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1. (WO2015044951) 3,7-DIAZABICYCLO[3.3.1 ]NONANE CARBOXAMIDES AS ANTITHROMBOTIC AGENTS
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2015/044951 International Application No.: PCT/IN2014/000458
Publication Date: 02.04.2015 International Filing Date: 09.07.2014
Chapter 2 Demand Filed: 19.05.2015
IPC:
C07D 471/08 (2006.01) ,A61K 31/439 (2006.01) ,A61P 7/02 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
471
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
02
in which the condensed system contains two hetero rings
08
Bridged systems
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
439
the ring forming part of a bridged ring system, e.g. quinuclidine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7
Drugs for disorders of the blood or the extracellular fluid
02
Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
Applicants:
COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH [IN/IN]; Anusandhan Bhawan 2 Rafi Marg New Delhi 110001, IN
Inventors:
DIKSHIT, Dinesh Kumar; IN
KARUNAKARAN SASIKALA, Anil Kumar; IN
DIKSHIT, Madhu; IN
BARTHWAL, Manoj Kumar; IN
MISRA, Ankita; IN
JAIN, Manish; IN
Agent:
NAIR, Manisha Singh; IN
Priority Data:
2892/DEL/201330.09.2013IN
Title (EN) 3,7-DIAZABICYCLO[3.3.1 ]NONANE CARBOXAMIDES AS ANTITHROMBOTIC AGENTS
(FR) CARBOXAMIDES DE 3,7-DIAZABICYCLO[3.3.1]NONANE À TITRE D'AGENTS ANTITHROMBOTIQUES
Abstract:
(EN) The present invention relates to the 3,7-diazabicyclo[3.3.1]nonane carboxamides and process for preparation thereof. The present invention further relates to the compounds of general formula (1) possessing anti-thrombotic (anti-platelet) activities. The invention also relates to use of these moieties as inhibitors of collagen induced platelet adhesion and aggregation mediated through collagen receptors both in vitro and in vivo. Further, invention also relates these class of compounds exhibiting anti-platelet efficacy through dual mechanism inhibited both collagen as well as U46619 (thromboxane receptor agonist) induced platelet aggregation. General formula (1) Wherein, R' is; wherein R is selected from alkyl, acyl, tosyl, tert-butyloxycarbonyl, araalkyl or substituted araalkyl groups; R'' is selected preferably from halogen, cyano, lower alkyl, aryl, substituted aryl, and tosyl groups; R1 is selected from hydrogen and lower alkyl groups; R2 is selected from lower alkyl and aryl groups; R3 is selected from tert-butyloxycarbonyl and bezyloxycarbonyl groups; n = 0,1.
(FR) Cette invention concerne des carboxamides de 3,7-diazabicyclo[3.3.1]nonane et leur procédé de préparation. Cette invention concerne en outre des composés de formule générale (1) possédant des activités anti-thrombotiques (anti-plaquettaires). L'utilisation de ces fragments à titre d'inhibiteurs de l'adhérence et de l'agrégation plaquettaire induite par le collagène par l'intermédiaire des récepteurs de collagène à la fois in vitro et in vivo est décrite. Cette invention concerne également les classes de composés faisant preuve d'une efficacité anti-plaquettaire par l'intermédiaire d'un double mécanisme inhibant l'agrégation plaquettaire à la fois induite par le collagène et U46619 (agoniste du récepteur de thromboxane). Formule générale (1) Dans la formule, R' est; R est choisi parmi les groupes alkyle, acyle, tosyle, tert-butyloxycarbonyle, aralkyle ou aralkyle substitué; R'' est de préférence choisi parmi un atome d'halogène, les groupes cyano, alkyle inférieur, aryle, aryle substitué, et tosyle; R1 est choisi parmi un atome d'hydrogène et les groupes alkyle inférieurs; R2 est choisi parmi les groupes alkyle inférieurs et aryle; R3 est choisi parmi les groupes tert-butyloxycarbonyle et bézyloxycarbonyle; n = 0,1.
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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, 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, IR, IS, JP, KE, KG, 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, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, 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, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (AL, 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, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)