JP2010526145A5 - - Google Patents
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- JP2010526145A5 JP2010526145A5 JP2010507528A JP2010507528A JP2010526145A5 JP 2010526145 A5 JP2010526145 A5 JP 2010526145A5 JP 2010507528 A JP2010507528 A JP 2010507528A JP 2010507528 A JP2010507528 A JP 2010507528A JP 2010526145 A5 JP2010526145 A5 JP 2010526145A5
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- Prior art keywords
- alkyl
- aryl
- heteroaryl
- cycloalkyl
- independently
- 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.)
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- 125000000217 alkyl group Chemical group 0.000 claims 97
- 125000001072 heteroaryl group Chemical group 0.000 claims 91
- 125000003118 aryl group Chemical group 0.000 claims 88
- 125000000623 heterocyclic group Chemical group 0.000 claims 56
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 42
- 125000005843 halogen group Chemical group 0.000 claims 36
- 229910052739 hydrogen Inorganic materials 0.000 claims 36
- 239000001257 hydrogen Substances 0.000 claims 36
- 125000004093 cyano group Chemical group *C#N 0.000 claims 33
- 125000000753 cycloalkyl group Chemical group 0.000 claims 32
- 150000002431 hydrogen Chemical class 0.000 claims 27
- 229910052760 oxygen Inorganic materials 0.000 claims 23
- 150000001875 compounds Chemical class 0.000 claims 21
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 21
- -1 —NH 2 Chemical group 0.000 claims 19
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 17
- 229910052717 sulfur Inorganic materials 0.000 claims 17
- 125000005842 heteroatom Chemical group 0.000 claims 11
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 8
- 125000003342 alkenyl group Chemical group 0.000 claims 8
- 125000000304 alkynyl group Chemical group 0.000 claims 8
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 8
- 125000003710 aryl alkyl group Chemical group 0.000 claims 7
- 125000001424 substituent group Chemical group 0.000 claims 6
- 229910052799 carbon Inorganic materials 0.000 claims 5
- 125000001188 haloalkyl group Chemical group 0.000 claims 5
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 208000032928 Dyslipidaemia Diseases 0.000 claims 3
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 3
- 239000003795 chemical substances by application Substances 0.000 claims 3
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 229940124597 therapeutic agent Drugs 0.000 claims 3
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims 2
- 206010020772 Hypertension Diseases 0.000 claims 2
- 208000008589 Obesity Diseases 0.000 claims 2
- 239000013543 active substance Substances 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 201000001421 hyperglycemia Diseases 0.000 claims 2
- 208000031225 myocardial ischemia Diseases 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- BCMCBBGGLRIHSE-UHFFFAOYSA-N 1,3-benzoxazole Chemical compound C1=CC=C2OC=NC2=C1 BCMCBBGGLRIHSE-UHFFFAOYSA-N 0.000 claims 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000020084 Bone disease Diseases 0.000 claims 1
- 208000028698 Cognitive impairment Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 102000003688 G-Protein-Coupled Receptors Human genes 0.000 claims 1
- 108090000045 G-Protein-Coupled Receptors Proteins 0.000 claims 1
- 208000010412 Glaucoma Diseases 0.000 claims 1
- 229940089838 Glucagon-like peptide 1 receptor agonist Drugs 0.000 claims 1
- 208000002705 Glucose Intolerance Diseases 0.000 claims 1
- 102100033839 Glucose-dependent insulinotropic receptor Human genes 0.000 claims 1
- 108010010369 HIV Protease Proteins 0.000 claims 1
- 101000996752 Homo sapiens Glucose-dependent insulinotropic receptor Proteins 0.000 claims 1
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 1
- 206010060378 Hyperinsulinaemia Diseases 0.000 claims 1
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 1
- 206010022489 Insulin Resistance Diseases 0.000 claims 1
- 206010049287 Lipodystrophy acquired Diseases 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 206010033645 Pancreatitis Diseases 0.000 claims 1
- 208000017442 Retinal disease Diseases 0.000 claims 1
- 206010038923 Retinopathy Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 230000000747 cardiac effect Effects 0.000 claims 1
- 208000010877 cognitive disease Diseases 0.000 claims 1
- 230000001149 cognitive effect Effects 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 230000003111 delayed effect Effects 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000004064 dysfunction Effects 0.000 claims 1
- 239000012634 fragment Substances 0.000 claims 1
- 239000003877 glucagon like peptide 1 receptor agonist Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 230000003451 hyperinsulinaemic effect Effects 0.000 claims 1
- 201000008980 hyperinsulinism Diseases 0.000 claims 1
- 208000006575 hypertriglyceridemia Diseases 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 150000002632 lipids Chemical class 0.000 claims 1
- 208000006132 lipodystrophy Diseases 0.000 claims 1
- 239000003607 modifier Substances 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 201000001119 neuropathy Diseases 0.000 claims 1
- 230000007823 neuropathy Effects 0.000 claims 1
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 201000009104 prediabetes syndrome Diseases 0.000 claims 1
- 230000000069 prophylactic effect Effects 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 125000003107 substituted aryl group Chemical group 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
- 230000002792 vascular Effects 0.000 claims 1
- 230000029663 wound healing Effects 0.000 claims 1
- OOHGCTWLGFSIMI-UHFFFAOYSA-N CC(C)(C)OC(N(CC1)CCC1N1c(ncnc2Nc3c(C)nc(C(F)(F)F)cc3)c2OCCC1)=O Chemical compound CC(C)(C)OC(N(CC1)CCC1N1c(ncnc2Nc3c(C)nc(C(F)(F)F)cc3)c2OCCC1)=O OOHGCTWLGFSIMI-UHFFFAOYSA-N 0.000 description 1
- GZZBBIOTKMFGIC-UHFFFAOYSA-N CC(C)(C)OC(N(CC1)CCC1N1c(ncnc2Oc3c(C)nccc3)c2OCCC1)=O Chemical compound CC(C)(C)OC(N(CC1)CCC1N1c(ncnc2Oc3c(C)nccc3)c2OCCC1)=O GZZBBIOTKMFGIC-UHFFFAOYSA-N 0.000 description 1
- RLLFMNMJIIVVSX-UHFFFAOYSA-N CC(C)(C)OC(N(CC1)CCC1N1c2ncnc(Nc(cc3)c(C)nc3-[n]3ncnc3)c2OCCC1)=O Chemical compound CC(C)(C)OC(N(CC1)CCC1N1c2ncnc(Nc(cc3)c(C)nc3-[n]3ncnc3)c2OCCC1)=O RLLFMNMJIIVVSX-UHFFFAOYSA-N 0.000 description 1
- MFVJSINRYYGIQD-UHFFFAOYSA-N CC(C)OC(N(CC1)CCC1N(C(C=C1)=O)c2c1c(Oc1cccnc1C)ncn2)=O Chemical compound CC(C)OC(N(CC1)CCC1N(C(C=C1)=O)c2c1c(Oc1cccnc1C)ncn2)=O MFVJSINRYYGIQD-UHFFFAOYSA-N 0.000 description 1
- 0 CC(C)OC(N(CC1)CCC1N1c(ncnc2*c(cc3)c(C)nc3-[n]3ncnc3)c2OCCC1)=O Chemical compound CC(C)OC(N(CC1)CCC1N1c(ncnc2*c(cc3)c(C)nc3-[n]3ncnc3)c2OCCC1)=O 0.000 description 1
- OYPJJYBFKYKASD-UHFFFAOYSA-N CC(C)OC(N(CC1)CCC1N1c(ncnc2Nc(c(C)ccn3)c3Cl)c2OCCC1)=O Chemical compound CC(C)OC(N(CC1)CCC1N1c(ncnc2Nc(c(C)ccn3)c3Cl)c2OCCC1)=O OYPJJYBFKYKASD-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US91594407P | 2007-05-04 | 2007-05-04 | |
| PCT/US2008/061928 WO2008137435A1 (en) | 2007-05-04 | 2008-04-30 | [6,6] and [6,7]-bicyclic gpr119 g protein-coupled receptor agonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010526145A JP2010526145A (ja) | 2010-07-29 |
| JP2010526145A5 true JP2010526145A5 (cg-RX-API-DMAC7.html) | 2011-05-12 |
Family
ID=39705174
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010507528A Withdrawn JP2010526145A (ja) | 2007-05-04 | 2008-04-30 | ［６，６］および［６，７］−二環式ｇｐｒ１１９ｇタンパク質結合受容体アゴニスト |
Country Status (10)
| Country | Link |
|---|---|
| US (4) | US7910583B2 (cg-RX-API-DMAC7.html) |
| EP (1) | EP2144902B1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP2010526145A (cg-RX-API-DMAC7.html) |
| CN (1) | CN101668756A (cg-RX-API-DMAC7.html) |
| AR (1) | AR066437A1 (cg-RX-API-DMAC7.html) |
