AR029090A1 - Derivados pirazol triciclicos - Google Patents
Derivados pirazol triciclicosInfo
- Publication number
- AR029090A1 AR029090A1 ARP010102343A ARP010102343A AR029090A1 AR 029090 A1 AR029090 A1 AR 029090A1 AR P010102343 A ARP010102343 A AR P010102343A AR P010102343 A ARP010102343 A AR P010102343A AR 029090 A1 AR029090 A1 AR 029090A1
- Authority
- AR
- Argentina
- Prior art keywords
- optionally substituted
- group
- formula
- phenyl
- cycloalkyl
- Prior art date
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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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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- 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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- 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
- C07D401/06—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 carbon chain containing only aliphatic carbon atoms
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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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- C07D403/10—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 carbon chain containing aromatic rings
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- 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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- C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
- C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
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- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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Abstract
Un compuesto derivado de pirazol tricíclico que está representado por la formula 1 las mezclas racémicas, las mezclas racémico-diastereoméricas, tautomeros e isomeros opticos de compuestos y las sales farmacéuticamente aceptables y las prodrogas de los mismos, en donde: m es un entero de 1 a 10; X representa a) un grupo opcionalmente sustituido de la formula -(CH2)n - en donde n es 1, 2, o 3, b) carbonilo, c) oxígeno, d) un grupo de la formula -C=NOR10, en donde R10 es un grupo alquilo C1-4, e) un grupo de la formula NR11 en donde R11 es -H, un grupo alquilo C1-4 opcionalmente sustituido, o un fenilo opcionalmente sustituido, o f) un grupo de formula S(O)p en donde p es de valor 0, 1 o 2; B representa un alquilo, un cicloalquilo, un arilo, un piridilo, un tienilo, un furilo o un pirrolilo; R1 es -H; un halo; hidroxilo, nitro, ciano, hidroxiamidino; aminometilo; formamidometilo; un alqueniloxilo opcionalmente sustituido; un alquenilo C2-4 opcionalmente sustituido; un alquinilo C2-4 opcionalmente sustituido; o un grupo representado por la formula -Y-W; con la condicion que cuando R1 es -H, un alquilo C1-6 sin sustituir, un alcoxilo C1-6 sin sustituir, un halogeno, o trifluorometilo, el anillo A se sustituye con por lo menos un sustituyente que no es un halo, un alquilo C1-6 opcionalmente sustituido o un alcoxilo C1-6 opcionalmente sustituido; Y no está o es un alquilo C1-6, alcoxilo C1-6, -O-, -S- o -C(O) -; W es -H, hidroxilo, fenilo opcionalmente sustituido, alcoxilo C1-6, o -NR2R3; con la condicion que cuando el B es fenilo y R1 es Y-W y W es -NR2R3, R2 y R3 son cada uno, independientemente, a) -H; b) un grupo alquilo C1-6 sustituido, con la condicion que el sustituyente no es -NR6R7; c) un cicloalquilo opcionalmente sustituido; d) un heterocicloalquilo opcionalmente sustituido; e) un cicloalquilo opcionalmente sustituido; f) un heterocicloalquilalquilo opcionalmente sustituido; g) un heteroarilo sustituido o un heteroaralquilo sustituido, con la condicion que el heteroarilo o heteroaralquilo se sustituye con -NR9(CH2)1-6OR4, -NR9(CH2)1-6 CO2R4, -NR9(CH2)1-6NR4R5, o un heterocicloalquilo opcionalmente sustituido; o cuando B es fenilo y R1 es -Y-W y W es -NR2R3, R2 y R3, junto con el átomo de nitrogeno a cual éstos están unidos, puede representar un heterocicloalquilo opcionalmente sustituido o un heteroarilo opcionalmente sustituido; cuando el B no es fenilo, R2 y R3 son cada uno, independientemente, -H, un grupo alquilo C1-6 opcionalmente sustituido, -NH(CH2)1-6NR4R5, un cicloalquilo opcionalmente sustituido, un heterocicloalquilo opcionalmente sustituido, un arilo opcionalmente sustituido, un heteroarilo opcionalmente sustituido, un cicloalquilalquilo opcionalmente sustituido, un heterocicloalquilalquilo opcionalmente sustituido, un aralquilo opcionalmente sustituido, o un heteroaralquilo opcionalmente sustituido; o cuando el B no es fenilo, R2 y R3 junto con el átomo de nitrogeno al cual los mismos están unidos representa un heterocicloalquilo opcionalmente sustituido o un heteroarilo opcionalmente sustituido; R4, R5 y R9 son en cada caso, independientemente, -H o un alquilo C1-6; y el anillo A se sustituye opcionalmente con uno o más sustituyentes seleccionados del grupo que consiste de a) un halo; b) un grupo alquilo C1-6 opcionalmente sustituido con uno o más sustituyentes seleccionados del grupo que consiste de hidroxilo, halo, y NR6R7; c) un grupo alcoxilo C1-6 opcionalmente sustituido con uno o más sustituyentes seleccionado del grupo que consiste de hidroxilo, halo, -NR6R7, un fenilo opcionalmente sustituido, y -NR17C(O)R19, con la condicion que los sustituyentes no están unidos al carbono a que se une el oxígeno del grupo alcoxilo; d) un fenoxilo opcionalmente sustituido; e) hidroxilo; f) un grupo de la formula -C (O) R12 en donde R12 es hidroxilo, un alcoxilo C1-6 o -NR13R14; g) un grupo de la formula NR17R18; h) un grupo de la formula -NR17C(O)R19; i) nitro; j) aralquilo opcionalmente sustituido; k) ciano; y l) un grupo alquenilo C2-4 o un grupo alquinilo C2-4 cada uno de los cuales es opcionalmente sustituido con uno o más sustituyentes seleccionados del grupo que consiste de un grupo alquilo C1-6, un grupo alcoxilo C1-6 y un halo; R6 y R7 son cada uno, independientemente, -H, un grupo alquilo C1-6 opcionalmente sustituido, un cicloalquilo opcionalmente sustituido, un arilo opcionalmente sustituidos, un heteroarilo opcionalmente sustituido, un heterocicloalquilo opcionalmente sustituido, un cicloalquilalquilo opcionalmente sustituido, un aralquilo opcionalmente sustituido, un heteroaralquilo opcionalmente sustituido, o un heterocicloalquilalquilo opcionalmente sustituido; o R6 y R7 junto con el átomo de nitrogeno al cual éstos están unidos representan un heterocicloalquilo opcionalmente sustituido o un heteroarilo opcionalmente sustituido, R13 y R14 son cada uno, independientemente, -H, un grupo alquilo C1-6 opcionalmente sustituido, un cicloalquilo opcionalmente sustituido, un arilo opcionalmente sustituidos, un heteroarilo opcionalmente sustituido, un heterocicloalquilo opcionalmente sustituido, un cicloalquilalquilo opcionalmente sustituido, un aralquilo opcionalmente sustituido, un heteroaralquilo opcionalmente sustituido, o un heterocicloalquilalquilo opcionalmente sustituido; o R13 y R14 junto con el átomo de nitrogeno al cual éstos están unidos representan un heterocicloalquilo opcionalmente sustituido o un heteroarilo opcionalmente sustituido; R17 y R18 son cada uno, independientemente, seleccionado del grupo que consiste de -H, un grupo alquilo C1-2, un grupo cicloalquilo C3-12, y fenilo; y R19 es -H, un grupo alquilo C1-12 opcionalmente sustituido, un grupo cicloalquilo C3-12 opcionalmente sustituido, un fenilo opcionalmente sustituido o un aralquilo opcionalmente sustituido. Con la condicion que, cuando B es arilo, piridilo, tienilo, furilo o pirrolilo, entonces el anillo A es sustituido con por lo menos un sustituyente seleccionado del grupo que consiste del grupo alquilo C1-6 que es sustituido con -NR6'R7'; un alcoxilo C1-6 que es sustituido con un grupo de la formula -NR17C(O)R19 o fenilo opcionalmente sustituido; y un grupo de la formula C(O)NR13'R14'. R6' y R7' son cada uno, independientemente, -H, un cicloalquilo opcionalmente sustituido, un arilo opcionalmente sustituido, un heteroarilo opcionalmente sustituido, un heterocicloalquilo opcionalmente sustituido, un cicloalquilalquilo opcionalmente sustituido, un aralquilo opcionalmente sustituido, un heteroalquilo opcionalmente sustituido, o un heterocicloalquilalquilo opcionalmente sustituido, con la condicion que por lo menos uno de R6' y R7' no sea -H; y R13' y R14' son cada uno, independientemente, -H, un cicloalquilo opcionalmente sustituido, un naftilo opcionalmente sustituido, un heteroarilo opcionalmente sustituido, un heterocicloalquilo opcionalmente sustituido, un cicloalquilalquilo opcionalmente sustituido, un aralquilo opcionalmente sustituido, un heteroaralquilo opcionalmente sustituido, o un heterocicloalquilalquilo opcionalmente sustituido, con la condicion que por lo menos uno de R13' p R14' no sea -H. Estos compuestos son de utilidad para inhibir la actividad de quinasa de quinasas tirosinas y quinasas serina/treonina.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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US09/573,366 US6462036B1 (en) | 1998-11-06 | 2000-05-17 | Tricyclic pyrazole derivatives |
Publications (1)
Publication Number | Publication Date |
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AR029090A1 true AR029090A1 (es) | 2003-06-04 |
Family
ID=24291696
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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ARP010102343A AR029090A1 (es) | 2000-05-17 | 2001-05-17 | Derivados pirazol triciclicos |
Country Status (11)
Country | Link |
---|---|
US (1) | US6462036B1 (es) |
EP (1) | EP1289525A2 (es) |
JP (1) | JP2003533514A (es) |
AR (1) | AR029090A1 (es) |
AU (1) | AU2001263272A1 (es) |
CA (1) | CA2409225A1 (es) |
CO (1) | CO5290256A1 (es) |
MX (1) | MXPA02011320A (es) |
PE (1) | PE20011263A1 (es) |
UY (1) | UY26713A1 (es) |
WO (1) | WO2001087846A2 (es) |
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CZ20011563A3 (cs) | 1998-11-06 | 2003-02-12 | Basf Aktiengesellschaft | Tricyklické pyrazolové deriváty |
CN1368970A (zh) | 1999-04-06 | 2002-09-11 | 克诺尔股份有限公司 | 作为酪氨酸激酶抑制剂的取代的1,4-二氢茚并[1,2-c]吡唑 |
-
2000
- 2000-05-17 US US09/573,366 patent/US6462036B1/en not_active Expired - Lifetime
-
2001
- 2001-05-17 PE PE2001000440A patent/PE20011263A1/es not_active Application Discontinuation
- 2001-05-17 JP JP2001584242A patent/JP2003533514A/ja not_active Withdrawn
- 2001-05-17 CO CO01039467A patent/CO5290256A1/es not_active Application Discontinuation
- 2001-05-17 AR ARP010102343A patent/AR029090A1/es unknown
- 2001-05-17 UY UY26713A patent/UY26713A1/es not_active Application Discontinuation
- 2001-05-17 WO PCT/US2001/016153 patent/WO2001087846A2/en not_active Application Discontinuation
- 2001-05-17 CA CA002409225A patent/CA2409225A1/en not_active Abandoned
- 2001-05-17 AU AU2001263272A patent/AU2001263272A1/en not_active Abandoned
- 2001-05-17 MX MXPA02011320A patent/MXPA02011320A/es unknown
- 2001-05-17 EP EP01937553A patent/EP1289525A2/en not_active Withdrawn
Also Published As
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UY26713A1 (es) | 2001-12-28 |
WO2001087846A3 (en) | 2002-03-21 |
WO2001087846A2 (en) | 2001-11-22 |
AU2001263272A1 (en) | 2001-11-26 |
MXPA02011320A (es) | 2004-09-10 |
CO5290256A1 (es) | 2003-06-27 |
JP2003533514A (ja) | 2003-11-11 |
US6462036B1 (en) | 2002-10-08 |
PE20011263A1 (es) | 2001-12-11 |
CA2409225A1 (en) | 2001-11-22 |
EP1289525A2 (en) | 2003-03-12 |
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