PE20161415A1 - Derivados de etinilo - Google Patents

Derivados de etinilo

Info

Publication number
PE20161415A1
PE20161415A1 PE2016001503A PE2016001503A PE20161415A1 PE 20161415 A1 PE20161415 A1 PE 20161415A1 PE 2016001503 A PE2016001503 A PE 2016001503A PE 2016001503 A PE2016001503 A PE 2016001503A PE 20161415 A1 PE20161415 A1 PE 20161415A1
Authority
PE
Peru
Prior art keywords
alkyl
phenyl
compounds
hexahydropyrimidin
phenylethynyl
Prior art date
Application number
PE2016001503A
Other languages
English (en)
Inventor
Fionn O`Hara
Jean-Marc Plancher
Barbara Biemans
Eric Vieira
Antonio Ricci
Wolfgang Guba
Georg Jaeschke
Daniel Rueher
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=50151209&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20161415(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 PE20161415A1 publication Critical patent/PE20161415A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/20—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D239/22—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to ring 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
    • A61K31/495—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
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • 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
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems

Landscapes

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

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE ETINILO DE FORMULA (I) DONDE Y ES N, ENTRE OTROS; R1 ES H, HALOGENO, ENTRE OTROS; R2 ES H O ALQUILO C1-C7; R3 ES FENILO O PIRIDINILO; R4’ ES H, ALQUILO C1-C7 O ALCOXIALQUILO C1-C7; R4 ES H, ALQUILO C1-C7, ENTRE OTROS; R5 Y R5’ SON H O ALQUILO C1-C7. SON COMPUESTOS PREFERIDOS: 3-[2,6-DIFLUORO-4-(2-FENILETINIL)FENIL]-1,6,6-TRIMETIL-HEXAHIDROPIRIMIDIN-2,4-DIONA; 3-[2-CLORO-4-(2-FENILETINIL)FENIL]-1,6,6-TRIMETIL-HEXAHIDROPIRIMIDIN-2,4-DIONA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON MODULADORES DEL RECEPTOR METABOTROPICO DE GLUTAMATO 4 (mGluR4) SIENDO UTILES EN EL TRATAMIENTO DE LA ENFERMEDAD DE PARKINSON, ANSIEDAD, DEPRESION
PE2016001503A 2014-02-25 2015-02-24 Derivados de etinilo PE20161415A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP14156461 2014-02-25

Publications (1)

Publication Number Publication Date
PE20161415A1 true PE20161415A1 (es) 2017-01-06

Family

ID=50151209

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2016001503A PE20161415A1 (es) 2014-02-25 2015-02-24 Derivados de etinilo

Country Status (31)

Country Link
US (1) US9725416B2 (es)
EP (1) EP3110802B1 (es)
JP (1) JP6286577B2 (es)
KR (1) KR101792452B1 (es)
CN (1) CN106029649B (es)
AR (1) AR099529A1 (es)
AU (1) AU2015222303B2 (es)
BR (1) BR112016017816A8 (es)
CA (1) CA2938009A1 (es)
CL (1) CL2016002064A1 (es)
CR (1) CR20160384A (es)
DK (1) DK3110802T3 (es)
EA (1) EA029261B1 (es)
ES (1) ES2701167T3 (es)
HR (1) HRP20182016T1 (es)
HU (1) HUE041392T2 (es)
IL (1) IL246842B (es)
LT (1) LT3110802T (es)
MA (1) MA39305A3 (es)
MX (1) MX369819B (es)
PE (1) PE20161415A1 (es)
PH (1) PH12016501481A1 (es)
PL (1) PL3110802T3 (es)
PT (1) PT3110802T (es)
RS (1) RS58208B1 (es)
SG (1) SG11201607010XA (es)
SI (1) SI3110802T1 (es)
TW (1) TWI576340B (es)
UA (1) UA117855C2 (es)
WO (1) WO2015128307A1 (es)
ZA (1) ZA201605243B (es)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6539749B2 (ja) * 2015-03-19 2019-07-03 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ ｍＧｌｕＲ４のモジュレーターとしての３−（４−エチニルフェニル）ヘキサヒドロピリミジン−２，４−ジオン誘導体
AU2016273751B2 (en) 2015-06-03 2020-04-02 F. Hoffmann-La Roche Ag Ethynyl derivatives
JP6761821B2 (ja) 2015-07-15 2020-09-30 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ 代謝性グルタミン酸受容体モジュレーターとしてのエチニル誘導体
AR105556A1 (es) * 2015-08-03 2017-10-18 Hoffmann La Roche Derivados de etinilo
SG11201811829QA (en) 2016-07-18 2019-02-27 Hoffmann La Roche Ethynyl derivatives

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2773038A1 (en) * 2009-09-04 2011-03-10 P. Jeffrey Conn Mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
US8759377B2 (en) * 2009-11-23 2014-06-24 Vanderbilt University Substituted dioxopiperidines and dioxopyrrolidines 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
MA38885B1 (fr) * 2013-09-25 2018-11-30 Hoffmann La Roche Dérivés d'éthynyle modulateurs allosteriques positifs (pam) du recepteur metabotropique du glutamate 4 (mglu4)
TWI649310B (zh) * 2014-01-10 2019-02-01 赫孚孟拉羅股份公司 乙炔基衍生物

Also Published As

Publication number Publication date
WO2015128307A1 (en) 2015-09-03
US20160362383A1 (en) 2016-12-15
MX369819B (es) 2019-11-22
ES2701167T3 (es) 2019-02-21
AR099529A1 (es) 2016-07-27
PH12016501481B1 (en) 2016-08-22
SI3110802T1 (sl) 2019-01-31
EP3110802B1 (en) 2018-10-10
RS58208B1 (sr) 2019-03-29
PH12016501481A1 (en) 2016-08-22
JP6286577B2 (ja) 2018-02-28
EA201691690A1 (ru) 2016-12-30
TW201546051A (zh) 2015-12-16
CR20160384A (es) 2016-11-07
KR101792452B1 (ko) 2017-11-01
IL246842B (en) 2018-11-29
US9725416B2 (en) 2017-08-08
CL2016002064A1 (es) 2017-01-13
HUE041392T2 (hu) 2019-05-28
LT3110802T (lt) 2018-12-27
EA029261B1 (ru) 2018-02-28
PL3110802T3 (pl) 2019-03-29
AU2015222303A1 (en) 2016-09-15
UA117855C2 (uk) 2018-10-10
KR20160111509A (ko) 2016-09-26
MX2016011099A (es) 2016-12-12
HRP20182016T1 (hr) 2019-01-25
CN106029649A (zh) 2016-10-12
AU2015222303B2 (en) 2019-02-28
PT3110802T (pt) 2018-12-04
ZA201605243B (en) 2017-09-27
CA2938009A1 (en) 2015-09-03
DK3110802T3 (en) 2019-01-07
JP2017506650A (ja) 2017-03-09
BR112016017816A8 (pt) 2020-06-30
MA39305A3 (fr) 2018-05-31
TWI576340B (zh) 2017-04-01
SG11201607010XA (en) 2016-09-29
CN106029649B (zh) 2019-02-12
EP3110802A1 (en) 2017-01-04

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