公开(公告)号：US20070032537A1

公开(公告)日：2007-02-08

申请号：US10560332

申请日：2004-06-10

申请人： Graeme Semple ,  Tawfik Gharbaoui ,  Young-Jun Shin ,  Marc Decaire ,  Claudia Averbuj ,  Philip Skinner

发明人： Graeme Semple ,  Tawfik Gharbaoui ,  Young-Jun Shin ,  Marc Decaire ,  Claudia Averbuj ,  Philip Skinner

IPC分类号： A61K31/4152 ,  C07D231/02

CPC分类号： C07D231/14 ,  A61K31/415 ,  A61K45/06 ,  A61K2300/00

摘要： The present invention relates to certain pyrazole carboxylic acid and ester derivatives, and pharmaceutically acceptable salts thereof, which exhibit useful pharmaceutical properties, for example as agonists for the RUP25 receptor. (I) Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the prophylaxis or treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers and the like the substituents are defined in claim 1.

摘要翻译： 本发明涉及表现出有用的药物性质的某些吡唑羧酸和酯衍生物及其药学上可接受的盐，例如作为RUP25受体的激动剂。 （I）本发明还提供含有本发明化合物的药物组合物，以及使用本发明化合物和组合物预防或治疗代谢相关疾病包括血脂异常，动脉粥样硬化，冠心病，胰岛素 抗性，2型糖尿病，综合征等。 此外，本发明还提供本发明化合物与其它活性剂如属于α-葡糖苷酶抑制剂类，醛糖还原酶抑制剂，双胍类，HMG-CoA还原酶抑制剂，角鲨烯合成 抑制剂，贝特类，LDL分解代谢增强剂，血管紧张素转换酶（ACE）抑制剂，胰岛素分泌增强剂等，取代基如权利要求1中所定义。

公开(公告)号：US20080194836A1

公开(公告)日：2008-08-14

申请号：US11883043

申请日：2006-01-25

申请人： Tawfik Gharbaoui ,  Claudia Averbuj ,  Marlony Carlos ,  Edward A. Lally ,  Dipanjan Sengupta ,  John Robert Fritch

发明人： Tawfik Gharbaoui ,  Claudia Averbuj ,  Marlony Carlos ,  Edward A. Lally ,  Dipanjan Sengupta ,  John Robert Fritch

IPC分类号： C07D231/10

CPC分类号： C07D231/16

摘要： The present invention is directed to processes for the preparation of substituted phenylpyrazole ureas of Formula (I) that are useful as 5-HT2A serotonin receptor modulators for the treatment of disease.

摘要翻译： 本发明涉及制备式（I）的取代苯基吡唑脲的方法，其可用作治疗疾病的5-HT 2A 2 5-羟色胺受体调节剂。

公开(公告)号：US06627574B2

公开(公告)日：2003-09-30

申请号：US09870022

申请日：2001-05-31

申请人： Moris Eisen ,  Victoria Volkis ,  Michal Shmulinson ,  Claudia Averbuj ,  Edith Tish

发明人： Moris Eisen ,  Victoria Volkis ,  Michal Shmulinson ,  Claudia Averbuj ,  Edith Tish

IPC分类号： B01J3128

CPC分类号： C08F10/00 ,  C08F4/65912 ,  C08F12/08 ,  C08F110/06 ,  C08F210/06 ,  Y10S526/905 ,  C08F4/659 ,  C08F2500/15 ,  C08F2500/21 ,  C08F212/08 ,  C08F2500/16 ,  C08F210/08 ,  C08F4/64044

摘要： A process for the polymerization of one or more alpha-olefins having at least 3 carbon atoms, which comprises contacting the monomer or monomers in a polar or non-polar solvent under polymerization conditions with a homogeneous catalyst system including (a) a cationic form of a racemic mixture of a chiral octahedral transition metal complex or of a non chiral octahedral transition metal complex, comprising 1, 2 or 3 bidentate chelating ligands and no cyclopentadienyl ligands and having C1, C2, or C3 symmetry; and (b) an anion of a Lewis acid or a Brönsted acid; and adjusting the pressure so as to obtain either a highly stereoregular polymer or copolymer or an elastomer.

