EA200200522A1 - 1-аминоалкилциклогексановые антагонисты рецептора nmda - Google Patents

1-аминоалкилциклогексановые антагонисты рецептора nmda

Info

Publication number
EA200200522A1
EA200200522A1 EA200200522A EA200200522A EA200200522A1 EA 200200522 A1 EA200200522 A1 EA 200200522A1 EA 200200522 A EA200200522 A EA 200200522A EA 200200522 A EA200200522 A EA 200200522A EA 200200522 A1 EA200200522 A1 EA 200200522A1
Authority
EA
Eurasian Patent Office
Prior art keywords
compounds
cyclic
nmda receptor
aminoalkyl
seizures
Prior art date
Application number
EA200200522A
Other languages
English (en)
Other versions
EA005684B1 (ru
Inventor
Маркус Гольд
Войцех Даныш
Кристофер Грахам Рафаэль Парсонс
Иварс Калвиньш
Валерьянс Каусс
Айгарс Йиргенсонс
Original Assignee
Мерц Фармацойтикалс Гмбх
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 Мерц Фармацойтикалс Гмбх filed Critical Мерц Фармацойтикалс Гмбх
Publication of EA200200522A1 publication Critical patent/EA200200522A1/ru
Publication of EA005684B1 publication Critical patent/EA005684B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/02—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements
    • C07D295/027—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring
    • C07D295/033—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring with the ring nitrogen atoms directly attached to carbocyclic 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4453—Non condensed piperidines, e.g. piperocaine only substituted in position 1, e.g. propipocaine, diperodon
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Некоторые 1-циклические аминоалкилциклогексаны являются системно активными неконкурентными антагонистами рецептора NMDA и следовательно могут применяться для облегчения состояний, возникающих в результате нарушений глутаматэргического переноса. Что более важно, данные соединения обладают повышенной противосудорожной и противоэпилептической активностью, которой не обладают ближайшие аналоги соединения с нециклической аминогруппой. Содержащие их фармацевтические композиции и способ лечения состояний, которые улучшаются в результате применения таких соединений, в особенности, ослабляются судороги и эпилептические припадки, а также включен способ получения активных 1-циклических аминоалкилциклогексановых соединений и промышленное получение на их основе лекарственных средств.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA200200522A 1999-11-01 1999-11-01 Производные 1-аминоалкилциклогексана в качестве антагонистов рецептора nmda EA005684B1 (ru)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/EP1999/008317 WO2001032640A1 (en) 1999-11-01 1999-11-01 1-cyclic amino-alkylcyclohexane compounds, pharmaceutical compositions thereof, and their use as anticonvulsants

Publications (2)

Publication Number Publication Date
EA200200522A1 true EA200200522A1 (ru) 2002-10-31
EA005684B1 EA005684B1 (ru) 2005-04-28

Family

ID=8167482

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200200522A EA005684B1 (ru) 1999-11-01 1999-11-01 Производные 1-аминоалкилциклогексана в качестве антагонистов рецептора nmda

Country Status (24)

