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 (https=) | 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 (https=) |
| EP (1) | EP1443929A4 (https=) |
| JP (1) | JP2005529840A (https=) |
| AU (1) | AU2002347906A2 (https=) |
| CA (1) | CA2463579A1 (https=) |
| WO (1) | WO2003032912A2 (https=) |
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 |
| JP2006525299A (ja) * | 2003-05-01 | 2006-11-09 | ヴァーナリス リサーチ リミテッド | アゼチジンカルボキサミド誘導体及びｃｂ１レセプター媒介障害の治療におけるその使用 |
| 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 |
| US7589103B2 (en) * | 2003-06-27 | 2009-09-15 | Janssen Pharmaceutica N.V. | Tricyclic-bridged piperidinylidene derivatives as 8-opioid modulators |
| US7482460B2 (en) | 2003-12-10 | 2009-01-27 | 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 |
| US7326721B2 (en) | 2003-12-10 | 2008-02-05 | 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 |
| KR20070032785A (ko) * | 2004-07-16 | 2007-03-22 | 교와 핫꼬 고교 가부시끼가이샤 | 수면 장해의 예방 및/또는 치료제 |
| US7807828B2 (en) * | 2005-08-11 | 2010-10-05 | Hypnion, Inc. | Olanzapine analogs and methods of use thereof |
| NZ573129A (en) * | 2006-06-28 | 2011-06-30 | Amgen Inc | Piperazine acetic acid glycine transporter-1 inhibitors |
| US8222419B2 (en) * | 2006-09-29 | 2012-07-17 | Nippon Zoki Pharmaceutical Co., Ltd. | Oxepin derivative |
| EP2231601B1 (en) | 2007-12-12 | 2014-06-18 | Amgen Inc. | Glycine transporter-1 inhibitors |
| AU2009220244B2 (en) | 2008-02-29 | 2014-10-09 | Lantheus Medical Imaging, Inc. | Contrast agents for applications including perfusion imaging |
| KR101602992B1 (ko) | 2009-04-15 | 2016-03-11 | 랜티우스 메디컬 이메징, 인크. | 아스코르브산을 사용한 방사성 약제 조성물의 안정화 |
| 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 |
| CN102858752B (zh) | 2010-02-08 | 2018-10-16 | 兰休斯医疗成像公司 | 用于合成显像剂和其中间体的方法和装置 |
| 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 |
| CN116898848A (zh) | 2012-01-18 | 2023-10-20 | 苏州泰飞尔医药有限公司 | 治疗肺部疾病的高穿透力前药组合物和医药组合物 |
| 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 |
| US10420756B2 (en) | 2015-03-26 | 2019-09-24 | Sen-Jam Pharmaceutical Llc. | Methods and compositions to inhibit symptoms associated with veisalgia |
| ES2957548T3 (es) | 2016-04-15 | 2024-01-22 | Univ Oxford Innovation Ltd | Moduladores del receptor de adenosina para el tratamiento de los trastornos del ritmo circadiano |
| 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 |
| JP7696354B2 (ja) | 2019-10-21 | 2025-06-20 | アライリオン インコーポレイテッド | 睡眠障害の治療のためのＨ１および５－ＨＴ２Ａ受容体調節物質としての３－（４－（１１Ｈ－ジベンゾ［ｂ，ｅ］［１，４］アゼピン－６－イル）ピペラジン－１－イル）－プロパン酸誘導体および３－（４－（ジベンゾ［ｂ，ｆ］［１，４］オキサゼピン／チアゼピン／ジアゼピン－１１－イル）ピペラジン－１－イル）－プロパン酸誘導体 |
| 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 |
| EP0231996B1 (en) * | 1986-01-07 | 1993-10-06 | Novo Nordisk A/S | Novel amino acid derivatives |
| 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 |
| US5095022A (en) * | 1989-07-04 | 1992-03-10 | Hokuriku Pharmaceutical Co., Ltd. | Piperidine derivatives and pharmaceutical compositions comprising the same |
| 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 |
| NZ332780A (en) | 1996-05-31 | 2000-07-28 | Allelix Neuroscience Inc | Substituted amines for the treatment of neurological and neuropsychiatric disorders |
| 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 |
| WO1999000376A1 (en) | 1997-06-25 | 1999-01-07 | Novo Nordisk A/S | Novel heterocyclic compounds |
| US6503926B2 (en) * | 1998-09-04 | 2003-01-07 | Millennium Pharmaceuticals, Inc. | Chemokine receptor antagonists and methods of use therefor |
| US6288083B1 (en) * | 1998-09-04 | 2001-09-11 | 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 |
| BR0013122A (pt) * | 1999-08-13 | 2002-04-30 | Vela Pharmaceuticals Inc | Ciclobenzaprina para tratamento de distúrbio de ansiedade generalizado e composições de ciclobenzaprina |
| 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 AU AU2002347906A patent/AU2002347906A2/en not_active Abandoned
- 2002-10-16 US US10/492,990 patent/US20050009730A1/en not_active Abandoned
- 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 EP EP02784116A patent/EP1443929A4/en not_active Withdrawn
- 2002-10-16 JP JP2003535718A patent/JP2005529840A/ja active Pending
-
2003
- 2003-12-04 US US10/728,340 patent/US7317026B2/en not_active Expired - Fee Related
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