IN2014DE00281A - - Google Patents

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Publication number
IN2014DE00281A
IN2014DE00281A IN281DE2014A IN2014DE00281A IN 2014DE00281 A IN2014DE00281 A IN 2014DE00281A IN 281DE2014 A IN281DE2014 A IN 281DE2014A IN 2014DE00281 A IN2014DE00281 A IN 2014DE00281A
Authority
IN
India
Prior art keywords
compounds
pdes
screened
vivo efficacy
better
Prior art date
Application number
Inventor
Sanghapal Damodhar Sawant
Lakshma Reddy Ginnereddy
Srinivas Mahesuni
Sajad Hussain Syed
Mohd Ishaq Dar
Amit Nargotra
Priya Mahajan
Ram Asrey Vishwakarma
Original Assignee
Council Scient Ind Res
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Council Scient Ind Res filed Critical Council Scient Ind Res
Priority to EP14824549.1A priority Critical patent/EP3099689B1/en
Priority to PCT/IN2014/000662 priority patent/WO2015114647A1/en
Priority to US15/115,573 priority patent/US10017511B2/en
Priority to IN281DE2014 priority patent/IN2014DE00281A/en
Publication of IN2014DE00281A publication Critical patent/IN2014DE00281A/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The present invention relates to Pyrazolopyrimidinone compounds as PDE5 inhibitors with better lC5O value, good in vivo efficacy and PK profile and a process for the preparation thereof., The present invention covers the pyrazolo pyrimidinone based compounds that have been designed, synthesized and screened for PDES inhibitory activity and its PDES inhibitory potential is provided in this invention. These designer compounds have shown nanomolar potency when screened for PDES inhibitory activity and also shown better in vivo efficacy. These compounds can be used in the treatment of male erectile dysfunction or in treating impotence.
IN281DE2014 2014-01-30 2014-10-20 IN2014DE00281A (en)

Priority Applications (4)

Application Number Priority Date Filing Date Title
EP14824549.1A EP3099689B1 (en) 2014-01-30 2014-10-20 Pyrazolopyrimidinones for the treatment of impotence and process for the preparation thereof
PCT/IN2014/000662 WO2015114647A1 (en) 2014-01-30 2014-10-20 Pyrazolopyrimidinones for the treatment of impotence and process for the preparation thereof
US15/115,573 US10017511B2 (en) 2014-01-30 2014-10-20 Pyrazolopyrimidinones for the treatment of impotence and process for the preparation thereof
IN281DE2014 IN2014DE00281A (en) 2014-01-30 2014-10-20

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
IN281DE2014 IN2014DE00281A (en) 2014-01-30 2014-10-20

Publications (1)

Publication Number Publication Date
IN2014DE00281A true IN2014DE00281A (en) 2015-08-07

Family

ID=52292987

Family Applications (1)

Application Number Title Priority Date Filing Date
IN281DE2014 IN2014DE00281A (en) 2014-01-30 2014-10-20

Country Status (4)

Country Link
US (1) US10017511B2 (en)
EP (1) EP3099689B1 (en)
IN (1) IN2014DE00281A (en)
WO (1) WO2015114647A1 (en)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108558890A (en) * 2018-06-28 2018-09-21 重庆康刻尔制药有限公司 A kind of silaenafil intermediate synthetic method
CN111005033B (en) * 2019-12-16 2020-10-16 浙江大学 Electro-reduction preparation method of sildenafil intermediate
CN114369064B (en) * 2022-01-10 2023-12-19 北京莱瑞森医药科技有限公司 Preparation method of sildenafil intermediate

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5958926A (en) * 1996-11-01 1999-09-28 Nitromed, Inc. Nitrosated and nitrosylated phosphodiesterase inhibitor compounds, compositions and their uses
CN1229349C (en) * 1998-04-20 2005-11-30 美国辉瑞有限公司 Pyridine-3-carboxylic acid derivative
CA2235642C (en) * 1998-05-15 2007-11-13 Torcan Chemical Ltd. Processes for preparing sildenafil
AU2004201386B2 (en) * 1998-09-04 2008-08-28 Ortho-Mcneil Pharmaceutical, Inc. 5-heterocyclyl pyrazolo[4,3-d]pyrimidin-7-ones for the treatment of male erectile dysfunction
WO2001003644A2 (en) * 1999-07-09 2001-01-18 The Picower Institute For Medical Research Pyrazolopyrimidinone derivatives conjugated to thiophene moieties or benzo [fused] 5-membered heterocycles for erectile dysfunction
IL130968A (en) * 1999-07-15 2002-12-01 Shmuel Simon Pharmaceutical composition comprising sildenafil or its analogs, useful for the treatment of tinnitus and hearing loss
WO2001087888A1 (en) 2000-05-17 2001-11-22 Sk Chemicals Co., Ltd. Pyrazolopyrimidinone derivatives, process for their preparation and their use
EP1630164A1 (en) * 2004-08-31 2006-03-01 Expotrend Company SA Pyrazolopyrimidinones as phosphodiesterase inhibitors
CN101891747B (en) * 2010-07-02 2012-04-25 张南 Compound capable of inhibiting phosphodiesterase type 5 and preparation method

Also Published As

Publication number Publication date
EP3099689A1 (en) 2016-12-07
EP3099689B1 (en) 2022-01-26
WO2015114647A1 (en) 2015-08-06
US20170066771A1 (en) 2017-03-09
US10017511B2 (en) 2018-07-10

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