ES2157337T3 - Derivados de morfolina y su uso como agentes terapeuticos. - Google Patents

Derivados de morfolina y su uso como agentes terapeuticos.

Info

Publication number
ES2157337T3
ES2157337T3 ES95927862T ES95927862T ES2157337T3 ES 2157337 T3 ES2157337 T3 ES 2157337T3 ES 95927862 T ES95927862 T ES 95927862T ES 95927862 T ES95927862 T ES 95927862T ES 2157337 T3 ES2157337 T3 ES 2157337T3
Authority
ES
Spain
Prior art keywords
4alkyl
pct
hydrogen
4alkoxy
hydroxy
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
ES95927862T
Other languages
English (en)
Inventor
Timothy Harrison
Andrew Pate Owens
Christopher John Swain
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Organon Pharma UK Ltd
Original Assignee
Merck Sharp and Dohme Ltd
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 GB9416427A external-priority patent/GB9416427D0/en
Priority claimed from GBGB9509605.3A external-priority patent/GB9509605D0/en
Application filed by Merck Sharp and Dohme Ltd filed Critical Merck Sharp and Dohme Ltd
Application granted granted Critical
Publication of ES2157337T3 publication Critical patent/ES2157337T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • 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
    • C07D413/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • C07D265/32—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings with oxygen atoms directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804—Compounds having Si-O-C linkages

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

LA PRESENTE INVENCION SE REFIERE A COMPUESTOS DE FORMULA (I) EN DONDE X ES -NR{SUP,6}R{SUP,7} O C- O IMIDAZOLILO N-ENLAZADO; Y ES HIDROGENO O C{SUB,1-4}ALQUILO OPCIONALMENTE SUSTITUIDO POR HIDROXIDO; R{SUP,1}, R{SUP,2}, R{SUP,3}, R{SUP,4} Y R{SUP,5} SE SELECCIONAN DE UNA VARIEDAD DE SUSTITUYENTES AROMATICOS ADECUADOS; R{SUP,6} ES HIDROGENO, C{SUB,1-6}ALQUILO, C{SUB,37}CICLOALQUILO, C{SUB,3-7}CICLOALQUILOC{SUB,1-4}ALQUILO, FENILO O C{SUB,2-4}ALQUILO SUSTITUIDO POR C{SUB,1-4}ALCOXI O HIDROXIDO; R{SUP,7} ES HIDROGENO, C{SUB,1-6}ALQUILO, C{SUB,3-7}CICLOALQUILO, C{SUB,3-7}CICLOALQUILOC{SUB,1-4}ALQUILO, FENILO O C{SUB,24}ALQUILO SUSTITUIDO POR UNO O DOS DE C{SUB,1-4}ALCOXI, HIDROXIDO O UN ANILLO HETEROALIFATICO DE 4, 5 O 6 MIEMBROS QUE CONTENGA UNO O DOS HETEROATOMOS SELECCIONADOS DE N, O Y S; O NR{SUP,6}R{SUP,7} ES UN ANILLO HETEROCICLICO SATURADO O PARCIALMENTE SATURADO DE 4 A 7 ATOMOS DE ANILLO, QUE CONTIENE OPCIONALMENTE UNO DE O, S, NR{SUP,8}, S(()O()) O S(()O()){SUB,2} Y OPCIONALMENTE SUSTITUIDO POR UNO O DOS DE HIDROXI{SUB,1-4}ALQUILO, C{SUB,14}ALCOXIC{SUB,1-5}ALQUILO, OXO, COR{SUP,A} O CO{SUB,2}R{SUP,A}; O NR{SUP,6}R{SUP,7} FORMA UN SISTEMA DE ANILLO AZABICICLICO NO AROMATICO DE 6 A 12 ATOMOS DE ANILLO; Y R{SUP,9A} Y R{SUP,9B} SON CADA UNO INDEPENDIENTEMENTE HIDROGENO O C{SUB,1-4}ALQUILO, O R{SUP,9A} Y R{SUP,9B} SON UNIDOS PARA, JUNTO CON EL ATOMO DE CARBONO AL QUE ESTAN INCORPORADOS, HAYA FORMADO UN C{SUB,57}ANILLO; O UNA SAL FARMACEUTICAMENTE ACEPTABLE DE LOS MISMOS. LOS COMPUESTOS SON DE PARTICULAR USO EN EL TRATAMIENTO O PREVENCION DE DOLOR, INFLAMACION, MIGRAÑA, VOMITOS Y NEURALGIA POST-HERPES.
ES95927862T 1994-08-15 1995-08-07 Derivados de morfolina y su uso como agentes terapeuticos. Expired - Lifetime ES2157337T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB9416427A GB9416427D0 (en) 1994-08-15 1994-08-15 Therapeutic agents
GBGB9509605.3A GB9509605D0 (en) 1995-05-11 1995-05-11 Therapeutic agents

Publications (1)

Publication Number Publication Date
ES2157337T3 true ES2157337T3 (es) 2001-08-16

Family

ID=26305450

Family Applications (1)

Application Number Title Priority Date Filing Date
ES95927862T Expired - Lifetime ES2157337T3 (es) 1994-08-15 1995-08-07 Derivados de morfolina y su uso como agentes terapeuticos.

Country Status (13)

Country Link
US (1) US5824678A (es)
EP (1) EP0777659B1 (es)
JP (1) JP2002502351A (es)
AT (1) ATE201866T1 (es)
AU (1) AU691327B2 (es)
CA (1) CA2195972A1 (es)
DE (1) DE69521208T2 (es)
DK (1) DK0777659T3 (es)
ES (1) ES2157337T3 (es)
GR (1) GR3036006T3 (es)
IL (1) IL114865A (es)
PT (1) PT777659E (es)
WO (1) WO1996005181A1 (es)

Families Citing this family (74)

* Cited by examiner, † Cited by third party
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US6117855A (en) 1996-10-07 2000-09-12 Merck Sharp & Dohme Ltd. Use of a NK-1 receptor antagonist and an antidepressant and/or an anti-anxiety agent
US6613765B1 (en) 1996-12-02 2003-09-02 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating major depressive disorders
US6114315A (en) * 1996-12-02 2000-09-05 Merck Sharp & Dohme Ltd. Use of NK-1 receptor antagonists for treating major depressive disorders with anxiety
EP0942732B1 (en) * 1996-12-02 2004-11-17 MERCK SHARP & DOHME LTD. Use of nk-1 receptor antagonists for treating movement disorders
CA2273807A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating schizophrenic disorders
AU731349B2 (en) * 1996-12-02 2001-03-29 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating sexual dysfunctions
US5977104A (en) * 1996-12-02 1999-11-02 Merck Sharp & Dohme Ltd. Use of NK-1 receptor antagonists for treating bipolar disorders
WO1998024438A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating major depressive disorders
JP2001504853A (ja) * 1996-12-02 2001-04-10 メルク シヤープ エンド ドーム リミテツド 物質使用障害の治療のためのｎｋ−１受容体拮抗薬の使用
AU736042B2 (en) * 1996-12-02 2001-07-26 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating major depressive disorders with anxiety
US6100256A (en) * 1996-12-02 2000-08-08 Merck Sharp & Dohme Ltd. Use of NK-1 receptors antagonists for treating schizophrenic disorders
EP0942730A1 (en) * 1996-12-02 1999-09-22 MERCK SHARP & DOHME LTD. Use of nk-1 receptor antagonists for treating bipolar disorders
WO1998024439A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating severe anxiety disorders
CA2273853A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating cognitive disorders
EP0942729B1 (en) * 1996-12-02 2004-09-01 MERCK SHARP & DOHME LTD. Use of nk-1 receptor antagonists for treating stress disorders
EP0977572A1 (en) * 1997-04-24 2000-02-09 Merck Sharp & Dohme Ltd. Use of nk-1 receptor antagonists for treating eating disorders
GB9716463D0 (en) * 1997-08-04 1997-10-08 Merck Sharp & Dohme Therapeutic agents
GB9716457D0 (en) * 1997-08-04 1997-10-08 Merck Sharp & Dohme Therapeutic agents
CA2298777A1 (en) * 1997-08-04 1999-02-18 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating mania
WO1999007375A1 (en) * 1997-08-04 1999-02-18 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating aggressive behaviour disorders
US6156749A (en) * 1997-12-01 2000-12-05 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating movement disorders
US6087348A (en) * 1997-12-01 2000-07-11 Merck Sharp & Dohme Ltd. Use of NK-1 receptor antagonists for treating stress disorders
US6271230B1 (en) 1997-12-01 2001-08-07 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating cognitive disorders
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US7279547B2 (en) * 2000-02-10 2007-10-09 University Of Connecticut Insecticidal compounds and methods for selection thereof
AU2001250820A1 (en) 2000-03-13 2001-09-24 Ortho-Mcneil Pharmaceutical, Inc. Novel cyclohexene derivatives useful as antagonists of the motilin receptor
AU2001247357A1 (en) 2000-03-13 2001-09-24 Ortho-Mcneil Pharmaceutical, Inc. Novel cyclobutene derivatives useful as antagonists of the motilin receptor
US6392040B2 (en) * 2000-03-13 2002-05-21 Ortho-Mcneil Pharmaceutical, Inc. Cyclopentene compounds useful as antagonists of the motilin receptor
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US20060205724A1 (en) * 2002-05-29 2006-09-14 The Regents Of The University Of California Antagonizing nk-1 receptors inhibits consumption of substances of abuse
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US8362075B2 (en) 2005-05-17 2013-01-29 Merck Sharp & Dohme Corp. Cyclohexyl sulphones for treatment of cancer
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KR20080048502A (ko) 2005-09-29 2008-06-02 머크 앤드 캄파니 인코포레이티드 멜라노코르틴-4 수용체 조절제로서의 아실화스피로피페리딘 유도체
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US20110218176A1 (en) 2006-11-01 2011-09-08 Barbara Brooke Jennings-Spring Compounds, methods, and treatments for abnormal signaling pathways for prenatal and postnatal development
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JP2010516731A (ja) 2007-01-24 2010-05-20 グラクソ グループ リミテッド ２−メトキシ−５−（５−トリフルオロメチル−テトラゾール−１−イル）−ベンジル］−（２ｓ−フェニル−ピペリジン−３ｓ−イル）−アミンを含む医薬組成物
JP5319518B2 (ja) 2007-04-02 2013-10-16 Ｍｓｄ株式会社 インドールジオン誘導体
AU2008269154B2 (en) 2007-06-27 2014-06-12 Merck Sharp & Dohme Llc 4-carboxybenzylamino derivatives as histone deacetylase inhibitors
CN102014631A (zh) 2008-03-03 2011-04-13 泰格尔医药科技公司 酪氨酸激酶抑制剂
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WO2010114780A1 (en) 2009-04-01 2010-10-07 Merck Sharp & Dohme Corp. Inhibitors of akt activity
WO2010132487A1 (en) 2009-05-12 2010-11-18 Bristol-Myers Squibb Company CRYSTALLINE FORMS OF (S)-7-([1,2,4]TRIAZOLO[1,5-a]PYRIDIN-6-YL)-4-(3,4-DICHLOROHPHENYL)-1,2,3,4-TETRAHYDROISOQUINOLINE AND USE THEREOF
US8802696B2 (en) 2009-05-12 2014-08-12 Albany Molecular Research, Inc. 7-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydroisoqu inoli and use thereof
CN102458123A (zh) 2009-05-12 2012-05-16 阿尔巴尼分子研究公司 芳基、杂芳基和杂环取代的四氢异喹啉及其用途
JP5099731B1 (ja) 2009-10-14 2012-12-19 メルク・シャープ・アンド・ドーム・コーポレーション ｐ５３活性を増大する置換ピペリジン及びその使用
EP2584903B1 (en) 2010-06-24 2018-10-24 Merck Sharp & Dohme Corp. Novel heterocyclic compounds as erk inhibitors
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US8883801B2 (en) 2010-08-23 2014-11-11 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as mTOR inhibitors
EP2613782B1 (en) 2010-09-01 2016-11-02 Merck Sharp & Dohme Corp. Indazole derivatives useful as erk inhibitors
US9242981B2 (en) 2010-09-16 2016-01-26 Merck Sharp & Dohme Corp. Fused pyrazole derivatives as novel ERK inhibitors
EP3766975A1 (en) 2010-10-29 2021-01-20 Sirna Therapeutics, Inc. Rna interference mediated inhibition of gene expression using short interfering nucleic acid (sina)
EP2654748B1 (en) 2010-12-21 2016-07-27 Merck Sharp & Dohme Corp. Indazole derivatives useful as erk inhibitors
EP2699567A1 (en) 2011-04-21 2014-02-26 Merck Sharp & Dohme Corp. Insulin-like growth factor-1 receptor inhibitors
WO2013063214A1 (en) 2011-10-27 2013-05-02 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
EP3358013B1 (en) 2012-05-02 2020-06-24 Sirna Therapeutics, Inc. Short interfering nucleic acid (sina) compositions
KR20150060724A (ko) 2012-09-28 2015-06-03 머크 샤프 앤드 돔 코포레이션 Erk 억제제인 신규 화합물
DK2925888T3 (en) 2012-11-28 2017-12-18 Merck Sharp & Dohme COMPOSITIONS AND METHODS OF CANCER TREATMENT
EP2935263B1 (en) 2012-12-20 2018-12-05 Merck Sharp & Dohme Corp. Substituted imidazopyridines as hdm2 inhibitors
US9540377B2 (en) 2013-01-30 2017-01-10 Merck Sharp & Dohme Corp. 2,6,7,8 substituted purines as HDM2 inhibitors
WO2015034925A1 (en) 2013-09-03 2015-03-12 Moderna Therapeutics, Inc. Circular polynucleotides
WO2018071283A1 (en) 2016-10-12 2018-04-19 Merck Sharp & Dohme Corp. Kdm5 inhibitors
US11098059B2 (en) 2017-11-08 2021-08-24 Merck Sharp & Dohme Corp. PRMT5 inhibitors
WO2019094311A1 (en) 2017-11-08 2019-05-16 Merck Sharp & Dohme Corp. Prmt5 inhibitors
EP3833668B1 (en) 2018-08-07 2025-03-19 Merck Sharp & Dohme LLC Prmt5 inhibitors
BR112021002267A8 (pt) 2018-08-07 2023-02-07 Merck Sharp & Dohme Inibidores de prmt5
EP3833667B1 (en) 2018-08-07 2024-03-13 Merck Sharp & Dohme LLC Prmt5 inhibitors
CN111004190A (zh) * 2019-11-08 2020-04-14 广州曼翔医药有限公司 一种阿瑞匹坦中间体的制备方法

Family Cites Families (4)

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Also Published As

Publication number Publication date
IL114865A0 (en) 1995-12-08
DK0777659T3 (da) 2001-09-03
PT777659E (pt) 2001-09-28
EP0777659A1 (en) 1997-06-11
WO1996005181A1 (en) 1996-02-22
ATE201866T1 (de) 2001-06-15
EP0777659B1 (en) 2001-06-06
DE69521208T2 (de) 2001-11-08
DE69521208D1 (de) 2001-07-12
GR3036006T3 (en) 2001-09-28
AU3185595A (en) 1996-03-07
CA2195972A1 (en) 1996-02-22
AU691327B2 (en) 1998-05-14
JP2002502351A (ja) 2002-01-22
US5824678A (en) 1998-10-20
IL114865A (en) 1999-06-20

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