RU2011124709A - ДВУЯДЕРНЫЕ ИНГИБИТОРЫ GlyT1 И СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ - Google Patents
ДВУЯДЕРНЫЕ ИНГИБИТОРЫ GlyT1 И СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ Download PDFInfo
- Publication number
- RU2011124709A RU2011124709A RU2011124709/04A RU2011124709A RU2011124709A RU 2011124709 A RU2011124709 A RU 2011124709A RU 2011124709/04 A RU2011124709/04 A RU 2011124709/04A RU 2011124709 A RU2011124709 A RU 2011124709A RU 2011124709 A RU2011124709 A RU 2011124709A
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- Prior art keywords
- hydrogen
- carbon atoms
- organic residue
- independently selected
- possibly substituted
- Prior art date
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- 238000000034 method Methods 0.000 title claims 9
- 102100023145 Sodium- and chloride-dependent glycine transporter 1 Human genes 0.000 title claims 3
- 101710083171 Sodium- and chloride-dependent glycine transporter 1 Proteins 0.000 title claims 3
- 239000003112 inhibitor Substances 0.000 title 1
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 28
- 239000001257 hydrogen Substances 0.000 claims abstract 28
- 125000004432 carbon atom Chemical group C* 0.000 claims abstract 26
- 229910052757 nitrogen Inorganic materials 0.000 claims abstract 25
- 150000001875 compounds Chemical class 0.000 claims abstract 17
- 229910052736 halogen Inorganic materials 0.000 claims abstract 17
- 150000002367 halogens Chemical class 0.000 claims abstract 17
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims abstract 16
- 125000001424 substituent group Chemical group 0.000 claims abstract 16
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims abstract 13
- 125000004093 cyano group Chemical group *C#N 0.000 claims abstract 10
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims abstract 9
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims abstract 6
- 125000005842 heteroatom Chemical group 0.000 claims abstract 6
- 229910052717 sulfur Chemical group 0.000 claims abstract 6
- 239000011593 sulfur Chemical group 0.000 claims abstract 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims abstract 5
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims abstract 5
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims abstract 5
- 229910052760 oxygen Inorganic materials 0.000 claims abstract 5
- 239000001301 oxygen Chemical group 0.000 claims abstract 5
- 125000001931 aliphatic group Chemical group 0.000 claims abstract 4
- 150000002825 nitriles Chemical class 0.000 claims abstract 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims abstract 4
- 125000002619 bicyclic group Chemical group 0.000 claims abstract 3
- 150000002431 hydrogen Chemical class 0.000 claims 14
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 12
- 208000035475 disorder Diseases 0.000 claims 12
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims 6
- 208000028017 Psychotic disease Diseases 0.000 claims 5
- 201000000980 schizophrenia Diseases 0.000 claims 4
- 208000019901 Anxiety disease Diseases 0.000 claims 3
- 208000020925 Bipolar disease Diseases 0.000 claims 3
- 239000004471 Glycine Substances 0.000 claims 3
- 241000124008 Mammalia Species 0.000 claims 3
- 230000004064 dysfunction Effects 0.000 claims 3
- 125000002950 monocyclic group Chemical group 0.000 claims 3
- 230000004044 response Effects 0.000 claims 3
- 125000006710 (C2-C12) alkenyl group Chemical group 0.000 claims 2
- 125000006711 (C2-C12) alkynyl group Chemical group 0.000 claims 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 2
- 208000012661 Dyskinesia Diseases 0.000 claims 2
- 208000026139 Memory disease Diseases 0.000 claims 2
- 208000019022 Mood disease Diseases 0.000 claims 2
- 208000016285 Movement disease Diseases 0.000 claims 2
- 208000012902 Nervous system disease Diseases 0.000 claims 2
- 230000036506 anxiety Effects 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 208000010877 cognitive disease Diseases 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 230000000926 neurological effect Effects 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 208000020016 psychiatric disease Diseases 0.000 claims 2
- 102000005962 receptors Human genes 0.000 claims 2
- 108020003175 receptors Proteins 0.000 claims 2
- 229920006395 saturated elastomer Polymers 0.000 claims 2
- 125000003107 substituted aryl group Chemical group 0.000 claims 2
- 230000024587 synaptic transmission, glutamatergic Effects 0.000 claims 2
- 208000011580 syndromic disease Diseases 0.000 claims 2
- 125000004400 (C1-C12) alkyl group Chemical group 0.000 claims 1
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 claims 1
- 208000027448 Attention Deficit and Disruptive Behavior disease Diseases 0.000 claims 1
- 208000036864 Attention deficit/hyperactivity disease Diseases 0.000 claims 1
- 206010003805 Autism Diseases 0.000 claims 1
- 208000020706 Autistic disease Diseases 0.000 claims 1
- 208000028698 Cognitive impairment Diseases 0.000 claims 1
- 206010012218 Delirium Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 208000030814 Eating disease Diseases 0.000 claims 1
- 208000019454 Feeding and Eating disease Diseases 0.000 claims 1
- 208000036626 Mental retardation Diseases 0.000 claims 1
- 102000004868 N-Methyl-D-Aspartate Receptors Human genes 0.000 claims 1
- 108090001041 N-Methyl-D-Aspartate Receptors Proteins 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 208000027465 Psychotic Affective disease Diseases 0.000 claims 1
- 206010043118 Tardive Dyskinesia Diseases 0.000 claims 1
- 208000000323 Tourette Syndrome Diseases 0.000 claims 1
- 208000016620 Tourette disease Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 208000015802 attention deficit-hyperactivity disease Diseases 0.000 claims 1
- 230000003542 behavioural effect Effects 0.000 claims 1
- 235000014632 disordered eating Nutrition 0.000 claims 1
- 208000035548 disruptive behavior disease Diseases 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 208000024714 major depressive disease Diseases 0.000 claims 1
- DOTMOQHOJINYBL-UHFFFAOYSA-N molecular nitrogen;molecular oxygen Chemical group N#N.O=O DOTMOQHOJINYBL-UHFFFAOYSA-N 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 230000000698 schizophrenic effect Effects 0.000 claims 1
- 238000001228 spectrum Methods 0.000 claims 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/52—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
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- A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
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- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
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- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
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-
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Addiction (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Psychology (AREA)
- Obesity (AREA)
- Urology & Nephrology (AREA)
- Hematology (AREA)
- Child & Adolescent Psychology (AREA)
- Rheumatology (AREA)
- Hospice & Palliative Care (AREA)
- Anesthesiology (AREA)
- Diabetes (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Ophthalmology & Optometry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Indole Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US14103008P | 2008-12-29 | 2008-12-29 | |
| US61/141,030 | 2008-12-29 | ||
| PCT/US2009/069716 WO2010078348A1 (en) | 2008-12-29 | 2009-12-29 | 3.1.0 bicyclic glyt1 inhibitors and methods of making and using same |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2011124709A true RU2011124709A (ru) | 2013-02-10 |
Family
ID=42310195
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2011124709/04A RU2011124709A (ru) | 2008-12-29 | 2009-12-29 | ДВУЯДЕРНЫЕ ИНГИБИТОРЫ GlyT1 И СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US8497289B2 (OSRAM) |
| EP (1) | EP2381941A4 (OSRAM) |
| JP (1) | JP2012514006A (OSRAM) |
| KR (1) | KR20110117087A (OSRAM) |
| CN (1) | CN102271677A (OSRAM) |
| AU (1) | AU2009335120A1 (OSRAM) |
| BR (1) | BRPI0923878A2 (OSRAM) |
| CA (1) | CA2747602A1 (OSRAM) |
| IL (1) | IL213541A0 (OSRAM) |
| MX (1) | MX2011006845A (OSRAM) |
| RU (1) | RU2011124709A (OSRAM) |
| WO (1) | WO2010078348A1 (OSRAM) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9012489B2 (en) * | 2011-08-03 | 2015-04-21 | Boehringer Ingelheim International Gmbh | Phenyl-3-aza-bicyclo[3.1.0]hex-3-yl-methanones and the use thereof as medicament |
| MX2016014581A (es) * | 2014-05-06 | 2018-02-16 | Univ Northwestern | Composiciones de compuestos que modulan nmdar. |
| US9987242B2 (en) | 2015-05-05 | 2018-06-05 | Northwestern University | Treatment of Levodopa-induced Dyskinesias |
| AR118839A1 (es) * | 2019-05-01 | 2021-11-03 | Boehringer Ingelheim Int | Formas sólidas de un inhibidor de glyt1 |
| BR112022026698A2 (pt) | 2020-08-13 | 2023-02-23 | Boehringer Ingelheim Int | Tratamento da deficiência cognitiva associada à esquizofrenia |
| AU2021360172A1 (en) | 2020-10-13 | 2023-03-30 | Boehringer Ingelheim International Gmbh | Process of reworking |
| JP2025528779A (ja) | 2022-08-09 | 2025-09-02 | シーザン ハイスーク ファーマシューティカル カンパニー リミテッド | Ｐｄｅ４ｂ阻害剤及びその用途 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5981168A (en) * | 1998-05-15 | 1999-11-09 | The University Of British Columbia | Method and composition for modulating amyloidosis |
| AU2004281794B2 (en) | 2003-10-14 | 2010-04-22 | Pfizer Products Inc. | Bicyclic [3.1.0] derivatives as glycine transporter inhibitors |
| ATE476431T1 (de) * | 2004-12-21 | 2010-08-15 | Merck Sharp & Dohme | Piperidin- und azetidinderivate als glyt1- inhibitoren |
| EP1888525A1 (en) * | 2005-05-03 | 2008-02-20 | Ranbaxy Laboratories Limited | 3,6-disubstituted azabicyclo [3.1.0]hexane derivatives as muscarinic receptor antagonists |
| GB0523998D0 (en) * | 2005-11-25 | 2006-01-04 | Merck Sharp & Dohme | Therapeutic agents |
| CA2662612A1 (en) * | 2006-09-29 | 2008-04-03 | Actelion Pharmaceuticals Ltd | 3-aza-bicyclo[3.1.0]hexane derivatives |
-
2009
- 2009-12-29 EP EP09837121A patent/EP2381941A4/en not_active Withdrawn
- 2009-12-29 WO PCT/US2009/069716 patent/WO2010078348A1/en not_active Ceased
- 2009-12-29 AU AU2009335120A patent/AU2009335120A1/en not_active Abandoned
- 2009-12-29 CA CA2747602A patent/CA2747602A1/en not_active Abandoned
- 2009-12-29 BR BRPI0923878-6A patent/BRPI0923878A2/pt not_active IP Right Cessation
- 2009-12-29 KR KR1020117016603A patent/KR20110117087A/ko not_active Withdrawn
- 2009-12-29 JP JP2011543717A patent/JP2012514006A/ja active Pending
- 2009-12-29 CN CN2009801530939A patent/CN102271677A/zh active Pending
- 2009-12-29 MX MX2011006845A patent/MX2011006845A/es not_active Application Discontinuation
- 2009-12-29 US US12/648,972 patent/US8497289B2/en not_active Expired - Fee Related
- 2009-12-29 RU RU2011124709/04A patent/RU2011124709A/ru not_active Application Discontinuation
-
2011
- 2011-06-14 IL IL213541A patent/IL213541A0/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2012514006A (ja) | 2012-06-21 |
| US8497289B2 (en) | 2013-07-30 |
| CN102271677A (zh) | 2011-12-07 |
| EP2381941A4 (en) | 2012-08-01 |
| MX2011006845A (es) | 2011-08-04 |
| IL213541A0 (en) | 2011-07-31 |
| CA2747602A1 (en) | 2010-07-08 |
| US20100256192A1 (en) | 2010-10-07 |
| WO2010078348A1 (en) | 2010-07-08 |
| AU2009335120A1 (en) | 2011-07-07 |
| KR20110117087A (ko) | 2011-10-26 |
| EP2381941A1 (en) | 2011-11-02 |
| BRPI0923878A2 (pt) | 2015-07-28 |
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| Date | Code | Title | Description |
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| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
Effective date: 20140314 |