CA2798514A1 - Heterocyclic sulfone mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction - Google Patents
Heterocyclic sulfone mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction Download PDFInfo
- Publication number
- CA2798514A1 CA2798514A1 CA2798514A CA2798514A CA2798514A1 CA 2798514 A1 CA2798514 A1 CA 2798514A1 CA 2798514 A CA2798514 A CA 2798514A CA 2798514 A CA2798514 A CA 2798514A CA 2798514 A1 CA2798514 A1 CA 2798514A1
- Authority
- CA
- Canada
- Prior art keywords
- optionally substituted
- alkyl
- cycloalkyl
- membered ring
- ring containing
- 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.)
- Abandoned
Links
- 238000000034 method Methods 0.000 title claims abstract 49
- -1 Heterocyclic sulfone Chemical class 0.000 title claims abstract 24
- 230000003281 allosteric effect Effects 0.000 title abstract 3
- 239000000203 mixture Substances 0.000 title 1
- 230000009251 neurologic dysfunction Effects 0.000 title 1
- 208000015015 neurological dysfunction Diseases 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 52
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract 31
- 230000004064 dysfunction Effects 0.000 claims abstract 23
- 201000010099 disease Diseases 0.000 claims abstract 9
- 108010010914 Metabotropic glutamate receptors Proteins 0.000 claims abstract 5
- 102000016193 Metabotropic glutamate receptors Human genes 0.000 claims abstract 5
- 208000012902 Nervous system disease Diseases 0.000 claims abstract 4
- 230000000926 neurological effect Effects 0.000 claims abstract 4
- 208000020016 psychiatric disease Diseases 0.000 claims abstract 4
- 229910052760 oxygen Inorganic materials 0.000 claims 100
- 229910052717 sulfur Inorganic materials 0.000 claims 99
- 229910052757 nitrogen Inorganic materials 0.000 claims 81
- 229910052799 carbon Inorganic materials 0.000 claims 67
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 58
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 54
- 125000001072 heteroaryl group Chemical group 0.000 claims 46
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 44
- 125000003118 aryl group Chemical group 0.000 claims 44
- 229910052736 halogen Inorganic materials 0.000 claims 44
- 150000002367 halogens Chemical class 0.000 claims 44
- 125000002813 thiocarbonyl group Chemical group *C(*)=S 0.000 claims 44
- 102100038354 Metabotropic glutamate receptor 4 Human genes 0.000 claims 39
- 108010038422 metabotropic glutamate receptor 4 Proteins 0.000 claims 39
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 33
- 241000124008 Mammalia Species 0.000 claims 29
- 230000000694 effects Effects 0.000 claims 24
- 125000000217 alkyl group Chemical group 0.000 claims 22
- 208000035475 disorder Diseases 0.000 claims 22
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 22
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical group C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 20
- 239000008194 pharmaceutical composition Substances 0.000 claims 19
- 150000003839 salts Chemical class 0.000 claims 14
- 125000003545 alkoxy group Chemical group 0.000 claims 11
- 239000003814 drug Substances 0.000 claims 10
- 230000003389 potentiating effect Effects 0.000 claims 10
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 10
- 210000004027 cell Anatomy 0.000 claims 9
- 229940079593 drug Drugs 0.000 claims 9
- 125000000753 cycloalkyl group Chemical group 0.000 claims 8
- 201000000980 schizophrenia Diseases 0.000 claims 8
- 230000005062 synaptic transmission Effects 0.000 claims 8
- 208000028017 Psychotic disease Diseases 0.000 claims 7
- 208000019901 Anxiety disease Diseases 0.000 claims 6
- 208000018737 Parkinson disease Diseases 0.000 claims 6
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 6
- 208000020925 Bipolar disease Diseases 0.000 claims 5
- 239000003937 drug carrier Substances 0.000 claims 5
- 208000010877 cognitive disease Diseases 0.000 claims 4
- 208000031091 Amnestic disease Diseases 0.000 claims 3
- 206010012218 Delirium Diseases 0.000 claims 3
- 208000030814 Eating disease Diseases 0.000 claims 3
