JP2011529069A5 - - Google Patents
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- Publication number
- JP2011529069A5 JP2011529069A5 JP2011520186A JP2011520186A JP2011529069A5 JP 2011529069 A5 JP2011529069 A5 JP 2011529069A5 JP 2011520186 A JP2011520186 A JP 2011520186A JP 2011520186 A JP2011520186 A JP 2011520186A JP 2011529069 A5 JP2011529069 A5 JP 2011529069A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- halo
- alkylene
- compound
- optionally substituted
- 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
- 125000000217 alkyl group Chemical group 0.000 claims description 277
- 125000005843 halogen group Chemical group 0.000 claims description 161
- 150000001875 compounds Chemical class 0.000 claims description 110
- 125000001153 fluoro group Chemical group F* 0.000 claims description 52
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 38
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 8
- 239000003814 drug Substances 0.000 claims description 8
- 208000027520 Somatoform disease Diseases 0.000 claims description 6
- 208000027753 pain disease Diseases 0.000 claims description 6
- 239000003795 chemical substances by application Substances 0.000 claims description 4
- 208000004296 neuralgia Diseases 0.000 claims description 4
- 208000021722 neuropathic pain Diseases 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 4
- 125000006239 protecting group Chemical group 0.000 claims description 4
- 150000003839 salts Chemical class 0.000 claims description 4
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 claims description 3
- 208000036864 Attention deficit/hyperactivity disease Diseases 0.000 claims description 3
- 206010008874 Chronic Fatigue Syndrome Diseases 0.000 claims description 3
- 208000028698 Cognitive impairment Diseases 0.000 claims description 3
- 208000001640 Fibromyalgia Diseases 0.000 claims description 3
- 208000019022 Mood disease Diseases 0.000 claims description 3
- 208000008589 Obesity Diseases 0.000 claims description 3
- 206010066218 Stress Urinary Incontinence Diseases 0.000 claims description 3
- 208000015802 attention deficit-hyperactivity disease Diseases 0.000 claims description 3
- 208000010877 cognitive disease Diseases 0.000 claims description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 3
- 208000035475 disorder Diseases 0.000 claims description 3
- 230000005764 inhibitory process Effects 0.000 claims description 3
- 230000009245 menopause Effects 0.000 claims description 3
- 208000029766 myalgic encephalomeyelitis/chronic fatigue syndrome Diseases 0.000 claims description 3
- 235000020824 obesity Nutrition 0.000 claims description 3
- 230000000697 serotonin reuptake Effects 0.000 claims description 3
- 208000024891 symptom Diseases 0.000 claims description 3
- 229940124597 therapeutic agent Drugs 0.000 claims description 3
- 230000001457 vasomotor Effects 0.000 claims description 3
- -1 — C 0-6 alkylene-OH Chemical group 0.000 claims description 3
- 208000024827 Alzheimer disease Diseases 0.000 claims description 2
- 208000018737 Parkinson disease Diseases 0.000 claims description 2
- 229940121991 Serotonin and norepinephrine reuptake inhibitor Drugs 0.000 claims description 2
- 239000000219 Sympatholytic Substances 0.000 claims description 2
- 230000001773 anti-convulsant effect Effects 0.000 claims description 2
- 230000001430 anti-depressive effect Effects 0.000 claims description 2
- 239000001961 anticonvulsive agent Substances 0.000 claims description 2
- 239000000935 antidepressant agent Substances 0.000 claims description 2
- 229940005513 antidepressants Drugs 0.000 claims description 2
- 229960003965 antiepileptics Drugs 0.000 claims description 2
- 230000015572 biosynthetic process Effects 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 238000000034 method Methods 0.000 claims description 2
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 claims description 2
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 claims description 2
- 239000002767 noradrenalin uptake inhibitor Substances 0.000 claims description 2
- 229940127221 norepinephrine reuptake inhibitor Drugs 0.000 claims description 2
- 239000003402 opiate agonist Substances 0.000 claims description 2
- 239000003775 serotonin noradrenalin reuptake inhibitor Substances 0.000 claims description 2
- 229940125794 sodium channel blocker Drugs 0.000 claims description 2
- 239000003195 sodium channel blocking agent Substances 0.000 claims description 2
- 230000000948 sympatholitic effect Effects 0.000 claims description 2
- 238000003786 synthesis reaction Methods 0.000 claims description 2
- 125000002947 alkylene group Chemical group 0.000 claims 2
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 229940127557 pharmaceutical product Drugs 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 description 2
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 description 2
- 0 C*c(c(*)c(C)c(C)c1C)c1ON Chemical compound C*c(c(*)c(C)c(C)c1C)c1ON 0.000 description 1
- 102000008092 Norepinephrine Plasma Membrane Transport Proteins Human genes 0.000 description 1
- 108010049586 Norepinephrine Plasma Membrane Transport Proteins Proteins 0.000 description 1
- 102000019208 Serotonin Plasma Membrane Transport Proteins Human genes 0.000 description 1
- 108010012996 Serotonin Plasma Membrane Transport Proteins Proteins 0.000 description 1
- 125000004429 atom Chemical group 0.000 description 1
- 208000037765 diseases and disorders Diseases 0.000 description 1
- 230000000966 norepinephrine reuptake Effects 0.000 description 1
- 229940076279 serotonin Drugs 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US13582808P | 2008-07-24 | 2008-07-24 | |
| US61/135,828 | 2008-07-24 | ||
| PCT/US2009/051496 WO2010011811A2 (en) | 2008-07-24 | 2009-07-23 | 3-(phenoxyphenylmethyl)pyrrolidine compounds |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011529069A JP2011529069A (ja) | 2011-12-01 |
| JP2011529069A5 true JP2011529069A5 (https=) | 2012-06-28 |
| JP5405571B2 JP5405571B2 (ja) | 2014-02-05 |
Family
ID=41078154
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011520186A Expired - Fee Related JP5405571B2 (ja) | 2008-07-24 | 2009-07-23 | ３−（フェノキシフェニルメチル）ピロリジン化合物 |
Country Status (7)
| Country | Link |
|---|---|
| US (3) | US7888386B2 (https=) |
| EP (1) | EP2318362B1 (https=) |
| JP (1) | JP5405571B2 (https=) |
| AR (1) | AR072611A1 (https=) |
| ES (1) | ES2434250T3 (https=) |
| TW (1) | TWI438190B (https=) |
| WO (1) | WO2010011811A2 (https=) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010011811A2 (en) * | 2008-07-24 | 2010-01-28 | Theravance, Inc. | 3-(phenoxyphenylmethyl)pyrrolidine compounds |
| US8304433B2 (en) | 2008-11-14 | 2012-11-06 | Theravance, Inc. | Crystalline form of a 4-[2-(2-fluorophenoxymethyl)phenyl]piperidine compound |
| AR075988A1 (es) | 2009-04-09 | 2011-05-11 | Lilly Co Eli | Compuesto de piridiloxi - pirrolidina inhibidor de recaptacion de serotonina y norepinefrina, composicion farmaceutica que lo comprende y su uso para la manufactura de un medicamento util para el tratamiento de dolor cronico |
| WO2010120910A1 (en) * | 2009-04-15 | 2010-10-21 | Theravance, Inc. | 3-(phenoxypyrrolidin-3-yl-methyl)heteroaryl, 3-(phenylpyrrolidin-3-ylmethoxy)heteroaryl, and 3-(heteroarylpyrrolidin-3-ylmethoxy)heteroaryl compounds |
| AU2010273645B2 (en) * | 2009-07-13 | 2014-12-04 | Theravance Biopharma R&D Ip, Llc | 3-phenoxymethylpyrrolidine compounds |
| US8273786B2 (en) | 2009-07-21 | 2012-09-25 | Theravance, Inc. | 3-phenoxymethylpyrrolidine compounds |
| NZ605490A (en) * | 2010-07-09 | 2014-10-31 | Theravance Biopharma R & D Ip Llc | Crystalline form of a 3-phenoxymethylpyrrolidine compound |
| US8471040B2 (en) | 2010-10-11 | 2013-06-25 | Theravance, Inc. | Serotonin reuptake inhibitors |
| US8501964B2 (en) | 2010-12-03 | 2013-08-06 | Theravance, Inc. | Serotonin reuptake inhibitors |
| US10056503B2 (en) * | 2016-10-25 | 2018-08-21 | International Business Machines Corporation | MIS capacitor for finned semiconductor structure |
Family Cites Families (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US363447A (en) * | 1887-05-24 | axel backsteom | ||
| GB1203149A (en) | 1968-06-10 | 1970-08-26 | Ici Ltd | Piperidine derivatives |
| DE2549999A1 (de) | 1975-11-07 | 1977-05-12 | Boehringer Mannheim Gmbh | Piperidin-derivate und verfahren zu ihrer herstellung |
| IL56369A (en) | 1978-01-20 | 1984-05-31 | Erba Farmitalia | Alpha-phenoxybenzyl propanolamine derivatives,their preparation and pharmaceutical compositions comprising them |
| US4956388A (en) | 1986-12-22 | 1990-09-11 | Eli Lilly And Company | 3-aryloxy-3-substituted propanamines |
| DE3835291A1 (de) | 1988-04-19 | 1989-11-02 | Bayer Ag | 1,3-disubstituierte pyrrolidine |
| GB9324018D0 (en) | 1993-11-23 | 1994-01-12 | Merck Sharp & Dohme | Therapeutic agents |
| US6518284B2 (en) | 1998-11-18 | 2003-02-11 | Faes, Fabrica Espanola De Productos Quimicos Y Farmaceuticos S.A. | 4-substituted piperidines |
| AU3898000A (en) * | 1999-03-19 | 2000-10-09 | Knoll Pharmaceutical Company | Treatment of neuropathic pain or fibromyalgia |
| US6465458B1 (en) | 1999-07-01 | 2002-10-15 | Pharmacia & Upjohn Company | Method of treating or preventing chronic pain with a highly selective norepinephrine reuptake inhibitor |
| US20020151712A1 (en) | 1999-09-14 | 2002-10-17 | Nan-Horng Lin | 3-pyrrolidinyloxy-3'-pyridyl ether compounds useful for controlling chemical synaptic transmission |
| US7294637B2 (en) | 2000-09-11 | 2007-11-13 | Sepracor, Inc. | Method of treating addiction or dependence using a ligand for a monamine receptor or transporter |
| JP2004538010A (ja) * | 2001-08-08 | 2004-12-24 | グラクソスミスクライン バイオロジカルズ ソシエテ アノニム | アッセイ |
| US6602911B2 (en) | 2001-11-05 | 2003-08-05 | Cypress Bioscience, Inc. | Methods of treating fibromyalgia |
| WO2004017977A2 (en) | 2002-08-23 | 2004-03-04 | Eli Lilly And Company | 2- (phenoxymethyl)- and 2- (phenylthiomethyl)-morpholine derivatives for use as selective norepinephrine reuptake inhibitors |
| SI1638933T1 (sl) | 2003-06-17 | 2008-10-31 | Pfizer | Derivati N-pirolidin-3-il-amida kot inhibitorji ponovnega privzema serotonina in noradrenalina |
| EP1729754B1 (en) | 2003-12-12 | 2008-07-02 | Eli Lilly And Company | Selective norepinephrine reuptake inhibitors for the treatment of hot flashes |
| US20070072859A1 (en) | 2004-03-05 | 2007-03-29 | Eli Lilly And Company | Pharmaceutical compounds |
| BRPI0510453A (pt) * | 2004-04-30 | 2007-10-30 | Warner Lambert Co | composto substituìdos com morfolina para o tratamento de distúrbios do sistema nervoso central |
| GB0409744D0 (en) | 2004-04-30 | 2004-06-09 | Pfizer Ltd | Novel compounds |
| CA2599478A1 (en) * | 2005-03-14 | 2006-09-21 | Teva Pharmaceutical Industries Ltd. | Process for the purification of duloxetine hydrochloride |
| US20090215857A1 (en) | 2005-09-13 | 2009-08-27 | Pfizer Products Inc. | Therapeutic Pyrrolidines |
| EP1854785A1 (en) | 2006-05-12 | 2007-11-14 | Faes Farma, S.A. | 4-[(3-fluorophenoxy)phenylmethyl]piperidine methanesulfonate: uses, process of synthesis and pharmaceutical compositions |
| EP1886898A2 (en) * | 2006-07-31 | 2008-02-13 | Fujikiko Co., Ltd. | Variable gear ratio steering device |
| EP2066630A1 (en) | 2006-08-23 | 2009-06-10 | Pfizer Products Incorporated | Piperidine derivatives |
| WO2010011811A2 (en) * | 2008-07-24 | 2010-01-28 | Theravance, Inc. | 3-(phenoxyphenylmethyl)pyrrolidine compounds |
| AR075988A1 (es) | 2009-04-09 | 2011-05-11 | Lilly Co Eli | Compuesto de piridiloxi - pirrolidina inhibidor de recaptacion de serotonina y norepinefrina, composicion farmaceutica que lo comprende y su uso para la manufactura de un medicamento util para el tratamiento de dolor cronico |
| WO2010120910A1 (en) | 2009-04-15 | 2010-10-21 | Theravance, Inc. | 3-(phenoxypyrrolidin-3-yl-methyl)heteroaryl, 3-(phenylpyrrolidin-3-ylmethoxy)heteroaryl, and 3-(heteroarylpyrrolidin-3-ylmethoxy)heteroaryl compounds |
| AU2010273645B2 (en) | 2009-07-13 | 2014-12-04 | Theravance Biopharma R&D Ip, Llc | 3-phenoxymethylpyrrolidine compounds |
| US8273786B2 (en) | 2009-07-21 | 2012-09-25 | Theravance, Inc. | 3-phenoxymethylpyrrolidine compounds |
-
2009
- 2009-07-23 WO PCT/US2009/051496 patent/WO2010011811A2/en not_active Ceased
- 2009-07-23 EP EP09790753.9A patent/EP2318362B1/en not_active Not-in-force
- 2009-07-23 US US12/507,965 patent/US7888386B2/en not_active Expired - Fee Related
- 2009-07-23 JP JP2011520186A patent/JP5405571B2/ja not_active Expired - Fee Related
- 2009-07-23 ES ES09790753T patent/ES2434250T3/es active Active
- 2009-07-23 TW TW098124917A patent/TWI438190B/zh not_active IP Right Cessation
- 2009-07-24 AR ARP090102844A patent/AR072611A1/es unknown
-
2011
- 2011-01-04 US US12/984,076 patent/US8242164B2/en not_active Expired - Fee Related
-
2012
- 2012-06-27 US US13/534,878 patent/US8933249B2/en not_active Expired - Fee Related
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