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CR20160384A - Derivados de etilino - Google Patents

Derivados de etilino

Info

Publication number
CR20160384A
CR20160384A CR20160384A CR20160384A CR20160384A CR 20160384 A CR20160384 A CR 20160384A CR 20160384 A CR20160384 A CR 20160384A CR 20160384 A CR20160384 A CR 20160384A CR 20160384 A CR20160384 A CR 20160384A
Authority
CR
Costa Rica
Prior art keywords
lower alkyl
hydrogen
halogen
optionally substituted
pyridinyl
Prior art date
Application number
CR20160384A
Other languages
English (en)
Inventor
Jean Marc Plancher
Eric Vieira
Georg Jaeschke
Barbara Biemans
Fionn O'hara
Daniel Rueher
Wolfgang Guba
Antonio Ricci
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=CR20160384(A) "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 CR20160384A publication Critical patent/CR20160384A/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/20Heterocyclic 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
    • C07D239/22Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/10Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/10Spiro-condensed systems
    • C07D491/107Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic 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
    • C07D498/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (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

La presente invención se refiere a compuestos de fórmula I en el que Y es N o C-R1¿; R1¿ es hidrógeno o F; R1 es hidrógeno, halógeno o alquilo inferior sustituido con halógeno; R2 es hidrógeno o alquilo inferior; o R2 forma junto con R4 un anillo heterocíclico de 6 miembros que contiene ¿CH2-CH2-O-CH2- o ¿CH2-CH2-NR-C(O); R es hidrógeno, alquilo inferior, fenilo o bencilo; R3 es fenilo o piridinilo, en el que el átomo de N en el grupo de piridinilo puede estar en diferentes posiciones; R4¿ es hidrógeno, alquilo inferior o alcoxialquilo inferior; R4 es hidrógeno, alquilo inferior, fenilo opcionalmente sustituido con halógeno o alcoxi inferior, o es cicloalquilo, o es piridinilo opcionalmente sustituido con halógeno, alquilo inferior, alcoxi inferior o =O, o es pirimidinilo opcionalmente sustituido con alquilo inferior, alcoxi inferior o =O, o es 1-alquilo inferior-piridinilo, o es pirazinilo, o es piridazinilo opcionalmente sustituido con alquilo inferior, alcoxi inferior o =O, o es 1-metilpirrolo[2,3-b]piridin-5-il, o es 6-imidazo[1,2-b]piridazin-6-il; o R4 forma junto con R4¿ un anillo heterocíclico de 4, 5 o 6 miembros que contiene ¿(CH2)5-, -CH2-CH2-O-CH2-CH2-, -CH2-CH2-CH2-, -CH2-CH2-CH2-CH2-, -CH2-O-CH2-CH2- o CH2-CH2-CH2-O-CH2; R5 y R5¿ son hidrógeno o alquilo inferior; o R4 forma junto con R5 un anillo saturado de 5 miembros que contiene -CH2-CH2-CH2-; o a una sal farmacéuticamente aceptable o sal de adición de ácido, a una mezcla racémica, o a su correspondiente enantiómero y/o isómero óptico y/o estereoisómeros del mismo.
CR20160384A 2014-02-25 2015-02-24 Derivados de etilino CR20160384A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP14156461 2014-02-25
PCT/EP2015/053785 WO2015128307A1 (en) 2014-02-25 2015-02-24 Ethynyl derivatives

Publications (1)

Publication Number Publication Date
CR20160384A true CR20160384A (es) 2016-11-07

Family

ID=50151209

Family Applications (1)

Application Number Title Priority Date Filing Date
CR20160384A CR20160384A (es) 2014-02-25 2015-02-24 Derivados de etilino

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) PH12016501481B1 (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
CN107849006B (zh) 2015-06-03 2020-11-13 豪夫迈·罗氏有限公司 乙炔基衍生物
HUE045145T2 (hu) 2015-07-15 2019-12-30 Hoffmann La Roche Etinil-származékok metabotróp glutamátreceptor-modulátorokként
AR105556A1 (es) 2015-08-03 2017-10-18 Hoffmann La Roche Derivados de etinilo
JP6936305B2 (ja) 2016-07-18 2021-09-15 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft エチニル誘導体

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IN2012DN02580A (es) * 2009-09-04 2015-08-28 Univ Vanderbilt
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
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

Also Published As

Publication number Publication date
EP3110802B1 (en) 2018-10-10
AU2015222303B2 (en) 2019-02-28
US9725416B2 (en) 2017-08-08
IL246842B (en) 2018-11-29
WO2015128307A1 (en) 2015-09-03
HRP20182016T1 (hr) 2019-01-25
PL3110802T3 (pl) 2019-03-29
CN106029649B (zh) 2019-02-12
AR099529A1 (es) 2016-07-27
RS58208B1 (sr) 2019-03-29
CA2938009A1 (en) 2015-09-03
EA201691690A1 (ru) 2016-12-30
KR20160111509A (ko) 2016-09-26
BR112016017816A8 (pt) 2020-06-30
US20160362383A1 (en) 2016-12-15
PH12016501481A1 (en) 2016-08-22
DK3110802T3 (en) 2019-01-07
AU2015222303A1 (en) 2016-09-15
SG11201607010XA (en) 2016-09-29
JP2017506650A (ja) 2017-03-09
UA117855C2 (uk) 2018-10-10
SI3110802T1 (sl) 2019-01-31
PE20161415A1 (es) 2017-01-06
PT3110802T (pt) 2018-12-04
CL2016002064A1 (es) 2017-01-13
KR101792452B1 (ko) 2017-11-01
LT3110802T (lt) 2018-12-27
MX369819B (es) 2019-11-22
TW201546051A (zh) 2015-12-16
ES2701167T3 (es) 2019-02-21
HUE041392T2 (hu) 2019-05-28
TWI576340B (zh) 2017-04-01
EA029261B1 (ru) 2018-02-28
JP6286577B2 (ja) 2018-02-28
CN106029649A (zh) 2016-10-12
PH12016501481B1 (en) 2019-11-08
ZA201605243B (en) 2017-09-27
MA39305A3 (fr) 2018-05-31
MX2016011099A (es) 2016-12-12
EP3110802A1 (en) 2017-01-04

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