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1. SK20010316 - Heterocyclic aromatic compounds possessing a phosphonate group, their use and pharmaceutical composition comprising the same

Office Slovakia
Application Number 2001000316
Application Date 03.09.1999
Publication Number 20010316
Publication Date 05.02.2002
Grant Number 286080
Grant Date 05.03.2008
Publication Kind B6
IPC
C07F 9/6558
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
FACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9Compounds containing elements of Groups 5 or 15 of the Periodic System
02Phosphorus compounds
547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
6558containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
A61K 31/675
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
66Phosphorus compounds
675having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
A61P 3/10
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
08for glucose homeostasis
10for hyperglycaemia, e.g. antidiabetics
C07F 9/655
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
FACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9Compounds containing elements of Groups 5 or 15 of the Periodic System
02Phosphorus compounds
547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
655having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms
C07F 9/6553
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
FACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9Compounds containing elements of Groups 5 or 15 of the Periodic System
02Phosphorus compounds
547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
6553having sulfur atoms, with or without selenium or tellurium atoms, as the only ring hetero atoms
C07F 9/6509
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
FACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9Compounds containing elements of Groups 5 or 15 of the Periodic System
02Phosphorus compounds
547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
645having two nitrogen atoms as the only ring hetero atoms
6509Six-membered rings
CPC
A61P 3/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
A61P 3/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
06Antihyperlipidemics
A61P 3/08
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
08for glucose homeostasis
A61P 3/10
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
08for glucose homeostasis
10for hyperglycaemia, e.g. antidiabetics
A61P 5/48
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
5Drugs for disorders of the endocrine system
48of the pancreatic hormones
A61P 9/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9Drugs for disorders of the cardiovascular system
Applicants METABASIS THERAPEUTICS, INC.
Inventors DangQun
KasibhatlaSrinivas Rao
ReddyK. Raja
ErionMark D.
ReddyM. Rami
AgarwalAtul
Agents Dagmar Cechvalova, INVENTA, Patentova a znamkova kancelaria, Palisady 50, 811 06 Bratislava,Slovenska republika
Title
(EN) Heterocyclic aromatic compounds possessing a phosphonate group, their use and pharmaceutical composition comprising the same
(SK) Heterocyklické aromatické zlúčeniny obsahujúce fosfonátovú skupinu, ich použitie a farmaceutická kompozícia obsahujúca uvedené zlúčeniny
Abstract
(EN)
The invention relates to the compounds of formulas (I) and (X), process for their preparation, their use for the manufacture of medicaments and pharmaceutical compositions comprising the same. The compounds of formulas (I) and (X) are inhibitors of fructose-1,6-bisphosphatase and therefore are suitable for preventing or treating of diabetes, glycogenosis, impaired glucose tolerance, insulin resistance, hyperglycemia, obesity, accelerated gluconeogenesis and increased hepatic glucose output.

(SK)
Opisujú sa zlúčeniny so všeobecným vzorcom (I) a (X), spôsob ich prípravy, použitie na prípravu liečiv a farmaceutické kompozície s ich obsahom. Zlúčeniny so všeobecným vzorcom (I) a (X) sú inhibítormi fruktóza-1,6-bisfosfatázy a sú vhodné na prevenciu alebo liečenie diabetu, glykogenózy, zhoršenej tolerancie na glukózu, inzulínovej rezistencie, hyperglykémie, obezity, zrýchlenej glukoneogenézy a zvýšenej produkcie hepatickej glukózy.