HK1206615A1 - 用於治療自閉症的 拮抗劑 - Google Patents

用於治療自閉症的 拮抗劑

Info

Publication number
HK1206615A1
HK1206615A1 HK15107205.9A HK15107205A HK1206615A1 HK 1206615 A1 HK1206615 A1 HK 1206615A1 HK 15107205 A HK15107205 A HK 15107205A HK 1206615 A1 HK1206615 A1 HK 1206615A1
Authority
HK
Hong Kong
Prior art keywords
mglu2
antagonists
treatment
autistic disorders
autistic
Prior art date
Application number
HK15107205.9A
Other languages
English (en)
Inventor
西爾維婭‧加蒂麥克阿瑟
米夏埃爾‧薩克斯
于爾根‧維希曼
托馬斯‧沃爾特林
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 HK1206615A1 publication Critical patent/HK1206615A1/zh

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    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (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)
  • Oil, Petroleum & Natural Gas (AREA)
  • Biophysics (AREA)
  • Molecular Biology (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)
HK15107205.9A 2012-10-23 2015-07-28 用於治療自閉症的 拮抗劑 HK1206615A1 (zh)

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
HK1206615A1 true HK1206615A1 (zh) 2016-01-15

Family

ID=47046481

Family Applications (1)

Application Number Title Priority Date Filing Date
HK15107205.9A HK1206615A1 (zh) 2012-10-23 2015-07-28 用於治療自閉症的 拮抗劑

Country Status (16)

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

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
KR20160143853A (ko) * 2014-04-23 2016-12-14 에프. 호프만-라 로슈 아게 지적 장애의 치료를 위한 mglu2/3 길항제
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
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
RU2708391C2 (ru) 2014-08-01 2019-12-06 Янссен Фармацевтика Нв 6,7-дигидропиразоло[1,5-а]пиразин-4(5h)-оновые соединения и их применение в качестве отрицательных аллостерических модуляторов рецепторов mglur2
CN107001373B (zh) 2014-08-01 2020-01-07 詹森药业有限公司 6,7-二氢吡唑并[1,5-a]吡嗪-4(5H)-酮化合物及其作为MGLUR2受体的负向别构调节剂的用途
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
CA2967153A1 (en) 2014-12-03 2016-06-09 Janssen Pharmaceutica Nv 6,7-dihydropyrazolo[1,5-.alpha.]pyrazin-4(5h)-one compounds and their use as negative allosteric modulators of mglur2 receptors
ES2727158T3 (es) 2014-12-03 2019-10-14 Janssen Pharmaceutica Nv Ligandos para PET de mGluR2 radiomarcados
LT3389727T (lt) 2015-12-18 2020-10-12 Janssen Pharmaceutica Nv Radioaktyviai pažymėti mglur2/3 pet ligandai
WO2017103179A1 (en) 2015-12-18 2017-06-22 Janssen Pharmaceutica Nv Radiolabelled mglur2/3 pet ligands
CN111601811B (zh) 2017-11-24 2023-05-05 住友制药株式会社 6,7-二氢吡唑并[1,5-a]吡嗪酮衍生物和其医药用途
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
CN1195522C (zh) 1999-10-15 2005-04-06 弗·哈夫曼-拉罗切有限公司 苯并二氮杂䓬衍生物
KR100481386B1 (ko) 1999-10-15 2005-04-08 에프. 호프만-라 로슈 아게 벤조디아제핀 유도체
US6916821B2 (en) * 2001-04-02 2005-07-12 Brown University Methods of treating disorders with Group I mGluR antagonists
AU2002307049A1 (en) * 2001-04-02 2002-10-15 Brown University Research Foundation Use of mglur5 antagonists in the manufacture of a medicament in the treatment of autism, mental retardation, schizophrenia
DE60202761T2 (de) 2001-04-12 2006-01-12 F. Hoffmann-La Roche Ag Dihydro-benzo(b)(1,4)diazepin-2-on-derivate als mglur2 antagonisten
DK1379511T3 (da) 2001-04-12 2005-11-07 Hoffmann La Roche Dihydro-benzo[b][1,4]diazepin-2-on-derivater som mGLuR2-antagonister II
US6949542B2 (en) 2002-02-06 2005-09-27 Hoffman-La Roche Inc. Dihydro-benzo[b][1,4]diazepin-2-one derivatives
ATE374030T1 (de) 2003-07-25 2007-10-15 Hoffmann La Roche Kombination eines mglur2 antagonists und eines ache inhibitors zur behandlung von akuten und/oder chronischen neurologischen krankheiten
US7329662B2 (en) 2003-10-03 2008-02-12 Hoffmann-La Roche Inc. Pyrazolo-pyridine
MXPA06014809A (es) 2004-06-21 2007-02-12 Hoffmann La Roche Derivados de pirazol-pirimidina.
WO2006012403A1 (en) * 2004-07-20 2006-02-02 Massachusetts Institute Of Technology Methods of treatment: cell signaling and glutamate release
CN101115755B (zh) 2005-02-11 2013-01-16 弗·哈夫曼-拉罗切有限公司 作为mglur2拮抗剂的吡唑并-嘧啶衍生物
KR100973609B1 (ko) * 2005-03-23 2010-08-03 에프. 호프만-라 로슈 아게 ｍＧｌｕＲ2 길항제로서 아세틸렌일-피라졸로-피리미딘유도체
DE602006013493D1 (de) 2005-09-27 2010-05-20 Hoffmann La Roche Oxadiazolylpyrazolopyrimidine als mglur2-antagonisten
CN101415681A (zh) * 2006-03-29 2009-04-22 弗·哈夫曼-拉罗切有限公司 作为mGluR2拮抗剂的吡啶和嘧啶衍生物
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
RU2015116749A (ru) 2016-12-20
US20170173022A1 (en) 2017-06-22
JP2015534993A (ja) 2015-12-07
AU2013336863A1 (en) 2015-03-19
KR20150070187A (ko) 2015-06-24
SG11201503192XA (en) 2015-06-29
AR093077A1 (es) 2015-05-20
BR112015008297A2 (pt) 2017-07-04
EP2925292A1 (en) 2015-10-07
CA2885808A1 (en) 2014-05-01
US20150252049A1 (en) 2015-09-10
IL237595A0 (en) 2015-04-30
CN104736140A (zh) 2015-06-24
MX2015004604A (es) 2015-10-08
ZA201501677B (en) 2016-02-24
WO2014064028A1 (en) 2014-05-01

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