AR051675A1 - Derivados de 3-fenil-pirazol como moduladores del receptor 5-ht2a de la serotonina utiles para el tratamiento de trastornos relacionados con este - Google Patents
Derivados de 3-fenil-pirazol como moduladores del receptor 5-ht2a de la serotonina utiles para el tratamiento de trastornos relacionados con esteInfo
- Publication number
- AR051675A1 AR051675A1 ARP050104844A ARP050104844A AR051675A1 AR 051675 A1 AR051675 A1 AR 051675A1 AR P050104844 A ARP050104844 A AR P050104844A AR P050104844 A ARP050104844 A AR P050104844A AR 051675 A1 AR051675 A1 AR 051675A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkoxy
- alkyl
- cycloalkyl
- alkenyl
- group
- Prior art date
Links
- 102100036321 5-hydroxytryptamine receptor 2A Human genes 0.000 title 1
- 101710138091 5-hydroxytryptamine receptor 2A Proteins 0.000 title 1
- 102000005962 receptors Human genes 0.000 title 1
- 108020003175 receptors Proteins 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 11
- -1 C1-6 alkylureyl Chemical group 0.000 abstract 11
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 11
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 10
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 10
- 229910052736 halogen Inorganic materials 0.000 abstract 10
- 150000002367 halogens Chemical group 0.000 abstract 10
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 9
- 125000005431 alkyl carboxamide group Chemical group 0.000 abstract 9
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 abstract 8
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 8
- 125000002252 acyl group Chemical group 0.000 abstract 8
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 8
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 8
- 125000001424 substituent group Chemical group 0.000 abstract 8
- 125000004423 acyloxy group Chemical group 0.000 abstract 7
- 125000004422 alkyl sulphonamide group Chemical group 0.000 abstract 7
- 125000005392 carboxamide group Chemical class NC(=O)* 0.000 abstract 7
- 125000005432 dialkylcarboxamide group Chemical group 0.000 abstract 7
- 125000001072 heteroaryl group Chemical group 0.000 abstract 7
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 7
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 6
- 125000004995 haloalkylthio group Chemical group 0.000 abstract 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 6
- 208000028017 Psychotic disease Diseases 0.000 abstract 5
- 125000000623 heterocyclic group Chemical group 0.000 abstract 5
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 abstract 4
- 125000004738 (C1-C6) alkyl sulfinyl group Chemical group 0.000 abstract 4
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 abstract 4
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 abstract 4
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 abstract 4
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 4
- 125000004749 (C1-C6) haloalkylsulfinyl group Chemical group 0.000 abstract 4
- 125000004741 (C1-C6) haloalkylsulfonyl group Chemical group 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 4
- 229940124530 sulfonamide Drugs 0.000 abstract 4
- 125000003396 thiol group Chemical class [H]S* 0.000 abstract 4
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 abstract 3
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 3
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 3
- 125000005277 alkyl imino group Chemical group 0.000 abstract 3
- 125000005363 dialkylsulfonamide group Chemical group 0.000 abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 3
- 208000035475 disorder Diseases 0.000 abstract 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 3
- 201000000980 schizophrenia Diseases 0.000 abstract 3
- 150000003456 sulfonamides Chemical class 0.000 abstract 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 2
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 abstract 2
- 125000004771 (C1-C4) haloalkylsulfinyl group Chemical group 0.000 abstract 2
- 125000004414 alkyl thio group Chemical group 0.000 abstract 2
- 125000002947 alkylene group Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000004438 haloalkoxy group Chemical group 0.000 abstract 2
- 125000004441 haloalkylsulfonyl group Chemical group 0.000 abstract 2
- 125000004043 oxo group Chemical group O=* 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 208000024891 symptom Diseases 0.000 abstract 2
- 125000004768 (C1-C4) alkylsulfinyl group Chemical group 0.000 abstract 1
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 abstract 1
- 125000006624 (C1-C6) alkoxycarbonylamino group Chemical group 0.000 abstract 1
- 125000006705 (C5-C7) cycloalkyl group Chemical group 0.000 abstract 1
- 206010002383 Angina Pectoris Diseases 0.000 abstract 1
- 200000000007 Arterial disease Diseases 0.000 abstract 1
- 206010003658 Atrial Fibrillation Diseases 0.000 abstract 1
- 208000020925 Bipolar disease Diseases 0.000 abstract 1
- 201000004311 Gilles de la Tourette syndrome Diseases 0.000 abstract 1
- 101001043818 Mus musculus Interleukin-31 receptor subunit alpha Proteins 0.000 abstract 1
- 206010061921 Psychotic disorder due to a general medical condition Diseases 0.000 abstract 1
- 208000006011 Stroke Diseases 0.000 abstract 1
- 208000000323 Tourette Syndrome Diseases 0.000 abstract 1
- 208000016620 Tourette disease Diseases 0.000 abstract 1
- 238000013019 agitation Methods 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 208000006673 asthma Diseases 0.000 abstract 1
- 230000003542 behavioural effect Effects 0.000 abstract 1
- 229910052794 bromium Inorganic materials 0.000 abstract 1
