SG52217A1 - Substituted morpholine derivatives and their use as therapeutic agents - Google Patents

Substituted morpholine derivatives and their use as therapeutic agents

Info

Publication number
SG52217A1
SG52217A1 SG1996000578A SG1996000578A SG52217A1 SG 52217 A1 SG52217 A1 SG 52217A1 SG 1996000578 A SG1996000578 A SG 1996000578A SG 1996000578 A SG1996000578 A SG 1996000578A SG 52217 A1 SG52217 A1 SG 52217A1
Authority
SG
Singapore
Prior art keywords
hydrogen
4alkyl
substituted
halogen
optionally substituted
Prior art date
Application number
SG1996000578A
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
Publication of SG52217A1 publication Critical patent/SG52217A1/en

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 System
    • 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 System
    • 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
SG1996000578A 1993-12-29 1994-12-23 Substituted morpholine derivatives and their use as therapeutic agents SG52217A1 (en)

Applications Claiming Priority (4)

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

Publications (1)

Publication Number Publication Date
SG52217A1 true SG52217A1 (en) 1998-09-28

Family

ID=27451102

Family Applications (1)

Application Number Title Priority Date Filing Date
SG1996000578A SG52217A1 (en) 1993-12-29 1994-12-23 Substituted morpholine derivatives and their use as therapeutic agents

Country Status (24)

Country Link
US (1) US5612337A (de)
EP (3) EP1462450B1 (de)
JP (2) JP3071467B2 (de)
KR (1) KR100286412B1 (de)
CN (1) CN1067683C (de)
AT (3) ATE207917T1 (de)
BG (1) BG62616B1 (de)
BR (1) BR9408442A (de)
CA (1) CA2178219C (de)
CZ (1) CZ288176B6 (de)
DE (3) DE69434063D1 (de)
DK (1) DK0737192T3 (de)
ES (1) ES2164758T3 (de)
HU (1) HU221139B1 (de)
IL (1) IL112134A (de)
LV (1) LV11687B (de)
NO (1) NO307090B1 (de)
NZ (1) NZ277839A (de)
PL (1) PL181214B1 (de)
RU (1) RU2131426C1 (de)
SG (1) SG52217A1 (de)
SK (1) SK283070B6 (de)
TW (1) TW449588B (de)
WO (1) WO1995018124A1 (de)

Families Citing this family (123)

* 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
JPH10500944A (ja) * 1994-05-05 1998-01-27 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タキキニンのアンタゴニストとしてのそれらの使用
DK0777659T3 (da) * 1994-08-15 2001-09-03 Merck Sharp & Dohme Morpholinderivater og deres anvendelse som terapeutiske midler
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
AU3716997A (en) 1996-07-17 1998-02-09 Merck & Co., Inc. Alteration of circadian rhythmicity with a tachykinin antagonist
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
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
DE69731657T2 (de) * 1996-12-02 2005-12-01 Merck Sharp & Dohme Ltd., Hoddesdon Die verwendung von nk-1 rezeptor antagonisten für die behandlung von substanz-verwendung störungen
JP2001505881A (ja) * 1996-12-02 2001-05-08 メルク シヤープ エンド ドーム リミテツド 精神分裂症疾患を治療するためのｎｋ−１受容体拮抗薬の使用
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
DK0942729T3 (da) * 1996-12-02 2005-01-10 Merck Sharp & Dohme Anvendelse af NK-1-receptorantagonister til behandling af stresslidelser
ES2234039T3 (es) * 1996-12-02 2005-06-16 MERCK SHARP & DOHME LTD. Uso de antagonistas del receptor nk-1 para tratar trastornos de depresion mayor.
AU729708B2 (en) * 1996-12-02 2001-02-08 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating severe anxiety disorders
DE69733148T2 (de) * 1996-12-02 2006-02-02 Merck Sharp & Dohme Ltd., Hoddesdon Die verwendung von nk-1 rezeptorantagonisten für die behandlung von kognitiven störungen
US6613765B1 (en) 1996-12-02 2003-09-02 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating major depressive 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
JP2001504852A (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 双極性障害の治療のためのｎｋ−１受容体拮抗薬の使用
ATE282417T1 (de) * 1996-12-02 2004-12-15 Merck Sharp & Dohme Die verwendung von nk-1 rezeptor antagonisten für die behandlung von bewegungsstörungen
US5977104A (en) * 1996-12-02 1999-11-02 Merck Sharp & Dohme Ltd. Use of NK-1 receptor antagonists for treating bipolar disorders
GB9700555D0 (en) * 1997-01-13 1997-03-05 Merck Sharp & Dohme Therapeutic agents
AU744261B2 (en) * 1997-04-24 2002-02-21 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating eating disorders
CA2298777A1 (en) * 1997-08-04 1999-02-18 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating mania
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
CA2298779A1 (en) * 1997-08-04 1999-02-18 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating aggressive behaviour disorders
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
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
WO1999064006A1 (en) * 1998-06-11 1999-12-16 Merck Sharp & Dohme Limited Use of a nk-1 receptor antagonist for treating psychiatric disorders
WO1999064010A1 (en) * 1998-06-11 1999-12-16 Merck Sharp & Dohme Limited Use of a nk-1 receptor antagonist for treating psychiatric disorders
GB9812617D0 (en) * 1998-06-11 1998-08-12 Merck Sharp & Dohme Therapeutic use
GB9812662D0 (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
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
WO2000026214A1 (en) * 1998-10-30 2000-05-11 Merck & Co., Inc. Linear process for the preparation of a morpholine compound
EP1124826A1 (de) * 1998-10-30 2001-08-22 Merck & Co., Inc. Verfahren zur herstellung von 2-(r)-(1-(r)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-4-((5-(dimethylaminomethyl)-1,2,3-triazol-4-yl)methyl)-3-(s)-(4-fluorophenyl)morpholin
DK1394150T3 (da) * 1999-02-24 2011-03-21 Hoffmann La Roche 4-phenylpyridinderivater og deres anvendelse som NK-1-receptorantagonister
WO2000050398A2 (en) 1999-02-24 2000-08-31 F. Hoffmann-La Roche Ag Phenyl- and pyridinyl derivatives as neurokinin 1 antagonists
JP4068305B2 (ja) 1999-02-24 2008-03-26 エフ．ホフマン−ラ ロシュ アーゲー ３−フェニルピリジン誘導体、およびそのｎｋ−１受容体拮抗薬としての用途
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 (de) * 1999-10-29 2002-08-07 Merck & Co., Inc. Polymorphe form eines tachykininrezeptorantagonisten
DK1103545T3 (da) * 1999-11-29 2004-03-15 Hoffmann La Roche 2-(3,5-bis-trifluormethyl-phenyl)-N-methyl-N-(6-morpholin-4-yl-4-o-tolyl-pyridin-3-yl)-isobutyramide
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
US6482829B2 (en) 2000-06-08 2002-11-19 Hoffmann-La Roche Inc. Substituted heterocyclic siprodecane compound active as an antagonist of neurokinin 1 receptor
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
WO2001096319A1 (en) * 2000-06-09 2001-12-20 Merck & 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
KR100501608B1 (ko) 2000-07-14 2005-07-18 에프. 호프만-라 로슈 아게 4-페닐-피리딘 유도체의 ｎｋ1 수용체의 길항성선구약물로서의 ｎ-산화물
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
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
CN100562320C (zh) 2003-01-31 2009-11-25 弗·哈夫曼-拉罗切有限公司 2-(3,5-二-三氟甲基-苯基)-N-[6-(1,1-二氧代-1λ6-硫代吗啉-4-基)-4-(4-氟-2-甲基-苯基)-吡啶-3-基]-N-甲基-异丁酰胺的新晶体变体
EP1643998B1 (de) 2003-07-03 2007-08-29 F. Hoffmann-La Roche Ag Duale nk1/nk3 antagonisten zur behandlung von schizophrenie
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.
ZA200701232B (en) 2004-07-15 2008-08-27 Amr Technology Inc Aryl-and heteroaryl-substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine and serotonin
CA2592605C (en) 2004-12-27 2010-12-07 Eisai R&D Management Co., Ltd. Method for stabilizing anti-dementia drug
JP4767973B2 (ja) 2005-02-22 2011-09-07 エフ．ホフマン−ラ ロシュ アーゲー Ｎｋ１アンタゴニスト
