MX2012000103A - Nuevos derivados de 1,2,3,4-tetrahidro-pirimido (1,2-a) pirimidin-6-ona, su preparacion y su uso farmaceutica. - Google Patents

Nuevos derivados de 1,2,3,4-tetrahidro-pirimido (1,2-a) pirimidin-6-ona, su preparacion y su uso farmaceutica.

Info

Publication number
MX2012000103A
MX2012000103A MX2012000103A MX2012000103A MX2012000103A MX 2012000103 A MX2012000103 A MX 2012000103A MX 2012000103 A MX2012000103 A MX 2012000103A MX 2012000103 A MX2012000103 A MX 2012000103A MX 2012000103 A MX2012000103 A MX 2012000103A
Authority
MX
Mexico
Prior art keywords
novel
pyrimido
pyrimidin
tetrahydro
derivatives
Prior art date
Application number
MX2012000103A
Other languages
English (en)
Inventor
Fabrice Viviani
Bruno Filoche-Romme
Frank Halley
Eric Bacque
Baptiste Ronan
Laurent Schio
Annie Clauss
Gilbert Marciniak
Bertrand Vivet
Maurice Brollo
Youssef El Ahmad
Andre Zimmermann
Karl Andreas Karlsson
Original Assignee
Sanofi 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
Priority claimed from FR0903237A external-priority patent/FR2947551B1/fr
Priority claimed from FR0957069A external-priority patent/FR2951174B1/fr
Application filed by Sanofi Sa filed Critical Sanofi Sa
Publication of MX2012000103A publication Critical patent/MX2012000103A/es

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
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06—Antimalarials
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • 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
    • C07D239/06—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • 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
    • C07D239/42—One nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La invención se relaciona con los nuevos materiales de fórmula (I), en donde: R1 es un L-arilo o un L-heteroarilo opcionalmente sustituido, tal que L es un enlace simple, alquilo, CO, o CO-alk, o L-X, en donde L es un alquilo y X es O o S; R2 es H o alquilo; R3 es un alquilo opcionalmente sustituido por Hal; y R4 es Hou Hal, en donde los materiales están en cualquier forma isomérica, y con las sales de los mismos para utilizarse como fármacos.
MX2012000103A 2009-07-02 2010-07-01 Nuevos derivados de 1,2,3,4-tetrahidro-pirimido (1,2-a) pirimidin-6-ona, su preparacion y su uso farmaceutica. MX2012000103A (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
FR0903237A FR2947551B1 (fr) 2009-07-02 2009-07-02 Nouveaux derives de 1,2,3,4-tetrahydro-pyrimido{1,2-a)pyrimidin-6-one, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de phosphorylation d'akt (pkb)
US24109809P 2009-09-10 2009-09-10
FR0957069A FR2951174B1 (fr) 2009-10-09 2009-10-09 Nouveaux derives de 1,2,3,4-tetrahydro-pyrimido{1,2-a}pyrimidin-6-one, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de phosphorylation d'akt(pkb)
PCT/FR2010/051374 WO2011001113A2 (fr) 2009-07-02 2010-07-01 NOUVEAUX DERIVES DE 1,2,3,4-TETRAHYDRO-PYRIMIDO{1,2-a}PYRIMIDIN-6-ONE,LEUR PREPARATION ET LEUR UTILISATION PHARMACEUTIQUE

Publications (1)

Publication Number Publication Date
MX2012000103A true MX2012000103A (es) 2012-05-22

Family

ID=43234240

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2012000103A MX2012000103A (es) 2009-07-02 2010-07-01 Nuevos derivados de 1,2,3,4-tetrahidro-pirimido (1,2-a) pirimidin-6-ona, su preparacion y su uso farmaceutica.

Country Status (24)

Country Link
US (1) US8846670B2 (es)
EP (1) EP2448940B1 (es)
JP (1) JP5655070B2 (es)
KR (1) KR20120103553A (es)
CN (1) CN102482286B (es)
AR (1) AR077363A1 (es)
AU (1) AU2010267815B2 (es)
BR (1) BRPI1015943A8 (es)
CA (1) CA2766909C (es)
DK (1) DK2448940T3 (es)
ES (1) ES2487623T3 (es)
HK (1) HK1169388A1 (es)
HR (1) HRP20140786T1 (es)
IL (1) IL217293A (es)
MX (1) MX2012000103A (es)
MY (1) MY155661A (es)
PL (1) PL2448940T3 (es)
PT (1) PT2448940E (es)
RU (1) RU2561130C2 (es)
SG (2) SG177464A1 (es)
SI (1) SI2448940T1 (es)
TW (1) TWI455940B (es)
UY (1) UY32754A (es)
WO (1) WO2011001113A2 (es)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI2655375T1 (sl) 2010-12-23 2015-03-31 Sanofi Derivati pirimidinona, njihova priprava in njihova farmacevtska uporaba
FR2969613B1 (fr) * 2010-12-23 2013-02-08 Sanofi Aventis Nouveaux derives de 1,2,3,4-tetrahydro-pyrimido{1,2-a}pyrimidin-6-one, leur preparation et leur utilisation pharmaceutique
EP2790705B1 (en) 2011-12-15 2017-12-06 Novartis AG Use of inhibitors of the activity or function of pi3k
FR2992316A1 (fr) * 2012-06-22 2013-12-27 Sanofi Sa Derives de pyrimidinones, leur preparation et leur application en therapeutique
FR2992314B1 (fr) * 2012-06-22 2015-10-16 Sanofi Sa Nouveaux derives de 2,3-dihydro-1h-imidazo{1,2-a}pyrimidin-5-one et 1,2,3,4-tetrahydro-pyrimido{1,2-a}pyrimidin-6-one comportant une morpholine substituee, leur preparation et leur utilisation pharmaceutique
EP3266455B1 (en) 2015-03-06 2020-12-30 Korea Advanced Institute of Science and Technology Composition for prevention or treatment of intractable epilepsy comprising mtor inhibitor
JP6997462B2 (ja) 2016-02-19 2022-01-17 スプリント バイオサイエンス アクティエボラーグ がんおよび糖尿病の治療に有用な６－アリール－４－モルホリン－１－イルピリドン化合物
RU2762968C2 (ru) 2016-02-19 2021-12-24 Спринт Биосайенс Аб 6-гетероциклил-4-морфолин-4-илпиридин-2-оны, пригодные для лечения рака и диабета
JP2023515708A (ja) * 2020-04-27 2023-04-13 アルナ バイオ， インコーポレーテッド 中枢神経系送達のための結合剤及びその使用

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2703712A1 (de) * 1977-01-29 1978-08-03 Bayer Ag Substituierte pyrimidinon eckige klammer auf (di)-thio eckige klammer zu -phosphor-(phosphon)-saeureester bzw. -esteramide, verfahren zu ihrer herstellung und ihre verwendung als insektizide, akarizide und nematizide
MY125533A (en) * 1999-12-06 2006-08-30 Bristol Myers Squibb Co Heterocyclic dihydropyrimidine compounds
ATE363471T1 (de) 2000-01-24 2007-06-15 Astrazeneca Ab Durch einen morpholinrest substituierte therapeutische verbindungen
WO2002018386A1 (en) 2000-09-01 2002-03-07 Sanofi-Synthelabo 2-PYRIDINYL-6,7,8,9-TETRAHYDROPYRIMIDO[1,2-a]PYRIMIDIN-4-ONE AND 7-PYRIDINYL-2,3-DIHYDROIMIDAZO[1,2-a]PYRIMIDIN-5(1H)ONE DERIVATI VES
GB0119865D0 (en) 2001-08-14 2001-10-10 Cancer Res Campaign Tech DNA-PK inhibitors
DE60205921T2 (de) * 2001-09-21 2006-06-22 Sanofi-Aventis SUBSTITUIERTE 2-PYRIDINYL-6,7,8,9-TETRAHYDROPYRIMIDOç1,2-A!PYRIMIDIN-4-ON- UND 7-PYRIDINYL-2,3-DIHYDROIMIDAZO-ç1,2-A!PYRIMIDIN-5(1H)ONDERIVATE
EP1340761A1 (en) 2002-02-28 2003-09-03 Sanofi-Synthelabo Substituted 2-pyridinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one and 7-pyridinyl-2,3-dihydroimidazo[1,2-a]pyrimidin-5(1H)one derivatives
DK1480983T3 (da) 2002-02-28 2006-03-27 Sanofi Aventis Heteroarylsubstituerede 2-pyridinyl- og 2-pyrimidinyl- 6,7,8,9-tetrahydropyrimido[1,2a]pyrimidin-4-onderivater
EP1537102A4 (en) 2002-08-16 2010-12-08 Astrazeneca Ab INHIBITORS OF PHOSPHOINOSITIDE-3-KINASE BETA
JP4733986B2 (ja) * 2002-12-27 2011-07-27 イステイチユート・デイ・リチエルケ・デイ・ビオロジア・モレコラーレ・ピ・アンジエレツテイ・エツセ・ピー・アー ＨＩＶインテグラーゼ阻害薬として有用なテトラヒドロ−４Ｈ−ピリド［１，２−ａ］ピリミジン類および関連する化合物
EP1454909B1 (en) 2003-03-07 2008-08-20 Sanofi Aventis 8'-pyridinyl-dihydrospiro (cycloalkyl) -pyrimido (1,2-a) pyrimidin-6-one and 8'-pyrimidinyl-dihydrospiro (cycloalkyl) pyrimido (1,2-a) pyrimidin-6 derivatives -one and their use against neurodegenerative diseases
EP1460076A1 (en) 2003-03-21 2004-09-22 Sanofi-Synthelabo Substituted 8-perfluoroalkyl-6,7,8,9-tetrahydropyrimido[1,2-a] pyrimidin-4-one derivatives
EP1557417B1 (en) 2003-12-19 2007-03-07 Sanofi-Aventis Substituted 8'-pyri(mi)dinyl-dihydrospiro-[cycloalkylamine]-pyrimido[1,2-a] pyrimidin-6-one derivatives
AR053358A1 (es) 2005-04-15 2007-05-02 Cancer Rec Tech Ltd Inhibidores de adn - pk
US20090035394A1 (en) 2005-05-26 2009-02-05 Graeme Cameron Murray Smith Use of dna-pk inhibition to sensitise atm deficient cancers to dna-damaging cancer therapies
WO2008064244A2 (en) 2006-11-20 2008-05-29 The Trustees Of Columbia University In The City Of New York Phosphoinositide modulation for the treatment of neurodegenerative diseases
WO2008148074A2 (en) 2007-05-24 2008-12-04 Research Foundation Of State University Of New York Inhibitors of mtor and methods of treatment using same

Also Published As

Publication number Publication date
RU2012103477A (ru) 2013-08-10
IL217293A (en) 2016-12-29
ES2487623T3 (es) 2014-08-22
SG10201403149YA (en) 2014-08-28
AU2010267815B2 (en) 2015-07-16
BRPI1015943A2 (pt) 2016-04-19
KR20120103553A (ko) 2012-09-19
MY155661A (en) 2015-11-13
AU2010267815A1 (en) 2012-02-16
IL217293A0 (en) 2012-02-29
CN102482286B (zh) 2015-07-15
PL2448940T3 (pl) 2014-10-31
UY32754A (es) 2011-01-31
HRP20140786T1 (hr) 2014-11-07
US20120208810A1 (en) 2012-08-16
TW201105673A (en) 2011-02-16
CA2766909A1 (fr) 2011-01-06
TWI455940B (zh) 2014-10-11
DK2448940T3 (da) 2014-08-25
PT2448940E (pt) 2014-09-03
SG177464A1 (en) 2012-02-28
BRPI1015943A8 (pt) 2018-01-09
US8846670B2 (en) 2014-09-30
WO2011001113A2 (fr) 2011-01-06
EP2448940B1 (fr) 2014-05-21
HK1169388A1 (en) 2013-01-25
JP2012531463A (ja) 2012-12-10
RU2561130C2 (ru) 2015-08-20
WO2011001113A3 (fr) 2011-02-24
JP5655070B2 (ja) 2015-01-14
AR077363A1 (es) 2011-08-24
EP2448940A2 (fr) 2012-05-09
SI2448940T1 (sl) 2014-10-30
CA2766909C (fr) 2018-06-05
CN102482286A (zh) 2012-05-30

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