JP2011500696A5 - - Google Patents
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- Publication number
- JP2011500696A5 JP2011500696A5 JP2010530052A JP2010530052A JP2011500696A5 JP 2011500696 A5 JP2011500696 A5 JP 2011500696A5 JP 2010530052 A JP2010530052 A JP 2010530052A JP 2010530052 A JP2010530052 A JP 2010530052A JP 2011500696 A5 JP2011500696 A5 JP 2011500696A5
- Authority
- JP
- Japan
- Prior art keywords
- oxo
- methyl
- pyridinyl
- disease
- benzofuranyl
- 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
- -1 methanesulfonylmethyl Chemical group 0.000 claims 29
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- 125000004076 pyridyl group Chemical group 0.000 claims 5
- UEXCJVNBTNXOEH-UHFFFAOYSA-N Ethynylbenzene Chemical compound C#CC1=CC=CC=C1 UEXCJVNBTNXOEH-UHFFFAOYSA-N 0.000 claims 4
- 229910052801 chlorine Inorganic materials 0.000 claims 4
- 239000000460 chlorine Substances 0.000 claims 4
- 150000001875 compounds Chemical class 0.000 claims 4
- 125000001425 triazolyl group Chemical group 0.000 claims 4
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 3
- YCKRFDGAMUMZLT-UHFFFAOYSA-N Fluorine atom Chemical compound [F] YCKRFDGAMUMZLT-UHFFFAOYSA-N 0.000 claims 3
- 229910052731 fluorine Inorganic materials 0.000 claims 3
- 239000011737 fluorine Substances 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 3
- KGIGUEBEKRSTEW-UHFFFAOYSA-N 2-vinylpyridine Chemical compound C=CC1=CC=CC=N1 KGIGUEBEKRSTEW-UHFFFAOYSA-N 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 208000028698 Cognitive impairment Diseases 0.000 claims 2
- 206010012289 Dementia Diseases 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- PPBRXRYQALVLMV-UHFFFAOYSA-N Styrene Chemical compound C=CC1=CC=CC=C1 PPBRXRYQALVLMV-UHFFFAOYSA-N 0.000 claims 2
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 2
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 2
- 125000002047 benzodioxolyl group Chemical group O1OC(C2=C1C=CC=C2)* 0.000 claims 2
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 2
- 125000003354 benzotriazolyl group Chemical group N1N=NC2=C1C=CC=C2* 0.000 claims 2
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims 2
- 208000010877 cognitive disease Diseases 0.000 claims 2
- 125000005433 dihydrobenzodioxinyl group Chemical group O1C(COC2=C1C=CC=C2)* 0.000 claims 2
- 125000000723 dihydrobenzofuranyl group Chemical group O1C(CC2=C1C=CC=C2)* 0.000 claims 2
- 125000006222 dimethylaminomethyl group Chemical group [H]C([H])([H])N(C([H])([H])[H])C([H])([H])* 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- 125000004857 imidazopyridinyl group Chemical group N1C(=NC2=C1C=CC=N2)* 0.000 claims 2
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 2
- 125000001041 indolyl group Chemical group 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- HRDXJKGNWSUIBT-UHFFFAOYSA-N methoxybenzene Chemical group [CH2]OC1=CC=CC=C1 HRDXJKGNWSUIBT-UHFFFAOYSA-N 0.000 claims 2
- 125000002757 morpholinyl group Chemical group 0.000 claims 2
- 125000002971 oxazolyl group Chemical group 0.000 claims 2
- 125000005476 oxopyrrolidinyl group Chemical group 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000006225 propoxyethyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 125000000168 pyrrolyl group Chemical group 0.000 claims 2
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 2
- 125000000335 thiazolyl group Chemical group 0.000 claims 2
- 125000001544 thienyl group Chemical group 0.000 claims 2
- BAYMNWJMIJZNLH-UHFFFAOYSA-N 2-[2-(2-methoxyethyl)hydrazinyl]ethanol Chemical compound COCCNNCCO BAYMNWJMIJZNLH-UHFFFAOYSA-N 0.000 claims 1
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 claims 1
- 208000036864 Attention deficit/hyperactivity disease Diseases 0.000 claims 1
- DWTGRRBWZVSRSG-UHFFFAOYSA-N CNC(C(NC=O)N(C)C)(NCCO)OC Chemical compound CNC(C(NC=O)N(C)C)(NCCO)OC DWTGRRBWZVSRSG-UHFFFAOYSA-N 0.000 claims 1
- 208000019888 Circadian rhythm sleep disease Diseases 0.000 claims 1
- 206010024264 Lethargy Diseases 0.000 claims 1
- 208000005793 Restless legs syndrome Diseases 0.000 claims 1
- 208000032140 Sleepiness Diseases 0.000 claims 1
