EA200900896A1 - Соединения-агонисты гетероциклических рецепторов (варианты), фармацевтическая композиция на их основе, способ лечения диабета и метаболических расстройств, способ стимулирования выработки инсулина (варианты) и способы снижения уровня глюкозы и триглицеридов в крови посредством указанных соединений - Google Patents

Соединения-агонисты гетероциклических рецепторов (варианты), фармацевтическая композиция на их основе, способ лечения диабета и метаболических расстройств, способ стимулирования выработки инсулина (варианты) и способы снижения уровня глюкозы и триглицеридов в крови посредством указанных соединений

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Publication number
EA200900896A1
EA200900896A1 EA200900896A EA200900896A EA200900896A1 EA 200900896 A1 EA200900896 A1 EA 200900896A1 EA 200900896 A EA200900896 A EA 200900896A EA 200900896 A EA200900896 A EA 200900896A EA 200900896 A1 EA200900896 A1 EA 200900896A1
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EA
Eurasian Patent Office
Prior art keywords
variants
methods
triglycerides
agonists
blood
Prior art date
Application number
EA200900896A
Other languages
English (en)
Other versions
EA016720B1 (ru
Inventor
Син Чэнь
Пэн Чэн
Л. Эдвард Клеменс
Джефри Д. Джонсон
Цзянюань Ма
Элисон Мерфи
Имад Нашашиби
Кристофер Дж. Рэббэт
Цзянгао Сон
Мария Е. Уилсон
Янь Чжу
Чжухунь Чжао
Original Assignee
Метаболэкс, Инк.
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Publication date
Application filed by Метаболэкс, Инк. filed Critical Метаболэкс, Инк.
Publication of EA200900896A1 publication Critical patent/EA200900896A1/ru
Publication of EA016720B1 publication Critical patent/EA016720B1/ru

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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
    • A61K31/495—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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/38—Nitrogen atoms
    • C07D277/42—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Abstract

Предлагаются соединения и способы лечения, в том числе, диабета типа II и других заболеваний, связанных с недостаточным гликемическим контролем. Соединения изобретения являются перорально активными.
EA200900896A 2006-12-28 2007-12-27 Соединения-агонисты гетероциклических рецепторов (варианты), фармацевтическая композиция на их основе, способ лечения диабета и метаболических расстройств, способ стимулирования выработки инсулина (варианты) и способы снижения уровня глюкозы и триглицеридов в крови посредством указанных соединений EA016720B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US87790306P 2006-12-28 2006-12-28
US11/964,461 US7638541B2 (en) 2006-12-28 2007-12-26 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine
PCT/US2007/088978 WO2008083238A2 (en) 2006-12-28 2007-12-27 Heterocyclic receptor agonists for the treatment of diabetes and metabolic disorders

Publications (2)

Publication Number Publication Date
EA200900896A1 true EA200900896A1 (ru) 2010-04-30
EA016720B1 EA016720B1 (ru) 2012-07-30

Family

ID=39589206

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200900896A EA016720B1 (ru) 2006-12-28 2007-12-27 Соединения-агонисты гетероциклических рецепторов (варианты), фармацевтическая композиция на их основе, способ лечения диабета и метаболических расстройств, способ стимулирования выработки инсулина (варианты) и способы снижения уровня глюкозы и триглицеридов в крови посредством указанных соединений

Country Status (14)

Country Link
US (8) US7638541B2 (ru)
EP (1) EP2111107B1 (ru)
JP (1) JP5455645B2 (ru)
KR (1) KR101539308B1 (ru)
AU (1) AU2007339772B9 (ru)
BR (1) BRPI0720675A2 (ru)
CA (1) CA2672725C (ru)
EA (1) EA016720B1 (ru)
ES (1) ES2405105T3 (ru)
HK (1) HK1136943A1 (ru)
IL (1) IL199397A (ru)
MX (1) MX2009007023A (ru)
NZ (1) NZ577996A (ru)
WO (1) WO2008083238A2 (ru)

Families Citing this family (99)

