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1. 发明授权

US5418242A Piperidinylthioindole derivatives, their methods of preparation and pharmaceutical compositions in which they are present, useful especially as analgesics 失效
标题翻译：哌啶基硫吲哚衍生物，它们的制备方法和它们存在的药物组合物，特别是作为止痛剂有用
公开(公告)号：US5418242A
公开(公告)日：1995-05-23
申请号：US228289
申请日：1994-04-15
申请人： Nicole Bru-Magniez , Dominique Potin , Jean-Marie Teulon
发明人： Nicole Bru-Magniez , Dominique Potin , Jean-Marie Teulon
IPC分类号： C07D401/12 , A61K31/445
CPC分类号： C07D401/12
摘要： The present invention relates to the derivatives of the formula ##STR1## and their addition salts, and to their use in therapeutics, especially as drugs with analgesic properties.
摘要翻译：本发明涉及式（I）的衍生物及其加成盐，以及它们在治疗学中的用途，特别是作为具有镇痛特性的药物。

2. 发明授权

US5229505A N.sup.6 -[3-(1-substituted)indolylethyl] adenosine 5'-carboxamides and their pharmaceutical compositions 失效
标题翻译： N6- [3-（1-取代）吲哚基乙基]腺苷5'-甲酰胺及其药物组合物
公开(公告)号：US5229505A
公开(公告)日：1993-07-20
申请号：US832576
申请日：1992-02-07
申请人： Nicole Bru-Magniez , Timur Gungor , Jean-Marie Teulon
发明人： Nicole Bru-Magniez , Timur Gungor , Jean-Marie Teulon
IPC分类号： C07H19/167 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7076 , A61P9/12 , A61P25/04 , A61P29/00 , A61P43/00 , C07H19/16
CPC分类号： C07H19/16 , Y02P20/55
摘要： The present invention relates to the derivatives of the formula ##STR1## and their addition salts, and to their use in therapeutics, especially in the central nervous system as analgesics, anticonvulsants, antiepileptics, anxiolytics, antidepressants and neuroprotectors, and in the cardiovascular system as antiarrhythmics, antihypertensives and platelet aggregation inhibitors.
摘要翻译：本发明涉及式（I）的衍生物及其加成盐，以及它们在治疗学中的用途，特别是在中枢神经系统中作为镇痛药，抗惊厥药，抗癫痫剂，抗焦虑药，抗抑郁药和神经保护剂，以及心血管系统作为抗心律失常药，抗高血压药和血小板聚集抑制剂。

3. 发明授权

US5021443A Noval benzimidazole and azabenzimiazole derivatives which are thromboxane receptor antagonists, their methods of preparation and pharmaceutical compositions in which they are present 失效
标题翻译：作为血栓烷受体拮抗剂的Noval苯并咪唑和氮杂苯并噻唑衍生物，其制备方法及其存在的药物组合物
公开(公告)号：US5021443A
公开(公告)日：1991-06-04
申请号：US493880
申请日：1990-03-15
申请人： Nicole Bru-Magniez , Eric Nicolai , Jean-Marie Teulon
发明人： Nicole Bru-Magniez , Eric Nicolai , Jean-Marie Teulon
IPC分类号： A61K31/415 , A61K31/4184 , A61K31/44 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/00 , A61P13/02 , A61P15/00 , A61P25/04 , A61P37/06 , A61P37/08 , A61P43/00 , C07D235/06 , C07D235/16 , C07D235/28 , C07D471/04 , C07F9/6506 , C07F9/6561
CPC分类号： C07D471/04 , C07D235/16 , C07D235/28 , C07F9/65068 , C07F9/6561
摘要： The present invention relates to the derivatives of the formula ##STR1## in which: A is an aromatic ring or a nitrogen heterocycle;X.sub.1, X.sub.2, X.sub.3 and X.sub.4 are independently a hydrogen atom, a halogen atom, a lower alkyl radical, an alkoxy radical, an alkylthio radical, a sulfone group, a sulfoxide group, a trifluoromethyl group, a nitro group, a hydroxyl group, a methylene alcohol radical or a group COOR', in which R' is a hydrogen or a lower alkyl; X.sub.3 and X.sub.4 can also form a naphthalene with the phenyl;B is CR.sub.5 R.sub.6, R.sub.5 and R.sub.6 being a hydrogen atom or a lower alkyl, or the sulfur atom;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently a hydrogen atom or a lower alkyl radical; CR.sub.1 R.sub.2 or CR.sub.3 R.sub.4 can form with B, when the latter is CR.sub.5 R.sub.6, a cycloalkyl or a cycloalkene having 3 to 7 carbon atoms; R.sub.1 R.sub.2 and R.sub.3 R.sub.4 can also form a ring having 3 to 6 carbon atoms;n is an integer from 1 to 4 and can be 0 if R.sub.1 and R.sub.2 are other than hydrogen; andD is a chemical group which can be: COOR.sub.7, R.sub.7 being the hydrogen atom or a lower alkyl, CONH--R.sub.8, R.sub.8 being the hydrogen atom or a lower alkyl, CN, ##STR2## R.sub.9 being the hydrogen atom or a lower alkyl, or NHSO.sub.2 CF.sub.3, and to their addition salts.
摘要翻译：本发明涉及式（I）的衍生物，其中：A是芳环或氮杂环; X 1，X 2，X 3和X 4独立地为氢原子，卤素原子，低级烷基，烷氧基，烷硫基，砜基，亚砜基，三氟甲基，硝基，羟基，亚甲基醇基或COOR'基团，其中R'是氢或低级烷基; X3和X4也可以与苯基形成萘; B是CR5R6，R5和R6是氢原子或低级烷基或硫原子; R1，R2，R3和R4独立地是氢原子或低级烷基; CR1R2或CR3R4可与B形成，当后者为CR5R6时，可以具有3-7个碳原子的环烷基或环烯烃; R1R2和R3R4也可以形成具有3至6个碳原子的环; n为1〜4的整数，如果R 1和R 2不是氢，则为0; 并且D是可以是：COOR7，R7是氢原子或低级烷基，CONH-R8，R8是氢原子或低级烷基的化学基团，CN，R9是氢原子或低级烷基，或NHSO 2 CF 3，以及它们的加成盐。

4. 发明授权

US4931584A Process for the preparation of monoesters or diesters of-9,10-endoethano-9,10-dihydroanthracene-11,11-dicarboxylic acid and for the preparation of symmetrical or asymmetrical methylidenemalonates 失效
标题翻译：制备-9,10-内联乙醇基-9,10-二氢蒽-10,11,11-二羧酸的单酯或二酯的方法，用于制备对称或不对称的亚甲基亚氨基三
公开(公告)号：US4931584A
公开(公告)日：1990-06-05
申请号：US162573
申请日：1988-03-01
申请人： Nicole Bru-Magniez , Christian De Cock , Jacques Poupaert , Jean-Luc De Keyser , Pierre Dumont
发明人： Nicole Bru-Magniez , Christian De Cock , Jacques Poupaert , Jean-Luc De Keyser , Pierre Dumont
IPC分类号： C07D303/16 , B01J31/04 , C07B61/00 , C07C67/00 , C07C67/343 , C07C69/38 , C07C69/593 , C07C69/73 , C07C69/732 , C07C69/753 , C07C253/00 , C07C255/52
CPC分类号： C07C69/38
摘要： The invention relates to novel monoesters and diesters of 9,10-endoethano-9,10-dihydroanthracene-11,11-dicarboxylic acid.These novel monoesters and diesters correspond to the following structural chemical formula (II): ##STR1## in which R.sup.1 and R.sup.2 are identical or different and can represent H, an alkali metal or alkaline earth metal atom, a linear or branched alkyl group having from 1 to 6 carbon atoms, an alicyclic group having from 3 to 6 carbon atoms, an alkenyl group having from 2 to 6 carbon atoms, defined in their cis or trans variety, or an alkynyl group having from 2 to 6 carbon atoms, the said groups optionally being substituted by one or more functional groups such as ether, epoxide, halogeno, cyano, ester, aldehyde, ketone, aryl etc., where R.sup.1 and R.sup.2 cannot be H or ethyl simultaneously. These addition products constitute valuable intermediates for the preparation of methylidenemalonates in high yields and with a high purity.
摘要翻译：本发明涉及9,10-内联乙醛-9,10-二氢蒽-11,11-二羧酸的新型单酯和二酯。这些新型单酯和二酯对应于以下结构化学式（II）：其中R 1和R 2相同或不同并可以表示H，碱金属或碱土金属原子，直链或支链烷基具有1至6个碳原子的基团，具有3至6个碳原子的脂环族基团，具有2至6个碳原子的烯基，其顺式或反式变体中定义，或具有2至6个碳原子的炔基所述基团任选被一个或多个官能团如醚，环氧化物，卤代，氰基，酯，醛，酮，芳基等所取代，其中R1和R2不能同时为H或乙基。这些加成产物构成用于以高产率和高纯度制备亚甲基亚氨基三甲酸酯的有价值的中间体。

5. 发明授权

US5663181A Naphthyridine derivatives, their methods of preparation and pharmaceutical compositions in which they are present, useful especially as antiproliferative drugs 失效
标题翻译：萘啶衍生物，它们的制备方法和它们存在的药物组合物，特别用作抗增生药物
公开(公告)号：US5663181A
公开(公告)日：1997-09-02
申请号：US549665
申请日：1995-11-29
申请人： Nicole Bru-Magniez , Michele Launay , Jean-Marie Teulon
发明人： Nicole Bru-Magniez , Michele Launay , Jean-Marie Teulon
IPC分类号： C07D471/04 , A61K31/44 , C07D471/02
CPC分类号： C07D471/04
摘要： The present invention relates to the derivatives of the formula ##STR1## and their addition salts, and to their use in therapeutics, especially as drugs having antiproliferative properties and affording an effective treatment for diseases such as cancer, psoriasis, atherosclerosis, restenosis phenomena or any other pathological condition due to cell proliferation.
摘要翻译： PCT No.PCT / FR94 / 00763 Sec。 371日期：1995年11月29日 102（e）1995年11月29日日期PCT 1994年6月24日PCT公布。第WO95 / 00513号公报日期1995年1月5日本发明涉及式“IMAGE”及其加成盐的衍生物及其在治疗学中的用途，特别是作为具有抗增殖性质的药物并对疾病如癌症，牛皮癣，动脉粥样硬化提供有效治疗，再狭窄现象或由细胞增殖引起的任何其他病理状况。

6. 发明授权

US5192781A Thiazole derivatives which are angiotensin II receptor antagonists, their methods of preparation and pharmaceutical compositions in which they are present 失效
标题翻译：作为ANGIOTENSIN II受体拮抗剂的噻唑衍生物，它们的制备方法和药物组合物
公开(公告)号：US5192781A
公开(公告)日：1993-03-09
申请号：US728393
申请日：1991-07-11
申请人： Nicole Bru-Magniez , Michele Launay , Jean-Marie Teulon
发明人： Nicole Bru-Magniez , Michele Launay , Jean-Marie Teulon
IPC分类号： C07D277/22 , C07D277/24 , C07D277/28 , C07D277/30 , C07D277/36 , C07D277/40 , C07D277/42 , C07D277/46 , C07D417/10
CPC分类号： C07D277/22 , C07D277/24 , C07D277/28 , C07D277/30 , C07D277/36 , C07D277/40 , C07D277/42 , C07D277/46 , C07D417/10
摘要： The present invention relates to the derivatives of formula (I): ##STR1## and their addition salts, and to their use in therapeutics, especially for the treatment of cardiovascular diseases and in particular for the treatment of hypertension and cardiac insufficiency.
摘要翻译：本发明涉及式（I）的衍生物：其中式（I）及其加成盐及其在治疗中的用途，特别是用于治疗心血管疾病，特别是用于治疗高血压和心脏功能不全。

7. 发明授权

US5124336A Azabenzimidazole derivatives which are thromboxane receptor antagonists 失效
标题翻译：作为血栓素受体拮抗剂的偶氮苯并咪唑衍生物
公开(公告)号：US5124336A
公开(公告)日：1992-06-23
申请号：US650732
申请日：1991-02-05
申请人： Nicole Bru-Magniez , Eric Nicolai , Jean-Marie Teulon
发明人： Nicole Bru-Magniez , Eric Nicolai , Jean-Marie Teulon
IPC分类号： A61K31/415 , A61K31/4184 , A61K31/44 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/00 , A61P13/02 , A61P15/00 , A61P25/04 , A61P37/06 , A61P37/08 , A61P43/00 , C07D235/06 , C07D235/16 , C07D235/28 , C07D471/04 , C07F9/6506 , C07F9/6561
CPC分类号： C07D471/04 , C07D235/16 , C07D235/28 , C07F9/65068 , C07F9/6561
摘要： The present invention relates to the derivatives of the formula ##STR1## in which: A is an aromatic ring or a nitrogen heterocycle;X.sub.1, X.sub.2, X.sub.3 and X.sub.4 are independently a hydrogen atom, a halogen atom, a lower alkyl radical, a C.sub.3 -C.sub.7 cycloalkyl radical, an alkoxy radical, an alkylthio radical, a sulfone group, SO.sub.2 -lower alkyl, a sulfoxide group, SO-lower alkyl, a trifluoromethyl group, a nitro group, a hydroxyl group, a methylene alcohol radical or a group COOR', in which R' is a hydrogen or a lower alkyl; X.sub.3 and X.sub.4 can also form a naphthalene with the phenyl;B is CR.sub.5 R.sub.6, R.sub.5 and R.sub.6 being a hydrogen atom, a lower alkyl or a C.sub.3 -C.sub.7 cycloalkyl radical, or the sulfur atom;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently a hydrogen atom, a lower alkyl radical or a C.sub.3 -C.sub.7 cycloalkyl radical; CR.sub.1 R.sub.2 or CR.sub.3 R.sub.4 can form with B, when the latter is CR.sub.5 R.sub.6, a cycloalkyl or a cycloalkene having 3 to 7 carbon atoms; R.sub.1 R.sub.2 and R.sub.3 R.sub.4 can also form a ring having 3 to 7 carbon atoms;n is an integer from 1 to 4 and can be 0 if R.sub.1 and R.sub.2 are other than hydrogen; andD is a chemical group which can be: COOR.sub.7, R.sub.7 being the hydrogen atom, a lower alky radical or a C.sub.3 -C.sub.7 cycloalkyl radical, CONH-R.sub.8, R.sub.8 being the hydrogen atom, a lower alkyl radical or a C.sub.3 -C.sub.7 cycloalkyl radical, or CN,and to their addition salts. The compounds are thromboxane antagonist receptors.
摘要翻译：本发明涉及式（I）的衍生物，其中：A是芳环或氮杂环; X 1，X 2，X 3和X 4独立地为氢原子，卤素原子，低级烷基，C 3 -C 7环烷基，烷氧基，烷硫基，砜基，SO 2 - 低级烷基，亚砜基， SO - 低级烷基，三氟甲基，硝基，羟基，亚甲基基团或COOR'基团，其中R'为氢或低级烷基; X3和X4也可以与苯基形成萘; B是CR5R6，R5和R6是氢原子，低级烷基或C3-C7环烷基或硫原子; R1，R2，R3和R4独立地为氢原子，低级烷基或C3-C7环烷基; CR1R2或CR3R4可与B形成，当后者为CR5R6时，可以具有3-7个碳原子的环烷基或环烯烃; R1R2和R3R4也可以形成具有3至7个碳原子的环; n为1〜4的整数，如果R 1和R 2不是氢，则为0; D为化学基团，可以是：COOR7，R7是氢原子，低级烷基或C3-C7环烷基，CONH-R8，R8是氢原子，低级烷基或C3-C7环烷基自由基或CN，以及它们的加成盐。化合物是血栓素拮抗剂受体。

8. 发明授权

US06440461B1 Poly(methylidene malonate) microspheres, preparation method and pharmaceutical compositions containing them 有权
标题翻译：聚（亚甲基丙二酸酯）微球，制备方法和含有它们的药物组合物
公开(公告)号：US06440461B1
公开(公告)日：2002-08-27
申请号：US09673255
申请日：2000-12-19
申请人： Nicole Bru-Magniez , Elias Fattal , Catherine Le Visage , Patrick Couvreur , Pascal Breton
发明人： Nicole Bru-Magniez , Elias Fattal , Catherine Le Visage , Patrick Couvreur , Pascal Breton
IPC分类号： A61K914
CPC分类号： C08J3/14 , A61K9/1635 , A61K9/1641 , C08J2335/00
摘要： The invention concerns novel microspheres particularly useful in pharmaceutics as particulate vectors for carrying biologically active substances, in particular hydrophilic substances, for oral administration. The invention is characterised in that said microspheres consist of a support material continuous lattice wherein is optionally dispersed a substance, said support material containing at least 70 wt. % of a homopolymer consisting of recurrent units corresponding to general formula (I): wherein: R1 represents an alkyl group containing 1 to 6 carbon atoms or a (CH2)m—COOR3 group wherein m is an integer ranging between 1 and 5 and R3 represents an alkyl group having 1 to 6 carbon atoms; R2 represents an alkyl group having 1 to 6 carbon atoms; and n is an integer ranging between 1 and 5. The invention is useful in pharmaceutics.
摘要翻译：本发明涉及在药物学中特别有用的新型微球，作为用于携带用于口服给药的生物活性物质，特别是亲水性物质的颗粒载体。本发明的特征在于，所述微球由支撑材料连续晶格组成，其中任选地分散物质，所述载体材料含有至少70wt。％的由通式（I）表示的反复单元组成的均聚物：其中：R1表示含有1至6个碳原子的烷基或（CH2）m -COOR3基团，其中m为1至5的整数，R3为表示碳原子数1〜6的烷基。 R2表示碳原子数1〜6的烷基， n为1〜5的整数。本发明可用于制药。

9. 发明授权

US06420468B2 Methylidene malonate nanoparticles 失效
标题翻译：亚甲基丙二酸酯纳米粒子
公开(公告)号：US06420468B2
公开(公告)日：2002-07-16
申请号：US09770303
申请日：2001-01-29
申请人： Nicole Bru-Magniez , Xavier Guillon , Pascal Breton , Patrick Couvreur , François Lescure , Claude Roques-Carmes , Gérard Riess
发明人： Nicole Bru-Magniez , Xavier Guillon , Pascal Breton , Patrick Couvreur , François Lescure , Claude Roques-Carmes , Gérard Riess
IPC分类号： C08K507
CPC分类号： A61K9/5138 , C08F22/14
摘要： Nanoparticles formed from a random polymer of at least one compound of formula (I) in which A represents a group or a group; R1 and R2, identical or different, represent a linear or branched C1-C6 alkyl group; n=1, 2, 3, 4 or 5, having a diameter of less than 500 nm and an average molecular mass (Mw) between about 8000 and 100000, the nanoparticles being formed from homogeneous molecular species, and optionally containing a biologically active material.
摘要翻译：由至少一种式（I）化合物的无规聚合物形成的纳米颗粒，其中A表示一个或多个基团; R 1和R 2相同或不同，表示直链或支链C 1 -C 6烷基; n = 4或5，具有小于500nm的直径和约8000至100000的平均分子量（Mw），所述纳米颗粒由均匀的分子种类形成，并且任选地含有生物活性材料。

10. 发明授权

US5358950A Triazolopyrimidine derivatives which are angiotensin II receptor antagonists 失效
标题翻译：作为血管紧张素II受体拮抗剂的三唑并嘧啶衍生物
公开(公告)号：US5358950A
公开(公告)日：1994-10-25
申请号：US906526
申请日：1992-06-24
申请人： Nicole Bru-Magniez , Eric Nicolai , Jean-Marie Teulon
发明人： Nicole Bru-Magniez , Eric Nicolai , Jean-Marie Teulon
IPC分类号： C07D487/04 , A61K31/505
CPC分类号： C07D487/04
摘要： The present invention relates to the derivatives of formula: ##STR1## and to their tautomeric forms as well as to their addition salts and to their use in therapy, in particular for the treatment of cardiovascular diseases, especially for the treatment of hypertension, cardiac insufficiency and diseases of the arterial wall.
摘要翻译：本发明涉及式（I）的衍生物及其互变异构形式及其加成盐及其在治疗中的用途，特别是用于治疗心血管疾病，特别是用于治疗心血管疾病高血压，心功能不全和动脉壁疾病。

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