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1. NZ510308 - Novel heteroaromatic inhibitors of Fructose 1,6-bisphosphatase

Office New Zealand
Application Number 510308
Application Date 03.09.1999
Publication Number 510308
Publication Date 27.06.2003
Grant Number
Grant Date 06.10.2003
Publication Kind B
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 Dang, Qun
Kasibhatla, Srinivas Rao
Reddy, K Raja
Erion, Mark D
Reddy, M Rami
Agarwal, Atul
Agents AJ PARK
Priority Data 98 111077 07.12.1998 US
98 135504 09.09.1998 US
Title
(EN) Novel heteroaromatic inhibitors of Fructose 1,6-bisphosphatase
Abstract
(EN)
Patent 510308 A heteroaromatic derivative or pharmaceutically acceptable salts thereof has the formula (I) R5-X-P(=O)(YR1)2 wherein: R5 is a group of formula (2); each G is independently selected from C, N, O, S, and Se, and wherein no more than one G is O, S, or Se, and at most one G is N; each G' is independently selected from C and N and wherein no more than two G' groups are N; X is a optionally substituted linking group that links R5 to the phosphorus atom via 2-4 atoms, wherein 0-1 atoms are heteroatoms selected from N, O, and S, and the remaining atoms are carbon, except that if X is urea or carbamate there are 2 heteroatoms, measured by the shortest path between R5 and the phosphorus atom, and wherein the atom attached to the phosphorus is a carbon atom, and wherein there is no N in the linking group unless it is connected directly to a carbonyl or in the ring of a heterocycle; and wherein X is not a 2 carbon atom -alkyl- or -alkenyl- group; with the proviso that X is not substituted with -COOR2, -SO3R1, or ���PO3(R1)2; Y is independently -O- or -NR6- and when Y is -O-, then R1 attached to -O- is independently -H, alkyl, optionally substituted aryl, alicyclic or -alkylaryl, -C(R2)2-OC(O)N(R2)2, -N(R2)2-C(O)-R3, -C(R2)2-OC(O)R3, -C(R2)2-O-C(O)OR3, -C(R2)2OC(O)SR3, alkyl-S-C(O)R3, -alkyl-S-S-alkylhydroxy, or -alkyl-S-S-S-alkylhydroxy and the cyclic moiety contains a carbonate or thiocarbonate, when Y is -NR6-, then R1 attached to ���NR6- is independently -H, -[C(R2)2]q-COOR3, -C(R4)2COOR3, -[C(R2)2]q-C(O)SR3 or cycloalkylene-COOR3 or when either Y is independently -O- or -NR6-, then together R1 and R1 are -alkyl-S-S-alkyl- to form a cyclic group, or together R1 and R1 are a group of formula (3) and A, B, D, J, E, q, p, R6, R2, R3, R4, V, Z, W, and W' is as defined in the specification limited by the listed provisos...