ATE364606T1 - Substituierte morpholinderivate und ihre verwendung als arzneimittel - Google Patents

Substituierte morpholinderivate und ihre verwendung als arzneimittel

Info

Publication number
ATE364606T1
ATE364606T1 AT04076888T AT04076888T ATE364606T1 AT E364606 T1 ATE364606 T1 AT E364606T1 AT 04076888 T AT04076888 T AT 04076888T AT 04076888 T AT04076888 T AT 04076888T AT E364606 T1 ATE364606 T1 AT E364606T1
Authority
AT
Austria
Prior art keywords
hydrogen
4alkyl
substituted
halogen
optionally substituted
Prior art date
Application number
AT04076888T
Other languages
English (en)
Inventor
Raymond Baker
Timothy Harrison
Angus Macloed
Andrew Pate Owens
Eileen Mary Seward
Christopher John Swain
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 ATE364606T1 publication Critical patent/ATE364606T1/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
AT04076888T 1993-12-29 1994-12-23 Substituierte morpholinderivate und ihre verwendung als arzneimittel ATE364606T1 (de)

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
ATE364606T1 true ATE364606T1 (de) 2007-07-15

Family

ID=27451102

Family Applications (3)

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

Family Applications Before (1)

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

Family Applications After (1)

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

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) ATE278687T1 (de)
BG (1) BG62616B1 (de)
BR (1) BR9408442A (de)
CA (1) CA2178219C (de)
CZ (1) CZ288176B6 (de)
DE (3) DE69434991T2 (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
PT777659E (pt) * 1994-08-15 2001-09-28 Merck Sharp & Dohme Derivados de morfolina e sua utilizacao como agentes terapeuticos
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
EP0912174B1 (de) * 1996-07-17 2004-04-28 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
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
AU732633B2 (en) * 1996-12-02 2001-04-26 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating schizophrenic disorders
ES2227728T3 (es) * 1996-12-02 2005-04-01 MERCK SHARP & DOHME LTD. Uso de antagonistas del receptor de nk-1 para tratar trastornos de ests.
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
EP0941092B1 (de) * 1996-12-02 2004-12-29 MERCK SHARP & DOHME LTD. Verfahren und vorrichtung zur kompensation von durch chrominanzsignalverarbeitung verursachten luminanzstörungen
CA2273809A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating movement disorders
EP0942730A1 (de) * 1996-12-02 1999-09-22 MERCK SHARP & DOHME LTD. Die verwendung von nk-1 rezeptor antagonisten für die behandlung von bipolaren störungen
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
US6100256A (en) * 1996-12-02 2000-08-08 Merck Sharp & Dohme Ltd. Use of NK-1 receptors antagonists for treating schizophrenic disorders
US6613765B1 (en) 1996-12-02 2003-09-02 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating major depressive disorders
AU731349B2 (en) * 1996-12-02 2001-03-29 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating sexual dysfunctions
US5977104A (en) * 1996-12-02 1999-11-02 Merck Sharp & Dohme Ltd. Use of NK-1 receptor antagonists for treating bipolar disorders
JP2001508412A (ja) * 1996-12-02 2001-06-26 メルク シヤープ エンド ドーム リミテツド 認識障害の治療のためのnk−1受容体拮抗薬の使用
JP2001504848A (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 重症不安障害の治療のためのnk−1受容体拮抗薬の使用
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
GB9716463D0 (en) * 1997-08-04 1997-10-08 Merck Sharp & Dohme Therapeutic agents
AU738047B2 (en) * 1997-08-04 2001-09-06 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating mania
AU737019B2 (en) * 1997-08-04 2001-08-09 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating aggressive behaviour disorders
GB9716457D0 (en) * 1997-08-04 1997-10-08 Merck Sharp & Dohme Therapeutic agents
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
US6271230B1 (en) 1997-12-01 2001-08-07 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating cognitive 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
EP1085873A1 (de) * 1998-06-11 2001-03-28 MERCK SHARP & DOHME LTD. Vewrwendung von nk-1 rezeptor antagonisten zur behandlung von psychiatrischen krankheiten
GB9812662D0 (en) * 1998-06-11 1998-08-12 Merck Sharp & Dohme Therapeutic use
AU4279699A (en) * 1998-06-11 1999-12-30 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
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
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
AU1230000A (en) * 1998-10-30 2000-05-22 Merck & Co., Inc. Linear process for the preparation of a morpholine compound
EP1394150B1 (de) 1999-02-24 2011-01-19 F. Hoffmann-La Roche AG 4-Phenylpyridinderivate und deren Verwendung als NK-1 Rezeptorantagonisten
ATE280158T1 (de) 1999-02-24 2004-11-15 Hoffmann La Roche 3-phenylpyridinderivative und deren verwendung als nk-1 rezeptorantagonisten
RU2238264C2 (ru) 1999-02-24 2004-10-20 Ф.Хоффманн-Ля Рош Аг Производные бензола или пиридина и фармацевтическая композиция на их основе
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
CA2388202A1 (en) * 1999-10-29 2001-05-10 Merck & Co., Inc. Polymorphic form of a tachykinin receptor antagonist
EP1103545B1 (de) * 1999-11-29 2003-11-05 F. Hoffmann-La Roche Ag 2-(3,5-Bis-trifluoromethyl-phenyl)-N-methyl-N-(6-morpholin-4-yl-4-o-tolyl-pyridin-3-yl)-isobutyramid
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
SI1303490T1 (sl) 2000-07-14 2008-10-31 Hoffmann La Roche N-oksidi kot predzdravila NK 1 receptorskega antagonista 4-fenil-piridin derivatov
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
MXPA05008171A (es) 2003-01-31 2005-10-05 Hoffmann La Roche Nueva forma cristalina de la 2-(3, 5-bis- trifluormetil -fenil) -n-[6- (1, 1-dioxo -1 lambda 6- tiomorfolin -4-il)- 4-(4-fluor -2-metil -fenil)- piridin-3 -il]-n -metil- isobutiramida.
DE602004008631T2 (de) 2003-07-03 2008-07-10 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.
MX2007000428A (es) 2004-07-15 2008-03-05 Amr Technology Inc Tetrahidroisoquinolinas sustituidas con arilo y heteroarilo y uso de las mismas para bloquear la captacion de norepinefrina, dopamina y serotonina.
NZ555693A (en) 2004-12-27 2010-10-29 Eisai R&D Man Co Ltd Matrix type sustained-release preparation containing donepezil
ATE441633T1 (de) 2005-02-22 2009-09-15 Hoffmann La Roche Nk1-antagonisten
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
CA2615403C (en) 2005-07-15 2015-06-16 Amr Technology, Inc. Aryl-and heteroaryl-substituted tetrahydrobenzazepines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin
KR20080043852A (ko) * 2005-09-23 2008-05-19 에프. 호프만-라 로슈 아게 신규 투여 제형
AU2006297443B2 (en) 2005-09-29 2010-08-12 Merck Sharp & Dohme Corp. Acylated spiropiperidine derivatives as melanocortin-4 receptor modulators
EP2266980A1 (de) * 2005-10-05 2010-12-29 Ranbaxy Laboratories Limited Polymorphe Form von Aprepitant-zwischenprodukt
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
