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21. 发明申请

WO01030788A1 NOVEL SALTS OF 4-AMINO-1-HYDROXYBUTYLIDENE-1,1-BISPHOSPHONIC ACID, THEIR PREPARATION AND USE 审中-公开
标题翻译： 4-氨基-1-羟基丁基-1,1-二磷酸的新型盐，其制备和使用
公开(公告)号：WO01030788A1
公开(公告)日：2001-05-03
申请号：PCT/DK2000/000589
申请日：2000-10-24
IPC分类号： A61P13/04 , A61P19/08 , C07F9/38 , A61K31/663
CPC分类号： C07F9/3873
摘要： The monopotassium salt of 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid and hydrates thereof, particularly the monohydrate and the dihydrate, pharmaceutical preparations containing such salts as active ingredient, a method for preparing them and their use for treatment or prophylaxis of diseases relating to the calcium metabolism are described.
摘要翻译： 4-氨基-1-羟基亚丁基-1,1-二膦酸的单钾盐及其水合物，特别是一水合物和二水合物，含有活性成分的盐的药物制剂，其制备方法及其用于治疗或预防的用途描述了与钙代谢有关的疾病。

22. 发明申请

WO01009146A1 RADIOLABELLED BISPHOSPHONATES AND METHOD 审中-公开
标题翻译：放射性二磷酸酯和方法
公开(公告)号：WO01009146A1
公开(公告)日：2001-02-08
申请号：PCT/EP2000/007490
申请日：2000-08-02
IPC分类号： A61K51/00 , A61K31/663 , A61P35/00 , A61P43/00 , C07B59/00 , C07F9/38 , C07F9/40
CPC分类号： C07B59/004 , C07F9/386 , C07F9/3873 , C07F9/409
摘要： A method of making a bisphosphonate RC(OH)(PO.]OH]2)2 comprises reacting a tris (silyl)phosphite with an activated carbonyl compound and hydrolysing the resulting intermediate. Preferably the tris (silyl)phosphite is labelled with P or P. Radiolabelled bisphosphonates are used to treat patients suffering from osteosarcoma or bone metastases.
摘要翻译：制备双膦酸盐RC（OH）（PO。）OH] 2）2的方法包括使三（甲基）亚磷酸酯与活化的羰基化合物反应并水解得到的中间体。优选地，三（3）（甲硅烷基）亚磷酸酯用32 P或33 P标记。放射性标记的双磷酸盐用于治疗患有骨肉瘤或骨转移的患者。

23. 发明申请

WO00034293A1 METHOD FOR PREPARATION OF DISODIUM PAMIDRONATE 审中-公开
标题翻译：制备二氨基磺酸钠的方法
公开(公告)号：WO00034293A1
公开(公告)日：2000-06-15
申请号：PCT/US1999/029284
申请日：1999-12-10
IPC分类号： A61K9/19 , A61K47/26 , C07F9/38 , A61K9/12 , A61K9/48 , A61K31/663
CPC分类号： A61K47/26 , A61K9/19 , C07F9/3873
摘要： The invention provides a method of preparing anhydrous disodium pamidronate or an aqueous disodium pamidronate solution for pharmaceutical use.
摘要翻译：本发明提供制备无水二氨基磷酸二钠或药物用帕米膦酸二钠水溶液的方法。

24. 发明申请

WO99020635A1 SALT OF A BISPHOSPHONIC ACID DERIVATIVE 审中-公开
标题翻译：二磷酸衍生物的盐
公开(公告)号：WO99020635A1
公开(公告)日：1999-04-29
申请号：PCT/IL1998/000508
申请日：1998-10-18
IPC分类号： C07F9/38 , A61K31/66
CPC分类号： C07F9/3873
摘要： The present invention relates to an anhydrous dipotassium alendronic acid salt and the dipotassium alendronic acid salt hydrates e.g. dipotassium alendronic acid salt pentahydrate. The present invention also relates to pharmaceutical preparations comprising as active ingredient the anhydrous dipotassium alendronic acid salt one of the dipotassium alendronic acid salt hydrates. The pharmaceutical preparation may be a tablet, a pellet, a film, sugar or enterocoated tablet or pellet, a capsule, a suspension, a solution, an emulsion, etc.
摘要翻译：本发明涉及无水二钾阿仑膦酸盐和二钾阿仑膦酸盐水合物。二氢阿卡膦酸盐五水合物。本发明还涉及包含作为有效成分的二氢阿卡膦酸盐水合物之一的无水二钾阿仑膦酸盐的药物制剂。药物制剂可以是片剂，丸剂，膜，糖或肠溶性片剂或丸剂，胶囊，悬浮液，溶液，乳液等。

