JP2007523175A5 - - Google Patents
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- Publication number
- JP2007523175A5 JP2007523175A5 JP2006554207A JP2006554207A JP2007523175A5 JP 2007523175 A5 JP2007523175 A5 JP 2007523175A5 JP 2006554207 A JP2006554207 A JP 2006554207A JP 2006554207 A JP2006554207 A JP 2006554207A JP 2007523175 A5 JP2007523175 A5 JP 2007523175A5
- Authority
- JP
- Japan
- Prior art keywords
- azabicyclo
- carboxylic acid
- amide
- ethyl
- indazole
- 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
Links
- 150000001875 compounds Chemical class 0.000 claims 54
- FHUPHXAYPNYFIU-UHFFFAOYSA-N 1-propan-2-ylindazole-3-carboxylic acid Chemical compound C1=CC=C2N(C(C)C)N=C(C(O)=O)C2=C1 FHUPHXAYPNYFIU-UHFFFAOYSA-N 0.000 claims 51
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 37
- -1 4-acetylpiperazin-1-yl Chemical group 0.000 claims 34
- 150000001408 amides Chemical class 0.000 claims 20
- 125000000217 alkyl group Chemical group 0.000 claims 17
- 125000003545 alkoxy group Chemical group 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 8
- 229910052739 hydrogen Inorganic materials 0.000 claims 7
- 239000001257 hydrogen Substances 0.000 claims 7
- 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 claims 6
- 239000012453 solvate Substances 0.000 claims 6
- 125000001475 halogen functional group Chemical group 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 125000006704 (C5-C6) cycloalkyl group Chemical group 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 150000002431 hydrogen Chemical class 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- 206010010774 Constipation Diseases 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 2
- HIOJBUUZILLMSD-UHFFFAOYSA-N 1-butylindazole-3-carboxylic acid Chemical compound C1=CC=C2N(CCCC)N=C(C(O)=O)C2=C1 HIOJBUUZILLMSD-UHFFFAOYSA-N 0.000 claims 1
- OVTXQAXXRCDBCP-UHFFFAOYSA-N 1-cyclobutylindazole-3-carboxylic acid Chemical compound C12=CC=CC=C2C(C(=O)O)=NN1C1CCC1 OVTXQAXXRCDBCP-UHFFFAOYSA-N 0.000 claims 1
- YOZGRUDRUTYFDN-UHFFFAOYSA-N 1-cyclopentylindazole-3-carboxylic acid Chemical compound C12=CC=CC=C2C(C(=O)O)=NN1C1CCCC1 YOZGRUDRUTYFDN-UHFFFAOYSA-N 0.000 claims 1
- SRLYWTDJCHALPO-UHFFFAOYSA-N 1-propylindazole-3-carboxylic acid Chemical compound C1=CC=C2N(CCC)N=C(C(O)=O)C2=C1 SRLYWTDJCHALPO-UHFFFAOYSA-N 0.000 claims 1
- IEIAQSWMJMZELU-UHFFFAOYSA-N 5-fluoro-1-propan-2-ylindazole-3-carboxylic acid Chemical compound FC1=CC=C2N(C(C)C)N=C(C(O)=O)C2=C1 IEIAQSWMJMZELU-UHFFFAOYSA-N 0.000 claims 1
- 206010051153 Diabetic gastroparesis Diseases 0.000 claims 1
- 206010021518 Impaired gastric emptying Diseases 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- VZTDIZULWFCMLS-UHFFFAOYSA-N ammonium formate Chemical compound [NH4+].[O-]C=O VZTDIZULWFCMLS-UHFFFAOYSA-N 0.000 claims 1
- 239000003054 catalyst Substances 0.000 claims 1
- 239000003638 chemical reducing agent Substances 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 230000008878 coupling Effects 0.000 claims 1
- 238000010168 coupling process Methods 0.000 claims 1
- 238000005859 coupling reaction Methods 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000006549 dyspepsia Diseases 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 208000013617 idiopathic gastroparesis Diseases 0.000 claims 1
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- NZJKEPNCNBWESN-UHFFFAOYSA-N tert-butyl 3-amino-8-azabicyclo[3.2.1]octane-8-carboxylate Chemical compound C1C(N)CC2CCC1N2C(=O)OC(C)(C)C NZJKEPNCNBWESN-UHFFFAOYSA-N 0.000 claims 1
- MENILFUADYEXNU-UHFFFAOYSA-N tert-butyl 3-oxo-8-azabicyclo[3.2.1]octane-8-carboxylate Chemical compound C1C(=O)CC2CCC1N2C(=O)OC(C)(C)C MENILFUADYEXNU-UHFFFAOYSA-N 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
- 229910052723 transition metal Inorganic materials 0.000 claims 1
- 150000003624 transition metals Chemical class 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US54570204P | 2004-02-18 | 2004-02-18 | |
| PCT/US2005/005070 WO2005080389A1 (en) | 2004-02-18 | 2005-02-17 | Indazole-carboxamide compounds as 5-ht4 receptor agonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2007523175A JP2007523175A (ja) | 2007-08-16 |
| JP2007523175A5 true JP2007523175A5 (https=) | 2008-03-13 |
Family
ID=34886184
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006554207A Pending JP2007523175A (ja) | 2004-02-18 | 2005-02-17 | 5−ht4レセプターアゴニストとしてのインダゾール−カルボキシアミド化合物 |
Country Status (16)
| Country | Link |
|---|---|
| US (3) | US7351704B2 (https=) |
| EP (1) | EP1718643A1 (https=) |
| JP (1) | JP2007523175A (https=) |
| KR (1) | KR20060132727A (https=) |
| CN (1) | CN1922175A (https=) |
| AR (1) | AR047681A1 (https=) |
| AU (1) | AU2005214368A1 (https=) |
| BR (1) | BRPI0507791A (https=) |
| CA (1) | CA2553696A1 (https=) |
| IL (1) | IL177059A0 (https=) |
| MA (1) | MA28435B1 (https=) |
| NO (1) | NO20064156L (https=) |
| RU (1) | RU2006133320A (https=) |
| TW (1) | TW200533348A (https=) |
| WO (1) | WO2005080389A1 (https=) |
| ZA (1) | ZA200606479B (https=) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW200533348A (en) * | 2004-02-18 | 2005-10-16 | Theravance Inc | Indazole-carboxamide compounds as 5-ht4 receptor agonists |
| TWI351282B (en) * | 2004-04-07 | 2011-11-01 | Theravance Inc | Quinolinone-carboxamide compounds as 5-ht4 recepto |
| US8309575B2 (en) | 2004-04-07 | 2012-11-13 | Theravance, Inc. | Quinolinone-carboxamide compounds as 5-HT4 receptor agonists |
| US7728006B2 (en) * | 2004-04-07 | 2010-06-01 | Theravance, Inc. | Quinolinone-carboxamide compounds as 5-HT4 receptor agonists |
| ATE441646T1 (de) * | 2004-11-05 | 2009-09-15 | Theravance Inc | 5-ht4-rezeptoragonistenverbindungen |
| EP1807423B1 (en) * | 2004-11-05 | 2009-05-20 | Theravance, Inc. | Quinolinone-carboxamide compounds |
| ATE469897T1 (de) * | 2004-12-22 | 2010-06-15 | Theravance Inc | Indazolcarbonsäureamidverbindungen |
| WO2006088988A1 (en) * | 2005-02-17 | 2006-08-24 | Theravance, Inc. | Crystalline form of an indazole-carboxamide compound |
| NZ560828A (en) * | 2005-03-02 | 2011-01-28 | Theravance Inc | Quinolinone compounds as 5-HT4 receptor agonists |
| US7317022B2 (en) * | 2005-06-07 | 2008-01-08 | Theravance, Inc. | Benzoimidazolone-carboxamide compounds as 5-HT4 receptors agonists |
| WO2007102883A2 (en) * | 2005-10-25 | 2007-09-13 | Smithkline Beecham Corporation | Chemical compounds |
| MY143574A (en) * | 2005-11-22 | 2011-05-31 | Theravance Inc | Carbamate compounds as 5-ht4 receptor agonists |
| GB0525068D0 (en) | 2005-12-08 | 2006-01-18 | Novartis Ag | Organic compounds |
| CA2637214C (en) * | 2006-02-16 | 2014-04-22 | Theravance, Inc. | Process for preparing 8-azabicylo[3.2.1]octan-3-one intermediates to 5-ht4 receptor agonist compounds |
| KR100812499B1 (ko) * | 2006-10-16 | 2008-03-11 | 이도훈 | 항경련제 |
| EP2121679B1 (de) * | 2007-02-23 | 2015-04-15 | K.H.S. Pharma Holding Gmbh | Verfahren zur herstellung von azoniaspironortropinestern |
| KR20100124262A (ko) * | 2008-02-13 | 2010-11-26 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 비시클로아민 유도체 |
| US8349852B2 (en) | 2009-01-13 | 2013-01-08 | Novartis Ag | Quinazolinone derivatives useful as vanilloid antagonists |
| JP2013518085A (ja) | 2010-02-01 | 2013-05-20 | ノバルティス アーゲー | CRF−1受容体アンタゴニストとしてのピラゾロ[5,1b]オキサゾール誘導体 |
| AR080056A1 (es) | 2010-02-01 | 2012-03-07 | Novartis Ag | Derivados de ciclohexil-amida como antagonistas de los receptores de crf |
| JP5748777B2 (ja) | 2010-02-02 | 2015-07-15 | ノバルティス アーゲー | Crf受容体アンタゴニストとしてのシクロヘキシルアミド誘導体 |
| JP6023926B2 (ja) * | 2010-02-12 | 2016-11-09 | 株式会社AskAt | 認知症治療のための5−ht4受容体アゴニスト |
| UY34094A (es) | 2011-05-27 | 2013-01-03 | Novartis Ag | Derivados de la piperidina 3-espirocíclica como agonistas de receptores de la ghrelina |
| CN103748087A (zh) * | 2011-06-07 | 2014-04-23 | 大日本住友制药株式会社 | 吲唑和吡咯并吡啶衍生物和其药学用途 |
| CA2867043A1 (en) | 2012-05-03 | 2013-11-07 | Novartis Ag | L-malate salt of 2,7-diaza-spiro[4.5]dec-7-yle derivatives and crystalline forms thereof as ghrelin receptor agonists |
| JP2014133739A (ja) * | 2012-12-12 | 2014-07-24 | Dainippon Sumitomo Pharma Co Ltd | インダゾール誘導体またはピロロピリジン誘導体からなる医薬 |
| CA2957498C (en) * | 2014-08-16 | 2019-02-12 | Suven Life Sciences Limited | Process for large scale production of 1-isopropyl-3-{5-[1-(3-methoxypropyl) piperidin-4-yl]-[1,3,4]oxadiazol-2-yl}-1h-indazole oxalate |
| WO2021046789A1 (zh) * | 2019-09-12 | 2021-03-18 | 广东东阳光药业有限公司 | 吲唑-甲酰胺衍生物及其用途 |
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| JPH045289A (ja) | 1990-04-24 | 1992-01-09 | Hokuriku Seiyaku Co Ltd | アミド化合物 |
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| JP3829880B2 (ja) | 1994-12-27 | 2006-10-04 | 大正製薬株式会社 | 化学中間体 |
| IT1275903B1 (it) * | 1995-03-14 | 1997-10-24 | Boehringer Ingelheim Italia | Esteri e ammidi della 1,4-piperidina disostituita |
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| ES2109190B1 (es) | 1996-03-22 | 1998-07-01 | Univ Madrid Complutense | Nuevos derivados de bencimidazol con afinidad por los receptores serotoninergicos 5-ht /5-ht |
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| FR2769915B1 (fr) | 1997-10-21 | 2000-10-13 | Synthelabo | Derives d'indazole tricycliques, leur preparation et leur application en therapeutique |
| IT1298271B1 (it) | 1998-02-18 | 1999-12-20 | Boehringer Ingelheim Italia | Esteri ed ammidi dell'acido 2-oxo-2,3-diidro-benzimidazol-1- carbossilico |
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| PE20001420A1 (es) | 1998-12-23 | 2000-12-18 | Pfizer | Moduladores de ccr5 |
| FR2792318B1 (fr) | 1999-04-16 | 2001-06-15 | Synthelabo | Derives d'indazole, leur preparation et leur application en therapeutique |
| WO2000064441A2 (en) * | 1999-04-28 | 2000-11-02 | Respiratorius Ab | Compound for use as a medicament for treatment of disorders involving bronchocontraction |
| ES2154605B1 (es) | 1999-09-14 | 2001-11-16 | Univ Madrid Complutense | Nuevos derivados mixtos de bencimidazol-arilpiperazina con afinidad por los receptores serotoninergicos 5-ht1a y 5-ht3 |
| IT1313625B1 (it) * | 1999-09-22 | 2002-09-09 | Boehringer Ingelheim Italia | Derivati benzimidazolonici aventi affinita' mista per i recettori diserotonina e dopamina. |
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| AU2002212888A1 (en) | 2000-11-01 | 2002-05-15 | Respiratorius Ab | Composition comprising: serotonin receptor antagonists (5ht-2, 5ht-3) and agonist (5ht-4) |
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| DOP2003000703A (es) * | 2002-09-20 | 2004-03-31 | Pfizer | Compuestos de imidazopiradina como agonistas del receptor 5-ht4 |
| JP2006502180A (ja) | 2002-09-20 | 2006-01-19 | ファイザー株式会社 | 5−ht4レセプターモジュレーターとしてのn−置換されたピペリジニル−イミダゾピリジン化合物 |
| BRPI0409592A (pt) * | 2003-04-21 | 2006-05-02 | Pfizer | compostos imidazopiridina tendo atividade agonìstica do receptor 5-ht4 e atividade antagonìstica do receptor 5-ht3 |
| WO2005000837A1 (en) | 2003-06-19 | 2005-01-06 | Janssen Pharmaceutica N.V. | Aminosulfonyl substituted 4-(aminomethyl)-piperidine benzamides as 5ht4-antagonists |
| JO2478B1 (en) | 2003-06-19 | 2009-01-20 | جانسين فارماسوتيكا ان. في. | (Aminomethyl) -biperidine benzamides as 5 HT4 antagonists |
| UA86204C2 (uk) | 2003-09-03 | 2009-04-10 | Пфайзер Инк. | Сполуки бензімідазолону, які мають 5-нт4 рецепторну агоністичну активність |
| DE602004026095D1 (de) | 2003-11-24 | 2010-04-29 | Pfizer | Chinoloncarbonsäureverbindungen mit 5-ht4-rezeptoragonistischer wirkung |
| DE602005005167T2 (de) | 2004-01-29 | 2009-04-30 | Pfizer Inc. | 1-isopropyl-2-oxo-1,2-dihydropyridin-3-carbonsäureamidderivate mit agonistischer wirkung am 5-ht4-rezeptor |
| TW200533348A (en) * | 2004-02-18 | 2005-10-16 | Theravance Inc | Indazole-carboxamide compounds as 5-ht4 receptor agonists |
| ATE441646T1 (de) * | 2004-11-05 | 2009-09-15 | Theravance Inc | 5-ht4-rezeptoragonistenverbindungen |
-
2005
- 2005-02-15 TW TW094104343A patent/TW200533348A/zh unknown
- 2005-02-17 EP EP05723216A patent/EP1718643A1/en not_active Withdrawn
- 2005-02-17 WO PCT/US2005/005070 patent/WO2005080389A1/en not_active Ceased
- 2005-02-17 BR BRPI0507791-5A patent/BRPI0507791A/pt not_active IP Right Cessation
- 2005-02-17 AU AU2005214368A patent/AU2005214368A1/en not_active Abandoned
- 2005-02-17 CA CA002553696A patent/CA2553696A1/en not_active Abandoned
- 2005-02-17 AR ARP050100560A patent/AR047681A1/es unknown
- 2005-02-17 CN CNA200580005307XA patent/CN1922175A/zh active Pending
- 2005-02-17 KR KR1020067019088A patent/KR20060132727A/ko not_active Withdrawn
- 2005-02-17 RU RU2006133320/04A patent/RU2006133320A/ru not_active Application Discontinuation
- 2005-02-17 JP JP2006554207A patent/JP2007523175A/ja active Pending
- 2005-02-17 US US11/060,195 patent/US7351704B2/en active Active
-
2006
- 2006-07-25 IL IL177059A patent/IL177059A0/en unknown
- 2006-08-03 ZA ZA200606479A patent/ZA200606479B/en unknown
- 2006-08-18 MA MA29276A patent/MA28435B1/fr unknown
- 2006-09-14 NO NO20064156A patent/NO20064156L/no not_active Application Discontinuation
-
2008
- 2008-02-04 US US12/012,579 patent/US7674908B2/en not_active Expired - Lifetime
-
2010
- 2010-01-19 US US12/689,763 patent/US8044045B2/en not_active Expired - Fee Related
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