WO2003057205A3 - Combination of mtp inhibitors or apob secretion inhibitors with fibrates for use as drugs - Google Patents

Combination of mtp inhibitors or apob secretion inhibitors with fibrates for use as drugs Download PDF

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Publication number
WO2003057205A3
WO2003057205A3 PCT/EP2003/000057 EP0300057W WO03057205A3 WO 2003057205 A3 WO2003057205 A3 WO 2003057205A3 EP 0300057 W EP0300057 W EP 0300057W WO 03057205 A3 WO03057205 A3 WO 03057205A3
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WO
WIPO (PCT)
Prior art keywords
inhibitors
fibrates
drugs
combination
mtp
Prior art date
Application number
PCT/EP2003/000057
Other languages
German (de)
French (fr)
Other versions
WO2003057205A2 (en
Inventor
Leo Thomas
Michael Mark
Original Assignee
Boehringer Ingelheim Pharma
Leo Thomas
Michael Mark
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 claimed from DE2002100633 external-priority patent/DE10200633A1/en
Priority claimed from DE10256184A external-priority patent/DE10256184A1/en
Application filed by Boehringer Ingelheim Pharma, Leo Thomas, Michael Mark filed Critical Boehringer Ingelheim Pharma
Priority to EP03702391A priority Critical patent/EP1465613A2/en
Priority to AU2003205570A priority patent/AU2003205570A1/en
Priority to CA002471566A priority patent/CA2471566A1/en
Priority to JP2003557563A priority patent/JP2005525309A/en
Publication of WO2003057205A2 publication Critical patent/WO2003057205A2/en
Publication of WO2003057205A3 publication Critical patent/WO2003057205A3/en

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/165Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/17Amides, e.g. hydroxamic acids having the group >N—C(O)—N< or >N—C(S)—N<, e.g. urea, thiourea, carmustine
    • AHUMAN NECESSITIES
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    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/192Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
    • AHUMAN NECESSITIES
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    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • AHUMAN NECESSITIES
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    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/216Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • 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
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    • 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
    • A61K31/4025Heterocyclic 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 not condensed and containing further heterocyclic rings, e.g. cromakalim
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    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • A61K31/438The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
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    • 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
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • 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
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4468Non condensed piperidines, e.g. piperocaine having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
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    • 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
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    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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    • A61K31/47Quinolines; Isoquinolines
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    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
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    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Hydrogenated Pyridines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

The invention relates to the use of fibrates for reducing the hepatic toxicity of MTP inhibitors and to pharmaceutical compositions that contain an MTP inhibitor and a fibrate.
PCT/EP2003/000057 2002-01-10 2003-01-07 Combination of mtp inhibitors or apob secretion inhibitors with fibrates for use as drugs WO2003057205A2 (en)

Priority Applications (4)

Application Number Priority Date Filing Date Title
EP03702391A EP1465613A2 (en) 2002-01-10 2003-01-07 Combination of mtp inhibitors or apob secretion inhibitors with fibrates for use as drugs
AU2003205570A AU2003205570A1 (en) 2002-01-10 2003-01-07 Combination of mtp inhibitors or apob secretion inhibitors with fibrates for use as drugs
CA002471566A CA2471566A1 (en) 2002-01-10 2003-01-07 Combination of mtp inhibitors or apob-secretion inhibitors with fibrates for use as pharmaceuticals
JP2003557563A JP2005525309A (en) 2002-01-10 2003-01-07 The combination of MTP inhibitors or apoB secretion inhibitor and fibrate for use as a medicament

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
DE10200633.4 2002-01-10
DE2002100633 DE10200633A1 (en) 2002-01-10 2002-01-10 Reducing hepatotoxicity of microsomal triglyceride transfer protein inhibitors, used e.g. in treatment of hyperlipemia, atherosclerosis or diabetes, by co-administration with fibrate
DE10256184A DE10256184A1 (en) 2002-12-02 2002-12-02 Reducing hepatotoxicity of microsomal triglyceride transfer protein inhibitors, used e.g. in treatment of hyperlipemia, atherosclerosis or diabetes, by co-administration with fibrate
DE10256184.2 2002-12-02

Publications (2)

Publication Number Publication Date
WO2003057205A2 WO2003057205A2 (en) 2003-07-17
WO2003057205A3 true WO2003057205A3 (en) 2004-04-01

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Application Number Title Priority Date Filing Date
PCT/EP2003/000057 WO2003057205A2 (en) 2002-01-10 2003-01-07 Combination of mtp inhibitors or apob secretion inhibitors with fibrates for use as drugs

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Country Link
EP (1) EP1465613A2 (en)
JP (1) JP2005525309A (en)
AR (1) AR038178A1 (en)
AU (1) AU2003205570A1 (en)
CA (1) CA2471566A1 (en)
PE (1) PE20030924A1 (en)
TW (1) TW200402292A (en)
UY (1) UY27610A1 (en)
WO (1) WO2003057205A2 (en)

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GB0215293D0 (en) 2002-07-03 2002-08-14 Rega Foundation Viral inhibitors
EP1578725A1 (en) * 2002-12-20 2005-09-28 Pfizer Products Inc. Microsomal triglyceride transfer protein inhibitors
JP2007008816A (en) * 2003-10-15 2007-01-18 Ube Ind Ltd New isoquinoline derivative
ES2381890T3 (en) 2003-12-22 2012-06-01 K.U.Leuven Research & Development Imidazo [4,5-c] pyridine compound and antiviral treatment methods
JP2008524335A (en) 2004-12-21 2008-07-10 ギリアド サイエンシズ, インコーポレイテッド Imidazo [4,5-c] pyridine compounds and antiviral treatment methods
US20060241073A1 (en) * 2005-04-20 2006-10-26 Wanders Ronaldus J A Means and methods for counteracting fatty acid accumulation
JP2009502816A (en) * 2005-07-29 2009-01-29 4エスツェー アクチェンゲゼルシャフト Novel heterocyclic NF-κB inhibitor
ATE454384T1 (en) 2006-07-07 2010-01-15 Gilead Sciences Inc NEW PYRIDAZINE COMPOUND AND USE THEREOF
JP5642922B2 (en) * 2007-04-24 2014-12-17 サントリーホールディングス株式会社 Evaluation method of liver injury using multiple liver injury markers as indicators
AR067354A1 (en) 2007-06-29 2009-10-07 Sunesis Pharmaceuticals Inc USEFUL COMPOUNDS AS INHIBITORS OF RAF QUINASA
UA99466C2 (en) 2007-07-06 2012-08-27 Гилиад Сайенсиз, Инк. Crystalline pyridazine compound
BRPI1010024A2 (en) 2009-06-05 2019-09-24 Link Medicine Corp aminopyrrolidinone derivatives and their use
CA3069720A1 (en) 2017-07-11 2019-01-17 Vertex Pharmaceuticals Incorporated Carboxamides as modulators of sodium channels
LT3762368T (en) 2018-03-08 2022-06-10 Incyte Corporation Aminopyrazine diol compounds as pi3k-y inhibitors
WO2020010003A1 (en) 2018-07-02 2020-01-09 Incyte Corporation AMINOPYRAZINE DERIVATIVES AS PI3K-γ INHIBITORS

Citations (4)

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WO1998003069A1 (en) * 1996-07-24 1998-01-29 Bristol-Myers Squibb Company Method for lowering serum lipid levels employing an mtp inhibitor in combination with another cholesterol lowering drug
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
DE10033337A1 (en) * 2000-07-08 2002-01-17 Boehringer Ingelheim Pharma Biphenylcarboxamides, their preparation and their use as medicaments
WO2003004020A1 (en) * 2001-07-05 2003-01-16 Boehringer Ingelheim Pharma Gmbh & Co. Kg Heteroaryl carboxylic acid amides, the production thereof and the use of the same as inhibitors of the microsomal triglyceride transfer protein (mtp)

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998003069A1 (en) * 1996-07-24 1998-01-29 Bristol-Myers Squibb Company Method for lowering serum lipid levels employing an mtp inhibitor in combination with another cholesterol lowering drug
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
DE10033337A1 (en) * 2000-07-08 2002-01-17 Boehringer Ingelheim Pharma Biphenylcarboxamides, their preparation and their use as medicaments
WO2003004020A1 (en) * 2001-07-05 2003-01-16 Boehringer Ingelheim Pharma Gmbh & Co. Kg Heteroaryl carboxylic acid amides, the production thereof and the use of the same as inhibitors of the microsomal triglyceride transfer protein (mtp)

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EP1465613A2 (en) 2004-10-13
CA2471566A1 (en) 2003-07-17
AU2003205570A8 (en) 2003-07-24
PE20030924A1 (en) 2003-12-17
TW200402292A (en) 2004-02-16
UY27610A1 (en) 2003-08-29
AU2003205570A1 (en) 2003-07-24
WO2003057205A2 (en) 2003-07-17
JP2005525309A (en) 2005-08-25
AR038178A1 (en) 2005-01-05

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