AU772947B2 - Triazolo-pyridazine derivatives as ligands for GABA receptors - Google Patents
Triazolo-pyridazine derivatives as ligands for GABA receptors Download PDFInfo
- Publication number
- AU772947B2 AU772947B2 AU30669/00A AU3066900A AU772947B2 AU 772947 B2 AU772947 B2 AU 772947B2 AU 30669/00 A AU30669/00 A AU 30669/00A AU 3066900 A AU3066900 A AU 3066900A AU 772947 B2 AU772947 B2 AU 772947B2
- Authority
- AU
- Australia
- Prior art keywords
- compound
- formula
- pharmaceutically acceptable
- triazolo
- triazol
- 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.)
- Ceased
Links
- 239000003446 ligand Substances 0.000 title abstract description 10
- CBHTTYDJRXOHHL-UHFFFAOYSA-N 2h-triazolo[4,5-c]pyridazine Chemical class N1=NC=CC2=C1N=NN2 CBHTTYDJRXOHHL-UHFFFAOYSA-N 0.000 title description 4
- 102000005915 GABA Receptors Human genes 0.000 title 1
- 108010005551 GABA Receptors Proteins 0.000 title 1
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- 230000036506 anxiety Effects 0.000 claims abstract description 8
- 230000002265 prevention Effects 0.000 claims abstract description 8
- 150000001875 compounds Chemical class 0.000 claims description 121
- 150000003839 salts Chemical class 0.000 claims description 27
- 238000000034 method Methods 0.000 claims description 25
- 239000000203 mixture Substances 0.000 claims description 25
- 125000001153 fluoro group Chemical group F* 0.000 claims description 8
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- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 7
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 7
- 230000008569 process Effects 0.000 claims description 6
- 239000003814 drug Substances 0.000 claims description 5
- IUGYQRQAERSCNH-UHFFFAOYSA-N pivalic acid Chemical compound CC(C)(C)C(O)=O IUGYQRQAERSCNH-UHFFFAOYSA-N 0.000 claims description 5
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- ROOXNKNUYICQNP-UHFFFAOYSA-N ammonium persulfate Chemical compound [NH4+].[NH4+].[O-]S(=O)(=O)OOS([O-])(=O)=O ROOXNKNUYICQNP-UHFFFAOYSA-N 0.000 claims description 4
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- 150000003624 transition metals Chemical class 0.000 claims description 3
- LDGXFPTUGULLJC-UHFFFAOYSA-N 5h-[1,2,4]triazolo[4,3-b]pyridazin-6-one Chemical compound N1C(=O)C=CC2=NN=CN21 LDGXFPTUGULLJC-UHFFFAOYSA-N 0.000 claims description 2
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- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 abstract description 2
- -1 trifluoro-substituted phenyl ring Chemical group 0.000 abstract 1
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- 239000000047 product Substances 0.000 description 12
- VLKZOEOYAKHREP-UHFFFAOYSA-N n-Hexane Chemical compound CCCCCC VLKZOEOYAKHREP-UHFFFAOYSA-N 0.000 description 11
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 10
- 239000002585 base Substances 0.000 description 9
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- A61P25/22—Anxiolytics
-
- 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
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (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)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Vascular Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB9901744.4A GB9901744D0 (en) | 1999-01-27 | 1999-01-27 | Therapeutic agents |
