LU91069I9 - Morpholine tachykinin receptor antagonists - Google Patents

Morpholine tachykinin receptor antagonists

Info

Publication number
LU91069I9
LU91069I9 LU91069C LU91069C LU91069I9 LU 91069 I9 LU91069 I9 LU 91069I9 LU 91069 C LU91069 C LU 91069C LU 91069 C LU91069 C LU 91069C LU 91069 I9 LU91069 I9 LU 91069I9
Authority
LU
Luxembourg
Prior art keywords
substituted
receptor antagonists
group
tachykinin receptor
unsubstituted
Prior art date
Application number
LU91069C
Other languages
English (en)
Other versions
LU91069I2 (fr
Inventor
Conrad P Dorn
Paul E Finke
Jeffrey J Hale
Malcolm Maccoss
Sander G Mills
Shrenik K Shah
Mark Stuart Chambers
Timothy Harrison
Tamara Ladduwahetty
Brian John Williams
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
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(I9) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Publication of LU91069I2 publication Critical patent/LU91069I2/fr
Publication of LU91069I9 publication Critical patent/LU91069I9/fr

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/08—Vasodilators for multiple indications
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • C07D265/32—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings with oxygen atoms directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/10—1,4-Thiazines; Hydrogenated 1,4-thiazines
    • C07D279/12—1,4-Thiazines; Hydrogenated 1,4-thiazines not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Otolaryngology (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)
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 LU91069I2 (fr) 2004-04-07
LU91069I9 true 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
IL112134A (en) * 1993-12-29 1999-12-22 Merck Sharp & Dohme Substituted morpholine derivatives 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
WO1995030674A1 (fr) * 1994-05-05 1995-11-16 Merck Sharp & Dohme Limited Derives de morpholine et utilisation comme antagonistes des tachykinines
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
PL191496B1 (pl) * 1997-07-02 2006-05-31 Merck & Co Inc Odmiana polimorficzna 2-(R)-{1-(R) -[3,5-bis(trifluorometylo)-fenylo]etoksy} -3-(S)-(4-fluoro) fenylo-4-[3-(5-okso-1H,4H-1,2,4-triazolo)metylo] morfoliny, sposób jej wytwarzania, zawierająca ją kompozycja farmaceutyczna i jej zastosowanie
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
TR200102490T2 (tr) * 1999-02-24 2001-12-21 F.Hoffmann-La Roche Ag Fenil ve piridinil türevleri
KR100437587B1 (ko) 1999-02-24 2004-06-30 에프. 호프만-라 로슈 아게 3-페닐피리딘 유도체 및 그의 뉴로키닌-1 수용체길항제로서의 용도
PT1035115E (pt) 1999-02-24 2005-01-31 Hoffmann La Roche Derivados de 4-fenilpiridina e a sua utilizacao como antagonistas do receptor nk-1
US6291465B1 (en) 1999-03-09 2001-09-18 Hoffmann-La Roche Inc. Biphenyl derivatives
MXPA02004330A (es) 1999-11-03 2004-07-30 Albany Molecular Res Inc Tetrahidroisoquinolinas aril-y heteroaril-sustituidas y uso de las mismas para bloquear la recaptacion de norepinefrina, dopamina y serotonina..
US7163949B1 (en) 1999-11-03 2007-01-16 Amr Technology, Inc. 4-phenyl substituted tetrahydroisoquinolines and use thereof
SI1103545T1 (en) * 1999-11-29 2004-02-29 F. Hoffmann-La Roche Ag 2-(3,5-Bis-trifluoromethyl-phenyl)-N-methyl-N-(6-morpholin-4-yl-4-o-tolyl-pyridin-3-yl)-isobutyramide
US6452001B2 (en) 2000-05-25 2002-09-17 Hoffmann-La Roche Inc. Diazapane derivatives useful as antagonists of neurokinin 1 receptor and methods for their formation
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
KR100821410B1 (ko) 2000-07-11 2008-04-10 에이엠알 테크놀로지, 인크. 4-페닐 치환된 테트라하이드로이소퀴놀린 및 이의치료학적 용도
MXPA03000366A (es) 2000-07-14 2003-05-27 Hoffmann La Roche N-oxidos como profarmacos antagonistas del receptor nk1 de derivados de 4-fenil-piridina.
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
CN1264847C (zh) 2001-05-14 2006-07-19 弗·哈夫曼-拉罗切有限公司 1－氧杂－3,9－二氮杂－螺[5.5]十一－2－酮衍生物及其作为神经激肽受体拮抗剂的用途
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
DE60205504T2 (de) * 2001-12-07 2006-06-08 Pfizer Products Inc., Groton Zitronensäure salz von einer therapeutischen verbindung und deren pharmazeutischen zusammensetzungen
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
RU2347777C2 (ru) 2003-07-03 2009-02-27 Ф.Хоффманн-Ля Рош Аг Двойные агонисты nk1/nk3 для лечения шизофрении
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.
NZ552397A (en) 2004-07-15 2011-04-29 Amr Technology Inc Aryl-and heteroaryl-substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin
MX2007010034A (es) 2005-02-22 2007-10-04 Hoffmann La Roche Antagonista de nk1.
ATE425144T1 (de) 2005-03-23 2009-03-15 Hoffmann La Roche Metaboliten für nk-i-antagonisten zur 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
KR101594898B1 (ko) 2005-07-15 2016-02-18 알바니 몰레큘라 리써치, 인크. 아릴- 및 헤테로아릴-치환된 테트라히드로벤자제핀, 및 노르에피네프린, 도파민 및 세로토닌의 재흡수를 차단하기 위한 용도
CN103893145A (zh) 2005-09-23 2014-07-02 弗·哈夫曼-拉罗切有限公司 新型制剂
EP1940842B1 (fr) 2005-09-29 2012-05-30 Merck Sharp & Dohme Corp. Dérivés acylés de spiropipéridine en tant que modulateurs du récepteur de la mélanocortine-4
US8133994B2 (en) 2005-10-06 2012-03-13 Dr. Reddy's Laboratories Ltd. Preparation of 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
EP2057151A4 (fr) * 2006-08-28 2010-07-21 Hetero Drugs Ltd Procédé de purification d'aprépitant
US8173629B2 (en) 2006-09-22 2012-05-08 Merck Sharp & Dohme Corp. 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
JP4611444B2 (ja) 2007-01-10 2011-01-12 イステイチユート・デイ・リチエルケ・デイ・ビオロジア・モレコラーレ・ピ・アンジエレツテイ・エツセ・ピー・アー ポリ（ａｄｐ−リボース）ポリメラーゼ（ｐａｒｐ）阻害剤としてのアミド置換インダゾール
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
AU2008240804B2 (en) 2007-04-20 2013-02-21 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
CN101778837A (zh) 2007-08-07 2010-07-14 弗·哈夫曼-拉罗切有限公司 作为nk3受体拮抗剂的吡咯烷芳基-醚
CA2716080C (fr) 2008-02-20 2016-12-13 Targia Pharmaceuticals Compositions pharmaceutiques actives sur le snc et methodes d'utilisation
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
PA8855601A1 (es) 2008-12-23 2010-07-27 Forformidatos de nucleósidos
NZ593649A (en) 2008-12-23 2013-11-29 Gilead Pharmasset Llc Nucleoside analogs
AU2009329872B2 (en) 2008-12-23 2016-07-07 Gilead Pharmasset Llc Synthesis of purine nucleosides
WO2010114780A1 (fr) 2009-04-01 2010-10-07 Merck Sharp & Dohme Corp. Inhibiteurs de l'activité akt
WO2010132437A1 (fr) 2009-05-12 2010-11-18 Albany Molecular Research, Inc. Aryle, hétéroaryle et tétrahydroisoquinolines à hétérocycle substitué et leur utilisation
AU2010247763B2 (en) 2009-05-12 2015-12-24 Albany Molecular Research, Inc. 7-([1,2,4,]triazolo[1,5,-a]pyridin-6-yl)-4-(3,4-dichlorophenyl)-1,2,3,4- tetrahydroisoquinoline and use thereof
AU2010247735B2 (en) 2009-05-12 2015-07-16 Albany Molecular Research, Inc. Crystalline forms of (S)-7-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-4-(3,4-dichlorophenyl)- 1,2,3,4-tetrahydroisoquinoline and use thereof
PE20121172A1 (es) 2009-10-14 2012-09-05 Merck Sharp & Dohme Piperidinas sustituidas con actividad en la hdm2
SG184324A1 (en) 2010-03-31 2012-11-29 Gilead Pharmasset Llc Nucleoside phosphoramidates
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
EP3330377A1 (fr) 2010-08-02 2018-06-06 Sirna Therapeutics, Inc. Inhibition à médiation par interférence arn de caténine (protéine associée à cadhérine), expression du gène bêta 1 (ctnnb1) à l'aide de petit acide nucléique interférent (sian)
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.
US9029341B2 (en) 2010-08-17 2015-05-12 Sirna Therapeutics, Inc. 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
EP2613782B1 (fr) 2010-09-01 2016-11-02 Merck Sharp & Dohme Corp. Dérivés d'indazole utilisables en tant qu'inhibiteurs de la voie erk
US9242981B2 (en) 2010-09-16 2016-01-26 Merck Sharp & Dohme Corp. Fused pyrazole derivatives as novel ERK inhibitors
BR112013006651A2 (pt) 2010-09-23 2017-07-18 Nuformix Ltd composição e cocristal de aprepitante l-prolina
WO2012058210A1 (fr) 2010-10-29 2012-05-03 Merck Sharp & Dohme Corp. INHIBITION FACILITÉE PAR L'INTERFÉRENCE D'ARN DE L'EXPRESSION D'UN GÈNE AU MOYEN D'ACIDES NUCLÉIQUES INTERFÉRENTS COURTS (siNA)
WO2012087772A1 (fr) 2010-12-21 2012-06-28 Schering Corporation Dérivés d'indazole utiles en tant qu'inhibiteurs de erk
AU2012245971A1 (en) 2011-04-21 2013-10-17 Piramal Enterprises Limited A crystalline form of a salt of a morpholino sulfonyl indole derivative and a process for its preparation
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
CN108640910A (zh) 2011-11-25 2018-10-12 诺弗米克斯技术有限公司 阿瑞吡坦l-脯氨酸溶剂化物-组合物和共晶体
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
US20150299696A1 (en) 2012-05-02 2015-10-22 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
RS56680B1 (sr) 2012-11-28 2018-03-30 Merck Sharp & Dohme Kompozicije i postupci za lečenje kancera
KR102196882B1 (ko) 2012-12-20 2020-12-30 머크 샤프 앤드 돔 코포레이션 Hdm2 억제제로서의 치환된 이미다조피리딘
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
CA3025837C (fr) 2016-06-06 2024-02-13 Helsinn Healthcare Sa Formulations injectables physiologiquement equilibrees de fosnetupitant
EP3525785B1 (fr) 2016-10-12 2025-08-27 Merck Sharp & Dohme LLC Inhibiteurs de kdm5
US10947234B2 (en) 2017-11-08 2021-03-16 Merck Sharp & Dohme Corp. PRMT5 inhibitors
EP3706747B1 (fr) 2017-11-08 2025-09-03 Merck Sharp & Dohme LLC Inhibiteurs de prmt5
EP3833668B1 (fr) 2018-08-07 2025-03-19 Merck Sharp & Dohme LLC Inhibiteurs de prmt5
US12173026B2 (en) 2018-08-07 2024-12-24 Merck Sharp & Dohme Llc PRMT5 inhibitors
US11981701B2 (en) 2018-08-07 2024-05-14 Merck Sharp & Dohme Llc PRMT5 inhibitors
CA3173697A1 (fr) 2020-04-03 2021-10-07 Mike TROWER Antagoniste du recepteur de nk-1 pour le traitement d'une maladie choisie parmi une septicemie, un choc septique, un syndrome de detresse respiratoire aigue (ards) ou un syndrome de dysfonctionnement des organes multiples (mods
CA3177477A1 (fr) 2020-06-02 2021-12-09 Nerre Therapeutics Limited Antagonistes du recepteur de la neurokinine (nk)-1 destines a etre utilises dans le traitement d'etats de fibrose pulmonaire favorises par une lesion mecanique des poumons

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
EP0600952B1 (fr) * 1991-08-20 1996-04-17 MERCK SHARP & DOHME LTD. Composes azacycliques, procedes de preparation 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
ATE166867T1 (de) * 1993-02-18 1998-06-15 Merck Sharp & Dohme Azacyclische verbindungen, sie enthaltende zusammensetzungen und ihre verwendung als tachykinin antagoniste

Also Published As

Publication number Publication date
JP3245424B2 (ja) 2002-01-15
NO308742B1 (no) 2000-10-23
NL300146I1 (nl) 2004-06-01
KR960706483A (ko) 1996-12-09
TW419471B (en) 2001-01-21
CA2178949A1 (fr) 1995-06-22
NO2018011I1 (no) 2018-04-04
NO2004003I2 (no) 2006-10-04
IL111960A (en) 1999-12-22
EP0734381B1 (fr) 2000-07-05
SK282800B6 (sk) 2002-12-03
ES2147840T3 (es) 2000-10-01
JPH09506628A (ja) 1997-06-30
SI0734381T1 (en) 2000-10-31
FI962489A7 (fi) 1996-08-13
HUT76476A (en) 1997-09-29
EP0734381A1 (fr) 1996-10-02
FI109532B (fi) 2002-08-30
CA2178949C (fr) 2006-03-21
ATE194336T1 (de) 2000-07-15
MY115164A (en) 2003-04-30
LV11617A (lv) 1996-12-20
NO962523D0 (no) 1996-06-14
DE122004000019I1 (de) 2004-09-30
YU74694A (sh) 1997-08-22
DE69425161D1 (de) 2000-08-10
HK1009046A1 (en) 1999-05-21
CY2203B1 (en) 2002-11-08
ZA9410008B (en) 1996-07-15
CY2004012I1 (el) 2010-07-28
CZ295381B6 (cs) 2005-07-13
LTPA2004002I1 (lt) 2016-11-10
BR9408351A (pt) 1997-08-26
NO2018011I2 (no) 2018-12-14
CO4340628A1 (es) 1996-07-30
FR04C0010I1 (fr) 2004-05-21
BG100715A (bg) 1997-01-31
NZ278222A (en) 1998-05-27
CN1142819A (zh) 1997-02-12
NO962523L (no) 1996-08-16
HU9601634D0 (en) 1996-08-28
HRP941000A2 (en) 1997-06-30
NL300146I2 (nl) 2004-07-01
SK75396A3 (en) 1996-12-04
FR04C0010I2 (fr) 2004-12-17
HRP941000B1 (en) 2001-04-30
PL315153A1 (en) 1996-10-14
HU224014B1 (hu) 2005-04-28
UA47397C2 (uk) 2002-07-15
DE69425161T2 (de) 2001-02-15
IL111960A0 (en) 1995-03-15
CY2004012I2 (el) 2017-04-05
RO118203B1 (ro) 2003-03-28
LV11617B (en) 1997-04-20
FI962489A0 (fi) 1996-06-14
PL182521B1 (pl) 2002-01-31
KR100335704B1 (ko) 2002-11-18
LU91069I2 (fr) 2004-04-07
LTC0734381I2 (lt) 2017-04-25
YU49037B (sh) 2003-07-07
DK0734381T3 (da) 2000-09-18
PT734381E (pt) 2000-12-29
BG64775B1 (bg) 2006-03-31
GR3034095T3 (en) 2000-11-30
HRP941000B9 (hr) 2014-11-07
SA95150523B1 (ar) 2006-03-15
CZ177296A3 (en) 1996-12-11
RU2201924C2 (ru) 2003-04-10
NO2004003I1 (no) 2004-06-28
AU1437595A (en) 1995-07-03
CN1057296C (zh) 2000-10-11
AU701862B2 (en) 1999-02-04
WO1995016679A1 (fr) 1995-06-22

Similar Documents

Publication Publication Date Title
LU91069I9 (en) Morpholine tachykinin receptor antagonists
AU4656193A (en) Morpholine and thiomorpholine tachykinin receptor antagonists
CA2237189A1 (fr) 3-azetidinylalkylpiperidines ou -pyrrolidines en tant qu'antagonistes des tachykinines
WO1999062893A3 (fr) Nouveaux antagonistes de la neurokinine, leur procede de production et compositions pharmaceutiques contenant ces composes
DE69402703D1 (de) 3-(INDOL-3-YL) PROPENSäURDERIVATE, DIE ALS NMDA- ANTAGONISTEN NÜTZLICH SIND
AU2002210537A1 (en) (4-acylaminopiperidin-1-yl) acetamides as neurokinin antagonists