JP2007521325A5 - - Google Patents
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- JP2007521325A5 JP2007521325A5 JP2006538402A JP2006538402A JP2007521325A5 JP 2007521325 A5 JP2007521325 A5 JP 2007521325A5 JP 2006538402 A JP2006538402 A JP 2006538402A JP 2006538402 A JP2006538402 A JP 2006538402A JP 2007521325 A5 JP2007521325 A5 JP 2007521325A5
- Authority
- JP
- Japan
- Prior art keywords
- aliphatic
- compound
- formula
- pharmaceutically acceptable
- independently selected
- 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.)
- Pending
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- 150000001875 compounds Chemical class 0.000 claims description 9
- 125000000623 heterocyclic group Chemical group 0.000 claims description 7
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 5
- 125000005842 heteroatoms Chemical group 0.000 claims description 4
- 229910052757 nitrogen Inorganic materials 0.000 claims description 3
- 229910052760 oxygen Inorganic materials 0.000 claims description 3
- 239000001301 oxygen Chemical group 0.000 claims description 3
- MYMOFIZGZYHOMD-UHFFFAOYSA-N oxygen Chemical group O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 claims description 3
- NINIDFKCEFEMDL-UHFFFAOYSA-N sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 3
- 229910052717 sulfur Chemical group 0.000 claims description 3
- 239000011593 sulfur Chemical group 0.000 claims description 3
- 125000003118 aryl group Chemical group 0.000 claims description 2
- 125000001931 aliphatic group Chemical group 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical group 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 229920000728 polyester Polymers 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000011780 sodium chloride Substances 0.000 claims 2
- -1 1,2-methylenedioxy Chemical group 0.000 claims 1
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 230000000240 adjuvant Effects 0.000 claims 1
- 125000002723 alicyclic group Chemical group 0.000 claims 1
- 230000001548 androgenic Effects 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 125000004435 hydrogen atoms Chemical group [H]* 0.000 claims 1
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 239000003981 vehicle Substances 0.000 claims 1
- 102000016913 Voltage-Gated Sodium Channels Human genes 0.000 description 1
- 108010053752 Voltage-Gated Sodium Channels Proteins 0.000 description 1
- 125000002619 bicyclic group Chemical group 0.000 description 1
- 125000004122 cyclic group Chemical group 0.000 description 1
- 230000000051 modifying Effects 0.000 description 1
- 125000002950 monocyclic group Chemical group 0.000 description 1
- OAICVXFJPJFONN-UHFFFAOYSA-N phosphorus Chemical compound [P] OAICVXFJPJFONN-UHFFFAOYSA-N 0.000 description 1
- 229910052698 phosphorus Inorganic materials 0.000 description 1
- 239000011574 phosphorus Substances 0.000 description 1
Description
本明細書中で用いられる場合、用語「ヘテロ脂肪族」、「複素環」、「ヘテロシクリル」、「ヘテロ脂環式」または「複素環式」は、1以上の環員が、独立して選択されるヘテロ原子である、非芳香族の、単環式、二環式または三環式の環系を意味する。いくつかの実施形態において、「複素環」基、「ヘテロシクリル」基、「ヘテロ脂環式」基または「複素環式」基は、1個以上の環員が酸素、硫黄、窒素、またはリンより独立して選択されるヘテロ原子である、3個〜14個の環員を有し、そして上記系における各環が3個〜7個の環員を含む。
