RU2010109449A - Фармацевтическая композиция, включающая ингибитор sglt2 в комбинации с ингибитором дпп-iv - Google Patents
Фармацевтическая композиция, включающая ингибитор sglt2 в комбинации с ингибитором дпп-iv Download PDFInfo
- Publication number
- RU2010109449A RU2010109449A RU2010109449/15A RU2010109449A RU2010109449A RU 2010109449 A RU2010109449 A RU 2010109449A RU 2010109449/15 A RU2010109449/15 A RU 2010109449/15A RU 2010109449 A RU2010109449 A RU 2010109449A RU 2010109449 A RU2010109449 A RU 2010109449A
- Authority
- RU
- Russia
- Prior art keywords
- methyl
- inhibitor
- aminopiperidin
- butyn
- xanthine
- Prior art date
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- 108010067722 Dipeptidyl Peptidase 4 Proteins 0.000 title claims abstract 12
- 102100025012 Dipeptidyl peptidase 4 Human genes 0.000 title claims abstract 12
- 239000003112 inhibitor Substances 0.000 title claims abstract 12
- 229940123518 Sodium/glucose cotransporter 2 inhibitor Drugs 0.000 title claims abstract 11
- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract 11
- -1 ([1,5] naphthyridin-2-yl) methyl Chemical group 0.000 claims abstract 22
- 150000003839 salts Chemical class 0.000 claims abstract 8
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims abstract 4
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims abstract 4
- XTNGUQKDFGDXSJ-ZXGKGEBGSA-N Canagliflozin Chemical compound CC1=CC=C([C@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O2)O)C=C1CC(S1)=CC=C1C1=CC=C(F)C=C1 XTNGUQKDFGDXSJ-ZXGKGEBGSA-N 0.000 claims abstract 3
- JVHXJTBJCFBINQ-ADAARDCZSA-N Dapagliflozin Chemical compound C1=CC(OCC)=CC=C1CC1=CC([C@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O2)O)=CC=C1Cl JVHXJTBJCFBINQ-ADAARDCZSA-N 0.000 claims abstract 3
- LTXREWYXXSTFRX-QGZVFWFLSA-N Linagliptin Chemical compound N=1C=2N(C)C(=O)N(CC=3N=C4C=CC=CC4=C(C)N=3)C(=O)C=2N(CC#CC)C=1N1CCC[C@@H](N)C1 LTXREWYXXSTFRX-QGZVFWFLSA-N 0.000 claims abstract 3
- 229960003834 dapagliflozin Drugs 0.000 claims abstract 3
- 239000012453 solvate Substances 0.000 claims abstract 3
- DNLMJEXNHFAGLZ-YMQHIKHWSA-N (2r,3r,4s,5s,6r)-2-[4-chloro-3-[(4-ethylphenyl)methyl]phenyl]-6-(hydroxymethyl)oxane-2,3,4,5-tetrol Chemical compound C1=CC(CC)=CC=C1CC1=CC([C@]2(O)[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O2)O)=CC=C1Cl DNLMJEXNHFAGLZ-YMQHIKHWSA-N 0.000 claims abstract 2
- AGJJCLBOHJQGFA-ZQGJOIPISA-N (2s,3r,4r,5s,6r)-2-[5-(azulen-2-ylmethyl)-2-hydroxyphenyl]-6-(hydroxymethyl)oxane-3,4,5-triol Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1C1=CC(CC=2C=C3C=CC=CC=C3C=2)=CC=C1O AGJJCLBOHJQGFA-ZQGJOIPISA-N 0.000 claims abstract 2
- 125000000069 2-butynyl group Chemical group [H]C([H])([H])C#CC([H])([H])* 0.000 claims abstract 2
- TTYUNRVFZJWXHB-MRXNPFEDSA-N 8-[(3r)-3-aminopiperidin-1-yl]-7-but-2-ynyl-3-methyl-1-(1,5-naphthyridin-2-ylmethyl)purine-2,6-dione Chemical compound N=1C=2N(C)C(=O)N(CC=3N=C4C=CC=NC4=CC=3)C(=O)C=2N(CC#CC)C=1N1CCC[C@@H](N)C1 TTYUNRVFZJWXHB-MRXNPFEDSA-N 0.000 claims abstract 2
- ILTRPILDWNCOMQ-QGZVFWFLSA-N 8-[(3r)-3-aminopiperidin-1-yl]-7-but-2-ynyl-3-methyl-1-(quinazolin-2-ylmethyl)purine-2,6-dione Chemical compound N=1C=2N(C)C(=O)N(CC=3N=C4C=CC=CC4=CN=3)C(=O)C=2N(CC#CC)C=1N1CCC[C@@H](N)C1 ILTRPILDWNCOMQ-QGZVFWFLSA-N 0.000 claims abstract 2
- QLXKHBNJTPICNF-QMCAAQAGSA-N Sergliflozin etabonate Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](COC(=O)OCC)O[C@H]1OC1=CC=CC=C1CC1=CC=C(OC)C=C1 QLXKHBNJTPICNF-QMCAAQAGSA-N 0.000 claims abstract 2
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims abstract 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims abstract 2
- AHFWIQIYAXSLBA-RQXATKFSSA-N ipragliflozin Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1C1=CC=C(F)C(CC=2SC3=CC=CC=C3C=2)=C1 AHFWIQIYAXSLBA-RQXATKFSSA-N 0.000 claims abstract 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims abstract 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims abstract 2
