公开(公告)号：US10934306B2

公开(公告)日：2021-03-02

申请号：US16715602

申请日：2019-12-16

申请人： ENANTA PHARMACEUTICALS, INC.

发明人： Yao-Ling Qiu ,  Xuri Gao ,  Wei Li ,  Hui Cao ,  Meizhong Jin ,  Jorden Kass ,  Xiaowen Peng ,  Yat Sun Or

IPC分类号： C07D493/08 ,  C07C317/44 ,  C07C323/62 ,  A61K31/167 ,  A61K31/18 ,  A61K31/196 ,  A61K31/215 ,  A61K31/223 ,  A61K31/277 ,  A61K31/325 ,  A61K31/335 ,  A61K31/336 ,  A61K31/341 ,  A61K31/351 ,  A61K31/357 ,  A61K31/365 ,  A61K31/39 ,  A61K31/401 ,  A61K31/41 ,  A61K31/415 ,  A61K31/416 ,  A61K31/4164 ,  A61K31/421 ,  A61K31/426 ,  A61K31/439 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4409 ,  A61K31/4425 ,  A61K31/445 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/655 ,  C07B59/00 ,  C07C235/56 ,  C07C311/53 ,  C07C317/32 ,  C07C323/42 ,  C07D207/16 ,  C07D211/54 ,  C07D213/52 ,  C07D213/81 ,  C07D213/89 ,  C07D231/12 ,  C07D233/64 ,  C07D257/04 ,  C07D261/02 ,  C07D261/08 ,  C07D261/20 ,  C07D263/52 ,  C07D277/26 ,  C07D295/088 ,  C07D303/26 ,  C07D303/34 ,  C07D307/32 ,  C07D307/33 ,  C07D309/08 ,  C07D313/04 ,  C07D317/72 ,  C07D327/10 ,  C07D401/04 ,  C07D451/04 ,  C07D493/04

摘要： The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: X-A-Y-L-R  (I) which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

公开(公告)号：US20210002242A1

公开(公告)日：2021-01-07

申请号：US16977548

申请日：2019-03-08

申请人： ENZYCHEM LIFESCIENCES CORPORATION

发明人： Ki Young SOHN ,  Jae Wha KIM ,  Sun Young YOON ,  Chang Hyun YOO ,  Jin Seon JEONG

IPC分类号： C07D307/32 ,  A23L33/00 ,  A23L29/00 ,  A61P31/04

摘要： Disclosed are a novel diacylglycerol lactone compound for improving immunity and inhibiting infection by promoting neutrophil movement, a preparation method therefor, and an immunostimulator containing same as an active ingredient. The diacyloglycerol lactone compound is represented by chemical formula 1 of the specification. In chemical formula 1, R1 and R2 are respectively N and independently a C2-30 fatty acid group.

公开(公告)号：US10787445B2

公开(公告)日：2020-09-29

申请号：US16439253

申请日：2019-06-12

申请人： Midwestern University

发明人： Mark Jon Olsen ,  John-Michael Thomas

IPC分类号： C07D307/26 ,  C07D405/04 ,  C07D417/04 ,  C07D409/04 ,  C07D405/12 ,  C07D307/32 ,  C07D307/66 ,  A61P35/00 ,  C12Q1/26

摘要： The present invention relates to compounds which modulate (e.g., inhibit) the activity of beta-hydrolase (e.g., ASPH), including novel 2-aryl-5-amino-3(2H)-furanone and 2-heteroaryl-5-amino-3(2H)-furanone compounds, pharmaceutical compositions thereof, methods for their synthesis, and methods of using these compounds to modulate the activity of ASPH in an a cell-free sample, a cell-based assay, and in a subject. Other aspects of the invention relate to use of the compounds disclosed herein to ameliorate or treat cell proliferation disorders.

公开(公告)号：US10273452B2

公开(公告)日：2019-04-30

申请号：US15159351

申请日：2016-05-19

申请人： MEMORIAL SLOAN-KETTERING CANCER CENTER

发明人： Stuart Chambers ,  Lorenz Studer ,  Zehra Dincer ,  Bastian Zimmer

IPC分类号： C12N5/0793 ,  A61K35/12 ,  C07D243/36 ,  C07D211/00 ,  C07D307/32

摘要： Cranial placodes are embryonic structures essential for sensory and endocrine organ development. The efficient derivation of cranial placodes from human pluripotent stem cells is disclosed where the timed removal of the BMP inhibitor Noggin, a component of the dual-SMAD inhibition strategy of neural induction, triggers placode induction at the expense of CNS fates. Further fate specification at the pre-placode stage enables the selective generation of placode-derived trigeminal ganglia capable of in vivo engraftment, mature lens fibers and anterior pituitary hormone-producing cells that upon transplantation produce hormones including, but not limited to, human growth hormone and adrenocortiocotropic hormone in vivo. Alternatively, anterior pituitary hormone-producing cells are generated in cell culture systems in vitro.

