CO2018013824A2 - Derivados de etinilo - Google Patents

Derivados de etinilo

Info

Publication number
CO2018013824A2
CO2018013824A2 CONC2018/0013824A CO2018013824A CO2018013824A2 CO 2018013824 A2 CO2018013824 A2 CO 2018013824A2 CO 2018013824 A CO2018013824 A CO 2018013824A CO 2018013824 A2 CO2018013824 A2 CO 2018013824A2
Authority
CO
Colombia
Prior art keywords
compounds
ethynyl derivatives
salt
emesis
neuroprotection
Prior art date
Application number
CONC2018/0013824A
Other languages
English (en)
Inventor
Georg Jaeschke
Fionn O`Hara
Antonio Ricci
Daniel Rueher
Barbara Biemans
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 CO2018013824A2 publication Critical patent/CO2018013824A2/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
    • C07D487/10—Spiro-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
    • A61K31/527—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim spiro-condensed
    • 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
    • A61P39/00—General protective or antinoxious agents
    • 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)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (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)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Toxicology (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La presente invención se refiere a compuestos de fórmulas IA y IB, o a una sal o sal de adición de ácido farmacéuticamente aceptable, a una mezcla racémica o a su enantiómero y/o isómero óptico y/o estereoisómero correspondiente de los mismos. Los compuestos pueden utilizarse en el tratamiento de la enfermedad de Parkinson, la ansiedad, la emesis, el trastorno obsesivo-compulsivo, el autismo, la neuroprotección, el cáncer, la depresión y la diabetes de tipo 2.
CONC2018/0013824A 2016-07-18 2018-12-19 Derivados de etinilo CO2018013824A2 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP16179837 2016-07-18
PCT/EP2017/067495 WO2018015235A1 (en) 2016-07-18 2017-07-12 Ethynyl derivatives

Publications (1)

Publication Number Publication Date
CO2018013824A2 true CO2018013824A2 (es) 2018-12-28

Family

ID=56418435

Family Applications (1)

Application Number Title Priority Date Filing Date
CONC2018/0013824A CO2018013824A2 (es) 2016-07-18 2018-12-19 Derivados de etinilo

Country Status (31)

Country Link
US (3) US20190144458A1 (es)
EP (1) EP3484889B1 (es)
JP (1) JP6936305B2 (es)
KR (1) KR20190026805A (es)
CN (1) CN109476671B (es)
AR (1) AR109075A1 (es)
AU (1) AU2017299083B2 (es)
BR (1) BR112019000314A2 (es)
CA (1) CA3030788A1 (es)
CL (1) CL2019000045A1 (es)
CO (1) CO2018013824A2 (es)
CR (1) CR20190014A (es)
DK (1) DK3484889T3 (es)
ES (1) ES2826389T3 (es)
HR (1) HRP20201615T1 (es)
HU (1) HUE051006T2 (es)
IL (1) IL263884A (es)
LT (1) LT3484889T (es)
MA (1) MA45665B1 (es)
MX (1) MX2019000442A (es)
PE (1) PE20190382A1 (es)
PH (1) PH12019500119A1 (es)
PL (1) PL3484889T3 (es)
PT (1) PT3484889T (es)
RS (1) RS60908B1 (es)
RU (1) RU2745068C2 (es)
SG (1) SG11201811829QA (es)
SI (1) SI3484889T1 (es)
TW (1) TWI729169B (es)
WO (1) WO2018015235A1 (es)
ZA (1) ZA201900113B (es)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107580598B (zh) 2015-07-15 2020-11-13 豪夫迈·罗氏有限公司 作为代谢型谷氨酸受体调节剂的乙炔基衍生物
CN110183456A (zh) * 2019-07-11 2019-08-30 河南师范大学 一种2-芳基吲唑琥珀酰亚胺螺环化合物的合成方法
US11515154B2 (en) * 2020-10-27 2022-11-29 Applied Materials, Inc. Selective deposition of a passivation film

Family Cites Families (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1569915A4 (en) * 2002-12-04 2007-07-11 Merck & Co Inc SPIROCYCLIC UREAS, COMPOSITIONS CONTAINING SAME, AND METHODS OF USE
WO2006125784A1 (en) 2005-05-24 2006-11-30 Laboratoires Serono S.A. Tricyclic spiro derivatives as crth2 modulators
EP2057127B1 (en) 2006-08-31 2012-01-11 Schering Corporation Hydantoin derivatives useful as antibacterial agents
KR20100033981A (ko) 2007-06-03 2010-03-31 벤더르빌트 유니버시티 벤즈아미드 대사성 글루타민산염 수용체5 양성 알로스테릭 조절자 및 이의 제조 및 사용방법
EP2473055A4 (en) 2009-09-04 2013-02-13 Univ Vanderbilt ALLOSTERIC MGLUR4 POTENTIATORS, COMPOSITIONS, AND METHODS OF TREATING NEUROLOGICAL DYSFUNCTIONS
US8389536B2 (en) 2009-10-27 2013-03-05 Hoffmann-La Roche Inc. Positive allosteric modulators (PAM)
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
US8586581B2 (en) 2009-12-17 2013-11-19 Hoffmann-La Roche Inc Ethynyl compounds useful for treatment of CNS disorders
US8420661B2 (en) 2010-04-13 2013-04-16 Hoffmann-La Roche Inc. Arylethynyl derivatives
US8772300B2 (en) 2011-04-19 2014-07-08 Hoffmann-La Roche Inc. Phenyl or pyridinyl-ethynyl derivatives
CA2829170C (en) 2011-04-26 2019-02-26 F. Hoffmann-La Roche Ag Ethynyl derivatives as positive allosteric modulators of the mglur5
US10533000B2 (en) 2011-05-26 2020-01-14 Sunovion Pharmaceuticals, Inc. Metabotrophic glutamate receptor 5 modulators and methods of use thereof
US9540343B2 (en) * 2011-07-06 2017-01-10 Gilead Sciences, Inc. Compounds for the treatment of HIV
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
SG11201501375YA (en) 2012-10-18 2015-03-30 Hoffmann La Roche Ethynyl derivatives as modulators of mglur5 receptor activity
CN104603110B (zh) 2012-10-18 2016-08-31 霍夫曼-拉罗奇有限公司 作为mGluR5受体活性的调节剂的乙炔基衍生物
WO2014124560A1 (en) 2013-02-18 2014-08-21 Hua Medicine (Shanghai) Ltd. Mglur regulators
UY35400A (es) 2013-03-15 2014-10-31 Novartis Ag Compuestos y composiciones para el tratamiento de enfermedades parasitarias
JO3368B1 (ar) 2013-06-04 2019-03-13 Janssen Pharmaceutica Nv مركبات 6، 7- ثاني هيدرو بيرازولو [5،1-a] بيرازين- 4 (5 يد)- اون واستخدامها بصفة منظمات تفارغية سلبية لمستقبلات ميجلور 2
BR112016005994A2 (pt) 2013-09-25 2017-08-01 Hoffmann La Roche derivados de etinila
TWI649310B (zh) 2014-01-10 2019-02-01 赫孚孟拉羅股份公司 乙炔基衍生物
SI3110802T1 (sl) 2014-02-25 2019-01-31 F. Hoffmann-La Roche Ag Derivati etinila
CN104860941B (zh) 2014-02-25 2017-03-22 上海海雁医药科技有限公司 2,4‑二取代苯‑1,5‑二胺衍生物及其应用以及由其制备的药物组合物和药用组合物
EP3271353B1 (en) 2015-03-19 2019-11-27 H. Hoffnabb-La Roche Ag 3-(4-ethynylphenyl)hexahydropyrimidin-2,4-dione derivatives as modulators of mglur4
CN107580598B (zh) * 2015-07-15 2020-11-13 豪夫迈·罗氏有限公司 作为代谢型谷氨酸受体调节剂的乙炔基衍生物
US10391998B2 (en) 2016-11-16 2019-08-27 Ford Global Technologies, Llc Vehicle systems and methods for reducing electrified vehicle noise, vibration, and harshness

Also Published As

Publication number Publication date
PH12019500119A1 (en) 2019-12-11
LT3484889T (lt) 2020-11-10
SI3484889T1 (sl) 2020-11-30
US11242349B2 (en) 2022-02-08
AU2017299083B2 (en) 2021-06-24
MA45665B1 (fr) 2020-11-30
RU2745068C2 (ru) 2021-03-18
CA3030788A1 (en) 2018-01-25
SG11201811829QA (en) 2019-02-27
WO2018015235A1 (en) 2018-01-25
CR20190014A (es) 2019-03-04
AR109075A1 (es) 2018-10-24
EP3484889B1 (en) 2020-08-19
RS60908B1 (sr) 2020-11-30
PT3484889T (pt) 2020-10-15
AU2017299083A1 (en) 2019-01-24
IL263884A (en) 2019-01-31
HRP20201615T1 (hr) 2020-12-11
BR112019000314A2 (pt) 2019-04-16
PL3484889T3 (pl) 2020-12-28
TW201805287A (zh) 2018-02-16
US20200255440A1 (en) 2020-08-13
TWI729169B (zh) 2021-06-01
US20190144458A1 (en) 2019-05-16
CN109476671B (zh) 2021-09-24
CL2019000045A1 (es) 2019-06-07
JP6936305B2 (ja) 2021-09-15
HUE051006T2 (hu) 2021-01-28
DK3484889T3 (da) 2020-10-26
EP3484889A1 (en) 2019-05-22
RU2019102757A (ru) 2020-08-18
CN109476671A (zh) 2019-03-15
MX2019000442A (es) 2019-06-20
RU2019102757A3 (es) 2020-08-18
ES2826389T3 (es) 2021-05-18
KR20190026805A (ko) 2019-03-13
US20220127275A1 (en) 2022-04-28
ZA201900113B (en) 2019-09-25
PE20190382A1 (es) 2019-03-08
JP2019521158A (ja) 2019-07-25

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