ES2188225T3 - Dihydro-(1,2,3)triazolo-(4,5-d)dippirimidin-7-ona- - Google Patents

Dihydro-(1,2,3)triazolo-(4,5-d)dippirimidin-7-ona-

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Publication number
ES2188225T3
ES2188225T3 ES99941615T ES99941615T ES2188225T3 ES 2188225 T3 ES2188225 T3 ES 2188225T3 ES 99941615 T ES99941615 T ES 99941615T ES 99941615 T ES99941615 T ES 99941615T ES 2188225 T3 ES2188225 T3 ES 2188225T3
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Spain
Prior art keywords
carbon atoms
formula
straight
remainder
substituted
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.)
Expired - Lifetime
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ES99941615T
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English (en)
Inventor
Helmut Haning
Ulrich Niewohner
Ulrich Rosentreter
Thomas Schenke
Erwin Bischoff
Karl-Heinz Schlemmer
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Bayer AG
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Bayer AG
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Publication of ES2188225T3 publication Critical patent/ES2188225T3/es
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    • 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
    • A61P13/00—Drugs for disorders of the urinary 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • 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
    • A61P9/06—Antiarrhythmics
    • 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
    • A61P9/08—Vasodilators for multiple indications
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • 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
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers

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

Abstract

Dihidro-[1, 2, 3]triazolo-[4, 5-d]pirimidin-7-onas de fórmula general (I) **(Fórmula)** en la que R1 significa cicloalquilo con 3 a 8 átomos de carbono o un resto de la fórmula, **(Fórmula)** en la que R2 significa alquilo de cadena lineal o ramificada con hasta 10 átomos de carbono, que, dado el caso, está sustituido por hidroxi, E significa un resto de fórmula -CH2-T, en la que T significa una cadena de alquileno lineal o ramificada con hasta 10 átomos de carbono, R3 significa hidrógeno o arilo con 6 a 10 átomos de carbono, que, dado el caso, está sustituido hasta 3 veces de forma igual o diferente por halógeno, hidroxi, nitro, trifluorometilo o por alquilo o alcoxi de cadena lineal o ramificada con hasta 6 átomos de carbono, respectivamente, A y D significan hidrógeno, o A hidrógeno y D hidroxi o A y D significan juntos un resto de la fórmula =O, L significa un resto de la fórmula**(Fórmula)** arilo con 6 a 10 átomos de carbono o un heterociclo aromático, dado el caso benzocondensado, de5 a 7 elementos con hasta 3 heteroátomos de la serie S, N y/u O, estando sustituidos los sistemas cíclicos arriba indicados bajo L hasta 3 veces de forma igual o diferente por uno o varios de los siguientes sustituyentes: halógeno, hidroxi, nitro, trifluorometilo, carboxi, alquilo, alcoxi y alcoxicarbonilo de cadena lineal o ramificada, con hasta 6 átomos de carbono, respectivamente, un resto de la fórmula -(V)a-NR4R5, en la que a significa el número 0 ó 1, V significa un resto de la fórmula -CO o -SO2, R4 y R5 son iguales o distintos y significan hidrógeno o acilo o alcoxicarbonilo de cadena lineal o ramificada con hasta 6 átomos de carbono, respectivamente, o alquilo de cadena lineal o ramificada con hasta 6 átomos de carbono, que, dado el caso, está sustituido por hidroxi, amino o por alquilamino o dialquilamino de cadena lineal o ramificada con hasta 6 átomos de carbono, respectivamente, o R4 y R5 forman junto con el átomo de nitrógeno un heterociclo saturado de 5 ó 6 elementos, que puede contener, dado el caso, otro heteroátomo de la serie S, O o un resto de la fórmula -NR6 y que, dado el caso, está sustituido por alcoxicarbonilo de cadena lineal o ramificada con hasta 6 átomos de carbono, en la que R6 significa hidrógeno o alquilo de cadena lineal o ramificada con hasta 4 átomos de carbono, y/o los sistemas cíclicos indicados bajo L están, dado el caso, sustituidos por arilo con 6 a 10 átomos de carbono y un heterociclo aromático, dado el caso benzocondensado, de 5 a 7 elementos con hasta 3 heteroátomos de la serie S, N y/u O, estando sustituidos estos sistemas cíclicos a su vez, dado el caso, hasta 2 veces de forma igual o distinta por sustituyentes de la serie halógeno, hidroxi, nitro, carboxilo, trifluorometilo o por alquilo, alcoxi o alcoxicarbonilo de cadena lineal o ramificada con hasta 5 átomos de carbono, respectivamente, o por un grupo de la fórmula -(V¿)b-NR7R8, en la que b tiene el significado arriba indicado de a y es igual o distinto a éste, R7 y R8 tienenel significado arriba indicado de R4 y R5 y son iguales o distintos a éste, V¿ tiene el significado arriba indicado de V y es igual o distinto a éste, y los tautómeros y sales de éstas.
ES99941615T 1998-08-26 1999-08-13 Dihydro-(1,2,3)triazolo-(4,5-d)dippirimidin-7-ona- Expired - Lifetime ES2188225T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE19838705A DE19838705A1 (de) 1998-08-26 1998-08-26 Neue Dihydro-(1,2,3)-triazolo-[4,5-d]pyrimidin-7-one

Publications (1)

Publication Number Publication Date
ES2188225T3 true ES2188225T3 (es) 2003-06-16

Family

ID=7878720

Family Applications (1)

Application Number Title Priority Date Filing Date
ES99941615T Expired - Lifetime ES2188225T3 (es) 1998-08-26 1999-08-13 Dihydro-(1,2,3)triazolo-(4,5-d)dippirimidin-7-ona-

Country Status (8)

Country Link
US (1) US6458796B1 (es)
EP (1) EP1107968B1 (es)
JP (1) JP2002523507A (es)
AU (1) AU5516399A (es)
CA (1) CA2342109A1 (es)
DE (2) DE19838705A1 (es)
ES (1) ES2188225T3 (es)
WO (1) WO2000012504A2 (es)

Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2003519153A (ja) * 1999-12-24 2003-06-17 バイエル アクチェンゲゼルシャフト イソオキサゾロピリミジノン類及びその使用
ES2233685T3 (es) * 2000-08-01 2005-06-16 Bayer Healthcare Ag Inhibidores selectivos de pde 2 como medicamentos para mejorar la percepcion.
DE10064105A1 (de) 2000-12-21 2002-06-27 Bayer Ag Neue Substituierte Imidazotriazinone
HN2002000317A (es) * 2001-11-02 2003-05-21 Pfizer Inhibidores de pde9 para tratamiento de trastornos cardiovasculares
FR2842809A1 (fr) * 2002-07-26 2004-01-30 Greenpharma Sas NOUVELLES PYRAZOLO[1,5-a]-1,3,5-TRIAZINES SUBSTITUEES ET LEURS ANALOGUES, COMPOSITIONS PHARMACEUTIQUES LES CONTENANT, UTILISATION A TITRE DE MEDICAMENT ET PROCEDES POUR LEUR PREPARATION
DE10238724A1 (de) 2002-08-23 2004-03-04 Bayer Ag Alkyl-substituierte Pyrazolpyrimidine
DE10238723A1 (de) * 2002-08-23 2004-03-11 Bayer Ag Phenyl-substituierte Pyrazolyprimidine
GB0219746D0 (en) * 2002-08-23 2002-10-02 Inst Of Ex Botany Ascr Azapurine derivatives
DE10238722A1 (de) * 2002-08-23 2004-03-11 Bayer Ag Selektive Phosphodiesterase 9A-Inhibitoren als Arzneimittel zur Verbesserung kognitiver Prozesse
FR2845993B1 (fr) * 2002-10-16 2005-02-11 Univ Pasteur Composes pharmaceutiques inhibiteurs specifiques de la pde5 du muscle lisse, compositions pharmaceutiques les contenant et utilisations therapeutiques
US8044060B2 (en) 2003-05-09 2011-10-25 Boehringer Ingelheim International Gmbh 6-cyclylmethyl- and 6-alkylmethyl pyrazolo[3,4-D]pyrimidines, methods for their preparation and methods for their use to treat impairments of perception, concentration learning and/or memory
DE10320785A1 (de) * 2003-05-09 2004-11-25 Bayer Healthcare Ag 6-Arylmethyl-substituierte Pyrazolopyrimidine
US7504401B2 (en) 2003-08-29 2009-03-17 Locus Pharmaceuticals, Inc. Anti-cancer agents and uses thereof
US7365075B2 (en) * 2003-12-22 2008-04-29 Amgen Inc. Aryl sulfonamide compounds and uses related thereto
DE102004001873A1 (de) 2004-01-14 2005-09-29 Bayer Healthcare Ag Cyanopyrimidinone
US7868037B2 (en) 2004-07-14 2011-01-11 Ptc Therapeutics, Inc. Methods for treating hepatitis C
US7772271B2 (en) 2004-07-14 2010-08-10 Ptc Therapeutics, Inc. Methods for treating hepatitis C
US7781478B2 (en) 2004-07-14 2010-08-24 Ptc Therapeutics, Inc. Methods for treating hepatitis C
NZ553329A (en) 2004-07-22 2010-09-30 Ptc Therapeutics Inc Thienopyridines for treating hepatitis C
EP1703668A1 (en) * 2005-03-18 2006-09-20 Nederlandse Organisatie voor toegepast-natuurwetenschappelijk Onderzoek TNO System for processing quality-of-service parameters in a communication network
JP2010508350A (ja) * 2006-10-31 2010-03-18 ヤンセン ファーマシューティカ エヌ．ベー． Ａｄｐｐ２ｙ１２レセプターアンタゴニストとしてのトリアゾロピリミジン誘導体
US8148385B2 (en) 2006-10-31 2012-04-03 Janssen Pharmaceutica N.V. Substituted [1,2,3] triazolo[4,5-d]pyrimidine derivatives as ADP P2Y12 receptor antagonists
EP2217602B1 (en) 2007-11-30 2018-08-29 Boehringer Ingelheim International GmbH 1,5-dihydro-pyrazolo[3,4-d]pyrimidin-4-one derivatives and their use as pde9a modulators for the treatment of cns disorders
UA105362C2 (en) 2008-04-02 2014-05-12 Бьорингер Ингельхайм Интернациональ Гмбх 1-heterocyclyl-1, 5-dihydro-pyrazolo [3, 4-d] pyrimidin-4-one derivatives and their use as pde9a modulators
EA201100446A1 (ru) 2008-09-08 2011-10-31 Бёрингер Ингельхайм Интернациональ Гмбх Пиразолопиримидины и их применение для лечения нарушений цнс
GEP20146098B (en) 2009-03-31 2014-05-27 Boehringer Ingelheim Int 1-heterocyclyl-1, 5-dihydro-pyrazolo [3, 4-d] pyrimidin-4-one derivatives and their usage as pde9a modulators
TW201118099A (en) * 2009-08-12 2011-06-01 Boehringer Ingelheim Int New compounds for the treatment of CNS disorders
CN103052639B (zh) 2010-08-12 2016-02-17 贝林格尔.英格海姆国际有限公司 6-环烷基-1,5-二氢-吡唑并[3,4-d]嘧啶-4-酮衍生物及其作为PDE9A抑制剂的用途
US8809345B2 (en) 2011-02-15 2014-08-19 Boehringer Ingelheim International Gmbh 6-cycloalkyl-pyrazolopyrimidinones for the treatment of CNS disorders
US20230041334A1 (en) * 2019-11-14 2023-02-09 Behavioral Diagnostics, Llc Methods and compositions for smoking cessation

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US4076711A (en) 1976-04-05 1978-02-28 Schering Corporation Triazolo [4,5-d]-pyrimidines
EP0229011A1 (de) 1986-01-06 1987-07-15 Ciba-Geigy Ag Trisubstituierte Triazole
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DE19541264A1 (de) 1995-11-06 1997-05-07 Bayer Ag Purin-6-on-derivate

Also Published As

Publication number Publication date
EP1107968A2 (de) 2001-06-20
JP2002523507A (ja) 2002-07-30
WO2000012504A3 (de) 2000-06-22
US6458796B1 (en) 2002-10-01
AU5516399A (en) 2000-03-21
DE19838705A1 (de) 2000-03-02
CA2342109A1 (en) 2000-03-09
WO2000012504A2 (de) 2000-03-09
DE59903421D1 (de) 2002-12-19
EP1107968B1 (de) 2002-11-13

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