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1. 发明申请

US20110053975A1 CHEMICAL MOLECULES THAT INHIBIT THE SLICING MECHANISM FOR TREATING DISEASES RESULTING FROM SPLICING ANOMALIES 有权
标题翻译：化学分子，禁止用于治疗由分离异常引起的疾病的机制
公开(公告)号：US20110053975A1
公开(公告)日：2011-03-03
申请号：US12811931
申请日：2009-01-12
申请人： Jamal Tazi , David Grierson , Florence Mahuteau-Betzer , Pierre Roux
发明人： Jamal Tazi , David Grierson , Florence Mahuteau-Betzer , Pierre Roux
IPC分类号： A61K31/4709 , C07D213/72 , C07D211/72 , C07D401/12 , C07D401/14 , C07D249/04 , C07D217/22 , A61K31/444 , A61K31/4439 , A61K31/4164 , A61K31/4192 , A61P31/12
CPC分类号： A61K31/166 , A61K31/417 , A61K31/4192 , A61K31/4406 , A61K31/4409 , A61K31/4439 , A61K31/4725 , C07C237/30 , C07D213/38 , C07D213/56 , C07D213/74 , C07D213/75 , C07D213/82 , C07D233/61 , C07D233/64 , C07D249/06 , C07D401/12 , C07D401/14
摘要： The present invention relates to a compound of one of the formulas I to XXI; a pharmaceutical composition comprising at least one such compound; and the use of at least one such compound in preparing a drug to treat, in a subject, a genetic disease resulting from at least one splicing anomaly.
摘要翻译：本发明涉及式I至XXI之一的化合物; 包含至少一种此类化合物的药物组合物; 以及至少一种这样的化合物在制备药物中的用途，以在受试者中治疗由至少一个拼接异常引起的遗传疾病。

2. 发明授权

US08604063B2 Chemical molecules that inhibit the slicing mechanism for treating diseases resulting from splicing anomalies 有权
标题翻译：抑制切片机制用于治疗由拼接异常引起的疾病的化学分子
公开(公告)号：US08604063B2
公开(公告)日：2013-12-10
申请号：US12811931
申请日：2009-01-12
申请人： Jamal Tazi , David Grierson , Florence Mahuteau-Betzer , Pierre Roux
发明人： Jamal Tazi , David Grierson , Florence Mahuteau-Betzer , Pierre Roux
IPC分类号： A61K31/44 , A61K31/235 , C07D213/72
CPC分类号： A61K31/166 , A61K31/417 , A61K31/4192 , A61K31/4406 , A61K31/4409 , A61K31/4439 , A61K31/4725 , C07C237/30 , C07D213/38 , C07D213/56 , C07D213/74 , C07D213/75 , C07D213/82 , C07D233/61 , C07D233/64 , C07D249/06 , C07D401/12 , C07D401/14
摘要： The present invention relates to a compound of one of the formulas I to XXI; a pharmaceutical composition comprising at least one such compound; and the use of at least one such compound in preparing a drug to treat, in a subject, a genetic disease resulting from at least one splicing anomaly.
摘要翻译：本发明涉及式I至XXI之一的化合物; 包含至少一种这样的化合物的药物组合物; 以及至少一种这样的化合物在制备药物中的用途，以在受试者中治疗由至少一个拼接异常引起的遗传疾病。

