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-isobutiramidaInfo
- 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
Links
- -1 3,5-Bis-trifluoromethyl-phenyl Chemical group 0.000 title abstract 3
- 230000004048 modification Effects 0.000 title abstract 3
- 238000012986 modification Methods 0.000 title abstract 3
- 238000002441 X-ray diffraction Methods 0.000 abstract 1
- 230000001154 acute effect Effects 0.000 abstract 1
- 238000002329 infrared spectrum Methods 0.000 abstract 1
- 230000008018 melting Effects 0.000 abstract 1
- 238000002844 melting Methods 0.000 abstract 1
- 230000005855 radiation Effects 0.000 abstract 1
- 125000004571 thiomorpholin-4-yl group Chemical group N1(CCSCC1)* 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic 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
- C07D213/02—Heterocyclic 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
- C07D213/04—Heterocyclic 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
- C07D213/60—Heterocyclic 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
- C07D213/72—Nitrogen atoms
- C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic 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
- C07D417/02—Heterocyclic 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
- C07D417/04—Heterocyclic 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/54—Heterocyclic 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
- A61K31/541—Non-condensed thiazines containing further heterocyclic rings
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P25/00—Drugs for disorders of the nervous system
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- A61P25/16—Anti-Parkinson drugs
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- A—HUMAN NECESSITIES
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- 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
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/34—Tobacco-abuse
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- A61P25/36—Opioid-abuse
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/16—Otologicals
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- 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]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
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- 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
- A61P37/08—Antiallergic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/10—Antioedematous agents; Diuretics
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Addiction (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Hospice & Palliative Care (AREA)
- Urology & Nephrology (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Epidemiology (AREA)
- Psychology (AREA)
- Diabetes (AREA)
- Physical Education & Sports Medicine (AREA)
- Hematology (AREA)
- Otolaryngology (AREA)
- Ophthalmology & Optometry (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.
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)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2007000198A (es) | 2004-07-06 | 2007-03-15 | Hoffmann La Roche | Proceso para la preparacion de derivados de carboxamida-piridina utilizados como intermediarios en la sintesis de antagonistas del receptor nk-1. |
| BRPI0606187A2 (pt) | 2005-02-25 | 2009-06-09 | Hoffmann La Roche | comprimidos com capacidade de dispersão da substáncia do fármaco melhorada |
| CA2772168C (en) * | 2009-08-27 | 2019-01-08 | Glaxosmithkline Llc | Anhydrate forms of a pyridine derivative |
| 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 (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2024507C1 (ru) * | 1991-11-18 | 1994-12-15 | Евгений Яковлевич Левитин | 5-хлор-2-пиридиламид-4-нитро-n-(карбоксиметил)антраниловой кислоты, проявляющий противовоспалительную активность |
| IL111960A (en) * | 1993-12-17 | 1999-12-22 | Merck & Co Inc | Morpholines and thiomorpholines their preparation and pharmaceutical compositions containing them |
| ATE364606T1 (de) * | 1993-12-29 | 2007-07-15 | Merck Sharp & Dohme | Substituierte morpholinderivate und ihre verwendung als arzneimittel |
| IL112778A0 (en) * | 1994-03-04 | 1995-05-26 | Merck & Co Inc | Substituted heterocycles, their preparation and pharmaceutical compositions containing them |
| US5972938A (en) * | 1997-12-01 | 1999-10-26 | Merck & Co., Inc. | Method for treating or preventing psychoimmunological disorders |
| 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. |
| MXPA03009720A (es) * | 2001-04-23 | 2004-01-29 | Hoffmann La Roche | USO DE ANTAGONISTAS DEL RECEPTOR DE NK-1 PARA TRATAMIENTO O PREVENCIoN DE HIPERPLASIA PROSTATICA BENIGNA. |
| US6849624B2 (en) * | 2001-07-31 | 2005-02-01 | Hoffmann-La Roche Inc. | Aromatic and heteroaromatic substituted amides |
-
2004
- 2004-01-23 PL PL378404A patent/PL378404A1/pl unknown
- 2004-01-23 MX MXPA05008171A patent/MXPA05008171A/es active IP Right Grant
- 2004-01-23 BR BR0406702-9A patent/BRPI0406702A/pt not_active Application Discontinuation
- 2004-01-23 AT AT04704575T patent/ATE366576T1/de active
- 2004-01-23 EP EP04704575A patent/EP1592428B1/en not_active Expired - Lifetime
- 2004-01-23 JP JP2005518353A patent/JP5026702B2/ja not_active Expired - Fee Related
- 2004-01-23 RU RU2005127216/04A patent/RU2330022C2/ru not_active IP Right Cessation
- 2004-01-23 WO PCT/EP2004/000547 patent/WO2004067007A1/en not_active Ceased
- 2004-01-23 ES ES04704575T patent/ES2290666T3/es not_active Expired - Lifetime
- 2004-01-23 HR HR20050664A patent/HRP20050664A2/xx not_active Application Discontinuation
- 2004-01-23 KR KR1020057014025A patent/KR100700421B1/ko not_active Expired - Fee Related
- 2004-01-23 NZ NZ541243A patent/NZ541243A/en unknown
- 2004-01-23 AU AU2004208483A patent/AU2004208483B8/en not_active Ceased
- 2004-01-23 DE DE602004007486T patent/DE602004007486T2/de not_active Expired - Lifetime
- 2004-01-23 CA CA2514037A patent/CA2514037C/en not_active Expired - Fee Related
- 2004-01-23 CN CN200480003306.7A patent/CN100562320C/zh not_active Expired - Fee Related
- 2004-01-27 US US10/766,122 patent/US7160881B2/en not_active Expired - Fee Related
- 2004-01-27 TW TW093101746A patent/TWI293294B/zh active
- 2004-01-28 PA PA20048594601A patent/PA8594601A1/es unknown
- 2004-01-28 PE PE2004000110A patent/PE20040944A1/es not_active Application Discontinuation
- 2004-01-29 GT GT200400009A patent/GT200400009A/es unknown
- 2004-01-30 MY MYPI20040288A patent/MY135785A/en unknown
- 2004-01-30 AR ARP040100284A patent/AR042980A1/es unknown
- 2004-01-30 CL CL200400150A patent/CL2004000150A1/es unknown
-
2005
- 2005-07-07 IL IL169600A patent/IL169600A/en unknown
- 2005-07-11 ZA ZA200505567A patent/ZA200505567B/en unknown
- 2005-07-14 NO NO20053431A patent/NO20053431L/no not_active Application Discontinuation
- 2005-07-18 CO CO05070753A patent/CO5580750A2/es not_active Application Discontinuation
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