RU2012121631A - АРИЛ- И ГЕТЕРОАРИЛСУЛЬФОНЫ КАК АЛЛОСТЕРИЧЕСКИЕ СРЕДСТВА ПОТЕНЦИРОВАНИЯ mGluR4, КОМПОЗИЦИИ И СПОСОБЫ ЛЕЧЕНИЯ НЕВРОЛОГИЧЕСКИХ ДИСФУНКЦИЙ - Google Patents
АРИЛ- И ГЕТЕРОАРИЛСУЛЬФОНЫ КАК АЛЛОСТЕРИЧЕСКИЕ СРЕДСТВА ПОТЕНЦИРОВАНИЯ mGluR4, КОМПОЗИЦИИ И СПОСОБЫ ЛЕЧЕНИЯ НЕВРОЛОГИЧЕСКИХ ДИСФУНКЦИЙ Download PDFInfo
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- RU2012121631A RU2012121631A RU2012121631/15A RU2012121631A RU2012121631A RU 2012121631 A RU2012121631 A RU 2012121631A RU 2012121631/15 A RU2012121631/15 A RU 2012121631/15A RU 2012121631 A RU2012121631 A RU 2012121631A RU 2012121631 A RU2012121631 A RU 2012121631A
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- Prior art keywords
- optionally substituted
- group
- alkyl
- cycloalkyl
- halogen
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- 125000003118 aryl group Chemical group 0.000 title claims abstract 50
- 238000000034 method Methods 0.000 title claims abstract 37
- 102100038354 Metabotropic glutamate receptor 4 Human genes 0.000 title claims abstract 18
- 108010038422 metabotropic glutamate receptor 4 Proteins 0.000 title claims abstract 18
- 230000003389 potentiating effect Effects 0.000 title claims 7
- -1 heteroaryl sulfones Chemical class 0.000 title claims 4
- 230000003281 allosteric effect Effects 0.000 title 1
- 239000000203 mixture Substances 0.000 title 1
- 230000009251 neurologic dysfunction Effects 0.000 title 1
- 208000015015 neurological dysfunction Diseases 0.000 title 1
- 229910052717 sulfur Inorganic materials 0.000 claims abstract 76
- 229910052736 halogen Inorganic materials 0.000 claims abstract 71
- 150000002367 halogens Chemical class 0.000 claims abstract 71
- 150000001875 compounds Chemical class 0.000 claims abstract 66
- 125000004122 cyclic group Chemical group 0.000 claims abstract 66
- 229910052799 carbon Inorganic materials 0.000 claims abstract 65
- 125000004430 oxygen atom Chemical group O* 0.000 claims abstract 64
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 59
- 229910052760 oxygen Inorganic materials 0.000 claims abstract 59
- 125000004432 carbon atom Chemical group C* 0.000 claims abstract 58
- 125000004433 nitrogen atom Chemical group N* 0.000 claims abstract 57
- 125000004434 sulfur atom Chemical group 0.000 claims abstract 57
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract 48
- 241000124008 Mammalia Species 0.000 claims abstract 27
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract 23
- 230000004064 dysfunction Effects 0.000 claims abstract 22
- 229910052757 nitrogen Inorganic materials 0.000 claims abstract 19
- 230000000694 effects Effects 0.000 claims abstract 17
- 150000003839 salts Chemical class 0.000 claims abstract 10
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims abstract 8
- 125000002813 thiocarbonyl group Chemical group *C(*)=S 0.000 claims abstract 8
- 201000010099 disease Diseases 0.000 claims abstract 6
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 67
- 125000000217 alkyl group Chemical group 0.000 claims 65
- 239000008194 pharmaceutical composition Substances 0.000 claims 29
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 17
- 208000035475 disorder Diseases 0.000 claims 17
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 13
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 12
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 9
- 201000000980 schizophrenia Diseases 0.000 claims 8
- 208000028017 Psychotic disease Diseases 0.000 claims 7
- 230000005062 synaptic transmission Effects 0.000 claims 7
- 208000019901 Anxiety disease Diseases 0.000 claims 6
- YLQBMQCUIZJEEH-UHFFFAOYSA-N Furan Chemical class C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims 6
- 208000020925 Bipolar disease Diseases 0.000 claims 5
- 208000018737 Parkinson disease Diseases 0.000 claims 5
- 208000028698 Cognitive impairment Diseases 0.000 claims 4
- KYQCOXFCLRTKLS-UHFFFAOYSA-N Pyrazine Chemical compound C1=CN=CC=N1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 claims 4
- 208000010877 cognitive disease Diseases 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 229940079593 drug Drugs 0.000 claims 4
- 150000003222 pyridines Chemical class 0.000 claims 4
- 208000031091 Amnestic disease Diseases 0.000 claims 3
- 208000019430 Motor disease Diseases 0.000 claims 3
- 102000004868 N-Methyl-D-Aspartate Receptors Human genes 0.000 claims 3
- 108090001041 N-Methyl-D-Aspartate Receptors Proteins 0.000 claims 3
- 208000008589 Obesity Diseases 0.000 claims 3
- 235000020824 obesity Nutrition 0.000 claims 3
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 2
- MESFXNGUDNODTJ-UHFFFAOYSA-N 2h-thiazine 1,1-dioxide Chemical compound O=S1(=O)NC=CC=C1 MESFXNGUDNODTJ-UHFFFAOYSA-N 0.000 claims 2
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 claims 2
- 208000036864 Attention deficit/hyperactivity disease Diseases 0.000 claims 2
- 206010012218 Delirium Diseases 0.000 claims 2
- 208000012661 Dyskinesia Diseases 0.000 claims 2
- 208000002720 Malnutrition Diseases 0.000 claims 2
- 208000019022 Mood disease Diseases 0.000 claims 2
- 208000012902 Nervous system disease Diseases 0.000 claims 2
- PCNDJXKNXGMECE-UHFFFAOYSA-N Phenazine Natural products C1=CC=CC2=NC3=CC=CC=C3N=C21 PCNDJXKNXGMECE-UHFFFAOYSA-N 0.000 claims 2
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical class C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 2
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical class C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims 2
- 230000036506 anxiety Effects 0.000 claims 2
- 208000015802 attention deficit-hyperactivity disease Diseases 0.000 claims 2
- 150000002240 furans Chemical class 0.000 claims 2
- 230000001771 impaired effect Effects 0.000 claims 2
- 230000001071 malnutrition Effects 0.000 claims 2
- 235000000824 malnutrition Nutrition 0.000 claims 2
- 230000000926 neurological effect Effects 0.000 claims 2
- 208000015380 nutritional deficiency disease Diseases 0.000 claims 2
- 208000020016 psychiatric disease Diseases 0.000 claims 2
- 150000003230 pyrimidines Chemical class 0.000 claims 2
- 102000005962 receptors Human genes 0.000 claims 2
- 108020003175 receptors Proteins 0.000 claims 2
- 206010000117 Abnormal behaviour Diseases 0.000 claims 1
- 206010003805 Autism Diseases 0.000 claims 1
- 208000020706 Autistic disease Diseases 0.000 claims 1
- 206010012239 Delusion Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 208000020401 Depressive disease Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 206010026749 Mania Diseases 0.000 claims 1
- 208000000172 Medulloblastoma Diseases 0.000 claims 1
- 208000026139 Memory disease Diseases 0.000 claims 1
- 208000036626 Mental retardation Diseases 0.000 claims 1
- 108010010914 Metabotropic glutamate receptors Proteins 0.000 claims 1
- 102000016193 Metabotropic glutamate receptors Human genes 0.000 claims 1
- 206010028980 Neoplasm 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
- 125000004429 atom Chemical group 0.000 claims 1
- 230000003542 behavioural effect Effects 0.000 claims 1
- 210000004027 cell Anatomy 0.000 claims 1
- 238000011260 co-administration Methods 0.000 claims 1
- 231100000868 delusion Toxicity 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 239000003937 drug carrier Chemical class 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 235000019441 ethanol Nutrition 0.000 claims 1
- 208000035231 inattentive type attention deficit hyperactivity disease Diseases 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 230000001272 neurogenic effect Effects 0.000 claims 1
- 210000002569 neuron Anatomy 0.000 claims 1
- 208000030212 nutrition disease Diseases 0.000 claims 1
- 235000019613 sensory perceptions of taste Nutrition 0.000 claims 1
- 230000004083 survival effect Effects 0.000 claims 1
- 230000024587 synaptic transmission, glutamatergic Effects 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 230000035923 taste sensation Effects 0.000 claims 1
- 0 CC1(*)*=C(*)*=C2N=C(*)N(*)C2=*1 Chemical compound CC1(*)*=C(*)*=C2N=C(*)N(*)C2=*1 0.000 description 2
- PKIMKGDKFZWDKL-UHFFFAOYSA-N O=C(c1ncccn1)Nc(cc1)ccc1S(Cc1ccccc1Cl)(=O)=O Chemical compound O=C(c1ncccn1)Nc(cc1)ccc1S(Cc1ccccc1Cl)(=O)=O PKIMKGDKFZWDKL-UHFFFAOYSA-N 0.000 description 1
- TZDLBFFKSAOKNE-UHFFFAOYSA-N OS(Cc(cccc1)c1Cl)(c(cc1)cc2c1[nH]c(-c1c[s]cn1)n2)=O Chemical compound OS(Cc(cccc1)c1Cl)(c(cc1)cc2c1[nH]c(-c1c[s]cn1)n2)=O TZDLBFFKSAOKNE-UHFFFAOYSA-N 0.000 description 1
- XGQSTTCYXJGHCX-UHFFFAOYSA-N OS(Cc1ccccc1Cl)(c(cc1)ccc1NC(c1ncccc1)=O)=O Chemical compound OS(Cc1ccccc1Cl)(c(cc1)ccc1NC(c1ncccc1)=O)=O XGQSTTCYXJGHCX-UHFFFAOYSA-N 0.000 description 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- 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
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
-
- 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
- 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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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
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- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/81—Amides; Imides
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
- C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D307/56—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Obesity (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Hospice & Palliative Care (AREA)
- Psychology (AREA)
- Child & Adolescent Psychology (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Furan Compounds (AREA)
- Pyridine Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US25885609P | 2009-11-06 | 2009-11-06 | |
| US61/258,856 | 2009-11-06 | ||
| PCT/US2010/055861 WO2011057208A2 (en) | 2009-11-06 | 2010-11-08 | Aryl and heteroaryl sulfones as mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2012121631A true RU2012121631A (ru) | 2013-12-20 |
Family
ID=43970815
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2012121631/15A RU2012121631A (ru) | 2009-11-06 | 2010-11-08 | АРИЛ- И ГЕТЕРОАРИЛСУЛЬФОНЫ КАК АЛЛОСТЕРИЧЕСКИЕ СРЕДСТВА ПОТЕНЦИРОВАНИЯ mGluR4, КОМПОЗИЦИИ И СПОСОБЫ ЛЕЧЕНИЯ НЕВРОЛОГИЧЕСКИХ ДИСФУНКЦИЙ |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US8912336B2 (enExample) |
| EP (1) | EP2498781A2 (enExample) |
| JP (1) | JP2013510178A (enExample) |
| KR (1) | KR20120115252A (enExample) |
| CN (1) | CN103079570A (enExample) |
| AU (1) | AU2010314891A1 (enExample) |
| BR (1) | BR112012010738A2 (enExample) |
| CA (1) | CA2780128A1 (enExample) |
| IL (1) | IL219568A0 (enExample) |
| MX (1) | MX2012005248A (enExample) |
| RU (1) | RU2012121631A (enExample) |
| WO (1) | WO2011057208A2 (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2722014C2 (ru) * | 2015-08-03 | 2020-05-26 | Ф. Хоффманн-Ля Рош Аг | Этинильные производные |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2751176A1 (en) | 2009-01-28 | 2010-08-05 | Vanderbilt University | Substituted 1,1,3,3-tetraoxidobenzo[d][1,3,2]dithiazoles as mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
| US8759377B2 (en) | 2009-11-23 | 2014-06-24 | Vanderbilt University | Substituted dioxopiperidines and dioxopyrrolidines as MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
| GB201104153D0 (en) | 2011-03-11 | 2011-04-27 | Glaxo Group Ltd | Novel compounds |
| US10221172B2 (en) | 2015-01-13 | 2019-03-05 | Vanderbilt University | Benzothiazole and benzisothiazole-substituted compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
| US10526323B2 (en) | 2015-01-30 | 2020-01-07 | Vanderbilt University | Indazole and azaindazole substituted compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
| US10227343B2 (en) | 2015-01-30 | 2019-03-12 | Vanderbilt University | Isoquiniline and napthalene-substituted compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
| WO2016179351A1 (en) | 2015-05-05 | 2016-11-10 | Northwestern University | Treatment of levodopa-induced dyskinesias |
| US10294222B2 (en) | 2016-09-01 | 2019-05-21 | Vanderbilt University | Benzomorpholine and benzomorpholine-substituted compounds as MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
| US10710997B2 (en) | 2016-09-01 | 2020-07-14 | Vanderbilt University | Isoquinoline amide and isoquinoline amide-substituted compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
| WO2018089544A1 (en) | 2016-11-08 | 2018-05-17 | Vanderbilt University | Isoquinoline amine compounds as mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
| US10968227B2 (en) | 2016-11-08 | 2021-04-06 | Vanderbilt University | Isoquinoline ether compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
| CN108148054B (zh) * | 2016-12-05 | 2021-01-08 | 中国科学院大连化学物理研究所 | 一种吡啶基桥联手性噁唑啉化合物及其合成方法 |
| US11319304B2 (en) | 2017-06-28 | 2022-05-03 | Vanderbilt University | Pyridine quinoline compounds as MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
| EA202090467A1 (ru) | 2017-08-16 | 2020-06-18 | Вандербилт Юниверсити | ИНДАЗОЛОВЫЕ СОЕДИНЕНИЯ КАК АЛЛОСТЕРИЧЕСКИЕ ПОТЕНЦИАТОРЫ mGLuR4, КОМПОЗИЦИИ И СПОСОБЫ ЛЕЧЕНИЯ НЕВРОЛОГИЧЕСКИХ ДИСФУНКЦИЙ |
| KR20210068399A (ko) * | 2018-08-06 | 2021-06-09 | 더 보드 오브 트러스티스 오브 더 리랜드 스탠포드 주니어 유니버시티 | 신경퇴행성 질병의 치료를 위한 피피에이알지씨1알파 활성제로서 2-아릴벤즈이미다졸 |
| CN112409251B (zh) * | 2020-11-26 | 2022-07-05 | 成都百泉生物医药科技有限公司 | 一种奥美拉唑工艺杂质及其制备方法 |
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| PT100905A (pt) * | 1991-09-30 | 1994-02-28 | Eisai Co Ltd | Compostos heterociclicos azotados biciclicos contendo aneis de benzeno, ciclo-hexano ou piridina e de pirimidina, piridina ou imidazol substituidos e composicoes farmaceuticas que os contem |
| FR2751649B1 (fr) | 1996-07-26 | 1998-08-28 | Adir | Nouveaux derives de benzimidazole, de benzoxazole et de benzothiazole, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
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- 2010-11-08 CA CA2780128A patent/CA2780128A1/en not_active Abandoned
- 2010-11-08 EP EP10829242A patent/EP2498781A2/en not_active Withdrawn
- 2010-11-08 MX MX2012005248A patent/MX2012005248A/es not_active Application Discontinuation
- 2010-11-08 KR KR1020127014657A patent/KR20120115252A/ko not_active Withdrawn
- 2010-11-08 RU RU2012121631/15A patent/RU2012121631A/ru not_active Application Discontinuation
- 2010-11-08 JP JP2012538064A patent/JP2013510178A/ja not_active Withdrawn
- 2010-11-08 WO PCT/US2010/055861 patent/WO2011057208A2/en not_active Ceased
- 2010-11-08 BR BR112012010738A patent/BR112012010738A2/pt not_active IP Right Cessation
- 2010-11-08 US US13/508,535 patent/US8912336B2/en active Active
- 2010-11-08 CN CN2010800589711A patent/CN103079570A/zh active Pending
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2722014C2 (ru) * | 2015-08-03 | 2020-05-26 | Ф. Хоффманн-Ля Рош Аг | Этинильные производные |
| RU2722014C9 (ru) * | 2015-08-03 | 2020-10-22 | Ф. Хоффманн-Ля Рош Аг | Этинильные производные |
Also Published As
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|---|---|
| WO2011057208A3 (en) | 2014-03-20 |
| CA2780128A1 (en) | 2011-05-12 |
| AU2010314891A1 (en) | 2012-06-07 |
| US8912336B2 (en) | 2014-12-16 |
| BR112012010738A2 (pt) | 2019-09-24 |
| EP2498781A2 (en) | 2012-09-19 |
| MX2012005248A (es) | 2012-06-14 |
| IL219568A0 (en) | 2012-06-28 |
| WO2011057208A2 (en) | 2011-05-12 |
| KR20120115252A (ko) | 2012-10-17 |
| CN103079570A (zh) | 2013-05-01 |
| JP2013510178A (ja) | 2013-03-21 |
| US20120245185A1 (en) | 2012-09-27 |
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