Abstract: The present invention relates to a crystalline form of (S)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetr a-hydropyrazolo[1,5-a]pyrimi dine-3-carboxamide for inhibiting Btk, methods of preparation thereof and pharmaceutical compositions, and use of the crystalline form above in the treatment of a disease, or in the manufacturing of a medicament for the treatment of a disease.
Type:
Grant
Filed:
December 1, 2023
Date of Patent:
April 30, 2024
Assignee:
BeiGene Switzerland GmbH
Inventors:
Zhiwei Wang, Yunhang Guo, Gongyin Shi, Lai Wang
Abstract: Provided herein are novel bifunctional compounds formed by conjugating EGFR inhibitor moieties with E3 ligase Ligand moieties, which function to recruit targeted proteins to E3 ubiquitin ligase for degradation. The disclosure also provides pharmaceutically acceptable compositions comprising compounds and methods for the treatment of EGFR mutant-related cancers.
Type:
Application
Filed:
October 30, 2023
Publication date:
April 25, 2024
Applicant:
BeiGene Switzerland GmbH
Inventors:
Bailin Lei, Huaqing Liu, Songzhe Han, Zhiwei Wang
Abstract: The present disclosure provides methods of treating B-cell malignancy in a subject with a Bcl-2 inhibitor, in particularly 2-((1H-pyrrolo[2,3-b]pyridin-5-yl)oxy)-N-((4-((((1r,4r)-4-hydroxy-4-methylcyclohexyl)methyl)amino)-3-nitrophenyl)sulfonyl)-4-(2-((S)-2-(2-isopropylphenyl)pyrrolidin-1-yl)-7-azaspiro[3.5]nonan-7-yl)benzamide or a pharmaceutically acceptable salt thereof, or its combination with a Bruton's tyrosine kinase (BTK) inhibitor, particularly (S)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetrahydropyrazolo-[1,5-a]pyrimidine-3-carboxamide or a pharmaceutically acceptable salt thereof.
Type:
Application
Filed:
November 30, 2023
Publication date:
April 18, 2024
Applicant:
BeiGene Switzerland GmbH
Inventors:
James D. Hilger, Jane Huang, David Simpson
Abstract: The present invention relates to salts of a PI3Kdelta inhibitor (referred to as “Compound A” hereinafter), preferably fumarate, and the crystalline forms thereof. The present invention also relates to the process of preparation and uses of the salts and crystalline forms of Compound A.
Type:
Application
Filed:
November 22, 2023
Publication date:
March 28, 2024
Applicant:
BeiGene Switzerland GmbH
Inventors:
Jing LI, Xiaosong YU, Xiaopeng CAI, Zhiwei WANG
Abstract: Provided herein is a method of treating a patient having a B-cell proliferative disorder, the method comprising administering to the patient zanubrutinib, or a pharmaceutically acceptable salt thereof, wherein the patient is characterized by being administered with a moderate CYP3A inducer. In one embodiment, zanubrutinib is administered at a dose of about 320 mg twice a day, or at a total daily dose of about 640 mg.
Type:
Grant
Filed:
May 31, 2023
Date of Patent:
February 27, 2024
Assignee:
BeiGene Switzerland GmbH
Inventors:
Jason Paik, Tommi Salmi, Ying Ou, Motohisa Takai
Abstract: Provided herein is a method of treating a patient having a B-cell proliferative disorder, the method comprising administering to the patient zanubrutinib, or a pharmaceutically acceptable salt thereof, wherein the patient is characterized by being administered with a moderate CYP3A inducer. In one embodiment, zanubrutinib is administered at a dose of about 320 mg twice a day, or at a total daily dose of about 640 mg.
Type:
Grant
Filed:
June 6, 2023
Date of Patent:
February 13, 2024
Assignee:
BeiGene Switzerland GmbH
Inventors:
Jason Paik, Tommi Salmi, Ying Ou, Motohisa Takai
Abstract: The present invention relates to a crystalline form of (S)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide for inhibiting Btk, methods of preparation thereof and pharmaceutical compositions, and use of the crystalline form above in the treatment of a disease, or in the manufacturing of a medicament for the treatment of a disease.
Type:
Grant
Filed:
July 6, 2022
Date of Patent:
January 30, 2024
Assignee:
BEIGENE SWITZERLAND GMBH
Inventors:
Zhiwei Wang, Yunhang Guo, Gongyin Shi, Lai Wang
Abstract: The present invention relates to a crystalline form of (S)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide for inhibiting Btk, methods of preparation thereof and pharmaceutical compositions, and use of the crystalline form above in the treatment of a disease, or in the manufacturing of a medicament for the treatment of a disease.
Abstract: The present invention relates to a crystalline form of (S)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide for inhibiting Btk, methods of preparation thereof and pharmaceutical compositions, and use of the crystalline form above in the treatment of a disease, or in the manufacturing of a medicament for the treatment of a disease.
