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1. (WO2019000504) PHOSPHODIESTERASE INHIBITOR TYPE 5 (PDE 5), AND PREPARATION METHOD AND APPLICATION THEREOF
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Pub. No.: WO/2019/000504 International Application No.: PCT/CN2017/093149
Publication Date: 03.01.2019 International Filing Date: 17.07.2017
IPC:
C07D 471/04 (2006.01) ,A61K 31/506 (2006.01) ,A61K 31/444 (2006.01) ,A61P 15/10 (2006.01) ,A61P 9/12 (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
04
Ortho-condensed 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
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
506
not condensed and containing further heterocyclic rings
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
44
Non-condensed pyridines; Hydrogenated derivatives thereof
4427
containing further heterocyclic ring systems
444
containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
15
Drugs for genital or sexual disorders; Contraceptives
10
for impotence
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9
Drugs for disorders of the cardiovascular system
12
Antihypertensives
Applicants:
山东大学 SHANDONG UNIVERSITY [CN/CN]; 中国山东省济南市 历下区文化西路44号 No.44, Wenhua West Road, Lixia District Jinan, Shandong 250101, CN
Inventors:
娄红祥 LOU, Hongxiang; CN
郑泓波 ZHENG, Hongbo; CN
孙斌 SUN, Bin; CN
李琳 LI, Lin; CN
高云 GAO, Yun; CN
Agent:
济南圣达知识产权代理有限公司 JINAN SHENGDA INTELLECTUAL PROPERTY AGENCY CO., LTD.; 中国山东省济南市 历下区经十路17703号华特广场B308 Room 308, Block B, Huate Square No.17703, Jingshi Road, Lixia District Jinan, Shandong 250061, CN
Priority Data:
201710501409.527.06.2017CN
Title (EN) PHOSPHODIESTERASE INHIBITOR TYPE 5 (PDE 5), AND PREPARATION METHOD AND APPLICATION THEREOF
(FR) INHIBITEUR DE LA PHOSPHODIESTÉRASE DE TYPE 5 (PDE 5), PROCÉDÉ DE PRÉPARATION ET APPLICATION ASSOCIÉS
(ZH) 5型磷酸二酯酶抑制剂及其制备方法和用途
Abstract:
(EN) Provided are a PDE 5 and a preparation method therefor, and application of the PDE 5 to preparation of drugs used for treating, alleviating or preventing PDE 5-related diseases or disease states of mammals. The structural formula of the compound is I or II. The preparation method for the compound is simple in process and mild in reaction conditions and utilizes cheap and easily available raw materials; the prepared PDE 5 has the advantages of a definite target, high security and outstanding active effect and shows good application prospects in preparation of drugs used for treating PDE 5-related diseases, especially Male Erectile Dysfunction (MED) or Pulmonary Hypertension (PAH).
(FR) L'invention concerne une PDE 5 et un procédé de préparation associé, ainsi que l'application de la PDE 5 à la préparation de médicaments utilisés pour traiter, soulager ou prévenir les maladies ou états pathologiques associés à la PDE 5 chez les mammifères. La formule structurale du composé est représentée par la formule I ou II. Le procédé de préparation du composé est simple à mettre en oeuvre et présente des conditions de réaction modérées et utilise des matières premières bon marché et facilement disponibles; la PDE 5 préparée présente les avantages d'une cible définie, une sécurité élevée et d'un effet actif remarquable et présente de bonnes perspectives d'application dans la préparation de médicaments utilisés pour traiter des maladies liées à la PDE 5, en particulier le dysfonctionnement érectile (DE) ou l'hypertension pulmonaire (HP).
(ZH) 提供了一种5型磷酸二酯酶抑制剂、其制备方法及在用于制备治疗、缓解或预防哺乳动物与PDE5相关的疾病或疾病状态的药物中的用途。该化合物的结构式为 I 或 II 。该化合物制备方法简单,反应条件温和,原料廉价易得,制备得到抑制剂靶点明确,安全性高,活性效果突出,在制备治疗与PDE5相关的疾病特别是男性勃起功能障碍(MED)或肺动脉高压(PAH)的药物中具有很好的应用前景。
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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, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, 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, ST, 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: Chinese (ZH)
Filing Language: Chinese (ZH)