AR070579A1 - Imidazolina -2,4- dionas sustituidas procesos para su preparacion medicamentos que comprenden estos compuestos y uso de los mismos - Google Patents

Imidazolina -2,4- dionas sustituidas procesos para su preparacion medicamentos que comprenden estos compuestos y uso de los mismos

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AR070579A1
AR070579A1 ARP090100399A ARP090100399A AR070579A1 AR 070579 A1 AR070579 A1 AR 070579A1 AR P090100399 A ARP090100399 A AR P090100399A AR P090100399 A ARP090100399 A AR P090100399A AR 070579 A1 AR070579 A1 AR 070579A1
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Argentina
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alkyl
cycloalkyl
aryl
heteroaryl
cooh
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ARP090100399A
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Sanofi Aventis
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34—Tobacco-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with 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
    • C07D233/72—Two oxygen atoms, e.g. hydantoin
    • C07D233/74—Two oxygen atoms, e.g. hydantoin with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to other ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D405/04—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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

Abstract

Los compuestos son adecuados, por ejemplo, como fármacos antiobesidad, diabetes, dependencia de nicotina, tabaco, esquizofrenia y Alzheimer. Reivindicacion 1: Un compuesto de la formula (1) en la que cada uno de R y R' es independientemente H, (CH2)n-arilo o alquilo C1-6, donde el radical alquilo C1-6 o arilo puede estar sustituido con halogeno, O-R14, S(O)m-R12 o NR13R15; o R y R' juntos forman un anillo que tiene de tres a ocho átomos de carbono, donde un átomo de carbono puede reemplazarse por O, S(O)m, N-(CH2)n-CO-NH-arilo, NR13 o NR15; m es 0, 1 o 2; n es 0, 1, 2, 3 o 4; p es 1, 2, 3, 4 o 5; q es 1, 2, 3 o 4; r es 2, 3, 4, 5 o 6; v es 0, 1, 2, 3 o 4; cada uno de A, D, E, G y L es independientemente C o N, donde no hay ningun sustituyente R1, R2, R3, R4, R5 correspondiente cuando se definen como N; o R2-D=E-R3, o R4-G=L-R5 se definen como S u O y donde el anillo de cinco miembros o de seis miembros puede estar condensado con -(CH2)3- o -(CH2)4- o -CH=CH-CH=CH- para formar un sistema bicíclico; cada uno de R1, R2, R3, R4 y R5 es independientemente H, F, CI, Br, I, CN, N3, NC, NO2, CF3, alquilo C1-8, cicloalquilo C3-8, (CH2)q-cicloalquilo C3-8, (CH2)n-cicloaIquenilo C3-8, (CH2)n-bicicloalquilo C7-12, (CH2)n-bicicloalquenilo C7-12, (CH2)n-tricicloalquilo C7-12, adamantan-1-ilo, adamantan-2-ilo, (CH2)n-arilo, (CH2)n-heteroarilo, OCF3, O-R11, NR13R15, NH-CN, S(O)m-R12, SO2-NH2, SO2-N=CH-N(CH3)2, SO2-NH-CO-R12, SO2-NH-CO-NHR12, SO2-NH-CO-R16, SO2-NH-alquilo C1-8, SO2-NH-cicloalquilo C3-8, SO2-NH-(CH2)r-OH, SO2-NH-(CH2)n-arilo, SO2-NH-(CH2)n-heteroarilo, SO2-N[alquilo C1-8]2, SO2-R16, SF5, CO-O[alquilo C1-8], CO-O[cicloalquilo C3-8], CO-O-(CH2)r-NH2, CO-O-(CH2)n-arilo, CO-O-(CH2)n-heteroarilo, CO-NH2, CO-NH-CN, CO-NH-[alquilo C1-8], CO-NH-(CH2)r-OH, CO-N[alquilo C1-8]2, CO-NH-[cicloalquilo C3-8], CO-N[cicloalquilo C3-8]2, C(=NH)-O-[alquilo C1-6], C(=NH)-NH2, C(=NH)-NR12R13, C(=NH)-R16, C(=NR13)-NR12R13, (CH2)n-C(=NSO2-R12)NH2, CO-NH-SO2-R16, CO-NH-SO2-NHR12, CO-R16, COOH, CO-alquilo C1-8, CO-cicloalquilo C3-8, CO-(CH2)n-[bicicloalquilo C7-12], CO-(CH2)n-[tricicloalquilo C7-12], CO-arilo, CO-heteroarilo, CH(OH)-arilo, CH(OH)-heteroarilo, CH[O-alquil C1-6]-arilo, CH[O-alquil C1-6]-heteroarilo, CHF-arilo, CHF-heteroarilo, CF2-arilo, CF2-heteroarilo, CHO, CH2-OH, CH2-CN, CH2-O-R12, CH2-O-(CH2)n-CO-O[alquilo C1-8], CH2-O-(CH2)n-CO-NH2 o CH2-O-(CH2)q-COOH, donde los radicales alquilo, cicloalquilo, cicloalquenilo, bicicloalquilo, bicicloalquenilo y tricicloalquilo pueden estar sustituidos con átomos de fluor y donde los radicales arilo o heteroarilo pueden estar sustituidos con halogeno, CN, alquilo C1-6, cicloalquilo C3-6, O-alquilo C1-6, (CH2)-arilo, O-(CH2)n-arilo, S(O)m-alquilo C1-6, SO2-NH2, COOH, CONH2, CO-O-alquilo C1-6 o CO-alquilo C1-6 y donde los radicales alquilo pueden estar sustituidos con átomos de fluor; cada uno de R6, R7, R8, R9 y R10 es independientemente C(Q1)(Q2)-heterociclo bicíclico, C(Q1)(Q2)-arilo o C(Q1)(Q2)-heteroarilo, donde el radical arilo o heteroarilo puede estar condensado con un anillo de carbono aromático o no aromático de 5 o 6 miembros en el que uno o más grupos CH o CH2 pueden reemplazarse por átomos de oxígeno y donde el anillo de carbono aromático o no aromático de 5 o 6 miembros puede estar sustituido con F, =O o alquilo C1-6 y donde el heterociclo bicíclico puede contener de 9 a 12 miembros de anillo y cada uno de hasta cinco grupos CH o CH2 puede reemplazarse independientemente por N, NR20, O, S(O)m o C=O y donde el radical C(Q1)(Q2)-arilo, C(Q1)(Q2)-heteroarilo o C(Q1)(Q2)-heterociclo bicíclico puede estar sin sustituir o mono o polisustituido con R11, F, Cl, Br, I, CN, N3, NC, NO2, CF3, (CH2)n-O-R11, (CH2)n-O-(CH2)r-OH, (CH2)n-O-CH(CH2OH)2, (CH2)n-O-(CH2)n-CO-O-(CH2)r-NH2, (CH2)n-O-(CH2)n-CO-NH-(CH2)r-OH, OR13, OCF3, (CH2)n-O-(CH2)r-NH2, (CH2)n-NH-R11, (CH2)n-N[(CH2)q-CO-O-alquilo C1-6]2, (CH2)n-N[(CH2)q-COOH]2, (CH2)n-N[(CH2)q-CONH2]2, (CH2)n-NH-R13, (CH2)n-N(R13)2, (CH2)n-NH-CN, (CH2)n-NH-SO2-R16, (CH2)n-NH-(CH2)n-SO2-R12, (CH2)n-NR12-CO-R16, (CH2)n-NR12-CO-NR12R13, (CH2)n-NR12-CO-N(R12)2, (CH2)n-NR12-CO-NHR11, (CH2)n-NH-C(=NH)-NH2, (CH2)n-NH-C(=NH)-R16, (CH2)n-NH-C(=NH)-NHR12, (CH2)n-NR12-C(=NR13)-NHR12, (CH2)n-NR12-C(=NR12)-NR12R13, (CH2)n-NH-(CH2)n-CO-O-(CH2)r-NH2, (CH2)n-NH-(CH2)n-CO-NH-[alquilo C1-8], (CH2)n-NH-(CH2)n-CO-NH-(CH2)r-OH, (CH2)n-NH-(CH2)n-CO-N[alquilo C1-6]2, (CH2)n-NH-(CH2)n-CO-NH-[cicloalquilo C3-8], (CH2)n-NH-(CH2)n-CO-N[cicloalquilo C3-8]2, (CH2)n-NH-C(CH3)2-CO-O-alquilo C1-8, (CH2)n-NH-C(CH3)2-CO-O-cicloalquilo C3-8, (CH2)n-NH-C(CH3)2-CO-O-(CH2)r-NH2, (CH2)n-NH-C(CH3)2-CO-O-(CH2)n-arilo, (CH2)n-NH-C(CH3)2-CO-O-(CH2)n-heteroarilo, (CH2)n-NH-C(CH3)2-CO-NH2, (CH2)n-NH-C(CH3)2-CO-NH-[alquilo C1-8], (CH2)n-NH-C(CH3)2-CO-NH-(CH2)r-OH, (CH2)n-NH-C(CH3)2-CO-N[alquilo C1-8]2, (CH2)n-NH-(CH3)2-CO-NH-[cicloalquilo C3-8], (CH2)n-NH-C(CH3)2-CO-N[cicloalquilo C3-8]2, (CH2)n-NH-C(CH3)2-COOH, S(O)mR12, SO2-R16, SO2-N=CH-N(CH3)2, un resto de formula (2), SO2-NH-CO-R12, SO2-NHR12, SO2-NH(CH2)r-OH, SO2-N[alquilo C1-8]2, SO2-NH-(CH2)r-NH2, SF5, COOH, CO-NH2, (CH2)q-CN, (CH2)n-CO-NH-CN, (CH2)n-CO-NH-piperidin-1-ilo, (CH2)n-CO-NH-SO2-NHR12, (CH2)n-CO-NH-SO2-R18, (CH2)n-CHO, (CH2)n-C(=NH)-NH2, (CH2)n-C(=NH)-NHOH, (CH2)n-C(=NH)[NH-O-alquilo C1-6], (CH2)n-C(=NH)(R16), (CH2)n-C(=NR13)NHR12, (CH2)n-C(=NR12)NR12R13, (CH2)n-C(=NSO2-R12)NH2 o (CH2)n-C(=NH)O[alquilo C1-6], donde los radicales alquilo y cicloalquilo pueden estar sustituidos con átomos de fluor y donde los radicales arilo o heteroarilo pueden estar sustituidos con halogeno, CN, alquilo C1-6, cicloalquilo C3-6, O-alquilo C1-6, S(O)m-alquilo C1-6, SO2-NH2, COOH, CONH2, CO-O-alquilo C1-6 o CO-alquilo C1-6 y donde los radicales alquilo pueden estar sustituidos con átomos de fluor; H, F, CI, Br, I, CN, N3, NC, NO2, CF3, alquilo C1-8, alquenilo C2-10, alquinilo C2-10, cicloalquilo C3-8, arilo, heteroarilo, (CH2)n-CO-[O-alquilo C1-8], (CH2)n-CO-[O-cicloalquilo C3-8], (CH2)n-CO-[alquilo C1-8], (CH2)n-CO-[cicloalquilo C3-8], (CH2)n-CO-[O-(CH2)v-arilo], (CH2)n-CO-NH2, (CH2)n-COOH, (CH2)n-CO-NH-CN, (CH2)n-P(O)(OH)[O-alquilo C1-6], (CH2)n-P(O)[O-alquilo C1-6]2, (CH2)n-P(O)(OH)(O-CH2-arilo), (CH2)n-P(O)(O-CH2-arilo)2, (CH2)n-P(O)(OH)2, (CH2)n-SO3H, (CH2)n-SO2-NH2, (CH2)n-CO-NH-[alquilo C1-8], (CH2)n-CO-N[alquilo C1-8]2, (CH2)n-CO-NH-[cicloalquilo C3-8], alquenil C2-10-CO-O[alquilo C1-6], alquenil C2-10-CONH2, alquenil C2-10-COOH, alquinil C2-10-CO-O[alquilo C1-6], alquinil C2-10-CONH2, alquinil C2-10-COOH, (CH2)n-CO-R16, (CH2)n-OH, (CH2)n-O-alquilo C1-8, (CH2)n-O-alquenilo C2-10, (CH2)n-O-alquinilo C2-10, (CH2)n-O-cicloalquilo C3-8, (CH2)n-O-(CH2)q-[cicloalquilo C3-8], (CH2)n-O-(CH2)n-CO-[O-alquilo C1-8], (CH2)n-O-(CH2)n-CO-[O-cicloalquilo C3-8], (CH2)n-O-(CH2)n-CO-[alquilo C1-8], (CH2)n-O-(CH2)n-CO-[cicloalquilo C3-8], (CH2)n-O-(CH2)n-CO-[O-(CH2)v-arilo], (CH2)n-O-(CH2)n-CO-[O-(CH2)v-heteroarilo], (CH2)n-O-(CH2)q-CO-NH2, (CH2)n-O-(CH2)q-COOH, (CH2)n-O-(CH2)q-CO-NH-CN, (CH2)n-O-(CH2)n-P(O)(OH)[O-alquilo C1-6], (CH2)n-O-(CH2)n-P(O)[O-alquilo C1-6]2, (CH2)n-O-(CH2)n-P(O)(OH)(O-CH2-arilo), (CH2)n-O-(CH2)n-P(O)(O-CH2-arilo)2, (CH2)n-O-(CH2)n-P(O)(OH)2, (CH2)n-O-(CH2)n-SO3H, (CH2)n-O-(CH2)n-SO2-NH2, (CH2)n-O-(CH2)n-CO-NH-[alquilo C1-8], (CH2)n-O-(CH2)n-CO-N[alquilo C1-8]2, (CH2)n-O-(CH2)n-CO-NH-[cicloalquilo C3-8], (CH2)n-O-(CH2)n-CR21R22-CO-O[alquilo C1-6], (CH2)n-O-(CH2)n-CR21R22-CONH2, (CH2)n-O-(CH2)n-CR21R22-COOH, (CH2)n-O-(CH2)n-CO-R16, (CH2)n-O-(CH2)r-OH, (CH2)n-O-CH(CH2OH)2, (CH2)n-O-(CH2)n-CO-O-(CH2)r-NH2, (CH2)n-O(CH2)n-CO-NH-(CH2)r-OH, O-R13, OCF3, (CH2)n-NH2, (CH2)n-NH-alquilo C1-8, (CH2)n-NH-cicloalquilo C3-8, (CH2)n-NH-(CH2)n-CO-[O-cicloalquilo C3-8], (CH2)n-NH-(CH2)n-CO-[alquilo C1-8], (CH2)n-NH-(CH2)n-CO-[cicloalquilo C3-8], (CH2)n-NH-(CH2)n-CO-[O-(CH2)v-arilo], (CH2)n-NH-(CH2)n-CO-[O-(CH2)v-heteroarilo], (CH2)n-NH-(CH2)q-CO-NH-CN, (CH2)n-NH-(CH2)n-P(O)(OH)2, (CH2)n-NH-(CH2)n-SO3H, (CH2)n-NH-(CH2)n-SO2-NH2, (CH2)n-NH-(CH2)-CR21R22-CO-O[alquilo C1-6], (CH2)n-NH-(CH2)n-CR21R22-CONH2, (CH2)n-NH-(CH2)n-CR21R22-COOH, (CH2)n-NH-(CH2)n-CO-R16, (CH2)n-NH-(CH2)n-SO2-[alquilo C1-8], (CH2)n-NH-(CH2)n-SO2-[cicloalquilo C3-8], (CH2)n-NH-SO2-(CH2)n-NH2, (CH2)n-NH-SO2-(CH2)n-NH-alquilo C1-8, (CH2)n-NH-SO2-(CH2)n-NH-cicloalquilo C3-8, (CH2)n-NH-SO2-(CH2)n-N[alquilo C1-8]2, (CH2)n-NH-CN, (CH2)n-NH-SO2-R16, (CH2)n-NR12-CO-NH-alquilo C1-8, (CH2)n-NR12-CO-NH-cicloalquilo C3-8, (CH2)n-NR12-CO-NH2, (CH2)n-NR12-CO-NH-SO2-alquilo C1-8, (CH2)n-NR12-CO-NH-SO2-cicloalquilo C3-8, (CH2)-NR12-CO-N[alquilo C1-8]2, (CH2)n-NH-CO-NH-(CH2)n-CO-[O-alquilo C1-8], (CH2)n-NH-CO-NH(CH2)q-CO-NH2, (CH2)n-NH-CO-NH-(CH2)q-COOH, (CH2)n-NH-C(=NH)-NH2, (CH2)n-NH-C(=NH)-R16, (CH2)n-NH-C(=NH)-NH[alquilo C1-8], (CH2)n-NH-C(=N-SO2-alquil C1-8)-NH2, (CH2)n-NH-C(=N-SO2-alquil C1-8)-NH[alquilo C1-8], (CH2)n-NH-C(=N-SO2-NH2)-NH2, (CH2)n-NH-C(=N-SO2-NH2)-NH[alquilo C1-8], (CH2)n-NH-C(=NH)-N[alquilo C1-8]2, (CH2)n-NH-C(=N-SO2-alquil C1-8)-N[alquilo C1-8]2, (CH2)n-NH-(CH2)n-CO-O-(CH2)r-NH2, (CH2)n-NH-(CH2)n-CO-NH-[alquilo C1-8], (CH2)n-NH-(CH2)n-CO-NH-(CH2)r-OH, (CH2)n-NH-(CH2)n-CO-N[alquilo C1-8]2, (CH2)n-NH-(CH2)n-CO-NH-[cicloalquilo C3-8] (CH2)n-NH-C(CH3)2-CO-O-cicloalquilo C3-8, (CH2)n-NH-C(CH3)2-CO-O-(CH2)r-NH2, (CH2)n-NH-C(CH3)2-CO-O-(CH2)n-arilo, (CH2)n-NH-C(CH3)2-CO-O-(CH2)n-heteroarilo, (CH2)n-NH-C(CH3)2-CO-NH-[alquilo C1-8], (CH2)n-NH-C(CH3)2-CO-NH-(CH2)r-OH, (CH2)n-NH-C(CH3)2-CO-N[alquilo C1-8]2, (CH2)n-NH-(CH3)2-CO-NH-[cicloalquilo C3-8], (CH2)n-NH-C(CH3)2-CO-N[cicloalquilo C3-8]2, (CH2)n-S(O)m-alquilo C1-8, (CH2)n-S(O)m-cicloalquilo C3-8, (CH2)n-SO2-R16, SO2-N=CH-N(CH3)2, el resto de formula (2), (CH2)n-SO2-NH-CO-alquilo C1-8, (CH2)n-SO2-NH-CO-cicloalquilo C3-8, (CH2)n-SO2-NH-alquilo C1-8, (CH2)n-SO2-NH-cicloalquilo C3-8, (CH2)n-SO2-N[alquilo C1-8]2, SO2-NH(CH2)r-OH, SO2-NH-(CH2)r-NH2, SF5, (CH2)q-CN, (CH2)n-CO-NH-piperidin-1-ilo, (CH2)n-CO-NH-SO2-NHR12, (CH2)n-CO-NH-SO2-alquilo C1-8, (CH2)n-CO-NH-SO2-cicloalquilo C3-8, (CH2)n-CHO, (CH2)n-C(=NH)NH2, (CH2)n-C(=NH)
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