Country Link
EP (1) EP1228052B1 (ru)
JP (1) JP4043236B2 (ru)
KR (1) KR100548600B1 (ru)
CN (1) CN1264827C (ru)
AT (1) ATE361284T1 (ru)
AU (1) AU782760B2 (ru)
CA (1) CA2389325C (ru)
CY (1) CY1106672T1 (ru)
CZ (1) CZ20021533A3 (ru)
DE (1) DE69936004T2 (ru)
DK (1) DK1228052T3 (ru)
EA (1) EA005684B1 (ru)
ES (1) ES2285870T3 (ru)
HK (1) HK1049160B (ru)
HU (1) HUP0203275A3 (ru)
IL (2) IL149401A0 (ru)
MX (1) MXPA02004368A (ru)
NO (1) NO322359B1 (ru)
PL (1) PL199587B1 (ru)
PT (1) PT1228052E (ru)
SI (1) SI1228052T1 (ru)
TW (1) TWI242547B (ru)
UA (1) UA72558C2 (ru)
WO (1) WO2001032640A1 (ru)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7732162B2 (en) 2003-05-05 2010-06-08 Probiodrug Ag Inhibitors of glutaminyl cyclase for treating neurodegenerative diseases
WO2008055945A1 (en) 2006-11-09 2008-05-15 Probiodrug Ag 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases
SI2091948T1 (sl) 2006-11-30 2012-07-31 Probiodrug Ag Novi inhibitorji glutaminil ciklaze
ZA200905537B (en) 2007-03-01 2010-10-27 Probiodrug Ag New use of glutaminyl cyclase inhibitors
EP2142514B1 (en) 2007-04-18 2014-12-24 Probiodrug AG Thiourea derivatives as glutaminyl cyclase inhibitors
ES2548913T3 (es) 2009-09-11 2015-10-21 Probiodrug Ag Derivados heterocíclicos como inhibidores de glutaminil ciclasa
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
JP5688745B2 (ja) 2010-03-10 2015-03-25 プロビオドルグ エージー グルタミニルシクラーゼ（ｑｃ、ｅｃ２．３．２．５）の複素環阻害剤
WO2011131748A2 (en) 2010-04-21 2011-10-27 Probiodrug Ag Novel inhibitors
WO2012123563A1 (en) 2011-03-16 2012-09-20 Probiodrug Ag Benz imidazole derivatives as inhibitors of glutaminyl cyclase
CN104211663B (zh) * 2014-08-11 2017-01-11 杭州偶联医药科技有限公司 一种(s)-n-甲氧基-甲基-2-(四氢吡咯基)丙酰胺及其制备方法和应用
EP3461819B1 (en) 2017-09-29 2020-05-27 Probiodrug AG Inhibitors of glutaminyl cyclase
RU2714135C1 (ru) * 2019-11-22 2020-02-12 Федеральное государственное бюджетное учреждение науки "Институт токсикологии Федерального медико-биологического агентства" Гидрохлорид (1-метилпиперидин-4-ил)-2-пропилпентаноата, обладающий холинолитической и противосудорожной активностью

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3097207A (en) * 1958-03-06 1963-07-09 Parke Davis & Co 1-halophenyl and 1-alkoxyphenyl cyclohexylamines
EA002254B1 (ru) * 1997-06-30 2002-02-28 Мерц + Ко. Гмбх Унд Ко. 1-аминоалкилциклогексановые антагонисты рецепторов nmda

Also Published As

Publication number Publication date
CA2389325A1 (en) 2001-05-10
UA72558C2 (ru) 2005-03-15
EA005684B1 (ru) 2005-04-28
PL199587B1 (pl) 2008-10-31
CN1264827C (zh) 2006-07-19
KR100548600B1 (ko) 2006-02-01
CN1374956A (zh) 2002-10-16
HK1049160A1 (en) 2003-05-02
HUP0203275A2 (hu) 2003-01-28
DE69936004D1 (de) 2007-06-14
EP1228052A1 (en) 2002-08-07
AU1158500A (en) 2001-05-14
CZ20021533A3 (cs) 2002-08-14
PT1228052E (pt) 2007-05-31
PL354519A1 (en) 2004-01-26
HUP0203275A3 (en) 2003-11-28
DK1228052T3 (da) 2007-06-18
ATE361284T1 (de) 2007-05-15
DE69936004T2 (de) 2008-01-10
JP2003513083A (ja) 2003-04-08
NO322359B1 (no) 2006-09-18
WO2001032640A1 (en) 2001-05-10
MXPA02004368A (es) 2002-11-14
IL149401A (en) 2008-03-20
IL149401A0 (en) 2002-11-10
ES2285870T3 (es) 2007-11-16
HK1049160B (zh) 2006-11-17
NO20022044D0 (no) 2002-04-30
SI1228052T1 (sl) 2007-10-31
KR20020063172A (ko) 2002-08-01
NO20022044L (no) 2002-04-30
JP4043236B2 (ja) 2008-02-06
TWI242547B (en) 2005-11-01
EP1228052B1 (en) 2007-05-02
CY1106672T1 (el) 2012-05-23
CA2389325C (en) 2007-01-09
AU782760B2 (en) 2005-08-25

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Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM RU