Abstract: The present invention is directed to bicyclic heteroaryl benzamide compounds of formulas (I): which are tropomyos-in-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
Type:
Grant
Filed:
April 4, 2016
Date of Patent:
February 11, 2020
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Craig A. Stump, Yi Heng Chen, Ping Liu, Dongfang Meng, Jane Yang Wu, Chun Sing Li, Zhiqi Qi
Abstract: Disclosed are cyclic-di-nucleotide cGAMP analogs, methods of synthesizing the compounds, pharmaceutical compositions comprising the compounds thereof, and use of compounds and compositions in medical therapy.
Type:
Grant
Filed:
April 15, 2018
Date of Patent:
December 31, 2019
Assignees:
ImmuneSensor Therapeutics, Inc., The Board of Regents of the University of Texas System
Inventors:
Boyu Zhong, Lijun Sun, Heping Shi, Qi Wei, Yuanwei Dai, Chuo Chen, Zhijian Chen
Abstract: Disclosed herein are new compounds and compositions and their application as pharmaceuticals for the treatment of diseases. Methods of inhibition of KDM1A, methods of increasing gamma globin gene expression, and methods to induce differentiation of cancer cells in a human or animal subject are also provided for the treatment of diseases such as acute myelogenous leukemia.
Type:
Grant
Filed:
April 12, 2018
Date of Patent:
December 31, 2019
Assignee:
Imago Biosciences, Inc.
Inventors:
Hugh Y. Rienhoff, Jr., John M. McCall, Michael Clare, Cassandra Celatka, Amy E. Tapper
Abstract: The present invention relates to pharmaceutical compounds of the Formula (I), or a pharmaceutically acceptable salt or composition thereof, and methods of their use for the treatment of pain, respiratory conditions, as well as inhibiting the Transient Receptor Potential A1 ion channel (TRPA1).
Abstract: Provided is a tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO) inhibitor compound for use in medicine, which compound comprises the general formula (I) detailed within.
Abstract: Polymorphs of a hydrochloride salt of (S)-2-(1-(9H-purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one, compositions thereof, methods for their preparation, and methods for their use are disclosed. Solvent forms of a hydrochloride salt of (S)-2-(1-(9H-purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one, compositions thereof, methods for their preparation, and methods for their use are also disclosed.
Type:
Grant
Filed:
June 16, 2017
Date of Patent:
October 15, 2019
Assignee:
Gilead Calistoga LLC
Inventors:
Suzanne Buttar, Ernest Carra, Tracy Ehiwe, Duong Tran, Fang Wang, Christopher Worrall, Jerry Evarts
Abstract: To provide a medicament which shows more remarkable effect in treatment of activated B-cell like diffuse large B-cell lymphoma ABC-DLBCL than the existing Btk inhibitor, and is excellent in safety. The present compound exhibits more remarkable effect in treatment of activated B-cell like diffuse large B-cell lymphoma (ABC-DLBCL) patients, inter alia, ABC-DLBCL patients having CD79B wild-type gene background than the existing Btk inhibitor, and therefore, it can attain the object of the present invention.
Abstract: The present invention relates to compounds of the Formula (I), or a pharmaceutically acceptable salt, pharmaceutical preparation, or pharmaceutical composition thereof, and their use for the treatment of pain, inflammatory disease, neuropathy, dermatological disorders, pulmonary conditions, and cough, as well as inhibiting the Transient Receptor Potential A1 ion channel (TRPA1).
Type:
Grant
Filed:
March 29, 2018
Date of Patent:
October 1, 2019
Assignee:
Eli Lilly and Company
Inventors:
Blaise S. Lippa, Xinyuan Wu, Qingyi Li, Iwona Wrona, Andrew J. Jackson, Bertrand L. Chenard, Christopher M. Liu, Guohua Liang, Matthew F. Baevsky, Richard A. Earl, Lisa Mcqueen, Jared Smit, Brett A. Cowans
Abstract: This disclosure provides pharmaceutical compositions comprising ceftolozane, pharmaceutical compositions comprising ceftolozane and tazobactam, methods of preparing those compositions, and related methods and uses of these compositions.
Type:
Grant
Filed:
December 18, 2017
Date of Patent:
September 24, 2019
Assignee:
Merck, Sharp & Dohme Corp.
Inventors:
Joseph Terracciano, Nicole Miller Damour, Chun Jiang, Giovanni Fogliato, Giuseppe Alessandron Donadelli, Dario Resemini
Abstract: Deuterated quinazolinone compounds and pharmaceutical compositions containing such compounds are provided. In particular, deuterated quinazolinone compounds of formula (I) are provided, as well as pharmaceutical compositions containing such compounds or crystal form, pharmaceutically acceptable salts, hydrates or solvates thereof. The deuterated quinazolinone compounds of formula (I) can be used for treating and/or preventing PI3K kinase-associated diseases, such as cancer, cell proliferative diseases and the like.
