ZA200004652B - Inhibitors of caspases. - Google Patents
Inhibitors of caspases. Download PDFInfo
- Publication number
- ZA200004652B ZA200004652B ZA200004652A ZA200004652A ZA200004652B ZA 200004652 B ZA200004652 B ZA 200004652B ZA 200004652 A ZA200004652 A ZA 200004652A ZA 200004652 A ZA200004652 A ZA 200004652A ZA 200004652 B ZA200004652 B ZA 200004652B
- Authority
- ZA
- South Africa
- Prior art keywords
- alkyl
- aryl
- hydrogen atom
- disease
- optionally replaced
- Prior art date
Links
- 102000011727 Caspases Human genes 0.000 title description 14
- 108010076667 Caspases Proteins 0.000 title description 14
- 239000003112 inhibitor Substances 0.000 title description 11
- 125000000217 alkyl group Chemical group 0.000 claims description 119
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 100
- 150000001875 compounds Chemical class 0.000 claims description 64
- 229910052799 carbon Inorganic materials 0.000 claims description 63
- 125000004122 cyclic group Chemical group 0.000 claims description 51
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 41
- 229910052757 nitrogen Inorganic materials 0.000 claims description 40
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 36
- 125000004429 atom Chemical group 0.000 claims description 32
- 201000010099 disease Diseases 0.000 claims description 28
- 125000003118 aryl group Chemical group 0.000 claims description 27
- 125000000623 heterocyclic group Chemical group 0.000 claims description 24
- 238000004519 manufacturing process Methods 0.000 claims description 22
- 125000003275 alpha amino acid group Chemical group 0.000 claims description 17
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 17
- 230000001404 mediated effect Effects 0.000 claims description 17
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 15
- 208000035475 disorder Diseases 0.000 claims description 13
- 239000008194 pharmaceutical composition Substances 0.000 claims description 13
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 12
- 125000002877 alkyl aryl group Chemical group 0.000 claims description 11
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 11
- 102000000589 Interleukin-1 Human genes 0.000 claims description 10
- 108010002352 Interleukin-1 Proteins 0.000 claims description 10
- 238000000034 method Methods 0.000 claims description 10
- 125000005213 alkyl heteroaryl group Chemical group 0.000 claims description 9
- 125000004432 carbon atom Chemical group C* 0.000 claims description 9
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 8
- 125000001072 heteroaryl group Chemical group 0.000 claims description 8
- 230000002757 inflammatory effect Effects 0.000 claims description 8
- 208000020084 Bone disease Diseases 0.000 claims description 7
- 206010040070 Septic Shock Diseases 0.000 claims description 7
- 230000006907 apoptotic process Effects 0.000 claims description 7
- 239000003814 drug Substances 0.000 claims description 7
- 125000004005 formimidoyl group Chemical group [H]\N=C(/[H])* 0.000 claims description 7
- 230000002401 inhibitory effect Effects 0.000 claims description 7
- 208000032839 leukemia Diseases 0.000 claims description 7
- -1 -NHz Chemical group 0.000 claims description 6
- 230000003247 decreasing effect Effects 0.000 claims description 6
- 208000023275 Autoimmune disease Diseases 0.000 claims description 5
- 208000035473 Communicable disease Diseases 0.000 claims description 5
- 230000001066 destructive effect Effects 0.000 claims description 5
- 208000015181 infectious disease Diseases 0.000 claims description 5
- 208000027866 inflammatory disease Diseases 0.000 claims description 5
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 5
- 230000002062 proliferating effect Effects 0.000 claims description 5
- 239000000203 mixture Substances 0.000 claims description 4
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 4
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 3
- 230000001684 chronic effect Effects 0.000 claims description 2
- 229910052739 hydrogen Inorganic materials 0.000 claims description 2
- 239000001257 hydrogen Substances 0.000 claims description 2
- 208000034578 Multiple myelomas Diseases 0.000 claims 9
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 9
- 208000024827 Alzheimer disease Diseases 0.000 claims 6
- 206010009900 Colitis ulcerative Diseases 0.000 claims 6
- 208000011231 Crohn disease Diseases 0.000 claims 6
- 206010012438 Dermatitis atopic Diseases 0.000 claims 6
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 6
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 6
- 206010033645 Pancreatitis Diseases 0.000 claims 6
- 201000004681 Psoriasis Diseases 0.000 claims 6
- 206010052779 Transplant rejections Diseases 0.000 claims 6
- 208000030886 Traumatic Brain injury Diseases 0.000 claims 6
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 6
- 208000006673 asthma Diseases 0.000 claims 6
- 201000008937 atopic dermatitis Diseases 0.000 claims 6
- 206010014599 encephalitis Diseases 0.000 claims 6
- 210000000056 organ Anatomy 0.000 claims 6
- 201000008482 osteoarthritis Diseases 0.000 claims 6
- 206010034674 peritonitis Diseases 0.000 claims 6
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 6
- 230000036303 septic shock Effects 0.000 claims 6
- 230000009529 traumatic brain injury Effects 0.000 claims 6
- 208000030507 AIDS Diseases 0.000 claims 3
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 3
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims 3
- 201000004384 Alopecia Diseases 0.000 claims 3
- 206010055128 Autoimmune neutropenia Diseases 0.000 claims 3
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 3
- 208000004429 Bacillary Dysentery Diseases 0.000 claims 3
- 201000006474 Brain Ischemia Diseases 0.000 claims 3
- 206010008120 Cerebral ischaemia Diseases 0.000 claims 3
- 206010008909 Chronic Hepatitis Diseases 0.000 claims 3
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 3
- 208000001490 Dengue Diseases 0.000 claims 3
- 206010012310 Dengue fever Diseases 0.000 claims 3
- 206010014596 Encephalitis Japanese B Diseases 0.000 claims 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 3
- 206010018364 Glomerulonephritis Diseases 0.000 claims 3
- 208000009329 Graft vs Host Disease Diseases 0.000 claims 3
- 208000003807 Graves Disease Diseases 0.000 claims 3
- 208000015023 Graves' disease Diseases 0.000 claims 3
- 208000035186 Hemolytic Autoimmune Anemia Diseases 0.000 claims 3
- 208000005176 Hepatitis C Diseases 0.000 claims 3
