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1. 发明申请

WO1995031436A1 PROCESS AND DIASTEREOMERIC SALTS USEFUL FOR THE OPTICAL RESOLUTION OF RACEMIC 'alpha'-[4-(1,1-DIMETHYLETHYL)PHENYL]-4-(HYDROXYDIPHENYLMETHYL)-1-PIPERIDINEBUTANOL AND DERIVATIVE COMPOUNDS 审中-公开
标题翻译： 4- [4-（1,1-二甲基乙基）苯基] -4-（羟基二苯基甲基）-1-哌啶丁醇和衍生化合物的光学分解有用的方法和二异辛基钠盐
公开(公告)号：WO1995031436A1
公开(公告)日：1995-11-23
申请号：PCT/US1995004422
申请日：1995-04-10
申请人： MERRELL DOW PHARMACEUTICALS INC. , NAKAMURA, Mitsuo , SHIGA, Masatoshi
发明人： MERRELL DOW PHARMACEUTICALS INC.
IPC分类号： C07D211/22
CPC分类号： C07D211/22 , Y02P20/582
摘要： A process and diastereomeric salts useful for the optical resolution of racemic alpha -[4-(1,1-dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1-piperidinebutanol, 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]- alpha , alpha -dimethylbenzeneacetic acid and lower alkyl 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]- alpha , alpha -dimethylbenzeneacetates. The process comprises placing into solution a chiral resolving agent, either (+)/(-)-di-paratoluoyltartaric acid or (-)/(+)-mandelic acid, in an amount equimolar to a compound corresponding to the desired enantiomer of the above compound, precipitating the resulting diastereomeric salt between the chiral resolving agent and the target enantiomer and separating the enantiomer.
摘要翻译：用于旋光拆分外消旋的α-[4-（1,1-二甲基乙基）苯基] -4-（羟基二苯基甲基）-1-哌啶丁醇，4- [4- [4-（羟基二苯基甲基）-1 - 哌啶基] -1-羟基丁基]-α，α-二甲基苯乙酸和4- [4- [4-（羟基二苯基甲基）-1-哌啶基] -1-羟基丁基]-α，α-二甲基苯乙酸酯的低级烷基酯。该方法包括将溶液中的（+）/（ - ） - 二对甲苯甲酰基酒石酸或（ - ）/（+） - 扁桃酸的手性拆分剂与等同于对应于在手性拆分剂和目标对映异构体之间沉淀所得的非对映异构体盐并分离对映异构体。

2. 发明申请

WO1995021854A1 NOVEL MERCAPTOACETYLAMIDO 1,3,4,5-TETRAHYDRO-BENZO[C]AZEPIN-3-ONE DISULFIDE DERIVATIVES USEFUL AS INHIBITORS OF ENKEPHALINASE AND ACE 审中-公开
标题翻译：新颖的羧甲基纤维素1,3,4,5-四氢苯并[C] AZEPIN-3-ONE DISHFIDE衍生物作为ENKEPHALINASE和ACE的抑制剂有用
公开(公告)号：WO1995021854A1
公开(公告)日：1995-08-17
申请号：PCT/US1995000279
申请日：1995-01-09
申请人： MERRELL DOW PHARMACEUTICALS INC.
发明人： MERRELL DOW PHARMACEUTICALS INC. , FLYNN, Gary, A. , BEIGHT, Douglas, W. , WARSHAWSKY, Alan, M. , MEHDI, Shujaath , FRENCH, John, F. , KEHNE, John, H.
IPC分类号： C07K05/06
CPC分类号： C07K5/06139 , A61K38/00
摘要： The present invention relates to certain novel mercaptoacetylamido 1,3,4,5-tetrahydro-benzo[c]azepin-3-one disulfide derivatives (formula I) useful as inhibitors of enkephalinase and of ACE.
摘要翻译：本发明涉及可用作脑啡肽酶和ACE抑制剂的某些新的巯基乙酰氨基1,3,4,5-四氢 - 苯并[c]氮杂-3-酮二硫化物衍生物（式I）。

