公开(公告)号：US10912836B2

公开(公告)日：2021-02-09

申请号：US16180494

申请日：2018-11-05

申请人： YALE UNIVERSITY

发明人： David A. Spiegel ,  Patrick McEnaney ,  Kelly Fitzgerald

IPC分类号： A61K47/55 ,  C07D249/04 ,  C07D249/06 ,  A61K47/54 ,  A61K31/194 ,  A61K38/10 ,  A61K45/06

摘要： The present invention relates to compounds which function as antibody mimetic compounds. These compounds are bifunctional/multifunctional compounds which contain at least one cancer cell binding moiety which selectively binds to prostate specific membrane antigen (PSMA) and a FC receptor binding moiety which modulates an FC immune receptor, preferably a FcγRI receptor. Compounds according to the present invention bind selectively to cancer cells which upregulate PSMA and through that interaction, place the Fc receptor binding moiety of the compound in proximity to a Fc receptor, preferably a FcγRI receptor, which can modulate (preferably, upregulate) a humoral response in a patient to cancer cells. Through this biological action of the compounds according to the present invention, cancer cells, including metastatic cancer cells, especially prostate cancer cells can be immune regulated, resulting in the favorable therapy of cancer in a patient. Methods of using these compounds to treat cancer and/or reduce the likelihood of metastasis of cancer are additional aspects of the present invention.

公开(公告)号：US20200345700A1

公开(公告)日：2020-11-05

申请号：US16479602

申请日：2018-01-24

申请人： MEDSHINE DISCOVERY INC.

发明人： Lingyun WU ,  Li ZHANG ,  Lele ZHAO ,  Jianjun SUN ,  Zhaoguo CHEN ,  Jian Ll ,  Shuhui CHEN

IPC分类号： A61K31/4245 ,  A61K33/243 ,  A61P35/00 ,  A61K31/277 ,  C07C255/46 ,  C07D257/04 ,  A61K31/41 ,  A61K31/135 ,  C07C211/40 ,  C07D207/335 ,  A61K31/40 ,  C07D207/09 ,  C07D233/64 ,  A61K31/417 ,  A61K31/4196 ,  C07D249/08 ,  C07D213/38 ,  A61K31/44 ,  A61K31/426 ,  C07D277/28 ,  C07D487/04 ,  A61K31/4188 ,  C07D271/06 ,  A61K31/165 ,  C07C233/58 ,  C07D413/04 ,  A61K31/4439 ,  A61K31/437 ,  C07D471/04 ,  C07D263/56 ,  A61K31/423 ,  A61K31/4375 ,  C07D217/26 ,  A61K31/472 ,  A61K31/451 ,  C07D211/18 ,  C07D211/34 ,  C07D209/44 ,  A61K31/4035 ,  A61K31/55 ,  C07D223/16 ,  C07D261/20 ,  A61K31/519 ,  C07D413/10 ,  C07D417/04 ,  A61K31/428 ,  A61K31/4192 ,  C07D249/06 ,  A61K31/4545 ,  C07D413/14 ,  A61K31/415 ,  C07D231/12 ,  C07D413/06 ,  A61K31/422

摘要： A cyclopropylamine compound as a lysine-specific demethylase 1 (LSD1) inhibitor. Particularly, the present invention relates to a compound represented by formula (I) and a pharmaceutically acceptable salt thereof. The present invention also provides an application of the same in preparing a drug for treating an LSD1-related disease.

公开(公告)号：US20200331872A1

公开(公告)日：2020-10-22

申请号：US16918687

申请日：2020-07-01

申请人： GAVISH-GALILEE BIO APPLICATIONS LTD.

发明人： Itai BLOCH ,  Elad COHEN ,  Rachel AMIR ,  Maayan GAL

IPC分类号： C07D277/42 ,  C07D271/06 ,  C07D249/06 ,  C07D257/04 ,  C07D413/04 ,  C07D401/12 ,  C07D405/12 ,  C07D403/12 ,  C07D239/36 ,  C07D237/14 ,  C07D233/70 ,  C07D417/10 ,  C07D471/04 ,  C07D403/06 ,  C07D413/06 ,  C07D413/14 ,  C07D249/18 ,  C07D231/56 ,  C07D401/06 ,  A01N43/90 ,  A01N43/82 ,  A01N43/713 ,  A01N43/707 ,  A01N43/80 ,  A01N43/86 ,  A01N43/54 ,  A01N43/58

摘要： The present invention provides novel inhibitors of cystathionin gamma synthase (CGS), their use as selective and non-selective herbicides, agricultural and non-agricultural herbicides, herbicides in integrated pest management, herbicides for gardening, clearing waste ground, clearing industrial or constructions sites, clearing railways and railway embankments, pesticide, fungicide, agricultural plant stimulant or antimicrobial agent. Also provided is a method for the control of undesired vegetation or clearing areas from the undesired vegetation comprising applying to the locus of said undesired vegetation, to the undesired plants or to a habitat thereof, a herbicidally effective amount of the compound of the present invention.

公开(公告)号：US20200299270A1

公开(公告)日：2020-09-24

申请号：US16691390

申请日：2019-11-21

申请人： Proteostasis Therapeutics, Inc.

发明人： Megan Foley ,  Bradley Tait ,  Matthew Cullen

IPC分类号： C07D403/06 ,  C07D207/333 ,  C07D207/337 ,  C07D231/12 ,  C07D249/06 ,  C07D263/32 ,  C07D275/02 ,  C07D295/185 ,  C07D333/20 ,  C07D401/06 ,  C07D405/06 ,  C07D471/04 ,  C07D333/22

摘要： The present invention is directed to compounds having the Formulae (Ia-Ie), (II), (IIIa-IIId), (IVa-IVc), (Va-Vb), (VIa-VIe), (VII), (VIIIa-VIIIc), and (IX), pharmaceutically acceptable salts, prodrugs and solvates thereof, compositions of any of thereof and methods for the treatment of a condition associated with a dysfunction in proteostasis comprising an effective amount of these compounds.

公开(公告)号：US20200231555A1

公开(公告)日：2020-07-23

申请号：US16639163

申请日：2018-08-16

申请人： GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED

发明人： Carlos ALEMPARTE-GALLARDO ,  Lourdes ENCINAS ,  Jorge ESQUIVIAS PROVENCIO

IPC分类号： C07D257/04 ,  C07D403/06 ,  C07D401/06 ,  C07D405/06 ,  C07D249/06 ,  A61P31/06

摘要： The invention relates to a compound of Formula (I) or a pharmaceutically acceptable salt thereof and their use in therapy, for example in the treatment of mycobacterial infections or in the treatment of diseases caused by Mycobacterium, such as tuberculosis.

公开(公告)号：US10662172B2

公开(公告)日：2020-05-26

申请号：US16223169

申请日：2018-12-18

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： Yan Shi ,  Peter Tai Wah Cheng ,  Ying Wang ,  Jun Shi ,  Shiwei Tao ,  Jun Li ,  Lawrence J. Kennedy ,  Robert F. Kaltenbach, III ,  Hao Zhang ,  James R. Corte

IPC分类号： C07D401/04 ,  C07D403/04 ,  C07D249/06 ,  A61P35/00 ,  A61P1/16 ,  A61P19/10 ,  A61P13/12 ,  A61P11/00 ,  C07C403/04 ,  C07C249/06

摘要： The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors.

公开(公告)号：US20200148665A1

公开(公告)日：2020-05-14

申请号：US16744303

申请日：2020-01-16

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： Yan Shi ,  Peter Tai Wah Cheng ,  Ying Wang ,  Jun Shi ,  Shiwei Tao ,  Jun Li ,  Lawrence J. Kennedy ,  Robert F. Kaltenbach, III ,  Hao Zhang ,  James R. Corte

IPC分类号： C07D401/04 ,  A61P35/00 ,  C07D249/06 ,  C07D403/04

摘要： The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors.

公开(公告)号：US10538495B2

公开(公告)日：2020-01-21

申请号：US16094910

申请日：2017-05-11

申请人： GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED

发明人： Brian Alvin Johns ,  Wieslaw Mieczyslaw Kazmierski ,  Martha Alicia De La Rosa ,  Vicente Samano

IPC分类号： C07D257/04 ,  C07D403/12 ,  C07F9/6524 ,  C07D401/04 ,  C07D401/10 ,  C07D405/12 ,  C07D417/12 ,  C07C323/63 ,  C07D249/06 ,  C07D249/08 ,  C07D271/06 ,  C07C323/42 ,  C07C323/45 ,  C07D285/08 ,  C07D401/12 ,  C07D413/12

摘要： Provided are IDO inhibitor compounds of Formula I and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and methods for their use in the prevention and/or treatment of diseases.

公开(公告)号：US20190322629A1

公开(公告)日：2019-10-24

申请号：US16390169

申请日：2019-04-22

申请人： Corcept Therapeutics, Inc.

发明人： Hazel Hunt ,  Arjen Christiaan Breman ,  Bas Wilhelmus Theodorus Gruijters

IPC分类号： C07D249/06

摘要： Methods of preparing N-2 alkylated triazoles substantially free from N-1 and N-3 alkylated triazoles are disclosed.The methods include one-step alkylation methods and two-step alkylation methods for the preparation of N-alkylated triazoles.

公开(公告)号：US10435374B2

公开(公告)日：2019-10-08

申请号：US15645814

申请日：2017-07-10

申请人： BAYER CROPSCIENCE AG

发明人： Eike Kevin Heilmann ,  Joerg Greul ,  Axel Trautwein ,  Hans-Georg Schwarz ,  Isabelle Adelt ,  Roland Andree ,  Peter Luemmen ,  Maike Hink ,  Martin Adamczewski ,  Mark Drewes ,  Angela Becker ,  Arnd Voerste ,  Ulrich Goergens ,  Kerstin Ilg ,  Johannes-Rudolf Jansen ,  Daniela Portz

IPC分类号： A01N43/40 ,  C07D231/40 ,  A01N43/56 ,  A01N43/58 ,  A01N43/647 ,  A01N43/76 ,  A01N43/78 ,  A01N43/82 ,  C07D231/52 ,  C07D231/56 ,  C07D403/12 ,  C07D231/06 ,  C07D231/22 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  A01N43/60 ,  A01N43/653 ,  C07D249/06

摘要： The present application relates to the use of heterocyclic compounds for controlling animal pests including arthropods, insects and nematodes, to novel heterocyclic compounds, to processes for their preparation and to intermediates for preparing the heterocyclic compounds.