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81. 发明申请

US20040213740A1 Light sensitive compounds for instant determination of organ function 失效
标题翻译：光敏化合物，用于即时测定器官功能
公开(公告)号：US20040213740A1
公开(公告)日：2004-10-28
申请号：US10751232
申请日：2004-01-02
申请人： Mallinckrodt Inc.
发明人： Samuel Achilefu , Raghavan Rajagopalan , Richard B. Dorshow , Joseph E. Bugaj , Hermo N. Jimenez , Muthunadar P. Periasamy
IPC分类号： A61K049/00 , A61K031/7056 , A61K031/428 , A61K031/423
CPC分类号： A61K49/0032 , C09B23/02
摘要： Highly hydrophilic indole and benzoindole derivatives that absorb and fluoresce in the visible region of light are disclosed. These compounds are useful for physiological and organ function monitoring. Particularly, the molecules of the invention are useful for optical diagnosis of renal and cardiac diseases and for estimation of blood volume in vivo.
摘要翻译：公开了在可见光区域吸收和发出荧光的高度亲水的吲哚和苯并吲哚衍生物。这些化合物可用于生理和器官功能监测。特别地，本发明的分子可用于肾脏和心脏疾病的光学诊断以及体内血液体积估计。

82. 发明申请

US20040204463A1 N-aryl-2-oxazolidinone-5-carboxamides and their derivatives 审中-公开
标题翻译： N-芳基-2-恶唑烷酮-5-甲酰胺及其衍生物
公开(公告)号：US20040204463A1
公开(公告)日：2004-10-14
申请号：US10795192
申请日：2004-03-05
发明人： Christina Renee Harris
IPC分类号： C07D413/02 , C07D45/02 , A61K031/55 , A61K031/423
CPC分类号： C07D263/20 , C07D413/10 , C07D413/12
摘要： The present invention provides antibacterial agents having the formula I described herein.
摘要翻译：本发明提供具有本文所述式I的抗菌剂。

83. 发明申请

US20040132791A1 Broadspectrum 2-(substituted-amino)-benzoxazole sulfonamide hiv protease inhibitors 失效
标题翻译： Bropectpectrum 2-（取代 - 氨基） - 苯并恶唑磺酰胺hiv蛋白酶抑制剂
公开(公告)号：US20040132791A1
公开(公告)日：2004-07-08
申请号：US10474162
申请日：2003-10-07
发明人： Dominique Louis Nestor Ghislain Surleraux , Sandrine Marie Helene Vendeville , Wim Gaston Berchem Verschueren , Marie-Pierre T.M.M.G. De Bethune , Herman Augustinus De Kock , Abdellah Tahri , Montserrat Erra Sola
IPC分类号： C07D263/58 , A61K031/423
CPC分类号： C07D413/04 , C07D263/58 , C07D417/12 , C07D417/14 , C07D493/04
摘要： The present invention concerns the compounds having the formula 1 N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7cycloalkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9null; t is 0, 1 or 2; R2 is H br C1-6alkyl; L is nullC(nullO)null, nullOnullC(nullO)null, nullNR8nullC(nullO)null, nullC1-6alkanediyl-C(nullO)null, nullNR8nullC1-6alkanediyl-C(nullO)null, nullS(nullO)2null, nullOnullS(nullO)2null, nullNR8nullS(nullO)2; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC(nullO), carboxyl, aminoC(nullO), mono- or di(C1-4alkyl)aminoC(nullO), C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; A is C1-6alkanediyl, nullC(nullO)null, nullC(nullS)null, nullS(nullO)2null, C1-6alkanediyl-C(nullO)null, C1-6alkanediyl-C(nullS)nullor C1-6alkanediyl-S(nullO)2null; R5 is H, OH, C1-6alkyl, Het1C1-6alkyl, Het2C1-6alkyl, optionally substituted aminoC1-6alkyl; R6 is C1-6alkylO, Het1, Het1O, Het2, Het2O, aryl, arylO, C1-6alkyloxycarbonylamino or amino; and in case -A- is other than C1-6alkanediyl then R6 may also be C1-6alkyl, Het1C1-4alkyl, Het1OC1-4alkyl, Het2C1-4alkyl, Het2OC1-4alkyl, arylC1-4alkyl, arylOC1-4alkyl or aminoC1-4alkyl; whereby each of the amino groups in the definition of R6 may optionally be substituted; -A-R6 is hydroxyC1-6alkyl; R5 and -A-R6 taken together with the nitrogen atom to which they are attached may also form Het1 or Het2. It further relates to their use as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with another anti-retroviral agent, and to their use in assays as reference compounds or as reagents.
摘要翻译：本发明涉及具有式N-氧化物，盐，立体异构形式，外消旋混合物，前药，酯和代谢物的化合物，其中R 1和R 8各自为H，任选取代的C 1-6烷基，C 2-6烯基，C 3-7环烷基，芳基，Het 1，Het 2; R1也可以是式（R11aR11b）NC（R10aR10b）CR9-的基团; t为0,1或2; R2是H-C 1-6烷基; L是-C（= O） - ， - OC（= O） - ， - NR 8 -C（= O） - ， - C 1-6烷二基-C（= O） - ， - NR 8 -C 1-6烷二基-C O） - ， - S（= O）2 - ， - OS（= O）2 - ， - NR 8 -S（= O） R 3是C 1-6烷基，芳基，C 3-7环烷基，C 3-7环烷基C 1-4烷基或芳基C 1-4烷基; R 4是H，C 1-4烷基OC（= O），羧基，氨基C（= O），单或二（C 1-4烷基）氨基C（= O），C 3-7环烷基，C 2-6烯基，C 2-6炔基或任选取代的C 1 -6-烷基; A是C 1-6烷二基，-C（= O） - ， - C（= S） - ， - S（= O）2 - ，C 1-6烷二基-C（= O） - ，C 1-6烷二基-C ） - 或C 1-6烷二基-S（= O）2 - ; R 5是H，OH，C 1-6烷基，Het 1 C 1-6烷基，Het 2 C 1-6烷基，任选取代的氨基C 1-6烷基; R 6是C 1-6烷基O，Het 1，Het 1 O，Het 2，Het 2 O，芳基，芳基O，C 1-6烷氧基羰基氨基或氨基; 并且在-A-不是C 1-6烷二基的情况下，则R6也可以是C <高

