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1. 发明授权

EP2837629B1 METHOD FOR SYNTHESIZING SAPROPTERIN DIHYDROCHLORIDE 失效
标题翻译：方法合成沙丙蝶呤二盐酸盐
公开(公告)号：EP2837629B1
公开(公告)日：2017-03-22
申请号：EP12874086.7
申请日：2012-12-27
申请人： Asymchem Laboratories (Tianjin) Co., Ltd , Asymchem Life Science (Tianjin) Co., Ltd , Tianjin Asymchem Pharmaceutical Co., Ltd , Asymchem Laboratories (Fuxin) Co., Ltd , Jilin Asymchem Laboratories Co., Ltd
发明人： HONG, Hao , GAGE, James , CHEN, Chaoyong , LU, Jiangping , ZHOU, Yan , LIU, Shuangyong
IPC分类号： C07C49/17
CPC分类号： C07D475/04 , C07C209/62 , C07C221/00 , C07C225/06 , C07D239/50 , C07D303/48 , C07D317/26 , C07D317/28 , C07D317/32

2. 发明授权

EP1828224B1 COMPOSITIONS CONTAINING, METHODS INVOLVING, AND USES OF NON-NATURAL AMINO ACIDS AND POLYPEPTIDES 有权
标题翻译：组合物，使用进程和非天然氨基酸和多肽用途
公开(公告)号：EP1828224B1
公开(公告)日：2016-04-06
申请号：EP05855215.9
申请日：2005-12-21
申请人： Ambrx, Inc.
发明人： MIAO, Zhenwei , LIU, Junjie , NORMAN, Thea , DRIVER, Russell
IPC分类号： C07C22/00 , C07C227/00 , C07C2/00 , A61K38/00
CPC分类号： C07C225/10 , A61K31/198 , A61K38/17 , A61K47/08 , A61K47/10 , A61K47/34 , A61K47/60 , C07C229/36 , C07C237/32 , C07C251/28 , C07C251/54 , C07C251/60 , C07C251/86 , C07C323/63 , C07C2601/08 , C07D209/38 , C07D209/46 , C07D307/83 , C07D307/88 , C07D307/89 , C07D317/22 , C07D317/26 , C07D317/28 , C07D317/30 , C07D333/72 , C07K14/61 , C12P21/02 , G01N33/5008 , G01N33/68 , G01N33/6848 , G01N2500/00 , Y02A50/473 , Y02P20/55
摘要： Disclosed herein are non-natural amino acids and polypeptides that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The non-natural amino acids, by themselves or as a part of a polypeptide, can include a wide range of possible functionalities, but typical have at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Also disclosed herein are non-natural amino acid polypeptides that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such polypeptides. Typically, the modified non-natural amino acid polypeptides include at least one oximine, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid polypeptides and modified non-natural amino acid polypeptides, including therapeutic, diagnostic, and other biotechnology uses.

3. 发明公开

EP2850057A4 METHOD FOR THE PREPARATION OF THIADIAZOLES 审中-公开
标题翻译：用于生产噻二唑
公开(公告)号：EP2850057A4
公开(公告)日：2016-01-27
申请号：EP13790539
申请日：2013-05-17
申请人： AMGEN INC
发明人： BERCOT ERIC A , BIO MATTHEW , CHAN JOHANN , COLYER JOHN , FANG YUANQING , MENNEN STEVEN , MILBURN ROBERT R , TEDROW JASON , RIAHI BABAK
IPC分类号： C07D317/26 , C07D417/04
CPC分类号： C07D317/26 , C07D317/72 , C07D417/04

4. 发明公开

EP2850057A1 METHOD FOR THE PREPARATION OF THIADIAZOLES 审中-公开
标题翻译：用于生产噻二唑
公开(公告)号：EP2850057A1
公开(公告)日：2015-03-25
申请号：EP13790539.4
申请日：2013-05-17
申请人： Amgen Inc.
发明人： BERCOT, Eric A. , BIO, Matthew , CHAN, Johann , COLYER, John , FANG, Yuanqing , MENNEN, Steven , MILBURN, Robert R. , TEDROW, Jason , RIAHI, Babak
IPC分类号： C07D20060101
CPC分类号： C07D317/26 , C07D317/72 , C07D417/04
摘要： The present invention relates to processes for preparing protected glyceraldehydes, such as (hydroxy)methanesulfonates. In addition, the invention relates to thiadiazoles, particularly 3-diooxolanyl-thiadiazoles.

5. 发明公开

EP2848612A1 METHOD FOR PRODUCING A SUBSTITUTED BENZOIC ACID COMPOUND 有权转让
标题翻译：生产取代的苯甲酸化合物的方法
公开(公告)号：EP2848612A1
公开(公告)日：2015-03-18
申请号：EP13788182.7
申请日：2013-04-30
申请人： Ishihara Sangyo Kaisha, Ltd.
发明人： JONISHI, Hisayoshi , OKAMOTO, Tomohiro , ADACHI, Norio , ISOGAI, Akihiko , JUKUROGI, Tatsuya , KONISHI, Hideaki , FUKUI, Fumihiro
IPC分类号： C07D317/22 , C07D319/06
CPC分类号： C07D319/06 , C07C317/22 , C07D317/22 , C07D317/26
摘要： To provide an industrial method for producing a substituted benzoic acid compound useful as an intermediate of pharmaceutical and agricultural chemicals with high purity and high yield.
A compound represented by the formula (II):

(wherein Q is a 5- or 6-membered saturated heterocyclic group (the heterocyclic group may be substituted by alkyl) containing one or two of at least one type of hetero atom selected from the group consisting of an oxygen atom and a sulfur atom, or dialkoxymethyl, T is trifluoromethyl, nitro, cyano, -SOA 1 , -SO 2 A 1 , -PO(OA 1 )(OA 2 ),-COA 1 , -CO 2 A 1 or -CONA 1 A 2 , each of A 1 and A 2 which are independent of each other, is a hydrogen atom, alkyl or haloalkyl, X is halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio, alkylsulfinyl, haloalkylsulfinyl, alkylsulfonyl, haloalkylsulfonyl, dialkylaminosulfonyl, di(haloalkyl)aminosulfonyl, nitro or cyano, Y is a chlorine atom, a bromine atom or an iodine atom, and n is an integer of from 1 to 6), carbon monoxide and a compound represented by the formula R-OH (wherein R is alkyl) are reacted, followed by hydrolysis to obtain a compound represented by the formula (I):

wherein Q, T, X and n are as defined above.
摘要翻译：本发明提供一种工业方法，用于制备高纯度和高收率的用作医药和农药中间体的取代苯甲酸化合物。式（II）所示的化合物，式中，Q表示5或6元的饱和杂环基（该杂环基可以被烷基取代），该杂环基中含有1或2个选自其由氧原子和硫原子或二烷氧基甲基组成，T是三氟甲基，硝基，氰基，-SOA1，-SO2A1，-PO（OA1）（OA2）， - COA1，-CO2A1或-CONA1A2，各自为A1和A2 烷基或卤代烷基，X是卤素，烷基，卤代烷基，烷氧基，卤代烷氧基，烷硫基，卤代烷硫基，烷基亚磺酰基，卤代烷基亚磺酰基，烷基磺酰基，卤代烷基磺酰基，二烷基氨基磺酰基，氰基，Y是氯原子，溴原子或碘原子，n是1至6的整数），一氧化碳和由式R-OH（其中R为烷基）表示的化合物反应，随后通过水解得到式（I）代表的化合物：其中Q，T，X和n是a 如上所述。

6. 发明公开

EP2666771A1 Synthesis of Aminocyclopentanetriol Derivatives 审中-公开
标题翻译：合成氨基环戊烷三醇衍生物
公开(公告)号：EP2666771A1
公开(公告)日：2013-11-27
申请号：EP12169182.8
申请日：2012-05-24
申请人： LEK Pharmaceuticals d.d.
发明人： Sterk, Damjan , Casar Zdenko
IPC分类号： C07D317/26
CPC分类号： C07D317/26
摘要： The present invention relates to the field of organic synthesis and describes the synthesis of specific intermediates suitable for the preparation of triazolopyrimidine compounds such as ticagrelor.
The present invention provides in particular a process for the preparation of a compound of formula V

comprising:
a) providing a compound of formula IV

, and
b) reducing the compound of formula IV with activated zinc in the presence of copper to give the compound of formula V.
摘要翻译：本发明涉及有机合成领域，并描述了适用于三唑并嘧啶化合物如替卡格雷的制备的特定中间体的合成。本发明特别提供制备式V化合物的方法，其包括：a）提供式IV的化合物，和b）在铜的存在下用活化的锌还原式IV的化合物，得到公式五

7. 发明公开

EP2399893A3 Compositions containing, methods involving, and uses of non-natural amino acids and polypeptides 有权
标题翻译：组合物及其使用的方法和非天然氨基酸和多肽使用
公开(公告)号：EP2399893A3
公开(公告)日：2012-08-08
申请号：EP11177567.2
申请日：2005-12-21
申请人： Ambrx, Inc.
发明人： Miao, Zhenwei , Liu, Junjie , Norman, Thea , Driver, Russell
IPC分类号： C07C22/00 , C07C227/00 , C07C2/00 , A61K38/00 , C07C251/28 , C07D307/83 , C07D307/88 , C07D307/89 , C07D317/22 , C07D317/26 , C07D317/28 , C07D317/30 , C07D333/72 , C07C229/36 , C07C237/32 , C07C251/54 , C07C251/60 , C07C251/86 , C07C323/63 , C07D209/38
CPC分类号： C07C225/10 , A61K31/198 , A61K38/17 , A61K47/08 , A61K47/10 , A61K47/34 , A61K47/60 , C07C229/36 , C07C237/32 , C07C251/28 , C07C251/54 , C07C251/60 , C07C251/86 , C07C323/63 , C07C2601/08 , C07D209/38 , C07D209/46 , C07D307/83 , C07D307/88 , C07D307/89 , C07D317/22 , C07D317/26 , C07D317/28 , C07D317/30 , C07D333/72 , C07K14/61 , C12P21/02 , G01N33/5008 , G01N33/68 , G01N33/6848 , G01N2500/00 , Y02A50/473 , Y02P20/55
摘要： Disclosed herein are non-natural amino acids and polypeptides that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The non-natural amino acids, by themselves or as a part of a polypeptide, can include a wide range of possible functionalities, but typical have at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Also disclosed herein are non-natural amino acid polypeptides that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such polypeptides. Typically, the modified non-natural amino acid polypeptides include at least one oximine, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid polypeptides and modified non-natural amino acid polypeptides, including therapeutic, diagnostic, and other biotechnology uses.
摘要翻译：公开在可用于制备寻求非天然氨基酸和多肽的非天然氨基酸和多肽也包括至少一个非天然氨基酸，和方法。非天然氨基酸，自身或作为多肽的部分，可以包括宽范围的可能功能性的，但典型的具有至少一个肟，羰基，二羰基，和/或羟胺基团。因此游离缺失盘的都是非天然氨基酸多肽没有被翻译后修饰的。此外，用于实现寻求修改提纯搜索多肽的方法，和方法。典型地，经修饰非天然氨基酸多肽包含至少一个氧肟，羰基，二羰基，和/或羟胺基团。进一步游离缺失光盘是使用搜索非天然氨基酸多肽和经修饰非天然氨基酸多肽，包括治疗，诊断和其它生物技术使用的方法。

8. 发明公开

EP2330908A4 FLUORESCENT CDK INHIBITORS FOR TREATMENT OF CANCER 审中-公开
标题翻译：荧光CDK抑制剂用于癌症治疗
公开(公告)号：EP2330908A4
公开(公告)日：2011-11-23
申请号：EP09807430
申请日：2009-08-17
申请人： UNIV GEORGETOWN
发明人： YENUGONDA VENKATA MAHIDHAR , BROWN MILTON L
IPC分类号： A01N43/90 , A61K31/4164 , A61K31/52 , A61K49/00 , C07D209/14 , C07D233/72 , C07D317/26 , C07D473/16
CPC分类号： A61K31/52 , A61K31/4164 , A61K49/0021 , A61K49/0052 , C07D209/14 , C07D233/72 , C07D317/26 , C07D473/16

9. 发明公开

EP2331093A1 COMPOUNDS, COMPOSITIONS AND METHODS FOR REDUCING TOXICITY AND TREATING OR PREVENTING DISEASES 审中-公开
标题翻译：化合物，组合物和方法降低毒性和加工或预防疾病
公开(公告)号：EP2331093A1
公开(公告)日：2011-06-15
申请号：EP09810596.8
申请日：2009-08-27
申请人： The Trustees of Columbia University in the City of New York , Sloan Kettering Institute For Cancer Research
发明人： DANISHEFSKY, Samuel, J. , CHOU, Ting-Chao , LEI, Xiaoguang , YUN, Heedong , NG, Fay , HARTUNG, John , SAMES, Dalibor
IPC分类号： A61K31/34
CPC分类号： C07C33/048 , A61K31/047 , A61K31/075 , A61K31/165 , A61K31/196 , A61K31/337 , A61K31/343 , A61K31/357 , A61K31/4192 , A61K31/427 , A61K31/661 , A61K31/675 , A61K31/7048 , A61K45/06 , C07B2200/07 , C07C33/05 , C07C33/14 , C07C33/30 , C07C43/315 , C07C49/24 , C07C2601/02 , C07C2601/14 , C07D249/04 , C07D317/16 , C07D317/18 , C07D317/20 , C07D317/22 , C07D317/24 , C07D317/26 , C07D317/28 , C07D317/30 , A61K2300/00
摘要： The present invention provides compounds of Formula (I), compositions comprising an effective amount of a Compound of Formula (I), optionally with chemotherapeutic drug, such as a tubulin-binding drug, and methods of their use for reducing the toxicity of cytotoxic agents, for example chemotherapy agents, treating or preventing cancer or a neurotrophic disorder, inducing a chemoprotective phase II enzyme, DNA, or protein synthesis, enhancing the immune system, treating inflammation, improving and enhancing general health or well-being, and methods for making Compounds of Formula (I).

10. 发明公开

EP2279196A2 COMPOUNDS INCLUDING AN ANTI-INFLAMMATORY PHARMACORE AND METHODS OF USE 有权
标题翻译：随着对使用消炎药物CORE和方法链接
公开(公告)号：EP2279196A2
公开(公告)日：2011-02-02
申请号：EP09755580.9
申请日：2009-04-20
申请人： Reata Pharmaceuticals, Inc.
发明人： O'BRIAN, Patrick, M. , ANDERSON, Eric , BOLTON, Gary, L. , FERGUSON, Deborah, A. , JIANG, Xin , KRAL, Robert, M., Jr. , VISNICK, Melean
IPC分类号： C07J41/00 , C07J71/00 , C07C255/46 , C07C255/47 , A61K31/565 , A61K31/58 , A61P29/00 , A61P35/00 , A61P9/00 , A61P25/00
CPC分类号： C07C255/46 , C07C2601/16 , C07D311/74 , C07D317/26 , C07D493/10 , C07F7/1856 , C07J21/003 , C07J41/0055 , C07J41/0094 , C07J53/001 , C07J71/0005
摘要： This invention provides novel compounds comprising the following anti-inflammatory pharmacore: wherein X, R1 and R2 are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
摘要翻译：本发明提供了包含以下的抗炎药物核心的新的化合物：worin X，R1和R2中所定义。所以提供了药物组合物，试剂盒和制造包含测试化合物，方法和制备所述化合物的有用的中间体的制品，以及使用该化合物和组合物的方法。

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