公开(公告)号：US20230322753A1

公开(公告)日：2023-10-12

申请号：US18026793

申请日：2021-09-18

Applicant: VORONOI INC. ,  VORONOIBIO INC. ,  B2SBIO INC.

Inventor： Younho LEE ,  Juhee KANG ,  Yikyung KO ,  Jung Beom SON ,  Eunhwa KO ,  Sung Hwan KIM ,  Nam Doo KIM ,  Hwan Geun CHOI

IPC: C07D413/14 ,  C07D413/04 ,  C07D498/08 ,  A61P35/00

CPC classification number: C07D413/14 ,  C07D413/04 ,  C07D498/08 ,  A61P35/00

Abstract: The present invention relates to a pharmaceutical composition comprising a compound of the present invention, an isomer thereof, a hydrate thereof, a solvate thereof, or a pharmaceutically acceptable salt thereof as an active ingredient for prevention or treatment of cancer. The compound exhibits high inhibitory activity against epidermal growth factor receptor (EGFR) mutants or at least one of the wild-type or mutant ErbB2 and ErbB4 and as such, can be advantageously used for treatment of the cancer expressing same.

公开(公告)号：USRE49686E1

公开(公告)日：2023-10-10

申请号：US17076227

申请日：2020-10-21

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Junya Shirai ,  Hideyuki Sugiyama ,  Taku Kamei ,  Hironobu Maezaki

IPC: C07D401/04 ,  C07D207/14 ,  C07D211/58 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/10 ,  C07D405/06 ,  C07D405/12 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D413/04 ,  C07D413/06 ,  C07D413/08 ,  C07D413/14 ,  C07D417/08

CPC classification number: C07D401/04 ,  C07D207/14 ,  C07D211/58 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/10 ,  C07D405/06 ,  C07D405/12 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D413/04 ,  C07D413/06 ,  C07D413/08 ,  C07D413/14 ,  C07D417/08

Abstract: The present invention relates to a compound represented by the formula




wherein ring A is a nitrogen-containing heterocycle;

ring B is an aromatic ring optionally having substituent(s);

ring D is an aromatic ring optionally having substituent(s);

L is a group represented by the formula





R2, R3, R4a ′ and R4b are each independently a hydrogen atom, an optionally halogenated C1-6 alkyl group or an optionally halogenated C3-6 cycloalkyl group, or R2 and R3 are optionally bonded via an alkylene chain or an alkenylene chain, or R4a and R4b are optionally bonded via an alkylene chain or an alkenylene chain;
R1 is a hydrogen atom or a substituent;
m and n are each independently an integer of 0 to 5;
m+n is an integer of 2 to 5; and
is a single bond or double bond, or a salt thereof; and the like. The compound has a superior tachykinin receptor antagonistic action, and is useful as an agent for the prophylaxis or treatment of various diseases such as lower urinary tract diseases, digestive tract diseases, central neurological disease and the like.

公开(公告)号：US20230303580A1

公开(公告)日：2023-09-28

申请号：US18190224

申请日：2023-03-27

Applicant: Isosterix, Inc.

Inventor： Roopa Rai ,  Mark Bures

IPC: C07D487/04 ,  A61P35/00 ,  C07D413/06 ,  C07D307/85 ,  C07D213/56 ,  C07D405/12 ,  C07D401/04 ,  C07D413/04 ,  C07D413/12

CPC classification number: C07D487/04 ,  A61P35/00 ,  C07D413/06 ,  C07D307/85 ,  C07D213/56 ,  C07D405/12 ,  C07D401/04 ,  C07D413/04 ,  C07D413/12

Abstract: Provided herein are compounds of Formula (I). Methods for the preparation of the compounds of Formula (I) and intermediates useful in the preparation of the compounds of Formula (I) are described herein. The compounds of Formula (I) may be useful as inhibitors of the MYST family of lysine acetyltransferases (KATs) for the treatment of and/or prophylaxis of hyperproliferative diseases, disorders or conditions such as cancer. In particular, the compounds of Formula (I) are useful for the inhibition of KAT6A and KAT6B which are enzymes frequently mutated, overexpressed, amplified and/or translocated in cancer altering their normal expression, activity and function. The use of the compounds of Formula (I) in the manufacture of pharmaceutical compositions or for treating cancers is further described, including for treating cancer in combination with other anti-cancer agents.

