AR080558A1 - ANTIMICROBIAL COMPOUNDS AND METHODS FOR PREPARATION AND USE - Google Patents

ANTIMICROBIAL COMPOUNDS AND METHODS FOR PREPARATION AND USE

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Publication number
AR080558A1
AR080558A1 ARP100103804A ARP100103804A AR080558A1 AR 080558 A1 AR080558 A1 AR 080558A1 AR P100103804 A ARP100103804 A AR P100103804A AR P100103804 A ARP100103804 A AR P100103804A AR 080558 A1 AR080558 A1 AR 080558A1
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Argentina
Prior art keywords
cr6r6
alkyl
unsaturated
group
aromatic
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ARP100103804A
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Spanish (es)
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Ashoke Bahattacharjee
Erin M Duffy
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Rib X Pharmaceuticals Inc
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Publication of AR080558A1 publication Critical patent/AR080558A1/en

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    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
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    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61B—DIAGNOSIS; SURGERY; IDENTIFICATION
    • A61B5/00—Measuring for diagnostic purposes; Identification of persons
    • A61B5/68—Arrangements of detecting, measuring or recording means, e.g. sensors, in relation to patient
    • A61B5/6846—Arrangements of detecting, measuring or recording means, e.g. sensors, in relation to patient specially adapted to be brought in contact with an internal body part, i.e. invasive
    • A61B5/6847—Arrangements of detecting, measuring or recording means, e.g. sensors, in relation to patient specially adapted to be brought in contact with an internal body part, i.e. invasive mounted on an invasive device
    • A61B5/6862—Stents
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
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    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0043—Nose
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    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0046—Ear
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    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0048—Eye, e.g. artificial tears
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    • C07D239/06—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D239/08—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms directly attached in position 2
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    • C07D239/20—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D239/22—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to ring carbon atoms
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    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/34—One oxygen atom
    • C07D239/36—One oxygen atom as doubly bound oxygen atom or as unsubstituted hydroxy radical
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    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
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    • C07D251/12—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D251/14—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom
    • C07D251/16—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to only one ring carbon atom
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    • C07D251/12—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D251/26—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hetero atoms directly attached to ring carbon atoms
    • C07D251/40—Nitrogen atoms
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    • 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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    • C07D401/12—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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    • 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
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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Materials For Medical Uses (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Reivindicacion 1: Un compuesto que tiene la formula (1), (2), (3) o (4) donde -G-H-J, alternativamente, se selecciona del resto de formula (5), donde cada H y J se selecciona de manera independiente, o -G-H-J se selecciona del resto de formula (6), donde Rx se selecciona de CH2, NH, N(alquilo C1-8), S, u O; Ry y Rz son C o CH, donde cada uno está sustituido en forma independiente con uno o más F, CH3, CF3, OH y OCH3; o Rx, Ry y Rz se seleccionan de modo independiente de CH2 o CRaRb donde Ra y Rb se toman juntos para formar un carbociclo C1-5; J se selecciona de NH2, NH(alquilo C1-8), N(alquilo C1-8)2, NHC(=O)CH3, NHC(=O)NH2, NHC(=NH)NH2, NHC(=NH)H; donde n es 0; 1 o 2; alternativamente, -G-H-J se selecciona del resto de formula (7) donde Rx se selecciona de CH2, NH, N(alquilo C1-8), S u O; Rz es un C o CH, sustituido con uno o más CH3, o Rz es CRaRb donde Ra y Rb se toman juntos para formar un carbociclo C1-5; donde m es 1; 2 o 3; J se selecciona de NH2, NH(alquilo C1-8), N(alquilo C1-8)2, NHC(=O)CH3, NHC(=O)NH2, NHC(=NH)NH2, NHC(=NH)H; C-B-A-, -D-E-F y -G-H-J son restos químicos, donde: A, D y G se seleccionan de manera independiente del grupo que consiste en: (a) un enlace simple, (b) -(alquilo C1-8)-, (c) -(alquenilo C2-8)-, (d) -(alquinilo C2-8)-, donde: i) 0 - 4 átomos de carbono en cualquiera de (b) - (d) inmediatamente anteriores están opcionalmente reemplazados por un resto seleccionado del grupo que consiste en -O-, -S(O)p-, -NR6-, -(C=O)-, -S(O)pNR6-, -NR6S(O)p- y -NR6S(O)pNR6-; ii) cualquiera de (b) - (d) inmediatamente anteriores está opcionalmente sustituido con uno o más grupos R5; y iii) cualquiera de (b) - (d) inmediatamente anteriores está opcionalmente sustituido con grupos -(alquilo C1-8)-R5; (e) -O-, (f) -NR6-, (g) -S(O)p-, (h) -C(O)-, (i) -C(O)O-, j) -OC(O)-, k) -OC(O)O-, (l) -C(O)NR6-, (m) -NR6CO-, (n) -NR6C(O)NR6-, (o) -C(=NR6)-, (p) -C(=NR6)O-, (q) -OC(=NR6)-, (r) -C(=NR6)NR6-, (s) -NR6C(=NR6)-, (t) -C(=S)-, (u) -C(=S)NR6-, (v) -NR6C(=S)-, (w) -C(O)S-, (x) -SC(O)-, (y) -OC(=S)-, (z) -C(=S)O-, (aa) -NR6(CNR6)NR6-, (bb) -CR6R6C(O)-, (cc) -C(O)NR6(CR6R6)t -, (dd) un heterociclo de 3 - 14 miembros saturado, insaturado, o aromático que contiene uno o más heteroátomos seleccionados del grupo que consiste en nitrogeno, oxígeno y azufre; (ee) un carbociclo de 3 - 14 miembros saturado, insaturado o aromático; y (ff) -(CR6R6)t-; donde (dd) o (ee) está opcionalmente sustituido con uno o más grupos R5; B, E y H se seleccionan de manera independiente del grupo que consiste en: (a) un enlace simple; (b) un heterociclo de 3 - 14 miembros saturado, insaturado o aromático, que contiene uno o más heteroátomos seleccionados del grupo que consiste en nitrogeno, oxígeno y azufre; (c) un carbociclo de 3 - 14 miembros saturado, insaturado o aromático; donde (b) o (c) está opcionalmente sustituido con uno o más grupos R5; (d) -(alquilo C1-8)-, (e) -(alquenilo C2-8)-, (f) -(alquinilo C2-8)-, donde: i) 0 - 4 átomos de carbono en cualquiera de (d) - (f) inmediatamente anteriores están opcionalmente reemplazados por un resto seleccionado del grupo que consiste en -O-, -S(O)p-, -NR6-, -(C=O)-, -C(=NR6)-, -S(O)pNR6-, -NR6S(O)p- y -NR6S(O)pNR6-; ii) cualquiera de (d) - (f) inmediatamente anteriores está opcionalmente sustituido con uno o más grupos R5; y iii) cualquiera de (d) - (f) inmediatamente anteriores está opcionalmente sustituido con grupos -(alquilo C1-8)-R5; y (g) -(CR6R6)t-; C, F y J se seleccionan de manera independiente del grupo que consiste en: (a) hidrogeno, (c) F, (d) Cl, (e) Br, (f) I, (g) -CF3, (h) -CN, (i) -N3, (j) -NO2, (k) -NR6(CR6R6)tR8, (l) -OR8, (m) -S(O)p(CR6R6)tR8, (n) -C(O)(CR6R6)tR8, (o) -OC(O)(CR6R6)tR8, (p) -SC(O)(CR6R6)tR8, (q) -C(O)O(CR6R6)tR8, (r) -NR6C(O)(CR6R6)tR8, (s) -C(O)NR6(CR6R6)tR8, (t) -C(=NR6)(CR6R6)tR8, (u) -C(=NNR6R6)(CR6R6)tR8, (v) -C(=NNR6C(O)R6)(CR6R6)tR8, (w) -C(=NOR8)(CR6R6)tR8, (x) -NR6C(O)O(CR6R6)tR8, (y) -OC(O)NR6(CR6R6)tR8, (z) -NR6C(O)NR6(CR6R6)tR8, (aa) -NR6S(O)p(CR6R6)tR8, (bb) -S(O)pNR6(CR6R6)tR8, (cc) -NR6S(O)pNR6(CR6R6)tR8, (dd) -NR6R8, (ee) -NR6(CR6R6)R8, (ff) -OH, (gg) -NR8R8, (hh) -OCH3, (ii) -S(O)pR8, (jj) -NC(O)R8, (kk) -NR6C(NR6)NR6R8, (II) un grupo alquilo C1-8, (mm) un grupo alquenilo C2-8, (nn) un grupo alquinilo C2-8, (oo) un heterociclo de 3 - 14 miembros saturado, insaturado o aromático que contiene uno o más heteroátomos seleccionados del grupo que consiste en nitrogeno, oxígeno y azufre, (pp) un carbociclo de 3 - 14 miembros saturado, insaturado, o aromático, (qq) -(CR6R6)tNR6(CR6R6)tR8, (rr) -N[(CR6R6)tR8][C=O(CR6R6)tR8], (ss) -(CR6R6)tN[(CR6R6)tR8][(CR6R6)tR8], (tt) -(CR6R6)tNR6(C=O)(CR6R6)tR8, (uu) -haloalquilo, (vv) -C(O)(CR6)[(CR6R6)tR8]R8, (ww) -(CR6R6)tC(O)NR8R8, (xx) -(CR6R6)tC(O)O(CR6R6)tR8, (yy) -NR6C(O)CR8R8R8, (zz) -N[(CR6R6)tR8]C(O)R8 y (aaa) -S(O)pNR8R8; donde (II) a (pp) están opcionalmente sustituidos con uno o más grupos R7; R5 se selecciona de (a) hidrogeno, (b) F, (e) Cl, (d) Br, (e) I, (f) -CF3, (g) -CN, (h) -N3 (i) -NO2, (j) -NR6R6, (k) -OR8, (l) -NR6(CNR6)NR6R6, (m) alquilo -C1-8, (n) alquenilo -C1-8, (o) alquinilo -C1-8, (p) -(alquilo C1-8)-(heterociclo de 3 - 14 miembros saturado, insaturado, o aromático, que contiene uno o más heteroátomos seleccionados del grupo que consiste en nitrogeno, oxígeno y azufre), (q) -(alquilo C1-8)-(carbociclo de 3 - 14 miembros saturado, insaturado, o aromático), (r) -haloalquilo, (s) -SR6, (t) -heterociclo de 3 - 14 miembros saturado, insaturado, o aromático que contiene uno o más heteroátomos seleccionados del grupo que consiste en nitrogeno, oxígeno y azufre, y (u) -carbociclo de 3 - 14 miembros saturado, insaturado, o aromático; alternativamente, dos grupos R5 se toman juntos para formar un carbociclo; donde (m) a (r) y (t) a (u) están opcionalmente sustituidos con uno o más R8; R6 se selecciona de (a) hidrogeno, (b) -alquilo C1-8, o alternativamente, dos grupos R6 se toman juntos para formar un carbociclo, (c) -haloalquilo, (d) -heterociclo de 3 - 14 miembros saturado, insaturado, o aromático que contiene uno o más heteroátomos seleccionados del grupo que consiste en nitrogeno, oxígeno y azufre; y (e) -carbociclo de 3 - 14 miembros saturado, insaturado, o aromático; donde (b) a (e) están opcionalmente sustituidos con uno o más R8; R7 se selecciona de (a) hidrogeno, (b) F, (c) Cl, (d) Br, (e) I, (f) -CF3, (g) -CN, (h) -N3, (i) -NO2, (j) -NR6R6, (k) -OR6, (l) -NR6(CNR)NR6R6, (m) -alquilo C1-8, (n) -alquenilo C1-8, (o) -alquinilo C1-8, (p) -(alquilo C1-8)-(heterociclo de 3 - 14 miembros saturado, insaturado, o aromático que contiene uno o más heteroátomos seleccionados del grupo que consiste en nitrogeno, oxígeno y azufre), (q) -(alquilo C1-8)-(carbociclo de 3 - 14 miembros saturado, insaturado, o aromático), (r) -haloalquilo, (s) -NR6R8, (t) -OR8, (u) -(CR6R6)tNR6R8, (v) -CR6R8R8, (w) -SR6, (x) -heterociclo de 3 - 14 miembros saturado, insaturado, o aromático, que contiene uno o más heteroátomos seleccionados del grupo que consiste en nitrogeno, oxígeno y azufre, (y) -carbociclo de 3 - 14 miembros saturado, insaturado o aromático, (z) -(CR6R6)tC(O)NR8R8, (aa) -S(O)pR8, (bb) -NR6C(O)NR6R6, (cc) -NR6C(O)R6 y (dd) -C(=NR6)NR6R6; donde (m) a (q) y (x) a (y) están opcionalmente sustituidos con uno o más R9; R8 se selecciona de (a) hidrogeno, (b) F, (c) Cl, (d) Br, (e) I, (f) -CF3, (g) -CN, (h) -N3, (i) -NO2, (j) -NR6R9, (k) -OR9, (l) -NR6(CNR6)NR6R6, (m) -alquilo C1-8, (n) -alquenilo C1-8, (o) -alquinilo C1-8, (p) -(alquilo C1-8)-(heterociclo de 3 - 14 miembros saturado, insaturado o aromático que contiene uno o más heteroátomos seleccionados del grupo que consiste en nitrogeno, oxígeno y azufre), (q) -(alquilo C1-8)-(carbociclo de 3 - 14 miembros saturado, insaturado o aromático), (r) -heterociclo de 3 - 14 miembros saturado, insaturado, o aromático que contiene uno o más heteroátomos seleccionados del grupo que consiste en nitrogeno, oxígeno y azufre, (s) -carbociclo de 3 - 14 miembros saturado, insaturado o aromático, (t) -haloalquilo, (u) -C(O)(CR6R6)tR9, (v) -SR6, (w) -OC(O)(CR6R6)tR9, (x) -NR6C(O)NR6R9, (y) -NR6C(O)R9, (z) -NR6(CNR9)(NR6R6), (aa) -ONR6(CNR6)NR6R6, (bb) -C(=NR9)NR6R6, (cc) -S(O)pR9, (dd) -(CR6R6)tC(O)NR6R9, (ee) -(CR6R6)tOR9 y (ff) -(CR6R6)tNR6R9; donde (m) a (s) están opcionalmente sustituidos con uno o más R9; R9 se selecciona de (a) hidrogeno, (b) F, (c) Cl, (d) Br, (e) I, (f) -CF3, (g) -CN, (h) -N3, (i) -NO2, (j) -NR6R10, (k) -OR6, (l) -NR6(CNR6)NR6R6, (m) -C(O)(CR6R6)tNR6R6, (n) -alquilo C1-8, (o) -alquenilo C1-4, (p) alquinilo C1-8, (q) -heterociclo de 3 - 14 miembros saturado, insaturado o aromático que contiene uno o más heteroátomos seleccionados del grupo que consiste en nitrogeno, oxígeno y azufre, (r) -carbociclo de 3 - 14 miembros saturado, insaturado o aromático, (s) -haloalquilo, (t) -(CR6R6)tOR6, (u) -O(CR6R6)tNR6R10, (v) -C(O)R6, (w) -SR6, (x) -C(O)OR10, (y) -S(O)pR6, (z) -(alquilo C1-8)-(heterociclo de 3 - 14 miembros saturado, insaturado o aromático que contiene uno o más heteroátomos seleccionados del grupo que consiste en nitrogeno, oxígeno y azufre), (aa)-(alquilo C1-8)-(carbociclo de 3 - 14 miembros saturado, insaturado o aromático), (bb) -O(CR6R6)tOR6, (cc) -C(=NR6)NR6R6, (dd) -ONR6R6, (ee) -NR6C(O)NR6R6, (ff) -O(CR6R6)tOR6, (gg) -NR6C(O)R6 y (hh) -(CR6R6)tNR6R10; donde (n) a (r) y (z) a (aa) están opcionalmente sustituidos con uno o más R10; R10 se selecciona de (a) hidrogeno, (b) F, (c) Cl, (d) Br, (e) I, (f) -CF3, (g) -CN, (h) -N3, (i) -NO2, (j) -NR6R6, (k) -OR6, (l) -NR6(CNR6)NR6R6, (m) -C(O)(CR6R6)tNR6R6, (n) -alquilo C1-8, (o) -alquenilo C1-8, (p) -alquinilo C1-8, (q) -heterociclo de 3 - 14 miembros saturado, insaturado o aromático que contiene uno o más heteroátomos seleccionados del grupo que consiste en nitrogeno, oxígeno y azufre, (r) -carbociclo de 3 - 14 miembros saturado, insaturado o aromático, (s) -haloalquilo, (t) -(CR6R6)tOR6, (u) -O(CR6R6)tNR6R6, (v) -C(O)R6, (w) -SR6, (x) -C(O)OR6, (y) -S(O)pR6, (z) -(alquilo C1-8)-(heterocicClaim 1: A compound having the formula (1), (2), (3) or (4) wherein -GHJ, alternatively, is selected from the rest of formula (5), where each H and J is independently selected , or -GHJ is selected from the rest of formula (6), where Rx is selected from CH2, NH, N (C1-8 alkyl), S, or O; Ry and Rz are C or CH, where each is independently substituted with one or more F, CH3, CF3, OH and OCH3; or Rx, Ry and Rz are independently selected from CH2 or CRaRb where Ra and Rb are taken together to form a C1-5 carbocycle; J is selected from NH2, NH (C1-8 alkyl), N (C1-8 alkyl) 2, NHC (= O) CH3, NHC (= O) NH2, NHC (= NH) NH2, NHC (= NH) H ; where n is 0; 1 or 2; alternatively, -G-H-J is selected from the rest of formula (7) where Rx is selected from CH2, NH, N (C1-8 alkyl), S or O; Rz is a C or CH, substituted with one or more CH3, or Rz is CRaRb where Ra and Rb are taken together to form a C1-5 carbocycle; where m is 1; 2 or 3; J is selected from NH2, NH (C1-8 alkyl), N (C1-8 alkyl) 2, NHC (= O) CH3, NHC (= O) NH2, NHC (= NH) NH2, NHC (= NH) H ; CBA-, -DEF and -GHJ are chemical residues, where: A, D and G are independently selected from the group consisting of: (a) a single bond, (b) - (C1-8 alkyl) -, ( c) - (C2-8 alkenyl) -, (d) - (C2-8 alkynyl), where: i) 0-4 carbon atoms in any of (b) - (d) immediately above are optionally replaced by a remainder selected from the group consisting of -O-, -S (O) p-, -NR6-, - (C = O) -, -S (O) pNR6-, -NR6S (O) p- and -NR6S ( O) pNR6-; ii) any of (b) - (d) immediately above is optionally substituted with one or more R5 groups; and iii) any of (b) - (d) immediately above is optionally substituted with groups - (C1-8 alkyl) -R5; (e) -O-, (f) -NR6-, (g) -S (O) p-, (h) -C (O) -, (i) -C (O) O-, j) -OC (O) -, k) -OC (O) O-, (l) -C (O) NR6-, (m) -NR6CO-, (n) -NR6C (O) NR6-, (o) -C ( = NR6) -, (p) -C (= NR6) O-, (q) -OC (= NR6) -, (r) -C (= NR6) NR6-, (s) -NR6C (= NR6) - , (t) -C (= S) -, (u) -C (= S) NR6-, (v) -NR6C (= S) -, (w) -C (O) S-, (x) - SC (O) -, (y) -OC (= S) -, (z) -C (= S) O-, (aa) -NR6 (CNR6) NR6-, (bb) -CR6R6C (O) -, (cc) -C (O) NR6 (CR6R6) t -, (dd) a saturated, unsaturated, or aromatic 3-14 membered heterocycle containing one or more heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur; (ee) a saturated, unsaturated or aromatic 3-14 membered carbocycle; and (ff) - (CR6R6) t-; where (dd) or (ee) is optionally substituted with one or more R5 groups; B, E and H are independently selected from the group consisting of: (a) a single link; (b) a 3-14 membered saturated, unsaturated or aromatic heterocycle, containing one or more heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur; (c) a 3-14 membered saturated, unsaturated or aromatic carbocycle; where (b) or (c) is optionally substituted with one or more R5 groups; (d) - (C1-8 alkyl) -, (e) - (C2-8 alkenyl) -, (f) - (C2-8 alkynyl) -, where: i) 0-4 carbon atoms in any of ( d) - (f) immediately above are optionally replaced by a remainder selected from the group consisting of -O-, -S (O) p-, -NR6-, - (C = O) -, -C (= NR6) -, -S (O) pNR6-, -NR6S (O) p- and -NR6S (O) pNR6-; ii) any of (d) - (f) immediately above is optionally substituted with one or more R5 groups; and iii) any of (d) - (f) immediately above is optionally substituted with groups - (C1-8 alkyl) -R5; and (g) - (CR6R6) t-; C, F and J are independently selected from the group consisting of: (a) hydrogen, (c) F, (d) Cl, (e) Br, (f) I, (g) -CF3, (h) -CN, (i) -N3, (j) -NO2, (k) -NR6 (CR6R6) tR8, (l) -OR8, (m) -S (O) p (CR6R6) tR8, (n) -C (O) (CR6R6) tR8, (o) -OC (O) (CR6R6) tR8, (p) -SC (O) (CR6R6) tR8, (q) -C (O) O (CR6R6) tR8, (r ) -NR6C (O) (CR6R6) tR8, (s) -C (O) NR6 (CR6R6) tR8, (t) -C (= NR6) (CR6R6) tR8, (u) -C (= NNR6R6) (CR6R6 ) tR8, (v) -C (= NNR6C (O) R6) (CR6R6) tR8, (w) -C (= NOR8) (CR6R6) tR8, (x) -NR6C (O) O (CR6R6) tR8, ( y) -OC (O) NR6 (CR6R6) tR8, (z) -NR6C (O) NR6 (CR6R6) tR8, (aa) -NR6S (O) p (CR6R6) tR8, (bb) -S (O) pNR6 (CR6R6) tR8, (cc) -NR6S (O) pNR6 (CR6R6) tR8, (dd) -NR6R8, (ee) -NR6 (CR6R6) R8, (ff) -OH, (gg) -NR8R8, (hh) -OCH3, (ii) -S (O) pR8, (jj) -NC (O) R8, (kk) -NR6C (NR6) NR6R8, (II) a C1-8 alkyl group, (mm) a C2 alkenyl group -8, (nn) a C2-8 alkynyl group, (oo) a saturated, unsaturated or aromatic 3-14 membered heterocycle containing one or more heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, ( pp) a 3-14 membered saturated, unsaturated, or aromatic carbocycle (qq) - (CR6R6) tNR6 (CR6R6) tR8, (rr) -N [(CR6R6) tR8] [C = O (CR6R6) tR8], (ss) - (CR6R6) tN [(CR6R6) tR8] [(CR6R6) tR8], (tt) - (CR6R6) tNR6 (C = O) (CR6R6) tR8, (uu) -haloalkyl, (vv) -C (O) (CR6) [(CR6R6) tR8] R8, (ww) - (CR6R6) tC (O) NR8R8, (xx) - (CR6R6) tC (O) O (CR6R6) tR8, (yy) -NR6C ( O) CR8R8R8, (zz) -N [(CR6R6) tR8] C (O) R8 and (aaa) -S (O) pNR8R8; where (II) to (pp) are optionally substituted with one or more R7 groups; R5 is selected from (a) hydrogen, (b) F, (e) Cl, (d) Br, (e) I, (f) -CF3, (g) -CN, (h) -N3 (i) - NO2, (j) -NR6R6, (k) -OR8, (l) -NR6 (CNR6) NR6R6, (m) -C1-8 alkyl, (n) -C1-8 alkenyl, (o) -C1-8 alkynyl , (p) - (C1-8 alkyl) - (3-14 membered saturated, unsaturated, or aromatic heterocycle, containing one or more heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur), (q) - ( C1-8 alkyl) - (3-14 membered saturated, unsaturated, or aromatic carbocycle), (r) -haloalkyl, (s) -SR6, (t) -3-14 saturated, unsaturated, or aromatic heterocycle which it contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, and (u) - 3-14 membered carboxycycle saturated, unsaturated, or aromatic; alternatively, two R5 groups are taken together to form a carbocycle; where (m) a (r) and (t) a (u) are optionally substituted with one or more R8; R6 is selected from (a) hydrogen, (b) -C 1-8 alkyl, or alternatively, two R6 groups are taken together to form a carbocycle, (c) -haloalkyl, (d) -3-14 saturated heterocycle, unsaturated, or aromatic, containing one or more heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur; and (e) - 3-14 membered saturated, unsaturated, or aromatic carbocycle; where (b) to (e) are optionally substituted with one or more R8; R7 is selected from (a) hydrogen, (b) F, (c) Cl, (d) Br, (e) I, (f) -CF3, (g) -CN, (h) -N3, (i) -NO2, (j) -NR6R6, (k) -OR6, (l) -NR6 (CNR) NR6R6, (m) -C1-8 alkyl, (n) -C1-8 alkenyl, (o) -C1 -alkyl 8, (p) - (C1-8 alkyl) - (3-14 membered saturated, unsaturated, or aromatic heterocycle containing one or more heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur), (q) - ( C1-8 alkyl) - (3-14 membered saturated, unsaturated, or aromatic carbocycle), (r) -haloalkyl, (s) -NR6R8, (t) -OR8, (u) - (CR6R6) tNR6R8, (v ) -CR6R8R8, (w) -SR6, (x) -3-14 saturated, unsaturated, or aromatic heterocycle, containing one or more heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, (y) -carbocycle 3 - 14 members saturated, unsaturated or aromatic, (z) - (CR6R6) tC (O) NR8R8, (aa) -S (O) pR8, (bb) -NR6C (O) NR6R6, (cc) -NR6C ( O) R6 and (dd) -C (= NR6) NR6R6; where (m) a (q) and (x) a (y) are optionally substituted with one or more R9; R8 is selected from (a) hydrogen, (b) F, (c) Cl, (d) Br, (e) I, (f) -CF3, (g) -CN, (h) -N3, (i) -NO2, (j) -NR6R9, (k) -OR9, (l) -NR6 (CNR6) NR6R6, (m) -C1-8 alkyl, (n) -C1-8 alkenyl, (o) -C1 -alkyl 8, (p) - (C1-8 alkyl) - (3-14 membered saturated, unsaturated or aromatic heterocycle containing one or more heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur), (q) - (alkyl C1-8) - (3 - 14 saturated, unsaturated or aromatic carbocycle), (r) - 3 - 14 saturated, unsaturated, or aromatic heterocycle containing one or more heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, (s)-3-14 membered saturated, unsaturated or aromatic carbocycle, (t) -haloalkyl, (u) -C (O) (CR6R6) tR9, (v) -SR6, (w) -OC ( O) (CR6R6) tR9, (x) -NR6C (O) NR6R9, (y) -NR6C (O) R9, (z) -NR6 (CNR9) (NR6R6), (aa) -ONR6 (CNR6) NR6R6, ( bb) -C (= NR9) NR6R6, (cc) -S (O) pR9, (dd) - (CR6R6) tC (O) NR6R9, (ee) - (CR6R6) tOR9 and (ff) - (CR6R6) tNR6R9 ; where (m) a (s) are optionally substituted with one or more R9; R9 is selected from (a) hydrogen, (b) F, (c) Cl, (d) Br, (e) I, (f) -CF3, (g) -CN, (h) -N3, (i) -NO2, (j) -NR6R10, (k) -OR6, (l) -NR6 (CNR6) NR6R6, (m) -C (O) (CR6R6) tNR6R6, (n) -C1-8 alkyl, (o) -C 1-4 alkenyl, (p) C 1-8 alkynyl, (q) -3-14 saturated, unsaturated or aromatic heterocycle containing one or more heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, (r) - 3-14 membered saturated, unsaturated or aromatic carbocycle, (s) -haloalkyl, (t) - (CR6R6) tOR6, (u) -O (CR6R6) tNR6R10, (v) -C (O) R6, (w ) -SR6, (x) -C (O) OR10, (y) -S (O) pR6, (z) - (C1-8 alkyl) - (3-14 membered saturated, unsaturated or aromatic heterocycle containing one or more heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur), (aa) - (C1-8 alkyl) - (3-14 membered saturated, unsaturated or aromatic carbocycle), (bb) -O (CR6R6) tOR6 , (cc) -C (= NR6) NR6R6, (dd) -ONR6R6, (ee) -NR6C (O) NR6R6, (ff) -O (CR6R6) tOR6, (gg) -NR6C (O) R6 and (hh ) - (CR6R6) tNR6 R10; where (n) a (r) and (z) a (aa) are optionally substituted with one or more R10; R10 is selected from (a) hydrogen, (b) F, (c) Cl, (d) Br, (e) I, (f) -CF3, (g) -CN, (h) -N3, (i) -NO2, (j) -NR6R6, (k) -OR6, (l) -NR6 (CNR6) NR6R6, (m) -C (O) (CR6R6) tNR6R6, (n) -C1-8 alkyl, (o) -C1-8 alkenyl, (p) -C 1-8 alkynyl, (q) -3-14 saturated, unsaturated or aromatic heterocycle containing one or more heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, (r ) - 3-14 membered saturated, unsaturated or aromatic carbocycle, (s) -haloalkyl, (t) - (CR6R6) tOR6, (u) -O (CR6R6) tNR6R6, (v) -C (O) R6, ( w) -SR6, (x) -C (O) OR6, (y) -S (O) pR6, (z) - (C1-8 alkyl) - (heterocic

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