AR076007A1 - Compuestos heterociclicos inhibidores de autotaxinas utiles para el tratamiento del cancer, composiciones farmaceuticas que los comprenden y proceso para prepararlos. - Google Patents

Compuestos heterociclicos inhibidores de autotaxinas utiles para el tratamiento del cancer, composiciones farmaceuticas que los comprenden y proceso para prepararlos.

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AR076007A1
AR076007A1 ARP100101049A ARP100101049A AR076007A1 AR 076007 A1 AR076007 A1 AR 076007A1 AR P100101049 A ARP100101049 A AR P100101049A AR P100101049 A ARP100101049 A AR P100101049A AR 076007 A1 AR076007 A1 AR 076007A1
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group
independently selected
alkyl
heterocyclyl
substituents
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ARP100101049A
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Wolfgang Staehle
Melanie Schultz
Kai Schiemann
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Merck Patent Gmbh
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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
    • C07D401/12—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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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4365—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • 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
    • A61P35/00—Antineoplastic agents
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen 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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    • 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
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    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
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  • Health & Medical Sciences (AREA)
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  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
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  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
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  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

Reivindicacion 1: Compuesto de acuerdo con la formula (1) en donde W1, W2 forman juntos, de modo independiente, -N=N-, -C(O)-O-, -C(O)-S-, -C(O)-N(R5)-, -C(O)-C(R6)(R7)-, -N=C[N(R8)(R9)]-; Y1 está seleccionado, de modo independiente, del grupo que consiste en C(O)-, -C(S)-, -N(R10)-C(O)-, -C(O)-N(R11)-, -C(R12)(R13)-, enlace simple; Y2 está seleccionado, de modo independiente, del grupo que consiste en C(R14)(R15)-, -O-, -N(R16)-, -C(O)-NH-, enlace simple; Z1 está seleccionado, de modo independiente, del grupo que consiste en O, S, N(R17); L está seleccionado, de modo independiente, del grupo que consiste en las formulas (2); B está seleccionado, de modo independiente, del grupo que consiste en cicloalquilo, heterociclilo, arilo, heteroarilo, en donde cicloalquilo, heterociclilo, arilo, heteroarilo pueden estar sustituidos, de modo independiente con uno o varios sustituyentes iguales o diferentes seleccionados del grupo que consiste en: (i) hidrogeno, alquilo, alquilo