AR037097A1 - Compuestos acilsulfonamidas, composiciones farmaceuticas y el uso de dichos compuestos para la preparacion de un medicamento - Google Patents

Compuestos acilsulfonamidas, composiciones farmaceuticas y el uso de dichos compuestos para la preparacion de un medicamento

Info

Publication number
AR037097A1
AR037097A1 ARP020103736A ARP020103736A AR037097A1 AR 037097 A1 AR037097 A1 AR 037097A1 AR P020103736 A ARP020103736 A AR P020103736A AR P020103736 A ARP020103736 A AR P020103736A AR 037097 A1 AR037097 A1 AR 037097A1
Authority
AR
Argentina
Prior art keywords
substituted
cycloalkyl
phenyl
substituents
defined above
Prior art date
Application number
ARP020103736A
Other languages
English (en)
Original Assignee
Novartis Ag
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
Priority claimed from GB0124028A external-priority patent/GB0124028D0/en
Priority claimed from GB0124027A external-priority patent/GB0124027D0/en
Priority claimed from GB0124839A external-priority patent/GB0124839D0/en
Priority claimed from GB0127173A external-priority patent/GB0127173D0/en
Priority claimed from GB0127174A external-priority patent/GB0127174D0/en
Priority claimed from GB0127343A external-priority patent/GB0127343D0/en
Priority claimed from GB0211524A external-priority patent/GB0211524D0/en
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of AR037097A1 publication Critical patent/AR037097A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/22—Bridged ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/08—Antiseborrheics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/28—Antiandrogens
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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
    • C07C311/50—Compounds containing any of the groups, X being a hetero atom, Y being any atom
    • C07C311/51—Y being a hydrogen or a carbon atom
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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
    • C07D211/08—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
    • C07D211/18—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 substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/20—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 substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms
    • C07D211/24—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 substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms by sulfur atoms to which a second hetero atom is attached
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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
    • C07D211/08—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
    • C07D211/18—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 substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/34—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 substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by 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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    • C07D211/06—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
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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
    • C07D211/56—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
    • 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
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    • 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
    • C07D211/60—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
    • 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
    • C07D211/68—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 one double bond between ring members or between a ring member and a non-ring member
    • C07D211/70—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 one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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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
    • C07D211/68—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 one double bond between ring members or between a ring member and a non-ring member
    • C07D211/72—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 one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D211/78—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/92—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with a hetero atom directly attached to the ring nitrogen atom
    • C07D211/96—Sulfur atom
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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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/70—Sulfur atoms
    • C07D213/71—Sulfur atoms to which a second hetero atom is attached
    • C—CHEMISTRY; METALLURGY
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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
    • C07D271/06—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
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    • 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
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur 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
    • C07D333/30—Hetero atoms other than halogen
    • C07D333/34—Sulfur atoms
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    • 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
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur 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
    • C07D333/38—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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    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
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    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
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    • C07D451/06—Oxygen atoms
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    • C07D451/14—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing 9-azabicyclo [3.3.1] nonane ring systems, e.g. granatane, 2-aza-adamantane; Cyclic acetals thereof
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/56—Ring systems containing bridged rings
    • C07C2603/58—Ring systems containing bridged rings containing three rings
    • C07C2603/70—Ring systems containing bridged rings containing three rings containing only six-membered rings
    • C07C2603/74—Adamantanes

Abstract

Un compuesto acilsulfonamidas de fórmula (1), en donde: R1 es haloalquilo C1-6, alquenilo C2-6, alquenilo C2-6 substituido por fenilo, no substituido o substituido por 1 hasta 5 sustituyentes, tienilo, piridina, benztiazolilo, cromanilo (esto es, 1,2-dihidrobenzopiranilo) o arilo C6-18, en donde los sustituyentes son seleccionados del grupo que consiste de halógeno, nitro, di-alquilamino C1-4, ciano, alquilo C1-6, haloalquilo C1-4, fenilcarbonilamino-alquilo C1-4 no sustituido, alcoxi C1-4, haloalcoxi C1-4, aminocarbonilo, di-alquilaminocarbonilo C1-4, alquilcarbonilo C1-4, alcoxicarbonilo C1-4, fenilo no sustituido, carboxilo y fenilcarbonilamino-alquilo C1-4 sustituido por fenilo o fenilo sustituido, en donde los sustituyentes fenilo son seleccionados del grupo que consiste de halógeno, nitro, di-alquilamino C1-4, ciano, alquilo C1-6, haloalquilo C1-4, alcoxi C1-4, haloalcoxi C1-4, aminocarbonilo, di-alquilaminocarbonilo C1-4, alquilcarbonilo C1-4, alcoxicarbonilo C1-4 y carboxilo, o R1 se selecciona del grupo de fórmulas (2); R2 se selecciona del grupo de fórmulas (3); R3 y R13 independientemente de cada uno son hidrógeno, hidroxi, halógeno, ciano, alquilo C1-4, alcoxi C1-4, fenilo o fenoxi, al menos uno de R4 y R5 junto con el átomo de carbono al cual están enlazados, R11 y R12 juntos con el átomo de carbono al cual están enlazados, independientemente de cada uno son un sustituido, sistema cicloalquilo de conexión, cicloalquilo C4-8, piperidina, tetrahidropiridina, o sistema heterocíclico de conexión, en donde los sustituyentes son seleccionados del grupo que consiste de alcoxicarbonilamino C1-6, alcoxicarbonil C1-6-(alquil C1-4)amino, alcoxicarbonil C1-6-(alquenil C2-4)amino, cicloalquilcarbonilamino C3-8, cicloalquilcarbonil C3-8-(alquil C1-4)amino, cicloalquilcarbonil C3-8-(alquenil C2-4)amino, alcoxicarboniloxi C1-6, fenil-alquilcarboniloxi C1-4, en donde fenilo está no sustituido o sustituido y en donde los sustituyentes son como se definió arriba por fenilo sustituido, fenilsulfonilo, en donde fenilo está no sustituido o sustituido y en donde los sustituyentes son como se definió arriba por fenilo sustituido, alquilo C4-8, por ejemplo, alquilo C5-8, hidroxialquilo C1-4, hidroxialquilo C1-4 sustituido por fenilo, en donde fenilo está no sustituido o sustituido y en donde los sustituyentes son como se definió arriba por fenilo sustituido, alcoxicarbonil C1-6-alquilo C1-4, cicloalcoxicarbonil C3-8-alquilo C1-4, alcoxicarbonilamino C1-6-alquilo C1-4, cicloalquilcarbonilamino C3-8-alquilo C1-4, fenilo o fenilo sustituido, en donde los sustituyentes son como se definió arriba por fenilo sustituido, heterociclilo que tiene 5 o 6 miembros en el anillo y 1 hasta 4 heteroátomos seleccionados de N, O, S, por ejemplo, oxadiazolilo, cicloalcoxicarbonilo C3-8, cicloalquil C3-8-alquilcarbonilo C1-4, en donde cicloalquilo está no sustituido o sustituido por hidroxi, fenilcarbonilo, en donde fenilo está no sustituido o sustituido y en donde los sustituyentes son como se definió arriba por fenilo sustituido, cicloalquilaminocarbonilo C3-8, cicloalquil C3-8-(alquil C1-4)aminocarbonilo, cicloalquil C3-8(alquenil C2-4)aminocarbonilo, y alcoxicarbonilo C1-8); R3, R8, R13 y R18 independientemente de cada uno son hidrógeno, hidroxi, halógeno, ciano, alquilo C1-4, alcoxi C1-4, fenilo o fenoxi, ya sea R8 o R18, respectivamente, independientemente de cada uno son hidrógeno, hidroxi, halógeno, ciano, alquilo C1-4, alcoxi C1-4, fenilo o fenoxi, y al menos uno de R9 y R10 junto con el átomo de carbono al cual están enlazados, R16 y R17 junto con el átomo de carbono al cual están enlazados, independientemente de cada uno tiene el significado de R4 y R5 junto con el átomo de carbono al cual están enlazados, como se definió arriba, o al menos uno de R9 y R10 juntos con el átomo de carbono al cual están enlazados, R16 y R17 juntos con el átomo de carbono al cual están enlazados, son cicloalquilo C3-8, y R8 o R18, respectivamente, independientemente de cada uno son un sustituido, sistema cicloalquilo de conexión, cicloalquilo C4-8, piperidina sustituida, tetrahidropiridina, o un sistema heterocíclico de conexión, en donde los sustituyentes son como se definió arriba para los grupos correspondientes, R6 y R15 independientemente de cada uno son haloalquilo C1-6, arilo C6-18 no sustituido o sustituido, en donde los sustituyentes arilo son como se definió arriba, o un sustituido, sistema cicloalquilo de conexión, cicloalquilo C4-8, piperidina, tetrahidropiridina, o sistema heterocíclico de conexión, en donde los sustituyentes son como se definió arriba para los grupos correspondientes o R6 y R15 independientemente de cada uno son amino sustituido por un sustituido sistema cicloalquilo de conexión, cicloalquilo C4-8, piperidina, tetrahidropiridina, o sistema heterocíclico de conexión, en donde los sustituyentes son como se definió arriba para el grupo correspondiente, R7 y R14 independientemente de cada uno son un sustituido sistema cicloalquilo de conexión, cicloalquilo C4-8, piperidina, tetrahidropiridina, o sistema heterocíclico de conexión, en donde los sustituyentes son como se definió arriba para los grupos correspondientes, o R7 y R14 independientemente de cada uno son amino sustituido por un sustituido sistema cicloalquilo de conexión, cicloalquilo C4-8, piperidina, tetrahidropiridina, o sistema heterocíclico de conexión, en donde los sustituyentes son como se definió arriba para el grupo correspondiente, m es 0, 1, 2, 3 ó 4, tal como 0 ó 1, n es 0, 1, 2, 3, ó 4, tal como 0 ó 1, y si m y/o n son diferentes a 0, entonces R1, si m es diferente a 0 y R2, n es diferente a 0, independientemente del otro tiene el significado como se define arriba, y adicionalmente puede ser piperazina sustituida, en donde los sustituyentes son como se definió arriba para piperidina sustituida; y un sistema cicloalquilo de conexión sustituido está sustituido como se definió arriba para un sistema cicloalquilo de conexión sustituido, y adicionalmente puede estar sustituido por oxo y/o alquilo C1-4; y si R1 es un sustituido sistema de anillo cicloalquilo de conexión, cicloalquilo C4-8, piperidina, tetrahidropiridina, o un sistema de anillo heterociclilo de conexión, en donde, los sustituyentes son como se definió arriba para los grupos correspondientes ,o si R1 es adicionalmente piperazina, si m es diferente a 0, entonces R2 tiene el significado como se definió arriba y adicionalmente puede ser haloalquilo C1-6, alquenilo C2-6 no sustituido, alquenilo C2-6 sustituido por fenilo, no sustituido o por 1 hasta 5 sustituyentes sustituido, tienilo, piridina, benztiazolilo, cromanilo (esta es, 1,2-dihidrobenzopiranilo) o arilo(C6-18), en donde los sustituyentes son como se definió arriba para los grupos correspondientes, y si m es 0, n es 0 y R2 es sustituido cicloalquilo C4-8 o un sistema de anillo sustituido de conexión en donde los sustituyentes son como se definieron arriba, entonces R1 es otro haloalquilo C1-6; composiciones farmacéuticas y el uso de dichos compuestos para la preparación de medicamentos para el tratamiento de padecimientos mediados por la acción de la sulfatasa esteroide.
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