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1. 发明申请

WO2009100690A8 AMOURPHOUS FORM OF THE ADAMANTYLAMINO-PLATINUM ( IV) COMPLEXLA-12 审中-公开
标题翻译：酰胺基 - 铂（IV）络合物-12的一种形式
公开(公告)号：WO2009100690A8
公开(公告)日：2009-12-17
申请号：PCT/CZ2009000013
申请日：2009-02-12
申请人： PLIVA LACHEMA AS , SOVA PETR , KROUTIL ALES , FRANC ALES
发明人： SOVA PETR , KROUTIL ALES , FRANC ALES
IPC分类号： A61K31/282 , A61P35/00 , C07C211/38 , C07F15/00
CPC分类号： C07C211/38 , C07C2603/74 , C07F15/0093
摘要： The present invention relates to the amorphous form of the compound (OC-6-43)- bis(acetato)(1-tricyclo[3,3,1,13,7]decylamine)amminedichloroplatinum(IV), (also called LA-12), methods of preparation, isolation and identification thereof, pharmaceutical compositions containing the same, and the use of such amorphous form and compositions in the treatment of oncological deseases.
摘要翻译：本发明涉及无定形形式的化合物（OC-6-43） - 双（乙酸根）（1-三环[3,3,1,13,7]癸胺）氨基二氯合铂（IV）（也称为LA- 12），其制备方法，分离和鉴定方法，含有其的药物组合物，以及这种无定形形式和组合物在治疗肿瘤疾病中的用途。

2. 发明申请

WO2009100691A1 POLYMORPHIC FORM ( III ) OF THE ADAMANTYLAMINO- PLATINUM (IV) COMPLEX LA- 12 审中-公开
标题翻译：氨基甲酰胺（IV）复合物LA-12的多晶型（III）
公开(公告)号：WO2009100691A1
公开(公告)日：2009-08-20
申请号：PCT/CZ2009/000014
申请日：2009-02-12
申请人： PLIVA-LACHEMA A.S. , SOVA, Petr , KROUTIL, Ales , FRANC, Ales
发明人： SOVA, Petr , KROUTIL, Ales , FRANC, Ales
IPC分类号： C07F15/00 , A61K31/282 , A61P35/00 , C07C211/38
CPC分类号： C07C211/38 , C07C2603/74 , C07F15/0093
摘要： The present invention relates to a novel polymorphic form of the compound (OC-6-43)- bis(acetato)(1-tricyclo[3,3,1,1 3,7 ]decylamine)amminedichloroplatinum(IV) (also called LA-12), methods of preparation, isolation and identification thereof, pharmaceutical compositions containing the same, use of such polymorph and compositions in the treatment of oncological deseases.
摘要翻译：本发明涉及一种新型多晶型化合物（OC-6-43） - 双（乙酸）（1-三环[3,3,1,13,7]癸胺）氨基二氯铂（IV）（也称为LA- 12），其制备方法，分离和鉴定方法，含有该组合物的药物组合物，这些多晶型物和组合物在治疗肿瘤学疾病中的用途。

3. 发明申请

WO2009100688A1 POLYMORPHIC FORM ( I ) OF THE ADAMANTYLAMINO-PLATINUM (IV) COMPLEX LA-12 审中-公开
标题翻译：酰氨基 - 铂（IV）复合物LA-12的多晶型（I）
公开(公告)号：WO2009100688A1
公开(公告)日：2009-08-20
申请号：PCT/CZ2009/000011
申请日：2009-02-12
申请人： PLIVA-LACHEMA A.S. , SOVA, Petr , KROUTIL, Ales , FRANC, Ales
发明人： SOVA, Petr , KROUTIL, Ales , FRANC, Ales
IPC分类号： C07F15/00 , C07C211/38 , A61K31/282 , A61P35/00
CPC分类号： C07F15/0093 , C07B2200/13 , C07C211/65 , C07C2603/74
摘要： The present invention relates to a novel polymorphic form of the compound (OC-6-43)- bis(acetato)(1-tricyclo[3,3,1,1 3,7 ]decylamine)amminedichloroplatinum(IV), (also called LA-12) methods of preparation, isolation and identification thereof, pharmaceutical compositions containing the same, use of such polymorph and compositions in the treatment of oncological deseases.
摘要翻译：本发明涉及一种新型多晶型的化合物（OC-6-43） - 双（乙酸）（1-三环[3,3,1,13,7]癸胺）氨基二氯铂（IV）（也称为LA -12）制备方法，分离和鉴定方法，含有该组合物的药物组合物，这些多晶型物和组合物在治疗肿瘤学疾病中的用途。

4. 发明申请

WO2008099160A1 SOLID ORAL DOSAGE FORM CONTAINING BICALUTAMIDE AND METHOD OF PREPARATION 审中-公开
标题翻译：含有贝他丁胺的固体口服剂型及其制备方法
公开(公告)号：WO2008099160A1
公开(公告)日：2008-08-21
申请号：PCT/GB2008/000484
申请日：2008-02-12
申请人： PLIVA HRVASTKA D.O.O. , BUCKS, Teresa, Anne , FRANC, Ales , GONEC, Roman , PETROVICOVA, Anna , ZALUDEK, Borek
发明人： FRANC, Ales , GONEC, Roman , PETROVICOVA, Anna , ZALUDEK, Borek
IPC分类号： A61K9/26 , A61K9/32 , A61K9/16 , A61K31/277
CPC分类号： A61K31/277 , A61K9/2054 , A61K9/2059 , A61K9/2077
摘要： A tablet comprising bicalutamide and a method for its production.
摘要翻译：包含比卡鲁胺的片剂及其制备方法。

5. 发明申请

WO2007147371B1 PHARMACEUTICAL COMPOSITION FOR ORAL ADMINISTRATION 审中-公开
标题翻译：口服给药的药物组合物
公开(公告)号：WO2007147371B1
公开(公告)日：2008-06-19
申请号：PCT/CZ2007000058
申请日：2007-06-20
申请人： PLIVA LACHEMA AS , FRANC ALES , SOVA PETR
发明人： FRANC ALES , SOVA PETR
IPC分类号： A61K9/10 , A61K9/48 , A61K31/282 , A61K33/24 , A61P35/00 , C07F15/00
CPC分类号： A61K47/14 , A61K9/10 , A61K9/4858 , A61K31/282 , A61K33/24
摘要： An oral pharmaceutical composition characterized in that it consists of a suspension of a platinum complex of general formula I, wherein A and A' independently of one another are an NH 3 group or an amino or diamino group containing 1 to 18 carbon atoms, B and B' independently of one another are a halogen atom or a hydroxy group or are an -0-C(O)-R or an -0-C(O)-R' group wherein R and R' independently of one another are hydrogen atom, an alkyl, alkenyl, aryl, aralkyl, alkylamino or alkoxy group which groups contain 1 to 10 carbon atoms, or functional derivatives of these groups, X and X' independently of one another are a halogen atom or a monocarboxylate group containing 1 to 20 carbon atoms, or X and X' together form a dicarboxylate group containing 2 to 20 carbon atoms, in at least one pharmaceutically acceptable vegetable, animal, mineral, synthetic or semisynthetic oil and/or in at least one pharmaceutically acceptable vegetable, animal, mineral, synthetic or semisynthetic oily substance, in which suspension the content of the platinum complex of general formula I is 0.5 to 50 % by weight based on the total weight of the composition, and which suspension optionally contains at least one pharmaceutically acceptable excipient.
摘要翻译：一种口服药物组合物，其特征在于它由通式I的铂配合物的悬浮液组成，其中A和A'彼此独立地是NH 3基团或含1个氨基或二氨基的基团至18个碳原子，B和B'彼此独立地为卤素原子或羟基或为-OC（O）-R或-OC（O）-R'基团，其中R和R 彼此独立地为氢原子，含1-10个碳原子的烷基，烯基，芳基，芳烷基，烷基氨基或烷氧基或这些基团的官能化衍生物，X和X'彼此独立地为卤原子或至少一种药学上可接受的植物油，动物油，矿物油，合成油或半合成油和/或至少一种可药用植物油和/或至少一种含有1至20个碳原子的单羧酸盐基团，或X和X'一起形成含有2至20个碳原子的二羧酸盐基团一种药学上可接受的植物，动物，矿物，合成或半合成物其中悬浮液中通式I的铂配合物的含量基于组合物的总重量为0.5至50重量％，并且该悬浮液任选地含有至少一种药学上可接受的赋形剂。

6. 发明申请

WO2007147373A3 PHARMACEUTICAL COMPOSITION FOR INJECTIONAL, PARTICULARLY TARGETED LOCAL ADMINISTRATION 审中-公开
标题翻译：注射用药物组合物，特别针对地方管理
公开(公告)号：WO2007147373A3
公开(公告)日：2008-03-13
申请号：PCT/CZ2007000060
申请日：2007-06-20
申请人： PLIVA LACHEMA AS , FRANC ALES , SOVA PETR
发明人： FRANC ALES , SOVA PETR
IPC分类号： A61K33/24 , C07F15/00
CPC分类号： A61K9/0019 , A61K31/282 , A61K33/24 , A61K47/26 , A61K47/38
摘要： The invention relates to a pharmaceutical composition for injectional, in particular targeted local administration, characterized in that it comprises a sterile suspension of platinum complex of general formula (I), wherein A and A' independently of one another are an NH 3 group or an amino or diamino group containing 1 to 18 carbon atoms, B and B' independently of one another are a halogen atom or a hydroxy group or are an -0-C(O)-R or an -0-C(O)-R' group wherein R and R' independently of one another are hydrogen atom, an alkyl, alkenyl, aryl, aralkyl, alkylamino or alkoxy group which groups contain 1 to 10 carbon atoms, or functional derivatives of these groups, X and X' independently of one another are a halogen atom or a monocarboxylate group containing 1 to 20 carbon atoms, or X and X' together form a dicarboxylate group containing 2 to 20 carbon atoms, in a pharmaceutically acceptable hydrophilic or hydrophobic injection liquid phase, 100 % of particles of the platinum complex of general formula I being of size smaller than 250 µm.
摘要翻译：本发明涉及用于注射，特别是靶向局部给药的药物组合物，其特征在于其包含通式（I）的铂络合物的无菌悬浮液，其中A和A'彼此独立地为NH 3 或含有1至18个碳原子的氨基或二氨基，B和B'彼此独立地为卤素原子或羟基或为-OC（O）-R或-O -C（O）-R'基团，其中R和R'彼此独立地为氢原子，含有1-10个碳原子的烷基，烯基，芳基，芳烷基，烷基氨基或烷氧基或这些基团的官能衍生物中，X和X'彼此独立地为卤素原子或含有1至20个碳原子的单羧酸根基团，或者X和X'一起形成含有2至20个碳原子的二羧酸根基团，在药学上可接受的亲水或疏水注射液体相，100％的铂颗粒通式I的配合物尺寸小于250μm。

7. 发明申请

WO2007147372A2 PHARMACEUTICAL COMPOSITION FOR ADMINISTRATION BY INJECTION 审中-公开
标题翻译：用于注射管理的药物组合物
公开(公告)号：WO2007147372A2
公开(公告)日：2007-12-27
申请号：PCT/CZ2007000059
申请日：2007-06-20
申请人： PLIVA LACHEMA AS , FRANC ALES , SOVA PETR
发明人： FRANC ALES , SOVA PETR
IPC分类号： A61K31/282 , A61K9/08 , A61K47/40 , A61K47/48
CPC分类号： A61K9/0019 , A61K9/19 , A61K31/282 , A61K33/24 , A61K47/40 , A61K47/6951 , B82Y5/00
摘要： A pharmaceutical composition for administration by injection, comprising a mixture of platinum complex of general formula (I), wherein A and A' independently of one another are an NH 3 group or an amino or diamino group containing 1 to 18 carbon atoms, B and B' independently of one another are a halogen atom or a hydroxy group or are an -0-C(O)-R or -0-C(O)-R' group wherein R and R' independently of one another are a hydrogen atom or an alkyl, alkenyl, aryl, aralkyl, alkylamino or alkoxy group, which groups contain 1 to 10 carbon atoms, or functional derivatives of these groups, X and X' independently of one another are a halogen atom or a monocarboxylate group containing 1 to 20 carbon atoms, or X and X' together form a dicarboxylate group containing 2 to 20 carbon atoms, and of at least one cyclodextrin and/or at least one cyclodextrin derivative, and optionally of at least one pharmaceutically acceptable excipient.
摘要翻译：一种通过注射给药的药物组合物，其包含通式（I）的铂络合物的混合物，其中A和A'彼此独立地为NH 3基团或含有1个氨基或二氨基的化合物至18个碳原子，B和B'彼此独立地是卤素原子或羟基，或者是-O-C（O）-R或-O-C（O）-R'基团，其中R和R' 相互独立的是氢原子或这些基团含有1至10个碳原子的烷基，烯基，芳基，芳烷基，烷基氨基或烷氧基，或这些基团的官能衍生物，X和X'彼此独立地是卤素原子或含有1至20个碳原子的单羧酸酯基，或X和X'一起形成含有2至20个碳原子的二羧酸酯基，和至少一种环糊精和/或至少一种环糊精衍生物，以及任选的至少一种药学上可接受的赋形剂。