C9-30, cicloalquilo, cicloalquilalquilo, heterociclilo, heterociclilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, halogeno, -F, -CI, -Br, -I, -CN, -CF3, -N3, -NH2, -NHX1, -NX2X3, -NO2, -OH, -OCF3, -SCF3, -SH, -O-SO3H, -OP(O)(OH)2, -CHO, -COOH, -C(O)NH2, -SO3H, -P(O)(OH)2, -C(O)-X4, -C(O)O-X5, -C(O)NH-X6, -C(O)NX7X8, -O-X9, -O(-X10-O)a-H (a = 1, 2, 3, 4, 5), -O(-X11-O)b-X12 (b = 1, 2, 3, 4, 5), -OC(O)-X13, -OC(O)-O-X1 4, -OC(O)-NHX15, -O-C(O)-NX16X17, -OP(O)(OX18)(OX19), -OSi(X20)(X21)(X22), -OS(O2)-X23, -NHC(O)-NH2, -NHC(O)-X24, -NX25C(O)-X26, -NH-C(O)-O-X27, -NH-C(O)-NH-X28, -NH-C(O)-NX29X30, -NX31-C(O)-O-X32, -NX33-C(O)-NH-X34, -NX35-C(O)-NX36X37, -NHS(O2)-X38, -NX39S(O2)-X40, -S- X41, -S(O)-X42, -S(O2)-X43, -S(O2)NH-X44, -S(O2)NX45X46, -S(O2)O-X47, -P(O)(OX48)(OX49), -Si(X50)(X51)(X52), -C(NH)-NH2, -C(NX53)-NH2, -C(NH)-NHX54, -C(NH)-NX55X56, -C(NX57)-NHX58, -C(NX59)-NX60X61, -NH-C(O)-NH-O-X62, -NH-C(O)-NX63-O-X64, -NX65-C(O)-NX66-O-X67, -N(-C(O)-NH-O-X68)2, -N(-C(O)-NX69-O-X70)2, -N(-C(O)-NH-O-X71)(-C(O)-NX72-O-X73), -C(S)-X74, -C(S)-O-X75, -C(S)-NH-X76, -C(S)-NX77X78, -C(O)-NH-O-X79, -C(O)-NX80-O-X81, -C(S)-NH-O-X82, -C(S)-NX83-O-X84, -C(O)-NH-NH-X85, -C(O)-NH-NX86X87, -C(O)-NX88-NX89X90, -C(S)-NH-NH-X91, -C(S)-NH-NX92X93, -C(S)-NX94-NX95X96, -C(O)-C(O)-O-X97, -C(O)-C(O)-NH2, -C(O)-C(O)-NHX98, -C(O)-C(O)-NX99X100, -C(S)-C(O)-O-X101, -C(O)-C(S)-O-X102, -C(S)-C(S)-O-X103, -C(S)-C(O)-NH2 , -C(S)-C(O)-NHX104, -C(S)-C(O)-NX105X1 06, -C(S)-C(S)-NH2, -C(S)-C(S)-NHX107, -C(S)-C(S)-NX108X109, -C(O)-C(S)-NH2, -C(O)-C(S)-NHX110, -C(O)-C(S)-NX111X112; en donde X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, X12, X13, X14, X15, X16, X17, X18, X19, X20, X21, X22, X23, X24, X25, X26, X27, X28, X29, X30, X31, X32, X33, X34, X35, X36, X37, X38, X39, X40, X41, X42, X43, X44, X45, X46, X47, X48, X49, X50, X51, X52, X53, X54, X55, X56, X57, X58, X59, X60, X61, X62, X63, X64, X65, X66, X67, X68, X69, X70, X71, X72, X73, X74, X75, X76, X77, X78, X79, X80, X81, X82, X83, X84, X85, X86, X87, X88, X89, X90, X91, X92, X93, X94, X95, X96, X97, X98, X99, X100, X101, X102, X103, X104, X105, X106, X107, X108, X109, X110, X111, X112 están seleccionados cada uno, de modo independiente entre sí, del grupo que consiste en alquilo, alquilo C9-30, cicloalquilo, cicloalquilalquilo, heterociclilo, heterociclilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo y en donde alternativamente X7, X8 y/o X16, X17 y/o X29, X30 y/o X36, X37 y/o X45, X46 y/o X55, X56 y/o X60, X61 y/o X77, X78 y/o X86, X87 y/o X89, X90 y/o X92, X93 y/o X95, X96 y/o X99, X100 y/o X105, X106 y/o X108, X109 y/o X111, X112, respectivamente, también pueden formar juntos heterociclilo, en donde opcionalmente los sustituyentes anteriores del grupo de sustituyentes (i) pueden estar sustituidos, a su vez, de modo independiente entre sí, con uno o varios sustituyentes V iguales o diferentes; R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17 están seleccionados cada uno, de modo independiente entre sí, del grupo que consiste en V; V está seleccionado, de modo independiente, del grupo que consiste en (i) ôhidrogeno, alquilo, alquilo C9-30, cicloalquilo, cicloalquilalquilo, heterociclilo, heterociclilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, halogeno, -F, -CI, -Br, -I, -CN, -CF3, -N3, -NH2, -NHA1, -NA2A3, -NO2, -OH, -OCF3, -SCF3, -SH, -O-SO3H, -OP(O)(OH)2, -CHO, -COOH, -C(O)NH2, -SO3H, -P(O)(OH)2, -C(O)-A4, -C(O)O-A5, -C(O)NH-A6, -C(O)NA7A8, -O-A9, -O-(-A10-O)a-H (a = 1, 2, 3, 4, 5), -O(-A11-O)b-A12 (b = 1, 2, 3, 4, 5), -OC(O)-A13, -OC(O)-O-A14, -OC(O)-NHA15, -O-(O)-A16A17, -P(O)(OA18)(OA19),-OSi(A20)(A21)(A22), -OS(O)2-A23, -NHC(O)-NH2, -NHC(O)-A24, -NA25C(O)-A26, -NH-C(O)-O-A27, -NH-C(O)-NH-A28, -NH-C(O)-NA29A30, -NA31-C(O)-O-A32, -NA33-C(O)-NH-A34, -NA35-C(O)-NA36A37, -NHS(O2)-A38, -NA39S(O2)-A40, -S-A41, -S(O)-A42, -S(O2)-A43, -S(O2)NH-A44, -S(O2)NA45A46, -S(O2)O-47, -P(O)(OA48)(OA49), -Si(A50)(A51)(A52), -C(NH)-NH2, -C(NA53)-NH2, -C(NH)-NHA54, -C(NH)-NA55A56, -C(NA57)-NHA58, -C(NA59)- NA60A61, -NH-C(O)-NH-O-A62, -NH-C(O)-NA63-O-A64, -NA65-C(O)-NA66-O-A67, -N(-C(O)-NH-O-A68)2, -N(-C(O)-NA69-O-A70)2, -N(-C(O)-NH-O-A71)(-C(O)-NA72-O-A73), -C(S)-A74, -C(S)-O-A75, -C(S)-NH-A76, -C(S)-NA77A78, -C(O)-NH-O-A79, -C(O)- NA80-O-A81, -C(S)-NH-O-A82, -C(S)-NA83-O-A84, -C(O)-NH-NH-A85, -C(O)-NH-NA86A87, -C(O)-NA88-NA89A90, -C(S)-NH-NH-A91, -C(S)-NH-NA92A93, -C(S)-NA94-NA95A96, -C(O)-C(O)-O-A97, -C(O)-C(O)-NH2, -C(O)-C(O)-NHA98, -C(O)-C(O)-NA99A100, -C(S)-C(O)-O-A101, -C(O)-C(S)-O-A102, -C(S)-C(S)-O-A103, -C(S)- C(O)-NH2, -C(S)-C(O)-NHA104, -C(S)-C(O)-NA105A106, -C(S)-C(S)-NH2, -C(S)-C(S)-NHA107, -C(S)-C(S)-NA108A109, -C(O)-C(S)-NH2, -C(O)-C(S)-NHA110, -C(O)-C(S)-NA111A112; en donde A1, A2, A3, A4, A5, A6, A7, A8, A9, A10, A11, A12, A13, A14, A15, A16, A17, A18, A19, A20, A21, A22, A23, A24, A25, A26, A27, A28, A29, A30, A31, A32, A33, A34, A35, A36, A37, A38, A39, A40, A41, A42, A43, A44, A45, A46, A47, A48, A49, A50, A51, A52, A53, A54, A55, A56, A57, A58, A59, A60, A61, A62, A63, A64, A65, A66, A67, A68, A69, A70, A71, A72, A73, A74, A75, A76, A77, A78, A79, A80, A81, A82, A83, A84, A85, A86, A87, A88, A89, A90, A91, A92, A93, A94, A95, A96, A97, A98, A99, A100, A101, A102, A103, A104, A105, A106, A107, A108, A109, A110, A111, A112 están seleccionados cada uno, de modo independiente entre sí, del grupo que consiste en alquilo, alquilo C9-30, cicloalquilo, cicloalquilalquilo, heterociclilo, heterociclilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo y en donde alternativamente A7, A8 y/o A16, A17 y/o A29, A30 y/o A36, A37 y/o A45, A46 y/o A55, A56 y/o A60, A61 y/o A77, A78 y/o A86, A87 y/o A89, A90 y/o A92, A93 y/o A95, A96 y/o A99, A100 y/o A105, A106 y/o A108, A109 y/o A111, A112, respectivamente, también pueden formar juntos heterociclilo; en donde opcionalmente los sustituyentes anteriores del grupo de sustituyentes (i) pueden estar sustituidos, a su vez, de modo independiente entre sí, con uno o varios sustituyentes V iguales o diferentes; n es, de modo independiente, 0, 1, 2, 3 o 4; y sus sales, derivados, profármacos, solvatos y estereoisomeros fisiologicamente aceptables, incluyendo sus mezclas en todas las proporciones.
ARP100101049A 2009-04-02 2010-03-31 Compuestos heterociclicos inhibidores de autotaxinas utiles para el tratamiento del cancer, composiciones farmaceuticas que los comprenden y proceso para prepararlos. AR076007A1 (es)

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CA2794153C (en) 2010-03-25 2018-01-02 Glaxosmithkline Llc Substituted indoline derivatives as perk inhibitors
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