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41. 发明申请

WO2011045648A3 PROCESS FOR PREPARING (S)-(-)-10-ACETOXY-10,11-DIHYDRO-5H-DIBENZ[B,F]AZEPINE-5-CARBOXAMIDE AND ITS ESTERS THEREOF 审中-公开
标题翻译：制备（S） - （ - ） - 10-乙酰氧基-10,11-二氢-5H-二苯并[b，F]亚胺-5-羧酰胺及其酯的方法
公开(公告)号：WO2011045648A3
公开(公告)日：2011-06-09
申请号：PCT/IB2010002574
申请日：2010-10-11
申请人： MATRIX LAB LTD , HUSAIN MOFAZZAL , DATTA DEBASHISH
发明人： HUSAIN MOFAZZAL , DATTA DEBASHISH
IPC分类号： C07D223/22 , A61K31/55
CPC分类号： C07D223/28
摘要： Disclosed herein an enzymatic process for preparing (S)-(-)-10-acetoxy-10,11- dihydro-5H-dibenz[b,f]azepine-5-carboxamide (eslicarbazepine) and its esters thereof. Further, the invention provides novel intermediates of eslicarbazepine and isomers thereof, enabling high purity and yield of eslicarbazepine.
摘要翻译：本文公开了制备（S） - （ - ） - 10-乙酰氧基-10,11-二氢-5H-二苯并[b，f]吖庚因-5-甲酰胺（西拉西平）及其酯的酶促方法。此外，本发明提供了eslicarbazepine及其异构体的新型中间体，能够实现eslicarbazepine的高纯度和产量。

42. 发明申请

WO2011016648A1 NOVEL ORGANIC ELECTROLUMINESCENT COMPOUNDS AND ORGANIC ELECTROLUMINESCENT DEVICE USING THE SAME 审中-公开
标题翻译：新型有机电致发光化合物和使用该有机电致发光化合物的有机电致发光器件
公开(公告)号：WO2011016648A1
公开(公告)日：2011-02-10
申请号：PCT/KR2010/005017
申请日：2010-07-30
申请人： ROHM AND HAAS ELECTRONIC MATERIALS KOREA LTD. , KIM, Chi Sik , CHO, Young Jun , KWON, Hyuck Joo , KIM, Bong Ok , KIM, Sung Min , YOON, Seung Soo
发明人： KIM, Chi Sik , CHO, Young Jun , KWON, Hyuck Joo , KIM, Bong Ok , KIM, Sung Min , YOON, Seung Soo
IPC分类号： C09K11/06 , C07C13/62 , C07C13/64 , C07C25/22 , C07C211/61 , C07C255/51 , C07C321/30 , C07D209/86 , C07D209/94 , C07D215/06 , C07D223/22 , C07D307/77 , C07D487/04 , C07D495/04 , C07F5/02 , C07F7/08 , C07F9/6568 , H01L51/54
CPC分类号： C07C25/22 , C07C13/62 , C07C211/61 , C07C255/51 , C07C321/30 , C07C2602/10 , C07C2603/18 , C07C2603/54 , C07C2603/74 , C07D209/58 , C07D307/77 , C07D307/91 , C07D401/12 , C07D403/12 , C07D495/04 , C07F5/027 , C07F7/0809 , C07F9/65685 , C09K11/06 , C09K2211/1011 , C09K2211/1029 , C09K2211/1092 , C09K2211/1096 , H01L51/0052 , H01L51/0072 , H01L51/5012 , H05B33/20
摘要： Provided are novel organic electroluminescent compounds and an organic electroluminescent device using the same. Since the organic electroluminescent compound disclosed herein exhibits good luminescent efficiency and excellent life property, it may be used to manufacture OLED devices having very superior operation life.
摘要翻译：提供新颖的有机电致发光化合物和使用其的有机电致发光器件。由于本文公开的有机电致发光化合物表现出良好的发光效率和优异的寿命性质，因此可用于制造具有非常优异的使用寿命的OLED器件。

43. 发明申请

WO2007027719A2 LISOFYLLINE ANALOGS AND METHODS FOR USE 审中-公开
标题翻译： LISOFYLLINE模拟和使用方法
公开(公告)号：WO2007027719A2
公开(公告)日：2007-03-08
申请号：PCT/US2006/033777
申请日：2006-08-29
申请人： UNIVERSITY OF VIRGINIA PATENT FOUNDATION , MACDONALD, Timothy, L. , NADLER, Jerry, L. , CUI, Peng
发明人： MACDONALD, Timothy, L. , NADLER, Jerry, L. , CUI, Peng
IPC分类号： C07D209/08 , C07D209/80 , C07D221/08 , C07D223/22
CPC分类号： A61K31/538 , A61K31/404 , A61K31/405 , A61K31/4196 , A61K31/495 , A61K31/502 , A61K31/53 , C07C215/68 , C07C219/32 , C07D209/08 , C07D209/80 , C07D221/08 , C07D223/22 , C07D241/08 , C07D241/18 , C07D249/12 , C07D253/04 , C07D265/26 , C07D265/36 , C07D265/38 , C07D275/04 , C07D279/22 , C07D487/04
摘要： The present invention provides analogs of a Lysofylline (LSF), and synthetic methods for the preparation of such analogs. The have the active side chain moiety (5-R-hydroxyhexyl) of LSF and can have greater potency and oral bioavailability than LSF.
摘要翻译：本发明提供了类似物溶血素（LSF）的类似物，以及制备这类类似物的合成方法。具有LSF的活性侧链部分（5-R-羟基己基），并且可以具有比LSF更大的效力和口服生物利用度。

44. 发明申请

WO2007012793A1 ASYMMETRIC CATALYTIC REDUCTION OF OXCARBAZEPINE 审中-公开
标题翻译：不对称催化还原氧化腈
公开(公告)号：WO2007012793A1
公开(公告)日：2007-02-01
申请号：PCT/GB2006/001473
申请日：2006-04-21
申请人： PORTELA & C.A., S.A. , LEARMONTH, David, Alexander , GRASA, Gabriela, Alexandra , ZANOTTI-GEROSA, Antonio
发明人： LEARMONTH, David, Alexander , GRASA, Gabriela, Alexandra , ZANOTTI-GEROSA, Antonio
IPC分类号： C07D223/22
CPC分类号： C07D223/28 , A61K31/55 , C07D223/22
摘要： A process for preparing (S)-(+)- 10,11 -dihydro-10-hydroxy-5H- dibenz/b,f/azepine-5-carboxamide or (R)-(-)-10,l l-dihydro-10-hydroxy-5H- dibenz/b,f/azepine-5-carboxamide, by reduction of oxcarbazepine in the presence of a catalyst and a hydride source is disclosed. The catalyst is prepared from a combination of [RuX 2 (L)] 2 wherein X is chlorine, bromine or iodine, and L is an aryl or aryl-aliphatic ligand, with a ligand of formula (A) or formula (B): wherein R 1 is chosen from C 1-6 alkoxy and C 1-6 alkyl, n is a number from 0 to 5, and when n is a number from 2 to 5, R 1 can be the same or different, and R 2 is alkyl, substituted alkyl, aryl, substituted aryl, alkaryl or substituted alkaryl. The hydride source is either NR 3 R 4 R 5 and formic acid, [R 3 R 4 R 5 NH][OOCH] and optionally formic acid, or [M][OOCH] x and formic acid, wherein R 3 , R 4 and R 5 are C 1-6 alkyl, M is an alkali metal or alkaline earth metal and x is 1 or 2. A pH from 6.5 to 8 is maintained during the process.
摘要翻译：制备（S） - （+） - 10,11-二氢-10-羟基-5H-二苯并/ b，f /吖庚因-5-甲酰胺或（R） - （ - ） - 10,11-二氢公开了在催化剂和氢化物源的存在下还原奥卡西平的方法，将10-羟基-5H-二苯并/ b，f /吖庚因-5-甲酰胺。催化剂由[RuX 2（L）] 2 N的组合制备，其中X是氯，溴或碘，L是芳基或芳基 - 脂族配体，与式（A）或式（B）的配位体反应：其中R 1选自C 1-6烷氧基和C 1-6 - >烷基，n是0至5的数，当n是2至5的数时，R 1可以相同或不同，R 2是烷基，取代的烷基，芳基，取代的芳基，烷芳基或取代的烷芳基。氢化物源是NR 3 S 4 R 5和甲酸，[R 3 S 3 R 5] 4 O 5 H] [OOCH]和任选的甲酸或[M] [OOCH] x X和甲酸，其中R 3， R 4，R 4和R 5是C 1-6烷基，M是碱金属或碱土金属，x是1 或2.在该过程中维持6.5至8的pH。

