PE20020332A1 - Derivados de 4-fenil-piridina como antagonistas de receptores de neuroquinina nk-1 - Google Patents
Derivados de 4-fenil-piridina como antagonistas de receptores de neuroquinina nk-1Info
- Publication number
- PE20020332A1 PE20020332A1 PE2001000779A PE2001000779A PE20020332A1 PE 20020332 A1 PE20020332 A1 PE 20020332A1 PE 2001000779 A PE2001000779 A PE 2001000779A PE 2001000779 A PE2001000779 A PE 2001000779A PE 20020332 A1 PE20020332 A1 PE 20020332A1
- Authority
- PE
- Peru
- Prior art keywords
- halogen
- alkyl
- trifluoromethyl
- alcoxy
- neuroquinin
- Prior art date
Links
- 150000005362 4-phenylpyridines Chemical class 0.000 title abstract 2
- 102000002002 Neurokinin-1 Receptors Human genes 0.000 title abstract 2
- 108010040718 Neurokinin-1 Receptors Proteins 0.000 title abstract 2
- 239000005557 antagonist Substances 0.000 title abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 6
- 150000002367 halogens Chemical class 0.000 abstract 6
- WZKSXHQDXQKIQJ-UHFFFAOYSA-N F[C](F)F Chemical class F[C](F)F WZKSXHQDXQKIQJ-UHFFFAOYSA-N 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- -1 3,5-BIS-TRIFLUOROMETHYL-BENZYL Chemical class 0.000 abstract 1
- 208000006673 asthma Diseases 0.000 abstract 1
- 210000003169 central nervous system Anatomy 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- DDXRSSAMBKGDNC-UHFFFAOYSA-N n-[[3,5-bis(trifluoromethyl)phenyl]methyl]-6-chloro-n-methyl-4-(2-methylphenyl)pyridine-3-carboxamide Chemical compound C=1N=C(Cl)C=C(C=2C(=CC=CC=2)C)C=1C(=O)N(C)CC1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1 DDXRSSAMBKGDNC-UHFFFAOYSA-N 0.000 abstract 1
- 206010039073 rheumatoid arthritis Diseases 0.000 abstract 1
Classifications
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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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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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P25/36—Opioid-abuse
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- 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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- A61P27/00—Drugs for disorders of the senses
- A61P27/16—Otologicals
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- A—HUMAN NECESSITIES
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- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
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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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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- 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
- C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
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- 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
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
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- 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
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
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- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
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- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
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- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- 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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- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Psychiatry (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Addiction (AREA)
- Hospice & Palliative Care (AREA)
- Ophthalmology & Optometry (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
