IL114865A - Morpholine derivatives pharmaceutical compositions containing them and their use - Google Patents

Morpholine derivatives pharmaceutical compositions containing them and their use

Info

Publication number
IL114865A
IL114865A IL11486595A IL11486595A IL114865A IL 114865 A IL114865 A IL 114865A IL 11486595 A IL11486595 A IL 11486595A IL 11486595 A IL11486595 A IL 11486595A IL 114865 A IL114865 A IL 114865A
Authority
IL
Israel
Prior art keywords
4alkyl
pct
hydrogen
4alkoxy
hydroxy
Prior art date
Application number
IL11486595A
Other languages
English (en)
Other versions
IL114865A0 (en
Original Assignee
Merck Sharp & Dohme
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 & Dohme filed Critical Merck Sharp & Dohme
Publication of IL114865A0 publication Critical patent/IL114865A0/xx
Publication of IL114865A publication Critical patent/IL114865A/xx

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)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (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)
IL11486595A 1994-08-15 1995-08-08 Morpholine derivatives pharmaceutical compositions containing them and their use IL114865A (en)

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 (2)

Publication Number Publication Date
IL114865A0 IL114865A0 (en) 1995-12-08
IL114865A true IL114865A (en) 1999-06-20

Family

ID=26305450

Family Applications (1)

Application Number Title Priority Date Filing Date
IL11486595A IL114865A (en) 1994-08-15 1995-08-08 Morpholine derivatives pharmaceutical compositions containing them and their use

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
CA2273853A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating cognitive disorders
ATE282417T1 (de) * 1996-12-02 2004-12-15 Merck Sharp & Dohme Die verwendung von nk-1 rezeptor antagonisten für die behandlung von bewegungsstörungen
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
US6613765B1 (en) 1996-12-02 2003-09-02 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating major depressive disorders
EP0942734A1 (en) * 1996-12-02 1999-09-22 MERCK SHARP & DOHME LTD. Use of nk-1 receptor antagonists for treating severe anxiety disorders
US5977104A (en) * 1996-12-02 1999-11-02 Merck Sharp & Dohme Ltd. Use of NK-1 receptor antagonists for treating bipolar disorders
JP2001504851A (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 性的機能不全の治療のためのｎｋ−１受容体拮抗薬の使用
CA2273807A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating schizophrenic disorders
US6100256A (en) * 1996-12-02 2000-08-08 Merck Sharp & Dohme Ltd. Use of NK-1 receptors antagonists for treating schizophrenic disorders
JP2001504850A (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 不安を伴う重抑鬱性障害を治療するためのｎｋ−１受容体拮抗薬の使用
DE69732133T2 (de) * 1996-12-02 2005-12-22 Merck Sharp & Dohme Ltd., Hoddesdon Verwendung von NK-1 Rezeptorantagonisten zur Behandlung von schweren Depressionen
WO1998024443A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating bipolar disorders
ATE282416T1 (de) * 1996-12-02 2004-12-15 Merck Sharp & Dohme Die verwendung von nk-1 rezeptor antagonisten für die behandlung von substanz-verwendung störungen
JP2001504849A (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 ストレス障害の治療のためのｎｋ−１受容体拮抗薬の使用
JP2001524960A (ja) * 1997-04-24 2001-12-04 メルク シヤープ エンド ドーム リミテツド 摂食障害を治療するためのｎｋ−１受容体拮抗薬の使用
CA2298777A1 (en) * 1997-08-04 1999-02-18 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating mania
GB9716457D0 (en) * 1997-08-04 1997-10-08 Merck Sharp & Dohme Therapeutic agents
AU737019B2 (en) * 1997-08-04 2001-08-09 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating aggressive behaviour disorders
GB9716463D0 (en) * 1997-08-04 1997-10-08 Merck Sharp & Dohme Therapeutic agents
US6271230B1 (en) 1997-12-01 2001-08-07 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating cognitive disorders
US6087348A (en) * 1997-12-01 2000-07-11 Merck Sharp & Dohme Ltd. Use of NK-1 receptor antagonists for treating stress disorders
US6156749A (en) * 1997-12-01 2000-12-05 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating movement disorders
WO2000026214A1 (en) * 1998-10-30 2000-05-11 Merck & Co., Inc. Linear process for the preparation of a morpholine compound
GB9907571D0 (en) * 1999-04-06 1999-05-26 Zeneca Ltd Compounds
US7163949B1 (en) 1999-11-03 2007-01-16 Amr Technology, Inc. 4-phenyl substituted tetrahydroisoquinolines and use thereof
MXPA02004330A (es) 1999-11-03 2004-07-30 Albany Molecular Res Inc Tetrahidroisoquinolinas aril-y heteroaril-sustituidas y uso de las mismas para bloquear la recaptacion de norepinefrina, dopamina y serotonina..
US7279547B2 (en) * 2000-02-10 2007-10-09 University Of Connecticut Insecticidal compounds and methods for selection thereof
US6384031B2 (en) 2000-03-13 2002-05-07 Ortho-Mcneil Pharmaceutical, Inc. Cyclobutene derivatives useful as antagonists of the motilin receptor
AU2001250820A1 (en) 2000-03-13 2001-09-24 Ortho-Mcneil Pharmaceutical, Inc. Novel cyclohexene derivatives useful as antagonists of the motilin receptor
WO2001068620A1 (en) * 2000-03-13 2001-09-20 Ortho-Mcneil Pharmaceutical, Inc. Novel cyclopentene derivatives useful as antagonists of the motilin receptor
KR100821410B1 (ko) 2000-07-11 2008-04-10 에이엠알 테크놀로지, 인크. 4-페닐 치환된 테트라하이드로이소퀴놀린 및 이의치료학적 용도
EP1556054A4 (en) * 2002-05-29 2007-09-05 Univ California ANTAGONIZING NK1 RECEPTORS RESTRICT DRUG ABUSE
UA91341C2 (ru) 2004-07-15 2010-07-26 Амр Текнолоджи, Інк. Арил- и гетероарилзамещенные тетрагидроизохинолины и их применение для блокирования обратного захвата норэпинефрина, допамина и серотонина
WO2006123182A2 (en) 2005-05-17 2006-11-23 Merck Sharp & Dohme Limited Cyclohexyl sulphones for treatment of cancer
UA95454C2 (uk) 2005-07-15 2011-08-10 Амр Текнолоджи, Інк. Арил- і гетероарилзаміщені тетрагідробензазепіни і їх застосування для блокування зворотного захоплення норепінефрину, допаміну і серотоніну
BRPI0616463A2 (pt) 2005-09-29 2011-06-21 Merck & Co Inc composto, composição farmacêutica, e, uso de um composto
GB0603041D0 (en) 2006-02-15 2006-03-29 Angeletti P Ist Richerche Bio Therapeutic compounds
JP5489333B2 (ja) 2006-09-22 2014-05-14 メルク・シャープ・アンド・ドーム・コーポレーション 脂肪酸合成阻害剤を用いた治療の方法
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
AR064777A1 (es) 2007-01-10 2009-04-22 Inst Di Reserche D Biolog Mole Indazoles sustituidos con amida como inhibidores de poli (adp- ribosa) polimerasa (parp)
WO2008090114A1 (en) 2007-01-24 2008-07-31 Glaxo Group Limited Pharmaceutical compositions comprising 2-methoxy-5- (5-trifluoromethyl-tetrazol-i-yl-benzyl) - (2s-phenyl-piperidin-3s-yl-)
CA2682727C (en) 2007-04-02 2016-03-22 Banyu Pharmaceutical Co., Ltd. Indoledione derivative
EP3103791B1 (en) 2007-06-27 2018-01-31 Merck Sharp & Dohme Corp. 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
US9156812B2 (en) 2008-06-04 2015-10-13 Bristol-Myers Squibb Company Crystalline form of 6-[(4S)-2-methyl-4-(2-naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyridazin-3-amine
WO2010114780A1 (en) 2009-04-01 2010-10-07 Merck Sharp & Dohme Corp. Inhibitors of akt activity
EP2429295B1 (en) 2009-05-12 2013-12-25 Albany Molecular Research, Inc. Aryl, heteroaryl, and heterocycle substituted tetrahydroisoquinolines and use thereof
AU2010247763B2 (en) 2009-05-12 2015-12-24 Albany Molecular Research, Inc. 7-([1,2,4,]triazolo[1,5,-a]pyridin-6-yl)-4-(3,4-dichlorophenyl)-1,2,3,4- tetrahydroisoquinoline and use thereof
US8815894B2 (en) 2009-05-12 2014-08-26 Bristol-Myers Squibb Company Crystalline forms of (S)-7-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydroisoquinoline and use thereof
US8859776B2 (en) 2009-10-14 2014-10-14 Merck Sharp & Dohme Corp. Substituted piperidines that increase p53 activity and the uses thereof
US8999957B2 (en) 2010-06-24 2015-04-07 Merck Sharp & Dohme Corp. Heterocyclic compounds as ERK inhibitors
CA2805265A1 (en) 2010-08-02 2012-02-09 Merck Sharp & Dohme Corp. Rna interference mediated inhibition of catenin (cadherin-associated protein), beta 1 (ctnnb1) gene expression using short interfering nucleic acid (sina)
WO2012024170A2 (en) 2010-08-17 2012-02-23 Merck Sharp & Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF HEPATITIS B VIRUS (HBV) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
US8883801B2 (en) 2010-08-23 2014-11-11 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as mTOR inhibitors
WO2012030685A2 (en) 2010-09-01 2012-03-08 Schering Corporation 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
WO2012058210A1 (en) 2010-10-29 2012-05-03 Merck Sharp & Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACIDS (siNA)
EP2654748B1 (en) 2010-12-21 2016-07-27 Merck Sharp & Dohme Corp. Indazole derivatives useful as erk inhibitors
WO2012143879A1 (en) 2011-04-21 2012-10-26 Piramal Healthcare Limited A crystalline form of a salt of a morpholino sulfonyl indole derivative and a process for its preparation
EP2770987B1 (en) 2011-10-27 2018-04-04 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
WO2013165816A2 (en) 2012-05-02 2013-11-07 Merck Sharp & Dohme Corp. SHORT INTERFERING NUCLEIC ACID (siNA) COMPOSITIONS
WO2014052563A2 (en) 2012-09-28 2014-04-03 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
ME02925B (me) 2012-11-28 2018-04-20 Merck Sharp & Dohme Kompozicije i postupci za liječenje kancera
TW201429969A (zh) 2012-12-20 2014-08-01 Merck Sharp & Dohme 作爲ｈｄｍ２抑制劑之經取代咪唑吡啶
WO2014120748A1 (en) 2013-01-30 2014-08-07 Merck Sharp & Dohme Corp. 2,6,7,8 substituted purines as hdm2 inhibitors
US20160194368A1 (en) 2013-09-03 2016-07-07 Moderna Therapeutics, Inc. Circular polynucleotides
US10975084B2 (en) 2016-10-12 2021-04-13 Merck Sharp & Dohme Corp. KDM5 inhibitors
EP3706747B1 (en) 2017-11-08 2025-09-03 Merck Sharp & Dohme LLC Prmt5 inhibitors
US10947234B2 (en) 2017-11-08 2021-03-16 Merck Sharp & Dohme Corp. PRMT5 inhibitors
WO2020033282A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
US11981701B2 (en) 2018-08-07 2024-05-14 Merck Sharp & Dohme Llc PRMT5 inhibitors
WO2020033288A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. 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

