AR071995A1 - Derivados de 3,4-diaril-4,5-dihidro-1h-pirazol-1-carboxamidina sustituidos con fluor que tienen actividad antagonista cb1, procesos de preparacion y composiciones farmaceuticas que los contienen - Google Patents

Derivados de 3,4-diaril-4,5-dihidro-1h-pirazol-1-carboxamidina sustituidos con fluor que tienen actividad antagonista cb1, procesos de preparacion y composiciones farmaceuticas que los contienen

Info

Publication number
AR071995A1
AR071995A1 ARP090101988A ARP090101988A AR071995A1 AR 071995 A1 AR071995 A1 AR 071995A1 AR P090101988 A ARP090101988 A AR P090101988A AR P090101988 A ARP090101988 A AR P090101988A AR 071995 A1 AR071995 A1 AR 071995A1
Authority
AR
Argentina
Prior art keywords
compounds
formula
pharmaceutical compositions
derivatives
carboxamidine
Prior art date
Application number
ARP090101988A
Other languages
English (en)
Inventor
Vliet Bernard J Van
Josephus H M Lange
Original Assignee
Solvay Pharm Bv
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 Solvay Pharm Bv filed Critical Solvay Pharm Bv
Publication of AR071995A1 publication Critical patent/AR071995A1/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Epidemiology (AREA)
  • Communicable Diseases (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Se refiere a derivados de 3,4-diaril-4,5-dihidro-1H-pirazol-1-carboxamidina fluorados como antagonistas de receptores CB1 cannabinoides, metodos para preparar estos compuestos intermediarios utiles para la s¡ntesis de dichos compuestos, metodos para la preparacion de estos intermediarios, composiciones farmaceuticas que contienen uno o m s de estos derivados de dihidropirazol como ingrediente activo, as¡ como el uso de estas composiciones farmaceuticas para el tratamiento de obesidad y trastornos cardiovasculares relacionados con la obesidad, adiccion a drogas, deficit de cognicion, fibrosis hep tica y trastornos inflamatorios. Reivindicacion 1: Un compuesto de la formula (1) o un tautomero, estereoisomero, N-oxido o una sal farmacologicamente aceptable, de cualquiera de los anteriores, en donde: n es 1 o 2, cuando n = 1, R1 es elegido de F o CF3, en cualquiera de las posiciones 3- o 4- del anillo de piperidina, cuando n = 2, R1 es F, ambos en las posiciones 3- o 4-, o uno en la posicion 3- y el segundo en la posicion 4- o en la posicion 5-, R2 es elegido de H o alquilo C1-3, R3 es elegido de H o metilo. Reivindicacion 7: Un compuesto de formula (7) en donde R1 y n tienen los significados dados en la reivindicacion 1, siendo tales compuestos utiles en la preparacion de compuestos de la formula (1). Reivindicacion 8: Un compuesto de formula (8) en donde R1 y n tienen los significados dados en la reivindicacion 1, siendo tales compuestos utiles en la preparacion de compuestos de la formula (1).
ARP090101988A 2008-06-16 2009-06-03 Derivados de 3,4-diaril-4,5-dihidro-1h-pirazol-1-carboxamidina sustituidos con fluor que tienen actividad antagonista cb1, procesos de preparacion y composiciones farmaceuticas que los contienen AR071995A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP08158309 2008-06-16

Publications (1)

Publication Number Publication Date
AR071995A1 true AR071995A1 (es) 2010-07-28

Family

ID=39869924

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP090101988A AR071995A1 (es) 2008-06-16 2009-06-03 Derivados de 3,4-diaril-4,5-dihidro-1h-pirazol-1-carboxamidina sustituidos con fluor que tienen actividad antagonista cb1, procesos de preparacion y composiciones farmaceuticas que los contienen

Country Status (14)

Country Link
US (1) US20110172274A1 (es)
EP (1) EP2315762A2 (es)
JP (1) JP2011524351A (es)
KR (1) KR20110023887A (es)
CN (1) CN102164910A (es)
AR (1) AR071995A1 (es)
AU (1) AU2009268271A1 (es)
BR (1) BRPI0915083A2 (es)
CA (1) CA2727146A1 (es)
EA (1) EA201170034A1 (es)
IL (1) IL209403A0 (es)
MX (1) MX2010013909A (es)
TW (1) TW201008924A (es)
WO (1) WO2010003760A2 (es)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10602642B2 (en) 2013-12-11 2020-03-24 Asia Vital Components Co., Ltd. Back cover unit applied to portable device and having heat conduction function

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MXPA03009439A (es) * 2001-09-21 2004-02-12 Solvay Pharm Bv Derivados de 4,5-dihidro-1h-pirazol que tienen una potente actividad antagonistica de cb1.

Also Published As

Publication number Publication date
MX2010013909A (es) 2011-02-15
JP2011524351A (ja) 2011-09-01
EA201170034A1 (ru) 2011-08-30
AU2009268271A1 (en) 2010-01-14
CA2727146A1 (en) 2010-01-14
TW201008924A (en) 2010-03-01
KR20110023887A (ko) 2011-03-08
CN102164910A (zh) 2011-08-24
WO2010003760A3 (en) 2011-07-21
WO2010003760A2 (en) 2010-01-14
EP2315762A2 (en) 2011-05-04
BRPI0915083A2 (pt) 2015-10-27
US20110172274A1 (en) 2011-07-14
IL209403A0 (en) 2011-01-31

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