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EP1444234A2 - Deuterierte pyrazolopyrimidinone sowie diese verbindungen enthaltende arzneimittel - Google Patents

Deuterierte pyrazolopyrimidinone sowie diese verbindungen enthaltende arzneimittel

Info

Publication number
EP1444234A2
EP1444234A2 EP02779219A EP02779219A EP1444234A2 EP 1444234 A2 EP1444234 A2 EP 1444234A2 EP 02779219 A EP02779219 A EP 02779219A EP 02779219 A EP02779219 A EP 02779219A EP 1444234 A2 EP1444234 A2 EP 1444234A2
Authority
EP
European Patent Office
Prior art keywords
propyl
sulfonyl
dihydropyrazolo
ethoxy
pyrimidin
Prior art date
Legal status (The legal status 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 status listed.)
Withdrawn
Application number
EP02779219A
Other languages
German (de)
English (en)
French (fr)
Inventor
Rudolf-Giesbert Alken
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
BDD Berolina Drug Development GmbH
Original Assignee
Turicum Drug Development AG
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 Turicum Drug Development AG filed Critical Turicum Drug Development AG
Publication of EP1444234A2 publication Critical patent/EP1444234A2/de
Withdrawn legal-status Critical Current

Links

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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • 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
    • 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
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

Definitions

  • Deuterated pyrazolopyrimidinones of the general formula I are preferred, where R 1 is D, R 2 is C 1 -C 3 alkyl,
  • Circulatory diseases hypertension, pulmonary hypertension, erectile dysfunction and obstructive
  • 2-ethoxybenzoic acid or deuterated 2-ethoxybenzoic acid is sulfochlorinated in the 5-position analogously to EP 812845 B1 and then reacted with optionally deuterated 4-methylpiperazine, so that 2-ethoxy-5- (4-methylpiperazine sulfonyl) ) benzoic acid or when using deuterated starting materials receives the corresponding deuterated compound.
  • inert diluents such as dextrose, sugar, sorbitol, mannitol, polyvinylpyrrolidone
  • disintegrants such as corn starch or alginic acid
  • binders such as starch or gelatin
  • lubricants such as magnesium stearate or talc and / or agents for achieving a depot effect
  • carboxylpolymethylene, carboxylmethylcellulo - se, cellulose acetate phthalate or polyvinyl acetate can be obtained.
  • the tablets can also consist of several layers.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Gynecology & Obstetrics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
EP02779219A 2001-11-07 2002-11-07 Deuterierte pyrazolopyrimidinone sowie diese verbindungen enthaltende arzneimittel Withdrawn EP1444234A2 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE10155018A DE10155018A1 (de) 2001-11-07 2001-11-07 Deuterierte Pyrazolopyrimidinone sowie diese Verbindungen enthaltende Arzneimittel
DE10155018 2001-11-07
PCT/DE2002/004216 WO2003039439A2 (de) 2001-11-07 2002-11-07 Deuterierte pyrazolopyrimidinone sowie diese verbindungen enthaltende arzneimittel

Publications (1)

Publication Number Publication Date
EP1444234A2 true EP1444234A2 (de) 2004-08-11

Family

ID=7705148

Family Applications (1)

Application Number Title Priority Date Filing Date
EP02779219A Withdrawn EP1444234A2 (de) 2001-11-07 2002-11-07 Deuterierte pyrazolopyrimidinone sowie diese verbindungen enthaltende arzneimittel

Country Status (16)

Country Link
US (1) US20050069276A1 (zh)
EP (1) EP1444234A2 (zh)
JP (1) JP2005509646A (zh)
KR (1) KR20050044381A (zh)
CN (1) CN1606557A (zh)
CA (1) CA2470271A1 (zh)
CZ (1) CZ2004639A3 (zh)
DE (1) DE10155018A1 (zh)
HU (1) HUP0401721A3 (zh)
IL (1) IL161790A0 (zh)
IS (1) IS7246A (zh)
NO (1) NO20042337L (zh)
NZ (1) NZ533385A (zh)
PL (1) PL369654A1 (zh)
RU (1) RU2004117157A (zh)
WO (1) WO2003039439A2 (zh)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20090291958A1 (en) * 2006-06-08 2009-11-26 Auspex Pharmaceuticals, Inc. Substituted PDE5 inhibitors
US20080194529A1 (en) * 2007-02-12 2008-08-14 Auspex Pharmaceuticals, Inc. HIGHLY SELECTIVE and LONG-ACTING PDE5 MODULATORS
ES2395241T3 (es) * 2007-03-07 2013-02-11 Concert Pharmaceuticals Inc. Derivados deuterados de piperazina como compuestos antianginosos
EP2312944B1 (en) 2008-07-15 2018-09-05 Theracos, Inc. Deuterated benzylbenzene derivatives and methods of use
CN102584592B (zh) * 2011-12-28 2014-10-15 李进 一种氘代的拟除虫菊酯化合物及其制备方法和应用
AU2013296627C9 (en) 2012-07-30 2018-03-22 Concert Pharmaceuticals, Inc. Deuterated ibrutinib
CN111116492B (zh) * 2019-01-25 2021-07-09 青岛吉澳医药科技有限公司 氘代苯甲氨嘧啶二酮衍生物及其用途
WO2021236891A1 (en) * 2020-05-20 2021-11-25 Augusta University Research Institute, Inc. Gut-targeted phosphodiesterase inhibitors
CN116444496B (zh) * 2023-06-16 2023-11-24 药康众拓(北京)医药科技有限公司 一种嘧啶联氘代吡唑类化合物及其应用

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9013750D0 (en) * 1990-06-20 1990-08-08 Pfizer Ltd Therapeutic agents
US5250534A (en) * 1990-06-20 1993-10-05 Pfizer Inc. Pyrazolopyrimidinone antianginal agents

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See references of WO03039439A2 *

Also Published As

Publication number Publication date
WO2003039439A2 (de) 2003-05-15
KR20050044381A (ko) 2005-05-12
CN1606557A (zh) 2005-04-13
US20050069276A1 (en) 2005-03-31
RU2004117157A (ru) 2006-01-10
CA2470271A1 (en) 2003-05-15
CZ2004639A3 (cs) 2004-09-15
IL161790A0 (en) 2005-11-20
DE10155018A1 (de) 2003-07-10
HUP0401721A2 (hu) 2005-08-29
PL369654A1 (en) 2005-05-02
JP2005509646A (ja) 2005-04-14
IS7246A (is) 2004-04-30
HUP0401721A3 (en) 2005-11-28
NZ533385A (en) 2006-02-24
NO20042337L (no) 2004-06-04
WO2003039439A3 (de) 2003-10-16

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