EA029759B1 - Антидиабетические лекарственные средства, содержащие ингибитор dpp-4 (линаглиптин) необязательно в комбинации с другими антидиабетическими средствами - Google Patents
Антидиабетические лекарственные средства, содержащие ингибитор dpp-4 (линаглиптин) необязательно в комбинации с другими антидиабетическими средствами Download PDFInfo
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- EA029759B1 EA029759B1 EA201101187A EA201101187A EA029759B1 EA 029759 B1 EA029759 B1 EA 029759B1 EA 201101187 A EA201101187 A EA 201101187A EA 201101187 A EA201101187 A EA 201101187A EA 029759 B1 EA029759 B1 EA 029759B1
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- EA
- Eurasian Patent Office
- Prior art keywords
- inhibitor
- treatment
- combination
- antidiabetic agent
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- 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
- C07D417/14—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 three or more hetero rings
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Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09152869 | 2009-02-13 | ||
| PCT/EP2010/051817 WO2010092163A2 (en) | 2009-02-13 | 2010-02-12 | Antidiabetic medications |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201101187A1 EA201101187A1 (ru) | 2012-10-30 |
| EA029759B1 true EA029759B1 (ru) | 2018-05-31 |
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| EA201101187A EA029759B1 (ru) | 2009-02-13 | 2010-02-12 | Антидиабетические лекарственные средства, содержащие ингибитор dpp-4 (линаглиптин) необязательно в комбинации с другими антидиабетическими средствами |
Country Status (14)
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| US (6) | US20120094894A1 (enExample) |
| EP (1) | EP2395988A2 (enExample) |
| JP (3) | JP2012517977A (enExample) |
| KR (2) | KR20110115582A (enExample) |
| CN (3) | CN106177958A (enExample) |
| AU (1) | AU2010212823B2 (enExample) |
| BR (1) | BRPI1013639A2 (enExample) |
| CA (1) | CA2752437C (enExample) |
| CL (1) | CL2011001853A1 (enExample) |
| EA (1) | EA029759B1 (enExample) |
| IL (1) | IL213716A0 (enExample) |
| MX (2) | MX387264B (enExample) |
| NZ (2) | NZ619520A (enExample) |
| WO (1) | WO2010092163A2 (enExample) |
Families Citing this family (107)
| 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 |
| EP2540725A1 (de) | 2006-05-04 | 2013-01-02 | Boehringer Ingelheim International GmbH | Polymorphe von 1-((4-Methyl-chinazolin-2-yl)methyl)-3-methyl-7-(2-butin-1-yl)-8-(3-(R)-amino-piperidin-1-yl)xanthin |
| 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 |
| PE20090938A1 (es) | 2007-08-16 | 2009-08-08 | Boehringer Ingelheim Int | Composicion farmaceutica que comprende un derivado de benceno sustituido con glucopiranosilo |
| PE20091730A1 (es) | 2008-04-03 | 2009-12-10 | Boehringer Ingelheim Int | Formulaciones que comprenden un inhibidor de dpp4 |
| EP2146210A1 (en) | 2008-04-07 | 2010-01-20 | Arena Pharmaceuticals, Inc. | Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditions modulated by PYY |
| UY32030A (es) | 2008-08-06 | 2010-03-26 | Boehringer Ingelheim Int | "tratamiento para diabetes en pacientes inapropiados para terapia con metformina" |
| BRPI0916997A2 (pt) | 2008-08-06 | 2020-12-15 | Boehringer Ingelheim International Gmbh | Inibidor de dpp-4 e seu uso |
| AU2009281122C1 (en) * | 2008-08-15 | 2016-04-21 | Boehringer Ingelheim International Gmbh | Purin derivatives for use in the treatment of fab-related diseases |
| JP2012502081A (ja) | 2008-09-10 | 2012-01-26 | 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 | 糖尿病及び関連症状の治療のための組み合わせ治療 |
| 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 |
| BRPI0920881B1 (pt) | 2008-10-17 | 2021-09-21 | Sanofi-Aventis Deutschland Gmbh | Composição farmacêutica, seu uso e método de preparação da mesma, kit e dispositivo |
| MX2011006713A (es) | 2008-12-23 | 2011-07-13 | Boehringer Ingelheim Int | Formas salinas de compuesto organico. |
| TW201036975A (en) | 2009-01-07 | 2010-10-16 | Boehringer Ingelheim Int | Treatment for diabetes in patients with inadequate glycemic control despite metformin therapy |
| AP2011005794A0 (en) | 2009-02-13 | 2011-08-31 | Boehringer Ingelheim Int | Pharmaceutical composition comprising a SGLT2 inhibitor, a DPP-IV inhibitor and optionally a furtherantidiabetic agent and uses thereof. |
| BR112012007085B8 (pt) | 2009-09-30 | 2021-05-25 | Boehringer Ingelheim Int | processos para a preparação de derivados de benzil-benzeno substituídos com glicopiranosila |
| 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 |
| DK2498802T3 (en) | 2009-11-13 | 2015-04-13 | Sanofi Aventis Deutschland | Pharmaceutical composition comprising a GLP-1 agonist, insulin and a methionine |
| LT2498758T (lt) | 2009-11-13 | 2018-11-26 | Astrazeneca Ab | Dvisluoksnės tabletės formuluotės |
| NZ599847A (en) | 2009-11-13 | 2013-09-27 | Sanofi Aventis Deutschland | Pharmaceutical composition comprising a glp-1 agonist and methionine |
| KR20120107080A (ko) | 2009-11-27 | 2012-09-28 | 베링거 인겔하임 인터내셔날 게엠베하 | 리나글립틴과 같은 dpp-iv 억제제를 사용한 유전자형 검사된 당뇨병 환자의 치료 |
| CN107961377B (zh) | 2010-05-05 | 2022-11-22 | 勃林格殷格翰国际有限公司 | 组合疗法 |
| US20120107398A1 (en) * | 2010-05-05 | 2012-05-03 | Boehringer Ingelheim International Gmbh | Pharmaceutical compositions |
| AU2011202239C1 (en) | 2010-05-19 | 2017-03-16 | Sanofi | Long-acting formulations of insulins |
| KR20130093012A (ko) | 2010-06-24 | 2013-08-21 | 베링거 인겔하임 인터내셔날 게엠베하 | 당뇨병 요법 |
| MX339614B (es) | 2010-08-30 | 2016-06-02 | Sanofi - Aventis Deutschland GmbH | Uso de ave0010 para la fabricacion de un medicamento para el tratamiento de la diabetes mellitus tipo 2. |
| AU2016202261B2 (en) * | 2010-11-15 | 2017-11-30 | Boehringer Ingelheim International Gmbh | Vasoprotective and cardioprotective antidiabetic therapy |
| MX371198B (es) * | 2010-11-15 | 2020-01-22 | Boehringer Ingelheim Int | Terapia antidiabetica vasoprotectora y cardioprotectora. |
| US9034883B2 (en) | 2010-11-15 | 2015-05-19 | Boehringer Ingelheim International Gmbh | Vasoprotective and cardioprotective antidiabetic therapy |
| AU2011343190B2 (en) | 2010-12-16 | 2016-12-08 | Novo Nordisk A/S | Solid compositions comprising a GLP-1 agonist and a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid |
| TR201107482A1 (tr) * | 2010-12-21 | 2012-07-23 | Sanovel İlaç San.Ve Ti̇c.A.Ş. | Vildagliptin ve gliklazidin iki tabakalı kombinasyon kompozisyonu. |
| EP2468268B1 (en) * | 2010-12-21 | 2017-12-13 | Sanovel Ilaç Sanayi Ve Ticaret Anonim Sirketi | Combination composition of vildagliptin and gliclazide |
| TR201101809A1 (tr) * | 2010-12-21 | 2012-07-23 | Sanovel İlaç Sanayi̇ Ve Ti̇caret Anoni̇m Şi̇rketi̇ | Vildagliptin ve glimepirid kombinasyonları. |
| MX2013008484A (es) * | 2011-02-02 | 2013-08-12 | Sanofi Aventis Deutschland | Prevencion de hidroglucemia en pacientes con diabetes mellitus tipo 2. |
| CN103391798A (zh) * | 2011-02-24 | 2013-11-13 | 久光制药株式会社 | 微针装置用glp-1类似物组合物 |
| AR085689A1 (es) | 2011-03-07 | 2013-10-23 | Boehringer Ingelheim Int | Composiciones farmaceuticas de metformina, linagliptina y un inhibidor de sglt-2 |
| EP3225631B1 (en) | 2011-04-12 | 2019-01-09 | Novo Nordisk A/S | Double-acylated glp-1 derivatives |
| US9821032B2 (en) | 2011-05-13 | 2017-11-21 | Sanofi-Aventis Deutschland Gmbh | Pharmaceutical combination for improving glycemic control as add-on therapy to basal insulin |
| MX362527B (es) * | 2011-05-13 | 2019-01-23 | Sanofi Aventis Deutschland | Combinacion farmaceutica para uso en el control glucemico en pacientes con diabetes de tipo 2. |
| UA113626C2 (xx) | 2011-06-02 | 2017-02-27 | Композиція для лікування діабету, що містить кон'югат інсуліну тривалої дії та кон'югат інсулінотропного пептиду тривалої дії | |
| EP3517539B1 (en) | 2011-07-15 | 2022-12-14 | Boehringer Ingelheim International GmbH | Substituted dimeric quinazoline derivative, its preparation and its use in pharmaceutical compositions for the treatment of type i and ii diabetes |
| CN108079281A (zh) * | 2011-08-29 | 2018-05-29 | 赛诺菲-安万特德国有限公司 | 用于2型糖尿病患者中的血糖控制的药物组合 |
| AR087744A1 (es) | 2011-09-01 | 2014-04-16 | Sanofi Aventis Deutschland | Composicion farmaceutica para uso en el tratamiento de una enfermedad neurodegenerativa |
| US20130172244A1 (en) * | 2011-12-29 | 2013-07-04 | Thomas Klein | Subcutaneous therapeutic use of dpp-4 inhibitor |
| US9555001B2 (en) | 2012-03-07 | 2017-01-31 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition and uses thereof |
| WO2013134546A1 (en) | 2012-03-07 | 2013-09-12 | Mayo Foundation For Medical Education And Research | Methods and materials for treating cancer |
| US9192617B2 (en) | 2012-03-20 | 2015-11-24 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
| EP2827885B1 (en) | 2012-03-22 | 2018-08-15 | Novo Nordisk A/S | Compositions of glp-1 peptides and preparation thereof |
| PL3542790T3 (pl) * | 2012-03-22 | 2024-02-26 | Novo Nordisk A/S | Kompozycje zawierające substancję dostarczającą i ich przygotowanie |
| ES2715308T3 (es) | 2012-03-22 | 2019-06-03 | Novo Nordisk As | Composiciones que comprenden un agente de suministro y su preparación |
| EP3685839A1 (en) | 2012-05-14 | 2020-07-29 | Boehringer Ingelheim International GmbH | Linagliptin for use in the treatment of albuminuria and kidney related diseases |
| 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 |
| 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 |
| JP6517690B2 (ja) | 2012-06-20 | 2019-05-22 | ノヴォ ノルディスク アー/エス | ペプチド及び送達剤を含む錠剤製剤 |
| DK2866825T3 (da) * | 2012-07-01 | 2020-06-08 | Novo Nordisk As | Anvendelse af langstidsvirkende glp-1-peptider |
| AU2013304178B2 (en) * | 2012-08-13 | 2017-08-17 | Sandoz Ag | Stable pharmaceutical composition containing 8-[(3R)-3-Amino-1-piperidinyl]-7-(2-butyn-1-yl)-3,7-dihydro-3-methyl-1-[(4-methyl-2-quinazolinyl)methyl]-1H-purine-2,6-dione or a pharmaceutically acceptable salt thereof |
| CN103877054B (zh) * | 2012-12-21 | 2016-05-25 | 北大方正集团有限公司 | 一种苯甲酸阿格列汀片剂及其制备方法 |
| WO2014102715A1 (en) | 2012-12-24 | 2014-07-03 | Ranbaxy Laboratories Limited | Pharmaceutical compositions comprising a biguanide and a low dose antidiabetic agent |
| JP6457484B2 (ja) | 2013-04-03 | 2019-01-23 | サノフイSanofi | インスリンの長時間作用型製剤による糖尿病の治療 |
| US20140303097A1 (en) | 2013-04-05 | 2014-10-09 | 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 |
| US11813275B2 (en) | 2013-04-05 | 2023-11-14 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
| HRP20190101T1 (hr) | 2013-04-05 | 2019-03-08 | Boehringer Ingelheim International Gmbh | Terapeutske uporabe empagliflozina |
| HUE058731T2 (hu) | 2013-04-18 | 2022-09-28 | Boehringer Ingelheim Int | Gyógyászati készítmények, kezelési eljárások és ezek alkalmazásai |
| MY172578A (en) | 2013-05-02 | 2019-12-03 | Novo Nordisk As | Oral dosing of glp-1 compounds |
| WO2014184742A1 (en) | 2013-05-13 | 2014-11-20 | Ranbaxy Laboratories Limited | Pharmaceutical compositions containing a biguanide and a low dose antidiabetic agent |
| WO2014184376A1 (en) * | 2013-05-17 | 2014-11-20 | Boehringer Ingelheim International Gmbh | Combination of a dpp-4 inhibitor and an alpha-glucosidase inhibitor |
| KR101598612B1 (ko) * | 2013-08-29 | 2016-02-26 | 재단법인 아산사회복지재단 | Dpp-4 억제제를 포함하는 혈관 또는 심장판막 석회화의 예방 또는 치료용 조성물 |
| EP2848241A1 (en) * | 2013-09-12 | 2015-03-18 | Sanovel Ilac Sanayi ve Ticaret A.S. | Effervescent formulations of linagliptin |
| EP2848242A1 (en) * | 2013-09-12 | 2015-03-18 | Sanovel Ilac Sanayi ve Ticaret A.S. | Orally disintegrating formulations of Linagliptin |
| 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 |
| EP3177292B1 (en) | 2014-08-07 | 2020-11-25 | Mayo Foundation for Medical Education and Research | Compounds and methods for treating cancer |
| KR20160062517A (ko) * | 2014-11-25 | 2016-06-02 | 경북대학교병원 | Dpp4 저해제를 유효성분으로 함유하는 혈관 석회화 억제용 약학적 조성물 |
| BR112017012406A2 (pt) | 2014-12-12 | 2018-07-31 | Sanofi Aventis Deutschland | formulação com relação fixa de insulina glargina/lixisenatida |
| KR101526825B1 (ko) * | 2014-12-23 | 2015-06-08 | 주식회사 한독 | 당뇨병 치료용 약제학적 조성물 |