25. 发明申请

WO1996031124A1 HERBICIDAL AZA BISPHOSPHONIC ACIDS AND COMPOSITIONS CONTAINING THE SAME 审中-公开
标题翻译：除草AZA二磷酸及其组合物
公开(公告)号：WO1996031124A1
公开(公告)日：1996-10-10
申请号：PCT/US1996004869
申请日：1996-04-08
申请人： ZENECA LIMITED , FISHER, Karl, J. , WOOLARD, Frank, X. , LEADBETTER, Michael, R. , GERDES, John, M.
发明人： ZENECA LIMITED
IPC分类号： A01N57/18
CPC分类号： C07F9/5532 , A01N57/18 , C07F9/3873 , C07F9/405 , C07F9/568 , C07F9/572 , C07F9/58 , C07F9/59 , C07F9/60 , C07F9/65031 , C07F9/6506 , C07F9/6512 , C07F9/6518 , C07F9/6533
摘要： Herbicidal compositions containing a bisphosphonic acid compound of formula (I) wherein n is 1, 2, 3, 4, 5 or 6, or an agrochemically acceptable salt or hydrolyzable ester thereof and methods of controlling undesirable plant growth using these bisphosphonic acid containing compositions. The herbicidal compositions exhibit desirable efficacy when applied to plants post-emergence, but exhibit little significant activity when applied to plants pre-emergence. Novel aza-bisphosphonic acid compounds are also disclosed.
摘要翻译：含有其中n为1,2,3,4,5或6的式（I）的双膦酸化合物或其农业化学上可接受的盐或可水解的酯的除草组合物以及使用这些含二膦酸的组合物来控制不期望的植物生长的方法。当施用于植物出苗后，除草组合物表现出期望的功效，但当施用于植物出苗前显示出很小的显着活性。还公开了新的氮杂双膦酸化合物。

26. 发明申请

WO1995026358A1 2,4-DIPHOSPHONOGLUTARIC ACID DERIVATIVES, METHODS OF PREPARING SUCH COMPOUNDS AND DRUGS CONTAINING THEM 审中-公开
标题翻译：新的2.4DIPHOSPHONOGLUTARSÄUREDERIVATE，方法为生产和药物含有它们的
公开(公告)号：WO1995026358A1
公开(公告)日：1995-10-05
申请号：PCT/EP1995001062
申请日：1995-03-22
申请人： BOEHRINGER MANNHEIM GMBH , ZIMMERMANN, Gerd , ESSWEIN, Angelika , TSAKLAKIDIS, Christos , BAUSS, Frieder
发明人： BOEHRINGER MANNHEIM GMBH
IPC分类号： C07F09/38
CPC分类号： C07F9/3869 , C07F9/3873 , C07F9/572
摘要： The invention concerns compounds of the formula (I) in which R is lower alkyl (which may optionally be substituted by hydroxy, alkoxy, amino, dialkylamino, alkylmercapto, alkylsulphinyl, alkansulphonyl, cycloalkyl, aryl or a heterocyclic ring), lower alkenyl, cycloalkyl, cycloalkenyl, aryl or a heterocyclic ring and R1 and R2, independently of each other, may be hydrogen, lower alkyl, cycloalkyl, aryl or arylmethyl, as well as their optically active compounds and their pharmacologically acceptable salts. The invention also concerns methods of preparing such compounds and drugs containing them for the treatment of metabolic calcium disorders. The invention further concerns compounds of the formula (II) for use as intermediates in the preparation of compounds of the formula (I).
摘要翻译：式（I）的化合物，其可任选地被羟基，烷氧基，氨基，二烷基氨基，烷基巯基，烷基亚磺酰基，烷磺酰基，环烷基，芳基或杂环，低级烯基，环烷基，环烯基，芳基或取代将R烷基低级杂环和R1和R2各自为氢，低级Aklyl，环烷基，芳基或芳甲基可以是彼此独立，它们的光学活性化合物及其药理学上可接受的盐，它们的制备方法和含有这些化合物的药物组合物，钙代谢障碍的治疗，此外，式（II）的本发明的化合物作为中间体用于制备式（I）的化合物。

