ME00541B - NOVI PIRIDOPIRAZINI I NJlUHOVA UPOTREBA KAO MODULATORA KlNAZA - Google Patents
NOVI PIRIDOPIRAZINI I NJlUHOVA UPOTREBA KAO MODULATORA KlNAZAInfo
- Publication number
- ME00541B ME00541B MEP-2008-831A MEP83108A ME00541B ME 00541 B ME00541 B ME 00541B ME P83108 A MEP83108 A ME P83108A ME 00541 B ME00541 B ME 00541B
- Authority
- ME
- Montenegro
- 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
- YEYHFKBVNARCNE-UHFFFAOYSA-N pyrido[2,3-b]pyrazine Chemical class N1=CC=NC2=CC=CN=C21 YEYHFKBVNARCNE-UHFFFAOYSA-N 0.000 claims abstract 7
- 201000010099 disease Diseases 0.000 claims abstract 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract 5
- 239000003814 drug Substances 0.000 claims abstract 5
- 230000004663 cell proliferation Effects 0.000 claims abstract 3
- 230000003211 malignant effect Effects 0.000 claims abstract 3
- 230000001575 pathological effect Effects 0.000 claims abstract 3
- -1 alkyl radical Chemical class 0.000 claims 32
- 125000000217 alkyl group Chemical group 0.000 claims 31
- 125000003118 aryl group Chemical group 0.000 claims 29
- 125000000623 heterocyclic group Chemical group 0.000 claims 28
- 125000000753 cycloalkyl group Chemical group 0.000 claims 25
- UDJFFSGCRRMVFH-UHFFFAOYSA-N pyrido[2,3-d]pyrimidine Chemical compound N1=CN=CC2=CC=CN=C21 UDJFFSGCRRMVFH-UHFFFAOYSA-N 0.000 claims 17
- 125000001072 heteroaryl group Chemical group 0.000 claims 15
- 229910052794 bromium Inorganic materials 0.000 claims 14
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 14
- 229910052801 chlorine Inorganic materials 0.000 claims 14
- 229910052731 fluorine Inorganic materials 0.000 claims 14
- UMGDCJDMYOKAJW-UHFFFAOYSA-N thiourea Chemical compound NC(N)=S UMGDCJDMYOKAJW-UHFFFAOYSA-N 0.000 claims 14
- 229910006074 SO2NH2 Inorganic materials 0.000 claims 11
- 229910006069 SO3H Inorganic materials 0.000 claims 11
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 11
- 125000000020 sulfo group Chemical group O=S(=O)([*])O[H] 0.000 claims 11
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 11
- 125000002877 alkyl aryl group Chemical group 0.000 claims 10
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 claims 9
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Natural products NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims 7
- 229910004727 OSO3H Inorganic materials 0.000 claims 6
- 150000001875 compounds Chemical class 0.000 claims 6
- 150000002431 hydrogen Chemical class 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 239000001257 hydrogen Substances 0.000 claims 6
- 125000005213 alkyl heteroaryl group Chemical group 0.000 claims 4
- 150000005840 aryl radicals Chemical class 0.000 claims 4
- 229940079593 drug Drugs 0.000 claims 4
- 125000003107 substituted aryl group Chemical group 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 3
- 125000000547 substituted alkyl group Chemical group 0.000 claims 3
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 3
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 230000004715 cellular signal transduction Effects 0.000 claims 2
- 150000004677 hydrates Chemical class 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 230000003472 neutralizing effect Effects 0.000 claims 2
- 230000021603 oncosis Effects 0.000 claims 2
- 239000008024 pharmaceutical diluent Substances 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- PXIZXHKMENZVJC-UHFFFAOYSA-N 1-methyl-3-(3-phenylpyrido[2,3-b]pyrazin-6-yl)thiourea Chemical compound N=1C2=NC(NC(=S)NC)=CC=C2N=CC=1C1=CC=CC=C1 PXIZXHKMENZVJC-UHFFFAOYSA-N 0.000 claims 1
- KKVYYGGCHJGEFJ-UHFFFAOYSA-N 1-n-(4-chlorophenyl)-6-methyl-5-n-[3-(7h-purin-6-yl)pyridin-2-yl]isoquinoline-1,5-diamine Chemical compound N=1C=CC2=C(NC=3C(=CC=CN=3)C=3C=4N=CNC=4N=CN=3)C(C)=CC=C2C=1NC1=CC=C(Cl)C=C1 KKVYYGGCHJGEFJ-UHFFFAOYSA-N 0.000 claims 1
- 206010003210 Arteriosclerosis Diseases 0.000 claims 1
- 125000006519 CCH3 Chemical group 0.000 claims 1
- ZEOWTGPWHLSLOG-UHFFFAOYSA-N Cc1ccc(cc1-c1ccc2c(n[nH]c2c1)-c1cnn(c1)C1CC1)C(=O)Nc1cccc(c1)C(F)(F)F Chemical compound Cc1ccc(cc1-c1ccc2c(n[nH]c2c1)-c1cnn(c1)C1CC1)C(=O)Nc1cccc(c1)C(F)(F)F ZEOWTGPWHLSLOG-UHFFFAOYSA-N 0.000 claims 1
- 102100023593 Fibroblast growth factor receptor 1 Human genes 0.000 claims 1
- 101710182386 Fibroblast growth factor receptor 1 Proteins 0.000 claims 1
- 206010016654 Fibrosis Diseases 0.000 claims 1
- 241000282412 Homo Species 0.000 claims 1
- 101001034652 Homo sapiens Insulin-like growth factor 1 receptor Proteins 0.000 claims 1
- 101001059454 Homo sapiens Serine/threonine-protein kinase MARK2 Proteins 0.000 claims 1
- 102100039688 Insulin-like growth factor 1 receptor Human genes 0.000 claims 1
- 101000913968 Ipomoea purpurea Chalcone synthase C Proteins 0.000 claims 1
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 claims 1
- 108091054455 MAP kinase family Proteins 0.000 claims 1
- 102000043136 MAP kinase family Human genes 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 101100381978 Mus musculus Braf gene Proteins 0.000 claims 1
- 101100335081 Mus musculus Flt3 gene Proteins 0.000 claims 1
- 101000907988 Petunia hybrida Chalcone-flavanone isomerase C Proteins 0.000 claims 1
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 claims 1
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 claims 1
- 102000016971 Proto-Oncogene Proteins c-kit Human genes 0.000 claims 1
- 108010014608 Proto-Oncogene Proteins c-kit Proteins 0.000 claims 1
- 108010029869 Proto-Oncogene Proteins c-raf Proteins 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 101710113459 RAC-alpha serine/threonine-protein kinase Proteins 0.000 claims 1
