ES2147840T3 - Antagonistas de receptores de taquiquininas con morfolina. - Google Patents

Antagonistas de receptores de taquiquininas con morfolina.

Info

Publication number
ES2147840T3
ES2147840T3 ES95905965T ES95905965T ES2147840T3 ES 2147840 T3 ES2147840 T3 ES 2147840T3 ES 95905965 T ES95905965 T ES 95905965T ES 95905965 T ES95905965 T ES 95905965T ES 2147840 T3 ES2147840 T3 ES 2147840T3
Authority
ES
Spain
Prior art keywords
sub
instituted
replaced
group
antagonists
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Lifetime
Application number
ES95905965T
Other languages
English (en)
Spanish (es)
Inventor
Conrad P Dorn
Paul E Finke
Jeffrey J Hale
Malcolm Maccoss
Sander G Mills
Shrenik K Shah
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck and Co Inc
Original Assignee
Merck and Co Inc
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=22617632&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ES2147840(T3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck and Co Inc filed Critical Merck and Co Inc
Application granted granted Critical
Publication of ES2147840T3 publication Critical patent/ES2147840T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D265/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/281,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/301,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • 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
    • 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
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • 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
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/08Vasodilators for multiple indications
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D265/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/281,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/301,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • C07D265/321,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings with oxygen atoms directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D279/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/101,4-Thiazines; Hydrogenated 1,4-thiazines
    • C07D279/121,4-Thiazines; Hydrogenated 1,4-thiazines not condensed with other rings
    • 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
    • C07D413/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Immunology (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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Peptides Or Proteins (AREA)
ES95905965T 1993-12-17 1994-12-13 Antagonistas de receptores de taquiquininas con morfolina. Expired - Lifetime ES2147840T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US16988993A 1993-12-17 1993-12-17

Publications (1)

Publication Number Publication Date
ES2147840T3 true ES2147840T3 (es) 2000-10-01

Family

ID=22617632

Family Applications (1)

Application Number Title Priority Date Filing Date
ES95905965T Expired - Lifetime ES2147840T3 (es) 1993-12-17 1994-12-13 Antagonistas de receptores de taquiquininas con morfolina.

Country Status (40)

Country Link
EP (1) EP0734381B1 (cg-RX-API-DMAC10.html)
JP (1) JP3245424B2 (cg-RX-API-DMAC10.html)
KR (1) KR100335704B1 (cg-RX-API-DMAC10.html)
CN (1) CN1057296C (cg-RX-API-DMAC10.html)
AT (1) ATE194336T1 (cg-RX-API-DMAC10.html)
AU (1) AU701862B2 (cg-RX-API-DMAC10.html)
BG (1) BG64775B1 (cg-RX-API-DMAC10.html)
BR (1) BR9408351A (cg-RX-API-DMAC10.html)
CA (1) CA2178949C (cg-RX-API-DMAC10.html)
CO (1) CO4340628A1 (cg-RX-API-DMAC10.html)
CY (2) CY2203B1 (cg-RX-API-DMAC10.html)
CZ (1) CZ295381B6 (cg-RX-API-DMAC10.html)
DE (2) DE122004000019I1 (cg-RX-API-DMAC10.html)
DK (1) DK0734381T3 (cg-RX-API-DMAC10.html)
ES (1) ES2147840T3 (cg-RX-API-DMAC10.html)
FI (1) FI109532B (cg-RX-API-DMAC10.html)
FR (1) FR04C0010I2 (cg-RX-API-DMAC10.html)
GR (1) GR3034095T3 (cg-RX-API-DMAC10.html)
HR (1) HRP941000B9 (cg-RX-API-DMAC10.html)
HU (1) HU224014B1 (cg-RX-API-DMAC10.html)
IL (1) IL111960A (cg-RX-API-DMAC10.html)
LT (1) LTC0734381I2 (cg-RX-API-DMAC10.html)
LU (1) LU91069I9 (cg-RX-API-DMAC10.html)
LV (1) LV11617B (cg-RX-API-DMAC10.html)
MY (1) MY115164A (cg-RX-API-DMAC10.html)
NL (1) NL300146I2 (cg-RX-API-DMAC10.html)
NO (3) NO308742B1 (cg-RX-API-DMAC10.html)
NZ (1) NZ278222A (cg-RX-API-DMAC10.html)
PL (1) PL182521B1 (cg-RX-API-DMAC10.html)
PT (1) PT734381E (cg-RX-API-DMAC10.html)
RO (1) RO118203B1 (cg-RX-API-DMAC10.html)
RU (1) RU2201924C2 (cg-RX-API-DMAC10.html)
SA (1) SA95150523B1 (cg-RX-API-DMAC10.html)
SI (1) SI0734381T1 (cg-RX-API-DMAC10.html)
SK (1) SK282800B6 (cg-RX-API-DMAC10.html)
TW (1) TW419471B (cg-RX-API-DMAC10.html)
UA (1) UA47397C2 (cg-RX-API-DMAC10.html)
WO (1) WO1995016679A1 (cg-RX-API-DMAC10.html)
YU (1) YU49037B (cg-RX-API-DMAC10.html)
ZA (1) ZA9410008B (cg-RX-API-DMAC10.html)

