CO5261525A1 - Forma poliformica de un antagonista de los receptores de las taquiquininas . - Google Patents

Forma poliformica de un antagonista de los receptores de las taquiquininas .

Info

Publication number
CO5261525A1
CO5261525A1 CO00081623A CO00081623A CO5261525A1 CO 5261525 A1 CO5261525 A1 CO 5261525A1 CO 00081623 A CO00081623 A CO 00081623A CO 00081623 A CO00081623 A CO 00081623A CO 5261525 A1 CO5261525 A1 CO 5261525A1
Authority
CO
Colombia
Prior art keywords
methyl
triazol
fluorophenyl
morpholine
dimethylamino
Prior art date
Application number
CO00081623A
Other languages
English (en)
Inventor
Louis Crocker
Cai Dongwei
Jian Wang
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
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Publication of CO5261525A1 publication Critical patent/CO5261525A1/es

Links

Classifications

    • 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
    • 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
    • A61P25/06—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
    • A61P25/18—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
    • A61P25/22—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C17/00—Preparation of halogenated hydrocarbons
    • C07C17/093—Preparation of halogenated hydrocarbons by replacement by halogens
    • C07C17/10—Preparation of halogenated hydrocarbons by replacement by halogens of hydrogen atoms
    • C07C17/12—Preparation of halogenated hydrocarbons by replacement by halogens of hydrogen atoms in the ring of aromatic compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/004—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reaction with organometalhalides

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (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)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Una forma polimórfica del compuesto clorhidrato de 2-(R)-(1-(R)-(3,5-bis(trifluorometil)fenil)etoxi)-4-(5-(dimetilamino)metil-1,2,3-triazol-4-il)metil-3-(s)-(4-fluorofenil)morfolina designada como Forma I.Una composición farmacéutica que comprende un vehículo portador-farmacéuticamente aceptable y una cantidad eficaz de la forma polimórfica acorde con la Reivindicación 1. Un proceso para la preparación de la Forma I del clorhidrato de 2-(R)-(1-(R)-(3,5-bis(trifluorometil)fenil)etoxi)-4-(5-(dimetilamino)metil-1,2,3-triazol-4-il)metil-3-(S)-(4-fluorofenil)morfolina, proceso que comprende:adición de ácido clorhídrico anhidro en isopropanol a una solución de clorhidrato de 2-(R)-(1-(R)-(3,5-bis(trifluorometil)fenil)etoxi)-4-(5-(dimetilamino)metil-1,2,3-triazol-4-il) metil-3-(S)-(4-fluorofenil)morfolina en acetato de etilo,a lo cual sigue la adición de heptano para obtener la Forma I del clorhidrato de 2-(R)-(1-(R)-(3,5-bis(trifluorometil)fenil)etoxi)-4-(5-(dimetilamino)metiI-1,2,3-triazol-4-il)metil-3-(S)-(4-fluorofenil)-morfolina.<EMI FILE="00081623_1" ID="1" IMF=JPEG >
CO00081623A 1999-10-29 2000-10-26 Forma poliformica de un antagonista de los receptores de las taquiquininas . CO5261525A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US16271199P 1999-10-29 1999-10-29

Publications (1)

Publication Number Publication Date
CO5261525A1 true CO5261525A1 (es) 2003-03-31

Family

ID=22586824

Family Applications (1)

Application Number Title Priority Date Filing Date
CO00081623A CO5261525A1 (es) 1999-10-29 2000-10-26 Forma poliformica de un antagonista de los receptores de las taquiquininas .

Country Status (9)

Country Link
US (1) US6432952B1 (es)
EP (1) EP1228068A1 (es)
JP (1) JP2003513095A (es)
AR (1) AR026288A1 (es)
AU (1) AU1343901A (es)
CA (1) CA2388202A1 (es)
CO (1) CO5261525A1 (es)
PE (1) PE20010824A1 (es)
WO (1) WO2001032656A1 (es)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7122376B2 (en) * 2001-11-01 2006-10-17 Facet Analytical Services And Technology, Llc Calibration standards, methods, and kits for water determination
US7049146B2 (en) 2000-11-14 2006-05-23 Facet Analytical Services And Technology, Llc Calibration standards, methods, and kits for water determination
EP1295599A1 (en) * 2001-09-21 2003-03-26 Boehringer Ingelheim International GmbH Method for the treatment of prevention of atopic dermatitis
AU2003270727A1 (en) * 2002-09-17 2004-04-08 Luna Innovations, Inc. Remote temperature sensing of small volume and related apparatus thereof
ATE462700T1 (de) * 2003-10-24 2010-04-15 Lilly Co Eli Neue kristalline formen von ä2-ä1-(3,5- bistrifluormethylbenzyl)-5-pyridin-4-yl-1h-ä1,2 3üütriazol-4-ylü-pyridin-3-ylü-(2- chlorphenyl)methanon
US20080200376A1 (en) * 2004-10-29 2008-08-21 Maccoss Malcolm Compositions and Methods For the Treatment Of Obesity and Sexual Dysfunction
WO2006083711A1 (en) * 2005-02-01 2006-08-10 Eli Lilly And Company Tachykinin receptor antagonists

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ277839A (en) * 1993-12-29 1998-01-26 Merck Sharp & Dohme Substituted morpholine derivatives, preparation and pharmaceutical compositions thereof
EA002405B1 (ru) * 1997-07-02 2002-04-25 Мерк Энд Ко., Инк. Полиморфная форма 2-(r)-(1-(r)-(3,5-бис(трифторметил)фенил)этокси)-3-(s)-(4-фтор)фенил-4-(3-(5-оксо-1h,4h-1,2,4-триазоло)метил)морфолина в качестве антагониста рецептора тахикинина

Also Published As

Publication number Publication date
WO2001032656A1 (en) 2001-05-10
EP1228068A1 (en) 2002-08-07
AR026288A1 (es) 2003-02-05
US6432952B1 (en) 2002-08-13
CA2388202A1 (en) 2001-05-10
JP2003513095A (ja) 2003-04-08
PE20010824A1 (es) 2001-09-07
AU1343901A (en) 2001-05-14

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