BRPI0406702A - Modificação cristalina de 2-(3,5-bis-trifluormetil-fenil)-n-[6-(1,1-dioxo-1 lâmboa^6^-tiomorfolin-4-il)-4-(4-flúor-2-metil-fenil)-pi ridin-3-il]-n-metil-isobutiramida - Google Patents

Modificação cristalina de 2-(3,5-bis-trifluormetil-fenil)-n-[6-(1,1-dioxo-1 lâmboa^6^-tiomorfolin-4-il)-4-(4-flúor-2-metil-fenil)-pi ridin-3-il]-n-metil-isobutiramida

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Publication number
BRPI0406702A
BRPI0406702A BR0406702-9A BRPI0406702A BRPI0406702A BR PI0406702 A BRPI0406702 A BR PI0406702A BR PI0406702 A BRPI0406702 A BR PI0406702A BR PI0406702 A BRPI0406702 A BR PI0406702A
Authority
BR
Brazil
Prior art keywords
methyl
phenyl
pyridin
bis
thiomorpholin
Prior art date
Application number
BR0406702-9A
Other languages
English (en)
Inventor
Torsten Hoffmann
Fabienne Hoffmann-Emery
Sonia Nick
Urs Schwitter
Pius Waldmeier
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of BRPI0406702A publication Critical patent/BRPI0406702A/pt

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72Nitrogen atoms
    • C07D213/75Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541Non-condensed thiazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P11/08Bronchodilators
    • AHUMAN NECESSITIES
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    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
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    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
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    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
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    • A61P25/00Drugs for disorders of the nervous system
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    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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    • A61P25/00Drugs for disorders of the nervous system
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    • A61P25/00Drugs for disorders of the nervous system
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34Tobacco-abuse
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
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    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10Antioedematous agents; Diuretics

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (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)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Addiction (AREA)
  • Immunology (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Otolaryngology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Detergent Compositions (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

"MODIFICAçãO CRISTALINA DE 2-(3,5-BIS-TRI-FLUORMETIL-FENIL)-N-¢6-(1,1-DIOXO-1 LâMBOA~ 6¬ -TIOMORFOLIN-4-IL)-4-(4-FLúOR-2-METIL-FENIL)-PIRIDIN-3-IL!- N-METIL-ISOBUTIRAMIDA". A presente invenção refere-se a uma nova modificação cristalina de 2-(3,5-bis-trifluormetil-fenil)-N-¢6-(1,1,-dioXo1<sym>¬ 6¬tiomorfolin-4-il)-4-(4-flúor-2-metil-fenil)-piridin-3-il!-N-metil-isobutirami da caracterizada pelo seguinte padrão de difração de raios X obtido com uma radiação CU~ K<244>~ a 20 (2 teta) = 4,5, 6,4, 7,5, 7,7, 8,0, 8,2, 10,0, 10,2, 10,9, 11,1, 12,9, 13,4, 14,0, 14,5, 15,1, 15,6, 16,2, 16,5, 17,3, 17,5, 18,0, 18,9, 19,3, 19,5, 19,9, 20,1, 20,6, 21,0, 21,4, 22,7, 23,1 e 23,6 e um espectro de infravermelho com faixas agudas a 2925, 2854, 1637, 1604, 1484, 1395, 1375, 1285, 1230, 1172, 1125, 1082, 999, 943, 893, 863, 860, 782, 705, 684 cm¬ -1¬ e em que o ponto de fusão extrapolado (DSC) é 137,2,198>C.
BR0406702-9A 2003-01-31 2004-01-23 Modificação cristalina de 2-(3,5-bis-trifluormetil-fenil)-n-[6-(1,1-dioxo-1 lâmboa^6^-tiomorfolin-4-il)-4-(4-flúor-2-metil-fenil)-pi ridin-3-il]-n-metil-isobutiramida BRPI0406702A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP03002134 2003-01-31
PCT/EP2004/000547 WO2004067007A1 (en) 2003-01-31 2004-01-23 NEW CRYSTALLINE MODIFICATION OF 2-(3,5-BIS-TRIFLUOROMETHYL-PHENYL)-N-[6-(1,1-DIOXO-1λ6-THIOMORPHOLIN-4-YL)-4(4-FLUORO-2-METHYL-PHENYL)-PYRIDIN-3-YL]-N-METHYL-ISOBUTYRAMIDE

Publications (1)

Publication Number Publication Date
BRPI0406702A true BRPI0406702A (pt) 2005-12-20

Family

ID=32798734

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0406702-9A BRPI0406702A (pt) 2003-01-31 2004-01-23 Modificação cristalina de 2-(3,5-bis-trifluormetil-fenil)-n-[6-(1,1-dioxo-1 lâmboa^6^-tiomorfolin-4-il)-4-(4-flúor-2-metil-fenil)-pi ridin-3-il]-n-metil-isobutiramida

Country Status (28)

Country Link
US (1) US7160881B2 (pt)
EP (1) EP1592428B1 (pt)
JP (1) JP5026702B2 (pt)
KR (1) KR100700421B1 (pt)
CN (1) CN100562320C (pt)
AR (1) AR042980A1 (pt)
AT (1) ATE366576T1 (pt)
AU (1) AU2004208483B8 (pt)
BR (1) BRPI0406702A (pt)
CA (1) CA2514037C (pt)
CL (1) CL2004000150A1 (pt)
CO (1) CO5580750A2 (pt)
DE (1) DE602004007486T2 (pt)
ES (1) ES2290666T3 (pt)
GT (1) GT200400009A (pt)
HR (1) HRP20050664A2 (pt)
IL (1) IL169600A (pt)
MX (1) MXPA05008171A (pt)
MY (1) MY135785A (pt)
NO (1) NO20053431L (pt)
NZ (1) NZ541243A (pt)
PA (1) PA8594601A1 (pt)
PE (1) PE20040944A1 (pt)
PL (1) PL378404A1 (pt)
RU (1) RU2330022C2 (pt)
TW (1) TWI293294B (pt)
WO (1) WO2004067007A1 (pt)
ZA (1) ZA200505567B (pt)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006002860A1 (en) 2004-07-06 2006-01-12 F. Hoffmann-La Roche Ag Process for preparing carboxamide pyridine derivatives used as intermediates in the synthesis of nk-1 receptor antagonists
RU2007129642A (ru) 2005-02-25 2009-03-27 Ф.Хоффманн-Ля Рош Аг (Ch) Таблетки с улучшенным распределением лекарственного вещества
ES2440938T3 (es) * 2009-08-27 2014-01-31 Nerre Therapeutics Limited Formas anhidrato de un derivado de piridina
CN103755592A (zh) * 2013-12-30 2014-04-30 镇江圣安医药有限公司 (2z)-氰基-3-羟基-n-[4-(三氟甲基)苯基]-2-丁烯酰胺的衍生物及其应用

Family Cites Families (7)

* 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
EP0737192B1 (en) 1993-12-29 2001-10-31 Merck Sharp & Dohme Ltd. Substituted morpholine derivatives and their use as therapeutic agents
TW385308B (en) 1994-03-04 2000-03-21 Merck & Co Inc Prodrugs of morpholine tachykinin receptor antagonists
US5972938A (en) * 1997-12-01 1999-10-26 Merck & Co., Inc. Method for treating or preventing psychoimmunological disorders
SE1035115T5 (sv) 1999-02-24 2015-08-04 Hoffmann La Roche 4-fenylpyridin-derivat och deras anvaendning som NK-1 receptor-antagonister
DE60210760T2 (de) * 2001-04-23 2006-11-23 F. Hoffmann-La Roche Ag Verwendung von nk-1-rezeptorantagonisten gegen benigne prostatahyperplasie
US6849624B2 (en) * 2001-07-31 2005-02-01 Hoffmann-La Roche Inc. Aromatic and heteroaromatic substituted amides

Also Published As

Publication number Publication date
JP5026702B2 (ja) 2012-09-19
DE602004007486D1 (de) 2007-08-23
EP1592428B1 (en) 2007-07-11
JP2006514999A (ja) 2006-05-18
US7160881B2 (en) 2007-01-09
KR100700421B1 (ko) 2007-03-28
CO5580750A2 (es) 2005-11-30
KR20050096964A (ko) 2005-10-06
ZA200505567B (en) 2007-05-30
RU2005127216A (ru) 2006-04-10
CA2514037A1 (en) 2004-08-12
AR042980A1 (es) 2005-07-13
RU2330022C2 (ru) 2008-07-27
AU2004208483B8 (en) 2008-04-03
MXPA05008171A (es) 2005-10-05
NO20053431L (no) 2005-10-05
TWI293294B (en) 2008-02-11
NZ541243A (en) 2008-04-30
AU2004208483B2 (en) 2008-03-06
PA8594601A1 (es) 2004-09-16
GT200400009A (es) 2004-12-01
CN100562320C (zh) 2009-11-25
ATE366576T1 (de) 2007-08-15
PL378404A1 (pl) 2006-04-03
CA2514037C (en) 2012-03-13
HRP20050664A2 (en) 2006-12-31
CN1744900A (zh) 2006-03-08
TW200510358A (en) 2005-03-16
WO2004067007A1 (en) 2004-08-12
NO20053431D0 (no) 2005-07-14
ES2290666T3 (es) 2008-02-16
MY135785A (en) 2008-06-30
DE602004007486T2 (de) 2008-04-30
US20040186100A1 (en) 2004-09-23
EP1592428A1 (en) 2005-11-09
AU2004208483A1 (en) 2004-08-12
IL169600A (en) 2010-11-30
CL2004000150A1 (es) 2005-01-07
PE20040944A1 (es) 2004-12-14

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B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B06A Patent application procedure suspended [chapter 6.1 patent gazette]
B11B Dismissal acc. art. 36, par 1 of ipl - no reply within 90 days to fullfil the necessary requirements