Families Citing this family (109)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1067683C (zh) * 1993-12-29 2001-06-27 默克·夏普-道姆公司 取代的吗啉衍生物及其作为治疗剂的用途
TW385308B (en) * 1994-03-04 2000-03-21 Merck & Co Inc Prodrugs of morpholine tachykinin receptor antagonists
EP0758329A1 (en) * 1994-05-05 1997-02-19 MERCK SHARP & DOHME LTD. Morpholine derivatives and their use as antagonists of tachikinins
US5824678A (en) * 1994-08-15 1998-10-20 Merck Sharp & Dohme Ltd. Morpholine derivatives and their use as therapeutic agents
GB9417956D0 (en) * 1994-09-02 1994-10-26 Merck Sharp & Dohme Therapeutic agents
GB9505491D0 (en) * 1995-03-18 1995-05-03 Merck Sharp & Dohme Therapeutic agents
GB9511031D0 (en) * 1995-06-01 1995-07-26 Merck Sharp & Dohme Chemical process
GB9513118D0 (en) * 1995-06-28 1995-08-30 Merck Sharp & Dohme Therapeutic agents
GB9523244D0 (en) * 1995-11-14 1996-01-17 Merck Sharp & Dohme Therapeutic agents
US5750549A (en) * 1996-10-15 1998-05-12 Merck & Co., Inc. Cycloalkyl tachykinin receptor antagonists
ZA985765B (en) * 1997-07-02 1999-08-04 Merck & Co Inc Polymorphic form of a tachykinin receptor antagonist.
DE69838421D1 (en) * 1997-07-02 2007-10-25 Merck & Co Inc Polymorphe form des tachykininrezeptorantagonisten 2-(r)-(1-(r)-(3,5-bis(trifluormethyl)phenyl)ethoxy)-3-(s)-(4-fluor)phenyl-4-(3-5-oxo-1h,4h-1,2,4-triazolo)methylmorpholin
GB9813025D0 (en) * 1998-06-16 1998-08-12 Merck Sharp & Dohme Chemical synthesis
EP1035115B1 (en) 1999-02-24 2004-09-29 F. Hoffmann-La Roche Ag 4-Phenylpyridine derivatives and their use as NK-1 receptor antagonists
HUP0200139A3 (en) 1999-02-24 2003-01-28 Hoffmann La Roche 3-phenylpyridine derivatives and their use as nk-1 receptor antagonists, process for their preparation and pharmaceutical compositions containing them
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
WO2001032625A1 (en) 1999-11-03 2001-05-10 Du Pont Pharmaceuticals Company Aryl- and heteroaryl-substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine and serotonin
US7163949B1 (en) 1999-11-03 2007-01-16 Amr Technology, Inc. 4-phenyl substituted tetrahydroisoquinolines and use thereof
ATE253561T1 (de) * 1999-11-29 2003-11-15 Hoffmann La Roche 2-(3,5-bis-trifluoromethyl-phenyl)-n-methyl-n-( - 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
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
CA2415532C (en) 2000-07-11 2010-05-11 Albany Molecular Research, Inc. Novel 4-phenyl substituted tetrahydroisoquinolines therapeutic use thereof
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
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
BR0209604A (pt) 2001-05-14 2004-03-23 Hoffmann La Roche Derivados de 1-oxa-3,9-diaza-spiro-5,5-undecan-2-onas e seu uso como antagonista do receptor para neuricinina
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
IL162096A0 (en) * 2001-12-07 2005-11-20 Pfizer Prod Inc Citric acid salt of a therapeutic compound and pharmaceutical compositions thereof
UA76810C2 (uk) * 2001-12-10 2006-09-15 Мерк Енд Ко., Інк. Фармацевтична композиція антагоніста рецептора тахікініну у формі наночастинок
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
NZ541243A (en) 2003-01-31 2008-04-30 Hoffmann La Roche New crystalline modification of 2-(3,5-bis-trifluoromethyl-phenyl)-N-[6-(1,1-dioxo-1lambda6-thiomorpholin-4-yl)-4-(4-fluoro-2-methyl-phenyl)-pyridin-3-yl]-N-methyl-isobutyramide
GB0310881D0 (en) * 2003-05-12 2003-06-18 Merck Sharp & Dohme Pharmaceutical formulation
WO2005002577A1 (en) 2003-07-03 2005-01-13 F. Hoffmann-La Roche Ag Dual nk1/nk3 antagonists for treating schizophrenia
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.
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
EP1856052B1 (en) 2005-02-22 2009-09-02 F.Hoffmann-La Roche Ag Nk1 antagonists
BRPI0609699A2 (pt) 2005-03-23 2010-04-20 Hoffmann La Roche metabolitos para antatonistas de nk-1 para êmese
WO2006123182A2 (en) 2005-05-17 2006-11-23 Merck Sharp & Dohme Limited Cyclohexyl sulphones for treatment of cancer
NZ565111A (en) 2005-07-15 2011-10-28 Amr Technology Inc Aryl-and heteroaryl-substituted tetrahydrobenzazepines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin
MY143784A (en) 2005-09-23 2011-07-15 Hoffmann La Roche Novel dosage formulation
WO2007041052A2 (en) 2005-09-29 2007-04-12 Merck & Co., Inc. Acylated spiropiperidine derivatives as melanocortin-4 receptor modulators
WO2007044829A2 (en) 2005-10-06 2007-04-19 Dr. Reddy's Laboratories Ltd. Preparation of aprepitant
US9227958B2 (en) * 2006-02-03 2016-01-05 Glenmark Pharmaceuticals Limited Amorphous and crystalline forms of aprepitant and processes for the preparation thereof
GB0603041D0 (en) 2006-02-15 2006-03-29 Angeletti P Ist Richerche Bio Therapeutic compounds
US20090149462A1 (en) * 2006-08-28 2009-06-11 Hetero Drugs Limited Process for purification of aprepitant
WO2008039327A2 (en) 2006-09-22 2008-04-03 Merck & Co., Inc. Method of treatment using fatty acid synthesis inhibitors
US20110218176A1 (en) 2006-11-01 2011-09-08 Barbara Brooke Jennings-Spring Compounds, methods, and treatments for abnormal signaling pathways for prenatal and postnatal development
CN101190330A (zh) 2006-11-30 2008-06-04 深圳市鼎兴生物医药技术开发有限公司 胆碱酯酶在拮抗速激肽药物中的应用
EP2805945B1 (en) 2007-01-10 2019-04-03 MSD Italia S.r.l. Amide substituted indazoles as poly(ADP-ribose)polymerase (PARP) inhibitors
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
JP5319518B2 (ja) 2007-04-02 2013-10-16 Msd株式会社 インドールジオン誘導体
CA2682506C (en) 2007-04-20 2016-05-24 F. Hoffmann-La Roche Ag Pyrrolidine derivatives as dual nk1/nk3 receptor antagonists
AU2008269154B2 (en) 2007-06-27 2014-06-12 Merck Sharp & Dohme Llc 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.
EP2254420A4 (en) 2008-02-20 2012-02-15 Targia Pharmaceuticals CNS PHARMACEUTICALS AND METHOD FOR THEIR USE
CA2717509A1 (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
EP2376514A2 (en) 2008-12-23 2011-10-19 Pharmasset, Inc. Nucleoside analogs
US8716262B2 (en) 2008-12-23 2014-05-06 Gilead Pharmasset Llc Nucleoside phosphoramidates
WO2010075554A1 (en) 2008-12-23 2010-07-01 Pharmasset, Inc. Synthesis of purine nucleosides
US8691825B2 (en) 2009-04-01 2014-04-08 Merck Sharp & Dohme Corp. Inhibitors of AKT activity
EP2429295B1 (en) 2009-05-12 2013-12-25 Albany Molecular Research, Inc. Aryl, heteroaryl, and heterocycle substituted tetrahydroisoquinolines and use thereof
KR20120023072A (ko) 2009-05-12 2012-03-12 브리스톨-마이어스 스큅 컴퍼니 (S)-7-(〔1,2,4〕트리아졸〔1,5-a〕피리딘-6-일)-4-(3,4-디클로로페닐)-1,2,3,4-테트라하이드로이소퀴놀린의 결정형 및 이의 용도
EA020553B1 (ru) 2009-05-12 2014-12-30 Олбани Молекьюлар Рисерч, Инк. 7-([1,2,4]ТРИАЗОЛО[1,5-α]ПИРИДИН-6-ИЛ)-4-(3,4-ДИХЛОРФЕНИЛ)-1,2,3,4-ТЕТРАГИДРОИЗОХИНОЛИН, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ЕГО ОСНОВЕ И СПОСОБЫ ЛЕЧЕНИЯ НЕВРОЛОГИЧЕСКИХ И ПСИХИЧЕСКИХ РАССТРОЙСТВ
