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1. 发明申请

US20050048471A1 Albumin derivatives with therapeutic functions 审中-公开
标题翻译：具有治疗功能的白蛋白衍生物
公开(公告)号：US20050048471A1
公开(公告)日：2005-03-03
申请号：US10794774
申请日：2004-03-08
申请人： Jerome Becquart , Reinhard Fleer , Philippe Hirel , David Klatzmann , Didier Landais , Jean-Francois Mayaux , Patrice Yeh
发明人： Jerome Becquart , Reinhard Fleer , Philippe Hirel , David Klatzmann , Didier Landais , Jean-Francois Mayaux , Patrice Yeh
IPC分类号： C12N15/09 , A61K38/00 , A61K39/00 , A61K39/12 , A61K39/21 , A61P31/12 , A61P31/18 , A61P35/00 , C07K14/00 , C07K14/47 , C07K14/705 , C07K14/73 , C07K14/765 , C07K14/82 , C07K19/00 , C12N1/19 , C12N15/12 , C12N15/14 , C12N15/62 , C12N15/67 , C12N15/81 , C12P21/00 , C12P21/04 , C12R1/645 , C12Q1/70 , C07H21/04 , C07K14/74 , C12N15/86 , C12Q1/68
CPC分类号： C07K14/765 , A61K38/00 , C07K14/00 , C07K14/4716 , C07K14/70514 , C07K14/82 , C07K2319/00 , C07K2319/02 , C07K2319/31 , C07K2319/32 , C07K2319/73 , C12N15/62 , C12N15/67 , C12N15/815
摘要： Utilization of albumin as a stable plasma transporter with a therapeutic function that is derived from a membrane receptor. The present invention is exemplified by the description of new therapeutic agents that can be used in the treatment of Acquired Immunodeficiency Syndrome: hybrid macromolecules composed of albumin derivatives coupled to derivatives of the CD4 receptor having a normal or a higher affinity for the HIV-1 virus.
摘要翻译：利用白蛋白作为具有衍生自膜受体的治疗功能的稳定血浆转运蛋白。本发明通过描述可用于治疗获得性免疫缺陷综合征的新的治疗剂的例子：由与HIV-1病毒具有正常或更高亲和力的CD4受体的衍生物偶联的白蛋白衍生物组成的杂合大分子。

2. 发明授权

US5298248A Method for continuous liberation of active constituents into water 失效
标题翻译：将活性成分连续释放到水中的方法
公开(公告)号：US5298248A
公开(公告)日：1994-03-29
申请号：US835079
申请日：1992-02-18
申请人： Porte Hugues , Torres Ghislaine
发明人： Porte Hugues , Torres Ghislaine
IPC分类号： A23L2/52 , A23L33/155 , A61K9/00 , A61K31/07 , A61K31/23 , B01J4/04 , C02F1/00 , C02F1/68
CPC分类号： C02F1/688 , A61K31/07 , A61K31/23 , A61K9/0004 , B01J4/04 , C02F2103/42
摘要： An apparatus is provided for continuous and regular liberation of active constituents into domestic water supplies. The apparatus comprises a receptacle having a body portion which is impermeable to water and to the active constituent. The receptacle is provided with an aperture closed by a membrane which is permeable to water and to the active constituent. An operculum surrounds the membrane to secure the membrane to the receptacle. The active constituent is provided into the receptacle and is released through the membrane in a controlled manner over an extended period of time. Preferably, the membrane has a mean pore diameter greater than 0.05 microns.
摘要翻译：提供了一种用于将活性成分持续定期释放到家庭用水中的装置。该装置包括具有不透水的主体部分和活性成分的容器。容器设置有由膜渗透的孔和可渗透活性成分的孔。操作者围绕膜以将膜固定到容器。活性成分被提供到容器中并且通过延长的时间段以受控的方式通过膜释放。优选地，膜具有大于0.05微米的平均孔径。

3. 发明授权

US5276045A Thioformamide derivative, process for its preparation, pharmaceutical composition thereof and treatment method 失效
标题翻译：硫代甲酰胺衍生物，其制备方法，药物组合物和治疗方法
公开(公告)号：US5276045A
公开(公告)日：1994-01-04
申请号：US860599
申请日：1992-03-30
申请人： Terance W. Hart , Bernard Y. J. Vacher , Roger J. A. Walsh
发明人： Terance W. Hart , Bernard Y. J. Vacher , Roger J. A. Walsh
IPC分类号： C07C327/46 , C07D209/20 , C07D213/59 , C07D215/12 , C07D217/14 , C07D237/08 , C07D239/26 , C07D241/12 , C07D277/30 , C07D495/04 , C07D213/44 , A61K31/44 , C07D211/70
CPC分类号： C07D239/26 , C07C327/46 , C07D209/20 , C07D213/59 , C07D215/12 , C07D217/14 , C07D237/08 , C07D241/12 , C07D277/30 , C07D495/04
摘要： A thioformamide derivative of the formula: ##STR1## wherein R represents alkyl, A represents optionally substituted pyrid-3-yl, isoquinolin-4-yl, tetrahydroquinolin-3-yl, quinolin-3-yl, pyridazin-4-yl, pyrimid-5-yl, thiazol-5-yl, thieno[2,3-b]pyridin-5-yl, pyrazin-2-yl, indol-3-yl and thieno[3,2-b]pyridin-6-yl, or phenyl and Y represents a valency bond, methylene or ethylene, R.sup.2 represents hydrogen, optionally substituted alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, aryloxyalkyl, aromatic heterocyclylalkyl or aromatic heterocyclyloxyalkyl group or a group ZC(.dbd.O)-- in which Z represents optionally substituted alkyl, aryl, or aromatic heterocyclic, n represents 0 or 1, and when n represents 0, R.sup.1 may represent a hydrogen atom, optionally substituted alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, aryloxyalkyl, aromatic heterocyclylalkyl or aromatic heterocyclyloxyalkyl group or a group ZC(.dbd.O)-- or ZSO.sub.2 --, and when n represents 1, R.sup.1 represents optionally substituted alkyl, benzyl, phenethyl, 1-naphthylmethyl, 2-naphthylmethyl or pyrid-3-ylmethyl radical and pharmaceutically acceptable salts thereof possess pharmacological properties.
摘要翻译：下式的硫代甲酰胺衍生物其中R代表烷基，A代表任意取代的吡啶-3-基，异喹啉-4-基，四氢喹啉-3-基，喹啉-3-基，哒嗪-4-基，嘧啶-5-基，噻唑-5-基，噻吩并[2,3-b]吡啶-5-基，吡嗪-2-基，吲哚-3-基和噻吩并[3,2-b] 芳基，芳烷基，芳氧基烷基，芳族杂环基烷基或芳族杂环基氧基烷基或基团ZC（= O） - ，其中R 1表示氢，烷基，环烷基，环烷基烷基，芳基， Z表示任选取代的烷基，芳基或芳族杂环，n表示0或1，当n表示0时，R 1可以表示氢原子，任选取代的烷基，环烷基，环烷基烷基，芳基，芳烷基，芳氧基烷基，芳族杂环基烷基或芳族杂环烷基基团或基团ZC（= O） - 或ZSO 2 - ，当n表示1时，R 1表示任选取代的烷基，苄基，苯乙基，1-萘基甲基，2-萘基甲基或吡啶-3-基甲基及其药学上可接受的盐具有药理学性质。

4. 发明授权

US5206025A Porous pharmaceutical form and its preparation 失效
标题翻译：多孔药物形式及其制备
公开(公告)号：US5206025A
公开(公告)日：1993-04-27
申请号：US892673
申请日：1992-06-04
申请人： Frederic Courteille , Magali Vanhoeve
发明人： Frederic Courteille , Magali Vanhoeve
IPC分类号： A61K9/14 , A61K9/20 , A61K47/48
CPC分类号： A61K31/00 , A61K47/48969 , A61K9/14 , A61K9/2095 , B82Y5/00 , Y10S514/937 , Y10S514/974
摘要： New porous, unitary freeze-dried pharmaceutical form, of homogeneous appearance, consisting of:a) an inclusion compound comprising:one or optionally more active substances,a predetermined quantity of cyclodextrin,optionally an additive facilitating inclusion,b) at least one substance chosen from:diluents,binders; andc) optionally one or more additives.
摘要翻译：新颖的多孔整体冷冻干燥的药物形式，外观均匀，由以下组成：a）包含一种或任选的更多活性物质，预定量的环糊精，任选的易于包合的添加剂的包合物，b）选择至少一种物质来自：稀释剂，粘合剂; 和c）任选的一种或多种添加剂。

5. 发明授权

US5188841A Sustained release pharmaceutical formulations 失效
标题翻译：可持续发布的药物制剂
公开(公告)号：US5188841A
公开(公告)日：1993-02-23
申请号：US539193
申请日：1990-06-18
申请人： Gordon T. Simpkin , Isabelle Husson
发明人： Gordon T. Simpkin , Isabelle Husson
IPC分类号： A61K9/36 , A61K9/50 , A61K9/62 , A61K31/19 , A61K47/38 , A61P29/00
CPC分类号： A61K9/5047 , A61K31/19
摘要： The invention provides a sustained release formulation of ketoprofen comprising granules each of which comprises a core comprising ketoprofen and microcrystalline cellulose and a coating comprising a water-soluble and a water-insoluble cellulose derivative.
摘要翻译：本发明提供酮洛芬的持续释放制剂，其包含颗粒，其各自包含包含酮洛芬和微晶纤维素的核心和包含水溶性和水不溶性纤维素衍生物的包衣。

6. 发明授权

US5114949A Heterocyclic derivatives, their preparation and medicinal products containing them 失效
标题翻译：杂环衍生物，其制备和含有它们的药物
公开(公告)号：US5114949A
公开(公告)日：1992-05-19
申请号：US615670
申请日：1990-11-19
申请人： Claude Gueremy , Jean-Luc Malleron , Serge Mignani
发明人： Claude Gueremy , Jean-Luc Malleron , Serge Mignani
IPC分类号： C07D209/46 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/415 , A61K31/4184 , A61K31/425 , A61K31/428 , A61K31/47 , A61K31/495 , A61K31/496 , A61P3/04 , A61P25/18 , A61P25/24 , A61P25/26 , A61P25/28 , A61P25/30 , A61P43/00 , C07D209/92 , C07D235/26 , C07D275/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/06 , C07D513/04 , C07D513/06
CPC分类号： C07D403/06 , C07D403/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/06 , C07D513/04
摘要： Compounds are disclosed of formula:R.sub.1 --(CH.sub.2).sub.n --Hetin which R.sub.1 represents a residue of formula ##STR1## X represents a hydrogen atom or an alkyl radical, Y represents a hydrogen atom or an alkyl or alkoxy radical,Z represents an alkyl radical,n is equal to 2 or 3,Het represents a substituted piperidino (substituted at the 4-position with a 1-indenylidene, 1-indenyl or 1-indanyl radical or with a chain --(CH.sub.2).sub.m --R.sub.2 or .dbd.CH--R.sub.2), substituted 1,2,3,6-tetrahydro-1-pyridyl (substituted at the 4-position with a chain --(CH.sub.2).sub.m --R.sub.2),m is equal to 1 or 2, andR.sub.2 represents an optionally substituted 2- or 3-indolyl radical, a 1- or 2-indanyl, 1- or 2-indenyl, an optionally substituted 1,2,3,4-tetrahydro-5H-pyrido[4,3-b]indol-2-yl radical, a 1,2,3,4-tetrahydro-3-quinolyl radical, an optionally substituted 1,2,3,4-tetrahydro-2-naphthyl radical or a 1-indolyl radical, their preparation and medicinal products containing them.
摘要翻译：（C）＆gt;（C）＆lt; IMAGE＆gt;（D）＆lt; IMAGE＆gt;（D）＆lt; IMAGE＆gt; J）X表示氢原子或烷基，Y表示氢原子或烷基或烷氧基，Z表示烷基，n表示2或3，Het表示取代的哌啶子基（在4-位取代具有1-茚基，1-茚基或1-茚满基或与链 - （CH 2）m -R 2或= CH-R 2）取代的1,2,3,6-四氢-1-吡啶基（在具有链 - （CH 2）m -R 2）的4-位，m等于1或2，并且R 2表示任选取代的2-或3-吲哚基，1-或2-二氢茚基，1-或2- 茚基，任选取代的1,2,3,4-四氢-5H-吡啶并[4,3-b]吲哚-2-基，1,2,3,4-四氢-3-喹啉基，任选地取代的1,2,3,4-四氢-2-萘基或1-吲哚基，它们的制备方法和含有它们的药用产品。

