Abstract: Described herein are crystalline forms of a compound of formula (II?), including toluene solvates off A TD-CLE, as well as processes for the preparation thereof and use thereof in the preparation of cephalosporin compounds such as ceftolozane. Provided herein is a crystalline form of a compound of formula (II?): wherein X is CI, Br, or I; and R1 and R2 are each independently an oxygen protecting group; processes for making the crystalline form, and use of said form in the synthesis of antibacterial cephalosporins such as ceftolozane.
Type:
Grant
Filed:
August 14, 2015
Date of Patent:
March 5, 2019
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Kristos Adrian Moshos, Valdas Jurkauskas, Giovanni Fogliato, Manuel Scanu, You Seok Hwang
Abstract: Thermally activated delayed fluorescent compounds and uses thereof are described. The thermally activated delayed fluorescent compounds are an analogs of 9,10-dihydro-9,9-dimethylacridine compounds.
Type:
Grant
Filed:
August 25, 2016
Date of Patent:
February 19, 2019
Assignee:
Arizona Board of Regents on behalf of Arizona State University
Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R3 are as defined herein, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
Type:
Grant
Filed:
June 14, 2018
Date of Patent:
February 12, 2019
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Roland Maier
Abstract: Disclosed are compounds of Formula (I) or salts thereof, wherein: HET is a heteroaryl selected from imidazo[1,2-b]pyridazinyl and pyrazolo[1,5-a]pyrimidinyl, wherein said heteroaryl is attached to the pyridinyl group in the compound of Formula (I) by a carbon ring atom in the heteroaryl and wherein said heteroaryl is substituted with zero to 2 Rb; A is pyrazolyl, imidazolyl, or triazolyl, each substituted with zero or 1 Ra; and R3, Ra, and Rb are define herein. Also disclosed are methods of using such compounds as modulators of IRAK4, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing inflammatory and autoimmune diseases, or in the treatment of cancer.
Type:
Grant
Filed:
June 23, 2016
Date of Patent:
February 12, 2019
Assignee:
Bristol-Myers Squibb Company
Inventors:
John V. Duncia, Daniel S. Gardner, John Hynes, John E. Macor, Satheesh Kesavan Nair, Venkatram Reddy Paidi, Joseph B. Santella, Kandhasamy Sarkunam, Ramesh Kumar Sistla, Subba Rao Polimera, Hong Wu
Abstract: The disclosure features amino lipids and compositions involving the same. Nanoparticle compositions include an amino lipid as well as additional lipids such as phospholipids, structural lipids, PEG lipids, or a combination thereof. Nanoparticle compositions further including therapeutic and/or prophylactic agents such as RNA are useful in the delivery of therapeutic and/or prophylactic agents to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression.
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:
November 18, 2016
Date of Patent:
January 29, 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: 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:
May 5, 2017
Date of Patent:
January 29, 2019
Assignee:
Novartis AG
Inventors:
Ha-Soon Choi, James Paul Lajiness, Srinivasa Reddy Natala, Bao Nguyen, Hank Michael James Petrassi, Zhicheng Wang
Abstract: The present invention relates to a liquid pharmaceutical composition suitable for parenteral administration comprising: a) pemetrexed diacid; b) at least one organic amine; c) at least one antioxidant; d) 10-200 mg/ml of propylene glycol; and e) one or more parenteral solvents, wherein the preparation thereof is conducted in an atmosphere of inert gas and wherein the organic amine(s) is present in an amount sufficient to reach a pH of the composition in the range from 8.3 to 9.1 The invention further relates to the use of said liquid pharmaceutical composition as medicament in the treatment of malignant pleural mesothelioma and non-small cell lung cancer.
Abstract: Cofactor analogs for methyltransferases are disclosed. The compounds are represented by formula (I) wherein R1 is COOH or COO—; X is an organic or inorganic anion carrying one or more negative charges; Y and Y? are H, or an alkyl; R2 is NH2, NHBoc, or H; and Z is S or Se. R comprises a carbon-carbon double bond, carbon-oxygen double bond, carbon-sulfur double bond, carbon-nitrogen double bond, a carbon-carbon triple bond, carbon-nitrogen triple bond, an aromatic carbocyclic or heterocyclic system in ?-position to the sulfonium center, unsaturated c-c bond, or c-heteroatom bond where the heteroatom is O, N, S.
Type:
Grant
Filed:
August 31, 2015
Date of Patent:
January 22, 2019
Assignee:
KATHOLIEKE UNIVERSITEIT LEUVEN
Inventors:
Robert Neely, Volker Leen, Johan Hofkens
Abstract: Provided is a bipyridine compound that exhibits an excellent controlling effect against noxious arthropods. In particular, provided is a bipyridine compound of formula (I) or an N-oxide thereof in which the variable groups are as defined in the specification. Also provided are compositions containing the biypridine compound or an N-oxide thereof, and methods of using such compounds and compositions to control noxious arthropods.
Abstract: Embodiments of calcium channel agonists, as well as methods of making and using the calcium channel agonists, are disclosed. The disclosed calcium channel agonists and corresponding salt forms have a structure according to general formula I: wherein each bond depicted as “” is a single bond or a double bond as needed to satisfy valence requirements; Z1, Z2, Z3, Z4, and Z5 independently are nitrogen or carbon; R1 and R3 are alkyl; R2 is alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; and R4 is alkyl or hydroxyalkyl.
Type:
Grant
Filed:
September 21, 2017
Date of Patent:
January 8, 2019
Assignee:
University of Pittsburgh—Of the Commonwealth System of Higher Education
Inventors:
Peter Wipf, Stephen D. Meriney, Mary Liang
Abstract: The present invention relates to co-crystals, salts and crystalline forms of tenofovir alafenamide and methods for preparation, use and isolation of such compounds.
Abstract: The present invention relates to a synthesis method of preventing the formation of impurities and byproducts in the synthesis of tenofovir disoproxil fumarate (Teno-DF) used as a medicine for hepatitis B and HIV treatment due to its function to promote bioactivities. In the synthesis method of the present invention, an ion-exchange resin (Dowex 50W hydrogen form, sulfonic acidic cation exchange resin) is used to enhance the yield and purity of the compound. The present invention also relates to a method of preparing an oral dissolving film dosage form in the manufacture of a medicine using the tenofovir compound with high purity obtained by the synthesis method of the present invention as an effective ingredient.
Type:
Grant
Filed:
May 19, 2015
Date of Patent:
December 18, 2018
Assignee:
FIRSON
Inventors:
Dong-Jin Kim, Chang-Hui Koo, Il-Hee Cho, Sung-Bae Lee, Dong-Hoon Han
Abstract: Provided are novel compounds of Formula (I): pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are liver X receptor modulators, and which are useful in the treatment of diseases and disorders associated with the liver X receptor. Also provided are the compounds of Formula (I) and pharmaceutical compositions thereof for treating atherosclerosis, cardiovascular disease, Alzheimer's disease, dermatitis, dyslipidemia, cancer and other diseases or disorders.
Type:
Grant
Filed:
August 4, 2015
Date of Patent:
December 4, 2018
Assignee:
Vitae Pharmaceuticals, Inc.
Inventors:
David A. Claremon, Chengguo Dong, Yi Fan, Katerina Leftheris, Stephen D. Lotesta, Suresh B. Singh, Colin M. Tice, Wei Zhao, Yajun Zheng, Linghang Zhuang
Abstract: To provide a medicament which shows more remarkable effect in treatment of activated B-cell like diffuse large B-cell lymphoma (ABC-CLBCL) 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 application relates to securinine or norsecurinine analogs that, when administered to immature myeloid cells, promote differentiation of these cells to mature cells that do not readily proliferate. Therefore, the agents are useful in the treatment of myeloid disorders including myeloproliferative disorders, acute myeloid leukemia, and autoimmune diseases. The agents may also be used as a myeloablative agent in conjunction with a bone marrow transplant or stem cell therapy.
Abstract: The present invention is directed to a method of isolating fractions of anthocyanin molecules from anthocyanin-containing vegetable and fruit juices and extracts, or combinations thereof, at a select pH based on differences in polarity of the anthocyanin molecules in the anthocyanin-containing vegetable and fruit juices and extracts.
Type:
Grant
Filed:
February 7, 2017
Date of Patent:
November 6, 2018
Assignees:
Mars, Incorporated, The Ohio State University
Inventors:
Rebecca J. Robbins, J. Christopher Johnson, Thomas M. Collins, Neda Ahmadiani, M. Monica Giusti