PE2017002405 A PE 2017002405A PE 20180357 A1 PE20180357 A1 PE 20180357A1
Authority
PE
Peru
Prior art keywords
phenyl
compounds
phenyletinyl
triona
difluoro
Prior art date
Application number
PE2017002405A
Other languages
English (en)
Inventor
Georg Jaeschke
Fionn Ohara
Jean Marc Plancher
Antonio Ricci
Daniel Rueher
Eric Vieira
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 PE20180357A1 publication Critical patent/PE20180357A1/es

Links

Classifications

    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • 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
    • 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
    • A61P25/22—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
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/09—Geometrical isomers

Landscapes

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

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE ETINILO DE FORMULA (I) DONDE R1 ES H, F O Cl; L ES UN ENLACE O ALQUILENO INFERIOR; R2 ES ALQUILO INFERIOR SUSTITUIDO CON HALOGENO, -(CH2)n-C(O)O-ALQUILO INFERIOR, ENTRE OTROS; n ES DE 1 A 3; R3 ES H, ALQUILO INFERIOR, ENTRE OTROS; R4 ES FENILO, PIRIDINILO O PIRIMIDINILO OPCIONALMENTE SUSTITUIDO POR F; Y ES CF O CCl. SON COMPUESTOS PREFERIDOS: (9aS)-7-[2,6-DIFLUORO-4-(2-FENILETINIL)FENIL]-2-(2-METOXIETIL)-9a-METIL-4,9-DIHIDRO-3H-PIRAZINO[1,2-c]PIRIMIDINA-1,6,8-TRIONA; (9aRS)-7-[2,6-DIFLUORO-4-(2-FENILETINIL)FENIL]-9a-METIL-2-(m-TOLILMETIL)-4,9-DIHIDRO-3H-PIRAZINO[1,2-c]PIRIMIDINA-1,6,8-TRIONA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON MODULADORES ALOSTERICOS POSITIVOS (MAP) DEL RECEPTOR METABOTROPICO DEL GLUTAMATO 4 (mGluR4) SIENDO UTILES PARA EL TRATAMIENTO DE LA ENFERMEDAD DEL PARKINSON, ANSIEDAD, DEPRESION, DIABETES TIPO 2
PE2017002405A 2015-08-03 2016-08-02 Derivados de etinilo PE20180357A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP15179550 2015-08-03

Publications (1)

Publication Number Publication Date
PE20180357A1 true PE20180357A1 (es) 2018-02-21

Family

ID=53776452

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2017002405A PE20180357A1 (es) 2015-08-03 2016-08-02 Derivados de etinilo

Country Status (20)

Country Link
US (1) US10011607B2 (es)
EP (1) EP3331882B1 (es)
JP (1) JP6975511B2 (es)
KR (1) KR20180030857A (es)
CN (1) CN107667107B (es)
AR (1) AR105556A1 (es)
AU (1) AU2016302696B2 (es)
BR (1) BR112017023951A2 (es)
CA (1) CA2983908A1 (es)
CL (1) CL2018000278A1 (es)
CO (1) CO2017011010A2 (es)
IL (1) IL255103B (es)
MX (1) MX2018001486A (es)
PE (1) PE20180357A1 (es)
PH (1) PH12018500247A1 (es)
RU (1) RU2722014C9 (es)
TW (1) TWI621619B (es)
UA (1) UA120888C2 (es)
WO (1) WO2017021384A1 (es)
ZA (1) ZA201707015B (es)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201513742D0 (en) 2015-08-03 2015-09-16 Heptares Therapeutics Ltd Muscarinic agonists
EP3331863B1 (en) 2015-08-03 2020-03-11 Glenmark Pharmaceuticals S.A. Novel compounds as ror gamma modulators
AR105575A1 (es) 2015-08-03 2017-10-18 Bristol Myers Squibb Co COMPUESTOS DE QUINOLINA COMO MODULADORES DE TNFa
EP3898588B1 (en) 2018-12-21 2023-01-11 Merck Patent GmbH Disubstituted alkyne derivatives

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011057208A2 (en) * 2009-11-06 2011-05-12 Vanderbilt University Aryl and heteroaryl sulfones as mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
US8420661B2 (en) * 2010-04-13 2013-04-16 Hoffmann-La Roche Inc. Arylethynyl derivatives
PE20141168A1 (es) * 2011-04-26 2014-09-22 Hoffmann La Roche Derivados de pirazolidin-3-ona
KR101757603B1 (ko) * 2013-09-25 2017-07-12 에프. 호프만-라 로슈 아게 에틴일 유도체
TWI649310B (zh) * 2014-01-10 2019-02-01 赫孚孟拉羅股份公司 乙炔基衍生物
UA117855C2 (uk) * 2014-02-25 2018-10-10 Ф. Хоффманн-Ля Рош Аг Похідні етинілу

Also Published As

Publication number Publication date
AU2016302696A1 (en) 2017-11-02
CN107667107B (zh) 2021-05-18
RU2722014C9 (ru) 2020-10-22
AU2016302696B2 (en) 2020-05-07
PH12018500247A1 (en) 2018-08-13
EP3331882B1 (en) 2020-04-29
RU2018105872A3 (es) 2019-12-26
AR105556A1 (es) 2017-10-18
IL255103A0 (en) 2017-12-31
US10011607B2 (en) 2018-07-03
EP3331882A1 (en) 2018-06-13
KR20180030857A (ko) 2018-03-26
MX2018001486A (es) 2018-03-15
HK1246790A1 (zh) 2018-09-14
TW201718589A (zh) 2017-06-01
UA120888C2 (uk) 2020-02-25
TWI621619B (zh) 2018-04-21
JP6975511B2 (ja) 2021-12-01
BR112017023951A2 (pt) 2018-07-24
US20180127429A1 (en) 2018-05-10
CN107667107A (zh) 2018-02-06
JP2018522037A (ja) 2018-08-09
CA2983908A1 (en) 2017-02-09
IL255103B (en) 2020-01-30
RU2018105872A (ru) 2019-09-05
CL2018000278A1 (es) 2018-07-06
CO2017011010A2 (es) 2018-02-09
ZA201707015B (en) 2018-11-28
RU2722014C2 (ru) 2020-05-26
WO2017021384A1 (en) 2017-02-09

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