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CA2112397A1 (en) * 1991-08-20 1993-03-04 Raymond Baker Azacyclic compounds, processes for their preparation and pharmaceutical compositions containing them
IL106142A (en) * 1992-06-29 1997-03-18 Merck & Co Inc Morpholine and thiomorpholine tachykinin receptor antagonists, their preparation and pharmaceutical compositions containing them
IL111960A (en) * 1993-12-17 1999-12-22 Merck & Co Inc Morpholines and thiomorpholines their preparation and pharmaceutical compositions containing them
CA2178219C (en) * 1993-12-29 2005-03-22 Raymond Baker Substituted morpholine derivatives and their use as therapeutic agents

Also Published As

Publication number Publication date
JP2002502351A (ja) 2002-01-22
DK0777659T3 (da) 2001-09-03
EP0777659A1 (en) 1997-06-11
GR3036006T3 (en) 2001-09-28
ES2157337T3 (es) 2001-08-16
EP0777659B1 (en) 2001-06-06
PT777659E (pt) 2001-09-28
IL114865A0 (en) 1995-12-08
US5824678A (en) 1998-10-20
ATE201866T1 (de) 2001-06-15
DE69521208D1 (de) 2001-07-12
AU3185595A (en) 1996-03-07
AU691327B2 (en) 1998-05-14
CA2195972A1 (en) 1996-02-22
DE69521208T2 (de) 2001-11-08
WO1996005181A1 (en) 1996-02-22

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