JP2014210821A - 多形体 - Google Patents
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- C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
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- C07D473/06—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
- A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
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- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
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- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Abstract
Description
該混合物を>40℃の温度まで加熱することによって得ることのできる純粋な高温形体(多形体A)は、206±3℃で融解する。粉末X線図(図3参照)では、この形体は以下のd値:11.49Å、7.60Å、7.15Å、3.86Å、3.54Å及び3.47Å(表1及び2も参照)で特徴的な反射を示す。
低温形体(多形体B)は、<10℃の温度まで冷却することによって得られる。粉末X線図(図4参照)では、この形体は以下のd値:11.25Å、9.32Å、7.46Å、6.98Å及び3.77Å(表3及び4も参照)で特徴的な反射を示す。
別の多形体(多形体C)は、粉末X線図(図5参照)において以下のd値:12.90Å、11.10Å、6.44Å、3.93Å及び3.74Å(図5も参照)で特徴的な反射を示す。
別の多形体(多形体D)は150±3℃で融解する。この多形体は、多形体Cを30-100℃の温度まで加熱し、この温度で乾燥させると得られる。
最後に、175±3℃の温度で融解する多形体Eも存在する。無水多形体Eは、多形体Dが融解すると形成される。さらに加熱すると、多形体Eは該融解物から晶出する。
以下の実施例は、本発明をより詳細に説明することを目的とする。
粗い1-[(4-メチル-キナゾリン-2-イル)メチル]-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-アミノ-ピペリジン-1-イル)-キサンチンを5倍量の無水エタノールでリフラックスし、この熱い溶液を活性炭に通して濾過した。濾過物を20℃まで冷却して結晶化を開始した後、該溶液をtert.-ブチルメチルエーテルで2倍の容積まで希釈した。続いて、この懸濁液を2℃まで冷却し、2時間攪拌し、吸引濾過し、及び真空乾燥機において45℃で乾燥させた。
多形体Aは206±3℃で融解する。該DSC図では、別のわずかな吸熱信号が約25℃で見ることができる。これは、該2種のエナンチオトロピー結晶修飾A及びBの間の完全に可逆な固体-固体の相転移である。該形体Aはこの変形温度よりも高温で熱力学的に安定な修飾であり、形態Bはこの変形温度よりも低温で熱力学的に安定な修飾である。
図2は周期的なDSC図を示しており、-40℃〜120℃の相転移及びその逆が計3回起こっている。加熱中、相転移は吸熱信号として観察され、従って冷却中は発熱信号として観察される。第一の加熱サイクル中に、相転移は吸熱の二重信号か又は非常にブロードな信号としても観察され、全ての他のサイクルにおいて該信号は非常に鋭い吸熱又は発熱信号として起こり、加熱又は冷却が起こるか否かに依存する
多形体Bは、実施例1からの形体Aを<10℃の温度まで冷却することによって得られる。
粗い1-[(4-メチル-キナゾリン-2-イル)メチル]-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-アミノ-ピペリジン-1-イル)-キサンチン(26kg)を、157Lのメタノールでリフラックスし、1.3kgの活性炭と混合し、30分攪拌した後に該混合物を濾過して26Lのメタノールで漱いだ。122Lのメタノールを濾過物から蒸留し、続いて残渣を45-55℃まで冷却した。52Lのtert.-ブチルメチルエーテルを30分かけて残渣に加えた。続いて、該混合物を45-55℃でさらに60分間攪拌した。結晶化がこの時間内に起こった。さらに78Lのtert. ブチルメチルエーテルを30分かけて該懸濁液に加え、続いて45-55℃でさらに60分間再び攪拌した。
それを4倍の体積に希釈した。該懸濁液を15-25℃まで穏やかに冷却し、この温度で終夜攪拌した。該懸濁液を0-5℃まで冷却した後、結晶を吸引濾過し、2バッチのtert.-ブチルメチルエーテルで洗浄し、及び70℃の真空乾燥機で乾燥させた。
多形体Cは、実施例3からの多形体Cを30-100℃の温度まで加熱し、この温度で乾燥して得られる。
実施例5 多形体Eの結晶化
無水多形体Eは、多形体Dが融解すると得られる。さらなる加熱により、多形体Eが該融解物から晶出する。
100℃の温度で保持されたサンプルに関する粉末X線図は、出発物質からの異なるX線反射を示しており、形体Cがおよそ半水化物又は一水和物の領域にある化学量論比を有する水和物相であることを示唆している。温度制御されたサンプルは別の無水修飾Dであり、無水条件下でのみ安定である。該D形体は約150℃で融解する。別の無水結晶修飾Eは該融解物から結晶化し、さらに加熱されると約175℃で融解する。最後に、形体Aは形体Eの融解物から結晶化する。形体Eは高温でのみ起こる準安定な結晶修飾でもある。
〔1〕206±3℃で融解することを特徴とする、化合物1-[(4-メチル-キナゾリン-2-イル)メチル]-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-アミノ-ピペリジン-1-イル)-キサンチンの無水多形体A。
〔2〕粉末X線図において、以下のd値:11.49Å、7.60Å、7.15Å、3.86Å、3.54Å及び3.47Åで特徴的な反射を有する、前記〔1〕記載の多形体A。
〔3〕10-40℃の温度で前記〔1〕記載の多形体Aに可逆的に変形することを特徴とする、化合物1-[(4-メチル-キナゾリン-2-イル)メチル]-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-アミノ-ピペリジン-1-イル)-キサンチンの無水多形体B。
〔4〕粉末X線図において、以下のd値:11.25Å、9.32Å、7.46Å、6.98Å及び3.77Åで特徴的な反射を有する、前記〔3〕記載の多形体B。
〔5〕30-100℃の温度で水を失い、且つDSC図において約150及び175℃でさらなる熱効果を示すことを特徴とする、化合物1-[(4-メチル-キナゾリン-2-イル)メチル]-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-アミノ-ピペリジン-1-イル)-キサンチンの多形体C。
〔5〕’30-100℃の温度で水を失い、且つDSC図において約150〜175℃でさらなる熱効果を示すことを特徴とする、化合物1-[(4-メチル-キナゾリン-2-イル)メチル]-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-アミノ-ピペリジン-1-イル)-キサンチンの多形体C。
〔6〕粉末X線図において、以下のd値:12.90Å、11.10Å、6.44Å、3.93Å及び3.74Åで特徴的な反射を有する、前記〔5〕記載の多形体C。
〔7〕150±3℃で融解することを特徴とする、化合物1-[(4-メチル-キナゾリン-2-イル)メチル]-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-アミノ-ピペリジン-1-イル)-キサンチンの無水多形体D。
〔8〕175±3℃で融解することを特徴とする、化合物1-[(4-メチル-キナゾリン-2-イル)メチル]-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-アミノ-ピペリジン-1-イル)-キサンチンの無水多形体E。
〔9〕前記〔5〕記載の多形体Cを調製する方法であって、(a)1-[(4-メチル-キナゾリン-2-イル)メチル]-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-アミノ-ピペリジン-1-イル)-キサンチンをメタノール中で還流する工程、(b)該メタノール性溶液を40-60℃の温度まで冷却する工程、(c)tert.-ブチルメチルエーテルなどの溶媒を加える工程、(d)得られた懸濁液をまずは15-25℃まで、続いて0-5℃まで冷却する工程、(e)結晶を吸引濾過する工程、及び(f)70℃の温度の真空下で乾燥する工程、を特徴とする方法。
〔10〕工程(a)の後に前記熱い溶液を濾過する、前記〔9〕記載の方法。
〔11〕I型及びII型糖尿病、前糖尿病又は減少した糖耐性、さらに関節リウマチ、肥満、又はカルシトニン誘導骨粗鬆症を有する患者、並びに同種移植が行われた患者の治療のための医薬組成物を調製するための、化合物1-[(4-メチル-キナゾリン-2-イル)メチル]-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-アミノ-ピペリジン-1-イル)-キサンチンの多形体A、B、又はCの1種の使用。
〔12〕化合物1-[(4-メチル-キナゾリン-2-イル)メチル]-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-アミノ-ピペリジン-1-イル)-キサンチンに加えて1種以上の不活性キャリア及び/又は希釈剤を含有する薬剤であって、少なくとも0.1%〜0.5%の多形体A、B、又はCの1種を含有することを特徴とする、薬剤。
Claims (12)
- 206±3℃で融解することを特徴とする、化合物1-[(4-メチル-キナゾリン-2-イル)メチル]-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-アミノ-ピペリジン-1-イル)-キサンチンの無水多形体A。
- 粉末X線図において、以下のd値:11.49Å、7.60Å、7.15Å、3.86Å、3.54Å及び3.47Åで特徴的な反射を有する、請求項1記載の多形体A。
- 10-40℃の温度で請求項1記載の多形体Aに可逆的に変形することを特徴とする、化合物1-[(4-メチル-キナゾリン-2-イル)メチル]-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-アミノ-ピペリジン-1-イル)-キサンチンの無水多形体B。
- 粉末X線図において、以下のd値:11.25Å、9.32Å、7.46Å、6.98Å及び3.77Åで特徴的な反射を有する、請求項3記載の多形体B。
- 30-100℃の温度で水を失い、且つDSC図において約150及び175℃でさらなる熱効果を示すことを特徴とする、化合物1-[(4-メチル-キナゾリン-2-イル)メチル]-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-アミノ-ピペリジン-1-イル)-キサンチンの多形体C。
- 粉末X線図において、以下のd値:12.90Å、11.10Å、6.44Å、3.93Å及び3.74Åで特徴的な反射を有する、請求項5記載の多形体C。
- 150±3℃で融解することを特徴とする、化合物1-[(4-メチル-キナゾリン-2-イル)メチル]-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-アミノ-ピペリジン-1-イル)-キサンチンの無水多形体D。
- 175±3℃で融解することを特徴とする、化合物1-[(4-メチル-キナゾリン-2-イル)メチル]-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-アミノ-ピペリジン-1-イル)-キサンチンの無水多形体E。
- 請求項5記載の多形体Cを調製する方法であって、(a)1-[(4-メチル-キナゾリン-2-イル)メチル]-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-アミノ-ピペリジン-1-イル)-キサンチンをメタノール中で還流する工程、(b)該メタノール性溶液を40-60℃の温度まで冷却する工程、(c)tert.-ブチルメチルエーテルなどの溶媒を加える工程、(d)得られた懸濁液をまずは15-25℃まで、続いて0-5℃まで冷却する工程、(e)結晶を吸引濾過する工程、及び(f)70℃の温度の真空下で乾燥する工程、を特徴とする方法。
- 工程(a)の後に前記熱い溶液を濾過する、請求項9記載の方法。
- I型及びII型糖尿病、前糖尿病又は減少した糖耐性、さらに関節リウマチ、肥満、又はカルシトニン誘導骨粗鬆症を有する患者、並びに同種移植が行われた患者の治療のための医薬組成物を調製するための、化合物1-[(4-メチル-キナゾリン-2-イル)メチル]-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-アミノ-ピペリジン-1-イル)-キサンチンの多形体A、B、又はCの1種の使用。
- 化合物1-[(4-メチル-キナゾリン-2-イル)メチル]-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-アミノ-ピペリジン-1-イル)-キサンチンに加えて1種以上の不活性キャリア及び/又は希釈剤を含有する薬剤であって、少なくとも0.1%〜0.5%の多形体A、B、又はCの1種を含有することを特徴とする、薬剤。
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Families Citing this family (105)
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 |
US7495005B2 (en) | 2002-08-22 | 2009-02-24 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Xanthine derivatives, their preparation and their use in pharmaceutical compositions |
US7482337B2 (en) | 2002-11-08 | 2009-01-27 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions |
DE10254304A1 (de) | 2002-11-21 | 2004-06-03 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Xanthinderivate, deren Herstellung und deren Verwendung als Arzneimittel |
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 |
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 |
US7179809B2 (en) * | 2004-04-10 | 2007-02-20 | Boehringer Ingelheim International Gmbh | 2-Amino-imidazo[4,5-d]pyridazin-4-ones, their preparation and their use as pharmaceutical compositions |
US7439370B2 (en) | 2004-05-10 | 2008-10-21 | Boehringer Ingelheim International Gmbh | Imidazole derivatives, their preparation and their use as intermediates for the preparation of pharmaceutical compositions and pesticides |
DE102004030502A1 (de) | 2004-06-24 | 2006-01-12 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Imidazole und Triazole, deren Herstellung und Verwendung als Arzneimittel |
US20060035903A1 (en) * | 2004-08-14 | 2006-02-16 | Boehringer Ingelheim International Gmbh | Storage stable perfusion solution for dihydropteridinones |
US20060058311A1 (en) | 2004-08-14 | 2006-03-16 | Boehringer Ingelheim International Gmbh | Combinations for the treatment of diseases involving cell proliferation |
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 |
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 |
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 |
US7439358B2 (en) | 2006-02-08 | 2008-10-21 | Boehringer Ingelheim International Gmbh | Specific salt, anhydrous and crystalline form of a dihydropteridione derivative |
PE20080251A1 (es) | 2006-05-04 | 2008-04-25 | Boehringer Ingelheim Int | Usos de inhibidores de dpp iv |
MX2008014024A (es) * | 2006-05-04 | 2008-11-14 | Boehringer Ingelheim Int | Formas poliformas. |
EP1852108A1 (en) | 2006-05-04 | 2007-11-07 | Boehringer Ingelheim Pharma GmbH & Co.KG | DPP IV inhibitor formulations |
WO2008017670A1 (en) | 2006-08-08 | 2008-02-14 | Boehringer Ingelheim International Gmbh | Pyrrolo [3, 2 -d] pyrimidines as dpp-iv inhibitors for the treatment of diabetes mellitus |
EP2025674A1 (de) | 2007-08-15 | 2009-02-18 | sanofi-aventis | Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
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. |
US20110112069A1 (en) * | 2007-08-17 | 2011-05-12 | Boehringer Ingelheim International Gmbh | Purin derivatives for use in the treatment of fab-related diseases |
WO2009097995A1 (de) * | 2008-02-07 | 2009-08-13 | Sanofi-Aventis | Neue phenyl-substituierte imidazolidine, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung |
PE20091730A1 (es) | 2008-04-03 | 2009-12-10 | Boehringer Ingelheim Int | Formulaciones que comprenden un inhibidor de dpp4 |
BRPI0916997A2 (pt) | 2008-08-06 | 2020-12-15 | Boehringer Ingelheim International Gmbh | Inibidor de dpp-4 e seu uso |
UY32030A (es) | 2008-08-06 | 2010-03-26 | Boehringer Ingelheim Int | "tratamiento para diabetes en pacientes inapropiados para terapia con metformina" |
WO2010018217A2 (en) | 2008-08-15 | 2010-02-18 | Boehringer Ingelheim International Gmbh | Organic compounds for wound healing |
US8513264B2 (en) | 2008-09-10 | 2013-08-20 | Boehringer Ingelheim International Gmbh | Combination therapy for the treatment of diabetes and related conditions |
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 |
CN107011345A (zh) * | 2008-12-23 | 2017-08-04 | 勃林格殷格翰国际有限公司 | 有机化合物的盐形式 |
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 |
TWI466672B (zh) | 2009-01-29 | 2015-01-01 | Boehringer Ingelheim Int | 小兒科病人糖尿病之治療 |
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 |
AU2010212867B2 (en) | 2009-02-13 | 2013-05-16 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition comprising a SGLT2 inhibitor, a DPP-IV inhibitor and optionally a further antidiabetic agent and uses thereof |
EA029759B1 (ru) | 2009-02-13 | 2018-05-31 | Бёрингер Ингельхайм Интернациональ Гмбх | Антидиабетические лекарственные средства, содержащие ингибитор dpp-4 (линаглиптин) необязательно в комбинации с другими антидиабетическими средствами |
