baber/WOPTO huggingface dataset:
Patent AT-E270665-T1 (AT)
Inventor: BRENNER MICHAEL
IPC: A61K31/40
Filed: 1999-04-14
Granted: 2004-07-15
Abstract: The invention relates to new diphenyl-substituted 5-ring heterocycles of general formula (I)wherein A, X and the groups R1, R2, R3, R4 and R5 are defined as in the claims, processes for preparing them and their use as pharmaceutical compositions.
Patent AT-E231933-T1 (AT)
Inventor: SZAMEITAT KLAUS
IPC: C25D3/04
Filed: 1999-06-24
Granted: 2003-02-15
Abstract: The present invention relates to a galvanic bath, to a process for the precipitation of chromium onto objects, and to the use of the process for the generation of textured hard-chrome layers on machine components. The galvanic bath contains in aqueous solution at least one compound delivering chromium(VI)-ions, and it comprises a) chromium(VI)-ions in an amount that corresponds to 100 to 600 g/ltr of chromic acid anhydride, b) sulfate ions in the form of sulfuric acid and/or of a soluble salt thereof in a molar concentration ratio of chromium(VI)-ions to sulfate ions (SO4-2) ranging from 90:1 to 120:1, and c) 2-hydroxyethane sulfonate ions in an amount that corresponds to 0.01 to 3.0 g/ltr of the sodium salt.
Patent AT-E390707-T1 (AT)
Inventor: EASON ROBERT WILLIAM
IPC: C03C15/00
Filed: 1999-07-20
Granted: 2008-04-15
Abstract: A method of selectively etching a substrate ( 1 ) comprises applying etchant ( 4 ) at a surface of the substrate and illuminating an area of the surface with light from a light source ( 7 ), whereby etching is at least partially inhibited in the illuminated area ( 18 ) of the substrate. Preferably LiNbO3 is patterned in HF KOH, or HF-HNO3 solutions by selective illumination using UV laser light with 300 to 1000 mn wavelength, thereby allowing for interferometric or holographic structures to be formed.
Patent AT-E221022-T1 (AT)
Inventor: GRAFFAGNINO ROBERTO
IPC: B65H5/28
Filed: 1999-09-10
Granted: 2002-08-15
Abstract: Apparatus (1, 1') for the collection, distribution and storage of flexible laminar elements, in particular of industrial hides (P) during various phases of their production, including a first support unit (2) and a second hide handling unit (3), adapted to be operatively supported by the first unit (2), the first and second units being provided with releasable connecting elements (7, 8, 9, 10) to allow their transfer both jointly and separately, the second unit including two rotating cylinders (18, 21) with substantially parallel axes, and flexible conveying device (22) for loading, unloading and stocking hides (P), said conveying device being provided with two extremity portions each respectively fixed to one of the cylinders.
Patent AT-E441675-T1 (AT)
Inventor: BORVE KJETIL
IPC: C08F8/00
Filed: 1999-06-18
Granted: 2009-09-15
Abstract: A process for the branching and foaming of a polypropylene resin, being performed continuously in an extruder, comprising: (i) mixing the polypropylene resin with a peroxide selected from the group comprising the structures represented by: R>1<-O-O-C(O)-C=C-C(O)-O-O-R>2<, R>3<-R>5<-O-C(O)-O-O-C(O)-O-R>6<-R>4<, wherein each R>1< and R>2< represents linear or branched alkyl groups having 1-15 carbon atoms, each R>3< and R>4< represents linear or branched alkyl groups having 4-30 carbon atoms, and each R>5< and R>6< represents cyclic or linear aliphatic groups having 6 carbon atoms, (ii) heating the constituents to a temperature higher than the melting temperature of the polypropylene resin and the decomposition temperature of the peroxide while being mixed and conveyed forward, (iii) keeping the polymer melt at said temperature for a period of 3 to 100 times the half-life of the peroxide at said temperature, (iv) introducing a foaming agent, optionally also a bubble initiator, into the polymer melt inside the extruder at a position where the branching is substantially complete, (v) extruding the processed polymer melt through an extrusion die into ambient atmosphere, whereupon the polymer composition expands. The obtained polymer resins may be used in manufacturing articles by pipe extrusion, thermoforming and blow molding. Branched polypropylene resins not being subjected to foaming may be used as such in manufacturing articles by injection molding, extrusion, thermoforming, blow molding, calandering and fibre spinning.
