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141. 发明申请

US20090325980A1 PIPERIDINE OR PIPERAZINE SUBSTITUTED TETRAHYDRO-NAPHTHALENE-1-CARBOXYLIC ACID MTP INHIBITING COMPOUNDS 有权
标题翻译：哌啶或哌啶取代的四氢萘-1-羧酸的MTP抑制化合物
公开(公告)号：US20090325980A1
公开(公告)日：2009-12-31
申请号：US12446580
申请日：2007-10-22
申请人： Lieven Meerpoel , Joannes Theodorus Maria Linders , Libuse Jaroskova , Marcel Viellevoye , Leo Jacobus Jozef Backx , Didier Jean-Claude Berthelot , Guuske Frederike Busscher
发明人： Lieven Meerpoel , Joannes Theodorus Maria Linders , Libuse Jaroskova , Marcel Viellevoye , Leo Jacobus Jozef Backx , Didier Jean-Claude Berthelot , Guuske Frederike Busscher
IPC分类号： A61K31/4468 , A61K31/4965 , A61K31/4545 , C07D295/10 , C07D401/14 , C07D401/12 , C07D211/58 , A61P3/00
CPC分类号： C07D241/20 , C07D211/58 , C07D295/10 , C07D401/12 , C07D401/14
摘要： The present invention is concerned with novel piperidine or piperazine substituted tetrahydro-naphthalene-1-carboxylic acid derivatives having apoB secretion/MTP inhibiting activity and concomitant lipid lowering activity. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of atherosclerosis, pancreatitis, obesity, hypertriglyceridemia, hypercholesterolemia, hyperlipidemia, diabetes and type II diabetes.
摘要翻译：本发明涉及具有apoB分泌/ MTP抑制活性和伴随的降脂活性的新型哌啶或哌嗪取代的四氢 - 萘-1-羧酸衍生物。本发明还涉及制备这些化合物的方法，包含所述化合物的药物组合物以及所述化合物作为治疗动脉粥样硬化，胰腺炎，肥胖症，高甘油三酯血症，高胆固醇血症，高脂血症，糖尿病和II型糖尿病的药物的用途。

142. 发明申请

US20090069310A1 Anti-inflammatory medicaments 审中-公开
公开(公告)号：US20090069310A1
公开(公告)日：2009-03-12
申请号：US11450852
申请日：2006-06-09
申请人： Daniel L. Flynn , Peter A. Petillo
发明人： Daniel L. Flynn , Peter A. Petillo
IPC分类号： A61K31/4155 , A61K31/506 , A61K31/4709 , A61K31/5377 , A61K31/541 , A61P29/00 , A61K31/4439 , A61K31/427 , A61K31/4184
CPC分类号： C07D239/42 , C07D295/10 , C07D401/04 , C07D403/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds.

143. 发明申请

US20080187978A1 Anti-inflammatory medicaments 审中-公开
标题翻译：抗炎药物
公开(公告)号：US20080187978A1
公开(公告)日：2008-08-07
申请号：US11337245
申请日：2006-01-20
申请人： Daniel L. Flynn , Peter A. Petillo
发明人： Daniel L. Flynn , Peter A. Petillo
IPC分类号： C12N9/96
CPC分类号： C07D239/42 , C07D295/10 , C07D401/04 , C07D403/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds.
摘要翻译：提供了新的化合物和使用这些化合物治疗炎性病症的方法。在优选的实施方案中，调节p38激酶蛋白的活化状态包括使激酶蛋白与新化合物接触的步骤。

144. 发明申请

US20040171075A1 Modulation of protein functionalities 审中-公开
标题翻译：蛋白质功能的调节
公开(公告)号：US20040171075A1
公开(公告)日：2004-09-02
申请号：US10746545
申请日：2003-12-24
发明人： Daniel L. Flynn , Peter A. Petillo
IPC分类号： G01N033/53 , G06F019/00 , G01N033/48 , G01N033/50
CPC分类号： C07D239/42 , C07D295/10 , C07D401/04 , C07D403/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： New methods for the rational identification of molecules capable of interacting with specific naturally occurring proteins are provided, in order to yield new pharmacologically important compounds and treatment modalities. Broadly, the method comprises the steps of identifying a switch control ligand forming a part of a particular protein of interest, and also identifying a complemental switch control pocket forming a part of the protein and which interacts with said switch control ligand. The ligand interacts in vivo with the pocket to regulate the conformation and biological activity of the protein such that the protein assumes a first conformation and a first biological activity upon the ligand-pocket interaction, and assumes a second, different conformation and biological activity in the absence of the ligand-pocket interaction. Next, respective samples of said protein in the first and second conformations are provided, and these are screened against one or more candidate molecules by contacting the molecules and the samples. Thereupon, small molecules which bind with the protein at the region of the pocket may be identified. Novel protein-modulator adducts and methods of altering protein activity are also provided.
摘要翻译：提供了用于合理鉴定能够与特定天然存在的蛋白质相互作用的分子的新方法，以产生新的药理学上重要的化合物和治疗方式。广泛地，该方法包括鉴定形成特定目的蛋白质的一部分的开关控制配体，以及鉴定形成蛋白质的一部分并与所述开关对照配体相互作用的互补开关控制袋。配体在体内与口袋相互作用以调节蛋白质的构象和生物学活性，使得蛋白质在配体 - 口袋相互作用上呈现第一构象和第一生物活性，并且在第二种不同构象和生物学活性中缺乏配体 - 口袋相互作用。接下来，提供第一和第二构象中的所述蛋白质的各个样品，并且通过使分子和样品接触将它们与一种或多种候选分子进行筛选。因此，可以鉴定在口袋区域与蛋白质结合的小分子。还提供了新的蛋白质调节剂加合物和改变蛋白质活性的方法。

145. 发明授权

US4064128A N,[3-(4'-fluorobenzoyl)propyl]-N.sub.2 -(2'-chloro-5'-methylphenoxy)ethyl]p i 失效
标题翻译： N，{8,3-（4 {40-氟苯甲酰基）丙基{9 -N {HD 2 {L - （2 {40-氯-5 {40-甲基苯氧基）乙基{
公开(公告)号：US4064128A
公开(公告)日：1977-12-20
申请号：US683336
申请日：1976-05-05
申请人： Wolfgang Milkowski , Horst Zeugner , Klaus-Wolf VON Eickstedt , Werner Stuhmer
发明人： Wolfgang Milkowski , Horst Zeugner , Klaus-Wolf VON Eickstedt , Werner Stuhmer
IPC分类号： C07D295/10 , C07D295/108
CPC分类号： C07D295/108 , C07D295/10
摘要： N.sub.1 -[3-(4'-fluorobenzoyl)-propyl]-N.sub.2 -[2-(2'-chloro-5'-methylphenoxy)ethyl]-piperazine of the formula ##STR1## or a pharmaceutically acceptable salt thereof. The compounds are sedatives of low toxicity.
摘要翻译： N1- [3-（4'-氟苯甲酰基） - 丙基] -N 2 - [2-（2'-氯-5'-甲基苯氧基）乙基] - 哌嗪或其药学上可接受的盐。这些化合物是低毒的镇静剂。

146. 发明授权

US4029646A Benzyl N,N-hexamethylenethiolcarbamate compounds and herbicidal compositions 失效
标题翻译：苄基N，N-六亚甲基硫代氨基甲酸酯化合物和除草组合物
公开(公告)号：US4029646A
公开(公告)日：1977-06-14
申请号：US114031
申请日：1971-02-09
申请人： Masahiro Aya , Masao Miyamoto , Nobuo Fukazawa , Masaaki Yamagishi
发明人： Masahiro Aya , Masao Miyamoto , Nobuo Fukazawa , Masaaki Yamagishi
IPC分类号： A01N47/16 , C07D295/10 , C07D295/20 , C07D295/21
CPC分类号： C07D295/21 , C07D295/10 , C07D295/20
摘要： Certain thiolcarbamate compounds of the general formula ##STR1## wherein X is alkyl, e.g., lower alkyl, e.g., of from 1 to 4 carbon atoms, lower alkoxy of from, e.g., 1 to 3 carbon atoms, or halogen, e.g., chlorine or bromine, preferably chlorine. When n is greater than 1, the various radicals X may be the same or different, with provisos.R is hydrogen, or methyl; andN is an integer from 0 to 3;Are outstandingly effective herbicides, especially selective herbicides that can be used in rice paddies.
摘要翻译：某些通式为“IMAGE”的硫代氨基甲酸酯化合物，其中X为烷基，例如1至4个碳原子的低级烷基，例如1至3个碳原子的低级烷氧基，或卤素，例如氯或溴，优选氯。当n大于1时，各种基团X可以相同或不同，具有条件。

147. 发明授权

US4005071A P-Chlorobenzyl N,N-hexamethylenethiolcarbamate 失效
标题翻译：对氯苄基N，N-六亚甲基硫代氨基甲酸酯
公开(公告)号：US4005071A
公开(公告)日：1977-01-25
申请号：US568750
申请日：1975-04-16
申请人： Masahiro Aya , Masao Miyamoto , Nobuo Fukazawa , Masaaki Yamagishi
发明人： Masahiro Aya , Masao Miyamoto , Nobuo Fukazawa , Masaaki Yamagishi
IPC分类号： C07D295/10 , C07D295/20
CPC分类号： C07D295/10 , C07D295/20
摘要： Certain novel thiolcarbamate compounds of the general formula ##STR1## wherein X is alkyl, e.g., lower alkyl, e.g., of from 1 to 4 carbon atoms, lower alkoxy of from, e.g., 1 to 3 carbon atoms, or halogen, e.g., chlorine or bromine, preferably chlorine. When n is greater than 1, the various radicals X may be the same or different, with provisos.R is hydrogen, or methyl; andn is an integer from 0 to 3;Are outstandingly effective herbicides, especially selective herbicides that can be used in rice paddies.
摘要翻译：某些具有通式“IMAGE”的新型硫代氨基甲酸酯化合物，其中X为烷基，例如低级烷基，例如1至4个碳原子，例如1至3个碳原子的低级烷氧基或卤素，例如氯或溴，优选氯。当n大于1时，各种基团X可以相同或不同，具有条件。

148. 发明授权

US3980707A Methylamino derivative of 2-ethylindandione-1,3 and the hydrochloride thereof 失效
标题翻译： 2-乙基二氢茚-1,3-二甲基氨基衍生物及其盐酸盐
公开(公告)号：US3980707A
公开(公告)日：1976-09-14
申请号：US362761
申请日：1973-05-22
申请人： Gustav Yanovich Vanags, deceased , Yan-Voldemar Yanovich Ozol , Avgust Karlovich Aren , Skaidrite Karlovna German , by Yan-Voldemar Yanovich Ozol, administrator , by Avgust Karlovich Aren, administrator , by Skaidrite Karlovna German, administrator , by Gunar Gustavovich Vanags, administrator , by Elga Vilgelmovna Vanga, administratrix
发明人： Gustav Yanovich Vanags, deceased , Yan-Voldemar Yanovich Ozol , Avgust Karlovich Aren , Skaidrite Karlovna German , by Yan-Voldemar Yanovich Ozol, administrator , by Avgust Karlovich Aren, administrator , by Skaidrite Karlovna German, administrator , by Gunar Gustavovich Vanags, administrator , by Elga Vilgelmovna Vanga, administratrix
IPC分类号： C07C45/59 , C07C45/63 , C07C49/697 , C07C49/747 , C07D295/10 , C07D295/116 , C07C97/10
CPC分类号： C07D295/116 , C07C45/59 , C07C45/63 , C07C49/697 , C07C49/747 , C07D295/10
摘要： Antiepileptic compounds of the formula: ##EQU1## wherein R is --NHCH.sub.3, --NHC.sub.2 H.sub.5, ##SPC1##and the hydrochlorides thereof.
摘要翻译：具有下式的抗癫痫化合物：COC2H5 ANGLE C ANGLE COR其中R是-NHCH 3，-NHC 2 H 5及其盐酸盐。

149. 发明授权

US3975390A N-methyl substituted piperazino nitrobenzophenones and a process for the preparation thereof 失效
标题翻译： N-甲基取代的哌嗪子基硝基二苯甲酮及其制备方法
公开(公告)号：US3975390A
公开(公告)日：1976-08-17
申请号：US603854
申请日：1975-08-12
申请人： Edit Toth , Jozsef Torley , Eva Palosi , Szaholes Szeberenyi , Laszlo Szporny , Sandor Gorog , Csilla Meszaros
发明人： Edit Toth , Jozsef Torley , Eva Palosi , Szaholes Szeberenyi , Laszlo Szporny , Sandor Gorog , Csilla Meszaros
IPC分类号： C07D295/10 , C07D295/06
CPC分类号： C07D295/10 , Y10S514/916
摘要： New compounds of the general formula (I), ##SPC1##whereinR.sub.1 and R.sub.2 each stand for a saturated or unsaturated, straight-chained or branched alkyl group, an aralkyl group, a saturated or unsaturated cycloalkyl group or an aryl group, orR.sub.1 and R.sub.2 together with the adjacent nitrogen atom may form an optionally substituted heterocyclic group optionally containing a further oxygen or nitrogen hetero atom,But if R.sub.1 stands for methyl, R.sub.2 may only stand for a group other than methyl,Are prepared by reacting a compound of the general formula (II), ##SPC2##wherein X stands for halogen, with a secondary amine of the general formula (III),r.sub.1 --nh--r.sub.2 (iii)wherein R.sub.1 and R.sub.2 each have the same meanings as defined above.The new compounds of the general formula (I), as well as their pharmaceutical acceptable acid addition salts or quaternary ammonium salts are active primarily in the induction of liver microsomal enzyme, but they also possess antipyretic activity.
摘要翻译：通式（I）的新化合物，其中R 1和R 2各自表示饱和或不饱和的直链或支链烷基，芳烷基，饱和或不饱和环烷基或芳基，或R 1和R 2一起相邻的氮原子可以形成任选地含有另外的氧或氮杂原子的任选取代的杂环基团，但是，R 1代表甲基，R 2可以仅代表甲基以外的基团，ARE通过反应通用化合物（II），其中X代表卤素，具有通式（III）的仲胺，R1-NH-R2（III）其中R1和R2各自具有与上述相同的含义。

150. 发明授权

US3912755A Preparation of pharmaceutical intermediates 失效
标题翻译：药物中间体的制备
公开(公告)号：US3912755A
公开(公告)日：1975-10-14
申请号：US43813674
申请日：1974-01-30
申请人： LILLY CO ELI
发明人： BOOHER RICHARD N
IPC分类号： A61K31/40 , C07D295/10 , C07D207/04
CPC分类号： C07D295/10 , A61K31/40
摘要： Alpha -1-1,2-diphenyl(-2-hydroxy-3-methyl-4-substitutedaminobutanes and Beta -dl-1,2-diphenyl-2-hydroxy-3-methyl-4substituted-aminobutanes are converted by treatment with base to dl-1-phenyl-2-methyl-3-substituted-amino-1-propanones, which are intermediates in the preparation of analgesic substances.
摘要翻译：将α-1-1,2-二苯基（-2-羟基-3-甲基-4-取代 - 氨基丁烷和β-1d-1,2-二苯基-2-羟基-3-甲基-4-取代氨基丁烷转化通过用作为制备镇痛物质的中间体的dl-1-苯基-2-甲基-3-取代的氨基-1-丙酮处理碱。

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