Abstract: A medicament for prophylactic and/or therapeutic treatment of dementia, which comprises a compound represented by the formula (I) having a xanthine oxidase inhibitory action as an active ingredient.
Type:
Grant
Filed:
February 23, 2016
Date of Patent:
September 17, 2019
Assignees:
NATIONAL UNIVERSITY CORPORATION TOTTORI UNIVERSITY, NIPPON MEDICAL SCHOOL FOUNDATION, NIPPON CHEMIPHAR CO., LTD.
Abstract: The specification generally relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof, where R1 and R2 have any of the meanings defined herein. The specification also relates to the use of such compounds and salts thereof to treat or prevent DNA-PK mediated disease, including cancer. The specification further relates to pharmaceutical compositions comprising such compounds and salts; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; intermediates useful in the manufacture of such compounds and salts; and to methods of treating DNA-PK mediated disease, including cancer, using such compounds and salts.
Type:
Grant
Filed:
December 19, 2017
Date of Patent:
September 10, 2019
Assignees:
AstraZeneca AB, Cancer Research Technology Limited
Inventors:
Maurice Raymond Verschoyle Finlay, Frederick Woolf Goldberg, Attilla Kuan Tsuei Ting
Abstract: The application relates to inhibitors of USP1 useful in the treatment of cancers, and other USP1 associated diseases and disorders, having the Formula: where R1, R2, R3, R3?, R4, R5, X1, X2, X3, X4, and n are described herein.
Type:
Grant
Filed:
August 1, 2018
Date of Patent:
September 3, 2019
Assignee:
FORMA Therapeutics, Inc.
Inventors:
Alexandre Joseph Buckmelter, Stephanos Ioannidis, Bruce Follows, Gary Gustafson, Minghua Wang, Justin A. Caravella, Zhongguo Wang, Edward L. Fritzen, Jian Lin
Abstract: Pharmaceutical compounds, compositions, and methods are presented in which various heterocyclic thiosemicarbazone derivatives are prepared. Contemplated compounds will be suitable to inhibit or reduce cellular growth or proliferation and are thus beneficial in the manufacture of drugs to treat neoplastic diseases.
Type:
Grant
Filed:
August 8, 2016
Date of Patent:
August 27, 2019
Assignees:
NantBio, Inc., Nant Holdings IP, LLC
Inventors:
Chunlin Tao, Qinwei Wang, Patrick Soon-Shiong
Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds, and methods of using such compounds for treatment of joint damage or joint injury in a mammal, and for inducing differentiation of mesenchymal stem cells into chondrocytes.
Type:
Grant
Filed:
November 28, 2018
Date of Patent:
August 20, 2019
Assignee:
Novartis AG
Inventors:
Ha-Soon Choi, James Paul Lajiness, Srinivasa Reddy Natala, Bao Nguyen, Hank Michael James Petrassi, Zhicheng Wang
Abstract: An organic electroluminescent element having high durability can be provided by using a compound represented by the following general formula (1), wherein: Z1 to Z4 each represent a carbon atom or a nitrogen atom; A1 represents an atomic group which is combined with Z1 and a nitrogen atom to form a 5- or 6-membered hetero ring; B1 represents an atomic group which is combined with Z2 and a carbon atom to form a 5- or 6-membered ring; C1 represents an atomic group which is combined with Z3 and a nitrogen atom to form a 5- or 6-membered hetero ring; D1 represents an atomic group which is combined with Z4 and a carbon atom to form a 5- or 6-membered ring; n represents 1 or 2; L represents a single bond or a linking group; and G represents a fused ring with 3 or more rings.
Abstract: The present invention relates to an amorphous form of Idelalisib and its methods of preparation. Using a Cu-K? radiation, the X-ray powder diffraction (XRPD) pattern does not contain sharp diffraction peaks at a diffraction angle expressed in degrees 2?, and the X-ray powder diffraction pattern is shown in FIG. 1. The present invention also provides a preparation method for the amorphous form of Idelalisib. The amorphous form of Idelalisib of the present invention increases the solubility of Idelalisib and improves bioavailability of the drug product. As compared to the existing crystalline forms of Idelalisib, its solubility increases significantly, which improves body's absorption of the drug and makes it more efficacious in the clinical therapeutic treatment of diseases. Under the stress test conditions, the amorphous material can maintain good physical and chemical stabilities. The preparation method of amorphous Idelalisib according to the present invention is simple to operate and easy to implement.