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AR104388A1 - Inhibidores de la replicación del virus de la inmunodeficiencia humana - Google Patents

Inhibidores de la replicación del virus de la inmunodeficiencia humana

Info

Publication number
AR104388A1
AR104388A1 ARP160101147A ARP160101147A AR104388A1 AR 104388 A1 AR104388 A1 AR 104388A1 AR P160101147 A ARP160101147 A AR P160101147A AR P160101147 A ARP160101147 A AR P160101147A AR 104388 A1 AR104388 A1 AR 104388A1
Authority
AR
Argentina
Prior art keywords
alkyl
aryl
heterocyclyl
haloalkyl
cycloalkyl
Prior art date
Application number
ARP160101147A
Other languages
English (en)
Inventor
Panda Manoranjan
Rao Mettu Mallikarjuna
Maheshwarappa Holehatti Shilpa
Onkardas Bora Rajesh
Thangathirupathy Srinivasan
Kumaravel Selvakumar
Wang Gan
Yang Zhong
N Nguyen Van
Belema Makonen
A Fridell Robert
B Beno Brett
A Meanwell Nicholas
Xiangdong Wang Alan
Pendri Annapurna
G Gentles Robert
A Bender John
Original Assignee
Bristol Myers Squibb Co
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of AR104388A1 publication Critical patent/AR104388A1/es

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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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • 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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    • C07C307/04—Diamides of sulfuric acids
    • C07C307/10—Diamides of sulfuric acids having nitrogen atoms of the sulfamide groups bound to carbon atoms of six-membered aromatic rings
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    • 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
    • C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/02—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C311/08—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
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    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
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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
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    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
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    • C07D207/325—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
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    • C07D209/04—Indoles; Hydrogenated indoles
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    • C07D209/80—[b, c]- or [b, d]-condensed
    • C07D209/82—Carbazoles; Hydrogenated carbazoles
    • C07D209/86—Carbazoles; Hydrogenated carbazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the ring system
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    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
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    • C07D211/96—Sulfur atom
    • C—CHEMISTRY; METALLURGY
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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
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/42—Radicals substituted by singly-bound nitrogen atoms having hetero atoms attached to the substituent nitrogen atom
    • C—CHEMISTRY; METALLURGY
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    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
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    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
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    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
    • C07D215/38—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
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    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/02—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
    • C07D217/08—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines with a hetero atom directly attached to the ring 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
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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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    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
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    • C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07C2602/04—One of the condensed rings being a six-membered aromatic ring
    • C07C2602/08—One of the condensed rings being a six-membered aromatic ring the other ring being five-membered, e.g. indane

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Abstract

Reivindicación 1: Un compuesto caracterizado por la fórmula (1), que incluye sales aceptables de este desde el punto de vista farmacéutico, en donde: R¹ᵃ y R¹ᵇ se seleccionan, cada uno independientemente, de hidrógeno, alquilo, arilo, arilalquilo, ariloxiarilo, cicloalquilo, heterociclilo, heterociclilalquilo y -alquil CO(Rˣ); en donde el heterociclilo está ligado a la molécula de origen a través de un átomo de carbono, y también en donde los grupos R¹ᵃ y R¹ᵇ se sustituyen con 0 - 4 grupos seleccionados independientemente de alquenilo, alcoxi, alcoxicarbonilo, alquilo, alquiltioxi, benciloxi, alquinilo, arilo, arilalquilo, ariloxi, ácido carboxílico, ciano, halo, haloalquilo, haloalcoxi, heterociclilo, heterociclilalquilo, hidroxi, hidroxialquilo, tioxi, -CH₂NH₂, -alquil-heteroarilo, -CO-alquilo, CO(Rˣ), -CON(Rʸ)₂, -NHCON(Rʸ)₂, -NHCO-alquilo, -NHCO₂-alquilo, -NHSO₂-alquilo, -OCH₂-arilo, -SO₂-alquilo, -SO₂-N(Rʸ)₂ y -SO₂-heterociclilo; o R¹ᵃ y R¹ᵇ junto con el átomo de nitrógeno al que están unidos, forman un heterociclo que se sustituye con 0 - 4 grupos seleccionados independientemente de alquenilo, alcoxi, alcoxicarbonilo, alquilo, alquiltioxi, benciloxi, alquinilo, arilo, ácido carboxílico, ciano, halo, haloalquilo, haloalcoxi, hidroxi, hidroxialquilo, tioxi, -CH₂NH₂, -alquil-heteroarilo, -CO-alquilo, -CO(Rˣ), -CON(Rʸ)₂, -N(Rʸ)CON(Rʸ)₂, -N(Rʸ)CO-alquilo, -N(Rʸ)CO₂-alquilo, -N(Rʸ)SO₂-alquilo, -OCH₂-arilo, -SO₂-alquilo, -SO₂-N(Rʸ)₂ y -SO₂-heterociclilo; R² es -H, C₁₋₄ alquilo o C₃₋₄ cicloalquilo; R³ es -H, C₁₋₄ alquilo o C₃₋₄ cicloalquilo; R⁴ es -H, alquilo, arilo, C₅₋₁₀ bicicloalquilo, C₃₋₇ cicloalquilo o heteroarilo con 0 - 4 grupos seleccionados independientemente de alquenoxi, alquenilo, alcoxi, alcoxicarbonilo, alquilo, benciloxi, carboamida, ciano, halo, haloalquilo, haloalquiloxi, -NHCO(alquilo), -SO₂(Rˣ), -OH y -CH₂OH; R⁵ y R⁶ son independientemente H o alquilo, o R⁵ y R⁶, junto con los átomos a los que están unidos, forman un C₃₋₄ cicloalquilo; R⁷ es -H, alquilo, arilo, heterociclilo o C₃₋₇ cicloalquilo, en donde el arilo o el heterociclilo se sustituyen con 0 - 3 grupos seleccionados de -OH, -NHCO-alquilo, -NHCON(alquilo)₂, -NHCO₂-alquilo, -CONH₂, -CN, -SO₂N(alquilo)₂, alcoxi, alquilo, halo, haloalcoxi y haloalquilo; R⁸ es -H, alquilo, cicloalquilo, haloalquilo, halocicloalquilo, alquenilo o ariloxialquilo; o R⁷ y R⁸, junto con el átomo de nitrógeno al que están unidos, forman un heterociclo que se sustituye con 0 - 4 grupos seleccionados independientemente de -OH, -NHCO-alquilo, -NHCON(alquilo)₂, -NHCO₂-alquilo, -CONH₂, -CN, -SO₂N(alquilo)₂, alcoxi, alquilo, halo, haloalcoxi, y haloalquilo; Rˣ es dialquilamina o un heterociclo que contiene nitrógeno que está unido al fragmento de origen a través de un átomo de nitrógeno; y cada Rʸ es independientemente hidrógeno, alquilo, haloalquilo o arilo.
ARP160101147A 2015-04-23 2016-04-22 Inhibidores de la replicación del virus de la inmunodeficiencia humana AR104388A1 (es)

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