JP2008516952A5 - - Google Patents
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- Publication number
- JP2008516952A5 JP2008516952A5 JP2007536740A JP2007536740A JP2008516952A5 JP 2008516952 A5 JP2008516952 A5 JP 2008516952A5 JP 2007536740 A JP2007536740 A JP 2007536740A JP 2007536740 A JP2007536740 A JP 2007536740A JP 2008516952 A5 JP2008516952 A5 JP 2008516952A5
- Authority
- JP
- Japan
- Prior art keywords
- pyrrolidin
- ylmethyl
- ylmethoxy
- fluoro
- phenyl
- 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
- 229910052736 halogen Inorganic materials 0.000 claims 17
- 150000001875 compounds Chemical class 0.000 claims 9
- 150000002367 halogens Chemical class 0.000 claims 9
- 150000003839 salts Chemical class 0.000 claims 9
- -1 5-methyl-isoxazol-3-ylmethoxy Chemical group 0.000 claims 3
- 125000006555 (C3-C5) cycloalkyl group Chemical group 0.000 claims 1
- RJANDLOOYJZMBS-AEFFLSMTSA-N 4-[[3-fluoro-4-[(2s)-2-[[(2r)-2-methylpyrrolidin-1-yl]methyl]pyrrolidine-1-carbonyl]phenoxy]methyl]thiophene-2-carbonitrile Chemical compound C[C@@H]1CCCN1C[C@H]1N(C(=O)C=2C(=CC(OCC=3C=C(SC=3)C#N)=CC=2)F)CCC1 RJANDLOOYJZMBS-AEFFLSMTSA-N 0.000 claims 1
- NJHNBQXYCPBMRF-INIZCTEOSA-N 5-[[3-fluoro-4-[(2s)-2-(pyrrolidin-1-ylmethyl)pyrrolidine-1-carbonyl]phenoxy]methyl]thiophene-2-carbonitrile Chemical compound C=1C=C(C(=O)N2[C@@H](CCC2)CN2CCCC2)C(F)=CC=1OCC1=CC=C(C#N)S1 NJHNBQXYCPBMRF-INIZCTEOSA-N 0.000 claims 1
- FDNVCEFBEKHKDT-SJORKVTESA-N 5-[[3-fluoro-4-[(2s)-2-[[(2r)-2-methylpyrrolidin-1-yl]methyl]pyrrolidine-1-carbonyl]phenoxy]methyl]thiophene-2-carbonitrile Chemical compound C[C@@H]1CCCN1C[C@H]1N(C(=O)C=2C(=CC(OCC=3SC(=CC=3)C#N)=CC=2)F)CCC1 FDNVCEFBEKHKDT-SJORKVTESA-N 0.000 claims 1
- FLOSJRIAPCQVDP-SFHVURJKSA-N 5-[[4-[(2s)-2-(pyrrolidin-1-ylmethyl)pyrrolidine-1-carbonyl]phenoxy]methyl]thiophene-2-carbonitrile Chemical compound C([C@@H]1CCCN1C(=O)C=1C=CC(OCC=2SC(=CC=2)C#N)=CC=1)N1CCCC1 FLOSJRIAPCQVDP-SFHVURJKSA-N 0.000 claims 1
- PVUGQUPKOGASSK-SFHVURJKSA-N [(2s)-2-(pyrrolidin-1-ylmethyl)pyrrolidin-1-yl]-[4-(1,3-thiazol-4-ylmethoxy)phenyl]methanone Chemical compound C([C@@H]1CCCN1C(=O)C=1C=CC(OCC=2N=CSC=2)=CC=1)N1CCCC1 PVUGQUPKOGASSK-SFHVURJKSA-N 0.000 claims 1
- MCHBDEXSONVGQC-HNNXBMFYSA-N [2,6-difluoro-4-(1,3-thiazol-4-ylmethoxy)phenyl]-[(2s)-2-(pyrrolidin-1-ylmethyl)pyrrolidin-1-yl]methanone Chemical compound C=1C(F)=C(C(=O)N2[C@@H](CCC2)CN2CCCC2)C(F)=CC=1OCC1=CSC=N1 MCHBDEXSONVGQC-HNNXBMFYSA-N 0.000 claims 1
