JP2005529840A5 - - Google Patents
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- JP2005529840A5 JP2005529840A5 JP2003535718A JP2003535718A JP2005529840A5 JP 2005529840 A5 JP2005529840 A5 JP 2005529840A5 JP 2003535718 A JP2003535718 A JP 2003535718A JP 2003535718 A JP2003535718 A JP 2003535718A JP 2005529840 A5 JP2005529840 A5 JP 2005529840A5
- Authority
- JP
- Japan
- Prior art keywords
- composition
- compound
- group
- sleep disorder
- therapeutic compound
- 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.)
- Pending
Links
- 239000000203 mixture Substances 0.000 claims 70
- 150000001875 compounds Chemical class 0.000 claims 60
- 208000019116 sleep disease Diseases 0.000 claims 34
- 208000020685 sleep-wake disease Diseases 0.000 claims 33
- 230000001225 therapeutic effect Effects 0.000 claims 29
- 210000003169 central nervous system Anatomy 0.000 claims 20
- 125000006850 spacer group Chemical group 0.000 claims 20
- 230000035515 penetration Effects 0.000 claims 12
- 230000004071 biological effect Effects 0.000 claims 10
- 125000000217 alkyl group Chemical group 0.000 claims 9
- 239000004215 Carbon black (E152) Substances 0.000 claims 7
- 229930195733 hydrocarbon Natural products 0.000 claims 7
- 150000002430 hydrocarbons Chemical class 0.000 claims 7
- 125000001424 substituent group Chemical group 0.000 claims 7
- 239000002253 acid Substances 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 230000000694 effects Effects 0.000 claims 4
- 150000002148 esters Chemical class 0.000 claims 4
- 230000002093 peripheral effect Effects 0.000 claims 4
- 230000005856 abnormality Effects 0.000 claims 3
- 125000002015 acyclic group Chemical group 0.000 claims 3
- 230000008499 blood brain barrier function Effects 0.000 claims 3
- 210000001218 blood-brain barrier Anatomy 0.000 claims 3
- 230000002060 circadian Effects 0.000 claims 3
- 150000004292 cyclic ethers Chemical class 0.000 claims 3
- 230000002349 favourable effect Effects 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 208000011580 syndromic disease Diseases 0.000 claims 3
- 208000007590 Disorders of Excessive Somnolence Diseases 0.000 claims 2
- 108090000371 Esterases Proteins 0.000 claims 2
- 102000000543 Histamine Receptors Human genes 0.000 claims 2
- 108010002059 Histamine Receptors Proteins 0.000 claims 2
- 208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 claims 2
- 125000001931 aliphatic group Chemical group 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- -1 carboxylate anion Chemical class 0.000 claims 2
- 125000002843 carboxylic acid group Chemical group 0.000 claims 2
- 150000001735 carboxylic acids Chemical class 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 125000000582 cycloheptyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
- 230000003247 decreasing effect Effects 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 206010020765 hypersomnia Diseases 0.000 claims 2
- 230000000147 hypnotic effect Effects 0.000 claims 2
- 238000001727 in vivo Methods 0.000 claims 2
- 206010022437 insomnia Diseases 0.000 claims 2
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 2
- 102000005962 receptors Human genes 0.000 claims 2
- 108020003175 receptors Proteins 0.000 claims 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- 206010000117 Abnormal behaviour Diseases 0.000 claims 1
- 208000019888 Circadian rhythm sleep disease Diseases 0.000 claims 1
- 206010010904 Convulsion Diseases 0.000 claims 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 1
- 208000001456 Jet Lag Syndrome Diseases 0.000 claims 1
- 206010040981 Sleep attacks Diseases 0.000 claims 1
