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1. 发明申请

US20130096119A1 Isoquinolin-3-Ylurea Derivatives 审中-公开
标题翻译：异喹啉-3-基脲衍生物
公开(公告)号：US20130096119A1
公开(公告)日：2013-04-18
申请号：US13638892
申请日：2011-03-30
申请人： Daniel Bur , Markus Gude , Christian Hubschwerlen , Philippe Panchaud
发明人： Daniel Bur , Markus Gude , Christian Hubschwerlen , Philippe Panchaud
IPC分类号： C07D471/04 , C07D413/14 , C07D401/12 , C07D217/22 , C07D401/10
CPC分类号： C07D471/04 , C07D217/22 , C07D401/04 , C07D401/10 , C07D401/12 , C07D405/04 , C07D409/04 , C07D413/14
摘要： The invention relates to isoquinolin-3-ylurea derivatives of formula (I) wherein R1 represents (C1-C3)alkyl, (C1-C3)haloalkyl or cyclopropyl, R4 represents H and the substituents R2 and R3 and R5 have the meanings disclosed in the specification; and to the salts of such compounds. These compounds are useful for the prevention or the treatment of bacterial infections.
摘要翻译：本发明涉及式（I）的异喹啉-3-基脲衍生物，其中R 1表示（C 1 -C 3）烷基，（C 1 -C 3）卤代烷基或环丙基，R 4表示H，取代基R 2和R 3和R 5具有规格; 和这些化合物的盐。这些化合物可用于预防或治疗细菌感染。

2. 发明授权

US08217029B2 Oxazolidinone antibiotics 有权
标题翻译：恶唑烷酮类抗生素
公开(公告)号：US08217029B2
公开(公告)日：2012-07-10
申请号：US12595720
申请日：2008-04-11
申请人： Daniel Bur , Christian Hubschwerlen , Georg Rueedi , Jean-Philippe Surivet , Cornelia Zumbrunn-Acklin
发明人： Daniel Bur , Christian Hubschwerlen , Georg Rueedi , Jean-Philippe Surivet , Cornelia Zumbrunn-Acklin
IPC分类号： A61K31/397 , A61K31/55 , A61K31/54 , A61K31/50 , A61K31/497 , A61K31/44 , C07D243/08 , C07D279/10 , C07D237/26 , C07D401/14 , C07D239/72 , C07D471/12 , C07D471/22 , C07D215/00
CPC分类号： C07D413/14 , C07D471/04 , C07D519/00
摘要： The invention relates to compounds of formula (I) wherein U, V, W, X, R1, R2, R3, R4, R5, R6, A, B, D, E, G, m, and n are as defined in the description, to pharmaceutically acceptable salts of such compounds for use in the manufacture of a medicament for the prevention or treatment of a bacterial infection. Certain compounds of formula (I) are new and are also part of this invention.
摘要翻译：本发明涉及式（I）化合物，其中U，V，W，X，R 1，R 2，R 3，R 4，R 5，R 6，A，B，D，E，G，m和n如描述了用于制备用于预防或治疗细菌感染的药物的这些化合物的药学上可接受的盐。某些式（I）化合物是新的，也是本发明的一部分。

3. 发明授权

US07981886B2 Antibiotics derivatives 失效
标题翻译：抗生素衍生物
公开(公告)号：US07981886B2
公开(公告)日：2011-07-19
申请号：US11915179
申请日：2006-05-24
申请人： Daniel Bur , Christian Hubschwerlen , Jean-Philippe Surivet , Cornelia Zumbrunn-Acklin
发明人： Daniel Bur , Christian Hubschwerlen , Jean-Philippe Surivet , Cornelia Zumbrunn-Acklin
IPC分类号： C07D417/12 , C07D413/12 , C07D409/12 , A61K31/5415 , A61K31/538
CPC分类号： C07D277/64 , C07D409/12 , C07D413/12 , C07D417/12 , C07D513/04
摘要： The invention relates to antibiotic derivatives of formula I wherein: A represents —O—, S, —C(═O)—, —C(═NOR6)—; Z—B represents NCH2CH2, NCOCH2, NCH2CO, NCH2CH(OH), CHN(R8)CH2 or CHN(R8)CO; D represents binuclear heteroaryl; Y1 represents —CR1— or —N—, Y2 represents —CR2— or —N—, Y3 represents —CR3— or —N— and Y4 represents —CR4— or —N—; U represents —NH—, —O— or —S— and V represents —N— or —CH—; W represents —CH2—, —O— or —NR7—; R1 represents H, methyl, ethyl or halogen; R2, R3 and R4 each represent independently H, C1-C4 alkyl, halogen, or C1-C4 alkoxy; R5 represents H, C1-C4 alkyl or fluorine; R6 represents H, C1-C4 alkyl or aryl-C1-C4 alkyl; R7 represents H, C1-C4 alkyl, aryl-C1-C4 alkyl or —CH2—COOH; R8 represents H, C1-C4 alkyl or —CH2—COOH; with the provisos that if Z—B represents NCH2CH2, NCOCH2, NCH2CO or NCH2CH(OH), then W represents —CH2—; if A represents O or S, then W represents —CH2—; and only one or two of Y1, Y2, Y3 and Y4 can represent N at the same time.
摘要翻译：本发明涉及式I的抗生素衍生物，其中：A表示-O-，S，-C（= O） - ， - C（= NOR 6） - ; Z-B表示NCH2CH2，NCOCH2，NCH2CO，NCH2CH（OH），CHN（R8）CH2或CHN（R8）CO; D表示双核杂芳基; Y1表示-CR1-或-N-，Y2表示-CR2-或-N-，Y3表示-CR3-或-N-，Y4表示-CR4-或-N-; U表示-NH-，-O-或-S-，V表示-N-或-CH-; W表示-CH 2 - ， - O-或-NR 7 - ; R1代表H，甲基，乙基或卤素; R2，R3和R4各自独立地表示H，C1-C4烷基，卤素或C1-C4烷氧基; R5表示H，C1-C4烷基或氟; R6表示H，C1-C4烷基或芳基-C1-C4烷基; R 7表示H，C 1 -C 4烷基，芳基-C 1 -C 4烷基或-CH 2 -COOH; R8表示H，C1-C4烷基或-CH2-COOH; 条件是如果Z-B表示NCH 2 CH 2，NCOCH 2，NCH 2 CO或NCH 2 CH（OH），则W表示-CH 2 - ; 如果A表示O或S，则W表示-CH 2 - ; Y1，Y2，Y3和Y4中只有一个可以同时表示N个。

4. 发明申请

US20110039823A1 OXAZOLIDINONE ANTIBIOTICS 有权
标题翻译：奥沙利汀抗生素
公开(公告)号：US20110039823A1
公开(公告)日：2011-02-17
申请号：US12595720
申请日：2008-04-11
申请人： Daniel Bur , Christian Hubschwerlen , Georg Rueedi , Jean-Philippe Surivet , Cornelia Zumbrunn-Acklin
发明人： Daniel Bur , Christian Hubschwerlen , Georg Rueedi , Jean-Philippe Surivet , Cornelia Zumbrunn-Acklin
IPC分类号： A61K31/4375 , C07D471/04 , C07D413/14 , A61K31/517 , C07D417/14 , A61K31/4709 , A61K31/5415 , A61K31/496 , A61K31/551 , C07D491/056 , A61K31/5025 , A61P31/04
CPC分类号： C07D413/14 , C07D471/04 , C07D519/00
摘要： The invention relates to compounds of formula (I) wherein U, V, W, X, R1, R2, R3, R4, R5, R6, A, B, D, E, G, m, and n are as defined in the description, to pharmaceutically acceptable salts of such compounds for use in the manufacture of a medicament for the prevention or treatment of a bacterial infection. Certain compounds of formula (I) are new and are also part of this invention.
摘要翻译：本发明涉及式（I）化合物，其中U，V，W，X，R 1，R 2，R 3，R 4，R 5，R 6，A，B，D，E，G，m和n如描述了用于制备用于预防或治疗细菌感染的药物的这些化合物的药学可接受的盐。某些式（I）化合物是新的，也是本发明的一部分。