- 206010041349 Somnolence Diseases 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 208000015802 attention deficit-hyperactivity disease Diseases 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 150000001804 chlorine Chemical class 0.000 claims 1
- 125000004230 chromenyl group Chemical group O1C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 125000004593 naphthyridinyl group Chemical group N1=C(C=CC2=CC=CN=C12)* 0.000 claims 1
- 201000003631 narcolepsy Diseases 0.000 claims 1
- 208000001797 obstructive sleep apnea Diseases 0.000 claims 1
- 230000000737 periodic effect Effects 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 208000019116 sleep disease Diseases 0.000 claims 1
- 208000020685 sleep-wake disease Diseases 0.000 claims 1
- 230000037321 sleepiness Effects 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US98060107P | 2007-10-17 | 2007-10-17 | |
| US60/980,601 | 2007-10-17 | ||
| PCT/US2008/079760 WO2009052065A1 (en) | 2007-10-17 | 2008-10-14 | Substituted n-phenyl-bipyrrolidine carboxamides and therapeutic use thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011500696A JP2011500696A (ja) | 2011-01-06 |
| JP2011500696A5 true JP2011500696A5 (enExample) | 2011-07-28 |
| JP5255644B2 JP5255644B2 (ja) | 2013-08-07 |
Family
ID=40243633
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010530052A Expired - Fee Related JP5255644B2 (ja) | 2007-10-17 | 2008-10-14 | 置換されたn−フェニル−ビピロリジンカルボキサミド及びその治療上の使用 |
Country Status (25)
| Country | Link |
|---|---|
| US (1) | US8618159B2 (enExample) |
| EP (1) | EP2212282B1 (enExample) |
| JP (1) | JP5255644B2 (enExample) |
| KR (1) | KR20100092441A (enExample) |
| CN (1) | CN101903339B (enExample) |
| AT (1) | ATE525350T1 (enExample) |
| AU (1) | AU2008312638B2 (enExample) |
| BR (1) | BRPI0818626A2 (enExample) |
| CA (1) | CA2702482C (enExample) |
| CO (1) | CO6190616A2 (enExample) |
| CY (1) | CY1112683T1 (enExample) |
| DK (1) | DK2212282T3 (enExample) |
| ES (1) | ES2374116T3 (enExample) |
| HR (1) | HRP20110953T1 (enExample) |
| IL (1) | IL205003A0 (enExample) |
| MA (1) | MA31855B1 (enExample) |
| MX (1) | MX2010004094A (enExample) |
| MY (1) | MY149650A (enExample) |
| NZ (1) | NZ584688A (enExample) |
| PL (1) | PL2212282T3 (enExample) |
| PT (1) | PT2212282E (enExample) |
| RU (1) | RU2477719C2 (enExample) |
| SI (1) | SI2212282T1 (enExample) |
| WO (1) | WO2009052065A1 (enExample) |
| ZA (1) | ZA201001946B (enExample) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2477720C2 (ru) * | 2007-10-17 | 2013-03-20 | Санофи-Авентис | Замещенные n-фенилбипирролидинкарбоксамиды и их применение в лечебных целях |
| PL2215058T3 (pl) | 2007-10-17 | 2012-04-30 | Sanofi Sa | Podstawione N-fenylo-bipirolidynomoczniki oraz ich zastosowanie terapeutyczne |
| JP5377504B2 (ja) | 2007-10-17 | 2013-12-25 | サノフイ | 置換されたn−フェニル−ピロリジニルメチルピロリジンアミドおよびその治療的用途 |
| AR074466A1 (es) * | 2008-12-05 | 2011-01-19 | Sanofi Aventis | Piperidina espiro pirrolidinona y piperidinona sustituidas y su uso terapeutico en enfermedades mediadas por la modulacion de los receptores h3. |
| AR074467A1 (es) | 2008-12-05 | 2011-01-19 | Sanofi Aventis | Tetrahidropiran espiro pirrolidinonas y piperidinonas sustituidas, composiciones farmaceuticas que las contienen y uso de las mismas en el tratamiento y/o prevencion de enfermedades del snc ,tales como alzheimer y parkinson, entre otras. |
| TW201206901A (en) * | 2010-05-11 | 2012-02-16 | Sanofi Aventis | Substituted N-heteroaryl bipyrrolidine carboxamides, preparation and therapeutic use thereof |
| TW201206910A (en) | 2010-05-11 | 2012-02-16 | Sanofi Aventis | Substituted N-heterocycloalkyl bipyrrolidinylphenyl amide derivatives, preparation and therapeutic use thereof |
| WO2011143148A1 (en) * | 2010-05-11 | 2011-11-17 | Sanofi | Substituted n-heteroaryl spirolactam bipyrrolidines, preparation and therapeutic use thereof |
| JP5784110B2 (ja) * | 2010-05-11 | 2015-09-24 | サノフイ | 置換されたn−ヘテロアリールテトラヒドロ−イソキノリン誘導体、その製造及び治療上の使用 |
| TW201206939A (en) * | 2010-05-11 | 2012-02-16 | Sanofi Aventis | Substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides, preparation and therapeutic use thereof |
