ATE207917T1 - Substituierte morpholinderivate und ihre verwendung als arzneimittel - Google Patents

Substituierte morpholinderivate und ihre verwendung als arzneimittel

Info

Publication number
ATE207917T1
ATE207917T1 AT95904621T AT95904621T ATE207917T1 AT E207917 T1 ATE207917 T1 AT E207917T1 AT 95904621 T AT95904621 T AT 95904621T AT 95904621 T AT95904621 T AT 95904621T AT E207917 T1 ATE207917 T1 AT E207917T1
Authority
AT
Austria
Prior art keywords
hydrogen
4alkyl
substituted
halogen
optionally substituted
Prior art date
Application number
AT95904621T
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 ATE207917T1 publication Critical patent/ATE207917T1/de

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/06Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6527Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07F9/6533Six-membered rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558Heterocyclic 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
    • C07F9/65583Heterocyclic 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
AT95904621T 1993-12-29 1994-12-23 Substituierte morpholinderivate und ihre verwendung als arzneimittel ATE207917T1 (de)

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
ATE207917T1 true ATE207917T1 (de) 2001-11-15

Family

ID=27451102

Family Applications (3)

Application Number Title Priority Date Filing Date
AT04076888T ATE364606T1 (de) 1993-12-29 1994-12-23 Substituierte morpholinderivate und ihre verwendung als arzneimittel
AT01200308T ATE278687T1 (de) 1993-12-29 1994-12-23 Substituierte morpholinderivate und ihre verwendung als therapeutische mittel
AT95904621T ATE207917T1 (de) 1993-12-29 1994-12-23 Substituierte morpholinderivate und ihre verwendung als arzneimittel

Family Applications Before (2)

Application Number Title Priority Date Filing Date
AT04076888T ATE364606T1 (de) 1993-12-29 1994-12-23 Substituierte morpholinderivate und ihre verwendung als arzneimittel
AT01200308T ATE278687T1 (de) 1993-12-29 1994-12-23 Substituierte morpholinderivate und ihre verwendung als therapeutische mittel

Country Status (24)

Country Link
US (1) US5612337A (de)
EP (3) EP1099702B1 (de)
JP (2) JP3071467B2 (de)
KR (1) KR100286412B1 (de)
CN (1) CN1067683C (de)
AT (3) ATE364606T1 (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
EP0758329A1 (de) * 1994-05-05 1997-02-19 MERCK SHARP & DOHME LTD. Morpholin-derivate und deren verwendung als antagonisten von tachykininen
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
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
AU733855B2 (en) * 1996-12-02 2001-05-31 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating major depressive disorders
US6613765B1 (en) 1996-12-02 2003-09-02 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating major depressive disorders
US6100256A (en) * 1996-12-02 2000-08-08 Merck Sharp & Dohme Ltd. Use of NK-1 receptors antagonists for treating schizophrenic disorders
CA2273856A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating bipolar disorders
EP0942729B1 (de) * 1996-12-02 2004-09-01 MERCK SHARP & DOHME LTD. Die verwendung von nk-1 rezeptor antagonisten für die behandlungen von stress störungen
JP2001507678A (ja) * 1996-12-02 2001-06-12 メルク シヤープ エンド ドーム リミテツド 運動障害の治療のためのnk−1受容体拮抗薬の使用
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
CA2273853A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating cognitive disorders
WO1998024439A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited 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
JP2001504853A (ja) * 1996-12-02 2001-04-10 メルク シヤープ エンド ドーム リミテツド 物質使用障害の治療のためのnk−1受容体拮抗薬の使用
EP0941093B1 (de) * 1996-12-02 2005-02-09 MERCK SHARP & DOHME LTD. Verwendung von nk-1 rezeptorantagonisten zur behandlung von schweren depressionen, die von angstzuständen begleitet werden
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
GB9700555D0 (en) * 1997-01-13 1997-03-05 Merck Sharp & Dohme Therapeutic agents
EP0977572A1 (de) * 1997-04-24 2000-02-09 Merck Sharp & Dohme Ltd. Verwendung von nk-1 rezeptor-antagonisten zur behandlung von essstörungen
AU738047B2 (en) * 1997-08-04 2001-09-06 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
WO1999007375A1 (en) * 1997-08-04 1999-02-18 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
US5972938A (en) 1997-12-01 1999-10-26 Merck & Co., Inc. Method for treating or preventing psychoimmunological 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
US6156749A (en) * 1997-12-01 2000-12-05 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating movement 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
CA2334609A1 (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
GB9812664D0 (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
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
AU1230000A (en) * 1998-10-30 2000-05-22 Merck & Co., Inc. Linear process for the preparation of a morpholine compound
CZ20013047A3 (cs) 1999-02-24 2002-02-13 F. Hoffmann-La Roche Ag 3-Fenylpyridinové deriváty a jejich pouľití jako antagonisty NK-1 receptorů
JP4070957B2 (ja) 1999-02-24 2008-04-02 エフ.ホフマン−ラ ロシュ アーゲー フェニルおよびピリジニル誘導体
ES2226622T3 (es) 1999-02-24 2005-04-01 F. Hoffmann-La Roche Ag Derivados de 4-fenil piridina y su empleo como antagonistas del receptor nk-1.
US6291465B1 (en) 1999-03-09 2001-09-18 Hoffmann-La Roche Inc. Biphenyl derivatives
US6274588B1 (en) 1999-05-31 2001-08-14 Hoffmann-La Roche Inc. 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
TR200302077T4 (tr) * 1999-11-29 2004-01-21 F. Hoffmann-La Roche Ag 2-(3,5-Bis-Trifluorometil-fenil)-N-metil-N- (6-morfonil-4-il-4-O-tolil-piridin-3-il)- izobütiramit
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
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
CZ303639B6 (cs) 2000-07-14 2013-01-23 F. Hoffmann-La Roche Ag N-Oxid derivátu 4-fenylpyridinu, zpusob jeho prípravy a lécivo s jeho obsahem
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
JP5026702B2 (ja) 2003-01-31 2012-09-19 エフ.ホフマン−ラ ロシュ アーゲー 2−(3,5−ビス−トリフルオロメチル−フェニル)−N−[6−(1,1−ジオキソ−1λ6−チオモルホリン−4−イル)−4−(4−フルオロ−2−メチル−フェニル)−ピリジン−3−イル]−N−メチル−イソブチルアミドの新規な結晶変形
PT1643998E (pt) 2003-07-03 2007-11-21 Hoffmann La Roche Antagonistas duplos dos receptores de nc1/nc3 para tratar a esquizofrenia
US7288658B2 (en) 2003-07-15 2007-10-30 Hoffmann-La Roche Inc. 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
NZ555693A (en) 2004-12-27 2010-10-29 Eisai R&D Man Co Ltd Matrix type sustained-release preparation containing donepezil
US7176205B2 (en) 2005-02-22 2007-02-13 Hoffmann-La Roche Inc. Bi-pyridinyl derivatives as NK-1 antagonists
CA2602445C (en) 2005-03-23 2013-08-20 F.Hoffmann-La Roche Ag Metabolites for nk-i antagonists for emesis
ES2382814T3 (es) 2005-05-17 2012-06-13 Merck Sharp & Dohme Ltd. Ácido cis-4-[(4-clorofenil)sulfonil]-4-(2,5-difluorofenil)ciclohexanopropanoico para el tratamiento del cáncer
EP1904069B1 (de) 2005-07-15 2018-06-13 Albany Molecular Research, Inc. Aryl- und heteroarylsubstituierte tetrahydrobenzazepine und verwendung damit zur wiederaufnahmeblockierung von norepinephrin, dopamin und serotonin
MY143784A (en) * 2005-09-23 2011-07-15 Hoffmann La Roche Novel dosage formulation
US8293900B2 (en) 2005-09-29 2012-10-23 Merck Sharp & Dohme Corp Acylated spiropiperidine derivatives as melanocortin-4 receptor modulators
WO2007039883A2 (en) * 2005-10-05 2007-04-12 Ranbaxy Laboratories Limited Process for preparation of aprepitant
GB0603041D0 (en) 2006-02-15 2006-03-29 Angeletti P Ist Richerche Bio Therapeutic compounds
CA2664113C (en) 2006-09-22 2013-05-28 Merck & Co., Inc. Use of platencin and platensimycin as fatty acid synthesis inhibitors to treat obesity, diabetes and cancer
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
BRPI0806245B1 (pt) 2007-01-10 2022-01-25 Msd Italia S.R.L. Compostos de fórmula i e seus usos
KR20090112722A (ko) 2007-01-24 2009-10-28 글락소 그룹 리미티드 3,5-디아미노-6-(2,3-디클로로페닐)-1,2,4-트리아진 또는 r(-)-2,4-디아미노-5-(2,3-디클로로페닐)-6-플루오로메틸 피리미딘 및 nk1을 포함하는 제약 조성물
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.
EP2170076B1 (de) 2007-06-27 2016-05-18 Merck Sharp & Dohme Corp. 4-carboxybenzylamino-derivate als histondeacetylase-hemmer
JP2010535733A (ja) 2007-08-07 2010-11-25 エフ.ホフマン−ラ ロシュ アーゲー Nk3受容体アンタゴニストとしてのピロリジンアリールエーテル
WO2009104080A2 (en) 2008-02-20 2009-08-27 Targia Pharmaceuticals Cns pharmaceutical compositions and methods of use
US8598184B2 (en) 2008-03-03 2013-12-03 Tiger Pharmatech Protein kinase inhibitors
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
KR20120034644A (ko) 2009-05-12 2012-04-12 알바니 몰레큘라 리써치, 인크. 아릴, 헤테로아릴, 및 헤테로사이클 치환된 테트라하이드로이소퀴놀린 및 이의 용도
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
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
WO2011046771A1 (en) 2009-10-14 2011-04-21 Schering Corporation 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
WO2011163330A1 (en) 2010-06-24 2011-12-29 Merck Sharp & Dohme Corp. Novel 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
US8946216B2 (en) 2010-09-01 2015-02-03 Merck Sharp & Dohme Corp. Indazole derivatives useful as ERK inhibitors
EP2615916B1 (de) 2010-09-16 2017-01-04 Merck Sharp & Dohme Corp. Kondensierte pyrazolderivate als neue erk-hemmer
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)
WO2012087772A1 (en) 2010-12-21 2012-06-28 Schering Corporation Indazole derivatives useful as erk inhibitors
JP2014514321A (ja) 2011-04-21 2014-06-19 メルク・シャープ・アンド・ドーム・コーポレーション インスリン様増殖因子1受容体阻害剤
US9023865B2 (en) 2011-10-27 2015-05-05 Merck Sharp & Dohme Corp. Compounds that are ERK inhibitors
US20150297613A1 (en) 2011-12-13 2015-10-22 Servicio Andaluz De Salud Use of agents that alter the peritumoral environment for the treatment of cancer
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
MX363243B (es) 2012-11-28 2019-03-14 Merck Sharp & Dohme Composiciones para tratar cáncer y usos de dichas composiciones.
RU2690663C2 (ru) 2012-12-20 2019-06-05 Мерк Шарп И Доум Корп. Замещенные имидазопиридины в качестве ингибиторов hdm2
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
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
EP3091977A2 (de) * 2013-12-30 2016-11-16 Oncoprevent GmbH Neurokinin-1-rezeptorantagonisten zur verwendung in einem verfahren zur prävention von krebs
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
CA3025837C (en) 2016-06-06 2024-02-13 Helsinn Healthcare Sa Physiologically balanced injectable formulations of 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
EP3833668A4 (de) 2018-08-07 2022-05-11 Merck Sharp & Dohme Corp. Prmt5-inhibitoren

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
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
IL112778A0 (en) * 1994-03-04 1995-05-26 Merck & Co Inc Substituted heterocycles, their preparation and pharmaceutical compositions containing them

Also Published As

Publication number Publication date
SK283070B6 (sk) 2003-02-04
DE69434991T2 (de) 2008-03-06
DE69434063D1 (de) 2004-11-11
BG100644A (bg) 1997-03-31
NO307090B1 (no) 2000-02-07
EP1099702A1 (de) 2001-05-16
EP0737192A1 (de) 1996-10-16
PL181214B1 (pl) 2001-06-29
CZ189896A3 (en) 1996-12-11
NZ277839A (en) 1998-01-26
AU1322395A (en) 1995-07-17
JPH09507484A (ja) 1997-07-29
RU2131426C1 (ru) 1999-06-10
NO962749D0 (no) 1996-06-28
SG52217A1 (en) 1998-09-28
DK0737192T3 (da) 2001-11-26
LV11687B (en) 1997-10-20
SK83996A3 (en) 1996-11-06
DE69434991D1 (de) 2007-07-26
PL315182A1 (en) 1996-10-14
CA2178219A1 (en) 1995-07-06
HU9601801D0 (en) 1996-09-30
IL112134A0 (en) 1995-03-15
DE69428913D1 (de) 2001-12-06
EP1462450B1 (de) 2007-06-13
LV11687A (lv) 1997-02-20
ATE278687T1 (de) 2004-10-15
EP1099702B1 (de) 2004-10-06
KR100286412B1 (ko) 2001-04-16
CZ288176B6 (en) 2001-05-16
TW449588B (en) 2001-08-11
HUT75872A (en) 1997-05-28
ATE364606T1 (de) 2007-07-15
HU221139B1 (en) 2002-08-28
BG62616B1 (bg) 2000-03-31
US5612337A (en) 1997-03-18
IL112134A (en) 1999-12-22
CA2178219C (en) 2005-03-22
DE69428913T2 (de) 2002-05-29
WO1995018124A1 (en) 1995-07-06
BR9408442A (pt) 1997-08-05
EP1462450A1 (de) 2004-09-29
CN1067683C (zh) 2001-06-27
ES2164758T3 (es) 2002-03-01
AU685209B2 (en) 1998-01-15
NO962749L (no) 1996-08-28
CN1139927A (zh) 1997-01-08
EP0737192B1 (de) 2001-10-31
JP3071467B2 (ja) 2000-07-31
JP2000219629A (ja) 2000-08-08

Similar Documents

Publication Publication Date Title
DE69428913T2 (de) Substituierte morpholinderivate und ihre verwendung als arzneimittel
HU9600834D0 (en) Quinazoline derivatives
HK1048989A1 (en) Heterocyclic derivatives and pharmaceutical use thereof.
DE69428142D1 (de) Quinolin- oder Quinazolinderivate, deren Herstellung und Verwendung
DK0625516T3 (da) Benzensulfonamidderivater til behandling af blæreustabilitet
DK0593766T3 (da) Pyridoncarboxylsyrederivat
DE69629838D1 (de) Inhibitoren der kainsäure-neurotoxizität sowie pyridothiazinderivate
DE69600231T2 (de) N-Arylalkylphenylacetamidderivate
DE69300318D1 (de) Flavonderivate.
DK0784973T3 (da) Quinoxalinderivater til behandling af tinnitus
EP0601181A4 (en) Benzofuran derivative and pharmaceutical composition.

Legal Events

Date Code Title Description
RER Ceased as to paragraph 5 lit. 3 law introducing patent treaties