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1. (WO2001003644) PYRAZOLOPYRIMIDINONE DERIVATIVES CONJUGATED TO THIOPHENE MOIETIES OR BENZO [FUSED] 5-MEMBERED HETEROCYCLES FOR ERECTILE DYSFUNCTION
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2001/003644 International Application No.: PCT/US2000/018751
Publication Date: 18.01.2001 International Filing Date: 07.07.2000
Chapter 2 Demand Filed: 09.02.2001
IPC:
A61K 31/519 (2006.01) ,C07D 487/04 (2006.01)
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
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519
ortho- or peri-condensed with heterocyclic rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
487
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
Applicants: THE PICOWER INSTITUTE FOR MEDICAL RESEARCH[US/US]; 350 Community Drive New York, NY 11030, US
Inventors: ABDEL-JALIL, Raid; US
AL-ABED, Yousef; US
EL-ABADELAH, Mustafa, M.; JO
KHANFAR, Monther; DE
SABRI, Salim, S.; JO
VOELTER, Wolfgang; DE
Agent: KELBER, Steven, B.; Attn: Supervisor Patent Prosecution Services Piper Marbury Rudnick & Wolfe LLP 1200 Nineteenth Street, NW Washington, DC 20036-2412, US
Priority Data:
60/143,09909.07.1999US
60/149,38917.08.1999US
Title (EN) PYRAZOLOPYRIMIDINONE DERIVATIVES CONJUGATED TO THIOPHENE MOIETIES OR BENZO [FUSED] 5-MEMBERED HETEROCYCLES FOR ERECTILE DYSFUNCTION
(FR) DERIVES DE PYRAZOLOPYRIMIDINONE CONJUGUES A DES FRACTIONS DE THIOPHENE OU DES HETEROCYCLES A 5 ELEMENTS [FUSIONNES] A BENZO UTILISES DANS LE TRAITEMENT DE LA DYSERECTION
Abstract:
(EN) There is disclosed a genus of substituted pyrazolopyrimidinones characterized, in part, by multiply substituted thiophene moieties and, in part, a genus of substituted bicyclic heteroaryl appendages. The compounds are potent inhibitors of phosphodiesterases, particularly cyclic guanosine 3',5'-monophosphate (cGMP) phosphodiesterase (PDE) activity (aka cGMP-PDE) and are useful for a variety of cardiovascular disorders relating to vascular patency, such as erectile dysfunction. Specifically, a selected set of [benzo]-fused heterocycles includes benzofuran, benzoazole, benzo[d]isoxazole, their 2,3-dihydro analogs, and benzo-1,3-dioxole moieties.
(FR) L'invention porte sur un genre de pyrazolopyrimidinones substituées se caractérisant, en partie, par la multiplication de fractions de thiophène substituées, et en partie, sur un genre d'appendices hétéroaryle bicycliques substitués. Les composés sont de puissants inhibiteurs de phosphodiestérases, notamment de l'activité de phosphodiestérases (PDE) guanosine 3',5'-monophosphate cyclique (cGMP) (aka cGMP-PDE) et sont utilisés pour traiter divers troubles cardio-vasculaires relatifs à une perméabilité vasculaire tels que la dysérection. L'invention porte notamment sur un ensemble sélectionné d'hétérocycles fusionnés à [benzo] et comprenant benzofurane, benzoazole, benzo[d]isoxazole, sur leurs analogues 2,3-dihydro et sur des fractions benzo-1,3-dioxole.
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Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, BZ, CA, CH, CN, CR, CU, CZ, DE, DK, DM, DZ, 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, MA, MD, MG, MK, MN, MW, MX, MZ, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, TJ, TM, TR, TT, TZ, UA, UG, UZ, VN, YU, ZA, ZW
African Regional Intellectual Property Organization (ARIPO) (GH, GM, KE, LS, MW, MZ, SD, SL, SZ, TZ, UG, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (EPO) (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)