Patents Assigned to The Scripps Research Institute
  • Patent number: 10774068
    Abstract: Disclosed herein are compounds, compositions, and methods of their use for the treatment of diabetes.
    Type: Grant
    Filed: June 24, 2016
    Date of Patent: September 15, 2020
    Assignees: THE SCRIPPS RESEARCH INSTITUTE, UNIVERSITÄT BREMEN
    Inventors: Hank Michael James Petrassi, Murali Mohan Reddy Peram Surakattula, Kathrin Maedler, Amin Ardestani, Jason T. Roland, Tyler D. Baguley, Matthew S. Tremblay, Weijun Shen, Peter G. Schultz, Arnab K. Chatterjee
  • Publication number: 20200283440
    Abstract: There are disclosed imidazolinopyrimidinone compounds that have activity to induce TRAIL gene expression in macrophages. There is further disclosed a method for treating various cancers comprising administering effective amounts of an imidazolinopyrimidinone having the structure of Formula I herein.
    Type: Application
    Filed: April 14, 2020
    Publication date: September 10, 2020
    Applicant: THE SCRIPPS RESEARCH INSTITUTE
    Inventors: Kim D. JANDA, Nicholas T. JACOB, Jonathan W. LOCKNER
  • Patent number: 10765645
    Abstract: This application describes a compound represented by Formula (I): YZX1—S(O)(X2)F)m]n??(I) wherein: Y is a biologically active organic core group comprising one or more of an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group, to which Z is covalently bonded; n is 1, 2, 3, 4 or 5; m is 1 or 2; Z is O, NR, or N; X1 is a covalent bond or —CH2CH2—, X2 is O or NR; and R comprises H or a substituted or unsubstituted group selected from an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group. Methods of preparing the compounds, methods of using the compounds, and pharmaceutical compositions comprising the compounds are described as well.
    Type: Grant
    Filed: October 12, 2018
    Date of Patent: September 8, 2020
    Assignee: THE SCRIPPS RESEARCH INSTITUTE
    Inventors: Jiajia Dong, K. Barry Sharpless, Jeffery W. Kelly, Aleksandra Baranczak, Wentao Chen
  • Patent number: 10758522
    Abstract: The invention is directed to a method of inhibiting, within a living cell, the interaction between NF-?B essential modulator (“NEMO”) with I?B kinase-? (IKK-?) at the NEMO binding domain (NBD), comprising exposing the cell to an effective amount or concentration of a compound of the invention, a NEMO-binding domain analog (NBDA). The invention is further directed to a method of treating a condition in a patient, wherein inhibiting the interaction between NF-?B essential modulator (“NEMO”) with I?B kinase-? (IKK-?) at the NEMO binding domain (NBD) is medically indicated, comprising administering to the patient an effective dose of a compound of the invention. Conditions that can be treated by a method of the invention includes muscular dystrophy, asthma, inflammatory bowel disease, multiple sclerosis, Parkinson's Disease, arthritis, diabetes, graft versus host disease, accelerated aging, heart ischemia, cancer, UV-induced skin damage, or an age-related pathology.
    Type: Grant
    Filed: May 25, 2016
    Date of Patent: September 1, 2020
    Assignee: THE SCRIPPS RESEARCH INSTITUTE
    Inventors: Paul Robbins, Laura Niedernhofer, Theodore Kamenecka, Gabriela Mustata Wilson
  • Patent number: 10759743
    Abstract: Pd(II)-catalyzed g-G(sp3)-H arylation or heteroarylation of primary amines is realized by using 2-hydroxynicotinaldehyde as a catalytic transient directing group. Importantly, the catalyst and the directing group loading can be lowered to 2% and 4% respectively, thus demonstrating high efficiency of this newly designed transient directing group. Heterocyclic aryl iodides are also compatible with this reaction. Furthermore, swift synthesis of 1,2,3,4-tetrahydronaphthyridine derivatives is accomplished using this reaction.
    Type: Grant
    Filed: October 19, 2017
    Date of Patent: September 1, 2020
    Assignee: THE SCRIPPS RESEARCH INSTITUTE
    Inventor: Jin-Quan Yu
  • Publication number: 20200271657
    Abstract: Described are methods for providing personalized medicine for the treatment of B cell malignancies including lymphoma. The methods make use of Chimeric Antigen Receptor (CAR) technology.
    Type: Application
    Filed: October 4, 2018
    Publication date: August 27, 2020
    Applicants: OPKO Pharmaceuticals, LLC, The Scripps Research Institute, Bioorganic Chemistry, Russian Academy of Sciences, PJSC Pharmsynthez
    Inventors: Alexey Vyacheslavovich Stepanov, Dmitry Dmitrievich Genkin, Richard A. Lerner, Alexey Anatolievich Belogurov, Alexander Gabibovich Gabibov, Jia Xie
  • Publication number: 20200268683
    Abstract: A high-throughput screening methods for identifying candidate anticancer medicinal agents is described herein. The candidate anticancer medicinal agents are arylfluorosulfate compounds derived from phenolic compounds. The method involves in situ generation of the arylfluorosulfate compounds in multi-well plates by reaction of phenolic compounds in DMSO with a saturated solution of SO2F2 dissolved in a solvent such as acetonitrile, in the presence of an organic base, followed by reaction of generated fluoride ion with trimethylsilyl chloride to form volatile trimethylsilyl fluoride. Solvents, organic base, and silyl compounds are then removed, in vacuo, to afford the arylfluorosulfate compounds suitable for biological screening in cancer cell lines without further purification.
    Type: Application
    Filed: May 11, 2020
    Publication date: August 27, 2020
    Applicant: THE SCRIPPS RESEARCH INSTITUTE
    Inventors: Jie LI, Zilei LIU, Suhua LI, Peng WU, K. Barry SHARPLESS
  • Patent number: 10751335
    Abstract: The invention provides—opioid receptor agonists that are analgesic agents and that promote diminished side effects relative to a comparably effective dose of morphine. The side effects that are absent or attenuated include one or more of the following: constipation, respiratory depression, tolerance, dependence, nausea, confusion, sedation, hypotension, and post-treatment withdrawal symptoms.
    Type: Grant
    Filed: March 15, 2017
    Date of Patent: August 25, 2020
    Assignee: THE SCRIPPS RESEARCH INSTITUTE
    Inventors: Thomas D. Bannister, Laura M. Bohn, Cullen L. Schmid
  • Patent number: 10745340
    Abstract: The invention provides processes and materials for the efficient and cost-effective functionalization of alkanes, such as methane from natural gas, to provide esters, alcohols, and other compounds. The method can be used to produce liquid fuels such as methanol from a natural gas methane-containing feedstock. The soft oxidizing electrophile, a compound of a main group, post-transitional element such as Tl, Pb, Bi, and I, that reacts to activate the alkane C—H bond can be regenerated using inexpensive regenerants such as hydrogen peroxide, oxygen, halogens, nitric acid, etc. Main group compounds useful for carrying out this reaction includes haloacetate salts of metals having a pair of available oxidation states, such as Tl, Pb, Bi, and I.
    Type: Grant
    Filed: February 25, 2014
    Date of Patent: August 18, 2020
    Assignee: The Scripps Research Institute
    Inventors: Roy A Periana, Brian G Hashiguchi, Michael M Konnick, Steven M Bischof
  • Patent number: 10744117
    Abstract: The invention provides methods of treatment of a progressive bone disease, such as osteoporosis, Paget's Disease, multiple myeloma, or hyperparathyroidism, comprising administration of an effective amount of a non-agonist PPARG modulator to a patient afflicted with the disease.
    Type: Grant
    Filed: July 6, 2018
    Date of Patent: August 18, 2020
    Assignees: The Scripps Research Institute, The University of Toledo
    Inventors: Patrick R. Griffin, Theodore Kamenecka, Beata Lecka-Czernik
  • Patent number: 10745456
    Abstract: The invention provides combinatorial peptide or polypeptide libraries that can become membrane tethered once expressed in cells. The invention additionally provides methods for selecting peptide modulators (e.g., agonists) of GPCRs from the combinatorial libraries of the invention. The invention also provides novel GPCR polypeptide modulators, e.g., biased polypeptide agonists of the glucagon-like peptide 1 receptor (GLP-1R). The invention further provides methods of promoting insulin sensitivity, lowering blood glucose, and reducing body weight as well as methods for treating various diseases such as diabetes and obesity.
    Type: Grant
    Filed: April 1, 2016
    Date of Patent: August 18, 2020
    Assignee: The Scripps Research Institute
    Inventors: Richard A. Lerner, Hongkai Zhang, Patricia McDonald, Jia Xie, Emmanuel Sturchler, Philip Dawson
  • Patent number: 10738281
    Abstract: The present invention provides for methods, compositions, and kits for producing an induced pluripotent stem cell from a non-pluripotent mammalian cell using a 3?-phosphoinositide-dependent kinase-1 (PDK1) activator or a compound that promotes glycolytic metabolism as well as other small molecules.
    Type: Grant
    Filed: January 3, 2019
    Date of Patent: August 11, 2020
    Assignee: The Scripps Research Institute
    Inventors: Saiyong Zhu, Sheng Ding
  • Patent number: 10741291
    Abstract: A computer-based genomic annotation system, including a database configured to store genomic data, non-transitory memory configured to store instructions, and at least one processor coupled with the memory, the processor configured to implement the instructions in order to implement an annotation pipeline and at least one module filtering or analysis of the genomic data.
    Type: Grant
    Filed: March 26, 2015
    Date of Patent: August 11, 2020
    Assignee: THE SCRIPPS RESEARCH INSTITUTE
    Inventor: Ali Torkamani
  • Patent number: 10717820
    Abstract: Condensation of fluoro-substituted and silyl-substituted monomers provides polymers suitable for use, e.g., as engineering polymers. A monomer composition is condensed in the presence of a bifluoride or poly(hydrogen fluoride) fluoride salt. The monomer composition contains a compound of formula F-X-F and a compound of formula (R1)3Si—Z—Si(R1)3, and forms an alternating X-Z polymer chain and a silyl fluoride byproduct. X has the formula -A(-R2-A)n-; each A is SO2, C(?O), or Het; R2 is an organic moiety; n is 0 or 1; Het is an aromatic nitrogen heterocycle; Z has the formula -L-R3-L-; each L is O, S, or N(R4); and each R3 is an organic moiety, and R4 comprises H or an organic moiety.
    Type: Grant
    Filed: June 22, 2016
    Date of Patent: July 21, 2020
    Assignee: THE SCRIPPS RESEARCH INSTITUTE
    Inventors: K. Barry Sharpless, Jiajia Dong, Bing Gao, Peng Wu, Hua Wang
  • Patent number: 10696720
    Abstract: Disclosed herein are proteins, methods, cells, engineered microorganisms, and kits for generating a modified nucleoside triphosphate transporter from Phaeodactylum tricornutum. Also disclosed herein proteins, methods, cells, engineered microorganisms, and kits for production of a nucleic acid molecule that comprises an unnatural nucleotide utilizing a modified nucleoside triphosphate transporter from Phaeodactylum tricornutum.
    Type: Grant
    Filed: August 20, 2019
    Date of Patent: June 30, 2020
    Assignee: THE SCRIPPS RESEARCH INSTITUTE
    Inventors: Floyd E. Romesberg, Yorke Zhang
  • Patent number: 10696635
    Abstract: A class of mono-protected 3-amino-2-hydroxypyridine (MPAHP) ligands that enable the meta-C—H arylation of anilines, phenols, phenylacetic acids, and biologically relevant heterocyclic compounds using norbornene as a transient mediator is disclosed, such as in the formation of a reaction product of Formula IA: The applicability of this meta-arylation methodology in the pharmaceutical industry is illustrated for heteroaryl substrates and heteroaryl iodide coupling partners, a feat made possible by using the MPAHP ligand. The enabling nature of MPAHP ligands to achieve other meta-C—H functionalization processes is also illustrated by the development of a meta-C—H amination reaction and a meta-C—H alkynylation reaction.
    Type: Grant
    Filed: April 18, 2017
    Date of Patent: June 30, 2020
    Assignee: THE SCRIPPS RESEARCH INSTITUTE
    Inventor: Jin-Quan Yu
  • Patent number: 10696719
    Abstract: Disclosed herein are proteins, methods, cells, engineered microorganisms, and kits for generating a modified nucleoside triphosphate transporter from Phaeodactylum tricornutum. Also disclosed herein proteins, methods, cells, engineered microorganisms, and kits for production of a nucleic acid molecule that comprises an unnatural nucleotide utilizing a modified nucleoside triphosphate transporter from Phaeodactylum tricornutum.
    Type: Grant
    Filed: August 20, 2019
    Date of Patent: June 30, 2020
    Assignee: THE SCRIPPS RESEARCH INSTITUTE
    Inventors: Floyd E. Romesberg, Yorke Zhang
  • Publication number: 20200197497
    Abstract: Disclosed herein are chimeric antigen receptor effector cells (CAR-ECs) and CAR-EC switches. The switchable CAR-ECs are generally T cells. The one or more chimeric antigen receptors may recognize a peptidic antigen on the CAR-EC switch. The CAR-ECs and switches may be used for the treatment of a condition in a subject in need thereof.
    Type: Application
    Filed: August 6, 2019
    Publication date: June 25, 2020
    Applicant: The Scripps Research Institute
    Inventors: Travis YOUNG, Chanhyuk KIM, Peter G. SCHULTZ
  • Patent number: 10689381
    Abstract: A vinca alkaloid compound substituted at the 20?-position with a carboxamido group is disclosed. The carbonyl of the carboxamido group is bonded to a 20?-amino group and to a ring system that contains up to three 5-, 6- or 7-membered rings that are fused or otherwise bonded together. Each ring can be carbocyclic or heterocyclic, with a heterocyclic ring containing up to three hetero ring atoms that are the same or different and are selected from nitrogen, oxygen and sulfur. The ring system can include up to four substituent groups other than hydrogen that are discussed within. Methods of preparing the compounds are disclosed as are compositions for their use and methods of treatment using d compound. A particularly preferred compound has an activity in specified cancer cell growth inhibition assays that is the same or better than its parental, unsubstituted vinca compound and is not subject to Pgp-mediated efflux.
    Type: Grant
    Filed: August 1, 2018
    Date of Patent: June 23, 2020
    Assignee: The Scripps Research Institute
    Inventor: Dale Boger
  • Patent number: 10683353
    Abstract: Disclosed herein are immunoglobulin fusion proteins comprising a first antibody region, a first therapeutic agent, and a first connecting peptide; wherein the first therapeutic agent is attached to the first antibody region by the connecting peptide; and wherein the connecting peptide does not comprise a region having beta strand secondary structure. The connecting peptide may comprise an extender peptide. The extender peptide may have an alpha helical secondary structure. The connecting peptide may comprise a linker peptide. The linker peptide may not comprise any secondary structure. Also disclosed herein are compositions comprising the immunoglobulin fusion proteins and methods for using the immunoglobulin fusion proteins for the treatment or prevention of a disease or condition in a subject.
    Type: Grant
    Filed: July 11, 2014
    Date of Patent: June 16, 2020
    Assignee: THE SCRIPPS RESEARCH INSTITUTE
    Inventors: Feng Wang, Yong Zhang, Yan Liu, Peter G. Schultz