DK0500409T3 - Derivatives of 4-pyrimidinols, their preparation and use in therapy - Google Patents

Derivatives of 4-pyrimidinols, their preparation and use in therapy

Info

Publication number
DK0500409T3
DK0500409T3 DK92400269.4T DK92400269T DK0500409T3 DK 0500409 T3 DK0500409 T3 DK 0500409T3 DK 92400269 T DK92400269 T DK 92400269T DK 0500409 T3 DK0500409 T3 DK 0500409T3
Authority
DK
Denmark
Prior art keywords
alkyl
optionally substituted
ring
branched
linear
Prior art date
Application number
DK92400269.4T
Other languages
Danish (da)
Inventor
Jean-Claude Muller
Michel Aletru
Christian Hoornaert
Marc Daumas
Original Assignee
Synthelabo
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 filed Critical Synthelabo
Application granted granted Critical
Publication of DK0500409T3 publication Critical patent/DK0500409T3/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/34One oxygen atom
    • C07D239/36One oxygen atom as doubly bound oxygen atom or as unsubstituted hydroxy radical
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52Two oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/10Heterocyclic 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)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (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)
  • Liquid Developers In Electrophotography (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (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
DK92400269.4T 1991-02-20 1992-02-03 Derivatives of 4-pyrimidinols, their preparation and use in therapy DK0500409T3 (en)

Applications Claiming Priority (1)

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.

Publications (1)

Publication Number Publication Date
DK0500409T3 true DK0500409T3 (en) 1996-07-15

Family

ID=9409925

Family Applications (1)

Application Number Title Priority Date Filing Date
DK92400269.4T DK0500409T3 (en) 1991-02-20 1992-02-03 Derivatives of 4-pyrimidinols, their preparation and use 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
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
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
EP2810951B1 (en) 2008-06-04 2017-03-15 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
ES2624828T3 (en) 2008-07-16 2017-07-17 Synergy Pharmaceuticals Inc. Guanylate cyclase agonists useful for the treatment of gastrointestinal disorders, inflammation, cancer and others
MA33071B1 (en) * 2009-01-30 2012-02-01 Takeda Pharmaceutical Composite of intensive nucleus and its use
US9616097B2 (en) 2010-09-15 2017-04-11 Synergy Pharmaceuticals, Inc. Formulations of guanylate cyclase C agonists and methods of use
CA2905438A1 (en) 2013-03-15 2014-09-25 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase and their uses
CA2905435A1 (en) 2013-03-15 2014-09-25 Synergy Pharmaceuticals Inc. Compositions useful for the treatment of gastrointestinal disorders
PT3004138T (en) 2013-06-05 2024-06-18 Bausch Health Ireland Ltd Ultra-pure agonists of guanylate cyclase c, method of making and using 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
RU2099330C1 (en) * 1989-06-30 1997-12-20 Е.И.Дюпон Де Немур Энд Компани Substituted imidazoles or their pharmaceutically acceptable salts and a pharmaceutical composition
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
JPH05505609A (en) * 1990-03-30 1993-08-19 メルク・エンド・カムパニー・インコーポレーテツド Substituted pyrimidines, pyrimidinones and pyridrimidines
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
CN1034171C (en) 1997-03-05
PL168617B1 (en) 1996-03-29
HU211886A9 (en) 1995-12-28
EP0500409B1 (en) 1996-03-20
IE920525A1 (en) 1992-08-26
FI920720A (en) 1992-08-21
CS49092A3 (en) 1992-09-16
FI920720A0 (en) 1992-02-19
FR2672892B1 (en) 1994-01-14
CA2061456A1 (en) 1992-08-21
DE69209113T2 (en) 1996-10-31
ATE135695T1 (en) 1996-04-15
CN1064269A (en) 1992-09-09
ES2086090T3 (en) 1996-06-16
NO920648L (en) 1992-08-21
JP2529798B2 (en) 1996-09-04
RU2073675C1 (en) 1997-02-20
GR3019404T3 (en) 1996-06-30
DE69209113D1 (en) 1996-04-25
KR920016434A (en) 1992-09-24
HU9200532D0 (en) 1992-05-28
NO920648D0 (en) 1992-02-19
AU650319B2 (en) 1994-06-16
PL293531A1 (en) 1992-08-24
IE76145B1 (en) 1997-10-08
HUT60477A (en) 1992-09-28
MX9200690A (en) 1992-08-01
IL101014A (en) 1996-06-18
ZA921203B (en) 1992-11-25
EP0500409A1 (en) 1992-08-26
NZ241659A (en) 1993-03-26
AU1105992A (en) 1992-08-27
FR2672892A1 (en) 1992-08-21
IL101014A0 (en) 1992-11-15
JPH04346980A (en) 1992-12-02

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