JP2009507034A5 - - Google Patents
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- Publication number
- JP2009507034A5 JP2009507034A5 JP2008529336A JP2008529336A JP2009507034A5 JP 2009507034 A5 JP2009507034 A5 JP 2009507034A5 JP 2008529336 A JP2008529336 A JP 2008529336A JP 2008529336 A JP2008529336 A JP 2008529336A JP 2009507034 A5 JP2009507034 A5 JP 2009507034A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- optionally substituted
- moiety
- fluoro substituents
- 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 572
- 125000001153 fluoro group Chemical group F* 0.000 claims 507
- 125000001424 substituent group Chemical group 0.000 claims 108
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 97
- 125000000753 cycloalkyl group Chemical group 0.000 claims 84
- -1 -SCFThree Chemical group 0.000 claims 32
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 29
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 29
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 24
- 125000004093 cyano group Chemical group *C#N 0.000 claims 21
- 125000005843 halogen group Chemical group 0.000 claims 21
- 125000004076 pyridyl group Chemical group 0.000 claims 20
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 15
- 229910052739 hydrogen Inorganic materials 0.000 claims 14
- 239000001257 hydrogen Substances 0.000 claims 14
- 125000005034 trifluormethylthio group Chemical group FC(S*)(F)F 0.000 claims 14
- 150000003839 salts Chemical class 0.000 claims 12
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical group [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 10
- 150000001875 compounds Chemical class 0.000 claims 10
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims 9
- 125000003545 alkoxy group Chemical group 0.000 claims 6
- 125000000842 isoxazolyl group Chemical group 0.000 claims 6
- 125000002971 oxazolyl group Chemical group 0.000 claims 6
- 125000000168 pyrrolyl group Chemical group 0.000 claims 6
- 125000000335 thiazolyl group Chemical group 0.000 claims 6
- 125000001544 thienyl group Chemical group 0.000 claims 6
- 239000003085 diluting agent Substances 0.000 claims 5
- 125000001786 isothiazolyl group Chemical group 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 239000000546 pharmaceutical excipient Substances 0.000 claims 5
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 5
- 229910052799 carbon Inorganic materials 0.000 claims 4
- 150000001721 carbon Chemical group 0.000 claims 4
- 125000004502 1,2,3-oxadiazolyl group Chemical group 0.000 claims 3
- 125000001399 1,2,3-triazolyl group Chemical group N1N=NC(=C1)* 0.000 claims 3
- 125000004504 1,2,4-oxadiazolyl group Chemical group 0.000 claims 3
- 125000004514 1,2,4-thiadiazolyl group Chemical group 0.000 claims 3
- 125000001376 1,2,4-triazolyl group Chemical group N1N=C(N=C1)* 0.000 claims 3
- 125000004506 1,2,5-oxadiazolyl group Chemical group 0.000 claims 3
- 125000004517 1,2,5-thiadiazolyl group Chemical group 0.000 claims 3
- 125000001781 1,3,4-oxadiazolyl group Chemical group 0.000 claims 3
- 125000004520 1,3,4-thiadiazolyl group Chemical group 0.000 claims 3
- 239000003937 drug carrier Substances 0.000 claims 3
- 125000002541 furyl group Chemical group 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 125000002883 imidazolyl group Chemical group 0.000 claims 3
- 125000002757 morpholinyl group Chemical group 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
- 150000002926 oxygen Chemical class 0.000 claims 3
- 125000003386 piperidinyl group Chemical group 0.000 claims 3
- 125000003226 pyrazolyl group Chemical group 0.000 claims 3
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 3
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 3
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 3
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 3
- 125000004568 thiomorpholinyl group Chemical group 0.000 claims 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 3
- 125000006526 (C1-C2) alkyl group Chemical group 0.000 claims 2
- 125000004511 1,2,3-thiadiazolyl group Chemical group 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 150000002431 hydrogen Chemical group 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 1
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims 1
- JGAPDRYDUPAXTC-UHFFFAOYSA-N 4-[4-[[(7-chloro-2,3,4,5-tetrahydro-1h-3-benzazepin-6-yl)amino]methyl]phenyl]-n-(cyclopropylmethyl)-1,3-thiazol-2-amine Chemical compound ClC1=CC=C2CCNCCC2=C1NCC(C=C1)=CC=C1C(N=1)=CSC=1NCC1CC1 JGAPDRYDUPAXTC-UHFFFAOYSA-N 0.000 claims 1
- BMNAANNLKHAPHJ-UHFFFAOYSA-N 7-chloro-n-[[4-(piperidin-1-ylmethyl)phenyl]methyl]-2,3,4,5-tetrahydro-1h-3-benzazepin-6-amine Chemical compound ClC1=CC=C2CCNCCC2=C1NCC(C=C1)=CC=C1CN1CCCCC1 BMNAANNLKHAPHJ-UHFFFAOYSA-N 0.000 claims 1
- 208000019901 Anxiety disease Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 208000021384 Obsessive-Compulsive disease Diseases 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000004414 alkyl thio group Chemical group 0.000 claims 1
- 230000036506 anxiety Effects 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 125000000118 dimethyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000001475 halogen functional group Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP05380191 | 2005-09-01 | ||
| EP05380191.6 | 2005-09-01 | ||
| US73108105P | 2005-10-28 | 2005-10-28 | |
| US60/731,081 | 2005-10-28 | ||
| PCT/US2006/034335 WO2007028083A2 (en) | 2005-09-01 | 2006-09-01 | 6-arylalkylamino- 2,3,4,5-tetrahydro-1h-benzo[d]azepines as 5-ht2c receptor agonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2009507034A JP2009507034A (ja) | 2009-02-19 |
| JP2009507034A5 true JP2009507034A5 (enExample) | 2009-10-15 |
| JP5155864B2 JP5155864B2 (ja) | 2013-03-06 |
Family
ID=39892208
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008529336A Expired - Fee Related JP5155864B2 (ja) | 2005-09-01 | 2006-09-01 | ５−ＨＴ２Ｃ受容体アゴニストとしての６−アリールアルキルアミノ−２，３，４，５−テトラヒドロ−１Ｈ−ベンゾ［ｄ］アゼピン |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US20080269196A1 (enExample) |
| EP (1) | EP1924561B1 (enExample) |
| JP (1) | JP5155864B2 (enExample) |
| CN (1) | CN101258131B (enExample) |
| AU (1) | AU2006287202B2 (enExample) |
| BR (1) | BRPI0615048A2 (enExample) |
| CA (1) | CA2619448C (enExample) |
| DK (1) | DK1924561T3 (enExample) |
| ES (1) | ES2397400T3 (enExample) |
| PL (1) | PL1924561T3 (enExample) |
| PT (1) | PT1924561E (enExample) |
| SI (1) | SI1924561T1 (enExample) |
| WO (1) | WO2007028083A2 (enExample) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0615033A2 (pt) * | 2005-09-01 | 2011-04-26 | Lilly Co Eli | composto, composição farmacêutica, e, uso de um composto |
| WO2007028132A2 (en) * | 2005-09-01 | 2007-03-08 | Eli Lilly And Company | 6-N-LINKED HETEROCYCLE-SUBSTITUTED 2,3,4,5-TETRAHYDRO-1H-BENZO[d]AZEPINES AS 5-HT2C RECEPTOR AGONISTS |
| EP2727585A1 (en) | 2006-05-16 | 2014-05-07 | Takeda Pharmaceutical Company Limited | In-vivo screening method |
| WO2007140213A1 (en) | 2006-05-26 | 2007-12-06 | Forest Laboratories Holdings Limited | Pyridoazepine derivatives |
| US20100266504A1 (en) | 2007-11-15 | 2010-10-21 | Takahiro Matsumoto | Condensed pyridine derivative and use thereof |
| JP5216912B2 (ja) | 2008-04-29 | 2013-06-19 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ｃｃｒ１受容体拮抗薬としてのインダゾール化合物 |
| EP2297112B1 (en) | 2008-05-06 | 2013-04-03 | Boehringer Ingelheim International GmbH | Pyrazole compounds as ccr1 antagonists |
| MX2011002951A (es) | 2008-09-26 | 2011-04-26 | Boehringer Ingelheim Int | Compuestos de azaindazol como antagonistas del receptor de ccr1. |
| MX2012004644A (es) | 2009-10-21 | 2012-05-08 | Boehringer Ingelheim Int | Compuestos de indazol y pirazolopiridina como antagonistas del receptor de ccr1. |
| WO2011056440A1 (en) | 2009-10-27 | 2011-05-12 | Boehringer Ingelheim International Gmbh | Heterocyclic compounds as ccr1 receptor antagonists |
| JP2013512954A (ja) * | 2009-12-08 | 2013-04-18 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 置換インダゾール及びアザインダゾール化合物の生成に有効な中間体の合成方法 |
| WO2011137109A1 (en) | 2010-04-30 | 2011-11-03 | Boehringer Ingelheim International Gmbh | Azaindazole amide compounds as ccr1 receptor antagonists |
| US20130267500A1 (en) | 2010-09-01 | 2013-10-10 | Arena Pharmaceuticals, Inc. | 5-ht2c receptor agonists in the treatment of disorders ameliorated by reduction of norepinephrine level |
| EP2655371B1 (en) | 2010-12-23 | 2015-02-25 | Boehringer Ingelheim International GmbH | Pyrazolopiperidine compounds as ccr1 receptor antagonists |
| JP6440625B2 (ja) | 2012-11-14 | 2018-12-19 | ザ・ジョンズ・ホプキンス・ユニバーシティー | 精神分裂病を処置するための方法および組成物 |
| WO2015066344A1 (en) | 2013-11-01 | 2015-05-07 | Arena Pharmaceuticals, Inc. | 5-ht2c receptor agonists and compositions and methods of use |
| SG11201610975RA (en) * | 2014-07-03 | 2017-01-27 | Celgene Quanticel Res Inc | Inhibitors of lysine specific demethylase-1 |
| CN105622511B (zh) * | 2014-11-03 | 2018-01-23 | 北京瑞都医药科技有限公司 | 一种减肥药物及其制备方法 |
| CN109071440A (zh) * | 2016-05-13 | 2018-12-21 | 日产化学株式会社 | 2-乙酰基吡啶化合物的制造方法 |
| US20210052600A1 (en) | 2017-12-27 | 2021-02-25 | Takeda Pharmaceutical Company Limited | Therapeutic agents for stress urinary incontinence and incotinence of feces |
| AU2020416203A1 (en) * | 2020-01-03 | 2022-06-16 | Blue Oak Pharmaceuticals, Inc. | Compounds and compositions for treating CNS disorders |
| CN114163426B (zh) * | 2020-09-10 | 2024-03-19 | 上海爱博医药科技有限公司 | 苯并含氧杂环类化合物及其医药应用 |
| GB202101734D0 (en) | 2021-02-08 | 2021-03-24 | Cerevance Inc | Novel Compounds |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4265890A (en) * | 1978-07-07 | 1981-05-05 | Smithkline Corporation | 6-Phenyl thio- and 6-cyclohexyl thio-2,3,4,5-tetrahydro-1H-3-benzazepines |
| US5023252A (en) | 1985-12-04 | 1991-06-11 | Conrex Pharmaceutical Corporation | Transdermal and trans-membrane delivery of drugs |
| EP0285287A3 (en) | 1987-03-23 | 1990-08-16 | Smithkline Beecham Corporation | 3-benzazepine compounds for use in treating gastrointestinal motility disorders |
| US4985352A (en) * | 1988-02-29 | 1991-01-15 | The Trustees Of Columbia University In The City Of New York | DNA encoding serotonin 1C (5HT1c) receptor, isolated 5HT1c receptor, mammalian cells expressing same and uses thereof |
| US5011472A (en) | 1988-09-06 | 1991-04-30 | Brown University Research Foundation | Implantable delivery system for biological factors |
| GB9116824D0 (en) | 1991-08-05 | 1991-09-18 | Smithkline Beecham Corp | Chemical compounds |
| US5639748A (en) * | 1991-08-05 | 1997-06-17 | Smithkline Beecham Corporation | 6,9-disubstituted benzazepines having α-adrenoceptor blocking activity |
