AR045686A1 - Derivados de pirido[2,3-b]pirazinas, y su uso como moduladores de quinasas - Google Patents
Derivados de pirido[2,3-b]pirazinas, y su uso como moduladores de quinasasInfo
- Publication number
- AR045686A1 AR045686A1 ARP040101772A ARP040101772A AR045686A1 AR 045686 A1 AR045686 A1 AR 045686A1 AR P040101772 A ARP040101772 A AR P040101772A AR P040101772 A ARP040101772 A AR P040101772A AR 045686 A1 AR045686 A1 AR 045686A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- aryl
- heteroaryl
- cycloalkyl
- heterocyclyl
- Prior art date
Links
- 108091000080 Phosphotransferase Proteins 0.000 title 1
- 102000020233 phosphotransferase Human genes 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 25
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 19
- 125000003118 aryl group Chemical group 0.000 abstract 18
- 125000001072 heteroaryl group Chemical group 0.000 abstract 18
- 125000000623 heterocyclic group Chemical group 0.000 abstract 16
- -1 alkyl radical Chemical class 0.000 abstract 10
- 125000002877 alkyl aryl group Chemical group 0.000 abstract 9
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 abstract 9
- 125000005213 alkyl heteroaryl group Chemical group 0.000 abstract 9
- 125000001424 substituent group Chemical group 0.000 abstract 7
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 229910004727 OSO3H Inorganic materials 0.000 abstract 4
- 229910052794 bromium Inorganic materials 0.000 abstract 4
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 4
- 150000002431 hydrogen Chemical class 0.000 abstract 4
- 229910006074 SO2NH2 Inorganic materials 0.000 abstract 3
- 229910006069 SO3H Inorganic materials 0.000 abstract 3
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 abstract 3
- 229910052801 chlorine Inorganic materials 0.000 abstract 3
- 229910052731 fluorine Inorganic materials 0.000 abstract 3
- 229910052740 iodine Inorganic materials 0.000 abstract 3
- 125000000020 sulfo group Chemical group O=S(=O)([*])O[H] 0.000 abstract 3
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- YEYHFKBVNARCNE-UHFFFAOYSA-N pyrido[2,3-b]pyrazine Chemical class N1=CC=NC2=CC=CN=C21 YEYHFKBVNARCNE-UHFFFAOYSA-N 0.000 abstract 2
- 229910003204 NH2 Inorganic materials 0.000 abstract 1
- 150000005840 aryl radicals Chemical class 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 230000004663 cell proliferation Effects 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 230000003211 malignant effect Effects 0.000 abstract 1
- 238000002483 medication Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 230000001575 pathological effect Effects 0.000 abstract 1
- 150000003254 radicals Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 1
- 125000003107 substituted aryl group Chemical group 0.000 abstract 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
Classifications
-
- 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
-
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
-