- 206010019773 Hepatitis G Diseases 0.000 claims 3
- 206010019755 Hepatitis chronic active Diseases 0.000 claims 3
- 101000960954 Homo sapiens Interleukin-18 Proteins 0.000 claims 3
- 102100039898 Interleukin-18 Human genes 0.000 claims 3
- 201000005807 Japanese encephalitis Diseases 0.000 claims 3
- 241000710842 Japanese encephalitis virus Species 0.000 claims 3
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 3
- 206010027480 Metastatic malignant melanoma Diseases 0.000 claims 3
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 3
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 3
- 208000001132 Osteoporosis Diseases 0.000 claims 3
- 208000018737 Parkinson disease Diseases 0.000 claims 3
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 claims 3
- 206010039710 Scleroderma Diseases 0.000 claims 3
- 206010040047 Sepsis Diseases 0.000 claims 3
- 206010040550 Shigella infections Diseases 0.000 claims 3
- 208000006011 Stroke Diseases 0.000 claims 3
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 3
- 208000003152 Yellow Fever Diseases 0.000 claims 3
- 208000011341 adult acute respiratory distress syndrome Diseases 0.000 claims 3
- 201000000028 adult respiratory distress syndrome Diseases 0.000 claims 3
- 230000032683 aging Effects 0.000 claims 3
- 231100000360 alopecia Toxicity 0.000 claims 3
- 201000005000 autoimmune gastritis Diseases 0.000 claims 3
- 201000000448 autoimmune hemolytic anemia Diseases 0.000 claims 3
- 206010008118 cerebral infarction Diseases 0.000 claims 3
- 230000006378 damage Effects 0.000 claims 3
- 208000025729 dengue disease Diseases 0.000 claims 3
- 235000005911 diet Nutrition 0.000 claims 3
- 230000000378 dietary effect Effects 0.000 claims 3
- 208000024908 graft versus host disease Diseases 0.000 claims 3
- 208000002672 hepatitis B Diseases 0.000 claims 3
- 208000021039 metastatic melanoma Diseases 0.000 claims 3
- 201000006417 multiple sclerosis Diseases 0.000 claims 3
- 206010028417 myasthenia gravis Diseases 0.000 claims 3
- 208000031225 myocardial ischemia Diseases 0.000 claims 3
- 230000001338 necrotic effect Effects 0.000 claims 3
- 230000000926 neurological effect Effects 0.000 claims 3
- 201000005113 shigellosis Diseases 0.000 claims 3
- 208000002320 spinal muscular atrophy Diseases 0.000 claims 3
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 3
- 206010043554 thrombocytopenia Diseases 0.000 claims 3
- 208000035408 type 1 diabetes mellitus 1 Diseases 0.000 claims 3
- 230000003612 virological effect Effects 0.000 claims 3
- 206010043781 Thyroiditis chronic Diseases 0.000 claims 2
- 239000002671 adjuvant Substances 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 239000003981 vehicle Substances 0.000 claims 2
- 206010043778 thyroiditis Diseases 0.000 claims 1
- 102000003810 Interleukin-18 Human genes 0.000 description 17
- 108090000171 Interleukin-18 Proteins 0.000 description 17
- 210000004027 cell Anatomy 0.000 description 16
- 102000004190 Enzymes Human genes 0.000 description 12
- 108090000790 Enzymes Proteins 0.000 description 12
- 229940088598 enzyme Drugs 0.000 description 12
- 230000000694 effects Effects 0.000 description 11
- 238000001727 in vivo Methods 0.000 description 8
- 125000001424 substituent group Chemical group 0.000 description 8
- 206010028980 Neoplasm Diseases 0.000 description 5
- 201000011510 cancer Diseases 0.000 description 5
- 125000002950 monocyclic group Chemical group 0.000 description 5
- 108090000623 proteins and genes Proteins 0.000 description 5
- 102100029855 Caspase-3 Human genes 0.000 description 4
- 241001465754 Metazoa Species 0.000 description 4
- ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 description 4
- 125000005842 heteroatom Chemical group 0.000 description 4
- 230000005764 inhibitory process Effects 0.000 description 4
- WFDIJRYMOXRFFG-UHFFFAOYSA-N Acetic anhydride Chemical compound CC(=O)OC(C)=O WFDIJRYMOXRFFG-UHFFFAOYSA-N 0.000 description 3
- 102100035904 Caspase-1 Human genes 0.000 description 3
- 108090000426 Caspase-1 Proteins 0.000 description 3
- 102000004127 Cytokines Human genes 0.000 description 3
- 108090000695 Cytokines Proteins 0.000 description 3
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 3
- 230000004913 activation Effects 0.000 description 3
- 235000001014 amino acid Nutrition 0.000 description 3
- 150000001413 amino acids Chemical class 0.000 description 3
- 239000003795 chemical substances by application Substances 0.000 description 3
- 238000000338 in vitro Methods 0.000 description 3
- 235000018102 proteins Nutrition 0.000 description 3
- 102000004169 proteins and genes Human genes 0.000 description 3
- 108090000397 Caspase 3 Proteins 0.000 description 2
- 102100025597 Caspase-4 Human genes 0.000 description 2
- 102100038902 Caspase-7 Human genes 0.000 description 2
- 101000828805 Cowpox virus (strain Brighton Red) Serine proteinase inhibitor 2 Proteins 0.000 description 2
- 241000531123 GB virus C Species 0.000 description 2
- 101000793880 Homo sapiens Caspase-3 Proteins 0.000 description 2
- 206010061218 Inflammation Diseases 0.000 description 2
- 241000124008 Mammalia Species 0.000 description 2
- FXHOOIRPVKKKFG-UHFFFAOYSA-N N,N-Dimethylacetamide Chemical compound CN(C)C(C)=O FXHOOIRPVKKKFG-UHFFFAOYSA-N 0.000 description 2
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 description 2
- 210000001744 T-lymphocyte Anatomy 0.000 description 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 2
- 230000001413 cellular effect Effects 0.000 description 2
- 238000006243 chemical reaction Methods 0.000 description 2
- 239000002299 complementary DNA Substances 0.000 description 2
- 229940125532 enzyme inhibitor Drugs 0.000 description 2
- 239000002532 enzyme inhibitor Substances 0.000 description 2
- 230000002349 favourable effect Effects 0.000 description 2
- 210000002865 immune cell Anatomy 0.000 description 2
- 230000002458 infectious effect Effects 0.000 description 2
- 230000004054 inflammatory process Effects 0.000 description 2
- 210000002540 macrophage Anatomy 0.000 description 2
- 229910052760 oxygen Inorganic materials 0.000 description 2
- 239000001301 oxygen Substances 0.000 description 2
- 230000007170 pathology Effects 0.000 description 2
- 125000001151 peptidyl group Chemical group 0.000 description 2
- 230000000144 pharmacologic effect Effects 0.000 description 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 2
- 239000002243 precursor Substances 0.000 description 2
- 108090000765 processed proteins & peptides Proteins 0.000 description 2
- 229940002612 prodrug Drugs 0.000 description 2
- 239000000651 prodrug Substances 0.000 description 2
- 230000000638 stimulation Effects 0.000 description 2
- 229910052717 sulfur Inorganic materials 0.000 description 2
- 239000011593 sulfur Substances 0.000 description 2
- 210000001519 tissue Anatomy 0.000 description 2
- 229930195735 unsaturated hydrocarbon Natural products 0.000 description 2
- ZIIUUSVHCHPIQD-UHFFFAOYSA-N 2,4,6-trimethyl-N-[3-(trifluoromethyl)phenyl]benzenesulfonamide Chemical compound CC1=CC(C)=CC(C)=C1S(=O)(=O)NC1=CC=CC(C(F)(F)F)=C1 ZIIUUSVHCHPIQD-UHFFFAOYSA-N 0.000 description 1
- 125000000094 2-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 description 1
- AUUIARVPJHGTSA-UHFFFAOYSA-N 3-(aminomethyl)chromen-2-one Chemical compound C1=CC=C2OC(=O)C(CN)=CC2=C1 AUUIARVPJHGTSA-UHFFFAOYSA-N 0.000 description 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 1
- 102000004018 Caspase 6 Human genes 0.000 description 1
- 108090000425 Caspase 6 Proteins 0.000 description 1
- 108090000567 Caspase 7 Proteins 0.000 description 1
- 229940123169 Caspase inhibitor Drugs 0.000 description 1
- 102000004068 Caspase-10 Human genes 0.000 description 1
- 108090000572 Caspase-10 Proteins 0.000 description 1
- 108090000570 Caspase-12 Proteins 0.000 description 1
- 102000004066 Caspase-12 Human genes 0.000 description 1
- 102000004046 Caspase-2 Human genes 0.000 description 1
- 108090000552 Caspase-2 Proteins 0.000 description 1
- 101710090338 Caspase-4 Proteins 0.000 description 1
- 102100038916 Caspase-5 Human genes 0.000 description 1
- 101710090333 Caspase-5 Proteins 0.000 description 1
- 102100026548 Caspase-8 Human genes 0.000 description 1
- 108090000538 Caspase-8 Proteins 0.000 description 1
- 102000004039 Caspase-9 Human genes 0.000 description 1
- 108090000566 Caspase-9 Proteins 0.000 description 1
- 102000029816 Collagenase Human genes 0.000 description 1
- 108060005980 Collagenase Proteins 0.000 description 1
- 206010014824 Endotoxic shock Diseases 0.000 description 1
- 102000010911 Enzyme Precursors Human genes 0.000 description 1
- 108010062466 Enzyme Precursors Proteins 0.000 description 1
- 241000711549 Hepacivirus C Species 0.000 description 1
- 241000700721 Hepatitis B virus Species 0.000 description 1
- 241000282412 Homo Species 0.000 description 1
- 101000715398 Homo sapiens Caspase-1 Proteins 0.000 description 1
- 101000933112 Homo sapiens Caspase-4 Proteins 0.000 description 1
- 101000741014 Homo sapiens Caspase-7 Proteins 0.000 description 1
- 101001033249 Homo sapiens Interleukin-1 beta Proteins 0.000 description 1
- 102000008070 Interferon-gamma Human genes 0.000 description 1
- 108010074328 Interferon-gamma Proteins 0.000 description 1
- 102100039065 Interleukin-1 beta Human genes 0.000 description 1
- 108090001005 Interleukin-6 Proteins 0.000 description 1
- 241001529936 Murinae Species 0.000 description 1
- 101100059157 Mus musculus Casp2 gene Proteins 0.000 description 1
- 101000933115 Mus musculus Caspase-4 Proteins 0.000 description 1
- 241000699670 Mus sp. Species 0.000 description 1
- 108091028043 Nucleic acid sequence Proteins 0.000 description 1
- 102000015439 Phospholipases Human genes 0.000 description 1
- 108010064785 Phospholipases Proteins 0.000 description 1
- 101000983552 Rattus norvegicus Caspase-1 Proteins 0.000 description 1
- 241000219061 Rheum Species 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 125000005073 adamantyl group Chemical group C12(CC3CC(CC(C1)C3)C2)* 0.000 description 1
- 239000000556 agonist Substances 0.000 description 1
- 150000001338 aliphatic hydrocarbons Chemical class 0.000 description 1
- 125000003342 alkenyl group Chemical group 0.000 description 1
- 125000000304 alkynyl group Chemical group 0.000 description 1
- 239000003242 anti bacterial agent Substances 0.000 description 1
- 229940121363 anti-inflammatory agent Drugs 0.000 description 1
- 239000002260 anti-inflammatory agent Substances 0.000 description 1
- 229940088710 antibiotic agent Drugs 0.000 description 1
- 206010003246 arthritis Diseases 0.000 description 1
- 150000005840 aryl radicals Chemical class 0.000 description 1
- 230000001363 autoimmune Effects 0.000 description 1
- 210000003651 basophil Anatomy 0.000 description 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 1
- 230000003851 biochemical process Effects 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000000988 bone and bone Anatomy 0.000 description 1
- 210000004900 c-terminal fragment Anatomy 0.000 description 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 description 1
- 101150055276 ced-3 gene Proteins 0.000 description 1
- 230000003915 cell function Effects 0.000 description 1
- 210000000170 cell membrane Anatomy 0.000 description 1
- 210000001612 chondrocyte Anatomy 0.000 description 1
- 229960002424 collagenase Drugs 0.000 description 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 1
- 230000007423 decrease Effects 0.000 description 1
- 230000007547 defect Effects 0.000 description 1
- 230000002950 deficient Effects 0.000 description 1
- 230000002939 deleterious effect Effects 0.000 description 1
- 230000001627 detrimental effect Effects 0.000 description 1
- 230000018109 developmental process Effects 0.000 description 1
- 230000004069 differentiation Effects 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000002158 endotoxin Substances 0.000 description 1
- 210000003979 eosinophil Anatomy 0.000 description 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- 210000002950 fibroblast Anatomy 0.000 description 1
- 230000012010 growth Effects 0.000 description 1
- 239000000833 heterodimer Substances 0.000 description 1
- 125000001183 hydrocarbyl group Chemical group 0.000 description 1
- 230000002519 immonomodulatory effect Effects 0.000 description 1
- 230000036039 immunity Effects 0.000 description 1
- 239000002955 immunomodulating agent Substances 0.000 description 1
- 229940121354 immunomodulator Drugs 0.000 description 1
- 230000004957 immunoregulator effect Effects 0.000 description 1
- 238000000099 in vitro assay Methods 0.000 description 1
- 239000000411 inducer Substances 0.000 description 1
- 230000001939 inductive effect Effects 0.000 description 1
- 230000028709 inflammatory response Effects 0.000 description 1
- 230000003993 interaction Effects 0.000 description 1
- 229960003130 interferon gamma Drugs 0.000 description 1