- 125000006504 o-cyanobenzyl group Chemical group [H]C1=C([H])C(C#N)=C(C([H])=C1[H])C([H])([H])* 0.000 claims abstract 2
- 229940126842 sergliflozin Drugs 0.000 claims abstract 2
- HFLCZNNDZKKXCS-OUUBHVDSSA-N sergliflozin Chemical compound C1=CC(OC)=CC=C1CC1=CC=CC=C1O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 HFLCZNNDZKKXCS-OUUBHVDSSA-N 0.000 claims abstract 2
- 229950000378 sergliflozin etabonate Drugs 0.000 claims abstract 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims abstract 2
- 150000003577 thiophenes Chemical class 0.000 claims abstract 2
- 238000000034 method Methods 0.000 claims 7
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 5
- 239000008280 blood Substances 0.000 claims 5
- 210000004369 blood Anatomy 0.000 claims 5
- 239000008103 glucose Substances 0.000 claims 5
- 208000004611 Abdominal Obesity Diseases 0.000 claims 4
- 208000008589 Obesity Diseases 0.000 claims 3
- 235000020824 obesity Nutrition 0.000 claims 3
- 238000009097 single-agent therapy Methods 0.000 claims 3
- 206010065941 Central obesity Diseases 0.000 claims 2
- 206010033307 Overweight Diseases 0.000 claims 2
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 claims 2
- 239000002552 dosage form Substances 0.000 claims 2
- 230000002641 glycemic effect Effects 0.000 claims 2
- 201000001421 hyperglycemia Diseases 0.000 claims 2
- XZWYZXLIPXDOLR-UHFFFAOYSA-N metformin Chemical compound CN(C)C(=N)NC(N)=N XZWYZXLIPXDOLR-UHFFFAOYSA-N 0.000 claims 2
- 229960003105 metformin Drugs 0.000 claims 2
- ZOTODWFVYUPZFO-GOSISDBHSA-N 2-[[8-[(3r)-3-aminopiperidin-1-yl]-7-but-2-ynyl-3-methyl-2,6-dioxopurin-1-yl]methyl]benzonitrile Chemical compound O=C1C=2N(CC#CC)C(N3C[C@H](N)CCC3)=NC=2N(C)C(=O)N1CC1=CC=CC=C1C#N ZOTODWFVYUPZFO-GOSISDBHSA-N 0.000 claims 1
- ISVBJQYIQQKSGK-MRXNPFEDSA-N 2-[[8-[(3r)-3-aminopiperidin-1-yl]-7-but-2-ynyl-3-methyl-2,6-dioxopurin-1-yl]methyl]pyridine-3-carbonitrile Chemical compound O=C1C=2N(CC#CC)C(N3C[C@H](N)CCC3)=NC=2N(C)C(=O)N1CC1=NC=CC=C1C#N ISVBJQYIQQKSGK-MRXNPFEDSA-N 0.000 claims 1
- HDARIOSGMVVPLE-LJQANCHMSA-N 2-[[8-[(3r)-3-aminopiperidin-1-yl]-7-but-2-ynyl-3-methyl-2,6-dioxopurin-1-yl]methyl]quinoline-3-carbonitrile Chemical compound N=1C=2N(C)C(=O)N(CC=3C(=CC4=CC=CC=C4N=3)C#N)C(=O)C=2N(CC#CC)C=1N1CCC[C@@H](N)C1 HDARIOSGMVVPLE-LJQANCHMSA-N 0.000 claims 1
- BNPBEDWUQOSRHB-UHFFFAOYSA-N 8-[(2-amino-2-methylpropyl)-methylamino]-7-but-2-ynyl-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]purine-2,6-dione Chemical compound C1=CC=CC2=NC(CN3C(=O)N(C)C=4N=C(N(C=4C3=O)CC#CC)N(C)CC(C)(C)N)=NC(C)=C21 BNPBEDWUQOSRHB-UHFFFAOYSA-N 0.000 claims 1
- ONMDRNPIEXAJEZ-MRXNPFEDSA-N 8-[(3r)-3-aminopiperidin-1-yl]-7-but-2-ynyl-1-[(4,6-dimethylpyrimidin-2-yl)methyl]-3-methylpurine-2,6-dione Chemical compound O=C1C=2N(CC#CC)C(N3C[C@H](N)CCC3)=NC=2N(C)C(=O)N1CC1=NC(C)=CC(C)=N1 ONMDRNPIEXAJEZ-MRXNPFEDSA-N 0.000 claims 1
- GFMVACPPQCXLGW-QGZVFWFLSA-N 8-[(3r)-3-aminopiperidin-1-yl]-7-but-2-ynyl-3-methyl-1-(quinoxalin-6-ylmethyl)purine-2,6-dione Chemical compound N=1C=2N(C)C(=O)N(CC=3C=C4N=CC=NC4=CC=3)C(=O)C=2N(CC#CC)C=1N1CCC[C@@H](N)C1 GFMVACPPQCXLGW-QGZVFWFLSA-N 0.000 claims 1
- YLTXBUGZVMPESA-OAHLLOKOSA-N 8-[(3r)-3-aminopiperidin-1-yl]-7-but-2-ynyl-3-methyl-1-[(4-methylpyrimidin-2-yl)methyl]purine-2,6-dione Chemical compound O=C1C=2N(CC#CC)C(N3C[C@H](N)CCC3)=NC=2N(C)C(=O)N1CC1=NC=CC(C)=N1 YLTXBUGZVMPESA-OAHLLOKOSA-N 0.000 claims 1
- OWVQLTBTGFYAHU-HNNXBMFYSA-N 8-[[(2s)-2-aminopropyl]-methylamino]-7-but-2-ynyl-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]purine-2,6-dione Chemical compound C1=CC=CC2=NC(CN3C(=O)N(C)C=4N=C(N(C=4C3=O)CC#CC)N(C)C[C@H](C)N)=NC(C)=C21 OWVQLTBTGFYAHU-HNNXBMFYSA-N 0.000 claims 1
- 208000002705 Glucose Intolerance Diseases 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 235000012000 cholesterol Nutrition 0.000 claims 1
- 230000035487 diastolic blood pressure Effects 0.000 claims 1
- 230000001771 impaired effect Effects 0.000 claims 1
- 235000012054 meals Nutrition 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 201000009104 prediabetes syndrome Diseases 0.000 claims 1
- PBMFSQRYOILNGV-UHFFFAOYSA-N pyridazine Chemical compound C1=CC=NN=C1 PBMFSQRYOILNGV-UHFFFAOYSA-N 0.000 claims 1
- 239000000725 suspension Substances 0.000 claims 1
- 230000035488 systolic blood pressure Effects 0.000 claims 1
- 238000011287 therapeutic dose Methods 0.000 claims 1
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
- GSINGUMRKGRYJP-VZWAGXQNSA-N Remogliflozin Chemical compound C1=CC(OC(C)C)=CC=C1CC1=C(C)N(C(C)C)N=C1O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 GSINGUMRKGRYJP-VZWAGXQNSA-N 0.000 abstract 1
- 229940126844 remogliflozin Drugs 0.000 abstract 1
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Abstract
1. Фармацевтическая композиция, содержащая ингибитор SGLT2, выбранный из группы, включающей ! (1) дапаглифлозин, ! (2) ремоглифлозин или этабонат ремоглифлозина, ! (3) серглифлозин или этабонат серглифлозина, ! (4) 1-хлор-4-(β-D-глюкопираноз-1-ил)-2-(4-этилбензил)бензол, ! (5) (1S)-1,5-ангидро-1-[5-(азулен-2-илметил)-2-гидроксифенил]-D-сорбит, ! (6) (1S)-1,5-ангидро-1-[3-(1-бензотиен-2-илметил)-4-фторфенил]-D-сорбит, ! (7) производное тиофена формулы (7-1) ! ! где R обозначает метоксигруппу или трифторметоксигруппу, ! (8) 1-(β-D-глюкопиранозил)-4-метил-3-[5-(4-фторфенил)-2-тиенилметил]бензол, ! (9) производное спирокеталя формулы (9-1) ! ! где R обозначает метоксигруппу, трифторметоксигруппу, этоксигруппу, этил, изопропил или трет-бутил, ! или их фармацевтически приемлемые соль, гидрат или сольват, ! в комбинации с ингибитором ДПП-IV формулы (I) ! ! или формулы (II) ! ! или формулы (III) ! ! или формулы (IV) ! ! где R1 обозначает ([1,5]нафтиридин-2-ил)метил, (хиназолин-2-ил)метил, (хиноксалин-6-ил)метил, (4-метилхиналозин-2-ил)метил, 2-цианобензил, (3-цианохинолин-2-ил)метил, (3-цианопиридин-2-ил)метил, (4-метилпиримидин-2-ил)метил или (4,6-диметилпиримидин-2-ил)метил, a R2 обозначает 3-(R)-аминопиперидин-1-ил, (2-амино-2-метилпропил)метиламино или (2-(S)-аминопропил)метиламиногруппу или их фармацевтически приемлемую соль. ! 2. Фармацевтическая композиция по п.1, где ингибитор ДПП-IV выбран из группы, включающей ! 1-[(4-метилхиназолин-2-ил)метил]-3-метил-7-(2-бутин-1-ил)-8-(3-(R)-аминопиперидин-1-ил)ксантин, ! 1-[([1,5]нафтиридин-2-ил)метил]-3-метил-7-(2-бутин-1-ил)-8-((R)-3-аминопиперидин-1-ил)ксантин, ! 1-[(хиназолин-2-ил)метил]-3-метил-7-(2-бутин-1-ил)-8-((R)-3-аминопиперидин-1-ил)ксантин, ! 2-((R)-3-аминопиперидин-1-ил)-3-(бут-2-инил)-5(4-метилхина
Claims (15)
1. Фармацевтическая композиция, содержащая ингибитор SGLT2, выбранный из группы, включающей
(1) дапаглифлозин,
(2) ремоглифлозин или этабонат ремоглифлозина,
(3) серглифлозин или этабонат серглифлозина,
(4) 1-хлор-4-(β-D-глюкопираноз-1-ил)-2-(4-этилбензил)бензол,
(5) (1S)-1,5-ангидро-1-[5-(азулен-2-илметил)-2-гидроксифенил]-D-сорбит,
(6) (1S)-1,5-ангидро-1-[3-(1-бензотиен-2-илметил)-4-фторфенил]-D-сорбит,
(7) производное тиофена формулы (7-1)
где R обозначает метоксигруппу или трифторметоксигруппу,
(8) 1-(β-D-глюкопиранозил)-4-метил-3-[5-(4-фторфенил)-2-тиенилметил]бензол,
(9) производное спирокеталя формулы (9-1)
где R обозначает метоксигруппу, трифторметоксигруппу, этоксигруппу, этил, изопропил или трет-бутил,
или их фармацевтически приемлемые соль, гидрат или сольват,
в комбинации с ингибитором ДПП-IV формулы (I)
или формулы (II)
или формулы (III)
или формулы (IV)
где R1 обозначает ([1,5]нафтиридин-2-ил)метил, (хиназолин-2-ил)метил, (хиноксалин-6-ил)метил, (4-метилхиналозин-2-ил)метил, 2-цианобензил, (3-цианохинолин-2-ил)метил, (3-цианопиридин-2-ил)метил, (4-метилпиримидин-2-ил)метил или (4,6-диметилпиримидин-2-ил)метил, a R2 обозначает 3-(R)-аминопиперидин-1-ил, (2-амино-2-метилпропил)метиламино или (2-(S)-аминопропил)метиламиногруппу или их фармацевтически приемлемую соль.
2. Фармацевтическая композиция по п.1, где ингибитор ДПП-IV выбран из группы, включающей
1-[(4-метилхиназолин-2-ил)метил]-3-метил-7-(2-бутин-1-ил)-8-(3-(R)-аминопиперидин-1-ил)ксантин,
1-[([1,5]нафтиридин-2-ил)метил]-3-метил-7-(2-бутин-1-ил)-8-((R)-3-аминопиперидин-1-ил)ксантин,
1-[(хиназолин-2-ил)метил]-3-метил-7-(2-бутин-1-ил)-8-((R)-3-аминопиперидин-1-ил)ксантин,
2-((R)-3-аминопиперидин-1-ил)-3-(бут-2-инил)-5(4-метилхиназолин-2-лиметил)-3,5-дигидроимидазо[4,5-d]пиридазин-4-он,
1-[(4-метилхиназолин-2-ил)метил]-3-метил-7-(2-бутин-1-ил)-8-[(2-амино-2-метилпропил)метиламино]ксантин,
1-[(3-цианохинолин-2-ил)метил]-3-метил-7-(2-бутин-1-ил)-8-((R)-3-аминопиперидин-1-ил)ксантин,
1-(2-цианобензил)-3-метил-7-(2-бутин-1-ил)-8-((R)-3-аминопиперидин-1-ил)ксантин,
1-[(4-метилхиназолин-2-ил)метил]-3-метил-7-(2-бутин-1-ил)-8-[(S)-(2-аминопропил)метиламино]ксантин,
1-[(3-цианопиридин-2-ил)метил]-3-метил-7-(2-бутин-1-ил)-8-((R)-3-аминопиперидин-1-ил)ксантин,
1-[(4-метилпиримидин-2-ил)метил]-3-метил-7-(2-бутин-1-ил)-8-((R)-3-аминопиперидин-1-ил)ксантин,
1-[(4,6-диметилпиримидин-2-ил)метил]-3-метил-7-(2-бутин-1-ил)-8-((R)-3-аминопиперидин-1-ил)ксантин,
1-[(хиноксалин-6-ил)метил]-3-метил-7-(2-бутин-1-ил)-8-((R)-3-аминопиперидин-1-ил)ксантин
или их фармацевтически приемлемые соли.
3. Фармацевтическая композиция по п.1 или 2, отличающаяся тем, что ингибитор ДПП-IV представляет собой 1-[(4-метилхиназолин-2-ил)метил]-3-метил-7-(2-бутин-1-ил)-8-(3-(R)-аминопиперидин-1-ил)ксантин или его фармацевтически приемлемую соль.
4. Фармацевтическая композиция по п.1 или 2, отличающаяся тем, что ингибитор SGLT2 представляет собой дапаглифлозин или его фармацевтически приемлемую соль, гидрат или сольват.
5. Фармацевтическая композиция по п.1 или 2, отличающаяся тем, что ингибитор SGLT2 представляет собой 1-(β-D-глюкопиранозил)-4-метил-3-[5-(4-фторфенил)-2-тиенилметил]бензол или его фармацевтически приемлемую соль, гидрат или сольват.
6. Фармацевтическая композиция по п.1 или 2, отличающаяся тем, что композиция является подходящей для совместного или одновременного, или последовательного использования ингибитора SGLT2 и ингибитора ДПП-IV.
7. Фармацевтическая композиция по п.1 или 2, отличающаяся тем, что ингибитор SGLT2 и ингибитор ДПП-IV содержатся в одной лекарственной форме.
8. Фармацевтическая композиция по п.1 или 2, отличающаяся тем, что ингибитор SGLT2 и ингибитор ДПП-IV каждый содержатся в отдельной лекарственной форме.
9. Способ профилактики, замедления прогрессирования, приостановки или лечения метаболического нарушения, выбранного из группы, включающей сахарный диабет типа 1, сахарный диабет типа 2, нарушенную толерантность к глюкозе, нарушенный уровень глюкозы в крови натощак, гипергликемию, гипергликемию после приема пищи, избыточную массу тела, ожирение и метаболический синдром у нуждающегося в таком лечении пациента, заключающийся в том, что ингибитор SGLT2 по пп.1, 4 или 5 вводят в комбинации или поочередно с ингибитором ДПП-IV по пп.1, 2 или 3.
10. Способ по п.9, где у пациента установлен диагноз одного или более состояний, выбранных из группы, включающей избыточную массу тела, ожирение, висцеральное ожирение и центральное ожирение.
11. Способ по п.9, где у пациента наблюдается одно, два или более следующих состояний:
(а) концентрация глюкозы в крови или глюкозы в плазме натощак более 110 мг/дл, прежде всего более 125 мг/дл,
(б) уровень глюкозы в плазме после приема пищи равен 140 мг/дл или более,
(в) уровень HbA1c равен 6,5% или более, прежде равен 8,0% или более.
12. Способ по п.9, где у пациента наблюдается одно, два или более следующих состояний:
(а) ожирение, висцеральное ожирение и/или центральное ожирение,
(б) уровень триглицеридов в крови ≥150 мг/дл,
(в) уровень холестерина-ЛПВП в крови <40 мг/дл у женщин и <50 мг/дл у мужчин,
(г) систолическое кровяное давление ≥130 мм рт.ст. и диастолическое кровяное давление ≥85 мм рт.ст.,
(д) уровень глюкозы в крови натощак ≥110 мг/дл.
13. Способ по п.9, где пациенту противопоказано лечение в режиме монотерапии метформином и/или у него наблюдается непереносимость метформина в терапевтических дозах.
14. Способ по п.9, где у пациента наблюдается недостаточное гликемическое регулирование, несмотря на лечение в режиме монотерапии ингибитором SGLT2, таким как ингибитор SGLT2 по пп.1, 4 или 5.
15. Способ по п.9, где у пациента наблюдается недостаточное гликемическое регулирование, несмотря на лечение в режиме монотерапии ингибитором ДПП-IV, таким как ингибитор ДПП-IV по пп.1, 2 или 3.
