公开(公告)号：US20240199535A1

公开(公告)日：2024-06-20

申请号：US18554365

申请日：2022-04-08

Applicant: IMMUNIC AG

Inventor： Christian GEGE ,  Hella KOHLHOF ,  Andreas MÜHLER ,  Daniel VITT

IPC: C07C233/75 ,  A61K31/16 ,  A61K31/167 ,  A61K31/341 ,  A61K31/381 ,  A61K31/426 ,  A61K31/437 ,  A61K31/44 ,  A61K31/472 ,  A61K31/5375 ,  A61P31/14 ,  C07C233/74 ,  C07D213/68 ,  C07D213/73 ,  C07D217/04 ,  C07D265/30 ,  C07D277/34 ,  C07D307/30 ,  C07D333/40 ,  C07D471/04

CPC classification number: C07C233/75 ,  A61K31/16 ,  A61K31/167 ,  A61K31/341 ,  A61K31/381 ,  A61K31/426 ,  A61K31/437 ,  A61K31/44 ,  A61K31/472 ,  A61K31/5375 ,  A61P31/14 ,  C07C233/74 ,  C07D213/68 ,  C07D213/73 ,  C07D217/04 ,  C07D265/30 ,  C07D277/34 ,  C07D307/30 ,  C07D333/40 ,  C07D471/04

Abstract: The invention relates to novel deuterated compounds of Formula (I)




and their use as medicaments.

公开(公告)号：US20240059654A1

公开(公告)日：2024-02-22

申请号：US18125961

申请日：2023-03-24

Applicant: The Regents of the University of California

Inventor： Michael E. Jung ,  Xiaohong Chen ,  Cun-Yu Wang ,  Jiong Li ,  Jie Zheng

IPC: C07D213/68 ,  A61P35/00 ,  C07C235/62 ,  C07C237/04 ,  C07C311/07 ,  C07D211/86 ,  C07D213/89 ,  C07D295/088 ,  C07D295/15 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07C237/38 ,  C07D213/50 ,  C07D213/55 ,  C07D213/40 ,  C07D213/06 ,  C07D213/38

CPC classification number: C07D213/68 ,  C07D213/38 ,  C07C235/62 ,  C07C237/04 ,  C07C311/07 ,  C07D211/86 ,  C07D213/89 ,  C07D295/088 ,  C07D295/15 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07C237/38 ,  C07D213/50 ,  C07D213/55 ,  C07D213/40 ,  C07D213/06 ,  A61P35/00

Abstract: The present disclosure relates to compounds that are capable of modulating the WNT/Beta-Catenin pathway. The disclosure further relates to methods of treating colorectal cancer and other WNT/Beta-Catenin mediated cancers.

公开(公告)号：US20230212123A1

公开(公告)日：2023-07-06

申请号：US17920794

申请日：2021-04-20

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Scott D. Larsen ,  James A. Shayman ,  Michael William Wilson ,  Neil Moss

IPC: C07D213/64 ,  C07D213/65 ,  C07D213/40 ,  C07D213/68 ,  C07D401/06 ,  C07D213/61 ,  A61K45/06

CPC classification number: C07D213/64 ,  A61K45/06 ,  C07D213/40 ,  C07D213/61 ,  C07D213/65 ,  C07D213/68 ,  C07D401/06

Abstract: Glucosylceramide synthase inhibitors and compositions containing the same are disclosed. Methods of using the glucosylceramide synthase inhibitors in the treatment of diseases and conditions wherein inhibition of glucosylceramide synthase provides a benefit, like Gaucher disease and Fabry disease, also are disclosed.

公开(公告)号：US20180354929A1

公开(公告)日：2018-12-13

申请号：US15864433

申请日：2018-01-08

Applicant: Global Blood Therapeutics, Inc.

Inventor： Brian W. Metcalf ,  Chihyuan Chuang

IPC: C07D401/12 ,  C07D471/04 ,  C07D213/80 ,  C07D213/69 ,  C07D401/14 ,  C07D213/68 ,  C07D213/65 ,  C07D405/14 ,  C07D413/12 ,  C07D487/04

CPC classification number: C07D401/12 ,  C07D213/65 ,  C07D213/68 ,  C07D213/69 ,  C07D213/80 ,  C07D401/14 ,  C07D405/14 ,  C07D413/12 ,  C07D471/04 ,  C07D487/04

Abstract: Provided are substituted heteroaryl aldehydes and derivatives thereof that act as allosteric modulators of hemoglobin, methods and intermediates for their preparation, pharmaceutical compositions comprising the modulators, and methods for their use in treating disorders mediate by hemoglobin and disorders that would benefit from increased tissue oxygenation.