7. 发明授权

US5098718A Enzymatically degradable coating compositions for feed additives intended for ruminants 失效
标题翻译：用于发酵剂的饲料添加剂的可降解涂料组合物
公开(公告)号：US5098718A
公开(公告)日：1992-03-24
申请号：US536403
申请日：1990-06-11
申请人： Pierre Ardaillon , Christine Franzoni
发明人： Pierre Ardaillon , Christine Franzoni
IPC分类号： A23K1/18 , A23K1/00 , A23K1/16 , A61K9/38 , A61K9/50 , A61K9/52
CPC分类号： A61K9/5015 , A23K40/35 , A61K9/5047 , A61K9/5052 , Y10S426/807
摘要： Enzymatically degradable compositions for the coating of feed additives intended for ruminants, including zein, at least one hydrophobic substance, optionally at least one non-water-soluble polymer and at least one inorganic filler. The compositions are used to coat feed additives such as medicinal products, vitamins and amino acids.
摘要翻译：用于涂覆用于反刍动物的饲料添加剂的酶促降解组合物，包括玉米醇溶蛋白，至少一种疏水物质，任选的至少一种非水溶性聚合物和至少一种无机填料。该组合物用于涂覆饲料添加剂，如药用产品，维生素和氨基酸。

8. 发明授权

US5023361A Process for preparing hydroxyalkylating agents, the agents so obtained, and their use 失效
标题翻译：制备羟烷基化剂的方法，所得试剂及其用途
公开(公告)号：US5023361A
公开(公告)日：1991-06-11
申请号：US485514
申请日：1990-02-27
申请人： Viviane Massonneau , Michel Mulhauser , Albert Buforn
发明人： Viviane Massonneau , Michel Mulhauser , Albert Buforn
IPC分类号： C07D233/92 , A61K31/4164 , A61P33/02 , C07B37/04 , C07C303/24 , C07C303/26 , C07C305/08 , C07C305/10 , C07C309/63 , C07C309/65 , C07C309/72 , C07C309/73 , C07D233/94 , C07D233/95 , C07D405/04
CPC分类号： C07C303/24 , C07C303/28 , C07D233/94
摘要： Hydroxyalkylating agents of formula: ##STR1## in which R denotes alkyl, n is 2 or 3, R.sub.1 denotes hydrogen or alkyl and R.sub.2 denotes alkyl an unsubstituted or substituted phenyl or ##STR2## are useful inter alia for the preparation of 1-(hydroxyalkyl)imidazoles. They are made by reaction of a sulphonic acid or dimethyl sulphate with a corresponding decarboxylate ester.

