AR072618A1 - Formulacion farmaceutica que comprende un compuesto de receptor cb-1 como por ejemplo, el 5-(4-clorofenil)-1-(2,4-diclorofenil)-n-(cis-2,6-dimetilpiperidin-1-il)-4-metil-4,5-dihidro-1h-pirazol-3-carboxamida en una disolucion solida y/o dispersion solida - Google Patents
Formulacion farmaceutica que comprende un compuesto de receptor cb-1 como por ejemplo, el 5-(4-clorofenil)-1-(2,4-diclorofenil)-n-(cis-2,6-dimetilpiperidin-1-il)-4-metil-4,5-dihidro-1h-pirazol-3-carboxamida en una disolucion solida y/o dispersion solidaInfo
- Publication number
- AR072618A1 AR072618A1 ARP090102866A ARP090102866A AR072618A1 AR 072618 A1 AR072618 A1 AR 072618A1 AR P090102866 A ARP090102866 A AR P090102866A AR P090102866 A ARP090102866 A AR P090102866A AR 072618 A1 AR072618 A1 AR 072618A1
- Authority
- AR
- Argentina
- Prior art keywords
- carboxamide
- chlorophenyl
- cis
- solid
- mixture
- Prior art date
Links
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
- A61K9/1635—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- 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
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- 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
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
Landscapes
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Organic Chemistry (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Child & Adolescent Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
Reivindicacion 1: Dispersion solida y/o disolucion solida de uno o más principios activos seleccionados de compuestos de formula (1), (2) o (3) o mezclas de los mismos cis-rac-5-(4-clorofenil)-1-(2,4-diclorofenil)-N-(2,6-dimetilpiperidin-1-il)-4-metil-4,5-dihidro-1H-pirazol-3-carboxamida (formula 1), (4S,5S)-5-(4-clorofenil))-1-(2,4-diclorofenil)-N-(cis-2,6-dimetilpiperidin-1-iI)-4-metil-4,5-dihidro-1H-pirazol-3-carboxamida (formula 2), (4S,5S)-5-(4-clorofenil))-1-(2,4-diclorofenil)-N-(trans-2,6-dimetilpiperidin-1-iI)-4-metil-4,5-dihidro-1H-pirazol-3-carboxamida (formula3) opcionalmente en forma de uno o más de los polimorfos apropiados, en forma amorfa y/o de sales correspondientes y/o de solvatos correspondientes de los mismos, que pueden obtenerse mediante un procedimiento en el que a) el/los principio(s) activo(s) se mezcla(n) con una cantidad al menos equimolar o al menos un peso igual de al menos un vehículo, b) después de so o durante la etapa a), se calienta la mezcla hasta que se funde el vehículo en la mezcla y c) posteriormente se enfría la mezcla por debajo del punto de fusion del vehículo en la mezcla. Reivindicacion 6: Una composicion farmacéutica que comprende la disolucion solida y/o dispersion solida segun cualquiera de las reivindicaciones 1 a 5 y opcionalmente ingredientes farmacéuticos aceptables adicionales.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP08384010A EP2151234A1 (en) | 2008-07-28 | 2008-07-28 | Pharmaceutical formulation comprising a CB1-receptor compound in a solid solution and/or solid dispersion |
Publications (1)
Publication Number | Publication Date |
---|---|
AR072618A1 true AR072618A1 (es) | 2010-09-08 |
Family
ID=40158635
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP090102866A AR072618A1 (es) | 2008-07-28 | 2009-07-28 | Formulacion farmaceutica que comprende un compuesto de receptor cb-1 como por ejemplo, el 5-(4-clorofenil)-1-(2,4-diclorofenil)-n-(cis-2,6-dimetilpiperidin-1-il)-4-metil-4,5-dihidro-1h-pirazol-3-carboxamida en una disolucion solida y/o dispersion solida |
Country Status (5)
Country | Link |
---|---|
US (1) | US20110159086A1 (es) |
EP (2) | EP2151234A1 (es) |
AR (1) | AR072618A1 (es) |
TW (1) | TW201006819A (es) |
WO (1) | WO2010012437A1 (es) |
Families Citing this family (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP2108643A1 (en) * | 2008-04-10 | 2009-10-14 | Laboratorios Del. Dr. Esteve, S.A. | 4-methyl-4, 5-dihydro-1H-pyrazole-3-carboxamide useful as a cannabinoid CB1 neutral antagonist |
AU2009308665B2 (en) * | 2008-10-31 | 2015-10-22 | The University Of Mississippi | Compositions containing delta-9-THC-amino acid esters and process of preparation |
US11224659B2 (en) | 2010-10-29 | 2022-01-18 | Infirst Healthcare Limited | Solid solution compositions and use in severe pain |
US11202831B2 (en) | 2010-10-29 | 2021-12-21 | Infirst Healthcare Limited | Solid solution compositions and use in cardiovascular disease |
DE102019117870B3 (de) * | 2019-07-02 | 2020-11-26 | Lts Lohmann Therapie-Systeme Ag | Oraler Dünnfilm |
Family Cites Families (32)
Publication number | Priority date | Publication date | Assignee | Title |
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FR2613720B1 (fr) * | 1987-04-10 | 1990-01-19 | Esteve Labor Dr | Derives d'aryl-heteroaryl carbinols avec activite analgesique |
FR2692575B1 (fr) * | 1992-06-23 | 1995-06-30 | Sanofi Elf | Nouveaux derives du pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant. |
FR2742147B1 (fr) * | 1995-12-06 | 1998-02-27 | Esteve Labor Dr | Procede de separation de carbinols |
US20020156104A1 (en) * | 1997-06-13 | 2002-10-24 | Jerry L. Adams | Novel pyrazole and pyrazoline substituted compounds |
ES2130079B1 (es) * | 1997-07-10 | 2000-01-16 | Esteve Labor Dr | Resolucion de aminas |
ES2130083B1 (es) * | 1997-08-04 | 2000-01-16 | Esteve Labor Dr | Procedimiento para la obtencion de los enantiomeros de cizolirtina. |
ES2150353B1 (es) * | 1998-04-15 | 2001-07-01 | Esteve Labor Dr | Tienilazolilalcoxietanaminas, su preparacion y su aplicacion como medicamentos. |
US6291476B1 (en) * | 1999-05-12 | 2001-09-18 | Ortho-Mcneil Pharmaceutical, Inc. | Pyrazole carboxamides useful for the treatment of obesity and other disorders |
ATE346047T1 (de) * | 2000-03-23 | 2006-12-15 | Solvay Pharm Bv | 4,5-dihydro-1h-pyrazolderivate mit cb1- antagonistischer aktivität |
HUP0301628A3 (en) * | 2000-06-22 | 2007-05-29 | Pharmos Corp | Novel non-psychotropic cannabinoids |
AU2001275798A1 (en) * | 2000-08-01 | 2002-02-13 | Ono Pharmaceutical Co., Ltd. | 3,4-dihydroisoquinoline derivative compounds and drugs containing these compounds as the active ingredient |
ES2180449B1 (es) * | 2001-07-06 | 2004-01-16 | Esteve Labor Dr | Derivados de aril (o heteroaril) azolilcarbinoles para el tratamiento de la incontinencia urinaria. |
HUP0401567A3 (en) * | 2001-09-21 | 2005-06-28 | Solvay Pharm Bv | Novel 4,5-dyhydro-1h-pyrazole derivatives having cb1-antagonistic activity, their use and pharmaceutical compositions containing them |
US6509367B1 (en) * | 2001-09-22 | 2003-01-21 | Virginia Commonwealth University | Pyrazole cannabinoid agonist and antagonists |
WO2003064389A1 (fr) * | 2002-01-31 | 2003-08-07 | Ono Pharmaceutical Co., Ltd. | Composes bicycliques contenant de l'azote et medicaments contenant ces composes en tant qu'ingredient actif |