| AU2015384339B2 (en) * | 2015-02-27 | 2018-08-09 | The Asan Foundation | Composition for preventing or treating valve calcification, containing DPP-4 inhibitor |
| JP6847044B2 (ja) * | 2015-03-11 | 2021-03-24 | シーシーエス・ベンチャーズ・リミテッド | 肥満及び2型糖尿病(t2d)の治療のための膵内分泌前駆細胞療法 |
| TWI748945B (zh) | 2015-03-13 | 2021-12-11 | 德商賽諾菲阿凡提斯德意志有限公司 | 第2型糖尿病病患治療 |
| TW201705975A (zh) | 2015-03-18 | 2017-02-16 | 賽諾菲阿凡提斯德意志有限公司 | 第2型糖尿病病患之治療 |
| HRP20200845T1 (hr) * | 2015-11-06 | 2020-08-07 | Genesis Pharma Sa | Kombinacija kanrenoata i eksenatida |
| KR101782119B1 (ko) * | 2016-02-01 | 2017-10-23 | 주식회사 한독 | 테넬리글립틴 및 설포닐우레아계 약물을 포함하는 정제 |
| MX390363B (es) | 2016-06-10 | 2025-03-20 | Boehringer Ingelheim Int | Combinacion de linagliptina y metformina |
| KR102758804B1 (ko) | 2016-10-31 | 2025-01-23 | 엘지디스플레이 주식회사 | 발광 영역들을 포함하는 디스플레이 장치 |
| MX2019005435A (es) | 2016-11-10 | 2019-07-10 | Boehringer Ingelheim Int | Composicion farmaceutica, metodos para tratamiento y sus usos. |
| SI3554534T1 (sl) | 2016-12-16 | 2021-09-30 | Novo Nordisk A/S | Farmacevtski sestavki, ki vsebujejo inzulin |
| EA039402B1 (ru) * | 2017-02-03 | 2022-01-24 | Гленмарк Фармасьтикалз Лимитед | Оксалаты тенелиглиптина и их сольваты, промежуточные соединения, способ получения и их маркеры |
| KR102469957B1 (ko) * | 2017-06-30 | 2022-11-24 | 한미약품 주식회사 | 리나글립틴, 메트포르민 및 항산화제를 포함하는, 안정성이 개선된 약제학적 조성물 |
| EP3694538A1 (en) | 2017-10-12 | 2020-08-19 | Novo Nordisk A/S | Semaglutide in medical therapy |
| KR102500835B1 (ko) * | 2017-10-24 | 2023-02-17 | 한미약품 주식회사 | 리나글립틴 및 메트포르민을 포함하는 복합제제 및 그의 제조방법 |
| EP3743092A4 (en) | 2018-01-23 | 2021-10-20 | Gila Therapeutics, Inc. | PHARMACEUTICAL PEPTIDE-YY FORMULATIONS, COMPOSITIONS, AND PROCEDURES |
| AR114353A1 (es) | 2018-02-02 | 2020-08-26 | Novo Nordisk As | Composiciones sólidas que comprenden un agonista del glp-1 y una sal del ácido n-(8-(2-hidroxibenzoil)amino)caprílico |
| KR102695130B1 (ko) * | 2018-05-31 | 2024-08-16 | 후아 메디슨 (상하이) 엘티디. | 글루코키나제 활성화제 및 ppar 수용체 활성화제를 함유하는 약제학적 병용물, 조성물, 및 병용 제제, 및 이의 제조 방법 및 용도 |
| EP3823624A1 (en) * | 2018-07-17 | 2021-05-26 | Boehringer Ingelheim International GmbH | Cardiosafe antidiabetic therapy |
| MX2021003830A (es) * | 2018-10-04 | 2021-09-30 | Hanmi Pharm Ind Co Ltd | Uso terapéutico del glucagón y combinación que incluye el mismo. |
| AU2020245801A1 (en) * | 2019-03-25 | 2021-11-11 | The George Institute for Global Health | Low-dose triple combination formulation |
| EP3996717A1 (en) * | 2019-07-09 | 2022-05-18 | Genesis Pharma SA | Combination |
| CN110314233B (zh) * | 2019-08-12 | 2021-07-23 | 浙江养生堂天然药物研究所有限公司 | 包含柠檬苦素类化合物和dpp-4抑制剂的组合产品 |
| CN110652498B (zh) * | 2019-11-22 | 2022-04-05 | 河南合智医药科技有限公司 | 一种用于治疗2型糖尿病的药物制剂及其制备方法 |
| CN116509844B (zh) * | 2019-12-31 | 2024-06-04 | 石药集团中奇制药技术(石家庄)有限公司 | 一种二肽基肽酶4抑制剂的药物组合物及其制备方法和应用 |
| KR102289381B1 (ko) * | 2020-03-17 | 2021-08-17 | 주식회사 대웅테라퓨틱스 | 당뇨치료제 및 고지혈증 치료제를 포함하는 약학적 조성물 |
| US11478533B2 (en) | 2020-04-27 | 2022-10-25 | Novo Nordisk A/S | Semaglutide for use in medicine |
| EP4415720A4 (en) * | 2021-10-17 | 2025-07-30 | Zenvision Pharma Llp | NEW PARENTERAL COMPOSITION COMPRISING LINAGLIPTIN OR ITS SALTS |
Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007120936A2 (en) * | 2006-01-06 | 2007-10-25 | Novartis Ag | Use.of vildagliptin for the treatment of diabetes |
| EP1852108A1 (en) * | 2006-05-04 | 2007-11-07 | Boehringer Ingelheim Pharma GmbH & Co.KG | DPP IV inhibitor formulations |
| WO2007128761A2 (de) * | 2006-05-04 | 2007-11-15 | Boehringer Ingelheim International Gmbh | Verwendungen von dpp iv inhibitoren |
| KR20070111099A (ko) * | 2006-05-16 | 2007-11-21 | 영진약품공업주식회사 | 시타글립틴 염산염의 신규 결정형, 이의 제조 방법과 이를포함하는 약학적 조성물 |
| WO2007149797A2 (en) * | 2006-06-19 | 2007-12-27 | Novartis Ag | Use of organic compounds |
| CN101234105A (zh) * | 2008-01-09 | 2008-08-06 | 北京润德康医药技术有限公司 | 一种含有二甲双胍和维格列汀的药用组合物及其制备方法 |
| WO2008093878A1 (en) * | 2007-02-01 | 2008-08-07 | Takeda Pharmaceutical Company Limited | Tablet preparation without causing a tableting trouble |
Family Cites Families (86)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5093330A (en) | 1987-06-15 | 1992-03-03 | Ciba-Geigy Corporation | Staurosporine derivatives substituted at methylamino nitrogen |
| TW225528B (enExample) | 1992-04-03 | 1994-06-21 | Ciba Geigy Ag | |
| CO4950519A1 (es) | 1997-02-13 | 2000-09-01 | Novartis Ag | Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion |
| CO5150173A1 (es) | 1998-12-10 | 2002-04-29 | Novartis Ag | Compuestos n-(glicilo sustituido)-2-cianopirrolidinas inhibidores de peptidasa de dipeptidilo-iv (dpp-iv) los cuales son efectivos en el tratamiento de condiciones mediadas por la inhibicion de dpp-iv |
| US6395767B2 (en) | 2000-03-10 | 2002-05-28 | Bristol-Myers Squibb Company | Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method |
| EP1930319B1 (en) | 2000-08-10 | 2012-05-02 | Mitsubishi Tanabe Pharma Corporation | Proline derivatives and use thereof as drugs |
| ES2326911T3 (es) | 2001-02-24 | 2009-10-21 | BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG | Derivados de xantina para uso como medicamentos, asi como su procedimiento de preparacion. |
| UA74912C2 (en) | 2001-07-06 | 2006-02-15 | Merck & Co Inc | Beta-aminotetrahydroimidazo-(1,2-a)-pyrazines and tetratriazolo-(4,3-a)-pyrazines as inhibitors of dipeptylpeptidase for the treatment or prevention of diabetes |
| US6861440B2 (en) | 2001-10-26 | 2005-03-01 | Hoffmann-La Roche Inc. | DPP IV inhibitors |
| GB0215676D0 (en) | 2002-07-05 | 2002-08-14 | Novartis Ag | Organic compounds |
| ATE453644T1 (de) | 2002-08-21 | 2010-01-15 | Boehringer Ingelheim Pharma | 8-[3-amino-piperidin-1-yl] -xanthine, deren herstellung und deren verwendung als arzneimittel |
| DE10238477A1 (de) | 2002-08-22 | 2004-03-04 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Purinderivate, deren Herstellung und deren Verwendung als Arzneimittel |
| DE10238470A1 (de) | 2002-08-22 | 2004-03-04 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Xanthinderivate, deren Herstellung und deren Verwendung als Arzneimittel |
| DE10251927A1 (de) | 2002-11-08 | 2004-05-19 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Xanthinderivate, deren Herstellung und deren Verwendung als Arzneimittel |
| DE10254304A1 (de) | 2002-11-21 | 2004-06-03 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Xanthinderivate, deren Herstellung und deren Verwendung als Arzneimittel |
| UY28103A1 (es) | 2002-12-03 | 2004-06-30 | Boehringer Ingelheim Pharma | Nuevas imidazo-piridinonas sustituidas, su preparación y su empleo como medicacmentos |
| US7420079B2 (en) | 2002-12-09 | 2008-09-02 | Bristol-Myers Squibb Company | Methods and compounds for producing dipeptidyl peptidase IV inhibitors and intermediates thereof |
| DE10327439A1 (de) | 2003-06-18 | 2005-01-05 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Imidazopyridazinon- und Imidazopyridonderivate, deren Herstellung und deren Verwendung als Arzneimittel |
| CN100374439C (zh) | 2003-06-20 | 2008-03-12 | 霍夫曼-拉罗奇有限公司 | 作为dpp-iv抑制剂的吡啶并‘2,1-a-异喹啉衍生物 |
| JO2625B1 (en) | 2003-06-24 | 2011-11-01 | ميرك شارب اند دوم كوربوريشن | Phosphoric acid salts of dipeptidyl betidase inhibitor 4 |
| BRPI0416444B8 (pt) | 2003-11-12 | 2021-05-25 | Chiesi Farm Spa | composto de ácido borônico heterocíclico, composição farmacêutica, e, combinação farmacêutica compreendendo o mesmo |
| 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 |
| DE10359098A1 (de) | 2003-12-17 | 2005-07-28 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue 2-(Piperazin-1-yl)- und 2-([1,4]Diazepan-1-yl)-imidazo[4,5-d]pyridazin-4-one, deren Herstellung und deren Verwendung als Arzneimittel |
| DE10360835A1 (de) | 2003-12-23 | 2005-07-21 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Bicyclische Imidazolverbindungen, deren Herstellung und deren Verwendung als Arzneimittel |
| PT3738585T (pt) | 2004-01-20 | 2023-01-30 | Novartis Ag | Formulação e processo de compressão direta |
| EP1712547B1 (en) | 2004-02-05 | 2011-12-14 | Kyorin Pharmaceutical Co., Ltd. | Bicycloester derivative |
| RS50982B (sr) | 2004-02-18 | 2010-10-31 | Boehringer Ingelheim International Gmbh. | 8-[3-amino piperidin-1-il]-ksantini, njihovo dobijanje i njihova primena kao dpp-iv inhibitora |
| DE102004009039A1 (de) | 2004-02-23 | 2005-09-08 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | 8-[3-Amino-piperidin-1-yl]-xanthine, deren Herstellung und Verwendung als Arzneimittel |
| WO2005095381A1 (en) | 2004-03-15 | 2005-10-13 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| CA2561210A1 (en) | 2004-04-10 | 2005-10-20 | Boehringer Ingelheim International Gmbh | Novel 2-amino-imidazo[4,5-d]pyridazin-4-ones and 2-amino-imidazo[4,5-c]pyridin-4-ones, production and use thereof as medicaments |
| US7741082B2 (en) | 2004-04-14 | 2010-06-22 | Bristol-Myers Squibb Company | Process for preparing dipeptidyl peptidase IV inhibitors and intermediates therefor |
| AP2320A (en) | 2004-05-12 | 2011-11-07 | Pfizer Procucts Inc | Proline derivatives and their use as dipeptidyl peptidase IV inhibitors. |
| US7214702B2 (en) | 2004-05-25 | 2007-05-08 | Bristol-Myers Squibb Company | Process for producing a dipeptidyl peptidase IV inhibitor |
| TWI415635B (zh) | 2004-05-28 | 2013-11-21 | 必治妥施貴寶公司 | 加衣錠片調製物及製備彼之方法 |
| DE102004043944A1 (de) | 2004-09-11 | 2006-03-30 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue 8-(3-Amino-piperidin-1-yl)-7-(but-2-inyl)-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 |
| BRPI0516446A (pt) | 2004-10-08 | 2008-09-02 | Novartis Ag | combinação de compostos orgánicos |
| JP4959569B2 (ja) | 2004-10-12 | 2012-06-27 | グレンマーク・ファーマシューティカルズ・エスエー | 新規なジペプチジルペプチダーゼiv阻害剤、それらを含む医薬品組成物、およびそれらを調製するためのプロセス |
| WO2006047248A1 (en) * | 2004-10-25 | 2006-05-04 | Novartis Ag | Combination of dpp-iv inhibitor, ppar antidiabetic and metformin |
| 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 |
| AU2005320134B2 (en) | 2004-12-24 | 2011-04-28 | Dainippon Sumitomo Pharma Co., Ltd. | Bicyclic pyrrole derivatives |
| GT200600008A (es) | 2005-01-18 | 2006-08-09 | Formulacion de compresion directa y proceso | |
| CN101119991B (zh) | 2005-02-18 | 2012-01-25 | 田边三菱制药株式会社 | 脯氨酸衍生物的盐,其溶剂合物,及其生产方法 |
| AU2006226447B2 (en) | 2005-03-22 | 2009-07-16 | F. Hoffmann-La Roche Ag | New salt and polymorphs of a DPP-IV inhibitor |
| BRPI0608469A2 (pt) | 2005-04-22 | 2010-01-05 | Alantos Pharmaceuticals Holding Inc | inibidores de dipeptidil peptidase-iv |
| US20090088442A1 (en) | 2005-04-26 | 2009-04-02 | Mitsubishi Tanabe Pharma Corporation | Prophylactic/therapeutic agent for abnormalities of sugar/lipid metabolism |
| DK1894567T3 (da) | 2005-06-03 | 2012-11-19 | Mitsubishi Tanabe Pharma Corp | Ledsagende farmaceutiske midler og anvendelse deraf |
| MY152185A (en) | 2005-06-10 | 2014-08-29 | Novartis Ag | Modified release 1-[(3-hydroxy-adamant-1-ylamino)-acetyl]-pyrrolidine-2(s)-carbonitrile formulation |
| EP2985022B1 (en) | 2005-07-01 | 2018-09-12 | Merck Sharp & Dohme Corp. | Process for synthesizing a cetp inhibitor |
| 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 |
| US20080279932A1 (en) | 2005-08-04 | 2008-11-13 | Jean-Louis Reber | Compounds |
| CA2617715A1 (en) | 2005-08-11 | 2007-02-15 | F. Hoffmann-La Roche Ag | Pharmaceutical composition comprising a dpp-iv inhibitor |
| PL1942898T5 (pl) | 2005-09-14 | 2014-10-31 | Takeda Pharmaceuticals Co | Inhibitory peptydazy dipeptydylowej do leczenia cukrzycy |
| CN102908351B (zh) | 2005-09-14 | 2014-07-23 | 武田药品工业株式会社 | 用于治疗糖尿病的二肽基肽酶抑制剂 |
| TW200745079A (en) | 2005-09-16 | 2007-12-16 | Takeda Pharmaceuticals Co | Polymorphs of benzoate salt of 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile and methods of use therefor |
| CN102675221A (zh) | 2005-09-16 | 2012-09-19 | 武田药品工业株式会社 | 用于制备嘧啶二酮衍生物的方法中的中间体 |
| AU2006306420A1 (en) | 2005-10-25 | 2007-05-03 | Merck Sharp & Dohme Corp. | Combination of a dipeptidyl peptidase-4 inhibitor and an anti-hypertensive agent for the treatment of diabetes and hypertension |
| WO2007071576A1 (en) | 2005-12-21 | 2007-06-28 | F. Hoffmann-La Roche Ag | New salt and polymorph of dpp-iv inhibitor |
| RU2008129873A (ru) | 2005-12-23 | 2010-01-27 | Новартис АГ (CH) | Конденсированные гетероциклические соединения, полезные в качестве ингибиторов дпп-iv |
| JP5094416B2 (ja) | 2005-12-28 | 2012-12-12 | 武田薬品工業株式会社 | 糖尿病治療剤 |
| JP2009531456A (ja) | 2006-03-28 | 2009-09-03 | 武田薬品工業株式会社 | (r)−3−アミノピペリジン二塩酸塩の調製 |
| EP2540725A1 (de) | 2006-05-04 | 2013-01-02 | Boehringer Ingelheim International GmbH | Polymorphe von 1-((4-Methyl-chinazolin-2-yl)methyl)-3-methyl-7-(2-butin-1-yl)-8-(3-(R)-amino-piperidin-1-yl)xanthin |
| WO2007148185A2 (en) | 2006-06-21 | 2007-12-27 | Pfizer Products Inc. | Substituted 3 -amino- pyrrolidino-4 -lactams as dpp inhibitors |
| EP2035395A2 (en) | 2006-06-27 | 2009-03-18 | Glenmark Pharmaceuticals S.A. | Novel processes for the preparation of dpp iv inhibitors |
| EP2057160A1 (en) | 2006-08-08 | 2009-05-13 | Boehringer Ingelheim International GmbH | Pyrrolo [3, 2 -d]pyrimidines as dpp-iv inhibitors for the treatment of diabetes mellitus |
| CL2007002499A1 (es) | 2006-08-30 | 2008-03-14 | Phenomix Corp | Sales citrato y tartrato de compuestos derivados de acido pirrolidinilaminoacetilpirrolidinboronico, inhibidores de dpp-iv; metodo de preparacion; forma solida; combinacion farmaceutica, util para el tratamiento de diabetes. |
| DK2073810T3 (da) | 2006-09-13 | 2011-10-31 | Takeda Pharmaceutical | Anvendelse af 2-6-(3-aminio-piperidin-l-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-l-ylmethyl-4-fluor-benzonitril til behandling af diabetes, cancer, autoimmune sygdomme og HIV infektion |
| EP2069343A2 (en) | 2006-09-15 | 2009-06-17 | F. Hoffmann-Roche AG | Process for the preparation of pyrido[2,1-a]isoquinoline derivatives by catalytic asymmetric hydrogenation of an enamine |
| ATE522529T1 (de) | 2006-09-15 | 2011-09-15 | Hoffmann La Roche | Verfahren zur herstellung von pyridoä2,1- aüisochinolinderivaten, das die racematspaltung eines enamins umfasst |
| US7956201B2 (en) | 2006-11-06 | 2011-06-07 | Hoffman-La Roche Inc. | Process for the preparation of (S)-4-fluoromethyl-dihydro-furan-2-one |
| TW200838536A (en) | 2006-11-29 | 2008-10-01 | Takeda Pharmaceutical | Polymorphs of succinate salt of 2-[6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethy]-4-fluor-benzonitrile and methods of use therefor |
| CN101646420B (zh) | 2007-02-01 | 2012-11-07 | 武田药品工业株式会社 | 包含阿格列汀和吡格列酮的固体制剂 |
| CA2680133A1 (en) | 2007-03-08 | 2008-09-12 | David Alan Campbell | Methods and intermediates for synthesis of selective dpp-iv inhibitors |
| MX2009009703A (es) | 2007-03-13 | 2010-03-03 | Takeda Pharmaceutical | Preparacion solida que comprende 2-[[6-[(3r)-3-amino-1-piperidinil ]-3,4-dihidro-3-metil-2,4-dioxo-1(2h)-pirimidinil]metil]-4-fluoro benzonitrilo. |
| US8093236B2 (en) | 2007-03-13 | 2012-01-10 | Takeda Pharmaceuticals Company Limited | Weekly administration of dipeptidyl peptidase inhibitors |
| JPWO2008114857A1 (ja) | 2007-03-22 | 2010-07-08 | 杏林製薬株式会社 | アミノアセチルピロリジンカルボニトリル誘導体の製造方法 |
| PE20090696A1 (es) | 2007-04-20 | 2009-06-20 | Bristol Myers Squibb Co | Formas cristalinas de saxagliptina y procesos para preparar las mismas |
| CA2688721A1 (en) | 2007-05-21 | 2008-11-27 | Phenomix Corporation | Stable pharmaceutical formulation for a dpp-iv inhibitor |
| CA2692758A1 (en) | 2007-07-12 | 2009-01-15 | Phenomix Corporation | A crystalline synthetic intermediate for preparation of a dpp-iv inhibitor and method of purification thereof |
| JO3272B1 (ar) | 2007-07-19 | 2018-09-16 | Takeda Pharmaceuticals Co | مستحضر صلب يشمل ألوجليبتين وميتفورمين هيدروكلوريد |
| TW200938200A (en) | 2007-12-28 | 2009-09-16 | Dainippon Sumitomo Pharma Co | Methyl-substituted piperidine derivative |
| PE20091730A1 (es) | 2008-04-03 | 2009-12-10 | 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" |
| UY32177A (es) * | 2008-10-16 | 2010-05-31 | Boehringer Ingelheim Int | Tratamiento de diabetes en pacientes con control glucémico insuficiente a pesar de la terapia con fármaco, oral o no, antidiabético |
| 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 |
| AP2011005794A0 (en) * | 2009-02-13 | 2011-08-31 | Boehringer Ingelheim Int | Pharmaceutical composition comprising a SGLT2 inhibitor, a DPP-IV inhibitor and optionally a furtherantidiabetic agent and uses thereof. |
-
2010
- 2010-02-12 CN CN201610580276.0A patent/CN106177958A/zh active Pending
- 2010-02-12 BR BRPI1013639A patent/BRPI1013639A2/pt not_active Application Discontinuation
- 2010-02-12 EP EP10704924A patent/EP2395988A2/en active Pending
- 2010-02-12 AU AU2010212823A patent/AU2010212823B2/en active Active
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- 2010-02-12 CA CA2752437A patent/CA2752437C/en active Active
- 2010-02-12 CN CN2010800161446A patent/CN102387795A/zh active Pending
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- 2010-02-12 KR KR1020167034411A patent/KR20160143897A/ko not_active Ceased
- 2010-02-12 MX MX2016013286A patent/MX387264B/es unknown
- 2010-02-12 MX MX2011008416A patent/MX2011008416A/es unknown
-
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- 2011-06-22 IL IL213716A patent/IL213716A0/en unknown
- 2011-08-02 CL CL2011001853A patent/CL2011001853A1/es unknown
-
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- 2014-12-08 JP JP2014248337A patent/JP2015044875A/ja active Pending
- 2014-12-22 US US14/578,552 patent/US20150105318A1/en not_active Abandoned
-
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- 2017-01-12 JP JP2017003403A patent/JP6556767B2/ja active Active
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-
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-
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- 2020-06-26 US US16/912,764 patent/US20200323861A1/en not_active Abandoned
-
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- 2021-12-03 US US17/541,357 patent/US20220088023A1/en active Pending
Patent Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007120936A2 (en) * | 2006-01-06 | 2007-10-25 | Novartis Ag | Use.of vildagliptin for the treatment of diabetes |
| EP1852108A1 (en) * | 2006-05-04 | 2007-11-07 | Boehringer Ingelheim Pharma GmbH & Co.KG | DPP IV inhibitor formulations |
| WO2007128761A2 (de) * | 2006-05-04 | 2007-11-15 | Boehringer Ingelheim International Gmbh | Verwendungen von dpp iv inhibitoren |
| KR20070111099A (ko) * | 2006-05-16 | 2007-11-21 | 영진약품공업주식회사 | 시타글립틴 염산염의 신규 결정형, 이의 제조 방법과 이를포함하는 약학적 조성물 |
| WO2007149797A2 (en) * | 2006-06-19 | 2007-12-27 | Novartis Ag | Use of organic compounds |
| WO2008093878A1 (en) * | 2007-02-01 | 2008-08-07 | Takeda Pharmaceutical Company Limited | Tablet preparation without causing a tableting trouble |
| CN101234105A (zh) * | 2008-01-09 | 2008-08-06 | 北京润德康医药技术有限公司 | 一种含有二甲双胍和维格列汀的药用组合物及其制备方法 |
Non-Patent Citations (2)
| Title |
|---|
| ROSENSTOCK J, ET AL: "Efficacy and tolerability of initial combination therapy with vildagliptin and pioglitazone compared with component monotherapy in patients with type 2 diabetes.", DIABETES, OBESITY AND METABOLISM, BLACKWELL SCIENCE, vol. 9, no. 2, 1 March 2007 (2007-03-01), pages 175 - 185, XP002541033, ISSN: 1462-8902, DOI: 10.1111/j.1463-1326.2006.00698.x * |
| THOMAS LEO; ECKHARDT MATTHIAS; LANGKOPF ELKE; TADAYYON MOH; HIMMELSBACH FRANK; MARK MICHAEL: "(R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1(4-methyl-quina zolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione (BI 1356), a novel xanthine-based dipeptidyl peptidase 4 inhibitor, has a superior potency and longer duration of action compared with other dipeptidyl peptidase-4 inhibitors", JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, AMERICAN SOCIETY FOR PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, US, vol. 325, no. 1, 1 April 2008 (2008-04-01), US, pages 175 - 182, XP009105508, ISSN: 0022-3565, DOI: 10.1124/jpet.107.135723 * |
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| CN106177958A (zh) | 2016-12-07 |
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| NZ619520A (en) | 2015-06-26 |
| KR20110115582A (ko) | 2011-10-21 |
| US20150105318A1 (en) | 2015-04-16 |
| JP2015044875A (ja) | 2015-03-12 |
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