RS50767B - Piperidinski derivati kao antagonisti nmda receptora - Google Patents

Piperidinski derivati kao antagonisti nmda receptora

Info

Publication number
RS50767B
RS50767B YUP-1039/03A YUP103903A RS50767B RS 50767 B RS50767 B RS 50767B YU P103903 A YUP103903 A YU P103903A RS 50767 B RS50767 B RS 50767B
Authority
RS
Serbia
Prior art keywords
alkyl
group
oxo
thioxo
groups
Prior art date
Application number
YUP-1039/03A
Other languages
English (en)
Inventor
István BORZA
Csilla HORVÁTH
Sándor FARKAS
József Nagy
Sándor KOLOK
István VÁGO
György DOMÁNY
Gizella BARTÁNÉ SZALAI
György Keseru
Éva KOVÁCSNÉ BOZÓ
Attila Bielik
Györgyi IGNÁCZNÉ SZENDREI
Original Assignee
Richter Gedeon Vegyeszeti Gyar Rt.
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
Priority claimed from HU0103055A external-priority patent/HU226978B1/hu
Priority claimed from HU0202213A external-priority patent/HU225905B1/hu
Application filed by Richter Gedeon Vegyeszeti Gyar Rt. filed Critical Richter Gedeon Vegyeszeti Gyar Rt.
Publication of RS103903A publication Critical patent/RS103903A/sr
Publication of RS50767B publication Critical patent/RS50767B/sr

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/10Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms
    • C07D211/14Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
    • 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
    • A61K47/26Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • 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
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • 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
    • A61K9/10Dispersions; Emulsions
    • 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
    • A61K9/19Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
    • 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
    • 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
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • 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
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32Alcohol-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/16Otologicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/10Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms
    • C07D211/16Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with acylated ring nitrogen atom
    • 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
    • C07D401/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Ophthalmology & Optometry (AREA)
  • Virology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Molecular Biology (AREA)
  • Psychology (AREA)
  • Communicable Diseases (AREA)
  • Pulmonology (AREA)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Biochemistry (AREA)
  • Emergency Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)

Abstract

Novi derivati amida karboksilne kiseline formule (I) gdei -(CHRl)m- i -(CHR2)n- predstavljaju -CH2-CH2 grupe, gde susedne V i U grupe grade zajedno i sa jednim ili više istih ili različitih dodatnih heteroatoma i -CH= i/ ili -CH2 grupama, ili 4-7 -očlani homo ili heterociklični prsten, koji je po mogućstvu supstituisan sa okso, tiokso, metil ili trifluorometil, najbolje morfolin, pirol, pirolidin, okso- ili tiokso-pirolidin, pirazol, pirazolidin, imidazol, imidazolidin, okso- ili tiokso-imidazol ili imidazolidin, 1,4-oksazin, oksazol, oksazolidin, okso- ili tiokso-oksazolidin, ili 3-okso-l,4-oksazinski prsten,gde X predstavlja -CO grupu,W je -CO-, -CH2, ili -CH(alkil)-grupa- u kojoj je alkil C1-4 alkil grupa, Y je kiseonikov atom, kao i C1-C4 alkilen, C2-C4 alkinilen, cikloalkilen, aminokarbonil, -NH-, -N(alkil)-, -CH20-, -CH(OH)-, -OCH2- grupa, u kojoj je Cl-4 alkil grupa,Z je vodonik ili atom halogena, nitro, amino, C1-C4 alkil, C1-C4 alkoksi, cijano, triflurometil, hidroksilna ili karboksilna grupa,i optički antipodi ili racemati i/ ili farmaceutski prihvatljive soli koje se grade sa kiselinama i bazama.Prijava sadrži još 9 patentnih zahteva.
YUP-1039/03A 2001-07-24 2002-07-23 Piperidinski derivati kao antagonisti nmda receptora RS50767B (sr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
HU0103055A HU226978B1 (en) 2001-07-24 2001-07-24 New carboxylic acid amide compounds, process for their preparation and pharmaceutical compositions containing them and their use
HU0202213A HU225905B1 (en) 2002-07-10 2002-07-10 Solid-supported parallel synthesis of new carboxylic acid amide derivatives
PCT/HU2002/000071 WO2003010159A1 (en) 2001-07-24 2002-07-23 Piperidine derivatives as nmda receptor antagonists

Publications (2)

Publication Number Publication Date
RS103903A RS103903A (en) 2007-02-05
RS50767B true RS50767B (sr) 2010-08-31

Family

ID=90001553

Family Applications (1)

Application Number Title Priority Date Filing Date
YUP-1039/03A RS50767B (sr) 2001-07-24 2002-07-23 Piperidinski derivati kao antagonisti nmda receptora

Country Status (33)

Country Link
US (1) US7435744B2 (sr)
EP (1) EP1409477B1 (sr)
JP (1) JP4322113B2 (sr)
KR (1) KR100890676B1 (sr)
CN (1) CN100413860C (sr)
AT (1) ATE408611T1 (sr)
AU (1) AU2002313566B2 (sr)
BG (1) BG66441B1 (sr)
BR (1) BR0211393A (sr)
CA (1) CA2453383C (sr)
CO (1) CO5560570A2 (sr)
CY (1) CY1109401T1 (sr)
CZ (1) CZ2004233A3 (sr)
DE (1) DE60228969D1 (sr)
DK (1) DK1409477T3 (sr)
EA (1) EA010162B1 (sr)
EE (1) EE05429B1 (sr)
ES (1) ES2312603T3 (sr)
HK (1) HK1063464A1 (sr)
HR (1) HRP20040178B1 (sr)
IL (1) IL159393A (sr)
IS (1) IS7066A (sr)
MX (1) MXPA04000737A (sr)
NO (1) NO327099B1 (sr)
NZ (1) NZ530055A (sr)
PL (1) PL216636B1 (sr)
PT (1) PT1409477E (sr)
RS (1) RS50767B (sr)
SI (1) SI1409477T1 (sr)
SK (1) SK287726B6 (sr)
UA (1) UA77684C2 (sr)
WO (1) WO2003010159A1 (sr)
ZA (1) ZA200400417B (sr)

Families Citing this family (49)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10210779A1 (de) * 2002-03-12 2003-10-09 Merck Patent Gmbh Cyclische Amide
PA8575901A1 (es) * 2002-07-18 2004-07-20 Pfizer Prod Inc Derivados de piperidina novedosos
ES2222833B1 (es) * 2003-07-30 2006-03-01 Laboratorios Del Dr. Esteve, S.A. Compuestos piperidinicos 1,4-disustituidos, su preparacion y su uso como medicamentos.
MXPA06002853A (es) 2003-09-11 2006-06-14 Kemia Inc Inhibidores citoquina.
WO2005030720A1 (ja) * 2003-09-25 2005-04-07 Shionogi & Co., Ltd. Nmda受容体拮抗作用を有するピペリジン誘導体
WO2005039564A1 (en) * 2003-10-02 2005-05-06 Vertex Pharmaceuticals Incorporated Phthalimide compounds useful as protein kinase inhibitors
HUP0401522A2 (en) * 2004-07-29 2006-04-28 Richter Gedeon Vegyeszet New 4-benzylidene-piperidine derivatives, pharmaceutical compositions containing the same and process for their preparation
HU227000B1 (en) * 2004-07-29 2010-04-28 Richter Gedeon Nyrt Nmda receptor antagonist benzoyl urea derivatives, and pharmaceutical compositions containing them
EP2520567A3 (en) 2006-02-23 2012-12-12 Shionogi & Co., Ltd. Nitrogen-containing heterocycle derivatives substituted with cyclic group
HUP0600810A3 (en) * 2006-10-27 2008-09-29 Richter Gedeon Nyrt New sulfonamide derivatives as bradykinin antagonists, process and intermediates for their preparation and pharmaceutical compositions containing them
HUP0600808A3 (en) * 2006-10-27 2008-09-29 Richter Gedeon Nyrt New benzamide derivatives as bradykinin antagonists, process for their preparation and pharmaceutical compositions containing them
HUP0600809A3 (en) * 2006-10-27 2008-09-29 Richter Gedeon Nyrt New phenylsulfamoyl-benzamide derivatives as bradykinin antagonists, process and intermediates for their preparation and pharmaceutical compositions containing them
EP1918281A1 (en) * 2006-11-02 2008-05-07 Laboratorios del Dr. Esteve S.A. Phenylamino-substituted piperidine compounds, their preparation and use as medicaments
JP5379692B2 (ja) 2006-11-09 2013-12-25 プロビオドルグ エージー 潰瘍、癌及び他の疾患の治療のためのグルタミニルシクラーゼの阻害薬としての3−ヒドロキシ−1,5−ジヒドロ−ピロール−2−オン誘導体
JP5523107B2 (ja) 2006-11-30 2014-06-18 プロビオドルグ エージー グルタミニルシクラーゼの新規阻害剤
ZA200905537B (en) 2007-03-01 2010-10-27 Probiodrug Ag New use of glutaminyl cyclase inhibitors
ES2533484T3 (es) 2007-04-18 2015-04-10 Probiodrug Ag Derivados de tiourea como inhibidores de la glutaminil ciclasa
EP2184272A4 (en) * 2007-08-21 2011-11-09 Shionogi & Co PIPERAZINE DERIVATIVE
DE102007047737A1 (de) * 2007-10-05 2009-04-30 Merck Patent Gmbh Piperidin- und Piperazinderivate
US20100298299A1 (en) * 2007-10-27 2010-11-25 Istvan Vago non-peptide derivatives as bradykinin b1 antagonists
US20100010044A1 (en) * 2008-07-08 2010-01-14 Forest Laboratories Holdings Limited Novel crystalline form of 2-[4-(4-fluoro-benzyl)-piperidine-1-yl]-2-oxo-n-(2-oxo-2,3-dihydro-benzoxazol-6-yl)-acetamide
US20100048629A1 (en) * 2008-08-21 2010-02-25 Allyson Gage Methods for treating neuropathic pain
AU2009282822A1 (en) * 2008-08-21 2010-02-25 Richter Gedeon Nyrt. Methods for treating CNS disorders
US8691866B2 (en) 2008-12-10 2014-04-08 The General Hospital Corporation HIF inhibitors and use thereof
HUP0900130A3 (en) 2009-03-03 2012-02-28 Richter Gedeon Nyrt Novel crystalline hydrate, amorphous and polymorphic forms of dihydro-benzoxazole-6-yl-acetamide derivative and processes for their preparation
EA022007B1 (ru) 2009-09-11 2015-10-30 Пробиодруг Аг Гетероциклические производные в качестве ингибиторов глутаминилциклазы
SG181733A1 (en) * 2009-12-15 2012-07-30 Neurop Inc Compounds for the treatment of neurologic disorders
CN102762554A (zh) 2010-02-16 2012-10-31 辉瑞大药厂 5-ht4受体的部分激动剂(r)-4-((4-((4-(四氢呋喃-3-基氧基)苯并[d]异*唑-3-基氧基)甲基)哌啶-1-基)甲基)四氢-2h-吡喃-4-醇
JP6026284B2 (ja) 2010-03-03 2016-11-16 プロビオドルグ エージー グルタミニルシクラーゼの阻害剤
KR101790806B1 (ko) 2010-03-10 2017-11-20 프로비오드룩 아게 글루타미닐 사이클라제(qc, ec 2.3.2.5)의 헤테로사이클릭 억제제
EP2560953B1 (en) 2010-04-21 2016-01-06 Probiodrug AG Inhibitors of glutaminyl cyclase
HUP1000424A2 (en) 2010-08-11 2012-05-02 Richter Gedeon Nyrt Use of radiprodil in attention deficit hyperactivity disorder
WO2012123563A1 (en) 2011-03-16 2012-09-20 Probiodrug Ag Benz imidazole derivatives as inhibitors of glutaminyl cyclase
DK2921491T3 (da) * 2011-12-27 2017-11-27 Bayer Ip Gmbh Mellemforbindelser til fremstilling af heteroarylpiperidiner og ¿piperazinderivater som fungicider
AU2013251079B2 (en) 2012-04-20 2017-03-23 Ucb Pharma S.A. Methods for treating Parkinson's disease
US9868730B2 (en) 2013-02-18 2018-01-16 The Trustees Of Columbia University In The City Of New York Kappa opioid receptor selective compounds, compositions, and uses thereof
JP2017538678A (ja) * 2014-11-05 2017-12-28 フレクサス・バイオサイエンシーズ・インコーポレイテッドFlexus Biosciences, Inc. 免疫調節剤
UY36390A (es) 2014-11-05 2016-06-01 Flexus Biosciences Inc Compuestos moduladores de la enzima indolamina 2,3-dioxigenasa (ido), sus métodos de síntesis y composiciones farmacéuticas que los contienen
EP3353161B1 (en) * 2015-09-25 2021-07-21 The United States of America, as represented by the Secretary, Department of Health and Human Services Triazole derivatives as p2y14 receptor antagonists
PL3461819T3 (pl) 2017-09-29 2020-11-30 Probiodrug Ag Inhibitory cyklazy glutaminylowej
PE20211454A1 (es) 2017-12-08 2021-08-05 Boehringer Ingelheim Int Derivados de imidazopiridina y su uso como medicamento
US20200352931A1 (en) * 2017-12-12 2020-11-12 Phenex Discovery Verwaltungs-GmbH Oxalamides as modulators of indoleamine 2,3-dioxygenase
JP7093470B2 (ja) * 2018-10-17 2022-06-29 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 4-ピリミジン-5-イルメチル-モルホリン誘導体および医薬としてのその使用
WO2020079042A1 (en) 2018-10-17 2020-04-23 Boehringer Ingelheim International Gmbh 4-pyridinylmethyl-morpholine derivatives and the use thereof as medicament
BR112021004993A2 (pt) 2018-10-17 2021-06-08 Boehringer Ingelheim International Gmbh derivados de 4-pirqazin-2-ilmetil-morfolina e o uso dos mesmos com medicamento
JP7318015B2 (ja) 2019-06-04 2023-07-31 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 特に抑うつ病性障害の処置のための、nr2bネガティブ調節剤としてのプリン誘導体および医薬としてのその使用
CN113234036B (zh) * 2021-05-12 2023-07-14 斯莱普泰(上海)生物医药科技有限公司 Nmda受体拮抗剂及其用途
KR20240052765A (ko) 2021-08-06 2024-04-23 그린 테라퓨틱스 인코포레이티드 라디프로딜의 제형
CN114163388A (zh) * 2021-12-15 2022-03-11 陕西汉江药业集团股份有限公司 芬苯达唑中的杂质i、杂质ⅱ和杂质ⅲ的制备方法

Family Cites Families (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE254999C (sr)
US2324123A (en) 1941-07-08 1943-07-13 Eastman Kodak Co Fog inhibitor for photographic developers
US3260723A (en) 1963-08-27 1966-07-12 Parke Davis & Co 4-phenoxy piperidines; alpha4-phenoxy piperideines
NL6501323A (sr) 1965-02-02 1966-08-03
US3632767A (en) 1968-02-12 1972-01-04 Mallinckrodt Chemical Works Treatment of depression with 4-substituted piperidines
AU639529B2 (en) 1987-03-04 1993-07-29 Higuchi, Yoshinari Carbostyril derivatives and salts thereof and anti-arrhythmic agents containing the carbostyril derivatives
SK232890A3 (en) 1989-05-17 1998-11-04 Pfizer 2-piperidino and 2-pyrrolidino-1-alkanols derivatives and preparation method thereof
FR2672286B1 (fr) * 1991-01-31 1994-11-18 Synthelabo Derives de 1-(4-chlorophenyl)-2-[4-(phenylmethyl)piperidin-1-yl]ethanol, leur preparation et leur application en therapeutique.
US5436255A (en) 1992-07-23 1995-07-25 Pfizer Inc. Method of treating diseases susceptable to treatment by blocking NMDA-receptors
TW281670B (sr) * 1993-09-02 1996-07-21 Hoffmann La Roche
ZA9610745B (en) 1995-12-22 1997-06-24 Warner Lambert Co 4-Subsituted piperidine analogs and their use as subtype selective nmda receptor antagonists
ZA9610738B (en) 1995-12-22 1997-06-24 Warner Lambert Co Subtype selective nmda receptor ligands and the use thereof
ZA9610741B (en) 1995-12-22 1997-06-24 Warner Lambert Co 4-Substituted piperidine analogs and their use as subtype selective nmda receptor antagonists
ZA9610736B (en) 1995-12-22 1997-06-27 Warner Lambert Co 2-Substituted piperidine analogs and their use as subtypeselective nmda receptor antagonists
AU1463997A (en) 1995-12-22 1997-07-17 Acea Pharmaceuticals, Inc. Subtype-selective nmda receptor ligands and the use thereof
TW498067B (en) * 1996-07-19 2002-08-11 Hoffmann La Roche 4-hydroxy-piperidine derivatives
DE19643790A1 (de) 1996-10-30 1998-05-07 Merck Patent Gmbh Benzoxazol-Derivat
US6048900A (en) * 1998-02-13 2000-04-11 Bayer Corporation Amide derivatives and methods for using the same as selective neuropeptide Y receptor antagonists
JP2000510870A (ja) * 1997-02-14 2000-08-22 バイエル・コーポレーシヨン Npy5受容体アンタゴニストとしてのアミド類
HUP0004900A3 (en) 1997-10-24 2002-03-28 Warner Lambert Co Pharmaceutical compositions for treating disease-related or drug-induced dyskinesias containing piperidine derivatives as nmda receptor antagonist as active ingredient
PE20000728A1 (es) 1998-06-26 2000-08-21 Cocensys Inc Heterociclos 4-bencil piperidina alquilsulfoxido y su uso como antagonistas receptores subtipo-selectivo nmda
US6553849B1 (en) 1998-10-28 2003-04-29 Dillon F. Scofield Electrodynamic particle size analyzer
US6399631B1 (en) * 1999-07-23 2002-06-04 Pfizer Inc. Carbazole neuropeptide Y5 antagonists
US6489477B1 (en) 1999-10-29 2002-12-03 Merck & Co., Inc. 2-aza-bicyclo[2.2.2]octane NMDA/NR2B antigonists
US6369076B1 (en) 1999-10-29 2002-04-09 Merck & Co. Inc. 5-benzyl-octahydroindole and 6-benzyl-decahydroquinoline NMDA/NR2B antagonists
US6476041B1 (en) 1999-10-29 2002-11-05 Merck & Co., Inc. 1,4 substituted piperidinyl NMDA/NR2B antagonists
JP2003512422A (ja) 1999-10-29 2003-04-02 メルク シャープ エンド ドーム リミテッド ベンズイミダゾールnmda/nr2bアンタゴニストを使用する疼痛の治療方法
US6432976B1 (en) 1999-10-29 2002-08-13 Merck & Co., Inc. 8-aza-bicyclo[3.2.1]octane NMDA/NR2B antagonists
US6291499B1 (en) 1999-10-29 2001-09-18 Merck & Co., Inc. 2-cyclohexyl benzimidazole NMDA/NR2B antagonists
US6316474B1 (en) 1999-10-29 2001-11-13 Merck & Co., Inc. 2-benzyl and 2-heteroaryl benzimidazole NMDA/NR2B antagonists

Also Published As

Publication number Publication date
PL367259A1 (en) 2005-02-21
JP2005515968A (ja) 2005-06-02
JP4322113B2 (ja) 2009-08-26
IL159393A (en) 2011-01-31
EA200400213A1 (ru) 2004-08-26
MXPA04000737A (es) 2004-07-08
NO20040307L (no) 2004-03-23
NZ530055A (en) 2005-07-29
AU2002313566B8 (en) 2003-02-18
KR20040041152A (ko) 2004-05-14
AU2002313566B2 (en) 2007-05-24
PT1409477E (pt) 2008-11-20
BG108592A (bg) 2005-03-31
UA77684C2 (en) 2007-01-15
CN1556805A (zh) 2004-12-22
CA2453383C (en) 2010-04-06
HRP20040178B1 (hr) 2013-05-31
CY1109401T1 (el) 2014-07-02
NO327099B1 (no) 2009-04-20
EP1409477A1 (en) 2004-04-21
BR0211393A (pt) 2004-08-17
WO2003010159A1 (en) 2003-02-06
DE60228969D1 (sr) 2008-10-30
KR100890676B1 (ko) 2009-03-26
EP1409477B1 (en) 2008-09-17
US20040157886A1 (en) 2004-08-12
US7435744B2 (en) 2008-10-14
EA010162B1 (ru) 2008-06-30
CO5560570A2 (es) 2005-09-30
EE200400058A (et) 2004-04-15
PL216636B1 (pl) 2014-04-30
IL159393A0 (en) 2004-06-01
CA2453383A1 (en) 2003-02-06
HK1063464A1 (en) 2004-12-31
HRP20040178A2 (en) 2005-04-30
IS7066A (is) 2003-12-05
EE05429B1 (et) 2011-06-15
RS103903A (en) 2007-02-05
SK287726B6 (en) 2011-07-06
CZ2004233A3 (cs) 2004-12-15
DK1409477T3 (da) 2008-12-08
BG66441B1 (bg) 2014-08-29
SI1409477T1 (sl) 2009-02-28
ATE408611T1 (de) 2008-10-15
WO2003010159A8 (en) 2004-02-12
CN100413860C (zh) 2008-08-27
SK1022004A3 (en) 2004-07-07
ZA200400417B (en) 2005-07-27
ES2312603T3 (es) 2009-03-01