45. 发明申请

WO2006075925A3 METHOD FOR PREPARATION OF 10,11-DIHYDRO-10-HYDROXY-5H-DIBENZ/B,F/AZEPINE-5-CARBOXAMIDE 审中-公开
标题翻译：制备10,11-二氢-10-羟基-5H-二苯并/ B，F /氮杂环庚烯-5-羧酰胺的方法
公开(公告)号：WO2006075925A3
公开(公告)日：2006-08-24
申请号：PCT/PT2006000002
申请日：2006-01-13
申请人： PORTELA & CA SA , LEARMONTH DAVID ALEXANDER , WEINGAERTNER GUENTER , KRAEMER MATTHIAS
发明人： LEARMONTH DAVID ALEXANDER , WEINGAERTNER GUENTER , KRAEMER MATTHIAS
IPC分类号： C07D223/22 , A61K31/55 , C07D491/04
CPC分类号： C07D491/04 , C07D223/22
摘要： A process for the preparation of 10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide (1) by ring opening of 11a,10b-dihydro-6H-dibenz/b,f/oxireno[d]azepine-6-carboxamide (5), characterised in that the ring opening is carried out under conditions of elevated pressure.
摘要翻译：制备10,11-二氢-10-羟基-5H-二苯并[b，f]氮杂-5-甲酰胺（1）的方法，通过11a，10b-二氢-6H-二苯并[b，f] 氧杂环戊二烯并[d]氮杂-6-甲酰胺（5），其特征在于开环在高压条件下进行。

46. 发明申请

WO2006005951A1 METHOD FOR CHIRAL INVERSION OF (S)-(+)- AND (R)-(-)-10,11-DIHYDRO-10-HYDROXY-5H-DIBENZ/B,F/AZEPINE-5-CARBOXAMIDE AND OPTICALLY ENRICHED MIXTURES THEREOF 审中-公开
标题翻译：（S） - （+） - 和（R） - （ - ） - 10,11-二氢-10-羟基-5H-二苯并/ B，F /亚胺-5-羧酰胺及其光学增强混合物的正交反应的方法
公开(公告)号：WO2006005951A1
公开(公告)日：2006-01-19
申请号：PCT/GB2005/002744
申请日：2005-07-13
申请人： PORTELA & C.A. S.A. , LEARMONTH, David, Alexander , WEINGAERTNER, Günter , KRAEMER, Matthias
发明人： LEARMONTH, David, Alexander , WEINGAERTNER, Günter , KRAEMER, Matthias
IPC分类号： C07D223/22
CPC分类号： C07D401/12 , C07B2200/07 , C07D223/22
摘要： A method for chiral inversion of optically pure or optically enriched mixtures of (S)-(+)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide (I) and (R)-(-)-10,11dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide (II) with a carboxylic acid nucleophile in the presence of a trisubstituted phosphine and a disubstituted azodicarboxylate in a substantially inert solvent is disclosed.
摘要翻译：（S） - （+） - 10,11-二氢-10-羟基-5H-二苯并/ b，f /吖庚因-5-甲酰胺（I）和（R）的光学纯的或光学富集的混合物的手性反转的方法） - （ - ） - 10,11-二氢-10-羟基-5H-二苯并/ b，f /吖庚因-5-甲酰胺（II）与羧酸亲核试剂在三取代膦和二取代的偶氮二羧酸酯存在下基本上公开了惰性溶剂。

47. 发明申请

WO2004045533A3 METHOD AND COMPOSITIONS FOR TREATING PERSISTENT PULMONARY HYPERTENSION USING ARALKYL ESTER SOFT DRUGS 审中-公开
标题翻译：使用阿拉伯酵母软膏治疗持续性肺动脉高压的方法和组合物
公开(公告)号：WO2004045533A3
公开(公告)日：2004-07-29
申请号：PCT/US0336686
申请日：2003-11-17
申请人： UNIV TOLEDO
发明人： ERHARDT PAUL W , AOUTHMANY MOUSTAFA M
IPC分类号： C07D499/68 , A61K31/185 , A61K31/195 , A61K31/216 , A61K31/235 , A61K31/24 , A61K31/245 , A61K31/277 , A61K31/401 , A61K31/4025 , A61K31/405 , A61K31/4166 , A61K31/4168 , A61K31/421 , A61K31/426 , A61K31/43 , A61K31/4422 , A61K31/454 , A61K31/46 , A61K31/517 , A61K31/519 , A61K31/522 , A61K31/55 , A61K31/58 , A61K31/65 , A61K31/66 , A61K45/00 , A61K47/48 , A61P9/06 , A61P17/02 , A61P17/06 , A61P25/02 , A61P29/00 , A61P31/10 , A61P35/00 , A61P43/00 , C07C217/40 , C07C219/10 , C07C219/14 , C07C229/60 , C07C237/04 , C07D207/16 , C07D209/26 , C07D209/28 , C07D211/90 , C07D223/22 , C07D233/26 , C07D233/50 , C07D233/76 , C07D261/16 , C07D277/20 , C07D277/56 , C07D295/14 , C07D401/06 , C07D405/12 , C07D451/06 , C07D451/10 , C07D473/06 , C07D475/08 , C07D501/22 , C07J43/00
CPC分类号： C07D209/28 , A61K31/235 , A61K31/24 , C07D211/90 , C07D223/22 , C07D233/50 , C07D233/76 , C07D261/16 , C07D277/56 , C07D401/06 , C07D405/12 , C07D451/06 , C07D473/06 , C07D475/08
摘要： A method and compositions for treating persistent pulmonary hypertension in human newborns that deploys an intravenous infusion of a modified drug formed by adding one or more of a predetermined chemical arrangement to an efficacious parent drug compound so as to retain efficacy while re-directing a preferred route and rate of the parent drug compound's metabolism to an inactive or very weakly active and non-toxic metabolite are disclosed. The chemical arrangement is ϕ-R-X-R'; wherein ϕ is a phenyl, substituted aryl or heteroaryl system that is already present in the parent drug compound or is specifically added to the parent drug compound via a metabolically stable connection; R is an alkyl or alkene containing chain either branched or unbranched from 0 to 10 carbons that is already present in the parent drug compound or is added to the parent drug compound via a metabolically stable connection to ϕ; X is a carboxyl, sulfoxyl or phosphatyl function that is specifically added to the parent drug compound via a metabolically stable connection to R; and, R' is an added alkyl, alkenyl or aralkyl group either branched or 20 unbranched containing from 1 to 10 carbons, or is a structural element already present as an inherent portion of the parent drug compound.
摘要翻译：一种用于治疗人类新生儿持续性肺动脉高压的方法和组合物，其通过将一种或多种预定化学排列添加到有效的母体药物中来部署静脉内输注的修饰药物，以便在重新引导优选途径时保持功效并且公开了母体药物化合物代谢为无活性或非常弱活性和无毒代谢物的速率。化学排列为φ-R-X-R' 其中φ是已经存在于母体药物中的苯基，取代的芳基或杂芳基体系，或通过代谢稳定的连接特异性地添加到母体药物化合物中; R是含有0至10个碳原子的支链或不含支链的烷基或烯烃，其已经存在于母体药物中，或通过与φ的代谢稳定连接加到母体药物中; X是通过与R的代谢稳定连接而特异性地添加到母体药物化合物中的羧基，亚砜基或磷酰基官能团; 并且R'是含有1-10个碳的支链或20个非支链的加成烷基，链烯基或芳烷基，或者是作为母体药物化合物的固有部分已经存在的结构元件。

48. 发明申请

WO02096881A8 METHOD FOR PREPARATION OF 10,11-DIHYDRO-10-HYDROXY-5H-DIBENZ/B,F/AZEPINE-5-CARBOXAMIDE AND 10,11-DIHYDRO-10-0X0-5H-DIBENZ/B,F/AZEPINE-5-CARBOXAMIDE 审中-公开
标题翻译：制备10,11-二氢-10-羟基-5H-二苯并噻吩/ B，F /亚胺-5-羧酰胺和10,11-二氢-10-0X0-5H-二苯并/ B，F / AZEPINE-5- 羧酰胺
公开(公告)号：WO02096881A8
公开(公告)日：2003-02-27
申请号：PCT/GB0202356
申请日：2002-05-22
申请人： PORTELA & CA SA , LEARMONTH DAVID ALEXANDER
发明人： LEARMONTH DAVID ALEXANDER
IPC分类号： A61P25/08 , C07B61/00 , C07D223/22 , C07D491/04 , C07D491/044 , A61K31/55
CPC分类号： C07D491/04 , C07D223/22
摘要： A method for the preparation of 10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide and 10,11-dihydro-10-oxo-5H-dibenz/b,f/azepine-5-carboxamide from carbamazepine via a three-step process involving (i) epoxidation of carbamazepine; (ii) ring-opening of the resulting epoxide and (iii) oxidation of the resulting alcohol.
摘要翻译：制备10,11-二氢-10-羟基-5H-二苯并/ b，f /氮杂-5-甲酰胺和10,11-二氢-10-氧代-5H-二苯并/ b，f /氮杂 - 通过三步法从卡马西平引入5-甲酰胺，其涉及（i）卡马西平的环氧化; （ii）所得环氧化物的开环和（iii）所得醇的氧化。

49. 发明申请

WO0156992A3 DIBENZO (B,F) AZEPINE INTERMEDIATES 审中-公开
标题翻译： DIBENZO（B，F）AZEPINE INTERMEDIATES
公开(公告)号：WO0156992A3
公开(公告)日：2002-01-24
申请号：PCT/EP0101330
申请日：2001-02-07
申请人： NOVARTIS AG , NOVARTIS ERFIND VERWALT GMBH , FUENFSCHILLING PETER , KAUFMANN DANIEL , LOHSE OLIVIER , BEUTLER ULRICH , ZAUGG WERNER
发明人： FUENFSCHILLING PETER , KAUFMANN DANIEL , LOHSE OLIVIER , BEUTLER ULRICH , ZAUGG WERNER
IPC分类号： C07D223/26 , A61K31/55 , A61P25/28 , C07D223/22 , C07D223/28 , C07C237/30 , C07C271/28
CPC分类号： C07D223/22
摘要： The invention relates to new processes for the preparation of the pharmaceutical oxcarbazepine as well as novel intermediates (I), (V), (VI), (VII), (IX) prepared by or used for said processes, and the preparation of said intermediates. R1, R3, R4 = C(1-4) alkyl, R2 = C(1-4) alkyl or phenyl.
摘要翻译：本发明涉及制备奥卡西平药物的新方法以及通过或用于所述方法制备的新型中间体（I），（V），（VI），（VII），（IX）和所述中间体。 R1，R3，R4 = C（1-4）烷基，R2 = C（1-4）烷基或苯基。

50. 发明申请

WO01087299A1 ARALKYL ESTER SOFT DRUGS 审中-公开
标题翻译： ARALKYL ESTER软药
公开(公告)号：WO01087299A1
公开(公告)日：2001-11-22
申请号：PCT/US2001/015146
申请日：2001-05-10
IPC分类号： C07D499/68 , A61K31/185 , A61K31/195 , A61K31/216 , A61K31/235 , A61K31/245 , A61K31/277 , A61K31/401 , A61K31/4025 , A61K31/405 , A61K31/4166 , A61K31/4168 , A61K31/421 , A61K31/426 , A61K31/43 , A61K31/4422 , A61K31/454 , A61K31/46 , A61K31/517 , A61K31/519 , A61K31/522 , A61K31/55 , A61K31/58 , A61K31/65 , A61K31/66 , A61K45/00 , A61K47/48 , A61P9/06 , A61P17/02 , A61P17/06 , A61P25/02 , A61P29/00 , A61P31/10 , A61P35/00 , A61P43/00 , C07C217/40 , C07C219/10 , C07C219/14 , C07C229/60 , C07C237/04 , C07D207/16 , C07D209/26 , C07D209/28 , C07D211/90 , C07D223/22 , C07D233/26 , C07D233/50 , C07D233/76 , C07D261/16 , C07D277/20 , C07D277/56 , C07D295/14 , C07D401/06 , C07D405/12 , C07D451/06 , C07D451/10 , C07D473/06 , C07D475/08 , C07D501/22 , C07J43/00 , A61K31/41 , C07D285/10
CPC分类号： C07D451/06 , A61K9/0048 , A61K31/4164 , A61K31/4166 , A61K45/06 , C07D209/28 , C07D211/90 , C07D223/22 , C07D233/50 , C07D233/76 , C07D261/16 , C07D277/56 , C07D401/06 , C07D405/12 , C07D473/06 , C07D475/08 , A61K2300/00
摘要： The present invention describes a method for programming a specific course and rate of metabolism for a parent drug compound that leads to an inactive or very weakly active and nontoxic metabolite when the modified drug compound is administered. The parent drug compound is modified by forming one or more of a predetermined chemical arrangement within the parent drug structure where the chemical arrangement is A--&phis;--(R)-X-R'; where A is absent or is a tether moiety which allows for a metabolically stable chemical connection to be made to the parent drug compound; &phis; is a substituted aryl or heteroaryl system that is already present within the parent drug compound or is specifically added to the parent drug compound via A; R is an alkyl or alkene containing chain either branched or unbranched from 0 to 10 carbons that is either also already present within the parent drug compound or is specifically added to the parent drug compound via connection to &phis; X is a carboxyl, sulfoxyl or phosphatyl function that is specifically added to the parent drug compound via connection to R; and, R' is an added alkyl, alkenyl, or aralkyl group either branched or unbranched containing from 1 to 10 carbons, other common leaving group, or a structural element already present as an inherent portion of the parent drug compound.
摘要翻译：本发明描述了当施用改性药物化合物时，导致导致非活性或非常弱活性和无毒代谢物的母体药物的特定途径和代谢速率的方法。 - 母体药物化合物通过在母体药物结构内形成预定化学排列中的一种或多种来进行修饰，其中化学排列是A - 和 - （R）-X-R'; 其中A不存在或是能够与母体药物化合物进行代谢稳定的化学连接的系链部分; ＆PHIS; 是已经存在于母体药物中的取代的芳基或杂芳基体系，或通过A特异性地添加到母体药物化合物中; R是含有0至10个碳原子的支链或非支链的烷基或烯烃链，其也已经存在于母体药物化合物中，或者通过连接到＆phi而特异性地添加到母体药物化合物中; X是通过与R连接而特异性地添加到母体药物化合物中的羧基，亚砜基或磷酰基官能团; R'是含有1至10个碳的支链或非支链的烷基，链烯基或芳烷基，其它常用的离去基团或已经作为母体药物化合物的固有部分存在的结构元件。

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