公开(公告)号：US07842324B2

公开(公告)日：2010-11-30

申请号：US11455314

申请日：2006-06-15

申请人： Catherine Tachdjian ,  Andrew P. Patron ,  Farid Bakir ,  Claudia Averbuj ,  Chad Priest ,  Sara L. Adamski-Werner ,  Qing Chen ,  Vincent Darmohusodo ,  Marketa Lebl-Rinnova ,  Rachel D. A. Kimmich ,  Xiao-Qing Tang ,  Rhondi Shigemura

发明人： Catherine Tachdjian ,  Andrew P. Patron ,  Farid Bakir ,  Claudia Averbuj ,  Chad Priest ,  Sara L. Adamski-Werner ,  Qing Chen ,  Vincent Darmohusodo ,  Marketa Lebl-Rinnova ,  Rachel D. A. Kimmich ,  Xiao-Qing Tang ,  Rhondi Shigemura

IPC分类号： A23L1/236

CPC分类号： A23L2/39 ,  A23G3/36 ,  A23G9/32 ,  A23L7/122 ,  A23L27/204 ,  A23L27/205 ,  A23L27/30 ,  A23V2002/00 ,  C07C233/11 ,  C07C233/22 ,  C07C235/34 ,  C07C235/78 ,  C07C237/20 ,  C07C255/57 ,  C07C271/22 ,  C07D213/30 ,  C07D213/85 ,  C07D239/26 ,  C07D241/24 ,  C07D307/52 ,  C07D307/54 ,  C07D333/24 ,  A23V2200/16

摘要： The inventions disclosed herein relate to man-made bi-aromatic amide compounds that, when contacted with comestible food or drinks or pharmaceutical compositions at concentrations preferably on the order of about 100 ppm or lower, serve as sweet taste modifiers, sweet flavoring agents, or sweet flavor enhancers, for use in foods, beverages, and other comestible products, or orally administered medicinal products or compositions, optionally in the presence of or in mixtures with conventional flavoring agents such as known natural saccharide sweeteners and previously known artificial sweeteners.

摘要翻译： 本文公开的本发明涉及人造双芳族酰胺化合物，当与可食食品或饮料或药物组合物以优选约100ppm或更低的量级的浓度接触时，可用作甜味调味剂，甜味调味剂或 用于食品，饮料和其他可食用产品的甜味增味剂或任选在常规调味剂如已知天然糖甜味剂和先前已知的人造甜味剂存在下或与之混合的口服药物或组合物。

公开(公告)号：US20070003680A1

公开(公告)日：2007-01-04

申请号：US11455314

申请日：2006-06-15

申请人： Catherine Tachdjian ,  Andrew Patron ,  Farid Bakir ,  Claudia Averbuj ,  Chad Priest ,  Sara Adamski-Werner ,  Qing Chen ,  Vincent Darmohusodo ,  Marketa Lebl-Rinnova ,  Rachel Kimmich ,  Xiao-Qing Tang ,  Rhondi Shigemura

发明人： Catherine Tachdjian ,  Andrew Patron ,  Farid Bakir ,  Claudia Averbuj ,  Chad Priest ,  Sara Adamski-Werner ,  Qing Chen ,  Vincent Darmohusodo ,  Marketa Lebl-Rinnova ,  Rachel Kimmich ,  Xiao-Qing Tang ,  Rhondi Shigemura

IPC分类号： A23L1/236

CPC分类号： A23L2/39 ,  A23G3/36 ,  A23G9/32 ,  A23L7/122 ,  A23L27/204 ,  A23L27/205 ,  A23L27/30 ,  A23V2002/00 ,  C07C233/11 ,  C07C233/22 ,  C07C235/34 ,  C07C235/78 ,  C07C237/20 ,  C07C255/57 ,  C07C271/22 ,  C07D213/30 ,  C07D213/85 ,  C07D239/26 ,  C07D241/24 ,  C07D307/52 ,  C07D307/54 ,  C07D333/24 ,  A23V2200/16

摘要： The inventions disclosed herein relate to man-made bi-aromatic amide compounds that, when contacted with comestible food or drinks or pharmaceutical compositions at concentrations preferably on the order of about 100 ppm or lower, serve as sweet taste modifiers, sweet flavoring agents, or sweet flavor enhancers, for use in foods, beverages, and other comestible products, or orally administered medicinal products or compositions, optionally in the presence of or in mixtures with conventional flavoring agents such as known natural saccharide sweeteners and previously known artificial sweeteners.

摘要翻译： 本文公开的本发明涉及人造双芳族酰胺化合物，当与可食食品或饮料或药物组合物以优选约100ppm或更低的量级的浓度接触时，可用作甜味调味剂，甜味调味剂或 用于食品，饮料和其他可食用产品的甜味增味剂或任选在常规调味剂如已知天然糖甜味剂和先前已知的人造甜味剂存在下或与之混合的口服药物或组合物。

公开(公告)号：US20060167270A1

公开(公告)日：2006-07-27

申请号：US10530902

申请日：2003-10-09

申请人： Graeme Semple ,  Claudia Averbuj ,  Philip Skinner ,  Tawfik Gharbaoui ,  Young-Jun Shin

发明人： Graeme Semple ,  Claudia Averbuj ,  Philip Skinner ,  Tawfik Gharbaoui ,  Young-Jun Shin

IPC分类号： C07D231/08

CPC分类号： C07D231/16 ,  C07D231/14

摘要： The present invention relates to certain pyrazole carboxylic acid derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, as antilipolytic agents and against for the receptor RUP25, wherein: R2 is H, halogen, C1-12 alkyl or C1-12 haloalkyl; and R3 is C3-6 cycloalkyl, C1-12 alkyl, C1-12 haloalkyl, C3-6 cycloalkyl-C1-4-alkylene, aryl-C1-4-alkylene or heteroaryl-C1-4-alkylene, wherein said aryl-C1-4-alkylene and heteroaryl-C1-4-alkylene can be optionally substituted 1 to 5 substituents selected from the substituents listed in the claims. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for pharmaceutical compositions in combination with other active agents, for example, those agents belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers, thiazolidinedione and the like.

摘要翻译： 本发明涉及式（Ia）的某些吡唑羧酸衍生物及其药学上可接受的盐作为抗脂解剂，并且针对受体RUP25，其中：R 2是H，卤素， C 1-12烷基或C 1-12卤代烷基; 且R 3是C 3-6环烷基，C 1-12烷基，C 1-12卤代烷基， C 3-6环烷基-C 1-4亚烷基，芳基-C 1-4 - 亚烷基或杂芳基-C 1 -4亚烷基，其中所述芳基-C 1-4 - 亚烷基和杂芳基-C 1-4 - 亚烷基可以是任选取代的1至5个取代基 选自权利要求中所列的取代基。 本发明还提供含有本发明化合物的药物组合物，以及使用本发明化合物和组合物治疗代谢相关疾病包括血脂异常，动脉粥样硬化，冠心病，胰岛素抵抗，2型糖尿病的方法 ，综合征-X等。 此外，本发明还提供了与其它活性剂（例如属于α-葡糖苷酶抑制剂，醛糖还原酶抑制剂，双胍类，HMG-CoA还原酶抑制剂，角鲨烯合成抑制剂，贝特类）的那些试剂组合的药物组合物 ，LDL分解代谢增强剂，血管紧张素转换酶（ACE）抑制剂，胰岛素分泌增强剂，噻唑烷二酮等。

公开(公告)号：US06653413B1

公开(公告)日：2003-11-25

申请号：US09492033

申请日：2000-01-27

申请人： Moris Eisen ,  Victoria Volkis ,  Michal Shmulinson ,  Claudia Averbuj ,  Edith Tish

发明人： Moris Eisen ,  Victoria Volkis ,  Michal Shmulinson ,  Claudia Averbuj ,  Edith Tish

IPC分类号： C08F400

CPC分类号： C08F10/00 ,  C08F4/65912 ,  C08F12/08 ,  C08F110/06 ,  C08F210/06 ,  Y10S526/905 ,  C08F4/659 ,  C08F2500/15 ,  C08F2500/21 ,  C08F212/08 ,  C08F2500/16 ,  C08F210/08 ,  C08F4/64044

摘要： A process for the polymerization of one or more alpha-olefins having at least 3 carbon atoms, which comprises contacting the monomer or monomers in a polar or non-polar solvent under polymerization conditions with a homogeneous catalyst system including (a) a cationic form of a racemic mixture of a chiral octahedral transition metal complex or of a non chiral octahedral transition metal complex, comprising 1, 2 or 3 bidentate chelating ligands and no cyclopentadienyl ligands and having C1, C2, or C3 symmetry; and (b) an anion of a Lewis acid or a Brönsted acid; and adjusting the pressure so as to obtain either a highly stereoregular polymer or copolymer or an elastomer.

摘要翻译： 聚合具有至少3个碳原子的一种或多种α-烯烃的方法，该方法包括在聚合条件下使单体或单体在极性或非极性溶剂中与均相催化剂体系接触，所述均相催化剂体系包括（a）阳离子形式的 手性八面体过渡金属络合物或非手性八面体过渡金属络合物的外消旋混合物，其包含1,2或3个二齿螯合配体，没有环戊二烯基配体并具有C1，C2或C3对称性; 和（b）路易斯酸或布朗斯台德酸的阴离子; 并调节压力以获得高度立构规整的聚合物或共聚物或弹性体。