公开(公告)号：US11993582B2

公开(公告)日：2024-05-28

申请号：US17264333

申请日：2019-07-29

Applicant: Novartis AG

Inventor： Andreas Kordikowski ,  Yanxiang Wu

IPC: C07D401/12 ,  A61K31/4439 ,  A61K45/06

CPC classification number: C07D401/12 ,  A61K31/4439 ,  A61K45/06 ,  C07B2200/13

Abstract: This application relates to various crystalline forms of (S)-3-amino-4-(5-(4-((5-chloro-3-fluoropyridin-2-yl)oxy)phenyl)-2H-tetrazol-2-yl)butanoic acid in its free form, as well as compositions, method of making and methods of using the same. In some embodiments the crystalline forms also contain water (“hydrates”). These materials are useful in the treatment of diseases and disorders which are typically ameliorated by the inhibition of LTA4H. Such diseases and disorders may include inflammatory and autoimmune disorders and pulmonary and respiratory tract inflammation.

公开(公告)号：US11992477B2

公开(公告)日：2024-05-28

申请号：US17058883

申请日：2019-05-28

Applicant: HUA Medicine (Shanghai) Ltd.

Inventor： Li Chen ,  Yongguo Li ,  Gaosen Wang ,  Huisheng Gao

IPC: A61K31/4155 ,  A61K9/16 ,  A61K9/20 ,  A61K9/28 ,  A61K31/155 ,  A61K31/40 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/4439 ,  A61K31/4985 ,  A61K31/522 ,  A61K31/7034 ,  A61K45/06 ,  A61K47/38 ,  A61P3/10 ,  C07D231/38 ,  C07D403/12

CPC classification number: A61K31/4155 ,  A61K9/1611 ,  A61K9/1617 ,  A61K9/1635 ,  A61K9/1694 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2027 ,  A61K9/2054 ,  A61K9/2086 ,  A61K9/2095 ,  A61K9/2813 ,  A61K9/284 ,  A61K9/2866 ,  A61K31/155 ,  A61K31/40 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/4439 ,  A61K31/4985 ,  A61K31/522 ,  A61K31/7034 ,  A61K45/06 ,  A61K47/38 ,  A61P3/10 ,  C07D231/38 ,  C07D403/12

Abstract: The present invention relates to a pharmaceutical combination, comprising a glucokinase activator or a pharmaceutically acceptable salt, isotopic label, crystal form, hydrate, solvate, diastereomer, or enantiomer thereof and an SGLT-2 inhibitor. The present invention further relates to a pharmaceutical composition, a fixed-dose combination preparation, and preparation methods and uses thereof.

公开(公告)号：US11986467B2

公开(公告)日：2024-05-21

申请号：US17861946

申请日：2022-07-11

Applicant: The University of Toledo

Inventor： Amit K. Tiwari ,  Chandrabose Karthikeyan ,  Haneen A. Amawi ,  Paul W. Erhardt ,  Piyush Trivedi

IPC: A61K31/4439 ,  A61K31/122 ,  C07D401/14 ,  C07D513/04

CPC classification number: A61K31/4439 ,  A61K31/122 ,  C07D401/14 ,  C07D513/04

Abstract: Compounds, compositions, and methods useful for inducing cancer cell death via methuosis, autophagy, or a combination thereof, are described. The compounds have a 4-pyridyl group linked by a heterocyclic group to an aryl, heteroaryl, aralkyl, or heteroaryl alkyl.

公开(公告)号：US20240148745A1

公开(公告)日：2024-05-09

申请号：US18549457

申请日：2022-03-09

Applicant: FONDAZIONE CENTRO SAN RAFFAELE ,  INSTITUT DU CERVEAU ET DE LA MOELLE ÉPINIÈRE ,  ASSISTANCE PUBLIQUE HOPITAUX DE PARIS ,  CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE ,  INSTITUT NATIONAL DE LA SANTÉ ET DE LA RECHERCHE MÉDICALE ,  SORBONNE UNIVERSITE ,  WESTFÄLISCHE WILHELMS-UNIVERSITÄT MÜNSTER ,  THE REGENTS OF THE UNIVERSITY OF CALIFORNIA ,  HEINRICH HEINE UNIVERSITY DÜSSELDORF ,  UNIVERSITÄTSMEDIZIN DER JOHANNES GUTENBERG-UNIVERSITÄT MAINZ ,  THE ROYAL INSTITUTION FOR THE ADVANCEMENT OF LEARNING / MCGILL UNIVERSITY ,  ISTITUTO SUPERIORE DI SANITÀ ,  CONSIGLIO NAZIONALE DELLE RICERCHE ,  IRBM S.P.A.

Inventor： Gianvito MARTINO ,  Paola PANINA ,  Brahim NAIT-OUMESMAR ,  Anne BARON-VAN EVERCOOREN ,  Tanja KUHLMANN ,  Sergio BARANZINI ,  Norbert GOEBELS ,  Frauke ZIPP ,  Nicholas HANUSCHECK ,  Jack ANTEL ,  Cristina AGRESTI ,  Maria Pia ABBRACCHIO ,  Ivano EBERINI ,  Chiara PARRAVICINI ,  Stefania OLLA ,  Alberto BRESCIANI

IPC: A61K31/5377 ,  A61K31/405 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/4995 ,  A61K31/5025 ,  A61K31/55 ,  A61P25/28 ,  G01N33/50

CPC classification number: A61K31/5377 ,  A61K31/405 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/4995 ,  A61K31/5025 ,  A61K31/55 ,  A61P25/28 ,  G01N33/5058

Abstract: The present invention provides compounds able to induce neuroprotection of damaged neurons and boost the remyelination potential of oligodendrocytes. The compounds have been identified through methods of pharmacological screening of a small molecule library consisting of known pharmacologically active compounds and approved drugs. The screening method is also included in the invention.

公开(公告)号：US20240148699A1

公开(公告)日：2024-05-09

申请号：US18405633

申请日：2024-01-05

Applicant: Otsuka Pharmaceutical Co., Ltd.

Inventor： Minoru Okada ,  Masaya Kato ,  Norifumi Sato ,  Tetsuyuki Uno ,  Hideki Kitagaki ,  Junpei Haruta ,  Hidetaka Hiyama ,  Tomonori Shibata

IPC: A61K31/421 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/497 ,  A61K31/5377 ,  C07D263/32 ,  C07D263/34 ,  C07D413/06 ,  C07D413/12 ,  C12N9/16

CPC classification number: A61K31/421 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/497 ,  A61K31/5377 ,  C07D263/32 ,  C07D263/34 ,  C07D413/06 ,  C07D413/12 ,  C12N9/16 ,  C12Y301/04012

Abstract: The present invention provides a oxazole compound represented by Formula (1), or a salt thereof:




wherein R1 is an aryl group which may have one or more substituents; R2 is an aryl group or a nitrogen atom-containing heterocyclic group each of which may have one or more substituents; and W is a divalent group represented by —Y1-A1- or —Y2—C(═O)— wherein Y1 is a group such as —C(═O)—, A1 is a group such as a lower alkylene group, and Y2 is a group such as a piperazinediyl group. The oxazole compound has a specific inhibitory action against phosphodiesterase 4.

公开(公告)号：US11976069B2

公开(公告)日：2024-05-07

申请号：US17438479

申请日：2020-03-16

Applicant: Merck Sharp & Dohme LLC

Inventor： Wensheng Yu ,  Joseph A. Kozlowski ,  Dane James Clausen ,  Jian Liu ,  James Fells

IPC: C07D471/22 ,  A61K31/426 ,  A61K31/438 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/4748 ,  A61K31/505 ,  A61K31/506 ,  A61K31/513 ,  A61K31/52 ,  A61K31/635 ,  A61K31/685 ,  A61P31/18 ,  C07D487/08 ,  C07D491/18 ,  C07D498/22

CPC classification number: C07D471/22 ,  A61K31/426 ,  A61K31/438 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/4748 ,  A61K31/505 ,  A61K31/506 ,  A61K31/513 ,  A61K31/52 ,  A61K31/635 ,  A61K31/685 ,  A61P31/18 ,  C07D487/08 ,  C07D491/18 ,  C07D498/22

Abstract: The present invention relates to Compounds of Formula I and Ia and pharmaceutically acceptable salts or prodrug thereof, wherein R1, R2, X, A and B are as defined herein. The present invention also relates to compositions comprising at least one compound of Formula I or Ia, and methods of using the compounds of Formula I or Ia for treating or preventing HIV infection in a subject.

公开(公告)号：US11976055B1

公开(公告)日：2024-05-07

申请号：US18237608

申请日：2023-08-24

Applicant: KING FAISAL UNIVERSITY

Inventor： Hany Mohamed Abd El-Lateef Ahmed ,  Mai Mostafa Khalaf Ali ,  Antar Ahmed Abdelhamid Ahmed ,  Adel A. Marzouk ,  Fawy M. Abd El Latif

IPC: A61K31/4178 ,  A61K31/4439 ,  A61P35/00 ,  C07D401/04

CPC classification number: C07D401/04 ,  A61K31/4178 ,  A61K31/4439 ,  A61P35/00 ,  C07B2200/13

Abstract: A compound 2-(1-(3-(dimethylamino)propyl)-4,5-diphenyl-1H-imidazol-2-yl)pyridin-3-ol compound, its synthesis, and its use as an anticancer, anti-inflammatory, and/or antimicrobial agent.

公开(公告)号：US11974997B2

公开(公告)日：2024-05-07

申请号：US17494458

申请日：2021-10-05

Applicant: Genfit

Inventor： Jean-Francois Delhomel ,  Enrico Perspicace ,  Zouher Majd ,  Peggy Parroche ,  Robert Walczak ,  Pascal Bonnet ,  Jade Fogha

IPC: C07D405/14 ,  A61K31/192 ,  A61K31/40 ,  A61K31/4184 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/506

CPC classification number: A61K31/496 ,  A61K31/192 ,  A61K31/40 ,  A61K31/4184 ,  A61K31/4439 ,  A61K31/506 ,  C07D405/14

Abstract: The present invention provides novel compounds that are modulators of RORgamma. These compounds, and pharmaceutical compositions comprising the same, are suitable means for treating any disease wherein the modulation of RORgamma has therapeutic effects, for instance in autoimmune diseases, autoimmune-related diseases, inflammatory diseases, metabolic diseases, fibrotic diseases, or cholestatic diseases.

公开(公告)号：US11957687B2

公开(公告)日：2024-04-16

申请号：US17622454

申请日：2020-07-01

Applicant: REGENERON PHARMACEUTICALS, INC.

Inventor： Joseph Vacca

IPC: A61K31/5377 ,  A61K31/4412 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/513 ,  A61P1/16 ,  C07D213/82 ,  C07D239/36 ,  C07D239/56 ,  C07D295/135 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D498/04 ,  C07D513/04

CPC classification number: A61K31/5377 ,  A61K31/4412 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/513 ,  A61P1/16 ,  C07D213/82 ,  C07D239/36 ,  C07D239/56 ,  C07D295/135 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D498/04 ,  C07D513/04

Abstract: The disclosure relates to compounds and pharmaceutical compositions capable of modulating the hydroxysteroid 17-beta dehydrogenase (HSD17B) family member proteins including inhibiting the HSD17B member proteins, e.g. HSD17B13. The disclosure further relates to methods of treating liver diseases, disorders, or conditions with the compounds and pharmaceutical compositions disclosed herein, in which the HSD17B family member protein plays a role.

公开(公告)号：US11957678B2

公开(公告)日：2024-04-16

申请号：US17479029

申请日：2021-09-20

Applicant: MOONSHOT PHARMA LLC

Inventor： Angela Christiano

IPC: A61K31/498 ,  A61K31/15 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/496 ,  A61K39/395 ,  A61K45/06 ,  A61P35/00 ,  C07K16/28 ,  A61K39/00

CPC classification number: A61K31/498 ,  A61K31/15 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/496 ,  A61K39/3955 ,  A61K45/06 ,  A61P35/00 ,  C07K16/2818 ,  A61K2039/505 ,  A61K2039/507 ,  A61K2039/53 ,  A61K31/4245 ,  A61K2300/00 ,  A61K31/498 ,  A61K2300/00 ,  A61K39/3955 ,  A61K2300/00

Abstract: Provided herein, inter alia, are compositions and methods for generating a immune response in an individual and/or inducing the expression of neoantigens on the surface of abnormal (such as proliferative) cells via promotion of premature termination codon (PTC) read-through and inhibition of nonsense-mediated decay (NMD) of messenger RNAs (mRNAs) bearing PTCs.