Patents by Inventor Kim D. Janda
Kim D. Janda has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Patent number: 11891392Abstract: 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: GrantFiled: July 12, 2021Date of Patent: February 6, 2024Assignee: The Scripps Research InstituteInventors: Kim D. Janda, Nicholas T. Jacob, Jonathan W. Lockner
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Publication number: 20230399418Abstract: The disclosure provides, inter alia, antibodies, pharmaceutical compositions containing antibodies, and the use of the antibodies and pharmaceutical compositions to treat or prevent opioid overdoses, to treat opioid use disorder, and to treat or prevent opioid-induced respiratory depression.Type: ApplicationFiled: November 8, 2021Publication date: December 14, 2023Inventors: Kim D. Janda, Paul T. Bremer, Bin Zhou
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Patent number: 11660331Abstract: An improved heroin conjugate vaccine is detailed; to accomplish this task the systematic exploration of twenty vaccine formulations with varying combinations of carrier proteins and adjuvants were undertaken. In regard to adjuvants, a Toll-like receptor 9 (TLR9) agonist and a TLR3 agonist in the presence of alum were explored. The vaccine formulations containing TLR3 or TLR9 agonist alone-elicited strong anti-heroin antibody titers and blockade of heroin-induced antinociception when formulated with alum; however, a combination of TLR3 and 9 adjuvants did not result in improved efficacy. Investigation of stability of the two lead formulations revealed that the TLR9 but not the TLR3 formulation was stable when stored over 30 days. Furthermore, mice immunized with the TLR9+alum heroin vaccine gained significant protection from lethal heroin doses, suggesting that this vaccine formulation is suitable for mitigating the lethal effects of heroin, even following long-term storage at room temperature.Type: GrantFiled: November 8, 2018Date of Patent: May 30, 2023Assignee: The Scripps Research InstituteInventor: Kim D. Janda
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Patent number: 11613535Abstract: There is disclosed a compound, a pharmaceutical composition and a method of cancer treatment with an improved Myc inhibitor compound. More specifically, there is disclosed an improved compound having with improved solubility, improved binding characteristics and better efficacy and therapeutic activity inhibiting c-MYC wherein the improved compound comprises a tri-substituted pyridine having a thiazoyl moiety at position R1 versus an earlier disclosed genus of tri-substituted pyridine structures.Type: GrantFiled: July 8, 2019Date of Patent: March 28, 2023Assignee: The Scripps Research InstituteInventor: Kim D. Janda
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Patent number: 11305010Abstract: Fentanyl is an addictive prescription opioid that is over 80 times mora potent than morphine. The synthetic nature of fentanyl has enabled the creation of dangerous “designer drug’ analogues that escape toxicology screening, yet display comparable potency to the parent drug. Alarmingly, a large number of fatalities have been linked to overdose of fentanyl derivatives. Herein, we report an effective immunotherapy for reducing the psychoactive effects of fentanyl class drugs. A single conjugate vaccine was created that elicited high levels of antibodies with cross-reactivity for a wide panel of fentanyl analogues, Moreover, vaccinated mice gained significant protection from lethal fentanyl doses. Lastly, a surface plasmon resonance (SPR)-based technique was established enabling drug specificity profiling of antibodies derived directly from serum. Our newly developed fentanyl vaccine and analytical methods may assist in the battle against synthetic opioid abuse.Type: GrantFiled: January 18, 2017Date of Patent: April 19, 2022Assignee: The Scripps Research InstituteInventor: Kim D. Janda
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Publication number: 20220081400Abstract: The disclosure provides, inter alia, opioid haptens, opioid hapten conjugates, opioid vaccines, methods of treating or preventing opioid use disorder, methods of treating opioid overdose, and methods of generating and/or isolating antibodies selective for opioids.Type: ApplicationFiled: July 16, 2019Publication date: March 17, 2022Inventors: Kim D. Janda, Paul Bremer, Yoshihiro Natori
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Publication number: 20220002300Abstract: 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: ApplicationFiled: July 12, 2021Publication date: January 6, 2022Inventors: Kim D. JANDA, Nicholas T. JACOB, Jonathan W. LOCKNER
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Publication number: 20210269430Abstract: There is disclosed a compound, a pharmaceutical composition and a method of cancer treatment with an improved Myc inhibitor compound. More specifically, there is disclosed an improved compound having with improved solubility, improved binding characteristics and better efficacy and therapeutic activity inhibiting c-MYC wherein the improved compound comprises a tri-substituted pyridine having a thiazoyl moiety at position R1 versus an earlier disclosed genus of tri-substituted pyridine structures.Type: ApplicationFiled: July 8, 2019Publication date: September 2, 2021Inventor: Kim D. Janda
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Publication number: 20210268088Abstract: An improved heroin conjugate vaccine is detailed; to accomplish this task the systematic exploration of twenty vaccine formulations with varying combinations of carrier proteins and adjuvants were undertaken. In regard to adjuvants, a Toll-like receptor 9 (TLR9) agonist and a TLR3 agonist in the presence of alum were explored. The vaccine formulations containing TLR3 or TLR9 agonist alone-elicited strong anti-heroin antibody titers and blockade of heroin-induced antinociception when formulated with alum; however, a combination of TLR3 and 9 adjuvants did not result in improved efficacy. Investigation of stability of the two lead formulations revealed that the TLR9 but not the TLR3 formulation was stable when stored over 30 days. Furthermore, mice immunized with the TLR9+alum heroin vaccine gained significant protection from lethal heroin doses, suggesting that this vaccine formulation is suitable for mitigating the lethal effects of heroin, even following long-term storage at room temperature.Type: ApplicationFiled: November 8, 2018Publication date: September 2, 2021Inventor: Kim D. Janda
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Patent number: 11066398Abstract: This invention provides small molecule Myc-inhibitors. Also provided in the invention are therapeutic applications of these compounds for treating Myc-driven cancer and other related methods.Type: GrantFiled: December 10, 2014Date of Patent: July 20, 2021Assignees: The Scripps Research Institute, Sorrento Therapeutics, Inc.Inventors: Peter K. Vogt, Francis X. Tavares, Kim D. Janda
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Publication number: 20210128720Abstract: Fentanyl is an addictive prescription opioid that is over 80 times mora potent than morphine. The synthetic nature of fentanyl has enabled the creation of dangerous “designer drug’ analogues that escape toxicology screening, yet display comparable potency to the parent drug. Alarmingly, a large number of fatalities have been linked to overdose of fentanyl derivatives. Herein, we report an effective immunotherapy for reducing the psychoactive effects of fentanyl class drugs. A single conjugate vaccine was created that elicited high levels of antibodies with cross-reactivity for a wide panel of fentanyl analogues, Moreover, vaccinated mice gained significant protection from lethal fentanyl doses. Lastly, a surface plasmon resonance (SPR)-based technique was established enabling drug specificity profiling of antibodies derived directly from serum. Our newly developed fentanyl vaccine and analytical methods may assist in the battle against synthetic opioid abuse.Type: ApplicationFiled: January 18, 2017Publication date: May 6, 2021Inventor: Kim D. Janda
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Publication number: 20210093605Abstract: In this study, we capitalized on the antimicrobial property and low oral bioavailability of known salicylanilide anthelmintics (closantel, rafoxanide, niclosamide, oxyclozanide) to target the gut pathogen. The anthelmintics displayed excellent potency against C. difficile strains 630 and 4118 (with MIC values as low as 0.06-0.13 ?g/mL for rafoxanide) via a membrane depolarization mechanism. Interestingly, closantel, rafoxanide and compound 8 were bactericidal against logarithmic- and stationary-phase cultures of the BI/NAP1/027 strain 4118. Further evaluation of the salicylanilides showed their preferential activity against Gram-positive over Gram-negative bacteria. Moreover, the salicylanilides were non-hemolytic and were non-toxic to mammalian cell lines HepG2 and HEK 293T/17 within the range of their in vitro MICs and MBCs. The salicylanilide anthelmintics exhibit desirable bactericidal and pharmacokinetic properties and are amenable to repositioning as anti-C. difficile agents.Type: ApplicationFiled: September 9, 2020Publication date: April 1, 2021Inventor: Kim D. Janda
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Patent number: 10792272Abstract: In this study, we capitalized on the antimicrobial property and low oral bioavailability of known salicylanilide anthelmintics (closantel, rafoxanide, niclosamide, oxyclozanide) to target the gut pathogen. The anthelmintics displayed excellent potency against C. difficile strains 630 and 4118 (with MIC values as low as 0.06-0.13 ?g/mL for rafoxanide) via a membrane depolarization mechanism, interestingly, closantel, rafoxanide and compound 8 were bactericidal against logarithmic- and stationary-phase cultures of the BI/NAP1/027 strain 4118. Further evaluation of the salicylanilides showed their preferential activity against Gram-positive over Gram-negative bacteria. Moreover, the salicylanilides were non-hemolytic and were non-toxic to mammalian cell lines HepG2 and HEK 293T/17 within the range of their in vitro MICs and MBCs. The salicylanilide anthelmintics exhibit desirable bactericidal and pharmacokinetic properties and are amenable to repositioning as anti-C. difficile agents.Type: GrantFiled: July 14, 2017Date of Patent: October 6, 2020Assignee: THE SCRIPPS RESEARCH INSTITUTEInventor: Kim D. Janda
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Publication number: 20200283440Abstract: 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: ApplicationFiled: April 14, 2020Publication date: September 10, 2020Applicant: THE SCRIPPS RESEARCH INSTITUTEInventors: Kim D. JANDA, Nicholas T. JACOB, Jonathan W. LOCKNER
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Patent number: 10633385Abstract: 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: GrantFiled: March 20, 2019Date of Patent: April 28, 2020Assignee: THE SCRIPPS RESEARCH INSTITUTEInventors: Kim D. Janda, Nicholas T. Jacob, Jonathan W. Lockner
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Patent number: 10487141Abstract: The invention provides chiral haptens (?)-3?-AmNic and (?)-N4N for use in generating antibodies in a patient specific for (?)-nicotine. The haptens can be conjugated to suitable carrier proteins and administered as an antigenic mixture, optionally comprising adjuvant(s), to a patient suffering from nicotine or tobacco addiction or habituation.Type: GrantFiled: December 10, 2018Date of Patent: November 26, 2019Assignee: The Scripps Research InstituteInventors: Kim D. Janda, Jonathan W. Lockner
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Publication number: 20190350891Abstract: In this study, we capitalized on the antimicrobial property and low oral bioavailability of known salicylanilide anthelmintics (closantel, rafoxanide, niclosamide, oxyclozanide) to target the gut pathogen. The anthelmintics displayed excellent potency against C. difficile strains 630 and 4118 (with MIC values as low as 0.06-0.13 ?g/mL for rafoxanide) via a membrane depolarization mechanism, interestingly, closantel, rafoxanide and compound 8 were bactericidal against logarithmic- and stationary-phase cultures of the BI/NAP1/027 strain 4118. Further evaluation of the salicylanilides showed their preferential activity against Gram-positive over Gram-negative bacteria. Moreover, the salicylanilides were non-hemolytic and were non-toxic to mammalian cell lines HepG2 and HEK 293T/17 within the range of their in vitro MICs and MBCs. The salicylanilide anthelmintics exhibit desirable bactericidal and pharmacokinetic properties and are amenable to repositioning as anti-C. difficile agents.Type: ApplicationFiled: July 14, 2017Publication date: November 21, 2019Inventor: Kim D. Janda
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Publication number: 20190284188Abstract: 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: ApplicationFiled: March 20, 2019Publication date: September 19, 2019Inventors: Kim D. Janda, Nicholas T. Jacob, Jonathan W. Lockner
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Publication number: 20190240306Abstract: The invention provides haptens and methods of preparation thereof, for producing immunoconjugates of oxycodone and hydrocodone suitable for raising antibodies in animals specific for the opioid drugs. Administration of the opioid-speeific antibodies to humans having the opioid drugs in a body fluid such as blood serum, binds the opioid drugs to the antibody, making the opioids unavailable for producing a drug effect. Accordingly the antibodies can be used to reverse the effects of a drug overdose of oxycodone and hydrocodone, or to reverse a perceived mental effect of the drugs, such as euphoria.Type: ApplicationFiled: October 17, 2017Publication date: August 8, 2019Inventor: Kim D. Janda
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Publication number: 20190119363Abstract: The invention provides chiral haptens (?)-3?-AmNic and (?)-N4N for use in generating antibodies in a patient specific for (?)-nicotine. The haptens can be conjugated to suitable carrier proteins and administered as an antigenic mixture, optionally comprising adjuvant(s), to a patient suffering from nicotine or tobacco addiction or habituation.Type: ApplicationFiled: December 10, 2018Publication date: April 25, 2019Inventors: Kim D. Janda, Jonathan W. Lockner