AR053653A1 - Formulaciones de benzoxazoles substituidos - Google Patents
Formulaciones de benzoxazoles substituidosInfo
- Publication number
- AR053653A1 AR053653A1 ARP050105015A ARP050105015A AR053653A1 AR 053653 A1 AR053653 A1 AR 053653A1 AR P050105015 A ARP050105015 A AR P050105015A AR P050105015 A ARP050105015 A AR P050105015A AR 053653 A1 AR053653 A1 AR 053653A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- trifluoroalkoxy
- halogen
- pharmaceutical formulation
- trifluoroalkyl
- Prior art date
Links
- 239000000203 mixture Substances 0.000 title abstract 3
- BCMCBBGGLRIHSE-UHFFFAOYSA-N 1,3-benzoxazole Chemical class C1=CC=C2OC=NC2=C1 BCMCBBGGLRIHSE-UHFFFAOYSA-N 0.000 title 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 6
- 229910052736 halogen Inorganic materials 0.000 abstract 6
- 150000002367 halogens Chemical class 0.000 abstract 6
- 239000008194 pharmaceutical composition Substances 0.000 abstract 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 5
- 125000004950 trifluoroalkyl group Chemical group 0.000 abstract 5
- 101100134925 Gallus gallus COR6 gene Proteins 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 4
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 3
- 125000000041 C6-C10 aryl group Chemical group 0.000 abstract 3
- 125000000304 alkynyl group Chemical group 0.000 abstract 3
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 2
- 239000000945 filler Substances 0.000 abstract 2
- 238000009472 formulation Methods 0.000 abstract 2
- 239000000546 pharmaceutical excipient Substances 0.000 abstract 2
- 239000002831 pharmacologic agent Substances 0.000 abstract 2
- 239000002904 solvent Substances 0.000 abstract 2
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract 1
- 125000002373 5 membered heterocyclic group Chemical group 0.000 abstract 1
- 125000004070 6 membered heterocyclic group Chemical group 0.000 abstract 1
- 102000000509 Estrogen Receptor beta Human genes 0.000 abstract 1
- 108010041356 Estrogen Receptor beta Proteins 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 239000003446 ligand Substances 0.000 abstract 1
- 230000001050 lubricating effect Effects 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 125000004001 thioalkyl group Chemical group 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1641—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- 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
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- 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
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- 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
- A61K31/42—Oxazoles
- A61K31/423—Oxazoles condensed with carbocyclic rings
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- 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
- A61K31/425—Thiazoles
- A61K31/428—Thiazoles condensed with carbocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2031—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/30—Oestrogens
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (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)
- Endocrinology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Diabetes (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Formulaciones y procesos para la fabricacion de formulaciones que contienen el ligando ERbeta-selectivo, ERB-0412. Reivindicacion 1: Una formulacion farmacéutica caracterizada porque comprende una cantidad farmacéuticamente efectiva de un agente farmacologico activo y un sistema vehículo o sistema excipiente, en donde dicho sistema vehículo o sistema excipiente comprende: a) un componente de relleno/disolvente que comprende desde alrededor de 40% hasta alrededor de 90% en peso de la formulacion farmacéutica; b) un componente agente modificador de superficie que comprende desde alrededor de 0,4% hasta alrededor de 15% en peso de la formulacion farmacéutica; c) un componente desintegrante desde alrededor de 0,01% hasta alrededor de 10% en peso de la formulacion farmacéutica; d) opcionalmente, un segundo componente de relleno/disolvente que comprende hasta alrededor de 20% en peso de la formulacion farmacéutica; y e) un componente lubricante que comprende desde alrededor de 0,01% hasta alrededor de 5% en peso de la formulacion farmacéutica; en donde el agente farmacologico activo tiene la formula (1) en la cual R1 es H, hidroxilo, halogeno, alquilo C1-8, trifluoroalquilo C1-6, cicloalquilo C3-8, alcoxi C1-6, trifluoroalcoxi C1-6, tioalquilo C1-6, sulfoxoalquilo C1-6, sulfonoalquilo C1-6, arilo C6-10, un anillo heterocíclico de 5 o 6 miembros que tiene 1 a 4 heteroátomos seleccionados de O, N o S, - NO2, -NR5R6, -N(R5)COR6, -CN, -CHFCN, -CF2CN, alquinilo C2-7, o alquenilo C2-7; en donde los residuos alquilo o alquenilo están opcionalmente sustituidos con hidroxilo, -CN, halogeno, trifluoralquilo, trifluoroalcoxi, -COR5, -CO2R5, -NO2, -CONR5R6, NR5R6 o N(R5) COR6; R2 y R2a son cada uno, independientemente, H, hidroxilo, halogeno, alquilo C1-6, alcoxi C1-4, alquenilo C2-7, alquinilo C2-7, trifluoroalquilo C1-6, trifluoroalcoxi C1-6; en donde los residuos de alquilo o alquenilo están opcionalmente sustituidos con hidroxilo, -CN, halogeno, trifluoroalquilo, trifluoroalcoxi, -COR5, -CO2R5, -NO2, -CONR5R6, -NR5R6 o N(R5)COR6; R3; R3a, y R4 son cada uno, independientemente, H, alquilo 1-6, alquenilo C2-7, alquinilo C2-7, halogeno, alcoxi C1-4, trifluoroalquilo C1-6 o trifluoroalcoxi C1-6; en donde los residuos alquilo o alquenilo están opcionalmente sustituidos con hidroxilo, -CN, halogeno, trifluoroalquilo, trifluoroalcoxi, - COR5, -CO2R5, -NO2, CONR5R6, NR5R6 o N(R5)COR6; R5, R6 son cada uno independientemente H, alquilo C1-6, o arilo C6-10, X es O, , o NR7; y R7 es H, alquilo C1-6 o arilo C6-10, -COR5, -CO2R5 o -SO2R5, o una sal farmacéuticamente aceptable de lo mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US63237504P | 2004-12-02 | 2004-12-02 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR053653A1 true AR053653A1 (es) | 2007-05-16 |
Family
ID=36565706
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP050105015A AR053653A1 (es) | 2004-12-02 | 2005-11-30 | Formulaciones de benzoxazoles substituidos |
Country Status (22)
| Country | Link |
|---|---|
| US (1) | US20060121110A1 (es) |
| EP (1) | EP1850833A2 (es) |
| JP (1) | JP2008521919A (es) |
| KR (1) | KR20070089921A (es) |
| CN (1) | CN101128188A (es) |
| AR (1) | AR053653A1 (es) |
| AU (1) | AU2005311823A1 (es) |
| BR (1) | BRPI0518786A2 (es) |
| CA (1) | CA2589033A1 (es) |
| CR (1) | CR9144A (es) |
| GT (1) | GT200500349A (es) |
| IL (1) | IL183393A0 (es) |
| MX (1) | MX2007006564A (es) |
| NI (1) | NI200700139A (es) |
| NO (1) | NO20072636L (es) |
| NZ (1) | NZ555395A (es) |
| PE (1) | PE20061083A1 (es) |
| RU (1) | RU2007120253A (es) |
| SV (1) | SV2006002317A (es) |
| TW (1) | TW200626144A (es) |
| WO (1) | WO2006060532A2 (es) |
| ZA (1) | ZA200705011B (es) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2008533012A (ja) * | 2005-03-08 | 2008-08-21 | ワイス | ２−（３−フルオロ−４−ヒドロキシフェニル）−７−ビニル−１，３−ベンゾキサゾール−５−オールの結晶形成およびエストロゲンレセプターモジュレーターとしてのその使用 |
| AR059574A1 (es) * | 2006-02-14 | 2008-04-16 | Wyeth Corp | Formulaciones farmaceuticas acuosas de ligandos selectivos er-beta |
| US20070208067A1 (en) * | 2006-03-06 | 2007-09-06 | Wyeth | Tablet Formulations and Processes |
| AR059742A1 (es) * | 2006-03-06 | 2008-04-23 | Wyeth Corp | Formulaciones farmaceuticas de una forma cristalina anhidra de 2-(3- fluor-4- dihidroxifenil) 7- vinil-1,3- benzoxazol -5-ol |
| AR059743A1 (es) * | 2006-03-06 | 2008-04-23 | Wyeth Corp | Formulaciones farmaceuticas de una forma cristalina de monohidrato de 2- (3- fluor-4- hidroxifenil )-7- vinil-1,3- benzoaxol-5-ol |
| AR059741A1 (es) * | 2006-03-06 | 2008-04-23 | Wyeth Corp | Formulaciones farmaceuticas liquidas y semisolidas y procedimientos |
| US20080175900A1 (en) * | 2006-11-21 | 2008-07-24 | Wyeth | Pharmaceutical formulations of an anhydrate crystal form of 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol |
| US20080175901A1 (en) * | 2006-11-21 | 2008-07-24 | Wyeth | Pharmaceutical formulations of a crystal form of 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol |
| US20080241234A1 (en) * | 2006-11-21 | 2008-10-02 | Wyeth | Pharmaceutical formulations of an anhydrate crystal form of 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol |
| GB0814953D0 (en) * | 2008-08-18 | 2008-09-24 | Unilever Plc | Improvements relating to nanodisperse compositions |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6331562B1 (en) * | 1998-12-30 | 2001-12-18 | Signal Pharmaceuticals, Inc. | Compounds and methods for modulation of estrogen receptors |
| JP2004524289A (ja) * | 2000-12-22 | 2004-08-12 | アストラゼネカ・アクチエボラーグ | 治療化合物 |
| UA83620C2 (ru) * | 2001-12-05 | 2008-08-11 | Уайт | Замещенные бензоксазолы и их аналоги как эстрогенные агенты |
| WO2003086319A2 (en) * | 2002-04-10 | 2003-10-23 | Merck & Co., Inc. | Pharmaceutical compositions containing an hiv integrase inhibitor and a nonionic surfactant |
-
2005
- 2005-11-30 BR BRPI0518786-9A patent/BRPI0518786A2/pt not_active IP Right Cessation
- 2005-11-30 JP JP2007544494A patent/JP2008521919A/ja not_active Withdrawn
- 2005-11-30 WO PCT/US2005/043407 patent/WO2006060532A2/en not_active Ceased
- 2005-11-30 SV SV2005002317A patent/SV2006002317A/es unknown
- 2005-11-30 AU AU2005311823A patent/AU2005311823A1/en not_active Abandoned
- 2005-11-30 CN CNA2005800474844A patent/CN101128188A/zh not_active Withdrawn
- 2005-11-30 GT GT200500349A patent/GT200500349A/es unknown
- 2005-11-30 RU RU2007120253/15A patent/RU2007120253A/ru not_active Application Discontinuation
- 2005-11-30 AR ARP050105015A patent/AR053653A1/es unknown
- 2005-11-30 US US11/290,197 patent/US20060121110A1/en not_active Abandoned
- 2005-11-30 EP EP05852593A patent/EP1850833A2/en not_active Withdrawn
- 2005-11-30 NZ NZ555395A patent/NZ555395A/en unknown
- 2005-11-30 MX MX2007006564A patent/MX2007006564A/es unknown
- 2005-11-30 TW TW094142062A patent/TW200626144A/zh unknown
- 2005-11-30 CA CA002589033A patent/CA2589033A1/en not_active Abandoned
- 2005-11-30 PE PE2005001386A patent/PE20061083A1/es not_active Application Discontinuation
- 2005-11-30 KR KR1020077012194A patent/KR20070089921A/ko not_active Withdrawn
-
2007
- 2007-05-23 CR CR9144A patent/CR9144A/es not_active Application Discontinuation
- 2007-05-24 NO NO20072636A patent/NO20072636L/no not_active Application Discontinuation
- 2007-05-24 IL IL183393A patent/IL183393A0/en unknown
- 2007-05-31 NI NI200700139A patent/NI200700139A/es unknown
- 2007-06-01 ZA ZA200705011A patent/ZA200705011B/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| ZA200705011B (en) | 2010-01-27 |
| CR9144A (es) | 2007-11-23 |
| PE20061083A1 (es) | 2006-11-14 |
| WO2006060532A2 (en) | 2006-06-08 |
| MX2007006564A (es) | 2007-06-19 |
| IL183393A0 (en) | 2007-09-20 |
| AU2005311823A1 (en) | 2006-06-08 |
| TW200626144A (en) | 2006-08-01 |
| RU2007120253A (ru) | 2009-01-10 |
| KR20070089921A (ko) | 2007-09-04 |
| NI200700139A (es) | 2008-05-09 |
| CN101128188A (zh) | 2008-02-20 |
| NZ555395A (en) | 2009-07-31 |
| JP2008521919A (ja) | 2008-06-26 |
| WO2006060532A3 (en) | 2006-11-16 |
| NO20072636L (no) | 2007-08-13 |
| US20060121110A1 (en) | 2006-06-08 |
| BRPI0518786A2 (pt) | 2008-12-09 |
| CA2589033A1 (en) | 2006-06-08 |
| SV2006002317A (es) | 2006-06-26 |
| GT200500349A (es) | 2006-07-03 |
| EP1850833A2 (en) | 2007-11-07 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |