EA200300919A1 - N-замещенные неарильные гетероциклические антагонисты nmda/nr2b - Google Patents

N-замещенные неарильные гетероциклические антагонисты nmda/nr2b

Info

Publication number
EA200300919A1
EA200300919A1 EA200300919A EA200300919A EA200300919A1 EA 200300919 A1 EA200300919 A1 EA 200300919A1 EA 200300919 A EA200300919 A EA 200300919A EA 200300919 A EA200300919 A EA 200300919A EA 200300919 A1 EA200300919 A1 EA 200300919A1
Authority
EA
Eurasian Patent Office
Prior art keywords
nr2b
substituted non
aryl heterocyclic
nmda
antagonists nmda
Prior art date
Application number
EA200300919A
Other languages
English (en)
Other versions
EA005974B1 (ru
Inventor
Кристофер Ф. Клэйборн
Джон У. Батчер
Дэвид А. Клэйрмон
Брайан И. Либби
Найджел Дж. Ливертон
Питер М. Мансон
Кевин Т. Нгуйен
Брайан Филлипс
Уэйн Томпсон
Джон А. Макколи
Original Assignee
Мерк Энд Ко., Инк.
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=23034191&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA200300919(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Мерк Энд Ко., Инк. filed Critical Мерк Энд Ко., Инк.
Publication of EA200300919A1 publication Critical patent/EA200300919A1/ru
Publication of EA005974B1 publication Critical patent/EA005974B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D403/12—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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/12—Heterocyclic 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
    • 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
    • C07D417/12—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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/16—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D475/00—Heterocyclic compounds containing pteridine ring systems
    • C07D475/06—Heterocyclic compounds containing pteridine ring systems with a nitrogen atom directly attached in position 4
    • C07D475/08—Heterocyclic compounds containing pteridine ring systems with a nitrogen atom directly attached in position 4 with a nitrogen atom directly attached in position 2

Abstract

Соединения, представленные формулой Iили их фармацевтически приемлемыми солями, эффективные в качестве антагонистов NMDA NR2B и применяемые для облегчения боли.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA200300919A 2001-02-23 2002-02-20 N-замещенные неарильные гетероциклические антагонисты nmda/nr2b EA005974B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US27110001P 2001-02-23 2001-02-23
PCT/US2002/005226 WO2002068409A1 (en) 2001-02-23 2002-02-20 N-substituted nonaryl-heterocyclic nmda/nr2b antagonists

Publications (2)

Publication Number Publication Date
EA200300919A1 true EA200300919A1 (ru) 2004-02-26
EA005974B1 EA005974B1 (ru) 2005-08-25

Family

ID=23034191

Family Applications (1)

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EA200300919A EA005974B1 (ru) 2001-02-23 2002-02-20 N-замещенные неарильные гетероциклические антагонисты nmda/nr2b

Country Status (33)

Country Link
US (2) US7217716B2 (ru)
EP (1) EP1379520B2 (ru)
JP (1) JP4179879B2 (ru)
KR (1) KR100849839B1 (ru)
CN (1) CN100567293C (ru)
AT (1) ATE324371T1 (ru)
AU (1) AU2002252053B2 (ru)
BG (1) BG108113A (ru)
BR (1) BR0207526A (ru)
CA (1) CA2438895A1 (ru)
CZ (1) CZ20032258A3 (ru)
DE (1) DE60210944T3 (ru)
DK (1) DK1379520T3 (ru)
EA (1) EA005974B1 (ru)
EC (1) ECSP034744A (ru)
EE (1) EE200300403A (ru)
ES (1) ES2261658T3 (ru)
GE (1) GEP20063741B (ru)
HR (1) HRP20030669A2 (ru)
HU (1) HUP0303258A3 (ru)
IL (2) IL157254A0 (ru)
IS (1) IS6902A (ru)
MX (1) MXPA03007621A (ru)
NO (1) NO20033732L (ru)
NZ (1) NZ527365A (ru)
PL (1) PL364625A1 (ru)
PT (1) PT1379520E (ru)
SI (1) SI1379520T1 (ru)
SK (1) SK10542003A3 (ru)
UA (1) UA75392C2 (ru)
WO (1) WO2002068409A1 (ru)
YU (1) YU64303A (ru)
ZA (1) ZA200306159B (ru)

Families Citing this family (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2449249A1 (en) * 2001-06-12 2002-12-19 Merck & Co., Inc. Nr2b receptor antagonists for the treatment or prevention of migraines
EP1452530A4 (en) * 2001-12-03 2005-11-30 Japan Tobacco Inc AZOL CONNECTION AND THEIR MEDICAL USE
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
JP2005520821A (ja) * 2002-03-15 2005-07-14 チバ　スペシャルティ　ケミカルズ　ホールディング　インコーポレーテッド ４−アミノピリミジン及び表面の抗菌処理のためのその使用
US6924285B2 (en) 2002-03-30 2005-08-02 Boehringer Ingelheim Pharma Gmbh & Co. Bicyclic heterocyclic compounds, pharmaceutical compositions containing these compounds, their use and process for preparing them
JP4429733B2 (ja) 2002-04-16 2010-03-10 帝人株式会社 Ｃｃｒ３拮抗作用を有するピペリジン誘導体
CN100360521C (zh) 2002-04-25 2008-01-09 帝人株式会社 具有ccr3拮抗作用的4,4-二取代的哌啶衍生物
JP2004315511A (ja) * 2003-03-31 2004-11-11 Taisho Pharmaceut Co Ltd Ｍｃｈ受容体アンタゴニスト
ATE403651T1 (de) * 2003-06-04 2008-08-15 Merck & Co Inc 3-fluoro-piperidine als nmda/nr2b antagonisten
US7592360B2 (en) 2003-06-04 2009-09-22 Merck & Co., Inc. 3-fluoro-piperidines as NMDA/NR2B antagonists
ES2421139T3 (es) 2003-07-30 2013-08-29 Rigel Pharmaceuticals, Inc. Compuestos de 2,4-pirimidindiamina para su uso en el tratamiento o la prevención de enfermedades autoinmunitarias
US7632840B2 (en) 2004-02-03 2009-12-15 Astrazeneca Ab Quinazoline compounds for the treatment of hyperproliferative disorders
AU2005271669A1 (en) * 2004-08-03 2006-02-16 Merck & Co., Inc. 1,3-disubstituted heteroaryl NMDA/NR2B antagonists
US20080153917A1 (en) * 2004-09-10 2008-06-26 Ucb Pharma, S.A. Sigma Receptor Ligands
US7776869B2 (en) 2004-10-18 2010-08-17 Amgen Inc. Heteroaryl-substituted alkyne compounds and method of use
US20100063081A1 (en) 2005-06-30 2010-03-11 Stuart Edward Bradly CPCR Agonists
JO2769B1 (en) 2005-10-26 2014-03-15 جانسين فارماسوتيكا ان. في Rapid decomposition of physiologically antagonistic agents of the 2-dopamine receptor
ATE461190T1 (de) * 2005-12-21 2010-04-15 Janssen Pharmaceutica Nv Substituierte pyradinon-derivate als alpha2- adrenorezeptor-antagonisten
JPWO2007099828A1 (ja) * 2006-02-23 2009-07-16 塩野義製薬株式会社 環式基で置換された含窒素複素環誘導体
US20100273776A1 (en) * 2006-03-29 2010-10-28 FOLDRx PHARMACEUTICALS, INC Inhibition of alpha-synuclein toxicity
EP1921070A1 (de) 2006-11-10 2008-05-14 Boehringer Ingelheim Pharma GmbH & Co. KG Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstelllung
KR101152162B1 (ko) * 2006-12-08 2012-07-10 에프. 호프만-라 로슈 아게 치환된 피리미딘 및 ｊｎｋ 조절제로서 그의 용도
JO2642B1 (en) 2006-12-08 2012-06-17 جانسين فارماسوتيكا ان. في Dopamine 2 receptor antagonists are rapidly hydrolyzed
EA200901041A1 (ru) 2007-02-06 2010-02-26 Бёрингер Ингельхайм Интернациональ Гмбх Бициклические гетероциклы, содержащие эти соединения лекарственные средства, их применение и способ их получения
JO2849B1 (en) 2007-02-13 2015-03-15 جانسين فارماسوتيكا ان. في Dopamine 2 receptor antagonists are rapidly hydrolyzed
KR101506156B1 (ko) 2007-04-23 2015-03-26 얀센 파마슈티카 엔.브이. 속해리성 도파민 2 수용체 길항제로서의 티아(디아)졸
ES2393818T3 (es) 2007-04-23 2012-12-28 Janssen Pharmaceutica, N.V. Derivados de tipo 4-alcoxipiridazina como antagonistas de los receptores 2 de la dopamina de disociación rápida
