JP2005504053A5 - - Google Patents
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- JP2005504053A5 JP2005504053A5 JP2003522514A JP2003522514A JP2005504053A5 JP 2005504053 A5 JP2005504053 A5 JP 2005504053A5 JP 2003522514 A JP2003522514 A JP 2003522514A JP 2003522514 A JP2003522514 A JP 2003522514A JP 2005504053 A5 JP2005504053 A5 JP 2005504053A5
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- JP
- Japan
- Prior art keywords
- group
- halogen
- substituted
- cycloalkyl
- unsubstituted
- 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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- 229910052736 halogen Inorganic materials 0.000 claims 45
- 150000002367 halogens Chemical class 0.000 claims 45
- 125000003118 aryl group Chemical group 0.000 claims 42
- 229910052739 hydrogen Inorganic materials 0.000 claims 37
- 239000001257 hydrogen Substances 0.000 claims 37
- 125000000753 cycloalkyl group Chemical group 0.000 claims 31
- -1 amidine compound Chemical class 0.000 claims 30
- 150000002431 hydrogen Chemical class 0.000 claims 27
- 150000001875 compounds Chemical class 0.000 claims 26
- 239000000126 substance Substances 0.000 claims 23
- 125000000623 heterocyclic group Chemical group 0.000 claims 22
- 125000000217 alkyl group Chemical group 0.000 claims 21
- 125000002947 alkylene group Chemical group 0.000 claims 21
- 125000006729 (C2-C5) alkenyl group Chemical group 0.000 claims 19
- 125000006730 (C2-C5) alkynyl group Chemical group 0.000 claims 19
- 125000001072 heteroaryl group Chemical group 0.000 claims 19
- 150000003839 salts Chemical class 0.000 claims 19
- 125000003545 alkoxy group Chemical group 0.000 claims 13
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 13
- 229910004013 NO 2 Inorganic materials 0.000 claims 12
- 125000003342 alkenyl group Chemical group 0.000 claims 12
- 125000002877 alkyl aryl group Chemical group 0.000 claims 12
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 12
- 125000005129 aryl carbonyl group Chemical group 0.000 claims 12
- 125000004475 heteroaralkyl group Chemical group 0.000 claims 12
- 125000005223 heteroarylcarbonyl group Chemical group 0.000 claims 12
- 125000000304 alkynyl group Chemical group 0.000 claims 11
- 150000001413 amino acids Chemical class 0.000 claims 11
- 125000003710 aryl alkyl group Chemical group 0.000 claims 11
- 125000005160 aryl oxy alkyl group Chemical group 0.000 claims 11
- 125000004104 aryloxy group Chemical group 0.000 claims 11
- 125000000649 benzylidene group Chemical group [H]C(=[*])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 11
- 125000004001 thioalkyl group Chemical group 0.000 claims 11
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 10
- 125000000732 arylene group Chemical group 0.000 claims 7
- 201000010099 disease Diseases 0.000 claims 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 7
- 229910052757 nitrogen Inorganic materials 0.000 claims 7
- 125000004429 atom Chemical group 0.000 claims 6
- 125000005549 heteroarylene group Chemical group 0.000 claims 6
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 6
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 6
- 125000006615 aromatic heterocyclic group Chemical group 0.000 claims 5
- 125000006527 (C1-C5) alkyl group Chemical group 0.000 claims 4
- 125000006833 (C1-C5) alkylene group Chemical group 0.000 claims 4
- 125000004450 alkenylene group Chemical group 0.000 claims 4
- 125000004419 alkynylene group Chemical group 0.000 claims 4
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 4
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 239000001301 oxygen Substances 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 125000004434 sulfur atom Chemical group 0.000 claims 4
- 150000001408 amides Chemical class 0.000 claims 3
- 230000002265 prevention Effects 0.000 claims 3
- 125000005420 sulfonamido group Chemical group S(=O)(=O)(N*)* 0.000 claims 3
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 125000001931 aliphatic group Chemical group 0.000 claims 2
- 230000003941 amyloidogenesis Effects 0.000 claims 2
- 229910052794 bromium Inorganic materials 0.000 claims 2
- 125000002837 carbocyclic group Chemical group 0.000 claims 2
- 230000003920 cognitive function Effects 0.000 claims 2
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 1
- 102000013455 Amyloid beta-Peptides Human genes 0.000 claims 1
- 108010090849 Amyloid beta-Peptides Proteins 0.000 claims 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 1
- 241000282693 Cercopithecidae Species 0.000 claims 1
- 208000005145 Cerebral amyloid angiopathy Diseases 0.000 claims 1
- 206010061818 Disease progression Diseases 0.000 claims 1
- 201000010374 Down Syndrome Diseases 0.000 claims 1
- 206010044688 Trisomy 21 Diseases 0.000 claims 1
- 125000003368 amide group Chemical group 0.000 claims 1
- 150000001409 amidines Chemical class 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- PXXJHWLDUBFPOL-UHFFFAOYSA-N benzamidine Chemical compound NC(=N)C1=CC=CC=C1 PXXJHWLDUBFPOL-UHFFFAOYSA-N 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 230000003013 cytotoxicity Effects 0.000 claims 1
- 231100000135 cytotoxicity Toxicity 0.000 claims 1
- 230000005750 disease progression Effects 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 201000008319 inclusion body myositis Diseases 0.000 claims 1
- 229910052740 iodine Inorganic materials 0.000 claims 1
- SUMDYPCJJOFFON-UHFFFAOYSA-N isethionic acid Chemical compound OCCS(O)(=O)=O SUMDYPCJJOFFON-UHFFFAOYSA-N 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 claims 1
- 230000006641 stabilisation Effects 0.000 claims 1
- 238000011105 stabilization Methods 0.000 claims 1
- 125000000547 substituted alkyl group Chemical group 0.000 claims 1
- 125000003107 substituted aryl group Chemical group 0.000 claims 1
- 125000000565 sulfonamide group Chemical group 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- DLFVBJFMPXGRIB-UHFFFAOYSA-N thioacetamide Natural products CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US31676101P | 2001-08-31 | 2001-08-31 | |
| US38700102P | 2002-06-07 | 2002-06-07 | |
| PCT/CA2002/001353 WO2003017994A1 (en) | 2001-08-31 | 2002-09-03 | Amidine derivatives for treating amyloidosis |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2005504053A JP2005504053A (ja) | 2005-02-10 |
| JP2005504053A5 true JP2005504053A5 (https=) | 2005-12-22 |
Family
ID=26980581
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003522514A Withdrawn JP2005504053A (ja) | 2001-08-31 | 2002-09-03 | アミロイドーシス治療のためのアミジン誘導体 |
Country Status (11)
| Country | Link |
|---|---|
| US (3) | US20040006092A1 (https=) |
| EP (1) | EP1420773A1 (https=) |
| JP (1) | JP2005504053A (https=) |
| KR (1) | KR20040036908A (https=) |
| CN (1) | CN1658852A (https=) |
| BR (1) | BR0212078A (https=) |
| CA (1) | CA2455497A1 (https=) |
| EA (1) | EA200400135A1 (https=) |
| IL (1) | IL160208A0 (https=) |
| MX (1) | MXPA04001153A (https=) |
| WO (1) | WO2003017994A1 (https=) |
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL146143A0 (en) * | 1999-04-28 | 2002-07-25 | Univ Kingston | Compositions and methods for treating amyloidosis |
| EP1237547A2 (en) * | 1999-07-09 | 2002-09-11 | Isis Innovation Limited | Compounds for inhibiting diseases and preparing cells for transplantation |
| EP1337510A4 (en) * | 2000-11-06 | 2005-02-23 | Univ North Carolina | SYNTHESIS AND ANTIMICROBIAL ACTIVITY OF NEW DICATIONIC REVERSED AMIDINES |
| US6737440B2 (en) | 2000-11-06 | 2004-05-18 | The University Of North Carolina At Chapel Hill | Synthesis and antimicrobial activity of novel dicationic “reversed amidines” |
| EP1572129A4 (en) * | 2002-06-07 | 2007-03-28 | Univ North Carolina | AMIDINE DERIVATIVES FOR THE TREATMENT OF AMYLOIDOSE |
