AR077549A1 - Una composicion farmaceutica topica para regular el factor de crecimiento endotelial vegf que comprende la (3-trifluoro-metil-fenil)-amida del acido 6-(6-hidroxi-metil-pirimidin-4-iloxi)-naftalen-1-carboxilico. - Google Patents
Una composicion farmaceutica topica para regular el factor de crecimiento endotelial vegf que comprende la (3-trifluoro-metil-fenil)-amida del acido 6-(6-hidroxi-metil-pirimidin-4-iloxi)-naftalen-1-carboxilico.Info
- Publication number
- AR077549A1 AR077549A1 ARP100102394A ARP100102394A AR077549A1 AR 077549 A1 AR077549 A1 AR 077549A1 AR P100102394 A ARP100102394 A AR P100102394A AR P100102394 A ARP100102394 A AR P100102394A AR 077549 A1 AR077549 A1 AR 077549A1
- Authority
- AR
- Argentina
- Prior art keywords
- methyl
- hydroxy
- pyrimidin
- trifluoro
- amide
- Prior art date
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Classifications
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- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
-
- 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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
-
- 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
- A61K9/10—Dispersions; Emulsions
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/04—Antipruritics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
- A61P31/22—Antivirals for DNA viruses for herpes viruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/34—One oxygen atom
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Dermatology (AREA)
- Virology (AREA)
- Ophthalmology & Optometry (AREA)
- Rheumatology (AREA)
- Oncology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Communicable Diseases (AREA)
- Molecular Biology (AREA)
- Biotechnology (AREA)
- Immunology (AREA)
- Dispersion Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
La presente se refiere a composiciones farmacéuticas de la (3-trifluoro-metil-fenil)-amida del ácido 6-(6-hidroxi-metil-pirimidin-4-iloxi)- naftalen-1-carboxílico, al uso de la (3-trifluoro-metil-fenil)-amida del ácido 6-(6- hidroxi-metil-pirimidin-4-iloxi)-naftalen-1-carboxílico, y a composiciones de la (3-trifluoro-metil-fenil)-amida del ácido 6-(6-hidroxi-metil-pirimidin-4-iloxi)-naftalen-1-carboxílico, en aplicaciones terapéuticas, en especial en las indicaciones con una desregulacion/sobre-expresion del factor de crecimiento endotelial vascular (VEGF), (neo)-vascularizacion, y angiogénesis impulsada por el factor de crecimiento endotelial vascular (VEGF), y a métodos para la elaboracion de estas composiciones; la presente se refiere además a las formas específicas de la (3-trifluoro-metil-fenil)-amida del ácido 6-(6-hidroxi-metil-pirimidin-4-iloxi)-naftalen-1-carboxílico, y a la elaboracion y el uso de estas formas. La presente solicitud también se refiere a un nuevo proceso para producir la (3-trifluoro-metil-fenil)-amida del ácido 6-(6-hidroxi-metil-pirimidin-4-iloxi)-naftalen-1-carboxílico. Reivindicacion 2. Una composicion de acuerdo con la reivindicacion 1, en donde la matriz contiene PEG de bajo peso molecular, PEG de alto peso molecular, y opcionalmente agua; de preferencia un PEG que tiene una masa molecular de 200 a 1,000 gramos/mol, un PEG que tiene una masa molecular de 2,000 a 5,000 gramos/mol, y agua. Reivindicacion 4: Una composicion de acuerdo con cualquiera de las reivindicaciones 1 a 3, en donde la matriz contiene entre el 10 y el 80 por ciento en peso de PEG de bajo peso molecular, y entre el 10 y el 80 por ciento en peso de PEG de alto peso molecular. Reivindicacion 5: Una composicion de acuerdo con cualquiera de las reivindicaciones 1 a 4 la cual además contiene del 0.01 por ciento al 2.0 por ciento de un antioxidante seleccionado a partir de los siguientes excipientes: hidroxi-toIueno butilado (BHT), hidroxi-anisol butilado (BHA), alfa-tocoferol, ácido ascorbico, o una mezcla de los mismos, de