公开(公告)号：US10179792B2

公开(公告)日：2019-01-15

申请号：US15450125

申请日：2017-03-06

申请人： ENANTA PHARMACEUTICALS, INC.

发明人： Yao-Ling Qiu ,  Xuri Gao ,  Wei Li ,  Hui Cao ,  Meizhong Jin ,  Jorden Kass ,  Xiaowen Peng ,  Yat Sun Or

IPC分类号： C07D211/54 ,  C07D231/12 ,  C07D233/64 ,  C07D257/04 ,  C07D261/02 ,  C07D263/52 ,  C07D277/26 ,  C07D295/088 ,  C07D303/26 ,  C07D307/33 ,  C07C235/56 ,  C07C311/53 ,  C07C317/32 ,  C07C323/42 ,  A61K31/167 ,  A61K31/18 ,  A61K31/196 ,  A61K31/215 ,  A61K31/341 ,  A61K31/351 ,  A61K31/357 ,  A61K31/401 ,  A61K31/421 ,  A61K31/439 ,  A61K31/44 ,  C07D493/08 ,  A61K31/223 ,  A61K31/277 ,  A61K31/325 ,  A61K31/335 ,  A61K31/336 ,  A61K31/365 ,  A61K31/39 ,  A61K31/41 ,  A61K31/415 ,  A61K31/416 ,  A61K31/4164 ,  A61K31/426 ,  A61K31/4402 ,  A61K31/4409 ,  A61K31/4425 ,  A61K31/445 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/655 ,  C07B59/00 ,  C07D207/16 ,  C07D213/52 ,  C07D213/81 ,  C07D213/89 ,  C07D261/08 ,  C07D261/20 ,  C07D303/34 ,  C07D307/32 ,  C07D309/08 ,  C07D313/04 ,  C07D317/72 ,  C07D327/10 ,  C07D401/04 ,  C07D451/04 ,  C07D493/04

摘要： The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: X-A-Y-L-R  (I) which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

公开(公告)号：US20170369519A1

公开(公告)日：2017-12-28

申请号：US15488603

申请日：2017-04-17

申请人： POSTECH ACADEMY-INDUSTRY FOUNDATION

发明人： Young Ho RHEE ,  Mijin KIM ,  Soyeong KANG

IPC分类号： C07H17/04 ,  C07H15/04 ,  C07H3/06 ,  C07H3/04 ,  C07D407/12 ,  C07D309/10 ,  C07D307/32 ,  C07H15/207 ,  C07C43/215

CPC分类号： C07H17/04 ,  C07C43/215 ,  C07C43/315 ,  C07C2601/14 ,  C07D307/32 ,  C07D309/10 ,  C07D407/12 ,  C07H3/04 ,  C07H3/06 ,  C07H15/04 ,  C07H15/207

摘要： The present invention relates to a method for the stereoselective preparation of apiose derivatives from allylic alcohol compounds and allene compounds using catalytic asymmetric synthesis. The method for the stereoselective preparation of apiose derivatives of the present invention is based on the catalytic asymmetric synthesis from allylic alcohol compounds and allene compounds in the presence of a metal catalyst, so that apiose derivatives can be produced stereoselectively, with high yield, with high optical purity regardless of the types of substituents of the compounds. The method of the invention can also be used for the preparation of oligosaccharides including monosaccharides, disaccharides, and polysaccharides or various compounds including apiose derivatives because the method can minimize the production of by-products without using an activating group, unlike the conventional method for the preparation of adipose derivatives.

