Bicyclo Ring System Having The Thiazole Ring As One Of The Cyclos Patents (Class 514/367)
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Patent number: 12187717Abstract: A compound represented by Formula 1, a stereoisomer thereof or a pharmaceutically acceptable salt thereof may be used for treating or preventing an autoimmune disease or a cancer. The autoimmune disease may be any one selected from the group consisting of inflammatory bowel disease, multiple sclerosis, graft-versus-host disease, asthma, atopy, psoriasis, rheumatoid arthritis, systemic lupus erythematous and type 1 diabetes. The cancer may be selected from the group consisting of colon cancer, melanoma, liver cancer, gliocytoma, ovarian cancer, colorectal cancer, head and neck cancer, bladder cancer, kidney cell cancer, stomach cancer, breast cancer, metastatic cancer, prostate cancer, gallbladder cancer, pancreatic cancer, blood cancer, skin cancer and lung cancer.Type: GrantFiled: August 30, 2023Date of Patent: January 7, 2025Assignee: PARENCHYMA BIOTECH INC.Inventors: Su Kil Seo, Eun Hye Yoon, Soung Min Lee, Hae Jeong Won, Won Hee Jang, Chae Eun Kim
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Patent number: 12162894Abstract: A structural analog of Cyclotheonellazole A, and a synthetic method therefor and an application method thereof are provided. A compound with a structure of formula (I) and a pharmaceutically acceptable salt thereof are provided. The formula (I) is as follows: R1, R2, R3 and R4 are independently selected form the group consisting of H, a C1-C6 alkyl group, a C1-C6 alkoxy group, a halogen group, a hydroxyl group, an amino group, a nitro group, a cyano group, and a sulfydryl group. Based on the total synthetic route of Cyclotheonellazole A, the classical reverse synthesis analysis is utilized, the structural modification is purposefully carried out, a mother nucleus of the natural product remains unchanged, and the structural analog 1a is obtained by replacing a left side chain with a simple formylamine, thereby confirming the excellent protease inhibitory activity thereof, and having a strong application prospect in the pharmaceutical industry.Type: GrantFiled: December 4, 2023Date of Patent: December 10, 2024Assignee: The Second People's Hospital of Shenzhen (Shenzhen Institute of Geriatrics)Inventors: Zhengzhi Wu, Bohua Long, Zhiyue Li, Liuyang Pu, Shengquan Hu, Limin Li
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Patent number: 12145941Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, thereof: which inhibit coronavirus replication activity. The invention further relates to pharmaceutical compositions comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof, and methods of treating or preventing a coronavirus infection in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt thereof.Type: GrantFiled: December 6, 2022Date of Patent: November 19, 2024Assignee: Enanta Pharmaceuticals, Inc.Inventors: Joseph D. Panarese, Sean Rafferty, Jonathan Thielman, Nathaniel T. Kenton, Samuel Bartlett, Yat Sun Or
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Patent number: 11919873Abstract: A compound 1,3-benzothiazol-2-yl-N?-(benzoyloxy)ethanimidamide, its synthesis, and its use as an anticancer and/or antimicrobial agent.Type: GrantFiled: August 29, 2023Date of Patent: March 5, 2024Assignee: KING FAISAL UNIVERSITYInventors: Mai Mostafa Khalaf Ali, Hany Mohamed Abd El-Lateef Ahmed, Antar Ahmed Abdelhamid Ahmed, Amer A. Amer, Doaa H. Ahmed
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Patent number: 11911369Abstract: Pharmaceutical compositions of the invention include substituted riluzole prodrugs useful for the treatment of cancers including melanoma, breast cancer, brain cancer, and prostate cancer through the release of riluzole. Prodrugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process.Type: GrantFiled: May 4, 2020Date of Patent: February 27, 2024Assignee: Biohaven Therapeutics Ltd.Inventors: Jay Edward Wrobel, Allen B. Reitz, Jeffery Claude Pelletier, Garry Robert Smith, Haiyan Bian
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Patent number: 11884673Abstract: Compounds useful in the modulation of ion channel activity in cells are disclosed herein. This disclosure also relates to use of these compounds in the treatment of pain, and pharmaceutical compositions containing these compounds and methods for their preparation.Type: GrantFiled: April 20, 2022Date of Patent: January 30, 2024Assignee: BIONOMICS LIMITEDInventors: Belinda Huff, Courtney Hollis, Hamish Toop, Nathan Kuchel, Lorna Helen Mitchell, Rajinder Singh
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Patent number: 11845740Abstract: The invention relates to chemistry of organic substances, pharmacology and medicine, and concerns treating diseases associated and with aberrant activity of cells of the immune system, more particularly for treating lung, respiratory tract and abdominal diseases, radiation sickness and pain syndrome, and also other diseases by using compounds of formula (A) wherein R1 is —C(O)—R2—(O)— or —R2—C(O)— group, where R2 is —(CH2)n-group optionally substituted with one or two C1-C6 alkyls, or phenyl, n is an integer from 0 to 4; wherein compounds are selected from the group consisting of the group of compounds as set out in the description. These compounds, as well as pharmaceutically acceptable salts thereof, are highly effective in inhibiting glutaminyl cyclase, which is involved, in particular, in processes of post-translational modification of chemokines and chemotaxis of monocytes, macrophages and other cells of the immune system.Type: GrantFiled: May 24, 2018Date of Patent: December 19, 2023Assignees: LTD “VALENTA-INTELLEKT”Inventors: Vladimir Evgenievich Nebolsin, Anastasia Vladimirovna Rydlovskaya, Tatyana Alexandrovna Kromova
