JP2005525392A5 - - Google Patents
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- Publication number
- JP2005525392A5 JP2005525392A5 JP2003580300A JP2003580300A JP2005525392A5 JP 2005525392 A5 JP2005525392 A5 JP 2005525392A5 JP 2003580300 A JP2003580300 A JP 2003580300A JP 2003580300 A JP2003580300 A JP 2003580300A JP 2005525392 A5 JP2005525392 A5 JP 2005525392A5
- Authority
- JP
- Japan
- Prior art keywords
- ring
- substituted
- cyclopropyl
- thienyl
- phenyl
- 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
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 15
- 125000001544 thienyl group Chemical group 0.000 claims 15
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 14
- 125000001424 substituent group Chemical group 0.000 claims 13
- 125000004432 carbon atom Chemical group C* 0.000 claims 10
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 10
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 9
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 9
- 229910052760 oxygen Inorganic materials 0.000 claims 7
- 125000001054 5 membered carbocyclic group Chemical group 0.000 claims 5
- 125000004008 6 membered carbocyclic group Chemical group 0.000 claims 5
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 125000005842 heteroatom Chemical group 0.000 claims 5
- 125000000623 heterocyclic group Chemical group 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 229910052717 sulfur Inorganic materials 0.000 claims 5
- 150000001875 compounds Chemical class 0.000 claims 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 125000006431 methyl cyclopropyl group Chemical group 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- CTAPFRYPJLPFDF-UHFFFAOYSA-N isoxazole Chemical compound C=1C=NOC=1 CTAPFRYPJLPFDF-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US36840802P | 2002-03-28 | 2002-03-28 | |
| PCT/US2003/009587 WO2003082832A2 (en) | 2002-03-28 | 2003-03-28 | Anxiolytic agents with reduced sedative and ataxic effects |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2005525392A JP2005525392A (ja) | 2005-08-25 |
| JP2005525392A5 true JP2005525392A5 (https=) | 2008-01-24 |
Family
ID=28675480
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003580300A Pending JP2005525392A (ja) | 2002-03-28 | 2003-03-28 | 減少された鎮静及び失調効果を有する抗不安薬剤 |
Country Status (16)
| Country | Link |
|---|---|
| US (6) | US7119196B2 (https=) |
| EP (1) | EP1490344B1 (https=) |
| JP (1) | JP2005525392A (https=) |
| KR (2) | KR100865410B1 (https=) |
| CN (1) | CN1642924A (https=) |
| AT (1) | ATE389640T1 (https=) |
| AU (1) | AU2003230754B2 (https=) |
| BR (1) | BR0308918A (https=) |
| CA (1) | CA2480869A1 (https=) |
| DE (1) | DE60319812T2 (https=) |
| DK (1) | DK1490344T3 (https=) |
| ES (1) | ES2300576T3 (https=) |
| IL (1) | IL163958A0 (https=) |
| MX (1) | MXPA04009332A (https=) |
| NZ (1) | NZ535517A (https=) |
| WO (1) | WO2003082832A2 (https=) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| USRE47475E1 (en) * | 2002-03-28 | 2019-07-02 | Wisys Technology Foundation, Inc. | Selective agents for pain suppression |
| CA2570185A1 (en) * | 2004-06-30 | 2006-01-12 | Wisys Technology Foundation Inc. | Stereospecific anxiolytic and anticonvulsant agents with reduced muscle-relaxant, sedative-hypnotic and ataxic effects |
