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1. 发明申请

WO2007031878A3 METHODS OF TREATING NERVOUS DISORDERS 审中-公开
标题翻译：治疗神经病的方法
公开(公告)号：WO2007031878A3
公开(公告)日：2007-09-07
申请号：PCT/IB2006003503
申请日：2006-07-26
申请人： EXONHIT THERAPEUTICS SA , DESIRE LAURENT , LEBLOND BETRAND , BEAUSOLEIL ERIC , TAVERNE THIERRY , SCHWEIGHOFFER FABIEN , PICARD VIRGINIE
发明人： DESIRE LAURENT , LEBLOND BETRAND , BEAUSOLEIL ERIC , TAVERNE THIERRY , SCHWEIGHOFFER FABIEN , PICARD VIRGINIE
IPC分类号： A61K31/5375 , A61P25/28
CPC分类号： A61K31/5375 , A61K31/4709 , A61K31/496 , A61K31/541
摘要： The invention relates to compositions and methods for treating nervous disorders. More particularly, the invention relates to methods of treating amyloÊd beta peptide-related disorders, particularly Alzheimer's disease, using Rac1 inhibitors. The invention may be used in mammalian subjects, particularly human subjects, at various stages of the disease, including disease onset. The invention also provides methods of producing, identifying, selecting or optimising compounds for use in the treatment of amyloÊd beta peptide-related disorders, based on a determination of the ability of a test compound to inhibit Rac 1 .
摘要翻译：本发明涉及用于治疗神经紊乱的组合物和方法。更具体地说，本发明涉及使用Rac1抑制剂治疗淀粉β肽相关病症，特别是阿尔茨海默氏病的方法。本发明可用于哺乳动物受试者，特别是人类受试者，在疾病的各个阶段，包括疾病发作。基于确定测试化合物抑制Rac1的能力，本发明还提供了产生，鉴定，选择或优化用于治疗淀粉β肽相关病症的化合物的方法。

2. 发明申请

WO2009007457A3 COMPOUNDS AND METHODS FOR MODULATING RHO GTPASES 审中-公开
标题翻译：用于调节RHO GTPASES的化合物和方法
公开(公告)号：WO2009007457A3
公开(公告)日：2009-03-26
申请号：PCT/EP2008059134
申请日：2008-07-11
申请人： EXONHIT THERAPEUTICS SA , LEBLOND BERTRAND , BEAUSOLEIL ERIC , CHAUVIGNAC CEDRIC , TAVERNE THIERRY , PICARD VIRGINIE , DE OLIVEIRA CATHERINE , SCHWEIGHOFFER FABIEN
发明人： LEBLOND BERTRAND , BEAUSOLEIL ERIC , CHAUVIGNAC CEDRIC , TAVERNE THIERRY , PICARD VIRGINIE , DE OLIVEIRA CATHERINE , SCHWEIGHOFFER FABIEN
IPC分类号： C07D217/10 , A61K31/4375 , A61K31/47 , A61K31/472 , A61K31/473 , A61P7/02 , A61P9/10 , A61P9/12 , A61P25/28 , A61P27/02 , C07D217/12 , C07D217/14 , C07D217/16 , C07D217/18 , C07D217/20
CPC分类号： A61K31/4375 , A61K31/47 , A61K31/472 , A61K31/473 , C07D217/10 , C07D217/20 , C07D471/04 , C07D491/14
摘要： The present invention relates to methods and compositions that affect the GTP-binding activity of members of the Rho family GTPases, preferably Rac GTPases (Rac1, Rac1b, Rac2 and/or Rac3).
摘要翻译：本发明涉及影响Rho家族GTP酶，优选Rac GTP酶（Rac1，Rac1b，Rac2和/或Rac3）成员的GTP结合活性的方法和组合物。

3. 发明申请

WO2004076445A3 COMPOUNDS AND METHODS OF TREATING CELL PROLIFERATIVE DISEASES, RETINOPATHIES AND ARTHRITIS 审中-公开
标题翻译：治疗细胞增殖性疾病的化合物和方法，治疗和治疗
公开(公告)号：WO2004076445A3
公开(公告)日：2005-01-06
申请号：PCT/IB2004000926
申请日：2004-02-27
申请人： EXONHIT THERAPEUTICS SA , LEBLOND BERTRAND , PETIT SILVERE , PICARD VIRGINIE , TAVERNE THIERRY , SCHWEIGHOFFER FABIEN
发明人： LEBLOND BERTRAND , PETIT SILVERE , PICARD VIRGINIE , TAVERNE THIERRY , SCHWEIGHOFFER FABIEN
IPC分类号： A61K31/351 , A61K31/4709 , A61P35/00 , C07D405/12 , C07D411/12
CPC分类号： C07D405/12 , C07D411/12
摘要： The present invention relates to compounds having a general formula (I) and their uses, particularly in the pharmaceutical industry. The invention discloses compounds having anti-proliferative and antiangiogenic activities, as well as methods for treating various diseases associated with abnormal cell proliferation, including cancer, or associated with unregulated angiogenesis including growth and metastasis of solid tumors, ocular diseases and especially retinopathies, or arthritis, by administering said compounds. It further deals with pharmaceutical compositions comprising said compounds, more particularly useful to treat cancers (such as leukemia), ocular diseases and arthritis.
摘要翻译：本发明涉及具有通式（I）的化合物及其用途，特别是在制药工业中。本发明公开了具有抗增殖和抗血管生成活性的化合物，以及用于治疗与异常细胞增殖（包括癌症）相关的各种疾病或与不稳定的血管生成相关的方法，包括实体瘤，眼部疾病，特别是视网膜病变或关节炎的生长和转移，通过施用所述化合物。它还涉及包含所述化合物的药物组合物，更特别可用于治疗癌症（如白血病），眼部疾病和关节炎。

4. 发明申请

WO03074508B1 COMPOUNDS AND METHODS OF TREATING CELL PROLIFERATIVE DISEASES 审中-公开
标题翻译：化合物和治疗细胞增殖性疾病的方法
公开(公告)号：WO03074508B1
公开(公告)日：2003-11-27
申请号：PCT/IB0301050
申请日：2003-02-28
申请人： EXONHIT THERAPEUTICS SA , LEBLANC VERONIQUE , LEBLOND BERTRAND , MELLE-MILOVANOVIC DOMINIQUE , LOPEZ RODRIGUEZ MARIA LUZ , VISO BERONDA ALMA , BEAUSOLEIL ERIC , PICARD VIRGINIE , PINAR PINEDO MARIA DEL CARMEN , TAVERNE THIERRY
发明人： LEBLANC VERONIQUE , LEBLOND BERTRAND , MELLE-MILOVANOVIC DOMINIQUE , LOPEZ RODRIGUEZ MARIA LUZ , VISO BERONDA ALMA , BEAUSOLEIL ERIC , PICARD VIRGINIE , PINAR PINEDO MARIA DEL CARMEN , TAVERNE THIERRY
IPC分类号： C07D473/40 , A61K31/351 , A61K31/381 , A61K31/404 , A61K31/437 , A61K31/4433 , A61K31/4439 , A61K31/4545 , A61K31/52 , A61P9/10 , A61P35/00 , C07D309/40 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/14 , C07D471/04 , C07D309/38 , C07D307/00 , C07D309/00 , C07D333/00 , C07D407/14 , C07D411/14
CPC分类号： A61K31/351 , C07D309/40
摘要： The present invention relates to compounds and their uses, particularly in the pharmaceutical industry. The invention discloses compounds having anti-proliferative activities, as well as methods for treating various diseases associated with abnormal cell proliferation, including cancer, by administering said compounds. It further deals with pharmaceutical compositions comprising said compounds, more particularly useful to treat cancers.
摘要翻译：本发明涉及化合物及其用途，特别是在制药工业中。本发明公开了具有抗增殖活性的化合物，以及通过施用所述化合物来治疗与异常细胞增殖相关的各种疾病（包括癌症）的方法。它还涉及包含所述化合物的药物组合物，更特别可用于治疗癌症。

5. 发明申请

WO2007034329A3 COMPOUNDS AND METHODS FOR TREATMENT OF AMYLOID-BETA-PEPTIDE RELATED DISORDERS 审中-公开
标题翻译：用于治疗淀粉样蛋白肽相关疾病的化合物和方法
公开(公告)号：WO2007034329A3
公开(公告)日：2007-08-30
申请号：PCT/IB2006003242
申请日：2006-07-21
申请人： EXONHIT THERAPEUTICS SA , LEBLOND BERTRAND , BEAUSOLEIL ERIC , TAVERNE THIERRY , DESIRE LAURENT , SCHWEIGERHOFFER FABIEN
发明人： LEBLOND BERTRAND , BEAUSOLEIL ERIC , TAVERNE THIERRY , DESIRE LAURENT , SCHWEIGERHOFFER FABIEN
IPC分类号： C07D401/12 , A61K31/47 , A61K31/4709 , A61P25/28 , C07D215/36
CPC分类号： C07D215/36 , C07D401/12
摘要： The present invention relates to compounds of formula (I), preparation and uses thereof, particularly in the pharmaceutical industry. The present invention discloses novel compounds more particularly useful for the treatment of Alzheimer's disease and other similar diseases, and more specifically the inventive compounds modulate (in particular, inhibit) the level of amyloid; peptide (Aß) exhibited by cells or tissues; Aß peptide is a major component of the amyloid plaques found in the brains of Alzheimer's sufferers. This invention also relates the use of these inhibitors to prevent, treat or ameliorate the symptoms of Alzheimer's disease or any Amyloid-ß-Peptide Related Disorder.
摘要翻译：本发明涉及式（I）的化合物，其制备和用途，特别是在制药工业中。本发明公开了更特别可用于治疗阿尔茨海默氏病和其他类似疾病的新化合物，更具体地说，本发明化合物调节（特别是抑制）淀粉样蛋白的水平; 肽（Aß）由细胞或组织表现; Aβ肽是阿尔茨海默病患者大脑中淀粉样斑块的主要成分。本发明还涉及这些抑制剂用于预防，治疗或改善阿尔茨海默病或任何淀粉样蛋白-β-肽相关疾病症状的用途。

6. 发明申请

WO2006081252A2 METHODS OF USING AS ANALGESICS 1-BENZYL-1-HYDROXY-2, 3-DIAMINO-PROPYL AMINES, 3-BENZYL-3-HYDROXY-2-AMINO-PROPIONIC ACID AMIDES AND RELATED COMPOUNDS 审中-公开
标题翻译：使用1-苄基-1-羟基-2,3-二氨基丙酸，3-苄氧基-3-羟基-2-氨基 - 丙酸和其相关化合物的方法
公开(公告)号：WO2006081252A2
公开(公告)日：2006-08-03
申请号：PCT/US2006002505
申请日：2006-01-25
申请人： ALLERGAN INC , LEBLOND BERTRAND , BEAUSOLEIL ERIC , TAVERNE THIERRY , DONELLO JOHN E , SCHWEIGHOFFER FABIEN JACQUES
发明人： LEBLOND BERTRAND , BEAUSOLEIL ERIC , TAVERNE THIERRY , DONELLO JOHN E , SCHWEIGHOFFER FABIEN JACQUES
IPC分类号： A61K31/40 , A61K31/4025 , A61K31/5375 , A61P25/04 , A61P29/00
CPC分类号： C07D265/30 , A61K31/40 , A61K31/4025 , A61K31/4409 , A61K31/4439 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/5375 , A61K31/5377 , A61K31/541 , C07D207/09 , C07D213/64 , C07D295/12 , C07D295/13 , C07D295/15 , C07D319/18 , C07D405/06
摘要： The compounds shown by the structural formulas below have analgesic effect and are used in compositions and methods for treating mammal in need of such treatment.
摘要翻译：由下述结构式表示的化合物具有镇痛作用，并用于治疗需要这种治疗的哺乳动物的组合物和方法中。

7. 发明申请

WO2006081276A8 3-HETEROARYL-3-HYDROXY-2-AMINO-PROPYL AMINES AND RELATED COMPOUNDS HAVING ANALGESIC AND/OR IMMUNO STIMULANT ACTIVITY 审中-公开
标题翻译： 3-羟基-3-羟基-2-氨基 - 丙氨酸和具有有毒和/或免疫刺激活性的相关化合物
公开(公告)号：WO2006081276A8
公开(公告)日：2007-05-03
申请号：PCT/US2006002570
申请日：2006-01-25
申请人： ALLERGAN INC , LEBLOND BERTRAND , BEAUSOLEIL ERIC , TAVERNE THIERRY , DONELLO JOHN E
发明人： LEBLOND BERTRAND , BEAUSOLEIL ERIC , TAVERNE THIERRY , DONELLO JOHN E
IPC分类号： C07D213/38 , A61K31/40 , A61K31/4409 , A61P29/00 , A61P37/04 , C07D295/12 , C07D319/18
CPC分类号： C07D265/30 , A61K31/40 , A61K31/4025 , A61K31/4409 , A61K31/4439 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/5375 , A61K31/5377 , A61K31/541 , C07D207/09 , C07D213/64 , C07D295/12 , C07D295/13 , C07D295/15 , C07D319/18 , C07D405/06
摘要： Compounds of the formula where the variables have the meaning defined in the specification have analgesic and or immunostimulant effect in mammals.
摘要翻译：变量具有本说明书中定义的含义的式的化合物在哺乳动物中具有止痛和/或免疫刺激作用。

8. 发明申请

WO2006081273A8 3-ARYL-3-HYDROXY-2-AMINO-PROPIONIC ACID AMIDES, 3-HETEROAYRYL-3-HYDROXY-2-AMINO-PROPIONIC ACID AMIDES AND RELATED COMPOUNDS HAVING ANALGESIC AND/OR IMMUNOSTIMULANT ACTIVITY 审中-公开
标题翻译： 3-亚氨基-3-羟基-2-氨基丙酸，3-环己基-3-羟基-2-氨基 - 丙酸和相关化合物，其具有抑制和/或免疫抑制活性
公开(公告)号：WO2006081273A8
公开(公告)日：2007-03-01
申请号：PCT/US2006002557
申请日：2006-01-25
申请人： ALLERGAN INC , LEBLOND BERTRAND , BEAUSOLEIL ERIC , TAVERNE THIERRY , DONELLO JOHN E
发明人： LEBLOND BERTRAND , BEAUSOLEIL ERIC , TAVERNE THIERRY , DONELLO JOHN E
IPC分类号： C07D213/81 , A61K31/381 , A61K31/4409 , A61P29/00 , A61P37/04 , C07D213/61 , C07D213/64 , C07D213/73 , C07D215/14 , C07D295/18 , C07D307/54 , C07D333/24 , C07D333/38 , C07D333/60 , C07D401/06
CPC分类号： C07D265/30 , A61K31/40 , A61K31/4025 , A61K31/4409 , A61K31/4439 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/5375 , A61K31/5377 , A61K31/541 , C07D207/09 , C07D213/64 , C07D295/12 , C07D295/13 , C07D295/15 , C07D319/18 , C07D405/06
摘要： Compounds of Formulas (1) and (2), where the variables have the meaning disclosed in the specification, have analgesic and in some cases immunostimulant activity.
摘要翻译：式（1）和（2）的化合物，其中变量具有说明书中公开的含义，具有镇痛作用，在某些情况下具有免疫刺激活性。

9. 发明专利

CA2052234A1 AMINES ALKYL HETEROCYCLIQUES, LEUR PROCEDE DE PREPARATION ET LES COMPOSITIONS PHARMACEUTIQUES QUI LES CONTIENNENT 未知
公开(公告)号：CA2052234A1
公开(公告)日：1992-03-27
申请号：CA2052234
申请日：1991-09-25
申请人： TAVERNE THIERRY , LESIEUR ISABELLE , DEPREUX PATRICK , HENRI DANIEL , GUARDIOLA BEATRICE , ADAM GERARD , RENARD PIERRE
发明人： TAVERNE THIERRY , LESIEUR ISABELLE , DEPREUX PATRICK , CAIGNARD DANIEL H , GUARDIOLA BEATRICE , ADAM GERARD , RENARD PIERRE
IPC分类号： A61K31/42 , A61K31/423 , A61K31/425 , A61K31/428 , A61K31/44 , A61K31/495 , A61K31/496 , A61K31/505 , A61K31/535 , A61K31/536 , A61K31/5377 , A61K31/538 , A61K31/54 , A61K31/5415 , A61P9/12 , A61P25/04 , A61P25/18 , A61P25/20 , C07D263/58 , C07D265/36 , C07D277/68 , C07D279/16 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D491/056
摘要： "NOUVELLES AMINES ALKYL, HETEROCYCLIQUES, LEUR PROCEDE DE PREPARATION ET LES COMPOSITIONS PHARMACEUTIQUES QUI LES CONTIENNENT" Composé de formule générale (I) : (I) où R1, R2, R3, n, X, A sont définis dans la description, Médicaments.

10. 发明专利

DE602004001864T2 未知
公开(公告)号：DE602004001864T2
公开(公告)日：2007-09-06
申请号：DE602004001864
申请日：2004-02-27
申请人： EXONHIT THERAPEUTICS SA
发明人： LEBLOND BERTRAND , PETIT SILVERE , PICARD VIRGINIE , TAVERNE THIERRY , SCHWEIGHOFFER FABIEN
IPC分类号： C07D405/12 , A61K31/351 , A61K31/4709 , A61P35/00 , C07D411/12
摘要： Quinoline derivatives (I) and their tautomers, optical and geometrical isomers, racemates, salts, hydrates or mixtures are new. Quinoline derivatives of formula (I) and their tautomers, optical and geometrical isomers, racemates, salts, hydrates or mixtures are new. [Image] R 1pyran derivative of formula (a1), piperdine derivative of formula (a2), dihydropyrrole derivative of formula (a3), alkane derivative of formula (a4) or amine derivative of formula (a5); R 2H, 3-6C alkyl or 3-6C alkenyl; B : halo, preferably chlorine, hydroxyl, O-CH 2-O-CH 3(MOM), O-CH 2-O-CH 2-CH 2-O-CH 3(MEM), OSO 2-alkyl or OSi(CH 3) 2tBu; D : O, NR 3, CR'R'' or S; X, Y : O, S or a radical NR 4; R 3H, alkyl, carboxylate, acyl, carboxamide or SO 2-alkyl; R', R'' : H or alkyl radical; R 4H, 1-10C alkyl, aryl or aralkyl; linker : (CH 2) n; n : 1-10; (optionally interrupted by an heteroatom (preferably N, O , S and P) or a carbonyl group, or an aryldialkyl (preferably xylenyl); and A : quinoline derivative of formulae (a6-a7), benzopyrimidine derivative of formula (a8) or benzothiophene derivative of formula (a9) (all optionally substituted). [Image] ACTIVITY : Cytostatic; Antiangiogenic; Vasotropic; Antiarthritic; Antidiabetic; Ophthalmological. MECHANISM OF ACTION : None given.

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