JP2009533343A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2009533343A5 JP2009533343A5 JP2009504253A JP2009504253A JP2009533343A5 JP 2009533343 A5 JP2009533343 A5 JP 2009533343A5 JP 2009504253 A JP2009504253 A JP 2009504253A JP 2009504253 A JP2009504253 A JP 2009504253A JP 2009533343 A5 JP2009533343 A5 JP 2009533343A5
- Authority
- JP
- Japan
- Prior art keywords
- methanone
- indol
- pyrrolidin
- methylamino
- methyl
- 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 25
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 14
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 12
- 150000003839 salts Chemical class 0.000 claims 8
- NTYJJOPFIAHURM-UHFFFAOYSA-N Histamine Chemical compound NCCC1=CN=CN1 NTYJJOPFIAHURM-UHFFFAOYSA-N 0.000 claims 4
- ZKQDDNKLQNOPFP-UHFFFAOYSA-N (3-aminopyrrolidin-1-yl)-(5-chloro-1h-indol-2-yl)methanone Chemical compound C1C(N)CCN1C(=O)C1=CC2=CC(Cl)=CC=C2N1 ZKQDDNKLQNOPFP-UHFFFAOYSA-N 0.000 claims 3
- IVMSTKHJTVCVCT-SECBINFHSA-N (4,6-difluoro-1h-indol-2-yl)-[(3r)-3-(methylamino)pyrrolidin-1-yl]methanone Chemical compound C1[C@H](NC)CCN1C(=O)C1=CC2=C(F)C=C(F)C=C2N1 IVMSTKHJTVCVCT-SECBINFHSA-N 0.000 claims 3
- IVMSTKHJTVCVCT-VIFPVBQESA-N (4,6-difluoro-1h-indol-2-yl)-[(3s)-3-(methylamino)pyrrolidin-1-yl]methanone Chemical compound C1[C@@H](NC)CCN1C(=O)C1=CC2=C(F)C=C(F)C=C2N1 IVMSTKHJTVCVCT-VIFPVBQESA-N 0.000 claims 3
- VCVCGLWPFWUIPZ-LLVKDONJSA-N (5-chloro-1h-indol-2-yl)-[(3r)-3-(methylamino)pyrrolidin-1-yl]methanone Chemical compound C1[C@H](NC)CCN1C(=O)C1=CC2=CC(Cl)=CC=C2N1 VCVCGLWPFWUIPZ-LLVKDONJSA-N 0.000 claims 3
- VCVCGLWPFWUIPZ-NSHDSACASA-N (5-chloro-1h-indol-2-yl)-[(3s)-3-(methylamino)pyrrolidin-1-yl]methanone Chemical compound C1[C@@H](NC)CCN1C(=O)C1=CC2=CC(Cl)=CC=C2N1 VCVCGLWPFWUIPZ-NSHDSACASA-N 0.000 claims 3
- GSGYZRSHGBBBRC-UHFFFAOYSA-N (5-chloro-1h-indol-2-yl)-[3-(dimethylamino)pyrrolidin-1-yl]methanone Chemical compound C1C(N(C)C)CCN1C(=O)C1=CC2=CC(Cl)=CC=C2N1 GSGYZRSHGBBBRC-UHFFFAOYSA-N 0.000 claims 3
- AHYOCROHXORPCX-LLVKDONJSA-N (5-fluoro-1h-indol-2-yl)-[(3r)-3-(methylamino)pyrrolidin-1-yl]methanone Chemical compound C1[C@H](NC)CCN1C(=O)C1=CC2=CC(F)=CC=C2N1 AHYOCROHXORPCX-LLVKDONJSA-N 0.000 claims 3
- AHYOCROHXORPCX-NSHDSACASA-N (5-fluoro-1h-indol-2-yl)-[(3s)-3-(methylamino)pyrrolidin-1-yl]methanone Chemical compound C1[C@@H](NC)CCN1C(=O)C1=CC2=CC(F)=CC=C2N1 AHYOCROHXORPCX-NSHDSACASA-N 0.000 claims 3
- SWRHBZDOOLIKCA-UHFFFAOYSA-N 1h-benzimidazol-2-yl-[3-(dimethylamino)pyrrolidin-1-yl]methanone Chemical compound C1C(N(C)C)CCN1C(=O)C1=NC2=CC=CC=C2N1 SWRHBZDOOLIKCA-UHFFFAOYSA-N 0.000 claims 3
- HBJJZCSNSGPOIE-UHFFFAOYSA-N 1h-benzimidazol-2-yl-[3-(methylamino)pyrrolidin-1-yl]methanone Chemical compound C1C(NC)CCN1C(=O)C1=NC2=CC=CC=C2N1 HBJJZCSNSGPOIE-UHFFFAOYSA-N 0.000 claims 3
- YWEWOQJERVEGGW-RYUDHWBXSA-N 1h-indol-2-yl-[(1s,4s)-5-methyl-2,5-diazabicyclo[2.2.1]heptan-2-yl]methanone Chemical compound C1=CC=C2NC(C(=O)N3C[C@]4(N(C[C@]3([H])C4)C)[H])=CC2=C1 YWEWOQJERVEGGW-RYUDHWBXSA-N 0.000 claims 3
- KKPZRVCLXPLEOA-LLVKDONJSA-N 1h-indol-2-yl-[(3r)-3-(methylamino)pyrrolidin-1-yl]methanone Chemical compound C1[C@H](NC)CCN1C(=O)C1=CC2=CC=CC=C2N1 KKPZRVCLXPLEOA-LLVKDONJSA-N 0.000 claims 3
- KKPZRVCLXPLEOA-UHFFFAOYSA-N 1h-indol-2-yl-[3-(methylamino)pyrrolidin-1-yl]methanone Chemical compound C1C(NC)CCN1C(=O)C1=CC2=CC=CC=C2N1 KKPZRVCLXPLEOA-UHFFFAOYSA-N 0.000 claims 3
- PQUQWZHUADYWIG-QWRGUYRKSA-N [(1s,4s)-2,5-diazabicyclo[2.2.1]heptan-2-yl]-(1h-indol-2-yl)methanone Chemical compound C1=CC=C2NC(C(=O)N3C[C@]4(NC[C@]3([H])C4)[H])=CC2=C1 PQUQWZHUADYWIG-QWRGUYRKSA-N 0.000 claims 3
- DOCRCNTVCILACW-GFCCVEGCSA-N [(3r)-3-(methylamino)pyrrolidin-1-yl]-(5-methyl-1h-indol-2-yl)methanone Chemical compound C1[C@H](NC)CCN1C(=O)C1=CC2=CC(C)=CC=C2N1 DOCRCNTVCILACW-GFCCVEGCSA-N 0.000 claims 3
- AEPVGIPVZCQCFW-GFCCVEGCSA-N [(3r)-3-(methylamino)pyrrolidin-1-yl]-(7-methyl-1h-indol-2-yl)methanone Chemical compound C1[C@H](NC)CCN1C(=O)C1=CC2=CC=CC(C)=C2N1 AEPVGIPVZCQCFW-GFCCVEGCSA-N 0.000 claims 3
- DOCRCNTVCILACW-LBPRGKRZSA-N [(3s)-3-(methylamino)pyrrolidin-1-yl]-(5-methyl-1h-indol-2-yl)methanone Chemical compound C1[C@@H](NC)CCN1C(=O)C1=CC2=CC(C)=CC=C2N1 DOCRCNTVCILACW-LBPRGKRZSA-N 0.000 claims 3
- AEPVGIPVZCQCFW-LBPRGKRZSA-N [(3s)-3-(methylamino)pyrrolidin-1-yl]-(7-methyl-1h-indol-2-yl)methanone Chemical compound C1[C@@H](NC)CCN1C(=O)C1=CC2=CC=CC(C)=C2N1 AEPVGIPVZCQCFW-LBPRGKRZSA-N 0.000 claims 3
- HCVCFHLEWCCHCP-BMIGLBTASA-N [(4ar,7ar)-1,2,3,4,4a,5,7,7a-octahydropyrrolo[3,4-b]pyridin-6-yl]-(5-chloro-1h-indol-2-yl)methanone Chemical compound C([C@@H]1C2)CCN[C@H]1CN2C(=O)C1=CC2=CC(Cl)=CC=C2N1 HCVCFHLEWCCHCP-BMIGLBTASA-N 0.000 claims 3
- BZEOKZZTFPIHSQ-SWLSCSKDSA-N [(4as,7as)-1,2,3,4,4a,5,7,7a-octahydropyrrolo[3,4-b]pyridin-6-yl]-(1h-indol-2-yl)methanone Chemical compound C1=CC=C2NC(C(N3C[C@H]4NCCC[C@H]4C3)=O)=CC2=C1 BZEOKZZTFPIHSQ-SWLSCSKDSA-N 0.000 claims 3
- HCVCFHLEWCCHCP-ZUZCIYMTSA-N [(4as,7as)-1,2,3,4,4a,5,7,7a-octahydropyrrolo[3,4-b]pyridin-6-yl]-(5-chloro-1h-indol-2-yl)methanone Chemical compound C([C@H]1C2)CCN[C@@H]1CN2C(=O)C1=CC2=CC(Cl)=CC=C2N1 HCVCFHLEWCCHCP-ZUZCIYMTSA-N 0.000 claims 3
- BDEUTHRRTAMHDY-UHFFFAOYSA-N [3-(dimethylamino)pyrrolidin-1-yl]-(1h-indol-2-yl)methanone Chemical compound C1C(N(C)C)CCN1C(=O)C1=CC2=CC=CC=C2N1 BDEUTHRRTAMHDY-UHFFFAOYSA-N 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 229960001340 histamine Drugs 0.000 claims 2
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US79042106P | 2006-04-07 | 2006-04-07 | |
| US60/790,421 | 2006-04-07 | ||
| PCT/US2007/008218 WO2007117401A2 (en) | 2006-04-07 | 2007-03-30 | Indoles and benzoimidazoles as modulators of the histamine h4 receptor |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2009533343A JP2009533343A (ja) | 2009-09-17 |
| JP2009533343A5 true JP2009533343A5 (https=) | 2010-05-13 |
| JP5132673B2 JP5132673B2 (ja) | 2013-01-30 |
Family
ID=38581556
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009504253A Expired - Fee Related JP5132673B2 (ja) | 2006-04-07 | 2007-03-30 | ヒスタミンｈ４受容体のモジュレーターとしてのインドールおよびベンゾイミダゾール |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US7544698B2 (https=) |
| EP (1) | EP2010172B1 (https=) |
| JP (1) | JP5132673B2 (https=) |
| CN (1) | CN101472584B (https=) |
| AU (1) | AU2007235578B2 (https=) |
| WO (1) | WO2007117401A2 (https=) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL2007752T3 (pl) | 2006-03-31 | 2011-02-28 | Janssen Pharmaceutica Nv | Benzoimidazol-2-ilopirymidyny i pirazyny jako modulatory receptora histaminowego H4 |
| WO2007120690A2 (en) * | 2006-04-10 | 2007-10-25 | Janssen Pharmaceutica N.V. | Combination histamine h1r and h4r antagonist therapy for treating pruritus |
| WO2008074703A1 (en) | 2006-12-19 | 2008-06-26 | F. Hoffmann-La Roche Ag | Heteroaryl pyrrolidinyl and piperidinyl ketone derivatives |
| CA2695989A1 (en) * | 2007-08-10 | 2009-02-19 | Glaxosmithkline Llc | Certain nitrogen containing bicyclic chemical entities for treating viral infections |
| MX2010013727A (es) * | 2008-06-12 | 2011-01-14 | Janssen Pharmaceutica Nv | Uso de un antagonista h4 de histamina para el tratamiento de adherencias postoperatorias. |
| US9371311B2 (en) | 2008-06-30 | 2016-06-21 | Janssen Pharmaceutica Nv | Benzoimidazol-2-yl pyrimidine derivatives |
| WO2010075270A1 (en) | 2008-12-22 | 2010-07-01 | Incyte Corporation | 4, 6-disubstituted 2-amino-pyrimidines as histamine h4 receptor modulators |
| EP2201982A1 (en) | 2008-12-24 | 2010-06-30 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Histamine H4 receptor antagonists for the treatment of vestibular disorders |
| US8349852B2 (en) | 2009-01-13 | 2013-01-08 | Novartis Ag | Quinazolinone derivatives useful as vanilloid antagonists |
| TW201035078A (en) | 2009-03-20 | 2010-10-01 | Incyte Corp | Substituted heterocyclic compounds |
| WO2011013752A1 (ja) * | 2009-07-31 | 2011-02-03 | 塩野義製薬株式会社 | 縮合へテロ環誘導体を含有する医薬組成物 |
| 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 |
| HUE039713T2 (hu) | 2012-06-08 | 2019-02-28 | Sensorion | H4 receptor inhibitorok tinnitus kezelésére |
| AR092211A1 (es) * | 2012-09-24 | 2015-04-08 | Merck Patent Ges Mit Beschränkter Haftung | Derivados de hidropirrolopirrol |
| SMT202000084T1 (it) | 2013-03-06 | 2020-03-13 | Janssen Pharmaceutica Nv | Modulatori benzoimidazol-2-il pirimidinici del recettore h4 dell'istamina |
| WO2019152883A1 (en) | 2018-02-02 | 2019-08-08 | Padforward Llc | Inhibitors of protein arginine deiminases |
| WO2025017105A1 (en) * | 2023-07-18 | 2025-01-23 | Muna Therapeutics Aps | Kv1.3 potassium channel antagonists |
| TW202527931A (zh) * | 2023-11-08 | 2025-07-16 | 美商奧科坦特公司 | 視紫質的藥理校正劑及其用途 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1373204B1 (en) * | 2001-03-09 | 2016-10-26 | Janssen Pharmaceuticals, Inc. | Heterocyclic compounds |
| WO2004022060A2 (en) * | 2002-09-06 | 2004-03-18 | Janssen Pharmaceutica, N.V. | (1h-benzoimidazol-2-yl)-(piperazinyl)-methanone derivatives and related compounds as histamine h4-receptor antagonists for the treatment of inflammatory and allergic disorders |
| EP1505064A1 (en) * | 2003-08-05 | 2005-02-09 | Bayer HealthCare AG | 2-Aminopyrimidine derivatives |
| WO2005054239A1 (en) | 2003-12-05 | 2005-06-16 | Bayer Healthcare Ag | 2-aminopyrimidine derivatives |
| US20060111416A1 (en) * | 2004-11-24 | 2006-05-25 | Lane Charlotte A L | Octahydropyrrolo[3,4-C]pyrrole derivatives |
| GT200600005A (es) | 2005-01-12 | 2006-08-16 | Un derivado de 2-(aminocarbonilo ciclico)-indolina y una composicion farmaceutica que lo contiene | |
| EA200901212A1 (ru) * | 2007-03-29 | 2010-04-30 | Новартис Аг | 3-имидазолилиндолы, предназначенные для лечения пролиферативных заболеваний |
-
2007
- 2007-03-30 EP EP07754702A patent/EP2010172B1/en not_active Not-in-force
- 2007-03-30 CN CN200780021127XA patent/CN101472584B/zh not_active Expired - Fee Related
- 2007-03-30 WO PCT/US2007/008218 patent/WO2007117401A2/en not_active Ceased
- 2007-03-30 JP JP2009504253A patent/JP5132673B2/ja not_active Expired - Fee Related
- 2007-03-30 AU AU2007235578A patent/AU2007235578B2/en not_active Ceased
- 2007-03-30 US US11/731,047 patent/US7544698B2/en active Active