preferencia hidroxi-tolueno butilado (BHT). Reivindicacion 7: Una composicion de acuerdo con cualquiera de las reivindicaciones 1 a 6 la cual además comprende uno o más excipientes seleccionados a partir del grupo que consiste en antioxidantes, agentes gelificantes, agentes de ajuste/reguladores del pH, agentes para modificar la consistencia, conservadores, (co-) solventes, rellenos, aglutinantes, desintegrantes, acondicionadores de flujo, lubricantes, fragancias, estabilizantes, agentes humectantes, emulsionantes, solubilizantes, y sales para regular la presion osmotica. Reivindicacion 8: Una composicion de acuerdo con cualquiera de las reivindicaciones 1 a 7, la cual no contiene un potenciador de la penetracion en cantidades de cuando menos el 2.5 por ciento en peso. Reivindicacion 14: Una composicion de acuerdo con cualquiera de las reivindicaciones 1 a 13, para el tratamiento de, o para utilizarse en el tratamiento de, i) una enfermedad o condicion dermatologica, ii) una enfermedad, condicion o dano de la retina, o iii) dermatología cosmética, en particular soriasis, dermatitis atopica, dermatitis alérgica por contacto, o rosácea. Reivindicacion 19: Un compuesto de la reivindicacion 18, en la forma de un solvato, en particular el hemi-hidrato. Reivindicacion 20: Un compuesto de la reivindicacion 19, en la forma de un hemi-hidrato caracterizado ya sea por los picos de difraccion en polvo de rayos-X picos a 7.4, 9.9, 14.9 y 15.8° 2-Teta para la forma del Cristal A, o valores 2-Teta de 12.3, 16.6 y 16.9 en el caso de la forma del Cristal B.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US22326909P | 2009-07-06 | 2009-07-06 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR077549A1 true AR077549A1 (es) | 2011-09-07 |
Family
ID=42686504
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100102394A AR077549A1 (es) | 2009-07-06 | 2010-07-05 | Una composicion farmaceutica topica para regular el factor de crecimiento endotelial vegf que comprende la (3-trifluoro-metil-fenil)-amida del acido 6-(6-hidroxi-metil-pirimidin-4-iloxi)-naftalen-1-carboxilico. |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US20110112121A1 (es) |
| EP (1) | EP2451458A2 (es) |
| JP (1) | JP2012532183A (es) |
| KR (1) | KR20120041745A (es) |
| CN (1) | CN102470134A (es) |
| AR (1) | AR077549A1 (es) |
| AU (1) | AU2010270361A1 (es) |
| BR (1) | BR112012000383A2 (es) |
| CA (1) | CA2767440A1 (es) |
| CO (1) | CO6480987A2 (es) |
| EA (1) | EA201200095A1 (es) |
| EC (1) | ECSP12011578A (es) |
| IL (1) | IL217329A0 (es) |
| MA (1) | MA33417B1 (es) |
| MX (1) | MX2012000391A (es) |
| SG (1) | SG176955A1 (es) |
| TN (1) | TN2011000653A1 (es) |
| TW (1) | TW201113258A (es) |
| WO (1) | WO2011003858A2 (es) |
| ZA (1) | ZA201200079B (es) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5520824B2 (ja) | 2007-08-17 | 2014-06-11 | ノバルティス アーゲー | 環状デプシペプチド類 |
| AR086168A1 (es) | 2011-04-20 | 2013-11-27 | Novartis Ag | Procesos para la elaboracion de depsipeptidos macrociclicos e intermediarios |
| US8680054B2 (en) * | 2011-04-20 | 2014-03-25 | Novartis Ag | Suspension type topical formulations comprising cyclic depsipeptide |
| US9067978B2 (en) | 2012-10-09 | 2015-06-30 | Novartis Ag | Solution phase processes for the manufacture of macrocyclic depsipeptides and new intermediates |
| US8987413B2 (en) | 2012-10-09 | 2015-03-24 | Novartis Ag | Aldehyde acetal based processes for the manufacture of macrocyclic depsipeptides and new intermediates |
| CN104860885B (zh) * | 2014-02-24 | 2017-11-17 | 中国科学院上海药物研究所 | 萘酰胺类化合物、其制备方法和用途 |
| SE1751461A1 (en) * | 2017-11-28 | 2019-05-29 | Ascilion Ab | Method of detecting an exogenous agent in interstitial fluid |
| WO2019126270A1 (en) * | 2017-12-20 | 2019-06-27 | Sienna Biopharmaceuticals, Inc. | Formulations for dermal delivery of polymer conjugates of indolocarbazole compounds with reduced exposure |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6355657B1 (en) * | 1998-12-30 | 2002-03-12 | Atrix Laboratories, Inc. | System for percutaneous delivery of opioid analgesics |
| US6833349B2 (en) * | 1999-06-08 | 2004-12-21 | Regeneron Pharmaceuticals, Inc. | Methods of treating inflammatory skin diseases |
| EP1330452B1 (en) * | 2000-09-20 | 2008-11-26 | Ortho-McNeil Pharmaceutical, Inc. | Pyrazine derivatives as modulators of tyrosine kinases |
| EP1415987B1 (en) * | 2000-10-20 | 2007-02-28 | Eisai R&D Management Co., Ltd. | Nitrogenous aromatic ring compounds as anti cancer agents |
| AU2003209116A1 (en) * | 2002-02-11 | 2003-09-04 | Bayer Pharmaceuticals Corporation | Aryl ureas with angiogenesis inhibiting activity |
| US20040266688A1 (en) * | 2003-05-14 | 2004-12-30 | Nayak Nihar R | Methods for modulating endometrium |
| CN1933839A (zh) * | 2004-01-23 | 2007-03-21 | 安进公司 | 化合物和使用方法 |
| PE20060664A1 (es) | 2004-09-15 | 2006-08-04 | Novartis Ag | Amidas biciclicas como inhibidores de cinasa |
| GB0518671D0 (en) * | 2005-09-13 | 2005-10-19 | Novartis Ag | Organic compounds |
| GT200600411A (es) * | 2005-09-13 | 2007-05-21 | Novartis Ag | Combinaciones que comprenden un inhibidor del receptor del factor de crecimiento endotelial vascular |
| KR101487027B1 (ko) * | 2005-09-30 | 2015-01-28 | 미카나 테라퓨틱스, 인크. | 치환된 피라졸 화합물 |
| GB0604937D0 (en) * | 2006-03-10 | 2006-04-19 | Novartis Ag | Organic compounds |
| WO2008031835A2 (en) * | 2006-09-13 | 2008-03-20 | Novartis Ag | Method of treating autoimmune diseases using vegf-pathway inhibitors |
-
2010
- 2010-06-30 US US12/827,218 patent/US20110112121A1/en not_active Abandoned
- 2010-07-05 MX MX2012000391A patent/MX2012000391A/es unknown
- 2010-07-05 JP JP2012518944A patent/JP2012532183A/ja active Pending
- 2010-07-05 WO PCT/EP2010/059553 patent/WO2011003858A2/en active Application Filing
- 2010-07-05 CA CA2767440A patent/CA2767440A1/en not_active Abandoned
- 2010-07-05 SG SG2011095205A patent/SG176955A1/en unknown
- 2010-07-05 AR ARP100102394A patent/AR077549A1/es not_active Application Discontinuation
- 2010-07-05 CN CN2010800305461A patent/CN102470134A/zh active Pending
- 2010-07-05 BR BR112012000383A patent/BR112012000383A2/pt not_active Application Discontinuation
- 2010-07-05 MA MA34518A patent/MA33417B1/fr unknown
- 2010-07-05 EA EA201200095A patent/EA201200095A1/ru unknown
- 2010-07-05 EP EP10734715A patent/EP2451458A2/en not_active Withdrawn
- 2010-07-05 KR KR1020127003043A patent/KR20120041745A/ko not_active Application Discontinuation
- 2010-07-05 AU AU2010270361A patent/AU2010270361A1/en not_active Abandoned
- 2010-07-05 TW TW099122023A patent/TW201113258A/zh unknown
-
2011
- 2011-12-20 TN TNP2011000653A patent/TN2011000653A1/en unknown
- 2011-12-30 CO CO11181737A patent/CO6480987A2/es not_active Application Discontinuation
-
2012
- 2012-01-02 IL IL217329A patent/IL217329A0/en unknown
- 2012-01-05 ZA ZA2012/00079A patent/ZA201200079B/en unknown
- 2012-01-06 EC EC2012011578A patent/ECSP12011578A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| ECSP12011578A (es) | 2012-02-29 |
| IL217329A0 (en) | 2012-02-29 |
| EP2451458A2 (en) | 2012-05-16 |
| EA201200095A1 (ru) | 2012-08-30 |
| MX2012000391A (es) | 2012-02-28 |
| AU2010270361A1 (en) | 2012-01-19 |
| BR112012000383A2 (pt) | 2016-03-29 |
| MA33417B1 (fr) | 2012-07-03 |
| CN102470134A (zh) | 2012-05-23 |
| WO2011003858A3 (en) | 2011-03-03 |
| CO6480987A2 (es) | 2012-07-16 |
| WO2011003858A2 (en) | 2011-01-13 |
| KR20120041745A (ko) | 2012-05-02 |
| US20110112121A1 (en) | 2011-05-12 |
| CA2767440A1 (en) | 2011-01-13 |
| JP2012532183A (ja) | 2012-12-13 |
| TW201113258A (en) | 2011-04-16 |
| SG176955A1 (en) | 2012-01-30 |
| ZA201200079B (en) | 2012-09-26 |
| TN2011000653A1 (en) | 2013-05-24 |
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| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |