AR034255A1 - CARBOXIALQUILETER COMBINATIONS, ACAT INHIBITOR - Google Patents
CARBOXIALQUILETER COMBINATIONS, ACAT INHIBITORInfo
- Publication number
- AR034255A1 AR034255A1 ARP010102688A ARP010102688A AR034255A1 AR 034255 A1 AR034255 A1 AR 034255A1 AR P010102688 A ARP010102688 A AR P010102688A AR P010102688 A ARP010102688 A AR P010102688A AR 034255 A1 AR034255 A1 AR 034255A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- branched
- straight
- substituted
- hydrogen
- Prior art date
Links
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/075—Ethers or acetals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/255—Esters, e.g. nitroglycerine, selenocyanates of sulfoxy acids or sulfur analogues thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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
- A61P9/08—Vasodilators for multiple indications
-
- 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
-
- 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
- A61P9/12—Antihypertensives
Landscapes
- 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)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
- Pulmonology (AREA)
- Obesity (AREA)
- Emergency Medicine (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Composición farmacéutica que comprende: a) un carboxialquiléter; b) un inhibidor de acilcoenzima A: colesterol aciltransferasa (ACAT) o sus sales farmacéuticamente aceptables; y c) un portador o diluyente. El portador de ACAT tiene la fórmula (1) donde: X e Y son oxígeno, azufre, y (CR'R'')n; n es un número entero de 1 a 4; y R' y R'' son hidrógeno, alquilo, alcoxi, halógeno, hidroxi, aciloxi, cicloalquilo, fenilo optativamente sustituido, o R' y R'' juntos forman un espirocicloalquilo o un carbonilo; con la condición que al menos uno de X e Y es (CR'R'')n y que cuando X e Y son ambos (CR'R'')n, y R' y R'' son hidrógeno y n es 1, R1 y R2 son arilo; R es hidrógeno, alquilo C1-8 recto o ramificado o bencilo; R1 y R2 son: a) fenilo o fenoxi no sustituido o sustituido con 1 a 5 grupos fenilo, alquilo C1-6 recto o ramificado, alcoxi C1-6 recto o ramificado, fenoxi, hidroxi, flúor, cloro, bromo, nitro, trifluorometilo, -COOH, -COO(alquilo C1-4 recto o ramificado), -(CH2)pNR3R4 donde p es 0 ó 1, y R3 y R4 son hidrógeno o alquilo C1-4 recto o ramificado; b) 1- ó 2-naftilo no sustituido o sustituido con 1 a 3 grupos como en (a); c) arilalquilo; d) alquilo C1-20 recto o ramificado, saturado o con 1-3 enlaces dobles; y e) adamatilo o cicloalquilo con cicloalquilo C3-6. El carboxialquiléter tiene la fórmula (2) donde: n y m son números enteros de 2 a 9; R1, R2, R3 y R4 son alquilo C1-6, alquenilo C2-6, alquinilo C2-6 y R1 y R2 junto con el carbono al cual están unidos, y R3 y R4 junto con el carbono al cual están unidos, pueden completar un anillo carbocíclico C3-6; Y1 e Y2 son COOH, CHO, tetrazol y COOR5; R5 es alquilo C1-6, alquenilo C2-6, y alquinilo C2-6; los grupos alquilo, alquenilo y alquinilo pueden ser sustituidos con 1ó 2 grupos halo, hidroxi, alcoxi C1-6 y fenilo. Una primer composición farmacéutica para uso con una segunda composición farmacéutica que comprenden un inhibidor de ACAT y un carboxialquiléter y conjunto correspondiente con formas de dosificación unitarias. Estas composiciones son útiles para tratar dislipidemias y síndromes isquémicos, ataques cardíacos y trastornos cardiovasculares relacionados.Pharmaceutical composition comprising: a) a carboxyalkyl ether; b) an acylcoenzyme A: cholesterol acyltransferase (ACAT) inhibitor or its pharmaceutically acceptable salts; and c) a carrier or diluent. The ACAT carrier has the formula (1) where: X and Y are oxygen, sulfur, and (CR'R '') n; n is an integer from 1 to 4; and R 'and R' 'are hydrogen, alkyl, alkoxy, halogen, hydroxy, acyloxy, cycloalkyl, optionally substituted phenyl, or R' and R '' together form a spirocycloalkyl or a carbonyl; with the condition that at least one of X and Y is (CR'R '') n and that when X and Y are both (CR'R '') n, and R 'and R' 'are hydrogen and n is 1, R1 and R2 are aryl; R is hydrogen, straight or branched C1-8 alkyl or benzyl; R1 and R2 are: a) phenyl or phenoxy not substituted or substituted with 1 to 5 phenyl groups, straight or branched C1-6 alkyl, straight or branched C1-6 alkoxy, phenoxy, hydroxy, fluorine, chlorine, bromine, nitro, trifluoromethyl , -COOH, -COO (straight or branched C1-4 alkyl), - (CH2) pNR3R4 where p is 0 or 1, and R3 and R4 are hydrogen or straight or branched C1-4 alkyl; b) 1- or 2-naphthyl unsubstituted or substituted with 1 to 3 groups as in (a); c) arylalkyl; d) straight or branched C1-20 alkyl, saturated or with 1-3 double bonds; and e) adamathyl or cycloalkyl with C3-6 cycloalkyl. The carboxyalkyl ether has the formula (2) where: n and m are whole numbers from 2 to 9; R1, R2, R3 and R4 are C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl and R1 and R2 together with the carbon to which they are attached, and R3 and R4 together with the carbon to which they are attached, can complete a C3-6 carbocyclic ring; Y1 and Y2 are COOH, CHO, tetrazole and COOR5; R5 is C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl; the alkyl, alkenyl and alkynyl groups can be substituted with 1 or 2 halo, hydroxy, C1-6 alkoxy and phenyl groups. A first pharmaceutical composition for use with a second pharmaceutical composition comprising an ACAT inhibitor and a corresponding carboxyalkylether and unit with unit dosage forms. These compositions are useful for treating dyslipidemias and ischemic syndromes, heart attacks and related cardiovascular disorders.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US21005600P | 2000-06-07 | 2000-06-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR034255A1 true AR034255A1 (en) | 2004-02-18 |
Family
ID=22781424
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP010102688A AR034255A1 (en) | 2000-06-07 | 2001-06-06 | CARBOXIALQUILETER COMBINATIONS, ACAT INHIBITOR |
Country Status (14)
| Country | Link |
|---|---|
| EP (1) | EP1292363A2 (en) |
| JP (1) | JP2003535125A (en) |
| AR (1) | AR034255A1 (en) |
| AU (1) | AU2001263003A1 (en) |
| BR (1) | BR0111428A (en) |
| CA (1) | CA2413906A1 (en) |
| GT (1) | GT200100106A (en) |
| MX (1) | MXPA02010762A (en) |
| PA (1) | PA8518601A1 (en) |
| PE (1) | PE20020265A1 (en) |
| SV (1) | SV2002000466A (en) |
| TN (1) | TNSN01085A1 (en) |
| UY (1) | UY26752A1 (en) |
| WO (1) | WO2001093845A2 (en) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7387236B2 (en) | 2001-10-09 | 2008-06-17 | Delaware Capital Formation, Inc. | Dispensing of currency |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2311356C (en) * | 1998-01-28 | 2004-07-13 | Warner-Lambert Company | Method for treating alzheimer's disease |
-
2001
- 2001-05-08 WO PCT/US2001/014804 patent/WO2001093845A2/en active Application Filing
- 2001-05-08 BR BR0111428-0A patent/BR0111428A/en not_active IP Right Cessation
- 2001-05-08 CA CA002413906A patent/CA2413906A1/en not_active Abandoned
- 2001-05-08 JP JP2002501418A patent/JP2003535125A/en active Pending
- 2001-05-08 AU AU2001263003A patent/AU2001263003A1/en not_active Abandoned
- 2001-05-08 EP EP01937250A patent/EP1292363A2/en not_active Withdrawn
- 2001-05-08 MX MXPA02010762A patent/MXPA02010762A/en not_active Application Discontinuation
- 2001-05-24 SV SV2001000466A patent/SV2002000466A/en not_active Application Discontinuation
- 2001-06-05 TN TNTNSN01085A patent/TNSN01085A1/en unknown
- 2001-06-05 UY UY26752A patent/UY26752A1/en not_active Application Discontinuation
- 2001-06-05 PE PE2001000517A patent/PE20020265A1/en not_active Application Discontinuation
- 2001-06-05 GT GT200100106A patent/GT200100106A/en unknown