DK1863767T3 (da) 2005-03-23 2009-05-04 Hoffmann La Roche Metabolitter til NK-I-antagonister til emesis
ATE550019T1 (de) 2005-05-17 2012-04-15 Merck Sharp & Dohme Cis-4-ä(4-chlorophenyl)sulfonylü-4-(2,5- difluorophenyl)cyclohexanepropansäure zur behandlug von krebs
US7956050B2 (en) 2005-07-15 2011-06-07 Albany Molecular Research, Inc. Aryl- and heteroaryl-substituted tetrahydrobenzazepines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin
DK1928427T3 (da) 2005-09-23 2010-03-08 Hoffmann La Roche Hidtil ukendt dosisformulering
EP1940842B1 (de) 2005-09-29 2012-05-30 Merck Sharp & Dohme Corp. Acylierte spiropiperidinderivate als modulatoren des melanocortin-4-rezeptors
US8080656B2 (en) 2005-10-05 2011-12-20 Ranbaxy Laboratories Limited Process for the preparation of aprepitant
GB0603041D0 (en) 2006-02-15 2006-03-29 Angeletti P Ist Richerche Bio Therapeutic compounds
EP2698157B1 (de) 2006-09-22 2015-05-20 Merck Sharp & Dohme Corp. Verfahren zur Behandlung von Fettsäure-Synthese-Hemmern
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
EP2109608B1 (de) 2007-01-10 2011-03-23 Istituto di Richerche di Biologia Molecolare P. Angeletti S.p.A. Amidsubstituierte indazole als poly-(adp-ribose)-polymerase (parp)-hemmer
EP2129381A1 (de) 2007-01-24 2009-12-09 Glaxo Group Limited Pharmazeutische zubereitungen enthaltend 3,5-diamino-6-(2,3-dichlophenyl)-1,2,4-triazin or r(-)-2,4-diamino-5-(2,3dichlorophenyl)-6-fluoromethyl pyrimidin und einen nk1- rezeptor-antagonisten
AU2008233662B2 (en) 2007-04-02 2012-08-23 Msd K.K. Indoledione derivative
DE602008001983D1 (de) 2007-04-20 2010-09-09 Hoffmann La Roche Pyrrolidinderivate als doppelte nk1/nk3-rezeptorenantagonisten
US8389553B2 (en) 2007-06-27 2013-03-05 Merck Sharp & Dohme Corp. 4-carboxybenzylamino derivatives as histone deacetylase inhibitors
MX2010001080A (es) 2007-08-07 2010-03-01 Hoffmann La Roche Pirrolidin-aril-eteres como antagonistas de receptor de nk3.
CA2716080C (en) 2008-02-20 2016-12-13 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
EP2413932A4 (de) 2009-04-01 2012-09-19 Merck Sharp & Dohme Hemmer der akt-aktivität
CA2760837C (en) 2009-05-12 2018-04-03 Albany Molecular Research, Inc. 7-([1,2,4]triazolo[1,5-.alpha.]pyridin-6-yl)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydroisoquinoline and use thereof
WO2010132437A1 (en) 2009-05-12 2010-11-18 Albany Molecular Research, Inc. Aryl, heteroaryl, and heterocycle substituted tetrahydroisoquinolines and use thereof
JP5739415B2 (ja) 2009-05-12 2015-06-24 ブリストル−マイヤーズ スクウィブ カンパニー （Ｓ）−７−（［１，２，４］トリアゾロ［１，５−ａ］ピリジン−６−イル）−４−（３，４−ジクロロフェニル）−１，２，３，４−テトラヒドロイソキノリンの結晶形態およびその使用
EP2488028B1 (de) 2009-10-14 2020-08-19 Merck Sharp & Dohme Corp. Substituierte piperidine zur erhöhung der p53-aktivität und ihre verwendung
US8487102B2 (en) 2010-04-20 2013-07-16 Hoffmann-La Roche Inc. Pyrrazolopyridine compounds as dual NK1/NK3 receptor antagonists
WO2011163330A1 (en) 2010-06-24 2011-12-29 Merck Sharp & Dohme Corp. Novel heterocyclic compounds as erk inhibitors
CN103068980B (zh) 2010-08-02 2017-04-05 瑟纳治疗公司 使用短干扰核酸（siNA）的RNA干扰介导的联蛋白（钙粘蛋白关联蛋白质），β1（CTNNB1）基因表达的抑制
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.
KR102072631B1 (ko) 2010-08-17 2020-02-03 시르나 쎄러퓨틱스 인코퍼레이티드 짧은 간섭 핵산 （ｓｉＮＡ）을 사용한 Ｂ형 간염 바이러스 （ＨＢＶ） 유전자 발현의 ＲＮＡ 간섭 매개 억제
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
EP3766975A1 (de) 2010-10-29 2021-01-20 Sirna Therapeutics, Inc. Rna-interferenz-vermittelte inhibition von genexpression unter verwendung kurzer interferierender nukleinsäure (sina)
WO2012087772A1 (en) 2010-12-21 2012-06-28 Schering Corporation Indazole derivatives useful as erk inhibitors
US20140046059A1 (en) 2011-04-21 2014-02-13 Piramal Enterprises Limited Process for the preparation of morpholino sulfonyl indole derivatives
US9023865B2 (en) 2011-10-27 2015-05-05 Merck Sharp & Dohme Corp. Compounds that are ERK inhibitors
EP2837381A4 (de) 2011-12-13 2015-12-09 Servicio Andaluz De Salud Verwendung von mitteln zur behandlung von krebs, die die peritumoralumgebung verändern
US20150299696A1 (en) 2012-05-02 2015-10-22 Sirna Therapeutics, Inc. SHORT INTERFERING NUCLEIC ACID (siNA) COMPOSITIONS
WO2014052563A2 (en) 2012-09-28 2014-04-03 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
ES2651347T3 (es) 2012-11-28 2018-01-25 Merck Sharp & Dohme Corp. Composiciones y métodos para el tratamiento del cáncer
CA2895504A1 (en) 2012-12-20 2014-06-26 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
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
WO2015034925A1 (en) 2013-09-03 2015-03-12 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
US20160324881A1 (en) * 2013-12-30 2016-11-10 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
EP3435980B1 (de) 2016-06-06 2019-11-13 Helsinn Healthcare SA Physiologisch ausgewogene injizierbare formulierungen von fosnetupitant
US10947234B2 (en) 2017-11-08 2021-03-16 Merck Sharp & Dohme Corp. PRMT5 inhibitors
WO2020033284A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
WO2020033282A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0600952B1 (de) * 1991-08-20 1996-04-17 MERCK SHARP & DOHME LTD. Azacyclische verbindungen, verfahren zu ihrer herstellung und diese enthaltende pharmazeutische zubereitungen
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
TW385308B (en) * 1994-03-04 2000-03-21 Merck & Co Inc Prodrugs of morpholine tachykinin receptor antagonists