公开(公告)号：US20230303501A1

公开(公告)日：2023-09-28

申请号：US18128603

申请日：2023-03-30

Applicant: The USA, as represented by the Secretary, Dept. of Health and Human Services ,  Pontificia Universidad Católica de Chile

Inventor： Juan J. Marugan ,  Marc Ferrer ,  Noel T. Southall ,  Andres E. Dulcey ,  Xin Hu ,  Christopher R. Dextras ,  Daniel C. Talley ,  Alejandra Alvarez ,  Silvana Zanlungo ,  Rommy M. Von Bernhardi

IPC: C07D243/38 ,  A61P25/28 ,  A61P33/06 ,  A61P35/02 ,  A61P25/08 ,  A61K31/5513 ,  A61K31/553 ,  A61K31/554 ,  C07C201/12 ,  C07C227/22 ,  C07C319/14 ,  C07D267/18 ,  C07D267/20 ,  C07D281/16 ,  C07D401/04 ,  C07D403/04 ,  C07D413/04 ,  C07D413/10 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04 ,  C07F5/02 ,  C07F7/08

CPC classification number: C07D243/38 ,  A61K31/5513 ,  A61K31/553 ,  A61K31/554 ,  A61P25/08 ,  A61P25/28 ,  A61P33/06 ,  A61P35/02 ,  C07C201/12 ,  C07C227/22 ,  C07C319/14 ,  C07D267/18 ,  C07D267/20 ,  C07D281/16 ,  C07D401/04 ,  C07D403/04 ,  C07D413/04 ,  C07D413/10 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04 ,  C07F5/025 ,  C07F7/0812

Abstract: Disclosed herein are embodiments of a compound that inhibits c-Abl tyrosine kinase (also referred to herein as “c-Abl”). The compound embodiments described herein are novel c-Abl inhibitors that can bind to c-Abl at an allosteric site and inhibit its activity in various pathways. The compound embodiments also are capable of crossing the blood brain barrier and therefore are useful in inhibiting c-Abl activity as it affects pathways and/or proteins in the brain. The compound embodiments described herein are effective therapeutic agents for treating diseases involving c-Abl, such as cancers, motor neuron diseases, and neurodegenerative diseases. Also disclosed herein are embodiments of methods for making and using the c-Abl inhibitory compound embodiments.

公开(公告)号：US11760751B2

公开(公告)日：2023-09-19

申请号：US17905531

申请日：2021-03-02

Applicant: HELIOEAST PHARMACEUTICAL CO., LTD. ,  HELIOEAST SCIENCE & TECHNOLOGY CO., LTD.

Inventor： Lingyun Wu ,  Peng Yang ,  Lele Zhao ,  Xu You ,  Jian Li ,  Shuhui Chen

IPC: C07D413/04 ,  C07D417/04 ,  C07D403/04

CPC classification number: C07D413/04

Abstract: Disclosed are a series of benzo 2-azaspiro[4.4]nonane compounds, and specifically disclosed are a compound as represented by formula (P) or a pharmaceutically acceptable salt thereof.

公开(公告)号：US20230286954A1

公开(公告)日：2023-09-14

申请号：US18319066

申请日：2023-05-17

Applicant: SYNGENTA CROP PROTECTION AG

Inventor： Sally Elizabeth RUSSELL ,  James Alan MORRIS

IPC: C07D403/04 ,  A01N43/54 ,  A01N43/58 ,  A01N43/80 ,  A01N43/90 ,  C07D401/04 ,  C07D401/14 ,  C07D409/14 ,  C07D413/04 ,  C07D471/04 ,  C07D487/04 ,  A01N43/56 ,  C07D207/337 ,  C07D207/34 ,  C07D207/325

CPC classification number: C07D403/04 ,  A01N43/54 ,  A01N43/58 ,  A01N43/80 ,  A01N43/90 ,  C07D401/04 ,  C07D401/14 ,  C07D409/14 ,  C07D413/04 ,  C07D471/04 ,  C07D487/04 ,  A01N43/56 ,  C07D207/337 ,  C07D207/34 ,  C07D207/325

Abstract: The present invention relates to pyrazole derivatives of formula (X)






wherein ring A is a pyrazole and substituents RB1, RB2, n, RQ1, RQ2, RQ3, and RQ4 are as defined in claim 1, their manufacture, and their use in the manufacture of agrochemicals and pharmaceuticals.

公开(公告)号：US20230265083A1

公开(公告)日：2023-08-24

申请号：US18041223

申请日：2021-08-10

Applicant: Prelude Therapeutics Incorporated

Inventor： Liang Lu ,  Andrew P. Combs ,  Chaofeng Dai ,  Raul A. Leal

IPC: C07D413/04 ,  C07D401/04 ,  C07D405/04

CPC classification number: C07D413/04 ,  C07D401/04 ,  C07D405/04

Abstract: The disclosure is directed to, in part, to heterocycle CDK inhibitors, pharmaceutical compositions comprising the same, as well as methods of their use and preparation.

公开(公告)号：US20230265061A1

公开(公告)日：2023-08-24

申请号：US17905847

申请日：2021-03-16

Applicant: Sumitomo Pharma Co., Ltd.

Inventor： Yoshiaki ISOBE ,  Tomoyuki TANAKA ,  Hirotaka MIYACHI

IPC: C07D271/06 ,  A61K45/06 ,  C07D413/04 ,  A61P25/08 ,  A61P25/24

CPC classification number: C07D271/06 ,  A61K45/06 ,  C07D413/04 ,  A61P25/08 ,  A61P25/24

Abstract: The present invention relates to a compound of formula (1) wherein Q1 is halogen atom, Q2 is hydrogen atom, etc., X, Y, and Z are nitrogen atom or oxygen atom, and R1 has a given structure, or a pharmaceutically acceptable salt thereof, and a medicament comprising the compound for treating and/or preventing a disease such as epilepsy.

公开(公告)号：US11724997B2

公开(公告)日：2023-08-15

申请号：US16971227

申请日：2019-02-28

Applicant: Annapurna Bio, Inc.

Inventor： Haifeng Tang ,  Sarah Boyce ,  Michael Hanson ,  Zhe Nie

IPC: C07D401/04 ,  C07D249/14 ,  C07D401/14 ,  C07D403/04 ,  C07D405/04 ,  C07D405/14 ,  C07D413/04

CPC classification number: C07D401/04 ,  C07D249/14 ,  C07D401/14 ,  C07D403/04 ,  C07D405/04 ,  C07D405/14 ,  C07D413/04

Abstract: This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt and/or hydrate and/or prodrug of the compound) that modulate (e.g., agonize) the apelin receptor (also referred to herein as the APJ receptor; gene symbol “APLNR”). This disclosure also features compositions containing the same as well as other methods of using and making the same. The chemical entities are useful, e.g., for treating a subject (e.g., a human) having a disease, disorder, or condition in which a decrease in APJ receptor activity (e.g., repressed or impaired APJ receptor signaling; e.g., repressed or impaired apelin-APJ receptor signaling) or downregulation of endogenous apelin contributes to the pathology and/or symptoms and/or progression of the disease, disorder, or condition. Non-limiting examples of such diseases, disorders, or conditions include: (i) cardiovascular disease; (ii) metabolic disorders; (iii) diseases, disorders, and conditions associated with vascular pathology; and (iv) organ failure; (v) diseases, disorders, and conditions associated with infections (e.g., microbial infections); and (vi) diseases, disorders, or conditions that are sequela or comorbid with any of the foregoing or any disclosed herein. More particular non-limiting examples of such diseases, disorders, or conditions include pulmonary hypertension (e.g., PAH); heart failure; type II diabetes; renal failure; sepsis; and systemic hypertension.

公开(公告)号：US11717501B2

公开(公告)日：2023-08-08

申请号：US16393298

申请日：2019-04-24

Applicant: Neurocentria, Inc.

Inventor： Guosong Liu ,  Fei Mao ,  Jason Gregory Weinger

IPC: A01N43/40 ,  A61K31/44 ,  C07D413/04 ,  C07D413/14 ,  A61K31/191 ,  A61K9/00 ,  A61P25/28 ,  A61K31/20 ,  A61K33/06 ,  A61K47/44

CPC classification number: A61K31/191 ,  A61K9/0053 ,  A61K31/20 ,  A61K33/06 ,  A61K47/44 ,  A61P25/28

Abstract: Provided is a dosage form comprising magnesium threonate having enhanced efficacy. Also provided is a pharmacokinetic profile of magnesium threonate having enhanced efficacy. The dosage forms and pharmacokinetic profile of magnesium threonate are used to treat a variety of diseases, disorders, syndromes and/or conditions.