AR047366A1 - Derivados de tiofeno como inhibidores de chk 1 - Google Patents
Derivados de tiofeno como inhibidores de chk 1Info
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- AR047366A1 AR047366A1 ARP050100025A ARP050100025A AR047366A1 AR 047366 A1 AR047366 A1 AR 047366A1 AR P050100025 A ARP050100025 A AR P050100025A AR P050100025 A ARP050100025 A AR P050100025A AR 047366 A1 AR047366 A1 AR 047366A1
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- alkyl
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- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
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- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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- 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
- A61K31/435—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
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- 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
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- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- 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]
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- 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
- 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
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- 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
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- 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
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
- C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
- C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom 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 to ring carbon atoms
- C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur 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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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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- 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
- C07D417/14—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 three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
- C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
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- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
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- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Cardiology (AREA)
- Hematology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Heart & Thoracic Surgery (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Steroid Compounds (AREA)
- Heterocyclic Compounds Containing Sulfur Atoms (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
La presente se refiere a derivados de tiofeno como inhibidores de CHK1. Compuestos que proveen tratamiento o profilaxis para el cáncer. Reivindicacion 1: Un compuesto, caracterizado porque es de formula (1) donde: X se selecciona entre NH, S y O; Y se selecciona entre CH o N; R1 se selecciona entre ciano, isociano, C1-6 alquilo, -NR11R12, C1-6alcoxi, C2-6alquenilo, C2-6 alquinilo, cicloalquilo, cicloalquenilo, arilo y heterociclilo, con la condicion que R1 no sea tienilo; y donde R1 puede estar sustituido opcionalmente en uno o más átomos de C por uno o más R9; y donde si dicho R1 contiene un grupo -NH-, el N de dicho grupo puede estar sustituido opcionalmente por un grupo seleccionado entre R10; R2 y R3 se seleccionan independientemente entre sí entre -C(=O)NR6R7, -SO2NR16R17, -NHC(=O)NHR4 y -NHC(=NR8)NH2; R4 se selecciona entre H, OH, -NR11R12, bencilo, C1-6 alcoxi, cicloalquilo, cicloalquenilo, arilo, heterociclilo, mercapto, CHO, -COarilo, -CO(C1-6alquilo), - CONR30R31, -CO2(C1-6 alquilo), -CO2arilo, -CO2NR30R31, -S-alquilo, -SO(C1-6 alquilo), -SO2(C1-6 alquilo), -S-arilo, -SOarilo, -SO2arilo, -SO2NR30R31 y -(C1-6 alquilo)SO2NR30R31 donde R4 puede estar sustituido opcionalmente en uno o más átomos de C por uno o más R15; y donde si dicho heterociclilo contiene un grupo NH-, el N puede estar sustituido opcionalmente por un grupo seleccionado entre R14; R6 y R7 se seleccionan independientemente entre sí entre H, OH, OCH3, C1-6 alcoxi, -NH2, -NHCH3, - N(CH3)2, (C1-3 alquilo)NR11R12, -CH2CH2OH, cicloalquilo y un anillo heterociclilo de 5, 6 o 7 miembros que contiene al menos un átomo de N, con la condicion que R6 y R7 no sean ambos H; como alternativa R6 y R7 tomados en conjunto con el N a cual están unidos forman un anillo heterocíclico; donde R6 y R7, independientemente entre sí, pueden estar sustituidos opcionalmente en uno o más átomos de C por uno o más R18; y donde si dicho heterociclilo contiene un grupo -NH-, el N de dicho grupo puede estar sustituido opcionalmente por un grupo seleccionado entre R19; R8 se selecciona entre ciano, isociano, -SO2(C1-6 alquilo), -SO2arilo, -SO2cicloalquilo, -SO2cicloalquenilo, -SO2heterociclilo y CF3; donde R8 puede estar sustituido opcionalmente en uno o más átomos de C por uno o más R23; R9; R15, R18, R23, R24 y R33 se seleccionan independientemente entre sí entre halogeno, nitro, -NR30R31, ciano, isociano, C1-6 alquilo, C2-6alquenilo, C2-6 alquinilo, arilo, cicloalquilo, heterociclilo, hidroxi, ceto(=O), -O(C1-6 alquilo), Oarilo, -OCOalquilo, -NHCHO, -N(C1-6 alquilo)CHO, -NHCONR30R31, -N(C1-6 alquil)CONR30R31, -NHCOalquilo, -NHCO2(C1-6 alquilo); -NHCO2H, -;N(C1-6 alquil)CO(C1-6 alquilo); -NHSO2(C1-6 alquilo); carboxi, -amidino, -CHO, -CONR30R31, -CO(C1-6 alquilo); -COheterociclilo, COcicloalquilo, -CO2H, CO2(C1-6 alquilo); -CO2(arilo), -CO2(NR30R31), mercapto, -S(C1-6 alquilo); -SO(C1-6 alquilo); -SO2(C1-6 alquilo);??-SO2NR31R31; donde R9, R15, R18, R23, R24 y R33, independientemente entre sí, pueden estar sustituidos opcionalmente en un C por uno o más R20 y en un N de cualquier grupo que contenga un NH o NH2 por R21; R10, R14, R19, R25 y R34 se seleccionan independientemente entre sí entre halogeno, nitro, -NR30R31, ciano, isociano, C1-6 alquilo, C2-6alquenilo, C2-6 alquinilo, arilo, cicloalquilo, heterociclilo, hidroxi, ceto(=O), -O(C1-6 alquilo), Oarilo, -OCOalquilo, -NHCHO, -N(C1-6 alquil)CHO, -NHCONR30R31, -N(C1-6 alquil)CONR30R31, -NHCOalquilo, -NHCO2(C1-6 alquilo); -NHCO2H; -N(C1-6 alquil)CO(C1-6 alquilo); -NHSO2(C1-6 alquilo); carboxi, -amidino, -CHO, -CONR30R31, -CO(C1-6 alquilo); -COheterociclilo, COcicloalquilo, -CO2H, CO2(C1-6 alquilo); -CO2(arilo), - CO2(NR30R31), mercapto, -S(C1-6 alquilo); -SO(C1-6 alquilo); -SO2(C1-6 alquilo);??-SO2NR30R31; donde R10, R14, R19, R25, y R34, independientemente entre sí, pueden estar sustituidos opcionalmente en un C por uno o más R22 y en un N de cualquier grupo que contenga un NH o NH2 por R23; R11 y R12 se seleccionan independientemente entre sí entre H, alquilo C1-6, cicloalquilo, arilo, heterociclilo; como alternativa R11 y R12 tomados en conjunto con el N al cual están unidos forman un anillo heterocíclico; donde R11 y R12, independientemente entre sí pueden estar sustituidos opcionalmente en un C por uno o más R33; y donde si dicho heterociclilo contiene un grupo NH-, el N de dicho grupo puede estar sustituido opcionalmente por un grupo seleccionado entre R34; R16 y R17 se seleccionan independientemente entre sí entre H, OH, OCH3, C1-6 alcoxi, NH2, -NHCH3, -N(CH3)2 (C1-3 alquilo)NR11R12, -CH2CH2OH; cicloalquilo, arilo, o un anillo heterociclilo de 5, 6 o 7 miembros que contiene al menos un átomo de N, con la condicion que R16 y R17 no sean ambos H; como alternativa R16 y R17 tomados en conjunto con el N al cual están unidos forman un anillo heterocíclico sustituido opcionalmente; donde R16 y R17, independientemente entre sí, pueden estar sustituidos opcionalmente en uno o más átomos e C por uno o más R24; y donde si dicho heterociclilo contiene un grupo -NH-, el N de dicho grupo puede estar sustituido opcionalmente por un grupo seleccionado entre R25; R20, R22 y R32 se seleccionan independientemente entre sí entre halogeno, nitro, -NR30R31, ciano, isociano, C1-6 alquilo, C2-6alquenilo, C2-6 alquinilo, arilo, cicloalquilo, heterociclilo, hidroxi, ceto(=O), -O(C1-6 alquilo), -Oarilo, -OCOalquilo, -NHCHO, -N(C1-6 alquil)CHO, -NHCONR30R31, -N(C1-6 alquil)CONR30R31, -NHCOalquilo, -NHCO2(C1-6 alquilo); -NHCO2H; -N(C1-6 alquil)CO(C1-6 alquilo); -NHSO2(C1-6 alquilo); carboxi, -amidino, -CHO, -CONR30R31, -CO(C1-6 alquilo); -COheterociclilo, COcicloalquilo, -CO2H, CO2(C1-6 alquilo); -CO2(arilo), -CO2(NR30R31), mercapto, -S(C1-6 alquilo); -SO(C1-6 alquilo); -SO2(C1-6 alquilo);??-SO2NR30R31; donde R20, R21 y R32, independientemente entre sí, pueden estar sustituidos opcionalmente en un C por uno o más R26 y en un N de cualquier grupo que contenga un NH o NH2 por R27; R21, R23 y R35 se seleccionan independientemente entre sí entre halogeno, nitro, -NR30R31, ciano, isociano, C1-6 alquilo, C2-6 alquenilo, C2-6 alquinilo, arilo, cicloalquilo, heterociclilo, hidroxi, ceto(=O), -O(C1-6 alquilo), -Oarilo, -OCOalquilo, -NHCHO, -N(C1-6 alquil)CHO, -NHCONR30R31, -N(C1-6 alquil)CONR30R31, -NHCOalquilo, -NHCO2(C1-6 alquilo); -NHCO2H, -;N(C1-6 alquil)CO(C1-6 alquilo); -NHSO2(C1-6 alquilo); carboxi, -amidino, - CHO, -CONR30R31, -CO(C1-6 alquilo); -COheterociclilo, COcicloalquilo, -CO2H, CO2(C1-6 alquilo); -CO2(arilo), -CO2(NR30R31), mercapto, -S(C1-6 alquilo); -SO(C1-6 alquilo); -SO2(C1-6 alquilo);??-SO2NR30R31; donde R21, R23 y R35, independientemente entre sí, pueden estar sustituidos opcionalmente en un C por uno o más R28 y en un N de cualquier grupo que contenga un NH por R29; R26 y R28 se seleccionan independientemente entre sí entre halogeno, nitro, -NR30R31, ciano, isociano, C1-6 alquilo, C2-6 alquenilo, C2-6 alquinilo, arilo, cicloalquilo, heterociclilo, hidroxi, ceto(=O), -O(C1-6 alquilo), -Oarilo, -OCOalquilo, -NHCHO, -N(C1-6 alquil)CHO, -NHCONR30R31, -N(C1-6 alquil)CONR30R31, -NHCOalquilo, -NHCO2(C1-6 alquilo); -NHCO2H, -;N(C1-6 alquil)CO(C1-6 alquilo); -NHSO2(C1-6 alquilo); carboxi, -amidino, -CHO, -CONR30R31, -CO(C1-6 alquilo); -COheterociclilo, -COcicloalquilo, -CO2H, CO2(C1-6 alquilo); -CO2(arilo), -CO2(NR30R31), mercapto, -S(C1-6 alquilo); -SO(C1-6 alquilo); -SO2(C1-6 alquilo);??-SO2NR31; R27 y R29 se seleccionan independientemente entre sí entre halogeno, nitro, -NR30R31, ciano, isociano, C1-6 alquilo, C2-6 alquenilo, C2-6 alquinilo, arilo, cicloalquilo, heterociclilo, hidroxi, ceto(=O), -O(C1-6 alquilo), - Oarilo, -OCOalquilo, -NHCHO, -N(C1-6 alquil)CHO, -NHCONR30R31, -N(C1-6 alquil)CONR30R31, -NHCOalquilo, -NHCO2(C1-6 alquilo); -NHCO2H, -;N(C1-6 alquil)CO(C1-6 alquilo); -NHSO2(C1-6 alquilo); carboxi, -amidino, -CHO, -CONR30R31, -CO(C1-6 alquilo); - COheterociclilo, -COcicloalquilo, -CO2H, CO2(C1-6 alquilo); -CO2(arilo), -CO2(NR30R31), mercapto, -S(C1-6 alquilo); -SO(C1-6 alquilo); -SO2(C1-6 alquilo);??-SO2NR30R31; R30 y R31 se seleccionan independientemente entre sí entre halogeno, nitro, -NH2, ciano, isociano, C1-6 alquilo, C2-6 alquenilo, C2-6 alquinilo, arilo, cicloalquilo, heterociclilo, hidroxi, ceto(=O), -O(C1-6 alquilo), -Oarilo, -OCOalquilo, -NHCHO, -N(C1-6 alquil)CHO, -NHCONR11R12, -N(C1-6 alquil)CONR11R12, -NHCOalquilo, -NHCO2(C1- 6 alquilo); -NHCO2H, -;N(C1-6 alquil)CO(C1-6 alquilo); -NHSO2(C1-6 alquilo); carbonilo, -amidino, -CHO, -CONR30R31, -CO(C1-6 alquilo); -COheterociclilo, -COcicloalquilo, -CO2H, CO2(C1-6 alquilo); -CO2(arilo), -CO2(NR30R31), mercapto, -S(C1-6 alquilo); -SO(C1-6 alquilo); -SO2(C1-6 alquilo);??-SO2NR11R12;donde R30 y R31, independientemente entre sí, pueden estar sustituidos opcionalmente en un C por uno o más R32, y donde si el heterociclilo mencionado contiene un grupo -NH- o -NH2, el N de dicho grupo puede estar sustituido opcionalmente por un grupo seleccionado entre R35; o una sal aceptable para uso farmacéutico del mismo; con la condicion que cuando X es S; Y es CH; R2 es C(=O)NR6R7; y R3 es NHC(=O)NHR4; entonces R1 no puede ser como se muestra en la formula (2) donde R5 se selecciona entre H, un carbociclilo sustituido opcionalmente, o un C1-6 alquilo sustituido opcionalmente; con la condicion adicional que dicho compuesto no sea: (1-etil-piperidin-3-il)-amida del ácido 5-metil-2-ureido-tiofeno-3-carboxílico; [3-((S)-3-amino-azepan-1-carbonil)-5-etil-tiofen-2-il]-urea; (S)-piperidin-3-ilamida del ácido 2-morfolin-4-il-4-ureido-tiazol-5-carboxílico; (S)-piperidin-3-ilamida del ácido 2-metil-5-ureido-oxazol-4- carboxílico; (S)-piperidin-3-ilamida del ácido 5-(4-cloro-fenil)-3-{3-[(R)-1-(2,2,2-trifluoro-acetil)-piperidin-3-il]-ureido}-tiofeno-2-carboxílico ácido; o N-(3-{[(3S)-3-aminoazepan-1-il]carbonil)-5-piridin-2-il-2-tienil)urea.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
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US53431004P | 2004-01-05 | 2004-01-05 | |
US55330504P | 2004-03-15 | 2004-03-15 |
Publications (1)
Publication Number | Publication Date |
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AR047366A1 true AR047366A1 (es) | 2006-01-18 |
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ID=34753019
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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ARP050100025A AR047366A1 (es) | 2004-01-05 | 2005-01-05 | Derivados de tiofeno como inhibidores de chk 1 |
Country Status (20)
Country | Link |
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US (1) | US20070010556A1 (es) |
EP (2) | EP1732920B1 (es) |
JP (1) | JP2007517843A (es) |
KR (1) | KR20060127127A (es) |
CN (1) | CN100584840C (es) |
AR (1) | AR047366A1 (es) |
AT (1) | ATE501138T1 (es) |
AU (1) | AU2004312193B2 (es) |
BR (1) | BRPI0418351A (es) |
CA (1) | CA2552050C (es) |
DE (1) | DE602004031777D1 (es) |
IL (1) | IL176554A0 (es) |
MX (1) | MXPA06007692A (es) |
MY (1) | MY142018A (es) |
NO (1) | NO20063449L (es) |
RU (1) | RU2397168C2 (es) |
SA (1) | SA05250449B1 (es) |
TW (1) | TW200536849A (es) |
UY (1) | UY28708A1 (es) |
WO (1) | WO2005066163A2 (es) |
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US8962639B2 (en) | 2009-05-29 | 2015-02-24 | Abbvie Inc. | Potassium channel modulators |
GB0911042D0 (en) | 2009-06-25 | 2009-08-12 | Istituto Superiore Di Sanito | Treatment of tumorigenic cells in solid tumours |
CA2689707A1 (en) | 2009-11-16 | 2011-05-16 | Jean-Simon Diallo | Identification of the novel small molecule viral sensitizer vse1 using high-throughput screening |
ES2481791T3 (es) * | 2009-09-18 | 2014-07-31 | Zhanggui Wu | Compuestos novedosos y uso terapéutico para la inhibición de proteína cinasa |
JP2013532683A (ja) | 2010-07-27 | 2013-08-19 | カディラ ヘルスケア リミティド | ポリ(adpリボース)ポリメラーゼ−1阻害剤としての、置換4−(4−フルオロ−3−(ピペラジン−1−カルボニル)ベンジル)フタラジン−1(2h)−オン誘導体 |
CN101967141A (zh) * | 2010-10-13 | 2011-02-09 | 信实生物医药(上海)有限公司 | 一种Chk蛋白激酶拮抗剂AZD-7762的制备方法 |
AR083575A1 (es) * | 2010-11-08 | 2013-03-06 | Lilly Co Eli | Aminopirazoles para inhibir la proteinquinasa chk1 |
WO2012074754A1 (en) | 2010-11-16 | 2012-06-07 | Array Biopharma Inc. | Combination of checkpoint kinase 1 inhibitors and wee 1 kinase inhibitors |
EA201591239A1 (ru) | 2012-12-31 | 2015-10-30 | Кадила Хелзкэр Лимитед | Замещенные фталазин-1(2h)-оновые производные в качестве селективных ингибиторов поли(адф-рибоза)полимеразы-1 |
CN103880746A (zh) * | 2014-02-26 | 2014-06-25 | 南通大学 | 一种(s)-3-(Boc-氨基)氮杂环庚烷的化学合成方法 |
CN104926801B (zh) | 2014-03-22 | 2019-06-04 | 浙江大学 | 取代氮杂环类衍生物、含其的药物组合物及其在抗肿瘤中的应用 |
RS59054B1 (sr) | 2014-06-17 | 2019-08-30 | Vertex Pharma | Postupak za lečenje raka korišćenjem kombinacije chk1 i atr inhibitora |
KR20180011843A (ko) | 2015-06-11 | 2018-02-02 | 바실리어 파마슈티카 인터내셔널 리미티드 | 유출-펌프 억제제 및 이의 치료적 용도 |
US11464774B2 (en) | 2015-09-30 | 2022-10-11 | Vertex Pharmaceuticals Incorporated | Method for treating cancer using a combination of DNA damaging agents and ATR inhibitors |
WO2017132928A1 (en) | 2016-02-04 | 2017-08-10 | Pharmaengine, Inc. | 3,5-disubstituted pyrazoles useful as checkpoint kinase 1 (chk1) inhibitors, and their preparations and applications |
JP6749422B2 (ja) * | 2016-02-16 | 2020-09-02 | コリア・インスティテュート・オブ・サイエンス・アンド・テクノロジー | プロテインキナーゼ阻害剤である新規な2,3,5−置換チオフェン化合物 |
EP3461480A1 (en) | 2017-09-27 | 2019-04-03 | Onxeo | Combination of a dna damage response cell cycle checkpoint inhibitors and belinostat for treating cancer |
JP7041322B2 (ja) * | 2018-05-30 | 2022-03-23 | ファロス・アイバイオ・カンパニー・リミテッド | 2,3,5-置換されたチオフェン化合物の乳癌の予防、改善または治療用途 |
EP3804719A4 (en) * | 2018-05-30 | 2022-03-30 | Pharos Ibio Co., Ltd. | USE OF 2,3,5-SUBSTITUTED THIOPHENE COMPOUND TO IMPROVE RADIATION THERAPY |
WO2021104461A1 (zh) | 2019-11-29 | 2021-06-03 | 南京明德新药研发有限公司 | 二氮杂吲哚类衍生物及其作为Chk1抑制剂的应用 |
JP7407298B2 (ja) * | 2020-03-04 | 2023-12-28 | ファロス・アイバイオ・カンパニー・リミテッド | 2,3,5-置換されたチオフェン化合物の卵巣癌の予防、改善または治療用途 |
KR102535842B1 (ko) * | 2020-07-31 | 2023-05-23 | (주)파로스아이바이오 | 2,3,5-치환된 싸이오펜 화합물의 비만세포증 예방, 개선 또는 치료 용도 |
KR102535840B1 (ko) * | 2020-07-31 | 2023-05-23 | (주)파로스아이바이오 | 2,3,5-치환된 싸이오펜 화합물의 위장관기질종양 예방, 개선 또는 치료 용도 |
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GB9624482D0 (en) | 1995-12-18 | 1997-01-15 | Zeneca Phaema S A | Chemical compounds |
IL125686A (en) | 1996-02-13 | 2002-11-10 | Zeneca Ltd | Quinazoline derivatives, processes for their preparation, pharmaceutical preparations containing them and their use in the manufacture of a drug with an anti-angiogenic effect and / or an effect of reducing vascular permeability |
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GB9718972D0 (en) | 1996-09-25 | 1997-11-12 | Zeneca Ltd | Chemical compounds |
US6344476B1 (en) * | 1997-05-23 | 2002-02-05 | Bayer Corporation | Inhibition of p38 kinase activity by aryl ureas |
US6187799B1 (en) * | 1997-05-23 | 2001-02-13 | Onyx Pharmaceuticals | Inhibition of raf kinase activity using aryl ureas |
GB9714249D0 (en) | 1997-07-08 | 1997-09-10 | Angiogene Pharm Ltd | Vascular damaging agents |
GB9900334D0 (en) | 1999-01-07 | 1999-02-24 | Angiogene Pharm Ltd | Tricylic vascular damaging agents |
GB9900752D0 (en) | 1999-01-15 | 1999-03-03 | Angiogene Pharm Ltd | Benzimidazole vascular damaging agents |
GB0003154D0 (en) * | 2000-02-12 | 2000-04-05 | Astrazeneca Uk Ltd | Novel compounds |
IL152682A0 (en) | 2000-05-31 | 2003-06-24 | Astrazeneca Ab | Indole derivatives with vascular damaging activity |
WO2002004434A1 (en) | 2000-07-07 | 2002-01-17 | Angiogene Pharmaceuticals Limited | Colchinol derivatives as vascular damaging agents |
RU2003103603A (ru) | 2000-07-07 | 2004-08-20 | Энджиоджен Фармасьютикалз Лимитед (Gb) | Производные колхинола в качестве ингибиторов ангиогенеза |
EP1324759A4 (en) * | 2000-10-12 | 2004-05-12 | Smithkline Beecham Corp | NF - G (K) B INHIBITORS |
SE0102617D0 (sv) * | 2001-07-25 | 2001-07-25 | Astrazeneca Ab | Novel compounds |
JP2005506334A (ja) * | 2001-10-04 | 2005-03-03 | スミスクライン・ビーチャム・コーポレイション | NF−κB阻害剤 |
WO2003028731A1 (en) * | 2001-10-04 | 2003-04-10 | Smithkline Beecham Corporation | Chk1 kinase inhibitors |
WO2003029241A1 (en) | 2001-10-04 | 2003-04-10 | Smithkline Beecham Corporation | Chk1 kinase inhibitors |
SE0300092D0 (sv) * | 2003-01-15 | 2003-01-15 | Astrazeneca Ab | Novel compounds |
SE0300091D0 (sv) * | 2003-01-15 | 2003-01-15 | Astrazeneca Ab | Novel compounds |
DE602004017478D1 (de) * | 2003-08-15 | 2008-12-11 | Astrazeneca Ab | Substituierte thiophene und deren verwendungen |
JP2008523071A (ja) * | 2004-12-07 | 2008-07-03 | ルーカス ファーマシューティカルズ, インコーポレイテッド | Mapキナーゼの尿素インヒビター |
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- 2004-12-24 RU RU2006128426/04A patent/RU2397168C2/ru not_active IP Right Cessation
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- 2004-12-24 DE DE602004031777T patent/DE602004031777D1/de active Active
- 2004-12-24 BR BRPI0418351-7A patent/BRPI0418351A/pt not_active IP Right Cessation
- 2004-12-24 WO PCT/GB2004/005400 patent/WO2005066163A2/en active Application Filing
- 2004-12-24 MX MXPA06007692A patent/MXPA06007692A/es active IP Right Grant
- 2004-12-24 EP EP10184816A patent/EP2305671A1/en not_active Withdrawn
- 2004-12-24 KR KR1020067015848A patent/KR20060127127A/ko not_active Application Discontinuation
- 2004-12-24 AT AT04806196T patent/ATE501138T1/de not_active IP Right Cessation
- 2004-12-24 CN CN200480042170A patent/CN100584840C/zh not_active Expired - Fee Related
- 2004-12-24 JP JP2006548370A patent/JP2007517843A/ja active Pending
- 2004-12-24 US US10/596,930 patent/US20070010556A1/en not_active Abandoned
- 2004-12-24 AU AU2004312193A patent/AU2004312193B2/en not_active Ceased
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- 2005-01-04 UY UY28708A patent/UY28708A1/es not_active Application Discontinuation
- 2005-01-05 TW TW094100276A patent/TW200536849A/zh unknown
- 2005-01-05 SA SA05250449A patent/SA05250449B1/ar unknown
- 2005-01-05 AR ARP050100025A patent/AR047366A1/es not_active Application Discontinuation
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Also Published As
Publication number | Publication date |
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MXPA06007692A (es) | 2007-01-26 |
JP2007517843A (ja) | 2007-07-05 |
NO20063449L (no) | 2006-07-27 |
EP2305671A1 (en) | 2011-04-06 |
US20070010556A1 (en) | 2007-01-11 |
CN100584840C (zh) | 2010-01-27 |
SA05250449B1 (ar) | 2008-11-18 |
UY28708A1 (es) | 2005-08-31 |
WO2005066163A2 (en) | 2005-07-21 |
RU2397168C2 (ru) | 2010-08-20 |
EP1732920B1 (en) | 2011-03-09 |
AU2004312193A1 (en) | 2005-07-21 |
IL176554A0 (en) | 2006-10-31 |
RU2006128426A (ru) | 2008-02-20 |
DE602004031777D1 (en) | 2011-04-21 |
WO2005066163A3 (en) | 2005-09-01 |
MY142018A (en) | 2010-08-16 |
BRPI0418351A (pt) | 2007-05-08 |
ATE501138T1 (de) | 2011-03-15 |
CN1922172A (zh) | 2007-02-28 |
TW200536849A (en) | 2005-11-16 |
AU2004312193B2 (en) | 2008-09-25 |
EP1732920A2 (en) | 2006-12-20 |
CA2552050A1 (en) | 2005-07-21 |
SA05250449A (ar) | 2005-12-03 |
CA2552050C (en) | 2011-08-09 |
KR20060127127A (ko) | 2006-12-11 |
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