JP2009539882A5 - - Google Patents
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- Publication number
- JP2009539882A5 JP2009539882A5 JP2009514564A JP2009514564A JP2009539882A5 JP 2009539882 A5 JP2009539882 A5 JP 2009539882A5 JP 2009514564 A JP2009514564 A JP 2009514564A JP 2009514564 A JP2009514564 A JP 2009514564A JP 2009539882 A5 JP2009539882 A5 JP 2009539882A5
- Authority
- JP
- Japan
- Prior art keywords
- chor
- independently
- compound
- lower alkyl
- cap
- 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.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims 23
- 125000000217 alkyl group Chemical group 0.000 claims 16
- 239000001257 hydrogen Substances 0.000 claims 13
- 229910052739 hydrogen Inorganic materials 0.000 claims 13
- 150000002431 hydrogen Chemical group 0.000 claims 10
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 9
- 108010052164 Sodium Channels Proteins 0.000 claims 4
- 102000018674 Sodium Channels Human genes 0.000 claims 4
- 102000012740 beta Adrenergic Receptors Human genes 0.000 claims 4
- 108010079452 beta Adrenergic Receptors Proteins 0.000 claims 4
- -1 methylenedioxy group Chemical group 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 125000004414 alkyl thio group Chemical group 0.000 claims 3
- 229930182480 glucuronide Natural products 0.000 claims 3
- 230000036571 hydration Effects 0.000 claims 3
- 238000006703 hydration reaction Methods 0.000 claims 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
- WNXJIVFYUVYPPR-UHFFFAOYSA-N 1,3-dioxolane Chemical compound C1COCO1 WNXJIVFYUVYPPR-UHFFFAOYSA-N 0.000 claims 2
- 108010078678 Osmolite Proteins 0.000 claims 2
- 206010035664 Pneumonia Diseases 0.000 claims 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims 2
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 2
- 229940124630 bronchodilator Drugs 0.000 claims 2
- 239000000168 bronchodilator agent Substances 0.000 claims 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 230000018044 dehydration Effects 0.000 claims 2
- 238000006297 dehydration reaction Methods 0.000 claims 2
- 206010013781 dry mouth Diseases 0.000 claims 2
- 239000008103 glucose Substances 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical group 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 1
- 206010006458 Bronchitis chronic Diseases 0.000 claims 1
- 101100240517 Caenorhabditis elegans nhr-11 gene Proteins 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 206010010774 Constipation Diseases 0.000 claims 1
- 201000003883 Cystic fibrosis Diseases 0.000 claims 1
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims 1
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims 1
- 206010013774 Dry eye Diseases 0.000 claims 1
- 206010013786 Dry skin Diseases 0.000 claims 1
- 206010014561 Emphysema Diseases 0.000 claims 1
- 241000792859 Enema Species 0.000 claims 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 claims 1
- 229930195725 Mannitol Natural products 0.000 claims 1
- 206010030216 Oesophagitis Diseases 0.000 claims 1
- 206010033078 Otitis media Diseases 0.000 claims 1
- 102100028045 P2Y purinoceptor 2 Human genes 0.000 claims 1
- 101710096700 P2Y purinoceptor 2 Proteins 0.000 claims 1
- 206010036790 Productive cough Diseases 0.000 claims 1
- 208000021386 Sjogren Syndrome Diseases 0.000 claims 1
