AR064724A1 - Compuestos amino n-halogenados y derivados composiciones y metodos para usarlos - Google Patents

Compuestos amino n-halogenados y derivados composiciones y metodos para usarlos

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Publication number
AR064724A1
AR064724A1 ARP080100005A ARP080100005A AR064724A1 AR 064724 A1 AR064724 A1 AR 064724A1 AR P080100005 A ARP080100005 A AR P080100005A AR P080100005 A ARP080100005 A AR P080100005A AR 064724 A1 AR064724 A1 AR 064724A1
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Argentina
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alkyl
aryl
group
cycloalkyl
atoms
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ARP080100005A
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Novabay Pharmaceuticals Inc
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/69—Boron compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • 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
    • A61P31/04—Antibacterial agents
    • 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
    • A61P31/10—Antimycotics
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/07—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing oxygen atoms bound to the carbon skeleton
    • C07C309/09—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing oxygen atoms bound to the carbon skeleton containing etherified hydroxy groups bound to the carbon skeleton
    • C07C309/10—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing oxygen atoms bound to the carbon skeleton containing etherified hydroxy groups bound to the carbon skeleton with the oxygen atom of at least one of the etherified hydroxy groups further bound to an acyclic carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/07—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing oxygen atoms bound to the carbon skeleton
    • C07C309/12—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing oxygen atoms bound to the carbon skeleton containing esterified hydroxy groups bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/17—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing carboxyl groups bound to the carbon skeleton
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    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/19—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of a saturated carbon skeleton containing rings
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/24—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of a carbon skeleton containing six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/25—Sulfonic acids having sulfo groups bound to carbon atoms of rings other than six-membered aromatic rings of a carbon skeleton
    • C07C309/26—Sulfonic acids having sulfo groups bound to carbon atoms of rings other than six-membered aromatic rings of a carbon skeleton containing nitrogen atoms, not being part of nitro or nitroso groups, bound to the carbon skeleton
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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
    • C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/31—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atoms of the sulfonamide groups bound to acyclic carbon atoms
    • C07C311/32—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atoms of the sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/45—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
    • C—CHEMISTRY; METALLURGY
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    • 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
    • C07C317/28—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 acyclic carbon atoms of the carbon skeleton
    • 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
    • C07D211/36—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
    • C07D211/40—Oxygen atoms
    • C07D211/44—Oxygen atoms attached in position 4
    • C07D211/52—Oxygen atoms attached in position 4 having an aryl radical as the second substituent in position 4
    • C—CHEMISTRY; METALLURGY
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    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/04—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D307/18—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings 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
    • C07D307/22—Nitrogen atoms not forming part of a nitro radical
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    • C07—ORGANIC CHEMISTRY
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    • 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
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
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    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Chemical & Material Sciences (AREA)
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  • Dermatology (AREA)
  • Engineering & Computer Science (AREA)
  • Virology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

