ES2547124T3 - Inhibidores de autotaxina - Google Patents

Inhibidores de autotaxina Download PDF

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ES2547124T3
ES2547124T3 ES10707839T ES10707839T ES2547124T3 ES 2547124 T3 ES2547124 T3 ES 2547124T3 ES 10707839 T ES10707839 T ES 10707839T ES 10707839 T ES10707839 T ES 10707839T ES 2547124 T3 ES2547124 T3 ES 2547124T3
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Melanie Schultz
Kai Schiemann
Wolfgang Staehle
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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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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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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    • A61P25/00—Drugs for disorders of the nervous system
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P27/02—Ophthalmic agents
    • 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
    • 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
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—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
    • 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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    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • 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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  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
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  • Ophthalmology & Optometry (AREA)
  • Dermatology (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Compuesto según la fórmula (I)**Fórmula** donde: W1, W2 juntos forman independientemente "-N>=N-, -C(O)-O--; Y1 se selecciona independientemente a partir del grupo compuesto por "-C(O)-, -C(S)-, -N(R10)-C(O)-, -C(O)-N(R11)-, -C(R12)(R13)- y enlace sencillo-; Y2 se selecciona independientemente a partir del grupo compuesto por "-C(R14)(R15)-, -O-, -N(R16)-, -C(O)-NH- y enlace sencillo-; Z1 se selecciona independientemente a partir del grupo compuesto por "O, S y N(R17)"; L se selecciona independientemente a partir del grupo compuesto por:**Fórmula** B se selecciona independientemente a partir del grupo compuesto por "arilo", en donde el "arilo" pueden estar sustituidos independientemente con uno o más sustituyentes idénticos o diferentes seleccionados a partir del grupo compuesto por: (i) "hidrógeno, alquilo, alquilo (C9-C30), cicloalquilo, cicloalquilalquilo, heterociclilo, heterociclilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, halógeno, -F, -Cl, -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-X14, -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, 10 -C(S)-C(O)-NX105X106, -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 y -C(O)-C(S)-NX111X112-; 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, 15 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 y X112 se seleccionan independientemente entre sí a partir del grupo compuesto por: "alquilo, alquilo (C9-C30), cicloalquilo, cicloalquilalquilo, heterociclilo, heterociclilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo" y 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, juntos también pueden formar un "heterociclilo"; donde, opcionalmente, los sustituyentes anteriores del grupo de sustituyentes (i) pueden estar sustituidos a su vez independientemente entre sí con uno o más sustituyentes V idénticos o diferentes R1, R2, R3, R4, R10, R11, R12, R13, R14, R15, R16 y R17 se seleccionan independientemente entre sí a partir del grupo compuesto por: "V";
ES10707839T 2009-04-02 2010-03-09 Inhibidores de autotaxina Active ES2547124T3 (es)

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EP09004866 2009-04-02
EP09004866 2009-04-02
PCT/EP2010/001457 WO2010112124A1 (en) 2009-04-02 2010-03-09 Autotaxin inhibitors

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US (2) US8329907B2 (es)
EP (1) EP2414346B1 (es)
JP (1) JP5779172B2 (es)
KR (1) KR20120004483A (es)
CN (1) CN102369195B (es)
AR (1) AR076007A1 (es)
AU (1) AU2010230585B2 (es)
CA (1) CA2757415C (es)
EA (1) EA201101396A1 (es)
ES (1) ES2547124T3 (es)
IL (1) IL215259A (es)
MX (1) MX2011010218A (es)
SG (1) SG174518A1 (es)
WO (1) WO2010112124A1 (es)

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