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1. WO2000039077 - THYROID RECEPTOR LIGANDS

Publication Number WO/2000/039077
Publication Date 06.07.2000
International Application No. PCT/IB1999/002084
International Filing Date 23.12.1999
Chapter 2 Demand Filed 22.04.2000
IPC
C07C 235/32 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
235Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
02having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
32the carbon skeleton containing six-membered aromatic rings
C07C 235/52 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
235Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
42having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
44with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
52having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
C07C 307/06 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
307Amides of sulfuric acids, i.e. compounds having singly-bound oxygen atoms of sulfate groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
04Diamides of sulfuric acids
06having nitrogen atoms of the sulfamide groups bound to acyclic carbon atoms
C07C 311/51 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
311Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
50Compounds containing any of the groups X being a hetero atom, Y being any atom
51Y being a hydrogen or a carbon atom
C07C 323/41 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
323Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
23containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
39at least one of the nitrogen atoms being part of any of the groups X being a hetero atom, Y being any atom
40Y being a hydrogen or a carbon atom
41Y being a hydrogen or an acyclic carbon atom
C07C 323/60 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
323Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
50containing thio groups and carboxyl groups bound to the same carbon skeleton
51having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
60with the carbon atom of at least one of the carboxyl groups bound to nitrogen atoms
CPC
A61P 17/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
A61P 17/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
02for treating wounds, ulcers, burns, scars, keloids, or the like
A61P 17/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
04Antipruritics
A61P 17/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
06Antipsoriatics
A61P 19/10
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19Drugs for skeletal disorders
08for bone diseases, e.g. rachitism, Paget's disease
10for osteoporosis
C07C 235/32
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
235Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
02having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
32the carbon skeleton containing six-membered aromatic rings
Applicants
  • KARO BIO AB [SE/SE]; Novum S-141 57 Huddinge, SE (AllExceptUS)
  • BRISTOL-MYERS SQUIBB COMPANY [US/US]; P.O. Box 4000 Princeton, NJ 08543-4000, US (AllExceptUS)
  • HANGELAND, Jon [US/US]; US (UsOnly)
  • ZHANG, Minsheng [CN/US]; US (UsOnly)
  • CARINGAL, Yolanda [US/US]; US (UsOnly)
  • RYONO, Denis [US/US]; US (UsOnly)
  • LI, Yi-Lin [CN/SE]; SE (UsOnly)
  • MALM, Johan [SE/SE]; SE (UsOnly)
  • LIU, Ye [CN/SE]; SE (UsOnly)
  • GARG, Neeraj [IN/SE]; SE (UsOnly)
  • LITTEN, Chris [IN/SE]; SE (UsOnly)
  • GARCIA COLLAZO, Ana Maria [ES/SE]; SE (UsOnly)
  • KOEHLER, Konrad [US/SE]; SE (UsOnly)
Inventors
  • HANGELAND, Jon; US
  • ZHANG, Minsheng; US
  • CARINGAL, Yolanda; US
  • RYONO, Denis; US
  • LI, Yi-Lin; SE
  • MALM, Johan; SE
  • LIU, Ye; SE
  • GARG, Neeraj; SE
  • LITTEN, Chris; SE
  • GARCIA COLLAZO, Ana Maria; SE
  • KOEHLER, Konrad; SE
Agents
  • BANNERMAN, David, Gardner; Withers & Rogers Goldings House 2 Hays Lane London SE1 2HW, GB
Priority Data
9828442.524.12.1998GB
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) THYROID RECEPTOR LIGANDS
(FR) NOUVEAUX LIGANDS DE RECEPTEURS THYROIDIENS ET PROCEDE II
Abstract
(EN)
New thyroid receptor ligands are provided which have general formula (I) in which: n is an integer from 0 to 4; R1 is halogen, trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7 carbons; R2 and R3 are the same or different and are hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 5 carbons, at least one of R2 and R3 being other than hydrogen; R4 is a carboxylic acid amide (CONR'R'') or an acylsulphonamide (CONHSO2R') derivative, or a pharmaceutically acceptable salt thereof, and all stereoisomers thereof; or when n is equal to or greater than one, R4 may be a heteroaromatic moiety which may be substituted or unsubstituted, or an amine (NR'R''). R5 is hydrogen or an acyl (such as acetyl or benzoyl) or other group capable of bioconversion to generate the free phenol structure (wherein R5=H). In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount. Examples of such diseases associated with metabolism dysfunction or are dependent upon the expression of a T3 regulated gene include obesity, hypercholesterolemia, atherosclerosis, cardiac arrhythmias, depression, osteoporosis, hypothyroidism, goiter, thyroid cancer as well as glaucoma, congestive heart failure and skin disorders.
(FR)
L'invention concerne de nouveaux ligands de récepteurs thyroïdiens. Ces ligands sont représentés par la formule générale (I) dans laquelle n représente une nombre entier compris entre 0 et 4; R1 représente l'halogène, le trifluorométhyle, ou un alkyle comprenant de 1 à 6 atomes de carbones ou un cycloalkyle comprenant de 3 à 7 atomes de carbone; R2 et R3 sont semblables ou différents et représentent l'hydrogène, l'halogène, un alkyle comprenant de 1 à 4 atomes de carbone ou un cycloalkyle comprenant de 3 à 5 atomes de carbone, et R2 et/ou R3 est/sont autres que l'hydrogène; R4 représente un amide acide carboxylique (CONR'R'') ou un dérivé d'acylsulfonamide (CONHSO2R'), ou un sel pharmaceutiquement acceptable, ainsi que tous les stéréoisomères ceux-ci ou, lorsque n est égal ou plus grand que un, R4 peut être un groupe hétéroaromatique substitué ou non substitué, ou une amine (NR'R''). R5 représente l'hydrogène ou un acyle (par exemple l'acétyle ou le benzoyle) ou un autre groupe capable d'une bioconversion permettant de produire la structure phénol libre (R5 représentant H). L'invention concerne en outre une méthode permettant de prévenir, d'inhiber, ou de traiter une maladie associée à un dysfonctionnement métabolique ou une maladie dépendant de l'expression d'un gène régulé par T3. Cette méthode consiste à administrer à raison d'une dose thérapeutiquement efficace un composant du type décrit. Ces maladies associées à un dysfonctionnement métabolique ou dépendantes de l'expression d'un gène régulé par T3 comprennent par exemple l'obésité, l'hypercholestérolémie, l'athérosclérose, les arythmies cardiaques, la dépression, l'ostéoporose, l'hypothyroïdie, le goitre, le cancer de la thyroïde ainsi que le glaucome, l'insuffisance cardiaque globale et des affections cutanées.
Also published as
CZPV2001-2204
ININ/PCT/2001/754/KOL
NO20012931
NZ512422
TR2001/01834
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