- HTKCUYXBXSHDSP-ZBFHGGJFSA-N [2,6-difluoro-4-(1,3-thiazol-4-ylmethoxy)phenyl]-[(2s)-2-[[(2r)-2-methylpyrrolidin-1-yl]methyl]pyrrolidin-1-yl]methanone Chemical compound C[C@@H]1CCCN1C[C@H]1N(C(=O)C=2C(=CC(OCC=3N=CSC=3)=CC=2F)F)CCC1 HTKCUYXBXSHDSP-ZBFHGGJFSA-N 0.000 claims 1
- PVSWTAKSGHNTRF-CABCVRRESA-N [2-fluoro-4-(1,2,4-oxadiazol-3-ylmethoxy)phenyl]-[(2s)-2-[[(2r)-2-methylpyrrolidin-1-yl]methyl]pyrrolidin-1-yl]methanone Chemical compound C[C@@H]1CCCN1C[C@H]1N(C(=O)C=2C(=CC(OCC3=NOC=N3)=CC=2)F)CCC1 PVSWTAKSGHNTRF-CABCVRRESA-N 0.000 claims 1
- YFWUYTNJRRVBFN-INIZCTEOSA-N [2-fluoro-4-(1,3-thiazol-4-ylmethoxy)phenyl]-[(2s)-2-(pyrrolidin-1-ylmethyl)pyrrolidin-1-yl]methanone Chemical compound C=1C=C(C(=O)N2[C@@H](CCC2)CN2CCCC2)C(F)=CC=1OCC1=CSC=N1 YFWUYTNJRRVBFN-INIZCTEOSA-N 0.000 claims 1
- ILFGLUNAXXOWES-WBVHZDCISA-N [2-fluoro-4-(1,3-thiazol-4-ylmethoxy)phenyl]-[(2s)-2-[[(2r)-2-methylpyrrolidin-1-yl]methyl]pyrrolidin-1-yl]methanone Chemical compound C[C@@H]1CCCN1C[C@H]1N(C(=O)C=2C(=CC(OCC=3N=CSC=3)=CC=2)F)CCC1 ILFGLUNAXXOWES-WBVHZDCISA-N 0.000 claims 1
- QTLZUZWCPCWZAE-INIZCTEOSA-N [2-fluoro-4-(thiophen-2-ylmethoxy)phenyl]-[(2s)-2-(pyrrolidin-1-ylmethyl)pyrrolidin-1-yl]methanone Chemical compound C=1C=C(C(=O)N2[C@@H](CCC2)CN2CCCC2)C(F)=CC=1OCC1=CC=CS1 QTLZUZWCPCWZAE-INIZCTEOSA-N 0.000 claims 1
- GPTVJPPWMAHWGB-SJORKVTESA-N [2-fluoro-4-(thiophen-2-ylmethoxy)phenyl]-[(2s)-2-[[(2r)-2-methylpyrrolidin-1-yl]methyl]pyrrolidin-1-yl]methanone Chemical compound C[C@@H]1CCCN1C[C@H]1N(C(=O)C=2C(=CC(OCC=3SC=CC=3)=CC=2)F)CCC1 GPTVJPPWMAHWGB-SJORKVTESA-N 0.000 claims 1
- MMANFHMGFZSBFD-KRWDZBQOSA-N [2-fluoro-4-(thiophen-3-ylmethoxy)phenyl]-[(2s)-2-(pyrrolidin-1-ylmethyl)pyrrolidin-1-yl]methanone Chemical compound C=1C=C(C(=O)N2[C@@H](CCC2)CN2CCCC2)C(F)=CC=1OCC=1C=CSC=1 MMANFHMGFZSBFD-KRWDZBQOSA-N 0.000 claims 1
- HUJXDNMOENJJJB-AEFFLSMTSA-N [2-fluoro-4-(thiophen-3-ylmethoxy)phenyl]-[(2s)-2-[[(2r)-2-methylpyrrolidin-1-yl]methyl]pyrrolidin-1-yl]methanone Chemical compound C[C@@H]1CCCN1C[C@H]1N(C(=O)C=2C(=CC(OCC3=CSC=C3)=CC=2)F)CCC1 HUJXDNMOENJJJB-AEFFLSMTSA-N 0.000 claims 1
- RXZKMRMIKZQLCR-KRWDZBQOSA-N [2-fluoro-4-[(2-methyl-1,3-thiazol-4-yl)methoxy]phenyl]-[(2s)-2-(pyrrolidin-1-ylmethyl)pyrrolidin-1-yl]methanone Chemical compound S1C(C)=NC(COC=2C=C(F)C(C(=O)N3[C@@H](CCC3)CN3CCCC3)=CC=2)=C1 RXZKMRMIKZQLCR-KRWDZBQOSA-N 0.000 claims 1
