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1. WO1991000855 - NOVEL VITAMIN D ANALOGUES

Publication Number WO/1991/000855
Publication Date 24.01.1991
International Application No. PCT/DK1990/000168
International Filing Date 04.07.1990
Chapter 2 Demand Filed 13.11.1990
IPC
C07C 401/00 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
401Irradiation products of cholesterol or its derivatives; Vitamin D derivatives, 9,10-seco cyclopentaphenanthrene or analogues obtained by chemical preparation without irradiation
C07F 9/117 2006.01
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
06without P-C bonds
08Esters of oxyacids of phosphorus
09Esters of phosphoric acids
117with cycloaliphatic alcohols
CPC
A61P 11/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
A61P 17/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
C07C 401/00
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
401Irradiation products of cholesterol or its derivatives; Vitamin D derivatives, 9,10-seco cyclopenta[a]phenanthrene or analogues obtained by chemical preparation without irradiation
C07F 9/117
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
06without P—C bonds
08Esters of oxyacids of phosphorus
09Esters of phosphoric acids
117with cycloaliphatic alcohols
Applicants
  • LEO PHARMACEUTICAL PRODUCTS LTD. A/S (LØVENS KEMISKE FABRIK PRODUKTIONSAKTIESELSKAB) [DK/DK]; Industriparken 55 DK-2750 Ballerup, DK (AllExceptUS)
  • BINDERUP, Ernst, Torndal [DK/DK]; DK (UsOnly)
  • CALVERLEY, Martin, John [GB/DK]; DK (UsOnly)
Inventors
  • BINDERUP, Ernst, Torndal; DK
  • CALVERLEY, Martin, John; DK
Agents
  • KRISTENSEN, P., Rydahl; Leo Pharmaceutical Products Industriparken 55 DK-2750 Ballerup, DK
Priority Data
8915770.510.07.1989GB
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) NOVEL VITAMIN D ANALOGUES
(FR) NOUVEAUX ANALOGUES DE LA VITAMINE D
Abstract
(EN)
The present invention relates to compounds of formula (I), in which formula n is 2 or 3, m is 0 or an integer from 1-4; R1 and R2 (which may be the same or different) stand for hydrogen or C1-C8-hydrocarbyl, hydrocarbyl indicating the residue after removal of a hydrogen atom from a straight, branched or cyclic saturated or unsaturated hydrocarbon, or taken together with the carbon bearing the hydroxyl group (starred in formula (I)), R1 and R2 can form a saturated or unsaturated C3-C8 carboxylic ring; in addition, R1 and/or R2 and/or one of the m carbons designated by the ''°'' may be optionally substituted with one or more chlorine or fluorine atom(s); and finally one of the carbons designated ''°'' may optionally be substituted by one or two C1-C2 alkyl groups(s); and derivatives of the compounds of formula (I) in which one or more hydroxy have been transformed into -O-acyl or O-glycosyl or phosphate ester groups; such masked groups being hydrolyzable $i(in vivo). The present compounds find use in both the human and veterinary practice in the treatment and prophylaxis of autoimmune diseases (including diabetes mellitus), hypertension, acne, alopecia, skin ageing, imbalance in the immune system, inflammatory diseases such as as rheumatoid arthritis and asthma as well as diseases characterized by abnormal cell differentiation and/or cell proliferation, such as e.g. psoriasis and cancer.
(FR)
L'invention concerne des composés de la formule (I). Dans cette formule, n est 2 ou 3, m est 0 ou un entier variant de 1 à 4; R1 et R2 (qui peuvent être identiques ou différents) représentent l'hydrogène ou C1-C8-hydrocarbyl, l'hydrocarbyl indiquant le résidu après enlèvement d'un atome d'hydrogène d'un hydrocarbure ramifié ou saturé ou insaturé cylique, ou pris ensemble avec le carbone portant le groupe hydroxyl (présenté dans la formule (I)), R1 et R2 peuvent former un anneau carboxylique (C3-C8 saturé; de plus, R1 et/ou R2 et/ou un des m carbones désignés par le ''°'' peut/peuvent être ou non substitués avec un ou plusieurs atomes de chlore ou de fluor; enfin, un des carbones désignés par le ''°'' peut ou non être substitué par un ou deux groupes C1-C2 alkyl; et des dérivés de composés de la formule (I) dans lesquels un ou plusieurs hydroxy ont été transformés en groupes -O-acyl ou -O-glycosyl ou d'ester de phosphate; de tels groupes étant hydrolysables $i(in vivo). Ces composés sont utilisables à la fois dans le domaine des maladies de l'homme et de l'animal, dans le traitement et la prophylaxive des maladies autoimmunitaires (y compris le diabète sucré) l'hypertension, l'acné, l'alopecie, le vieillissement cutané, le déséquilibre du système immunitaire, les maladies inflammatoires comme l'arthrite rhumatismale et l'asthme ainsi que les maladies caractérisées par une différenciation anormale des cellules et/ou une prolifération des cellules comme dans le cas du psoriasis et du cancer.
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