| GB9901744 | 1999-01-27 | ||
| GB9901743 | 1999-01-27 | ||
| GBGB9901743.6A GB9901743D0 (en) | 1999-01-27 | 1999-01-27 | Therapeutic agents |
| GB9912429 | 1999-05-27 | ||
| GBGB9912429.9A GB9912429D0 (en) | 1999-05-27 | 1999-05-27 | Therapeutic agents |
| PCT/GB2000/000183 WO2000044752A1 (en) | 1999-01-27 | 2000-01-19 | Triazolo-pyridazine derivatives as ligands for gaba receptors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU3066900A AU3066900A (en) | 2000-08-18 |
| AU772947B2 true AU772947B2 (en) | 2004-05-13 |
Family
ID=27269629
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU30669/00A Ceased AU772947B2 (en) | 1999-01-27 | 2000-01-19 | Triazolo-pyridazine derivatives as ligands for GABA receptors |
Country Status (9)
| Country | Link |
|---|---|
| US (2) | US6500828B1 (enExample) |
| EP (1) | EP1149102B1 (enExample) |
| JP (1) | JP2002535407A (enExample) |
| AT (1) | ATE284403T1 (enExample) |
| AU (1) | AU772947B2 (enExample) |
| CA (1) | CA2359008C (enExample) |
| DE (1) | DE60016566T2 (enExample) |
| ES (1) | ES2232416T3 (enExample) |
| WO (1) | WO2000044752A1 (enExample) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0000564D0 (en) * | 2000-01-11 | 2000-03-01 | Merck Sharp & Dohme | Therapeutic agents |
| US6958334B2 (en) | 2001-04-10 | 2005-10-25 | Merck & Co., Inc. | Inhibitors of Akt activity |
| WO2002083139A1 (en) | 2001-04-10 | 2002-10-24 | Merck & Co., Inc. | Inhibitors of akt activity |
| WO2002083675A2 (en) | 2001-04-10 | 2002-10-24 | Merck Sharp & Dohme Limited | Inhibitors of akt activity |
| WO2004048980A1 (en) * | 2002-11-28 | 2004-06-10 | Neurosearch A/S | Method for screening for compounds as potential sedatives or anxiolytics |
| WO2006061428A2 (en) * | 2004-12-10 | 2006-06-15 | Universität Zürich | Gaba-a alpha 2 and alpha 3 receptor agonists for treating neuropathic, inflammatory and migraine associated pain |
| EP2258358A3 (en) | 2005-08-26 | 2011-09-07 | Braincells, Inc. | Neurogenesis with acetylcholinesterase inhibitor |
| EP2275096A3 (en) | 2005-08-26 | 2011-07-13 | Braincells, Inc. | Neurogenesis via modulation of the muscarinic receptors |
| AU2006304787A1 (en) | 2005-10-21 | 2007-04-26 | Braincells, Inc. | Modulation of neurogenesis by PDE inhibition |
| CA2625210A1 (en) | 2005-10-31 | 2007-05-10 | Braincells, Inc. | Gaba receptor mediated modulation of neurogenesis |
| US20100216734A1 (en) | 2006-03-08 | 2010-08-26 | Braincells, Inc. | Modulation of neurogenesis by nootropic agents |
| AU2007249399A1 (en) | 2006-05-09 | 2007-11-22 | Braincells, Inc. | Neurogenesis by modulating angiotensin |
| AU2007249435A1 (en) | 2006-05-09 | 2007-11-22 | Braincells, Inc. | 5 HT receptor mediated neurogenesis |
| BRPI0716604A2 (pt) | 2006-09-08 | 2013-04-09 | Braincells Inc | combinaÇÕes contendo um derivado de 4-acilaminopiridina |
| EP2328414B1 (en) * | 2008-08-29 | 2013-12-11 | Concert Pharmaceuticals Inc. | Substituted triazolo-pyridazine derivatives |
| US20100216805A1 (en) | 2009-02-25 | 2010-08-26 | Braincells, Inc. | Modulation of neurogenesis using d-cycloserine combinations |
| EP2454259A1 (en) | 2009-06-23 | 2012-05-23 | Concert Pharmaceuticals Inc. | Deuterium-modified triazolo-pyridazine derivatives as gaba-a receptor modulators |
