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1. 发明申请

WO2004084810A3 NOVEL IMIDAZOLINE RECEPTOR HOMOLOGS 审中-公开
标题翻译：新的咪唑啉受体同种异体
公开(公告)号：WO2004084810A3
公开(公告)日：2006-10-19
申请号：PCT/US2004008207
申请日：2004-03-16
申请人： SQUIBB BRISTOL MYERS CO , FEDER JOHN N , KINNEY GENE G , MINTIER GABRIEL , RAMANATHAN CHANDRA S , BOL DAVID K , RYSECK ROLF-PETER
发明人： FEDER JOHN N , KINNEY GENE G , MINTIER GABRIEL , RAMANATHAN CHANDRA S , BOL DAVID K , RYSECK ROLF-PETER
IPC分类号： C12P21/06 , A01N37/18 , A61K20060101 , A61K38/00 , C07K1/00 , C07K14/705 , C07K16/00 , C12N5/00 , C12N15/00 , C12N15/12 , G01N33/53
CPC分类号： C07K14/705 , A61K38/00
摘要： Novel imidazoline receptor homologs, designated imidazoline receptor related protein 1 (IMRRP1), imidazoline receptor related protein 1b (IMRRP1b), and derivatives thereof are described. Pharmaceutical compositions comprising at least one IMRRP1, IMRRP1b, or a functional portion thereof, are provided as are methods for producing IMRRP1, IMRRP1b or a functional portion thereof. In addition, nucleic acid sequences encoding polypeptides, oligonucleotides, fragments, portions or antisense molecules thereof, and expression vectors and host cells comprising polynucleotides that encode IMRRP1 or IMRRP1b are provided. The novel association of IMRRP1 and/or IMRRP1b to modulating the NFkB pathway and the p21 cell cycle checkpoint, and uses thereof are also provided.
摘要翻译：描述了新的咪唑啉受体同系物，命名为咪唑啉受体相关蛋白1（IMRRP1），咪唑啉受体相关蛋白1b（IMRRP1b）及其衍生物。提供包含至少一种IMRRP1，IMRRP1b或其功能部分的药物组合物，如制备IMRRP1，IMRRP1b或其功能部分的方法。此外，提供了编码多肽，寡核苷酸，片段，部分或反义分子的核酸序列，以及包含编码IMRRP1或IMRRP1b的多核苷酸的表达载体和宿主细胞。还提供了IMRRP1和/或IMRRP1b对调节NFkB途径和p21细胞周期检查点的新型关联，以及其用途。

2. 发明申请

WO0216585A3 IMIDAZOLINE RECEPTOR HOMOLOGS 审中-公开
标题翻译：咪唑啉受体HOMOLOGS
公开(公告)号：WO0216585A3
公开(公告)日：2003-03-27
申请号：PCT/US0125851
申请日：2001-08-17
申请人： SQUIBB BRISTOL MYERS CO , FEDER JOHN N , MINTIER GABE , KINNEY GENE G , RAMANATHAN CHANDRA S
发明人： FEDER JOHN N , MINTIER GABE , KINNEY GENE G , RAMANATHAN CHANDRA S
IPC分类号： G01N33/50 , A61K38/00 , A61K39/395 , A61P9/00 , A61P25/04 , A61P25/28 , A61P25/36 , A61P43/00 , C07K14/705 , C07K16/28 , C12N1/15 , C12N1/19 , C12N1/21 , C12N5/10 , C12N15/09 , C12N15/12 , C12P21/02 , G01N33/15 , G01N33/53 , G01N33/566 , C12Q1/68 , G01N33/68
CPC分类号： C07K14/705 , A61K38/00
摘要： Novel imidazoline receptor homologs, designated imidazoline receptor related protein 1 (IMRRP1), imidazoline receptor related protein 1b (IMRRP1) and derivatives thereof are described. Pharmaceutical compositions comprising at least one IMRRP1, IMRRP1b or a functional portion thereof are provided as are methods for producing IMRRP1, IMRRP1b or a functional portion thereof. In addition, nucleic acid sequences encoding polypeptides, oligonucleotides, fragments, portions or antisense molecules thereof, and expression vectors and host cells comprising polynucleotides that encode IMRRP1 or IMRRP1b are provided. The use of the nucleic acid sequences, polypeptide, peptide and antibodies for diagnosis and treatment of disorders or diseases associated with aberrant regulation of blood pressure, induction of feeding, stimulation of firing of locus coeruleus neurons, and stimulation of insulin release, as well as the aberrant induction of the expression of glial fibrillary acidic protein independent of the action of alpha-2 adrenoceptors, dysphoric premenstrual syndrome, neurodegenerative disorders such as Alzheimer's disease, opiate addiction, monoamine turnover and therefore nociception, aging, mood and stroke, salivary disorders and developmental disroders is also described.
摘要翻译：描述了新的咪唑啉受体同系物，命名为咪唑啉受体相关蛋白1（IMRRP1），咪唑啉受体相关蛋白1b（IMRRP1）及其衍生物。提供包含至少一种IMRRP1，IMRRP1b或其功能部分的药物组合物，如制备IMRRP1，IMRRP1b或其功能部分的方法。此外，提供了编码多肽，寡核苷酸，片段，部分或反义分子的核酸序列，以及包含编码IMRRP1或IMRRP1b的多核苷酸的表达载体和宿主细胞。核酸序列，多肽，肽和抗体用于诊断和治疗与血压异常调节相关的病症，诱导进食，刺激烧伤神经元和刺激胰岛素释放的用途，以及神经胶质纤维酸性蛋白的表达异常诱导，与α-2肾上腺素受体的作用无关，烦躁经前综合征，神经退行性疾病如阿尔茨海默病，阿片成瘾，单胺周转和因此伤害感，衰老，情绪和中风，唾液疾病和还描述了发育障碍。