公开(公告)号：US09796694B2

公开(公告)日：2017-10-24

申请号：US14328515

申请日：2014-07-10

申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION

发明人： Helen E. Blackwell ,  Grant D. Geske ,  Jennifer C. Campbell Butler

IPC分类号： C07D307/33 ,  A61K31/365 ,  C07D307/32 ,  C07D309/30 ,  C07D333/32 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C12N1/36

CPC分类号： C07D307/33 ,  A61K31/365 ,  C07D307/32 ,  C07D309/30 ,  C07D333/32 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C12N1/36 ,  Y02A50/471 ,  Y02A50/473

摘要： The present invention provides compounds and methods for modulation of the quorum sensing of bacteria. In an embodiment, the compounds of the present invention are able to act as replacements for naturally occurring bacterial quorum sensing ligands in a ligand-protein binding system; that is, they imitate the effect of natural ligands and produce an agonistic effect. In another embodiment, the compounds of the present invention are able to act in a manner which disturbs or inhibits the naturally occurring ligand-protein binding system in quorum sensing bacteria; that is, they produce an antagonistic effect. The compounds of the present invention comprise N-acylated-homoserine lactones (AHLs) comprised of a wide range of acyl groups.

公开(公告)号：US20160090391A1

公开(公告)日：2016-03-31

申请号：US14890127

申请日：2014-05-09

申请人： ALPHORA RESEARCH INC.

发明人： Fabio E.s. Souza ,  Jason A. Bexrud ,  Ricardo Orprecio ,  Boris Gorin

IPC分类号： C07F7/08 ,  C07D307/32 ,  C07D493/22 ,  C07D307/28

CPC分类号： C07F7/0812 ,  C07D307/28 ,  C07D307/32 ,  C07D493/22 ,  Y02P20/55

摘要： Discloses is a process for preparation of a compound of formula 11, or a derivative thereof, wherein PG1 is an alcohol protecting group. Also, disclosed are intermediates and processes for their preparation. The compound of formula 11 can be useful in the preparation of halinchondrin analogs.

摘要翻译： 公开了制备式11化合物或其衍生物的方法，其中PG1是醇保护基。 还公开了它们的制备的中间体和方法。 式11的化合物可用于制备软蛋白类似物。

公开(公告)号：US08563279B2

公开(公告)日：2013-10-22

申请号：US12810220

申请日：2008-12-19

申请人： Ben De Lange ,  Anna Maria Cornelia Francisca Castelijns ,  Johannes Gerardus De Vries ,  Andreas Hendrikus Maria De Vries ,  Jeroen Antonius Franciscus Boogers ,  Quirinus Bernardus Broxterman

发明人： Ben De Lange ,  Anna Maria Cornelia Francisca Castelijns ,  Johannes Gerardus De Vries ,  Andreas Hendrikus Maria De Vries ,  Jeroen Antonius Franciscus Boogers ,  Quirinus Bernardus Broxterman

IPC分类号： C07C231/18 ,  C07C253/16 ,  C07C255/20 ,  C07F1/02 ,  C07F7/18 ,  C07D307/32 ,  C07D307/33 ,  C12P13/00

CPC分类号： C07D307/33 ,  C07C231/02 ,  C07C231/18 ,  C07D307/32 ,  C07F1/02 ,  C07F7/1804 ,  C07C237/22

摘要： Described is a method for the preparation of renin inhibitors such as aliskiren, and intermediates useful therein. The method introduces a nitrogen-containing intermediate such as a lactone of formula (8). with R4 being a branched C3—6 alkyl. In the preparation of the lactone, or related intermediates, a desired stereochemical configuration can be controlled by starting from a chiral aldehyde satisfying formula (10).

摘要翻译： 描述了制备肾素抑制剂如阿利吉仑的方法和其中有用的中间体。 该方法引入含氮中间体如式（8）的内酯。 其中R4是支链C 3-6烷基。 在内酯或相关中间体的制备中，可以通过从满足式（10）的手性醛开始来控制所需的立体化学构型。

公开(公告)号：US08124649B2

公开(公告)日：2012-02-28

申请号：US12495666

申请日：2009-06-30

申请人： Mustapha Haddach ,  Johnny Yasuo Nagasawa

发明人： Mustapha Haddach ,  Johnny Yasuo Nagasawa

IPC分类号： A61K31/195 ,  A61K31/341 ,  C07D307/32 ,  C07D409/04

CPC分类号： C07D405/06 ,  C07D405/14 ,  C07D417/14

摘要： The invention provides compounds that inhibit PIM kinases and Flt3 kinase, and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation.

摘要翻译： 本发明提供抑制PIM激酶和Flt3激酶的化合物，以及含有这些化合物的组合物。 这些化合物和组合物可用于治疗增殖性疾病如癌症，以及其它激酶相关病症，包括炎症。