Patent AT-E218212-T1 (AT)
Inventor: NIEBAUER DANIEL A
IPC: G02B1/10
Filed: 1999-09-02
Granted: 2002-06-15
Abstract: An improved partial reflector is disclosed in which the reflector is configured to provide selected levels of reflectance, transmittance and efficiency that are substantially uniform over the visible wavelength range of 400 to 700 nanometers. This result is achieved using a special three-layer coating that includes a metal layer sandwiched between two metal oxide dielectric layers having relatively high refractive indices >2.0. Advantageously, the three layers all incorporate the same metal, preferably niobium.
Patent AT-E268712-T1 (AT)
Inventor: COTTARD ANDRE
IPC: B62K27/00
Filed: 1999-10-29
Granted: 2004-06-15
Abstract: The invention concerns a single-wheel trailer for all-terrain touring bike. The trailer is fixed on the saddle rod via hitch linkage (3) comprising a fixing part (9a,9b) on the saddle extended by a plate (11) from which projects a vertical shaft (13) whereon is articulated a fork joint (15) interlocked with a rod (16) of the trailer body.
Patent AT-E233780-T1 (AT)
Inventor: BERENS ULRICH
IPC: C07D295/18
Filed: 1999-11-03
Granted: 2003-03-15
Abstract: An enantiomerically enriched compound of formula (4)or the opposite enantiomer thereof, wherein R is C1-10 alkyl. This compound, in the form of a transition metal complex, is useful as a catalyst for stereoselective hydrogenation.
Patent AT-E250465-T1 (AT)
Inventor: BOUGAMONT JEAN-LOUIS
IPC: B65D83/76
Filed: 1999-11-26
Granted: 2003-10-15
Abstract: A device for connecting the body (C) of a pump (P) to a flexible bag (S) containing a liquid or semi-liquid fluid, the device being characterized in that it comprises a cylindrical sleeve (10) for leakproof fixing of the bag (S), which sleeve is connected at the top to a shoulder (11) carrying firstly a peripheral ring (13) for assembly with the wall of a rigid outer container (B) and secondly a central bushing (12) for leakproof support of the pump (P).
Patent AT-E281571-T1 (AT)
Inventor: HARDER SVEN
IPC: E04B1/64
Filed: 1999-12-21
Granted: 2004-11-15
Abstract: The present invention relates to a water vapour barrier (15) that comprises a first, water impervious membrane (19) having a plurality of first through openings (21) defined therein, and a second, water impervious membrane (22) which is arranged opposite to the first membrane (19). A water absorbing material (18) is arranged within one or more spaces defined between the first and second membranes (19, 22), and the water vapour barrier (15) is characterised in that at least part of the second membrane (22) is of a material of the type having a water vapour diffusion resistance, which varies in dependency of the relative humidity of air in contact therewith, such that the vapour diffusion resistance is reduced when the relative humidity increases, and vice versa. The invention further relates to a method of making the water vapour barrier.
Patent AT-E369415-T1 (AT)
Inventor: SHAMAYELI KHALIL
IPC: C11D1/04
Filed: 1999-12-04
Granted: 2007-08-15
Abstract: The invention relates to a pasty washing agent for use in commercial laundering which contains a non-ionic surfactant, an organic and/or inorganic builder, a bleaching agent based on peroxygen, and optionally contains other common constituents. The inventive pasty washing agent is characterized in that it contains 30 wt. % to 60 wt. % of non-ionic surfactant, 0.5 wt. % to 5 wt. % of a fatty acid and/or fatty acid alkaline-salt, 5 wt. % to 15 wt. % of citrate and/or citric acid and 15 wt. % to 35 wt. % of an inorganic peroxygen compound. In addition, the pasty washing agent does not contain alkali metasilicate nor a bleach activator. In addition to exhibiting a good cleaning efficiency, the inventive agent has a disinfecting action.
Patent AT-E354658-T1 (AT)
Inventor: CONTRERAS ROLAND H
IPC: G01N33/50
Filed: 1999-12-06
Granted: 2007-03-15
Abstract: The present invention is concerned with the identification of genes or functional fragments thereof from Candida albicans which are critical for growth and cell division and which genes may be used as selective drug targets to treat Candida albicans associated infections. Novel nucleic acid sequences from Candida albicans are also provided and which encode the polypeptides which are critical for growth of Candida albicans. Methods for the identification of anti-fungal compounds which inhibit fungal or yeast growth are also contemplated.
Patent DE-14792521-T1 (DE)
Title: Verpackungsschachtel, zuschnitt, verfahren und vorrichtung zur formung davon
Inventor: VISTRÖM MAGNUS
IPC: B65D5/20
Filed: 2014-10-31
Abstract: Verpackungsbox umfassend: einen Bodenabschnitt, der eine erste Ebene definiert; und mindestens einen ersten Seitenwandabschnitt, der in einem Winkel zu dem Bodenabschnitt angeordnet ist, wobei der erste Seitenwandabschnitt mit dem Bodenabschnitt über eine Falzlinie an einer ersten Kante des Bodenabschnitts verbunden ist, der erste Seitenwandabschnitt ein Paar von Verlängerungsabschnitten aufweist, die sich von gegenüberliegenden Kanten des Seitenwandabschnitts erstrecken, so dass mindestens Teil eines Paars zweiter Seitenwandabschnitte, die in einem Winkel zu dem Bodenabschnitt und in einem Winkel zu dem ersten Seitenwandabschnitt angeordnet sind, bereitgestellt ist, jeder Seitenwandabschnitt des zweiten Paars von Seitenwandabschnitten mindestens Teil eines der sich von dem ersten Seitenwandabschnitt erstreckenden Paare von Verlängerungsabschnitten umfasst, ein Verbindungsabschnitt jedes Verlängerungsabschnitts, der den ersten Seitenwandabschnitt mit einem der beiden Seitenwandabschnitte verbindet, gleichförmig gekrümmt ist; mindestens ein Seitenlaschenabschnitt, der in einem Winkel zu dem Bodenabschnitt angeordnet ist und mit dem Bodenabschnitt über eine Falzlinie an einer Kante des Bodenabschnitts derart verbunden ist, dass der Seitenlaschenabschnitt an einer Oberfläche des jeweiligen Verlängerungsabschnitts des ersten Seitenwandabschnitts anliegt; und mindestens einen Deckelabschnitt, wobei der mindestens eine Deckelabschnitt mit dem Seitenlaschenabschnitt über eine Falzlinie verbunden ist und sich in einem Winkel zu dem jeweiligen Seitenwandabschnitt erstreckt, um die Verpackungsbox mindestens teilweise zu schließen.
Patent DE-263723-T1 (DE)
IPC: C04B28/22
Filed: 1987-11-27
Abstract: In a process for the manufacture of green shaped articles having a density of at least 1000 kg/m<3> and a matrix of a cured inorganic binder said articles are prepared by dewatering an aqueous slurry of fibres and a matrix forming material comprising particles of an inorganic hydraulic binder, particulate inorganic additive and possibly other additives containing an excess of water in relation to the amount necessary to secure curing of the hydraulic binder, and containing, on a dry weight basis, 3-20%, preferably 5-20%, in particular 7-15%, cellulose fibres, after which the green shaped articles are cured. The matrix forming material comprises, on a dry weight basis,   40-90%, preferably 45-85%, of a coarse material with an average particle size of 35-12  mu m, preferably 25-18  mu m, preferably with a particle size distribution exhibiting only one maximum, comprising the hydraulic binder and possibly a silica- or silicate-containing, preferably pozzolanic active additive,   5-45%, preferably 10-40%, in particular 10-35%, of a fine inorganic, preferably silica- or silicate-containing, in particular pozzolanic active additiv                       e with an average particle size of 10-1  mu m, preferably 7-3  mu m, preferably with a particle size distribution cxhibiting only one maximum,   3-25% of an ultra fine preferably pozzolanic active additive with an average particle size within the range 1-0.02  mu m, preferably less than 0.5  mu m, and   0-30% other additives.
Patent DE-637274-T1 (DE)
Inventor: SATRAN AMIR
IPC: B23C5/20
Filed: 1994-02-18
Abstract: PCT No. PCT/EP94/00474 Sec. 371 Date Dec. 8, 1994 Sec. 102(e) Date Dec. 8, 1994 PCT Filed Feb. 18, 1994 PCT Pub. No. WO94/19133 PCT Pub. Date Sep. 1, 1994A cutting insert for with a rotary milling cutting tool is disclosed. The insert has a cutting edge defined between a cutting rake surface and a relief flank and a base edge defined between the relief flank and a base surface. The cutting edge comprises a plurality of successive component cutting edges and intermediate edges located between successive component cutting edges. Each component cutting edge has a leading end and a trailing end, and is downwardly inclined from its leading end towards the base edge. Each leading end, other than that belonging to a first leading component cutting edge, is connected to an immediately preceding trailing end via an intermediate edge which rises from the preceding trailing end away from the base edge.
Patent ES-2032370-T1 (ES)
Title: Cerradura para sistemas de cinturon de seguridad en vehiculos.
IPC: A44B11/25
Filed: 1990-12-11
Abstract: EL CIERRE PARA UN CINTURON DE SEGURIDAD PARA VEHICULOS, PROVISTO CON UN DISPOSITIVO QUE SE APRIETA HACIA ATRAS, ENGRANABLE A ESTE CIERRE, ESTA PROVISTO DE UNA MASA COMPENSADORA (42) QUE IMPIDE EN EL EXTREMO DE ELEVACION DEL APRIETE, UN MOVIMIENTO CONDICIONADO POR INERCIA DE LAS MASAS DE LA TECLA DE DESBLOQUEO (28), EN DIRECCION AL ACCIONAMIENTO. LA MASA COMPENSADORA ESTA FORMADA A TRAVES DE UNA PALANCA GIRATORIA SITUADA EN LA CAJA, QUE MUESTRA UN ELEMENTO DE ENGRANAJE (44) QUE ESTA DE FORMA PERMANENTE EN UN ENGRANE DE PEINE JUNTO CON UN LISTON DENTADO (40) DE LA TECLA DE DESBLOQUEO. CON CADA ACCIONAMIENTO DE LA TECLA DE DESBLOQUEO, LA PALANCA (42) GIRARA, POR LO CUAL SE GARANTIZARA SU MARCHA FACIL, AUN DESPUES DE UNA LARGA DURACION DE USO.
Patent CY-1113090-T1 (CY)
Title: Διαταξη για την εξισορροπηση κρουσεων πιεσης σε κλειστα συστηματα, οπως σιλο ή παρομοια
Inventor: THORWESTEN ALBERT
IPC: B65D90/22
Filed: 2012-09-05
Abstract: Με μια διάταξη (1) για την εξισορρόπηση κρούσεων πίεσης σε ενδεχόμενες εκρήξεις σκόνης ή αερίου εντός κλειστών συστημάτων, όπως σιλό, σωληνώσεις ή παρόμοια, με ένα εις ένα στόμιο εκροής ή αντίστοιχα ένα πλαίσιο (2) δυνάμενο να περιστρέφεται αρθρωτό καπάκι (3), το οποίο παρουσιάζει μία επίπεδη εξωτερική επιφάνεια (12), όπου εις το στόμιο εκροής ή αντίστοιχα το πλαίσιο (2) προβλέπεται μία πλάκα πρόσκρουσης (8) για την πρόσκρουση του καπακιού (3) στην περίπτωση έκρηξης, επιδιώκεται εκτός από μια οικονομικότερη κατασκευή, ειδικότερα μία σαφής μείωση βάρους εις το αρθρωτό καπάκι, μία ταχεία αντικατάσταση του καπακιού εις την περίπτωση καταστροφής ή αντίστοιχα μία ταχεία πρώτη συναρμολόγηση και μία βελτίωση της προστατευτικής δράσης του συστήματος. Αυτό επιτυγχάνεται δια του ότι το αρθρωτό καπάκι (3) κατασκευάζεται από ένα υλικό ανθρακονημάτων/υαλονημάτων.
Patent CY-1114278-T1 (CY)
Title: Καπακι κλειστρου για υποδοχεις, ασφαλες εναντι καταποσης, ειδικοτερα υποδοχεις τροφιμων και ειδικοτερα ασκους ποτων
Inventor: SCHWARTZ ERHARD
IPC: B65D81/36
Filed: 2013-08-21
Abstract: Περιγράφεται καπάκι κλείστρου (1) για υποδοχείς, ασφαλές έναντι κατάποση, όπως παραδείγματος χάριν για ασκούς ποτού. Δια του ότι το καπάκι κλείστρου είναι διαμορφωμένο ως καπάκι με πτερύγια, το οποίο δεν είναι δυνατόν να καταποθεί από μικρά παιδιά, είναι δυνατόν να ελαχιστοποιηθεί ο κίνδυνος υγείας για μικρά παιδιά ο οποίος προέρχεται από το καπάκι κλείστρου.
Patent CY-1115580-T1 (CY)
Title: Συνθεση και αντι-ιικη δραστηριοτητα των υποκατεστημενων παραγωγων αζαϊνδολοοξικης πιπεραζινης
Inventor: WANG TAO
IPC: A61K45/06
Filed: 2014-07-31
Abstract: Αυτή η εφεύρεση παρέχει ενώσεις που έχουν ιδιότητες φαρμακευτικής και βιολογικής επίδρασης, τις φαρμακευτικές συνθέσεις και τη μέθοδο χρήσης αυτών. Ειδικότερα, η παρούσα εφεύρεση αφορά παράγωγα αζαϊνδολοοξοακετυλο πιπεραζίνης. Αυτές οι ενώσεις διαθέτουν μοναδική αντι-ιική δραστηριότητα, είτε χρησιμοποιούνται μόνες τους είτε σε συνδυασμό με άλλα αντι-ιικά, αντιλοιμωξιακά, ανοσοτροποποιητικά ή αναστολείς της εισόδου ΗIV. Ειδικότερα, η παρούσα εφεύρεση αφορά τη θεραπεία του ΗΙV και του ΑIDS.
Patent CY-1116551-T1 (CY)
Title: Ορθωτικη διαταξη και μεθοδος κατασκευης μιας ορθωτικης διαταξης
Inventor: MATTHEWS MARTIN
IPC: A61F5/02
Filed: 2015-06-11
Abstract: Μια ορθωτική διάταξη, η οποία μπορεί να είναι ιδιαίτερα αποτελεσματική στη θεραπεία της σκολίωσης, περιλαμβάνει ένα τμήμα κορμού καθώς και μια ελαστική ενίσχυση προσαρτημένη στο τμήμα κορμού. Η ενίσχυση εκτείνεται διαγωνίως έναντι ενός μπροστινού και/είτε πίσω μέρους του τμήματος του κορμού ανάμεσα σε ένα πρώτο σημείο προσάρτησης μιας πλευράς του τμήματος κορμού και σε ένα δεύτερο σημείο προσάρτησης σε μια δεύτερη πλευρά του τμήματος του κορμού. Τουλάχιστον ένα από τα πρώτο και δεύτερο σημεία προσάρτησης έχει εισαχθεί τοπικά μέσα στο τμήμα κορμού κατά τρόπο, ώστε η ενίσχυση να επιμηκύνεται, όταν η διάταξη φορεθεί από έναν ασθενή, και ως εκ τούτου εφαρμοστεί μια δύναμη στον κορμό του ασθενούς.
Patent CY-1117039-T1 (CY)
Title: Τροποποιηση της εκφρασης toy hsp47
Inventor: JIN XIAOMEI
IPC: C07H21/00
Filed: 2015-12-11
Abstract: Παρέχονται εις το παρόν συνθέσεις, μέθοδοι και κιτ για τροποποίηση της έκφρασης γονιδίων-στόχοι, ειδικότερα δε της πρωτεΐνης θερμικού σοκ 47 (hsp47). Οι συνθέσεις, οι μέθοδοι και τα κιτ μπορεί να συμπεριλάβουν μόρια πυρηνικών οξέων (για παράδειγμα, βραχύ παρεισφρέον πυρηνικό οξύ (siNA), βραχύ παρεισφρέον RNA (siRNA), διπλά-κλωνισμένο RNA (dsRNA), μικρο-RNA (miRNA) ή βραχύ RNA φουρκέτας (shRNA)) που τροποποιούν ένα γονίδιο εγκωδικεύοντας το hsp47, για παράδειγμα, το γονίδιο εγκωδικεύοντας το hsp47 ανθρώπου. Η σύνθεση και οι μέθοδοι που αποκαλύπτονται εις το παρόν μπορεί επίσης να χρησιμοποιηθούν και στην αγωγή καταστάσεων και διαταραχών που συσχετίζονται με το hsp47 όπως είναι η ίνωση του ήπατος, η πνευμονική ίνωση, η περιτοναϊκή ίνωση και η ίνωση των νεφρών.
