JP2010524898A5 - - Google Patents
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- JP2010524898A5 JP2010524898A5 JP2010503515A JP2010503515A JP2010524898A5 JP 2010524898 A5 JP2010524898 A5 JP 2010524898A5 JP 2010503515 A JP2010503515 A JP 2010503515A JP 2010503515 A JP2010503515 A JP 2010503515A JP 2010524898 A5 JP2010524898 A5 JP 2010524898A5
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- JP
- Japan
- Prior art keywords
- alkyl
- phenyl
- compound according
- optionally substituted
- group
- 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.)
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- 125000000217 alkyl group Chemical group 0.000 claims 42
- 150000001875 compounds Chemical class 0.000 claims 31
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 17
- 125000001072 heteroaryl group Chemical group 0.000 claims 11
- 125000000623 heterocyclic group Chemical group 0.000 claims 8
- 125000003545 alkoxy group Chemical group 0.000 claims 7
- 125000003118 aryl group Chemical group 0.000 claims 7
- 125000004452 carbocyclyl group Chemical group 0.000 claims 7
- 229910052736 halogen Inorganic materials 0.000 claims 7
- 150000002367 halogens Chemical class 0.000 claims 7
- 239000003112 inhibitor Substances 0.000 claims 7
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 6
- 125000002950 monocyclic group Chemical group 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- 206010019375 Helicobacter infections Diseases 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 238000006243 chemical reaction Methods 0.000 claims 4
- -1 cyano, hydroxyl Chemical group 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 230000001771 impaired effect Effects 0.000 claims 4
- 238000004519 manufacturing process Methods 0.000 claims 4
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 3
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 3
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 3
- LZCDAPDGXCYOEH-UHFFFAOYSA-N adapalene Chemical compound C1=C(C(O)=O)C=CC2=CC(C3=CC=C(C(=C3)C34CC5CC(CC(C5)C3)C4)OC)=CC=C21 LZCDAPDGXCYOEH-UHFFFAOYSA-N 0.000 claims 3
- 125000003302 alkenyloxy group Chemical group 0.000 claims 3
- 125000002877 alkyl aryl group Chemical group 0.000 claims 3
- 125000005133 alkynyloxy group Chemical group 0.000 claims 3
- 239000003795 chemical substances by application Substances 0.000 claims 3
- 230000002757 inflammatory effect Effects 0.000 claims 3
- 201000006417 multiple sclerosis Diseases 0.000 claims 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 3
- 125000001424 substituent group Chemical group 0.000 claims 3
- 125000004001 thioalkyl group Chemical group 0.000 claims 3
- MSYGAHOHLUJIKV-UHFFFAOYSA-N 3,5-dimethyl-1-(3-nitrophenyl)-1h-pyrazole-4-carboxylic acid ethyl ester Chemical compound CC1=C(C(=O)OCC)C(C)=NN1C1=CC=CC([N+]([O-])=O)=C1 MSYGAHOHLUJIKV-UHFFFAOYSA-N 0.000 claims 2
- NUKYPUAOHBNCPY-UHFFFAOYSA-N 4-aminopyridine Chemical compound NC1=CC=NC=C1 NUKYPUAOHBNCPY-UHFFFAOYSA-N 0.000 claims 2
- 208000023697 ABri amyloidosis Diseases 0.000 claims 2
- 208000017227 ADan amyloidosis Diseases 0.000 claims 2
- 102000012440 Acetylcholinesterase Human genes 0.000 claims 2
- 108010022752 Acetylcholinesterase Proteins 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 201000001320 Atherosclerosis Diseases 0.000 claims 2
- 208000012639 Balance disease Diseases 0.000 claims 2
- 206010068597 Bulbospinal muscular atrophy congenital Diseases 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 2
- 201000010374 Down Syndrome Diseases 0.000 claims 2
- 206010061825 Duodenal neoplasm Diseases 0.000 claims 2
- 208000030814 Eating disease Diseases 0.000 claims 2
- 208000019454 Feeding and Eating disease Diseases 0.000 claims 2
- 208000035895 Guillain-Barré syndrome Diseases 0.000 claims 2
- 208000023105 Huntington disease Diseases 0.000 claims 2
- 201000000162 ITM2B-related cerebral amyloid angiopathy 1 Diseases 0.000 claims 2
- 201000000194 ITM2B-related cerebral amyloid angiopathy 2 Diseases 0.000 claims 2
- 208000027747 Kennedy disease Diseases 0.000 claims 2
- 206010027476 Metastases Diseases 0.000 claims 2
- 206010049567 Miller Fisher syndrome Diseases 0.000 claims 2
- 206010033645 Pancreatitis Diseases 0.000 claims 2
- 208000018737 Parkinson disease Diseases 0.000 claims 2
- 201000004681 Psoriasis Diseases 0.000 claims 2
- 206010037779 Radiculopathy Diseases 0.000 claims 2
- 206010054184 Small intestine carcinoma Diseases 0.000 claims 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 2
- 230000024932 T cell mediated immunity Effects 0.000 claims 2
- 102000011017 Type 4 Cyclic Nucleotide Phosphodiesterases Human genes 0.000 claims 2
- 108010037584 Type 4 Cyclic Nucleotide Phosphodiesterases Proteins 0.000 claims 2
- 208000006269 X-Linked Bulbo-Spinal Atrophy Diseases 0.000 claims 2
- 201000008629 Zollinger-Ellison syndrome Diseases 0.000 claims 2
- 229940022698 acetylcholinesterase Drugs 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000005213 alkyl heteroaryl group Chemical group 0.000 claims 2
- 125000002947 alkylene group Chemical group 0.000 claims 2
- 230000033228 biological regulation Effects 0.000 claims 2
- 230000015572 biosynthetic process Effects 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 230000001684 chronic effect Effects 0.000 claims 2
- 230000003210 demyelinating effect Effects 0.000 claims 2
- 235000014632 disordered eating Nutrition 0.000 claims 2
- 201000000312 duodenum cancer Diseases 0.000 claims 2
- 230000008482 dysregulation Effects 0.000 claims 2
- 230000037149 energy metabolism Effects 0.000 claims 2
- 206010017758 gastric cancer Diseases 0.000 claims 2
- 201000000052 gastrinoma Diseases 0.000 claims 2
- 230000013632 homeostatic process Effects 0.000 claims 2
- 230000003054 hormonal effect Effects 0.000 claims 2
- 230000028996 humoral immune response Effects 0.000 claims 2
- 208000000509 infertility Diseases 0.000 claims 2
- 230000036512 infertility Effects 0.000 claims 2
- 231100000535 infertility Toxicity 0.000 claims 2
- 230000023404 leukocyte cell-cell adhesion Effects 0.000 claims 2
- KWGKDLIKAYFUFQ-UHFFFAOYSA-M lithium chloride Chemical compound [Li+].[Cl-] KWGKDLIKAYFUFQ-UHFFFAOYSA-M 0.000 claims 2
- 230000003211 malignant effect Effects 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- 230000009401 metastasis Effects 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 230000005012 migration Effects 0.000 claims 2
- 238000013508 migration Methods 0.000 claims 2
- 230000004770 neurodegeneration Effects 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 208000006473 polyradiculopathy Diseases 0.000 claims 2
- 208000037803 restenosis Diseases 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 201000000980 schizophrenia Diseases 0.000 claims 2
- 208000020685 sleep-wake disease Diseases 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 201000011549 stomach cancer Diseases 0.000 claims 2
- NITUEMISTORFON-PPFXTMJRSA-N (2S)-1-[(2S,3R)-2-[[(2S)-2-[[(2S)-1-[(2S,3R)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-6-amino-2-[[(2R)-2-aminopropanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-3-methylbutanoyl]amino]-3-methylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]propanoyl]amino]-4-oxobutanoyl]amino]-3-methylpentanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-hydroxybutanoyl]pyrrolidine-2-carboxylic acid Chemical compound C([C@@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1[C@@H](CCC1)C(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CCCCN)NC(=O)[C@@H](C)N)C(C)C)C(C)C)C1=CC=CC=C1 NITUEMISTORFON-PPFXTMJRSA-N 0.000 claims 1
- DXOZRRSUIYMSAE-UHFFFAOYSA-N 1-(3,4-dimethoxyphenyl)-3-[3-(4-methylimidazol-1-yl)propyl]urea Chemical compound C1=C(OC)C(OC)=CC=C1NC(=O)NCCCN1C=C(C)N=C1 DXOZRRSUIYMSAE-UHFFFAOYSA-N 0.000 claims 1
- UXSPRKSPXIWEHE-UHFFFAOYSA-N 1-(3,4-dimethoxyphenyl)-3-[3-(5-methylimidazol-1-yl)propyl]urea Chemical compound C1=C(OC)C(OC)=CC=C1NC(=O)NCCCN1C(C)=CN=C1 UXSPRKSPXIWEHE-UHFFFAOYSA-N 0.000 claims 1
- UKBIXXCMXVDVNK-UHFFFAOYSA-N 1-(3-cyclopentyloxy-4-methoxyphenyl)-3-[3-(4-methylimidazol-1-yl)propyl]urea Chemical compound C1=C(OC2CCCC2)C(OC)=CC=C1NC(=O)NCCCN1C=NC(C)=C1 UKBIXXCMXVDVNK-UHFFFAOYSA-N 0.000 claims 1
- GLTQOSTWSIBICS-UHFFFAOYSA-N 1-(3-cyclopentyloxy-4-methoxyphenyl)-3-[3-(5-methylimidazol-1-yl)propyl]urea Chemical compound C1=C(OC2CCCC2)C(OC)=CC=C1NC(=O)NCCCN1C=NC=C1C GLTQOSTWSIBICS-UHFFFAOYSA-N 0.000 claims 1
- PJJPDYIMHWXLIS-UHFFFAOYSA-N 1-(3h-benzimidazol-5-yl)-3-(3,4-dimethoxyphenyl)urea Chemical compound C1=C(OC)C(OC)=CC=C1NC(=O)NC1=CC=C(NC=N2)C2=C1 PJJPDYIMHWXLIS-UHFFFAOYSA-N 0.000 claims 1
- BZEJGWYFKLLLCW-UHFFFAOYSA-N 1-(3h-benzimidazol-5-yl)-3-[(3,4-dimethoxyphenyl)methyl]urea Chemical compound C1=C(OC)C(OC)=CC=C1CNC(=O)NC1=CC=C(NC=N2)C2=C1 BZEJGWYFKLLLCW-UHFFFAOYSA-N 0.000 claims 1
- LVIMNVFLBRDRLS-UHFFFAOYSA-N 1-(3h-benzimidazol-5-ylmethyl)-3-(3,4-dimethoxyphenyl)urea Chemical compound C1=C(OC)C(OC)=CC=C1NC(=O)NCC1=CC=C(N=CN2)C2=C1 LVIMNVFLBRDRLS-UHFFFAOYSA-N 0.000 claims 1
- 102000013455 Amyloid beta-Peptides Human genes 0.000 claims 1
- 108010090849 Amyloid beta-Peptides Proteins 0.000 claims 1
- 102000009091 Amyloidogenic Proteins Human genes 0.000 claims 1
- 108010048112 Amyloidogenic Proteins Proteins 0.000 claims 1
- 206010003840 Autonomic nervous system imbalance Diseases 0.000 claims 1
- 102000004190 Enzymes Human genes 0.000 claims 1
- 108090000790 Enzymes Proteins 0.000 claims 1
- 229940125373 Gamma-Secretase Inhibitor Drugs 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 101710144961 Interferon tau-1 Proteins 0.000 claims 1
- 101710144950 Interferon tau-2 Proteins 0.000 claims 1
- 101710144962 Interferon tau-3 Proteins 0.000 claims 1
- 102000004388 Interleukin-4 Human genes 0.000 claims 1
- 108090000978 Interleukin-4 Proteins 0.000 claims 1
- 229940082332 Muscarinic M1 receptor antagonist Drugs 0.000 claims 1
- 108010008881 NBI 5788 Proteins 0.000 claims 1
- 229940099433 NMDA receptor antagonist Drugs 0.000 claims 1
- 229930012538 Paclitaxel Natural products 0.000 claims 1
- 102100031674 Protein-L-isoaspartate(D-aspartate) O-methyltransferase Human genes 0.000 claims 1
- 102100028656 Sigma non-opioid intracellular receptor 1 Human genes 0.000 claims 1
- 101710104750 Sigma non-opioid intracellular receptor 1 Proteins 0.000 claims 1
- 208000025865 Ulcer Diseases 0.000 claims 1
- 229960000548 alemtuzumab Drugs 0.000 claims 1
- 229940035678 anti-parkinson drug Drugs 0.000 claims 1
- 239000000935 antidepressant agent Substances 0.000 claims 1
- 229940005513 antidepressants Drugs 0.000 claims 1
- 239000000939 antiparkinson agent Substances 0.000 claims 1
- 239000000164 antipsychotic agent Substances 0.000 claims 1
- 229940005529 antipsychotics Drugs 0.000 claims 1
- 239000002249 anxiolytic agent Substances 0.000 claims 1
- 230000000949 anxiolytic effect Effects 0.000 claims 1
- 229940005530 anxiolytics Drugs 0.000 claims 1
- 210000000467 autonomic pathway Anatomy 0.000 claims 1
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 claims 1
- 239000002439 beta secretase inhibitor Substances 0.000 claims 1
- 210000001124 body fluid Anatomy 0.000 claims 1
- 239000010839 body fluid Substances 0.000 claims 1
- 208000035269 cancer or benign tumor Diseases 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 208000010877 cognitive disease Diseases 0.000 claims 1
- 230000008021 deposition Effects 0.000 claims 1
- 229940002658 differin Drugs 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 230000004064 dysfunction Effects 0.000 claims 1
- 239000003623 enhancer Substances 0.000 claims 1
- 239000002792 enkephalinase inhibitor Substances 0.000 claims 1
- 229940088598 enzyme Drugs 0.000 claims 1
- 239000002532 enzyme inhibitor Substances 0.000 claims 1
- 229940125532 enzyme inhibitor Drugs 0.000 claims 1
- 239000012530 fluid Substances 0.000 claims 1
- 239000003540 gamma secretase inhibitor Substances 0.000 claims 1
- 239000003395 histamine H3 receptor antagonist Substances 0.000 claims 1
- 239000002955 immunomodulating agent Substances 0.000 claims 1
- 229940121354 immunomodulator Drugs 0.000 claims 1
- 230000002584 immunomodulator Effects 0.000 claims 1
- 229960003444 immunosuppressant agent Drugs 0.000 claims 1
- 230000001861 immunosuppressant effect Effects 0.000 claims 1
- 239000003018 immunosuppressive agent Substances 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 108700027921 interferon tau Proteins 0.000 claims 1
- 229940028885 interleukin-4 Drugs 0.000 claims 1
- 229940121386 matrix metalloproteinase inhibitor Drugs 0.000 claims 1
- 239000003771 matrix metalloproteinase inhibitor Substances 0.000 claims 1
- 208000027061 mild cognitive impairment Diseases 0.000 claims 1
- 239000000234 muscarinic M1 receptor antagonist Substances 0.000 claims 1
- 239000003703 n methyl dextro aspartic acid receptor blocking agent Substances 0.000 claims 1
- 229960005027 natalizumab Drugs 0.000 claims 1
- 230000009826 neoplastic cell growth Effects 0.000 claims 1
- 239000004090 neuroprotective agent Substances 0.000 claims 1
- 229960001592 paclitaxel Drugs 0.000 claims 1
- 230000001568 sexual effect Effects 0.000 claims 1
- 238000003786 synthesis reaction Methods 0.000 claims 1
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 claims 1
- 108010018276 trimethylguanosine synthase Proteins 0.000 claims 1
- 229940046728 tumor necrosis factor alpha inhibitor Drugs 0.000 claims 1
- 239000002452 tumor necrosis factor alpha inhibitor Substances 0.000 claims 1
- 0 C*(C)C*c1ccc2[n]c(*)nc2c1 Chemical compound C*(C)C*c1ccc2[n]c(*)nc2c1 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US91252507P | 2007-04-18 | 2007-04-18 | |
| US60/912,525 | 2007-04-18 | ||
| PCT/EP2008/054716 WO2008128986A1 (en) | 2007-04-18 | 2008-04-18 | Urea derivatives as glutaminyl cyclase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010524898A JP2010524898A (ja) | 2010-07-22 |
| JP2010524898A5 true JP2010524898A5 (show.php) | 2011-05-26 |
| JP5675343B2 JP5675343B2 (ja) | 2015-02-25 |
Family
ID=39638975
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010503515A Expired - Fee Related JP5675343B2 (ja) | 2007-04-18 | 2008-04-18 | グルタミニルシクラーゼ阻害剤としての尿素誘導体 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US9512082B2 (show.php) |
| EP (1) | EP2146968B1 (show.php) |
| JP (1) | JP5675343B2 (show.php) |
| WO (1) | WO2008128986A1 (show.php) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7732162B2 (en) * | 2003-05-05 | 2010-06-08 | Probiodrug Ag | Inhibitors of glutaminyl cyclase for treating neurodegenerative diseases |
| JP5676249B2 (ja) * | 2007-04-20 | 2015-02-25 | プロビオドルグ エージー | グルタミニルシクラーゼ阻害剤としてのアミノピリジン誘導体 |
| WO2009034158A2 (en) * | 2007-09-12 | 2009-03-19 | Probiodrug Ag | Transgenic mice |
| JP2011511622A (ja) * | 2008-01-14 | 2011-04-14 | プロビオドルグ エージー | グルタミニルシクラーゼ遺伝子のノックアウト変異を有するマウスモデル |
| BRPI0916366B1 (pt) | 2008-07-21 | 2021-08-10 | Probiodrug Ag | Anticorpo que se liga às variantes de peptídeos abeta, sua composição, seu uso, seu kit de diagnóstico, e linhagem celular de hibridoma |
| KR101755737B1 (ko) | 2009-09-11 | 2017-07-07 | 프로비오드룩 아게 | 글루타미닐 사이클라제의 억제제로서 헤테로사이클릭 유도체 |
| WO2011076854A1 (en) | 2009-12-22 | 2011-06-30 | Probiodrug Ag | CLEAVAGE OF β-AMYLOID PRECURSOR PROTEIN |
| EP2537029A1 (en) | 2010-02-18 | 2012-12-26 | Probiodrug AG | Methods of diagnosing inflammatory diseases by determining pyroglutamate-modified mcp-1 and screening methods for inhibitors of glutaminyl cyclase |
| MX343873B (es) | 2011-03-16 | 2016-11-25 | Probiodrug Ag | Ensayo de diagnostico de anticuerpo. |
| WO2014113495A1 (en) * | 2013-01-15 | 2014-07-24 | The Trustees Of Columbia University In The City Of New York | Activation or reactivation of ache |
| EP3234611A1 (en) | 2014-12-19 | 2017-10-25 | Probiodrug AG | Novel method for the detection of pglu-abeta peptides |
| EP3135709B1 (en) * | 2015-08-31 | 2018-01-10 | ATOTECH Deutschland GmbH | Imidazoyl urea polymers and their use in metal or metal alloy plating bath compositions |
| PL3461819T3 (pl) | 2017-09-29 | 2020-11-30 | Probiodrug Ag | Inhibitory cyklazy glutaminylowej |
| EP3521308B1 (en) | 2018-01-31 | 2024-03-13 | Vivoryon Therapeutics N.V. | Humanized and de-immunized antibodies |
| CN109734677A (zh) * | 2019-03-07 | 2019-05-10 | 四川大学 | 抑制组蛋白赖氨酸甲基转移酶nsd2的小分子化合物及其应用 |
| KR102230832B1 (ko) * | 2019-06-17 | 2021-03-24 | (주) 메디프론디비티 | N-치환된 티오우레아 또는 우레아 유도체 및 이를 유효성분으로 함유하는 글루타미닐 사이클레이즈 활성 관련 질환의 예방 또는 치료용 약학적 조성물 |
| TR2023016729A2 (tr) * | 2023-12-07 | 2025-06-23 | Bogazici Ueniversitesi | Alzhei̇mer hastaliğinin tedavi̇si̇ne yöneli̇k bi̇leşi̇kler ve bu bi̇leşi̇kleri̇n elde edi̇lme yöntemi̇ |
| CN119954726B (zh) * | 2025-02-08 | 2025-12-05 | 平原实验室 | 芳基脲-咪唑盐类化合物及其合成方法和抗肿瘤活性 |
Family Cites Families (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3399212A (en) * | 1966-05-16 | 1968-08-27 | Smith Kline French Lab | Benzimidazole ureas |
| DE3044566A1 (de) * | 1980-11-26 | 1982-07-15 | Basf Ag, 6700 Ludwigshafen | N-substituierte imidazol-derivate, ihre herstellung, diese enthaltende arzneimittel und ihre verwendung |
| US4576957A (en) * | 1984-07-05 | 1986-03-18 | American Cyanamid Company | N-(Substituted phenyl)-N'-[(1H-imidazol-1-yl) and (1H-1,2,4-triazol-1-yl)alkyl]ureas |
| JPH0275676A (ja) * | 1988-09-12 | 1990-03-15 | Mitsubishi Petrochem Co Ltd | 熱硬化性エポキシ樹脂ワニス |
| EP0386931A1 (en) * | 1989-03-04 | 1990-09-12 | Konica Corporation | A novel cyan coupler |
| GB9823873D0 (en) | 1998-10-30 | 1998-12-30 | Pharmacia & Upjohn Spa | 2-ureido-thiazole derivatives,process for their preparation,and their use as antitumour agents |
| JP2000290260A (ja) * | 1999-04-01 | 2000-10-17 | Shikoku Chem Corp | 新規イミダゾール化合物およびイミダゾール化合物を有効成分とするエポキシ樹脂硬化剤 |
| US6387900B1 (en) | 1999-08-12 | 2002-05-14 | Pharmacia & Upjohn S.P.A. | 3(5)-ureido-pyrazole derivatives process for their preparation and their use as antitumor agents |
| EP1256578B1 (en) | 2001-05-11 | 2006-01-11 | Pfizer Products Inc. | Thiazole derivatives and their use as cdk inhibitors |
| US6948038B2 (en) * | 2001-07-24 | 2005-09-20 | Microsoft Corporation | System and method for backing up and restoring data |
| JP2003192587A (ja) | 2001-12-26 | 2003-07-09 | Bayer Ag | 尿素誘導体 |
| DE602004026712D1 (de) * | 2003-05-05 | 2010-06-02 | Probiodrug Ag | Medizinische verwendung von hemmern von glutaminyl und glutamatcyclasen |
| US7732162B2 (en) * | 2003-05-05 | 2010-06-08 | Probiodrug Ag | Inhibitors of glutaminyl cyclase for treating neurodegenerative diseases |
| WO2004098591A2 (en) | 2003-05-05 | 2004-11-18 | Probiodrug Ag | Inhibitors of glutaminyl cyclase and their use in the treatment of neurological diseases |
| US8338120B2 (en) * | 2003-05-05 | 2012-12-25 | Probiodrug Ag | Method of treating inflammation with glutaminyl cyclase inhibitors |
| WO2005039548A2 (en) | 2003-10-15 | 2005-05-06 | Probiodrug Ag | Use of effectors of glutaminyl and glutamate cyclases |
| US20050171112A1 (en) * | 2003-11-03 | 2005-08-04 | Probiodrug Ag | Combinations useful for the treatment of neuronal disorders |
| CA2544573A1 (en) * | 2003-11-03 | 2005-06-02 | Probiodrug Ag | Combinations useful for the treatment of neuronal disorders |
| US7667044B2 (en) * | 2003-11-03 | 2010-02-23 | Probiodrug Ag | Compounds for the treatment of neurological disorders |
| KR101099206B1 (ko) * | 2004-02-05 | 2011-12-27 | 프로비오드룩 아게 | 신규한 글루타미닐 시클라제 저해제 |
| AR059826A1 (es) * | 2006-03-13 | 2008-04-30 | Univ California | Inhibidores de urea conformacionalmente restringidos de epoxido hidrolasa soluble |
| WO2008034891A2 (en) * | 2006-09-21 | 2008-03-27 | Probiodrug Ag | Novel genes related to glutaminyl cyclase |
| US8420684B2 (en) * | 2006-11-09 | 2013-04-16 | Probiodrug Ag | Inhibitors of glutaminyl cyclase |
| US7741354B2 (en) * | 2006-11-09 | 2010-06-22 | Probiodrug Ag | Inhibitors of glutaminyl cyclase |
| DK2091948T3 (da) * | 2006-11-30 | 2012-07-23 | Probiodrug Ag | Nye inhibitorer af glutaminylcyclase |
| DK2121944T3 (da) * | 2007-01-19 | 2011-10-31 | Probiodrug Ag | In vivo screeningsmodeller til behandling af Alzheimers sygdom og andre QPCT-relaterede lidelser |
| JP5612860B2 (ja) * | 2007-03-09 | 2014-10-22 | プロビオドルグ エージー | グルタミニルシクラーゼ阻害剤としてのイミダゾ［１，５−ａ］ピリジン誘導体 |
-
2008
- 2008-04-18 US US12/105,753 patent/US9512082B2/en not_active Expired - Fee Related
- 2008-04-18 EP EP08736365.1A patent/EP2146968B1/en active Active
- 2008-04-18 JP JP2010503515A patent/JP5675343B2/ja not_active Expired - Fee Related
- 2008-04-18 WO PCT/EP2008/054716 patent/WO2008128986A1/en not_active Ceased
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