公开(公告)号：US20240277659A1

公开(公告)日：2024-08-22

申请号：US18405593

申请日：2024-01-05

申请人： Trustees of Tufts College

发明人： William W. Bachovchin ,  Hung-sen Lai ,  Wengen Wu

IPC分类号： A61K31/402 ,  A61K31/4025 ,  A61K31/4035 ,  A61K31/4439 ,  A61K31/69 ,  A61K35/13 ,  A61K39/00 ,  A61K39/39 ,  A61K45/06 ,  A61P35/00 ,  A61P37/04

CPC分类号： A61K31/402 ,  A61K31/4025 ,  A61K31/4035 ,  A61K31/4439 ,  A61K31/69 ,  A61K35/13 ,  A61K39/39 ,  A61K45/06 ,  A61P35/00 ,  A61P37/04 ,  A61K2039/505

摘要： Disclosed are combination therapies including administration of I-DASH inhibitors and PGE2 antagonists, and the use of such therapies in the treatment of cell proliferative diseases.

公开(公告)号：US12023333B2

公开(公告)日：2024-07-02

申请号：US17609177

申请日：2020-05-07

申请人： GREY WOLF THERAPEUTICS LIMITED

发明人： Martin Quibell ,  Jason John Shiers ,  Michael Sparenberg

IPC分类号： A61K31/505 ,  A61K31/192 ,  A61K31/277 ,  A61K31/341 ,  A61K31/381 ,  A61K31/40 ,  A61K31/402 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4164 ,  A61K31/4196 ,  A61K31/421 ,  A61K31/422 ,  A61K31/425 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/50 ,  A61K45/06 ,  A61P37/02 ,  C07C311/29 ,  C07D207/325 ,  C07D207/327 ,  C07D207/335 ,  C07D213/42 ,  C07D213/56 ,  C07D213/57 ,  C07D231/12 ,  C07D233/64 ,  C07D237/08 ,  C07D239/26 ,  C07D249/08 ,  C07D257/04 ,  C07D263/32 ,  C07D275/02 ,  C07D277/28 ,  C07D277/30 ,  C07D307/52 ,  C07D333/20 ,  C07D333/22 ,  C07D333/24 ,  C07D333/38 ,  C07D401/10 ,  C07D403/10 ,  C07D409/10 ,  C07D413/10 ,  C07D417/10

CPC分类号： A61K31/505 ,  A61K31/192 ,  A61K31/277 ,  A61K31/341 ,  A61K31/381 ,  A61K31/40 ,  A61K31/402 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4164 ,  A61K31/4196 ,  A61K31/421 ,  A61K31/422 ,  A61K31/425 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/50 ,  A61K45/06 ,  A61P37/02 ,  C07C311/29 ,  C07D207/325 ,  C07D207/327 ,  C07D207/335 ,  C07D213/42 ,  C07D213/56 ,  C07D213/57 ,  C07D231/12 ,  C07D233/64 ,  C07D237/08 ,  C07D239/26 ,  C07D249/08 ,  C07D257/04 ,  C07D263/32 ,  C07D275/02 ,  C07D277/28 ,  C07D277/30 ,  C07D307/52 ,  C07D333/20 ,  C07D333/22 ,  C07D333/24 ,  C07D333/38 ,  C07D401/10 ,  C07D403/10 ,  C07D409/10 ,  C07D413/10 ,  C07D417/10

摘要： The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, wherein: the group X—Y is —NHSO2— or —SO2NH—; Z is a monocyclic aryl or heteroaryl group, each of which is optionally substituted by one or more substituents selected from alkyl, cycloalkyl, halo, alkoxy, CN, haloalkyl and OH; R1 is H or alkyl; R2 is selected from COOH and a tetrazolyl group; R3 is selected from H, C land alkyl; R4 is selected from H and halo; R5 is selected from H, alkyl, haloalkyl, SO2-alkyl, Cl, alkoxy, OH, CN, hydroxyalkyl, alkylthio, heteroaryl, cycloalkyl, heterocycloalkyl and haloalkoxy; R6 is H; R7 is selected from H, CN, haloalkyl, halo, SO2-alkyl, SO2NR12R13, heteroaryl, CONR10R11 and alkyl, wherein said heteroaryl group is optionally substituted by one or more substituents selected from alkyl, halo, alkoxy, CN, haloalkyl and OH; R8 is selected from H, alkyl, haloalkyl and halo; and R9 is H, alkyl or halo; R10 and R11 are each independently H or alkyl; and R12 and R13 are each independently H or alkyl. Further aspects of the invention relate to such compounds for use in the field of immuno-oncology and related applications. Another aspect of the invention relates to compounds of formulae (1a) and (1b).

公开(公告)号：US20240115521A1

公开(公告)日：2024-04-11

申请号：US18470317

申请日：2023-09-19

申请人： Saint Louis University ,  Research Foundation of the City University of New York

发明人： Getahun ABATE ,  John TAVIS ,  David W. GRIGGS ,  Ryan MURELLI

IPC分类号： A61K31/122 ,  A61K31/136 ,  A61K31/235 ,  A61K31/353 ,  A61K31/402 ,  A61K31/426 ,  A61K31/495 ,  A61K31/496 ,  A61K31/5375 ,  A61K31/55 ,  A61K45/06 ,  A61P31/04 ,  A61P31/06

CPC分类号： A61K31/122 ,  A61K31/136 ,  A61K31/235 ,  A61K31/353 ,  A61K31/402 ,  A61K31/426 ,  A61K31/495 ,  A61K31/496 ,  A61K31/5375 ,  A61K31/55 ,  A61K45/06 ,  A61P31/04 ,  A61P31/06

摘要： The present disclosure provides compounds, methods, and compositions which may be used to treat tuberculosis. In some embodiments, these compounds and compositions have a bactericidal property against Mycobacterium tuberculosis (Mtb). Methods of employing such agents are also provided.

公开(公告)号：US20230133011A1

公开(公告)日：2023-05-04

申请号：US17816980

申请日：2022-08-02

申请人： MONTEFIORE MEDICAL CENTER

发明人： Richard M. LOPACHIN ,  Terrence GAVIN ,  Brian GEOHAGEN

IPC分类号： A61K31/12 ,  A61K31/167 ,  A61K31/495 ,  A61K31/05 ,  A61K31/095 ,  A61K31/36 ,  A61P39/06 ,  A01N1/02 ,  A61K31/381 ,  A61K31/402 ,  A61K31/5375 ,  C07C49/80 ,  C07C49/807 ,  C07C49/825 ,  C07C49/84 ,  C07C233/33 ,  C07C323/22 ,  C07D207/04 ,  C07D207/325 ,  C07D295/112 ,  C07D333/22

摘要： Methods, filters and compositions are disclosed for treating toxicity due to oxidative stress and toxic electrophiles.

公开(公告)号：US20230090439A1

公开(公告)日：2023-03-23

申请号：US17795652

申请日：2021-01-27

申请人： Bayer Animal Health GmbH

发明人： Anne FROEHLICH ,  Andreas TURBERG ,  Sandra MENSINGER ,  Daris GRIZIC ,  Daniel GONDOL ,  William BARTON

IPC分类号： A61K31/4439 ,  A61K9/08 ,  A61K31/415 ,  A61K31/42 ,  A61K31/402 ,  A61K9/00 ,  A61P33/14

摘要： The present invention relates to a pharmaceutical composition comprising at least one pharmaceutically active ingredient, which is completely soluble in a solvent phase, characterized in that the pharmaceutically active ingredient is in particular from the group of fluorinated heteroarylamides, and that the solvent phase is configured as a solvent mixture and comprises at least one first solvent and a second solvent different from the first solvent, wherein the first solvent comprises a C1 to C15-alcohol, wherein the second solvent comprises an organic carbonate, and also wherein the first solvent is present in a proportion from 50% by weight to 95% by weight and wherein the second solvent is present in a proportion from 5% by weight to 50% by weight, based in each case on the sum total of the solvents in the solvent phase.

公开(公告)号：US11452781B2

公开(公告)日：2022-09-27

申请号：US16054412

申请日：2018-08-03

申请人： CHILDREN'S MEDICAL CENTER CORPORATION

发明人： Paolo Fiorina ,  Andrea Vergani

IPC分类号： A61P3/10 ,  A61K47/68 ,  A61K31/436 ,  A61K31/7076 ,  A61K45/06 ,  A61K31/166 ,  A61K31/402 ,  A61K31/53

摘要： The present invention relates to the role of purinergic receptors and ATP in T cell activation and autocrine system signaling. In one embodiment, the present invention provides a method of preventing or treating diabetes by administering a therapeutically effective inhibitor of ATP to a subject. In another embodiment, the present invention provides a method of preventing or treating fibrosis by administering a P2X7R soluble fusion protein. In another embodiment, the present invention provides a method of preventing or treating graft rejection by administering an inhibitor of P2X receptor signaling.

公开(公告)号：US11419870B2

公开(公告)日：2022-08-23

申请号：US16898886

申请日：2020-06-11

申请人： Novartis AG

发明人： Stephane Ferretti ,  Sebastien Jeay

IPC分类号： A61K31/506 ,  A61K31/402 ,  A61K31/404 ,  A61K31/4178 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/47 ,  A61K31/472 ,  A61K31/496 ,  A61K9/00 ,  A61K45/06

摘要： The present disclosure relates to mdm2 inhibitors for use in specific dosing schedules. It was found that if sufficiently potent or, in alternative, sufficiently high dose of a Mdm2 inhibitor is used, it can cause antineoplastic effect by triggering much longer lasting antiproliferative mechanism in cells. The long lasting effect can sustain for several weeks after a single dose, which eliminates the need for daily treatment and allows administering the Mdm2i intermittently. A treatment with the intermittent dosing schedule of a Mdm2 inhibitor can be combined with a daily treatment of the Mdm2i or with another pharmaceutically acceptable ingredient.

公开(公告)号：US11219625B2

公开(公告)日：2022-01-11

申请号：US15746043

申请日：2016-07-22

申请人： YALE UNIVERSITY ,  THE UNIVERSITY OF KANSAS

发明人： Joseph N. Contessa ,  Jennifer E. Golden ,  Daniel P. Flaherty

IPC分类号： A61K31/5377 ,  A61K31/402 ,  A61K31/426 ,  A61K31/427 ,  A61K31/454 ,  C07D295/192 ,  C07D213/75 ,  A61P35/00 ,  A61K45/06 ,  C07D277/46 ,  C07D277/82 ,  C07D295/155 ,  C07D417/12

摘要： The present invention includes novel compounds and methods for preventing or treating diseases associated with N-linked glycosylation in a subject in need thereof. The methods comprise administering to the subject an effective amount of at least one compound of the invention.

公开(公告)号：US11084784B2

公开(公告)日：2021-08-10

申请号：US15128932

申请日：2015-03-25

申请人： PIRAMAL ENTERPRISES LIMITED

发明人： Rajiv Sharma ,  Bichismita Sahu ,  Sunil Vasantrao Mali ,  Deepak Singh ,  Pramod Bhaskar Kumar ,  Mahesh Dawange ,  Hitesh Mistry

IPC分类号： C07C317/32 ,  C07D311/22 ,  C07D335/06 ,  C07D265/36 ,  C07D207/27 ,  C07D295/26 ,  C07C233/29 ,  C07C237/22 ,  A61K31/18 ,  A61K31/351 ,  C07C217/88 ,  C07C317/24 ,  C07C311/08 ,  C07C255/46 ,  C07C233/54 ,  C07C217/48 ,  C07C211/45 ,  C07C215/70 ,  C07C255/50 ,  A61K31/277 ,  C07C309/89 ,  C07C225/22 ,  C07C229/42 ,  C07C317/44 ,  A61K31/165 ,  C07C323/09 ,  A61K31/5375 ,  C07C311/37 ,  C07F5/02 ,  A61K31/402 ,  C07D317/72 ,  C07C217/76 ,  C07C205/36 ,  A61K31/382 ,  C07F7/18 ,  C07C237/52 ,  C07C311/21 ,  C07C381/10 ,  C07D211/14 ,  C07D213/30 ,  C07D231/12 ,  C07D233/58 ,  C07D257/04 ,  C07D295/088 ,  C07D295/135 ,  C07D295/192 ,  C07D305/08

摘要： The present invention relates to a compound of formula I, or an isotopic form, stereoisomer, a tautomer, a pharmaceutically acceptable salt, a solvate, a polymorph, a prodrug, N-oxide or S-oxide thereof; and processes for their preparation. The invention further relates to pharmaceutical compositions containing the compounds and their use in the treatment of diseases or disorders mediated by RORγ.

公开(公告)号：US10913714B2

公开(公告)日：2021-02-09

申请号：US15547522

申请日：2015-11-11

申请人： JIANGSU CAREPHAR PHARMACEUTICAL CO., LTD ,  NANJING CAREPHAR SHENGHUI PHARMACEUTICAL CO., LTD

发明人： Yinlin Qin ,  Mei Su ,  Qiu Jin ,  Tao Chen ,  Jianhua Jiang

IPC分类号： A61K31/454 ,  A61K31/402 ,  A61K31/4025 ,  C07D207/48 ,  C07D405/04 ,  C07D401/12 ,  C07D413/12 ,  C07D403/04 ,  A61K31/404

摘要： The present invention relates to a new pyrrole sulfonyl derivative, and a preparation method and medical use thereof. In particular, the present invention relates to a pyrrole sulfonyl derivative as represented by general formula (I), a preparation method thereof, a pharmaceutical composition comprising the derivative, and a use thereof as a therapeutic agent, in particular as a gastric acid secretion inhibitor and as potassium-competitive acid blockers (P-CABs), wherein each substituent group of general formula (I) is the same as that defined in the description.