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51. 发明公开

EP2513104A1 ANTI PARASITIC DIHYDROAZOLE COMPOUNDS AND COMPOSITIONS COMPRISING SAME 有权转让
标题翻译： Z IT UNG EN IT IT IT IT IT IT IT IT IT IT IT
公开(公告)号：EP2513104A1
公开(公告)日：2012-10-24
申请号：EP10796566.7
申请日：2010-12-16
申请人： Merial Limited
发明人： LE HIR DE FALOIS, Loic, Patrick , LEE, Hyoung, Lk , WILKINSON, Douglas, Edward , BECK, Brent, Christopher
IPC分类号： C07D471/04 , A01N43/90 , A61K31/437 , A01P5/00 , A01P7/04 , A61P33/00
CPC分类号： C07D471/04 , A01N43/80 , A01N43/90 , A61K31/365 , A61K31/437 , A61K31/495 , A61K38/05 , A61K45/06 , C07K5/06 , A61K2300/00
摘要： The present invention relates to novel dihydroazole of formula (I) and salts thereof: Wherein R
1 , A
1 , A
2 , G, X and Y are as defined in the description, compositions thereof, processes for their preparation and their uses to prevent or treat parasitic infections or infestations in animals and as pesticides.
摘要翻译：本发明涉及包含式（I）的二氢唑及其盐的组合物：其中R 1，A 1，A 2，G，X和Y如说明书中所定义，其组合物，其制备方法及其用途预防或治疗动物和农药中的寄生虫感染或侵染。

52. 发明公开

EP2476691A1 METHOD FOR MANUFACTURING A LIPIDIC PEPTIDE COMPOUND 有权转让
标题翻译： VERFAHREN ZUR HERSTELLUNG EINER LIPID-PEPTID-VERBINDUNG
公开(公告)号：EP2476691A1
公开(公告)日：2012-07-18
申请号：EP10813843.9
申请日：2010-09-07
申请人： Nissan Chemical Industries, Ltd.
发明人： KAKIUCHI, Nobuyuki , SHOJI, Takeaki , HIRASADA, Kazuki , MATSUMOTO, Keigo , YAMAGUCHI, Hiroki
IPC分类号： C07K5/062 , C07K1/02
CPC分类号： A61K47/48046 , A61K38/05 , A61K47/543 , C07K1/026 , C07K1/107 , C07K1/1072 , C07K1/1075 , C07K5/06 , C07K5/06026 , C07K5/06043 , C07K5/06052
摘要： There is provided a practical method for preparing lipopeptide compounds, which method is capable of inexpensive mass production without requiring complicated operations. The lipopeptide compound of formula (3):

is produced by reacting an ester compound of formula (1):

with an α-amino acid compound of formula (2):

in the presence of a base and within a solvent containing a nonpolar organic solvent.
摘要翻译：提供了制备脂肽化合物的实用方法，该方法能够在不需要复杂操作的情况下廉价地批量生产。式（3）的脂肽化合物：通过使式（1）的酯化合物与式（2）的±氨基酸化合物在碱的存在下和含有非极性有机溶剂的溶剂。

53. 发明公开

EP2346882A1 DERIVATIVES OF 1-AMINO-2-CYCLOBUTYLETHYLBORONIC ACID 有权转让
标题翻译：衍生物1-氨基-2-环己基四氢呋喃
公开(公告)号：EP2346882A1
公开(公告)日：2011-07-27
申请号：EP09789372.1
申请日：2009-09-25
申请人： Millennium Pharmaceuticals, Inc.
发明人： FLEMING, Paul, E. , LI, Jing
IPC分类号： C07F5/02 , A61K31/69 , A61K35/00
CPC分类号： C07F5/025 , C07F5/04 , C07K5/06 , C07K5/06078 , C07K5/08
摘要： The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
摘要翻译：本发明提供了可用作蛋白酶体抑制剂的新型化合物。本发明还提供包含本发明化合物的药物组合物和使用该组合物治疗各种疾病的方法。

54. 发明公开

EP2344516A1 PSEUDOPROLINE DIPEPTIDES 有权
标题翻译：伪麻黄碱二萜
公开(公告)号：EP2344516A1
公开(公告)日：2011-07-20
申请号：EP09783513.6
申请日：2009-09-29
申请人： F. Hoffmann-La Roche AG
发明人： HILDBRAND, Stefan
IPC分类号： C07K1/02 , C07K5/06 , C07K5/062
CPC分类号： C07K1/02 , C07D263/06 , C07K5/06 , C07K5/06069 , Y02P20/55
摘要： Disclosed is a process for the manufacture of pseudo proline dipeptides of the formula wherein R
1 is a side chain of an alpha amino acid, R
2 is an amino protecting group and R
3 and R
4 are independently selected from hydrogen, or C
1-4 -alkyl, with the proviso that not both R
3 and R
4 are hydrogen R
5 is hydrogen or methyl starting from an amino acid derivative of the formula wherein R
1 and R
2 are as above. Pseudo proline dipeptides can be used as reversible protecting groups for Ser, Thr and Cys and thus are versatile tools in peptide chemistry.
摘要翻译：本发明公开了制备下式的假脯氨酸二肽的方法，其中R 1是α氨基酸的侧链，R 2是氨基保护基，R 3和R 4独立地选自氢或C 1- 条件是不是R 3和R 4都是氢，R 5是氢或甲基，起始于下式的氨基酸衍生物，其中R 1和R 2如上所述。假脯氨酸二肽可用作Ser，Thr和Cys的可逆保护基，因此是肽化学中的通用工具。

55. 发明公开

EP2293847A1 DEPSIPEPTIDES AND THEIR THERAPEUTIC USE 有权
标题翻译：酯肽及其治疗用途
公开(公告)号：EP2293847A1
公开(公告)日：2011-03-16
申请号：EP09750137.3
申请日：2009-05-22
申请人： Karus Therapeutics Limited
发明人： SHUTTLEWORTH, Stephen Joseph , SILVA, Franck Alexandre , TOMASSI, Cyrille Davy , CECIL, Alexander Richard Liam , HILL, Thomas James
IPC分类号： A61P35/00 , C07K5/02
CPC分类号： C07K5/06 , C07K5/06026 , C07K5/06139 , Y02P20/55
摘要： Compounds of the invention have Structure (III) or (IV) or a pharmaceutically acceptable salt thereof, wherein: R
1 , R
2 , R
3 , R
4 , R
5 , R
6 , R
7 , and R
9 are the same or different and represent hydrogen or natural or unnatural amino acid side-chain moiety; each R
10 is the same of different and represents hydrogen or C
1 -C
6 alkyl, C
2 -C
6 alkenyl or C
2 -C
6 alkynyl; Pr is hydrogen or an alcohol protecting group; R
8 represents -CR
11 R
11 -CR
11 R
11 -(CH
2 )
n -R
12, CR
11 =CR
11 -(CH
2 )
n -R
12, or -C≡C-(CH
2 )n-R
12 ; R
11 is hydrogen, C
1 -C
6 alkyl, aryl, C
2 -C
6 alkenyl, C
2 -C
6 alkynyl or heteroaryl; R
12 is a linear or cyclic metal-chelating moiety; and n is an integer between 0 and 7, with the proviso that R
12 is not -SH or -SPr
2, wherein Pr
2 is a thiol protecting group.

56. 发明授权

EP2038295B1 PSEUDO PROLINE DIPEPTIDES 有权
标题翻译： PSEUDOPROLINDIPEPTIDE
公开(公告)号：EP2038295B1
公开(公告)日：2011-02-09
申请号：EP07730209.9
申请日：2007-06-18
申请人： F.Hoffmann-La Roche AG
发明人： AMMANN, Thomas , GOETZOE, Stephan , THERN, Bernd , WELZ, Sandra , WOLTER, Klaus-Juergen
IPC分类号： C07K1/02 , C07K1/00 , C07K1/06 , C07K5/06
CPC分类号： C07K1/02 , C07K1/006 , C07K1/065 , C07K5/06 , C07K5/06069 , Y02P20/55
摘要： Disclosed is a three step process for the manufacture of pseudo proline dipeptides of the formula (I) wherein R1 is a side chain of an alpha amino acid , R2 is an amino protecting group and R3 and R4 are independently selected from hydrogen or C1-4-alkyl, R5 is hydrogen or methyl starting from an amino acid derivative of the formula (II) wherein R1 and R2 are as above. Pseudo proline dipeptides can be used as reversible protecting groups for Ser, Thr and Cys and thus are versatile tools in peptide chemistry.

57. 发明公开

EP2241564A1 3,8-DIAMINOTETRAHYDROQUINOLINE DERIVATIVE 有权
标题翻译： 3,8-二氨基四氢喹喔啉衍生物
公开(公告)号：EP2241564A1
公开(公告)日：2010-10-20
申请号：EP09707360.5
申请日：2009-02-06
申请人： Zeria Pharmaceutical Co., Ltd.
发明人： WATANABE, Takeshi , TERAUCHI, Masaru , NAGASAWA, Masaaki , TANAKA, Kouichirou , WASHIDUKA, Masataka
IPC分类号： C07D401/14 , A61K31/4709 , A61K38/00 , A61P3/00 , A61P9/04 , A61P11/00 , A61P29/00 , A61P31/04 , A61P43/00 , C07D215/38 , C07D401/04 , C07D409/14 , C07K5/06
CPC分类号： C07D401/04 , C07D401/06 , C07D401/14 , C07D405/06 , C07D409/14 , C07K5/06 , C07K5/06034 , C07K5/0606 , C07K5/06078 , C07K5/06156
摘要： To provide a compound which has a potent agonistic activity on GHS-R and which is useful as a therapeutic agent for systemic wasting diseases such as cachexia.
A 3,8-diaminotetrahydroquinoline derivative represented by formula (la) (wherein X represents CH 2 , C=O, CH-OR, CH-SR, or CH-NRR'; m is a number of 1 or 2; Ar represents a phenyl group, a naphthyl group, a 5-membered or 6-membered aromatic heterocyclic group having one or two elements selected from S, N, and O, or a similar group; R 1 and R 2 , which may be identical to or different from each other, each represent a hydrogen atom or a methyl group; R 3 represents a C1 to C6 alkyl group or a similar group; n is a number of 0 or 1; R 4 and R 5 , which may be identical to or different from each other, each represent a hydrogen atom, or a C1 to C6 alkyl group, etc.; and R 6 , R 7 , R, and R', which may be identical to or different from one another, each represent a hydrogen atom or a C1 to C6 alkyl group), or a salt thereof.
摘要翻译：提供一种对GHS-R具有强效激动活性并且可用作全身性消耗性疾病如恶病质的治疗剂的化合物。由式（Ia）表示的3,8-二氨基四氢喹啉衍生物（其中X代表CH 2，C = O，CH-OR，CH-SR或CH-NRR'; m是1或2的数; Ar代表苯基基团，萘基，具有选自S，N和O中的一种或两种元素或类似基团的5元或6元芳族杂环基; R 1和R 2可彼此相同或不同各自表示氢原子或甲基; R 3表示C 1 -C 6烷基或类似基团; n是0或1的数; R 4和R 5可彼此相同或不同，各自表示氢原子或C1〜C6烷基等; R6，R7，R，R'可以相同也可以不同，表示氢原子或C1〜C6烷基）或其盐。

58. 发明公开

EP2189536A1 Rapid FRET based anthrax diagnosis 审中-公开
标题翻译： Schnelle炭疽诊断FRET基础
公开(公告)号：EP2189536A1
公开(公告)日：2010-05-26
申请号：EP08169548.8
申请日：2008-11-20
申请人： Nederlandse Organisatie voor toegepast-natuurwetenschappelijk onderzoek TNO
发明人： Bikker, Floris Jacob , Kaman-van Zanten, Wendy Esmeralda
IPC分类号： C12Q1/04 , C07K7/06 , C07K5/06 , C12Q1/37 , C07K5/08 , C07K5/10
CPC分类号： C12Q1/04 , C07K5/0207 , C07K5/06 , C07K5/06043 , C07K5/08 , C07K5/1013 , C07K7/06 , C12Q1/37 , G01N2333/32
摘要： The invention comprises a substrate for detection of micro-organisms, wherein said substrate comprises a set of molecular markers linked to a di, tri- or tetrapeptide consisting of amino acids X1 and X2, X1, X2 and X3 or X1, X2, X3 and X4, respectively, in which one of them, for example X1 is a D-amino acid and the others, for example X2, X3 and X4 may be any D- or L-amino acid. Said substrate preferably is used for the detection of Bacillus anthracis and preferably a set of molecular markers linked to a dipeptide or tripeptide consisting of two amino acids X1 and X2 or three amino acids X1, X2 and X3. respectively, in which either
- one of X1, X2 and X3 is DLeu and one of the others is any L- or D-amino acid, preferably Leu, or
- one of X1, X2 and X3 is a D-amino acid and one of the others is preferably Leu.
The invention further comprises methods for detection of micro-organisms, specifically Bacillus anthracis , with the substrates of the invention.
The preferred substrates are, for example,
Ac-NH-Cys(S-Ac)-Leu-(D)Leu-Cys(S-Ac)-OH
and
FITC-Ahx-(D)Leu-Leu-Lys-DABCYL.
摘要翻译：本发明包括用于检测微生物的底物，其中所述底物包含一组连接于由氨基酸X1和X2，X1，X2和X3或X1，X2，X3组成的二肽，三肽或四肽的分子标记， X4，其中一个，例如X1是D-氨基酸，而其它的，例如X2，X3和X4可以是任何D-或L-氨基酸。所述底物优选用于检测炭疽芽孢杆菌，优选用于与由两个氨基酸X1和X2或三个氨基酸X1，X2和X3组成的二肽或三肽连接的一组分子标记。其中X1，X2和X3之一是DLeu，其中之一是任何L-或D-氨基酸，优选Leu，或 - X1，X2和X3之一是D-氨基酸，一个其他的优选为Leu。本发明还包括用本发明的底物检测微生物，特别是炭疽芽孢杆菌的方法。优选的底物是例如Ac-NH-Cys（S-Ac）-Leu-（D）Leu-Cys（S-Ac）-OH和FITC-Ahx-（D）Leu-Leu-Lys-DABCYL。

59. 发明公开

EP2079309A1 SMAC MIMETIC DIMERS AND TRIMERS USEFUL AS ANTI-CANCER AGENTS 无效
标题翻译： MIME TABLES SMAC二聚体和三聚体的抗癌药
公开(公告)号：EP2079309A1
公开(公告)日：2009-07-22
申请号：EP08745697.6
申请日：2008-04-11
申请人： Joyant Pharmaceuticals, Inc.
发明人： HANSON, Gunnar , SUN, Haizhou
IPC分类号： A01N43/76 , A61K31/42
CPC分类号： A61K38/06 , A61K38/05 , A61K45/06 , C07D207/16 , C07D403/14 , C07D409/14 , C07K5/06 , C07K5/08
摘要： The invention provides small molecule mimics of the SMAC peptide that are dimer-like or trimer-like compounds having two or three amide-containing domains connected by a linker. These compounds are useful to promote apoptosis. The invention includes pharmaceutical compositions comprising such compounds and methods to use them to treat conditions including cancer and autoimmune disorders.

60. 发明公开

EP2041157A1 PEPTIDE DERIVATIVES WITH THERAPEUTIC ACTIVITY 有权
标题翻译：具有治疗作用的肽衍生物
公开(公告)号：EP2041157A1
公开(公告)日：2009-04-01
申请号：EP07734839.9
申请日：2007-06-15
申请人： Flamma S.P.A.
发明人： NEGRISOLI, Gianpaolo , CANEVOTTI, Renato
IPC分类号： C07K5/06 , A61K38/05
CPC分类号： A61K31/4172 , A61K38/00 , C07D233/64 , C07K5/06 , C07K5/06026 , C07K5/06078
摘要： Dipeptide compounds containing a histidine residue proved to have interesting blocking activity on secondary products from lipid oxidative stress, in particular on unsaturated aldehydes such as malondialdehyde and hydroxynonenal, which are known to contribute to the inset of quite a number telles que des maladies of chronic pathologies such as neurodegenerative, inflammatory chronic, cardiovascular diseases, diabetes complications and cataract.

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