JP2010504277A5 - - Google Patents
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- JP2010504277A5 JP2010504277A5 JP2009516579A JP2009516579A JP2010504277A5 JP 2010504277 A5 JP2010504277 A5 JP 2010504277A5 JP 2009516579 A JP2009516579 A JP 2009516579A JP 2009516579 A JP2009516579 A JP 2009516579A JP 2010504277 A5 JP2010504277 A5 JP 2010504277A5
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- JP
- Japan
- Prior art keywords
- hydrogen
- substituted
- groups
- compound
- alkyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Ceased
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- 150000001875 compounds Chemical class 0.000 claims description 38
- 125000000623 heterocyclic group Chemical group 0.000 claims description 15
- 206010028980 Neoplasm Diseases 0.000 claims description 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 5
- 201000011510 cancer Diseases 0.000 claims description 4
- 208000024827 Alzheimer disease Diseases 0.000 claims description 3
- 208000035475 disorder Diseases 0.000 claims description 3
- 208000023105 Huntington disease Diseases 0.000 claims description 2
- 208000018737 Parkinson disease Diseases 0.000 claims description 2
- 201000010099 disease Diseases 0.000 claims description 2
- 208000020431 spinal cord injury Diseases 0.000 claims description 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 51
- 239000001257 hydrogen Substances 0.000 claims 51
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 30
- 150000002431 hydrogen Chemical class 0.000 claims 21
- -1 methylenedioxy Chemical group 0.000 claims 15
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 12
- 125000003118 aryl group Chemical group 0.000 claims 12
- 125000000753 cycloalkyl group Chemical group 0.000 claims 10
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 claims 8
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 claims 8
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 8
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 8
- 229910052736 halogen Inorganic materials 0.000 claims 8
- 150000002367 halogens Chemical class 0.000 claims 8
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 claims 8
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 7
- 150000003839 salts Chemical group 0.000 claims 5
- GBXQPDCOMJJCMJ-UHFFFAOYSA-M trimethyl-[6-(trimethylazaniumyl)hexyl]azanium;bromide Chemical compound [Br-].C[N+](C)(C)CCCCCC[N+](C)(C)C GBXQPDCOMJJCMJ-UHFFFAOYSA-M 0.000 claims 5
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 239000003937 drug carrier Substances 0.000 claims 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 238000000034 method Methods 0.000 claims 3
- 125000000590 4-methylphenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 claims 2
- 108010025454 Cyclin-Dependent Kinase 5 Proteins 0.000 claims 2
- 102000013717 Cyclin-Dependent Kinase 5 Human genes 0.000 claims 2
- 241000790917 Dioxys <bee> Species 0.000 claims 2
- 101001055085 Homo sapiens Mitogen-activated protein kinase kinase kinase 9 Proteins 0.000 claims 2
- 101000851007 Homo sapiens Vascular endothelial growth factor receptor 2 Proteins 0.000 claims 2
- 102100026909 Mitogen-activated protein kinase kinase kinase 9 Human genes 0.000 claims 2
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 2
- 102100033177 Vascular endothelial growth factor receptor 2 Human genes 0.000 claims 2
- 125000000539 amino acid group Chemical group 0.000 claims 2
- 230000002491 angiogenic effect Effects 0.000 claims 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000001301 oxygen Substances 0.000 claims 2
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 239000011593 sulfur Substances 0.000 claims 2
- 125000004800 4-bromophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Br 0.000 claims 1
- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 claims 1
- 208000030507 AIDS Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 201000009273 Endometriosis Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000001132 Osteoporosis Diseases 0.000 claims 1
- 108091000080 Phosphotransferase Proteins 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- 208000036142 Viral infection Diseases 0.000 claims 1
- 206010047571 Visual impairment Diseases 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 210000000988 bone and bone Anatomy 0.000 claims 1
- 210000004556 brain Anatomy 0.000 claims 1
- 208000029028 brain injury Diseases 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 201000002222 hemangioblastoma Diseases 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 208000028867 ischemia Diseases 0.000 claims 1
- 208000002780 macular degeneration Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000000636 p-nitrophenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)[N+]([O-])=O 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 102000020233 phosphotransferase Human genes 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 230000009385 viral infection Effects 0.000 claims 1
- 208000029257 vision disease Diseases 0.000 claims 1
- 230000004393 visual impairment Effects 0.000 claims 1
- 0 CC(C)(C(C(*)=NC(*)C*)=*(C(C)=O)S)C#* Chemical compound CC(C)(C(C(*)=NC(*)C*)=*(C(C)=O)S)C#* 0.000 description 9
- 230000000694 effects Effects 0.000 description 6
- 230000037361 pathway Effects 0.000 description 6
- 101000950669 Homo sapiens Mitogen-activated protein kinase 9 Proteins 0.000 description 3
- 108010055717 JNK Mitogen-Activated Protein Kinases Proteins 0.000 description 3
- 102000019145 JUN kinase activity proteins Human genes 0.000 description 3
- 102100037809 Mitogen-activated protein kinase 9 Human genes 0.000 description 3
- 230000006907 apoptotic process Effects 0.000 description 3
- 210000004027 cell Anatomy 0.000 description 3
- 239000003112 inhibitor Substances 0.000 description 3
- 230000004083 survival effect Effects 0.000 description 3
- BLZKSRBAQDZAIX-UHFFFAOYSA-N Cc1cc(cccc2)c2[s]1 Chemical compound Cc1cc(cccc2)c2[s]1 BLZKSRBAQDZAIX-UHFFFAOYSA-N 0.000 description 2
- 102000001253 Protein Kinase Human genes 0.000 description 2
- 230000030833 cell death Effects 0.000 description 2
- 230000003828 downregulation Effects 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 108060006633 protein kinase Proteins 0.000 description 2
- 108090000623 proteins and genes Proteins 0.000 description 2
- 108020003175 receptors Proteins 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- 201000006474 Brain Ischemia Diseases 0.000 description 1
- 102100022291 C-Jun-amino-terminal kinase-interacting protein 1 Human genes 0.000 description 1
- 101710105206 C-Jun-amino-terminal kinase-interacting protein 1 Proteins 0.000 description 1
- 102000017420 CD3 protein, epsilon/gamma/delta subunit Human genes 0.000 description 1
- GSNUFIFRDBKVIE-UHFFFAOYSA-N Cc1ccc(C)[o]1 Chemical compound Cc1ccc(C)[o]1 GSNUFIFRDBKVIE-UHFFFAOYSA-N 0.000 description 1
- FKNQCJSGGFJEIZ-UHFFFAOYSA-N Cc1ccncc1 Chemical compound Cc1ccncc1 FKNQCJSGGFJEIZ-UHFFFAOYSA-N 0.000 description 1
- ALHUXMDEZNLFTA-UHFFFAOYSA-N Cc1cnc(cccc2)c2n1 Chemical compound Cc1cnc(cccc2)c2n1 ALHUXMDEZNLFTA-UHFFFAOYSA-N 0.000 description 1