CN102638981B (zh) 2009-10-14 2015-07-22 默沙东公司 提高p53活性的取代的哌啶和其用途
RS54368B1 (sr) 2010-03-31 2016-04-28 Gilead Pharmasset Llc Kristalni (s)-izopropil 2-(((s)-(((2r,3r,4r,5r)-5-(2,4-diokso-3,4-dihidropirimidin-1-(2h)-il)-4-fluoro-3-hidroksi-4-metiltetrahidrofuran-2-il)metoksi)(fenoksi)fosforil)amino)propanoat
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
EP2601293B1 (en) 2010-08-02 2017-12-06 Sirna Therapeutics, Inc. 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)
EP2608669B1 (en) 2010-08-23 2016-06-22 Merck Sharp & Dohme Corp. NOVEL PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES 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
EP2618828B1 (en) 2010-09-23 2016-11-23 Nuformix Limited Aprepitant l-proline composition and cocrystal
EP3766975A1 (en) 2010-10-29 2021-01-20 Sirna Therapeutics, Inc. Rna interference mediated inhibition of gene expression using short interfering nucleic acid (sina)
WO2012087772A1 (en) 2010-12-21 2012-06-28 Schering Corporation Indazole derivatives useful as erk inhibitors
IN2013MN02170A (cg-RX-API-DMAC10.html) 2011-04-21 2015-06-12 Piramal Entpr Ltd
WO2012146692A1 (en) 2011-04-29 2012-11-01 Sandoz Ag Novel intermediates for the preparation of highly pure aprepitant or fosaprepitant
US9023865B2 (en) 2011-10-27 2015-05-05 Merck Sharp & Dohme Corp. Compounds that are ERK inhibitors
WO2013076659A1 (en) 2011-11-25 2013-05-30 Nuformix Limited Aprepitant l-proline solvates - compositions and cocrystals
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
CZ304770B6 (cs) 2012-03-13 2014-10-08 Zentiva, K.S. Způsob výroby 3-(((2R,3S)-2-((R)-1-(3,5-bis(trifluormethyl)fenyl)ethoxy)-3-(4-fluorfenyl)morfolino)methyl)-1H-1,2,4-triazol-5(4H)-onu (Aprepitantu) v polymorfní formě II
EP3919620A1 (en) 2012-05-02 2021-12-08 Sirna Therapeutics, Inc. Short interfering nucleic acid (sina) compositions
RU2660429C2 (ru) 2012-09-28 2018-07-06 Мерк Шарп И Доум Корп. Новые соединения, которые являются ингибиторами erk
PL2925888T3 (pl) 2012-11-28 2018-03-30 Merck Sharp & Dohme Corp. Kompozycje i sposoby do stosowania w leczeniu nowotworów
KR102196882B1 (ko) 2012-12-20 2020-12-30 머크 샤프 앤드 돔 코포레이션 Hdm2 억제제로서의 치환된 이미다조피리딘
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
CN103694146B (zh) * 2013-12-04 2015-10-28 深圳万乐药业有限公司 2-(2-氯-1-亚乙基)酰肼甲酸甲酯的制备方法
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
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
SI3435980T1 (sl) 2016-06-06 2020-03-31 Helsinn Healthcare Sa Fiziološko uravnotežene injektabilne formulacije fosnetupitanta
EP3525785B1 (en) 2016-10-12 2025-08-27 Merck Sharp & Dohme LLC 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
EP3833668B1 (en) 2018-08-07 2025-03-19 Merck Sharp & Dohme LLC Prmt5 inhibitors
WO2020033284A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
MA53287A (fr) 2018-08-07 2022-05-11 Merck Sharp & Dohme Inhibiteurs de prmt5
EP4125875A1 (en) 2020-04-03 2023-02-08 NeRRe Therapeutics Limited An nk-1 receptor antagonist for treating a disease selecting from sepsis, septic shock,, acute respiratory distress syndrome (ards) or multiple organ dysfunction syndrome (mods)
MX2022014901A (es) 2020-06-02 2023-01-18 Nerre Therapeutics Ltd Antagonistas del receptor de neuroquinina (nk)-1 para su uso en el tratamiento de condiciones de fibrosis pulmonar promovidas por lesion mecanica a los pulmones.

Family Cites Families (4)

* 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
ATE136885T1 (de) * 1991-08-20 1996-05-15 Merck Sharp & Dohme 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
EP0683767B1 (en) * 1993-02-18 1998-06-03 MERCK SHARP & DOHME LTD. Azacyclic compounds, compositions containing them and their use as tachykinin antagonists

Also Published As

Publication number Publication date
LTC0734381I2 (lt) 2017-04-25
RO118203B1 (ro) 2003-03-28
LV11617A (lv) 1996-12-20
CZ295381B6 (cs) 2005-07-13
HU9601634D0 (en) 1996-08-28
HRP941000A2 (en) 1997-06-30
WO1995016679A1 (en) 1995-06-22
RU2201924C2 (ru) 2003-04-10
JPH09506628A (ja) 1997-06-30
CA2178949A1 (en) 1995-06-22
NO2004003I2 (no) 2006-10-04
PL315153A1 (en) 1996-10-14
HRP941000B1 (en) 2001-04-30
AU1437595A (en) 1995-07-03
CZ177296A3 (en) 1996-12-11
NL300146I2 (nl) 2004-07-01
NO2018011I1 (no) 2018-04-04
FR04C0010I1 (cg-RX-API-DMAC10.html) 2004-05-21
BG100715A (bg) 1997-01-31
CN1057296C (zh) 2000-10-11
BR9408351A (pt) 1997-08-26
ZA9410008B (en) 1996-07-15
NO308742B1 (no) 2000-10-23
JP3245424B2 (ja) 2002-01-15
NL300146I1 (nl) 2004-06-01
CN1142819A (zh) 1997-02-12
LU91069I2 (fr) 2004-04-07
EP0734381A1 (en) 1996-10-02
ATE194336T1 (de) 2000-07-15
KR960706483A (ko) 1996-12-09
DE69425161T2 (de) 2001-02-15
HUT76476A (en) 1997-09-29
FI962489A7 (fi) 1996-08-13
PT734381E (pt) 2000-12-29
DK0734381T3 (da) 2000-09-18
IL111960A0 (en) 1995-03-15
NO2004003I1 (no) 2004-06-28
SI0734381T1 (en) 2000-10-31
FR04C0010I2 (fr) 2004-12-17
IL111960A (en) 1999-12-22
UA47397C2 (uk) 2002-07-15
YU74694A (sh) 1997-08-22
LTPA2004002I1 (lt) 2016-11-10
HK1009046A1 (en) 1999-05-21
EP0734381B1 (en) 2000-07-05
CA2178949C (en) 2006-03-21
YU49037B (sh) 2003-07-07
GR3034095T3 (en) 2000-11-30
BG64775B1 (bg) 2006-03-31
SK282800B6 (sk) 2002-12-03
NO2018011I2 (no) 2018-12-14
PL182521B1 (pl) 2002-01-31
LU91069I9 (en) 2018-07-24
TW419471B (en) 2001-01-21
KR100335704B1 (ko) 2002-11-18
FI109532B (fi) 2002-08-30
HRP941000B9 (hr) 2014-11-07
CO4340628A1 (es) 1996-07-30
HU224014B1 (hu) 2005-04-28
CY2203B1 (en) 2002-11-08
DE69425161D1 (de) 2000-08-10
NO962523D0 (no) 1996-06-14
SK75396A3 (en) 1996-12-04
SA95150523B1 (ar) 2006-03-15
DE122004000019I1 (de) 2004-09-30
MY115164A (en) 2003-04-30
NZ278222A (en) 1998-05-27
AU701862B2 (en) 1999-02-04
CY2004012I2 (el) 2017-04-05
LV11617B (en) 1997-04-20
CY2004012I1 (el) 2010-07-28
FI962489A0 (fi) 1996-06-14
NO962523L (no) 1996-08-16

Similar Documents

Publication Publication Date Title
ES2147840T3 (es) Antagonistas de receptores de taquiquininas con morfolina.
MX9303888A (es) Antagonistas receptores de taquiquinina de morfolina y tiomorfolina.
ES2054872T3 (es) Nuevos derivados de acido bencimidazolin-2-oxo-1-carboxilico utiles como antagonistas de los receptores 5-ht.
ES2188584T3 (es) Derivados heterociclicos de amina.
AR039489A1 (es) Derivados de tetrahidropiranil ciclopentil tetrahidropiridopiridina, moduladores de actividad de receptores de citoquinas
ES2113368T3 (es) Antagonistas de serotonina.
LTPA2016013I1 (lt) 2-okso-1-pirolidino dariniai, jų gamybos būdas ir jų panaudojimas
ES2138977T3 (es) Agonistas muscarinicos.
ES2159758T3 (es) Nuevas n-aminoalquilfluorenocarboxamidas; una nueva clase de ligandos especificos a subtipos del receptor de la dopamina.
MX9300842A (es) Antagonistas de endotelina de sulfonamida.
ES2116587T3 (es) Derivados espiroazaciclicos como antagonistas de la sustancia p.
ES2067248T3 (es) Derivados de indol como agentes antialergicos y antiinflamatorios.
ES2181995T3 (es) Derivados de bencimidazol y uso como antagonistas del factor de liberacion de la corticotropina.
PE83999A1 (es) Azetidinas
PE16399A1 (es) Compuestos heterociclicos de guanidinilo utiles como agonistas de alfa-2 adrenoreceptores
ES2123873T3 (es) Pirrolocarbazol.
MX9700959A (es) Derivados de becimidazol que tienen actividad dopaminergica.
UY26329A1 (es) Antagonistas de los receptores de vitronectina
ES2161916T3 (es) Derivados de la tiazolidinona o de la oxazolidinona para el tratamiento de la angina de pecho y composiciones que las contienen como ingrediente activo.
ES2187783T3 (es) Derivados de indolina utiles como antagonistas del receptor 5-ht-2c.
AR022536A1 (es) INHIBIDORES DE CAPROLACTAMA DEL FACTOR Xa Y METODO
ES2070772B1 (es) Derivados de acilaminoindol
UY24571A1 (es) Nuevos derivados del pirrol

Legal Events

Date Code Title Description
FG2A Definitive protection

Ref document number: 734381

Country of ref document: ES