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1. 发明授权

US08481586B2 Pyrrolo[2,3-a] carbazoles and use thereof as PIM kinase inhibitors 失效
标题翻译：吡咯并[2,3-a]咔唑及其作为PIM激酶抑制剂的用途
公开(公告)号：US08481586B2
公开(公告)日：2013-07-09
申请号：US13002423
申请日：2009-06-25
申请人： Fabrice Anizon , Pascale Moreau , Michelle Prudhomme , Philip Cohen , Bettina Aboab , Rufine Akue-Gedu , Emilie Rossignol
发明人： Fabrice Anizon , Pascale Moreau , Michelle Prudhomme , Philip Cohen , Bettina Aboab , Rufine Akue-Gedu , Emilie Rossignol
IPC分类号： A61K31/403 , C07D209/82 , C07D209/86
CPC分类号： A61K31/407 , C07D487/04
摘要： The invention relates to pyrrolo[2,3-a]carbazole derivatives, to a method for preparing the same, and to the use thereof as PIM kinase inhibitors. The invention can particularly be used in the pharmaceutical field.
摘要翻译：本发明涉及吡咯并[2,3-a]咔唑衍生物，其制备方法及其作为PIM激酶抑制剂的用途。本发明可以特别用于制药领域。

2. 发明申请

US20110263669A1 Novel Pyrrolo [2,3-A] Carbazoles and Use Thereof as PIM Kinase Inhibitors 失效
标题翻译：新型吡咯并[2,3-A]咔唑及其用途作为PIM激酶抑制剂
公开(公告)号：US20110263669A1
公开(公告)日：2011-10-27
申请号：US13002423
申请日：2009-06-25
申请人： Fabrice Anizon , Pascale Moreau , Michelle Prudhomme , Philip Cohen , Bettina Aboab , Rufine Akue-Gedu , Emilie Rossignol
发明人： Fabrice Anizon , Pascale Moreau , Michelle Prudhomme , Philip Cohen , Bettina Aboab , Rufine Akue-Gedu , Emilie Rossignol
IPC分类号： A61K31/407 , A61P35/00 , A61P3/10 , C07D487/04 , A61P9/00
CPC分类号： A61K31/407 , C07D487/04
摘要： The invention relates to pyrrolo[2,3-a]carbazole derivatives, to a method for preparing the same, and to the use thereof as PIM kinase inhibitors. The invention can particularly be used in the pharmaceutical field.
摘要翻译：本发明涉及吡咯并[2,3-a]咔唑衍生物，其制备方法及其作为PIM激酶抑制剂的用途。本发明可以特别用于制药领域。

3. 发明授权

US07727950B2 Methods and reagents for assaying protein kinase activity 有权
标题翻译：用于测定蛋白激酶活性的方法和试剂
公开(公告)号：US07727950B2
公开(公告)日：2010-06-01
申请号：US10510875
申请日：2003-03-26
申请人： Chris Armstrong , Philip Cohen
发明人： Chris Armstrong , Philip Cohen
IPC分类号： A61K38/00 , A61K38/04 , A61K38/10 , C07K16/00 , G01N33/53
CPC分类号： C12Q1/485
摘要： A kit of parts comprising two or more protein kinase substrate polypeptides, each said substrate polypeptide comprising a specificity conferring portion (which is different for each said kinase substrate polypeptide) and a phosphorylatable portion, wherein the phosphorylatable portions of each polypeptide are capable of being bound in a phosphorylation state-sensitive manner by the same specific binding partner, for example and antibody preparation, and wherein the said specific binding partner is not an antibody specific for phosphotyrosine, phosphoserine or phosphothreonine. The phosphorylatable portion preferably comprises the amino acid sequence LSFAEPG.
摘要翻译：一种包含两种或多种蛋白激酶底物多肽的试剂盒，每种所述底物多肽包含特异性赋予部分（其对于每种所述激酶底物多肽不同）和可磷酸化部分，其中每个多肽的可磷酸化部分能够结合以相同的特异性结合配偶体（例如抗体制剂）以磷酸化状态敏感的方式，并且其中所述特异性结合配偶体不是对磷酸酪氨酸，磷酸丝氨酸或磷酸苏氨酸具有特异性的抗体。可磷酸化部分优选包含氨基酸序列LSFAEPG。

4. 发明授权

US07122360B1 Polypeptides, polynucleotides and uses thereof 有权
标题翻译：多肽，多核苷酸及其用途
公开(公告)号：US07122360B1
公开(公告)日：2006-10-17
申请号：US09720582
申请日：1999-06-08
申请人： Dario Alessi , Marin Deak , Philip Cohen , Matilde Caivano
发明人： Dario Alessi , Marin Deak , Philip Cohen , Matilde Caivano
IPC分类号： C12N9/12 , C12N1/20 , C12N15/00 , C07K1/00 , C07H21/04
CPC分类号： C12N9/0083 , A61K31/352 , A61K31/4409 , A61K38/00 , C07K2319/00 , C12N9/1205 , Y10S435/81
摘要： Substantially pure two kinase domain protein kinases comprising the amino acid sequences provided in the description, variants, fusions, fragments, or derivatives thereof useful in screening assays for drugs. Applications thereof in the modulation of CREB, COX2 and IL2 activities.
摘要翻译：基本上纯的两个激酶结构域蛋白激酶，其包含在用于药物筛选测定的描述，变体，融合物，片段或衍生物中提供的氨基酸序列。其用于调节CREB，COX2和IL2活性。

5. 发明授权

US06686467B2 Amide derivatives for the treatment of diseases mediated by cytokines 失效
标题翻译：用于治疗由细胞因子介导的疾病的酰胺衍生物
公开(公告)号：US06686467B2
公开(公告)日：2004-02-03
申请号：US10265736
申请日：2002-10-08
申请人： Dearg S Brown , George R Brown , Philip Cohen
发明人： Dearg S Brown , George R Brown , Philip Cohen
IPC分类号： C07D41300
CPC分类号： C07D295/185 , A61K31/167 , A61K31/196 , A61K31/277 , A61K31/495 , A61K31/5375 , A61K31/5377 , A61K31/54 , C07C235/56 , C07C235/84 , C07C237/40 , C07C237/42 , C07C255/57 , C07C2601/08 , C07C2601/14 , C07D295/155
摘要： The invention concerns the use of amide derivatives of formula (I) wherein: R1 and R2 are substituents such as hydroxy, C1-6alkoxy, mercapto, C1-6alkylthio, amino, C1-6alkylamino and di-(C1-6alkyl)amino; m and p are independently 0-3; R3 is C1-4alkyl; q is 0-4; and R4 is aryl or cycloalkyl; or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for use in the treatment of diseases or medical conditions mediated by cytokines
摘要翻译：本发明涉及式（I）的酰胺衍生物的用途，其中：R 1和R 2是取代基，例如羟基，C 1-6烷氧基，巯基，C 1-6烷硫基，氨基，C 1-6烷基氨基和二（C1 -6-烷基）氨基; m和p独立为0-3; R 3是C 1-4烷基; q为0-4; 和R 4是芳基或环烷基; 或其药学上可接受的盐在制备用于治疗由细胞因子介导的疾病或医学病症的药物中的用途

6. 发明授权

US07083511B1 Methods 失效
标题翻译：方法
公开(公告)号：US07083511B1
公开(公告)日：2006-08-01
申请号：US09868131
申请日：1999-12-14
申请人： Philip Cohen , Takayasu Kobayashi , Maria Deak
发明人： Philip Cohen , Takayasu Kobayashi , Maria Deak
IPC分类号： C12Q1/48 , C12N9/12 , C12N1/20 , C07H21/04
CPC分类号： C12N9/1205 , C12Q1/485
摘要： A method of activating serum and glucocorticoid-induced protein kinase (SGK) is provided wherein the SGK is phosphorylated. The SGK may be phosphorylated by PDK1 and/or a preparation containing PDK2 activity. A method of identifying a compound that modulates the activity of SGK is provided, wherein the activity of SGK is measured by measuring the phosphorylation by SGK of a polypeptide comprising an amino acid sequence corresponding to the consensus sequence (Arg/Lys; preferably Arg)-X-(X/Arg)-X-X-Ser/Thr)-Z wherein X indicates any amino acid, X/Arg indicates any amino acid, with a preference for arginine, and Z indicates that the amino acid residue is preferably a hydrophobic residue. The SGK may be activated by phosphorylation.
摘要翻译：提供了激活血清和糖皮质激素诱导的蛋白激酶（SGK）的方法，其中SGK被磷酸化。 SGK可以被PDK1和/或含有PDK2活性的制剂磷酸化。提供了鉴定调节SGK活性的化合物的方法，其中SGK的活性通过测量SGK对包含对应于共有序列（Arg / Lys;优选Arg）的氨基酸序列的多肽的磷酸化来测量 - X-（X / Arg）-XX-Ser / Thr）-Z其中X表示任何氨基酸，X / Arg表示任何氨基酸，优选精氨酸，Z表示氨基酸残基优选为疏水残基。 SGK可能被磷酸化激活。

7. 发明授权

US06617117B1 MAP kinases: polypeptides, polynucleotides and uses thereof 失效
标题翻译： MAP激酶：多肽，多核苷酸及其用途
公开(公告)号：US06617117B1
公开(公告)日：2003-09-09
申请号：US09809464
申请日：2001-03-15
申请人： Philip Cohen , Michel Goedert
发明人： Philip Cohen , Michel Goedert
IPC分类号： G01N3353
CPC分类号： C12N9/1205 , A61K38/00 , C07K16/40
摘要： The present invention relates to a method of identifying a compound which blocks the activation of a stress-activated protein kinase selected from the group consisting of SAPK4 and SAPK3 by SKK3. The method includes contacting the stress-activated protein kinase with the compound and determining whether the compound enhances or disrupts the interaction between the stress-activated protein kinase and SKK3. The invention further relates to a screening assay, a method of identifying agents able to influence the activity of a stress-activated protein kinase and a method of activating a stress-activated protein kinase.
摘要翻译：本发明涉及鉴定通过SKK3阻断选自SAPK4和SAPK3的应激活化蛋白激酶活化的化合物的方法。该方法包括使应激活化蛋白激酶与化合物接触并确定化合物是否增强或破坏应激活化蛋白激酶与SKK3之间的相互作用。本发明进一步涉及筛选试验，鉴定能够影响应激活化蛋白激酶活性的试剂的方法和激活应激活化蛋白激酶的方法。

8. 发明授权

US06498274B1 Amide derivatives for the treatment of diseases mediated by cytokines 失效
标题翻译：用于治疗由细胞因子介导的疾病的酰胺衍生物
公开(公告)号：US06498274B1
公开(公告)日：2002-12-24
申请号：US09508055
申请日：2000-03-07
申请人： Dearg S Brown , George R Brown , Philip Cohen
发明人： Dearg S Brown , George R Brown , Philip Cohen
IPC分类号： C07C23305
CPC分类号： C07D295/185 , A61K31/167 , A61K31/196 , A61K31/277 , A61K31/495 , A61K31/5375 , A61K31/5377 , A61K31/54 , C07C235/56 , C07C235/84 , C07C237/40 , C07C237/42 , C07C255/57 , C07C2601/08 , C07C2601/14 , C07D295/155
摘要： The invention concerns the use of amide derivatives of formula (I) wherein: R1 and R2 are substituents such as hydroxy, C1-6alkoxy, mercapto, C1-6alkylthio, amino, C1-6alkylamino and di-(C1-6alkyl)amino; m and p are independently 0-3R3 is C1-4alkyl; q is 0-4; and R4 is aryl or cycloalkyl; or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for use in the treatment of diseases or medical conditions mediated by cytokines
摘要翻译：本发明涉及式（I）的酰胺衍生物的用途，其中：R 1和R 2是取代基，例如羟基，C 1-6烷氧基，巯基，C 1-6烷硫基，氨基，C 1-6烷基氨基和二 - （C 1-6烷基）氨基; m和p独立地为0-3R3为C1-4烷基; q为0-4; R4是芳基或环烷基; 或其药学上可接受的盐在制备用于治疗由细胞因子介导的疾病或医学病症的药物中的用途

