JP2004504301A5 - - Google Patents
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- Publication number
- JP2004504301A5 JP2004504301A5 JP2002512140A JP2002512140A JP2004504301A5 JP 2004504301 A5 JP2004504301 A5 JP 2004504301A5 JP 2002512140 A JP2002512140 A JP 2002512140A JP 2002512140 A JP2002512140 A JP 2002512140A JP 2004504301 A5 JP2004504301 A5 JP 2004504301A5
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- oxy
- tolyl
- trifluoromethyl
- morpholin
- 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.)
- Granted
Links
- -1 cyclic tertiary amine Chemical class 0.000 claims 22
- 150000001875 compounds Chemical class 0.000 claims 15
- 125000000217 alkyl group Chemical group 0.000 claims 7
- 229910052739 hydrogen Inorganic materials 0.000 claims 7
- 239000001257 hydrogen Substances 0.000 claims 7
- 150000002431 hydrogen Chemical group 0.000 claims 5
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 102000002002 Neurokinin-1 Receptors Human genes 0.000 claims 3
- 108010040718 Neurokinin-1 Receptors Proteins 0.000 claims 3
- 239000002253 acid Substances 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 229940047889 isobutyramide Drugs 0.000 claims 3
- 239000002464 receptor antagonist Substances 0.000 claims 3
- 229940044551 receptor antagonist Drugs 0.000 claims 3
- 125000004182 2-chlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(*)C([H])=C1[H] 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 229960003966 nicotinamide Drugs 0.000 claims 2
- 239000011570 nicotinamide Substances 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 1
- 125000002927 2-methoxybenzyl group Chemical group [H]C1=C([H])C([H])=C(C(OC([H])([H])[H])=C1[H])C([H])([H])* 0.000 claims 1
- WFKAJVHLWXSISD-UHFFFAOYSA-N anhydrous dimethyl-acetamide Natural products CC(C)C(N)=O WFKAJVHLWXSISD-UHFFFAOYSA-N 0.000 claims 1
- 150000001721 carbon Chemical group 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- KVNIEWQWLOMTMV-UHFFFAOYSA-N n-[(2-chloro-5-methoxyphenyl)methyl]-n-methyl-4-(2-methylphenyl)-6-morpholin-4-ylpyridine-3-carboxamide Chemical compound COC1=CC=C(Cl)C(CN(C)C(=O)C=2C(=CC(=NC=2)N2CCOCC2)C=2C(=CC=CC=2)C)=C1 KVNIEWQWLOMTMV-UHFFFAOYSA-N 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 239000007800 oxidant agent Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 229940002612 prodrug Drugs 0.000 claims 1
- 239000000651 prodrug Substances 0.000 claims 1
- DLFVBJFMPXGRIB-UHFFFAOYSA-N thioacetamide Natural products CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP00115287 | 2000-07-14 | ||
| PCT/EP2001/007850 WO2002006236A1 (en) | 2000-07-14 | 2001-07-09 | N-oxides as nk1 receptor antagonist prodrugs of 4-phenyl-pyridine derivatives |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2004504301A JP2004504301A (ja) | 2004-02-12 |
| JP2004504301A5 true JP2004504301A5 (enExample) | 2005-02-03 |
| JP3950044B2 JP3950044B2 (ja) | 2007-07-25 |
Family
ID=8169262
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2002512140A Expired - Lifetime JP3950044B2 (ja) | 2000-07-14 | 2001-07-09 | Ｎｋ１受容体拮抗物質プロドラッグとしての４−フェニル−ピリジン誘導体のｎ−オキシド |
Country Status (38)
Families Citing this family (43)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1103545B1 (en) * | 1999-11-29 | 2003-11-05 | F. Hoffmann-La Roche Ag | 2-(3,5-Bis-trifluoromethyl-phenyl)-N-methyl-N-(6-morpholin-4-yl-4-o-tolyl-pyridin-3-yl)-isobutyramide |
| CN1178917C (zh) * | 2000-07-14 | 2004-12-08 | 弗·哈夫曼-拉罗切有限公司 | 作为nk1受体拮抗剂前药的4-苯基-吡啶衍生物的n-氧化物 |
| TWI287003B (en) * | 2000-07-24 | 2007-09-21 | Hoffmann La Roche | 4-phenyl-pyridine derivatives |
| 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. |
| HRP20070471T3 (hr) | 2003-07-03 | 2007-11-30 | F. Hoffmann - La Roche Ag | Dvojni nk1/nk3 antagonisti za liječenje shizofrenije |
| 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. |
| US20060030600A1 (en) * | 2004-08-06 | 2006-02-09 | Patrick Schnider | Dual NK1/NK3 receptor antagonists for the treatment of schizophrenia |
