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1. 发明授权

US5182273A Spirocyclic N, O derivatives of cyclotriphosphazenes and their use in therapy 失效
标题翻译：环磷酰胺的螺环N，O衍生物及其在治疗中的应用
公开(公告)号：US5182273A
公开(公告)日：1993-01-26
申请号：US780480
申请日：1991-10-22
申请人： Alain Duflos , Jean-Francois Patoiseau , Dennis Bigg , Robert Kiss
发明人： Alain Duflos , Jean-Francois Patoiseau , Dennis Bigg , Robert Kiss
IPC分类号： A61K31/675 , A61P35/00 , C07F9/6593
CPC分类号： C07F9/65815
摘要： The present invention relates to compounds of the Formula I: ##STR1## wherein R is hydrogen, alkyl, cycloalkyl, phenyl, or alkylphenyl, and n is 2 through 4, the production thereof, pharmaceutical compositions thereof, and their use in antineoplastic therapy.
摘要翻译：本发明涉及式I化合物：其中R为氢，烷基，环烷基，苯基或烷基苯基，n为2至4，其制备，其药物组合物及其在抗肿瘤治疗中的用途。

2. 发明授权

US5385931A Sulfonamides derived from benzocyclic or benzoheterocyclic acids, their preparation and application in therapeutics 失效
标题翻译：衍生自苯环或苯并杂环酸的磺酰胺，其制备和在治疗中的应用
公开(公告)号：US5385931A
公开(公告)日：1995-01-31
申请号：US613842
申请日：1990-12-28
申请人： Dennis Bigg , Alain Duflos , Jean-Pierre Rieu
发明人： Dennis Bigg , Alain Duflos , Jean-Pierre Rieu
IPC分类号： A61K31/19 , A61K31/215 , A61K31/22 , A61K31/335 , A61K31/34 , A61K31/343 , A61K31/35 , A61K31/352 , A61K31/357 , A61K31/38 , A61K31/381 , A61P7/02 , C07C69/757 , C07C229/26 , C07C311/19 , C07D307/85 , C07D311/66 , C07D317/46 , C07D333/70 , C07D307/81 , C07D333/60
CPC分类号： C07D311/66 , C07C229/26 , C07C311/19 , C07C69/757 , C07D307/85 , C07D317/46 , C07D333/70 , C07C2102/08
摘要： The invention relates to new sulphonamide derivatives of benzo-cyclic or benzo-heterocyclic acids and their derivatives of general formula I ##STR1## in which: R represents a straight-chain or branched lower alkyl radical having 1 to 9 C;a phenyl radical which is unsubstituted or substituted by one or more groups:straight-chain or branched lower alkyl having 1 to 4 C, halogeno, alkoxy, nitro, amino, dialkylamino or CF.sub.3 ;a substituted or unsubstituted naphthalene;a thiophenyl radical;R.sub.1 represents a hydrogen or a straight-chain or branched lower alkyl or a benzyl;R.sub.2 represents a hydrogen, a straight-chain or branched lower alkyl group, a substituted or unsubstituted phenyl group or an aralkyl group;R.sub.3 represents a hydrogen or a straight-chain or branched lower alkyl (1 to 6 C);--X-- represents a divalent functional radical chosen from the following: --CH.sub.2 --; ##STR2## where R.sub.4 =H or Me; A represents a benzo-cyclic or benzo-heterocyclic divalent radical chosen from the following (a) to (j): ##STR3## and n can assume the values 1 to 4 inclusive; and the therapeutically acceptable organic or inorganic salts (R.sub.3 =H), the pure isomers or diastereoisomers or their mixture and all the pharmaceutical compositions of formula I with other active principles.The invention relates to the application of I as a medicament and the preparation processes.
摘要翻译： PCT No.PCT / FR90 / 00234 Sec。 371 1990年12月28日第 102（e）1990年12月28日日期PCT提交1990年4月4日PCT公布。 WO90 / 12007 PCT出版物日本1990年10月18日。本发明涉及苯并环或苯并杂环酸的新磺酰胺衍生物及其通式I的衍生物或具有1〜9个C的支链低级烷基; 未取代或被一个或多个基团取代的苯基：具有1-4个碳原子的直链或支链低级烷基，卤代，烷氧基，硝基，氨基，二烷基氨基或CF 3; 取代或未取代的萘; 硫代苯基; R1表示氢或直链或支链的低级烷基或苄基; R2表示氢，直链或支链的低级烷基，取代或未取代的苯基或芳烷基; R3表示氢或直链或支链的低级烷基（1-6）; -X-表示选自以下的二价官能团：-CH 2 - ; 其中R4 = H或Me; A表示选自以下（a）至（j）的苯并环或苯并杂环二价基团：（a）GE（e）图像（f）（h）（i）（j），n可以取值1〜4，和治疗上可接受的有机或无机盐（R3 = H），纯异构体或非对映异构体或其混合物以及具有其它活性成分的式I的所有药物组合物。本发明涉及I作为药物的应用及其制备方法。

