GEP20053720B - Triamide-Substituted Indoles, Benzofuranes and Benzothiophenes as Inhibitors of Microsomal Triglyceride Transfer Protein (MTP) and/or Apolipoprotein B (Apo B) Secretion - Google Patents

Triamide-Substituted Indoles, Benzofuranes and Benzothiophenes as Inhibitors of Microsomal Triglyceride Transfer Protein (MTP) and/or Apolipoprotein B (Apo B) Secretion

Info

Publication number
GEP20053720B
GEP20053720B GE5350A GEAP2002005350A GEP20053720B GE P20053720 B GEP20053720 B GE P20053720B GE 5350 A GE5350 A GE 5350A GE AP2002005350 A GEAP2002005350 A GE AP2002005350A GE P20053720 B GEP20053720 B GE P20053720B
Authority
GE
Georgia
Prior art keywords
benzofuranes
benzothiophenes
triamide
mtp
apolipoprotein
Prior art date
Application number
GE5350A
Other languages
English (en)
Inventor
Peter Bertinato
Alan Elwood Blize
Brian Scott Bronk
Hengmiao Cheng
Hiep Huatan
Jin Li
Clive Philip Mason
Original Assignee
Pfizer Prod 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 Pfizer Prod Inc filed Critical Pfizer Prod Inc
Publication of GEP20053720B publication Critical patent/GEP20053720B/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/343Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/38Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • A61K31/405Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/655Azo (—N=N—), diazo (=N2), azoxy (>N—O—N< or N(=O)—N<), azido (—N3) or diazoamino (—N=N—N<) compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/30Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/82Benzo [b] furans; Hydrogenated benzo [b] furans with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
    • C07D307/84Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D307/85Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Child & Adolescent Psychology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Furan Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
GE5350A 2001-06-28 2002-05-24 Triamide-Substituted Indoles, Benzofuranes and Benzothiophenes as Inhibitors of Microsomal Triglyceride Transfer Protein (MTP) and/or Apolipoprotein B (Apo B) Secretion GEP20053720B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US30164401P 2001-06-28 2001-06-28

Publications (1)

Publication Number Publication Date
GEP20053720B true GEP20053720B (en) 2006-01-10

Family

ID=23164253

Family Applications (2)

Application Number Title Priority Date Filing Date
GEAP20027236A GEP20063720B (en) 2001-06-28 2002-05-24 Triamide-Substituted Indoles, Benzofuranes and Benzothiophenes as Inhibitors of Microsomal Triglyceride Transfer Protein (MTP) and/or Apolipoprotein B (Apo B) Secretion
GE5350A GEP20053720B (en) 2001-06-28 2002-05-24 Triamide-Substituted Indoles, Benzofuranes and Benzothiophenes as Inhibitors of Microsomal Triglyceride Transfer Protein (MTP) and/or Apolipoprotein B (Apo B) Secretion

Family Applications Before (1)

Application Number Title Priority Date Filing Date
GEAP20027236A GEP20063720B (en) 2001-06-28 2002-05-24 Triamide-Substituted Indoles, Benzofuranes and Benzothiophenes as Inhibitors of Microsomal Triglyceride Transfer Protein (MTP) and/or Apolipoprotein B (Apo B) Secretion

Country Status (47)

Country Link
US (5) US6720351B2 (US06720351-20040413-C00034.png)
EP (1) EP1404653B1 (US06720351-20040413-C00034.png)
JP (1) JP4139325B2 (US06720351-20040413-C00034.png)
KR (2) KR100575944B1 (US06720351-20040413-C00034.png)
CN (2) CN1880304B (US06720351-20040413-C00034.png)
AP (1) AP1649A (US06720351-20040413-C00034.png)
AR (1) AR036158A1 (US06720351-20040413-C00034.png)
AT (1) ATE405548T1 (US06720351-20040413-C00034.png)
AU (1) AU2002307839B2 (US06720351-20040413-C00034.png)
BG (1) BG108487A (US06720351-20040413-C00034.png)
BR (1) BR0210616A (US06720351-20040413-C00034.png)
CA (1) CA2451474C (US06720351-20040413-C00034.png)
CR (1) CR7151A (US06720351-20040413-C00034.png)
CY (1) CY1108407T1 (US06720351-20040413-C00034.png)
CZ (1) CZ20033558A3 (US06720351-20040413-C00034.png)
DE (1) DE60228447D1 (US06720351-20040413-C00034.png)
DK (1) DK1404653T3 (US06720351-20040413-C00034.png)
EA (1) EA007008B1 (US06720351-20040413-C00034.png)
EC (1) ECSP034925A (US06720351-20040413-C00034.png)
EE (1) EE05452B1 (US06720351-20040413-C00034.png)
ES (1) ES2307799T3 (US06720351-20040413-C00034.png)
GE (2) GEP20063720B (US06720351-20040413-C00034.png)
GT (1) GT200200136A (US06720351-20040413-C00034.png)
HK (2) HK1064369A1 (US06720351-20040413-C00034.png)
HR (1) HRP20031051B1 (US06720351-20040413-C00034.png)
HU (1) HU229551B1 (US06720351-20040413-C00034.png)
IL (1) IL158516A0 (US06720351-20040413-C00034.png)
IS (1) IS2603B (US06720351-20040413-C00034.png)
MA (1) MA27045A1 (US06720351-20040413-C00034.png)
MX (1) MXPA03011707A (US06720351-20040413-C00034.png)
MY (1) MY129328A (US06720351-20040413-C00034.png)
NO (1) NO326700B1 (US06720351-20040413-C00034.png)
NZ (1) NZ528752A (US06720351-20040413-C00034.png)
OA (1) OA12626A (US06720351-20040413-C00034.png)
PA (1) PA8549301A1 (US06720351-20040413-C00034.png)
PE (1) PE20030135A1 (US06720351-20040413-C00034.png)
PL (1) PL367680A1 (US06720351-20040413-C00034.png)
PT (1) PT1404653E (US06720351-20040413-C00034.png)
RS (1) RS50712B (US06720351-20040413-C00034.png)
SI (1) SI1404653T1 (US06720351-20040413-C00034.png)
SK (1) SK287806B6 (US06720351-20040413-C00034.png)
TN (1) TNSN03146A1 (US06720351-20040413-C00034.png)
TW (2) TW200628447A (US06720351-20040413-C00034.png)
UA (1) UA75660C2 (US06720351-20040413-C00034.png)
UY (1) UY27360A1 (US06720351-20040413-C00034.png)
WO (1) WO2003002533A1 (US06720351-20040413-C00034.png)
ZA (1) ZA200307818B (US06720351-20040413-C00034.png)

Families Citing this family (58)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE60144284D1 (de) 2000-11-01 2011-05-05 Millennium Pharm Inc Stickstoffhaltige heterozyklische verbindungen und verfahren zu deren herstellung
KR100575944B1 (ko) * 2001-06-28 2006-05-02 화이자 프로덕츠 인코포레이티드 미소체 트리글리세라이드 전달 단백질(mtp) 및/또는아포지방단백질 b(apo b)분비의 억제제로서의트리아미드-치환된 인돌, 벤조푸란 및 벤조티오펜
ATE536993T1 (de) * 2002-01-02 2011-12-15 Visen Medical Inc Aminfunktionalisierte superparamagnetisierte nanoteilchen für die synthese von biokonjugaten
JP2006519229A (ja) * 2003-02-13 2006-08-24 アルバート・アインシュタイン・カレッジ・オヴ・メディシン・オヴ・イェシヴァ・ユニヴァーシティ 視床下部内の長鎖脂肪アシルCoAレベルの変調による摂食量およびグルコース産生量の調節
JP2007500229A (ja) * 2003-05-20 2007-01-11 ジョンズ・ホプキンズ・ユニバーシティ 腫瘍の治療のためのカテコールブタンの投与のための方法と組成物
EP1636592B1 (en) 2003-06-19 2012-12-19 Merck Serono SA Use of prion conversion modulating agents
US20080293801A1 (en) * 2003-11-14 2008-11-27 Pfizer Inc. Solid Amorphous Dispersions of An Mtp Inhibitor For Treatment of Obesity
JP2007520543A (ja) 2004-02-04 2007-07-26 ファイザー・プロダクツ・インク 置換キノリン化合物
JP5697296B2 (ja) 2004-03-05 2015-04-08 ザ トラスティーズ オブ ザ ユニバーシティ オブ ペンシルバニア 高脂血症および高コレステロール血症に関連する障害または疾患を、副作用を最小限にしつつ処置するための方法
FR2873694B1 (fr) * 2004-07-27 2006-12-08 Merck Sante Soc Par Actions Si Nouveaux aza-indoles inhibiteurs de la mtp et apob
WO2006041922A2 (en) * 2004-10-08 2006-04-20 Dara Biosciences, Inc. Agents and methods for administration to the central nervous system
PA8660701A1 (es) 2005-02-04 2006-09-22 Pfizer Prod Inc Agonistas de pyy y sus usos
US20090012067A1 (en) * 2005-02-14 2009-01-08 Luciano Rossetti Modulation of Hypothalamic Atp-Sensitive Potassium Channels
WO2006129193A2 (en) * 2005-05-27 2006-12-07 Pfizer Products Inc. Combination of a cannabinoid-1- receptor-antagonist and a microsomal triglyceride transfer protein inhibitor for treating obesity or mainataining weight loss
US7417066B2 (en) 2005-06-08 2008-08-26 Schering Ag Inhibitors of soluble adenylate cyclase
DE102005027274A1 (de) * 2005-06-08 2006-12-14 Schering Ag Inhibitoren der löslichen Adenylatzyklase
CA2617654A1 (en) * 2005-08-04 2007-02-08 Pfizer Limited Piperidinoyl-pyrrolidine and piperidinoyl-piperidine compounds
EP1951224A2 (en) * 2005-10-18 2008-08-06 Aegerion Pharmaceuticals Methods for treating disorders associated with hyperlipidemia in a mammal
US7741317B2 (en) 2005-10-21 2010-06-22 Bristol-Myers Squibb Company LXR modulators
US20090111778A1 (en) * 2005-11-18 2009-04-30 Richard Apodaca 2-Keto-Oxazoles as Modulators of Fatty Acid Amide Hydrolase
US7888376B2 (en) 2005-11-23 2011-02-15 Bristol-Myers Squibb Company Heterocyclic CETP inhibitors
US9913917B2 (en) 2005-12-22 2018-03-13 Visen Medical, Inc. Biocompatible fluorescent metal oxide nanoparticles
US8383660B2 (en) 2006-03-10 2013-02-26 Pfizer Inc. Dibenzyl amine compounds and derivatives
US10022352B2 (en) 2006-04-07 2018-07-17 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
EP2007756B1 (en) * 2006-04-07 2015-08-26 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters
US7645789B2 (en) 2006-04-07 2010-01-12 Vertex Pharmaceuticals Incorporated Indole derivatives as CFTR modulators
US8563573B2 (en) 2007-11-02 2013-10-22 Vertex Pharmaceuticals Incorporated Azaindole derivatives as CFTR modulators
CA2669311C (en) 2006-11-13 2011-09-20 Pfizer Products Inc. Diaryl, dipyridinyl and aryl-pyridinyl derivatives and uses thereof
ES2382009T3 (es) 2006-12-01 2012-06-04 Bristol-Myers Squibb Company Derivados de N-((3-bencil)-2,2-(bis-fenil-)-propan-1-amina como inhibidores de CETP para el tratamiento de aterosclerosis y enfermedades cardiovasculares
US20080161279A1 (en) * 2006-12-21 2008-07-03 Wisler Gerald L Methods of Treating Obesity
