AR051788A1 - Derivados 2,4 (4,6) pirimidina como inhibidores de quinasa - Google Patents
Derivados 2,4 (4,6) pirimidina como inhibidores de quinasaInfo
- Publication number
- AR051788A1 AR051788A1 ARP050105123A ARP050105123A AR051788A1 AR 051788 A1 AR051788 A1 AR 051788A1 AR P050105123 A ARP050105123 A AR P050105123A AR P050105123 A ARP050105123 A AR P050105123A AR 051788 A1 AR051788 A1 AR 051788A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- mono
- optionally substituted
- hydroxy
- amino
- Prior art date
Links
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- -1 C1-4 alkyl sulfide Chemical compound 0.000 abstract 37
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 16
- 125000001424 substituent group Chemical group 0.000 abstract 13
- 125000000217 alkyl group Chemical group 0.000 abstract 12
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 12
- 229910052739 hydrogen Inorganic materials 0.000 abstract 12
- 239000001257 hydrogen Substances 0.000 abstract 12
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 12
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 11
- 125000001475 halogen functional group Chemical group 0.000 abstract 10
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 10
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 9
- 125000006526 (C1-C2) alkyl group Chemical group 0.000 abstract 8
- 125000000623 heterocyclic group Chemical group 0.000 abstract 8
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 8
- 125000003545 alkoxy group Chemical group 0.000 abstract 7
- 125000004193 piperazinyl group Chemical group 0.000 abstract 7
- 125000003386 piperidinyl group Chemical group 0.000 abstract 7
- 125000004076 pyridyl group Chemical group 0.000 abstract 7
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 6
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract 6
- QMMFVYPAHWMCMS-UHFFFAOYSA-N Dimethyl sulfide Chemical compound CSC QMMFVYPAHWMCMS-UHFFFAOYSA-N 0.000 abstract 6
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 abstract 6
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 6
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 6
- 125000002795 guanidino group Chemical group C(N)(=N)N* 0.000 abstract 6
- 125000001041 indolyl group Chemical group 0.000 abstract 6
- 125000003396 thiol group Chemical class [H]S* 0.000 abstract 6
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 5
- ORTFAQDWJHRMNX-UHFFFAOYSA-N hydroxidooxidocarbon(.) Chemical group O[C]=O ORTFAQDWJHRMNX-UHFFFAOYSA-N 0.000 abstract 5
- 125000004464 hydroxyphenyl group Chemical group 0.000 abstract 5
- 125000001544 thienyl group Chemical group 0.000 abstract 4
- 125000004466 alkoxycarbonylamino group Chemical group 0.000 abstract 3
- 125000004448 alkyl carbonyl group Chemical group 0.000 abstract 3
- 125000004472 dialkylaminosulfonyl group Chemical group 0.000 abstract 3
- 125000002757 morpholinyl group Chemical group 0.000 abstract 3
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 abstract 2
- 101100070530 Neurospora crassa (strain ATCC 24698 / 74-OR23-1A / CBS 708.71 / DSM 1257 / FGSC 987) het-6 gene Proteins 0.000 abstract 2
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 2
- 125000000304 alkynyl group Chemical group 0.000 abstract 2
- 125000000000 cycloalkoxy group Chemical group 0.000 abstract 2
- 125000004856 decahydroquinolinyl group Chemical group N1(CCCC2CCCCC12)* 0.000 abstract 2
- 125000005879 dioxolanyl group Chemical group 0.000 abstract 2