Abstract: Disclosed herein is a method for the prevention, delay of progression or treatment of indolent or aggressive B-cell lymphomas in an individual in need thereof, comprising administering a Btk inhibitor (in particularly (S)-7-(1-actyloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetrahydropyrazolo-[1,5-a]pyrimidine-3-carboxamide or a pharmaceutically acceptable salt thereof) in combination with an anti-PD-1 antibody. The potent and selective BTK inhibitor in combination with the anti-PD-1 antibody have a manageable toxicity profile in patients with indolent and aggressive lymphomas.
Type:
Grant
Filed:
November 29, 2018
Date of Patent:
October 17, 2023
Assignee:
BEIGENE SWITZERLAND GMBH
Inventors:
James Hilger, Xiaoping Zhang, Shibao Feng, Sunhee Ro, Jane Huang
Abstract: Provided herein is a method of treating a patient having a B-cell proliferative disorder, the method comprising administering to the patient zanubrutinib, or a pharmaceutically acceptable salt thereof, wherein the patient is characterized by being administered with a moderate CYP3A inducer. In one embodiment, zanubrutinib is administered at a dose of about 320 mg twice a day, or at a total daily dose of about 640 mg.
Abstract: Disclosed herein is a method for the prevention, delay of progression or treatment of cancer in a subject, comprising administering to the subject in need thereof a Btk inhibitor, particularly, (S)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide or a pharmaceutically acceptable salt thereof, in combination with an immune checkpoint inhibitor or a targeted therapy agent. Also, disclosed a pharmaceutical combination comprising a Btk inhibitor, particularly, (S)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide or a pharmaceutically acceptable salt thereof, in combination with an immune checkpoint inhibitor, or a targeted therapy agent and the use thereof.
Type:
Grant
Filed:
August 18, 2017
Date of Patent:
July 18, 2023
Assignee:
BEIGENE SWITZERLAND GMBH
Inventors:
Nan Hu, Lai Wang, Jing Song, Tong Zhang, Kang Li, Lusong Luo, Min Wei, Zhiwei Wang, Yunhang Guo
Abstract: Provided are antibodies that specifically bind to Programmed Death-1 (PD1, Pdcd-1, or CD279) and inhibit PD1-mediated cellular signaling and activities in immune cells, antibodies binding to a set of amino acid residues required for its ligand binding, and uses of these antibodies to treat or diagnose cancer, infectious diseases or other pathological disorders modulated by PD1-mediated functions.
Abstract: The present invention relates to a crystalline form of (S)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide for inhibiting Btk, methods of preparation thereof and pharmaceutical compositions, and use of the crystalline form above in the treatment of a disease, or in the manufacturing of a medicament for the treatment of a disease.
Type:
Grant
Filed:
May 10, 2022
Date of Patent:
February 28, 2023
Assignee:
BEIGENE SWITZERLAND GMBH
Inventors:
Zhiwei Wang, Yunhang Guo, Gongyin Shi, Lai Wang
Abstract: Disclosed herein is a pharmaceutical combination for use in the prevention, delay of progression or treatment of cancer, wherein the pharmaceutical combination exhibits a synergistic efficacy. The pharmaceutical combination comprises a humanized antagonist monoclonal antibody against PD- and a RAF inhibitor. Also disclosed herein is a combination for use in the prevention, delay of progression or treatment of cancer in a subject, comprising administering to the subject a therapeutically effective amount of a humanized antagonist monoclonal antibody against PD-1 and a therapeutically effective amount of a RAF inhibitor.
Type:
Grant
Filed:
November 16, 2020
Date of Patent:
December 27, 2022
Assignee:
BEIGENE SWITZERLAND GMBH
Inventors:
Jing Song, Lai Wang, Kang Li, Tong Zhang, Lusong Luo, Min Wei, Zhiyu Tang, Guoliang Zhang, Changyou Zhou
Abstract: Provided are antibodies that specifically bind to Programmed Death-1 (PD1, Pdcd-1, or CD279) and inhibit PD1-mediated cellular signaling and activities in immune cells, antibodies binding to a set of amino acid residues required for its ligand binding, and uses of these antibodies to treat or diagnose cancer, infectious diseases or other pathological disorders modulated by PD1-mediated functions.
Abstract: The invention is fused heterocyclic compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain fused heterocyclic compounds that can be useful for inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby.
Abstract: The present invention relates to a crystalline form of (S)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide for inhibiting Btk, methods of preparation thereof and pharmaceutical compositions, and use of the crystalline form above in the treatment of a disease, or in the manufacturing of a medicament for the treatment of a disease.
Abstract: The invention is fused heterocyclic compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain fused heterocyclic compounds that can be useful for inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby.
Abstract: Provided are antibodies that specifically bind to Programmed Death-1 (PD1, Pdcd-1, or CD279) and inhibit PD1-mediated cellular signaling and activities in immune cells, antibodies binding to a set of amino acid residues required for its ligand binding, and uses of these antibodies to treat or diagnose cancer, infectious diseases or other pathological disorders modulated by PD1-mediated functions.