AR044579A1 - Antagonistas de nmda/ nr2b nonaril - heterociclicos n- sustituidos - Google Patents

Antagonistas de nmda/ nr2b nonaril - heterociclicos n- sustituidos

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Publication number
AR044579A1
AR044579A1 ARP040101878A ARP040101878A AR044579A1 AR 044579 A1 AR044579 A1 AR 044579A1 AR P040101878 A ARP040101878 A AR P040101878A AR P040101878 A ARP040101878 A AR P040101878A AR 044579 A1 AR044579 A1 AR 044579A1
Authority
AR
Argentina
Prior art keywords
aryl
alkyl
nmda
substituted
nonaril
Prior art date
Application number
ARP040101878A
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English (en)
Original Assignee
Merck & Co Inc
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.)
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Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=33511734&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR044579(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Publication of AR044579A1 publication Critical patent/AR044579A1/es

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    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • 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
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • 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
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    • 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
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32Alcohol-abuse
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
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    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
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    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • A61P31/20Antivirals for DNA viruses
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    • A61P35/00Antineoplastic agents
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    • 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
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    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
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    • 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

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

Abstract

Sales farmacéuticamente aceptables de los mismos, son eficaces como antagonistas de NMDA NR2B útiles para tratar afecciones tales como, por ejemplo, enfermedad de Parkinson, enfermedad de Alzheimer, migraña, epilepsia y dolor. Reivindicación 1: Un compuesto que tiene la fórmula (1), o las sales farmacéuticas de los mismos, en la que: HetAr es un anillo heteroaromático de 5 ó 6 eslabones que contiene 1 ó 2 átomos de nitrógeno en el anillo, tiazolilo, o tiadiazolilo; HetAr está opcionalmente sustituido con 1 o 2 sustituyentes, cada sustituyente independientemente es alquil c1-4, flúor, cloro, bromo, o yodo; A es un enlace o alquil-C1-2; y B es aril(CH2)0-3-O-C(O)-, indanil(CH2)0-3-O-C(O)-, aril(CH2)1-3-C(O)-, aril-ciclopropil-C(O)-, aril(CH2)1-3-NH-C(O)-, en el que cualquier arilo está opcionalmente sustituido con 1-5 sustituyentes, cada sustituyentes independientemente es alquilo C-14, fluoro, o cloro. R1 y R2 son independientemente, H, alquilo C1-4, fluoro, bromo o yodo.
ARP040101878A 2003-06-04 2004-05-31 Antagonistas de nmda/ nr2b nonaril - heterociclicos n- sustituidos AR044579A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US47593803P 2003-06-04 2003-06-04

Publications (1)

Publication Number Publication Date
AR044579A1 true AR044579A1 (es) 2005-09-21

Family

ID=33511734

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP040101878A AR044579A1 (es) 2003-06-04 2004-05-31 Antagonistas de nmda/ nr2b nonaril - heterociclicos n- sustituidos

Country Status (30)

Country Link
EP (1) EP1648882B1 (es)
JP (1) JP3927228B2 (es)
KR (1) KR20060017839A (es)
CN (1) CN1798744A (es)
AR (1) AR044579A1 (es)
AT (1) ATE403651T1 (es)
AU (1) AU2004245522B2 (es)
BR (1) BRPI0410837A (es)
CA (1) CA2527093C (es)
CL (1) CL2004001365A1 (es)
CO (1) CO5700762A2 (es)
DE (1) DE602004015610D1 (es)
DK (1) DK1648882T3 (es)
EC (1) ECSP056192A (es)
ES (1) ES2309540T3 (es)
HR (1) HRP20080490T3 (es)
IS (1) IS8117A (es)
MA (1) MA27781A1 (es)
MX (1) MXPA05013151A (es)
MY (1) MY138547A (es)
NO (1) NO20060020L (es)
PE (1) PE20050245A1 (es)
PL (1) PL1648882T3 (es)
PT (1) PT1648882E (es)
RU (1) RU2339630C2 (es)
SI (1) SI1648882T1 (es)
TW (1) TW200510378A (es)
UA (1) UA81319C2 (es)
WO (1) WO2004108705A1 (es)
ZA (1) ZA200509000B (es)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2007247851A1 (en) * 2006-05-03 2007-11-15 Relevare Aust. Pty Ltd Methods and composition for treatment of inflammatory pain
EP2148879B1 (en) * 2007-04-23 2012-11-28 Janssen Pharmaceutica, N.V. Thia(dia)zoles as fast dissociating dopamine 2 receptor antagonists
EP2175886A1 (en) * 2007-06-28 2010-04-21 CNSBio Pty Ltd Combination methods and compositions for treatment of neuropathic pain
SG183111A1 (en) 2010-02-16 2012-09-27 Pfizer (r)-4-((4-((4-(tetrahydrofuran-3-yloxy)benzo[d]isoxazol-3-yloxy)methyl)piperidin-1-yl)methyl)tetrahydro-2h-pyran-4-ol, a partial agonist of 5-ht4 receptors
WO2013156614A1 (en) 2012-04-20 2013-10-24 Ucb Pharma S.A. Methods for treating parkinson's disease
CN103936663B (zh) * 2013-01-23 2016-12-28 艾琪康医药科技(上海)有限公司 一种1-r1-3,3-二氟(或3-氟)-4-r2-4-氨甲基哌啶及其衍生物的制备方法
US9221796B2 (en) 2014-01-09 2015-12-29 Bristol-Myers Squibb Company Selective NR2B antagonists
US9187506B2 (en) 2014-01-09 2015-11-17 Bristol-Myers Squibb Company (R)-3-((3S,4S)-3-fluoro-4-(4-hydroxyphenyl)piperidin-1-yl)-1-(4-methylbenzyl)pyrrolidin-2-one and its prodrugs for the treatment of psychiatric disorders
TW201609741A (zh) 2014-06-04 2016-03-16 盧郡控股(開曼)有限公司 作為nr2b nmda受體拮抗劑之二氟乙基吡啶衍生物
CA2957898C (en) 2014-09-15 2023-02-21 Rugen Holdings (Cayman) Limited Pyrrolopyrimidine derivatives as nr2b nmda receptor antagonists
US20180271869A1 (en) * 2014-09-22 2018-09-27 Jie Liu Treatment of anxiety disorders and autism spectrum disorders
JP2018506514A (ja) * 2014-12-23 2018-03-08 セレコー,インコーポレイテッド 化合物、組成物および方法
US10221182B2 (en) 2015-02-04 2019-03-05 Rugen Holdings (Cayman) Limited 3,3-difluoro-piperidine derivatives as NR2B NMDA receptor antagonists
JP6876625B2 (ja) * 2015-06-01 2021-05-26 リューゲン ホールディングス (ケイマン) リミテッド Nr2bnmdaレセプターアンタゴニストとしての3,3−ジフルオロピペリジンカルバメート複素環式化合物
US10344020B2 (en) 2015-10-14 2019-07-09 Bristol-Myers Squibb Company Selective NR2B antagonists
JP6843853B2 (ja) 2015-10-14 2021-03-17 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company 選択的nr2bアンタゴニスト
US10227349B2 (en) 2016-08-31 2019-03-12 Eisai R&D Management Co., Ltd. Pyrazolo[1,5-a]pyrimidine compound
WO2018098128A1 (en) 2016-11-22 2018-05-31 Rugen Holdings (Cayman) Limited Treatment of autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA005974B1 (ru) * 2001-02-23 2005-08-25 Мерк Энд Ко., Инк. N-замещенные неарильные гетероциклические антагонисты nmda/nr2b

Also Published As

Publication number Publication date
DK1648882T3 (da) 2008-11-24
SI1648882T1 (sl) 2009-02-28
HRP20080490T3 (en) 2008-11-30
CL2004001365A1 (es) 2005-05-06
RU2005137704A (ru) 2006-05-27
EP1648882A1 (en) 2006-04-26
CA2527093A1 (en) 2004-12-16
BRPI0410837A (pt) 2006-06-27
IS8117A (is) 2005-11-07
JP3927228B2 (ja) 2007-06-06
NO20060020L (no) 2006-03-03
CO5700762A2 (es) 2006-11-30
TW200510378A (en) 2005-03-16
ECSP056192A (es) 2006-04-19
KR20060017839A (ko) 2006-02-27
PT1648882E (pt) 2008-10-20
JP2006526650A (ja) 2006-11-24
AU2004245522A1 (en) 2004-12-16
PL1648882T3 (pl) 2008-12-31
WO2004108705A1 (en) 2004-12-16
PE20050245A1 (es) 2005-04-13
RU2339630C2 (ru) 2008-11-27
UA81319C2 (en) 2007-12-25
CN1798744A (zh) 2006-07-05
CA2527093C (en) 2009-10-20
ATE403651T1 (de) 2008-08-15
MY138547A (en) 2009-06-30
AU2004245522B2 (en) 2009-10-29
EP1648882B1 (en) 2008-08-06
MXPA05013151A (es) 2006-03-17
ES2309540T3 (es) 2008-12-16
ZA200509000B (en) 2006-12-27
MA27781A1 (fr) 2006-02-01
DE602004015610D1 (de) 2008-09-18

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