PE20030924A1 - Combinacion de inhibidores de ptm o inhibidores de la secrecion de apob con fibratos para la utilizacion como medicamentos - Google Patents
Combinacion de inhibidores de ptm o inhibidores de la secrecion de apob con fibratos para la utilizacion como medicamentosInfo
- 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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
- 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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- A61K31/17—Amides, e.g. hydroxamic acids having the group >N—C(O)—N< or >N—C(S)—N<, e.g. urea, thiourea, carmustine
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- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
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- A61K31/19—Carboxylic acids, e.g. valproic acid
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- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/216—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
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- A61K31/4025—Heterocyclic 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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- A61K31/41—Heterocyclic 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
- A61K31/4164—1,3-Diazoles
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- A61K31/4164—1,3-Diazoles
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- A61K31/4353—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4468—Non condensed piperidines, e.g. piperocaine having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
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- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
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- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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- 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)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE2002100633 DE10200633A1 (de) | 2002-01-10 | 2002-01-10 | Kombination von MTP Inhibitoren oder apoB-Sekretions-Inhibitoren mit Fibraten zur Verwendung als Arzneimittel |
DE10256184A DE10256184A1 (de) | 2002-12-02 | 2002-12-02 | Kombination von MTP Inhibitoren oder apoB-Sekretions-Inhibitoren mit Fibraten zur Verwendung als Arzneimittel |
Publications (1)
Publication Number | Publication Date |
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PE20030924A1 true PE20030924A1 (es) | 2003-12-17 |
Family
ID=26010911
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2003000036A PE20030924A1 (es) | 2002-01-10 | 2003-01-09 | Combinacion de inhibidores de ptm o inhibidores de la secrecion de apob con fibratos para la utilizacion como medicamentos |
Country Status (9)
Country | Link |
---|---|
EP (1) | EP1465613A2 (es) |
JP (1) | JP2005525309A (es) |
AR (1) | AR038178A1 (es) |
AU (1) | AU2003205570A1 (es) |
CA (1) | CA2471566A1 (es) |
PE (1) | PE20030924A1 (es) |
TW (1) | TW200402292A (es) |
UY (1) | UY27610A1 (es) |
WO (1) | WO2003057205A2 (es) |
Families Citing this family (15)
Publication number | Priority date | Publication date | Assignee | Title |
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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 (ja) * | 2003-10-15 | 2007-01-18 | Ube Ind Ltd | 新規イソキノリン誘導体 |
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 |
ES2324794T3 (es) | 2004-12-21 | 2009-08-14 | Gilead Sciences Inc | Imidazo(4,5-c)pyridine componente y metodo de tratamiento antiviral. |
US20060241073A1 (en) * | 2005-04-20 | 2006-10-26 | Wanders Ronaldus J A | Means and methods for counteracting fatty acid accumulation |
UA97348C2 (en) * | 2005-07-29 | 2012-02-10 | 4Сц Аг | HETEROCYCLIC NF-kB INHIBITORS |
PT2038275E (pt) | 2006-07-07 | 2010-04-08 | Puerstinger Gerhard | Novo composto de piridazina e sua utilização |
JP5642922B2 (ja) * | 2007-04-24 | 2014-12-17 | サントリーホールディングス株式会社 | 複数の肝障害マーカーを指標とする肝障害の評価方法 |
TWI444379B (zh) | 2007-06-29 | 2014-07-11 | Sunesis Pharmaceuticals Inc | 有用於作為Raf激酶抑制劑之化合物 |
UA99466C2 (en) | 2007-07-06 | 2012-08-27 | Гилиад Сайенсиз, Инк. | Crystalline pyridazine compound |
CN102548986A (zh) | 2009-06-05 | 2012-07-04 | 链接医药公司 | 氨基吡咯烷酮衍生物及其用途 |
CN111065383A (zh) | 2017-07-11 | 2020-04-24 | 沃泰克斯药物股份有限公司 | 用作钠通道调节剂的羧酰胺 |
EP3762368B1 (en) | 2018-03-08 | 2022-01-26 | Incyte Corporation | Aminopyrazine diol compounds as pi3k-y inhibitors |
US11046658B2 (en) | 2018-07-02 | 2021-06-29 | Incyte Corporation | Aminopyrazine derivatives as PI3K-γ inhibitors |
Family Cites Families (4)
Publication number | Priority date | Publication date | Assignee | Title |
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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 (de) * | 2000-07-08 | 2002-01-17 | Boehringer Ingelheim Pharma | Biphenylcarbonsäureamide, ihre Herstellung und ihre Verwendung als Arzneimittel |
DE10132686A1 (de) * | 2001-07-05 | 2003-01-16 | Boehringer Ingelheim Pharma | Heteroarylcarbonsäureamide, ihre Herstellung und ihre Verwendung als Arzneimittel |
-
2003
- 2003-01-07 AU AU2003205570A patent/AU2003205570A1/en not_active Abandoned
- 2003-01-07 WO PCT/EP2003/000057 patent/WO2003057205A2/de active Application Filing
- 2003-01-07 JP JP2003557563A patent/JP2005525309A/ja active Pending
- 2003-01-07 EP EP03702391A patent/EP1465613A2/de not_active Ceased
- 2003-01-07 UY UY27610A patent/UY27610A1/es not_active Application Discontinuation
- 2003-01-07 CA CA002471566A patent/CA2471566A1/en not_active Abandoned
- 2003-01-08 TW TW092100321A patent/TW200402292A/zh unknown
- 2003-01-09 PE PE2003000036A patent/PE20030924A1/es not_active Application Discontinuation
- 2003-01-10 AR ARP030100056A patent/AR038178A1/es not_active Withdrawn
Also Published As
Publication number | Publication date |
---|---|
EP1465613A2 (de) | 2004-10-13 |
AU2003205570A8 (en) | 2003-07-24 |
WO2003057205A3 (de) | 2004-04-01 |
AR038178A1 (es) | 2005-01-05 |
TW200402292A (en) | 2004-02-16 |
UY27610A1 (es) | 2003-08-29 |
WO2003057205A2 (de) | 2003-07-17 |
AU2003205570A1 (en) | 2003-07-24 |
JP2005525309A (ja) | 2005-08-25 |
CA2471566A1 (en) | 2003-07-17 |
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