* Cited by examiner, † Cited by third party
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
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
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
PE20080251A1 (es) 2006-05-04 2008-04-25 Boehringer Ingelheim Int Usos de inhibidores de dpp iv
EP2540725A1 (de) 2006-05-04 2013-01-02 Boehringer Ingelheim International GmbH Polymorphe von 1-((4-Methyl-chinazolin-2-yl)methyl)-3-methyl-7-(2-butin-1-yl)-8-(3-(R)-amino-piperidin-1-yl)xanthin
EP1852108A1 (en) 2006-05-04 2007-11-07 Boehringer Ingelheim Pharma GmbH & Co.KG DPP IV inhibitor formulations
GB0610746D0 (en) * 2006-06-01 2006-07-12 Prosidion Ltd Method of treatment
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
BRPI0808775A2 (pt) * 2007-03-08 2017-05-30 Irm Llc compostos e composições como moduladores de atividade de gpr119
US7751907B2 (en) 2007-05-24 2010-07-06 Smiths Medical Asd, Inc. Expert system for insulin pump therapy
US8221345B2 (en) 2007-05-30 2012-07-17 Smiths Medical Asd, Inc. Insulin pump based expert system
US8183381B2 (en) * 2007-07-19 2012-05-22 Metabolex Inc. N-linked heterocyclic receptor agonists for the treatment of diabetes and metabolic disorders
DE102007047735A1 (de) * 2007-10-05 2009-04-09 Merck Patent Gmbh Thiazolderivate
US20090177147A1 (en) 2008-01-07 2009-07-09 Michael Blomquist Insulin pump with insulin therapy coaching
MX2010010562A (es) * 2008-03-31 2010-12-07 Metabolex Inc Compuestos de oximetilen-arilo y uso de los mismos.
PE20140960A1 (es) 2008-04-03 2014-08-15 Boehringer Ingelheim Int Formulaciones que comprenden un inhibidor de dpp4
EP2303859A4 (en) * 2008-06-20 2012-08-22 Metabolex Inc ARYL GPR119 AGONISTS AND USES THEREOF
JPWO2010013849A1 (ja) * 2008-08-01 2012-01-12 日本ケミファ株式会社 Ｇｐｒ１１９作動薬
KR20190016601A (ko) 2008-08-06 2019-02-18 베링거 인겔하임 인터내셔날 게엠베하 메트포르민 요법이 부적합한 환자에서의 당뇨병 치료
UY32030A (es) 2008-08-06 2010-03-26 Boehringer Ingelheim Int "tratamiento para diabetes en pacientes inapropiados para terapia con metformina"
RU2011113823A (ru) * 2008-09-10 2012-10-20 БЕРИНГЕР ИНГЕЛЬХАЙМ ИНТЕРНАЦИОНАЛЬ ГмбХ (DE) Комбинированная терапия, предназначенная для лечения диабета и связанных с ним состояний
JP5785495B2 (ja) * 2008-10-01 2015-09-30 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ 植物保護剤としてのヘテロシクリル置換チアゾール類
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
US20110160222A1 (en) * 2008-11-26 2011-06-30 Metabolex, Inc. Modulators of glucose homeostasis for the treatment of diabetes and metabolic disorders
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
TW201036975A (en) 2009-01-07 2010-10-16 Boehringer Ingelheim Int Treatment for diabetes in patients with inadequate glycemic control despite metformin therapy
AR076936A1 (es) 2009-06-02 2011-07-20 Vitae Pharmaceuticals Inc Inhibidores de carbamato y urea de la 11 beta hidroxiesteroide deshidrogenasa 1
SG176865A1 (en) * 2009-06-18 2012-01-30 Cadila Healthcare Ltd Novel gpr 119 agonists
EP2272846A1 (de) * 2009-06-23 2011-01-12 Bayer CropScience AG Thiazolylpiperidin Derivate als Fungizide
JP2012530758A (ja) 2009-06-24 2012-12-06 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 新規化合物、医薬組成物及びそれに関する方法
NZ596445A (en) 2009-06-24 2013-04-26 Boehringer Ingelheim Int New compounds, pharmaceutical composition and methods relating thereto
JP2011006366A (ja) * 2009-06-26 2011-01-13 Sanwa Kagaku Kenkyusho Co Ltd 新規チオフェンカルボキサミド誘導体及びその医薬用途
AR077638A1 (es) * 2009-07-15 2011-09-14 Lilly Co Eli Compuesto de (metanosulfonil -piperidin )-( alcoxi-aril) -tetrahidro- piridina , composicion farmaceutica que lo comprende y su uso para preparar un medicamento util para el tratamiento de diabetes u obesidad
