AR065297A1 - Formulaciones biodisponibles de compuestos heterociclicos - Google Patents

Formulaciones biodisponibles de compuestos heterociclicos

Info

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
Application number
ARP080100581A
Other languages
English (en)
Inventor
Raul Surans
Anil Chhettry
Mahendra G Dedhiya
Suneel K Rastogi
Original Assignee
Glenmark Pharmaceuticals Sa
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Glenmark Pharmaceuticals Sa filed Critical Glenmark Pharmaceuticals Sa
Publication of AR065297A1 publication Critical patent/AR065297A1/es

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/443Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/04Heterocyclic 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)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (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)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Ophthalmology & Optometry (AREA)
  • Otolaryngology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Plural Heterocyclic Compounds (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.
ARP080100581A 2007-02-09 2008-02-11 Formulaciones biodisponibles de compuestos heterociclicos AR065297A1 (es)

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)

* Cited by examiner, † Cited by third party
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
US9067949B2 (en) 2011-01-19 2015-06-30 Albany Molecular Research, Inc. Benzofuro[3,2-c] pyridines and related analogs as serotonin sub-type 6 (5-HT6) modulators for the treatment of obesity, metabolic syndrome, cognition and schizophrenia
WO2015175502A2 (en) * 2014-05-12 2015-11-19 Palatin Technologies, Inc. Replacement therapy for natriuretic peptide deficiencies
SG10202100916PA (en) 2015-02-02 2021-02-25 Valo Early Discovery Inc 3-aryl-4-amido-bicyclic [4,5,0] hydroxamic acids as hdac inhibitors
US10183934B2 (en) 2015-02-02 2019-01-22 Forma Therapeutics, Inc. Bicyclic [4,6,0] 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
US11957669B2 (en) 2017-08-11 2024-04-16 Amorepacific Corporation Pharmaceutical composition containing (R)-N-[1-(3,5-difluoro-4-methansulfonylamino-phenyl)-ethyl]-3-(2-propyl-6-trifluoromethyl-pyridin-3-yl)-acrylamide

Family Cites Families (2)

* Cited by examiner, † Cited by third party
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
EP1620429B1 (en) * 2003-04-11 2009-04-01 Glenmark Pharmaceuticals S.A. Novel heterocyclic compounds useful for the treatment of inflammatory and allergic disorders: process for their preparation and pharmaceutical compositions containing them

Also Published As

Publication number Publication date
JP2010518114A (ja) 2010-05-27
TW200846323A (en) 2008-12-01
CL2008000424A1 (es) 2008-08-18
BRPI0806447A2 (pt) 2011-09-06
MX2009008463A (es) 2010-01-27
WO2008100800A1 (en) 2008-08-21
US20080194638A1 (en) 2008-08-14
CA2677649A1 (en) 2008-08-21

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