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21. 发明授权

US09139524B2 Fluorinated bridged spiro[2.4]heptane derivatives as ALX receptor agonists 有权
标题翻译：氟化桥接螺[2.4]庚烷衍生物作为ALX受体激动剂
公开(公告)号：US09139524B2
公开(公告)日：2015-09-22
申请号：US14401769
申请日：2013-05-15
申请人： Actelion Pharmaceuticals Ltd.
发明人： Olivier Corminboeuf , Davide Pozzi
IPC分类号： C07D211/58 , C07D207/14
CPC分类号： C07D211/58 , C07D207/14
摘要： The present invention relates to fluorinated bridged spiro[2.4]heptane derivatives of formula (I), wherein n and R1 are as defined in the description, their preparation and their use as pharmaceutically active compounds.
摘要翻译：本发明涉及式（I）的氟化桥接螺[2.4]庚烷衍生物，其中n和R 1如说明书中所定义，其制备及其作为药物活性化合物的用途。

22. 发明申请

US20140148460A1 THERAPEUTIC COMPOSITIONS 审中-公开
标题翻译：治疗组合物
公开(公告)号：US20140148460A1
公开(公告)日：2014-05-29
申请号：US14162280
申请日：2014-01-23
申请人： Martine CLOZEL
发明人： Martine CLOZEL
IPC分类号： A61K31/513 , A61K31/4985 , A61K31/53 , A61K31/519
CPC分类号： A61K31/513 , A61K31/4985 , A61K31/506 , A61K31/519 , A61K31/53 , A61K45/06 , A61K2300/00
摘要： The invention relates to a product containing the compound of formula (I) below (I) or a pharmaceutically acceptable salt of this compound, in combination with at least one compound having PDE5-inhibitory properties, or a pharmaceutically acceptable salt thereof, for therapeutic use, simultaneously, separately or over a period of time, in the treatment of a disease wherein vasoconstriction is involved.
摘要翻译：本发明涉及含有本发明化合物（I）的化合物或该化合物的药学上可接受的盐与至少一种具有PDE5抑制性质的化合物或其药学上可接受的盐组合用于治疗用途的产品，同时分开或在一段时间内，用于治疗涉及血管收缩的疾病。

23. 发明申请

US20140142093A1 TRICYCLIC OXAZOLIDINONE ANTIBIOTIC COMPOUNDS 有权
标题翻译：三氧化二氮唑酮类抗生素化合物
公开(公告)号：US20140142093A1
公开(公告)日：2014-05-22
申请号：US14096419
申请日：2013-12-04
申请人： Christian HUBSCHWERLEN , Daniel RITZ , Georg RUEEDI , Jean-Philippe SURIVET , Cornelia ZUMBRUNN-ACKLIN
发明人： Christian HUBSCHWERLEN , Daniel RITZ , Georg RUEEDI , Jean-Philippe SURIVET , Cornelia ZUMBRUNN-ACKLIN
IPC分类号： C07D471/06 , C07D487/06 , C07D519/00 , C07D471/16
CPC分类号： C07D471/06 , C07D471/16 , C07D487/06 , C07D519/00
摘要： The present invention relates to antibacterial compounds of formula (I) wherein “----” is a bond or is absent, V is CH, CR6 or N; R0 is H or, if “----” is a bond, may also be alkoxy; R1 is cyano, alkyl, or ethynyl; U is CH or N when “----” is a bond, or, if “----” is absent, U is CH2, NH or NH9; R2 is H, alkylcarbonyl or CH2—R3; R3 is H, alkyl or hydroxyalkyl; R4 is H or, if n is not 0 and R5 is H, may also be OH; R5 is H, alkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, carboxy or alkoxycarbonyl; R6 is hydroxyalkyl, carboxy, alkoxycarbonyl or —(CH2)q—NR7R8, q being 1, 2 or 3 and each of R7 and R8 independently being H or alkyl or R7 and R8 forming with the N atom bearing them a ring; R9 is alkyl or hydroxyalkyl; A is —(CH2)p—, —CH2CH2CH(OH)— or —COCH2CH(OH)—; G is substituted phenyl or G1 or G2, wherein Q is O or S and X is CH or N; and Y1, Y2 and Y3 may each be CH or N; and n is 0 when A is —CH2CH2CH(OH)— or —COCH2CH(OH)—, and n is 0, 1 or 2 when A is —(CH2)p—, p being 1, 2, 3 or 4, with the proviso that the sum of n and p is then 2, 3 or 4; and to salts of such compounds.
摘要翻译：本发明涉及式（I）的抗菌化合物，其中“----”是键或不存在，V是CH，CR 6或N; R 0是H，或者如果“----”是键，也可以是烷氧基; R1是氰基，烷基或乙炔基; 当“----”是键时，U是CH或N，或者如果不存在“----”，则U是CH 2，NH或NH 9; R2是H，烷基羰基或CH2-R3; R3是H，烷基或羟烷基; R4是H或如果n不为0且R5是H，也可以是OH; R5是H，烷基，羟基烷基，氨基烷基，烷氧基烷基，羧基或烷氧基羰基; R6是羟基烷基，羧基，烷氧基羰基或 - （CH2）q-NR7R8，q是1,2或3，R7和R8各自独立地是H或烷基或R7和R8与带有它们的N原子形成环; R9是烷基或羟烷基; A是 - （CH 2）p - ， - CH 2 CH 2 CH（OH） - 或-COCH 2 CH（OH） - ; G是取代的苯基或G1或G2，其中Q是O或S，X是CH或N; Y1，Y2和Y3各自为CH或N; 当A为-CH 2 CH 2 CH（OH） - 或-COCH 2 CH（OH） - 时，n为0，当A为 - （CH 2）p - ，p为1,2,3或4时，n为0,1或2，条件是n和p之和为2,3或4; 和这些化合物的盐。

24. 发明授权

US08709734B2 Method for identifying modulators of GPCR GPR1 function 有权
标题翻译：识别GPCR GPR1功能调制器的方法
公开(公告)号：US08709734B2
公开(公告)日：2014-04-29
申请号：US13499896
申请日：2010-10-01
申请人： Xavier Leroy
发明人： Xavier Leroy
IPC分类号： G01N33/53 , G01N33/566 , C07K14/705
CPC分类号： G01N33/566 , G01N2333/726 , G01N2500/02 , G01N2500/10
摘要： The invention relates to the identification of Humanin and derivatives thereof as ligands of the GPR1 GPCR (G-protein coupled receptor). The invention encompasses the use of the interaction of GPR1 polypeptides and Humanin polypeptides as the basis of screening assays for agents that modulate the activity of the GPR1 receptor. The invention also encompasses diagnostic assays based upon the GPR1/Humanin polypeptide interaction, as well as kits for performing diagnostic and screening assays.
摘要翻译：本发明涉及作为GPR1 GPCR（G蛋白偶联受体）的配体的人源蛋白及其衍生物的鉴定。本发明包括使用GPR1多肽和人源多肽的相互作用作为调节GPR1受体活性的试剂的筛选测定的基础。本发明还包括基于GPR1 / Humanin多肽相互作用的诊断测定，以及用于进行诊断和筛选测定的试剂盒。

25. 发明授权

US08697732B2 Pyridine derivatives 失效
标题翻译：吡啶衍生物
公开(公告)号：US08697732B2
公开(公告)日：2014-04-15
申请号：US13438657
申请日：2012-04-03
申请人： Martin Bolli , David Lehmann , Boris Mathys , Claus Mueller , Oliver Nayler , Beat Steiner , Jörg Velker
发明人： Martin Bolli , David Lehmann , Boris Mathys , Claus Mueller , Oliver Nayler , Beat Steiner , Jörg Velker
IPC分类号： A61K31/4433 , C07D413/14
CPC分类号： C07D409/06 , C07D413/14
摘要： The invention relates to novel pyridine derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents.
摘要翻译：本发明涉及新颖的吡啶衍生物，其制备及其作为药物活性化合物的用途。所述化合物特别充当免疫抑制剂。

26. 发明申请

US20130345199A1 1-[M-CARBOXAMIDO(HETERO)ARYL-METHYL]-PIPERIDINE-4-CARBOXAMIDE DERIVATIVES 审中-公开
标题翻译： 1- [M-CARBOXAMIDO（HETERO）ARYL-METHYL] - 哌啶-4-羧酰胺衍生物
公开(公告)号：US20130345199A1
公开(公告)日：2013-12-26
申请号：US13923981
申请日：2013-06-21
申请人： Heinz FRETZ , Markus Gude , Philippe Guerry , Thierry Kimmerlin , Francois Lehembre , Thomas Pfeifer , Anja Valdenaire
发明人： Heinz FRETZ , Markus Gude , Philippe Guerry , Thierry Kimmerlin , Francois Lehembre , Thomas Pfeifer , Anja Valdenaire
IPC分类号： C07D211/66 , C07D401/14 , C07D417/12 , C07D409/12 , C07D401/12 , C07D405/12
摘要： The present invention relates to 1-[m-Carboxamido(hetero)aryl-methyl]-piperidine-4-carboxamide derivatives of formula (I) wherein X, Ar1, R1, R2, R3, R4, R5 and p are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as CXCR7 receptor modulators.
摘要翻译：本发明涉及式（I）的1- [间 - 甲酰氨基（杂）芳基 - 甲基] - 哌啶-4-甲酰胺衍生物，其中X，Ar1，R1，R2，R3，R4，R5和p如对其制备的描述，其药学上可接受的盐及其作为药物的用途，含有一种或多种式（I）化合物的药物组合物，特别是其作为CXCR7受体调节剂的用途。

27. 发明授权

US08580824B2 Pyridin-4-yl derivatives as immunomodulating agents 有权
标题翻译：吡啶-4-基衍生物作为免疫调节剂
公开(公告)号：US08580824B2
公开(公告)日：2013-11-12
申请号：US12310801
申请日：2007-09-06
申请人： Martin Bolli , David Lehmann , Boris Mathys , Claus Mueller , Oliver Nayler , Beat Steiner , Jörg Velker
发明人： Martin Bolli , David Lehmann , Boris Mathys , Claus Mueller , Oliver Nayler , Beat Steiner , Jörg Velker
IPC分类号： A61K31/443 , C07D413/04
CPC分类号： C07D413/04 , C07D417/04
摘要： The invention relates to pyridine derivatives of Formula (I) wherein A, R1, R2, R3, R4, R5, and R6 are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
摘要翻译：本发明涉及式（I）的吡啶衍生物，其中A，R 1，R 2，R 3，R 4，R 5和R 6如描述中所述，其制备及其作为药物活性化合物的用途。所述化合物特别充当免疫调节剂。

28. 发明授权

US08575200B2 Pyridin-2-yl derivatives as immunomodulating agents 有权
标题翻译：吡啶-2-基衍生物作为免疫调节剂
公开(公告)号：US08575200B2
公开(公告)日：2013-11-05
申请号：US12920656
申请日：2009-02-25
申请人： Martin Bolli , Cyrille Lescop , Boris Mathys , Claus Mueller , Oliver Nayler , Beat Steiner
发明人： Martin Bolli , Cyrille Lescop , Boris Mathys , Claus Mueller , Oliver Nayler , Beat Steiner
IPC分类号： A61K31/4439 , C07D413/04
CPC分类号： C07D413/04
摘要： The invention relates to pyridine derivatives of Formula (I) wherein A, R1, R2, R3, R4, R5, R6 and R7 are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
摘要翻译：本发明涉及式（I）的吡啶衍生物，其中A，R 1，R 2，R 3，R 4，R 5，R 6和R 7如说明书中所述，其制备及其作为药物活性化合物的用途。所述化合物特别充当免疫调节剂。