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
CN101641099A (zh) 2007-01-24 2010-02-03 葛兰素集团有限公司 包含3,5-二氨基-6-(2,3-二氯苯基)-1,2,4-三嗪或r(-)-2,4-二氨基-5-(2,3-二氯苯基)-6-氟甲基嘧啶和nk1的药物组合物
US8106086B2 (en) 2007-04-02 2012-01-31 Msd K.K. Indoledione derivative
KR101163847B1 (ko) 2007-04-20 2012-07-09 에프. 호프만-라 로슈 아게 이중 nk1/nk3 수용체 길항제로서의 피롤리딘 유도체
JP5501227B2 (ja) 2007-06-27 2014-05-21 メルク・シャープ・アンド・ドーム・コーポレーション ヒストンデアセチラーゼ阻害剤としての4−カルボキシベンジルアミノ誘導体
KR101167774B1 (ko) 2007-08-07 2012-07-24 에프. 호프만-라 로슈 아게 Nk3 수용체 길항제로서의 피롤리딘 아릴-에터
WO2009104080A2 (en) 2008-02-20 2009-08-27 Targia Pharmaceuticals Cns pharmaceutical compositions and methods of use
AU2009222122A1 (en) 2008-03-03 2009-09-11 Tiger Pharmatech Tyrosine 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
EP2413932A4 (de) 2009-04-01 2012-09-19 Merck Sharp & Dohme Hemmer der akt-aktivität
KR20120034644A (ko) 2009-05-12 2012-04-12 알바니 몰레큘라 리써치, 인크. 아릴, 헤테로아릴, 및 헤테로사이클 치환된 테트라하이드로이소퀴놀린 및 이의 용도
EP2429293B1 (de) 2009-05-12 2014-10-29 Bristol-Myers Squibb Company KRISTALLINE FORMEN VON (S)-7-([1,2,4]TRIAZOL[1,5-a]PYRIDIN-6-YL)-4-(3,4-DICHLORPHENYL)-1,2,3,4-TETRAHYDROISOCHINOLIN UND IHRE VERWENDUNG
ES2662072T3 (es) 2009-05-12 2018-04-05 Albany Molecular Research, Inc. 7-([1,2,4]triazolo[1,5-a]piridin-6-il)-4-(3,4-diclorofenil)-1,2,3,4-tetrahidroisoquinolina y uso de la misma
KR101485645B1 (ko) 2009-10-14 2015-01-22 머크 샤프 앤드 돔 코포레이션 p53 활성을 증가시키는 치환된 피페리딘 및 그의 용도
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
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
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.
HUE044815T2 (hu) 2010-08-17 2019-11-28 Sirna Therapeutics Inc Hepatitisz B vírus (HBV) génexpressziójának RNS-interferencia közvetített gátlása, rövid interferáló nukleinsav (SINS) alkalmazásával
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)
US9351965B2 (en) 2010-12-21 2016-05-31 Merck Sharp & Dohme Corp. Indazole derivatives useful as ERK inhibitors
CN103732592A (zh) 2011-04-21 2014-04-16 默沙东公司 ***-1受体抑制剂
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
EP3919620A1 (de) 2012-05-02 2021-12-08 Sirna Therapeutics, Inc. Zusammensetzungen mit kurzer interferierender nukleinsäure (sina)
CA2882950A1 (en) 2012-09-28 2014-04-03 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
LT2925888T (lt) 2012-11-28 2018-01-10 Merck Sharp & Dohme Corp. Vėžio gydymo kompozicijos ir būdai
BR112015013611A2 (pt) 2012-12-20 2017-11-14 Merck Sharp & Dohme composto, e, composição farmacêutica
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
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
EA036605B1 (ru) 2016-06-06 2020-11-27 Хелсинн Хелскеа Са Физиологически сбалансированный состав для инъекций, включающий фоснетупитант
US10947234B2 (en) 2017-11-08 2021-03-16 Merck Sharp & Dohme Corp. PRMT5 inhibitors
US20210277009A1 (en) 2018-08-07 2021-09-09 Merck Sharp & Dohme Corp. Prmt5 inhibitors
US20210309688A1 (en) 2018-08-07 2021-10-07 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
WO1993004040A1 (en) * 1991-08-20 1993-03-04 Merck Sharp & Dohme Limited 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
TW385308B (en) * 1994-03-04 2000-03-21 Merck & Co Inc Prodrugs of morpholine tachykinin receptor antagonists

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HU221139B1 (en) 2002-08-28
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NO962749D0 (no) 1996-06-28
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IL112134A (en) 1999-12-22
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