- 229910052801 chlorine Inorganic materials 0.000 abstract 1
- 230000035602 clotting Effects 0.000 abstract 1
- 125000006254 cycloalkyl carbonyl group Chemical group 0.000 abstract 1
- 125000002993 cycloalkylene group Chemical group 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 230000002964 excitative effect Effects 0.000 abstract 1
- 229910052731 fluorine Inorganic materials 0.000 abstract 1
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 abstract 1
- 230000000302 ischemic effect Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 208000010125 myocardial infarction Diseases 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 206010036807 progressive multifocal leukoencephalopathy Diseases 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 208000019116 sleep disease Diseases 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 208000010110 spontaneous platelet aggregation Diseases 0.000 abstract 1
- 230000001052 transient effect Effects 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- 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
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
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- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
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- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
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- A61P9/12—Antihypertensives
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings 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
- C07D231/16—Halogen atoms or nitro radicals
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- C—CHEMISTRY; METALLURGY
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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
- C07D401/12—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
- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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- 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
- C07D413/10—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 carbon chain containing aromatic rings
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- 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
-
- 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
- C07D487/08—Bridged systems
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Diabetes (AREA)
- Biomedical Technology (AREA)
- Epidemiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Cardiology (AREA)
- Pulmonology (AREA)
- Obesity (AREA)
- Psychiatry (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Anesthesiology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US62977404P | 2004-11-19 | 2004-11-19 | |
| US64763905P | 2005-01-26 | 2005-01-26 | |
| US65838405P | 2005-03-02 | 2005-03-02 | |
| US71338405P | 2005-09-01 | 2005-09-01 | |
| US73316505P | 2005-11-04 | 2005-11-04 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR051675A1 true AR051675A1 (es) | 2007-01-31 |
Family
ID=36218810
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP050104844A AR051675A1 (es) | 2004-11-19 | 2005-11-17 | Derivados de 3-fenil-pirazol como moduladores del receptor 5-ht2a de la serotonina utiles para el tratamiento de trastornos relacionados con este |
Country Status (36)
Families Citing this family (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RS20060035A (sr) * | 2003-07-22 | 2008-08-07 | Arena Pharmaceuticals Inc., | Derivati diaril i arilheteroaril uree kao modulatori receptora 5-ht2a serotonina korisni u profilaksi i lečenju poremećaja u vezi sa njima |
| WO2005103011A1 (en) | 2004-03-23 | 2005-11-03 | Arena Pharmaceuticals, Inc. | Processes for preparing substituted n-aryl-n’-[3-(1h-pyrazol-5-yl) phenyl] ureas and intermediates thereof |
| PE20061130A1 (es) * | 2004-11-19 | 2007-01-05 | Arena Pharm Inc | Derivados de 3-fenil-pirazol como moduladores del receptor de serotonina 5-ht2a |
| MX349156B (es) * | 2006-05-18 | 2017-07-14 | Arena Pharm Inc | Formas cristalinas y procesos para la preparacion de fenil-pirazoles utiles como moduladores del receptor de serotonina 5-ht2a. |
| CN101479261A (zh) | 2006-05-18 | 2009-07-08 | 艾尼纳制药公司 | 3-吡唑基-苯甲酰胺-4-醚、其仲胺及其衍生物作为5-ht2a血清素受体的调节剂用于治疗与其相关的病症 |
| ES2536762T3 (es) | 2006-05-18 | 2015-05-28 | Arena Pharmaceuticals, Inc. | Aminas primarias y sus derivados como moduladores del receptor de la serotonina 5-HT2A útiles para el tratamiento de trastornos relacionados con este |
| JP2010502618A (ja) * | 2006-08-31 | 2010-01-28 | アリーナ ファーマシューティカルズ， インコーポレイテッド | セロトニン５−ｈｔ２ａ受容体のモジュレータとしてのベンゾフラン誘導体 |
| TWI415845B (zh) | 2006-10-03 | 2013-11-21 | Arena Pharm Inc | 用於治療與５-ｈｔ2ａ血清素受體相關聯病症之作為５-ｈｔ2ａ血清素受體之調節劑的吡唑衍生物 |
| WO2008054748A2 (en) * | 2006-10-31 | 2008-05-08 | Arena Pharmaceuticals, Inc. | Indazole derivatives as modulators of the 5-ht2a serotonin receptor useful for the treatment of disorders related thereto |
| ITMI20062230A1 (it) * | 2006-11-22 | 2008-05-23 | Acraf | Composto 2-alchil-indazolico procedimento per preparalo e composizione farmaceutica che lo comprende |
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2008
- 2008-11-13 CY CY20081101299T patent/CY1108508T1/el unknown
-
2010
- 2010-12-22 US US12/976,887 patent/US20110105456A1/en not_active Abandoned
-
2012
- 2012-09-14 US US13/616,842 patent/US8785441B2/en not_active Expired - Lifetime
-
2016
- 2016-04-25 US US15/137,228 patent/US20160304463A1/en not_active Abandoned
-
2018
- 2018-11-01 US US16/177,672 patent/US10781180B2/en not_active Expired - Lifetime
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