RU2008135239A - Ингибиторы вирусной полимеразы - Google Patents
Ингибиторы вирусной полимеразы Download PDFInfo
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- RU2008135239A RU2008135239A RU2008135239/04A RU2008135239A RU2008135239A RU 2008135239 A RU2008135239 A RU 2008135239A RU 2008135239/04 A RU2008135239/04 A RU 2008135239/04A RU 2008135239 A RU2008135239 A RU 2008135239A RU 2008135239 A RU2008135239 A RU 2008135239A
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- alkyl
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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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/235—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
- A61K31/24—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group having an amino or nitro group
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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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C205/00—Compounds containing nitro groups bound to a carbon skeleton
- C07C205/49—Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by carboxyl groups
- C07C205/57—Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by carboxyl groups having nitro groups and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
- C07C205/59—Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by carboxyl groups having nitro groups and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton the carbon skeleton being further substituted by singly-bound oxygen atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C233/00—Carboxylic acid amides
- C07C233/57—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings
- C07C233/63—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
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- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
- C07C235/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
- C07C235/44—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
- C07C235/46—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
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- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
- C07C323/50—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
- C07C323/62—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton
- C07C323/63—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton the carbon skeleton being further substituted by nitrogen atoms, not being part of nitro or nitroso groups
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- 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
- C07D207/04—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 no double bonds between ring members or between ring members and non-ring members
- C07D207/06—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 no double bonds between ring members or between ring members and non-ring members with radicals, containing only hydrogen and carbon atoms, attached to ring carbon atoms
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- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- 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
- C07D207/04—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 no double bonds between ring members or between ring members and non-ring members
- C07D207/08—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 no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
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- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- 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
- C07D207/04—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 no double bonds between ring members or between ring members and non-ring members
- C07D207/10—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 no 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
- C07D207/12—Oxygen or sulfur atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- 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
- C07D207/04—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 no double bonds between ring members or between ring members and non-ring members
- C07D207/10—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 no 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
- C07D207/14—Nitrogen atoms not forming part of a nitro radical
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/44—Iso-indoles; Hydrogenated iso-indoles
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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
- C07D211/08—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 with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/10—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 with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms
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- 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
- C07D211/36—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 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
- C07D211/56—Nitrogen atoms
- C07D211/58—Nitrogen atoms attached in position 4
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- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
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- 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
- C07D211/36—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 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
- 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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- 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
- C07D211/36—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 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
- C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D211/62—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
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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
- 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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- 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
- C07D213/60—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
- C07D213/72—Nitrogen atoms
- C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon 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
- 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
- C07D213/72—Nitrogen atoms
- C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
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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
- C07D231/12—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
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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
- C07D231/40—Acylated on said nitrogen atom
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- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
- C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
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- 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
- C07D233/60—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 with hydrocarbon radicals, substituted by oxygen or sulfur atoms, attached to ring nitrogen atoms
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- 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
- C07D233/64—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 substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
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- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
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- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/26—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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
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- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having 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
- C07D241/20—Nitrogen atoms
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- C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
- C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
- C07D243/08—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 not condensed with other rings
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Abstract
1. Соединение формулы I ! ! в которой Х выбран из группы, включающей О и S; ! R2 обозначает арил, необязательно замещенный с помощью R20, где R20 обозначает от 1 до 5 заместителей, каждый из которых независимо выбран из группы, включающей: ! a) галоген, (C1-C6)алкил, (С1-С6)галогеналкил, (С3-С7)циклоалкил и (С3-С7)циклоалкил-(С1-С6)алкил-; ! b) -N(R7)R8 или -Y-N(R7)R8, где ! Y выбран из группы, включающей -С(=O)-, -SO2- и -(С1-С6)алкилен-; ! R7 в каждом случае независимо выбран из группы, включающей Н и (С1-С6)алкил; и ! R8 в каждом случае независимо выбран из группы, включающей Н, (С1-С6)алкил, (С1-С6)галогеналкил, (С3-С7)циклоалкил, (С3-С7)циклоалкил-(С1-С6)алкил-, арил, Het, -C(=O)-R9, -C(=O)OR9 и -C(=O)NHR9; ! где (С1-С6)алкил необязательно содержит в качестве заместителей -ОН, -O-(C1-С6)алкил, цианогруппу, -NH2, -NH(С1-С4)алкил или -N((С1-С4)алкил)2; и где каждый из арилов и Het необязательно содержит от 1 до 3 заместителей, каждый из которых независимо выбран из группы, включающей ! i) галоген, -ОН, (С1-С6)галогеналкил, -С(=O)-(С1-С6)алкил, -SO2(С1-С6)алкил, -(=O)-NH2, -С(=O)-NH(С1-С4)алкил, -C(=O)-N((C1-C4)алкил)2, -NH2, -NH(C1-С4)алкил, -N((С1-С4)алкил)2 или -NH-C(=O)(C1-C4)алкил; ! ii) (С1-С6)алкил, необязательно замещенный с помощью -ОН или -O-(C1-С6)алкила; и ! iii) арил или Het, где каждый из арилов и Het необязательно содержит в качестве заместителей галоген или (С1-С6)алкил; и ! где R9 выбран из группы, включающей ! i) (С1-С6)алкил, необязательно содержащий в качестве заместителей -СООН, -Н2, -NH(С1-С4)алкил или -N((С1-С4)алкил)2; и ! ii) Het, необязательно замещенный с помощью (С1-С6)алкила; или ! R7 и R8 вместе с атомом N, с которым они связаны, образуют 4- - 7-членный гетероцикл, необязательно содержащий от 1 до 3 дополнительных гетероатомов, каждый из которых независимо выбран из группы, включающей N, О и S,
Claims (28)
1. Соединение формулы I
в которой Х выбран из группы, включающей О и S;
R2 обозначает арил, необязательно замещенный с помощью R20, где R20 обозначает от 1 до 5 заместителей, каждый из которых независимо выбран из группы, включающей:
a) галоген, (C1-C6)алкил, (С1-С6)галогеналкил, (С3-С7)циклоалкил и (С3-С7)циклоалкил-(С1-С6)алкил-;
b) -N(R7)R8 или -Y-N(R7)R8, где
Y выбран из группы, включающей -С(=O)-, -SO2- и -(С1-С6)алкилен-;
R7 в каждом случае независимо выбран из группы, включающей Н и (С1-С6)алкил; и
R8 в каждом случае независимо выбран из группы, включающей Н, (С1-С6)алкил, (С1-С6)галогеналкил, (С3-С7)циклоалкил, (С3-С7)циклоалкил-(С1-С6)алкил-, арил, Het, -C(=O)-R9, -C(=O)OR9 и -C(=O)NHR9;
где (С1-С6)алкил необязательно содержит в качестве заместителей -ОН, -O-(C1-С6)алкил, цианогруппу, -NH2, -NH(С1-С4)алкил или -N((С1-С4)алкил)2; и где каждый из арилов и Het необязательно содержит от 1 до 3 заместителей, каждый из которых независимо выбран из группы, включающей
i) галоген, -ОН, (С1-С6)галогеналкил, -С(=O)-(С1-С6)алкил, -SO2(С1-С6)алкил, -(=O)-NH2, -С(=O)-NH(С1-С4)алкил, -C(=O)-N((C1-C4)алкил)2, -NH2, -NH(C1-С4)алкил, -N((С1-С4)алкил)2 или -NH-C(=O)(C1-C4)алкил;
ii) (С1-С6)алкил, необязательно замещенный с помощью -ОН или -O-(C1-С6)алкила; и
iii) арил или Het, где каждый из арилов и Het необязательно содержит в качестве заместителей галоген или (С1-С6)алкил; и
где R9 выбран из группы, включающей
i) (С1-С6)алкил, необязательно содержащий в качестве заместителей -СООН, -Н2, -NH(С1-С4)алкил или -N((С1-С4)алкил)2; и
ii) Het, необязательно замещенный с помощью (С1-С6)алкила; или
R7 и R8 вместе с атомом N, с которым они связаны, образуют 4- - 7-членный гетероцикл, необязательно содержащий от 1 до 3 дополнительных гетероатомов, каждый из которых независимо выбран из группы, включающей N, О и S, или 7- - 14-членный полициклический гетероцикл, необязательно содержащий от 1 до 3 дополнительных гетероатомов, каждый из которых независимо выбран из группы, включающей N, О и S; каждый гетероцикл и полициклический гетероцикл необязательно содержит от 1 до 3 заместителей, каждый из которых независимо выбран из группы, включающей
i) галоген, -ОН, (С1-С6)галогеналкил, -С(=O)-(С1-С6)алкил, -SO2(С1-С6)алкил, -(=O)-NH2, -С(=O)-NH(С1-С4)алкил, -C(=O)-N((C1-C4)алкил)2, -NH2, -NH(C1-С4)алкил, -N((С1-С4)алкил)2 или -NH-С(=O)(С1-С4)алкил;
ii) (С1-С6)алкил, необязательно замещенный с помощью -ОН или -O-(C1-С6)алкила; и
iii) арил или Het, где каждый из арилов и Het необязательно содержит в качестве заместителей галоген или (С1-С6)алкил;
с) арил, арил-(С1-С6)алкил-, Het или Het-(С1-С6)алкил-, где
каждый арил, арил-(С1-С6)алкил-, Het и Het-(С1-С6)алкил- необязательно содержит от 1 до 3 заместителей, каждый из которых независимо выбран из группы, включающей
i) галоген, -ОН, (С1-С6)галогеналкил, -С(=O)-(С1-С6)алкил, -SO2(С1-С6)алкил, -(=O)-NH2, -С(=O)-NH(С1-С4)алкил, -C(=O)-N((C1-C4)алкил)2, -NH2, -NH(C1-С4)алкил, -N((С1-С4)алкил)2 или -NH-С(=O)(С1-С4)алкил;
ii) (С1-С6)алкил, необязательно замещенный с помощью -ОН или -O-(C1-С6)алкила; и
iii) арил или Het, где каждый из арилов и Het необязательно содержит в качестве заместителей галоген или (С1-С6)алкил; и
d) -C(=O)-R10, -O-R10, -C(=O)-O-R10, -(С1-С6)алкилен-O-R10, -S-R10, -SO-R10, -O2-R10, -(C1-C6)алкилен-S-R10, -(С1-С6)алкилен-SO-R10 или -(С1-С6)алкилен-SO2-R10, где
R10 в каждом случае независимо выбран из группы, включающей Н, (C1-С6)алкил, (С1-С6)галогеналкил, (С3-С7)циклоалкил, (С3-С7)циклоалкил-(С1-С6)алкил-, арил и Het;
где (С1-С6)алкил необязательно содержит в качестве заместителей -ОН, -O-(C1-С6)алкил, цианогруппу, -NH2, -NH(C1-C4)алкил или -N((С1-С4)алкил)2; и где каждый из арилов и Het необязательно содержит от 1 до 3 заместителей, каждый из которых независимо выбран из группы, включающей
i) галоген, -ОН, (С1-С6)галогеналкил, -С(=O)-(С1-С6)алкил, -SO2(С1-С6)алкил, -(=O)-NH2, -C(=O)-NH(C1-C4)алкил, -С(=O)-N((С1-С4)алкил)2, -NH2, -NH(C1-С4)алкил, -N((С1-С4)алкил)2 или -NH-С(=O)(С1-С4)алкил;
ii) (С1-С6)алкил, необязательно замещенный с помощью -ОН или -O-(C1-С6)алкила; и
iii) арил или Het, где каждый из арилов и Het необязательно содержит в качестве заместителей галоген или (С1-С6)алкил;
при условии, что, если Х обозначает О, R2 не обозначает группу формулы
R3 выбран из группы, включающей Н, галоген, (С1-С4)алкил, -O-(С1-С4)алкил, -(С1-С4)алкил, -NH2, -NH(С1-С4)алкил и -N((С1-С4)алкил)2;
R5 выбран из группы, включающей Н, (С1-С6)алкил, (С3-С7)циклоалкил, (С3-С7)циклоалкил-(С1-С3)алкил- и Het; (С1-С6)алкил и Het необязательно содержит от 1 до 4 заместителей, каждый из которых независимо выбран из группы, включающей (С1-С6)алкил, -ОН, -СООН, -С(=O)-(С1-С6)алкил, -C(=O)-O-(C1-С6)алкил, -С(=O)-NH-(С1-С6)алкил, -С(=O)-N((С1-С6)алкил)2 и -SO2(C1-С6)алкил; и
R6 выбран из группы, включающей (С5-С7)циклоалкил, (С5-С7)циклоалкил-(С1-С3)алкил-, арил и арил-(С1-С3)алкил;
(С5-С7)циклоалкил, (С5-С7)циклоалкил-(С1-С3)алкил-, арил и арил-(С1-С3)алкил необязательно содержит от 1 до 5 заместителей, каждый из которых независимо выбран из группы, включающей галоген, (С1-С6)алкил, (С1-С6)галогеналкил, -Н, -SH, -O-(С1-С4)алкил и -S-(С1-С4)алкил;
где Het обозначает 4- - 7-членный насыщенный, ненасыщенный или ароматический гетероцикл, содержащий от 1 до 4 гетероатомов, каждый из которых независимо выбран из группы, включающей N, О и S, или 7- - 14-членный насыщенный, ненасыщенный или ароматический полициклический гетероцикл, если это возможно, содержащий от 1 до 5 гетероатомов, каждый из которых независимо выбран из группы, включающей N, О и S;
или его соль или сложный эфир.
2. Соединение по п.1, в котором Х обозначает О.
3. Соединение по п.1, в котором Х обозначает S.
6. Соединение по п.5, в котором R2 обозначает группу формулы
в которой R21 выбран из группы, включающей Н, галоген, (С1-С6)алкил, (С1-С6)галогеналкил и -O-(С1-С6)галогеналкил; и
R22 выбран из группы, включающей Н, галоген, (С1-С3)алкил, (C1-С3)галогеналкил, -(С1-С3)алкилен-ОН, -С(=O)-(С1-С3)алкил и -СООН.
7. Соединение по п.5, в котором R2 обозначает группу формулы
в которой R21 выбран из группы, включающей Н, галоген, (С1-С6)алкил, (С1-С6)галогеналкил и -O-(С1-С6)галогеналкил; и
R22 выбран из группы, включающей:
b) -N(R7)R8 или -Y-N(R7)R8, где
Y выбран из группы, включающей -С(=O)-, -SO2- и -(С1-С6)алкилен-;
R7 выбран из группы, включающей Н и (С1-С6)алкил; и
R8 выбран из группы, включающей Н, (С1-С6)алкил, (С1-С6)галогеналкил, (С3-С7)циклоалкил, (С3-С7)циклоалкил-(С1-С6)алкил-, арил, Het, -C(=O)-R9, -(=O)OR9 и -C(=O)NHR9;
в которой (С1-С6)алкил необязательно содержит в качестве заместителей -ОН, -(С1-С6)алкил, цианогруппу, -NH2, -NH(С1-С4)алкил или -N((С1-С4)алкил)2; и
где каждый арил и Het необязательно содержит от 1 до 3 заместителей, каждый из которых независимо выбран из группы, включающей
i) галоген, -ОН, (С1-С6)галогеналкил, -С(=O)-(С1-С6)алкил, -SO2(С1-С6)алкил, -(=O)-NH2, -С(=O)-NH(С1-C4)алкил, -C(=O)-N((C1-C4)алкил)2, -NH2, -NH(C1-С4)алкил, -N((С1-С4)алкил)2 или -NH-С(=O)(С1-С4)алкил;
ii) (С1-С6)алкил, необязательно замещенный с помощью -ОН или -O-(C1-С6)алкила; и
iii) арил или Het, где каждый из арилов и Het необязательно содержит в качестве заместителей галоген или (С1-С6)алкил; и
в которой R9 выбран из группы, включающей
i) (С1-С6)алкил, необязательно содержащий в качестве заместителей -СООН, -Н2, -NH(С1-С4)алкил или -N((C1-C4)алкил)2; и
ii) Het, необязательно замещенный с помощью (С1-С6)алкила; или
R7 и R8 вместе с атомом N, с которым они связаны, образуют 4- - 7-членный гетероцикл, необязательно содержащий от 1 до 3 дополнительных гетероатомов, каждый из которых независимо выбран из группы, включающей N, О и S, или 7- - 14-членный полициклический гетероцикл, необязательно содержащий от 1 до 3 дополнительных гетероатомов, каждый из которых независимо выбран из группы, включающей N, О и S; каждый гетероцикл и полициклический гетероцикл необязательно содержит от 1 до 3 заместителей, каждый из которых независимо выбран из группы, включающей
i) галоген, -ОН, (С1-С6)галогеналкил, -С(=O)-(С1-С6)алкил, -SO2(С1-С6)алкил, -(=O)-NH2, -С(=O)-NH(С1-С4)алкил, -С(=O)-N((С1-С4)алкил)2, -NH2, -NH(C1-С4)алкил, -N((С1-С4)алкил)2 или -NH-С(=O)(С1-С4)алкил;
ii) (С1-С6)алкил, необязательно замещенный с помощью -ОН или -O-(C1-С6)алкила; и
iii) арил или Het, где каждый из арилов и Het необязательно содержит в качестве заместителей галоген или (С1-С6)алкил; и
с) арил, Het или Het-(С1-С6)алкил-, где каждый арил, Het и Het-(С1-С6)алкил- необязательно содержит от 1 до 3 заместителей, каждый из которых независимо выбран из группы, включающей
i) галоген, -ОН, (С1-С6)галогеналкил, -С(=О)-(C1-C6)алкил, -SO2(С1-С6)алкил, -(=O)-NH2, -С(=O)-NH(С1-С4)алкил, -С(=O)-N((С1-С4)алкил)2, -NH2, -NH(C1-С4)алкил, -N((С1-С4)алкил)2 или -NH-С(=O)(С1-С4)алкил;
ii) (С1-С6)алкил, необязательно замещенный с помощью -ОН или -O-(С1-С6)алкила; и
iii) арил или Het, где каждый из арилов и Het необязательно содержит в качестве заместителей галоген или (С1-С6)алкил.
8. Соединение по п.7, в котором R2 обозначает группу формулы
в которой R21 обозначает CF3; и
R22 выбран из группы, включающей:
b) -N(R7)R8, где
R7 выбран из группы, включающей Н и (С1-С6)алкил; и
R8 выбран из группы, включающей Н, (С1-С6)алкил, (С1-С6)галогеналкил, (С3-С7)циклоалкил, (С3-С7)циклоалкил-(С1-С6)алкил-, арил, Het, -C(=O)-R9, -(=O)OR9 и -C(=O)NHR9;
в которой (С1-С6)алкил необязательно содержит в качестве заместителей -ОН, -(С1-С6)алкил, цианогруппу, -NH2, -NH(С1-С4)алкил или -N((С1-С4)алкил)2; и в которой каждый арил и Het необязательно содержит от 1 до 3 заместителей, каждый из которых независимо выбран из группы, включающей
i) галоген, -ОН, (С1-С6)галогеналкил, -С(=O)-(С1-С6)алкил, -SO2(С1-С6)алкил, -(=O)-NH2, -C(=O)-NH(C1-C4)алкил, -С(=O)-N((С1-С4)алкил)2, -NH2, -NH(C1-С4)алкил, -N((С1-С4)алкил)2 или -NH-С(=O)(С1-С4)алкил;
ii) (С1-С6)алкил, необязательно замещенный с помощью -ОН или -O-(С1-С6)алкила; и
iii) арил или Het, где каждый из арилов и Het необязательно содержит в качестве заместителей галоген или (С1-С6)алкил; и
в которой R9 выбран из группы, включающей
i) (С1-С6)алкил, необязательно содержащий в качестве заместителей -СООН, -H2, -NH(С1-С4)алкил или -N((С1-С4)алкил)2; и
ii) Het, необязательно замещенный с помощью (С1-С6)алкила; или
R7 и R8 вместе с атомом N, с которым они связаны, образуют 4- - 7-членный гетероцикл, необязательно содержащий от 1 до 3 дополнительных гетероатомов, каждый из которых независимо выбран из группы, включающей N, О и S, или 7- - 14-членный полициклический гетероцикл, необязательно содержащий от 1 до 3 дополнительных гетероатомов, каждый из которых независимо выбран из группы, включающей N, О и S; каждый гетероцикл и полициклический гетероцикл необязательно содержит от 1 до 3 заместителей, каждый из которых независимо выбран из группы, включающей
i) галоген, -ОН, (С1-С6)галогеналкил, -С(=O)-(С1-С6)алкил, -SO2(С1-С6)алкил, -(=O)-NH2, -С(=O)-NH(С1-С4)алкил, -C(=O)-N((C1-C4)алкил)2, -NH2, -NH(C1-С4)алкил, -N((С1-С4)алкил)2 или -NH-С(=O)(С1-С4)алкил;
ii) (С1-С6)алкил, необязательно замещенный с помощью -ОН или -O-(C1-С6)алкила; и
iii) арил или Het, где каждый из арилов и Het необязательно содержит в качестве заместителей галоген или (С1-С6)алкил; и
с) Het необязательно содержит от 1 до 3 заместителей, каждый из которых независимо выбран из группы, включающей
i) галоген, -ОН, (С1-С6)галогеналкил, -С(=O)-(С1-С6)алкил, -SO2(C1-C6)алкил, -(=O)-NH2, -C(=O)-NH(C1-C4)алкил, -C(=O)-N((C1-C4)алкил)2, -NH2, -NH(C1-С4)алкил, -N((С1-С4)алкил)2 или -NH-C(=O)(C1-C4)алкил;
ii) (C1-C6)алкил, необязательно замещенный с помощью -ОН или -O-(C1-С6)алкила; и
iii) арил или Het, где каждый из арилов и Het необязательно содержит в качестве заместителей галоген или (C1-C6)алкил.
9. Соединение по п.7, в котором R2 обозначает группу формулы
в которой R21 обозначает CF3; и
R22 выбран из группы, включающей:
b) -Y-N(R7)R8, где
Y выбран из группы, включающей -С(=O)-, -SO2- и -СН2-;
R7 выбран из группы, включающей Н и (C1-C6)алкил; и
R8 выбран из группы, включающей Н, (C1-C6)алкил, (C1-C6)галогеналкил, (С3-С7)циклоалкил, (С3-С7)циклоалкил-(C1-C6)алкил-, арил, Het, -C(=O)-R9, -C(=O)OR9 и -C(=O)NHR9;
в которой (С1-С6)алкил необязательно содержит в качестве заместителей -ОН, -O-(C1-C6)алкил, цианогруппу, -NH2, -NH(С1-С4)алкил или -N((С1-С4)алкил)2; и в которой каждый арил и Het необязательно содержит от 1 до 3 заместителей, каждый из которых независимо выбран из группы, включающей
i) галоген, -ОН, (C1-C6)галогеналкил, -С(=O)-(C1-C6)алкил, -SO2(C1-C6)алкил, -C(=O)-NH2, -С(=O)-NH(С1-С4)алкил, -С(=O)-N((С1-С4)алкил)2, -NH2, -NH(C1-С4)алкил, -N((С1-С4)алкил)2 или -NH-С(=O)(С1-С4)алкил;
ii) (C1-C6)алкил, необязательно замещенный с помощью -ОН или -O-(C1-С6)алкила; и
iii) арил или Het, где каждый из арилов и Het необязательно содержит в качестве заместителей галоген или (C1-C6)алкил; и
где R9 выбран из группы, включающей
i) (C1-C6)алкил, необязательно содержащий в качестве заместителей -СООН, -NH2, -NH(С1-С4)алкил или -N((С1-С4)алкил)2; и
ii) Het, необязательно замещенный с помощью (C1-C6)алкила; или
R7 и R8 вместе с атомом N, с которым они связаны, образуют 4- - 7-членный гетероцикл, необязательно содержащий от 1 до 3 дополнительных гетероатомов, каждый из которых независимо выбран из группы, включающей N, О и S, или 7- - 14-членный полициклический гетероцикл, необязательно содержащий от 1 до 3 дополнительных гетероатомов, каждый из которых независимо выбран из группы, включающей N, О и S; каждый гетероцикл и полициклический гетероцикл необязательно содержит от 1 до 3 заместителей, каждый из которых независимо выбран из группы, включающей
i) галоген, -ОН, (C1-C6)галогеналкил, -С(=O)-(C1-C6)алкил, -SO2(С1-С6)алкил, -C(=O)-NH2, -C(=O)-NH(C1-C4)алкил, -С(=O)-N((С1-С4)алкил)2, -NH2, -NH(C1-С4)алкил, -N((С1-С4)алкил)2 или -NH-С(=O)(С1-С4)алкил;
ii) (С1-С6)алкил, необязательно замещенный с помощью -ОН или -O-(C1-С6)алкила; и
iii) арил или Het, где каждый из арилов и Het необязательно содержит в качестве заместителей галоген или (C1-C6)алкил; и
с) Het-(C1-C6)алкил-, необязательно содержит от 1 до 3 заместителей, каждый из которых независимо выбран из группы, включающей
i) галоген, -ОН, (С1-С6)галогеналкил, -С(=O)-(C1-C6)алкил, -SO2(C1-C6)алкил, -С(=О)-NH2, -C(=O)-NH(C1-C4)алкил, -С(=O)-N((С1-С4)алкил)2, -NH2, -NH(C1-С4)алкил, -N((С1-С4)алкил)2 или -NH-С(=O)(С1-С4)алкил;
ii) (С1-С6)алкил, необязательно замещенный с помощью -ОН или -O-(С1-С6)алкила; и
iii) арил или Het, где каждый из арилов и Het необязательно содержит в качестве заместителей галоген или (C1-C6)алкил.
10. Соединение по п.1, в котором R3 обозначает Н или F.
11. Соединение по п.10, в котором R3 обозначает Н.
12. Соединение по п.1, в котором R5 обозначает Н или (С1-С6)алкил, где (C1-C6)алкил необязательно содержит от 1 до 4 заместителей, каждый из которых независимо выбран из группы, включающей -ОН, -СООН, -C(=O)-(C1-С6)алкил, -С(=O)-O-(C1-C6)алкил, -С(=O)-NH-(C1-C6)алкил, -C(=O)-N((C1-С6)алкил)2 и -SO2(C1-C6)алкил.
13. Соединение по п.12, в котором R5 обозначает 1-метилэтил.
14. Соединение по п.1, в котором R5 обозначает Het, необязательно содержащий от 1 до 4 заместителей, каждый из которых независимо выбран из группы, включающей (С1-С6)алкил, -ОН, -СООН, -С(=O)-(С1-С6)алкил, -С(=О)-O-(С1-С6)алкил, -C(=O)-NH-(C1-C6)алкил, -C(=O)-N((C1-C6)алкил)2 и -SO2(C1-С6)алкил.
15. Соединение по п.1, в котором R6 выбран из группы, включающей (C5-С7)циклоалкил и (С5-С7)циклоалкил-(С1-С3)алкил-, (С5-С7)циклоалкил и (C5-С7)циклоалкил-(С1-С3)алкил- необязательно содержит от 1 до 5 заместителей, каждый из которых независимо выбран из группы, включающей галоген, (C1-С6)алкил, (С1-С6)галогеналкил, -ОН, -SH, -O-(С1-С4)алкил и -S-(С1-С4)алкил.
17. Соединение по п.1, в котором R6 обозначает арил, необязательно содержащий от 1 до 5 заместителей, каждый из которых независимо выбран из группы, включающей галоген, (С1-С6)алкил, (С1-С6)галогеналкил, -ОН, -SH, -O-(С1-С4)алкил и -S-(С1-С4)алкил.
18. Соединение по одному или большему количеству пп.1-17 или его фармацевтически приемлемая соль или сложный эфир в качестве лекарственного средства.
19. Фармацевтическая композиция, включающая терапевтически эффективное количество соединения по одному или большему количеству пп.1-17 или его фармацевтически приемлемой соли или сложного эфира и один или большее количество фармацевтически приемлемых носителей.
20. Фармацевтическая композиция по п.19, дополнительно включающая по меньшей мере одно другое противовирусное средство.
21. Применение композиции по одному или большему количеству пп.19 или 20 для борьбы с инфицированием вирусом гепатита С у млекопитающего, инфицированного или подвергающегося опасности инфицирования.
22. Способ борьбы с инфицированием вирусом гепатита С у млекопитающего, инфицированного или подвергающегося опасности инфицирования, способ включает введение млекопитающему терапевтически эффективное количество соединения по одному или большему количеству пп.1-17, его фармацевтически приемлемой соли или сложного эфира или его композиции.
23. Способ борьбы с инфицированием вирусом гепатита С у млекопитающего, инфицированного или подвергающегося опасности инфицирования, способ включает введение млекопитающему терапевтически эффективного количества комбинации соединения по одному или большему количеству пп.1-17 или его фармацевтически приемлемой соли или сложного эфира и по меньшей мере одного другого противовирусного средства; или его композиции.
24. Применение соединения по одному или большему количеству пп.1-17 или его фармацевтически приемлемой соли или сложного эфира для борьбы с инфицированием вирусом гепатита С у млекопитающего, инфицированного или подвергающегося опасности инфицирования.
25. Применение соединения по одному или большему количеству пп.1-17 или его фармацевтически приемлемой соли или сложного эфира, для приготовления лекарственного средства, предназначенного для борьбы с инфицированием вирусом гепатита С у млекопитающего, инфицированного или подвергающегося опасности инфицирования.
26. Изделие, включающее композицию, эффективную для борьбы с инфицированием вирусом гепатита С, и упаковочный материал, содержащий этикетку, которая указывает, что композицию можно применять для борьбы с инфицированием вирусом гепатита С, в котором композиция включает соединение по одному или большему количеству пп.1-17 или его фармацевтически приемлемую соль или сложный эфир.
27. Способ подавления репликации вируса гепатита С, включающий воздействие на вирус эффективного количества соединения по одному или большему количеству пп.1-17 или его соли или сложного эфира, при условиях, при которых подавляется репликация вируса гепатита С.
28. Применение соединения по одному или большему количеству пп.1-17 или его соли или сложного эфира для подавления репликации вируса гепатита С.
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-
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- 2007-01-29 US US11/668,197 patent/US7816348B2/en active Active
- 2007-02-01 RU RU2008135239/04A patent/RU2008135239A/ru unknown
- 2007-02-01 CA CA002638784A patent/CA2638784A1/en not_active Abandoned
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- 2007-02-01 JP JP2008552656A patent/JP2009525287A/ja active Pending
- 2007-02-01 BR BRPI0707689-4A patent/BRPI0707689A2/pt not_active IP Right Cessation
- 2007-02-01 KR KR1020087021597A patent/KR20080091294A/ko not_active Application Discontinuation
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WO2007087717A1 (en) | 2007-08-09 |
TW200804240A (en) | 2008-01-16 |
KR20080091294A (ko) | 2008-10-09 |
ZA200805855B (en) | 2009-10-28 |
UY30127A1 (es) | 2007-09-28 |
US20070219176A1 (en) | 2007-09-20 |
EP1984323A4 (en) | 2012-02-22 |
JP2009525287A (ja) | 2009-07-09 |
AU2007211789A1 (en) | 2007-08-09 |
US7816348B2 (en) | 2010-10-19 |
IL193151A0 (en) | 2009-02-11 |
PE20071326A1 (es) | 2008-02-21 |
CA2638784A1 (en) | 2007-08-09 |
EP1984323A1 (en) | 2008-10-29 |
CN101410368A (zh) | 2009-04-15 |
BRPI0707689A2 (pt) | 2011-05-10 |
AR059292A1 (es) | 2008-03-26 |
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