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Families Citing this family (84)
| 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 |
| US7501426B2 (en) | 2004-02-18 | 2009-03-10 | Boehringer Ingelheim International Gmbh | 8-[3-amino-piperidin-1-yl]-xanthines, their preparation 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 |
| US7772191B2 (en) | 2005-05-10 | 2010-08-10 | Boehringer Ingelheim International Gmbh | Processes for preparing of glucopyranosyl-substituted benzyl-benzene derivatives and intermediates therein |
| DE102005035891A1 (de) | 2005-07-30 | 2007-02-08 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | 8-(3-Amino-piperidin-1-yl)-xanthine, deren Herstellung und deren Verwendung als Arzneimittel |
| TW200745075A (en) * | 2005-09-08 | 2007-12-16 | Boehringer Ingelheim Int | Crystalline forms of 1-chloro-4-(β-D-glucopyranos-1-yl)-2-(4-ethynyl-benzyl)-benzene, methods for its preparation and the use thereof for preparing medicaments |
| PE20080697A1 (es) | 2006-05-03 | 2008-08-05 | Boehringer Ingelheim Int | Derivados de benzonitrilo sustituidos con glucopiranosilo, composiciones farmaceuticas que contienen compuestos de este tipo, su uso y procedimiento para su fabricacion |
| PE20080251A1 (es) | 2006-05-04 | 2008-04-25 | Boehringer Ingelheim Int | Usos de inhibidores de dpp iv |
| KR101452915B1 (ko) | 2006-05-04 | 2014-10-21 | 베링거 인겔하임 인터내셔날 게엠베하 | 다형태 |
| EP1852108A1 (en) | 2006-05-04 | 2007-11-07 | Boehringer Ingelheim Pharma GmbH & Co.KG | DPP IV inhibitor formulations |
| US8039441B2 (en) * | 2006-08-15 | 2011-10-18 | Boehringer Ingelheim International Gmbh | Glucopyranosyl-substituted cyclopropylbenzene derivatives, pharmaceutical compositions containing such compounds, their use as SGLT inhibitors and process for their manufacture |
| EP2086991A1 (en) * | 2006-10-27 | 2009-08-12 | Boehringer Ingelheim International GmbH | CRYSTALLINE FORM OF 4-(ß-D-GLUCOPYRANOS-1-YL)-1-METHYL-2-[4-((S)-TETRAHYDROFURAN-3-YLOXY)-BENZYL]-BENZENE, A METHOD FOR ITS PREPARATION AND THE USE THEREOF FOR PREPARING MEDICAMENTS |
| CL2008002427A1 (es) | 2007-08-16 | 2009-09-11 | Boehringer Ingelheim Int | Composicion farmaceutica que comprende 1-cloro-4-(b-d-glucopiranos-1-il)-2-[4-((s)-tetrahidrofurano-3-iloxi)bencil]-benceno combinado con 1-[(4-metilquinazolin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-(3-(r)-aminopiperidin-1-il)xantina; y su uso para tratar diabetes mellitus tipo 2. |
| CN101801371B (zh) | 2007-09-10 | 2012-11-28 | 詹森药业有限公司 | 可用作sglt抑制剂的化合物的制备方法 |
| CA2706018C (en) | 2007-11-30 | 2015-11-24 | Boehringer Ingelheim International Gmbh | 1, 5-dihydro-pyrazolo [3,4-d]pyrimidin-4-one derivatives and their use as pde9a modulators for the treatment of cns disorders |
| CL2008003653A1 (es) | 2008-01-17 | 2010-03-05 | Mitsubishi Tanabe Pharma Corp | Uso de un inhibidor de sglt derivado de glucopiranosilo y un inhibidor de dppiv seleccionado para tratar la diabetes; y composicion farmaceutica. |
| UA105362C2 (en) | 2008-04-02 | 2014-05-12 | Бьорингер Ингельхайм Интернациональ Гмбх | 1-heterocyclyl-1, 5-dihydro-pyrazolo [3, 4-d] pyrimidin-4-one derivatives and their use as pde9a modulators |
| PE20140960A1 (es) | 2008-04-03 | 2014-08-15 | Boehringer Ingelheim Int | Formulaciones que comprenden un inhibidor de dpp4 |
| UY32030A (es) | 2008-08-06 | 2010-03-26 | Boehringer Ingelheim Int | "tratamiento para diabetes en pacientes inapropiados para terapia con metformina" |
| KR20190016601A (ko) | 2008-08-06 | 2019-02-18 | 베링거 인겔하임 인터내셔날 게엠베하 | 메트포르민 요법이 부적합한 환자에서의 당뇨병 치료 |
| WO2010018217A2 (en) * | 2008-08-15 | 2010-02-18 | Boehringer Ingelheim International Gmbh | Organic compounds for wound healing |
| EP2334687B9 (en) | 2008-08-28 | 2012-08-08 | Pfizer Inc. | Dioxa-bicyclo[3.2.1.]octane-2,3,4-triol derivatives |
| NZ590788A (en) | 2008-09-08 | 2012-11-30 | Boehringer Ingelheim Int | Pyrazolopyrimidines and their use for the treatment of cns disorders |
| MX2011002558A (es) | 2008-09-10 | 2011-04-26 | Boehringer Ingelheim Int | Terapia de combinacion para el tratamiento de diabetes y estados relacionados. |
| 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 |
| US20240148737A1 (en) * | 2008-10-16 | 2024-05-09 | Boehringer Ingelheim International Gmbh | Treatment for diabetes in patients with insufficient glycemic control despite therapy with an oral antidiabetic drug |
| US9056850B2 (en) | 2008-10-17 | 2015-06-16 | Janssen Pharmaceutica N.V. | Process for the preparation of compounds useful as inhibitors of SGLT |
| AU2009331471B2 (en) | 2008-12-23 | 2015-09-03 | Boehringer Ingelheim International Gmbh | Salt forms of organic compound |
| AR074990A1 (es) | 2009-01-07 | 2011-03-02 | Boehringer Ingelheim Int | Tratamiento de diabetes en pacientes con un control glucemico inadecuado a pesar de la terapia con metformina |
| PT2395983T (pt) | 2009-02-13 | 2020-07-03 | Boehringer Ingelheim Int | Composição farmacêutica compreendendo um inibidor de sglt2, um inibidor de dp-iv e opcionalmente um agente antidiabético adicional e suas utilizações |
| UY32427A (es) * | 2009-02-13 | 2010-09-30 | Boheringer Ingelheim Internat Gmbh | Composicion farmaceutica, forma farmaceutica, procedimiento para su preparacion, metodos de tratamiento y usos de la misma |
| CN102316875A (zh) | 2009-02-13 | 2012-01-11 | 贝林格尔.英格海姆国际有限公司 | 用于治疗i型糖尿病、ii型糖尿病、葡萄糖耐量降低或高血糖症的sglt-2抑制剂 |
| DK2395968T3 (da) * | 2009-02-13 | 2024-03-04 | Boehringer Ingelheim Int | Farmaceutisk sammensætning omfattende glucopyranosyldiphenylmethanderivater, farmaceutisk doseringsform deraf, fremgangsmåde til deres forberedelse og anvendelser deraf til forbedret glykæmisk kontrol hos en patient |
| CA2757231A1 (en) | 2009-03-31 | 2010-10-07 | Boehringer Ingelheim International Gmbh | 1-heterocyclyl-1,5-dihydro-pyrazolo [3,4-d] pyrimidin-4-one derivatives and their use as pde9a modulators |
| SG175154A1 (en) | 2009-04-16 | 2011-11-28 | Taisho Pharmaceutical Co Ltd | Pharmaceutical compositions |
| US20110009347A1 (en) | 2009-07-08 | 2011-01-13 | Yin Liang | Combination therapy for the treatment of diabetes |
| DK2451797T3 (da) | 2009-07-10 | 2013-06-24 | Janssen Pharmaceutica Nv | Fremgangsmåde til krystallisation for 1-(b-D-GLUCOPYRANOSYL)-4-METHYL-3-[5-(4-fluorphenyl)-2- thienylmethyl]benzen |
| ES2546762T3 (es) | 2009-09-30 | 2015-09-28 | Boehringer Ingelheim International Gmbh | Procedimientos para preparar derivados de bencil-benceno sustituidos con glucopiranosilo |
| EA020798B1 (ru) * | 2009-09-30 | 2015-01-30 | Бёрингер Ингельхайм Интернациональ Гмбх | СПОСОБ ПОЛУЧЕНИЯ КРИСТАЛЛИЧЕСКОЙ ФОРМЫ 1-ХЛОР-4-(β-D-ГЛЮКОПИРАНОЗ-1-ИЛ)-2-[4-((S)-ТЕТРАГИДРОФУРАН-3-ИЛОКСИ)БЕНЗИЛ]БЕНЗОЛА |
| UY32919A (es) | 2009-10-02 | 2011-04-29 | Boehringer Ingelheim Int | Composición farmacéutica, forma de dosificación farmacéutica, procedimiento para su preparación, mé todos para su tratamiento y sus usos |
| RU2012121183A (ru) * | 2009-10-23 | 2013-11-27 | Астеллас Фарма Инк. | Фармацевтическая композиция для перорального введения |
| KR101426180B1 (ko) | 2009-11-02 | 2014-07-31 | 화이자 인코포레이티드 | 디옥사-비시클로[3.2.1]옥탄-2,3,4-트리올 유도체 |
| KR20120107080A (ko) | 2009-11-27 | 2012-09-28 | 베링거 인겔하임 인터내셔날 게엠베하 | 리나글립틴과 같은 dpp-iv 억제제를 사용한 유전자형 검사된 당뇨병 환자의 치료 |
| WO2011080276A1 (en) | 2009-12-29 | 2011-07-07 | Genfit | Pharmaceutical combinations comprising a dpp-4 inhibitor and a 1,3-diphenylprop-2-en-1-one derivative |
| TWI562775B (en) * | 2010-03-02 | 2016-12-21 | Lexicon Pharmaceuticals Inc | Methods of using inhibitors of sodium-glucose cotransporters 1 and 2 |
| EP2368552A1 (en) | 2010-03-25 | 2011-09-28 | Boehringer Ingelheim Vetmedica GmbH | 1-[(3-cyano-pyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-[3-(r)-amino-piperidin-1-yl]-xanthine for the treatment of a metabolic disorder of a predominantly carnivorous non-human animal |
| KR101927068B1 (ko) | 2010-05-05 | 2018-12-10 | 베링거 인겔하임 인터내셔날 게엠베하 | 체중 감소 치료에 후속하는 dpp-4 억제제에 의한 순차적 병용 요법 |
| NZ703128A (en) * | 2010-05-11 | 2016-04-29 | Janssen Pharmaceutica Nv | Pharmaceutical formulations comprising 1 - (beta-d-glucopyranosyl) - 2 -thienylmethylbenzene derivatives as inhibitors of sglt |
| KR101869110B1 (ko) * | 2010-05-11 | 2018-06-19 | 미쓰비시 타나베 파마 코퍼레이션 | 카나글리플로진 함유 정제 |
| KR20220025926A (ko) | 2010-06-24 | 2022-03-03 | 베링거 인겔하임 인터내셔날 게엠베하 | 당뇨병 요법 |
| GEP20156217B (en) | 2010-08-12 | 2015-01-12 | Boehringer Ingelheim Int | 6-cycloalkyl-1, 5-dihydro-pyrazolo [3, 4-d] pyrimidin-4-one derivatives and their use as pde9a inhibitors |
| AR083878A1 (es) | 2010-11-15 | 2013-03-27 | Boehringer Ingelheim Int | Terapia antidiabetica vasoprotectora y cardioprotectora, linagliptina, metodo de tratamiento |
| US8809345B2 (en) | 2011-02-15 | 2014-08-19 | Boehringer Ingelheim International Gmbh | 6-cycloalkyl-pyrazolopyrimidinones for the treatment of CNS disorders |
