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1. 发明申请

US20110230447A1 OSTEOGENESIS PROMOTER COMPRISING [4-(METHYLTHIO)PHENYLTHIO]METHANEBISPHOSPHONIC ACID OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF AS ACTIVE INGREDIENT 审中-公开
标题翻译：含有[4-（甲基硫代）苯基]甲烷二磷酸或其药学上可接受的盐作为活性成分的蛋白质促进剂
公开(公告)号：US20110230447A1
公开(公告)日：2011-09-22
申请号：US13059969
申请日：2009-08-05
申请人： Hisashi Shinoda , Kaoru Igarashi , Shinobu Murakami , Keiko Suzuki
发明人： Hisashi Shinoda , Kaoru Igarashi , Shinobu Murakami , Keiko Suzuki
IPC分类号： A61K31/663 , C07F9/38 , A61P19/08
CPC分类号： A61K31/663
摘要： Disclosed are: a compound which can be produced through a chemical synthesis at low cost, has an excellent osteogenesis-promoting activity, has high affinity for a bone, and can be applied without the need of any special DDS; and a method for promoting osteogenesis by administering the compound and applying the promotion of osteogenesis to the formation or regeneration of a bone. Specifically disclosed are: an osteogenesis promoter or a pharmaceutical composition comprising [4-(methylthio)phenylthio]methanebisphosphonic acid, which is one of bisphosphonic acids, or a pharmaceutically acceptable salt thereof as an active ingredient; and a method for promoting osteogenesis, which comprises administering the osteogenesis promoter or the pharmaceutical composition to a subject to be treated.
摘要翻译：公开了以低成本化学合成制造的化合物，具有优异的成骨促进活性，对骨骼具有高亲和力，可以无需特殊的DDS而应用; 以及通过施用化合物并促进成骨促进骨的形成或再生来促进成骨的方法。具体公开的是：成骨促进剂或包含作为双膦酸之一的[4-（甲硫基）苯硫基]甲烷二膦酸或其药学上可接受的盐作为活性成分的药物组合物; 以及促进成骨的方法，其包括将骨发生促进剂或药物组合物施用于待治疗的对象。

2. 发明授权

US5283057A Risedronate in oral compositions 失效
标题翻译：利塞膦酸盐在口服组合物中
公开(公告)号：US5283057A
公开(公告)日：1994-02-01
申请号：US874269
申请日：1992-04-24
申请人： Hisashi Shinoda
发明人： Hisashi Shinoda
IPC分类号： A61K8/55 , A61K31/67 , A61Q11/00 , A61K7/16 , A61K7/22
CPC分类号： A61K8/55 , A61K31/67 , A61Q11/00 , Y10S514/90 , Y10S514/902
摘要： The present invention relates to compositions and methods which are effective against alveolar bone resorption and enhance the ability of a tooth moved in orthodontic therapy to remain in its new position or to stay in its original position when adjacent teeth are moved.
摘要翻译：本发明涉及对齿槽骨吸收有效的组合物和方法，并且提高在正畸治疗中移动的牙齿保持在其新位置或在相邻牙齿移动时保持其初始位置的能力。

3. 发明授权

US5668120A Iontophoretic delivery of bisphosphonates to the alveolar bone 失效
公开(公告)号：US5668120A
公开(公告)日：1997-09-16
申请号：US495266
申请日：1995-06-27
申请人： Hisashi Shinoda , Hiroshi Horiuchi
发明人： Hisashi Shinoda , Hiroshi Horiuchi
IPC分类号： A61C19/06 , A61K9/00 , A61K31/675 , A61N1/30 , A61K31/66
CPC分类号： A61K31/663 , A61K31/675 , A61K9/0009 , A61K9/0063 , A61N1/30
摘要： The present invention relates to methods of inhibiting alveolar bone resorption or the undesirable movement of teeth of a human or other animal comprising:a) administering a reservoir to the gingival tissue of the oral cavity such that the reservoir is in contact with the exposed tissue nearest to the alveolar bone to be treated wherein the reservoir is a composition having a pH which maintains an active compound in a negatively charged state and comprises a safe and effective amount of the active compound having the structure: ##STR1## wherein: n is an integer from 0 to 7 (preferably from 0 to 3, more preferably 1); R.sup.1 is hydrogen, chloro, amino, or hydroxy (preferably hydrogen or hydroxy); X is --NH--, quaternary amine, oxygen, sulfur, or a single bond (preferably --NH-- or single bond); R.sup.2 is a 5- to 7-membered carbocycle (preferably 6- to 7-membered, more preferably benzene or cycloheptyl), a 5- to 7-membered heterocycle having from 1 to 3 heteroatoms (preferably a 6-membered heterocycle having 1 or 2 nitrogen atoms, wherein a ring nitrogen may be quaternarized), --NH.sub.2, amino substituted with one alkyl or two alkyl (preferably C.sub.1 -C.sub.5) groups to give a secondary or tertiary amine, respectively, quaternary amino, or hydrogen; wherein if R.sup.2 is a substituted 5- to 7-membered carbocycle or heterocycle, the substituent is one or more substituents selected from the group consisting of substituted and unsubstituted, saturated or unsaturated alkyl having from 1 to about 6 carbon atoms, substituted and unsubstituted aryl, substituted and unsubstituted benzyl, hydroxy, halogen, carbonyl, alkoxy, nitro, amido, amino, substituted amino, carboxylate, and combinations thereof; each R.sup.3 is, independently, hydrogen, or substituted or unsubstituted alkyl (saturated or unsaturated) having from 1 to about 4 carbon atoms; or their pharmaceutically-acceptable salts and esters; andb) passing a safe and effective amount of electrical current through two electrodes, one electrode being a negative electrode in contact with the reservoir, the second electrode being a positive electrode in contact with the human or other animal being treated.

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