| JP5766278B2 (ja) * | 2010-05-11 | 2015-08-19 | サノフイ | 置換されたn−アルキルおよびn−アシルテトラヒドロ−イソキノリン誘導体、それらの製造および治療上の使用 |
| WO2011143163A1 (en) * | 2010-05-11 | 2011-11-17 | Sanofi | Substituted n-phenyl spirolactam bipyrrolidines, preparation and therapeutic use thereof |
| US9309212B2 (en) | 2011-05-24 | 2016-04-12 | The Wistar Institute | Compositions and methods for modulating the activity of Epstein-Barr nuclear antigen 1 |
| CN105102448B (zh) | 2013-02-28 | 2018-03-06 | 百时美施贵宝公司 | 作为rock1和rock2抑制剂的苯基吡唑衍生物 |
| AR094929A1 (es) | 2013-02-28 | 2015-09-09 | Bristol Myers Squibb Co | Derivados de fenilpirazol como inhibidores potentes de rock1 y rock2 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PE20020507A1 (es) * | 2000-10-17 | 2002-06-25 | Schering Corp | Compuestos no-imidazoles como antagonistas del receptor histamina h3 |
| JP2006505590A (ja) * | 2002-10-23 | 2006-02-16 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | ヒスタミンh3受容体調節物質としてのフェニルピペリジンおよびフェニルピロリジン |
| DE10306250A1 (de) * | 2003-02-14 | 2004-09-09 | Aventis Pharma Deutschland Gmbh | Substituierte N-Arylheterozyklen, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
| US7223788B2 (en) * | 2003-02-14 | 2007-05-29 | Sanofi-Aventis Deutschland Gmbh | Substituted N-aryl heterocycles, process for their preparation and their use as medicaments |
| CA2600757C (en) | 2005-03-17 | 2014-02-18 | Eli Lilly And Company | Pyrrolidine derivatives as histamine h3 receptor antagonists |
| EP1868991B1 (en) * | 2005-04-01 | 2014-07-30 | Eli Lilly And Company | Histamine h3 receptor agents, preparation and therapeutic uses |
| CA2613192C (en) * | 2005-07-01 | 2013-12-31 | Eli Lilly And Company | Histamine h3 receptor agents, preparation and therapeutic uses |
| TW200804274A (en) * | 2005-10-27 | 2008-01-16 | Ucb Sa | Compounds comprising a lactam or a lactam derivative moiety, processes for making them, and their uses |
| JP5377504B2 (ja) * | 2007-10-17 | 2013-12-25 | サノフイ | 置換されたn−フェニル−ピロリジニルメチルピロリジンアミドおよびその治療的用途 |
| RU2477720C2 (ru) * | 2007-10-17 | 2013-03-20 | Санофи-Авентис | Замещенные n-фенилбипирролидинкарбоксамиды и их применение в лечебных целях |
| PL2215058T3 (pl) | 2007-10-17 | 2012-04-30 | Sanofi Sa | Podstawione N-fenylo-bipirolidynomoczniki oraz ich zastosowanie terapeutyczne |
-
2008
- 2008-10-14 HR HR20110953T patent/HRP20110953T1/hr unknown
- 2008-10-14 WO PCT/US2008/079760 patent/WO2009052065A1/en not_active Ceased
- 2008-10-14 CA CA2702482A patent/CA2702482C/en not_active Expired - Fee Related
- 2008-10-14 SI SI200830482T patent/SI2212282T1/sl unknown
- 2008-10-14 JP JP2010530052A patent/JP5255644B2/ja not_active Expired - Fee Related
- 2008-10-14 NZ NZ584688A patent/NZ584688A/en not_active IP Right Cessation
- 2008-10-14 BR BRPI0818626A patent/BRPI0818626A2/pt not_active IP Right Cessation
- 2008-10-14 PT PT08839473T patent/PT2212282E/pt unknown
- 2008-10-14 ES ES08839473T patent/ES2374116T3/es active Active
- 2008-10-14 MX MX2010004094A patent/MX2010004094A/es active IP Right Grant
- 2008-10-14 CN CN2008801211996A patent/CN101903339B/zh not_active Expired - Fee Related
- 2008-10-14 KR KR1020107010545A patent/KR20100092441A/ko not_active Ceased
- 2008-10-14 MY MYPI2010001276A patent/MY149650A/en unknown
- 2008-10-14 RU RU2010119560/04A patent/RU2477719C2/ru not_active IP Right Cessation
- 2008-10-14 DK DK08839473.9T patent/DK2212282T3/da active
- 2008-10-14 AU AU2008312638A patent/AU2008312638B2/en not_active Ceased
- 2008-10-14 AT AT08839473T patent/ATE525350T1/de active
- 2008-10-14 PL PL08839473T patent/PL2212282T3/pl unknown
- 2008-10-14 EP EP08839473A patent/EP2212282B1/en active Active
-
2010
- 2010-03-15 US US12/724,035 patent/US8618159B2/en active Active
- 2010-03-18 ZA ZA201001946A patent/ZA201001946B/xx unknown
- 2010-04-11 IL IL205003A patent/IL205003A0/en unknown
- 2010-04-16 CO CO10044768A patent/CO6190616A2/es not_active Application Discontinuation
- 2010-05-17 MA MA32846A patent/MA31855B1/fr unknown
-
2011
- 2011-12-21 CY CY20111101272T patent/CY1112683T1/el unknown
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