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

Antagonistas de nmda/ nr2b nonaril - heterociclicos n- sustituidos

Info

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
Other languages
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.)
Filing date
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
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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    • 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
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    • 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
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
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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
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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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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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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
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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
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    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Virology (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Addiction (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Communicable Diseases (AREA)
  • Endocrinology (AREA)
  • Oncology (AREA)
  • Molecular Biology (AREA)
  • Psychology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Diabetes (AREA)
  • Biotechnology (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • AIDS & HIV (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
JP2009535364A (ja) * 2006-05-03 2009-10-01 シーエヌエスバイオ ピーティーワイ リミテッド 炎症性疼痛の治療のための方法および組成物
ES2400710T3 (es) * 2007-04-23 2013-04-11 Janssen Pharmaceutica, N.V. Tia(dia)zoles como antagonistas del receptor de dopamina 2 de disociación rápida
EP2175886A1 (en) * 2007-06-28 2010-04-21 CNSBio Pty Ltd Combination methods and compositions for treatment of neuropathic pain
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
AU2013251079B2 (en) 2012-04-20 2017-03-23 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
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
US9221796B2 (en) 2014-01-09 2015-12-29 Bristol-Myers Squibb Company Selective NR2B antagonists
EP3152213B1 (en) 2014-06-04 2018-10-31 Rugen Holdings (Cayman) Limited Difluoroethylpyridine derivatives as nr2b nmda receptor antagonists
MX2017002775A (es) 2014-09-15 2017-08-10 Rugen Holdings (Cayman) Ltd Derivados de pirrolopirimidina como antagonistas del receptor de n-metil-d-aspartato (nmda), subunidad nr2b.
US20180271869A1 (en) * 2014-09-22 2018-09-27 Jie Liu Treatment of anxiety disorders and autism spectrum disorders
EP3237399B1 (en) * 2014-12-23 2022-11-30 Avalo Therapeutics, Inc. Compounds, compositions and methods
US10221182B2 (en) 2015-02-04 2019-03-05 Rugen Holdings (Cayman) Limited 3,3-difluoro-piperidine derivatives as NR2B NMDA receptor antagonists
CN107849010B (zh) 2015-06-01 2021-11-09 卢郡控股(开曼)有限公司 作为nr2b nmda受体拮抗剂的3,3‐二氟哌啶氨基甲酸酯杂环化合物
ES2822830T3 (es) 2015-10-14 2021-05-05 Bristol Myers Squibb Co Antagonistas selectivos de NR2B
WO2017066366A1 (en) 2015-10-14 2017-04-20 Bristol-Myers Squibb Company Selective nr2b antagonists
TWI732031B (zh) 2016-08-31 2021-07-01 日商衛材R&D企管股份有限公司 吡唑并[1, 5-a]嘧啶化合物
US11000526B2 (en) 2016-11-22 2021-05-11 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
DE60210944T3 (de) * 2001-02-23 2015-07-23 Merck Sharp & Dohme Corp. N-substituierte nichtaryl-heterocyclische nmda/nr2b antagonisten

Also Published As

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

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