ZA200306887B - Pyrazolopyrimidines as therapeutic agents. - Google Patents
Pyrazolopyrimidines as therapeutic agents. Download PDFInfo
- Publication number
- ZA200306887B ZA200306887B ZA200306887A ZA200306887A ZA200306887B ZA 200306887 B ZA200306887 B ZA 200306887B ZA 200306887 A ZA200306887 A ZA 200306887A ZA 200306887 A ZA200306887 A ZA 200306887A ZA 200306887 B ZA200306887 B ZA 200306887B
- Authority
- ZA
- South Africa
- Prior art keywords
- substituted
- unsubstituted
- alkyl
- group
- independently
- Prior art date
Links
- 239000003814 drug Substances 0.000 title claims description 21
- 229940124597 therapeutic agent Drugs 0.000 title description 2
- APXRHPDHORGIEB-UHFFFAOYSA-N 1H-pyrazolo[4,3-d]pyrimidine Chemical class N1=CN=C2C=NNC2=C1 APXRHPDHORGIEB-UHFFFAOYSA-N 0.000 title 1
- -1 imidazo[1,2-a]pyrimidinyl Chemical group 0.000 claims description 203
- 125000000217 alkyl group Chemical group 0.000 claims description 189
- 125000003118 aryl group Chemical group 0.000 claims description 108
- 150000001875 compounds Chemical class 0.000 claims description 106
- 125000000623 heterocyclic group Chemical group 0.000 claims description 93
- 229910052757 nitrogen Inorganic materials 0.000 claims description 92
- 229910020008 S(O) Inorganic materials 0.000 claims description 88
- 229910052739 hydrogen Inorganic materials 0.000 claims description 59
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 58
- 239000001257 hydrogen Substances 0.000 claims description 58
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 58
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 53
- 125000001072 heteroaryl group Chemical group 0.000 claims description 49
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 47
- 239000000203 mixture Substances 0.000 claims description 47
- 238000000034 method Methods 0.000 claims description 45
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 45
- 125000001424 substituent group Chemical group 0.000 claims description 45
- 125000003545 alkoxy group Chemical group 0.000 claims description 38
- 150000002431 hydrogen Chemical class 0.000 claims description 35
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims description 33
- 229910052799 carbon Inorganic materials 0.000 claims description 30
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims description 27
- 229920006395 saturated elastomer Polymers 0.000 claims description 27
- 229910052736 halogen Inorganic materials 0.000 claims description 26
- 150000002367 halogens Chemical class 0.000 claims description 26
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 25
- 239000002207 metabolite Substances 0.000 claims description 25
- 229940002612 prodrug Drugs 0.000 claims description 25
- 239000000651 prodrug Substances 0.000 claims description 25
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 24
- 150000003839 salts Chemical class 0.000 claims description 24
- 229910052717 sulfur Inorganic materials 0.000 claims description 22
- 101100481410 Mus musculus Tek gene Proteins 0.000 claims description 21
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 21
- 229910052760 oxygen Inorganic materials 0.000 claims description 21
- 101100481408 Danio rerio tie2 gene Proteins 0.000 claims description 20
- 125000000392 cycloalkenyl group Chemical group 0.000 claims description 20
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 20
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 20
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 19
- 230000000694 effects Effects 0.000 claims description 19
- 125000005518 carboxamido group Chemical group 0.000 claims description 18
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 18
- 238000011282 treatment Methods 0.000 claims description 18
- 125000004103 aminoalkyl group Chemical group 0.000 claims description 17
- 201000010099 disease Diseases 0.000 claims description 17
- 125000003386 piperidinyl group Chemical group 0.000 claims description 17
- 206010028980 Neoplasm Diseases 0.000 claims description 16
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 16
- 125000000168 pyrrolyl group Chemical group 0.000 claims description 16
- 125000001544 thienyl group Chemical group 0.000 claims description 16
- 102000001253 Protein Kinase Human genes 0.000 claims description 15
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 claims description 15
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 claims description 15
- 125000002541 furyl group Chemical group 0.000 claims description 15
- 108060006633 protein kinase Proteins 0.000 claims description 15
- 230000033115 angiogenesis Effects 0.000 claims description 14
- 229910052698 phosphorus Inorganic materials 0.000 claims description 14
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims description 14
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims description 14
- 125000003368 amide group Chemical group 0.000 claims description 13
- 201000011510 cancer Diseases 0.000 claims description 13
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims description 12
- 125000000335 thiazolyl group Chemical group 0.000 claims description 12
- 125000002102 aryl alkyloxo group Chemical group 0.000 claims description 11
- 239000003102 growth factor Substances 0.000 claims description 11
- 125000005843 halogen group Chemical group 0.000 claims description 11
- 125000005114 heteroarylalkoxy group Chemical group 0.000 claims description 11
- 125000005842 heteroatom Chemical group 0.000 claims description 11
- 125000002883 imidazolyl group Chemical group 0.000 claims description 11
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims description 11
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 11
- 125000002971 oxazolyl group Chemical group 0.000 claims description 11
- 125000004592 phthalazinyl group Chemical group C1(=NN=CC2=CC=CC=C12)* 0.000 claims description 11
- 125000004076 pyridyl group Chemical group 0.000 claims description 11
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims description 11
- 125000003831 tetrazolyl group Chemical group 0.000 claims description 11
- 101100381481 Caenorhabditis elegans baz-2 gene Proteins 0.000 claims description 10
- 101100372762 Rattus norvegicus Flt1 gene Proteins 0.000 claims description 10
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims description 10
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims description 10
- 125000001041 indolyl group Chemical group 0.000 claims description 10
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims description 10
- 230000004913 activation Effects 0.000 claims description 9
- 125000003342 alkenyl group Chemical group 0.000 claims description 9
- 125000000304 alkynyl group Chemical group 0.000 claims description 9
- 125000005110 aryl thio group Chemical group 0.000 claims description 9
- 125000004104 aryloxy group Chemical group 0.000 claims description 9
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims description 9
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims description 9
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims description 9
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims description 9
- 125000001951 carbamoylamino group Chemical group C(N)(=O)N* 0.000 claims description 9
- 125000001589 carboacyl group Chemical group 0.000 claims description 9
- 125000002837 carbocyclic group Chemical group 0.000 claims description 9
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims description 9
- 125000005553 heteroaryloxy group Chemical group 0.000 claims description 9
- 125000005368 heteroarylthio group Chemical group 0.000 claims description 9
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims description 9
- 125000003387 indolinyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 claims description 9
- 125000001786 isothiazolyl group Chemical group 0.000 claims description 9
- 125000000842 isoxazolyl group Chemical group 0.000 claims description 9
- 125000001624 naphthyl group Chemical group 0.000 claims description 9
- 230000003287 optical effect Effects 0.000 claims description 9
- 125000001715 oxadiazolyl group Chemical group 0.000 claims description 9
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 9
- 125000005420 sulfonamido group Chemical group S(=O)(=O)(N*)* 0.000 claims description 9
- 125000001712 tetrahydronaphthyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 claims description 9
- 125000001113 thiadiazolyl group Chemical group 0.000 claims description 9
- 101001059454 Homo sapiens Serine/threonine-protein kinase MARK2 Proteins 0.000 claims description 8
- 102100028904 Serine/threonine-protein kinase MARK2 Human genes 0.000 claims description 8
- 108010053100 Vascular Endothelial Growth Factor Receptor-3 Proteins 0.000 claims description 8
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims description 8
- 125000005129 aryl carbonyl group Chemical group 0.000 claims description 8
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims description 8
- 208000035475 disorder Diseases 0.000 claims description 8
- 238000004519 manufacturing process Methods 0.000 claims description 8
- OAICVXFJPJFONN-UHFFFAOYSA-N Phosphorus Chemical compound [P] OAICVXFJPJFONN-UHFFFAOYSA-N 0.000 claims description 7
- 102100040681 Platelet-derived growth factor C Human genes 0.000 claims description 7
- 108010073923 Vascular Endothelial Growth Factor C Proteins 0.000 claims description 7
- 125000003806 alkyl carbonyl amino group Chemical group 0.000 claims description 7
- 125000002947 alkylene group Chemical group 0.000 claims description 7
- 125000004658 aryl carbonyl amino group Chemical group 0.000 claims description 7
- 125000004391 aryl sulfonyl group Chemical group 0.000 claims description 7
- 125000005223 heteroarylcarbonyl group Chemical group 0.000 claims description 7
- 125000005224 heteroarylcarbonylamino group Chemical group 0.000 claims description 7
- 125000005143 heteroarylsulfonyl group Chemical group 0.000 claims description 7
- 125000004437 phosphorous atom Chemical group 0.000 claims description 7
- 239000011574 phosphorus Substances 0.000 claims description 7
- 108010017992 platelet-derived growth factor C Proteins 0.000 claims description 7
- 125000002098 pyridazinyl group Chemical group 0.000 claims description 7
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 7
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims description 7
- 125000006356 alkylene carbonyl group Chemical group 0.000 claims description 6
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 6
- 108090000386 Fibroblast Growth Factor 1 Proteins 0.000 claims description 5
- 108010073919 Vascular Endothelial Growth Factor D Proteins 0.000 claims description 5
- 102000016663 Vascular Endothelial Growth Factor Receptor-3 Human genes 0.000 claims description 5
- 102100033177 Vascular endothelial growth factor receptor 2 Human genes 0.000 claims description 5
- 230000002401 inhibitory effect Effects 0.000 claims description 5
- 125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims description 4
- 206010052779 Transplant rejections Diseases 0.000 claims description 4
- 102000005789 Vascular Endothelial Growth Factors Human genes 0.000 claims description 4
- 108010019530 Vascular Endothelial Growth Factors Proteins 0.000 claims description 4
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 4
- 208000015181 infectious disease Diseases 0.000 claims description 4
- 125000005958 tetrahydrothienyl group Chemical group 0.000 claims description 4
- 125000004632 tetrahydrothiopyranyl group Chemical group S1C(CCCC1)* 0.000 claims description 4
- 102100022014 Angiopoietin-1 receptor Human genes 0.000 claims description 3
- 101100481403 Bos taurus TIE1 gene Proteins 0.000 claims description 3
- 206010012689 Diabetic retinopathy Diseases 0.000 claims description 3
- 102100023593 Fibroblast growth factor receptor 1 Human genes 0.000 claims description 3
- 101710182386 Fibroblast growth factor receptor 1 Proteins 0.000 claims description 3
- 206010017533 Fungal infection Diseases 0.000 claims description 3
- 101000753291 Homo sapiens Angiopoietin-1 receptor Proteins 0.000 claims description 3
- 208000031888 Mycoses Diseases 0.000 claims description 3
- 102100026547 Platelet-derived growth factor receptor beta Human genes 0.000 claims description 3
- 201000004681 Psoriasis Diseases 0.000 claims description 3
- 108010073925 Vascular Endothelial Growth Factor B Proteins 0.000 claims description 3
- 102100038217 Vascular endothelial growth factor B Human genes 0.000 claims description 3
- 230000003463 hyperproliferative effect Effects 0.000 claims description 3
- 230000028709 inflammatory response Effects 0.000 claims description 3
- 208000002780 macular degeneration Diseases 0.000 claims description 3
- 210000001616 monocyte Anatomy 0.000 claims description 3
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 claims description 3
- 208000037803 restenosis Diseases 0.000 claims description 3
- 230000004862 vasculogenesis Effects 0.000 claims description 3
- 125000004485 2-pyrrolidinyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])([H])C1([H])* 0.000 claims description 2
- 101000692455 Homo sapiens Platelet-derived growth factor receptor beta Proteins 0.000 claims description 2
- 206010021143 Hypoxia Diseases 0.000 claims description 2
- 101150028321 Lck gene Proteins 0.000 claims description 2
- 206010030113 Oedema Diseases 0.000 claims description 2
- 241000700639 Parapoxvirus Species 0.000 claims description 2
- 108010053099 Vascular Endothelial Growth Factor Receptor-2 Proteins 0.000 claims description 2
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 2
- 230000007954 hypoxia Effects 0.000 claims description 2
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims description 2
- 125000002757 morpholinyl group Chemical group 0.000 claims description 2
- 125000004193 piperazinyl group Chemical group 0.000 claims description 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 2
- 125000002221 trityl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C([*])(C1=C(C(=C(C(=C1[H])[H])[H])[H])[H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims description 2
- 239000000126 substance Substances 0.000 claims 38
- 208000025865 Ulcer Diseases 0.000 claims 14
- 231100000397 ulcer Toxicity 0.000 claims 14
- 230000001023 pro-angiogenic effect Effects 0.000 claims 7
- 208000028867 ischemia Diseases 0.000 claims 5
- 230000001684 chronic effect Effects 0.000 claims 3
- 206010012601 diabetes mellitus Diseases 0.000 claims 3
- 230000002526 effect on cardiovascular system Effects 0.000 claims 3
- NGNBDVOYPDDBFK-UHFFFAOYSA-N 2-[2,4-di(pentan-2-yl)phenoxy]acetyl chloride Chemical compound CCCC(C)C1=CC=C(OCC(Cl)=O)C(C(C)CCC)=C1 NGNBDVOYPDDBFK-UHFFFAOYSA-N 0.000 claims 2
- DLAJQEFZFUKNBV-UHFFFAOYSA-N 4,4,5,5-tetramethyl-n-phenyl-1,3,2-dioxaborolan-2-amine Chemical compound O1C(C)(C)C(C)(C)OB1NC1=CC=CC=C1 DLAJQEFZFUKNBV-UHFFFAOYSA-N 0.000 claims 2
- 201000001320 Atherosclerosis Diseases 0.000 claims 2
- 230000003844 B-cell-activation Effects 0.000 claims 2
- 208000035143 Bacterial infection Diseases 0.000 claims 2
- 206010009900 Colitis ulcerative Diseases 0.000 claims 2
- 206010010741 Conjunctivitis Diseases 0.000 claims 2
- 206010054044 Diabetic microangiopathy Diseases 0.000 claims 2
- 208000019878 Eales disease Diseases 0.000 claims 2
- 102000003971 Fibroblast Growth Factor 1 Human genes 0.000 claims 2
- 102000003974 Fibroblast growth factor 2 Human genes 0.000 claims 2
- 108090000379 Fibroblast growth factor 2 Proteins 0.000 claims 2
- 201000008808 Fibrosarcoma Diseases 0.000 claims 2
- 206010016654 Fibrosis Diseases 0.000 claims 2
- 206010017711 Gangrene Diseases 0.000 claims 2
- 208000010412 Glaucoma Diseases 0.000 claims 2
- 206010018364 Glomerulonephritis Diseases 0.000 claims 2
- 208000002250 Hematologic Neoplasms Diseases 0.000 claims 2
- 102100021866 Hepatocyte growth factor Human genes 0.000 claims 2
- 208000017604 Hodgkin disease Diseases 0.000 claims 2
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 2
- 101000898034 Homo sapiens Hepatocyte growth factor Proteins 0.000 claims 2
- 101001076408 Homo sapiens Interleukin-6 Proteins 0.000 claims 2
- 101000868152 Homo sapiens Son of sevenless homolog 1 Proteins 0.000 claims 2
- 206010061216 Infarction Diseases 0.000 claims 2
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 2
- 206010025323 Lymphomas Diseases 0.000 claims 2
- 208000001344 Macular Edema Diseases 0.000 claims 2
- 206010025415 Macular oedema Diseases 0.000 claims 2
- 206010025538 Malignant ascites Diseases 0.000 claims 2
- 208000024599 Mooren ulcer Diseases 0.000 claims 2
- 206010028851 Necrosis Diseases 0.000 claims 2
- 206010029260 Neuroblastoma Diseases 0.000 claims 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 2
- 206010063837 Reperfusion injury Diseases 0.000 claims 2
- 206010038848 Retinal detachment Diseases 0.000 claims 2
- 208000017442 Retinal disease Diseases 0.000 claims 2
- 201000000582 Retinoblastoma Diseases 0.000 claims 2
- 206010038923 Retinopathy Diseases 0.000 claims 2
- 206010039491 Sarcoma Diseases 0.000 claims 2
- 206010039705 Scleritis Diseases 0.000 claims 2
- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 claims 2
- 208000027073 Stargardt disease Diseases 0.000 claims 2
- 230000006044 T cell activation Effects 0.000 claims 2
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 2
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 2
- 206010064996 Ulcerative keratitis Diseases 0.000 claims 2
- 206010046851 Uveitis Diseases 0.000 claims 2
- 102000009520 Vascular Endothelial Growth Factor C Human genes 0.000 claims 2
- 102000009519 Vascular Endothelial Growth Factor D Human genes 0.000 claims 2
- 206010053648 Vascular occlusion Diseases 0.000 claims 2
- 206010047663 Vitritis Diseases 0.000 claims 2
- 206010052428 Wound Diseases 0.000 claims 2
- 208000027418 Wounds and injury Diseases 0.000 claims 2
- 208000007502 anemia Diseases 0.000 claims 2
- 230000001580 bacterial effect Effects 0.000 claims 2
- 208000022362 bacterial infectious disease Diseases 0.000 claims 2
- 230000003247 decreasing effect Effects 0.000 claims 2
- 201000009101 diabetic angiopathy Diseases 0.000 claims 2
- 125000000723 dihydrobenzofuranyl group Chemical group O1C(CC2=C1C=CC=C2)* 0.000 claims 2
- 230000035558 fertility Effects 0.000 claims 2
- 208000005017 glioblastoma Diseases 0.000 claims 2
- 230000009033 hematopoietic malignancy Effects 0.000 claims 2
- 210000003630 histaminocyte Anatomy 0.000 claims 2
- 208000013653 hyalitis Diseases 0.000 claims 2
- 230000007574 infarction Effects 0.000 claims 2
- 238000013532 laser treatment Methods 0.000 claims 2
- 208000032839 leukemia Diseases 0.000 claims 2
- 201000010230 macular retinal edema Diseases 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- 201000000050 myeloid neoplasm Diseases 0.000 claims 2
- 208000001491 myopia Diseases 0.000 claims 2
- 230000004379 myopia Effects 0.000 claims 2
- 230000017074 necrotic cell death Effects 0.000 claims 2
- 230000000414 obstructive effect Effects 0.000 claims 2
- 208000008798 osteoma Diseases 0.000 claims 2
- CTSLXHKWHWQRSH-UHFFFAOYSA-N oxalyl chloride Chemical compound ClC(=O)C(Cl)=O CTSLXHKWHWQRSH-UHFFFAOYSA-N 0.000 claims 2
- NFHFRUOZVGFOOS-UHFFFAOYSA-N palladium;triphenylphosphane Chemical compound [Pd].C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1.C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1.C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1.C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1 NFHFRUOZVGFOOS-UHFFFAOYSA-N 0.000 claims 2
- 230000004264 retinal detachment Effects 0.000 claims 2
- 201000009410 rhabdomyosarcoma Diseases 0.000 claims 2
- 208000024891 symptom Diseases 0.000 claims 2
- 208000001608 teratocarcinoma Diseases 0.000 claims 2
- 208000035408 type 1 diabetes mellitus 1 Diseases 0.000 claims 2
- 208000021331 vascular occlusion disease Diseases 0.000 claims 2
- LUSJXEMIZFYDSZ-UHFFFAOYSA-N 3-iodo-2h-pyrazolo[3,4-d]pyrimidine Chemical compound C1=NC=C2C(I)=NNC2=N1 LUSJXEMIZFYDSZ-UHFFFAOYSA-N 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 101100503636 Danio rerio fyna gene Proteins 0.000 claims 1
- 201000009273 Endometriosis Diseases 0.000 claims 1
- 101150018272 FYN gene Proteins 0.000 claims 1
- 208000031953 Hereditary hemorrhagic telangiectasia Diseases 0.000 claims 1
- 208000009889 Herpes Simplex Diseases 0.000 claims 1
- 208000007514 Herpes zoster Diseases 0.000 claims 1
- 241000725303 Human immunodeficiency virus Species 0.000 claims 1
- 206010051151 Hyperviscosity syndrome Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000019693 Lung disease Diseases 0.000 claims 1
- 208000016604 Lyme disease Diseases 0.000 claims 1
- 101150058160 Lyn gene Proteins 0.000 claims 1
- 206010027295 Menometrorrhagia Diseases 0.000 claims 1
- 101100381649 Mus musculus Bik gene Proteins 0.000 claims 1
- 101100381845 Mus musculus Blk gene Proteins 0.000 claims 1
- 208000010191 Osteitis Deformans Diseases 0.000 claims 1
- 206010033266 Ovarian Hyperstimulation Syndrome Diseases 0.000 claims 1
- 101150038994 PDGFRA gene Proteins 0.000 claims 1
- 208000027868 Paget disease Diseases 0.000 claims 1
- 206010034277 Pemphigoid Diseases 0.000 claims 1
- 108010051742 Platelet-Derived Growth Factor beta Receptor Proteins 0.000 claims 1
- 101150001535 SRC gene Proteins 0.000 claims 1
- 206010040047 Sepsis Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 201000005485 Toxoplasmosis Diseases 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 150000001732 carboxylic acid derivatives Chemical class 0.000 claims 1
- 208000037976 chronic inflammation Diseases 0.000 claims 1
- 230000006020 chronic inflammation Effects 0.000 claims 1
- 230000007882 cirrhosis Effects 0.000 claims 1
- 208000019425 cirrhosis of liver Diseases 0.000 claims 1
- 230000004761 fibrosis Effects 0.000 claims 1
- 208000014674 injury Diseases 0.000 claims 1
- 206010025135 lupus erythematosus Diseases 0.000 claims 1
- 208000027202 mammary Paget disease Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 208000030761 polycystic kidney disease Diseases 0.000 claims 1
- 201000011461 pre-eclampsia Diseases 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 230000005855 radiation Effects 0.000 claims 1
- 201000000306 sarcoidosis Diseases 0.000 claims 1
- 208000007056 sickle cell anemia Diseases 0.000 claims 1
- 229910000029 sodium carbonate Inorganic materials 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 201000004595 synovitis Diseases 0.000 claims 1
- 230000009885 systemic effect Effects 0.000 claims 1
- 206010043778 thyroiditis Diseases 0.000 claims 1
- 230000008733 trauma Effects 0.000 claims 1
- 208000006542 von Hippel-Lindau disease Diseases 0.000 claims 1
- 210000004027 cell Anatomy 0.000 description 41
- 102000005962 receptors Human genes 0.000 description 25
- 108020003175 receptors Proteins 0.000 description 24
- 230000005764 inhibitory process Effects 0.000 description 19
- 108091008598 receptor tyrosine kinases Proteins 0.000 description 19
- 102000027426 receptor tyrosine kinases Human genes 0.000 description 18
- 239000003446 ligand Substances 0.000 description 16
- 108091000080 Phosphotransferase Proteins 0.000 description 14
- 102000020233 phosphotransferase Human genes 0.000 description 14
- 108090000623 proteins and genes Proteins 0.000 description 11
- 239000000758 substrate Substances 0.000 description 11
- 108091007914 CDKs Proteins 0.000 description 10
- 102000004190 Enzymes Human genes 0.000 description 10
- 108090000790 Enzymes Proteins 0.000 description 10
- 229940088598 enzyme Drugs 0.000 description 10
- 229910052740 iodine Inorganic materials 0.000 description 10
- 230000014509 gene expression Effects 0.000 description 9
- 238000006366 phosphorylation reaction Methods 0.000 description 9
- 102000004169 proteins and genes Human genes 0.000 description 9
- 108010024986 Cyclin-Dependent Kinase 2 Proteins 0.000 description 8
- 102100036239 Cyclin-dependent kinase 2 Human genes 0.000 description 8
- 239000003112 inhibitor Substances 0.000 description 8
- 108091008046 non-receptor tyrosine kinases Proteins 0.000 description 8
- 102000037979 non-receptor tyrosine kinases Human genes 0.000 description 8
- 230000026731 phosphorylation Effects 0.000 description 8
- 235000018102 proteins Nutrition 0.000 description 8
- 230000004663 cell proliferation Effects 0.000 description 7
- 230000001413 cellular effect Effects 0.000 description 7
- 230000006870 function Effects 0.000 description 7
- 101150012716 CDK1 gene Proteins 0.000 description 6
- 230000033228 biological regulation Effects 0.000 description 6
- 210000002889 endothelial cell Anatomy 0.000 description 6
- 230000008569 process Effects 0.000 description 6
- 230000019491 signal transduction Effects 0.000 description 6
- 230000002792 vascular Effects 0.000 description 6
- 230000008728 vascular permeability Effects 0.000 description 6
- 101100464293 Caenorhabditis elegans plk-1 gene Proteins 0.000 description 5
- 102000016736 Cyclin Human genes 0.000 description 5
- 108050006400 Cyclin Proteins 0.000 description 5
- 102000003903 Cyclin-dependent kinases Human genes 0.000 description 5
- 108090000266 Cyclin-dependent kinases Proteins 0.000 description 5
- 108010057466 NF-kappa B Proteins 0.000 description 5
- 102000003945 NF-kappa B Human genes 0.000 description 5
- 108700020796 Oncogene Proteins 0.000 description 5
- 235000008331 Pinus X rigitaeda Nutrition 0.000 description 5
- 235000011613 Pinus brutia Nutrition 0.000 description 5
- 241000018646 Pinus brutia Species 0.000 description 5
- 102100038232 Vascular endothelial growth factor C Human genes 0.000 description 5
- 230000015572 biosynthetic process Effects 0.000 description 5
- 230000003993 interaction Effects 0.000 description 5
- 230000003834 intracellular effect Effects 0.000 description 5
- 230000035755 proliferation Effects 0.000 description 5
- 238000012552 review Methods 0.000 description 5
- 210000003556 vascular endothelial cell Anatomy 0.000 description 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 4
- 102000002427 Cyclin B Human genes 0.000 description 4
- 108010068150 Cyclin B Proteins 0.000 description 4
- 101100323232 Mus musculus Ang3 gene Proteins 0.000 description 4
- 102100035194 Placenta growth factor Human genes 0.000 description 4
- 230000018199 S phase Effects 0.000 description 4
- 150000001413 amino acids Chemical group 0.000 description 4
- 230000022131 cell cycle Effects 0.000 description 4
- 230000033077 cellular process Effects 0.000 description 4
- 230000004069 differentiation Effects 0.000 description 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 4
- 125000002768 hydroxyalkyl group Chemical group 0.000 description 4
- 238000001727 in vivo Methods 0.000 description 4
- 229940043355 kinase inhibitor Drugs 0.000 description 4
- 230000001404 mediated effect Effects 0.000 description 4
- 125000004430 oxygen atom Chemical group O* 0.000 description 4
- 239000003757 phosphotransferase inhibitor Substances 0.000 description 4
- 238000011160 research Methods 0.000 description 4
- 230000004044 response Effects 0.000 description 4
- 230000000638 stimulation Effects 0.000 description 4
- 210000001519 tissue Anatomy 0.000 description 4
- 102100034608 Angiopoietin-2 Human genes 0.000 description 3
- 101100059559 Emericella nidulans (strain FGSC A4 / ATCC 38163 / CBS 112.46 / NRRL 194 / M139) nimX gene Proteins 0.000 description 3
- 102100031706 Fibroblast growth factor 1 Human genes 0.000 description 3
- HTTJABKRGRZYRN-UHFFFAOYSA-N Heparin Chemical compound OC1C(NC(=O)C)C(O)OC(COS(O)(=O)=O)C1OC1C(OS(O)(=O)=O)C(O)C(OC2C(C(OS(O)(=O)=O)C(OC3C(C(O)C(O)C(O3)C(O)=O)OS(O)(=O)=O)C(CO)O2)NS(O)(=O)=O)C(C(O)=O)O1 HTTJABKRGRZYRN-UHFFFAOYSA-N 0.000 description 3
- 101001001487 Homo sapiens Phosphatidylinositol-glycan biosynthesis class F protein Proteins 0.000 description 3
- 101000595923 Homo sapiens Placenta growth factor Proteins 0.000 description 3
- 101000808011 Homo sapiens Vascular endothelial growth factor A Proteins 0.000 description 3
- 206010029113 Neovascularisation Diseases 0.000 description 3
- 102000001708 Protein Isoforms Human genes 0.000 description 3
- 108010029485 Protein Isoforms Proteins 0.000 description 3
- 108091008605 VEGF receptors Proteins 0.000 description 3
- 102100038234 Vascular endothelial growth factor D Human genes 0.000 description 3
- 102100033179 Vascular endothelial growth factor receptor 3 Human genes 0.000 description 3
- 101100273808 Xenopus laevis cdk1-b gene Proteins 0.000 description 3
- 125000004453 alkoxycarbonyl group Chemical group 0.000 description 3
- 230000035578 autophosphorylation Effects 0.000 description 3
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 description 3
- 238000004891 communication Methods 0.000 description 3
- 230000001419 dependent effect Effects 0.000 description 3
- 238000011161 development Methods 0.000 description 3
- 230000018109 developmental process Effects 0.000 description 3
- 229960002897 heparin Drugs 0.000 description 3
- 229920000669 heparin Polymers 0.000 description 3
- 102000058223 human VEGFA Human genes 0.000 description 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 3
- 230000001105 regulatory effect Effects 0.000 description 3
- 241000894007 species Species 0.000 description 3
- 125000005504 styryl group Chemical group 0.000 description 3
- 125000001493 tyrosinyl group Chemical group [H]OC1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])(N([H])[H])C(*)=O 0.000 description 3
- MTCFGRXMJLQNBG-REOHCLBHSA-N (2S)-2-Amino-3-hydroxypropansäure Chemical compound OC[C@H](N)C(O)=O MTCFGRXMJLQNBG-REOHCLBHSA-N 0.000 description 2
- 208000023275 Autoimmune disease Diseases 0.000 description 2
- 206010006187 Breast cancer Diseases 0.000 description 2
- 208000026310 Breast neoplasm Diseases 0.000 description 2
- 208000005623 Carcinogenesis Diseases 0.000 description 2
- 102000002554 Cyclin A Human genes 0.000 description 2
- 108010068192 Cyclin A Proteins 0.000 description 2
- 241000282412 Homo Species 0.000 description 2
- 101000924533 Homo sapiens Angiopoietin-2 Proteins 0.000 description 2
- 101000851007 Homo sapiens Vascular endothelial growth factor receptor 2 Proteins 0.000 description 2
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 description 2
- 102100028762 Neuropilin-1 Human genes 0.000 description 2
- 108090000772 Neuropilin-1 Proteins 0.000 description 2
- 241000700635 Orf virus Species 0.000 description 2
- 101000852966 Rattus norvegicus Interleukin-1 receptor-like 1 Proteins 0.000 description 2
- 108060006706 SRC Proteins 0.000 description 2
- 102000001332 SRC Human genes 0.000 description 2
- MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 description 2
- 102000002262 Thromboplastin Human genes 0.000 description 2
- 108010000499 Thromboplastin Proteins 0.000 description 2
- 108010073929 Vascular Endothelial Growth Factor A Proteins 0.000 description 2
- 208000036142 Viral infection Diseases 0.000 description 2
- 241000700605 Viruses Species 0.000 description 2
- 230000002159 abnormal effect Effects 0.000 description 2
- 125000005078 alkoxycarbonylalkyl group Chemical group 0.000 description 2
- 230000002491 angiogenic effect Effects 0.000 description 2
- 238000013459 approach Methods 0.000 description 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 2
- 230000004071 biological effect Effects 0.000 description 2
- 210000004204 blood vessel Anatomy 0.000 description 2
- 229910052794 bromium Inorganic materials 0.000 description 2
- 230000036952 cancer formation Effects 0.000 description 2
- 125000004181 carboxyalkyl group Chemical group 0.000 description 2
- 231100000504 carcinogenesis Toxicity 0.000 description 2
- 230000006369 cell cycle progression Effects 0.000 description 2
- 230000036755 cellular response Effects 0.000 description 2
- 229910052801 chlorine Inorganic materials 0.000 description 2
- 125000004966 cyanoalkyl group Chemical group 0.000 description 2
- 230000001086 cytosolic effect Effects 0.000 description 2
- 231100000433 cytotoxic Toxicity 0.000 description 2
- 230000001472 cytotoxic effect Effects 0.000 description 2
- 239000000539 dimer Substances 0.000 description 2
- 230000003511 endothelial effect Effects 0.000 description 2
- 229910052731 fluorine Inorganic materials 0.000 description 2
- 230000012010 growth Effects 0.000 description 2
- 239000000833 heterodimer Substances 0.000 description 2
- 238000005734 heterodimerization reaction Methods 0.000 description 2
- 238000000338 in vitro Methods 0.000 description 2
- 230000002779 inactivation Effects 0.000 description 2
- 230000001939 inductive effect Effects 0.000 description 2
- 230000031146 intracellular signal transduction Effects 0.000 description 2
- 210000004072 lung Anatomy 0.000 description 2
- 239000011159 matrix material Substances 0.000 description 2
- 108020004999 messenger RNA Proteins 0.000 description 2
- 238000013508 migration Methods 0.000 description 2
- 230000002297 mitogenic effect Effects 0.000 description 2
- 230000000394 mitotic effect Effects 0.000 description 2
- 210000002569 neuron Anatomy 0.000 description 2
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 description 2
- 125000003170 phenylsulfonyl group Chemical group C1(=CC=CC=C1)S(=O)(=O)* 0.000 description 2
- DCWXELXMIBXGTH-UHFFFAOYSA-N phosphotyrosine Chemical compound OC(=O)C(N)CC1=CC=C(OP(O)(O)=O)C=C1 DCWXELXMIBXGTH-UHFFFAOYSA-N 0.000 description 2
- 230000003389 potentiating effect Effects 0.000 description 2
- 230000006884 regulation of angiogenesis Effects 0.000 description 2
- 230000011664 signaling Effects 0.000 description 2
- 150000003384 small molecules Chemical class 0.000 description 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- 125000000341 threoninyl group Chemical group [H]OC([H])(C([H])([H])[H])C([H])(N([H])[H])C(*)=O 0.000 description 2
- 231100000419 toxicity Toxicity 0.000 description 2
- 230000001988 toxicity Effects 0.000 description 2
- 230000009261 transgenic effect Effects 0.000 description 2
- 230000007704 transition Effects 0.000 description 2
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 description 2
- 229940121358 tyrosine kinase inhibitor Drugs 0.000 description 2
- 239000005483 tyrosine kinase inhibitor Substances 0.000 description 2
- 230000006459 vascular development Effects 0.000 description 2
- 210000005166 vasculature Anatomy 0.000 description 2
- 230000009385 viral infection Effects 0.000 description 2
- 108091032973 (ribonucleotides)n+m Proteins 0.000 description 1
- WIQRSJOCVVPMPS-UHFFFAOYSA-N 3-(1h-indol-2-yl)pyrrole-2,5-dione Chemical class O=C1NC(=O)C(C=2NC3=CC=CC=C3C=2)=C1 WIQRSJOCVVPMPS-UHFFFAOYSA-N 0.000 description 1
- 108010048036 Angiopoietin-2 Proteins 0.000 description 1
- 108010009906 Angiopoietins Proteins 0.000 description 1
- 102000009840 Angiopoietins Human genes 0.000 description 1
- 206010003445 Ascites Diseases 0.000 description 1
- 201000002909 Aspergillosis Diseases 0.000 description 1
- 241000228212 Aspergillus Species 0.000 description 1
- 208000036641 Aspergillus infections Diseases 0.000 description 1
- OGBVRMYSNSKIEF-UHFFFAOYSA-N Benzylphosphonic acid Chemical class OP(O)(=O)CC1=CC=CC=C1 OGBVRMYSNSKIEF-UHFFFAOYSA-N 0.000 description 1
- 101150047144 CDC28 gene Proteins 0.000 description 1
- 241000283707 Capra Species 0.000 description 1
- 235000002566 Capsicum Nutrition 0.000 description 1
- 102000016289 Cell Adhesion Molecules Human genes 0.000 description 1
- 108010067225 Cell Adhesion Molecules Proteins 0.000 description 1
- 102000019034 Chemokines Human genes 0.000 description 1
- 108010012236 Chemokines Proteins 0.000 description 1
- 208000005590 Choroidal Neovascularization Diseases 0.000 description 1
- 206010060823 Choroidal neovascularisation Diseases 0.000 description 1
- 208000035473 Communicable disease Diseases 0.000 description 1
- 102000003910 Cyclin D Human genes 0.000 description 1
- 108090000259 Cyclin D Proteins 0.000 description 1
- 102000003909 Cyclin E Human genes 0.000 description 1
- 108090000257 Cyclin E Proteins 0.000 description 1
- 108010025464 Cyclin-Dependent Kinase 4 Proteins 0.000 description 1
- 102100032857 Cyclin-dependent kinase 1 Human genes 0.000 description 1
- 101710106279 Cyclin-dependent kinase 1 Proteins 0.000 description 1
- 102100036252 Cyclin-dependent kinase 4 Human genes 0.000 description 1
- 108090000695 Cytokines Proteins 0.000 description 1
- 102000004127 Cytokines Human genes 0.000 description 1
- 108020004414 DNA Proteins 0.000 description 1
- 230000006820 DNA synthesis Effects 0.000 description 1
- BWGNESOTFCXPMA-UHFFFAOYSA-N Dihydrogen disulfide Chemical compound SS BWGNESOTFCXPMA-UHFFFAOYSA-N 0.000 description 1
- 206010063045 Effusion Diseases 0.000 description 1
- 206010015866 Extravasation Diseases 0.000 description 1
- 241000233866 Fungi Species 0.000 description 1
- 102000001267 GSK3 Human genes 0.000 description 1
- 108060006662 GSK3 Proteins 0.000 description 1
- 102000002254 Glycogen Synthase Kinase 3 Human genes 0.000 description 1
- 108010014905 Glycogen Synthase Kinase 3 Proteins 0.000 description 1
- 108010009202 Growth Factor Receptors Proteins 0.000 description 1
- 102000009465 Growth Factor Receptors Human genes 0.000 description 1
- 101001005128 Homo sapiens LIM domain kinase 1 Proteins 0.000 description 1
- 101001092185 Homo sapiens Regulator of cell cycle RGCC Proteins 0.000 description 1
- 241000701806 Human papillomavirus Species 0.000 description 1
- 206010061218 Inflammation Diseases 0.000 description 1
- 102100026023 LIM domain kinase 1 Human genes 0.000 description 1
- 108010002481 Lymphocyte Specific Protein Tyrosine Kinase p56(lck) Proteins 0.000 description 1
- 102000036243 Lymphocyte Specific Protein Tyrosine Kinase p56(lck) Human genes 0.000 description 1
- 206010027476 Metastases Diseases 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 102100023482 Mitogen-activated protein kinase 14 Human genes 0.000 description 1
- 102000007474 Multiprotein Complexes Human genes 0.000 description 1
- 241001529936 Murinae Species 0.000 description 1
- 101100216078 Mus musculus Ang4 gene Proteins 0.000 description 1
- 101000851005 Mus musculus Vascular endothelial growth factor receptor 2 Proteins 0.000 description 1
- 101100268066 Mus musculus Zap70 gene Proteins 0.000 description 1
- 208000001132 Osteoporosis Diseases 0.000 description 1
- 108091008606 PDGF receptors Proteins 0.000 description 1
- 229910019142 PO4 Inorganic materials 0.000 description 1
- 241001111421 Pannus Species 0.000 description 1
- 208000034038 Pathologic Neovascularization Diseases 0.000 description 1
- 241001494479 Pecora Species 0.000 description 1
- 239000006002 Pepper Substances 0.000 description 1
- 102000004160 Phosphoric Monoester Hydrolases Human genes 0.000 description 1
- 108090000608 Phosphoric Monoester Hydrolases Proteins 0.000 description 1
- 235000016761 Piper aduncum Nutrition 0.000 description 1
- 235000017804 Piper guineense Nutrition 0.000 description 1
- 244000203593 Piper nigrum Species 0.000 description 1
- 235000008184 Piper nigrum Nutrition 0.000 description 1
- 108010082093 Placenta Growth Factor Proteins 0.000 description 1
- 102000012335 Plasminogen Activator Inhibitor 1 Human genes 0.000 description 1
- 108010022233 Plasminogen Activator Inhibitor 1 Proteins 0.000 description 1
- 102100037787 Protein-tyrosine kinase 2-beta Human genes 0.000 description 1
- 108010071563 Proto-Oncogene Proteins c-fos Proteins 0.000 description 1
- 102000007568 Proto-Oncogene Proteins c-fos Human genes 0.000 description 1
- 101000851003 Rattus norvegicus Vascular endothelial growth factor receptor 2 Proteins 0.000 description 1
- 102000004278 Receptor Protein-Tyrosine Kinases Human genes 0.000 description 1
- 108090000873 Receptor Protein-Tyrosine Kinases Proteins 0.000 description 1
- 102100035542 Regulator of cell cycle RGCC Human genes 0.000 description 1
- 206010038933 Retinopathy of prematurity Diseases 0.000 description 1
- 241000283984 Rodentia Species 0.000 description 1
- 102000014400 SH2 domains Human genes 0.000 description 1
- 108050003452 SH2 domains Proteins 0.000 description 1
- 101710172711 Structural protein Proteins 0.000 description 1
- 102000003990 Urokinase-type plasminogen activator Human genes 0.000 description 1
- 108090000435 Urokinase-type plasminogen activator Proteins 0.000 description 1
- 108010053096 Vascular Endothelial Growth Factor Receptor-1 Proteins 0.000 description 1
- 102000016549 Vascular Endothelial Growth Factor Receptor-2 Human genes 0.000 description 1
- 102000009484 Vascular Endothelial Growth Factor Receptors Human genes 0.000 description 1
- 108010034265 Vascular Endothelial Growth Factor Receptors Proteins 0.000 description 1
- 102100039037 Vascular endothelial growth factor A Human genes 0.000 description 1
- 102100033178 Vascular endothelial growth factor receptor 1 Human genes 0.000 description 1
- 230000001594 aberrant effect Effects 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- 230000003213 activating effect Effects 0.000 description 1
- 230000002411 adverse Effects 0.000 description 1
- 206010064930 age-related macular degeneration Diseases 0.000 description 1
- 239000000556 agonist Substances 0.000 description 1
- 230000001270 agonistic effect Effects 0.000 description 1
- 150000001412 amines Chemical class 0.000 description 1
- 235000001014 amino acid Nutrition 0.000 description 1
- 125000000539 amino acid group Chemical group 0.000 description 1
- 230000003042 antagnostic effect Effects 0.000 description 1
- 239000005557 antagonist Substances 0.000 description 1
- 230000001772 anti-angiogenic effect Effects 0.000 description 1
- 239000002246 antineoplastic agent Substances 0.000 description 1
- 230000001640 apoptogenic effect Effects 0.000 description 1
- 230000006907 apoptotic process Effects 0.000 description 1
- 230000002917 arthritic effect Effects 0.000 description 1
- 206010003246 arthritis Diseases 0.000 description 1
- 238000003556 assay Methods 0.000 description 1
- 125000004429 atom Chemical group 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 125000002619 bicyclic group Chemical group 0.000 description 1
- 230000002051 biphasic effect Effects 0.000 description 1
- 210000000988 bone and bone Anatomy 0.000 description 1
- 230000009702 cancer cell proliferation Effects 0.000 description 1
- 208000001969 capillary hemangioma Diseases 0.000 description 1
- 125000004432 carbon atom Chemical group C* 0.000 description 1
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 description 1
- 230000003197 catalytic effect Effects 0.000 description 1
- 230000020411 cell activation Effects 0.000 description 1
- 230000021164 cell adhesion Effects 0.000 description 1
- 230000030833 cell death Effects 0.000 description 1
- 230000024245 cell differentiation Effects 0.000 description 1
- 230000032823 cell division Effects 0.000 description 1
- 230000003915 cell function Effects 0.000 description 1
- 230000010261 cell growth Effects 0.000 description 1
- 210000000170 cell membrane Anatomy 0.000 description 1
- 230000012292 cell migration Effects 0.000 description 1
- 230000019522 cellular metabolic process Effects 0.000 description 1
- 230000005754 cellular signaling Effects 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 230000035605 chemotaxis Effects 0.000 description 1
- 230000003081 coactivator Effects 0.000 description 1
- 235000018417 cysteine Nutrition 0.000 description 1
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 description 1
- 229940127089 cytotoxic agent Drugs 0.000 description 1
- 230000009849 deactivation Effects 0.000 description 1
- 230000034994 death Effects 0.000 description 1
- 230000008021 deposition Effects 0.000 description 1
- 238000006471 dimerization reaction Methods 0.000 description 1
- 208000037765 diseases and disorders Diseases 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 238000007876 drug discovery Methods 0.000 description 1
- 210000002257 embryonic structure Anatomy 0.000 description 1
- 230000002124 endocrine Effects 0.000 description 1
- 230000036251 extravasation Effects 0.000 description 1
- 210000000416 exudates and transudate Anatomy 0.000 description 1
- 230000001605 fetal effect Effects 0.000 description 1
- 210000002950 fibroblast Anatomy 0.000 description 1
- 208000024908 graft versus host disease Diseases 0.000 description 1
- 238000011102 hetero oligomerization reaction Methods 0.000 description 1
- 125000006517 heterocyclyl carbonyl group Chemical group 0.000 description 1
- 230000000521 hyperimmunizing effect Effects 0.000 description 1
- 230000028993 immune response Effects 0.000 description 1
- 210000000987 immune system Anatomy 0.000 description 1
- 230000000415 inactivating effect Effects 0.000 description 1
- 230000006698 induction Effects 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 230000000977 initiatory effect Effects 0.000 description 1
- 210000003734 kidney Anatomy 0.000 description 1
- 230000003902 lesion Effects 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 210000005073 lymphatic endothelial cell Anatomy 0.000 description 1
- 210000001365 lymphatic vessel Anatomy 0.000 description 1
- 238000012423 maintenance Methods 0.000 description 1
- 230000036244 malformation Effects 0.000 description 1
- 230000003211 malignant effect Effects 0.000 description 1
- 230000035800 maturation Effects 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- 230000002503 metabolic effect Effects 0.000 description 1
- 230000031864 metaphase Effects 0.000 description 1
- 230000009401 metastasis Effects 0.000 description 1
- 230000005012 migration Effects 0.000 description 1
- 239000003226 mitogen Substances 0.000 description 1
- 230000011278 mitosis Effects 0.000 description 1
- 210000000479 mitotic spindle apparatus Anatomy 0.000 description 1
- 125000002950 monocyclic group Chemical group 0.000 description 1
- 230000035772 mutation Effects 0.000 description 1
- 239000002773 nucleotide Substances 0.000 description 1
- 125000003729 nucleotide group Chemical group 0.000 description 1
- 230000008520 organization Effects 0.000 description 1
- 210000000963 osteoblast Anatomy 0.000 description 1
- 210000002997 osteoclast Anatomy 0.000 description 1
- 230000002018 overexpression Effects 0.000 description 1
- 125000004043 oxo group Chemical group O=* 0.000 description 1
- 230000001717 pathogenic effect Effects 0.000 description 1
- 230000037361 pathway Effects 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
- 239000010452 phosphate Substances 0.000 description 1
- 125000002467 phosphate group Chemical group [H]OP(=O)(O[H])O[*] 0.000 description 1
- DCWXELXMIBXGTH-QMMMGPOBSA-N phosphonotyrosine Chemical group OC(=O)[C@@H](N)CC1=CC=C(OP(O)(O)=O)C=C1 DCWXELXMIBXGTH-QMMMGPOBSA-N 0.000 description 1
- LFGREXWGYUGZLY-UHFFFAOYSA-N phosphoryl Chemical group [P]=O LFGREXWGYUGZLY-UHFFFAOYSA-N 0.000 description 1
- 230000004481 post-translational protein modification Effects 0.000 description 1
- 230000002062 proliferating effect Effects 0.000 description 1
- 230000007115 recruitment Effects 0.000 description 1
- 230000022983 regulation of cell cycle Effects 0.000 description 1
- 230000006760 regulation of extracellular matrix disassembly Effects 0.000 description 1
- 238000007634 remodeling Methods 0.000 description 1
- 150000003346 selenoethers Chemical class 0.000 description 1
- 230000009919 sequestration Effects 0.000 description 1
- 238000001228 spectrum Methods 0.000 description 1
- 239000004575 stone Substances 0.000 description 1
- 230000008093 supporting effect Effects 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 230000004083 survival effect Effects 0.000 description 1
- 230000008685 targeting Effects 0.000 description 1
- 230000002123 temporal effect Effects 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 230000002463 transducing effect Effects 0.000 description 1
- 238000012546 transfer Methods 0.000 description 1
- 238000006276 transfer reaction Methods 0.000 description 1
- 102000027257 transmembrane receptors Human genes 0.000 description 1
- 108091008578 transmembrane receptors Proteins 0.000 description 1
- 210000004881 tumor cell Anatomy 0.000 description 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 description 1
- 230000003827 upregulation Effects 0.000 description 1
- 230000029812 viral genome replication Effects 0.000 description 1
- 230000029663 wound healing Effects 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- 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
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- 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
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/18—Feminine 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
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- 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
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
-
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
-
- 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)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Immunology (AREA)
- Hematology (AREA)
- Ophthalmology & Optometry (AREA)
- Pulmonology (AREA)
- Physical Education & Sports Medicine (AREA)
- Endocrinology (AREA)
- Oncology (AREA)
- Rheumatology (AREA)
- Urology & Nephrology (AREA)
- Reproductive Health (AREA)
- Heart & Thoracic Surgery (AREA)
- Dermatology (AREA)
- Cardiology (AREA)
- Communicable Diseases (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Gynecology & Obstetrics (AREA)
- Emergency Medicine (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Transplantation (AREA)
- Virology (AREA)
- Vascular Medicine (AREA)
- Biomedical Technology (AREA)
- Obesity (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US27804701P | 2001-03-22 | 2001-03-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA200306887B true ZA200306887B (en) | 2004-09-13 |
Family
ID=23063472
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA200306887A ZA200306887B (en) | 2001-03-22 | 2003-09-03 | Pyrazolopyrimidines as therapeutic agents. |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US7332497B2 (ja) |
| EP (1) | EP1379528A4 (ja) |
| JP (1) | JP4319412B2 (ja) |
| KR (1) | KR20030088114A (ja) |
| CN (1) | CN101426792A (ja) |
| BG (1) | BG108268A (ja) |
| BR (1) | BR0205890A (ja) |
| CA (1) | CA2440714C (ja) |
| CO (1) | CO5570669A2 (ja) |
| CZ (1) | CZ20032837A3 (ja) |
| EC (1) | ECSP034773A (ja) |
| HU (1) | HUP0400267A2 (ja) |
| IL (1) | IL157640A0 (ja) |
| MX (1) | MXPA03008560A (ja) |
| NO (1) | NO20034177L (ja) |
| PE (1) | PE20030047A1 (ja) |
| PL (1) | PL363946A1 (ja) |
| SK (1) | SK13122003A3 (ja) |
| UY (1) | UY27222A1 (ja) |
| WO (1) | WO2002076986A1 (ja) |
| ZA (1) | ZA200306887B (ja) |
Families Citing this family (133)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6921763B2 (en) * | 1999-09-17 | 2005-07-26 | Abbott Laboratories | Pyrazolopyrimidines as therapeutic agents |
| AU8473401A (en) * | 2000-08-04 | 2002-02-18 | Human Genome Sciences, Inc. | Vascular endothelial growth factor 2 |
| DE60236646D1 (de) * | 2001-04-13 | 2010-07-22 | Human Genome Sciences Inc | Anti-VEGF-2 Antikörper |
| EP1385862A4 (en) * | 2001-04-13 | 2005-03-02 | Human Genome Sciences Inc | VASCULAR ENDOTHEL GROWTH FACTOR 2 |
| US20050232921A1 (en) * | 2001-04-13 | 2005-10-20 | Rosen Craig A | Vascular endothelial growth factor 2 |
| US20030199525A1 (en) * | 2002-03-21 | 2003-10-23 | Hirst Gavin C. | Kinase inhibitors |
| ATE323702T1 (de) | 2002-08-06 | 2006-05-15 | Astrazeneca Ab | Kondensierte pyridine und pyrimidine mit tie2 (tek) aktivität |
| US20050008640A1 (en) * | 2003-04-23 | 2005-01-13 | Wendy Waegell | Method of treating transplant rejection |
| US7429596B2 (en) * | 2003-06-20 | 2008-09-30 | The Regents Of The University Of California | 1H-pyrrolo [2,3-D] pyrimidine derivatives and methods of use thereof |
| DE10344223A1 (de) * | 2003-09-24 | 2005-04-21 | Merck Patent Gmbh | 1,3-Benzoxazolylderivate als Kinase-Inhibitoren |
| UA83509C2 (en) | 2003-10-15 | 2008-07-25 | Оси Фармасьютикалз, Инк. | Imidazopyrazines as tyrosine kinase inhibitors |
| JP2007520559A (ja) * | 2004-02-03 | 2007-07-26 | アボット・ラボラトリーズ | 治療薬としてのアミノベンゾオキサゾール類 |
| CN102924458B (zh) * | 2004-04-02 | 2014-11-05 | Osi制药有限责任公司 | 6,6-双环取代的杂双环蛋白激酶抑制剂 |
| US20060074102A1 (en) * | 2004-05-14 | 2006-04-06 | Kevin Cusack | Kinase inhibitors as therapeutic agents |
| WO2005112936A1 (en) * | 2004-05-14 | 2005-12-01 | The Regents Of The University Of Michigan | Compositions and methods relating to protein kinase inhibitors |
| AR053090A1 (es) | 2004-07-20 | 2007-04-25 | Osi Pharm Inc | Imidazotriazinas como inhibidores de proteina quinasas y su uso para la preparacion de medicamentos |
| EP1831225A2 (en) * | 2004-11-19 | 2007-09-12 | The Regents of the University of California | Anti-inflammatory pyrazolopyrimidines |
| US8575164B2 (en) * | 2005-12-19 | 2013-11-05 | OSI Pharmaceuticals, LLC | Combination cancer therapy |
| EA200870409A1 (ru) | 2006-04-04 | 2009-04-28 | Дзе Риджентс Оф Дзе Юниверсити Оф Калифорния | Антагонисты киназы pi3 |
| PT2526933E (pt) * | 2006-09-22 | 2015-06-23 | Pharmacyclics Inc | Inibidores da tirosina-quinase de bruton |
| WO2008082856A1 (en) * | 2006-12-26 | 2008-07-10 | Pharmacyclics, Inc. | Method of using histone deacetylase inhibitors and monitoring biomarkers in combination therapy |
| US20080200458A1 (en) * | 2007-01-18 | 2008-08-21 | Joseph Barbosa | Methods and compositions for the treatment of body composition disorders |
| WO2008089307A2 (en) * | 2007-01-18 | 2008-07-24 | Lexicon Pharmaceuticals, Inc. | Delta 5 desaturase inhibitors for the treatment of pain, inflammation and cancer |
| EP2132177B1 (en) * | 2007-03-01 | 2013-07-17 | Novartis AG | Pim kinase inhibitors and methods of their use |
| US20120101113A1 (en) | 2007-03-28 | 2012-04-26 | Pharmacyclics, Inc. | Inhibitors of bruton's tyrosine kinase |
| IL295053A (en) * | 2007-03-28 | 2022-09-01 | Pharmacyclics Llc | Broton tyrosine kinase inhibitors |
| WO2009046448A1 (en) * | 2007-10-04 | 2009-04-09 | Intellikine, Inc. | Chemical entities and therapeutic uses thereof |
| US8193182B2 (en) | 2008-01-04 | 2012-06-05 | Intellikine, Inc. | Substituted isoquinolin-1(2H)-ones, and methods of use thereof |
| MX2010007418A (es) | 2008-01-04 | 2010-11-12 | Intellikine Inc | Ciertas entidades quimicas, composiciones y metodos. |
| EP2250173A1 (en) * | 2008-01-18 | 2010-11-17 | OSI Pharmaceuticals, Inc. | Imidazopyrazinol derivatives for the treatment of cancers |
| US7998688B2 (en) * | 2008-03-07 | 2011-08-16 | OSI Pharmaceuticals, LLC | Inhibition of EMT induction in tumor cells by anti-cancer agents |
| US8993580B2 (en) | 2008-03-14 | 2015-03-31 | Intellikine Llc | Benzothiazole kinase inhibitors and methods of use |
| US8637542B2 (en) | 2008-03-14 | 2014-01-28 | Intellikine, Inc. | Kinase inhibitors and methods of use |
| JP2011520970A (ja) * | 2008-05-19 | 2011-07-21 | オーエスアイ・フアーマスーテイカルズ・インコーポレーテツド | 置換されたイミダゾピラジン類およびイミダゾトリアジン類 |
| US20100101977A1 (en) * | 2008-06-05 | 2010-04-29 | United Comb & Novelty Corporation | Stackable Packaging For Lipped Containers |
| BRPI0915231A2 (pt) | 2008-07-08 | 2018-06-12 | Intellikine Inc | compostos inibidores de quinase e métodos de uso |
| US20110224223A1 (en) * | 2008-07-08 | 2011-09-15 | The Regents Of The University Of California, A California Corporation | MTOR Modulators and Uses Thereof |
| AU2009270856B2 (en) | 2008-07-16 | 2013-07-25 | Pharmacyclics Llc | Inhibitors of Bruton's tyrosine kinase for the treatment of solid tumors |
| WO2010026124A1 (en) | 2008-09-02 | 2010-03-11 | Novartis Ag | Picolinamide derivatives as kinase inhibitors |
| WO2010036380A1 (en) * | 2008-09-26 | 2010-04-01 | Intellikine, Inc. | Heterocyclic kinase inhibitors |
| DK2358720T3 (en) * | 2008-10-16 | 2016-06-06 | Univ California | Heteroarylkinaseinhibitorer fused-ring |
| US8476282B2 (en) | 2008-11-03 | 2013-07-02 | Intellikine Llc | Benzoxazole kinase inhibitors and methods of use |
| CA2752826A1 (en) | 2009-04-20 | 2010-10-28 | OSI Pharmaceuticals, LLC | Preparation of c-pyrazine-methylamines |
| WO2010129740A1 (en) * | 2009-05-07 | 2010-11-11 | Osi Pharmaceuticals, Inc. | Use of osi-906 for treating adrenocortical carcinoma |
| CA2760791C (en) | 2009-05-07 | 2017-06-20 | Intellikine, Inc. | Heterocyclic compounds and uses thereof |
| JP6073677B2 (ja) | 2009-06-12 | 2017-02-01 | デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド | 縮合複素環式化合物およびそれらの使用 |
| GEP201706639B (en) | 2009-08-17 | 2017-03-27 | Intellikine Llc | Heterocyclic compounds and uses thereof |
| US7718662B1 (en) | 2009-10-12 | 2010-05-18 | Pharmacyclics, Inc. | Pyrazolo-pyrimidine inhibitors of bruton's tyrosine kinase |
| US8980899B2 (en) | 2009-10-16 | 2015-03-17 | The Regents Of The University Of California | Methods of inhibiting Ire1 |
| US20110130711A1 (en) * | 2009-11-19 | 2011-06-02 | Follica, Inc. | Hair growth treatment |
| US9180127B2 (en) | 2009-12-29 | 2015-11-10 | Dana-Farber Cancer Institute, Inc. | Type II Raf kinase inhibitors |
| WO2011094628A1 (en) * | 2010-01-28 | 2011-08-04 | University Of Washington | Compositions and methods for treating toxoplasmosis. cryptosporidiosis and other apicomplexan protozoan related diseases |
| US9765037B2 (en) | 2010-01-28 | 2017-09-19 | University Of Washington Through Its Center For Commercialization | Compositions and methods for treating toxoplasmosis, cryptosporidiosis, and other apicomplexan protozoan related diseases |
| EP2571357B1 (en) | 2010-05-21 | 2016-07-06 | Infinity Pharmaceuticals, Inc. | Chemical compounds, compositions and methods for kinase modulation |
| US9096531B2 (en) | 2010-05-24 | 2015-08-04 | Toa Eiyo Ltd. | Fused imidazole derivative |
| EA201890869A3 (ru) | 2010-06-03 | 2019-03-29 | Фармасайкликс, Инк. | Применение ингибиторов тирозинкиназы брутона (btk) |
| WO2011153553A2 (en) * | 2010-06-04 | 2011-12-08 | The Regents Of The University Of California | Methods and compositions for kinase inhibition |
| JP5810157B2 (ja) * | 2010-07-09 | 2015-11-11 | ザ・ウォルター・アンド・エリザ・ホール・インスティテュート・オブ・メディカル・リサーチ | プロテインキナーゼ阻害剤および処置の方法 |
| WO2012064973A2 (en) | 2010-11-10 | 2012-05-18 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| AR084824A1 (es) | 2011-01-10 | 2013-06-26 | Intellikine Inc | Procesos para preparar isoquinolinonas y formas solidas de isoquinolinonas |
| WO2012097196A1 (en) * | 2011-01-12 | 2012-07-19 | Acea Biosciences Inc. | Pyrazolopyrimidine derivatives and uses as anticancer agents |
| AR085397A1 (es) | 2011-02-23 | 2013-09-25 | Intellikine Inc | Combinacion de inhibidores de quinasa y sus usos |
| US9580427B2 (en) | 2011-05-17 | 2017-02-28 | The Regents Of The University Of California | Kinase inhibitors |
| WO2013010136A2 (en) | 2011-07-13 | 2013-01-17 | Pharmacyclics, Inc. | Inhibitors of bruton's tyrosine kinase |
| CN103946226A (zh) | 2011-07-19 | 2014-07-23 | 无限药品股份有限公司 | 杂环化合物及其应用 |
| AU2012284088B2 (en) | 2011-07-19 | 2015-10-08 | Infinity Pharmaceuticals Inc. | Heterocyclic compounds and uses thereof |
| WO2013032591A1 (en) | 2011-08-29 | 2013-03-07 | Infinity Pharmaceuticals Inc. | Heterocyclic compounds and uses thereof |
| AU2012341028C1 (en) | 2011-09-02 | 2017-10-19 | Mount Sinai School Of Medicine | Substituted pyrazolo[3,4-D]pyrimidines and uses thereof |
| ES2627820T3 (es) | 2011-09-13 | 2017-07-31 | Pharmacyclics, Inc. | Formulaciones de inhibidor de histona desacetilasa en combinación con bendamustina y usos de las mismas |
| AU2012340200B2 (en) | 2011-11-17 | 2017-10-12 | Dana-Farber Cancer Institute, Inc. | Inhibitors of c-Jun-N-Terminal Kinase (JNK) |
| US8377946B1 (en) | 2011-12-30 | 2013-02-19 | Pharmacyclics, Inc. | Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase inhibitors |
| US8940742B2 (en) | 2012-04-10 | 2015-01-27 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| PE20150194A1 (es) | 2012-05-21 | 2015-02-08 | Novartis Ag | Novedosas n-piridinil amidas ciclicas sustituidas como inhibidores de quinasa |
| CA3015208C (en) | 2012-06-04 | 2024-01-02 | Pharmacyclics Llc | Crystalline forms of a bruton's tyrosine kinase inhibitor |
| US8828998B2 (en) | 2012-06-25 | 2014-09-09 | Infinity Pharmaceuticals, Inc. | Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors |
| CN104704129A (zh) | 2012-07-24 | 2015-06-10 | 药品循环公司 | 与对布鲁顿酪氨酸激酶(btk)抑制剂的抗性相关的突变 |
| JP6327713B2 (ja) * | 2012-07-27 | 2018-05-23 | 国立研究開発法人理化学研究所 | 急性骨髄性白血病の治療又は再発抑制剤 |
| DK3181567T3 (da) * | 2012-09-10 | 2019-06-11 | Principia Biopharma Inc | Pyrazolopyrimidinforbindelser som kinasehæmmere |
| WO2014052669A1 (en) | 2012-09-26 | 2014-04-03 | The Regents Of The University Of California | Modulation of ire1 |
| WO2014063068A1 (en) | 2012-10-18 | 2014-04-24 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
| WO2014063054A1 (en) | 2012-10-19 | 2014-04-24 | Dana-Farber Cancer Institute, Inc. | Bone marrow on x chromosome kinase (bmx) inhibitors and uses thereof |
| WO2014063061A1 (en) * | 2012-10-19 | 2014-04-24 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged small molecules as inducers of protein degradation |
| BR112015011171A2 (pt) | 2012-11-15 | 2017-07-11 | Pharmacyclics Inc | compostos de pirrolopirimidina como inibidores da quinase |
| WO2014122474A1 (en) | 2013-02-07 | 2014-08-14 | Takeda Pharmaceutical Company Limited | Piperidin-1 -yl and azepin-1 -yl carboxylates as muscarinic m4 receptor agonists |
| US9481667B2 (en) | 2013-03-15 | 2016-11-01 | Infinity Pharmaceuticals, Inc. | Salts and solid forms of isoquinolinones and composition comprising and methods of using the same |
| CN105209042B (zh) | 2013-03-22 | 2019-03-08 | 米伦纽姆医药公司 | 催化性mtorc 1/2抑制剂与选择性极光a激酶抑制剂的组合 |
| EP2999696B1 (en) | 2013-05-20 | 2017-08-16 | University Of Washington Through Its Center For Commercialization | 5-aminopyrazole-4-carboxamide inhibitors of cdpk1 from t. gondii and c. parvum |
| RU2681849C2 (ru) * | 2013-06-05 | 2019-03-13 | Си энд Си РИСЕРЧ ЛЭБОРЕТРИЗ | Гетероциклические производные и их применение |
| GB201311888D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| GB201311891D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compound |
| US9421208B2 (en) | 2013-08-02 | 2016-08-23 | Pharmacyclics Llc | Methods for the treatment of solid tumors |
| ES2709509T3 (es) | 2013-08-12 | 2019-04-16 | Pharmacyclics Llc | Procedimientos para el tratamiento de cáncer amplificado por HER2 |
| CA2925124A1 (en) | 2013-09-30 | 2015-04-02 | Pharmacyclics Llc | Inhibitors of bruton's tyrosine kinase |
| WO2015051241A1 (en) | 2013-10-04 | 2015-04-09 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| JP6466924B2 (ja) | 2013-10-04 | 2019-02-06 | インフィニティー ファーマシューティカルズ， インコーポレイテッド | 複素環式化合物及びその使用 |
| ES2676734T3 (es) | 2013-10-18 | 2018-07-24 | Syros Pharmaceuticals, Inc. | Compuestos heteroatómicos útiles para el tratamiento de enfermedades proliferativas |
| JP6491202B2 (ja) | 2013-10-18 | 2019-03-27 | デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド | サイクリン依存性キナーゼ７（ｃｄｋ７）の多環阻害剤 |
| CA2928721C (en) | 2013-10-25 | 2020-12-22 | Pharmacyclics Llc | Use of ibrutinib for treating and preventing chronic graft versus host disease |
| CN112353806A (zh) | 2014-02-21 | 2021-02-12 | 普林斯匹亚生物制药公司 | Btk抑制剂的盐和固体形式 |
| US9775844B2 (en) | 2014-03-19 | 2017-10-03 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| WO2015143400A1 (en) | 2014-03-20 | 2015-09-24 | Pharmacyclics, Inc. | Phospholipase c gamma 2 and resistance associated mutations |
| US20150320755A1 (en) | 2014-04-16 | 2015-11-12 | Infinity Pharmaceuticals, Inc. | Combination therapies |
| WO2015164614A1 (en) | 2014-04-23 | 2015-10-29 | Dana-Farber Cancer Institute, Inc. | Janus kinase inhibitors and uses thereof |
| WO2015164604A1 (en) | 2014-04-23 | 2015-10-29 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged janus kinase inhibitors and uses thereof |
| AU2015296215A1 (en) | 2014-08-01 | 2017-03-23 | Pharmacyclics Llc | Inhibitors of bruton's tyrosine kinase |
| US9545407B2 (en) | 2014-08-07 | 2017-01-17 | Pharmacyclics Llc | Formulations of a bruton's tyrosine kinase inhibitor |
| US9708348B2 (en) | 2014-10-03 | 2017-07-18 | Infinity Pharmaceuticals, Inc. | Trisubstituted bicyclic heterocyclic compounds with kinase activities and uses thereof |
| US10196397B2 (en) | 2014-11-19 | 2019-02-05 | Sun Pharmaceutical Industries Limited | Process for the preparation of ibrutinib |
| PT3233103T (pt) | 2014-12-18 | 2021-01-18 | Principia Biopharma Inc | Tratamento de pênfigo |
| EP3236959A4 (en) | 2014-12-23 | 2018-04-25 | Dana Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
| KR20170122220A (ko) | 2015-03-03 | 2017-11-03 | 파마싸이클릭스 엘엘씨 | 브루톤 타이로신 키나제 저해제의 약제학적 제제 |
| CA2978518C (en) | 2015-03-27 | 2023-11-21 | Nathanael S. Gray | Inhibitors of cyclin-dependent kinases |
| CN105906630B (zh) * | 2015-04-06 | 2018-10-23 | 四川百利药业有限责任公司 | 用作fgfr抑制剂的n-(1h-吡唑-5-基)嘧啶并吡唑-4,6-二取代胺类化合物 |
| GB201508747D0 (en) * | 2015-05-21 | 2015-07-01 | Univ Edinburgh | Compounds |
| AU2016276963C1 (en) | 2015-06-12 | 2021-08-05 | Dana-Farber Cancer Institute, Inc. | Combination therapy of transcription inhibitors and kinase inhibitors |
| TW201718572A (zh) | 2015-06-24 | 2017-06-01 | 普林斯匹亞生物製藥公司 | 酪胺酸激酶抑制劑 |
| US10688093B2 (en) * | 2015-09-09 | 2020-06-23 | Lau Warren C | Methods, compositions, and uses of novel Fyn kinase inhibitors |
| CA2996978A1 (en) | 2015-09-09 | 2017-03-16 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinases |
| CA2998469A1 (en) | 2015-09-14 | 2017-03-23 | Infinity Pharmaceuticals, Inc. | Solid forms of isoquinolinones, and process of making, composition comprising, and methods of using the same |
| WO2017161116A1 (en) | 2016-03-17 | 2017-09-21 | Infinity Pharmaceuticals, Inc. | Isotopologues of isoquinolinone and quinazolinone compounds and uses thereof as pi3k kinase inhibitors |
| TW201806953A (zh) * | 2016-04-26 | 2018-03-01 | 印度商托仁特生技有限公司 | 取代稠合嘧啶酮化合物 |
| US10919914B2 (en) | 2016-06-08 | 2021-02-16 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| CN107513068A (zh) * | 2016-06-16 | 2017-12-26 | 中国科学院上海药物研究所 | 一种具有fgfr抑制活性的新型化合物及其制备和应用 |
| SG11201811237WA (en) | 2016-06-24 | 2019-01-30 | Infinity Pharmaceuticals Inc | Combination therapies |
| CA3028169A1 (en) | 2016-06-29 | 2018-01-04 | Principia Biopharma Inc. | Modified release formulations of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile |
| BR112019012682A2 (pt) | 2016-12-23 | 2019-12-17 | Arvinas Operations Inc | moléculas quiméricas visando a proteólise de egfr e métodos associados de uso |
| CN108503648B (zh) * | 2018-04-27 | 2020-04-14 | 安徽医科大学 | 苯乙烯基吡唑并嘧啶类化合物、药物组合物及制备方法与用途 |
| WO2020113094A1 (en) | 2018-11-30 | 2020-06-04 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
| CN110015985B (zh) * | 2019-05-16 | 2022-05-13 | 河南师范大学 | 2-(α-氘-α-羟基-α-芳基/烷基)氮杂芳烃类化合物及其制备方法和应用 |
| WO2021038540A1 (en) | 2019-08-31 | 2021-03-04 | Sun Pharma Advanced Research Company Limited | Cycloalkylidene carboxylic acids and derivatives as btk inhibitors |
| AU2020436612A1 (en) | 2020-03-16 | 2022-09-01 | Flash Therapeutics, Llc | Compounds for treating or inhibiting recurrence of acute myeloid leukemia |
| US20230203045A1 (en) | 2020-06-08 | 2023-06-29 | Halia Therapeutics, Inc. | Inhibitors of nek7 kinase |
| CA3214042A1 (en) | 2021-04-05 | 2022-10-13 | Halia Therapeutics, Inc. | Nek7 inhibitors |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4966849A (en) | 1985-09-20 | 1990-10-30 | President And Fellows Of Harvard College | CDNA and genes for human angiogenin (angiogenesis factor) and methods of expression |
| US4966846A (en) * | 1987-10-01 | 1990-10-30 | W. R. Grace & Co.-Conn. | Molecular cloning and expression of a vibrio proteolyticus neutral protease gene |
| US5217999A (en) * | 1987-12-24 | 1993-06-08 | Yissum Research Development Company Of The Hebrew University Of Jerusalem | Styryl compounds which inhibit EGF receptor protein tyrosine kinase |
| WO1991015495A1 (en) | 1990-04-02 | 1991-10-17 | Pfizer Inc. | Benzylphosphonic acid tyrosine kinase inhibitors |
| US5302606A (en) * | 1990-04-16 | 1994-04-12 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Styryl-substituted pyridyl compounds which inhibit EGF receptor tyrosine kinase |
| SG64322A1 (en) | 1991-05-10 | 1999-04-27 | Rhone Poulenc Rorer Int | Bis mono and bicyclic aryl and heteroaryl compounds which inhibit egf and/or pdgf receptor tyrosine kinase |
| EP0586608A1 (en) | 1991-05-29 | 1994-03-16 | Pfizer Inc. | Tricyclic polyhydroxylic tyrosine kinase inhibitors |
| AU661533B2 (en) | 1992-01-20 | 1995-07-27 | Astrazeneca Ab | Quinazoline derivatives |
| CA2140440A1 (en) | 1992-08-06 | 1994-02-17 | Ellen M. Dobrusin | 2-thioindoles (selenoindoles) and related disulfides (selenides) which inhibit protein tyrosine kinases and which have antitumor properties |
| US5330992A (en) * | 1992-10-23 | 1994-07-19 | Sterling Winthrop Inc. | 1-cyclopropyl-4-pyridyl-quinolinones |
| RO119721B1 (ro) | 1992-10-28 | 2005-02-28 | Genentech Inc. | Antagonişti ai factorului de creştere al celulelor vasculare endoteliale |
| GB9226855D0 (en) | 1992-12-23 | 1993-02-17 | Erba Carlo Spa | Vinylene-azaindole derivatives and process for their preparation |
| US5593997A (en) * | 1995-05-23 | 1997-01-14 | Pfizer Inc. | 4-aminopyrazolo(3-,4-D)pyrimidine and 4-aminopyrazolo-(3,4-D)pyridine tyrosine kinase inhibitors |
| GB9624482D0 (en) | 1995-12-18 | 1997-01-15 | Zeneca Phaema S A | Chemical compounds |
| EP0888310B1 (en) | 1996-03-15 | 2005-09-07 | AstraZeneca AB | Cinnoline derivatives and use as medicine |
| UA54427C2 (uk) | 1996-05-01 | 2003-03-17 | Елі Ліллі Енд Компані | Спосіб лікування очних захворювань, які пов'язані з фактором васкулярного ендотеліального росту |
| IL126837A0 (en) | 1996-05-01 | 1999-09-22 | Lilly Co Eli | Therapeutic treatment for vegf related diseases |
| GB9707800D0 (en) | 1996-05-06 | 1997-06-04 | Zeneca Ltd | Chemical compounds |
| ES2251740T3 (es) | 1996-08-23 | 2006-05-01 | Ludwig Institute For Cancer Research | Factor de crecimiento de celulas de endotelio vascular d recombinante (vegf-d). |
| JP4876239B2 (ja) | 1999-01-11 | 2012-02-15 | プリンストン ユニバーシティー | 標的確認のための高親和性阻害剤およびその使用 |
| US6921763B2 (en) * | 1999-09-17 | 2005-07-26 | Abbott Laboratories | Pyrazolopyrimidines as therapeutic agents |
| NZ517758A (en) * | 1999-09-17 | 2004-06-25 | Abbott Gmbh & Co | Pyrazolopyrimidines useful as therapeutic agents |
-
2002
- 2002-03-21 MX MXPA03008560A patent/MXPA03008560A/es active IP Right Grant
- 2002-03-22 CA CA2440714A patent/CA2440714C/en not_active Expired - Fee Related
- 2002-03-22 KR KR10-2003-7012350A patent/KR20030088114A/ko not_active Application Discontinuation
- 2002-03-22 CN CNA028103149A patent/CN101426792A/zh active Pending
- 2002-03-22 PE PE2002000222A patent/PE20030047A1/es not_active Application Discontinuation
- 2002-03-22 UY UY27222A patent/UY27222A1/es not_active Application Discontinuation
- 2002-03-22 CZ CZ20032837A patent/CZ20032837A3/cs unknown
- 2002-03-22 JP JP2002576244A patent/JP4319412B2/ja not_active Expired - Fee Related
- 2002-03-22 IL IL15764002A patent/IL157640A0/xx unknown
- 2002-03-22 SK SK1312-2003A patent/SK13122003A3/sk not_active Application Discontinuation
- 2002-03-22 PL PL02363946A patent/PL363946A1/xx not_active Application Discontinuation
- 2002-03-22 HU HU0400267A patent/HUP0400267A2/hu unknown
- 2002-03-22 EP EP02728546A patent/EP1379528A4/en not_active Withdrawn
- 2002-03-22 BR BR0205890-1A patent/BR0205890A/pt not_active IP Right Cessation
- 2002-03-22 WO PCT/US2002/008996 patent/WO2002076986A1/en not_active Application Discontinuation
- 2002-07-19 US US10/104,140 patent/US7332497B2/en not_active Expired - Fee Related
-
2003
- 2003-09-03 ZA ZA200306887A patent/ZA200306887B/en unknown
- 2003-09-19 NO NO20034177A patent/NO20034177L/no not_active Application Discontinuation
- 2003-09-19 EC EC2003004773A patent/ECSP034773A/es unknown
- 2003-09-22 CO CO03084062A patent/CO5570669A2/es not_active Application Discontinuation
- 2003-10-14 BG BG108268A patent/BG108268A/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CN101426792A (zh) | 2009-05-06 |
| US7332497B2 (en) | 2008-02-19 |
| EP1379528A4 (en) | 2005-12-07 |
| UY27222A1 (es) | 2002-10-31 |
| CA2440714A1 (en) | 2002-10-03 |
| MXPA03008560A (es) | 2004-06-30 |
| PL363946A1 (en) | 2004-11-29 |
| CO5570669A2 (es) | 2005-10-31 |
| NO20034177D0 (no) | 2003-09-19 |
| CZ20032837A3 (cs) | 2004-01-14 |
| JP2005501811A (ja) | 2005-01-20 |
| BR0205890A (pt) | 2004-06-29 |
| ECSP034773A (es) | 2003-12-24 |
| SK13122003A3 (sk) | 2004-04-06 |
| NO20034177L (no) | 2003-11-21 |
| PE20030047A1 (es) | 2003-02-07 |
| KR20030088114A (ko) | 2003-11-17 |
| US20040006083A1 (en) | 2004-01-08 |
| EP1379528A1 (en) | 2004-01-14 |
| WO2002076986A1 (en) | 2002-10-03 |
| IL157640A0 (en) | 2004-03-28 |
| CA2440714C (en) | 2010-08-10 |
| JP4319412B2 (ja) | 2009-08-26 |
| BG108268A (en) | 2005-04-30 |
| HUP0400267A2 (hu) | 2004-08-30 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| ZA200306887B (en) | Pyrazolopyrimidines as therapeutic agents. | |
| JP4707167B2 (ja) | キナーゼ阻害剤 | |
| ZA200202123B (en) | Pyrazolopyrimidines as therapeutic agents. | |
| ZA200202122B (en) | Kinase inhibitors as therapeutic agents. | |
| ZA200102201B (en) | 4-aminopyrrolopyrimidines as kinase inhibitors. | |
| ZA200206235B (en) | 2-Benzothiazolyl urea derivatives and their use as protein kinase inhibitors. | |
| US7829570B2 (en) | Substituted 4-amino isoxazolo[5,4-d]pyrimidines as kinase inhibitors | |
| AU2022219987A1 (en) | Cdk inhibitors and methods of use thereof | |
| JP2002526500A (ja) | プロテインキナーゼ阻害剤としてのピロロピリミジン | |
| JP2004531513A (ja) | 治療剤としてのピラゾールピリミジン | |
| US7071199B1 (en) | Kinase inhibitors as therapeutic agents | |
| BG108286A (bg) | Използване на азитромицин за получаване на фармацевтично средство за лечение на възпалителни неинфекциозни заболявания | |
| WO2016127455A1 (zh) | 嘧啶衍生物、细胞毒性剂、药物组合物及其应用 | |
| ZA200102204B (en) | Pyrrolopyrimidines as protein kinase inhibitors. |