Similar Documents

Publication Publication Date Title
RS50767B (sr) Piperidinski derivati kao antagonisti nmda receptora
NO2015020I1 (no) Ceritinib, 5-klor-N-5-metyl-4-(piperidin-4-yl)-2-[(propan-2-yl)oksy]fenyl-N-[2-(propan-2-sulfonyl)fenyl]pyrimidine-2,4-diamin, eller et farmasøytisk akseptabelt salt derav
YU74694A (sh) Morfolin i tiomorfolin antagonisti receptora tahikinina -
MEP12608A (en) Derivatives of n-[phenyl (pyrrolidine-2-yl) methyl]benzamide and n-[(azepan-2-yl)phenylmethyl]benzamide, preparation method thereof and application of same in therapeutics
RS51200B (sr) (imidazol-1-il-metil)-piridazin kao blokator nmda receptora
RS50573B (sr) Novi derivati 4-benziliden-piperidina
GB0128499D0 (en) Therapeutic agents
YU46787B (sh) Derivati heteroaril 3-okso-propan-nitrila i postupak za njihovo dobijanje
NZ503396A (en) o(phenyl or benzyl)methyl]-1-(substituted phenyl, thiophene, furan or piperidinyl)-cyclohexanol derivatives and medicaments
EA200100090A3 (ru) Новые пиперидин-4-сульфонамидные производные, способ их получения и содержащие их фармацевтические композиции
TNSN07017A1 (en) New benzoyl urea derivatives
RS51126B (sr) Postupak za pripremanje mezilata piperazin derivata
ES2172376A1 (es) Nuevos derivados de isoquinoleinas, su procedimiento de preparacion y las composiciones farmaceuticas que los contienen.
NO20030509D0 (no) Nye N-(2-fenyl-3-aminopropyl)naftamider
PT1430047E (pt) Derivados de alquilaminopiridazinona substituida, processo para a sua preparacao e composicoes farmaceuticas que os contem
DE69402703D1 (de) 3-(INDOL-3-YL) PROPENSäURDERIVATE, DIE ALS NMDA- ANTAGONISTEN NÜTZLICH SIND
ATE336487T1 (de) Benzoesaüre derivate und deren verwendung
EA200300691A1 (ru) Производные 2,3-бензодиазепина и фармацевтические композиции, содержащие эти производные в качестве активного ингредиента
DE60204668D1 (de) Piperazinderivate und deren verwendung als 5-ht1b liganden
TR200001621A2 (tr) Yeni arilpiperazinilalkil-3(2H)-Piridaziononlar
ATE291016T1 (de) Amidinophenylalaninderivate als thrombininhibitoren
PE20001520A1 (es) Composiciones farmaceuticas que comprenden derivados sustituidos de indazol como inhibidores de pde tipo iv y la produccion de tnf
KR870006047A (ko) 트리사이틀릭 피리다조피리돈 유도체 및 그의 제조 방법
YU21595A (sh) Supstituisani derivati morfolina, farmaceutske kompozicije koje ih sadrže i postupci za njihovo dobijanje
HUP0202213A2 (hu) Szilárd fázisú párhuzamos szintézis új karbonsavamidszármazékok előállítására