EA201390421A1 - Модуляторы рецептора gpr119 и лечение связанных с ним нарушений - Google Patents

Модуляторы рецептора gpr119 и лечение связанных с ним нарушений

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Publication number
EA201390421A1
EA201390421A1 EA201390421A EA201390421A EA201390421A1 EA 201390421 A1 EA201390421 A1 EA 201390421A1 EA 201390421 A EA201390421 A EA 201390421A EA 201390421 A EA201390421 A EA 201390421A EA 201390421 A1 EA201390421 A1 EA 201390421A1
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EA
Eurasian Patent Office
Prior art keywords
fluoro
fluoropropan
oxadiazol
gpr119 receptor
inhibitor
Prior art date
Application number
EA201390421A
Other languages
English (en)
Inventor
Роберт М. Джонс
Юэрг Леманн
Вэйчао Чэнь
Джеффри Эдвардс
Глен Маркес
Майкл Е. Морган
Абу Дж.М. Садекве
Сун Хи Ким
Original Assignee
Арена Фармасьютикалз, Инк.
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Publication date
Application filed by Арена Фармасьютикалз, Инк. filed Critical Арена Фармасьютикалз, Инк.
Publication of EA201390421A1 publication Critical patent/EA201390421A1/ru

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Abstract

Изобретение относится к агонистам рецептора GPR119: 3-фтор-4-(5-фтор-6-(4-(3-(2-фторпропан-2-ил)-1,2,4-оксадиазол-5-ил)пиперидин-1-ил)пиримидин-4-иламино)-N,N-диметилбензамиду; 3-фтор-4-(5-фтор-6-(4-(3-(2-фторпропан-2-ил)-1,2,4-оксадиазол-5-ил)пиперидин-1-ил)пиримидин-4-иламино)-N-метилбензамиду; и 3-фтор-4-(5-фтор-6-(4-(3-(2-фторпропан-2-ил)-1,2,4-оксадиазол-5-ил)пиперидин-1-ил)пиримидин-4-иламино)бензамиду, и их фармацевтически приемлемым солям, сольватам и гидратам, которые могут быть пригодны в качестве единичного фармацевтического агента или в комбинации с одним или более дополнительными фармацевтическими агентами, такими как ингибитор ДПП-IV, бигуанид, ингибитор альфа-глюкозидазы, аналог инсулина, сульфонилмочевина, ингибитор SGLT2, меглитинид, тиазолидиндион или противодиабетический пептидный аналог, при лечении, например, нарушения, выбранного из связанного с GPR119-рецептором нарушения; состояния, улучшенного с помощью повышения секреции инкретина; состояния, улучшенного с помощью повышения уровня инкретина в крови; состояния, охарактеризованного с помощью низкой костной массы; неврологического нарушения; связанного с метаболизмом нарушения; сахарного диабета 2-го типа; ожирения и связанных с ним осложнений.
EA201390421A 2010-09-22 2011-09-21 Модуляторы рецептора gpr119 и лечение связанных с ним нарушений EA201390421A1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US38541010P 2010-09-22 2010-09-22
US201161478262P 2011-04-22 2011-04-22
PCT/US2011/052478 WO2012040279A1 (en) 2010-09-22 2011-09-21 Modulators of the gpr119 receptor and the treatment of disorders related thereto

Publications (1)

Publication Number Publication Date
EA201390421A1 true EA201390421A1 (ru) 2013-09-30

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US (2) US10894787B2 (ru)
EP (2) EP3323818A1 (ru)
JP (1) JP5941916B2 (ru)
KR (1) KR101871011B1 (ru)
CN (2) CN103221410B (ru)
AU (2) AU2011305525B2 (ru)
BR (1) BR112013008100A2 (ru)
CA (1) CA2812061A1 (ru)
CL (1) CL2013000785A1 (ru)
CO (1) CO6700841A2 (ru)
CR (1) CR20130145A (ru)
DO (1) DOP2013000061A (ru)
EA (1) EA201390421A1 (ru)
EC (1) ECSP13012704A (ru)
GT (1) GT201300075A (ru)
HK (1) HK1254745A1 (ru)
MX (1) MX2013003184A (ru)
NI (1) NI201300030A (ru)
PE (1) PE20131371A1 (ru)
SG (1) SG188548A1 (ru)
WO (1) WO2012040279A1 (ru)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GEP20084540B (en) 2003-01-14 2008-11-25 Arena Pharm Inc 1,2,3-trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prpphylaxis and treatment of disorders related thereto such as diabetes and hyperglycemia
WO2011094008A1 (en) 2010-01-27 2011-08-04 Arena Pharmaceuticals, Inc. Processes for the preparation of (r)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid and salts thereof
CN103221410B (zh) 2010-09-22 2017-09-15 艾尼纳制药公司 Gpr119受体调节剂和对与其相关的障碍的治疗
JP6463631B2 (ja) 2011-06-09 2019-02-06 ライゼン・ファーマシューティカルズ・エスアー Gpr−119のモジュレータとしての新規化合物
CN104780915A (zh) 2012-07-11 2015-07-15 埃尔舍利克斯治疗公司 包含他汀、双胍和用于减小心脏代谢风险的其它药剂的组合物
WO2014074668A1 (en) 2012-11-08 2014-05-15 Arena Pharmaceuticals, Inc. Modulators of gpr119 and the treatment of disorders related thereto
NZ734220A (en) 2015-01-06 2022-01-28 Arena Pharm Inc Methods of treating conditions related to the s1p1 receptor
IL285890B (en) 2015-06-22 2022-07-01 Arena Pharm Inc Slate-free crystal of the arginine salt of (Ar)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-4,3,2,1-tetrahydro-cyclopent[b]indole-3-yl ) acetic acid
JP2020507611A (ja) 2017-02-16 2020-03-12 アリーナ ファーマシューティカルズ, インコーポレイテッド 原発性胆汁性胆管炎の治療のための化合物および方法
HRP20231673T1 (hr) 2019-06-10 2024-03-15 Lupin Limited Inhibitori prmt5

Family Cites Families (558)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH389134A (de) 1960-03-15 1965-03-15 Ciba Geigy Verfahren zur Herstellung neuer Anthrachinonküpenfarbstoffe
CH478816A (de) 1965-10-22 1969-09-30 Ciba Geigy Verfahren zur Herstellung neuer N,N'-Di-(pyrimidyl-(4)-aminoalkyl)-diazacycloalkanen
CH480410A (de) 1967-01-09 1969-10-31 Geigy Ag J R Verfahren zur Herstellung von wasserlöslichen Azopyrimidinfarbstoffen
CA961052A (en) 1967-01-12 1975-01-14 Max Schellenbaum N-2-ethylhexyl-n'-aryl ureas and preparation containing them
FR1593586A (ru) 1967-10-17 1970-06-01
US3608087A (en) 1968-06-21 1971-09-21 Merck & Co Inc Feed compositions
US3887329A (en) 1969-05-05 1975-06-03 Ciba Geigy Ag Hexamethyl phosphotriamide-dye compositions
BE756953A (fr) 1969-10-02 1971-04-01 Merck & Co Inc Potentialisation d'antibiotiques
US3686238A (en) 1970-01-19 1972-08-22 Syntex Corp Glycerol esterified with 2-naphthyl-acetic acids and fatty acids
US3852434A (en) 1970-09-11 1974-12-03 Merck & Co Inc Potentiation of ({31 ) cis-1,2-epoxypropyl)phosphonic acid and analogues thereof
US3966744A (en) 1971-01-11 1976-06-29 Syva Company Spin labeled compounds
US3690834A (en) 1971-01-11 1972-09-12 Syva Co Ligand determination with spin labeled compounds by receptor displacement
DE2106585A1 (de) 1971-02-11 1972-08-24 Farbenfabriken Bayer Ag, 5090 Leverkusen Aminothiodiazole und Thiodiazol-Azofarbstoffe
CH558137A (de) 1971-05-17 1975-01-31 Ciba Geigy Ag Mittel zur beeinflussung des pflanzenwachstums.
CH560197A5 (en) 1971-05-17 1975-03-27 Ciba Geigy Ag 2-alkylthio-4,6-bis (subst amino)-5-nitropyrimidines - - herbicides
US3966764A (en) 1972-07-10 1976-06-29 Syva Company Ligand determination of spin labeled compounds by receptor displacement-amphetamine analogs
US3849420A (en) 1972-10-20 1974-11-19 Dow Chemical Co Bis-(alkylthio-and alkylsulfonyl)-pentachloroquinolines
CH574206A5 (ru) 1972-11-16 1976-04-15 Ciba Geigy Ag
DE2340569C2 (de) 1973-08-10 1982-12-02 Bayer Ag, 5090 Leverkusen Azofarbstoffe
AT340933B (de) 1973-08-20 1978-01-10 Thomae Gmbh Dr K Verfahren zur herstellung neuer pyrimidinderivate und ihrer saureadditionssalze
DE2341925A1 (de) 1973-08-20 1975-03-06 Thomae Gmbh Dr K Neue pyrimidinderivate und verfahren zu ihrer herstellung
US4101541A (en) 1973-12-21 1978-07-18 Ciba-Geigy Corporation 3-Cyano-1,2,4-thiadiazolyl-5-czo dyestuffs
CH584739A5 (ru) 1973-12-21 1977-02-15 Ciba Geigy Ag
FR2258841B1 (ru) 1974-01-29 1977-11-04 Ugine Kuhlmann
AT327605B (de) 1974-05-06 1976-02-10 Ciba Geigy Ag Mittel zur hemmung des pflanzenwachstums
AU492126B2 (en) 1974-05-14 1975-11-20 Ciba-Geigy Ag Nitropyrimidine derivatives
FR2306697A1 (fr) 1975-04-10 1976-11-05 Sogeras Nouvelles pyrimidines utilisables comme medicaments antidiabetiques et hypocholesterolemiants
US4189579A (en) 1977-05-20 1980-02-19 The Dow Chemical Company Aminoalkylthiopurines
US4139705A (en) 1977-05-20 1979-02-13 The Dow Chemical Company Pyrazolopyrimidines
DE2731264A1 (de) 1977-07-11 1979-02-01 Boehringer Mannheim Gmbh Neue 1-acyl-2-cyanaziridine, verfahren zu deren herstellung und diese verbindungen enthaltende pharmazeutische zubereitungen
JPS6038696B2 (ja) 1977-12-09 1985-09-02 コニカ株式会社 ハロゲン化銀カラ−写真感光材料
US4242507A (en) 1978-02-23 1980-12-30 Fujisawa Pharmaceutical Co., Ltd. Sulfonic acid esters
DE2831580C2 (de) 1978-07-18 1980-09-18 Boehringer Mannheim Gmbh, 6800 Mannheim Verfahren und Reagens zur Bestimmung von Glycerin
DE2831850A1 (de) 1978-07-20 1980-02-07 Basf Ag N-arylsulfonylpyrrole, ihre herstellung und diese enthaltende therapeutische mittel
DE2906603A1 (de) 1979-02-21 1980-09-04 Boehringer Mannheim Gmbh N-substituierte aziridin-2-carbonsaeurederivate, verfahren zu deren herstellung sowie diese substanzen enthaltende arzneimittel
US4343804A (en) 1979-03-26 1982-08-10 A. H. Robins Company, Inc. 4-Amino-3-quinolinecarboxylic acids and esters-antisecretory anti-ulcer compounds
WO1981003174A1 (en) 1980-04-28 1981-11-12 Teijin Ltd Thiazolo(3,2-a)pyrimidine derivatives,process for preparing same,and drug containing same
EP0053678A1 (de) 1980-12-05 1982-06-16 BASF Aktiengesellschaft 5-Amino-1-phenyl-4-cyanpyrazole, diese enthaltende herbizide Mittel, Verfahren zu ihrer Herstellung und ihre Anwendung als Herbizide
DOP1981004033A (es) 1980-12-23 1990-12-29 Ciba Geigy Ag Procedimiento para proteger plantas de cultivo de la accion fitotoxica de herbicidas.
DE3334455A1 (de) 1983-03-04 1984-09-06 Bayer Ag, 5090 Leverkusen Guanidin - derivate
US4612376A (en) 1983-03-25 1986-09-16 Fujisawa Pharmaceutical Co., Ltd. Substituted-3,4-dihydro-4-(2,4,6-trimethoxyphenylimino)-2(1H)-pyrimidones useful as cardiotonic, antihypertensive, cerebrovascular vasodilator and anti-platelet agent
ZA848275B (en) 1983-12-28 1985-08-28 Degussa New piridine-2-ethers or pyridine-2-thioethers having a nitrogen-containing cycloaliphatic ring
DE3406329A1 (de) 1984-02-22 1985-08-22 Merck Patent Gmbh, 6100 Darmstadt Pyridone
JPS6157587A (ja) 1984-08-29 1986-03-24 Shionogi & Co Ltd 縮合複素環誘導体および抗潰瘍剤
PH22302A (en) 1985-02-11 1988-07-22 Fujisawa Pharmaceutical Co Piperidine compounds
IE860511L (en) 1985-03-01 1986-09-01 Alfa Farmaceutici Spa "Benzoyl urea derivatives having anti-tumor activity"
DE3601196A1 (de) 1986-01-17 1987-07-23 Merck Patent Gmbh 1,4-dihydropyridine
CA1340284C (en) 1987-03-19 1998-12-22 Zeneca Inc. Herbicidal substituted cyclic diones
DE68926687T2 (de) 1988-01-11 1997-03-06 Fuji Photo Film Co Ltd Verfahren zur Erzeugung von extrem hochkontrastreichen negativen Bildern
DD296075A5 (de) 1989-08-07 1991-11-21 Martin-Luther-Universitaet Halle-Wittenberg,De Verfahren zur herstellung neuer inhibitoren der dipeptidyl peptidase iv
DK0528858T3 (da) 1990-04-14 1997-07-28 Univ Tufts Med Inhibitorer af dipeptidyl-aminopeptidase type IV
NZ238863A (en) 1990-07-19 1993-03-26 Janssen Pharmaceutica Nv Substituted thiazolyl and pyridinyl derivatives
EP0567643A4 (en) 1991-01-16 1995-07-19 Yoshitomi Pharmaceutical PYRIDINE COMPOUND USED AS A SELECTIVE DRUG AND NEW PYRIDINE COMPOUND.
CA2070978A1 (en) 1991-06-11 1992-12-12 William J. Greenlee Cyclic renin inhibitors
GB9114760D0 (en) 1991-07-09 1991-08-28 Pfizer Ltd Therapeutic agents
JPH0533359A (ja) 1991-08-02 1993-02-09 Kubota Corp 全旋回型の小型バツクホウ
ES2153831T3 (es) 1991-10-22 2001-03-16 New England Medical Center Inc Inhibidores de dipeptidil-aminopeptidasa de tipo iv.
MX9206628A (es) 1991-11-22 1993-05-01 Boehringer Ingelheim Pharma Ester de prolinaboronato y metodo para su preparacion.
EP0556889A1 (en) 1992-02-18 1993-08-25 Duphar International Research B.V Method of preparing aryl(homo)piperazines
DE4208254A1 (de) 1992-03-14 1993-09-16 Hoechst Ag Substituierte pyrimidine, verfahren zu ihrer herstellung und ihre verwendung als schaedlingsbekaempfungsmittel und fungizid
TW237456B (ru) 1992-04-09 1995-01-01 Ciba Geigy
FR2692575B1 (fr) 1992-06-23 1995-06-30 Sanofi Elf Nouveaux derives du pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant.
NZ314207A (en) 1992-09-28 2000-12-22 Vertex Pharma 1-(2-Oxoacetyl)-piperidine-2-carboxylic acid derivatives as multi drug resistant cancer cell sensitizers
DE4241632A1 (de) 1992-12-10 1994-06-16 Thomae Gmbh Dr K Carbonsäurederivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
TW370529B (en) 1992-12-17 1999-09-21 Pfizer Pyrazolopyrimidines
JPH0753546A (ja) 1993-08-09 1995-02-28 Kuraray Co Ltd ジアリール置換複素環化合物およびその医薬用途
EP0723533A1 (en) 1993-10-12 1996-07-31 The Du Pont Merck Pharmaceutical Company 1n-alkyl-n-arylpyrimidinamines and derivatives thereof
IL111785A0 (en) 1993-12-03 1995-01-24 Ferring Bv Dp-iv inhibitors and pharmaceutical compositions containing them
GB9400889D0 (en) 1994-01-18 1994-03-16 Sandoz Ltd Novel compounds
US5543396A (en) 1994-04-28 1996-08-06 Georgia Tech Research Corp. Proline phosphonate derivatives
TW574214B (en) 1994-06-08 2004-02-01 Pfizer Corticotropin releasing factor antagonists
CN1118454C (zh) 1994-09-09 2003-08-20 日本新药株式会社 杂环衍生物和医药
CA2206307A1 (en) 1994-11-29 1996-06-06 Dainippon Pharmaceutical Co., Ltd. Indole derivative
DK0813525T3 (da) 1995-03-10 2004-02-16 Berlex Lab Benzamidinderivater, deres fremstilling og anvendelse som antikoagulanter
US5691364A (en) 1995-03-10 1997-11-25 Berlex Laboratories, Inc. Benzamidine derivatives and their use as anti-coagulants
IL117659A (en) 1995-04-13 2000-12-06 Dainippon Pharmaceutical Co Substituted 2-phenyl pyrimidino amino acetamide derivative process for preparing the same and a pharmaceutical composition containing same
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
WO1996033994A1 (fr) 1995-04-28 1996-10-31 Nippon Soda Co., Ltd. Derives amino-substitues, leur procede de preparation et herbicide
WO1996035689A1 (en) 1995-05-12 1996-11-14 Neurogen Corporation Novel deazapurine derivatives; a new class of crf1 specific ligands
WO1996036613A1 (fr) 1995-05-19 1996-11-21 Nippon Soda Co., Ltd. Derives d'acides benzoiques substitues, procede de production desdits derives et herbicides
US6956047B1 (en) 1995-06-06 2005-10-18 Pfizer Inc. Corticotropin releasing factor antagonists
US6403599B1 (en) 1995-11-08 2002-06-11 Pfizer Inc Corticotropin releasing factor antagonists
TW438587B (en) 1995-06-20 2001-06-07 Takeda Chemical Industries Ltd A pharmaceutical composition for prophylaxis and treatment of diabetes
KR0169813B1 (ko) 1995-07-12 1999-01-15 김종인 4-아미노-3-아실나프티리딘 유도체
US6248571B1 (en) 1995-08-31 2001-06-19 Lonza Ag Method of producing dihydroxypyrimidine derivatives
WO1997015549A1 (fr) 1995-10-26 1997-05-01 Tokyo Tanabe Company Limited COMPOSES DE PHENYLETHANOLAMINE UTILES EN TANT QUE β3 AGONISTES, LEURS PROCEDE ET INTERMEDIAIRES DE PRODUCTION
US5849759A (en) 1995-12-08 1998-12-15 Berlex Laboratories, Inc. Naphthyl-substituted benzimidazole derivatives as anti-coagulants
USH2007H1 (en) 1996-01-19 2001-12-04 Fmc Corporation Insecticidal N-heterocyclylalkyl-or N-[(polycyclyl)alkyl]-N′substituted piperazines
DE19602095A1 (de) 1996-01-22 1997-07-24 Bayer Ag Halogenpyrimidine
ATE236137T1 (de) 1996-02-02 2003-04-15 Merck & Co Inc Heterocyclische verbindungen als antidiabetische mittel und für die behandlung von fettleibigkeit
WO1997029109A1 (en) 1996-02-07 1997-08-14 Janssen Pharmaceutica N.V. Pyrazolopyrimidines as crf receptor antagonists
US5948786A (en) 1996-04-12 1999-09-07 Sumitomo Pharmaceuticals Company, Limited Piperidinylpyrimidine derivatives
DE19616486C5 (de) 1996-04-25 2016-06-30 Royalty Pharma Collection Trust Verfahren zur Senkung des Blutglukosespiegels in Säugern
US20020006899A1 (en) 1998-10-06 2002-01-17 Pospisilik Andrew J. Use of dipeptidyl peptidase IV effectors for lowering blood pressure in mammals
JPH1081666A (ja) 1996-06-12 1998-03-31 Ishihara Sangyo Kaisha Ltd フタルイミド誘導体又はその塩、それらの製造方法及びそれらを含有する医薬組成物
DE19624659A1 (de) 1996-06-20 1998-01-08 Klinge Co Chem Pharm Fab Neue Pyridylalken- und Pyridylalkinsäureamide
AU3176297A (en) 1996-06-25 1998-01-14 Novartis Ag Substituted 7-amino-pyrrolo{3,2-d}pyrimidines and the use thereof
US6060478A (en) 1996-07-24 2000-05-09 Dupont Pharmaceuticals Azolo triazines and pyrimidines
AR008789A1 (es) 1996-07-31 2000-02-23 Bayer Corp Piridinas y bifenilos substituidos
TW477787B (en) 1996-08-27 2002-03-01 Pfizer Pyrido six-membered nitrogen-containing cyclic ring derivatives having corticotropin releasing factor antagonist activity and pharmaceutical composition containing same
WO1998008847A1 (en) 1996-08-28 1998-03-05 Pfizer Inc. Substituted 6,5-hetero-bicyclic derivatives
US6008234A (en) 1996-09-12 1999-12-28 Berlex Laboratories, Inc. Benzamidine derivatives substituted by cyclic amino acid and cyclic hydroxy acid derivatives and their use as anti-coagulants
IL128691A (en) 1996-09-12 2007-07-24 Bayer Schering Pharma Ag History of enzamidine converted by annular amino acid and history of annular hydroxy acid and their use against coagulation
GB9718972D0 (en) 1996-09-25 1997-11-12 Zeneca Ltd Chemical compounds
AU4721897A (en) 1996-10-25 1998-05-22 Tanabe Seiyaku Co., Ltd. Tetrahydroisoquinoline derivatives
JPH10182613A (ja) 1996-10-25 1998-07-07 Tanabe Seiyaku Co Ltd テトラヒドロイソキノリン誘導体
TW492957B (en) 1996-11-07 2002-07-01 Novartis Ag N-substituted 2-cyanopyrrolidnes
DZ2376A1 (fr) 1996-12-19 2002-12-28 Smithkline Beecham Plc Dérivés de sulfonamides nouveaux procédé pour leurpréparation et compositions pharmaceutiques les c ontenant.
NO980546L (no) 1997-02-11 1998-08-12 Lilly Co Eli Farmas°ytiske midler
EP0970082A2 (en) 1997-02-18 2000-01-12 Neurocrine Biosciences, Inc. Biazacyclic crf antagonists
US6211195B1 (en) 1997-04-22 2001-04-03 Neurocrine Biosciences, Inc. CRF antagonistic thiophenopyridines
DE69818248T2 (de) 1997-04-22 2004-06-17 Janssen Pharmaceutica N.V. Chinolin- und chinazolin-derivate als crf antagonisten
US6100234A (en) 1997-05-07 2000-08-08 Tufts University Treatment of HIV
US6040145A (en) 1997-05-07 2000-03-21 Tufts University Potentiation of the immune response
JPH11193277A (ja) 1997-05-14 1999-07-21 Nippon Soda Co Ltd ピリミジン誘導体、その製法および有害生物防除剤
DE19737723A1 (de) 1997-08-14 1999-02-18 Bayer Ag Methoximinomethyloxadiazine
AU9256898A (en) 1997-08-14 1999-03-08 Bayer Aktiengesellschaft Methoximinomethyloxadiazines used as pesticides
NL1010018C2 (nl) 1997-09-09 1999-03-10 Duphar Int Res Chinoline en chinazoline derivaten met corticotropine releasing factor (CRF) antagonistische werking.
EP1019494B1 (en) 1997-09-29 2007-03-21 Point Therapeutics, Inc. Stimulation of hematopoietic cells in vitro
WO1999025719A1 (fr) 1997-11-18 1999-05-27 Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai Substance physiologiquement active, la sulphostine, procede de fabrication et utilisation
EP2433623A1 (en) 1998-02-02 2012-03-28 Trustees Of Tufts College Use of dipeptidylpeptidase inhibitors to regulate glucose metabolism
US6187777B1 (en) 1998-02-06 2001-02-13 Amgen Inc. Compounds and methods which modulate feeding behavior and related diseases
CA2326383A1 (en) 1998-04-02 1999-10-14 Neurogen Corporation Aminoalkyl substituted pyrrolo[2,3-b]pyridine and pyrrolo[2,3-d]pyrimidine derivatives: modulators of crf1 receptors
IL139247A0 (en) 1998-05-04 2001-11-25 Point Therapeutics Inc Hematopoietic stimulation
JP2000038350A (ja) 1998-05-18 2000-02-08 Yoshitomi Pharmaceut Ind Ltd 糖尿病治療薬
DE19823831A1 (de) 1998-05-28 1999-12-02 Probiodrug Ges Fuer Arzneim Neue pharmazeutische Verwendung von Isoleucyl Thiazolidid und seinen Salzen
KR100704814B1 (ko) 1998-06-05 2007-04-10 포인트 써러퓨틱스, 인크. 시클릭 보로프롤린 화합물
DE19828113A1 (de) 1998-06-24 2000-01-05 Probiodrug Ges Fuer Arzneim Prodrugs von Inhibitoren der Dipeptidyl Peptidase IV
DE19834591A1 (de) 1998-07-31 2000-02-03 Probiodrug Ges Fuer Arzneim Verfahren zur Steigerung des Blutglukosespiegels in Säugern
KR20010079669A (ko) 1998-08-21 2001-08-22 바바라 피. 월너 기질 활성의 조절
CA2339188A1 (en) 1998-08-21 2000-03-02 Dupont Pharmaceuticals Company Isoxazolo¬4,5-d|pyrimidines as crf antagonists
WO2000020592A1 (en) 1998-10-07 2000-04-13 Medical College Of Georgia Research Institute, Inc. Glucose-dependent insulinotropic peptide for use as an osteotropic hormone
US6242422B1 (en) 1998-10-22 2001-06-05 Idun Pharmacueticals, Inc. (Substituted)Acyl dipeptidyl inhibitors of the ice/ced-3 family of cysteine proteases
AP1683A (en) 1998-11-10 2006-11-29 Janssen Pharmaceutica Nv HIV replication inhibiting pyrimidines.
US6262088B1 (en) 1998-11-19 2001-07-17 Berlex Laboratories, Inc. Polyhydroxylated monocyclic N-heterocyclic derivatives as anti-coagulants
ES2308759T3 (es) 1998-11-20 2008-12-01 Arena Pharmaceuticals, Inc. Receptores acoplados a proteina g humanos huerfanos.
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
CN1335835A (zh) 1998-12-17 2002-02-13 美国家用产品公司 具有5ht1a受体活性的芳基哌啶和芳基-1,2,5,6-四氢吡啶脲衍生物
US6239126B1 (en) 1998-12-17 2001-05-29 American Home Products Corporation Arylpiperidine and aryl-1,2,5,6-tetra-hydropyridine urea derivatives
EA200100675A1 (ru) 1998-12-18 2001-12-24 Аксис Фармасьютикалз, Инк. Ингибиторы протеазы
JP2000191616A (ja) 1998-12-24 2000-07-11 Senju Pharmaceut Co Ltd 新規ジペプチジルアルデヒド誘導体およびそれを含有する医薬
CZ27399A3 (cs) 1999-01-26 2000-08-16 Ústav Experimentální Botaniky Av Čr Substituované dusíkaté heterocyklické deriváty, způsob jejich přípravy, tyto deriváty pro použití jako léčiva, farmaceutická kompozice a kombinovaný farmaceutický přípravek tyto deriváty obsahující a použití těchto derivátů pro výrobu léčiv
US6267985B1 (en) 1999-06-30 2001-07-31 Lipocine Inc. Clear oil-containing pharmaceutical compositions
CZ300293B6 (cs) 1999-03-17 2009-04-15 Astrazeneca Ab Nové amidové deriváty, zpusob jejich prípravy a farmaceutická kompozice, která je obsahuje
GB9906714D0 (en) 1999-03-23 1999-05-19 Ferring Bv Compositions for improving fertility
GB9906715D0 (en) 1999-03-23 1999-05-19 Ferring Bv Compositions for promoting growth
EP1040831A3 (en) 1999-04-02 2003-05-02 Pfizer Products Inc. Use of corticotropin releasing factor (CRF) antagonists to prevent sudden death
JP4121215B2 (ja) 1999-05-17 2008-07-23 財団法人微生物化学研究会 スルフォスチン類縁体、並びにスルフォスチン及びその類縁体の製造方法
JP2003500360A (ja) 1999-05-25 2003-01-07 ポイント セラピューティクス, インコーポレイテッド ボロプロリン化合物類を含む抗癌剤
US6617340B1 (en) 1999-07-29 2003-09-09 Novartis Ag N-(substituted glycyl)-pyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
EP1074549B1 (en) 1999-08-06 2003-11-19 F. Hoffmann-La Roche Ag Tetrahydro-benzo(d)azepines and their use as antagonists at metabotropic glutamate receptors
US6921763B2 (en) 1999-09-17 2005-07-26 Abbott Laboratories Pyrazolopyrimidines as therapeutic agents
CZ2002936A3 (cs) 1999-09-17 2002-10-16 Abbott Gmbh & Co. Kg Pyrazolopyrimidiny jako terapeutické prostředky
US6414002B1 (en) 1999-09-22 2002-07-02 Bristol-Myers Squibb Company Substituted acid derivatives useful as antidiabetic and antiobesity agents and method
JP2001089452A (ja) 1999-09-22 2001-04-03 Sankyo Co Ltd ピリミジン誘導体
UA74797C2 (ru) 1999-09-24 2006-02-15 Янссен Фармацевтика Н.В. Противовирусная композиция
US6372743B1 (en) 1999-09-30 2002-04-16 Neurogen Corporation Certain alkylene diamine-substituted pyrazlo (1,5-a)-1,5-pyrimidines and pyrazolo (1,5-a) 1,3,5-triazines
CN1377356A (zh) 1999-09-30 2002-10-30 纽罗杰有限公司 亚烷基二胺取代的杂环
AU7737900A (en) 1999-09-30 2001-04-30 Neurogen Corporation Amino substituted pyrazolo(1,5,-a)-1,5-pyrimidines and pyrazolo(1,5-a)-1,3,5-triazines
DE19947154A1 (de) 1999-10-01 2001-10-04 Bayer Ag Substituierte 2-Thio-3,5-dicyano-4-aryl-6-aminopyridine und ihre Verwendung
US6887870B1 (en) 1999-10-12 2005-05-03 Bristol-Myers Squibb Company Heterocyclic sodium/proton exchange inhibitors and method
IL139197A0 (en) 1999-10-29 2001-11-25 Pfizer Prod Inc Use of corticotropin releasing factor antagonists and related compositions
GR990100388A (el) 1999-11-09 2001-07-31 Φαρμακευτικος συνδυασμος αποτελουμενος απο χωριστες δοσολογικες μορφες σε συσκευασια συμμορφωσης (compliance package) ενος αναστολεα της αναγωγασης του υδροξυ-μεθυλο-γλουταρυλο συνενζυμου α (στατινης, statin) και ενος παραγωγου του φιμπρικου οξεος....
JP2003535034A (ja) 1999-11-12 2003-11-25 ギルフォード ファーマシューティカルズ インコーポレイテッド ジペプチジルペプチダーゼiv阻害剤並びにジペプチジルペプチダーゼiv阻害剤の製造及び使用法
JP2003518128A (ja) 1999-12-22 2003-06-03 メルク フロスト カナダ アンド カンパニー タンパク質チロシンホスファターゼ1b(ptp−1b)のインヒビターとなる芳香族ホスホネート
DE19962936A1 (de) 1999-12-24 2001-06-28 Bayer Ag Neue beta-Aminosäureverbindungen als Integrinantagonisten
DE60009154D1 (de) 1999-12-30 2004-04-22 Lundbeck & Co As H Phenylpiperazinyl-derivate
US6380398B2 (en) 2000-01-04 2002-04-30 Novo Nordisk A/S Therapeutically active and selective heterocyclic compounds that are inhibitors of the enzyme DPP-IV
KR20020063934A (ko) 2000-01-18 2002-08-07 화이자 프로덕츠 인코포레이티드 코르티코트로핀 방출 인자 길항제
ES2436610T3 (es) 2000-01-21 2014-01-03 Novartis Ag Combinaciones que contienen inhibidores de la dipeptidilpeptidasa-IV y agentes antidiabéticos
JP2003520849A (ja) 2000-01-24 2003-07-08 ノボ ノルディスク アクティーゼルスカブ 酵素dpp−ivの阻害剤であるn−置換2−シアノピロールおよび−ピロリン
MXPA02007525A (es) 2000-02-09 2002-12-13 Hokuriku Pharmaceutical Derivados 1h-imidazopiridina..
AU2001236948A1 (en) 2000-02-15 2001-08-27 Foster-Miller Inc. No voc radiation curable resin compositions
US6569879B2 (en) 2000-02-18 2003-05-27 Merck & Co., Inc. Aryloxyacetic acids for diabetes and lipid disorders
EP1259494A4 (en) 2000-02-18 2004-09-15 Merck & Co Inc ARYLOXY ACETIC ACIDS FOR DIABETES AND LIPID DISEASES
EP1261327B1 (en) 2000-02-25 2005-04-27 F.Hoffmann-La Roche Ag Adenosine receptor modulators
US6395767B2 (en) 2000-03-10 2002-05-28 Bristol-Myers Squibb Company Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method
PE20020229A1 (es) 2000-04-12 2002-04-11 Novartis Ag COMBINACION DE UN ANTAGONISTA DEL RECEPTOR AT1; UN INHBIDOR DE HMG-CoA REDUCTASA Y UN INHIBIDOR DE ACE
GB0010183D0 (en) 2000-04-26 2000-06-14 Ferring Bv Inhibitors of dipeptidyl peptidase IV
GB0010188D0 (en) 2000-04-26 2000-06-14 Ferring Bv Inhibitors of dipeptidyl peptidase IV
JP4969010B2 (ja) 2000-05-08 2012-07-04 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ Hiv複製阻害性ピリミジンのプロドラッグ
DE10024319A1 (de) 2000-05-17 2001-11-22 Merck Patent Gmbh Bisacylguanidine
AU6744501A (en) 2000-05-18 2001-11-26 Bayer Aktiengesellschaft Regulation of human dopamine-like g protein-coupled receptor
WO2001087892A1 (en) 2000-05-18 2001-11-22 Neurocrine Biosciences, Inc. Crf receptor antagonists
ATE280162T1 (de) 2000-05-25 2004-11-15 Hoffmann La Roche Substituierte 1-aminoalkyl-lactame und ihre verwendung als muscarinrezeptor antagonisten
TW583185B (en) 2000-06-13 2004-04-11 Novartis Ag N-(substituted glycyl)-2-cyanopyrrolidines and pharmaceutical composition for inhibiting dipeptidyl peptidase-IV (DPP-IV) or for the prevention or treatment of diseases or conditions associated with elevated levels of DPP-IV comprising the same
US6432969B1 (en) 2000-06-13 2002-08-13 Novartis Ag N-(substituted glycyl)-2 cyanopyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
US6620821B2 (en) 2000-06-15 2003-09-16 Bristol-Myers Squibb Company HMG-CoA reductase inhibitors and method
GB0014969D0 (en) 2000-06-19 2000-08-09 Smithkline Beecham Plc Novel method of treatment
KR20030017569A (ko) 2000-06-28 2003-03-03 테바 파마슈티컬 인더스트리즈 리미티드 카르베딜올
AU2001268718B2 (en) 2000-06-29 2006-01-05 Abbott Laboratories Aryl phenylheterocyclyl sulfide derivatives and their use as cell adhesion-inhibiting anti-inflammatory and immune-suppressive agents
JP2004502690A (ja) 2000-07-04 2004-01-29 ノボ ノルディスク アクティーゼルスカブ 酵素dpp−ivのインヒビターである複素環式化合物
AR028782A1 (es) 2000-07-05 2003-05-21 Taisho Pharmaceutical Co Ltd Derivados heterociclicos tetrahidropiridino o piperidino
US6444685B1 (en) 2000-07-17 2002-09-03 Wyeth N-(4-sulfonylaryl)Cyclylamine 2-hydroxyethylamines as beta-3 adrenergic receptor agonists
KR20030026979A (ko) 2000-07-18 2003-04-03 야마노우치세이야쿠 가부시키가이샤 디시아노피리딘 유도체를 포함하는 의약
AU7705601A (en) 2000-07-25 2002-02-05 Merck & Co Inc N-substituted indoles useful in the treatment of diabetes
AU7775401A (en) 2000-08-10 2002-02-25 Welfide Corp Proline derivatives and use thereof as drugs
AU2001284417A1 (en) 2000-09-05 2002-03-22 Taisho Pharmaceutical Co. Ltd. Hair growth stimulants
EP1322289B1 (en) 2000-09-20 2007-07-25 Jagotec AG Spray drying process of compositions containing fenofibrate
US7276249B2 (en) 2002-05-24 2007-10-02 Elan Pharma International, Ltd. Nanoparticulate fibrate formulations
US20030224058A1 (en) 2002-05-24 2003-12-04 Elan Pharma International, Ltd. Nanoparticulate fibrate formulations
WO2002030891A1 (fr) 2000-10-06 2002-04-18 Tanabe Seiyaku Co., Ltd. Composes aliphatiques azotes a noyau a cinq elements
JP4329291B2 (ja) 2000-10-06 2009-09-09 田辺三菱製薬株式会社 含窒素五員環化合物
JP2004035574A (ja) 2000-10-06 2004-02-05 Tanabe Seiyaku Co Ltd 脂肪族含窒素五員環化合物
JP4329290B2 (ja) 2000-10-06 2009-09-09 田辺三菱製薬株式会社 脂肪族含窒素五員環化合物
PE20020507A1 (es) 2000-10-17 2002-06-25 Schering Corp Compuestos no-imidazoles como antagonistas del receptor histamina h3
WO2002032408A2 (en) 2000-10-20 2002-04-25 Novartis Ag Combinations of a thyromimetic compound and a statin
ES2372028T3 (es) 2000-10-23 2012-01-13 Glaxosmithkline Llc Nuevo compuesto de 8h-pirido[2,3-d]pirimidin-7-ona trisustituida para el tratamiento de enfermedades mediadas por la csbp/p38 quinasa.
AUPR107800A0 (en) 2000-10-27 2000-11-23 University Of Sydney, The Peptide and nucleic acid molecule ii
CA2427610A1 (en) 2000-10-31 2002-08-08 Merck & Co., Inc. Benzopyrancarboxylic acid derivatives for the treatment of diabetes and lipid disorders
ES2279835T3 (es) 2000-11-03 2007-09-01 Neurocrine Biosciences, Inc. Antagonistas del receptor de crf y metodos relacionados.
TWI243162B (en) 2000-11-10 2005-11-11 Taisho Pharmaceutical Co Ltd Cyanopyrrolidine derivatives
US20020058026A1 (en) 2000-11-13 2002-05-16 Milton Hammerly HMG CoA reductase inhibitor medications combined wih CoEnzyme Q-10
WO2002040458A1 (fr) 2000-11-17 2002-05-23 Takeda Chemical Industries, Ltd. Derives d'isoxazole
UA77165C2 (en) 2000-11-17 2006-11-15 Lilly Co Eli (n)-((s)-2-hydroxy-3-methyl-butyryl)-1-(l-alaninyl)-(s)-1-amino-3-methyl-4,5,6,7-tetrahydro-2h-3-benzazepin-2-one dihydrate, processes for manufacturing and pharmaceutical composition
EP1335907B1 (en) 2000-11-20 2010-06-09 Biovitrum AB (publ) Piperazinylpyrazine compounds as agonist or antagonist of serotonin 5ht-2 receptor
JP3438186B2 (ja) 2000-12-01 2003-08-18 山之内製薬株式会社 糖尿病治療剤スクリーニング方法
US20020137755A1 (en) 2000-12-04 2002-09-26 Bilodeau Mark T. Tyrosine kinase inhibitors
US6545017B1 (en) 2000-12-08 2003-04-08 3M Innovative Properties Company Urea substituted imidazopyridines
US6525064B1 (en) 2000-12-08 2003-02-25 3M Innovative Properties Company Sulfonamido substituted imidazopyridines
US20020107262A1 (en) 2000-12-08 2002-08-08 3M Innovative Properties Company Substituted imidazopyridines
US6545016B1 (en) 2000-12-08 2003-04-08 3M Innovative Properties Company Amide substituted imidazopyridines
AU2002231139B2 (en) 2000-12-21 2007-03-22 Bristol-Myers Squibb Company Thiazolyl inhibitors of tec family tyrosine kinases
CA2433090A1 (en) 2000-12-27 2002-07-04 Kyowa Hakko Kogyo Co., Ltd. Dipeptidyl peptidase iv inhibitor
US20040038942A1 (en) 2001-01-16 2004-02-26 Takumi Yamashita Medicament for treatment of bone marrow suppression, for treatment of infectious diseases and for increasing the number of leukocytes
RU2756946C2 (ru) 2001-01-26 2021-10-07 Мерк Шарп И Доум Корп. Применение замещенных азетидинонов для лечения ситостеролемии
AU2002240235B2 (en) 2001-01-30 2006-07-06 Merck & Co., Inc. Acyl sulfamides for treatment of obesity, diabetes and lipid disorders
US7034039B2 (en) 2001-02-02 2006-04-25 Takeda Pharmaceutical Company Limited Fused heterocyclic compounds
JP4213390B2 (ja) 2001-02-02 2009-01-21 武田薬品工業株式会社 縮合複素環化合物
BR0207302A (pt) 2001-02-08 2004-02-10 Memory Pharm Corp Trifluorometilpurinas como inibidores da fosfodiesterase 4
EP1366012A4 (en) 2001-02-09 2005-11-02 Merck & Co Inc 2-ARYLOXY-2-ARYLALCANO ACIDS AS USED FOR THE TREATMENT OF DIAB TES AND LIPID DISORDERS
ATE353900T1 (de) 2001-02-24 2007-03-15 Boehringer Ingelheim Pharma Xanthinderivate, deren herstellung und deren verwendung als arzneimittel
DE10110754A1 (de) 2001-03-07 2002-09-19 Bayer Ag Substituierte 2-Thio-3,5-dicyano-4-aryl-6-aminopyridine und ihre Verwendung
JP2002265439A (ja) 2001-03-08 2002-09-18 Mitsubishi Pharma Corp シアノピロリジン誘導体およびその医薬用途
WO2002072101A1 (en) 2001-03-13 2002-09-19 Bristol-Myers Squibb Pharma Company A corticotropin releasing factor receptor ligand, its enantiomer and pharmaceutically acceptable salts
DE60226723D1 (de) 2001-03-27 2008-07-03 Merck & Co Inc Dipeptidylpeptidase-hemmer für die behandlung oder prävention von diabetes
FR2822826B1 (fr) 2001-03-28 2003-05-09 Servier Lab Nouveaux derives sulfonyles d'alpha-amino-acides, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
WO2002081454A1 (en) 2001-04-09 2002-10-17 Dr. Reddy's Laboratories Ltd. Derivatives of aryl acids, their use in medicine, process for their preparation and pharmaceutical compositions containing them
GB0109146D0 (en) 2001-04-11 2001-05-30 Ferring Bv Treatment of type 2 diabetes
US6573287B2 (en) 2001-04-12 2003-06-03 Bristo-Myers Squibb Company 2,1-oxazoline and 1,2-pyrazoline-based inhibitors of dipeptidyl peptidase IV and method
AR035235A1 (es) 2001-04-20 2004-05-05 Wyeth Corp Derivados heterocicliloxi-,-tioxi- y -aminobenzazol como ligandos de 5-hidroxitriptamina-6, un procedimiento para su preparacion, composicion farmaceutica, y el uso de dichos derivados para la manufactura de un medicamento
FR2824825B1 (fr) 2001-05-15 2005-05-06 Servier Lab Nouveaux derives d'alpha-amino-acides, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
DE60234338D1 (de) 2001-06-01 2009-12-24 Hoffmann La Roche Pyrimidin, triazin und pyrazinderivate als glutamatrezeptoren
US20050013939A1 (en) 2001-06-15 2005-01-20 Peter Vinden Boron-based wood preservatives and treatment of wood with boron-based preservatives
WO2002102313A2 (en) 2001-06-19 2002-12-27 Bristol-Myers Squibb Company Pyrimidine inhibitors of phosphodiesterase (pde) 7
WO2003000181A2 (en) 2001-06-20 2003-01-03 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment of diabetes
JP2004535433A (ja) 2001-06-20 2004-11-25 メルク エンド カムパニー インコーポレーテッド 糖尿病治療用のジペプチジルペプチダーゼ阻害薬
US6825198B2 (en) 2001-06-21 2004-11-30 Pfizer Inc 5-HT receptor ligands and uses thereof
GB0115517D0 (en) 2001-06-25 2001-08-15 Ferring Bv Novel antidiabetic agents
CA2451128A1 (en) 2001-06-26 2003-01-09 Bristol-Myers Squibb Company N-heterocyclic inhibitors of tnf-alpha expression
DE60222667T2 (de) 2001-06-27 2008-07-17 Smithkline Beecham Corp. Fluorpyrrolidine als dipeptidylpeptidaseinhibitoren
AU2002321135B2 (en) 2001-06-27 2007-11-08 Probiodrug Ag Dipepitdyl peptidase IV inhibitors and their uses as anti-cancer agents
US7368421B2 (en) 2001-06-27 2008-05-06 Probiodrug Ag Use of dipeptidyl peptidase IV inhibitors in the treatment of multiple sclerosis
EP1399420B1 (en) 2001-06-27 2007-12-05 SmithKline Beecham Corporation Pyrrolidines as dipeptidyl peptidase inhibitors
US20030130199A1 (en) 2001-06-27 2003-07-10 Von Hoersten Stephan Dipeptidyl peptidase IV inhibitors and their uses as anti-cancer agents
DE60221983T2 (de) 2001-06-27 2008-05-15 Smithkline Beecham Corp. Fluorpyrrolidine als dipeptidyl-peptidase inhibitoren
RU2299066C2 (ru) 2001-06-27 2007-05-20 Пробиодруг Аг Новые ингибиторы дипептидилпептидазы iv и их применение в качестве противораковых агентов
DE10154689A1 (de) 2001-11-09 2003-05-22 Probiodrug Ag Substituierte Aminoketonverbindungen
ATE388951T1 (de) 2001-07-03 2008-03-15 Novo Nordisk As Dpp-iv-inhibierende purin-derivative zur behandlung von diabetes
US6869947B2 (en) 2001-07-03 2005-03-22 Novo Nordisk A/S Heterocyclic compounds that are inhibitors of the enzyme DPP-IV
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
GB0117899D0 (en) 2001-07-23 2001-09-12 Astrazeneca Ab Chemical compounds
DE10143840A1 (de) 2001-09-06 2003-03-27 Probiodrug Ag Neue Inhibitoren der Dipeptidylpeptidase I
US6844316B2 (en) 2001-09-06 2005-01-18 Probiodrug Ag Inhibitors of dipeptidyl peptidase I
US20040259883A1 (en) 2001-09-14 2004-12-23 Hiroshi Sakashita Thiazolidine derivative and medicinal use thereof
JPWO2003026661A1 (ja) 2001-09-14 2005-01-06 山之内製薬株式会社 インスリン分泌促進剤及び新規なピリミジン誘導体
WO2003024965A2 (en) 2001-09-19 2003-03-27 Novo Nordisk A/S Heterocyclic compounds that are inhibitors of the enzyme dpp-iv
US6825184B2 (en) 2001-10-18 2004-11-30 Boehringer Ingelheim Pharmaceuticals, Inc. 1,4-Disubstituted benzo-fused urea compounds
GB0125445D0 (en) 2001-10-23 2001-12-12 Ferring Bv Protease Inhibitors
GB0125446D0 (en) 2001-10-23 2001-12-12 Ferring Bv Novel anti-diabetic agents
US6861440B2 (en) 2001-10-26 2005-03-01 Hoffmann-La Roche Inc. DPP IV inhibitors
EP1470246A2 (en) 2001-10-31 2004-10-27 Novartis AG Methods to treat diabetes and related conditions based on polymorphisms in the tcf1 gene
US20030125304A1 (en) 2001-11-09 2003-07-03 Hans-Ulrich Demuth Substituted amino ketone compounds
EP2769715A3 (en) 2001-11-26 2014-09-17 Trustees Of Tufts College Methods for treating autoimmune disorders, and reagents related thereto
EP2316470A3 (en) 2001-11-26 2011-08-24 Trustees Of Tufts College Peptidomimetic inhibitors of post-proline cleaving enzymes
SE0104334D0 (sv) 2001-12-19 2001-12-19 Astrazeneca Ab Therapeutic agents
GB0229931D0 (en) 2002-12-21 2003-01-29 Astrazeneca Ab Therapeutic agents
WO2003057144A2 (en) 2001-12-26 2003-07-17 Guilford Pharmaceuticals Change inhibitors of dipeptidyl peptidase iv
US6727261B2 (en) 2001-12-27 2004-04-27 Hoffman-La Roche Inc. Pyrido[2,1-A]Isoquinoline derivatives
EP1461069A2 (en) 2001-12-29 2004-09-29 Novo Nordisk A/S Combined use of a glp-1 compound and another drug for treating dyslipidemia
US20050043315A1 (en) 2002-01-02 2005-02-24 Hideo Tsutsumi Aminopyrimidine compounds, processes for their preparation and pharmaceutical compositions containing them
US20070225351A1 (en) 2002-01-11 2007-09-27 Lippa Arnold S Methods and compositions for controlling body weight and appetite
GB0201850D0 (en) 2002-01-26 2002-03-13 Astrazeneca Ab Therapeutic treatment
EP1480999A2 (en) 2002-02-08 2004-12-01 Idun Pharmaceuticals (substituted)acyl dipeptidyl inhibitors of the ice/ced-3 family of cysteine proteases
ATE309988T1 (de) 2002-02-13 2005-12-15 Hoffmann La Roche Neue pyridin- und quinolin-derivate
JP4359146B2 (ja) 2002-02-13 2009-11-04 エフ.ホフマン−ラ ロシュ アーゲー 新規なピリジン−およびピリミジン−誘導体
US6906074B2 (en) 2002-02-22 2005-06-14 Nippon Zoki Pharmaceutical Co., Ltd. 2-phenylpiperazine derivatives
JP2004043429A (ja) 2002-02-25 2004-02-12 Eisai Co Ltd 新規キサンチン誘導体およびdppiv阻害剤
US7074798B2 (en) 2002-02-25 2006-07-11 Eisai Co., Ltd Xanthine derivative and DPPIV inhibitor
HUP0600057A2 (en) 2002-02-28 2006-05-29 Prosidion Ltd Glutaminyl based dpiv inhibitors, pharmaceutical compositions comprising thereof and their use
HUP0200849A2 (hu) 2002-03-06 2004-08-30 Sanofi-Synthelabo N-aminoacetil-2-ciano-pirrolidin-származékok, e vegyületeket tartalmazó gyógyszerkészítmények és eljárás előállításukra
DE60336901D1 (de) 2002-03-07 2011-06-09 X Ceptor Therapeutics Inc Chinazolinon modulatoren von nukleinrezeptoren
EP1484971B1 (en) 2002-03-15 2007-07-04 Ciba SC Holding AG Use of 4-aminopyrimidines for the antimicrobial treatment of surfaces
AR039090A1 (es) 2002-03-22 2005-02-09 Novartis Ag Combinacion de compuestos organicos
JP2005526811A (ja) 2002-03-25 2005-09-08 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用β−アミノ複素環式ジペプチジルペプチダーゼ阻害剤
WO2003080633A1 (en) 2002-03-25 2003-10-02 Nippon Kayaku Kabushiki Kaisha Novel $g(a)-amino-n-(diaminophosphinyl)lactam derivative
JP4329382B2 (ja) 2002-04-04 2009-09-09 田辺三菱製薬株式会社 医薬組成物
JP4329381B2 (ja) 2002-04-04 2009-09-09 田辺三菱製薬株式会社 医薬組成物
CN1633420A (zh) 2002-04-08 2005-06-29 托伦脱药品有限公司 噻唑烷-4-腈和类似物以及它们作为二肽基-肽酶抑制剂的用途
JP2003300977A (ja) 2002-04-10 2003-10-21 Sumitomo Pharmaceut Co Ltd キサンチン誘導体
WO2003088962A1 (en) 2002-04-16 2003-10-30 Merck & Co., Inc. Combination therapy using a ppar alpha/gamma agonist
AU2003222786A1 (en) 2002-04-18 2003-10-27 Ucb, S.A. Chemical compounds with dual activity, processes for their preparation and pharmaceutical compositions
DE10219435A1 (de) 2002-05-02 2003-11-13 Bayer Cropscience Ag Substituierte Pyrazolo-pyrimidin-4-one
AU2003225305A1 (en) 2002-05-08 2003-11-11 Bristol-Myers Squibb Company Pyridine-based thyroid receptor ligands
JP2004026820A (ja) 2002-05-09 2004-01-29 Taisho Pharmaceut Co Ltd ジペプチジルペプチダーゼiv阻害剤
WO2003095425A1 (fr) 2002-05-09 2003-11-20 Taisho Pharmaceutical Co.,Ltd. Derives de cyanopyrrolidine
JP2003327532A (ja) 2002-05-10 2003-11-19 Takeda Chem Ind Ltd ペプチダーゼ阻害剤
US7057046B2 (en) 2002-05-20 2006-06-06 Bristol-Myers Squibb Company Lactam glycogen phosphorylase inhibitors and method of use
GB0212412D0 (en) 2002-05-29 2002-07-10 Novartis Ag Combination of organic compounds
CN101273987A (zh) 2002-06-03 2008-10-01 诺瓦提斯公司 取代的氰基吡咯烷和含有它们的组合制剂用于治疗高脂血症和相关疾病的用途
US6710040B1 (en) 2002-06-04 2004-03-23 Pfizer Inc. Fluorinated cyclic amides as dipeptidyl peptidase IV inhibitors
AU2003233010A1 (en) 2002-06-04 2003-12-19 Pfizer Products Inc. Process for the preparation of 3,3,4,4-tetrafluoropyrrolidine and derivatives thereof
AU2003232405A1 (en) 2002-06-04 2003-12-19 Pfizer Products Inc. Flourinated cyclic amides as dipeptidyl peptidase iv inhibitors
CA2485641C (en) 2002-06-06 2010-12-14 Eisai Co., Ltd. Novel condensed imidazole derivatives
WO2003103632A1 (en) 2002-06-10 2003-12-18 Elan Pharma International, Ltd. Nanoparticulate polycosanol formulations and novel polycosanol combinations
AU2003241478A1 (en) 2002-06-10 2003-12-22 Elan Pharma International, Ltd. Nanoparticulate sterol formulations and sterol combinations
AR040241A1 (es) 2002-06-10 2005-03-23 Merck & Co Inc Inhibidores de la 11-beta-hidroxiesteroide deshidrogrenasa 1 para el tratamiento de la diabetes obesidad y dislipidemia
EP1531799A1 (en) 2002-06-10 2005-05-25 Elan Pharma International Limited Nanoparticulate formulations comprising hmg coa reductase inhibitor derivatives ("statins"), novel combinations thereof as well as manufacturing of these pharmaceutical compositions
DE60335639D1 (de) 2002-06-14 2011-02-17 Amylin Pharmaceuticals Inc Prävention und/oder behandlung von colitis ulcerosa mit pyy oder pyyä3-36ü
HUP0202001A2 (hu) 2002-06-14 2005-08-29 Sanofi-Aventis DDP-IV gátló hatású azabiciklooktán- és nonánszármazékok
DE10226943A1 (de) 2002-06-17 2004-01-08 Bayer Ag Phenylaminopyrimidine und ihre Verwendung
GB0214254D0 (en) 2002-06-20 2002-07-31 Glaxo Group Ltd Chemical compounds
SE0201976D0 (sv) 2002-06-24 2002-06-24 Astrazeneca Ab Novel compounds
JP2004026678A (ja) 2002-06-24 2004-01-29 Microbial Chem Res Found 2型糖尿病治療剤
SE0201980D0 (sv) 2002-06-24 2002-06-24 Astrazeneca Ab Novel compounds
JP5219329B2 (ja) 2002-06-28 2013-06-26 ネステク、リミテッド 下痢の予防又は治療用の医薬組成物
US20040053842A1 (en) 2002-07-02 2004-03-18 Pfizer Inc. Methods of treatment with CETP inhibitors and antihypertensive agents
US7071210B2 (en) 2002-07-02 2006-07-04 Pfizer Inc. CETP inhibitors in combination with antihypertensive agents and uses thereof
EP1578362A4 (en) 2002-07-09 2008-11-05 Point Therapeutics Inc COMBINATION THERAPY WITH A BOROPROLINE COMPOUND
JPWO2004007446A1 (ja) 2002-07-10 2005-11-10 アステラス製薬株式会社 新規なアゼチジン誘導体又はその塩
DE10231370B4 (de) 2002-07-11 2006-04-06 Sanofi-Aventis Deutschland Gmbh Thiophenglycosidderivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zur Herstellung dieser Arzneimittel
CA2490818A1 (en) 2002-07-15 2004-01-22 Merck & Co., Inc. Piperidino pyrimidine dipeptidyl peptidase inhibitors for the treatment of diabetes
AU2003261204A1 (en) 2002-07-23 2004-02-09 Smithkline Beecham Corporation Pyrazolopyrimidines as kinase inhibitors
TW200401635A (en) 2002-07-23 2004-02-01 Yamanouchi Pharma Co Ltd 2-Cyano-4-fluoropyrrolidine derivative or salt thereof
WO2004009597A2 (en) 2002-07-23 2004-01-29 Smithkline Beecham Corporation Pyrazolopyrimidines as protein kinase inhibitors
JP2006514918A (ja) 2002-07-23 2006-05-18 スミスクライン ビーチャム コーポレーション キナーゼインヒビターとしてのピラゾロピリミジン
US20060105445A1 (en) 2002-07-29 2006-05-18 Klaus Godl Medium and method for enriching, purifying or depleting atp binding proteins from a pool of proteins
EP1539137B1 (en) 2002-07-30 2010-05-26 Merck Sharp & Dohme Corp. Ppar alpha selective compounds for the treatment of dyslipidemia and other lipid disorders
AU2003256842B8 (en) 2002-07-30 2009-06-18 Merck Sharp & Dohme Corp. PPAR alpha selective compounds for the treatment of dyslipidemia and other lipid disorders
JP2004067575A (ja) 2002-08-06 2004-03-04 Yaizu Suisankagaku Industry Co Ltd 糖尿病治療薬効果促進剤
JP4542757B2 (ja) 2002-08-08 2010-09-15 武田薬品工業株式会社 縮合複素環化合物
PL376372A1 (en) 2002-08-08 2005-12-27 Amgen Inc. Vanilloid receptor ligands and their use in treatments
DE60322224D1 (de) 2002-08-08 2008-08-28 Takeda Pharmaceutical Kondensierte heterozyklische verbindungen als petidase inhibitoren
DE10237722A1 (de) 2002-08-17 2004-08-19 Aventis Pharma Deutschland Gmbh Indol- oder Benzimidazolderivate zur Modulation der IKappaB-Kinase
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
EA016166B1 (ru) 2002-08-21 2012-02-28 Бёрингер Ингельхайм Фарма Гмбх & Ко. Кг 8-[3-аминопиперидин-1-ил]ксантины, способ их получения и их применение в качестве лекарственных средств
EP1545540A2 (en) 2002-08-21 2005-06-29 Merck & Co., Inc. Combination therapy using a dual ppar alpha/gamma agonist and an angiotensin ii type i receptor antagonist
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
DE10238477A1 (de) 2002-08-22 2004-03-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Purinderivate, deren Herstellung und deren Verwendung als Arzneimittel
DE10238470A1 (de) 2002-08-22 2004-03-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Xanthinderivate, deren Herstellung und deren Verwendung als Arzneimittel
EA007613B1 (ru) 2002-08-29 2006-12-29 Тайсо Фармасьютикал Ко., Лтд. Бензолсульфонатная соль (2s,4s)-1-циано-4-фтор-1-[(2-гидрокси-1,1-диметил)этиламино]ацетилпирролидина
BR0313825A (pt) 2002-08-29 2005-07-12 Merck & Co Inc Composto, composição farmacêutica, método para tratar de diabete mellitus tipo 2 em um mamìfero, e, uso de composto
AU2003260085B2 (en) 2002-08-29 2008-09-11 Merck & Co., Inc. Indoles having anti-diabetic activity
WO2004024943A1 (ja) 2002-09-11 2004-03-25 Yamanouchi Pharmaceutical Co., Ltd. インスリン含量増加剤スクリーニング方法
ATE368647T1 (de) 2002-09-19 2007-08-15 Abbott Lab Pharmazeutische zusammensetzung und ihre verwendung als inhibitoren von der dipeptidyl peptidase iv (dpp-iv)
JP2006510597A (ja) 2002-09-27 2006-03-30 メルク エンド カムパニー インコーポレーテッド 置換ピリミジン類
US7067658B2 (en) 2002-09-30 2006-06-27 Bristol-Myers Squibb Company Pyridino and pyrimidino pyrazinones
WO2004033431A2 (en) 2002-10-04 2004-04-22 Arena Pharmaceuticals, Inc. Hydroxypyrazoles for use against metabolic-related disorders
DE60315687T2 (de) 2002-10-07 2008-06-05 Merck & Co., Inc. Antidiabetische heterocyclische beta-aminoverbindungen als inhibitoren von dipeptidylpeptidase
WO2004033455A2 (en) 2002-10-08 2004-04-22 Novo Nordisk A/S Hemisuccinate salts of heterocyclic dpp-iv inhibitors
AU2003284111A1 (en) 2002-10-09 2004-05-04 Genaissance Pharmaceuticals, Inc. Itgb3 gene haplotypes and atorvastatin dose effects on hdl cholesterol
JP2006504755A (ja) 2002-10-15 2006-02-09 スミスクライン ビーチャム コーポレーション Gsk−3阻害薬としてのピリダジン化合物
NZ538897A (en) 2002-10-18 2007-02-23 Merck & Co Inc Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
AU2003282983A1 (en) 2002-10-23 2004-05-13 Bristol-Myers Squibb Company Glycinenitrile-based inhibitors of dipeptidyl peptidase iv and methods
US7129239B2 (en) 2002-10-28 2006-10-31 Pfizer Inc. Purine compounds and uses thereof
AU2003285007A1 (en) 2002-10-30 2004-06-07 Merck & Co., Inc. Kinase inhibitors
AU2003286776A1 (en) 2002-10-30 2004-06-07 Guilford Pharmaceuticals Inc. Novel inhibitors of dipeptidyl peptidase iv
AU2003280680A1 (en) 2002-11-01 2004-06-18 Sumitomo Pharmaceuticals Co., Ltd. Xanthine compound
DE60310991T2 (de) 2002-11-07 2007-10-18 Merck & Co, Inc. Phenylalaninderivate als hemmer der dipeptidyl peptidase zur behandlung oder prävention von diabetes
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
US7098235B2 (en) 2002-11-14 2006-08-29 Bristol-Myers Squibb Co. Triglyceride and triglyceride-like prodrugs of glycogen phosphorylase inhibiting compounds
JP2006508975A (ja) 2002-11-18 2006-03-16 ファイザー・プロダクツ・インク ジペプチジルペプチダーゼivを阻害するフッ素化環状アミド
UY28103A1 (es) 2002-12-03 2004-06-30 Boehringer Ingelheim Pharma Nuevas imidazo-piridinonas sustituidas, su preparación y su empleo como medicacmentos
DE10256264A1 (de) 2002-12-03 2004-06-24 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue substituierte Imidazo-pyridinone und Imidazo-pyridazinone, ihre Herstellung und ihre Verwendung als Arzneimittel
CA2508487A1 (en) 2002-12-04 2004-06-17 Merck & Co., Inc. Phenylalanine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US20040110241A1 (en) 2002-12-06 2004-06-10 Segal Mark S. Materials and methods for monitoring vascular endothelial function
US7420079B2 (en) 2002-12-09 2008-09-02 Bristol-Myers Squibb Company Methods and compounds for producing dipeptidyl peptidase IV inhibitors and intermediates thereof
CN100348189C (zh) 2002-12-10 2007-11-14 诺瓦提斯公司 DPP-IV抑制剂与PPAR-α化合物的组合
WO2004058174A2 (en) 2002-12-20 2004-07-15 Bayer Pharmaceuticals Corporation Indane acetic acid derivatives and their use as pharmaceutical agents, intermediates, and method of preparation
JO2397B1 (en) 2002-12-20 2007-06-17 ميرك شارب اند دوم كوربوريشن Terazol derivatives as beta-hydroxy steroid dihydrogenase-1 inhibitors
US20060052382A1 (en) 2002-12-20 2006-03-09 Duffy Joseph L 3-Amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
AU2003299791A1 (en) 2002-12-20 2004-07-22 Bayer Pharmaceuticals Corporation Substituted 3,5-dihydro-4h-imidazol-4-ones for the treatment of obesity
GB0230020D0 (en) 2002-12-23 2003-01-29 Syngenta Ltd Fungicides
GB0230021D0 (en) 2002-12-23 2003-01-29 Syngenta Ltd Fungicides
GEP20084540B (en) 2003-01-14 2008-11-25 Arena Pharm Inc 1,2,3-trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prpphylaxis and treatment of disorders related thereto such as diabetes and hyperglycemia
ATE359782T1 (de) 2003-01-16 2007-05-15 Sb Pharmco Inc Heteroaryl-substituierte pyrrol(2, 3- b)pyridin- derivate als crf-rezeptor-antagonisten
CA2512546A1 (en) 2003-01-17 2004-08-05 Merck & Co., Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
AU2004207444B2 (en) 2003-01-17 2008-07-31 Merck & Co., Inc. N-cyclohexylaminocarbonyl benzenesulfonamide derivatives
JP2004244412A (ja) 2003-01-20 2004-09-02 Kotobuki Seiyaku Kk 4位に置換基を有する2−シアノピロリジン誘導体及びその製造方法並びにそれを含有する薬剤
EP1595866B1 (en) 2003-01-31 2016-06-08 Sanwa Kagaku Kenkyusho Co., Ltd. Cyanopyrrolidines useful for the treatment of inter alia metabolic syndrome
AU2004210149A1 (en) 2003-01-31 2004-08-19 Merck & Co., Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
WO2004071454A2 (en) 2003-02-13 2004-08-26 Guilford Pharmaceuticals Inc. Substituted azetidine compounds as inhibitors of dipeptidyl peptidase iv
TW200418829A (en) 2003-02-14 2004-10-01 Avanir Pharmaceutics Inhibitors of macrophage migration inhibitory factor and methods for identifying the same
WO2004076413A2 (en) * 2003-02-24 2004-09-10 Arena Pharmaceuticals, Inc. Phenyl- and pyridylpiperidine-derivatives as modulators of glucose metabolism
AU2003207881A1 (en) 2003-02-28 2004-09-17 Aic Dipeptidyl peptidase inhibitors
WO2004076434A1 (en) 2003-02-28 2004-09-10 Aic Dipeptidyl peptidase inhibitors
JP2004269468A (ja) 2003-03-12 2004-09-30 Yamanouchi Pharmaceut Co Ltd ピリミジン誘導体又はその塩
JP2004269469A (ja) 2003-03-12 2004-09-30 Yamanouchi Pharmaceut Co Ltd ピリミジン誘導体又はその塩
ZA200507754B (en) 2003-03-14 2007-01-31 Astellas Pharma Inc C-glycoside derivatives and salts thereof
AR043515A1 (es) 2003-03-19 2005-08-03 Merck & Co Inc Procedimiento para preparar derivados quirales beta aminoacidos mediante hidrogenacion asimetrica
WO2004085661A2 (en) 2003-03-24 2004-10-07 Merck & Co., Inc Process to chiral beta-amino acid derivatives
US7550590B2 (en) 2003-03-25 2009-06-23 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
WO2004087650A2 (en) 2003-03-27 2004-10-14 Merck & Co. Inc. Process and intermediates for the preparation of beta-amino acid amide dipeptidyl peptidase-iv inhibitors
CN1795177A (zh) 2003-03-28 2006-06-28 辉瑞产品公司 作为治疗动脉粥样硬化和肥胖症的cetp抑制剂的 1 , 2 , 4 , -取代的1,2,3,4,-四氢-和1,2二氢-喹啉以及1, 2 , 3 , 4-四氢-喹喔啉衍生物
WO2004092128A1 (en) 2003-04-10 2004-10-28 Smithkline Beecham Corporation Anhydrous crystalline forms of (2s, 4s)-1-{(2r)-2-amino-3-‘4-methoxybenzyl)sulfonyl!-3-methylbutanoyl}-4-fluoropyrrolindine-2-carbonitrile
WO2004096806A1 (ja) 2003-04-30 2004-11-11 Sumitomo Pharmaceuticals Co. Ltd. 縮合イミダゾール誘導体
TWI494102B (zh) 2003-05-02 2015-08-01 Japan Tobacco Inc 包含s-〔2(〔〔1-(2-乙基丁基)環己基〕羰基〕胺基)苯基〕2-甲基丙烷硫酯及hmg輔酶a還原酶抑制劑之組合
US20040229848A1 (en) 2003-05-05 2004-11-18 Hans-Ulrich Demuth Glutaminyl based DP IV-inhibitors
ATE475421T1 (de) 2003-05-06 2010-08-15 Ustav Ex Botan Akademie Ved Ce Pyrazoloä4,3-düpyrimidines, verfahren zur ihre herstellung und deren verwendung
US7083933B1 (en) 2003-05-09 2006-08-01 Prosidion Limited Methods for identification of modulators of OSGPR116 activity
SE0301368D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab Chemical compounds
WO2004103276A2 (en) 2003-05-14 2004-12-02 Merck & Co., Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
JP2007511467A (ja) 2003-05-14 2007-05-10 タケダ サン ディエゴ インコーポレイテッド ジペプチジルペプチダーゼインヒビター
US6987118B2 (en) 2003-05-21 2006-01-17 Pfizer Inc. Tetrahydroisoquinoline derivatives as PPAR-alpha activators
EP1631679A2 (en) 2003-05-21 2006-03-08 Bayer HealthCare AG Diagnostics and therapeutics for diseases associated with dipeptidylpeptidase 7 (dpp7)
WO2004104216A2 (en) 2003-05-21 2004-12-02 Bayer Healthcare Ag Diagnostics and therapeutics for diseases associated with dipeptidylpeptidase iv (dpp4)
AU2003902828A0 (en) 2003-06-05 2003-06-26 Fujisawa Pharmaceutical Co., Ltd. Dpp-iv inhibitor
EP1635773A2 (en) 2003-06-06 2006-03-22 Merck & Co., Inc. (a New Jersey corp.) Combination therapy for the treatment of hypertension
CA2526770A1 (en) 2003-06-06 2004-12-23 Merck & Co., Inc. Fused indoles as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
EP1635832A2 (en) 2003-06-06 2006-03-22 Merck & Co., Inc. Combination therapy for the treatment of diabetes
AU2003902882A0 (en) 2003-06-10 2003-06-26 Fujisawa Pharmaceutical Co., Ltd. Piperidyl derivatives
AU2003902946A0 (en) 2003-06-12 2003-06-26 Fujisawa Pharmaceutical Co., Ltd. Dpp-iv inhibitor
WO2004112701A2 (en) 2003-06-17 2004-12-29 Merck & Co., Inc. Cyclohexylglycine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
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
EP1638970B1 (en) 2003-06-20 2010-11-24 F. Hoffmann-La Roche AG Pyrid (2, 1-a) - isoquinoline derivatives as dpp-iv inhibitors
CN101090901B (zh) 2003-06-20 2010-12-15 霍夫曼-拉罗奇有限公司 作为dpp-iv抑制剂的六氢吡啶并异喹啉类
JO2625B1 (en) 2003-06-24 2011-11-01 ميرك شارب اند دوم كوربوريشن Phosphoric acid salts of dipeptidyl betidase inhibitor 4
JP2005023038A (ja) 2003-07-04 2005-01-27 Taisho Pharmaceut Co Ltd 慢性腎疾患治療薬
US20050005717A1 (en) 2003-07-10 2005-01-13 Pfizer Inc Probe holder
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
KR20060056944A (ko) 2003-07-14 2006-05-25 아레나 파마슈티칼스, 인크. 대사 조절제로서 융합된 아릴 및 헤테로아릴 유도체 및이에 관련된 장애의 예방 또는 치료
AU2004259741A1 (en) 2003-07-21 2005-02-03 Smithkline Beecham Corporation (2S,4S)-4-fluoro-1-[4-fluoro-beta-(4-fluorophenyl)-L-phenylalanyl]-2-pyrrolidinecarbonitrile p-toluenesulfonic acid salt and anhydrous crystalline forms thereof
US7008957B2 (en) 2003-07-25 2006-03-07 Sanofi-Aventis Deutschland Gmbh Bicyclic cyanoheterocycles, process for their preparation and their use as medicaments
PE20050249A1 (es) 2003-07-25 2005-06-01 Aventis Pharma Gmbh Nuevas cianopirrolididas y procedimiento para su preparacion como medicamentos
US7094800B2 (en) 2003-07-25 2006-08-22 Sanofi-Aventis Deutschland Gmbh Cyanopyrrolidides, process for their preparation and their use as medicaments
DE10333935A1 (de) 2003-07-25 2005-02-24 Aventis Pharma Deutschland Gmbh Neue bicyclische Cyanoheterocyclen, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
US7259160B2 (en) 2003-07-31 2007-08-21 Merck & Co., Inc. Hexahydrodiazepinones as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
US6995183B2 (en) 2003-08-01 2006-02-07 Bristol Myers Squibb Company Adamantylglycine-based inhibitors of dipeptidyl peptidase IV and methods
LT2896397T (lt) 2003-08-01 2017-11-27 Mitsubishi Tanabe Pharma Corporation Nauji junginiai, turintys inhibitorinį aktyvumą prieš nuo natrio priklausomą gliukozės transporterį
MXPA06001759A (es) 2003-08-15 2006-05-12 Novartis Ag 2,4-pirimidinadiaminas utiles en el tratamiento de enfermedades neoplasticas, desordenes del sistema inmune e inflamatorios.
WO2005019168A2 (en) 2003-08-20 2005-03-03 Pfizer Products Inc. Fluorinated lysine derivatives as dipeptidyl peptidase iv inhibitors
US20050043327A1 (en) 2003-08-21 2005-02-24 Pfizer Inc Pharmaceutical composition for the prevention and treatment of addiction in a mammal
JP2007504230A (ja) 2003-09-02 2007-03-01 メルク エンド カムパニー インコーポレーテッド ジペプチジルペプチダーゼ−iv阻害剤のリン酸塩の新規結晶性形態
WO2005023762A1 (en) 2003-09-04 2005-03-17 Abbott Laboratories Pyrrolidine-2-carbonitrile derivatives and their use as inhibitors of dipeptidyl peptidase-iv (dpp-iv)
TW201127828A (en) 2003-09-05 2011-08-16 Vertex Pharma Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
JP2007513058A (ja) 2003-09-08 2007-05-24 武田薬品工業株式会社 ジペプチジルぺプチダーゼ阻害剤
EP1699777B1 (en) 2003-09-08 2012-12-12 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
WO2005025554A2 (en) 2003-09-09 2005-03-24 Japan Tobacco Inc. Dipeptidyl peptidase iv inhibitor
WO2005030127A2 (en) 2003-09-23 2005-04-07 Merck & Co., Inc. Novel crystalline form of a phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor
CN1856307A (zh) 2003-09-23 2006-11-01 默克公司 喹啉钾通道抑制剂
CA2540741A1 (en) 2003-10-03 2005-04-14 Takeda Pharmaceutical Company Limited Agent for treating diabetes
WO2005033099A2 (en) 2003-10-03 2005-04-14 Glenmark Pharmaceuticals Ltd. Novel dipeptidyl peptidase iv inhibitors; processes for their preparation and compositions thereof
US20060089335A1 (en) 2003-10-14 2006-04-27 Guosong Liu Compositions and methods for enhancing cognitive function and synaptic plasticity
DE10348022A1 (de) 2003-10-15 2005-05-25 Imtm Gmbh Neue Dipeptidylpeptidase IV-Inhibitoren zur funktionellen Beeinflussung unterschiedlicher Zellen und zur Behandlung immunologischer, entzündlicher, neuronaler und anderer Erkrankungen
DE10348044A1 (de) 2003-10-15 2005-05-19 Imtm Gmbh Duale Alanyl-Aminopeptidase- und Dipeptidylpeptidase IV-Inhibitoren zur funktionellen Beeinflussung unterschiedlicher Zellen und zur Behandlung immunologischer, entzündlicher, neuronaler und anderer Erkrankungen
GB0324236D0 (en) 2003-10-16 2003-11-19 Astrazeneca Ab Chemical compounds
TW200519105A (en) 2003-10-20 2005-06-16 Lg Life Science Ltd Novel inhibitors of DPP-IV, methods of preparing the same, and pharmaceutical compositions containing the same as an active agent
PE20050444A1 (es) 2003-10-31 2005-08-09 Takeda Pharmaceutical Compuestos de piridina como inhibidores de la peptidasa
CN1870990A (zh) 2003-11-04 2006-11-29 默克公司 作为糖尿病治疗或预防用二肽基肽酶iv抑制剂的稠合苯基丙氨酸衍生物
US7338951B2 (en) 2003-11-10 2008-03-04 Synta Pharmaceuticals Corp. Pyridine compounds
EP1743676A1 (en) 2003-11-12 2007-01-17 Phenomix Corporation Heterocyclic boronic acid derivatives, dipeptidyl peptidase IV inhibitors
MY141220A (en) 2003-11-17 2010-03-31 Astrazeneca Ab Pyrazole derivatives as inhibitors of receptor tyrosine kinases
WO2005049022A2 (en) 2003-11-17 2005-06-02 Novartis Ag Use of dipeptidyl peptidase iv inhibitors
WO2005058315A1 (en) 2003-12-12 2005-06-30 Ribapharm, Inc. Novel heterocyclic compounds as ikk2 inhibitors with anti-hbv activity
WO2005058849A1 (en) 2003-12-15 2005-06-30 Glenmark Pharmaceuticals Ltd. New dipeptidyl peptidase in inhibitors; process for their preparation and compositions containing them
DE10360835A1 (de) 2003-12-23 2005-07-21 Boehringer Ingelheim Pharma Gmbh & Co. Kg Bicyclische Imidazolverbindungen, deren Herstellung und deren Verwendung als Arzneimittel
WO2005061489A1 (en) 2003-12-24 2005-07-07 Prosidion Limited Heterocyclic derivatives as gpcr receptor agonists
US20080227786A1 (en) 2004-01-16 2008-09-18 Ferlita Russell R Novel Crystalline Salts of a Dipeptidyl Peptidase-IV Inhibitor
WO2005075426A1 (en) 2004-02-03 2005-08-18 Glenmark Pharmaceuticals Ltd. Novel dipeptidyl peptidase iv inhibitors; processes for their preparation and compositions thereof
KR101130433B1 (ko) 2004-02-05 2012-03-27 교린 세이야꾸 가부시키 가이샤 비시클로에스테르 유도체
WO2005077938A1 (en) 2004-02-11 2005-08-25 Amgen Inc. Vanilloid receptor ligands and their use in treatments
KR20060124712A (ko) 2004-02-20 2006-12-05 노파르티스 아게 신경퇴행 및 인지 장애를 치료하기 위한 dpp ⅳ 억제제
EP1732885A1 (en) 2004-02-23 2006-12-20 Trustees Of Tufts College Lactams as conformationally constrained peptidomimetic inhibitors
US20050203027A1 (en) 2004-02-23 2005-09-15 Trustees Of Tufts College Inhibitors of dipeptidylpeptidase IV
TW200530236A (en) 2004-02-23 2005-09-16 Chugai Pharmaceutical Co Ltd Heteroaryl phenylurea
CA2559611C (en) 2004-03-09 2012-01-17 National Health Research Institutes Pyrrolidine compounds
NZ549716A (en) 2004-03-15 2010-04-30 Takeda Pharmaceutical Pyrimidin-dione derivatives as dipeptidyl peptidase inhibitors
WO2005092877A1 (de) 2004-03-16 2005-10-06 Boehringer Ingelheim International Gmbh Glucopyranosyl-substituierte benzol-derivate, diese verbindungen enthaltende arzneimittel, deren verwendung und verfahren zu ihrer herstellung
GB0405933D0 (en) 2004-03-16 2004-04-21 Glaxo Group Ltd Compounds
US20070219234A1 (en) 2004-04-12 2007-09-20 Kiyoshi Oizumi Thienopyridine Derivatives
AU2005249380C1 (en) 2004-04-23 2012-09-20 Exelixis, Inc. Kinase modulators and methods of use
AP2320A (en) 2004-05-12 2011-11-07 Pfizer Procucts Inc Proline derivatives and their use as dipeptidyl peptidase IV inhibitors.
MXPA06014129A (es) * 2004-06-04 2007-03-07 Arena Pharm Inc Derivados de arilo y heteroarilo sustituidos como moduladores del metabolismo y profilaxis y tratamiento de trastornos relacionados con los mismos.
US7453002B2 (en) * 2004-06-15 2008-11-18 Bristol-Myers Squibb Company Five-membered heterocycles useful as serine protease inhibitors
DE102004038270A1 (de) 2004-08-06 2006-03-16 Sanofi-Aventis Deutschland Gmbh Substituierte, bizyklische 8-Amino-xanthine, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
WO2006034446A2 (en) 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Pyridine derivatives for inhibiting human stearoyl-coa-desaturase
WO2006039325A2 (en) 2004-10-01 2006-04-13 Merck & Co., Inc. Aminopiperidines as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
EP1806347A4 (en) 2004-10-08 2009-07-01 Astellas Pharma Inc PYRIMIDINE DERIVATIVES FUSED WITH AN AROMATIC RING
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
TW200621257A (en) 2004-10-20 2006-07-01 Astellas Pharma Inc Pyrimidine derivative fused with nonaromatic ring
AR051596A1 (es) 2004-10-26 2007-01-24 Irm Llc Compuestos heterociclicos condensados nitrogenados como inhibidores de la actividad del receptor canabinoide 1; composiciones farmaceuticas que los contienen y su empleo en la preparacion de medicamentos para el tratamiento de trastornos alimentarios
AU2005305083B2 (en) 2004-11-03 2012-02-02 Arena Pharmaceuticals, Inc. GPR41 and modulators thereof for the treatment of insulin-related disorders
GB0425035D0 (en) 2004-11-12 2004-12-15 Novartis Ag Organic compounds
EP1857118A1 (en) * 2004-12-13 2007-11-21 Daiichi Sankyo Company, Limited Medicinal composition for treating diabetes
MX2007007553A (es) 2004-12-24 2007-08-15 Prosidion Ltd Agonistas del receptor acoplado a proteina g (gpr116) y uso de los mismos para tratar obesidad y diabetes.
US8193359B2 (en) 2004-12-24 2012-06-05 Prosidion Limited G-protein coupled receptor agonists
KR20070090206A (ko) 2004-12-24 2007-09-05 다이닛본 스미토모 세이야꾸 가부시끼가이샤 2환식 피롤 유도체
GB0428514D0 (en) 2004-12-31 2005-02-09 Prosidion Ltd Compounds
DOP2006000010A (es) 2005-01-10 2006-07-31 Arena Pharm Inc Procedimiento para preparar eteres aromáticos
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
DOP2006000009A (es) 2005-01-13 2006-08-15 Arena Pharm Inc Procedimiento para preparar eteres de pirazolo [3,4-d] pirimidina
US20080124384A1 (en) 2005-01-19 2008-05-29 Blum Charles A Heteroaryl Substituted Piperazinyl-Pyridine Analogues
TW200637869A (en) 2005-01-28 2006-11-01 Chugai Pharmaceutical Co Ltd The spiroketal derivatives and the use as therapeutical agent for diabetes of the same
CN102372705A (zh) 2005-02-18 2012-03-14 田边三菱制药株式会社 脯氨酸衍生物的盐,其溶剂合物,及其生产方法
EP1888571A2 (en) 2005-03-22 2008-02-20 F. Hoffmann-Roche AG New salt and polymorphs of a dpp-iv inhibitor
US7553861B2 (en) 2005-04-22 2009-06-30 Alantos Pharmaceuticals Holding, Inc. Dipeptidyl peptidase-IV inhibitors
EP1902730A4 (en) 2005-06-09 2009-11-11 Banyu Pharma Co Ltd NPY Y2 AGONIST FOR USE AS A THERAPEUTIC AGENT AGAINST DIARRHEA-ASSOCIATED DISEASE
AU2006264651A1 (en) 2005-06-30 2007-01-11 Prosidion Limited G-protein coupled receptor agonists
EP1899329B1 (en) 2005-07-01 2011-10-05 Irm Llc Pyrimidine-substituted benzimidazole derivatives as protein kinase inhibitors
KR20080031936A (ko) 2005-08-04 2008-04-11 노파르티스 아게 빌다글립틴의 염
AU2006285005B2 (en) 2005-08-30 2012-03-29 Abbvie Inc. Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV)
TW200745079A (en) 2005-09-16 2007-12-16 Takeda Pharmaceuticals Co Polymorphs of benzoate salt of 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile and methods of use therefor
CA2619093A1 (en) 2005-09-16 2007-03-29 Arena Pharmaceuticals, Inc. Modulators of metabolism and the treatment of disorders related thereto
TW200745055A (en) 2005-09-23 2007-12-16 Organon Nv 4-Phenyl-6-substituted-pyrimidine-2-carbonitrile derivatives
ATE482947T1 (de) 2005-12-21 2010-10-15 Hoffmann La Roche Neues salz und polymorph des dpp-iv-hemmers
ZA200805192B (en) 2005-12-29 2009-11-25 Lexicon Pharmaceuticals Inc Multicyclic amino acid derivatives and methods of their use
BRPI0621226A2 (pt) 2006-01-19 2012-07-10 Orchid Reseach Lab Ltd compostos heterociclos
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
ES2354390T3 (es) 2006-04-11 2011-03-14 Arena Pharmaceuticals, Inc. Procedimientos de uso del receptor gpr119 para identificar compuestos útiles para aumentar la masa ósea en un individuo.
CA2810839A1 (en) 2006-05-04 2007-11-15 Boehringer Ingelheim International Gmbh A polymorphic form of 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(r)-amino-piperidin-1-yl)-xanthine
WO2007148185A2 (en) 2006-06-21 2007-12-27 Pfizer Products Inc. Substituted 3 -amino- pyrrolidino-4 -lactams as dpp inhibitors
TW200811140A (en) 2006-07-06 2008-03-01 Arena Pharm Inc Modulators of metabolism and the treatment of disorders related thereto
TW200811147A (en) 2006-07-06 2008-03-01 Arena Pharm Inc Modulators of metabolism and the treatment of disorders related thereto
EP2043744A2 (en) 2006-07-13 2009-04-08 SmithKline Beecham Corporation Chemical compounds
WO2008025800A1 (en) 2006-08-30 2008-03-06 Biovitrum Ab (Publ) Pyrimidine compounds for treating gpr119 related disorders
CL2007002499A1 (es) 2006-08-30 2008-03-14 Phenomix Corp Sales citrato y tartrato de compuestos derivados de acido pirrolidinilaminoacetilpirrolidinboronico, inhibidores de dpp-iv; metodo de preparacion; forma solida; combinacion farmaceutica, util para el tratamiento de diabetes.
TW200838536A (en) 2006-11-29 2008-10-01 Takeda Pharmaceutical Polymorphs of succinate salt of 2-[6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethy]-4-fluor-benzonitrile and methods of use therefor
CA2671749C (en) 2006-12-06 2013-07-09 Smithkline Beecham Corporation Bicyclic compounds and uses as antidiabetics
JP2010513272A (ja) 2006-12-14 2010-04-30 メルク エンド カムパニー インコーポレーテッド アシルビピペリジニル化合物、そのような化合物を含む組成物、及び治療方法
WO2008109591A1 (en) 2007-03-08 2008-09-12 Lexicon Pharmaceuticals, Inc. Phlorizin analogs as inhibitors of sodium glucose co-transporter 2
JPWO2008114857A1 (ja) 2007-03-22 2010-07-08 杏林製薬株式会社 アミノアセチルピロリジンカルボニトリル誘導体の製造方法
WO2008128832A1 (en) 2007-04-18 2008-10-30 Nicox S.A. Nitroderivatives of non-peptidic renin inhibitors for the treatment of cardiovascular, renal and chronic liver disease, inflammations and metabolic syndrome
JP2010526145A (ja) 2007-05-04 2010-07-29 ブリストル−マイヤーズ スクイブ カンパニー [6,6]および[6,7]−二環式gpr119gタンパク質結合受容体アゴニスト
KR20100033419A (ko) * 2007-07-19 2010-03-29 메타볼렉스, 인코포레이티드 당뇨병 및 대사 장애의 치료를 위한 rup3 또는 gpr119 수용체의 작용제로서 n-아자시클릭 치환된 피롤, 피라졸, 이미다졸, 트리아졸 및 테트라졸 유도체
NZ583495A (en) 2007-09-20 2011-11-25 Irm Llc Compounds and compositions as modulators of gpr119 activity
TW200938200A (en) 2007-12-28 2009-09-16 Dainippon Sumitomo Pharma Co Methyl-substituted piperidine derivative
EP2146210A1 (en) 2008-04-07 2010-01-20 Arena Pharmaceuticals, Inc. Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditions modulated by PYY
JP2011516557A (ja) 2008-04-07 2011-05-26 アイアールエム・リミテッド・ライアビリティ・カンパニー Gpr119活性のモジュレーターとしての化合物および組成物
WO2009125434A2 (en) 2008-04-07 2009-10-15 Cadila Healthcare Limited Oxime derivatives
WO2010008739A2 (en) * 2008-06-20 2010-01-21 Metabolex, Inc. Aryl gpr119 agonists and uses thereof
WO2010075273A1 (en) * 2008-12-23 2010-07-01 Schering Corporation Bicyclic heterocycle derivatives and methods of use thereof
AU2009330208A1 (en) 2008-12-23 2011-08-04 Merck Sharp & Dohme Corp. Bicyclic heterocycle derivatives and methods of use thereof
WO2010074271A1 (ja) 2008-12-26 2010-07-01 武田薬品工業株式会社 糖尿病治療剤
TW201031668A (en) 2009-01-22 2010-09-01 Mitsubishi Tanabe Pharma Corp Novel pyrrolo[2,3-d] pyrimidine compound
AR077642A1 (es) 2009-07-09 2011-09-14 Arena Pharm Inc Moduladores del metabolismo y el tratamiento de trastornos relacionados con el mismo
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
WO2011030139A1 (en) 2009-09-11 2011-03-17 Astrazeneca Ab 4- (pyrimidin-2-yl) -piperazine and 4- (pyrimidin-2-yl) -piperidine derivatives as gpr119 modulators
US8440693B2 (en) 2009-12-22 2013-05-14 Novartis Ag Substituted isoquinolinones and quinazolinones
CA2795513A1 (en) 2010-04-06 2011-10-13 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
CN103221410B (zh) 2010-09-22 2017-09-15 艾尼纳制药公司 Gpr119受体调节剂和对与其相关的障碍的治疗
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
WO2012170702A1 (en) 2011-06-08 2012-12-13 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2013055910A1 (en) 2011-10-12 2013-04-18 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto

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