- 208000019454 Feeding and Eating 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
- 230000036506 anxiety Effects 0.000 claims 3
- 235000014632 disordered eating Nutrition 0.000 claims 3
- 235000020824 obesity Nutrition 0.000 claims 3
- 238000001228 spectrum Methods 0.000 claims 3
- 208000027691 Conduct disease Diseases 0.000 claims 2
- 208000019022 Mood disease Diseases 0.000 claims 2
- 208000016285 Movement disease Diseases 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 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
- 208000020706 Autistic disease Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 208000012661 Dyskinesia Diseases 0.000 claims 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 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
- 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
- 208000015802 attention deficit-hyperactivity disease Diseases 0.000 claims 1
- 230000003542 behavioural effect Effects 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 208000035548 disruptive behavior disease Diseases 0.000 claims 1
- 239000003623 enhancer Substances 0.000 claims 1
- 230000002708 enhancing effect Effects 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 230000000848 glutamatergic effect Effects 0.000 claims 1
- 210000005260 human cell Anatomy 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 208000024714 major depressive disease Diseases 0.000 claims 1
- 210000004962 mammalian cell Anatomy 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- 230000001095 motoneuron effect Effects 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
- 230000006576 neuronal survival Effects 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 abstract 1
- 208000025966 Neurological disease Diseases 0.000 abstract 1
- 229930195712 glutamate Natural products 0.000 abstract 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
- A61K31/435—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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/425—Thiazoles
- A61K31/426—1,3-Thiazoles
-
- 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
- A61K31/433—Thidiazoles
-
- 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
- A61K31/435—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
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- 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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
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- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07D401/12—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
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D417/12—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 linked by a chain containing hetero atoms as chain links
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Pain & Pain Management (AREA)
- Obesity (AREA)
- Psychology (AREA)
- Hematology (AREA)
- Psychiatry (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US33392610P | 2010-05-12 | 2010-05-12 | |
| US61/333,926 | 2010-05-12 | ||
| PCT/US2011/036308 WO2011143466A1 (en) | 2010-05-12 | 2011-05-12 | Heterocyclic sulfone mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2798514A1 true CA2798514A1 (en) | 2011-11-17 |
Family
ID=44914713
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2798514A Abandoned CA2798514A1 (en) | 2010-05-12 | 2011-05-12 | Heterocyclic sulfone mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US9192603B2 (enExample) |
| EP (1) | EP2568809A4 (enExample) |
| JP (1) | JP2013526544A (enExample) |
| KR (1) | KR20130079429A (enExample) |
| CN (1) | CN102939006A (enExample) |
| AU (1) | AU2011252974A1 (enExample) |
| BR (1) | BR112012028894A2 (enExample) |
| CA (1) | CA2798514A1 (enExample) |
| IL (1) | IL222854A0 (enExample) |
| MX (1) | MX2012013031A (enExample) |
| RU (1) | RU2012154447A (enExample) |
| SG (1) | SG185414A1 (enExample) |
| WO (1) | WO2011143466A1 (enExample) |
Families Citing this family (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2735521A1 (en) | 2008-09-04 | 2010-03-11 | Boehringer Ingelheim International Gmbh | Indolizine inhibitors of leukotriene production |
