AR108185A1 - Amidas terciarias y método para su uso - Google Patents

Amidas terciarias y método para su uso

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Publication number
AR108185A1
AR108185A1 ARP170100880A ARP170100880A AR108185A1 AR 108185 A1 AR108185 A1 AR 108185A1 AR P170100880 A ARP170100880 A AR P170100880A AR P170100880 A ARP170100880 A AR P170100880A AR 108185 A1 AR108185 A1 AR 108185A1
Authority
AR
Argentina
Prior art keywords
substituted
group
hydrogen
3alkoxy
3alkyl
Prior art date
Application number
ARP170100880A
Other languages
English (en)
Inventor
Wei Zhu
Qiangang Zheng
Qingwei Zhang
Lin Zhang
Ruihong Tao
Meena V Patel
Greta L Lundgaard
Mingfeng Li
Chih Lee
- Lang Qingyu Hung
Linglong Kong
Lisa A Hazelwood
Liqiang Fu
Xiangjun Deng
David A Degoey
Bruce Clapham
Da Chen
William H Bunnelle
Lawrence A Black
Original Assignee
Abbvie Inc
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 Abbvie Inc filed Critical Abbvie Inc
Publication of AR108185A1 publication Critical patent/AR108185A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/32—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
    • C07C235/34—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/64—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C233/81—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • C07C233/82—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C07C233/83—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom of an acyclic saturated carbon skeleton
    • C—CHEMISTRY; METALLURGY
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/40—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/44—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
    • C07C235/52—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
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    • 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
    • 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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    • 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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    • 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
    • C—CHEMISTRY; METALLURGY
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    • C07C313/00—Sulfinic acids; Sulfenic acids; Halides, esters or anhydrides thereof; Amides of sulfinic or sulfenic acids, i.e. compounds having singly-bound oxygen atoms of sulfinic or sulfenic groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C313/02—Sulfinic acids; Derivatives thereof
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    • C07C317/00—Sulfones; Sulfoxides
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • 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
    • C07C323/52—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 the carbon skeleton being acyclic and saturated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • 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
    • C07C323/53—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 the carbon skeleton being saturated and containing rings
    • 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
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18—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
    • C07D209/20—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 substituted additionally by nitrogen atoms, e.g. tryptophane
    • 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
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    • 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
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    • C07D213/69—Two or more oxygen atoms
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    • 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
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    • 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
    • C07D213/78—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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    • 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
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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Abstract

Compuestos y sales aceptables farmacéuticamente del mismo, útiles en el tratamiento de condiciones y trastornos que se previenen o mejoran mediante la modulación del receptor 1 de ácido lisofosfatídico. Reivindicación 1: Un compuesto caracterizado porque es de fórmula (1) o una sal aceptable farmacéuticamente del mismo, donde: G¹ se selecciona entre los compuestos del grupo de fórmulas (2); donde RG¹ᵃ se selecciona entre el grupo que consiste en hidrógeno y flúor; RG¹ᵇ y RG¹ᵈ se seleccionan en forma independiente entre el grupo que consiste en hidrogeno, C₁₋₃alcoxi, y halógeno; donde C₁₋₃alcoxi no está sustituido o está opcionalmente sustituido con uno, dos o tres átomos de flúor; RG¹ᶜ se selecciona entre el grupo que consiste en hidrógeno, C₁₋₃alcoxi, C₁₋₃alquilo, C₃₋₅cicloalquilo, halógeno, y -NO₂; donde el C₁₋₃alquilo y C₁₋₃alcoxi no están sustituidos o están opcionalmente sustituidos con un hidroxilo o uno, dos o tres átomos de flúor; donde al menos uno de RG¹ᵇ, RG¹ᶜ, y RG¹ᵈ no es hidrógeno; RG¹ᵉ y RG¹ᶠ se seleccionan en forma independiente entre el grupo que consiste en hidrógeno, C₁₋₃alcoxi, y -NHC(O)Rˣ; donde el C₁₋₃alcoxi no está sustituido o está opcionalmente sustituido con uno, dos o tres átomos de flúor; Rˣ es C₁₋₃alquilo; donde el C₁₋₃alquilo no está sustituido o está opcionalmente sustituido con uno, dos o tres átomos de flúor; RG¹ᵍ se selecciona entre el grupo que consiste en halógeno y C₁₋₃alcoxi; donde el C₁₋₃alcoxi no está sustituido o está opcionalmente sustituido con uno, dos o tres átomos de flúor; RG¹ʰ y RG¹ⁱ se seleccionan en forma independiente entre el grupo que consiste en hidrógeno, C₁₋₃alcoxi, y C₁₋₃alquilo; donde el C₁₋₃alquilo y C₁₋₃alcoxi no están sustituidos o están opcionalmente sustituidos con uno, dos o tres átomos de flúor; RG¹ʲ se selecciona entre el grupo que consiste en hidrógeno o halógeno; RG¹ᵏ y RG¹ˡ se seleccionan en forma independiente entre el grupo que consiste en hidrógeno y flúor; RG¹ᵐ, RG¹ᵒ, RG¹ᵖ, RG¹q, y RG¹ˢ se seleccionan en forma independiente en cada caso del grupo que consiste en hidrógeno y C₁₋₃alquilo; donde el C₁₋₃alquilo no está sustituido o está opcionalmente sustituido con uno, dos o tres átomos de flúor; RG¹ⁿ se selecciona entre el grupo que consiste en halógeno y C₁₋₃alcoxi; donde el C₁₋₃alcoxi no está sustituido o está opcionalmente sustituido con uno, dos o tres átomos de flúor; RG¹ʳ se selecciona en forma independiente en cada caso del grupo que consiste en hidrógeno, C₁₋₃alcoxi, C₁₋₃alquilo, C₃₋₅cicloalquilo, halógeno, y -NO₂; donde el C₁₋₃alquilo y C₁₋₃alcoxi no están sustituidos o están opcionalmente sustituidos con un hidroxilo o uno, dos o tres átomos de flúor; uno de X¹ y X² es O y el otro es CH; m es uno, dos o tres; n es uno, dos o tres; L¹ es una unión o C(R¹R²); R¹ y R² so seleccionan en forma independiente entre el grupo que consiste en hidrógeno, C₁₋₃alcoxi, y C₁₋₃alquilo; donde el C₁₋₃alquilo y C₁₋₃alcoxi no están sustituidos o están opcionalmente sustituidos con uno, dos o tres átomos de flúor; o R¹ y R² y el átomo de carbono al cual están unidos forman un C₃₋₆cicloalquileno u oxetano; donde el C₃₋₆cicloalquileno no está sustituido o está opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados entre C₁₋₃alcoxi, C₁₋₃alquilo y oxo; donde el C₁₋₃alquilo y C₁₋₃alcoxi no están sustituidos o están opcionalmente sustituidos con uno, dos o tres átomos de flúor; G² se selecciona entre el grupo que consiste en fenilo, 2-furanilo y 2-tiofenilo; donde el fenilo no está sustituido o está opcionalmente sustituido con 1, 2 ó 3 sustituyentes seleccionados en forma independiente entre C₁₋₃alcoxi, C₁₋₃alquilo, o halógeno, donde el C₁₋₃alquilo y C₁₋₃alcoxi no están sustituidos o están opcionalmente sustituidos con uno, dos o tres átomos de flúor; y donde el 2-furanilo y 2-tiofenilo no están sustituidos o están opcionalmente sustituidos con 1 ó 2 sustituyentes seleccionados en forma independiente entre halógeno o C₁₋₃alquilo, donde el C₁₋₃alquilo no está sustituido o está opcionalmente sustituido con uno, dos o tres átomos de flúor; L² es -CH₂CH₂CH₂-, donde el -CH₂CH₂CH₂- no está sustituido o está opcionalmente sustituido con C₁₋₃alquilo, donde el sustituyente -CH₂CH₂CH₂- o C₁₋₃alquilo están opcionalmente sustituidos en forma independiente entre sí con uno, dos o tres átomos de flúor, y donde el carbono central de -CH₂CH₂CH₂- puede estar unido opcionalmente con un puente de metileno a G²; G³ se selecciona entre el grupo que consiste en -CO₂H, -P(O)(OH)₂, -P(O)(OH)(OC₁₋₆alquilo), -P(O)(CH₃)(OH), -B(OH)₂, -SO₃H, -CH(OH)CF₃, -C(O)NH(OH), -C(O)NH(CN), -C(O)NHSO₂RG³ᵃ, -SO₂NHC(O)RG³ᵃ, -C(O)NHSO₂NHRG³ᵃ, -NHSO₂NHC(O)RG³ᵃ, -OC(O)NHSO₂RG³ᵃ, -SO₂NH₂, -SO₂NHRG³ᵃ, -C(O)NHS(O)(RG³ᵃ)=NC(O)RG³ᵃ, C(O)NHS(O)(RG³ᵃ)=NRG³ᵇ, o un resto del grupo de fórmulas (3); donde, RG³ᵃ es C₁₋₆alquilo, C₁₋₆haloalquilo, o GA; RG³ᵇ es hidrógeno, C₁₋₆alquilo, C₁₋₆haloalquilo, o GA; GA es cicloalquilo, cicloalquenilo, arilo, o heteroarilo, cada uno do los cuales no está sustituido o está sustituido en forma independiente con 1, 2, ó 3 grupos Rᵘ seleccionados en forma independiente; donde Rᵘ, en cada caso, es en forma independiente C₁₋₆alquilo, C₂₋₆alquenilo, C₂₋₆alquinilo, halógeno, C₁₋₆haloalquilo, -CN, oxo, -NO₂, -ORʲ, -OC(O)Rᵏ, -OC(O)N(Rʲ)₂, -S(O)₂Rʲ, -S(O)₂N(Rʲ)₂, -C(O)Rᵏ, -C(O)ORʲ, -C(OR)N(Rʲ)₂, -N(Rʲ)C(O)Rᵏ, -N(Rʲ)S(O)₂Rᵏ, -N(Rʲ)C(O)O(Rʲ)₂ o -N(Rʲ)C(O)N(Rʲ)₂; Rʲ, en cada caso, se selecciona en forma independiente entre el grupo que consiste en hidrógeno, C₁₋₆alquilo, o C₁₋₆haloalquilo; Rᵏ, en cada caso, se selecciona en forma independiente entre el grupo que consiste en C₁₋₆alquilo o C₁₋₆haloalquilo; L³ se selecciona entre el grupo que consiste en -(CH₂)₂₋₅-, -(CH₂)₁₋₄-(CR³R⁴)-, -(CH₂)-(CR⁵R⁶)₁₋₃-(CH₂)-, -(CR⁷R⁸)₁₋₄-(CH₂)-, -CH₂CH₂-X³-(CR⁹R¹⁰)₁₋₂-, -(CH₂)₁₋₂CH=CH-(CH₂)₁₋₂- y -CH₂C(O)NH(CR¹¹R¹²)-; R³ y R⁴ se seleccionan entre el grupo que consiste en hidrógeno, C₁₋₆alquilo, -(C₁₋₆alquilenil)-GB, e hidroxilo, donde uno de R³ y R⁴ no es hidrógeno; o R³ y R⁴ y el carbono al cual están unidos forman un C₃₋₆cicloalquileno; GB es arilo o heteroarilo, cada uno de los cuales no está sustituido o está sustituido en forma independiente con 1, 2, ó 3 grupos Rᵘ seleccionados en forma independiente; R⁵ se selecciona en forma independiente, en cada caso, del grupo que consiste en hidrógeno y C₁₋₆alquilo; un R⁶ es hidroxilo, y cualquier R⁶ adicional se selecciona en forma independiente, en cada caso, del grupo que consiste en hidrógeno y C₁₋₆alquilo; R⁷ y R⁸ se seleccionan en forma independiente, en cada caso, del grupo que consiste en hidrógeno y C₁₋₆alquilo; R⁹ y R¹⁰ se seleccionan en forma independiente, en cada caso, del grupo que consiste en hidrógeno y C₁₋₆alquilo; o un R⁹ y R¹⁰ y el carbono al cual están unidos forman un C₃₋₆cicloalquileno y cualesquier R⁹ y R¹⁰ adicionales se seleccionan en forma independiente, en cada caso, del grupo que consiste en hidrógeno y C₁₋₆alquilo; X³ es O, S, o S(O)₁₋₂; y R¹¹ y R¹² se seleccionan en forma independiente entre el grupo que consiste en hidrógeno, C₁₋₆alquilo, y -(C₁₋₆alquilenil)-GB; o R¹¹ y R¹² y el carbono al cual están unidos forman un C₃₋₆cicloalquileno, donde el C₃₋₆cicloalquileno no está sustituido o está opcionalmente sustituido con uno, dos o tres C₁₋₆alquilo o el C₃₋₆cicloalquileno está opcionalmente fusionado a un anillo fenilo.
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