ES2139195T3 - Derivados de sulfonamidas como inhibidores de la aspartil-proteasa. - Google Patents
Derivados de sulfonamidas como inhibidores de la aspartil-proteasa.Info
- Publication number
- ES2139195T3 ES2139195T3 ES95911960T ES95911960T ES2139195T3 ES 2139195 T3 ES2139195 T3 ES 2139195T3 ES 95911960 T ES95911960 T ES 95911960T ES 95911960 T ES95911960 T ES 95911960T ES 2139195 T3 ES2139195 T3 ES 2139195T3
- Authority
- ES
- Spain
- Prior art keywords
- pct
- hiv
- compounds
- protease inhibitors
- provides
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
- C07D213/30—Oxygen atoms
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/22—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms
- C07C311/29—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
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- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/37—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
- C07C311/38—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered rings of the same carbon skeleton
- C07C311/39—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered rings of the same carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
- C07C311/41—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered rings of the same carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms, not being part of nitro or nitroso groups
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
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- C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
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- C07D213/62—Oxygen or sulfur atoms
- C07D213/70—Sulfur atoms
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- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/81—Amides; Imides
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- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/81—Amides; Imides
- C07D213/82—Amides; Imides in position 3
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- C—CHEMISTRY; METALLURGY
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- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
- C07D217/24—Oxygen atoms
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- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
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- 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
- C07D231/14—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 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
- C07D231/38—Nitrogen atoms
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- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
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- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
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- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
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- C07D233/72—Two oxygen atoms, e.g. hydantoin
- C07D233/76—Two oxygen atoms, e.g. hydantoin with substituted hydrocarbon radicals attached to the third ring carbon atom
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- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
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- C07D233/88—Nitrogen atoms, e.g. allantoin
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- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
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- C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated
Abstract
LA INVENCION SE REFIERE A UNA NUEVA CLASE DE SULFONAMIDAS QUE SON INHIBIDORAS DE LA PROTEASA DE ASPARTILO. EN UNA RELACION ESTA INVENCION SE REFIERE A UNA NUEVA CLASE DE INHIBIDORES DE LA PROTEASA DE ASPARTILO CARACTERIZADOS POR CARACTERISTICAS ESTRUCTURALES Y FISIQUIMICAS ESPECIFICAS. ESTA INVENCION TAMBIEN SE REFIERE A LAS COMPOSICIONES FARMACEUTICAS QUE COMPRENDEN ESTOS COMPUESTOS. LOS COMPUESTOS Y LAS COMPOSICIONES FARMACEUTICAS DE ESTA INVENCION ESTAN PARTICULARMENTE BIEN ADAPTADOS PARA INHIBIR LA ACTIVIDAD DE LAS PROTEASAS DEL VIH-1 Y DEL VIH-2 Y POR CONSIGUIENTE, PUEDE SER VENTAJOSAMENTE USADOS COMO AGENTES ANTIVIRICOS CONTRA LOS VIRUS DEL VIH-1 Y DEL VIH-2. ESTA INVENCION TAMBIEN SE REFIERE A LOS METODOS PARA INHIBIR LA ACTIVIDAD DE LA PROTEASA DE ASPARTILO Y METODOS PARA TRATAR INFECCIONES VIRICAS USANDO LOS COMPUESTOS Y LAS COMPOSICIONES DE ESTA INVENCION.
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DE69316223T2 (de) * | 1992-08-25 | 1998-05-28 | Searle & Co | Sulfonylalkanoylaminohydroxyethylaminosulfonamide verwendbar als retrovirale protease-inhibitoren |
CA2143191A1 (en) * | 1992-10-30 | 1994-05-11 | Michael L. Vazquez | Sulfonylalkanoylamino hydroxyethylamino sulfamic acids useful as retroviral protease inhibitors |
EP0810208B1 (en) * | 1992-10-30 | 2002-01-02 | G.D. Searle & Co. | N-substituted Hydroxyethylamino sulfamic acid derivatives useful as retroviral protease inhibitors |
AU6135294A (en) * | 1993-02-12 | 1994-08-29 | Merck & Co., Inc. | Piperazine derivatives as hiv protease inhibitors |
TW281669B (es) * | 1993-02-17 | 1996-07-21 | Chugai Pharmaceutical Co Ltd |
-
1995
- 1995-02-24 WO PCT/US1995/002420 patent/WO1995024385A1/en active IP Right Grant
- 1995-02-24 AT AT95911960T patent/ATE184594T1/de active
- 1995-02-24 EP EP95911960A patent/EP0749421B1/en not_active Expired - Lifetime
- 1995-02-24 DE DE69512220T patent/DE69512220T2/de not_active Expired - Lifetime
- 1995-02-24 CA CA002183653A patent/CA2183653A1/en not_active Abandoned
- 1995-02-24 JP JP7523497A patent/JPH10500938A/ja active Pending
- 1995-02-24 AU AU19332/95A patent/AU699483B2/en not_active Expired
- 1995-02-24 ES ES95911960T patent/ES2139195T3/es not_active Expired - Lifetime
- 1995-02-24 US US08/424,372 patent/US6127372A/en not_active Expired - Lifetime
- 1995-02-24 MX MX9603909A patent/MX9603909A/es unknown
- 1995-02-24 DK DK95911960T patent/DK0749421T3/da active
- 1995-02-24 CN CN95192473A patent/CN1146201A/zh active Pending
- 1995-03-01 IL IL11284195A patent/IL112841A0/xx unknown
- 1995-03-01 ZA ZA951688A patent/ZA951688B/xx unknown
-
1998
- 1998-12-17 HK HK98113972A patent/HK1012622A1/xx not_active IP Right Cessation
-
1999
- 1999-12-15 GR GR990403237T patent/GR3032151T3/el unknown
Also Published As
Publication number | Publication date |
---|---|
WO1995024385A1 (en) | 1995-09-14 |
DE69512220T2 (de) | 2000-03-16 |
HK1012622A1 (en) | 1999-08-06 |
CN1146201A (zh) | 1997-03-26 |
ZA951688B (en) | 1995-12-11 |
AU1933295A (en) | 1995-09-25 |
GR3032151T3 (en) | 2000-04-27 |
MX9603909A (es) | 1997-03-29 |
AU699483B2 (en) | 1998-12-03 |
DK0749421T3 (da) | 2000-03-20 |
ATE184594T1 (de) | 1999-10-15 |
EP0749421A1 (en) | 1996-12-27 |
IL112841A0 (en) | 1995-06-29 |
US6127372A (en) | 2000-10-03 |
DE69512220D1 (en) | 1999-10-21 |
EP0749421B1 (en) | 1999-09-15 |
JPH10500938A (ja) | 1998-01-27 |
CA2183653A1 (en) | 1995-09-14 |
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