9. 发明申请

US20110275102A1 ACTIVATION OF MUTATED RAC-PK 审中-公开
标题翻译：突变型RAC-PK的活化
公开(公告)号：US20110275102A1
公开(公告)日：2011-11-10
申请号：US13021048
申请日：2011-02-04
申请人： Dario Alessi , Mirjana Andjelkovic , Philip Cohen , Peter David Cron , Darren Cross , Brian A. Hemmings
发明人： Dario Alessi , Mirjana Andjelkovic , Philip Cohen , Peter David Cron , Darren Cross , Brian A. Hemmings
IPC分类号： C12Q1/48 , C12N9/12 , C07K7/06
CPC分类号： C07K14/47 , A61K38/00 , C12N9/12 , C12N9/1205 , C12Q1/42 , C12Q1/48
摘要： The invention concerns RAC-PK and fragments thereof, as well as activators and inhibitors of RAC-PK for use as medicaments, particularly in the treatment of diseases concerned with abnormalities in processes modulated by insulin, such as cellular proliferation, insulin deficiency and/or excess blood sugar levels. Moreover, the invention provides RAC-PK for use in screening potential mimics or modulators thereof. A method for screening for agents capable of affecting the activity of GSK3 is also disclosed. The invention further provides a screening kit comprising the RAC-PK as an active principle, and a method for screening compounds which are candidate mimics or modulators of RAC-PK activity comprising detecting specific interactions between the candidate compounds and RAC-PK. There is also provided a process for activating RAC-PK comprising treatment thereof with a phosphatase inhibitor.
摘要翻译：本发明涉及RAC-PK及其片段，以及用作药物的RAC-PK的活化剂和抑制剂，特别是用于治疗与胰岛素调节的过程有关的疾病如细胞增殖，胰岛素缺乏和/或血糖过高。此外，本发明提供了用于筛选潜在模拟物或其调节剂的RAC-PK。还公开了能够影响GSK3活性的试剂的筛选方法。本发明进一步提供了包含作为活性成分的RAC-PK的筛选试剂盒，以及筛选作为RAC-PK活性的候选模拟物或调节剂的化合物的方法，包括检测候选化合物与RAC-PK之间的特异性相互作用。还提供了用于激活RAC-PK的方法，其包括用磷酸酶抑制剂处理它。

10. 发明申请

US20100063085A1 METHOD OF TREATING LEARNING IMPAIRMENT IN DOWN'S SYNDROME SUBJECTS 审中-公开
标题翻译：治疗下肢综合症患者学习障碍的方法
公开(公告)号：US20100063085A1
公开(公告)日：2010-03-11
申请号：US12208677
申请日：2008-09-11
申请人： Philip Cohen
发明人： Philip Cohen
IPC分类号： A61K31/437 , A61P25/00
CPC分类号： A61K31/437 , A61K9/0073
摘要： The present invention provides compounds for use in the preparation of pharmaceutical formulations and medicaments, which alleviate learning and/or mental impairment in people suffering from Down's syndrome.
摘要翻译：本发明提供了用于制备药物制剂和药物的化合物，其减轻患有唐氏综合征的人的学习和/或精神障碍。

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