ES2670852T3 (es) 2007-02-09 2018-06-01 Visen Medical, Inc. Colorantes con policiclo y uso de los mismos
WO2008100423A1 (en) * 2007-02-09 2008-08-21 Sirtris Pharmaceuticals, Inc. Gut microsomal triglyceride transport protein inhibitors
CN103450077B (zh) 2007-06-08 2016-07-06 满康德股份有限公司 IRE-1α抑制剂
WO2009014674A1 (en) * 2007-07-23 2009-01-29 Sirtris Pharmaceuticals, Inc. Heterocyclylamides as gut microsomal triglyceride transport protein inhibitors
WO2009090210A2 (en) * 2008-01-16 2009-07-23 Janssen Pharmaceutica Nv Combination of metformin and an mtp inhibitor
US20090197947A1 (en) * 2008-02-01 2009-08-06 The Research Foundation Of State University Of New York Medicaments and methods for lowering plasma lipid levels and screening drugs
US8642770B2 (en) * 2010-01-06 2014-02-04 Takeda Pharmaceutical Company Limited Indole derivative
US8802868B2 (en) 2010-03-25 2014-08-12 Vertex Pharmaceuticals Incorporated Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxo1-5-yl)-N-(1-(2,3-dihydroxypropyl-6-fluoro-2-(1-hydroxy-2-methylpropan2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide
MX342288B (es) 2010-04-22 2016-09-23 Vertex Pharma Proceso para producir compuestos de cicloalquilcarboxamido-indol.
WO2012099785A2 (en) * 2011-01-20 2012-07-26 The Regents Of The University Of Colorado, A Body Corporate Modulators of tlr3/dsrna complex and uses thereof
CN102108070B (zh) * 2011-01-26 2013-05-22 上海优贝德生物医药有限公司 5-氨基苯并呋喃-2-甲酸酯及其中间体的制备方法
US9012496B2 (en) 2012-07-16 2015-04-21 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions of (R)-1-(2,2-difluorobenzo[D][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide and administration thereof
EP2963013A4 (en) 2013-02-27 2016-09-14 Shionogi & Co INDOLE AND AZAINDOLE DERIVATIVES HAVING AMPK ACTIVATION ACTIVITY EACH
WO2015121877A2 (en) * 2014-02-17 2015-08-20 Hetero Research Foundation Polymorphs of lomitapide and its salts
CN103880797B (zh) * 2014-03-26 2015-12-02 沈阳大学 苯并呋喃类化合物及其医药用途
ES2957761T3 (es) 2014-04-15 2024-01-25 Vertex Pharma Composiciones farmacéuticas para el tratamiento de enfermedades mediadas por el regulador de la conductancia transmembrana de fibrosis quística
RU2020134082A (ru) 2014-10-06 2020-11-27 Вертекс Фармасьютикалз Инкорпорейтед Модуляторы регулятора трансмембранной проводимости при муковисцидозе
PL3436446T3 (pl) 2016-03-31 2023-09-11 Vertex Pharmaceuticals Incorporated Modulatory mukowiscydozowego przezbłonowego regulatora przewodnictwa
SI3519401T1 (sl) 2016-09-30 2022-01-31 Vertex Pharmaceuticals Incorporated Modulator regulatorja transmembranske prevodnosti pri cistični fibrozi, farmacevtski sestavki, postopki zdravljenja in proces za izdelavo modulatorja
DK3551622T3 (da) 2016-12-09 2020-11-23 Vertex Pharma Modulator af transmembrankonduktansregulator af cystisk fibrose, farmaceutiske sammensætninger, behandlingsfremgangsmåder og fremgangsmåde til fremstilling af modulatoren
EP3634402A1 (en) 2017-06-08 2020-04-15 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
AU2018304168B2 (en) 2017-07-17 2023-05-04 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
AR112467A1 (es) 2017-08-02 2019-10-30 Vertex Pharma Procesos para preparar compuestos
AU2018351533B2 (en) 2017-10-19 2023-02-02 Vertex Pharmaceuticals Incorporated Crystalline forms and compositions of CFTR modulators
MX2020005753A (es) 2017-12-08 2020-08-20 Vertex Pharma Procesos para producir moduladores de regulador de conductancia transmembranal de fibrosis quistica.
TWI810243B (zh) 2018-02-05 2023-08-01 美商維泰克斯製藥公司 用於治療囊腫纖化症之醫藥組合物
EP3774825A1 (en) 2018-04-13 2021-02-17 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator
CN112608271A (zh) * 2020-11-26 2021-04-06 安润医药科技(苏州)有限公司 酰胺衍生物及其在制备ep4受体拮抗剂中的应用

Family Cites Families (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4022900A (en) 1970-09-09 1977-05-10 Marion Laboratories, Inc. Compositions containing 1,2,3,4-tetrahydroisoquinolines used as hypotensive agents
US4397855A (en) 1981-06-26 1983-08-09 Warner-Lambert Company 4-(Substituted)-α, α-dimethyl-1-piperazine pentanoic acids and derivatives as anti-arteriosclerotic agents and method
US4647576A (en) * 1984-09-24 1987-03-03 Warner-Lambert Company Trans-6-[2-(substitutedpyrrol-1-yl)alkyl]-pyran-2-one inhibitors of cholesterol synthesis
US5416009A (en) 1991-01-23 1995-05-16 The United States Of America Nucleotide molecule encoding a specific Onchocerca volvulus antigen for the immunodiagnosis of onchocerciasis
US5595872A (en) 1992-03-06 1997-01-21 Bristol-Myers Squibb Company Nucleic acids encoding microsomal trigyceride transfer protein
HU218419B (hu) 1992-03-06 2000-08-28 E.R. Squibb And Sons, Inc. Mikroszomális triglicerid transzfer protein (MTP) nagy molekulatömegű alegységének rekombináns úton történő előállítására és a protein és inhibitorainak kimutatására szolgáló eljárások
GB9225141D0 (en) 1992-12-01 1993-01-20 Smithkline Beecham Corp Chemical compounds
US5739135A (en) 1993-09-03 1998-04-14 Bristol-Myers Squibb Company Inhibitors of microsomal triglyceride transfer protein and method
FR2723739B1 (fr) * 1994-08-19 1997-02-14 Sanofi Sa Derives de glycinamide, procedes pour leur preparation et medicaments les contenant.
ES2191706T3 (es) 1995-06-07 2003-09-16 Pfizer Derivados de tetrahidro-isoquinolinil-6-il amida del acido bifenil-2-carboxilico, su preparacion y su uso como inhibidores de la proteina de transferencia de trigliceridos microsomal y/o secrecion de apolipoproteina b (apo b).
WO1996040640A1 (en) * 1995-06-07 1996-12-19 Pfizer Inc. BIPHENYL-2-CARBOXYLIC ACID-TETRAHYDRO-ISOQUINOLIN-6-YL AMIDE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS INHIBITORS OF MICROSOMAL TRIGLYCERIDE TRANSFER PROTEIN AND/OR APOLIPOPROTEIN B (Apo B) SECRETION
US5919795A (en) 1995-06-07 1999-07-06 Pfizer Inc. Biphenyl-2-carboxylic acid-tetrahydro-isoquinolin-6-yl amide derivatives, their preparation and their use as inhibitors of microsomal triglyceride transfer protein and/or apolipoprotein B (Apo B) secretion
EP0879120A1 (de) 1996-02-02 1998-11-25 Merritt, Mark W. Vorrichtung zum bearbeiten eines stranges aus plastischem material
US5827875A (en) 1996-05-10 1998-10-27 Bristol-Myers Squibb Company Inhibitors of microsomal triglyceride transfer protein and method
AU716151B2 (en) 1996-11-27 2000-02-17 Pfizer Inc. Apo B-secretion/MTP inhibitory amides
AU5513298A (en) 1996-12-20 1998-07-17 Bristol-Myers Squibb Company Heterocyclic inhibitors of microsomal triglyceride transfer protein and method
US6066653A (en) 1997-01-17 2000-05-23 Bristol-Myers Squibb Co. Method of treating acid lipase deficiency diseases with an MTP inhibitor and cholesterol lowering drugs
US5968950A (en) 1997-06-23 1999-10-19 Pfizer Inc Apo B-secretion/MTP inhibitor hydrochloride salt
TW460478B (en) * 1997-08-15 2001-10-21 Chugai Pharmaceutical Co Ltd Phenethylamine derivatives
JP2959765B2 (ja) 1997-12-12 1999-10-06 日本たばこ産業株式会社 3−ピペリジル−4−オキソキナゾリン誘導体及びそれを含有してなる医薬組成物
ES2241194T3 (es) 1997-12-24 2005-10-16 Aventis Pharma Deutschland Gmbh Derivados de indol en calidad de inhibidores de factor xa.
KR20010025074A (ko) 1998-05-22 2001-03-26 니뽄 신야쿠 가부시키가이샤 Mtp 활성 저하 조성물
AU4543899A (en) 1998-06-08 1999-12-30 Advanced Medicine, Inc. Multibinding inhibitors of microsomal triglyceride transferase protein
CO5090829A1 (es) * 1998-07-21 2001-10-30 Novartis Ag Compuestos organicos de la formula i, utiles como inhibido res de la proteina de transferencia de triglicerido microso mal y de la secrecion de la apolipoproteina b.
US6197798B1 (en) 1998-07-21 2001-03-06 Novartis Ag Amino-benzocycloalkane derivatives
WO2000076971A2 (en) * 1999-06-14 2000-12-21 Eli Lilly And Company Serine protease inhibitors
DE19933926A1 (de) 1999-07-20 2001-01-25 Boehringer Ingelheim Pharma Biphenylderivate, ihre Herstellung und ihre Verwendung als Arzneimittel
DE19945594A1 (de) 1999-09-23 2001-03-29 Boehringer Ingelheim Pharma Substituierte Piperazinderivate, ihre Herstellung und ihre Verwendung als Arzneimittel
CA2325358C (en) * 1999-11-10 2005-08-02 Pfizer Products Inc. 7-¬(4'-trifluoromethyl-biphenyl-2-carbonyl)amino|-quinoline-3-carboxylic acid amides, and methods of inhibiting the secretion of apolipoprotein b
DE19963234A1 (de) 1999-12-27 2002-01-24 Boehringer Ingelheim Pharma Substituierte Piperazinderivate, ihre Herstellung und ihre Verwendung als Arzneimittel
DE19963235A1 (de) 1999-12-27 2001-07-05 Boehringer Ingelheim Pharma Substituierte Piperazinderivate, ihre Herstellung und ihre Verwendung als Arzneimittel
ES2240420T3 (es) 2000-01-18 2005-10-16 Novartis Ag Carboxamidas utiles como inhibidores de la proteina de transferencia de trigliceridos microsomicos y de la secrecion de apolipoproteina b.
WO2001077077A1 (en) 2000-04-10 2001-10-18 Novartis Ag Substituted (hetero)aryl carboxamide derivatives as microsomal triglyceride transfer protein (mtp) and apolipoprotein b (apo b) secretion
GB0013378D0 (en) 2000-06-01 2000-07-26 Glaxo Group Ltd Use of therapeutic benzamide derivatives
GB0013346D0 (en) 2000-06-01 2000-07-26 Glaxo Group Ltd Therapeutic benzamide derivatives
GB0013383D0 (en) 2000-06-01 2000-07-26 Glaxo Group Ltd Therapeutic benzamide derivatives
US20020032238A1 (en) 2000-07-08 2002-03-14 Henning Priepke Biphenylcarboxylic acid amides, the preparation thereof and the use thereof as medicaments
DE10033337A1 (de) 2000-07-08 2002-01-17 Boehringer Ingelheim Pharma Biphenylcarbonsäureamide, ihre Herstellung und ihre Verwendung als Arzneimittel
FR2816940A1 (fr) 2000-11-23 2002-05-24 Lipha Derives de 4-(biphenylcarbonylamino)-piperidine, compositions les contenant et leur utilisation
GB0109287D0 (en) 2001-04-12 2001-05-30 Glaxo Group Ltd Therapeutic benzamide derivatives
KR100575944B1 (ko) * 2001-06-28 2006-05-02 화이자 프로덕츠 인코포레이티드 미소체 트리글리세라이드 전달 단백질(mtp) 및/또는아포지방단백질 b(apo b)분비의 억제제로서의트리아미드-치환된 인돌, 벤조푸란 및 벤조티오펜
SG165154A1 (en) 2002-02-28 2010-10-28 Japan Tobacco Inc Ester compound and medical use thereof

Also Published As

Publication number Publication date
HK1096665A1 (en) 2007-06-08
UA75660C2 (en) 2006-05-15
IL158516A0 (en) 2004-05-12
US7482368B2 (en) 2009-01-27
TW200628447A (en) 2006-08-16
KR100575944B1 (ko) 2006-05-02
DK1404653T3 (da) 2008-10-06
PL367680A1 (en) 2005-03-07
SI1404653T1 (sl) 2008-12-31
HUP0400348A2 (hu) 2004-12-28
NO20035607D0 (no) 2003-12-16
RS100403A (en) 2007-02-05
US6720351B2 (en) 2004-04-13
CN1522246A (zh) 2004-08-18
SK287806B6 (sk) 2011-10-04
HRP20031051B1 (en) 2012-01-31
BR0210616A (pt) 2004-09-28
MY129328A (en) 2007-03-30
PE20030135A1 (es) 2003-03-03
AP2002002567A0 (en) 2002-06-30
CA2451474A1 (en) 2003-01-09
DE60228447D1 (de) 2008-10-02
HU229551B1 (hu) 2014-01-28
ECSP034925A (es) 2004-02-26
UY27360A1 (es) 2003-01-31
US20050288335A1 (en) 2005-12-29
EA007008B1 (ru) 2006-06-30
IS2603B (is) 2010-04-15
US20030187053A1 (en) 2003-10-02
SK16102003A3 (sk) 2004-08-03
KR20040013006A (ko) 2004-02-11
TWI313264B (en) 2009-08-11
EE05452B1 (et) 2011-08-15
ZA200307818B (en) 2004-10-07
IS6988A (is) 2003-10-09
PA8549301A1 (es) 2003-02-14
RS50712B (sr) 2010-06-30
US7348355B2 (en) 2008-03-25
MXPA03011707A (es) 2004-03-19
HK1064369A1 (en) 2005-01-28
WO2003002533A1 (en) 2003-01-09
EA200301310A1 (ru) 2004-06-24
NZ528752A (en) 2006-06-30
AR036158A1 (es) 2004-08-18
HUP0400348A3 (en) 2011-07-28
CA2451474C (en) 2009-06-16
CR7151A (es) 2004-02-23
KR100575919B1 (ko) 2006-05-02
EP1404653A1 (en) 2004-04-07
PT1404653E (pt) 2008-09-23
CN1880304A (zh) 2006-12-20
CZ20033558A3 (cs) 2004-04-14
US20060194772A1 (en) 2006-08-31
US6979692B2 (en) 2005-12-27
GT200200136A (es) 2003-05-15
OA12626A (en) 2006-06-13
ATE405548T1 (de) 2008-09-15
NO326700B1 (no) 2009-02-02
CN1522246B (zh) 2010-04-21
JP4139325B2 (ja) 2008-08-27
GEP20063720B (en) 2006-01-10
CN1880304B (zh) 2010-11-24
AU2002307839B2 (en) 2006-03-16
KR20060006107A (ko) 2006-01-18
EE200400040A (et) 2004-06-15
CY1108407T1 (el) 2014-02-12
ES2307799T3 (es) 2008-12-01
US6949572B2 (en) 2005-09-27
AP1649A (en) 2006-08-07
MA27045A1 (fr) 2004-12-20
TNSN03146A1 (fr) 2005-12-23
HRP20031051A2 (en) 2005-08-31
BG108487A (bg) 2005-04-30
US20040087625A1 (en) 2004-05-06
US20050080108A1 (en) 2005-04-14
JP2004537541A (ja) 2004-12-16
EP1404653B1 (en) 2008-08-20

Similar Documents

Publication Publication Date Title
GEP20053720B (en) Triamide-Substituted Indoles, Benzofuranes and Benzothiophenes as Inhibitors of Microsomal Triglyceride Transfer Protein (MTP) and/or Apolipoprotein B (Apo B) Secretion
GEP20053600B (en) 3-(4-Amidopyrrol-2-Ylmethlidene)-2- Indolinone Derivatives as Protein Kinase Inhibitors
NO20093464L (no) Nye medikamentblandinger basert pa anti-cholinergisk effektive forbindelser og beta-mimetika
DE60226729D1 (de) Hydroxyalkylaminderivate als beta-secretase-inhibitoren und deren verwendung zur behandlung der alzheimerschen krankheit oder ähnlicher krankheiten
EP1562897A4 (en) PHENYL ACARBOXAMIDE AS A BETA SEKRETASE INHIBITOR FOR THE TREATMENT OF ALZHEIMER
MXPA02012272A (es) Compuestos heterociclicos que son inhibidores de la enzima dipeptidilpeptidasa-iv.
ATE269846T1 (de) N-substituierte aminotetraline als neuropeptid y y5 rezeptor-liganden und ihre anwendung zur behandlung von fettleibigkeit und anderen erkrankungen
ATE399553T1 (de) Pharmazeutische zusammensetzungen mit dextromethorphan und chinidin zur behandlung von neurologischen erkrankungen
DE60126980D1 (de) Therapeutische agentien und methoden ihrer verwendung zur behandlung von amyloidogenen erkrankungen
HK1080459A1 (en) Novel pyrimidineamide derivatives and the use thereof
ATE457027T1 (de) Substituierte 1,4,8-triazaspiroä4.5 decan-2-on- verbindungen zur behandlung von fettsucht
DE69309492D1 (de) Antipyretische und analgetische zusammensetzungen, die optisch reines r-ketorolac enthalten
DE60221283D1 (de) Verwendung von oxindolderivaten zur behandlung von mit demenz in zusammenhang stehenden krankheiten, alzheimer-krankheit und mit glycogensynthasekinase-3 assoziierten leiden
DE602004002394D1 (de) (3-ä3-&#39;(2,4-BIS-TRIFLUORMETHYL-BENZYL)-(5-ETHYL-PYRIMIDIN-2-YL)-AMINOÜ-PROPOXYü-PHENYL)-ESSIGSÄURE UND VERWANDTE VERBINDUNGEN ALS MODULATOREN VON PPARS UND VERFAHREN ZUR BEHANDLUNG VON STOFFWECHSELSTÖRUNGEN
DE60008753D1 (de) Verwendung von naaladase inhibitoren zur behandlung von angstzuständen und gedächtnisstörungen
DE69328838D1 (de) Antipyretische und analgetische verfahren und zusammensetzungen, die optisch reines r-etodolac enthalten
NO20025015L (no) Et pyridin-1-oksidderivat, og fremgangsmåte for dets overföring til farmasöytisk effektive forbindelser
ATE369348T1 (de) Zyklisierte benzamid-neurokinin-antagonisten zur verwendung in therapie
ATE287886T1 (de) Verwendung von 5-thio, sulfinyl- und sulfonylpyrazolo 3,4-b) pyridinen als cyclin- abhängige kinase-hemmer
MA26732A1 (fr) Composition pharmaceutique nouvelle comprenant un inhibiteur de nos, et procede pour sa preparation
PL350568A1 (en) N-(2-phenyl-4-aminobutyl)-1-naphtamides as antagonists of neurokinin 1 receptors
NO982863L (no) Nye forbindelser med analgetisk effekt
GB0019008D0 (en) Therapeutic compounds
DE60306503D1 (de) Statin-therapie zur verbesserung der aufrechterhaltung der kognitiven funktion
IL153182A0 (en) Heterocyclic compounds, which are inhibitors of the enzyme dpp-iv