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AR073047A1 - IMIDAZOL DERIVATIVES - Google Patents

IMIDAZOL DERIVATIVES

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Publication number
AR073047A1
AR073047A1 ARP090103196A ARP090103196A AR073047A1 AR 073047 A1 AR073047 A1 AR 073047A1 AR P090103196 A ARP090103196 A AR P090103196A AR P090103196 A ARP090103196 A AR P090103196A AR 073047 A1 AR073047 A1 AR 073047A1
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AR
Argentina
Prior art keywords
heterocyclyl
carbocyclyl
alkyl
optionally substituted
opportunity
Prior art date
Application number
ARP090103196A
Other languages
Spanish (es)
Inventor
Lynsie Almeida
Claudio E Chuaqui
Stephanos Ioannidis
Huiping Guan
Bo Peng
Qibin Su
Michelle Lamb
Original Assignee
Astrazeneca Ab
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Publication date
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of AR073047A1 publication Critical patent/AR073047A1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—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 three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • C07D401/14—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 three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Un compuesto de formula (1) y sus sales, composiciones farmacéuticas, métodos de uso y métodos para su preparacion. Estos compuestos proveen un tratamiento para trastornos mieloproliferativos y cáncer. Reivindicacion 1: Un compuesto caracterizado porque responde a la formula (1) o una sal aceptable farmacéuticamente de la misma, donde el anillo A es heteroarilo de 5 o 6 miembros, donde dicho heteroarilo de 5 o 6 miembros se sustituye opcionalmente sobre carbono con uno o más R6, y donde si dicho heteroarilo de 5 o 6 miembros contiene una porcion -NH-, esa porcion -NH- se sustituye opcionalmente con R6*; D se selecciona entre N y C-R3; E se selecciona entre N y C-R4; donde al menos uno de D y E es carbono; X se selecciona entre -NH-, -O-, y -S-; R1* se selecciona entre H, -CN, alquilo C1-6, carbociclilo, heterociclilo, -OR1a, -N(R1a)2, -C(O)H, -C(O)R1b, -C(O)2R1c, -C(O)N(R1a)2, -S(O)R1b, -S(O)2R1b, -S(O)2N(R1a)2, -C(R1a)=N(R1a), y -C(R1a)=N(OR1a) donde dichos alquilo C1-6, carbociclilo, y heterociclilo se sustituyen opcionalmente sobre carbono con uno o más R10, y donde si dicho heterociclilo contiene una porcion -NH-, esa porcion -NH- se sustituye opcionalmente con R10*; R2 se selecciona entre H, halo, -CN, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, carbociclilo de 3 a 6 miembros, heterociclilo de 4 a 6 miembros, -OR2a, -SR2a, -N(R2a)2, -N(R2a)C(O)R2b, -N(R2a)N(R2a)2, -NO2, -N(R2a)(OR2a), -ON(R2a)2, -C(O)H, -C(O)R2b, -C(O)2R2a, -C(O)N(R2a)2, -C(O)N(R2a)(OR2a)-oc(o)N(R2a)2, -N(R2a)c(o)2R2a, -N(R2a)c(o)N(R2a)2, -OC(O)R2b, -S(O)R2b, -S(O)2R2b, -S(O)2N(R2a)2, -N(R2a)s(o)2R2b, y -C(R2a)=N(OR2a), donde dichos alquilo C1-6, alquenilo C2-6, alquinilo C2-6, carbociclilo, y heterociclilo se sustituyen opcionalmente sobre carbono con uno o más R20, y donde si dicho heterociclilo contiene una porcion -NH-, esa porcion -NH- se sustituye opcionalmente con R20*; R2a en cada oportunidad se selecciona independientemente entre H, alquilo C1-6, carbociclilo, y heterociclilo, donde dichos alquilo C1-6, carbociclilo, y heterociclilo en cada oportunidad se sustituyen opcionalmente e independientemente sobre carbono con uno o más R20, y donde si dicho heterociclilo contiene una porcion -NH-, esa porcion -NH- se sustituye opcionalmente con R20*; R2b en cada oportunidad se selecciona entre alquilo C1-6, alquenilo C2-6, alquinilo C2-6, carbociclilo, y heterociclilo, donde dichos alquilo C1-6, alquenilo C2-6, alquinilo C2-6, carbociclilo, y heterociclilo en cada oportunidad se sustituyen opcionalmente e independientemente sobre carbono con uno o más R20, y donde si dicho heterociclilo contiene una porcion -NH-, esa porcion -NH- se sustituye opcionalmente con R20; R2c en cada oportunidad se selecciona independientemente entre alquilo C1-6, carbociclilo, y heterociclilo, donde dichos alquilo C1-6, carbociclilo, y heterociclilo en cada oportunidad se sustituyen opcionalmente a independientemente sobre carbono con uno o más R20 y donde si dicho heterociclilo contiene una porcion -NH-, esa porcion -NH- se sustituye opcionalmente con R20*; R3 se selecciona entre H, halo, -CN, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, carbociclilo, heterociclilo, -OR3a, -SR3a, -N(R3a)2, -N(R3a)C(O)R3b, -N(R3a)N(R3a)2, -NO2, -N(R3a)(OR3a), -O-N(R3a)2, -C(O)H, -C(O)R3b, -C(O)2R3a, -C(O)N(R3a)2, -c(O)N(R3a)(OR3a), -OC(O)N(R3a)2, -N(R3a)C(O)2R3, -N(R)c(o)N(R3a)2, -OC(O)R3b, -S(O)R3b, -S(O)2R3b, -s(o)2N(R3a)2, -N(R3a)S(O)2R3b, -C(R3a)=N(R3a), y -C(R3a)=N(OR3a), donde dichos alquilo C1-6, alquenilo C2-6, alquinilo C2-6, carbociclilo y heterociclilo se sustituyen opcionalmente sobre carbono con uno o más R30, y donde si dicho heterociclilo contiene una porcion -NH-, esa porcion -NH- se sustituye opcionalmente con R30*; R3a en cada oportunidad se selecciona independientemente entre H, alquilo C1-6, carbociclilo, y heterociclilo, donde dicho alquilo C1-6, carbociclilo, y heterociclilo en cada oportunidad se sustituyen opcionalmente e independientemente sobre carbono con uno o más R30, y donde si dicho heterociclilo contiene una porcion -NH-, esa porcion -NH- se sustituye opcionalmente con R30*; R3b en cada oportunidad se selecciona entre alquilo C1-6, alquenilo C2-6, alquinilo C2-6, carbociclilo y heterociclilo, donde dicho alquilo C1-6, alquenilo C2-6, alquinilo C2-6, carbociclilo, y heterociclilo en cada oportunidad se sustituyen opcionalmente e independientemente sobre carbono con uno o más R30 y donde si dicho heterociclilo contiene una porcion -NH-, esa porcion -NH- se sustituye opcionalmente con R30*; R4 se selecciona entre H, halo, -CN, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, carbociclilo, heterociclilo, -OR4a, -sR4a, -N(R4a)2, -N(R4a)c(o)R4b, -N(R4a)N(R4a)2, -NO2, -N(R4a)(OR4a), -ON(R4a)2, -C(O)H, -C(O)R4b, -C(O)2R4a, -C(O)N(R4a)2, -C(O)N(R4a)(OR4a), -OC(O)N(R4a)2, -N(R4a)c(o)2R4a, -N(R4a)C(O)N(R4a)2, -OC(O)R4b, -S(O)R4b, -S(O)2R4b, -s(o)2N(R4a)2, -N(R4a)S(O)2R4b, -C(R4a)=N(R4a), y -C(R4a)=N(OR4a), donde dicho alquilo C1-6, alquenilo C2-6, alquinilo C2-6, carbociclilo y heterociclilo se sustituyen opcionalmente sobre carbono con uno o más R40; y donde si dicho heterociclilo contiene una porcion -NH-, esa porcion -NH- se sustituye opcionalmente con R40*; R4a en cada oportunidad se selecciona independientemente entre H, alquilo C1-6, carbociclilo, y heterociclilo, donde dicho alquilo C1-6, carbociclilo, y heterociclilo en cada oportunidad se sustituyen opcionalmente e independientemente sobre carbono con uno o más R40, y donde si dicho heterociclilo contiene una porcion -NH-, esa porcion -NH- se sustituye opcionalmente con R40*; R4b en cada oportunidad se selecciona entre alquilo C1-6, alquenilo C2-6, alquinilo C2-6, carbociclilo, y heterociclilo, donde dicho alquilo C1-6, alquenilo C2-6, alquinilo C2-6, carbociclilo, y heterociclilo en cada oportunidad se sustituyen opcionalmente e independientemente sobre carbono con uno o más R40, y donde si dicho heterociclilo contiene una porcion -NH-, esa porcion -NH- se sustituye opcionalmente con R40*; R4c en cada oportunidad se selecciona independientemente entre alquilo C1-6, carbociclilo, y heterociclilo, donde dicho alquilo C1-6, carbociclilo, y heterociclilo en cada oportunidad se sustituyan opcionalmente e independientemente sobre carbono con uno o más R40 y donde si dicho heterociclilo contiene una porcion -NH-, esa porcion -NH- se sustituye opcionalmente con R40*; R5 se selecciona entre H, halo, -CN, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, carbociclilo, heterociclilo, -OR5a, -SR5a, -N(R5a)2, -N(R5a)C(O)R5b, -N(R5a)N(R5a)2, -NO2, -N(R5a)(OR5a), -O-N(R5a)2, -C(O)H, -C(O)R5b, -c(o)2R5a, -C(O)N(R5a)2, -C(O)N(R5a)(OR5a), -OC(O)N(R5a)2, -N(R5a)c(O)2R5a, -N(R5a)C(O)N(R5a)2, -OC(O)R5b, -S(O)R5b, -SCO)2R5b, -S(O)2N(R5a)2, -N(R5a)S(O)2R5b, -C(R5a)=N(R5a), y -C(R5a)=N(OR5a), donde dicho alquilo C1-6, alquenilo C2-6, alquinilo C2-6, carbociclilo, y heterociclilo se sustituyen opcionalmente sobre carbono con uno o más R50 y donde si dicho heterociclilo contiene una porcion -NH-, esa porcion -NH- se sustituye opcionalmente con R50*; R5a en cada oportunidad se selecciona independientemente entre H, alquilo C1-6, carbociclilo, y heterociclilo, donde dichos alquilo C1-6, carbociclilo, y heterociclilo en cada oportunidad se sustituyen opcionalmente e independientemente sobre carbono con uno o más R50 y donde si dicho heterociclilo contiene una porcion -NH-, esa porcion -NH- se sustituye opcionalmente con R50*; R5b en cada oportunidad se selecciona entre alquilo C1-6, alquenilo C2-6, alquinilo C2-6, carbociclilo, y heterociclilo, donde dichos alquilo C1-6, alquenilo C2-6, alquinilo C2-6, carbociclilo, y heterociclilo en cada oportunidad se sustituyen opcionalmente e independientemente sobre carbono con uno o más R50, y donde si dicho heterociclilo contiene una porcion -NH-, esa porcion -NH- se sustituye opcionalmente con R50*; R5c en cada oportunidad se selecciona independientemente entre alquilo C1-6, carbociclilo, y heterociclilo, donde dichos alquilo C1-6, carbociclilo, y heterociclilo en cada oportunidad se sustituyen opcionalmente e independientemente sobre carbono con uno o más R50, y donde si dicho heterociclilo contiene una porcion -NH-, esa porcion -NH- se sustituye opcionalmente con R50*; R6 en cada oportunidad se selecciona independientemente entre halo, -CN, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, carbociclilo, heterociclilo, -OR6a, -SR6a, -N(R6a)2, -N(R6a)c(o)R6b, -N(R6a)N(R6a)2, -NO2, -N(R6a)(OR6a), -O-N(R6a)2, -C(O)H, -C(O)R6b, -C(O)2R6a, -c(o)N(R6a)2, -C(O)N(R6a)(OR6a), -OC(O)N(R6a)2, -N(R6a)c(o)2R6a, -N(R6a)C(O)N(R6a)2, -OC(O)R6b, -S(O)R6b, -S(O)2R6b, s(o)2N(R6a)2, -N(R6a)S(O)2R6b, -C(R6a)=N(R6a), y -C(R5a)=N(OR5a), donde dichos alquilo C1-6, alquenilo C2-6, alquinilo C2-6, carbociclilo, heterociclilo en cada oportunidad se sustituyen opcionalmente e independientemente sobro carbono con uno o más R60, y donde si dicho heterociclilo contiene una porcion -NH-, esa porcion -NH- se sustituye opcionalmente con R60*; R6* en cada oportunidad se selecciona independientemente entre -CN, alquilo C1-6, carbociclilo, heterociclilo, -OR6a, -N(R6a)2, -C(O)H, -C(O)R6b, -C(O)2R6c, -C(O)N(R6a)2, -S(O)R6b, -S(O)2R6b, -S(O)2N(R6a)2, -C(R6a)=N(R6a)y -C(R6a)=N(OR6a), donde dichos alquilo C1-6, carbociclilo, y heterociclilo en cada oportunidad se sustituyen opcionalmente e independientemente sobre carbono con uno o más R60, y donde si dicho heterociclilo contiene una porcion -NH-, esa porcion -NH- se sustituye opcionalmente con R60*; R6a en cada oportunidad se selecciona independientemente entre H, alquilo C1-6, carbociclilo, y heterociclilo, donde dichos alquilo C1-6, carbociclilo, y heterociclilo en cada oportunidad se sustituyen opcionalmente e independientemente sobre carbono con uno o más R60 y donde si dicho heterociclilo contiene una porcion -NH-, esa porcion -NH- se sustituye opcionalmente con R60*; R6b en cada oportunidad se selecciona entre alquilo C1-6, alquenilo C2-6, alquinilo C2-6, carbociclilo, heA compound of formula (1) and its salts, pharmaceutical compositions, methods of use and methods for its preparation. These compounds provide a treatment for myeloproliferative disorders and cancer. Claim 1: A compound characterized in that it responds to formula (1) or a pharmaceutically acceptable salt thereof, wherein ring A is 5 or 6 membered heteroaryl, wherein said 5 or 6 membered heteroaryl is optionally substituted on carbon with one or more R6, and where if said 5 or 6 membered heteroaryl contains a portion -NH-, that portion -NH- is optionally substituted with R6 *; D is selected from N and C-R3; E is selected from N and C-R4; where at least one of D and E is carbon; X is selected from -NH-, -O-, and -S-; R1 * is selected from H, -CN, C1-6 alkyl, carbocyclyl, heterocyclyl, -OR1a, -N (R1a) 2, -C (O) H, -C (O) R1b, -C (O) 2R1c, -C (O) N (R1a) 2, -S (O) R1b, -S (O) 2R1b, -S (O) 2N (R1a) 2, -C (R1a) = N (R1a), and -C (R1a) = N (OR1a) where said C1-6 alkyl, carbocyclyl, and heterocyclyl are optionally substituted on carbon with one or more R10, and where if said heterocyclyl contains a portion -NH-, that portion -NH- is optionally substituted with R10 *; R2 is selected from H, halo, -CN, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, 3-6 membered carbocyclyl, 4-6 membered heterocyclyl, -OR2a, -SR2a, -N (R2a ) 2, -N (R2a) C (O) R2b, -N (R2a) N (R2a) 2, -NO2, -N (R2a) (OR2a), -ON (R2a) 2, -C (O) H , -C (O) R2b, -C (O) 2R2a, -C (O) N (R2a) 2, -C (O) N (R2a) (OR2a) -oc (o) N (R2a) 2, - N (R2a) c (o) 2R2a, -N (R2a) c (o) N (R2a) 2, -OC (O) R2b, -S (O) R2b, -S (O) 2R2b, -S (O ) 2N (R2a) 2, -N (R2a) s (o) 2R2b, and -C (R2a) = N (OR2a), wherein said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, carbocyclyl, and heterocyclyl are optionally substituted on carbon with one or more R20, and where if said heterocyclyl contains a portion -NH-, that portion -NH- is optionally substituted with R20 *; R2a at each opportunity is independently selected from H, C1-6 alkyl, carbocyclyl, and heterocyclyl, wherein said C1-6 alkyl, carbocyclyl, and heterocyclyl at each opportunity are optionally and independently substituted on carbon with one or more R20, and where yes said heterocyclyl contains a portion -NH-, that portion -NH- is optionally substituted with R20 *; R2b is each time selected from C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, carbocyclyl, and heterocyclyl, wherein said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, carbocyclyl, and heterocyclyl at each opportunity is optionally and independently substituted on carbon with one or more R20, and where if said heterocyclyl contains a portion -NH-, that portion -NH- is optionally substituted with R20; R2c at each opportunity is independently selected from C1-6 alkyl, carbocyclyl, and heterocyclyl, wherein said C1-6 alkyl, carbocyclyl, and heterocyclyl at each opportunity is optionally substituted independently on carbon with one or more R20 and where said heterocyclyl contains a portion -NH-, that portion -NH- is optionally substituted with R20 *; R3 is selected from H, halo, -CN, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, carbocyclyl, heterocyclyl, -OR3a, -SR3a, -N (R3a) 2, -N (R3a) C ( O) R3b, -N (R3a) N (R3a) 2, -NO2, -N (R3a) (OR3a), -ON (R3a) 2, -C (O) H, -C (O) R3b, -C (O) 2R3a, -C (O) N (R3a) 2, -c (O) N (R3a) (OR3a), -OC (O) N (R3a) 2, -N (R3a) C (O) 2R3 , -N (R) c (o) N (R3a) 2, -OC (O) R3b, -S (O) R3b, -S (O) 2R3b, -s (o) 2N (R3a) 2, -N (R3a) S (O) 2R3b, -C (R3a) = N (R3a), and -C (R3a) = N (OR3a), wherein said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, carbocyclyl and heterocyclyl are optionally substituted on carbon with one or more R30, and where if said heterocyclyl contains a portion -NH-, that portion -NH- is optionally substituted with R30 *; R3a at each opportunity is independently selected from H, C1-6 alkyl, carbocyclyl, and heterocyclyl, wherein said C1-6 alkyl, carbocyclyl, and heterocyclyl at each opportunity is optionally and independently substituted on carbon with one or more R30, and where yes said heterocyclyl contains a portion -NH-, that portion -NH- is optionally substituted with R30 *; R3b at each opportunity is selected from C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, carbocyclyl and heterocyclyl, wherein said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, carbocyclyl, and heterocyclyl at each opportunity they are optionally and independently substituted on carbon with one or more R30 and where if said heterocyclyl contains a portion -NH-, that portion -NH- is optionally substituted with R30 *; R4 is selected from H, halo, -CN, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, carbocyclyl, heterocyclyl, -OR4a, -sR4a, -N (R4a) 2, -N (R4a) c ( o) R4b, -N (R4a) N (R4a) 2, -NO2, -N (R4a) (OR4a), -ON (R4a) 2, -C (O) H, -C (O) R4b, -C (O) 2R4a, -C (O) N (R4a) 2, -C (O) N (R4a) (OR4a), -OC (O) N (R4a) 2, -N (R4a) c (o) 2R4a , -N (R4a) C (O) N (R4a) 2, -OC (O) R4b, -S (O) R4b, -S (O) 2R4b, -s (o) 2N (R4a) 2, -N (R4a) S (O) 2R4b, -C (R4a) = N (R4a), and -C (R4a) = N (OR4a), wherein said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, carbocyclyl and heterocyclyl are optionally substituted on carbon with one or more R40; and where if said heterocyclyl contains a portion -NH-, that portion -NH- is optionally substituted with R40 *; R4a at each opportunity is independently selected from H, C1-6 alkyl, carbocyclyl, and heterocyclyl, wherein said C1-6 alkyl, carbocyclyl, and heterocyclyl at each opportunity is optionally and independently substituted on carbon with one or more R40, and where yes said heterocyclyl contains a portion -NH-, that portion -NH- is optionally substituted with R40 *; R4b on each occasion is selected from C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, carbocyclyl, and heterocyclyl, wherein said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, carbocyclyl, and heterocyclyl at each opportunity is optionally and independently substituted on carbon with one or more R40, and where if said heterocyclyl contains a portion -NH-, that portion -NH- is optionally substituted with R40 *; R4c at each opportunity is independently selected from C1-6 alkyl, carbocyclyl, and heterocyclyl, wherein said C1-6 alkyl, carbocyclyl, and heterocyclyl at each opportunity is optionally and independently substituted on carbon with one or more R40 and where if said heterocyclyl contains a portion -NH-, that portion -NH- is optionally substituted with R40 *; R5 is selected from H, halo, -CN, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, carbocyclyl, heterocyclyl, -OR5a, -SR5a, -N (R5a) 2, -N (R5a) C ( O) R5b, -N (R5a) N (R5a) 2, -NO2, -N (R5a) (OR5a), -ON (R5a) 2, -C (O) H, -C (O) R5b, -c (o) 2R5a, -C (O) N (R5a) 2, -C (O) N (R5a) (OR5a), -OC (O) N (R5a) 2, -N (R5a) c (O) 2R5a , -N (R5a) C (O) N (R5a) 2, -OC (O) R5b, -S (O) R5b, -SCO) 2R5b, -S (O) 2N (R5a) 2, -N (R5a ) S (O) 2R5b, -C (R5a) = N (R5a), and -C (R5a) = N (OR5a), wherein said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, carbocyclyl, and heterocyclyl are optionally substituted on carbon with one or more R50 and where if said heterocyclyl contains a portion -NH-, that portion -NH- is optionally substituted with R50 *; R5a at each opportunity is independently selected from H, C1-6 alkyl, carbocyclyl, and heterocyclyl, wherein said C1-6 alkyl, carbocyclyl, and heterocyclyl at each opportunity are optionally and independently substituted on carbon with one or more R50 and where said heterocyclyl contains a portion -NH-, that portion -NH- is optionally substituted with R50 *; R5b on each occasion is selected from C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, carbocyclyl, and heterocyclyl, wherein said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, carbocyclyl, and heterocyclyl at each opportunity is optionally and independently substituted on carbon with one or more R50, and where if said heterocyclyl contains a portion -NH-, that portion -NH- is optionally substituted with R50 *; R5c at each opportunity is independently selected from C1-6 alkyl, carbocyclyl, and heterocyclyl, wherein said C1-6 alkyl, carbocyclyl, and heterocyclyl at each opportunity is optionally and independently substituted on carbon with one or more R50, and where said heterocyclyl it contains a portion -NH-, that portion -NH- is optionally substituted with R50 *; R6 on each occasion is independently selected from halo, -CN, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, carbocyclyl, heterocyclyl, -OR6a, -SR6a, -N (R6a) 2, -N (R6a) c (o) R6b, -N (R6a) N (R6a) 2, -NO2, -N (R6a) (OR6a), -ON (R6a) 2, -C (O) H, -C (O) R6b, -C (O) 2R6a, -c (o) N (R6a) 2, -C (O) N (R6a) (OR6a), -OC (O) N (R6a) 2, -N (R6a) c (or ) 2R6a, -N (R6a) C (O) N (R6a) 2, -OC (O) R6b, -S (O) R6b, -S (O) 2R6b, s (o) 2N (R6a) 2, - N (R6a) S (O) 2R6b, -C (R6a) = N (R6a), and -C (R5a) = N (OR5a), wherein said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, carbocyclyl, heterocyclyl on each occasion are optionally and independently substituted on carbon with one or more R60, and where if said heterocyclyl contains a portion -NH-, that portion -NH- is optionally substituted with R60 *; R6 * on each occasion is independently selected from -CN, C1-6 alkyl, carbocyclyl, heterocyclyl, -OR6a, -N (R6a) 2, -C (O) H, -C (O) R6b, -C (O) 2R6c, -C (O) N (R6a) 2, -S (O) R6b, -S (O) 2R6b, -S (O) 2N (R6a) 2, -C (R6a) = N (R6a) and - C (R6a) = N (OR6a), where said C1-6 alkyl, carbocyclyl, and heterocyclyl are each optionally and independently substituted on carbon with one or more R60, and where if said heterocyclyl contains a portion -NH-, that portion -NH- is optionally substituted with R60 *; R6a at each opportunity is independently selected from H, C1-6 alkyl, carbocyclyl, and heterocyclyl, wherein said C1-6 alkyl, carbocyclyl, and heterocyclyl at each opportunity are optionally and independently substituted on carbon with one or more R60 and where said heterocyclyl contains a portion -NH-, that portion -NH- is optionally substituted with R60 *; R6b is selected each time from C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, carbocyclyl, he

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