Also Published As

Publication number Publication date
PL315182A1 (en) 1996-10-14
EP1099702B1 (de) 2004-10-06
JPH09507484A (ja) 1997-07-29
CZ288176B6 (en) 2001-05-16
CN1067683C (zh) 2001-06-27
HUT75872A (en) 1997-05-28
EP1099702A1 (de) 2001-05-16
ATE207917T1 (de) 2001-11-15
JP3071467B2 (ja) 2000-07-31
AU1322395A (en) 1995-07-17
ATE364606T1 (de) 2007-07-15
BG100644A (bg) 1997-03-31
AU685209B2 (en) 1998-01-15
EP0737192B1 (de) 2001-10-31
HU221139B1 (en) 2002-08-28
EP1462450B1 (de) 2007-06-13
CA2178219C (en) 2005-03-22
CZ189896A3 (en) 1996-12-11
TW449588B (en) 2001-08-11
CA2178219A1 (en) 1995-07-06
ES2164758T3 (es) 2002-03-01
PL181214B1 (pl) 2001-06-29
DE69434991D1 (de) 2007-07-26
HU9601801D0 (en) 1996-09-30
DK0737192T3 (da) 2001-11-26
NO962749L (no) 1996-08-28
RU2131426C1 (ru) 1999-06-10
LV11687A (lv) 1997-02-20
NO307090B1 (no) 2000-02-07
IL112134A0 (en) 1995-03-15
US5612337A (en) 1997-03-18
EP1462450A1 (de) 2004-09-29
ATE278687T1 (de) 2004-10-15
NO962749D0 (no) 1996-06-28
IL112134A (en) 1999-12-22
DE69434991T2 (de) 2008-03-06
DE69434063D1 (de) 2004-11-11
BG62616B1 (bg) 2000-03-31
CN1139927A (zh) 1997-01-08
WO1995018124A1 (en) 1995-07-06
KR100286412B1 (ko) 2001-04-16
SK283070B6 (sk) 2003-02-04
EP0737192A1 (de) 1996-10-16
LV11687B (en) 1997-10-20
NZ277839A (en) 1998-01-26
SK83996A3 (en) 1996-11-06
DE69428913D1 (de) 2001-12-06
DE69428913T2 (de) 2002-05-29
BR9408442A (pt) 1997-08-05
JP2000219629A (ja) 2000-08-08

Similar Documents

Publication Publication Date Title
SG52217A1 (en) Substituted morpholine derivatives and their use as therapeutic agents
AU4257889A (en) Sulphonamido-phenylalkanoic acid derivatives having thromboxane A2 antagonist activity
HU9600834D0 (en) Quinazoline derivatives
MY129540A (en) Quinazoline derivatives, pharmaceutical compositions containing them processes for their preparation and their use in the production of an antiangiogenic and/or vascular permeability reducing effect
DE68914793T2 (de) Chinazolinon-Derivate.
DK0625516T3 (da) Benzensulfonamidderivater til behandling af blæreustabilitet
ATE161531T1 (de) Acridine-1,8-dionderivate als therapeutisches mittel
FR2458556B1 (de)
HU9400908D0 (en) Pharmaceutical compositions for treatng skin disorders
DK0566288T3 (da) Flavon-derivater
ES2168119T3 (es) Derivados de quinoxalina para el tratamiento de tinnitus.
MX9205408A (es) Metodo para tratar hipertension.
MY105852A (en) New 2-methoxycarbonyl substituted n, n'' -di- (trimethoxybenzoyl) piperazines, process for preparing the same and therapeutical compounds containing them.