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1. (WO2001032178) USE OF 3,4-SUBSTITUTED PIPERIDINES
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2001/032178 International Application No.: PCT/DK2000/000595
Publication Date: 10.05.2001 International Filing Date: 26.10.2000
Chapter 2 Demand Filed: 23.05.2001
IPC:
A61K 31/451 (2006.01) ,A61K 31/4525 (2006.01) ,A61K 31/4535 (2006.01) ,A61K 31/46 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
445
Non-condensed piperidines, e.g. piperocaine
451
having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
445
Non-condensed piperidines, e.g. piperocaine
4523
containing further heterocyclic ring systems
4525
containing a five-membered ring with oxygen as a ring hetero atom
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
445
Non-condensed piperidines, e.g. piperocaine
4523
containing further heterocyclic ring systems
4535
containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
46
8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
Applicants:
THOMSEN, Christian [DK/DK]; DK (UsOnly)
HOHLWEG, Rolf [DE/DK]; DK (UsOnly)
NOVO NORDISK A/S [DK/DK]; Health Care Patents Novo Allé DK-2880 Bagsvaerd, DK (AllExceptUS)
Inventors:
THOMSEN, Christian; DK
HOHLWEG, Rolf; DK
Priority Data:
PA 1999 0155329.10.1999DK
PA 1999 0155429.10.1999DK
PA 1999 0155529.10.1999DK
PA 1999 0155629.10.1999DK
PA 1999 0155729.10.1999DK
PA 1999 0155829.10.1999DK
PA 2000 0015931.01.2000DK
Title (EN) USE OF 3,4-SUBSTITUTED PIPERIDINES
(FR) UTILISATION DE PIPERIDINES 3,4-SUBSTITUEES
Abstract:
(EN) The present invention relates to the use of compounds of the general formula (I) wherein R1 represents hydrogen, a straight or branched C1-8-alkyl or C3-7-cycloalkyl group; and R2 and R3 independently represent hydrogen, alkyl, alkynyl, alkoxy, trifluoroalkyl, hydroxy, halogen, methylthio, cyano, or aralkyloxy; and R4 and R5 independently represent hydrogen, alkyl, C3-7-cycloalkyl, alkynyl, alkoxy, trifluoroalkyl, hydroxy, halogen, methylthio, cyano, acylamino, methylsulfonyl, methylenedioxy, aryloxy or aralkyloxy, or R4 and R5 together represent a methylenedioxy group; and Ar independently represents a phenyl, tetrahydronaphthyl or thienyl group; or a pharmaceutically acceptable salt thereof for the preparation of a pharmaceutical preparation for the : treatment, prevention, alleviation or amelioration of conditions in which there is alteration of blood pressure, hypotension, excessive vasodilation or migraine; treatment, prevention, alleviation or amelioration of memory and attention deficits resulting from but not limited to Alzheimer's disease, Parkinson's disease, trauma and stroke; treatment, prevention, alleviation or amelioration of painful conditions such as acute pain, chronic pain, arthritic pain or migraine; treatment, prevention, alleviation or amelioration of conditions in which there is excessive dopamine such as Schizophrenia, Parkinson's disease and depression; treatment, prevention, alleviation or amelioration of conditions in which there is symptoms of addictive drug withdrawal, including alcoholism; treatment, prevention, alleviation or amelioration of metabolic disorders such as hyperglycaemia, dyslipidemia, Type 1 diabetes, Type 2 diabetes, hypertriglyceridemia, syndrome X, insulin resistance, IGT or obesity. The present invention also embraces pharmaceutical compositions comprising these compounds and methods of using the compounds and their pharmaceutical compositions.
(FR) La présente invention concerne l'utilisation de composés de formule (I). Dans la formule, R1 représente hydrogène, un alkyle C1-8 linéaire ou ramifié ou un groupe cycloalkyle C3-7; et R2 et R3 représentent indépendamment hydrogène, alkyle, alcynyle, alcoxy, trifluoroalkyle, hydroxy, halogène, méthylthio, cyano, ou aralkyloxy; et R4 et R5 représentent indépendamment hydrogène, alkyle, cycloalkyle C3-7, alcynyle, alcoxy, trifluoroalkyle, hydroxy, halogène, méthylthio, cyano, acylamino, méthylsulfonyle, méthylènedioxy, aryloxy ou aralkyloxy, ou R4 et R5 représentent ensemble un groupe méthylènedioxy; et Ar représente indépendamment un groupe phényle, tétrahydronaphtyle ou thiényle. Ces composés ou un de leurs sels pharmaceutiquement acceptables sont utiles pour préparer une formulation pharmaceutique permettant de: traiter, prévenir, soulager ou améliorer des états dans lesquels il existe une altération de la pression sanguine, de l'hypotension, une vasodilatation excessive ou de la migraine ; traiter, prévenir, soulager ou améliorer les pertes de la mémoire et de l'attention liées entre autres à la maladie d'Alzheimer, à la maladie de Parkinson, aux traumatismes et aux accidents cérébrovasculaires ; traiter, prévenir, soulager ou améliorer les états douloureux tels que la douleur aiguë, la douleur chronique, la douleur arthritique ou la migraine ; traiter, prévenir, soulager ou améliorer des états dans lesquels on retrouve une quantité excessive de dopamine tels que la schizophrénie, la maladie de Parkinson et la dépression; traiter, prévenir, soulager ou améliorer des états associés à des symptômes de sevrage d'une drogue toxicomanogène, y compris l'alcoolisme; traiter, prévenir, soulager ou améliorer des troubles du métabolisme tels que l'hyperglycémie, la dyslipidémie, le diabète de Type 1, le diabète de Type 2, l'hypertriglycéridémie, le syndrome X, la résistance à l'insuline, la tolérance diminuée au glucose ou l'obésité. La présente invention concerne également des compositions pharmaceutiques comprenant ces composés et des procédés d'utilisation de ces mêmes composés et des compositions pharmaceutiques les contenant.
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Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, BZ, CA, CH, CN, CR, CU, CZ, DE, DK, DM, DZ, EE, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, MZ, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, TJ, TM, TR, TT, TZ, UA, UG, US, UZ, VN, YU, ZA, ZW
African Regional Intellectual Property Organization (ARIPO) (GH, GM, KE, LS, MW, MZ, SD, SL, SZ, TZ, UG, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (EPO) (AT, BE, CH, CY, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GW, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)