SI2195293T1 (sl) 2007-08-22 2014-02-28 Astrazeneca Ab Derivati ciklopropil amida
EP2215073A4 (en) * 2007-10-31 2011-04-06 Merck Sharp & Dohme SLEEP MODULATION WITH NR2B RECEPTOR ANTAGONISTS
EA019709B1 (ru) 2008-02-07 2014-05-30 Бёрингер Ингельхайм Интернациональ Гмбх Спирогетероциклы и их применение в качестве лекарственных средств
EP2303276B1 (en) 2008-05-13 2013-11-13 AstraZeneca AB Fumarate salt of 4-(3-chloro-2-fluoroanilino)-7-methoxy-6-{[1-(n-methylcarbamoylmethyl)piperidin-4-yl]oxy}quinazoline
JP5417439B2 (ja) 2008-07-03 2014-02-12 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ ５−ｈｔ６受容体アンタゴニストとしての置換された６−（１−ピペラジニル）−ピリダジン類
CN102171189B (zh) 2008-07-31 2013-11-20 詹森药业有限公司 作为快速解离多巴胺2受体拮抗剂的哌嗪-1-基-三氟甲基取代的吡啶
US8648191B2 (en) 2008-08-08 2014-02-11 Boehringer Ingelheim International Gmbh Cyclohexyloxy substituted heterocycles, pharmaceutical compositions containing these compounds and processes for preparing them
TW201039825A (en) * 2009-02-20 2010-11-16 Astrazeneca Ab Cyclopropyl amide derivatives 983
US8389536B2 (en) * 2009-10-27 2013-03-05 Hoffmann-La Roche Inc. Positive allosteric modulators (PAM)
WO2011102793A1 (en) * 2010-02-18 2011-08-25 Astrazeneca Ab Solid forms comprising a cyclopropyl amide derivative
SG183274A1 (en) 2010-02-18 2012-09-27 Astrazeneca Ab Processes for making cyclopropyl amide derivatives and intermediates associated therewith
AU2010363329A1 (en) 2010-11-07 2013-05-09 Targegen, Inc. Compositions and methods for treating myelofibrosis
JP6001049B2 (ja) * 2011-03-31 2016-10-05 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ Ｍｐｓ−１キナーゼ阻害剤としての置換ベンズイミダゾール類
EP2760856B1 (en) * 2011-09-30 2016-09-14 Bristol-Myers Squibb Company Selective nr2b antagonists
KR20140146217A (ko) 2012-04-20 2014-12-24 유씨비 파마, 에스.에이. 파킨슨병을 치료하는 방법
JP2016028017A (ja) * 2012-12-13 2016-02-25 大正製薬株式会社 フッ素置換ピペリジン化合物
JP2017001954A (ja) * 2013-11-08 2017-01-05 石原産業株式会社 含窒素飽和複素環化合物
CN106459030B (zh) * 2014-05-28 2019-01-29 东亚荣养株式会社 取代托品烷衍生物
CA2950285A1 (en) * 2014-06-04 2015-12-10 Rugen Holdings (Cayman) Limited Difluoroethylpyridine derivatives as nr2b nmda receptor antagonists
CN106715435B (zh) * 2014-09-15 2019-10-01 卢郡控股(开曼)有限公司 作为nr2b nmda受体拮抗剂的吡咯并嘧啶衍生物
WO2016100349A2 (en) * 2014-12-16 2016-06-23 Rugen Holdings (Cayman) Limited Bicyclic azaheterocyclic compounds as nr2b nmda receptor antagonists
EP3253761A4 (en) 2015-02-04 2018-06-20 Rugen Holdings (Cayman) Limited 3,3-difluoro-piperidine derivatives as nr2b nmda receptor antagonists
KR20230145498A (ko) 2015-05-11 2023-10-17 바스프 에스이 4-아미노-피리다진의 제조 방법
US10584127B2 (en) 2015-06-01 2020-03-10 Rugen Holdings (Cayman) Limited 3,3-difluoropiperidine carbamate heterocyclic compounds as NR2B NMDA receptor antagonists
EP3544610A1 (en) 2016-11-22 2019-10-02 Rugen Holdings (Cayman) Limited Treatment of autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders
AU2019223215B2 (en) * 2018-02-23 2022-09-15 Fraunhofer-Gesellschaft zur Förderung der angewandten Forschung e.V. Novel inhibitors of bacterial glutaminyl cyclases for use in the treatment of periodontal and related diseases

Family Cites Families (45)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL265777A (ru) 1960-06-09
DE2341965C3 (de) 1973-08-20 1979-01-25 C.H. Boehringer Sohn, 6507 Ingelheim 4- [N- (o-PyridyD- N-acyl] -aminolphenäthylpiperidine, Verfahren zu deren Herstellung sowie deren Verwendung bei der Bekämpfung von Schmerzzuständen
US4197304A (en) * 1975-09-23 1980-04-08 Janssen Pharmaceutica N.V. N-Aryl-N-(1-L-4-piperidinyl)-arylacetamides
EP0126087A1 (en) * 1982-09-24 1984-11-28 Beecham Group Plc Amino-azabicycloalkyl derivatives as dopamine antagonists
WO1991012005A1 (en) 1990-02-06 1991-08-22 Pfizer Inc. Neuroprotective 3-piperidino-4-hydroxychroman derivatives and analogs
ATE192149T1 (de) 1990-05-10 2000-05-15 Pfizer Neuroprotective indolone und verwandte derivate
US5189036A (en) 1990-06-20 1993-02-23 Schering Ag Imidazolylbenzoyl substituted heterocycles
US5455250A (en) 1991-04-18 1995-10-03 Pfizer Inc. Prodrug esters of phenolic 2-piperidino-1-alkanols
HUT70528A (en) 1991-07-17 1995-10-30 Pfizer 2-(4-hydroxypiperidino)-1-alkanol derivatives as antiischemic agents and process for production thereof
MY110227A (en) 1991-08-12 1998-03-31 Ciba Geigy Ag 1-acylpiperindine compounds.
SI9300097B (en) * 1992-02-27 2001-12-31 Janssen Pharmaceutica Nv (benzodioxan, benzofuran or benzopyran) alkylamino) alkyl substituted guanidines
DK55192D0 (da) * 1992-04-28 1992-04-28 Lundbeck & Co As H 1-piperazino-1,2-dihydroindenderivater
US5436255A (en) 1992-07-23 1995-07-25 Pfizer Inc. Method of treating diseases susceptable to treatment by blocking NMDA-receptors
DE4241632A1 (de) 1992-12-10 1994-06-16 Thomae Gmbh Dr K Carbonsäurederivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
EP0674623B1 (en) 1992-12-21 2003-04-09 Smithkline Beecham Corporation Bicyclic fibrinogen antagonists
DE4304650A1 (de) 1993-02-16 1994-08-18 Thomae Gmbh Dr K Kondensierte 5-gliedrige Heterocyclen, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel
WO1994020062A2 (en) 1993-03-03 1994-09-15 Eli Lilly And Company Balanoids as protein kinase c inhibitors
EP0689535B1 (en) 1993-03-18 1998-09-23 MERCK SHARP &amp; DOHME LTD. Benzimidazole derivatives
WO1996002250A1 (en) 1994-07-20 1996-02-01 Acea Pharmaceuticals Inc. Haloperidol analogs and the use thereof
US5661161A (en) 1994-09-29 1997-08-26 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
EP0742208A1 (en) 1995-05-05 1996-11-13 Grelan Pharmaceutical Co., Ltd. 2-Ureido-benzamide derivatives
DE69532482T2 (de) 1995-05-26 2004-11-25 Pfizer Inc. Kombinationspräparat zur behandlung der parkinsonschen krankheit, das selektive nmda-antagonisten enthält
DE69620974T2 (de) 1995-11-06 2003-01-16 Kuraray Co Verfahren zur Herstellung von Acetalen
DE19541264A1 (de) 1995-11-06 1997-05-07 Bayer Ag Purin-6-on-derivate
