Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective Factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
Type:
Grant
Filed:
December 22, 2014
Date of Patent:
October 31, 2017
Assignee:
Bristol-Myers Squibb Company
Inventors:
James R. Corte, Tianan Fang, Carl P. Decicco, Donald J. P. Pinto, Karen A. Rossi, Zilun Hu, Yoon Jeon, Mimi L. Quan, Joanne M. Smallheer, Yufeng Wang, Wu Yang
Abstract: Use of particles in controlling a population of arthropod pests, wherein the particles comprise i) a hydrophobic exterior that adheres to the cuticle of at least one species of an arthropod pest; and ii) at least one pesticide associated with the said particles, wherein the pesticide is present at a weight of no more than 2% of the weight of the particles, populations of particles, methods of producing populations of particles and methods of application of such populations.
Abstract: A method of making a mono-ether of an isohexide and art assemblage of novel. Song-chain isohexide mono-ethers are described. In particular, the method involves reacting an isohexide stereoisomer with a Bronsted base and an alkyl species. The resultant mono-ethers can serve as attractive antecedents or chemical scaffolds for making a derivative compound, such as various amphiphiles with potential uses as surfactants, dispersants, and lubricants, among others.
Abstract: The present invention is directed to a method for continuous production of dihydroartemisinin and also artemisinin derivatives derived from dihydroartemisinin by using artemisinin or dihydroartemisinic acid (DHAA) as starting material as well as to a continuous flow reactor for producing dihydroartemisinin as well as the artemisinin derivatives. It was found that the reduction of artemisinin to dihydroartemisinin in a continuous process requires a special kind of reactor and a special combination of reagents comprising a hydride reducing agent, at least one activator such as an inorganic activator, at least one solid base, at least one aprotic solvent and at least one C1-C5 alcohol.
Type:
Grant
Filed:
July 14, 2014
Date of Patent:
October 31, 2017
Assignee:
Max-Plank-Gesellschaft zur Förderung der Wissenschaften e.V.
Inventors:
Daniel Kopetzki, David Tyler McQuade, Peter H. Seeberger, Kerry Gilmore
Abstract: Disclosed are compounds of Formula 1, or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, and R4 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating Type I hypersensitivity reactions, autoimmune diseases, inflammatory disorders, cancer, non-malignant proliferative disorders, and other conditions associated with BTK.
Type:
Grant
Filed:
June 29, 2016
Date of Patent:
October 31, 2017
Assignee:
Takeda Pharmaceutical Company Limited
Inventors:
John David Lawson, Mark Sabat, Nicholas Scorah, Christopher Smith, Phong H. Vu, Haixia Wang
Abstract: The present invention relates to a novel ligand compound, a preparation method thereof, a transition metal compound including the ligand compound, and a preparation method thereof. The ligand compound of novel structure according to the present invention and the transition metal compound including the same may be used as a polymerization reaction catalyst for preparing olefin polymers.
Type:
Grant
Filed:
November 19, 2013
Date of Patent:
October 17, 2017
Assignee:
LG Chem, Ltd.
Inventors:
Jae Kwon Jang, Hyo Jung Han, Ki Won Han, Seul Ki Kim, Eun Jung Lee, Choong Hoon Lee, In Sung Park
Abstract: The present invention relates to dual delta (?) and gamma (?) PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of Pi3K kinase mediated diseases or disorders with them.
Type:
Grant
Filed:
June 4, 2014
Date of Patent:
October 17, 2017
Assignee:
RHIZEN PHARMACEUTICALS SA
Inventors:
Swaroop K. V. S. Vakkalanka, Prashant K. Bhavar, Srikant Viswanadha, Govindarajulu Babu
Abstract: Described herein are methods for synthesizing heterocyclic, 8-membered ring structures. The methods may allow for preparation of highly substituted 8-membered rings. Also disclosed are heterocyclic, 8-membered ring compounds and pharmaceutical compositions comprising the compounds.
Abstract: The invention relates to chiral imidodiphosphates and derivatives thereof having the general formula I, The compounds are suitable as chiral Brønsted acid catalysts, phase-transfer catalysts, chiral anions for organic salts, metal salts or metal complexes for catalysis.
Type:
Grant
Filed:
January 8, 2013
Date of Patent:
October 10, 2017
Assignee:
STUDIENGESELLSCHAFT KOHLE MBH
Inventors:
Benjamin List, Ilija Coric, Sreekumar Vellalath
Abstract: A synergistic microbicidal composition comprising a non-ionic surfactant and glutaraldehyde and a method for inhibiting the growth of microorganisms in an aqueous medium.
Abstract: The invention provides methods for the synthesis of eribulin or a pharmaceutically acceptable salt thereof (e.g., eribulin mesylate) through a macrocyclization strategy. The macrocyclization strategy of the present invention involves subjecting a non-macrocyclic intermediate to a carbon-carbon bond-forming reaction (e.g., an olefination reaction (e.g., Homer-Wadsworth-Emmons olefination), Dieckmann reaction, catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic intermediate. The invention also provides compounds useful as intermediates in the synthesis of eribulin or a pharmaceutically acceptable salt thereof and methods for preparing the same.
Type:
Grant
Filed:
November 4, 2014
Date of Patent:
October 10, 2017
Assignee:
EISAI R&D MANAGEMENT CO., LTD.
Inventors:
Francis G. Fang, Dae-Shik Kim, Hyeong-Wook Choi, Charles E. Chase, Jaemoon Lee
Abstract: A synergistic microbicidal composition comprising a non-ionic surfactant and glutaraldehyde and a method for inhibiting the growth of microorganisms in an aqueous medium.
Abstract: A compound for an organic photoelectric device is represented by Chemical Formula 1, and an organic photoelectric device, an image sensor, and an electronic device include the same.
Type:
Grant
Filed:
November 16, 2015
Date of Patent:
October 10, 2017
Assignee:
Samsung Electronics Co., Ltd.
Inventors:
Seon-Jeong Lim, Sung Young Yun, Takkyun Ro, Yong Wan Jin
Abstract: The present invention discloses oxindole compounds and a single step, one pot reaction for the synthesis of oxindole derivates via a solvent free Passerini reaction of isocyanides, isatins and carboxylic acids.
Type:
Grant
Filed:
April 2, 2014
Date of Patent:
October 10, 2017
Assignee:
Council of Scientific & Industrial Research
Inventors:
Akkattu Thankappan Biju, Trinadh Kaicharla, Santhivardhana Reddy Yetra, Tony Roy
Abstract: The invention relates to a series of quinoline derivatives of general formula I, pharmaceutically acceptable salts, hydrates, solvates or prodrugs. Thereof M, R1, R2, X, Y and n are defined as claims. And the compounds of general formula I show potent inhibitory activity against c-Met kinase. The present invention further relates to the uses of the compounds, pharmaceutically acceptable salts and hydrates for the preparation of medicaments for the treatment and/or prevention of diseases caused by abnormal expression of c-Met kinase, especially for treatment and/or prevention of cancer.
Abstract: The present invention relates to a thiophene derivative of the following general formula I or an enantiomer, diastereoisomer, hydrate, solvate, tautomer, racemic mixture or pharmaceutically acceptable salt thereof or to its use as a drug in particular intended for treating and/or preventing diabetes, its complications and/or associated pathologies, advantageously diabetes of type II and hyperglycemia.
Type:
Grant
Filed:
July 16, 2013
Date of Patent:
October 3, 2017
Assignee:
METABRAIN RESEARCH
Inventors:
Franck F. Lepifre, Gersande R. Lena, Valerie Autier, Micheline R. Kergoat, Lauren R. Faveriel, Christine G. Charon, Sophie N. Raynal, Annick M. Audet
Abstract: Disclosed are processes for preparing [(3-hydroxypyridine-2-carbonyl)amino]-alkanoic acids, derivatives, inter alia, 5-aryl substituted and 5-heteroaryl substituted [(3-hydroxypyridine-2-carbonyl]amino}acetic acids. Further disclosed are methods for making prodrugs of [(3-hydroxypyridine-2-carbonyl)-amino]acetic acids, for example, {[(3-hydroxypyridine-2-carbonyl]amino}acetic acid esters and {[3-hydroxypyridine-2-carbonyl]amino}acetic acid amides. The disclosed compounds are useful as prolyl hydroxylase inhibittors or for treating conditions wherein prolyl hydroxylase inhibition is desired.
Type:
Grant
Filed:
August 24, 2015
Date of Patent:
October 3, 2017
Assignee:
Akebia Therapeutics, Inc.
Inventors:
Christopher M. Lanthier, Boris Gorin, Jan Oudenes, Craig Edward Dixon, Alan Quigbo Lu, James Densmore Copp, John Michael Janusz
Abstract: Provided is a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity, and useful as a prophylactic or therapeutic drug for Alzheimer's disease, schizophrenia, pain, sleep disorder and the like. The present invention relates to a compound represented by the formula wherein ring A is a 4- to 7-membered ring optionally having substituent(s); L is —O—, —S—, —SO— or —SO2—; R1 is a C1-6 alkyl group optionally having substituent(s) (provided that when L is —O—, R1 is not a C1-6 alkyl group optionally substituted by halogen atom(s)), or a cyclic group optionally having substituent(s); X1 is —CRa? or —N?; X2 is —CRb? or —N?; X3 is —CRc= or —N?; Ra, Rb and Rc are each a C1-6 alkyl group, C2-6 alkenyl group, C1-6 alkoxy group, C3-6 cycloalkyl group, C3-6 cycloalkoxy group or C6-14 aryl group, each of which optionally having substituent(s), H or halogen, or a salt thereof.
Abstract: The present invention provides tricyclic fused thiophene derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
Abstract: The invention relates to besylate salts of the compound of formula (I): Methods of preparing the salts, and their use as medicaments, in particular for sedative or hypnotic, anxiolytic, muscle relaxant, or anticonvulsant purposes is also described.
Type:
Grant
Filed:
November 23, 2015
Date of Patent:
October 3, 2017
Assignee:
PAION UK LIMITED
Inventors:
Gary Stuart Tilbrook, Louisa Jane Quegan