HUP0001050A2 - Gombaellenes hatású, azolgyűrűt tartalmazó aminosav-észterek, eljárás előállításukra, az ezeket tartalmazó gyógyszerkészítmények és intermedierjeik - Google Patents
Gombaellenes hatású, azolgyűrűt tartalmazó aminosav-észterek, eljárás előállításukra, az ezeket tartalmazó gyógyszerkészítmények és intermedierjeikInfo
- Publication number
- HUP0001050A2 HUP0001050A2 HU0001050A HUP0001050A HUP0001050A2 HU P0001050 A2 HUP0001050 A2 HU P0001050A2 HU 0001050 A HU0001050 A HU 0001050A HU P0001050 A HUP0001050 A HU P0001050A HU P0001050 A2 HUP0001050 A2 HU P0001050A2
- Authority
- HU
- Hungary
- Prior art keywords
- general formula
- group
- intermediates
- compounds
- amino acid
- Prior art date
Links
- 229940121375 antifungal agent Drugs 0.000 title abstract 2
- 239000003814 drug Substances 0.000 title abstract 2
- 239000000543 intermediate Substances 0.000 title abstract 2
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 title 2
- -1 Amino acid ester Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- 239000002253 acid Substances 0.000 abstract 2
- 230000000843 anti-fungal effect Effects 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 241001480043 Arthrodermataceae Species 0.000 abstract 1
- 201000007336 Cryptococcosis Diseases 0.000 abstract 1
- 241000221204 Cryptococcus neoformans Species 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 125000000815 N-oxide group Chemical group 0.000 abstract 1
- 239000004480 active ingredient Substances 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 150000001413 amino acids Chemical class 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 238000001990 intravenous administration Methods 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 244000052769 pathogen Species 0.000 abstract 1
- 230000001717 pathogenic effect Effects 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/10—Antimycotics
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- 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
Abstract
A találmány az (I) általános képletű új vegyületekre, azok N-oxidalakjaira, gyógyászati szempontból elfogadható savaddíciós sóikra éssztereokémiai izomer formáikra vonatkozik, ahol az (I) általánosképletben -A-B-jelentése -N=CH- (a), -CH=N- (b), -CH=CH- (c) képletű kétvegyértékű csoport, ahol az (a) és (b) csoportokban egy hidrogénatomot1-6 szénatomos alkilcsoport helyettesíthet; és a (c) képletűcsoportban egy vagy két hidrogénatomot 1-6 szénatomos alkilcsoporthelyettesíthet; L jelentése egy aminosav acilegysége; D jelentése (D1) vagy (D2) általános képletű csoport, ahol X jelentésenitrogénatom vagy CH-csoport; R1 jelentése halogénatom; és R2 jelentése hidrogén- vagy halogénatom. A találmány új vegyületekelőállítására, e vegyületeket tartalmazó gyógyászati készítményekre ésezek gyógyszerként való alkalmazására, valamint a (II) általánosképletű intermedierekre is kiterjed. A találmány szerinti (I)általános képletű hatóanyagok gombaellenes hatással rendelkeznek.Előnyük, hogy savaddíciós sóik vízben vagy vizes keverékekben mutatottoldhatósága az eddig ismert származékokénál nagyobb, és így intravénásalkalmazásra is megfelelők. A találmány szerinti (I) általános képletűvegyületek gombaellenes hatásosságát különböző dermatofita gombákkalszemben, valamint Cryptococcus neoformans<> kórokozóval szembenigazolták. Ó
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP97200374 | 1997-02-11 | ||
| EP97203228 | 1997-10-15 | ||
| PCT/EP1998/000646 WO1998034934A1 (en) | 1997-02-11 | 1998-02-03 | Amino acid ester containing azole antifungals |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| HUP0001050A2 true HUP0001050A2 (hu) | 2001-04-28 |
| HUP0001050A3 HUP0001050A3 (en) | 2001-07-30 |
| HU227744B1 HU227744B1 (en) | 2012-02-28 |
Family
ID=26146124
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0001050A HU227744B1 (en) | 1997-02-11 | 1998-02-03 | Amino acid ester containing azole antifungals, process for their preparation, pharmaceuticals containing the same and intermediates |
Country Status (31)
| Country | Link |
|---|---|
| US (3) | US6262052B1 (hu) |
| EP (1) | EP0958289B1 (hu) |
| JP (1) | JP4347911B2 (hu) |
| KR (1) | KR100509171B1 (hu) |
| CN (1) | CN1238353C (hu) |
| AT (1) | ATE270290T1 (hu) |
| AU (1) | AU725302C (hu) |
| BG (1) | BG63872B1 (hu) |
| BR (1) | BR9809744A (hu) |
| CA (1) | CA2262791C (hu) |
| CZ (1) | CZ297197B6 (hu) |
| DE (1) | DE69824834T2 (hu) |
| DK (1) | DK0958289T3 (hu) |
| EE (1) | EE03876B1 (hu) |
| ES (1) | ES2224364T3 (hu) |
| HU (1) | HU227744B1 (hu) |
| ID (1) | ID21755A (hu) |
| IL (2) | IL128513A (hu) |
| MY (1) | MY129537A (hu) |
| NO (1) | NO316668B1 (hu) |
| NZ (1) | NZ334477A (hu) |
| PL (1) | PL191152B1 (hu) |
| PT (1) | PT958289E (hu) |
| RU (1) | RU2197489C2 (hu) |
| SI (1) | SI0958289T1 (hu) |
| SK (1) | SK284910B6 (hu) |
| TR (1) | TR199900584T2 (hu) |
| TW (1) | TW495508B (hu) |
| UA (1) | UA61919C2 (hu) |
| WO (1) | WO1998034934A1 (hu) |
| ZA (1) | ZA981079B (hu) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0957101A1 (en) * | 1998-05-14 | 1999-11-17 | Janssen Pharmaceutica N.V. | Water soluble azoles as broad-spectrum antifungals |
| WO2000030655A1 (en) | 1998-11-20 | 2000-06-02 | Bristol-Myers Squibb Company | Water soluble prodrugs of azole compounds |
| DE60001734T2 (de) * | 1999-05-04 | 2004-02-05 | Janssen Pharmaceutica N.V. | Antimykotische ether |
| AU2002365077A1 (en) * | 2001-09-19 | 2003-06-30 | Massachusetts Institute Of Technology | Methods and products related to non-viral transfection |
| ITMI20032020A1 (it) | 2003-10-17 | 2005-04-18 | Italfarmaco Spa | Nuovi agenti antifungini azolici con diminuita interazione con i citocromi metabolici |
| RU2585760C2 (ru) * | 2010-05-19 | 2016-06-10 | Сандоз Аг | Способ получения хиральных триазолонов |
| BR102019004480B1 (pt) * | 2018-03-08 | 2023-03-28 | Dow Agrosciences Llc | Picolinamidas como fungicidas |
| CN111138421A (zh) * | 2019-12-26 | 2020-05-12 | 上海英诺富成生物科技有限公司 | 抗真菌水溶性化合物及其制备方法与应用 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4267179A (en) | 1978-06-23 | 1981-05-12 | Janssen Pharmaceutica, N.V. | Heterocyclic derivatives of (4-phenylpiperazin-1-yl-aryloxymethyl-1,3-dioxolan-2-yl)methyl-1H-imidazoles and 1H-1,2,4-triazoles |
| US4791111A (en) * | 1985-12-23 | 1988-12-13 | Janssen Pharmaceutica, N.V. | [[4-[4-(4-phenyl-1-piperazinyl)phenoxymethyl]-1,3-dioxolan-2-yl]methyl]-1H-imidazoles and 1H-1,2,4-triazoles having anti-microbial properties |
| US4916134A (en) | 1987-03-25 | 1990-04-10 | Janssen Pharmacuetica N.V. | 4-[4-[4-[4-[[2-(2,4-difluorophenyl)-2-(1H-azolylmethyl)-1,3-dioxolan-4-yl]me]phenyl]-1-piperazinyl]phenyl]triazolones |
| CA1331757C (en) | 1988-02-29 | 1994-08-30 | Janssen Pharmaceutica Naamloze Vennootschap | 5-lipoxygenase inhibiting 4-(4-phenyl-1-piperazinyl)phenols |
| DK0631578T3 (da) | 1992-03-18 | 2001-08-27 | Janssen Pharmaceutica Nv | Itraconazol- og saperconazol-stereoisomerer |
| DK0736030T3 (da) * | 1993-12-21 | 2001-10-29 | Schering Corp | Fungicide tetrahydrofuraner |
| SI0741737T1 (en) * | 1994-01-24 | 2000-02-29 | Janssen Pharmaceutica N.V. | Watersoluble azole antifungals |
| DE69628117T2 (de) * | 1995-06-02 | 2004-04-01 | Schering Corp. | Antifungale tetrahydrofurane |
| ATE247108T1 (de) | 1995-06-19 | 2003-08-15 | Schering Corp | Antifungale tetrahydrofurane |
-
1998
- 1998-02-03 EP EP98908064A patent/EP0958289B1/en not_active Expired - Lifetime
- 1998-02-03 AU AU66207/98A patent/AU725302C/en not_active Expired
- 1998-02-03 IL IL12851398A patent/IL128513A/en not_active IP Right Cessation
- 1998-02-03 AT AT98908064T patent/ATE270290T1/de active
- 1998-02-03 CA CA002262791A patent/CA2262791C/en not_active Expired - Lifetime
- 1998-02-03 CZ CZ0283599A patent/CZ297197B6/cs not_active IP Right Cessation
- 1998-02-03 KR KR10-1999-7001983A patent/KR100509171B1/ko active IP Right Grant
- 1998-02-03 TR TR1999/00584T patent/TR199900584T2/xx unknown
- 1998-02-03 DK DK98908064T patent/DK0958289T3/da active
- 1998-02-03 RU RU99106585/04A patent/RU2197489C2/ru active
- 1998-02-03 SK SK1059-99A patent/SK284910B6/sk not_active IP Right Cessation
- 1998-02-03 DE DE69824834T patent/DE69824834T2/de not_active Expired - Lifetime
- 1998-02-03 JP JP53376398A patent/JP4347911B2/ja not_active Expired - Lifetime
- 1998-02-03 US US09/355,369 patent/US6262052B1/en not_active Expired - Lifetime
- 1998-02-03 ID IDW990505A patent/ID21755A/id unknown
- 1998-02-03 HU HU0001050A patent/HU227744B1/hu unknown
- 1998-02-03 PL PL332008A patent/PL191152B1/pl unknown
- 1998-02-03 EE EEP199900100A patent/EE03876B1/xx unknown
- 1998-02-03 WO PCT/EP1998/000646 patent/WO1998034934A1/en active IP Right Grant
- 1998-02-03 BR BR9809744-0A patent/BR9809744A/pt not_active Application Discontinuation
- 1998-02-03 ES ES98908064T patent/ES2224364T3/es not_active Expired - Lifetime
- 1998-02-03 CN CNB988011352A patent/CN1238353C/zh not_active Expired - Lifetime
- 1998-02-03 NZ NZ334477A patent/NZ334477A/en not_active IP Right Cessation
- 1998-02-03 SI SI9830687T patent/SI0958289T1/xx unknown
- 1998-02-03 PT PT98908064T patent/PT958289E/pt unknown
- 1998-02-09 MY MYPI98000513A patent/MY129537A/en unknown
- 1998-02-09 TW TW087101662A patent/TW495508B/zh not_active IP Right Cessation
- 1998-02-10 ZA ZA9801079A patent/ZA981079B/xx unknown
- 1998-03-02 UA UA99020835A patent/UA61919C2/uk unknown
-
1999
- 1999-02-02 NO NO19990484A patent/NO316668B1/no not_active IP Right Cessation
- 1999-02-11 BG BG103171A patent/BG63872B1/bg unknown
-
2001
- 2001-05-04 US US09/848,989 patent/US6512116B2/en not_active Expired - Lifetime
-
2002
- 2002-04-23 IL IL149285A patent/IL149285A/en not_active IP Right Cessation
- 2002-11-15 US US10/298,038 patent/US6703506B2/en not_active Expired - Lifetime
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