| UY33937A (es) | 2011-03-07 | 2012-09-28 | Boehringer Ingelheim Int | Composiciones farmacéuticas que contienen inhibidores de dpp-4 y/o sglt-2 y metformina |
| KR101841087B1 (ko) | 2011-04-22 | 2018-03-23 | 아스텔라스세이야쿠 가부시키가이샤 | 고형 의약 조성물 |
| CN103781788B (zh) | 2011-07-15 | 2016-08-17 | 勃林格殷格翰国际有限公司 | 经取代的喹唑啉、其制备及其在药物组合物中的用途 |
| BR112014010574A2 (pt) * | 2011-10-31 | 2017-05-02 | Scinopharm Taiwan Ltd | formas cristalinas e não cristalinas de inibidores sglt2 |
| US9555001B2 (en) | 2012-03-07 | 2017-01-31 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition and uses thereof |
| US9192617B2 (en) | 2012-03-20 | 2015-11-24 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
| WO2013171166A1 (en) | 2012-05-14 | 2013-11-21 | Boehringer Ingelheim International Gmbh | A xanthine derivative as dpp-4 inhibitor for use in the treatment of sirs and/or sepsis |
| JP6224084B2 (ja) | 2012-05-14 | 2017-11-01 | 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 | 糸球体上皮細胞関連障害及び/又はネフローゼ症候群の治療に用いるdpp−4阻害薬としてのキサンチン誘導体 |
| EP2854812A1 (en) * | 2012-05-24 | 2015-04-08 | Boehringer Ingelheim International GmbH | A xanthine derivative as dpp -4 inhibitor for use in the treatment of autoimmune diabetes, particularly lada |
| WO2013174767A1 (en) | 2012-05-24 | 2013-11-28 | Boehringer Ingelheim International Gmbh | A xanthine derivative as dpp -4 inhibitor for use in modifying food intake and regulating food preference |
| WO2014008374A2 (en) * | 2012-07-06 | 2014-01-09 | Thetis Pharmaceuticals Llc | Combination therapies comprising metformin salts and antihyperglycemia agents or antihyperlipidemia agents |
| ES2702174T3 (es) | 2013-04-05 | 2019-02-27 | Boehringer Ingelheim Int | Usos terapéuticos de empagliflozina |
| US11813275B2 (en) | 2013-04-05 | 2023-11-14 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
| CA2812519A1 (en) | 2013-04-05 | 2014-10-05 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
| HK1213818A1 (zh) | 2013-04-05 | 2016-07-15 | 勃林格殷格翰国际有限公司 | 依帕列净的治疗用途 |
| DK2986304T3 (da) | 2013-04-18 | 2022-04-04 | Boehringer Ingelheim Int | Farmaceutisk sammensætning, fremgangsmåder til behandling og anvendelser deraf. |
| CN111494357A (zh) * | 2013-12-17 | 2020-08-07 | 勃林格殷格翰动物保健有限公司 | 猫科动物中代谢紊乱的治疗 |
| JP6615109B2 (ja) | 2014-02-28 | 2019-12-04 | 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 | Dpp−4阻害薬の医学的使用 |
| CN104765500B (zh) * | 2015-04-20 | 2018-07-17 | 合肥京东方光电科技有限公司 | 彩膜基板及其制作方法、显示装置 |
| US20170071970A1 (en) | 2015-09-15 | 2017-03-16 | Janssen Pharmaceutica Nv | Co-therapy comprising canagliflozin and phentermine for the treatment of obesity and obesity related disorders |
| MX390363B (es) | 2016-06-10 | 2025-03-20 | Boehringer Ingelheim Int | Combinacion de linagliptina y metformina |
| CN109922813A (zh) | 2016-11-10 | 2019-06-21 | 勃林格殷格翰国际有限公司 | 药物组合物、治疗方法及其用途 |
| WO2018167589A1 (en) | 2017-03-16 | 2018-09-20 | Inventia Healthcare Private Limited | Pharmaceutical composition comprising dapagliflozin |
| CN109549939A (zh) * | 2017-09-26 | 2019-04-02 | 江苏恒瑞医药股份有限公司 | Sglt2抑制剂和dpp-4抑制剂联合在制备治疗糖尿病的药物中的用途 |
| KR102204439B1 (ko) * | 2018-05-14 | 2021-01-18 | 에이치케이이노엔 주식회사 | Sglt-2 억제제 및 dpp-iv 억제제를 포함하는 약제학적 조성물 |
| CA3142325A1 (en) * | 2019-05-31 | 2020-12-03 | Avolynt | Compositions and methods for treating metabolic disease |
| EP4037691A4 (en) * | 2019-10-04 | 2023-11-22 | United States Government as Represented by The Department of Veterans Affairs | IMAGING DEVELOPMENT AND THERAPEUTIC GLUCOSE ANALOGS OF SODIUM-DEPENDENT GLUCOSE TRANSPORTERS |
| KR20220143732A (ko) | 2020-02-17 | 2022-10-25 | 베링거잉겔하임베트메디카게엠베하 | 고양이과에서 심장 질환을 예방 및/또는 치료하기 위한 sglt-2 억제제의 사용 |
| AU2022319909A1 (en) | 2021-07-28 | 2024-02-22 | Boehringer Ingelheim Vetmedica Gmbh | Use of sglt-2 inhibitors for the prevention and/or treatment of cardiac diseases in non-human mammals excluding felines, in particular canines |
| MA71282A1 (fr) * | 2022-10-05 | 2025-12-31 | Daewoong Pharmaceutical Co., Ltd. | Composition pharmaceutique pour la prévention ou le traitement d'une néphropathie et/ou du diabète sucré, comprenant de l'énavogliflozine |
| WO2024240632A1 (en) | 2023-05-24 | 2024-11-28 | Boehringer Ingelheim Vetmedica Gmbh | Combination treatment and/or prevention of cardiac diseases in non-human mammals comprising one or more sglt-2 inhibitors and pimobendan and/or telmisartan |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6515117B2 (en) * | 1999-10-12 | 2003-02-04 | Bristol-Myers Squibb Company | C-aryl glucoside SGLT2 inhibitors and method |