3. 发明授权

US08101180B2 Anti-IGF-IR and/or anti-insulin/IGF-I hybrid receptors antibodies and uses thereof 有权
标题翻译：抗IGF-1R和/或抗胰岛素/ IGF-I杂合受体抗体及其用途
公开(公告)号：US08101180B2
公开(公告)日：2012-01-24
申请号：US12388534
申请日：2009-02-19
申请人： Liliane Goetsch , Nathalie Corvaia , Alain Duflos , Jean-Francois Haeuw , Olivier Leger , Alain Beck
发明人： Liliane Goetsch , Nathalie Corvaia , Alain Duflos , Jean-Francois Haeuw , Olivier Leger , Alain Beck
IPC分类号： A61K39/00 , A61K39/395 , A61K51/10 , G01N33/53 , G01N33/574 , G01N33/561 , G01N33/557 , G01N33/566
CPC分类号： A61K47/6805 , C07K2317/732
摘要： The present invention relates to novel antibodies capable of binding specifically to the human insulin-like growth factor I receptor (IGF-IR) and/or the insulin/IGF-I hybrid receptor (hybrid-R) and/or capable of specifically inhibiting the tyrosine kinase activity of said IGF-IR and/or hybrid-R, especially monoclonal antibodies of murine, chimeric and humanized origin, as well as the amino acid and nucleic acid sequences coding for these antibodies. The invention likewise comprises the use of these antibodies as a medicament for the prophylactic and/or therapeutic treatment of cancers overexpressing IGF-IR and/or hybrid-R or any pathology connected with the overexpression of said receptor as well as in processes or kits for diagnosis of illnesses connected with the overexpression of the IGF-IR and/or hybrid-R. The invention finally comprises products and/or compositions comprising such antibodies in combination with anti-EGFR antibodies and/or compounds and/or anti-cancer agents or agents conjugated with toxins and their use for the prevention and/or the treatment of certain cancers.
摘要翻译：本发明涉及能够特异性结合人胰岛素样生长因子I受体（IGF-1R）和/或胰岛素/ IGF-I杂合受体（杂合-R）和/或能够特异性抑制所述IGF-1R和/或杂种-R，特别是鼠，嵌合和人源化起始的单克隆抗体以及编码这些抗体的氨基酸和核酸序列的酪氨酸激酶活性。本发明同样包括使用这些抗体作为用于预防和/或治疗过度表达IGF-1R和/或杂合-R的癌症或与所述受体的过度表达相关的任何病理学以及在用于诊断与IGF-1R和/或杂合体R的过表达相关的疾病。本发明最终包括包含抗体与抗EGFR抗体和/或化合物和/或与毒素缀合的抗癌剂或试剂的组合的产品和/或组合物及其用于预防和/或治疗某些癌症的用途。

4. 发明授权

US08168410B2 Anti-IGF-IR antibodies and uses thereof 有权
标题翻译：抗IGF-1R抗体及其用途
公开(公告)号：US08168410B2
公开(公告)日：2012-05-01
申请号：US13037734
申请日：2011-03-01
申请人： Liliane Goetsch , Nathalie Corvaia , Olivier Leger , Alain Duflos , Jean-François Haeuw , Alain Beck
发明人： Liliane Goetsch , Nathalie Corvaia , Olivier Leger , Alain Duflos , Jean-François Haeuw , Alain Beck
IPC分类号： C12P19/34 , C12N15/00 , C12N15/13 , C07H21/04 , C07K16/28
CPC分类号： A61K47/6805 , C07K2317/732 , Y10S425/81
摘要： The present invention relates to novel antibodies capable of binding specifically to the human insulin-like growth factor I receptor IGF-IR and/or capable of specifically inhibiting the tyrosine kinase activity of said IGF-IR receptor, especially monoclonal antibodies of murine, chimeric and humanized origin, as well as the amino acid and nucleic acid sequences coding for these antibodies. The invention likewise comprises the use of these antibodies as a medicament for the prophylactic and/or therapeutic treatment of cancers overexpressing IGF-IR or any pathology connected with the overexpression of said receptor as well as in processes or kits for diagnosis of illnesses connected with the overexpression of the IGF-IR receptor. The invention finally comprises products and/or compositions comprising such antibodies in combination with anti-EGFR antibodies and/or compounds and/or anti-cancer agents or agents conjugated with toxins and their use for the prevention and/or the treatment of certain cancers.
摘要翻译：本发明涉及能够特异性结合人类胰岛素样生长因子I受体IGF-1R和/或能够特异性抑制所述IGF-1R受体的酪氨酸激酶活性的新型抗体，特别是鼠，嵌合体的单克隆抗体，人源化，以及编码这些抗体的氨基酸和核酸序列。本发明同样包括使用这些抗体作为用于预防和/或治疗过度表达IGF-1R的癌症或与所述受体的过度表达相关的任何病理学以及用于诊断与所述受体相关的疾病的过程或试剂盒 IGF-1R受体的过度表达。本发明最终包括包含抗体与抗EGFR抗体和/或化合物和/或与毒素缀合的抗癌剂或试剂的这些抗体及其用于预防和/或治疗某些癌症的用途的产品和/或组合物。

5. 发明申请

US20080063639A1 Method for the treatment of psoriasis comprising novel anti-IGF-IR antibodies 审中-公开
标题翻译：用于治疗牛皮癣的方法，其包含新的抗IGF-1R抗体
公开(公告)号：US20080063639A1
公开(公告)日：2008-03-13
申请号：US11783666
申请日：2007-04-11
申请人： Liliane Goetsch , Nathalie Corvaia , Olivier Leger , Alain Duflos , Jean-Francois Haeuw , Alain Beck , Yann Duflos
发明人： Liliane Goetsch , Nathalie Corvaia , Olivier Leger , Alain Duflos , Jean-Francois Haeuw , Alain Beck , Yann Duflos
IPC分类号： A61K39/395 , A61P17/06
CPC分类号： A61K47/6805 , C07K2317/732
摘要： The present invention relates to a method for the prevention or for the treatment of psoriasis comprising administering to a patient in need thereof an effective amount of an isolated antibody, or one of its functional fragments, capable of binding to the human insulin-like growth factor I receptor IGF-IR. The present invention is also directed to said method wherein a second compound selected from the compounds capable of specifically inhibiting the attachment of the EGF to the human epidermal growth factor receptor EGFR, such as an isolated anti-EGFR antibody, or a functional fragment thereof, is administered to the patient in addition to the anti-IGR-IR antibody.
摘要翻译：本发明涉及一种预防或治疗牛皮癣的方法，包括向有需要的患者施用有效量的能够结合人类胰岛素样生长因子的分离抗体或其功能片段之一 I受体IGF-1R。本发明还涉及所述方法，其中选自能够特异性抑制EGF与人表皮生长因子受体EGFR（例如分离的抗EGFR抗体或其功能片段）附着的化合物的第二化合物，除了抗IGR-IR抗体外还施用于患者。

6. 发明申请

US20120208721A1 NOVEL ANTI-IGF-IR AND/OR ANTI-INSULIN/IGF-I HYBRID RECEPTORS ANTIBODIES AND USES THEREOF 有权
标题翻译：新型抗IGF-1R和/或抗胰蛋白胨/ IGF-I混合受体抗体及其用途
公开(公告)号：US20120208721A1
公开(公告)日：2012-08-16
申请号：US13352599
申请日：2012-01-18
申请人： Liliane GOETSCH , Nathalie Corvaia , Alain Duflos , Jean-Francois Haeuw , Olivier Leger , Alain Beck
发明人： Liliane GOETSCH , Nathalie Corvaia , Alain Duflos , Jean-Francois Haeuw , Olivier Leger , Alain Beck
IPC分类号： C40B30/06 , C40B30/00
CPC分类号： A61K47/6805 , C07K2317/732
摘要： The present invention relates to methods of identifying IGF-IR modulators and hybrid-R modulators comprising contacting IGF-IR with a humanized anti-IGF-IR antibody and contacting hybrid-R with a humanized anti-hybrid-R antibody, respectively.
摘要翻译：本发明涉及鉴定IGF-1R调节剂和杂合-R调节剂的方法，其包括将IGF-1R与人源化抗IGF-1R抗体接触并分别使杂交-R与人源化抗混合-R抗体接触。

7. 发明申请

US20110014122A1 NOVEL ANTI-IGF-IR AND/OR ANTI-INSULIN/IGF-I HYBRID RECEPTORS ANTIBODIES AND USES THEREOF 有权
标题翻译：新型抗IGF-1R和/或抗胰蛋白胨/ IGF-I混合受体抗体及其用途
公开(公告)号：US20110014122A1
公开(公告)日：2011-01-20
申请号：US12388534
申请日：2009-02-19
申请人： Liliane GOETSCH , Nathalie Corvaia , Alain Duflos , Jean-Francois Haeuw , Olivier Leger , Alain Beck
发明人： Liliane GOETSCH , Nathalie Corvaia , Alain Duflos , Jean-Francois Haeuw , Olivier Leger , Alain Beck
IPC分类号： A61K49/00 , C07K16/00 , A61K39/395 , A61P35/00 , C12N5/071 , C12N5/09 , C40B30/04
CPC分类号： A61K47/6805 , C07K2317/732
摘要： The present invention relates to novel antibodies capable of binding specifically to the human insulin-like growth factor I receptor (IGF-IR) and/or the insulin/IGF-I hybrid receptor (hybrid-R) and/or capable of specifically inhibiting the tyrosine kinase activity of said IGF-IR and/or hybrid-R, especially monoclonal antibodies of murine, chimeric and humanized origin, as well as the amino acid and nucleic acid sequences coding for these antibodies. The invention likewise comprises the use of these antibodies as a medicament for the prophylactic and/or therapeutic treatment of cancers overexpressing IGF-IR and/or hybrid-R or any pathology connected with the overexpression of said receptor as well as in processes or kits for diagnosis of illnesses connected with the overexpression of the IGF-IR and/or hybrid-R. The invention finally comprises products and/or compositions comprising such antibodies in combination with anti-EGFR antibodies and/or compounds and/or anti-cancer agents or agents conjugated with toxins and their use for the prevention and/or the treatment of certain cancers.
摘要翻译：本发明涉及能够特异性结合人胰岛素样生长因子I受体（IGF-1R）和/或胰岛素/ IGF-I杂合受体（杂合-R）和/或能够特异性抑制所述IGF-1R和/或杂种-R，特别是鼠，嵌合和人源化起始的单克隆抗体以及编码这些抗体的氨基酸和核酸序列的酪氨酸激酶活性。本发明同样包括使用这些抗体作为预防和/或治疗过度表达IGF-1R和/或杂合-R的癌症或与所述受体的过度表达相关的任何病理学以及用于诊断与IGF-1R和/或杂合体R的过表达相关的疾病。本发明最终包括包含抗体与抗EGFR抗体和/或化合物和/或与毒素缀合的抗癌剂或试剂的组合的产品和/或组合物及其用于预防和/或治疗某些癌症的用途。

8. 发明申请

US20050249730A1 Novel anti-IGF-IR and/or anti-insulin/IGF-I hybrid receptors antibodies and uses thereof 有权
标题翻译：新型抗IGF-1R和/或抗胰岛素/ IGF-I杂合体受体抗体及其用途
公开(公告)号：US20050249730A1
公开(公告)日：2005-11-10
申请号：US11012353
申请日：2004-12-16
申请人： Liliane Goetsch , Nathalie Corvaia , Alain Duflos , Jean-Francois Haeuw , Olivier Leger , Alain Beck
发明人： Liliane Goetsch , Nathalie Corvaia , Alain Duflos , Jean-Francois Haeuw , Olivier Leger , Alain Beck
IPC分类号： A61K47/48 , A61K39/395 , C07K16/30
CPC分类号： A61K47/6805 , C07K2317/732
摘要： The present invention relates to novel antibodies capable of binding specifically to the human insulin-like growth factor I receptor (IGF-IR) and/or the insulin/IGF-I hybrid receptor (hybrid-R) and/or capable of specifically inhibiting the tyrosine kinase activity of said IGF-IR and/or hybrid-R, especially monoclonal antibodies of murine, chimeric and humanized origin, as well as the amino acid and nucleic acid sequences coding for these antibodies. The invention likewise comprises the use of these antibodies as a medicament for the prophylactic and/or therapeutic treatment of cancers overexpressing IGF-IR and/or hybrid-R or any pathology connected with the overexpression of said receptor as well as in processes or kits for diagnosis of illnesses connected with the overexpression of the IGF-IR and/or hybrid-R. The invention finally comprises products and/or compositions comprising such antibodies in combination with anti-EGFR antibodies and/or compounds and/or anti-cancer agents or agents conjugated with toxins and their use for the prevention and/or the treatment of certain cancers.
摘要翻译：本发明涉及能够特异性结合人胰岛素样生长因子I受体（IGF-1R）和/或胰岛素/ IGF-I杂合受体（杂合-R）和/或能够特异性抑制所述IGF-1R和/或杂种-R，特别是鼠，嵌合和人源化起始的单克隆抗体以及编码这些抗体的氨基酸和核酸序列的酪氨酸激酶活性。本发明同样包括使用这些抗体作为用于预防和/或治疗过度表达IGF-1R和/或杂合-R的癌症或与所述受体的过度表达相关的任何病理学以及在用于诊断与IGF-1R和/或杂合体R的过表达相关的疾病。本发明最终包括包含抗体与抗EGFR抗体和/或化合物和/或与毒素缀合的抗癌剂或试剂的组合的产品和/或组合物及其用于预防和/或治疗某些癌症的用途。

9. 发明授权

US6127377A Vinca alkaloid antimitotic halogenated derivatives 有权
标题翻译：长春花碱类抗生素卤化衍生物
公开(公告)号：US6127377A
公开(公告)日：2000-10-03
申请号：US402678
申请日：1999-10-07
申请人： Alain Duflos , Jacques Fahy , Valerie Thillaye du Boullay , Jean-Marc Barret , Bridget Hill
发明人： Alain Duflos , Jacques Fahy , Valerie Thillaye du Boullay , Jean-Marc Barret , Bridget Hill
IPC分类号： A61K31/395 , A61K31/439 , A61P35/00 , C07D519/00 , C07D519/04 , A61K31/475 , A61P37/90
CPC分类号： C07D519/04
摘要： The invention concerns novel halogenated derivatives of the vinblastine and vinorelbine family, corresponding to general formula (I) and their therapeutically acceptable salts. The invention also concerns the application of these compounds in therapy and their method of preparation. The invention further concerns a novel method for preparing vinflunine or 20',20'-difluoro-3',4'-dihydrovinorelbine, of formula (a). ##STR1##
摘要翻译： PCT No.PCT / FR98 / 00730 Sec。 371 1999年10月7日第 102（e）日期1999年10月7日PCT提交1998年4月10日PCT公布。 WO98 / 45301 PCT出版物日期1998年10月15日本发明涉及长春花碱和长春瑞滨家族的新型卤代衍生物，对应于通式（I）及其治疗上可接受的盐。本发明还涉及这些化合物在治疗中的应用及其制备方法。本发明还涉及式（a）的维生素或20'，20'-二氟-3'，4'-二氢维罗瑞伦的新方法。

10. 发明申请

US20110183376A1 NOVEL ANTI-IGF-IR ANTIBODIES AND USES THEREOF 有权
标题翻译：新型抗IGF-1R抗体及其用途
公开(公告)号：US20110183376A1
公开(公告)日：2011-07-28
申请号：US13037734
申请日：2011-03-01
申请人： Liliane GOETSCH , Nathalie Corvaia , Olivier Leger , Alain Duflos , Jean-François Haeuw , Alain Beck
发明人： Liliane GOETSCH , Nathalie Corvaia , Olivier Leger , Alain Duflos , Jean-François Haeuw , Alain Beck
IPC分类号： C12P21/04 , C07H21/04 , C12N15/63 , C12N5/10
CPC分类号： A61K47/6805 , C07K2317/732 , Y10S425/81
摘要： The present invention relates to novel antibodies capable of binding specifically to the human insulin-like growth factor I receptor IGF-IR and/or capable of specifically inhibiting the tyrosine kinase activity of said IGF-IR receptor, especially monoclonal antibodies of murine, chimeric and humanized origin, as well as the amino acid and nucleic acid sequences coding for these antibodies. The invention likewise comprises the use of these antibodies as a medicament for the prophylactic and/or therapeutic treatment of cancers overexpressing IGF-IR or any pathology connected with the overexpression of said receptor as well as in processes or kits for diagnosis of illnesses connected with the overexpression of the IGF-IR receptor. The invention finally comprises products and/or compositions comprising such antibodies in combination with anti-EGFR antibodies and/or compounds and/or anti-cancer agents or agents conjugated with toxins and their use for the prevention and/or the treatment of certain cancers.
摘要翻译：本发明涉及能够特异性结合人类胰岛素样生长因子I受体IGF-1R和/或能够特异性抑制所述IGF-1R受体的酪氨酸激酶活性的新型抗体，特别是鼠，嵌合体的单克隆抗体，人源化，以及编码这些抗体的氨基酸和核酸序列。本发明同样包括使用这些抗体作为用于预防和/或治疗过度表达IGF-1R的癌症或与所述受体的过度表达相关的任何病理学以及用于诊断与所述受体相关的疾病的过程或试剂盒 IGF-1R受体的过度表达。本发明最终包括包含抗体与抗EGFR抗体和/或化合物和/或与毒素缀合的抗癌剂或试剂的组合的产品和/或组合物及其用于预防和/或治疗某些癌症的用途。

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