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公开(公告)号:US20240368120A1
公开(公告)日:2024-11-07
申请号:US18622057
申请日:2024-03-29
Applicant: Terns Pharmaceuticals, Inc.
Inventor: Gary W. LUEHR , Christopher T. JONES , Kevin P. QUINN
IPC: C07D401/14 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , C07D401/06 , C07D401/10 , C07D401/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
Abstract: The present application provides compounds that may be used as a glucagon-like peptide-1 receptors (GLP-1R) agonist, or pharmaceutically acceptable salts thereof. Also provided are pharmaceutical compositions containing such compounds, or pharmaceutically acceptable salts thereof. Methods of preparing these compounds and compositions, and methods of using these compounds and compositions to treat or prevent a disease or a condition mediated by GLP-1R, are also provided.
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公开(公告)号:US20240368087A1
公开(公告)日:2024-11-07
申请号:US18433099
申请日:2024-02-05
Applicant: VANDERBILT UNIVERSITY , The UAB Research Foundation , The Trustees of the University of Pennsylvania , The Trustees of the University of Pennsylvania
Inventor: David J. MALONEY , Alex Gregory WATERSON , Ganesh Rai BANTUKALLU , Kyle Ryan BRIMACOMBE , Plamen CHRISTOV , Chi V. DANG , Victor DARLEY-USMAR , Xin HU , Ajit JADHAV , Somnath JANA , Kwangho KIM , Jennifer L. KOUZNETSOVA , William J. MOORE , Bryan T. MOTT , Leonard M. NECKERS , Anton SIMEONOV , Gary Allen SULIKOWSKI , Daniel Jason URBAN , Shyh Ming YANG
IPC: C07D231/20 , A61K31/415 , A61K31/4155 , A61K31/4178 , A61K31/422 , A61K31/427 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/501 , A61K31/506 , A61K31/519 , A61K31/5355 , A61K45/06 , C07D231/38 , C07D401/04 , C07D403/04 , C07D403/06 , C07D409/04 , C07D413/04 , C07D417/04 , C07D417/14 , C07D471/04 , C07D495/04 , C07D495/14
Abstract: Provided is a compound of formula (I) in which Ar1, R1, U, V, W, X, and p are as described herein. Also provided are methods of using a compound of formula (I), including a method of treating cancer, a method of treating a patient with cancer cells resistant to an anti-cancer agent, and a method of inhibiting lactate dehydrogenase A (LDHA) and/or lactate dehydrogenase B (LDHB) activity in a cell.
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公开(公告)号:US20240366608A1
公开(公告)日:2024-11-07
申请号:US18262155
申请日:2022-01-19
Applicant: Lupin Limited
Inventor: Mandar Ramesh Bhonde , Sukanya Patra , Venkata P. Palle , Rajender Kumar Kamboj
IPC: A61K31/519 , A61K31/415 , A61K31/4439 , A61K31/496 , A61K31/506 , A61K31/517 , A61K31/5377 , A61K31/7068 , A61P35/00
Abstract: This disclosure relates to pharmaceutical combinations for treating and/or preventing cancer and methods and uses thereof. More particularly, provided is a pharmaceutical combination comprising a SOS1 Inhibitor and an additional active ingredient selected from a KRAS inhibitor such as a KRAS G12C inhibitor and a KRASG12D inhibitor, KRAS G13C inhibitor, and panKRAS inhibitor; an EGFR inhibitor; an ERK1/2 inhibitor; a BRAF inhibitor; a pan-RAF inhibitor; a MEK inhibitor; a AKT inhibitor; a SHP2 inhibitor; protein arginine methyltransferases (PRMTs) inhibitor such as a PRMT5 inhibitor and Type 1 PRMT inhibitor; a PI3K inhibitor; a cyclin-dependent kinase (CDK) inhibitor such as CDK4/6 inhibitor; a FGFR inhibitor; a c-Met inhibitor; a RTK inhibitor; a non-receptor tyrosine kinase inhibitor; a histone methyltransferases (HMTs) inhibitor; a DNA methyltransferases (DNMTs) inhibitor; a Focal Adhesion Kinase (FAK) inhibitor; a Bcr-Abl tyrosine kinase inhibitor; a mTOR inhibitor; a PD1 inhibitor; a PD-L1 inhibitor; CTLA4 inhibitor; and chemotherapeutic agents such as gemcitabine, doxorubicin, cisplatin, carboplatin, paclitaxel, docetaxel, topotecan, irinotecan and temozolomide.
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公开(公告)号:US20240366580A1
公开(公告)日:2024-11-07
申请号:US18566931
申请日:2022-06-01
Applicant: Zim Laboratories Limited
Inventor: Chandrashekhar Mainde , Uttam Kedar , Kuldeep Gangawat
IPC: A61K31/4439 , A61K9/48 , A61K31/661
Abstract: The present invention relates to novel pharmaceutical compositions comprising dabigatran etexilate or salt thereof for the prophylaxis and treatment of Deep Venous Thrombosis and Pulmonary Embolism. The pharmaceutical composition comprising dabigatran etexilate or salt thereof, glycerophosphoric acid (GPA) along with one or more pharmaceutically acceptable excipient.
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35.
公开(公告)号:US20240360104A1
公开(公告)日:2024-10-31
申请号:US18553988
申请日:2022-04-26
Applicant: Dana-Farber Cancer Institute, Inc.
Inventor: Nathanael S. Gray , Tinghu Zhang , Mengyang Fan , Jianwei Che , Wenchao Lu , Sirano Dhe-Paganon , Nicholas Paul Kwiatkowski
IPC: C07D403/12 , A61K31/40 , A61K31/4155 , A61K31/4178 , A61K31/4192 , A61K31/422 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/551 , C07D207/14 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D495/04
CPC classification number: C07D403/12 , A61K31/40 , A61K31/4155 , A61K31/4178 , A61K31/4192 , A61K31/422 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/551 , C07D207/14 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D495/04
Abstract: Provided herein are compounds of Formula (I′), Formula (II), Formula (III), Formula (IV), Formula (V), Formula (VI), Formula (VII), or Formula (VIII) and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, or prodrugs thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing diseases (e.g., proliferative diseases (e.g., cancers, such as carcinoma, sarcoma, lung cancer, thyroid cancer, skin cancer, ovarian cancer, colorectal cancer, prostate cancer, pancreatic cancer, esophageal cancer, liver cancer, breast cancer)) in a subject. Provided are methods of inhibiting a TEAD transcription factors (e.g., TEAD1, TEAD2, TEAD3, TEAD4) in a subject.
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36.
公开(公告)号:US20240351986A1
公开(公告)日:2024-10-24
申请号:US18683623
申请日:2022-07-26
Inventor: Youhong HU , Yi CHEN , Zhicheng XIE , Jian DING , Xin LI , Yanfen FANG , Qianqian SHEN
IPC: C07D213/75 , A61K31/4418 , A61K31/443 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4985 , A61K31/505 , A61K31/5377 , A61K31/5383 , A61K31/55 , A61P35/00 , C07D239/42 , C07D401/04 , C07D401/12 , C07D405/04 , C07D405/12 , C07D487/04 , C07D498/04
CPC classification number: C07D213/75 , A61K31/4418 , A61K31/443 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4985 , A61K31/505 , A61K31/5377 , A61K31/5383 , A61K31/55 , A61P35/00 , C07D239/42 , C07D401/04 , C07D401/12 , C07D405/04 , C07D405/12 , C07D487/04 , C07D498/04
Abstract: The present invention relates to a urea compound containing 2-heteroaromatic ring substitution represented by formula (I), its enantiomers, diastereomers, racemates or mixtures thereof, or pharmaceutically acceptable salts thereof, solvate, metabolite or prodrug. The compound of formula (I) of the present invention has inhibitory activity against CDK9, and representative compounds have significant anti-tumor activity against CDK9 high-expressing tumor cells. Representative compounds have plasma stability and low clearance.
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公开(公告)号:US20240350468A1
公开(公告)日:2024-10-24
申请号:US18751439
申请日:2024-06-24
Applicant: AICURIS GMBH & CO. KG
Inventor: Yogeshwar BACHHAV , Wilfried SCHWAB , Alexander BIRKMANN , Susanne BONSMANN , Thomas GOLDNER
IPC: A61K31/4439 , A61K9/00 , A61K45/06 , C07D417/12
CPC classification number: A61K31/4439 , A61K9/0014 , A61K45/06 , C07D417/12
Abstract: The present invention relates to the field of anti-viral active agents, particularly to salts, more particularly to a maleate salt of the free base of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)-phenyl]-acetamide, to pharmaceutical formulations thereof as well as to methods for the production of these salts. The present invention also relates to the use of theses salts and of respective pharmaceutical formulations thereof in methods of treatment and/or prevention of human herpes simplex virus infections, particularly infections caused by HSV-1 and HSV-2.
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公开(公告)号:US12121511B2
公开(公告)日:2024-10-22
申请号:US17159485
申请日:2021-01-27
Applicant: Gilead Sciences, Inc.
Inventor: Stephen E. Ammann , Gediminas J. Brizgys , James S. Cassidy , Elbert Chin , Chienhung Chou , Jeromy J. Cottell , Chao-I Hung , Kavoos Kolahdouzan , Daniel G. Shore , Suzanne M. Szewczyk , James G. Taylor , Rhiannon Thomas-Tran , Nathan E. Wright , Zheng-Yu Yang
IPC: A61K31/4184 , A61K31/4192 , A61K31/4196 , A61K31/422 , A61K31/424 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K45/06 , C07D405/10 , C07D405/14 , C07D409/14 , C07D413/10 , C07D471/04 , C07D493/04 , C07D493/10 , C07D498/04
CPC classification number: A61K31/4184 , A61K31/4192 , A61K31/4196 , A61K31/422 , A61K31/424 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K45/06 , C07D405/10 , C07D405/14 , C07D409/14 , C07D413/10 , C07D471/04 , C07D493/04 , C07D493/10 , C07D498/04
Abstract: The present disclosure provides GLP-1R agonists, and compositions, methods, and kits thereof. Such compounds are generally useful for treating a GLP-1R mediated disease or condition.
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公开(公告)号:US20240342176A1
公开(公告)日:2024-10-17
申请号:US18292362
申请日:2022-07-27
Inventor: Yongguo Li , Wei Wei , Wei Ye
IPC: A61K31/519 , A61K31/4439 , A61K39/00 , A61P35/00
CPC classification number: A61K31/519 , A61K31/4439 , A61P35/00 , A61K2039/505
Abstract: A pharmaceutical combination and an application thereof. The pharmaceutical combination comprises a PI3K inhibitor and an immune checkpoint inhibitor, wherein the PI3K inhibitor is selected from a compound represented by formula (I), linperlisib, samotolisib, copanlisib, SHC014748M, pilaralisib, buparlisib, taselisib, YZJ-0673, gedatolisib, omipalisib, bimiralisib, voxtalisib, AL58805, and HEC68498, and pharmaceutically acceptable salts thereof, and the immune checkpoint inhibitor is a PD-1/PD-L1 inhibitor. The compound represented by formula (Ia) has a high inhibitory effect on PI3Kδ and PI3Kγ kinases, and the pharmaceutical combination uses a PI3K inhibitor and a PD-1 inhibitor in combination, thereby effectively improving the inhibitory effect on tumors, and solving the problem of drug resistance of PD-1/PD-L1 inhibitors.
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公开(公告)号:US12110263B2
公开(公告)日:2024-10-08
申请号:US17740260
申请日:2022-05-09
Applicant: CORTEXYME, INC.
Inventor: Andrei W. Konradi , Robert A. Galemmo, Jr. , Stephen S. Dominy , Casey C. Lynch , Leslie J. Holsinger
IPC: C07C233/62 , A61K31/165 , A61K31/167 , A61K31/41 , A61K31/42 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4439 , A61K31/505 , A61K31/513 , A61K31/655 , A61K45/06 , A61P25/00 , A61P31/04 , C07B59/00 , C07C233/78 , C07C235/10 , C07C235/50 , C07C237/42 , C07C245/08 , C07C247/16 , C07C247/18 , C07C317/28 , C07C323/40 , C07C323/42 , C07C381/00 , C07D213/65 , C07D213/68 , C07D213/70 , C07D213/81 , C07D213/82 , C07D239/34 , C07D239/36 , C07D239/38 , C07D257/04 , C07D261/12 , C07D401/12 , C07D413/12 , C07F5/02
CPC classification number: C07C233/62 , A61K31/165 , A61K31/167 , A61K31/41 , A61K31/42 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4439 , A61K31/505 , A61K31/513 , A61K31/655 , A61K45/06 , A61P25/00 , A61P31/04 , C07B59/001 , C07C233/78 , C07C235/10 , C07C235/50 , C07C237/42 , C07C245/08 , C07C247/16 , C07C247/18 , C07C317/28 , C07C323/40 , C07C323/42 , C07C381/00 , C07D213/65 , C07D213/68 , C07D213/70 , C07D213/81 , C07D213/82 , C07D239/34 , C07D239/36 , C07D239/38 , C07D257/04 , C07D261/12 , C07D401/12 , C07D413/12 , C07F5/02 , C07C2601/08
Abstract: The present invention provides compounds according to Formula I as described herein, and their use for inhibiting the lysine gingipain protease (Kgp) from the bacterium Porphyromonas gingivalis. Also described are gingipain activity probe compounds and methods for assaying gingipain activity are also described, as well as methods for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease.
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