| US8119629B2 (en) | 2007-10-03 | 2012-02-21 | Bristol-Meyers Squibb Company | Carboxamide GABAA α2 modulators |
| JP5345637B2 (ja) * | 2008-01-22 | 2013-11-20 | イーライ リリー アンド カンパニー | κ選択的オピオイド受容体アンタゴニスト |
| US20100261711A1 (en) * | 2009-03-20 | 2010-10-14 | Wisys Technology Foundation | Selective anticonvulsant agents and their uses |
| JP2013209292A (ja) * | 2010-07-23 | 2013-10-10 | Nippon Chemiphar Co Ltd | Ｐ２ｘ４受容体拮抗剤 |
| US9006233B2 (en) | 2011-04-28 | 2015-04-14 | Uwm Research Foundation, Inc. | Gabaergic receptor subtype selective ligands and their uses |
| US20150374705A1 (en) | 2012-02-14 | 2015-12-31 | Shanghai Institues for Biological Sciences | Substances for treatment or relief of pain |
| CA2885148A1 (en) | 2012-09-21 | 2014-03-27 | Uwm Research Foundation, Inc. | Novel gabaa agonists and methods of using to control airway hyperresponsiveness and inflammation in asthma |
| FR3010785B1 (fr) * | 2013-09-18 | 2015-08-21 | Snecma | Procede de controle de la densite d'energie d'un faisceau laser par analyse d'image et dispositif correspondant |
| SG11201806393QA (en) | 2016-01-27 | 2018-08-30 | Univ Zuerich | Use of gabaa receptor modulators for treatment of itch |
| DK3439665T3 (da) | 2016-03-18 | 2022-09-26 | Uwm Res Foundation Inc | Behandling af kognitive og sindsstemningssymptomer ved neurodegenerative og neuropsykiatriske lidelser med alpha5-holdige gabaa-receptoragonister |
| JP7013446B2 (ja) | 2016-08-16 | 2022-02-15 | ユーダブリューエム・リサーチ・ファウンデーション，インコーポレーテッド | Ｇａｂａ（ａ）受容体モジュレーター、及び、喘息における気道過敏及び炎症を抑制するための方法 |
| JP7139323B2 (ja) * | 2016-11-01 | 2022-09-20 | エフ．ホフマン－ラ ロシュ アーゲー | Ｃｎｓ関連疾患を処置するための１，３－ジヒドロ－１，４－ベンゾジアゼピン－２－チオン |
| CN107056760A (zh) * | 2017-01-22 | 2017-08-18 | 苏州楚凯药业有限公司 | 5,7位取代的1H‑苯并[e][1,4]二氮杂‑2(3H)‑酮衍生物的制备方法 |
| CN107216332B (zh) * | 2017-06-29 | 2019-04-30 | 上海药明康德新药开发有限公司 | 叔丁基-7-羟甲基-7,8-二氢4h吡唑并二氮杂卓5(6h)甲酸基酯的合成方法 |
| CN107325101B (zh) * | 2017-06-29 | 2019-03-26 | 上海合全药物研发有限公司 | 6-羟甲基-6,7-二氢-5h,9h-咪唑并二氮杂卓-8-羧酸叔丁酯的合成方法 |
| WO2019070910A1 (en) | 2017-10-03 | 2019-04-11 | Uwm Research Foundation, Inc. | NEW POLYTHERAPY FOR ANXIETY, EPILEPSY AND PAIN DISORDERS |
| PE20230440A1 (es) | 2020-03-31 | 2023-03-08 | Hoffmann La Roche | Derivados de benzodiazepinas como pam de gaba a gamma1 |
| US12161622B2 (en) | 2021-05-04 | 2024-12-10 | Janssen Pharmaceuticals, Inc. | Compositions and methods for the treatment of depression |
| AR127127A1 (es) * | 2021-09-24 | 2023-12-20 | Hoffmann La Roche | NUEVOS DERIVADOS DE PIRIDODIAZEPINAS COMO PAM DE GABAA g1 |
| CN118019742A (zh) | 2021-09-29 | 2024-05-10 | 豪夫迈·罗氏有限公司 | 作为GABA A γ1 PAM的新颖苯并二氮杂䓬衍生物 |
| CA3232152A1 (en) | 2021-10-06 | 2023-04-13 | F. Hoffman-La Roche Ag | Benzodiazepine derivatives as positive allosteric modulators of the gaba a gamma1 receptor |
| WO2023170554A1 (en) | 2022-03-07 | 2023-09-14 | Janssen Pharmaceuticals, Inc. | Compositions comprising aticaprant |
| WO2023170550A1 (en) | 2022-03-07 | 2023-09-14 | Janssen Pharmaceuticals, Inc. | Polymorph forms of aticaprant for use in treating major depressive disorder |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2893992A (en) | 1959-07-07 | I ii i i | ||
| US3886141A (en) * | 1971-10-07 | 1975-05-27 | Hoffmann La Roche | Preparation of 5-pyridyl benzodiazepine utilizing hexamethylenetetramine |
| US4440685A (en) * | 1974-09-11 | 1984-04-03 | Hoffmann-La Roche Inc. | Imidazodiazepines and processes therefor |
| US4280957A (en) | 1974-09-11 | 1981-07-28 | Hoffmann-La Roche Inc. | Imidazodiazepines and processes therefor |
| US4401597A (en) | 1978-05-15 | 1983-08-30 | Hoffmann-La Roche Inc. | Imidazodiazepines and processes therefor |
| DE3435973A1 (de) * | 1984-10-01 | 1986-04-10 | Boehringer Ingelheim KG, 6507 Ingelheim | Diazepine enthaltende pharmazeutische zusammensetzungen mit paf-antagonistischer wirkung |
| EP0230942B1 (de) * | 1986-01-21 | 1992-04-29 | Boehringer Ingelheim Kg | Thieno-1,4-diazepine |
| MC1999A1 (fr) * | 1987-12-18 | 1990-01-26 | Hoffmann La Roche | Composes tricycliques |
| US4959361A (en) | 1987-12-18 | 1990-09-25 | Hoffmann-La Roche Inc. | Triazolo(4,3-A)(1,4)benzodiazepines and thieno (3,2-F)(1,2,4)triazolo(4,3-A)(1,4)diazepine compounds which have useful activity as platelet activating factor (PAF) antagonists |
| US5968176A (en) * | 1997-05-29 | 1999-10-19 | 3Com Corporation | Multilayer firewall system |
| SK13682003A3 (sk) | 2001-04-12 | 2004-07-07 | F. Hoffmann-La Roche Ag | Dihydrobenzo[b][1,4]diazepin-2-ónové deriváty ako mGluR2 antagonisty II |
| US7161904B2 (en) * | 2002-06-04 | 2007-01-09 | Fortinet, Inc. | System and method for hierarchical metering in a virtual router based network switch |
| US7415723B2 (en) * | 2002-06-11 | 2008-08-19 | Pandya Ashish A | Distributed network security system and a hardware processor therefor |
-
2003
- 2003-03-28 DE DE60319812T patent/DE60319812T2/de not_active Expired - Lifetime
- 2003-03-28 EP EP03723846A patent/EP1490344B1/en not_active Expired - Lifetime
- 2003-03-28 CA CA002480869A patent/CA2480869A1/en not_active Abandoned
- 2003-03-28 ES ES03723846T patent/ES2300576T3/es not_active Expired - Lifetime
- 2003-03-28 DK DK03723846T patent/DK1490344T3/da active
- 2003-03-28 NZ NZ535517A patent/NZ535517A/en not_active IP Right Cessation
- 2003-03-28 KR KR1020047015305A patent/KR100865410B1/ko not_active Expired - Fee Related
- 2003-03-28 BR BR0308918-5A patent/BR0308918A/pt not_active IP Right Cessation
- 2003-03-28 IL IL16395803A patent/IL163958A0/xx unknown
- 2003-03-28 JP JP2003580300A patent/JP2005525392A/ja active Pending
- 2003-03-28 US US10/402,538 patent/US7119196B2/en not_active Expired - Lifetime
- 2003-03-28 AU AU2003230754A patent/AU2003230754B2/en not_active Ceased
- 2003-03-28 AT AT03723846T patent/ATE389640T1/de not_active IP Right Cessation
- 2003-03-28 WO PCT/US2003/009587 patent/WO2003082832A2/en not_active Ceased
- 2003-03-28 CN CNA038073439A patent/CN1642924A/zh active Pending
- 2003-03-28 KR KR1020087012062A patent/KR20080060286A/ko not_active Ceased
- 2003-03-28 MX MXPA04009332A patent/MXPA04009332A/es active IP Right Grant
-
2006
- 2006-07-20 US US11/458,855 patent/US20070049580A1/en not_active Abandoned
- 2006-07-20 US US11/458,739 patent/US7235656B2/en not_active Expired - Fee Related
-
2007
- 2007-06-24 US US11/767,515 patent/US20070299058A1/en not_active Abandoned
- 2007-10-30 US US11/929,860 patent/US20080108605A1/en not_active Abandoned
-
2010
- 2010-01-08 US US12/684,845 patent/US20100130481A1/en not_active Abandoned
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