公开(公告)号：EP3519383B1

公开(公告)日：2024-08-21

申请号：EP17772733.6

申请日：2017-09-28

IPC: C07C259/06 ,  A61P35/02

CPC classification number: C07C271/02 ,  C07C271/20 ,  C07C271/22 ,  C07C279/14 ,  C07C279/24 ,  C07C323/41 ,  C07C229/34 ,  C07C233/65 ,  C07D487/08 ,  C07C235/50 ,  C07D487/18 ,  C07C239/12 ,  C07C243/28 ,  C07C251/40 ,  C07C251/60 ,  C07C59/72 ,  C07C59/74 ,  C07C59/90 ,  C07C2601/1620170501 ,  C07C2603/7420170501 ,  C07D215/14 ,  C07D215/38 ,  C07D295/145 ,  C07D295/155 ,  A61P35/00 ,  A61P35/02 ,  C07C259/04

公开(公告)号：EP4410776A1

公开(公告)日：2024-08-07

申请号：EP22875174.9

申请日：2022-09-30

Applicant: Wuhan Createrna Science and Technology Co.,Ltd.

Inventor： LOU, Jun ,  WU, Jingkang ,  LIU, Li ,  SUN, Youyou ,  CHEN, Yongkai ,  ZHANG, Yihan ,  LU, Xiaoqin ,  ZHOU, Feng ,  CHEN, Ying ,  ZHANG, Liqian ,  YANG, Fan ,  WANG, Chaodong

IPC: C07D213/04 ,  C07C229/34 ,  A61K31/4418 ,  A61K31/4427 ,  A61K31/195 ,  A61P7/00 ,  A61P11/00 ,  A61P9/00 ,  A61P13/00 ,  A61P25/00 ,  A61P37/00

CPC classification number: A61K31/195 ,  A61K31/4418 ,  A61K31/4427 ,  A61P7/00 ,  A61P9/00 ,  A61P13/00 ,  A61P11/00 ,  A61P25/00 ,  A61P37/00 ,  C07C229/34 ,  C07D213/04

Abstract: Disclosed are a compound as an inhibitor of complement factor D, and a pharmaceutical composition thereof and the use thereof. Specifically disclosed are a compound as represented by formula (I), a tautomer thereof, a stereoisomer thereof and a prodrug thereof, or a pharmaceutically acceptable salt of any one of the above-mentioned compounds, or a solvate of any one of the above-mentioned compounds. The compound has a good inhibitory activity on complement factor D, and has an excellent pharmacokinetic and pharmacodynamic activity. Formula (I)

公开(公告)号：EP3409776A1

公开(公告)日：2018-12-05

申请号：EP17744466.8

申请日：2017-01-30

Applicant: BONAC CORPORATION

Inventor： AOKI, Eriko ,  OHGI, Tadaaki ,  KINOSHITA, Takashi

IPC: C12N15/09 ,  C07C229/04 ,  C07C229/34 ,  C12N9/16

CPC classification number: C07C229/04 ,  C07C229/34 ,  C12N9/16 ,  C12N15/09 ,  Y02P20/55

Abstract: The present invention provides a novel artificial sgRNA having an activity equal to or higher than that of a natural form sgRNA and improved in stability in vivo, and an efficient CRISPR/Cas9 system by combining the artificial sgRNA and Cas9. Even when a nucleotide linker region for forming a single strand by linking the 3'-terminal of crRNA and the 5'-terminal of tracrRNA in sgRNA is substituted with an amino acid derivative linker, an activity equal to or higher than that of the original sgRNA is retained in an in vitro DNA cleavage assay. Furthermore, even when the linker region existing between stem-loop 1 and stem-loop 2 of tracrRNA and/or the loop portion of stem-loop 2 are/is substituted with an amino acid derivative linker, or even when an amino acid derivative linker is added/inserted into the vicinity of the 5'-terminal and/or the 3'-terminal of sgRNA, an activity equal to or higher than that of the original sgRNA is retained. The stability in vivo can be improved by introducing one or more amino acid derivative linkers into sgRNA.

公开(公告)号：EP3388429A1

公开(公告)日：2018-10-17

申请号：EP18175796.4

申请日：2011-11-16

Applicant: Texas Heart Institute

Inventor： BIEDIGER, Ronald, J. ,  GUNDLACH, IV, William ,  MARKET, Robert, V ,  SAVAGE, Michael, M ,  VANDERSLICE, Peter

IPC: C07D409/12 ,  A61K31/381 ,  A61P9/00

CPC classification number: C07D333/20 ,  A61K35/12 ,  A61K35/17 ,  A61K35/51 ,  C07C229/34 ,  C07C271/20 ,  C07C271/22 ,  C07C311/08 ,  C07D213/64 ,  C07D275/02 ,  C07D317/60 ,  C07D333/10 ,  C07D333/24 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14

Abstract: A method of enhancing binding of cells to an integrin-binding ligand comprises treating integrin-expressing cells in vitro with an agonist of integrin, wherein the integrin is selected from the group consisting of α4β1, α5β1, α4β7, αvβ3 and αLβ2, and contacting the treated cells with an integrin-binding ligand; integrin agonist compounds having the general formula I; methods of treating integrin-expressing cells with such agonists to enhance binding; and therapeutic methods comprising administering agonist-treated cells or agonist compounds to a mammal.

公开(公告)号：EP3301085A1

公开(公告)日：2018-04-04

申请号：EP16191348.8

申请日：2016-09-29

Applicant: BIOGEM S.CA.R.L.

Inventor： PISANO, Claudio ,  DALLAVALLE, Sabrina ,  CINCINELLI, Raffaella ,  MERLINI, Lucio

IPC: C07C59/72 ,  C07C59/74 ,  C07C59/90 ,  C07C229/34 ,  C07C235/42 ,  C07C251/40 ,  C07C251/48 ,  C07C251/60 ,  C07C259/06 ,  C07C279/14 ,  C07C279/24 ,  C07C271/20 ,  C07C271/22 ,  C07C323/41 ,  C07C403/20 ,  C07D215/12 ,  C07D241/04 ,  C07D215/28 ,  A61K31/201 ,  A61P35/00

CPC classification number: C07C59/72 ,  C07C59/74 ,  C07C59/90 ,  C07C229/34 ,  C07C233/65 ,  C07C235/50 ,  C07C239/12 ,  C07C243/28 ,  C07C251/40 ,  C07C251/60 ,  C07C259/06 ,  C07C271/02 ,  C07C271/20 ,  C07C271/22 ,  C07C279/14 ,  C07C279/24 ,  C07C323/41 ,  C07C2601/16 ,  C07C2603/74 ,  C07D215/14 ,  C07D215/38 ,  C07D295/145 ,  C07D295/155 ,  C07D487/08 ,  C07D487/18

Abstract: The present invention relates to new compounds of formula (I) and to pharmaceutical compositions containing them:

The use of such compounds for the treatment of cancer and other diseases related to altered angiogenesis, such as arthritic pathology, diabetic retinopathy, psoriasis and chronic inflammatory disease, is also within the scope of the present invention.

Abstract translation: 本发明涉及新的式（I）化合物和含有它们的药物组合物：这些化合物用于治疗与改变血管生成有关的癌症和其它疾病如关节炎病理学，糖尿病性视网膜病，牛皮癣和慢性炎性疾病 也在本发明的范围内。

公开(公告)号：EP3204347A4

公开(公告)日：2018-03-28

申请号：EP16847622

申请日：2016-12-23

Applicant: COMMW SCIENT IND RES ORG

Inventor： YORK MARK ,  RYAN JOHN

IPC: C07C49/203 ,  A61K8/40 ,  A61K8/46 ,  A61K8/49 ,  A61K8/58 ,  A61Q17/04 ,  C07D209/10 ,  C07D221/04 ,  C08K5/16 ,  C09D5/32 ,  C11D3/26 ,  G02C7/10

CPC classification number: C07C225/22 ,  A61K8/41 ,  A61K8/411 ,  A61K8/466 ,  A61K8/49 ,  A61K8/4906 ,  A61K8/4913 ,  A61K8/492 ,  A61K8/4926 ,  A61K8/494 ,  A61K8/4953 ,  A61K8/585 ,  A61K8/70 ,  A61Q17/04 ,  C07C225/16 ,  C07C229/34 ,  C07C229/60 ,  C07C235/78 ,  C07C255/42 ,  C07C255/58 ,  C07C311/37 ,  C07D209/08 ,  C07D209/10 ,  C07D215/06 ,  C07D217/04 ,  C07D221/04 ,  C07D295/108 ,  C07F7/1852 ,  C08K5/005 ,  C08K5/16 ,  C08K5/17 ,  C08K5/175 ,  C08K5/18 ,  C08K5/3412 ,  C08K5/3415 ,  C08K5/3417 ,  C08K5/3432 ,  C08K5/3435 ,  C08K5/3437 ,  C08K5/3442 ,  C08K5/3462 ,  C08K5/3465 ,  C08K5/357 ,  C09D5/32 ,  C09D7/48 ,  C09D133/12 ,  C11D3/30 ,  G02B1/041 ,  G02C7/108

Abstract: The present invention describes compounds and uses thereof in applications relating to absorption of electromagnetic energy. Preferred compounds are double bond-containing compounds capable of absorbing electromagnetic radiation energy and having improved properties.

公开(公告)号：EP3235796A1

公开(公告)日：2017-10-25

申请号：EP17000929.4

申请日：2012-02-29

Applicant: Microbial Chemistry Research Foundation

Inventor： Shibasaki, Masakatsu ,  Yamatsugu, Kenzo

IPC: C07B53/00 ,  C07C229/30 ,  C07C229/48 ,  C07C269/06 ,  C07C271/24

CPC classification number: C07C229/48 ,  C07B53/00 ,  C07C229/30 ,  C07C229/34 ,  C07C229/60 ,  C07C269/06 ,  C07C271/24 ,  C07C2601/16 ,  Y02P20/55

Abstract: A compound represented by the following general formula (8), a method for producing it, and its use in the preparation of oseltamivir phosphate.

Abstract translation: 由以下通式（8）表示的化合物，其制备方法及其在制备磷酸奥司他韦中的用途。

公开(公告)号：EP2847177B1

公开(公告)日：2017-10-11

申请号：EP13724059.4

申请日：2013-05-01

Applicant: Boehringer Ingelheim International GmbH

Inventor： KAPADIA, Suresh, R. ,  REEVES, Jonathan, Timothy ,  ZENG, Xingzhong ,  ERIKSSON, Magnus Carl Arne

IPC: C07D305/06 ,  C07C213/02 ,  C07C215/10 ,  C07C227/10 ,  C07C229/24

CPC classification number: C07D305/06 ,  C07C213/00 ,  C07C215/10 ,  C07C215/28 ,  C07C227/10 ,  C07C229/24 ,  C07C229/34

公开(公告)号：EP2588450B1

公开(公告)日：2017-05-24

申请号：EP11738878.5

申请日：2011-07-01

Applicant: Gilead Sciences, Inc.

Inventor： BABAOGLU, Kerim ,  BJORNSON, Kyla ,  GUO, Hongyan ,  HALCOMB, Randall, L. ,  LINK, John, O. ,  MCFADDEN, Ryan ,  MITCHELL, Michael, L. ,  ROETHLE, Paul A. ,  TRENKLE, James, D. ,  VIVIAN, Randall, W. ,  XU, Lianhong ,  LIU, Hongtao ,  TAYLOR, James ,  HRVATIN, Paul ,  BACON, Elizabeth

IPC: C07D205/04 ,  C07D215/04 ,  C07D309/10 ,  C07D211/48 ,  C07D231/12 ,  C07D311/20 ,  C07D213/64 ,  C07D233/58 ,  C07D493/04 ,  C07D213/65 ,  C07D239/34 ,  C07D295/073 ,  C07D213/73 ,  C07D241/12 ,  A61P31/18

CPC classification number: C07C59/64 ,  C07C229/34 ,  C07C233/47 ,  C07C255/57 ,  C07C271/22 ,  C07C311/16 ,  C07D205/04 ,  C07D211/48 ,  C07D213/64 ,  C07D213/65 ,  C07D213/73 ,  C07D215/04 ,  C07D215/14 ,  C07D231/12 ,  C07D233/58 ,  C07D239/26 ,  C07D239/34 ,  C07D239/36 ,  C07D239/42 ,  C07D241/12 ,  C07D295/073 ,  C07D295/155 ,  C07D309/10 ,  C07D311/20 ,  C07D311/58 ,  C07D487/04 ,  C07D491/06 ,  C07D493/04

公开(公告)号：EP3099678A1

公开(公告)日：2016-12-07

申请号：EP15705859.5

申请日：2015-01-29

Applicant: Theravance Biopharma R&D IP, LLC

Inventor： FLEURY, Melissa ,  BEAUSOLIEL, Anne-Marie ,  HUGHES, Adam D. ,  LONG, Daniel D. ,  WILTON, Donna A.A.

IPC: C07D405/14 ,  C07D309/40 ,  C07C271/22 ,  C07D319/06 ,  C07D231/14 ,  C07D231/18 ,  C07D231/20 ,  C07D233/70 ,  C07D233/90 ,  C07D401/04 ,  C07D235/08 ,  C07D403/06 ,  C07D237/14 ,  C07D239/34 ,  C07D405/12 ,  C07C229/34 ,  C07D249/10 ,  C07D249/12 ,  C07D249/18 ,  C07D471/04

CPC classification number: C07D249/04 ,  A61K31/415 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/42 ,  A61K31/421 ,  A61K31/4245 ,  A61K31/425 ,  A61K31/437 ,  A61K31/44 ,  A61K31/4985 ,  A61K31/505 ,  A61K45/06 ,  A61P9/04 ,  A61P9/12 ,  A61P13/12 ,  C07C229/34 ,  C07C271/22 ,  C07D213/81 ,  C07D231/14 ,  C07D231/18 ,  C07D231/20 ,  C07D233/70 ,  C07D233/90 ,  C07D235/08 ,  C07D237/14 ,  C07D239/28 ,  C07D239/34 ,  C07D249/10 ,  C07D249/12 ,  C07D249/18 ,  C07D261/12 ,  C07D261/18 ,  C07D263/18 ,  C07D263/34 ,  C07D263/38 ,  C07D271/07 ,  C07D275/03 ,  C07D295/10 ,  C07D309/40 ,  C07D319/06 ,  C07D401/04 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D471/04

Abstract: In one aspect, the invention relates to compounds having the formula I: where R1-R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.

Abstract translation: 其中R 1 -R 6如说明书中所定义，或其药学上可接受的盐。 这些化合物具有尿丙氨酸抑制活性。 另一方面，本发明涉及包含这些化合物的药物组合物; 使用这些化合物的方法; 以及制备这些化合物的方法和中间体。