| CL (1) | CL2008001271A1 (cg-RX-API-DMAC7.html) |
| ES (1) | ES2388967T3 (cg-RX-API-DMAC7.html) |
| PE (1) | PE20090222A1 (cg-RX-API-DMAC7.html) |
| TW (1) | TW200848055A (cg-RX-API-DMAC7.html) |
| WO (1) | WO2008137435A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (65)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7407955B2 (en) | 2002-08-21 | 2008-08-05 | Boehringer Ingelheim Pharma Gmbh & Co., Kg | 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions |
| DE102004054054A1 (de) | 2004-11-05 | 2006-05-11 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Verfahren zur Herstellung chiraler 8-(3-Amino-piperidin-1-yl)-xanthine |
| PE20080251A1 (es) | 2006-05-04 | 2008-04-25 | Boehringer Ingelheim Int | Usos de inhibidores de dpp iv |
| EP1852108A1 (en) | 2006-05-04 | 2007-11-07 | Boehringer Ingelheim Pharma GmbH & Co.KG | DPP IV inhibitor formulations |
| JP5323684B2 (ja) | 2006-05-04 | 2013-10-23 | 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 | 多形体 |
| NZ582661A (en) * | 2007-07-17 | 2012-03-30 | Bristol Myers Squibb Co | Method for modulating gpr119 g protein-coupled receptor and selected compounds |
| PE20091730A1 (es) | 2008-04-03 | 2009-12-10 | Boehringer Ingelheim Int | Formulaciones que comprenden un inhibidor de dpp4 |
| US8188098B2 (en) | 2008-05-19 | 2012-05-29 | Hoffmann-La Roche Inc. | GPR119 receptor agonists |
| MX2011000664A (es) * | 2008-07-16 | 2011-02-24 | Schering Corp | Derivados biciclicos heterociclicos y uso de los mismos como moduladores de gpr119. |
| US20110118286A1 (en) * | 2008-07-16 | 2011-05-19 | Santhosh Francis Neelamkavil | Bicyclic heterocycle derivatives and their use as gpcr modulators |
| CA2730606A1 (en) * | 2008-07-16 | 2010-01-21 | Schering Corporation | Bicyclic heterocycle derivatives and methods of use thereof |
| TW201006821A (en) * | 2008-07-16 | 2010-02-16 | Bristol Myers Squibb Co | Pyridone and pyridazone analogues as GPR119 modulators |
| BRPI0916997A2 (pt) | 2008-08-06 | 2020-12-15 | Boehringer Ingelheim International Gmbh | Inibidor de dpp-4 e seu uso |
| US20200155558A1 (en) | 2018-11-20 | 2020-05-21 | Boehringer Ingelheim International Gmbh | Treatment for diabetes in patients with insufficient glycemic control despite therapy with an oral antidiabetic drug |
| TWI508965B (zh) | 2008-12-23 | 2015-11-21 | Boehringer Ingelheim Int | 有機化合物的鹽形式 |
| WO2010075273A1 (en) * | 2008-12-23 | 2010-07-01 | Schering Corporation | Bicyclic heterocycle derivatives and methods of use thereof |
| US20120016119A1 (en) * | 2009-01-22 | 2012-01-19 | Yasunori Tsuboi | NOVEL PYRROLO(2,3-d)PYRIMIDINE COMPOUND |
| WO2010088518A2 (en) * | 2009-01-31 | 2010-08-05 | Kalypsys, Inc. | Heterocyclic modulators of gpr119 for treatment of disease |
| JP5657518B2 (ja) | 2009-02-18 | 2015-01-21 | 武田薬品工業株式会社 | 縮合複素環化合物 |
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| JP2012530758A (ja) | 2009-06-24 | 2012-12-06 | 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 | 新規化合物、医薬組成物及びそれに関する方法 |
| EA201200046A1 (ru) | 2009-06-24 | 2012-08-30 | Бёрингер Ингельхайм Интернациональ Гмбх | Новые соединения, фармацевтическая композиция и связанные с ними способы |
| KR20190071840A (ko) | 2009-11-27 | 2019-06-24 | 베링거 인겔하임 인터내셔날 게엠베하 | 리나글립틴과 같은 ｄｐｐ－ｉｖ 억제제를 사용한 유전자형 검사된 당뇨병 환자의 치료 |
| WO2011107494A1 (de) | 2010-03-03 | 2011-09-09 | Sanofi | Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
| EP2547339A1 (en) | 2010-03-18 | 2013-01-23 | Boehringer Ingelheim International GmbH | Combination of a gpr119 agonist and the dpp-iv inhibitor linagliptin for use in the treatment of diabetes and related conditions |
| SG184168A1 (en) | 2010-04-08 | 2012-10-30 | Bristol Myers Squibb Co | Pyrimidinylpiperidinyloxypyridinone analogues as gpr119 modulators |
| MX366325B (es) | 2010-05-05 | 2019-07-05 | Boehringer Ingelheim Int | Terapia de combinacion. |
| JP2013525489A (ja) | 2010-05-06 | 2013-06-20 | ブリストル−マイヤーズ スクイブ カンパニー | Ｇｐｒ１１９修飾因子としての二環式ヘテロアリール類似体 |
| US8729084B2 (en) | 2010-05-06 | 2014-05-20 | Bristol-Myers Squibb Company | Benzofuranyl analogues as GPR119 modulators |
| TW201202230A (en) * | 2010-05-24 | 2012-01-16 | Mitsubishi Tanabe Pharma Corp | Novel quinazoline compound |
| US8530413B2 (en) | 2010-06-21 | 2013-09-10 | Sanofi | Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments |
| CA2803504C (en) | 2010-06-24 | 2022-08-30 | Boehringer Ingelheim International Gmbh | A combination for diabetes therapy comprising linagliptin and a long-acting insulin |
| TW201215388A (en) | 2010-07-05 | 2012-04-16 | Sanofi Sa | (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments |
| TW201215387A (en) | 2010-07-05 | 2012-04-16 | Sanofi Aventis | Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament |
| TW201221505A (en) | 2010-07-05 | 2012-06-01 | Sanofi Sa | Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament |
| BR112013008100A2 (pt) | 2010-09-22 | 2016-08-09 | Arena Pharm Inc | "moduladores do receptor de gpr19 e o tratamento de distúrbios relacionados a eles." |
| JP2013253019A (ja) * | 2010-09-28 | 2013-12-19 | Kowa Co | 新規なピペリジン誘導体及びこれを含有する医薬 |
| US9034883B2 (en) | 2010-11-15 | 2015-05-19 | Boehringer Ingelheim International Gmbh | Vasoprotective and cardioprotective antidiabetic therapy |
| UY33805A (es) * | 2010-12-17 | 2012-07-31 | Boehringer Ingelheim Int | ?Derivados de dihidrobenzofuranil-piperidinilo, aza-dihidrobenzofuranilpiperidinilo y diaza-dihidrobenzofuranil-piperidinilo, composiciones farmacéuticas que los contienen y usos de los mismos?. |
| JP2014501274A (ja) * | 2011-01-03 | 2014-01-20 | ハンミ ファーム． シーオー．， エルティーディー． | Ｇタンパク質共役受容体調節のための新規な二環式化合物 |
| CN102617548A (zh) * | 2011-01-31 | 2012-08-01 | 北京赛林泰医药技术有限公司 | 作为gpr受体激动剂的双环杂芳基化合物及其组合物和应用 |
| EA031618B1 (ru) | 2011-06-09 | 2019-01-31 | Ризен Фармасьютикалз Са | Соединения-модуляторы gpr-119 |
| KR101985384B1 (ko) | 2011-07-15 | 2019-06-03 | 베링거 인겔하임 인터내셔날 게엠베하 | 치환된 퀴나졸린, 이의 제조 및 약제학적 조성물에서의 이의 용도 |
| WO2013037390A1 (en) | 2011-09-12 | 2013-03-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| WO2013045413A1 (en) | 2011-09-27 | 2013-04-04 | Sanofi | 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| US9555001B2 (en) | 2012-03-07 | 2017-01-31 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition and uses thereof |
| EP2849755A1 (en) | 2012-05-14 | 2015-03-25 | Boehringer Ingelheim International GmbH | A xanthine derivative as dpp -4 inhibitor for use in the treatment of podocytes related disorders and/or nephrotic syndrome |
| JP6218811B2 (ja) | 2012-05-14 | 2017-10-25 | 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 | Ｓｉｒｓ及び／又は敗血症の治療に用いるｄｐｐ−４阻害薬としてのキサンチン誘導体 |
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2008
- 2008-04-30 JP JP2010507528A patent/JP2010526145A/ja not_active Withdrawn
- 2008-04-30 CN CN200880014028A patent/CN101668756A/zh active Pending
- 2008-04-30 PE PE2008000777A patent/PE20090222A1/es not_active Application Discontinuation
- 2008-04-30 EP EP08747129A patent/EP2144902B1/en not_active Not-in-force
- 2008-04-30 ES ES08747129T patent/ES2388967T3/es active Active
- 2008-04-30 US US12/112,080 patent/US7910583B2/en active Active
- 2008-04-30 WO PCT/US2008/061928 patent/WO2008137435A1/en not_active Ceased
- 2008-05-02 TW TW097116364A patent/TW200848055A/zh unknown
- 2008-05-02 AR ARP080101887A patent/AR066437A1/es not_active Application Discontinuation
- 2008-05-02 CL CL200801271A patent/CL2008001271A1/es unknown
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2011
- 2011-02-08 US US13/022,819 patent/US8076322B2/en active Active
- 2011-11-04 US US13/289,375 patent/US8314095B2/en active Active
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2012
- 2012-10-10 US US13/648,436 patent/US8513265B2/en active Active