5. 发明申请

US20080280888A1 Antibiotics Derivatives 失效
公开(公告)号：US20080280888A1
公开(公告)日：2008-11-13
申请号：US11915179
申请日：2006-05-24
申请人： Daniel Bur , Christian Hubschwerlen , Jean-Philippe Surivet , Cornelia Zumbrunn-Acklin
发明人： Daniel Bur , Christian Hubschwerlen , Jean-Philippe Surivet , Cornelia Zumbrunn-Acklin
IPC分类号： A61K31/5415 , C07D417/02 , A61K31/538 , A61K31/428 , A61K31/542 , C07D513/04
CPC分类号： C07D277/64 , C07D409/12 , C07D413/12 , C07D417/12 , C07D513/04
摘要： The invention relates to antibiotic derivatives of formula I wherein: A represents —O—, S, —C(═O)—, —C(═NOR6)—; Z-B represents NCH2CH2, NCOCH2, NCH2CO, NCH2CH(OH), CHN(R8)CH2 or CHN(R8)CO; D represents binuclear heteroaryl; Y1 represents —CR1— or —N—, Y2 represents —CR2— or —N—, Y3 represents —CR3— or —N— and Y4 represents —CR4— or —N—; U represents —NH—, —O— or —S— and V represents —N— or —CH—; W represents —CH2—, —O— or —NR7—; R1 represents H, methyl, ethyl or halogen; R2, R3 and R4 each represent independently H, C1-C4 alkyl, halogen, or C1-C4 alkoxy; R5 represents H, C1-C4 alkyl or fluorine; R6 represents H, C1-C4 alkyl or aryl-C1-C4 alkyl; R7 represents H, C1-C4 alkyl, aryl-C1-C4 alkyl or —CH2—COOH; R8 represents H, C1-C4 alkyl or —CH2—COOH; with the provisos that if Z-B represents NCH2CH2, NCOCH2, NCH2CO or NCH2CH(OH), then W represents —CH2—; if A represents O or S, then W represents —CH2—; and only one or two of Y1, Y2, Y3 and Y4 can represent N at the same time.

6. 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。

7. 发明申请

US20120115841A1 BRIDGED SPIRO [2.4] HEPTANE DERIVATIVES AS ALX RECEPTOR AND/OR FPRL2 AGONISTS 有权
标题翻译： BRIDGED SPIRO [2.4]作为ALX受体和/或FPRL2激动剂的HEPTANE衍生物
公开(公告)号：US20120115841A1
公开(公告)日：2012-05-10
申请号：US13321372
申请日：2010-05-17
申请人： Daniel Bur , Olivier Corminboeuf , Sylvaine Cren , Corinna Grisostomi , Xavier Leroy , Sylvia Richard-Bildstein
发明人： Daniel Bur , Olivier Corminboeuf , Sylvaine Cren , Corinna Grisostomi , Xavier Leroy , Sylvia Richard-Bildstein
IPC分类号： A61K31/397 , C07D207/09 , C07D211/58 , C07C233/58 , C07D233/36 , C07D241/04 , C07D273/01 , C07D205/04 , C07D401/12 , C07D417/12 , C07D405/12 , C07D403/12 , C07D413/12 , C07D409/12 , A61K31/428 , A61K31/167 , A61K31/40 , A61K31/4468 , A61K31/341 , A61K31/4166 , A61K31/4184 , A61K31/415 , A61K31/5375 , A61K31/4439 , A61K31/506 , A61K31/422 , A61K31/4245 , A61K31/4965 , A61P11/00 , A61P29/00 , A61P37/08 , A61P31/18 , A61P9/00 , A61P25/00 , A61P37/00 , C07D235/14 , C07C233/62
CPC分类号： C07D295/13 , C07C233/58 , C07C233/59 , C07C233/60 , C07C233/61 , C07C233/63 , C07C255/29 , C07C2603/94 , C07D205/04 , C07D207/14 , C07D211/26 , C07D211/56 , C07D211/58 , C07D213/40 , C07D213/75 , C07D231/12 , C07D233/36 , C07D233/64 , C07D235/14 , C07D239/30 , C07D249/08 , C07D261/08 , C07D271/08 , C07D275/04 , C07D277/46 , C07D277/58 , C07D277/62 , C07D285/08 , C07D295/125 , C07D295/185 , C07D307/14 , C07D307/52 , C07D333/28 , C07D417/12
摘要： The present invention relates to bridged spiro[2.4]heptane derivatives of formula (I), wherein W, Y, Z, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds as ALX receptor and/or FPRL2 agonists for the treatment of inflammatory and obstructive airways diseases.
摘要翻译：本发明涉及式（I）的桥连螺[2.4]庚烷衍生物，其中W，Y，Z，R 1和R 2如说明书中所定义，它们的制备及其作为药物活性化合物作为ALX受体和/或 FPRL2激动剂用于治疗炎性和阻塞性气道疾病。

8. 发明申请

US20110034516A1 AMINOPYRAZOLE DERIVATIVES 有权
标题翻译：氨基吡唑衍生物
公开(公告)号：US20110034516A1
公开(公告)日：2011-02-10
申请号：US12808137
申请日：2008-12-12
申请人： Daniel Bur , Olivier Corminboeuf , Sylvaine Cren , Heinz Fretz , Corinna Grisostomi , Xavier Leroy , Julien Pothier , Sylvia Richard-Bildstein
发明人： Daniel Bur , Olivier Corminboeuf , Sylvaine Cren , Heinz Fretz , Corinna Grisostomi , Xavier Leroy , Julien Pothier , Sylvia Richard-Bildstein
IPC分类号： A61K31/4439 , C07D231/10 , C07D263/02 , A61K31/415 , A61K31/421 , A61P37/02 , A61P9/00 , A61P25/00 , A61K31/422
CPC分类号： C07D231/40 , C07D411/12 , C07D413/12
摘要： The invention relates to aminopyrazole derivatives of formula (I), wherein A, E, R1 and R2 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）的氨基吡唑衍生物，其中A，E，R 1和R 2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。

9. 发明申请

US20090088457A1 Primary Amines as Renin Inhibitors 审中-公开
标题翻译：主要胺类作为肾素抑制剂
公开(公告)号：US20090088457A1
公开(公告)日：2009-04-02
申请号：US12224590
申请日：2007-03-01
申请人： Olivier Bezencon , Daniel Bur , Olivier Corminboeuf , Corinna Grisostomi , Lubos Remen , Sylvia Richard-Bildstein , Thomas Weller
发明人： Olivier Bezencon , Daniel Bur , Olivier Corminboeuf , Corinna Grisostomi , Lubos Remen , Sylvia Richard-Bildstein , Thomas Weller
IPC分类号： A61K31/426 , C07D277/20 , C07D417/02 , A61K31/427 , A61P9/00 , A61P25/00 , A61P13/12 , A61K31/454 , C07D401/14 , C07D213/02
CPC分类号： C07D277/34 , C07D213/64 , C07D401/04 , C07D417/04
摘要： The invention relates to novel primary amine derivatives and the use thereof as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as inhibitors of renin.
摘要翻译：本发明涉及新型伯胺衍生物及其在制备药物组合物中作为活性成分的用途。本发明还涉及包括制备化合物的方法，含有一种或多种这些化合物的药物组合物，特别是其作为肾素抑制剂的用途的相关方面。

10. 发明申请

US20080064740A1 Novel Thiophene Derivatives 失效
公开(公告)号：US20080064740A1
公开(公告)日：2008-03-13
申请号：US11572801
申请日：2005-07-20
申请人： Martin Bolli , Daniel Bur , Martine Clozel , Walter Fischli , David Lehmann , Boris Mathys , Claus Mueller , Oliver Nayler , Michael Scherz , Thomas Weller
发明人： Martin Bolli , Daniel Bur , Martine Clozel , Walter Fischli , David Lehmann , Boris Mathys , Claus Mueller , Oliver Nayler , Michael Scherz , Thomas Weller
IPC分类号： A61K31/381 , A61P37/00 , C07D333/78
CPC分类号： C07D333/78 , C07D409/12
摘要： The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents.

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