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31. 发明申请

WO2012009372A2 TRIAZOLIUM CARBENE CATALYSTS AND PROCESSES FOR ASYMMETRIC CARBON-CARBON BOND FORMATION 审中-公开
标题翻译：三唑碳烯催化剂及不对称碳 - 碳键形成过程
公开(公告)号：WO2012009372A2
公开(公告)日：2012-01-19
申请号：PCT/US2011/043735
申请日：2011-07-12
申请人： COLORADO STATE UNIVERSITY RESEARCH FOUNDATION , ROVIS, Tomislav , DIROCCO, Daniel , GUILES, Joseph
发明人： ROVIS, Tomislav , DIROCCO, Daniel , GUILES, Joseph
IPC分类号： C07D487/04 , C07D207/263 , C07D207/267 , C07D213/55 , C07D241/14
CPC分类号： C07D249/16 , C07D213/46 , C07D237/08 , C07D241/12 , C07D487/04
摘要： Provided herein are chiral triazolium catalysts useful for asymmetric C-C bond formation and processes for their preparation. Also provided are synthetic reactions in which these catalysts are used, in particular, in asymmetric C-C bond formation.
摘要翻译：本文提供了用于不对称C-C键形成的手性三唑鎓催化剂及其制备方法。还提供了使用这些催化剂的合成反应，特别是在不对称C-C键形成中。

32. 发明申请

WO2011088797A1 INTERMEDIATES OF NEUTRAL ENDOPEPTIDASE INHIBITORS AND PREPARATION METHOD THEREOF 审中-公开
标题翻译：中性内切酶抑制剂的中间体及其制备方法
公开(公告)号：WO2011088797A1
公开(公告)日：2011-07-28
申请号：PCT/CN2011/070458
申请日：2011-01-21
申请人： NOVARTIS AG , HOOK, David , ZHOU, Jianguang , LI, Yunzhong , KU, Jie
发明人： HOOK, David , ZHOU, Jianguang , LI, Yunzhong , KU, Jie
IPC分类号： C07D207/277 , C07D207/263 , C07D207/267 , C07D207/26 , C07C229/34 , C07C227/22
CPC分类号： C07C231/10 , C07D207/26 , C07D207/263 , C07D207/267 , C07D207/27 , C07D207/277 , C07D207/38
摘要： Disclosed are intermediates for the manufacture of neutral endopeptidase (NEP) inhibitors or prodrugs thereof, and preparation method thereof. In particular, the said NEP inhibitors comprise a γ-amino-δ-biphenyl-α-methylalkanoic acid, or acid ester, backbone, such as N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.
摘要翻译：公开了用于制备中性内肽酶（NEP）抑制剂或其前药的中间体及其制备方法。特别地，所述NEP抑制剂包括α-氨基 - 联苯-α-甲基链烷酸或酸酯主链，例如N-（3-羧基-1-氧代丙基） - （4S） - （对苯基苯基甲基）-4-氨基 - （2R） - 甲基丁酸乙酯或其盐。

33. 发明申请

WO2009103218A8 亚乙基肼酰胺类衍生物、其制备方法及其在医药上的应用审中-公开
公开(公告)号：WO2009103218A8
公开(公告)日：2009-08-27
申请号：PCT/CN2009/000136
申请日：2009-02-06
申请人：上海恒瑞医药有限公司 , 邓炳初 , 吕贺军 , 陈一千 , 宋鹏 , 王胜蓝
发明人：邓炳初 , 吕贺军 , 陈一千 , 宋鹏 , 王胜蓝
IPC分类号： C07D207/263 , C07D209/14 , C07D231/22 , C07D403/12 , C07C243/38 , C07D257/04 , A61K31/4015 , A61K31/4152 , A61K31/4155 , A61P7/04 , A61P43/00

34. 发明申请

WO2009103218A1 ETHYLIDENE HYDRAZINE CARBOXAMIDE DERIVATIVES, PREPARATION PROCESS AND PHARMACEUTICAL USE THEREOF 审中-公开
标题翻译：乙炔肼羧酰胺衍生物，其制备方法及其药物用途
公开(公告)号：WO2009103218A1
公开(公告)日：2009-08-27
申请号：PCT/CN2009000136
申请日：2009-02-06
申请人： SHANGHAI HENGRUI PHARM CO LTD , TANG PENG CHO , LU HEJUN , CHEN YIQIAN , SONG PENG , WANG SHENGLAN
发明人： TANG PENG CHO , LU HEJUN , CHEN YIQIAN , SONG PENG , WANG SHENGLAN
IPC分类号： C07D207/263 , A61K31/4015 , A61K31/4152 , A61K31/4155 , A61P7/04 , A61P43/00 , C07C243/38 , C07D209/14 , C07D231/22 , C07D257/04 , C07D403/12
CPC分类号： C07D207/263 , C07C335/40 , C07D209/14 , C07D231/22 , C07D257/04 , C07D403/12
摘要： Ethylidene hydrazidecarboxamide derivatives of formula (I) or pharmaceutically acceptable salts, hydrate or solvation thereof, methods for their preparation, pharmaceutical compositions containing the same and their use as a therapeutic agent, especially as thrombopoietin (TPO) mimetics and their use as agonists of thrombopoietin receptor. The definitions of substituents in formula (I) are the same as the description.
摘要翻译：式（I）的亚乙基酰肼甲酰胺衍生物或其药学上可接受的盐，水合物或溶剂化物，其制备方法，含有该化合物的药物组合物及其作为治疗剂的用途，特别是作为血小板生成素（TPO）模拟物及其作为血小板生成素受体。式（I）中取代基的定义与描述相同。

35. 发明申请

WO2009090251A2 NEW PROCESSES 审中-公开
标题翻译：新工艺
公开(公告)号：WO2009090251A2
公开(公告)日：2009-07-23
申请号：PCT/EP2009/050510
申请日：2009-01-16
申请人： NOVARTIS AG , HOOK, David , RISS, Bernhard , KAUFMANN, Daniel , NAPP, Matthias , BAPPERT, Erhard , POLLEUX, Philippe , MEDLOCK, Jonathan , ZANOTTI-GEROSA, Antonio
发明人： HOOK, David , RISS, Bernhard , KAUFMANN, Daniel , NAPP, Matthias , BAPPERT, Erhard , POLLEUX, Philippe , MEDLOCK, Jonathan , ZANOTTI-GEROSA, Antonio
IPC分类号： C07D207/38 , C07D207/263 , C07C269/06 , C07C271/22 , A61K31/4015
CPC分类号： C07D207/38 , C07C271/22 , C07D207/26 , C07D207/263 , C07D207/36 , C07D403/06 , Y02P20/55
摘要： The invention relates to a new process for producing NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a γ-amino-δ-biphenyl-α-methylalkanoic acid, or acid ester, backbone. In detail, the new processes, according to the present invention, are ultimately related to the synthesis of intermediates to prepare the above NEP inhibitors, namely compounds according to formula (1), or salt thereof, wherein R1 and R2 are, independently of each other, hydrogen or a nitrogen protecting group, and R3 is a carboxyl group or an ester group, preferably carboxyl group or alkyl ester.
摘要翻译：本发明涉及用于产生NEP抑制剂或其前药的新方法，特别是包含α-氨基 - 联苯-α-甲基链烷酸或酸酯主链的NEP抑制剂。具体而言，根据本发明的新方法最终与制备上述NEP抑制剂的中间体的合成有关，即根据式（1）的化合物或其盐，其中R 1和R 2各自独立地另一个是氢或氮保护基，R3是羧基或酯基，优选羧基或烷基酯。

36. 发明申请

WO02006224A1 PYRROLIDINE-2-CARBOXYLIC ACID HYDRAZIDE DERIVATIVES FOR USE AS METALLOPROTEASE INHIBITORS 审中-公开
标题翻译：用作金属蛋白酶抑制剂的吡咯烷-2-羧酸氢化物衍生物
公开(公告)号：WO02006224A1
公开(公告)日：2002-01-24
申请号：PCT/EP2001/007995
申请日：2001-07-11
IPC分类号： A61K31/40 , A61K31/401 , A61K31/4025 , A61K31/454 , A61K31/455 , A61K31/4709 , A61K31/501 , A61P3/10 , A61P9/00 , A61P9/04 , A61P9/06 , A61P9/10 , A61P9/12 , A61P11/06 , A61P13/12 , A61P15/00 , A61P17/02 , A61P25/00 , A61P25/06 , A61P27/02 , A61P27/06 , A61P31/04 , A61P35/00 , A61P37/06 , C07D207/16 , C07D207/263 , C07D401/12 , C07D403/06 , C07D405/12 , C07D409/12
CPC分类号： C07D401/12 , C07D207/16 , C07D405/12
摘要： The present invention relates to compounds of formula (I) wherein R , R , R , R , R and X are as defined in the description and the claims and pharmaceutically acceptable esters and/or salts thereof. The compounds are useful as inhibitors of metalloproteases, e.g. zinc proteases, particularly zinc hydrolases, and which are effective in treating disease states are associated with vasoconstriction of increasing occurrences.
摘要翻译：本发明涉及式（I）的化合物，其中R 1，R 2，R 3，R 4，R 5和X如说明书和权利要求和药学上可接受的定义酯和/或其盐。这些化合物可用作金属蛋白酶的抑制剂，例如。锌蛋白酶，特别是锌水解酶，其在治疗疾病状态中有效，与增加事件的血管收缩相关。

37. 发明申请

WO01083444A1 METHOD FOR PRODUCING CYCLIC LACTAMS 审中-公开
标题翻译：用于生产环内酰胺
公开(公告)号：WO01083444A1
公开(公告)日：2001-11-08
申请号：PCT/EP2001/004841
申请日：2001-04-30
IPC分类号： C07D223/10 , C07B61/00 , C07D201/08 , C07D207/263 , C07D211/76 , C07D225/02
CPC分类号： C07D201/08
摘要： The invention relates to a method for producing cyclic lactams of the formula (II), wherein n and m may each represent 0, 1, 2, 3, 4, 5, 6, 7, 8 and 9 and the sum of n + m is at least 3, preferably at least 4, R and R represent C1-C6 alkyl, C5-C7 cycloalkyl or C6-C12 aryl groups, by reacting a compound of the formula (I), wherein R , R , m and n have the meaning indicated above, and R represents nitrile groups, carboxylic acid amide groups and carboxylic acid groups, with water vapor in the gaseous phase. The inventive method is further characterized in that a) the compound (I) is reacted with water vapor in the gaseous phase, adding an organic diluent (III) before or after the reaction, which diluent has a miscibility gap under certain quantitative, pressure and temperature conditions, said reaction resulting in a mixture (IV) that contains a lactam (II), b) adjusting the mixture (IV) before or after the removal of ammonia to quantitative, pressure and temperature conditions under which the diluent (III) and water are present in a liquid form and have a miscibility gap, and obtaining a two-phase system consisting of a phase (V) that has a higher proportion of diluent (III) than water, and a phase (VI) that has a higher proportion of water than diluent (III), c) separating phase (V) from phase (VI) and, d) removing from phase (V) the diluent (III) and optionally by-products selected from the group of the low-boilers, high-boilers and unreacted compound (I), and obtaining a lactam (II).
摘要翻译：一种用于制备式（II），其中n和m的环状内酰胺过程各自为0，1，2，3，4，5，6，7，8和9可以具有和n + m的和至少为3，优选至少4，R <1>和R <2> C 1 -C 6 - 烷基，代表C 5 -C 7环烷基或C 6 -C 12 - 芳基，通过将式（I）化合物进行反应，其中R <1 >，R <2>，m和n是如上，R腈，羧酰胺和羧酸基团的意思是与水蒸汽在气相中通过使作为定义，与在气相中的水蒸汽，其特征在于：a）化合物（I）之前或有机稀释剂（III）的反应之后被添加，含有水在一定的量，压力和温度条件下混溶隙，以得到混合物（IV），其包括内酰胺（II），b）将该混合物（转换后的IV）之前或在数量，压力和温度条件的去除氨之后在其下Verdünnungsm edium（III）和水的液体，并表现出混溶性间隙，得到的两两相体系包括包含稀释剂（III）比水高的比例的相（V），和一个相（VI）含有水的比例较高具有作为稀释剂（III）中，c）相（V）（相VI）被分离出来和d）的相位（V），所述稀释剂（III）和任选的副产物选自低锅炉，高沸点和未反应的Verbindug的组中选择（I）分离，得到内酰胺（II）。

38. 发明申请

WO0039081A3 CELL ADHESION-INHIBITING ANTIINFLAMMATORY AND IMMUNE-SUPPRESSIVE COMPOUNDS 审中-公开
标题翻译：细胞粘附抑制抗炎和免疫抑制化合物
公开(公告)号：WO0039081A3
公开(公告)日：2001-05-25
申请号：PCT/US9931162
申请日：1999-12-29
申请人： ABBOTT LAB
发明人： LINK JAMES , LIU GANG , PEI ZHONGHUA , VON GELDERN TOM , WINN MARTIN , XIN ZHILI , BOYD STEVEN A , JAE HWAN-SOO , LYNCH JOHN K , ZHU GUI-DONG , FREEMAN JENNIFER C , GUNAWARDANA INDRANI W , STAEGER MICHAEL A
IPC分类号： C07D295/12 , A61K31/16 , A61K31/164 , A61K31/165 , A61K31/167 , A61K31/40 , A61K31/4015 , A61K31/404 , A61K31/407 , A61K31/417 , A61K31/438 , A61K31/44 , A61K31/443 , A61K31/445 , A61K31/4465 , A61K31/4468 , A61K31/45 , A61K31/453 , A61K31/454 , A61K31/472 , A61K31/495 , A61K31/496 , A61K31/506 , A61K31/5375 , A61K31/5377 , A61K31/54 , A61K31/541 , A61P29/00 , A61P37/02 , C07C323/00 , C07C323/62 , C07C323/63 , C07D207/08 , C07D207/09 , C07D207/12 , C07D207/14 , C07D207/20 , C07D207/22 , C07D207/26 , C07D207/263 , C07D207/27 , C07D207/273 , C07D207/34 , C07D207/36 , C07D209/08 , C07D209/12 , C07D209/14 , C07D209/18 , C07D211/22 , C07D211/26 , C07D211/42 , C07D211/44 , C07D211/46 , C07D211/54 , C07D211/60 , C07D211/62 , C07D211/66 , C07D211/74 , C07D213/74 , C07D213/75 , C07D213/81 , C07D213/82 , C07D215/04 , C07D215/36 , C07D217/06 , C07D233/61 , C07D235/26 , C07D239/42 , C07D241/04 , C07D241/18 , C07D241/24 , C07D243/08 , C07D265/30 , C07D295/13 , C07D295/16 , C07D295/18 , C07D295/185 , C07D295/205 , C07D295/215 , C07D295/26 , C07D295/32 , C07D307/52 , C07D307/68 , C07D317/58 , C07D317/62 , C07D319/18 , C07D319/20 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D411/04 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/10 , C07D487/08 , C07D491/10 , A61K31/10 , A61K31/33 , C07D295/20
CPC分类号： C07D207/27 , C07C323/62 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D207/09 , C07D207/14 , C07D207/20 , C07D207/22 , C07D207/26 , C07D209/08 , C07D209/18 , C07D211/22 , C07D211/26 , C07D211/42 , C07D211/46 , C07D211/54 , C07D211/60 , C07D211/62 , C07D211/74 , C07D213/74 , C07D213/75 , C07D213/81 , C07D215/36 , C07D217/06 , C07D235/26 , C07D239/42 , C07D241/04 , C07D241/24 , C07D243/08 , C07D265/30 , C07D295/13 , C07D295/185 , C07D295/205 , C07D295/215 , C07D295/26 , C07D295/32 , C07D307/52 , C07D307/68 , C07D317/58 , C07D317/62 , C07D319/18 , C07D319/20 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/04 , C07D413/14 , C07D471/10 , C07D487/08 , C07D491/10
摘要： The present invention relates to novel cinnamide compounds that are useful for treating inflammatory and immune diseases, to pharmaceutical compositions containing these compounds, and to methods of inhibiting inflammation or suppressing immune response in a mammal.
摘要翻译：本发明涉及可用于治疗炎症和免疫疾病的新颖的肉桂酰胺化合物，含有这些化合物的药物组合物，以及抑制哺乳动物炎症或抑制免疫反应的方法。

39. 发明申请

WO00048974A1 STABILISED COMPOSITIONS OF O- AND N-VINYL COMPOUNDS AND THE USE OF AMMONIUM SALTS AS STABILISERS 审中-公开
标题翻译： AS稳定剂O-和N-乙烯基化合物和铵盐使用稳定的组合物
公开(公告)号：WO00048974A1
公开(公告)日：2000-08-24
申请号：PCT/EP2000/000821
申请日：2000-02-02
IPC分类号： C07D233/58 , C07C41/58 , C07C43/16 , C07C43/178 , C07C43/188 , C07D207/26 , C07D207/263 , C07D207/267 , C07D223/10 , C07D233/60 , C07D521/00 , C08F2/00 , C07C41/46
CPC分类号： C07D207/267 , C07D223/10 , C07D231/12 , C07D233/56 , C07D249/08
摘要： The invention relates to a composition of vinyl compounds containing e) at least one polymerisable compound that is provided with at least one O-vinyl group or N-vinyl group and f) at least one ammonium salt of general formula (I) wherein R means NH2, O NH4 , C1-C18-alkyl, C6-C18-cycloalkyl or C7-C18-alkylcycloalkyl. The invention also relates to the use of an ammonium salt of general formula (I) as additive for polymerisable compounds that are provided with at least one O-vinyl group or one N-vinyl group. The invention further relates to a method for preventing premature polymerisation of compositions which contain polymerisable compounds and which are provided with at least one O-vinyl group or one N-vinyl group. According to the inventive method, an ammonium salt of general formula (I) is added to the compositions.
摘要翻译：本发明包括含有e。至少一个可聚合的化合物，其具有至少一个O-乙烯基乙烯基化合物），或一个N-乙烯基团的组合物，和f）通式（Ⅰ）其中R是NH 2，O中的至少一种铵盐< - > NH4 <+>，C1-C18烷基，C6-C18环烷基或C7-C18烷基环烷基的装置。本发明还涉及使用通式（I）作为添加剂的铵盐，以可聚合具有至少一个O形乙烯基或一个N-乙烯基团和用于防止组合物的过早聚合，其包含含有至少可聚合化合物的方法的化合物有一个O形乙烯基或一个N-乙烯基团，其包括将通式（I）的组合物的铵盐的。

40. 发明申请

WO99062506A1 USE OF COMPOUNDS FOR THE ELEVATION OF PYRUVATE DEHYDROGENASE ACTIVITY 审中-公开
标题翻译：化合物用于增加脱氢脱氢酶活性的用途
公开(公告)号：WO99062506A1
公开(公告)日：1999-12-09
申请号：PCT/GB1999/001669
申请日：1999-05-26
IPC分类号： C07D249/12 , A61K31/165 , A61K31/167 , A61K31/18 , A61K31/26 , A61K31/27 , A61K31/341 , A61K31/4015 , A61K31/41 , A61K31/415 , A61K31/4184 , A61K31/42 , A61K31/421 , A61K31/423 , A61K31/4245 , A61K31/426 , A61K31/428 , A61K31/433 , A61K31/44 , A61K31/4409 , A61K31/445 , A61K31/454 , A61K31/495 , A61K31/496 , A61K31/4965 , A61K31/50 , A61K31/505 , A61K31/517 , A61K31/5355 , A61K31/5375 , A61K31/5377 , A61K31/54 , A61K31/541 , A61P3/06 , A61P3/10 , A61P9/04 , A61P9/08 , A61P9/10 , A61P21/00 , A61P25/28 , A61P43/00 , C07C235/16 , C07C317/38 , C07C317/40 , C07C317/42 , C07C317/44 , C07C323/65 , C07D207/08 , C07D207/12 , C07D207/263 , C07D207/48 , C07D211/14 , C07D211/22 , C07D211/42 , C07D211/46 , C07D213/70 , C07D213/71 , C07D213/75 , C07D213/82 , C07D213/89 , C07D231/14 , C07D231/40 , C07D233/84 , C07D233/90 , C07D235/26 , C07D237/20 , C07D239/26 , C07D239/38 , C07D239/42 , C07D239/46 , C07D239/96 , C07D241/20 , C07D257/04 , C07D261/10 , C07D261/14 , C07D263/46 , C07D263/56 , C07D263/58 , C07D271/06 , C07D277/04 , C07D277/20 , C07D277/36 , C07D277/74 , C07D277/76 , C07D285/125 , C07D295/08 , C07D295/096 , C07D295/12 , C07D295/13 , C07D295/14 , C07D295/15 , C07D295/18 , C07D295/192 , C07D295/205 , C07D295/24 , C07D295/26 , C07D307/52
CPC分类号： C07D295/192 , A61K31/167 , C07C235/16 , C07C317/40 , C07C317/42 , C07C317/44 , C07C323/65 , C07D295/096 , C07D295/13 , C07D295/15 , C07D295/205 , C07D295/24 , C07D295/26
摘要： The use of compounds of formula (I), and salts thereof; and pharmaceutically acceptable in vivo cleavable prodrugs of said compound of formula (I); and pharmaceutically acceptable salts of said compound or said prodrugs; in formula (I), Ring C is phenyl or a carbon linked heteroaryl ring substituted as defined within; R is an ortho substituent as defined within; n is 1 or 2; A-B is a linking group as defined within; R and R are as defined within; R is hydroxy, hydrogen, halo, amino or methyl; in the manufacture of a medicament for use in the elevation of PDH activity in warm-blooded animals such as humans is described. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are also described.
摘要翻译：使用式（I）化合物及其盐; 和所述式（I）化合物的药学上可接受的体内可切割前药; 和所述化合物或所述前药的药学上可接受的盐; 在式（I）中，环C是苯基或被定义为碳原子的杂芳基环; R 1是如上所定义的邻位取代基; n为1或2; A-B是定义的连接基团; R 2和R 3如上所定义; R 4是羟基，氢，卤素，氨基或甲基; 在制备用于升高温血动物（例如人）中PDH活性的药物中的用途。还描述了制备式（I）化合物的药物组合物，方法和方法。

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