| NZ560232A (en) | 2005-02-25 | 2010-11-26 | Hoffmann La Roche | Tablets with improved drug substance dispersibility |
| DK1863767T3 (da) * | 2005-03-23 | 2009-05-04 | Hoffmann La Roche | Metabolitter til NK-I-antagonister til emesis |
| 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 |
| JP2010516731A (ja) | 2007-01-24 | 2010-05-20 | グラクソ グループ リミテッド | ２−メトキシ−５−（５−トリフルオロメチル−テトラゾール−１−イル）−ベンジル］−（２ｓ−フェニル−ピペリジン−３ｓ−イル）−アミンを含む医薬組成物 |
| 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 |
| CN106512010A (zh) | 2009-11-18 | 2017-03-22 | 赫尔辛医疗股份公司 | 用于治疗中枢介导的恶心及呕吐的组合物及方法 |
| EP2722045B1 (en) | 2009-11-18 | 2016-07-06 | Helsinn Healthcare SA | Compositions for treating centrally mediated nausea and vomiting |
| EP2744497B1 (en) | 2011-10-18 | 2016-04-06 | Helsinn Healthcare SA | Therapeutic combinations of netupitant and palonosetron |
| US8426450B1 (en) * | 2011-11-29 | 2013-04-23 | Helsinn Healthcare Sa | Substituted 4-phenyl pyridines having anti-emetic effect |
| DK3738434T3 (da) | 2011-12-28 | 2023-12-04 | Global Blood Therapeutics Inc | Mellemprodukter til opnåelse af substituerede benzaldehydforbindelser og fremgangsmåder til anvendelse deraf ved øgning af vævsoxygenering |
| 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 |
| BR112015021982B1 (pt) * | 2013-03-15 | 2022-12-13 | Global Blood Therapeutics, Inc | Compostos e seus usos para a modulação de hemoglobina |
| AU2014237330A1 (en) | 2013-03-15 | 2015-09-17 | Global Blood Therapeutics, Inc. | Compounds and uses thereof for the modulation of hemoglobin |
| KR102280614B1 (ko) | 2013-03-15 | 2021-07-21 | 글로벌 블러드 테라퓨틱스, 인크. | 헤모글로빈 조정을 위한 화합물 및 이의 용도 |
| 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 |
| 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 |
| US9458139B2 (en) | 2013-03-15 | 2016-10-04 | Global Blood Therapeutics, Inc. | Compounds and uses thereof for the modulation of hemoglobin |
| US9422279B2 (en) | 2013-03-15 | 2016-08-23 | Global Blood Therapeutics, Inc. | Compounds and uses thereof for the modulation of hemoglobin |
| US10100043B2 (en) | 2013-03-15 | 2018-10-16 | Global Blood Therapeutics, Inc. | Substituted aldehyde compounds and methods for their use in increasing tissue oxygenation |
| BR112016009811A2 (pt) | 2013-11-08 | 2017-12-05 | Kissei Pharmaceutical | derivado de carboximetil piperidina |
| EA201992707A1 (ru) | 2013-11-18 | 2020-06-30 | Глобал Блад Терапьютикс, Инк. | Соединения и их применения для модуляции гемоглобина |
| US10350098B2 (en) * | 2013-12-20 | 2019-07-16 | Volcano Corporation | Devices and methods for controlled endoluminal filter deployment |
| SI3102208T2 (sl) | 2014-02-07 | 2024-10-30 | Global Blood Therapeutics, Inc. | Kristalinični polimorf proste baze 2-hidroksi-6-((2-(1-izopropil-1H-pirazol-5-IL)piridin-3-IL)metoksi)- benzaldehida |
| 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 |
| US11020382B2 (en) | 2015-12-04 | 2021-06-01 | Global Blood Therapeutics, Inc. | Dosing regimens for 2-hydroxy-6-((2-(1-isopropyl-1h-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde |
| AR108435A1 (es) | 2016-05-12 | 2018-08-22 | Global Blood Therapeutics Inc | Proceso para sintetizar 2-hidroxi-6-((2-(1-isopropil-1h-pirazol-5-il)-piridin-3-il)metoxi)benzaldehído |
| 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 |
| IL271464B2 (en) | 2017-06-30 | 2024-08-01 | Chase Therapeutics Corp | NK-1 antagonist compositions and methods for use in the treatment of depression |
| EP3860975B1 (en) | 2018-10-01 | 2023-10-18 | Global Blood Therapeutics, Inc. | Modulators of hemoglobin for the treatment of sickle cell disease |
| WO2020163689A1 (en) | 2019-02-08 | 2020-08-13 | University Of Pittsburgh - Of The Commonwealth System Of Higher Education | 20-hete formation inhibitors |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| DE69434063D1 (de) | 1993-12-29 | 2004-11-11 | Merck Sharp & Dohme | Substituierte Morpholinderivate und ihre Verwendung als therapeutische Mittel |
| 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 |
| EP1157005B1 (en) * | 1999-02-24 | 2004-10-20 | F. Hoffmann-La Roche Ag | 3-phenylpyridine derivatives and their use as nk-1 receptor antagonists |
| WO2000050398A2 (en) * | 1999-02-24 | 2000-08-31 | F. Hoffmann-La Roche Ag | Phenyl- and pyridinyl derivatives as neurokinin 1 antagonists |
| DK1394150T3 (da) * | 1999-02-24 | 2011-03-21 | Hoffmann La Roche | 4-phenylpyridinderivater og deres anvendelse som NK-1-receptorantagonister |
| EP1103545B1 (en) * | 1999-11-29 | 2003-11-05 | F. Hoffmann-La Roche Ag | 2-(3,5-Bis-trifluoromethyl-phenyl)-N-methyl-N-(6-morpholin-4-yl-4-o-tolyl-pyridin-3-yl)-isobutyramide |
| CN1178917C (zh) * | 2000-07-14 | 2004-12-08 | 弗·哈夫曼-拉罗切有限公司 | 作为nk1受体拮抗剂前药的4-苯基-吡啶衍生物的n-氧化物 |
| US20030083345A1 (en) * | 2001-07-10 | 2003-05-01 | Torsten Hoffmann | Method of treatment and/or prevention of brain, spinal or nerve injury |
-
2001
- 2001-07-09 CN CNB018128246A patent/CN1178917C/zh not_active Expired - Lifetime
- 2001-07-09 CZ CZ20030428A patent/CZ303639B6/cs not_active IP Right Cessation
- 2001-07-09 DE DE60134749T patent/DE60134749D1/de not_active Expired - Lifetime
- 2001-07-09 SI SI200130848T patent/SI1303490T1/sl unknown
- 2001-07-09 AU AU7061901A patent/AU7061901A/xx active Pending
- 2001-07-09 EP EP01949475A patent/EP1303490B1/en not_active Expired - Lifetime
- 2001-07-09 AT AT01949475T patent/ATE400556T1/de active
- 2001-07-09 PT PT01949475T patent/PT1303490E/pt unknown
- 2001-07-09 KR KR10-2003-7000476A patent/KR100501608B1/ko not_active Expired - Lifetime
- 2001-07-09 NZ NZ523273A patent/NZ523273A/en not_active IP Right Cessation
- 2001-07-09 WO PCT/EP2001/007850 patent/WO2002006236A1/en not_active Ceased
- 2001-07-09 HU HU0301311A patent/HU230316B1/hu unknown
- 2001-07-09 IL IL15383401A patent/IL153834A0/xx unknown
- 2001-07-09 MX MXPA03000366A patent/MXPA03000366A/es active IP Right Grant
- 2001-07-09 PL PL365684A patent/PL205207B1/pl unknown
- 2001-07-09 BR BRPI0112475A patent/BRPI0112475B8/pt not_active IP Right Cessation
- 2001-07-09 JP JP2002512140A patent/JP3950044B2/ja not_active Expired - Lifetime
- 2001-07-09 ES ES01949475T patent/ES2309075T3/es not_active Expired - Lifetime
- 2001-07-09 RU RU2003102612/04A patent/RU2266284C2/ru active
- 2001-07-09 ME MEP-2008-770A patent/ME01311B/me unknown
- 2001-07-09 DK DK01949475T patent/DK1303490T3/da active
- 2001-07-09 HR HR20030003A patent/HRP20030003B1/xx not_active IP Right Cessation
- 2001-07-09 RS YUP-6/03A patent/RS50932B/sr unknown
- 2001-07-09 CA CA002415890A patent/CA2415890C/en not_active Expired - Lifetime
- 2001-07-10 JO JO2001106A patent/JO2372B1/en active
- 2001-07-11 EG EG2001070771A patent/EG24968A/xx active
- 2001-07-11 PA PA20018522001A patent/PA8522001A1/es unknown
- 2001-07-12 MY MYPI20013310A patent/MY154976A/en unknown
- 2001-07-12 US US09/904,059 patent/US6593472B2/en not_active Expired - Lifetime
- 2001-07-12 GT GT200100137A patent/GT200100137A/es unknown
- 2001-07-13 AR ARP010103335A patent/AR029717A1/es active IP Right Grant
- 2001-07-13 PE PE2001000704A patent/PE20020272A1/es active IP Right Grant
- 2001-07-13 UY UY26839A patent/UY26839A1/es not_active IP Right Cessation
-
2002
- 2002-12-17 ZA ZA200210207A patent/ZA200210207B/en unknown
-
2003
- 2003-01-07 US US10/337,543 patent/US6747026B2/en not_active Expired - Lifetime
- 2003-01-07 IL IL153834A patent/IL153834A/en active IP Right Grant
- 2003-01-13 NO NO20030154A patent/NO324700B1/no not_active IP Right Cessation
- 2003-01-13 MA MA26997A patent/MA26929A1/fr unknown
- 2003-01-14 EC EC2003004431A patent/ECSP034431A/es unknown
- 2003-07-09 US US10/616,276 patent/US6897226B2/en not_active Expired - Lifetime
- 2003-08-21 US US10/645,895 patent/US6806370B2/en not_active Expired - Lifetime
-
2008
- 2008-10-07 CY CY20081101108T patent/CY1108557T1/el unknown