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1. (WO2007008942) PHENYLAMINO-ACETIC ACID [1-(PYRIDIN-4-YL)-METHYLIDENE]-HYDRAZIDE DERIVATIVES AND RELATED COMPOUNDS AS MODULATORS OF G PROTEIN-COUPLED RECEPTOR KINASES FOR THE TREATMENT OF EYE DISEASES
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2007/008942    International Application No.:    PCT/US2006/026976
Publication Date: 18.01.2007 International Filing Date: 11.07.2006
IPC:
C07D 213/61 (2006.01), C07D 213/36 (2006.01), C07D 215/42 (2006.01), C07D 233/88 (2006.01), C07D 333/36 (2006.01), C07D 307/52 (2006.01), C07D 239/54 (2006.01), C07C 251/86 (2006.01), A61K 31/44 (2006.01), A61K 31/47 (2006.01), A61K 31/4164 (2006.01), A61K 31/381 (2006.01), A61K 31/341 (2006.01), A61K 31/513 (2006.01), A61P 27/02 (2006.01)
Applicants: AERIE PHARMACEUTICALS, INC. [US/US]; 7020 Kit Creek Road, Suite 270, P.O. Box 12320, Research Triangle Park, NC 27709 (US) (For All Designated States Except US).
DELONG, Mitchell, A. [US/US]; (US) (For US Only).
SZNAIDMAN, Marcos, L. [US/US]; (US) (For US Only).
OAKLEY, Robert, H. [US/US]; (US) (For US Only).
ECKHARDT, Allen, E. [US/US]; (US) (For US Only).
HUDSON, Christine [US/US]; (US) (For US Only).
YINGLING, Jeffrey, D. [US/US]; (US) (For US Only).
PEEL, Michael [GB/US]; (US) (For US Only).
RICHARDSON, Thomas, E. [US/US]; (US) (For US Only).
MURRAY, Claire, Louise [GB/US]; (US) (For US Only).
RAO, Byappanahally, N. Narasinga [IN/US]; (US) (For US Only).
HEASLEY, Brian, H. [US/US]; (US) (For US Only).
PATEL, Paresma, R. [US/US]; (US) (For US Only)
Inventors: DELONG, Mitchell, A.; (US).
SZNAIDMAN, Marcos, L.; (US).
OAKLEY, Robert, H.; (US).
ECKHARDT, Allen, E.; (US).
HUDSON, Christine; (US).
YINGLING, Jeffrey, D.; (US).
PEEL, Michael; (US).
RICHARDSON, Thomas, E.; (US).
MURRAY, Claire, Louise; (US).
RAO, Byappanahally, N. Narasinga; (US).
HEASLEY, Brian, H.; (US).
PATEL, Paresma, R.; (US)
Agent: HARTWIG, Gregory, J.; Michael Best & Friedrich LLP, 100 East Wisconsin Avenue, Suite 3300, Milwaukee, WI 53202-4108 (US)
Priority Data:
60/698,190 11.07.2005 US
Title (EN) PHENYLAMINO-ACETIC ACID [1-(PYRIDIN-4-YL)-METHYLIDENE]-HYDRAZIDE DERIVATIVES AND RELATED COMPOUNDS AS MODULATORS OF G PROTEIN-COUPLED RECEPTOR KINASES FOR THE TREATMENT OF EYE DISEASES
(FR) DERIVES DE [1-(PYRIDIN-4-YL)-METHYLIDENE]-HYDRAZIDE D'ACIDE PHENYLAMINO-ACETIQUE ET COMPOSES ASSOCIES EN TANT QUE MODULATEURS DES KINASES DU RECEPTEUR COUPLE A LA PROTEINE G POUR LE TRAITEMENT DE TROUBLES OCULAIRES
Abstract: front page image
(EN)Hydrazide compounds with GPCR desensitization inhibitory activity are provided that may be used to influence, inhibit or reduce the action of a G-protein receptor kinase. Pharmaceutical compositions including therapeutically effective amounts of the hydrazide compounds and pharmaceutically acceptable carriers are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions controlled or influenced by GPCRs are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions such as cancer osteoporosis and glaucoma are also provided. (Formula (I)). A is selected from a heteroaryl group (i): wherein X1, X2, X3 and X4 are, independently, CH, O, S or N-R6, with the proviso that at least one of X2 or X3 is O, S or N-R6; and a heteroaryl group (ii): wherein X5 and X9 are CH or C-halogen, X6 and X8 are CH, and X7 is N, and wherein the six-membered heteroaryl group may be further fused with an unsubstituted six-member aryl group; R1, R2, R3, R4, and R5 are, independently, hydrogen; halogen; C1-C4 alkyl; amino; nitro; cyano; heteroaryl; carboxy, carbonylamino; aminosulfonyl; sulfonylamino; aminoacyl; thioalkyl; sulfonyl; acyl; heterocycle; -OR; -O-C1-C4alkyl-heterocycle; -C(O)NH-C1-C4alkyl-heterocycle; -C(O)NH-heteroaryl; -C(O)NH-aryl; or carboxylamino; wherein R is C1-C4 alkyl; aryl, heteroaryl, C1-C4 alkyl aryl or C1-C4 alkyl heteroaryl; R6 is H or C1-C4 alkyl; R7 is hydrogen, C1-C4 alkyl or C1-C4 alkoxy; and X is N-R6.
(FR)La présente invention concerne des composés d'hydrazide ayant une activité d'inhibition de désensibilisation de GPCR et pouvant être utilisés pour agir sur, inhiber ou réduire l'action de la kinase de récepteur de protéine G. L'invention a également pour objet des compositions pharmaceutiques comprenant des quantités efficaces d'un point de vue thérapeutique des composés d'hydrazide et des excipients acceptables d'un point de vue pharmaceutique. L'invention concerne aussi différents procédés faisant intervenir les composés et/ou les compositions, pour agir sur des maladies ou des états pathologiques contrôlés ou influencés par GPCR, ainsi que différents procédés faisant intervenir les composés et/ou les compositions pour agir sur des maladies ou des états pathologiques tels que le cancer, l'ostéoporose et le glaucome. Dans la formule (I) : A est choisi entre un groupe hétéroaryle (i) dans lequel X1, X2, X3 et X4 sont indépendamment CH, O, S ou N-R6, à la condition que X2 et/ou X3 soit/soient O, S ou N-R6, et un groupe hétéroaryle (ii) dans lequel X5 et X9 sont CH ou C-halogène, X6 et X8 sont CH, et X7 est N, et le groupe hétéroaryle à six éléments peut également être fusionné à un groupe aryle à six éléments non substitué ; R1, R2, R3, R4, et R5 sont indépendamment hydrogène; halogène; alkyle en C1-C4; amino; nitro; cyano; hétéroaryle carboxy, carbonylamino; aminosulfonyle; sulfonylamino; aminoacyle; thioalkyle; sulfonyle; acyle; hétérocycle; -OR; -O-C1-C4alkyl-hétérocycle; -C(O)NH-C1-C4alkyl-hétérocycle; -C(O)NH-hétéroaryle; -C(O)NH-aryle; ou carboxylamino, où R est alkyle en C1-C4; aryle, hétéroaryle, alkylaryle en C1-C4 ou alkylhétéroaryle en C1-C4; R6 est H ou alkyle en C1-C4; R7 est hydrogène, alkyle en C1-C4 ou alcoxy C1-C4; et X est N-R6.
Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LV, LY, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW.
African Regional Intellectual Property Organization (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, HU, IE, IS, IT, LT, LU, LV, MC, NL, PL, PT, RO, SE, SI, SK, 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)