3. 发明授权

US08895726B2 Compounds derived from indole and pharmaceutical compositions containing them 有权
标题翻译：衍生自吲哚的化合物和含有它们的药物组合物
公开(公告)号：US08895726B2
公开(公告)日：2014-11-25
申请号：US12527071
申请日：2008-02-19
申请人： Fabrice Lejeune , Jamal Tazi , David Grierson , Christian Rivalle , Florence Mahuteau-Betzer
发明人： Fabrice Lejeune , Jamal Tazi , David Grierson , Christian Rivalle , Florence Mahuteau-Betzer
IPC分类号： C07D345/00 , C07D517/00 , C07D471/04 , C07D471/14 , C07D401/12
CPC分类号： C07D471/14 , C07D401/12 , C07D471/04
摘要： The present invention relates to a compound derived from indole corresponding to the following formula II: wherein X represents N, CR8 or N+R8, wherein R8 represents a hydrogen atom, a hydroxyl or alkyl or methoxy group optionally substituted with a phenyl group; R2, R3 and R4 independently represent a hydrogen atom or a halogen atom or an optionally substituted alkyl, amine, alkene, ester, sulfonamide, ether or benzyl group; R5 represents a hydrogen atom or an optionally substituted, saturated or unsaturated alkyl group, amine, benzyl group; R6 represents an optionally substituted C1-C3 alkyl group; R7 represents a hydrogen atom or an optionally substituted C1-C3 alkyl group and R7 is absent when the ring A is in the b position, and A represents a ring; R9 and R10 represent together a carbon bond or independently represent an R11 OR11, SR11 group; wherein R11 represents a hydrogen atom, an optionally substituted, saturated or unsaturated, C1-C3 alkyl group, which may contain one or more sulfur, oxygen or nitrogen atoms; pharmaceutically acceptable salts of said compounds, their isomers and/or a mixture thereof; pharmaceutical composition comprising such a compound; the use of such a compound for preparing a drug intended to treat a genetic disease resulting from at least one mutation causing the occurrence of an early termination codon.
摘要翻译：本发明涉及对应于下式II的衍生自吲哚的化合物：其中X表示N，CR8或N + R8，其中R8表示氢原子，羟基或任选被苯基取代的烷基或甲氧基; R2，R3和R4独立地表示氢原子或卤素原子或任选取代的烷基，胺，烯烃，酯，磺酰胺，醚或苄基; R5表示氢原子或任选取代的饱和或不饱和的烷基，胺，苄基; R 6表示任选取代的C 1 -C 3烷基; R7表示氢原子或任意取代的C1-C3烷基，当环A在b位时，R7不存在，A表示环; R 9和R 10一起表示碳键或独立地表示R11 OR11，SR11基团; 其中R11表示氢原子，任选取代的，饱和或不饱和的C 1 -C 3烷基，其可以含有一个或多个硫，氧或氮原子; 所述化合物的药学上可接受的盐，它们的异构体和/或它们的混合物; 包含这种化合物的药物组合物; 使用这种化合物来制备旨在治疗由引起早期终止密码子的发生的至少一个突变引起的遗传疾病的药物。

4. 发明申请

US20110003843A1 NOVEL COMPOUNDS DERIVED FROM INDOLE AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 有权
标题翻译：从含有它们的药物和药物组合物衍生的新化合物
公开(公告)号：US20110003843A1
公开(公告)日：2011-01-06
申请号：US12527071
申请日：2008-02-19
申请人： Fabrice Lejeune , Jamal Tazi , David Grierson , Christian Rivalle , Florence Mahuteau-Betzer
发明人： Fabrice Lejeune , Jamal Tazi , David Grierson , Christian Rivalle , Florence Mahuteau-Betzer
IPC分类号： A61K31/4745 , C07D471/14 , C07D471/04 , C07D217/24 , A61K31/47 , A61P9/00 , A61P21/00 , A61P27/02 , A61P11/00 , A61P17/00 , A61P13/00 , A61P1/00 , A61P15/08
CPC分类号： C07D471/14 , C07D401/12 , C07D471/04
摘要： The present invention relates to a compound derived from indole corresponding to the following formula II: wherein X represents N, CR8 or N+R8, wherein R8 represents a hydrogen atom, a hydroxyl or alkyl or methoxy group optionally substituted with a phenyl group; R2, R3 and R4 independently represent a hydrogen atom or a halogen atom or an optionally substituted alkyl, amine, alkene, ester, sulfonamide, ether or benzyl group; R5 represents a hydrogen atom or an optionally substituted, saturated or unsaturated alkyl group, amine, benzyl group; R6 represents an optionally substituted C1-C3 alkyl group; R7 represents a hydrogen atom or an optionally substituted C1-C3 alkyl group and R7 is absent when the ring A is in the b position, and A represents a ring; R9 and R10 represent together a carbon bond or independently represent an R11 OR11, SR11 group; wherein R11 represents a hydrogen atom, an optionally substituted, saturated or unsaturated, C1-C3 alkyl group, which may contain one or more sulfur, oxygen or nitrogen atoms; pharmaceutically acceptable salts of said compounds, their isomers and/or a mixture thereof; pharmaceutical composition comprising such a compound; the use of such a compound for preparing a drug intended to treat a genetic disease resulting from at least one mutation causing the occurrence of an early termination codon.
摘要翻译：本发明涉及对应于下式II的衍生自吲哚的化合物：其中X表示N，CR8或N + R8，其中R8表示氢原子，羟基或任选被苯基取代的烷基或甲氧基; R2，R3和R4独立地表示氢原子或卤素原子或任选取代的烷基，胺，烯烃，酯，磺酰胺，醚或苄基; R5表示氢原子或任选取代的饱和或不饱和的烷基，胺，苄基; R 6表示任选取代的C 1 -C 3烷基; R7表示氢原子或任意取代的C1-C3烷基，当环A在b位时，R7不存在，A表示环; R 9和R 10一起表示碳键或独立地表示R11 OR11，SR11基团; 其中R11表示氢原子，任选取代的，饱和或不饱和的C 1 -C 3烷基，其可以含有一个或多个硫，氧或氮原子; 所述化合物的药学上可接受的盐，它们的异构体和/或它们的混合物; 包含这种化合物的药物组合物; 使用这种化合物来制备旨在治疗由引起早期终止密码子的发生的至少一个突变引起的遗传疾病的药物。

5. 发明授权

US07989467B2 Use of indole-derived compounds for the preparation of a medicament that can be used to treat diseases related to the splicing process 有权
标题翻译：吲哚衍生化合物在制备可用于治疗与拼接过程有关的疾病的药物中的应用
公开(公告)号：US07989467B2
公开(公告)日：2011-08-02
申请号：US10570849
申请日：2004-09-06
申请人： Jamal Tazi , Johann Soret , Philippe Jeanteur , David Grierson , Christian Rivalle , Emile Bisagni , Chi Hung Nguyen
发明人： Jamal Tazi , Johann Soret , Philippe Jeanteur , David Grierson , Christian Rivalle , Emile Bisagni , Chi Hung Nguyen
IPC分类号： A61K31/44 , C07D211/68
CPC分类号： A61K31/4375 , A61K31/403 , A61K31/437 , A61K31/4745 , A61K31/496 , A61K31/5377 , C07D209/80 , C07D471/04 , C07D471/14
摘要： The invention relates to indole-derived compounds and to the use of said compounds for the preparation of a medicament that can be used to treat diseases related to the process of splicing pre-messenger RNAs in the cell, such as Frasier syndrome, frontotemporal dementia linked to chromosome 17 (a form of Parkinson's disease), Leigh syndrome (a type of encephalopathy), atypical cystic fibrosis, certain neuropathologies including Alzheimer's disease linked to a mutation in the Tau protein, muscle atorphy which affects the SMN (Survival of Motor Neuron) gene, depression linked to a serotonin splicing impairment, and certain cancers in which the global splicing process is affected (e.g. breast cancer, colon cancer and certain lymphomas), as well as viral diseases such as AIDS.
摘要翻译：本发明涉及吲哚衍生的化合物和所述化合物用于制备药物的用途，所述药物可用于治疗与剪接细胞中的前信使RNA的过程相关的疾病，例如Frasier综合征，额颞额痴呆到17号染色体（帕金森病的一种形式），Leigh综合征（一种脑病），非典型囊性纤维化，某些神经病理学包括与Tau蛋白突变有关的阿尔茨海默氏病，影响SMN的肌肉萎缩（运动神经元的存活）基因，与血清素剪接损伤相关的抑郁症，以及影响全球剪接过程的某些癌症（例如乳腺癌，结肠癌和某些淋巴瘤）以及病毒性疾病如艾滋病。

6. 发明申请

US20070054905A1 Use of indole-derived compounds for the preparation of a medicament that can be used to treat diseases related to the splicing process 有权
标题翻译：吲哚衍生化合物在制备可用于治疗与拼接过程有关的疾病的药物中的应用
公开(公告)号：US20070054905A1
公开(公告)日：2007-03-08
申请号：US10570849
申请日：2004-09-06
申请人： Jamal Tazi , Johann Soret , Philippe Jeanteur , David Grierson
发明人： Jamal Tazi , Johann Soret , Philippe Jeanteur , David Grierson
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/4745
CPC分类号： A61K31/4375 , A61K31/403 , A61K31/437 , A61K31/4745 , A61K31/496 , A61K31/5377 , C07D209/80 , C07D471/04 , C07D471/14
摘要： The invention relates to indole-derived compounds and to the use of said compounds for the preparation of a medicament that can be used to treat diseases related to the process of splicing pre-messenger RNAs in the cell, such as Frasier syndrome, frontotemporal dementia linked to chromonsoem 17 (a form of Parkinson's disease), Leigh syndrome (a type of encephalopathy), atypical cystic fibrosis, certain neuropathologies including Alzheimer's disease linked to a mutation in the Tau protein, muscle atorphy which affects the SMN (survival of Motor Neuron) gene, depression linked to a serotonin splicing impairment, and certain cancers in which the global splicing process is affected (e.g. breast cancer, colon cancer and certain lymphomas), as well as viral diseases such as AIDS.
摘要翻译：本发明涉及吲哚衍生的化合物和所述化合物用于制备药物的用途，所述药物可用于治疗与剪接细胞中的前信使RNA的过程相关的疾病，例如Frasier综合征，额颞额痴呆（一种形式的帕金森病），Leigh综合征（一种脑病），非典型囊性纤维化，某些神经病理学包括与Tau蛋白突变有关的阿尔茨海默氏病，影响SMN的肌肉萎缩（运动神经元的存活）基因，与血清素剪接损伤相关的抑郁症，以及影响全球剪接过程的某些癌症（例如乳腺癌，结肠癌和某些淋巴瘤）以及病毒性疾病如艾滋病。

7. 发明申请

US20110201648A1 POLY-HETEROARYL DERIVATIVES FOR THE TREATMENT OF CANCER 审中-公开
标题翻译：用于治疗癌症的多异体衍生物
公开(公告)号：US20110201648A1
公开(公告)日：2011-08-18
申请号：US13124136
申请日：2009-11-02
申请人： Chi-hung Nguyen , Myriam Rouchon Dagois , Aurore Guedin-Beaurepaire , David Monchaud , Marie-Paule Teulade-Fichou , Jean-François Riou , Jean-Louis Mergny , David Grierson
发明人： Chi-hung Nguyen , Myriam Rouchon Dagois , Aurore Guedin-Beaurepaire , David Monchaud , Marie-Paule Teulade-Fichou , Jean-François Riou , Jean-Louis Mergny , David Grierson
IPC分类号： A61K31/444 , C07D401/14 , C07D413/14 , A61K31/4439 , C07H21/04 , C07H1/00 , G01N33/48 , A61P35/00 , A61P31/00
CPC分类号： C07D413/14 , Y10T436/143333
摘要： The present invention relates to Penta-hexa-, hepta-, octa-, nona- and, deca-heteroaryl derivatives, comprising a combination of heterocycle 1 (Het-1)a and/or heterocycle 2 (Het-2)b and/or heterocycle 3 (Het-3)c and/or heterocycle 4 (Het-4)d of formulae I, II, III and IV respectively, the N-oxides, the pharmaceutically acceptable addition salts. The compounds claimed are suitable for the treatment of cancer.
摘要翻译：本发明涉及包含杂环1（Het-1）a和/或杂环2（Het-2）b和/或其杂环的组合的五 - 六 - ，七 - ，八 - ， - 和 - 或杂环3（Het-3）c和/或式I，II，III和IV的杂环4（Het-4）d，N-氧化物，药学上可接受的加成盐。所要求的化合物适用于治疗癌症。

8. 发明授权

US07981400B2 Shiga toxin B-subunit as a vector for tumor diagnosis and drug delivery to GB3 expressing tumors 有权
标题翻译：志贺毒素B亚基作为肿瘤诊断和药物递送到GB3表达肿瘤的载体
公开(公告)号：US07981400B2
公开(公告)日：2011-07-19
申请号：US12723361
申请日：2010-03-12
申请人： Ludger Johannes , David Grierson , Sylvie Robine , Jean-Claude Florent , Philipe Maillard , Jacky Roger
发明人： Ludger Johannes , David Grierson , Sylvie Robine , Jean-Claude Florent , Philipe Maillard , Jacky Roger
IPC分类号： A61K49/00 , C07K14/00
CPC分类号： A61K49/085 , A61K38/00 , A61K41/0071 , A61K47/6415 , A61K47/67 , A61K49/0008 , A61K49/14 , B82Y5/00 , C07K14/25 , C07K14/36
摘要： The invention relates to new compounds for cancer therapy or diagnosis and more specifically to the use of a non-toxic B subunit of Shiga toxin mutant as a vector for diagnostic products or drugs in over-expressing Gb3 receptor cells, such compounds having the following formula: STxB-Z(n)-Cys-Y(m)-T wherein STxB is the Shiga Toxin B subunit or a functional equivalent thereof, Z(n) wherein n is 0 or 1 and when n is 1, Z is an amino-acid residue devoid of sulfhydryl group, or is a polypeptide, Cys is the amino-acid residue for Cysteine, T is a molecule linked by a covalent bound to the S part of Cys, selected in a group comprising: agents for in vivo diagnosis, cytotoxic agents, prodrugs, or enzymes for the conversion of a prodrug to a drug, Y(m) wherein m is 0 or 1 and when m is 1, Y is a linker between T and Cys, said linker being either cleavable or not cleavable for the release of T after the internalization of the hybrid compound into said cells.
摘要翻译：本发明涉及用于癌症治疗或诊断的新化合物，更具体地涉及使用志贺毒素突变体的无毒性B亚基作为过表达Gb3受体细胞的诊断产物或药物的载体，具有下式：STxB-Z（n）-Cys-Y（m）-T其中STxB是滋贺毒素B亚基或其功能等同物，Z（n）其中n为0或1，当n为1时，Z为氨基 - 没有巯基的酸性残基，或是多肽，Cys是半胱氨酸的氨基酸残基，T是通过共价结合到Cys的S部分的分子连接的分子，所述组分选自：用于体内诊断的试剂，前药或前药转化为药物的Y（m），其中m为0或1，当m为1时，Y为T和Cys之间的接头，所述接头可切割或不切割在将杂化化合物内化至所述细胞后，可以切割T释放T。

