JP2006508935A5 - - Google Patents
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- JP2006508935A5 JP2006508935A5 JP2004544241A JP2004544241A JP2006508935A5 JP 2006508935 A5 JP2006508935 A5 JP 2006508935A5 JP 2004544241 A JP2004544241 A JP 2004544241A JP 2004544241 A JP2004544241 A JP 2004544241A JP 2006508935 A5 JP2006508935 A5 JP 2006508935A5
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- JP
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- Prior art keywords
- alkyl
- substituted
- optionally
- compound
- formula
- 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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- 150000001875 compounds Chemical class 0.000 claims 20
- 125000000217 alkyl group Chemical group 0.000 claims 12
- 229910052736 halogen Inorganic materials 0.000 claims 7
- 150000002367 halogens Chemical class 0.000 claims 7
- -1 methoxy, butoxy Chemical group 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 5
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 239000001257 hydrogen Substances 0.000 claims 4
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 4
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 4
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 3
- 208000012902 Nervous system disease Diseases 0.000 claims 3
- 208000025966 Neurological disease Diseases 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 229910052731 fluorine Inorganic materials 0.000 claims 3
- 239000011737 fluorine Substances 0.000 claims 3
- 208000027866 inflammatory disease Diseases 0.000 claims 3
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 3
- 230000000926 neurological effect Effects 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 210000002345 respiratory system Anatomy 0.000 claims 3
- 125000001424 substituent group Chemical group 0.000 claims 3
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 2
- 125000002877 alkyl aryl group Chemical group 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000003725 azepanyl group Chemical group 0.000 claims 2
- 229910052801 chlorine Inorganic materials 0.000 claims 2
- 239000000460 chlorine Substances 0.000 claims 2
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- YFJCXXMXXDBLTO-UHFFFAOYSA-N (4-methylsulfonylphenyl)-[4-[4-(1-propan-2-ylpiperidin-4-yl)oxyphenyl]piperazin-1-yl]methanone Chemical compound C1CN(C(C)C)CCC1OC1=CC=C(N2CCN(CC2)C(=O)C=2C=CC(=CC=2)S(C)(=O)=O)C=C1 YFJCXXMXXDBLTO-UHFFFAOYSA-N 0.000 claims 1
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 claims 1
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims 1
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 1
- CSBKEGBTNFFHSO-UHFFFAOYSA-N 3-[4-[4-(3-piperidin-1-ylpropoxy)phenyl]piperazine-1-carbonyl]benzonitrile Chemical compound N1(CCCCC1)CCCOC1=CC=C(C=C1)N1CCN(CC1)C(=O)C=1C=C(C#N)C=CC=1 CSBKEGBTNFFHSO-UHFFFAOYSA-N 0.000 claims 1
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 1
- 229910052794 bromium Inorganic materials 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 229920001577 copolymer Chemical group 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000003754 ethoxycarbonyl group Chemical group C(=O)(OCC)* 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 229910052757 nitrogen Chemical group 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 150000003053 piperidines Chemical class 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000004434 sulfur atom Chemical group 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- NQRYJNQNLNOLGT-UHFFFAOYSA-N tetrahydropyridine hydrochloride Natural products C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 125000004568 thiomorpholinyl group Chemical group 0.000 claims 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0224084.4A GB0224084D0 (en) | 2002-10-16 | 2002-10-16 | Novel compounds |
| PCT/EP2003/011423 WO2004035556A1 (en) | 2002-10-16 | 2003-10-14 | Substituted piperazines, (1,4) diaszepines, and 2,5-diazabicyclo (2.2.1) heptanes as histamine h1 and/or h3 antagonists or histamine h3 reverse antagonists |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006231163A Division JP2007016041A (ja) | 2002-10-16 | 2006-08-28 | ヒスタミンｈ１および／もしくはｈ３アンタゴニストまたはｈ３逆アンタゴニストとしての置換ピペラジン、（１，４）ジアゼピン、および２，５−ジアザビシクロ（２．２．１）へプタン。 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2006508935A JP2006508935A (ja) | 2006-03-16 |
| JP2006508935A5 true JP2006508935A5 (enExample) | 2006-10-19 |
Family
ID=9946029
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2004544241A Pending JP2006508935A (ja) | 2002-10-16 | 2003-10-14 | ヒスタミンｈ１および／もしくはｈ３アンタゴニストまたはｈ３逆アンタゴニストとしての置換ピペラジン、（１，４）ジアゼピン、および２，５−ジアザビシクロ（２．２．１）へプタン。 |
| JP2006231163A Pending JP2007016041A (ja) | 2002-10-16 | 2006-08-28 | ヒスタミンｈ１および／もしくはｈ３アンタゴニストまたはｈ３逆アンタゴニストとしての置換ピペラジン、（１，４）ジアゼピン、および２，５−ジアザビシクロ（２．２．１）へプタン。 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006231163A Pending JP2007016041A (ja) | 2002-10-16 | 2006-08-28 | ヒスタミンｈ１および／もしくはｈ３アンタゴニストまたはｈ３逆アンタゴニストとしての置換ピペラジン、（１，４）ジアゼピン、および２，５−ジアザビシクロ（２．２．１）へプタン。 |
Country Status (18)
| Country | Link |
|---|---|
| US (2) | US7615550B2 (enExample) |
| EP (1) | EP1567511A1 (enExample) |
| JP (2) | JP2006508935A (enExample) |
| KR (1) | KR20050049553A (enExample) |
| CN (2) | CN101070309A (enExample) |
| AU (1) | AU2003280380A1 (enExample) |
| BR (1) | BR0315283A (enExample) |
| CA (1) | CA2502249A1 (enExample) |
| GB (1) | GB0224084D0 (enExample) |
| IS (1) | IS7782A (enExample) |
| MA (1) | MA27482A1 (enExample) |
| MX (1) | MXPA05004078A (enExample) |
| NO (1) | NO20051689L (enExample) |
| NZ (2) | NZ539446A (enExample) |
| PL (1) | PL376477A1 (enExample) |
| RU (1) | RU2328494C2 (enExample) |
| WO (1) | WO2004035556A1 (enExample) |
| ZA (2) | ZA200502873B (enExample) |
Families Citing this family (108)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7842693B2 (en) | 2002-06-12 | 2010-11-30 | Chemocentryx, Inc. | Substituted piperazines |
| US7589199B2 (en) | 2002-06-12 | 2009-09-15 | Chemocentryx, Inc. | Substituted piperazines |
| US20050256130A1 (en) * | 2002-06-12 | 2005-11-17 | Chemocentryx, Inc. | Substituted piperazines |
| GB0224084D0 (en) * | 2002-10-16 | 2002-11-27 | Glaxo Group Ltd | Novel compounds |
| GB0224557D0 (en) | 2002-10-22 | 2002-11-27 | Glaxo Group Ltd | Novel compounds |
| US20070293216A1 (en) * | 2003-02-14 | 2007-12-20 | Roamware Inc. | Method and system for providing PLN service to inbound roamers in a VPMN using a standalone approach when no roaming relationship exists between HPMN and VPMN |
| EP1611902A4 (en) * | 2003-04-03 | 2006-04-12 | Kyowa Hakko Kogyo Kk | MEANS FOR THE PREVENTION AND / OR TREATMENT OF NEUROPATHIC PAIN |
| US20060293298A1 (en) * | 2003-04-10 | 2006-12-28 | Bamford Mark J | Compounds |
| GB0316915D0 (en) | 2003-07-18 | 2003-08-20 | Glaxo Group Ltd | Compounds |
| GB0324159D0 (en) * | 2003-10-15 | 2003-11-19 | Glaxo Group Ltd | Novel compounds |
| CN1972914A (zh) * | 2004-03-31 | 2007-05-30 | 詹森药业有限公司 | 作为组胺h3受体配合体的非咪唑杂环化合物 |
| WO2005110982A2 (en) | 2004-04-07 | 2005-11-24 | Neurogen Corporation | Substituted 1-benzyl-4-substituted piperazine analogues |
| EP1755605A2 (en) * | 2004-04-15 | 2007-02-28 | Samaritan Pharmaceuticals, Inc. | Use of (4-alkylpiperazinyl)(phenyl) methanones in the treatment of alzheimer's disease |
| JP2007538011A (ja) * | 2004-05-07 | 2007-12-27 | メモリー・ファーマシューティカルズ・コーポレイション | １ｈ−インダゾール、ベンゾチアゾール、１，２−ベンゾイソキサゾール、１，２−ベンゾイソチアゾール、およびクロモン、ならびにそれらの調製および使用 |
| JPWO2006059778A1 (ja) * | 2004-12-01 | 2008-06-05 | 萬有製薬株式会社 | 置換ピリドン誘導体 |
| EP1851201A1 (en) * | 2005-02-24 | 2007-11-07 | Glaxo Group Limited | 1-{4-[(1-cyclobutyl-4-piperidinyl)oxy]phenyl}-4-{[4-(methylsulfonyl)phenyl]carbonyl}piperazine as histamine h3 antagonist |
| ES2335305T3 (es) * | 2005-03-17 | 2010-03-24 | Eli Lilly And Company | Derivados de pirrolidina como antagonistas del receptor h3 de histamina. |
| EP1717235A3 (en) * | 2005-04-29 | 2007-02-28 | Bioprojet | Phenoxypropylpiperidines and -pyrrolidines and their use as histamine H3-receptor ligands |
| US8138206B2 (en) * | 2005-05-30 | 2012-03-20 | Msd. K.K. | Piperidine derivative |
| CN101228127B (zh) * | 2005-05-30 | 2012-05-16 | Msdk.K.公司 | 哌啶衍生物 |
| GB0514811D0 (en) * | 2005-07-19 | 2005-08-24 | Glaxo Group Ltd | Compounds |
| GB0514812D0 (en) * | 2005-07-19 | 2005-08-24 | Glaxo Group Ltd | Compounds |
| GB0521563D0 (en) | 2005-10-21 | 2005-11-30 | Glaxo Group Ltd | Novel compounds |
| AU2006308167A1 (en) * | 2005-10-27 | 2007-05-03 | Ucb Pharma, S.A. | Compounds comprising a lactam or a lactam derivative moiety, processes for making them, and their uses |
| RU2417226C2 (ru) * | 2005-11-18 | 2011-04-27 | Ф.Хоффманн-Ля Рош Аг | Производные азаиндол-2-карбоксамида |
| WO2007062999A2 (en) * | 2005-11-30 | 2007-06-07 | F. Hoffmann-La Roche Ag | 1,5-substituted indol-2-yl amide derivatives |
| EP1968967B1 (en) * | 2005-11-30 | 2011-04-27 | F. Hoffmann-La Roche AG | 1,1-dioxo-thiomorpholinyl indolyl methanone derivatives for use as h3 modulators |
| JP2009519293A (ja) * | 2005-12-16 | 2009-05-14 | エフ．ホフマン−ラ ロシュ アーゲー | Ｈ３レセプター調節剤としてのピロロ［２，３−ｂ］ピリジン誘導体 |
| PE20071068A1 (es) * | 2005-12-20 | 2007-12-13 | Glaxo Group Ltd | Acido 3-(4-{[4-(4-{[3-(3,3-dimetil-1-piperidinil)propil]oxi}fenil)-1-piperidinil]carbonil}-1-naftalenil)propanoico o propenoico, sales de los mismos, como antagonistas de los receptores h1 y h3 |
| US20090105225A1 (en) * | 2006-04-20 | 2009-04-23 | Glaxo Group Limited | 2-Substituted 4-Benzylphthalazinone Derivatives as Histamine H1 and H3 Antagonists |
| KR20090003349A (ko) | 2006-04-20 | 2009-01-09 | 글락소 그룹 리미티드 | 화합물 |
| GB0609897D0 (en) * | 2006-05-18 | 2006-06-28 | Glaxo Group Ltd | Compounds |
| KR101372941B1 (ko) * | 2006-05-30 | 2014-03-14 | 얀센 파마슈티카 엔.브이. | 히스타민 ｈ３ 수용체 조절제로서의 치환된 피리딜 아미드 화합물 |
| GB0611587D0 (en) | 2006-06-12 | 2006-07-19 | Glaxo Group Ltd | Novel compounds |
| US9108948B2 (en) | 2006-06-23 | 2015-08-18 | Abbvie Inc. | Cyclopropyl amine derivatives |
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| US20080045507A1 (en) * | 2006-06-29 | 2008-02-21 | Allison Brett D | Substituted benzamide modulators of the histamine h3 receptor |
| KR101007469B1 (ko) | 2006-12-22 | 2011-01-12 | 성균관대학교산학협력단 | 사스 코로나 바이러스의 ｒｎａ 유사매듭구조에 결합하여 리보솜 틀 이동을 억제하는 호모피페라진계 화합물 |
| PE20081889A1 (es) | 2007-03-23 | 2009-03-05 | Smithkline Beecham Corp | Indol carboxamidas como inhibidores de ikk2 |
| US20090170869A1 (en) | 2007-09-06 | 2009-07-02 | Desmond John Best | Piperazine derivative having affinity for the histamine h3 receptor |
| CA2697551C (en) | 2007-09-20 | 2013-03-12 | Irm Llc | Piperidine derivatives as modulators of gpr119 activity |
| BRPI0820481A2 (pt) | 2007-11-20 | 2015-06-16 | Janssen Pharmaceutica Nv | Composotos cicloalquilóxi e heterocicloalquilóxi piridina como moduladores do receptor de h3 de histamina |
| JP2011516557A (ja) * | 2008-04-07 | 2011-05-26 | アイアールエム・リミテッド・ライアビリティ・カンパニー | Ｇｐｒ１１９活性のモジュレーターとしての化合物および組成物 |
| CN102137858B (zh) | 2008-05-23 | 2014-07-23 | 潘米拉制药有限责任公司 | 5-脂氧合酶-活化蛋白抑制剂 |
| JP5502858B2 (ja) | 2008-06-05 | 2014-05-28 | グラクソ グループ リミテッド | Ｐｉ３キナーゼの阻害剤として有用な４−カルボキサミドインダゾール誘導体 |
| WO2010094643A1 (en) | 2009-02-17 | 2010-08-26 | Glaxo Group Limited | Quinoline derivatives and their uses for rhinitis and urticaria |
| EP2406255B1 (en) | 2009-03-09 | 2015-04-29 | Glaxo Group Limited | 4-oxadiazol-2-yl-indazoles as inhibitors of pi3 kinases |
| WO2010102968A1 (en) | 2009-03-10 | 2010-09-16 | Glaxo Group Limited | Indole derivatives as ikk2 inhibitors |
| WO2010106016A1 (en) | 2009-03-17 | 2010-09-23 | Glaxo Group Limited | Pyrimidine derivatives used as itk inhibitors |
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| JP5916730B2 (ja) * | 2010-09-06 | 2016-05-11 | グアンジョウ インスティテュート オブ バイオメディスン アンド ヘルス，チャイニーズ アカデミー オブ サイエンスィズ | アミド化合物 |
| RS54286B1 (sr) | 2010-09-08 | 2016-02-29 | Glaxosmithkline Intellectual Property Development Limited | Polimorfi i soli n-[5-[4-(5-{[(2r,6s)-2,6-dimetil-4-morfolinil]metil}-1,3-oksazol-2-il)-1h-indazol-6-il]-2(metiloksi)-3-piridinil]-metansulfonamida |
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-
2002
- 2002-10-16 GB GBGB0224084.4A patent/GB0224084D0/en not_active Ceased
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2003
- 2003-10-14 CA CA002502249A patent/CA2502249A1/en not_active Abandoned
- 2003-10-14 JP JP2004544241A patent/JP2006508935A/ja active Pending
- 2003-10-14 BR BR0315283-9A patent/BR0315283A/pt not_active IP Right Cessation
- 2003-10-14 NZ NZ539446A patent/NZ539446A/en unknown
- 2003-10-14 RU RU2005110061/04A patent/RU2328494C2/ru not_active IP Right Cessation
- 2003-10-14 NZ NZ549963A patent/NZ549963A/en unknown
- 2003-10-14 MX MXPA05004078A patent/MXPA05004078A/es unknown
- 2003-10-14 PL PL03376477A patent/PL376477A1/xx unknown
- 2003-10-14 CN CNA2006101086109A patent/CN101070309A/zh active Pending
- 2003-10-14 US US10/531,758 patent/US7615550B2/en not_active Expired - Fee Related
- 2003-10-14 KR KR1020057006621A patent/KR20050049553A/ko not_active Withdrawn
- 2003-10-14 AU AU2003280380A patent/AU2003280380A1/en not_active Abandoned
- 2003-10-14 CN CNB2003801060141A patent/CN100400523C/zh not_active Expired - Fee Related
- 2003-10-14 WO PCT/EP2003/011423 patent/WO2004035556A1/en not_active Ceased
- 2003-10-14 EP EP03772221A patent/EP1567511A1/en not_active Withdrawn
-
2005
- 2005-03-31 IS IS7782A patent/IS7782A/is unknown
- 2005-04-05 NO NO20051689A patent/NO20051689L/no not_active Application Discontinuation
- 2005-04-08 ZA ZA200502873A patent/ZA200502873B/en unknown
- 2005-04-29 MA MA28246A patent/MA27482A1/fr unknown
-
2006
- 2006-05-05 ZA ZA200603604A patent/ZA200603604B/en unknown
- 2006-08-28 JP JP2006231163A patent/JP2007016041A/ja active Pending
-
2009
- 2009-09-18 US US12/562,285 patent/US20100075953A1/en not_active Abandoned
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