- 210000001865 kupffer cell Anatomy 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- 230000002503 metabolic effect Effects 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- 210000001616 monocyte Anatomy 0.000 description 1
- 238000010172 mouse model Methods 0.000 description 1
- BXGTVNLGPMZLAZ-UHFFFAOYSA-N n'-ethylmethanediimine;hydrochloride Chemical compound Cl.CCN=C=N BXGTVNLGPMZLAZ-UHFFFAOYSA-N 0.000 description 1
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- WOOWBQQQJXZGIE-UHFFFAOYSA-N n-ethyl-n-propan-2-ylpropan-2-amine Chemical compound CCN(C(C)C)C(C)C.CCN(C(C)C)C(C)C WOOWBQQQJXZGIE-UHFFFAOYSA-N 0.000 description 1
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 125000001624 naphthyl group Chemical group 0.000 description 1
- 210000000440 neutrophil Anatomy 0.000 description 1
- 125000002868 norbornyl group Chemical group C12(CCC(CC1)C2)* 0.000 description 1
- 150000007523 nucleic acids Chemical group 0.000 description 1
- 229940094443 oxytocics prostaglandins Drugs 0.000 description 1
- 230000037361 pathway Effects 0.000 description 1
- 230000035515 penetration Effects 0.000 description 1
- 210000005259 peripheral blood Anatomy 0.000 description 1
- 239000011886 peripheral blood Substances 0.000 description 1
- 125000003367 polycyclic group Chemical group 0.000 description 1
- 229920001184 polypeptide Polymers 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 1
- 102000004196 processed proteins & peptides Human genes 0.000 description 1
- 230000000770 proinflammatory effect Effects 0.000 description 1
- 230000035755 proliferation Effects 0.000 description 1
- 230000000069 prophylactic effect Effects 0.000 description 1
- 238000011321 prophylaxis Methods 0.000 description 1
- 150000003180 prostaglandins Chemical class 0.000 description 1
- 108020003175 receptors Proteins 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 230000000717 retained effect Effects 0.000 description 1
- 229920006395 saturated elastomer Polymers 0.000 description 1
- 230000028327 secretion Effects 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
- 230000004936 stimulating effect Effects 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 210000001179 synovial fluid Anatomy 0.000 description 1
- 210000002437 synoviocyte Anatomy 0.000 description 1
- 125000001712 tetrahydronaphthyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 238000011830 transgenic mouse model Methods 0.000 description 1
- 230000032258 transport Effects 0.000 description 1
- 238000011282 treatment Methods 0.000 description 1
- 230000005748 tumor development Effects 0.000 description 1
- 108010087967 type I signal peptidase Proteins 0.000 description 1
- 239000002023 wood Substances 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
- C07K5/0202—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
-
- 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
-
- 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- 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
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/16—Central respiratory analeptics
-
- 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
- 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
- A61P17/02—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
- 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
- A61P19/00—Drugs for skeletal disorders
-
- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/08—Antiepileptics; Anticonvulsants
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/32—Alcohol-abuse
-
- 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
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
-
- 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
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- 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
- A61P31/20—Antivirals for DNA viruses
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
-
- 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
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic 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
- A61P5/00—Drugs for disorders of the endocrine system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
- A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
-
- 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
-
- 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
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Physical Education & Sports Medicine (AREA)
- Neurology (AREA)
- Immunology (AREA)
- Oncology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Virology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Molecular Biology (AREA)
- Communicable Diseases (AREA)
- Hematology (AREA)
- Pulmonology (AREA)
- Endocrinology (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Pain & Pain Management (AREA)
- Biochemistry (AREA)
- Cardiology (AREA)
- Addiction (AREA)
- Crystallography & Structural Chemistry (AREA)
- Psychiatry (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US7877098P | 1998-03-19 | 1998-03-19 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA200004652B true ZA200004652B (en) | 2002-04-24 |
Family
ID=22146109
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA200004652A ZA200004652B (en) | 1998-03-19 | 2000-09-05 | Inhibitors of caspases. |
Country Status (34)
| Country | Link |
|---|---|
| US (3) | US6531474B1 (uk) |
| EP (6) | EP2261233A3 (uk) |
| JP (3) | JP4594520B2 (uk) |
| KR (2) | KR100898094B1 (uk) |
| CN (1) | CN1321129C (uk) |
| AP (1) | AP2000001919A0 (uk) |
| AR (1) | AR019011A1 (uk) |
| AT (1) | ATE410439T1 (uk) |
| AU (1) | AU769033B2 (uk) |
| BG (1) | BG104863A (uk) |
| BR (2) | BR9909660A (uk) |
| CA (1) | CA2324226C (uk) |
| CZ (1) | CZ302281B6 (uk) |
| DE (1) | DE69939689D1 (uk) |
| DK (1) | DK1064298T3 (uk) |
| ES (1) | ES2315010T3 (uk) |
| GE (1) | GEP20043163B (uk) |
| HK (1) | HK1035733A1 (uk) |
| HU (1) | HU227920B1 (uk) |
| ID (1) | ID27002A (uk) |
| IL (3) | IL138469A0 (uk) |
| IS (1) | IS5622A (uk) |
| NO (1) | NO331829B1 (uk) |
| NZ (2) | NZ506963A (uk) |
| PL (1) | PL204619B1 (uk) |
| PT (1) | PT1064298E (uk) |
| RU (1) | RU2274642C2 (uk) |
| SI (1) | SI1064298T1 (uk) |
| SK (1) | SK286736B6 (uk) |
| TR (1) | TR200103406T2 (uk) |
| TW (1) | TWI243828B (uk) |
| UA (2) | UA74133C2 (uk) |
| WO (1) | WO1999047545A2 (uk) |
| ZA (1) | ZA200004652B (uk) |
Families Citing this family (77)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR9909660A (pt) * | 1998-03-19 | 2000-11-21 | Vertex Pharma | Inibidores de caspases |
| US7157430B2 (en) | 1998-10-22 | 2007-01-02 | Idun Pharmaceuticals, Inc. | (Substituted)acyl dipeptidyl inhibitors of the ICE/CED-3 family of cysteine proteases |
