PE20030924A1 - COMBINATION OF PTM INHIBITORS OR INHIBITORS OF APOB SECRETION WITH FIBRATES FOR USE AS MEDICINES - Google Patents
COMBINATION OF PTM INHIBITORS OR INHIBITORS OF APOB SECRETION WITH FIBRATES FOR USE AS MEDICINESInfo
- Publication number
- PE20030924A1 PE20030924A1 PE2003000036A PE2003000036A PE20030924A1 PE 20030924 A1 PE20030924 A1 PE 20030924A1 PE 2003000036 A PE2003000036 A PE 2003000036A PE 2003000036 A PE2003000036 A PE 2003000036A PE 20030924 A1 PE20030924 A1 PE 20030924A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- inhibitors
- ptm
- carbonylamine
- trifluoromethylbiphenyl
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 5
- 229940125753 fibrate Drugs 0.000 title abstract 3
- 102100040202 Apolipoprotein B-100 Human genes 0.000 title 1
- 101000889953 Homo sapiens Apolipoprotein B-100 Proteins 0.000 title 1
- 239000003814 drug Substances 0.000 title 1
- 230000028327 secretion Effects 0.000 title 1
- IPDRRTURNBKLIH-UHFFFAOYSA-N 2-[4-(trifluoromethyl)phenyl]benzamide Chemical compound NC(=O)C1=CC=CC=C1C1=CC=C(C(F)(F)F)C=C1 IPDRRTURNBKLIH-UHFFFAOYSA-N 0.000 abstract 3
- -1 CYPROFIBRATE Chemical compound 0.000 abstract 3
- 150000001408 amides Chemical class 0.000 abstract 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- WZKSXHQDXQKIQJ-UHFFFAOYSA-N F[C](F)F Chemical class F[C](F)F WZKSXHQDXQKIQJ-UHFFFAOYSA-N 0.000 abstract 1
- HEMJJKBWTPKOJG-UHFFFAOYSA-N Gemfibrozil Chemical compound CC1=CC=C(C)C(OCCCC(C)(C)C(O)=O)=C1 HEMJJKBWTPKOJG-UHFFFAOYSA-N 0.000 abstract 1
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical class [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 1
- 229960000516 bezafibrate Drugs 0.000 abstract 1
- IIBYAHWJQTYFKB-UHFFFAOYSA-N bezafibrate Chemical compound C1=CC(OC(C)(C)C(O)=O)=CC=C1CCNC(=O)C1=CC=C(Cl)C=C1 IIBYAHWJQTYFKB-UHFFFAOYSA-N 0.000 abstract 1
- 229960001214 clofibrate Drugs 0.000 abstract 1
- KNHUKKLJHYUCFP-UHFFFAOYSA-N clofibrate Chemical compound CCOC(=O)C(C)(C)OC1=CC=C(Cl)C=C1 KNHUKKLJHYUCFP-UHFFFAOYSA-N 0.000 abstract 1
- 229960003627 gemfibrozil Drugs 0.000 abstract 1
- 230000002440 hepatic effect Effects 0.000 abstract 1
- 231100000304 hepatotoxicity Toxicity 0.000 abstract 1
- 230000007056 liver toxicity Effects 0.000 abstract 1
- 230000003228 microsomal effect Effects 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 102000004169 proteins and genes Human genes 0.000 abstract 1
- 108090000623 proteins and genes Proteins 0.000 abstract 1
- XTQHKBHJIVJGKJ-UHFFFAOYSA-N sulfur monoxide Chemical class S=O XTQHKBHJIVJGKJ-UHFFFAOYSA-N 0.000 abstract 1
- 230000001988 toxicity Effects 0.000 abstract 1
- 231100000419 toxicity Toxicity 0.000 abstract 1
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 abstract 1
Classifications
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- A61K31/167—Amides, 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
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- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
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- Obesity (AREA)
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- Gastroenterology & Hepatology (AREA)
- Pain & Pain Management (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Hydrogenated Pyridines (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
SE REFIERE AL USO DE FIBRATO SELECCIONADO DE BEZAFIBRATO, CIPROFIBRATO, CLOFIBRATO Y GEMFIBROZIL PARA REDUCIR LA TOXICIDAD DEL HIGADO DE INHIBIDORES DE PTM DE FORMULA I DONDE X1 ES CR1; X2 ES CR2; X3 ES CR3; X4 ES CR4 O UNO O DOS DE LOS GRUPO X1 A X4 SON NITROGENO Y EL RESTO ES CR1 A CR4; R1-R4 SON H, HALO, ALQUILO C1-C3, TRIFLUOROMETILO, OH, ALCOXI C1-C3, ENTRE OTROS; Aa ES O, S, NH, -N(ALQUILO C1-C3)-, SULFINILO, ENTRE OTROS; Ra ES FENILO, 1-NAFTILO, 2-NAFTILO, UN GRUPO HETEROARILO DE 5 MIEMBROS; R5 ES H, ALQUILO C1-C5; HET ES HETEROARILENO DE 5 MIEMBROS UNIDOS A TRAVES DE DOS ATOMOS DE C; R6 ES H, ALQUILO C1-C6; R7 ES ALQUILO C1-C9, ALQUENILO C3-C9, ENTRE OTROS. LOS COMPUESTOS DE FORMULA I SON AMIDA DE ACIDO N-[3-(BIFENIL-4-IL)-PROP-2-INIL]-4-(4´-TRIFLUOROMETILBIFENIL-2-CARBONILAMINO)-1-METIL-PIRROL-2-CARBOXILICO, AMIDA DE ACIDO N-[4-(1,4-DIOXA-8-AZA-ESPIRO[4.5]DEC-8-IL)-FENILMETIL]-4-(4´-TRIFLUOROMETILBIFENIL-2-CARBONILAMINO)-1-METIL-PIRROL-2-CARBOXILICO, AMIDA DE ACIDO N-[4-(3-AZA-ESPIRO[5.5]UNDEC-8-IL)-FENILMETIL]-4-(4´-TRIFLUOROMETILBIFENIL-2-CARBONILAMINO)-1-METIL-PIRROL-2-CARBOXILICO, ENTRE OTROS. SE REFIERE TAMBIEN A COMPOSICIONES FARMACEUTICAS QUE CONTIENEN UN INHIBIDOR DE PTM Y UN FIBRATO. LOS COMPUESTOS MENCIONADOS REDUCEN LA TOXICIDAD HEPATICA DE INHIBIDORES DE LA PROTEINA DE TRANSFERENCA DE TRIGLICERIDOS MICROSOMAL (PTM)REFERS TO THE USE OF SELECTED BEZAFIBRATE, CYPROFIBRATE, CLOFIBRATE, AND GEMFIBROZIL FIBRATE TO REDUCE THE LIVER TOXICITY OF FORMULA I PTM INHIBITORS WHERE X1 IS CR1; X2 IS CR2; X3 IS CR3; X4 IS CR4 OR ONE OR TWO OF THE GROUP X1 TO X4 ARE NITROGEN AND THE REST IS CR1 TO CR4; R1-R4 ARE H, HALO, C1-C3 ALKYL, TRIFLUOROMETHYL, OH, C1-C3 ALCOXY, AMONG OTHERS; Aa IS O, S, NH, -N (C1-C3 ALKYL) -, SULFINYL, AMONG OTHERS; Ra IS PHENYL, 1-NAPHTHYLUS, 2-NAPHTHYL, A HETEROARYL GROUP OF 5 MEMBERS; R5 IS H, C1-C5 ALKYL; HET IS 5-MEMBER HETEROARYLENE UNITED THROUGH TWO C ATOMS; R6 IS H, C1-C6 ALKYL; R7 IS C1-C9 ALKYL, C3-C9 ALKYL, AMONG OTHERS. THE COMPOUNDS OF FORMULA I ARE ACID AMIDE N- [3- (BIPHENYL-4-IL) -PROP-2-INYL] -4- (4'-TRIFLUOROMETHYLBIPHENYL-2-CARBONYLAMINE) -1-METHYL-PYRROL-2- CARBOXYL, ACID AMIDE N- [4- (1,4-DIOXA-8-AZA-SPIRO [4.5] DEC-8-IL) -PHENYLMETHYL] -4- (4'-TRIFLUOROMETHYLBIPHENYL-2-CARBONYLAMINE) -1- METHYL-PYRROL-2-CARBOXYL ACID AMIDE N- [4- (3-AZA-SPIRO [5.5] UNDEC-8-IL) -PHENYLMETHYL] -4- (4'-TRIFLUOROMETHYLBIPHENYL-2-CARBONYLAMINE) -1- METHYL-PYRROL-2-CARBOXYL, AMONG OTHERS. IT ALSO REFERS TO PHARMACEUTICAL COMPOSITIONS CONTAINING A PTM INHIBITOR AND A FIBRATE. THE MENTIONED COMPOUNDS REDUCE THE HEPATIC TOXICITY OF MICROSOMAL TRIGLYCERIDE TRANSFERENCE PROTEIN (PTM) INHIBITORS
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
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 |
Publications (1)
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PE20030924A1 true PE20030924A1 (en) | 2003-12-17 |
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Family Applications (1)
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PE2003000036A PE20030924A1 (en) | 2002-01-10 | 2003-01-09 | COMBINATION OF PTM INHIBITORS OR INHIBITORS OF APOB SECRETION WITH FIBRATES FOR USE AS MEDICINES |
Country Status (9)
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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 |
CA2505604A1 (en) * | 2002-12-20 | 2004-07-08 | Pfizer Products Inc. | Microsomal triglyceride transfer protein inhibitors |
JP2007008816A (en) * | 2003-10-15 | 2007-01-18 | Ube Ind Ltd | New isoquinoline derivative |
US20050222198A1 (en) | 2003-12-22 | 2005-10-06 | K.U. Leuven Research & Development, Gerhard Puerstinger And Gilead Sciences, Inc. | Imidazo[4,5-c]pyridine compounds and methods of antiviral treatment |
EP1841765B1 (en) | 2004-12-21 | 2009-03-25 | Gilead Sciences, Inc. | Imidazo[4,5-c]pyridine compound and method of antiviral treatment |
US20060241073A1 (en) * | 2005-04-20 | 2006-10-26 | Wanders Ronaldus J A | Means and methods for counteracting fatty acid accumulation |
BRPI0614188A2 (en) * | 2005-07-29 | 2011-03-15 | 4Sc Ag | heterocyclic nf-kappab inhibitor compounds, their use and pharmaceutical composition |
US7754720B2 (en) | 2006-07-07 | 2010-07-13 | Gilead Sciences, Inc. | 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 |
CL2008001933A1 (en) * | 2007-06-29 | 2009-09-25 | Millennium Pharm Inc | Pyrimidine derived compounds, raph kinase inhibitors; intermediate compounds; preparation procedure; pharmaceutical composition; and its use to treat proliferative, cardiac, neurodegenerative, inflammatory, bone, immunological, viral disease, among others. |
UA99466C2 (en) | 2007-07-06 | 2012-08-27 | Гилиад Сайенсиз, Инк. | Crystalline pyridazine compound |
SG176628A1 (en) | 2009-06-05 | 2012-01-30 | Link Medicine Corp | Aminopyrrolidinone derivatives and uses thereof |
JOP20200001A1 (en) | 2017-07-11 | 2022-10-30 | Vertex Pharma | Carboxamides as modulators of sodium channels |
PT3762368T (en) | 2018-03-08 | 2022-05-06 | Incyte Corp | Aminopyrazine diol compounds as pi3k-y inhibitors |
WO2020010003A1 (en) | 2018-07-02 | 2020-01-09 | Incyte Corporation | AMINOPYRAZINE DERIVATIVES AS PI3K-γ INHIBITORS |
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US5883109A (en) * | 1996-07-24 | 1999-03-16 | Bristol-Myers Squibb Company | Method for lowering serum lipid levels employing an MTP inhibitor in combination with another cholesterol lowering drug |
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 |
DE10033337A1 (en) * | 2000-07-08 | 2002-01-17 | Boehringer Ingelheim Pharma | Biphenylcarboxamides, their preparation and their use as medicaments |
DE10132686A1 (en) * | 2001-07-05 | 2003-01-16 | Boehringer Ingelheim Pharma | Heteroarylcarboxamides, their preparation and their use as medicines |
-
2003
- 2003-01-07 AU AU2003205570A patent/AU2003205570A1/en not_active Abandoned
- 2003-01-07 JP JP2003557563A patent/JP2005525309A/en active Pending
- 2003-01-07 UY UY27610A patent/UY27610A1/en not_active Application Discontinuation
- 2003-01-07 CA CA002471566A patent/CA2471566A1/en not_active Abandoned
- 2003-01-07 EP EP03702391A patent/EP1465613A2/en not_active Ceased
- 2003-01-07 WO PCT/EP2003/000057 patent/WO2003057205A2/en active Application Filing
- 2003-01-08 TW TW092100321A patent/TW200402292A/en unknown
- 2003-01-09 PE PE2003000036A patent/PE20030924A1/en not_active Application Discontinuation
- 2003-01-10 AR ARP030100056A patent/AR038178A1/en not_active Withdrawn
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Publication number | Publication date |
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EP1465613A2 (en) | 2004-10-13 |
AR038178A1 (en) | 2005-01-05 |
JP2005525309A (en) | 2005-08-25 |
AU2003205570A8 (en) | 2003-07-24 |
TW200402292A (en) | 2004-02-16 |
CA2471566A1 (en) | 2003-07-17 |
WO2003057205A2 (en) | 2003-07-17 |
WO2003057205A3 (en) | 2004-04-01 |
AU2003205570A1 (en) | 2003-07-24 |
UY27610A1 (en) | 2003-08-29 |
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