27. 发明申请

WO1995011249A1 2,4-DIPHOSPHONOGLUTARIC ACID DERIVATIVES, METHODS OF PREPARING THEM AND DRUGS CONTAINING THEM 审中-公开
标题翻译：新的2.4DIPHOSPHONOGLUTARSÄUREDERIVATE，方法为生产和药物含有它们的
公开(公告)号：WO1995011249A1
公开(公告)日：1995-04-27
申请号：PCT/EP1994003434
申请日：1994-10-19
申请人： BOEHRINGER MANNHEIM GMBH , ESSWEIN, Angelika , TSAKLAKIDIS, Christos , ZIMMERMANN, Gerd , BAUSS, Frieder
发明人： BOEHRINGER MANNHEIM GMBH
IPC分类号： C07F09/38
CPC分类号： C07F9/3873 , C07F9/386 , C07F9/3869 , C07F9/572 , C07F9/58 , C07F9/59 , C07F9/6506 , C07F9/6533 , C07F9/65515 , C07F9/655345
摘要： The invention concerns compounds of formula (I) in which R is hydrogen, lower alkyl (which may be substituted by hydroxy, alkoxy, amino, dialkylamino, alkylmercapto, alkylsulphinyl, alkansulphonyl, cycloalkyl, aryl or a heterocyclic ring), lower alkenyl, cycloalkyl, cycloalkenyl, aryl or a heterocyclic ring and R1 and R2, independently of each other, may be hydrogen, lower alkyl, cycloalkyl or arylmethyl, plus pharmacologically acceptable salts of these compounds. The invention also concerns methods of preparing such compounds and drugs containing them for the treatment of metabolic disorders relating to calcium.
摘要翻译：式（I）的化合物，其中其可任选地被羟基，烷氧基，氨基，二烷基氨基，烷基巯基，烷基亚磺酰基，烷磺酰基，环烷基，芳基或杂环，低级烯基，环烷基，环烯基被取代R =氢，低级烷基基，芳基或杂环，R1和R2unhabhängig可以是氢，低级烷基，环烷基或芳甲基另一在每种情况下，以及它们的药理学上可接受的盐，它们的制备方法和含有这些化合物，钙代谢紊乱的治疗药物组合物。

28. 发明申请

WO1995010188A2 HERBICIDAL AZA BISPHOSPHONIC ACID COMPOSITIONS 审中-公开
标题翻译：除草AZA二膦酸组合物
公开(公告)号：WO1995010188A2
公开(公告)日：1995-04-20
申请号：PCT/GB1994002183
申请日：1994-10-07
申请人： ZENECA LIMITED
发明人： ZENECA LIMITED , FISHER, Karl, Joseph , WOOLARD, Frank, Xavier , GERDES, John, Montgomery
IPC分类号： A01N67/18
CPC分类号： C07F9/405 , A01N57/18 , C07F9/3873 , C07F9/5532 , C07F9/568 , C07F9/572 , C07F9/58 , C07F9/59 , C07F9/60 , C07F9/65031 , C07F9/6506 , C07F9/6512 , C07F9/6518 , C07F9/6533
摘要： Herbicidal compositions comprising: (A) a compound of formula (I), wherein R is hydrogen, hydroxy, C1-C4 alkoxy, halogen, C1-C4 alkyl, C1-C4 haloalkyl, hydroxy-C1-C4-alkyl, hydroxy-C1-C4-alkoxy or N(R )(R ) wherein R and R are each independently hydrogen or C1-C3 alkyl; R and R are each independently hydrogen; hydrocarbyl; substituted hydrocarbyl; hydrocarbyloxy; substituted hydrocarbyloxy; hydrocarbyl-S(O)m-; or substituted hydrocarbyl-S(O)m-; or R and R together form a 3-6 membered carbocyclic ring, optionally substituted with halogen, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylthio or N(R )(R ) wherein R and R are each independently hydrogen or C1-C12 alkyl; and R and R are each independently hydrogen; hydrocarbyl; substituted hydrocarbyl; hydrocarbyloxy; substituted hydrocarbyloxy; hydrocarbylthio; substituted hydrocarbylthio; pyridyl; substituted pyridyl; or are of the formula N(R )(R ) wherein R and R are independently hydrogen, hydrocarbyl or substituted hydrocarbyl; or R and R together with the nitrogen to which they are bound form an aziridine, piperazine, morpholine, thiomorpholine, thiomorpholine sulfinyl, thiomorpholine sulfonyl, hexamethyleneimine, piperidine, tetrahydropyridine, pyrazole, imidazole, pyrrole, triazole, tetrahydropyrimidine, dihydroimidazole, pyrroline, azetidine, perhydroindole, perhydroquinoline, perhydroisoquinoline or pyrrolidine ring, any of which may be optionally substituted with C1-C12 alkyl, halo, C6-C10 aryl, C6-C10 aryl substituted with halo or C1-C6 alkyl, C7-C16 aralkyl, C7-C16 aralkyl substituted with halo or C1-C6 alkyl, nitro, halo-C1-C10-alkyl, C1-C10 alkoxy, C1-C10 alkylthio, C1-C10 alkylsulfonyl, phenoxy, phenoxy substituted with halo or C1-C6 alkyl, C1-C10 alkenyl or cyano; or R and R together with the nitrogen and carbon atoms to which they are bound form an aziridine, piperazine, morpholine, thiomorpholine, thiomorpholine sulfinyl, thiomorpholine sulfonyl, hexamethyleneimine, piperidine, tetrahydropyridine, pyrazole, imidazole, pyrrole, triazole, tetrahydropyrimidine, dihydroimidazole, pyrroline, azetidine, perhydroindole, perhydroquinoline, perhydroisoquinoline or pyrrolidine ring, any of which may be optionally substituted with C1-C12 alkyl, halo, C6-C10 aryl, C6-C10 aryl substituted with halo or C1-C6 alkyl, C7-C16 aralkyl, C7-C16 aralkyl substituted with halo or C1-C6 alkyl, nitro, halo-C1-C10-alkyl, C1-C10 alkoxy, C1-C10 alkylthio, C1-C10 alkylsulfonyl, phenoxy, phenoxy substituted with halo or C1-C6 alkyl, C1-C10 alkenyl or cyano; and m is 0, 1 or 2; and agrochemically acceptable salts thereof; and (B) an agrochemically acceptable carrier therefor. In other aspects, this invention is directed to a method of controlling the growth of plants comprising applying to the area where control is desired an herbicidally effective amount of a compound of formula (I) above; as well as to certain novel compounds having a structure within the scope of formula (I) above.
摘要翻译：本发明涉及除草组合物，包括：（A）式（I）其中R <1>代表氢，羟基，C1-C4烷氧基，卤素，烷基C 1 -C 4烷基，卤代烷基C1-C4的化合物，羟基-C 1 -C 4 - 烷基，羟基-C 1 -C 4 - 烷氧基或N（R <6>）（R <7>），其中R <6>和R <7>各自独立地为氢或烷基C 1 -C C3; R 2和R 3各自独立地表示氢; 烃基; 取代的烃基; 烃; 取代的烃氧基; 烃基-S（O）间; 或烃基-S（O）m-取代的; 或R <2>和R <3>的形式，以及，碳环具有3至6个成员，任选被卤素取代，羟基，C1-C6烷氧基C1-C6烷硫基C1-C6烷基或N（R <8>）（R <9>），其中R <8>和R <9>各自独立为氢或C1-C12; 且R <4>和R <5>各自独立地是氢; 烃基; 取代的烃基; 烃; 取代的烃氧基; 烃硫基; 取代的烃基硫代; 吡啶基; 取代的吡啶基; 或者是下式的部分N（R <10>）（R <11>），其中R <10>和R <11>独立地为氢，烃基或取代烃基; 或R <4>和R <5>的氮一起与它们所结合的形式的氮丙啶，哌嗪，吗啉，硫代吗啉，硫代吗啉亚磺酰基，硫代吗啉磺酰基，六亚甲基亚胺，哌啶，四氢吡啶，吡唑，咪唑，吡咯，三唑，四氢嘧啶，二氢咪唑，吡咯啉，氮杂环丁烷，perhydroindole，全氢喹啉，全氢异或吡咯烷环，其中任何一个可以被C1-C12烷基，卤素任选被取代，C6-C10芳基，C6-C10芳基被卤素取代的或C1-C6烷基，芳烷基，C7-C16芳烷基，C7-C16替代被卤素或C1-C6烷基，硝基，卤代C1-C10烷基，烷氧基C1-C10烷硫基，C1-C10烷基磺酰基，C1-C10，苯氧基基，苯氧基替代被卤素或C1-C6烷基，C1-C10链烯基或氰基; 或R <2>和R <4>与氮和碳原子一起与它们所结合的形式的氮丙啶，哌嗪，吗啉，硫代吗啉，硫代吗啉亚磺酰基，硫代吗啉磺酰基，六亚甲基亚胺，哌啶，四氢吡啶，吡唑，咪唑，吡咯，三唑，四氢嘧啶，二氢咪唑，吡咯啉，氮杂环丁烷，perhydroindole，全氢喹啉，全氢异或吡咯烷环，其中任何一个可以被C1-C12烷基，卤素，C 6 -C 10芳基，芳基任选地被取代 C6-C10取代的被卤素或烷基C1-C6烷基，芳烷基C7-C16芳烷基，C7-C16被卤素或C1-C6烷基，硝基，卤代C1-C10烷基，烷氧基C1-C10取代的烷硫基，C1-C10， C1-C10烷基磺酰基，苯氧基，苯氧基被卤素或C1-C6烷基，C1-C10链烯基或氰基取代; 和m是0,1或2; 和其农业化学上可接受的盐; 和（B）这些化合物的农业化学上可接受的赋形剂。在其它方面，本发明涉及调节植物生长的方法，它包括对一个有效的量需要治疗的式（I）的除草化合物的表面如上所述 -Dessus。本发明还涉及一种具有对应于式（I）的结构的某些新型化合物上述。

29. 发明申请

WO1994002492A1 NOVEL ACYCLIC AMIDINE-GROUP-CONTAINING DIPHOSPHONIC ACID DERIVATIVES, PROCESS FOR PRODUCING THEM AND MEDICAMENTS CONTAINING THESE COMPOUNDS 审中-公开
标题翻译： NEW无环含脒二膦酸衍生物，其制造方法相同，并且含药物
公开(公告)号：WO1994002492A1
公开(公告)日：1994-02-03
申请号：PCT/EP1993001833
申请日：1993-07-13
申请人： BOEHRINGER MANNHEIM GMBH , ZILCH, Harald , BAUSS, Frieder
发明人： BOEHRINGER MANNHEIM GMBH
IPC分类号： C07F09/38
CPC分类号： C07F9/3873
摘要： Compounds of formula (I) in which R1 is hydrogen, a straight-chained, branched, saturated or unsaturated, possibly phenyl-substituted alkyl radical with 1-9 carbon atoms or a phenyl ring, which may be substituted by C1-C3-alkyl, C1-C3-alkoxy or halogen; R2 is hydrogen or C1-C3-alkyl, in which the two radicals may be the same or different, R is hydrogen or a straight-chained or branched alkyl radical with 1-4 carbon atoms, X is an alkylene chain with 1-6 carbon atoms, which may be singly or multiply substituted by C1-C3-alkyl and may be interrupted by oxygen, and 1 or 2 carbon atoms in the alkylene chain may be a component of a cyclopentyl or cyclohexyl ring, and A is hydrogen or possibly amino substituted by alkyl groups with 1-6 carbon atoms, and their pharmacologically acceptable salts, process for producing them and medicaments for the treatment of calcium metabolism disorders.

30. 发明申请

WO8911877A3 CONJUGATES FOR BONE IMAGING AND BONE CANCER THERAPY 审中-公开
标题翻译：骨骼成像和骨癌治疗结合
公开(公告)号：WO8911877A3
公开(公告)日：1990-03-08
申请号：PCT/US8902510
申请日：1989-06-08
申请人： NEORX CORP
发明人： FRITZBERG ALAN R , VANDERHEYDEN JEAN-LUC E , KASINA SUDHAKAR , FITZNER JEFFREY N
IPC分类号： A61K51/00 , A61K51/04 , A61P35/00 , C07F1/08 , C07F1/12 , C07F9/38 , C07F13/00 , A61K49/02
CPC分类号： C07F13/005 , A61K51/0497 , A61K2121/00 , A61K2123/00 , C07F9/3873
摘要： The present invention provides conjugates formed from calcified tissues targeting agents and radiolabeled compounds. One such conjugate comprises a chelate and a targeting agent that is capable of associating with calcified tissue, wherein the chelate contains at least four atoms selected from nitrogen atoms or sulfur atoms or combinations thereof as the donor atoms. Another aspect of the invention provides conjugates for diagnostic and therapeutic purposes, including those related to bone cancer.

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