表2に示されるような本発明の化合物は、25.0μM以下において電位依存性ナトリウムチャネルを調節することを見出した。
Claims (5)
- 下式(I)の化合物:
または薬学的に受容可能なその塩であって、ここで:
rは、0であり;
Zは、Nであり;
Yは、水素であり;Wは、下式Ia:
であり、式Iaにおいて
Aは、−T−NH−であって、ここで:
Tは、−CH 2 −CH 2 −であり;
Vは、−C(O)−であり;
Qは、−CH 2 O−であり;
mは、1であり;
環Eは、フェニルであり;そして
sは、0〜1であり;
R B は、Jより選択され、
Jは、ハロゲン、CN、NO2、CF3、OCF3、OH、SR6、S(O)R6、SO2R6、NH2、NHR6、N(R6)2、NR6R8、C(O)OH、C(O)OR6もしくはOR6であり;
R 6は、水素、または、R 7で置換されているC 1〜6 脂肪族基であり、ここで:
R7は、C3〜8脂環式、C6〜10アリール、窒素、酸素もしくは硫黄より独立して選択される1〜4個のヘテロ原子を有する5〜10員ヘテロアリール環または窒素、酸素もしくは硫黄より独立して選択される1〜4個のヘテロ原子を有する3〜10員ヘテロシクリル環であり、ここでR7は、必要に応じてR、1,2−メチレンジオキシ、1,2−エチレンジオキシ、もしくは(CH2)n−Gから独立して選択される、2つまでの置換基で置換され、ここで、nは、0もしくは1であり、Gは、ハロゲン、CN、NO2、CF3、OCF3、OH、S−脂肪族、S(O)−脂肪族、SO2−脂肪族、NH2、N−脂肪族、N(脂肪族)2、N(脂肪族)R8、COOH、C(O)O(−脂肪族、もしくはO−脂肪族から選択され;そして
R8は、アミノ保護基である、化合物。 - 請求項1に記載の化合物であって、ここで該化合物は、式IIa:
である化合物、またはその薬学的に受容可能な塩である、化合物。 - 請求項2に記載の化合物であって、ここで:
R Bは、OR6、N(R6)2 、ハロゲン、もしくはNO2である、
化合物。 - 以下:
からなる群より選択される、請求項1に記載の化合物。
- 請求項1〜4のいずれか一項で定義される式Iの化合物および薬学的に受容可能なキャリア、アジュバントまたはビヒクルを含む、薬学的組成物。
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US51508803P | 2003-10-28 | 2003-10-28 | |
PCT/US2004/036297 WO2005042497A2 (en) | 2003-10-28 | 2004-10-28 | Benzimidazoles useful as modulators of ion channels |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2007521325A JP2007521325A (ja) | 2007-08-02 |
JP2007521325A5 true JP2007521325A5 (ja) | 2011-07-28 |
Family
ID=34549374
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2006538402A Pending JP2007521325A (ja) | 2003-10-28 | 2004-10-28 | イオンチャネルのモジュレーターとして有用なベンズイミダゾール |
Country Status (13)
Country | Link |
---|---|
US (2) | US7309716B2 (ja) |
EP (1) | EP1678145A2 (ja) |
JP (1) | JP2007521325A (ja) |
KR (1) | KR20060115396A (ja) |
CN (1) | CN1902181A (ja) |
AU (1) | AU2004285053B2 (ja) |
CA (1) | CA2543918A1 (ja) |
IL (1) | IL175252A0 (ja) |
NO (1) | NO20062426L (ja) |
NZ (1) | NZ547109A (ja) |
RU (1) | RU2006118312A (ja) |
WO (1) | WO2005042497A2 (ja) |
ZA (1) | ZA200603864B (ja) |
Families Citing this family (38)
Publication number | Priority date | Publication date | Assignee | Title |
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WO2002036587A2 (en) | 2000-11-01 | 2002-05-10 | Cor Therapeutics, Inc. | Process for the production of 4-quinazolinylpiperazin-1-carboxylic acid phenylamides |
FR2880889B1 (fr) * | 2005-01-14 | 2007-04-06 | Merck Sante Soc Par Actions Si | Derives de l'acide 1h-indole-3-carboxylique, procedes pour leur preparation, compositions pharmaceutiques les contenant et applications en therapeutique |
GB0514018D0 (en) * | 2005-07-07 | 2005-08-17 | Ionix Pharmaceuticals Ltd | Chemical compounds |
KR20080033281A (ko) * | 2005-07-12 | 2008-04-16 | 바이엘 크롭사이언스 소시에떼아노님 | 새로운 벤조헤테로시클릴에틸벤즈아미드 유도체 |
AR057455A1 (es) * | 2005-07-22 | 2007-12-05 | Merck & Co Inc | Inhibidores de la transcriptasa reversa de vih y composicion farmaceutica |
CN101282929A (zh) * | 2005-08-15 | 2008-10-08 | Irm责任有限公司 | 用作tpo模拟物的化合物和组合物 |
US9018222B2 (en) | 2006-03-27 | 2015-04-28 | Wex Medical Limited | Use of sodium channel blockers for the treatment of neuropathic pain developing as a consequence of chemotherapy |
US7951829B2 (en) * | 2006-05-03 | 2011-05-31 | Janssen Pharmaceutica Nv | Benzimidazole modulators of VR1 |
HUE030052T4 (en) | 2007-06-29 | 2017-06-28 | Pfizer | Benzimidazole derivatives |
US8519137B2 (en) * | 2007-10-11 | 2013-08-27 | Vertex Pharmaceuticals Incorporated | Heteroaryl amides useful as inhibitors of voltage-gated sodium channels |
EP3018122B1 (en) | 2007-11-06 | 2018-10-10 | BioElectron Technology Corporation | 4-(p-quinonyl)-2-hydroxybutanamide derivatives for treatment of mitochondrial diseases |
RU2518073C2 (ru) * | 2008-12-26 | 2014-06-10 | ДАЙНИППОН СУМИТОМО ФАРМА Ко., ЛТД. | Новое бициклическое гетероциклическое соединение |
JPWO2010101164A1 (ja) * | 2009-03-05 | 2012-09-10 | 第一三共株式会社 | ピリジン誘導体 |
EP2582666B1 (en) | 2010-06-16 | 2014-08-13 | Purdue Pharma L.P. | Aryl substituted indoles and their use as blockers of sodium channels |
RU2443690C1 (ru) * | 2010-12-13 | 2012-02-27 | Российская Федерация, От Имени Которой Выступает Министерство Образования И Науки Российской Федерации | 2-(9-антрилметил)амино-1-[3-(диметиламино)пропил]бензимидазол, обладающий свойствами флуоресцентного хемосенсора на катионы h+ |
EP2681200A4 (en) * | 2011-03-03 | 2015-05-27 | Zalicus Pharmaceuticals Ltd | INHIBITORS OF BENZIMIDAZOLE TYPE OF SODIUM CHANNEL |
CA2849057C (en) * | 2011-09-19 | 2021-05-11 | Vitas Pharma Research Pvt Ltd | Heterocyclic compounds as inhibitors of fatty acid biosynthesis for bacterial infections |
US8859780B2 (en) | 2011-12-28 | 2014-10-14 | Allergan, Inc. | Benzimidazole derivatives as selective blockers of persistent sodium current |
US20130172342A1 (en) | 2011-12-28 | 2013-07-04 | Allergan, Inc. | Benzimidazole derivatives as selective blockers of persistent sodium current |
US9828348B2 (en) * | 2013-11-08 | 2017-11-28 | Purdue Pharma L.P. | Benzimidazole derivatives and use thereof |
US20150203812A1 (en) * | 2014-01-20 | 2015-07-23 | Francesco Tombola | Inhibitors of Voltage Gated Ion Channels |
WO2016029146A1 (en) * | 2014-08-22 | 2016-02-25 | University Of Washington | Specific inhibitors of methionyl-trna synthetase |
CN104926745A (zh) * | 2015-07-14 | 2015-09-23 | 佛山市赛维斯医药科技有限公司 | 含苯并异恶唑和末端卤代苄基类结构的化合物及其用途 |
CN104974103A (zh) * | 2015-07-14 | 2015-10-14 | 佛山市赛维斯医药科技有限公司 | 一类含苯并异恶唑和烷氧苯基类结构的化合物及其用途 |
CA2995881A1 (en) * | 2015-08-20 | 2017-02-23 | Boehringer Ingelheim International Gmbh | Novel annelated benzamides |
ES2818529T3 (es) * | 2015-09-11 | 2021-04-13 | Sumitomo Dainippon Pharma Co Ltd | Derivados de bencimidazol como inhibidores Nav 1.7 (subunidad alfa del canal de sodio, dependiente del voltaje, tipo IX (SCN9A)) para tratar el dolor, la disuria y la esclerosis múltiple |
GB201619694D0 (en) * | 2016-11-22 | 2017-01-04 | Entpr Therapeutics Ltd | Compounds |
WO2018235926A1 (ja) | 2017-06-23 | 2018-12-27 | 協和発酵キリン株式会社 | α、β不飽和アミド化合物 |
KR101938982B1 (ko) | 2017-07-17 | 2019-01-15 | 연세대학교 산학협력단 | 자가포식 조절제를 포함하는 대사성 질환 치료용 약학 조성물 |
KR102070882B1 (ko) * | 2017-10-17 | 2020-01-29 | 성균관대학교산학협력단 | Bietpc를 유효성분으로 포함하는 암 예방 또는 치료용 약학적 조성물 |
KR20210019119A (ko) | 2018-07-09 | 2021-02-19 | 리버 인스티튜트, 아이엔씨 | Nav1.8을 억제하기 위한 피리다진(PYRIDAZINE) 화합물 |
CA3130269A1 (en) * | 2019-02-19 | 2020-08-27 | The Regents Of The University Of California | Nurr1 receptor modulators |