| US20050020945A1 (en) * | 2002-07-02 | 2005-01-27 | Tosaya Carol A. | Acoustically-aided cerebrospinal-fluid manipulation for neurodegenerative disease therapy |
| US20040049134A1 (en) * | 2002-07-02 | 2004-03-11 | Tosaya Carol A. | System and methods for treatment of alzheimer's and other deposition-related disorders of the brain |
| US20070010573A1 (en) * | 2003-06-23 | 2007-01-11 | Xianqi Kong | Methods and compositions for treating amyloid-related diseases |
| US7244764B2 (en) * | 2003-06-23 | 2007-07-17 | Neurochem (International) Limited | Methods and compositions for treating amyloid-related diseases |
| JP2007521237A (ja) * | 2003-09-05 | 2007-08-02 | ユニバーシティ オブ ノース カロライナ アット チャペル ヒル | 微生物感染症処置用の新規アミジン化合物 |
| JP2007509176A (ja) * | 2003-10-24 | 2007-04-12 | ザ ユニバーシティ オブ ノース カロライナ アット チャペル ヒル | 抗原虫薬としてのジカチオン性トリアリール類似体 |
| CA2549736A1 (en) * | 2003-12-05 | 2005-06-23 | The University Of North Carolina At Chapel Hill | Cationic substituted benzofurans as antimicrobial agents |
| US7262223B2 (en) * | 2004-01-23 | 2007-08-28 | Neurochem (International) Limited | Amidine derivatives for treating amyloidosis |
| WO2005079780A1 (en) * | 2004-01-23 | 2005-09-01 | Neurochem (International) Limited | Amidine derivatives for treating amyloidosis |
| BRPI0519243A2 (pt) | 2004-12-22 | 2009-01-06 | Neurochem Int Ltd | mÉtodos e composiÇÕes para tratar doenÇas relacionadas a amilàide |
| TW200716088A (en) * | 2005-04-15 | 2007-05-01 | Neurochem Int Ltd | Formulations and methods for treating amyloidosis |
| AU2006201739A1 (en) * | 2005-05-05 | 2006-11-23 | The University Of North Carolina At Chapel Hill | Synthesis and antiprotozoal activity of dicationic 3,5-diphenylisoxazoles |
| WO2007023389A2 (en) * | 2005-07-21 | 2007-03-01 | Neurochem (International) Limited | Polymorphic forms of 3-amino-1-propanesulfonic acid |
| JP5301999B2 (ja) * | 2005-10-31 | 2013-09-25 | メルク・シャープ・アンド・ドーム・コーポレーション | Cetp阻害薬 |
| MX2008008213A (es) * | 2005-12-22 | 2008-09-03 | Neurochem Int Ltd | Tratamiento de trastornos renales, nefropatia diabetica y dislipidemias. |
| DK2089417T3 (en) | 2006-10-12 | 2015-03-23 | Bhi Ltd Partnership | Methods, Compounds, Compositions and Vehicles for Delivery of 3-Amion-1-Propanesulfonic Acid |
| CN101730529A (zh) * | 2006-12-22 | 2010-06-09 | 贝鲁斯健康(国际)有限公司 | 用于治疗代谢疾病和糖尿病的方法、化合物和组合物 |
| CA2676715A1 (en) | 2007-02-12 | 2008-08-21 | Merck & Co., Inc. | Piperazine derivatives for treatment of ad and related conditions |
| EP2247558B2 (en) | 2008-02-14 | 2024-07-03 | Eli Lilly and Company | Novel imaging agents for detecting neurological dysfunction |
| EP2116236A1 (en) * | 2008-04-21 | 2009-11-11 | Université de Mons-Hainaut | Bisbenzamidine derivatives for use as antioxidant |
| FR2933692B1 (fr) * | 2008-07-10 | 2022-12-02 | Univ Nancy 1 Henri Poincare | Nouveaux composes, leur utilisation comme medicaments, et leur procede de preparation |
| ES2355031B2 (es) * | 2009-07-15 | 2011-12-26 | Universidade De Santiago De Compostela | Derivados de bis-benzamidinios y su uso como agentes de reconocimiento de secuencias de adn. |
| ES2368276B2 (es) * | 2010-04-27 | 2012-06-28 | Universidad De Santiago De Compostela | Compuestos derivados de bis-benzamidinios como agentes fluorogénicos para señalizar secuencias específicas de adn de doble cadena. |
| CN103012200B (zh) * | 2011-09-20 | 2014-12-17 | 北京大学 | 具有β-分泌酶抑制功能的化合物及其制备方法与应用 |
| GB201506658D0 (en) | 2015-04-20 | 2015-06-03 | Cellcentric Ltd | Pharmaceutical compounds |
| GB201506660D0 (en) | 2015-04-20 | 2015-06-03 | Cellcentric Ltd | Pharmaceutical compounds |
| CN109553608B (zh) * | 2017-09-26 | 2020-12-08 | 北京大学 | 一类五元六元杂环化合物及其制备方法和治疗肿瘤的用途 |
| US12595251B2 (en) | 2018-06-14 | 2026-04-07 | Georgia State University Research Foundation, Inc. | Amidines and amidine analogs for the treatment of bacterial infections and potentiation antibiotics |
