BR9916732A - Derivados de ácido malÈnico, processo para a sua preparação, seu uso e composições farmacêuticas contendo-os (inibição da atividade do fator xa) - Google Patents

Derivados de ácido malÈnico, processo para a sua preparação, seu uso e composições farmacêuticas contendo-os (inibição da atividade do fator xa)

Info

Publication number
BR9916732A
BR9916732A BR9916732-8A BR9916732A BR9916732A BR 9916732 A BR9916732 A BR 9916732A BR 9916732 A BR9916732 A BR 9916732A BR 9916732 A BR9916732 A BR 9916732A
Authority
BR
Brazil
Prior art keywords
formula
factor
inhibition
activity
preparation
Prior art date
Application number
BR9916732-8A
Other languages
English (en)
Inventor
Elisabeth Defossa
Uwe Heinelt
Otmar Klingler
Gerhard Zoller
Hans Matter
Fahad A Al-Obeidi
Armin Walser
Peter Wildgoose
Original Assignee
Aventis Pharma 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 Gmbh filed Critical Aventis Pharma Gmbh
Publication of BR9916732A publication Critical patent/BR9916732A/pt

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

Abstract

Patente de Invenção: <B>"DERIVADOS DE áCIDO MALÈNICO, PROCESSO PARA A SUA PREPARAçãO, SEU USO E COMPOSIçõES FARMACêUTICAS CONTENDO-OS (INIBIçãO DA ATIVIDADE DO FATOR XA)"<D>. A presente invenção refere-se a novos compostos para a inibição de proteínas de coagulação do sangue, e mais particularmente, a derivados de ácido malónico da fórmula (I), em que R(1), R(2), R(3), R(4), R(5) e R(6) têm os significados indicados nas reivindicações. Os compostos de fórmula I são inibidores do fator Xa da enzima de coagulação do sangue. A invenção também refere-se a processos para a preparação dos compostos de fórmula I, a métodos de inibição da atividade do fator Xa e de inibição da coagulação do sangue, ao uso dos compostos de fórmula I no tratamento e profilaxia de doenças, que podem ser tratadas ou prevenidas pela inibição da atividade do fator Xa tais como doenças tromboembólicas, e ao uso dos compostos de fórmula I na preparação de medicamentos a serem aplicados em tais doenças. A invenção ainda refere-se a composições contendo um composto de fórmula I em mistura ou de outro modo em associação com um veículo inerte, em particular composições farmacêuticas contendo um composto de fórmula I juntamente com substâncias veículose substâncias auxiliares farmaceuticamente aceitáveis.
BR9916732-8A 1999-01-02 1999-12-23 Derivados de ácido malÈnico, processo para a sua preparação, seu uso e composições farmacêuticas contendo-os (inibição da atividade do fator xa) BR9916732A (pt)

Applications Claiming Priority (3)

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
PCT/EP1999/010340 WO2000040571A1 (en) 1999-01-02 1999-12-23 Novel malonic acid derivatives, processes for their preparation, their use and pharmaceutical compositions containing them (inhibition of factor xa activity)

Publications (1)

Publication Number Publication Date
BR9916732A true BR9916732A (pt) 2001-09-25

Family

ID=26152843

Family Applications (1)

Application Number Title Priority Date Filing Date
BR9916732-8A BR9916732A (pt) 1999-01-02 1999-12-23 Derivados de ácido malÈnico, processo para a sua preparação, seu uso e composições farmacêuticas contendo-os (inibição da atividade do fator xa)

Country Status (17)

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

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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
WO2004050637A2 (en) 2002-12-03 2004-06-17 Axys Pharmaceuticals, Inc. 2-(2-hydroxybiphenyl-3-yl)-1h-benzoimidazole-5-carboxamidine derivatives as factor viia inhibitors
US10414839B2 (en) 2010-10-20 2019-09-17 Sirrus, Inc. Polymers including a methylene beta-ketoester 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
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
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
JP2014503474A (ja) 2010-10-20 2014-02-13 バイオフオーミツクス・インコーポレイテツド エネルギー移動手段の存在下での急速回収を用いたメチレンマロナートの合成
ES2699226T3 (es) 2011-10-14 2019-02-08 Bristol Myers Squibb Co Compuestos de tetrahidroisoquinolina sustituidos como inhibidores del factor XIa
HUE034857T2 (en) 2011-10-14 2018-03-28 Bristol Myers Squibb Co Substituted tetrahydroisoquinoline compounds are inhibitors of factor XIA
ES2579832T3 (es) 2011-10-14 2016-08-17 Bristol-Myers Squibb Company Compuestos de tetrahidroisoquinolina sustituida como inhibidores del factor XIa
JP6267643B2 (ja) 2011-10-19 2018-01-24 シラス・インコーポレイテッド 多官能性モノマー、多官能性モノマーを製造する方法、これらから形成された重合性組成物および製品
JP6188252B2 (ja) 2012-03-30 2017-08-30 シラス・インコーポレイテッド 重合性組成物の活性化方法、重合系およびこれにより形成される製品
US9234107B2 (en) 2012-03-30 2016-01-12 Sirrus, Inc. Ink coating formulations and polymerizable systems for producing the same
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
TR201807316T4 (tr) 2012-10-12 2018-06-21 Squibb Bristol Myers Co Bir faktör XIa inhibitörünün kristalli formları.
EP2906552B1 (en) 2012-10-12 2017-11-22 Bristol-Myers Squibb Company Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
EP2906541B1 (en) 2012-10-12 2017-11-22 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
WO2014085570A1 (en) 2012-11-30 2014-06-05 Bioformix, Inc. Composite compositions for electronics applications
EP2943462B1 (en) 2013-01-11 2018-06-27 Sirrus, Inc. Method to obtain methylene malonate via bis(hydroxymethyl) malonate pathway
ES2712699T3 (es) 2013-03-25 2019-05-14 Bristol Myers Squibb Co Tetrahidroisoquinolinas que contienen azoles sustituidos como inhibidores del factor XIa
MY190429A (en) 2014-01-31 2022-04-21 Bristol Myers Squibb Co Macrocycles with hetrocyclic p2' groups as factor xia inhibitors
NO2760821T3 (pt) 2014-01-31 2018-03-10
AU2015284307A1 (en) 2014-07-01 2017-02-02 Rempex Pharmaceuticals, Inc. Boronic acid derivatives and therapeutic uses thereof
JP6526796B2 (ja) 2014-09-04 2019-06-05 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ Ｆｘｉａ阻害剤であるジアミドマクロ環
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
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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
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US9518001B1 (en) 2016-05-13 2016-12-13 Sirrus, Inc. High purity 1,1-dicarbonyl substituted-1-alkenes and methods for their preparation
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Also Published As

Publication number Publication date
WO2000040571A1 (en) 2000-07-13
TR200101903T2 (tr) 2001-11-21
HK1041700A1 (zh) 2002-07-19
NO20012983L (no) 2001-06-15
CN1332734A (zh) 2002-01-23
KR20010101355A (ko) 2001-11-14
US6395737B1 (en) 2002-05-28
NO20012983D0 (no) 2001-06-15
EP1140878A1 (en) 2001-10-10
HUP0105437A3 (en) 2003-03-28
PL349343A1 (en) 2002-07-15
JP2002534420A (ja) 2002-10-15
CZ20012379A3 (cs) 2001-09-12
CA2358578A1 (en) 2000-07-13
HUP0105437A2 (hu) 2002-05-29
IL144096A0 (en) 2002-05-23
AU3043100A (en) 2000-07-24
ID29979A (id) 2001-10-25

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Legal Events

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FA10 Dismissal: dismissal - article 33 of industrial property law
B11N Dismissal: publication cancelled [chapter 11.14 patent gazette]
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 5O, 6O E 7O ANUIDADES.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 1913 DE 04/09/2007.