AU701862B2 - Morpholine and thiomorpholine tachykinin receptor antagonists - Google Patents

Morpholine and thiomorpholine tachykinin receptor antagonists Download PDF

Info

Publication number
AU701862B2
AU701862B2 AU14375/95A AU1437595A AU701862B2 AU 701862 B2 AU701862 B2 AU 701862B2 AU 14375/95 A AU14375/95 A AU 14375/95A AU 1437595 A AU1437595 A AU 1437595A AU 701862 B2 AU701862 B2 AU 701862B2
Authority
AU
Australia
Prior art keywords
phenyl
morpholine
ethoxy
defined above
oxo
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, expires
Application number
AU14375/95A
Other languages
English (en)
Other versions
AU1437595A (en
Inventor
Mark Stuart Chambers
Conrad P. Dorn
Paul E. Finke
Jeffrey J. Hale
Timothy Harrison
Tamara Ladduwahetty
Malcolm Maccoss
Sander G. Mills
Shrenik K. Shah
Brian John Williams
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 Sharp and Dohme LLC
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=AU701862(B2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from AU41568/93A external-priority patent/AU663595C/en
Priority claimed from AU46561/93A external-priority patent/AU4656193A/en
Application filed by Merck and Co Inc filed Critical Merck and Co Inc
Publication of AU1437595A publication Critical patent/AU1437595A/en
Application granted granted Critical
Publication of AU701862B2 publication Critical patent/AU701862B2/en
Assigned to MERCK SHARP & DOHME CORP. reassignment MERCK SHARP & DOHME CORP. Request to Amend Deed and Register Assignors: MERCK & CO., INC.
Assigned to MERCK SHARP & DOHME CORP. reassignment MERCK SHARP & DOHME CORP. Request to Amend Deed and Register Assignors: MERCK SHARP & DOHME CORP.
Adjusted expiration legal-status Critical
Expired legal-status Critical Current

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)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (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)
AU14375/95A 1992-06-29 1994-12-13 Morpholine and thiomorpholine tachykinin receptor antagonists Expired AU701862B2 (en)

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
US905976 1992-06-29
US971448 1992-11-04
US061914 1993-05-19
AU41568/93A AU663595C (en) 1992-06-29 1993-06-28 Morpholine and thiomorpholine tachykinin receptor antagonists
AU46561/93A AU4656193A (en) 1992-06-29 1993-06-29 Morpholine and thiomorpholine tachykinin receptor antagonists
US16988993A 1993-12-17 1993-12-17
US169889 1993-12-17
PCT/US1994/014497 WO1995016679A1 (en) 1993-12-17 1994-12-13 Morpholine and thiomorpholine tachykinin receptor antagonists

Related Parent Applications (2)

Application Number Title Priority Date Filing Date
AU41568/93A Division AU663595C (en) 1992-06-29 1993-06-28 Morpholine and thiomorpholine tachykinin receptor antagonists
AU46561/93A Division AU4656193A (en) 1992-06-29 1993-06-29 Morpholine and thiomorpholine tachykinin receptor antagonists

Publications (2)

Publication Number Publication Date
AU1437595A AU1437595A (en) 1995-07-03
AU701862B2 true AU701862B2 (en) 1999-02-04

Family

ID=22617632

Family Applications (1)

Application Number Title Priority Date Filing Date
AU14375/95A Expired AU701862B2 (en) 1992-06-29 1994-12-13 Morpholine and thiomorpholine tachykinin receptor antagonists

Country Status (40)

