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71. 发明公开

EP3275859A1 GLAUCOCALYXIN A DERIVATIVE AND PREPARATION METHOD AND APPLICATION THEREOF 审中-公开
标题翻译： GLAUCOCALYXIN A衍生物及其制备方法和应用
公开(公告)号：EP3275859A1
公开(公告)日：2018-01-31
申请号：EP15886129.4
申请日：2015-12-17
申请人： Suzhou Pharmavan Cancer Research Center Co., Ltd.
发明人： FENG, Haimei , ZHOU, Rensen , CHEN, Xiang , YU, Yunhui , LIU, Qian , LI, Yong , DENG, Shiping , JIANG, Chuanliang
IPC分类号： C07C225/12 , C07C221/00 , C07C237/30 , C07D295/116 , C07D233/60 , C07D207/00 , C07D473/18 , A61P37/02 , A61P35/00
CPC分类号： C07C225/12 , A61P35/00 , A61P37/00 , C07C221/00 , C07C2603/86 , C07D207/00 , C07D233/60 , C07D295/116 , C07D473/18
摘要： Provided is a glaucocalyxin A derivative, or salt thereof, as represented by the formula (I), a method for preparation of said glaucocalyxin A derivative, and a use for said glaucocalyxin A derivative in preparing pharmaceuticals for fighting autoimmune diseases and tumors, e.g. difficult-to-treat diseases such as systemic lupus erythematosus, psoriasis and triple-negative breast cancer
摘要翻译：本发明提供式（I）所示的glaucocalyxin A衍生物或其盐，该glaococalyxin A衍生物的制备方法，以及该glaococalyxin A衍生物在制备用于抗击自身免疫性疾病和肿瘤的药物中的用途，例如，难治性疾病，如系统性红斑狼疮，牛皮癣和三阴性乳腺癌

72. 发明公开

EP1532101A1 VERFAHREN ZUR HERSTELLUNG VON MONOALKYLAMINOKETONEN 审中-公开
公开(公告)号：EP1532101A1
公开(公告)日：2005-05-25
申请号：EP03790843.1
申请日：2003-08-01
申请人： Merck Patent GmbH
发明人： FABIAN, Kai , NIESERT, Claus-Peter , KRALIK, Joachim , GLÜSENKAMP, Karl-Heinz
IPC分类号： C07C225/12 , C07C221/00 , C07D333/22
CPC分类号： C07D333/22 , C07C225/16
摘要： The invention relates to monoalkylamino ketones of formula (I), wherein R1 and R2 have the meanings as cited in the description.
摘要翻译：本发明涉及式（I）的单烷基氨基酮，其中R 1和R 2具有在说明书中引用的含义。

73. 发明申请

US20180079711A1 GLAUCOCALYXIN A DERIVATIVE AND PREPARATION METHOD AND APPLICATION THEREOF 审中-公开
公开(公告)号：US20180079711A1
公开(公告)日：2018-03-22
申请号：US15561685
申请日：2015-12-17
申请人： SUZHOU PHARMAVAN CANCER RESEARCH CENTER CO., LTD.
发明人： Haimei Feng , Rensen Zhou , Xiang Chen , Yunhui Yu , Qian Liu , Yong Li , Shiping Deng , Chuangliang Jiang
IPC分类号： C07C225/12 , C07C221/00
CPC分类号： C07C225/12 , A61P35/00 , A61P37/00 , C07C221/00 , C07C2603/86 , C07D207/00 , C07D233/60 , C07D295/116 , C07D473/18
摘要： Provided is a glaucocalyxin A derivative, or salt thereof, as represented by the formula (I), a method for preparation of said glaucocalyxin A derivative, and a use for said glaucocalyxin A derivative in preparing pharmaceuticals for fighting autoimmune diseases and tumors, e.g. difficult-to-treat diseases such as systemic lupus erythematosus, psoriasis and triple-negative breast cancer