- 125000002541 furyl group Chemical group 0.000 abstract 2
- 125000002883 imidazolyl group Chemical group 0.000 abstract 2
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 abstract 2
- 125000000842 isoxazolyl group Chemical group 0.000 abstract 2
- 125000001715 oxadiazolyl group Chemical group 0.000 abstract 2
- 125000002971 oxazolyl group Chemical group 0.000 abstract 2
- 125000003226 pyrazolyl group Chemical group 0.000 abstract 2
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 abstract 2
- 125000000335 thiazolyl group Chemical group 0.000 abstract 2
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 abstract 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 1
- 125000000815 N-oxide group Chemical group 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000005360 alkyl sulfoxide group Chemical group 0.000 abstract 1
- 125000002393 azetidinyl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000005265 dialkylamine group Chemical group 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 125000000168 pyrrolyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- 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
- C07D487/12—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 three hetero rings
- C07D487/18—Bridged systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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
- A61K31/495—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
- 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
- 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
- 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
- C07D487/08—Bridged 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
- C07D487/22—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 four or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/18—Bridged systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Saccharide Compounds (AREA)
Abstract
Reivindicacion 1: Un compuesto que tiene la formula (1), las formas de N-oxido, las sales de adicion farmacéuticamente aceptables y las formas isoméricas de las mismas, donde: Z1 y Z2, cada una independientemente representa NR22; en particular Z1 y Z2 representa NH; Y representa -alquiloC3-9-; -alqueniloC3-9-; -alquiniloC3-9-; alquiloC3-7-CO-NH- opcionalmente sustituido con amino, mono- o dialquilamino C1-4, aminosulfonilo, mono- o dialquilaminosulfonilo C1-4, sulfuro de alquilo C1-4, sulfoxido de alquilo C1-4, sulfuro de alquilo C1-4, o alquiloxicarbonilaminoC1-4-; -alqueniloC3-7-CO-NH- opcionalmente sustituido con amino, mono- o -dialquilamino C1-4, aminosulfonilo, mono- o dialquilaminosulfonilo C1-4, sulfuro de alquilo C1-4, sulfoxido de alquilo C1-4, sulfuro de alquilo C1-4 o alquiloxicarbonilaminoC1-4-; -alquiniloC3-7-CO-NH- opcionalmente sustituido con amino, mono- o dialquilamino C1-4, aminosulfonilo, mono- o dialquilamino C1-4, aminosulfonilo, mono dialquilamino C1- 4, sulfuro de alquilo C1-4 o sulfoxido de alquilo C1-4, sulfuro de alquilo C1-4, alquiloxicarbonilaminoC1-4-; -alquiloxiC1-5-alquiloC1-5-; -alquiloC1-5-NR6-alquiloC1-5-; -alquiloC1-5-NR7-CO-alquiloC1-5-; -alquiloC1-6-CO-NH-; -alquiloC1-6-NH-CO-; alquiloC1-3-NH-CS-Het9-; -alquiloC1-3-NH-CO-Het3-; alquiloC1-7-CO-Het10-CO-; -Het4-alquiloC1-3-CO-NH-alquiloC1-3-; -alquiloC1-7-CO-; -alquiloC1-6-CO-alquiloC1-6-; -alquiloC1-2-NH-CO-L1-NH-; -NH-CO-L2-NH-; -alquiloC1-2-CO-NH-L3-CO-; -alquiloC1-2-NH- CO-L1-NH-CO-alquiloC1-3-; -alquiloC1-2-NH-CO-L1-NH-CO-; -CO-NH-L2-CO-; -alquiloC1-2-CO-NH-L3-CO-NH-alquiloC1-3-; alquiloC1-2-CO-NH-L3-CO-NH-; -alquiloC1-2-CO-NR10-alquiloC1-3-CO-; -alquiloC1-2-NR11-CH2-CO-NH-alquiloC1-3-; -NR12-CO-alquiloC1-3-NH-; Het5-CO-alquiloC1-2-; -alquiloC1-5-CO-NH-alquiloC1-3-CO-NH; -alquiloC1-5-NR13-CO-alquiloC1-3-NH-; -Het6-CO-Het7; -Het8-NH-alquiloC1-3-CO-NH-; -alquiloC1-3-NH-CO-Het32-CO- o alquiloC1-3-CO-Het33-CO-NH-; X1 representa un enlace directo, O, -O- alquiloC1-2-, CO, -CO-alquiloC1-2-, NR16, -NR16-alquiloC1-2-, -CO-NR17-, -Het23, -Het23-alquiloC1-2-, -O-N=CH- o -alquiloC1-2-; X2 representa un enlace directo, O, -O-alquiloC1-2-, CO, -CO-alquiloC1-2-, NR18, -NR18-alquiloC1-2-, -CO-NR19-, -Het24, - Het24-alquiloC1-2-, -O-N=CH- o -alquiloC1-2-; R1 representa hidrogeno, ciano, halo, hidroxi, formilo, alcoxiC1-6-, alquiloC1-6-, halo-fenil-carbonilamino-, Het20, alcoxiC1-6- sustituido con halo, Het1 o alquiloxiC1-4-, o R1 representa alquilo C1-6 sustituido con uno o cuando es posible con dos o más sustituyentes seleccionados de hidroxi, Het18 o halo; R2 representa hidrogeno, ciano, halo, hidroxi, hidroxicarbonil-, alquiloxicarboniloC1-4-, alquilcarboniloC1-4-, aminocarbonil-, mono- o dialquilaminocarboniloC1-4-, alquiloC1-4-, alquiniloC2-6-, cicloalquiloxi C3-6, aminosulfonilo, mono- o dialquilaminosulfoniloC1-4-, sulfuro de alquilo C1-4, sulfoxido de alquilo C1-4, sulfuro de alquilo C1-4 o alcoxiC1-6-; R3 representa hidrogeno, ciano, nitro, alquilo C1-4, o alquilo C1-4 sustituido con uno o más sustituyentes seleccionados de halo, alquiloxiC1-4-, amino-, mono- o dialquilaminoC1-4-, alquilsulfoniloC1-4- o fenilo; R4 representa hidrogeno, ciano, halo, hidroxi, hidroxicarbonilo-, alquiloxicarboniloC1-4-, alquilcarboniloC1-4-, aminocarbonilo-, mono- o dialquilaminocarbonilo C1-4, alquiloC1-4-, alquiniloC2-6-, cicloalquiloxi C3-6-, aminosulfonilo, mono- o dialquilaminosulfonilo C1-4 sulfuro de alquilo C1-4, sulfoxido de alquilo C1-4, sulfuro de alquilo C1-4 o alcoxiC1-6-; R5 representa hidrogeno, ciano, halo, hidroxi, formilo, alcoxiC1-6-, alquiloC1-6-, halo-fenil-carbonilamino-, Het21, alcoxiC1-6-sustituido con halo, Het2 o alquiloxiC1-4-, o R5 representa alquilo C1-6 sustituido con uno o cuando es posible dos o más sustituyentes seleccionados de hidroxi, Het19 o halo; R6 representa hidrogeno, alquilo C1-4, Het11, Het12-alquiloC1-4-, fenilalquiloC1-4- o fenilo donde dicho R6 está opcionalmente sustituido con uno o cuando es posible dos o más sustituyentes seleccionados de hidroxi, amino o alquiloxiC1-4-; R7 representa hidrogeno, alquilo C1-4, Het13-alquiloC1-4- o alquiloxi C1-4-alquiloC1-4-; R10, R12, y R13 cada uno independientemente, representan hidrogeno, o alquilo C1-4 opcionalmente sustituido con hidroxi, amino, mono- o dialquilamina C1-4, fenilo, Het26 o alquiloxi C1-4; R11 representa hidrogeno, alquilo C1-4 o representa mono- o dialquilaminoC1-4- alquilcarboniloC1-4 opcionalmente sustituido con hidroxi, pirimidinilo, mono- o dialquilamino C1-4 o alquiloxi C1-4; R16 y R18 cada uno independientemente representa hidrogeno, alquilo C1-4, alquiloxicarboniloC1-4-, Het16, Het17-alquiloC1-4- o fenilalquiloC1-4-; R17 y R19 cada uno independientemente representa hidrogeno, alquilo C1-4, Het14, Het15-alquiloC1-4- o fenilalquiloC1-4-; R22 representa hidrogeno, C1-4alquilo- opcionalmente sustituido con uno o cuando es posible dos o tres sustituyentes seleccionados de halo, ciano y fenilo; L1 representa alquilo C1-8 opcionalmente sustituido con uno o cuando es posible con dos o más sustituyentes seleccionados de fenilo, indolilo, tienilo, piridinilo, sulfuro de metilo, hidroxi, tiol, ciano, tiazolilo, polihaloalquilfeniloC1-4-, alquiloxiC1-4-, hidroxifenilo, alquiloxifeniloC1-4-, aminocarbonilo, hidroxicarbonilo, cicloalquilo C3-6, amino, mono- o dialquilaminoC1-4-, imidazoilo o guanidino; en particular L1 representa alquilo C1-8 opcionalmente sustituido con uno o cuando es posible con dos o más sustituyentes seleccionados de fenilo, indolilo, piridinilo, sulfuro de metilo, hidroxi, tiol, ciano, tiazolilo, polihaloalquilfeniloC1-4-, alquiloxiC1-4-, hidroxifenilo, alquiloxifeniloC1-4-, aminocarbonilo, hidroxicarbonilo, cicloalquilo C3-6, amino, mono- o dialquilaminoC1-4-, imidazoilo o guanidino; L2 representa alquilo C1-8 opcionalmente sustituido con uno o cuando es posible con dos o más sustituyentes seleccionados de fenilo, indolilo, tienilo, piridinilo, sulfuro de metilo, hidroxi, tiol, ciano, tiazolilo, polihaloalquilfeniloC1-4-, alquiloxiC1-4-, hidroxifenilo, alquiloxifeniloC1-4-, aminocarbonilo, hidroxicarbonilo, cicloalquilo C3-6, amino, mono- o dialquilaminoC1-4-, imidazoilo o guanidino; en particular L2 representa alquilo C1-8 opcionalmente sustituido con uno o cuando es posible con dos o más sustituyentes seleccionados de fenilo, indolilo, tienilo, sulfuro de metilo, hidroxi, tiol, hidroxifenilo, aminocarbonilo, amino, mono- o dialquilaminoC1-4, imidazoilo o guanidino; L3 representa alquilo C1-8 opcionalmente sustituido con uno o cuando es posible con dos o más sustituyentes seleccionados de fenilo, indolilo, tienilo, piridinilo, sulfuro de metilo, hidroxi, tiol, ciano, tiazolilo, polihaloalquilfeniloC1-4-, alquiloxiC1-4-, hidroxifenilo, alquiloxifeniloC1-4-, aminocarbonilo, hidroxicarbonilo, cicloalquilo C3-6, amino, mono- o dialquilaminoC1-4-, imidazoilo o guanidino; en particular L3 representa alquilo C1-8 opcionalmente sustituido con uno o cuando es posible con dos o más sustituyentes seleccionados de fenilo, indolilo, piridinilo, sulfuro de metilo, hidroxi, tiol, ciano, hidroxifenil-, polihaloalquilfenilo C1-4, alquiloxi C1-4, aminocarbonilo, hidroxicarbonilo, cicloalquilo C3-6, amino, mono- o dialquilamino C1-4, imidazoilo o guanidino; Het1 representa un heterociclo seleccionado de piperidinilo, morfolinilo, piperazinilo, furanilo, pirazolilo, dioxolanilo, tiazolilo, oxazolilo, imidazolilo, isoxazolilo, oxadiazolilo, piridinilo o pirrolidinilo donde dicho Het1 está opcionalmente sustituido con amino, alquilo C1-4, hidroxialquiloC1-4-, fenilo, fenilalquiloC1-4-, alquiloxiC1-4-alquiloC1-4-, mono- o dialquilaminoC1-4- o amino-carbonilo-; Het2 representa un heterociclo seleccionado de piperidinilo, morfolinilo, piperazinilo, furanilo, pirazolilo, dioxolanilo, tiazolilo, oxazolilo, imidazolilo, isoxazolilo, oxadiazolilo, piridinilo o pirrolidinilo donde dicho Het1 está opcionalmente sustituido con amino, alquilo C1-4, hidroxialquiloC1-4-, fenilo, fenilalquiloC1-4-, alquiloxiC1-4-alquiloC1-4-, mono- o dialquilaminoC1-4- o amino-carbonilo-; Het3 y Het4 cada uno independientemente representan un heterociclo seleccionado de pirrolidinilo, 2-pirrolidinonilo, quinolinilo, isoquinolinilo, decahidroquinolinilo, piperazinilo o piperidinilo donde dichos Het1 y Het4 están opcionalmente sustituidos con uno o cuando es posible con dos o más