ATE372991T1 - Polymorphe form des tachykininrezeptorantagonisten 2-(r)-(1-(r)-(3,5- bis(trifluormethyl)phenyl)ethoxy)-3-(s)-(4- fluor)phenyl-4-(3-5-oxo-1h,4h-1,2,4- triazolo)methylmorpholin - Google Patents

Polymorphe form des tachykininrezeptorantagonisten 2-(r)-(1-(r)-(3,5- bis(trifluormethyl)phenyl)ethoxy)-3-(s)-(4- fluor)phenyl-4-(3-5-oxo-1h,4h-1,2,4- triazolo)methylmorpholin

Info

Publication number
ATE372991T1
ATE372991T1 AT98933088T AT98933088T ATE372991T1 AT E372991 T1 ATE372991 T1 AT E372991T1 AT 98933088 T AT98933088 T AT 98933088T AT 98933088 T AT98933088 T AT 98933088T AT E372991 T1 ATE372991 T1 AT E372991T1
Authority
AT
Austria
Prior art keywords
phenyl
triazolo
methylmorpholine
oxo
trifluoromethyl
Prior art date
Application number
AT98933088T
Other languages
English (en)
Inventor
Louis Crocker
James Mccauley
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
Priority claimed from GBGB9800216.5A external-priority patent/GB9800216D0/en
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Application granted granted Critical
Publication of ATE372991T1 publication Critical patent/ATE372991T1/de

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
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Otolaryngology (AREA)
  • Rheumatology (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)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Polyamides (AREA)
  • Polyurethanes Or Polyureas (AREA)
AT98933088T 1997-07-02 1998-07-01 Polymorphe form des tachykininrezeptorantagonisten 2-(r)-(1-(r)-(3,5- bis(trifluormethyl)phenyl)ethoxy)-3-(s)-(4- fluor)phenyl-4-(3-5-oxo-1h,4h-1,2,4- triazolo)methylmorpholin ATE372991T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US5160097P 1997-07-02 1997-07-02
GBGB9800216.5A GB9800216D0 (en) 1998-01-07 1998-01-07 Polymorphic form of a tachykinin receptor antagonist

Publications (1)

Publication Number Publication Date
ATE372991T1 true ATE372991T1 (de) 2007-09-15

Family

ID=26312895

Family Applications (1)

Application Number Title Priority Date Filing Date
AT98933088T ATE372991T1 (de) 1997-07-02 1998-07-01 Polymorphe form des tachykininrezeptorantagonisten 2-(r)-(1-(r)-(3,5- bis(trifluormethyl)phenyl)ethoxy)-3-(s)-(4- fluor)phenyl-4-(3-5-oxo-1h,4h-1,2,4- triazolo)methylmorpholin

Country Status (26)

