CN104936593B - 用于治疗cns疾病的催产素受体激动剂 - Google Patents

用于治疗cns疾病的催产素受体激动剂 Download PDF

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Publication number
CN104936593B
CN104936593B CN201480004903.5A CN201480004903A CN104936593B CN 104936593 B CN104936593 B CN 104936593B CN 201480004903 A CN201480004903 A CN 201480004903A CN 104936593 B CN104936593 B CN 104936593B
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pyrazole
yls
benzsulfamide
base
pyridine
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CN104936593A (zh
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卡泰丽娜·比桑茨
克里斯托夫·格伦德绍博
马蒂亚斯·内特科文
让-马克·普朗谢
沃尔特·维凡
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F Hoffmann La Roche AG
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/415—1,2-Diazoles
    • 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
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further 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
    • 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
    • A61K31/433—Thidiazoles
    • 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
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim 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
    • A61P25/22—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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • 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
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/38—Nitrogen atoms
    • C07D231/42—Benzene-sulfonamido pyrazoles
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
CN201480004903.5A 2013-01-17 2014-01-14 用于治疗cns疾病的催产素受体激动剂 Expired - Fee Related CN104936593B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP13151632 2013-01-17
EP13151632.0 2013-01-17
PCT/EP2014/050526 WO2014111356A1 (en) 2013-01-17 2014-01-14 Oxytocin receptor agonists for the treatment of cns diseases

Publications (2)

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CN104936593A CN104936593A (zh) 2015-09-23
CN104936593B true CN104936593B (zh) 2018-05-18

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CN201480004903.5A Expired - Fee Related CN104936593B (zh) 2013-01-17 2014-01-14 用于治疗cns疾病的催产素受体激动剂

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Country Link
US (1) US9751870B2 (enExample)
EP (1) EP2945624B1 (enExample)
JP (1) JP6263553B2 (enExample)
KR (1) KR20150108384A (enExample)
CN (1) CN104936593B (enExample)
BR (1) BR112015016323A2 (enExample)
CA (1) CA2898015A1 (enExample)
MX (1) MX2015008830A (enExample)
RU (1) RU2664705C2 (enExample)
WO (1) WO2014111356A1 (enExample)

Families Citing this family (7)

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Publication number Priority date Publication date Assignee Title
US10039777B2 (en) 2012-03-20 2018-08-07 Neuro-Lm Sas Methods and pharmaceutical compositions of the treatment of autistic syndrome disorders
US10441627B2 (en) * 2014-09-19 2019-10-15 Ferring B.V. Method of treating prader-willi syndrome
EP3852723B1 (en) 2018-09-20 2025-11-05 ACADIA Pharmaceuticals Inc. Stable intranasal formulations of carbetocin
AU2019345313A1 (en) 2018-09-20 2021-03-18 Levo Therapeutics, Inc. Carbetocin drug product and process for preparing same
WO2020178441A1 (en) * 2019-03-06 2020-09-10 INSERM (Institut National de la Santé et de la Recherche Médicale) Inhibitors of ngal protein
WO2022200568A1 (en) 2021-03-26 2022-09-29 Ot4B Treatment of dysphagia
CN116459261A (zh) * 2023-02-27 2023-07-21 徐州医科大学 Lit-001在治疗焦虑疾病中的应用

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE655242A (enExample) * 1963-11-05 1965-05-04
EP2221298A1 (en) * 2007-11-13 2010-08-25 Taisho Pharmaceutical Co., Ltd Phenylpyrazole derivatives

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3014038A (en) 1961-12-19 Xnhxs
DE1115739B (de) 1958-06-25 1961-10-26 Ciba Geigy Verfahren zur Herstellung von 1-Phenyl-5-(benzolsulfonamido)-pyrazolen
GB893755A (en) 1958-06-25 1962-04-11 Ciba Ltd New pyrazoles and process for their manufacture
GB865341A (en) 1958-07-30 1961-04-12 Bayer Ag 5-benzene-sulphonamido-1-phenyl pyrazole derivatives
DE1115261B (de) 1958-07-30 1961-10-19 Bayer Ag Verfahren zur Herstellung von 1-Phenyl-5-(benzolsulfonamido)-pyrazolen
US6531478B2 (en) * 2000-02-24 2003-03-11 Cheryl P. Kordik Amino pyrazole derivatives useful for the treatment of obesity and other disorders
FR2864958B1 (fr) * 2004-01-12 2006-02-24 Sanofi Synthelabo Derive de n-[(1,5-diphenyl-1h-pyrazol-3-yl)methyl] sulfonamide, leur preparation et leur application en therapeutique.
EP2417123A2 (en) 2009-04-06 2012-02-15 Agios Pharmaceuticals, Inc. Therapeutic compositions and related methods of use
WO2012016229A2 (en) 2010-07-30 2012-02-02 The Regents Of The University Of California Oxytocin treatment to improve memory and modify blood glucose

Patent Citations (2)

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Publication number Priority date Publication date Assignee Title
BE655242A (enExample) * 1963-11-05 1965-05-04
EP2221298A1 (en) * 2007-11-13 2010-08-25 Taisho Pharmaceutical Co., Ltd Phenylpyrazole derivatives

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
4365-68-8;STN;《REGISTRY》;19841116;1 *
93734-53-3;STN;《REGISTRY》;19841218;1 *
PROBING SMALL-MOLECULE BINDING TO CYTOCHROME P450 2D6 AND F2C9:AN IN SILICO PROTOCOL FOR GENERATING TOXICITY ALERTS;ROSSATO ET AL;《CHEMMEDCHEM》;20101231;第5卷;2088-2101 *

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Publication number Publication date
JP2016506910A (ja) 2016-03-07
US20150322058A1 (en) 2015-11-12
KR20150108384A (ko) 2015-09-25
EP2945624A1 (en) 2015-11-25
RU2015130950A (ru) 2017-02-21
JP6263553B2 (ja) 2018-01-17
EP2945624B1 (en) 2018-04-18
CA2898015A1 (en) 2014-07-24
RU2664705C2 (ru) 2018-08-21
MX2015008830A (es) 2015-10-14
CN104936593A (zh) 2015-09-23
US9751870B2 (en) 2017-09-05
HK1209032A1 (en) 2016-03-24
BR112015016323A2 (pt) 2017-07-11
WO2014111356A1 (en) 2014-07-24

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