公开(公告)号：US20240294539A1

公开(公告)日：2024-09-05

申请号：US18626788

申请日：2024-04-04

Applicant: Bayer Aktiengesellschaft

Inventor： Thomas HIMMLER ,  Peter BRUECHNER ,  Werner LINDNER ,  Julia Johanna HAHN ,  Wahed Ahmed MORADI ,  Reiner FISCHER ,  Michael DOCKNER

IPC: C07D491/113 ,  C07C229/48 ,  C07C233/52 ,  C07D209/54

CPC classification number: C07D491/113 ,  C07C229/48 ,  C07C233/52 ,  C07D209/54 ,  C07C2601/14 ,  C07C2601/16

Abstract: The present invention relates to a novel process for preparing substituted cyclohexane amino acid esters and spiroketal-substituted cyclic keto-enols, and to novel intermediates or starting compounds that are passed through or used in the process according to the invention.

公开(公告)号：US12076306B2

公开(公告)日：2024-09-03

申请号：US18144890

申请日：2023-05-09

Applicant: Alkermes Pharma Ireland Limited

Inventor： Tarek A. Zeidan ,  Scott Duncan ,  Christopher P. Hencken ,  Thomas Andrew Wynn ,  Carlos N. Sanrame

IPC: C07C235/88 ,  A61K31/225 ,  C07C219/08 ,  C07C229/16 ,  C07C233/18 ,  C07C233/91 ,  C07C317/18 ,  C07C317/28 ,  C07D207/06 ,  C07D207/40 ,  C07D209/52 ,  C07D211/06 ,  C07D211/38 ,  C07D295/088 ,  C07D491/113

CPC classification number: A61K31/225 ,  C07C219/08 ,  C07C229/16 ,  C07C233/18 ,  C07C233/91 ,  C07C235/88 ,  C07C317/18 ,  C07C317/28 ,  C07D207/06 ,  C07D207/40 ,  C07D209/52 ,  C07D211/06 ,  C07D211/38 ,  C07D295/088 ,  C07D491/113

Abstract: The present invention provides compounds of formula (I), and pharmaceutical compositions thereof.

公开(公告)号：US20240246910A1

公开(公告)日：2024-07-25

申请号：US18405058

申请日：2024-01-05

Applicant: Sensorium Therapeutics, Inc.

Inventor： Jacob M. Hooker ,  Michael S. Placzek

IPC: C07D209/12 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D475/04 ,  C07D491/113 ,  C07D491/20 ,  C07D495/04 ,  C07D495/10 ,  C07D497/10 ,  C07D498/10 ,  C07D519/00 ,  C07F7/18

CPC classification number: C07D209/12 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D475/04 ,  C07D491/113 ,  C07D491/20 ,  C07D495/04 ,  C07D495/10 ,  C07D497/10 ,  C07D498/10 ,  C07D519/00 ,  C07F7/1804

Abstract: Disclosed are prodrug compounds that can be converted to mesembrine under biologically relevant conditions, such as hydrolysis in vivo; and related methods of preparing and using these compounds. Stable preparations of isolated mesembrine stereoisomers are also provided.

公开(公告)号：US12042541B2

公开(公告)日：2024-07-23

申请号：US18194540

申请日：2023-03-31

Applicant: ARBUTUS BIOPHARMA CORPORATION

Inventor： Muthiah Manoharan ,  Muthusamy Jayaraman ,  Kallanthottathil G. Rajeev ,  Laxman Eltepu ,  Steven Ansell ,  Jianxin Chen

IPC: A61K47/44 ,  A61K9/127 ,  A61K31/7088 ,  A61K31/713 ,  A61K39/00 ,  A61K39/39 ,  A61K47/10 ,  A61K47/18 ,  A61K47/20 ,  A61K47/28 ,  C07C229/08 ,  C07C229/30 ,  C07C237/16 ,  C07C251/38 ,  C07C251/78 ,  C07C271/12 ,  C07C271/20 ,  C07C323/25 ,  C07D203/10 ,  C07D317/28 ,  C07D317/44 ,  C07D317/46 ,  C07D317/72 ,  C07D319/06 ,  C07D405/12 ,  C07D491/056 ,  C07D491/113 ,  C12N15/11 ,  C12N15/113

CPC classification number: A61K47/44 ,  A61K9/1272 ,  A61K31/7088 ,  A61K31/713 ,  A61K39/00 ,  A61K39/39 ,  A61K47/10 ,  A61K47/18 ,  A61K47/20 ,  A61K47/28 ,  C07C229/08 ,  C07C229/30 ,  C07C237/16 ,  C07C251/38 ,  C07C251/78 ,  C07C271/12 ,  C07C271/20 ,  C07C323/25 ,  C07D203/10 ,  C07D317/28 ,  C07D317/44 ,  C07D317/46 ,  C07D317/72 ,  C07D319/06 ,  C07D405/12 ,  C07D491/056 ,  C07D491/113 ,  C12N15/111 ,  C12N15/113 ,  A61K2039/55555 ,  A61K2039/55561 ,  C12N2310/14 ,  C12N2310/3515 ,  C12N2320/32 ,  Y02A50/30

Abstract: The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure




wherein:



R1 and R2 are each independently for each occurrence optionally substituted C10-C30 alkyl, optionally substituted C10-C30 alkenyl, optionally substituted C10-C30 alkynyl, optionally substituted C10-C30 acyl, or -linker-ligand; R3 is H, optionally substituted C1-C10 alkyl, optionally substituted C2-C10 alkenyl, optionally substituted C2-C10 alkynyl, alkylhetrocycle, alkylphosphate, alkylphosphorothioate, alkylphosphorodithioate, alkylphosphonates, alkylamines, hydroxyalkyls, ω-aminoalkyls, ω-(substituted)aminoalkyls, ω-phosphoalkyls, ω-thiophosphoalkyls, optionally substituted polyethylene glycol (PEG, mw 100-40K), optionally substituted mPEG (mw 120-40K), heteroaryl, heterocycle, or linker-ligand; and E is C(O)O or OC(O).

公开(公告)号：US20240116897A1

公开(公告)日：2024-04-11

申请号：US18274864

申请日：2022-01-21

Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY ,  PINOTBIO, INC.

Inventor： Kwang Rok KIM ,  Kwan Young JEONG ,  Hee Jung JUNG ,  Doyoun KIM ,  Junmi LEE ,  Sang Dal RHEE ,  Kyu Myung LEE

IPC: C07D403/12 ,  A61P35/00 ,  C07D235/32 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D471/10 ,  C07D487/08 ,  C07D491/113 ,  C07D513/04

CPC classification number: C07D403/12 ,  A61P35/00 ,  C07D235/32 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D471/10 ,  C07D487/08 ,  C07D491/113 ,  C07D513/04

Abstract: The present invention relates to a benzothiazole or benzimidazole derivative, a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising same as an active ingredient for prevention or treatment of SIRTUIN 7 protein-related diseases. With excellent inhibitory activity against SIRTUIN 7 protein the derivative can be used for preventing or treating SIRTUIN 7 protein-related diseases.

公开(公告)号：US20240101549A1

公开(公告)日：2024-03-28

申请号：US18257123

申请日：2021-12-16

Applicant: AstraZeneca AB

Inventor： Jonas BRÅNALT ,  Björn HOLM ,  Maria JOHANSSON ,  Olle KARLSSON ,  Daniel Laurent KNERR ,  Anneli NORDQVIST ,  Robert John SHEPPARD ,  Marianne SWANSON ,  Anna TOMBERG

IPC: C07D417/14 ,  C07D493/10 ,  C07D487/04 ,  C07D491/107 ,  C07D491/113 ,  C07D487/10 ,  C07D498/08 ,  C07D495/10 ,  A61P1/16

CPC classification number: C07D417/14 ,  C07D493/10 ,  C07D487/04 ,  C07D491/107 ,  C07D491/113 ,  C07D487/10 ,  C07D498/08 ,  C07D495/10 ,  A61P1/16

Abstract: Compounds having the structure of Formula (I): and pharmaceutically acceptable salts thereof, wherein X1, R1, R2, R3, R4, R5 and R6 are as defined in the specification; pharmaceutical compositions comprising such compounds and salts; use of such compounds and salts to treat or prevent Prolyl endopeptidase fibroblast activation protein (FAP)-mediated conditions; kits comprising such compounds and salts; and methods for manufacturing such compounds and salts.

公开(公告)号：US20230150993A1

公开(公告)日：2023-05-18

申请号：US17930352

申请日：2022-09-07

Applicant: Merck Patent GmbH ,  Vertex Pharmaceuticals Incorporated

Inventor： Henry YU ,  Michael Clark ,  Guy Bemis ,  Micheal Boyd ,  Kishan Chandupatla ,  Philip Collier ,  Hongbo Deng ,  Huijun Dong ,  Warren Dorsch ,  Russell R. Hoover ,  Mac Arthur Johnson, JR. ,  Shashank Kulkarni ,  Marina Penney ,  Steven Ronkin ,  Darin Takemoto ,  Qing Tang ,  Nathan D. Waal ,  Tiansheng Wang ,  David J. Lauffer ,  Pan Li

IPC: C07D413/14 ,  A61P35/00 ,  C07D417/14 ,  C07D491/107 ,  C07D401/14 ,  C07D413/04 ,  C07D491/113 ,  C07D403/04

CPC classification number: C07D413/14 ,  A61P35/00 ,  C07D417/14 ,  C07D491/107 ,  C07D401/14 ,  C07D413/04 ,  C07D491/113 ,  C07D403/04

Abstract: The present invention provides compounds of Formula I′, or pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and methods of use thereof for treating cellular proliferative disorders (e.g., cancer).

公开(公告)号：US20180221510A1

公开(公告)日：2018-08-09

申请号：US15788575

申请日：2017-10-19

Applicant: Arbutus Biopharma Corporation

Inventor： Muthiah Manoharan ,  Kallanthottathil G. Rajeev ,  Muthusamy Jayaraman ,  Michael E. Jung

IPC: A61K48/00 ,  A61K47/18 ,  A61K47/14 ,  C07C229/12 ,  A61K31/7088 ,  C07D491/113 ,  C07C323/25 ,  C07C251/38 ,  A61K31/713

CPC classification number: A61K48/0033 ,  A61K31/7088 ,  A61K31/713 ,  A61K47/14 ,  A61K47/18 ,  C07C229/12 ,  C07C251/38 ,  C07C323/25 ,  C07C2601/02 ,  C07D491/113

Abstract: A lipid particle can include a cationic lipid. The cationic lipid can include one or more hydrophobic tails, which can include one or more sites of unsaturation. The sites of unsaturation can include cycloalkyl groups, e.g., cyclopropyl, cyclobutyl, cyclopentyl, or cyclohexyl groups. The lipid particle is suitable for delivering an active agent.

公开(公告)号：US10028937B2

公开(公告)日：2018-07-24

申请号：US15434789

申请日：2017-02-16

Applicant: AbbVie Inc.

Inventor： Mary E. Bellizzi ,  David A. Betebenner ,  Jean-Christophe C. Califano ,  William A. Carroll ,  Daniel D. Caspi ,  David A. DeGoey ,  Pamela L. Donner ,  Charles A. Flentge ,  Yi Gao ,  Charles W. Hutchins ,  Douglas K. Hutchinson ,  Tammie K. Jinkerson ,  Warren M. Kati ,  Ryan G. Keddy ,  Allan C. Krueger ,  Wenke Li ,  Dachun Liu ,  Clarence J. Maring ,  Mark A. Matulenko ,  Christopher E. Motter ,  Lissa T. Nelson ,  Sachin V. Patel ,  John K. Pratt ,  John T. Randolph ,  Todd W. Rockway ,  Kathy Sarris ,  Michael D. Tufano ,  Seble H. Wagaw ,  Rolf Wagner ,  Kevin R. Woller

IPC: A61K38/00 ,  C07K16/00 ,  A61K31/4184 ,  A61K31/454 ,  A61K31/4439 ,  A61K31/422 ,  A61K31/4418 ,  A61K31/4545 ,  A61K31/695 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/438 ,  A61K31/435

CPC classification number: A61K31/454 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/422 ,  A61K31/435 ,  A61K31/4355 ,  A61K31/438 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/695 ,  A61K45/06 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D453/00 ,  C07D491/113 ,  C07F7/02 ,  Y02P20/582

Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.

公开(公告)号：US20180201603A1

公开(公告)日：2018-07-19

申请号：US15918195

申请日：2018-03-12

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Michael J. Orwat ,  Donald J. P. Pinto ,  Leon M. Smith, II ,  Shefali Srivastava

IPC: C07D401/14 ,  C07D491/113 ,  A61K31/4725 ,  C07D491/10 ,  C07D487/10 ,  C07D487/08 ,  C07D487/04 ,  C07D471/10 ,  C07D413/14 ,  C07D401/10 ,  C07D401/04 ,  C07D217/26 ,  C07D491/107 ,  A61K31/551 ,  A61K31/55 ,  A61K31/541 ,  A61K31/5377 ,  A61K31/496

CPC classification number: C07D401/14 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  A61K31/551 ,  A61P7/02 ,  C07B2200/13 ,  C07D217/26 ,  C07D401/04 ,  C07D401/10 ,  C07D413/14 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D491/10 ,  C07D491/107 ,  C07D491/113

Abstract: The present invention provides compounds of Formula (I): or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments.