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31. 发明授权

US06344464B1 Use of tetrahydropyridine derivatives to prepare medicines for treating diseases causing demyelination 失效
公开(公告)号：US06344464B1
公开(公告)日：2002-02-05
申请号：US09403507
申请日：2000-04-18
申请人： Bernard Bourrie , Pierre Casellas , Jean-Pierre Maffrand
发明人： Bernard Bourrie , Pierre Casellas , Jean-Pierre Maffrand
IPC分类号： A61K31445
CPC分类号： A61K31/444 , A61K31/4418
摘要： The invention relates to the use of tetrahydropyridine derivatives of the formula in which: R1 is a halogen or a CF3, (C1-C4)alkyl or (C1-C4)alkoxy group; Y is a nitrogen atom or a CH group; Z′ and Z″ are each hydrogen or a (C1-C3)alkyl group, or one is hydrogen and the other is a hydroxyl group, or the two together are an oxo group; and Z is: a phenyl radical; a phenyl radical monosubstituted by a substituent X, X being: (a) a (C1-C6)alkyl, (C1-C6)alkoxy, (C3-C7)carboxyalkyl, (C1-C4)alkoxycarbonyl(C1-C6)alkyl, (C3-C7)carboxyalkoxy or (C1-C4)alkoxycarbonyl(C1-C6)alkoxy group; (b) a group selected from (C3-C7)cycloalkyl, (C3-C7)cycloalkoxy, (C3-C7)cycloalkylmethyl, (C3-C7)cycloalkylamino and cyclohexenyl, it being possible for said group to be substituted by a halogen, hydroxy, (C1-C4)alkoxy, carboxy, (C1-C4)alkoxycarbonyl, amino or mono- or di-(C1-C4)alkylamino group; or (c) a group selected from phenyl, phenoxy, phenylamino, N—(C1-C3)alkyl-phenylamino, phenylmethyl, phenylethyl, phenylcarbonyl, phenylthio, phenylsulfonyl, phenylsulfinyl and styryl, it being possible for said group to be monosubstituted or polysubstituted on the phenyl group by a halogen, CF3, (C1-C4)alkyl, (C1-C4)alkoxy, cyano, amino, mono- or di-(C1-C4)alkylamino, (C1-C4)acylamino, carboxy, (C1-C4)alkoxycarbonyl, aminocarbonyl, mono- or di-(C1-C4)alkylaminocarbonyl, amino(C1-C4)alkyl, hydroxy(C1-C4)alkyl or halogeno(C1-C4)alkyl group; a phenyl radical disubstituted by a substituent R2, R2 being a halogen or a hydroxy, methyl, ethyl, (C3-C6)alkyl, (C1-C4)alkoxy or trifluoromethyl group, and by a substituent X, X being as defined above; a 1-naphthyl or 2-naphthyl radical; or a 1-naphthyl or 2-naphthyl radical substituted in the 5-, 6-, 7- and/or 8-positions by one or two hydroxy groups, one or two (C1-C4)alkoxy groups or a 6,7-methylenedioxy group; or Z″ is hydrogen and Z and Z′ are each independently an unsubstituted or mono-, di- or tri-substituted phenyl group, or a pharmaceutically acceptable salt and solvate thereof, for the preparation of pharmaceutical compositions intended for treating diseases which cause demyelination.

32. 发明授权

US4911912A Ribosome-inactivating glycoproteins, modified by oxidation of their osidic units and reduction, and in vivo prolonged-action immunotoxins containing such a glycoprotein 失效
标题翻译：核糖体失活的糖蛋白，通过其氧化单位的还原而被修饰，并且含有这种糖蛋白的体内延长作用的免疫毒素
公开(公告)号：US4911912A
公开(公告)日：1990-03-27
申请号：US941989
申请日：1986-12-15
申请人： Pierre Casellas , Bernard Bourrie , Xavier Canat
发明人： Pierre Casellas , Bernard Bourrie , Xavier Canat
IPC分类号： C07K14/00 , A61K36/00 , A61K36/18 , A61K36/42 , A61K36/896 , A61K38/00 , A61K38/36 , A61K39/395 , A61K47/48 , C07K1/107 , C07K1/113 , C07K14/415 , C07K14/42 , C07K19/00
CPC分类号： C07K14/415 , A61K47/48469 , A61K47/48476 , C07K1/107 , A61K38/00 , Y10S530/863 , Y10S530/866
摘要： Glycoprotein (GPIR) having the ribosome-inhibiting activity of the native GPIR and having a prolonged-action in vivo which is obtained by oxidation of its osidic units by the action of periodate ions, and simultaneous reduction with cyanoborohydride ions. Said modified glycoprotein may be coupled to an antibody or a fragment thereof in order to form an immunotoxin having a prolonged-action in vivo.
摘要翻译：糖蛋白（GPIR）具有天然GPIR的核糖体抑制活性并且在体内具有延长的作用，其通过氧化高碘酸根离子的其奥昔单位而得到，同时用氰基硼氢化合物还原。所述修饰的糖蛋白可以与抗体或其片段偶联，以形成在体内具有延长作用的免疫毒素。

33. 发明授权

US08236811B2 Therapeutic use for treating of leukemia 失效
标题翻译：治疗白血病的治疗用途
公开(公告)号：US08236811B2
公开(公告)日：2012-08-07
申请号：US12485401
申请日：2009-06-16
申请人： Bernard Bourrie , Pierre Casellas
发明人： Bernard Bourrie , Pierre Casellas
IPC分类号： A61K31/519
CPC分类号： A61K31/519 , A61K31/704 , A61K31/7068 , A61K2300/00
摘要： The disclosure relates to methods of treating leukaemia, in particular myeloid leukaemia, comprising administering the compound N-[2-(2,1,3-benzothiadiazol-5-ylamino)-6-(2,6-dichlorophenyl)pyrido[2,3-d]pyrimidin-7-yl]-N′-(1,1-dimethylethyl)-urea or a hydrate, a pharmaceutically acceptable salt or a solvate thereof.
摘要翻译：本公开涉及治疗白血病，特别是骨髓性白血病的方法，包括给予化合物N- [2-（2,1,3-苯并噻二唑-5-基氨基）-6-（2,6-二氯苯基）吡啶并[ 3-d]嘧啶-7-基] -N' - （1,1-二甲基乙基） - 脲或其水合物，其药学上可接受的盐或溶剂化物。

34. 发明授权

US07893259B2 Pyrido-pyrimidine derivatives, preparation thereof, and therapeutic use thereof 有权
标题翻译：吡啶并嘧啶衍生物及其制备方法及其治疗用途
公开(公告)号：US07893259B2
公开(公告)日：2011-02-22
申请号：US12415256
申请日：2009-03-31
申请人： Bernard Bourrie , Pierre Casellas , Samir Jegham , Pierre Perreaut
发明人： Bernard Bourrie , Pierre Casellas , Samir Jegham , Pierre Perreaut
IPC分类号： C07D471/04 , A61P35/00 , A61P35/02
CPC分类号： C07D471/04
摘要： The disclosure concerns pyrido[2,3-d]pyrimidine derivatives, their preparation and their therapeutic application, of general formula (I): and acid addition salts, hydrates and solvates thereof, as well as in the form of enantiomers, diastereoisomers and mixtures thereof. The disclosure also concerns methods for preparing said derivatives, pharmaceutical compositions containing a compound of general formula (I), and their therapeutic use.
摘要翻译：本公开涉及通式（I）的吡啶并[2,3-d]嘧啶衍生物及其制备方法及其治疗应用：及其酸加成盐，水合物和溶剂化物，以及对映异构体，非对映异构体和混合物的形式其中。本公开还涉及制备所述衍生物的方法，含有通式（I）的化合物的药物组合物及其治疗用途。

35. 发明授权

US07816368B2 Pyridoindolone derivatives substituted in the 3-position by a heterocyclic group, their preparation and their application in therapeutics 失效
标题翻译：吡啶并吲哚酮衍生物在3位被杂环基取代，其制备及其在治疗中的应用
公开(公告)号：US07816368B2
公开(公告)日：2010-10-19
申请号：US12252647
申请日：2008-10-16
申请人： Bernard Bourrie , Pierre Casellas , Jean-Marie Derocq , Samir Jegham , Yvette Muneaux
发明人： Bernard Bourrie , Pierre Casellas , Jean-Marie Derocq , Samir Jegham , Yvette Muneaux
IPC分类号： A61K31/44
CPC分类号： C07D471/04
摘要： The present disclosure relates to pyridoindolone derivatives of general formula (I): in which R1 to R5 are as defined in the specification, to processes for preparing said derivatives, and to methods of use thereof.
摘要翻译：本公开涉及通式（I）的吡啶并吲哚酮衍生物：其中R 1至R 5如本说明书中所定义，用于制备所述衍生物的方法及其使用方法。

36. 发明申请

US20070129365A1 6-Substituted pyridoindolone derivatives, production and therapeutic use thereof 失效
标题翻译： 6-取代的吡啶并吲哚酮衍生物，其制备和治疗用途
公开(公告)号：US20070129365A1
公开(公告)日：2007-06-07
申请号：US11582769
申请日：2006-10-18
申请人： Bernard Bourrie , Pierre Casellas , Paola Ciapetti , Jean-Marie Deroco , Samir Jegham , Yvette Muneaux , Camille-Georges Wermuth
发明人： Bernard Bourrie , Pierre Casellas , Paola Ciapetti , Jean-Marie Deroco , Samir Jegham , Yvette Muneaux , Camille-Georges Wermuth
IPC分类号： A61K31/5377 , A61K31/4745 , C07D471/02
CPC分类号： C07D471/04
摘要： Compounds of formula: and pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1, R2, R3, R4, and R5, have the meanings given in the description; pharmaceutical compositions comprising said compounds; and processes for preparing said compounds and methods of use thereof.
摘要翻译：其中R 1，R 2，R 3，R 3，R 3， 4 和R 5 5具有在说明书中给出的含义; 包含所述化合物的药物组合物; 以及制备所述化合物的方法及其使用方法。

37. 发明授权

US06482986B1 Benzene derivatives, preparation method and pharmaceutical compositions containing same 有权
标题翻译：苯衍生物，制备方法和含有它们的药物组合物
公开(公告)号：US06482986B1
公开(公告)日：2002-11-19
申请号：US10009140
申请日：2002-02-27
申请人： Robert Boigegrain , Bernard Bourrie , Martine Bourrie , Pierre Casellas , Jean Marc Herbert , Pierre Lair , Dino Nisato , Raymond Paul , Jean Claude Vernieres
发明人： Robert Boigegrain , Bernard Bourrie , Martine Bourrie , Pierre Casellas , Jean Marc Herbert , Pierre Lair , Dino Nisato , Raymond Paul , Jean Claude Vernieres
IPC分类号： C07C21100
CPC分类号： C07C211/40 , C07C2601/14 , C07C2603/74
摘要： The invention concerns compounds of formula (I) wherein A, X, Y, n, R1, R2 and R3 are as defined in claim 1. Said compounds are specifically binding to sigma receptors particularly those of the peripheral nervous system.
摘要翻译：本发明涉及式（I）化合物，其中A，X，Y，n，R 1，R 2和R 3如权利要求1中所定义。所述化合物特异性结合σ受体，特别是外周神经系统的受体。

38. 发明授权

US5106956A Ribosome-inactivating glycoproteins, modified by oxidation of their osidic units and reduction, and in vivo prolonged-action immunotoxins containing such a glycoprotein 失效
标题翻译：通过氧化其功能单位和减少修饰的糖蛋白 - 灭活性糖蛋白，以及含有这种糖蛋白的体内促进作用的免疫调节蛋白
公开(公告)号：US5106956A
公开(公告)日：1992-04-21
申请号：US404611
申请日：1989-09-08
申请人： Pierre Casellas , Bernard Bourrie , Xavier Canat
发明人： Pierre Casellas , Bernard Bourrie , Xavier Canat
IPC分类号： C07K14/00 , A61K36/00 , A61K36/18 , A61K36/42 , A61K36/896 , A61K38/00 , A61K38/36 , A61K39/395 , A61K47/48 , C07K1/107 , C07K1/113 , C07K14/415 , C07K14/42 , C07K19/00
CPC分类号： C07K14/415 , A61K47/48469 , A61K47/48476 , C07K1/107 , A61K38/00 , Y10S530/863 , Y10S530/866
摘要： Glycoprotein which inactivates ribosomes (GPIR) having the ribosome-inhibiting activity of the native GPIR and having a prolonged-action in vivo which is obtained by oxidation of its osidic units by the action of periodate ions, and simultaneous reduction with cyanoborohydride ions. Said modified glycoprotein may be coupled to an antibody or a fragment thereof in order to form an immunotoxin having a prolonged-action in vivo.

39. 发明授权

US5104976A Ribosome-inactivating glycoproteins, modified by oxidation of their osidic units and formation of a Schiff's base and in-vivo prolonged action immunotoxins containing such a glycoprotein 失效
标题翻译： RIBOSOME-灭活GLYCOPROTEIN，其通过氧化其功能单元和形成SCHIFF的基础和体内促进的作用修饰的含有这种糖蛋白的免疫原性
公开(公告)号：US5104976A
公开(公告)日：1992-04-14
申请号：US404052
申请日：1989-09-08
申请人： Pierre Casellas , Bernard Bourrie , Xavier Canat
发明人： Pierre Casellas , Bernard Bourrie , Xavier Canat
IPC分类号： C07K14/00 , A61K36/00 , A61K36/18 , A61K36/42 , A61K36/896 , A61K38/00 , A61K38/36 , A61K39/395 , A61K47/48 , A61P35/00 , C07K1/107 , C07K1/113 , C07K14/415 , C07K14/42 , C07K19/00
CPC分类号： A61K47/48469 , A61K47/48476 , A61K47/48715 , C07K1/1072 , C07K1/1077 , C07K14/415 , A61K38/00 , Y10S530/863
摘要： Glycoprotein which inactivates ribosomes (GPIR) the ribosome-inhibiting activity of the native GPIR and having a prolonged-action in vivo which is obtained by oxidation of its osidic units by the action of periodate ions, and simultaneous blocking of the oxidation product by formation of a Schiff's base with a suitable primary amine. Said modified glycoprotein may be coupled to an antibody or a fragment thereof in order to form an immunotoxin.

40. 发明授权

US4749566A Pharmaceutical composition comprising a combination of at least one immunotoxin and at least one mannose-containing polymer 失效
标题翻译：药物组合物，其包含至少一种免疫毒素和至少一种含甘露糖的聚合物的组合
公开(公告)号：US4749566A
公开(公告)日：1988-06-07
申请号：US801843
申请日：1985-11-26
申请人： Pierre Casellas , Bernard Bourrie , Pierre Gros
发明人： Pierre Casellas , Bernard Bourrie , Pierre Gros
IPC分类号： A61K39/395 , A61K45/00 , A61P35/00 , A61P37/00
CPC分类号： A61K39/395 , Y10S435/81 , Y10S514/885
摘要： The invention relates to pharmaceutical compositions comprising a combination of at least one immunotoxin and at least one mannose-containing polymer. This combination makes it possible to inhibit the rapid elimination of immunotoxins from the plasma after injection.
摘要翻译：本发明涉及包含至少一种免疫毒素和至少一种含甘露糖的聚合物的组合的药物组合物。这种组合使得可以抑制注射后等离子体的免疫毒素的快速消除。

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