DE60319812T2 - Angstlösende wirkstoffe mit verminderten beruhigenden und ataktischen nebenwirkungen - Google Patents
Angstlösende wirkstoffe mit verminderten beruhigenden und ataktischen nebenwirkungen Download PDFInfo
- Publication number
- DE60319812T2 DE60319812T2 DE60319812T DE60319812T DE60319812T2 DE 60319812 T2 DE60319812 T2 DE 60319812T2 DE 60319812 T DE60319812 T DE 60319812T DE 60319812 T DE60319812 T DE 60319812T DE 60319812 T2 DE60319812 T2 DE 60319812T2
- Authority
- DE
- Germany
- Prior art keywords
- mmol
- mixture
- compound
- nmr
- 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.)
- Expired - Lifetime
Links
- 0 C*C(*1C(C*=C2ON)=*(C)*C1*)=C2N Chemical compound C*C(*1C(C*=C2ON)=*(C)*C1*)=C2N 0.000 description 6
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
- C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
- C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
- C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
- C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
- C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
- C07D243/12—1,5-Benzodiazepines; Hydrogenated 1,5-benzodiazepines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
- C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
- C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
- C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
- C07D243/16—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
- C07D243/18—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
- C07D243/20—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
- C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
- C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
- C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
- C07D243/16—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
- C07D243/18—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
- C07D243/24—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/06—Peri-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D495/14—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Hospice & Palliative Care (AREA)
- Otolaryngology (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US36840802P | 2002-03-28 | 2002-03-28 | |
| US368408P | 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 |
|---|---|
| DE60319812D1 DE60319812D1 (de) | 2008-04-30 |
| DE60319812T2 true DE60319812T2 (de) | 2009-04-23 |
Family
ID=28675480
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE60319812T Expired - Lifetime DE60319812T2 (de) | 2002-03-28 | 2003-03-28 | Angstlösende wirkstoffe mit verminderten beruhigenden und ataktischen nebenwirkungen |
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
Also Published As
| Publication number | Publication date |
|---|---|
| EP1490344B1 (en) | 2008-03-19 |
| MXPA04009332A (es) | 2005-12-12 |
| KR20040098029A (ko) | 2004-11-18 |
| EP1490344A2 (en) | 2004-12-29 |
| ATE389640T1 (de) | 2008-04-15 |
| US20070054881A1 (en) | 2007-03-08 |
| ES2300576T3 (es) | 2008-06-16 |
| US20070049580A1 (en) | 2007-03-01 |
| WO2003082832A3 (en) | 2004-04-08 |
| US7119196B2 (en) | 2006-10-10 |
| US20100130481A1 (en) | 2010-05-27 |
| WO2003082832A2 (en) | 2003-10-09 |
| KR100865410B1 (ko) | 2008-10-24 |
| CA2480869A1 (en) | 2003-10-09 |
| US20040082573A1 (en) | 2004-04-29 |
| DK1490344T3 (da) | 2008-06-16 |
| NZ535517A (en) | 2007-02-23 |
| JP2005525392A (ja) | 2005-08-25 |
| AU2003230754A1 (en) | 2003-10-13 |
| US20070299058A1 (en) | 2007-12-27 |
| IL163958A0 (en) | 2005-12-18 |
| US7235656B2 (en) | 2007-06-26 |
| KR20080060286A (ko) | 2008-07-01 |
| CN1642924A (zh) | 2005-07-20 |
| US20080108605A1 (en) | 2008-05-08 |
| AU2003230754B2 (en) | 2007-10-25 |
| DE60319812D1 (de) | 2008-04-30 |
| BR0308918A (pt) | 2005-01-04 |
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