9. 发明授权

US07718676B2 2-aminoaryloxazole compounds as tyrosine kinase inhibitors 有权
标题翻译： 2-氨基吡唑化合物作为酪氨酸激酶抑制剂
公开(公告)号：US07718676B2
公开(公告)日：2010-05-18
申请号：US10576267
申请日：2004-10-22
申请人： Alain Moussy , Camille Wermuth , David Grierson , Abdellah Benjahad , Martine Croisy , Marco Ciufolini , Bruno Giethlen
发明人： Alain Moussy , Camille Wermuth , David Grierson , Abdellah Benjahad , Martine Croisy , Marco Ciufolini , Bruno Giethlen
IPC分类号： A61K31/44 , A61K31/422 , C07D263/30 , C07D413/04
CPC分类号： C07D263/48 , C07D413/04 , C07D413/14 , E21B33/038 , E21B43/121
摘要： The present invention relates to novel compounds selected from 2-aminoaryloxazoles of formula I that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. More particularly, these compounds are potent and selective c-kit, bcr-abl, FGFR3 and/or Flt-3 inhibitors.
摘要翻译：本发明涉及选自式I的2-氨基咪唑的新化合物，其选择性调节，调节和/或抑制由涉及多种人和动物疾病如细胞增殖的某些天然和/或突变型酪氨酸激酶介导的信号转导，代谢，过敏和退行性疾病。更具体地说，这些化合物是有效和选择性的c-kit，bcr-abl，FGFR3和/或Flt-3抑制剂。

10. 发明申请

US20100113471A1 2-Aminoaryloxazole compounds as tyrosine kinase inhibitors 有权
标题翻译： 2-氨基芳唑化合物作为酪氨酸激酶抑制剂
公开(公告)号：US20100113471A1
公开(公告)日：2010-05-06
申请号：US12654957
申请日：2010-01-11
申请人： Alain Moussy , Camille Wermuth , David Grierson , Abdellah Benjahad , Martine Croisy , Marco Ciufolini , Bruno Giethlen
发明人： Alain Moussy , Camille Wermuth , David Grierson , Abdellah Benjahad , Martine Croisy , Marco Ciufolini , Bruno Giethlen
IPC分类号： A61K31/496 , A61K31/4439 , C07D413/14 , C07D413/04 , A61P41/00 , A61P35/00 , A61P35/02 , A61P37/00 , A61P29/00 , A61P1/00
CPC分类号： C07D263/48 , C07D413/04 , C07D413/14 , E21B33/038 , E21B43/121
摘要： The present invention relates to novel compounds selected from 2-aminoaryloxazoles that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic and degenerative disorders. More particularly, these compounds are potent and selective c-kit, bcr-abl, FGFR3 and/or Flt-3 inhibitors.
摘要翻译：本发明涉及选自2-氨基咪唑的新化合物，其选择性调节，调节和/或抑制由涉及多种人和动物疾病的某些天然和/或突变型酪氨酸激酶介导的信号转导，例如细胞增殖，代谢，过敏性和退行性疾病。更具体地说，这些化合物是有效和选择性的c-kit，bcr-abl，FGFR3和/或Flt-3抑制剂。

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