29. 发明申请

US20130231319A1 Bridged Spiro[2.4]heptane Ester Derivatives 有权
标题翻译：桥接螺[2.4]庚烷酯衍生物
公开(公告)号：US20130231319A1
公开(公告)日：2013-09-05
申请号：US13988204
申请日：2011-11-16
申请人： Daniel Bur , Olivier Corminboeup , Sylvaine Gren , Corinna Grisostomi , Xavier Leroy , Sylvia Richard-Bildstein , Davide Pozzi
发明人： Daniel Bur , Olivier Corminboeup , Sylvaine Gren , Corinna Grisostomi , Xavier Leroy , Sylvia Richard-Bildstein , Davide Pozzi
IPC分类号： C07D263/32 , C07C69/753 , C07D241/04 , C07D207/12 , C07D205/04 , C07D211/14 , C07D207/08
CPC分类号： C07D263/32 , C07C69/753 , C07D205/04 , C07D207/08 , C07D207/10 , C07D207/12 , C07D211/14 , C07D211/22 , C07D211/42 , C07D213/75 , C07D241/04 , C07D261/08 , C07D295/088 , C07D401/12 , C07D413/12
摘要： The invention relates to a method for preparing linear polymers having an amide end or having a star architecture comprising an amide core, by means of a ring opening using lactide and glycolide monomers or a lactide monomer ring in the presence of a catalyst, wherein the method includes the steps of: (i) reacting the excess monomer(s) with an initiator in a solvent, said initiator being selected from among an amine and an amino alcohol, given that the initiator has at least one primary or secondary amine function; (ii) adding a catalyst, said catalyst being a non-nucleophilic base and including at least one neutral sp2 nitrogen atom; and (iii) neutralizing the reaction mixture. Said novel method is particularly advantageous in that it can be easily monitored and enables better modulation of the polymers, and thus of the properties thereof, than the methods of the prior art. The invention also relates to novel polymers that are obtainable by means of said method.
摘要翻译：本发明涉及一种通过在催化剂存在下通过使用丙交酯和乙交酯单体或丙交酯单体环的开环制备具有酰胺末端或具有包含酰胺核心的星型结构的线性聚合物的方法，其中所述方法包括以下步骤：（i）使多余的单体与引发剂在溶剂中反应，所述引发剂选自胺和氨基醇，假定引发剂具有至少一个伯或仲胺官能团; （ii）加入催化剂，所述催化剂是非亲核碱，并包括至少一个中性sp2氮原子; 和（iii）中和反应混合物。所述新颖的方法特别有利的是，与现有技术的方法相比，其可以容易地被监测并且能够更好地调节聚合物，并因此实现其性质。本发明还涉及通过所述方法可获得的新型聚合物。

30. 发明授权

US08415375B2 2-hydroxyethyl-1H-quinolin-2-one derivatives and their azaisosteric analogues with antibacterial activity 有权
标题翻译： 2-羟乙基-1H-喹啉-2-酮衍生物及其具有抗菌活性的azaisosteric类似物
公开(公告)号：US08415375B2
公开(公告)日：2013-04-09
申请号：US13263922
申请日：2010-04-08
申请人： Christian Hubschwerlen , Georg Rueedi , Jean-Philippe Surivet , Cornelia Zumbrunn Acklin
发明人： Christian Hubschwerlen , Georg Rueedi , Jean-Philippe Surivet , Cornelia Zumbrunn Acklin
IPC分类号： A01N43/42 , A61K31/47
CPC分类号： C07D491/056 , C07D497/04
摘要： The invention relates to antibacterial compounds of formula I wherein R1 represents alkoxy; each of U and V represents CH and W represents CH or N, or U represents N, V represents CH and W represents N, or each of U and V represents N and W represents CH; R2 represents hydrogen or fluorine when W represents CH or R2 represents hydrogen when W represents N; A represents O or CH2; Y represents CH or N; Q represents O or S; and n represents 0 or 1; and salts of such compounds.
摘要翻译：本发明涉及式Ⅰ的抗菌化合物，其中R1代表烷氧基; U和V各自表示CH，W表示CH或N，或U表示N，V表示CH，W表示N，或U和V表示N，W表示CH; 当W表示CH时，R2表示氢或氟，当W表示N时，R2表示氢; A表示O或CH 2; Y表示CH或N; Q表示O或S; n表示0或1; 和这些化合物的盐。

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