GB9523675D0 (en) * 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
ZA9610745B (en) 1995-12-22 1997-06-24 Warner Lambert Co 4-Subsituted piperidine analogs and their use as subtype selective nmda receptor antagonists
FR2744449B1 (fr) 1996-02-02 1998-04-24 Pf Medicament Nouvelles piperazines aromatiques derivees de cycloazanes substitues, ainsi que leur procede de preparation, les compositions pharmaceutiques et leur utilisation comme medicaments
EP0787493A1 (en) 1996-02-03 1997-08-06 F. Hoffmann-La Roche Ag Tetrahydroisoquinoline derivatives
TW504510B (en) * 1996-05-10 2002-10-01 Janssen Pharmaceutica Nv 2,4-diaminopyrimidine derivatives
AU2898297A (en) 1996-05-24 1998-01-05 Novartis Ag Use of substance p antagonists for treating social phobia
PL191082B1 (pl) 1996-07-25 2006-03-31 Biogen Inhibitor IIb/IIIa, sposób jego wytwarzania i jego zastosowanie
DZ2285A1 (fr) 1996-08-08 2002-12-25 Smithkline Beecham Corp Inhibiteurs de protéase de la cystéine.
EP0846683B1 (en) 1996-12-03 2001-09-19 F. Hoffmann-La Roche Ag 4-Hydroxy-piperidine derivatives
FR2758327B1 (fr) 1997-01-15 1999-04-02 Pf Medicament Nouvelles arylpiperazines derivees de piperidine
FR2758328B1 (fr) 1997-01-15 1999-04-02 Pf Medicament Nouvelles amines aromatiques derivees d'amines cycliques utiles comme medicaments
IT1291569B1 (it) 1997-04-15 1999-01-11 Angelini Ricerche Spa Indazolammidi come agenti serotoninergici
US6020347A (en) 1997-11-18 2000-02-01 Merck & Co., Inc. 4-substituted-4-piperidine carboxamide derivatives
WO1999025685A1 (en) 1997-11-18 1999-05-27 Merck & Co., Inc. 4-substituted-4-piperidine carboxamide derivatives
DE19815026A1 (de) * 1998-04-03 1999-10-07 Hoechst Schering Agrevo Gmbh Substituierte Piperidine, Verfahren zu ihrer Herstellung und ihre Verwendung als Schädlingsbekämpfungsmittel und Fungizide
PE20000728A1 (es) 1998-06-26 2000-08-21 Cocensys Inc Heterociclos 4-bencil piperidina alquilsulfoxido y su uso como antagonistas receptores subtipo-selectivo nmda
ATE329911T1 (de) 1998-08-07 2006-07-15 Applied Research Systems Fsh mimetika zur behandlung von infertilität
DE19838300A1 (de) 1998-08-24 2000-03-02 Bayer Ag 9-Dialkylaminopurinon-derivate
US6303637B1 (en) 1998-10-30 2001-10-16 Merck & Co., Inc. Heterocyclic potassium channel inhibitors
HUP0203338A2 (hu) 1999-04-13 2003-03-28 Abbott Gmbh & Co. Kg Integrin receptor ligandumok
WO2001000207A1 (en) 1999-06-30 2001-01-04 Merck & Co., Inc. Src kinase inhibitor compounds

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US20020165241A1 (en) 2002-11-07
DE60210944D1 (de) 2006-06-01
IL157254A0 (en) 2004-02-19
UA75392C2 (en) 2006-04-17
ATE324371T1 (de) 2006-05-15
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DE60210944T3 (de) 2015-07-23
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