- IXMSJMMDPFQCIY-QAPCUYQASA-N [2-fluoro-4-[(2-methyl-1,3-thiazol-4-yl)methoxy]phenyl]-[(2s)-2-[[(2r)-2-methylpyrrolidin-1-yl]methyl]pyrrolidin-1-yl]methanone Chemical compound C[C@@H]1CCCN1C[C@H]1N(C(=O)C=2C(=CC(OCC=3N=C(C)SC=3)=CC=2)F)CCC1 IXMSJMMDPFQCIY-QAPCUYQASA-N 0.000 claims 1
- ADWVCLGYPBXOQO-SFHVURJKSA-N [4-(furan-2-ylmethoxy)phenyl]-[(2s)-2-(pyrrolidin-1-ylmethyl)pyrrolidin-1-yl]methanone Chemical compound C([C@@H]1CCCN1C(=O)C=1C=CC(OCC=2OC=CC=2)=CC=1)N1CCCC1 ADWVCLGYPBXOQO-SFHVURJKSA-N 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- GSXCEVHRIVLFJV-UHFFFAOYSA-N thiophene-3-carbonitrile Chemical compound N#CC=1C=CSC=1 GSXCEVHRIVLFJV-UHFFFAOYSA-N 0.000 claims 1
- 0 Cc1c(*)[n](C)nc1C Chemical compound Cc1c(*)[n](C)nc1C 0.000 description 6
- BNYXZUHLZRBMCQ-UHFFFAOYSA-N CBc1n[o]c(C)n1 Chemical compound CBc1n[o]c(C)n1 BNYXZUHLZRBMCQ-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US61978504P | 2004-10-18 | 2004-10-18 | |
| US60/619,785 | 2004-10-18 | ||
| PCT/US2005/036023 WO2006044228A1 (en) | 2004-10-18 | 2005-10-11 | Histamine h3 receptor inhibitors, preparation and therapeutic uses |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2008516952A JP2008516952A (ja) | 2008-05-22 |
| JP2008516952A5 true JP2008516952A5 (enExample) | 2008-10-30 |
| JP5057982B2 JP5057982B2 (ja) | 2012-10-24 |
Family
ID=35677663
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007536740A Expired - Fee Related JP5057982B2 (ja) | 2004-10-18 | 2005-10-11 | ヒスタミンｈ３受容体阻害剤、製造及び治療的使用 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US7846950B2 (enExample) |
| EP (1) | EP1805169B1 (enExample) |
| JP (1) | JP5057982B2 (enExample) |
| AT (1) | ATE418553T1 (enExample) |
| CY (1) | CY1110453T1 (enExample) |
| DE (1) | DE602005011988D1 (enExample) |
| DK (1) | DK1805169T3 (enExample) |
| ES (1) | ES2318565T3 (enExample) |
| PL (1) | PL1805169T3 (enExample) |
| PT (1) | PT1805169E (enExample) |
| SI (1) | SI1805169T1 (enExample) |
| WO (1) | WO2006044228A1 (enExample) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8008301B2 (en) * | 2004-04-01 | 2011-08-30 | Eli Lilly And Company | Histamine H3 receptor agents, preparation and therapeutic uses |
| CA2600757C (en) * | 2005-03-17 | 2014-02-18 | Eli Lilly And Company | Pyrrolidine derivatives as histamine h3 receptor antagonists |
| SA110310332B1 (ar) | 2009-05-01 | 2013-12-10 | Astrazeneca Ab | مركبات ميثانون (3 استبدال -ازيتيدين -1-يل )(5- فينيل -1، 3، 4- أوكساديازول -2-يل ) |