Patent CY-1119988-T1 (CY)
Title: Αναστολεις του ιου της ηπατιτιδας c
Inventor: BACHAND CAROL
IPC: C07D403/14
Filed: 2018-02-28
Abstract: Η παρούσα αποκάλυψη σχετίζεται με μια ένωση του Χημικού Τύπου (I), με συνθέσεις και μεθόδους για την αγωγή της λοίμωξης από τον ιό της ηπατίτιδας C (HCV). Επίσης αποκαλύπτονται και θεραπευτικές συνθέσεις που περιέχουν τέτοιες ενώσεις και μέθοδοι για χρήση αυτών των ενώσεων στην αγωγή της λοίμωξης από τον HCV.
Patent CY-1124089-T1 (CY)
Title: Μη ανθρωπινα ζωα που εχουν ενα εξανθρωπισμενο γονιδιο συμπλεγματος διαφοροποιησης 47
Inventor: GURER CAGAN
IPC: A01K67/027
Filed: 2021-05-06
Abstract: Παρέχονται μη ανθρώπινα ζώα, μέθοδοι και συνθέσεις για δημιουργία και χρήση των ιδίων, όπου τα εν λόγω μη ανθρώπινα ζώα συμβάλλουν στον εξανθρωπισμό ενός ενδογενούς γονιδίου συμπλέγματος διαφοροποίησης (CD), συγκεκριμένα στον εξανθρωπισμό ενός γονιδίου CD47. Τα εν λόγω μη ανθρώπινα ζώα μπορεί να περιγράφονται, σε μερικές υλοποιήσεις, ως έχοντα μια γενετική τροποποίηση σε ένα ενδογενές γονίδιο CD47, έτσι ώστε να εκφράζουν ένα πολυπεπτίδιο CD47, που περιλαμβάνει ένα ανθρώπινο τμήμα και ένα μη ανθρώπινο τμήμα (π.χ., ένα τμήμα ποντικού).
Patent GR-900300102-T1 (GR)
Title: Device for testing the coupling elements of trailers, in particular inclusive of their mounting means, under simulated operative load conditions
Inventor: KLOCK JURGEN DIPL-ING
IPC: G01M99/00
Filed: 1990-09-27
Abstract: The invention provides a device for testing trailer couplings which transmit a traction to a trailer by way of a trailer coupling ring on the drawbar of the trailer, the test being carried out under loading conditions similar to those occurring in practice, preferably with inclusion of the construction for fixing the trailer coupling, in particular the tail cross-member to which the trailer coupling is attached and optionally frame parts adjoining the tail cross-member. A longitudinal force generating device which produces a longitudinal force acting in the direction of traction of the connection between the trailer coupling and the trailer coupling ring and a vertical force generating device which produces a vertical force extending perpendicularly or approximately perpendicularly to the direction of action of the traction are coupled to a force transmitting connecting member to which can be attached the trailer coupling ring which is connected to the trailer coupling. The parts are coupled together in such a manner that the direction of action of the vertical force exerted on the force transmitting connecting member by the vertical force generating device and the direction of action of the longitudinal force exerted on the force transmitting connecting member by the longitudinal force generating device intersect at the point at which the trailer coupling ring is attached to the trailer coupling.
Patent HR-P20110245-T1 (HR)
Inventor: GUZI TIMOTHY J
IPC: A61P35/00
Filed: 2011-04-04
Abstract: Spoj, naznačen time što ima formulu: ili njegova farmaceutski prihvatljiva sol ili solvat. Patent sadrži još 21 patentni zahtjev.
Patent HR-P20120708-T1 (HR)
Title: Combination of anticholinergics, glucocorticoids and beta2-agonists for the treatment of inflammatory diseases
Inventor: MAUS JOACHIM
IPC: A61K45/06
Filed: 2012-09-06
Abstract: The invention relates to novel combinations based on anticholinergics, ² 2 -adrenoceptor agonists, and glucocorticoids, process for production and its use for the treatment of inflammatory diseases, preferably respiratory diseases as bronchial asthma and chronic obstructive pulmonary diseases (COPD) or rheumatic or autoimmune diseases.
Patent SI-1685829-T1 (SI)
Title: Use of (1RS,3RS,6RS)-6-dimethylaminomethyl-1-(3-methoxy-phenyl)-cyclohexane-1,3-diol for treating inflammatory pain
Inventor: SCHIENE KLAUS DR
IPC: A61K31/135
Filed: 2003-11-18
Abstract: Mixture (X) of at least one analgesic (A) and an inhibitor (B) of cyclo-oxygenase II (COXII). Mixture (X) of at least one analgesic (A) and an inhibitor (B) of cyclo-oxygenase II (COXII), where (A) is a phenyl-substituted tertiary amine of formulae (I)-(III), as racemates, pure or mixed stereoisomers (particularly enantiomers or diastereoisomers), optionally in the form of acids, bases, salts or solvates, preferably hydrates. [Image] X : hydroxy, fluoro, chloro, hydrogen or OCOR 7>; R 1>1-4C linear, branched, saturated or unsaturated alkyl, optionally substituted one or more times, in (I), or 1-4C alkyl, benzyl, trifluoromethyl, hydroxy, benzyloxy. 1-3C alkoxy, chloro or fluoro in (II); R 2> and R 3>hydrogen or 1-4C alkyl (as for R 1>) or together form an optionally substituted 4-7C cycloalkyl; R 9>-R 1> 3>hydrogen, fluoro, chloro, bromo, iodo, (di)fluoromethyl, trifluoromethyl, hydroxy, thiol, OR 1> 4>, trifluoromethoxy, SR 1> 4>, NR 1> 7>R 1> 8>, (trifluoro)methyl- sulfinyl or -sulfonyl, cyano, COOR 1> 4>, nitro, CONR 1> 7>R 1> 8>, 1-6C alkyl (as above) or phenyl, optionally substituted one or more times; R 1> 4>1-6C alkyl, pyridyl, thienyl, thiazolyl, phenyl, benzyl, phenethyl (all optionally substituted one or more times), PO(O-1-4C alkyl)-2, COO1-5C alkyl, CONH(1-3C alkylphenyl), CO(1-5C)alkyl, COCHR 1> 7>-NHR 1> 8>, or CO-phenylene-R 1> 5>; R 1> 5>ortho-OCO(1-3C)alkyl, or meta- or para-CH 2N(R 1> 6>) 2; R 1> 6>1-4C alkyl or morpholino, and all alkyl in R 1> 4>-R 1> 6> are optionally substituted one or more times; R 1> 7> and R 1> 8>hydrogen, 1-6C alkyl (as above), phenyl, benzyl or phenethyl, all optionally substituted one or more times; R 1> 0> with either of R 9> or R 1> together : a OCH 2O, OCH 2CH 2O, OCH=CH, CH=CHO, CH=CMeO, OCMe=CH, (CH 2) 4 or OCH=CHO ring; proviso: in (III), when R 9>, R 1> 1> and R 1> 3> are all hydrogen, one of R 1> 0> and R 1> 2> is hydrogen and the other methoxy, then X is nor hydroxy. ACTIVITY : Analgesic. In the mouse writhing test ( J. Pharmacol. Exp. Ther., 228 (1984) 1) animals were treated with (a) (1R,2R)-3-(3-dimethylamino-1-ethyl-2-methylpropyl)phenol (X); (b) rofecoxib (Y) or (c) a mixture of both at ratio 1:2, then after 30 minutes injected with acetic acid. The ED50 for reduction of writhing was 33 mg/kg for (X) alone and 60.1 mg/kg for (Y) alone, but only 23.3 mg/kg (compare 47 mg/kg for an additive effect) for the mixture. MECHANISM OF ACTION : None given.