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1. 发明申请

WO2012131079A1 COMPOUNDS INHIBITING GALECTIN-1 EXPRESSION, CANCER CELL PROLIFERATION, INVASION, AND TUMORIGENESIS 审中-公开
标题翻译：化合物抑制GALECTIN-1表达，癌细胞增殖，入侵和肿瘤发生
公开(公告)号：WO2012131079A1
公开(公告)日：2012-10-04
申请号：PCT/EP2012/055902
申请日：2012-03-30
申请人： ONCOETHIX , RAYMOND, Eric , ASTORGUES-XERRI, Lucile , FAIVRE, Sandrine , CVITKOVIC, Esteban
发明人： RAYMOND, Eric , ASTORGUES-XERRI, Lucile , FAIVRE, Sandrine , CVITKOVIC, Esteban
IPC分类号： A61K31/00 , A61K31/165 , A61P35/00
CPC分类号： A61K31/165 , A61K31/00 , A61K45/06 , A61K2300/00
摘要： Disclosed herein are compositions comprising a galectin-1-targeting compound in a therapeutically effective composition for treating cancer. In an aspect, a galectin-1-targeting compound is OTX-008. Also disclosed herein are methods of making and using such compositions.
摘要翻译：本文公开了包含用于治疗癌症的治疗有效组合物中的半乳凝素-1-靶向化合物的组合物。一方面，半乳凝素-1-靶向化合物是OTX-008。本文还公开了制备和使用这些组合物的方法。

2. 发明申请

WO2009050143A1 COMBINATIONS OF (1R, 2R, 3S, 4S) -N4- (3-AMINOCARBONYLBICYCLO [2. 2. 1] HEPT-5-ENE-2-YL) - 5-FLUORO-N2- [ ( 3 - METHYL-4- (4 -METHYLPIPERAZIN-1-YL] PHENYL-2, 4-PYRIMIDINEAMINE 审中-公开
标题翻译：（1R，2R，3S，4S）-N4-（3-氨基羰基双环[2.2.1] HEPT-5-ENE-2-YL）-5-氟-N 2 - [（3-甲基-4- （4-甲基哌嗪-1-基）苯基] -2,4-吡啶胺
公开(公告)号：WO2009050143A1
公开(公告)日：2009-04-23
申请号：PCT/EP2008/063729
申请日：2008-10-13
申请人： MERCK SERONO S.A. , ROMANELLI, Angela , GIANELLA-BORRADORI, Athos , RAYMOND, Eric , SEROVA, Maria , FAIVRE, Sandrine
发明人： ROMANELLI, Angela , GIANELLA-BORRADORI, Athos , RAYMOND, Eric , SEROVA, Maria , FAIVRE, Sandrine
IPC分类号： A61K31/506 , A61K31/44 , A61K31/517 , A61K39/395 , A61P35/00
CPC分类号： A61K45/06 , A61K31/44 , A61K31/506 , A61K31/517 , A61K39/39558 , A61K2300/00
摘要： The invention relates to combinations of (1 R,2R,3S,4S)-N4-(3- aminocarbonylbicyclo[2.2.1]hept-5-ene-2-yl)-5-fluoro-N2-[(3-nnethyl-4-(4- methylpiperazin-1 -yl)]phenyl-2,4-pyrimidinediamine and/or its physiologically acceptable salts and solvates, and other cancer therapeutics, and the use of such combinations for the treatment of cancer.
摘要翻译：本发明涉及（1R，2R，3S，4S）-N4-（3-氨基羰基双环[2.2.1]庚-5-烯-2-基）-5-氟-N 2 - [（3-甲基 -4-（4-甲基哌嗪-1-基）]苯基-2,4-嘧啶二胺和/或其生理上可接受的盐和溶剂合物，以及其它癌症治疗剂，以及这些组合用于治疗癌症的用途。

3. 发明申请

WO2015078929A1 METHOD OF TREATING LEUKEMIA USING PHARMACEUTICAL FORMULATION CONTAINING THIENOTRIAZOLODIAZEPINE COMPOUNDS 审中-公开
标题翻译：使用含有噻唑烷酮化合物的药物制剂治疗白喉病的方法
公开(公告)号：WO2015078929A1
公开(公告)日：2015-06-04
申请号：PCT/EP2014/075709
申请日：2014-11-26
申请人： ONCOETHIX SA , RIVEIRO, Maria, E. , RAYMOND, Eric
发明人： RIVEIRO, Maria, E. , RAYMOND, Eric
IPC分类号： A61K31/551 , A61K9/14 , A61K9/16 , A61K47/02 , A61K47/32 , A61K9/10 , A61K47/38 , A61K9/48 , A61P35/02 , A61K45/06 , A61K31/436 , A61K31/167 , A61K31/4045 , A61K31/519 , A61K31/573
CPC分类号： A61K31/5517 , A61K9/10 , A61K9/146 , A61K9/4866 , A61K31/167 , A61K31/4045 , A61K31/436 , A61K31/519 , A61K31/573 , A61K31/704 , A61K31/706 , A61K31/7068 , A61K45/06 , A61K47/38 , A61K2300/00
摘要： A method of treating leukemia in a mammal by administering a solid dispersion comprising an amorphous thienotriazolodiazepine compound of the Formula (1) wherein R 1 is alkyl having a carbon number of 1-4, R 2 is a hydrogen atom; a halogen atom; or alkyl having a carbon number of 1-4 optionally substituted by a halogen atom or a hydroxyl group, R 3 is a halogen atom; phenyl optionally substituted by a halogen atom, alkyl having a carbon number of 1-4, alkoxy having a carbon number of 1-4 or cyano; —NR 5 —(CH 2 ) m —R 6 wherein R 5 is a hydrogen atom or alkyl having a carbon number of 1-4, m is an integer of 0-4, and R 6 is phenyl or pyridyl optionally substituted by a halogen atom; or —NR 7 —CO—(CH 2 ) n —R 8 wherein R 7 is a hydrogen atom or alkyl having a carbon number of 1-4, n is an integer of 0-2, and R 8 is phenyl or pyridyl optionally substituted by a halogen atom, and R 4 is —(CH 2 ) a —CO—NH—R 9 wherein a is an integer of 1-4, and R 9 is alkyl having a carbon number of 1-4; hydroxyalkyl having a carbon number of 1-4; alkoxy having a carbon number of 1-4; or phenyl or pyridyl optionally substituted by alkyl having a carbon number of 1-4, alkoxy having a carbon number of 1-4, amino or a hydroxyl group or —(CH 2 ) b —COOR 10 wherein b is an integer of 1-4, and R 10 is alkyl having a carbon number of 1-4, or a pharmaceutically acceptable salt thereof or a hydrate or solvate thereof.
摘要翻译：一种通过施用包含式（1）的无定形噻吩并三唑并基噻嗪化合物的固体分散体来治疗哺乳动物的白血病的方法，其中R1是碳数为1-4的烷基，R2是氢原子; 卤素原子; 或任选被卤素原子或羟基取代的碳数为1-4的烷基，R 3为卤素原子; 任选被卤素原子取代的苯基，碳数为1-4的烷基，碳数为1-4的烷氧基或氰基; -NR5-（CH2）m -R6，其中R5是氢原子或碳数为1-4的烷基，m为0-4的整数，R6为任选被卤素原子取代的苯基或吡啶基; 或-NR7-CO-（CH2）n-R8，其中R7是氢原子或碳数为1-4的烷基，n为0-2的整数，R8为苯基或任选被卤素原子取代的吡啶基 R 4为 - （CH 2）a -CO-NH-R 9，其中a为1-4的整数，R 9为碳数为1-4的烷基; 碳数为1-4的羟烷基; 碳数为1-4的烷氧基; 或任选被碳数为1-4的烷基，碳数为1-4的烷氧基，氨基或羟基或 - （CH 2）b -COOR 10取代的苯基或吡啶基，其中b为1-4的整数，且R 10为碳数为1-4的烷基或其药学上可接受的盐或其水合物或溶剂合物。

4. 发明申请

WO2015189814A1 METHOD OF TREATING NON-SMALL CELL LUNG CANCER AND/OR SMALL CELL LUNG CANCER USING THIENOTRIAZOLODIAZEPINE COMPOUNDS 审中-公开
标题翻译：治疗非小细胞肺癌和/或小细胞肺癌的方法使用噻吗啉二酮化合物
公开(公告)号：WO2015189814A1
公开(公告)日：2015-12-17
申请号：PCT/IB2015/054457
申请日：2015-06-12
申请人： ONCOETHIX GMBH
发明人： RIVEIRO, Maria Eugenia , RAYMOND, Eric , BERTONI, Francesco
IPC分类号： A61K31/551 , A61K9/14 , A61K9/16 , A61K47/02 , A61K47/32 , A61K9/10 , A61K47/38 , A61K9/48 , A61P35/00 , A61K45/06 , A61K31/436 , A61K31/4545
CPC分类号： A61K31/551 , A61K9/0019 , A61K9/0053 , A61K9/08 , A61K9/10 , A61K9/146 , A61K9/1652 , A61K9/48 , A61K9/4858 , A61K9/4866 , A61K31/436 , A61K31/4545 , A61K45/06 , A61K47/02 , A61K47/32 , A61K47/38 , A61K2300/00
摘要： A method of treating non-small cell lung cancer and/or small cell lung cancer in a mammal comprises the step of administering to a patient a pharmaceutical acceptable amount of a compound being a thienotriazolodiazepine compound of the Formula (1).
摘要翻译：在哺乳动物中治疗非小细胞肺癌和/或小细胞肺癌的方法包括给予患者药物可接受量的化合物为式（1）的噻吩并三氮唑并氮杂化合物的步骤。

5. 发明申请

WO2009109649A1 IMPROVED ANTITUMORAL TREATMENTS 审中-公开
标题翻译：改善抗肿瘤治疗
公开(公告)号：WO2009109649A1
公开(公告)日：2009-09-11
申请号：PCT/EP2009/052649
申请日：2009-03-06
申请人： PHARMA MAR, S.A. , RAMÓN Y CAJAL AGÜERAS, Santiago , HERNÁNDEZ LOSA, Javier , JIMENO DOÑAQUE, José Mª , RAYMOND, Eric
发明人： RAMÓN Y CAJAL AGÜERAS, Santiago , HERNÁNDEZ LOSA, Javier , JIMENO DOÑAQUE, José Mª , RAYMOND, Eric
IPC分类号： A61K38/15 , A61K33/24 , A61K31/7068 , A61K31/337 , A61K31/282 , A61K31/505 , A61K31/495 , A61K31/436 , A61K31/404
CPC分类号： A61K31/7068 , A61K31/282 , A61K31/337 , A61K31/404 , A61K31/436 , A61K31/495 , A61K31/505 , A61K33/24 , A61K38/15 , A61K45/06 , A61K2300/00
摘要： The present invention relates to combinations of PM02734 with another anticancer drug selected from Cisplatin, Gemcitabine, Paclitaxel, Oxaliplatin, 5-Fluorouracil, Trabectedin, Rapamycin, and Sunitinib, and the use of these combinations in the treatment of cancer.
摘要翻译：本发明涉及PM02734与选自顺铂，吉西他滨，紫杉醇，奥沙利铂，5-氟尿嘧啶，曲马替丁，雷帕霉素和舒尼替尼的另一种抗癌药物的组合，以及这些组合在癌症治疗中的应用。

6. 发明申请

WO2015078928A1 METHOD OF TREATING NON-SMALL-CELL LUNG CANCER USING PHARMACEUTICAL FORMULATION CONTAINING THIENOTRIAZOLODIAZEPINE COMPOUNDS 审中-公开
标题翻译：使用含有三苯并噻唑啉酮化合物的药物制剂治疗非小细胞肺癌的方法
公开(公告)号：WO2015078928A1
公开(公告)日：2015-06-04
申请号：PCT/EP2014/075707
申请日：2014-11-26
申请人： ONCOETHIX SA
发明人： RIVEIRO, Maria E. , RAYMOND, Eric
IPC分类号： A61K31/551 , A61K9/14 , A61K9/16 , A61K47/02 , A61K47/32 , A61K9/10 , A61K47/38 , A61K9/48 , A61P35/00 , A61K45/06 , A61K31/436 , A61K31/4545
CPC分类号： A61K31/551 , A61K9/0019 , A61K9/10 , A61K9/146 , A61K9/1635 , A61K9/1641 , A61K9/1652 , A61K9/4816 , A61K9/4866 , A61K9/5078 , A61K31/436 , A61K31/4545 , A61K45/06 , A61K47/38 , A61K2300/00
摘要： A method of treating non-small cell lung cancer in a mammal by administering to a patient a pharmaceutically acceptable amount of a compound being a thienotriazolodiazepine compound of the Formula (1) wherein R 1 is alkyl having a carbon number of 1-4, R 2 is a hydrogen atom; a halogen atom; or alkyl having a carbon number of 1-4 optionally substituted by a halogen atom or a hydroxyl group, R 3 is a halogen atom; phenyl optionally substituted by a halogen atom, alkyl having a carbon number of 1- 4, alkoxy having a carbon number of 1-4 or cyano;— NR 5 — (CH 2 ) m — R 6 wherein R 5 is a hydrogen atom or alkyl having a carbon number of 1-4, m is an integer of 0-4, and R 6 is phenyl or pyridyl optionally substituted by a halogen atom; or -NR 7 — CO— (CH 2 ) n — R 8 wherein R 7 is a hydrogen atom or alkyl having a carbon number of 1-4, n is an integer of 0-2, and R 8 is phenyl or pyridyl optionally substituted by a halogen atom, and R 4 is— (CH 2 ) a — CO— NH— R 9 wherein a is an integer of 1-4, and R 9 is alkyl having a carbon number of 1-4; hydroxyalkyl having a carbon number of 1-4; alkoxy having a carbon number of 1-4; or phenyl or pyridyl optionally substituted by alkyl having a carbon number of 1-4, alkoxy having a carbon number of 1-4, amino or a hydroxyl group or— (CH 2 ) b — COOR 10 wherein b is an integer of 1-4, and R 10 is alkyl having a carbon number of 1-4, or a pharmaceutically acceptable salt thereof or a hydrate or solvate thereof.
摘要翻译：一种治疗哺乳动物中非小细胞肺癌的方法，其通过向患者施用药学上可接受量的化合物，其为式（1）的噻吩并三氮唑并氮杂化合物，其中R 1为碳数为1-4的烷基，R 2为氢原子; 卤素原子; 或任选被卤素原子或羟基取代的碳数为1-4的烷基，R 3为卤素原子; 任选被卤素原子取代的苯基，碳数为1-4的烷基，碳数为1-4的烷氧基或氰基; -NR5-（CH2）m -R6，其中R5为氢原子或具有碳原子的烷基数1-4，m为0-4的整数，R6为任选被卤素原子取代的苯基或吡啶基; 或-NR 7 -CO-（CH 2）n -R 8，其中R 7是氢原子或碳数为1-4的烷基，n为0-2的整数，R 8为苯基或任选被卤素原子取代的吡啶基，R 4为 - （CH 2）a -CO-NH-R 9，其中a为1-4的整数，并且R 9为碳数为1-4的烷基; 碳数为1-4的羟烷基; 碳数为1-4的烷氧基; 或任选被碳数为1-4的烷基，碳数为1-4的烷氧基，氨基或羟基或 - （CH 2）b -COOR 10任意取代的苯基或吡啶基，其中b为1-4的整数，且R 10为碳数为1-4的烷基或其药学上可接受的盐或其水合物或溶剂合物。

7. 发明申请

WO2015018523A1 A NOVEL BET-BRD INHIBITOR FOR TREATMENT OF SOLID TUMORS 审中-公开
标题翻译：一种用于治疗固体肿瘤的新型BETBBR抑制剂
公开(公告)号：WO2015018523A1
公开(公告)日：2015-02-12
申请号：PCT/EP2014/002166
申请日：2014-08-06
申请人： ONCOETHIX SA
发明人： RAYMOND, Eric , RIVEIRO, Maria, E.
IPC分类号： A61K31/5517 , A61P35/00
CPC分类号： A61K9/4866 , A61K9/0019 , A61K9/0056 , A61K9/10 , A61K9/1635 , A61K9/1652 , A61K31/551
摘要： A method of treating a solid in a mammal comprising the step of: administering a pharmaceutical acceptable amount of a thienotriazolodiazepine compound being represented by the following Formula (1): wherein R 1 is alkyl having a carbon number of 1-4, R 2 is a hydrogen atom; a halogen atom; or alkyl having a carbon number of 1-4 optionally substituted by a halogen atom or a hydroxyl group, R 3 is a halogen atom; phenyl optionally substituted by a halogen atom, alkyl having a carbon number of 1 -4, alkoxy having a carbon number of 1-4 or cyano;— NR 5 — (CH 2 )m— R 6 wherein R 5 is a hydrogen atom or alkyl having a carbon number of 1-4, m is an integer of 0-4, and R 6 is phenyl or pyridyl optionally substituted by a halogen atom; or -NR 7— CO— (CH 2 ) n — R 8 wherein R 7 is a hydrogen atom or alkyl having a carbon number of 1-4, n is an integer of 0-2, and R 8 is phenyl or pyridyl optionally substituted by a halogen atom, and R 4 is — (CH 2 ) a — CO— NH— R 9 wherein a is an integer of 1-4, and R 9 is alkyl having a carbon number of 1-4; hydroxyalkyl having a carbon number of 1-4; alkoxy having a carbon number of 1-4; or phenyl or pyridyl optionally substituted by alkyl having a carbon number of 1-4, alkoxy having a carbon number of 1-4, amino or a hydroxyl group or— (CH 2 ) b — COOR 10 wherein b is an integer of 1-4, and R 10 is alkyl having a carbon number of 1-4, or a pharmaceutically acceptable salt thereof or a hydrate or solvate thereof.
摘要翻译：一种治疗哺乳动物固体的方法，包括以下步骤：施用药物可接受量的由下式（1）表示的噻吩并三唑并氮杂化合物：其中R 1为碳数为1-4的烷基，R 2为氢原子; 卤素原子; 或任选被卤素原子或羟基取代的碳数为1-4的烷基，R 3为卤素原子; 任选被卤素原子取代的苯基，碳数为1-4的烷基，碳数为1-4的烷氧基或氰基; -NR5-（CH2）m -R6，其中R5为氢原子或具有碳原子的烷基数1-4，m为0-4的整数，R6为任选被卤素原子取代的苯基或吡啶基; 或-NR 7 -CO-（CH 2）n -R 8，其中R 7为氢原子或碳数为1-4的烷基，n为0-2的整数，R8为任选被卤素取代的苯基或吡啶基并且R 4是 - （CH 2）a -CO-NH-R 9，其中a是1-4的整数，并且R 9是碳数为1-4的烷基; 碳数为1-4的羟烷基; 碳数为1-4的烷氧基; 或任选被碳数为1-4的烷基，碳数为1-4的烷氧基，氨基或羟基或 - （CH 2）b -COOR 10任意取代的苯基或吡啶基，其中b为1-4的整数，且R 10为碳数为1-4的烷基或其药学上可接受的盐或其水合物或溶剂合物。

8. 发明申请

WO2007054731A1 ANTIPROLIFERATIVE COMBINATION COMPRISING CYC-682 AND A CYTOTOXIC AGENT 审中-公开
标题翻译：包含CYC-682和CYTOTOXIC AGENT的抗菌组合
公开(公告)号：WO2007054731A1
公开(公告)日：2007-05-18
申请号：PCT/GB2006/004230
申请日：2006-11-13
申请人： CYCLACEL LIMITED , GREEN, Simon , FLEMING, Ian , RAYMOND, Eric
发明人： GREEN, Simon , FLEMING, Ian , RAYMOND, Eric
IPC分类号： A61K45/06 , A61K31/7068 , A61P35/00
CPC分类号： A61K45/06 , A61K31/7068 , Y02A50/411
摘要： A first aspect of the invention relates to a combination comprising 2'-cyano-2'-deoxy-N4-palmitoyl-l-beta-D-arabinofuranosyl-cytosine, or a metabolite thereof, or a pharmaceutically acceptable salt thereof, and a cytotoxic agent selected from (a) a vinca alkaloid; (b) a taxane; (c) a cytosine analogue; (d) an anthracycline; and (e) a platinum antineoplastic agent. A second aspect of the invention relates to a pharmaceutical product comprising the above combination as a combined preparation for simultaneous, sequential or separate use in therapy. A third aspect of the invention relates to a method for treating a proliferative disorder, said method comprising simultaneously, sequentially or separately administering the above combination.
摘要翻译：本发明的第一方面涉及包含2'-氰基-2'-脱氧-N4-棕榈酰-1-β-D-阿拉伯呋喃糖基 - 胞嘧啶或其代谢物或其药学上可接受的盐和细胞毒性选自（a）长春花生物碱的试剂; （b）紫杉烷; （c）胞嘧啶类似物; （d）蒽环类; 和（e）铂抗肿瘤剂。本发明的第二方面涉及包含上述组合作为用于在治疗中同时，连续或分开使用的组合制剂的药物产品。本发明的第三方面涉及一种治疗增殖性病症的方法，所述方法同时依次或分别施用上述组合。

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