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1. 发明申请

WO1995013054A1 PROCESS FOR PREPARING A CLODRONATE PREPARATION 审中-公开
标题翻译：制备氯仿制剂的方法
公开(公告)号：WO1995013054A1
公开(公告)日：1995-05-18
申请号：PCT/FI1994000509
申请日：1994-11-11
申请人： LEIRAS OY , POHJALA, Esko , NUPPONEN, Heikki , LEHMUSSAARI, Kari
发明人： LEIRAS OY
IPC分类号： A61K09/16
CPC分类号： A61K31/663 , A61K9/0095 , A61K9/1688 , A61K9/2054 , A61K9/4858 , A61K9/5042 , A61K31/66
摘要： The object of the invention is a process for preparing a clodronate preparation which process is characterized in that clodronate is crystallized as disodium clodronate tetrahydrate from an aqueous solution of disodium clodronate; the resulting disodium clodronate tetrahydrate is dry granulated by compressing in such a way that the crystal structure of the disodium clodronate tetrahydrate is preserved and by crumbling and screening the mass to granules of a suitable size; the dry granulated disodium clodronate tetrahydrate is optionally mixed with suitable excipients, such as filling agents and gliding agents and, if necessary, disintegrants.
摘要翻译：本发明的目的是制备氯膦酸盐制剂的方法，该方法的特征在于氯膦酸盐从氯代膦酸二钠的水溶液中结晶为氯四膦酸二钠四水合物; 所得到的氯四膦酸四水合物二钠通过压缩干燥造粒，使得氯二膦酸二钠四水合物的晶体结构得以保存，并且将物质粉碎并筛分成适合尺寸的颗粒; 任选地将干粒状氯膦酸二钠四水合物与合适的赋形剂混合，例如填充剂和滑动剂，如果需要，与崩解剂混合。

2. 发明申请

WO1995000144A1 COMPOSITION FOR OPHTHALMIC USE 审中-公开
标题翻译：眼用组合物
公开(公告)号：WO1995000144A1
公开(公告)日：1995-01-05
申请号：PCT/FI1994000270
申请日：1994-06-17
申请人： LEIRAS OY , URTTI, Arto , JÄRVINEN, Tomi , SUHONEN, Pekka , LEHMUSSAARI, Kari , REUNAMÄKI, Timo , ALARANTA, Sakari , OKSALA, Olli , POHJALA, Esko , HANHIJÄRVI, Hannu
发明人： LEIRAS OY
IPC分类号： A61K31/415
CPC分类号： B82Y5/00 , A61K9/0048 , A61K31/415 , A61K47/40 , A61K47/6951
摘要： The present invention relates to a composition for the topical administration of bispilocarpic acid diesters to the eye in the form of an aqueous solution, which includes cyclodextrin and optionally a viscosity and enhancing and pH-adjusting agent.
摘要翻译：本发明涉及一种以水溶液形式向眼睛局部施用双糖皮质二酯的组合物，其包括环糊精和任选的粘度和增强和pH调节剂。

3. 发明申请

WO1995026711A1 OPHTHALMIC COMPOSITION WITH DECREASED VISCOSITY 审中-公开
标题翻译：具有降低粘度的眼底组合物
公开(公告)号：WO1995026711A1
公开(公告)日：1995-10-12
申请号：PCT/FI1995000166
申请日：1995-03-29
申请人： LEIRAS OY , REUNAMÄKI, Timo , LEHMUSSAARI, Kari , VARTIAINEN, Eija , OKSALA, Olli , ALARANTA, Sakari , POHJALA, ESKO
发明人： LEIRAS OY
IPC分类号： A61K09/00
CPC分类号： A61K9/0048 , Y10S514/912
摘要： The present invention is directed to an ophthalmic composition in the form of a topical aqueous solution consisting essentially of: an ophthalmologically active agent, an ion sensitive, hydrophilic polymer in an amount of 0.004 to 1.5 % by weight, at least one salt selected from the group of inorganic salts and buffers in a total amount of from 0.01 to 2.0 % by weight, a wetting agent in an amount of 0 to 3.0 % by weight, a preservative in an amount of 0 to 0.02 % by weight, water, and optionally a pH regulating agent in an amount sufficient to give a pH of 4.0 to 8.0 to the composition, the ratio between salt and polymer components being such that the solution exhibits a viscosity of less than 1000 mPas. The composition contains a sufficient amount of polymer to provide for a controlled absorption of the drug into the eye, its viscosity having been reduced to provide for better handling characteristics.
摘要翻译：本发明涉及一种局部水溶液形式的眼用组合物，其基本上由以下组成：眼科活性剂，0.004至1.5重量％的离子敏感性亲水性聚合物，至少一种选自组合的无机盐和缓冲剂的总量为0.01-2.0重量％，润湿剂的量为0-3.0重量％，防腐剂的量为0至0.02重量％，水和任选地一种pH调节剂，其量足以使组合物的pH为4.0-8.0，盐和聚合物组分之间的比例使溶液的粘度小于1000mPa·s。组合物含有足够量的聚合物以提供药物对眼睛的受控吸收，其粘度已经降低以提供更好的处理特性。

4. 发明申请

WO1995026712A1 OPHTHALMIC COMPOSITION CONTAINING AN ION SENSITIVE, HYDROPHILIC POLYMER AND AN INORGANIC SALT IN A RATIO WHICH GIVES LOW VISCOSITY 审中-公开
标题翻译：含有敏感性的亲水性组合物，水解聚合物和无机盐在低粘度的比例
公开(公告)号：WO1995026712A1
公开(公告)日：1995-10-12
申请号：PCT/FI1995000167
申请日：1995-03-29
申请人： LEIRAS OY , LEHMUSSAARI, Kari , VARTIAINEN, Eija , REUNAMÄKI, Timo , OKSALA, Olli , ALARANTA, Sakari , POHJALA, Esko
发明人： LEIRAS OY
IPC分类号： A61K09/00
CPC分类号： A61K9/0048 , A61K47/32 , Y10S514/912
摘要： The present invention is directed to an ophthalmic composition in the form of a topical aqueous solution consisting essentially of: an ophthalmologically active agent containing basic groups, an ion sensitive, hydrophilic polymer containing acidic groups in an amount of 0.004 to 1.5 % by weight, at least one salt selected from the group of inorganic salts and buffers in a total amount of from 0.01 to 2.0 % by weight, and optionally a wetting agent and a preservative, the ratio between salt and polymer being such that the solution exhibits a viscosity of less than 1000 mPas, and the pH of the solution is 4.0 to 8.0. The composition contains a sufficient amount of polymer to provide for a controlled absorption of the drug into the eye, its viscosity having been reduced to provide for better handling characteristics.
摘要翻译：本发明涉及一种局部水溶液形式的眼用组合物，其基本上由以下组成：含有碱性基团的眼科活性剂，含有0.004至1.5重量％的酸性基团的离子敏感的亲水性聚合物，选自无机盐和缓冲剂组中的至少一种盐，其总量为0.01至2.0重量％，以及任选的润湿剂和防腐剂，盐和聚合物之间的比例使得溶液表现出较小的粘度超过1000mPas，溶液的pH为4.0〜8.0。组合物含有足够量的聚合物以提供药物对眼睛的受控吸收，其粘度已经降低以提供更好的处理特性。

5. 发明申请

WO1995000143A1 COMPOSITION FOR OPHTHALMIC USE 审中-公开
标题翻译：眼用组合物
公开(公告)号：WO1995000143A1
公开(公告)日：1995-01-05
申请号：PCT/FI1994000269
申请日：1994-06-17
申请人： LEIRAS OY , JÄRVINEN, Tomi , URTTI, Arto , SUHONEN, Pekka , PEURA, Pekka , LEHMUSSAARI, Kari , REUNAMÄKI, Timo , ALARANTA, Sakari , OKSALA, Olli , POHJALA, Esko , HANHIJÄRVI, Hannu
发明人： LEIRAS OY
IPC分类号： A61K31/415
CPC分类号： A61K9/0048 , A61K31/415
摘要： The present invention relates to a composition for the topical administration of bispilocarpic acid diesters to the eye in the form of an aqueous solution, which includes a viscosity enhancing agent and a buffer, and which has a pH of 3-6.
摘要翻译：本发明涉及一种以水溶液形式向眼睛局部施用双糖皮质二酯的组合物，其包括粘度增强剂和缓冲剂，其pH为3-6。

6. 发明申请

WO1993024466A1 NOVEL PILOCARPINE DERIVATIVES AND PROCESS FOR THEIR PREPARATION 审中-公开
标题翻译：新型吡啶衍生物及其制备方法
公开(公告)号：WO1993024466A1
公开(公告)日：1993-12-09
申请号：PCT/FI1993000226
申请日：1993-05-26
申请人： LEIRAS OY , JÄRVINEN, Tomi , PEURA, Pekka , SUHONEN, Pekka , URTTI, Arto , HANHIJÄRVI, Hannu , POHJALA, Esko
发明人： LEIRAS OY
IPC分类号： C07D233/64
CPC分类号： C07D233/64
摘要： The object of the invention are pharmaceutically useful bispilocarpic acid ester derivatives of general formula (I), wherein Y is -C(=O)-R, wherein R is C1-C4-alkyl, C3-C6-cycloalkyl or phenyl, whereby W is a group of formula (Ia), or Y is a group of formula (Ib), whereby W is R', which is C1-C4-alkyl or C3-C6-cycloalkyl, wherein Y has the meaning given above, and A is a direct bond or a methylene group, which can be substituted with hydroxy, the group Y-O- wherein Y has the meaning given, or with one or two methyl groups, and B is a direct bond, methylene or ethylene, and their acid addition salts.
摘要翻译：本发明的目的是药学上有用的通式（I）的双壳糖酸酯衍生物，其中Y是-C（= O）-R，其中R是C 1 -C 4烷基，C 3 -C 6环烷基或苯基，由此W 是式（Ia）的基团，或Y是式（Ib）的基团，其中W是R'，它是C1-C4-烷基或C3-C6-环烷基，其中Y具有上面给出的含义，A 是直接键或亚甲基，其可以被羟基取代，YO-基团，其中Y具有给定的含义，或与一个或两个甲基，B是直接键，亚甲基或亚乙基，以及它们的酸加成盐。

7. 发明申请

WO1994004134A1 OPHTHALMOLOGICAL PREPARATION 审中-公开
标题翻译：眼科准备
公开(公告)号：WO1994004134A1
公开(公告)日：1994-03-03
申请号：PCT/FI1993000326
申请日：1993-08-18
申请人： LEIRAS OY , LEHMUSSAARI, Kari , OKSALA, Olli , REUNAMÄKI, Timo
发明人： LEIRAS OY
IPC分类号： A61K09/08
CPC分类号： A61K9/0048 , Y10S514/912
摘要： The present invention relates to an eye drop formulation, which, in combination, comprises pilocarpine and a further agent for the treatment of ocular hypertension, as well as an ophthalmologically acceptable carrier and optionally further, ophthalmologically acceptable adjuvants. The formulation is characterized in that the pH thereof is from 3.5 to 5.8 and the viscosity is from 10 to 25000 mPas. The invention also relates to the preparation of the said formulation, as well as its use for the treatment of ocular hypertension and glaucoma.
摘要翻译：本发明涉及一种眼药水制剂，其组合包含毛果芸香碱和用于治疗高眼压症的另外的药剂，以及眼科学上可接受的载体和任选的其它眼科学上可接受的佐剂。该制剂的特征在于其pH为3.5至5.8，粘度为10至25000mPas。本发明还涉及所述制剂的制备及其用于治疗高眼压症和青光眼的用途。

8. 发明申请

WO1995031969A1 PHARMACEUTICAL COMPOSITIONS DERIVED FROM MICROELMULSION-BASED GELS, METHOD FOR THEIR PREPARATION AND NEW MICROEMULSION-BASED GELS 审中-公开
标题翻译：由基于微胶囊的凝胶衍生的药物组合物，其制备方法和新的基于微乳液的凝胶
公开(公告)号：WO1995031969A1
公开(公告)日：1995-11-30
申请号：PCT/FI1995000234
申请日：1995-04-28
申请人： LEIRAS OY , BACKLUND, Sune , ERIKSSON, Folke , RANTALA, Maria , RANTALA, Pertti , VARHO, Kari
发明人： LEIRAS OY
IPC分类号： A61K09/107
CPC分类号： A61K9/06 , A61K9/1075 , Y10S514/937 , Y10S514/938 , Y10S514/944
摘要： The invention relates to a pharmaceutical composition comprising a microemulsion made up of a hydrophilic component, a lipophilic component, a surfactant and a drug, wherein the hydrophilic component, the lipophilic component and the surfactant form, when examined on a macroscopic scale, a one-phase solution. The hydrophilic component is dispersed as colloidal droplets in the lipophilic component, or the lipophilic component is dispersed as colloidal droplets in the hydrophilic component. According to still another alternative the hydrophilic and the lipophilic components form a microemulsion with bicontinuous structure wherein said components form elongated adjacent channels. The drug is dissolved in the dispersed component or, in case of a microemulsion with a bicontinuous structure, in the hydrophilic or the lipophilic component. The microemulsion is stabilized by means of the surfactant. It is characteristic that a gelatinizer and water are added to the microemulsion thereby bringing the microemulsion into a gel form.
摘要翻译：本发明涉及一种药物组合物，其包含由亲水组分，亲脂性组分，表面活性剂和药物组成的微乳液，其中亲水组分，亲油性组分和表面活性剂形式在宏观尺度上检查时，相溶液。亲水性成分作为胶体液滴分散在亲油性成分中，或者亲油性成分作为胶体液滴分散在亲水性成分中。根据另一替代方案，亲水和亲油组分形成具有双连续结构的微乳液，其中所述组分形成细长的相邻通道。将该药物溶解在分散组分中，或在具有双连续结构的微乳液的情况下溶解在亲水或亲油组分中。微乳液通过表面活性剂稳定。特征在于，将微凝胶和水加入到微乳液中，从而使微乳液成为凝胶形式。

9. 发明申请

WO1994003144A1 AN EQUIPMENT FOR PROVIDING A MEDICINE ROD WITH A SHELL 审中-公开
标题翻译：用于提供带有壳的药物棒的设备
公开(公告)号：WO1994003144A1
公开(公告)日：1994-02-17
申请号：PCT/FI1993000297
申请日：1993-07-14
申请人： LEIRAS OY
发明人： LEIRAS OY , HELLE, Timo , HARTZELL, Rolf , NIEMINEN, Pekka , LANKINEN, Pekka
IPC分类号： A61J03/00
CPC分类号： A61M31/00 , A61F6/14 , A61J3/00 , Y10S53/90 , Y10T29/53526
摘要： The invention relates to providing a medicinal rod with a shell. The shell is formed from a hose, which is expanded by pressurizing its inner space. The medicinal rod is pushed into the expanded hose, after which the pressure is relieved. The hose tightens over the rod after the pressure relief.
摘要翻译：本发明涉及提供具有外壳的药棒。壳体由软管形成，软管通过对其内部空间进行加压而膨胀。将药棒推入膨胀软管中，然后释放压力。压力释放后，软管在杆上收紧。

10. 发明申请

WO1992016629A1 PROCESS FOR THE PRODUCTION OF ANTIBIOTICS, DNA-SEQUENCES, RECOMBINANT-DNA-CONSTRUCTS AND MICROBIAL STRAINS USED THEREIN 审中-公开
标题翻译：生产抗生素，DNA序列，重组DNA构建体及其使用的微生物菌株的方法
公开(公告)号：WO1992016629A1
公开(公告)日：1992-10-01
申请号：PCT/FI1992000084
申请日：1992-03-23
申请人： LEIRAS OY , NIEMI, Jarmo , HAKALA, Juha , KOPIO, Anja , PÄRSSINEN, Raimo , YLIHONKO, Kristiina , LAMPI, Klaus
发明人： LEIRAS OY
IPC分类号： C12N15/31
CPC分类号： C12R1/465 , C12N15/52 , C12P19/56
摘要： The invention concerns a process according to which by means of known microorganisms of the Streptomyces-genus, by transferring into them specific genes from certain microbial strains which produce structurally closely related antibiotics, such antibiotics of the anthracycline group are biotechnically produced, which these microorganisms do not produce naturally. The invention concerns also microorganisms needed in such a process and formed by recombinant-DNA-technology, recombinant-DNA-constructions and DNA-sequences needed therein. The invention belongs to the field of biotechnical production of antibiotics and relates to the application of hybrid antibiotic technology to antibiotics of the anthracycline group.
摘要翻译：本发明涉及一种方法，根据该方法，通过将已知的链霉菌微生物转移到产生结构紧密相关的抗生素的某些微生物菌株中，这些抗生素的蒽环类抗生素生物技术生产这些微生物不自然产生。本发明还涉及这种方法中需要的微生物，并通过重组DNA技术，重组DNA构建和DNA序列形成。本发明属于抗生素生物技术生产领域，涉及将蒽环类抗生素应用于复合抗生素技术。

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