ES2171134A1 - Procedimiento para la preparacion del pompuesto 2-(3,5-bis-trifluorometil-fenil)-n-,etil-n-(6-morfolin-4-il-o-tolil-priridin-3-il)-isobutiramida. el producto per se, y su uso para la preparacion de medicamentos. - Google Patents
Procedimiento para la preparacion del pompuesto 2-(3,5-bis-trifluorometil-fenil)-n-,etil-n-(6-morfolin-4-il-o-tolil-priridin-3-il)-isobutiramida. el producto per se, y su uso para la preparacion de medicamentos.Info
- Publication number
- ES2171134A1 ES2171134A1 ES200002839A ES200002839A ES2171134A1 ES 2171134 A1 ES2171134 A1 ES 2171134A1 ES 200002839 A ES200002839 A ES 200002839A ES 200002839 A ES200002839 A ES 200002839A ES 2171134 A1 ES2171134 A1 ES 2171134A1
- Authority
- ES
- Spain
- Prior art keywords
- preparation
- procedure
- morfolin
- medicines
- bis
- Prior art date
- Legal status (The legal status 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 status listed.)
- Withdrawn
Links
- 239000003814 drug Substances 0.000 title abstract 4
- 238000000034 method Methods 0.000 title abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 229940079593 drug Drugs 0.000 abstract 3
- 208000019901 Anxiety disease Diseases 0.000 abstract 1
- 208000020401 Depressive disease Diseases 0.000 abstract 1
- 102000002002 Neurokinin-1 Receptors Human genes 0.000 abstract 1
- 108010040718 Neurokinin-1 Receptors Proteins 0.000 abstract 1
- 206010047700 Vomiting Diseases 0.000 abstract 1
- 230000036506 anxiety Effects 0.000 abstract 1
- 208000015114 central nervous system disease Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 229940047889 isobutyramide Drugs 0.000 abstract 1
- 238000002483 medication Methods 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- 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
- C07D413/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
-
- 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
- A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
-
- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
- A61P25/18—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
- 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)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pulmonology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Otolaryngology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
Procedimiento para la preparación del compuesto 2-(3-5-BIS- TRIFLUOROMETIL-FENIL)-N-METIL-N-(6-MORFOLIN-4-IL-O-TOLILPIRIDI N-3-IL)-ISOBUTIRAMIDA, el producto per se, y su uso para la preparación de medicamentos. La invención se refiere a compuestos de fórmula I y a sus sales de adición farmaceúticamente aceptables. Describe también el procedimiento de su preparación y el uso de este compuesto para la preparación de medicamentos para el tratamiento de enfermedades relacionadas con el receptor NK-1. Estos medicamentos se usan para el tratamiento de, entre otros, transtornos del sistema nervioso central, como trastornos depresivos, ansiedad o emesis.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP99123685 | 1999-11-29 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2171134A1 true ES2171134A1 (es) | 2002-08-16 |
Family
ID=8239481
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES00125450T Expired - Lifetime ES2208205T3 (es) | 1999-11-29 | 2000-11-21 | 2-(3,5-bis-trifluorometil-fenil)-n-metil-n-(6-morfolin-4-il-4-otolil-piridin-3-il)-isobutiramida. |
| ES200002839A Withdrawn ES2171134A1 (es) | 1999-11-29 | 2000-11-28 | Procedimiento para la preparacion del pompuesto 2-(3,5-bis-trifluorometil-fenil)-n-,etil-n-(6-morfolin-4-il-o-tolil-priridin-3-il)-isobutiramida. el producto per se, y su uso para la preparacion de medicamentos. |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES00125450T Expired - Lifetime ES2208205T3 (es) | 1999-11-29 | 2000-11-21 | 2-(3,5-bis-trifluorometil-fenil)-n-metil-n-(6-morfolin-4-il-4-otolil-piridin-3-il)-isobutiramida. |
Country Status (49)
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK1394150T3 (da) * | 1999-02-24 | 2011-03-21 | Hoffmann La Roche | 4-phenylpyridinderivater og deres anvendelse som NK-1-receptorantagonister |
| RU2238264C2 (ru) * | 1999-02-24 | 2004-10-20 | Ф.Хоффманн-Ля Рош Аг | Производные бензола или пиридина и фармацевтическая композиция на их основе |
| NZ523273A (en) * | 2000-07-14 | 2004-08-27 | F | N-oxides as NK1 receptor antagonist prodrugs of 4-phenyl-pyridine derivatives |
| TWI287003B (en) * | 2000-07-24 | 2007-09-21 | Hoffmann La Roche | 4-phenyl-pyridine derivatives |
| TWI259180B (en) * | 2000-08-08 | 2006-08-01 | Hoffmann La Roche | 4-Phenyl-pyridine derivatives |
| US20030083345A1 (en) * | 2001-07-10 | 2003-05-01 | Torsten Hoffmann | Method of treatment and/or prevention of brain, spinal or nerve injury |
| WO2003064685A2 (en) * | 2002-01-31 | 2003-08-07 | F. Hoffmann-La Roche Ag | Genetic polymorphisms in the preprotachykinin gene |
| DE602004008631T2 (de) | 2003-07-03 | 2008-07-10 | F. Hoffmann-La Roche Ag | Duale nk1/nk3 antagonisten zur behandlung von schizophrenie |
| TWI280239B (en) | 2003-07-15 | 2007-05-01 | Hoffmann La Roche | Process for preparation of pyridine derivatives |
| CA2572645C (en) | 2004-07-06 | 2011-01-18 | F. Hoffmann-La Roche Ag | Process for preparing carboxamide derivatives used as intermediates in the synthesis of nk-1 receptor antagonists |
| WO2006089674A2 (en) | 2005-02-25 | 2006-08-31 | F.Hoffmann-La Roche Ag | Tablets with improved drug substance dispersibility |
| EP1863767B1 (en) | 2005-03-23 | 2009-03-11 | F. Hoffmann-Roche AG | Metabolites for nk-i antagonists for emesis |
| SI1928427T1 (sl) * | 2005-09-23 | 2010-03-31 | Hoffmann La Roche | Nove formulacije za doziranje |
| WO2008090114A1 (en) | 2007-01-24 | 2008-07-31 | Glaxo Group Limited | Pharmaceutical compositions comprising 2-methoxy-5- (5-trifluoromethyl-tetrazol-i-yl-benzyl) - (2s-phenyl-piperidin-3s-yl-) |
| US8426450B1 (en) * | 2011-11-29 | 2013-04-23 | Helsinn Healthcare Sa | Substituted 4-phenyl pyridines having anti-emetic effect |
| EP2970308B1 (en) | 2013-03-15 | 2021-07-14 | Global Blood Therapeutics, Inc. | Compounds and uses thereof for the modulation of hemoglobin |
| ES2671418T3 (es) | 2013-11-08 | 2018-06-06 | Kissei Pharmaceutical Co., Ltd. | Derivado de carboximetilpiperidina |
| AP2016009261A0 (en) | 2014-02-07 | 2016-06-30 | Global Blood Therapeutics Inc | Crystalline polymorphs of the free base of 2-hydroxy-6-((2-(1-isopropyl-1h-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde |
| TWI649307B (zh) | 2014-05-07 | 2019-02-01 | 日商橘生藥品工業股份有限公司 | Cyclohexylpyridine derivative |
| KR101948238B1 (ko) | 2016-08-19 | 2019-02-14 | (주)케어젠 | 미녹시딜과 펩타이드의 결합체 |
| KR102328682B1 (ko) | 2018-08-27 | 2021-11-18 | 주식회사 대웅제약 | 신규한 헤테로사이클릭아민 유도체 및 이를 포함하는 약학 조성물 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0733632A1 (en) * | 1995-03-24 | 1996-09-25 | Takeda Chemical Industries, Ltd. | Cyclic compounds, their production and use as tachykinin receptor antagonists |
| EP0916346A2 (en) * | 1991-09-20 | 1999-05-19 | Glaxo Group Limited | NK-1 receptor antagonists and 5HT3 receptor antagonists for the treatment of emesis |
| EP1035115A1 (en) * | 1999-02-24 | 2000-09-13 | F. Hoffmann-La Roche Ag | 4-Phenylpyridine derivatives and their use as NK-1 receptor antagonists |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL106142A (en) * | 1992-06-29 | 1997-03-18 | Merck & Co Inc | Morpholine and thiomorpholine tachykinin receptor antagonists, their preparation and pharmaceutical compositions containing them |
| IL111960A (en) * | 1993-12-17 | 1999-12-22 | Merck & Co Inc | Morpholines and thiomorpholines their preparation and pharmaceutical compositions containing them |
| NZ277839A (en) * | 1993-12-29 | 1998-01-26 | Merck Sharp & Dohme | Substituted morpholine derivatives, preparation and pharmaceutical compositions thereof |
| 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 |
| US6303790B1 (en) * | 1999-11-29 | 2001-10-16 | Hoffman-La Roche Inc. | Process for the preparation of pyridine derivatives |
| NZ523273A (en) * | 2000-07-14 | 2004-08-27 | F | N-oxides as NK1 receptor antagonist prodrugs of 4-phenyl-pyridine derivatives |
| TWI287003B (en) * | 2000-07-24 | 2007-09-21 | Hoffmann La Roche | 4-phenyl-pyridine derivatives |
| TWI259180B (en) * | 2000-08-08 | 2006-08-01 | Hoffmann La Roche | 4-Phenyl-pyridine derivatives |
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2000
- 2000-11-21 SI SI200030246T patent/SI1103545T1/xx unknown
- 2000-11-21 TR TR2003/02077T patent/TR200302077T4/xx unknown
- 2000-11-21 DK DK00125450T patent/DK1103545T3/da active
- 2000-11-21 DE DE60006340T patent/DE60006340T2/de not_active Expired - Lifetime
- 2000-11-21 AT AT00125450T patent/ATE253561T1/de active
- 2000-11-21 PT PT00125450T patent/PT1103545E/pt unknown
- 2000-11-21 ES ES00125450T patent/ES2208205T3/es not_active Expired - Lifetime
- 2000-11-21 EP EP00125450A patent/EP1103545B1/en not_active Expired - Lifetime
- 2000-11-23 AU AU71787/00A patent/AU775292B2/en not_active Expired
- 2000-11-23 GB GB0028566A patent/GB2356863A/en not_active Withdrawn
- 2000-11-23 IL IL139868A patent/IL139868A/en active IP Right Grant
- 2000-11-23 NZ NZ508386A patent/NZ508386A/xx unknown
- 2000-11-23 YU YU73400A patent/YU73400A/sh unknown
- 2000-11-23 JO JO2000187A patent/JO2298B1/en active
- 2000-11-23 PE PE2000001254A patent/PE20010901A1/es not_active Application Discontinuation
- 2000-11-23 CA CA002326529A patent/CA2326529C/en not_active Expired - Lifetime
- 2000-11-24 DE DE10058310A patent/DE10058310A1/de not_active Withdrawn
- 2000-11-24 FR FR0015193A patent/FR2801590A1/fr not_active Withdrawn
- 2000-11-24 JP JP2000356833A patent/JP3480835B2/ja not_active Expired - Lifetime
- 2000-11-24 PA PA20008507201A patent/PA8507201A1/es unknown
- 2000-11-24 SG SG200006945A patent/SG97171A1/en unknown
- 2000-11-24 CZ CZ20004399A patent/CZ299286B6/cs not_active IP Right Cessation
- 2000-11-24 HR HR20000809A patent/HRP20000809A2/hr not_active Application Discontinuation
- 2000-11-24 IS IS5725A patent/IS2212B/is unknown
- 2000-11-26 GC GCP20001052 patent/GC0000151A/xx active
- 2000-11-27 HU HU0004725A patent/HU224703B1/hu active IP Right Grant
- 2000-11-27 AR ARP000106217A patent/AR033659A1/es unknown
- 2000-11-27 ZA ZA200006964A patent/ZA200006964B/xx unknown
- 2000-11-27 GE GEAP20005644A patent/GEP20022763B/en unknown
- 2000-11-27 MX MXPA00011672A patent/MXPA00011672A/es active IP Right Grant
- 2000-11-27 CO CO00090625A patent/CO5251405A1/es active IP Right Grant
- 2000-11-27 MY MYPI20005527A patent/MY127426A/en unknown
- 2000-11-27 SK SK1793-2000A patent/SK285373B6/sk unknown
- 2000-11-28 GT GT200000197A patent/GT200000197A/es unknown
- 2000-11-28 SV SV2000000227A patent/SV2002000227A/es unknown
- 2000-11-28 MA MA26111A patent/MA26754A1/fr unknown
- 2000-11-28 DO DO2000000106A patent/DOP2000000106A/es unknown
- 2000-11-28 UY UY26458A patent/UY26458A1/es not_active Application Discontinuation
- 2000-11-28 BG BG104992A patent/BG64622B1/bg unknown
- 2000-11-28 PL PL344147A patent/PL195957B1/pl unknown
- 2000-11-28 KR KR10-2000-0071141A patent/KR100390117B1/ko not_active Expired - Lifetime
- 2000-11-28 BR BRPI0005616A patent/BRPI0005616B8/pt not_active IP Right Cessation
- 2000-11-28 NO NO20006012A patent/NO317264B1/no not_active IP Right Cessation
- 2000-11-28 ES ES200002839A patent/ES2171134A1/es not_active Withdrawn
- 2000-11-28 UA UA2000116781A patent/UA70326C2/uk unknown
- 2000-11-28 EA EA200001114A patent/EA004404B1/ru not_active IP Right Cessation
- 2000-11-29 TN TNTNSN00226A patent/TNSN00226A1/fr unknown
- 2000-11-29 CN CNB001342606A patent/CN1152016C/zh not_active Expired - Lifetime
- 2000-11-29 ID IDP20001029D patent/ID28483A/id unknown
- 2000-11-29 OA OA1200000324A patent/OA11513A/fr unknown
- 2000-11-29 IT IT2000MI002575A patent/IT1320120B1/it active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0916346A2 (en) * | 1991-09-20 | 1999-05-19 | Glaxo Group Limited | NK-1 receptor antagonists and 5HT3 receptor antagonists for the treatment of emesis |
| EP0733632A1 (en) * | 1995-03-24 | 1996-09-25 | Takeda Chemical Industries, Ltd. | Cyclic compounds, their production and use as tachykinin receptor antagonists |
| EP1035115A1 (en) * | 1999-02-24 | 2000-09-13 | F. Hoffmann-La Roche Ag | 4-Phenylpyridine derivatives and their use as NK-1 receptor antagonists |
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