IL133357A - Polymorphic form of the tachykinin receptor antagonist 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 - Google Patents

Polymorphic form of the tachykinin receptor antagonist 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

Info

Publication number
IL133357A
IL133357A IL13335798A IL13335798A IL133357A IL 133357 A IL133357 A IL 133357A IL 13335798 A IL13335798 A IL 13335798A IL 13335798 A IL13335798 A IL 13335798A IL 133357 A IL133357 A IL 133357A
Authority
IL
Israel
Prior art keywords
phenyl
triazolo
methylmorpholine
oxo
trifluoromethyl
Prior art date
Application number
IL13335798A
Other languages
English (en)
Other versions
IL133357A0 (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
Priority claimed from GBGB9800216.5A external-priority patent/GB9800216D0/en
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Publication of IL133357A0 publication Critical patent/IL133357A0/xx
Publication of IL133357A publication Critical patent/IL133357A/xx

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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (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)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (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)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Polyamides (AREA)
  • Polyurethanes Or Polyureas (AREA)
IL13335798A 1997-07-02 1998-07-01 Polymorphic form of the tachykinin receptor antagonist 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 IL133357A (en)

Applications Claiming Priority (3)

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
PCT/US1998/013766 WO1999001444A1 (en) 1997-07-02 1998-07-01 Polymorphic form of the tachykinin receptor antagonist 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

Publications (2)

Publication Number Publication Date
IL133357A0 IL133357A0 (en) 2001-04-30
IL133357A true IL133357A (en) 2003-12-10

Family

ID=26312895

Family Applications (1)

Application Number Title Priority Date Filing Date
IL13335798A IL133357A (en) 1997-07-02 1998-07-01 Polymorphic form of the tachykinin receptor antagonist 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

Country Status (27)

Country Link
EP (1) EP0994867B1 (cs)
JP (1) JP2000513383A (cs)
KR (1) KR20010020593A (cs)
CN (1) CN1106390C (cs)
AT (1) ATE372991T1 (cs)
AU (1) AU735230B2 (cs)
BG (1) BG64703B1 (cs)
CA (1) CA2293836C (cs)
CZ (1) CZ295410B6 (cs)
DE (1) DE69838421D1 (cs)
DZ (1) DZ2551A1 (cs)
EA (1) EA002405B1 (cs)
EE (1) EE04152B1 (cs)
HK (1) HK1029345A1 (cs)
HR (1) HRP980370B1 (cs)
HU (1) HU228003B1 (cs)
ID (1) ID23191A (cs)
IL (1) IL133357A (cs)
IS (1) IS2617B (cs)
NO (1) NO316893B1 (cs)
NZ (1) NZ501589A (cs)
PE (1) PE86499A1 (cs)
PL (1) PL191496B1 (cs)
SK (1) SK285644B6 (cs)
TR (1) TR199903299T2 (cs)
TW (1) TW577887B (cs)
WO (1) WO1999001444A1 (cs)

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
ES2299720T3 (es) * 2002-05-31 2008-06-01 Schering Corporation Formas polimorfas de un inhibidor de xantina-fosfodiesterasa v.
GB0417702D0 (en) * 2004-08-09 2004-09-08 Merck Sharp & Dohme New uses
EP2266980A1 (en) 2005-10-05 2010-12-29 Ranbaxy Laboratories Limited Polymorphic form of aprepitant intermediate
US9227958B2 (en) 2006-02-03 2016-01-05 Glenmark Pharmaceuticals Limited Amorphous and crystalline forms of aprepitant and processes for the preparation thereof
SG10201500027TA (en) * 2006-04-05 2015-02-27 Opko Health Inc Hydrochloride salts of 8-[{1-(3,5-bis-(trifluoromethyl) phenyl) -ethoxy}-methyl] -8-phenyl-1,7-diaza-spiro[4.5] decan-2-one and preparation process therefor
WO2008026216A2 (en) * 2006-08-28 2008-03-06 Hetero Drugs Limited Process for purification of aprepitant
WO2008044102A1 (en) * 2006-10-13 2008-04-17 Glenmark Pharmaceuticals Limited Polymorph form of aprepitant and process for the preparation thereof
US8093268B2 (en) 2007-01-24 2012-01-10 Glaxo Group Limited Pharmaceutical compositions comprising 2-methoxy-5-(5-trifluoromethyl-tetrazol-1-yl-benzyl)-(2S-phenylpiperidin-3S-yl-)
HUE036546T2 (hu) * 2008-02-18 2018-07-30 Esteve Labor Dr Szigma-receptor ligandumokhoz kötõdõ vegyületek alkalmazása kemoterápia következményeként kifejlõdõ neuropátiás fájdalom kezelésére
EP2116539A1 (en) 2008-04-25 2009-11-11 Laboratorios Del. Dr. Esteve, S.A. 1-aryl-3-aminoalkoxy-pyrazoles as sigma ligands enhancing analgesic effects of opioids and attenuating the dependency thereof
EP2353598A1 (en) 2010-02-04 2011-08-10 Laboratorios Del. Dr. Esteve, S.A. Sigma ligands for use in the prevention and/or treatment of postoperative pain
EP2353591A1 (en) 2010-02-04 2011-08-10 Laboratorios Del. Dr. Esteve, S.A. Sigma ligands for potentiating the analgesic effect of opioids and opiates in post-operative pain and attenuating the dependency thereof
EP2388005A1 (en) 2010-05-21 2011-11-23 Laboratorios Del. Dr. Esteve, S.A. Sigma ligands for the prevention and/or treatment of emesis induced by chemotherapy or radiotherapy
EP2415471A1 (en) 2010-08-03 2012-02-08 Laboratorios Del. Dr. Esteve, S.A. Use of sigma ligands in opioid-induced hyperalgesia
EP2524694A1 (en) 2011-05-19 2012-11-21 Laboratorios Del. Dr. Esteve, S.A. Use of sigma ligands in diabetes type-2 associated pain
JP5998933B2 (ja) * 2011-06-30 2016-09-28 東レ株式会社 グリシン誘導体の結晶及びその医薬用途
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
WO2015091508A1 (en) 2013-12-17 2015-06-25 Laboratorios Del Dr. Esteve, S.A. 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
EE9900603A (et) 2000-08-15
NZ501589A (en) 2001-10-26
AU8283398A (en) 1999-01-25
IS2617B (is) 2010-04-15
CA2293836A1 (en) 1999-01-14
TR199903299T2 (xx) 2000-07-21
EP0994867A1 (en) 2000-04-26
EP0994867B1 (en) 2007-09-12
ID23191A (id) 2000-03-23
BG64703B1 (bg) 2005-12-30
TW577887B (en) 2004-03-01
CN1261882A (zh) 2000-08-02
NO996549D0 (no) 1999-12-29
ATE372991T1 (de) 2007-09-15
HK1029345A1 (en) 2001-03-30
HU228003B1 (en) 2012-08-28
CZ477799A3 (cs) 2000-09-13
AU735230B2 (en) 2001-07-05
CN1106390C (zh) 2003-04-23
KR20010020593A (ko) 2001-03-15
CA2293836C (en) 2007-06-05
PL337579A1 (en) 2000-08-28
CZ295410B6 (cs) 2005-08-17
JP2000513383A (ja) 2000-10-10
NO996549L (no) 2000-03-01
SK285644B6 (sk) 2007-05-03
DE69838421D1 (en) 2007-10-25
HRP980370B1 (en) 2002-10-31
IS5293A (is) 1999-12-10
WO1999001444A1 (en) 1999-01-14
HRP980370A2 (en) 1999-04-30
HUP0004008A2 (hu) 2002-02-28
EE04152B1 (et) 2003-10-15
IL133357A0 (en) 2001-04-30
EA199901114A1 (ru) 2000-08-28
EA002405B1 (ru) 2002-04-25
NO316893B1 (no) 2004-06-14
DZ2551A1 (fr) 2003-08-15
PE86499A1 (es) 1999-10-25
SK187299A3 (en) 2000-07-11
HUP0004008A3 (en) 2002-03-28
PL191496B1 (pl) 2006-05-31
BG104010A (en) 2001-08-31

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