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

Families Citing this family (109)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2131426C1 (ru) * 1993-12-29 1999-06-10 Мерк Шарп Энд Домэ Лимитед Замещенные производные морфолина, способ их получения, фармацевтическая композиция на их основе, способ снижения количества тахикининов при лечении или профилактике физиологических состояний, ассоциируемых с избытком тахикининов
IL112778A0 (en) * 1994-03-04 1995-05-26 Merck & Co Inc Substituted heterocycles, their preparation and pharmaceutical compositions containing them
US5747491A (en) * 1994-05-05 1998-05-05 Merck Sharp & Dohme Ltd. Morpholine derivatives and their use as antagonists of tachikinins
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
ZA985765B (en) 1997-07-02 1999-08-04 Merck & Co Inc Polymorphic form of a tachykinin receptor antagonist.
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
GB9813025D0 (en) * 1998-06-16 1998-08-12 Merck Sharp & Dohme Chemical synthesis
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.
PL350427A1 (en) 1999-02-24 2002-12-16 Hoffmann La Roche Phenyl− and pyridinyl derivatives as neurokinin 1 antagonists
CA2364662C (en) 1999-02-24 2009-10-20 F. Hoffmann-La Roche Ag 3-phenylpyridine derivatives and their use as nk-1 receptor antagonists
US6291465B1 (en) 1999-03-09 2001-09-18 Hoffmann-La Roche Inc. Biphenyl derivatives
ATE387429T1 (de) 1999-11-03 2008-03-15 Amr Technology Inc Arly- und heteroaryl-substituierte tetrahydroisoquinoline und ihre verwendung als hemmer der wiederaufnahme von norepinephrin, dopamin und 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
EP1299393A2 (en) 2000-07-11 2003-04-09 Bristol-Myers Squibb Pharma Company 4-phenyl substituted tetrahydroisoquinolines and therapeutic use thereof
IL153834A0 (en) 2000-07-14 2003-07-31 Hoffmann La Roche N-oxides as nk1 receptor antagonist prodrugs of 4-phenyl-pyridine derivatives
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
KR100618063B1 (ko) * 2001-05-14 2006-08-30 에프. 호프만-라 로슈 아게 1-옥사-3,9-디아자-스피로[5.5]운데칸-2-온 유도체, 및 이의 뉴로키닌 수용체 길항제로서의 용도
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
NZ532993A (en) * 2001-12-07 2006-09-29 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
KR100700421B1 (ko) * 2003-01-31 2007-03-28 에프. 호프만-라 로슈 아게 2-(3,5-비스-트라이플루오로메틸-페닐)-Ｎ-[6-(1,1-다이옥소-1λ6-티오모폴린-4-일)-4-(4-플루오로-2-메틸-페닐)-피리딘-3-일]-Ｎ-메틸-아이소부티르아미드의 새로운 결정변형체
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.
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.
CN101119969B (zh) 2004-07-15 2014-04-09 阿尔巴尼分子研究公司 芳基和杂芳基取代的四氢异喹啉及其阻断去甲肾上腺素、多巴胺和血清素的重摄取的应用
BRPI0606843A2 (pt) 2005-02-22 2009-07-21 Hoffmann La Roche antagonistas de nk 1
PT1863767E (pt) 2005-03-23 2009-03-27 Hoffmann La Roche Metabolitos para antagonistas de nk-1 para vómitos
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
BRPI0613403A2 (pt) 2005-07-15 2009-02-10 Amr Technology Inc tetrahidrobenzodiazepinas aril- e heteroarila-substituÍdas e uso das mesmas para bloquear a recaptaÇço de norepinefrina, dopamina e serotonina
AU2006298898B2 (en) 2005-09-23 2011-06-30 F. Hoffmann-La Roche Ag Novel dosage formulation
AU2006297443B2 (en) 2005-09-29 2010-08-12 Merck Sharp & Dohme Corp. Acylated spiropiperidine derivatives as melanocortin-4 receptor modulators
US8133994B2 (en) 2005-10-06 2012-03-13 Dr. Reddy's Laboratories Ltd. Preparation of aprepitant
CA2640966A1 (en) * 2006-02-03 2007-08-09 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
EP2057151A4 (en) * 2006-08-28 2010-07-21 Hetero Drugs Ltd PROCESS FOR PURIFYING APREPITANT
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
RS58936B1 (sr) 2007-01-10 2019-08-30 Msd Italia Srl Indazoli supstituisani amidom kao inhibitori poli(adp-riboza)polimeraze (parp)
JP2010516731A (ja) 2007-01-24 2010-05-20 グラクソ グループ リミテッド ２−メトキシ−５−（５−トリフルオロメチル−テトラゾール−１−イル）−ベンジル］−（２ｓ−フェニル−ピペリジン−３ｓ−イル）−アミンを含む医薬組成物
EP2145884B1 (en) 2007-04-02 2014-08-06 Msd K.K. Indoledione derivative
DE602008001983D1 (de) 2007-04-20 2010-09-09 Hoffmann La Roche Pyrrolidinderivate als doppelte nk1/nk3-rezeptorenantagonisten
JP5501227B2 (ja) 2007-06-27 2014-05-21 メルク・シャープ・アンド・ドーム・コーポレーション ヒストンデアセチラーゼ阻害剤としての４−カルボキシベンジルアミノ誘導体
EP2185540B1 (en) 2007-08-07 2011-07-20 F. Hoffmann-La Roche AG Pyrrolidine aryl-ether as nk3 receptor antagonists
WO2009104080A2 (en) 2008-02-20 2009-08-27 Targia Pharmaceuticals Cns pharmaceutical compositions and methods of use
JP2011515343A (ja) 2008-03-03 2011-05-19 タイガー ファーマテック チロシンキナーゼ阻害薬
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
SG172363A1 (en) 2008-12-23 2011-07-28 Pharmasset Inc Synthesis of purine nucleosides
WO2010075549A2 (en) 2008-12-23 2010-07-01 Pharmasset, Inc. Nucleoside phosphoramidates
NZ617066A (en) 2008-12-23 2015-02-27 Gilead Pharmasset Llc Nucleoside analogs
US8691825B2 (en) 2009-04-01 2014-04-08 Merck Sharp & Dohme Corp. Inhibitors of AKT activity
US8815894B2 (en) 2009-05-12 2014-08-26 Bristol-Myers Squibb Company 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
CA2760837C (en) 2009-05-12 2018-04-03 Albany Molecular Research, Inc. 7-([1,2,4]triazolo[1,5-.alpha.]pyridin-6-yl)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydroisoquinoline and use thereof
ES2446971T3 (es) 2009-05-12 2014-03-11 Albany Molecular Research, Inc. Tetrahidroisoquinolinas sustituidas con arilo, heteroarilo, y heterociclo y su uso
MX2012004377A (es) 2009-10-14 2012-06-01 Merck Sharp & Dohme Piperidinas sustituidas que aumentan la actividad de p53 y sus usos.
ES2516466T3 (es) 2010-03-31 2014-10-30 Gilead Pharmasset Llc Síntesis estereoselectiva de agentes activos que contienen fósforo
US8487102B2 (en) 2010-04-20 2013-07-16 Hoffmann-La Roche Inc. Pyrrazolopyridine compounds as dual NK1/NK3 receptor antagonists
WO2011163330A1 (en) 2010-06-24 2011-12-29 Merck Sharp & Dohme Corp. Novel heterocyclic compounds as erk inhibitors
US8518907B2 (en) 2010-08-02 2013-08-27 Merck Sharp & Dohme Corp. RNA interference mediated inhibition of catenin (cadherin-associated protein), beta 1 (CTNNB1) gene expression using short interfering nucleic acid (siNA)
