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
Publication number Priority date Publication date Assignee Title
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
US6100256A (en) * 1996-12-02 2000-08-08 Merck Sharp & Dohme Ltd. Use of NK-1 receptors antagonists for treating schizophrenic disorders
AU731676B2 (en) * 1996-12-02 2001-04-05 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating stress disorders
CA2273856A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating bipolar disorders
ATE285776T1 (de) * 1996-12-02 2005-01-15 Merck Sharp & Dohme Verfahren und vorrichtung zur kompensation von durch chrominanzsignalverarbeitung verursachten luminanzstörungen
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
EP0942731B1 (en) * 1996-12-02 2004-11-17 MERCK SHARP & DOHME LTD. Use of nk-1 receptor antagonists for treating substance use disorders
AU734860B2 (en) * 1996-12-02 2001-06-21 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating cognitive disorders
US5977104A (en) * 1996-12-02 1999-11-02 Merck Sharp & Dohme Ltd. Use of NK-1 receptor antagonists for treating bipolar disorders
WO1998024441A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating major depressive disorders with anxiety
WO1998024445A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating schizophrenic disorders
WO1998024439A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating severe anxiety disorders
US6613765B1 (en) 1996-12-02 2003-09-02 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating major depressive disorders
EP0942732B1 (en) * 1996-12-02 2004-11-17 MERCK SHARP & DOHME LTD. Use of nk-1 receptor antagonists for treating movement 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
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
WO1999007376A1 (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
GB9716463D0 (en) * 1997-08-04 1997-10-08 Merck Sharp & Dohme Therapeutic agents
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
AU1230000A (en) * 1998-10-30 2000-05-22 Merck & Co., Inc. Linear process for the preparation of a morpholine compound
GB9907571D0 (en) 1999-04-06 1999-05-26 Zeneca Ltd Compounds
KR100885986B1 (ko) 1999-11-03 2009-03-03 에이엠알 테크놀로지, 인크. 노르에피네프린, 도파민 및 세로토닌의 재흡수를 방지하기위한 아릴 및 헤테로아릴 치환된테트라하이드로이소퀴놀린 및 이들의 용도
US7163949B1 (en) 1999-11-03 2007-01-16 Amr Technology, Inc. 4-phenyl substituted tetrahydroisoquinolines and use thereof
US7279547B2 (en) * 2000-02-10 2007-10-09 University Of Connecticut Insecticidal compounds and methods for selection thereof
AU2001247357A1 (en) 2000-03-13 2001-09-24 Ortho-Mcneil Pharmaceutical, Inc. Novel cyclobutene 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
WO2001068621A1 (en) 2000-03-13 2001-09-20 Ortho-Mcneil Pharmaceutical, Inc. Novel cyclohexene derivatives useful as antagonists of the motilin receptor
CA2415532C (en) 2000-07-11 2010-05-11 Albany Molecular Research, Inc. Novel 4-phenyl substituted tetrahydroisoquinolines therapeutic use thereof
WO2003101459A1 (en) * 2002-05-29 2003-12-11 The Regents Of The University Of California Antagonizing nk1 receptors inhibits consumption of substances of abuse
KR101389246B1 (ko) 2004-07-15 2014-04-24 브리스톨-마이어스스퀴브컴파니 아릴- 및 헤테로아릴-치환된 테트라히드로이소퀴놀린, 및 이것의 노르에피네프린, 도파민 및 세로토닌의 재흡수를 차단하기 위한 용도
EP1888050B1 (en) 2005-05-17 2012-03-21 Merck Sharp & Dohme Ltd. cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid for the treatment of cancer
ZA200800440B (en) 2005-07-15 2009-12-30 Amr Technology Inc Aryl-and heteroaryl-substituted tetrahydrobenzazepines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin
US8293900B2 (en) 2005-09-29 2012-10-23 Merck Sharp & Dohme Corp Acylated spiropiperidine derivatives as melanocortin-4 receptor modulators
GB0603041D0 (en) 2006-02-15 2006-03-29 Angeletti P Ist Richerche Bio Therapeutic compounds
EP2698157B1 (en) 2006-09-22 2015-05-20 Merck Sharp & Dohme Corp. Method of treatment using fatty acid synthesis inhibitors
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
EP2805945B1 (en) 2007-01-10 2019-04-03 MSD Italia S.r.l. Amide substituted indazoles as poly(ADP-ribose)polymerase (PARP) inhibitors
JP2010516734A (ja) 2007-01-24 2010-05-20 グラクソ グループ リミテッド ３，５−ジアミノ−６−（２，３−ジクロロフェニル）−１，２，４−トリアジンまたはｒ（−）−２，４−ジアミノ−５−（２，３−ジクロロフェニル）−６−フルオロメチルピリミジンを含む医薬組成物
US8106086B2 (en) 2007-04-02 2012-01-31 Msd K.K. Indoledione derivative
US8389553B2 (en) 2007-06-27 2013-03-05 Merck Sharp & Dohme Corp. 4-carboxybenzylamino derivatives as histone deacetylase inhibitors
KR20100126467A (ko) 2008-03-03 2010-12-01 타이거 파마테크 티로신 키나아제 억제제
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
US8691825B2 (en) 2009-04-01 2014-04-08 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
CN102638982B (zh) 2009-05-12 2015-07-08 百时美施贵宝公司 (S)-7-([1,2,4]三唑并[1,5-a]吡啶-6-基)-4-(3,4-二氯苯基)-1,2,3,4-四氢异喹啉的晶型及其用途
KR101830447B1 (ko) 2009-05-12 2018-02-20 알바니 몰레큘라 리써치, 인크. 7-(［1,2,4］트리아졸로［1,5-α］피리딘-6-일)-4-(3,4-디클로로페닐)-1,2,3,4-테트라하이드로이소퀴놀린 및 이의 용도
EP2488028B1 (en) 2009-10-14 2020-08-19 Merck Sharp & Dohme Corp. Substituted piperidines that increase p53 activity and the uses thereof
WO2011163330A1 (en) 2010-06-24 2011-12-29 Merck Sharp & Dohme Corp. Novel heterocyclic compounds as erk inhibitors
CN107090456B (zh) 2010-08-02 2022-01-18 瑟纳治疗公司 使用短干扰核酸的RNA干扰介导的联蛋白（钙粘蛋白关联蛋白质），β1基因表达的抑制
JP2013537423A (ja) 2010-08-17 2013-10-03 メルク・シャープ・エンド・ドーム・コーポレイション 低分子干渉核酸（ｓｉＮＡ）を用いたＢ型肝炎ウイルス（ＨＢＶ）遺伝子発現のＲＮＡ干渉媒介性阻害
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
EP2615916B1 (en) 2010-09-16 2017-01-04 Merck Sharp & Dohme Corp. Fused pyrazole derivatives as novel erk inhibitors
DK2632472T3 (en) 2010-10-29 2018-03-19 Sirna Therapeutics Inc RNA INTERFERENCE-MEDIATED INHIBITION OF GENE EXPRESSION USING SHORT INTERFERRING NUCLEIC ACIDS (SINA)
WO2012087772A1 (en) 2010-12-21 2012-06-28 Schering Corporation Indazole derivatives useful as erk inhibitors
EP2699568A1 (en) 2011-04-21 2014-02-26 Piramal Enterprises Limited A crystalline form of a salt of a morpholino sulfonyl indole derivative and a process for its preparation
WO2013063214A1 (en) 2011-10-27 2013-05-02 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
EP2844261B1 (en) 2012-05-02 2018-10-17 Sirna Therapeutics, Inc. SHORT INTERFERING NUCLEIC ACID (siNA) COMPOSITIONS
CN105050598B (zh) 2012-09-28 2018-04-27 默沙东公司 作为erk抑制剂的新型化合物
RS56680B1 (sr) 2012-11-28 2018-03-30 Merck Sharp & Dohme Kompozicije i postupci za lečenje kancera
US8846657B2 (en) 2012-12-20 2014-09-30 Merck Sharp & Dohme Corp. Substituted imidazopyridines as HDM2 inhibitors
WO2014120748A1 (en) 2013-01-30 2014-08-07 Merck Sharp & Dohme Corp. 2,6,7,8 substituted purines as hdm2 inhibitors
EP3041938A1 (en) 2013-09-03 2016-07-13 Moderna Therapeutics, Inc. Circular polynucleotides
US10975084B2 (en) 2016-10-12 2021-04-13 Merck Sharp & Dohme Corp. KDM5 inhibitors
US11098059B2 (en) 2017-11-08 2021-08-24 Merck Sharp & Dohme Corp. PRMT5 inhibitors
EP3706742B1 (en) 2017-11-08 2023-03-15 Merck Sharp & Dohme LLC Prmt5 inhibitors
CA3108388A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
EP3833667B1 (en) 2018-08-07 2024-03-13 Merck Sharp & Dohme LLC Prmt5 inhibitors
EP3833668B1 (en) 2018-08-07 2025-03-19 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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2112397A1 (en) * 1991-08-20 1993-03-04 Raymond Baker Azacyclic compounds, processes for their preparation and pharmaceutical compositions containing them
CA2099233A1 (en) * 1992-06-29 1993-12-30 Conrad P. Dorn Morpholine and thiomorpholine tachykinin receptor antagonists
IL111960A (en) * 1993-12-17 1999-12-22 Merck & Co Inc Morpholines and thiomorpholines their preparation and pharmaceutical compositions containing them
DE69428913T2 (de) * 1993-12-29 2002-05-29 Merck Sharp & Dohme Ltd., Hoddesdon Substituierte morpholinderivate und ihre verwendung als arzneimittel

Also Published As

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

Similar Documents

Publication Publication Date Title
ES2157337T3 (es) Derivados de morfolina y su uso como agentes terapeuticos.
IL176110A0 (en) Azabicyclic heterocycles as cannabinoid receptor modulators
GB9426103D0 (en) Therapeutic agents
ATE360630T1 (de) Azabicyclische heterocyclen als modulatoren des cannabinoidrezeptors
ES2188584T3 (es) Derivados heterociclicos de amina.
TR199901417T2 (xx) Analjezik etkisi olan yeni bile�imler.
ES2159558T3 (es) Derivados de guanidina como inhibidores del intercambio na+/h+ en las celulas.
PT880508E (pt) Derivados de quinazolina como inibidores de vegf
BR9901491A (pt) 7-hetero-biciclo [2.2.1] - heptanos.
TR200201505T2 (tr) Terapötik maddeler olarak pirazolopirimidinler
IL144236A0 (en) Tetrahydropyran derivatives and their use as therapeutic agents
DK1346041T3 (da) Terapeutiske midler og fremgangsmåder til anvendelse deraf til behandling af en amyloidogen sygdom
PA8485601A1 (es) Azalidas de 13 miembros y su uso como agentes antibioticos.
ES2098947T3 (es) Derivados de beta,beta-dimetil-4-piperidinoetanamina como inhibidores de la biosintesis del colesterol.
ES2135769T3 (es) Derivados de isotiourea como inhibidores de no-sintasa.
EA200500882A1 (ru) N-арилсульфонил-3-аминоалкоксииндолы
DK0759026T3 (da) Amidderivater og deres terapeutiske anvendelse
AR004474A1 (es) Compuestos de 10-aminoalifatil-dibenz [b,f]oxepinas antineurodegenerativamente activas, utiles para el tratamiento de estados neurodegenerativos y composiciones farmaceuticas que los contienen
JO2231B1 (en) Derivatives of Trahydroperan and its use as a therapeutic agent
PA8471801A1 (es) Derivados de higromicina a
ES2163730T3 (es) Derivados espirocetales y su uso como agentes terapeuticos.
AP9901559A0 (en) Tricyclic 3-keto derivatives of 6-0-methylerythromycin.
PA8471901A1 (es) Derivados de 2"-desoxi higromicina
DK0802920T3 (da) Fusacandin-antisvampemidler
ECSP993239A (es) Derivados de higromicina

Legal Events

Date Code Title Description
FG2A Definitive protection

Ref document number: 777659

Country of ref document: ES