3. 发明申请

WO1995009832A1 NOVEL PROCESS FOR PREPARING POLYAMINE DERIVATIVES AND INTERMEDIATES THEREOF 审中-公开
标题翻译：制备聚氨酯衍生物的新方法及其中间体
公开(公告)号：WO1995009832A1
公开(公告)日：1995-04-13
申请号：PCT/US1994010141
申请日：1994-09-12
申请人： MERRELL DOW PHARMACEUTICALS INC.
发明人： MERRELL DOW PHARMACEUTICALS INC. , ANGELL, Paul, T. , MARTIN, John , ANZEVENO, Peter, B.
IPC分类号： C07C209/62
CPC分类号： C07C209/62 , C07C211/14 , C07D239/04
摘要： The present invention provides a novel process for preparing polyamine derivatives and pharmaceutically acceptable salts thereof, which are useful as antineoplastic agents and novel intermediates thereof.
摘要翻译：本发明提供了一种制备多胺衍生物及其药学上可接受的盐的新方法，其可用作抗肿瘤剂及其新型中间体。

4. 发明申请

WO1995008528A1 TRIARYL-ETHYLENE DERIVATIVES FOR USE IN THERAPY 审中-公开
标题翻译：用于治疗的三联乙烯衍生物
公开(公告)号：WO1995008528A1
公开(公告)日：1995-03-30
申请号：PCT/US1994009314
申请日：1994-08-19
申请人： MERRELL DOW PHARMACEUTICALS INC.
发明人： MERRELL DOW PHARMACEUTICALS INC. , MATTHEWS, Donald, P. , BITONTI, Alan, J. , VAN SICKLE, William, A. , KAPLAN, Donald, A.
IPC分类号： C07C217/20
CPC分类号： C07D295/088 , C07C217/20
摘要： The present invention relates to novel triaryl-ethylene derivatives that are useful as anti-neoplastic agents, antiatherosclerotic agents, and hypocholesterolemic agents.
摘要翻译：本发明涉及可用作抗肿瘤剂，抗动脉粥样硬化剂和降血胆固醇剂的新型三芳基 - 乙烯衍生物。

5. 发明申请

WO1995007917A1 5-(1-FLUORO-VINYL)-1H-PYRIMIDINE-2,4-DIONE DERIVATIVES USEFUL AS ANTINEOPLASTIC AGENTS 审中-公开
标题翻译： 5-（1-氟代 - 乙烯基）-1H-嘌呤-2,4-二酮衍生物作为抗原药物有用
公开(公告)号：WO1995007917A1
公开(公告)日：1995-03-23
申请号：PCT/US1994009502
申请日：1994-08-23
申请人： MERRELL DOW PHARMACEUTICALS INC.
发明人： MERRELL DOW PHARMACEUTICALS INC. , McCARTHY, James, R. , MATTHEWS, Donald, P. , SABOL, Jeffrey, S.
IPC分类号： C07H19/06
CPC分类号： C07D239/54 , C07H19/06
摘要： The present invention provides novel 5-(1-fluorovinyl)-1H-pyrimidine-2,4-dione derivatives of formula (I) which are useful as antineoplastic agents by themselves or in conjunctive therapy with the antineoplastic agent 5-fluorouracil. In said formula, R1 and R2 are each independently hydrogen, C1-C4 alkyl, or a phenyl group unsubstituted or substituted with from 1 to 3 substituents, wherein each substituent is selected from the group consisting of C1-C4 alkyl and C1-C4 alkoxy; and R3 is hydrogen, ribose, 2'-deoxyribose or arabinose.
摘要翻译：本发明提供式（I）的新型5-（1-氟乙烯基）-1H-嘧啶-2,4-二酮衍生物，它们自身可用作抗肿瘤剂或与抗肿瘤药物5-氟尿嘧啶联合治疗。在所述式中，R 1和R 2各自独立地为氢，C 1 -C 4烷基或未被取代或被1至3个取代基取代的苯基，其中每个取代基选自C 1 -C 4烷基和C 1 -C 4烷氧基 ; R3是氢，核糖，2'-脱氧核糖或阿拉伯糖。

6. 发明申请

WO1995003304A1 NOVEL 9-N-BICYCLIC NUCLEOSIDE AGENTS USEFUL AS SELECTIVE INHIBITORS OF PROINFLAMMATORY CYTOKINES 审中-公开
标题翻译：新型9-N-BICYCLIC NUCLEOSIDE AGENTS有效用作抗炎细胞因子的选择性抑制剂
公开(公告)号：WO1995003304A1
公开(公告)日：1995-02-02
申请号：PCT/US1994007147
申请日：1994-06-24
申请人： MERRELL DOW PHARMACEUTICALS INC.
发明人： MERRELL DOW PHARMACEUTICALS INC. , BORCHERDING, David, R. , EDWARDS, Carl, K., III , MUNSON, H., Randall, Jr.
IPC分类号： C07D473/00
CPC分类号： C07D473/34
摘要： The present invention relates to novel 9-N-bicyclic nucleoside agents which are useful as selective inhibitors of proinflammatory cytokines.
摘要翻译：本发明涉及可用作促炎细胞因子的选择性抑制剂的新型9-N-双环核苷试剂。

7. 发明申请

WO1994029255A1 AROMATIC ACETYLCHOLINESTERASE INHIBITORS 审中-公开
标题翻译：芳香乙酰胆碱酯酶抑制剂
公开(公告)号：WO1994029255A1
公开(公告)日：1994-12-22
申请号：PCT/US1994004957
申请日：1994-05-05
申请人： MERRELL DOW PHARMACEUTICALS INC. , COLLARD, Jean-Noel , HORNSPERGER, Jean-Marie , SCHIRLIN, Daniel
发明人： MERRELL DOW PHARMACEUTICALS INC.
IPC分类号： C07C49/80
CPC分类号： C07C225/22 , C07C17/35 , C07C17/361 , C07C33/46 , C07C45/45 , C07C45/673 , C07C49/80 , C07C49/82 , C07C49/84 , C07C69/63 , C07C25/02 , C07C25/13
摘要： Compounds of general formula (I), stereoisomers and pharmaceutically acceptable salts thereof, wherein each of Z and Z' are independently H or F; Q is (a), CH(OH), (b); X is H, Br, Cl, F or CF3; Y is H, Br, Cl, F, OH, OR5, OC(O)R4, N3, CN, NO2, SO3H, CO2R4, NH2, NHR9, NR9R'9, C(R6)(R7)(V'R8) or C(O)R7, provided that when both Z and Z' are F, then Y is H or F; V and V' are each independently CH2 or O; R1 is H or CH3; R2, R9 and R'9 are each independently (C1-6)alkyl, or R2 and V-R3 taken together with the carbon atom to which they are attached form a 3-6 membered ring; R3, R6, R7 and R8 are each independently H, (C1-6)alkyl, or (C3-6)cycloalkyl; R4 is H, (C1-10)alkyl, (C0-4)alkylene aryl or (C3-8)cycloalkyl; and R5 is (C1-10)alkyl, benzyl, phenethyl or (C3-6)cycloalkyl, possess anticholinesterase activity and may be used in the treatment of Degenerativa Dementias.
摘要翻译：通式（I）的化合物，其立体异构体和药学上可接受的盐，其中Z和Z'各自独立地为H或F; Q是（a），CH（OH），（b）; X是H，Br，Cl，F或CF 3; Y为H，Br，Cl，F，OH，OR5，OC（O）R4，N3，CN，NO2，SO3H，CO2R4，NH2，NHR9，NR9R'9，C（R6）（R7）（V'R8）或C（O）R7，条件是当Z和Z'均为F时，则Y为H或F; V和V'各自独立地为CH 2或O; R1是H或CH3; R2，R9和R'9各自独立地为（C1-6）烷基，或R2和V-R3与它们所连接的碳原子一起形成3-6元环; R 3，R 6，R 7和R 8各自独立地为H，（C 1-6）烷基或（C 3-6）环烷基; R4是H，（C1-10）烷基，（C0-4）亚烷基芳基或（C3-8）环烷基; 并且R 5是（C 1-10）烷基，苄基，苯乙基或（C 3-6）环烷基）具有抗胆碱酯酶活性并可用于治疗退行性痴呆。

8. 发明申请

WO1994026735A1 SUBSTITUTED PYRROLIDIN-3-YL-ALKYL-PIPERIDINES USEFUL AS TACHYKININ ANTAGONISTS 审中-公开
标题翻译：取代的吡咯烷-3-基-L-鸟苷可用作TACHYKININ ANTAGONISTS
公开(公告)号：WO1994026735A1
公开(公告)日：1994-11-24
申请号：PCT/US1994004498
申请日：1994-04-22
申请人： MERRELL DOW PHARMACEUTICALS INC. , BURKHOLDER, Timothy, P. , LE, Tieu-Binh , KUDLACZ, Elizabeth, M. , MAYNARD, George, D.
发明人： MERRELL DOW PHARMACEUTICALS INC.
IPC分类号： C07D401/06
CPC分类号： C07D401/06 , C07D401/14 , C07D409/14 , C07D471/10
摘要： The present invention relates to substituted pyrrolidinyl-3-yl-alkyl-piperidines, their stereoisomers, and pharmaceutically acceptable salts thereof and processes for preparation of the same. The compounds of the present invention are useful in their pharmacological activities such as tachykinin antagonism, especially substance P and neurokinin A antagonism, and the like. Compounds having the property of tachykinin antagonism are indicated for conditions associated with neurogenic inflammation and other diseases described herein.
摘要翻译：本发明涉及取代的吡咯烷基-3-基 - 烷基 - 哌啶，其立体异构体及其药学上可接受的盐及其制备方法。本发明的化合物可用于其药理活性如速激肽拮抗作用，特别是P物质和神经激肽A拮抗作用等。具有速激肽拮抗作用的化合物适用于与本文所述的神经源性炎症和其他疾病相关的病症。

9. 发明申请

WO1994019008A1 COMBINATIONS OF RETROVIRAL INHIBITORS 审中-公开
标题翻译：复方抑制剂的组合
公开(公告)号：WO1994019008A1
公开(公告)日：1994-09-01
申请号：PCT/US1994000710
申请日：1994-01-18
申请人： MERRELL DOW PHARMACEUTICALS INC. , TYMS, A., Stanley , TAYLOR, Debra, L.
发明人： MERRELL DOW PHARMACEUTICALS INC.
IPC分类号： A61K37/64
CPC分类号： A61K38/55 , A61K31/445 , A61K2300/00
摘要： The combination of castanospermine esters and short peptide analogs can be used for the treatment of retroviral infections. The combination can be used to treat AIDS and ARC and other diseases caused by the retrovirus HIV or other related viruses.
摘要翻译：蓖麻醇酯和短肽类似物的组合可用于治疗逆转录病毒感染。该组合可用于治疗艾滋病和ARC等由逆转录病毒HIV或其他相关病毒引起的疾病。

10. 发明申请

WO1994007905A1 2-SUBSTITUTED ADENOSINES WITH A-2 RECEPTOR AFFINITY 审中-公开
标题翻译：具有A-2受体亲和力的2-取代腺苷
公开(公告)号：WO1994007905A1
公开(公告)日：1994-04-14
申请号：PCT/US1993008269
申请日：1993-09-02
申请人： MERRELL DOW PHARMACEUTICALS INC.
发明人： MERRELL DOW PHARMACEUTICALS INC. , PEET, Norton, P. , BORCHERDING, David, R. , LENTZ, Nelsen, L. , WEINTRAUB, Philip, M.
IPC分类号： C07H19/167
CPC分类号： C07H19/16
摘要： Adenosine analogues which act selectively at adenosine receptors and which act in general as adenosine agonists are disclosed. From (in vitro) studies it is known that specific physiological effects can be distinguished as a result of this selectivity and that adenosine receptor activity (in vitro) correlates with adenosine receptor activity (in vivo). Pharmaceutical preparations of the subject compounds can be prepared on the basis of the selective binding activity of the compounds disclosed herein which will enhance certain physiological effects while minimizing others, such as decreasing blood pressure without decreasing heart rate.
摘要翻译：公开了在腺苷受体上选择性作用并且通常作为腺苷激动剂起作用的腺苷类似物。从（体外）研究可以看出，由于这种选择性，特定的生理作用可以被区分，并且腺苷受体活性（体外）与腺苷受体活性（体内）相关。本发明化合物的药物制剂可以基于本文公开的化合物的选择性结合活性来制备，这将增强某些生理效应，同时使其他方式最小化，例如降低血压而不降低心率。

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