公开(公告)号：US20180194710A1

公开(公告)日：2018-07-12

申请号：US15820194

申请日：2017-11-21

Applicant: Sanford-Burnham Medical Research Institute

Inventor： Raveendra Panickar Dhanya ,  Douglas J. Sheffler ,  Nicholas D. P. Cosford

IPC: C07C65/40 ,  C07F7/02 ,  C07F5/04 ,  C07C49/84 ,  C07F5/02 ,  C07D333/24 ,  C07D311/16 ,  C07D307/68 ,  C07D307/54 ,  C07D307/42 ,  C07D295/26 ,  C07D295/16 ,  C07D295/108 ,  C07D285/12 ,  C07D285/08 ,  C07D277/24 ,  C07D271/07 ,  C07D271/06 ,  C07D257/04 ,  C07D241/24 ,  C07D241/12 ,  C07D239/26 ,  C07D213/80 ,  C07D213/79 ,  C07D213/70 ,  C07D213/68 ,  C07D213/64 ,  C07D213/55 ,  C07D213/50 ,  C07C311/51 ,  C07C259/10 ,  C07C255/56 ,  C07C251/48 ,  C07C235/54 ,  C07C235/46 ,  C07C69/92 ,  C07C59/90

CPC classification number: C07C65/40 ,  C07C49/84 ,  C07C59/90 ,  C07C65/05 ,  C07C65/10 ,  C07C69/92 ,  C07C235/46 ,  C07C235/54 ,  C07C251/48 ,  C07C255/56 ,  C07C259/10 ,  C07C311/51 ,  C07C2601/02 ,  C07C2601/08 ,  C07D213/50 ,  C07D213/55 ,  C07D213/64 ,  C07D213/68 ,  C07D213/70 ,  C07D213/79 ,  C07D213/80 ,  C07D239/26 ,  C07D241/12 ,  C07D241/24 ,  C07D257/04 ,  C07D271/06 ,  C07D271/07 ,  C07D277/24 ,  C07D285/08 ,  C07D285/12 ,  C07D295/108 ,  C07D295/16 ,  C07D295/26 ,  C07D307/42 ,  C07D307/54 ,  C07D307/68 ,  C07D311/16 ,  C07D333/24 ,  C07F5/025 ,  C07F5/04 ,  C07F7/025

Abstract: Provided herein are small molecule active metabotropic glutamate subtype-2 and -3 receptor positive allosteric modulators (PAMS), compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.

公开(公告)号：US09964531B2

公开(公告)日：2018-05-08

申请号：US14760696

申请日：2014-01-21

Applicant: University of Oregon

Inventor： Michael M. Haley ,  Darren W. Johnson ,  Jeff Engle ,  Calden Carroll

IPC: C07D213/61 ,  C07D213/73 ,  C07D213/74 ,  G01N33/18 ,  C07D213/36 ,  C07D213/56 ,  C07D207/335 ,  C07D213/40 ,  C07D213/68 ,  G01N31/22

CPC classification number: G01N33/182 ,  C07D207/335 ,  C07D213/36 ,  C07D213/40 ,  C07D213/56 ,  C07D213/68 ,  C07D213/74 ,  G01N31/22 ,  Y10T436/193333

Abstract: Disclosed herein are host or receptor compounds that bind targets of interest. In one embodiment the compounds bind ions, such as metal ions.A compound, or a protonate or salt thereof, having the formula of: Formula IIa wherein R6 is an aminoalkoxy, alkylamino, nitro or —NH2; n is 1 or 2; each R2 is independently selected from an optionally substituted alkyl, halogen, optionally substituted alkoxy, optionally substituted carboxyl, or amide; a is 0 to 4.

公开(公告)号：US09879183B2

公开(公告)日：2018-01-30

申请号：US15317412

申请日：2015-06-04

Applicant: JNC CORPORATION ,  JNC PETROCHEMICAL CORPORATION

Inventor： Michiko Takahashi ,  Sayaka Fujimori ,  Yasuyuki Sasada

IPC: G02F1/1333 ,  C09K19/34 ,  C09K19/30 ,  C07C43/225 ,  C07D239/26 ,  C07D213/30 ,  C07D213/68 ,  C07D239/34 ,  C09K19/04 ,  G02F1/29

CPC classification number: C09K19/3402 ,  C07C43/225 ,  C07D213/30 ,  C07D213/68 ,  C07D239/26 ,  C07D239/34 ,  C09K19/12 ,  C09K19/18 ,  C09K19/20 ,  C09K19/30 ,  C09K19/3001 ,  C09K19/3003 ,  C09K19/3066 ,  C09K19/3068 ,  C09K19/32 ,  C09K19/34 ,  C09K19/42 ,  C09K19/54 ,  C09K2019/0466 ,  C09K2019/3004 ,  C09K2019/3009 ,  C09K2019/301 ,  C09K2019/3071 ,  C09K2019/3075 ,  C09K2019/3077 ,  C09K2019/3083 ,  C09K2019/3422 ,  C09K2019/3425 ,  G02F1/13 ,  G02F1/29

Abstract: To show a liquid crystal compound satisfying at least one of physical properties such as high chemical stability, a high clearing point, a low minimum temperature of a liquid crystal phase, low viscosity, large optical anisotropy, large dielectric anisotropy, a suitable elastic constant and excellent compatibility with other liquid crystal compounds, a liquid crystal composition containing the compound and a liquid crystal display device including the composition.A compound is represented by formula (1).

公开(公告)号：US20180022736A1

公开(公告)日：2018-01-25

申请号：US15723785

申请日：2017-10-03

Applicant: INVENTISBIO SHANGHAI LTD.

Inventor： Yueheng Jiang

IPC: C07D405/10 ,  C07D401/04 ,  C07D213/57 ,  C07D213/74 ,  C07D213/70 ,  C07B59/00 ,  C07C323/63 ,  C07D213/68

CPC classification number: C07D405/10 ,  A61K31/277 ,  A61K31/4418 ,  A61K31/4725 ,  C07B59/002 ,  C07B2200/05 ,  C07C319/20 ,  C07C323/62 ,  C07C323/63 ,  C07C2601/02 ,  C07D213/57 ,  C07D213/68 ,  C07D213/70 ,  C07D213/74 ,  C07D401/04

Abstract: The present invention relates to the technical field of medicine, and specifically relates to the carboxylic acid compound represented by the chemical formula I or chemical formula II, and a pharmaceutically acceptable salt, a prodrug, and a solvate thereof, and a method for preparation thereof, as well as a pharmaceutical composition containing the described substances, and a use thereof.

公开(公告)号：US09809580B2

公开(公告)日：2017-11-07

申请号：US15501387

申请日：2015-08-11

Applicant: INVENTISBIO SHANGHAI LTD.

Inventor： Yueheng Jiang

IPC: C07D405/10 ,  C07D213/70 ,  C07C323/63 ,  C07D213/74 ,  C07D213/68 ,  C07D401/04 ,  C07D213/57 ,  C07B59/00

CPC classification number: C07D405/10 ,  A61K31/277 ,  A61K31/4418 ,  A61K31/4725 ,  C07B59/002 ,  C07B2200/05 ,  C07C319/20 ,  C07C323/62 ,  C07C323/63 ,  C07C2601/02 ,  C07D213/57 ,  C07D213/68 ,  C07D213/70 ,  C07D213/74 ,  C07D401/04

Abstract: The present invention relates to the technical field of medicine, and specifically relates to the carboxylic acid compound represented by the chemical formula I or chemical formula II, and a pharmaceutically acceptable salt, a prodrug, and a solvate thereof, and a method for preparation thereof, as well as a pharmaceutical composition containing the described substances, and a use thereof.

公开(公告)号：US20170190715A1

公开(公告)日：2017-07-06

申请号：US15313712

申请日：2015-05-28

Applicant: ASTELLAS PHARMA INC. ,  KOTOBUKI PHARMACEUTICAL CO., LTD.

Inventor： Kenichi KAWAGUCHI ,  Akihiro ISHIHATA ,  Yusuke INAGAKI ,  Kazuyuki TSUCHIYA ,  Tadaatsu HANADATE ,  Akira KANAI ,  Hiroyuki KAIZAWA ,  Junichi KAZAMI ,  Hiroshi MORIKAWA ,  Masashi HIRAMOTO ,  Kentaro ENJO ,  Hajime TAKAMATSU

IPC: C07D495/04 ,  C07D405/06 ,  C07D491/056 ,  C07D401/12 ,  C07D409/12 ,  C07D471/04 ,  C07D401/10 ,  C07D405/12 ,  C07D401/04 ,  C07D213/68 ,  C07D491/048

CPC classification number: C07D495/04 ,  A61K31/4355 ,  A61K31/436 ,  A61K31/437 ,  A61K31/439 ,  A61K31/44 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  C07D213/68 ,  C07D213/70 ,  C07D213/74 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12 ,  C07D407/06 ,  C07D407/12 ,  C07D409/12 ,  C07D471/04 ,  C07D491/048 ,  C07D491/056 ,  C07D491/08

Abstract: The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically a pharmaceutically composition for treating nocturia.The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and/or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP.As a result, the inventors have found that (2R)-3-amino-2-{[4-(substituted pyridine)-2-yl]methyl}-2-hydroxy-propanoic acid derivatives have excellent P-LAP inhibitory activity. The inventors have evaluated antidiuretic effects in water-loaded rats and have found that the compounds increase endogenous AVP levels by inhibiting P-LAP and consequently reduce urine production. The present invention therefore provides compounds expected to be used as an agent for treating nocturia based on P-LAP inhibition.