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    • 1. 发明申请
    • SUBSTITUTED 2,3-DIHYDROIMIDAZO[1,2-C]QUINAZOLINE-CONTAINING COMBINATIONS
    • 取代的2,3-二氢吲哚并[1,2-C]喹唑啉的组合
    • WO2011128407A9
    • 2011-12-22
    • PCT/EP2011055917
    • 2011-04-14
    • BAYER PHARMA AGLIU NINGSHU
    • LIU NINGSHU
    • A61K45/00
    • A61K31/519A61K31/18A61K31/4406A61K31/5377A61K45/06A61K2300/00
    • The present invention relates to : * combinations of : component A : one or more 2,3-dihydroimidazo[1,2-c]quinazoline compounds of general formula (A1) or (A2), or a physiologically acceptable salt, solvate, hydrate or stereoisomer thereof; component B : one or more N-(2-arylamino) aryl sulfonamide compounds of general formula (B), or Lapatinib, or Paclitaxel, or a physiologically acceptable salt, solvate, hydrate or stereoisomer thereof; and, optionally, component C : one or more further pharmaceutical agents; in which optionally some or all of the components are in the form of a pharmaceutical formulation which is ready for use to be administered simultaneously, concurrently, separately or sequentially. dependently of one another by the oral, intravenous, topical, local installations, intraperitoneal or nasal route; * use of such combinations for the preparation of a medicament for the treatment or prophylaxis of a cancer; and * a kit comprising such a combination.
    • 本发明涉及:组合物A:一种或多种通式(A1)或(A2)的2,3-二氢咪唑并[1,2-c]喹唑啉化合物或其生理学上可接受的盐,溶剂合物,水合物 或其立体异构体; 组分B:通式(B)的一种或多种N-(2-芳基氨基)芳基磺酰胺化合物或拉帕替尼或紫杉醇或其生理学上可接受的盐,溶剂化物,水合物或立体异构体; 和任选的组分C:一种或多种另外的药剂; 其中任选地,一些或所有组分是药物制剂的形式,其可以同时使用,同时,单独或顺序地使用。 通过口服,静脉内,局部,局部装置,腹膜内或鼻道相互依赖; *使用这种组合来制备用于治疗或预防癌症的药物; 和*包含这种组合的试剂盒。
    • 2. 发明申请
    • SUBSTITUTED 2,3-DIHYDROIMIDAZO[1,2-C]QUINAZOLINE-CONTAINING COMBINATIONS
    • 取代的2,3-二氢吲哚并[1,2-C]喹唑啉的组合
    • WO2011128407A3
    • 2012-02-23
    • PCT/EP2011055917
    • 2011-04-14
    • BAYER PHARMA AGLIU NINGSHU
    • LIU NINGSHU
    • A61K45/06A61K31/18A61K31/4406A61K31/519A61K31/5377
    • A61K31/519A61K31/18A61K31/4406A61K31/5377A61K45/06A61K2300/00
    • The present invention relates to : * combinations of : component A : one or more 2,3-dihydroimidazo[1,2-c]quinazoline compounds of general formula (A1) or (A2), or a physiologically acceptable salt, solvate, hydrate or stereoisomer thereof; component B : one or more N-(2-arylamino) aryl sulfonamide compounds of general formula (B), or Lapatinib, or Paclitaxel, or a physiologically acceptable salt, solvate, hydrate or stereoisomer thereof; and, optionally, component C : one or more further pharmaceutical agents; in which optionally some or all of the components are in the form of a pharmaceutical formulation which is ready for use to be administered simultaneously, concurrently, separately or sequentially. dependently of one another by the oral, intravenous, topical, local installations, intraperitoneal or nasal route; * use of such combinations for the preparation of a medicament for the treatment or prophylaxis of a cancer; and * a kit comprising such a combination.
    • 本发明涉及:组合物A:一种或多种通式(A1)或(A2)的2,3-二氢咪唑并[1,2-c]喹唑啉化合物或其生理学上可接受的盐,溶剂合物,水合物 或其立体异构体; 组分B:通式(B)的一种或多种N-(2-芳基氨基)芳基磺酰胺化合物或拉帕替尼或紫杉醇或其生理学上可接受的盐,溶剂化物,水合物或立体异构体; 和任选的组分C:一种或多种另外的药剂; 其中任选地,一些或所有组分是药物制剂的形式,其可以同时使用,同时,单独或顺序地使用。 通过口服,静脉内,局部,局部装置,腹膜内或鼻道相互依赖; *使用这种组合来制备用于治疗或预防癌症的药物; 和*包含这种组合的试剂盒。
    • 6. 发明专利
    • USE OF SUBSTITUTED 2,3-DIHYDROIMIDAZ0[1,2-C]QUINAZOLINES.
    • TN2017000385A1
    • 2019-01-16
    • TN2017000385
    • 2016-03-07
    • BAYER HEALTHCARE PHARMACEUTICALS INCBAYER PHARMA AG
    • GENVRESSE ISABELLEJEFFERS MICHAELLIU NINGSHUPENA CAROL
    • A61K31/519A61K45/06A61P35/00C12Q1/68
    • The present invention relates to : use of a 2,3-dihydroimidazo[l ,2-c]quinazoline compound, or of a pharmaceutical composition containing same, as a sole active agent, or of a combination of a) said compound or a pharmaceutical composition containing said compound and b) one or more further active agents, for the preparation of a medicament for the treatment or prophylaxis of endometrial cancer (hereinafter abbreviated to "EC"), particularly Ist line, 2nd line, relapsed, refractory, type 1 or type Il EC, or endometriosis ; - combinations of a) said compound and b) one or more further active agents; - a pharmaceutical composition comprising said compound as a sole active agent for the treatment of endometrial cancer (hereinafter abbreviated to "EC"), particularly Ist line, 2nd line, relapsed, refractory, type 1 or type Il EC, or endometriosis ; - a pharmaceutical composition comprising a combination of a) said compound and b) one or more further active agents ; - use of biomarkers which is the loss of tumor suppressor PTEN or FBXW7, for predicting the sensitivity and/or resistance of a cancer patient to said compound and providing a rationale-based dosage to increase sensitivity and/or to overcome resistance ; - a method of determining the loss of tumor suppressor PTEN or FBXW7 ; and - a method for determining perturbations in PIK3CA, PIK3CB, PIK3CD, PIK3CG, PIK3Rl, PIK3R2, PIK3R3, PIK3R4, PIK3R5, FGFRI, FGFR2, FGFR3 and/or FGFR4. PTEN loss and alteration of PIK3CA, PIK3CB, PIK3CD, PIK3CG, PIK3Rl, PIK3R2, PIK3R3, PIK3R4, PIK3R5, FGFRI, FGFR2, FGFR3 and/or FGFR4.
    • 8. 发明专利
    • COMBINACIONES QUE CONTIENEN 2,3- DIHIDROIMIDAZO[1,2-C]QUINAZOLINA SUSTITUIDA
    • SV2017005530A
    • 2018-10-02
    • SV2017005530
    • 2017-09-08
    • BAYER PHARMA AGBAYER HEALTHCARE PHARMACEUTICALS INC
    • LIU NINGSHUPENA CAROLJEFFERS MICHAELGENVRESSE ISABELLE
    • A61K31/519A61K31/53A61K45/06A61P35/00C12Q1/68
    • COMBINACIONES DE: COMPONENTE A : UNO O MÁS COMPUESTOS DE 2,3-DIHIDROIMIDAZO[1,2-C]QUINAZOLINA DE FÓRMULA GENERAL (A1) O (A2), O UNA SAL, SOLVATO, HIDRATO O ESTEREOISÓMERO FISIOLÓGICAMENTE ACEPTABLE DE LOS MISMOS; COMPONENTE B : UNO O MÁS COMPUESTOS DE 5-(1-BENZOTIOFEN-2-IL)PIRROLO[2,1-F][1,2,4]-TRIAZIN-4- AMINA SUSTITUIDA DE FÓRMULA GENERAL (B), O UNA SAL, SOLVATO, HIDRATO O ESTEREOISÓMERO FISIOLÓGICAMENTE ACEPTABLE DE LOS MISMOS; EN LAS CUALES OPCIONALMENTE ALGUNOS O TODOS LOS COMPONENTES ESTÁN EN FORMA DE UNA FORMULACIÓN FARMACÉUTICA LA CUAL ESTÁ LISTA PARA SU UTILIZACIÓN Y SE ADMINISTRA SIMULTÁNEA, CONCURRENTE, SEPARADA O CONSECUTIVAMENTE. DEPENDIENTEMENTE UNO DEL OTRO POR LA VÍA ORAL, INTRAVENOSA, TÓPICA, INSTILACIONES LOCALES, INTRAPERITONEAL O NASAL; USO DE DICHAS COMBINACIONES PARA LA PREPARACIÓN DE UN MEDICAMENTO PARA EL TRATAMIENTO O PROFILAXIS DE UN CÁNCER; UN KIT QUE COMPRENDE ESE TIPO DE COMBINACIÓN; USO DE BIOMARCADORES QUE ES LA PÉRDIDA DEL SUPRESOR TUMORAL PTEN O FBXW7, PARA PREDECIR LA SENSIBILIDAD Y/O LA RESISTENCIA DE UN PACIENTE CON CÁNCER A DICHO COMPUESTO Y PROPORCIONAR UNA DOSIS FUNDAMENTADA PARA AUMENTAR LA SENSIBILIDAD Y/O PARA SOLUCIONAR LA RESISTENCIA; UN MÉTODO PARA DETERMINAR LA PÉRDIDA DEL SUPRESOR TUMORAL PTEN O FBXW7 ; Y UN MÉTODO PARA DETERMINAR PERTURBACIONES EN PIK3CA, PIK3CB, PIK3CD, PIK3CG, PIK3R1, PIK3R2, PIK3R3, PIK3R4, PIK3R5, FGFR1, FGFR2, FGFR3 Y/O FGFR4. PÉRDIDA DE PTEN Y ALTERACIÓN DE PIK3CA, PIK3CB, PIK3CD, PIK3CG, PIK3R1, PIK3R2, PIK3R3, PIK3R4, PIK3R5, FGFR1, FGFR2, FGFR3 Y/O FGFR4.