JP2010529991A5 - - Google Patents
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- Publication number
- JP2010529991A5 JP2010529991A5 JP2010512311A JP2010512311A JP2010529991A5 JP 2010529991 A5 JP2010529991 A5 JP 2010529991A5 JP 2010512311 A JP2010512311 A JP 2010512311A JP 2010512311 A JP2010512311 A JP 2010512311A JP 2010529991 A5 JP2010529991 A5 JP 2010529991A5
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- substituted
- ylmethyl
- alkyl
- nhco
- 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.)
- Granted
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- -1 substituted Chemical class 0.000 claims 158
- 125000000217 alkyl group Chemical group 0.000 claims 45
- 125000000623 heterocyclic group Chemical group 0.000 claims 37
- 229910052760 oxygen Inorganic materials 0.000 claims 29
- 229910052731 fluorine Inorganic materials 0.000 claims 26
- 125000005842 heteroatom Chemical group 0.000 claims 26
- 229910052799 carbon Inorganic materials 0.000 claims 24
- 229910052717 sulfur Inorganic materials 0.000 claims 22
- 229910052739 hydrogen Inorganic materials 0.000 claims 20
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 20
- 125000004432 carbon atom Chemical group C* 0.000 claims 14
- 150000001875 compounds Chemical class 0.000 claims 13
- 150000001721 carbon Chemical group 0.000 claims 12
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 10
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 claims 9
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 7
- 208000035475 disorder Diseases 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 7
- 230000009424 thromboembolic effect Effects 0.000 claims 7
- 125000003626 1,2,4-triazol-1-yl group Chemical group [*]N1N=C([H])N=C1[H] 0.000 claims 6
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 6
- 125000003342 alkenyl group Chemical group 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 6
- 125000001072 heteroaryl group Chemical group 0.000 claims 6
- 125000004076 pyridyl group Chemical group 0.000 claims 6
- 125000004523 tetrazol-1-yl group Chemical group N1(N=NN=C1)* 0.000 claims 6
- 125000004299 tetrazol-5-yl group Chemical group [H]N1N=NC(*)=N1 0.000 claims 6
- GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical group NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 claims 5
- 125000004429 atom Chemical group 0.000 claims 5
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 5
- 125000001544 thienyl group Chemical group 0.000 claims 5
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 4
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 125000004438 haloalkoxy group Chemical group 0.000 claims 4
- 125000002962 imidazol-1-yl group Chemical group [*]N1C([H])=NC([H])=C1[H] 0.000 claims 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 3
- 125000004847 2-fluorobenzyl group Chemical group [H]C1=C([H])C(F)=C(C([H])=C1[H])C([H])([H])* 0.000 claims 3
- 125000006288 3,5-difluorobenzyl group Chemical group [H]C1=C(F)C([H])=C(C([H])=C1F)C([H])([H])* 0.000 claims 3
- 125000006284 3-fluorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C(F)=C1[H])C([H])([H])* 0.000 claims 3
- 125000004176 4-fluorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1F)C([H])([H])* 0.000 claims 3
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 3
- 125000002837 carbocyclic group Chemical group 0.000 claims 3
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 125000000814 indol-3-yl group Chemical group [H]C1=C([H])C([H])=C2N([H])C([H])=C([*])C2=C1[H] 0.000 claims 3
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 3
- 125000000335 thiazolyl group Chemical group 0.000 claims 3
- 125000001607 1,2,3-triazol-1-yl group Chemical group [*]N1N=NC([H])=C1[H] 0.000 claims 2
- 125000003287 1H-imidazol-4-ylmethyl group Chemical group [H]N1C([H])=NC(C([H])([H])[*])=C1[H] 0.000 claims 2
- 125000000094 2-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 claims 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 2
- 208000007536 Thrombosis Diseases 0.000 claims 2
- 206010047249 Venous thrombosis Diseases 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 2
- 125000004603 benzisoxazolyl group Chemical group O1N=C(C2=C1C=CC=C2)* 0.000 claims 2
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 2
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims 2
- 230000002526 effect on cardiovascular system Effects 0.000 claims 2
- 125000002541 furyl group Chemical group 0.000 claims 2
- 125000001188 haloalkyl group Chemical group 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 2
- 125000001041 indolyl group Chemical group 0.000 claims 2
- 125000004458 methylaminocarbonyl group Chemical group [H]N(C(*)=O)C([H])([H])[H] 0.000 claims 2
- 125000001971 neopentyl group Chemical group [H]C([*])([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 125000002971 oxazolyl group Chemical group 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 1
- YBYIRNPNPLQARY-UHFFFAOYSA-N 1H-indene Natural products C1=CC=C2CC=CC2=C1 YBYIRNPNPLQARY-UHFFFAOYSA-N 0.000 claims 1
- 208000004476 Acute Coronary Syndrome Diseases 0.000 claims 1
- 206010002388 Angina unstable Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 206010003658 Atrial Fibrillation Diseases 0.000 claims 1
- 206010008088 Cerebral artery embolism Diseases 0.000 claims 1
- 206010008092 Cerebral artery thrombosis Diseases 0.000 claims 1
- 206010011091 Coronary artery thrombosis Diseases 0.000 claims 1
- 206010051055 Deep vein thrombosis Diseases 0.000 claims 1
- 206010014513 Embolism arterial Diseases 0.000 claims 1
- 208000032382 Ischaemic stroke Diseases 0.000 claims 1
- 208000030831 Peripheral arterial occlusive disease Diseases 0.000 claims 1
- 206010063544 Renal embolism Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 208000007814 Unstable Angina Diseases 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 208000002528 coronary thrombosis Diseases 0.000 claims 1
- 125000005045 dihydroisoquinolinyl group Chemical group C1(NC=CC2=CC=CC=C12)* 0.000 claims 1
- 125000005044 dihydroquinolinyl group Chemical group N1(CC=CC2=CC=CC=C12)* 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000010102 embolization Effects 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 210000002837 heart atrium Anatomy 0.000 claims 1
- 239000007943 implant Substances 0.000 claims 1
- 125000003387 indolinyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 claims 1
- 201000004332 intermediate coronary syndrome Diseases 0.000 claims 1
- 201000010849 intracranial embolism Diseases 0.000 claims 1
- 125000000904 isoindolyl group Chemical group C=1(NC=C2C=CC=CC12)* 0.000 claims 1
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 1
- 125000001786 isothiazolyl group Chemical group 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 230000003836 peripheral circulation Effects 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 230000000069 prophylactic effect Effects 0.000 claims 1
- 230000002685 pulmonary effect Effects 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000003039 tetrahydroisoquinolinyl group Chemical group C1(NCCC2=CC=CC=C12)* 0.000 claims 1
- RWRDLPDLKQPQOW-UHFFFAOYSA-N tetrahydropyrrole Substances C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 1
- 125000000147 tetrahydroquinolinyl group Chemical group N1(CCCC2=CC=CC=C12)* 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 1
- 201000005060 thrombophlebitis Diseases 0.000 claims 1
- 230000001052 transient effect Effects 0.000 claims 1
- 0 CC(C*(C)N(C1)C(C(C)(*)I*)=O)c2c1cccc2 Chemical compound CC(C*(C)N(C1)C(C(C)(*)I*)=O)c2c1cccc2 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US94379107P | 2007-06-13 | 2007-06-13 | |
| US60/943,791 | 2007-06-13 | ||
| US4951608P | 2008-05-01 | 2008-05-01 | |
| US61/049,516 | 2008-05-01 | ||
| PCT/US2008/066506 WO2008157162A1 (en) | 2007-06-13 | 2008-06-11 | Dipeptide analogs as coagulation factor inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010529991A JP2010529991A (ja) | 2010-09-02 |
| JP2010529991A5 true JP2010529991A5 (enExample) | 2010-11-04 |
| JP5318094B2 JP5318094B2 (ja) | 2013-10-16 |
Family
ID=39714076
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010512311A Expired - Fee Related JP5318094B2 (ja) | 2007-06-13 | 2008-06-11 | 凝固因子阻害剤としてのジペプチド類似体 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US8367709B2 (enExample) |
| EP (1) | EP2152664B1 (enExample) |
| JP (1) | JP5318094B2 (enExample) |
| KR (1) | KR20100037600A (enExample) |
| CN (1) | CN101784516B (enExample) |
| AR (1) | AR067329A1 (enExample) |
| AU (1) | AU2008266228A1 (enExample) |
| CL (1) | CL2008001724A1 (enExample) |
| MX (1) | MX2009012847A (enExample) |
| PE (1) | PE20091002A1 (enExample) |
| TW (1) | TW200848024A (enExample) |
| WO (1) | WO2008157162A1 (enExample) |
Families Citing this family (65)
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|---|---|---|---|---|
| EP1567487A4 (en) | 2002-11-15 | 2005-11-16 | Bristol Myers Squibb Co | OPEN-CHAINED, PROLYL-FROSTED MODULATORS OF ANDROGEN RECEPTOR FUNCTION |
| CN102026996B (zh) * | 2008-03-13 | 2015-01-07 | 百时美施贵宝公司 | 作为凝血因子xia抑制剂的哒嗪衍生物 |
| AU2009250843A1 (en) * | 2008-05-19 | 2009-11-26 | Actelion Pharmaceuticals Ltd | Tetrahydroisoquinolines as antimalarial agents |
| JP5536876B2 (ja) * | 2009-04-22 | 2014-07-02 | アクテリオン ファーマシューティカルズ リミテッド | チアゾール誘導体及びｐ２ｙ１２受容体拮抗剤としてのそれらの使用 |
| JP5844287B2 (ja) | 2010-02-11 | 2016-01-13 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | 第ｘｉａ因子阻害剤としてのマクロ環 |
| GB2494851A (en) * | 2011-07-07 | 2013-03-27 | Kalvista Pharmaceuticals Ltd | Plasma kallikrein inhibitors |
| TW201311689A (zh) | 2011-08-05 | 2013-03-16 | 必治妥美雅史谷比公司 | 作為因子ｘｉａ抑制劑之新穎巨環化合物 |
| TW201319068A (zh) | 2011-08-05 | 2013-05-16 | 必治妥美雅史谷比公司 | 作為ｘｉａ因子抑制劑之環狀ｐ１接合劑 |
| IN2014CN02805A (enExample) * | 2011-10-14 | 2015-07-03 | Bristol Myers Squibb Co | |
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| LT2766346T (lt) | 2011-10-14 | 2017-06-12 | Bristol-Myers Squibb Company | Pakeistieji tetrahidroizochinolino junginiai, kaip faktoriaus xia inhibitoriai |
| JP2015083542A (ja) * | 2012-02-08 | 2015-04-30 | 大日本住友製薬株式会社 | ３位置換プロリン誘導体 |
| GB201209138D0 (en) * | 2012-05-24 | 2012-07-04 | Ono Pharmaceutical Co | Compounds |
| US9758480B2 (en) | 2012-07-19 | 2017-09-12 | Sumitomo Dainippon Pharma Co., Ltd. | 1-(cycloalkyl-carbonyl)proline derivative |
| KR20150038372A (ko) | 2012-08-03 | 2015-04-08 | 브리스톨-마이어스 스큅 컴퍼니 | 인자 XIa 억제제로서의 디히드로피리돈 P1 |
| CA2880898A1 (en) | 2012-08-03 | 2014-02-06 | Bristol-Myers Squibb Company | Dihydropyridone p1 as factor xia inhibitors |
| US9403774B2 (en) | 2012-10-12 | 2016-08-02 | Bristol-Myers Squibb Company | Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| EP2906552B1 (en) | 2012-10-12 | 2017-11-22 | Bristol-Myers Squibb Company | Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| HRP20180465T1 (hr) | 2012-10-12 | 2018-05-04 | Bristol-Myers Squibb Company | Kristalni oblici inhibitora faktora xia |
| JP6479763B2 (ja) | 2013-03-25 | 2019-03-06 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | 第ｘｉａ因子阻害剤としての置換アゾール含有のテトラヒドロイソキノリン |
| EP3054944B1 (en) | 2013-10-07 | 2019-12-04 | Merck Sharp & Dohme Corp. | Factor xia inhibitors |
| NO2760821T3 (enExample) | 2014-01-31 | 2018-03-10 | ||
| JP6505727B2 (ja) | 2014-01-31 | 2019-04-24 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | ヘテロ環式ｐ２’基を有する第ｘｉａ因子阻害剤としてのマクロ環 |
| EP3104703B1 (en) | 2014-02-11 | 2020-11-18 | Merck Sharp & Dohme Corp. | Factor xia inhibitors |
| EP3104702B1 (en) | 2014-02-11 | 2022-08-10 | Merck Sharp & Dohme LLC | Factor xia inhibitors |
| WO2015164308A1 (en) | 2014-04-22 | 2015-10-29 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
| WO2015183709A1 (en) * | 2014-05-28 | 2015-12-03 | Merck Sharp & Dohme Corp. | Factor xia inhibitors |
| US9868727B2 (en) | 2014-07-28 | 2018-01-16 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
| EP3180325B1 (en) * | 2014-07-28 | 2019-03-20 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
| JP6526796B2 (ja) | 2014-09-04 | 2019-06-05 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | Ｆｘｉａ阻害剤であるジアミドマクロ環 |
| US9453018B2 (en) | 2014-10-01 | 2016-09-27 | Bristol-Myers Squibb Company | Pyrimidinones as factor XIa inhibitors |
| CN105294669B (zh) * | 2014-10-24 | 2019-01-22 | 山东凯森制药有限公司 | 一种第十因子抑制剂及其制备方法和应用 |
| JP2018502137A (ja) * | 2015-01-20 | 2018-01-25 | メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． | 第ＸＩａ因子阻害剤 |
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| IT201600074606A1 (it) * | 2016-07-18 | 2018-01-18 | Italfarmaco Spa | New benzo-N-hydroxy amide compounds having antitumor activity |
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| WO2021032933A1 (en) * | 2019-08-21 | 2021-02-25 | Kalvista Pharmaceuticals Limited | Enzyme inhibitors |
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| CN113943259A (zh) * | 2020-07-17 | 2022-01-18 | 西安禾渼生物医药有限公司 | 一种氨基酸衍生物、其制备方法及应用 |
| RS66874B1 (sr) * | 2020-09-17 | 2025-06-30 | Novartis Ag | Jedinjenja i kompozicije kao inhibitori sppl2a |
| CN112341398B (zh) * | 2020-11-11 | 2022-05-03 | 湖北文理学院 | 具有生物活性的1,2,3-三氮唑取代的查尔酮衍生物、制备方法及其应用 |
| WO2022122035A1 (zh) * | 2020-12-11 | 2022-06-16 | 上海领泰生物医药科技有限公司 | 凝血因子XIa抑制剂及其制备方法和应用 |
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| CN113636982A (zh) * | 2021-04-28 | 2021-11-12 | 合肥工业大学 | 一种肉桂酸衍生物及其制备方法和用途 |
| CN116655534A (zh) * | 2023-06-07 | 2023-08-29 | 上海吉奉生物科技有限公司 | 一种Boc-3-（3-吡唑）- L -丙氨酸的合成方法 |
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2008
- 2008-06-11 KR KR1020107000723A patent/KR20100037600A/ko not_active Withdrawn
- 2008-06-11 WO PCT/US2008/066506 patent/WO2008157162A1/en not_active Ceased
- 2008-06-11 US US12/663,861 patent/US8367709B2/en active Active
- 2008-06-11 CL CL200801724A patent/CL2008001724A1/es unknown
- 2008-06-11 MX MX2009012847A patent/MX2009012847A/es active IP Right Grant
- 2008-06-11 EP EP08770664.4A patent/EP2152664B1/en not_active Not-in-force
- 2008-06-11 JP JP2010512311A patent/JP5318094B2/ja not_active Expired - Fee Related
- 2008-06-11 AR ARP080102487A patent/AR067329A1/es not_active Application Discontinuation
- 2008-06-11 TW TW097121816A patent/TW200848024A/zh unknown
- 2008-06-11 AU AU2008266228A patent/AU2008266228A1/en not_active Abandoned
- 2008-06-11 CN CN200880103481.1A patent/CN101784516B/zh not_active Expired - Fee Related
- 2008-06-11 PE PE2008001000A patent/PE20091002A1/es not_active Application Discontinuation