| WO1993004866A1 (fr) | 1991-09-11 | 1993-03-18 | Canon Kabushiki Kaisha | Element de nettoyage ameliore pour tete de jet d'encre et dispositif a jet d'encre equipe d'un tel element de nettoyage |
| GB9119467D0 (en) | 1991-09-12 | 1991-10-23 | Smithkline Beecham Corp | Chemical compounds |
| US5698766A (en) * | 1995-04-05 | 1997-12-16 | The Regents Of The University Of California | Transgenic animal model for testing drugs for treating eating disorders and epilepsy |
| EP1213017A3 (en) | 2000-12-05 | 2003-11-12 | Akzo Nobel N.V. | Use of a 5-HT2C receptor agonist for the treatment of hot flushes |
| JPWO2002074746A1 (ja) * | 2001-03-16 | 2004-07-08 | 山之内製薬株式会社 | ベンゾアゼピン誘導体 |
| DE60206762T2 (de) | 2001-07-13 | 2006-07-13 | Pharmacia & Upjohn Co. Llc, Kalamazoo | Hexahydroazepino(4,5-g)indole und -indoline als 5-ht rezeptor-liganden |
| CA2468010A1 (en) | 2001-11-28 | 2003-06-05 | Pharmacia & Upjohn Company | Benzazepine derivatives and their use as 5-ht ligands |
| US6953787B2 (en) | 2002-04-12 | 2005-10-11 | Arena Pharmaceuticals, Inc. | 5HT2C receptor modulators |
| JP4782003B2 (ja) | 2003-06-17 | 2011-09-28 | アリーナ ファーマシューティカルズ， インコーポレイテッド | ５ｈｔ２ｃレセプター関連疾患の処置に有用なベンズアゼピン誘導体 |
| DK2332921T3 (en) | 2003-06-17 | 2016-05-09 | Arena Pharm Inc | 8-Chloro-1-methyl-2,3,4,5-tetrahydro-1H-3benzazepine hydrochloride |
| TW200510324A (en) | 2003-08-11 | 2005-03-16 | Lilly Co Eli | 6-(2,2,2-trifluoroethylamino)-7-chiloro-2, 3, 4, 5-tetrahydro-1h-benzo[d]azepine as a 5-ht2c receptor agonist |
| US20070275949A1 (en) | 2003-10-22 | 2007-11-29 | Arena Pharmaceuticals, Inc. | Benzazepine Derivatives and Methods of Prophylaxis or Treatment of 5Ht2C Receptor Associated Diseases |
| WO2005042491A1 (en) * | 2003-10-22 | 2005-05-12 | Arena Pharmaceuticals, Inc. | Benzazepine derivatives and methods of prophylaxis or treatment of 5ht2c receptor associated diseases |
| EP2479168B1 (en) * | 2004-02-25 | 2014-04-09 | Eli Lilly And Company | 6-Substituted 2,3,4,5-Tetrahydro-1H-Benzo [d]Azepines as 5-HT2C Receptor Agonists |
| RS50996B (sr) | 2004-12-21 | 2010-10-31 | Arena Pharmaceuticals Inc. | Kristalni oblici (r)-8-hloro-1-metil-2,3,4,5-tetrahidro-1h-benzazepin hlorhidrat |
| KR101519441B1 (ko) | 2004-12-23 | 2015-05-12 | 아레나 파마슈티칼스, 인크. | 5ｈｔ２ｃ 수용체 조정물질 조성물 및 그의 사용 방법 |
| BRPI0615033A2 (pt) * | 2005-09-01 | 2011-04-26 | Lilly Co Eli | composto, composição farmacêutica, e, uso de um composto |
-
2006
- 2006-09-01 ES ES06802859T patent/ES2397400T3/es active Active
- 2006-09-01 CN CN2006800322352A patent/CN101258131B/zh not_active Expired - Fee Related
- 2006-09-01 WO PCT/US2006/034335 patent/WO2007028083A2/en not_active Ceased
- 2006-09-01 US US11/996,751 patent/US20080269196A1/en not_active Abandoned
- 2006-09-01 PT PT68028596T patent/PT1924561E/pt unknown
- 2006-09-01 BR BRPI0615048-9A patent/BRPI0615048A2/pt not_active IP Right Cessation
- 2006-09-01 EP EP06802859A patent/EP1924561B1/en not_active Not-in-force
- 2006-09-01 DK DK06802859.6T patent/DK1924561T3/da active
- 2006-09-01 SI SI200631496T patent/SI1924561T1/sl unknown
- 2006-09-01 PL PL06802859T patent/PL1924561T3/pl unknown
- 2006-09-01 JP JP2008529336A patent/JP5155864B2/ja not_active Expired - Fee Related
- 2006-09-01 CA CA2619448A patent/CA2619448C/en not_active Expired - Fee Related
- 2006-09-01 AU AU2006287202A patent/AU2006287202B2/en not_active Ceased
-
2011
- 2011-06-09 US US13/156,575 patent/US8680091B2/en not_active Expired - Fee Related
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