9. 发明授权

US4994470A Benzopyran derivatives and pharmaceutical compositions containing them 失效
标题翻译：苯并吡喃衍生物和含有它们的药物组合物
公开(公告)号：US4994470A
公开(公告)日：1991-02-19
申请号：US465448
申请日：1990-01-16
申请人： Michel Barreau , Jean-Claude Hardy , Christian Renault
发明人： Michel Barreau , Jean-Claude Hardy , Christian Renault
IPC分类号： A61K31/443 , A61K31/445 , A61P9/06 , C07D405/06 , C07D405/14
CPC分类号： C07D405/06
摘要： New benzopyran derivatives of general formula (I) in which:R.sub.1 denotes a hydrogen or halogen atom or a hydroxy, alkyloxy, nitro, amino, alkylsulphonamido, bis(alkylsulphonyl)amino, or acylamino radical,R denotes a radical of general formula: ##STR1## in which A denotes a single bond or a methylene radical and R.sub.2 and R.sub.3 which may be identical or different, denote a hydrogen or halogen atom or a hydroxy, alkyl, alkyloxy, nitro, amino, alkylsulphonamido, bis(alkylsulphonyl)amino, acylamino, sulphamoyl or cyano radical, or form together, when they are adjacent, a methylenedioxy or ethylenedioxy radical, or alternatively R denotes a 2-oxo-2H-benzimidazolyl radical,and R' and R" are identical and denote hydrogen atoms or alkyl radicals, their isomeric forms and their preparation.These new products are useful as antiarrhythmic and antifibrillating agents. ##STR2##
摘要翻译：新的通式（I）的苯并吡喃衍生物，其中：R1表示氢或卤素原子或羟基，烷氧基，硝基，氨基，烷基磺酰氨基，双（烷基磺酰基）氨基或酰基氨基，R表示通式的基团： IMAGE>其中A表示单键或亚甲基，R 2和R 3可以相同或不同，表示氢或卤素原子或羟基，烷基，烷氧基，硝基，氨基，烷基磺酰氨基，双（烷基磺酰基）氨基，酰基氨基，氨磺酰基或氰基，或者当它们相邻时一起形成亚甲二氧基或亚乙二氧基，或者R表示2-氧代-2H-苯并咪唑基，R'和R“相同且表示氢原子或烷基，它们的异构形式及其制备方法。这些新产品可用作抗心律不齐和抗纤颤剂。（一）

10. 发明授权

US4990515A Benzo[1,8]naphthyridine derivatives as antimicrobials 失效
标题翻译：苯并[1,8]萘啶衍生物作为抗微生物剂
公开(公告)号：US4990515A
公开(公告)日：1991-02-05
申请号：US465316
申请日：1990-01-16
申请人： Michel Antoine , Michel Barreau , Jean-Francois Desconclois , Philippe Girard , Guy Picaut
发明人： Michel Antoine , Michel Barreau , Jean-Francois Desconclois , Philippe Girard , Guy Picaut
IPC分类号： A01N43/90 , A61K31/435 , A61K31/4375 , A61P31/04 , C07D471/04
CPC分类号： C07D471/04
摘要： New benzo[b][1,8]naphthyridine derivatives of general formula (I), in which R is a hydrogen atom or an alkyl, fluoroalkyl, cycloalkyl (3 to 6 C), alkoxy or alkylamino radical or an amine protective radical and either Hal is a fluorine, chlorine or bromine atom and R' is a hydrogen atom or Hal and R' are simultaneously fluorine atoms, their salts, their preparation and the compositions which contain them.These new products can be used as antimicrobial agents for topical application or as synthesis intermediates. ##STR1##
摘要翻译：其中R为氢原子或烷基，氟烷基，环烷基（3至6个C），烷氧基或烷基氨基或胺保护基的新的苯并[b] [1,8]萘啶衍生物， Hal是氟，氯或溴原子，R'是氢原子，或Hal和R'同时是氟原子，它们的盐，它们的制备和含有它们的组合物。这些新产品可用作局部应用的抗微生物剂或合成中间体。（一）

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