CA2681092A1 - Combinaisons anti-diabetiques comprenant une composition de biguanide a liberation lente et une composition d'inhibiteur de dipeptidyl peptidase iv a liberation immediate - Google Patents
Combinaisons anti-diabetiques comprenant une composition de biguanide a liberation lente et une composition d'inhibiteur de dipeptidyl peptidase iv a liberation immediate Download PDFInfo
- Publication number
- CA2681092A1 CA2681092A1 CA002681092A CA2681092A CA2681092A1 CA 2681092 A1 CA2681092 A1 CA 2681092A1 CA 002681092 A CA002681092 A CA 002681092A CA 2681092 A CA2681092 A CA 2681092A CA 2681092 A1 CA2681092 A1 CA 2681092A1
- Authority
- CA
- Canada
- Prior art keywords
- inhibitor
- dipeptidyl peptidase
- biguanide
- sitagliptin
- pharmaceutically acceptable
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Abandoned
Links
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Classifications
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/13—Amines
- A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/401—Proline; Derivatives thereof, e.g. captopril
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4196—1,2,4-Triazoles
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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
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US11/724,486 | 2007-03-15 | ||
| US11/724,486 US20070172525A1 (en) | 2007-03-15 | 2007-03-15 | Anti-diabetic combinations |
| US11/789,080 | 2007-04-24 | ||
| US11/789,080 US20080064701A1 (en) | 2007-04-24 | 2007-04-24 | Anti-diabetic combinations |
| PCT/US2008/057054 WO2008113000A1 (fr) | 2007-03-15 | 2008-03-14 | Combinaisons anti-diabétiques comprenant une composition de biguanide à libération lente et une composition d'inhibiteur de dipeptidyl peptidase iv à libération immédiate |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2681092A1 true CA2681092A1 (fr) | 2008-09-18 |
Family
ID=39496119
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002681092A Abandoned CA2681092A1 (fr) | 2007-03-15 | 2008-03-14 | Combinaisons anti-diabetiques comprenant une composition de biguanide a liberation lente et une composition d'inhibiteur de dipeptidyl peptidase iv a liberation immediate |
Country Status (4)
| Country | Link |
|---|---|
| EP (1) | EP2139464A1 (fr) |
| JP (1) | JP2010521492A (fr) |
| CA (1) | CA2681092A1 (fr) |
| WO (1) | WO2008113000A1 (fr) |
Families Citing this family (55)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7407955B2 (en) | 2002-08-21 | 2008-08-05 | Boehringer Ingelheim Pharma Gmbh & Co., Kg | 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions |
| US7501426B2 (en) | 2004-02-18 | 2009-03-10 | Boehringer Ingelheim International Gmbh | 8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions |
| DE102004054054A1 (de) | 2004-11-05 | 2006-05-11 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Verfahren zur Herstellung chiraler 8-(3-Amino-piperidin-1-yl)-xanthine |
| 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 |
| PE20110235A1 (es) | 2006-05-04 | 2011-04-14 | Boehringer Ingelheim Int | Combinaciones farmaceuticas que comprenden linagliptina y metmorfina |
| KR101452915B1 (ko) | 2006-05-04 | 2014-10-21 | 베링거 인겔하임 인터내셔날 게엠베하 | 다형태 |
| EP1852108A1 (fr) | 2006-05-04 | 2007-11-07 | Boehringer Ingelheim Pharma GmbH & Co.KG | Compositions d'inhibiteurs de la DPP IV |
| PE20090938A1 (es) | 2007-08-16 | 2009-08-08 | Boehringer Ingelheim Int | Composicion farmaceutica que comprende un derivado de benceno sustituido con glucopiranosilo |
| 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 |
| MX2010009731A (es) * | 2008-03-04 | 2010-09-30 | Merck Sharp & Dohme | Composiciones farmaceuticas de una combinacion de metformina y un inhibidor de dipeptidil peptidasa-iv. |
| US8551524B2 (en) | 2008-03-14 | 2013-10-08 | Iycus, Llc | Anti-diabetic combinations |
| AU2014262269B2 (en) * | 2008-04-03 | 2017-02-02 | Boehringer Ingelheim International Gmbh | DPP-IV inhibitor combined with a further antidiabetic agent, tablets comprising such formulations, their use and process for their preparation |
| PE20091730A1 (es) * | 2008-04-03 | 2009-12-10 | Boehringer Ingelheim Int | Formulaciones que comprenden un inhibidor de dpp4 |
| UY32030A (es) | 2008-08-06 | 2010-03-26 | Boehringer Ingelheim Int | "tratamiento para diabetes en pacientes inapropiados para terapia con metformina" |
| KR20190016601A (ko) | 2008-08-06 | 2019-02-18 | 베링거 인겔하임 인터내셔날 게엠베하 | 메트포르민 요법이 부적합한 환자에서의 당뇨병 치료 |
| CA2736421A1 (fr) | 2008-09-10 | 2010-03-18 | Boehringer Ingelheim International Gmbh | Polytherapie pour le traitement du diabete et des etats pathologiques apparentes |
| 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 |
| JP2012512848A (ja) | 2008-12-23 | 2012-06-07 | 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 | 有機化合物の塩の形態 |
| WO2010074271A1 (fr) * | 2008-12-26 | 2010-07-01 | 武田薬品工業株式会社 | Agent thérapeutique pour le diabète |
| TW201036975A (en) | 2009-01-07 | 2010-10-16 | Boehringer Ingelheim Int | Treatment for diabetes in patients with inadequate glycemic control despite metformin therapy |
| BRPI1008560B1 (pt) | 2009-02-13 | 2021-08-31 | Boehringer Ingelheim International Gmbh | Composição farmacêutica compreendendo um inibidor de sglt2, um inibidor de dpp-iv e opcionalmente um outro agente antidiabético e usos dos mesmos |
| US20110009347A1 (en) | 2009-07-08 | 2011-01-13 | Yin Liang | Combination therapy for the treatment of diabetes |
| JP5662453B2 (ja) | 2009-10-02 | 2015-01-28 | 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 | 医薬組成物の治療上の使用 |
| EP3315124B1 (fr) * | 2009-11-13 | 2021-01-06 | Astrazeneca AB | Formulations de comprimés bicouches |
| JP5784623B2 (ja) | 2009-11-13 | 2015-09-24 | アストラゼネカ・アクチエボラーグＡｓｔｒａｚｅｎｅｃａ Ａｋｔｉｅｂｏｌａｇ | 速放性錠剤製剤 |
| AU2016203426B2 (en) * | 2009-11-13 | 2017-12-07 | Astrazeneca Ab | Bilayer tablet formulations |
| AU2014218385B2 (en) * | 2009-11-13 | 2016-02-25 | Astrazeneca Ab | Bilayer tablet formulations |
| KR20240090632A (ko) | 2009-11-27 | 2024-06-21 | 베링거 인겔하임 인터내셔날 게엠베하 | 리나글립틴과 같은 ｄｐｐ－ｉｖ 억제제를 사용한 유전자형 검사된 당뇨병 환자의 치료 |
| US20190262367A1 (en) * | 2010-03-03 | 2019-08-29 | Volant Holdings Gmbh | Oral formulations mimetic of roux-en-y gastric bypass actions on the ileal brake; compositions, methods of treatment, diagnostics and systems for treatment of metabolic syndrome manifestations including insulin resistance, fatty liver disease, hyperlipidemia, and type 2 diabetes |
| CA3070513C (fr) | 2010-05-05 | 2023-01-03 | Boehringer Ingelheim International Gmbh | Inhibiteur de dpp-4 a utiliser dans le traitement des transformations dela peau ou de la necrose |
| TWI599360B (zh) | 2010-05-11 | 2017-09-21 | 健生藥品公司 | 醫藥調配物 |
| KR20130093012A (ko) | 2010-06-24 | 2013-08-21 | 베링거 인겔하임 인터내셔날 게엠베하 | 당뇨병 요법 |
| EP2590631B1 (fr) * | 2010-07-06 | 2016-10-26 | Janssen Pharmaceutica NV | Formulation pour le traitement par co-therapie du diabete |
| AR083878A1 (es) | 2010-11-15 | 2013-03-27 | Boehringer Ingelheim Int | Terapia antidiabetica vasoprotectora y cardioprotectora, linagliptina, metodo de tratamiento |
| US9211263B2 (en) | 2012-01-06 | 2015-12-15 | Elcelyx Therapeutics, Inc. | Compositions and methods of treating metabolic disorders |
| US8796338B2 (en) | 2011-01-07 | 2014-08-05 | Elcelyx Therapeutics, Inc | Biguanide compositions and methods of treating metabolic disorders |
| US9480663B2 (en) | 2011-01-07 | 2016-11-01 | Elcelyx Therapeutics, Inc. | Biguanide compositions and methods of treating metabolic disorders |
| US9572784B2 (en) | 2011-01-07 | 2017-02-21 | Elcelyx Therapeutics, Inc. | Compositions comprising statins, biguanides and further agents for reducing cardiometabolic risk |
| HUE051738T2 (hu) | 2011-01-07 | 2021-03-29 | Anji Pharma Us Llc | Kemoszenzoros receptorligandum-alapú terápiák |
| US11974971B2 (en) | 2011-01-07 | 2024-05-07 | Anji Pharmaceuticals Inc. | Compositions and methods for treating metabolic disorders |
| US11759441B2 (en) | 2011-01-07 | 2023-09-19 | Anji Pharmaceuticals Inc. | Biguanide compositions and methods of treating metabolic disorders |
| AR085689A1 (es) | 2011-03-07 | 2013-10-23 | Boehringer Ingelheim Int | Composiciones farmaceuticas de metformina, linagliptina y un inhibidor de sglt-2 |
| DK2731947T3 (en) | 2011-07-15 | 2019-04-23 | Boehringer Ingelheim Int | SUBSTITUTED DIMERIC QUINAZOLINE DERIVATIVE, PREPARATION AND USE thereof IN PHARMACEUTICAL COMPOSITIONS FOR TREATMENT OF TYPE I AND TYPE II DIABETES |
| KR20200137035A (ko) | 2012-01-06 | 2020-12-08 | 앤지 파마 유에스 엘엘씨 | 바이구아나이드 조성물 및 대사 장애를 치료하는 방법 |
| EA033067B1 (ru) | 2012-01-06 | 2019-08-30 | Элселикс Терапьютикс, Инк. | Способ лечения метаболических расстройств у пациента, имеющего противопоказание к назначению бигуанидного соединения |
| US20130189358A1 (en) * | 2012-01-10 | 2013-07-25 | Roey Solomonovich | Saxagliptin pharmaceutical formulations |
| US9555001B2 (en) | 2012-03-07 | 2017-01-31 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition and uses thereof |
| TWI469785B (zh) * | 2012-04-25 | 2015-01-21 | Inovobiologic Inc | 用於治療代謝性疾病之膳食纖維組成物 |
| WO2013171167A1 (fr) | 2012-05-14 | 2013-11-21 | Boehringer Ingelheim International Gmbh | Dérivé de xanthine en tant qu'inhibiteur de dpp-4 pour l'utilisation dans le traitement de troubles associés aux podocytes et/ou un syndrome néphrotique |
| WO2013171166A1 (fr) | 2012-05-14 | 2013-11-21 | Boehringer Ingelheim International Gmbh | Dérivé de xanthine en tant qu'inhibiteur de dpp-4 pour l'utilisation dans le traitement de sirs et/ou d'une sepsie |
| WO2013174767A1 (fr) | 2012-05-24 | 2013-11-28 | Boehringer Ingelheim International Gmbh | Dérivé de xanthine en tant qu'inhibiteur de la dpp-4 à utiliser dans la modification de l'apport alimentaire et dans la régulation des préférences alimentaires |
| EP3110449B1 (fr) | 2014-02-28 | 2023-06-28 | Boehringer Ingelheim International GmbH | Utilisation médicale d'un inhibiteur de dpp-4 |
| EP4233840A3 (fr) | 2016-06-10 | 2023-10-18 | Boehringer Ingelheim International GmbH | Combinaisons de linagliptine et de metformine |
| KR20200021774A (ko) * | 2018-08-21 | 2020-03-02 | 대화제약 주식회사 | 시타글립틴 속방층을 포함하는 제제의 제조방법, 상기 제조방법으로 제조된 제제, 시타글립틴 속방층 코팅 방법, 및 시타글립틴 속방층 코팅용 조성물 |
| EP4045048A4 (fr) | 2019-10-14 | 2023-05-24 | Santa Farma Ilaç Sanayi A.S. | Formulations orales comprenant du monohydrate de hci de sitagliptine présentant des caractéristiques pharmaceutiques améliorées |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6099859A (en) * | 1998-03-20 | 2000-08-08 | Andrx Pharmaceuticals, Inc. | Controlled release oral tablet having a unitary core |
| IN192749B (fr) * | 2002-11-15 | 2004-05-15 | Ranbaxy Lab Ltd | |
| WO2004045622A1 (fr) * | 2002-11-15 | 2004-06-03 | Ranbaxy Laboratories Limited | Formes galeniques pharmaceutiques de combinaisons de biguanide-sulfonyluree |
| CN1805738A (zh) * | 2003-06-16 | 2006-07-19 | 兰贝克赛实验室有限公司 | 持续释放的二甲双胍片剂 |
| US20090253752A1 (en) * | 2004-10-25 | 2009-10-08 | Bryan Burkey | Combination of dpp-iv inhibitor, ppar antidiabetic and metmorfin |
| EP1841448A2 (fr) * | 2004-12-30 | 2007-10-10 | Diakine Therapeutics, Inc. | Compositions pharmaceutiques et procedes pour le retablissement de masse et de fonction de cellule-beta |
| WO2006082523A2 (fr) * | 2005-01-25 | 2006-08-10 | Aurobindo Pharma Limited | Compositions pharmaceutiques de metformine |
| JP2008115080A (ja) * | 2005-04-22 | 2008-05-22 | Taisho Pharmaceutical Co Ltd | 併用医薬 |
-
2008
- 2008-03-14 CA CA002681092A patent/CA2681092A1/fr not_active Abandoned
- 2008-03-14 EP EP08782756A patent/EP2139464A1/fr not_active Withdrawn
- 2008-03-14 WO PCT/US2008/057054 patent/WO2008113000A1/fr not_active Ceased
- 2008-03-14 JP JP2009553813A patent/JP2010521492A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| JP2010521492A (ja) | 2010-06-24 |
| WO2008113000A1 (fr) | 2008-09-18 |
| EP2139464A1 (fr) | 2010-01-06 |
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