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71. 发明申请

US20100016304A1 GLUCOKINASE ACTIVATOR 有权
公开(公告)号：US20100016304A1
公开(公告)日：2010-01-21
申请号：US12448549
申请日：2007-12-21
申请人： Yasumichi Fukuda , Yoshikazu Asahina , Ayako Nakamura , Kenji Fujita , Tomohiro Ide , Fumiyoshi Kobayashi , Shinji Kobayashi , Kanji Komatsu , Masanori Yamamoto
发明人： Yasumichi Fukuda , Yoshikazu Asahina , Ayako Nakamura , Kenji Fujita , Tomohiro Ide , Fumiyoshi Kobayashi , Shinji Kobayashi , Kanji Komatsu , Masanori Yamamoto
IPC分类号： A61K31/5377 , C07D263/14 , A61K31/421 , A61K31/426 , C07D277/28 , C07D513/04 , A61K31/4365 , C07D417/12 , A61P3/10
CPC分类号： C07C317/44 , C07C2601/08 , C07D213/75 , C07D213/80 , C07D215/38 , C07D217/22 , C07D231/40 , C07D237/20 , C07D239/42 , C07D241/20 , C07D241/28 , C07D241/44 , C07D261/14 , C07D263/48 , C07D275/02 , C07D277/20 , C07D277/46 , C07D277/82 , C07D285/08 , C07D417/04 , C07D471/04 , C07D487/04 , C07D498/04 , C07D513/04
摘要： A compound represented by the following formula (1): (wherein the carbon atom denoted by * is in the R-configuration; R1 and R2 are each independently a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C1-C6 alkyl group, a C1-C6 alkoxy group, a C1-C6 alkylsulfanyl group, a C1-C6 alkylsulfinyl group or a C1-C6 alkylsulfonyl group; and A is a substituted or unsubstituted heteroaryl group), or a pharmaceutically acceptable salt thereof.
摘要翻译：由下式（1）表示的化合物：（其中由*表示的碳原子为R构型; R 1和R 2各自独立地为氢原子，卤素原子，氨基，羟基，羟基氨基基团，硝基，氰基，氨磺酰基，C1-C6烷基，C1-C6烷氧基，C1-C6烷基硫烷基，C1-C6烷基亚磺酰基或C1-C6烷基磺酰基;以及 A是取代或未取代的杂芳基）或其药学上可接受的盐。

72. 发明授权

US07345043B2 Inhibitors of histone deacetylase 失效
标题翻译：组蛋白脱乙酰酶抑制剂
公开(公告)号：US07345043B2
公开(公告)日：2008-03-18
申请号：US11096550
申请日：2005-04-01
申请人： Sampath K. Anandan , Xiao-Yi Xiao , Dinesh V. Patel , John Ward
发明人： Sampath K. Anandan , Xiao-Yi Xiao , Dinesh V. Patel , John Ward
IPC分类号： A61K31/497 , A61K31/427 , A61K31/4535 , A61K31/454 , C07D417/04 , C07D277/28
CPC分类号： C07D277/56 , C07D277/42 , C07D417/04
摘要： Disclosed are compounds which inhibit histone deacetylase (HDAC) enzymatic activity. Also disclosed are pharmaceutical compositions comprising such compounds as well as methods to treat conditions, particularly proliferative conditions, mediated at least in part by HDAC.
摘要翻译：公开了抑制组蛋白脱乙酰酶（HDAC）酶活性的化合物。还公开了包含这些化合物的药物组合物以及至少部分由HDAC介导的治疗条件，特别是增殖病症的方法。

73. 发明申请

US20070254930A1 Oral Preparation Having Improved Bioavailability 审中-公开
标题翻译：具有改善生物利用度的口服制剂
公开(公告)号：US20070254930A1
公开(公告)日：2007-11-01
申请号：US11577469
申请日：2005-11-22
申请人： Jei Ryu , Soon Cho , Se Jung , Seung-Kyoo Seong , Eun Cho , Seok Ahn , Yun-Jung Kim
发明人： Jei Ryu , Soon Cho , Se Jung , Seung-Kyoo Seong , Eun Cho , Seok Ahn , Yun-Jung Kim
IPC分类号： A61K31/426 , A61P19/10 , C07D277/28
CPC分类号： C07D277/24 , A61K9/143 , A61K31/426
摘要： The present invention relates to an oral preparation of N-hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl) phenoxy]pentoxyl-benzamidine having improved bioavailability. More particularly, the present invention relates to an oral preparation comprising: N-hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl) phenoxy]pentoxy}-benzamidine or pharmaceutically acceptable salt thereof; and one or more carbonates selected from the group consisting of alkalimetal carbonate, alkalimetal bicarbonate and alkaline earth metal carbonate, and/or one or more disintegrants selected from the group consisting of sodium starch glycolate, carmellose calcium and croscarmellose sodium. The oral preparation according to the present invention inhibits gelation of N-hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl) phenoxy]pentoxy}-benzamidine or pharmaceutically acceptable salt thereof in the early stage of release, which increases dissolution rate and remarkably raises bioavailability.
摘要翻译：本发明涉及具有改善的生物利用度的N-羟基-4- {5- [4-（5-异丙基-2-甲基-1,3-噻唑-4-基）苯氧基]戊氧基 - 苄脒的口服制剂。更具体地说，本发明涉及包含N-羟基-4- {5- [4-（5-异丙基-2-甲基-1,3-噻唑-4-基）苯氧基]戊氧基} - 苄脒的口服制剂或其药学上可接受的盐; 和一种或多种选自碳酸亚烷基碳酸盐，碱金属碳酸氢盐和碱土金属碳酸盐的碳酸盐，和/或选自淀粉羟乙酸钠，羧甲纤维素钙和交联羧甲基纤维素钠的一种或多种崩解剂。根据本发明的口服制剂抑制N-羟基-4- {5- [4-（5-异丙基-2-甲基-1,3-噻唑-4-基）苯氧基]戊氧基} - 苄脒或药学上的凝胶化在释放的早期阶段可接受的盐，其增加溶解速率并显着提高生物利用度。

74. 发明授权

US07189722B2 Aryl spirohydantoin CGRP receptor antagonists 有权
标题翻译：芳基螺乙内酰脲CGRP受体拮抗剂
公开(公告)号：US07189722B2
公开(公告)日：2007-03-13
申请号：US10547227
申请日：2004-03-10
申请人： Ian M. Bell , Cory R. Theberge , Xu-Fang Zhang , C. Blair Zartman
发明人： Ian M. Bell , Cory R. Theberge , Xu-Fang Zhang , C. Blair Zartman
IPC分类号： A61K31/4166 , A61K31/498 , A61K31/4709 , A61K31/427 , C07D233/76 , C07D241/36 , C07D215/14 , C07D277/28
CPC分类号： C07D235/02 , C07D401/12 , C07D403/12 , C07D417/12
摘要： The present invention is directed to compounds that are antagonists of CGRP receptors and that are useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
摘要翻译：本发明涉及作为CGRP受体的拮抗剂的化合物，其可用于治疗或预防涉及CGRP的疾病，例如头痛，偏头痛和丛集性头痛。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预防或治疗涉及CGRP的疾病中的用途。

75. 发明授权

US07098227B2 Disubstituted thiazolyl carboxanilides and their use as microbicides 有权
标题翻译：二取代噻唑基甲酰苯胺及其作为杀微生物剂的用途
公开(公告)号：US07098227B2
公开(公告)日：2006-08-29
申请号：US10502962
申请日：2003-01-22
申请人： Ralf Dunkel , Hans-Ludwig Elbe , Heiko Rieck , Karl-Heinz Kuck , Ulrike Wachendorff-Neumann , Astrid Mauler-Machnik
发明人： Ralf Dunkel , Hans-Ludwig Elbe , Heiko Rieck , Karl-Heinz Kuck , Ulrike Wachendorff-Neumann , Astrid Mauler-Machnik
IPC分类号： A01N43/78 , C07D277/28
CPC分类号： C07D277/56 , A01N43/78 , C07F5/025
摘要： The present invention relates to novel thiazolylcarboxanilides of formula (I) in which R1 and R2 are as defined in the disclosure, to a plurality of processes for preparing these substances and their use for controlling unwanted microorganisms, and further relates to novel intermediates of their preparation.
摘要翻译：本发明涉及式（I）的新的噻唑羧酰苯胺，其中R 1和R 2如本公开所定义，涉及制备这些物质的多种方法和它们用于控制有害微生物的用途，还涉及其制备的新型中间体。

76. 发明申请

US20050267032A1 Sulfone-containing prodrugs 审中-公开
标题翻译：含砜的前药
公开(公告)号：US20050267032A1
公开(公告)日：2005-12-01
申请号：US11136243
申请日：2005-05-23
申请人： Alan Fulp , Grant McNaughton-Smith , Aimee Reed , Xiadong Wang
发明人： Alan Fulp , Grant McNaughton-Smith , Aimee Reed , Xiadong Wang
IPC分类号： A61K31/18 , A61K31/381 , A61K31/4245 , A61K31/66 , A61K38/18 , A61P27/06 , C07C311/21 , C07D263/30 , C07D263/32 , C07D271/06 , C07D277/28 , C07F9/09 , C07F9/653
CPC分类号： C07D271/06 , C07C311/21 , C07D263/32 , C07D277/28 , C07F9/653
摘要： Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides sulfone-containing prodrugs, and compositions and methods utilizing sulfone-containing prodrugs that are useful in the treatment of diseases by blocking potassium channels associated with the onset or recurrence of the indicated conditions. Exemplary diseases treatable with the compounds, compositions and methods of the invention include sickle cell disease and glaucoma.
摘要翻译：提供了通过电压依赖钾通道调节钾离子通量可用于治疗疾病的化合物，组合物和方法。更具体地，本发明提供含砜的前药，以及利用含砜前药的组合物和方法，其可用于通过阻断与指定条件的发作或复发相关的钾通道来治疗疾病。用本发明化合物，组合物和方法治疗的示例性疾病包括镰状细胞病和青光眼。

77. 发明申请

US20050240023A1 Cathepsin cysteine protease inhibitors 有权
标题翻译：组织蛋白酶半胱氨酸蛋白酶抑制剂
公开(公告)号：US20050240023A1
公开(公告)日：2005-10-27
申请号：US10505796
申请日：2003-02-28
申请人： Christopher Bayly , Cameron Black , Serge Leger , Chun Ku , Dan McKay , Christophe Mellon , Jacques Gauthier , Vouy-Linh Truong , Cheuk Lau , Michel Therien
发明人： Christopher Bayly , Cameron Black , Serge Leger , Chun Ku , Dan McKay , Christophe Mellon , Jacques Gauthier , Vouy-Linh Truong , Cheuk Lau , Michel Therien
IPC分类号： C07D295/12 , A61K31/275 , A61K31/381 , A61K31/404 , A61K31/417 , A61K31/42 , A61K31/4245 , A61K31/426 , A61K31/427 , A61K31/44 , A61K31/4406 , A61K31/4409 , A61K31/4465 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/5375 , A61K45/00 , A61P1/02 , A61P3/14 , A61P19/02 , A61P19/08 , A61P19/10 , A61P29/00 , A61P35/00 , A61P43/00 , C07C255/25 , C07C255/29 , C07C255/46 , C07C255/58 , C07C255/60 , C07C259/10 , C07C311/37 , C07C317/32 , C07C317/36 , C07D209/08 , C07D211/26 , C07D211/38 , C07D213/36 , C07D213/38 , C07D213/57 , C07D213/61 , C07D213/64 , C07D213/70 , C07D213/71 , C07D213/74 , C07D213/89 , C07D215/12 , C07D231/12 , C07D233/54 , C07D233/64 , C07D239/06 , C07D239/26 , C07D241/12 , C07D261/08 , C07D263/32 , C07D271/06 , C07D277/28 , C07D295/135 , C07D295/22 , C07D307/52 , C07D333/20 , C07D401/04 , C07D417/04
CPC分类号： C07C237/20 , A61K31/165 , A61K31/18 , A61K31/4174 , A61K31/426 , A61K31/44 , A61K31/4418 , A61K31/495 , C07C255/25 , C07C255/29 , C07C255/46 , C07C255/58 , C07C259/10 , C07C311/37 , C07C317/32 , C07C2601/02 , C07C2601/14 , C07D209/08 , C07D213/38 , C07D213/57 , C07D213/64 , C07D213/70 , C07D213/89 , C07D215/12 , C07D231/12 , C07D233/64 , C07D239/26 , C07D241/12 , C07D261/08 , C07D263/32 , C07D271/06 , C07D277/28 , C07D277/30 , C07D295/135 , C07D295/155 , C07D307/52 , C07D333/20 , C07D401/04 , C07D417/04
摘要： This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
摘要翻译：本发明涉及一类新的化合物，它们是半胱氨酸蛋白酶抑制剂，包括但不限于组织蛋白酶K，L，S和B的抑制剂。这些化合物可用于治疗其中指示抑制骨吸收的疾病，例如骨质疏松症

78. 发明授权

US06958331B1 Bradykinin receptor antagonists 失效
标题翻译：缓激肽受体拮抗剂
公开(公告)号：US06958331B1
公开(公告)日：2005-10-25
申请号：US10009009
申请日：2000-06-02
申请人： Christopher Thomas Brain , William Cantrell , Andrew James Culshaw , Edward Karol Dziadulewicz , Terance William Hart , Timothy John Ritchie , Liladhar Waykole
发明人： Christopher Thomas Brain , William Cantrell , Andrew James Culshaw , Edward Karol Dziadulewicz , Terance William Hart , Timothy John Ritchie , Liladhar Waykole
IPC分类号： C07D295/18 , A61K31/4406 , A61K31/4409 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K31/63 , A61P1/04 , A61P1/18 , A61P7/10 , A61P9/02 , A61P9/10 , A61P11/00 , A61P11/02 , A61P11/06 , A61P13/10 , A61P15/00 , A61P15/06 , A61P17/00 , A61P17/02 , A61P17/04 , A61P17/06 , A61P19/02 , A61P19/04 , A61P19/06 , A61P21/00 , A61P21/02 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/06 , A61P25/08 , A61P27/02 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/08 , A61P41/00 , A61P43/00 , C07C311/44 , C07D211/34 , C07D211/62 , C07D211/82 , C07D213/38 , C07D261/08 , C07D277/28 , C07D295/192 , C07D295/26 , C07D333/20 , C07D401/12 , C07D413/14
CPC分类号： C07D295/192 , C07D211/34 , C07D211/62 , C07D295/26 , C07D401/12
摘要： The invention relates to sulfonyl amine derivatives of formula IA wherein R5A, X1, X2, R9 and R10 are as defined herein, which derivatives are useful as bradykinin B1 receptor antagonists.
摘要翻译：本发明涉及式IA的磺酰胺衍生物，其中R 5，X 1，X 2，R 9， R 10和R 10如本文所定义，该衍生物可用作缓激肽B 1受体拮抗剂。

79. 发明申请

US20050222207A1 Phosphodiesterase 4 inhibitors, including N-substituted diarylamine analogs 审中-公开
标题翻译：磷酸二酯酶4抑制剂，包括N-取代的二芳基胺类似物
公开(公告)号：US20050222207A1
公开(公告)日：2005-10-06
申请号：US11008775
申请日：2004-12-10
申请人： Richard Schumacher , Allen Hopper , Robert Dunn , Erik Kuester , Ashok Tehim , Thomas Renau , Joan Caroon , Francisco Talamas , Sharada Labadie
发明人： Richard Schumacher , Allen Hopper , Robert Dunn , Erik Kuester , Ashok Tehim , Thomas Renau , Joan Caroon , Francisco Talamas , Sharada Labadie
IPC分类号： A61K31/444 , A61K31/4545 , C07D213/74 , C07D213/75 , C07D277/28 , C07D401/12 , C07D405/12 , C07D405/14 , C07D41/14
CPC分类号： C07D213/74 , A61K31/444 , A61K31/4545 , C07C229/60 , C07D213/36 , C07D213/75 , C07D277/28 , C07D401/12 , C07D405/12 , C07D405/14
摘要： PDE4 inhibition is achieved by novel compounds, e.g., N-substituted diarylamine analogs. The compounds of the present invention are of Formula I: wherein A, B, D, R1, R2, R3 and R4 are as defined herein.
摘要翻译： PDE4抑制通过新化合物，例如N-取代的二芳基胺类似物来实现。本发明的化合物具有式I：其中A，B，D，R 1，R 2，R 3和R 3， SUP> 4 如本文所定义。

80. 发明授权

US06936630B2 Substituted 1-aryl-3-heteroaryl-thioureas and substituted 1-aryl-3-heteroaryl-isothioureas as antiatherosclerotic agents 失效
标题翻译：取代的1-芳基-3-杂芳基 - 硫脲和取代的1-芳基-3-杂芳基 - 异硫脲作为抗动脉粥样硬化剂
公开(公告)号：US06936630B2
公开(公告)日：2005-08-30
申请号：US10733507
申请日：2003-12-10
申请人： Robert J. Steffan , Amedeo A. Failli
发明人： Robert J. Steffan , Amedeo A. Failli
IPC分类号： A61K31/415 , C07D231/40 , C07D263/48 , C07D275/02 , C07D275/03 , C07D277/28 , C07D277/48 , C07D277/82 , C07D277/84 , C07D285/12 , C07D285/135 , A61K31/425
CPC分类号： C07D275/03 , A61K31/415 , C07D231/40 , C07D263/48 , C07D277/48 , C07D277/82 , C07D277/84 , C07D285/135
摘要： Antiatherosclerotic agents are provided which are represented by Formulas I or II: wherein R is wherein R9, R10, R11, R12, R13, and R14 are each, independently, hydrogen or a lower alkyl of 1-6 carbon atoms; R6, and R7 are each, independently, hydrogen, lower alkyl of 1-6 carbon atoms, or CH2COOR8, where R8 is a lower alkyl of 1-6 carbon atoms; and X is O or S; R1 is hydrogen or a lower alkyl of 1-6 carbon atoms; R2, R3, and R4 are each, independently, hydrogen or halogen; and R5 is a lower alkyl of 1-6 carbon atoms; or a pharmaceutically acceptable salt thereof.
摘要翻译：提供抗动脉粥样硬化剂，其由式I或II表示：其中R是其中R 9，R 10，R 11，R SUB R 12，R 13和R 14各自独立地为氢或1-6个碳原子的低级烷基; R 6和R 7各自独立地为氢，1-6个碳原子的低级烷基或CH 2 CO 2， 8，其中R 8是1-6个碳原子的低级烷基; X为O或S; R 1是氢或1-6个碳原子的低级烷基; R 2，R 3和R 4各自独立地为氢或卤素; 并且R 5是1-6个碳原子的低级烷基; 或其药学上可接受的盐。

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