AU1105992A - 4-pyrimidinone derivatives, their preparation and their application in therapy - Google Patents

4-pyrimidinone derivatives, their preparation and their application in therapy

Info

Publication number
AU1105992A
AU1105992A AU11059/92A AU1105992A AU1105992A AU 1105992 A AU1105992 A AU 1105992A AU 11059/92 A AU11059/92 A AU 11059/92A AU 1105992 A AU1105992 A AU 1105992A AU 1105992 A AU1105992 A AU 1105992A
Authority
AU
Australia
Prior art keywords
alkyl
optionally substituted
ring
branched
linear
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.)
Granted
Application number
AU11059/92A
Other versions
AU650319B2 (en
Inventor
Michel Aletru
Marc Daumas
Christian Hoornaert
Jean-Claude Muller
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.)
Synthelabo SA
Original Assignee
Synthelabo SA
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 Synthelabo SA filed Critical Synthelabo SA
Publication of AU1105992A publication Critical patent/AU1105992A/en
Application granted granted Critical
Publication of AU650319B2 publication Critical patent/AU650319B2/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/34—One oxygen atom
    • C07D239/36—One oxygen atom as doubly bound oxygen atom or as unsubstituted hydroxy radical
    • 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
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Macromolecular Compounds Obtained By Forming Nitrogen-Containing Linkages In General (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Liquid Developers In Electrophotography (AREA)

Abstract

1. Compounds, existing in three tautomeric forms, corresponding to the general formulae (I), (I') and (I'') <IMAGE> in which R1 = linear or branched (C1-7)alkyl, linear or branched (C3-9)alkenyl, cyclo(C3-7)alkyl(C1-6)alkyl, R2 = H, linear or branched (C1-7)alkyl, cyclo(C3-7)alkyl(C1-3)alkyl, aryl(C1-3)alkyl optionally substituted in the ring, aryloxy(C1-3)alkyl optionally substituted in the ring, arylthio(C1-3)alkyl optionally substituted in the ring, arylsulphonyl(C1-3)alkyl optionally substituted in the ring, heteroaryl(C1-3)alkyl optionally substituted in the ring, R3 = CO2H 1H-tetrazol-5-yl, NHCOR11, NHSO2R11, CONHSO2R11, CONHOR12, where R11 = CH3, CF3 or optionally substituted phenyl, R12 = H, CH3 or optionally substituted phenyl, as well as their pharmaceutically acceptable organic or inorganic salts. Therapeutic application.t
AU11059/92A 1991-02-20 1992-02-19 4-pyrimidinone derivatives, their preparation and their application in therapy Ceased AU650319B2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FR9102032A FR2672892B1 (en) 1991-02-20 1991-02-20 DERIVATIVES OF 4-PYRIMIDINONES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION.
FR9102032 1991-02-20

Publications (2)

Publication Number Publication Date
AU1105992A true AU1105992A (en) 1992-08-27
AU650319B2 AU650319B2 (en) 1994-06-16

Family

ID=9409925

Family Applications (1)

Application Number Title Priority Date Filing Date
AU11059/92A Ceased AU650319B2 (en) 1991-02-20 1992-02-19 4-pyrimidinone derivatives, their preparation and their application in therapy

Country Status (23)