| WO2010088406A1 (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 |
| WO2011068821A1 (en) | 2009-12-04 | 2011-06-09 | Boehringer Ingelheim International Gmbh | Benzimidazole inhibitors of leukotriene production |
| WO2012024150A1 (en) | 2010-08-16 | 2012-02-23 | Boehringer Ingelheim International Gmbh | Oxadiazole inhibitors of leukotriene production |
| JP5862669B2 (ja) | 2010-08-26 | 2016-02-16 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ロイコトリエン産生のオキサジアゾール阻害剤 |
| EP2619197B1 (en) | 2010-09-23 | 2015-08-05 | Boehringer Ingelheim International GmbH | Oxadiazole inhibitors of leukotriene production |
| WO2012040137A1 (en) | 2010-09-23 | 2012-03-29 | Boehringer Ingelheim International Gmbh | Oxadiazole inhibitors of leukotriene production |
| EP2632915B1 (en) | 2010-10-29 | 2015-08-12 | Boehringer Ingelheim International GmbH | Benzimidazole inhibitors of leukotriene production |
| EP2635566B1 (en) | 2010-11-01 | 2018-05-16 | Boehringer Ingelheim International GmbH | Benzimidazole inhibitors of leukotriene production |
| EP2651930B1 (en) | 2010-12-16 | 2015-10-28 | Boehringer Ingelheim International GmbH | Biarylamide inhibitors of leukotriene production |
| AR089853A1 (es) | 2012-02-01 | 2014-09-24 | Boehringer Ingelheim Int | Inhibidores de oxadiazol de la produccion de leucotrienos para terapia de combinacion, composicion farmaceutica, uso |
| EP2863738A2 (en) | 2012-06-14 | 2015-04-29 | Basf Se | Pesticidal methods using substituted 3-pyridyl thiazole compounds and derivatives for combating animal pests |
| SI3049409T1 (sl) * | 2013-09-25 | 2017-08-31 | F. Hoffmann-La Roche Ag | Derivati etinila |
| WO2016115272A1 (en) | 2015-01-13 | 2016-07-21 | Vanderbilt University | Benzothiazole and benzisothiazole-substituted compounds as mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
| WO2016123627A1 (en) | 2015-01-30 | 2016-08-04 | Vanderbilt University | Isoquiniline and napthalene-substituted compounds as mglur4 allosteric potentiators, compounds, and methods of treating neurological dysfunction |
| WO2016123629A1 (en) | 2015-01-30 | 2016-08-04 | Vanderbilt University | Indazole and azaindazole 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 |
| WO2016202935A1 (en) | 2015-06-19 | 2016-12-22 | Bayer Pharma Aktiengesellschaft | Glucose transport inhibitors |
| 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 |
| 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 |
| US10968227B2 (en) | 2016-11-08 | 2021-04-06 | Vanderbilt University | Isoquinoline ether compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
| US11242342B2 (en) | 2016-11-08 | 2022-02-08 | Vanderbilt University | Isoquinoline amine compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
| JP7098630B2 (ja) | 2017-01-10 | 2022-07-11 | バイエル・アクチエンゲゼルシヤフト | 有害生物防除剤としてのヘテロサイクレン誘導体 |
| KR102515694B1 (ko) | 2017-01-10 | 2023-03-29 | 바이엘 악티엔게젤샤프트 | 해충 방제제로서의 헤테로사이클 유도체 |
| WO2019006157A1 (en) | 2017-06-28 | 2019-01-03 | Vanderbilt University | Pyridine quinoline compounds as mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
| UA128084C2 (uk) | 2017-08-16 | 2024-04-03 | Вандербілт Юніверсіті | ІНДАЗОЛОВІ СПОЛУКИ ЯК АЛОСТЕРИЧНІ ПОТЕНЦІАТОРИ mGLuR4, КОМПОЗИЦІЇ І СПОСОБИ ЛІКУВАННЯ НЕВРОЛОГІЧНИХ ДИСФУНКЦІЙ |
| EP4227302A1 (en) | 2018-02-13 | 2023-08-16 | Gilead Sciences, Inc. | Pd-1/pd-l1 inhibitors |
| US11724997B2 (en) | 2018-03-01 | 2023-08-15 | Annapurna Bio, Inc. | Compounds and compositions for treating conditions associated with APJ receptor activity |
| US10899735B2 (en) | 2018-04-19 | 2021-01-26 | Gilead Sciences, Inc. | PD-1/PD-L1 inhibitors |
| UA126421C2 (uk) | 2018-07-13 | 2022-09-28 | Гіліад Сайєнсіз, Інк. | Інгібітори pd-1/pd-l1 |
| AU2019366355B2 (en) | 2018-10-24 | 2022-10-13 | Gilead Sciences, Inc. | PD-1/PD-L1 inhibitors |
| JP7627008B2 (ja) | 2019-04-03 | 2025-02-05 | アリゴス セラピューティクス インコーポレイテッド | ピロール化合物 |
| WO2021127643A1 (en) | 2019-12-20 | 2021-06-24 | Tenaya Therapeutics, Inc. | Fluoroalkyl-oxadiazoles and uses thereof |
| WO2022002818A1 (de) | 2020-07-02 | 2022-01-06 | Bayer Aktiengesellschaft | Heterocyclen-derivate als schädlingsbekämpfungsmittel |
| US20240252502A1 (en) | 2021-05-04 | 2024-08-01 | Tenaya Therapeutics, Inc. | Hdac6 inhibitors for treatment of metabolic disease and hfpef |
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|---|---|---|---|---|
| DE3272640D1 (en) | 1982-01-22 | 1986-09-18 | Basf Ag | Thiadiazole derivatives, process for their preparation, and their use in combatting unwanted plant growth |
| US6262096B1 (en) | 1997-11-12 | 2001-07-17 | Bristol-Myers Squibb Company | Aminothiazole inhibitors of cyclin dependent kinases |
| US6040321A (en) | 1997-11-12 | 2000-03-21 | Bristol-Myers Squibb Company | Aminothiazole inhibitors of cyclin dependent kinases |
| US6468977B1 (en) | 1998-03-02 | 2002-10-22 | Apotex Inc. | Thiadiazole compounds useful as inhibitors of cysteine activity dependent enzymes |
| US6162791A (en) | 1998-03-02 | 2000-12-19 | Apotex Inc. | Thiadiazole compounds useful as inhibitors of cysteine activity dependent enzymes |
| WO1999047507A2 (en) | 1998-03-19 | 1999-09-23 | Pharmacia & Upjohn Company | 1,3,4-thiadiazoles useful for the treatment of cmv infections |
| DK1347971T3 (da) | 2000-12-21 | 2006-05-15 | Bristol Myers Squibb Co | Thiazolylinhibitorer af tyrosinkinaser fra Tec-familien |
| WO2005007096A2 (en) | 2003-07-11 | 2005-01-27 | Merck & Co., Inc. | Treatment of movement disorders with a metabotropic glutamate 4 receptor positive allosteric modulator |
| JP2009524677A (ja) | 2006-01-25 | 2009-07-02 | シンタ ファーマシューティカルズ コーポレーション | 炎症および免疫関連使用用のチアゾールおよびチアジアゾール化合物 |
| US7951824B2 (en) * | 2006-02-17 | 2011-05-31 | Hoffman-La Roche Inc. | 4-aryl-pyridine-2-carboxyamide derivatives |
| JP5448164B2 (ja) | 2006-07-28 | 2014-03-19 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ｃｂ２受容体を変調する化合物 |
| EP2074084B1 (en) | 2006-09-25 | 2013-08-28 | Boehringer Ingelheim International GmbH | Compounds which modulate the cb2 receptor |
| MX2009003892A (es) * | 2006-10-25 | 2009-04-23 | Neurosearch As | Compuestos de oxadiazol y tiadiazol y su uso como moduladores del receptor de acetilcolina nicotinico. |
| GB0622202D0 (en) | 2006-11-07 | 2006-12-20 | Addex Pharmaceuticals Sa | Novel compounds |
| GB0713686D0 (en) * | 2007-07-13 | 2007-08-22 | Addex Pharmaceuticals Sa | New compounds 2 |
| WO2010033350A1 (en) * | 2008-09-16 | 2010-03-25 | Merck & Co., Inc. | Sulfonamide derivative metabotropic glutamate r4 ligands |
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2011
- 2011-05-12 JP JP2013510307A patent/JP2013526544A/ja not_active Withdrawn
- 2011-05-12 KR KR1020127032242A patent/KR20130079429A/ko not_active Withdrawn
- 2011-05-12 CN CN201180029055XA patent/CN102939006A/zh active Pending
- 2011-05-12 US US13/697,783 patent/US9192603B2/en active Active
- 2011-05-12 MX MX2012013031A patent/MX2012013031A/es not_active Application Discontinuation
- 2011-05-12 RU RU2012154447/04A patent/RU2012154447A/ru not_active Application Discontinuation
- 2011-05-12 SG SG2012081162A patent/SG185414A1/en unknown
- 2011-05-12 CA CA2798514A patent/CA2798514A1/en not_active Abandoned
- 2011-05-12 BR BR112012028894A patent/BR112012028894A2/pt not_active IP Right Cessation
- 2011-05-12 WO PCT/US2011/036308 patent/WO2011143466A1/en not_active Ceased
- 2011-05-12 AU AU2011252974A patent/AU2011252974A1/en not_active Abandoned
- 2011-05-12 EP EP11781297.4A patent/EP2568809A4/en not_active Withdrawn
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2012
- 2012-11-05 IL IL222854A patent/IL222854A0/en unknown
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| SG185414A1 (en) | 2012-12-28 |
| MX2012013031A (es) | 2012-12-17 |
| KR20130079429A (ko) | 2013-07-10 |
| US9192603B2 (en) | 2015-11-24 |
| US20130158078A1 (en) | 2013-06-20 |
| IL222854A0 (en) | 2012-12-31 |
| AU2011252974A1 (en) | 2012-12-13 |
| CN102939006A (zh) | 2013-02-20 |
| RU2012154447A (ru) | 2014-06-20 |
| EP2568809A1 (en) | 2013-03-20 |
| WO2011143466A1 (en) | 2011-11-17 |
| BR112012028894A2 (pt) | 2019-09-24 |
| EP2568809A4 (en) | 2013-11-06 |
| JP2013526544A (ja) | 2013-06-24 |
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