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11. 发明公开

EP1768951A2 NON-NATURAL AMINO ACIDS 审中-公开
标题翻译：非天然氨基酸
公开(公告)号：EP1768951A2
公开(公告)日：2007-04-04
申请号：EP05790012.8
申请日：2005-06-17
申请人： MUSC Foundation For Research Development , Dix, Thomas A.
发明人： DIX, Thomas, A.
IPC分类号： C07C229/00 , C07C205/00 , C07C57/30 , C07D231/06
CPC分类号： C07C279/14 , A61K38/00 , C07C229/08 , C07C229/12 , C07C257/14 , C07D231/06 , C07D233/46 , C07D233/48 , C07D239/14 , C07K7/083
摘要： This invention relates to non-natural desamino alkyl amino acid compounds, methods of making, and peptides containing these compounds as their N-terminus moieties. A preferred example is neurotensin (8-13) in which the N terminus is an alpha desamino, alpha methyl N,N dimethyl homolysine residue.

12. 发明公开

EP1737811A1 CETP INHIBITORS 有权
标题翻译： CETP抑制剂
公开(公告)号：EP1737811A1
公开(公告)日：2007-01-03
申请号：EP05736159.4
申请日：2005-04-08
申请人： Merck & Co., Inc.
发明人： ALI, Amjad , BOHN, Joann , DENG, Qiaolin , LU, Zhijian , SINCLAIR, Peter, J. , TAYLOR, Gayle, E. , THOMPSON, Christopher, F. , QURAISHI, Nazia
IPC分类号： C07C205/00 , C07C229/00
CPC分类号： C07C271/20 , C07C233/18 , C07C271/16 , C07C271/22 , C07C279/08 , C07C311/04 , C07C311/08 , C07C317/32 , C07D209/08 , C07D213/40 , C07D213/64 , C07D213/65 , C07D213/68 , C07D213/89 , C07D215/12 , C07D215/26 , C07D217/02 , C07D217/14 , C07D261/08 , C07D271/06 , C07D307/52 , C07D307/79 , C07D333/20 , C07D333/22 , C07D333/28
摘要： Compounds of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula 1, A1 and A2 are each an aromatic ring, a 5-6-membered heterocyclic ring, an aromatic ring fused to a heterocyclic ring, a phenyl ring fused to a heterocyclic ring, or a cycloalkyl ring.

13. 发明公开

EP1554237A1 METHODS FOR SYNTHESIS OF ACYLOXYALKYL DERIVATIVES OF GABA ANALOGS 审中-公开
标题翻译： VERFAHREN ZUR SYNTHESE VON ACYLOXYALKYLDERIVATEN VON GABA-ANALOGA
公开(公告)号：EP1554237A1
公开(公告)日：2005-07-20
申请号：EP03757492.8
申请日：2003-06-11
申请人： Xenoport, Inc.
发明人： RAILLARD, Stephen, P. , ZHOU, Cindy, X. , YAO, Fenmei , MANTHATI, Suresh, Kumar , XIANG, Jia-Ning , GALLOP, Mark, A.
IPC分类号： C07C205/00 , C07C261/00 , C07C269/00 , C07C271/00
CPC分类号： C07C271/22 , C07C269/06 , C07C2601/14 , C07D309/06 , C07D335/02
摘要： The synthesis of 1-(acyloxy)-alkyl carbamates of GABA analogs from 1-haloalkyl carbamates of GABA analogs are described. Also described are new 1-haloalkyl carbamates of GABA analogs.
摘要翻译：本发明涉及结晶1 - {[（±）异丁酰氧基乙氧基）羰基]氨基甲基} -1-环己烷乙酸。

14. 发明公开

EP1336602A1 Nitrate prodrugs able to release nitric oxide in a controlled and selective way and their use for prevention and treatment of inflammatory, ischemic and proliferative diseases 审中-公开
标题翻译：硝酸盐的前药为一氧化氮以受控的和选择性的方式释放以及它们用于治疗炎性，缺血性和增殖性疾病的预防和治疗
公开(公告)号：EP1336602A1
公开(公告)日：2003-08-20
申请号：EP02425075.5
申请日：2002-02-13
申请人： Scaramuzzino, Giovanni
发明人： Scaramuzzino, Giovanni
IPC分类号： C07C205/00 , A61K31/00
CPC分类号： C07C291/02 , C07C401/00 , C07D221/20 , C07D231/12 , C07D231/56 , C07D261/08 , C07D311/30 , C07D311/72 , C07D333/20 , C07D401/12 , C07D487/04 , C07H5/06 , C07J41/0005 , C07J41/0038 , C07J41/005 , C07J41/0055 , C07J43/003 , C07J43/006 , C07J51/00 , C07J71/0031 , C07J73/003 , C07J73/005
摘要： New pharmaceutical compounds of general formula (I): F-(X) q where q is an integer from 1 to 5, preferably 1; -F is chosen among drugs described in the text, -X is chosen among 4 groups -M, -T, -V and -Y as described in the text.
The compounds of general formula (I) are nitrate prodrugs which can release nitric oxide in vivo in a controlled and selective way and without hypotensive side effects and for this reason they are useful for the preparation of medicines for prevention and treatment of inflammatory, ischemic, degenerative and proliferative diseases of musculoskeletal, tegumental, respiratory, gastrointestinal, genito-urinary and central nervous systems.
摘要翻译：通式（I）新的药物化合物：F（X）q其中q是从1至5的整数，优选1; -F是文中所述的药物选自，X是四组-M，-T，-V和Y如在文本中所描述中选择的。通式（I）的化合物是硝酸前药可以以受控的和选择性的方式和不降压的副作用并且由于这个原因它们是用于制备药物用于治疗炎性，缺血的预防和治疗有用的释放一氧化氮在体内肌肉骨骼，体被系统，呼吸系统，胃肠道，泌尿生殖系统和中枢神经系统退行性和增殖性疾病。

15. 发明公开

EP1165490A1 SUBSTITUTED 2-AMINOBENZAMIDE CASPASE INHIBITORS AND THE USE THEREOF 有权
标题翻译：取代的2- AMINOBENZAMIN蛋白酶抑制剂及其用途
公开(公告)号：EP1165490A1
公开(公告)日：2002-01-02
申请号：EP00917859.1
申请日：2000-03-15
申请人： Cytovia, Inc.
发明人： CAI, Sui, Xiong , WANG, Yan , WEBER, Eckard , MILLS, Gordon, B. , GREEN, Douglas, R.
IPC分类号： C07C229/00 , C07C69/74 , C07C205/00 , A01N37/10 , A01N37/12 , A01N37/00
CPC分类号： C07D333/38 , C07C271/22 , C07C271/24 , C07C271/28 , C07C2601/08 , C07C2601/14
摘要： The present invention is directed to novel 2-aminobenzamide thereof, represented by general Formula (I) where R1-R3, X and A-D are defined herein. The present invention also relates to the discovery that compounds having Formula (I) are potent inhibitors of caspases and apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.

16. 发明公开

EP1052968A1 $g(a)-AMIDES OF $i(L)-AMINO ACIDS AS FRAGRANCE PRECURSORS 有权
标题翻译： L-氨基酸THAN香料前体阿尔法 - 酰胺
公开(公告)号：EP1052968A1
公开(公告)日：2000-11-22
申请号：EP98961953.1
申请日：1998-12-07
申请人： THE GILLETTE COMPANY
发明人： SLIFE, Charles, W. , LANEY, Judith, Wolfe , GOLDMAN, Virginia, Streusand
IPC分类号： A61K7/32 , A61K7/06 , A61K7/15 , A61K6/00 , A61K7/00 , A61K7/46 , C07C205/00 , C07C207/00 , C07C229/00
CPC分类号： A61Q15/00 , A61K8/02 , A61K8/046 , A61K8/44 , A61K8/492 , A61K2800/57 , A61K2800/77 , A61Q13/00
摘要： Disclosed are α-amides of L-amino acids that produce fragrance or attenuate or mask malodor. In particular, glutamine and asparagine amides can be used in the invention. Such α-amides of L-amino acids are useful for generating pleasant fragrances or attenuating or masking malodor upon cleavage of the α-amides of L-amino acids by bacteria in axillae. The α-amides of L-amino acids can be incorporated into skin treatment compositions and personal care products, such as deodorants, body sprays and antiperspirants, and used in methods for producing fragrance or attenuating or masking malodor.

17. 发明公开

EP1047391A1 ALPHA-AMIDES OF L-AMINO ACIDS AS FRAGRANCE PRECURSORS 审中-公开
标题翻译：阿尔法 - 酰胺（L）氨基酸芳香剂
公开(公告)号：EP1047391A1
公开(公告)日：2000-11-02
申请号：EP98961952.3
申请日：1998-12-07
申请人： THE GILLETTE COMPANY
发明人： GOLDMAN, Virginia, Streusand , LANEY, Judith, Wolfe , SLIFE, Charles, W.
IPC分类号： A61K7/32 , A61K7/06 , A61K7/15 , A61K6/00 , A61K7/00 , A61K7/46 , C07C205/00 , C07C207/00 , C07C229/00
CPC分类号： A61Q13/00 , A61K8/44 , A61K2800/57 , A61Q15/00 , C07C233/50 , C07C233/63 , C07C233/83 , C07C235/52 , C07C2601/08
摘要： Disclosed are α-amides of L-amino acids that produce fragrance or attenuate or mask malodor. In particular, threonine amides, glycine amides, serine amides, and alanine amides can be used in the invention. Such α-amides of L-amino acids are useful for generating pleasant fragrances or attenuating or masking malodor upon cleavage of the α-amides of L-amino acids by bacteria in axillae. The α-amides of L-amino acids can be incorporated into skin treatment compositions and personal care products, such as deodorants, body sprays and antiperspirants, and used in methods for producing fragrance or attenuating or masking malodor.

18. 发明公开

EP0934248A4 PRODUCTION OF D,L-ASPARTIC ACID 失效
标题翻译： HERSTELLUNG VON D，L-ASPARAGINSÄURE
公开(公告)号：EP0934248A4
公开(公告)日：2000-02-02
申请号：EP97927843
申请日：1997-05-30
申请人： DONLAR CORP
发明人： MAZO GRIGORY YA , MAZO JACOB , VALLINO BARNEY JR , ROSS ROBERT J
IPC分类号： C07C227/08 , C07C229/24 , C07C205/00 , C07C207/00 , C07C229/00
CPC分类号： C07C227/08 , C07C229/24
摘要： The present invention is directed to a method for the production of D,L-aspartic acid. The method comprises reacting an unsatured dicarboxylic acid or anhydride such as maleic acid, fumaric acid, maleic anhydride or mixtures thereof with excess aqueous ammonia at an elevated temperature and pressure for a time sufficient to produce diammonium D,L aspartate. The diammonium D,L aspartate is then neutralized to D,L-aspartic acid; excess unreacted ammonia and various by-products may be recycled and re-used in the method, thereby minimizing waste and cost; i.e. the process is useful for a continuous production process which may be represented conveniently as a schematic block diagram wherein a pressurized reactor (10) receives a reactant admixture from feed tank (12), the reactants being fed subsequently to flash vessel (14) and then precipitator (16) where D,L-aspartic acid is produced upon neutralization, with dicarboxylic acid salts being recovered in a centrifuge (18) and dried in a drier (20). The D,L-aspartic acid may subsequently be used to make polyaspartic acid.
摘要翻译：本发明涉及生产D，L-天冬氨酸的方法。该方法包括使不饱和二羧酸或酸酐如马来酸，富马酸，马来酸酐或其混合物与过量的氨水在升高的温度和压力下反应足够的时间以产生二铵D，L-天冬氨酸盐。然后将二铵D，L-天冬氨酸中和成D，L-天冬氨酸; 过量的未反应的氨和各种副产品可以在该方法中再循环和再利用，从而最大限度地减少浪费和成本; 即该过程对于连续生产过程是有用的，其可以简单地表示为其中加压反应器（10）接收来自进料罐（12）的反应物混合物的示意性框图，反应物随后被供给至闪蒸器（14），并且然后在中和后产生D，L-天冬氨酸的沉淀器（16）与二羧酸盐在离心机（18）中回收并在干燥器（20）中干燥。 D，L-天冬氨酸可随后用于制造聚天冬氨酸。

19. 发明授权

EP0433449B1 SECOND-ORDER NONLINEAR OPTICAL ELEMENT 失效
标题翻译：非线性光学元件二阶。
公开(公告)号：EP0433449B1
公开(公告)日：1994-10-12
申请号：EP89907306.8
申请日：1989-06-27
申请人： TORAY INDUSTRIES, INC.
发明人： GOTOH, Tetsuya , TSUNEKAWA, Tetsuya , FUKUDA, Seiji , MATAKI, Hiroshi , EGAWA, Keiichi
IPC分类号： G02F1/35 , C07C205/00 , G02F1/03
CPC分类号： G02F1/3611 , C07C205/35
摘要： The invention relates to a high-performance nonlinear optical element showing a large secondary nonlinear optical effect and causing no problems as to stability and processability. It has at least one substantially optically smooth surface and contains monoclinic crystals of 4-hydroxy-3-methoxy-4'-nitrostilbene belonging to space group P2 and point group #4 and having at least one, substantially optically smooth surface.

20. 发明公开

EP0433449A4 SECONDARY NONLINEAR OPTICAL ELEMENT 失效
标题翻译：二次非线性光学元件
公开(公告)号：EP0433449A4
公开(公告)日：1992-01-08
申请号：EP89907306
申请日：1989-06-27
申请人： TORAY INDUSTRIES, INC.
发明人： GOTOH, TETSUYA , TSUNEKAWA, TETSUYA , FUKUDA, SEIJI , MATAKI, HIROSHI , EGAWA, KEIICHI
IPC分类号： C07C205/00 , C07C205/35 , G02F1/03 , G02F1/35 , G02F1/361
CPC分类号： G02F1/3611 , C07C205/35

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