Country Link
EP (1) EP0994867B1 (de)
JP (1) JP2000513383A (de)
KR (1) KR20010020593A (de)
CN (1) CN1106390C (de)
AT (1) ATE372991T1 (de)
AU (1) AU735230B2 (de)
BG (1) BG64703B1 (de)
CA (1) CA2293836C (de)
CZ (1) CZ295410B6 (de)
DE (1) DE69838421D1 (de)
DZ (1) DZ2551A1 (de)
EA (1) EA002405B1 (de)
EE (1) EE04152B1 (de)
HR (1) HRP980370B1 (de)
HU (1) HU228003B1 (de)
ID (1) ID23191A (de)
IL (1) IL133357A (de)
IS (1) IS2617B (de)
NO (1) NO316893B1 (de)
NZ (1) NZ501589A (de)
PE (1) PE86499A1 (de)
PL (1) PL191496B1 (de)
SK (1) SK285644B6 (de)
TR (1) TR199903299T2 (de)
TW (1) TW577887B (de)
WO (1) WO1999001444A1 (de)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU1343901A (en) 1999-10-29 2001-05-14 Merck & Co., Inc. Polymorphic form of a tachykinin receptor antagonist
GB0203061D0 (en) * 2002-02-08 2002-03-27 Novartis Ag Organic compounds
JP2005529933A (ja) * 2002-05-31 2005-10-06 シェーリング　コーポレイション キサンチンホスホジエステラーゼｖインヒビター多形体
GB0417702D0 (en) * 2004-08-09 2004-09-08 Merck Sharp & Dohme New uses
WO2007039883A2 (en) 2005-10-05 2007-04-12 Ranbaxy Laboratories Limited Process for preparation of aprepitant
EP1984359A1 (de) * 2006-02-03 2008-10-29 Glenmark Pharmaceuticals Limited Amorphe und kristalline formen von aprepitant und verfahren zu deren herstellung
HUE028908T2 (en) 2006-04-05 2017-01-30 Opko Health Inc The hydrochloride salt of 8 - [{1- (3,5-bis (trifluoromethyl) phenyl) ethoxy} methyl] -8-phenyl-1,7-diazaspiro [4.5] decan-2-one, and process
EP2057151A4 (de) * 2006-08-28 2010-07-21 Hetero Drugs Ltd Verfahren zur reinigung von aprepitant
WO2008044102A1 (en) * 2006-10-13 2008-04-17 Glenmark Pharmaceuticals Limited Polymorph form of aprepitant and process for the preparation thereof
EP2117538A1 (de) 2007-01-24 2009-11-18 Glaxo Group Limited Pharmazeutische zusammensetzungen mit 2-methoxy-5- (5-trifluoromethyl-tetrazol-i-yl-benzyl) - (2s-phenyl-piperidin-3s-yl-)
ES2665042T3 (es) * 2008-02-18 2018-04-24 Laboratorios Del Dr. Esteve, S.A. Uso de compuestos que se unen a ligandos del receptor sigma para el tratamiento del dolor neuropático que se desarrolla como consecuencia de la quimioterapia
EP2116539A1 (de) 2008-04-25 2009-11-11 Laboratorios Del. Dr. Esteve, S.A. 1-Aryl-3-Amino-alkoxy-pyrazole als Sigma-Liganden zur Verbesserung der analgetischen Wirkung von Opioiden und zur Schwächung der Abhängigkeit davon
EP2353598A1 (de) 2010-02-04 2011-08-10 Laboratorios Del. Dr. Esteve, S.A. Sigma-Liganden zur Anwendung in der Vorbeugung und/oder Behandlung von postoperativem Schmerz
EP2353591A1 (de) 2010-02-04 2011-08-10 Laboratorios Del. Dr. Esteve, S.A. Sigma-Liganden zur Verstärkung der analgesischen Wirkung von Opioden und Opiaten bei postoperativem Schmerz und zur Schwächung der Abhängigkeit davon
EP2388005A1 (de) 2010-05-21 2011-11-23 Laboratorios Del. Dr. Esteve, S.A. Sigma-Liganden zur Vorbeugung und/oder Behandlung von Erbrechen infolge von Chemotherapie oder Strahlentherapie
EP2415471A1 (de) 2010-08-03 2012-02-08 Laboratorios Del. Dr. Esteve, S.A. Verwendung von Sigmaliganden bei opioidinduzierter Hyperalgesie
EP2524694A1 (de) 2011-05-19 2012-11-21 Laboratorios Del. Dr. Esteve, S.A. Verwendung von Sigmaliganden bei Schmerz im Zusammenhang mit Typ-2-Diabetes
CA2837453C (en) 2011-06-30 2017-04-11 Toray Industries, Inc. Crystals of glycine derivative and pharmaceutical use thereof
CN103030668B (zh) * 2011-10-09 2016-06-15 江苏豪森药业集团有限公司 一种制备福沙匹坦二甲葡胺的方法
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
CN102850339B (zh) * 2012-10-17 2014-10-15 上海博志研新药物技术有限公司 一种神经激肽(nk-1)受体拮抗剂晶型制备方法
CN103288813A (zh) * 2013-06-04 2013-09-11 四川百利药业有限责任公司 一种阿瑞匹坦的制备方法
TN2016000228A1 (en) 2013-12-17 2017-10-06 Esteve Labor Dr SEROTONIN-NOREPINEPHRINE REUPTAKE INHIBITORS (SNRIs) AND SIGMA RECEPTOR LIGANDS COMBINATIONS.
CN104119325B (zh) * 2014-07-15 2017-03-22 中山奕安泰医药科技有限公司 阿瑞吡坦多晶型物的制备方法
CN105837526B (zh) * 2016-01-22 2018-02-27 浙江工业大学 一种阿瑞吡坦重要合成中间体(2s,3r)‑4‑苄基‑3‑(4‑氟苯基)吗啉‑2‑醇的制备方法

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL111960A (en) * 1993-12-17 1999-12-22 Merck & Co Inc Morpholines and thiomorpholines their preparation and pharmaceutical compositions containing them

Also Published As

Publication number Publication date
EE04152B1 (et) 2003-10-15
TW577887B (en) 2004-03-01
AU8283398A (en) 1999-01-25
ID23191A (id) 2000-03-23
IL133357A (en) 2003-12-10
WO1999001444A1 (en) 1999-01-14
AU735230B2 (en) 2001-07-05
DE69838421D1 (en) 2007-10-25
IL133357A0 (en) 2001-04-30
HK1029345A1 (en) 2001-03-30
HRP980370B1 (en) 2002-10-31
JP2000513383A (ja) 2000-10-10
EA199901114A1 (ru) 2000-08-28
EE9900603A (et) 2000-08-15
EA002405B1 (ru) 2002-04-25
IS2617B (is) 2010-04-15
CZ295410B6 (cs) 2005-08-17
HUP0004008A2 (hu) 2002-02-28
SK285644B6 (sk) 2007-05-03
CA2293836A1 (en) 1999-01-14
TR199903299T2 (xx) 2000-07-21
CN1261882A (zh) 2000-08-02
KR20010020593A (ko) 2001-03-15
NZ501589A (en) 2001-10-26
DZ2551A1 (fr) 2003-08-15
HUP0004008A3 (en) 2002-03-28
BG104010A (en) 2001-08-31
IS5293A (is) 1999-12-10
NO996549D0 (no) 1999-12-29
HU228003B1 (en) 2012-08-28
HRP980370A2 (en) 1999-04-30
CN1106390C (zh) 2003-04-23
PL191496B1 (pl) 2006-05-31
NO996549L (no) 2000-03-01
SK187299A3 (en) 2000-07-11
NO316893B1 (no) 2004-06-14
CZ477799A3 (cs) 2000-09-13
EP0994867B1 (de) 2007-09-12
BG64703B1 (bg) 2005-12-30
PL337579A1 (en) 2000-08-28
CA2293836C (en) 2007-06-05
EP0994867A1 (de) 2000-04-26
PE86499A1 (es) 1999-10-25

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