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1. 发明授权

US09856253B2 Tricyclic modulators of TNF signaling 有权
公开(公告)号：US09856253B2
公开(公告)日：2018-01-02
申请号：US15130362
申请日：2016-04-15
申请人： AbbVie Inc.
发明人： Eric C. Breinlinger , Phil B. Cox , Justin Dietrich , Kristine E. Frank , Michael M. Friedman , Huan-Qui Li , Kenton Longenecker , Augustine Osuma , Ann Marie Rowley , Anil Vasudevan , Noel Wilson
IPC分类号： C07D227/00 , C07D471/04 , C07D471/14 , C07D487/04 , C07D498/04 , C07D498/14 , C07D498/18 , C07D498/20 , C07D498/22 , C07D519/00 , C07D471/18 , C07D491/147 , C07D491/22
CPC分类号： C07D471/04 , C07D471/14 , C07D471/18 , C07D487/04 , C07D491/147 , C07D491/22 , C07D498/04 , C07D498/14 , C07D498/18 , C07D498/20 , C07D498/22 , C07D519/00
摘要： The invention provides tricyclic heterocyclic compounds, pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variables are defined herein. The compounds of the invention may be useful for treating immunological and oncological conditions.

2. 发明授权

US07999120B2 Process for continuously removing a target product X in the form of fine crystals 有权
标题翻译：连续除去细晶体形式的目标产物X的方法
公开(公告)号：US07999120B2
公开(公告)日：2011-08-16
申请号：US12209594
申请日：2008-09-12
申请人： Jörg Heilek , Peter Schlemmer , Ulrich Hammon , Klaus Joachim Müller-Engel
发明人： Jörg Heilek , Peter Schlemmer , Ulrich Hammon , Klaus Joachim Müller-Engel
IPC分类号： C07D227/00 , C07C51/43 , C07C7/14
CPC分类号： B01D9/0013 , B01D9/0045 , B01D9/0063 , C07C51/43 , C07C57/04
摘要： A process for continuously removing a target product X in the form of fine crystals from a liquid phase P comprising the target product X and constituents other than the target product X by cooling suspension crystallization in the secondary chamber, into which the liquid phase P flows continuously, of an indirect heat exchanger with simultaneous continuous flow of a coolant through the primary chamber of the indirect heat exchanger and continuous withdrawal of a crystal suspension S having a degree of crystallization Y from the secondary chamber, in which the degree of crystallization Y is adjusted on the basis of a heat balance conducted continuously with the aid of a process computer.
摘要翻译：从液相P连续除去来自包含目标产物X的液相P和除了目标产物X以外的成分的微晶形式的目标产物X的方法，通过冷却液相P连续流入的二次室中的悬浮液结晶的间接热交换器，其通过间接热交换器的主室同时连续流动冷却剂，并且从二级室连续取出具有结晶度Y的晶体悬浮液S，其中结晶度Y被调节基于在过程计算机的帮助下连续进行的热平衡。

3. 发明授权

US5741789A Compounds having effects on serotonin-related systems 失效
公开(公告)号：US5741789A
公开(公告)日：1998-04-21
申请号：US467434
申请日：1995-06-06
申请人： David J. Hibschman , Joseph H. Krushinski, Jr. , Kurt Rasmussen , Vincent P. Rocco , John M. Schaus , Dennis C. Thompson
发明人： David J. Hibschman , Joseph H. Krushinski, Jr. , Kurt Rasmussen , Vincent P. Rocco , John M. Schaus , Dennis C. Thompson
IPC分类号： C07D209/08 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D471/08 , C07D471/10 , C07D491/10 , C07D491/20 , C07D495/10 , C07D513/04 , C07D227/00 , A61K31/395 , A61K31/445
CPC分类号： C07D209/08 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D471/08 , C07D471/10 , C07D491/10 , C07D495/10 , C07D513/04
摘要： A series of hetero-oxy alkanamines are effective pharmaceuticals for the treatment of conditions related to or affected by the reuptake of serotonin and by the serotonin 1.sub.A receptor. The compounds are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal, and for the treatment of depression and other conditions for which serotonin reuptake inhibitors are used.

4. 发明授权

US4804753A Process for the preparation of Schiff's bases 失效
标题翻译：制备席夫碱的方法
公开(公告)号：US4804753A
公开(公告)日：1989-02-14
申请号：US817205
申请日：1986-01-08
申请人： Hans-Helmut Schwarz
发明人： Hans-Helmut Schwarz
IPC分类号： C07D207/263 , C07D207/20 , C07D211/70 , C07D223/04 , C07D225/02 , C07D227/00 , C08G69/00 , C08G69/18 , C07D223/02
CPC分类号： C07D207/20 , C07D223/04
摘要： A process for the preparation of Schiff's bases which contain amino groups, of the formula ##STR1## wherein n is 3 to 12,by reacting cyclic lactams of the formula ##STR2## wherein n is 3 to 12,or of their ring-opened polymers of the formula ##STR3## wherein n is 3 to 12 andm is 1 to 100,000,with inorganic bases at elevated temperature, the reaction being carried out in the presence of inert, high-boiling suspending agents.
摘要翻译：或其开环聚合物（其中n为3-12）的式IMAMA的环状内酰胺或其开环聚合物，其中n为3至12，通式为“IMAGE”，其中n为3至12的含有氨基的席夫碱其中n为3〜12，m为1〜100,000，无机碱在升高的温度下进行，反应在惰性高沸点悬浮剂的存在下进行。

5. 发明授权

US4137417A Process for producing an enamide 失效
标题翻译：生产烯酰胺的方法
公开(公告)号：US4137417A
公开(公告)日：1979-01-30
申请号：US790908
申请日：1977-04-26
申请人： Motoo Hazama
发明人： Motoo Hazama
IPC分类号： C07B61/00 , B01J23/46 , C07C20060101 , C07C67/00 , C07C231/00 , C07C231/10 , C07C233/00 , C07C233/05 , C07C233/06 , C07C233/16 , C07C233/31 , C07C233/47 , C07C233/65 , C07C233/71 , C07C233/85 , C07C233/90 , C07C233/91 , C07C233/92 , C07C237/16 , C07C237/22 , C07C253/00 , C07C255/24 , C07C255/30 , C07D209/18 , C07D227/00 , C07D233/64 , C07C102/00
CPC分类号： C07C255/00
摘要： Enamides are prepared by hydrogenating oximes having at least one hydrogen atom at the .alpha.-position in the presence of a carboxylic anhydride using a ruthenium catalyst. These enamides are important to obtain amino group-containing compounds by reduction or polymerization.
摘要翻译：酰胺通过使用钌催化剂在羧酸酐存在下，通过氢化在α位上具有至少一个氢原子的肟来制备。这些酰胺对于通过还原或聚合获得含氨基化合物是重要的。

6. 发明授权

US07579339B2 Ring-substituted diphenylazetidinones, process for their preparation, medicaments comprising these compounds, and their use 有权
标题翻译：环取代的二苯基氮杂环丁酮，其制备方法，包含这些化合物的药物及其用途
公开(公告)号：US07579339B2
公开(公告)日：2009-08-25
申请号：US11501758
申请日：2006-08-10
申请人： Gerhard Jaehne , Wendelin Frick , Stefanie Flohr , Andreas Lindenschmidt , Heiner Glombik , Werner Kramer , Hubert Heuer , Hans-Ludwig Schaefer
发明人： Gerhard Jaehne , Wendelin Frick , Stefanie Flohr , Andreas Lindenschmidt , Heiner Glombik , Werner Kramer , Hubert Heuer , Hans-Ludwig Schaefer
IPC分类号： C07D205/08 , C07D227/00 , A61K31/397 , A61P3/06 , A61P9/10
CPC分类号： C07D403/12 , C07D205/08 , C07D453/02 , C07D487/08 , Y10S930/28
摘要： One embodiment of the invention relates to compounds of the formula I, in which R1, R2, R3, R4, R5 and R6 have the meanings given in the specification. Other embodiments of the invention relate to physiologically acceptable salts of compounds of formula I, to processes for their preparation and to medicaments comprising these compounds. The compounds of the invention are suitable for use, for example, as hypolipidemics.
摘要翻译：本发明的一个实施方案涉及式I化合物，其中R 1，R 2，R 3，R 4，R 5和R 6具有说明书中给出的含义。本发明的其它实施方案涉及式I化合物的生理上可接受的盐，其制备方法和包含这些化合物的药物。本发明的化合物适合用作例如降血脂药。

7. 发明授权

US07390790B2 Ring-substituted diphenylazetidinones, process for their preparation, medicaments comprising these compounds, and their use 有权
公开(公告)号：US07390790B2
公开(公告)日：2008-06-24
申请号：US11544718
申请日：2006-10-10
申请人： Gerhard Jaehne , Wendelin Frick , Stefanie Flohr , Andreas Lindenschmidt , Heiner Glombik , Werner Kramer , Hubert Heuer , Hans-Ludwig Schaefer
发明人： Gerhard Jaehne , Wendelin Frick , Stefanie Flohr , Andreas Lindenschmidt , Heiner Glombik , Werner Kramer , Hubert Heuer , Hans-Ludwig Schaefer
IPC分类号： A61K31/7052 , C07H7/02 , C07H7/04 , A61P3/06 , A61P9/10 , A61K31/397 , C07D205/08 , C07D227/00
CPC分类号： C07D403/12 , C07D205/08 , C07D453/02 , C07D487/08 , Y10S930/28
摘要： One embodiment of the invention relates to compounds of the formula I, in which R1, R2, R3, R4, R5 and R6 have the meanings given in the specification. Other embodiments of the invention relate to physiologically acceptable salts of compounds of formula I, to processes for their preparation and to medicaments comprising these compounds. The compounds of the invention are suitable for use, for example, as hypolipidemics.

8. 发明授权

US6165800A Chemiluminescent energy transfer conjugates and their uses as labels in binding assays 失效
标题翻译：化学发光能量转移共轭物及其用作结合测定中的标记物
公开(公告)号：US6165800A
公开(公告)日：2000-12-26
申请号：US86003
申请日：1998-05-27
申请人： Qingping Jiang , Jun Xi , Anand Natrajan , David Sharpe , Marcus Baumann , Rolf Hilfiker , Erika Schmidt , Paul Senn , Fritz Thommen , Adrian Waldner , Alex Alder , Say-Jong Law
发明人： Qingping Jiang , Jun Xi , Anand Natrajan , David Sharpe , Marcus Baumann , Rolf Hilfiker , Erika Schmidt , Paul Senn , Fritz Thommen , Adrian Waldner , Alex Alder , Say-Jong Law
IPC分类号： C09B11/04 , C09B15/00 , C09K11/07 , G01N33/533 , G01N33/542 , G01N33/58 , C07D227/00 , G01N33/553
CPC分类号： C09B15/00 , C09B11/04 , G01N33/533 , G01N33/542 , G01N33/582 , Y10S436/80 , Y10S436/816 , Y10S436/817
摘要： A new class of chemiluminescent acridinium or benzacridinium compounds is disclosed by virtue of forming an intramolecular energy transfer conjugate (ETC) between the acridinium or benzacridinium compound and a luminophore. A method of extending the emission wavelengths of acridinium or benzacridinium esters in order to further reduce or eliminate the emission spectral overlap between the parent polysubstituted aryl Acridinium Esters (DMAE) and Benzacridinium Esters (LEAE) is disclosed. The ETC's retain the unique desired properties of acridinium or benzacridinium compounds including complete light emission in very short period of time, monophasic emission spectrum, simplicity of triggering mechanism, ability of labeling the biological molecules of interest to form a tracer, and good stability. Additionally, the range of the emission spectrum of an acridinium or benzacridinium compound can now be shifted at will and at longer leap through the choice of a luminophore as the integral part of an ETC molecule. Disclosed are chemiluminescent labeled conjugates comprising an acridinium or benzacridinium moiety covalently attached to a luminophore via a spacer, said moiety further conjugated to a biological molecule of interest, wherein said spacer is of an appropriate length to allow the excited species generated from said moiety to transfer energy efficiently to said luminophore, resulting in the emission of light in the spectral region of said luminophore. Also disclosed are binding assays using said conjugates, test kits comprising said conjugates and methods of preparing the conjugates.
摘要翻译：通过在吖啶鎓或苯并吖啶鎓化合物和发光体之间形成分子内能量转移缀合物（ETC），公开了一类新的化学发光吖啶鎓或苯并吖啶鎓化合物。公开了延长吖啶鎓或苯并吖啶酯的发射波长以进一步减少或消除母体多取代芳基吖啶酯（DMAE）和苯并吖啶酯（LEAE）之间的发射光谱重叠的方法。 ETC保留吖啶鎓或苯并吖啶鎓化合物独特的所需性质，包括在很短的时间内完全发光，单相发射光谱，触发机制简单，标记生物分子的能力，形成示踪剂，以及良好的稳定性。此外，吖啶鎓或苯并吖啶鎓化合物的发射光谱的范围现在可以随意移动，并且通过选择发光体作为ETC分子的组成部分而更长的跨越。公开了化学发光标记的缀合物，其包含通过间隔基共价连接到发光体的吖啶鎓或苯并吖啶鎓部分，所述部分还与感兴趣的生物分子缀合，其中所述间隔物具有适当长度以允许从所述部分产生的激发物质转移能量有效地发送到所述发光体，导致发光在所述发光体的光谱区域。还公开了使用所述缀合物的结合测定法，包含所述缀合物的测试试剂盒和制备缀合物的方法。

9. 发明授权

US5977178A Compounds with growth hormone releasing properties 失效
公开(公告)号：US5977178A
公开(公告)日：1999-11-02
申请号：US769020
申请日：1996-12-18
申请人： Thomas Kruse Hansen , Bernd Peschke , Jesper Lau , Behrend Friedrich Lundt , Michael Ankersen , Brett Watson , Kjeld Madsen
发明人： Thomas Kruse Hansen , Bernd Peschke , Jesper Lau , Behrend Friedrich Lundt , Michael Ankersen , Brett Watson , Kjeld Madsen
IPC分类号： C07D333/20 , A61K31/00 , A61K31/17 , A61K31/18 , A61K31/216 , A61K31/27 , A61K31/38 , A61K31/381 , A61K31/41 , A61K31/4245 , A61K31/454 , A61K38/00 , A61K38/07 , A61K38/08 , A61P3/00 , A61P5/00 , A61P5/06 , A61P5/10 , A61P15/00 , A61P15/14 , A61P19/00 , B41J19/20 , C07C237/00 , C07C237/22 , C07C311/05 , C07C335/14 , C07D213/12 , C07D227/00 , C07D271/06 , C07D333/00 , C07D333/24 , C07D333/60 , C07D409/00 , C07D413/12 , C07K5/03 , C07K5/06 , C07K5/065 , C07K5/078 , C07K5/10 , C07K7/02 , C07K14/60 , A61K31/16 , C07C233/01
CPC分类号： C07D271/06 , B41J19/205 , C07C237/22 , C07D333/24 , C07D413/12 , C07K5/0606 , C07K5/06078 , C07K5/06139 , C07K5/06191 , A61K38/00
摘要： Compounds of peptide mimetic nature having the general formula I ##STR1## wherein a and b are independently 1 or 2, R.sup.1 and R.sup.2 are independently H or C.sub.1-6 alkyl, G and J are independently, inter alia, aromats, and D and E are independently several different groups are growth hormone secretagogous with improved bioavailability.

10. 发明授权

US5541317A Azetidinone compounds useful in the preparation of carbapenem antibiotics and process for preparing carbapenem and penem compounds 失效
标题翻译：可用于制备碳青霉烯类抗生素的氮杂环丁酮化合物及其制备碳青霉烯和青霉烯化合物的方法
公开(公告)号：US5541317A
公开(公告)日：1996-07-30
申请号：US289133
申请日：1994-08-11
申请人： Koichi Hirai , Yuji Iwano , Takahide Nishi , Akira Yoshida , Kozo Oda , Hiroo Koyama
发明人： Koichi Hirai , Yuji Iwano , Takahide Nishi , Akira Yoshida , Kozo Oda , Hiroo Koyama
IPC分类号： C07D205/08 , C07D401/12 , C07D403/12 , C07D477/02 , C07D477/04 , C07D477/20 , C07D499/88 , C07F7/10 , C07F7/18 , C07D227/00 , C07D487/04 , C07D499/04
CPC分类号： C07D401/12 , C07D205/08 , C07D403/12 , C07D477/02 , C07D477/04 , C07D477/20 , C07D499/88 , C07F7/10 , C07F7/186 , C07F7/1892 , Y02P20/55
摘要： Compounds of formula (I): ##STR1## wherein: R.sup.1 is hydrogen or a hydroxy-protecting group; R.sup.2 is alkyl, alkoxy, halogen, optionally substituted phenyl or optionally substituted phenoxy; R.sup.3 is optionally substituted pyridyl, optionally substituted quinolyl or phenyl group which has a substituent of formula --CYNR.sup.5 R.sup.6, where Y is oxygen or sulfur, and R.sup.5 and R.sup.6 are each alkyl, aryl or aralkyl, or R.sup.5 and R.sup.6 and the nitrogen to which they are attached together form a heterocyclic group; is R.sup.4 hydrogen or an amino-protecting group; and Z is sulfur or oxygen; are valuable intermediates in the preparation of carbapenem compounds and retain a desirable configuration during conversion to such carbapenem compounds. Penem and carbapenem compounds having a group of formula --SA' are prepared from a corresponding compound having a substituted thio, sulfinyl or sulfonyl group at this position by reaction with a compound A'SH (where A' is an organic group) in the presence of a salt of a metal of Group II or III of the Periodic Table.
摘要翻译：式（I）的化合物：其中：R1是氢或羟基保护基; R 2是烷基，烷氧基，卤素，任选取代的苯基或任选取代的苯氧基; R3是任选取代的吡啶基，任选取代的具有式-CYNR 5 R 6的取代基的喹啉基或苯基，其中Y是氧或硫，R 5和R 6各自是烷基，芳基或芳烷基，或者R 5和R 6以及它们一起形成杂环基; 是R 4氢或氨基保护基; Z为硫或氧; 是制备碳青霉烯化合物的有价值的中间体，并且在转化成这种碳青霉烯化合物期间保留期望的构型。在具有取代的硫代，亚磺酰基或磺酰基的相应化合物的化合物A'SH（其中A'为有机基团）的存在下，通过与化合物A'SH（其中A'为有机基团）反应，由具有取代的硫代，亚磺酰基或磺酰基的相应化合物制备具有式-SA'基团的Penem和carbapenem化合物的元素周期表II或III族金属的盐。

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