- 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
-
- 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)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Dermatology (AREA)
- Urology & Nephrology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Epidemiology (AREA)
- Vascular Medicine (AREA)
- Gastroenterology & Hepatology (AREA)
- Pulmonology (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Derivados de pirido[2,3-b]pirazina, procedimientos para prepararlas y su uso como medicamentos, en especial para el tratamiento de enfermedades malignas y otras enfermedades basadas en proliferaciones celulares patológicas. Reivindicación 1: Derivados de pirido[2,3-b]pirazina de acuerdo con la fórmula (1) caracterizados porque los substituyentes R1-R4 tienen los siguientes significados: R1 y R2 pueden ser, de modo independiente entre sí: (i) hidrógeno (ii) hidroxilo (iii) halógeno (iv) alquilo, en donde el radical alquilo está saturado y puede estar compuesto por 1 a 8 átomos de carbono, (v) arilo insubstituido o substituido, en donde el radical arilo puede estar mono o polisubstituido, igual o diferente, con F, Cl, Br, I, CF3, CN, NH2, NH-alquilo, NH-cicloalquilo, NH-heterociclilo, NH-arilo, NH-heteroarilo, NH-alquil-cicloalquilo, NH-alquil-heterociclilo, NH-alquil-arilo, NH-alquil-heteroarilo, NH-alquil-NH2, NH-alquil-OH, N(alquilo)2, NHC(O)-alquilo, NHC(O)-cicloalquilo, NHC(O)-heterociclilo, NHC(O)-arilo, NHC(O)-heteroarilo, NHC(O)-alquil-arilo, NHC(O)-alquil-heteroarilo, NHSO2-alquilo, NHSO2-cicloalquilo, NHSO2-heterociclilo, NHSO2-arilo, NHSO2-heteroarilo, NHSO2-alquil-arilo, NHSO2-alquil-heteroarilo, NO2, SH, S-alquilo, S-arilo, S-heteroarilo, OH, OCF3, O-alquilo, O-cicloalquilo, O-heterociclilo, O-arilo, O-heteroarilo, O-alquil-cicloalquilo, O-alquil-heterociclilo, O-alquil-arilo, O-alquil-heteroarilo, O-alquil-OH, O-(CH2)n-O, OC(O)-alquilo, OC(O)-cicloalquilo, OC(O)-heterociclilo, OC(O)-arilo, OC(O)-heteroarilo, OC(O)-alquil-arilo, OC(O)-alquil-heteroarilo, OSO3H, OSO2-alquilo, OSO2-cicloalquilo, OSO2-heterociclilo, OSO2-arilo, OSO2-heteroarilo, OSO2-alquil-arilo, OSO2-alquil-heteroarilo, OP(O)(OH)2, C(O)-alquilo, C(O)-arilo, C(O)-heteroarilo, CO2H, CO2-alquilo, CO2-cicloalquilo, CO2-heterociclilo, CO2-arilo, CO2-heteroarilo, CO2-alquil-cicloalquilo, CO2-alquil-heterociclilo, CO2-alquil-arilo, CO2-alquil-heteroarilo, C(O)-NH2, C(O)NH-alquilo, C(O)NH-cicloalquilo, C(O)NH-heterociclilo, C(O)NH-arilo, C(O)NH-heteroarilo, C(O)NH-alquil-cicloalquilo, C(O)NH-alquil-heterociclilo, C(O)NH-alquil-arilo, C(O)NH-alquil-heteroarilo, C(O)N(alquilo)2, C(O)N(cicloalquilo)2, C(O)N(arilo)2, C(O)N(heteroarilo)2, SO-alquilo, SO-arilo, SO2-alquilo, SO2-arilo, SO2NH2, SO2NH-alquilo, SO2NH-arilo, SO2NH-heteroarilo, SO2NH-alquil-arilo, SO3H, SO2O-alquilo, SO2O-arilo, SO2O-alquil-arilo, alquilo, cicloalquilo, heterociclilo, arilo o heteroarilo, n puede adoptar el valor 1,2 o 3 y los substituyentes de alquilo, cicloalquilo, heterociclilo, arilo, heteroarilo, alquil-cicloalquilo, alquil-heterociclilo, alquilarilo y alquil-heteroarilo pueden estar, a su vez, substituidos, (vi) heteroarilo insubstituido o substituido, en donde el radical heteroarilo puede estar mono o polisubstituido, igual o diferente, con F, Cl, Br, I, CF3, CN, NH2, NH-alquilo, NH-cicloalquilo, NH-heterociclilo, NH-arilo, NH-heteroarilo, NH-alquil-cicloalquilo, NH-alquil-heterociclilo, NH-alquil-arilo, NH-alquil-heteroarilo, NH-alquil-NH2, NH-alquil-OH, N(alquilo)2, NHC(O)-alquilo, NHC(O)-cicloalquilo, NHC(O)-heterociclilo, NHC(O)-arilo, NHC(O)-heteroarilo, NHC(O)-alquil-arilo, NHC(O)-alquil-heteroarilo, NHSO2-alquilo, NHSO2-cicloalquilo, NHSO2-heterociclilo, NHSO2-arilo, NHSO2-heteroarilo, NHSO2-alquil-arilo, NHSO2-alquil-heteroarilo, NO2, SH, S-alquilo, S-arilo, S-heteroarilo, OH, OCF3, O-alquilo, O-cicloalquilo, O-arilo, O-heteroarilo, O-alquil-cicloalquilo, O-alquil-arilo, O-alquil-heteroarilo, OC(O)-alquilo, OC(O)-cicloalquilo, OC(O)-heterociclilo, OC(O)-arilo, OC(O)-heteroarilo, OC(O)-alquil-arilo, OC(O)-alquil-heteroarilo, OSO3H, OSO2-alquilo, OSO2-cicloalquilo, OSO2-arilo, OSO2-heteroarilo, OSO2-alquil-arilo, OSO2-alquil-heteroarilo, OP(O)(OH)2, C(O)-alquilo, C(O)-arilo, C(O)-heteroarilo, CO2H, CO2-alquilo, CO2-cicloalquilo, CO2-heterociclilo, CO2-arilo, CO2-heteroarilo, CO2-alquil-cicloalquilo, CO2-alquil-heterociclilo, CO2-alquil-arilo, CO2-alquil-heteroarilo, C(O)-NH2, C(O)NH-alquilo, C(O)NH-cicloalquilo, C(O)NH-heterociclilo, C(O)NH-arilo, C(O)NH-heteroarilo, C(O)NH-alquil-cicloalquilo, C(O)NH-alquil-heterociclilo, C(O)NH-alquil-arilo, C(O)NH-alquil-heteroarilo, C(O)N(alquilo)2, C(O)N(cicloalquilo)2, C(O)N(arilo)2, C(O)N(heteroarilo)2, SO2NH2, SO2NH-alquilo, SO2NH-arilo, SO2NH-heteroarilo, SO2NH-alquil-arilo, SO3H, SO2O-alquilo, SO2O-arilo, SO2O-alquil-arilo, alquilo, cicloalquilo, heterociclilo, arilo o heteroarilo, y los substituyentes de alquilo, cicloalquilo, heterociclilo, arilo, heteroarilo, pueden estar, a su vez, substituidos, (vii) OR5, en donde R5 puede ser alquilo, cicloalquilo, heterociclilo, arilo, heteroarilo, alquilcicloalquilo, alquil-heterociclilo, alquil-arilo o alquil-heteroarilo, y los substituyentes de alquilo, cicloalquilo, heterociclilo, arilo, heteroarilo, alquilcicloalquilo, alquil-heterociclilo, alquil-arilo o alquil-heteroarilo, pueden estar, a su vez, substituidos, (viii) SR6, en donde R6 puede ser alquilo, cicloalquilo, heterociclilo, arilo, heteroarilo, alquilcicloalquilo, alquil-heterociclilo, alquil-arilo o alquil-heteroarilo, y los substituyentes de alquilo, cicloalquilo, heterociclilo, arilo, heteroarilo, alquilcicloalquilo, alquil-heterociclilo, alquil-arilo o alquil-heteroarilo, pueden estar, a su vez, substituidos, (ix) NR7R8, en donde R7 y R8 pueden ser, de modo independiente entre sí, hidrógeno, alquilo, cicloalquilo, heterociclilo, arilo, heteroarilo, alquil-cicloalquilo, alquil-heterociclilo, alquil-arilo o alquil-heteroarilo, y los substituyentes de alquilo, cicloalquilo, heterociclilo, arilo, heteroarilo, alquilcicloalquilo, alquil-heterociclilo, alquil-arilo o alquil-heteroarilo, pueden estar, a su vez, substituidos, o R7 y R8 significan juntos cicloalquilo o heterociclilo, en donde cicloalquilo y heterociclilo pueden estar, a su vez, substituidos. R3 y R4 pueden significar, de modo independiente entre sí, hidrógeno o NR9R10, con la condición de que, cuando R3 = NR9R10, R4 = H, y cuando R4 = NR9R10, R3 = H, en donde R9 puede ser hidrógeno, alquilo, cicloalquilo, heterociclilo, arilo, heteroarilo, alquilcicloalquilo, alquil-heterociclilo, alquil-arilo o alquil-heteroarilo, y los substituyentes de alquilo, cicloalquilo, heterociclilo, arilo, heteroarilo, alquilcicloalquilo, alquil-heterociclilo, alquil-arilo o alquil-heteroarilo, pueden estar, a su vez, substituidos, y R10 puede significar -C(Y)NR11R12, en donde Y = O, S y R11 y R12 son de modo independiente entre sí, (i) hidrógeno, (ii) alquilo insubstituido o substituido, en donde el radical alquilo puede estar mono o polisubstituido, igual o diferente, con F, CI, Br, I, CF3, CN, NH2, NH-alquilo, NH-cicloalquilo, NH-heterociclilo, NH-arilo, NH-heteroarilo, NH-alquil-cicloalquilo, NH-alquil-heterociclilo, NH-alquil-arilo, NH-alquil-heteroarilo, N(alquilo)2, NHC(O)-alquilo, NHC(O)-cicloalquilo, NHC(O)-heterociclilo, NHC(O)-arilo, NHC(O)-heteroarilo, NHC(O)-alquil-arilo, NHC(O)-alquil-heteroarilo, NHSO2-alquilo, NHSO2-cicloalquilo, NHSO2-heterociclilo, NHSO2-arilo, NHSO2-heteroarilo, NHSO2-alquil-arilo, NHSO2-alquil-heteroarilo, NO2, SH, S-alquilo, S-cicloalquilo, S-heterociclilo, S-arilo, S-heteroarilo, OH, OCF3, O-alquilo, O-cicloalquilo, O-heterociclilo, O-arilo, O-heteroarilo, O-alquil-cicloalquilo, O-alquil-heterociclilo, O-alquil-arilo, O-alquil-heteroarilo, OC(O)-alquilo, OC(O)-cicloalquilo, OC(O)-heterociclilo, OC(O)-arilo, OC(O)-heteroarilo, OC(O)-alquil-arilo, OC(O)-alquil-heteroarilo, OSO3H, OSO2-alquilo, OSO2-cicloalquilo, OSO2-heterociclilo, OSO2-arilo, OSO2-heteroarilo, OSO2-alquil-arilo, OSO2-alquil-heteroarilo, OP(O)(OH)2, C(O)-alquilo, C(O)-arilo, C(O)-heteroarilo, CO2H, CO2-alquilo, CO2-cicloalquilo, CO2-heterociclilo, CO2-arilo, CO2-heteroarilo, CO2-alquil-cicloalquilo, CO2-alquil-heterociclilo, CO2-alquil-arilo, CO2-alquil-heteroarilo, C(O)-NH2, C(O)NH-alquilo, C(O)NH-cicloalquilo, C(O)NH-heterociclilo, C(O)NH-arilo, C(O)NH-heteroarilo, C(O)NH-alquil-cicloalquilo, C(O)NH-alquil-heterociclilo, C(O)NH-alquil-arilo, C(O)NH-alquil-heteroarilo, C(O)N(alquilo)2, C(O)N(cicloalquilo)2, C(O)N(arilo)2, C(O)N(heteroarilo)2, SO-alquilo, SO-arilo, SO2-alquilo, SO2-arilo, SO2NH2, SO2NH-alquilo, SO2NH-arilo, SO2NH-heteroarilo, SO2NH-alquil-arilo, SO3H, SO2O-alquilo, SO2O-arilo, SO2O-alquil-arilo, cicloalquilo, heterociclilo, arilo o heteroarilo, (iii) cicloalquilo insubstituido o substituido, en donde el radical cicloalquilo puede estar