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1. (WO2010113180) ANTIPSYCHOTIC AGENTS AND STANDARDIZED ANTIPSYCHOTIC FRACTIONS FROM RAUWOLFIA TETRAPHYLLA AND PROCESS OF THEIR ISOLATION
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2010/113180    International Application No.:    PCT/IN2010/000208
Publication Date: 07.10.2010 International Filing Date: 31.03.2010
Chapter 2 Demand Filed:    21.01.2011    
IPC:
A61K 36/24 (2006.01), A61P 25/18 (2006.01)
Applicants: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH [IN/IN]; [An Indian Registered body incorporated under the Registration of Societies Act (Act XXXI of 1860)] Anusandhan Bhawan 2, Rafi Marg New Delhi 110 001 (IN) (For All Designated States Except US).
SRIVASTAVA, Santosh, Kumar [IN/IN]; (IN) (For US Only).
AGRAWAL, Ashok, Kumar [IN/IN]; (IN) (For US Only).
SINGH, Subhash, Chandra [IN/IN]; (IN) (For US Only).
KHANNA, Vinay, Kumar [IN/IN]; (IN) (For US Only).
SINGH, Janardan [IN/IN]; (IN) (For US Only).
NATH, Chandeshwar [IN/IN]; (IN) (For US Only).
GUPTA, Madan, Mohan [IN/IN]; (IN) (For US Only).
GUPTA, Shikha [IN/IN]; (IN) (For US Only).
VERMA, Ram, Kishor [IN/IN]; (IN) (For US Only).
PAL, Anirban [IN/IN]; (IN) (For US Only).
BAWANKULE, Dnyaneshwar, Umrao [IN/IN]; (IN) (For US Only).
SAIKIA, Dharmendra [IN/IN]; (IN) (For US Only).
GUPTA, Anil, Kumar [IN/IN]; (IN) (For US Only).
MAURYA, Anupam [IN/IN]; (IN) (For US Only).
KHANUJA, Suman, Preet, Singh [IN/IN]; (IN) (For US Only)
Inventors: SRIVASTAVA, Santosh, Kumar; (IN).
AGRAWAL, Ashok, Kumar; (IN).
SINGH, Subhash, Chandra; (IN).
KHANNA, Vinay, Kumar; (IN).
SINGH, Janardan; (IN).
NATH, Chandeshwar; (IN).
GUPTA, Madan, Mohan; (IN).
GUPTA, Shikha; (IN).
VERMA, Ram, Kishor; (IN).
PAL, Anirban; (IN).
BAWANKULE, Dnyaneshwar, Umrao; (IN).
SAIKIA, Dharmendra; (IN).
GUPTA, Anil, Kumar; (IN).
MAURYA, Anupam; (IN).
KHANUJA, Suman, Preet, Singh; (IN)
Agent: DHAWAN, Ramesh, Chander; LALL LAHIRI & SALHOTRA Plot N°B-28, Sector 32 Institutional Area, Gurgaon 122 001 Haryana (IN)
Priority Data:
658/DEL/2009 31.03.2009 IN
Title (EN) ANTIPSYCHOTIC AGENTS AND STANDARDIZED ANTIPSYCHOTIC FRACTIONS FROM RAUWOLFIA TETRAPHYLLA AND PROCESS OF THEIR ISOLATION
(FR) ANTIPSYCHOTIQUES ET FRACTIONS ANTIPSYCHOTIQUES NORMALISÉES PROVENANT DE RAUWOLFIA TETRAPHYLLA ET PROCÉDÉ POUR LEUR ISOLEMENT
Abstract: front page image
(EN)The present invention relates to bioactive extracts its fractions and isolation of compound from Rauwolfia tetraphylla. The extracts and fractions are useful for the treatment of psychosis based on in-vivo validation on animal model and proportional binding affinities for dopaminergic - D2, Cholinergic (muscarinic) and Serotonergic (5HT2A) receptors for antipsychotic activity. The present invention relates to novel antipsychotic activity in the leaf alkaloids of Formula 1 and 2 named tetrahydroalstonine, 10-methoxytetrahydroalstonine, isoreserpiline, 10- derαethoxyreserpiline, 11-demethoxyreserpiline, reserpiline and α -yohimbine. The present invention also relates to processes for obtaining antipsychotic extracts as well as for the isolation of alkaloids of formula 1 and 2 from the leaves of Rauwolfia tetraphylla. The present invention particularly relates to significant antipsychotic activity in the MeOH extract, ethylacetate and chloroform fractions of R. tetraphylla and in the isolated compounds α -yohimbine, reserpiline and in a mixture 10- demethoxyreserpiline and 11-demethoxyreserpiline in 1:1.5 ratios for treating psychosis without any extra pyramidal symptoms (EPS).►1. R1=R2 = OMe R3 = α-H (Isoreserpiline) ► 2. R1=R2 = OMe R3 = β-H (Reserpiline) "3. R1 = OMe R2 = HR3 = β-H (11-Demethoxy reserpiline) "4. R1 = H R2 = OMe R3 = β-H (10-Demethoxy reserpiline) "5. R1 = R2 = H R3 = α -H (Tetrahydroalstonine) * 7. R1 = OMe R2 = H R3 = α -H (10-Methoxytetrahudroalstonine).
(FR)La présente invention concerne des extraits bioactifs, leurs fractions et l'isolement d'un composé provenant de Rauwolfia tetraphylla. Les extraits et fractions se révèlent utiles pour le traitement d'une psychose fondé sur la validation in vivo dans un modèle animal et sur les affinités de liaison proportionnelles des récepteurs dopaminergiques - D2, cholinergiques (muscariniques) et sérotoninergiques (5HT2A) conduisant à une activité antipsychotique. La présente invention concerne une activité antipsychotique originale dans des alcaloïdes foliaires représentés par les formules 1 et 2, dénommés tétrahydroalstonine, 10-méthoxytétrahydroalstonine, isoreserpiline, 10-déméthoxyreserpiline, 11-déméthoxyreserpiline, reserpiline et α-yohimbine. La présente invention concerne également des procédés permettant d'obtenir des extraits antipsychotiques ainsi que l'isolement d'alcaloïdes représentés par les formules 1 et 2 à partir des feuilles de Rauwolfia tetraphylla. La présente invention concerne particulièrement l'activité antipsychotique significative dans l'extrait au méthanol (MeOH), les fractions acétate d'éthyle et chloroforme de R. tetraphylla et dans les composés isolés d'α-yohimbine, de reserpiline ainsi que dans un mélange de 10-déméthoxyreserpiline et de 11-déméthoxyreserpiline dans le rapport 1:1,5, en vue du traitement d'une psychose sans survenue d'aucun symptôme extrapyramidal (EPS).►1. R1=R2 = OMe R3 = α-H (isoreserpiline) ► 2. R1=R2 = OMe R3 = β-H (reserpiline) "3. R1 = OMe R2 = HR3 = β-H (11-déméthoxyreserpiline) "4. R1 = H R2 = OMe R3 = β-H (10-déméthoxyreserpiline) "5. R1 = R2 = H R3 = α -H (tétrahydroalstonine) *7. R1 = OMe R2 = H R3 = α -H (10-méthoxytétrahydroalstonine)
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 (BW, GH, GM, KE, LR, 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)