公开(公告)号：EP2970224A1

公开(公告)日：2016-01-20

申请号：EP14722443.0

申请日：2014-03-14

申请人： Onyx Therapeutics, Inc.

发明人： MCMINN, Dustin ,  JOHNSON, Henry ,  BOWERS, Simeon ,  MOEBIUS, David, C.

IPC分类号： C07D405/12 ,  A61K31/336 ,  A61K31/404 ,  C07D409/12 ,  C07D303/32

CPC分类号： C07K5/0821 ,  A61K38/00 ,  A61K38/06 ,  C07D303/32 ,  C07D405/12 ,  C07D409/12 ,  C07K5/0202 ,  C07K5/0205 ,  C07K5/06026 ,  C07K5/0606 ,  C07K5/06069 ,  C07K5/06078 ,  C07K5/06113 ,  C07K5/06121 ,  C07K5/06139 ,  C07K5/06147 ,  C07K5/06173 ,  C07K5/06191 ,  C07K5/0806

摘要： Provided herein are tripeptide epoxy ketone protease inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula (X): and pharmaceutically acceptable salts and compositions including the same. The compounds and compositions provided herein may be used, for example, in the treatment of diseases including inflammation and neurodegenerative disease.

摘要翻译： 本文提供三肽环氧酮蛋白酶抑制剂，其制备方法，相关药物组合物及其使用方法。 例如，本文提供了式（X）的化合物及其药学上可接受的盐和包含它们的组合物。 本文提供的化合物和组合物可用于例如治疗包括炎症和神经变性疾病的疾病。

公开(公告)号：EP2319894A4

公开(公告)日：2013-06-12

申请号：EP09802800

申请日：2009-06-19

申请人： NISSAN CHEMICAL IND LTD

发明人： MIYAMOTO MISAO ,  MIYACHI NOBUHIDE ,  IWAMA TAKEHISA

IPC分类号： A61K9/70 ,  A23L29/20 ,  A61K9/18 ,  A61K47/10 ,  A61K47/18 ,  C07K5/062 ,  C07K5/078 ,  C07K5/10 ,  C07K5/103

CPC分类号： A61K47/22 ,  A61K9/0014 ,  A61K9/7007 ,  A61K47/10 ,  A61K47/183 ,  C07K5/06026 ,  C07K5/06052 ,  C07K5/06139 ,  C07K5/06147 ,  C07K5/1008

公开(公告)号：EP2391620A1

公开(公告)日：2011-12-07

申请号：EP10700508.4

申请日：2010-01-19

申请人： Bayer Pharma Aktiengesellschaft

发明人： VAKALOPOULOS, Alexandros ,  MEIBOM, Daniel ,  ALBRECHT-KÜPPER. Barbara ,  ZIMMERMANN, Katja ,  KELDENICH, Joerg ,  LERCHEN, Hans-Georg ,  NELL, Peter ,  SÜSSMEIER, Frank ,  KRENZ, Ursula

IPC分类号： C07D417/12 ,  C07D417/14 ,  C07K5/037 ,  C07K5/062 ,  A61K31/4439 ,  A61P3/06 ,  A61P3/10

CPC分类号： C07D417/14 ,  A61K47/64 ,  C07D417/12 ,  C07K5/0202 ,  C07K5/06026 ,  C07K5/06034 ,  C07K5/06086 ,  C07K5/06147 ,  C07K5/06165

摘要： The invention relates to new 6-alkylamine-substituted dicyanopyridine, amino acid ester prodrugs thereof, to a method for the production thereof, to the use thereof for treatment and/or prevention of illnesses and to the use thereof for producing pharmaceuticals for treatment and/or prevention of illnesses, preferably for treatment and/or prevention of cardiovascular illnesses.

公开(公告)号：EP2268657A2

公开(公告)日：2011-01-05

申请号：EP09723139.3

申请日：2009-03-18

申请人： The Henry M. Jackson Foundation for the Advancement of Military Medicine, Inc.

发明人： ARISPE, Nelson

IPC分类号： C07K7/06 ,  A61K38/08 ,  A61P25/28

CPC分类号： A61K38/05 ,  A61K38/06 ,  A61K38/07 ,  A61K38/08 ,  C07K5/06147 ,  C07K5/1024 ,  C07K14/4711 ,  G01N33/5041 ,  G01N33/5058 ,  G01N33/6872 ,  G01N33/6896 ,  G01N2333/4709 ,  G01N2500/00 ,  G01N2800/2821

摘要： The present disclosure relates to amyloid beta (Aβ) channels and the diseases and disorders caused by abnormal activity in these channels, such as Alzheimer's disease, Lewy body dementia, inclusion body myositis, or cerebral amyloid angiopathy. The disclosure provides compositions and methods that block Aβ channel activity and/or reduce Aβ-induced toxicity in a cell. Compositions comprised of compounds having histidine coordinating capacity are used in methods to prevent, reduce, or eliminate damage caused by Aβ ion channels.

摘要翻译： 本公开涉及淀粉样蛋白β（Aβ）通道以及由这些通道中的异常活性引起的疾病和病症，诸如阿尔茨海默氏病，路易体痴呆，包涵体肌炎或脑淀粉样血管病。 本公开提供了阻断细胞中Aβ通道活性和/或减少Aβ诱导的毒性的组合物和方法。 由具有组氨酸配位能力的化合物组成的组合物用于预防，减少或消除由Aβ离子通道引起的损伤的方法中。

公开(公告)号：EP1781596A1

公开(公告)日：2007-05-09

申请号：EP05770911.5

申请日：2005-07-12

申请人： Xenoport, Inc.

发明人： XU, Feng ,  GALLOP, Mark A. ,  SASIKUMAR, Vivek

IPC分类号： C07C237/12 ,  C07K5/062 ,  C07C323/60 ,  C07K5/068 ,  C07K5/072 ,  C07K5/078 ,  C07D233/54 ,  C07C237/20 ,  A61P25/00 ,  A61P25/06 ,  A61P25/08 ,  A61P25/28 ,  A61K38/05 ,  A61K31/16

CPC分类号： C07C323/60 ,  A61K38/00 ,  C07C229/22 ,  C07C237/12 ,  C07C237/20 ,  C07D233/64 ,  C07K5/06026 ,  C07K5/06043 ,  C07K5/06052 ,  C07K5/0606 ,  C07K5/06069 ,  C07K5/06086 ,  C07K5/06095 ,  C07K5/06113 ,  C07K5/06147 ,  C07K5/06165

摘要： The present invention provides propofol prodrugs, methods of making propofol prodrugs, pharmaceutical compositions of propofol prodrugs and methods of using propofol prodrugs and pharmaceutical compositions thereof to treat or prevent diseases or disorders such as migraine headache pain and post?chemotherapy or post?operative surgery nausea and vomiting.

公开(公告)号：EP1103560B1

公开(公告)日：2006-12-27

申请号：EP99931561.7

申请日：1999-07-27

申请人： SANTEN PHARMACEUTICAL CO., LTD.

发明人： NISHIMURA, Kazuo, Santen Pharmaceutical Co., Ltd ,  FUJIMURA, Ken-ichi, Santen Pharmaceutical Co., Ltd ,  MATSUMOTO, Junzo, Santen Pharmaceutical Co., Ltd ,  KOBAYASHI, Tadayuki, Santen Pharmaceutical Co.,Ltd

IPC分类号： C07K5/083 ,  C07D277/06 ,  A61K31/425 ,  A61K31/495 ,  A61K31/445 ,  C07K5/06 ,  A61K38/06 ,  A61K38/07

CPC分类号： C07K5/06078 ,  A61K38/00 ,  C07D277/06 ,  C07K5/0202 ,  C07K5/06052 ,  C07K5/06069 ,  C07K5/06113 ,  C07K5/06139 ,  C07K5/06147 ,  C07K5/0808 ,  C07K5/081 ,  C07K5/0819 ,  C07K5/0821

摘要： Novel thiazolidine derivatives which are useful as drugs. These thiazolidine derivatives are compounds represented by general formula (I) and salts thereof wherein R1 represents alkyl, hydroxy, alkoxy, alkoxyalkyl, phenyl, phenylalkyl, phenylalkoxy, phenoxy, phenoxyalkyl, amino, alkylamino or a non-aromatic heterocycle; R2 represents H or alkyl; R3 represents H, alkyl or phenyl; R4 represents H or alkyl; R5 represents alkyl, halogenoalkyl, hydroxy, alkoxy, phenyl, phenylalkoxy, phenoxy, carboxy, alkoxy, carbonyl, phenylalkoxycarbonyl or heteroaryl; A1 represents alkylene; and A2 represents alkylene.

公开(公告)号：EP1315738A4

公开(公告)日：2006-06-07

申请号：EP01968707

申请日：2001-09-07

申请人： GRYPHON THERAPEUTICS INC

发明人： BOTTI PAOLO ,  BRADBURNE JAMES A ,  KENT STEPHEN B H ,  LOW DONALD W

IPC分类号： C07K1/00 ,  C07K5/04 ,  A61K38/00 ,  C07K1/04 ,  C07K1/08 ,  C07K5/06 ,  C07K5/068 ,  C07K5/078 ,  C07K5/087 ,  C07K7/04 ,  C07K7/06 ,  C07K14/00 ,  C07K14/505 ,  C07K14/80 ,  C12N9/02

CPC分类号： C07K14/80 ,  C07K5/06026 ,  C07K5/06086 ,  C07K5/06147 ,  C07K5/0812 ,  C07K7/06

摘要： The invention is directed to methods and compositions for chemical ligation of components comprising a first component having a carboxythioester, and preferable an alpha -carboxythioester, moiety and a second component having an N-substituted, and preferably an N alpha -substituted, 2 or 3 carbon chain alkyl or aryl thiol to give a ligation product having an N-substituted amide bond at the ligation site. The reactants of the invention are chemoselective, and the alkyl or aryl thiol moiety is removable from the ligation product. Removal of the alkyl or aryl thiol gives a native amide bond at the ligation site. The methods and compositions of the invention are particularly useful for ligation of peptides and polypeptides. The ligation system of the invention is applicable to a wide variety of molecules, and thus can be exploited to generate peptides, polypeptides and other amino acid containing polymers having a native amide bond at the ligation site.

公开(公告)号：EP1553171A1

公开(公告)日：2005-07-13

申请号：EP03794067.3

申请日：2003-07-25

申请人： Ajinomoto Co., Inc.

发明人： YOKOZEKI, Kenzo, /o Ajinomoto Co., Inc. ,  SUZUKI, Sonoko, c/o Ajinomoto Co., Inc. ,  HARA, Seiichi, c/o Ajinomoto Co., Inc. ,  KATAYAMA, Satoshi, c/o Ajinomoto Co., Inc.

IPC分类号： C12N9/18 ,  C12N9/48 ,  C12P21/02

CPC分类号： C07K5/06026 ,  C07K5/06034 ,  C07K5/06043 ,  C07K5/06052 ,  C07K5/0606 ,  C07K5/06069 ,  C07K5/06078 ,  C07K5/06086 ,  C07K5/06095 ,  C07K5/06104 ,  C07K5/06113 ,  C07K5/06147 ,  C07K5/06156 ,  C07K5/06165 ,  C07K5/06191 ,  C07K5/0806 ,  C07K5/081 ,  C07K5/1008 ,  C07K7/06 ,  C12N9/18 ,  C12N9/48 ,  C12N9/93 ,  C12P21/02 ,  C12R1/01

摘要： The present invention relates to a novel enzyme that allows peptide to be produced easily, inexpensively and at high yield without going through a complex synthesis method. More particularly, the present invention provides a novel enzyme that catalyzes a peptide-producing reaction from a carboxy component and an amine component, a microbe that produces the enzyme, and a method for inexpensive production of peptides using this enzyme or microbe. The novel enzyme that efficiently produces peptide was discovered from a newly discovered microbe belonging to the genus Empedobacter, and a method was found that allows peptides to be produced inexpensively and easily.

摘要翻译： 本发明涉及一种新型酶做允许容易地产生肽，廉价且高收率，而无需通过复杂的合成方法去。 更具体地，本发明提供了一种新的酶做催化从的，微生物确实产生该酶，羧基成分和胺成分和廉价的生产使用这种酶或微生物肽的方法的肽生成反应。 该新型酶确实有效地产生从属于稳杆菌属新发现的微生物发现的肽，和其中发现做了方法允许廉价且容易地制造的肽。

公开(公告)号：EP1446665A2

公开(公告)日：2004-08-18

申请号：EP02774759.1

申请日：2002-10-30

申请人： Bayer HealthCare AG

发明人： LERCHEN, Hans-Georg ,  SIEGMUND, Hans-Ulrich ,  IMMLER, Dorian ,  SCHUMACHER, Andreas ,  AURIEL, Daniel

IPC分类号： G01N33/532

CPC分类号： C07D207/452 ,  C07D495/04 ,  C07K1/13 ,  C07K5/06026 ,  C07K5/06052 ,  C07K5/06113 ,  C07K5/06147 ,  C07K5/06165 ,  G01N33/58 ,  G01N2458/15 ,  Y10T436/24

摘要： The invention concerns isotopically coded affinity markers (ICAT) for mass spectrometric analysis of proteins, and the preparation and use of said markers.

公开(公告)号：EP0951471B1

公开(公告)日：2004-03-17

申请号：EP97954575.3

申请日：1997-12-16

申请人： WARNER-LAMBERT COMPANY LLC

发明人： DOHERTY, Annette, Marian ,  KALTENBRONN, James Stanley ,  LEONARD, Daniele, M. ,  MC NAMARA, Dennis, Joseph

IPC分类号： C07K5/078 ,  A61K38/05

CPC分类号： C07K5/06147 ,  A61K38/00

摘要： Novel inhibitors of protein farnesyltransferase enzymes are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in controlling tissue proliferative diseases, including cancer, restenosis, atherosclerosis, psoriasis, and endometriosis.