- ITQTTZVARXURQS-UHFFFAOYSA-N Cc1cnccc1 Chemical compound Cc1cnccc1 ITQTTZVARXURQS-UHFFFAOYSA-N 0.000 description 1
- PJQIBTFOXWGAEN-UHFFFAOYSA-N Cc1nc2ccccc2[n]1C Chemical compound Cc1nc2ccccc2[n]1C PJQIBTFOXWGAEN-UHFFFAOYSA-N 0.000 description 1
- GIWQSPITLQVMSG-UHFFFAOYSA-N Cc1ncc[n]1C Chemical compound Cc1ncc[n]1C GIWQSPITLQVMSG-UHFFFAOYSA-N 0.000 description 1
- VZWOXDYRBDIHMA-UHFFFAOYSA-N Cc1ncc[s]1 Chemical compound Cc1ncc[s]1 VZWOXDYRBDIHMA-UHFFFAOYSA-N 0.000 description 1
- BSKHPKMHTQYZBB-UHFFFAOYSA-N Cc1ncccc1 Chemical compound Cc1ncccc1 BSKHPKMHTQYZBB-UHFFFAOYSA-N 0.000 description 1
- 206010008120 Cerebral ischaemia Diseases 0.000 description 1
- 206010010904 Convulsion Diseases 0.000 description 1
- 102100023274 Dual specificity mitogen-activated protein kinase kinase 4 Human genes 0.000 description 1
- 101001115395 Homo sapiens Dual specificity mitogen-activated protein kinase kinase 4 Proteins 0.000 description 1
- 101000628949 Homo sapiens Mitogen-activated protein kinase 10 Proteins 0.000 description 1
- 101001005602 Homo sapiens Mitogen-activated protein kinase kinase kinase 11 Proteins 0.000 description 1
- 101000611023 Homo sapiens Tumor necrosis factor receptor superfamily member 6 Proteins 0.000 description 1
- 206010022998 Irritability Diseases 0.000 description 1
- 102100026931 Mitogen-activated protein kinase 10 Human genes 0.000 description 1
- 102100025207 Mitogen-activated protein kinase kinase kinase 11 Human genes 0.000 description 1
- 241000699670 Mus sp. Species 0.000 description 1
- 208000012902 Nervous system disease Diseases 0.000 description 1
- 208000025966 Neurological disease Diseases 0.000 description 1
- 208000030886 Traumatic Brain injury Diseases 0.000 description 1
- 102100040403 Tumor necrosis factor receptor superfamily member 6 Human genes 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- VLSMHEGGTFMBBZ-UHFFFAOYSA-N alpha-Kainic acid Natural products CC(=C)C1CNC(C(O)=O)C1CC(O)=O VLSMHEGGTFMBBZ-UHFFFAOYSA-N 0.000 description 1
- 230000001640 apoptogenic effect Effects 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 244000309464 bull Species 0.000 description 1
- 206010008118 cerebral infarction Diseases 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 210000002950 fibroblast Anatomy 0.000 description 1
- 210000004295 hippocampal neuron Anatomy 0.000 description 1
- 208000027866 inflammatory disease Diseases 0.000 description 1
- VLSMHEGGTFMBBZ-OOZYFLPDSA-N kainic acid Chemical compound CC(=C)[C@H]1CN[C@H](C(O)=O)[C@H]1CC(O)=O VLSMHEGGTFMBBZ-OOZYFLPDSA-N 0.000 description 1
- 229950006874 kainic acid Drugs 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 230000001537 neural effect Effects 0.000 description 1
- 230000004770 neurodegeneration Effects 0.000 description 1
- 208000015122 neurodegenerative disease Diseases 0.000 description 1
- 230000002018 overexpression Effects 0.000 description 1
- 230000001737 promoting effect Effects 0.000 description 1
- 230000001681 protective effect Effects 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 230000009466 transformation Effects 0.000 description 1
- 230000009529 traumatic brain injury Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US81571706P | 2006-06-22 | 2006-06-22 | |
| US11/820,887 US7732447B2 (en) | 2006-06-22 | 2007-06-21 | Fused [d]pyridazin-7-ones |
| PCT/US2007/014559 WO2007149557A1 (en) | 2006-06-22 | 2007-06-22 | FUSED [d]PYRIDAZIN-7-ONES |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010504277A JP2010504277A (ja) | 2010-02-12 |
| JP2010504277A5 true JP2010504277A5 (https=) | 2010-08-05 |
Family
ID=38626544
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009516579A Ceased JP2010504277A (ja) | 2006-06-22 | 2007-06-22 | 縮合［ｄ］ピリダジン−７−オン類 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US7732447B2 (https=) |
| EP (1) | EP2035429B1 (https=) |
| JP (1) | JP2010504277A (https=) |
| CN (1) | CN101501038B (https=) |
| AU (1) | AU2007261305B2 (https=) |
| CA (1) | CA2656034A1 (https=) |
| ES (1) | ES2393216T3 (https=) |
| IL (1) | IL196014A0 (https=) |
| MX (1) | MX2008016388A (https=) |
| NZ (1) | NZ573693A (https=) |
| WO (1) | WO2007149557A1 (https=) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2744498C (en) | 2008-11-25 | 2017-10-24 | University Of Rochester | Mlk inhibitors and methods of use |
| AU2011258465B2 (en) | 2010-05-24 | 2016-12-15 | University Of Rochester | Bicyclic heteroaryl kinase inhibitors and methods of use |
| EP2925319B1 (en) | 2012-11-30 | 2019-01-09 | University Of Rochester | Mixed lineage kinase inhibitors for hiv/aids therapies |
| UA115576C2 (uk) * | 2012-12-06 | 2017-11-27 | Байєр Фарма Акцієнгезелльшафт | Похідні бензимідазолу як антагоністи ер4 |
| KR102129842B1 (ko) * | 2013-10-02 | 2020-07-06 | 주식회사 대웅제약 | 술포닐인돌 유도체 및 이의 제조방법 |
| CN110573509B (zh) * | 2017-02-28 | 2023-05-26 | 北京生命科学研究所 | Mlkl抑制剂 |
| RU2019133646A (ru) * | 2017-03-30 | 2021-04-30 | Ф. Хоффманн-Ля Рош Аг | Изохинолины в качестве ингибиторов hpk1 |
| US11485734B2 (en) | 2018-10-02 | 2022-11-01 | Northwestern University | Beta-carbolines as positive allosteric modulators of the human serotonin receptor 2C (5-HT2C) |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9109972D0 (en) * | 1991-05-09 | 1991-07-03 | Ici Plc | Therapeutic compounds |
| JP3553158B2 (ja) | 1994-10-14 | 2004-08-11 | ポーラ化成工業株式会社 | ピリダジノインドール誘導体 |
| EP1002535A1 (en) | 1998-10-28 | 2000-05-24 | Hrissanthi Ikonomidou | New use of glutamate antagonists for the treatment of cancer |
| GB0121941D0 (en) | 2001-09-11 | 2001-10-31 | Astrazeneca Ab | Chemical compounds |
| FR2833953B1 (fr) * | 2001-12-21 | 2004-12-03 | Sanofi Synthelabo | DERIVES DE 3-HETEROARYL-3,5-DIHYDRO-4-OXO-4H-PYRIDAZINO [4,5-b]INDOLE-1-CARBOXAMIDE, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE |
| AU2003272175A1 (en) | 2002-10-21 | 2004-05-04 | Aprea Ab | Reactivation of wild type p53 in human tumour cells by a low molecular weight compound |
| FR2876377B1 (fr) | 2004-10-11 | 2007-03-16 | Univ Claude Bernard Lyon | Nouveaux derives de 9h-pyrido[2,3-b]indole, leur procede de preparation, ainsi que les compositions pharmaceutiques contenant de tels composes |
-
2007
- 2007-06-21 US US11/820,887 patent/US7732447B2/en not_active Expired - Fee Related
- 2007-06-22 CN CN2007800297073A patent/CN101501038B/zh not_active Expired - Fee Related
- 2007-06-22 NZ NZ573693A patent/NZ573693A/en not_active IP Right Cessation
- 2007-06-22 WO PCT/US2007/014559 patent/WO2007149557A1/en not_active Ceased
- 2007-06-22 ES ES07796360T patent/ES2393216T3/es active Active
- 2007-06-22 AU AU2007261305A patent/AU2007261305B2/en not_active Ceased
- 2007-06-22 MX MX2008016388A patent/MX2008016388A/es active IP Right Grant
- 2007-06-22 EP EP07796360A patent/EP2035429B1/en not_active Not-in-force
- 2007-06-22 JP JP2009516579A patent/JP2010504277A/ja not_active Ceased
- 2007-06-22 CA CA002656034A patent/CA2656034A1/en not_active Abandoned
-
2008
- 2008-12-17 IL IL196014A patent/IL196014A0/en unknown
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