ES2497566T3 (es) * 2009-10-01 2014-09-23 Cymabay Therapeutics, Inc. Sales de tetrazol-1-il-fenoximetil-tiazol-2-il-piperidinil-pirimidina sustituida
JP5827626B2 (ja) * 2009-10-30 2015-12-02 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ ヘテロアリールピペリジン及びピペラジン誘導体
NZ599298A (en) 2009-11-27 2014-11-28 Boehringer Ingelheim Int Treatment of genotyped diabetic patients with dpp-iv inhibitors such as linagliptin
US8882701B2 (en) 2009-12-04 2014-11-11 Smiths Medical Asd, Inc. Advanced step therapy delivery for an ambulatory infusion pump and system
JP2013047188A (ja) * 2009-12-24 2013-03-07 Nippon Chemiphar Co Ltd Ｇｐｒ１１９作動薬
WO2011093501A1 (ja) 2010-02-01 2011-08-04 日本ケミファ株式会社 Ｇｐｒ１１９作動薬
WO2011107494A1 (de) 2010-03-03 2011-09-09 Sanofi Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung
WO2011113947A1 (en) 2010-03-18 2011-09-22 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
GB201006166D0 (en) 2010-04-14 2010-05-26 Prosidion Ltd Compounds for the treatment of metabolic disorders
GB201006167D0 (en) 2010-04-14 2010-05-26 Prosidion Ltd Compounds for the treatment of metabolic disorders
JP6034781B2 (ja) 2010-05-05 2016-11-30 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 併用療法
GB2488360A (en) * 2011-02-25 2012-08-29 Prosidion Ltd Heterocyclic GPCR agonists
TW201209054A (en) 2010-05-28 2012-03-01 Prosidion Ltd Novel compounds
WO2011153435A1 (en) * 2010-06-04 2011-12-08 Metabolex, Inc. Preparation of 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine
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
EP2585048B1 (en) * 2010-06-23 2018-04-11 CymaBay Therapeutics, Inc. Compositions of 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine
EP3725325B1 (en) 2010-06-24 2023-05-31 Boehringer Ingelheim International GmbH Diabetes therapy
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
TW201215388A (en) 2010-07-05 2012-04-16 Sanofi Sa (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments
DK2625177T3 (en) 2010-10-08 2015-10-12 Cadila Healthcare Ltd New GPR 119 agonists
US9034883B2 (en) 2010-11-15 2015-05-19 Boehringer Ingelheim International Gmbh Vasoprotective and cardioprotective antidiabetic therapy
WO2012086735A1 (ja) * 2010-12-22 2012-06-28 大正製薬株式会社 縮合複素環化合物
WO2012170867A1 (en) 2011-06-09 2012-12-13 Rhizen Pharmaceuticals Sa Novel compounds as modulators of gpr-119
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
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
CN104350051B (zh) * 2011-11-23 2017-03-08 德克萨斯大学系统董事会 用于糖尿病的异噁唑治疗剂
US9555001B2 (en) 2012-03-07 2017-01-31 Boehringer Ingelheim International Gmbh Pharmaceutical composition and uses thereof
AU2013251683A1 (en) 2012-04-26 2014-12-18 Bristol-Myers Squibb Company Imidazothiadiazole derivatives as protease activated receptor 4 (PAR4) inhibitors for treating platelet aggregation
WO2013163241A1 (en) 2012-04-26 2013-10-31 Bristol-Myers Squibb Company Imidazothiadiazole and imidazopyridazine derivatives as protease activated receptor 4 (par4) inhibitors for treating platelet aggregation
EP3243826B1 (en) 2012-04-26 2019-10-30 Bristol-Myers Squibb Company Imidazothiadiazole and imidazopyrazine derivatives as protease activated receptor 4 (par4) inhibitors for treating platelet aggregation
EP2849755A1 (en) 2012-05-14 2015-03-25 Boehringer Ingelheim International GmbH A xanthine derivative as dpp -4 inhibitor for use in the treatment of podocytes related disorders and/or nephrotic syndrome
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
US9238100B2 (en) 2012-06-07 2016-01-19 Tandem Diabetes Care, Inc. Device and method for training users of ambulatory medical devices
JP6527520B2 (ja) 2013-12-17 2019-06-05 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ ピルビン酸脱水素酵素キナーゼの阻害剤としてのｎ１−（３，３，３−トリフルオロ−２−ヒドロキソ−２−メチルプロピオニル）−ピペリジン誘導体
WO2015101958A2 (en) * 2014-01-06 2015-07-09 Rhizen Pharmaceuticals Sa Novel inhibitors of glutaminase
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
KR101651505B1 (ko) 2014-05-02 2016-08-29 현대약품 주식회사 싸이클로 헥센 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 대사성 질환의 예방 또는 치료용 약학적 조성물
CN107074805B (zh) 2014-07-03 2021-02-26 德州大学系统董事会 用于治疗疾病的gls1抑制剂
SI3300500T1 (sl) 2015-05-20 2020-07-31 Amgen Inc. Triazolni agonisti receptorja APJ
CA2990457A1 (en) * 2015-06-30 2017-01-05 Board Of Regents, University Of Texas System Pyrrolidinyl and piperidinyl derivatives and pharmaceutical compositions thereof useful as gls1 inhibitors
WO2017078352A1 (en) 2015-11-04 2017-05-11 Hyundai Pharm Co., Ltd. Cyclohexene derivative, preparation method thereof, and pharmaceutical composition for preventing or treating metabolic disease comprising the same as active ingredient
JP6976248B2 (ja) 2015-12-22 2021-12-08 ボード オブ リージェンツ、ザ ユニバーシテイ オブ テキサス システム （ｒ）−１−（４−（６−（２−（４−（３，３−ジフルオロシクロブトキシ）−６−メチルピリジン−２−イル）アセトアミド）ピリダジン−３−イル）−２−フルオロブチル）−ｎ−メチル−１ｈ−１，２，３−トリアゾール−４−カルボキサミドの塩形態および多形体
US10569016B2 (en) 2015-12-29 2020-02-25 Tandem Diabetes Care, Inc. System and method for switching between closed loop and open loop control of an ambulatory infusion pump
WO2017167676A1 (en) 2016-03-29 2017-10-05 Merck Patent Gmbh N1-(3,3,3-trifluoro-2-hydroxy-2-methylpropionyl)-piperidine derivatives as inhibitors of pyruvate dehydrogenase kinase
CN109071490B (zh) 2016-04-28 2021-04-06 默克专利股份公司 哌啶基衍生物
US9988369B2 (en) 2016-05-03 2018-06-05 Amgen Inc. Heterocyclic triazole compounds as agonists of the APJ receptor
BR112018075484A2 (pt) * 2016-06-09 2019-03-19 Pramana Pharmaceuticals Inc. compostos contendo benzo[d][1,3]oxatiol, 3-óxido de benzo[d][1,3]oxatiol ou 3,3-dióxido de benzo[d][1,3]oxatiol e métodos/usos dos mesmos como agonistas do receptor 119 acoplado a proteína g
CA3022202A1 (en) 2016-06-10 2017-12-14 Boehringer Ingelheim International Gmbh Combinations of linagliptin and metformin
KR20190035752A (ko) 2016-08-03 2019-04-03 사이머베이 쎄라퓨틱스, 인코퍼레이티드 염증성 위장 질환 또는 위장 상태를 치료하기 위한 옥시메틸렌 아릴 화합물
EP3541810B1 (en) 2016-11-16 2020-12-23 Amgen Inc. Triazole phenyl compounds as agonists of the apj receptor
US11020395B2 (en) 2016-11-16 2021-06-01 Amgen Inc. Cycloalkyl substituted triazole compounds as agonists of the APJ receptor
US10736883B2 (en) 2016-11-16 2020-08-11 Amgen Inc. Triazole furan compounds as agonists of the APJ receptor
EP3541805B1 (en) 2016-11-16 2020-10-14 Amgen Inc. Heteroaryl-substituted triazoles as apj receptor agonists
US10689367B2 (en) 2016-11-16 2020-06-23 Amgen Inc. Triazole pyridyl compounds as agonists of the APJ receptor
WO2018093576A1 (en) 2016-11-16 2018-05-24 Amgen Inc. Alkyl substituted triazole compounds as agonists of the apj receptor
EP3697764A4 (en) 2017-10-18 2021-07-21 Board Of Regents, The University Of Texas System GLUTAMINASE INHIBITOR THERAPY
US11149040B2 (en) 2017-11-03 2021-10-19 Amgen Inc. Fused triazole agonists of the APJ receptor
MA52487A (fr) 2018-05-01 2021-03-10 Amgen Inc Pyrimidinones substituées en tant qu'agonistes du récepteur apj
CA3121202A1 (en) 2018-11-30 2020-06-04 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
JP2023526625A (ja) 2020-05-19 2023-06-22 キャリーオペ，インク． Ａｍｐｋアクチベーター
CA3183575A1 (en) 2020-06-26 2021-12-30 Iyassu Sebhat Ampk activators

Family Cites Families (134)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3108117A (en) 1959-02-12 1963-10-22 Mead Johnson & Co 3-benzyl-1, 2-diloweralkyl-3-pyrrolidinols
US3778443A (en) * 1969-02-13 1973-12-11 Ciba Geigy Ag 4-tetrahydro pyridyl,hydroxy alkyl pyrazoles
US3536809A (en) * 1969-02-17 1970-10-27 Alza Corp Medication method
US3598123A (en) * 1969-04-01 1971-08-10 Alza Corp Bandage for administering drugs
US3845770A (en) * 1972-06-05 1974-11-05 Alza Corp Osmatic dispensing device for releasing beneficial agent
GB1422263A (en) 1973-01-30 1976-01-21 Ferrosan As 4-phenyl-piperidine compounds
US3916899A (en) * 1973-04-25 1975-11-04 Alza Corp Osmotic dispensing device with maximum and minimum sizes for the passageway
DE2701705A1 (de) 1976-01-28 1977-08-04 Sandoz Ag Neue organische verbindungen, ihre verwendung und herstellung
US4008719A (en) * 1976-02-02 1977-02-22 Alza Corporation Osmotic system having laminar arrangement for programming delivery of active agent
CA1146866A (en) * 1979-07-05 1983-05-24 Yamanouchi Pharmaceutical Co. Ltd. Process for the production of sustained release pharmaceutical composition of solid medical material
DE3438830A1 (de) * 1984-10-23 1986-04-30 Rentschler Arzneimittel Nifedipin enthaltende darreichungsform und verfahren zu ihrer herstellung
US5013556A (en) * 1989-10-20 1991-05-07 Liposome Technology, Inc. Liposomes with enhanced circulation time
EP0580860B2 (en) * 1991-04-16 2004-12-15 Nippon Shinyaku Company, Limited Method of manufacturing solid dispersion
US5817667A (en) 1991-04-17 1998-10-06 University Of Georgia Research Foudation Compounds and methods for the treatment of cancer
US5187677A (en) 1991-08-23 1993-02-16 Hewlett-Packard Company Waveform synthesizer through simulating multiplication
US5340591A (en) * 1992-01-24 1994-08-23 Fujisawa Pharmaceutical Co., Ltd. Method of producing a solid dispersion of the sparingly water-soluble drug, nilvadipine
JP3265680B2 (ja) * 1992-03-12 2002-03-11 大正製薬株式会社 経口製剤用組成物
AU4444393A (en) 1992-09-01 1994-03-10 Zeneca Limited Pyrrolidine derivatives
GB9310713D0 (en) 1993-05-24 1993-07-07 Zeneca Ltd Aryl substituted heterocycles
WO1996021661A1 (en) 1995-01-12 1996-07-18 Glaxo Group Limited Piperidine derivatives having tachykinin antagonist activity
HU226635B1 (en) 1995-01-23 2009-05-28 Asubio Pharma Co Piperidine and piperazine derivatives, medicines containing them as active ingredient and their use
DE19504832A1 (de) * 1995-02-14 1996-08-22 Basf Ag Feste Wirkstoff-Zubereitungen
DE19519496A1 (de) 1995-05-27 1996-11-28 Lau Matthias Dipl Ing Sauerstoffsensitives Einschichtsystem und Verfahren zur Anordnung des Systems
KR100384979B1 (ko) 1995-09-07 2003-10-17 에프. 호프만-라 로슈 아게 심부전증및신부전증치료용의신규한4-(옥시알콕시페닐)-3-옥시-피페리딘
US5792769A (en) 1995-09-29 1998-08-11 3-Dimensional Pharmaceuticals, Inc. Guanidino protease inhibitors
EP0858457A1 (de) 1995-10-20 1998-08-19 Dr. Karl Thomae GmbH 5-gliedrige heterocyclen, diese verbindungen enthaltende arzneimittel und deren verwendung sowie verfahren zu ihrer herstellung
KR100537843B1 (ko) 1996-07-22 2006-04-28 다이이치 아스비오파마 가부시키가이샤 아릴피페리디놀및아릴피페리딘유도체및이들을함유하는약제
EP0915875B1 (en) 1996-07-25 2003-04-09 MERCK SHARP & DOHME LTD. Substituted triazolo-pyridazine derivatives as ligands for gaba receptors
US5880138A (en) 1996-10-01 1999-03-09 Eli Lilly And Company NMDA receptor selective antagonists
IT1297894B1 (it) 1997-07-23 1999-12-20 C T A Srl Apparecchiatura automatica per il lavaggio, disinfezione, asciugatura e stimolazione dei capezzoli di animali da latte.
ES2287971T3 (es) 1997-08-11 2007-12-16 Pfizer Products Inc. Dispersiones farmaceuticas solidas con biodisponibilidad incrementada.
DE69941777D1 (de) * 1998-03-10 2010-01-21 Ono Pharmaceutical Co Carbonsäurederivate und medikamente die diese als aktiven wirkstoff enthalten
US6274735B1 (en) 1998-08-10 2001-08-14 Hoffmann-La Roche Inc. Process and intermediates for preparation of substituted piperidines
IT1303737B1 (it) 1998-11-11 2001-02-23 Smithkline Beecham Spa Derivati fenilpiperidinici procedimento per la loro preparazione eloro uso come ligandi del recettore orl-1.
KR100926209B1 (ko) 1998-11-20 2009-11-09 아레나 파마슈티칼스, 인크. 사람의 오르판 ｇ 단백질 커플링 수용체
US20030017528A1 (en) 1998-11-20 2003-01-23 Ruoping Chen Human orphan G protein-coupled receptors
US6221660B1 (en) 1999-02-22 2001-04-24 Synaptic Pharmaceutical Corporation DNA encoding SNORF25 receptor
CZ20013248A3 (cs) 1999-03-15 2002-04-17 Axys Pharmaceuticals, Inc. Nové sloučeniny a prostředky jako inhibitory proteázy
GB9912416D0 (en) 1999-05-28 1999-07-28 Pfizer Ltd Compounds useful in therapy
US6015712A (en) 1999-07-19 2000-01-18 Isis Pharmaceuticals Inc. Antisense modulation of FADD expression
AR035016A1 (es) * 1999-08-25 2004-04-14 Takeda Chemical Industries Ltd Composicion de azol promotor de produccion/secrecion de neurotrofina, compuesto prodroga del mismo, composicion farmaceutica que lo comprende y uso del mismo para preparar esta ultima.
GB9923177D0 (en) 1999-09-30 1999-12-01 Pfizer Ltd Novel polypeptide
IL139073A0 (en) 1999-10-21 2001-11-25 Pfizer Treatment of neuropathy
EP1176147A1 (en) 2000-07-28 2002-01-30 Pfizer Limited Process for the preparation of pyrazolo[4,3-d]pyrimidin-7-ones and intermediates thereof
US6770645B2 (en) 2001-03-16 2004-08-03 Pfizer Inc. Pharmaceutically active compounds
US6784185B2 (en) 2001-03-16 2004-08-31 Pfizer Inc. Pharmaceutically active compounds
AU2002256418A1 (en) 2001-04-27 2002-11-11 Vertex Pharmaceuticals Incorporated Inhibitors of bace
US20030003157A1 (en) 2001-06-06 2003-01-02 University Of Medicine & Dentistry Of New Jersey Collagen compositions and methods for making and using the same
US7262185B2 (en) 2001-08-08 2007-08-28 Takeda Chemical Industries Ltd. Benzazepine derivative, process for producing the same, and use
AU2003224632A1 (en) 2002-03-01 2003-09-16 Smithkline Beecham Corporation Hppars activators
WO2003091216A1 (fr) 2002-04-25 2003-11-06 Sumitomo Pharmaceuticals Co., Ltd. Nouveaux derives de piperidine
US7091232B2 (en) 2002-05-21 2006-08-15 Allergan, Inc. 4-(substituted cycloalkylmethyl) imidazole-2-thiones, 4-(substituted cycloalkenylmethyl) imidazole-2-thiones, 4-(substituted cycloalkylmethyl) imidazol-2-ones and 4-(substituted cycloalkenylmethyl) imidazol-2-ones and related compounds
CA2491191C (en) 2002-07-15 2014-02-04 Exelixis, Inc. Receptor-type kinase modulators and methods of use
GB0224919D0 (en) * 2002-10-25 2002-12-04 Pfizer Ltd Triazole compounds useful in therapy
US7084145B2 (en) * 2002-10-25 2006-08-01 Pfizer Inc. Triazole compounds useful in therapy
GB0230162D0 (en) 2002-12-24 2003-02-05 Metris Therapeutics Ltd Compounds useful in inhibiting angiogenesis
PL378295A1 (pl) 2003-02-24 2006-03-20 Arena Pharmaceuticals, Inc. Podstawione pochodne arylowe i heteroarylowe jako modulatory metabolizmu glukozy oraz profilaktyka i leczenie zaburzeń tego metabolizmu
ATE332210T1 (de) 2003-03-05 2006-07-15 Maus Spa Verfahren zum bearbeiten von bremsscheiben
GB0308333D0 (en) 2003-04-10 2003-05-14 Glaxo Group Ltd Novel compounds
CA2525325A1 (en) 2003-05-01 2004-11-18 Abbott Laboratories Pyrazole-amides and sulfonamides as sodium channel modulators
US20040220170A1 (en) 2003-05-01 2004-11-04 Atkinson Robert N. Pyrazole-amides and sulfonamides as sodium channel modulators
ES2350837T3 (es) 2003-05-01 2011-01-27 Bristol-Myers Squibb Company Compuestos de pirazol-amida sustituidos con arilo útiles como inhibidores de quinasas.
AU2004249698A1 (en) 2003-06-13 2004-12-29 Schering Aktiengesellschaft Quinolyl amide derivatives as CCR-5 antagonists
SG144942A1 (en) 2003-07-14 2008-08-28 Arena Pharm Inc Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
MXPA06000554A (es) 2003-07-14 2006-07-03 Arena Pharm Inc Derivados arilo y heteroarilo fusionados como moduladores del metabolismo y la profilaxis y tratamiento de trastornos relacionados con los mismos.
KR20060036105A (ko) 2003-07-29 2006-04-27 제논 파마슈티칼스 인크. 피리딜 유도체 및 그의 치료제로서의 용도
FR2862647B1 (fr) 2003-11-25 2008-07-04 Aventis Pharma Sa Derives de pyrazolyle, procede de preparation et intermediaires de ce procede a titre de medicaments et de compositions pharmaceutiques les renfermant
US7235641B2 (en) 2003-12-22 2007-06-26 Micromet Ag Bispecific antibodies
NZ547965A (en) 2003-12-24 2009-12-24 Prosidion Ltd 1,2,4-Oxadiazole derivatives as GPCR receptor agonists
TW200538433A (en) 2004-02-24 2005-12-01 Irm Llc Immunosuppressant compounds and compositiions
JP4787529B2 (ja) 2004-04-09 2011-10-05 大塚製薬株式会社 医薬組成物
US20080306114A1 (en) * 2004-04-13 2008-12-11 Arena Pharmaceuticals, Inc Human G Protein-Coupled Receptor and Modulators Thereof for the Treatment of Hyperglycemia and Related Disorders
US8710232B2 (en) 2004-04-22 2014-04-29 Sanofi-Aventis Deutschland Gmbh Imidazole derivatives used as TAFIa inhibitors
DE102004020186A1 (de) 2004-04-22 2005-11-17 Aventis Pharma Deutschland Gmbh Heterocyclylessigsäuren als Inhibitoren von TAFla
PL1773772T3 (pl) 2004-06-08 2010-11-30 Nsab Filial Af Neurosearch Sweden Ab Sverige Nowe dwupodstawione fenylopiperydyny/piperazyny jako modulatory neurotransmisji dopaminy
ES2378177T3 (es) 2004-10-29 2012-04-09 Zeria Pharmaceutical Co., Ltd. Derivado de carbazol, solvato del mismo o sal del mismo farmaceúticamente aceptable
TW200633990A (en) * 2004-11-18 2006-10-01 Takeda Pharmaceuticals Co Amide compound
JPWO2006057448A1 (ja) 2004-11-26 2008-06-05 武田薬品工業株式会社 アリールアルカン酸誘導体
EP1841760B1 (en) 2004-12-30 2011-08-10 Exelixis, Inc. Pyrimidine derivatives as kinase modulators and method of use
GB0428526D0 (en) 2004-12-30 2005-02-09 Novartis Ag Organic compounds
WO2006073167A1 (ja) * 2005-01-07 2006-07-13 Ono Pharmaceutical Co., Ltd. ピロリジン誘導体
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
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
US8277495B2 (en) 2005-01-13 2012-10-02 Candela Corporation Method and apparatus for treating a diseased nail
KR20070107040A (ko) 2005-02-16 2007-11-06 쉐링 코포레이션 Ｃｘｃｒ3 길항제 활성을 갖는 헤테로아릴-치환된피라지닐-피페라진-피페리딘
GB0504850D0 (en) 2005-03-09 2005-04-13 Novartis Ag Organic compounds
US20060206074A1 (en) 2005-03-11 2006-09-14 The Procter & Gamble Company Absorbent core structures having undulations
EP1707202A1 (de) 2005-03-31 2006-10-04 Speedel Experimenta AG Organische Verbindungen
KR100712289B1 (ko) 2005-04-07 2007-04-27 삼성에스디아이 주식회사 평판표시장치 및 그의 제조방법
EP1888529A2 (en) 2005-05-18 2008-02-20 Wyeth 3-cyanoquinoline inhibitors of tpl2 kinase and methods of making and using the same
WO2006133216A2 (en) * 2005-06-06 2006-12-14 Smithkline Beecham Corporation 4-substituted arylamine derivatives and their use in pharmaceutical compositions
CA2611216A1 (en) 2005-06-15 2006-12-21 Pfizer Limited 3-phenylazetidine derivatives as dopamine agonists
US20090018123A1 (en) 2005-06-20 2009-01-15 Milind D Sindkhedkar Oxazolidinones Bearing Antimicrobial Activity Composition and Methods of Preparation
JP5114395B2 (ja) 2005-06-30 2013-01-09 プロシディオン・リミテッド Ｇｐｃｒアゴニスト
EP1907384A2 (en) 2005-06-30 2008-04-09 Prosidion Limited Gpcr agonists
TW200738701A (en) 2005-07-26 2007-10-16 Du Pont Fungicidal carboxamides
JP2007045752A (ja) 2005-08-10 2007-02-22 Takeda Chem Ind Ltd ５員芳香族複素環誘導体、その製造法および用途
ES2326391T3 (es) 2005-09-16 2009-10-08 Arena Pharmaceuticals, Inc. Moduladores del metabolismo y el tratamiento de trastornos relacionados con el mismo.
WO2007039177A2 (en) 2005-09-29 2007-04-12 Sanofi-Aventis Phenyl- and pyridinyl- 1, 2 , 4 - oxadiazolone derivatives, processes for their preparation and their use as pharmaceuticals
JP5201817B2 (ja) * 2005-10-28 2013-06-05 大塚製薬株式会社 医薬組成物
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
PE20080069A1 (es) 2006-05-15 2008-02-22 Merck & Co Inc Compuestos biciclicos como agonistas del receptor 40 acoplado a proteina g (gpr40)
FR2902767B1 (fr) 2006-06-22 2008-09-19 J P B Creations Sa Dispositif de conditionnement d'un produit a base de colle
WO2007147843A2 (en) 2006-06-23 2007-12-27 Ciba Holding Inc. Reversibly thermochromic compositions
EP2043744A2 (en) 2006-07-13 2009-04-08 SmithKline Beecham Corporation Chemical compounds
US20080103123A1 (en) 2006-08-30 2008-05-01 Biovitrum New compounds
ES2374952T3 (es) 2006-12-06 2012-02-23 Glaxosmithkline Llc Compuestos bicíclicos y uso como antidiabéticos.
JP2010512418A (ja) 2006-12-11 2010-04-22 ワイス エルエルシー イオンチャネルモジュレータ−としてのカルボキサミド誘導体
US20100267697A1 (en) * 2006-12-11 2010-10-21 Wyeth Ion channel modulators
ES2509820T3 (es) 2006-12-20 2014-10-20 Nerviano Medical Sciences S.R.L. Derivados de indazol como inhibidores de la cinasa para el tratamiento del cáncer
ZA200904281B (en) 2006-12-28 2010-08-25 Metabolex Inc Heterocyclic receptor agonists for the treatment of diabetes and metabolic disorders
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
BRPI0808775A2 (pt) 2007-03-08 2017-05-30 Irm Llc compostos e composições como moduladores de atividade de gpr119
EP2152707B1 (en) 2007-05-04 2012-06-20 Bristol-Myers Squibb Company [6,5]-bicyclic gpr119 g protein-coupled receptor agonists
WO2008138876A1 (en) 2007-05-10 2008-11-20 Glaxo Group Limited Pyrazole derivatives as p2x7 modulators
EP2014656A3 (en) 2007-06-11 2011-08-24 High Point Pharmaceuticals, LLC New heteocyclic h3 antagonists
UY31232A1 (es) 2007-07-19 2009-03-02 Compuestos derivados de dibenzotifenilamino-cromen-4-onas activas sustituidas y sus isomeros y aplicaciones
CA2695998A1 (en) 2007-07-19 2009-01-22 F. Hoffmann-La Roche Ag Novel heterocyclyl compounds
US8183381B2 (en) * 2007-07-19 2012-05-22 Metabolex Inc. N-linked heterocyclic receptor agonists for the treatment of diabetes and metabolic disorders
PT2019104E (pt) 2007-07-19 2013-12-03 Sanofi Sa Agentes citotóxicos compreendendo novos derivados de tomaimicina e sua utilização terapêutica
FR2918986B1 (fr) 2007-07-19 2009-09-04 Sanofi Aventis Sa Derives de 6-cycloamino-3-(pyridazin-4-yl)imidazo[1,2-b]- pyridazine, leur preparation et leur application en therapeutique
AR067585A1 (es) 2007-07-19 2009-10-14 Schering Corp Compuestos heterociclicos de amidas como inhibidores de la proteincinasa
JP2011505388A (ja) 2007-12-04 2011-02-24 メルク フロスト カナダ リミテツド レニン阻害剤
MX2010010562A (es) 2008-03-31 2010-12-07 Metabolex Inc Compuestos de oximetilen-arilo y uso de los mismos.
US8188098B2 (en) 2008-05-19 2012-05-29 Hoffmann-La Roche Inc. GPR119 receptor agonists
EP2303859A4 (en) 2008-06-20 2012-08-22 Metabolex Inc ARYL GPR119 AGONISTS AND USES THEREOF
JPWO2010013849A1 (ja) 2008-08-01 2012-01-12 日本ケミファ株式会社 Ｇｐｒ１１９作動薬
RU2011113823A (ru) 2008-09-10 2012-10-20 БЕРИНГЕР ИНГЕЛЬХАЙМ ИНТЕРНАЦИОНАЛЬ ГмбХ (DE) Комбинированная терапия, предназначенная для лечения диабета и связанных с ним состояний
WO2010048149A2 (en) 2008-10-20 2010-04-29 Kalypsys, Inc. Heterocyclic modulators of gpr119 for treatment of disease
US20110160222A1 (en) 2008-11-26 2011-06-30 Metabolex, Inc. Modulators of glucose homeostasis for the treatment of diabetes and metabolic disorders
ES2497566T3 (es) 2009-10-01 2014-09-23 Cymabay Therapeutics, Inc. Sales de tetrazol-1-il-fenoximetil-tiazol-2-il-piperidinil-pirimidina sustituida
WO2011153435A1 (en) 2010-06-04 2011-12-08 Metabolex, Inc. Preparation of 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine
EP2585048B1 (en) 2010-06-23 2018-04-11 CymaBay Therapeutics, Inc. Compositions of 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine
US20120184572A1 (en) 2011-01-13 2012-07-19 Metabolex, Inc. Aryl gpr119 agonists and uses thereof

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US8227495B2 (en) 2012-07-24
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IL199397A (en) 2014-07-31
AU2007339772A1 (en) 2008-07-10
US8975258B2 (en) 2015-03-10
BRPI0720675A2 (pt) 2014-02-04
KR101539308B1 (ko) 2015-07-24
KR20090098898A (ko) 2009-09-17
AU2007339772B2 (en) 2014-03-20
EP2111107B1 (en) 2013-04-24
US20180021335A1 (en) 2018-01-25
JP5455645B2 (ja) 2014-03-26
JP2010514795A (ja) 2010-05-06
EP2111107A4 (en) 2011-04-06
US8921350B2 (en) 2014-12-30
EA016720B1 (ru) 2012-07-30
HK1136943A1 (en) 2010-07-16
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US9925189B2 (en) 2018-03-27
US20150239881A1 (en) 2015-08-27
US20100130511A1 (en) 2010-05-27
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AU2007339772B9 (en) 2014-09-11
US9737537B2 (en) 2017-08-22
US20100087465A1 (en) 2010-04-08
US20090054475A1 (en) 2009-02-26
US8288384B2 (en) 2012-10-16
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CA2672725A1 (en) 2008-07-10
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