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1. 发明专利

PH12017501644A1 USE OF SUBSTITUTED 2,3-DIHYDROIMIDAZO[1,2-C]QUINAZOLINES 未知
公开(公告)号：PH12017501644A1
公开(公告)日：2018-03-12
申请号：PH12017501644
申请日：2017-09-08
申请人： BAYER PHARMA AG , BAYER HEALTHCARE PHARMACEUTICALS INC
发明人： LIU NINGSHU , PENA CAROL , JEFFERS MICHAEL , GENVRESSE ISABELLE
IPC分类号： A61K31/519 , A61K45/06 , A61P35/00 , C12Q1/68
摘要： The present invention relates to : - use of a 2,3-dihydroimidazo[1,2-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 1st line, 2nd line, relapsed, refractory, type I or type II 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 1st line, 2nd line, relapsed, refractory, type I or type II 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, PIK3R1, PIK3R2, PIK3R3, PIK3R4, PIK3R5, FGFR1, FGFR2, FGFR3 and/or FGFR4.

2. 发明专利

SG11201707239WA USE OF SUBSTITUTED 2,3-DIHYDROIMIDAZO[1,2-C]QUINAZOLINES 未知
公开(公告)号：SG11201707239WA
公开(公告)日：2017-10-30
申请号：SG11201707239W
申请日：2016-03-07
申请人： BAYER PHARMA AG , BAYER HEALTHCARE PHARMACEUTICALS INC
发明人： LIU NINGSHU , PENA CAROL , JEFFERS MICHAEL , GENVRESSE ISABELLE
IPC分类号： A61K31/519 , A61K45/06 , A61P35/00 , C12Q1/68
摘要： The present invention relates to: use of a 2,3-dihydroimidazo[1,2-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 1st line, 2nd line, relapsed, refractory, type I or type II 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 1st line, 2nd line, relapsed, refractory, type I or type II 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, P1K3R1, PIK3R2, PIK3R3, PIK3R4, PIK3R5, FGFR1, FGFR2, FGFR3 and/or FGFR4.

3. 发明专利

TN2017000385A1 USE OF SUBSTITUTED 2,3-DIHYDROIMIDAZ0[1,2-C]QUINAZOLINES. 未知
公开(公告)号：TN2017000385A1
公开(公告)日：2019-01-16
申请号：TN2017000385
申请日：2016-03-07
申请人： BAYER HEALTHCARE PHARMACEUTICALS INC , BAYER PHARMA AG
发明人： GENVRESSE ISABELLE , JEFFERS MICHAEL , LIU NINGSHU , PENA CAROL
IPC分类号： A61K31/519 , A61K45/06 , A61P35/00 , C12Q1/68
摘要： 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.

4. 发明专利

HK1250645A1 取代的2，3-二氫咪唑並[1，2-C]喹唑啉類化合物的用途未知
公开(公告)号：HK1250645A1
公开(公告)日：2019-01-11
申请号：HK18110118
申请日：2018-08-07
申请人： BAYER PHARMA AG , BAYER HEALTHCARE PHARMACEUTICALS INC
发明人： LIU NINGSHU , PENA CAROL , JEFFERS MICHAEL , GENVRESSE ISABELLE
IPC分类号： A61K20060101 , A61P20060101 , C12Q20060101

5. 发明专利

SV2017005530A COMBINACIONES QUE CONTIENEN 2,3- DIHIDROIMIDAZO[1,2-C]QUINAZOLINA SUSTITUIDA 未知
公开(公告)号：SV2017005530A
公开(公告)日：2018-10-02
申请号：SV2017005530
申请日：2017-09-08
申请人： BAYER PHARMA AG , BAYER HEALTHCARE PHARMACEUTICALS INC
发明人： LIU NINGSHU , PENA CAROL , JEFFERS MICHAEL , GENVRESSE ISABELLE
IPC分类号： A61K31/519 , A61K31/53 , A61K45/06 , A61P35/00 , C12Q1/68
摘要： 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.

6. 发明专利

AU2016231260A1 Use of substituted 2,3-dihydroimidazo[1,2-c]quinazolines 未知
公开(公告)号：AU2016231260A1
公开(公告)日：2017-09-21
申请号：AU2016231260
申请日：2016-03-07
申请人： BAYER HEALTHCARE PHARMACEUTICALS INC , BAYER PHARMA AG
发明人： LIU NINGSHU , PENA CAROL , JEFFERS MICHAEL , GENVRESSE ISABELLE
IPC分类号： A61K31/519 , A61K45/06 , A61P35/00 , C12Q1/68
摘要： The present invention relates to : - use of a 2,3-dihydroimidazo[1,2-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 1st line, 2nd line, relapsed, refractory, type I or type II 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 1st line, 2nd line, relapsed, refractory, type I or type II 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, PIK3R1, PIK3R2, PIK3R3, PIK3R4, PIK3R5, FGFR1, FGFR2, FGFR3 and/or FGFR4.

