Abstract: The present invention provides azetidinyl phenyl, pyridyl, or pyrazinyl carboxamide derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAKs) 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: A compound represented by the general formula (V) wherein all the symbols are as defined in the specification, has an improved balance of the agonist activity against the S1P5 receptor relative to the S1P1 receptor, and can thus serve as a therapeutic agent for S1P5-mediated diseases such as schizophrenia and Binswanger's disease and other neurodegenerative diseases.
Abstract: The present invention relates to a process for carbonylating allyl alcohols at low temperature, low pressure and/or low catalyst loading. In an alternative embodiment, an acylation product of the allyl alcohol is used for the carbonylation. The present invention likewise relates to the preparation of conversion products of these carbonylation products and specifically of (?)-ambrox.
Type:
Grant
Filed:
February 13, 2018
Date of Patent:
December 7, 2021
Assignee:
BASF SE
Inventors:
Mathias Schelwies, Rocco Paciello, Ralf Pelzer, Wolfgang Siegel
Abstract: Disclosed are an intermediate of Eribulin and a preparation method therefor. In particular, disclosed are compounds as represented by formula II, formula III and formula V and a preparation method therefor. Ar is C1-10 alkyl substituted, alkyloxy substituted or unsubstituted aryl; R1 and R2 is an acetal protecting group or a thioacetal protecting group; R3 is hydrogen or a hydroxyl protecting group; and X is halogen or a leaving group. The preparation method therefor has the advantages of mild reaction conditions, high selectivity, easy purification, low synthesis cost and the like, being suitable for large scale production.
Abstract: The present invention provides substituted pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives of formula (I), which are therapeutically useful, particularly as selective transcriptional CDK inhibitors including CDK7, CDK9, CDK12, CDK13 and CDK18, more particularly transcriptional CDK7 inhibitors wherein X, ring A, ring B, L1, L2, R1, R2, R3, R4, R6, m, n and p have the meanings given in the specification and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorder associated with selective transcriptional CDKs in a mammal. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives of formula (I) or a pharmaceutically acceptable salt thereof or a stereoisomer thereof.
Abstract: Compounds having the following Formula (I), or a pharmaceutically acceptable salt or pharmaceutically acceptable tautomer thereof, and methods of their use and preparation are disclosed:
Type:
Grant
Filed:
July 3, 2019
Date of Patent:
November 30, 2021
Assignee:
Gilead Sciences, Inc.
Inventors:
Mark J. Bartlett, Britton Kenneth Corkey, Kristyna M. Elbel, Rao V. Kalla, Xiaofen Li, Thao Perry
Abstract: The present invention relates to the following compounds wherein the integers are as defined in the description, and where the compounds may be useful as medicaments, for instance for use in the treatment of tuberculosis.
Type:
Grant
Filed:
June 15, 2017
Date of Patent:
November 23, 2021
Assignee:
Janssen Sciences Ireland UC
Inventors:
Jérôme Émile Georges Guillemont, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri
Abstract: Compositions comprising metal organic frameworks and related methods and uses are generally provided, including use in selective carbonylation of heterocyclic compounds.
Type:
Grant
Filed:
October 4, 2017
Date of Patent:
November 23, 2021
Assignee:
Massachusetts Institute of Technology
Inventors:
Yuriy Román-Leshkov, Mircea Dinca, Hoyoung Park
Abstract: An object of the present invention is to provide a method for producing 1,2,4,5-cyclohexanetetracarboxylic dianhydride, which is capable of stably achieving a high dehydration rate. The method for producing 1,2,4,5-cyclohexanetetracarboxylic dianhydride of the present invention is a method for producing 1,2,4,5-cyclohexanetetracarboxylic dianhydride by subjecting 1,2,4,5-cyclohexanetetracarboxylic acid to a dehydration reaction in a slurry state in the presence of a dehydrating agent, wherein an average particle size of the 1,2,4,5-cyclohexanetetracarboxylic acid is 20 ?m or more.
Abstract: The present invention relates to a new preparation method for escitalopram pamoate ((S)-(+)-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-cyanoisob enzofuran pamoate), wherein the method is environmentally friendly and pollution-free, and the escitalopram pamoate prepared by means of the method has a high purity and a good repeatability.
Abstract: The present invention relates to methods of modulating activity of histone deacetylases (HDACs). The present invention also relates to methods of treating HDAC-associated diseases including, but not limited to, cancers, inflammatory disorders, and neurodegenerative disorders. The present invention also provides novel compounds and compositions thereof and methods of preparation of the same. The present invention also includes methods of inhibiting HDACs, and methods of treating HDAC-associated diseases using the compounds of the invention.
Abstract: The present invention provides halichondrin analogs, such as compounds of Formula (I). The compounds may bind to microtubule sites, thereby inhibiting microtubule dynamics. Also provided are methods of synthesis, pharmaceutical compositions, kits, methods of treatment, and uses that involve the compounds for treatment of a proliferative disease (e.g., cancer). Compounds of the present invention are particularly useful for the treatment of metastatic breast cancer, non-small cell lung cancer, prostate cancer, and sarcoma. The included methods of synthesis are useful for the preparation of compounds of Formula (I)-(III) along with naturally occurring halicondrins (e.g., halichondrin B & C, norhalichondrin A, B, & C, and homohalichondrin A, B, & C). Also included are methods for interconverting between the halichondrins, norhalichondrins, and homohalichondrins and their unnatural epimers at the C38 ketal stereocenter through the use of an acid-mediated equilibration.
Type:
Grant
Filed:
January 17, 2020
Date of Patent:
October 26, 2021
Assignee:
President and Fellows of Harvard College
Inventors:
Yoshito Kishi, Atsushi Ueda, Akihiko Yamamoto, Daisuke Kato
Abstract: This disclosure is directed to methods of treating ophthalmic disease/disorder or injury associated with neurodegenerative disease/disorder, such as progressive multiple sclerosis, or a neuro-ophthalmologic disorder in human patients using ibudilast.
Abstract: The present invention discloses a 9,10-dihydro-acridine derivative having a structure of Formula (I). The compound has a suitable HOMO energy level that matches that of an anode and light emitting layer when used as a material of a hole transport layer, thus reducing the potential barrier needed to overcome when holes are transported to the light emitting layer, and reducing the operating voltage of the device. Moreover, the 9,10-dihydro-acridine derivative has high triplet energy level and LUMO level, to avoid the returning of energy from the light emitting layer, retain the electrons in the light emitting layer, increase the probability of recombination of electrons and holes in the light emitting layer, and enhance the luminescence efficiency of the device. The compound of Formula (I) has high glass transition temperature, good film forming performance, and high thermal stability.
Abstract: The invention provides methods for the synthesis of a halichondrin macrolides or analogs thereof through a cyclization reaction strategy. The strategy of the present invention involves subjecting an intermediate to Prins reaction conditions to afford a macrolide. The invention also provides compounds useful as intermediates in the synthesis of a halichondrin macrolides or analogs thereof and methods for preparing the same.
Type:
Grant
Filed:
June 30, 2017
Date of Patent:
October 5, 2021
Assignee:
EISAI R&D MANAGEMENT CO., LTD.
Inventors:
Charles E. Chase, Hyeong-Wook Choi, Atsushi Endo, Francis G. Fang, Dae-Shik Kim
Abstract: The present invention provides crystalline forms of compound of formula (Ia) and processes of making the crystalline forms. Also provided are compositions comprising the crystalline forms and methods of use of the crystalline forms.
Type:
Grant
Filed:
March 20, 2020
Date of Patent:
September 28, 2021
Assignee:
BOEHRINGER INGELHEIM ANIMAL HEALTH USA INC.
Inventors:
Roelof Johannes Gorter de Vries, Bruno Baillon, Sylvaine Lafont, Myriam Gay de Saint Michel, Stephane Kozlovic
Abstract: This disclosure relates generally to the facile and selective mono-perfluoro and poly-fluoroarylation of Meldrum's acid to generate a versatile synthon for highly fluorinated alpha-phenyl acetic acid derivatives which provide straightforward access to fluorinated building blocks. The reaction takes place quickly and all products were isolated without the need for chromatography. An embodiment provides an alternative strategy to access alpha-arylated Meldrum's acids which avoids the need for aryl-Pb(IV) salts or diaryliodonium salts and provides access to the tertiary product which was not previously synthetically accessible. The synthetic versatility and utility of the Meldrum's acid products is demonstrated by subjecting the products to several derivatizations of the Meldrum's acid products as well as photocatalytic hydrodefluorination which provide access to difficult but valuable synthetic targets such as multifluorinated aromatics.
Type:
Grant
Filed:
May 6, 2019
Date of Patent:
September 14, 2021
Assignee:
The Board of Regents for Oklahoma State University
Abstract: Stable Phytonadione compositions for parenteral administration are provided which comprise (E) isomer of phytonadione at or greater than 97% w/w as the active ingredient, and is substantially free of (Z) isomer. Said compositions are stable, sterile, and particulate-free. Further, said compositions reduce or avoid allergic reactions to benzyl alcohol and polysorbate. In some aspects, the compositions are free or substantially free of benzyl alcohol and/or reduced amounts of polysorbate. Methods of manufacture and methods of administration also provided.
Type:
Grant
Filed:
July 24, 2018
Date of Patent:
August 24, 2021
Assignee:
Exela Holdings, Inc.
Inventors:
Phanesh Koneru, Sreerarama Murthy Mallipeddi, Jonathan E. Sterling
Abstract: It is an aim of the present invention to provide inhibitors of human diphtheria toxin-like ADP-ribosyltransferases, such as ARTD10, for use as a medicine. It is another aim of the invention to provide compounds for use as human mono-ADP-ribosyltransferase (mARTD) inhibitors in vitro. In the present invention, it has been discovered that human ARTD10, which belongs to an enzyme family linked to cancer biology, can be specifically inhibited by the benzamide comprising compounds disclosed in the invention, such as 4,4?-oxydibenzamide.
Type:
Grant
Filed:
April 6, 2017
Date of Patent:
August 24, 2021
Assignee:
University of Oulu
Inventors:
Lari Lehtiö, Harikanth Venkannagari, Bernhard Lüscher, Patricia Verheugd