ATE253073T1 - Neue benzimidazol inhibitoren der fructose-1,6- bisphosphatase - Google Patents

Neue benzimidazol inhibitoren der fructose-1,6- bisphosphatase

Info

Publication number
ATE253073T1
ATE253073T1 AT98909031T AT98909031T ATE253073T1 AT E253073 T1 ATE253073 T1 AT E253073T1 AT 98909031 T AT98909031 T AT 98909031T AT 98909031 T AT98909031 T AT 98909031T AT E253073 T1 ATE253073 T1 AT E253073T1
Authority
AT
Austria
Prior art keywords
fructose
bisphosphatase
new benzimidazole
benzimidazole inhibitors
inhibitors
Prior art date
Application number
AT98909031T
Other languages
English (en)
Inventor
Srinivas Rao Kasibhatla
K Raja Reddy
Mark D Erion
Qun Dang
Gerard R Scarlato
M Rami Reddy
Original Assignee
Metabasis Therapeutics Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Metabasis Therapeutics Inc filed Critical Metabasis Therapeutics Inc
Application granted granted Critical
Publication of ATE253073T1 publication Critical patent/ATE253073T1/de

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6503Five-membered rings
    • C07F9/6506Five-membered rings having the nitrogen atoms in positions 1 and 3
    • C07F9/65068Five-membered rings having the nitrogen atoms in positions 1 and 3 condensed with carbocyclic rings or carbocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65586Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system at least one of the hetero rings does not contain nitrogen as ring hetero atom

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
AT98909031T 1997-03-07 1998-03-06 Neue benzimidazol inhibitoren der fructose-1,6- bisphosphatase ATE253073T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US4062797P 1997-03-07 1997-03-07
PCT/US1998/004498 WO1998039343A1 (en) 1997-03-07 1998-03-06 Novel benzimidazole inhibitors of fructose-1,6-bisphosphatase

Publications (1)

Publication Number Publication Date
ATE253073T1 true ATE253073T1 (de) 2003-11-15

Family

ID=21912034

Family Applications (1)

Application Number Title Priority Date Filing Date
AT98909031T ATE253073T1 (de) 1997-03-07 1998-03-06 Neue benzimidazol inhibitoren der fructose-1,6- bisphosphatase

Country Status (11)

Country Link
US (2) US6110903A (de)
EP (1) EP0970095B1 (de)
JP (1) JP2001515482A (de)
AT (1) ATE253073T1 (de)
AU (1) AU6691498A (de)
DE (1) DE69819311T2 (de)
DK (1) DK0970095T3 (de)
ES (1) ES2210728T3 (de)
PT (1) PT970095E (de)
WO (1) WO1998039343A1 (de)
ZA (1) ZA981936B (de)

Families Citing this family (115)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT970095E (pt) * 1997-03-07 2004-03-31 Metabasis Therapeutics Inc Novos inibidores benzimidazole de frutose-1,6-bisfosfatase
AU6452098A (en) 1997-03-07 1998-09-22 Metabasis Therapeutics, Inc. Novel purine inhibitors of fructose-1,6-bisphosphatase
US6312662B1 (en) * 1998-03-06 2001-11-06 Metabasis Therapeutics, Inc. Prodrugs phosphorus-containing compounds
AU767599B2 (en) 1998-03-06 2003-11-20 Metabasis Therapeutics, Inc. Novel prodrugs for phosphorus-containing compounds
CA2343027A1 (en) 1998-09-09 2000-03-16 Metabasis Therapeutics, Inc. Novel heteroaromatic inhibitors of fructose 1,6-bisphosphatase
ID28787A (id) 1998-11-03 2001-07-05 Basf Ag 2-fenilbenzimidazol tersubstitusi, pembuatannya dan penggunaannya
ATE300288T1 (de) * 1998-12-24 2005-08-15 Metabasis Therapeutics Inc Zusammensetzung enthaltend insulin- sensibilisierenden wirkstoffe und inhibitoren der fruktose-1,6-bisphosphatase (fbpase) zur behandlung von diabetes
US6756360B1 (en) * 1998-12-24 2004-06-29 Metabasis Therapeutics, Inc. Combination of FBPase inhibitors and insulin sensitizers for the treatment of diabetes
US7205404B1 (en) 1999-03-05 2007-04-17 Metabasis Therapeutics, Inc. Phosphorus-containing prodrugs
EP1724276A1 (de) 1999-03-05 2006-11-22 Metabasis Therapeutics, Inc. Neue Phosphor enthaltende Medikamentenvorläuferverbindungen
US6831069B2 (en) 1999-08-27 2004-12-14 Ribapharm Inc. Pyrrolo[2,3-d]pyrimidine nucleoside analogs
EP1210354A1 (de) 1999-09-08 2002-06-05 Metabasis Therapeutics, Inc. Prodrugs für leberspezifische verabreichung von arzneimitteln
US6965033B2 (en) * 1999-12-22 2005-11-15 Metabasis Therapeutics, Inc. Bisamidate phosphonate prodrugs
AU2006202624B2 (en) * 1999-12-22 2008-08-14 Metabasis Therapeutics, Inc. Novel bisamidate phosphonate prodrugs
ATE385421T1 (de) 2000-01-21 2008-02-15 Novartis Pharma Gmbh Zusammensetzungen bestehend aus dipeptidylpeptidase-iv inhibitoren und antidiabetica
RU2002126616A (ru) * 2000-03-08 2004-03-20 Метабэйсис Терапьютикс, Инк. (Us) Новые арильные ингибиторы фруктозо-1, 6-бисфосфатазы
US7563774B2 (en) * 2000-06-29 2009-07-21 Metabasis Therapeutics, Inc. Combination of FBPase inhibitors and antidiabetic agents useful for the treatment of diabetes
CZ20035A3 (cs) * 2000-07-06 2003-05-14 Metabasis Therapeutics, Inc. Kombinace FBPázových inhibitorů a antidiabetických činidel užitečná při léčení diabetes
JP4332496B2 (ja) * 2002-05-13 2009-09-16 メタバシス・セラピューティクス・インコーポレイテッド Pmeaおよびpmpa環生成合成
CA2485702C (en) * 2002-05-13 2011-07-19 Metabasis Therapeutics, Inc. Novel phosphonic acid based prodrugs of pmea and its analogues
KR101115210B1 (ko) * 2002-10-31 2012-04-12 메타베이시스 테라퓨틱스, 인크. 신규 시타라빈 모노포스페이트 전구약물
RU2422450C2 (ru) 2003-11-19 2011-06-27 Метабазис Терапеутикс, Инк. Новые фосфорсодержащие тиромиметики
US7129049B2 (en) * 2003-12-22 2006-10-31 Regents Of The University Of Minnesota Method of detecting equine glycogen storage disease IV
AU2005254940A1 (en) * 2004-06-08 2005-12-29 Metabasis Therapeutics, Inc. Lewis acid mediated synthesis of cyclic esters
WO2006023515A2 (en) * 2004-08-18 2006-03-02 Metabasis Therapeutics, Inc. Novel thiazole inhibitors of fructose 1,6-bisphosphatase
TWI375673B (en) 2005-04-11 2012-11-01 Abbott Lab 1h-benzimidazole-4-carboxamides substituted with a quaternary carbon at the 2-position are potent parp inhibitors
US7728026B2 (en) 2005-04-11 2010-06-01 Abbott Laboratories, Inc. 2-substituted-1 h-benzimidazile-4-carboxamides are PARP inhibitors
TW200720255A (en) 2005-07-13 2007-06-01 Taiho Pharmaceutical Co Ltd Benzoimidazole compound capable of inhibiting prostaglandin d synthetase
EP1752450A1 (de) 2005-08-01 2007-02-14 Merck Sante Imidazolderivate als Fruktose-1,6-biphosphataseinhibitoren und pharmazeutische Zusammensetzungen diese enthaltend
CN102908350B (zh) 2005-09-14 2014-07-23 武田药品工业株式会社 用于治疗糖尿病的二肽基肽酶抑制剂
ES2342007T3 (es) 2005-11-15 2010-06-30 Abbott Laboratories 1h-benzimidazol-4-carboxamidas sustituidos eficaces como inhibidores de (parp).
MX2008014004A (es) 2006-05-02 2008-11-12 Abbott Lab 1h-benzimidazol-4-carboxamidas sustituidas son inhibidores de parp potentes.
US8466096B2 (en) * 2007-04-26 2013-06-18 Afton Chemical Corporation 1,3,2-dioxaphosphorinane, 2-sulfide derivatives for use as anti-wear additives in lubricant compositions
US8067613B2 (en) 2007-07-16 2011-11-29 Abbott Laboratories Benzimidazole poly(ADP ribose)polymerase inhibitors
EP2058308A1 (de) 2007-11-12 2009-05-13 Merck Sante Benzimidazoldihydrothiadiazinonderivate als Fructose-1,6-biphosphatase-Hemmer und diese enthaltende pharmazeutische Zusammensetzungen.
PL2294066T3 (pl) 2008-04-28 2015-02-27 Janssen Pharmaceutica Nv Benzimidazole jako inhibitory hydroksylazy prolilowej
MX2011003239A (es) 2008-09-26 2011-04-28 Merck Sharp & Dohme Nuevos derivados de bencimidazol ciclicos utiles como agentes anti-diabeticos.
WO2010047982A1 (en) 2008-10-22 2010-04-29 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
JP5557845B2 (ja) * 2008-10-31 2014-07-23 メルク・シャープ・アンド・ドーム・コーポレーション 糖尿病用剤として有用な新規環状ベンゾイミダゾール誘導体
JO2870B1 (en) 2008-11-13 2015-03-15 ميرك شارب اند دوهم كورب Amino Tetra Hydro Pirans as Inhibitors of Peptide Dipeptide IV for the Treatment or Prevention of Diabetes
US8759539B2 (en) 2008-11-17 2014-06-24 Merck Sharp & Dohme Corp. Substituted bicyclic amines for the treatment of diabetes
WO2010083199A1 (en) 2009-01-19 2010-07-22 Abbott Laboratories Benzthiazole inhibitors of poly(adp-ribose)polymerase
US20120046364A1 (en) 2009-02-10 2012-02-23 Metabasis Therapeutics, Inc. Novel Sulfonic Acid-Containing Thyromimetics, and Methods for Their Use
EP2805951B1 (de) 2009-03-20 2018-03-14 Metabasis Therapeutics, Inc. Inhibitoren von Diacylglycerin-O-acyltransferase 1 (DGAT-1) und Verwendungen davon
WO2011011506A1 (en) 2009-07-23 2011-01-27 Schering Corporation Spirocyclic oxazepine compounds as stearoyl-coenzyme a delta-9 desaturase inhibitors
WO2011011508A1 (en) 2009-07-23 2011-01-27 Schering Corporation Benzo-fused oxazepine compounds as stearoyl-coenzyme a delta-9 desaturase inhibitors
EP2464228B1 (de) 2009-08-13 2017-12-06 Merck Sharp & Dohme Corp. Substituierte cyclopropylverbindungen, zusammensetzungen mit solchen verbindungen und behandlungsverfahren damit
EP2473047B1 (de) 2009-09-02 2014-08-13 Merck Sharp & Dohme Corp. Aminotetrahydropyrane als dipeptidylpeptidase-iv-inhibitoren zur behandlung oder prävention von diabetes
WO2011041293A1 (en) 2009-09-30 2011-04-07 Takeda Pharmaceutical Company Limited Pyrazolo [1, 5-a] pyrimidine derivatives as apoptosis signal-regulating kinase 1 inhibitors
PT2531501E (pt) 2010-02-03 2014-02-17 Takeda Pharmaceutical Inibidores da cinase de regulação do sinal de apoptose 1
EP2538783B1 (de) 2010-02-22 2016-06-01 Merck Sharp & Dohme Corp. Substituierte aminotetrahydrothiopyrane als dipeptidylpeptidase-iv-hemmer zur behandlung von diabetes
EP2538784B1 (de) 2010-02-25 2015-09-09 Merck Sharp & Dohme Corp. Benzimidazolderivate als antidiabetika
WO2011146358A1 (en) 2010-05-21 2011-11-24 Merck Sharp & Dohme Corp. Substituted seven-membered heterocyclic compounds as dipeptidyl peptidase-iv inhibitors for the treatment of diabetes
US8742110B2 (en) 2010-08-18 2014-06-03 Merck Sharp & Dohme Corp. Spiroxazolidinone compounds
KR101594002B1 (ko) 2010-10-06 2016-02-15 글락소스미스클라인 엘엘씨 Pi3 키나제 억제제로서의 벤즈이미다졸 유도체
EP2677869B1 (de) 2011-02-25 2017-11-08 Merck Sharp & Dohme Corp. Neue cyclische azabenzimidazolderivate als antidiabetika
US8957062B2 (en) 2011-04-08 2015-02-17 Merck Sharp & Dohme Corp. Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment
EP2714678A1 (de) 2011-06-02 2014-04-09 Intervet International B.V. Imidazolderivate
US9006228B2 (en) 2011-06-16 2015-04-14 Merck Sharp & Dohme Corp. Substituted cyclopropyl compounds, compositions containing such compounds, and methods of treatment
US9422266B2 (en) 2011-09-30 2016-08-23 Merck Sharp & Dohme Corp. Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment
EP2771000B1 (de) 2011-10-24 2016-05-04 Merck Sharp & Dohme Corp. Substituierte piperidinylverbindungen als gpr119-agonisten
AU2012328763A1 (en) 2011-10-25 2014-05-01 Janssen Pharmaceutica Nv Meglumine salt formulations of 1-(5,6-dichloro-1H-benzo(d)imidazol-2-yl)-1H-pyrazole-4-carboxylic acid
WO2013068328A1 (en) 2011-11-07 2013-05-16 Intervet International B.V. Bicyclo [2.2.2] octan-1-ylcarboxylic acid compounds as dgat-1 inhibitors
WO2013068439A1 (en) 2011-11-09 2013-05-16 Intervet International B.V. 4-amino-5-oxo-7,8-dihydropyrimido[5, 4 -f] [1, 4] oxazepine compounds as dgat1 inhibitors
CA2855009C (en) 2011-11-15 2019-07-09 Merck Sharp & Dohme Corp. Substituted cyclopropyl compounds useful as gpr119 agonists
EP2814485A4 (de) 2012-02-17 2015-08-26 Merck Sharp & Dohme Dipeptidylpeptidase-iv-inhibitoren zur behandlung oder prävention von diabetes
EP2838906A4 (de) 2012-04-16 2015-07-15 Kaneq Pharma Inc Fusionierte aromatische phosphonatderivate als vorläufer für ptp-1b-inhibitoren
EP2874622A4 (de) 2012-07-23 2015-12-30 Merck Sharp & Dohme Behandlung von diabetes mit dipeptidylpeptidase-iv-hemmern
RU2015106909A (ru) 2012-08-02 2016-09-27 Мерк Шарп И Доум Корп. Антидиабетические трициклические соединения
EP2888008B1 (de) 2012-08-22 2018-12-26 Merck Sharp & Dohme Corp. Neuartige azabenzimidazol-tetrahydrofuranderivate
WO2014031441A1 (en) 2012-08-22 2014-02-27 Merck Sharp & Dohme Corp. Novel benzimidazole tetrahydrofuran derivatives
EP2888005B1 (de) 2012-08-22 2019-04-03 Merck Sharp & Dohme Corp. Neuartige azabenzimidazol-hexahydrofuro[3,2-b]furan-derivate
EP2887807B1 (de) 2012-08-22 2019-09-18 Merck Sharp & Dohme Corp. Benzimidazol-hexahydrofuro[3,2-b]furanderivate als amp-aktivierte proteinkinase-aktivatoren
US9527839B2 (en) 2012-08-22 2016-12-27 Merck Sharp & Dohme Corp. Benzimidazole tetrahydropyran derivatives
EP2888006B1 (de) 2012-08-22 2019-04-24 Merck Sharp & Dohme Corp. Neuartige azabenzimidazol-tetrahydropyran-derivate als ampk aktivatoren
US9453038B2 (en) 2012-12-17 2016-09-27 Merck Sharp & Dohme Corp. Glucokinase activator compounds, compositions containing such compounds, and methods of treatment
WO2014139388A1 (en) 2013-03-14 2014-09-18 Merck Sharp & Dohme Corp. Novel indole derivatives useful as anti-diabetic agents
WO2015051496A1 (en) 2013-10-08 2015-04-16 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
EP3068768B1 (de) 2013-11-15 2019-07-31 Merck Sharp & Dohme Corp. Antidiabetische tricyclische verbindungen
WO2015089809A1 (en) 2013-12-19 2015-06-25 Merck Sharp & Dohme Corp. Antidiabetic substituted heteroaryl compounds
EP3097101B1 (de) 2014-01-24 2020-12-23 Merck Sharp & Dohme Corp. Isochinolinderivate als mgat2-inhibitoren
CN106061984A (zh) 2014-02-13 2016-10-26 配体药物公司 前药化合物及其用途
WO2015176267A1 (en) 2014-05-22 2015-11-26 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
EP3164136A4 (de) 2014-07-02 2018-04-04 Ligand Pharmaceuticals, Inc. Prodrug-verbindungen und verwendungen davon
WO2016022742A1 (en) 2014-08-08 2016-02-11 Merck Sharp & Dohme Corp. Antidiabetic bicyclic compounds
US10662171B2 (en) 2014-08-08 2020-05-26 Merck Sharp & Dohme Corp. Antidiabetic bicyclic compounds
WO2016022446A1 (en) 2014-08-08 2016-02-11 Merck Sharp & Dohme Corp. [5,6]-fused bicyclic antidiabetic compounds
JP6581656B2 (ja) 2014-10-24 2019-09-25 メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. グルカゴンおよびglp−1受容体のコアゴニスト
TN2017000113A1 (en) 2014-10-31 2018-07-04 Ngm Biopharmaceuticals Inc Compositions and methods of use for treating metabolic disorders
TW201625635A (zh) 2014-11-21 2016-07-16 默沙東藥廠 作為可溶性鳥苷酸環化酶活化劑之三唑并吡基衍生物
EP3078378B1 (de) 2015-04-08 2020-06-24 Vaiomer Verwendung von faktor-xa-inhibitoren zur regulierung von glykämie
US10245264B2 (en) 2015-05-27 2019-04-02 Merck Sharp & Dohme Corp. Substituted imidazo[1,2-a]pyrazines as soluble guanylate cyclase activators
EP3310782B1 (de) 2015-05-28 2021-12-01 Merck Sharp & Dohme Corp. Als lösliche guanylat-cyclase-aktivatoren geeignete imidazopyrazinylderivate
US10800826B2 (en) 2015-10-05 2020-10-13 Merck Sharp & Dohme Corp. Antibody peptide conjugates that have agonist activity at both the glucagon and glucagon-like peptide 1 receptors
EP3383868B1 (de) 2015-11-30 2022-10-05 Merck Sharp & Dohme LLC Arylsulfonamide als blt1-antagonisten
WO2017107052A1 (en) 2015-12-22 2017-06-29 Merck Sharp & Dohme Corp. Soluble guanylate cyclase stimulators
WO2017197555A1 (en) 2016-05-16 2017-11-23 Merck Sharp & Dohme Corp. Fused pyrazine derivatives useful as soluble guanylate cyclase stimulators
WO2017201683A1 (en) 2016-05-25 2017-11-30 Merck Sharp & Dohme Corp. Substituted tetrahydroisoquinoline compounds useful as gpr120 agonists
EP3496715B1 (de) 2016-08-15 2021-11-03 Merck Sharp & Dohme Corp. Zur veränderung der konzentrationen von gallensäuren nützliche verbindungen zur behandlung von diabetes und kardiometabolischen erkrankungen
EP3496716B1 (de) 2016-08-15 2021-11-03 Merck Sharp & Dohme Corp. Verbindungen zur änderung der konzentrationen von gallensäuren zur behandlung von diabetes und kardiometabolischen erkrankungen
EP3515891B1 (de) 2016-09-20 2023-03-08 Merck Sharp & Dohme LLC Substituierte 1-methyl-1,2,3,4-tetrahydroisochinolin-moleküle als allosterische pcsk9-bindemittel
BR112019009731A2 (pt) 2016-11-18 2019-08-13 Merck Sharp & Dohme composto, composição farmacêutica, uso de um composto, e, método de tratamento
WO2018107415A1 (en) 2016-12-15 2018-06-21 Merck Sharp & Dohme Corp. Hydroxy isoxazole compounds useful as gpr120 agonists
CA3087932A1 (en) 2018-01-09 2019-07-18 Ligand Pharmaceuticals, Inc. Acetal compounds and therapeutic uses thereof
JOP20190150A1 (ar) 2018-06-21 2019-12-21 Merck Sharp & Dohme مركبات مناهضة لـ pcsk9
US20220177465A1 (en) 2019-04-04 2022-06-09 Merck Sharp & Dohme Corp. Inhibitors of histone deacetylase-3 useful for the treatment of cancer, inflammation, neurodegeneration diseases and diabetes
TW202123960A (zh) 2019-08-30 2021-07-01 美商默沙東藥廠 Pcsk9拮抗劑化合物
EP3842060A1 (de) 2019-12-23 2021-06-30 Merck Sharp & Dohme Corp. Geheftete lactam-co-agonisten der glucagon- und glp-1-rezeptoren
EP3842449A1 (de) 2019-12-23 2021-06-30 Merck Sharp & Dohme Corp. Geklammerte olefin-co-agonisten der glucagon- und glp-1-rezeptoren
EP3842061A1 (de) 2019-12-23 2021-06-30 Merck Sharp & Dohme Corp. Geheftete triazol-co-agonisten der glucagon- und glp-1-rezeptoren
AR122092A1 (es) 2020-05-18 2022-08-10 Merck Sharp & Dohme Inhibidores de diacilglicerol o-aciltransferasa 2
CA3195014A1 (en) 2020-10-08 2022-04-14 Yeon-Hee Lim Preparation of benzimidazolone derivatives as novel diacylglyceride o-acyltransferase 2 inhibitors
EP4387645A1 (de) 2021-08-19 2024-06-26 Merck Sharp & Dohme LLC Verbindungen zur behandlung von erkrankungen im zusammenhang mit pcsk9-aktivität
US20230406885A1 (en) 2022-06-15 2023-12-21 Merck Sharp & Dohme Llc Cyclic peptides for trapping interleukin-1 beta
WO2024118858A1 (en) 2022-12-02 2024-06-06 Merck Sharp & Dohme Llc Preparation of fused azole derivatives as novel diacylglyceride o-acyltransferase 2 inhibitors

Family Cites Families (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1428137A (en) * 1972-09-27 1976-03-17 Ici Ltd Prostanoic acid derivatives
US4000305A (en) * 1972-09-27 1976-12-28 Imperial Chemical Industries Limited 15-, 16- AND 17-Indolyl or indolinyl nor prostanoic acid derivatives
DE2855659A1 (de) * 1978-12-22 1980-07-03 Bayer Ag Benzimidazolyl-2-alkan-phosphonsaeuren
NZ206920A (en) * 1983-01-28 1986-10-08 Schering Corp Phosphorus-containing amide,urea or carbamate derivatives and pharmaceutical compositions
ES2038692T4 (es) * 1986-11-21 2012-02-10 Novartis Ag Procedimiento para la obtencion de acidos alcanodifosfonicos substituidos.
US4968790A (en) * 1988-08-12 1990-11-06 American Cyanamid Company Antidiabetic phosphates
US4943629A (en) * 1988-08-12 1990-07-24 American Cyanamid Company Antidiabetic alpha-substituted phosphonates
US5658889A (en) * 1989-01-24 1997-08-19 Gensia Pharmaceuticals, Inc. Method and compounds for aica riboside delivery and for lowering blood glucose
IL93164A0 (en) * 1989-01-24 1990-11-05 Gensia Pharma Purine nucleosides and their medical use
DE3932953A1 (de) * 1989-10-03 1991-04-11 Boehringer Mannheim Gmbh Neue 2-bicyclo-benzimidazole, verfahren zu ihrer herstellung und diese verbindungen enthaltende arzneimittel
FR2658511B1 (fr) * 1990-02-16 1992-06-19 Union Pharma Scient Appl Nouveaux derives de benzimidazole et d'azabenzimidazole, antagonistes des recepteurs au thromboxane; leurs procedes de preparation, compositions pharmaceutiques les contenant.
DE4123341A1 (de) * 1991-07-15 1993-01-21 Thomae Gmbh Dr K Phenylalkylderivate, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung
US5124319A (en) * 1991-10-11 1992-06-23 American Home Products Corporation Benzimidazole phosphono-amino acids
TW222637B (de) * 1991-12-12 1994-04-21 Hoechst Ag
US5302586A (en) * 1991-12-19 1994-04-12 G. D. Searle & Co. Phosphonomethyl-imidazo[1,2-a]pyrimidine-2-carboxylic acid compounds for treatment of neurotoxic injury
ATE188704T1 (de) * 1992-05-21 2000-01-15 Otsuka Pharma Co Ltd Phosphonsäurediester-derivat
CA2145640C (en) * 1992-09-28 2001-01-30 Banavara L. Mylari Substituted pyrimidines for control of diabetic complications
ATE176476T1 (de) * 1992-12-02 1999-02-15 Hoechst Ag Guanidinalkyl-1, 1-bisphosphonsäurederivate, verfahren zu ihrer herstellung und ihre verwendung
TW260664B (de) * 1993-02-15 1995-10-21 Otsuka Pharma Factory Inc
JP3526575B2 (ja) * 1993-03-08 2004-05-17 エーザイ株式会社 ホスホン酸誘導体
JPH06298779A (ja) * 1993-04-15 1994-10-25 Hoechst Japan Ltd ヘテロ環イミノビスメチレンビスホスホン酸誘導体
PT970095E (pt) * 1997-03-07 2004-03-31 Metabasis Therapeutics Inc Novos inibidores benzimidazole de frutose-1,6-bisfosfatase
WO1998039342A1 (en) 1997-03-07 1998-09-11 Metabasis Therapeutics, Inc. Novel indole and azaindole inhibitors of fructose-1,6-bisphosphatase
CA2317008C (en) * 1997-12-31 2009-01-20 The University Of Kansas Water soluble prodrugs of tertiary amine containing drugs and methods of making thereof

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EP0970095A1 (de) 2000-01-12
EP0970095B1 (de) 2003-10-29
US6399782B1 (en) 2002-06-04
AU6691498A (en) 1998-09-22
DE69819311T2 (de) 2004-07-29
PT970095E (pt) 2004-03-31
ZA981936B (en) 1999-09-06
JP2001515482A (ja) 2001-09-18
ES2210728T3 (es) 2004-07-01
US6110903A (en) 2000-08-29
WO1998039343A1 (en) 1998-09-11
DE69819311D1 (de) 2003-12-04
DK0970095T3 (da) 2004-03-08

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