ES2376564B1 (es) 2010-08-12 2013-01-24 Manuel Vicente Salinas Martín Utilización de anticuerpos contra los receptores nk1, nk2 y/o nk3, para producir apoptosis en las células tumorales y modificar el estroma, la inmunidad y la vascularización intra y peritumorales, como tratamiento del cáncer.
RU2624045C2 (ru) 2010-08-17 2017-06-30 Сирна Терапьютикс,Инк ОПОСРЕДУЕМОЕ РНК-ИНТЕРФЕРЕНЦИЕЙ ИНГИБИРОВАНИЕ ЭКСПРЕССИИ ГЕНОВ ВИРУСА ГЕПАТИТА B (HBV) С ПРИМЕНЕНИЕМ МАЛОЙ ИНТЕРФЕРИРУЮЩЕЙ НУКЛЕИНОВОЙ КИСЛОТЫ (миНК)
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
EP2615916B1 (en) 2010-09-16 2017-01-04 Merck Sharp & Dohme Corp. Fused pyrazole derivatives as novel erk inhibitors
KR101833578B1 (ko) 2010-09-23 2018-02-28 누포믹스 리미티드 아프레피탄트 l-프롤린 조성물 및 공결정
EP2632472B1 (en) 2010-10-29 2017-12-13 Sirna Therapeutics, Inc. Rna interference mediated inhibition of gene expression using short interfering nucleic acids (sina)
EP2654748B1 (en) 2010-12-21 2016-07-27 Merck Sharp & Dohme Corp. Indazole derivatives useful as erk inhibitors
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 (en) 2011-04-29 2012-11-01 Sandoz Ag Novel intermediates for the preparation of highly pure aprepitant or fosaprepitant
EP2770987B1 (en) 2011-10-27 2018-04-04 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
US9532993B2 (en) 2011-11-25 2017-01-03 Nuformix Limited Aprepitant L-proline solvates—compositions and cocrystals
EP2837381A4 (en) 2011-12-13 2015-12-09 Servicio Andaluz De Salud USE OF MEDICAMENTS FOR THE TREATMENT OF CANCER THAT CHANGE THE PERITUMORAL ENVIRONMENT
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
WO2013165816A2 (en) 2012-05-02 2013-11-07 Merck Sharp & Dohme Corp. SHORT INTERFERING NUCLEIC ACID (siNA) COMPOSITIONS
MX2015004041A (es) 2012-09-28 2015-07-06 Merck Sharp & Dohme Compuestos novedosos que son inhibidores de erk.
ES2651347T3 (es) 2012-11-28 2018-01-25 Merck Sharp & Dohme Corp. Composiciones y métodos para el tratamiento del cáncer
CN105073746B (zh) 2012-12-20 2017-03-22 默沙东公司 作为hdm2抑制剂的取代的咪唑并吡啶
EP2951180B1 (en) 2013-01-30 2018-05-02 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
WO2015034925A1 (en) 2013-09-03 2015-03-12 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
ES2771226T3 (es) 2016-06-06 2020-07-06 Helsinn Healthcare Sa Formulaciones inyectables de fosnetupitante fisiológicamente equilibrados
US10975084B2 (en) 2016-10-12 2021-04-13 Merck Sharp & Dohme Corp. KDM5 inhibitors
EP3706742B1 (en) 2017-11-08 2023-03-15 Merck Sharp & Dohme LLC Prmt5 inhibitors
US11098059B2 (en) 2017-11-08 2021-08-24 Merck Sharp & Dohme Corp. PRMT5 inhibitors
EP3833667B1 (en) 2018-08-07 2024-03-13 Merck Sharp & Dohme LLC Prmt5 inhibitors
EP3833668B1 (en) 2018-08-07 2025-03-19 Merck Sharp & Dohme LLC Prmt5 inhibitors
US12173026B2 (en) 2018-08-07 2024-12-24 Merck Sharp & Dohme Llc PRMT5 inhibitors
IL296635A (en) 2020-04-03 2022-11-01 Nerre Therapeutics Ltd An nk-1 receptor antagonist for the treatment of a disease selected from sepsis, septic shock, acute respiratory distress syndrome (ARDS), or multiple organ dysfunction syndrome (MODS)
CN115697332A (zh) 2020-06-02 2023-02-03 尼尔医疗有限公司 用于治疗由肺的机械损伤促进的肺纤维化状况的神经激肽(nk)-1受体拮抗剂

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU4156893A (en) * 1992-06-29 1994-01-06 Merck Sharp & Dohme Corp. Morpholine and thiomorpholine tachykinin receptor antagonists

Family Cites Families (3)

* 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
US5459270A (en) * 1991-08-20 1995-10-17 Merck Sharp & Dohme Limited Azacyclic compounds, processes for their preparation and pharmaceutical compositions containing them
AU679207B2 (en) * 1993-02-18 1997-06-26 Merck Sharp & Dohme Limited Azacyclic compounds, compositions containing them and their use as tachykinin antagonists

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU4156893A (en) * 1992-06-29 1994-01-06 Merck Sharp & Dohme Corp. Morpholine and thiomorpholine tachykinin receptor antagonists
AU4656193A (en) * 1992-06-29 1994-01-24 Merck & Co., Inc. Morpholine and thiomorpholine tachykinin receptor antagonists

Also Published As

Publication number Publication date
HUT76476A (en) 1997-09-29
RU2201924C2 (ru) 2003-04-10
NO2018011I1 (no) 2018-04-04
BG64775B1 (bg) 2006-03-31
LV11617A (lv) 1996-12-20
HRP941000B9 (hr) 2014-11-07
SA95150523B1 (ar) 2006-03-15
FR04C0010I1 (Direct) 2004-05-21
CY2203B1 (en) 2002-11-08
DE69425161D1 (de) 2000-08-10
NO962523D0 (no) 1996-06-14
AU1437595A (en) 1995-07-03
CA2178949A1 (en) 1995-06-22
FI109532B (fi) 2002-08-30
LTC0734381I2 (lt) 2017-04-25
DE69425161T2 (de) 2001-02-15
JP3245424B2 (ja) 2002-01-15
KR100335704B1 (ko) 2002-11-18
SI0734381T1 (en) 2000-10-31
YU74694A (sh) 1997-08-22
CY2004012I2 (el) 2017-04-05
SK282800B6 (sk) 2002-12-03
NO308742B1 (no) 2000-10-23
LU91069I2 (fr) 2004-04-07
DE122004000019I1 (de) 2004-09-30
TW419471B (en) 2001-01-21
HRP941000B1 (en) 2001-04-30
CN1142819A (zh) 1997-02-12
IL111960A (en) 1999-12-22
CO4340628A1 (es) 1996-07-30
PL315153A1 (en) 1996-10-14
NO962523L (no) 1996-08-16
PL182521B1 (pl) 2002-01-31
SK75396A3 (en) 1996-12-04
NZ278222A (en) 1998-05-27
FR04C0010I2 (fr) 2004-12-17
KR960706483A (ko) 1996-12-09
CN1057296C (zh) 2000-10-11
WO1995016679A1 (en) 1995-06-22
UA47397C2 (uk) 2002-07-15
JPH09506628A (ja) 1997-06-30
HU9601634D0 (en) 1996-08-28
GR3034095T3 (en) 2000-11-30
FI962489A0 (fi) 1996-06-14
HU224014B1 (hu) 2005-04-28
CZ177296A3 (en) 1996-12-11
NO2004003I2 (no) 2006-10-04
NL300146I2 (nl) 2004-07-01
LV11617B (en) 1997-04-20
ZA9410008B (en) 1996-07-15
LU91069I9 (en) 2018-07-24
YU49037B (sh) 2003-07-07
LTPA2004002I1 (lt) 2016-11-10
RO118203B1 (ro) 2003-03-28
NO2004003I1 (no) 2004-06-28
EP0734381A1 (en) 1996-10-02
CZ295381B6 (cs) 2005-07-13
CY2004012I1 (el) 2010-07-28
HRP941000A2 (en) 1997-06-30
HK1009046A1 (en) 1999-05-21
BR9408351A (pt) 1997-08-26
BG100715A (bg) 1997-01-31
CA2178949C (en) 2006-03-21
MY115164A (en) 2003-04-30
IL111960A0 (en) 1995-03-15
NO2018011I2 (no) 2018-12-14
FI962489A7 (fi) 1996-08-13
ES2147840T3 (es) 2000-10-01
ATE194336T1 (de) 2000-07-15
DK0734381T3 (da) 2000-09-18
PT734381E (pt) 2000-12-29
NL300146I1 (nl) 2004-06-01
EP0734381B1 (en) 2000-07-05

Similar Documents

Publication Publication Date Title
AU701862B2 (en) Morpholine and thiomorpholine tachykinin receptor antagonists
US5922706A (en) Morpholine and thiomorpholine tachykinin receptor antagonists
EP0577394B1 (en) Morpholine and thiomorpholine tachykinin receptor antagonists
US5637699A (en) Process for preparing morpholine tachykinin receptor antagonists
US5716942A (en) Treatment of migraine with morpholine tachykinin receptor antagonists
US6048859A (en) Morpholine and thiomorpholine tachykinin receptor antagonists
HK1009046B (en) Morpholine tachykinin receptor antagonists
HK1009268B (en) Morpholine and thiomorpholine tachykinin receptor antagonists

Legal Events

Date Code Title Description
NC Extension of term for standard patent requested (sect. 70)

Free format text: PRODUCT NAME: EMEND APREPITANT

MK14 Patent ceased section 143(a) (annual fees not paid) or expired