AR057455A1 - Inhibidores de la transcriptasa reversa de vih y composicion farmaceutica - Google Patents
Inhibidores de la transcriptasa reversa de vih y composicion farmaceuticaInfo
- Publication number
- AR057455A1 AR057455A1 ARP060102994A ARP060102994A AR057455A1 AR 057455 A1 AR057455 A1 AR 057455A1 AR P060102994 A ARP060102994 A AR P060102994A AR P060102994 A ARP060102994 A AR P060102994A AR 057455 A1 AR057455 A1 AR 057455A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- group
- nr3r4
- optionally
- fluoroalkyl
- Prior art date
Links
- 108010078851 HIV Reverse Transcriptase Proteins 0.000 title abstract 3
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 10
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 125000003709 fluoroalkyl group Chemical group 0.000 abstract 5
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- 229910052757 nitrogen Inorganic materials 0.000 abstract 3
- 150000003839 salts Chemical class 0.000 abstract 3
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 125000002950 monocyclic group Chemical group 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 238000011321 prophylaxis Methods 0.000 abstract 2
- 229920006395 saturated elastomer Polymers 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 238000011282 treatment Methods 0.000 abstract 2
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 1
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 1
- 208000030507 AIDS Diseases 0.000 abstract 1
- 101100203601 Caenorhabditis elegans sor-3 gene Proteins 0.000 abstract 1
- 208000031886 HIV Infections Diseases 0.000 abstract 1
- 208000037357 HIV infectious disease Diseases 0.000 abstract 1
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical compound O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 abstract 1
- 241000347391 Umbrina cirrosa Species 0.000 abstract 1
- 239000003242 anti bacterial agent Substances 0.000 abstract 1
- 229940088710 antibiotic agent Drugs 0.000 abstract 1
- 239000003443 antiviral agent Substances 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 230000003111 delayed effect Effects 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 abstract 1
- 239000002955 immunomodulating agent Substances 0.000 abstract 1
- 229940121354 immunomodulator Drugs 0.000 abstract 1
- 239000004615 ingredient Substances 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 229940042443 other antivirals in atc Drugs 0.000 abstract 1
- 125000004043 oxo group Chemical group O=* 0.000 abstract 1
- 125000003373 pyrazinyl group Chemical group 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 1
- 239000003419 rna directed dna polymerase inhibitor Substances 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 229960005486 vaccine Drugs 0.000 abstract 1
Classifications
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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
- C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/45—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the singly-bound nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfonamides
- C07C311/46—Y being a hydrogen or a carbon atom
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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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
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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
- 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
- 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
- C07C255/00—Carboxylic acid nitriles
- C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
- C07C255/54—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and etherified hydroxy groups bound to the carbon skeleton
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C255/00—Carboxylic acid nitriles
- C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
- C07C255/58—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
- C07C255/60—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton at least one of the singly-bound nitrogen atoms being acylated
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C307/00—Amides of sulfuric acids, i.e. compounds having singly-bound oxygen atoms of sulfate groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
- C07C307/04—Diamides of sulfuric acids
- C07C307/06—Diamides of sulfuric acids having nitrogen atoms of the sulfamide groups bound to acyclic carbon atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C317/00—Sulfones; Sulfoxides
- C07C317/26—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
- C07C317/32—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
- C07C317/34—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having sulfone or sulfoxide groups and amino groups bound to carbon atoms of six-membered aromatic rings being part of the same non-condensed ring or of a condensed ring system containing that ring
- C07C317/38—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having sulfone or sulfoxide groups and amino groups bound to carbon atoms of six-membered aromatic rings being part of the same non-condensed ring or of a condensed ring system containing that ring with the nitrogen atom of at least one amino group being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfones
- C07C317/40—Y being a hydrogen or a carbon atom
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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
- C07D209/04—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
- 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
- C07D213/62—Oxygen or sulfur atoms
- C07D213/63—One oxygen atom
- C07D213/65—One oxygen atom attached in position 3 or 5
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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
- C07D213/60—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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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- 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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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
- C07D249/06—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
- C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
- C07D263/56—Benzoxazoles; Hydrogenated benzoxazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
- C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
- C07D271/06—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
- C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
- C07D271/10—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
- C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
- C07D271/10—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
- C07D271/107—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles with two aryl or substituted aryl radicals attached in positions 2 and 5
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
- C07D277/62—Benzothiazoles
- C07D277/64—Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
- C07D333/46—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings substituted on the ring sulfur atom
- C07D333/48—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings substituted on the ring sulfur atom by oxygen atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
- C07C2601/14—The ring being saturated
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Virology (AREA)
- Engineering & Computer Science (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- AIDS & HIV (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Indole Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pyridine Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
Estos compuestos son inhibidores de transcriptasa reversa de VIH. Los compuestos y sus sales farmacéuticamente aceptables son utiles en la inhibicion de transcriptasa reversa de VIH, la profilaxis y tratamiento de la infeccion mediante VIH y en la profilaxis, retraso en la aparicion, y tratamiento de SIDA. Los compuestos y sus sales se pueden emplear como ingredientes en composiciones farmacéuticas, opcionalmente en combinacion con otros antivirales, inmunomoduladores, antibioticos o vacunas. Reivindicacion 1: Un compuesto de formula (1), o una sal farmacéuticamente aceptable del mismo, en la que: R1 y R2 se seleccionan independientemente del grupo constituido por: a) H, b) alquilo C1-6, c) cicloalquilo C3-6, d) fluoroalquilo C1-3, e) NO2, f) halogeno, g) OR3, h) O(CH2)sOR3, i) CO2R3, j) (CO)NR3R4, k) O(CO)NR3R4, 1) N(R3)(CO)NR3R4. m) N(R3)(CO)R4, n) N(R3)(CO)OR3, o) SO2NR3R4. p) N(R3)SO2R4, q) S(O)mR3, r) CN, s) NR3R4, t) N(R3)(CO)NR3R4, y u) O(CO)R3; A es arilo, cicloalquilo C3-7, o heterociclilo; V es -C(R5R6)-; X se selecciona del grupo constituido por -O-, -NH-, y -C(R5R6)-; Y se selecciona del grupo constituido por de -O-, -C(R5R6)-, y -S(O)m-; R5 y R6 se seleccionan independientemente del grupo constituido por hidrogeno, alquilo C1-6, fluoroalquilo C1-3, y OR3; R10 es un heterociclilo seleccionado del grupo constituido por las formulas (2) a (28), donde R12 y R13 se seleccionan independientemente del grupo constituido por hidrogeno, halogeno, oxo, NO2, CN, OR3, O(CH2)tCF3, CO2R3, CONR3R4, O(CH2)tNR3R4, O(CH2)vCOR3, S(O)mR3, SO2NR3R4, alquilo C1-6, fluoroalquilo C1-3, cicloalquilo C3-6, y NR3R4; R3 y R4 se seleccionan independientemente del grupo constituido por hidrogeno, alquilo C1-6, fluoroalquilo C1-3, y cicloalquilo C3-6; o, alternativamente y opcionalmente, cuando R3 y R4 están en un grupo NR3R4, entonces: A) uno de R3 y R4 se selecciona del grupo que consta de hidrogeno, alquilo C1-6, fluoroalquilo C1-3, y cicloalquilo C3-6, y el otro R3 y R4 es alquilo Cl-6 sustituido con O-alquiloC1-6, C(O)RA, CO2RA, C(O)N(RA)RB; o (B) R3 y R4 conjuntamente con átomo de nitrogeno al cual se unen formando: i) una anillo monocíclico saturado o insaturado de 4-7 miembros que contienen opcionalmente 1 o 2 heteroátomos además del nitrogeno unidos a R3 y R4 seleccionados de N, O, y S, donde la S se oxida opcionalmente a S(O) o S(O)2, o ii) un sistema anillo bicíclico de 7 a 12-miembros en el que cada anillo en ii) es independiente de, está fusionado a, o unido mediante puente con el otro anillo y cada anillo estará saturado o insaturado, y en el que sistema de anillo bicíclico contiene opcionalmente de 1 a 3 heteroátomos además del nitrogeno unido a R3 y R4 seleccionados de N, O, y S, donde la S se oxida opcionalmente a S(O) o S(O)2, y en el que el anillo monocíclico del sistema anillo bicíclico está sustituido opcionalmente con de 1 a 3 sustituyentes cada uno de los cuales es independientemente: alquilo C1-6; haloalquilo C1-6, alquilo C1-6 sustituido con OH, O-alquilC1-6, O-haloalquilC1-6, CN, NO2, N(RA)RB, C(O)N(RA)RB, C(O)RA, CO2RA, SRA, S(O)RA SO2RA, o SO2N(RA)RB; O-alquilC1-6; O-haloalquilC1-6; OH; oxo; halogeno; CN; N02; N(RA)RB; C(O)N(RA)RB; C(O)RA; C(O)- haloalquilC1-6; C(O)ORA; OC(O)N(RA)RB; SRA; S(O)RA; S(O)2RA; S(O)2N(RA)RB; N(RA)CORB; o N(RA)SO2RB y en el que cada RA es independientemente H o alquilo C1-6, y cada RB es independientemente H o alquilo 1-6; HetA es heteroarilo seleccionado del grupo constituido por piridinilo, pirimidinilo, y pirazinilo; s es 1-5; t es 2-3; v es 1-2; y m, en cada caso en el cual aparece, se selecciona independientemente de 0-2; y siempre que cuando X es -C(R5R6)-, entonces ni R1 ni R2 es OR3.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US70179705P | 2005-07-22 | 2005-07-22 | |
| US72791605P | 2005-10-18 | 2005-10-18 | |
| US79070506P | 2006-04-10 | 2006-04-10 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR057455A1 true AR057455A1 (es) | 2007-12-05 |
Family
ID=37488064
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP060102994A AR057455A1 (es) | 2005-07-22 | 2006-07-12 | Inhibidores de la transcriptasa reversa de vih y composicion farmaceutica |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US7807684B2 (es) |
| EP (2) | EP1912935A2 (es) |
| JP (1) | JP5075821B2 (es) |
| KR (1) | KR20080039379A (es) |
| AR (1) | AR057455A1 (es) |
| AT (1) | ATE459624T1 (es) |
| AU (1) | AU2006276231B2 (es) |
| CA (1) | CA2615019C (es) |
| CR (1) | CR9694A (es) |
| DE (1) | DE602006012683D1 (es) |
| IL (1) | IL188615A0 (es) |
| MA (1) | MA29745B1 (es) |
| MX (1) | MX2008000959A (es) |
| NO (1) | NO20080913L (es) |
| PE (1) | PE20070243A1 (es) |
| TW (1) | TW200738702A (es) |
| WO (2) | WO2007015812A2 (es) |
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-
2006
- 2006-07-12 AR ARP060102994A patent/AR057455A1/es not_active Application Discontinuation
- 2006-07-14 TW TW095125857A patent/TW200738702A/zh unknown
- 2006-07-17 US US11/487,885 patent/US7807684B2/en not_active Expired - Fee Related
- 2006-07-17 DE DE602006012683T patent/DE602006012683D1/de active Active
- 2006-07-17 EP EP06787584A patent/EP1912935A2/en not_active Withdrawn
- 2006-07-17 JP JP2008522860A patent/JP5075821B2/ja not_active Expired - Fee Related
- 2006-07-17 KR KR1020087001775A patent/KR20080039379A/ko not_active Ceased
- 2006-07-17 WO PCT/US2006/027700 patent/WO2007015812A2/en not_active Ceased
- 2006-07-17 WO PCT/US2006/027694 patent/WO2007015809A2/en not_active Ceased
- 2006-07-17 AU AU2006276231A patent/AU2006276231B2/en not_active Ceased
- 2006-07-17 AT AT06787590T patent/ATE459624T1/de not_active IP Right Cessation
- 2006-07-17 EP EP06787590A patent/EP1910360B1/en active Active
- 2006-07-17 MX MX2008000959A patent/MX2008000959A/es unknown
- 2006-07-17 CA CA2615019A patent/CA2615019C/en not_active Expired - Fee Related
- 2006-07-18 PE PE2006000863A patent/PE20070243A1/es not_active Application Discontinuation
-
2008
- 2008-01-06 IL IL188615A patent/IL188615A0/en unknown
- 2008-01-28 CR CR9694A patent/CR9694A/es not_active Application Discontinuation
- 2008-02-19 MA MA30661A patent/MA29745B1/fr unknown
- 2008-02-21 NO NO20080913A patent/NO20080913L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| PE20070243A1 (es) | 2007-05-12 |
| JP2009502787A (ja) | 2009-01-29 |
| US7807684B2 (en) | 2010-10-05 |
| WO2007015809A3 (en) | 2007-03-29 |
| AU2006276231A1 (en) | 2007-02-08 |
| EP1912935A2 (en) | 2008-04-23 |
| CR9694A (es) | 2008-02-20 |
| MA29745B1 (fr) | 2008-09-01 |
| WO2007015812A3 (en) | 2007-04-12 |
| WO2007015809A2 (en) | 2007-02-08 |
| CA2615019C (en) | 2011-12-06 |
| WO2007015812A2 (en) | 2007-02-08 |
| ATE459624T1 (de) | 2010-03-15 |
| CA2615019A1 (en) | 2007-02-08 |
| NO20080913L (no) | 2008-04-09 |
| JP5075821B2 (ja) | 2012-11-21 |
| IL188615A0 (en) | 2008-04-13 |
| DE602006012683D1 (es) | 2010-04-15 |
| AU2006276231B2 (en) | 2010-11-11 |
| TW200738702A (en) | 2007-10-16 |
| US20070021442A1 (en) | 2007-01-25 |
| KR20080039379A (ko) | 2008-05-07 |
| EP1910360A2 (en) | 2008-04-16 |
| EP1910360B1 (en) | 2010-03-03 |
| MX2008000959A (es) | 2008-03-27 |
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