84. 发明申请

US20040102458A1 Small molecule compositions for binding to hsp90 有权
标题翻译：用于结合hsp90的小分子组合物
公开(公告)号：US20040102458A1
公开(公告)日：2004-05-27
申请号：US10415868
申请日：2003-05-01
发明人： Gabriela Chiosis , Neal Rosen
IPC分类号： C07D277/62 , C07D263/52 , C07D473/02 , A61K031/519 , A61K031/52 , A61K031/428 , A61K031/423 , A61K031/4184
CPC分类号： C07D473/00 , A61K31/52 , C07D209/36 , C07D473/34 , C07D473/40
摘要： Structural differences in binding pockets of members of the HSP90 family can be exploited to achieve differential degradation of kinases and other signaling proteins through the use of designed small molecules which interact with the N-terminal binding pocket with an affinity which is greater than ADP and different from the ansamycin antibiotics for at least one species of the HSP90 family. Moreover, these small molecules can be designed to be soluble in aqueous media, thus providing a further advantage over the use of ansamycin antibiotics. Pharmaceutical compositions can be formulated containing a pharmaceutically acceptable carrier and a molecule that includes a binding moiety which binds to the N-terminal pocket of at least one member of the HSP90 family of proteins. Such binding moieties were found to have antiproliferative activity against tumor cells which are dependent on proteins requiring chaperones of the HSP90 family for their function. Different chemical species have different activity, however, allowing the selection of, for example Her2 degradation without degradation of Raf kinase. Thus, the binding moieties possess an inherent targeting capacity. In addition, the small molecules can be linked to targeting moieties to provide targeting of the activity to specific classes of cells. Thus, the invention further provides a method for treatment of diseases, including cancers, by administration of these compositions. Dimeric forms of the binding moieties may also be employed.
摘要翻译：可以利用HSP90家族成员的结合口袋的结构差异，通过使用与N末端结合口袋相互作用的设计的小分子来实现激酶和其他信号传导蛋白质的差异降解，其亲和力大于ADP和不同对于至少一种HSP90家族的安莎霉素抗生素。此外，这些小分子可以被设计成可溶于含水介质，因此比使用安莎霉素抗生素提供了进一步的优点。药物组合物可以配制成含有药学上可接受的载体和分子，该分子包括与蛋白质的HSP90家族的至少一个成员的N-末端口袋结合的结合部分。发现这样的结合部分具有抗肿瘤细胞的抗增殖活性，其依赖于需要HSP90家族伴侣的功能的蛋白质。不同的化学物质具有不同的活性，然而，允许选择例如Her2降解而不降解Raf激酶。因此，结合部分具有固有的靶向能力。此外，小分子可以连接到靶向部分，以提供对特定细胞类别的活性的靶向。因此，本发明还提供了通过施用这些组合物来治疗疾病，包括癌症的方法。还可以使用结合部分的二聚体形式。

85. 发明申请

US20040087626A1 Substituted benz-azoles and methods of their use as inhibitors of Raf kinase 失效
标题翻译：取代的苯并唑及其用作Raf激酶抑制剂的方法
公开(公告)号：US20040087626A1
公开(公告)日：2004-05-06
申请号：US10405945
申请日：2003-03-31
发明人： Paul A. Renhowe , Savithri Ramurthy , Payman Amiri , Barry Haskell Levine , Daniel J. Poon , Skaradha Subramanian , Leonard Sung , Wendy Fantl
IPC分类号： A61K031/4439 , A61K031/428 , A61K031/423 , C07D277/82 , C07D263/60 , C07D417/02 , C07D413/02
CPC分类号： C07D401/14 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/12 , C07D417/14 , C07D453/02
摘要： New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
摘要翻译：提供了新的取代的苯并唑化合物，抑制人或动物受试者中Raf激酶活性的组合物和方法。新化合物组合物可以单独使用或与至少一种另外的药物组合使用，用于治疗Raf激酶介导的病症，例如癌症。

86. 发明申请

US20040082564A1 Methods for treating metabolic diseases using malonyl-coa decarboxylase inhibitors 失效
标题翻译：用丙二酰辅酶脱羧酶抑制剂治疗代谢疾病的方法
公开(公告)号：US20040082564A1
公开(公告)日：2004-04-29
申请号：US10468378
申请日：2003-08-19
发明人： Thomas Arrhenius , Jie Fei Cheng , Mark E. Wilson , Rossy Serafimov , Masahiro Nishimoto , David Mark Wallace , Sovouthy Tith , Steve Joel Brown , Charles Stanford Harmon
IPC分类号： A61K031/541 , A61K031/5377 , A61K031/496 , A61K031/454 , A61K031/428 , A61K031/427 , A61K031/423 , A61K031/422
CPC分类号： A61K31/423 , A61K31/425 , A61K31/426 , A61K31/428 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541
摘要： The present invention relates to methods of treatment of certain metabolic diseases, and to the use of compounds and their prodrugs, and/or pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds useful in treating such diseases. In particular, the invention relates to the use of compounds and compositions for treatment of cardiovascular diseases, diabetes, cancers, acidosis, and obesity through the inhibition of malonyl-CoA decarboxylase (MCD). These compounds have the following formulae: (I) and (II) Wherein Y, C, R1, R2, R6, and R7 are defined herein. 1
摘要翻译：本发明涉及治疗某些代谢疾病的方法，以及使用化合物及其前药，和/或药学上可接受的盐，含有可用于治疗这些疾病的化合物的药物组合物。特别地，本发明涉及通过抑制丙二酰辅酶A脱羧酶（MCD）来治疗心血管疾病，糖尿病，癌症，酸中毒和肥胖的化合物和组合物的用途。这些化合物具有下式：（I）和（II）其中Y，C，R 1，R 2，R 6和R 7在本文中定义。

87. 发明申请

US20040063755A1 Aryl aniline beta2 adrenergic receptor agonists 有权
标题翻译：芳基苯胺β2肾上腺素受体激动剂
公开(公告)号：US20040063755A1
公开(公告)日：2004-04-01
申请号：US10643196
申请日：2003-08-18
发明人： Edmund J. Moran , John R. Jacobsen , Michael R. Leadbetter , Matthew B. Nodwell , Sean G. Trapp , James Aggen , Timothy J. Church
IPC分类号： A61K031/4709 , A61K031/428 , A61K031/423 , A61K031/405 , A61K031/4184 , A61K031/277
CPC分类号： C07D213/75 , C07C215/60 , C07C217/84 , C07C229/38 , C07C233/43 , C07C317/36 , C07D213/76 , C07D215/227 , C07D215/26 , C07D231/22 , C07D239/38 , C07D239/42 , C07D239/47 , C07D277/46 , C07D277/52 , C07D295/26 , C07D311/80 , C07D319/18 , C07D321/10 , C07D401/12 , C07D409/12 , C07D413/12
摘要： The invention provides novel null2 adrenergic receptor agonist compounds of formula (I): 1 wherein R1-R13 and w have any of the values described in the specification. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with null2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.
摘要翻译：本发明提供式（I）的新型β2肾上腺素能受体激动剂化合物：其中R 1 -R 13和w具有说明书中描述的任何值。本发明还提供包含这些化合物的药物组合物，使用这些化合物治疗与β2肾上腺素能受体活性有关的疾病的方法，以及可用于制备这些化合物的方法和中间体。

88. 发明申请

US20040058905A1 FKBP inhibitors 审中-公开
标题翻译： FKBP抑制剂
公开(公告)号：US20040058905A1
公开(公告)日：2004-03-25
申请号：US10404524
申请日：2003-04-01
申请人： Pfizer Inc.
发明人： Martin J. Wythes , Michael J. Palmer , Mark I. Kemp , Malcolm C. MacKenny , Robert J. Maguire , James F. Blake JR.
IPC分类号： A61K031/454 , A61K031/428 , A61K031/423 , A61K031/4178
CPC分类号： C07D401/04 , A61K31/423 , A61K31/428 , C07D211/60 , C07D413/04 , C07D413/14 , C07D471/14
摘要： Compounds of formula (I), their salts and solvates, wherein the substituents are as described herein, are FKBP inhibitors. 1
摘要翻译：式（I）化合物，其盐和溶剂化物，其中取代基如本文所述，是FKBP抑制剂。

89. 发明申请

US20040039016A1 HIV protease inhibitors 失效
标题翻译： HIV蛋白酶抑制剂
公开(公告)号：US20040039016A1
公开(公告)日：2004-02-26
申请号：US10382435
申请日：2003-03-06
发明人： Arun K. Ghosh , Geoffrey M. Bilcer , Thippeswamy Devasamudram
IPC分类号： A61K031/47 , A61K031/44 , A61K031/428 , A61K031/423 , A61K031/4015 , A61K031/325
CPC分类号： C07D213/70 , A61K31/34 , A61K31/35 , A61K45/06 , C07C311/29 , C07C311/41 , C07D209/96 , C07D307/20 , C07D307/935 , C07D307/94 , C07D317/44 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D419/12 , C07D491/10 , C07D493/04 , A61K2300/00
摘要： Compounds useful for inhibiting HIV protease are disclosed. Methods of making the compounds, and their use as therapeutic agents, for example, in treating wild-type HIV and of multidrug-resistant strains of HIV, also are disclosed.
摘要翻译：公开了可用于抑制HIV蛋白酶的化合物。还公开了制备化合物的方法及其作为治疗剂的用途，例如用于治疗野生型HIV和HIV耐药多药耐药菌株。

90. 发明申请

US20040029935A1 Heterocyclic aromatic compounds useful as growth hormone secretagogues 有权
公开(公告)号：US20040029935A1
公开(公告)日：2004-02-12
申请号：US10281649
申请日：2002-10-28
发明人： Jeffrey A. Robl , Joseph A. Tino , Andres S. Hernandez , Jun Li
IPC分类号： A61K031/427 , A61K031/426 , A61K031/4245 , A61K031/423 , A61K031/421 , A61K031/4184 , C07D271/06 , C07D271/12
CPC分类号： C07D233/54 , C07D235/14 , C07D249/08 , C07D249/12 , C07D257/04 , C07D263/32 , C07D271/06 , C07D277/28 , C07D277/64 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/06 , C07D417/06 , C07D417/12
摘要： Heterocyclic aromatic compounds are provided which are useful in stimulating endogenous production or release of growth hormone and in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength. The heterocyclic aromatic compounds have the structure 1 including pharmaceutically acceptable salts thereof and all stereoisomers thereof, wherein Xa is heteroaryl, preferably, 2 and R1, R1a, R6, Y, Xb, A, B, Z, R3, R4, R4a, R5 and R5a are as defined herein.

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