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

    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D401/14—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
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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
    • 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

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)
HK (1) HK1179607A1 (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)
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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EA022019B1 (ru) * 2011-04-26 2015-10-30 Ф.Хоффманн-Ля Рош Аг Этинильные производные в качестве положительных аллостерических модуляторов 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
CA2871389C (en) * 2012-07-17 2020-08-25 F. Hoffmann-La Roche Ag Arylethynyl derivatives
UA113223C2 (xx) * 2012-08-13 2016-12-26 Арилетинілпіримідини
UA113779C2 (xx) * 2012-09-27 2017-03-10 Похідні арилетинілу
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
PE20161415A1 (es) * 2014-02-25 2017-01-06 Hoffmann La Roche Derivados de etinilo
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
UA120309C2 (uk) * 2015-06-03 2019-11-11 Ф. Хоффманн-Ля Рош Аг Етинільні похідні
KR20180026438A (ko) * 2015-07-15 2018-03-12 에프. 호프만-라 로슈 아게 대사형 글루타메이트 수용체 조절제로서의 에틴일 유도체
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
CR20190014A (es) 2016-07-18 2019-03-04 Hoffmann La Roche Derivados etinilo
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
CA3065874A1 (en) 2017-06-02 2018-12-06 F. Hoffman-La Roche Ag Compounds
AR113299A1 (es) 2017-06-02 2020-04-08 Hoffmann La Roche Compuestos de isoindolina
CA3103166A1 (en) 2018-06-29 2020-01-02 F. Hoffmann-La Roche Ag Compounds
EP3837264A1 (en) * 2018-08-13 2021-06-23 F. Hoffmann-La Roche AG New heterocyclic compounds as monoacylglycerol lipase inhibitors
JP2021534139A (ja) 2018-08-13 2021-12-09 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft モノアシルグリセロールリパーゼ阻害剤としての新規の複素環化合物
WO2020048826A1 (en) 2018-09-03 2020-03-12 Bayer Aktiengesellschaft 5-substituted 1-oxa-3,9-diazaspiro[5.5]undecan-2-one compounds
TW202115070A (zh) 2019-06-21 2021-04-16 瑞士商赫孚孟拉羅股份公司 新穎的egfr抑制劑
CN113993872A (zh) 2019-06-21 2022-01-28 豪夫迈·罗氏有限公司 用于治疗癌症的egfr抑制剂
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Also Published As

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

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