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1. (WO2010078247) SPHINGO-GUANIDINES AND THEIR USE AS INHIBITORS OF SPHINGOSINE KINASE
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2010/078247 International Application No.: PCT/US2009/069583
Publication Date: 08.07.2010 International Filing Date: 28.12.2009
IPC:
A01N 37/52 (2006.01) ,A61K 31/155 (2006.01)
A HUMAN NECESSITIES
01
AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
N
PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
37
Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids
52
containing groups, e.g. carboxylic acid amidines
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
13
Amines, e.g. amantadine
155
Amidines (), e.g. guanidine (H2N-C(NH)-NH2), isourea (HNC(OH)NH2), isothiourea (HNC(SH)-NH2)
Applicants:
MUSC FOUNDATION FOR RESEARCH DEVELOPMENT [US/US]; 19 Hagood Avenue, Suite 909 Charleston, SC 29425, US (AllExceptUS)
SZULC, Zdzislaw, M. [US/US]; US (UsOnly)
BIELAWSKA, Alicja [US/US]; US (UsOnly)
OBEID, Lina, M. [US/US]; US (UsOnly)
HANNUN, Yusuf, A. [US/US]; US (UsOnly)
NORRIS, James [US/US]; US (UsOnly)
XIANG, Liu [CN/US]; US (UsOnly)
Inventors:
SZULC, Zdzislaw, M.; US
BIELAWSKA, Alicja; US
OBEID, Lina, M.; US
HANNUN, Yusuf, A.; US
NORRIS, James; US
XIANG, Liu; US
Agent:
TAYLOR, Arles, A., Jr.; Jenkins Wilson, Taylor & Hunt, P.A. Suite 1200 University Tower 3100 Tower Boulevard Durham, NC 27707, US
Priority Data:
61/141,46430.12.2008US
Title (EN) SPHINGO-GUANIDINES AND THEIR USE AS INHIBITORS OF SPHINGOSINE KINASE
(FR) SPHINGO-GUANIDINES ET LEUR EMPLOI EN TANT QU'INHIBITEURS DE SPHINGOSINE KINASE
Abstract:
(EN) The presently disclosed subject matter provides compounds of the formula:(1) and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, and R8 are as defined herein. Also disclosed are methods for making the compounds of the formula as set forth hereinabove, their use in inhibiting sphingosine kinase, and their use in the treatment and/or prevention of diseases and/or conditions associated with undesirable ceramidase or sphingosine kinase activity, including, but not limited to, cancer, cancer metastasis, atherosclerosis, stenosis, inflammation, immunological disorders, asthma, atopic dermatitis, wound healing, and other proliferative diseases.
(FR) La présente invention concerne des composés de formule (1) et leurs sels de qualité pharmaceutique, où R1, R2, R3, R4, R5, R6, R7 et R8 sont tels que définis dans la présente invention. La présente invention concerne également des méthodes de fabrication des composés de la formule comme présenté ci-avant, leur emploi dans l'inhibition de la sphingosine kinase, et leur application au traitement prophylactique et/ou thérapeutique de pathologies et/ou d'états pathologiques associés à une activité indésirable de la céramidase ou de la sphingosine kinase, ce qui inclut sans y être limité les cancers, les métastases cancéreuses, l'athérosclérose, la sténose, l'inflammation, les troubles immunologiques, l'asthme, la dermatite atopique, la guérison des blessures et d'autres maladies prolifératives.
front page image
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PE, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
EP2384118US20120035268CA2748546AU2009332952