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1. (WO1999039712) SUBSTITUTED SEMICARBAZIDES AND THE USE THEREOF
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/1999/039712    International Application No.:    PCT/US1999/002419
Publication Date: 12.08.1999 International Filing Date: 04.02.1999
Chapter 2 Demand Filed:    07.09.1999    
IPC:
C07C 281/06 (2006.01)
Applicants: EURO-CELTIQUE S.A. [BE/BE]; 122 Boulevard de la Petrusse L-2330 Luxembourg (BE) (For All Designated States Except US).
CAI, Sui, X. [CN/US]; (US) (For US Only).
LAN, Nancy, C. [US/US]; (US) (For US Only).
HONG-BAE, Soo [US/US]; (US) (For US Only)
Inventors: CAI, Sui, X.; (US).
LAN, Nancy, C.; (US).
HONG-BAE, Soo; (US)
Agent: ESMOND, Robert, W.; Sterne, Kessler, Goldstein & Fox P.L.L.C. Suite 600 1100 New York Avenue, N.W. Washington, DC 20005-3934 (US)
Priority Data:
60/073,710 04.02.1998 US
Title (EN) SUBSTITUTED SEMICARBAZIDES AND THE USE THEREOF
(FR) SEMICARBAZIDES SUBSTITUES ET LEUR UTILISATION
Abstract: front page image
(EN)This invention is related to substituted semicarbazides represented by Formula (I) or a pharmaceutically acceptable salt or prodrug thereof, wherein: R¿1? and R¿2? are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; R¿3?, R¿4?, R¿5? and R¿6? are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl, or R¿3? and R¿4? is defined as above, and R¿5? and R¿6? together with the nitrogen atom to which they are attached form a heterocycle, including piperidine, piperazine, morpholine; A¿1? and A¿2? are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or satured or partially unsaturated heterocycle, any of which is optionally substituted; X is one of O, S, NR¿7?, CH¿2?, C(O), NR¿7?C(O), C(O)NR¿7?, SO, SO¿2? or a covalent bond; where R¿7? is hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; n is 0, 1, 2 or 3. m is 0, 1, 2 or 3. The invention also is directed to the use of substituted semicarbazides for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as anticonvulsants, and as antimanic depressants, as anti-migraine agents, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.
(FR)L'invention concerne des semicarbazides substitués représentés par la formule (I), un sel pharmaceutiquement acceptable ou un promédicament de ceux-ci. Dans cette formule, R¿1? et R¿2? représentent chacun indépendamment hydrogène, alkyle, cycloalkyle, alcényle, alcynyle, haloalkyle, aryle, aminoalkyle, hydroxyalkyle, alcoxyalkyle ou carboxyalkyle; R¿3?, R¿4?, R¿5? et R¿6? sont indépendamment hydrogène, alkyle, cycloalkyle, alcényle, alcynyle, haloalkyle, aryle, aminoalkyle, hydroxyalkyle, alcoxyalkyle ou carboxyalkyle; ou R¿3? et R¿4? sont définis comme susmentionnés, et R¿5? et R¿6? forment ensemble avec l'atome d'azote auquel ils sont attachés un hétérocycle comprenant pipéridine, pipérazine, morpholine; A¿1? et A¿2? représentent indépendamment aryle, hétéroaryle, cyclocarbone saturé ou partiellement non saturé ou hétérocycle saturé ou partiellement non saturé, l'un quelconque étant éventuellement substitué. X représente l'un de O, S, NR¿7?, CH¿2?, C(O), NR¿7?C(O), C(O)NR¿7?, SO, SO¿2? ou une liaison covalente; où R¿7? est hydrogène, alkyle, cycloalkyle, alcényle, alcynyle, haloalkyle, aryle, aminoalkyle, hydroxyalkyle, alcoxyalkyle ou carboxyalkyle; n est 0, 1, 2 ou 3. m est 0, 1, 2 ou 3. L'invention concerne également l'utilisation des semicarbazides substitués pour traiter les lésions neuronales consécutives à une ischémie globale ou focale, pour traiter ou prévenir des états neurodégénératifs tels que la sclérose latérale amyotrophique (ALS), pour traiter, prévenir ou améliorer une douleur chronique ou aiguë et pour traiter ou prévenir la neuropathie diabétique. Ces semicarbazides sont notamment des anesthésiques locaux, des dépresseurs anti-maniaco-dépressifs, des médicaments antimigraineux, des anesthésiques locaux, des antiarythmiques.
Designated States: AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, CA, CH, CN, CU, CZ, DE, DK, 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, MD, MG, MK, MN, MW, MX, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, TJ, TM, TR, TT, UA, UG, US, UZ, VN, YU, ZW.
African Regional Intellectual Property Organization (GH, GM, KE, LS, MW, SD, SZ, UG, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (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)