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MX2015004604A - Antagonistas de los receptores metabotropicos de glutamato 2/3 (mglu2/3) para el tratamiento de los trastornos autistas. - Google Patents

Antagonistas de los receptores metabotropicos de glutamato 2/3 (mglu2/3) para el tratamiento de los trastornos autistas.

Info

Publication number
MX2015004604A
MX2015004604A MX2015004604A MX2015004604A MX2015004604A MX 2015004604 A MX2015004604 A MX 2015004604A MX 2015004604 A MX2015004604 A MX 2015004604A MX 2015004604 A MX2015004604 A MX 2015004604A MX 2015004604 A MX2015004604 A MX 2015004604A
Authority
MX
Mexico
Prior art keywords
treatment
mglu2
antagonists
relates
autistic disorders
Prior art date
Application number
MX2015004604A
Other languages
English (en)
Inventor
Thomas Woltering
Juergen Wichmann
Silvia Gatti Mcarthur
Michael Saxe
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 MX2015004604A publication Critical patent/MX2015004604A/es

Links

Classifications

    • 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
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0031Rectum, anus
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0087Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/02Suppositories; Bougies; Bases therefor; Ovules
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1629Organic macromolecular compounds
    • A61K9/1652Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4816Wall or shell material
    • A61K9/4825Proteins, e.g. gelatin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4858Organic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4866Organic macromolecular compounds
    • 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
    • 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2121/00Preparations for use in therapy

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Dermatology (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La presente invención se refiere a un nuevo uso médico para determinados compuestos químicos y composiciones farmacéuticas que los contienen. La invención se refiere a compuestos que son moduladores alostéricos negativos de mGlu2/3 para el uso en el tratamiento de TEA, en particular el autismo. En otro aspecto, la invención se refiere a una composición farmacéutica para el uso en el tratamiento de TEA que comprende un compuesto de acuerdo con la invención y un portador farmacéuticamente aceptable.
MX2015004604A 2012-10-23 2013-10-21 Antagonistas de los receptores metabotropicos de glutamato 2/3 (mglu2/3) para el tratamiento de los trastornos autistas. MX2015004604A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP12189553 2012-10-23
PCT/EP2013/071921 WO2014064028A1 (en) 2012-10-23 2013-10-21 Mglu2/3 antagonists for the treatment of autistic disorders

Publications (1)

Publication Number Publication Date
MX2015004604A true MX2015004604A (es) 2015-10-08

Family

ID=47046481

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2015004604A MX2015004604A (es) 2012-10-23 2013-10-21 Antagonistas de los receptores metabotropicos de glutamato 2/3 (mglu2/3) para el tratamiento de los trastornos autistas.

Country Status (16)

Country Link
US (2) US20150252049A1 (es)
EP (1) EP2925292A1 (es)
JP (1) JP2015534993A (es)
KR (1) KR20150070187A (es)
CN (1) CN104736140A (es)
AR (1) AR093077A1 (es)
AU (1) AU2013336863A1 (es)
BR (1) BR112015008297A2 (es)
CA (1) CA2885808A1 (es)
HK (1) HK1206615A1 (es)
IL (1) IL237595A0 (es)
MX (1) MX2015004604A (es)
RU (1) RU2015116749A (es)
SG (1) SG11201503192XA (es)
WO (1) WO2014064028A1 (es)
ZA (1) ZA201501677B (es)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
CA2943877A1 (en) * 2014-04-23 2015-10-29 F. Hoffmann-La Roche Ag Mglu2/3 antagonists for the treatment of intellectual disabilities
US10220032B2 (en) 2014-08-01 2019-03-05 Janssen Pharmaceutica Nv 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one compounds and their use as negative allosteric modulators of mGluR2 receptors
JOP20150177B1 (ar) 2014-08-01 2021-08-17 Janssen Pharmaceutica Nv مركبات 6 ، 7 ثاني هيدرو بيرازولو [ 1، 5 الفا ] بيرازين – 4 (5 يد) – اون واستخدامها كمنظمات الوسترية سلبية لمستقبلات ملجور 2
JO3601B1 (ar) * 2014-08-01 2020-07-05 Janssen Pharmaceutica Nv مركبات 6 ، 7 ثاني هيدرو بيرازولو [ 1، 5 الفا ] بيرازين – 4 (5 يد) – اون واستخدامها كمنظمات الوسترية سلبية لمستقبلات ملجور 2
US10017514B2 (en) 2014-08-01 2018-07-10 Janssen Pharmaceutica Nv 6,7-dihydropyrazolo[1,5-α]pyrazin-4(5H)-one compounds and their use as negative allosteric modulators of mGluR2 receptors
JOP20150179B1 (ar) 2014-08-01 2021-08-17 Janssen Pharmaceutica Nv مركبات 6 ، 7 ثاني هيدرو بيرازولو [ 1، 5 الفا ] بيرازين – 4 (5 يد) – اون واستخدامها كمنظمات الوسترية سلبية لمستقبلات ملجور 2
EP3000814A1 (en) 2014-09-26 2016-03-30 Domain Therapeutics Substituted pyrazoloquinazolinones and pyrroloquinazolinones as allosteric modulators of group II metabotropic glutamate receptors
JP6689856B2 (ja) 2014-12-03 2020-04-28 ヤンセン ファーマシューティカ エヌ.ベー. 6,7−ジヒドロピラゾロ[1,5−a]ピラジン−4(5H)−オン化合物およびMGLUR2受容体の負のアロステリック調節因子としてのそれらの使用
AU2015357169B2 (en) 2014-12-03 2021-03-04 Janssen Pharmaceutica Nv Radiolabelled mGluR2 PET ligands
PT3389727T (pt) 2015-12-18 2020-10-30 Janssen Pharmaceutica Nv Ligantes pet de mglur2/3 radiomarcados
US11045562B2 (en) 2015-12-18 2021-06-29 Janssen Pharmaceutica Nv Radiolabelled mGluR2/3 PET ligands
ES2991283T3 (es) 2017-11-24 2024-12-03 Sumitomo Pharma Co Ltd Derivado de 6,7-dihidropirazolo[1,5-a]pirazinona y aplicación médica del mismo
GB202106872D0 (en) * 2021-05-13 2021-06-30 Addex Pharmaceuticals Sa Novel compounds

Family Cites Families (17)

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HUP0203142A3 (en) 1999-10-15 2003-03-28 Hoffmann La Roche Benzodiazepine derivatives, process for preparation of the compounds, pharmaceutical compositions containing them and their use
SI1224175T1 (en) 1999-10-15 2004-08-31 F. Hoffmann-La Roche Ag Benzodiazepine derivatives as metabotropic glutamate receptor antagonists
US6890931B2 (en) * 2001-04-02 2005-05-10 Brown University Methods of treating disorders with group I mGluR antagonists
US6916821B2 (en) * 2001-04-02 2005-07-12 Brown University Methods of treating disorders with Group I mGluR antagonists
DK1379511T3 (da) 2001-04-12 2005-11-07 Hoffmann La Roche Dihydro-benzo[b][1,4]diazepin-2-on-derivater som mGLuR2-antagonister II
SI1379522T1 (en) 2001-04-12 2005-04-30 F. Hoffmann-La Roche Ag DIHYDRO-BENZO(b)(1,4)DIAZEPIN-2-ONE DERIVATIVES AS MGLUR2 ANTAGONISTS I
US6949542B2 (en) 2002-02-06 2005-09-27 Hoffman-La Roche Inc. Dihydro-benzo[b][1,4]diazepin-2-one derivatives
EP1651234B1 (en) 2003-07-25 2007-09-26 F. Hoffmann-La Roche Ag Combination of mglur2 antagonist and ache inhibitor for treatment of acute and/or chronic neurological disorders
US7329662B2 (en) 2003-10-03 2008-02-12 Hoffmann-La Roche Inc. Pyrazolo-pyridine
EP1761541B1 (en) 2004-06-21 2008-01-09 F.Hoffmann-La Roche Ag Pyrrazolo-pyrimidine derivatives
WO2006012403A1 (en) * 2004-07-20 2006-02-02 Massachusetts Institute Of Technology Methods of treatment: cell signaling and glutamate release
BRPI0607927A2 (pt) 2005-02-11 2009-10-20 Hoffmann La Roche derivados de pirazol-pirimidina
KR100973609B1 (ko) * 2005-03-23 2010-08-03 에프. 호프만-라 로슈 아게 mGluR2 길항제로서 아세틸렌일-피라졸로-피리미딘유도체
CN101273040B (zh) 2005-09-27 2011-11-09 弗·哈夫曼-拉罗切有限公司 作为mglur2拮抗剂的*二唑基吡唑并嘧啶类化合物
RU2451673C2 (ru) 2006-03-29 2012-05-27 Ф. Хоффманн-Ля Рош Аг ПРОИЗВОДНЫЕ ПИРИДИНА И ПИРИМИДИНА В КАЧЕСТВЕ АНТАГОНИСТОВ mGluR2
US8012986B2 (en) 2007-04-02 2011-09-06 Hoffmann-La Roche Inc. Pyridine and pyrimidine derivatives as MGLUR2 antagonists
WO2011156245A2 (en) * 2010-06-09 2011-12-15 Merck Sharp & Dohme Corp. Positive allosteric modulators of mglur2

Also Published As

Publication number Publication date
RU2015116749A (ru) 2016-12-20
US20150252049A1 (en) 2015-09-10
WO2014064028A1 (en) 2014-05-01
CA2885808A1 (en) 2014-05-01
AU2013336863A1 (en) 2015-03-19
US20170173022A1 (en) 2017-06-22
ZA201501677B (en) 2016-02-24
KR20150070187A (ko) 2015-06-24
HK1206615A1 (en) 2016-01-15
CN104736140A (zh) 2015-06-24
IL237595A0 (en) 2015-04-30
SG11201503192XA (en) 2015-06-29
BR112015008297A2 (pt) 2017-07-04
JP2015534993A (ja) 2015-12-07
AR093077A1 (es) 2015-05-20
EP2925292A1 (en) 2015-10-07

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