AR065297A1 - Formulaciones biodisponibles de compuestos heterociclicos - Google Patents
Formulaciones biodisponibles de compuestos heterociclicosInfo
- Publication number
- AR065297A1 AR065297A1 ARP080100581A ARP080100581A AR065297A1 AR 065297 A1 AR065297 A1 AR 065297A1 AR P080100581 A ARP080100581 A AR P080100581A AR P080100581 A ARP080100581 A AR P080100581A AR 065297 A1 AR065297 A1 AR 065297A1
- Authority
- AR
- Argentina
- Prior art keywords
- substituted
- unsubstituted
- group
- ora
- alkyl
- Prior art date
Links
- 239000000203 mixture Substances 0.000 title abstract 3
- 150000001875 compounds Chemical class 0.000 title abstract 2
- -1 -OH Chemical group 0.000 abstract 5
- 125000003118 aryl group Chemical group 0.000 abstract 5
- 125000001072 heteroaryl group Chemical group 0.000 abstract 5
- 125000000623 heterocyclic group Chemical group 0.000 abstract 5
- OKFDRAHPFKMAJH-UHFFFAOYSA-N n-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)-8-(methanesulfonamido)dibenzofuran-1-carboxamide Chemical compound C=12C3=CC(NS(=O)(=O)C)=CC=C3OC2=C(OC(F)F)C=CC=1C(=O)NC1=C(Cl)C=NC=C1Cl OKFDRAHPFKMAJH-UHFFFAOYSA-N 0.000 abstract 5
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 4
- 229950000175 oglemilast Drugs 0.000 abstract 4
- 125000003342 alkenyl group Chemical group 0.000 abstract 3
- 125000000304 alkynyl group Chemical group 0.000 abstract 3
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 3
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 3
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- 125000004415 heterocyclylalkyl group Chemical group 0.000 abstract 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 3
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 abstract 2
- 125000004122 cyclic group Chemical group 0.000 abstract 2
- 238000009472 formulation Methods 0.000 abstract 2
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 150000002391 heterocyclic compounds Chemical class 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 125000006239 protecting group Chemical group 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 229920006395 saturated elastomer Polymers 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 238000001727 in vivo Methods 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000001012 protector Effects 0.000 abstract 1
- 125000001424 substituent 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
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/443—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- 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
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/02—Nasal agents, e.g. decongestants
-
- 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
- A61P11/06—Antiasthmatics
-
- 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
- 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
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pulmonology (AREA)
- Immunology (AREA)
- Dermatology (AREA)
- Epidemiology (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Ophthalmology & Optometry (AREA)
- Urology & Nephrology (AREA)
- Otolaryngology (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicinal Preparation (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Abstract
Formulaciones farmacéuticas biodisponibles de compuestos heterocíclicos, tales como N-(3,5-dicloropirid-4-il)-4-difluorometoxi-8- metanosulfonamido-dibenzo[b,d]furan-1-carboxamida (oglemilast) y sales farmacéuticamente aceptables de estos, a procesos para su preparacion y a métodos de tratamiento que utilizan las mismas. La presente también se relaciona con formas amorfas sustancialmente puras de compuestos heterocíclicos, tales como oglemilast. Se dirige particularmente a formas de dosis orales farmacéuticas biodisponibIes que contienen oglemilast amorfo. Reivindicacion 1 Una formulacion que comprende de 0,05 aprox. a 2,5 mg aprox. de oglemilast o una sal farmacéuticamente aceptable de éste, en la cual la formulacion proporciona un perfil in vivo de plasma que comprende (i) un Cmax medio de más de 2 ng/mL aprox., (ii) un AUC0-24 medio de más de 26 ng.hr/mL aprox. y (iii) un Tmax medio de aprox. 0.25 horas o más. Reivindicacion 26: Una forma sustancialmente amorfa de un compuesto de formula (1) donde R1, R2 y R3 se seleccionan independientemente del grupo que consta de hidrogeno, alquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, alquinilo sustituido o no sustituido, cicloalquilo, sustituido o no sustituido, cicloalquilaquilo sustituido o no sustituido, cicloalquenilo sustituido o no sustituido, arilo sustituido o no sustituido, arilalquilo sustituido o no sustituido, heteroarilo sustituido o no sustituido, grupo heterocíclico sustituido o no sustituido, hetérociclilalquilo sustituido o no sustituido, heteroarilalquilo sustituido o no sustituido, nitro, -OH, ciano, formilo, acetilo, halogeno, grupos. protectores, -C(O)Ra, -C(O)ORa, -C(O)NRaRa, - S(O)qRa, S(O)qNRaRa, -NRRa, -ORa, y -SRa, o dos orto-sustituyentes R3 entre si, pueden estar unidos para formar un anillo cíclico saturado o insaturado de 3 a 7 miembros que puede incluir opcionalmente hasta dos heteroátomos que pueden ser idénticos o diferentes seleccionados de O, NRa y S; R4 es -NR5R6 donde R5 y R6 se seleccionan independientemente del grupo que consta de hidrogeno, alquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, alquinilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, cicloalquilalquilo sustituido o no sustituido, cicloalquenilo sustituido o no sustituido, arilo sustituido o no sustituido, arilalquilo sustituido o no sustituido, heteroarilo sustituido o no sustituido, anillo heterocíclico sustituido o no sustituido, heterociclilalquilo sustituido o no sustituido, heteroarilalquilo sustituido o no sustituido, nitro, -OH, ciano, halogeno, -C(O)Ra, -C(O)ORa, -C(O)NRaRa, -S(O)qRa, -S(O)qNRaRa, -C(=NRa)Ra, - C(=NRa)NRaRa, -C(=S)NRaRa, -C(=S)Ra,-N=C(RaRa)-, -NRaRa, -ORa, SRa, y grupos protectores, o R5 y R6 pueden estar unidos para formar un anillo cíclico saturado o insaturado de 3 a 7 miembros, que puede incluir opcionalmente hasta dos heteroátomos que pueden ser idénticos o diferentes, de O, NRa y S; Ar se selecciona del grupo que consta de arilo sustituido o no sustituido, arilalquilo sustituido o no sustituido, anillo heterocíclico sustituido o no sustituido y anillo heteroarilo sustituido o no sustituido; X se selecciona del grupo que consta de O, S(O)q y NRa; Y se selecciona del grupo que consta de -C(O)NR7, -NR7S(O)q, -S(O)qNR7 y -NR7C (O); cada Z es independientemente C o N; R7 se selecciona del grupo que consta de hidrogeno, alquilo sustituido o no sustituido, hidroxilo, -ORa, arilo sustituido o no sustituido, y anillo heterocíclico sustituido o no sustituido; p se elige de O y S; m representa 0-3; n representa 1-4; q representa 0, 1 o 2;y Ra se selecciona del grupo que consta de hidrogeno, alquil sustituido o no sustituido, alquenilo sustituida o no sustituida, alquinilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, cicloalquilalquilo sustituido o no sustituido, cicloalquenilo sustituido o no sustituido, arilo sustituido o no sustituido, arilalquilo sustituido o no sustituido, heteroarilo sustituido o no sustituido, anillo heterocíclico sustituido o no sustituido, heterociclilalquilo sustituido o no sustituido, heteroarilalquilo sustituido o no sustituido, nitro, -OH, ciano, formilo, acetilo, halogena, grupos protectores, -C(O)Ra, -C(O)ORa, -C(O)NRaRa, -S(O)qRa, -S(O)qNRaRa, -NaRa, -ORa, y -SRa.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US88900907P | 2007-02-09 | 2007-02-09 | |
