DK0737192T3 - Substituerede morpholinderivater og deres anvendelse som terapeutiske midler - Google Patents

Substituerede morpholinderivater og deres anvendelse som terapeutiske midler

Info

Publication number
DK0737192T3
DK0737192T3 DK95904621T DK95904621T DK0737192T3 DK 0737192 T3 DK0737192 T3 DK 0737192T3 DK 95904621 T DK95904621 T DK 95904621T DK 95904621 T DK95904621 T DK 95904621T DK 0737192 T3 DK0737192 T3 DK 0737192T3
Authority
DK
Denmark
Prior art keywords
hydrogen
4alkyl
substituted
halogen
optionally substituted
Prior art date
Application number
DK95904621T
Other languages
English (en)
Inventor
Raymond Baker
Timothy Harrison
Angus Murray Macleod
Andrew Pate Owens
Eileen Mary Seward
Christopher John Swain
Martin Richard Teall
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 GB9326480A external-priority patent/GB9326480D0/en
Priority claimed from GB9407189A external-priority patent/GB9407189D0/en
Priority claimed from GB9408065A external-priority patent/GB9408065D0/en
Priority claimed from GB9416428A external-priority patent/GB9416428D0/en
Application filed by Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Application granted granted Critical
Publication of DK0737192T3 publication Critical patent/DK0737192T3/da

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
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6527—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07F9/6533—Six-membered rings
    • 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
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Psychiatry (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)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
DK95904621T 1993-12-29 1994-12-23 Substituerede morpholinderivater og deres anvendelse som terapeutiske midler DK0737192T3 (da)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
GB9326480A GB9326480D0 (en) 1993-12-29 1993-12-29 Therapeutic agents
GB9407189A GB9407189D0 (en) 1994-04-12 1994-04-12 Therapeutic agents
GB9408065A GB9408065D0 (en) 1994-04-22 1994-04-22 Therapeutic agents
GB9416428A GB9416428D0 (en) 1994-08-15 1994-08-15 Therapeutic agents
PCT/GB1994/002819 WO1995018124A1 (en) 1993-12-29 1994-12-23 Substituted morpholine derivatives and their use as therapeutic agents

Publications (1)

Publication Number Publication Date
DK0737192T3 true DK0737192T3 (da) 2001-11-26

Family

ID=27451102

Family Applications (1)

Application Number Title Priority Date Filing Date
DK95904621T DK0737192T3 (da) 1993-12-29 1994-12-23 Substituerede morpholinderivater og deres anvendelse som terapeutiske midler

Country Status (24)

Country Link
US (1) US5612337A (da)
EP (3) EP1462450B1 (da)
JP (2) JP3071467B2 (da)
KR (1) KR100286412B1 (da)
CN (1) CN1067683C (da)
AT (3) ATE278687T1 (da)
BG (1) BG62616B1 (da)
BR (1) BR9408442A (da)
CA (1) CA2178219C (da)
CZ (1) CZ288176B6 (da)
DE (3) DE69434063D1 (da)
DK (1) DK0737192T3 (da)
ES (1) ES2164758T3 (da)
HU (1) HU221139B1 (da)
IL (1) IL112134A (da)
LV (1) LV11687B (da)
NO (1) NO307090B1 (da)
NZ (1) NZ277839A (da)
PL (1) PL181214B1 (da)
RU (1) RU2131426C1 (da)
SG (1) SG52217A1 (da)
SK (1) SK283070B6 (da)
TW (1) TW449588B (da)
WO (1) WO1995018124A1 (da)

Families Citing this family (133)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5719147A (en) * 1992-06-29 1998-02-17 Merck & Co., Inc. Morpholine and thiomorpholine tachykinin receptor antagonists
WO1995030674A1 (en) * 1994-05-05 1995-11-16 Merck Sharp & Dohme Limited Morpholine derivatives and their use as antagonists of tachikinins
JP2002502351A (ja) * 1994-08-15 2002-01-22 メルク シヤープ エンド ドーム リミテツド モルホリン誘導体及び治療薬としてそれらの使用
GB9417956D0 (en) * 1994-09-02 1994-10-26 Merck Sharp & Dohme Therapeutic agents
GB9426104D0 (en) * 1994-12-23 1995-02-22 Merck Sharp & Dohme Use of surfactants and emulsions
GB9505491D0 (en) * 1995-03-18 1995-05-03 Merck Sharp & Dohme Therapeutic agents
GB9513972D0 (en) * 1995-07-08 1995-09-06 Merck Sharp & Dohme Pharmaceutical compositions
GB9523244D0 (en) * 1995-11-14 1996-01-17 Merck Sharp & Dohme Therapeutic agents
US5891875A (en) * 1996-05-20 1999-04-06 Eli Lilly And Company Morpholinyl tachykinin receptor antagonists
ATE265209T1 (de) * 1996-07-17 2004-05-15 Merck & Co Inc Änderung des zirkadischen rhythmus mit nicht- peptidischen neurokinin-1 rezeptor antagonisten
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
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
US6613765B1 (en) 1996-12-02 2003-09-02 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating major depressive disorders
CA2273853A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating cognitive disorders
CA2273807A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating schizophrenic disorders
EP0942734A1 (en) * 1996-12-02 1999-09-22 MERCK SHARP & DOHME LTD. Use of nk-1 receptor antagonists for treating severe anxiety 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
ATE282417T1 (de) * 1996-12-02 2004-12-15 Merck Sharp & Dohme Die verwendung von nk-1 rezeptor antagonisten für die behandlung von bewegungsstörungen
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
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
US6100256A (en) * 1996-12-02 2000-08-08 Merck Sharp & Dohme Ltd. Use of NK-1 receptors antagonists for treating schizophrenic disorders
US5977104A (en) * 1996-12-02 1999-11-02 Merck Sharp & Dohme Ltd. Use of NK-1 receptor antagonists for treating bipolar disorders
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
WO1998024443A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating bipolar disorders
GB9700555D0 (en) * 1997-01-13 1997-03-05 Merck Sharp & Dohme Therapeutic agents
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
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
AU737019B2 (en) * 1997-08-04 2001-08-09 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating aggressive behaviour disorders
CA2298777A1 (en) * 1997-08-04 1999-02-18 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating mania
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
US6156749A (en) * 1997-12-01 2000-12-05 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating movement disorders
US5972938A (en) 1997-12-01 1999-10-26 Merck & Co., Inc. Method for treating or preventing psychoimmunological disorders
GB9810092D0 (en) * 1998-05-11 1998-07-08 Merck Sharp & Dohme Therapeutic agents
GB9812617D0 (en) * 1998-06-11 1998-08-12 Merck Sharp & Dohme Therapeutic use
GB9812664D0 (en) * 1998-06-11 1998-08-12 Merck Sharp & Dohme Therapeutic use
JP2002517448A (ja) * 1998-06-11 2002-06-18 メルク シャープ エンド ドーム リミテッド 精神障害の治療用ｎｋ−１受容体アンタゴニストの使用
GB9812662D0 (en) * 1998-06-11 1998-08-12 Merck Sharp & Dohme Therapeutic use
JP2002517446A (ja) * 1998-06-11 2002-06-18 メルク シャープ エンド ドーム リミテッド 精神障害の治療のためのｎｋ−１受容体アンタゴニストの使用
GB9813025D0 (en) * 1998-06-16 1998-08-12 Merck Sharp & Dohme Chemical synthesis
GB9816897D0 (en) * 1998-08-04 1998-09-30 Merck Sharp & Dohme Therapeutic use
CA2348526A1 (en) * 1998-10-30 2000-05-11 Merck & Co., Inc. Process for the preparation of 2-(r)-(1- (r)-(3,5-bis (trifluoromethyl) phenyl)ethoxy) -4-((5-dimethylaminomethyl) -1,2,3-triazol -4-yl)methyl) -3-(s)-(4- fluorophenyl) morpholine
WO2000026214A1 (en) * 1998-10-30 2000-05-11 Merck & Co., Inc. Linear process for the preparation of a morpholine compound
EP1394150B1 (en) * 1999-02-24 2011-01-19 F. Hoffmann-La Roche AG 4-Phenylpyridine derivatives and their use as NK-1 receptor antagonists
SI1157005T1 (en) 1999-02-24 2005-02-28 F. Hoffmann-La Roche Ag 3-phenylpyridine derivatives and their use as nk-1 receptor antagonists
HRP20010603A2 (en) 1999-02-24 2002-08-31 Hoffmann La Roche Phenyl-and pyridinyl derivatives
US6291465B1 (en) 1999-03-09 2001-09-18 Hoffmann-La Roche Inc. Biphenyl derivatives
TW550258B (en) 1999-05-31 2003-09-01 Hoffmann La Roche 4-phenyl-pyrimidine derivatives
JO2308B1 (en) 1999-05-31 2005-09-12 اف. هوفمان- لاروش أيه جي‏ Derivatives of phenylpyrmidine
EP1228068A1 (en) * 1999-10-29 2002-08-07 Merck & Co., Inc. Polymorphic form of a tachykinin receptor antagonist
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..
PT1103545E (pt) * 1999-11-29 2004-03-31 Hoffmann La Roche 2-(3,5-bis-trifluorometil-fenil)-n-metil-n-(6-morfolin-4-il-4-o-totil-piridin-3-il)-isobutiramida
US6452001B2 (en) 2000-05-25 2002-09-17 Hoffmann-La Roche Inc. Diazapane derivatives useful as antagonists of neurokinin 1 receptor and methods for their formation
AR030284A1 (es) 2000-06-08 2003-08-20 Merck & Co Inc Proceso para la sintesis de (2r, 2-alfa-r,3a) -2-[1-(3,5-bis(trifluorometil) fenil) etoxi]-3-(4-fluorofenil)-1,4-oxazina; dicho compuesto y sus formas polimorficas
US6482829B2 (en) 2000-06-08 2002-11-19 Hoffmann-La Roche Inc. Substituted heterocyclic siprodecane compound active as an antagonist of neurokinin 1 receptor
AU2001269749A1 (en) * 2000-06-09 2001-12-24 Merck And Co., Inc. Trans-glycosidation process for the synthesis of (2r, 2-alpha-r, 3a)-2-(1-(3,5-bis(trifluoromethyl)phenyl) ethoxy)-3-(4-fluorophenyl)-1,4-oxazine
KR100821410B1 (ko) 2000-07-11 2008-04-10 에이엠알 테크놀로지, 인크. 4-페닐 치환된 테트라하이드로이소퀴놀린 및 이의치료학적 용도
PT1303490E (pt) 2000-07-14 2008-09-04 Hoffmann La Roche Óxidos de aminas como pró-fármacos de antagonistas dosreceptores nk1, de derivados de 4-fenil-piridina
TWI287003B (en) 2000-07-24 2007-09-21 Hoffmann La Roche 4-phenyl-pyridine derivatives
TWI259180B (en) 2000-08-08 2006-08-01 Hoffmann La Roche 4-Phenyl-pyridine derivatives
GB0020721D0 (en) * 2000-08-22 2000-10-11 Merck Sharp & Dohme Therapeutic agents
YU39503A (sh) 2000-11-22 2006-05-25 F. Hoffmann-La Roche Ag. Derivati pirimidina
US6642226B2 (en) 2001-02-06 2003-11-04 Hoffman-La Roche Inc. Substituted phenyl-piperidine methanone compounds
DK1406606T3 (da) * 2001-07-16 2007-03-05 Ortho Mcneil Pharm Inc Carbamatforbindelser til forebyggelse eller behandling af neuropatisk smerte og smerte forbundet med klynge- og migrænehovedpine
US6849624B2 (en) 2001-07-31 2005-02-01 Hoffmann-La Roche Inc. Aromatic and heteroaromatic substituted amides
US6638981B2 (en) 2001-08-17 2003-10-28 Epicept Corporation Topical compositions and methods for treating pain
AR039625A1 (es) * 2002-04-18 2005-03-02 Merck & Co Inc Proceso para la preparacion de 5-((2(r)--(1(r)- (3,5-bis (trifluormetil) fenil)etoxi-3 (s) - (4-fluorfenil) -4-morfolinil) metil) -1,2-dihidro-3h-1,2,4-triazol-3-ona
ATE366576T1 (de) * 2003-01-31 2007-08-15 Hoffmann La Roche Neue kristallmodifikation von 2-(3,5-bis- trifluormethyl-phenyl)-n-6-(1,1-dioxo-1lamda-6-
RU2228752C1 (ru) * 2003-03-21 2004-05-20 Государственный научный центр - Институт биофизики Фармацевтическая композиция, содержащая ондансетрон и бензамид
SI1643998T1 (sl) 2003-07-03 2007-12-31 Hoffmann La Roche Dvojni nk1/nk3 antagonisti za zdravljenje shizofrenije
TWI280239B (en) 2003-07-15 2007-05-01 Hoffmann La Roche Process for preparation of pyridine derivatives
ES2246687B2 (es) 2004-02-11 2006-11-16 Miguel Muñoz Saez Utilizacion de antagonistas no peptidicos de receptores nk1 para la produccion de apoptosis en celulas tumorales.
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
JP2008525313A (ja) 2004-12-27 2008-07-17 エーザイ・アール・アンド・ディー・マネジメント株式会社 抗痴呆薬の安定化方法
ES2329827T3 (es) 2005-02-22 2009-12-01 F. Hoffmann-La Roche Ag Antagonistas de nk1.
CA2602445C (en) 2005-03-23 2013-08-20 F.Hoffmann-La Roche Ag Metabolites for nk-i antagonists for emesis
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
DE602006011485D1 (de) * 2005-09-23 2010-02-11 Hoffmann La Roche Neue dosierformulierung
BRPI0616463A2 (pt) 2005-09-29 2011-06-21 Merck & Co Inc composto, composição farmacêutica, e, uso de um composto
EP2266980A1 (en) * 2005-10-05 2010-12-29 Ranbaxy Laboratories Limited Polymorphic form of aprepitant intermediate
RU2392277C2 (ru) * 2005-12-28 2010-06-20 Асино Фарма Аг Способ получения рацемического небиволола
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
MX2009011051A (es) 2007-04-20 2009-10-30 Hoffmann La Roche Derivados de pirrolidina como antagonistas del receptor nk1/nk3 doble.
EP3103791B1 (en) 2007-06-27 2018-01-31 Merck Sharp & Dohme Corp. 4-carboxybenzylamino derivatives as histone deacetylase inhibitors
BRPI0815658A2 (pt) 2007-08-07 2015-02-18 Hoffmann La Roche Aril-éter pirrolidina como antagonistas do receptor nk3
WO2009104080A2 (en) 2008-02-20 2009-08-27 Targia Pharmaceuticals Cns pharmaceutical compositions and methods of use
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
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
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
EP2429295B1 (en) 2009-05-12 2013-12-25 Albany Molecular Research, Inc. Aryl, heteroaryl, and heterocycle substituted tetrahydroisoquinolines 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
US8487102B2 (en) 2010-04-20 2013-07-16 Hoffmann-La Roche Inc. Pyrrazolopyridine compounds as dual NK1/NK3 receptor antagonists
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)
ES2376564B1 (es) 2010-08-12 2013-01-24 Manuel Vicente Salinas Martín Utilización de anticuerpos contra los receptores nk1, nk2 y/o nk3, para producir apoptosis en las células tumorales y modificar el estroma, la inmunidad y la vascularización intra y peritumorales, como tratamiento del cáncer.
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
EP2837381A4 (en) 2011-12-13 2015-12-09 Servicio Andaluz De Salud USE OF MEDICAMENTS FOR THE TREATMENT OF CANCER THAT CHANGE THE PERITUMORAL ENVIRONMENT
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
ES2493693B1 (es) 2013-02-11 2015-07-07 Servicio Andaluz De Salud Método para predecir o pronosticar la respuesta de un sujeto humano que padece un cáncer al tratamiento con un antagonista del receptor NK1
US20160194368A1 (en) 2013-09-03 2016-07-07 Moderna Therapeutics, Inc. Circular polynucleotides
ES2541870B1 (es) 2013-12-27 2016-05-12 Servicio Andaluz De Salud Uso de antagonistas no peptídicos de NK1 en una determinada dosis para el tratamiento del cáncer
WO2015101596A2 (en) * 2013-12-30 2015-07-09 Oncoprevent Gmbh Neurokinin-1 receptor antagonists for use in a method of prevention of cancer
TW201613888A (en) 2014-09-26 2016-04-16 Helsinn Healthcare Sa Crystalline forms of an NK-1 antagonist
US10005803B2 (en) 2015-10-06 2018-06-26 Helsinn Healthcare Sa Crystalline forms of fosnetupitant
PT3435980T (pt) 2016-06-06 2020-02-21 Helsinn Healthcare Sa Formulações injetáveis fisiologicamente equilibradas de fosnetupitant
US10975084B2 (en) 2016-10-12 2021-04-13 Merck Sharp & Dohme Corp. KDM5 inhibitors
US10947234B2 (en) 2017-11-08 2021-03-16 Merck Sharp & Dohme Corp. PRMT5 inhibitors
EP3706747B1 (en) 2017-11-08 2025-09-03 Merck Sharp & Dohme LLC Prmt5 inhibitors
US11981701B2 (en) 2018-08-07 2024-05-14 Merck Sharp & Dohme Llc PRMT5 inhibitors
WO2020033282A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
WO2020033288A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2534915B1 (fr) * 1982-10-26 1985-10-25 Lafon Labor Nouveaux derives de 2-(phenoxymethyl)-morpholine, utilisation en therapeutique et procede de preparation
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
IL112778A0 (en) * 1994-03-04 1995-05-26 Merck & Co Inc Substituted heterocycles, their preparation and pharmaceutical compositions containing them

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ATE364606T1 (de) 2007-07-15
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ATE207917T1 (de) 2001-11-15
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US5612337A (en) 1997-03-18
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JPH09507484A (ja) 1997-07-29
EP0737192B1 (en) 2001-10-31
ATE278687T1 (de) 2004-10-15
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SG52217A1 (en) 1998-09-28
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