AR076076A1 - FUSIONED BICYCLIC AND HETEROCICLIC COMPOUNDS, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, PROCEDURE TO PREPARE THEM, AND USE OF THEM IN THE TREATMENT OF INFLAMMATORY AND / OR AUTOIMMUNE DISEASES - Google Patents

FUSIONED BICYCLIC AND HETEROCICLIC COMPOUNDS, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, PROCEDURE TO PREPARE THEM, AND USE OF THEM IN THE TREATMENT OF INFLAMMATORY AND / OR AUTOIMMUNE DISEASES

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AR076076A1
AR076076A1 ARP100100635A ARP100100635A AR076076A1 AR 076076 A1 AR076076 A1 AR 076076A1 AR P100100635 A ARP100100635 A AR P100100635A AR P100100635 A ARP100100635 A AR P100100635A AR 076076 A1 AR076076 A1 AR 076076A1
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indicates
atoms
het1
cycloalkyl
hal
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ARP100100635A
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Merck Serono Sa
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/68—Benzothiazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • C07D277/82—Nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D419/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms
    • C07D419/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D419/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur 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
    • 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
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
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  • Animal Behavior & Ethology (AREA)
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Abstract

Compuestos de formula (1) para la regulacion de la actividad de las PI3K y enfermedades relacionadas. Reivindicacion 1: Un compuesto de acuerdo con la formula (1), en donde - - - - - indica un enlace simple o un enlace doble; U indica CRc, CH, o S; V indica C o N; W indica N o CR1; X indica CO, SO, SO2, CS o un enlace; Y indica CR2 o N; Ra indica NH-Ab, NA2, NH(CH2)p-Ab, -NH-(CH2)p-Ar, -NH(CH2)p-Het4, -NH-(CH2)pCHOR6-Het1, -NH-(CH2)pCOAr, -NH-(CH2)pCOHet1, -NH-cicloalquilo, COHet1, o un resto del grupo de formulas (2), o si X indica un enlace, también CO-N(H)2-m(A)m, CO, CS, o si X indica CO, SO, SO2, CS, también H, o si V indica C, también Ar o Het1, o si Rb es Ar, Het3, o uno de los restos del grupo de formulas (3), Ra también indica A, -(CH2)s-Ar, -(CH2)s-Het1, Het1, Het4, o perfluoroalquilo, o si Rb indica Ar, Ra es también -OA o cicloalquilo; Rb indica Ar, Het2, Het3 o un resto del grupo de formulas (3); R', R'' son independientemente hidrogeno, alquilo, Ar, Het1, Het2 o A; R' y R'' juntamente con el átomo de nitrogeno al que se encuentran fijados, pueden opcionalmente formar un anillo heterocíclico de 3-8 miembros; Rc indica H, A, alquilo, Ar, Het1; Ar indica un anillo carbocíclico aromático monocíclico o bicíclico que posee 6 a 14 átomos de carbono, que es insustituido o monosustituido, disustituido o trisustituido por, Hal, CF3, OCF3, NO2, CN, perfluoroalquilo, A, OA, OH, NH2, COH, CONH2, -NHCOA, -NHCO2A, NHCO2(CH2)sHet1, -(CH2)pHet1, -NHSO2A, -NHSO2-N(H)2-m(A)m, N(H)1-qAqCOA, N(H)1-qASO2N(H)2-m(A)m, N(H)1-qAqCON(H)2-m(A)m, COOA, COA, -SO2A, -SO2N(H)2-m(A)m, -SO2Het1, -SO2NHHet1, Het1, -NHSO2NHHet1, o cicloalquilo; Het1 indica un anillo monocíclico o bicíclico saturado o insaturado o aromático heterocíclico que posee 1 a 4 átomos N, O y/o S y/o 1 grupo CO, que es insustituido o monosustituido, disustituido o trisustituido por alquilo con 1 a 8 átomos de carbono, alcoxi con 1 a 8 átomos de carbono, Hal, CF3, OCF3, NO2, CN, perfluoroalquilo, A, OA, O(CH2)sAr, O(CH2)sHet1, -(CH2)pHet2, OH, amino, CONH2, NHCOA, -NHCO2A, -NHCO2(CH2)sAr, -NHSO2-N(H)2-m(A)m, COA, COOA, -SO2A, -SO2N(H)2-m(A)m, -SO2Het2, -SO2NHHet2, -NHSO2NHHet2, Ar, -NHSO2NHAr, -SO2NHAr, SO2Ar, cicloalquilo; Het2 indica un anillo monocíclico o bicíclico saturado, insaturado o aromático heterocíclico que posee 1 a 4 átomos N, O y/o S y/o 1 grupo CO, que es insustituido o monosustituido, disustituido o trisustituido por alquilo con 1 a 8 átomos de carbono, alcoxi con 1 a 8 átomos de carbono, Hal, CF3, OCF3, NO2, CN, perfluoroalquilo, A, OA, O(CH2)sAr, O(CH2)sHet1, -(CH2)pHet1, OH, NA2, CONH2, -NHCOA, -NHCO2A, -NHCO2(CH2)sHet1, -NHCO2(CH2)sAr, -NHSO2-N(H)2-m(A)m, COA, COOA, -SO2A, -SO2N(H)2-m(A)m, -SO2Het1, SO2NHHet2, Ar, SO2Ar, o cicloalquilo; Het3 indica un anillo monocíclico saturado, insaturado o aromático heterocíclico que posee 1 a 4 átomos N, O y/o S y/o 1 grupo CO, que es insustituido o monosustituido, disustituido o trisustituido por NO2, CN, perfluoroalquilo, OH, CONH2, -NHCOA, -NHCO2A, -NHCO2(CH2)sHet1, -NHCO2(CH2)sAr, -NHSO2A, -NHSO2-N(H)2-m(A)m, COA, COOA, -COH, -SO2A, SO2N(H)2-m(A)m, -SO2Het1, SO2NHHet2, o cicloalquilo o Het3 indica uno de los restos del grupo de formulas (4); Het4 indica un anillo monocíclico o bicíclico insaturado o aromático heterocíclico que posee 1 a 4 átomos N, O y/o S y/o 1 grupo CO, que es insustituido o monosustituido, disustituido o trisustituido por alquilo con 1 a 8 átomos de carbono, alcoxi con 1 a 8 átomos de carbono, Hal, CF3, OCF3, NO2, CN, perfluoroalquilo, A, OA, O(CH2)sAr, O(CH2)sHet1, -(CH2)pHet2, OH, amino, CONH2, -NHCOA, -NHCO2A, -NHCO2(CH2)sAr, -NHSO2-N(H)2-m(A)m, COA, COOA, -SO2A, -SO2N(H)2-m(A)m, -SO2Het2, -SO2NHHet2, NHSO2NHHet2, Ar, -NHSO2NHAr, -SO2NHAr, SO2Ar, cicloalquilo o Het4 indica uno de los restos del grupo de formulas (5); m indica 0, 1 o 2; n indica 1, 2, 3 o 4; p indica 0, 1, 2, 3, 4; q indica 0 o 1; s indica 1, 2, 3, 4; A es un alquilo ramificado o lineal que posee 1 a 12 átomos de carbono, en donde uno o más, preferentemente 1 a 7 átomos H pueden ser reemplazados por Hal, Ar, Het1, Het2, OR6, CN, NHCO, CONR'R'', COOR6 o NR'R'' y en donde uno o más, preferentemente 1 a 7 grupos CH2 no adyacentes pueden ser reemplazados por O, NR6 o S y/o por grupos -CH=CH- o -CsC-, o indica cicloalquilo, cicloalqueno o cicloalquilalquileno que posee 3-7 átomos de C de anillo en donde el cicloalquileno es opcionalmente sustituido por 1 o 2 grupos OH; Ab es un alquilo ramificado o lineal que posee 1 a 12 átomos de carbono, en donde uno o más, preferentemente 1 a 7 átomos H pueden ser reemplazados por Hal, Ar, OR6, CN, NHCO, CONR'R'', COOR6 o NR'R'' y en donde uno o más, preferentemente 1 a 7 grupos CH2 no adyacentes pueden ser reemplazados por grupos O, NR6 o S y/o por -CH=CH- o -CsC-, o indica cicloalquilo, cicloalqueno o cicloalquilalquileno que posee 3-7 átomos de C de anillo en donde el cicloalquileno es opcionalmente sustituido por 1 o 2 grupos OH; R1, R2 son cada uno independientemente H, Hal, CF3, A, Ar, Het1 o Het2; R3 es H o Hal; R', R'' denotan cada uno independientemente H, Ar, Het1, Het2, o A, y di R' o R'' se une a un átomo C también OA; R6 es H, un alquilo ramificado o lineal o hidroxialquilo que posee 1 a 12 átomos de carbono; y derivados, solvatos, tautomeros, sales y sus estereoisomeros farmacéuticamente aceptables, con inclusion de sus mezclas en todas las relaciones.Compounds of formula (1) for the regulation of the activity of PI3K and related diseases. Claim 1: A compound according to formula (1), wherein - - - - - indicates a single bond or a double bond; U indicates CRc, CH, or S; V indicates C or N; W indicates N or CR1; X indicates CO, SO, SO2, CS or a link; Y indicates CR2 or N; Ra indicates NH-Ab, NA2, NH (CH2) p-Ab, -NH- (CH2) p-Ar, -NH (CH2) p-Het4, -NH- (CH2) pCHOR6-Het1, -NH- (CH2 ) pCOAr, -NH- (CH2) pCOHet1, -NH-cycloalkyl, COHet1, or a remainder of the group of formulas (2), or if X indicates a bond, also CO-N (H) 2-m (A) m , CO, CS, or if X indicates CO, SO, SO2, CS, also H, or if V indicates C, also Ar or Het1, or if Rb is Ar, Het3, or one of the remains of the formula group (3 ), Ra also indicates A, - (CH2) s-Ar, - (CH2) s-Het1, Het1, Het4, or perfluoroalkyl, or if Rb indicates Ar, Ra is also -OA or cycloalkyl; Rb indicates Ar, Het2, Het3 or a remainder of the group of formulas (3); R ', R' 'are independently hydrogen, alkyl, Ar, Het1, Het2 or A; R 'and R' 'together with the nitrogen atom to which they are attached, can optionally form a 3-8 membered heterocyclic ring; Rc indicates H, A, alkyl, Ar, Het1; Ar indicates a monocyclic or bicyclic aromatic carbocyclic ring having 6 to 14 carbon atoms, which is unsubstituted or monosubstituted, disubstituted or trisubstituted by, Hal, CF3, OCF3, NO2, CN, perfluoroalkyl, A, OA, OH, NH2, COH , CONH2, -NHCOA, -NHCO2A, NHCO2 (CH2) sHet1, - (CH2) pHet1, -NHSO2A, -NHSO2-N (H) 2-m (A) m, N (H) 1-qAqCOA, N (H ) 1-qASO2N (H) 2-m (A) m, N (H) 1-qAqCON (H) 2-m (A) m, COOA, COA, -SO2A, -SO2N (H) 2-m (A ) m, -SO2Het1, -SO2NHHet1, Het1, -NHSO2NHHet1, or cycloalkyl; Het1 indicates a saturated or unsaturated monocyclic or bicyclic or heterocyclic aromatic ring having 1 to 4 N, O and / or S atoms and / or 1 CO group, which is unsubstituted or monosubstituted, disubstituted or trisubstituted by alkyl with 1 to 8 atoms of carbon, alkoxy with 1 to 8 carbon atoms, Hal, CF3, OCF3, NO2, CN, perfluoroalkyl, A, OA, O (CH2) sAr, O (CH2) sHet1, - (CH2) pHet2, OH, amino, CONH2 , NHCOA, -NHCO2A, -NHCO2 (CH2) sAr, -NHSO2-N (H) 2-m (A) m, COA, COOA, -SO2A, -SO2N (H) 2-m (A) m, -SO2Het2 , -SO2NHHet2, -NHSO2NHHet2, Ar, -NHSO2NHAr, -SO2NHAr, SO2Ar, cycloalkyl; Het2 indicates a saturated, unsaturated or aromatic heterocyclic monocyclic or bicyclic ring having 1 to 4 N, O and / or S atoms and / or 1 CO group, which is unsubstituted or monosubstituted, disubstituted or trisubstituted by alkyl with 1 to 8 atoms of carbon, alkoxy with 1 to 8 carbon atoms, Hal, CF3, OCF3, NO2, CN, perfluoroalkyl, A, OA, O (CH2) sAr, O (CH2) sHet1, - (CH2) pHet1, OH, NA2, CONH2 , -NHCOA, -NHCO2A, -NHCO2 (CH2) sHet1, -NHCO2 (CH2) sAr, -NHSO2-N (H) 2-m (A) m, COA, COOA, -SO2A, -SO2N (H) 2- m (A) m, -SO2Het1, SO2NHHet2, Ar, SO2Ar, or cycloalkyl; Het3 indicates a saturated, unsaturated or aromatic heterocyclic monocyclic ring having 1 to 4 N, O and / or S atoms and / or 1 CO group, which is unsubstituted or monosubstituted, disubstituted or trisubstituted by NO2, CN, perfluoroalkyl, OH, CONH2 , -NHCOA, -NHCO2A, -NHCO2 (CH2) sHet1, -NHCO2 (CH2) sAr, -NHSO2A, -NHSO2-N (H) 2-m (A) m, COA, COOA, -COH, -SO2A, SO2N (H) 2-m (A) m, -SO2Het1, SO2NHHet2, or cycloalkyl or Het3 indicates one of the moieties of the group of formulas (4); Het4 indicates an unsaturated monocyclic or bicyclic or heterocyclic aromatic ring having 1 to 4 N, O and / or S atoms and / or 1 CO group, which is unsubstituted or monosubstituted, disubstituted or trisubstituted by alkyl with 1 to 8 carbon atoms, alkoxy with 1 to 8 carbon atoms, Hal, CF3, OCF3, NO2, CN, perfluoroalkyl, A, OA, O (CH2) sAr, O (CH2) sHet1, - (CH2) pHet2, OH, amino, CONH2, - NHCOA, -NHCO2A, -NHCO2 (CH2) sAr, -NHSO2-N (H) 2-m (A) m, COA, COOA, -SO2A, -SO2N (H) 2-m (A) m, -SO2Het2, -SO2NHHet2, NHSO2NHHet2, Ar, -NHSO2NHAr, -SO2NHAr, SO2Ar, cycloalkyl or Het4 indicates one of the remains of the formula group (5); m indicates 0, 1 or 2; n indicates 1, 2, 3 or 4; p indicates 0, 1, 2, 3, 4; q indicates 0 or 1; s indicates 1, 2, 3, 4; A is a branched or linear alkyl having 1 to 12 carbon atoms, wherein one or more, preferably 1 to 7 H atoms can be replaced by Hal, Ar, Het1, Het2, OR6, CN, NHCO, CONR'R ' ', COOR6 or NR'R' 'and where one or more, preferably 1 to 7 non-adjacent CH2 groups can be replaced by O, NR6 or S and / or by groups -CH = CH- or -CsC-, or indicates cycloalkyl, cycloalkene or cycloalkylalkylene having 3-7 ring C atoms wherein the cycloalkylene is optionally substituted by 1 or 2 OH groups; Ab is a branched or linear alkyl having 1 to 12 carbon atoms, wherein one or more, preferably 1 to 7 H atoms, can be replaced by Hal, Ar, OR6, CN, NHCO, CONR'R '', COOR6 or NR'R '' and wherein one or more, preferably 1 to 7 non-adjacent CH2 groups can be replaced by O, NR6 or S groups and / or by -CH = CH- or -CsC-, or indicates cycloalkyl, cycloalkene or cycloalkylalkylene having 3-7 ring C atoms wherein the cycloalkylene is optionally substituted by 1 or 2 OH groups; R1, R2 are each independently H, Hal, CF3, A, Ar, Het1 or Het2; R3 is H or Hal; R ', R' 'each independently denotes H, Ar, Het1, Het2, or A, and di R' or R '' is attached to a C atom also OA; R6 is H, a branched or linear alkyl or hydroxyalkyl having 1 to 12 carbon atoms; and derivatives, solvates, tautomers, salts and their pharmaceutically acceptable stereoisomers, including their mixtures in all relationships.

ARP100100635A 2009-03-04 2010-03-03 FUSIONED BICYCLIC AND HETEROCICLIC COMPOUNDS, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, PROCEDURE TO PREPARE THEM, AND USE OF THEM IN THE TREATMENT OF INFLAMMATORY AND / OR AUTOIMMUNE DISEASES AR076076A1 (en)

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