| US89635307P | 2007-03-22 | 2007-03-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR065297A1 true AR065297A1 (es) | 2009-05-27 |
Family
ID=39686385
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP080100581A AR065297A1 (es) | 2007-02-09 | 2008-02-11 | Formulaciones biodisponibles de compuestos heterociclicos |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US20080194638A1 (es) |
| JP (1) | JP2010518114A (es) |
| AR (1) | AR065297A1 (es) |
| BR (1) | BRPI0806447A2 (es) |
| CA (1) | CA2677649A1 (es) |
| CL (1) | CL2008000424A1 (es) |
| MX (1) | MX2009008463A (es) |
| TW (1) | TW200846323A (es) |
| WO (1) | WO2008100800A1 (es) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8575186B2 (en) * | 2009-10-05 | 2013-11-05 | Albany Molecular Research, Inc. | Epiminocycloalkyl[b] indole derivatives as serotonin sub-type 6 (5-HT6) modulators and uses thereof |
| EP2668191A4 (en) | 2011-01-19 | 2014-08-20 | Albany Molecular Res Inc | BENZOFURO- [3,2-C-] PYRIDINES AND RELATED ANALOGS AS SEROTONIN-SUBTYPE-6 (5-HT6) MODULATORS FOR THE TREATMENT OF ADIPOSITAS, METABOLISM SYNDROME, COGNITION AND SCHIZOPHRENIA |
| WO2015175502A2 (en) * | 2014-05-12 | 2015-11-19 | Palatin Technologies, Inc. | Replacement therapy for natriuretic peptide deficiencies |
| TW201636329A (zh) | 2015-02-02 | 2016-10-16 | 佛瑪治療公司 | 作為ｈｄａｃ抑制劑之雙環［４，６，０］異羥肟酸 |
| CA2975605C (en) | 2015-02-02 | 2023-12-12 | Forma Therapeutics, Inc. | 3-alkyl-4-amido-bicyclic [4,5,0] hydroxamic acids as hdac inhibitors |
| CN105461728A (zh) * | 2015-12-29 | 2016-04-06 | 中山大学 | 一种4-取代胺基-6-甲氧羰基苯并呋喃并[2,3-d]嘧啶类化合物及制备方法 |
| EP3472131B1 (en) | 2016-06-17 | 2020-02-19 | Forma Therapeutics, Inc. | 2-spiro-5- and 6-hydroxamic acid indanes as hdac inhibitors |
| TWI805601B (zh) | 2017-08-11 | 2023-06-21 | 南韓商愛茉莉太平洋股份有限公司 | 醫藥組成物及抑制其形成結晶的方法 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ITMI20011338A1 (it) * | 2001-06-26 | 2002-12-26 | Farmatron Ltd | Composizioni farmaceutiche orali a rilascio immediato del principio attivo |
| ATE427308T1 (de) * | 2003-04-11 | 2009-04-15 | Glenmark Pharmaceuticals Sa | Neue heterozyklische verbindungen, die sich fur die behandlung von entzundlichen und allergischen erkrankungen eignen: verfahren zu deren herstellung und pharmazeutische zusammensetzungen,die diese enthalten |
-
2008
- 2008-02-08 US US12/028,058 patent/US20080194638A1/en not_active Abandoned
- 2008-02-08 CA CA002677649A patent/CA2677649A1/en not_active Abandoned
- 2008-02-08 MX MX2009008463A patent/MX2009008463A/es not_active Application Discontinuation
- 2008-02-08 JP JP2009549246A patent/JP2010518114A/ja not_active Withdrawn
- 2008-02-08 WO PCT/US2008/053368 patent/WO2008100800A1/en active Application Filing
- 2008-02-08 BR BRPI0806447-4A patent/BRPI0806447A2/pt not_active IP Right Cessation
- 2008-02-11 CL CL200800424A patent/CL2008000424A1/es unknown
- 2008-02-11 AR ARP080100581A patent/AR065297A1/es unknown
- 2008-02-12 TW TW097104812A patent/TW200846323A/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| TW200846323A (en) | 2008-12-01 |
| US20080194638A1 (en) | 2008-08-14 |
| JP2010518114A (ja) | 2010-05-27 |
| BRPI0806447A2 (pt) | 2011-09-06 |
| CL2008000424A1 (es) | 2008-08-18 |
| MX2009008463A (es) | 2010-01-27 |
| CA2677649A1 (en) | 2008-08-21 |
| WO2008100800A1 (en) | 2008-08-21 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |