AR104389A1 - Inhibidores de la replicación del virus de inmunodeficiencia humana - Google Patents

Inhibidores de la replicación del virus de inmunodeficiencia humana

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Publication number
AR104389A1
AR104389A1 ARP160101148A ARP160101148A AR104389A1 AR 104389 A1 AR104389 A1 AR 104389A1 AR P160101148 A ARP160101148 A AR P160101148A AR P160101148 A ARP160101148 A AR P160101148A AR 104389 A1 AR104389 A1 AR 104389A1
Authority
AR
Argentina
Prior art keywords
alkyl
independently selected
alkoxy
aryl
heterocyclyl
Prior art date
Application number
ARP160101148A
Other languages
English (en)
Inventor
Thangathirupathy Srinivasan
Belema Makonen
A Fridell Robert
R Beno Brett
A Meanwell Nicholas
Wang Gan
Xiangdong Wang Alan
Yang Zhong
N Nguyen Van
d lopez Omar
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 AR104389A1 publication Critical patent/AR104389A1/es

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    • C12N7/00—Viruses; Bacteriophages; Compositions thereof; Preparation or purification thereof
    • C12N7/04—Inactivation or attenuation; Producing viral sub-units
    • C12N7/06—Inactivation or attenuation by chemical treatment
    • 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
    • A61K31/13—Amines
    • A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
    • 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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    • A61P31/18—Antivirals for RNA viruses for HIV
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/22—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/22—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
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    • C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/04—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms
    • C07C275/20—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an unsaturated carbon skeleton
    • C07C275/24—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing six-membered aromatic rings
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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
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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
    • C07C311/03—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C311/06—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms to acyclic carbon atoms of hydrocarbon radicals substituted by carboxyl groups
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    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
    • C07C311/19—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
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    • 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
    • C07C323/51—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 atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/60—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 atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton with the carbon atom of at least one of the carboxyl groups bound to nitrogen atoms
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    • 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
    • C07D213/61—Halogen atoms or nitro radicals
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    • 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
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
    • C07D235/26—Oxygen atoms
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    • 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
    • C07D271/113—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
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    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
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    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
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    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
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    • C07D317/44—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D317/46—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D317/48—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring
    • C07D317/62—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring 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 atoms of the carbocyclic ring
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    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
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    • C07K5/022—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -X-C(=O)-(C)n-N-C-C(=O)-Y-; X and Y being heteroatoms; n being 1 or 2
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    • C12N2740/00011—Details
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    • C12N2740/16011—Human Immunodeficiency Virus, HIV
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  • Medicinal Chemistry (AREA)
  • Genetics & Genomics (AREA)
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  • Communicable Diseases (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • AIDS & HIV (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyridine Compounds (AREA)

Abstract

Reivindicación 1: Un compuesto caracterizado por la fórmula (1), que incluye sus sales farmacéuticamente aceptables, en donde: A es un enlace o se selecciona de alquilo C₁₋₅, alquenilo C₂₋₅, alquinilo C₂₋₅, arilo, cicloalquilo C₃₋₆, bicicloalquilo C₂₋₅, -CO-, -CS-, -C(=N-CN)-, heterociclilo, nitrógeno, azufre, oxígeno, -O-(alquil C₂₋₄)-O-, -N(Rˣᵃ)CON(Rˣᵇ)- y ferroceno; cada R¹ se selecciona, de modo independiente, de hidrógeno, alquilo C₁₋₄, alquenilo C₂₋₄, alcoxi C₁₋₄, (alcoxialquilo) C₂₋₄, (alcoxi C₁₋₄)carbonilo, alquil C₁₋₄-tioxi, benciloxi, alquinilo C₂₋₄, arilo, ácido carboxílico, ciano, halógeno, haloalquilo C₁₋₄, haloalcoxi C₁₋₄, heterociclilo, hidroxi, hidroxialquilo C₁₋₄, tioxi, -CH₂NH₂, -(alquil C₁₋₄)-heteroarilo, -CO-(alquilo C₁₋₄), -CO(Rʸ), -CON(Rˣᵃ)₂, -NHCON(Rˣᵃ)₂, -NHCO-(alquilo C₁₋₄), -NHCO₂-(alquilo C₁₋₄), -NHSO₂-(alquilo C₁₋₄), -OCH₂-arilo, -SO₂-(alquilo C₁₋₄), -SO₂-N(Rˣᵃ)₂, -SO₂-heterociclilo, -N(Rˣᵃ)₂ y nitro; p es de 0 a 5; Rˣᵃ y Rˣᵇ se seleccionan, de modo independiente, de hidrógeno, alquilo o haloalquilo; Rʸ se selecciona de (dialquilamina) C₂₋₄ o heterociclilo que contiene nitrógeno y se une con su fragmento principal a través de su nitrógeno; X y X¹ son cada uno, de modo independiente, un enlace o se seleccionan de los restos del grupo de fórmulas (2), en donde la unión de X y X¹ con la estructura principal es tal que el enlace con la flecha se orienta hacia el respectivo nitrógeno mostrado en la fórmula (1); sin embargo, siempre que, cuando A es un enlace, al menos un X o X¹ no sea un enlace; cada n es, de modo independiente, de 0 a 2; cada R⁴ se selecciona, de modo independiente, de hidrógeno, alquilo C₁₋₃, alquenilo C₁₋₃, arilo, aril(alquilo C₁₋₂), hidroxilo y halógeno, con la opción de que dos R⁴ en los mismos carbonos o en carbonos adyacentes formen un anillo; R²ᵃ y R²ᵇ se seleccionan, de modo independiente, de hidrógeno, alquilo C₁₋₄, alquenilo C₃₋₄, alquinilo C₃₋₅ y cicloalquilo C₃₋₄ y cada uno está opcionalmente sustituido con 1 a 3 sustituyentes seleccionados de halógeno, hidroxilo, alcoxi C₁₋₂ y haloalcoxi C₁₋₂; G y G se seleccionan cada uno, de modo independiente, de un compuesto de fórmula (3) y de fórmula (4); cada Y es, de modo independiente, oxígeno o azufre; cada J es un enlace o se selecciona, de modo independiente, de arilo, heterociclilo o cicloalquilo C₃₋₇; cada R⁵ se selecciona, de modo independiente, de hidrógeno, alcoxi C₁₋₄, alquilo C₁₋₄, halógeno, bicicloalquilo C₂₋₅, haloalcoxi C₁₋₄, haloalquilo C₁₋₄, -CONH₂, -CN, -NHCO(alquilo C₁₋₄), -NHCON(alquilo C₁₋₄)₂, -NHCO₂(alquilo C₁₋₄), -OH, -SO₂N(alquilo C₁₋₄)₂ y heterociclilo; cada r es, de modo independiente, de 0 a 5; cada R⁶ se selecciona, de modo independiente, de hidrógeno, alquilo C₁₋₄, alquenilo C₂₋₄ y cicloalquilo C₃₋₄, opcionalmente sustituido con halógeno, hidroxilo, alcoxi C₁₋₂ o haloalcoxi C₁₋₂; cada L se selecciona, de modo independiente, de un anillo heteroarilo de cinco o seis miembros; cada R⁷ se selecciona, de modo independiente, de alcoxi C₁₋₃, alquilo C₁₋₃, halógeno, haloalcoxi C₁₋₃, haloalquilo C₁₋₃, -CONH₂, -CN, -OH, -alquino C₂₋₅, -NHCO(alquilo C₁₋₃), -NHCON(alquilo C₁₋₃)₂, -NHCO₂(alquilo C₁₋₃), -SO₂N(alquilo C₁₋₃)₂ y alquino C₂₋₆ opcionalmente sustituido con 1 a 2 haluros; cada s es, de modo independiente, de 0 a 4; E y E se seleccionan cada uno, de modo independiente, de alquilo C₁₋₈, alquenilo C₂₋₈, alquinilo C₂₋₈, bicicloalquilo C₅₋₈, cicloalquilo C₃₋₇, arilo, heterociclilo y un grupo alquilo C₁₋₂ que contiene cualquiera de los siguientes grupos: bicicloalquilo C₅₋₈, cicloalquilo C₃₋₇, arilo y heterociclilo; R³ᵃ y R³ᵇ se seleccionan cada uno, de modo independiente, de alquen C₂₋₄-oxi, alquenilo C₂₋₄, alcoxi C₁₋₄, (alcoxialquilo) C₂₋₄, (alcoxi C₁₋₄)carbonilo, alquilo C₁₋₄, haloalquilo C₁₋₄, haloalcoxi C₁₋₄, carboxiamida, halógeno, -CN, -NHCO(alquilo C₁₋₄), -OH, hidroxialquilo C₁₋₄ y -SO₂N-heterociclo; y q y q son cada uno, de modo independiente, de 0 a 5; en donde la unión de cada de X, X¹ o N a A puede estar en el mismo átomo o en diferentes átomos de A.
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