HRP20110467T1 - Mono-lizinske soli azolovih spojeva - Google Patents
Mono-lizinske soli azolovih spojeva Download PDFInfo
- Publication number
- HRP20110467T1 HRP20110467T1 HR20110467T HRP20110467T HRP20110467T1 HR P20110467 T1 HRP20110467 T1 HR P20110467T1 HR 20110467 T HR20110467 T HR 20110467T HR P20110467 T HRP20110467 T HR P20110467T HR P20110467 T1 HRP20110467 T1 HR P20110467T1
- Authority
- HR
- Croatia
- Prior art keywords
- formula
- image
- mono
- solvate
- lysine salt
- Prior art date
Links
- 150000003851 azoles Chemical class 0.000 title 1
- 239000012453 solvate Substances 0.000 claims abstract 40
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 22
- 239000001257 hydrogen Substances 0.000 claims abstract 22
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract 15
- 125000005843 halogen group Chemical group 0.000 claims abstract 12
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims abstract 11
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims abstract 10
- 150000001875 compounds Chemical class 0.000 claims abstract 10
- 229910052736 halogen Inorganic materials 0.000 claims abstract 10
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims abstract 7
- -1 methylpyrazolyl Chemical group 0.000 claims abstract 6
- 125000000714 pyrimidinyl group Chemical group 0.000 claims abstract 5
- 125000000335 thiazolyl group Chemical group 0.000 claims abstract 5
- 125000001425 triazolyl group Chemical group 0.000 claims abstract 5
- 150000002431 hydrogen Chemical group 0.000 claims abstract 4
- 238000000034 method Methods 0.000 claims 21
- 239000002904 solvent Substances 0.000 claims 14
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 12
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 8
- 239000003960 organic solvent Substances 0.000 claims 8
- BDERNNFJNOPAEC-UHFFFAOYSA-N propan-1-ol Chemical compound CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 claims 8
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- 206010017533 Fungal infection Diseases 0.000 claims 4
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims 4
- 239000004472 Lysine Substances 0.000 claims 4
- 208000031888 Mycoses Diseases 0.000 claims 4
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims 4
- 230000015572 biosynthetic process Effects 0.000 claims 4
- 238000006243 chemical reaction Methods 0.000 claims 4
- 238000010511 deprotection reaction Methods 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- KEAYESYHFKHZAL-UHFFFAOYSA-N Sodium Chemical compound [Na] KEAYESYHFKHZAL-UHFFFAOYSA-N 0.000 claims 2
- 239000002671 adjuvant Substances 0.000 claims 2
- 239000003085 diluting agent Substances 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 125000006239 protecting group Chemical group 0.000 claims 2
- 229910000104 sodium hydride Inorganic materials 0.000 claims 2
- 239000012312 sodium hydride Substances 0.000 claims 2
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims 2
- 125000004215 2,4-difluorophenyl group Chemical group [H]C1=C([H])C(*)=C(F)C([H])=C1F 0.000 claims 1
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 239000006071 cream Substances 0.000 claims 1
- 239000000839 emulsion Substances 0.000 claims 1
- 239000006210 lotion Substances 0.000 claims 1
- CAAULPUQFIIOTL-UHFFFAOYSA-N methyl dihydrogen phosphate Chemical compound COP(O)(O)=O CAAULPUQFIIOTL-UHFFFAOYSA-N 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000002674 ointment Substances 0.000 claims 1
- 239000000843 powder Substances 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000000243 solution Substances 0.000 claims 1
- 239000007921 spray Substances 0.000 claims 1
- 239000007858 starting material Substances 0.000 claims 1
- 239000000725 suspension Substances 0.000 claims 1
- 239000003826 tablet Substances 0.000 claims 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
-
- 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
-
- 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
- A61P31/04—Antibacterial agents
-
- 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
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
- C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C229/04—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
- C07C229/26—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having more than one amino group bound to the carbon skeleton, e.g. lysine
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—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
- 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
- C07D417/06—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 linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/06—Phosphorus compounds without P—C bonds
- C07F9/08—Esters of oxyacids of phosphorus
- C07F9/09—Esters of phosphoric acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
- C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
- C07F9/65586—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system at least one of the hetero rings does not contain nitrogen as ring hetero atom
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Oncology (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Communicable Diseases (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US67693205P | 2005-05-03 | 2005-05-03 | |
| PCT/JP2006/309435 WO2006118351A1 (en) | 2005-05-03 | 2006-05-01 | Mono-lysine salts of azole compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20110467T1 true HRP20110467T1 (hr) | 2011-07-31 |
Family
ID=36910951
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HR20110467T HRP20110467T1 (hr) | 2005-05-03 | 2011-06-21 | Mono-lizinske soli azolovih spojeva |
Country Status (34)
| Country | Link |
|---|---|
| US (1) | US20060264406A1 (zh) |
| EP (1) | EP1877403B1 (zh) |
| JP (1) | JP4015691B1 (zh) |
| KR (1) | KR100887044B1 (zh) |
| CN (1) | CN101213193B (zh) |
| AR (1) | AR053862A1 (zh) |
| AT (1) | ATE503753T1 (zh) |
| AU (1) | AU2006241694B2 (zh) |
| BR (1) | BRPI0610423B8 (zh) |
| CA (1) | CA2606185C (zh) |
| CY (1) | CY1111569T1 (zh) |
| DE (1) | DE602006020998D1 (zh) |
| DK (1) | DK1877403T3 (zh) |
| EC (1) | ECSP077812A (zh) |
| ES (1) | ES2361768T3 (zh) |
| HK (1) | HK1117502A1 (zh) |
| HR (1) | HRP20110467T1 (zh) |
| IL (1) | IL187059A (zh) |
| JO (1) | JO2691B1 (zh) |
| MX (1) | MX2007013605A (zh) |
| MY (1) | MY138095A (zh) |
| NO (1) | NO20075541L (zh) |
| NZ (1) | NZ563092A (zh) |
| PE (1) | PE20071423A1 (zh) |
| PL (1) | PL1877403T3 (zh) |
| PT (1) | PT1877403E (zh) |
| RS (1) | RS51779B (zh) |
| RU (1) | RU2399625C2 (zh) |
| SA (1) | SA06270126B1 (zh) |
| SI (1) | SI1877403T1 (zh) |
| TW (1) | TWI363630B (zh) |
| UY (1) | UY29507A1 (zh) |
| WO (1) | WO2006118351A1 (zh) |
| ZA (1) | ZA200709127B (zh) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1964843B1 (en) * | 2005-12-20 | 2013-08-28 | Eisai R&D Management Co., Ltd. | Process for production of water-soluble azole prodrug |
| DE602007009489D1 (de) | 2006-02-22 | 2010-11-11 | Eisai R&D Man Co Ltd | Stabilisierte pharmazeutische zusammensetzung |
| CN105287403A (zh) * | 2014-08-02 | 2016-02-03 | 陕西合成药业股份有限公司 | 一种泊沙康唑前体药物的冻干组合物及其制备方法和用途 |
| CN106432338A (zh) * | 2015-08-08 | 2017-02-22 | 陕西合成药业股份有限公司 | 泊沙康唑衍生物、合成和在长效制剂中的用途 |
| WO2019106571A1 (en) | 2017-11-28 | 2019-06-06 | Roivant Sciences Gmbh | Dosing regimens for the treatment of fungal infections |
| CN110938093B (zh) * | 2018-09-21 | 2022-08-19 | 华创合成制药股份有限公司 | 一种泊沙康唑磷酸酯单胆碱盐及其制备方法和用途 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL181947B1 (en) * | 1994-01-24 | 2001-10-31 | Janssen Pharmaceutica Nv | Water-soluble azole-type antimycotic agents |
| NZ270418A (en) * | 1994-02-07 | 1997-09-22 | Eisai Co Ltd | Polycyclic triazole & imidazole derivatives, antifungal compositions |
| US5883097A (en) * | 1998-04-16 | 1999-03-16 | Schering Corporation | Soluble azole antifungal salt |
| US6265584B1 (en) * | 1998-05-22 | 2001-07-24 | Bristol-Myers Squibb Company | Water soluble prodrugs of azole compounds |
| WO2000030655A1 (en) * | 1998-11-20 | 2000-06-02 | Bristol-Myers Squibb Company | Water soluble prodrugs of azole compounds |
| US6235728B1 (en) * | 1999-02-19 | 2001-05-22 | Bristol-Myers Squibb Company | Water-soluble prodrugs of azole compounds |
| US6362172B2 (en) * | 2000-01-20 | 2002-03-26 | Bristol-Myers Squibb Company | Water soluble prodrugs of azole compounds |
| US6448401B1 (en) * | 2000-11-20 | 2002-09-10 | Bristol-Myers Squibb Company | Process for water soluble azole compounds |
-
2006
- 2006-04-17 JO JO2006103A patent/JO2691B1/en active
- 2006-04-28 MY MYPI20061985A patent/MY138095A/en unknown
- 2006-04-28 UY UY29507A patent/UY29507A1/es active IP Right Grant
- 2006-05-01 CN CN2006800150290A patent/CN101213193B/zh not_active Expired - Fee Related
- 2006-05-01 DK DK06746245.7T patent/DK1877403T3/da active
- 2006-05-01 MX MX2007013605A patent/MX2007013605A/es active IP Right Grant
- 2006-05-01 RU RU2007140788/04A patent/RU2399625C2/ru active
- 2006-05-01 WO PCT/JP2006/309435 patent/WO2006118351A1/en active Application Filing
- 2006-05-01 ES ES06746245T patent/ES2361768T3/es active Active
- 2006-05-01 PL PL06746245T patent/PL1877403T3/pl unknown
- 2006-05-01 JP JP2007509811A patent/JP4015691B1/ja active Active
- 2006-05-01 CA CA2606185A patent/CA2606185C/en active Active
- 2006-05-01 AT AT06746245T patent/ATE503753T1/de active
- 2006-05-01 DE DE602006020998T patent/DE602006020998D1/de active Active
- 2006-05-01 KR KR1020077001773A patent/KR100887044B1/ko active IP Right Grant
- 2006-05-01 SI SI200630984T patent/SI1877403T1/sl unknown
- 2006-05-01 AU AU2006241694A patent/AU2006241694B2/en not_active Ceased
- 2006-05-01 EP EP06746245A patent/EP1877403B1/en active Active
- 2006-05-01 NZ NZ563092A patent/NZ563092A/en not_active IP Right Cessation
- 2006-05-01 PT PT06746245T patent/PT1877403E/pt unknown
- 2006-05-01 BR BRPI0610423A patent/BRPI0610423B8/pt active IP Right Grant
- 2006-05-01 RS RS20110275A patent/RS51779B/en unknown
- 2006-05-02 PE PE2006000458A patent/PE20071423A1/es active IP Right Grant
- 2006-05-02 AR ARP060101759A patent/AR053862A1/es not_active Application Discontinuation
- 2006-05-03 US US11/416,322 patent/US20060264406A1/en not_active Abandoned
- 2006-05-03 SA SA06270126A patent/SA06270126B1/ar unknown
- 2006-05-03 TW TW095115682A patent/TWI363630B/zh not_active IP Right Cessation
-
2007
- 2007-10-16 EC EC2007007812A patent/ECSP077812A/es unknown
- 2007-10-23 ZA ZA200709127A patent/ZA200709127B/en unknown
- 2007-10-31 IL IL187059A patent/IL187059A/en active IP Right Grant
- 2007-11-02 NO NO20075541A patent/NO20075541L/no not_active Application Discontinuation
-
2008
- 2008-07-14 HK HK08107745.5A patent/HK1117502A1/xx unknown
-
2011
- 2011-06-17 CY CY20111100582T patent/CY1111569T1/el unknown
- 2011-06-21 HR HR20110467T patent/HRP20110467T1/hr unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| HRP20110467T1 (hr) | Mono-lizinske soli azolovih spojeva | |
| RU2496774C2 (ru) | Гетероциклические ингибиторы аспартильной протеазы | |
| EP1280795B1 (en) | N-substituted carbamoyloxyalkyl-azolium derivatives | |
| CA2397734A1 (en) | Water soluble prodrugs of azole compounds | |
| US20080125467A1 (en) | Amino-Containing Compounds Which Inhibit Memapsin 2 Beta-Secretase Activity and Methods of Use Thereof | |
| HU228507B1 (hu) | Neurotrofin termelõdését/szekrécióját elõsegítõ, azolszármazékokat tartalmazó gyógyszerkészítmények | |
| NZ590355A (en) | Stat3 inhibitor containing quinolinecarboxamide derivative as active ingredient | |
| DK2959903T3 (en) | Medicine for the treatment of eye disease | |
| US6300353B1 (en) | Azoles for treatment of fungal infections | |
| KR20180015262A (ko) | 피라졸 유도체, 또는 그 약리학적으로 허용되는 염 | |
| AU691506B2 (en) | Novel (1-heteroazolyl-1-heterocyclyl)alkane derivatives and their use as neuroprotective agents | |
| EP1401435B1 (de) | Topische anwendung von thiazolylamiden | |
| JP2008540427A (ja) | 置換β−ラクタム及び医薬におけるその使用 | |
| RU2690161C1 (ru) | 3,5-Замещенные производные тиазолидин-2,4-диона, обладающие противомикробной активностью | |
| DE60113689T2 (de) | 2-aminothiazolinderivate und ihre verwendung als no-synthase inhibitoren | |
| KR100252433B1 (ko) | 엔-벤질아졸륨 유도체 | |
| SK159995A3 (en) | Novel (1-phenyl-1-heterocyclyl)alkane derivatives and their use as neuroprotective agents | |
| RU2703997C1 (ru) | Гибридные амиды на основе триазола и тиазолидина, обладающие антимикробной активностью | |
| US5843971A (en) | 1, 1-BIS (heteroazolyl) alkane derivatives and their use as neuroprotective agents | |
| US6699895B2 (en) | 2-aminothiazoline derivatives and process for preparing the same | |
| US4307105A (en) | Imidazolylethoxymethyl derivatives of thiazole | |
| RU2771027C1 (ru) | Гибридные производные (1Н-1,2,4) триазола и серосодержащих гетероциклов: производных тиазолидин-2,4-диона, тиоморфолин-3-она и 1,4-тиазепан-3-она, обладающих антимикробной активностью | |
| CA2304624C (en) | Tetrahydrofuran phosphate- and hydroxy esters, as prodrugs for the corresponding antifungal agent | |
| DE10129717A1 (de) | Kombinationspräparate zur Herpes-Behandlung | |
| JP2003531145A (ja) | １−（１ｈ−１，２，４−トリアゾール−１−イル）ブタン−２−オール誘導体 |