BG106732A - Фармацевтичен състав с антидиабетично действие и метод за лечение на диабет - Google Patents

Фармацевтичен състав с антидиабетично действие и метод за лечение на диабет Download PDF

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Publication number: BG106732A
Authority: BG; Bulgaria
Prior art keywords: metformin; glyburide; dose; diabetes; treatment
Prior art date: 1999-11-03

Application number

BG106732A

Other languages

Bulgarian (bg)

English (en)

Inventor

Beth PIPER

Original Assignee

Bristol-Myers Squibb Company

Priority date (The priority date 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 date listed.)

1999-11-03

Filing date

2002-05-22

Publication date

2003-02-28

Family has litigation

First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=23716278&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BG106732(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.

2002-05-22 Application filed by Bristol-Myers Squibb Company filed Critical Bristol-Myers Squibb Company

2003-02-28 Publication of BG106732A publication Critical patent/BG106732A/bg

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BG106732A 1999-11-03 2002-05-22 Фармацевтичен състав с антидиабетично действие и метод за лечение на диабет BG106732A (bg)

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US09/432,465 US6586438B2 (en)	1999-11-03	1999-11-03	Antidiabetic formulation and method
PCT/US2000/028467 WO2001032158A2 (en)	1999-11-03	2000-10-13	Pharmaceutical composition comprising a combination of metformin and another antidiabetic agent

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BG106732A true BG106732A (bg)	2003-02-28

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BG106733A BG65850B1 (bg)	1999-11-03	2002-05-22	Използване на фармацевтичен състав, съдържащ комбинация от метформин и глибенкламид
BG106732A BG106732A (bg)	1999-11-03	2002-05-22	Фармацевтичен състав с антидиабетично действие и метод за лечение на диабет

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BG106733A BG65850B1 (bg)	1999-11-03	2002-05-22	Използване на фармацевтичен състав, съдържащ комбинация от метформин и глибенкламид

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US (2)	US6586438B2 (et)
EP (1)	EP1253944A2 (et)
JP (2)	JP2003529551A (et)
KR (2)	KR100769786B1 (et)
CN (3)	CN101273981B (et)
AR (1)	AR026355A1 (et)
AU (1)	AU781781B2 (et)
BG (2)	BG65850B1 (et)
BR (1)	BR0015295A (et)
CA (1)	CA2389931A1 (et)
CZ (2)	CZ304090B6 (et)
DE (1)	DE60038455T2 (et)
EE (1)	EE05210B1 (et)
ES (1)	ES2302702T3 (et)
GE (2)	GEP20053539B (et)
HK (1)	HK1045655A1 (et)
HU (1)	HUP0300642A3 (et)
IL (3)	IL149138A0 (et)
LT (1)	LT5025B (et)
LV (1)	LV12907B (et)
MX (1)	MXPA02004290A (et)
MY (2)	MY136636A (et)
NO (1)	NO20022086L (et)
NZ (1)	NZ552074A (et)
PL (1)	PL366112A1 (et)
RO (1)	RO123109B1 (et)
RU (1)	RU2276604C2 (et)
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TN (2)	TNSN00207A1 (et)
TW (1)	TWI241185B (et)
UA (2)	UA75583C2 (et)
UY (1)	UY26425A1 (et)
WO (1)	WO2001032158A2 (et)
ZA (2)	ZA200203368B (et)

Families Citing this family (100)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US7235627B2 (en) *	1996-08-30	2007-06-26	Novo Nordisk A/S	Derivatives of GLP-1 analogs
US6528486B1 (en)	1999-07-12	2003-03-04	Zealand Pharma A/S	Peptide agonists of GLP-1 activity
US6414002B1 (en)	1999-09-22	2002-07-02	Bristol-Myers Squibb Company	Substituted acid derivatives useful as antidiabetic and antiobesity agents and method
US20030040469A1 (en) *	2000-03-08	2003-02-27	Knudsen Liselotte Bjerre	Lowering serum lipids
AU4116801A (en) *	2000-03-17	2001-09-24	Ajinomoto Kk	Drugs for complications of diabetes and neuropathy and utilization thereof
FR2816840B1 (fr)	2000-11-17	2004-04-09	Flamel Tech Sa	Medicament a base de microcapsules d'anti-hyperclycemiant a liberation prolongee et son procede de preparation
US7062312B2 (en) *	2001-01-17	2006-06-13	Pediamed Pharmaceuticals, Inc.	Combination and method including a visual marker for determining compliance with a medication regimen
US20020187926A1 (en) *	2001-03-07	2002-12-12	Knudsen Liselotte Bjerre	Combined use of derivatives of GLP-1 analogs and PPAR ligands
US20030022816A1 (en) *	2001-03-07	2003-01-30	Knudsen Liselotte Bjerre	Combined use of derivatives of GLP-1 analogs and PPAR ligands
FR2825023B1 (fr) *	2001-05-23	2005-04-15	Flamel Tech Sa	Forme pharmaceutique orale antidiabetique "une prise par jour"comprenant une biguanide et au moins un autre principe actif
HUP0402328A2 (hu) *	2001-09-28	2005-02-28	Sun Pharmaceutical Industries Limited	Diabétesz mellitusz kezelésére szolgáló gyógyszerkészítmény
US6924311B2 (en) *	2001-10-17	2005-08-02	X-Ceptor Therapeutics, Inc.	Methods for affecting various diseases utilizing LXR compounds
US7183321B2 (en) *	2001-12-17	2007-02-27	Bristol-Myers Squibb Company	Antidiabetic formulation and method
MXPA04007183A (es) *	2002-01-25	2006-03-06	Silanes Sa De Cv Lab	Composicion farmaceutica para el control de la glucosa en sangre de pacientes con diabetes tipo 2.
JP4732696B2 (ja)	2002-04-09	2011-07-27	フラメル・テクノロジー	活性成分の改変された放出のための、マイクロカプセルの水性懸濁液形態での経口医薬品製剤
EP1515701B1 (en)	2002-06-17	2014-09-17	Inventia Healthcare Private Limited	Process for the manufacture of multilayer tablet compositions comprising thiazolidinedione and biguanide
ATE432289T1 (de) *	2002-07-04	2009-06-15	Zealand Pharma As	Glp-1 und behandlungsmethode für diabetes
JP2004067575A (ja) *	2002-08-06	2004-03-04	Yaizu Suisankagaku Industry Co Ltd	糖尿病治療薬効果促進剤
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
SE526943C2 (sv) *	2002-08-26	2005-11-22	Indevex Ab	Födoämneskompositionsprodukt
UA80991C2 (en)	2002-10-07	2007-11-26		Solid preparation containing an insulin resistance improving drug and an active ingredient useful as a remedy for diabetes
US20040147564A1 (en) *	2003-01-29	2004-07-29	Rao Vinay U.	Combinations of glimepiride and the thiazolidinedione for treatment of diabetes
CA2536111A1 (en) *	2003-07-24	2005-02-03	Wockhardt Limited	Oral compositions for treatment of diseases
US20060241019A1 (en) *	2003-07-25	2006-10-26	Bridon Dominique P	Long lasting insulin derivatives and methods thereof
US20050202063A1 (en) *	2003-08-26	2005-09-15	Ebn International Kft	Food product
EP1732513A2 (en) *	2003-12-31	2006-12-20	Alpharma, Inc.	Rosiglitazone formulations
EP1841414A1 (en) *	2003-12-31	2007-10-10	Alpharma, Inc.	Rosiglitazone and metformin formulations
EP1746993A4 (en) *	2004-04-29	2007-08-29	Andrx Labs Llc	METFORMIN COMPOSITIONS WITH CONTROLLED RELEASE
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
KR100760430B1 (ko) *	2004-12-31	2007-10-04	한미약품 주식회사	당뇨병 치료제의 경구 투여용 서방성 복합 제제 및 이의제조 방법
US20060188590A1 (en) *	2005-01-05	2006-08-24	Mitsunori Ono	Compositions for treating diabetes or obesity
EP1891971A4 (en) *	2005-01-31	2010-02-03	Ajinomoto Kk	MEDICAL COMPOSITION USING HYPERGLY CRAB MEDICAMENT TO TREAT OR TREAT GLUCOSE-INTOLERANCE, BORDERLINE DIABETES, INSULIN RESISTANCE AND HYPERINSULINEMIA
JPWO2006126673A1 (ja) *	2005-05-27	2008-12-25	第一三共株式会社	組み合わせによる糖尿病治療薬
RU2308265C2 (ru) *	2005-07-25	2007-10-20	Илья Николаевич Медведев	Способ выбора лечения тромбоцитопатии при метаболическом синдроме
BRPI0620718A2 (pt) *	2005-10-28	2011-11-22	Takeda Pharmaceutical	agente para a proteção do páncreas, e, uso de uma droga para a redução de glicose
EP1968559A4 (en) *	2005-12-09	2013-08-07	Metaproteomics Llc	INFLAMMATORY BOTANICAL PRODUCTS FOR THE TREATMENT OF METABOLIC SYNDROME AND DIABETES
FR2896157B1 (fr) *	2006-01-13	2008-09-12	Merck Sante Soc Par Actions Si	Combinaison de derives de triazine et d'agents de stimulation de secretion d'insuline.
KR101452915B1 (ko)	2006-05-04	2014-10-21	베링거 인겔하임 인터내셔날 게엠베하	다형태
PE20080251A1 (es)	2006-05-04	2008-04-25	Boehringer Ingelheim Int	Usos de inhibidores de dpp iv
EP1852108A1 (en)	2006-05-04	2007-11-07	Boehringer Ingelheim Pharma GmbH & Co.KG	DPP IV inhibitor formulations
US20100008899A1 (en) *	2006-07-26	2010-01-14	Diamedica, Inc.	Methods of diagnosis and treatment for metabolic disorders
PE20140960A1 (es)	2008-04-03	2014-08-15	Boehringer Ingelheim Int	Formulaciones que comprenden un inhibidor de dpp4
US20100136561A1 (en) *	2008-05-16	2010-06-03	Interleukin Genetics, Inc.	Genetic Markers for Weight Management and Methods of Use Thereof
KR20190016601A (ko)	2008-08-06	2019-02-18	베링거 인겔하임 인터내셔날 게엠베하	메트포르민 요법이 부적합한 환자에서의 당뇨병 치료
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
KR101189639B1 (ko) *	2008-12-15	2012-10-12	씨제이제일제당 (주)	메트포르민 및 α-글리코시다제 억제제를 포함하는 경구 제제 및 그 제조방법
EP2732818B1 (en)	2009-03-31	2017-05-03	Ligand Pharmaceuticals Inc.	A biphenylsulfonamide endothelin and angiotensin ii receptor antagonist to treat glomerulosclerosis
SG10201605794PA (en)	2009-04-29	2016-09-29	Amarin Pharmaceuticals Ie Ltd	Stable Pharmaceutical Composition And Methods Of Using Same
WO2010127099A2 (en)	2009-04-29	2010-11-04	Amarin Corporation Plc	Pharmaceutical compositions comprising epa and a cardiovascular agent and methods of using the same
CN108096209A (zh)	2009-06-15	2018-06-01	阿马里纳制药公司	在相伴他汀类疗法的对象中降低甘油三酯、没有增加ldl-c水平的组合物和方法
US20110009347A1 (en)	2009-07-08	2011-01-13	Yin Liang	Combination therapy for the treatment of diabetes
KR20120107080A (ko)	2009-11-27	2012-09-28	베링거 인겔하임 인터내셔날 게엠베하	리나글립틴과 같은 ｄｐｐ－ｉｖ 억제제를 사용한 유전자형 검사된 당뇨병 환자의 치료
CN101810628B (zh) *	2010-04-13	2012-05-23	北京四环科宝制药有限公司	二甲双胍格列吡嗪片及其制备方法
AU2011247452B2 (en)	2010-04-27	2016-03-17	Zealand Pharma A/S	Peptide conjugates of GLP-1 receptor agonists and gastrin and their use
KR101927068B1 (ko)	2010-05-05	2018-12-10	베링거 인겔하임 인터내셔날 게엠베하	체중 감소 치료에 후속하는 dpp-4 억제제에 의한 순차적 병용 요법
NZ703128A (en)	2010-05-11	2016-04-29	Janssen Pharmaceutica Nv	Pharmaceutical formulations comprising 1 - (beta-d-glucopyranosyl) - 2 -thienylmethylbenzene derivatives as inhibitors of sglt
AR083878A1 (es)	2010-11-15	2013-03-27	Boehringer Ingelheim Int	Terapia antidiabetica vasoprotectora y cardioprotectora, linagliptina, metodo de tratamiento
EP2646013A4 (en)	2010-11-29	2014-03-26	Amarin Pharma Inc	Low eructation composition and methods for treating and/or preventing cardiovascular disease in a subject with fish allergy/hypersensitivity
WO2012090225A2 (en) *	2010-12-29	2012-07-05	Nutracryst Therapeutics Private Limited	Novel cocrystals / molecular salts of metformin with oleoylethanolamide as an effective anti-diabetic + anti- obesity agent
US11759441B2 (en)	2011-01-07	2023-09-19	Anji Pharmaceuticals 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
SI2661266T1 (sl)	2011-01-07	2021-01-29	Anji Pharma (Us) Llc	Terapije, na osnovi kemosenzoričnih receptorskih ligandov
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
US11974971B2 (en)	2011-01-07	2024-05-07	Anji Pharmaceuticals Inc.	Compositions and methods for treating metabolic disorders
MX2014005351A (es)	2011-11-03	2014-05-28	Zealand Pharma As	Conjugados de gastrina peptidicos de agonistas de receptor glp-1.
US11291643B2 (en)	2011-11-07	2022-04-05	Amarin Pharmaceuticals Ireland Limited	Methods of treating hypertriglyceridemia
BR112014016810A8 (pt)	2012-01-06	2017-07-04	Elcelyx Therapeutics Inc	composições e métodos para tratamento de distúrbios metabólicos
MX2014008190A (es)	2012-01-06	2015-02-04	Elcelyx Therapeutics Inc	Composiciones de biguanida y métodos para tratar transtornos metabólicos.
WO2013115742A1 (en) *	2012-01-31	2013-08-08	Mahmut Bilgic	Pharmaceutical composition comprising alpha-glucosidase inhibitor
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
JP6224084B2 (ja)	2012-05-14	2017-11-01	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	糸球体上皮細胞関連障害及び／又はネフローゼ症候群の治療に用いるｄｐｐ−４阻害薬としてのキサンチン誘導体
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
WO2013173923A1 (en)	2012-05-25	2013-11-28	Diamedica, Inc.	Formulations of human tissue kallikrein-1 for parenteral delivery and related methods
PT2854841T (pt)	2012-06-04	2017-05-15	Diamedica Inc	Isoformas de glicosilação da calicreína 1 em tecido humano
IN2015DN00544A (et)	2012-07-23	2015-06-26	Zealand Pharma As
TWI608013B (zh)	2012-09-17	2017-12-11	西蘭製藥公司	升糖素類似物
US20140187633A1 (en)	2012-12-31	2014-07-03	Amarin Pharmaceuticals Ireland Limited	Methods of treating or preventing nonalcoholic steatohepatitis and/or primary biliary cirrhosis
KR101336499B1 (ko) *	2013-03-06	2013-12-03	씨제이제일제당 (주)	당뇨병의 예방 또는 치료용 복합 조성물
US20140271841A1 (en)	2013-03-15	2014-09-18	Amarin Pharmaceuticals Ireland Limited	Pharmaceutical composition comprising eicosapentaenoic acid and derivatives thereof and a statin
US9585859B2 (en)	2013-10-10	2017-03-07	Amarin Pharmaceuticals Ireland Limited	Compositions and methods for lowering triglycerides without raising LDL-C levels in a subject on concomitant statin therapy
ES2688708T3 (es)	2013-10-17	2018-11-06	Zealand Pharma A/S	Análogos de glucagón acilados
US9988429B2 (en)	2013-10-17	2018-06-05	Zealand Pharma A/S	Glucagon analogues
US10131702B2 (en)	2013-11-06	2018-11-20	Zealand Pharma A/S	Glucagon-GLP-1-GIP triple agonist compounds
EP3065767B1 (en)	2013-11-06	2020-12-30	Zealand Pharma A/S	Gip-glp-1 dual agonist compounds and methods
JP6615109B2 (ja)	2014-02-28	2019-12-04	ベーリンガーインゲルハイムインターナショナルゲゼルシャフトミットベシュレンクテルハフツング	Ｄｐｐ−４阻害薬の医学的使用
WO2015195662A1 (en)	2014-06-16	2015-12-23	Amarin Pharmaceuticals Ireland Limited	Methods of reducing or preventing oxidation of small dense ldl or membrane polyunsaturated fatty acids
US10253078B2 (en)	2014-10-29	2019-04-09	Zealand Pharma A/S	GIP agonist compounds and methods
PL3283507T3 (pl)	2015-04-16	2020-05-18	Zealand Pharma A/S	Acylowany analog glukagonu
MX390363B (es)	2016-06-10	2025-03-20	Boehringer Ingelheim Int	Combinacion de linagliptina y metformina
SG11201903938XA (en)	2016-12-09	2019-05-30	Zealand Pharma As	Acylated glp-1/glp-2 dual agonists
AU2018230478B2 (en)	2017-03-09	2025-01-23	Diamedica Inc.	Dosage forms of tissue kallikrein 1
EP3675882A4 (en)	2017-08-30	2021-07-28	Pendulum Therapeutics, Inc.	METHODS AND COMPOSITIONS FOR THE TREATMENT OF MICROBIOMA ASSOCIATED DISORDERS
WO2020068827A1 (en) *	2018-09-24	2020-04-02	Pendulum Therapeutics, Inc.	Microbial compositions and methods of use
EP3700518A4 (en)	2018-09-24	2020-12-16	Amarin Pharmaceuticals Ireland Limited	METHODS OF REDUCING THE RISK OF CARDIOVASCULAR EVENTS IN A SUBJECT
CN114980973A (zh)	2019-11-12	2022-08-30	阿马里纳药物爱尔兰有限公司	降低心房纤颤和/或心房扑动受试者心血管事件风险的方法
CN113648318B (zh) *	2020-05-12	2023-08-25	中国科学院上海营养与健康研究所	增强细胞产热和治疗疾病的应用
EP4326244A4 (en)	2021-04-21	2025-03-19	Amarin Pharmaceuticals Ireland Limited	METHODS TO REDUCE THE RISK OF HEART FAILURE

Family Cites Families (30)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US3174901A (en)	1963-01-31	1965-03-23	Jan Marcel Didier Aron Samuel	Process for the oral treatment of diabetes
US4060634A (en)	1973-09-26	1977-11-29	Boehringer Mannheim G.M.B.H.	Rapidly resorbable glibenclamide
DE2348334C2 (de)	1973-09-26	1982-11-11	Boehringer Mannheim Gmbh, 6800 Mannheim	Neue Zubereitungsform des N-4-[2-(5-Chlor-2-methoxybenzamido)äthyl]- phenyl-sulfonyl-N'-cyclohexylharnstoffs
NO154918C (no)	1977-08-27	1987-01-14	Bayer Ag	Analogifremgangsmaate til fremstilling av terapeutisk aktive derivater av 3,4,5-trihydroksypiperidin.
EP0062704A1 (de)	1980-12-03	1982-10-20	Hoechst Aktiengesellschaft	Cyclopropancarbonsäureester-derivate als Mittel zum Bekämpfen von Magendasseln bei Equiden
JPS6051189A (ja)	1983-08-30	1985-03-22	Sankyo Co Ltd	チアゾリジン誘導体およびその製造法
US4916163A (en)	1985-06-04	1990-04-10	The Upjohn Company	Spray-dried lactose formulation of micronized glyburide
DE3543999A1 (de)	1985-12-13	1987-06-19	Bayer Ag	Hochreine acarbose
US5614492A (en)	1986-05-05	1997-03-25	The General Hospital Corporation	Insulinotropic hormone GLP-1 (7-36) and uses thereof
DE3833439A1 (de)	1988-10-01	1991-09-12	Hoechst Ag	Verfahren zur mikronisierung von glibenclamid
US5258185A (en) *	1989-08-23	1993-11-02	Bauer Kurt H	Highly active, rapidly absorbable formulations of glibenclamide, processes for the production thereof and their use
DK36392D0 (da)	1992-03-19	1992-03-19	Novo Nordisk As	Anvendelse af kemisk forbindelse
DE4323636A1 (de)	1993-07-15	1995-01-19	Hoechst Ag	Arzneistoffzubereitungen aus umhüllten, schwerstwasserlöslichen Arzneistoffen für Inhalationsarzneiformen und Verfahren zu ihrer Herstellung
TWI238064B (en)	1995-06-20	2005-08-21	Takeda Chemical Industries Ltd	A pharmaceutical composition for prophylaxis and treatment of diabetes
IT1276130B1 (it)	1995-11-14	1997-10-27	Gentili Ist Spa	Associazione glibenclamide-metformina, composizioni farmaceutiche che la contengono e loro uso nel trattamento del diabete mellito di tipo
US6011049A (en) *	1997-02-19	2000-01-04	Warner-Lambert Company	Combinations for diabetes
US6153632A (en)	1997-02-24	2000-11-28	Rieveley; Robert B.	Method and composition for the treatment of diabetes
WO1998055107A1 (en) *	1997-06-06	1998-12-10	Depomed, Inc.	Gastric-retentive oral drug dosage forms for controlled release of highly soluble drugs
JP2002500677A (ja)	1997-06-13	2002-01-08	ノボノルディスクアクティーゼルスカブ	新規ｎｉｄｄｍ療法
CZ298469B6 (cs)	1997-06-18	2007-10-10	Smithkline Beecham Plc	Farmaceutický prostredek obsahující 5-[4-/2-(N-methyl-N-(2-pyridyl)amino)ethoxy/benzyl]thiazolidin-2,4-dion a metformin, a lécivo pro lécení diabetesmellitus
GB9715306D0 (en)	1997-07-18	1997-09-24	Smithkline Beecham Plc	Novel method of treatment
JP2001520193A (ja)	1997-10-17	2001-10-30	アヴェンティスファーマシューティカルズプロダクツインコーポレイテッド	キノリン誘導体の治療的使用
DE69822505T2 (de)	1997-12-08	2005-01-20	Bristol-Myers Squibb Co.	Neue metformin-salze und verfahren
FR2774591B1 (fr)	1998-02-12	2000-05-05	Lipha	Composition pharmaceutique comprenant l'association metformine et fibrate et son utilisation pour la preparation de medicaments destines a reduire l'hyperglycemie
FI111167B (fi) *	1998-02-24	2003-06-13	Kemira Chemicals Oy	Menetelmä lietteen säilyvyyden parantamiseksi
WO1999043705A1 (en)	1998-02-27	1999-09-02	Novo Nordisk A/S	N-terminally truncated glp-1 derivatives
EP0974356B1 (en)	1998-07-15	2003-09-24	Merck Sante	Tablets comprising a combination of metformin and glibenclamide
CA2344309A1 (en)	1998-09-17	2000-03-23	Scott A. Biller	Method for treating diabetes employing an ap2 inhibitor and combination
CO5200844A1 (es)	1999-09-17	2002-09-27	Novartis Ag	Una combinacion que comprende nateglinida y cuando por menos otro compuesto antidiabetico usada para el tratamiento de desordenes metabolicos, especialmente diabetes, o de una enfermedad o condicion asociada con dibetes
EP2620443A1 (en)	2012-01-25	2013-07-31	Galecto Biotech AB	Novel galactoside inhibitors of galectins

1999
- 1999-11-03 US US09/432,465 patent/US6586438B2/en not_active Expired - Lifetime
- 1999-12-14 US US09/460,920 patent/US7598262B2/en not_active Expired - Lifetime
2000
- 2000-10-13 CN CN2008100817553A patent/CN101273981B/zh not_active Expired - Lifetime
- 2000-10-13 NZ NZ552074A patent/NZ552074A/en not_active IP Right Cessation
- 2000-10-13 KR KR1020027005673A patent/KR100769786B1/ko not_active Expired - Lifetime
- 2000-10-13 GE GE4802A patent/GEP20053539B/en unknown
- 2000-10-13 CZ CZ20021546A patent/CZ304090B6/cs not_active IP Right Cessation
- 2000-10-13 CZ CZ20021547A patent/CZ20021547A3/cs unknown
- 2000-10-13 BR BR0015295-1A patent/BR0015295A/pt not_active Application Discontinuation
- 2000-10-13 HU HU0300642A patent/HUP0300642A3/hu unknown
- 2000-10-13 IL IL14913800A patent/IL149138A0/xx active IP Right Grant
- 2000-10-13 EE EEP200200241A patent/EE05210B1/et not_active IP Right Cessation
- 2000-10-13 CN CNB008180288A patent/CN100386114C/zh not_active Expired - Lifetime
- 2000-10-13 JP JP2001534363A patent/JP2003529551A/ja active Pending
- 2000-10-13 KR KR1020027005677A patent/KR20020050253A/ko not_active Ceased
- 2000-10-13 CN CN2011101796999A patent/CN102283853A/zh active Pending
- 2000-10-13 ES ES00972122T patent/ES2302702T3/es not_active Expired - Lifetime
- 2000-10-13 PL PL00366112A patent/PL366112A1/xx not_active Application Discontinuation
- 2000-10-13 CA CA002389931A patent/CA2389931A1/en not_active Abandoned
- 2000-10-13 MX MXPA02004290A patent/MXPA02004290A/es not_active Application Discontinuation
- 2000-10-13 GE GE4798A patent/GEP20053538B/en unknown
- 2000-10-13 RO ROA200200560A patent/RO123109B1/ro unknown
- 2000-10-13 UA UA2002054481A patent/UA75583C2/uk unknown
- 2000-10-13 HK HK02107208.1A patent/HK1045655A1/zh unknown
- 2000-10-13 WO PCT/US2000/028467 patent/WO2001032158A2/en not_active Ceased
- 2000-10-13 EP EP00970913A patent/EP1253944A2/en not_active Withdrawn
- 2000-10-13 RU RU2002113764/15A patent/RU2276604C2/ru not_active IP Right Cessation
- 2000-10-13 AU AU80229/00A patent/AU781781B2/en not_active Ceased
- 2000-10-13 UA UA2002054480A patent/UA76706C2/uk unknown
- 2000-10-13 DE DE60038455T patent/DE60038455T2/de not_active Expired - Lifetime
- 2000-10-13 SK SK499-2002A patent/SK4992002A3/sk not_active Application Discontinuation
- 2000-10-24 MY MYPI20004995A patent/MY136636A/en unknown
- 2000-10-24 MY MYPI20004996A patent/MY125118A/en unknown
- 2000-10-27 TN TNTNSN00207A patent/TNSN00207A1/en unknown
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- 2000-10-27 TW TW089122629A patent/TWI241185B/zh not_active IP Right Cessation
- 2000-11-02 UY UY26425A patent/UY26425A1/es unknown
- 2000-11-03 AR ARP000105804A patent/AR026355A1/es unknown
2002
- 2002-04-15 IL IL149138A patent/IL149138A/en not_active IP Right Cessation
- 2002-04-15 IL IL149139A patent/IL149139A/en active IP Right Grant
- 2002-04-26 ZA ZA200203368A patent/ZA200203368B/xx unknown
- 2002-04-26 ZA ZA200203367A patent/ZA200203367B/xx unknown
- 2002-05-02 NO NO20022086A patent/NO20022086L/no unknown
- 2002-05-22 BG BG106733A patent/BG65850B1/bg unknown
- 2002-05-22 BG BG106732A patent/BG106732A/bg unknown
- 2002-05-24 LT LT2002062A patent/LT5025B/lt not_active IP Right Cessation
- 2002-06-03 LV LVP-02-93A patent/LV12907B/en unknown
2012
- 2012-09-25 JP JP2012211400A patent/JP2013028631A/ja not_active Withdrawn

Also Published As

Publication number	Publication date
EE05210B1 (et)	2009-10-15
TWI241185B (en)	2005-10-11
AR026355A1 (es)	2003-02-05
CN101273981A (zh)	2008-10-01
NO20022086D0 (no)	2002-05-02
BG65850B1 (bg)	2010-03-31
CN101273981B (zh)	2011-01-26
CZ304090B6 (cs)	2013-10-16
CA2389931A1 (en)	2001-05-10
HUP0300642A2 (hu)	2003-07-28
IL149139A (en)	2011-11-30
PL366112A1 (en)	2005-01-24
KR20020050253A (ko)	2002-06-26
DE60038455D1 (de)	2008-05-08
CN1414862A (zh)	2003-04-30
JP2013028631A (ja)	2013-02-07
KR20020057994A (ko)	2002-07-12
EP1253944A2 (en)	2002-11-06
MY125118A (en)	2006-07-31
LT2002062A (en)	2003-03-25
US6586438B2 (en)	2003-07-01
WO2001032158A2 (en)	2001-05-10
UA76706C2 (uk)	2006-09-15
IL149138A (en)	2007-12-03
CZ20021547A3 (cs)	2003-01-15
AU781781B2 (en)	2005-06-16
JP2003529551A (ja)	2003-10-07
LT5025B (lt)	2003-06-25
ES2302702T3 (es)	2008-08-01
BR0015295A (pt)	2003-06-24
SK4992002A3 (en)	2003-04-01
CN102283853A (zh)	2011-12-21
DE60038455T2 (de)	2009-04-23
UA75583C2 (uk)	2006-05-15
ZA200203367B (en)	2003-09-10
RO123109B1 (ro)	2010-11-30
BG106733A (bg)	2003-02-28
MY136636A (en)	2008-11-28
US7598262B2 (en)	2009-10-06
GEP20053538B (en)	2005-06-10
US20020183345A1 (en)	2002-12-05
HUP0300642A3 (en)	2006-05-29
US20020177602A1 (en)	2002-11-28
UY26425A1 (es)	2001-07-31
WO2001032158A3 (en)	2002-08-29
HK1045655A1 (zh)	2002-12-06
AU8022900A (en)	2001-05-14
IL149138A0 (en)	2002-11-10
ZA200203368B (en)	2003-09-02
TNSN00207A1 (en)	2005-11-10
RU2276604C2 (ru)	2006-05-20
NZ552074A (en)	2008-06-30
RU2002113764A (ru)	2004-03-20
MXPA02004290A (es)	2003-02-12
KR100769786B1 (ko)	2007-10-24
NO20022086L (no)	2002-06-24
TNSN00206A1 (en)	2005-11-10
LV12907B (en)	2003-08-20
EE200200241A (et)	2003-12-15
GEP20053539B (en)	2005-06-10
CN100386114C (zh)	2008-05-07

Publication	Publication Date	Title
BG106732A (bg)	2003-02-28	Фармацевтичен състав с антидиабетично действие и метод за лечение на диабет
AU780106B2 (en)	2005-03-03	Method for treating diabetes
JP2003519621A5 (et)	2007-11-29
AU8022900B2 (et)	2005-06-16