公开(公告)号：US20240360165A1

公开(公告)日：2024-10-31

申请号：US18635402

申请日：2024-04-15

Applicant: Syros Pharmaceuticals, Inc.

Inventor： Jason J. MARINEAU ,  Robert Zahler ,  Stephane Ciblat ,  Dana K. Winter ,  Anzhelika Kabro ,  Stephanie Roy ,  Darby Schmidt ,  Claudio Chuaqui ,  Goran Malojcic ,  Henri Piras ,  Kenneth Matthew Whitmore ,  Kate-Lyn Lund ,  William Sinko ,  Kevin Sprott

IPC: C07F9/6558 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08

CPC classification number: C07F9/65583 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08

Abstract: The present invention provides novel compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of cyclin-dependent kinase 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.

公开(公告)号：US20240360155A1

公开(公告)日：2024-10-31

申请号：US18584520

申请日：2024-02-22

Applicant: Enanta Pharmaceuticals, Inc.

Inventor： Brian C. SHOOK ,  In Jong KIM ,  Thomas P. BLAISDELL ,  Jianming YU ,  Joseph D. PANARESE ,  Yat Sun OR

IPC: C07D513/04 ,  A61K31/5513 ,  A61K31/56 ,  A61K31/58 ,  A61K45/06 ,  C07D243/16 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/08 ,  C07D491/048 ,  C07D495/04 ,  C07D498/08

CPC classification number: C07D513/04 ,  A61K31/5513 ,  A61K31/56 ,  A61K31/58 ,  A61K45/06 ,  C07D243/16 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/08 ,  C07D491/048 ,  C07D495/04 ,  C07D498/08

Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof:




which inhibit Respiratory Syncytial Virus (RSV). The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from RSV infection. The invention also relates to methods of treating an RSV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

公开(公告)号：US20240360152A1

公开(公告)日：2024-10-31

申请号：US18659374

申请日：2024-05-09

Applicant: Arvinas Operations, Inc.

Inventor： Erika Marina Vieira Araujo ,  Michael Berlin ,  Hanqing Dong ,  Steven M. Sparks ,  Jing Wang ,  Wei Zhang

IPC: C07D498/10 ,  A61K45/06 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/08 ,  C07D487/10

CPC classification number: C07D498/10 ,  A61K45/06 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/08 ,  C07D487/10

Abstract: Bifunctional compounds, which find utility as modulators of leucine-rich repeat kinase 2 (LRRK2), are described herein. In particular, the hetero-bifunctional compounds of the present disclosure contain on one end a moiety that binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds LRRK2, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The hetero-bifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aberrant regulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

公开(公告)号：US20240360118A1

公开(公告)日：2024-10-31

申请号：US18506164

申请日：2023-11-10

Applicant: Novartis AG

Inventor： Vincent BORDAS ,  Jvan BRUN ,  Andrea DECKER ,  Markus FUREGATI ,  Geoffrey GOGNIAT ,  Wanben GONG ,  Jacques HAMON ,  Jürgen Hans-Hermann HINRICHS ,  Philipp HOLZER ,  Fatma LIMAM ,  Henrik MÖBITZ ,  Sandro NOCITO ,  Simone PLATTNER ,  Niko SCHMIEDEBERG ,  Joseph SCHOEPFER ,  Jessica SOTO ,  Ross Sinclair STRANG ,  Shuping YAO ,  Huangchao YU ,  Frédéric ZECRI ,  Sisi ZHANG

IPC: C07D413/14 ,  C07D401/14 ,  C07D405/14

CPC classification number: C07D413/14 ,  C07D401/14 ,  C07D405/14 ,  C07B2200/13

Abstract: The present invention provides a compound, or a pharmaceutically acceptable salt thereof, of formula (I):




wherein R1, R2, R3, R4, R5, R26, R27, y, R, M, W, L, V, T, Y, J, K and A are as described herein, therapeutic uses of said compounds, uses of said compounds as research chemicals, a pharmaceutical composition and combinations comprising said compounds, and methods for manufacturing the compounds of the invention.

公开(公告)号：US20240360085A1

公开(公告)日：2024-10-31

申请号：US18672406

申请日：2024-05-23

Applicant: Kadmon Corporation, LLC

Inventor： Kevin G. Liu ,  Kellen Olszewski ,  Ji-In Kim ,  Masha V. Poyurovsky ,  Koi Morris ,  Xuemei Yu ,  Christophe Lamarque

IPC: C07D239/42 ,  C07D239/94 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D473/34 ,  C07D491/048 ,  C07D491/052 ,  C07D495/04 ,  C07D519/00

CPC classification number: C07D239/42 ,  C07D239/94 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D473/34 ,  C07D491/048 ,  C07D491/052 ,  C07D495/04 ,  C07D519/00

Abstract: This invention provides compounds that modulate glucose uptake activity and cellular transport/uptake of glucose, and particularly GLUT3, but also including but not limited to GLUT1-14 (SLC2A1-SLC2A14). Compounds of the invention are useful for treating diseases, including cancer, autoimmune diseases and inflammation, infectious diseases, and metabolic diseases.

公开(公告)号：US20240360084A1

公开(公告)日：2024-10-31

申请号：US18633495

申请日：2024-04-11

Applicant: REATA PHARMACEUTICALS, INC.

Inventor： Xin JIANG ,  Melean VISNICK ,  Christopher F. BENDER ,  Gary BOLTON ,  Bradley CAPRATHE ,  Chitase LEE ,  Brian KORNBERG ,  Patrick O'BRIEN ,  Martha R. HOTEMA

IPC: C07D231/54 ,  C07D235/02 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D403/14 ,  C07D405/04 ,  C07D409/04 ,  C07D413/10 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

CPC classification number: C07D231/54 ,  C07D235/02 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D403/14 ,  C07D405/04 ,  C07D409/04 ,  C07D413/10 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

Abstract: Disclosed herein are compounds of the formula:




as well as analogs thereof, wherein the variables are defined herein. Also provided are pharmaceutical compositions thereof. In some aspects, the compounds and compositions provided herein may be used to modulate the activity of IL-17 and RORγ. Also provided are methods of administering compounds and composition provided herein to a patient in need thereof, for example, for the treatment or prevention of diseases or disorders associated with inflammation or for autoimmune disorders.

公开(公告)号：US12129236B2

公开(公告)日：2024-10-29

申请号：US17204206

申请日：2021-03-17

Applicant: CANCER RESEARCH TECHNOLOGY LIMITED

Inventor： Alison E. McGonagle ,  Allan M. Jordan ,  Bohdan Waszkowycz ,  Colin P. Hutton ,  Ian D. Waddell ,  James R. Hitchin ,  Kate M. Smith ,  Niall M. Hamilton

IPC: C07D235/26 ,  A61P35/00 ,  C07D307/85 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D405/04 ,  C07D405/06 ,  C07D409/04 ,  C07D413/04 ,  C07D413/06 ,  C07D413/14 ,  C07D417/04 ,  C07D417/06 ,  C07D417/14

CPC classification number: C07D235/26 ,  A61P35/00 ,  C07D307/85 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D405/04 ,  C07D405/06 ,  C07D409/04 ,  C07D413/04 ,  C07D413/06 ,  C07D413/14 ,  C07D417/04 ,  C07D417/06 ,  C07D417/14

Abstract: The present invention relates to compounds of formula I that function as inhibitors of PARG (Poly ADP-ribose glycohydrolase) enzyme activity: wherein R1a, R1b, R1c, R1d, W, X1, X2, X3, X4, X5, X6, X7, c are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which PARG activity is implicated.

公开(公告)号：US20240351987A1

公开(公告)日：2024-10-24

申请号：US18615563

申请日：2024-03-25

Applicant: Escient Pharmaceuticals, Inc.

Inventor： Marion LANIER ,  Marcus BOEHM ,  Liming HUANG ,  Esther MARTINBOROUGH ,  Marcos SAINZ ,  Brandon SELFRIDGE ,  Adam YEAGER

IPC: C07D215/44 ,  C07D239/94 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04

CPC classification number: C07D215/44 ,  C07D239/94 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04

Abstract: Methods are provided for modulating MRGPR X2 generally, or for treating a MRGPR X2 dependent condition more specifically, by contacting the MRGPR X2 or administering to a subject in need thereof, respectively, an effective amount of a compound having structure (I):




or a pharmaceutically acceptable salt, isomer, hydrate, solvate or isotope thereof, wherein W, Z, R1, R2, R3, R4, R5, R6 and Rx are as defined herein. Pharmaceutical compositions containing such compounds, as well as the compounds themselves, are also provided.

公开(公告)号：US20240343699A1

公开(公告)日：2024-10-17

申请号：US18740059

申请日：2024-06-11

Applicant: Supernus Pharmaceuticals, Inc.

Inventor： Janak Khimchand Padia ,  Chungping Yu

IPC: C07D265/30 ,  A61K31/5375 ,  A61K31/5377 ,  C07D413/14

CPC classification number: C07D265/30 ,  A61K31/5375 ,  A61K31/5377 ,  C07D413/14

Abstract: A compound of Formula I includes a stereoisomer thereof and/or a salt thereof; wherein R1 is a substituted alkane group, a heterocylic group, or a pyridine group; X is hydrogen, a halogen, an amino acid residue, a substituted amino acid residue, an alkyl group, or an ester. Such compounds may be used in pharmaceutical compositions and for the treatment of central nervous system (CNS) disorders:

公开(公告)号：US20240341178A1

公开(公告)日：2024-10-10

申请号：US18592645

申请日：2024-03-01

Applicant: ROHM AND HAAS ELECTRONIC MATERIALS KOREA LTD.

Inventor： Hee-Ryong KANG ,  So-Young JUNG ,  Hyo-Soon PARK ,  Jeong-Eun YANG ,  Sang-Hee CHO ,  So-Mi PARK

IPC: H10K85/60 ,  C07D413/04 ,  C07D413/14 ,  C09K11/06 ,  H10K50/11 ,  H10K101/00

CPC classification number: H10K85/657 ,  C07D413/04 ,  C07D413/14 ,  C09K11/06 ,  H10K85/615 ,  H10K85/636 ,  H10K85/654 ,  H10K85/6574 ,  C09K2211/1018 ,  H10K50/11 ,  H10K2101/90

Abstract: The present disclosure relates to a plurality of host materials, an organic electroluminescent compound, and an organic electroluminescent device comprising the same. By comprising a plurality of host materials and/or an organic electroluminescent compound according to the present disclosure, an organic electroluminescent device having low driving voltage and/or high luminous efficiency and/or long lifespan characteristics can be provided.