Country Link
EP (1) EP0500409B1 (en)
JP (1) JP2529798B2 (en)
KR (1) KR920016434A (en)
CN (1) CN1034171C (en)
AT (1) ATE135695T1 (en)
AU (1) AU650319B2 (en)
CA (1) CA2061456A1 (en)
CS (1) CS49092A3 (en)
DE (1) DE69209113T2 (en)
DK (1) DK0500409T3 (en)
ES (1) ES2086090T3 (en)
FI (1) FI920720A (en)
FR (1) FR2672892B1 (en)
GR (1) GR3019404T3 (en)
HU (2) HUT60477A (en)
IE (1) IE76145B1 (en)
IL (1) IL101014A (en)
MX (1) MX9200690A (en)
NO (1) NO920648L (en)
NZ (1) NZ241659A (en)
PL (1) PL168617B1 (en)
RU (1) RU2073675C1 (en)
ZA (1) ZA921203B (en)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL102183A (en) * 1991-06-27 1999-11-30 Takeda Chemical Industries Ltd Biphenyl substituted heterocyclic compounds their production and pharmaceutical compositions comprising them
FR2700543B1 (en) * 1993-01-15 1995-03-17 Synthelabo Salts of 4-pyrimidinone derivatives, their preparation and their therapeutic use.
SE9903028D0 (en) 1999-08-27 1999-08-27 Astra Ab New use
EA020466B1 (en) 2007-06-04 2014-11-28 Синерджи Фармасьютикалз Инк. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
US8969514B2 (en) 2007-06-04 2015-03-03 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases
CA2726917C (en) 2008-06-04 2018-06-26 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
CA2730603C (en) 2008-07-16 2019-09-24 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
TW201444848A (en) * 2009-01-30 2014-12-01 Takeda Pharmaceutical Fused ring compound and use thereof
US9616097B2 (en) 2010-09-15 2017-04-11 Synergy Pharmaceuticals, Inc. Formulations of guanylate cyclase C agonists and methods of use
CA2905435A1 (en) 2013-03-15 2014-09-25 Synergy Pharmaceuticals Inc. Compositions useful for the treatment of gastrointestinal disorders
EP2970384A1 (en) 2013-03-15 2016-01-20 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase and their uses
CN113388007A (en) 2013-06-05 2021-09-14 博士医疗爱尔兰有限公司 Ultra-pure agonists of guanylate cyclase C, methods of making and using the same

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1334092C (en) * 1986-07-11 1995-01-24 David John Carini Angiotensin ii receptor blocking imidazoles
US5064825A (en) * 1989-06-01 1991-11-12 Merck & Co., Inc. Angiotensin ii antagonists
KR0163595B1 (en) * 1989-06-30 1998-12-01 미리암디, 메코너헤이 Substituted imidazoles
EP0407342A3 (en) * 1989-07-06 1991-07-10 Ciba-Geigy Ag Pyrimidine derivatives
EP0424317A3 (en) * 1989-10-19 1991-09-25 Ciba-Geigy Ag Pyrimidines
EP0435827A3 (en) * 1989-12-28 1991-11-13 Ciba-Geigy Ag Diaza compounds
CA2079344A1 (en) * 1990-03-30 1991-10-01 Eric E. Allen Substituted pyrimidines, pyrimidinones and pyridopyrimidines
IE912114A1 (en) * 1990-07-02 1992-01-15 Union Pharma Scient Appl Novel pyrimidine derivatives which are angiotensin ii¹receptor antagonists, their methods of preparation and¹pharmaceutical compositions in which they are present

Also Published As

Publication number Publication date
PL168617B1 (en) 1996-03-29
HU9200532D0 (en) 1992-05-28
KR920016434A (en) 1992-09-24
IE920525A1 (en) 1992-08-26
EP0500409B1 (en) 1996-03-20
FR2672892A1 (en) 1992-08-21
DE69209113D1 (en) 1996-04-25
FI920720A (en) 1992-08-21
FI920720A0 (en) 1992-02-19
GR3019404T3 (en) 1996-06-30
IL101014A (en) 1996-06-18
ATE135695T1 (en) 1996-04-15
AU650319B2 (en) 1994-06-16
IL101014A0 (en) 1992-11-15
JP2529798B2 (en) 1996-09-04
CA2061456A1 (en) 1992-08-21
MX9200690A (en) 1992-08-01
CS49092A3 (en) 1992-09-16
NZ241659A (en) 1993-03-26
HUT60477A (en) 1992-09-28
CN1064269A (en) 1992-09-09
EP0500409A1 (en) 1992-08-26
ES2086090T3 (en) 1996-06-16
HU211886A9 (en) 1995-12-28
CN1034171C (en) 1997-03-05
NO920648D0 (en) 1992-02-19
FR2672892B1 (en) 1994-01-14
RU2073675C1 (en) 1997-02-20
PL293531A1 (en) 1992-08-24
NO920648L (en) 1992-08-21
DK0500409T3 (en) 1996-07-15
JPH04346980A (en) 1992-12-02
DE69209113T2 (en) 1996-10-31
ZA921203B (en) 1992-11-25
IE76145B1 (en) 1997-10-08

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