3. 发明申请

WO02066426A3 FLUORO OXINDOLE DERIVATIVES AS MODULATORS OF KCNQ POTASSIUM CHANNELS 审中-公开
标题翻译：氟尿嘧啶衍生物作为KCNQ钾通道调节剂
公开(公告)号：WO02066426A3
公开(公告)日：2002-11-21
申请号：PCT/US0204304
申请日：2002-02-14
申请人： SQUIBB BRISTOL MYERS CO
发明人： HEWAWASAM PIYASENA , DEXTRAZE PIERRE , GRIBKOFF VALENTIN K , KINNEY GENE G , DWORETZKY STEVEN I
IPC分类号： A61K31/404 , A61P25/06 , A61P43/00 , C07D209/34
CPC分类号： C07D209/34
摘要： There is provided novel 3-fluoro-3-phenyl oxindole derivatives of Formula I wherein R , R , R and R each are independently hydrogen, C1-4 alkyl, halogen, fluoromethyl, trifluoromethyl, phenyl, 4-methylphenyl or 4-trifluoromethylphenyl; R is C1-6 alkyl optionally substituted with one to three same or different groups selected from fluoro and chloro, provided R is not C1-6 alkyl when Y is O; Y is O or S; and R and R each are independently hydrogen, chloro, bromo or trifluoromethy; which are openers of the KCNQ potassium channels and are useful in the treatment of disorders which are responsive to the opening of the KCNQ potassium channels.
摘要翻译：提供了式I的新的3-氟-3-苯基羟吲哚衍生物，其中R 1，R 2，R 3和R 4各自独立地为氢，C 1-4烷基，卤素，氟甲基，三氟甲基，苯基，4-甲基苯基或4-三氟甲基苯基; R 5为任选被1-3个选自氟和氯的相同或不同基团取代的C 1-6烷基，条件是当Y为O时R 5不是C 1-6烷基; Y是O或S; 并且R 6和R 7各自独立地为氢，氯，溴或三氟甲基; 它们是KCNQ钾通道的开放剂，并且可用于治疗对KCNQ钾通道开放有反应的病症。

4. 发明申请

WO02072088A2 MODULATORS OF KCNQ POTASSIUM CHANNELS AND USE THEREOF IN TREATING MIGRAINE AND MECHANISTICALLY RELATED DISEASES 审中-公开
标题翻译： KCNQ钾通道的调节剂及其在治疗机体和机械相关疾病中的应用
公开(公告)号：WO02072088A2
公开(公告)日：2002-09-19
申请号：PCT/US0204374
申请日：2002-02-14
申请人： SQUIBB BRISTOL MYERS CO
发明人： DWORETZKY STEVEN , GRIBKOFF VALENTIN K , KINNEY GENE G , HEWAWASAM PIYASENA
IPC分类号： G01N33/50 , A61K31/404 , A61K31/506 , A61K45/00 , A61P25/06 , G01N33/15 , C07D209/34 , C07D239/42
CPC分类号： A61K31/404 , A61K31/506
摘要： Compounds which function as modulators, particularly, openers, of human KCNQ potassium channel proteins or polypeptides, particularly, central nervous system(CNS)-located KCNQ potassium channels, and heteromultimers thereof, and their use in the treatment of migraine are provided by the present invention. One novel type of potassium channel polypeptide openers provided by the present invention is the fluorooxindole compounds, described for the first time as therapeutics for the treatment of migraine by preventing the asynchronous firing of neurons. Other KCNQ potassium channel opener compounds that are also useful in the treatments of the invention include 2,4-disubstituted pyrimidine-5-carboxamide derivatives. One or more of the compounds according to the present invention may be utilized alone, in combination, or in conjunction with other treatment modalities for reducing, ameliorating and/or alleviating migraine or diseases similar to, or mechanistically related to, migraine, e.g., cluster headache.
摘要翻译：作为人KCNQ钾通道蛋白或多肽，特别是中枢神经系统（CNS）分配的KCNQ钾通道及其异源多肽的调节剂，特别是开放剂的化合物及其在治疗偏头痛中的用途由本发明提供发明。本发明提供的一种新型的钾通道多肽开放剂是氟氧吲哚化合物，首次作为通过防止神经元的异步烧制来治疗偏头痛的治疗剂。也可用于本发明处理的其它KCNQ钾通道开放剂化合物包括2,4-二取代的嘧啶-5-甲酰胺衍生物。根据本发明的一种或多种化合物可以单独使用，或与其它治疗方式联用，用于减少，改善和/或减轻与偏头痛相似或机械相关的偏头痛或类似疾病，例如，集群头痛。

5. 发明申请

WO2011133919A4 USE OF TAU TO MONITOR IMMUNOTHERAPY 审中-公开
标题翻译：使用TA监测免疫
公开(公告)号：WO2011133919A4
公开(公告)日：2012-01-12
申请号：PCT/US2011033649
申请日：2011-04-22
申请人： JANSSEN ALZHEIMER IMMUNOTHERAP , WYETH LLC , BLACK RONALD , JACOBSEN JACK STEVEN , TCHISTIAKOVA LIOUDMILA , WIDOM ANGELA , GILL DAVINDER , EKMAN LARS , LIEBERBURG IVAN , GRUNDMAN MICHAEL , CALLAWAY JAMES , GREGG KEITH M , ZAGO WAGNER , BUTTINI MANUEL J , KINNEY GENE G
发明人： BLACK RONALD , JACOBSEN JACK STEVEN , TCHISTIAKOVA LIOUDMILA , WIDOM ANGELA , GILL DAVINDER , EKMAN LARS , LIEBERBURG IVAN , GRUNDMAN MICHAEL , CALLAWAY JAMES , GREGG KEITH M , ZAGO WAGNER , BUTTINI MANUEL J , KINNEY GENE G
IPC分类号： A61K39/00 , C07K16/00
CPC分类号： A61K39/3955 , A61K2039/505 , A61K2039/545 , A61K2039/55 , C07K16/18 , C07K2317/24 , C07K2317/34
摘要： The invention provides methods of immunotherapy of Alzheimer's and similar diseases in which the regime administered is monitored by measuring levels of tau.
摘要翻译：本发明提供了阿尔茨海默病和类似疾病的免疫治疗方法，其中通过测量tau的水平来监测施用的状态。

6. 发明申请

WO2005007096A2 TREATMENT OF MOVEMENT DISORDERS WITH A METABOTROPIC GLUTAMATE 4 RECEPTOR POSITIVE ALLOSTERIC MODULATOR 审中-公开
标题翻译：代谢型谷氨酸受体4正向调节剂治疗运动障碍
公开(公告)号：WO2005007096A2
公开(公告)日：2005-01-27
申请号：PCT/US2004021776
申请日：2004-07-07
申请人： MERCK & CO INC , CONN P JEFFREY , DILELLA ANTHONY G , KINNEY GENE G , MARINO MICHAEL J , SEABROOK GUY R , WILLIAMS DAVID L
发明人： CONN P JEFFREY , DILELLA ANTHONY G , KINNEY GENE G , MARINO MICHAEL J , SEABROOK GUY R , WILLIAMS DAVID L
IPC分类号： A61K20060101 , A61K31/35 , A61K
CPC分类号： A61K31/35 , A61K31/198 , A61K31/445 , A61K31/48 , A61K31/5415 , A61K31/551 , A61K31/5513 , A61K31/553
摘要： An mGluR4 receptor positive allosteric modulator is useful, alone or in combination with a neuroleptic agent, for treating or preventing movement disorders such as Parkinson's disease, dyskinesia, tardive dyskinesia, drug-induced parkinsonism, postencephalitic parkinsonism, progressive supranuclear palsy, multiple system atrophy, corticobasal degeneration, parkinsonian-ALS dementia complex, basal ganglia calcification, akinesia, akinetic-rigid syndrome, bradykinesia, dystonia, medication-induced parkinsonian, Gilles de la Tourette syndrome, Huntington's disease, tremor, chorea, myoclonus, tick disorder, and dystonia.
摘要翻译： mGluR4受体正变构调节剂单独或与精神安定剂组合用于治疗或预防运动障碍，例如帕金森病，运动障碍，迟发性运动障碍，药物诱导的帕金森病，脑炎后帕金森病，进行性核上性麻痹，多系统萎缩，皮质基底节变性，帕金森病-ALS痴呆综合征，基底神经节钙化，运动不能，运动迟钝综合征，运动迟缓，肌张力障碍，药物诱发帕金森病，吉勒斯德拉图雷特综合征，亨廷顿病，震颤，舞蹈病，肌阵挛，蜱障碍和肌张力障碍。

7. 发明公开

EP1608320A4 NOVEL IMIDAZOLINE RECEPTOR HOMOLOGS 审中-公开
标题翻译：新型咪唑啉受体同系
公开(公告)号：EP1608320A4
公开(公告)日：2007-05-30
申请号：EP04757780
申请日：2004-03-16
申请人： SQUIBB BRISTOL MYERS CO
发明人： FEDER JOHN N , KINNEY GENE G , MINTIER GABRIEL , RAMANATHAN CHANDRA S , BOL DAVID K , RYSECK ROLF-PETER
IPC分类号： C12P21/06 , A61K20060101 , A61K38/00 , C07K14/705 , C12N15/11 , C12N15/12
CPC分类号： C07K14/705 , A61K38/00

8. 发明专利

HU0303841A2 2,4-DISUBSTITUTED PYRIMIDINE-5-CARBOXAMIDE DERIVATIVES AS KCNQ POTASSIUM CHANNEL MODULATORS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND PREPARATION THEREOF 未知
公开(公告)号：HU0303841A2
公开(公告)日：2004-03-01
申请号：HU0303841
申请日：2002-02-14
申请人： SQUIBB BRISTOL MYERS CO
发明人： DEXTRAZE PIERRE , DODD DHARMPAL S , DWORETZKY STEVEN I , GRIBKOFF VALENTIN K , HEWAWASAM PIYASENA , KINNEY GENE G , WEAVER CHARLES D
IPC分类号： A61K31/505 , A61K31/506 , A61K31/5377 , A61P25/06 , A61P43/00 , C07D239/42 , C07D405/12 , C07D409/04 , C07D409/12
摘要： There is provided a method of treatment for disorders responsive to the modulation of KCNQ potassium channels by administering to a mammal in need thereof a therapeutically effective amount of a 2,4-disubstituted pyrimidine-5-carboxamide derivative of the Formula I wherein R1, R2, R3, R4 and R5 are as defined below. The present invention also provides pharmaceutical compositions comprising openers or activators of the KCNQ potassium channels and especially to the method of treatment of disorders sensitive to KCNQ potassium channel opening activity such as migraine.

10. 发明专利

CZ20032233A3 Derivative of 2,4-disubstituted pyrimidine-5-carboxamide functioning as KCNQ potassium channel modulator 未知
公开(公告)号：CZ20032233A3
公开(公告)日：2004-12-15
申请号：CZ20032233
申请日：2002-02-14
申请人： SQUIBB BRISTOL MYERS CO
发明人： DEXTRAZE PIERRE , GRIBKOFF VALENTIN K , KINNEY GENE G , DWORETZKY STEVEN I , HEWAWASAM PIYASENA , DODD DHARMPAL S , WEAVER CHARLES D
IPC分类号： A61K31/505 , A61K31/506 , A61K31/5377 , A61P25/06 , A61P43/00 , C07D239/42 , C07D405/12 , C07D409/04 , C07D409/12
摘要： There is provided a method of treatment for disorders responsive to the modulation of KCNQ potassium channels by administering to a mammal in need thereof a therapeutically effective amount of a 2,4-disubstituted pyrimidine-5-carboxamide derivative of the Formula I wherein R1, R2, R3, R4 and R5 are as defined below. The present invention also provides pharmaceutical compositions comprising openers or activators of the KCNQ potassium channels and especially to the method of treatment of disorders sensitive to KCNQ potassium channel opening activity such as migraine.

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