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31. 发明专利

AU698762B2 A method of identifying CFTR-binding compounds useful for activating chloride conductance in animal cells 未知
公开(公告)号：AU698762B2
公开(公告)日：1998-11-05
申请号：AU4146096
申请日：1995-11-06
申请人： US HEALTH
发明人： POLLARD HARVEY B , JACOBSON KENNETH A
IPC分类号： G01N33/566 , A61K31/52 , A61K31/522 , A61K38/00 , A61K38/17 , A61P11/00 , A61P43/00 , C07D473/04 , C07D473/06 , C07D473/08 , C07D473/12 , C07H21/00 , C07K14/47 , C12N15/09
摘要： The present invention provides a method of identifying CFTR-binding compounds for treating cells having a reduced apical Cl- conductance, such as cystic fibrosis cells. This identification method involves the use of polypeptide I alpha , which constitutes a portion of the CFTR protein. The present invention also provides a method of treating CF cells by contacting cells having a reduced apical Cl- conductance with a therapeutically effective quantity of a compound selected by the present inventive identification method. Preferred compounds for such treatment have little or no affinity for adenosine cell receptors. The present invention provides novel compounds useful in practicing the present inventive method, as well as pharmaceutical compositions containing such compounds.

32. 发明专利

PL2539352T3 POCHODNE AMP DO LECZENIA CHORÓB SERCA 未知
公开(公告)号：PL2539352T3
公开(公告)日：2018-03-30
申请号：PL11713395
申请日：2011-02-22
申请人： UNIV CONNECTICUT , US HEALTH
发明人： LIANG BRUCE , JACOBSON KENNETH A , JOSHI BHALCHANDRA V , KUMAR THATIKONDA SANTOSH
IPC分类号： C07F9/6561 , A61K31/675 , A61P9/10

33. 发明专利

CA2789259A1 COMPOSITIONS AND METHODS TO TREAT CARDIAC DISEASES 未知
公开(公告)号：CA2789259A1
公开(公告)日：2011-08-25
申请号：CA2789259
申请日：2011-02-22
申请人： US HEALTH , UNIV CONNECTICUT
发明人： LIANG BRUCE , JACOBSON KENNETH A , JOSHI BHALCHANDRA V , KUMAR THATIKONDA SANTHOSH
IPC分类号： C07F9/6561 , A61K31/675 , A61P9/04
摘要： Phosphonate and phosphinate N-methanocarba derivatives of AMP including their prodrug analogs are described. MRS2339, a 2-chloro-AMP derivative containing a (N)- methanocarba (bicyclo[3.1.0]hexane) ring system in place of ribose, activates P2X receptors, ligand-gated ion channels. Phosphonate analogues of MRS2339 were synthesized using Michaelis-Arbuzov and Wittig reactions, based on the expectation of increased half-life in vivo due to the stability of the C-P bond. When administered to calsequestrin-overexpressing mice (a genetic model of heart failure) via a mini-osmotic pump (Alzet), some analogues significantly increased intact heart contractile function in vivo, as assessed by echocardiography-derived fractional shortening (FS) as compared to vehicle-infused mice. The range of carbocyclic nucleotide analogues for treatment of heart failure has been expanded.

34. 发明专利

CA2732320A1 A3 ADENOSINE RECEPTOR ANTAGONISTS AND PARTIAL AGONISTS 未知
公开(公告)号：CA2732320A1
公开(公告)日：2010-02-04
申请号：CA2732320
申请日：2009-07-31
申请人： US HEALTH
发明人： JACOBSON KENNETH A , MELMAN ARTEM , WANG BEN BIH-REN
IPC分类号： C07D473/34 , A61K31/52
摘要： Disclosed are A3 adenosine receptor antagonists and/or partial agonists of formula (I): wherein R1 to R5 are as described herein, as well as pharmaceutical compositions thereof and methods of use thereof. The antagonists or partial agonists find use in treating a number of diseases including cancer, glaucoma, inflammatory diseases, asthma, stroke, myocardial infarction, allergic reactions, rhinitis, poison ivy induced responses, urticaria, scleroderma, arthritis, brain arteriole diameter constriction, bronchoconstriction, and myocardial ischemia, as well as in preventing cardiac ischemia. Also disclosed are radiolabeled compounds of formula (I) and the use thereof in diagnostic imaging of tissues and organs.

35. 发明专利

CA2336967A1 A3 ADENOSINE RECEPTOR ANTAGONISTS 未知
公开(公告)号：CA2336967A1
公开(公告)日：2000-01-20
申请号：CA2336967
申请日：1999-07-02
申请人： US HEALTH
发明人： LI AN-HU , JACOBSON KENNETH A
IPC分类号： C07D211/90 , C07D213/80 , C07D213/83 , C07D471/04 , C07D491/04 , C07D495/04 , A61K31/451 , A61K31/455 , A61K31/4738
摘要： The present invention provides certain novel pyridine and dihydropyridine derivatives, pharmaceutical compositions comprising one or more of these derivatives, and a method of treating a mammal by selectively blocking an A3 adenosine receptor of the mammal by the administration of a pyridine or dihydropyridine derivative of the present invention. Thus, for example, the present invention provides the following pyridine derivatives of formula (I) or a pharmaceutically acceptable salt thereof; wherein R2 is selected from t he group consisting of C1-C6 alkyl, C3-C7 cycloalkyl, and C1-C6 alkoxy C1-C6 alkyl; R3 is selected from the group consisting of C1-C6 alkoxy, C1-C6 alkylsulfanyl, hydroxy, C1-C6 alkoxy C1-C6 alkylsulfanyl, hydroxy C1-C6 alkylsulfanyl, and halo C1-C6 alkylsulfanyl, or R3 together with R4 forms a 3- 7 membered heterocyclic ring containing O, N, or S; R4 is selected from the group consisting of C1-C6 alkyl, halo C1-C6 alkyl, hydroxy C1-C6 alkyl, C1-C 6 alkoxy, C1-C6 alkylsulfanyl, C1-C6 alkylamino, C1-C6 alkylcarbonyl sulfanyl C1- C6 alkyl, aryl C2-C6 alkenyl, aryl C2-C6 alkynyl, formyl, and acetal; R5 is selected from the group consisting of C1-C6 alkyl, aryl C1-C6 alkyl, hydroxy C1-C6 alkyl, and halo C1-C6 alkyl; and R6 is selected from the group consisting of aryl, C3-C7 cycloalkyl, and haloaryl; wherein said aryl is a phenyl or naphthyl. The compounds of the present invention can be used for inhibiting the binding of ligands to an adenosine receptor of a substrate. T he compounds of the present invention can be used for characterizing an adenosi ne receptor in a substrate.

36. 发明专利

CA2244774A1 DIHYDROPYRIDINE DERIVATIVES, THEIR PREPARATION AND THEIR USEAS ADENOSINE RECEPTOR ANTAGONISTS 未知
公开(公告)号：CA2244774A1
公开(公告)日：1997-07-31
申请号：CA2244774
申请日：1997-01-29
申请人： US HEALTH
发明人： KARTON YISHAI , JACOBSON KENNETH A , JIANG JI-LONG , VAN RHEE ALBERT M , KIM YONG-CHUL
IPC分类号： A61K31/4422 , A61K31/4545 , A61P7/02 , A61P9/10 , A61P25/22 , A61P43/00 , C07D211/90 , C07D311/22 , C07D311/30 , C07D311/32 , C07D317/70 , C07D401/04 , C07D401/12 , C07D405/04 , C07D409/04 , C07D487/04 , C07D493/04 , C07F7/08 , C07D221/04 , C07F7/10 , C07D409/14 , A61K31/435 , C07D215/54 , A61K31/695
摘要： The present invention provides certain novel compounds, compositions, and a method of treating a mammal by blocking its adenosine receptors comprising administering at least one compound of the present invention. Examples of the present inventive compounds include certain flavonoids of formulae (I) and (II), wherein R1 to R4 are as defined in the description, and M is -CH(OH)-CH(R2)- or -C(OH)= C(R2)- and R1, R2 are as defined in the description; or dihydropyridines of formula (III), wherein R2 to R6 are as defined in the description; or pyridines of formula (IV), wherein R2 to R6 are as defined in the description, or triazoloquinazolines of formula (V), wherein R1 and R2 are as defined in the description; and their derivatives, or pharmaceutically acceptable salts thereof.

37. 发明专利

CA2205540A1 A METHOD OF IDENTIFYING CFTR-BINDING COMPOUNDS USEFUL FOR ACTIVATING CHLORIDE CONDUCTANCE IN ANIMAL CELLS 未知
公开(公告)号：CA2205540A1
公开(公告)日：1996-05-30
申请号：CA2205540
申请日：1995-11-06
申请人： US HEALTH
发明人： JACOBSON KENNETH A , POLLARD HARVEY B
IPC分类号： G01N33/566 , A61K31/52 , A61K31/522 , A61K38/00 , A61K38/17 , A61P11/00 , A61P43/00 , C07D473/04 , C07D473/06 , C07D473/08 , C07D473/12 , C07H21/00 , C07K14/47 , C12N15/09
摘要： The present invention provides a method of identifying CFTR-binding compounds for treating cells having a reduced apical Cl- conductance, such as cystic fibrosis cells. This identification method involves the use of polypeptide I.alpha., which constitutes a portion of the CFTR protein. The present invention also provides a method of treating CF cells by contacting cells having a reduced apical C1- conductance with a therapeutically effective quantity of a compound selected by the present inventive identification method. Preferred compounds for such treatment have little or no affinity for adenosine cell receptors. The present invention provides novel compounds useful in practicing the present inventive method, as well as pharmaceutical compositions containing such compounds.

38. 发明专利

DK2539352T3 AMP-derivater til behandling af hjertesygdomme 未知
公开(公告)号：DK2539352T3
公开(公告)日：2018-01-08
申请号：DK11713395
申请日：2011-02-22
申请人： UNIV CONNECTICUT , US HEALTH
发明人： LIANG BRUCE , JACOBSON KENNETH A , JOSHI BHALCHANDRA V , KUMAR THATIKONDA SANTOSH
IPC分类号： C07F9/6561 , A61K31/675 , A61P9/10

39. 发明专利

CA2732320C A3 ADENOSINE RECEPTOR ANTAGONISTS AND PARTIAL AGONISTS 未知
公开(公告)号：CA2732320C
公开(公告)日：2017-08-29
申请号：CA2732320
申请日：2009-07-31
申请人： US HEALTH
发明人： JACOBSON KENNETH A , MELMAN ARTEM , WANG BEN BIH-REN
IPC分类号： C07D473/34 , A61K31/52
摘要： Disclosed are A3 adenosine receptor antagonists and/or partial agonists of formula (I): wherein R1 to R5 are as described herein, as well as pharmaceutical compositions thereof and methods of use thereof. The antagonists or partial agonists find use in treating a number of diseases including cancer, glaucoma, inflammatory diseases, asthma, stroke, myocardial infarction, allergic reactions, rhinitis, poison ivy induced responses, urticaria, scleroderma, arthritis, brain arteriole diameter constriction, bronchoconstriction, and myocardial ischemia, as well as in preventing cardiac ischemia. Also disclosed are radiolabeled compounds of formula (I) and the use thereof in diagnostic imaging of tissues and organs.

40. 发明专利

CA2720037C PURINE DERIVATIVES AS A3 ADENOSINE RECEPTOR-SELECTIVE AGONISTS 未知
公开(公告)号：CA2720037C
公开(公告)日：2016-08-23
申请号：CA2720037
申请日：2009-03-24
申请人： US HEALTH
发明人： JACOBSON KENNETH A , MELMAN ARTEM
IPC分类号： C07D473/34 , A61K31/52 , A61P3/00 , A61P25/00 , A61P29/00 , A61P35/00
摘要： Disclosed are (N)-methanocarba adenine nucleosides, e.g., of formula (I) as highly potent A3 adenosine receptor agonists, pharmaceutical compositions comprising such nucleosides, and a method of use of these nucleosides, wherein R1-R6 are as defined in the specification. These nucleosides exhibit similar selectivities as agonists of the A3 versus the A1 receptor for both human and mouse adenosine receptors, and are contemplated for use in the treatment a number of diseases, for example, inflam-mation, cardiac ischemia, stroke, asthma, diabetes, and cardiac arrhythmias.

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