AR077642A1 (es) | 2009-07-09 | 2011-09-14 | Arena Pharm Inc | Moduladores del metabolismo y el tratamiento de trastornos relacionados con el mismo |
KR101763659B1 (ko) | 2009-10-02 | 2017-08-01 | 베링거 인겔하임 인터내셔날 게엠베하 | Bi―1356 및 메트포르민을 포함하는 약제학적 조성물 |
EP3646859A1 (en) | 2009-11-27 | 2020-05-06 | Boehringer Ingelheim International GmbH | Treatment of genotyped diabetic patients with dpp-iv inhibitors such as linagliptin |
WO2011107494A1 (de) | 2010-03-03 | 2011-09-09 | Sanofi | Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
US20130109703A1 (en) | 2010-03-18 | 2013-05-02 | Boehringer Ingelheim International Gmbh | Combination of a GPR119 Agonist and the DPP-IV Inhibitor Linagliptin for Use in the Treatment of Diabetes and Related Conditions |
CN102918027A (zh) | 2010-04-06 | 2013-02-06 | 艾尼纳制药公司 | Gpr119受体调节剂和对与所述受体有关的障碍的治疗 |
AU2011249722B2 (en) | 2010-05-05 | 2015-09-17 | Boehringer Ingelheim International Gmbh | Combination therapy |
EP2566464A1 (en) | 2010-05-05 | 2013-03-13 | Boehringer Ingelheim International GmbH | Pharmaceutical formulations comprising pioglitazone and linagliptin |
EP2582709B1 (de) | 2010-06-18 | 2018-01-24 | Sanofi | Azolopyridin-3-on-derivate als inhibitoren von lipasen und phospholipasen |
US8530413B2 (en) | 2010-06-21 | 2013-09-10 | Sanofi | Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments |
BR112012032579B1 (pt) | 2010-06-24 | 2021-05-11 | Boehringer Ingelheim International Gmbh | uso de linagliptina e composição farmacêutica compreendendo linagliptina e insulina basal de longa duração |
TW201215388A (en) | 2010-07-05 | 2012-04-16 | Sanofi Sa | (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments |
TW201215387A (en) | 2010-07-05 | 2012-04-16 | Sanofi Aventis | Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament |
TW201221505A (en) | 2010-07-05 | 2012-06-01 | Sanofi Sa | Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament |
AU2011305525B2 (en) | 2010-09-22 | 2016-08-18 | Arena Pharmaceuticals, Inc. | Modulators of the GPR119 receptor and the treatment of disorders related thereto |
US8546566B2 (en) | 2010-10-12 | 2013-10-01 | Boehringer Ingelheim International Gmbh | Process for manufacturing dihydropteridinones and intermediates thereof |
US9034883B2 (en) | 2010-11-15 | 2015-05-19 | Boehringer Ingelheim International Gmbh | Vasoprotective and cardioprotective antidiabetic therapy |
US9358233B2 (en) | 2010-11-29 | 2016-06-07 | Boehringer Ingelheim International Gmbh | Method for treating acute myeloid leukemia |
AR085689A1 (es) | 2011-03-07 | 2013-10-23 | Boehringer Ingelheim Int | Composiciones farmaceuticas de metformina, linagliptina y un inhibidor de sglt-2 |
EP2683699B1 (de) | 2011-03-08 | 2015-06-24 | Sanofi | Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
US8871758B2 (en) | 2011-03-08 | 2014-10-28 | Sanofi | Tetrasubstituted oxathiazine derivatives, method for producing them, their use as medicine and drug containing said derivatives and the use thereof |
US8901114B2 (en) | 2011-03-08 | 2014-12-02 | Sanofi | Oxathiazine derivatives substituted with carbocycles or heterocycles, method for producing same, drugs containing said compounds, and use thereof |
WO2012120054A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
EP2683704B1 (de) | 2011-03-08 | 2014-12-17 | Sanofi | Verzweigte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
US20140018371A1 (en) | 2011-04-01 | 2014-01-16 | Arena Pharmaceuticals, Inc. | Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto |
US20140066369A1 (en) | 2011-04-19 | 2014-03-06 | Arena Pharmaceuticals, Inc. | Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto |
WO2012145604A1 (en) | 2011-04-22 | 2012-10-26 | Arena Pharmaceuticals, Inc. | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
WO2012145603A1 (en) | 2011-04-22 | 2012-10-26 | Arena Pharmaceuticals, Inc. | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
US8785455B2 (en) | 2011-05-10 | 2014-07-22 | Sandoz Ag | Polymorph of linagliptin benzoate |
US9370535B2 (en) | 2011-05-17 | 2016-06-21 | Boehringer Ingelheim International Gmbh | Method for treatment of advanced solid tumors |
WO2012170702A1 (en) | 2011-06-08 | 2012-12-13 | Arena Pharmaceuticals, Inc. | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
HUE043540T2 (hu) | 2011-07-15 | 2019-08-28 | Boehringer Ingelheim Int | Szubsztituált dimer kinazolin-származék, elõállítása, valamint alkalmazása 1-es és 2-es típusú cukorbetegség kezelésére szolgáló gyógyászati készítményekben |
WO2013037390A1 (en) | 2011-09-12 | 2013-03-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
WO2013045413A1 (en) | 2011-09-27 | 2013-04-04 | Sanofi | 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
WO2013055910A1 (en) | 2011-10-12 | 2013-04-18 | Arena Pharmaceuticals, Inc. | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
ITMI20112053A1 (it) * | 2011-11-11 | 2013-05-12 | Dipharma Francis Srl | Forma amorfa di un inibitore enzimatico |
US20130123282A1 (en) | 2011-11-16 | 2013-05-16 | Leonid Metsger | Solid state forms of linagliptin |
US20130172244A1 (en) | 2011-12-29 | 2013-07-04 | Thomas Klein | Subcutaneous therapeutic use of dpp-4 inhibitor |
WO2013128379A2 (en) * | 2012-02-27 | 2013-09-06 | Dr. Reddy's Laboratories Limited | Crystalline polymorphic forms of linagliptin |
US9555001B2 (en) | 2012-03-07 | 2017-01-31 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition and uses thereof |
EP2825539A1 (en) * | 2012-03-12 | 2015-01-21 | Cadila Healthcare Limited | Amorphous form of linagliptin and process for preparation 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 |
EP3685839A1 (en) | 2012-05-14 | 2020-07-29 | Boehringer Ingelheim International GmbH | Linagliptin for use in the treatment of albuminuria and kidney related diseases |
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 |
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 |
EP2854824A1 (en) | 2012-05-25 | 2015-04-08 | Boehringer Ingelheim International GmbH | Use of keratinocytes as a biologically active substance in the treatment of wounds, such as diabetic wounds, optionally in combination with a dpp-4 inhibitor |
WO2014026939A1 (en) | 2012-08-13 | 2014-02-20 | 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 |
WO2014045266A1 (en) | 2012-09-24 | 2014-03-27 | Ulf Eriksson | Treatment of type 2 diabetes and related conditions |
EP2911655A1 (en) | 2012-10-24 | 2015-09-02 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Tpl2 kinase inhibitors for preventing or treating diabetes and for promoting -cell survival |
WO2014074668A1 (en) | 2012-11-08 | 2014-05-15 | Arena Pharmaceuticals, Inc. | Modulators of gpr119 and the treatment of disorders related thereto |
US20150031699A1 (en) | 2013-07-26 | 2015-01-29 | Boehringer Ingelheim International Gmbh | Treatment of myelodysplastic syndrome |
CN104418857A (zh) * | 2013-08-22 | 2015-03-18 | 北京蓝丹医药科技有限公司 | 无定型利格列汀及其制备方法 |
EP3107540A4 (en) * | 2014-02-17 | 2017-08-30 | Hetero Research Foundation | Polymorphs of lomitapide and its salts |
ES2950384T3 (es) | 2014-02-28 | 2023-10-09 | Boehringer Ingelheim Int | Uso médico de un inhibidor de DPP-4 |
US9867831B2 (en) | 2014-10-01 | 2018-01-16 | Boehringer Ingelheim International Gmbh | Combination treatment of acute myeloid leukemia and myelodysplastic syndrome |
CN104496989A (zh) * | 2014-12-26 | 2015-04-08 | 寿光富康制药有限公司 | 一种利格列汀工业化制备工艺 |
ES2805743T3 (es) | 2015-03-24 | 2021-02-15 | Inst Nat Sante Rech Med | Método y composición farmacéutica para uso en el tratamiento de la diabetes |
KR102442536B1 (ko) * | 2015-09-17 | 2022-09-13 | 한미정밀화학주식회사 | 리나글립틴 결정형 및 이의 제조방법 |
US10668073B2 (en) | 2015-10-09 | 2020-06-02 | Hexal Ag | 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 |
EP3156048A1 (en) | 2015-10-13 | 2017-04-19 | Galenicum Health S.L. | Stable pharmaceutical composition of linagliptin in the form of immediate release tablets |
WO2017206689A1 (zh) * | 2016-05-30 | 2017-12-07 | 深圳市塔吉瑞生物医药有限公司 | 一种取代的黄嘌呤及其药物组合物 |
BR112018072401A2 (pt) | 2016-06-10 | 2019-02-19 | Boehringer Ingelheim International Gmbh | combinações de linagliptina e metformina |
CN106543180B (zh) * | 2016-10-28 | 2018-03-30 | 南京正大天晴制药有限公司 | 苯甲酸利格列汀晶型及其制备方法 |
WO2018104263A1 (en) | 2016-12-06 | 2018-06-14 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods of enhancing the potency of incretin-based drugs in subjects in need thereof |
MX2020004050A (es) | 2017-09-27 | 2020-11-06 | Biocon Ltd | Intermediario cristalino de linagliptina y proceso para la preparacion de linagliptina. |
CN109111443A (zh) * | 2018-08-28 | 2019-01-01 | 上海迪赛诺药业股份有限公司 | Dpp-iv抑制剂类降糖药的新晶型及其制备方法 |
CN110305131B (zh) * | 2019-07-03 | 2021-12-31 | 山东百诺医药股份有限公司 | 利格列汀新晶型及其制备方法 |
WO2021250995A1 (ja) * | 2020-06-10 | 2021-12-16 | 有機合成薬品工業株式会社 | 1-[(4-メチル-キナゾリン-2-イル)メチル]-3-メチル-7-(2-ブチン-1-イル)-8-(3-(r)-アミノ-ピペリジン-1-イル)-キサンチンの結晶形態 |
KR20220127965A (ko) | 2021-03-12 | 2022-09-20 | 이니스트에스티 주식회사 | 리나글립틴의 안정한 결정형 b의 제조방법 |
Citations (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2000080087A (ja) * | 1994-10-12 | 2000-03-21 | Euro Celtique Sa | 新規ベンゾオキサゾ―ル類 |
JP2003525941A (ja) * | 2000-03-06 | 2003-09-02 | エフ.ホフマン−ラ ロシュ アーゲー | 新規アザインドリル誘導体 |
WO2004016587A1 (ja) * | 2002-08-19 | 2004-02-26 | Ono Pharmaceutical Co., Ltd. | 含窒素化合物 |
JP2006503013A (ja) * | 2002-08-21 | 2006-01-26 | ベーリンガー インゲルハイム ファルマ ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディトゲゼルシャフト | 8−[3−アミノ−ピペリジン−1−イル]−キサンチン、その製造およびその薬理組成物としての使用 |
JP5323684B2 (ja) * | 2006-05-04 | 2013-10-23 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 多形体 |
Family Cites Families (484)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US2056046A (en) * | 1933-05-19 | 1936-09-29 | Rhone Poulenc Sa | Manufacture of bases derived from benz-dioxane |
US2375138A (en) * | 1942-05-01 | 1945-05-01 | American Cyanamid Co | Alkamine esters of aryloxymethyl benzoic acid |
US2629736A (en) * | 1951-02-24 | 1953-02-24 | Searle & Co | Basically substituted n-alkyl derivatives of alpha, beta, beta-triarylpropionamides |
US2730544A (en) * | 1952-07-23 | 1956-01-10 | Sahyun Lab | Alkylaminoalkyl esters of hydroxycyclohexylbenzoic acid |
US2750387A (en) * | 1953-11-25 | 1956-06-12 | Searle & Co | Basically substituted derivatives of diarylaminobenzamides |
DE1211359B (de) * | 1955-11-29 | 1966-02-24 | Oreal | Oxydationsmittelfreies Kaltfaerbemittel fuer menschliches Haar |
US3039477A (en) | 1957-12-02 | 1962-06-19 | Alf F Harbo | Apparatus for cleaning musical instruments of the cup mouthpiece type |
US2928833A (en) * | 1959-03-03 | 1960-03-15 | S E Massengill Company | Theophylline derivatives |
US3174901A (en) * | 1963-01-31 | 1965-03-23 | Jan Marcel Didier Aron Samuel | Process for the oral treatment of diabetes |
US3454635A (en) * | 1965-07-27 | 1969-07-08 | Hoechst Ag | Benzenesulfonyl-ureas and process for their manufacture |
US3673241A (en) * | 1968-04-04 | 1972-06-27 | Ciba Geigy Corp | Substituted benzaldehyde guanylhydrazones |
ES385302A1 (es) | 1970-10-22 | 1973-04-16 | Miquel S A Lab | Procedimiento para la obtencion de derivados trisubstitui- dos de etilendiamina. |
DE2205815A1 (de) | 1972-02-08 | 1973-08-16 | Hoechst Ag | Piperazinderivate und verfahren zu ihrer herstellung |
JPS5512435B2 (ja) * | 1972-07-01 | 1980-04-02 | ||
US4005208A (en) * | 1975-05-16 | 1977-01-25 | Smithkline Corporation | N-Heterocyclic-9-xanthenylamines |
US4061753A (en) | 1976-02-06 | 1977-12-06 | Interx Research Corporation | Treating psoriasis with transient pro-drug forms of xanthine derivatives |
AU508480B2 (en) | 1977-04-13 | 1980-03-20 | Asahi Kasei Kogyo Kabushiki Kaisha | Microcrystalline cellulose excipient and pharmaceutical composition containing thesame |
DE2758025A1 (de) | 1977-12-24 | 1979-07-12 | Bayer Ag | Neue derivate von 3,4,5-trihydroxypiperidin, verfahren zu ihrer herstellung und ihre verwendung |
NO154918C (no) | 1977-08-27 | 1987-01-14 | Bayer Ag | Analogifremgangsmaate til fremstilling av terapeutisk aktive derivater av 3,4,5-trihydroksypiperidin. |
DE2929596A1 (de) | 1979-07-21 | 1981-02-05 | Hoechst Ag | Verfahren zur herstellung von oxoalkyl-xanthinen |
CY1306A (en) | 1980-10-01 | 1985-12-06 | Glaxo Group Ltd | Aminoalkyl furan derivative |
US4382091A (en) | 1981-04-30 | 1983-05-03 | Syntex (U.S.A.) Inc. | Stabilization of 1-substituted imidazole derivatives in talc |
FR2558162B1 (fr) * | 1984-01-17 | 1986-04-25 | Adir | Nouveaux derives de la xanthine, leurs procedes de preparation et les compositions pharmaceutiques les renfermant |
FI79107C (fi) * | 1984-06-25 | 1989-11-10 | Orion Yhtymae Oy | Foerfarande foer framstaellning av stabil -form av prazosinhydroklorid. |
JPS6130567A (ja) | 1984-07-23 | 1986-02-12 | Shiseido Co Ltd | 尿素の安定化法 |
JPS61124383A (ja) | 1984-11-16 | 1986-06-12 | Unitika Ltd | 固定化線維素溶解活性酵素の安定化法 |
AR240698A1 (es) * | 1985-01-19 | 1990-09-28 | Takeda Chemical Industries Ltd | Procedimiento para preparar compuestos de 5-(4-(2-(5-etil-2-piridil)-etoxi)benzil)-2,4-tiazolidindiona y sus sales |
CA1242699A (en) | 1985-02-01 | 1988-10-04 | Bristol-Myers Company | Cefbuperazone and derivatives thereof |
US4741898A (en) | 1985-04-01 | 1988-05-03 | Fisher Scientific Company | Stabilized stain composition |
GB8515934D0 (en) * | 1985-06-24 | 1985-07-24 | Janssen Pharmaceutica Nv | (4-piperidinomethyl and-hetero)purines |
US5258380A (en) * | 1985-06-24 | 1993-11-02 | Janssen Pharmaceutica N.V. | (4-piperidinylmethyl and -hetero)purines |
ES2058061T3 (es) | 1985-10-25 | 1994-11-01 | Beecham Group Plc | Derivado de piperidina, su preparacion y su uso como medicamento. |
US5034225A (en) | 1985-12-17 | 1991-07-23 | Genentech Inc. | Stabilized human tissue plasminogen activator compositions |
US5433959A (en) | 1986-02-13 | 1995-07-18 | Takeda Chemical Industries, Ltd. | Stabilized pharmaceutical composition |
DE3683760D1 (de) | 1986-03-21 | 1992-03-12 | Heumann Pharma Gmbh & Co | Kristalline, wasserfreie sigma -form von 2-(4-(2-furoyl-(2-piperazin)-1-yl)-4-amino-6,7-dimethoxychinazolinhydrochlorid und verfahren zu ihrer herstellung. |
ATE110083T1 (de) | 1986-05-05 | 1994-09-15 | Gen Hospital Corp | Insulinotropes hormon. |
US5120712A (en) | 1986-05-05 | 1992-06-09 | The General Hospital Corporation | Insulinotropic hormone |
AU619444B2 (en) | 1986-06-02 | 1992-01-30 | Nippon Chemiphar Co. Ltd. | 2-(2-aminobenzylsulfinyl)- benzimidazole derivatives |
US4968672A (en) | 1987-01-02 | 1990-11-06 | The United States Of America As Represented By The Department Of Health And Human Services | Adenosine receptor prodrugs |
US4743450A (en) | 1987-02-24 | 1988-05-10 | Warner-Lambert Company | Stabilized compositions |
JPS63273159A (ja) | 1987-04-30 | 1988-11-10 | Sharp Corp | 文字処理装置 |
JPS6440433A (en) | 1987-08-05 | 1989-02-10 | Green Cross Corp | Aqueous liquid composition of thrombin |
EP0342675B1 (en) | 1988-05-19 | 1995-01-25 | Chugai Seiyaku Kabushiki Kaisha | Novel quinolonecarboxylic acid derivatives |
US5329025A (en) * | 1988-09-21 | 1994-07-12 | G. D. Searle & Co. | 3-azido compound |
US5234897A (en) * | 1989-03-15 | 1993-08-10 | Bayer Aktiengesellschaft | Herbicidal 3-amino-5-aminocarbonyl-1,2,4-triazoles |
DE3926119A1 (de) | 1989-08-08 | 1991-02-14 | Bayer Ag | 3-amino-5-aminocarbonyl-1,2,4-triazol-derivate |
GB8906792D0 (en) | 1989-03-23 | 1989-05-10 | Beecham Wuelfing Gmbh & Co Kg | Treatment and compounds |
DE3916430A1 (de) | 1989-05-20 | 1990-11-22 | Bayer Ag | Verfahren zur herstellung von 3-amino-5-aminocarbonyl-1,2,4-triazol-derivaten |
US5223499A (en) * | 1989-05-30 | 1993-06-29 | Merck & Co., Inc. | 6-amino substituted imidazo[4,5-bipyridines as angiotensin II antagonists |
IL94390A (en) | 1989-05-30 | 1996-03-31 | Merck & Co Inc | The 6-membered trans-nitrogen-containing heterocycles are compressed with imidazo and pharmaceutical preparations containing them |
US5332744A (en) * | 1989-05-30 | 1994-07-26 | Merck & Co., Inc. | Substituted imidazo-fused 6-membered heterocycles as angiotensin II antagonists |
FI94339C (fi) | 1989-07-21 | 1995-08-25 | Warner Lambert Co | Menetelmä farmaseuttisesti käyttökelpoisen /R-(R*,R*)/-2-(4-fluorifenyyli)- , -dihydroksi-5-(1-metyylietyyli)-3-fenyyli-4-/(fenyyliamino)karbonyyli/-1H-pyrroli-1-heptaanihapon ja sen farmaseuttisesti hyväksyttävien suolojen valmistamiseksi |
HU208115B (en) | 1989-10-03 | 1993-08-30 | Biochemie Gmbh | New process for producting pleuromutilin derivatives |
FR2654935B1 (fr) | 1989-11-28 | 1994-07-01 | Lvmh Rech | Utilisation de xanthines, eventuellement incorporees dans des liposomes, pour favoriser la pigmentation de la peau ou des cheveux. |
ES2084801T3 (es) * | 1990-02-19 | 1996-05-16 | Ciba Geigy Ag | Acil compuestos. |
KR930000861B1 (ko) | 1990-02-27 | 1993-02-08 | 한미약품공업 주식회사 | 오메프라졸 직장투여 조성물 |
ATE112491T1 (de) | 1990-09-13 | 1994-10-15 | Akzo Nobel Nv | Stabilisierte feste chemische zusammensetzungen. |
GB9020959D0 (en) | 1990-09-26 | 1990-11-07 | Beecham Group Plc | Novel compounds |
US5084460A (en) * | 1990-12-24 | 1992-01-28 | A. H. Robins Company, Incorporated | Methods of therapeutic treatment with N-(3-ouinuclidinyl)-2-hydroxybenzamides and thiobenzamides |
US5602127A (en) | 1991-02-06 | 1997-02-11 | Karl Thomae Gmbh | (Alkanesultam-1-yl)-benzimidazol-1-yl)-1yl)-methyl-biphenyls useful as angiotensin-II antagonists |
US5594003A (en) | 1991-02-06 | 1997-01-14 | Dr. Karl Thomae Gmbh | Tetrahydroimidazo[1,2-a]pyridin-2-yl-(benzimidazol-1-yl)-methyl-biphenyls useful as angiotensin-II antagonists |
US5614519A (en) | 1991-02-06 | 1997-03-25 | Karl Thomae Gmbh | (1-(2,3 or 4-N-morpholinoalkyl)-imidazol-4-yl)-benizimidazol-1-yl-methyl]-biphenyls useful as angiotensin-II antagonists |
GB9109862D0 (en) | 1991-05-08 | 1991-07-03 | Beecham Lab Sa | Pharmaceutical formulations |
DE4124150A1 (de) | 1991-07-20 | 1993-01-21 | Bayer Ag | Substituierte triazole |
DK0610317T3 (da) | 1991-10-22 | 2001-02-19 | New England Medical Center Inc | Inhibitorer af dipeptidyl-aminopeptidase type IV |
US5300298A (en) * | 1992-05-06 | 1994-04-05 | The Pennsylvania Research Corporation | Methods of treating obesity with purine related compounds |
GB9215633D0 (en) | 1992-07-23 | 1992-09-09 | Smithkline Beecham Plc | Novel treatment |
ATE165360T1 (de) * | 1992-07-31 | 1998-05-15 | Shionogi & Co | Triazolylthiomethylthiocephalosporin- hydrochlorid, sein kristallines hydrat und seine herstellung |
TW252044B (ja) * | 1992-08-10 | 1995-07-21 | Boehringer Ingelheim Kg | |
US5358941A (en) | 1992-12-02 | 1994-10-25 | Merck & Co., Inc. | Dry mix formulation for bisphosphonic acids with lactose |
DE4242459A1 (de) * | 1992-12-16 | 1994-06-23 | Merck Patent Gmbh | Imidazopyridine |
AU6087894A (en) | 1993-01-14 | 1994-08-15 | Cell Therapeutics, Inc. | Acetal or ketal substituted therapeutic compounds |
CA2118117A1 (en) | 1993-02-18 | 1994-08-19 | Shigeki Fujiwara | Adenosine uptake inhibitor |
JP3726291B2 (ja) | 1993-07-05 | 2005-12-14 | 三菱ウェルファーマ株式会社 | 安定な結晶構造を有するベンゾオキサジン化合物およびその製造法 |
FR2707641B1 (fr) | 1993-07-16 | 1995-08-25 | Fournier Ind & Sante | Composés de l'imidazol-5-carboxamide, leur procédé de préparation leurs intermédiaires et leur utilisation en thérapeutique. |
DE4339868A1 (de) | 1993-11-23 | 1995-05-24 | Merck Patent Gmbh | Imidazopyridazine |
DE4404183A1 (de) | 1994-02-10 | 1995-08-17 | Merck Patent Gmbh | 4-Amino-1-piperidylbenzoylguanidine |
US5545745A (en) | 1994-05-23 | 1996-08-13 | Sepracor, Inc. | Enantioselective preparation of optically pure albuterol |
CO4410191A1 (es) | 1994-09-19 | 1997-01-09 | Lilly Co Eli | SINTESIS DE 3-[4-(2-AMINOETOXI)BENZOIL]-2-ARIL-6- HIDROXIBENZO [b] TIOFENOS |
WO1996011917A1 (en) | 1994-10-12 | 1996-04-25 | Euro-Celtique, S.A. | Novel benzoxazoles |
US5470059A (en) * | 1995-01-18 | 1995-11-28 | Largent; Gerald A. | Soft spherical playing ball and method of making same |
GB9501178D0 (en) * | 1995-01-20 | 1995-03-08 | Wellcome Found | Guanine derivative |
CA2218548A1 (en) | 1995-05-19 | 1996-11-21 | Chiroscience Limited | Xanthines and their therapeutic use |
JPH08333339A (ja) | 1995-06-08 | 1996-12-17 | Fujisawa Pharmaceut Co Ltd | 光学活性なピペリジン酢酸誘導体の製造法 |
GB9523752D0 (en) | 1995-11-21 | 1996-01-24 | Pfizer Ltd | Pharmaceutical formulations |
DE19543478A1 (de) | 1995-11-22 | 1997-05-28 | Bayer Ag | Kristallines Hydrochlorid von {(R)-(-)-2- N-[4-(1,1-Dioxido-3-oxo-2,3-dihydrobenzisothiazol-2-yl)-buytl]-aminomethyl}-chroman |
FR2742751B1 (fr) | 1995-12-22 | 1998-01-30 | Rhone Poulenc Rorer Sa | Nouveaux taxoides, leur preparation et les compositions pharmaceutiques qui les contiennent |
WO1997023447A1 (en) | 1995-12-26 | 1997-07-03 | Alteon Inc. | N-acylaminoalkylhydrazinecarboximidamides |
US5891855A (en) | 1996-02-12 | 1999-04-06 | The Scripps Research Institute | Inhibitors of leaderless protein export |
DE122010000020I1 (de) * | 1996-04-25 | 2010-07-08 | Prosidion Ltd | Verfahren zur Senkung des Blutglukosespiegels in Säugern |
TWI240627B (en) | 1996-04-26 | 2005-10-01 | Chugai Pharmaceutical Co Ltd | Erythropoietin solution preparation |
WO1997046526A1 (en) | 1996-06-07 | 1997-12-11 | Eisai Co., Ltd. | Stable polymorphs of donepezil (1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine) hydrochloride and process for production |
US5965555A (en) * | 1996-06-07 | 1999-10-12 | Hoechst Aktiengesellschaft | Xanthine compounds having terminally animated alkynol side chains |
JPH1053576A (ja) * | 1996-06-07 | 1998-02-24 | Eisai Co Ltd | 塩酸ドネペジルの多形結晶およびその製造法 |
US5958951A (en) * | 1996-06-14 | 1999-09-28 | Novo Nordiskials | Modified form of the R(-)-N-(4,4-di(3-methylthien-2-yl)but-3-enyl)-nipecotic acid hydrochloride |
US5753635A (en) * | 1996-08-16 | 1998-05-19 | Berlex Laboratories, Inc. | Purine derivatives and their use as anti-coagulants |
EA001881B1 (ru) | 1996-09-23 | 2001-10-22 | Эли Лилли Энд Компани | Форма d дигидрата оланзапина |
WO1998018770A1 (en) | 1996-10-28 | 1998-05-07 | Novo Nordisk A/S | A process for the preparation of (-)-3,4-trans-diarylchromans |
UA65549C2 (uk) | 1996-11-05 | 2004-04-15 | Елі Ліллі Енд Компані | Спосіб регулювання ожиріння шляхом периферійного введення аналогів та похідних glp-1 (варіанти) та фармацевтична композиція |
DE69732572T2 (de) | 1996-11-12 | 2005-12-29 | Novo Nordisk A/S | Verwendung von glp-1 peptiden |
GB9623859D0 (en) | 1996-11-15 | 1997-01-08 | Chiroscience Ltd | Novel compounds |
EE04266B1 (et) | 1996-12-24 | 2004-04-15 | Biogen, Incorporated | Interferooni stabiilne vedelkompositsioon |
DE19705233A1 (de) | 1997-02-12 | 1998-08-13 | Froelich Juergen C | Verfahren zur Herstellung einer Formulierung enthaltend Arginin |
US6011049A (en) | 1997-02-19 | 2000-01-04 | Warner-Lambert Company | Combinations for diabetes |
DK0991407T4 (da) | 1997-03-13 | 2005-08-08 | Hexal Ag | Stabilisering af syresensitive benzimidazoler med amino/cyclodextrin-kombinationer |
US5972332A (en) | 1997-04-16 | 1999-10-26 | The Regents Of The University Of Michigan | Wound treatment with keratinocytes on a solid support enclosed in a porous material |
ZA984697B (en) | 1997-06-13 | 1999-12-01 | Lilly Co Eli | Stable insulin formulations. |
US6174548B1 (en) | 1998-08-28 | 2001-01-16 | Andrx Pharmaceuticals, Inc. | Omeprazole formulation |
TR200001603T2 (tr) * | 1997-12-05 | 2000-10-23 | Astrazeneca Uk Limited | Yeni bileşikler |
ID21411A (id) | 1997-12-10 | 1999-06-10 | Takeda Chemical Industries Ltd | Agen untuk mengobati daya tahan glukosa yang berisiko tinggi rusak |
JPH11193270A (ja) | 1997-12-26 | 1999-07-21 | Koei Chem Co Ltd | 光学活性1−メチル−3−ピペリジンメタノールの製造方法 |
CA2315736A1 (en) * | 1998-01-05 | 1999-07-15 | Eisai Co., Ltd. | Purine compounds and adenosine a2 receptor antagonist as preventive or therapeutic for diabetes mellitus |
AU766219B2 (en) | 1998-02-02 | 2003-10-09 | 1149336 Ontario Inc. | Method of regulating glucose metabolism, and reagents related thereto |
US20030013740A1 (en) | 1998-03-27 | 2003-01-16 | Martin P. Redmon | Stable dosage forms of fluoxetine and its enantiomers |
JP2002509919A (ja) | 1998-03-31 | 2002-04-02 | 日産化学工業株式会社 | ピリダジノン化合物塩酸塩及びその製造法 |
CA2268621A1 (en) | 1998-04-13 | 1999-10-13 | Takeda Chemical Industries, Ltd. | 2-pipirazinone-1-acetic acid derivative, production and use thereof |
US6207207B1 (en) | 1998-05-01 | 2001-03-27 | Mars, Incorporated | Coated confectionery having a crispy starch based center and method of preparation |
DE19823831A1 (de) * | 1998-05-28 | 1999-12-02 | Probiodrug Ges Fuer Arzneim | Neue pharmazeutische Verwendung von Isoleucyl Thiazolidid und seinen Salzen |
DE19828114A1 (de) | 1998-06-24 | 2000-01-27 | Probiodrug Ges Fuer Arzneim | Produgs instabiler Inhibitoren der Dipeptidyl Peptidase IV |
DE19828113A1 (de) | 1998-06-24 | 2000-01-05 | Probiodrug Ges Fuer Arzneim | Prodrugs von Inhibitoren der Dipeptidyl Peptidase IV |
WO2000003735A1 (fr) | 1998-07-15 | 2000-01-27 | Asahi Kasei Kogyo Kabushiki Kaisha | Excipient |
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 |
IT1312018B1 (it) * | 1999-03-19 | 2002-04-04 | Fassi Aldo | Procedimento migliorato per la produzione di sali non igroscopicidella l(-)-carnitina. |
WO2000066101A2 (en) | 1999-04-30 | 2000-11-09 | City Of Hope | Method of inhibiting glycation product formation |
AU4431000A (en) | 1999-05-12 | 2000-12-05 | Fujisawa Pharmaceutical Co., Ltd. | Novel use |
US20040152659A1 (en) | 1999-05-12 | 2004-08-05 | Fujisawa Pharmaceutical Co. Ltd. | Method for the treatment of parkinson's disease comprising administering an A1A2a receptor dual antagonist |
WO2000072799A2 (en) | 1999-05-27 | 2000-12-07 | The University Of Virginia Patent Foundation | Method and compositions for treating the inflammatory response |
CN100448482C (zh) | 1999-05-31 | 2009-01-07 | 三菱化学株式会社 | Hgf冻干制剂 |
WO2000072973A1 (en) | 1999-06-01 | 2000-12-07 | Elan Pharma International Ltd. | Small-scale mill and method thereof |
US6545002B1 (en) | 1999-06-01 | 2003-04-08 | University Of Virginia Patent Foundation | Substituted 8-phenylxanthines useful as antagonists of A2B adenosine receptors |
YU90901A (sh) | 1999-06-21 | 2004-07-15 | Boehringer Ingelheim Pharma Gmbh. & Co.Kg. | Biciklični heterocikli, lekovi koji sadrže ta jedinjenja, njihova primena i postupci za njihovo pripremanje |
US6448323B1 (en) | 1999-07-09 | 2002-09-10 | Bpsi Holdings, Inc. | Film coatings and film coating compositions based on polyvinyl alcohol |
ES2166270B1 (es) | 1999-07-27 | 2003-04-01 | Almirall Prodesfarma Sa | Derivados de 8-fenil-6,9-dihidro-(1,2,4,)triazolo(3,4-i)purin-5-ona. |
US6515117B2 (en) | 1999-10-12 | 2003-02-04 | Bristol-Myers Squibb Company | C-aryl glucoside SGLT2 inhibitors and method |
US6586438B2 (en) | 1999-11-03 | 2003-07-01 | Bristol-Myers Squibb Co. | Antidiabetic formulation and method |
GB9928330D0 (en) | 1999-11-30 | 2000-01-26 | Ferring Bv | Novel antidiabetic agents |
SG149676A1 (en) | 1999-12-23 | 2009-02-27 | Novartis Ag | Use of hypoglycemic agent for treating impaired glucose metabolism |
WO2001051919A2 (en) | 2000-01-07 | 2001-07-19 | Transform Pharmaceuticals, Inc. | High-throughput formation, identification, and analysis of diverse solid-forms |
US6362172B2 (en) | 2000-01-20 | 2002-03-26 | Bristol-Myers Squibb Company | Water soluble prodrugs of azole compounds |
ES2436610T3 (es) | 2000-01-21 | 2014-01-03 | Novartis Ag | Combinaciones que contienen inhibidores de la dipeptidilpeptidasa-IV y agentes antidiabéticos |
JP4621326B2 (ja) | 2000-02-01 | 2011-01-26 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | テプレノンの安定化組成物 |
CA2369076A1 (en) * | 2000-02-05 | 2001-08-09 | Vertex Pharmaceuticals Incorporated | Pyrazole compositions useful as inhibitors of erk |
AU2001234114A1 (en) | 2000-02-24 | 2001-09-03 | Takeda Chemical Industries Ltd. | Drugs containing combined active ingredients |
US6395767B2 (en) | 2000-03-10 | 2002-05-28 | Bristol-Myers Squibb Company | Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method |
GB0006133D0 (en) | 2000-03-14 | 2000-05-03 | Smithkline Beecham Plc | Novel pharmaceutical |
JP2001278812A (ja) | 2000-03-27 | 2001-10-10 | Kyoto Pharmaceutical Industries Ltd | 錠剤用崩壊剤及びこれを用いた錠剤 |
US6399101B1 (en) | 2000-03-30 | 2002-06-04 | Mova Pharmaceutical Corp. | Stable thyroid hormone preparations and method of making same |
US7282219B2 (en) | 2000-03-31 | 2007-10-16 | Kirin Beer Kabushiki Kaisha | Powdery preparation for transmucosal administration containing a polymeric form of drug and exhibiting improved storage stability |
DK2055302T3 (da) | 2000-03-31 | 2014-10-27 | Royalty Pharma Collection Trust | Fremgangsmåde til forbedring af signalering af øceller ved diabetes mellitus og til forebyggelse deraf |
JP2001292388A (ja) | 2000-04-05 | 2001-10-19 | Sharp Corp | 再生装置 |
GB0008694D0 (en) | 2000-04-07 | 2000-05-31 | Novartis Ag | Organic compounds |
WO2001096301A1 (fr) | 2000-06-14 | 2001-12-20 | Toray Industries, Inc. | Procedes de production de derive de piperidine racemique et de production de derive de piperidine a activite optique |
US7078397B2 (en) | 2000-06-19 | 2006-07-18 | Smithkline Beecham Corporation | Combinations of dipeptidyl peptidase IV inhibitors and other antidiabetic agents for the treatment of diabetes mellitus |
GB0014969D0 (en) | 2000-06-19 | 2000-08-09 | Smithkline Beecham Plc | Novel method of treatment |
US6689353B1 (en) | 2000-06-28 | 2004-02-10 | Bayer Pharmaceuticals Corporation | Stabilized interleukin 2 |
MXPA02012272A (es) | 2000-07-04 | 2003-04-25 | Novo Nordisk As | Compuestos heterociclicos que son inhibidores de la enzima dipeptidilpeptidasa-iv. |
EP1950199B1 (en) * | 2000-08-10 | 2009-12-02 | Mitsubishi Tanabe Pharma Corporation | Proline derivatives and use thereof as drugs |
US6821978B2 (en) | 2000-09-19 | 2004-11-23 | Schering Corporation | Xanthine phosphodiesterase V inhibitors |
US20060034922A1 (en) | 2000-11-03 | 2006-02-16 | Andrx Labs, Llc | Controlled release metformin compositions |
US6722883B2 (en) | 2000-11-13 | 2004-04-20 | G & H Technologies Llc | Protective coating for abrasive dental tools and burs |
US6821261B2 (en) | 2000-12-12 | 2004-11-23 | Dj Orthopedics, Llc | Orthopedic brace having length-adjustable supports |
JPWO2002051836A1 (ja) | 2000-12-27 | 2004-04-22 | 協和醗酵工業株式会社 | ジペプチジルペプチダーゼ−iv阻害剤 |
FR2818906B1 (fr) | 2000-12-29 | 2004-04-02 | Dospharma | Association medicamenteuse d'une biguanine et d'un transporteur, par exemple de metformine et d'arginine |
FR2819254B1 (fr) | 2001-01-08 | 2003-04-18 | Fournier Lab Sa | Nouveaux composes de la n-(phenylsulfonyl) glycine, leur procede de preparation et leur utilisation pour obtenir des compostions pharmaceutiques |
DE10117803A1 (de) | 2001-04-10 | 2002-10-24 | Boehringer Ingelheim Pharma | Xanthinderivate, deren Herstellung und deren Verwendung als Arzneimittel |
DE10109021A1 (de) | 2001-02-24 | 2002-09-05 | Boehringer Ingelheim Pharma | Xanthinderivate, deren Herstellung und deren Verwendung als Arzneimittel |
PL364221A1 (en) | 2001-02-02 | 2004-12-13 | Takeda Chemical Industries, Ltd. | Fused heterocyclic compounds |
US6610326B2 (en) | 2001-02-16 | 2003-08-26 | Andrx Corporation | Divalproex sodium tablets |
WO2002066015A1 (en) | 2001-02-16 | 2002-08-29 | Bristol-Myers Squibb Pharma Company | Use of polyalkylamine polymers in controlled release devices |
PT1368349E (pt) * | 2001-02-24 | 2007-04-30 | Boehringer Ingelheim Pharma | Derivados de xantina, sua preparação e sua utilização como medicamento |
US6936590B2 (en) | 2001-03-13 | 2005-08-30 | Bristol Myers Squibb Company | C-aryl glucoside SGLT2 inhibitors and method |
US6693094B2 (en) | 2001-03-22 | 2004-02-17 | Chrono Rx Llc | Biguanide and sulfonylurea formulations for the prevention and treatment of insulin resistance and type 2 diabetes mellitus |
CN1160122C (zh) | 2001-04-20 | 2004-08-04 | 清华大学 | 一种制备口服胰岛素油相制剂的方法 |
JP2002348279A (ja) * | 2001-05-25 | 2002-12-04 | Nippon Kayaku Co Ltd | 光学活性ピリジルケトン誘導体の製造方法並びに光学活性ピリジルケトン誘導体 |
DE10130371A1 (de) | 2001-06-23 | 2003-01-02 | Boehringer Ingelheim Pharma | Neue Arzneimittelkompositionen auf der Basis von Anticholinergika, Corticosteroiden und Betamimetika |
GB0115517D0 (en) | 2001-06-25 | 2001-08-15 | Ferring Bv | Novel antidiabetic agents |
IL158923A0 (en) | 2001-06-27 | 2004-05-12 | Smithkline Beecham Corp | Fluoropyrrolidines as dipeptidyl peptidase inhibitors |
ATE370943T1 (de) | 2001-06-27 | 2007-09-15 | Smithkline Beecham Corp | Fluoropyrrolidine als dipeptidyl-peptidase inhibitoren |
US6869947B2 (en) * | 2001-07-03 | 2005-03-22 | Novo Nordisk A/S | Heterocyclic compounds that are inhibitors of the enzyme DPP-IV |
EP1404675B1 (en) | 2001-07-03 | 2008-03-12 | Novo Nordisk A/S | Dpp-iv-inhibiting purine derivatives for the treatment of diabetes |
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 |
WO2003006424A1 (en) | 2001-07-10 | 2003-01-23 | 4Sc Ag | Novel compounds as anti-inflammatory, immunomodulatory and anti-proliferatory agents |
US7638522B2 (en) | 2001-08-13 | 2009-12-29 | Janssen Pharmaceutica N.V. | Salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino] benzonitrile |
AR035119A1 (es) | 2001-08-16 | 2004-04-14 | Lilly Co Eli | Anticuerpos humanos antagonistas anti-htnfsf13b |
TWI246510B (en) | 2001-09-14 | 2006-01-01 | Mitsubishi Pharma Corp | Thiazolidine derivatives and pharmaceutical uses thereof |
WO2003024965A2 (en) * | 2001-09-19 | 2003-03-27 | Novo Nordisk A/S | Heterocyclic compounds that are inhibitors of the enzyme dpp-iv |
CA2461454A1 (en) | 2001-09-24 | 2003-04-03 | Oregon Health And Science University | Assessment of neurons in the arcuate nucleus to screen for agents that modify feeding behavior |
DK1435877T3 (da) | 2001-10-15 | 2009-08-03 | Hemoteq Ag | Overtrækning af stents for at forhindre restenose |
DE10151296A1 (de) | 2001-10-17 | 2003-04-30 | Boehringer Ingelheim Pharma | Keratinozyten verwendbar als biologisch aktive Substanz bei der Behandlung von Wunden |
US6723340B2 (en) | 2001-10-25 | 2004-04-20 | Depomed, Inc. | Optimal polymer mixtures for gastric retentive tablets |
US20030083354A1 (en) | 2001-10-26 | 2003-05-01 | Pediamed Pharmaceuticals, Inc. | Phenylephrine tannate and pyrilamine tannate salts in pharmaceutical compositions |
US6861440B2 (en) | 2001-10-26 | 2005-03-01 | Hoffmann-La Roche Inc. | DPP IV inhibitors |
CA2464995A1 (en) | 2001-10-31 | 2003-05-08 | Novartis Ag | Methods to treat diabetes and related conditions based on polymorphisms in the tcf1 gene |
CA2363053C (en) | 2001-11-09 | 2011-01-25 | Bernard Charles Sherman | Clopidogrel bisulfate tablet formulation |
WO2003045228A2 (en) | 2001-11-26 | 2003-06-05 | Trustees Of Tufts College | Methods for treating autoimmune disorders, and reagents related thereto |
KR20040064687A (ko) | 2001-12-21 | 2004-07-19 | 도오레 화인케미칼 가부시키가이샤 | 광학 활성 시스 피페리딘 유도체의 제조법 |
US6727261B2 (en) | 2001-12-27 | 2004-04-27 | Hoffman-La Roche Inc. | Pyrido[2,1-A]Isoquinoline derivatives |
WO2003057245A1 (fr) | 2001-12-28 | 2003-07-17 | Nrl Pharma, Inc. | Compositions servant a ameliorer le metabolisme lipidique |
JP4733922B2 (ja) | 2002-01-10 | 2011-07-27 | インペリアル・イノベ−ションズ・リミテッド | 摂食行動の修正 |
US20070197552A1 (en) | 2002-01-11 | 2007-08-23 | Novo Nordisk A/S | Method and composition for treatment of diabetes, hypertension, chronic heart failure and fluid retentive states |
WO2003057200A2 (en) | 2002-01-11 | 2003-07-17 | Novo Nordisk A/S | Compositions comprising inhibitors of dpp-iv and nep enzymes for the treatment of diabetes |
EP1854454B1 (en) | 2002-01-16 | 2013-11-06 | Boehringer Ingelheim Pharma GmbH & Co. KG | Method for the preparation of amorphous telmisartan |
EP1477182A4 (en) | 2002-01-21 | 2009-05-27 | Nrl Pharma Inc | NEW ANALGETICS |
EP1333033A1 (en) | 2002-01-30 | 2003-08-06 | Boehringer Ingelheim Pharma GmbH & Co.KG | FAP-activated anti-tumor compounds |
JP2005517690A (ja) | 2002-02-01 | 2005-06-16 | ファイザー・プロダクツ・インク | 固体薬物分散物を含有する即時放出剤形 |
US7610153B2 (en) | 2002-02-13 | 2009-10-27 | Virginia Commonwealth University | Multi-drug titration and evaluation |
SI1476138T1 (sl) | 2002-02-21 | 2012-07-31 | Valeant Internat Barbados Srl | Formulacije s prirejenim sproščanjem vsaj ene oblike tramadola |
US7074798B2 (en) * | 2002-02-25 | 2006-07-11 | Eisai Co., Ltd | Xanthine derivative and DPPIV inhibitor |
HUP0200849A2 (hu) | 2002-03-06 | 2004-08-30 | Sanofi-Synthelabo | N-aminoacetil-2-ciano-pirrolidin-származékok, e vegyületeket tartalmazó gyógyszerkészítmények és eljárás előállításukra |
JP4298212B2 (ja) * | 2002-03-29 | 2009-07-15 | 大日本印刷株式会社 | 塩酸エピナスチン高融点型結晶の製造法 |
JP2003300977A (ja) | 2002-04-10 | 2003-10-21 | Sumitomo Pharmaceut Co Ltd | キサンチン誘導体 |
EP1496982A4 (en) | 2002-04-16 | 2006-07-19 | Merck & Co Inc | SOLID FORMS OF SALTS WITH TYROSINE KINASE EFFECT |
CA2484306A1 (en) | 2002-04-26 | 2003-11-06 | Katsumi Maezono | Prophylactic and therapeutic agent of diabetes mellitus |
AU2003231252A1 (en) | 2002-05-09 | 2003-11-11 | Enos Pharmaceuticals, Inc. | Methods and compositions for the treatment and prevention of intermittent claudication or alzheimer's disease |
GB0212412D0 (en) | 2002-05-29 | 2002-07-10 | Novartis Ag | Combination of organic compounds |
DK1509525T5 (da) | 2002-05-31 | 2007-07-30 | Schering Corp | Fremgangsmåde til fremstilling af xanthin-phosphodiesterase V-inhibitorer og præcursorer derfor |
BR0311697A (pt) | 2002-06-06 | 2005-03-22 | Eisai Co Ltd | Novos derivados condensados de imidazol |
ES2199061B1 (es) | 2002-06-10 | 2005-02-16 | Laboratorios Vita, S.A. | Comprimidos bucodispersables y procedimiento para su obtencion. |
FR2840897B1 (fr) | 2002-06-14 | 2004-09-10 | Fournier Lab Sa | Nouveaux derives d'arylsulfonamides et leur utilisation en therapeutique |
US20040002615A1 (en) | 2002-06-28 | 2004-01-01 | Allen David Robert | Preparation of chiral amino-nitriles |
US20040023981A1 (en) | 2002-07-24 | 2004-02-05 | Yu Ren | Salt forms with tyrosine kinase activity |
AR040661A1 (es) | 2002-07-26 | 2005-04-13 | Theravance Inc | Diclorhidrato cristalino de n-{2-[-((r)-2-hidroxi-2-feniletilamino)fenil]etil}-(r)-2hidroxi-2-(3-formamido-4-hidroxifenil)etilamina, agonista del receptor adrenergico beta 2 |
DE10238243A1 (de) | 2002-08-21 | 2004-03-04 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | 8-[3-Amino-piperidin-1-yl]-xanthine, deren Herstellung und deren Verwendung als Arzneimittel |
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 |
DE10238470A1 (de) | 2002-08-22 | 2004-03-04 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Xanthinderivate, deren Herstellung und deren Verwendung als Arzneimittel |
US7495005B2 (en) * | 2002-08-22 | 2009-02-24 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Xanthine derivatives, their preparation and their use in pharmaceutical compositions |
US7569574B2 (en) * | 2002-08-22 | 2009-08-04 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Purine derivatives, the preparation thereof and their use as pharmaceutical compositions |
DE10238477A1 (de) | 2002-08-22 | 2004-03-04 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Purinderivate, deren Herstellung und deren Verwendung als Arzneimittel |
DE10238723A1 (de) | 2002-08-23 | 2004-03-11 | Bayer Ag | Phenyl-substituierte Pyrazolyprimidine |
DE10238724A1 (de) | 2002-08-23 | 2004-03-04 | Bayer Ag | Alkyl-substituierte Pyrazolpyrimidine |
US20060039974A1 (en) | 2002-09-11 | 2006-02-23 | Takeda Pharmaceutical Company Limited | Sustained release preparation |
CN1688293A (zh) | 2002-09-16 | 2005-10-26 | 韦思公司 | 多肽治疗剂口服给药的缓释配方及其使用方法 |
US7262207B2 (en) | 2002-09-19 | 2007-08-28 | Abbott Laboratories | Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV) |
AU2003266559B2 (en) * | 2002-09-26 | 2008-01-24 | Eisai R&D Management Co., Ltd. | Combination drug |
US20060039968A1 (en) | 2002-10-08 | 2006-02-23 | Ramalingam Manikandan | Gabapentin tablets and method for their preparation |
AU2003269850A1 (en) | 2002-10-08 | 2004-05-04 | Novo Nordisk A/S | Hemisuccinate salts of heterocyclic dpp-iv inhibitors |
US20040122048A1 (en) | 2002-10-11 | 2004-06-24 | Wyeth Holdings Corporation | Stabilized pharmaceutical composition containing basic excipients |
US6861526B2 (en) | 2002-10-16 | 2005-03-01 | Pfizer Inc. | Process for the preparation of (S,S)-cis-2-benzhydryl-3-benzylaminoquinuclidine |
JP4352001B2 (ja) | 2002-10-18 | 2009-10-28 | メルク エンド カムパニー インコーポレーテッド | 糖尿病の治療または予防のためのベータ−アミノ複素環式ジペプチジルペプチダーゼ阻害剤 |
JP2004161749A (ja) | 2002-10-24 | 2004-06-10 | Toray Fine Chemicals Co Ltd | 光学活性含窒素化合物の製造方法 |
WO2004048379A1 (ja) | 2002-11-01 | 2004-06-10 | Sumitomo Pharmaceuticals Co., Ltd. | キサンチン化合物 |
RU2005117383A (ru) | 2002-11-07 | 2006-01-20 | Мерк энд Ко., Инк. (US) | Производные фенилаланина в качестве ингибиторов дипептидилпептидазы для лечения или профилактики диабета |
DE10251927A1 (de) | 2002-11-08 | 2004-05-19 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Xanthinderivate, deren Herstellung und deren Verwendung als Arzneimittel |
US7482337B2 (en) | 2002-11-08 | 2009-01-27 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions |
DE10254304A1 (de) * | 2002-11-21 | 2004-06-03 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Xanthinderivate, deren Herstellung und deren Verwendung als Arzneimittel |
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 |
UY28103A1 (es) | 2002-12-03 | 2004-06-30 | Boehringer Ingelheim Pharma | Nuevas imidazo-piridinonas sustituidas, su preparación y su empleo como medicacmentos |
ATE404191T1 (de) | 2002-12-10 | 2008-08-15 | Novartis Pharma Ag | Kombinationen von einem dpp-iv inhibitor und einem ppar- alpha agonist |
DE10351663A1 (de) * | 2002-12-20 | 2004-07-01 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Pulverförmige Arzneimittel enthaltend ein Tiotropiumsalz und Salmeterolxinafoat |
US20040152720A1 (en) | 2002-12-20 | 2004-08-05 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Powdered medicaments containing a tiotropium salt and salmeterol xinafoate |
DK1599222T3 (da) | 2003-01-08 | 2009-04-27 | Novartis Vaccines & Diagnostic | Stabiliserede vandige pr parater omfattende v vsfaktorvej-inhibitor (TFPI) eller v vsfaktorvej-inhibitorvariant |
EP1599468B1 (en) | 2003-01-14 | 2007-10-03 | Arena Pharmaceuticals, Inc. | 1,2,3-trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto such as diabetes and hyperglycemia |
DE10335027A1 (de) | 2003-07-31 | 2005-02-17 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Verwendung von Angiotensin II Rezeptor Antagonisten |
PE20040950A1 (es) | 2003-02-14 | 2005-01-01 | Theravance Inc | DERIVADOS DE BIFENILO COMO AGONISTAS DE LOS RECEPTORES ADRENERGICOS ß2 Y COMO ANTAGONISTAS DE LOS RECEPTORES MUSCARINICOS |
JP2004250336A (ja) | 2003-02-18 | 2004-09-09 | Kao Corp | コーティング錠及び糖衣錠の製造法 |
US7135575B2 (en) | 2003-03-03 | 2006-11-14 | Array Biopharma, Inc. | P38 inhibitors and methods of use thereof |
US7442387B2 (en) | 2003-03-06 | 2008-10-28 | Astellas Pharma Inc. | Pharmaceutical composition for controlled release of active substances and manufacturing method thereof |
CA2515289A1 (en) | 2003-03-12 | 2004-09-23 | Arizona Board Of Regents On Behalf Of The University Of Arizona | Weak base salts |
CN100415224C (zh) | 2003-03-18 | 2008-09-03 | 诺瓦提斯公司 | 包含脂肪酸和氨基酸的组合物 |
CN104383542B (zh) | 2003-04-08 | 2017-09-26 | 普罗热尼奇制药公司 | 包含甲基纳曲酮的药物配方 |
US20040220186A1 (en) | 2003-04-30 | 2004-11-04 | Pfizer Inc. | PDE9 inhibitors for treating type 2 diabetes,metabolic syndrome, and cardiovascular disease |
WO2004096806A1 (ja) | 2003-04-30 | 2004-11-11 | Sumitomo Pharmaceuticals Co. Ltd. | 縮合イミダゾール誘導体 |
TW200510277A (en) | 2003-05-27 | 2005-03-16 | Theravance Inc | Crystalline form of β2-adrenergic receptor agonist |
FR2855521B1 (fr) | 2003-05-28 | 2005-08-05 | Flamel Tech Sa | Polyaminoacides fonctionnalises par au moins un groupement h ydrophobe et leurs applications notamment therapeutiques. |
AU2003902828A0 (en) | 2003-06-05 | 2003-06-26 | Fujisawa Pharmaceutical Co., Ltd. | Dpp-iv inhibitor |
US7566707B2 (en) * | 2003-06-18 | 2009-07-28 | Boehringer Ingelheim International Gmbh | Imidazopyridazinone and imidazopyridone derivatives, the preparation thereof and their use as pharmaceutical compositions |
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 |
MXPA05013734A (es) | 2003-06-20 | 2006-03-08 | Hoffmann La Roche | Hexahidropiroisoquinolinas como inhibidores de dpp-iv. |
DE602004030244D1 (de) | 2003-06-20 | 2011-01-05 | Hoffmann La Roche | Itoren |
JO2625B1 (en) | 2003-06-24 | 2011-11-01 | ميرك شارب اند دوم كوربوريشن | Phosphoric acid salts of dipeptidyl betidase inhibitor 4 |
US7364755B2 (en) | 2003-07-07 | 2008-04-29 | Synthon Ip Inc. | Modified calcium phosphate excipient |
AR045047A1 (es) | 2003-07-11 | 2005-10-12 | Arena Pharm Inc | Derivados arilo y heteroarilo trisustituidos como moduladores del metabolismo y de la profilaxis y tratamiento de desordenes relacionados con los mismos |
EP2287165A3 (en) | 2003-07-14 | 2011-06-22 | Arena Pharmaceuticals, Inc. | Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto |
US20050027012A1 (en) | 2003-07-16 | 2005-02-03 | Boehringer Ingelheim International Gmbh | Tablets containing ambroxol |
US20060134206A1 (en) | 2003-07-24 | 2006-06-22 | Iyer Eswaran K | Oral compositions for treatment of diseases |
CN1829709A (zh) | 2003-08-01 | 2006-09-06 | 健亚生物科技公司 | 对抗黄病毒的双环咪唑衍生物 |
US6995183B2 (en) | 2003-08-01 | 2006-02-07 | Bristol Myers Squibb Company | Adamantylglycine-based inhibitors of dipeptidyl peptidase IV and methods |
EP1656158B1 (en) | 2003-08-14 | 2016-03-09 | Novo Nordisk Health Care AG | Liquid, aqueous pharmaceutical composition of factor vii polypeptides |
CN102349927A (zh) | 2003-08-29 | 2012-02-15 | Hdac默克研究有限责任公司 | 联合治疗癌症的方法 |
WO2005026148A1 (en) | 2003-09-08 | 2005-03-24 | Takeda San Diego, Inc. | Dipeptidyl peptidase inhibitors |
US20070072810A1 (en) | 2003-10-03 | 2007-03-29 | Takeda Pharmaceutical Company, Limited | Agent for treating diabetes |
US7284625B2 (en) | 2003-10-22 | 2007-10-23 | Kirk Jones | Quick connect assembly for ATV implements |
BR0304443B1 (pt) | 2003-10-28 | 2012-08-21 | processo para obtenção de concentrados de titánio com elevado teor de tio2 e baixo teor de radionuclìdeos a partir de concentrados mecánicos de anatásio. | |
US7107714B2 (en) | 2003-11-10 | 2006-09-19 | Marketing Displays, Inc. | Portable snap-fit sign stand |
KR20140089408A (ko) | 2003-11-17 | 2014-07-14 | 노파르티스 아게 | 디펩티딜 펩티다제 ⅳ 억제제의 용도 |
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 |
JPWO2005053695A1 (ja) * | 2003-12-04 | 2007-12-06 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 多発性硬化症予防剤または治療剤 |
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 |
US7217711B2 (en) * | 2003-12-17 | 2007-05-15 | Boehringer Ingelheim International Gmbh | Piperazin-1-yl and 2-([1,4]diazepan-1-yl)-imidazo[4,5-d]-pyridazin-4-ones, the preparation thereof and their use as pharmaceutical compositions |
ATE501135T1 (de) * | 2003-12-18 | 2011-03-15 | Tibotec Pharm Ltd | Piperidinamino-benzimidazol-derivate al respiratorisches syncytialvirus replikation inhibitoren |
DE10360835A1 (de) | 2003-12-23 | 2005-07-21 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Bicyclische Imidazolverbindungen, deren Herstellung und deren Verwendung als Arzneimittel |
CA2549955A1 (en) | 2003-12-24 | 2005-07-07 | Prosidion Limited | Heterocyclic derivatives as gpcr receptor agonists |
EP1708680A2 (en) | 2004-01-21 | 2006-10-11 | Janssen Pharmaceutica N.V. | Mitratapide oral solution |
SE0400234D0 (sv) | 2004-02-06 | 2004-02-06 | Active Biotech Ab | New compounds, methods for their preparation and use thereof |
PT1758905E (pt) | 2004-02-18 | 2009-07-16 | Boehringer Ingelheim Int | 8-[3-amino-piperidin-1-il]-xantinas, sua preparação e sua utilização como inibidores de dpp-iv |
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 |
DE102004019540A1 (de) | 2004-04-22 | 2005-11-10 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Arzneimittelkombinationen zur Behandlung von Atemwegserkrankungen |
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 |
EP1593671A1 (en) | 2004-03-05 | 2005-11-09 | Graffinity Pharmaceuticals AG | DPP-IV inhibitors |
US7393847B2 (en) * | 2004-03-13 | 2008-07-01 | Boehringer Ingleheim International Gmbh | Imidazopyridazinediones, their preparation and their use as pharmaceutical compositions |
CN102079743B (zh) | 2004-03-15 | 2020-08-25 | 武田药品工业株式会社 | 二肽基肽酶抑制剂 |
EA011158B1 (ru) | 2004-03-16 | 2009-02-27 | Бёрингер Ингельхайм Интернациональ Гмбх | Замещённые глюкопиранозилом бензольные производные, содержащие эти соединения лекарственные средства, их применение и способ их получения |
EP1577306A1 (de) | 2004-03-17 | 2005-09-21 | Boehringer Ingelheim Pharma GmbH & Co.KG | Neue Benzoxazinonderivate als langwirksame Betamimetika zur Behandlung von Atemwegserkrankungen |
US7179809B2 (en) * | 2004-04-10 | 2007-02-20 | Boehringer Ingelheim International Gmbh | 2-Amino-imidazo[4,5-d]pyridazin-4-ones, their preparation and their use as pharmaceutical compositions |
WO2005097798A1 (de) | 2004-04-10 | 2005-10-20 | Boehringer Ingelheim International Gmbh | Neue 2-amino-imidazo[4,5-d]pyridazin-4-one und 2-amino-imidazo[4,5-c]pyridin-4-one, deren herstellung und deren verwendung als arzneimittel |
US20050239778A1 (en) | 2004-04-22 | 2005-10-27 | Boehringer Ingelheim International Gmbh | Novel medicament combinations for the treatment of respiratory diseases |
US20050244502A1 (en) | 2004-04-28 | 2005-11-03 | Mathias Neil R | Composition for enhancing absorption of a drug and method |
CN1976691B (zh) | 2004-05-03 | 2010-10-13 | 奥加生物药业(I.P.3)有限公司 | 半胱胺用于治疗高胆固醇血症和糖尿病并发症 |
US7439370B2 (en) * | 2004-05-10 | 2008-10-21 | Boehringer Ingelheim International Gmbh | Imidazole derivatives, their preparation and their use as intermediates for the preparation of pharmaceutical compositions and pesticides |
GEP20084421B (en) | 2004-05-12 | 2008-07-10 | Pfizer Prod Inc | Proline derivatives and their use as dipeptidyl peptidase iv inhibitors |
DE102004024454A1 (de) | 2004-05-14 | 2005-12-08 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Enantiomerenreine Betaagonisten, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel |
PE20060315A1 (es) | 2004-05-24 | 2006-05-15 | Irm Llc | Compuestos de tiazol como moduladores de ppar |
TWI354569B (en) | 2004-05-28 | 2011-12-21 | Bristol Myers Squibb Co | Coated tablet formulation and method |
WO2005117948A1 (en) | 2004-06-01 | 2005-12-15 | Ares Trading S.A. | Method of stabilizing proteins |
WO2005119526A1 (en) | 2004-06-03 | 2005-12-15 | Pfizer Products Inc. | Crystal structure of dipeptidyl peptidase iv (dpp-iv) and uses thereof |
US7935723B2 (en) | 2004-06-04 | 2011-05-03 | Novartis Pharma Ag | Use of organic compounds |
EP1604989A1 (en) | 2004-06-08 | 2005-12-14 | Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft | DPP-IV inhibitors |
US20050276794A1 (en) | 2004-06-09 | 2005-12-15 | Papas Klearchos K | Composition and method for improving pancreatic islet cell survival |
DE102004030502A1 (de) * | 2004-06-24 | 2006-01-12 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Imidazole und Triazole, deren Herstellung und Verwendung als Arzneimittel |
CA2511269A1 (en) | 2004-07-07 | 2006-01-07 | F. Hoffmann-La Roche Ag | Multimarker panel based on p1gf for diabetes type 1 and 2 |
CA2573209A1 (en) | 2004-07-14 | 2006-01-19 | Novartis Ag | Combination of dpp-iv inhibitors and compounds modulating 5-ht3 and/or 5-ht4 receptors |
JP2006045156A (ja) | 2004-08-06 | 2006-02-16 | Sumitomo Pharmaceut Co Ltd | 縮合ピラゾール誘導体 |
TW200613275A (en) | 2004-08-24 | 2006-05-01 | Recordati Ireland Ltd | Lercanidipine salts |
EP1782832A4 (en) | 2004-08-26 | 2009-08-26 | Takeda Pharmaceutical | MEANS FOR THE TREATMENT OF DIABETES |
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 |
CN1759834B (zh) | 2004-09-17 | 2010-06-23 | 中国医学科学院医药生物技术研究所 | 黄连素或其与辛伐他汀联合在制备用于预防或治疗与血脂有关疾病或症状的产品中用途 |
CA2580461A1 (en) | 2004-09-23 | 2006-04-06 | Amgen Inc. | Substituted sulfonamidopropionamides and methods of use |
BRPI0516446A (pt) | 2004-10-08 | 2008-09-02 | Novartis Ag | combinação de compostos orgánicos |
EA013463B1 (ru) | 2004-10-12 | 2010-04-30 | ГЛЕНМАРК ФАРМАСЬЮТИКАЛС Эс.Эй. | Новые ингибиторы дипептидилпептидазы iv, содержащие их фармацевтические композиции, способ их получения и способ лечения с их применением |
MX2007004934A (es) | 2004-10-25 | 2007-06-12 | Novartis Ag | Combinacion de inhibidor de dpp-iv, anti-diabetico de ppar, y metformina. |
DE102005013967A1 (de) | 2004-11-05 | 2006-10-05 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Bradykinin-B1-Antagonisten, Verfahren zu deren Herstellung sowie deren Verwendung als Arzneimittel |
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 |
JP2006137678A (ja) | 2004-11-10 | 2006-06-01 | Shionogi & Co Ltd | インターロイキン−2組成物 |
BRPI0518651A2 (pt) | 2004-12-24 | 2008-12-02 | Dainippon Sumitomo Pharma | composto, uma prà-droga do mesmo, ou um sal do composto ou prà-droga farmaceuticamente aceitÁvel, composiÇço farmacÊutica, inibidor de dipeptidil peptidase iv, uso de um composto, uma prà-droga do mesmo ou um sal do composto ou prà-droga farmaceuticamente aceitÁvel, e, mÉtodo para tratar diabetes |
KR100760430B1 (ko) | 2004-12-31 | 2007-10-04 | 한미약품 주식회사 | 당뇨병 치료제의 경구 투여용 서방성 복합 제제 및 이의제조 방법 |
DOP2006000008A (es) | 2005-01-10 | 2006-08-31 | Arena Pharm Inc | Terapia combinada para el tratamiento de la diabetes y afecciones relacionadas y para el tratamiento de afecciones que mejoran mediante un incremento de la concentración sanguínea de glp-1 |
MY148521A (en) | 2005-01-10 | 2013-04-30 | Arena Pharm Inc | Substituted pyridinyl and pyrimidinyl derivatives as modulators of metabolism and the treatment of disorders related thereto |
GT200600008A (es) | 2005-01-18 | 2006-08-09 | Formulacion de compresion directa y proceso | |
EP1874339A1 (en) | 2005-04-21 | 2008-01-09 | Gastrotech Pharma A/S | Pharmaceutical preparations of a glp-1 molecule and an anti-emetic drug |
AU2006239929B2 (en) | 2005-04-22 | 2011-11-03 | Alantos Pharmaceuticals Holding, Inc. | Dipeptidyl peptidase-IV inhibitors |
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 |
CN101203494A (zh) | 2005-05-25 | 2008-06-18 | 惠氏公司 | 合成经取代3-氰基喹啉和其中间物的方法 |
EP1894567B1 (en) | 2005-06-03 | 2012-08-15 | Mitsubishi Tanabe Pharma Corporation | Concomitant pharmaceutical agents and use thereof |
GT200600218A (es) | 2005-06-10 | 2007-03-28 | Formulación y proceso de compresión directa | |
NZ564285A (en) | 2005-06-20 | 2010-03-26 | Decode Genetics Ehf | Genetic variants in the TCF7L2 gene as diagnostic markers for risk of type 2 diabetes mellitus |
ATE483732T1 (de) | 2005-07-08 | 2010-10-15 | Pfizer Ltd | Madcam-antikörper |
UY29694A1 (es) | 2005-07-28 | 2007-02-28 | Boehringer Ingelheim Int | Metodos para prevenir y tratar trastornos metabolicos y nuevos derivados de pirazol-o-glucosido |
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 |
MX2008001799A (es) | 2005-08-11 | 2008-04-16 | Hoffmann La Roche | Composicion farmaceutica que comprende un inhibidor de dipeptidil peptidasa iv. |
EP1760076A1 (en) | 2005-09-02 | 2007-03-07 | Ferring B.V. | FAP Inhibitors |
WO2007033350A1 (en) | 2005-09-14 | 2007-03-22 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors for treating diabetes |
PL1931350T5 (pl) | 2005-09-14 | 2021-11-15 | Takeda Pharmaceutical Company Limited | Podanie inhibitorów dipeptydylo-peptydazy |
RS20080112A (en) | 2005-09-16 | 2009-05-06 | Arena Pharmaceuticals Inc., | Modulators of metabolism and the treatment of disorders related thereto |
RU2440143C2 (ru) | 2005-09-20 | 2012-01-20 | Новартис Аг | Применение ингибитора dpp-iv для снижения приступов гликемии |
WO2007038979A1 (en) | 2005-09-22 | 2007-04-12 | Swissco Development Ag | Effervescent metformin composition and tablets and granules made therefrom |
JOP20180109A1 (ar) | 2005-09-29 | 2019-01-30 | Novartis Ag | تركيبة جديدة |
US20080221200A1 (en) | 2005-09-30 | 2008-09-11 | Malcolm Allison | Combination of Organic Compounds |
CA2625646A1 (en) | 2005-10-25 | 2007-05-03 | Merck & Co., Inc. | Combination of a dipeptidyl peptidase-4 inhibitor and an anti-hypertensive agent for the treatment of diabetes and hypertension |
CN101300298A (zh) | 2005-11-04 | 2008-11-05 | Ls电线有限公司 | Mdh-聚合物混合粒子的合成 |
EP1962827A4 (en) | 2005-12-16 | 2011-02-16 | Merck Sharp & Dohme | PHARMACEUTICAL COMPOSITIONS OF COMBINATIONS OF DIPEPTIDYL-PEPTIDASE-4-INHIBITORS WITH METFORMIN |
GB0526291D0 (en) | 2005-12-23 | 2006-02-01 | Prosidion Ltd | Therapeutic method |
JP2009520763A (ja) | 2005-12-23 | 2009-05-28 | ノバルティス アクチエンゲゼルシャフト | Dpp−iv阻害剤として有用な縮合ヘテロ環式化合物 |
US20090054512A1 (en) | 2006-01-06 | 2009-02-26 | Foley James E | Use of organic compounds |
KR20080102395A (ko) | 2006-02-15 | 2008-11-25 | 베링거 인겔하임 인터내셔날 게엠베하 | 글루코피라노실-치환된 벤조니트릴 유도체, 당해 화합물을 함유하는 약제학적 조성물, 이들의 용도 및 이들의 제조방법 |
WO2007099345A1 (en) | 2006-03-02 | 2007-09-07 | Betagenon Ab | Medical use of bmp-2 and/ or bmp-4 |
PE20071221A1 (es) | 2006-04-11 | 2007-12-14 | Arena Pharm Inc | Agonistas del receptor gpr119 en metodos para aumentar la masa osea y para tratar la osteoporosis y otras afecciones caracterizadas por masa osea baja, y la terapia combinada relacionada a estos agonistas |
US8455435B2 (en) | 2006-04-19 | 2013-06-04 | Ludwig-Maximilians-Universitat Munchen | Remedies for ischemia |
EP1852108A1 (en) * | 2006-05-04 | 2007-11-07 | Boehringer Ingelheim Pharma GmbH & Co.KG | DPP IV inhibitor formulations |
PE20080251A1 (es) | 2006-05-04 | 2008-04-25 | Boehringer Ingelheim Int | Usos de inhibidores de dpp iv |
KR20070111099A (ko) | 2006-05-16 | 2007-11-21 | 영진약품공업주식회사 | 시타글립틴 염산염의 신규 결정형, 이의 제조 방법과 이를포함하는 약학적 조성물 |
NZ572368A (en) | 2006-05-16 | 2011-04-29 | Gilead Sciences Inc | Method and compositions for treating hematological malignancies |
WO2007137107A2 (en) | 2006-05-19 | 2007-11-29 | Abbott Laboratories | Inhibitors of diacylglycerol o-acyltransferase type 1 enzyme |
KR100858848B1 (ko) | 2006-05-23 | 2008-09-17 | 한올제약주식회사 | 메트포르민 서방정 |
WO2007149797A2 (en) | 2006-06-19 | 2007-12-27 | Novartis Ag | Use of organic compounds |
WO2007148185A2 (en) | 2006-06-21 | 2007-12-27 | Pfizer Products Inc. | Substituted 3 -amino- pyrrolidino-4 -lactams as dpp inhibitors |
AT503443B1 (de) | 2006-06-23 | 2007-10-15 | Leopold Franzens Uni Innsbruck | Verfahren zur herstellung einer eisfläche für eissportbahnen |
TW200811147A (en) | 2006-07-06 | 2008-03-01 | Arena Pharm Inc | Modulators of metabolism and the treatment of disorders related thereto |
TW200811140A (en) | 2006-07-06 | 2008-03-01 | Arena Pharm Inc | Modulators of metabolism and the treatment of disorders related thereto |
WO2008017670A1 (en) | 2006-08-08 | 2008-02-14 | Boehringer Ingelheim International Gmbh | Pyrrolo [3, 2 -d] pyrimidines as dpp-iv inhibitors for the treatment of diabetes mellitus |
JP5384343B2 (ja) | 2006-08-15 | 2014-01-08 | 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−置換シクロプロピルベンゼン誘導体、そのような化合物を含む医薬組成物、sglt阻害剤としてのそれらの使用及びそれらの製造方法 |
JP2010501010A (ja) | 2006-08-17 | 2010-01-14 | ウェルスタット セラピューティクス コーポレイション | 代謝障害のための併用処置 |
DE102006042586B4 (de) | 2006-09-11 | 2014-01-16 | Betanie B.V. International Trading | Verfahren zum mikropartikulären Beladen von hochpolymeren Kohlenhydraten mit hydrophoben Wirkflüssigkeiten |
US7956201B2 (en) | 2006-11-06 | 2011-06-07 | Hoffman-La Roche Inc. | Process for the preparation of (S)-4-fluoromethyl-dihydro-furan-2-one |
EP2079753A1 (en) | 2006-11-06 | 2009-07-22 | Boehringer Ingelheim International GmbH | Glucopyranosyl-substituted benzyl-benzonitrile derivatives, medicaments containing such compounds, their use and process for their manufacture |
JP5337040B2 (ja) | 2006-11-09 | 2013-11-06 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Sglt−2インヒビターとの組み合わせ治療及びそれらの医薬組成物 |
EA015835B1 (ru) | 2006-12-06 | 2011-12-30 | Смитклайн Бичем Корпорейшн | Производные 4-окса(тиа)метилпиперидина и их применение в качестве противодиабетических средств |
ES2319596B1 (es) | 2006-12-22 | 2010-02-08 | Laboratorios Almirall S.A. | Nuevos derivados de los acidos amino-nicotinico y amino-isonicotinico. |
US7638541B2 (en) | 2006-12-28 | 2009-12-29 | Metabolex Inc. | 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine |
AR064736A1 (es) | 2007-01-04 | 2009-04-22 | Prosidion Ltd | Agonistas de gpcr |
CL2008000133A1 (es) | 2007-01-19 | 2008-05-23 | Boehringer Ingelheim Int | Composicion farmaceutica que comprende un compuesto derivado de pirazol-o-glucosido combinado con al menos un segundo agente terapeutico; y uso de la composicion para el tratamiento de diabetes mellitus, cataratas, neuropatia, infarto de miocardio, e |
ME01239B (me) | 2007-02-01 | 2013-06-20 | Takeda Pharmaceuticals Co | Čvrsti preparat koji sadrži alogliptin i pioglitazon |
EP2124901B1 (en) | 2007-02-01 | 2017-07-19 | Takeda Pharmaceutical Company Limited | Tablet preparation without causing a tableting trouble |
ES2366000T3 (es) | 2007-02-06 | 2011-10-14 | Chelsea Therapeutics, Inc. | Nuevos compuestos, métodos para su preparación y uso de los mismos. |
WO2008113000A1 (en) | 2007-03-15 | 2008-09-18 | Nectid, Inc. | Anti-diabetic combinations comprising a slow release biguanide composition and an immediate release dipeptidyl peptidase iv inhibitor composition |
EP2143443B1 (en) | 2007-04-03 | 2014-11-19 | Mitsubishi Tanabe Pharma Corporation | A combination of dipeptidyl peptidase iv inhibitor and sweetener for use in the treatment of obesity |
WO2008130998A2 (en) | 2007-04-16 | 2008-10-30 | Smith & Nephew, Inc. | Powered surgical system |
PE20090696A1 (es) | 2007-04-20 | 2009-06-20 | Bristol Myers Squibb Co | Formas cristalinas de saxagliptina y procesos para preparar las mismas |
EP2144902B1 (en) | 2007-05-04 | 2012-05-16 | Bristol-Myers Squibb Company | [6,6]and [6,7]-bicyclic gpr119 g protein-coupled receptor agonists |
WO2007135196A2 (en) | 2007-07-09 | 2007-11-29 | Symrise Gmbh & Co. Kg | Stable soluble salts of phenylbenzimidazole sulfonic acid at phs at or below 7.0 |
WO2009011451A1 (en) | 2007-07-19 | 2009-01-22 | Takeda Pharmaceutical Company Limited | Solid preparation comprising alogliptin and metformin hydrochloride |
CL2008002424A1 (es) | 2007-08-16 | 2009-09-11 | Boehringer Ingelheim Int | Composicion farmaceutica que comprende un compuesto derivado de pirazol-o-glucosido; y uso de la composicion farmaceutica para el tratamiento de la diabetes mellitus, tolerancia anormal a la glucosa e hiperglucemia, trastornos metabolicos, entre otras. |
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. |
CL2008002425A1 (es) | 2007-08-16 | 2009-09-11 | Boehringer Ingelheim Int | Composición farmacéutica que comprende un inhibidor de sglt2 y 1-(4-metil-quinazolin-2-il)metil-3metil-7-(-2-butin-1-il)-8-(3-(r)-amino-piperidin-1il)-xantina, un inhibidor de dpp iv y su uso para el tratamiento de la obesidad y de la diabetes tipo 1 y 2 y complicaciones de esta. |
UY31291A1 (es) | 2007-08-16 | 2009-03-31 | Composicion farmacéutica que comprende un derivado de pirazol-0-glucosido | |
US20110112069A1 (en) | 2007-08-17 | 2011-05-12 | Boehringer Ingelheim International Gmbh | Purin derivatives for use in the treatment of fab-related diseases |
WO2009037719A1 (en) | 2007-09-21 | 2009-03-26 | Lupin Limited | Novel compounds as dipeptidyl peptidase iv (dpp iv) inhibitors |
JP5241849B2 (ja) | 2007-11-16 | 2013-07-17 | ノボ・ノルデイスク・エー/エス | インスリン及びインスリン分泌性ペプチドを含む薬学的組成物 |
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 |
US20090186086A1 (en) | 2008-01-17 | 2009-07-23 | Par Pharmaceutical, Inc. | Solid multilayer oral dosage forms |
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. |
TW200936136A (en) | 2008-01-28 | 2009-09-01 | Sanofi Aventis | Tetrahydroquinoxaline urea derivatives, their preparation and their therapeutic application |
US20100330177A1 (en) | 2008-02-05 | 2010-12-30 | Merck Sharp & Dohme Corp. | Pharmaceutical compositions of a combination of metformin and a dipeptidyl peptidase-iv inhibitor |
CA2716130A1 (en) | 2008-03-04 | 2009-09-11 | Nazaneen Pourkavoos | Pharmaceutical compositions of a combination of metformin and a dipeptidyl peptidase-iv inhibitor |
CA2717138A1 (en) | 2008-03-05 | 2009-09-11 | Takeda Pharmaceutical Company Limited | 5-membered heterocyclic compounds and bicyclic heteroaryl having glucagon antagonistic action useful for treating diabetes |
US8551524B2 (en) | 2008-03-14 | 2013-10-08 | Iycus, Llc | Anti-diabetic combinations |
PL2280704T3 (pl) | 2008-03-31 | 2015-10-30 | Cymabay Therapeutics Inc | Związki oksymetylenoarylowe i ich zastosowania |
PE20091730A1 (es) | 2008-04-03 | 2009-12-10 | Boehringer Ingelheim Int | Formulaciones que comprenden un inhibidor de dpp4 |
CN101590007A (zh) | 2008-05-27 | 2009-12-02 | 北京瑞伊人科技发展有限公司 | 一种盐酸二甲双胍/伏格列波糖降糖口服制剂组合物及其制备 |
PE20100156A1 (es) | 2008-06-03 | 2010-02-23 | Boehringer Ingelheim Int | Tratamiento de nafld |
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 |
WO2010018217A2 (en) | 2008-08-15 | 2010-02-18 | Boehringer Ingelheim International Gmbh | Organic compounds for wound healing |
JP2010053576A (ja) | 2008-08-27 | 2010-03-11 | Sumitomo Forestry Co Ltd | 舗装用マット |
US8513264B2 (en) | 2008-09-10 | 2013-08-20 | Boehringer Ingelheim International Gmbh | Combination therapy for the treatment of diabetes and related conditions |
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 |
WO2010045656A2 (en) | 2008-10-17 | 2010-04-22 | Nectid, Inc. | Novel sglt2 inhibitor dosage forms |
CN107011345A (zh) | 2008-12-23 | 2017-08-04 | 勃林格殷格翰国际有限公司 | 有机化合物的盐形式 |
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 |
TWI466672B (zh) | 2009-01-29 | 2015-01-01 | Boehringer Ingelheim Int | 小兒科病人糖尿病之治療 |
EA029759B1 (ru) | 2009-02-13 | 2018-05-31 | Бёрингер Ингельхайм Интернациональ Гмбх | Антидиабетические лекарственные средства, содержащие ингибитор dpp-4 (линаглиптин) необязательно в комбинации с другими антидиабетическими средствами |
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 |
AU2010212867B2 (en) | 2009-02-13 | 2013-05-16 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition comprising a SGLT2 inhibitor, a DPP-IV inhibitor and optionally a further antidiabetic agent and uses thereof |
TW201031661A (en) | 2009-02-17 | 2010-09-01 | Targacept Inc | Fused benzazepines as neuronal nicotinic acetylcholine receptor ligands |
EP2408780A2 (en) | 2009-03-20 | 2012-01-25 | Pfizer Inc. | 3-oxa-7-azabicycloý3.3.1¨nonanes |
JP2012525396A (ja) | 2009-04-27 | 2012-10-22 | レバレジオ コーポレイション | インスリン耐性および真性糖尿病を治療するための組成物および方法 |
US8815292B2 (en) | 2009-04-27 | 2014-08-26 | Revalesio Corporation | Compositions and methods for treating insulin resistance and diabetes mellitus |
US20120100221A1 (en) | 2009-06-02 | 2012-04-26 | Ranbaxy Laboratories Limited | Pharmaceutical compositions containing a combination of an antihistamine and a decongestant |
AU2010260373A1 (en) | 2009-06-15 | 2012-01-12 | Merck Sharp & Dohme Corp. | Pharmaceutical compositions of combinations of dipeptidyl peptidase-4 inhibitors with pioglitazone |
EP2456426A1 (en) | 2009-07-21 | 2012-05-30 | Keryx Biopharmaceuticals, Inc. | Ferric citrate dosage forms |
KR101763659B1 (ko) | 2009-10-02 | 2017-08-01 | 베링거 인겔하임 인터내셔날 게엠베하 | Bi―1356 및 메트포르민을 포함하는 약제학적 조성물 |
US10610489B2 (en) | 2009-10-02 | 2020-04-07 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, pharmaceutical dosage form, process for their preparation, methods for treating and uses thereof |
JP5446716B2 (ja) | 2009-10-21 | 2014-03-19 | 大正製薬株式会社 | アルギニン及びカルニチン含有錠剤の製造方法 |
EP3646859A1 (en) | 2009-11-27 | 2020-05-06 | Boehringer Ingelheim International GmbH | Treatment of genotyped diabetic patients with dpp-iv inhibitors such as linagliptin |
JP2010070576A (ja) | 2009-12-28 | 2010-04-02 | Sato Pharmaceutical Co Ltd | 速溶解性錠剤 |
TWI562775B (en) | 2010-03-02 | 2016-12-21 | Lexicon Pharmaceuticals Inc | Methods of using inhibitors of sodium-glucose cotransporters 1 and 2 |
US20130109703A1 (en) | 2010-03-18 | 2013-05-02 | Boehringer Ingelheim International Gmbh | Combination of a GPR119 Agonist and the DPP-IV Inhibitor Linagliptin for Use in the Treatment of Diabetes and Related Conditions |
EP2566464A1 (en) | 2010-05-05 | 2013-03-13 | Boehringer Ingelheim International GmbH | Pharmaceutical formulations comprising pioglitazone and linagliptin |
AU2011249722B2 (en) | 2010-05-05 | 2015-09-17 | Boehringer Ingelheim International Gmbh | Combination therapy |
US9271984B2 (en) | 2010-06-09 | 2016-03-01 | Poxel | Treatment of type 1 diabetes |
AR084698A1 (es) | 2010-06-22 | 2013-06-05 | Twi Pharmaceuticals Inc | Composiciones de liberacion controlada con reducido efecto de alimentos, reducida interaccion entre farmaco y los alimentos |
BR112012032579B1 (pt) | 2010-06-24 | 2021-05-11 | Boehringer Ingelheim International Gmbh | uso de linagliptina e composição farmacêutica compreendendo linagliptina e insulina basal de longa duração |
EP2611442B1 (en) | 2010-09-03 | 2018-07-04 | Bristol-Myers Squibb Company | Drug formulations using water soluble antioxidants |
WO2012039420A1 (ja) | 2010-09-21 | 2012-03-29 | 国立大学法人九州大学 | 動脈圧反射機能障害に関連した疾患を治療するためのバイオニック動脈圧反射システム |
US9034883B2 (en) | 2010-11-15 | 2015-05-19 | Boehringer Ingelheim International Gmbh | Vasoprotective and cardioprotective antidiabetic therapy |
WO2012088682A1 (en) | 2010-12-29 | 2012-07-05 | Shanghai Fochon Pharmaceutical Co Ltd. | 2-(3-aminopiperidin-1-yl)-[1,2,4]triazolo[1,5-c]pyrimidine-5,7(3h,6h)-dione derivates as dipeptidyl peptidase iv(dpp-iv) inhibitors |
WO2012106303A1 (en) | 2011-02-01 | 2012-08-09 | Bristol-Myers Squibb Company | Pharmaceutical formulations including an amine compound |
AR085689A1 (es) | 2011-03-07 | 2013-10-23 | Boehringer Ingelheim Int | Composiciones farmaceuticas de metformina, linagliptina y un inhibidor de sglt-2 |
US8785455B2 (en) | 2011-05-10 | 2014-07-22 | Sandoz Ag | Polymorph of linagliptin benzoate |
HUE043540T2 (hu) | 2011-07-15 | 2019-08-28 | Boehringer Ingelheim Int | Szubsztituált dimer kinazolin-származék, elõállítása, valamint alkalmazása 1-es és 2-es típusú cukorbetegség kezelésére szolgáló gyógyászati készítményekben |
US8849828B2 (en) | 2011-09-30 | 2014-09-30 | International Business Machines Corporation | Refinement and calibration mechanism for improving classification of information assets |
US20130172244A1 (en) | 2011-12-29 | 2013-07-04 | Thomas Klein | Subcutaneous therapeutic use of dpp-4 inhibitor |
MX353496B (es) | 2012-01-04 | 2018-01-16 | Procter & Gamble | Estructuras fibrosas que contienen activos con múltiples regiones. |
US9555001B2 (en) | 2012-03-07 | 2017-01-31 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition 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 |
EP3685839A1 (en) | 2012-05-14 | 2020-07-29 | Boehringer Ingelheim International GmbH | Linagliptin for use in the treatment of albuminuria and kidney related diseases |
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 |
EP2854824A1 (en) | 2012-05-25 | 2015-04-08 | Boehringer Ingelheim International GmbH | Use of keratinocytes as a biologically active substance in the treatment of wounds, such as diabetic wounds, optionally in combination with a dpp-4 inhibitor |
WO2013179307A2 (en) | 2012-05-29 | 2013-12-05 | Mylan Laboratories Limited | Stabilized pharmaceutical compositions of saxagliptin |
EP2887961B1 (en) | 2012-08-24 | 2021-04-28 | Novartis AG | Nep inhibitors for treating diseases characterized by atrial enlargement or remodeling |
WO2014056941A1 (en) | 2012-10-09 | 2014-04-17 | Boehringer Ingelheim International Gmbh | Use of moisture-conditioned disintegrants in tablet manufacture |
JP2015533134A (ja) | 2012-10-09 | 2015-11-19 | 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 | 錠剤の機械的安定性に適切な少なくとも1種の水和物形成活性物質及び/又はアジュバントを含有する機械的に安定な錠剤、特にアルギニン含有錠剤の製造における選択的に水分調整された打錠材料の使用 |
US9050302B2 (en) | 2013-03-01 | 2015-06-09 | Jazz Pharmaceuticals Ireland Limited | Method of administration of gamma hydroxybutyrate with monocarboxylate transporters |
JP2016510795A (ja) | 2013-03-15 | 2016-04-11 | 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 | 心臓保護及び腎臓保護の抗糖尿病治療におけるリナグリプチンの使用 |
CN113181161A (zh) | 2013-04-18 | 2021-07-30 | 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 |
JP2016518438A (ja) | 2013-05-17 | 2016-06-23 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | DPP−4阻害薬とα−グルコシダーゼ阻害薬との組合せ |
JP6507154B2 (ja) | 2013-06-14 | 2019-04-24 | 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 | 糖尿病及びその合併症を治療するためのddp−4阻害薬 |
ES2950384T3 (es) | 2014-02-28 | 2023-10-09 | Boehringer Ingelheim Int | Uso médico de un inhibidor de DPP-4 |
CN104130258B (zh) | 2014-08-13 | 2016-06-01 | 广东东阳光药业有限公司 | 一种二聚体的转化方法 |
WO2016059219A1 (en) | 2014-10-17 | 2016-04-21 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition and uses thereof |
BR112018072401A2 (pt) | 2016-06-10 | 2019-02-19 | Boehringer Ingelheim International Gmbh | combinações de linagliptina e metformina |
US20210299129A1 (en) | 2018-07-17 | 2021-09-30 | Boehringer Ingelheim International Gmbh | Cardiosafe Antidiabetic Therapy |
US11752145B2 (en) | 2020-03-30 | 2023-09-12 | Sanjay Gupta | Quinoline derivatives with other anti-viral agents |
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Patent Citations (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2000080087A (ja) * | 1994-10-12 | 2000-03-21 | Euro Celtique Sa | 新規ベンゾオキサゾ―ル類 |
JP2003525941A (ja) * | 2000-03-06 | 2003-09-02 | エフ.ホフマン−ラ ロシュ アーゲー | 新規アザインドリル誘導体 |
WO2004016587A1 (ja) * | 2002-08-19 | 2004-02-26 | Ono Pharmaceutical Co., Ltd. | 含窒素化合物 |
JP2006503013A (ja) * | 2002-08-21 | 2006-01-26 | ベーリンガー インゲルハイム ファルマ ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディトゲゼルシャフト | 8−[3−アミノ−ピペリジン−1−イル]−キサンチン、その製造およびその薬理組成物としての使用 |
JP5323684B2 (ja) * | 2006-05-04 | 2013-10-23 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 多形体 |
JP5800773B2 (ja) * | 2006-05-04 | 2015-10-28 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 多形体 |
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