HUP0303443A2 - Eljárás imidazolszármazékok előállítására - Google Patents
Eljárás imidazolszármazékok előállításáraInfo
- Publication number
- HUP0303443A2 HUP0303443A2 HU0303443A HUP0303443A HUP0303443A2 HU P0303443 A2 HUP0303443 A2 HU P0303443A2 HU 0303443 A HU0303443 A HU 0303443A HU P0303443 A HUP0303443 A HU P0303443A HU P0303443 A2 HUP0303443 A2 HU P0303443A2
- Authority
- HU
- Hungary
- Prior art keywords
- methyl
- preparation
- chlorophenyl
- imidazole derivatives
- quinolinone
- Prior art date
Links
- 229940079865 intestinal antiinfectives imidazole derivative Drugs 0.000 title abstract 3
- 238000000034 method Methods 0.000 title abstract 3
- 150000002460 imidazoles Chemical class 0.000 title abstract 2
- -1 5-substituted imidazole Chemical class 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- LXBGSDVWAMZHDD-UHFFFAOYSA-N 2-methyl-1h-imidazole Chemical compound CC1=NC=CN1 LXBGSDVWAMZHDD-UHFFFAOYSA-N 0.000 abstract 1
- 102000007317 Farnesyltranstransferase Human genes 0.000 abstract 1
- 108010007508 Farnesyltranstransferase Proteins 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 230000002349 favourable effect Effects 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- XLSZMDLNRCVEIJ-UHFFFAOYSA-N methylimidazole Natural products CC1=CNC=N1 XLSZMDLNRCVEIJ-UHFFFAOYSA-N 0.000 abstract 1
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- 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
- C07D401/06—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 carbon chain containing only aliphatic carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Epoxy Resins (AREA)
Abstract
A találmány olyan 5-szubsztituált-imidazol-származékok előállításáravonatkozik, amelyeknek farnezil-transzferázt gátló aktivitásuk van,továbbá amelyek felhasználhatók ilyen aktivitást mutató másimdazolszármazékok előállításánál mint köztitermékek. Közelebbről atalálmány tárgya eljárás a (III) képletű 4-(3-klórfenil)-6-[(4-klórfenil)hidroxi(1-metil-lH-imidazol-5-il)metil]-1-metil-2(1H)-kinolinon és gyógyászatilag elfogadható sói előállítására. A találmányértelmében úgy járnak el, hogy a (II) képletű 6-(4-klórbenzoil)-4-(3-klórfenil)-1-metil-2(H)-kinolinont egy, az alkilrészben 6-8 szénatomottartalmazó alkillítiumszármazékkal, 1-metilimidazollal és egy tri(4-6szénatomot tartalmazó)alkilszililhalogeniddel reagáltatják. Atalálmány szerinti eljárás főbb előnyei a magasabb hozamban, nagyobbtisztaságban és az ipari alkalmazhatóság szempontjából kedvezőbbreakcióparaméterekben rejlenek. Ó
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP01200928.8 | 2001-03-12 | ||
EP01200928 | 2001-03-12 | ||
PCT/EP2002/002459 WO2002072574A1 (en) | 2001-03-12 | 2002-03-05 | Process for the preparation of imidazole compounds |
Publications (3)
Publication Number | Publication Date |
---|---|
HUP0303443A2 true HUP0303443A2 (hu) | 2004-01-28 |
HUP0303443A3 HUP0303443A3 (en) | 2012-09-28 |
HU230282B1 HU230282B1 (hu) | 2015-12-28 |
Family
ID=8180004
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HU0303443A HU230282B1 (hu) | 2001-03-12 | 2002-03-05 | Eljárás imidazol-származékok előállítására |
Country Status (32)
Country | Link |
---|---|
US (1) | US6844439B2 (hu) |
