KR102106310B1 - 벤질벤젠 소듐­의존성 글루코스 공동수송체 2 (sglt2) 억제제의 제조 방법 - Google Patents

벤질벤젠 소듐­의존성 글루코스 공동수송체 2 (sglt2) 억제제의 제조 방법 Download PDF

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KR102106310B1
KR102106310B1 KR1020147031540A KR20147031540A KR102106310B1 KR 102106310 B1 KR102106310 B1 KR 102106310B1 KR 1020147031540 A KR1020147031540 A KR 1020147031540A KR 20147031540 A KR20147031540 A KR 20147031540A KR 102106310 B1 KR102106310 B1 KR 102106310B1
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alkoxy
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바이후아 수
빈후아 엘브이
게 수
브라이언 시드
자크스 로베지
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테라코스 서브, 엘엘씨
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KR1020147031540A 2012-04-10 2013-03-14 벤질벤젠 소듐­의존성 글루코스 공동수송체 2 (sglt2) 억제제의 제조 방법 Expired - Fee Related KR102106310B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
PCT/CN2012/073697 WO2013152476A1 (en) 2012-04-10 2012-04-10 Process for the preparation of benzylbenzene sglt2 inhibitors
CNPCT/CN2012/073697 2012-04-10
PCT/CN2013/072642 WO2013152654A1 (en) 2012-04-10 2013-03-14 Process for preparation of benzylbenzene sodium-dependent glucose cotransporter 2 (sglt2) inhibitors

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Publication Number Publication Date
KR20150001811A KR20150001811A (ko) 2015-01-06
KR102106310B1 true KR102106310B1 (ko) 2020-05-04

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US (2) US9193751B2 (https=)
EP (1) EP2836500A4 (https=)
JP (1) JP6208745B2 (https=)
KR (1) KR102106310B1 (https=)
AR (1) AR090618A1 (https=)
AU (1) AU2013247304B2 (https=)
BR (1) BR112014025105B1 (https=)
CA (1) CA2867057C (https=)
HK (1) HK1207084A1 (https=)
IL (1) IL234800B (https=)
MX (1) MX353307B (https=)
NZ (1) NZ630408A (https=)
RU (1) RU2625795C2 (https=)
SG (1) SG11201406434PA (https=)
TW (1) TWI597289B (https=)
WO (2) WO2013152476A1 (https=)
ZA (1) ZA201406899B (https=)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013152476A1 (en) 2012-04-10 2013-10-17 Theracos, Inc. Process for the preparation of benzylbenzene sglt2 inhibitors
CN105611920B (zh) 2013-10-12 2021-07-16 泰拉科斯萨普有限责任公司 羟基-二苯甲烷衍生物的制备
US9902751B2 (en) 2013-12-30 2018-02-27 Mylan Laboratories Limited Process for the preparation of empagliflozin
CN104529970A (zh) * 2015-01-08 2015-04-22 江苏联环药业股份有限公司 制备达格列净的方法
CN104478671B (zh) * 2015-01-15 2016-03-09 佛山市赛维斯医药科技有限公司 一类双烷氧苯基丙二醇衍生物和用途
CN104478674B (zh) * 2015-01-15 2016-03-09 佛山市赛维斯医药科技有限公司 一类烷氧苯基丙二醇衍生物和用途
CN104478675B (zh) * 2015-01-15 2016-01-06 佛山市赛维斯医药科技有限公司 一类含烷氧苯基和三氟甲苯基丙二醇结构的衍生物和用途
EP3256482B1 (en) 2015-02-09 2019-11-27 Indoco Remedies Limited Process for the preparation of sglt inhibitor compounds
CZ2015729A3 (cs) * 2015-10-13 2017-04-26 Zentiva, K.S. Příprava intermediátů pro syntézu Canagliflozinu a Dapagliflozinu
KR101770302B1 (ko) * 2016-06-28 2017-08-22 주식회사 녹십자 다이페닐메탄 유도체의 제조방법
CN107641139A (zh) * 2016-07-22 2018-01-30 江苏豪森药业集团有限公司 达格列净中间体的晶型及其制备方法
WO2018142422A1 (en) * 2017-02-02 2018-08-09 Indoco Remedies Limited Process for the preparation of dapagliflozin
US11312740B2 (en) 2017-05-09 2022-04-26 Piramal Pharma Limited Process for the preparation of SGLT2 inhibitors and intermediates thereof
EP3784231A4 (en) * 2018-04-25 2022-05-11 Theracos Sub, LLC Methods of treating hypertension
MX2022012955A (es) 2020-04-14 2023-02-23 Flagship Pioneering Innovations Vi Llc Composiciones de trem y usos de las mismas.
WO2022073151A1 (en) 2020-10-05 2022-04-14 Theracos Sub, Llc Pharmaceutical formulations
CN114570303A (zh) * 2022-03-02 2022-06-03 南京市计量监督检测院 微通道反应器及基于反应器制备达格列净中间体的方法
WO2025056984A1 (en) * 2023-09-12 2025-03-20 Vijayasri Organics Private Limited A novel process for the preparation of bexagliflozin a sglt2 inhibitor and its intermediates thereof

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010519273A (ja) 2007-02-21 2010-06-03 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 四置換グルコピラノシル化ベンゼン誘導体、このような化合物を含む薬物、それらの使用及びそれらの製造方法
WO2011039108A2 (en) * 2009-09-30 2011-04-07 Boehringer Ingelheim International Gmbh Processes for preparing of glucopyranosyl-substituted benzyl-benzene derivatives
KR101107425B1 (ko) * 2007-08-23 2012-01-19 테라코스, 인코포레이티드 벤질벤젠 유도체 및 사용 방법

Family Cites Families (85)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1020944C (zh) 1990-01-30 1993-05-26 阿图尔-费希尔股份公司费希尔厂 紧固件
WO1994011030A1 (en) 1992-11-13 1994-05-26 The Ohio State University Research Foundation C-glycoside analogues of n-(4-hydroxyphenyl)retinamide-o-glucuronide
AU6024998A (en) 1997-01-15 1998-08-07 Glycomed Incorporated Aryl c-glycoside compounds and sulfated esters thereof
US6069238A (en) 1998-09-30 2000-05-30 Eli Lilly And Company Spirocyclic C-glycosides
US7407978B2 (en) 1999-04-06 2008-08-05 Theracos, Inc. Heterocyclic analogs of diphenylethylene compounds
US6515117B2 (en) 1999-10-12 2003-02-04 Bristol-Myers Squibb Company C-aryl glucoside SGLT2 inhibitors and method
PH12000002657B1 (en) 1999-10-12 2006-02-21 Bristol Myers Squibb Co C-aryl glucoside SGLT2 inhibitors
US6555519B2 (en) 2000-03-30 2003-04-29 Bristol-Myers Squibb Company O-glucosylated benzamide SGLT2 inhibitors and method
US6683056B2 (en) 2000-03-30 2004-01-27 Bristol-Myers Squibb Company O-aryl glucoside SGLT2 inhibitors and method
EP1340749A4 (en) 2000-11-17 2007-09-05 Takeda Pharmaceutical ISOXAZOLE DERIVATIVES
TWI255817B (en) 2001-02-14 2006-06-01 Kissei Pharmaceutical Glucopyranosyloxybenzylbenzene derivatives and medicinal use thereof
US6936590B2 (en) 2001-03-13 2005-08-30 Bristol Myers Squibb Company C-aryl glucoside SGLT2 inhibitors and method
AU2002254567B2 (en) 2001-04-11 2007-10-11 Bristol-Myers Squibb Company Amino acid complexes of C-aryl glucosides for treatment of diabetes and method
WO2003020737A1 (en) 2001-09-05 2003-03-13 Bristol-Myers Squibb Company O-pyrazole glucoside sglt2 inhibitors and method of use
MXPA04009229A (es) 2002-03-22 2004-11-26 Kissei Pharmaceutical Cristales derivados de glucopiranosiloxibencil benceno.
TWI254635B (en) 2002-08-05 2006-05-11 Yamanouchi Pharma Co Ltd Azulene derivative and salt thereof
RU2356906C2 (ru) 2002-08-08 2009-05-27 Киссеи Фармасьютикал Ко., Лтд. Производные пиразола, лекарственные композиции, содержащие эти производные, их применение в медицине и промежуточные соединения для их получения
RU2322449C2 (ru) 2002-08-09 2008-04-20 Тайсо Фармасьютикал Ко., Лтд. ПРОИЗВОДНЫЕ АРИЛ 5-ТИО-β-D-ГЛЮКОПИРАНОЗИДА И ТЕРАПЕВТИЧЕСКИЕ СРЕДСТВА ПРИ ДИАБЕТЕ, СОДЕРЖАЩИЕ ИХ
DE10258008B4 (de) 2002-12-12 2006-02-02 Sanofi-Aventis Deutschland Gmbh Heterocyclische Fluorglycosidderivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zur Herstellung dieser Arzneimittel
DE10258007B4 (de) 2002-12-12 2006-02-09 Sanofi-Aventis Deutschland Gmbh Aromatische Fluorglycosidderivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zur Herstellung dieser Arzneimittel
JP2006516257A (ja) 2003-01-03 2006-06-29 ブリストル−マイヤーズ スクイブ カンパニー C−アリールグルコシドsglt2阻害剤の製造法
ES2363941T3 (es) 2003-03-14 2011-08-19 Astellas Pharma Inc. Derivados de c-glucósido para el tratamiento de diabetes.
JP2004300102A (ja) 2003-03-31 2004-10-28 Kissei Pharmaceut Co Ltd 縮合複素環誘導体、それを含有する医薬組成物およびその医薬用途
ES2531660T3 (es) 2003-08-01 2015-03-18 Mitsubishi Tanabe Pharma Corporation Compuestos novedosos que tienen actividad inhibidora frente a transportador de glucosa dependiente de sodio
WO2005012242A2 (en) 2003-08-01 2005-02-10 Janssen Pharmaceutica Nv Substituted benzimidazole-, benztriazole-, and benzimidazolone-o-glucosides
EP1679965A4 (en) 2003-08-01 2009-05-27 Janssen Pharmaceutica Nv SUBSTITUTED ANELLIERED HETEROCYCLIC C-GLYCOSIDES
EP1660509B1 (de) 2003-08-26 2009-02-04 Boehringer Ingelheim International GmbH Glucopyranosyloxy-pyrazole, diese verbindungen enthaltende arzneimittel, deren verwendung und verfahren zu ihrer herstellung
US7375090B2 (en) 2003-08-26 2008-05-20 Boehringer Ingelheim International Gmbh Glucopyranosyloxy-pyrazoles, pharmaceutical compositions containing these compounds, the use thereof and processed for the preparation thereof
US7371732B2 (en) 2003-12-22 2008-05-13 Boehringer Ingelheim International Gmbh Glucopyranosyloxy-substituted aromatic compounds, medicaments containing such compounds, their use and process for their manufacture
DE10361133A1 (de) 2003-12-22 2005-07-21 Boehringer Ingelheim Pharma Gmbh & Co. Kg Glucopyranosyloxy-substituierte Aromaten, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
US20050142312A1 (en) 2003-12-29 2005-06-30 Unilever Home & Personal Care Usa Bottle
BRPI0508259A (pt) 2004-03-04 2007-07-31 Kissei Pharmaceutical derivado heterocìclico fundido, composição medicinal contendo o mesmo, e uso medicinal do mesmo
DE102004012676A1 (de) 2004-03-16 2005-10-06 Boehringer Ingelheim Pharma Gmbh & Co. Kg Glucopyranosyl-substituierte Phenyle, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
CN103030617A (zh) 2004-03-16 2013-04-10 贝林格尔.英格海姆国际有限公司 吡喃葡萄糖基取代的苯基衍生物、含该化合物的药物、其用途及其制造方法
EP1731524A4 (en) 2004-03-31 2009-05-20 Kissei Pharmaceutical PHENOLE DERIVATIVE, MEDICINAL COMPOSITION CONTAINING THE DERIVATIVE, AND ITS MEDICINAL USE
EP1582523A1 (en) 2004-04-02 2005-10-05 Ludwig-Maximilians-Universität München Method of preparing organomagnesium compounds
US7393836B2 (en) 2004-07-06 2008-07-01 Boehringer Ingelheim International Gmbh D-xylopyranosyl-substituted phenyl derivatives, medicaments containing such compounds, their use and process for their manufacture
DE102004034690A1 (de) 2004-07-17 2006-02-02 Boehringer Ingelheim Pharma Gmbh & Co. Kg Methyliden-D-xylopyranosyl-und Oxo-D-xylopyranosyl-substituierte Phenyle, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
TW200606129A (en) 2004-07-26 2006-02-16 Chugai Pharmaceutical Co Ltd Novel cyclohexane derivative, its prodrug, its salt and diabetic therapeutic agent containing the same
WO2006010557A1 (de) 2004-07-27 2006-02-02 Boehringer Ingelheim International Gmbh D-glucopyranosyl-phenyl-substituierte cyclen, diese verbindungen enthaltende arzneimittel, deren verwendung und verfahren zu ihrer herstellung
WO2006018150A1 (de) 2004-08-11 2006-02-23 Boehringer Ingelheim International Gmbh D-xylopyranosyl-phenyl-substituierte cyclen, diese verbindungen enthaltende arzneimittel, deren verwendung und verfahren zu ihrer herstellung
AR051446A1 (es) 2004-09-23 2007-01-17 Bristol Myers Squibb Co Glucosidos de c-arilo como inhibidores selectivos de transportadores de glucosa (sglt2)
WO2006035796A1 (ja) 2004-09-29 2006-04-06 Kissei Pharmaceutical Co., Ltd. 1-(β-D-グリコピラノシル)-3-置換含窒素ヘテロ環化合物、それを含有する医薬組成物及びその医薬用途
DE102004048388A1 (de) 2004-10-01 2006-04-06 Boehringer Ingelheim Pharma Gmbh & Co. Kg D-Pyranosyl-substituierte Phenyle, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
DE602005009745D1 (de) 2004-12-16 2008-10-23 Boehringer Ingelheim Pharma Glucopyranosyl-substituierte benzen-derivate, medikamente mit solchen verbindungen, ihre verwendung und herstellungsverfahren dafür
TW200637839A (en) * 2005-01-07 2006-11-01 Taisho Pharmaceutical Co Ltd 1-thio-d-glucitol derivatives
TW200637869A (en) 2005-01-28 2006-11-01 Chugai Pharmaceutical Co Ltd The spiroketal derivatives and the use as therapeutical agent for diabetes of the same
JP5264183B2 (ja) 2005-02-23 2013-08-14 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 グルコピラノシル置換((ヘテロ)アリールエチニル−ベンジル)−ベンゼン誘導体及びナトリウム依存性グルコース共輸送体2(sglt2)インヒビターとしてのそれらの使用
AR053710A1 (es) 2005-04-11 2007-05-16 Xenon Pharmaceuticals Inc Compuestos espiroheterociclicos y sus usos como agentes terapeuticos
ATE453656T1 (de) 2005-04-15 2010-01-15 Boehringer Ingelheim Int Glucopyranosyl-substituierte (heteroaryloxy- benzyl)-benzen-derivate als sglt-inhibitoren
UA91546C2 (uk) 2005-05-03 2010-08-10 Бьорінгер Інгельхайм Інтернаціональ Гмбх КРИСТАЛІЧНА ФОРМА 1-ХЛОР-4-(β-D-ГЛЮКОПІРАНОЗ-1-ИЛ)-2-[4-((S)-ТЕТРАГІДРОФУРАН-3-ІЛОКСИ)-БЕНЗИЛ]-БЕНЗОЛУ, СПОСІБ ЇЇ ОДЕРЖАННЯ ТА ЇЇ ЗАСТОСУВАННЯ ПРИ ПРИГОТУВАННІ ЛІКАРСЬКИХ ЗАСОБІВ
US7723309B2 (en) 2005-05-03 2010-05-25 Boehringer Ingelheim International Gmbh Crystalline forms of 1-chloro-4-(β-D-glucopyranos-1-yl)-2-[4-((R)-tetrahydrofuran-3-yloxy)-benzyl]-benzene, a method for its preparation and the use thereof for preparing medicaments
TW200726746A (en) 2005-05-06 2007-07-16 Microbia Inc Processes for production of 4-biphenylylazetidin-2-ones
US7772191B2 (en) 2005-05-10 2010-08-10 Boehringer Ingelheim International Gmbh Processes for preparing of glucopyranosyl-substituted benzyl-benzene derivatives and intermediates therein
WO2007000445A1 (en) 2005-06-29 2007-01-04 Boehringer Ingelheim International Gmbh Glucopyranosyl-substituted benzyl-benzene derivatives, medicaments containing such compounds, their use and process for their manufacture
TW200726755A (en) 2005-07-07 2007-07-16 Astellas Pharma Inc A crystalline choline salt of an azulene derivative
AR054871A1 (es) 2005-07-27 2007-07-25 Boehringer Ingelheim Int Derivados de (hetero)cicloalquiletinil-bencil)-benceno sustituidos con glucopiranosilo, medicamentos que contienen dichos compuestos, sus uso y proceso para su fabricacion
GB0516156D0 (en) 2005-08-05 2005-09-14 Eisai London Res Lab Ltd JNK inhibitors
WO2007025943A2 (en) 2005-08-30 2007-03-08 Boehringer Ingelheim International Gmbh Glucopyranosyl-substituted benzyl-benzene derivatives, medicaments containing such compounds, their use and process for their manufacture
AU2006289093A1 (en) 2005-09-08 2007-03-15 Boehringer Ingelheim International Gmbh Crystalline forms of 1-chloro-4-(beta-D-glucopyranos-1-yl)-2-(4-ethynyl-benzyl)-benzene, methods for its preparation and the use thereof for preparing medicaments
TWI370818B (en) 2006-04-05 2012-08-21 Astellas Pharma Inc Cocrystal of c-glycoside derivative and l-proline
EP2076503B1 (en) 2006-05-19 2013-07-17 Taisho Pharmaceutical Co., Ltd C-phenyl glycitol compound for the treatment of diabetes
US7803778B2 (en) 2006-05-23 2010-09-28 Theracos, Inc. Glucose transport inhibitors and methods of use
US7919598B2 (en) 2006-06-28 2011-04-05 Bristol-Myers Squibb Company Crystal structures of SGLT2 inhibitors and processes for preparing same
TWI403516B (zh) 2006-07-27 2013-08-01 Chugai Pharmaceutical Co Ltd To replace spirocyclic alcohol derivatives, and its use as a therapeutic agent for diabetes
US20080027014A1 (en) 2006-07-28 2008-01-31 Tanabe Seiyaku Co., Ltd. Novel SGLT inhibitors
WO2008034859A1 (en) 2006-09-21 2008-03-27 Boehringer Ingelheim International Gmbh Glucopyranosyl-substituted difluorobenzyl-benzene derivatives, medicaments containing such compounds, their use and process for their manufacture
WO2008049923A1 (en) 2006-10-27 2008-05-02 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
UY30730A1 (es) 2006-12-04 2008-07-03 Mitsubishi Tanabe Pharma Corp Forma cristalina del hemihidrato de 1-(b (beta)-d-glucopiranosil) -4-metil-3-[5-(4-fluorofenil) -2-tienilmetil]benceno
UY30801A1 (es) 2006-12-18 2008-07-03 Smithkline Beecham Corp Compuestos calciliticos
JP5583003B2 (ja) 2007-04-02 2014-09-03 セラコス・インコーポレイテッド ベンジルグルコシド誘導体およびその用途
US20080287529A1 (en) 2007-05-18 2008-11-20 Bristol-Myers Squibb Company Crystal structures of sglt2 inhibitors and processes for preparing same
PT2183263E (pt) 2007-07-26 2012-01-11 Lexicon Pharmaceuticals Inc Processos e compostos úteis na preparação de inibidores do co-transportador 2 de glucose e sódio
RS56990B1 (sr) 2007-09-10 2018-05-31 Janssen Pharmaceutica Nv Postupak za dobijanje jedinjenja koja su korisna kao inhibitori sglt
CN101250330B (zh) 2008-03-25 2011-05-11 上海拓引数码技术有限公司 可用于dvd-r的光记录染料及其记录层的制备方法
AU2009270936B2 (en) 2008-07-15 2014-12-18 Theracos, Inc. Deuterated benzylbenzene derivatives and methods of use
CN103910702A (zh) * 2008-08-22 2014-07-09 泰拉科斯有限公司 制备sglt2抑制剂的方法
AU2009286380B2 (en) 2008-08-28 2011-09-15 Pfizer Inc. Dioxa-bicyclo[3.2.1.]octane-2,3,4-triol derivatives
US9056850B2 (en) 2008-10-17 2015-06-16 Janssen Pharmaceutica N.V. Process for the preparation of compounds useful as inhibitors of SGLT
JP5365304B2 (ja) 2009-03-30 2013-12-11 Jfeスチール株式会社 電磁鋼板の単板磁気特性試験用試験器および磁気特性測定方法
US8541380B2 (en) 2009-06-19 2013-09-24 Green Cross Corporation C-aryl glucoside SGLT2 inhibitors and pharmaceutical compositions comprising same
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
HUE031375T2 (en) 2009-10-14 2017-07-28 Janssen Pharmaceutica Nv Process for the preparation of compounds useful as inhibitors of sglt2
KR101466838B1 (ko) 2010-06-18 2014-11-28 주식회사 녹십자 Sglt2 억제제로서의 티아졸 유도체 및 이를 포함하는 약학 조성물
WO2013152476A1 (en) 2012-04-10 2013-10-17 Theracos, Inc. Process for the preparation of benzylbenzene sglt2 inhibitors

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010519273A (ja) 2007-02-21 2010-06-03 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 四置換グルコピラノシル化ベンゼン誘導体、このような化合物を含む薬物、それらの使用及びそれらの製造方法
KR101107425B1 (ko) * 2007-08-23 2012-01-19 테라코스, 인코포레이티드 벤질벤젠 유도체 및 사용 방법
WO2011039108A2 (en) * 2009-09-30 2011-04-07 Boehringer Ingelheim International Gmbh Processes for preparing of glucopyranosyl-substituted benzyl-benzene derivatives

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