SE REFIERE A DERIVADOS DE 4-FENIL PIRIDINA DE FORMULA I DONDE R ES H, HALOGENO, R1 ES (C=C)mR1', (CR'=CR")mR1'; R1 ES HALOGENO, CIANO, (C)mR'R"R5; CONR'R", COO(CH2)mR5, ENTRE OTROS; R' Y R" SON H, OH, ALQUILO, CICLOALQUILO, ARILO; R5 ES H, CIANO, OH, HALOGENO, TRIFLUOROMETILO, ENTRE OTROS; R6 ES H, ALQUILO, TRIFLUOROMETILO, ARILO, ENTRE OTROS; R7 ES CO(CH2)mOH, OXO; R2 ES H, ALQUILO, ALCOXI, HALOGENO, CF3; R3 Y R3' SON H, ALQUILO O FORMAN JUNTOS CICLOALQUILO; R4 Y R4' SON H, HALOGENO, CF3, ALQUILO, ALCOXI; R Y R2, R4 Y R4' SON HC=CH-CH=CH OPCIONALMENTE SUSTITUIDO POR ALQUILO HALOGENO, ALCOXI; X ES CONR8, (CH2)pO, NR8CO, ENTRE OTROS; n ES 1-2; m ES 0-4; o Y p SON 1-2. SON COMPUESTOS PREFERIDOS N-(3,5-BIS-TRIFLUOROMETIL-BENCIL)-6-(4-HIDROXIACETIL-PIPERACIN-1-ILO)-N-METIL-4-o-TOLIL-NICOTINAMIDA, N-(3,5-BIS-TRIFLUOROMETIL-BENCIL)-6-CLORO-N-METIL-4-o-TOLIL-NICOTINAMIDA, ENTRE OTROS; TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION. LOS COMPUESTOS SON ANTAGONISTAS DE RECEPTORES DE NEUROQUININA NK-1 Y PUEDEN SER UTILES PARA EL TRATAMIENTO DE ARTRITIS REUMATOIDE, ASMA, ENFERMEDAD INFLAMATORIA DEL INTESTINO, MODULACION DEL SISTEMA NERVIOSO CENTRAL
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP00117003 | 2000-08-08 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20020332A1 true PE20020332A1 (es) | 2002-05-10 |
Family
ID=8169466
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2001000779A PE20020332A1 (es) | 2000-08-08 | 2001-08-06 | Derivados de 4-fenil-piridina como antagonistas de receptores de neuroquinina nk-1 |
Country Status (36)
| Country | Link |
|---|---|
| US (1) | US6770637B2 (es) |
| EP (1) | EP1309559B1 (es) |
| JP (1) | JP4053877B2 (es) |
| KR (1) | KR100518201B1 (es) |
| CN (1) | CN1293056C (es) |
| AR (1) | AR030324A1 (es) |
| AT (1) | ATE328871T1 (es) |
| AU (2) | AU2002212118B2 (es) |
| BR (1) | BR0113173A (es) |
| CA (1) | CA2418868C (es) |
| CZ (1) | CZ2003684A3 (es) |
| DE (1) | DE60120419T2 (es) |
| DK (1) | DK1309559T3 (es) |
| EC (1) | ECSP034475A (es) |
| ES (1) | ES2264706T3 (es) |
| GT (1) | GT200100160A (es) |
| HR (1) | HRP20030055A2 (es) |
| HU (1) | HUP0301671A3 (es) |
| IL (2) | IL154079A0 (es) |
| JO (1) | JO2371B1 (es) |
| MA (1) | MA27680A1 (es) |
| MX (1) | MXPA03001143A (es) |
| MY (1) | MY128993A (es) |
| NO (1) | NO324841B1 (es) |
| NZ (1) | NZ523751A (es) |
| PA (1) | PA8524401A1 (es) |
| PE (1) | PE20020332A1 (es) |
| PL (1) | PL359849A1 (es) |
| PT (1) | PT1309559E (es) |
| RU (1) | RU2277087C2 (es) |
| SI (1) | SI1309559T1 (es) |
| TW (1) | TWI259180B (es) |
| UY (1) | UY26872A1 (es) |
| WO (1) | WO2002016324A1 (es) |
| YU (1) | YU8703A (es) |
| ZA (1) | ZA200300614B (es) |
Families Citing this family (49)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT1103545E (pt) * | 1999-11-29 | 2004-03-31 | Hoffmann La Roche | 2-(3,5-bis-trifluorometil-fenil)-n-metil-n-(6-morfolin-4-il-4-o-totil-piridin-3-il)-isobutiramida |
| EP1688408A3 (en) * | 2002-08-08 | 2007-08-22 | Amgen, Inc | Vanilloid receptor ligands and their use in treatments |
| JP4555082B2 (ja) | 2002-08-08 | 2010-09-29 | アムジエン・インコーポレーテツド | バニロイド受容体リガンドおよびそれの治療での使用 |
| US20070060593A1 (en) * | 2003-06-25 | 2007-03-15 | Kerns Jeffrey K | 4-Carboxamido quinoline derivatives for use as nk-2 and nk-3 |
| CA2530886C (en) * | 2003-07-03 | 2013-05-28 | F. Hoffmann-La Roche Ag | Dual nk1/nk3 antagonists for treating schizophrenia |
| MY139645A (en) | 2004-02-11 | 2009-10-30 | Amgen Inc | Vanilloid receptor ligands and their use in treatments |
| AU2005212438A1 (en) | 2004-02-11 | 2005-08-25 | Amgen Inc. | Vanilloid receptor ligands and their use in treatments |
| KR100881240B1 (ko) * | 2004-07-06 | 2009-02-05 | 에프. 호프만-라 로슈 아게 | Nk-1 수용체 길항제의 합성에 있어서 중간체로서사용되는 카르복스아미드 피리딘 유도체의 제조 방법 |
| ATE500224T1 (de) | 2004-07-06 | 2011-03-15 | Hoffmann La Roche | Herstellungsverfahren für carboxamid-pyridin- derivate als zwischenprodukte bei der synthese von nk-1-rezeptor-antagonisten |
| BRPI0418939A (pt) * | 2004-07-06 | 2008-04-08 | Xenon Pharmaceuticals Inc | derivados de nicotinamida e sua utilização como agentes terapêuticos |
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| PT1103545E (pt) * | 1999-11-29 | 2004-03-31 | Hoffmann La Roche | 2-(3,5-bis-trifluorometil-fenil)-n-metil-n-(6-morfolin-4-il-4-o-totil-piridin-3-il)-isobutiramida |
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