SG11201503192XA - Mglu2/3 antagonists for the treatment of autistic disorders - Google Patents

Mglu2/3 antagonists for the treatment of autistic disorders

Info

Publication number
SG11201503192XA
SG11201503192XA SG11201503192XA SG11201503192XA SG11201503192XA SG 11201503192X A SG11201503192X A SG 11201503192XA SG 11201503192X A SG11201503192X A SG 11201503192XA SG 11201503192X A SG11201503192X A SG 11201503192XA SG 11201503192X A SG11201503192X A SG 11201503192XA
Authority
SG
Singapore
Prior art keywords
mglu2
antagonists
treatment
autistic disorders
autistic
Prior art date
Application number
SG11201503192XA
Inventor
Mcarthur Silvia Gatti
Michael Saxe
Juergen Wichmann
Thomas Woltering
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 SG11201503192XA publication Critical patent/SG11201503192XA/en

Links

Classifications

    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0031—Rectum, anus
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/02—Suppositories; Bougies; Bases therefor; Ovules
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4816—Wall or shell material
    • A61K9/4825—Proteins, e.g. gelatin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds
    • 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
    • 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
    • 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
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2121/00—Preparations for use in therapy
SG11201503192XA 2012-10-23 2013-10-21 Mglu2/3 antagonists for the treatment of autistic disorders SG11201503192XA (en)

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
SG11201503192XA true SG11201503192XA (en) 2015-06-29

Family

ID=47046481

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11201503192XA SG11201503192XA (en) 2012-10-23 2013-10-21 Mglu2/3 antagonists for the treatment of autistic disorders

Country Status (16)

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

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JO3368B1 (en) 2013-06-04 2019-03-13 Janssen Pharmaceutica Nv 6,7-DIHYDROPYRAZOLO[1,5-a]PYRAZIN-4(5H)-ONE COMPOUNDS AND THEIR USE AS NEGATIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
BR112016021727A2 (en) * 2014-04-23 2017-08-15 Hoffmann La Roche MGLU2/3 ANTAGONISTS FOR THE TREATMENT OF INTELLECTUAL DISABILITIES
WO2016016383A1 (en) 2014-08-01 2016-02-04 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 (en) * 2014-08-01 2021-08-17 Janssen Pharmaceutica Nv 6,7-DIHYDROPYRAZOLO[1,5-a]PYRAZIN-4(5H)-ONE COMPOUNDS AND THEIR USE AS NEGATIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
EP3174882B1 (en) 2014-08-01 2018-11-07 Janssen Pharmaceutica NV 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5h)-one compounds and their use as negative allosteric modulators of mglu2 receptors
JO3601B1 (en) * 2014-08-01 2020-07-05 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 (en) 2014-08-01 2021-08-17 Janssen Pharmaceutica Nv 6,7-DIHYDROPYRAZOLO[1,5-a]PYRAZIN-4(5H)-ONE COMPOUNDS AND THEIR USE AS NEGATIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
EP3000814A1 (en) 2014-09-26 2016-03-30 Domain Therapeutics Substituted pyrazoloquinazolinones and pyrroloquinazolinones as allosteric modulators of group II metabotropic glutamate receptors
US10967078B2 (en) 2014-12-03 2021-04-06 Janssen Pharmaceutica Nv Radiolabelled mGluR2 PET ligands
AU2015357167B2 (en) 2014-12-03 2020-06-25 Janssen Pharmaceutica Nv 6,7-dihydropyrazolo(1,5-alpha)pyrazin-4(5H)-one compounds and their use as negative allosteric modulators of mGluR2 receptors
US11045562B2 (en) 2015-12-18 2021-06-29 Janssen Pharmaceutica Nv Radiolabelled mGluR2/3 PET ligands
US11033641B2 (en) 2015-12-18 2021-06-15 Janssen Pharmaceutica Nv Radiolabelled mGluR2/3 pet ligands
CN111601811B (en) 2017-11-24 2023-05-05 住友制药株式会社 6, 7-dihydropyrazolo [1,5-a ] pyrazinone derivatives and medical uses thereof
GB202106872D0 (en) * 2021-05-13 2021-06-30 Addex Pharmaceuticals Sa Novel compounds

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU779874B2 (en) 1999-10-15 2005-02-17 F. Hoffmann-La Roche Ag Benzodiazepine derivatives
RU2259360C2 (en) 1999-10-15 2005-08-27 Ф.Хоффманн-Ля Рош Аг Derivatives of benzodiazepine and medicinal agent comprising thereof
US6916821B2 (en) * 2001-04-02 2005-07-12 Brown University Methods of treating disorders with Group I mGluR antagonists
DE60214846T2 (en) * 2001-04-02 2007-05-16 Brown University Research Foundation Use of mGLuR5 antagonists for the manufacture of medicaments for the treatment of sensitive X syndromes, autism and mental retardation
ATE299868T1 (en) 2001-04-12 2005-08-15 Hoffmann La Roche DIHYDRO-BENZO (B) (1,4) DIAZEPINE-2-ONE DERIVATIVES AS MGLUR2 ANTAGONISTS
KR100566178B1 (en) 2001-04-12 2006-03-29 에프. 호프만-라 로슈 아게 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
RU2357734C2 (en) 2003-07-25 2009-06-10 Ф.Хоффманн-Ля Рош Аг COMBINATION OF mGluR2 RECEPTOR ANTAGONIST AND AChE ENZYME INHIBITOR FOR ACUTE ANDN/OR CHRONIC NEURALGIC DISEASES
US7329662B2 (en) 2003-10-03 2008-02-12 Hoffmann-La Roche Inc. Pyrazolo-pyridine
WO2005123738A1 (en) 2004-06-21 2005-12-29 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
RU2402553C2 (en) 2005-02-11 2010-10-27 Ф. Хоффманн-Ля Рош Аг PYRAZOLE-PYRIMIDINE DERIVATIVES AS mGluR2 ANTAGONISTS
KR100968989B1 (en) 2005-03-23 2010-07-09 에프. 호프만-라 로슈 아게 Acetylenyl-pyrazolo-pyrimidine derivatives as mglur2 antagonists
CN101273040B (en) 2005-09-27 2011-11-09 弗·哈夫曼-拉罗切有限公司 Oxadiazolyl pyrazolo-pyrimidines as MGLUR2 antagonists
PL2001849T3 (en) 2006-03-29 2015-04-30 Hoffmann La Roche Pyridine and pyrimidine derivatives as mglur2 antagonists
US8012986B2 (en) 2007-04-02 2011-09-06 Hoffmann-La Roche Inc. Pyridine and pyrimidine derivatives as MGLUR2 antagonists
US8765784B2 (en) * 2010-06-09 2014-07-01 Merck Sharp & Dohme Corp. Positive allosteric modulators of MGLUR2

Also Published As

Publication number Publication date
US20170173022A1 (en) 2017-06-22
JP2015534993A (en) 2015-12-07
KR20150070187A (en) 2015-06-24
RU2015116749A (en) 2016-12-20
WO2014064028A1 (en) 2014-05-01
MX2015004604A (en) 2015-10-08
ZA201501677B (en) 2016-02-24
US20150252049A1 (en) 2015-09-10
IL237595A0 (en) 2015-04-30
CN104736140A (en) 2015-06-24
AR093077A1 (en) 2015-05-20
AU2013336863A1 (en) 2015-03-19
BR112015008297A2 (en) 2017-07-04
HK1206615A1 (en) 2016-01-15
CA2885808A1 (en) 2014-05-01
EP2925292A1 (en) 2015-10-07

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