La presente solicitud se refiere a compuestos y composiciones bactericidas, antibacterianos, antiinfecciosos, antimicrobianos, esporicidas, desinfectantes, antifungicos y antivirales activos, y a nuevos usos de estas composiciones en terapia. Esta memoria descriptiva también describe métodos de uso para los nuevos compuestos y composiciones. La memoria descriptiva además describe métodos para preparar estos compuestos. Reivindicacion 1: Un compuesto que comprende la formula (1); donde X1 es Cl o Br; X2 es H o se selecciona del grupo que consiste en Cl, Br, alquilo C1-5, cicloalquilo C3-6, cicloalquil C3-6-alquilo C1-3 y haloalquilo C1-5; R1 y R2 se seleccionan cada uno independientemente del grupo que consiste en alquilo C1-5, haloalquilo C1-5, cicloalquilo C3-12, cicloalquil C3-6-alquilo C1-3, aril C6-10-alquilo C1-4, arilo C6-14 y heterocicloalquilo que contiene 2-10 átomos de C y de 1 a 4 heteroátomos seleccionados de N, O o S, o R1 y R2 junto con el átomo de C al cual están unidos forman un carbocíclico C3-12 o heterociclilo C3-12 con al menos un heteroátomo seleccionado de N, O o S en el anillo; R0 y R00 son cada uno independientemente H, F o los mismos de R1 y R2; Y es un miembro seleccionado de un enlace simple -O- y un grupo alquilenilo C1-18 divalente en el cual opcionalmente uno o dos grupos metileno están reemplazados con un grupo metileno mono- o di-sustituido, u opcionalmente donde uno o dos grupos metileno están reemplazados con 1 o 2 -NR'-, -O-, -S-, -S(=O)-, >C=O o -S(=O)2-, donde R' es H o se selecciona del grupo que consiste en Cl, Br, alquilo C1-5, cicloalquilo C3-6, arilo C6-10, aril C6-10-alquilo C1-4, alquil C1-5-NHC(=O)-, alcoxi C1-5-C(=O)-, RaRbNC(=O)-, alquil C1-5-C(=O)-, aril C6-10-C(=O)-, aril C6-10-alquil C1-4-C(=O)-, arilo C6-14, heteroarilo que comprende de 4 a 10 átomos anulares con al menos un heteroátomo seleccionado de O, S, y N en el anillo, y heterociclialquilo que contiene 2-10 átomos de C y de 1 a 4 heteroátomos seleccionados de N, O o S, donde Ra y Rb son cada uno independientemente H, alquilo C1-5, cicloalquilo C3-6, alquil C1-5-NHC(=O)-, alquil C1-5-C(=O)-, arilo C6-14, aril C6-10-alquil C1-4, heteroarilo que comprende de 4 a 10 átomos anulares con al menos un heteroátomo seleccionado de O, S, y N en el anillo, y heterociclialquilo C1-4, donde el grupo heterocicloalquilo contiene 2-10 átomos de C y de 1 a 4 heteroátomos seleccionados de N, O o S, donde cuando R1 es alquilo C1-5 o R1 y R2 junto con el átomo de C al cual están unidos forman un cicloalquilo C3-6, entonces X2 debe ser alquilo C1-5, cicloalquilo C3-6, cicloalquil C3-6-alquilo C1-3 o haloalquilo C1-5; o cuando R1 es alquilo C1-5, entonces R2 debe ser haloalquilo C1-5, cicloalquilo C3-12 o cicloalquil C3-6-alquilo C1-3; o cuando R1 es alquilo C1-5 o R1 y R2 junto con el átomo de C al cual están unidos forman un cicloalquilo C3-6, entonces Y debe ser -O- o un grupo alquilenilo C1-18 divalente donde uno o dos grupos metileno están reemplazados con un grupo metileno sustituido o con -NR'-, -O-, -S-, -S(=O)-, o -S(=O)2-, donde R' es H o se selecciona del grupo que consiste en Cl, Br, alquilo C1-5, cicloalquilo C3-6, arilo C6-10, aril C6-10-alquilo C1-4, alquil C1-5-NHC(=O)-, alcoxi C1-5-C(=O)-, RaRbNC(=O)-, alquil C1-5-C(=O)-, aril C6-10-C(=O)-, aril C6-10-alquil C1-4-C(=O)-, arilo C6-14, heteroarilo que comprende de 4 a 10 átomos anulares con al menos un heteroátomo seleccionado de O, S, y N en el anillo, y heterociclialquilo que contiene 2-10 átomos de C y de 1 a 4 heteroátomos seleccionados de N, O o S, donde Ra y Rb son cada uno independientemente H, alquilo C1-5, cicloalquilo C3-6, alquil C1-5-NHC(=O)-, alquil C1-5-C(=O)-, arilo C6-14, aril C6-10-alquil C1-4, heteroarilo que comprende de 4 a 10 átomos anulares con al menos un heteroátomo seleccionado de O, S, y N en el anillo, y heterociclialquilo C1-4, donde el grupo heterocicloalquilo contiene 2-10 átomos de C y de 1 a 4 heteroátomos seleccionados de N, O o S, Z se selecciona del grupo que consiste en -SO3H, -PO3H2, una sal o éster de éstos, y un isostero ácido de estos pero no -C(=O)OH; o se selecciona del grupo que consiste en -S(=O)2NRcRd, -S(=O)2NHC(=O)Re, - S(=O)2OC(=O)NRcRd, -S(=O)2NRcC(=O)NRcRd y -S(=O)(N=)C(OH)NRcRd, donde Rc y Rd son cada uno independientemente H o se seleccionan independientemente del grupo que consiste en alquilo C1-5, cicloalquilo C3-6, alquil C1-5-NHC(=O)-, alquil C1-5-C(=O)-, arilo C6-10-C(=O), aril C6-10-alquil C1-4-C(=O)-, arilo C6-14, aril C6-10-alquilo C1-4, heteroarilo comprende de 4 a 10 átomos anulares con al menos un heteroátomo seleccionado de O, S, y N en el anillo, y heterociclilo que contiene 2-10 átomos de C y de 1 a 4 heteroátomos seleccionados de N, O o S, y Re es H o se selecciona del grupo que consiste en alquilo C1-5, cicloalquilo C3-6, arilo C6-14, aril C6-10-alquilo C1-4, heteroarilo comprende de 4 a 10 átomos anulares con al menos un heteroátomo seleccionado de O, S, y N en el anillo, y heterociclilo que contiene 2-10 átomos de C y de 1 a 4 heteroátomos seleccionados de N, O o S, o una sal, un oxido de amina de dicho compuesto, o un derivado o un bioisostero o un profármaco he dicho compuesto. Reivindicacion 52: Un proceso para preparar un compuesto de la reivindicacion 1, proceso que comprende uno o varios de los siguientes pasos: (1) proteccion del grupo amino; (2) doble alquilacion del átomo de C en posicion alfa a un grupo amino; (3) reduccion de un grupo carboxi al amino alcohol (reduccion directa o por medio de un éster); (4) introduccion del grupo Z (por ejemplo, -SO3H o -PO3H2); (5) elongacion de estructura central de Y; (6) desproteccion del grupo amino; (7) introduccion de X2 no halo después de la desproteccion del grupo amino; (8)halogenacion para introducir X1 y X2 o solo X1 si X2 es distinto de halogeno; (9) formacion de sal de Z o cualquier grupo básico o ácido de la molécula; (10) conversion de una sal en un ácido o una base; (11) conversion de una sal en otra sal; o (12) derivacion del grupo Z o W u otros grupos de los compuestos de la reivindicacion 1 o 2.
ARP080100005A 2006-12-29 2008-01-02 Compuestos amino n-halogenados y derivados composiciones y metodos para usarlos AR064724A1 (es)

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US8415497B2 (en) 2013-04-09
EP2120965B1 (en) 2014-11-05
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