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1. 发明申请

WO1992011267A1 NOVEL METHYLENEBISPHOSPHONIC ACID DERIVATIVES 审中-公开
标题翻译：新型亚甲基双膦酸衍生物
公开(公告)号：WO1992011267A1
公开(公告)日：1992-07-09
申请号：PCT/FI1991000394
申请日：1991-12-18
申请人： HUHTAMÄKI OY , NIKANDER, Hannu , HEIKKILÄ-HOIKKA, Marjaana , POHJALA, Esko , HANHIJÄRVI, Hannu , LAUREN, Leena
发明人： HUHTAMÄKI OY
IPC分类号： C07F09/40
CPC分类号： C07F9/5537 , C07F9/4025
摘要： Novel pharmacologically active methylenebisphosphonates having formula (I) wherein R , R , R and R independently are straight or branched, optionally unsaturated C1-C10-alkyl, optionally unsaturated C3-C10-cycloalkyl, aryl, aralkyl, silyl SiR3 or hydrogen, whereby in formula (I) at least one of the groups R , R , R and R is hydrogen and at least one of the groups is different from hydrogen, Q is hydrogen, hydroxyl, halogen, amino NH2, or OR', wherein R' is C1-C4-lower alkyl or acyl, Q is straight or branched, optionally unsaturated C1-C10-alkyl, -hydroxyalkyl or -aminoalkyl, whereby the oxygen may, as a substituent, contain one group or the nitrogen as a substituent may contain one or two groups, which are C1-C4-lower alkyl or acyl, or the two substituents of the nitrogen form together with the nitrogen atom a saturated, partly saturated or an aromatic heterocyclic ring, or Q is optionally substituted and optionally unsaturated C3-C10-cycloalkyl, which optionally is bound to the molecule over a straight or branched alkylene group containing 1-4 C-atoms, including the stereoisomers, such as the geometrical isomers and the optically active isomers, of the compounds, as well as the pharmacologically acceptable salts of these compounds.
摘要翻译：具有式（I）的新的药理活性亚甲基二膦酸酯，其中R 1，R 2，R 3和R 4独立地是直链或支链的，任选不饱和的C 1 -C 10 - 烷基，任选不饱和的C 3 -C 10 - 环烷基，芳基，芳烷基，甲硅烷基SiR 3或氢，其中在式（I）中，基团R 1，R 2，R 3和R 4中的至少一个是氢和至少一个基团不同于氢，Q 1是氢，羟基，卤素，氨基NH 2或OR'，其中R'是C 1 -C 4 - 低级烷基或酰基，Q 2是直链或支链的，任选不饱和的C1-C10 - 烷基， - 羟烷基或 - 氨基烷基，其中氧可以作为取代基含有一个基团，或者氮作为取代基可以含有一个或两个基团，它们是C 1 -C 4 - 低级烷基或酰基，或两个取代基氮原子与氮原子一起饱和，部分饱和或芳族杂环，或Q 2是任选取代的和任选不饱和的C 3 -C 10 - 环烷基，其优选在包含1-4个C原子的直链或支链亚烷基上，包括立体异构体，如化合物的几何异构体和旋光异构体，以及这些化合物的药理学上可接受的盐。

2. 发明申请

WO1995033466A1 PYRIDYLBISPHOSPHONATES FOR USE AS A THERAPEUTICAL AGENT 审中-公开
标题翻译：吡啶二磷酸盐作为治疗药物使用
公开(公告)号：WO1995033466A1
公开(公告)日：1995-12-14
申请号：PCT/FI1995000315
申请日：1995-06-02
申请人： LEIRAS OY , HEIKKILÄ-HOIKKA, Marjaana , NIKANDER, Hannu , HANNUNIEMI, Ritva , LAURÉN, Leena , KLEIMOLA, Terttu , LIUKKO-SIPI, Sirpi , VÄÄNÄNEN, Kalervo , SELLMAN, Raija
发明人： LEIRAS OY
IPC分类号： A61K31/675
CPC分类号： A61K31/683 , A61K31/675
摘要： The present invention relates to certain optionally ring substituted pyridinylaminomethylidene bisphosphonic acid tetralkyl esters (I) and their use for the treatment of bone diseases, such as osteolytic bone diseases due to malignancy, Paget's disease and primary and secondary osteoporosis.
摘要翻译：本发明涉及某些任选环取代的吡啶基氨基亚甲基双膦酸四烷基酯（I）及其用于治疗由于恶性肿瘤引起的溶骨性骨疾病，佩吉特氏病和原发性和继发性骨质疏松症等骨疾病的用途。

3. 发明申请

WO2009122016A1 AN INTRAUTERINE SYSTEM 审中-公开
标题翻译：内脏系统
公开(公告)号：WO2009122016A1
公开(公告)日：2009-10-08
申请号：PCT/FI2009/050244
申请日：2009-04-01
申请人： BAYER SCHERING PHARMA OY , KORTESUO, Pirjo , CALVO ALONSO, Ulla , INKI, Pirjo , JUKARAINEN, Harri , JUTILA, Ilkka , LEHTINEN, Juha , LUKKARI-LAX, Eeva , LYYTIKÄINEN, Heikki , MOEDE, Joachim , NIKANDER, Hannu , SALLINEN, Pirjo , TJÄDER, Taina , MacLEOD, Andrew , NOBLE, Michael , WHITAKER, David
发明人： KORTESUO, Pirjo , CALVO ALONSO, Ulla , INKI, Pirjo , JUKARAINEN, Harri , JUTILA, Ilkka , LEHTINEN, Juha , LUKKARI-LAX, Eeva , LYYTIKÄINEN, Heikki , MOEDE, Joachim , NIKANDER, Hannu , SALLINEN, Pirjo , TJÄDER, Taina , MacLEOD, Andrew , NOBLE, Michael , WHITAKER, David
IPC分类号： A61F6/14
CPC分类号： A61F6/142 , A61B34/20 , A61B90/39 , A61B2034/2065 , A61F6/18
摘要： The present invention relates to novel intrauterine systems and to methods for manufacturing these systems. An intrauterine system according to the invention comprises a reservoir and a continuous, closed and flexible frame.
摘要翻译：本发明涉及新颖的子宫内系统和用于制造这些系统的方法。根据本发明的子宫内系统包括储存器和连续的，封闭且柔性的框架。

4. 发明申请

WO2009066006A1 VAGINAL DELIVERY SYSTEM 审中-公开
标题翻译： VAGINAL交付系统
公开(公告)号：WO2009066006A1
公开(公告)日：2009-05-28
申请号：PCT/FI2008/050670
申请日：2008-11-19
申请人： BAYER SCHERING PHARMA OY , TALLING, Christine , HANES, Vladimir , KEINÄNEN, Antti , HOLMBERG, Svante , NIKANDER, Hannu
发明人： TALLING, Christine , HANES, Vladimir , KEINÄNEN, Antti , HOLMBERG, Svante , NIKANDER, Hannu
IPC分类号： A61K9/00 , A61K31/00 , A61K31/56
CPC分类号： A61K31/56 , A61K9/0036 , A61K31/565 , A61K31/585 , A61K2300/00
摘要： The present invention is related to an intravaginal delivery system for the controlled release of drospirenone and an estrogen, optionally also comprising one or more therapeutically active or a health-promoting substance capable of giving and/or enhancing protection against bacterial and fungal infections, and/or enhancing protection against sexually transmitted diseases. The delivery system consists of one or more compartments (2, 4, 5), one of each comprising a core (7) and a membrane (3) encasing the core, said core and membrane essentially consisting of a same or different polymer composition, wherein at least one compartment comprises drospirenone ant at least one compartment which may be the same or different from the one comprising drospirenone, comprises an estrogen or a mixture of drospirenone and an estrogen, and wherein the membrane or the surface of the membrane or at least one of the cores comprises said therapeutically active or a health-promoting substance.
摘要翻译：本发明涉及用于控制释放屈螺酮和雌激素的阴道内递送系统，任选地还包含一种或多种治疗活性或健康促进物质，其能够给予和/或增强针对细菌和真菌感染的保护作用，和/ 或加强对性传播疾病的保护。输送系统由一个或多个隔室（2,4,5）组成，每个隔室包括芯（7）和包围芯的膜（3），所述芯和膜基本上由相同或不同的聚合物组合物组成，其中至少一个隔室包含屈螺酮蚂蚁，至少一个与包含屈螺酮的药物相同或不同的隔室，包含雌激素或屈螺酮和雌激素的混合物，并且其中所述膜或膜表面至少核心之一包括所述治疗活性物质或健康促进物质。

5. 发明申请

WO1992011269A1 NOVEL METHYLENEBISPHOSPHONIC ACID DERIVATIVES 审中-公开
标题翻译：新型亚甲基双膦酸衍生物
公开(公告)号：WO1992011269A1
公开(公告)日：1992-07-09
申请号：PCT/FI1991000395
申请日：1991-12-18
申请人： HUHTAMÄKI OY , POHJALA, Esko , HEIKKILÄ-HOIKKA, Marjaana , NIKANDER, Hannu , HANHIJÄRVI, Hannu
发明人： HUHTAMÄKI OY
IPC分类号： C07F09/58
CPC分类号： C07F9/4025 , C07F9/58
摘要： Novel pharmacologically active methylenebisphosphonates having formula (I) wherein R -R independently are C1-C10-alkyl, C3-C10-cycloalkyl, aryl, aralkyl, silyl SiR3 or hydrogen, whereby in formula (I) at least one of the groups R -R is hydrogen and at least one of the groups R -R is different from hydrogen, Q is hydrogen, hydroxyl, halogen, amino NH2, or OR'1, wherein R'1 is C1-C4-alkyl or acyl, Q is the group ( alpha ) wherein Y is a six-membered heterocyclic group, or a carbocyclic aromatic group, X is a bond, O, S or NR''', wherein R''' is hydrogen, lower alkyl, or acyl, n is the integer 0 to 6, and R' and R" are hydrogen or lower alkyl provided that as a ring atom of the ring Y and/or a chain atom of the group X, there is always at least one heteroatom from the group of O, N and S, including the stereoisomers and the salts of the compounds.
摘要翻译：具有式（I）的新的药理活性亚甲基双膦酸酯，其中R 1 -R 4独立地是C 1 -C 10 - 烷基，C 3 -C 10 - 环烷基，芳基，芳烷基，甲硅烷基SiR 3或氢，其中式（I）至少基团R 1 -R 4之一是氢，并且基团R 1 -R 4中的至少一个不同于氢，Q 1是氢，羟基，卤素，氨基NH 2，或OR 1，其中R 1是C 1 -C 4烷基或酰基，Q 2是其中Y是六元杂环基或碳环芳基，X是键，O ，S或NR“'，其中R”'是氢，低级烷基或酰基，n是整数0至6，并且R'和R“是氢或低级烷基，条件是作为环的环原子 Y和/或X基团的链原子，总是存在至少一个来自O，N和S基团的杂原子，包括立体异构体和化合物的盐。

6. 发明申请

WO1988007041A1 ISOQUINOLINE DERIVATIVES, THEIR MANUFACTURE AND USE 审中-公开
标题翻译： ISOQUINOLINE衍生物，其制造和使用
公开(公告)号：WO1988007041A1
公开(公告)日：1988-09-22
申请号：PCT/FI1987000032
申请日：1987-03-12
申请人： HUHTAMÄKI OY , ALLONEN, Hannu , NIKANDER, Hannu
发明人： HUHTAMÄKI OY
IPC分类号： C07D401/04
CPC分类号： C07D401/04 , C07D401/06
摘要： The invention relates to dihydro- and tetrahydroisoquinolines and their physiologically acceptable salts of formula (I) or (I'), in which formulae A is -CH= or -N=, n is 0 or 1, R1 and R2 are the same or different and designate H, halogen, OH, a C1-C4 alkoxy, R3 is H when R1 and R2 are H, or halogen or a C1-C6 alkyl group, R4 is halogen, a C1-C6 alkyl group or designates an amino group of formula (II), where R5 and R6 are the same or different and designate H or a C1-C3 alkyl group which can be substituted with a phenyl group substituted with one or two lower alkoxy, and R4 can also be H when A is -N=. The invention also relates to a method for preparing same whereby an amide of formula (III), where R1-R4 and A have the above significance, is cyclisized with Lewis acid; and the use of compounds of the formula (I) or (I') or their physiologically acceptable derivatives or salts as therapeutical agents.
摘要翻译：本发明涉及式（I）或（I'）的二氢和四氢异喹啉及其生理上可接受的盐，其中式A为-CH =或-N =，n为0或1，R 1和R 2为相同或不同，表示H，卤素，OH，C1-C4烷氧基，当R1和R2为H时，R3为H，或为卤素或C1-C6烷基，R4为卤素，C1-C6烷基或氨基（II）的化合物，其中R 5和R 6相同或不同，并且表示H或可被被一个或两个低级烷氧基取代的苯基取代的C 1 -C 3烷基，当A为 -N =。本发明还涉及其制备方法，其中式（III）的酰胺，其中R 1 -R 4和A具有上述含义，用路易斯酸进行环化; 以及使用式（I）或（I'）化合物或其生理上可接受的衍生物或盐作为治疗剂。

7. 发明申请

WO2011039418A1 AN INTRAUTERINE SYSTEM 审中-公开
标题翻译：输入系统
公开(公告)号：WO2011039418A1
公开(公告)日：2011-04-07
申请号：PCT/FI2010/050753
申请日：2010-09-30
申请人： BAYER SCHERING PHARMA OY , TJÄDER, Taina , CALVO ALONSO, Ulla , INKI, Pirjo , JUKARAINEN, Harri , JUTILA, Ilkka , KORTESUO, Pirjo , LEHTINEN, Juha , LUKKARI-LAX, Eeva , LYYTIKÄINEN, Heikki , MOEDE, Joachim , NIKANDER, Hannu , SALLINEN, Pirjo , SHAFIQ, Faisal , KAUFHOLD, Wolfgang , WAMPRECHT, Christian
发明人： TJÄDER, Taina , CALVO ALONSO, Ulla , INKI, Pirjo , JUKARAINEN, Harri , JUTILA, Ilkka , KORTESUO, Pirjo , LEHTINEN, Juha , LUKKARI-LAX, Eeva , LYYTIKÄINEN, Heikki , MOEDE, Joachim , NIKANDER, Hannu , SALLINEN, Pirjo , SHAFIQ, Faisal , KAUFHOLD, Wolfgang , WAMPRECHT, Christian
IPC分类号： A61F6/14 , A61K9/00
CPC分类号： A61F6/142 , A61K9/0039
摘要： The present invention relates to novel intrauterine systems and to methods for manufacturing these systems. An intrauterine system according to the invention comprises a reservoir and a continuous, closed and flexible frame. The frame comprises a thermoplastic polyurethane elastomer made of a polycarbonate diol, 1,6-hexamethylenediisocyanate, and a chain extender.
摘要翻译：本发明涉及新颖的子宫内系统和用于制造这些系统的方法。根据本发明的子宫内系统包括储存器和连续的，封闭且柔性的框架。框架包括由聚碳酸酯二醇，1,6-六亚甲基二异氰酸酯和扩链剂制成的热塑性聚氨酯弹性体。

8. 发明申请

WO1988007991A1 NOVEL SULFONAMIDES, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THESE NEW SULFONAMIDES 审中-公开
标题翻译：新型磺胺类，其制备和含有这些新磺酰胺的药物组合物的方法
公开(公告)号：WO1988007991A1
公开(公告)日：1988-10-20
申请号：PCT/FI1988000043
申请日：1988-03-29
申请人： HUHTAMÄKI OY , ANDERSEN, Lars , KANGASAHO, Mauno , NIKANDER, Hannu
发明人： HUHTAMÄKI OY
IPC分类号： C07D209/48
CPC分类号： C07D209/48 , C07D401/12
摘要： The invention relates to new 2-Phthalimidoethanesulfone-N-arylamides, methods for their preparation pharmaceutical compositions containing this new compound as well as the therapeutic use of the new compound. These new compounds have formula (I), wherein n = 1-4 and R1 is hydrogen or an alkyl or a hydroxyalkyl group having 1-6 carbon atoms, R2 is a) phenyl or substituted phenyl or b) formula (II), wherein Z = O, N or S.
摘要翻译：本发明涉及新的2-邻苯二甲酰亚氨基乙烷磺酰-N-芳基酰胺，其制备方法包含该新化合物的药物组合物以及新化合物的治疗用途。这些新化合物具有式（I），其中n = 1-4且R 1是氢或具有1-6个碳原子的烷基或羟烷基，R 2是a）苯基或取代的苯基或b）式（II），其中 Z = O，N或S.

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