8. 发明申请

WO2007091059A1 PREPARATION AND COMPOSITION OF A SOLID DOSAGE FORM CONTAINING TACROLIMUS AND/OR SIROLIMUS 审中-公开
标题翻译：含有TACROLIMUS和/或SIROLIMUS的固体剂型的制备和组合
公开(公告)号：WO2007091059A1
公开(公告)日：2007-08-16
申请号：PCT/GB2007/000422
申请日：2007-02-06
申请人： PLIVA ISTRAZIVANJE I RAZVOJ D.O.O. , MCLEISH, Nicholas, Alistair, Maxwell , FRANC, Ales , ZALUDEK, Borek , GONEC, Roman , CIRKVA, Ales , MALOVANA, Sabina , PETROVICOVA, Anna
发明人： FRANC, Ales , ZALUDEK, Borek , GONEC, Roman , CIRKVA, Ales , MALOVANA, Sabina , PETROVICOVA, Anna
IPC分类号： A61K9/20 , A61K9/48 , A61K31/436
CPC分类号： A61K9/2054 , A61K9/2027 , A61K9/2059 , A61K9/4866 , A61K31/436
摘要： A method is provided for preparing a solid dosage form comprising a water-insoluble medicinally active substance selected from tacrolimus and sirolimus, whereby the medicinally active substance is dissolved in an organic solvent, a mixture comprising at least one pharmaceutically acceptable carrier with swelling ability is then coated with the solvent containing the medicinally active substance, the solvent is evaporated, and the mixture is processed into a suitable solid dosage form.
摘要翻译：提供了一种制备包含选自他克莫司和西罗莫司的水不溶性药物活性物质的固体剂型的方法，由此将药物活性物质溶解在有机溶剂中，然后将包含至少一种具有溶胀能力的药学上可接受的载体的混合物涂覆含有药物活性物质的溶剂，蒸发溶剂，并将混合物加工成合适的固体剂型。

9. 发明申请

WO2004087126A1 PHARMACEUTICAL COMPOSITION CONTAINING PLATINUM COMPLEX AS ACTIVE SUBSTANCE AND METHOD OF MANUFACTURING THEREOF 审中-公开
标题翻译：含有作为活性物质的铂复合物的药物组合物及其制备方法
公开(公告)号：WO2004087126A1
公开(公告)日：2004-10-14
申请号：PCT/CZ2004/000017
申请日：2004-03-30
申请人： PLIVA-LACHEMA A.S. , FRANC Ales , SOVa Peter
发明人： FRANC Ales , SOVa Peter
IPC分类号： A61K31/282
CPC分类号： A61K31/282 , A61K9/1623 , A61K9/2013 , A61K9/2846 , A61K9/2866 , A61K9/2886 , A61K9/4808 , A61K9/4891 , A61K9/5015 , A61K9/5026 , A61K9/5042 , A61K9/5047 , A61K9/5057 , A61K9/5073
摘要： The invention relates to a pharmaceutical composition containing the platinum complex of formula (I) as an active substance where A, A', B, B', X and X' have specific meanings, in a mixture with at least one pharmaceutically acceptable excipient, characterized in that it is formed of a granulate with particles smaller than 0.5 mm in size prepared by wet granulation of a mixture of platinum complex of tetravalent platinum of formula (I) wetted by water, at least one neutral saccharide and at least one native and/or modified polysaccharide, being optionally contained in a capsule or a sack or being optionally pressed into the form of a tablet, while the surface of the granulate, the capsule or the tablet is optionally coated with a layer of at least one pharmaceutically acceptable substance enabling enterosolvent dissolution of the active substance in bowels only and/or at least one pharmaceutically acceptable substance enabling the controlled release of the active substance. The invention relates also to a method of manufacturing of said pharmaceutical composition.
摘要翻译：本发明涉及在与至少一种药学上可接受的赋形剂的混合物中含有式（I）的铂络合物作为活性物质的方法，其中A，A'，B，B'，X和X'具有特定含义，其特征在于，其由粒径小于0.5mm的颗粒形成，颗粒通过湿法造粒由水润湿的至少一种中性糖和至少一种天然的式（I）的四价铂的四价铂络合物的混合物制备， /或修饰的多糖，任选地包含在胶囊或袋中或任选地压制成片剂形式，同时颗粒，胶囊或片剂的表面任选地涂覆有至少一种药学上可接受的物质使得活性物质仅在肠中的肠溶溶解溶解和/或使得能够控制活性物质释放的至少一种药学上可接受的物质。本发明还涉及制备所述药物组合物的方法。

10. 发明申请

WO2007147371A3 PHARMACEUTICAL COMPOSITION FOR ORAL ADMINISTRATION 审中-公开
标题翻译：用于口服管理的药物组合物
公开(公告)号：WO2007147371A3
公开(公告)日：2008-04-17
申请号：PCT/CZ2007000058
申请日：2007-06-20
申请人： PLIVA LACHEMA AS , FRANC ALES , SOVA PETR
发明人： FRANC ALES , SOVA PETR
IPC分类号： A61K9/10 , A61K9/48 , A61K31/282 , A61K33/24 , A61P35/00 , C07F15/00
CPC分类号： A61K47/14 , A61K9/10 , A61K9/4858 , A61K31/282 , A61K33/24
摘要： An oral pharmaceutical composition characterized in that it consists of a suspension of a platinum complex of general formula I, wherein A and A' independently of one another are an NH 3 group or an amino or diamino group containing 1 to 18 carbon atoms, B and B' independently of one another are a halogen atom or a hydroxy group or are an -0-C(O)-R or an -0-C(O)-R' group wherein R and R' independently of one another are hydrogen atom, an alkyl, alkenyl, aryl, aralkyl, alkylamino or alkoxy group which groups contain 1 to 10 carbon atoms, or functional derivatives of these groups, X and X' independently of one another are a halogen atom or a monocarboxylate group containing 1 to 20 carbon atoms, or X and X' together form a dicarboxylate group containing 2 to 20 carbon atoms, in at least one pharmaceutically acceptable vegetable, animal, mineral, synthetic or semisynthetic oil and/or in at least one pharmaceutically acceptable vegetable, animal, mineral, synthetic or semisynthetic oily substance, in which suspension the content of the platinum complex of general formula I is 0.5 to 50 % by weight based on the total weight of the composition, and which suspension optionally contains at least one pharmaceutically acceptable excipient.
摘要翻译：一种口服药物组合物，其特征在于其由通式I的铂络合物的悬浮液组成，其中A和A'彼此独立地为NH 3基团或含有1个氨基或二氨基的1 至18个碳原子，B和B'彼此独立地是卤素原子或羟基，或者是-O-C（O）-R或-O-C（O）-R'基团，其中R和R “独立地是氢原子，含有1-10个碳原子的烷基，烯基，芳基，芳烷基，烷基氨基或烷氧基，或这些基团的官能衍生物，X和X'彼此独立地是卤素原子或含有1至20个碳原子的单羧酸酯基，或X和X'在至少一种药学上可接受的植物，动物，矿物，合成或半合成油中和/或至少在一起形成含有2-20个碳原子的二羧酸酯基一种药学上可接受的植物，动物，矿物，合成或半合成其中悬浮液中通式I的铂络合物的含量基于组合物的总重量为0.5至50重量％，并且该悬浮液任选地含有至少一种药学上可接受的赋形剂。

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