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31. 发明申请

WO0230884A3 SULFIDE AND DISULFIDE COMPOUNDS AND COMPOSITIONS FOR CHOLESTEROL MANAGEMENT AND RELATED USES 审中-公开
标题翻译：硫化物和脱水化合物及其组合物用于胆固醇管理及相关用途
公开(公告)号：WO0230884A3
公开(公告)日：2003-09-25
申请号：PCT/US0131869
申请日：2001-10-11
申请人： ESPERION THERAPEUTICS INC
发明人： DASSEUX JEAN-LOUIS H , ONICIU CARMEN DANIELA
IPC分类号： C07D233/76 , A61K31/11 , A61K31/12 , A61K31/185 , A61K31/19 , A61K31/192 , A61K31/194 , A61K31/195 , A61K31/216 , A61K31/222 , A61K31/275 , A61K31/351 , A61K31/365 , A61K31/366 , A61K31/381 , A61K31/382 , A61K31/41 , A61K31/4178 , A61K31/42 , A61K31/422 , A61K31/4365 , A61K31/4743 , A61K31/663 , A61K31/664 , A61K31/675 , A61P1/18 , A61P3/04 , A61P3/06 , A61P3/08 , A61P5/00 , A61P7/02 , A61P9/00 , A61P9/12 , A61P13/12 , A61P15/10 , A61P25/28 , A61P29/00 , A61P31/04 , A61P35/00 , A61P43/00 , C07C323/12 , C07C323/16 , C07C323/19 , C07C323/22 , C07C323/52 , C07C323/56 , C07C323/60 , C07C323/62 , C07C323/66 , C07D233/84 , C07D233/86 , C07D257/04 , C07D261/12 , C07D305/12 , C07D307/33 , C07D309/10 , C07D309/30 , C07D309/40 , C07D333/18 , C07D333/24 , C07D335/02 , C07D519/00 , C07F9/09 , C07F9/24 , C07F9/44 , A61K31/33 , A61K31/66
CPC分类号： C07F9/2408 , A61K31/194 , A61K31/381 , A61K31/382 , A61K31/4178 , A61K31/42 , A61K31/4743 , A61K31/675 , C07C323/12 , C07C323/16 , C07C323/22 , C07C323/52 , C07C323/56 , C07C323/60 , C07C323/66 , C07F9/091 , C07F9/4407
摘要： The present invention relates to novel sulfide and disulfide compounds, compositions comprising sulfide and disulfide compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatits, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
摘要翻译：本发明涉及新型硫化物和二硫化物化合物，包含硫化物和二硫化物的组合物，以及可用于治疗和预防心血管疾病，血脂异常，dysproteinemias和葡萄糖代谢紊乱的方法，包括施用包含醚化合物的组合物。本发明的化合物，组合物和方法还可用于治疗和预防阿尔茨海默病，综合征X，过氧化物酶体增殖物激活受体相关病症，败血病，血栓形成障碍，肥胖，胰腺，高血压，肾脏疾病，癌症，炎症和阳痿。在某些实施方案中，本发明的化合物，组合物和方法可用于与其它治疗剂如降胆固醇和降血糖药物组合治疗。

32. 发明申请

WO03065789A2 N-BIPHENYLMETHYL AMINOCYCLOALKANECARBOXAMIDE DERIVATIVES 审中-公开
标题翻译： N-二苯甲基氨基甲酰氧基甲酰胺衍生物
公开(公告)号：WO03065789A2
公开(公告)日：2003-08-14
申请号：PCT/US0305782
申请日：2003-02-04
申请人： MERCK & CO INC , WOOD MICHAEL R , ANTHONY NEVILLE J , BOCK MARK G , FENG DONG-MEI , KUDUK SCOTT D , SU DAI-SHI , WAI JENNY MIU-CHUN
发明人： WOOD MICHAEL R , ANTHONY NEVILLE J , BOCK MARK G , FENG DONG-MEI , KUDUK SCOTT D , SU DAI-SHI , WAI JENNY MIU-CHUN
IPC分类号： C07D249/08 , A61K31/235 , A61K31/341 , A61K31/343 , A61K31/352 , A61K31/36 , A61K31/381 , A61K31/4035 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/4196 , A61K31/42 , A61K31/421 , A61K31/4245 , A61K31/426 , A61K31/44 , A61K31/4406 , A61K31/498 , A61K31/50 , A61K31/505 , A61P1/02 , A61P19/02 , A61P29/00 , A61P29/02 , A61P43/00 , C07C233/50 , C07C237/24 , C07D209/48 , C07D213/81 , C07D213/82 , C07D213/89 , C07D231/12 , C07D231/14 , C07D233/64 , C07D233/90 , C07D237/24 , C07D239/28 , C07D241/44 , C07D257/04 , C07D261/18 , C07D263/34 , C07D271/06 , C07D271/08 , C07D277/20 , C07D277/56 , C07D307/33 , C07D307/56 , C07D307/68 , C07D309/30 , C07D317/68 , C07D333/24 , C07D333/40 , C07D333/70 , C07D403/12 , C07D413/12
CPC分类号： C07C237/24 , C07C237/22 , C07C2601/02 , C07D209/48 , C07D213/81 , C07D213/82 , C07D231/12 , C07D237/24 , C07D239/28 , C07D241/44 , C07D249/08 , C07D249/10 , C07D257/04 , C07D261/18 , C07D263/34 , C07D271/06 , C07D307/68 , C07D317/68 , C07D333/38 , C07D333/70 , C07D403/12 , C07D413/12
摘要： N-Biphenyl(substituted methyl) aminocycloalkanecarboxamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.
摘要翻译： N-联苯（取代的甲基）氨基环烷甲酰胺衍生物是缓激肽B1拮抗剂或反激动剂，其可用于治疗或预防与缓激肽B1途径相关的疼痛和炎症等症状。

33. 发明申请

WO2003044004A1 METHOD FOR THE PRODUCTION OF A PHENOLIC SUBSTANCE FROM WOOD 审中-公开
标题翻译：从木材生产苯酚物质的方法
公开(公告)号：WO2003044004A1
公开(公告)日：2003-05-30
申请号：PCT/FI2002/000905
申请日：2002-11-15
申请人： HORMOS NUTRACEUTICAL OY LTD , PARHI, Seppo , PUSKA, Mervi , KALAPUDAS, Arja , KORTE, Helena , HUKKA, Petri
发明人： PARHI, Seppo , PUSKA, Mervi , KALAPUDAS, Arja , KORTE, Helena , HUKKA, Petri
IPC分类号： C07D307/33
CPC分类号： C07D307/33
摘要： This invention concerns a method for the production of hydroxymatairesinol or a hydroxymatairesinol complex from wood comprising the steps of a) extracting finely divided wood material with a polar solvent, b) optionally concentrating the extract by separating at least part of the solvent. The invention is characterized by the steps of, c) adding to the extract an agent able to form a complex with hydroxymatairesinol, and, d) precipitating the hydroxymatairesinol complex, and optionally, e) releasing the hydroxymatairesinol from the complex.
摘要翻译：本发明涉及一种从木材生产羟基木蜡醇或羟基木硫醇配合物的方法，包括以下步骤：a）用极性溶剂萃取细碎木材; b）通过分离至少部分溶剂任选地浓缩提取物。本发明的特征在于以下步骤：c）向所述提取物中加入能够与羟基木蜡醇形成络合物的试剂，以及d）沉淀所述羟基木糖醇复合物，以及任选地e）从所述络合物中释放所述羟基木蜡醇。

34. 发明申请

WO03039231A2 COMPOUNDS AND METHODS FOR TREATING TRANSPLANT REJECTION 审中-公开
标题翻译：用于处理运输垃圾的化合物和方法
公开(公告)号：WO03039231A2
公开(公告)日：2003-05-15
申请号：PCT/US0234187
申请日：2002-10-25
申请人： ATHEROGENICS INC , GLASS MITCHELL , EDWARDS DAVID B
发明人： GLASS MITCHELL , EDWARDS DAVID B
IPC分类号： C07D307/33 , A61K31/10 , A61K31/138 , A61K31/165 , A61K31/192 , A61K31/216 , A61K31/223 , A61K31/225 , A61K31/365 , A61K31/66 , A61K31/7004 , A61K31/7034 , A61K45/06 , A61L31/00 , A61P1/04 , A61P3/10 , A61P9/00 , A61P9/04 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/12 , A61P17/02 , A61P19/02 , A61P25/00 , A61P27/02 , A61P27/16 , A61P29/00 , A61P37/06 , A61P37/08 , C07H15/04
CPC分类号： A61K31/138 , A61K31/10 , A61K31/165 , A61K31/192 , A61K31/216 , A61K31/223 , A61K31/225 , A61K31/66 , A61K31/7034 , A61K45/06
摘要： The use of compounds of the formula (I) and pharmaceutically acceptable salts thereof, alone or in combination for the treatment of transplant rejection, wherein the substituents are defined in the application.
摘要翻译：使用式（I）化合物及其药学上可接受的盐单独或组合用于治疗移植排斥反应，其中取代基在本申请中定义。

35. 发明申请

WO0185664A3 COMPOUNDS AND METHODS FOR REGULATING BACTERIAL GROWTH AND PATHOGENESIS 审中-公开
标题翻译：化合物和调节细菌生长和致病的方法
公开(公告)号：WO0185664A3
公开(公告)日：2002-08-08
申请号：PCT/US0115221
申请日：2001-05-10
申请人： UNIV PRINCETON , QUOREX PHARMACEUTICALS INC , UNIV TECHNOLOGIES INT , BASSLER BONNIE L , DAMMEL CAROL S , SCHAUDER STEPHAN , SHOKAT KEVAN , STEIN JEFFREY , SURETTE MICHAEL G
发明人： BASSLER BONNIE L , DAMMEL CAROL S , SCHAUDER STEPHAN , SHOKAT KEVAN , STEIN JEFFREY , SURETTE MICHAEL G
IPC分类号： G01N33/50 , A61K31/00 , A61K31/12 , A61K31/121 , A61K31/122 , A61K31/201 , A61K31/215 , A61K31/34 , A61K31/341 , A61K31/351 , A61K31/357 , A61K31/365 , A61K31/38 , A61K31/381 , A61K31/385 , A61K31/40 , A61K31/42 , A61K31/43 , A61K31/496 , A61K38/00 , A61K39/00 , A61K45/00 , A61K45/06 , A61P31/04 , A61P43/00 , C07C49/395 , C07C49/597 , C07C49/647 , C07C69/145 , C07D215/56 , C07D261/16 , C07D307/12 , C07D307/20 , C07D307/32 , C07D307/33 , C07D307/58 , C07D307/60 , C07D309/10 , C07D317/20 , C07D317/34 , C07D333/32 , C07D499/68 , C07K14/28 , C12N1/20 , C12P7/26 , C12Q1/02 , C12Q1/18 , C12R1/63 , G01N33/15 , A61K319/34 , C12Q1/04
CPC分类号： C12Q1/18 , A61K31/00 , A61K31/34 , A61K31/365 , A61K31/38 , A61K31/385 , A61K31/40 , A61K39/00 , A61K45/06 , C07K14/28 , A61K2300/00
摘要： The invention provides autoinducer-2 analogs that regulate the activity of autoinducer-2 and methods of using such analogs for regulating bacterial growth and pathogenesis.
摘要翻译：本发明提供了调节自体诱导剂-2的活性的自动诱导剂-2类似物和使用这种类似物调节细菌生长和发病机理的方法。

36. 发明申请

WO02057298A2 C-TERMINAL MODIFIED OXAMYL DIPEPTIDES AS INHIBITORS OF THE ICE/CED-3 FAMILY OF CYSTEINE PROTEASES 审中-公开
标题翻译：作为ICE / CED-3家族蛋白家族的抑制剂的C-末端修饰的氧化酶抑制剂
公开(公告)号：WO02057298A2
公开(公告)日：2002-07-25
申请号：PCT/US2002/001538
申请日：2002-01-16
IPC分类号： C07D307/33 , A61K31/341 , A61K38/00 , A61K38/05 , A61P1/04 , A61P1/16 , A61P3/10 , A61P5/14 , A61P7/00 , A61P7/04 , A61P7/06 , A61P9/10 , A61P11/00 , A61P13/12 , A61P17/02 , A61P17/12 , A61P19/02 , A61P21/04 , A61P25/00 , A61P25/16 , A61P25/28 , A61P29/00 , A61P31/04 , A61P31/12 , A61P31/14 , A61P31/16 , A61P31/20 , A61P37/00 , A61P37/02 , A61P43/00 , C07C237/12 , C07C237/22 , C07C317/50 , C07D295/135 , C07D295/185 , C07F9/32 , C07K5/023 , C07K5/06 , C07K5/02 , A61K38/06
CPC分类号： C07D295/185 , C07B2200/07 , C07C237/22 , C07C317/50 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2603/74 , C07D295/135 , C07F9/3264
摘要： This invention is directed to novel oxamyl dipeptide ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as to the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.
摘要翻译：本发明涉及新型牛磺酰二肽ICE / ced-3家族抑制剂化合物。本发明还涉及含有这些化合物的药物组合物，以及这些组合物在治疗患有炎症，自身免疫和神经变性疾病的患者中的用途，用于预防缺血性损伤以及用于保护进行移植手术。

37. 发明申请

WO0198238A3 CATALYTIC HYDROGENATION OF KETONES AND ALDEHYDES 审中-公开
标题翻译：酮和醛的催化氢化
公开(公告)号：WO0198238A3
公开(公告)日：2002-07-25
申请号：PCT/US0119680
申请日：2001-06-20
申请人： DU PONT
发明人： BULLOCK R MORRIS , FAGAN PAUL JOSEPH , HAUPTMAN ELISABETH M , SCHLAF MARCEL
IPC分类号： C07D307/33 , C07B61/00 , C07C1/22 , C07C15/24 , C07C29/141 , C07C29/143 , C07C29/145 , C07C31/10 , C07C31/125 , C07C33/20 , C07C35/20 , C07C67/31 , C07C69/708 , C07D309/30 , C07D315/00 , C07C1/207 , C07D307/32
CPC分类号： C07D315/00 , C07C1/22 , C07C29/141 , C07C29/145 , C07C67/31 , C07C2531/20 , C07C2531/22 , C07C2601/18 , C07C69/708 , C07C15/24 , C07C15/073 , C07C35/20 , C07C33/20 , C07C31/125 , C07C31/10
摘要： Ketones and aldehydes are hydrogenated to the corresponding alcohol of alkyl group, using H2 gas as the stoichiometric reductant, and a ruthenium- or iron-containing catalyst precursor having the formula {[CpM(CO)2]2( mu -H+Q-, wherein M is selected from the group consisting of Ru and Fe; Cp is an optionally substituted cyclopentadienyl group; and Q- is a non-coordinating or weakly coordinating non-reactive anion.
摘要翻译：使用H 2气体作为化学计量还原剂，将酮和醛氢化成相应的烷基醇，具有式{[CpM（CO）2] 2（μ-H + Q- 其中M选自Ru和Fe; Cp是任选取代的环戊二烯基; Q-是非配位或弱配位的非反应性阴离子。

38. 发明申请

WO0218316A3 TWO-STAGE PROCESS FOR THE HYDROGENATION OF MALEIC ACID TO 1,4-BUTANEDIOL 审中-公开
标题翻译：将马来酸氢化成1,4-丁二醇的两阶段方法
公开(公告)号：WO0218316A3
公开(公告)日：2002-06-20
申请号：PCT/US0126765
申请日：2001-08-27
申请人： STANDARD OIL CO
发明人： HEPFER ROBERT P , MILLER CRAIG T , ATTIG THOMAS G , NORENBERG GREGORY A , BUDGE JOHN R
IPC分类号： C07D307/33 , C07B61/00 , C07C29/149 , C07C31/20 , C07C51/36 , C07C55/10
CPC分类号： C07C29/149 , C07C31/207
摘要： In the process for the conversion of maleic acid to gamma-butyrolactone. 1.4-butanediol and/or tetrahydrofuran, a feedstream comprising maleic acid is hydrogenated in a first hydrogenation zone to produce a reaction product comprising succinic acid and unreacted hydrogen which is then supplied to a second hydrogenation zone, where succinic acid is converted to 1,4-butanediol, the temper atures of the feedstream comprising maleic acid and the first hydrogenation zone are controlled such that the temperature of mal eic acid in the feedstream and the first hydrogenation zone does not exceed about 130 DEG C, thereby minimizing the corrosive effects of the maleic acid and prolonging reactor life and improving overall process economics.
摘要翻译：在马来酸转化为γ-丁内酯的过程中。在1,4-丁二醇和/或四氢呋喃中，包含马来酸的原料流在第一氢化区中氢化以产生包含琥珀酸和未反应的氢的反应产物，然后将其供应到第二氢化区，其中琥珀酸转化成1,4 - 丁二醇中，控制包含马来酸和第一加氢区的进料流的温度，使得进料流和第一加氢区中的丙二酸的温度不超过约130℃，由此使马来酸和延长反应器寿命并改善整个过程的经济性。

39. 发明申请

WO02018316A2 TWO-STAGE PROCESS FOR THE HYDROGENATION OF MALEIC ACID TO 1,4-BUTANEDIOL 审中-公开
标题翻译：将马来酸加成1,4-丁二醇的两步法
公开(公告)号：WO02018316A2
公开(公告)日：2002-03-07
申请号：PCT/US2001/026765
申请日：2001-08-27
IPC分类号： C07D307/33 , C07B61/00 , C07C29/149 , C07C31/20 , C07C51/36 , C07C55/10
CPC分类号： C07C29/149 , C07C31/207
摘要： In the process for the conversion of maleic acid to gamma-butyrolactone. 1.4-butanediol and/or tetrahydrofuran, a feedstream comprising maleic acid is hydrogenated in a first hydrogenation zone to produce a reaction product comprising succinic acid and unreacted hydrogen which is then supplied to a second hydrogenation zone, where succinic acid is converted to 1,4-butanediol, the temper atures of the feedstream comprising maleic acid and the first hydrogenation zone are controlled such that the temperature of mal eic acid in the feedstream and the first hydrogenation zone does not exceed about 130 DEG C, thereby minimizing the corrosive effects of the maleic acid and prolonging reactor life and improving overall process economics.
摘要翻译：在马来酸转化为γ-丁内酯的过程中。 1,4-丁二醇和/或四氢呋喃中，将包含马来酸的进料流在第一氢化区中氢化以产生包含琥珀酸和未反应的氢的反应产物，然后将其供应到第二加氢区，其中琥珀酸被转化为1,4 丁二醇，控制包含马来酸和第一氢化区的进料流的回火，使得进料流和第一氢化区中的异戊酸的温度不超过约130℃，从而最小化马来酸和延长反应器寿命，提高整体工艺经济性。

40. 发明申请

WO02010147A1 CONTINUOUS PROCESS FOR THE PRODUCTION OF OPTICALLY PURE (S)- beta -HYDROXY- gamma -BUTYROLACTONE 审中-公开
标题翻译：用于生产光学纯（S）-β-羟基-γ-丁基酮的连续方法
公开(公告)号：WO02010147A1
公开(公告)日：2002-02-07
申请号：PCT/KR2001/000071
申请日：2001-01-17
IPC分类号： C07D307/32 , C07D307/33
CPC分类号： C07D307/33
摘要： Disclosed is a process for the production of optically pure (S)-beta-hydroxy-gamma-butyrolactone through the hydrogenation of substituted carboxylic acid derivatives. A solution containing 1 to 50 % by weight of a substituted carboxylic acid derivative is fed at a WHSV of 0.1 to 10 h , to a fixed bed reactor which is filled with a catalyst and maintained at a reaction temperature of 50 to 550 DEG C under a halogen partial pressure of 15 to 5,500 psig. The catalyst is composed of a noble metal as a catalytically effective ingredient which is impregnated in an inorganic oxide as a support. The molar ratio of the hydrogen to the substituted carboxylic acid derivative is maintained at a molar ratio of 1:1 to 10:1. The process can produce optically pure (S)-beta-hydroxy-gamma-butyrolactone with higher purities at higher yields than can conventional techniques. In addition to being relatively simple and environmentally friendly, the process is so economically favorable as to apply to industrial production.
摘要翻译：公开了通过取代的羧酸衍生物的氢化制备光学纯的（S）-β-羟基-γ-丁内酯的方法。将含有1至50重量％的取代的羧酸衍生物的溶液以0.1至10小时的WHSV加入到固定床反应器中，该反应器填充有催化剂并保持在反应温度为50至 550℃，卤素分压为15-55psig。催化剂由作为载体的无机氧化物中浸渍的催化有效成分的贵金属组成。氢与取代的羧酸衍生物的摩尔比保持在1:1至10:1的摩尔比。该方法可以以比常规技术更高的产率产生具有更高纯度的光学纯（S）-β-羟基-γ-丁内酯。除了相对简单和环保，该工艺在经济上也适用于工业生产。

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