US20050137251A1 (en) * | 2002-03-18 | 2005-06-23 | Aaron Garzon | Dexanabinol and dexanabinol analogs regulate inflammation related genes |
JP4613130B2 (ja) * | 2002-08-23 | 2011-01-12 | ノバルティス バクシンズ アンド ダイアグノスティックス,インコーポレーテッド | ベンゾイミダゾールキノリノンおよびそれらの使用 |
SE0300010D0 (sv) * | 2003-01-07 | 2003-01-07 | Astrazeneca Ab | Novel Compounds |
WO2004078261A1 (en) * | 2003-03-07 | 2004-09-16 | The University Court Of The University Of Aberdeen | Cannabinoid receptor inverse agonists and neutral antagonists as therapeutic agents for the treatment of bone disorders |
PL1651612T3 (pl) * | 2003-07-22 | 2012-09-28 | Astex Therapeutics Ltd | Związki 3,4-pochodne 1h-pirazolu i ich zastosowanie jako kinazy zależne od cyklin (cdk) i modulatory kinazy syntazy glikogenu-3 (gsk-3) |
US7745476B2 (en) * | 2004-01-30 | 2010-06-29 | Solvay Pharmaceuticals B.V. | 1,3,5-trisubstituted 4,5-dihydro-1H-pyrazole derivatives having CB1-antagonistic activity |
ES2238923B1 (es) * | 2004-02-16 | 2006-11-01 | Laboratorios Del Dr. Esteve, S.A. | Nuevos derivados pirazolinicos sustituidos. |
TW200533657A (en) * | 2004-02-17 | 2005-10-16 | Esteve Labor Dr | Substituted pyrazoline compounds, their preparation and use as medicaments |
ITMI20041033A1 (it) * | 2004-05-24 | 2004-08-24 | Neuroscienze S C A R L | Composti farmaceutici |
JP4232703B2 (ja) * | 2004-07-13 | 2009-03-04 | ヤマハ株式会社 | ディジタルミキサ装置 |
WO2006044556A2 (en) * | 2004-10-14 | 2006-04-27 | Galileo Pharmaceuticals, Inc. | Dual inhibitors of lipoxygenase for treating diabetes |
BRPI0517434A (pt) * | 2004-10-25 | 2008-10-07 | Solvay Pharm Gmbh | composições farmacêuticas compreendendo antagonistas do receptor canabinóide cb1 e abridores de canal de potássio para o tratamento de diabetes mellitus do tipo i, obesidade e estados relacionados |
EP1743892A1 (en) * | 2005-07-15 | 2007-01-17 | Laboratorios del Dr. Esteve S.A. | Substituted pyrazoline compounds, their preparation and use as medicaments |
US7897589B2 (en) * | 2005-07-15 | 2011-03-01 | Laboratorios Del Dr. Esteve, S.A. | Substituted pyrazoline compounds, their preparation and use as medicaments |
EP1743890A1 (en) | 2005-07-15 | 2007-01-17 | Laboratorios Del Dr. Esteve, S.A. | 4,5-Dihydro-1H-pyrazole derivatives, their preparation and use as medicaments |
EP1757587A1 (en) * | 2005-07-15 | 2007-02-28 | Laboratorios Del Dr. Esteve, S.A. | Substituted pyrazoline compounds, their preparation and use as medicaments |
EP1946777A1 (en) * | 2007-01-16 | 2008-07-23 | Laboratorios del Dr. Esteve S.A. | Substituted pyrazoline for preventing weight gain |
-
2008
- 2008-07-28 EP EP08384010A patent/EP2151234A1/en not_active Withdrawn
-
2009
- 2009-07-27 EP EP09802452A patent/EP2317983A1/en not_active Withdrawn
- 2009-07-27 US US13/056,366 patent/US20110159086A1/en not_active Abandoned
- 2009-07-27 WO PCT/EP2009/005425 patent/WO2010012437A1/en active Application Filing
- 2009-07-28 AR ARP090102866A patent/AR072618A1/es unknown
- 2009-07-28 TW TW098125338A patent/TW201006819A/zh unknown
Also Published As
Publication number | Publication date |
---|---|
TW201006819A (en) | 2010-02-16 |
WO2010012437A1 (en) | 2010-02-04 |
US20110159086A1 (en) | 2011-06-30 |
EP2317983A1 (en) | 2011-05-11 |
EP2151234A1 (en) | 2010-02-10 |
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