ZA200200830B - Tricyclic inhibitors of poly(ADP-ribose) polymerases. - Google Patents
Tricyclic inhibitors of poly(ADP-ribose) polymerases. Download PDFInfo
- Publication number
- ZA200200830B ZA200200830B ZA200200830A ZA200200830A ZA200200830B ZA 200200830 B ZA200200830 B ZA 200200830B ZA 200200830 A ZA200200830 A ZA 200200830A ZA 200200830 A ZA200200830 A ZA 200200830A ZA 200200830 B ZA200200830 B ZA 200200830B
- Authority
- ZA
- South Africa
- Prior art keywords
- aryl
- alkynyl
- cycloalkyl
- alkenyl
- heterocycloalkyl
- Prior art date
Links
- 229920000776 Poly(Adenosine diphosphate-ribose) polymerase Polymers 0.000 title claims description 52
- 108010061844 Poly(ADP-ribose) Polymerases Proteins 0.000 title claims description 44
- 102000012338 Poly(ADP-ribose) Polymerases Human genes 0.000 title claims description 43
- 239000003112 inhibitor Substances 0.000 title description 13
- 125000003118 aryl group Chemical group 0.000 claims description 134
- 125000001072 heteroaryl group Chemical group 0.000 claims description 129
- 125000000304 alkynyl group Chemical group 0.000 claims description 125
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 113
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 111
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 107
- 125000003342 alkenyl group Chemical group 0.000 claims description 104
- -1 cycloall:yl Chemical group 0.000 claims description 100
- 125000000217 alkyl group Chemical group 0.000 claims description 42
- 150000001875 compounds Chemical class 0.000 claims description 38
- 229910052736 halogen Inorganic materials 0.000 claims description 31
- 150000002367 halogens Chemical class 0.000 claims description 31
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 20
- 102000004190 Enzymes Human genes 0.000 claims description 16
- 108090000790 Enzymes Proteins 0.000 claims description 16
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 15
- 230000000694 effects Effects 0.000 claims description 14
- 230000002401 inhibitory effect Effects 0.000 claims description 14
- 230000005764 inhibitory process Effects 0.000 claims description 14
- 125000001424 substituent group Chemical group 0.000 claims description 14
- 238000000034 method Methods 0.000 claims description 11
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 8
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 8
- 125000003545 alkoxy group Chemical group 0.000 claims description 7
- 229910052760 oxygen Inorganic materials 0.000 claims description 7
- 239000003795 chemical substances by application Substances 0.000 claims description 6
- 229910052717 sulfur Inorganic materials 0.000 claims description 6
- 238000000338 in vitro Methods 0.000 claims description 5
- 108010017601 Tankyrases Proteins 0.000 claims description 4
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 3
- 239000001301 oxygen Substances 0.000 claims description 3
- 239000008194 pharmaceutical composition Substances 0.000 claims description 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 2
- 150000003839 salts Chemical class 0.000 claims 27
- 239000000651 prodrug Substances 0.000 claims 22
- 229940002612 prodrug Drugs 0.000 claims 22
- 239000012453 solvate Substances 0.000 claims 22
- 239000002207 metabolite Substances 0.000 claims 19
- 101710179684 Poly [ADP-ribose] polymerase Proteins 0.000 claims 12
- 102100023712 Poly [ADP-ribose] polymerase 1 Human genes 0.000 claims 12
- 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 claims 8
- ATJFFYVFTNAWJD-UHFFFAOYSA-N Tin Chemical compound [Sn] ATJFFYVFTNAWJD-UHFFFAOYSA-N 0.000 claims 4
- 125000004104 aryloxy group Chemical group 0.000 claims 4
- 238000003556 assay Methods 0.000 claims 4
- 125000005553 heteroaryloxy group Chemical group 0.000 claims 4
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 4
- 235000010582 Pisum sativum Nutrition 0.000 claims 3
- 240000004713 Pisum sativum Species 0.000 claims 3
- 230000003013 cytotoxicity Effects 0.000 claims 3
- 231100000135 cytotoxicity Toxicity 0.000 claims 3
- JGFZNNIVVJXRND-UHFFFAOYSA-N N,N-Diisopropylethylamine (DIPEA) Chemical compound CCN(C(C)C)C(C)C JGFZNNIVVJXRND-UHFFFAOYSA-N 0.000 claims 2
- 102100037664 Poly [ADP-ribose] polymerase tankyrase-1 Human genes 0.000 claims 2
- 101001091385 Homo sapiens Kallikrein-6 Proteins 0.000 claims 1
- 102100034866 Kallikrein-6 Human genes 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 102100035591 POU domain, class 2, transcription factor 2 Human genes 0.000 claims 1
- 101710084411 POU domain, class 2, transcription factor 2 Proteins 0.000 claims 1
- 125000005282 allenyl group Chemical group 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 239000012661 PARP inhibitor Substances 0.000 description 12
- 229940121906 Poly ADP ribose polymerase inhibitor Drugs 0.000 description 12
- 108091026813 Poly(ADPribose) Proteins 0.000 description 10
