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HUP0105437A2 - Új malonsavszármazékok, előállításuk és alkalmazásuk, valamint e vegyületeket tartalmazó gyógyászati készítmények - Google Patents

Új malonsavszármazékok, előállításuk és alkalmazásuk, valamint e vegyületeket tartalmazó gyógyászati készítmények

Info

Publication number
HUP0105437A2
HUP0105437A2 HU0105437A HUP0105437A HUP0105437A2 HU P0105437 A2 HUP0105437 A2 HU P0105437A2 HU 0105437 A HU0105437 A HU 0105437A HU P0105437 A HUP0105437 A HU P0105437A HU P0105437 A2 HUP0105437 A2 HU P0105437A2
Authority
HU
Hungary
Prior art keywords
group
preparation
processes
pharmaceutical compositions
compositions containing
Prior art date
Application number
HU0105437A
Other languages
English (en)
Inventor
Fahad A. Al-Obeidi
Elisabeth Defossa
Uwe Heinelt
Otmar Klingler
Hans Matter
Armin Walser
Peter Wildgoose
Gerhard Zoller
Original Assignee
Aventis Pharma Deutschland Gmbh.
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 EP99100002A external-priority patent/EP1016663A1/en
Application filed by Aventis Pharma Deutschland Gmbh. filed Critical Aventis Pharma Deutschland Gmbh.
Publication of HUP0105437A2 publication Critical patent/HUP0105437A2/hu
Publication of HUP0105437A3 publication Critical patent/HUP0105437A3/hu

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C257/00—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines
    • C07C257/10—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines
    • C07C257/18—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines having carbon atoms of amidino groups bound to carbon atoms of six-membered aromatic rings
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C279/00—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C07C279/04—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton
    • C07C279/14—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton being further substituted by carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/10—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulphur atoms

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyridine Compounds (AREA)

Abstract

A találmány szerinti vegyületek (I) általános képletében R(1)jelentése hidroxilcsoport vagy szerves csoport; R(2) jelentésehidrogénatom vagy alkilcsoport; R(3) jelentése szerves csoport; R(4)jelentése hidrogénatom vagy alkilcsoport, cikloalkilcsoport,cikloalkilalkil-csoport vagy aril-alkilcsoport; R(5) jelentésehidrogénatom vagy szerves csoport; vagy R(4) és R(5) együtt adottesetben helyettesített karboaromás csoportot alkot; és R(6) jelentésehidroxilcsoport vagy szerves csoport. A találmány tárgyköréheztartoznak a fenti vegyületek előállítása és alkalmazása, valamint evegyületeket tartalmazó gyógyászati készítmények, melyektromboembóliás betegségek kezelésére alkalmazhatók. Ó
HU0105437A 1999-01-02 1999-12-23 Novel malonic acid derivatives, processes for their preparation, their use and pharmaceutical compositions containing them HUP0105437A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP99100002A EP1016663A1 (en) 1999-01-02 1999-01-02 Novel malonic acid derivatives, processes for their preparation, their use and pharmaceutical compositions containing them (inhibition of factor Xa activity)
EP99119537 1999-10-01

Publications (2)

Publication Number Publication Date
HUP0105437A2 true HUP0105437A2 (hu) 2002-05-29
HUP0105437A3 HUP0105437A3 (en) 2003-03-28

Family

ID=26152843

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0105437A HUP0105437A3 (en) 1999-01-02 1999-12-23 Novel malonic acid derivatives, processes for their preparation, their use and pharmaceutical compositions containing them

Country Status (17)

Country Link
US (1) US6395737B1 (hu)
EP (1) EP1140878A1 (hu)
JP (1) JP2002534420A (hu)
KR (1) KR20010101355A (hu)
CN (1) CN1332734A (hu)
AU (1) AU3043100A (hu)
BR (1) BR9916732A (hu)
CA (1) CA2358578A1 (hu)
CZ (1) CZ20012379A3 (hu)
HK (1) HK1041700A1 (hu)
HU (1) HUP0105437A3 (hu)
ID (1) ID29979A (hu)
IL (1) IL144096A0 (hu)
NO (1) NO20012983D0 (hu)
PL (1) PL349343A1 (hu)
TR (1) TR200101903T2 (hu)
WO (1) WO2000040571A1 (hu)

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EP1127884A1 (en) * 2000-02-26 2001-08-29 Aventis Pharma Deutschland GmbH Novel malonic acid derivatives, processes for their preparation, their use as inhibitor of factor XA activity and pharmaceutical compositions containing them
FR2812635B1 (fr) * 2000-08-01 2002-10-11 Aventis Pharma Sa Nouveaux composes heterocycliques, preparation et utilisation comme medicaments notamment comme anti- bacteriens
US20050232995A1 (en) * 2002-07-29 2005-10-20 Yam Nyomi V Methods and dosage forms for controlled delivery of paliperidone and risperidone
HUE025683T2 (hu) 2002-12-03 2016-04-28 Pharmacyclics Llc VIIA faktor inhibitor 2-(2-hidroxi-bifenil-3-il)-1H-benzoimidazol-5-karboxamidin-származékok
US9828324B2 (en) 2010-10-20 2017-11-28 Sirrus, Inc. Methylene beta-diketone monomers, methods for making methylene beta-diketone monomers, polymerizable compositions and products formed therefrom
US9249265B1 (en) 2014-09-08 2016-02-02 Sirrus, Inc. Emulsion polymers including one or more 1,1-disubstituted alkene compounds, emulsion methods, and polymer compositions
US10414839B2 (en) 2010-10-20 2019-09-17 Sirrus, Inc. Polymers including a methylene beta-ketoester and products formed therefrom
US9279022B1 (en) 2014-09-08 2016-03-08 Sirrus, Inc. Solution polymers including one or more 1,1-disubstituted alkene compounds, solution polymerization methods, and polymer compositions
CN103502198B (zh) 2010-10-20 2016-07-06 瑟拉斯公司 在传热剂存在下使用快速回收合成亚甲基丙二酸酯
EP2766345B1 (en) 2011-10-14 2016-03-16 Bristol-Myers Squibb Company Substituted tetrahydroisoquinoline compounds as factor xia inhibitors
US9000172B2 (en) 2011-10-14 2015-04-07 Bristol-Myers Squibb Company Substituted tetrahydroisoquinoline compounds as factor XIa inhibitors
WO2013056034A1 (en) 2011-10-14 2013-04-18 Bristol-Myers Squibb Company Substituted tetrahydroisoquinoline compounds as factor xia inhibitors
EP3339301A3 (en) 2011-10-19 2018-08-08 Sirrus, Inc. Methods for making methylene beta-diketone monomers
EP3848402A1 (en) 2012-03-30 2021-07-14 Sirrus, Inc. Ink and coating formulations and polymerizable systems for producing the same
WO2013149165A1 (en) 2012-03-30 2013-10-03 Bioformix Inc. Methods for activating polymerizable compositions, polymerizable systems, and products formed thereby
JP6553505B2 (ja) 2012-03-30 2019-07-31 シラス・インコーポレイテッド 複合材およびラミネート物品ならびにこれらを作製するための重合系
US10047192B2 (en) 2012-06-01 2018-08-14 Sirrus, Inc. Optical material and articles formed therefrom
WO2014059202A1 (en) 2012-10-12 2014-04-17 Bristol-Myers Squibb Company Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
LT2906551T (lt) 2012-10-12 2018-04-25 Bristol-Myers Squibb Company Faktoriaus xia kristalinės formos
WO2014059214A1 (en) 2012-10-12 2014-04-17 Bristol-Myers Squibb Company Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
WO2014078689A1 (en) 2012-11-16 2014-05-22 Bioformix Inc. Plastics bonding systems and methods
EP2926368B1 (en) 2012-11-30 2020-04-08 Sirrus, Inc. Electronic assembly
WO2014110388A1 (en) 2013-01-11 2014-07-17 Bioformix Inc. Method to obtain methylene malonate via bis(hydroxymethyl) malonate pathway
EP2978751B1 (en) 2013-03-25 2018-12-05 Bristol-Myers Squibb Company Tetrahydroisoquinolines containing substituted azoles as factor xia inhibitors
UY35971A (es) 2014-01-31 2015-07-31 Bristol Myers Squibb Company Una Corporación Del Estado De Delaware Macrociclos con grupos p2? aromáticos como inhibidores del factor xia
NO2760821T3 (hu) 2014-01-31 2018-03-10
AU2015284307A1 (en) 2014-07-01 2017-02-02 Rempex Pharmaceuticals, Inc. Boronic acid derivatives and therapeutic uses thereof
EP3189047B1 (en) 2014-09-04 2018-12-26 Bristol-Myers Squibb Company Diamide macrocycles that are fxia inhibitors
US9416091B1 (en) 2015-02-04 2016-08-16 Sirrus, Inc. Catalytic transesterification of ester compounds with groups reactive under transesterification conditions
US9315597B2 (en) 2014-09-08 2016-04-19 Sirrus, Inc. Compositions containing 1,1-disubstituted alkene compounds for preparing polymers having enhanced glass transition temperatures
US9453018B2 (en) 2014-10-01 2016-09-27 Bristol-Myers Squibb Company Pyrimidinones as factor XIa inhibitors
US10501400B2 (en) 2015-02-04 2019-12-10 Sirrus, Inc. Heterogeneous catalytic transesterification of ester compounds with groups reactive under transesterification conditions
US9334430B1 (en) 2015-05-29 2016-05-10 Sirrus, Inc. Encapsulated polymerization initiators, polymerization systems and methods using the same
US9217098B1 (en) 2015-06-01 2015-12-22 Sirrus, Inc. Electroinitiated polymerization of compositions having a 1,1-disubstituted alkene compound
US9518001B1 (en) 2016-05-13 2016-12-13 Sirrus, Inc. High purity 1,1-dicarbonyl substituted-1-alkenes and methods for their preparation
US9567475B1 (en) 2016-06-03 2017-02-14 Sirrus, Inc. Coatings containing polyester macromers containing 1,1-dicarbonyl-substituted 1 alkenes
US10196481B2 (en) 2016-06-03 2019-02-05 Sirrus, Inc. Polymer and other compounds functionalized with terminal 1,1-disubstituted alkene monomer(s) and methods thereof
US10428177B2 (en) 2016-06-03 2019-10-01 Sirrus, Inc. Water absorbing or water soluble polymers, intermediate compounds, and methods thereof
US9617377B1 (en) 2016-06-03 2017-04-11 Sirrus, Inc. Polyester macromers containing 1,1-dicarbonyl-substituted 1 alkenes

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EP1016663A1 (en) 1999-01-02 2000-07-05 Aventis Pharma Deutschland GmbH Novel malonic acid derivatives, processes for their preparation, their use and pharmaceutical compositions containing them (inhibition of factor Xa activity)

Also Published As

Publication number Publication date
IL144096A0 (en) 2002-05-23
PL349343A1 (en) 2002-07-15
HK1041700A1 (zh) 2002-07-19
BR9916732A (pt) 2001-09-25
NO20012983L (no) 2001-06-15
ID29979A (id) 2001-10-25
WO2000040571A1 (en) 2000-07-13
AU3043100A (en) 2000-07-24
CZ20012379A3 (cs) 2001-09-12
HUP0105437A3 (en) 2003-03-28
KR20010101355A (ko) 2001-11-14
CA2358578A1 (en) 2000-07-13
NO20012983D0 (no) 2001-06-15
US6395737B1 (en) 2002-05-28
CN1332734A (zh) 2002-01-23
JP2002534420A (ja) 2002-10-15
TR200101903T2 (tr) 2001-11-21
EP1140878A1 (en) 2001-10-10

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