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AR076052A1 - Derivados de pirimidinas sustituidas, composiciones farmaceuticas que los contienen y uso de los mismos en trastornos asociados con receptores de histamina h4, tales como trastornos inflamatorios, prurito y dolor. - Google Patents

Derivados de pirimidinas sustituidas, composiciones farmaceuticas que los contienen y uso de los mismos en trastornos asociados con receptores de histamina h4, tales como trastornos inflamatorios, prurito y dolor.

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Publication number
AR076052A1
AR076052A1 ARP100100885A ARP100100885A AR076052A1 AR 076052 A1 AR076052 A1 AR 076052A1 AR P100100885 A ARP100100885 A AR P100100885A AR P100100885 A ARP100100885 A AR P100100885A AR 076052 A1 AR076052 A1 AR 076052A1
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AR
Argentina
Prior art keywords
cr11ar11b
cr12ar12b
nrcrd
alkyl
nrcc
Prior art date
Application number
ARP100100885A
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English (en)
Inventor
Thomas P Maduskuie
Wenqing Yao
Jincong Zhuo
Ding-Quan Qian
Original Assignee
Incyte Corp
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Publication date
Application filed by Incyte Corp filed Critical Incyte Corp
Publication of AR076052A1 publication Critical patent/AR076052A1/es

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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
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
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    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
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    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/84—Nitrogen atoms
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    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
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    • 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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    • 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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    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • 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
    • C07D409/12—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 linked by a chain containing hetero atoms as chain links
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    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • General Health & Medical Sciences (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
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  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Reivindicacion 1: Un compuesto de la formula (1) o (2) o su sal farmacéuticamente aceptable o N-oxido o su sal de amonio cuaternario, caracterizado porque: el anillo A es un grupo arilo o heteroarilo de 5 o 6 miembros en donde el anillo A está ligado con el anillo pirimidina a través de un átomo de carbono del anillo A, en donde cada uno de los átomos formadores del anillo del grupo heteroarilo de 5 o 6 miembros está seleccionado, de modo independiente, de C, N, O y S y en donde el anillo A está sustituido con 0, 1, 2 o 3 -W1a-X1a-W1-X1-Y1-Z1; en donde -W1a-X1a-W1-X1-Y1-Z1 es distinto de H; el anillo B es un grupo cicloalquilo o heterocicloalquilo de 4 - 20 miembros que está fusionado con el anillo A, en donde cada uno de los átomos formadores del anillo del grupo heterocicloalquilo de 4 - 20 miembros está seleccionado, de modo independiente, de C, N, O y S, en donde el anillo B está sustituido con 0, 1, 2, 3, 4, 5 o 6 -W2a-X2a-W2-X2-Y2-Z2; en donde -W2a-X2a-W2-X2-Y2-Z2 es distinto de H; el anillo C es grupo arilo o heteroarilo de 5 o 6 miembros fusionado con el anillo pirimidina, en donde cada uno de los átomos formadores del anillo del grupo heteroarilo de 5 o 6 miembros está seleccionado, de modo independiente, de C, N, O y S y en donde el anillo C está sustituido con -C(O)NR9R10 y con 0, 1, 2 o 3 R8; R1 es NR2R3, en donde R2 y R3 junto con el átomo de N al que están unidos forman un grupo heterocicloalquilo de 4 - 10 miembros en donde cada uno de los átomos formadores del anillo del grupo heterocicloalquilo de 4 - 10 miembros está seleccionado, de modo independiente, de C, N, O y S y en donde el grupo heterocicloalquilo de 4 - 10 miembros está sustituido con 0, 1, 2, 3, 4, 5, 6, 7 u 8 R4; cada R4 está seleccionado, de modo independiente, de halo, CN, alquilo C1-6, haloalquilo C1-6, cicloalquilo C3-7, OH, oxo, alcoxi C1-6, haloalcoxi C1-6, NH2, NH(alquilo C1-4), NH(cicloalquilo C3-7) y N(alquilo C1-4)2, en donde cada uno del alquilo C1-6 y cicloalquilo C3-7 está sustituido con 0, 1, 2 o 3 sustituyentes seleccionados cada uno, de modo independiente, de halo, OH, CN, NH2, NH(alquilo C1-4) y N(alquilo C1-4)2; cada R8 está seleccionado, de modo independiente, de halo, CN, NO2, ORa4, SRa4, SF5, C(O)Rb4, C(O)NRc4Rd4, C(O)ORa4, OC(O)Rb4, OC(O)NRc4Rd4, NRc4Rd4, NRc4C(O)Rb4, NRc4C(O)NRc4Rd4, NRc4C(O)ORa4, C(=NRg4)NRc4Rd4, NRc4C(=NRg4)NRc4Rd4, NRc4S(O)2NRc4Rd4, S(O)Rb4, S(O)NRc4Rd4, S(O)2Rb4, NRc4S(O)2Rb4, S(O)2NRc4Rd4, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo y heterocicloalquilalquilo, en donde cada uno del alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo y heterocicloalquilalquilo está sustituido con 0, 1, 2, 3, 4 o 5 sustituyentes seleccionados cada uno, de modo independiente, de R8a, halo, CN, NO2, oxo, ORa4, SRa4, SF5, C(O)Rb4, C(O)NRc4Rd4, C(O)ORa4, OC(O)Rb4, OC(O)NRc4Rd4, NRc4Rd4, NRc4C(O)Rd4, NRc4C(O)ORa4, NRc4S(O)2Rb4, NRc4S(O)2NRc4Rd4, S(O)Rb4, S(O)NRc4Rd4, S(O)2Rb4 y S(O)2NRc4Rd4; R9 y R10 están seleccionados cada uno, de modo independiente, de H, alquilo C1-6, haloalquilo C1-6, arilalquilo, heteroarilalquilo, cicloalquilalquilo, heterocicloalquilalquilo, alquenilo C2-6, alquinilo C2-6, arilo, heteroarilo, cicloalquilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo y heterocicloalquilalquilo, en donde cada uno del alquilo C1-6, haloalquilo C1-6, arilalquilo, heteroarilalquilo, cicloalquilalquilo, heterocicloalquilalquilo, alquenilo C2-6, alquinilo C2-6, arilo, heteroarilo, cicloalquilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo y heterocicloalquilalquilo está sustituido con 0, 1, 2, 3, 4 o 5 sustituyentes seleccionados, de modo independiente, de R10a, halo, CN, NO2, ORa5, SRa5, C(O)Rb5, C(O)NRc5Rd5, C(O)ORa5, OC(O)Rb5, OC(O)NRc5Rd5, NRc5Rd5, NRc5C(O)Rb5, NRc5C(O)NRc5Rd5, NRc5C(O)ORa5, C(=NRg5)NRc5Rd5, NRc5C(=NRg5)NRc5Rd5, NRc5S(O)2NRc5Rd5, S(O)Rb5, S(O)NRc5Rd5, S(O)2Rb5, NRc5S(O)2Rb5 y S(O)2NRc5Rd5; o R9 y R10 junto con el átomo de N al que están unidos forman un grupo heterocicloalquilo de 4 - 14 miembros que está sustituido con 0, 1, 2, 3, 4 o 5 sustituyentes seleccionados, de modo independiente, de R10a, halo, CN, NO2, oxo, ORa5, SRa5, C(O)Rb5, C(O)NRc5Rd5, C(O)ORa5, OC(O)Rb5, OC(O)NRc5Rd5, NRc5Rd5, NRc5C(O)Rb5, NRc5C(O)NRc5Rd5, NRc5C(O)ORa5, C(=NRg5)NRc5Rd5, NRc5C(=NRg5)NRc5Rd5, NRc5S(O)2NRc5Rd5, S(O)Rb5, S(O)NRc5Rd5, S(O)2Rb5, NRc5S(O)2Rb5 y S(O)2NRc5Rd5; W1a, W2a, W1 y W2 están seleccionados cada uno, de modo independiente, de ausente, alquilenilo C1-6, alquenilenilo C2-6, alquinilenilo C2-6, (CR11aR11b)p1O(CR11aR11b)p2, (CR11aR11b)p1S(CR11aR11b)p2, (CR11aR11b)p1NRe(CR11aR11b)p2, (CR11aR11b)p1C(O)(CR11aR11b)p2, (CR11aR11b)p1C(S)(CR11aR11b)p2, (CR11aR11b)p1C(O)O(CR11aR11b)p2, (CR11aR11b)p1C(O)NRe(CR11aR11b)p2, (CR11aR11b)p1C(S)NRe(CR11aR11b)p2, (CR11aR11b)p1S(O)(CR11aR11b)p2, (CR11aR11b)p1S(O)2(CR11aR11b)p2, (CR11aR11b)p1S(O)NRe(CR11aR11b)p2, (CR11aR11b)p1S(O)2NRe(CR11aR11b)p2, (CR11aR11b)p1NReC(O)NRf(CR11aR11b)p2, (CR11aR11b)p1NReC(S)NRf(CR11aR11b)p2, (CR11aR11b)p1NReS(O)2NRf(CR11aR11b)p2, (CR11aR11b)p1C(=NRg)NRe(CR11aR11b)p2, (CR11aR11b)p1NReC(=NRg)NRf(CR11aR11b)p2, O(CR11aR11b)q1C(O), S(CR11aR11b)q1C(O), NRe(CR11aR11b)q1C(O), C(O)(CR11aR11b)q1C(O), NRe(CR11aR11b)q1NRf, O(CR11aR11b)q1NRf, y O(CR11aR11b)q1O, en donde cada uno del alquilenilo C2-6, alquenilenilo C2-6 y alquinilenilo C2-6 está sustituido con 0, 1, 2, 3, 4, 5, 6, 7 u 8 sustituyentes seleccionados cada uno, de modo independiente, de halo, CN, NO2, ORa, SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, NRcRd, NRcC(O)Rb, NRcC(O)NRcRd, NRcC(O)ORa, C(=NRg)NRcRd, NRcC(=NRg)NRcRd, NRcS(O)2NRcRd, S(O)Rb, S(O)NRcRd, S(O)2Rb, NRcS(O)2Rb y S(O)2NRcRd; X1a, X2a, X1 y X2 están seleccionados cada uno, de modo independiente, de ausente, alquilenilo C1-6, alquenilenilo C2-6, alquinilenilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo y heterocicloalquilalquilo, en donde cada uno de dicho alquilenilo C1-6, alquenilenilo C2-6, alquinilenilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo y heterocicloalquilalquilo está sustituido con 0, 1, 2, 3, 4, 5, 6, 7 u 8 sustituyentes seleccionados cada uno, de modo independiente, de RXX, halo, CN, NO2, oxo, ORa, SRa, SF5, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, NRcRd, NRcC(O)Rb, NRcC(O)NRcRd, NRcC(O)ORa, C(=NRg)NRcRd, NRcC(=NRg)NRcRd, NRcS(O)2NRcRd, S(O)Rb, S(O)NRcRd, S(O)2Rb, NRcS(O)2Rb y S(O)2NRcRd; Y1 e Y2 están seleccionados cada uno, de modo independiente, de ausente, alquilenilo C1-6, alquenilenilo C2-6, alquinilenilo C2-6, (CR12aR12b)p3O(CR12aR12b)p4, (CR12aR12b)p3S(CR12aR12b)p4, (CR12aR12b)p3NRe(CR12aR12b)p4, (CR12aR12b)p3C(O)(CR12aR12b)p4, (CR12aR12b)p3C(S)(CR12aR12b)p4, (CR12aR12b)p3C(O)O(CR12aR12b)p4, (CR12aR12b)p3C(O)NRe(CR12aR12b)p4, (CR12aR12b)p3C(S)NRe(CR12aR12b)p4, (CR12aR12b)p3S(O)(CR12aR12b)p4, (CR12aR12b)p3S(O)2(CR12aR12b)p4, (CR12aR12b)p3S(O)NRe(CR12aR12b)p4, (CR12aR12b)p3S(O)2NRe(CR12aR12b)p4, (CR12aR12b)p3NReC(O)NRf(CR12aR12b)p4, (CR12aR12b)p3NReC(S)NRf(CR12aR12b)p4, (CR12aR12b)p3NReS(O)2NRf(CR12aR12b)p4, (CR12aR12b)p3C(=NRg)NRe(CR12aR12b)p4, (CR12aR12b)p3NReC(=NRg)NRf(CR12aR12b)p4, O(CR12aR12b)q2C(O), S(CR12aR12b)q2C(O), NRe(CR12aR12b)q2C(O), NRe(CR12aR12b)q2NRf, O(CR12aR12b)q2NRf, y O(CR12aR12b)q2O, en donde cada uno del alquilenilo C1-6, alquenilenilo C2-6 y alquinilenilo C2-6 está sustituido con 0, 1, 2, 3, 4, 5, 6, 7 u 8 sustituyentes seleccionados, de modo independiente, de alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, halo, CN, NO2, oxo, ORa, SRa, SF5, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, NRcRd, NRcC(O)Rb, NRcC(O)NRcRd, NRcC(O)ORa, C(=NRg)NRcRd, NRcC(=NRg)NRcRd, NRcS(O)2NRcRd, S(O)Rb, S(O)NRcRd, S(O)2Rb, NRcS(O)2Rb, y S(O)2NRcRd; z1 y z2 están seleccionados cada uno, de modo independiente, de H, halo, CN, NO2, ORa, SRa, SF5, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, NRcRd, NRcC(O)Rb, NRcC(O)NRcRd, NRcC(O)ORa, C(=NRg)NRcRd, NRcC(=NRg)NRcRd, NRcS(O)2NRcRd, S(O)Rb, S(O)NRcRd, S(O)2Rb, NRcS(O)2Rb y S(O)2NRcRd; alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo y heterocicloalquilalquilo, en donde cada uno del alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo y heterocicloalquilalquilo está sustituido con 0, 1, 2, 3, 4, 5, 6, 7 u 8 sustituyentes seleccionados cada uno, de modo independiente, de RZZ, halo, CN, NO2, ORa, SRa, SF5, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, NRcRd, NRcC(O)Rd, NRcC(O)ORa, NRcS(O)2Rb, NRcS(O)2NRcRd, S(O)Rb, S(O)NRcRd, S(O)2Rb y S(O)2NRcRd; R11a, R11b, R12a y R12b están seleccionados cada uno, de modo independiente, de H, halo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, cicloalquilo, heterocicloalquilo, arilo, heteroarilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo, heterocicloalquilalquilo, CN, NO2, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)NRc1Rd1, NRc1C(O)ORa1, C(=NRg1)NRc1Rd1, NRc1C(=NRg1)NRc1Rd1, NRc1S(O)2NRc1Rd1, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1, NRc1S(O)2Rb1 y S(O)2NRc1Rd1; en donde cada uno de dicho alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, cicloalquilo, heterocicloalquilo, arilo, heteroarilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo y heterocicloalquilalquilo está sustituido con 0, 1, 2, 3, 4 o 5 sustituyentes seleccionados cada uno, de modo independiente, de halo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, cic
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