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 (https=) | 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 (https=) |
| EP (1) | EP1805169B1 (https=) |
| JP (1) | JP5057982B2 (https=) |
| AT (1) | ATE418553T1 (https=) |
| CY (1) | CY1110453T1 (https=) |
| DE (1) | DE602005011988D1 (https=) |
| DK (1) | DK1805169T3 (https=) |
| ES (1) | ES2318565T3 (https=) |
| PL (1) | PL1805169T3 (https=) |
| PT (1) | PT1805169E (https=) |
| SI (1) | SI1805169T1 (https=) |
| WO (1) | WO2006044228A1 (https=) |
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 |
| BRPI0608523A2 (pt) * | 2005-03-17 | 2010-11-16 | Lilly Co Eli | composto ou um sal farmaceuticamente aceitável do mesmo, composição farmacêutica, métodos para inibir receptor de histamina h3 em um mamìfero, para tratar ou prevenir um distúrbio do sistema nervoso, para tratar ou prevenir obesidade e para tratar ou prevenir um distúrbio ou doença, e, uso de um composto ou um sal do mesmo |
| 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 ) |
| AU2011275547B2 (en) | 2010-07-06 | 2015-10-29 | Astrazeneca Ab | Therapeutic agents 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. |
| DE69619381T2 (de) | 1995-05-30 | 2002-11-21 | Gliatech, Inc. | 1h-4(5)substituierte imidazolderivate |
| US5652258A (en) | 1995-05-30 | 1997-07-29 | Gliatech, Inc. | 2-(4-imidazoyl) cyclopropyl derivatives |
| WO1997029092A1 (en) | 1996-02-09 | 1997-08-14 | James Black Foundation Limited | Histamine h3 receptor ligands |
| JP2004532834A (ja) * | 2001-03-23 | 2004-10-28 | イーライ・リリー・アンド・カンパニー | ヒスタミンｈ３受容体アンタゴニストである非イミダゾール系アリールアルキルアミン化合物、その製造および治療的使用 |
| EP1756051B1 (en) * | 2004-06-02 | 2012-09-12 | Eli Lilly And Company | Histamine H3 receptor agents, preparation and therapeutic uses |
-
2005
- 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 WO PCT/US2005/036023 patent/WO2006044228A1/en not_active Ceased
- 2005-10-11 AT AT05804419T patent/ATE418553T1/de active
- 2005-10-11 SI SI200530613T patent/SI1805169T1/sl unknown
- 2005-10-11 PT PT05804419T patent/PT1805169E/pt unknown
- 2005-10-11 DK DK05804419T patent/DK1805169T3/da active
- 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 PL PL05804419T patent/PL1805169T3/pl unknown
- 2005-10-11 ES ES05804419T patent/ES2318565T3/es not_active Expired - Lifetime
-
2009
- 2009-03-10 CY CY20091100269T patent/CY1110453T1/el unknown
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