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71. 发明申请

US20170107251A1 NOVEL RUTHENIUM COMPLEXES AND THEIR USES IN PROCESSES FOR FORMATION AND/OR HYDROGENATION OF ESTERS, AMIDES AND DERIVATIVES THEREOF 审中-公开
公开(公告)号：US20170107251A1
公开(公告)日：2017-04-20
申请号：US15355082
申请日：2016-11-18
申请人： YEDA RESEARCH AND DEVELOPMENT CO. LTD.
发明人： David MILSTEIN , Ekambaram Balaraman , Chidambaram Gunanathan , Boopathy Gnanaprakasam , Jing Zhang
IPC分类号： C07K5/12 , C07C209/62 , C07D305/06 , C07D307/44 , C07C29/149 , C07D295/027 , C07D207/06 , C07D207/08 , C07D211/12 , C07C231/10 , C07D307/52 , C07D295/185 , C07C67/00 , C07C213/02 , C07C51/00 , C07D309/30 , C07D307/33 , C07D307/83 , C07C67/297 , C07D241/12 , C07B41/02 , C07B43/04 , C07B41/08 , C07B41/12 , C07B43/06 , B01J31/24 , C07C41/26
CPC分类号： C07K5/12 , B01J31/18 , B01J31/189 , B01J31/2404 , B01J31/2409 , B01J31/248 , B01J31/2485 , B01J2231/40 , B01J2231/49 , B01J2231/643 , B01J2231/763 , B01J2531/0244 , B01J2531/821 , C07B41/02 , C07B41/08 , C07B41/12 , C07B43/04 , C07B43/06 , C07C29/136 , C07C29/149 , C07C29/177 , C07C41/16 , C07C41/26 , C07C45/002 , C07C45/006 , C07C51/00 , C07C51/02 , C07C51/23 , C07C51/295 , C07C67/00 , C07C67/03 , C07C67/297 , C07C209/00 , C07C209/62 , C07C213/00 , C07C213/02 , C07C231/02 , C07C231/10 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07D207/06 , C07D207/08 , C07D211/12 , C07D213/38 , C07D241/08 , C07D241/12 , C07D295/023 , C07D295/027 , C07D295/185 , C07D305/06 , C07D307/14 , C07D307/33 , C07D307/44 , C07D307/52 , C07D307/83 , C07D309/30 , C07D487/14 , C07F9/58 , C07F9/65583 , C07F15/0046 , C07F15/0053 , C07K1/00 , C08G69/00 , Y02P20/52 , C07C233/05 , C07C235/06 , C07C233/07 , C07C235/16 , C07C235/14 , C07C235/10 , C07C211/27 , C07C211/07 , C07C211/35 , C07C211/46 , C07C211/10 , C07C215/28 , C07C217/58 , C07C69/14 , C07C69/24 , C07C31/125 , C07C31/12 , C07C49/78 , C07C49/04 , C07C49/10 , C07C49/08 , C07C49/403 , C07C31/205 , C07C31/202 , C07C31/04 , C07C31/08 , C07C33/20 , C07C33/22 , C07C31/1355 , C07C31/10 , C07C43/13 , C07C69/78 , C07C69/75 , C07C53/124 , C07C53/126 , C07C59/125 , C07C57/32 , C07C61/08 , C07C57/30 , C07C65/21 , C07C63/08 , C07C63/06
摘要： The present invention relates to novel Ruthenium complexes and related borohydride complexes, and their use for (1) hydrogenation of amides (including polyamides) to alcohols and amines; (2) preparing amides from alcohols with amines (including preparing polyamides (e.g., polypeptides) by reacting dialcohols and diamines or by polymerization of amino alcohols); (3) hydrogenation of esters to alcohols (including hydrogenation of cyclic esters (lactones), cyclic di-esters (di-lactones) or polyesters); (4) hydrogenation of organic carbonates (including polycarbonates) to alcohols and of carbamates (including polycarbamates) or urea derivatives to alcohols and amines; (5) dehydrogenative coupling of alcohols to esters; (6) hydrogenation of secondary alcohols to ketones; (7) amidation of esters (synthesis of amides from esters and amines); (8) acylation of alcohols using esters; (9) coupling of alcohols with water to form carboxylic acids; and (10) dehydrogenation of beta-amino alcohols to form pyrazines. The present invention further relates to novel uses of certain pyridine Ruthenium complexes.

72. 发明申请

US20170001988A1 PIPERIDINE AND PIPERAZINE DERIVATIVES AND THEIR USE IN TREATING VIRAL INFECTIONS AND CANCER 审中-公开
标题翻译：哌啶和哌嗪衍生物及其在治疗病毒感染和癌症中的应用
公开(公告)号：US20170001988A1
公开(公告)日：2017-01-05
申请号：US15039781
申请日：2014-11-20
申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN
发明人： Tsanyang Jake Liang , Marc Ferrer , Shanshan He , Xin Hu , Zongyi Hu , Juan Jose Marugan , Noel Terrence Southall , Jingbo Xiao , Wei Zheng
IPC分类号： C07D405/10 , A61K31/55 , A61K45/06 , C07D211/58 , A61K31/453 , A61K31/4468 , C07D295/073 , A61K31/495 , C07D213/16 , A61K31/4409 , A61K31/4465 , C07D211/12 , C07D295/03 , C07D211/14 , C07D403/12 , A61K31/496 , C07D243/08
CPC分类号： C07D405/10 , A61K31/4409 , A61K31/4465 , A61K31/4468 , A61K31/453 , A61K31/495 , A61K31/496 , A61K31/55 , A61K45/06 , C07D209/48 , C07D211/12 , C07D211/14 , C07D211/58 , C07D213/16 , C07D243/08 , C07D295/03 , C07D295/073 , C07D295/088 , C07D295/096 , C07D295/185 , C07D403/12
摘要： Disclosed are compounds of formula (I) (formula I), as antiviral agents, antineoplastic agents, pharmaceutical compositions comprising such compounds, and a method of use of these compounds, wherein X and Y are independently CH or N, o is 0, 1 or 2, and E is absent or is (CR13R14)m, NH, or S, F is absent or is (CR15R16)n, C=O, or —SO2—, G is absent or is (CR17 CR18)r, H is absent or is C═O, or —SO2- and R1, Ar1, Ar2 are as defined in the specification. These compounds are antiviral agents and are contemplated in the treatment of viral infections, for example, hepatitis C, or are antineoplastic agents.
摘要翻译：公开了式（I）（式I）的化合物，作为抗病毒剂，抗肿瘤剂，包含这些化合物的药物组合物和这些化合物的使用方法，其中X和Y独立地是CH或N，O是0,1 或（2），E不存在或为（CR 13 R 14）m，NH或S，F不存在或为（CR 15 R 16）n，C = O或-SO 2 - ，G不存在或为（CR 17 CR 18）r ，H不存在或C = O或-SO 2 - ，且R 1，Ar 1，Ar 2如说明书中所定义。这些化合物是抗病毒剂，并且被考虑用于治疗病毒感染，例如丙型肝炎，或是抗肿瘤剂。

73. 发明申请

US20150087841A1 SYNTHESIS OF MSE-FRAMEWORK TYPE MOLECULAR SIEVES 有权
标题翻译： MSE-FRAMEWORK型分子筛的合成
公开(公告)号：US20150087841A1
公开(公告)日：2015-03-26
申请号：US14541777
申请日：2014-11-14
申请人： Simon C. Weston , Karl G. Strohmaier , Hilda B. Vroman
发明人： Simon C. Weston , Karl G. Strohmaier , Hilda B. Vroman
IPC分类号： C07D453/02 , C07D211/12
CPC分类号： C07D453/02 , B01J29/70 , C01B39/04 , C01B39/48 , C07D211/12 , C07D295/037
摘要： A method of synthesizing a crystalline molecular sieve having an MSE framework type comprises crystallizing a reaction mixture comprising a source of water, a source of an oxide of a tetravalent element, Y, selected from at least one of silicon, tin, titanium, vanadium, and germanium, optionally a source of a trivalent element, X, a source of an alkali or alkaline earth metal, M, and a source of organic dications, Q, such as 3-hydroxy-1-(4-(1-methylpiperidin-1-ium-1-yl)butyl)quinuclidin-1-ium, 3-hydroxy-1-(5-(1-methylpiperidin-1-ium-1-yl)pentyl)quinuclidin-1-ium, 1,1′-(butane-1,4-diyl)bis(1-methylpiperidin-1-ium), 1,1′-(pentane-1,5-diyl)bis(1-methylpiperidin-1-ium), 1,1′-(hexane-1,6-diyl)bis(1-methylpiperidin-1-ium), and 1,1′-((3as,6as)-octahydropentalene-2,5-diyl)bis(1-methylpiperidin-1-ium).
摘要翻译：合成具有MSE骨架类型的结晶分子筛的方法包括使包含水源，四价元素的氧化物源Y的反应混合物结晶，Y选自硅，锡，钛，钒，和锗，任选的三价元素的源，X，碱金属或碱土金属的源，M和有机二价元素的Q，例如3-羟基-1-（4-（1-甲基哌啶-4-基）（1-（1-甲基哌啶-1-基）戊基）奎宁环ium，1,1'ium基-1- yl基）丁基）奎宁环ium，3-羟基-1- - （丁烷-1,4-二基）双（1-甲基哌啶-1-基），1,1' - （戊烷-1,5-二基）双（1-甲基哌啶-1-基），1,1' - （己烷-1,6-二基）双（1-甲基哌啶-1-基）和1,1' - （（3as，6as） - 八氢二烯-2,5-二基）双（1-甲基哌啶-1-基） ium）。

74. 发明授权

US08927579B2 Male contraceptive 有权
标题翻译：男性避孕
公开(公告)号：US08927579B2
公开(公告)日：2015-01-06
申请号：US12504287
申请日：2009-07-16
申请人： Nnae-Meka Ikechukwu Amobi , Christopher Smith
发明人： Nnae-Meka Ikechukwu Amobi , Christopher Smith
IPC分类号： A01N43/00 , A61K31/445 , A01N43/64 , A61K31/41 , A01N31/14 , A61K31/075 , A01N33/18 , A01N33/24 , A61K31/04 , C07C211/27 , C07C211/45 , C07C217/16 , C07D207/09 , C07D209/08 , C07D211/12 , C07D211/14 , C07D211/26 , C07D215/06 , C07D215/12 , C07D217/10 , C07D221/04 , C07D279/26 , C07D279/28 , C07D295/03 , C07D401/06 , C07D417/06
CPC分类号： C07C211/27 , C07C211/45 , C07C217/16 , C07C2603/26 , C07D207/09 , C07D209/08 , C07D211/12 , C07D211/14 , C07D211/26 , C07D215/06 , C07D215/12 , C07D217/10 , C07D221/04 , C07D279/26 , C07D279/28 , C07D295/03 , C07D401/06 , C07D417/06
摘要： A compound having formula I. R1, R2, R3 and R4 are independently H or lower alkyl. R5 is aryl, heteroaryl, cycloalkyl, heterocycloalkyl, aryloxy, heteroaryloxy, cycloalkyloxy, heterocycloalkyloxy, arylamino, heteroarylamino, cycloalkylamino, heterocycloalkyl amino, arylthio, heteroarylthio, cycloalkylthio, heterocycloalkylthio, or cyclic olefin, any of which may be substituted or non-substituted; or substituted alkyl, substituted alkyl oxy or substituted alkyl amino wherein the substituent is an aryl, a heteroaryl, a cycloalkyl, a heterocycloalkyl or a cyclic olefin, any of which may be substituted or non-substituted. X is C or N. n and p are independently whole numbers selected from 0, 1 and 2. (CH2)n and (CH2)p may be substituted or non-substituted. Ar1 and Ar2 are independently aryl or heteroaryl groups which may be substituted or non-substituted. Certain specific compounds are excluded.The compounds can be used in a medicament or a method for the reduction or prevention of the emission of sperm, or for the reduction or prevention of transmission of viral agents transmitted in seminal fluid.
摘要翻译：具有式I的化合物.R 1，R 2，R 3和R 4独立地为H或低级烷基。 R5是芳基，杂芳基，环烷基，杂环烷基，芳氧基，杂芳氧基，环烷氧基，杂环烷氧基，芳基氨基，杂芳基氨基，环烷基氨基，杂环烷基氨基，芳硫基，杂芳硫基，环烷硫基，杂环烷硫基或环烯烃，其中任何一个可以是取代或未取代的; 或取代的烷基，取代的烷基氧基或取代的烷基氨基，其中取代基是芳基，杂芳基，环烷基，杂环烷基或环烯烃，其中任何一个可以被取代或未取代。 X是C或N.n，p独立地是选自0,1和2的整数。（CH 2）n和（CH 2）p可以是取代或未取代的。 Ar 1和Ar 2独立地为可被取代或未取代的芳基或杂芳基。排除某些具体化合物。这些化合物可以用于减少或预防精子发射的药物或方法，或用于减少或防止在精液中传播的病毒剂的传播。

75. 发明授权

US08440697B2 Treatment of heart failure 有权
标题翻译：治疗心力衰竭
公开(公告)号：US08440697B2
公开(公告)日：2013-05-14
申请号：US12785077
申请日：2010-05-21
申请人： Houman Ashrafian , Michael P. Frenneaux
发明人： Houman Ashrafian , Michael P. Frenneaux
IPC分类号： A61K31/4458 , C07D211/12 , A61P9/00
CPC分类号： A61K31/4458 , A61K45/06
摘要： The invention relates to perhexiline, or a pharmaceutically acceptable salt thereof, for use in the treatment of HfnEF, as well as to a method of treating HfnEF, which comprises administering to an animal in need thereof an effective amount of perhexiline, or a pharmaceutically acceptable salt thereof, to treat said HFnEF. The invention further relates to a treatment program for treating HFnEF, which involves the co-use or co-administration of perhexiline with one or more other compounds that are advantageous in treating HFnEF or the symptoms thereof.
摘要翻译：本发明涉及用于治疗HfnEF的过己胺或其药学上可接受的盐，以及治疗HfnEF的方法，其包括向有需要的动物施用有效量的己烯胺或药学上可接受的的盐，以治疗所述HFnEF。本发明还涉及用于治疗HFnEF的治疗程序，其涉及使用或共同给予己烯胺与一种或多种有利于治疗HFnEF或其症状的其它化合物。

76. 发明授权

US08247561B2 Preparation of methylpentamethylenediamine and methylpiperidine 有权
标题翻译：甲基五亚甲基二胺和甲基哌啶的制备
公开(公告)号：US08247561B2
公开(公告)日：2012-08-21
申请号：US12934465
申请日：2009-03-13
申请人： Philippe Marion
发明人： Philippe Marion
IPC分类号： C07D211/12 , C07D213/133 , C07C209/48
CPC分类号： C07C209/48 , C07D211/12 , C07D213/08 , C07D213/133 , C07C211/09
摘要： Methyl-2-pentamethylenediamine and methyl-3-piperidine are prepared by hydrogenation of methylglutaronitrile in the presence of a catalyst including cobalt, chromium, and nickel, especially a catalyst based on Raney cobalt doped with nickel and chromium.
摘要翻译：甲基戊二胺和甲基-3-哌啶是通过甲基戊二腈在包括钴，铬和镍的催化剂存在下，特别是基于掺杂有镍和铬的阮内钴的催化剂进行氢化来制备的。

77. 发明申请

US20080275028A1 Modulators or Alpha7 Nicotinic Acetylcholine Receptors and Therapeutic Uses Thereof 审中-公开
标题翻译：调节剂或α7烟碱乙酰胆碱受体及其治疗用途
公开(公告)号：US20080275028A1
公开(公告)日：2008-11-06
申请号：US11632545
申请日：2005-07-19
申请人： Giovanni Gaviraghi , Chiara Ghiron , Hendrik Bothmann , Renza Roncarati , Georg Christian Terstappenn
发明人： Giovanni Gaviraghi , Chiara Ghiron , Hendrik Bothmann , Renza Roncarati , Georg Christian Terstappenn
IPC分类号： A61K31/445 , C07D401/12 , C07D211/12 , C07D295/15 , C07D243/08 , C07D211/60 , C07D409/12 , C07D207/09 , A61P29/00 , A61P25/28 , A61P37/00 , A61P25/00 , A61K31/5375 , A61K31/55 , A61K31/551 , A61K31/496 , A61K31/495 , A61K31/4545
CPC分类号： C07D213/40 , C07D209/08 , C07D209/18 , C07D211/52 , C07D211/60 , C07D213/56 , C07D213/82 , C07D215/38 , C07D217/04 , C07D239/26 , C07D243/08 , C07D295/13 , C07D295/15 , C07D295/185 , C07D319/18 , C07D333/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D409/12
摘要： The present invention relates to compounds with α7 nAChR agonistic activity, processes for their preparation, pharmaceutical compositions containing the same and the use thereof for the treatment of neurological, psychiatric, cognitive, immunological and inflammatory disorders.
摘要翻译：本发明涉及具有α7nAChR激动活性的化合物，其制备方法，含有它们的药物组合物及其用于治疗神经，精神，认知，免疫学和炎症性疾病的用途。

78. 发明授权

US07405298B2 Process for making risperidone and intermediates therefor 失效
标题翻译：制备利培酮及其中间体的方法
公开(公告)号：US07405298B2
公开(公告)日：2008-07-29
申请号：US10705926
申请日：2003-11-13
申请人： Pavel Slanina , Jiri Bartl
发明人： Pavel Slanina , Jiri Bartl
IPC分类号： C07D487/04 , C07D211/12
CPC分类号： C07D471/04 , C07D211/58
摘要： The formation of risperidone is enhanced by the use of enriched Z-isomer oxime intermediate(s) of formula (3) or (7). The oxime(s) can be isomerically enriched by a variety of techniques including the use of the novel acetic acid salt thereof, which affords, inter alia, resolution of the isomers and/or by heat conversion.
摘要翻译：通过使用式（3）或（7）的富集的Z-异构体肟中间体增强了利培酮的形成。肟可以通过各种技术异构富集，包括使用其新颖的乙酸盐，其特别是提供异构体的拆分和/或通过热转化。

79. 发明申请

US20080004259A1 Inhibitors of Checkpoint Kinases 审中-公开
标题翻译：检查点激酶抑制剂
公开(公告)号：US20080004259A1
公开(公告)日：2008-01-03
申请号：US11795189
申请日：2006-02-03
申请人： Kenneth Arrington , Mark Fraley , Robert Garbaccio , Shaei Huang , Craig Lindsley , Justin Steen , Feng Yang
发明人： Kenneth Arrington , Mark Fraley , Robert Garbaccio , Shaei Huang , Craig Lindsley , Justin Steen , Feng Yang
IPC分类号： A61K31/416 , A61K31/41 , A61K31/4192 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/551 , A61P35/00 , C07D211/12 , C07D231/56 , C07D243/08 , C07D249/04 , C07D257/04 , C07D403/14 , C07D413/14
CPC分类号： C07D403/04 , C07D401/14 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D487/04 , C07D487/08 , C07D487/10 , C07D491/10
摘要： The instant invention provides for compounds which comprise substituted indolyl indazoles that inhibit CHK1 activity. The instant compounds provide a novel mechanism of action with unexpected advantageous properties; such unexpected advantageous properties may include increased cellular potency/solubility, greater selectivity, enhanced pharmacokinetic properties, lack of off target activity and so on. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound to a patient in need of treatment of cancer.
摘要翻译：本发明提供了包含抑制CHK1活性的取代的吲哚吲嗪的化合物。本发明化合物提供具有意想不到的有利性质的新颖作用机理; 这种意想不到的有利性质可以包括增加的细胞效能/溶解度，更大的选择性，增强的药代动力学性质，缺乏目标活性等。本发明还提供了包含这种抑制化合物的组合物和通过将该化合物给予需要治疗癌症的患者来抑制CHK1活性的方法。

80. 发明授权

US06943177B2 Cis-2,6-disubstituted piperidines for the treatment of psychostimulant abuse and withdrawal, eating disorders, and central nervous system diseases and pathologies 有权
标题翻译：用于治疗精神兴奋剂滥用和戒断，进食障碍和中枢神经系统疾病和病症的顺式2,6-二取代哌啶
公开(公告)号：US06943177B2
公开(公告)日：2005-09-13
申请号：US10231156
申请日：2002-08-30
申请人： Linda P. Dwoskin , Peter A. Crooks , Marlon D. Jones
发明人： Linda P. Dwoskin , Peter A. Crooks , Marlon D. Jones
IPC分类号： A61K31/445 , C07D211/12 , C07D211/22 , C07D211/32 , C07D211/18 , C07D211/20
CPC分类号： C07D211/32 , A61K31/445 , C07D211/12 , C07D211/22
摘要： Cis-2,6-disubstituted piperdine analogs, or lobeline analogs, having the general formula: are used to treat diseases of the central nervous system, drug abuse and withdrawal therefrom as well as to treating eating disorders.
摘要翻译：具有以下通式的顺式2,6-二取代的哌啶类似物或叶片类似物用于治疗中枢神经系统疾病，药物滥用和从其中撤出以及治疗进食障碍。

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