- 206010047791 Vulvovaginal dryness Diseases 0.000 claims 1
- 239000000556 agonist Substances 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000005036 alkoxyphenyl group Chemical group 0.000 claims 1
- 125000005037 alkyl phenyl group Chemical group 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 230000000903 blocking effect Effects 0.000 claims 1
- 206010006451 bronchitis Diseases 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 239000000460 chlorine Substances 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 230000001713 cholinergic effect Effects 0.000 claims 1
- 208000007451 chronic bronchitis Diseases 0.000 claims 1
- 208000027157 chronic rhinosinusitis Diseases 0.000 claims 1
- 230000001886 ciliary effect Effects 0.000 claims 1
- 208000007784 diverticulitis Diseases 0.000 claims 1
- 230000037336 dry skin Effects 0.000 claims 1
- 239000007920 enema Substances 0.000 claims 1
- 229940095399 enema Drugs 0.000 claims 1
- 208000006881 esophagitis Diseases 0.000 claims 1
- 150000008134 glucuronides Chemical class 0.000 claims 1
- 125000005059 halophenyl group Chemical group 0.000 claims 1
- 208000003243 intestinal obstruction Diseases 0.000 claims 1
- 239000000594 mannitol Substances 0.000 claims 1
- 235000010355 mannitol Nutrition 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 210000000214 mouth Anatomy 0.000 claims 1
- 230000008881 mucosal defense Effects 0.000 claims 1
- 210000003097 mucus Anatomy 0.000 claims 1
- 239000001301 oxygen Substances 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000003379 purinergic P1 receptor agonist Substances 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 201000009890 sinusitis Diseases 0.000 claims 1
- 239000011780 sodium chloride Substances 0.000 claims 1
- 210000003802 sputum Anatomy 0.000 claims 1
- 208000024794 sputum Diseases 0.000 claims 1
- 239000000829 suppository Substances 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 125000003396 thiol group Chemical group [H]S* 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US81207706P | 2006-06-09 | 2006-06-09 | |
| US60/812,077 | 2006-06-09 | ||
| PCT/US2007/070861 WO2007146869A1 (en) | 2006-06-09 | 2007-06-11 | Phenyl substituted pyrazinoylguanidine sodium channel blockers possessing beta agonist activity |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2009539882A JP2009539882A (ja) | 2009-11-19 |
| JP2009539882A5 true JP2009539882A5 (https=) | 2010-07-29 |
| JP5254961B2 JP5254961B2 (ja) | 2013-08-07 |
Family
ID=38832114
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009514564A Expired - Fee Related JP5254961B2 (ja) | 2006-06-09 | 2007-06-11 | ベータアゴニスト活性を有するフェニル置換ピラジノイルグアニジンナトリウムチャネル遮断薬 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US8163758B2 (https=) |
| EP (1) | EP2035004B1 (https=) |
| JP (1) | JP5254961B2 (https=) |
| AU (1) | AU2007257781B2 (https=) |
| CA (1) | CA2654244A1 (https=) |
| DK (1) | DK2035004T3 (https=) |
| ES (1) | ES2392999T3 (https=) |
| NO (1) | NO20085128L (https=) |
| PL (1) | PL2035004T3 (https=) |
| PT (1) | PT2035004E (https=) |
| SI (1) | SI2035004T1 (https=) |
| WO (1) | WO2007146869A1 (https=) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6858615B2 (en) | 2002-02-19 | 2005-02-22 | Parion Sciences, Inc. | Phenyl guanidine sodium channel blockers |
| ES2432529T3 (es) | 2003-08-18 | 2013-12-04 | Parion Sciences, Inc. | Bloqueadores del canal de sodio de pirazinoilguanidina rematada |
| US7807834B2 (en) | 2005-08-03 | 2010-10-05 | Parion Sciences, Inc. | Capped pyrazinoylguanidine sodium channel blockers |
| KR100901664B1 (ko) | 2007-08-06 | 2009-06-09 | 주식회사 오스코텍 | β-아미노알콜 유도체, 이의 제조방법 및 이를유효성분으로 함유하는 ＴＮＦ-α 매개성 질환의 예방 및치료용 약학적 조성물 |
| DE102007040615A1 (de) * | 2007-08-27 | 2009-03-05 | Bitop Ag | Osmolyte zur Behandlung von allergisch oder viral bedingten Atemwegserkrankungen |
| CA2702094C (en) | 2007-10-10 | 2018-05-01 | Parion Sciences, Inc. | Delivering osmolytes by nasal cannula |
| DE102007052380A1 (de) * | 2007-10-31 | 2009-05-07 | Bitop Ag | Osmolythaltige Zubereitungen zur Anwendung bei trockenen Schleimhäuten |
| ES2485642T3 (es) * | 2008-02-26 | 2014-08-14 | Parion Sciences, Inc. | Bloqueantes poli-aromáticos de los canales de sodio |
| EP2569285A1 (en) | 2010-05-10 | 2013-03-20 | Gilead Sciences, Inc. | Bifunctional quinoline derivatives |
| US8367829B2 (en) | 2010-05-10 | 2013-02-05 | Gilead Sciences, Inc. | Bi-functional pyrazolopyridine compounds |
| WO2012032546A2 (en) * | 2010-09-08 | 2012-03-15 | Cadila Healthcare Limited | Process for the preparation of salmeterol and its intermediates |
| DE102011103347B4 (de) * | 2011-05-27 | 2014-10-30 | Meda Pharma Gmbh & Co. Kg | Nasale pharmazeutische Formulierung |
| EP2717855A4 (en) | 2011-06-07 | 2014-11-12 | Parion Sciences Inc | Methods of Treatment |
| US8945605B2 (en) | 2011-06-07 | 2015-02-03 | Parion Sciences, Inc. | Aerosol delivery systems, compositions and methods |
| CN103687488B (zh) | 2011-06-27 | 2015-06-10 | 帕里昂科学公司 | 化学和代谢稳定的具有钠通道阻滞剂活性的二肽 |
| AR086745A1 (es) | 2011-06-27 | 2014-01-22 | Parion Sciences Inc | 3,5-diamino-6-cloro-n-(n-(4-(4-(2-(hexil(2,3,4,5,6-pentahidroxihexil)amino)etoxi)fenil)butil)carbamimidoil)pirazina-2-carboxamida |
| HUE039734T2 (hu) | 2012-05-29 | 2019-01-28 | Parion Sciences Inc | Nátriumcsatorna-blokkoló aktivitású, dendrimerszerû amino-amid-származékok száraz szem és más nyálkahártya-megbetegedések kezelésére |
| CN108658876A (zh) | 2012-12-17 | 2018-10-16 | 帕里昂科学公司 | 3,5-二氨基-6-氯-n-(n-(4-苯基丁基)甲脒基)吡嗪-2-甲酰胺化合物 |
| ES2674665T3 (es) * | 2012-12-17 | 2018-07-03 | Parion Sciences, Inc. | Compuestos de 3,5-diamino-6-cloro-N-(N-(4-fenilbutilo)carbamimidoilo)-pirazina-2-carboxamida |
| CA2895512C (en) | 2012-12-17 | 2021-10-19 | Parion Sciences, Inc. | Chloro-pyrazine carboxamide derivatives useful for the treatment of diseases favoured by insufficient mucosal hydration |
| MX368243B (es) | 2013-08-23 | 2019-09-25 | Parion Sciences Inc | Agentes mucolíticos de ditiol. |
| US9102633B2 (en) | 2013-12-13 | 2015-08-11 | Parion Sciences, Inc. | Arylalkyl- and aryloxyalkyl-substituted epithelial sodium channel blocking compounds |
| GB201406225D0 (en) * | 2014-04-07 | 2014-05-21 | Hall Roderick L | Treatment for respiratory disease |
| US20150376145A1 (en) | 2014-06-30 | 2015-12-31 | Parion Sciences, Inc. | Stable sodium channel blockers |
| CA2974210A1 (en) | 2015-01-30 | 2016-08-04 | Parion Sciences, Inc. | Novel monothiol mucolytic agents |
| CA2984424A1 (en) | 2015-04-30 | 2016-11-03 | Parion Sciences, Inc. | Novel prodrugs of dithiol mucolytic agents |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AUPR034000A0 (en) * | 2000-09-25 | 2000-10-19 | Fujisawa Pharmaceutical Co., Ltd. | Aminoalcohol derivatives |
| US6858614B2 (en) | 2002-02-19 | 2005-02-22 | Parion Sciences, Inc. | Phenolic guanidine sodium channel blockers |
| US6858615B2 (en) | 2002-02-19 | 2005-02-22 | Parion Sciences, Inc. | Phenyl guanidine sodium channel blockers |
| US6903105B2 (en) | 2003-02-19 | 2005-06-07 | Parion Sciences, Inc. | Sodium channel blockers |
| US7268147B2 (en) * | 2003-05-15 | 2007-09-11 | Pfizer Inc | Compounds useful for the treatment of diseases |
| GB0312832D0 (en) * | 2003-06-04 | 2003-07-09 | Pfizer Ltd | 2-amino-pyridine derivatives useful for the treatment of diseases |
| ES2432529T3 (es) | 2003-08-18 | 2013-12-04 | Parion Sciences, Inc. | Bloqueadores del canal de sodio de pirazinoilguanidina rematada |
| US20050090505A1 (en) | 2003-08-18 | 2005-04-28 | Johnson Michael R. | Methods of reducing risk of infection from pathogens |
| JP2007502829A (ja) | 2003-08-18 | 2007-02-15 | パリオン・サイエンシィズ・インコーポレーテッド | 環状ピラジノイルグアニジンナトリウムチャネルブロッカー |
| US7375107B2 (en) | 2003-08-18 | 2008-05-20 | Parion Sciences, Inc. | Alaphatic pyrazinoylguanidine sodium channel blockers |
| US7745442B2 (en) | 2003-08-20 | 2010-06-29 | Parion Sciences, Inc. | Methods of reducing risk of infection from pathogens |
| US7399766B2 (en) * | 2004-08-18 | 2008-07-15 | Parion Sciences, Inc. | Soluble amide & ester pyrazinoylguanidine sodium channel blockers |
| CA2575680A1 (en) | 2004-08-18 | 2006-03-02 | Michael R. Johnson | Cyclic amide & ester pyrazinoylguanidine sodium channel blockers |
| US20070021439A1 (en) * | 2005-07-25 | 2007-01-25 | Parion Sciences, Inc. | Methods of reducing risk of infection from pathogens with soluble amide and ester pyrazinoylguanidine sodium channel blockers |
| US7807834B2 (en) | 2005-08-03 | 2010-10-05 | Parion Sciences, Inc. | Capped pyrazinoylguanidine sodium channel blockers |
| EA200970258A1 (ru) | 2006-09-07 | 2009-08-28 | Пэрион Сайенсиз, Инк. | Способ усиления гидратации слизистой оболочки и клиренса слизистой оболочки обработкой блокаторами натриевых каналов и осмолитами |
| WO2008124496A1 (en) | 2007-04-03 | 2008-10-16 | Parion Sciences, Inc. | Method of treating acid-sensing ion channel mediated pain, cough, and central nervous system disorders |
| US8288391B2 (en) | 2007-04-03 | 2012-10-16 | Parion Sciences, Inc. | Pyrazinoylguanidine compounds for use as taste modulators |
-
2007
- 2007-06-11 PL PL07784388T patent/PL2035004T3/pl unknown
- 2007-06-11 AU AU2007257781A patent/AU2007257781B2/en not_active Ceased
- 2007-06-11 ES ES07784388T patent/ES2392999T3/es active Active
- 2007-06-11 JP JP2009514564A patent/JP5254961B2/ja not_active Expired - Fee Related
- 2007-06-11 EP EP07784388A patent/EP2035004B1/en not_active Not-in-force
- 2007-06-11 DK DK07784388.6T patent/DK2035004T3/da active
- 2007-06-11 US US12/304,006 patent/US8163758B2/en not_active Expired - Fee Related
- 2007-06-11 CA CA002654244A patent/CA2654244A1/en not_active Abandoned
- 2007-06-11 PT PT07784388T patent/PT2035004E/pt unknown
- 2007-06-11 WO PCT/US2007/070861 patent/WO2007146869A1/en not_active Ceased
- 2007-06-11 SI SI200731054T patent/SI2035004T1/sl unknown
-
2008
- 2008-12-09 NO NO20085128A patent/NO20085128L/no not_active Application Discontinuation
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