- MWUXSHHQAYIFBG-UHFFFAOYSA-N Nitric oxide Chemical compound O=[N] MWUXSHHQAYIFBG-UHFFFAOYSA-N 0.000 description 8
- 238000011161 development Methods 0.000 description 7
- 230000018109 developmental process Effects 0.000 description 7
- 230000006378 damage Effects 0.000 description 6
- 239000003814 drug Substances 0.000 description 6
- 108020004414 DNA Proteins 0.000 description 5
- 102000003960 Ligases Human genes 0.000 description 5
- 108090000364 Ligases Proteins 0.000 description 5
- 208000006011 Stroke Diseases 0.000 description 5
- 210000004027 cell Anatomy 0.000 description 5
- 206010012601 diabetes mellitus Diseases 0.000 description 5
- 230000003389 potentiating effect Effects 0.000 description 5
- 108090000623 proteins and genes Proteins 0.000 description 5
- PLRACCBDVIHHLZ-UHFFFAOYSA-N 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine Chemical compound C1N(C)CCC(C=2C=CC=CC=2)=C1 PLRACCBDVIHHLZ-UHFFFAOYSA-N 0.000 description 4
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 description 4
- 230000004913 activation Effects 0.000 description 4
- 230000015572 biosynthetic process Effects 0.000 description 4
- 230000030833 cell death Effects 0.000 description 4
- 229940079593 drug Drugs 0.000 description 4
- 208000028867 ischemia Diseases 0.000 description 4
- 230000004770 neurodegeneration Effects 0.000 description 4
- 102000004169 proteins and genes Human genes 0.000 description 4
- 230000001225 therapeutic effect Effects 0.000 description 4
- 206010019196 Head injury Diseases 0.000 description 3
- 208000027089 Parkinsonian disease Diseases 0.000 description 3
- 206010034010 Parkinsonism Diseases 0.000 description 3
- 208000027418 Wounds and injury Diseases 0.000 description 3
- 238000013459 approach Methods 0.000 description 3
- 208000014674 injury Diseases 0.000 description 3
- 208000015122 neurodegenerative disease Diseases 0.000 description 3
- 238000011275 oncology therapy Methods 0.000 description 3
- 102000055501 telomere Human genes 0.000 description 3
- 108091035539 telomere Proteins 0.000 description 3
- 210000003411 telomere Anatomy 0.000 description 3
- SRNWOUGRCWSEMX-KEOHHSTQSA-N ADP-beta-D-ribose Chemical group C([C@H]1O[C@H]([C@@H]([C@@H]1O)O)N1C=2N=CN=C(C=2N=C1)N)OP(O)(=O)OP(O)(=O)OC[C@H]1O[C@@H](O)[C@H](O)[C@@H]1O SRNWOUGRCWSEMX-KEOHHSTQSA-N 0.000 description 2
- 201000006474 Brain Ischemia Diseases 0.000 description 2
- HMFHBZSHGGEWLO-SOOFDHNKSA-N D-ribofuranose Chemical compound OC[C@H]1OC(O)[C@H](O)[C@@H]1O HMFHBZSHGGEWLO-SOOFDHNKSA-N 0.000 description 2
- 102000011724 DNA Repair Enzymes Human genes 0.000 description 2
- 108010076525 DNA Repair Enzymes Proteins 0.000 description 2
- 230000005778 DNA damage Effects 0.000 description 2
- 231100000277 DNA damage Toxicity 0.000 description 2
- 206010061218 Inflammation Diseases 0.000 description 2
- 241000699670 Mus sp. Species 0.000 description 2
- 208000007201 Myocardial reperfusion injury Diseases 0.000 description 2
- BAWFJGJZGIEFAR-NNYOXOHSSA-N NAD zwitterion Chemical compound NC(=O)C1=CC=C[N+]([C@H]2[C@@H]([C@H](O)[C@@H](COP([O-])(=O)OP(O)(=O)OC[C@@H]3[C@H]([C@@H](O)[C@@H](O3)N3C4=NC=NC(N)=C4N=C3)O)O2)O)=C1 BAWFJGJZGIEFAR-NNYOXOHSSA-N 0.000 description 2
- 206010029350 Neurotoxicity Diseases 0.000 description 2
- DFPAKSUCGFBDDF-UHFFFAOYSA-N Nicotinamide Chemical compound NC(=O)C1=CC=CN=C1 DFPAKSUCGFBDDF-UHFFFAOYSA-N 0.000 description 2
- PYMYPHUHKUWMLA-LMVFSUKVSA-N Ribose Natural products OC[C@@H](O)[C@@H](O)[C@@H](O)C=O PYMYPHUHKUWMLA-LMVFSUKVSA-N 0.000 description 2
- 102000004535 Tankyrases Human genes 0.000 description 2
- 206010044221 Toxic encephalopathy Diseases 0.000 description 2
- 238000009825 accumulation Methods 0.000 description 2
- HIMXGTXNXJYFGB-UHFFFAOYSA-N alloxan Chemical compound O=C1NC(=O)C(=O)C(=O)N1 HIMXGTXNXJYFGB-UHFFFAOYSA-N 0.000 description 2
- HMFHBZSHGGEWLO-UHFFFAOYSA-N alpha-D-Furanose-Ribose Natural products OCC1OC(O)C(O)C1O HMFHBZSHGGEWLO-UHFFFAOYSA-N 0.000 description 2
- 206010003246 arthritis Diseases 0.000 description 2
- 210000004556 brain Anatomy 0.000 description 2
- 208000029028 brain injury Diseases 0.000 description 2
- 230000001413 cellular effect Effects 0.000 description 2
- 238000002512 chemotherapy Methods 0.000 description 2
- VYFYYTLLBUKUHU-UHFFFAOYSA-N dopamine Chemical compound NCCC1=CC=C(O)C(O)=C1 VYFYYTLLBUKUHU-UHFFFAOYSA-N 0.000 description 2
- 238000009510 drug design Methods 0.000 description 2
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 description 2
- 230000005865 ionizing radiation Effects 0.000 description 2
- 230000000302 ischemic effect Effects 0.000 description 2
- 208000031225 myocardial ischemia Diseases 0.000 description 2
- 229950006238 nadide Drugs 0.000 description 2
- 230000001537 neural effect Effects 0.000 description 2
- 230000007135 neurotoxicity Effects 0.000 description 2
- 231100000228 neurotoxicity Toxicity 0.000 description 2
- 230000002265 prevention Effects 0.000 description 2
- 230000004224 protection Effects 0.000 description 2
- 230000008439 repair process Effects 0.000 description 2
- ZSJLQEPLLKMAKR-GKHCUFPYSA-N streptozocin Chemical compound O=NN(C)C(=O)N[C@H]1[C@@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O ZSJLQEPLLKMAKR-GKHCUFPYSA-N 0.000 description 2
- 229960001052 streptozocin Drugs 0.000 description 2
- 238000003786 synthesis reaction Methods 0.000 description 2
- 238000012546 transfer Methods 0.000 description 2
- 238000011282 treatment Methods 0.000 description 2
- IOEPOEDBBPRAEI-UHFFFAOYSA-N 1,2-dihydroisoquinoline Chemical class C1=CC=C2CNC=CC2=C1 IOEPOEDBBPRAEI-UHFFFAOYSA-N 0.000 description 1
- KLNFQJDLPUPRJZ-UHFFFAOYSA-N 2-nitro-5h-phenanthridin-6-one Chemical compound C1=CC=C2C3=CC([N+](=O)[O-])=CC=C3NC(=O)C2=C1 KLNFQJDLPUPRJZ-UHFFFAOYSA-N 0.000 description 1
- GSCPDZHWVNUUFI-UHFFFAOYSA-N 3-aminobenzamide Chemical compound NC(=O)C1=CC=CC(N)=C1 GSCPDZHWVNUUFI-UHFFFAOYSA-N 0.000 description 1
- SSMIFVHARFVINF-UHFFFAOYSA-N 4-amino-1,8-naphthalimide Chemical compound O=C1NC(=O)C2=CC=CC3=C2C1=CC=C3N SSMIFVHARFVINF-UHFFFAOYSA-N 0.000 description 1
- PWJFNRJRHXWEPT-UHFFFAOYSA-N ADP ribose Natural products C1=NC=2C(N)=NC=NC=2N1C1OC(COP(O)(=O)OP(O)(=O)OCC(O)C(O)C(O)C=O)C(O)C1O PWJFNRJRHXWEPT-UHFFFAOYSA-N 0.000 description 1
- 210000002237 B-cell of pancreatic islet Anatomy 0.000 description 1
- 208000024172 Cardiovascular disease Diseases 0.000 description 1
- 206010008120 Cerebral ischaemia Diseases 0.000 description 1
- 125000000824 D-ribofuranosyl group Chemical group [H]OC([H])([H])[C@@]1([H])OC([H])(*)[C@]([H])(O[H])[C@]1([H])O[H] 0.000 description 1
- 102000053602 DNA Human genes 0.000 description 1
- 102000012410 DNA Ligases Human genes 0.000 description 1
- 108010061982 DNA Ligases Proteins 0.000 description 1
- 108090000323 DNA Topoisomerases Proteins 0.000 description 1
- 102000003915 DNA Topoisomerases Human genes 0.000 description 1
- 230000033616 DNA repair Effects 0.000 description 1
- 231100001074 DNA strand break Toxicity 0.000 description 1
- 102000004163 DNA-directed RNA polymerases Human genes 0.000 description 1
- 108090000626 DNA-directed RNA polymerases Proteins 0.000 description 1
- 102000004533 Endonucleases Human genes 0.000 description 1
- 108010042407 Endonucleases Proteins 0.000 description 1
- 208000009386 Experimental Arthritis Diseases 0.000 description 1
- 229940123457 Free radical scavenger Drugs 0.000 description 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
- 208000032843 Hemorrhage Diseases 0.000 description 1
- 108010033040 Histones Proteins 0.000 description 1
- 102000006947 Histones Human genes 0.000 description 1
- 102000004877 Insulin Human genes 0.000 description 1
- 108090001061 Insulin Proteins 0.000 description 1
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 241000699666 Mus <mouse, genus> Species 0.000 description 1
- 101100238304 Mus musculus Morc1 gene Proteins 0.000 description 1
- 239000005104 Neeliglow 4-amino-1,8-naphthalimide Substances 0.000 description 1
- 206010028980 Neoplasm Diseases 0.000 description 1
- 101710138657 Neurotoxin Proteins 0.000 description 1
- 102000008299 Nitric Oxide Synthase Human genes 0.000 description 1
- 108010021487 Nitric Oxide Synthase Proteins 0.000 description 1
- 208000018737 Parkinson disease Diseases 0.000 description 1
- 206010063837 Reperfusion injury Diseases 0.000 description 1
- 108010017842 Telomerase Proteins 0.000 description 1
- 102000004357 Transferases Human genes 0.000 description 1
- 108090000992 Transferases Proteins 0.000 description 1
- DFPAKSUCGFBDDF-ZQBYOMGUSA-N [14c]-nicotinamide Chemical compound N[14C](=O)C1=CC=CN=C1 DFPAKSUCGFBDDF-ZQBYOMGUSA-N 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 230000003712 anti-aging effect Effects 0.000 description 1
- 229940124650 anti-cancer therapies Drugs 0.000 description 1
- 230000000259 anti-tumor effect Effects 0.000 description 1
- 238000011319 anticancer therapy Methods 0.000 description 1
- 230000006907 apoptotic process Effects 0.000 description 1
- 230000008901 benefit Effects 0.000 description 1
- 150000003936 benzamides Chemical class 0.000 description 1
- 125000003785 benzimidazolyl group Chemical class N1=C(NC2=C1C=CC=C2)* 0.000 description 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 1
- 230000033228 biological regulation Effects 0.000 description 1
- 210000004204 blood vessel Anatomy 0.000 description 1
- 201000011510 cancer Diseases 0.000 description 1
- 239000003560 cancer drug Substances 0.000 description 1
- 230000003197 catalytic effect Effects 0.000 description 1
- 230000009134 cell regulation Effects 0.000 description 1
- 230000010094 cellular senescence Effects 0.000 description 1
- 230000003727 cerebral blood flow Effects 0.000 description 1
- 206010008118 cerebral infarction Diseases 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 238000003776 cleavage reaction Methods 0.000 description 1
- 230000002860 competitive effect Effects 0.000 description 1
- 230000002089 crippling effect Effects 0.000 description 1
- 231100000433 cytotoxic Toxicity 0.000 description 1
- 230000001472 cytotoxic effect Effects 0.000 description 1
- 230000007812 deficiency Effects 0.000 description 1
- 230000007850 degeneration Effects 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 238000013461 design Methods 0.000 description 1
- 125000004663 dialkyl amino group Chemical group 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 229960003638 dopamine Drugs 0.000 description 1
- 230000002526 effect on cardiovascular system Effects 0.000 description 1
- 125000001033 ether group Chemical group 0.000 description 1
- 210000003527 eukaryotic cell Anatomy 0.000 description 1
- 239000008103 glucose Substances 0.000 description 1
- 229930195712 glutamate Natural products 0.000 description 1
- 125000001475 halogen functional group Chemical group 0.000 description 1
- 210000005260 human cell Anatomy 0.000 description 1
- 125000004356 hydroxy functional group Chemical group O* 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 230000004968 inflammatory condition Effects 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 229940125396 insulin Drugs 0.000 description 1
- 230000003834 intracellular effect Effects 0.000 description 1
- 210000004153 islets of langerhan Anatomy 0.000 description 1
- LFUJIPVWTMGYDG-UHFFFAOYSA-N isoquinoline-1,5-diol Chemical compound N1=CC=C2C(O)=CC=CC2=C1O LFUJIPVWTMGYDG-UHFFFAOYSA-N 0.000 description 1
- 238000011813 knockout mouse model Methods 0.000 description 1
- 238000012423 maintenance Methods 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 230000001035 methylating effect Effects 0.000 description 1
- 208000010125 myocardial infarction Diseases 0.000 description 1
- 210000005036 nerve Anatomy 0.000 description 1
- 230000000626 neurodegenerative effect Effects 0.000 description 1
- 210000002569 neuron Anatomy 0.000 description 1
- 230000007171 neuropathology Effects 0.000 description 1
- 230000004112 neuroprotection Effects 0.000 description 1
- 239000004090 neuroprotective agent Substances 0.000 description 1
- 239000002581 neurotoxin Substances 0.000 description 1
- 231100000618 neurotoxin Toxicity 0.000 description 1
- 239000002858 neurotransmitter agent Substances 0.000 description 1
- 229960003966 nicotinamide Drugs 0.000 description 1
- 235000005152 nicotinamide Nutrition 0.000 description 1
- 239000011570 nicotinamide Substances 0.000 description 1
- 229930027945 nicotinamide-adenine dinucleotide Natural products 0.000 description 1
- CMFNMSMUKZHDEY-UHFFFAOYSA-N peroxynitrous acid Chemical compound OON=O CMFNMSMUKZHDEY-UHFFFAOYSA-N 0.000 description 1
- 230000005731 poly ADP ribosylation Effects 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 230000001681 protective effect Effects 0.000 description 1
- JWVCLYRUEFBMGU-UHFFFAOYSA-N quinazoline Chemical compound N1=CN=CC2=CC=CC=C21 JWVCLYRUEFBMGU-UHFFFAOYSA-N 0.000 description 1
- 150000003246 quinazolines Chemical class 0.000 description 1
- 239000002516 radical scavenger Substances 0.000 description 1
- 238000001959 radiotherapy Methods 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 230000010410 reperfusion Effects 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 230000028617 response to DNA damage stimulus Effects 0.000 description 1
- 230000000979 retarding effect Effects 0.000 description 1
- 230000007017 scission Effects 0.000 description 1
- 230000009758 senescence Effects 0.000 description 1
- 230000011664 signaling Effects 0.000 description 1
- 230000009759 skin aging Effects 0.000 description 1
- 150000003384 small molecules Chemical class 0.000 description 1
- 230000002269 spontaneous effect Effects 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 210000003523 substantia nigra Anatomy 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 239000003053 toxin Substances 0.000 description 1
- 231100000765 toxin Toxicity 0.000 description 1
- 108700012359 toxins Proteins 0.000 description 1
- 210000004881 tumor cell Anatomy 0.000 description 1
- 208000035408 type 1 diabetes mellitus 1 Diseases 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
- C07D487/06—Peri-condensed systems
-
- 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
- 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
- A61P25/28—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
- 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
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Diabetes (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Endocrinology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Hematology (AREA)
- Hospice & Palliative Care (AREA)
- Emergency Medicine (AREA)
- Obesity (AREA)
- Psychiatry (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US15214299P | 1999-08-31 | 1999-08-31 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA200200830B true ZA200200830B (en) | 2003-03-26 |
Family
ID=22541675
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA200200830A ZA200200830B (en) | 1999-08-31 | 2002-01-30 | Tricyclic inhibitors of poly(ADP-ribose) polymerases. |
Country Status (48)
Families Citing this family (68)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6291425B1 (en) | 1999-09-01 | 2001-09-18 | Guilford Pharmaceuticals Inc. | Compounds, methods and pharmaceutical compositions for treating cellular damage, such as neural or cardiovascular tissue damage |
| PL347885A1 (en) * | 1999-09-28 | 2002-04-22 | Basf Ag | Azepinoindole derivatives, the production and use thereof |
| DE19946289A1 (de) * | 1999-09-28 | 2001-03-29 | Basf Ag | Benzodiazepin-Derivate, deren Herstellung und Anwendung |
| DE10021468A1 (de) * | 2000-05-04 | 2001-11-08 | Basf Ag | Verwendung von PARP-Inhibitoren in kosmetischen Zubereitungen |
| US7151102B2 (en) | 2000-10-30 | 2006-12-19 | Kudos Pharmaceuticals Limited | Phthalazinone derivatives |
| FR2816942B1 (fr) * | 2000-11-23 | 2003-05-09 | Sanofi Synthelabo | Derives de benzimidazole, leur preparation et leur application en therapeutique |
| AU2002358650A1 (en) * | 2001-12-14 | 2003-06-30 | Altana Pharma Ag | Known and novel 4,5-dihydro-imidazo(4,5,1-ij)quinolin-6-ones useful as poly(adp-ribose)polymerase inhibitors |
| US7026311B2 (en) | 2002-01-10 | 2006-04-11 | Abbott Gmbh & Co., Kg | Dibenzodiazepine derivatives, their preparation and use |
| ES2357057T3 (es) | 2002-04-30 | 2011-04-15 | Kudos Pharmaceuticals Limited | Derivados de ftalazinona. |
| AU2003236686A1 (en) * | 2002-06-07 | 2003-12-22 | Altana Pharma Ag | 4,5-dihydro-imidazo(4,5,1-j) quinolin-6-ones as parp inhibitors |
| HRP20050624A2 (en) | 2003-01-09 | 2006-02-28 | Pfizer Inc. | Diazepinoindole derivatives as kinaze inhibitors |
| US7449464B2 (en) | 2003-03-12 | 2008-11-11 | Kudos Pharmaceuticals Limited | Phthalazinone derivatives |
| GB0305681D0 (en) | 2003-03-12 | 2003-04-16 | Kudos Pharm Ltd | Phthalazinone derivatives |
| SI1660095T1 (sl) * | 2003-07-25 | 2010-05-31 | Cancer Rec Tech Ltd | Triciklični parp inhibitorji |
| GB0317466D0 (en) * | 2003-07-25 | 2003-08-27 | Univ Sheffield | Use |
| WO2005035534A1 (ja) * | 2003-10-08 | 2005-04-21 | Ono Pharmaceutical Co., Ltd. | 複素ビシクロ環および複素トリシクロ環化合物およびその医薬 |
| WO2005053662A1 (en) | 2003-12-01 | 2005-06-16 | Kudos Pharmaceuticals Limited | Dna damage repair inhibitors for treatment of cancer |
| GB0419072D0 (en) | 2004-08-26 | 2004-09-29 | Kudos Pharm Ltd | Phthalazinone derivatives |
| DE602005018506D1 (de) * | 2004-09-22 | 2010-02-04 | Pfizer | Verfahren zur herstellung von poly(adp-ribose)polymeraseinhibitoren |
| MX2007008771A (es) * | 2005-01-19 | 2007-09-11 | Mgi Gp Inc | Compuestos de diazabenzo [des] antracen-3-ona y metodos para inhibir parp. |
| EP1902057B1 (en) | 2005-06-14 | 2013-10-23 | Merck Sharp & Dohme Corp. | Macrocyclic heterocyclic aspartyl protease inhibitors |
| JPWO2006137510A1 (ja) | 2005-06-24 | 2009-01-22 | 小野薬品工業株式会社 | 脳血管障害時における出血低減剤 |
| CA2615374A1 (en) * | 2005-07-18 | 2007-01-25 | Ernest Kun Kun | Treatment of cancer |
| MX2008001152A (es) * | 2005-08-05 | 2008-04-02 | Astrazeneca Ab | Benzimidazoles triciclicos y su uso como moduladores del receptor de glutamato metabotropico. |
| GB0521373D0 (en) | 2005-10-20 | 2005-11-30 | Kudos Pharm Ltd | Pthalazinone derivatives |
| US20070292883A1 (en) * | 2006-06-12 | 2007-12-20 | Ossovskaya Valeria S | Method of treating diseases with PARP inhibitors |
| US20100279327A1 (en) * | 2006-06-12 | 2010-11-04 | Bipar Sciences, Inc. | Method of treating diseases with parp inhibitors |
| US20080262062A1 (en) * | 2006-11-20 | 2008-10-23 | Bipar Sciences, Inc. | Method of treating diseases with parp inhibitors |
| CA2662517A1 (en) * | 2006-09-05 | 2008-03-13 | Jerome Moore | Treatment of cancer |
| EP2061479A4 (en) * | 2006-09-05 | 2010-08-04 | Bipar Sciences Inc | FETTIC ACID SYNTHESIS INHIBITED BY PARP HEMMER AND TREATMENT PROCEDURES THEREWITH |
| TWI404716B (zh) | 2006-10-17 | 2013-08-11 | Kudos Pharm Ltd | 酞嗪酮(phthalazinone)衍生物 |
| US8188301B2 (en) | 2007-06-05 | 2012-05-29 | Nsab, Filial Af Neurosearch Sweden Ab, Sverige | Disubstituted phenylpyrrolidines as modulators of cortical catecholaminergic neurotransmission |
| WO2008154129A1 (en) * | 2007-06-08 | 2008-12-18 | Bausch & Lomb Incorporated | Pharmaceutical compositions and method for treating, reducing, ameliorating, alleviating, or preventing dry eye |
| JP2010539149A (ja) | 2007-09-14 | 2010-12-16 | アストラゼネカ アクチボラグ | フタラジノン誘導体 |
| KR20100102607A (ko) * | 2007-11-12 | 2010-09-24 | 바이파 사이언스 인코포레이티드 | Parp 억제제를 단독으로 사용하거나 항종양제와 병용하여 자궁암 및 난소암을 치료하는 방법 |
| CA2705537A1 (en) * | 2007-11-12 | 2009-05-22 | Bipar Sciences, Inc. | Treatment of breast cancer with a parp inhibitor alone or in combination with anti-tumor agents |
| MX2010006154A (es) * | 2007-12-07 | 2010-09-24 | Bipar Sciences Inc | Tratamiento del cancer con combinaciones de inhibidores de la topoisomerasa e inhibidores de la poli-adp-ribosa-polimerasa. |
| AR070221A1 (es) | 2008-01-23 | 2010-03-25 | Astrazeneca Ab | Derivados de ftalazinona inhibidores de polimerasas, composiciones farmaceuticas que los contienen y usos de los mismos para prevenir y/o tratar tumores cancerigenos,lesiones isquemicas y otras enfermedades asociadas. |
| RU2010136966A (ru) * | 2008-02-04 | 2012-03-20 | Байпар Сайенсиз, Инк. (Us) | Способы диагностики и лечения заболеваний, опосредованных parp |
| GB0804755D0 (en) * | 2008-03-14 | 2008-04-16 | Angeletti P Ist Richerche Bio | Therapeutic compounds |
| PT2346495T (pt) | 2008-10-07 | 2016-11-11 | Astrazeneca Uk Ltd | Formulação farmacêutica 514 |
| WO2011058367A2 (en) | 2009-11-13 | 2011-05-19 | Astrazeneca Ab | Diagnostic test for predicting responsiveness to treatment with poly(adp-ribose) polymerase (parp) inhibitor |
| EP2892344A1 (de) * | 2012-09-05 | 2015-07-15 | Bayer CropScience AG | Verwendung substituierter benzodiazepinone und benzazepinone oder deren salze als wirkstoffe gegen abiotischen pflanzenstress |
| ES2700348T3 (es) * | 2014-01-05 | 2019-02-15 | Univ Washington | Trazadores radioetiquetados para poli (ADP-ribosa) polimerasa-1 (PARP-1), métodos y usos para estos |
| LT3325623T (lt) | 2015-07-23 | 2019-10-25 | Inst Curie | Dbait molekulės ir parp inhibitorių derinio panaudojimas vėžiui gydyti |
| GB201519573D0 (en) | 2015-11-05 | 2015-12-23 | King S College London | Combination |
| US10874641B2 (en) | 2016-07-28 | 2020-12-29 | Mitobridge, Inc. | Methods of treating acute kidney injury |
| CN110300600A (zh) | 2016-11-02 | 2019-10-01 | 伊缪诺金公司 | 利用抗体-药物缀合物和parp抑制剂的组合治疗 |
| WO2018162439A1 (en) | 2017-03-08 | 2018-09-13 | Onxeo | New predictive biomarker for the sensitivity to a treatment of cancer with a dbait molecule |
| EP3615026B1 (en) | 2017-04-28 | 2021-03-03 | Akribes Biomedical GmbH | A parp inhibitor in combination with a glucocorticoid and/or ascorbic acid and/or a protein growth factor for the treatment of impaired wound healing |
| EP3735297A1 (en) | 2018-01-05 | 2020-11-11 | Cybrexa 1, Inc. | Compounds, compositions, and methods for treatment of diseases involving acidic or hypoxic diseased tissues |
| CN111819282A (zh) | 2018-03-13 | 2020-10-23 | 欧恩科斯欧公司 | 对抗癌症治疗中获得性耐药性的Dbait分子 |
| TW202019408A (zh) * | 2018-06-28 | 2020-06-01 | 美商永恒生物科技公司 | 稠合三環雜環化合物及其治療用途 |
| WO2020038387A1 (zh) * | 2018-08-24 | 2020-02-27 | 杭州阿诺生物医药科技有限公司 | 高活性sting蛋白激动剂 |
| US20220056044A1 (en) * | 2018-12-14 | 2022-02-24 | Jiangsu Hengrui Medicine Co., Ltd. | Tricyclic compounds as sting agonists, and preparation methods and medicinal uses thereof |
| AU2020214351A1 (en) * | 2019-02-02 | 2021-09-09 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Indolo heptamyl oxime analogue as PARP inhibitor |
| CN111909157B (zh) * | 2019-05-07 | 2023-02-03 | 南京药石科技股份有限公司 | Ezh2抑制剂及其用途 |
| JP7675060B2 (ja) | 2019-07-10 | 2025-05-12 | サイブレクサ 3,インコーポレイテッド | 治療薬としての微小管標的化剤のペプチドコンジュゲート |
| US11634508B2 (en) | 2019-07-10 | 2023-04-25 | Cybrexa 2, Inc. | Peptide conjugates of cytotoxins as therapeutics |
| GB201913030D0 (en) | 2019-09-10 | 2019-10-23 | Francis Crick Institute Ltd | Treatment of hr deficient cancer |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| ES3014370T3 (en) | 2020-04-28 | 2025-04-22 | Rhizen Pharmaceuticals Ag | Novel compounds useful as poly(adp-ribose) polymerase (parp) inhibitors |
| WO2022090938A1 (en) | 2020-10-31 | 2022-05-05 | Rhizen Pharmaceuticals Ag | Phthalazinone derivatives useful as parp inhibitors |
| PE20240119A1 (es) | 2021-01-08 | 2024-01-22 | Cybrexa 2 Inc | Proceso para preparar un resto enlazador de conjugados |
| WO2022155172A1 (en) | 2021-01-13 | 2022-07-21 | Cybrexa 3, Inc. | Peptide conjugates of therapeutics |
| JP2024515338A (ja) | 2021-04-08 | 2024-04-09 | ライゼン ファーマシューティカルズ アーゲー | ポリ(adp-リボース)ポリメラーゼの阻害剤 |
| WO2024261243A1 (en) | 2023-06-21 | 2024-12-26 | Hemispherian As | Combination comprising a deoxycytidine derivative and a parp inhibitor for use in a method of treating hr proficient cancer |
| WO2025106920A1 (en) * | 2023-11-15 | 2025-05-22 | Yale University | Parp pet imaging agents and methods of using the same |
Family Cites Families (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1052390A (cs) | 1964-03-24 | |||
| US3642820A (en) * | 1969-11-03 | 1972-02-15 | Upjohn Co | 4 5-dihydropyrrolo(3 2 1-jk)(1 4)bezodiazepines |
| US3734919A (en) * | 1969-11-03 | 1973-05-22 | Upjohn Co | 4,5-di-hydropyrrolo(3,2,1-jk)(1,4)benzodiazepin-7(6h)-ones and 4,5-di-hydropyrrolo(1,2,3-ef)(1,5)benzodiazepin-6(7h)-ones |
| DE2056215A1 (de) | 1970-11-16 | 1972-05-18 | Farbwerke Hoechst AG, vorm. Meister Lucius & Brüning, 6000 Frankfurt | Verfahren zur Herstellung von N-Mono-(beta-Cyanäthyl>anilinen |
| US3883590A (en) | 1971-06-01 | 1975-05-13 | Universal Oil Prod Co | Preparation of n-alkylarylcarboxamides |
| US3978066A (en) | 1973-11-06 | 1976-08-31 | Ayerst, Mckenna And Harrison Ltd. | Certain 4,6-dihydropyrrolotriazoline-quinoline derivatives |
| US3950343A (en) | 1973-11-06 | 1976-04-13 | Ayerst, Mckenna And Harrison Ltd. | Pyrroloisoquinoline derivatives |
| US3900477A (en) | 1973-11-06 | 1975-08-19 | Ayerst Mckenna & Harrison | 5-amino-and 5-hydrazinodihydropyrroloisoquinoline derivatives |
| JPS57144286A (en) | 1981-03-02 | 1982-09-06 | Takeda Chem Ind Ltd | Azepinoindole derivative and its preparation |
| US4910193A (en) | 1985-12-16 | 1990-03-20 | Sandoz Ltd. | Treatment of gastrointestinal disorders |
| DE4125292A1 (de) | 1991-07-31 | 1993-02-04 | Kali Chemie Pharma Gmbh | 6-oxo-azepinoindol-verbindungen sowie verfahren und zwischenprodukte zu ihrer herstellung und diese verbindungen enthaltende arzneimittel |
| US5342946A (en) | 1992-12-02 | 1994-08-30 | Guilford Pharmaceuticals Inc. | Phosphonoalkylquinolin-2-ones as novel antagonists of non-NMDA ionotropic excitatory amino acid receptors |
| EP0670831A1 (en) | 1993-09-28 | 1995-09-13 | Otsuka Pharmaceutical Co., Ltd. | Quinoxaline derivative as antidiabetic agent |
| US5587384A (en) | 1994-02-04 | 1996-12-24 | The Johns Hopkins University | Inhibitors of poly(ADP-ribose) synthetase and use thereof to treat NMDA neurotoxicity |
| GB9404485D0 (en) | 1994-03-09 | 1994-04-20 | Cancer Res Campaign Tech | Benzamide analogues |
| US5561161A (en) | 1994-03-25 | 1996-10-01 | Oxigene, Inc. | Methods of administering and pharmaceutical formulations containing n-substituted benzamides and/or acid addition salts thereof |
| US5589483A (en) | 1994-12-21 | 1996-12-31 | Geron Corporation | Isoquinoline poly (ADP-ribose) polymerase inhibitors to treat skin diseases associated with cellular senescence |
| ES2105959B1 (es) | 1995-01-17 | 1998-07-01 | Zeneca Pharma Sa | Derivados de 1,4-dioxido de quinoxalina, procedimiento de preparacion y de utilizacion. |
| US5756548A (en) | 1995-04-03 | 1998-05-26 | Centaur Pharmaceuticals, Inc. | Acetamidobenzamide compounds for neurodegenerative disorders |
| US5659082A (en) | 1995-04-03 | 1997-08-19 | Centaur Pharmaceuticals, Inc. | Nitro- and aminobenzamide compounds for neurodegenerative disorders |
| PT841924E (pt) | 1995-08-02 | 2003-02-28 | Univ Newcastle Ventures Ltd | Compostos de benzimidazolo |
| HUT76302A (en) | 1995-11-30 | 1997-07-28 | Chinoin Gyogyszer Es Vegyeszet | Quinoxaline derivatives, pharmaceutical compositions containing them and process for producing them |
| GB9702701D0 (en) | 1997-02-01 | 1997-04-02 | Univ Newcastle Ventures Ltd | Quinazolinone compounds |
| WO1998051308A1 (en) | 1997-05-13 | 1998-11-19 | Octamer, Inc. | METHODS FOR TREATING INFLAMMATION AND INFLAMMATORY DISEASES USING pADPRT INHIBITORS |
| US6197785B1 (en) | 1997-09-03 | 2001-03-06 | Guilford Pharmaceuticals Inc. | Alkoxy-substituted compounds, methods, and compositions for inhibiting PARP activity |
| US6635642B1 (en) | 1997-09-03 | 2003-10-21 | Guilford Pharmaceuticals Inc. | PARP inhibitors, pharmaceutical compositions comprising same, and methods of using same |
| WO1999011622A1 (en) | 1997-09-03 | 1999-03-11 | Guilford Pharmaceuticals Inc. | Amino-substituted compounds, methods, and compositions for inhibiting parp activity |
| US20020022636A1 (en) | 1997-09-03 | 2002-02-21 | Jia-He Li | Oxo-substituted compounds, process of making, and compositions and methods for inhibiting parp activity |
| AU9298198A (en) | 1997-09-03 | 1999-03-22 | Guilford Pharmaceuticals Inc. | Di-n-heterocyclic compounds, methods, and compositions for inhibiting parp activity |
| US6514983B1 (en) | 1997-09-03 | 2003-02-04 | Guilford Pharmaceuticals Inc. | Compounds, methods and pharmaceutical compositions for treating neural or cardiovascular tissue damage |
| US20020028813A1 (en) | 1997-09-03 | 2002-03-07 | Paul F. Jackson | Thioalkyl compounds, methods, and compositions for inhibiting parp activity |
| WO1999059975A1 (en) | 1998-05-15 | 1999-11-25 | Guilford Pharmaceuticals Inc. | Fused tricyclic compounds which inhibit parp activity |
| WO1999059973A1 (en) | 1998-05-15 | 1999-11-25 | Guilford Pharmaceuticals Inc. | Carboxamide compounds, compositions, and methods for inhibiting parp activity |
-
2000
- 2000-08-29 EC EC2000003637A patent/ECSP003637A/es unknown
- 2000-08-30 CO CO00065062A patent/CO5200769A1/es not_active Application Discontinuation
- 2000-08-30 MY MYPI20004039A patent/MY135910A/en unknown
- 2000-08-30 GT GT200000145A patent/GT200000145A/es unknown
- 2000-08-31 WO PCT/US2000/023882 patent/WO2001016136A2/en not_active Ceased
- 2000-08-31 UA UA2002042574A patent/UA73144C2/uk unknown
- 2000-08-31 DK DK00961437T patent/DK1208104T3/da active
- 2000-08-31 DZ DZ003216A patent/DZ3216A1/fr active
- 2000-08-31 IL IL14786300A patent/IL147863A0/xx unknown
- 2000-08-31 YU YU15102A patent/YU15102A/sh unknown
- 2000-08-31 OA OA1200200064A patent/OA12016A/en unknown
- 2000-08-31 PL PL00354242A patent/PL354242A1/xx not_active Application Discontinuation
- 2000-08-31 SV SV2000000162A patent/SV2003000162A/es unknown
- 2000-08-31 KR KR1020027002629A patent/KR20020038742A/ko not_active Abandoned
- 2000-08-31 SK SK259-2002A patent/SK2592002A3/sk unknown
- 2000-08-31 US US09/653,184 patent/US6548494B1/en not_active Expired - Lifetime
- 2000-08-31 AP APAP/P/2002/002449A patent/AP1553A/en active
- 2000-08-31 EP EP00961437A patent/EP1208104B1/en not_active Expired - Lifetime
- 2000-08-31 UY UY26323A patent/UY26323A1/es not_active Application Discontinuation
- 2000-08-31 CA CA002382404A patent/CA2382404C/en not_active Expired - Fee Related
- 2000-08-31 AR ARP000104549A patent/AR035162A1/es unknown
- 2000-08-31 SI SI200030643T patent/SI1208104T1/xx unknown
- 2000-08-31 PE PE2000000896A patent/PE20010538A1/es not_active Application Discontinuation
- 2000-08-31 MX MXPA02002138A patent/MXPA02002138A/es active IP Right Grant
- 2000-08-31 PA PA20008501801A patent/PA8501801A1/es unknown
- 2000-08-31 JP JP2001519702A patent/JP4272375B2/ja not_active Expired - Lifetime
- 2000-08-31 GE GEAP20006389A patent/GEP20043268B/en unknown
- 2000-08-31 HU HU0202703A patent/HUP0202703A3/hu unknown
- 2000-08-31 BR BR0015051-7A patent/BR0015051A/pt not_active Application Discontinuation
- 2000-08-31 PT PT00961437T patent/PT1208104E/pt unknown
- 2000-08-31 AT AT00961437T patent/ATE287406T1/de not_active IP Right Cessation
- 2000-08-31 DE DE60017575T patent/DE60017575T2/de not_active Expired - Lifetime
- 2000-08-31 NZ NZ516793A patent/NZ516793A/en unknown
- 2000-08-31 ES ES00961437T patent/ES2234657T3/es not_active Expired - Lifetime
- 2000-08-31 CN CN00815066A patent/CN1384835A/zh active Pending
- 2000-08-31 CZ CZ2002613A patent/CZ2002613A3/cs unknown
- 2000-08-31 HR HR20020271A patent/HRP20020271A2/hr not_active Application Discontinuation
- 2000-08-31 HK HK02106977.2A patent/HK1045509B/en not_active IP Right Cessation
- 2000-08-31 AU AU73389/00A patent/AU781826B2/en not_active Ceased
- 2000-08-31 EA EA200200306A patent/EA200200306A1/ru unknown
- 2000-08-31 EE EEP200200100A patent/EE200200100A/xx unknown
- 2000-09-20 DO DO2000000069A patent/DOP2000000069A/es unknown
-
2002
- 2002-01-28 NO NO20020421A patent/NO322475B1/no unknown
- 2002-01-30 ZA ZA200200830A patent/ZA200200830B/en unknown
- 2002-02-01 CR CR6577A patent/CR6577A/es not_active Application Discontinuation
- 2002-02-27 IS IS6289A patent/IS6289A/is unknown
- 2002-03-29 MA MA26577A patent/MA25876A1/fr unknown
- 2002-03-29 BG BG106562A patent/BG106562A/bg unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| ZA200200830B (en) | Tricyclic inhibitors of poly(ADP-ribose) polymerases. | |
| Curtin | PARP inhibitors for cancer therapy | |
| Southan et al. | Poly (ADP-ribose) polymerase inhibitors | |
| TWI338000B (en) | Dna damage repair inhibitors for treatment of cancer | |
| Cosi | New inhibitors of poly (ADP-ribose) polymerase and their potential therapeutic targets | |
| EP1633362B1 (en) | Compounds, methods and pharmaceutical compositions for inhibiting parp | |
| MXPA05010563A (es) | Sales de los inhibidores triciclicos de las poli(adp-ribosa) polimerasas. | |
| Jiang et al. | Inhibition of calmodulin-dependent phosphodiesterase induces apoptosis in human leukemic cells. | |
| Bürkle et al. | The emerging role of poly (ADP-ribose) polymerase-1 in longevity | |
| ZA200103566B (en) | Pharmaceutical compositions containing poly(ADP-ribose) glycohydrolase inhibitors and methods of using the same. | |
| Woon et al. | Poly (ADP-ribose) polymerase inhibition-where now? | |
| ZA200105399B (en) | Tricyclic inhibitors of poly(ADP-ribose) polymerases. | |
| WO2000000202A1 (en) | Method for inhibiting c-jun expression using jak-3 inhibitors | |
| ZA200610774B (en) | Phthalazine derivatives as PARP inhibitors | |
| US20030147813A1 (en) | Method for treating chronic myelogenous leukemia | |
| Komjati et al. | Poly (adp-ribose) polymerase inhibitors as potential therapeutic agents in stroke and neurotrauma | |
| JP2025061603A (ja) | 骨髄増殖性腫瘍の治療のためのヤヌスキナーゼ阻害剤およびテロメラーゼ阻害剤の使用 | |
| EP2177222B1 (en) | Pyrimidylaminobenzamide derivatives for the treatment of neurofibromatosis | |
| US20030144178A1 (en) | Method for inhibiting C-jun expression using JAK-3 inhibitors | |
| WO2010006153A2 (en) | Topopyrones: dual topoisomerase inhibitors | |
| Lawrence et al. | Targeting DNA repair mechanisms to treat glioblastoma | |
| CN115038440A (zh) | 使用chk抑制剂的癌症联合疗法 | |
| Rouleau et al. | Potential role of PARP inhibitors in cancer treatment and cell death | |
| TW202428280A (zh) | 組合療法 | |
| HK40087531A (zh) | Janus激酶抑制剂和端粒酶抑制剂用於治疗骨髓增殖性肿瘤的用途 |