mono o polisubstituido, igual o diferente, con F, Cl, Br, I, NH2, NH-alquilo, NH-cicloalquilo, NH-heterociclilo, NH-arilo, NH-heteroarilo, NH-alquil-arilo, NH-alquil-heteroarilo, N(alquilo)2, NHC(O)-alquilo, NHC(O)-cicloalquilo, NHC(O)-heterociclilo, NHC(O)-arilo, NHC(O)-heteroarilo, NHC(O)-alquil-arilo, NHC(O)-alquil-heteroarilo, NHSO2-alquilo, NHSO2-cicloalquilo, NHSO2-heterociclilo, NHSO2-arilo, NHSO2-heteroarilo, NHSO2-alquil-arilo, NHSO2-alquil-heteroarilo, OH, O-alquilo, O-cicloalquilo, O-heterociclilo, O-arilo, O-heteroarilo, O-alquil-arilo, O-alquil-heteroarilo, OC(O)-alquilo, OC(O)-cicloalquilo, OC(O)-heterociclilo, OC(O)-arilo, OC(O)-heteroarilo, OC(O)-alquil-arilo, OC(O)-alquil-heteroarilo, OSO3H, OSO2-alquilo, OSO2-cicloalquilo, OSO2-heterociclilo, OSO2-arilo, OSO2-heteroarilo, OSO2-alquil-arilo, OSO2-alquil-heteroarilo, OP(O)(OH)2, CO2H, CO2-alquilo, CO2-cicloalquilo, CO2-heterociclilo, CO2-arilo, CO2-heteroarilo, CO2-alquil-cicloalquilo, CO2-alquil-heterociclilo, CO2-alquil-arilo, CO2-alquil-heteroarilo, C(O)-NH2, C(O)NH-alquilo, C(O)NH-cicloalquilo, C(O)NH-heterociclilo, C(O)NH-arilo, C(O)NH-heteroarilo, C(O)NH-alquil-cicloalquilo, C(O)NH-alquil-heterociclilo, C(O)NH-alquil-arilo, C(O)NH-alquil-heteroarilo, C(O)N(alquilo)2, C(O)N(cicloalquilo)2, C(O)N(arilo)2, C(O)N(heteroarilo)2, alquilo o arilo, (iv) heterociclilo insubstituido o substituido, en donde el radical heterociclilo puede estar mono o polisubstituido, igual o diferente, con OH, O-alquilo, O-arilo, NH2, NH-alquilo, NH-arilo, alquilo, alquil-aril
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10323345A DE10323345A1 (de) | 2003-05-23 | 2003-05-23 | Neue Pyridopyrazine und deren Verwendung als Kinase-Inhibitoren |
| DE102004022383A DE102004022383A1 (de) | 2004-05-06 | 2004-05-06 | Neue Pyridopyrazine und deren Verwendung als Modulatoren von Kinasen |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR045686A1 true AR045686A1 (es) | 2005-11-09 |
Family
ID=33477517
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP040101772A AR045686A1 (es) | 2003-05-23 | 2004-05-21 | Derivados de pirido[2,3-b]pirazinas, y su uso como moduladores de quinasas |
Country Status (25)
| Country | Link |
|---|---|
| US (1) | US7276507B2 (es) |
| EP (1) | EP1636228B1 (es) |
| JP (2) | JP4571944B2 (es) |
| KR (1) | KR101111464B1 (es) |
| AR (1) | AR045686A1 (es) |
| AT (1) | ATE411992T1 (es) |
| AU (1) | AU2004240747B2 (es) |
| BR (1) | BRPI0410633A (es) |
| CA (1) | CA2524525C (es) |
| CY (1) | CY1108715T1 (es) |
| DE (1) | DE502004008322D1 (es) |
| DK (1) | DK1636228T3 (es) |
| ES (1) | ES2316985T3 (es) |
| HR (1) | HRP20090036T3 (es) |
| ME (1) | ME00541B (es) |
| MX (1) | MXPA05012645A (es) |
| NO (1) | NO332005B1 (es) |
| NZ (1) | NZ544112A (es) |
| PL (1) | PL1636228T3 (es) |
| PT (1) | PT1636228E (es) |
| RU (1) | RU2330851C9 (es) |
| SI (1) | SI1636228T1 (es) |
| TW (1) | TWI341839B (es) |
| UA (1) | UA78929C2 (es) |
| WO (1) | WO2004104003A1 (es) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2006216998B2 (en) * | 2005-02-14 | 2010-12-23 | Merck Sharp & Dohme Corp. | Inhibitors of Akt activity |
| AU2006313701B2 (en) * | 2005-11-11 | 2012-05-31 | Aeterna Zentaris Gmbh | Novel pyridopyrazines and their use as modulators of kinases |
| US8217042B2 (en) | 2005-11-11 | 2012-07-10 | Zentaris Gmbh | Pyridopyrazines and their use as modulators of kinases |
| EP1785423A1 (de) * | 2005-11-11 | 2007-05-16 | Zentaris GmbH | Neue Pyridopyrazine und deren Verwendung als Modulatoren von Kinasen |
| EP1790342A1 (de) * | 2005-11-11 | 2007-05-30 | Zentaris GmbH | Pyridopyrazin-Derivate und deren Verwendung als Modulatoren der Signaltransduktionswege |
| JO2985B1 (ar) | 2006-12-20 | 2016-09-05 | Takeda Pharmaceuticals Co | مثبطات كينازmapk/erk |
| EP1990342A1 (en) | 2007-05-10 | 2008-11-12 | AEterna Zentaris GmbH | Pyridopyrazine Derivatives, Process of Manufacturing and Uses thereof |
| KR20120082906A (ko) | 2009-09-30 | 2012-07-24 | 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 | 자가포식현상-향상 유전자 생성물의 조절을 통한 자가포식현상의 조절 방법 |
| GB201007286D0 (en) | 2010-04-30 | 2010-06-16 | Astex Therapeutics Ltd | New compounds |
| GB201020179D0 (en) | 2010-11-29 | 2011-01-12 | Astex Therapeutics Ltd | New compounds |
| EP2508184A1 (en) * | 2011-04-06 | 2012-10-10 | Æterna Zentaris GmbH | Pyridopyrazine derivatives and their use |
| GB201118654D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201118652D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201118656D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201118675D0 (en) | 2011-10-28 | 2011-12-14 | Astex Therapeutics Ltd | New compounds |
| GB201209613D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| GB201209609D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| GB201307577D0 (en) | 2013-04-26 | 2013-06-12 | Astex Therapeutics Ltd | New compounds |
| MA39784B1 (fr) | 2014-03-26 | 2021-03-31 | Astex Therapeutics Ltd | Combinaisons des inhibiteurs du fgfr et du cmet destinées au traitement du cancer |
| AU2015238305B2 (en) | 2014-03-26 | 2020-06-18 | Astex Therapeutics Ltd | Combinations of an FGFR inhibitor and an IGF1R inhibitor |
| JO3512B1 (ar) | 2014-03-26 | 2020-07-05 | Astex Therapeutics Ltd | مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز |
| JO3695B1 (ar) | 2015-02-10 | 2020-08-27 | Astex Therapeutics Ltd | تركيبات صيدلانية تشتمل على n- (3.5- ثنائي ميثوكسي فينيل)-n-(1-ميثيل إيثيل)-n- 3-( ميثيل-h1-بيرازول-4-يل) كينوكسالين-6-يل) إيثان- 1.2-ثنائي الأمين) |
| US10478494B2 (en) | 2015-04-03 | 2019-11-19 | Astex Therapeutics Ltd | FGFR/PD-1 combination therapy for the treatment of cancer |
| KR102703498B1 (ko) | 2015-09-23 | 2024-09-04 | 얀센 파마슈티카 엔브이 | 신규 화합물 |
| CN108137546B (zh) | 2015-09-23 | 2021-07-27 | 詹森药业有限公司 | 双杂芳基取代的1,4-苯并二氮杂卓化合物及其用于治疗癌症的用途 |
| US11117894B2 (en) | 2017-06-22 | 2021-09-14 | City Of Hope | Pyridopyrazine compounds and uses thereof |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9413975D0 (en) * | 1994-07-11 | 1994-08-31 | Fujisawa Pharmaceutical Co | New heterobicyclic derivatives |
| TW274550B (es) * | 1992-09-26 | 1996-04-21 | Hoechst Ag | |
| US5700823A (en) * | 1994-01-07 | 1997-12-23 | Sugen, Inc. | Treatment of platelet derived growth factor related disorders such as cancers |
| UA71555C2 (en) * | 1997-10-06 | 2004-12-15 | Zentaris Gmbh | Methods for modulating function of serine/threonine protein kinases by 5-azaquinoline derivatives |
| WO2003024448A2 (en) | 2001-09-14 | 2003-03-27 | Methylgene, Inc. | Inhibitors of histone deacetylase |
| WO2003086394A1 (en) | 2002-04-08 | 2003-10-23 | Merck & Co., Inc. | Inhibitors of akt activity |
| US20060142178A1 (en) * | 2002-04-08 | 2006-06-29 | Barnett Stanley F | Method of treating cancer |
| WO2003086403A1 (en) | 2002-04-08 | 2003-10-23 | Merck & Co., Inc. | Inhibitors of akt activity |
| EP1538907A4 (en) | 2002-07-02 | 2008-12-24 | Southern Res Inst | FTSZ-HEMMER AND ITS USE |
| BR0315053A (pt) | 2002-10-03 | 2005-08-09 | Targegen Inc | Agentes vasculostáticos , composição, artigo e processo de preparação dos mesmos |
| DE10323345A1 (de) * | 2003-05-23 | 2004-12-16 | Zentaris Gmbh | Neue Pyridopyrazine und deren Verwendung als Kinase-Inhibitoren |
-
2004
- 2004-05-19 ME MEP-2008-831A patent/ME00541B/me unknown
- 2004-05-19 PT PT04733768T patent/PT1636228E/pt unknown
- 2004-05-19 SI SI200431009T patent/SI1636228T1/sl unknown
- 2004-05-19 CA CA2524525A patent/CA2524525C/en not_active Expired - Fee Related
- 2004-05-19 DK DK04733768T patent/DK1636228T3/da active
- 2004-05-19 KR KR1020057022424A patent/KR101111464B1/ko not_active Expired - Fee Related
- 2004-05-19 JP JP2006529872A patent/JP4571944B2/ja not_active Expired - Fee Related
- 2004-05-19 WO PCT/EP2004/005388 patent/WO2004104003A1/de not_active Ceased
- 2004-05-19 RU RU2005140377/04A patent/RU2330851C9/ru not_active IP Right Cessation
- 2004-05-19 EP EP04733768A patent/EP1636228B1/de not_active Expired - Lifetime
- 2004-05-19 AT AT04733768T patent/ATE411992T1/de active
- 2004-05-19 HR HR20090036T patent/HRP20090036T3/xx unknown
- 2004-05-19 DE DE502004008322T patent/DE502004008322D1/de not_active Expired - Lifetime
- 2004-05-19 NZ NZ544112A patent/NZ544112A/en not_active IP Right Cessation
- 2004-05-19 PL PL04733768T patent/PL1636228T3/pl unknown
- 2004-05-19 UA UAA200510686A patent/UA78929C2/uk unknown
- 2004-05-19 MX MXPA05012645A patent/MXPA05012645A/es active IP Right Grant
- 2004-05-19 ES ES04733768T patent/ES2316985T3/es not_active Expired - Lifetime
- 2004-05-19 AU AU2004240747A patent/AU2004240747B2/en not_active Ceased
- 2004-05-19 BR BRPI0410633-4A patent/BRPI0410633A/pt not_active IP Right Cessation
- 2004-05-20 TW TW093114324A patent/TWI341839B/zh not_active IP Right Cessation
- 2004-05-21 US US10/851,976 patent/US7276507B2/en not_active Expired - Fee Related
- 2004-05-21 AR ARP040101772A patent/AR045686A1/es not_active Application Discontinuation
-
2005
- 2005-12-19 NO NO20056032A patent/NO332005B1/no not_active IP Right Cessation
-
2009
- 2009-01-21 CY CY20091100081T patent/CY1108715T1/el unknown
-
2010
- 2010-07-01 JP JP2010150895A patent/JP5447855B2/ja not_active Expired - Fee Related
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR045685A1 (es) | Piridopirazinas, procedimiento para prepararlas y su uso como inhibidores de quinasas | |
| AR056216A1 (es) | Derivados de piridopirazina y su uso | |
| HRP20090036T3 (en) | Novel pyridopyrazines and use thereof as kinase modulators | |
| AR085844A1 (es) | Derivados de piridopirazina y sus usos | |
| SU650510A3 (ru) | Способ получени водорастворимых моноазокрасителей 2,6-диаминопиридинового р да | |
| DE59510140D1 (de) | Heterocyclische Carbene enthaltende Metallkomplexverbindungen | |
| DK172889A (da) | Triaza makrocykliske forbindelser og metalkomplekser deraf | |
| RU2007123025A (ru) | Способ предсказуемого окрашивания кератиновых волокон нанесением композиции, содержащей производное диамино-n, n-дигидропиразолона, и основной композиции или композиции с золотистым отливом | |
| ES2370353T3 (es) | Mezclas de tintura dispersas que poseen un alto grado de firmeza ante la luz. | |
| DK147095B (da) | Haarfarvemiddel paa basis af oxydationsfarvestoffer og tetraaminopyrimidiner som fremkalderstoffer | |
| AR075935A1 (es) | Derivados de quinoxalina y su uso para el tratamiento de tumores benignos y malignos | |
| ATE207937T1 (de) | Wasserlösliche polymerisate und deren verwendung in kosmetischen formulierungen | |
| IT9047624A1 (it) | Derivato di 1, 2-etandiolo e suo sale, procedimento per produrli ed applicarli ed agente migliorante la funzione cerebrale che li contiene | |
| EP0455380A3 (en) | Tetra-aza macrocycles; processes for their preparation, and their use in magnetic resonance imaging | |
| BR0007953A (pt) | Tintas para tingimento em preto e seu uso | |
| JP2849198B2 (ja) | 分散染料組成物及び疎水性繊維の染色法 | |
| ES2686508T3 (es) | Emisor fosforescente binuclear de metales del grupo principal | |
| ES475254A1 (es) | Un procedimiento para la preparacion de colorantes monoazo amarillos insolubles en agua. | |
| Walsh | Padé approximants as limits of rational functions of best approximation | |
| Leygue et al. | New advances in the synthesis of tripyridinophane macrocycles suitable to enhance the luminescence of Ln (III) ions in aqueous solution | |
| US3870696A (en) | Benzthiazole-azo-(4-n-sulfopropyl)phenyl compounds | |
| KR960022859A (ko) | 청색계 반응 염료 조성물 및 이를 배합하여 이루어지는 염료 조성물 | |
| GB1121367A (en) | Readily dispersible inorganic pulverous compositions and process for their production | |
| GB1471478A (en) | Scarcely soluble monoazo compounds | |
| Hasegawa et al. | The Electron Spin Resonance of the Trinuclear Vanadyl Pyrophosphate Complex |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration | ||
| FD | Application declared void or lapsed, e.g., due to non-payment of fee |