EP (1) | EP1373255B1 (hu) |
JP (1) | JP4257698B2 (hu) |
KR (1) | KR100849042B1 (hu) |
CN (1) | CN1246318C (hu) |
AR (1) | AR035944A1 (hu) |
AT (1) | ATE287882T1 (hu) |
AU (1) | AU2002253101B2 (hu) |
BR (1) | BRPI0208075B8 (hu) |
CA (1) | CA2438421C (hu) |
CZ (1) | CZ300622B6 (hu) |
DE (1) | DE60202755T2 (hu) |
DK (1) | DK1373255T3 (hu) |
EA (1) | EA006770B1 (hu) |
EE (1) | EE05247B1 (hu) |
ES (1) | ES2236505T3 (hu) |
HK (1) | HK1063315A1 (hu) |
HR (1) | HRP20030695B1 (hu) |
HU (1) | HU230282B1 (hu) |
IL (2) | IL157839A0 (hu) |
MX (1) | MXPA03008205A (hu) |
MY (1) | MY124838A (hu) |
NO (1) | NO324954B1 (hu) |
NZ (1) | NZ528620A (hu) |
PL (1) | PL208238B1 (hu) |
PT (1) | PT1373255E (hu) |
SI (1) | SI1373255T1 (hu) |
SK (1) | SK287807B6 (hu) |
TW (1) | TWI249532B (hu) |
UA (1) | UA74871C2 (hu) |
WO (1) | WO2002072574A1 (hu) |
ZA (1) | ZA200307117B (hu) |
Families Citing this family (15)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ES2291455T3 (es) | 2001-03-12 | 2008-03-01 | Avanir Pharmaceuticals | Compuestos de bencimidazol para modular ige e inhibir la proliferacion celular. |
TWI276631B (en) | 2002-09-12 | 2007-03-21 | Avanir Pharmaceuticals | Phenyl-aza-benzimidazole compounds for modulating IgE and inhibiting cellular proliferation |
AU2003270426A1 (en) | 2002-09-12 | 2004-04-30 | Avanir Pharmaceuticals | PHENYL-INDOLE COMPOUNDS FOR MODULATING IgE AND INHIBITING CELLULAR PROLIFERATION |
JP2007538004A (ja) * | 2004-03-18 | 2007-12-27 | ザ ブライハム アンド ウイメンズ ホスピタル, インコーポレイテッド | シヌクレイノパチーを治療する方法 |
US7524961B2 (en) | 2004-05-03 | 2009-04-28 | Janssen Pharmaceutica, N.V. | Diastereoselective addition of lithiated N-methylimidazole on sulfinimines |
JP4917022B2 (ja) * | 2004-05-03 | 2012-04-18 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | 6−ブロモ−4−(3−クロロフェニル)−2−メトキシ−キノリンを用いるジアステレオ選択的合成方法 |
ATE397600T1 (de) | 2004-05-03 | 2008-06-15 | Janssen Pharmaceutica Nv | Diastereoselektives syntheseverfahren zur herstellung vn imidazolverbindungen |
EP1968591A4 (en) | 2005-12-23 | 2010-02-17 | Link Medicine Corp | TREATMENT OF SYNUCLEINOPATHIES |
US8232402B2 (en) * | 2008-03-12 | 2012-07-31 | Link Medicine Corporation | Quinolinone farnesyl transferase inhibitors for the treatment of synucleinopathies and other indications |
KR101044430B1 (ko) * | 2009-09-25 | 2011-06-27 | 듀오백코리아 주식회사 | 요추받이를 포함하는 의자의 등 지지 장치 |
KR101107900B1 (ko) * | 2009-10-21 | 2012-01-25 | 성용기업 주식회사 | 의자용 허리지지장치 |
PT3277842T (pt) | 2015-08-17 | 2019-09-05 | Kura Oncology Inc | Métodos de tratamento de doentes com cancro usando inibidores da farnesiltransferase |
EP3838275A1 (en) | 2016-11-03 | 2021-06-23 | Kura Oncology, Inc. | Farnesyltransferase inhibitors for use in methods of treating cancer |
US10954210B2 (en) | 2016-12-08 | 2021-03-23 | Hangzhou Solipharma Co., Ltd. | Crystal form of tipifarnib and preparation method and pharmaceutical composition thereof |
AU2019270163A1 (en) * | 2018-05-18 | 2020-12-03 | Kura Oncology, Inc. | Synthesis of tipifarnib |
Family Cites Families (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
TW349948B (en) | 1995-10-31 | 1999-01-11 | Janssen Pharmaceutica Nv | Farnesyl transferase inhibiting 2-quinolone derivatives |
SI1162201T1 (sl) * | 1995-12-08 | 2006-08-31 | Janssen Pharmaceutica Nv | (Imidazol-5-il)metil-2-kinolinonski derivati kot inhibitorji farnezil protein transferaze |
TW591030B (en) | 1997-03-10 | 2004-06-11 | Janssen Pharmaceutica Nv | Farnesyl transferase inhibiting 1,8-annelated quinolinone derivatives substituted with N- or C-linked imidazoles |
CA2288140C (en) | 1997-04-25 | 2007-04-03 | Janssen Pharmaceutica N.V. | Farnesyltransferase inhibiting quinazolinones |
JP3495706B2 (ja) * | 1998-08-27 | 2004-02-09 | ファイザー・プロダクツ・インク | 抗癌薬として有用なアルキニル置換キノリン−2−オン誘導体 |
ES2237125T3 (es) | 1998-08-27 | 2005-07-16 | Pfizer Products Inc. | Derivados de quinolin-2-ona utiles como agentes anticancerigenos. |
-
2002
- 2002-03-05 JP JP2002571490A patent/JP4257698B2/ja not_active Expired - Lifetime
- 2002-03-05 EA EA200300998A patent/EA006770B1/ru not_active IP Right Cessation
- 2002-03-05 CZ CZ20032704A patent/CZ300622B6/cs not_active IP Right Cessation
- 2002-03-05 CN CNB02806335XA patent/CN1246318C/zh not_active Expired - Lifetime
- 2002-03-05 BR BRPI0208075-3 patent/BRPI0208075B8/pt not_active IP Right Cessation
- 2002-03-05 DE DE60202755T patent/DE60202755T2/de not_active Expired - Lifetime
- 2002-03-05 HU HU0303443A patent/HU230282B1/hu unknown
- 2002-03-05 SI SI200230100T patent/SI1373255T1/xx unknown
- 2002-03-05 AU AU2002253101A patent/AU2002253101B2/en not_active Expired
- 2002-03-05 EE EEP200300442A patent/EE05247B1/xx unknown
- 2002-03-05 DK DK02722184T patent/DK1373255T3/da active
- 2002-03-05 MX MXPA03008205A patent/MXPA03008205A/es active IP Right Grant
- 2002-03-05 WO PCT/EP2002/002459 patent/WO2002072574A1/en active IP Right Grant
- 2002-03-05 PL PL363263A patent/PL208238B1/pl unknown
- 2002-03-05 ES ES02722184T patent/ES2236505T3/es not_active Expired - Lifetime
- 2002-03-05 KR KR1020037010091A patent/KR100849042B1/ko active IP Right Grant
- 2002-03-05 NZ NZ528620A patent/NZ528620A/en not_active IP Right Cessation
- 2002-03-05 US US10/471,215 patent/US6844439B2/en not_active Expired - Lifetime
- 2002-03-05 SK SK1246-2003A patent/SK287807B6/sk unknown
- 2002-03-05 IL IL15783902A patent/IL157839A0/xx unknown
- 2002-03-05 EP EP02722184A patent/EP1373255B1/en not_active Expired - Lifetime
- 2002-03-05 AT AT02722184T patent/ATE287882T1/de active
- 2002-03-05 CA CA2438421A patent/CA2438421C/en not_active Expired - Lifetime
- 2002-03-05 PT PT02722184T patent/PT1373255E/pt unknown
- 2002-03-11 AR ARP020100873A patent/AR035944A1/es active IP Right Grant
- 2002-03-11 TW TW091104444A patent/TWI249532B/zh not_active IP Right Cessation
- 2002-03-11 MY MYPI20020866A patent/MY124838A/en unknown
- 2002-05-03 UA UA2003087776A patent/UA74871C2/uk unknown
-
2003
- 2003-09-01 HR HR20030695A patent/HRP20030695B1/xx not_active IP Right Cessation
- 2003-09-10 IL IL157839A patent/IL157839A/en unknown
- 2003-09-10 NO NO20034003A patent/NO324954B1/no not_active IP Right Cessation
- 2003-09-11 ZA ZA200307117A patent/ZA200307117B/en unknown
-
2004
- 2004-08-12 HK HK04106065A patent/HK1063315A1/xx not_active IP Right Cessation
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Legal Events
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TK4A | Correction of change of decision |