| WO2002051836A1 (en) * | 2000-12-27 | 2002-07-04 | Kyowa Hakko Kogyo Co., Ltd. | Dipeptidyl peptidase iv inhibitor |
| 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 |
| US7109192B2 (en) * | 2002-12-03 | 2006-09-19 | Boehringer Ingelheim Pharma Gmbh & Co Kg | Substituted imidazo-pyridinones and imidazo-pyridazinones, the preparation thereof and their use as pharmaceutical compositions |
| WO2004080990A1 (ja) * | 2003-03-14 | 2004-09-23 | Astellas Pharma Inc. | C-グリコシド誘導体又はその塩 |
| DE10355304A1 (de) * | 2003-11-27 | 2005-06-23 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue 8-(Piperazin-1-yl)-und 8-([1,4]Diazepan-1-yl)-xanthine, deren Herstellung und deren Verwendung als Arzneimittel |
| DE102004044221A1 (de) * | 2004-09-14 | 2006-03-16 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue 3-Methyl-7-butinyl-xanthine, deren Herstellung und deren Verwendung als Arzneimittel |
| PE20080251A1 (es) * | 2006-05-04 | 2008-04-25 | Boehringer Ingelheim Int | Usos de inhibidores de dpp iv |
| CL2008002427A1 (es) * | 2007-08-16 | 2009-09-11 | Boehringer Ingelheim Int | Composicion farmaceutica que comprende 1-cloro-4-(b-d-glucopiranos-1-il)-2-[4-((s)-tetrahidrofurano-3-iloxi)bencil]-benceno combinado con 1-[(4-metilquinazolin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-(3-(r)-aminopiperidin-1-il)xantina; y su uso para tratar diabetes mellitus tipo 2. |
| PT2395983T (pt) * | 2009-02-13 | 2020-07-03 | Boehringer Ingelheim Int | Composição farmacêutica compreendendo um inibidor de sglt2, um inibidor de dp-iv e opcionalmente um agente antidiabético adicional e suas utilizações |
| EP2368552A1 (en) * | 2010-03-25 | 2011-09-28 | Boehringer Ingelheim Vetmedica GmbH | 1-[(3-cyano-pyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-[3-(r)-amino-piperidin-1-yl]-xanthine for the treatment of a metabolic disorder of a predominantly carnivorous non-human animal |
-
2008
- 2008-08-14 PE PE2008001381A patent/PE20090603A1/es not_active Application Discontinuation
- 2008-08-14 CL CL2008002425A patent/CL2008002425A1/es unknown
- 2008-08-15 AU AU2008288410A patent/AU2008288410A1/en not_active Abandoned
- 2008-08-15 EP EP08787272A patent/EP2187966A1/en not_active Withdrawn
- 2008-08-15 TW TW097131319A patent/TW200914031A/zh unknown
- 2008-08-15 KR KR1020107003406A patent/KR20100055422A/ko not_active Ceased
- 2008-08-15 CA CA2696271A patent/CA2696271A1/en not_active Abandoned
- 2008-08-15 NZ NZ583240A patent/NZ583240A/xx not_active IP Right Cessation
- 2008-08-15 MX MX2010001560A patent/MX2010001560A/es not_active Application Discontinuation
- 2008-08-15 AR ARP080103591A patent/AR067969A1/es unknown
- 2008-08-15 RU RU2010109449/15A patent/RU2010109449A/ru unknown
- 2008-08-15 WO PCT/EP2008/060744 patent/WO2009022010A1/en not_active Ceased
- 2008-08-15 US US12/673,319 patent/US20110098240A1/en not_active Abandoned
- 2008-08-15 CN CN200880102900A patent/CN101784286A/zh active Pending
- 2008-08-15 UY UY31295A patent/UY31295A1/es not_active Application Discontinuation
- 2008-08-15 BR BRPI0815170 patent/BRPI0815170A2/pt not_active IP Right Cessation
- 2008-08-15 JP JP2010520595A patent/JP2010536734A/ja active Pending
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- 2009-12-17 ZA ZA200908992A patent/ZA200908992B/xx unknown
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2012
- 2012-12-04 US US13/693,239 patent/US20130096076A1/en not_active Abandoned
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|---|---|
| WO2009022010A1 (en) | 2009-02-19 |
| US20130096076A1 (en) | 2013-04-18 |
| IL202748A0 (en) | 2010-06-30 |
| JP2010536734A (ja) | 2010-12-02 |
| CL2008002425A1 (es) | 2009-09-11 |
| EP2187966A1 (en) | 2010-05-26 |
| UY31295A1 (es) | 2009-03-31 |
| MX2010001560A (es) | 2010-03-11 |
| AU2008288410A1 (en) | 2009-02-19 |
| CA2696271A1 (en) | 2009-02-19 |
| US20110098240A1 (en) | 2011-04-28 |
| ZA200908992B (en) | 2010-08-25 |
| KR20100055422A (ko) | 2010-05-26 |
| TW200914031A (en) | 2009-04-01 |
| CN101784286A (zh) | 2010-07-21 |
| PE20090603A1 (es) | 2009-06-11 |
| BRPI0815170A2 (pt) | 2015-03-31 |
| AR067969A1 (es) | 2009-10-28 |
| NZ583240A (en) | 2012-10-26 |
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