WO2003002533A1 - 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 Download PDF

Info

Publication number
WO2003002533A1
WO2003002533A1 PCT/IB2002/001876 IB0201876W WO03002533A1 WO 2003002533 A1 WO2003002533 A1 WO 2003002533A1 IB 0201876 W IB0201876 W IB 0201876W WO 03002533 A1 WO03002533 A1 WO 03002533A1
Authority
WO
WIPO (PCT)
Prior art keywords
alkyl
independently
methyl
phenyl
compound
Prior art date
Application number
PCT/IB2002/001876
Other languages
English (en)
French (fr)
Inventor
Peter Bertinato
Alan Elwood Blize
Brian Scott Bronk
Hengmiao Cheng
Hiep Huatan
Jin Li
Clive Philip Mason
Original Assignee
Pfizer Products 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
Priority to JP2003508914A priority Critical patent/JP4139325B2/ja
Priority to MXPA03011707A priority patent/MXPA03011707A/es
Priority to EEP200400040A priority patent/EE05452B1/xx
Priority to IL15851602A priority patent/IL158516A0/xx
Priority to NZ528752A priority patent/NZ528752A/en
Priority to DE60228447T priority patent/DE60228447D1/de
Priority to DK02780923T priority patent/DK1404653T3/da
Priority to YUP-1004/03A priority patent/RS50712B/sr
Priority to KR1020037017167A priority patent/KR100575919B1/ko
Priority to CA002451474A priority patent/CA2451474C/en
Priority to HU0400348A priority patent/HU229551B1/hu
Priority to BR0210616-7A priority patent/BR0210616A/pt
Application filed by Pfizer Products Inc. filed Critical Pfizer Products Inc.
Priority to EP02780923A priority patent/EP1404653B1/en
Priority to EA200301310A priority patent/EA007008B1/ru
Priority to PL02367680A priority patent/PL367680A1/xx
Priority to CN028130219A priority patent/CN1522246B/zh
Priority to SI200230732T priority patent/SI1404653T1/sl
Priority to AU2002307839A priority patent/AU2002307839B2/en
Priority to SK1610-2003A priority patent/SK287806B6/sk
Priority to UA20031212657A priority patent/UA75660C2/uk
Publication of WO2003002533A1 publication Critical patent/WO2003002533A1/en
Priority to IS6988A priority patent/IS2603B/is
Priority to NO20035607A priority patent/NO326700B1/no
Priority to HR20031051A priority patent/HRP20031051B1/xx
Priority to HK04106993.0A priority patent/HK1064369A1/xx

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)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Child & Adolescent Psychology (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)
PCT/IB2002/001876 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 WO2003002533A1 (en)

Priority Applications (24)

Application Number Priority Date Filing Date Title
EP02780923A EP1404653B1 (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
MXPA03011707A MXPA03011707A (es) 2001-06-28 2002-05-24 Compuestos heterobiciclicos sustituidos con triamida.
EA200301310A EA007008B1 (ru) 2001-06-28 2002-05-24 Триамидзамещённые индолы, бензофураны и бензотиофены в качестве ингибиторов микросомального белка, переносящего триглицериды, (мтр) и/или ингибиторов секреции аполипопротеина в (аро в)
NZ528752A NZ528752A (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
DE60228447T DE60228447D1 (de) 2001-06-28 2002-05-24 Triamidsubstituierte indole, benzofurane und benzothiophene als inhibitoren des mikrosomalen triglyceridtransferproteins (mtp) und/oder der sekretion von apolipoprotein b (apo b)
DK02780923T DK1404653T3 (da) 2001-06-28 2002-05-24 Triamid-substituerede indoler, benzofuraner og benzothiophener som inhibitorer for mikrosomal triglycerid overförselsprotein (MTP) og/eller apolipoprotein B (ApoB) sekretion
YUP-1004/03A RS50712B (sr) 2001-06-28 2002-05-24 Triamid-supstituisani indoli, benzofurani i benzotiofeni kao inhibitori mikrozomalnog triglicerid transfer proteina (mtp) i/ili sekrecije apolipoproteina b (apo b)
KR1020037017167A KR100575919B1 (ko) 2001-06-28 2002-05-24 미소체 트리글리세라이드 전달 단백질(mtp) 및/또는아포지방단백질 b(apo b)분비의 억제제로서의트리아미드-치환된 인돌, 벤조푸란 및 벤조티오펜
CA002451474A CA2451474C (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
HU0400348A HU229551B1 (hu) 2001-06-28 2002-05-24 Mikroszóma triglicerid transzfer protein (MTP) és/vagy apolipoprotein B(APO B) kiválasztás inhibitorokként alkalmazható triamiddal helyettesített indol-, benzofurán- és benzotiofén-származékok
BR0210616-7A BR0210616A (pt) 2001-06-28 2002-05-24 Indóis, benzofuranos e benzotiofenos substituìdos com triamida, composição farmacêutica, uso dos referidos compostos, bem como processo para preparação dos mesmos
JP2003508914A JP4139325B2 (ja) 2001-06-28 2002-05-24 ミクロソーム・トリグリセリド・トランスファータンパク質(mtp)及び/又はアポリポタンパク質b(apob)分泌の阻害剤としてのトリアミド置換インドール、ベンゾフラン及びベンゾチオフェン
EEP200400040A EE05452B1 (et) 2001-06-28 2002-05-24 Triamiidasendatud indoolid, bensofuraanid ja bensotiofeenid kui mikrosomaalse trigltseriidide transportvalgu (MTP) ja/v?i apolipoproteiin B (apoB) sekretsiooni inhibiitorid
IL15851602A IL158516A0 (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
PL02367680A PL367680A1 (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
CN028130219A CN1522246B (zh) 2001-06-28 2002-05-24 三酰胺取代的吲哚、苯并呋喃及苯并噻吩
SI200230732T SI1404653T1 (sl) 2001-06-28 2002-05-24 S triamidom substituirani indoli, benzofurani in benzotiofeni kot zaviralci mikrosomske prenašalnebeljakovine za trigliceride (MTP) in/ali izločanja apolipoproteina B (APO B)
AU2002307839A AU2002307839B2 (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
SK1610-2003A SK287806B6 (sk) 2001-06-28 2002-05-24 Triamid-substituované indoly, benzofurány a benzotiofény ako inhibítory mikrozómového proteínu prenášajúceho triglyceridu (MTP) a/alebo sekrécie apolipoproteínu B (Apo B)
UA20031212657A UA75660C2 (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
IS6988A IS2603B (is) 2001-06-28 2003-10-09 Tríamíð-setin indól, bensófúrön og bensóþíófen sem hindrar á netbólu þríglýseríð flutningsprótín (MTP) og/eða apófituprótein B (APO B) seyti
NO20035607A NO326700B1 (no) 2001-06-28 2003-12-16 Triamid-substituerte indoler, benzofuraner og benzotiofener, anvendelse og fremstilling derav, samt farmasøytisk preparat
HR20031051A HRP20031051B1 (en) 2001-06-28 2003-12-17 Triamide-substituted indoles, benzofuranes and benzothiophenes as inhibitors of microsomal triglyceride transfer protein (mtp) and/or apolipoprotein b (apo b) secretion
HK04106993.0A HK1064369A1 (en) 2001-06-28 2004-09-14 Triamide-substituted indoles, benzofuranes and benzothiophenes

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US30164401P 2001-06-28 2001-06-28
US60/301,644 2001-06-28

Publications (1)

Publication Number Publication Date
WO2003002533A1 true WO2003002533A1 (en) 2003-01-09

Family

ID=23164253

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB2002/001876 WO2003002533A1 (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-C00046.png)
EP (1) EP1404653B1 (US06720351-20040413-C00046.png)
JP (1) JP4139325B2 (US06720351-20040413-C00046.png)
KR (2) KR100575919B1 (US06720351-20040413-C00046.png)
CN (2) CN1880304B (US06720351-20040413-C00046.png)
AP (1) AP1649A (US06720351-20040413-C00046.png)
AR (1) AR036158A1 (US06720351-20040413-C00046.png)
AT (1) ATE405548T1 (US06720351-20040413-C00046.png)
AU (1) AU2002307839B2 (US06720351-20040413-C00046.png)
BG (1) BG108487A (US06720351-20040413-C00046.png)
BR (1) BR0210616A (US06720351-20040413-C00046.png)
CA (1) CA2451474C (US06720351-20040413-C00046.png)
CR (1) CR7151A (US06720351-20040413-C00046.png)
CY (1) CY1108407T1 (US06720351-20040413-C00046.png)
CZ (1) CZ20033558A3 (US06720351-20040413-C00046.png)
DE (1) DE60228447D1 (US06720351-20040413-C00046.png)
DK (1) DK1404653T3 (US06720351-20040413-C00046.png)
EA (1) EA007008B1 (US06720351-20040413-C00046.png)
EC (1) ECSP034925A (US06720351-20040413-C00046.png)
EE (1) EE05452B1 (US06720351-20040413-C00046.png)
ES (1) ES2307799T3 (US06720351-20040413-C00046.png)
GE (2) GEP20053720B (US06720351-20040413-C00046.png)
GT (1) GT200200136A (US06720351-20040413-C00046.png)
HK (2) HK1096665A1 (US06720351-20040413-C00046.png)
HR (1) HRP20031051B1 (US06720351-20040413-C00046.png)
HU (1) HU229551B1 (US06720351-20040413-C00046.png)
IL (1) IL158516A0 (US06720351-20040413-C00046.png)
IS (1) IS2603B (US06720351-20040413-C00046.png)
MA (1) MA27045A1 (US06720351-20040413-C00046.png)
MX (1) MXPA03011707A (US06720351-20040413-C00046.png)
MY (1) MY129328A (US06720351-20040413-C00046.png)
NO (1) NO326700B1 (US06720351-20040413-C00046.png)
NZ (1) NZ528752A (US06720351-20040413-C00046.png)
OA (1) OA12626A (US06720351-20040413-C00046.png)
PA (1) PA8549301A1 (US06720351-20040413-C00046.png)
PE (1) PE20030135A1 (US06720351-20040413-C00046.png)
PL (1) PL367680A1 (US06720351-20040413-C00046.png)
PT (1) PT1404653E (US06720351-20040413-C00046.png)
RS (1) RS50712B (US06720351-20040413-C00046.png)
SI (1) SI1404653T1 (US06720351-20040413-C00046.png)
SK (1) SK287806B6 (US06720351-20040413-C00046.png)
TN (1) TNSN03146A1 (US06720351-20040413-C00046.png)
TW (2) TW200628447A (US06720351-20040413-C00046.png)
UA (1) UA75660C2 (US06720351-20040413-C00046.png)
UY (1) UY27360A1 (US06720351-20040413-C00046.png)
WO (1) WO2003002533A1 (US06720351-20040413-C00046.png)
ZA (1) ZA200307818B (US06720351-20040413-C00046.png)

Cited By (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004111652A1 (en) 2003-06-19 2004-12-23 Applied Research Systems Ars Holding N.V. Use of prion conversion modulating agents
WO2005046644A1 (en) * 2003-11-14 2005-05-26 Pfizer Products Inc. Solid amorphous dispersions of an mtp inhibitor for treatment of obesity
WO2005080373A1 (en) 2004-02-04 2005-09-01 Pfizer Products Inc. Substituted quinoline compounds
WO2006010423A2 (en) * 2004-07-27 2006-02-02 Merck Patent Gmbh Azaindole inhibitors of mtp and apob
DE102005027274A1 (de) * 2005-06-08 2006-12-14 Schering Ag Inhibitoren der löslichen Adenylatzyklase
WO2007117715A2 (en) 2006-04-07 2007-10-18 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters
WO2008100423A1 (en) * 2007-02-09 2008-08-21 Sirtris Pharmaceuticals, Inc. Gut microsomal triglyceride transport protein inhibitors
US7417066B2 (en) 2005-06-08 2008-08-26 Schering Ag Inhibitors of soluble adenylate cyclase
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
US7645789B2 (en) 2006-04-07 2010-01-12 Vertex Pharmaceuticals Incorporated Indole derivatives as CFTR modulators
CN102108070A (zh) * 2011-01-26 2011-06-29 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
WO2012099785A3 (en) * 2011-01-20 2012-09-27 The Regents Of The University Of Colorado, A Body Corporate Modulators of tlr3/dsrna complex and uses thereof
WO2014133008A1 (ja) 2013-02-27 2014-09-04 塩野義製薬株式会社 Ampk活性化作用を有するインドールおよびアザインドール誘導体
US9241942B2 (en) 2007-06-08 2016-01-26 Mannkind Corporation IRE-1α inhibitors
US9732080B2 (en) 2006-11-03 2017-08-15 Vertex Pharmaceuticals Incorporated Azaindole derivatives as CFTR modulators
US9782408B2 (en) 2014-10-06 2017-10-10 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
US10022352B2 (en) 2006-04-07 2018-07-17 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
US10058546B2 (en) 2012-07-16 2018-08-28 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions of (R)-1-(2,2-difluorobenzo[D][1,3]dioxo1-5-y1)-N-(1-(2,3-dihydroxypropy1)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-y1)-1H-indol-5-y1) cyclopropanecarbox-amide and administration thereof
US10071979B2 (en) 2010-04-22 2018-09-11 Vertex Pharmaceuticals Incorporated Process of producing cycloalkylcarboxamido-indole compounds
US10081621B2 (en) 2010-03-25 2018-09-25 Vertex Pharmaceuticals Incorporated Solid forms 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
US10206877B2 (en) 2014-04-15 2019-02-19 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions for the treatment of cystic fibrosis transmembrane conductance regulator mediated diseases
US10570115B2 (en) 2016-09-30 2020-02-25 Vertex Pharmaceuticals Incorporated Modulator of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator
US10654829B2 (en) 2017-10-19 2020-05-19 Vertex Pharmaceuticals Incorporated Crystalline forms and compositions of CFTR modulators
US10738030B2 (en) 2016-03-31 2020-08-11 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
US10793547B2 (en) 2016-12-09 2020-10-06 Vertex Pharmaceuticals Incorporated Modulator of the cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator
US11179367B2 (en) 2018-02-05 2021-11-23 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions for treating cystic fibrosis
US11253509B2 (en) 2017-06-08 2022-02-22 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
US11414439B2 (en) 2018-04-13 2022-08-16 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator
US11434201B2 (en) 2017-08-02 2022-09-06 Vertex Pharmaceuticals Incorporated Processes for preparing pyrrolidine compounds
US11465985B2 (en) 2017-12-08 2022-10-11 Vertex Pharmaceuticals Incorporated Processes for making modulators of cystic fibrosis transmembrane conductance regulator
US11517564B2 (en) 2017-07-17 2022-12-06 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002036587A2 (en) * 2000-11-01 2002-05-10 Cor Therapeutics, Inc. Process for the production of 4-quinazolinylpiperazin-1-carboxylic acid phenylamides
AU2002307839B2 (en) * 2001-06-28 2006-03-16 Zoetis P Llc Triamide-substituted indoles, benzofuranes and benzothiophenes as inhibitors of microsomal triglyceride transfer protein (MTP) and/or apolipoprotein B (Apo B) secretion
WO2003057175A2 (en) * 2002-01-02 2003-07-17 Visen Medical, Inc. Amine functionalized superparamagnetic nanoparticles for the synthesis of bioconjugates and uses therefor
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
JP2006528700A (ja) * 2003-05-20 2006-12-21 エリモス・ファーマスーティカルズ・エルエルシー 肥満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
WO2005087234A1 (en) 2004-03-05 2005-09-22 The Trustees Of The University Of Pennsylvania Methods for treating disorders or diseases associated with hyperlipidemia and hypercholesterolemia while minimizing side-effects
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
WO2006088798A2 (en) * 2005-02-14 2006-08-24 Albert Einstein College Of Medicine Of Yeshiva University Modulation of hypothalamic atp-sensitive potassium channels
CA2609783A1 (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
US20080269233A1 (en) * 2005-08-04 2008-10-30 Mark David Andrews Piperidinoyl-Pyrrolidine and Piperidinoyl-Piperidine Compounds
WO2007047880A2 (en) * 2005-10-18 2007-04-26 Aegerion Pharmaceuticals Compositions for lowering serum cholesterol and/or triglycerides
US7741317B2 (en) 2005-10-21 2010-06-22 Bristol-Myers Squibb Company LXR modulators
EP1954137A4 (en) * 2005-11-18 2008-12-17 Janssen Pharmaceutica Nv 2-KETO-OXAZOLE AS MODULATORS OF FATTY ACID AMIDHYDROLASE
US7888376B2 (en) 2005-11-23 2011-02-15 Bristol-Myers Squibb Company Heterocyclic CETP inhibitors
WO2007136413A2 (en) 2005-12-22 2007-11-29 Visen Medical, Inc. Biocompatible fluorescent metal oxide nanoparticles
US8383660B2 (en) 2006-03-10 2013-02-26 Pfizer Inc. Dibenzyl amine compounds and derivatives
WO2008059335A1 (en) 2006-11-13 2008-05-22 Pfizer Products Inc. Diaryl, dipyridinyl and aryl-pyridinyl derivatives and uses thereof
US8404896B2 (en) 2006-12-01 2013-03-26 Bristol-Myers Squibb Company N-((3-benzyl)-2,2-(bis-phenyl)-propan-1-amine derivatives as CETP inhibitors for the treatment of atherosclerosis and cardiovascular diseases
EP2120927A1 (en) * 2006-12-21 2009-11-25 Aegerion Pharmaceuticals, Inc. Methods for treating obesity with a combination comprising a mtp inhibitor and a cholesterol absorption inhibitor
DK2118206T3 (en) 2007-02-09 2018-06-18 Visen Medical Inc POLYCYCLOF COLORS AND APPLICATION THEREOF
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
US9624172B2 (en) 2014-02-17 2017-04-18 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
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

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US5731340A (en) * 1994-08-19 1998-03-24 Sanofi Glycinamide derivatives, processes for their preparation and medicines containing them
WO2000005201A1 (en) * 1998-07-21 2000-02-03 Novartis Ag N-benzocycloalkyl-amide derivatives and their use as medicaments
EP1006122A1 (en) * 1997-08-15 2000-06-07 Chugai Seiyaku Kabushiki Kaisha Phenethylamine derivatives
WO2000076971A2 (en) * 1999-06-14 2000-12-21 Eli Lilly And Company Serine protease inhibitors
EP1099701A1 (en) * 1999-11-10 2001-05-16 Pfizer Products Inc. 7-[(4'-Trifluoromethyl-biphenyl-2-carbonyl)amino]-quinoline-3-carboxylic acid amides, and methods of inhibiting the secretion of apolipoprotein B

Family Cites Families (36)

* 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
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
US5595872A (en) 1992-03-06 1997-01-21 Bristol-Myers Squibb Company Nucleic acids encoding microsomal trigyceride transfer protein
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
MX9709914A (es) 1995-06-07 1998-03-31 Pfizer Derivados de acido bifenil-2-carboxilico-tetrahidro-isoquinolin-6-ilo, su preparacion y el uso de los mismos.
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).
AU1595897A (en) 1996-02-02 1997-08-22 Mark W. Merritt Device for processing a strand of plastic material
US5827875A (en) 1996-05-10 1998-10-27 Bristol-Myers Squibb Company Inhibitors of microsomal triglyceride transfer protein and method
YU23499A (sh) 1996-11-27 2001-07-10 Pfizer Inc. Inhibitorski amidi apo-b-sekrecije/mtp-a
WO1998027979A1 (en) 1996-12-20 1998-07-02 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
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
IL136954A0 (en) 1997-12-24 2001-06-14 Aventis Pharma Gmbh Indole derivatives as inhibitors of 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
US6197798B1 (en) 1998-07-21 2001-03-06 Novartis Ag Amino-benzocycloalkane derivatives
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
DE19963235A1 (de) 1999-12-27 2001-07-05 Boehringer Ingelheim Pharma Substituierte Piperazinderivate, ihre Herstellung und ihre Verwendung als Arzneimittel
DE19963234A1 (de) 1999-12-27 2002-01-24 Boehringer Ingelheim Pharma Substituierte Piperazinderivate, ihre Herstellung und ihre Verwendung als Arzneimittel
WO2001053260A1 (en) 2000-01-18 2001-07-26 Novartis Ag Carboxamides useful as inhibitors of microsomal triglyceride transfer protein and of apolipoprotein b secretion
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
GB0013346D0 (en) 2000-06-01 2000-07-26 Glaxo Group Ltd Therapeutic benzamide derivatives
GB0013378D0 (en) 2000-06-01 2000-07-26 Glaxo Group Ltd Use of therapeutic benzamide derivatives
GB0013383D0 (en) 2000-06-01 2000-07-26 Glaxo Group Ltd Therapeutic benzamide derivatives
DE10033337A1 (de) 2000-07-08 2002-01-17 Boehringer Ingelheim Pharma Biphenylcarbonsäureamide, ihre Herstellung und ihre Verwendung als Arzneimittel
US20020032238A1 (en) 2000-07-08 2002-03-14 Henning Priepke Biphenylcarboxylic acid amides, the preparation thereof and the use thereof as medicaments
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
AU2002307839B2 (en) * 2001-06-28 2006-03-16 Zoetis P Llc Triamide-substituted indoles, benzofuranes and benzothiophenes as inhibitors of microsomal triglyceride transfer protein (MTP) and/or apolipoprotein B (Apo B) secretion
KR100717098B1 (ko) 2002-02-28 2007-05-10 니뽄 다바코 산교 가부시키가이샤 에스테르 화합물 및 그 의약 용도

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5731340A (en) * 1994-08-19 1998-03-24 Sanofi Glycinamide derivatives, processes for their preparation and medicines containing them
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
EP1006122A1 (en) * 1997-08-15 2000-06-07 Chugai Seiyaku Kabushiki Kaisha Phenethylamine derivatives
WO2000005201A1 (en) * 1998-07-21 2000-02-03 Novartis Ag N-benzocycloalkyl-amide derivatives and their use as medicaments
WO2000076971A2 (en) * 1999-06-14 2000-12-21 Eli Lilly And Company Serine protease inhibitors
EP1099701A1 (en) * 1999-11-10 2001-05-16 Pfizer Products Inc. 7-[(4'-Trifluoromethyl-biphenyl-2-carbonyl)amino]-quinoline-3-carboxylic acid amides, and methods of inhibiting the secretion of apolipoprotein B

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
ZHANG, J. ET AL: "Identification of inhibitors of heparin-growth factor interactions from combinatorial libraries of four-component condensation reactions", BIOORGANIC & MEDICINAL CHEMISTRY (2001), 9(4), 825-836, XP002205124 *

Cited By (70)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004111652A1 (en) 2003-06-19 2004-12-23 Applied Research Systems Ars Holding N.V. Use of prion conversion modulating agents
US7598046B2 (en) 2003-06-19 2009-10-06 Laboratories Serono Sa Use of prion conversion modulating agents
WO2005046644A1 (en) * 2003-11-14 2005-05-26 Pfizer Products Inc. Solid amorphous dispersions of an mtp inhibitor for treatment of obesity
WO2005080373A1 (en) 2004-02-04 2005-09-01 Pfizer Products Inc. Substituted quinoline compounds
US7468378B2 (en) 2004-02-04 2008-12-23 Pfizer Inc. Substituted quinoline compounds
US7393958B2 (en) 2004-02-04 2008-07-01 Pfizer, Inc. Triamide-substituted heterobicyclic compounds
US7368573B2 (en) 2004-02-04 2008-05-06 Pfizer Inc. Triamide-substituted heterobicyclic compounds
WO2006010423A2 (en) * 2004-07-27 2006-02-02 Merck Patent Gmbh Azaindole inhibitors of mtp and apob
US7838533B2 (en) 2004-07-27 2010-11-23 Merck Patent Gmbh Azaindole inhibitors of MTP and ApoB
WO2006010423A3 (en) * 2004-07-27 2006-03-02 Merck Patent Gmbh Azaindole inhibitors of mtp and apob
FR2873694A1 (fr) * 2004-07-27 2006-02-03 Merck Sante Soc Par Actions Si Nouveaux aza-indoles inhibiteurs de la mtp et apob
DE102005027274A1 (de) * 2005-06-08 2006-12-14 Schering Ag Inhibitoren der löslichen Adenylatzyklase
US7417066B2 (en) 2005-06-08 2008-08-26 Schering Ag Inhibitors of soluble adenylate cyclase
WO2007117715A3 (en) * 2006-04-07 2008-01-10 Vertex Pharma Modulators of atp-binding cassette transporters
US10022352B2 (en) 2006-04-07 2018-07-17 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
US10987348B2 (en) 2006-04-07 2021-04-27 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
US11639347B2 (en) 2006-04-07 2023-05-02 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
US10975061B2 (en) 2006-04-07 2021-04-13 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
US7776905B2 (en) 2006-04-07 2010-08-17 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
WO2007117715A2 (en) 2006-04-07 2007-10-18 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters
US10239867B2 (en) 2006-04-07 2019-03-26 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
EP3882245A1 (en) * 2006-04-07 2021-09-22 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters
US8415387B2 (en) 2006-04-07 2013-04-09 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
EP2674428A1 (en) * 2006-04-07 2013-12-18 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
EP3327016A1 (en) * 2006-04-07 2018-05-30 Vertex Pharmaceuticals Incorporated Preparation of modulators of atp-binding cassette transporters
US8912199B2 (en) 2006-04-07 2014-12-16 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
US8952049B2 (en) 2006-04-07 2015-02-10 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
US8952050B2 (en) 2006-04-07 2015-02-10 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
US9974781B2 (en) 2006-04-07 2018-05-22 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
EP3091011A1 (en) * 2006-04-07 2016-11-09 Vertex Pharmaceuticals Inc. Modulators of atp-binding cassette transporters
US20160332997A1 (en) * 2006-04-07 2016-11-17 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters
US9758510B2 (en) * 2006-04-07 2017-09-12 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
US9732080B2 (en) 2006-11-03 2017-08-15 Vertex Pharmaceuticals Incorporated Azaindole derivatives as CFTR modulators
WO2008100423A1 (en) * 2007-02-09 2008-08-21 Sirtris Pharmaceuticals, Inc. Gut microsomal triglyceride transport protein inhibitors
US9546149B2 (en) 2007-06-08 2017-01-17 Mannkind Corporation IRE-1α inhibitors
US9241942B2 (en) 2007-06-08 2016-01-26 Mannkind Corporation IRE-1α inhibitors
US9981901B2 (en) 2007-06-08 2018-05-29 Fosun Orinove Pharmatech, Inc. IRE-1α inhibitors
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
WO2009090210A3 (en) * 2008-01-16 2009-10-15 Janssen Pharmaceutica Nv Combination of metformin and an mtp inhibitor
US10906891B2 (en) 2010-03-25 2021-02-02 Vertex Pharmaceuticals Incoporated Solid forms 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
US10081621B2 (en) 2010-03-25 2018-09-25 Vertex Pharmaceuticals Incorporated Solid forms 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
US11578062B2 (en) 2010-03-25 2023-02-14 Vertex Pharmaceuticals Incorporated Solid forms 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
US10071979B2 (en) 2010-04-22 2018-09-11 Vertex Pharmaceuticals Incorporated Process of producing cycloalkylcarboxamido-indole compounds
WO2012099785A3 (en) * 2011-01-20 2012-09-27 The Regents Of The University Of Colorado, A Body Corporate Modulators of tlr3/dsrna complex and uses thereof
CN102108070A (zh) * 2011-01-26 2011-06-29 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
US10058546B2 (en) 2012-07-16 2018-08-28 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions of (R)-1-(2,2-difluorobenzo[D][1,3]dioxo1-5-y1)-N-(1-(2,3-dihydroxypropy1)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-y1)-1H-indol-5-y1) cyclopropanecarbox-amide and administration thereof
WO2014133008A1 (ja) 2013-02-27 2014-09-04 塩野義製薬株式会社 Ampk活性化作用を有するインドールおよびアザインドール誘導体
US9890119B2 (en) 2013-02-27 2018-02-13 Shionogi & Co., Ltd. Indole and azaindole derivative having AMPK-activating activity
US11951212B2 (en) 2014-04-15 2024-04-09 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions for the treatment of cystic fibrosis transmembrane conductance regulator mediated diseases
US10206877B2 (en) 2014-04-15 2019-02-19 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions for the treatment of cystic fibrosis transmembrane conductance regulator mediated diseases
US10980746B2 (en) 2014-04-15 2021-04-20 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions for the treatment of cystic fibrosis transmembrane conductance regulator mediated diseases
US9782408B2 (en) 2014-10-06 2017-10-10 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
US10258624B2 (en) 2014-10-06 2019-04-16 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
US10758534B2 (en) 2014-10-06 2020-09-01 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
US11426407B2 (en) 2014-10-06 2022-08-30 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
US10738030B2 (en) 2016-03-31 2020-08-11 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
US11186566B2 (en) 2016-09-30 2021-11-30 Vertex Pharmaceuticals Incorporated Modulator of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator
US10570115B2 (en) 2016-09-30 2020-02-25 Vertex Pharmaceuticals Incorporated Modulator of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator
US11453655B2 (en) 2016-12-09 2022-09-27 Vertex Pharmaceuticals Incorporated Modulator of the cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator
US10793547B2 (en) 2016-12-09 2020-10-06 Vertex Pharmaceuticals Incorporated Modulator of the cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator
US11253509B2 (en) 2017-06-08 2022-02-22 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
US11517564B2 (en) 2017-07-17 2022-12-06 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
US11434201B2 (en) 2017-08-02 2022-09-06 Vertex Pharmaceuticals Incorporated Processes for preparing pyrrolidine compounds
US11155533B2 (en) 2017-10-19 2021-10-26 Vertex Pharmaceuticals Incorporated Crystalline forms and compositions of CFTR modulators
US10654829B2 (en) 2017-10-19 2020-05-19 Vertex Pharmaceuticals Incorporated Crystalline forms and compositions of CFTR modulators
US11465985B2 (en) 2017-12-08 2022-10-11 Vertex Pharmaceuticals Incorporated Processes for making modulators of cystic fibrosis transmembrane conductance regulator
US11179367B2 (en) 2018-02-05 2021-11-23 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions for treating cystic fibrosis
US11414439B2 (en) 2018-04-13 2022-08-16 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator

Also Published As

Publication number Publication date
NO20035607D0 (no) 2003-12-16
OA12626A (en) 2006-06-13
JP2004537541A (ja) 2004-12-16
CN1880304A (zh) 2006-12-20
DE60228447D1 (de) 2008-10-02
AR036158A1 (es) 2004-08-18
KR100575919B1 (ko) 2006-05-02
CR7151A (es) 2004-02-23
SK287806B6 (sk) 2011-10-04
PA8549301A1 (es) 2003-02-14
CA2451474C (en) 2009-06-16
RS100403A (en) 2007-02-05
SK16102003A3 (sk) 2004-08-03
EP1404653A1 (en) 2004-04-07
EA200301310A1 (ru) 2004-06-24
US20050080108A1 (en) 2005-04-14
EP1404653B1 (en) 2008-08-20
CN1522246B (zh) 2010-04-21
TNSN03146A1 (fr) 2005-12-23
GEP20063720B (en) 2006-01-10
MY129328A (en) 2007-03-30
AP1649A (en) 2006-08-07
EE200400040A (et) 2004-06-15
ECSP034925A (es) 2004-02-26
TW200628447A (en) 2006-08-16
PL367680A1 (en) 2005-03-07
ES2307799T3 (es) 2008-12-01
AU2002307839B2 (en) 2006-03-16
RS50712B (sr) 2010-06-30
BR0210616A (pt) 2004-09-28
KR20040013006A (ko) 2004-02-11
US20030187053A1 (en) 2003-10-02
US6979692B2 (en) 2005-12-27
HU229551B1 (hu) 2014-01-28
TWI313264B (en) 2009-08-11
IL158516A0 (en) 2004-05-12
HRP20031051A2 (en) 2005-08-31
CZ20033558A3 (cs) 2004-04-14
HUP0400348A3 (en) 2011-07-28
PT1404653E (pt) 2008-09-23
PE20030135A1 (es) 2003-03-03
KR100575944B1 (ko) 2006-05-02
US20050288335A1 (en) 2005-12-29
CY1108407T1 (el) 2014-02-12
ZA200307818B (en) 2004-10-07
AP2002002567A0 (en) 2002-06-30
ATE405548T1 (de) 2008-09-15
US20060194772A1 (en) 2006-08-31
DK1404653T3 (da) 2008-10-06
SI1404653T1 (sl) 2008-12-31
NZ528752A (en) 2006-06-30
EA007008B1 (ru) 2006-06-30
IS2603B (is) 2010-04-15
UA75660C2 (en) 2006-05-15
MA27045A1 (fr) 2004-12-20
HK1064369A1 (en) 2005-01-28
US7348355B2 (en) 2008-03-25
GT200200136A (es) 2003-05-15
EE05452B1 (et) 2011-08-15
BG108487A (bg) 2005-04-30
HUP0400348A2 (hu) 2004-12-28
HK1096665A1 (en) 2007-06-08
CN1522246A (zh) 2004-08-18
UY27360A1 (es) 2003-01-31
KR20060006107A (ko) 2006-01-18
CN1880304B (zh) 2010-11-24
IS6988A (is) 2003-10-09
NO326700B1 (no) 2009-02-02
JP4139325B2 (ja) 2008-08-27
GEP20053720B (en) 2006-01-10
CA2451474A1 (en) 2003-01-09
US7482368B2 (en) 2009-01-27
US20040087625A1 (en) 2004-05-06
US6949572B2 (en) 2005-09-27
MXPA03011707A (es) 2004-03-19
US6720351B2 (en) 2004-04-13
HRP20031051B1 (en) 2012-01-31

Similar Documents

Publication Publication Date Title
EP1404653B1 (en) Triamide-substituted indoles, benzofuranes and benzothiophenes as inhibitors of microsomal triglyceride transfer protein (mtp) and/or apolipoprotein b (apo b) secretion
AU2002307839A1 (en) Triamide-substituted indoles, benzofuranes and benzothiophenes as inhibitors of microsomal triglyceride transfer protein (MTP) and/or apolipoprotein B (Apo B) secretion
EP3319444B1 (en) Mu opioid receptor modulators
WO2003044016A1 (en) 3-SUBSTITUTED OXINDOLE β3 AGONISTS
JP2009242437A (ja) スルホンアミド誘導体
EP3565543A1 (en) Mu opioid receptor modulators
AU2009232836A1 (en) Indolinone compound
JPWO2003024950A1 (ja) クマリン誘導体
KR20040028769A (ko) 카텝신 억제제로서의 화합물 및 조성물

Legal Events

Date Code Title Description
WWE Wipo information: entry into national phase

Ref document number: P-1004/03

Country of ref document: YU

AK Designated states

Kind code of ref document: A1

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BY BZ CA CH CN CO CR CU CZ DE DK DM DZ EC EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NO NZ OM PH PL PT RO RU SD SE SG SI SK SL TJ TM TN TR TT TZ UA UG US UZ VN YU ZA ZM ZW

AL Designated countries for regional patents

Kind code of ref document: A1

Designated state(s): GH GM KE LS MW MZ SD SL SZ TZ UG ZM ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE TR BF BJ CF CG CI CM GA GN GQ GW ML MR NE SN TD TG

DFPE Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101)
121 Ep: the epo has been informed by wipo that ep was designated in this application
WWE Wipo information: entry into national phase

Ref document number: 2003/07818

Country of ref document: ZA

Ref document number: 200307818

Country of ref document: ZA

WWE Wipo information: entry into national phase

Ref document number: 528752

Country of ref document: NZ

WWE Wipo information: entry into national phase

Ref document number: 00954/MUMNP/2003

Country of ref document: IN

Ref document number: 954/MUMNP/2003

Country of ref document: IN

WWE Wipo information: entry into national phase

Ref document number: 158516

Country of ref document: IL

WWE Wipo information: entry into national phase

Ref document number: 2002307839

Country of ref document: AU

WWE Wipo information: entry into national phase

Ref document number: 2002780923

Country of ref document: EP

WWE Wipo information: entry into national phase

Ref document number: PA/a/2003/011707

Country of ref document: MX

WWE Wipo information: entry into national phase

Ref document number: P20031051A

Country of ref document: HR

WWE Wipo information: entry into national phase

Ref document number: 2451474

Country of ref document: CA

ENP Entry into the national phase

Ref document number: 10848702

Country of ref document: BG

Kind code of ref document: A

WWE Wipo information: entry into national phase

Ref document number: PV2003-3558

Country of ref document: CZ

Ref document number: 16102003

Country of ref document: SK

WWE Wipo information: entry into national phase

Ref document number: 2003508914

Country of ref document: JP

WWE Wipo information: entry into national phase

Ref document number: 7236

Country of ref document: GE

Ref document number: 5350

Country of ref document: GE

Ref document number: 1200301169

Country of ref document: VN

Ref document number: 200301310

Country of ref document: EA

WWE Wipo information: entry into national phase

Ref document number: 028130219

Country of ref document: CN

Ref document number: 1020037017167

Country of ref document: KR

WWP Wipo information: published in national office

Ref document number: 2002780923

Country of ref document: EP

WWP Wipo information: published in national office

Ref document number: PV2003-3558

Country of ref document: CZ

REG Reference to national code

Ref country code: DE

Ref legal event code: 8642

WWE Wipo information: entry into national phase

Ref document number: 1020057025027

Country of ref document: KR

WWG Wipo information: grant in national office

Ref document number: 2002780923

Country of ref document: EP