sustituyentes seleccionados de hidroxi, Het22-carbonilo, alquilo C1-4, hidroxialquiloC1-4- o polihidroxialquiloC1-4-; Het5 y Het6 cada uno independientemente representan un heterociclo seleccionado de pirrolidinilo, 2-pirrolidinonilo, quinolinilo, isoquinolinilo, decahidroquinolinilo, piperazinilo o piperidinilo donde dichos Het5 y Het6 están opcionalmente sustituidos con uno o cuando es posible con dos o más sustituyentes seleccionados de hidroxi, alquilo C1- 4, hidroxialquiloC1-4- o polihidroxialquiloC1-4-; Het y Het8 cada uno independientemente representan un heterociclo seleccionado de pirrolidinilo, 2-pirrolidinonilo, piperazinilo o piperidinilo donde dichos Het7 y Het8 están opcionalmente sustituidos con uno o cuando es posible con dos o más sustituyentes seleccionados de hidroxi, alquilo C1-4, hidroxialquiloC1-4- o polihidroxialquiloC1-4-; Het9 y Het10 cada uno independientemente representan un heterociclo seleccionado de pirrolidinilo, pirrolilo, azetidinilo, 2-pirrolidinonilo, piperazinilo, o piperidinilo donde dichos Het9 y Het10 están opcionalmente sustituidos con uno o cuando es posible con dos o más sustituyentes seleccionados de hidroxi, alquiloC1-4-, hidroxialquilo C1-4 o polihidroxialquiloC1-4-; Het11 representa un heterociclo seleccionado de pirrolidinilo o piperidinilo donde dicho Het11 está opcionalmente sustituido con uno o cuando es posible con dos o más sustituyentes seleccionados de alquilo C1-4, cicloalquilo C1-4, hidroxialquilo C1-4, alquiloxi C14-alquiloC1-4, o polihidroxialquiloC1-4-; Het12 representa un heterociclo seleccionado de morfolinilo, pirrolidinilo, piperazinilo o pip
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP04106384 | 2004-12-08 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR051788A1 true AR051788A1 (es) | 2007-02-07 |
Family
ID=34930016
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP050105123A AR051788A1 (es) | 2004-12-08 | 2005-12-07 | Derivados 2,4 (4,6) pirimidina como inhibidores de quinasa |
Country Status (22)
| Country | Link |
|---|---|
| US (2) | US8148388B2 (es) |
| EP (1) | EP1824856B1 (es) |
| JP (1) | JP5022909B2 (es) |
| KR (1) | KR101428506B1 (es) |
| CN (1) | CN101072779B (es) |
| AR (1) | AR051788A1 (es) |
| AU (1) | AU2005313348B2 (es) |
| BR (1) | BRPI0518424B8 (es) |
| CA (1) | CA2588761C (es) |
| CR (1) | CR9234A (es) |
| DK (1) | DK1824856T3 (es) |
| EA (1) | EA013368B1 (es) |
| ES (1) | ES2442458T3 (es) |
| IL (1) | IL183706A0 (es) |
| MX (1) | MX2007006821A (es) |
| MY (1) | MY169441A (es) |
| NO (1) | NO340130B1 (es) |
| NZ (1) | NZ554820A (es) |
| TW (1) | TWI374140B (es) |
| UA (1) | UA90693C2 (es) |
| WO (1) | WO2006061415A1 (es) |
| ZA (1) | ZA200705040B (es) |
Families Citing this family (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ547794A (en) | 2003-12-18 | 2009-11-27 | Janssen Pharmaceutica Nv | Pyrido- and pyrimidopyrimidine derivatives as anti-proliferative agents |
| JP5031564B2 (ja) * | 2004-08-10 | 2012-09-19 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | Ｈｉｖ抑制１，２，４−トリアジン−６−オン誘導体 |
| JO3088B1 (ar) * | 2004-12-08 | 2017-03-15 | Janssen Pharmaceutica Nv | مشتقات كوينازولين كبيرة الحلقات و استعمالها بصفتها موانع كينيز متعددة الاهداف |
| NI200700147A (es) | 2004-12-08 | 2019-05-10 | Janssen Pharmaceutica Nv | Derivados de quinazolina inhibidores de cinasas dirigidos a multip |
| PT1951730E (pt) * | 2005-11-16 | 2010-08-27 | S Bio Pte Ltd | Derivados de pirimidina ligados a heteroalquilo |
| CA2654583C (en) * | 2006-07-13 | 2015-11-24 | Janssen Pharmaceutica N.V. | Mtki quinazoline derivatives |
| WO2008060248A1 (en) * | 2006-11-15 | 2008-05-22 | S*Bio Pte Ltd. | Indole sustituted pyrimidines and use thereof in the treatment of cancer |
| JP5536647B2 (ja) | 2007-07-27 | 2014-07-02 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | ピロロピリミジン |
| TWI475996B (zh) | 2007-10-19 | 2015-03-11 | Celgene Avilomics Res Inc | 雜芳基化合物及其用途 |
| US7989465B2 (en) | 2007-10-19 | 2011-08-02 | Avila Therapeutics, Inc. | 4,6-disubstituted pyrimidines useful as kinase inhibitors |
| DK2283024T3 (da) * | 2008-03-10 | 2013-08-05 | Janssen Pharmaceutica Nv | 4-aryl-2-anilinpyrimidiner som PLK-kinaseinhibitorer |
| CA2722326A1 (en) * | 2008-04-24 | 2009-10-29 | Incyte Corporation | Macrocyclic compounds and their use as kinase inhibitors |
| US8338439B2 (en) | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| US11351168B1 (en) | 2008-06-27 | 2022-06-07 | Celgene Car Llc | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| EA201100450A1 (ru) * | 2008-09-08 | 2011-10-31 | Мерк Патент Гмбх | Макроциклические пирамидины в качестве ингибиторов протеинкиназы |
| WO2010085597A1 (en) * | 2009-01-23 | 2010-07-29 | Incyte Corporation | Macrocyclic compounds and their use as kinase inhibitors |
| JP2012197231A (ja) * | 2009-08-06 | 2012-10-18 | Oncotherapy Science Ltd | Ｔｔｋ阻害作用を有するピリジンおよびピリミジン誘導体 |
| RU2528386C2 (ru) | 2010-05-21 | 2014-09-20 | Кемилиа Аб | Новые производные пиримидина |
| JP5957460B2 (ja) | 2010-11-01 | 2016-07-27 | セルジーン アヴィロミクス リサーチ， インコーポレイテッド | 複素環式化合物またはその使用 |
| PT2646448T (pt) * | 2010-11-29 | 2017-10-04 | Osi Pharmaceuticals Llc | Inibidores macrocíclicos de cinases |
| CA2830129C (en) | 2011-03-24 | 2016-07-19 | Chemilia Ab | Novel pyrimidine derivatives |
| US9056839B2 (en) | 2012-03-15 | 2015-06-16 | Celgene Avilomics Research, Inc. | Solid forms of an epidermal growth factor receptor kinase inhibitor |
| DK2825042T3 (en) | 2012-03-15 | 2018-11-26 | Celgene Car Llc | SALTS OF THE CHINASE INHIBITOR OF THE EPIDERMAL GROWTH FACTOR RECEPTOR |
| US9861635B2 (en) * | 2013-05-06 | 2018-01-09 | Merck Patent Gmbh | Macrocycles as kinase inhibitors |
| MA39822A (fr) | 2014-04-03 | 2018-02-06 | Janssen Pharmaceutica Nv | Dérivés de pyrimidine bicycle |
| MA39823A (fr) | 2014-04-03 | 2018-01-09 | Janssen Pharmaceutica Nv | Dérivés de pyridine macrocyclique |
| SG11201704628VA (en) * | 2015-02-05 | 2017-07-28 | Merck Patent Gmbh | Macrocyclic compounds as irak1/4 inhibitors and uses thereof |
| WO2018177889A1 (en) | 2017-03-28 | 2018-10-04 | Bayer Aktiengesellschaft | Novel ptefb inhibiting macrocyclic compounds |
| CA3057892A1 (en) | 2017-03-28 | 2018-10-04 | Bayer Aktiengesellschaft | Novel ptefb inhibiting macrocyclic compounds |
| EP3983370B1 (en) | 2019-06-12 | 2023-08-02 | Nouryon Chemicals International B.V. | Process for the production of diacyl peroxides |
| US12215074B2 (en) | 2019-06-12 | 2025-02-04 | Nouryon Chemicals International B.V. | Process for the production of peroxyesters |
| EP3983340B1 (en) * | 2019-06-12 | 2023-08-02 | Nouryon Chemicals International B.V. | Method for isolating carboxylic acid from an aqueous side stream |
| EP3983368B1 (en) | 2019-06-12 | 2023-08-02 | Nouryon Chemicals International B.V. | Process for the production of diacyl peroxides |
| ES2961184T3 (es) | 2019-06-12 | 2024-03-08 | Nouryon Chemicals Int Bv | Proceso para la producción de peróxidos de diacilo |
| JP2023513793A (ja) * | 2020-02-14 | 2023-04-03 | ソーク インスティテュート フォー バイオロジカル スタディーズ | 大環状ｕｌｋ１／２阻害剤 |
| CN113549113A (zh) * | 2020-06-17 | 2021-10-26 | 广州百霆医药科技有限公司 | 一种含膦大环化合物及其制备方法与应用 |
| EP4450505A4 (en) * | 2021-12-15 | 2025-07-02 | Whan In Pharmaceutical Co Ltd | MACROCYCLIC PYRIMIDINE DERIVATIVE, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION FOR PREVENTION OR TREATMENT OF NEURODEGENERATIVE DISEASE AND CONTAINING THIS DERIVATIVE AS ACTIVE INGREDIENT |
| KR102613509B1 (ko) * | 2021-12-15 | 2023-12-13 | 환인제약 주식회사 | 마크로사이클릭 피리미딘 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 신경 퇴행성 질환의 예방 또는 치료용 약학적 조성물 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2274634T3 (es) * | 1998-08-29 | 2007-05-16 | Astrazeneca Ab | Compuestos de pirimidina. |
| GB9828511D0 (en) * | 1998-12-24 | 1999-02-17 | Zeneca Ltd | Chemical compounds |
| GB0004890D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| TWI329105B (en) * | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| GB0206215D0 (en) * | 2002-03-15 | 2002-05-01 | Novartis Ag | Organic compounds |
| NZ537752A (en) * | 2002-07-29 | 2006-12-22 | Rigel Pharmaceuticals Inc | Use of 2,4-pyrimidinediamine compounds in the preparation of medicaments for treating autoimmune diseases |
| DE10239042A1 (de) | 2002-08-21 | 2004-03-04 | Schering Ag | Makrozyclische Pyrimidine, deren Herstellung und Verwendung als Arzneimittel |
| JO2785B1 (en) | 2003-05-27 | 2014-03-15 | شركة جانسين فارماسوتيكا ان. في | Quinazoline derivatives |
| NZ547794A (en) | 2003-12-18 | 2009-11-27 | Janssen Pharmaceutica Nv | Pyrido- and pyrimidopyrimidine derivatives as anti-proliferative agents |
| NZ547795A (en) | 2003-12-18 | 2009-07-31 | Janssen Pharmaceutica Nv | 3-Cyano-quinoline derivatives with antiproliferative activity |
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2005
- 2005-12-06 MY MYPI20055703A patent/MY169441A/en unknown
- 2005-12-07 AR ARP050105123A patent/AR051788A1/es unknown
- 2005-12-07 TW TW094143059A patent/TWI374140B/zh not_active IP Right Cessation
- 2005-12-08 UA UAA200705051A patent/UA90693C2/ru unknown
- 2005-12-08 CA CA2588761A patent/CA2588761C/en not_active Expired - Lifetime
- 2005-12-08 NZ NZ554820A patent/NZ554820A/en not_active IP Right Cessation
- 2005-12-08 AU AU2005313348A patent/AU2005313348B2/en not_active Expired
- 2005-12-08 KR KR1020077011771A patent/KR101428506B1/ko not_active Expired - Lifetime
- 2005-12-08 JP JP2007544917A patent/JP5022909B2/ja not_active Expired - Lifetime
- 2005-12-08 DK DK05819148.7T patent/DK1824856T3/da active
- 2005-12-08 ES ES05819148.7T patent/ES2442458T3/es not_active Expired - Lifetime
- 2005-12-08 US US11/720,681 patent/US8148388B2/en active Active
- 2005-12-08 EP EP05819148.7A patent/EP1824856B1/en not_active Expired - Lifetime
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- 2005-12-08 CN CN2005800420717A patent/CN101072779B/zh not_active Expired - Lifetime
- 2005-12-08 WO PCT/EP2005/056606 patent/WO2006061415A1/en not_active Ceased
- 2005-12-08 BR BRPI0518424A patent/BRPI0518424B8/pt active IP Right Grant
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2007
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- 2007-06-07 ZA ZA200705040A patent/ZA200705040B/xx unknown
- 2007-07-06 CR CR9234A patent/CR9234A/es not_active Application Discontinuation
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