| EA201291384A1 (ru) | 2010-07-06 | 2013-07-30 | Астразенека Аб | Терапевтические агенты 976 |
| UY34194A (es) | 2011-07-15 | 2013-02-28 | Astrazeneca Ab | ?(3-(4-(espiroheterocíclico)metil)fenoxi)azetidin-1-il)(5-(fenil)-1,3,4-oxadiazol-2-il)metanona en el tratamiento de la obesidad? |
| WO2013151982A1 (en) | 2012-04-03 | 2013-10-10 | Arena Pharmaceuticals, Inc. | Methods and compounds useful in treating pruritus, and methods for identifying such compounds |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2579596B1 (fr) | 1985-03-26 | 1987-11-20 | Inst Nat Sante Rech Med | (imidazolyl-4) piperidines, leur preparation et leur application en therapeutique |
| FR2671083B1 (fr) | 1990-12-31 | 1994-12-23 | Inst Nat Sante Rech Med | Nouvelles 4-(4-imidazolyl) piperidines substituees en 1, leur preparation ainsi que leurs applications therapeutiques. |
| AU721325B2 (en) | 1995-05-30 | 2000-06-29 | Gliatech Inc. | 1H-4(5)-substituted imidazole derivatives |
| US5652258A (en) | 1995-05-30 | 1997-07-29 | Gliatech, Inc. | 2-(4-imidazoyl) cyclopropyl derivatives |
| CA2244745A1 (en) | 1996-02-09 | 1997-08-14 | James Black Foundation Limited | Histamine h3 receptor ligands |
| EP1379493A2 (en) * | 2001-03-23 | 2004-01-14 | Eli Lilly and Company | Non-imidazole aryl alkylamines compounds as histamine h3 receptor antagonists, preparation and therapeutic uses |
| US7696234B2 (en) * | 2004-06-02 | 2010-04-13 | Eli Lilly And Company | Histamine H3 receptor agents, preparation and therapeutic uses |
-
2005
- 2005-10-11 WO PCT/US2005/036023 patent/WO2006044228A1/en not_active Ceased
- 2005-10-11 JP JP2007536740A patent/JP5057982B2/ja not_active Expired - Fee Related
- 2005-10-11 US US11/577,388 patent/US7846950B2/en not_active Expired - Fee Related
- 2005-10-11 EP EP05804419A patent/EP1805169B1/en not_active Expired - Lifetime
- 2005-10-11 DE DE602005011988T patent/DE602005011988D1/de not_active Expired - Lifetime
- 2005-10-11 AT AT05804419T patent/ATE418553T1/de active
- 2005-10-11 ES ES05804419T patent/ES2318565T3/es not_active Expired - Lifetime
- 2005-10-11 PL PL05804419T patent/PL1805169T3/pl unknown
- 2005-10-11 DK DK05804419T patent/DK1805169T3/da active
- 2005-10-11 SI SI200530613T patent/SI1805169T1/sl unknown
- 2005-10-11 PT PT05804419T patent/PT1805169E/pt unknown
-
2009
- 2009-03-10 CY CY20091100269T patent/CY1110453T1/el unknown
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