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1. 发明申请

US20180055851A1 SUBSTITUTED 2,3-DIHYDROIMIDAZO[1,2-C]QUINAZOLINE-CONTAINING COMBINATIONS 审中-公开
公开(公告)号：US20180055851A1
公开(公告)日：2018-03-01
申请号：US15556908
申请日：2016-03-07
申请人： BAYER PHARMA AKTIENGESELLSCHAFT , BAYER HEALTHCARE PHARMACEUTICALS INC.
发明人： Ningshu LIU , Carol PENA , Michael JEFFERS , Isabelle GENVRESSE
IPC分类号： A61K31/53 , A61K31/5377
CPC分类号： A61K31/53 , A61K31/519 , A61K31/535 , A61K31/5377 , C12Q1/6886 , C12Q2600/156 , C12Q2600/158 , A61K2300/00
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.

2. 发明申请

US20180042929A1 USE OF SUBSTITUTED 2,3-DIHYDROIMIDAZO[1,2-C]QUINAZOLINES 审中-公开
公开(公告)号：US20180042929A1
公开(公告)日：2018-02-15
申请号：US15557036
申请日：2016-03-07
申请人： Bayer Pharma Aktiengesellschaft , Bayer HealthCare Pharmaceuticals Inc.
发明人： Ningshu LIU , Carol PENA , Michael JEFFERS , Isabelle GENVRESSE
IPC分类号： A61K31/519 , C12Q1/68 , A61K31/5377
CPC分类号： A61K31/519 , A61K31/5377 , A61K2300/00 , C12Q1/6886 , C12Q2600/106 , C12Q2600/158
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. 发明申请

WO2016142312A1 SUBSTITUTED 2,3-DIHYDROIMIDAZO[1,2-C]QUINAZOLINE-CONTAINING COMBINATIONS 审中-公开
标题翻译：取代的2,3-二氢吲哚并[1,2-C]喹唑啉的组合
公开(公告)号：WO2016142312A1
公开(公告)日：2016-09-15
申请号：PCT/EP2016/054727
申请日：2016-03-07
申请人： BAYER PHARMA AKTIENGESELLSCHAFT , BAYER HEALTHCARE PHARMACEUTICALS INC.
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
CPC分类号： A61K31/53 , A61K31/519 , A61K31/535 , A61K31/5377 , C12Q1/6886 , C12Q2600/156 , C12Q2600/158 , A61K2300/00
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.
摘要翻译：本发明涉及以下组合：组分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：一种或多种通式（B）的取代的5-（1-苯并噻吩-2-基）吡咯并[2,1-f] [1,2,4] - 三嗪-4-胺化合物，或其生理学上可接受的盐，溶剂化物，水合物或立体异构体; •其中任选的部分或全部组分为药物制剂的形式，其准备用于同时，同时，分别或顺序施用。 •通过口服，静脉内，局部，局部安装，•腹膜内或鼻道相互依赖; *使用这些组合来制备用于治疗或预防癌症的药物; *包含这种组合的试剂盒; *使用作为肿瘤抑制基因PTEN或FBXW7的丧失的生物标志物，用于预测癌症患者对所述化合物的敏感性和/或抗性，并提供基于理论的剂量以增加敏感性和/或克服抗性; *确定肿瘤抑制基因PTEN或FBXW7的损失的方法; 以及用于确定PIK3CA，PIK3CB，PIK3CD，PIK3CG，PIK3R1，PIK3R2，PIK3R3，PIK3R4，PIK3R5，FGFR1，FGFR2，FGFR3和/或FGFR4中的扰动的方法。

4. 发明申请

WO2016142313A1 USE OF SUBSTITUTED 2,3-DIHYDROIMIDAZO[1,2-C]QUINAZOLINES 审中-公开
标题翻译：取代的2,3-二氢吲哚并[1,2-C]喹唑啉的使用
公开(公告)号：WO2016142313A1
公开(公告)日：2016-09-15
申请号：PCT/EP2016/054728
申请日：2016-03-07
申请人： BAYER PHARMA AKTIENGESELLSCHAFT , BAYER HEALTHCARE PHARMACEUTICALS INC.
发明人： LIU, Ningshu , PENA, Carol , JEFFERS, Michael , GENVRESSE, Isabelle
IPC分类号： A61K31/519 , A61P35/00 , A61K45/06 , C12Q1/68
CPC分类号： A61K31/519 , A61K31/5377 , A61K2300/00 , C12Q1/6886 , C12Q2600/106 , C12Q2600/158
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.
摘要翻译：本发明涉及： - 使用2,3-二氢咪唑并[1,2-c]喹唑啉化合物或其包含其的药物组合物作为唯一活性剂，或组合a）所述化合物或含有所述化合物的药物组合物和b）一种或多种其它活性剂，用于制备用于治疗或预防子宫内膜癌（以下简称为“EC”）的药物，特别是第一线，第二系，复发型，难治性类型 I或II型EC或子宫内膜异位症; - a）所述化合物和b）一种或多种其它活性剂的组合; - 包含所述化合物作为治疗子宫内膜癌的唯一活性剂（以下简称为“EC”）的药物组合物，特别是第一线，第二系，复发型，难治性，I型或II型EC或子宫内膜异位症; - 药物组合物，其包含a）所述化合物和b）一种或多种其它活性剂的组合; - 使用作为肿瘤抑制基因PTEN或FBXW7的丧失的生物标志物，用于预测癌症患者对所述化合物的敏感性和/或抗性，并提供基于理论的剂量以增加敏感性和/或克服抗性; - 确定肿瘤抑制基因PTEN或FBXW7的损失的方法; 以及 - 用于确定PIK3CA，PIK3CB，PIK3CD，PIK3CG，PIK3R1，PIK3R2，PIK3R3，PIK3R4，PIK3R5，FGFR1，FGFR2，FGFR3和/或FGFR4中的扰动的方法。

5. 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.

6. 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.

7. 发明专利

CZ2008628A3 N-Heterocyklické deriváty jako inhibitory NOS 未知
公开(公告)号：CZ2008628A3
公开(公告)日：2016-09-29
申请号：CZ2008628
申请日：1998-02-19
申请人： BAYER HEALTHCARE PHARMACEUTICALS INC , PHARMACOPEIA INC
发明人： ARNAIZ DAMIAN O , BALDWIN JOHN J , DAVEY DAVID D , DEVLIN JAMES J , DOLLE ROLAND ELLWOOD III
IPC分类号： C07D401/14 , C07D403/14 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/547 , A61P3/10 , A61P9/00 , A61P9/02 , A61P9/04 , A61P9/08 , A61P9/10 , A61P11/00 , A61P11/06 , A61P17/06 , A61P19/02 , A61P25/00 , A61P25/16 , A61P25/28 , A61P29/00 , A61P31/18 , A61P35/00 , A61P37/00 , A61P37/06 , A61P43/00 , C07D213/00 , C07D233/00 , C07D239/00 , C07D241/02 , C07D265/00 , C07D279/00 , C07D317/44 , C07D319/00 , C07D333/02 , C07D401/04 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D521/00
摘要： Řešení se týká N-heterocyklických derivátů vzorce I a též N-heterocyklů jako inhibitorů syntázy oxidu dusnatého. Též jsou popsány farmaceutické prostředky, obsahující tyto sloučeniny, způsoby jejich použití jako inhibitorů syntázy oxidu dusnatého a jejich syntézy.

8. 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.

9. 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

10. 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.

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