74. 发明申请

US20110028725A1 Preparation and Use of Alkylating Agents 有权
标题翻译：烷基化剂的制备和应用
公开(公告)号：US20110028725A1
公开(公告)日：2011-02-03
申请号：US12858238
申请日：2010-08-17
申请人： John L. Lim
发明人： John L. Lim
IPC分类号： C07D453/02 , C07C215/40 , C07C317/14 , C07C271/44 , C07D213/02 , C07C225/12 , C07C69/78 , C07C321/16 , G05B21/00
CPC分类号： C07D213/20 , C07B2200/05 , C07C67/10 , C07C213/08 , C07C227/16 , C07C269/06 , C07C319/14 , C07D453/02 , C07C69/78 , C07C69/68 , C07C323/03 , C07C323/58 , C07C215/40 , C07C229/36 , C07C271/34
摘要： The present disclosure provides methods of synthesizing alkylating agents and methods of use.
摘要翻译：本公开提供了合成烷基化剂的方法和使用方法。

75. 发明申请

US20050256318A1 Process for the preparation of n-monosubstituted beta-amino alcohols 审中-公开
标题翻译：制备正单取代的β-氨基醇的方法
公开(公告)号：US20050256318A1
公开(公告)日：2005-11-17
申请号：US10520362
申请日：2003-07-09
申请人： Dominique Michel
发明人： Dominique Michel
IPC分类号： C07D333/58 , C07C213/00 , C07C213/08 , C07C215/08 , C07C221/00 , C07C225/12 , C07C225/16 , C07D307/02 , C07D307/46 , C07D307/52 , C07D333/22
CPC分类号： C07C213/00 , C07C221/00 , C07C225/16 , C07D307/46 , C07D333/22
摘要： A process for the preparation of a compound of formula and/or an addition salt of a proton acid, wherein R1 and R2 independently represent alkyl, cycloalkyl, aryl or aralkyl, each aryl or aralkyl being optionally further substituted with alkyl, alkoxy and/or halogen, which process comprises the following steps: (a) reacting a mixture comprising (i) a methyl ketone of formula wherein R1 is as defined above, and (ii) a compound of formula H2N—R2 (V) and/or an addition salt of proton acid, wherein R2 is as defined above, and (iii) formaldehyde or a source of formaldehyde selected from the group consisting of formaldehyde in aqueous solution, 1,3,5-trioxane, paraformaldehyde and mixtures thereof, in the presence of a solvent selected from the group consisting of water, aliphatic alcohols, cycloaliphatic alcohols and mixtures thereof, and optionally a proton acid to afford a β-amino ketone of formula and/or an addition salt of a proton acid, and (b) reducing the carbonyl group of said β-amino ketone to afford a compound of formula I, and/or an addition salt of a proton acid wherein the first step is carried out at a pressure above 1.5 bar.
摘要翻译：制备式和/或质子酸加成盐的方法，其中R 1和R 2独立地代表烷基，环烷基，芳基或芳烷基每个芳基或芳烷基任选进一步被烷基，烷氧基和/或卤素取代，该方法包括以下步骤：（a）使包含（i）下式的甲酮：其中R 1，如上所定义，和（ii）式<β的化合物在线公式描述=“在线公式”end =“lead”→> H 2 NR < （V）<？in-line-formula description =“In-line Formulas”end =“tail”？>和/或质子酸的加成盐，其中R 2为和（iii）甲醛或甲醛源，其选自甲醛在水溶液中，1,3,5-三恶烷，多聚甲醛及其混合物，在选自水的溶剂存在下，脂族醇，环脂醇和其混合物，以及任选的质子酸，得到式和（或）质子酸的加成盐的β-氨基酮，和（b）还原所述β-氨基酮的羰基，得到式I和/或质子酸的加成盐，其中第一步在高于1.5巴的压力下进行。

76. 发明授权

US06890959B2 Aminomethyl-phenyl-cyclohexanone derivatives 失效
标题翻译：氨基甲基 - 苯基 - 环己酮衍生物
公开(公告)号：US06890959B2
公开(公告)日：2005-05-10
申请号：US10189184
申请日：2002-07-05
申请人： Claudia Puetz , Helmut Buschmann , Babette-Yvonne Koegel
发明人： Claudia Puetz , Helmut Buschmann , Babette-Yvonne Koegel
IPC分类号： C07D319/08 , A61K31/135 , A61P1/04 , A61P1/12 , A61P9/00 , A61P11/04 , A61P11/14 , A61P13/00 , A61P17/00 , A61P23/00 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/24 , A61P25/30 , A61P29/00 , A61P37/08 , C07B61/00 , C07C221/00 , C07C225/00 , C07C225/12 , C07C225/14 , C07C225/18
CPC分类号： C07C225/18 , C07C2601/14
摘要： Aminomethyl-phenyl-cyclohexanone derivatives of formula I or Ia, their diastereomers, enantiomers and salts formed with a physiologically tolerated acid. Also disclosed are processes for preparing the same, pharmaceutical compositions comprising the same, and methods of using the same for the treatment of pain, inflammatory reaction, allergic reactions, depression, drug abuse, alcohol abuse, gastritis, cardiovascular disease, respiratory tract disease, coughing, mental illness, epilepsy, urinary incontinence, itching, and diarrhoea.
摘要翻译：式I或Ia的氨基甲基 - 苯基 - 环己酮衍生物，它们的非对映异构体，对映体和与生理上耐受的酸形成的盐。还公开了其制备方法，包含其的药物组合物及其用途，用于治疗疼痛，炎症反应，过敏反应，抑郁症，药物滥用，酒精滥用，胃炎，心血管疾病，呼吸道疾病，咳嗽，精神疾病，癫痫，尿失禁，瘙痒和腹泻。

77. 发明授权

US5276198A Process for producing 2-methyl-1,3-cyclohexanedione and 2-methylresorcinol 失效
标题翻译： 2-甲基-1,3-环己二酮和2-甲基间苯二酚的制备方法
公开(公告)号：US5276198A
公开(公告)日：1994-01-04
申请号：US933175
申请日：1992-08-21
申请人： Toshio Nakamatsu , Yasuhiro Nishida , Norio Kometani
发明人： Toshio Nakamatsu , Yasuhiro Nishida , Norio Kometani
IPC分类号： B01J23/42 , B01J23/44 , B01J25/02 , C07B61/00 , C07C37/06 , C07C37/07 , C07C39/08 , C07C45/65 , C07C45/67 , C07C49/403 , C07C211/00 , C07C225/12
CPC分类号： C07C211/00 , C07C37/07 , C07C45/673 , C07C2101/14
摘要： A process for producing 2-methyl-1,3-cyclohexanedione which comprises subjecting 1,3-cyclohexanedione, formaldehyde and a dialkylamine to Mannich reaction to obtain a 2-dialkylaminomethyl-1,3-cyclohexanedione, and subjecting the 2-dialkylaminomethyl to hydrogenolysis, and a process for producing 2-methylresorcinol which comprises aromatizing 2-methyl-1,3-cyclohexanedione obtained. According to these processes, it is possible to produce high-purity 2-methylresorcinol and 2-methyl-1,3-cyclohexanedione commercially easily and advantageously.
摘要翻译：一种2-甲基-1,3-环己二酮的制备方法，其包括使1,3-环己二酮，甲醛和二烷基胺进行曼尼希反应，得到2-二烷基氨基甲基-1,3-环己二酮，并使2-二烷基氨基甲基氢解，以及制备2-甲基间苯二酚的方法，其包括使得到的2-甲基-1,3-环己二酮芳构化。根据这些方法，可以容易且有利地生产高纯度2-甲基间苯二酚和2-甲基-1,3-环己二酮。

78. 发明授权

US5180746A Aralkylamine compounds 失效
标题翻译： ARALKYLAMINE化合物
公开(公告)号：US5180746A
公开(公告)日：1993-01-19
申请号：US480564
申请日：1990-02-15
申请人： Giichi Goto , Akinobu Nagaoka , Yuji Ishihara
发明人： Giichi Goto , Akinobu Nagaoka , Yuji Ishihara
IPC分类号： C12N9/99 , A61K31/00 , A61K31/33 , A61K31/357 , A61K31/36 , A61K31/40 , A61P25/00 , A61P25/28 , C07C211/30 , C07C217/58 , C07C217/74 , C07C225/12 , C07C225/18 , C07D295/112 , C07D295/12 , C07D317/70 , C07D521/00
CPC分类号： C07D295/112 , C07C217/74 , C07C225/18 , C07D317/70 , C07C2102/08
摘要： An aralkylamine compound of the formula ##STR1## wherein R.sup.1 means a hydrogen atom or a lower alkyl group; R.sup.2 means an aromatic group which may be substituted; R.sup.3 means a hydrogen atom, a lower alkyl group or an aromatic group which may be substituted; n means an integer of 0 to 7; ring A means a five-through eight-membered cyclic group which may be substituted and may contain one or two hetero atom(s) of O and S atoms as the ring-constituents; and ring B means a benzene ring which may be substituted, or a salt thereof, which is useful as an cholinesterase inhibitor and a cerebral function ameliorating agent.
摘要翻译：式IMA的芳烷基胺化合物，其中R 1表示氢原子或低级烷基; R2表示可以被取代的芳基; R3表示氢原子，低级烷基或可被取代的芳基; n表示0〜7的整数，环A表示可以被取代的五元至八元环基，并且可以含有一个或两个O原子和S原子作为环组成的杂原子; 环B表示作为胆碱酯酶抑制剂和脑功能改善剂有用的可被取代的苯环或其盐。

79. 发明授权

US4435426A Ethers of phenol active on the cardiovascular system, process for preparing same and use thereof in drugs 失效
标题翻译：心血管系统上活性酚的醚，其制备方法及其在药物中的应用
公开(公告)号：US4435426A
公开(公告)日：1984-03-06
申请号：US381796
申请日：1982-05-25
申请人： Henri Demarne , Jean Wagnon
发明人： Henri Demarne , Jean Wagnon
IPC分类号： A61K31/13 , A61K31/135 , A61P9/00 , C07B31/00 , C07B57/00 , C07C45/67 , C07C45/68 , C07C67/00 , C07C213/00 , C07C213/04 , C07C217/32 , C07C217/38 , C07C225/12 , C07C231/00 , C07C231/12 , C07C233/25 , C07C233/33 , C07D303/22 , C07C97/10 , A61K31/165
CPC分类号： C07D303/22 , C07C45/673 , C07C45/68 , Y10S514/821
摘要： The present invention relates to novel products, responding to general formula: ##STR1## in which R.sub.1 and R.sub.2 taken together represent an atom of oxygen .dbd.O or R.sub.1 represents hydrogen and R.sub.2 represents an OH radical, R.sub.3 designates an atom of hydrogen or a straight or branched alkyl radical, or an alkynyl group having from 1 to 6 atoms of carbon, R.sub.4 represents a straight or branched alkyl radical having from 1 to 6 atoms of carbon, R.sub.5 designates an atom of hydrogen, an alkyl group having from 1 to 4 atoms of carbon or an acylamine group and n=3 or 4; as well as to the acid addition salts of said products, to a process for preparing said products and to drugs, particularly active on the cardiovascular system, containing at least one of said products.
摘要翻译：本发明涉及响应以下通式的新产物：其中R 1和R 2一起表示氧原子= O或R 1表示氢，R 2表示OH基团，R 3表示氢原子或具有1至6个碳原子的直链或支链烷基或炔基，R4表示具有1至6个碳原子的直链或支链烷基，R5表示氢原子，具有 1至4个碳原子或酰胺基团，n = 3或4; 以及所述产物的酸加成盐，涉及制备所述产物的方法以及含有至少一种所述产物的在心血管系统上特别活性的药物。

80. 发明授权

US3950420A Cyclohexane derivatives 失效
公开(公告)号：US3950420A
公开(公告)日：1976-04-13
申请号：US490349
申请日：1974-07-22
申请人： Mikio Sawaki , Isao Iwataki , Yoshihiko Hirono , Hisao Ishikawa
发明人： Mikio Sawaki , Isao Iwataki , Yoshihiko Hirono , Hisao Ishikawa
IPC分类号： A01N35/06 , A01N33/24 , A01P13/00 , C07C225/12 , C07D307/52 , C07D333/22 , C07C87/36
CPC分类号： C07D307/52 , C07D333/22
摘要： Various substituted cyclohexane-1,3-diones are useful as herbicides.An exemplary species is 2-[1-(allyloxyamino)propylidene]5,5-dimethylcyclohexane-1,3-dione.

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