- 102100033479 RAF proto-oncogene serine/threonine-protein kinase Human genes 0.000 claims 1
- 102100028904 Serine/threonine-protein kinase MARK2 Human genes 0.000 claims 1
- 150000007513 acids Chemical class 0.000 claims 1
- 125000000641 acridinyl group Chemical group C1(=CC=CC2=NC3=CC=CC=C3C=C12)* 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 229960001748 allylthiourea Drugs 0.000 claims 1
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 claims 1
- 208000011775 arteriosclerosis disease Diseases 0.000 claims 1
- 150000007514 bases Chemical class 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 125000004369 butenyl group Chemical group C(=CCC)* 0.000 claims 1
- 125000000480 butynyl group Chemical group [*]C#CC([H])([H])C([H])([H])[H] 0.000 claims 1
- 239000004202 carbamide Substances 0.000 claims 1
- 125000000609 carbazolyl group Chemical group C1(=CC=CC=2C3=CC=CC=C3NC12)* 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 230000033077 cellular process Effects 0.000 claims 1
- 230000007882 cirrhosis Effects 0.000 claims 1
- 208000019425 cirrhosis of liver Diseases 0.000 claims 1
- 239000012059 conventional drug carrier Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000005469 ethylenyl group Chemical group 0.000 claims 1
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000006038 hexenyl group Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 1
- 125000003406 indolizinyl group Chemical group C=1(C=CN2C=CC=CC12)* 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 150000007529 inorganic bases Chemical class 0.000 claims 1
- 125000001972 isopentyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])C([H])([H])* 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 150000007522 mineralic acids Chemical class 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 125000001280 n-hexyl group Chemical group C(CCCCC)* 0.000 claims 1
- 125000000740 n-pentyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 125000001971 neopentyl group Chemical group [H]C([*])([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 125000004365 octenyl group Chemical group C(=CCCCCCC)* 0.000 claims 1
- 150000007524 organic acids Chemical class 0.000 claims 1
- 235000005985 organic acids Nutrition 0.000 claims 1
- 150000007530 organic bases Chemical class 0.000 claims 1
- 230000002611 ovarian Effects 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 125000002255 pentenyl group Chemical group C(=CCCC)* 0.000 claims 1
- 125000006194 pentinyl group Chemical group 0.000 claims 1
- 239000008177 pharmaceutical agent Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 125000001791 phenazinyl group Chemical group C1(=CC=CC2=NC3=CC=CC=C3N=C12)* 0.000 claims 1
- 125000001484 phenothiazinyl group Chemical group C1(=CC=CC=2SC3=CC=CC=C3NC12)* 0.000 claims 1
- 125000004592 phthalazinyl group Chemical group C1(=NN=CC2=CC=CC=C12)* 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 244000144977 poultry Species 0.000 claims 1
- 125000006238 prop-1-en-1-yl group Chemical group [H]\C(*)=C(/[H])C([H])([H])[H] 0.000 claims 1
- 125000004368 propenyl group Chemical group C(=CC)* 0.000 claims 1
- 125000002568 propynyl group Chemical group [*]C#CC([H])([H])[H] 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 125000004944 pyrazin-3-yl group Chemical group [H]C1=C([H])N=C(*)C([H])=N1 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000002098 pyridazinyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 230000019491 signal transduction Effects 0.000 claims 1
- 210000003491 skin Anatomy 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- XJVIPPHGDPEDJL-UHFFFAOYSA-N thiourea;hydrochloride Chemical compound Cl.NC(N)=S XJVIPPHGDPEDJL-UHFFFAOYSA-N 0.000 claims 1
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 claims 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims 1
- 229920002554 vinyl polymer Polymers 0.000 claims 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)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Dermatology (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Heart & Thoracic Surgery (AREA)
- Epidemiology (AREA)
- Vascular Medicine (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Pulmonology (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Pronalazak se odnosi na nove derivate pirido[2, 3-b]pirazina opšte formule (I), njihovo dobijanje i upotrebu kao lekova, naročito za lečenje malignih i ostalih oboljenja koja se baziraju na patološkoj ćelijskoj proliferaciji.
Claims (14)
1. Novi derivati pirido[2, 3-b]pirazina opšte formule I u kojima supstituenti R1-R4 imaju sledeća značenja: gde R1 i R2 mogu nezavisno jedan od drugog da budu: (i) vodonik (ii) hidroksil (iii) halogen, (iv) alkil, gde je alkil radikal zasićen i može da sadrži od 1 do 8 atoma ugljenika, (v) nesupstituisani ili supstituisani aril, gde aril radikal može da ima jednu ili više istih ili različitih F, Cl, Br, J, CF3, CN, NH2, NH-alkil, NH-cikloalkil, NH-heterociklil, NH-aril, NH-heteroaril, NH-alkil-cikloalkil, NH-alkil-heterociklil, NH-alkil-aril, NH-alkil-heteroaril, NH-alkil-NH2, NH-alkil-OH, N(alkil)2, NHC(O)-alkil, NHC(O)-cikloalkil, NHC(O)-heterociklil, NHC(O)-aril, NHC(O)-heteroaril, NHC(O)-alkil-aril, NHC(O)- alkil-heteroaril, NHSO2-alkil, NHSO2-cikloalkil NHSO2-heterociklil, NHSO2-aril, NHSO2-heteroaril, NHSO2-alkil-aril, NHSO2-alkil-heteroaril, N02, SH, S-alkil, S-aril, S-heteroaril, OH, OCF3, O-alkil, O-cikloalkil, O-heterociklil, O-aril, O-heteroaril, O-alkil-cikloalkil, O-alkil-heterociklil, O-alkil-aril, O-alkil-heteroaril, O-alkil-OH, O-(CH2)n-0, OC(O)-alkil, OC(O)-cikloalkil, OC(O)-heterociklil, OC(O)-aril, OC(O)-heteroaril, OC(O)-alkil-aril, OC(O)-alkil-heteroaril, OSO3H, OSO2-alkil, OSO2-cikloalkl, OSO2-heterociklil, OSO2-aril, OSO2-heteroaril, OSO2-alkil-aril, OSO2-alkil-heteroaril, OP(O) (OH)2, C(O)-alkil, C(O)-aril, C(O)-heteroaril, CO2H, CO2-alkil, CO2-cikloalkil, CO2-heterociklil, CO2-aril, CO2-heteroaril, CO2-alkil-cikloalkil, CO2-alkil-heterociklil, CO2-alkil-aril, CO2-alkil-heteroaril, C(O)-NH2, C(O)NH-alkil, C(O)NH-cikloalkil, C(O)NH-heterociklil, C(O)NH-aril, C(O)NH-heteroaril, C(O)NH-alkil-cikloalkil, C(O)NH-alkil-heterociklil, C(O)NH-alkil-aril, C(O)NH-alkil-heteroaril, C(O)N(alkil)2, C(O)N(cikloalkil)2, C(O)N(aril)2, C(O)N(heteroaril)2, SO-alkil, SO-aril, SO2-alkil, SO2-aril, SO2NH2, SO2-NH-alkil, SO2NH-aril, SO2NH-heteroaril, SO2NH-alkil-aril, SO3H, SO2O-alkil, SO2O-aril, SO2O-alkil-aril, alkil, cikloalkil, heterociklil, aril ili heteroarilni supstituenti, gde n ima vrednost 1, 2 ili 3, i gde alkil, cikloalkil, heterociklil, aril, heteroaril, alkil-cikloalkil, alkil-heterociklil, alkil-aril i alkil-heteroarilni supstituenti mogu redom da budu supstituisani, (vi) nesupstituisani ili supstituisani heteroaril, gde heteroarilni radikal može da ima jedan ili više istih ili različitih F, Cl, Br, J, CF3, CN, NH2, NH-alkil, NH-cikloalkil, NH-heterociklil, NH-aril, NH-heteroaril, NH-alkil-cikloalkil, NH-alkil-heterociklil, NH-alkil-aril, NH-alkil-heteroaril, NH-alkil-NH2, NH-alkil-OH, N(alkil)2, NHC(O)-alkil, NHC(O)-cikloalkil, NHC(O)-heterociklil, NHC(O)-aril, NHC(O)-heteroaril, NHC(O)-alkil-aril, NHC(O)-alkil-heteroaril, NHSO2-alkil, NHSO2-cikloalkil, NHSO2-heterociklil, NHSO2-aril, NHSO2-heteroaril, NHSO2-alkil-aril, NHSO2-alkil-heteroaril, NO2, SH, S-alkil, S-aril, S-heteroaril, OH, OCF3, O-alkil, O-cikloalkil, O-aril, O-heteroaril, O-alkil-cikloalkil, O-alkil-heterociklil, O-alkil-aril, O-alkil-heteroaril, OC(O)-alkil, OC(O)-cikloalkil, OC(O)-heterociklil, OC(O)-aril, OC(O)-heteroaril, OC(O)-alkil-aril, OC(O)-alkil-heteroaril, OSO3H, OSO2-alkil, OSO2-cikloalkil, OSO2-heterociklil, OSO2-aril, OSO2-heteroaril, OSO2-alkil-aril, OSO2-alkil-heteroaril, OP(O) (OH)2, C(O)-alkil, C(O)-aril, C(O)-heteroaril, CO2H, CO2-alkil, CO2-cikloalkil, CO2-heterociklil, CO2-aril, CO2-heteroaril, CO2-alkil-cikloalkil, CO2-alkil-heterociklil, CO2-alkil-aril, CO2-alkil-heteroaril, C(O)-NH2, C(O)NH-alkil, C(O)NH-cikloalkil, C(O)NH-heterociklil, C(O)NH-aril, C(O)NH-heteroaril, C(O)NH-alkil-cikloalkil, C(O)NH-alkil-heterociklil, C(O)NH-alkil-aril, C(O)NH-alkil-heteroaril, C(O)N(alkil)2, C(O)N(cikloalkil)2, C(O)N(aril)2, C(O)N(heteroaril)2, SO2NH2, SO2-NH-alkil, SO2NH-aril, SO2NH-heteroaril, SO2NH-alkil-aril, SO3H, SO2O-alkil, SO2O-aril, SO2O-alkil-aril, alkil, cikloalkil, heterociklil, aril ili heteroarilni supstituenti, i gde alkil, cikloalkil, heterociklil, aril i heteroarilni supstituenti mogu redom da budu supstituisani, (vii) OR5, gde R5 može da bude alkil, cikloalkil, heterociklil, aril, heteroaril, alkilcikloalkil, alkilheterociklil, alkilaril ili alkilheteroaril, i alkil, cikloalkil, heterociklil, aril, heteroaril, alkilcikloalkil, alkilheterociklil, alkilaril ili alkilheteroarilni supstituenti koji sa njihove strane mogu redom da budu supstituisani, (viii) SR6, gde R6 može da bude alkil, cikloalkil, heterociklil, aril, heteroaril, alkilcikloalkil, alkilheterociklil, alkilaril ili alkilheteroaril, i gde alkil, cikloalkil, heterociklil, aril i heteroaril, alkilcikloalkil, alkilheterociklil, alkilaril ili alkilheteroarilni supstituenti mogu, sa njihove strane da budu supstituisani, (ix) NR7R8 gde R7 i R8 mogu, svaki za sebe da predstavljaju vodonik, alkil, cikloalkil, heterociklil, aril, heteroaril, alkilciklil, alkilheterociklil, alkilaril ili alkilheteroaril, i alkil, cikloalkil, heterociklil, aril i heteroaril, alkilcikloalkil, alkilheterociklil, alkilaril ili alkilheteroarilni supstituenti mogu sa njihove strane da budu redom supstituisani, ili R7 i R8 zajedno predstavljaju cikloalkil, heterociklil, gde cikloalkil I heterociklil mogu redom da budu supstituisani, R3 i R4 mogu, svaki za sebe, da predstavljaju vodonik ili NR9R10 pod uslovom da, kada je R3= NR9R10, R4 = H i kada je R4 = NR9R10, R3= H, kada R9 može da predstavlja vodonik, alkil, cikloalkil, heterociklil, aril, heteroaril, alkilcikloalkil, alkilheterociklil, alkilaril ili alkilheteroaril, i alkil, cikloalkil, heterociklil, aril i heteroaril, alkilcikloalkil, alkilheterociklil, alkilaril ili alkilheteroarilni supstituenti mogu redom da budu supstituisani, i R10 može da bude: -C(Y)NR11R12, gde Y predstavlja O, S i R11 i R12 mogu svaki za sebe da predstavljaju vodonik, (ii) nesupstituisani ili supstituisani alkil, gde alkil radikal može da ima jednu ili više istih ili različitih F, Cl, Br, J, CF3, CN, NH2, NH-alkil, NH-cikloalkil, NH-heterociklil, NH-aril, NH-heteroaril, NH-alkil-cikloalkil, NH-alkil-heterociklil, NH-alkil-aril, NH-alkil-heteroaril, N(alkil)2, NHC(O)-alkil, NHC(O)-cikloalkil, NHC(O)-heterociklil, NHC(O)-aril, NHC(O)-heteroaril, NHC(O)-alkil-aril, NHC(O)-alkil-heteroaril, NHSO2-alkil, NHSO2-cikloalkil, NHSO2-heterociklil, NHSO2-aril, NHSO2-heteroaril, NHSO2-alkil-aril, NHSO2-alkil-heteroaril, N02, SH, S-alkil, S-cikloalkil, S-heterociklil, S-aril, S-heteroaril, OH, OCF3, O-alkil, O-cikloalkil, O-heterociklil, O-aril, O-heteroaril, O-alkil-cikloalkil, O-alkil-heterociklil, O-alkil-aril, O-alkil-heteroaril, OC(O)-alkil, OC(O)-cikloalkil, OC(O)-heterociklil, OC(O)-aril, OC(O)-heteroaril, OC(O)-alkil-aril, OC(O)-alkil-heteroaril, OSO3H, OSO2-alkil, OSO2-cikloalkil, OSO2-heterociklil, OSO2-aril, OSO2-heteroaril, OSO2-alkil-aril, OSO2-alkil-heteroaril, OP(O) (OH)2, C(O)-alkil, C(O)-aril, C(O)-heteroaril, CO2H, CO2-alkil, CO2-cikloalkil, CO2-heterociklil, CO2-aril, CO2-heteroaril, CO2-alkil-cikloalkil, CO2-alkil-heterociklil, CO2-alkil-aril, CO2-alkil-heteroaril, C(O)-NH2, C(O)NH-alkil, C(O)NH-cikloalkil, C(O)NH-heterociklil, C(O)NH-aril, C(O)NH-heteroaril, C(O)NH-alkil-cikloalkil, C(O)NH-alkil-heterocildil, C(O)NH-alkil-aril, C(O)NH-alkil-heteroaril, C(O)N(alkil)2, C(O)N(cikloalkil)2, C(O)N(aril)2, C(O)N(heteroari 1)2, SO-alkil, SO-aril, SO2-alkil, SO2-aril, SO2NH2, SO2-NH-alkil, SO2NH-aril, SO2NH-heteroaril, SO2NH-alkil-aril, SO3H, SO2O-alkil, SO2O-aril, SO2O-alkil-aril, cikloalkil, heterociklil, aril ili heteroarilni supstituenti, (iii) nesupstituisani ili supstituisani cikloalkil, gde cikloalkil radikal može da ima jednu ili više istih ili različitih F, Cl, Br, J, NH2, NH-alkil, NH-cikloalkil, NH-heterociklil, NH-aril, NH-heteroaril, NH-alkil-aril, NH-alkil-heteroaril, N(alkil)2, NHC(O)-alkil, NHC(O)-cikloalkil, NHC(O)-heterociklil, NHC(O)-aril, NHC(O)-heteroaril, NHC(O)-alkil-aril, NHC(O)-alkil-heteroaril, NHSO2-alkil, NHSO2-cikloalkil, NHSO2-heterociklil, NHSO2-aril, NHSO2-heteroaril, NHSO2-alkil-aril, NHSO2-alkil-heteroaril, OH, O-alkil, O-cikloalkil, O-heterociklil, O-aril, O-heteroaril, O-alkil-aril, O-alkil-heteroaril, OC(O)-alkil, OC(O)-cikloalkil, OC(O)-heterociklil, OC(O)-aril, OC(O)-heteroaril, OC(O)-alkil-aril, OC(O)-alkil-heteroaril, OSO3H, OSO2-alkil, OSO2-cikloalkil, OSO2-heterociklil, OSO2-aril, OSO2-heteroaril, OSO2alkil-aril, OSO2-alkil-heteroaril, OP(O) (OH)2, CO2H, CO2-alkil, CO2-cikloalkil, CO2-heterociklil, CO2-aril, CO2-heteroaril, CO2-alkil-cikloalkil, CO2-alkil-heterociklil, CO2-alkil-aril, CO2-alkil-heteroaril, C(O)-NH2, C(O)NH-aril, C(O)NH-cikloalkil, C(O)NH-heterociklil, C(O)NH-aril, C(O)NH-heteroaril, C(O)NH-alkil-cikloalkil, C(O)NH-alkil-heterociklil, C(O)NH-alkil-aril, C(O)NH-alkil-heteroaril, C(O)N(alkil)2, C(O)N(cikloalkil)2, C(O)N(aril)2, C(O)N(heteroaril)2, alkil iili aril supstituenti, (iv) nesupstituisani ili supstituisani heterociklil, gde heterociklil radikal može da ima jednu ili više istih ili različitih OH, O-alkil, O-aril, NH2, NH-alkil, NH-aril, alkil, alkil-aril ili arilni supstituenti, (v) nesupstituisani ili supstituisani aril, gde arilni radikal može da ima jednu ili više istih ili različitih F, Cl, Br, J, CF3, CN, NH2, NH-alkil, NH-cikloalkil, NH-heterociklil, NH-aril, NH-heteroaril, NH-alkil-cikloalkil, NH-alkil-heterociklil, NH-alkil-aril, NH-alkil-heteroaril, NH-alkil-NH2, NH-alkil-OH, N(alkil)2, NHC(O)-alkil, NHC(O)-cikloalkil, NHC(O)-heterociklil, NHC(O)-aril, NHC(O)-heteroaril, NHC(O)-alkil-aril, NHC(O)-alkil-heteroaril, NHSO2-alkil, NHSO2-cikloalkil, NHSO2-heterociklil, NHSO2-aril, NHSO2-heteroaril, NHSO2-alkil-aril, NHSO2-alkil-heteroaril, N02, SH, S-alkil, S-cikloalkil, S-heterociklil, S-aril, S-heteroaril, OH, OCF3, O-alkil, O-cikloalkil, O-heterociklil, O-aril, O-heteroaril, O-alkil-cikloalkil, O-alkil-heterociklil, O-alkil-aril, O-alkil-heteroaril, O-alkil-OH, O-(CH2)n-0, OC(O)-alkil, OC(O)-cikloalkil, OC(O)-heterociklil, OC(O)-aril, OC(O)-heteroaril, OC(O)-alkil-aril, OC(O)-alkil-heteroaril, OSO3H, OSO2-alkil, OSO2-cikloalkl, OSO2-heterociklil, OSO2-aril, OSO2-heteroaril, OSO2-alkil-aril, OSO2-alkil-heteroaril, OP(O) (OH)2, C(O)-alkil, C(O)-aril, C(O)-heteroaril, CO2H, CO2-alkil, CO2-cikloalkil, CO2-heterociklil, CO2-aril, CO2-heteroaril, CO2-alkil-cikloalkil, CO2-alkil-heterociklil, CO2-alkil-aril, CO2-alkil-heteroaril, C(O)-NH2, C(O)NH-alkil, C(O)NH-cikloalkil, C(O)NH-heterociklil, C(O)NH-aril, C(O)NH-heteroaril, C(O)NH-alkil-cikloalkil, C(O)NH-alkil-heterociklil, C(O)NH-alkil-aril, C(O)NH-alkil-heteroaril, C(O)N(alkil)2, C(O)N(cikloalkil)2, C(O)N(aril)2, C(O)N(heteroaril)2, SO-alkil, SO-aril, SO2-alkil, SO2-aril, SO2NH2, SO2-NH-alkil, SO2NH-aril, SO2NH-heteroaril, SO2NH-alkil-aril, SO3H, SO2O-alkil, SO2O-aril, SO2O-alkilaril, alkil, cikloalkil, heterociklil, aril ili heteroarilni supstituenti, gde n ima vrednost 1, 2 ili 3, (vi) nesupstituisani ili supstituisani heteroaril, gde heteroaril radikal može da ima jednu ili više istih ili različitih F, Cl, Br, J, CF3, CN, NH2, NH-alkil, NH-cikloalkil, NH- heterociklil, NH-aril, NH-heteroaril, NH-alkil-cikloalkil, NH-alkil-heterociklil, NH-alkil-aril, NH-alkil-heteroaril, NH-alkil-NH2, NH-alkil-OH, N(alkil)2, NHC(O)-alkil, NHC(O)-cikloalkil, NHC(O)-heterociklil, NHC(O)-aril, NHC(O)-heteroaril, NHC(O)-alkil-aril, NHC(O)-alkil-heteroaril, NHSO2-alkil, NHSO2-cikloalkil, NHSO2-heterociklil, NHSO2-aril, NHSO2-heteroaril, NHSO2-alkil-aril, NHSO2-alkil-heteroaril, N02, SH, S-alkil, S-aril, S-heteroaril, OH, OCF3, O-alkil, O-cikloalkil, O-aril, O-heteroaril, O-alkil-cikloalkil, O-alkil-heterociklil, O-alkil-aril, O-alkil-heteroaril, OC(O)-alkil, OC(O)-cikloalkil, OC(O)-heterociklil, OC(O)-aril, OC(O)-heteroaril, OC(O)-alkil-aril, OC(O)-alkil-heteroaril, OSO3H, OSO2-alkil, OSO2-cikloalkil, OSO2-heterociklil, OSO2-aril, OSO2-heteroaril, OSO2-alkil-aril, OSO2-alkil-heteroaril, OP(O) (OH)2, C(O)-alkil, C(O)-aril, C(O)-heteroaril, CO2H, CO2-alkil, CO2-cikloalkil, CO2-heterociklil, CO2-aril, CO2-heteroaril, CO2-alkil-cikloalkil, CO2-alkil-heterociklil, CO2-alkil-aril, CO2-alkil-heteroaril, C(O)-NH2, C(O)NH-alkil, C(O)NH-cikloalkil, C(O)NH-heterociklil, C(O)NH-aril, C(O)NH-heteroaril, C(O)NH-alkil-cikloalkil, C(O)NH-alkil-heterociklil, C(O)NH-alkil-aril, C(O)NH-alkil-heteroaril, C(O)N(alkil)2, C(O)N(cikloalkil)2, C(O)N(aril)2, C(O)N(heteroaril)2, SO2NH2, SO2-NH-alkil, SO2NH-aril, SO2NH-heteroaril, SO2NH-alkil-aril, SO3H, SO2O-alkil, SO2O-aril, SO2O-alkil-aril, alkil, cikloalkil, heterociklil, aril ili heteroarilni supstituenti, (vii) -C(O)-R17, gde R17 može da predstavlja alkil, aril ili heteroaril, i alkil i arilni supstituenti mogu jedan za drugim da budu supstituisani, (viii) ili R11 i R12 zajedno mogu da budu cikloalkil ili heterociklil, -C(Y)NR13R14, gde Y predstavlja NH i R13 i R14 mogu svaki za sebe da budu (i) vodonik (ii) nesupstituisani ili supstituisani alkil, gde alkil radikal može da ima jednu ili više istih ili različitih F, Cl, Br, J, CF3, CN, NH2, NH-alkil, NH-cikloalkil, NH-heterociklil, NH-aril, NH-heteroaril, NH-alkil-aril, NH-alkil-heteroaril, N(alkil)2, NHC(O)-alkil, NHC(O)-cikloalkil, NHC(O)-heterociklil, NHC(O)-aril, NHC(O)-heteroaril, NHSO2-alkil, NHSO2-cikloalkil, NHSO2-aril, NHSO2-heteroaril, N02, SH, S-alkil, S-cikloalkil, S-heterociklil, S-aril, S-heteroaril, OH, OCF3, O-alkil, O-cikloalkil, O-heterociklil, O-aril, O-heteroaril, O-alkil-cikloalkil, O-alkil-aril, O-alkil-heteroaril, OC(O)-alkil, OC(O)-cikloalkil, OC(O)-heterociklil, OC(O)-aril, OC(O)-heteroaril, OSO2-alkil, OSO2-cikloalkil, OSO2-aril, OSO2-heteroaril, C(O)-alkil, C(O)-aril, CO2H, CO2-alkil, CO2-cikloalkil, CO2-heterociklil, CO2-aril, CO2-heteroaril, CO2-alkil-cikloalkil, CO2-alkil-heterociklil, CO2-alkil-aril, CO2-alkil-heteroaril, C(O)-NH2, C(O)NH-alkil, C(O)NH-cikloalkil, C(O)NH-heterociklil, C(O)NH-aril, C(O)NH-heteroaril, C(O)NH-alkil-cikloalkil, C(O)NH-alkil-heterociklil, C(O)NH-alkil-aril, C(O)NH-alkil-heteroaril, C(O)N(alkil)2, C(O)N(cikloalkil)2, C(O)N(aril)2, C(O)N(heteroaril)2, SO-alkil, SO-aril, SO2-alkil, SO2-aril, SO2NH2, SO3H, alkil, cikloalkil, heterociklil, aril ili heteroarilni supstituenti, (iii) nesupstituisani ili supstituisani cikloalkil, gde ciklalkil radikal ima jednu ili više identičnih ili istih F, Cl, Br, J, NH2, NH-alkil, NH-cikloalkil, NH-heterociklil, NH-aril, NH-heteroaril. NH-alkil-aril, NH-alkil-heteroaril, N(alkil)2, NHC(O)-alkil, NHC(O)-cikloalkil, NHC(O)-heterociklil, NHC(O)-aril, NHC(O)-heteroaril, NHSO2-alkil, NHSOi-cikloalkil, NHSO2-aril, NHSO2-heteroaril, OH, O-alkil, O-cikloalkil, O-heterociklil, O-aril, O-heteroaril, O-alkil-aril, O-alkil-heteroaril, OC(O)-alkil, OC(O)-cikloalkil, OC(O)-heterociklil, OC(O)-aril, OC(O)-heteroaril, OSO2-alkil, OSO2-cikloalkil, OSO2-aril, OSO2-heteroaril, CO2H, CO2-alkil, CO2-cikloalkil, CO2-heterociklil, CO2-aril, CO2-heteroaril, C(O)-NH2, C(O)NH-alkil, C(O)NH-cikloalkil, C(O)NH-heterociklil, C(O)NH-aril, C(O)NH-heteroaril, C(O)NH-alkil-aril, C(O)NH-alkil-heteroaril, C(O)N(alkil)2, alkil iili aril supstituenti, (iv) nesupstituisani ili supstituisani heterociklil, gde heterociklični radikal može da ima jednu ili više istih ili različitih OH, O-alkil, O-aril, NH2, NH-alkil, NH-aril, alkil ili aril supstituenata, (v) nesupstituisani ili supstituisani aril, gde aril radikal ima jednu ili više istih ili različitih F, Cl, Br, J, CF3, CN, NH2, NH-alkil, NH-cikloalkil, NH-heterociklil, NH-aril, NH-heteroaril, NH-alkil-cikloalkil, NH-alkil-heterociklil, NH-alkil-aril, NH-alkil-heteroaril, NH-alkil-NH2, NH-alkil-OH, N(alkil)2, NHC(O)-alkil, NHC(O)-cikloalkil, NHC(O)-heterociklil, NHC(O)-aril, NHC(O)-heteroaril, NHSO2-alkil, NHSO2-aril, NHSO2-heteroaril, N02, SH, S-alkil, S-cikloalkil, S-heterociklil, S-aril, S-heteroaril, OH, OCF3, O-alkil, O-cikloalkil, O-heterociklil, O-aril, O-heteroaril, O-alkil-cikloalkil, O-alkil-heterociklil, O-alkil-aril, O-alkil-heteroaril, O-alkil-OH, O-(CH2)n-0, OC(O)-alkil, OC(O)-cikloalkil, OC(O)-heterocikliL OC(O)-aril, OC(O)-heteroaril, OSO2-alkil, OSO2-cikloalkil. OSO2-aril, OSO2-heteroaril, C(O)-alkil, C(O)-aril, C(O)-heteroaril, CO2H, CO2-alkil, CO2-cikloalkil, CO2-heterociklil, CO2-arik CO2-heteroaril, CO2-alkil-cikloalkil, CO2-alkil-heterociklil, CO2-alkil-aril, CO2-alkil-heteroaril, C(O)-NH2, C(O)NH-alkil, C(O)NH-cikloalkil, C(O)NH-heterociklil, C(O)NH-aril, C(O)NH-heteroaril, C(O)NH-alkil-cikloalkil, C(O)NH-alkil-heterociklil, C(O)NH-alkil-aril, C(O)NH-alkil-heteroaril, C(O)N(alkil)2, C(O)N(cikloalkil)2, C(O)N(aril)2, C(O)N(heteroaril)2, SO-alkil, SO-aril, SO2-alkil, SO2-aril, SO2NH2, SOrNH-alkil, SO2NH-aril, SO2NH-heteroaril, SO3H, SO2O-alkil, SO2O-aril, SO2O-heteroaril, alkil, cikloalkil, heterociklil, aril ili heteroarilni supstituenti, gde n ima vrednost 1, 2 ili 3, (vi) nesupstituisani ili supstituisani heteroaril, gde heteroarilni radikal može da ima jednu ili više istih ili različitih F, Cl, Br, J, CF3, CN, NH2, NH-alkil, NH-cikloalkil, NH-heterociklil, NH-aril, NH-heteroaril, NH-alkil-aril, NH-alkil-heteroaril, N(alkil)2, NHC(O)-alkil, NHC(O)-cikloalkil, NHC(O)-heterociklil, NHC(O)-aril, NHC(O)-heteroaril, NHSO2-alkil, NHSO2-aril, NHSO2-heteroaril, N02) SH, S-alkil, S-aril, OH, OCF3, O-alkil, O-cikloalkil, O-heterociklil, O-aril, O-heteroaril, OC(O)-alkil, OC(O)-cikloalkil, OC(O)-heterociklil, OC(O)-aril, OC(O)-heteroaril, OSO2-alkil, OSO2-cikloalkil, OSO2-aril, OSO2-heteroaril, C(O)-alkil, C(O)-aril, C(O)-heteroaril, CO2H, CO2-alkil, CO2-cikloalkil, CO2-heterociklil, CO2-aril, CO2-heteroaril, CO2-alkil-cikloalkil, CO2-alkil-heterociklil, CO2-alkil-aril, CO2-alkil-heteroaril, C(O)-NH2, C(O)NH-alkil, C(O)NH-cikloalkil, C(O)NH-heterociklil, C(O)NH-aril, C(O)NH-heteroaril, C(O)NH-alkil-cikloalkil, C(O)NH-alkil-heterociklil, C(O)NH-alkil-aril, C(O)NH-alkil-heteroaril, C(O)N(alkil)2, C(O)N(cikloalkil)2, C(O)N(aril)2, C(O)N(heteroaril)2, SO2-alkil, SO2-aril, SO2NH2, SO2NH-alkil, SO2NH-aril. SO2NH-heteroariI, SO3H, SO2O-alkil, SO2O-aril, SO2O-heteroaril, alkil, cikloalkil, heterociklil, aril ili heteroarilnih supstituenata, (vii) ili R13 i R14 zajedno mogu da budu cikloalkil ili heterociklil,-C(NR15)R16 gde R može da bude H i R16 može da bude, (i) nesupstituisani ili supstituisani alkil, gde alkil radikal može da ima jednu ili više istih ili različitih F, Cl, Br, J, CF3, NH2, NH-alkil, NH-cikloalkil, NH-heterociklil, NH-aril, NH-heteroaril, NH-alkil-aril, NH-alkil-heteroaril, N(alkil)2, NHC(O)-alkil, NHC(O)-cikloalkil, NHC(O)-heterociklil, NHC(O)-aril, NHC(O)-heteroaril, NHSO2-alkil, NHSO2-cikloalkil, NHSO2-aril, NHSO2-heteroaril, N02, SH, S-alkil, S-cikloalkil, S-heterociklil, S-aril, S-heteroaril, OH, OCF3, O-alkil, O-cikloalkil, O-heterociklil, O-aril, O-heteroaril, O-alkil-cikloalkil, O-alkil-aril, O-alkil-heteroaril, OC(O)-alkil, OC(O)-cikloalkil, OC(O)-heterociklil, OC(O)-aril, OC(O)-heteroaril, OSO2-alkil, OSO2-cikloalkil, OSO2-aril, OSO2-heteroaril, C(O)-alkil, C(O)-aril, CO2H, CO2-alkil, CO2-cikloalkil, CO2-heterociklil, CO2-aril, CO2-heteroaril, CO2-alkil-cikloalkil, CO2-alkil-heterociklil, CO2-alkil-aril, CO2-alkil-heteroaril, C(O)-NH2, C(O)NH-alkil, C(O)NH-cikloalkil, C(O)NH-heterociklil, C(O)NH-aril, C(O)NH-heteroaril, C(O)NH-alkil-cikloalkil, C(O)NH-alkil-heterociklil, C(O)NH-alkil-aril, C(O)NH-alkil-heteroaril, C(O)N(alkil)2, C(O)N(cikloalkil)2, C(O)N(aril)2, C(O)N(heteroaril)2, SO-alkil, SO-aril, SO2-alkil, SO2-aril, SO2NH2, SO3H, alkil, cikloalkil, heterociklil, aril ili heteroarilni supstituenata, (ii) nesupstituisani ili supstituisani cikloalkil,, gde ciklalkil radikal ima jednu ili više identičnih ili istih F, Cl, Br, J, NH2, NH-alkil, NH-cikloalkil, NH-heterociklil, NH-aril, NH-heteroaril, NH-alkil-aril, NH-alkil-heteroaril, N(alkil)2, NHC(O)-alkil, NHC(O)-cikloalkil, NHC(O)-heterociklil, NHC(O)-aril, NHC(O)-heteroaril, NHSO2-alkil, NHSO2-cikloalkil, NHSO2-aril, NHSO2-heteroaril, OH, O-alkil, O-cikloalkil, O-heterociklil, O-aril, O-heteroaril, O-alkil-aril, O-alkil-heteroaril, OC(O)-alkil, OC(O)-cikloalkil, OC(O)-heterociklil, OC(O)-aril, OC(O)-heteroaril, OSO2-alkil, OSO2-cikloalkil, OSO2-aril, OSO2-heteroaril, CO2H, CO2-alkil, CO2-cikloalkil, CO2-heterociklil, CO2-aril, CO2-heteroaril, C(O)-NH2, C(O)NH-alkil, C(O)NH-cikloalkil, C(O)NH-heterociklil, C(O)NH-aril, C(O)NH-heteroaril, C(O)NH-alkil-aril, C(O)NH-alkil-heteroaril, C(O)N(alkil)2, alkil ili aril supstituenata, (iii) nesupstituisani ili supstituisani heterociklil, gde heterociklični radikal može da ima jedan ili više istih ili različitih OH, O-alkil, O-aril, NH2, NH-alkil, NH-aril, alkil ili aril supstituenata, (iv) nesupstituisani ili supstituisani aril, gde aril radikal ima jednu ili više istih ili različitih F, Cl, Br, J, CF3, NH2, NH-alkil, NH-cikloalkil, NH-heterociklil, NH-aril, NH-heteroaril, NH-alkil-cikloalkil, NH-alkil-heterociklil, NH-alkil-aril, NH-alkil-heteroaril, NH-alkil-NH2, NH-alkil-OH, N(alkil)2, NHC(O)-alkil, NHC(O)-cikloalkil, NHC(O)-heterociklil, NHC(O)-aril, NHC(O)-heteroaril, NHSO2-alkil, NHSO2-aril, NHSO2-heteroaril, N02, SH, S-alkil, S-cikloalkil, S-heterociklil, S-aril, S-heteroaril, OH, OCF3, O-alkil, O-cikloalkil, O-heterociklil, O-aril, O-heteroaril, O-alkil-cikloalkil, O-alkil-heterociklil. O-alkil-aril, O-alkil-heteroaril. O-alkil-OH, O-(CH2)n-0. OC(O)-alkil. OC(O)-cikloalkil, OC(O)-heterociklil, OC(O)-aril, OC(O)-heteroaril, OSO2-alkil, OSO2-cikloalkik OSO2-aril, OSOrheteroaril, C(O)-alkil, C(O)-aril, C(O)-heteroaril, CO2H, CO2-alkil, CO2-kloalkil, CO2-heterociklil, CO2-aril, CO2-heteroaril, CO2-alkil-cikloalkil, CO2-alkil-heterociklil, CO2-alkil-aril, CO2-alkil-heteroaril, C(O)-NH2, C(O)NH-alkil, C(O)NH-cikloalkil, C(O)NH-heterociklil, C(O)NH-aril, C(O)NH-heteroaril, C(O)NH-alkil-cikloalkil, C(O)NH-alkil-heterociklil, C(O)NH-alkil-aril, C(O)NH-alkil-heteroaril, C(O)N(alkil)2, C(O)N(cikloalkil)2, C(O)N(aril)2, C(O)N(heteroaril)2, SO-alkil, SO-aril, SO2-alkil, SO2-aril, SO2NH2, SO2-NH-alkil, SO2NH-aril, SO2NH-heteroaril, SO3H, SO2O-alkil, SO2O-aril, SO2O-heteroaril, alkil, cikloalkil, heterociklil, aril ili heteroarilni supstituenti, gde n ima vrednost 1, 2 ili 3, (v) nesupstituisani ili supstituisani heteroaril, gde heteroarilni radikal može da ima jednu ili više istih ili različitih F, Cl, Br, J, CF3, NH2, NH-alkil, NH-cikloalkil, NH-heterociklil, NH-aril, NH-heteroaril, NH-alkil-aril, NH-alkil-heteroaril, N(alkil)2, NHC(O)-alkil, NHC(O)-cikloalkil, NHC(O)-heterociklil, NHC(O)-aril, NHC(O)-heteroaril, NHSO2-alkil, NHSO2-aril, NHSO2-heteroaril, N02, SH, S-alkil, S-aril, OH, OCF3, O-alkil, O-cikloalkil, O-heterociklil, O-aril, O-heteroaril, OC(O)-alkil, OC(O)-cikloalkil, OC(O)-heterociklil, OC(O)-aril, OC(O)-heteroaril, OSO2-alkil, OSO2-cikloalkil, OSO2-aril, OSO2-heteroaril, C(O)-alkil, C(O)-aril, C(O)-heteroaril, CO2H, CO2-alkil, CO2-cikloalkil, CO2-heterociklil, CO2-aril, CO2-heteroaril, CO2-alkil-cikloalkil, CO2-alkil-heterociklil, CO2-alkil-aril, CO2-alkil-heteroaril, C(O)-NH2, C(O)NH-alkil, C(O)NH-cikloalkil, C(O)NH-heterociklil, C(O)NH-aril, C(O)NH-heteroaril, C(O)NH-alkil-cikloalkil, C(O)NH-alkil-heterociklil, C(O)NH-alkil-aril, C(O)NH-alkil-heteroaril, C(O)N(alkil)2, C(O)N(cikloalkil)2, C(O)N(aril)2, C(O)N(heteroaril)2, SO2-alkil, SO2-aril, SO2NH2,SO2NH-alkil, SO2NH-aril, SO2NH-heteroaril, SO3H, SO2O-alkil. SO2O-aril, SO2O-heteroaril, alkil cikloalkil, heterociklil, aril ili heteroarilnih supstituenata; i fiziološki prihvatljive soli, derivati i analozi jedinjenja prema formuli I, gde se soli mogu dobiti neutralizacijom baznih jedinjenja sa neorganskim i organskim kiselinama ili neutralizacijom kiselih jedinjenja sa neorganskim i organskim bazama, i solvatima, hidratima i njihovim polimorfnim oblicima, gde jedinjenja opšte formule I i soli, derivati i njihovi analozi, njihovi solvati, hidrati i njihovi polimorfni oblici mogu da budu prisutni u obliku njihovih racemata, u obliku čistih enantiomera i/ili diastereoizmoera ili u obliku smeša ovih enantiomera i/ili diastereoizomera ili u obliku tautomera.
2. Derivati pirido[2, 3-b]pirazina opšte formule I prema patentnom zahtevu 1, naznačen time, što alkil radikal može da bude metil, etil, n-propil, 2-propil, n-butil, sek-butil, terc-butil, n-pentil, izopentil, neopentil, n-heksil, 2-heksil, n-oktil, etilenil(vinil), etinil, propenil (-CH2CH=CH2; -CH=CH-CH3, -C(=CH2)-CH3), propinil (-CH2C=CH -C=C-CH3), butenil, butinil, pentenil, pentinil, heksenil, heksinil, heptenil, heptinil, oktenil i oktinil.
3. Derivati pirido[2, 3-b]pirazina opšte formule I prema patentnom zahtevu 1, naznačen time, što heterociklični radikal može da bude odabran iz grupe koju sačinjavaju tetrahidrofuril, tetrahidropiranil, pirolidinil, piperidinil, piperazinil i morfolinil.
4. Derivati pirido[2, 3-b]pirazina opšte formule I prema patentnom zahtevu 1, naznačen time, što heteroarilni radikal bude odabran iz grupe koju sačinjavaju pirolil, furil, tienil, tiazolil, oksazolil, izoksazolil, pirazolil, imidazolil, piridinil, pirimidinil, piridazinil, pirazinil, ftalazinil, indolil, indazolil, indolizinil, hinolinil, izohinolinil, hinoksalinil, hinoazolinil, karbazolil, fenazinil, fenotiazinil, akridinil.
5. Derivati pirido[2, 3-b]pirazina opšte formule I prema patentnim zahtevima 1 do 4. naročito jedno od sledećih jedinjenja: l-alil-3-(3-fenilpirido[2, 3-b]pirazin-6-il)tiourea l-alil-3-(3-naftalen-2-ilpirido[2, 3-b]pirazin-6-il)tiourea l-alil-3-[3-(4-metoksifenil)pirido[2, 3-b]pirazin-6-il]tiourea l-alil-3-[3-(4-hidroksifenil)pirido[2, 3-b]pirazin-6-il]tiourea hidrohlorid l-(2-metilalil)-3-(3-fenilpirido[2, 3-b]pirazin-6-il]tiourea l-(2-metilalil)-3-(3-naftalen-2-ilpirido[2, 3-b]pirazin-6-il)tiourea l-[3-(4-metoksifenil)pirido[2, 3-b]pirazin-6-il)-3-(2-metilalil)tiourea l-(3-naftalen-2-ilpirido[2, 3-b]pirazin-6-il)-3-(4-nitrofenil)tiourea l-[3-(4-metoksifenil)pirido[2, 3-b]pirazin-6-il)-3-(4-nitrofenil)tiourea l-terc-butil-3-(3-fenilpirido[2, 3-b]pirazin-6-il)-tiourea l-cilopropil-3-(3-fenilpirido[2, 3-b]pirazin-6-il)-tiourea 1 -metil-3 -(3 -fenilpirido [2, 3 -b]pirazin-6-il)-tiourea l-benzil-3-(3-fenilpirido[2, 3-b]pirazin-6-il)-tiourea l-(4-fluorofenil)-3-(3-fenilpirido[2, 3-b]pirazin-6-il)-tiourea l-cikloheksil-3-(3-fenilpirido[2, 3-b]pirazin-6-il)-6-il-tiourea l-izopropil-3-(3-fenilpirido[2, 3-b]pirazin-6-il)tiourea l-furan-2-ilmetil-3-(3-fenilpirido[2, 3-b]pirazin-6-il)-tiourea l-metil-3-[3-(4-nitrofenil)pirido[2, 3-b]pirazin-6-il]-tiourea l-[3-(4-hidroksifenil) pirido[2, 3-b]pirazin-6-il]-3-metiltiourea l-alil-3-[3-(4-nitrofenil)pirido[2, 3-b]pirazin-6-il]-tiourea etil 4-[6-(3-aliltiourea) pirido[2, 3-b]pirazin-3-il]-benzoat l-alil-3-[3-(3-hidroksifenil)pirido[2. 3-b]pirazin-6-il]-tiourea l-alil-3-(3-benzo[l, 3]dioksol-5-ilpirido[2, 3-b]pirazin-6-il]-tiourea l-[3-(4-hidroksifenil)pirido[2, 3-b]pirazin-6-il]-3-prop-2-iniltiourea l-alil-3-[3-(4-hidroksifenil)pirido[2, 3-b]pirazin-6-il]-tiourea l-[3-(4-hidroksifenil)pirido[2, 3-b]pirazin-6-il]-3-(propenil)-tiourea l-alil-3-[2, 3-bis(4-hidroksifenil)pirido[2, 3-b]pirazin-6-il]-tiourea l-[2, 3-bis-(4-hidroksifenil)pirido[2, 3-b]pirazin-6-il]-3-(propenil)-tiourea l-alil-3-[2-(4-hidroksifenil)pirido[2, 3-b]pirazin-6-il]-tiourea l-alil-3-[3-(4-nitrofenil)pirido[2, 3-b]pirazin-7-il]-tiourea l-ciklopropil-3-(3-fenilpirido[2, 3-b]pirazin-6-il]-urea l-alil-3-[3-(4-hidroksifenil)pirido[2, 3-b]pirazin-6-il]-urea l-(3-fenilpirido[2, 3-b]pirazin-6-il)-3-p-tolilurea l-(4-hloro-3-trifluorometilfenil)-3-(3-fenilpirido[2, 3-b]pirazin-6-il]-urea l-(2-morfolin-4-il-etil)-3-(3-fenilpirido[2, 3-b]pirazin-6-il]-urea l-fenetil-3-(3-fenilpirido[2, 3-b]pirazin-6-il]-urea l-(2, 3-dipiridin-2-ilpirido[2, 3-b]pirazin-6-il)-3-etilurea l-(2, 3-dimetilpirido[2, 3-b]pirazin-6-il]3-etiltiourea.
6. Lek, koji sadrži najmanje jedno jedinjenje opšte formule I prema patentnim zahtevima 1 do 5.
7. Lek prema patentnom zahtevu 6, naznačen time, što je jedinjenje prisustno u kompoziciji u kombinaciji sa najmanje jednim farmaceutski aktivnim sredstvom i/ili farmaceutskim nosačima i/ili diluentima ili ostalim ekscipijentima.
8. Postupak za proizvodnju leka prema patentnom zahtevu 6 i 7, naznačen time, što se jedan ili više derivata pirido[2, 3-b]pirazina opšte formule I prema bilo kojem od patentnih zahteva od 1 do 5, koriste se za dobijanje farmaceutskih preparata ili se prevode u terapeutski korisni oblik sa uobičajenim farmaceutskim nosačima i/ili diluentima ili ostalim pomoćnim sredstvima.
9. Jedinjenje prema bilo kojem od patentnih zahteva 1 do 5 za upotrebu kao farmaceutskog sredstva.
10. Upotreba derivata pirido[2, 3-b]pirazina opšte formule I prema bilo kojem od patentnih zahteva 1 do 5 kao terapeutski aktivnih sastojaka za proizvodnju lekova za lečenje oboljenja koja nastaju kao rezultat pogrešno usmerenih ćelijskih procesa signalne transdukcije.
11. Upotreba prema patentnom zahtevu 10 za lečenje oboljenja koja se baziraju na patološkoj proliferaciji ćelija kao što su restenoza, psorijaza, arteroskleroza i ciroza jetre.
12. Upotreba prema patentnom zahtevu 10 za lečenje malignih ili benignih onkoza, naročito onkoza dojke, prostate, pluća, kože i jajnih ćelija.
13. Upotreba prema patentnom zahtevu 10 do 12 za lečenje oboljenja koja se javljaju usled pogrešno usmerenih ćelijskih procesa signalne transdukcije, i oboljenja koja se baziraju na patološkoj ćelijskoj proliferaciji i malignim i benignim onkozama kod ljudi, kod sisara i kod živine.
14. Upotreba prema patentnom zahtevu 10 za modulaciju pogrešno usmerenih ćelijskih procesa signalne transdukcije. naročito radi uticaja na funkciju tirozin i serin/treonin kinaza, kao što su c-Raf, B-Raf, Mek, MAPKs, PDGFRbeta, Flt-3, IGF1R, PKB/Aktil, c-Kit, c-Abl, FGFR1 i KDR.
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| 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 |
| PCT/EP2004/005388 WO2004104003A1 (de) | 2003-05-23 | 2004-05-19 | Neue pyridopyrazine und deren verwendung als modulatoren von kinasen |
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| EP (1) | EP1636228B1 (me) |
| JP (2) | JP4571944B2 (me) |
| KR (1) | KR101111464B1 (me) |
| AR (1) | AR045686A1 (me) |
| AT (1) | ATE411992T1 (me) |
| AU (1) | AU2004240747B2 (me) |
| BR (1) | BRPI0410633A (me) |
| CA (1) | CA2524525C (me) |
| CY (1) | CY1108715T1 (me) |
| DE (1) | DE502004008322D1 (me) |
| DK (1) | DK1636228T3 (me) |
| ES (1) | ES2316985T3 (me) |
| HR (1) | HRP20090036T3 (me) |
| ME (1) | ME00541B (me) |
| MX (1) | MXPA05012645A (me) |
| NO (1) | NO332005B1 (me) |
| NZ (1) | NZ544112A (me) |
| PL (1) | PL1636228T3 (me) |
| PT (1) | PT1636228E (me) |
| RU (1) | RU2330851C9 (me) |
| SI (1) | SI1636228T1 (me) |
| TW (1) | TWI341839B (me) |
| UA (1) | UA78929C2 (me) |
| WO (1) | WO2004104003A1 (me) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2597456A1 (en) * | 2005-02-14 | 2006-08-31 | Merck & Co., Inc. | Inhibitors of akt activity |
| KR101400905B1 (ko) | 2005-11-11 | 2014-05-29 | 아에테르나 젠타리스 게엠베하 | 신규한 피리도피라진 및 키나제의 조절제로서의 이의 용도 |
| EP1790342A1 (de) | 2005-11-11 | 2007-05-30 | Zentaris GmbH | Pyridopyrazin-Derivate und deren Verwendung als Modulatoren der Signaltransduktionswege |
| 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 |
| 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 |
| EP2483406A2 (en) | 2009-09-30 | 2012-08-08 | President and Fellows of Harvard College | Methods for modulation of autophagy through the modulation of autophagy-inhibiting gene products |
| 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 |
| GB201118675D0 (en) | 2011-10-28 | 2011-12-14 | Astex Therapeutics Ltd | New compounds |
| GB201118656D0 (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 |
| GB201209609D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| GB201209613D0 (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 |
| JO3512B1 (ar) | 2014-03-26 | 2020-07-05 | Astex Therapeutics Ltd | مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز |
| JP6980385B2 (ja) | 2014-03-26 | 2021-12-15 | アステックス、セラピューティックス、リミテッドAstex Therapeutics Limited | Ｆｇｆｒ阻害剤とｉｇｆ１ｒ阻害剤の組合せ |
| MA55696A (fr) | 2014-03-26 | 2022-02-23 | Astex Therapeutics Ltd | Combinaisons |
| JOP20200201A1 (ar) | 2015-02-10 | 2017-06-16 | Astex Therapeutics Ltd | تركيبات صيدلانية تشتمل على n-(3.5- ثنائي ميثوكسي فينيل)-n'-(1-ميثيل إيثيل)-n-[3-(ميثيل-1h-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 |
| HRP20220012T1 (hr) | 2015-09-23 | 2022-04-01 | Janssen Pharmaceutica Nv | Bi-heteroaril supstituirani 1,4-benzodiazepini i njihova upotreba za liječenje raka |
| BR112018005637B1 (pt) | 2015-09-23 | 2023-11-28 | Janssen Pharmaceutica Nv | Compostos derivados de quinoxalina, quinolina e quinazolinona,composições farmacêuticas que os compreende, e uso dos referidos compostos |
| WO2018237190A1 (en) * | 2017-06-22 | 2018-12-27 | 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 (me) | 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 |
| KR20100107509A (ko) | 2001-09-14 | 2010-10-05 | 9222-9129 퀘벡 인코포레이티드 | 히스톤 데아세틸라아제의 억제제 |
| JP4451136B2 (ja) | 2002-04-08 | 2010-04-14 | メルク エンド カムパニー インコーポレーテッド | Ａｋｔ活性阻害薬 |
| AU2003223467B2 (en) | 2002-04-08 | 2007-10-04 | Merck Sharp & Dohme Corp. | Inhibitors of Akt activity |
| US20060142178A1 (en) * | 2002-04-08 | 2006-06-29 | Barnett Stanley F | Method of treating cancer |
| JP4903997B2 (ja) | 2002-07-02 | 2012-03-28 | サザン リサーチ インスティチュート | ＦｔｓＺの阻害剤およびそれらの用途 |
| CA2500727A1 (en) | 2002-10-03 | 2004-04-15 | Targegen, Inc. | Vasculostatic agents and methods of use thereof |
| DE10323345A1 (de) | 2003-05-23 | 2004-12-16 | Zentaris Gmbh | Neue Pyridopyrazine und deren Verwendung als Kinase-Inhibitoren |
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- 2004-05-19 WO PCT/EP2004/005388 patent/WO2004104003A1/de not_active Ceased
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- 2004-05-19 UA UAA200510686A patent/UA78929C2/uk unknown
- 2004-05-19 AT AT04733768T patent/ATE411992T1/de active
- 2004-05-19 DE DE502004008322T patent/DE502004008322D1/de not_active Expired - Lifetime
- 2004-05-19 EP EP04733768A patent/EP1636228B1/de not_active Expired - Lifetime
- 2004-05-19 SI SI200431009T patent/SI1636228T1/sl unknown
- 2004-05-19 ES ES04733768T patent/ES2316985T3/es not_active Expired - Lifetime
- 2004-05-19 PL PL04733768T patent/PL1636228T3/pl unknown
- 2004-05-19 NZ NZ544112A patent/NZ544112A/en not_active IP Right Cessation
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- 2004-05-19 RU RU2005140377/04A patent/RU2330851C9/ru not_active IP Right Cessation
- 2004-05-19 AU AU2004240747A patent/AU2004240747B2/en not_active Ceased
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- 2004-05-20 TW TW093114324A patent/TWI341839B/zh not_active IP Right Cessation
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