| WO2021127452A1 (en) | 2019-12-19 | 2021-06-24 | Georgia State University Research Foundation, Inc. | Compounds for the treatment of bacterial infections and potentiation of antibiotics |
| CN113264925A (zh) * | 2020-02-14 | 2021-08-17 | 上海美悦生物科技发展有限公司 | 一种杂环化合物及其制备方法和用途 |
| US20250382261A1 (en) * | 2021-11-05 | 2025-12-18 | The Broad Institute, Inc. | Pentamidine analogs |
| CN115850219B (zh) * | 2022-11-30 | 2024-05-28 | 三峡大学 | 泽兰素开链多聚体,制备方法及用途 |
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| US4397863A (en) * | 1980-08-26 | 1983-08-09 | Research Triangle Institute | Inhibition of respiratory syncytial virus-induced cell fusion by amidino compounds |
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| US4619942A (en) * | 1982-04-08 | 1986-10-28 | University Of North Carolina | Inhibition of Respiratory Syncytial virus-induced cell fusion by amidino compounds |
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| US5434050A (en) * | 1991-08-13 | 1995-07-18 | Regents Of The University Of Minnesota | Labelled β-amyloid peptide and methods of screening for Alzheimer's disease |
| JP3008615B2 (ja) * | 1991-11-15 | 2000-02-14 | 大同特殊鋼株式会社 | ラジアル異方性リング磁石及びその製造方法 |
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| US5935982A (en) * | 1997-02-28 | 1999-08-10 | The University Of North Carolina At Chapel Hill | Methods of treating retroviral infection and compounds useful therefor |
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| US6635668B1 (en) * | 1998-07-22 | 2003-10-21 | The University Of North Carolina At Chapel Hill | Imidazoline receptor binding compounds |
| AU758563B2 (en) * | 1998-08-20 | 2003-03-27 | University Of North Carolina At Chapel Hill, The | Dicationic dibenzofuran and dibenzothiophene compounds and methods of use thereof |
| ES2275362T3 (es) * | 1998-09-17 | 2007-06-01 | The University Of North Carolina At Chapel Hill | Actividad antifungica de moleculas dicationicas. |
| US6319944B1 (en) * | 1999-05-10 | 2001-11-20 | Merck & Co., Inc. | Aryl amidines, compositions containing such compounds and methods of use |
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| US20010036949A1 (en) * | 2000-05-09 | 2001-11-01 | Coe Jotham Wadsworth | Pharmaceutical composition and method of treatment of diseases of cognitive dysfunction in a mammal |
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| WO2002002516A2 (en) * | 2000-06-30 | 2002-01-10 | Thomas Jefferson University | Inhibitors of hiv integrase |
| US6737440B2 (en) * | 2000-11-06 | 2004-05-18 | The University Of North Carolina At Chapel Hill | Synthesis and antimicrobial activity of novel dicationic “reversed amidines” |
| JP4368582B2 (ja) * | 2001-01-13 | 2009-11-18 | ユニバーシティ オブ ノース カロライナ アット チャペル ヒル | 牛ウイルス性下痢ウイルス(bvdv)感染およびc型肝炎ウイルス(hcv)感染を処置するのに有用な化合物、方法、および組成物 |
-
2002
- 2002-09-03 EA EA200400135A patent/EA200400135A1/ru unknown
- 2002-09-03 KR KR10-2004-7002085A patent/KR20040036908A/ko not_active Ceased
- 2002-09-03 BR BR0212078-0A patent/BR0212078A/pt not_active IP Right Cessation
- 2002-09-03 JP JP2003522514A patent/JP2005504053A/ja not_active Withdrawn
- 2002-09-03 IL IL16020802A patent/IL160208A0/xx unknown
- 2002-09-03 WO PCT/CA2002/001353 patent/WO2003017994A1/en not_active Ceased
- 2002-09-03 EP EP02758012A patent/EP1420773A1/en not_active Withdrawn
- 2002-09-03 CA CA002455497A patent/CA2455497A1/en not_active Abandoned
- 2002-09-03 CN CN028157702A patent/CN1658852A/zh active Pending
- 2002-09-03 US US10/234,643 patent/US20040006092A1/en not_active Abandoned
- 2002-09-03 MX MXPA04001153A patent/MXPA04001153A/es not_active Application Discontinuation
-
2003
- 2003-12-05 US US10/731,463 patent/US20040147531A1/en not_active Abandoned
-
2006
- 2006-01-19 US US11/335,171 patent/US20070021483A1/en not_active Abandoned
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