7. 发明专利

CL2017002284A1 Uso de 2,3–dihidroimidazo[1,2–c]quinazolinas sustituidas. 未知
公开(公告)号：CL2017002284A1
公开(公告)日：2018-05-18
申请号：CL2017002284
申请日：2017-09-08
申请人： BAYER PHARMA AG , BAYER HEALTHCARE PHARMACEUTICALS INC
发明人： LIU NINGSHU , PENA CAROL , JEFFERS MICHAEL , GENVRESSE ISABELLE
IPC分类号： A61K31/519 , A61K45/06 , A61P35/00 , C12Q1/68
摘要： La presente invención se refiere a: – uso de un compuesto de 2,3–dihidroimidazo[1,2–c]quinazolina o de una composición farmacéutica que lo contiene, como un único agente activo o de una combinación de a) dicho compuesto o una composición farmacéutica que contiene dicho compuesto y b) uno o varios otros agentes activos, para la preparación de un medicamento para el tratamiento o la prevención de cáncer de endometrio (de ahora en más en la presente, abreviado como “EC”), en particular EC de primera línea, de segunda línea, recurrente, refractario, de tipo I o de tipo II o endometriosis; – combinaciones de a) dicho compuesto y b) uno o varios otros agentes activos; – una composición farmacéutica que comprende dicho compuesto como un único agente activo para el tratamiento de cáncer de endometrio (de ahora en más en la presente, abreviado como “EC”), en particular EC de primera línea, de segunda línea, recurrente, refractario, de tipo I o de tipo II o endometriosis; – una composición farmacéutica que comprende una combinación de a) dicho compuesto y b) uno o varios otros agentes activos; – uso de biomarcadores que es la pérdida de supresor tumoral PTEN o FBXW7, para predecir la sensibilidad y/o la resistencia de un paciente con cáncer a dicho compuesto y suministro de una dosis racional para incrementar la sensibilidad y/o para superar la resistancia; – un método de determinación de la pérdida de supresor tumoral PTEN o FBXW7; y un método de determinación de perturbaciones en PIK3CA, PIK3CB, PIK3CD, PIK3CG, PIK3R1, PIK3R2, PIK3R3, PIK3R4, PIK3R5, FGFR1, FGFR2, FGFR3 y/o FGFR4; pérdida y alteración de PTEN de PIK3CA, PIK3CB, PIK3CD, PIK3CG, PIK3R1, PIK3R2, PIK3R3, PIK3R4, PIK3R5, FGFR1, FGFR2, FGFR3 y/o FGFR4.

8. 发明专利

AU2016231259A1 Substituted 2,3-dihydroimidazo[1,2-c]quinazoline-containing combinations 未知
公开(公告)号：AU2016231259A1
公开(公告)日：2017-09-21
申请号：AU2016231259
申请日：2016-03-07
申请人： BAYER HEALTHCARE PHARMACEUTICALS INC , BAYER PHARMA AG
发明人： LIU NINGSHU , PENA CAROL , JEFFERS MICHAEL , GENVRESSE ISABELLE
IPC分类号： C12Q1/68 , A61K31/519 , A61K31/53 , A61K45/06 , A61P35/00
摘要： 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 substituted 5-(1-benzothiophen-2-yl)pyrrolo[2,1-f][1,2,4]-triazin-4-amine compounds of general formula (B), or a physiologically acceptable salt, solvate, hydrate or stereoisomer thereof; • 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; * a kit comprising such a combination; * 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, PI K3R1, PIK3R2, PIK3R3, PIK3R4, PIK3R5, FGFR1, FGFR2, FGFR3 and/or FGFR4.

9. 发明专利

SG11201707240SA SUBSTITUTED 2,3-DIHYDROIMIDAZO[1,2-C]QUINAZOLINE-CONTAINING COMBINATIONS 未知
公开(公告)号：SG11201707240SA
公开(公告)日：2017-10-30
申请号：SG11201707240S
申请日：2016-03-07
申请人： BAYER PHARMA AG , BAYER HEALTHCARE PHARMACEUTICALS INC
发明人： LIU NINGSHU , PENA CAROL , JEFFERS MICHAEL , GENVRESSE ISABELLE
IPC分类号： A61K31/519 , C12Q1/68 , A61K31/53 , A61K45/06 , A61P35/00
摘要： 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 substituted 5-(1-benzothiophen-2-yl)pyrrolo[2,1-f][1,2,4]-triazin-4-amine compounds of general formula (B), or a physiologically acceptable salt, solvate, hydrate or stereoisomer thereof; ⋅ 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; * a kit comprising such a combination; * 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, PIK3R1, PIK3R2, PIK3R3, PIK3R4, PIK3R5, FGFR1, FGFR2, FGFR3 and/or FGFR4.

10. 发明专利

CA2978807A1 USE OF SUBSTITUTED 2,3-DIHYDROIMIDAZO[1,2-C]QUINAZOLINES 未知
公开(公告)号：CA2978807A1
公开(公告)日：2016-09-15
申请号：CA2978807
申请日：2016-03-07
申请人： BAYER PHARMA AG , BAYER HEALTHCARE PHARMACEUTICALS INC
发明人： LIU NINGSHU , PENA CAROL , JEFFERS MICHAEL , GENVRESSE ISABELLE
IPC分类号： A61K31/519 , A61K45/06 , A61P35/00 , C12Q1/68
摘要： The present invention relates to : - use of a 2,3-dihydroimidazo[1,2-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 1st line, 2nd line, relapsed, refractory, type I or type II 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 1st line, 2nd line, relapsed, refractory, type I or type II 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, PIK3R1, PIK3R2, PIK3R3, PIK3R4, PIK3R5, FGFR1, FGFR2, FGFR3 and/or FGFR4.

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