MA53521B1 (fr) * | 2021-05-12 | 2023-03-31 | Univ Ibn Tofail | Nouveaux composés inhibiteurs de la protéase mpro et de la réplication du sars-cov2, leurs formulations et applications |
IL309232A (en) | 2021-06-14 | 2024-02-01 | Scorpion Therapeutics Inc | History of urea which can be used to treat cancer |
EP4408941A1 (en) * | 2021-09-30 | 2024-08-07 | Universidade Do Porto | Antifouling compound, method and uses thereof |
US12084453B2 (en) | 2021-12-10 | 2024-09-10 | Incyte Corporation | Bicyclic amines as CDK12 inhibitors |
US11478464B1 (en) | 2022-02-06 | 2022-10-25 | King Faisal University | Method for treating inflammation |
US11786535B1 (en) | 2023-02-22 | 2023-10-17 | King Faisal University | Methods of inhibiting cyclooxygenase |
Family Cites Families (9)
Publication number | Priority date | Publication date | Assignee | Title |
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NL280954A (ja) * | 1961-07-14 | |||
US4088768A (en) | 1975-05-06 | 1978-05-09 | Eli Lilly And Company | N-heterocyclic ureas as immune regulants |
DK40192D0 (da) * | 1992-03-26 | 1992-03-26 | Neurosearch As | Imidazolforbindelser, deres fremstilling og anvendelse |
AU4055300A (en) | 1999-04-02 | 2000-10-23 | Neurogen Corporation | Aryl and heteroaryl fused aminoalkyl-imidazole derivatives: selective modulators of Bradykinin B2 receptors |
EP1194410B1 (en) * | 1999-06-22 | 2006-01-18 | Neurosearch A/S | Benzimidazole derivatives and pharmaceutical compositions comprising these compounds |
US6316474B1 (en) | 1999-10-29 | 2001-11-13 | Merck & Co., Inc. | 2-benzyl and 2-heteroaryl benzimidazole NMDA/NR2B antagonists |
DE60104697T2 (de) | 2000-06-13 | 2005-08-04 | Eli Lilly And Co., Indianapolis | Sulfonamid-derivate |
US20050113283A1 (en) * | 2002-01-18 | 2005-05-26 | David Solow-Cordero | Methods of treating conditions associated with an EDG-4 receptor |
WO2003062392A2 (en) | 2002-01-18 | 2003-07-31 | Ceretek Llc | Methods of treating conditions associated with an edg receptor |
-
2004
- 2004-10-28 CN CNA2004800392479A patent/CN1902181A/zh active Pending
- 2004-10-28 US US10/977,609 patent/US7309716B2/en not_active Expired - Fee Related
- 2004-10-28 CA CA002543918A patent/CA2543918A1/en not_active Abandoned
- 2004-10-28 JP JP2006538402A patent/JP2007521325A/ja active Pending
- 2004-10-28 WO PCT/US2004/036297 patent/WO2005042497A2/en active Application Filing
- 2004-10-28 ZA ZA200603864A patent/ZA200603864B/en unknown
- 2004-10-28 AU AU2004285053A patent/AU2004285053B2/en not_active Ceased
- 2004-10-28 KR KR1020067010407A patent/KR20060115396A/ko not_active Application Discontinuation
- 2004-10-28 EP EP04796881A patent/EP1678145A2/en not_active Withdrawn
- 2004-10-28 RU RU2006118312/04A patent/RU2006118312A/ru not_active Application Discontinuation
- 2004-10-28 NZ NZ547109A patent/NZ547109A/en not_active IP Right Cessation
-
2006
- 2006-04-27 IL IL175252A patent/IL175252A0/en unknown
- 2006-05-29 NO NO20062426A patent/NO20062426L/no not_active Application Discontinuation
-
2007
- 2007-11-01 US US11/933,724 patent/US7705031B2/en not_active Expired - Lifetime
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