BRPI0414671A - inibidores da cetp e metabolitos dos mesmos - Google Patents
inibidores da cetp e metabolitos dos mesmosInfo
- Publication number
- BRPI0414671A BRPI0414671A BRPI0414671-9A BRPI0414671A BRPI0414671A BR PI0414671 A BRPI0414671 A BR PI0414671A BR PI0414671 A BRPI0414671 A BR PI0414671A BR PI0414671 A BRPI0414671 A BR PI0414671A
- Authority
- BR
- Brazil
- Prior art keywords
- inhibitors
- metabolites
- plasma
- cetp
- torcetrapib
- Prior art date
Links
- 239000003354 cholesterol ester transfer protein inhibitor Substances 0.000 title abstract 2
- 239000002207 metabolite Substances 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 abstract 3
- 102000012336 Cholesterol Ester Transfer Proteins Human genes 0.000 abstract 2
- 108010061846 Cholesterol Ester Transfer Proteins Proteins 0.000 abstract 2
- 108010023302 HDL Cholesterol Proteins 0.000 abstract 2
- 108010007622 LDL Lipoproteins Proteins 0.000 abstract 2
- 102000007330 LDL Lipoproteins Human genes 0.000 abstract 2
- 241000124008 Mammalia Species 0.000 abstract 2
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 150000002632 lipids Chemical class 0.000 abstract 2
- CMSGWTNRGKRWGS-NQIIRXRSSA-N torcetrapib Chemical compound COC(=O)N([C@H]1C[C@@H](CC)N(C2=CC=C(C=C21)C(F)(F)F)C(=O)OCC)CC1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1 CMSGWTNRGKRWGS-NQIIRXRSSA-N 0.000 abstract 2
- 229950004514 torcetrapib Drugs 0.000 abstract 2
- 102000015779 HDL Lipoproteins Human genes 0.000 abstract 1
- 239000000090 biomarker Substances 0.000 abstract 1
- 235000012000 cholesterol Nutrition 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003626 triacylglycerols Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
- C07C309/01—Sulfonic acids
- C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
- C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
- C07C309/13—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing nitrogen atoms, not being part of nitro or nitroso groups, bound to the carbon skeleton
- C07C309/14—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing nitrogen atoms, not being part of nitro or nitroso groups, bound to the carbon skeleton containing amino groups bound to the carbon skeleton
- C07C309/15—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing nitrogen atoms, not being part of nitro or nitroso groups, bound to the carbon skeleton containing amino groups bound to the carbon skeleton the nitrogen atom of at least one of the amino groups being part of any of the groups, X being a hetero atom, Y being any atom
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/04—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms
- C07D215/06—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms having only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to the ring nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/04—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms
- C07D215/08—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms with acylated ring nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/12—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/12—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D215/14—Radicals substituted by oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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 ring carbon atoms
- C07D215/38—Nitrogen atoms
- C07D215/42—Nitrogen atoms attached in position 4
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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 ring carbon atoms
- C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Steroid Compounds (AREA)
- Quinoline Compounds (AREA)
- Saccharide Compounds (AREA)
Abstract
"INIBIDORES DA CETP E METABOLITOS DOS MESMOS". A presente invenção refere-se a compostos resultantes da administração de torcetrapib a um mamífero, e a utilização de tais compostos como indicador ou biomarcador para a presença ou exposição de torcetrapib no plasma de um mamífero, incluindo o ser humano. A invenção também se refere a inibidores da proteína de transferência de éster de colesterila (CETP), composições farmacêuticas contendo tais inibidores e a utilização de tais inibidores para elevar certos níveis de lipídeo no plasma, incluindo a lipoproteína de elevada densidade, colesterol (HDL) e para diminuir certos nívis de outros lipídeos no plasma, tais como o da lipoproteína de baixa densidade, colesterol (LDL) e triglicerídeos.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US50738503P | 2003-09-30 | 2003-09-30 | |
| PCT/IB2004/003054 WO2005033082A2 (en) | 2003-09-30 | 2004-09-20 | Cetp inhibitors and metabolites thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BRPI0414671A true BRPI0414671A (pt) | 2006-11-21 |
Family
ID=34421617
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0414671-9A BRPI0414671A (pt) | 2003-09-30 | 2004-09-20 | inibidores da cetp e metabolitos dos mesmos |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US20070004774A1 (pt) |
| EP (1) | EP1670765A2 (pt) |
| JP (1) | JP2007507481A (pt) |
| AR (1) | AR045951A1 (pt) |
| BR (1) | BRPI0414671A (pt) |
| CA (1) | CA2540231A1 (pt) |
| MX (1) | MXPA06003499A (pt) |
| TW (1) | TW200511993A (pt) |
| WO (1) | WO2005033082A2 (pt) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE602004023100D1 (de) | 2003-10-08 | 2009-10-22 | Lilly Co Eli | Verbindungen und verfahren zur behandlung von dyslipidemie |
| WO2006033004A1 (en) * | 2004-09-23 | 2006-03-30 | Pfizer Products Inc. | Quinoline compounds as cetp inhibitors |
| US7737155B2 (en) | 2005-05-17 | 2010-06-15 | Schering Corporation | Nitrogen-containing heterocyclic compounds and methods of use thereof |
| US8022217B2 (en) | 2006-07-31 | 2011-09-20 | Cadila Healthcare Limited | Compounds suitable as modulators of HDL |
| CA2681628C (en) | 2007-03-16 | 2016-10-18 | Concert Pharmaceuticals, Inc. | Inhibitors of cholesterol ester transfer protein |
| AU2012202172B2 (en) * | 2007-11-05 | 2013-08-29 | Novartis Ag | 4-benzylamino-1-carboxyacyl-piperidine derivatives as CETP inhibitors useful for the treatment of diseases such as hyperlipidemia or arteriosclerosis |
| CN101910150B (zh) | 2007-11-05 | 2013-09-18 | 诺瓦提斯公司 | 作为cetp抑制剂、可用于治疗疾病如高脂血症或动脉硬化的4-苄基氨基-1-羧基酰基哌啶衍生物 |
| MX2010006063A (es) | 2007-12-03 | 2010-07-01 | Novartis Ag | Derivados de 4-bencil-amino-pirrolidina 1,2-disustituida como inhibidores de la proteina de transferencia de colesteril-ester (cetp) utiles para el tratamiento de las enfermedades tales como hiperlipidemia o arterioesclerosis. |
| US20110243940A1 (en) | 2008-12-16 | 2011-10-06 | Schering Corporation | Bicyclic pyranone derivatives and methods of use thereof |
| EP2379547A1 (en) | 2008-12-16 | 2011-10-26 | Schering Corporation | Pyridopyrimidine derivatives and methods of use thereof |
| ES2648788T3 (es) | 2011-01-26 | 2018-01-08 | Inserm - Institut National De La Santé Et De La Recherche Médicale | Método para evaluar el riesgo de un sujeto de tener una enfermedad cardiovascular |
| CN111004177A (zh) * | 2019-12-26 | 2020-04-14 | 河南省科学院高新技术研究中心 | 一种1-羟乙基-2,2,4-三甲基-1,2,3,4-四氢喹啉的制备方法 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GT199900147A (es) * | 1998-09-17 | 1999-09-06 | 1, 2, 3, 4- tetrahidroquinolinas 2-sustituidas 4-amino sustituidas. | |
| US6197786B1 (en) * | 1998-09-17 | 2001-03-06 | Pfizer Inc | 4-Carboxyamino-2-substituted-1,2,3,4-tetrahydroquinolines |
| US7115279B2 (en) * | 2000-08-03 | 2006-10-03 | Curatolo William J | Pharmaceutical compositions of cholesteryl ester transfer protein inhibitors |
| EA200301139A1 (ru) * | 2001-06-21 | 2004-12-30 | Пфайзер Продактс Инк. | Самоэмульгирующиеся препараты ингибиторов белка-переносчика эфиров холестерина |
| US7071210B2 (en) * | 2002-07-02 | 2006-07-04 | Pfizer Inc. | CETP inhibitors in combination with antihypertensive agents and uses thereof |
-
2004
- 2004-09-20 WO PCT/IB2004/003054 patent/WO2005033082A2/en not_active Ceased
- 2004-09-20 JP JP2006530727A patent/JP2007507481A/ja active Pending
- 2004-09-20 BR BRPI0414671-9A patent/BRPI0414671A/pt not_active Application Discontinuation
- 2004-09-20 CA CA002540231A patent/CA2540231A1/en not_active Abandoned
- 2004-09-20 EP EP04769424A patent/EP1670765A2/en not_active Withdrawn
- 2004-09-20 MX MXPA06003499A patent/MXPA06003499A/es unknown
- 2004-09-28 AR ARP040103515A patent/AR045951A1/es unknown
- 2004-09-29 TW TW093129424A patent/TW200511993A/zh unknown
- 2004-09-30 US US10/579,898 patent/US20070004774A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| US20070004774A1 (en) | 2007-01-04 |
| WO2005033082A3 (en) | 2005-06-16 |
| WO2005033082A2 (en) | 2005-04-14 |
| AR045951A1 (es) | 2005-11-16 |
| CA2540231A1 (en) | 2005-04-14 |
| EP1670765A2 (en) | 2006-06-21 |
| JP2007507481A (ja) | 2007-03-29 |
| TW200511993A (en) | 2005-04-01 |
| MXPA06003499A (es) | 2006-06-08 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B11A | Dismissal acc. art.33 of ipl - examination not requested within 36 months of filing | ||
| B11Y | Definitive dismissal acc. article 33 of ipl - extension of time limit for request of examination expired |