SI9300365B - Novi alkilni ali alkenski fosfati, postopek za njihovo pripravo in njihova uporaba kot zdravilnega sredstva - Google Patents
Novi alkilni ali alkenski fosfati, postopek za njihovo pripravo in njihova uporaba kot zdravilnega sredstva Download PDFInfo
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- SI9300365B SI9300365B SI9300365A SI9300365A SI9300365B SI 9300365 B SI9300365 B SI 9300365B SI 9300365 A SI9300365 A SI 9300365A SI 9300365 A SI9300365 A SI 9300365A SI 9300365 B SI9300365 B SI 9300365B
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- 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 System
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
-
- 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 System
- 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
- C07F9/10—Phosphatides, e.g. lecithin
- C07F9/106—Adducts, complexes, salts of phosphatides
-
- 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
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
-
- 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
-
- 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
- A61P31/12—Antivirals
-
- 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
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- 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 System
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
- C07F9/5532—Seven-(or more) membered rings
-
- 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 System
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
- C07F9/572—Five-membered rings
-
- 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 System
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
- C07F9/576—Six-membered rings
- C07F9/59—Hydrogenated pyridine rings
Claims (16)
- - 1 - PATENTNI ZAHTEVKI 1. Spojine s splošno formulo I O (CH2)m) R-Χ-Α-Ρ-Ο- (CH2)y-CH. O (CH2)nR2 v kateri je R ravnoverižni ali razvejani alkilni ostanek z 10 do 24 ogljikovimi atomi, ki lahko vsebuje tudi eno do tri dvojne ali trojne vezi, R1 in R2 neodvisno drug od drugega vsebujeta vodik ali vsak en ravnoverižen, razvejan cikličen nasičen ali nenasičen alkilni ostanek z 1 do 6 ogljikovimi atomi, ki lahko vsebujeta tudi eno skupino CI-, OH-ali NH2- in pri čemer sta dva ta ostanka lahko tudi spojena v obroč, A je enostavna vez ali ena od skupin s formulami - CH2 - CH2 - CH2 - O - (II) - CH2 - CH2 - O - (III) -CH2-CH-0- (IV) -(CH2)8-0-(V) I ch3 -CH-CH-CH2-0- l \ h2c o(VI) - 2- pri čemer so skupine (II) do (VI) orientirane tako, da je kisikov atom zvezan s fosforjevim atomom vezi (I) in je X kisikov aii žveplov atom ali NH, če je A enostavna vez ali pa kisikov ali žveplov atom, če je A ena od skupin (II) do (IV), kar pomeni, da je y enako 0 ali enemu naravnemu številu med 1 in 3, m in n sta neodvisno drug od drugega naravni števili, določeni z m + n = 2 do 8.
- 2. Spojine po zahtevku 1, označene s tem, da X pomeni kisikov atom.
- 3. Spojine po zahtevkih 1 ali 2, označene s tem, da A pomeni enostavno vez.
- 4. Spojine po zahtevkih 1 do 3, označene s tem, da sta R1 in R2 vsakokrat metilni skupini. - 3 -
- 5. Oktadecil - (1,1-dimetilpiperidin - 4- il) - fosfat, oktadecil - (1,1-dimetilheksahidroazepino - 4- il) - fosfat.
- 6. Postopek za pripravo spojine po enem od zahtevkov 1 do 5, označen s tem, da se doseže, da spojina splošne formule R-X-A-H (VII) v kateri imajo R, X in A v. zahtevku 1.navedene pomene, reagira s fosforoksitrikloridom v navzočnosti primerne pomožne baze za reakcijo z ali brez topila in se nato s spojino splošne formule HO - (CH2)y - CH(CH2 )m(CH2 )ny- (Vlil) v kateri imajo R1 in R2, y, m in n pomene, navedene v zahtevku 1 in y-pomeni halogenid, mesilat ali tosilat pretvori v spojino s splošno formulo I, na primer so lahko spojine s splošno formulo (CH2) HO - (CH2)y - CH (CH2)nN- R (IX) - 4 - v kateri imajo R1, y, m in n pomene, navedene v zahtevku 1, pretvorjene, pri čemer se spojine s splošno formulo (I), pri katerih sta R1 in/ali R2 vodika, z alkilirnimi sredstvi R2-Y, pri katerih ima R2 pomen, naveden v zahtevku 1 in je Y Cl, brom, jod, tosil ali mesil, pretvorijo na svoj poznani način.
- 7. Postopek čiščenja spojin s formulo I, označen s tem, da se raztopina spojine, primerna formuli I, oziroma pripravljena po poznanemu postopku oziroma primerno postopku, primernemu zahtevku 5, obdela v organskem topilu z ionskim izmenjevalcem v mešalnem sloju oziroma eden za drugim ali istočasno s kislim ali bazičnim ionskim izmenjevalcem.
- 8. Zdravilno sredstvo, označeno s tem, da kot aktivno substanco vsebuje eno ali več spojin po enem od zahtevkov 1 do 5 oziroma farmacevtsko primerno sol iz ene od njih, na primer skupaj s farmacevtsko običajnimi nosilnimi, pomagalnimi, polnilnimi in razredčilnimi sredstvi, pri čemer je količina aktivne substance med 50 mg in 250 mg. ' 5 -
- 9. Zdravilno sredstvo po zahtevku 7, označeno s tem, da kot aktivno sredstvo vsebuje oktadecil-(1,1 -dimetilpiperidin-4-il)-fosfat, oktadecil-(1,1-dimetilhidroazepino-4-il)-fosfat, erucil-(1,1-dimetilpiperidin-4-il)-fosfat ali erucil-(1,1 -dimetilperhidroazepinio-4-il) fosfat, pri čemer je količina aktivnega sredstva med 50 mg in 250 mg.
- 10. Zdravilno sredstvo po zahtevku 8, označeno s tem, da kot aktivno substanco vsebuje oktadecil-(1.1 -dimetilpiperidin-4-il) fosfat, pri čemer je količina aktivnega sredstva med 50 mg in 250 mg.
- 11. Uporaba spojin po zahtevkih od 1 do 5 za pripravo zdravil za zatiranje tumorjev.
- 12. Uporaba spojin po zahtevkih od 1 do 5 za pripravo zdravil za zatiranje protozojskih in glivičnih obolenj, zlasti leishmaniaze
- 13. Uporaba spojin po zahtevkih od 1 do 5 za pripravo zdravil za terapijo avtoimunskih bolezni, zlasti multiple skleroze. 6-
- 14. Uporaba spojin po zahtevkih od 1 do 5 za pripravo zdravil za terapijo kožnih obolenj, zlasti psoriaze.
- 15. Uporaba spojin po zahtevkih od 1 do 5 za pripravo zdravil za terapijo poškodb kostnega mozga zaradi zdravljenja s citostatiki in drugimi učinkovinami, škodljivimi za kostni mozeg.
- 16. Postopek za pripravo antitumorskega sredstva, označen s tem, da pripravimo formulacijo, ki kot učinkovino vsebuje eno ali več spojin po enem od zahtevkov 1 do 5, po izibiri skupaj s farmacevtsko običajnimi nosilnimi, pomožnimi, polnilnimi in razredčilnimi sredstvi.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE4222910A DE4222910A1 (de) | 1992-07-11 | 1992-07-11 | Neue Phospholipidderivate |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| SI9300365A SI9300365A (en) | 1994-03-31 |
| SI9300365B true SI9300365B (sl) | 2002-02-28 |
Family
ID=6463031
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SI9300365A SI9300365B (sl) | 1992-07-11 | 1993-07-09 | Novi alkilni ali alkenski fosfati, postopek za njihovo pripravo in njihova uporaba kot zdravilnega sredstva |
Country Status (31)
| Country | Link |
|---|---|
| EP (1) | EP0579939B1 (sl) |
| JP (1) | JP3311431B2 (sl) |
| KR (1) | KR100297180B1 (sl) |
| CN (1) | CN1039012C (sl) |
| AT (1) | ATE176477T1 (sl) |
| AU (1) | AU664101B2 (sl) |
| BR (1) | BR9302809A (sl) |
| CA (2) | CA2100228C (sl) |
| CZ (1) | CZ290863B6 (sl) |
| DE (2) | DE4222910A1 (sl) |
| DK (1) | DK0579939T3 (sl) |
| EE (1) | EE03140B1 (sl) |
| ES (1) | ES2129053T3 (sl) |
| FI (1) | FI111262B (sl) |
| GR (1) | GR3029602T3 (sl) |
| HR (1) | HRP931046B1 (sl) |
| HU (1) | HU218783B (sl) |
| IL (1) | IL106289A (sl) |
| LT (1) | LT3113B (sl) |
| LV (1) | LV10870B (sl) |
| MX (1) | MX9304133A (sl) |
| NO (1) | NO306468B1 (sl) |
| PL (3) | PL173388B1 (sl) |
| RU (1) | RU2108336C1 (sl) |
| SG (1) | SG46249A1 (sl) |
| SI (1) | SI9300365B (sl) |
| SK (1) | SK283827B6 (sl) |
| TW (1) | TW304956B (sl) |
| UA (1) | UA40567C2 (sl) |
| YU (1) | YU49079B (sl) |
| ZA (1) | ZA934971B (sl) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20080161251A1 (en) | 2005-01-21 | 2008-07-03 | Astex Therapeutics Limited | Pharmaceutical Compounds |
| RU2469727C2 (ru) * | 2005-12-19 | 2012-12-20 | Этерна Центарис ГмбХ | Способ лечения или профилактики заболеваний и/или патофизиологических состояний, вызванных микроорганизмами, посредством производных алкилфосфолипидов |
| EP1800684A1 (en) * | 2005-12-20 | 2007-06-27 | Zentaris GmbH | Novel alkyl phospholipid derivatives and uses thereof |
| EP1869981A1 (de) * | 2006-06-21 | 2007-12-26 | Staatliches Weinbauinstitut Freiburg | Alkylphospholipide und Lyso-Phospholipide zur Bekämpfung von Pflanzenpathogenen |
| WO2008044041A1 (en) | 2006-10-12 | 2008-04-17 | Astex Therapeutics Limited | Pharmaceutical combinations |
| JP5528807B2 (ja) | 2006-10-12 | 2014-06-25 | アステックス、セラピューティックス、リミテッド | 複合薬剤 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0050327B1 (de) * | 1980-10-21 | 1984-06-20 | Roche Diagnostics GmbH | Neue schwefelhaltige Phospholipide, Verfahren zu deren Herstellung und diese Verbindungen enthaltende Arzneimittel |
| JPS5984824A (ja) * | 1982-11-08 | 1984-05-16 | Takeda Chem Ind Ltd | 抗腫瘍剤 |
| DE3530767A1 (de) * | 1985-08-28 | 1987-03-12 | Max Planck Gesellschaft | Mittel gegen multiple sklerose |
| CA1338627C (en) * | 1985-12-04 | 1996-10-01 | Hansjorg Eibl | Pharmaceuticals based on phosphoric acid esters for use in tumor therapy, and process for their preparation |
| EP0257762B1 (en) * | 1986-07-14 | 1990-10-10 | Nippon Chemiphar Co., Ltd. | Novel glycerol derivative and anti-hypertensive agent |
| DE3881925T2 (de) * | 1987-03-24 | 1994-01-27 | Nippon Chemiphar Co | Glycerol-Derivate und anti-hypertensives Mittel. |
| DE3906952A1 (de) * | 1989-03-04 | 1990-09-06 | Boehringer Mannheim Gmbh | (3-(c(pfeil abwaerts)1(pfeil abwaerts)(pfeil abwaerts)6(pfeil abwaerts)-c(pfeil abwaerts)1(pfeil abwaerts)(pfeil abwaerts)8(pfeil abwaerts))alkansulfinyl- und sulfonyl-2-methoxymethyl-propyl)-(2-trimethylammonio-ethyl) phosphate, verfahren zu deren herstellung diese verbindungen enthaltende arzneimittel |
| DE3942933A1 (de) * | 1989-12-23 | 1991-06-27 | Boehringer Mannheim Gmbh | Verwendung von alkylphospholipiden als antivirale arzneimittel und neue phospholipid-derivate |
| DE4114586A1 (de) * | 1991-05-04 | 1992-11-05 | Boehringer Mannheim Gmbh | Arzneimittel enthaltend azacyclodiphosphonsaeurederivate, neue azacyclodiphosphonsaeurederivate sowie verfahren zu deren herstellung |
-
1992
- 1992-07-11 DE DE4222910A patent/DE4222910A1/de not_active Ceased
-
1993
- 1993-06-01 TW TW082104345A patent/TW304956B/zh not_active IP Right Cessation
- 1993-06-03 AT AT93108904T patent/ATE176477T1/de active
- 1993-06-03 DE DE59309355T patent/DE59309355D1/de not_active Expired - Lifetime
- 1993-06-03 EP EP93108904A patent/EP0579939B1/de not_active Expired - Lifetime
- 1993-06-03 DK DK93108904T patent/DK0579939T3/da active
- 1993-06-03 ES ES93108904T patent/ES2129053T3/es not_active Expired - Lifetime
- 1993-06-03 SG SG1996001626A patent/SG46249A1/en unknown
- 1993-06-04 LT LTIP620A patent/LT3113B/lt not_active IP Right Cessation
- 1993-06-23 CZ CZ19931249A patent/CZ290863B6/cs not_active IP Right Cessation
- 1993-06-28 SK SK670-93A patent/SK283827B6/sk not_active IP Right Cessation
- 1993-07-06 YU YU47393A patent/YU49079B/sh unknown
- 1993-07-08 JP JP16911493A patent/JP3311431B2/ja not_active Expired - Lifetime
- 1993-07-08 PL PL93299624A patent/PL173388B1/pl unknown
- 1993-07-08 NO NO932502A patent/NO306468B1/no not_active IP Right Cessation
- 1993-07-08 PL PL93318679A patent/PL177811B1/pl unknown
- 1993-07-08 PL PL93318680A patent/PL175607B1/pl unknown
- 1993-07-09 HR HR931046A patent/HRP931046B1/xx not_active IP Right Cessation
- 1993-07-09 UA UA93002052A patent/UA40567C2/uk unknown
- 1993-07-09 CA CA002100228A patent/CA2100228C/en not_active Expired - Lifetime
- 1993-07-09 AU AU41864/93A patent/AU664101B2/en not_active Expired
- 1993-07-09 IL IL10628993A patent/IL106289A/xx not_active IP Right Cessation
- 1993-07-09 CA CA002511753A patent/CA2511753C/en not_active Expired - Lifetime
- 1993-07-09 ZA ZA934971A patent/ZA934971B/xx unknown
- 1993-07-09 SI SI9300365A patent/SI9300365B/sl unknown
- 1993-07-09 HU HU9301992A patent/HU218783B/hu unknown
- 1993-07-09 RU RU93047049A patent/RU2108336C1/ru active
- 1993-07-09 BR BR9302809A patent/BR9302809A/pt not_active Application Discontinuation
- 1993-07-09 MX MX9304133A patent/MX9304133A/es active IP Right Grant
- 1993-07-09 FI FI933165A patent/FI111262B/fi not_active IP Right Cessation
- 1993-07-10 CN CN93108564A patent/CN1039012C/zh not_active Expired - Lifetime
- 1993-07-10 KR KR1019930012980A patent/KR100297180B1/ko not_active IP Right Cessation
- 1993-07-12 LV LVP-93-988A patent/LV10870B/lv unknown
-
1994
- 1994-10-25 EE EE9400199A patent/EE03140B1/xx unknown
-
1999
- 1999-03-08 GR GR990400689T patent/GR3029602T3/el unknown
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