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91. 发明授权

US08357689B2 Substituted arylsulfonylaminomethylphosphonic acid derivatives, their preparation and their use in the treatment of type I and II diabetes mellitus 有权
标题翻译：取代的芳基磺酰氨基甲基膦酸衍生物，其制备及其在治疗I型和II型糖尿病中的应用
公开(公告)号：US08357689B2
公开(公告)日：2013-01-22
申请号：US12669978
申请日：2008-07-25
申请人： Holger Wagner , Elke Langkopf , Matthias Eckhardt , Ruediger Streicher , Corinna Schoelch , Annette Schuler-Metz , Alexander Pautsch
发明人： Holger Wagner , Elke Langkopf , Matthias Eckhardt , Ruediger Streicher , Corinna Schoelch , Annette Schuler-Metz , Alexander Pautsch
IPC分类号： A61K31/404 , A61K31/416 , A61K31/4184 , A61K31/423 , A61K31/428 , C07D237/04 , C07D403/04
CPC分类号： C07F9/5728 , C07F9/65038 , C07F9/65068 , C07F9/65324 , C07F9/6541 , C07F9/655354 , C07F9/65583 , C07F9/65586
摘要： The present invention relates to substituted arylsulphonylaminomethyl-phosphonic acid derivatives of general formula wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.
摘要翻译：本发明涉及以下通式的取代芳基磺酰氨基甲基膦酸衍生物其中R，X，Y和Z如权利要求1所定义，其互变异构体，对映异构体，非对映体，其混合物及其盐具有有价值的药理学性质，的糖原磷酸化酶a与糖原相关蛋白磷酸酶1（PP1）的GL亚基的相互作用，以及它们作为药物组合物的用途。

92. 发明申请

US20120225846A1 HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK 审中-公开
公开(公告)号：US20120225846A1
公开(公告)日：2012-09-06
申请号：US13410378
申请日：2012-03-02
申请人： John M. McCall , Donna L. Romero , Michael Clare
发明人： John M. McCall , Donna L. Romero , Michael Clare
IPC分类号： A61K31/404 , C07D241/12 , A61K31/4965 , C07D413/04 , A61K31/5377 , C07D471/04 , C07D487/04 , A61K31/55 , C07F9/572 , A61K31/675 , C07F5/02 , A61K31/69 , C07F9/6506 , A61P35/00 , A61P3/00 , A61P3/10 , A61P3/06 , A61P1/16 , A61P3/04 , A61P5/48 , C12N9/99 , C07D209/10
CPC分类号： A61K31/404 , C07D209/10 , C07D209/18 , C07D213/74 , C07D241/12 , C07D405/14 , C07D413/04 , C07D471/04 , C07D487/04 , C07F5/025 , C07F9/5728 , C07F9/65068 , C07F9/650952 , C12N9/1205
摘要： Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.

93. 发明授权

US07893271B2 Benzimidazole carbamates and (thio) carbamates, and the synthesis and use thereof 有权
标题翻译：苯并咪唑氨基甲酸酯和（硫代）氨基甲酸酯，及其合成和用途
公开(公告)号：US07893271B2
公开(公告)日：2011-02-22
申请号：US11997057
申请日：2006-07-18
申请人： Christophe Pierre Alain Chassaing
发明人： Christophe Pierre Alain Chassaing
IPC分类号： A61K31/675 , C07F9/06
CPC分类号： C07F9/65068
摘要： This invention relates to benzimidazole carbamates and (thio)carbamates corresponding to Formula I: Here, X1 and X2 are independently O or S, wherein at least one of X1 and X2 is O; Y1 and Y2 are independently O or S, wherein at least one of Y1 and Y2 is O; R1 is alkyl having from 1-4 carbon atoms; R2, R3, and R4 are independently hydrogen or a cation; R5 and R6 are independently hydrogen, halogen, alkyl (having from 1-8 carbon atoms), —OR7, —SR8, —CO—R9, —OSO2—Ar, or —S(O)R10; R7 is alkyl having from 1-8 carbon atoms; R8 is alkyl (having from 1-8 carbon atoms) or aryl; R9 is alkyl (having from 1-8 carbon atoms), cycloalkyl (having from 3-6 carbon atoms), or aryl; Ar is aryl; and R10 is alkyl (having from 1-8 carbon atoms) or aryl. The compounds generally are soluble and stable in water, and have antiparasitic (particularly anthelmintic) activity in vivo that is comparable to known water-insoluble benzimidazole carbamates (e.g., albendazole and fenbendazole).
摘要翻译：本发明涉及对应于式I的苯并咪唑氨基甲酸酯和（硫代）氨基甲酸酯：这里，X 1和X 2独立地为O或S，其中X 1和X 2中的至少一个为O; Y1和Y2独立地为O或S，其中Y1和Y2中的至少一个为O; R1是具有1-4个碳原子的烷基; R2，R3和R4独立地为氢或阳离子; R5和R6独立地是氢，卤素，具有1-8个碳原子的烷基，-OR7，-SR8，-CO-R9，-OSO2-Ar或-S（O）R10; R7是具有1-8个碳原子的烷基; R8是烷基（具有1-8个碳原子）或芳基; R9是烷基（具有1-8个碳原子），环烷基（具有3-6个碳原子）或芳基; Ar为芳基; 和R 10是烷基（具有1-8个碳原子）或芳基。化合物通常在水中是可溶的和稳定的，并且在体内具有与已知的水不溶性苯并咪唑氨基甲酸酯（例如阿苯达唑和芬苯达唑）相当的抗寄生虫（特别是驱肠虫）活性。

94. 发明申请

US20100210594A1 SUBSTITUTED ARYLSULFONYLAMINOMETHYLPHOSPHONIC ACID DERIVATIVES, THEIR PREPARATION AND THEIR USE IN THE TREATMENT OF TYPE I AND II DIABETES MELLITUS 有权
公开(公告)号：US20100210594A1
公开(公告)日：2010-08-19
申请号：US12669978
申请日：2008-07-25
申请人： Holger Wagner , Elke Langkopf , Matthias Eckhardt , Ruediger Streicher , Corinna Schoelch , Annette Schuler-Metz , Alexander Pautsch
发明人： Holger Wagner , Elke Langkopf , Matthias Eckhardt , Ruediger Streicher , Corinna Schoelch , Annette Schuler-Metz , Alexander Pautsch
IPC分类号： A61K31/675 , C07F9/6512 , C07F9/572 , C07F9/6509 , C07F9/645 , C07F9/6533 , C07F9/6521 , C07F9/6544 , C07F9/6503 , A61P3/10
CPC分类号： C07F9/5728 , C07F9/65038 , C07F9/65068 , C07F9/65324 , C07F9/6541 , C07F9/655354 , C07F9/65583 , C07F9/65586
摘要： The present invention relates to substituted arylsulphonylaminomethyl-phosphonic acid derivatives of general formula wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.

95. 发明申请

US20080070867A1 2-Imidazolone and 2-Imidazolidinone Heterocyclic Inhibitors of Tyrosine Phosphatases 审中-公开
标题翻译： 2-咪唑啉酮和2-咪唑啉酮杂环抑制剂酪氨酸磷酸酶
公开(公告)号：US20080070867A1
公开(公告)日：2008-03-20
申请号：US11814239
申请日：2006-01-17
申请人： Zacharia Cheruvallath , Joseph Semple , Vasanthakumar Rajappan , Darryl Rideout , Venkatachalapathi Yalamoori , Chung-Ying Tsai , Feiyue Wu , Lars Thoresen , Mark Shenderovich
发明人： Zacharia Cheruvallath , Joseph Semple , Vasanthakumar Rajappan , Darryl Rideout , Venkatachalapathi Yalamoori , Chung-Ying Tsai , Feiyue Wu , Lars Thoresen , Mark Shenderovich
IPC分类号： A61K31/675 , A61P3/10 , C07F9/02
CPC分类号： C07F9/65583 , C07F9/6506 , C07F9/65068 , C07F9/65586
摘要： Compounds and compositions are provided for modulating the activity of protein tyrosine phosphatases. The compounds for use in the compositions and methods provided herein have formulae (I) Protein tyrosine phosaphatase, including PTB-IB, mediated diseases and disorders include diabetes including Type 1 and Type 2 diabetes (and associated complications such as hypertension, ischemic diseases of the large and small blood vessels, blindness, circulatory problems, kidney failure and atherosclerosis), syndrome X, metabolic syndrome, glucose intolerance, insulin resistance, obesity, cancer, and neurodegenerative diseases.
摘要翻译：提供化合物和组合物用于调节蛋白酪氨酸磷酸酶的活性。用于本文提供的组合物和方法的化合物具有式（I）蛋白酪氨酸磷酸酶，包括PTB-IB，介导的疾病和病症包括糖尿病，包括1型和2型糖尿病（以及相关并发症，例如高血压，缺血性疾病大，小血管，失明，循环问题，肾功能衰竭和动脉粥样硬化），综合征X，代谢综合征，葡萄糖不耐受，胰岛素抵抗，肥胖，癌症和神经变性疾病。

96. 发明授权

US07064217B2 Agonists and antagonists of sphingosine-1-phosphate receptors 有权
标题翻译：激动剂和鞘氨醇-1-磷酸受体的拮抗剂
公开(公告)号：US07064217B2
公开(公告)日：2006-06-20
申请号：US10470820
申请日：2002-01-30
申请人： Timothy L. Macdonald , Kevin R. Lynch
发明人： Timothy L. Macdonald , Kevin R. Lynch
IPC分类号： C07D233/61 , A61K31/415
CPC分类号： C07F9/65068 , C07C237/04 , C07F9/091 , C07F9/3808
摘要： The present invention relates to S1P analogs that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds have the general structure (I), wherein R1 is C8–C22 alkyl, C8–C22 alkenyl or R12 is O, or R1 and R12 taken together form an optionally substituted aryl or an optionally substituted heteroaryl; R17 is H, alkyl or alkylaryl; R18 is N or CH; R2 and R3 are independently selected from the group consisting of H, NH2, and OH, with the proviso that at least one of R2 and R3 is NH2; R4 is selected from the group consisting of hydroxyl, phosphate, phosphonate methylene phosphonate, α-substituted methylene phosphonate, thiophoasphate and thiophosphonate; and R5 is C8–C22alkenyl.
摘要翻译：本发明涉及具有作为S1P受体调节剂的活性的S1P类似物以及这些化合物用于治疗与不适当S1P受体活性相关的疾病的用途。化合物具有通式（I），其中R 1是C 8 -C 22烷基，C 8 -C 22亚烯基或R 12是O，或R 1和R 12一起形成任选地取代的芳基或任选取代的杂芳基; R 17是H，烷基或烷基芳基; R 18是N或CH; R 2和R 3独立地选自H，NH 2和OH，条件是至少一个 R 2和R 3均为NH 2; R 4选自羟基，磷酸酯，膦酸亚甲基膦酸酯，α-取代亚甲基膦酸酯，硫代硫代磷酸酯和硫代膦酸酯; R 5是C 8 -C 22烯基。

97. 发明授权

US06645950B1 Benzimidazole vascular damaging agents 失效
标题翻译：苯并咪唑血管损伤剂
公开(公告)号：US06645950B1
公开(公告)日：2003-11-11
申请号：US09889061
申请日：2001-10-22
申请人： Peter David Davis
发明人： Peter David Davis
IPC分类号： A61K314184
CPC分类号： C07F9/65068 , A61K31/4184 , A61K31/675 , C07D235/32
摘要： Vascular damaging agents composed of substituted 5(6)-substituted benzimidazole-2-carbamates are provided. These agents are useful in the preparation of medicaments for the treatment of diseases involving neovascularisation, particularly for the treatment of solid tumors, macular degeneration, diabetic retinopathy, rheumatoid arthritis, psoriasis, and atherosclerosis. Embodiments include a 5(6)-substituted benzimidazole-2-carbamate of formula I wherein A represents a multi-substituted alkyl group or aromatic ring.
摘要翻译：提供由取代的5（6） - 取代的苯并咪唑-2-氨基甲酸酯组成的血管损伤剂。这些试剂可用于制备用于治疗涉及新血管形成的疾病的药物，特别是用于治疗实体瘤，黄斑变性，糖尿病性视网膜病，类风湿性关节炎，牛皮癣和动脉粥样硬化。实施方案包括式I的5（6） - 取代的苯并咪唑-2-氨基甲酸酯，其中A表示多取代的烷基或芳环。

98. 发明申请

US20030119754A1 Benzimidazole compounds and antiviral uses thereof 失效
标题翻译：苯并咪唑化合物及其抗病毒用途
公开(公告)号：US20030119754A1
公开(公告)日：2003-06-26
申请号：US10141839
申请日：2002-05-09
发明人： John William Lackey , Daniel S. Kinder , Nicolai A. Tvermoes
IPC分类号： A61K031/7052 , A61K031/675 , A61K031/655 , A61K031/4184 , C07H017/00 , C07D235/12 , C07D235/14
CPC分类号： C07D401/14 , C07D231/12 , C07D233/56 , C07D235/12 , C07D235/14 , C07D249/08 , C07D401/06 , C07D403/14 , C07D405/06 , C07D405/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/14 , C07F9/65068 , C07F9/65583
摘要： The present invention relates to novel benzimidazole compounds that have useful antiviral activity. More specifically, the invention encompasses benzimidazole compounds that inhibit membrane fusion associated events such as viral transmission, reduce viral load or otherwise treat viral infections. The invention also encompasses the use of benzimidazole compounds as inhibitors of membrane fusion associated events, such as viral transmission. In another embodiment, the invention encompasses processes for making benzimidazole compounds, methods of using the benzimidazole compounds and compositions comprising the benzimidazole compounds. Finally, the invention provides methods for treating, preventing or ameliorating symptoms associated with respiratory infection, particularly that caused by Respiratory Syncytial Virus utilizing the novel benzimidazole compounds of the invention.
摘要翻译：本发明涉及具有有用抗病毒活性的新型苯并咪唑化合物。更具体地，本发明包括抑制膜融合相关事件的苯并咪唑化合物，例如病毒传播，减少病毒载量或以其它方式治疗病毒感染。本发明还包括苯并咪唑化合物作为膜融合相关事件如病毒传播的抑制剂的用途。在另一个实施方案中，本发明包括制备苯并咪唑化合物的方法，使用苯并咪唑化合物的方法和包含苯并咪唑化合物的组合物。最后，本发明提供治疗，预防或改善与呼吸道感染有关的症状的方法，特别是利用本发明的新型苯并咪唑化合物由呼吸道合胞病毒引起的症状。

99. 发明授权

US06174874B1 Phosphonic acids derivatives as inhibitors of protein tyrosine phosphate 1B (PTP-1B) 失效
标题翻译：磷酸衍生物作为蛋白质酪氨酸磷酸1B（PTP-1B）的抑制剂
公开(公告)号：US06174874B1
公开(公告)日：2001-01-16
申请号：US09398356
申请日：1999-09-17
申请人： Zhaoyin Wang , Claude Dufresne , Yves Leblanc , Chun Sing Li , Jacques Y. Gauthier , Cheuk K. Lau , Michel Therien , Patrick Roy
发明人： Zhaoyin Wang , Claude Dufresne , Yves Leblanc , Chun Sing Li , Jacques Y. Gauthier , Cheuk K. Lau , Michel Therien , Patrick Roy
IPC分类号： A61K31663
CPC分类号： H04M3/42314 , C07F9/3856 , C07F9/386 , C07F9/3865 , C07F9/3869 , C07F9/3882 , C07F9/5537 , C07F9/65068 , C07F9/65188 , C07F9/6524 , C07F9/65318 , C07F9/65324 , C07F9/6539 , C07F9/65395 , C07F9/6541 , H04Q3/625 , H04Q2213/13104 , H04Q2213/13107 , H04Q2213/1322 , H04Q2213/1329 , H04Q2213/13389
摘要： The invention encompasses the novel class of compounds represented by formula I which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases.
摘要翻译：本发明包括作为PTP-1B酶抑制剂的由式I表示的新一类化合物。本发明还包括治疗或预防PTP-1B介导的疾病的药物组合物和方法。

100. 发明授权

US5910600A Bisphosphite compound, process for its production and hydroformylation process employing the bisphosphite compound 失效
标题翻译：二亚磷酸酯化合物，其生产方法和使用双亚磷酸酯化合物的加氢甲酰化方法
公开(公告)号：US5910600A
公开(公告)日：1999-06-08
申请号：US845835
申请日：1997-04-28
申请人： Hisao Urata , Hiroaki Itagaki , Eitaro Takahashi , Yasuhiro Wada , Yoshiyuki Tanaka , Yasukazu Ogino
发明人： Hisao Urata , Hiroaki Itagaki , Eitaro Takahashi , Yasuhiro Wada , Yoshiyuki Tanaka , Yasukazu Ogino
IPC分类号： C07C45/50 , C07C45/72 , C07C45/74 , C07F9/145 , C07F9/572 , C07F9/58 , C07F9/60 , C07F9/64 , C07F9/6506 , C07F9/6509 , C07F9/6512 , C07F9/6541 , C07F9/655 , C07F9/12
CPC分类号： C07F9/65517 , C07C45/50 , C07C45/72 , C07C45/74 , C07F9/145 , C07F9/5728 , C07F9/585 , C07F9/60 , C07F9/64 , C07F9/65068 , C07F9/650994 , C07F9/65125 , C07F9/65128 , C07F9/6541
摘要： A bisphosphite compound of the following formula (A): ##STR1## wherein --Ar--Ar-- is a bisarylene group represented by any one of the formulae (A-I) to (A-III) defined in the specification, and each of Z.sub.1 to Z.sub.4 is a C.sub.4-20 aromatic or heteroaromatic group which may have a substituent, wherein each of substituents on carbon atoms of an aromatic ring adjacent to the carbon atom bonded to the oxygen atom in each of Z.sub.1 to Z.sub.4, is a C.sub.0-2 group, and each pair of Z.sub.1 and Z.sub.2, and Z.sub.3 and Z.sub.4, are not bonded to each other.
摘要翻译：下式（A）的双亚磷酸酯化合物：其中-Ar-Ar-是由说明书中定义的式（AI）至（A-III）中任一个表示的双亚芳基，Z1至Z4各自为可以具有取代基的C 4-20芳族或杂芳族基，其中与Z1〜Z4各自键合的氧原子上的碳原子相邻的芳香环的碳原子上的各取代基为C0-2基，各自为一对Z1和Z2以及Z3和Z4彼此不接合。

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