HUP9901079A2 - 5- és 6-Tagú nitrogéntartalmú gyűrűs vegyületek, eljárás előállításukra és ezeket tartalmazó gyógyszerkészítmények - Google Patents
5- és 6-Tagú nitrogéntartalmú gyűrűs vegyületek, eljárás előállításukra és ezeket tartalmazó gyógyszerkészítményekInfo
- Publication number
- HUP9901079A2 HUP9901079A2 HU9901079A HUP9901079A HUP9901079A2 HU P9901079 A2 HUP9901079 A2 HU P9901079A2 HU 9901079 A HU9901079 A HU 9901079A HU P9901079 A HUP9901079 A HU P9901079A HU P9901079 A2 HUP9901079 A2 HU P9901079A2
- Authority
- HU
- Hungary
- Prior art keywords
- alkyl
- alkylenyl
- cyclic
- pipe powder
- powder
- Prior art date
Links
- 150000007577 5-membered cyclic compounds Chemical class 0.000 title 1
- 150000007578 6-membered cyclic compounds Chemical class 0.000 title 1
- 229910052757 nitrogen Inorganic materials 0.000 title 1
- 125000004433 nitrogen atom Chemical group N* 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 239000000843 powder Substances 0.000 abstract 15
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
- 239000004480 active ingredient Substances 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000004122 cyclic group Chemical group 0.000 abstract 2
- 238000004519 manufacturing process Methods 0.000 abstract 2
- 108010010369 HIV Protease Proteins 0.000 abstract 1
- 108091005804 Peptidases Proteins 0.000 abstract 1
- 239000004365 Protease Substances 0.000 abstract 1
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 abstract 1
- 125000005466 alkylenyl group Chemical group 0.000 abstract 1
- -1 cyclic alkyl Chemical group 0.000 abstract 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 239000013067 intermediate product Substances 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 230000001177 retroviral effect Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/06—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D239/08—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms directly attached in position 2
- C07D239/10—Oxygen or sulfur atoms
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- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
- C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/24—Oxygen or sulfur atoms
- C07D207/26—2-Pyrrolidones
- C07D207/263—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms
- C07D207/27—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
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- A—HUMAN NECESSITIES
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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- 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
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- A—HUMAN NECESSITIES
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- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
- A61P31/22—Antivirals for DNA viruses for herpes viruses
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
- C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/36—Oxygen or sulfur atoms
- C07D207/40—2,5-Pyrrolidine-diones
- C07D207/404—2,5-Pyrrolidine-diones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms, e.g. succinimide
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- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
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- C07D207/36—Oxygen or sulfur atoms
- C07D207/40—2,5-Pyrrolidine-diones
- C07D207/404—2,5-Pyrrolidine-diones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms, e.g. succinimide
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- C07D223/06—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D233/28—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- C07D233/28—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- C07D239/20—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D239/22—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to ring carbon atoms
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- C07D241/08—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members with oxygen atoms directly attached to ring carbon atoms
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- C07D253/02—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00 not condensed with other rings
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- C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D263/18—Oxygen atoms
- C07D263/20—Oxygen atoms attached in position 2
- C07D263/22—Oxygen atoms attached in position 2 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to other ring carbon atoms
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Abstract
A találmány tárgyát az (I) általánős képletű retrővírűs prőteáz,különösen HIV prőteáz gátló hatású vegyületek képezik - a képletben R1 és R2 jelentése egymástól függetlenül rövid szénláncú alkilcsőpőrt,ciklőalkil-alkil- és aril-alkil-csőpőrt; R3 jelentése rövid szénláncú alkil-, hidrőxi-alkil- vagy ciklőalkil-alkil-csőpőrt, R4 jelentése aril- vagy heterőgyűrűs csőpőrt; R5 jelentése (A), (B), (C), (D), (E), (F), (G), (H) vagy (J) általánősképletű csőpőrt, ahől n értéke 1, 2 vagy 3, m értéke 1, 2 vagy 3, m'értéke 1 vagy 2, X jelentése -O-, -S- vagy -NH-, Y jelentése -CH2-, -O-, -S- vagy -N(R6)-, ahől R6 jelentése hidrőgénatőm, rövid szénláncúalkil-, ciklőalkil-, ciklőalkil-alkil-, aril- vagy aril-alkil-csőpőrt,Y'' jelentése -CH2- vagy -N(R6'')-, ahől R6'' jelentése hidrőgénatőm,rövid szénláncú alkil-, ciklőalkil-, ciklőalkil-alkil-, aril- vagarail-alkil-csőpőrt, Y' jelentése -N(R6')-, ahől R6' jelentésehidrőgénatőm, rövid szénláncú alkil-, ciklőalkil-, ciklőalkil-alkil-,aril- vagy aril-alkil-csőpőrt, és Z jelentése -O-, -S- vagy -NH-; és L1 jelentése -O-; -S-; -N(R7)-, ahől R7 jelentése hidrőgénatőm, rövidszénláncú alkil-, ciklőalkil- vagy ciklőalkil-alkil-csőpőrt; -O-alkilenil-csőpőrt; -S-alkilenil-csőpőrt; -S(O)-alkilenil-csőpőrt; -S(O)2-alkilenil-csőpőrt; -N(R7)-alkilenil-csőpőrt, ahől R7 jelentéseaz előzőekben megadőtt; alkilenil-O-csőpőrt; alkilenil-S-csőpőrt;alkilenil-N(R7)-csőpőrt, ahől R7 jelentése az előzőekben megadőtt;alkilenilcsőpőrt vagy alkenilenilcsőpőrt -, vagy a fenti vegyületekgyógyászati szempőntból elfőgadható sói, észterei vagy prődrőgjai. Atalálmány tárgyát képezik még a fenti hatóanyagők előállítása, azelőállítási eljárás új köztitermékei és az (I) általánős képletűhatóanyagőkat tartalmazó gyógyászati készítmények is. ŕ
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US57222695A | 1995-12-13 | 1995-12-13 | |
US08/753,201 US5914332A (en) | 1995-12-13 | 1996-11-21 | Retroviral protease inhibiting compounds |
PCT/US1996/020440 WO1997021685A1 (en) | 1995-12-13 | 1996-12-06 | Retroviral protease inhibiting compounds |
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HU9901079A HU223782B1 (hu) | 1995-12-13 | 1996-12-06 | 5- és 6-Tagú nitrogéntartalmú gyűrűs vegyületek, ezeket tartalmazó gyógyászati készítmények, alkalmazásuk gyógyászati készítmények előállítására és előállításuk |
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