PE20020272A1 - N-oxidos de derivados de 4-fenil-piridina como prodrogas de los antagonistas del receptor de neuroquinina 1 (nk-1) - Google Patents
N-oxidos de derivados de 4-fenil-piridina como prodrogas de los antagonistas del receptor de neuroquinina 1 (nk-1)Info
- Publication number
- PE20020272A1 PE20020272A1 PE2001000704A PE2001000704A PE20020272A1 PE 20020272 A1 PE20020272 A1 PE 20020272A1 PE 2001000704 A PE2001000704 A PE 2001000704A PE 2001000704 A PE2001000704 A PE 2001000704A PE 20020272 A1 PE20020272 A1 PE 20020272A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- phenyl
- trifluoromethyl
- oxides
- pyridine derivatives
- Prior art date
Links
- 150000005362 4-phenylpyridines Chemical class 0.000 title abstract 3
- 239000002464 receptor antagonist Substances 0.000 title abstract 2
- 229940044551 receptor antagonist Drugs 0.000 title abstract 2
- 229940002612 prodrug Drugs 0.000 title 1
- 239000000651 prodrug Substances 0.000 title 1
- -1 3,5-BIS-TRIFLUORomethyl-BENZYL Chemical class 0.000 abstract 2
- WZKSXHQDXQKIQJ-UHFFFAOYSA-N F[C](F)F Chemical class F[C](F)F WZKSXHQDXQKIQJ-UHFFFAOYSA-N 0.000 abstract 2
- 239000002253 acid Substances 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical class [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 1
- 208000006673 asthma Diseases 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- QUPDWYMUPZLYJZ-UHFFFAOYSA-N ethyl Chemical class C[CH2] QUPDWYMUPZLYJZ-UHFFFAOYSA-N 0.000 abstract 1
- 230000004968 inflammatory condition Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 206010039073 rheumatoid arthritis Diseases 0.000 abstract 1
- 150000003512 tertiary amines Chemical class 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
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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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
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- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—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
- 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
- C07D401/12—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
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Immunology (AREA)
- Pain & Pain Management (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Addiction (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Ophthalmology & Optometry (AREA)
- Otolaryngology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
Abstract
SE REFIERE A N-OXIDOS DE DERIVADOS DE 4-FENIL-PIRIDINA DE FORMULA I DONDE R ES H, ALQUILO, ALCOXILO, HALOGENO, TRIFLUOROMETILO; R1 ES H, HALO; R Y R1 PUEDEN ESTAR JUNTOS CON LOS ATOMOS DE CARBONO DEL ANILLO A LOS QUE ESTAN UNIDOS -CH=CH-CH=CH-; R2 Y R2' SON H, HALOGENO, TRIFLUOROMETILO, ALCOXILO, CIANO; R3 Y R3' SON H, ALQUILO, CICLOALQUILO; R4 Y R4' SON -(CH2)mOR6, ALQUILO; R4 Y R4' FORMAN JUNTO CON EL ATOMO DE N AL QUE ESTAN UNIDOS UNA AMINA TERCIARIA CICLICA DEL GRUPO a ; R5 ES H, OH, ALQUILO, ENTRE OTROS; R6 ES H, ALQUILO, FENILO; X ES -C(O)N(R6)-, ENTRE OTROS; n ES 0-4; m ES 1-3. SON COMPUESTOS PREFERIDOS ESTER TERC-BUTILICO DEL ACIDO 4-{5-[(3,5-BIS-TRIFLUOROMETIL-BENCIL)-METIL-CARBAMOIL-4-o-TOLIL-PIRIDIN-2-IL}-4-OXI-PIPERAZIN-1-CARBOXILICO, ESTER ETILICO DEL ACIDO 5'-[(3,5-BIS-TRIFLUOROMETIL-BENCIL)-METIL-CARBAMOIL-4-o-TOLIL-1-OXI-3,4,5,6-TETRAHIDRO-2H-[1,2']PIRIDINIL-4-CARBOXILICO, ENTRE OTROS. SE REFIERE TAMBIEN A UN PROCESO PARA LA PREPARACION. LOS N-OXIDOS DE DERIVADOS DE 4-FENIL-PIRIDINA COMO PRODROGAS DE LOS ANTAGONISTAS DEL RECEPTOR DE NEUROQUININA 1 (NK-1) SON UTILES PARA EL TRATAMIENTO DE CONDICIONES INFLAMATORIAS, MIGRANA, ARTRITIS REUMATOIDEA, ASMA
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP00115287 | 2000-07-14 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20020272A1 true PE20020272A1 (es) | 2002-04-16 |
Family
ID=8169262
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2001000704A PE20020272A1 (es) | 2000-07-14 | 2001-07-13 | N-oxidos de derivados de 4-fenil-piridina como prodrogas de los antagonistas del receptor de neuroquinina 1 (nk-1) |
Country Status (38)
| Country | Link |
|---|---|
| US (4) | US6593472B2 (es) |
| EP (1) | EP1303490B1 (es) |
| JP (1) | JP3950044B2 (es) |
| KR (1) | KR100501608B1 (es) |
| CN (1) | CN1178917C (es) |
| AR (1) | AR029717A1 (es) |
| AT (1) | ATE400556T1 (es) |
| AU (1) | AU7061901A (es) |
| BR (1) | BRPI0112475B8 (es) |
| CA (1) | CA2415890C (es) |
| CY (1) | CY1108557T1 (es) |
| CZ (1) | CZ303639B6 (es) |
| DE (1) | DE60134749D1 (es) |
| DK (1) | DK1303490T3 (es) |
| EC (1) | ECSP034431A (es) |
| EG (1) | EG24968A (es) |
| ES (1) | ES2309075T3 (es) |
| GT (1) | GT200100137A (es) |
| HR (1) | HRP20030003B1 (es) |
| HU (1) | HU230316B1 (es) |
| IL (2) | IL153834A0 (es) |
| JO (1) | JO2372B1 (es) |
| MA (1) | MA26929A1 (es) |
| ME (1) | ME01311B (es) |
| MX (1) | MXPA03000366A (es) |
| MY (1) | MY154976A (es) |
| NO (1) | NO324700B1 (es) |
| NZ (1) | NZ523273A (es) |
| PA (1) | PA8522001A1 (es) |
| PE (1) | PE20020272A1 (es) |
| PL (1) | PL205207B1 (es) |
| PT (1) | PT1303490E (es) |
| RS (1) | RS50932B (es) |
| RU (1) | RU2266284C2 (es) |
| SI (1) | SI1303490T1 (es) |
| UY (1) | UY26839A1 (es) |
| WO (1) | WO2002006236A1 (es) |
| ZA (1) | ZA200210207B (es) |
Families Citing this family (43)
| 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 |
| RS50932B (sr) * | 2000-07-14 | 2010-08-31 | F. Hoffmann-La Roche Ag. | N-oksidi kao prolekovi 4-fenil-piridinskih derivata koji su antagonisti nk1 receptora |
| TWI287003B (en) * | 2000-07-24 | 2007-09-21 | Hoffmann La Roche | 4-phenyl-pyridine derivatives |
| DK1385577T3 (da) * | 2001-04-23 | 2006-08-21 | Hoffmann La Roche | Anvendelse af NK-1-receptorantagonister mod godartet prostatahyperplasi |
| JP4490421B2 (ja) * | 2003-07-03 | 2010-06-23 | エフ．ホフマン−ラ ロシュ アーゲー | 統合失調症を処置するデュアルｎｋ１／ｎｋ３アンタゴニスト |
| CN1984891B (zh) | 2004-07-06 | 2012-08-08 | 弗·哈夫曼-拉罗切有限公司 | 用作合成nk-1受体拮抗剂的中间体的甲酰胺吡啶衍生物的制备方法 |
| US20060030600A1 (en) * | 2004-08-06 | 2006-02-09 | Patrick Schnider | Dual NK1/NK3 receptor antagonists for the treatment of schizophrenia |
| EP2281556A1 (en) | 2005-02-25 | 2011-02-09 | F. Hoffmann-La Roche AG | Tablets with improved drugs substance dispersibility |
| BRPI0609699A2 (pt) * | 2005-03-23 | 2010-04-20 | Hoffmann La Roche | metabolitos para antatonistas de nk-1 para êmese |
| JP2008280248A (ja) * | 2005-11-02 | 2008-11-20 | Eisai R & D Management Co Ltd | アルツハイマー型痴呆症治療薬塩酸ドネペジルのプロドラッグ |
| 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-) |
| GB0808747D0 (en) | 2008-05-14 | 2008-06-18 | Glaxo Wellcome Mfg Pte Ltd | Novel compounds |
| US8966414B2 (en) | 2009-05-29 | 2015-02-24 | Cypress Semiconductor Corporation | Implementing a circuit using an integrated circuit including parametric analog elements |
| US9858367B1 (en) * | 2009-08-31 | 2018-01-02 | Cypress Semiconductor Corporation | Integrated circuit including parametric analog elements |
| EP2722045B1 (en) | 2009-11-18 | 2016-07-06 | Helsinn Healthcare SA | Compositions for treating centrally mediated nausea and vomiting |
| RS53491B1 (sr) | 2009-11-18 | 2015-02-27 | Helsinn Healthcare Sa | Kompozicije za lečenje centralno posredovane mučnine i povraćanja |
| PT2744497T (pt) | 2011-10-18 | 2016-07-18 | Helsinn Healthcare Sa | Combinações terapêuticas de antiemético e quimioterapia induzida |
| US8426450B1 (en) | 2011-11-29 | 2013-04-23 | Helsinn Healthcare Sa | Substituted 4-phenyl pyridines having anti-emetic effect |
| WO2013102145A1 (en) | 2011-12-28 | 2013-07-04 | Global Blood Therapeutics, Inc. | Substituted heteroaryl aldehyde compounds and methods for their use in increasing tissue oxygenation |
| AP2014007805A0 (en) | 2011-12-28 | 2014-07-31 | Cytokinetics Inc The Regents Of The University Of California | Substituted benzaldehyde compounds and methods fortheir use in increasing tissue oxygenation |
| ES2852054T3 (es) | 2013-03-15 | 2021-09-10 | Global Blood Therapeutics Inc | Compuestos y usos de los mismos para la modulación de hemoglobina |
| AP2015008718A0 (en) | 2013-03-15 | 2015-09-30 | Global Blood Therapeutics Inc | Compounds and uses thereof for the modulation of hemoglobin |
| US8952171B2 (en) | 2013-03-15 | 2015-02-10 | Global Blood Therapeutics, Inc. | Compounds and uses thereof for the modulation of hemoglobin |
| US10266551B2 (en) | 2013-03-15 | 2019-04-23 | Global Blood Therapeutics, Inc. | Compounds and uses thereof for the modulation of hemoglobin |
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| US9604999B2 (en) | 2013-03-15 | 2017-03-28 | Global Blood Therapeutics, Inc. | Compounds and uses thereof for the modulation of hemoglobin |
| US9802900B2 (en) | 2013-03-15 | 2017-10-31 | Global Blood Therapeutics, Inc. | Bicyclic heteroaryl compounds and uses thereof for the modulation of hemoglobin |
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| RU2673084C2 (ru) | 2013-11-08 | 2018-11-22 | Киссеи Фармасьютикал Ко., Лтд. | Производное карбоксиметилпиперидина |
| EA201992707A1 (ru) | 2013-11-18 | 2020-06-30 | Глобал Блад Терапьютикс, Инк. | Соединения и их применения для модуляции гемоглобина |
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| TWI649307B (zh) | 2014-05-07 | 2019-02-01 | 日商橘生藥品工業股份有限公司 | Cyclohexylpyridine derivative |
| CN106588899B (zh) * | 2015-10-15 | 2019-11-15 | 江苏恒瑞医药股份有限公司 | 吡啶基取代的6-氧杂螺[4.5]癸烷类衍生物、其制备方法及其在医药上的应用 |
| SG10201912511WA (en) | 2015-12-04 | 2020-02-27 | Global Blood Therapeutics Inc | Dosing regimens for 2-hydroxy-6-((2-(1-isopropyl-1h-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde |
| TWI752307B (zh) | 2016-05-12 | 2022-01-11 | 美商全球血液治療公司 | 新穎化合物及製造化合物之方法 |
| TWI778983B (zh) | 2016-10-12 | 2022-10-01 | 美商全球血液治療公司 | 包含2-羥基-6-((2-(1-異丙基-1h-吡唑-5-基)吡啶-3-基)甲氧基)-苯甲醛之片劑 |
| IL312486B2 (en) | 2017-04-10 | 2025-05-01 | Chase Therapeutics Corp | NK1 antagonist combination and method for treating synucleinopathies |
| EA202090180A1 (ru) | 2017-06-30 | 2020-05-26 | Чейс Терапьютикс Корпорейшн | Композиции nk1-антагониста и способы лечения депрессии |
| US11014884B2 (en) | 2018-10-01 | 2021-05-25 | Global Blood Therapeutics, Inc. | Modulators of hemoglobin |
| US12479816B2 (en) | 2019-02-08 | 2025-11-25 | University of Pittsburgh—of the Commonwealth System of Higher Education | 20-HETE formation inhibitors |
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| JPS56106286A (en) | 1980-01-28 | 1981-08-24 | Nippon Musical Instruments Mfg | Electronic musical instrument |
| EP0103545A3 (en) | 1982-09-13 | 1984-10-03 | Arc Technologies Systems, Ltd. | Electrode for arc furnaces |
| IL111960A (en) | 1993-12-17 | 1999-12-22 | Merck & Co Inc | Morpholines and thiomorpholines their preparation and pharmaceutical compositions containing them |
| KR100286412B1 (ko) | 1993-12-29 | 2001-04-16 | 더블유. 지. 콜 | 치환된 모르폴린 유도체, 이의 제조방법 및 이를 포함하는 약제학적 조성물 |
| IL112778A0 (en) | 1994-03-04 | 1995-05-26 | Merck & Co Inc | Substituted heterocycles, their preparation and pharmaceutical compositions containing them |
| DE19627431A1 (de) * | 1996-07-08 | 1998-01-15 | Bayer Ag | Heterocyclisch kondensierte Pyridine |
| AR008789A1 (es) * | 1996-07-31 | 2000-02-23 | Bayer Corp | Piridinas y bifenilos substituidos |
| 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. |
| WO2000050398A2 (en) * | 1999-02-24 | 2000-08-31 | F. Hoffmann-La Roche Ag | Phenyl- and pyridinyl derivatives as neurokinin 1 antagonists |
| BR0008494A (pt) * | 1999-02-24 | 2002-02-05 | Hoffmann La Roche | Derivados de 3-fenilpiridina e seu uso como antagonista do receptor de nk-1 |
| 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 |
| RS50932B (sr) * | 2000-07-14 | 2010-08-31 | F. Hoffmann-La Roche Ag. | N-oksidi kao prolekovi 4-fenil-piridinskih derivata koji su antagonisti nk1 receptora |
| US20030083345A1 (en) * | 2001-07-10 | 2003-05-01 | Torsten Hoffmann | Method of treatment and/or prevention of brain, spinal or nerve injury |
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