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51. 发明授权

US4824852A Substituted indole compounds which have useful effects on the central nervous system 失效
标题翻译：对中枢神经系统有用的取代吲哚化合物
公开(公告)号：US4824852A
公开(公告)日：1989-04-25
申请号：US153692
申请日：1988-02-08
申请人： Henning Bottcher , Hans-Heinrich Hausberg , Christoph Seyfried , Klaus-Otto Minck
发明人： Henning Bottcher , Hans-Heinrich Hausberg , Christoph Seyfried , Klaus-Otto Minck
IPC分类号： A61K31/435 , A61K31/47 , A61P9/12 , A61P25/00 , A61P25/20 , C07D401/06 , C07D401/12 , C07D491/04 , C07D491/048 , C07D495/04 , C07F7/18 , A61K31/44 , C07D231/02
CPC分类号： C07D401/06 , C07D401/12 , C07D491/04 , C07D495/04
摘要： New indole derivatives of the general formula I ##STR1## in which Ind is a 3-indolyl radical which can be substituted by a hydroxymethyl, methylenedioxy, S-alkyl, SO-alkyl, SO.sub.2 -alkyl, CN or COW group and/or can be substituted once or twice by alkyl, O-alkyl, OH, F, Cl or Br,is H, OH, O-alkyl, NH.sub.2, NH-alkyl or N(alkyl).sub.2,is --(CH.sub.2).sub.n --, --CH.sub.2 --S--CH.sub.2 CH.sub.2 --, --CH.sub.2 --SO--CH.sub.2 CH.sub.2 --or --CH.sub.2 --SO.sub.2 --CH.sub.2 CH.sub.2 --,Z is --(CH.sub.2).sub.m --, --CH.dbd.CH--, --CHOH--, --CO--, S, SO, SO.sub.2 or O,is 2, 3, 4 or 5 andis 1, 2 or 3, in which the alkyl groups each have 1-4 C atoms, and their salts,have effects on the central nervous system.
摘要翻译：其中Ind是可以被羟甲基，亚甲二氧基，S-烷基，SO-烷基，SO 2 - 烷基，CN或COW基团取代的3-吲哚基，和/或可以被烷基，O-烷基，OH，F，Cl或Br取代一次或两次，是H，OH，O-烷基，NH 2，NH-烷基或N（烷基）2是 - （CH 2）n - -CH 2 -S-CH 2 CH 2 - ， - CH 2 -SO 2 -CH 2 CH 2 - 或-CH 2 -SO 2 -CH 2 CH 2 - ，Z是 - （CH 2）m - ， - CH = CH-，-CHOH-，-CO-，S，SO ，SO 2或O 2为2,3,4或5并且为1,2或3，其中烷基各自具有1-4个C原子，并且它们的盐对中枢神经系统具有影响。

52. 发明授权

US4256665A Preparation of .beta.-aminopropionamides 失效
标题翻译： β-氨基丙酰胺的制备
公开(公告)号：US4256665A
公开(公告)日：1981-03-17
申请号：US71530
申请日：1979-08-31
申请人： Edward E. McEntire
发明人： Edward E. McEntire
IPC分类号： C07B61/00 , B01J27/00 , B01J27/20 , C07C20060101 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/14 , C07C237/10 , C07C237/12 , C07D231/02 , C07D231/12 , C07D237/04 , C07D295/00 , C07D295/12 , C07D295/13 , C07C102/06
CPC分类号： C07C231/02
摘要： Covers a process for the preparation of a .beta.-aminopropionamide of the formula ##STR1## wherein R.sub.1 is H or methyl, n is an integer of 2 to 6 and R.sub.2 and R.sub.3, taken singly are hydrogen or lower alkyl groups containing 1 to 4 carbon atoms or R.sub.2 and R.sub.3, taken jointly are combined with the nitrogen atom to form a heterocyclic group selected from the groups consisting of morpholine, pyrrollidine and piperidine ring groups; which process comprises reacting in the presence of carbon dioxide acting as a catalyst a tertiaryaminoalkyl amine of the formula. ##STR2## where R.sub.2, R.sub.3 and n are as above with an acrylic or methacrylic compound of the formula: ##STR3## where R.sub.1 is as above and R.sub.4 is lower alkyl and recovering said .beta.-aminopropionamide.
摘要翻译：包括制备式IMAMA的β-氨基丙酰胺的方法，其中R 1为H或甲基，n为2至6的整数，R 2和R 3为单独为氢或含有1至4个碳的低级烷基原子或R 2和R 3与氮原子一起形成选自吗啉，吡咯烷和哌啶环基团的杂环基; 该方法包括在作为催化剂的二氧化碳存在下使下式的叔氨基烷基胺反应。其中R 2，R 3和n如上述与下式的丙烯酸或甲基丙烯酸化合物：其中R1如上所述，R4是低级烷基并回收所述β-氨基丙酰胺。

53. 发明授权

US11478438B2 Necrosis inhibitors 有权
公开(公告)号：US11478438B2
公开(公告)日：2022-10-25
申请号：US16787052
申请日：2020-02-11
申请人： National Institute of Biological Sciences, Beijing
发明人： Zhiyuan Zhang , Xiaodong Wang , Yaning Su , Hanying Ruan , Yan Ren
IPC分类号： A61K31/165 , A61K31/10 , A61K31/167 , C07C233/01 , C07C235/38 , C07D231/02 , C07D263/04 , C07D205/04 , C07D265/30 , C07D207/12 , C07D211/70 , C07D231/04 , C07D231/08 , C07D233/38 , C07D405/04 , C07D409/04 , C07D241/04 , C07D417/04 , C07D261/02 , C07D263/22 , C07D203/18 , C07D205/08 , C07D207/06 , C07D207/08 , C07D207/20 , C07D207/24 , C07D207/27 , C07D207/333 , C07D211/16 , C07D211/82 , G01C19/5649 , G01C19/5747
摘要： The invention provides amides that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrates and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.

54. 发明授权

US10736899B2 Animal and human anti-malarial agents 有权
公开(公告)号：US10736899B2
公开(公告)日：2020-08-11
申请号：US16540248
申请日：2019-08-14
申请人： Celgene Corporation
发明人： Stacie S. Canan , Natalie Anne Hawryluk
IPC分类号： A61K31/52 , C07C211/36 , C07C13/06 , C07C217/02 , C07D473/32 , C07D231/02 , G01N33/569
摘要： Provided herein are Purine Compounds of Formula (I) or pharmaceutically acceptable salts, tautomers, isotopologues, or stereoisomers thereof, wherein R1, R2, and R3 are as defined herein, compositions comprising an effective amount of a Purine Compound, and methods for treating or preventing malaria comprising the administration of an effective amount of a Purine Compound.

55. 发明授权

US10555920B2 Necrosis inhibitors 有权
公开(公告)号：US10555920B2
公开(公告)日：2020-02-11
申请号：US16153706
申请日：2018-10-06
申请人： National Institute of Biological Sciences, Beijing
发明人： Zhiyuan Zhang , Xiaodong Wang , Yaning Su , Hanying Ruan , Yan Ren
IPC分类号： A61K31/10 , A61K31/165 , A61K31/167 , C07D263/04 , C07D265/30 , C07D207/12 , C07D211/70 , C07D231/04 , C07D231/08 , C07D233/38 , C07D405/04 , C07D409/04 , C07D241/04 , C07D417/04 , C07D261/02 , C07D263/22 , C07D203/18 , C07D205/08 , C07D207/06 , C07D207/08 , C07D207/20 , C07D207/24 , C07D207/27 , C07D207/333 , C07D211/16 , C07D211/82 , C07D231/02 , C07C233/01 , C07C235/38 , C07D205/04
摘要： The invention provides amides that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrates and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.

56. 发明申请

US20170304237A1 Necrosis Inhibitors 审中-公开
公开(公告)号：US20170304237A1
公开(公告)日：2017-10-26
申请号：US15632422
申请日：2017-06-26
申请人： National Institute of Biological Sciences, Beijing
发明人： Zhiyuan Zhang , Xiaodong Wang , Yaning Su , Hanying Ruan , Yan Ren
IPC分类号： A61K31/165 , C07D231/02 , C07C235/38 , A61K31/10 , C07C233/01 , A61K31/167 , C07D241/04 , C07D205/08
CPC分类号： A61K31/165 , A61K31/10 , A61K31/167 , C07C233/01 , C07C235/38 , C07D203/18 , C07D205/04 , C07D205/08 , C07D207/06 , C07D207/08 , C07D207/12 , C07D207/20 , C07D207/24 , C07D207/27 , C07D207/333 , C07D211/16 , C07D211/70 , C07D211/82 , C07D231/02 , C07D231/04 , C07D231/08 , C07D233/38 , C07D241/04 , C07D261/02 , C07D263/04 , C07D263/22 , C07D265/30 , C07D405/04 , C07D409/04 , C07D417/04
摘要： The invention provides amides that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.

57. 发明授权

US08921360B2 Heterobicycle-substituted azolyl benzene fungicides 有权
标题翻译：异环取代的唑基苯类杀真菌剂
公开(公告)号：US08921360B2
公开(公告)日：2014-12-30
申请号：US13500928
申请日：2010-10-12
申请人： John Lawrence Andreassi, II , Andrew Edmund Taggi
发明人： John Lawrence Andreassi, II , Andrew Edmund Taggi
IPC分类号： A01N43/50 , A01N43/647 , A01N43/32 , C07D265/36 , C07D231/02 , C07D405/04 , A01N43/56 , A01N47/18 , A01N47/28
CPC分类号： C07D405/04 , A01N43/56 , A01N47/18 , A01N47/28
摘要： Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein Y is a 5-membered, fully or partially unsaturated heterocyclic ring containing 2-4 carbon atoms and 2-3 nitrogen atoms as ring members, the ring substituted with Z on a ring member atom connected through an adjacent single ring member atom to the ring member atom attaching the heterocyclic ring to the phenyl ring of Formula 1, and optionally further substituted with up to 2 substituents independently selected from R5 on carbon atom ring members and from R6 on nitrogen atom ring members; Z is an 8-, 9-, 10- or 11-membered fused heterobicyclic ring system containing ring members selected from carbon atoms and 1 to 4 heteroatoms independently selected from up to 2 O, up to 2 S and up to 4 N atoms, wherein up to 3 carbon atom ring members are independently selected from C(═O) and C(═S), and the sulfur atom ring members are independently selected from S(═O)u(═NR7)z, the ring system optionally substituted with substituents independently selected from R8 on carbon atom ring members and from R9 on nitrogen atom ring members; and R1, R2, R3, R4, R5, R6, R7, R8, R9, u and z are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
摘要翻译：公开了式1的化合物，包括所有的立体异构体，N-氧化物及其盐，其中Y是含有2-4个碳原子和2-3个氮原子作为环成员的5元全部或部分不饱和的杂环，在通过相邻单环原子连接的环成员原子上被Z取代的环与连接杂环的环原子连接到式1的苯环上，并且任选被至多2个独立地选自在碳原子上的R5的取代基取代环成员和R6上的氮原子环成员; Z是含有选自碳原子和1至4个独立地选自至多2个，至多2个和至多4个N原子的1至4个杂原子的环成员的8-，9-，10-或11-元稠合杂双环体系，其中最多3个碳原子环成员独立地选自C（= O）和C（= S），并且硫原子环成员独立地选自S（= O）u（= NRR）z，被取代基独立地选自碳原子环上的R 8和氮原子环上的R 9; 并且R1，R2，R3，R4，R5，R6，R7，R8，R9，u和z如本公开所定义。还公开了含有式1化合物的组合物和用于控制由真菌病原体引起的植物病害的方法，包括施用有效量的本发明化合物或组合物。

58. 发明授权

US08779158B2 Trisubstituted pyrazoles as acetylcholine receptor modulators 有权
标题翻译：三取代吡唑作为乙酰胆碱受体调节剂
公开(公告)号：US08779158B2
公开(公告)日：2014-07-15
申请号：US12991119
申请日：2009-05-08
申请人： Johannes Wilhelmus John F. Thuring , Gregor James MacDonald , Wei Zhuang
发明人： Johannes Wilhelmus John F. Thuring , Gregor James MacDonald , Wei Zhuang
IPC分类号： A61K31/4155 , A01N43/36 , C07D231/02 , C07D401/04
CPC分类号： C07D401/04 , C07D231/38 , C07D405/04 , C07D405/14
摘要： The present invention relates to 1-alkyl-3-aniline-5-aryl-pyrazole derivatives and pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, according to Formula (I).The invention particularly relates to positive allosteric modulators of nicotinic acetylcholine receptors, such positive allosteric modulator having the capability to increase the efficacy of nicotinic receptor agonists.
摘要翻译：本发明涉及1-烷基-3-苯胺-5-芳基吡唑衍生物及其药学上可接受的盐，其制备方法，含有它们的药物组合物及其在治疗中的用途，根据式（I）。本发明特别涉及烟碱乙酰胆碱受体的正变构调节剂，这种正变构调节剂具有增加烟碱受体激动剂功效的能力。

59. 发明授权

US08106070B2 Substituted imidazoles as bombesin receptor subtype-3 modulators 失效
标题翻译：取代的咪唑作为铃蟾肽受体亚型-3调节剂
公开(公告)号：US08106070B2
公开(公告)日：2012-01-31
申请号：US12311541
申请日：2007-10-16
申请人： David Chen , Christopher L. Franklin , Peter R. Guzzo , Linus S. Lin , Jian Liu , Michael M. -C. Lo , Ravi P. Nargund , Iyassu K. Sebhat
发明人： David Chen , Christopher L. Franklin , Peter R. Guzzo , Linus S. Lin , Jian Liu , Michael M. -C. Lo , Ravi P. Nargund , Iyassu K. Sebhat
IPC分类号： A61K31/437 , A61K31/44 , A61K31/4178 , C07D401/10 , C07D231/02 , C07D471/04
CPC分类号： C07D401/10 , C07D233/64 , C07D401/14 , C07D403/10 , C07D417/10 , C07D471/04
摘要： Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.
摘要翻译：某些新颖的取代的咪唑是人类bombesin受体的配体，特别是人类bombesin受体亚型-3（BRS-3）的选择性配体。因此，它们可用于治疗，控制或预防对调节BRS-3的疾病和病症，例如肥胖症和糖尿病。

60. 发明授权

US08084452B2 Substituted enaminocarbonyl compounds used as insecticides 有权
标题翻译：用作杀虫剂的取代的烯氨基羰基化合物
公开(公告)号：US08084452B2
公开(公告)日：2011-12-27
申请号：US12295458
申请日：2007-03-19
申请人： Peter Jeschke , Robert Velten , Thomas Schenke , Otto Schallner , Michael Edmund Beck , Olga Malsam , Ralf Nauen , Thomas Müller , Christian Arnold , Erich Sanwald , Ulrich Görgens
发明人： Peter Jeschke , Robert Velten , Thomas Schenke , Otto Schallner , Michael Edmund Beck , Olga Malsam , Ralf Nauen , Thomas Müller , Christian Arnold , Erich Sanwald , Ulrich Görgens
IPC分类号： A61K31/506 , A61K31/4427 , A61K31/433 , A61K31/4245 , A61K31/425 , A61K31/422 , A61K31/4196 , A61K31/4155 , C07D271/06 , C07D285/10 , C07D275/02 , C07D263/02 , C07D261/02 , C07D249/08 , C07D241/02 , C07D231/02 , C07D203/02
CPC分类号： C07D405/12 , A01N43/40
摘要： The present application relates to novel substituted enaminocarbonyl compounds, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.
摘要翻译：本申请涉及新的取代的烯氨基羰基化合物，其制备方法及其用于控制动物害虫，特别是节肢动物，特别是昆虫的用途。

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