- 2001-06-05 PA PA20018518601A patent/PA8518601A1/en unknown
- 2001-06-06 AR ARP010102688A patent/AR034255A1/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2003535125A (en) | 2003-11-25 |
| TNSN01085A1 (en) | 2005-11-10 |
| EP1292363A2 (en) | 2003-03-19 |
| GT200100106A (en) | 2002-05-20 |
| BR0111428A (en) | 2003-06-10 |
| PA8518601A1 (en) | 2002-07-30 |
| MXPA02010762A (en) | 2003-03-10 |
| CA2413906A1 (en) | 2001-12-13 |
| WO2001093845A3 (en) | 2002-10-10 |
| AU2001263003A1 (en) | 2001-12-17 |
| SV2002000466A (en) | 2002-04-03 |
| PE20020265A1 (en) | 2002-04-19 |
| WO2001093845A2 (en) | 2001-12-13 |
| UY26752A1 (en) | 2001-07-31 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR061341A1 (en) | COMPOSITE OF 5-AMINO-N - [(DISUSTITUTED-PHENYL) CARBONIL- (AMINO-TRIFLUORO-2-HIDROXIPROPIL) -FUOROFENIL] -1H-PIRAZOL-4-CARBOXANMIDA, ITS USE FOR THE PREPARATION OF A PHARMACEUTICAL COMPOSITION COMPOSITION , PROCESS AND INTERMEDIATE COMPOUNDS FOR PREPARATION | |
| ES2188957T3 (en) | N- (4- (HETEROARILMETIL) FENIL) -HETEROARILAMINAS. | |
| AR070861A1 (en) | USE OF COMBINATION THERAPY WITH C-MET AND EGFR ANTAGONISTS | |
| CO6170406A2 (en) | DERIVATIVES OF 2-ALQUILTIO-2-QUINOLINILOXI-ACETAMIDA AS FUNGICIDES | |
| ECSP077290A (en) | DERIVATIVES OF ISOXAZOLINE AND ITS USE AS HERBICIDES | |
| PA8517101A1 (en) | USEFUL TROPANO DERIVATIVES IN THERAPY | |
| CR7583A (en) | NEW VENLAFAXINA O-DESMETIL FORMAMATE SALT | |
| RS53420B (en) | Combinations of a macrocyclic quinoxaline compound which is an hcv ns3 protease inhibitor with other hcv agents | |
| CO6190534A2 (en) | NEW DERIVATIVES OF 1,4 BENZOTIEPINA-1, 1-DIOXIDE REPLACED WITH RADICALS BENCILO METHOD FOR PREPARATION PHARMACEUTICAL PRODUCTS THAT UNDERSTAND THESE COMPOUNDS AND THEIR USE | |
| BRPI0516735B8 (en) | methods for producing (r)-2-acetamido-n-benzyl-3-methoxypropionamide (lacosamide) and a pharmaceutical formulation, and use of (r)-n-benzyl-2-nboc-amino-3-methoxypropionamide (c -937) | |
| ECSP055886A (en) | ISOINDOLINE DERIVATIVES | |
| SV2003000633A (en) | NEW TIADIAZOLS AND OXADIAZOLS AND THEIR USE AS INHIBITORS OF PHOSPHODIESTERASA-7 | |
| CO5700779A2 (en) | A PROCESS FOR THE PREPARATION OF OXI- (1H) -QUINOLIN-2-ONAS 5- (HALOACETIL) -8-SUBSTITUTED | |
| AR062620A1 (en) | INSECTICIDES N- REPLACED (2-SUBSTITUTES-1.3- TIAZOL) SULFOXIMINAL RENTAL | |
| AR017851A1 (en) | PHARMACEUTICAL COMPOSITION THAT INCLUDES A CARBOXIALCHYLICAL ETER AND A STATIN, FIRST PHARMACEUTICAL COMPOSITION FOR USE WITH A SECOND COMPOSITION PHARMACEUTICAL COMPOSITION TO ACHIEVE A HYPOLIPIDEMIC EFFECT AND CONTROL THE ADDITIONAL CARDIAC RISK IN A DIFFERENT LOGO | |
| AR044453A1 (en) | METOXI-PIRAZIN-TIENIL SULFONAMIDE DERIVATIVES | |
| AR034255A1 (en) | CARBOXIALQUILETER COMBINATIONS, ACAT INHIBITOR | |
| AR033350A1 (en) | ACIDOS (AMINOPROPIL) METHYLPHOSPHINICS, ITS USE FOR THE MANUFACTURE OF MEDICINES, PHARMACEUTICAL FORMULATION, AND INTERMEDIARIES | |
| CO6180429A2 (en) | PHARMACEUTICAL AGENT CONTAINING A HER2 INHIBITOR AND A HORMONAL THERAPEUTIC AGENT OR ANTI-BANERIGEN AGENT IN COMBINATION | |
| EA200500237A1 (en) | A NEW METHOD OF SYNTHESIS OF 1,3-DIHYDRO-2H-3-BENZAZEPIN-2-IT COMPOUNDS AND APPLICATION IN IVABRADINE SYNTHESIS AND ITS SALTS OF ACCESSION WITH PHARMACEUTICALS WITH ACCESSABLE | |
| AR025093A1 (en) | NEW DERIVATIVES OF TETRAZOLINONA | |
| DE60317894D1 (en) | TOOTH PAINT AGAINST KARIES | |
| AR032455A1 (en) | METHOD FOR THE PREPARATION OF CITALOPRAM, AN INTERMEDIARY EMPLOYED IN THE METHOD, A METHOD FOR THE PREPARATION OF THE INTERMEDIARY EMPLOYED IN THE METHOD AND PHARMACEUTICAL COMPOSITION ANTIDEPRESSIVE | |
| CO5611130A2 (en) | NEW OXAZOL DERIVATIVES, ITS MANUFACTURE AND USE AS PHARMACEUTICAL AGENTS | |
| EP2239254A4 (en) | Benzylpiperizine compound |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |