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1. 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。

2. 发明申请

WO2004029089A2 NOVEL ANGIOGENESIS TARGET AND USES THEREOF 审中-公开
标题翻译：新的血管生成目标及其应用
公开(公告)号：WO2004029089A2
公开(公告)日：2004-04-08
申请号：PCT/FR0302810
申请日：2003-09-24
申请人： EXONHIT THERAPEUTICS SA , SCHWEIGHOFFER FABIEN , PETIT SILVERE , VALENTIN EMMANUEL
发明人： SCHWEIGHOFFER FABIEN , PETIT SILVERE , VALENTIN EMMANUEL
IPC分类号： A61K38/00 , A61P9/10 , A61P17/00 , A61P19/02 , A61P35/00 , C07K14/705 , C12N15/12
CPC分类号： C07K14/705 , A61K38/00
摘要： The invention relates to the biology and health field. More specifically, the invention relates to the identification and functional characterisation of a novel protein involved in the vascular permeability, cell adhesion and angiogenesis mechanisms and to the use of the aforementioned protein as a therapeutic, diagnostic or screening target. The invention also relates to the tools which can be used to perform therapeutic, diagnostic or screening methods such as, for example, probes, antibodies, vectors, recombinant cells, etc. The invention is intended, in particular, to be employed for the preparation of pharmaceutical compounds used in the field of cancers, angiogenesis, inflammatory diseases or tissue alterations.
摘要翻译：本发明涉及生物学和健康领域。更具体地说，本发明涉及涉及血管渗透性，细胞粘附和血管生成机制的新蛋白质的鉴定和功能表征，并涉及前述蛋白质作为治疗，诊断或筛选目标的用途。本发明还涉及可用于进行治疗，诊断或筛选方法的工具，例如探针，抗体，载体，重组细胞等。本发明特别旨在用于制备用于癌症领域的药物化合物，血管生成，炎性疾病或组织改变。

3. 发明专利

AU2003299096A8 Novel angiogenesis target and uses thereof 未知
公开(公告)号：AU2003299096A8
公开(公告)日：2004-04-19
申请号：AU2003299096
申请日：2003-09-24
申请人： EXONHIT THERAPEUTICS SA
发明人： PETIT SILVERE , VALENTIN EMMANUEL , SCHWEIGHOFFER FABIEN
IPC分类号： A61K38/00 , A61P9/10 , A61P17/00 , A61P19/02 , A61P35/00 , C07K14/705 , C12N15/12 , A61K31/7088 , C07K16/28 , C12N15/11

4. 发明专利

AT335734T 未知
公开(公告)号：AT335734T
公开(公告)日：2006-09-15
申请号：AT04715422
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： A61K31/351 , A61K31/4709 , A61P35/00 , C07D405/12 , 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.

5. 发明专利

AU2004215577A1 Novel compounds and methods of treating cell proliferative diseases, retinopathies and arthritis 未知
公开(公告)号：AU2004215577A1
公开(公告)日：2004-09-10
申请号：AU2004215577
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： A61K31/351 , A61K31/4709 , A61P35/00 , C07D405/12 , 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.

6. 发明专利

FR2844713A1 Use of inhibitor of FLJ protein, for treatment and prevention of e.g. cancer, diabetic retinopathy or arthritis, also new protein, nucleic acid and their inhibitors 未知
公开(公告)号：FR2844713A1
公开(公告)日：2004-03-26
申请号：FR0211853
申请日：2002-09-25
申请人： EXONHIT THERAPEUTICS SA
发明人： SCHWEIGHOFFER FABIEN , PETIT SILVERE , VALENTIN EMMANUEL
IPC分类号： A61K38/00 , A61P9/10 , A61P17/00 , A61P19/02 , A61P35/00 , C07K14/705 , C12N15/12 , A61K31/7088 , A61K39/395 , C07H21/00 , C07K14/47 , C07K16/18 , C12N15/63 , C12Q1/68 , G01N33/68
摘要： Use of an inhibitor (I) of the FLJ protein to prepare a composition for (i) treating or preventing cancers, including metastatic spread; (ii) inhibiting angiogenesis; (iii) treating diabetic retinopathy, osteoarthritis, rheumatoid arthritis, psoriasis and disorders of delayed healing; (iv) regulating vascular or paracellular permeability or (v) preserving or restoring tissue integrity. Independent claims are also included for: (1) antibodies (Ab) specific for FLJ protein; (2) antisense nucleic acid that inhibits transcription of the FLJ gene or translation of the corresponding mRNA; (3) cytotoxic ligand specific for FLJ protein containing cytotoxic and FLJ-specific segments; (4) human FLJ having a 226 amino acid sequence (2), reproduced; (5) nucleic acid probes for detecting the FLJ gene (or its mRNA) by selective hybridization, comprising at least part of a 1871 bp sequence (1), reproduced; (6) primer comprising a single-stranded nucleic acid of 5-60 nucleotides complementary to part of (1) or its complement; (7) detecting a disease (or predisposition), also for monitoring and staging, by determining the amount, relative or absolute, or distribution of FLJ protein, its expression, altered forms or the corresponding gene or mRNA; (8) selecting, screening, characterizing, optimizing or producing active compounds (A) by determining their capacity to interact with FLJ protein or to modify its expression or activity; (9) cloning and expression vector containing nucleic acid that encodes FLJ protein; and (10) recombinant cell containing the vector of (9) or nucleic acid that encodes and expresses FLJ protein.

7. 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.

8. 发明专利

DE602004001864D1 未知
公开(公告)号：DE602004001864D1
公开(公告)日：2006-09-21
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.

9. 发明专利

CA2516239A1 COMPOUNDS AND METHODS OF TREATING CELL PROLIFERATIVE DISEASES, RETINOPATHIES AND ARTHRITIS 未知
公开(公告)号：CA2516239A1
公开(公告)日：2004-09-10
申请号：CA2516239
申请日：2004-02-27
申请人： EXONHIT THERAPEUTICS SA
发明人： PICARD VIRGINIE , TAVERNE THIERRY , SCHWEIGHOFFER FABIEN , PETIT SILVERE , LEBLOND BERTRAND
IPC分类号： A61K31/351 , A61K31/4709 , A61P35/00 , C07D405/12 , 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.

10. 发明专利

FR2849055A1 Using inhibitors of protein FKBP65 for treating cancer and other diseases where angiogenesis is involved, also new isoforms of FKBP65, related nucleic acids and diagnostic uses 未知
公开(公告)号：FR2849055A1
公开(公告)日：2004-06-25
申请号：FR0216123
申请日：2002-12-18
申请人： EXONHIT THERAPEUTICS SA
发明人： SCHWEIGHOFFER FABIEN , PETIT SILVERE , VALENTIN EMMANUEL
IPC分类号： A61K38/00 , A61P9/00 , A61P17/00 , A61P29/00 , A61P35/00 , C12N9/90 , C12N15/61 , A61K31/453 , A61K39/395 , A61K48/00 , C07H21/00 , C12N15/63 , C12Q1/68 , G01N33/573 , G01N33/68
摘要： Use of an inhibitor (A) of protein FKBP65 to prepare a composition for treating cancer; for inhibiting angiogenesis, and for treating diabetic retinopathy, macular degeneration, atherosclerosis, arthritis, rheumatoid polyarthritis, psoriasis and disorders of wound healing. Independent claims are also included for the following: (1) polypeptides (I) having any of 3 sequences (644, 601 and 431 amino acids (aa), reproduced) or their fragments; (2) nucleic acid (II) that encodes (I); (3) nucleic acid probes (III) that can detect the FKBP65 gene, or corresponding RNA, by selective hybridization, containing at least part of any of 4 sequences (2641 (1), 2824 (3), 2698 (5) or 2630 (7) bp, reproduced), or their fragments; (4) single-stranded primer (IV) that contains 6-50 nucleotides (nt) complementary to at least part of sequence (1), (3), (5) or (7), to their complements or their border regions; (5) method for detecting a disease, or predisposition, or for monitoring or staging, by detecting the presence, amount or distribution of FKBP65 protein, its expression, altered forms of it, or the corresponding mRNA; (6) method for selecting, screening, characterizing, optimizing or producing active compounds by determining their capacity to interact with FKBP65 (gene or protein) or to modulate its expression or activity; (7) cloning or expression vector that contains (II); and (8) recombinant cells containing the vector of (7) or (II).

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