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2. 发明专利

ES2564352T3 Derivados de tranilcipromina como inhibidores de la histona-desmetilasa LSD1 y/o LSD2 未知
公开(公告)号：ES2564352T3
公开(公告)日：2016-03-22
申请号：ES11716208
申请日：2011-04-15
申请人： UNIVERSITÀ DEGLI STUDI DI ROMA LA SAPIENZA , FOND IEO , UNIVERSITA' DEGLI STUDI DI PAVIA , UNIVERSITA' DEGLI STUDI DI MILANO
发明人： MINUCCI SAVERIO , MAI ANTONELLO , MATTEVI ANDREA
IPC分类号： C07C233/43 , A61K31/167 , A61K31/17 , A61K31/325 , A61K31/381 , A61P31/12 , A61P35/00 , C07C233/44 , C07C233/80 , C07C271/22 , C07C271/28 , C07C275/24 , C07D333/60
摘要： Un compuesto de fórmula general (I)**Fórmula** o un isómero, tautómero, forma racémica, enantiómero, diastereómero, epímero, solvato, mezclas del mismo, sal farmacéuticamente aceptable del mismo, en la que: A es R o CH(R1)-NH-CO-R2; R y R2 se seleccionan entre: alquilo, alquenilo, alquinilo, cicloalquilo, arilo, heteroarilo, heterocicloalquilo, cicloalquilalquiloxi, arilalquiloxi, heteroarilalquiloxi, heterocicloalquilalquiloxi, cicloalquilalquilo, arilalquilo, heteroarilalquilo, heterocicloalquilalquilo, cicloalquilalquilamino, arilalquilamino, heteroarilalquilamino, heterocicloalquilalquilamino; R1 se selecciona entre: alquilo, alquenilo, alquinilo, cicloalquilo, arilo, heteroarilo, heterocicloalquilo, cicloalquilalquilo, arilalquilo, heteroarilalquilo, heterocicloalquilalquilo; R3 es H, alquilo C1-C6, y en la que cualquiera de los grupos alquilo, alquenilo, alquinilo, cicloalquilo, arilo, heteroarilo, heterocicloalquilo anteriores está opcionalmente sustituido adicionalmente en cualquiera de sus posiciones libres con uno o más grupos seleccionados entre halógeno, carboxi, ciano, alquilo, alquilo polifluorado, alquenilo, alquinilo, cicloalquilo, arilo, heteroarilo, alquil-heteroarilo, heteroaril-alquilo, aminoalquilo, grupos amino y derivados de los mismos seleccionados entre alquilamino, dialquilamino, arilamino, diarilamino, ureido, alquilureido o arilureido; grupos carbonilamino y derivados de los mismos seleccionados entre formilamino, alquilcarbonilamino, alquenilcarbonilamino, arilcarbonilamino, alcoxicarbonilamino; grupos hidroxi y derivados de los mismos seleccionados entre alcoxi, alcoxi polifluorado, ariloxi, heteroariloxi, alquilcarboniloxi, arilcarboniloxi o cicloalquiloxi; grupos carbonilo y derivados de los mismos seleccionados entre alquilcarbonilo, arilcarbonilo, alcoxicarbonilo, ariloxicarbonilo, cicloalquiloxicarbonilo, aminocarbonilo, alquilaminocarbonilo, dialquilaminocarbonilo, ácido hidroxámico; derivados sulfurados seleccionados entre alquiltio, ariltio, alquilsulfonilo, arilsulfonilo, alquilsulfinilo, arilsulfinilo, arilsulfoniloxi, aminosulfonilo, alquilaminosulfonilo o dialquilaminosulfonilo; cada uno de dichos sustituyentes pueden estar sustituido adicionalmente con uno o más de los grupos mencionados anteriormente.

3. 发明专利

CA2797011C TRANYLCYPROMINE DERIVATIVES AS INHIBITORS OF HISTONE DEMETHYLASE LSD1 AND/OR LSD2 未知
公开(公告)号：CA2797011C
公开(公告)日：2018-10-02
申请号：CA2797011
申请日：2011-04-15
申请人： UNIV DEGLI STUDI ROMA LA SAPIENZA , FOND IEO , UNIV DEGLI STUDI DI PAVIA , UNIV DEGLI STUDI MILANO
发明人： MINUCCI SAVERIO , MAI ANTONELLO , MATTEVI ANDREA
IPC分类号： C07C233/43 , A61K31/167 , A61K31/17 , A61K31/325 , A61K31/381 , A61P31/12 , A61P35/00 , C07C233/44 , C07C233/80 , C07C271/22 , C07C271/28 , C07C275/24 , C07D333/60
摘要： Tranylcypromme derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of histone demethylases LSD1 and LSD2, such as the diseases characterized by deregulation of gene transcription, cell differentiation and proliferation, e g tumors, viral infections, are herem described. These compounds belong to the structural formula (I) wherein A and R3 are as defined in the specification The invention also relates to the preparation of these compounds, as well as to compositions containing them and to therapeutic use thereof.

4. 发明专利

AU2011244478A1 Tranylcypromine derivatives as inhibitors of histone demethylase LSD1 and/or LSD2 未知
公开(公告)号：AU2011244478A1
公开(公告)日：2012-11-01
申请号：AU2011244478
申请日：2011-04-15
申请人： UNI DELGI STUDI DI PAVIA , UNIV DEGLI STUDI MILANO , FOND IEO , UNIV ROMA
发明人： MINUCCI SAVERIO , MAI ANTONELLO , MATTEVI ANDREA
IPC分类号： C07C233/43 , A61K31/167 , A61K31/17 , A61K31/325 , A61K31/381 , A61P31/12 , A61P35/00 , C07C233/44 , C07C233/80 , C07C271/22 , C07C271/28 , C07C275/24 , C07D333/60
摘要： Tranylcypromine derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of histone demethylases LSD1 and LSD2, such as the diseases characterized by deregulation of gene transcription, cell differentiation and proliferation, e.g. tumors, viral infections, are herein described. These compounds belong to the structural formula (I) wherein A and R are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to compositions containing them and to therapeutic use thereof.

5. 发明专利

EA022459B1 ПРОИЗВОДНЫЕ ТРАНИЛЦИПРОМИНА В КАЧЕСТВЕ ИНГИБИТОРОВ ГИСТОН ДЕМЕТИЛАЗ LSD1 И/ИЛИ LSD2 未知
公开(公告)号：EA022459B1
公开(公告)日：2016-01-29
申请号：EA201291073
申请日：2011-04-15
申请人： UNIV ROMA , FOND IEO , UNIV PAVIA , UNIV DEGLI STUDI MILANO
发明人： MINUCCI SAVERIO , MAI ANTONELLO , MATTEVI ANDREA
IPC分类号： C07C233/43 , A61K31/167 , A61K31/17 , A61K31/325 , A61K31/381 , A61P31/12 , A61P35/00 , C07C233/44 , C07C233/80 , C07C271/22 , C07C271/28 , C07C275/24 , C07D333/60
摘要： Визобретенииописаныпроизводныетранилципромина, используемыев качестветерапевтическихагентов, вчастностидляпрофилактикии/илилечениязаболеванийи состояний, связанныхс активностьюгистондеметилаз LSD1 и LSD2, напримерзаболеваний, характеризующихсянарушениемрегуляциитранскрипциигенов, дифференцировкии пролиферацииклеток, такихкакопухолии вирусныеинфекции. Этисоединениясоответствуютструктурнойформуле (I), гдеА и Rопределеныв описанииизобретения. Крометого, изобретениеотноситсяк препаратамэтихсоединений, атакжек содержащимихкомпозициями кихтерапевтическомуприменению.

6. 发明专利

AU2011244478B2 Tranylcypromine derivatives as inhibitors of histone demethylase LSD1 and/or LSD2 未知
公开(公告)号：AU2011244478B2
公开(公告)日：2014-07-17
申请号：AU2011244478
申请日：2011-04-15
申请人： FOND IEO CCM , UNIV DEGLI STUDI MILANO , UNIV DEGLI STUDI ROMA LA SAPIENZA , UNIV DELGI STUDI DI PAVIA
发明人： MINUCCI SAVERIO , MAI ANTONELLO , MATTEVI ANDREA
IPC分类号： C07C233/43 , A61K31/167 , A61K31/17 , A61K31/325 , A61K31/381 , A61P31/12 , A61P35/00 , C07C233/44 , C07C233/80 , C07C271/22 , C07C271/28 , C07C275/24 , C07D333/60
摘要： Tranylcypromine derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of histone demethylases LSD1 and LSD2, such as the diseases characterized by deregulation of gene transcription, cell differentiation and proliferation, e.g. tumors, viral infections, are herein described. These compounds belong to the structural formula (I) wherein A and R

7. 发明专利

ZA201207856B TRANYLCYPROMINE DERIVATIVES AS INHIBITORS OF HISTONE DEMETHYLASE LSD1 AND/OR LSD2 未知
公开(公告)号：ZA201207856B
公开(公告)日：2013-06-29
申请号：ZA201207856
申请日：2012-10-18
申请人： UNIV DEGLI STUDI ROMA LA SAPIENZA , FOND IEO , UNIV DEGLI STUDI DI PAVIA , UNIV DEGLI STUDI MILANO
发明人： MINUCCI SAVERIO , MATTEVI ANDREA , MAI ANTONELLO
IPC分类号： A61P20060101 , A61K20060101 , C07C20060101 , C07D20060101
摘要： Tranylcypromine derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of histone demethylases LSD1 and LSD2, such as the diseases characterized by deregulation of gene transcription, cell differentiation and proliferation, e.g. tumors, viral infections, are herein described. These compounds belong to the structural formula (I) wherein A and R3 are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to compositions containing them and to therapeutic use thereof.

8. 发明专利

CA2797011A1 TRANYLCYPROMINE DERIVATIVES AS INHIBITORS OF HISTONE DEMETHYLASE LSD1 AND/OR LSD2 未知
公开(公告)号：CA2797011A1
公开(公告)日：2011-10-27
申请号：CA2797011
申请日：2011-04-15
申请人： UNIV ROMA , FOND IEO , UNIV PAVIA , UNI DEGLI STUDI MILANO
发明人： MINUCCI SAVERIO , MAI ANTONELLO , MATTEVI ANDREA
IPC分类号： C07C233/43 , A61K31/167 , A61K31/17 , A61K31/325 , A61K31/381 , A61P31/12 , A61P35/00 , C07C233/44 , C07C233/80 , C07C271/22 , C07C271/28 , C07C275/24 , C07D333/60
摘要： Tranylcypromine derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of histone demethylases LSD1 and LSD2, such as the diseases characterized by deregulation of gene transcription, cell differentiation and proliferation, e.g. tumors, viral infections, are herein described. These compounds belong to the structural formula (I) wherein A and R3 are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to compositions containing them and to therapeutic use thereof.

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