AR033996A1 - Una 7-oxo-piridopirimidina, su uso, un proceso para prepararla, una composicion farmaceutica que la comprende, un proceso para producir una pirimidina, un proceso para producir una piridopirimidina, y compuestos preparados mediante dichos procesos - Google Patents

Una 7-oxo-piridopirimidina, su uso, un proceso para prepararla, una composicion farmaceutica que la comprende, un proceso para producir una pirimidina, un proceso para producir una piridopirimidina, y compuestos preparados mediante dichos procesos

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Publication number
AR033996A1
AR033996A1 ARP010104131A ARP010104131A AR033996A1 AR 033996 A1 AR033996 A1 AR 033996A1 AR P010104131 A ARP010104131 A AR P010104131A AR P010104131 A ARP010104131 A AR P010104131A AR 033996 A1 AR033996 A1 AR 033996A1
Authority
AR
Argentina
Prior art keywords
alkyl
pyridopirimidine
produce
oxo
hydrogen
Prior art date
Application number
ARP010104131A
Other languages
English (en)
Inventor
James Patrick Dunn
David Michael Goldstein
Julie Anne Lim
Jian Jeffrey Chen
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR033996A1 publication Critical patent/AR033996A1/es

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    • 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
    • C07D239/47One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61P27/00Drugs for disorders of the senses
    • A61P27/16Otologicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/16Antivirals for RNA viruses for influenza or rhinoviruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • A61P31/22Antivirals for DNA viruses for herpes viruses
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    • A61P33/00Antiparasitic agents
    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06Antimalarials
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    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
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    • AHUMAN NECESSITIES
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    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
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  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
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  • Pharmacology & Pharmacy (AREA)
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  • Diabetes (AREA)
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  • Biomedical Technology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Reproductive Health (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
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Abstract

Una 7-oxo piridopirimidina de fórmula (1) en donde e R1 es hidrógeno, alquilo; R2 es -CR'R''-Ra (donde R' y R'' son hidrógeno, hidroxialquilo o alquilo siendo al menos uno alquilo o hidroxialquilo y Ra es hidroxialquilo), Rx-S(O)2-Ry (donde Rx es alquilo y Ry es alquenilo), alquilo sustituido con alcoxilo, heterociclilalquilo o C4-5 cicloalquilo, en donde cada uno de los grupos hidroxilo presentes en R2 pueden estar independientemente en la forma de un derivado de sulfonato, éster, carbamato o carbonato; o R1 y R2 junto con el átomo de nitrógeno al que están unidos forman un heterocíclico; R3 es hidrógeno, alquilo, amino, monoalquilamino, dialquilamino, cicloalquilo, arilo, aralquilo, haloalquilo, heteroalquilo, cianoalquilo, alquilen-C(O)-R (donde R es hidrógeno, alquilo, hidroxilo, alcoxilo, amino, monoalquilamino o dialquilamino) o acilo; y Ar1 es arilo, o un profármaco o una sal farmacéuticamente aceptable de las mismas, su uso para la preparación de medicamentos, un proceso para prepararla, una composición farmacéutica que la comprende, un proceso para producir pirimidina, un proceso para producir una piridopirimidina, y compuestos preparados mediante los procesos, La 7-oxo-piridopirimidina es útil para el tratamiento de trastornos mediados por p38.
ARP010104131A 2000-08-31 2001-08-30 Una 7-oxo-piridopirimidina, su uso, un proceso para prepararla, una composicion farmaceutica que la comprende, un proceso para producir una pirimidina, un proceso para producir una piridopirimidina, y compuestos preparados mediante dichos procesos AR033996A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US22957700P 2000-08-31 2000-08-31

Publications (1)

Publication Number Publication Date
AR033996A1 true AR033996A1 (es) 2004-01-21

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ID=22861834

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ARP010104131A AR033996A1 (es) 2000-08-31 2001-08-30 Una 7-oxo-piridopirimidina, su uso, un proceso para prepararla, una composicion farmaceutica que la comprende, un proceso para producir una pirimidina, un proceso para producir una piridopirimidina, y compuestos preparados mediante dichos procesos

Country Status (18)

Country Link
EP (1) EP1315727B1 (es)
JP (1) JP4146721B2 (es)
KR (1) KR100582325B1 (es)
CN (2) CN100358892C (es)
AR (1) AR033996A1 (es)
AT (1) ATE298751T1 (es)
AU (2) AU1214702A (es)
BR (1) BR0113590A (es)
CA (1) CA2420122A1 (es)
DE (1) DE60111752T2 (es)
ES (1) ES2243568T3 (es)
GT (1) GT200100190A (es)
MX (1) MXPA03001733A (es)
PA (1) PA8527401A1 (es)
PE (1) PE20020524A1 (es)
UY (1) UY26920A1 (es)
WO (1) WO2002018379A2 (es)
ZA (1) ZA200301078B (es)

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AU2003225072A1 (en) * 2002-04-19 2003-11-03 Smithkline Beecham Corporation Novel compounds
ATE457716T1 (de) 2002-12-30 2010-03-15 Angiotech Int Ag Wirkstofffreisetzung von schnell gelierender polymerzusammensetzung
WO2005007193A2 (en) * 2003-07-07 2005-01-27 Vande Woude, George, F. Inhibition of tumor angiogenesis by combination of thrombospondin-1 and inhibitors of vascular endothelial growth factor
WO2005105097A2 (en) * 2004-04-28 2005-11-10 Gpc Biotech Ag Pyridopyrimidines for treating inflammatory and other diseases
MXPA06014486A (es) 2004-06-15 2007-03-01 Pfizer Derivados de acido carboxilico de bencimidazolona.
WO2006115237A1 (ja) * 2005-04-25 2006-11-02 Ube Industries, Ltd. 4-アミノ-2-アルキルチオ-5-ピリミジンカルバルデヒドの製法
JP2006321749A (ja) * 2005-05-19 2006-11-30 Ube Ind Ltd 2−シアノマロンアルデヒドのアルカリ金属塩の製法
JP2009525292A (ja) 2006-01-31 2009-07-09 エフ.ホフマン−ラ ロシュ アーゲー 7h−ピリド[3,4−d]ピリミジン−8−オン、それらの製造及びプロテインキナーゼ阻害剤としての使用
EP2094698A1 (en) * 2006-11-09 2009-09-02 F. Hoffmann-Roche AG Substituted 6-phenyl-pyrido [2,3-d]pyrimidin-7-one derivatives as kinase inhibitors and methods for using the same
CA2690327A1 (en) 2007-06-15 2008-12-18 Thomas P. Cleary A novel process for the preparation of 3-amino-pentan-1,5-diol
CA2776770A1 (en) * 2009-10-09 2011-04-14 Afraxis, Inc. 8-ethyl-6-(aryl)pyrido[2,3-d]pyrimidin-7(8h)-ones for the treatment of cns disorders
US20120184542A1 (en) 2011-01-19 2012-07-19 Kevin Anderson Pyrido pyrimidines
EP2828259B1 (en) * 2012-03-22 2018-08-08 Oscotec, Inc. Substituted pyridopyrimidine compounds and their use as flt3 inhibitors
NZ711376A (en) 2013-03-15 2020-01-31 Sanofi Sa Heteroaryl compounds and uses thereof
TWI647220B (zh) 2013-03-15 2019-01-11 美商西建卡爾有限責任公司 雜芳基化合物及其用途
JP6576325B2 (ja) 2013-03-15 2019-09-18 セルジーン シーエーアール エルエルシー ヘテロアリール化合物およびそれらの使用
US10342786B2 (en) 2017-10-05 2019-07-09 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD
AU2018346709A1 (en) 2017-10-05 2020-04-16 Fulcrum Therapeutics, Inc. Use of p38 inhibitors to reduce expression of DUX4
CN112119064B (zh) * 2018-09-14 2023-06-23 上海和誉生物医药科技有限公司 Fgfr抑制剂、其制备方法和应用
WO2022052924A1 (zh) * 2020-09-11 2022-03-17 上海凌达生物医药有限公司 一类含氮稠环类化合物的制备方法和用途

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JPS6183168A (ja) * 1984-09-28 1986-04-26 Ube Ind Ltd 2−メルカプト−4−アミノ−5−ホルミルピリミジンおよびその製法
IL117923A (en) * 1995-05-03 2000-06-01 Warner Lambert Co Anti-cancer pharmaceutical compositions containing polysubstituted pyrido¬2,3-d¾pyrimidine derivatives and certain such novel compounds
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US6184226B1 (en) * 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
EP1315726A1 (en) * 2000-08-31 2003-06-04 F. Hoffmann-La Roche Ag 7- oxo pyridopyrimidines as inhibitors of cellular proliferation

Also Published As

Publication number Publication date
CN1721412A (zh) 2006-01-18
KR20030022423A (ko) 2003-03-15
PE20020524A1 (es) 2002-06-18
BR0113590A (pt) 2003-07-22
GT200100190A (es) 2002-05-23
JP2004507540A (ja) 2004-03-11
JP4146721B2 (ja) 2008-09-10
EP1315727A2 (en) 2003-06-04
CA2420122A1 (en) 2002-03-07
EP1315727B1 (en) 2005-06-29
ATE298751T1 (de) 2005-07-15
CN1303072C (zh) 2007-03-07
WO2002018379A3 (en) 2002-07-25
KR100582325B1 (ko) 2006-05-22
MXPA03001733A (es) 2003-05-27
DE60111752D1 (de) 2005-08-04
AU1214702A (en) 2002-03-13
DE60111752T2 (de) 2006-05-04
CN100358892C (zh) 2008-01-02
UY26920A1 (es) 2002-02-28
WO2002018379A2 (en) 2002-03-07
CN1451004A (zh) 2003-10-22
ES2243568T3 (es) 2005-12-01
PA8527401A1 (es) 2002-07-30
ZA200301078B (en) 2004-05-07
AU2002212147B2 (en) 2007-10-18

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