AR059098A1 - Inhibidores de quinasa heterobiciclicos fusionados - Google Patents
Inhibidores de quinasa heterobiciclicos fusionadosInfo
- Publication number
- AR059098A1 AR059098A1 ARP070100248A ARP070100248A AR059098A1 AR 059098 A1 AR059098 A1 AR 059098A1 AR P070100248 A ARP070100248 A AR P070100248A AR P070100248 A ARP070100248 A AR P070100248A AR 059098 A1 AR059098 A1 AR 059098A1
- Authority
- AR
- Argentina
- Prior art keywords
- cr6ar7a
- alkyl
- cycloalkenyl
- alkynyl
- alkenyl
- Prior art date
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Classifications
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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- 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
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- 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
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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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Cardiology (AREA)
- Pulmonology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Transplantation (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Virology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Resultan utiles para el tratamiento y/o prevencion de enfermedades hiperproliferativas tales como cáncer. Los compuestos también son utiles en el tratamiento de: inflamacion, alergia, asma, enfermedades y trastornos del sistema inmunologico, enfermedades y trastornos del sistema nervioso, enfermedades cardiovasculares, enfermedades y trastornos del ojo, enfermedades dermatologicas, osteoporosis, diabetes, esclerosis multiple, e infecciones. Reivindicacion 1: Un compuesto de formula (1) o una sal farmacéuticamente aceptable del mismo, donde: X1 o X2 son cada uno independientemente N o -C(E1)-; X3, X4 y X5 son cada uno independientemente N, O, S, C(E1a)-, o =C(E1)-; siempre y cuando X3 es O o S cuando X4 y X5 se combinan para igualar- C(E1a)=C(E1)-; X5 es NH, O, o S cuando X3 y X4 se combinan para igualar -C(E1a)=C(E1)-; X5 es NH cuando X3 y X4 se combinan para igualar -N=C(E1)-; X5 es NH cuando X3 y X4 se combinan para igualar -C(E1)=N-; Q1 es alquilo C0-10, alquenilo C2-10, alquinilo C2-10, alcoxi C1-10-alquilo C1-10, alcoxi C1-10-alquenilo C2-10, alcoxi C1-10-alquinilo C2-10, alquiltio C1-10- alquilo C1-10, alquiltio C1-10-alquenilo C2-10, alquiltio C1-10-alquinilo C2-10, cicIoaIquilo C3-8, cicloalquenilo C3-8, cicIoalquil C3-8-alquilo C1-10, cicloalquenil C3-8-alquilo C1-10, cicloalquil C3-8-alquenilo C2-10, cicloalquenil C3-8-alqueniIo C2-10, cicloalquil C3-8-aIquinilo C2-10, cicloalquenil C3-8-alquinilo C2-10, heterociclilalquilo C0-10, heterociclilalquenilo C2-10, heterociclilalquinilo C2-10, arilalquilo C0-10, arilalquenilo C2-10, arilalquinilo C2-10, hetarilalquilo C0-10, hetarilalquenilo C2-10, hetarilalquinilo C2-10, heterobicicloalquilo C5-10, espiroalquilo, o heteroespiroalquilo; o -(Z1)n-(Y1)m-R1; cualquiera de los cuales está opcionalmente sustituido con uno o más sustituyentes independientes G1; E1, E1a, y G1 son, en cada caso, cada uno independientemente iguales a halo, -CF3, -OCF3, -OR2, - NR2R3(R4)j1, -C(=O)R2, -CO2R2,-CONR2R3, -NO2, -CN, -S(O)j1R2, -SO2NR2R3, -NR2C(=O)R3, -NR2C(=O)OR3, -NR2C(=O)NR3R4, -NR2S(O)j1R3, -C(=S)0R2, -C(=O)SR2, -NR2C(=NR3)NR4R5, -NR2C(=NR3)OR4, -NR2C(=NR3)SR4, -OC(=O)OR2, -OC(=O)NR2R3, -OC(=O)SR2, - SC(=O)OR2, -SC(=O)NR2R3, alquilo C0-10, alquenilo C2-10, alquinilo C2-10, alcoxi C1-10-alquilo C1-10, alcoxi C1-10-alquenilo C2-10, alcoxi C1-10-alquinilo C2-10, alquiltio C1-10- alquilo C1-10, alquiltio C1-10-alquenilo C2-10, alquiltio C1-10- alquinilo C2-10, cicIoaIquilo C3-8, cicloalquenilo C3-8, cicIoalquil C3-8-alquilo C1-10, cicloalquenil C3-8-alquilo C1-10, cicloalquil C3-8-alquenilo C2-10, cicloalquenil C3-8-alqueniIo C2-10, cicloalquil C3-8-aIquinilo C2-10, cicloalquenil C3-8- alquinilo C2-10, heterociclilalquilo C0-10, heterociclilalquenilo C2-10, heterociclilalquinilo C2-10, arilalquilo C0-10, arilalquenilo C2-10, arilalquinilo C2-10, hetarilalquilo C0-10, hetarilalquenilo C2-10, o hetarilalquinilo C2-10, cualquiera de los cuales está opcionalmente sustituido con uno o más sustituyentes independientes halo, oxo, -CF3, -OCF3, -OR22, -NR22R33(R22a)j1, -C(=O)R22, -CO2R22,-C(=O)NR22R33, -NO2, -CN, -S(=O)j1aR22, -SO2NR22R33, -NR22C(=O)R33, -NR22C(=O)OR33, - NR22C(=O)NR33R22a, -NR22S(O)j1aR22, -C(=S)OR22, -C(=O)SR22, -NR22C(=NR33)NR22aR33a, -NR22C(=NR33)OR22a, -NR22C(=NR33)SR22a, -OC(=O)OR22, -OC(=O)NR22R33, -OC(=O)SR22, -SC(=O)OR22, o -SC(=O)NR22R33, Z1 es cicloalquilo C3-8, heterociclilalquilo C0-10, arilalquilo C0-10, hetarilalquilo C0-10, heterobicicloalquilo C5-10, espiroalquilo, o heteroespiroalquilo, cualquiera de los cuales está opcionalmente sustituido con uno o más sustituyentes G1; Y1 es -O-,-NR6-,-S(O)j2-, -CR6aR7a-, -N(C(O)OR6)-, - N(C(O)R6)- -N(SO2R6)-, -(CR6aR7a)O-, -(CR6aR7a)S-, -(CR6aR7a)N(R6)-, -CR6a(NR6)-,-(CR6aR7a)N(C(O)R6)-, -(CR6aR7a)N(C(O)OR6)-, -(CR6aR7a)N(SO2R6)-, -(CR6a)(NHR6)-(CR6a)(NHC(O)R6)-, -(CR6a)(NHSO2R6)-, -(CR6a)(NHC(O)OR6)-, -(CR6a)(OC(O)R6)-, - (CR6a)(OC(O)NHR6)-, -(CR6a)=(CR6a)-, -C:::C-, -C(=NOR6)-, -C(O)-, -(CR6a)(OR6)-, -C(O)N(R6)-, -N(R6)C(O)-, -N(R6)S(O)-, -N(R6)S(O)2-, -OC(O)N(R6)-, -N(R6)C(O)N(R6a)-,-NR6C(O)O-, -S(O)N(R6)-, -S(O)2N(R6)-, -N(C(O)R6)S(O)-, -N(C(O)R6)S(O)2-, N(R6)S(O)N(R7)-, -N(R6)S(O)2N(R7)-, -C(O)N(R6)C(O)-, -S(O)N(R7)C(O)-, -S(O)2N(R6)C(O)-, -OS(O)N(R6)-, -OS(O)2N(R6)-, -N(R6)S(O)O-, -N(R6)S(O)2O-, -N(R6)S(O)C(O)-, -N(R6)S(O)2C(O)-, -SON(C(O)R6)-, -SO2N(C(O)R6-, -N(R6)SON(R7)-, -N(R6)SO2N(R7)-, - C(O)O-, -N(R6)P(OR7)O-, -N(R6)P(OR7)-, -N(R6)P(O)(OR7)O-, -N(R6)P(O)(OR7)-, -N(C(O)R6)P(OR7)O-, -N(C(O)R6)P(OR7)-, -N(C(O)R6)P(O)(OR7)O-, -N(C(O)R6)P(OR7)-, -(CR6aR7a)S(O)-, -(CR6aR7a)S(O)2-, -(CR6aR7a)N(C(O)OR7)-, -(CR6aR7a)N(C(O)R7)-, - (CR6aR7a)N(SO2R7)-, -(CR6aR7a)C(=NOR7)-, -(CR6aR7a)C(O)-, -(CR6aR7a)(CR6aa)(OR7)-, -(CR6aR7a)C(O)N(R7)-, -(CR6aR7a)N(R6)C(O)-, -(CR6aR7a)N(R7)S(O)-, -(CR6aR7a)N(R7)S(O)2-, -(CR6aR7a)OC(O)N(R7)-, -(CR6aR7a)N(R7)C(O)N(R8)-, -(CR6aR7a)NR7C(O)O-, - (CR6aR7a)S(O)N(R7)-, -(CR6aR7a)S(O)2N(R7)-, -(CR6aR7a)N(C(O)R7)S(O)-, -(CR6aR7a)N(C(O)R7)S(O)-, -(CR6aR7a)N(R7)S(O)N(R8)-, -(CR6aR7a)N(R7)S(O)2N(R8)-, -(CR6aR7a)C(O)N(R7)C(O)-, -(CR6aR7a)S(O)N(R7)C(O)-, -(CR6aR7a)S(O)2N(R7)C(O)-, - (CR6aR7a)OS(O)N(R7)-, -(CR6aR7a)OS(O)2N(R7)-, -(CR6aR7a)N(R7)S(O)O-, -(CR6aR7a)N(R7)S(O)2s-, -(CR6aR7a)N(R7)S(O)C(O)-, -(CR6aR7a)N(R7)S(O)2C(O)-, -(CR6aR7a)SON(C(O)R7)-, -(CR6aR7a)SO2N(C(O)R7)-, -(CR6aR7a)N(R7)SON(R8)-, -(CR6aR7a)N(R7)SO2N(R8)-, - (CR6aR7a)C(O)O-, -(CR6aR7a)N(R7)P(OR8)O-, -(CR6aR7a)N(R7)P(OR8)-, -(CR6aR7a)N(R7)P(O)(OR8)O-, -(CR6aR7a)N(R7)P(O)(OR8)-, -(CR6aR7a)N(C(O)R7)P(OR8)O-, -(CR6aR7a)N(C(O)R7P(OR8)-, -(CR6aR7a)N(C(O)R7P(O)(OR8)O-, o -(CR6aR7a)N(C(O)R7P(OR8)-; R1, R2, R3, R4, R5, R6, R7, R8, R22, R22a, R33, y R33a son, en cada caso, cada uno independientemente alquilo C0-10, alquenilo C2-10, alquinilo C2-10, alcoxi C1-10-alquilo C1-10, alcoxi C1-10-alquenilo C2-10, alcoxi C1-10-alquinilo C2-10, alquiltio C1-10- alquilo C1-10, alquiltio C1-10-alquenilo C2-10, alquiltio C1-10-alquinilo C2-10, cicIoaIquilo C3-8, cicloalquenilo C3-8, cicIoalquil C3-8-alquilo C1-10, cicloalquenil C3-8-alquilo C1-10, cicloalquil C3-8-alquenilo C2-10, cicloalquenil C3-8-alqueniIo C2-10, cicloalquil C3-8-aIquinilo C2-10, cicloalquenil C3-8-alquinilo C2-10, heterociclilalquilo C0-10, heterociclilalquenilo C2-10, heterociclilalquinilo C2-10, arilalquilo C0-10, arilalquenilo C2-10, o arilalquinilo C2-10, hetarilalquilo C0-10, hetarilalquenilo C2-10, o hetarilalquinilo C2-10, cualquiera de los cuales está opcionalmente sustituido con uno o más sustituyentes independientes G11; R6a, R6aa, y R7a son, en cada caso, cada uno independientemente fluor, trifluorometilo, alquilo C0-10, alquenilo C2-10, alquinilo C2-10, alcoxi C1-10-alquilo C1-10, alcoxi C1-10-alquenilo C2-10, alcoxi C1-10-alquinilo C2-10, alquiltio C1-10- alquilo C1-10, alquiltio C1-10-alquenilo C2-10, alquiltio C1-10-alquinilo C2-10, cicIoaIquilo C3-8, cicloalquenilo C3-8, cicIoalquil C3-8-alquilo C1-10, cicloalquenil C3-8-alquilo C1-10, cicloalquil C3-8-alquenilo C2-10, cicloalquenil C3-8-alqueniIo C2-10, cicloalquil C3-8-aIquinilo C2-10, cicloalquenil C3-8-alquinilo C2-10, heterociclilalquilo C0- 10, heterociclilalquenilo C2-10, heterociclilalquinilo C2-10, arilalquilo C0-10, arilalquenilo C2-10, o arilalquinilo C2-10, hetarilalquilo C0-10, hetarilalquenilo C2-10, o hetarilalquinilo C2-10, cualquiera de los cuales está opcionalmente sustituido con uno o más sustituyentes independientes G11a; o en el caso de -NR2R3(R4)j1, -NR3R4, -NR4R5, -NR2bR3b(R4b)j1b, -NR3bR4b, -NR4bR5b, -NR9R10, -NR10R11, -NR11R12, -NR22R33(R22a)J1a, -NR22aR33a, -NR33R22a, -NR6R1, -NR7R1, y -NR8R1 entonces R2 y R3, o R3 y R4, o R4 y R5, R2b y R3b, o R3b y R4b, o R4b y R5b, o R9 y R10, o R10 y R11, o R11y R12, o R22 y R33, o R22a y R33a, o R33 y R22a, o R6 y R1, o R7 y R1, o R8 y R1, respectivamente, se toman opcionalmente junto con el átomo de nitrogeno al cual están unidos para formar un anillo saturado o insaturado de 3 a 10 miembros, donde dicho anillo está opcionalmente sustituido con uno o más sustituyentes independientes G111 y donde dicho anillo opcionalmente incluye uno o más heteroátomos distintos de nitrogeno a los cuales R2 y R3, o R3 y R4, o R4 y R5, R2b y R3b, o R3b y R4b, o R4b y R5b, o R9 y R10, o R10 y R11, o R11 y R12, o R22 y R33, o R22a y R33a, o R33 y R22a, o R6 y R1, o R7 y R1, o R8 y R1 están unidos respectivamente; o en el caso de CR6aR7a, R6a y R7a pueden tomarse junto con el carbono al cual están unidos para formar un anillo cicloalquilo o heterocicloalquilo saturado o insaturado de 3 a 10 miembros, donde dicho anillo está opcionalmente sustituido con uno o más sustituyentes independientes G111a y donde dicho anillo opcionalmente incluye uno o más heteroátomos; G11, G11a, G111, y G111a son, en cada caso, cada uno independientemente halo, -CF3,-OCF3, -OR2b, NR2bR3b(R4b)j1b, - C(=O)R2b, -CO2R2b, -CONR2bR3b, -NO2, -CN, -S(O)j1bR2b, -SO2NR2bR3b, -NR2bC(=O)R3b, -NR2bC(=O)OR3b, -NR2bC(=O)NR3bR4b, -NR2bS(O)j1bR3b, -C(=S)OR2b, -C(=O)SR2b, -NR2bC(=NR3b)NR4bR5b, -NR2bC(=NR3b)OR4b, -NR2bC(=NR3b)SR4b, -OC(=O)OR2b, -OC(=O)NR2bR3b, - OC(=O)SR2b, -SC(=O)OR2b, -SC(=O)NR2bR3b, alquilo C0-10, alquenilo C2-10, alquinilo C2-10, alcoxi C1-10-alquilo C1-10, alcoxi C1-10-alquenilo C2-10, alcoxi C1-10-alquinilo C2-10, alquiltio C1-10- alquilo C1-10, alquiltio C1-10-alquenilo C2-10, alquiltio C1-10-alquinilo C2-10, cicIoaIquilo C3-8, cicloalquenilo C3-8, cicIoalquil C3-8-alquilo C1-10, cicloalquenil C3-8-alquilo C1-10, cicloalquil C3-8-alquenilo C2-10, cicloalquenil C3-8-alqueniIo C2-10, cicloalquil C3-8-aIquinilo C2-10, cicloalquenil C3-8-alquinilo C2-10, heterociclilalquilo C0-10, heterociclilalquenilo C2-10, heterociclilalquinilo C2-10, arilalquilo C0-10, arilalquenilo C2-10, arilalquinilo C2-10, hetarilalquilo C0-10, hetarilalquenilo C2-10, o hetarilalquinilo C2- 10, cualquiera de los cuales está opcionalmente sustituido con uno o más sustituyentes independientes halo, -CF3, -OCF3, -OR9, -NR9R10, -C(O)R9, -CO2R9, -CONR9R10, -NO2, -CN, -S(O)j2aR9, -SO2NR9R10, -NR9C(=O)R10, -NR9C(=O)0R
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US76012406P | 2006-01-19 | 2006-01-19 |
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AR059098A1 true AR059098A1 (es) | 2008-03-12 |
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ARP070100248A AR059098A1 (es) | 2006-01-19 | 2007-01-19 | Inhibidores de quinasa heterobiciclicos fusionados |
Country Status (7)
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US (1) | US20070208053A1 (es) |
EP (1) | EP1979353A2 (es) |
JP (1) | JP2009523812A (es) |
AR (1) | AR059098A1 (es) |
CA (1) | CA2635899A1 (es) |
TW (1) | TW200738709A (es) |
WO (1) | WO2007084667A2 (es) |
Families Citing this family (89)
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MY179032A (en) | 2004-10-25 | 2020-10-26 | Cancer Research Tech Ltd | Ortho-condensed pyridine and pyrimidine derivatives (e.g.purines) as protein kinase inhibitors |
MX2007014619A (es) * | 2005-05-20 | 2009-02-13 | Vertex Pharma | Pirrolopiridinas de utilidad como inhibidores de proteina quinasa. |
CN103214483B (zh) | 2005-12-13 | 2014-12-17 | 因塞特公司 | 作为两面神激酶抑制剂的杂芳基取代的吡咯并[2,3-b]吡啶和吡咯并[2,3-b]嘧啶 |
DK3421471T3 (da) | 2006-04-25 | 2021-06-14 | Astex Therapeutics Ltd | Purin- og deazapurinderivater som farmaceutiske forbindelser |
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US20070208053A1 (en) | 2007-09-06 |
JP2009523812A (ja) | 2009-06-25 |
WO2007084667A2 (en) | 2007-07-26 |
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