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41. 发明申请

US20100016349A1 PSEUDOAZULENYL NITRONES 有权
公开(公告)号：US20100016349A1
公开(公告)日：2010-01-21
申请号：US12306246
申请日：2007-06-27
申请人： David A. Becker , Amolkumar Kolhe
发明人： David A. Becker , Amolkumar Kolhe
IPC分类号： A61K31/435 , C07D221/04 , A61P9/10
CPC分类号： C07D221/04 , C07D311/94 , C07D401/06 , C07D417/12
摘要： Disclosed herein are pseudoazulenyl nitrone compounds and methods of using these compounds to trap free radicals and to treat, prevent, or ameliorate various diseases associated with free radicals.
摘要翻译：本文公开的是假薁基硝酮化合物和使用这些化合物捕获自由基并治疗，预防或改善与自由基相关的各种疾病的方法。

42. 发明申请

US20090215815A1 Neurotrophin antagonist compositions 审中-公开
标题翻译：神经营养因子拮抗剂组合物
公开(公告)号：US20090215815A1
公开(公告)日：2009-08-27
申请号：US12453032
申请日：2009-04-28
申请人： Ashok Tehim , Xiannong Chen
发明人： Ashok Tehim , Xiannong Chen
IPC分类号： A61K31/473 , C07D221/04
CPC分类号： C07D221/14 , A61K31/473 , A61K31/4738 , C07D401/04 , C07D401/06 , C07D405/06
摘要： A pharmaceutical composition comprising a compound of Formula I wherein R1 is selected from, inter alia, alkyl, aryl-loweralkyl, heterocycle-loweralkyl, loweralkyl-carbonate; optionally substituted amino; benimidaz-2-yl; optionally substituted phenyl; loweralkyl-(R5)(R6) wherein one of R5 and R6 is selected from H and the other is selected from carboxy, carboxy-loweralkyl and loweralkoxycarbonyl; NHCH2CH2OX wherein X represents an in vivo hydrolyzable ester; and R2 and R3 are independently selected from H, NO2, halo, di(loweralkyl)amino, cyano, C(O)OH, phenyl-S—, loweralkyl, and Z(O)OR7 wherein Z is selected from C and S and R7 is selected from H, loweralkylamino and arylamino; or pharmaceutically acceptable salts or certain in vivo hydrolyzable esters or amides thereof, in an amount effective to inhibit neurotrophin-mediated activity, and a suitable carrier, is described.The compositions are useful to inhibit undesirable neurotrophin-mediated activity such as the neurite outgrowth that occurs in some neurodegenerative disease states.
摘要翻译：一种药物组合物，其包含式I化合物，其中R 1特别选自烷基，芳基 - 低级烷基，杂环 - 低级烷基，低级烷基 - 碳酸酯; 任选取代的氨基; 本咪唑-2-基; 任选取代的苯基; 低级烷基 - （R5）（R6）其中R5和R6之一选自H，另一个选自羧基，羧基 - 低级烷基和低级烷氧基羰基; NHCH2CH2OX其中X表示体内可水解的酯; 并且R 2和R 3独立地选自H，NO 2，卤素，二（低级烷基）氨基，氰基，C（O）OH，苯基-S-，低级烷基和Z（O）OR 7，其中Z选自C和S， R7选自H，低级烷基氨基和芳基氨基; 或其药学上可接受的盐或某些体内可水解的酯或酰胺，以有效抑制神经营养因子介导的活性的量和合适的载体。该组合物可用于抑制不期望的神经营养因子介导的活性，例如在一些神经变性疾病状态中发生的神经突生长。

43. 发明授权

US07553965B2 5-HT7 receptor antagonists 失效
标题翻译： 5-HT7受体拮抗剂
公开(公告)号：US07553965B2
公开(公告)日：2009-06-30
申请号：US11813069
申请日：2005-12-27
申请人： Antoni Torrens Jover , Susana Yenes Mínguez , Josep Mas Prió , Luz Romero Alonso , Alberto Dordal Zueras , Helmut Henrich Buschmann
发明人： Antoni Torrens Jover , Susana Yenes Mínguez , Josep Mas Prió , Luz Romero Alonso , Alberto Dordal Zueras , Helmut Henrich Buschmann
IPC分类号： C07D221/04 , A01N43/42
CPC分类号： C07D221/16 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14 , Y10S514/914 , Y10S514/923
摘要： The invention relates to compounds having pharmacological activity towards the 5-HT7 receptor, and more particularly to some 2,2a,4,5-tetrahydro-1H-3-aza-acenaphthylen substituted sulfonamide compounds, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which 5-HT is involved, such as CNS disorders.
摘要翻译：本发明涉及对5-HT 7受体具有药理活性的化合物，更具体地涉及一些2,2a，4,5-四氢-1H-3-氮杂 - 苊烯取代的磺酰胺化合物，用于制备这些化合物的方法，包含它们的药物组合物，以及它们用于治疗和/或预防其中涉及5-HT的疾病如CNS障碍的用途。

44. 发明申请

US20090121620A1 ORGANOMETALLIC COMPLEX, ORGANIC EL ELEMENT AND ORGANIC EL DISPLAY 审中-公开
标题翻译：有机复合物，有机EL元素和有机EL显示
公开(公告)号：US20090121620A1
公开(公告)日：2009-05-14
申请号：US12243695
申请日：2008-10-01
申请人： Tasuku SATOH , Wataru SOTOYAMA , Norio SAWATARI , Tetsuya MIYATAKE
发明人： Tasuku SATOH , Wataru SOTOYAMA , Norio SAWATARI , Tetsuya MIYATAKE
IPC分类号： H01J1/63 , C07D213/89 , C07F15/00 , C07D221/04
CPC分类号： C07F13/005 , C07F13/00 , C09K11/06 , C09K2211/10 , C09K2211/1007 , C09K2211/1011 , C09K2211/1022 , C09K2211/1029 , C09K2211/1037 , C09K2211/1044 , C09K2211/1088 , C09K2211/1092 , C09K2211/185 , C09K2211/187 , C09K2211/188 , H01L27/322 , H01L51/0035 , H01L51/005 , H01L51/0052 , H01L51/0059 , H01L51/0062 , H01L51/007 , H01L51/0081 , H01L51/0084 , H01L51/0087 , H01L51/5016 , H05B33/14
摘要： An organic EL element includes an organometallic complex including a rhenium atom; one ligand which has a coordinated nitrogen atom and a coordinated oxygen atom, each coordinated with the rhenium atom, and has at least one π conjugation part; and the other ligand coordinated with the rhenium atom in such a way that the ligand saturates the coordination number of the rhenium atom and the charge of the whole organometallic complex is neutral.
摘要翻译：有机EL元件包括含有铼原子的有机金属络合物; 一个具有配位的氮原子和配位氧原子的配位体，每个与铼原子配位，并具有至少一个π共轭部分; 而另一配体与铼原子配位，使配体饱和铼原子的配位数，整个有机金属络合物的电荷是中性的。

45. 发明申请

US20080176891A1 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：US20080176891A1
公开(公告)日：2008-07-24
申请号：US11858144
申请日：2007-09-20
申请人： Paul Bamborough , Michael David Barker , Sebastien Andre Campos , Richard Peter Charles Cousins , Paul Faulder , Heather Hobbs , Duncan Stuart Holmes , Michael John Johnston , John Liddle , Jeremy John Payne , John Martin Pritchard , Caroline Whitworth
发明人： Paul Bamborough , Michael David Barker , Sebastien Andre Campos , Richard Peter Charles Cousins , Paul Faulder , Heather Hobbs , Duncan Stuart Holmes , Michael John Johnston , John Liddle , Jeremy John Payne , John Martin Pritchard , Caroline Whitworth
IPC分类号： A61K31/437 , C07D221/04 , A61P29/00 , A61P19/02 , A61P11/06
CPC分类号： C07D471/04
摘要： The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds according to formula (I): and salts thereof.The compounds of the invention are inhibitors of kinase activity, in particular IKK2 activity.
摘要翻译：本发明涉及某些新化合物。具体地，本发明涉及根据式（I）的化合物及其盐。本发明的化合物是激酶活性的抑制剂，特别是IKK2活性。

46. 发明申请

US20080146563A1 1,7-Naphthyridines as Pde4 Inhibitors 审中-公开
标题翻译： 1,7-萘乙酸作为Pde4抑制剂
公开(公告)号：US20080146563A1
公开(公告)日：2008-06-19
申请号：US11908188
申请日：2006-03-16
申请人： Colin David Eldred , John Edward Robinson
发明人： Colin David Eldred , John Edward Robinson
IPC分类号： A61K31/5377 , C07D221/04 , A61K31/4375 , A61K31/496 , A61P37/08 , A61P29/00 , C07D295/00
CPC分类号： C07D471/04
摘要： There are provided according to the invention novel compounds of formula (I) and pharmaceutically acceptable salts and solvates thereof: wherein R1 is selected from the group consisting of C1-4alkyl, C4-6cycloalkyl(CH2)m—, methoxyC2-4alkyl, HOCH2CH2—, R3(O)2S(CH2)2—, R5R4NCO(CH2)n—, and heterocyclyl(CH2)m— wherein any nitrogen heteroatom of the heterocyclyl radical may be unsubstituted or substituted by methyl; R2 is hydrogen or methyl; R3 is methyl or NH2; R4-5 independently represent methyl, m is 0, 1 or 2; and n is 1 or 2; or R1 and R2 together with the nitrogen atom to which they are attached may form a heterocyclyl ring, which may be unsubstituted or substituted by one or two substituents selected from the group consisting of; methyl, ═O and (CH3)2N—.
摘要翻译：根据本发明提供新的式（I）化合物及其药学上可接受的盐和溶剂合物：其中R 1选自C 1-4烷基，烷基，C 4-6环烷基（CH 2 CH 2）m - ，甲氧基C 2-4烷基，（O）2 S 2（CH 2）2 - - - - （CH 2） R 2，R 5，R 5，R 5，N 2，N 2，和杂环基（CH 2 CH 2）m - ，其中杂环基的任何氮杂原子可以是未取代的或被甲基取代; R 2是氢或甲基; R 3是甲基或NH 2; R 4-5独立地表示甲基，m是0,1或2; n为1或2; 或R 1和R 2与它们所连接的氮原子一起可以形成杂环基环，其可以是未取代的或被一个或两个选自以下的取代基取代：组成; 甲基，-O和（CH 3）2 N - 。

47. 发明申请

US20080139538A1 Tertiary Carbinamines Having Substituted Heterocycles Which Are Active As Beta-Secretase Inhibitors For The Treatment Of Alzheimer's Disease 有权
标题翻译：具有作为β-分泌酶抑制剂作为阿尔茨海默氏病治疗活性的取代的杂环的三级甲苯胺
公开(公告)号：US20080139538A1
公开(公告)日：2008-06-12
申请号：US11795190
申请日：2006-01-13
申请人： Georgia B. McGaughey , Philippe G. Nantermet , Hemaka A. Rajapakse , Shaun R. Stauffer
发明人： Georgia B. McGaughey , Philippe G. Nantermet , Hemaka A. Rajapakse , Shaun R. Stauffer
IPC分类号： A61K31/4245 , C07D243/14 , C07D403/02 , C07D237/30 , C07D221/04 , C07D401/02 , C07D271/06 , A61K31/5513 , A61K31/5377 , A61K31/501 , A61K31/4439 , A61K31/454 , A61P25/28
CPC分类号： C07D413/04 , C07D271/10 , C07D271/107 , C07D405/04 , C07D413/06 , C07D413/08 , C07D413/10 , C07D413/14 , C07D417/04 , C07D417/06 , C07D451/02 , C07D453/02 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention is directed to tertiary carbinamine compounds having substituted heterocycles, which are inhibitors of the beta-secretase enzyme, and are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
摘要翻译：本发明涉及具有取代杂环的叔胺组合物，其是β-分泌酶的抑制剂，并且可用于治疗涉及β-分泌酶的疾病，例如阿尔茨海默氏病。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗涉及β-分泌酶的疾病中的用途。

48. 发明申请

US20080139461A1 Peptidomimetic Compounds and Preparation of Biologically Active Derivatives 审中-公开
标题翻译：拟肽化合物和生物活性衍生物的制备
公开(公告)号：US20080139461A1
公开(公告)日：2008-06-12
申请号：US11883880
申请日：2006-03-03
申请人： Carlo Scolastico , Leonardo Manzoni , Daniela Arosio
发明人： Carlo Scolastico , Leonardo Manzoni , Daniela Arosio
IPC分类号： A61K38/06 , C07D221/04 , C07D487/04 , A61K31/55 , A61P35/00 , A61K31/435 , C07K5/02
CPC分类号： C07K7/64 , C07D401/06 , C07D471/04 , C07K5/06139
摘要： The invention relates to novel cyclic peptidomimetic compounds containing the sequence RGD for the preparation of appropriately functionalised antagonists of αvβ3 and αvβ5 integrins, and intended, for example, for the treatment of altered angiogenic phenomena or for the preparation of diagnostically useful compounds.
摘要翻译：本发明涉及含有序列RGD的新型环状拟肽化合物，其用于制备αphavbeta3和alphavbeta5整联蛋白的适当功能化的拮抗剂，并且旨在例如用于治疗改变的血管发生现象或用于制备诊断上有用的化合物。

49. 发明申请

US20080103139A1 3-Carbamoyl-2-Pyridone Derivative 有权
标题翻译： 3-氨基甲酰基-2-吡啶酮衍生物
公开(公告)号：US20080103139A1
公开(公告)日：2008-05-01
申请号：US11628804
申请日：2005-10-28
申请人： Natsuki Ishizuka , Takashi Sasatani , Yoshiharu Hiramatsu , Masanao Inagaki , Masahide Odan , Hiroshi Hashizume , Susumu Mitsumori , Yasuhiko Fujii , Yoshikazu Fukui , Hideaki Watanabe , Jun Sato
发明人： Natsuki Ishizuka , Takashi Sasatani , Yoshiharu Hiramatsu , Masanao Inagaki , Masahide Odan , Hiroshi Hashizume , Susumu Mitsumori , Yasuhiko Fujii , Yoshikazu Fukui , Hideaki Watanabe , Jun Sato
IPC分类号： A61K31/5377 , C07D221/04 , A61K31/435 , C07D211/84 , A61K31/4412 , A61P17/00 , C07D401/12 , A61K31/496 , A61K31/506 , C07D413/12
CPC分类号： C07D213/82
摘要： The present invention provides compounds having an agonistic activity to the cannabinoid receptor, which is represented by the formula (I): wherein R1 is optionally substituted C1-C8 alkyl and the like; R2 is C1-C6 alkyl; R3 is C1-C6 alkyl and the like; or R2 and R3 taken together with may form an optionally substituted 5 to 10 membered non-aromatic carbon ring; R4 is hydrogen and the like; G is a group selected from the groups shown by the formula an the like: wherein R5 is hydrogen and the like; X1 is a single bond and the like; X2 is optionally substituted C1-C8 alkylene that may be replaced by one or two groups of —O—, or —N(R6)—, wherein R6 is hydrogen and the like, and the like; X3 is a single bond and the like; a pharmaceutically acceptable salt or a solvate thereof, and pharmaceutical compositions, atopic dermatitis treating agents, and anti-pruritus agents, especially anti-pruritus agents for oral used and for external application, which each contains the said compound as an active ingredient.
摘要翻译：本发明提供对大麻素受体具有激动作用的化合物，其由式（I）表示：其中R 1是任选取代的C 1 -C 8烷基等; R 2是C 1 -C 6烷基; R 3是C 1 -C 6烷基等; 或R 2和R 3与相邻碳原子一起可以形成任选取代的5至10元非芳族碳环; R 4是氢等; G为选自下式的基团：其中R 5为氢等; X 1是单键等; X 2是任选取代的C 1 -C 8亚烷基，其可以被一个或两个-O-或-N（R 6） - 基团取代，其中R 0 > 6是氢等; X 3是单键等; 其药学上可接受的盐或溶剂合物，以及药物组合物，特应性皮炎治疗剂和抗瘙痒剂，特别是用于口服和外用的抗瘙痒剂，其各自含有所述化合物作为活性成分。

50. 发明授权

US06972296B2 Carboxylic acid derivatives that inhibit the binding of integrins to their receptors 有权
标题翻译：抑制整联蛋白与其受体结合的羧酸衍生物
公开(公告)号：US06972296B2
公开(公告)日：2005-12-06
申请号：US09973142
申请日：2001-10-09
申请人： Ronald J. Biediger , Qi Chen , E. Radford Decker , George W. Holland , Jamal M. Kassir , Wen Li , Robert V. Market , Ian L. Scott , Chengde Wu , Jian Li
发明人： Ronald J. Biediger , Qi Chen , E. Radford Decker , George W. Holland , Jamal M. Kassir , Wen Li , Robert V. Market , Ian L. Scott , Chengde Wu , Jian Li
IPC分类号： C07D221/04 , A61K31/435 , A61K31/44 , A61K31/4412 , A61K31/4704 , A61K31/495 , A61K31/50 , A61K31/505 , A61P1/00 , A61P3/10 , A61P9/10 , A61P11/06 , A61P19/02 , A61P25/00 , A61P29/00 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/08 , C07D207/416 , C07D211/86 , C07D213/02 , C07D213/62 , C07D213/69 , C07D213/72 , C07D213/75 , C07D215/22 , C07D215/38 , C07D221/16 , C07D237/16 , C07D237/22 , C07D239/28 , C07D239/46 , C07D239/47 , C07D317/46 , C07D317/60 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/06 , C07D413/12 , C07D417/06 , C07D471/04 , C07D498/04 , C07K14/78 , C07D211/72
CPC分类号： C07D213/75 , C07D215/22 , C07D221/04 , C07D221/16 , C07D237/22 , C07D239/47 , C07D317/60 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/12 , C07D417/06 , C07D471/04
摘要： A method for the inhibition of the binding of α4β1 integrin to its receptors, for example VCAM-1 (vascular cell adhesion molecule-1) and fibronectin; compounds that inhibit this binding; pharmaceutically active compositions comprising such compounds; and to the use of such compounds either a above, or in formulations for the control or prevention of diseases states in which α4β1 is involved.
摘要翻译：用于抑制α4A/β1整联蛋白与其受体例如VCAM-1（血管细胞粘附分子-1）和纤连蛋白的结合的方法; 抑制这种结合的化合物; 包含这些化合物的药物活性组合物; 以及上述或在制剂中使用这些化合物用于控制或预防涉及α4β1的疾病状态。

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