| US6242422B1 (en) | 1998-10-22 | 2001-06-05 | Idun Pharmacueticals, Inc. | (Substituted)Acyl dipeptidyl inhibitors of the ice/ced-3 family of cysteine proteases |
| US6720415B2 (en) | 1998-12-02 | 2004-04-13 | Princeton University | Compositions and methods for regulating bacterial pathogenesis |
| US7326542B2 (en) | 1998-12-02 | 2008-02-05 | Princeton University | Compositions and methods for regulating bacterial pathogenesis |
| WO2001027085A1 (en) * | 1999-10-13 | 2001-04-19 | Merck Frosst Canada & Co. | Nicotinyl aspartyl ketones as inhibitors of caspase-3 |
| US6395767B2 (en) * | 2000-03-10 | 2002-05-28 | Bristol-Myers Squibb Company | Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method |
| US6525024B1 (en) | 2000-04-17 | 2003-02-25 | Idun Pharmaceuticals, Inc. | Inhibitors of the ICE/ced-3 family of cysteine proteases |
| JP2003532698A (ja) | 2000-05-10 | 2003-11-05 | プリンストン ユニバーシティ | 細菌の増殖および病理発生を調節するための化合物ならびに方法 |
| PE20011350A1 (es) | 2000-05-19 | 2002-01-15 | Vertex Pharma | PROFARMACO DE UN INHIBIDOR DE ENZIMA CONVERTIDORA DE INTERLEUCINA-1ß (ICE) |
| PE20020500A1 (es) * | 2000-09-13 | 2002-06-25 | Vertex Pharma | Derivados de piperidina, tetrahidroquinolina, tetrahidroisoquinolina como inhibidores de caspasas |
| AU2002245649A1 (en) * | 2001-03-02 | 2002-09-19 | Idun Pharmaceuticals, Inc. | Methods, compositions and kits for preserving antigenicity |
| YU103003A (sh) | 2001-06-26 | 2006-05-25 | Abgenix Inc. | Antitela za opgl |
| WO2003068242A1 (en) * | 2002-02-11 | 2003-08-21 | Vertex Pharmaceuticals Incorporated | Phospholipids as caspase inhibitor prodrugs |
| WO2003075853A2 (en) | 2002-03-08 | 2003-09-18 | Bristol-Myers Squibb Company | Cyclic derivatives as modulators of chemokine receptor activity |
| FR2839309B1 (fr) | 2002-05-03 | 2004-07-23 | Aventis Pharma Sa | Nouveaux derives de l'acide hexahydro-pyridazine-3- carboxylique, chimiotheques les contenant, leur utilisation comme medicaments, compositions pharmaceutiques les contenant et leurs procedes de preparation |
| US7001899B2 (en) | 2002-06-10 | 2006-02-21 | The Procter & Gamble Company | Interleukin converting enzyme inhibitors |
| AU2003263393A1 (en) * | 2002-09-04 | 2004-03-29 | Glenmark Pharmaceuticals Limited | New heterocyclic amide compounds useful for the treatment of inflammatory and allergic disorders: process for their preparation and pharmaceutical compositions containing them |
| NZ538569A (en) | 2002-09-06 | 2009-02-28 | Amgen Inc | Therapeutic human anti-IL-1R1 monoclonal antibody |
| JP2006506379A (ja) | 2002-10-23 | 2006-02-23 | グレンマーク・ファーマシューティカルズ・リミテッド | 炎症性およびアレルギー性疾患の治療に有用な新規三環式化合物：その調製方法およびそれらを含む医薬組成物 |
| FR2846969A1 (fr) * | 2002-11-08 | 2004-05-14 | Salles Jean Pierre | Nouveaux vecteurs moleculaires amphiphiles fluorocarbones a usage biomedical et medical |
| FR2847160A1 (fr) * | 2002-11-20 | 2004-05-21 | Oreal | Composition capillaire contenant un compose pyrasol-carboxamide, son utilisation pour stimuler la pousse des cheveux et/ou freiner leur chute |
| JP2006519755A (ja) * | 2002-11-20 | 2006-08-31 | ロレアル | ピラゾール−カルボキシアミドを含有する毛髪の手入れ用又は睫毛用の組成物、毛髪及び睫毛の成長を刺激し、及び／又は抜毛を防止するためのそれらの使用 |
| BRPI0409747A (pt) | 2003-04-11 | 2006-05-09 | Glenmark Pharmaceuticals Sa | novos compostos heterocìclicos úteis para tratamento de distúrbios inflamatórios e alérgicos, processo para sua preparação e composições farmacêuticas contendo estes |
| AU2003902704A0 (en) * | 2003-05-29 | 2003-06-19 | Crc For Waste Management And Pollution Control Limited Of Unsw | Process for producing a nanoscale zero-valent metal |
| JP2007513092A (ja) * | 2003-12-01 | 2007-05-24 | バーテックス ファーマシューティカルズ インコーポレイテッド | Ｉｃｅ阻害剤を使用する感染性疾患の処置 |
| DK1541124T3 (da) * | 2003-12-12 | 2009-05-18 | Straetmans Chemische Produkte | Sammensætninger med anissyre og glycerider |
| CA2820541A1 (en) * | 2004-02-27 | 2005-09-15 | Vertex Pharmaceuticals Incorporated | Caspase inhibitors and uses thereof |
| AU2011226946B2 (en) * | 2004-02-27 | 2012-05-03 | Vertex Pharmaceuticals Incoporated | Caspase Inhibitors and Uses Thereof |
| JP2007525503A (ja) * | 2004-02-27 | 2007-09-06 | バーテックス ファーマシューティカルズ インコーポレイテッド | カスパーゼインヒビターおよびそれらの使用 |
| WO2005090334A2 (en) | 2004-03-12 | 2005-09-29 | Vertex Pharmaceuticals Incorporated | Processes and intermediates for the preparation of aspartic acetal caspase inhibitors |
| MXPA06013252A (es) * | 2004-05-14 | 2007-02-28 | Emisphere Tech Inc | Compuestos y composiciones para suministrar agentes activos. |
| AU2012200214B2 (en) * | 2004-05-14 | 2013-10-24 | Emisphere Technologies, Inc. | Compounds and compositions for delivering active agents |
| EP1750689A1 (en) * | 2004-05-15 | 2007-02-14 | Vertex Pharmaceuticals Incorporated | Treating seizures using ice inhibitors |
| GB0411056D0 (en) | 2004-05-18 | 2004-06-23 | Novartis Ag | Organic compounds |
| US7531570B2 (en) * | 2004-05-27 | 2009-05-12 | Vertex Pharmaceuticals Incorporated | Treatment of diseases using ICE inhibitors |
| EA200700225A1 (ru) * | 2004-07-12 | 2008-02-28 | Айдан Фармасьютикалз, Инк. | Аналоги тетрапептида |
| AU2005283719A1 (en) * | 2004-09-17 | 2006-03-23 | Biomas Ltd. | Compositions and methods for inducing hair growth |
| CA2583497A1 (en) | 2004-10-13 | 2006-04-20 | Glenmark Pharmaceuticals S.A. | Process for the preparation of n-(3,5-dichloropyrid-4-yl)-4difluoromethoxy-8-methanesulfonamido-dibenzo[b,d]furan-1-carboxamide |
| KR101317119B1 (ko) | 2004-12-17 | 2013-10-11 | 그렌마크 파머수티칼스 에스. 아. | 염증성 및 알레르기성 장애의 치료에 유용한 신규한헤테로사이클릭 화합물 |
| SI1831227T1 (sl) | 2004-12-17 | 2013-09-30 | Glenmark Pharmaceuticals S.A. | Nove heterociklične spojine uporabne za zdravljenje vnetnih in alergijskih motenj |
| JP4673068B2 (ja) * | 2005-01-19 | 2011-04-20 | 独立行政法人科学技術振興機構 | Ｔｈ１型アレルギー疾患治療用組成物 |
| DE102005017116A1 (de) * | 2005-04-13 | 2006-10-26 | Novartis Ag | Hemmstoffe für Inhibitoren von Apoptose Proteinen (IAP) |
| CN101268084A (zh) | 2005-07-28 | 2008-09-17 | 沃泰克斯药物股份有限公司 | 天冬氨酸特异性半胱氨酸蛋白酶抑制剂前体药物 |
| PE20070684A1 (es) | 2005-11-14 | 2007-08-06 | Amgen Inc | MOLECULAS QUIMERICAS DE ANTICUERPO RANKL-PTH/PTHrP |
| CA2656487A1 (en) * | 2006-07-07 | 2008-01-17 | The Board Of Trustees Of The Leland Stanford Junior University | Selective caspase inhibitors |
| WO2008060621A2 (en) * | 2006-11-17 | 2008-05-22 | Abbott Laboratories | Aminopyrrolidines as chemokine receptor antagonists |
| US8084862B2 (en) * | 2007-09-20 | 2011-12-27 | International Business Machines Corporation | Interconnect structures with patternable low-k dielectrics and method of fabricating same |
| US7709370B2 (en) | 2007-09-20 | 2010-05-04 | International Business Machines Corporation | Spin-on antireflective coating for integration of patternable dielectric materials and interconnect structures |
| US8618663B2 (en) | 2007-09-20 | 2013-12-31 | International Business Machines Corporation | Patternable dielectric film structure with improved lithography and method of fabricating same |
| WO2009124265A1 (en) * | 2008-04-03 | 2009-10-08 | The Board Of Trustees Of The Leland Stanford Junior University | Probes for in vivo targeting of active cysteine proteases |
| US20110144765A1 (en) * | 2008-05-27 | 2011-06-16 | Imperial Innovations Limited | Process For Producing Porous Scaffolds From Sinterable Glass |
| US20110152343A1 (en) * | 2009-12-22 | 2011-06-23 | Functional Genetics, Inc. | Protease inhibitors and broad-spectrum antiviral |
| GB201001070D0 (en) | 2010-01-22 | 2010-03-10 | St George's Hospital Medical School | Theraputic compounds and their use |
| US9365612B2 (en) | 2010-01-29 | 2016-06-14 | United States Of America As Represented By The Secretary, Department Of Health And Human Services | Caspase inhibitors |
| GB201011411D0 (en) | 2010-07-06 | 2010-08-18 | St Georges Hosp Medical School | Therapeutic compounds and their use |
| WO2012061785A2 (en) | 2010-11-05 | 2012-05-10 | Brandeis University | Ice inhibiting compounds and uses thereof |
| US9956260B1 (en) | 2011-07-22 | 2018-05-01 | The J. David Gladstone Institutes | Treatment of HIV-1 infection and AIDS |
| CA2851810C (en) | 2011-10-14 | 2020-01-07 | Bristol-Myers Squibb Company | Substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| ES2579832T3 (es) | 2011-10-14 | 2016-08-17 | Bristol-Myers Squibb Company | Compuestos de tetrahidroisoquinolina sustituida como inhibidores del factor XIa |
| ES2699226T3 (es) | 2011-10-14 | 2019-02-08 | Bristol Myers Squibb Co | Compuestos de tetrahidroisoquinolina sustituidos como inhibidores del factor XIa |
| KR20150046259A (ko) * | 2012-08-23 | 2015-04-29 | 앨리오스 바이오파마 인크. | 파라믹소바이러스 바이러스성 감염의 치료용 화합물 |
| US9403774B2 (en) | 2012-10-12 | 2016-08-02 | Bristol-Myers Squibb Company | Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| EP2906552B1 (en) | 2012-10-12 | 2017-11-22 | Bristol-Myers Squibb Company | Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| BR112015007937A2 (pt) | 2012-10-12 | 2017-07-04 | Bristol Myers Squibb Co | formas cristalinas de um inibidor de fator xia |
| WO2014160668A1 (en) | 2013-03-25 | 2014-10-02 | Bristol-Myers Squibb Company | Tetrahydroisoquinolines containing substituted azoles as factor xia inhibitors |
| RS57659B1 (sr) | 2014-01-31 | 2018-11-30 | Bristol Myers Squibb Co | Makrociklusi sa heterocikličnim p2' grupama kao inhibitori faktora xia |
| NO2760821T3 (uk) | 2014-01-31 | 2018-03-10 | ||
| EP4299134A3 (en) | 2014-06-13 | 2024-03-27 | Bach Biosciences, LLC | Fap-activated therapeutic agents, and uses related thereto |
| US9737556B2 (en) | 2014-06-13 | 2017-08-22 | Trustees Of Tufts College | FAP-activated therapeutic agents, and uses related thereto |
| US10081623B2 (en) | 2014-09-04 | 2018-09-25 | Bristol-Myers Squibb Company | Diamide macrocycles that are FXIa inhibitors |
| US9453018B2 (en) | 2014-10-01 | 2016-09-27 | Bristol-Myers Squibb Company | Pyrimidinones as factor XIa inhibitors |
| EP3349754A4 (en) | 2015-09-17 | 2019-03-20 | City of Hope | PCNA INHIBITORS |
| CN109476639B (zh) * | 2016-07-22 | 2021-02-26 | 橘生药品工业股份有限公司 | 吡咯烷衍生物 |
| DK3558335T3 (da) | 2016-12-23 | 2023-07-24 | Casp Aid Inc | Caspase-1 inhibition and uses thereof for prevention and treatment of neurological conditions |
| US20210236599A1 (en) | 2018-08-13 | 2021-08-05 | Iltoo Pharma | Combination of interleukin-2 with an interleukin 1 inhibitor, conjugates and therapeutic uses thereof |
| EP4251140A1 (en) * | 2020-11-25 | 2023-10-04 | Lysosomal and Rare Disorders Research and Treatment Center, Inc. | Inhibition of caspase pathway as a treatment for lysosomal storage disorders |
Family Cites Families (80)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2973111A (en) * | 1958-02-11 | 1961-02-28 | Dempster Brothers Inc | Compaction bodies |
| US5874424A (en) | 1995-12-20 | 1999-02-23 | Vertex Pharmaceuticals Incorporated | Inhibitors of interleukin-1β converting enzyme |
| US6204261B1 (en) | 1995-12-20 | 2001-03-20 | Vertex Pharmaceuticals Incorporated | Inhibitors of interleukin-1β Converting enzyme inhibitors |
| US4465679A (en) | 1983-01-31 | 1984-08-14 | Usv Pharmaceutical Corporation | 1,2-Diaza-3-one compounds, their use in treating hypertension and pharmaceutical compositions thereof |
| IL72523A (en) | 1983-08-12 | 1988-06-30 | Takeda Chemical Industries Ltd | 3-amino-4-oxo-2,3,4,5-tetrahydro-1,5-benzoxazepine derivatives,their production and pharmaceutical compositions containing them |
| US5055451A (en) | 1986-12-22 | 1991-10-08 | Syntex Inc. | Aryloxy and arylacyloxy methyl ketones as thiol protease inhibitors |
| US5158936A (en) | 1986-12-22 | 1992-10-27 | Syntex (U.S.A.) Inc. | Aryloxy and arylacyloxy methyl ketones as thiol protease inhibitors |
| US5008245A (en) | 1988-10-27 | 1991-04-16 | University Of Kentucky Research Foundation | Novel peptidyl carbamate inhibitors of the enzyme elastase |
| CA2021660A1 (en) | 1989-07-26 | 1991-01-27 | Philippe Bey | Peptidase inhibitors |
| NZ235155A (en) | 1989-09-11 | 1993-04-28 | Merrell Dow Pharma | Peptidase substrates in which the carboxy terminal group has been replaced by a tricarbonyl radical |
| US5416013A (en) | 1990-04-04 | 1995-05-16 | Sterling Winthrop Inc. | Interleukin 1β protease and interleukin 1β protease inhibitors |
| WO1991015577A1 (en) | 1990-04-04 | 1991-10-17 | Black, Roy, A. | INTERLEUKIN 1'beta' PROTEASE |
| EP0503561B1 (de) | 1991-03-15 | 1998-10-28 | Hoechst Aktiengesellschaft | Verfahren zur diastereoselektiven reduktiven Pinakol-Kupplung von homochiralen alpha-Aminoaldehyden |
| DE69226820T2 (de) * | 1991-06-21 | 1999-05-12 | Merck & Co., Inc., Rahway, N.J. | Peptidylderivate als Inhibitoren von Interleukin-1B-konvertierenden Enzymen |
| JP3190431B2 (ja) | 1991-07-01 | 2001-07-23 | 三菱化学株式会社 | ケトン誘導体 |
| US5278061A (en) | 1991-08-16 | 1994-01-11 | Merck & Co., Inc. | Affinity chromatography matrix useful in purifying interleukin-1β converting enzyme |
| EP0533226A3 (en) | 1991-08-16 | 1993-08-18 | Merck & Co. Inc. | Novel chromophore containing compounds |
| US6348570B1 (en) | 1991-08-16 | 2002-02-19 | Merck & Co., Inc. | Chromophore containing compounds and their use in determining interleukin-1β convertase activity |
| DE69229252T2 (de) | 1991-08-16 | 1999-12-16 | Merck & Co., Inc. | DNS, welche das Interleukin-1B-Vorläufer-Converting-Enzym kodiert |
| ATE257517T1 (de) | 1991-08-30 | 2004-01-15 | Vertex Pharma | Interleukin 1-beta protease und ihre inhibitoren |
| DE59206778D1 (de) | 1991-10-07 | 1996-08-22 | Hoechst Ag | Verfahren zur diastereoselektiven reduktiven Pinakol-Kupplung von homochiralen alpha-Aminoaldehyden |
| GB9123326D0 (en) | 1991-11-04 | 1991-12-18 | Sandoz Ltd | Improvements in or relating to organic compounds |
| WO1993012076A1 (en) | 1991-12-13 | 1993-06-24 | Corvas International Inc. | Reagents for automated synthesis of peptide analogs |
| EP0547699A1 (en) | 1991-12-19 | 1993-06-23 | Merck & Co. Inc. | Peptidyl derivatives as inhibitors of interleukin-1B converting enzyme |
| AU3479593A (en) | 1992-01-31 | 1993-09-01 | Merck & Co., Inc. | Peptidyl derivatives as inhibitors of interleukin-1beta converting enzyme |
| EP0627926B1 (en) | 1992-02-21 | 1998-08-05 | Merck & Co., Inc. (a New Jersey corp.) | PEPTIDYL DERIVATIVES AS INHIBITORS OF INTERLEUKIN-1$g(b) CONVERTING ENZYME |
| AU4634993A (en) | 1992-06-24 | 1994-01-24 | Merck & Co., Inc. | Dna encoding precursor interleukin 1beta converting enzyme |
| US5739279A (en) | 1992-07-31 | 1998-04-14 | Pfizer Inc. | Peptidyl 4-amino-2,2-difluoro-3-oxo-1,6-hexanedioic acid derivatives as antiinflammatory agents |
| CA2109646C (en) | 1992-11-24 | 2000-03-07 | Gaston O. Daumy | Para-nitroanilide peptides |
| EP0618223A3 (en) | 1993-03-08 | 1996-06-12 | Sandoz Ltd | Peptides, the release of Interleukin 1-Bêta, useful as anti-inflammatory agents. |
| TW494094B (en) | 1993-04-29 | 2002-07-11 | Vertex Pharma | Peptide analogs as irreversible interleukin-1β protease inhibitors and pharmaceutical compositions comprising the same |
| US5462939A (en) | 1993-05-07 | 1995-10-31 | Sterling Winthrop Inc. | Peptidic ketones as interleukin-1β-converting enzyme inhibitors |
| US5411985A (en) | 1993-05-17 | 1995-05-02 | Merck & Co., Inc. | Gamma-pyrone-3-acetic acid as an inhibitor or interleukin-1 β inventory enzyme |
| JPH0789951A (ja) | 1993-06-03 | 1995-04-04 | Sterling Winthrop Inc | インターロイキン−１β転換酵素阻害剤 |
| ATE170868T1 (de) | 1993-06-04 | 1998-09-15 | Vertex Pharma | Peptid-phosphinyloxymethyl-ketonen als inhibitoren von interleukin-1 beta- konvertierenden enzymen |
| CA2165777A1 (en) | 1993-06-24 | 1995-01-05 | Junying Yuan | Programmed cell death genes and proteins |
| AU7714594A (en) | 1993-08-13 | 1995-03-14 | Merck & Co., Inc. | Substituted ketone derivatives as inhibitors of interleukin-1beta converting enzyme |
| ATE163639T1 (de) * | 1993-11-11 | 1998-03-15 | Basf Ag | P-hydroxyanilinderivate, verfahren zu ihrer herstellung und ihre verwendung zur bekämpfung von schadpilzen oder schädlingen |
| US5486623A (en) | 1993-12-08 | 1996-01-23 | Prototek, Inc. | Cysteine protease inhibitors containing heterocyclic leaving groups |
| US5714484A (en) | 1993-12-08 | 1998-02-03 | Prototek, Inc. | α-(1,3-dicarbonylenol ether) methyl ketones as cysteine protease inhibitors |
| CN1504462A (zh) | 1994-03-31 | 2004-06-16 | ������˹ҩƷ��˾ | 作为白细胞介素抑制剂的嘧啶基衍生物 |
| CA2189036A1 (en) | 1994-04-29 | 1995-11-09 | Roland E. Dolle | Halomethyl amides as il-1.beta. protease inhibitors |
| US5492824A (en) | 1994-05-12 | 1996-02-20 | Basf Ag | Ice and ice-like compositions and methods of making same |
| US5552400A (en) | 1994-06-08 | 1996-09-03 | Sterling Winthrop Inc. | Fused-bicyclic lactams as interleukin-1β converting enzyme inhibitors |
| US5716929A (en) | 1994-06-17 | 1998-02-10 | Vertex Pharmaceuticals, Inc. | Inhibitors of interleukin-1β converting enzyme |
| US5856116A (en) | 1994-06-17 | 1999-01-05 | Vertex Pharmaceuticals, Incorporated | Crystal structure and mutants of interleukin-1 beta converting enzyme |
| US5756466A (en) | 1994-06-17 | 1998-05-26 | Vertex Pharmaceuticals, Inc. | Inhibitors of interleukin-1β converting enzyme |
| US5847135A (en) | 1994-06-17 | 1998-12-08 | Vertex Pharmaceuticals, Incorporated | Inhibitors of interleukin-1β converting enzyme |
| US5565430A (en) | 1994-08-02 | 1996-10-15 | Sterling Winthrop Inc. | Azaaspartic acid analogs as interleukin-1β converting enzyme inhibitors |
| GB2292149A (en) * | 1994-08-09 | 1996-02-14 | Ferring Res Ltd | Peptide inhibitors of pro-interleukin-1beta converting enzyme |
| US5498616A (en) | 1994-11-04 | 1996-03-12 | Cephalon, Inc. | Cysteine protease and serine protease inhibitors |
| TW394764B (en) | 1995-02-14 | 2000-06-21 | Mitsubishi Chemcal Corp | Oxygen-containing heterocyclic derivatives |
| WO1996030395A2 (en) | 1995-03-31 | 1996-10-03 | Takeda Chemical Industries, Ltd. | Cysteine protease inhibitor |
| JPH09165360A (ja) * | 1995-03-31 | 1997-06-24 | Takeda Chem Ind Ltd | システインプロテアーゼ阻害剤 |
| US5798442A (en) | 1995-04-21 | 1998-08-25 | Merck Frosst Canada, Inc. | Peptidyl derivatives as inhibitors of pro-apoptotic cysteine proteinases |
| WO1997007805A1 (en) | 1995-08-31 | 1997-03-06 | Smithkline Beecham Corporation | Interleukin converting enzyme and apoptosis |
| WO1997008174A1 (en) | 1995-08-31 | 1997-03-06 | Smithkline Beecham Corporation | Interleukin converting enzyme and apoptosis |
| EP0761680A3 (en) | 1995-09-12 | 1999-05-06 | Ono Pharmaceutical Co., Ltd. | Tetrazole compounds having Interleukin-1beta converting enzyme inhibitory activity |
| US5744451A (en) | 1995-09-12 | 1998-04-28 | Warner-Lambert Company | N-substituted glutamic acid derivatives with interleukin-1 β converting enzyme inhibitory activity |
| EP0900791A1 (en) | 1995-12-27 | 1999-03-10 | Ono Pharmaceutical Co., Ltd. | Tetrazole derivatives and drugs containing the same as the active ingredient |
| AU3359697A (en) | 1996-07-08 | 1998-02-02 | Yamanouchi Pharmaceutical Co., Ltd. | Bone resorption inhibitors |
| WO1998004539A1 (fr) | 1996-07-29 | 1998-02-05 | Mitsubishi Chemical Corporation | Derives heterocycliques oxygenes |
| CN1234038A (zh) * | 1996-09-12 | 1999-11-03 | 伊邓药品公司 | 作为ICE/ced－3类半胱氨酸蛋白酶抑制剂的C－末端修饰的(N－取代)－2－吲哚基二肽 |
| EP0929311B8 (en) | 1996-09-12 | 2006-02-01 | Idun Pharmaceuticals, Inc. | INHIBITION OF APOPTOSIS USING INTERLEUKIN-1 beta-CONVERTING ENZYME (ICE)/CED-3 FAMILY INHIBITORS |
| EP0874850B1 (en) | 1996-09-12 | 2002-04-10 | Idun Pharmaceuticals, Inc. | Novel tricyclic compounds for the inhibition of the ice/ced-3 protease family of enzymes |
| US5869519A (en) | 1996-12-16 | 1999-02-09 | Idun Pharmaceuticals, Inc. | C-terminal modified (n-substituted)-2-indolyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases |
| US5968927A (en) | 1996-09-20 | 1999-10-19 | Idun Pharmaceuticals, Inc. | Tricyclic compounds for the inhibition of the ICE/ced-3 protease family of enzymes |
| US5877197A (en) | 1996-12-16 | 1999-03-02 | Karanewsky; Donald S. | C-terminal modified (N-substituted)-2-indolyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases |
| US6184244B1 (en) | 1996-12-16 | 2001-02-06 | Idun Pharmaceuticals, Inc. | C-terminal modified (N-substituted)-2-indolyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases |
| US6054487A (en) | 1997-03-18 | 2000-04-25 | Basf Aktiengesellschaft | Methods and compositions for modulating responsiveness to corticosteroids |
| HUP9700816A3 (en) | 1997-04-28 | 1999-06-28 | Gyogyszerkutato Intezet | 3(r)-3-amino-4-carboxy-butiraldehyde derivatives inhibiting release of interleukin-1-beta |
| US6184210B1 (en) | 1997-10-10 | 2001-02-06 | Cytovia, Inc. | Dipeptide apoptosis inhibitors and the use thereof |
| ES2229545T3 (es) * | 1997-10-31 | 2005-04-16 | Kimberly-Clark Worldwide, Inc. | Materiales no tejidos, rizados y recubrimiento. |
| BR9909660A (pt) * | 1998-03-19 | 2000-11-21 | Vertex Pharma | Inibidores de caspases |
| US6197750B1 (en) | 1998-07-02 | 2001-03-06 | Idun Pharmaceuticals, Inc. | C-terminal modified oxamyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases |
| US6242422B1 (en) | 1998-10-22 | 2001-06-05 | Idun Pharmacueticals, Inc. | (Substituted)Acyl dipeptidyl inhibitors of the ice/ced-3 family of cysteine proteases |
| PE20011350A1 (es) | 2000-05-19 | 2002-01-15 | Vertex Pharma | PROFARMACO DE UN INHIBIDOR DE ENZIMA CONVERTIDORA DE INTERLEUCINA-1ß (ICE) |
| AU2004290413A1 (en) | 2003-11-10 | 2005-05-26 | Vertex Pharmaceuticals Incorporated | Methods for monitoring IL-18 |
| JP2007525503A (ja) | 2004-02-27 | 2007-09-06 | バーテックス ファーマシューティカルズ インコーポレイテッド | カスパーゼインヒビターおよびそれらの使用 |
| US7531570B2 (en) | 2004-05-27 | 2009-05-12 | Vertex Pharmaceuticals Incorporated | Treatment of diseases using ICE inhibitors |
-
1999
- 1999-03-19 BR BR9909660-9A patent/BR9909660A/pt not_active IP Right Cessation
- 1999-03-19 PT PT99912662T patent/PT1064298E/pt unknown
- 1999-03-19 AR ARP990101240A patent/AR019011A1/es active IP Right Grant
- 1999-03-19 IL IL138469??A patent/IL138469A0/xx unknown
- 1999-03-19 DE DE69939689T patent/DE69939689D1/de not_active Expired - Lifetime
- 1999-03-19 TW TW088104386A patent/TWI243828B/zh not_active IP Right Cessation
- 1999-03-19 AP APAP/P/2000/001919A patent/AP2000001919A0/en unknown
- 1999-03-19 NZ NZ506963A patent/NZ506963A/en not_active IP Right Cessation
- 1999-03-19 KR KR1020007010376A patent/KR100898094B1/ko not_active IP Right Cessation
- 1999-03-19 EP EP10012064A patent/EP2261233A3/en not_active Withdrawn
- 1999-03-19 BR BRPI9909660A patent/BRPI9909660B8/pt unknown
- 1999-03-19 SI SI9931021T patent/SI1064298T1/sl unknown
- 1999-03-19 CA CA2324226A patent/CA2324226C/en not_active Expired - Lifetime
- 1999-03-19 RU RU2000126298/04A patent/RU2274642C2/ru not_active IP Right Cessation
- 1999-03-19 SK SK1382-2000A patent/SK286736B6/sk not_active IP Right Cessation
- 1999-03-19 GE GEAP19995601A patent/GEP20043163B/en unknown
- 1999-03-19 CZ CZ20003409A patent/CZ302281B6/cs not_active IP Right Cessation
- 1999-03-19 UA UA2000105920A patent/UA74133C2/uk unknown
- 1999-03-19 EP EP99912662A patent/EP1064298B1/en not_active Expired - Lifetime
- 1999-03-19 EP EP08017565A patent/EP2011800A3/en not_active Withdrawn
- 1999-03-19 EP EP10012063A patent/EP2261232A3/en not_active Withdrawn
- 1999-03-19 EP EP10012065A patent/EP2261234A3/en not_active Withdrawn
- 1999-03-19 AT AT99912662T patent/ATE410439T1/de active
- 1999-03-19 AU AU30986/99A patent/AU769033B2/en not_active Expired
- 1999-03-19 JP JP2000536738A patent/JP4594520B2/ja not_active Expired - Lifetime
- 1999-03-19 TR TR2001/03406T patent/TR200103406T2/xx unknown
- 1999-03-19 ES ES99912662T patent/ES2315010T3/es not_active Expired - Lifetime
- 1999-03-19 ID IDW20002100A patent/ID27002A/id unknown
- 1999-03-19 PL PL343611A patent/PL204619B1/pl unknown
- 1999-03-19 CN CNB998059730A patent/CN1321129C/zh not_active Expired - Lifetime
- 1999-03-19 DK DK99912662T patent/DK1064298T3/da active
- 1999-03-19 KR KR1020087002806A patent/KR100928878B1/ko not_active IP Right Cessation
- 1999-03-19 NZ NZ528282A patent/NZ528282A/en not_active IP Right Cessation
- 1999-03-19 EP EP10012066A patent/EP2261235A3/en not_active Withdrawn
- 1999-03-19 HU HU0103575A patent/HU227920B1/hu unknown
- 1999-03-19 WO PCT/US1999/005919 patent/WO1999047545A2/en active IP Right Grant
-
2000
- 2000-09-05 ZA ZA200004652A patent/ZA200004652B/en unknown
- 2000-09-08 IS IS5622A patent/IS5622A/is unknown
- 2000-09-12 NO NO20004546A patent/NO331829B1/no not_active IP Right Cessation
- 2000-09-14 IL IL138469A patent/IL138469A/en not_active IP Right Cessation
- 2000-09-19 US US09/665,503 patent/US6531474B1/en not_active Expired - Lifetime
- 2000-10-16 BG BG104863A patent/BG104863A/xx unknown
-
2001
- 2001-06-20 HK HK01104313.1A patent/HK1035733A1/xx not_active IP Right Cessation
-
2002
- 2002-12-06 US US10/314,103 patent/US7358273B2/en not_active Expired - Fee Related
-
2004
- 2004-12-15 UA UA20041210341A patent/UA96113C2/ru unknown
-
2006
- 2006-03-17 JP JP2006075461A patent/JP2006206600A/ja not_active Withdrawn
-
2008
- 2008-01-22 US US12/009,829 patent/US8691848B2/en not_active Expired - Fee Related
-
2010
- 2010-06-24 IL IL206621A patent/IL206621A0/en unknown
- 2010-07-01 JP JP2010151471A patent/JP2010241822A/ja not_active Withdrawn
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| ZA200004652B (en) | Inhibitors of caspases. | |
| US6350741B1 (en) | Inhibitors of interleukin-1β converting enzyme | |
| ES2380915T3 (es) | Profármaco de un inhibidor de ICE | |
| US6329365B1 (en) | Inhibitors of interleukin-1β converting enzyme | |
| ES2244178T3 (es) | Derivados de 1,2-diazepan como inhibidores de la enzima convertidora de interleuquina-1 beta. | |
| US6008217A (en) | Inhibitors of interleukin-1β converting enzyme | |
| EP1466921A1 (en) | Inhibitors of interleukin-1 beta converting enzyme | |
| ES2344890T3 (es) | Nuevos peptidos como inhibidores de la serina proteasa ns3 del virus de la hepatitis c. | |
| Weston et al. | Granzymes as potential targets for rational drug design | |
| BRPI9917881B1 (pt) | compostos inibidores de caspases, composição farmacêutica e uso de ditos compostos |