| WO2011047315A1 (en) | 2009-10-15 | 2011-04-21 | Concert Pharmaceuticals, Inc. | Subsitituted benzimidazoles |
| WO2013170242A1 (en) * | 2012-05-11 | 2013-11-14 | Concert Pharmaceuticals, Inc. | Form 2 polymorph of 7-(tert-butyl-d9)-3-(2,5-difluorophenyl)-6-((1-methyl-1h-1,2,4-triazol-5-yl)methoxy)-[1,2,4]triazolo[4,3-b]pyridazine |
| WO2013170241A1 (en) * | 2012-05-11 | 2013-11-14 | Concert Pharmaceuticals, Inc. | Polymorphs of 7-(tert-butyl-d9)-3-(2,5-difluorophenyl)-6-((1-methyl-1h-1,2,4-triazol-5-yl)methoxy)-[1,2,4]triazolol[4,3b]pyridazine |
| US20150099753A1 (en) * | 2012-05-11 | 2015-04-09 | Concert Pharmaceuticals Inc. | Form 5 polymorph of 7-(tert-butyl-d9)-3-(2,5-difluorophenyl)-6-((1-methyl-1h-1,2,4-triazol-5-yl)methoxy)-[1,2,4]triazolo[4,3-b]pyridazine |
| WO2015095549A1 (en) * | 2013-12-18 | 2015-06-25 | Concert Pharmaceuticals, Inc. | Dosage regimen for gabaa receptor subtype selective drug |
| WO2020053377A1 (en) * | 2018-09-13 | 2020-03-19 | Saniona A/S | A gabaa receptor ligand |
| CN119136800A (zh) * | 2022-04-20 | 2024-12-13 | 恩格莱尔治疗公司 | Gabaa受体调节剂盐、颗粒及其用途 |
| CN115837022B (zh) * | 2023-02-20 | 2023-04-25 | 中山大学附属第八医院（深圳福田） | 1,2,4三唑并4,3-b哒嗪衍生物在制备抗衰老药物中的应用 |
| WO2025141131A1 (en) | 2023-12-27 | 2025-07-03 | Saniona A/S | A gabaa receptor ligand and the use thereof in medicine, in particular in the treatment of epilepsy |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1998004559A2 (en) * | 1996-07-25 | 1998-02-05 | Merck Sharp & Dohme Limited | Substituted triazolo-pyridazine derivatives as ligands for gaba receptors |
-
2000
- 2000-01-19 AT AT00900748T patent/ATE284403T1/de not_active IP Right Cessation
- 2000-01-19 DE DE60016566T patent/DE60016566T2/de not_active Expired - Fee Related
- 2000-01-19 ES ES00900748T patent/ES2232416T3/es not_active Expired - Lifetime
- 2000-01-19 JP JP2000596008A patent/JP2002535407A/ja not_active Withdrawn
- 2000-01-19 WO PCT/GB2000/000183 patent/WO2000044752A1/en not_active Ceased
- 2000-01-19 AU AU30669/00A patent/AU772947B2/en not_active Ceased
- 2000-01-19 CA CA002359008A patent/CA2359008C/en not_active Expired - Fee Related
- 2000-01-19 EP EP00900748A patent/EP1149102B1/en not_active Expired - Lifetime
- 2000-01-19 US US09/890,000 patent/US6500828B1/en not_active Expired - Fee Related
-
2002
- 2002-12-20 US US10/324,968 patent/US20030158203A1/en not_active Abandoned
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1998004559A2 (en) * | 1996-07-25 | 1998-02-05 | Merck Sharp & Dohme Limited | Substituted triazolo-pyridazine derivatives as ligands for gaba receptors |
Also Published As
| Publication number | Publication date |
|---|---|
| ES2232416T3 (es) | 2005-06-01 |
| US20030158203A1 (en) | 2003-08-21 |
| CA2359008A1 (en) | 2000-08-03 |
| AU3066900A (en) | 2000-08-18 |
| CA2359008C (en) | 2008-05-20 |
| DE60016566D1 (de) | 2005-01-13 |
| EP1149102A1 (en) | 2001-10-31 |
| WO2000044752A1 (en) | 2000-08-03 |
| EP1149102B1 (en) | 2004-12-08 |
| JP2002535407A (ja) | 2002-10-22 |
| US6500828B1 (en) | 2002-12-31 |
| DE60016566T2 (de) | 2005-12-15 |
| ATE284403T1 (de) | 2004-12-15 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FGA | Letters patent sealed or granted (standard patent) |