- 150000007513 acids Chemical class 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 150000001298 alcohols Chemical class 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- 230000001078 anti-cholinergic effect Effects 0.000 claims 1
- 230000001022 anti-muscarinic effect Effects 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 230000007850 degeneration Effects 0.000 claims 1
- 230000008030 elimination Effects 0.000 claims 1
- 238000003379 elimination reaction Methods 0.000 claims 1
- NBVXSUQYWXRMNV-UHFFFAOYSA-N fluoromethane Chemical compound FC NBVXSUQYWXRMNV-UHFFFAOYSA-N 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 230000007062 hydrolysis Effects 0.000 claims 1
- 238000006460 hydrolysis reaction Methods 0.000 claims 1
- 230000006698 induction Effects 0.000 claims 1
- 230000008595 infiltration Effects 0.000 claims 1
- 238000001764 infiltration Methods 0.000 claims 1
- 238000002955 isolation Methods 0.000 claims 1
- 208000033915 jet lag type circadian rhythm sleep disease Diseases 0.000 claims 1
- 230000003204 osmotic effect Effects 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 208000033914 shift work type circadian rhythm sleep disease Diseases 0.000 claims 1
- 201000002859 sleep apnea Diseases 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- OWQUZNMMYNAXSL-UHFFFAOYSA-N CN(CC1)CCC1OC(c1ccccc1)c1ccccc1 Chemical compound CN(CC1)CCC1OC(c1ccccc1)c1ccccc1 OWQUZNMMYNAXSL-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US32970101P | 2001-10-16 | 2001-10-16 | |
| US38150702P | 2002-05-17 | 2002-05-17 | |
| US41424302P | 2002-09-27 | 2002-09-27 | |
| PCT/US2002/032970 WO2003032912A2 (en) | 2001-10-16 | 2002-10-16 | Treatment of cns disorders using cns target modulators |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2005529840A JP2005529840A (ja) | 2005-10-06 |
| JP2005529840A5 true JP2005529840A5 (enExample) | 2006-01-05 |
Family
ID=29716072
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003535718A Pending JP2005529840A (ja) | 2001-10-16 | 2002-10-16 | Ｃｎｓ標的モジュレータを使用するｃｎｓ障害の治療 |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US20050009730A1 (enExample) |
| EP (1) | EP1443929A4 (enExample) |
| JP (1) | JP2005529840A (enExample) |
| AU (1) | AU2002347906A2 (enExample) |
| CA (1) | CA2463579A1 (enExample) |
| WO (1) | WO2003032912A2 (enExample) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7344702B2 (en) | 2004-02-13 | 2008-03-18 | Bristol-Myers Squibb Pharma Company | Contrast agents for myocardial perfusion imaging |
| US7355042B2 (en) * | 2001-10-16 | 2008-04-08 | Hypnion, Inc. | Treatment of CNS disorders using CNS target modulators |
| KR100579813B1 (ko) * | 2001-10-16 | 2006-05-12 | 주식회사 에스티씨나라 | 피페리딘 유도체, 이의 제조방법 및 이를 포함하는 치매치료용 약학적 조성물 |
| JP4550353B2 (ja) * | 2002-07-24 | 2010-09-22 | 株式会社医薬分子設計研究所 | 造血器型プロスタグランジンｄ２合成酵素阻害剤 |
| US20070173486A1 (en) * | 2003-05-01 | 2007-07-26 | Vernalis Research Limited | Azetidinecarboxamide derivatives and their use in the treatment of cb1 receptor mediated disordrs |
| GB0312419D0 (en) * | 2003-05-30 | 2003-07-02 | Boots Healthcare Int Ltd | Use of a compound in the treatment of sleep disorders and the like, in providing refreshedness on waking and a method for the treatment of grogginess |
| EP1644373A1 (en) * | 2003-06-27 | 2006-04-12 | Janssen Pharmaceutica N.V. | Tricyclic delta opioid modulators |
| US7482460B2 (en) | 2003-12-10 | 2009-01-27 | Hypnion, Inc. | Doxepin analogs and methods of use thereof |
| US7326721B2 (en) | 2003-12-10 | 2008-02-05 | Hypnion, Inc. | Doxepin analogs and methods of use thereof |
| US7411069B2 (en) | 2003-12-10 | 2008-08-12 | Hypnion, Inc. | Doxepin analogs and methods of use thereof |
| WO2005102335A2 (en) | 2004-04-23 | 2005-11-03 | Hypnion, Inc. | Methods of treating sleep disorders |
| US7485283B2 (en) * | 2004-04-28 | 2009-02-03 | Lantheus Medical Imaging | Contrast agents for myocardial perfusion imaging |
| US20080287531A1 (en) * | 2004-07-16 | 2008-11-20 | Kyowa Hakko Co., Ltd. | Preventive and/or Therapeutic Agent for Sleeping Disorder |
| US7807828B2 (en) * | 2005-08-11 | 2010-10-05 | Hypnion, Inc. | Olanzapine analogs and methods of use thereof |
| JP5179486B2 (ja) * | 2006-06-28 | 2013-04-10 | アムジエン・インコーポレーテツド | グリシン輸送体−１阻害剤 |
| AU2007301145B2 (en) * | 2006-09-29 | 2012-12-13 | Nippon Zoki Pharmaceutical Co., Ltd. | Oxepin derivative |
| EP2231601B1 (en) | 2007-12-12 | 2014-06-18 | Amgen Inc. | Glycine transporter-1 inhibitors |
| DK2257315T3 (da) | 2008-02-29 | 2020-01-27 | Lantheus Medical Imaging Inc | Kontrastmidler til anvendelser omfattende perfusionsbilleddannelse |
| JP5662416B2 (ja) | 2009-04-15 | 2015-01-28 | ランセウス メディカル イメージング， インコーポレイテッド | アスコルビン酸による放射性医薬組成物の安定化 |
| CN101838234B (zh) * | 2009-06-17 | 2012-02-08 | 重庆华邦制药股份有限公司 | 阿法乙酯衍生物的合成方法 |
| TWI664169B (zh) | 2010-02-08 | 2019-07-01 | 藍瑟斯醫學影像公司 | 用於合成造影劑及其中間體之方法及裝置 |
| CN102311381A (zh) * | 2010-07-06 | 2012-01-11 | 重庆华邦胜凯制药有限公司 | 阿伐乙酯衍生物的合成方法 |
| CA3189252A1 (en) | 2012-01-18 | 2013-11-21 | Techfields Pharma Co., Ltd. | High penetration prodrug compositions and pharmaceutical composition thereof for treatment of pulmonary conditions |
| AU2013203000B9 (en) | 2012-08-10 | 2017-02-02 | Lantheus Medical Imaging, Inc. | Compositions, methods, and systems for the synthesis and use of imaging agents |
| CN104447516B (zh) * | 2014-12-15 | 2017-05-31 | 重庆华邦制药有限公司 | 一种阿伐斯丁的制备方法 |
| CN107635549A (zh) | 2015-03-26 | 2018-01-26 | 杰奎琳·M·艾弗森 | 抑制与宿醉相关的症状的方法和组合物 |
| WO2017178820A1 (en) | 2016-04-15 | 2017-10-19 | Oxford University Innovation Limited | Adenosine receptor modulators for the treatment of circadian rhythm disorders |
| EP3391886A1 (en) | 2017-04-19 | 2018-10-24 | Novartis AG | The use of a h3r inverse agonist for the treatment of shift work disorder |
| CN108558860B (zh) * | 2018-06-04 | 2020-12-25 | 成都伊诺达博医药科技有限公司 | 一种合成芜地溴铵的方法 |
| CN110903182A (zh) * | 2018-09-14 | 2020-03-24 | 北京艾德旺科技发展有限公司 | 简单环保的4-氟-2-甲基苯甲酸的化学合成方法 |
| CN114929688B (zh) | 2019-10-21 | 2024-11-01 | 阿莱瑞恩公司 | 作为H1和5-HT2A-受体调节剂、用于治疗睡眠障碍的3-(4-(11H-二苯并[b,e][1,4]吖庚英-6-基)哌嗪-1-基)-和3-(4-(二苯并[b,f][1,4]氧杂吖庚英/硫杂吖庚英/二吖庚英-11-基)哌嗪-1-基)-丙酸衍生物 |
| EP4333821A4 (en) * | 2021-05-04 | 2025-07-09 | Texas A & M Univ Sys | SARS-COV-2 INHIBITORS |
Family Cites Families (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3045023A (en) * | 1960-04-06 | 1962-07-17 | Searle & Co | Dialkylaminoethyl diphenylmethylpiperidinepropionates |
| US4072756A (en) * | 1973-05-17 | 1978-02-07 | Sandoz Ltd. | Tricyclo piperidino ketones and soporific compositions thereof |
| US4383999A (en) * | 1981-05-26 | 1983-05-17 | Smithkline Beckman Corporation | Inhibition of GABA uptake by N-substituted azaheterocyclic carboxylic acids and their esters |
| US4514414A (en) * | 1982-10-25 | 1985-04-30 | Smithkline Beckman Corporation | N-Substituted pyrrolidineacetic acids and their esters |
| US4610995A (en) * | 1984-07-27 | 1986-09-09 | Coker Geoffrey G | Certain 1,1-diaryl-propenyl-3-(1-pyrrolidino-2-carboxylic acids, derivatives thereof and their anti-histaminic properties |
| NO170976C (no) * | 1986-01-07 | 1993-01-06 | Novo Nordisk As | Analogifremgangsmaate for fremstilling av terapeutisk aktive fenylbuten-syrederivater |
| US5231105A (en) * | 1987-06-02 | 1993-07-27 | Ajinomoto Co., Inc. | Ethylamine derivatives and antihypertensives containing the same |
| US4829064A (en) * | 1987-06-08 | 1989-05-09 | Analgesic Associates | Cough/cold mixtures comprising non-sedating antihistamine drugs |
| US4929618A (en) | 1988-03-25 | 1990-05-29 | Ube Industries, Ltd. | Piperdine and piperazine derivatives, and antihistaminic pharmaceutical compositions containing the same |
| US5250681A (en) * | 1988-06-02 | 1993-10-05 | Ajinomoto Co., Inc. | Piperidine derivatives and hypotensives containing the same |
| US5393890A (en) * | 1988-06-02 | 1995-02-28 | Ajinomoto Co., Inc. | Piperidine derivatives and hypotensives containing the same |
| JPH0812127B2 (ja) * | 1988-11-11 | 1996-02-07 | オリンパス光学工業株式会社 | 曲率半径測定装置及び方法 |
| CA2015949A1 (en) | 1989-05-22 | 1990-11-22 | Yasuo Ito | Piperidine derivative, method for preparation thereof, and a pharmaceutical composition comprising the same |
| AU620996B2 (en) | 1989-07-04 | 1992-02-27 | Hokuriku Pharmaceutical Co. Ltd. | 4-{(dibenzocycloheptene) or (dibenzoxepin)}-1-substituted piperidines |
| JPH03133956A (ja) * | 1989-10-20 | 1991-06-07 | Hokuriku Seiyaku Co Ltd | ピペリジン誘導体 |
| JP2624372B2 (ja) * | 1990-11-15 | 1997-06-25 | 宇部興産株式会社 | ジアリールメトキシピペリジン誘導体 |
| JPH0517442A (ja) | 1991-07-05 | 1993-01-26 | Hokuriku Seiyaku Co Ltd | ピペリジン誘導体 |
| JPH0517443A (ja) | 1991-07-11 | 1993-01-26 | Hokuriku Seiyaku Co Ltd | ピペリジン誘導体 |
| JP2625294B2 (ja) | 1991-10-08 | 1997-07-02 | 宇部興産株式会社 | ピペリジン誘導体 |
| JP3338913B2 (ja) | 1993-06-29 | 2002-10-28 | 大鵬薬品工業株式会社 | テトラゾール誘導体 |
| US5801175A (en) * | 1995-04-07 | 1998-09-01 | Schering Corporation | Tricyclic compounds useful for inhibition of G-protein function and for treatment of proliferative diseases |
| IL117798A (en) | 1995-04-07 | 2001-11-25 | Schering Plough Corp | Tricyclic compounds useful for inhibiting the function of protein - G and for the treatment of malignant diseases, and pharmaceutical preparations containing them |
| WO1997017073A1 (en) * | 1995-11-03 | 1997-05-15 | Novo Nordisk A/S | A method of treating filariae |
| CN1327383A (zh) | 1996-05-31 | 2001-12-19 | 阿列里克斯神经科学公司 | 治疗神经和神经精神障碍的药物 |
| US6191165B1 (en) * | 1996-05-31 | 2001-02-20 | Allelix Neuroscience Inc. | Pharmaceutical for treatment of neurological and neuropsychiatric disorders |
| TW486475B (en) | 1996-12-26 | 2002-05-11 | Ube Industries | Acid addition salt of optically active piperidine compound and process for preparing the same |
| EP0991633A1 (en) | 1997-06-25 | 2000-04-12 | Novo Nordisk A/S | Novel heterocyclic compounds |
| US6288083B1 (en) * | 1998-09-04 | 2001-09-11 | Millennium Pharmaceuticals, Inc. | Chemokine receptor antagonists and methods of use therefor |
| US6503926B2 (en) * | 1998-09-04 | 2003-01-07 | Millennium Pharmaceuticals, Inc. | Chemokine receptor antagonists and methods of use therefor |
| DE19840611A1 (de) | 1998-09-05 | 2000-03-09 | Klaus Wanner | GABA-uptake-Inhibitoren mit Pyrrolidinstruktur |
| US6387930B1 (en) * | 1999-05-04 | 2002-05-14 | Schering Corporation | Piperidine derivatives useful as CCR5 antagonists |
| JP2003506483A (ja) * | 1999-08-13 | 2003-02-18 | ベラ・ファーマシューティカルズ・インコーポレイテッド | シクロベンザプリンおよびその組成物による全般性不安障害の処置 |
| JP3909998B2 (ja) | 2000-03-22 | 2007-04-25 | 田辺製薬株式会社 | 経口投与製剤 |
| KR100579813B1 (ko) | 2001-10-16 | 2006-05-12 | 주식회사 에스티씨나라 | 피페리딘 유도체, 이의 제조방법 및 이를 포함하는 치매치료용 약학적 조성물 |
| JP4550353B2 (ja) | 2002-07-24 | 2010-09-22 | 株式会社医薬分子設計研究所 | 造血器型プロスタグランジンｄ２合成酵素阻害剤 |
-
2002
- 2002-10-16 EP EP02784116A patent/EP1443929A4/en not_active Withdrawn
- 2002-10-16 WO PCT/US2002/032970 patent/WO2003032912A2/en not_active Ceased
- 2002-10-16 CA CA002463579A patent/CA2463579A1/en not_active Abandoned
- 2002-10-16 AU AU2002347906A patent/AU2002347906A2/en not_active Abandoned
- 2002-10-16 JP JP2003535718A patent/JP2005529840A/ja active Pending
- 2002-10-16 US US10/492,990 patent/US20050009730A1/en not_active Abandoned
-
2003
- 2003-12-04 US US10/728,340 patent/US7317026B2/en not_active Expired - Fee Related
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