LU91069I2 - Aprepitant et ses sels pharmaceutiquement acceptables (EMEND) - Google Patents

Aprepitant et ses sels pharmaceutiquement acceptables (EMEND)

Info

Publication number
LU91069I2
LU91069I2 LU91069C LU91069C LU91069I2 LU 91069 I2 LU91069 I2 LU 91069I2 LU 91069 C LU91069 C LU 91069C LU 91069 C LU91069 C LU 91069C LU 91069 I2 LU91069 I2 LU 91069I2
Authority
LU
Luxembourg
Prior art keywords
substituted
pharmaceutically acceptable
group
emend
aprepitant
Prior art date
Application number
LU91069C
Other languages
English (en)
Other versions
LU91069I9 (en
Original Assignee
Merck & 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=LU91069(I2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Publication of LU91069I2 publication Critical patent/LU91069I2/fr
Publication of LU91069I9 publication Critical patent/LU91069I9/fr

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)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Otolaryngology (AREA)
  • Vascular Medicine (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Peptides Or Proteins (AREA)
LU91069C 1993-12-17 1994-12-13 Morpholine tachykinin receptor antagonists LU91069I9 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US16988993A 1993-12-17 1993-12-17
PCT/US1994/014497 WO1995016679A1 (fr) 1993-12-17 1994-12-13 Antagonistes de recepteurs des tachykinines, a base de morpholine et thiomorpholine

Publications (2)

Publication Number Publication Date
LU91069I2 true LU91069I2 (fr) 2004-04-07
LU91069I9 LU91069I9 (en) 2018-07-24

Family

ID=22617632

Family Applications (1)

Application Number Title Priority Date Filing Date
LU91069C LU91069I9 (en) 1993-12-17 1994-12-13 Morpholine tachykinin receptor antagonists

Country Status (40)

Country Link
EP (1) EP0734381B1 (fr)
JP (1) JP3245424B2 (fr)
KR (1) KR100335704B1 (fr)
CN (1) CN1057296C (fr)
AT (1) ATE194336T1 (fr)
AU (1) AU701862B2 (fr)
BG (1) BG64775B1 (fr)
BR (1) BR9408351A (fr)
CA (1) CA2178949C (fr)
CO (1) CO4340628A1 (fr)
CY (2) CY2203B1 (fr)
CZ (1) CZ295381B6 (fr)
DE (2) DE69425161T2 (fr)
DK (1) DK0734381T3 (fr)
ES (1) ES2147840T3 (fr)
FI (1) FI109532B (fr)
FR (1) FR04C0010I2 (fr)
GR (1) GR3034095T3 (fr)
HR (1) HRP941000B9 (fr)
HU (1) HU224014B1 (fr)
IL (1) IL111960A (fr)
LT (1) LTC0734381I2 (fr)
LU (1) LU91069I9 (fr)
LV (1) LV11617B (fr)
MY (1) MY115164A (fr)
NL (1) NL300146I2 (fr)
NO (3) NO308742B1 (fr)
NZ (1) NZ278222A (fr)
PL (1) PL182521B1 (fr)
PT (1) PT734381E (fr)
RO (1) RO118203B1 (fr)
RU (1) RU2201924C2 (fr)
SA (1) SA95150523B1 (fr)
SI (1) SI0734381T1 (fr)
SK (1) SK282800B6 (fr)
TW (1) TW419471B (fr)
UA (1) UA47397C2 (fr)
WO (1) WO1995016679A1 (fr)
YU (1) YU49037B (fr)
ZA (1) ZA9410008B (fr)

Families Citing this family (109)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995018124A1 (fr) * 1993-12-29 1995-07-06 Merck Sharp & Dohme Limited Derives de morpholine substitues et une utilisation en tant qu'agents therapeutiques
IL112778A0 (en) * 1994-03-04 1995-05-26 Merck & Co Inc Substituted heterocycles, their preparation and pharmaceutical compositions containing them
WO1995030674A1 (fr) * 1994-05-05 1995-11-16 Merck Sharp & Dohme Limited Derives de morpholine et utilisation comme antagonistes des tachykinines
ES2157337T3 (es) * 1994-08-15 2001-08-16 Merck Sharp & Dohme Derivados de morfolina y su uso como agentes terapeuticos.
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
WO1999001444A1 (fr) * 1997-07-02 1999-01-14 Merck & Co., Inc. Forme polymorphe de l'antagoniste de recepteur de tachykinine 2-(r)-(1-(r) -(3,5-bis(trifluoromethyl) phenyl)ethoxy)-3-(s)-(4-fluoro) phenyl-4-(3-5 (-oxo-1h,4h-1,2,4,-triazolo) methylmorpholine
ZA985765B (en) 1997-07-02 1999-08-04 Merck & Co Inc Polymorphic form of a tachykinin receptor antagonist.
GB9813025D0 (en) * 1998-06-16 1998-08-12 Merck Sharp & Dohme Chemical synthesis
CN1134417C (zh) 1999-02-24 2004-01-14 弗·哈夫曼-拉罗切有限公司 3-苯基吡啶衍生物及其作为nk-1受体拮抗剂的应用
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.
IL144717A0 (en) 1999-02-24 2002-06-30 Hoffmann La Roche Phenyl-and pyridinyl derivatives
US6291465B1 (en) 1999-03-09 2001-09-18 Hoffmann-La Roche Inc. Biphenyl derivatives
US7163949B1 (en) 1999-11-03 2007-01-16 Amr Technology, Inc. 4-phenyl substituted tetrahydroisoquinolines and use thereof
PT1246806E (pt) 1999-11-03 2008-04-03 Amr Technology Inc Tetra-hidroisoquinolinas aril- e heteroaril-substituídas e sua utilização no bloqueio da recaptação de norepinefrina, dopamina e serotonina.
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
CA2415532C (fr) 2000-07-11 2010-05-11 Albany Molecular Research, Inc. Nouvelles tetrahydroisoquinolines 4-phenyl substituees et leur utilisation a des fins therapeutiques
WO2002006236A1 (fr) 2000-07-14 2002-01-24 F. Hoffmann-La Roche Ag N-oxydes en tant que promedicaments de derives de 4-phenyl-pyridine, antagonistes du recepteur nk1
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
WO2002092604A1 (fr) 2001-05-14 2002-11-21 F. Hoffmann-La Roche Ag Derives de 1-oxa-3,9-diaza-spiro[5,5]undecan-2-ones et leur utilisation comme antagoniste du recepteur de neurikinie
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
MXPA04005418A (es) * 2001-12-07 2005-04-19 Pfizer Prod Inc Sal de acido citrico de un compuesto terapeutico y composiciones farmaceuticas que la contienen.
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
RU2330022C2 (ru) * 2003-01-31 2008-07-27 Ф.Хоффманн-Ля Рош Аг НОВАЯ КРИСТАЛЛИЧЕСКАЯ МОДИФИКАЦИЯ 2-(3, 5-БИС-ТРИФТОРМЕТИЛФЕНИЛ)-N-[6-(1, 1-ДИОКСО-1 λ6-ТИОМОРФОЛИН-4-ИЛ)-4-(4-ФТОР-2-МЕТИЛФЕНИЛ)ПИРИДИН-3-ИЛ]-N-МЕТИЛИЗОБУТИРАМИДА
GB0310881D0 (en) * 2003-05-12 2003-06-18 Merck Sharp & Dohme Pharmaceutical formulation
ES2291891T3 (es) 2003-07-03 2008-03-01 F. Hoffmann-La Roche Ag Antagonistas duales de nk1/nk3 para tratamiento de esquizofrenia.
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.
KR101389246B1 (ko) 2004-07-15 2014-04-24 브리스톨-마이어스스퀴브컴파니 아릴- 및 헤테로아릴-치환된 테트라히드로이소퀴놀린, 및 이것의 노르에피네프린, 도파민 및 세로토닌의 재흡수를 차단하기 위한 용도
CA2601935C (fr) 2005-02-22 2013-04-09 F. Hoffmann-La Roche Ag Antagonistes de nk1
RU2404969C2 (ru) 2005-03-23 2010-11-27 Ф. Хоффманн-Ля Рош Аг Метаболиты антагонистов nk-1 против рвоты
US8362075B2 (en) 2005-05-17 2013-01-29 Merck Sharp & Dohme Corp. Cyclohexyl sulphones for treatment of cancer
GEP20125566B (en) 2005-07-15 2012-07-10 Amr Technology Inc Aryl-and heteroaryl-substituded tetrahydro-benzazepines and use thereof to block reuptake of norepinephrine, dopamine and serotonin
CA2623237C (fr) 2005-09-23 2013-07-09 F. Hoffmann-La Roche Ag Nouvelle forme galenique
WO2007041052A2 (fr) 2005-09-29 2007-04-12 Merck & Co., Inc. Derives spiropiperidines acyles convenant comme modulateurs des recepteurs de la melanocortine-4
EP1942734A4 (fr) 2005-10-06 2010-04-07 Reddys Lab Ltd Dr Preparation de l'aprepitant
EP1984359A1 (fr) * 2006-02-03 2008-10-29 Glenmark Pharmaceuticals Limited Formes amorphes et cristallines d'aprépitant et procédés pour leur préparation
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
EP2698157B1 (fr) 2006-09-22 2015-05-20 Merck Sharp & Dohme Corp. Procédé de traitement utilisant des inhibiteurs de synthèse d'acide gras
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
DK2805945T3 (da) 2007-01-10 2019-07-15 Msd Italia Srl Amid-substituerede indazoler som poly(adp-ribose)polymerase- (parp) hæmmere
EP2117538A1 (fr) 2007-01-24 2009-11-18 Glaxo Group Limited Compositions pharmaceutiques contenant du 2-méthoxy-5- (5-trifluorométhyl-tétrazol-i-yl-benzyl) - (2s-phényl-pipéridin-3s-yl-)
JP5319518B2 (ja) 2007-04-02 2013-10-16 Msd株式会社 インドールジオン誘導体
JP5203449B2 (ja) 2007-04-20 2013-06-05 エフ.ホフマン−ラ ロシュ アーゲー 二重nk1/nk3受容体アンタゴニストとしてのピロリジン誘導体
EP3103791B1 (fr) 2007-06-27 2018-01-31 Merck Sharp & Dohme Corp. Dérivés de 4-carboxybenzylamino utilisés comme inhibiteurs de l'histone désacétylase
EP2185540B1 (fr) 2007-08-07 2011-07-20 F. Hoffmann-La Roche AG Composés de pyrrolidine aryle-éther utilisés comme antagonistes des récepteurs nk3
EP2254420A4 (fr) 2008-02-20 2012-02-15 Targia Pharmaceuticals Compositions pharmaceutiques actives sur le snc et méthodes d'utilisation
EP2247185B1 (fr) 2008-03-03 2014-04-16 Tiger Pharmatech Inhibiteurs de la tyrosine kinase
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
BRPI0922508A8 (pt) 2008-12-23 2016-01-19 Pharmasset Inc Análogos de nucleosídeo
CA2748057C (fr) 2008-12-23 2018-07-03 Pharmasset, Inc. Phosphoramidates de nucleosides
EA019295B1 (ru) 2008-12-23 2014-02-28 Джилид Фармассет, Ллс. Соединения пуриновых нуклеозидов и способ их получения
WO2010114780A1 (fr) 2009-04-01 2010-10-07 Merck Sharp & Dohme Corp. Inhibiteurs de l'activité akt
CN102458123A (zh) 2009-05-12 2012-05-16 阿尔巴尼分子研究公司 芳基、杂芳基和杂环取代的四氢异喹啉及其用途
ES2528404T3 (es) 2009-05-12 2015-02-10 Bristol-Myers Squibb Company Formas cristalinas de (S)-7-([1,2,4]triazol[1,5-a]piridin-6-il)-4-(3,4-diclorofenil)-1,2,3,4-tetrahidroisoquinolina y sus usos
SG175420A1 (en) 2009-05-12 2011-12-29 Albany Molecular Res Inc 7-([1,2,4,]triazolo[1,5,-a]pyridin-6-yl)-4-(3,4-dichlorophenyl)-1,2,3,4- tetrahydroisoquinoline and use thereof
AU2010307198C9 (en) 2009-10-14 2014-02-13 Merck Sharp & Dohme Corp. Substituted piperidines that increase p53 activity and the uses thereof
TWI498117B (zh) 2010-03-31 2015-09-01 Gilead Pharmasset Llc 核苷氨基磷酸酯
US8487102B2 (en) 2010-04-20 2013-07-16 Hoffmann-La Roche Inc. Pyrrazolopyridine compounds as dual NK1/NK3 receptor antagonists
WO2011163330A1 (fr) 2010-06-24 2011-12-29 Merck Sharp & Dohme Corp. Nouveaux composés hétérocycliques utilisés comme inhibiteurs de erk
JP6043285B2 (ja) 2010-08-02 2016-12-14 サーナ・セラピューティクス・インコーポレイテッドSirna Therapeutics,Inc. 低分子干渉核酸(siNA)を用いたカテニン(カドヘリン結合型タンパク質)β1(CTNNB1)遺伝子発現のRNA干渉媒介性阻害
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
EP2608669B1 (fr) 2010-08-23 2016-06-22 Merck Sharp & Dohme Corp. Nouveaux dérivés de pyrazolo[1,5-a]pyrimidine utilisés comme inhibiteurs de mtor
EP2613782B1 (fr) 2010-09-01 2016-11-02 Merck Sharp & Dohme Corp. Dérivés d'indazole utilisables en tant qu'inhibiteurs de la voie erk
EP2615916B1 (fr) 2010-09-16 2017-01-04 Merck Sharp & Dohme Corp. Dérivés condensés de pyrazole utilisés comme nouveaux inhibiteurs erk
EP2618828B1 (fr) 2010-09-23 2016-11-23 Nuformix Limited Composition et cocristal d'aprépitant l-proline
EP3327125B1 (fr) 2010-10-29 2020-08-05 Sirna Therapeutics, Inc. Inhibition au moyen d'interférence arn d'une expression de gène utilisant des acides nucléiques à petit interférent (sina)
WO2012087772A1 (fr) 2010-12-21 2012-06-28 Schering Corporation Dérivés d'indazole utiles en tant qu'inhibiteurs de erk
EP2699568A1 (fr) 2011-04-21 2014-02-26 Piramal Enterprises Limited Forme cristalline d'un sel d'un dérivé de morpholinosulfonylindole et son procédé de préparation
WO2012146692A1 (fr) 2011-04-29 2012-11-01 Sandoz Ag Nouveaux intermédiaires pour la préparation d'aprépitant ou de fosaprépitant de pureté élevée
EP2770987B1 (fr) 2011-10-27 2018-04-04 Merck Sharp & Dohme Corp. Nouveaux composés qui sont des inhibiteurs d'erk
CN104159584A (zh) 2011-11-25 2014-11-19 诺弗米克斯有限公司 阿瑞吡坦l-脯氨酸溶剂化物-组合物和共晶体
WO2013087964A1 (fr) 2011-12-13 2013-06-20 Servicio Andaluz De Salud Utilisation d'agents modificateurs de l'environnement péritumoral pour le traitement du 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
US20150299696A1 (en) 2012-05-02 2015-10-22 Sirna Therapeutics, Inc. SHORT INTERFERING NUCLEIC ACID (siNA) COMPOSITIONS
KR20150060724A (ko) 2012-09-28 2015-06-03 머크 샤프 앤드 돔 코포레이션 Erk 억제제인 신규 화합물
JP6290237B2 (ja) 2012-11-28 2018-03-07 メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. 癌を処置するための組成物および方法
US8846657B2 (en) 2012-12-20 2014-09-30 Merck Sharp & Dohme Corp. Substituted imidazopyridines as HDM2 inhibitors
WO2014120748A1 (fr) 2013-01-30 2014-08-07 Merck Sharp & Dohme Corp. Purines 2,6,7,8-substituées utilisées en tant qu'inhibiteurs de hdm2
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 (fr) 2013-09-03 2015-03-12 Moderna Therapeutics, Inc. Polynucléotides circulaires
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
EP3435980B1 (fr) 2016-06-06 2019-11-13 Helsinn Healthcare SA Formulations injectables de fosnetupitant physiologiquement equilibrees
EP3525785B1 (fr) 2016-10-12 2025-08-27 Merck Sharp & Dohme LLC Inhibiteurs de kdm5
EP3706742B1 (fr) 2017-11-08 2023-03-15 Merck Sharp & Dohme LLC Inhibiteurs de prmt5
WO2019094312A1 (fr) 2017-11-08 2019-05-16 Merck Sharp & Dohme Corp. Inhibiteurs de prmt5
CA3108388A1 (fr) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Inhibiteurs de prmt5
US11993602B2 (en) 2018-08-07 2024-05-28 Merck Sharp & Dohme Llc PRMT5 inhibitors
US11981701B2 (en) 2018-08-07 2024-05-14 Merck Sharp & Dohme Llc PRMT5 inhibitors
BR112022018876A2 (pt) 2020-04-03 2022-11-22 Nerre Therapeutics Ltd Antagonista de receptor de nk-1 para tratar uma doença selecionada a partir de sepse, choque séptico, síndrome de desconforto respiratório agudo (ards) ou síndrome de disfunção múltipla dos órgãos
AU2021285503A1 (en) 2020-06-02 2022-12-08 Nerre Therapeutics Limited Neurokinin (NK)-1 receptor antagonists for use in the treatment of pulmonary fibrosis conditions promoted by mechanical injury to the lungs

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
CA2112397A1 (fr) * 1991-08-20 1993-03-04 Raymond Baker Composes azacyclique, procedes pour les preparer et compositions pharmaceutiques les contenant
IL106142A (en) * 1992-06-29 1997-03-18 Merck & Co Inc Morpholine and thiomorpholine tachykinin receptor antagonists, their preparation and pharmaceutical compositions containing them
CA2152925A1 (fr) * 1993-02-18 1994-09-01 Raymond Baker Composes azacycliques; compositions qui en renferment et leur utilisation comme antagonistes de la tachykinine

Also Published As

Publication number Publication date
AU701862B2 (en) 1999-02-04
SI0734381T1 (en) 2000-10-31
RU2201924C2 (ru) 2003-04-10
NO2018011I1 (no) 2018-04-04
HU9601634D0 (en) 1996-08-28
NL300146I2 (nl) 2004-07-01
CY2004012I1 (el) 2010-07-28
NZ278222A (en) 1998-05-27
KR100335704B1 (ko) 2002-11-18
JP3245424B2 (ja) 2002-01-15
PT734381E (pt) 2000-12-29
AU1437595A (en) 1995-07-03
HU224014B1 (hu) 2005-04-28
EP0734381B1 (fr) 2000-07-05
NO2004003I2 (no) 2006-10-04
ATE194336T1 (de) 2000-07-15
IL111960A (en) 1999-12-22
BG100715A (bg) 1997-01-31
CN1057296C (zh) 2000-10-11
HUT76476A (en) 1997-09-29
DE122004000019I1 (de) 2004-09-30
CZ177296A3 (en) 1996-12-11
JPH09506628A (ja) 1997-06-30
LTC0734381I2 (lt) 2017-04-25
LTPA2004002I1 (lt) 2016-11-10
MY115164A (en) 2003-04-30
PL315153A1 (en) 1996-10-14
HK1009046A1 (en) 1999-05-21
PL182521B1 (pl) 2002-01-31
IL111960A0 (en) 1995-03-15
NO2018011I2 (no) 2018-12-14
ES2147840T3 (es) 2000-10-01
DE69425161D1 (de) 2000-08-10
NO962523D0 (no) 1996-06-14
TW419471B (en) 2001-01-21
WO1995016679A1 (fr) 1995-06-22
YU49037B (sh) 2003-07-07
NO962523L (no) 1996-08-16
BR9408351A (pt) 1997-08-26
ZA9410008B (en) 1996-07-15
FI962489A0 (fi) 1996-06-14
GR3034095T3 (en) 2000-11-30
LV11617B (en) 1997-04-20
CZ295381B6 (cs) 2005-07-13
CO4340628A1 (es) 1996-07-30
RO118203B1 (ro) 2003-03-28
HRP941000B9 (hr) 2014-11-07
DK0734381T3 (da) 2000-09-18
FR04C0010I2 (fr) 2004-12-17
SA95150523B1 (ar) 2006-03-15
YU74694A (sh) 1997-08-22
EP0734381A1 (fr) 1996-10-02
UA47397C2 (uk) 2002-07-15
LU91069I9 (en) 2018-07-24
NL300146I1 (nl) 2004-06-01
SK282800B6 (sk) 2002-12-03
CN1142819A (zh) 1997-02-12
LV11617A (lv) 1996-12-20
DE69425161T2 (de) 2001-02-15
NO2004003I1 (no) 2004-06-28
SK75396A3 (en) 1996-12-04
BG64775B1 (bg) 2006-03-31
CA2178949A1 (fr) 1995-06-22
CY2203B1 (en) 2002-11-08
KR960706483A (ko) 1996-12-09
FI109532B (fi) 2002-08-30
HRP941000A2 (en) 1997-06-30
CA2178949C (fr) 2006-03-21
FI962489A7 (fi) 1996-08-13
HRP941000B1 (en) 2001-04-30
NO308742B1 (no) 2000-10-23
CY2004012I2 (el) 2017-04-05
FR04C0010I1 (fr) 2004-05-21

Similar Documents

Publication Publication Date Title
LU91069I2 (fr) Aprepitant et ses sels pharmaceutiquement acceptables (EMEND)
BR1100375A (pt) Composto, composição farmacêutica, e, processo para a preparação de um composto
NO911525D0 (no) Nye 2,9-disubstituerte-4h-pyrido(1,2-a)pyrimidin-4-oner.
EA199800603A1 (ru) Производные 1-(1,2-дизамещенный пиперидинил)-4-(конденсированный имидазол)-пиперидина
HRP20000585B1 (en) Substituted bisindolymaleimides for the inhibition of cell proliferation
DK0920425T3 (da) Substituerede 4-(1H-benzimidazol-2-yl-amino)piperidiner, der er nyttige til behandling af allergiske sygdomme
ATE284871T1 (de) Bicyclische vasopressin-agoniste
NO933837L (no) 4-aryl-3-(heteroarylureido)kinolin-derivater
DE69402703D1 (de) 3-(INDOL-3-YL) PROPENSäURDERIVATE, DIE ALS NMDA- ANTAGONISTEN NÜTZLICH SIND
DE50112633D1 (de) (4-acylaminopiperidin-1-yl)acetamide als neurokininantagonisten
ITMI20032102A1 (it) Composti peptidomimetici, procedimento stereoselettivo per la loro preparazione, loro uso come intermedi di sintesi di derivati biologicamente attivi.