PE20130155A1 - Derivados de ariletinilo - Google Patents

Derivados de ariletinilo

Info

Publication number
PE20130155A1
PE20130155A1 PE2012002013A PE2012002013A PE20130155A1 PE 20130155 A1 PE20130155 A1 PE 20130155A1 PE 2012002013 A PE2012002013 A PE 2012002013A PE 2012002013 A PE2012002013 A PE 2012002013A PE 20130155 A1 PE20130155 A1 PE 20130155A1
Authority
PE
Peru
Prior art keywords
alcoxy
lower alkyl
cycloalkyl
independently
carbon atom
Prior art date
Application number
PE2012002013A
Other languages
English (en)
Inventor
Luke Green
Wolfgang Guba
Georg Jaeschke
Synese Jolidon
Lothar Lindemann
Antonio Ricci
Daniel Rueher
Heinz Stadler
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 PE20130155A1 publication Critical patent/PE20130155A1/es

Links

Classifications

    • 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
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42Oxazoles
    • A61K31/422Oxazoles not condensed and containing further heterocyclic rings
    • 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
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D401/14Heterocyclic 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
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyridine Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

SE REFIERE A COMPUESTOS DE FORMULA I DONDE: U ES =N- O =C(R5), V ES -CH= O -N=, W ES =CH O =N-, CON LA CONDICION DE QUE UNO SOLAMENTE PUEDA SER N; R5 ES H, METILO O HALOGENO; Y ES -O-, -CH2O-, -CH2S(O)2, ENTRE OTROS; R1 ES FENILO O HETEROARILO OPCIONALMENTE SUSTITUIDOS POR HALOGENO, ALQUILO INFERIOR Y ALCOXI INFERIOR; R2/R2´ JUNTO CON EL ATOMO DE CARBONO AL QUE ESTAN UNIDOS FORMAN CICLOALQUILO C3-C6 O UN ANILLO QUE CONTIENE -CH2OCH2-, O SON INDEPENDIENTEMENTE H, ALQUILO INFERIOR, HIDROXI, ALCOXI INFERIOR, ENTRE OTROS; m ES 0, 1, O 2; CUANDO m ES 1: R3/R3´ JUNTO CON EL ATOMO DE CARBONO AL QUE ESTAN UNIDOS FORMAN CICLOALQUILO C3-C6, O SON INDEPENDIENTEMENTE H, ALQUILO INFERIOR, CH2-ALCOXI INFERIOR; n ES 0 O 1; CUANDO n ES 1: R4/R4´ JUNTO CON EL ATOMO DE CARBONO AL QUE ESTAN UNIDOS FORMAN CICLOALQUILO C3-C6, O SON INDEPENDIENTEMENTE H, ALQUILO INFERIOR, CH2-ALCOXI INFERIOR. REFERIDO ADEMAS A UNA COMPOSICION FARMACEUTICA Y UN PROCEDIMIENTO DE OBTENCION. DICHOS COMPUESTOS SON MODULADORES ALOSTERICOS DE MGLUR5, SIENDO UTILES PARA EL TRATAMIENTO DE ESQUIZOFRENIA, AUTISMO
PE2012002013A 2010-04-13 2011-04-11 Derivados de ariletinilo PE20130155A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP10159754 2010-04-13

Publications (1)

Publication Number Publication Date
PE20130155A1 true PE20130155A1 (es) 2013-02-21

Family

ID=44140916

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2012002013A PE20130155A1 (es) 2010-04-13 2011-04-11 Derivados de ariletinilo

Country Status (33)

Country Link
US (4) US8420661B2 (es)
EP (1) EP2558457B1 (es)
JP (1) JP5559418B2 (es)
KR (1) KR101431367B1 (es)
CN (1) CN102947289B (es)
AR (1) AR080878A1 (es)
AU (1) AU2011240131B2 (es)
BR (1) BR112012026004A2 (es)
CA (1) CA2786216C (es)
CL (1) CL2012002771A1 (es)
CR (1) CR20120480A (es)
CY (1) CY1117441T1 (es)
DK (1) DK2558457T3 (es)
EC (1) ECSP12012212A (es)
ES (1) ES2565761T3 (es)
HR (1) HRP20160617T1 (es)
HU (1) HUE027105T2 (es)
IL (1) IL220982A (es)
MA (1) MA34078B1 (es)
MX (1) MX2012011841A (es)
MY (1) MY160490A (es)
NZ (1) NZ601024A (es)
PE (1) PE20130155A1 (es)
PH (1) PH12012501773A1 (es)
PL (1) PL2558457T3 (es)
RS (1) RS54708B1 (es)
RU (1) RU2573560C2 (es)
SG (1) SG183974A1 (es)
SI (1) SI2558457T1 (es)
TW (1) TWI445706B (es)
UA (1) UA107491C2 (es)
WO (1) WO2011128279A1 (es)
ZA (1) ZA201207285B (es)

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US8420661B2 (en) * 2010-04-13 2013-04-16 Hoffmann-La Roche Inc. Arylethynyl derivatives
PL2702051T3 (pl) * 2011-04-26 2015-08-31 Hoffmann La Roche Pochodne etynylu jako pozytywne allosteryczne modulatory mglur5
US20130123254A1 (en) * 2011-09-30 2013-05-16 Barbara Biemans Pharmaceutically acceptable mglur5 positive allosteric modulators and their methods of identification
UA110862C2 (uk) * 2011-10-07 2016-02-25 Ф. Хоффманн-Ля Рош Аг Похідні етинілу як алостеричні модулятори метаботропного рецептора глутамату mglur 5
EA026593B1 (ru) * 2012-07-17 2017-04-28 Ф. Хоффманн-Ля Рош Аг Арилэтиниловые производные
UA113223C2 (xx) * 2012-08-13 2016-12-26 Арилетинілпіримідини
JP6027251B2 (ja) * 2012-09-27 2016-11-16 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft アリールエチニル誘導体
UA116023C2 (uk) 2013-07-08 2018-01-25 Ф. Хоффманн-Ля Рош Аг Етинільні похідні як антагоністи метаботропного глутаматного рецептора
EP3049409B1 (en) * 2013-09-25 2017-05-03 F. Hoffmann-La Roche AG Ethynyl derivatives
TWI649310B (zh) * 2014-01-10 2019-02-01 赫孚孟拉羅股份公司 乙炔基衍生物
MA39305A3 (fr) * 2014-02-25 2018-05-31 Hoffmann La Roche Dérivés d'éthynyle
CN107207481B (zh) * 2015-03-19 2020-03-03 豪夫迈·罗氏有限公司 作为mglur4的调节剂的3-(4-乙炔基苯基)六氢嘧啶-2,4-二酮衍生物
LT3303316T (lt) * 2015-06-03 2020-05-11 F. Hoffmann-La Roche Ag Etinilo dariniai
ES2733468T3 (es) * 2015-07-15 2019-11-29 Hoffmann La Roche Derivados de etinilo como moduladores de los receptores metabotrópicos de glutamato
AR105556A1 (es) * 2015-08-03 2017-10-18 Hoffmann La Roche Derivados de etinilo
CN106632243B (zh) * 2015-10-28 2019-03-15 华领医药技术(上海)有限公司 吡咯烷衍生物
WO2018015235A1 (en) 2016-07-18 2018-01-25 F. Hoffmann-La Roche Ag Ethynyl derivatives
CN108947883A (zh) * 2017-05-25 2018-12-07 北京万全德众医药生物技术有限公司 布瓦西坦的制备
JP7191045B2 (ja) * 2017-06-02 2022-12-16 エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト 化合物
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SG11202011818YA (en) 2018-06-29 2020-12-30 Hoffmann La Roche Compounds
MA53220A (fr) * 2018-08-13 2021-11-17 Hoffmann La Roche Nouveaux composés hétérocycliques utilisés en tant qu'inhibiteurs de monoacylglycérol lipase
ES2986417T3 (es) 2018-08-13 2024-11-11 Hoffmann La Roche Nuevos compuestos heterocíclicos como inhibidores de la monoacilglicerol lipasa
WO2020048826A1 (en) 2018-09-03 2020-03-12 Bayer Aktiengesellschaft 5-substituted 1-oxa-3,9-diazaspiro[5.5]undecan-2-one compounds
ES2955037T3 (es) 2018-11-22 2023-11-28 Hoffmann La Roche Nuevos compuestos heterocíclicos
CN113993591A (zh) 2019-06-21 2022-01-28 豪夫迈·罗氏有限公司 新egfr抑制剂
CN114008049B (zh) 2019-06-21 2024-07-05 豪夫迈·罗氏有限公司 用于癌症治疗的egfr抑制剂
EP4028403B1 (en) 2019-09-12 2023-11-22 F. Hoffmann-La Roche AG 4,4a,5,7,8,8a-hexapyrido[4,3-b][1,4]oxazin-3-one compounds as magl inhibitors
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UA110862C2 (uk) * 2011-10-07 2016-02-25 Ф. Хоффманн-Ля Рош Аг Похідні етинілу як алостеричні модулятори метаботропного рецептора глутамату mglur 5

Also Published As

Publication number Publication date
CA2786216A1 (en) 2011-10-20
ES2565761T3 (es) 2016-04-06
BR112012026004A2 (pt) 2016-06-28
CY1117441T1 (el) 2017-04-26
IL220982A0 (en) 2012-09-24
US8420661B2 (en) 2013-04-16
MX2012011841A (es) 2012-11-09
DK2558457T3 (en) 2016-03-29
KR20130018294A (ko) 2013-02-20
RU2012145237A (ru) 2014-05-20
TW201136924A (en) 2011-11-01
JP2013523854A (ja) 2013-06-17
KR101431367B1 (ko) 2014-08-20
US8618296B2 (en) 2013-12-31
EP2558457A1 (en) 2013-02-20
IL220982A (en) 2015-09-24
US20130178456A1 (en) 2013-07-11
HRP20160617T1 (hr) 2016-07-01
PH12012501773A1 (en) 2012-11-12
MA34078B1 (fr) 2013-03-05
ECSP12012212A (es) 2012-10-30
SG183974A1 (en) 2012-10-30
AU2011240131A1 (en) 2012-07-19
US9315498B2 (en) 2016-04-19
RU2573560C2 (ru) 2016-01-20
EP2558457B1 (en) 2016-03-09
UA107491C2 (uk) 2015-01-12
US20140155602A1 (en) 2014-06-05
WO2011128279A1 (en) 2011-10-20
SI2558457T1 (sl) 2016-05-31
CR20120480A (es) 2012-10-30
HK1179607A1 (en) 2013-10-04
CL2012002771A1 (es) 2013-04-12
CA2786216C (en) 2017-05-30
AR080878A1 (es) 2012-05-16
CN102947289A (zh) 2013-02-27
TWI445706B (zh) 2014-07-21
MY160490A (en) 2017-03-15
HUE027105T2 (en) 2016-08-29
US8513273B2 (en) 2013-08-20
PL2558457T3 (pl) 2016-09-30
AU2011240131B2 (en) 2015-01-22
CN102947289B (zh) 2014-06-11
US20130274464A1 (en) 2013-10-17
ZA201207285B (en) 2013-06-26
US20110251169A1 (en) 2011-10-13
NZ601024A (en) 2014-08-29
JP5559418B2 (ja) 2014-07-23
RS54708B1 (sr) 2016-08-31

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