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Patent number: 11827630Abstract: Provided are novel crystalline forms of Lanifibranor (Referred to as “Compound I”) and preparation methods thereof, pharmaceutical compositions containing the crystalline forms, and uses of the crystalline forms for preparing pan-PPAR agonists drugs and drugs for treating NASH. Compared with prior arts, the provided crystalline forms of Compound I have one or more improved properties, which solve the problems of the prior art and is of great value to the optimization and development of the drugs.Type: GrantFiled: August 15, 2022Date of Patent: November 28, 2023Assignee: CRYSTAL PHARMACEUTICAL (SUZHOU) CO., LTD.Inventors: Minhua Chen, Hongyan Zhu
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Patent number: 11739104Abstract: The present invention provides compositions and methods for inhibiting group II intron splicing for treating or preventing a disease or disorder associated with an organism harboring an active group II intron. The present invention also provides compositions and methods for inhibiting group II intron splicing for inhibiting, preventing or reducing growth of an organism harboring an active group II intron.Type: GrantFiled: January 25, 2019Date of Patent: August 29, 2023Assignee: YALE UNIVERSITYInventors: Anna Pyle, Olga Fedorova, Erik Gunnar Jagdmann, Michael Van Zandt, Lin Yuan, Albert DeBerardinis
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Patent number: 11717804Abstract: An 8-hydroxyquinoline modified halloysite nanoclay (8-HQHNC) is provided. The 8-HQHNC is used in a method of removing heavy metals and/or salt from a solution which includes steps of contacting the solution with 8-HQHNC under conditions suitable for the adsorption of the heavy metals and/or salt to the 8-HQHNC and recovering the 8-HQHNC from the solution.Type: GrantFiled: November 16, 2022Date of Patent: August 8, 2023Assignee: KING ABDULAZIZ UNIVERSITYInventors: Mohamed Abdel Salam, Radwan K. Al-Farawati, Naif Salama Aljohani, Ibrahim I. Shabbaj
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Patent number: 11639337Abstract: The present invention relates compounds of Formula (A), as well as their preparation and uses, and further relates pharmaceutical compositions comprising these compounds and their uses as modulators of dysfunctional glutamate transmission. The present invention also relates to uses of the compounds or pharmaceutical compositions in treating or preventing certain neurological and psychiatric disorders and diseases as well as cancer in humans.Type: GrantFiled: June 8, 2022Date of Patent: May 2, 2023Assignee: XWPHARMA LTD.Inventors: Jia-Ning Xiang, Xuesong Xu, Wei Zhou
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Patent number: 11554117Abstract: Methods of treating mental disorders, including anxiety disorders such as obsessive-compulsive disorder, are provided. The methods comprise administering an effective amount of a glutamate modulator to an individual in need thereof. Also provided are methods of enhancing the activity of a serotonin reuptake inhibitor (SRI) comprising co-administering a glutamate modulator and a serotonin reuptake inhibitor. Pharmaceutical composition comprising a serotonin reuptake inhibitor and a glutamate modulator are also provided.Type: GrantFiled: July 10, 2018Date of Patent: January 17, 2023Assignee: YALE UNIVERSITYInventors: Vladimir Coric, John H. Krystal, Gerard Sanacora
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Patent number: 11547700Abstract: The present invention describes the use of a 5HT3-antagonist, in combination with a 6-propylamino-4,5,6,7-tetrahydro-1,3-benzothiazole-2-amine, to reduce adverse effects and to facilitate the neuroprotective treatment of a patient suffering from a synucleinopathic disorder to enable a therapeutically effective 6-propylamino-4,5,6,7-tetrahydro-1,3-benzothiazole-2-amine daily dose without the dose-limiting adverse effects caused by pramipexole when administered alone.Type: GrantFiled: August 31, 2020Date of Patent: January 10, 2023Assignee: CHASE THERAPEUTICS CORPORATIONInventors: Thomas N. Chase, Kathleen E. Clarence-Smith
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Patent number: 11504380Abstract: The invention relates to a method of treating cirrhosis which comprises administering to a subject in need thereof lanifibranor or a deuterated derivative thereof.Type: GrantFiled: November 8, 2019Date of Patent: November 22, 2022Assignee: INVENTIVAInventors: Guillaume Wettstein, Pierre Broqua, Jean-Louis Junien
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Patent number: 11400155Abstract: Disclosed are methods of treating cancer using a combination of an immunotherapeutic agent, such as, for example, a PD-1, PD-L1 or CTLA-4 checkpoint inhibitor, and a glutamate modulating agent such as riluzole or trigriluzole. Pharmaceutical compositions including the immunotherapeutic agents and glutamate modulating agents are also disclosed.Type: GrantFiled: May 19, 2017Date of Patent: August 2, 2022Assignee: Biohaven Therapeutics Ltd.Inventor: Vladimir Coric
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Patent number: 11366121Abstract: Research tool assay for identifying a specific modulator of GNAI, compositions and methods of use. The assay includes combining a drug candidate with GNAI and a C-terminal GIV peptide and determining if the drug candidate inhibits GNAI interaction with the C-terminal GIV peptide; and combining the drug candidate with GNAI and a DAPLE peptide and determining if the drug candidate inhibits GNAI interaction with DAPLE peptide. Also provided are compositions and methods of treatment relating to the same.Type: GrantFiled: February 22, 2018Date of Patent: June 21, 2022Assignee: The Regents of the University of CaliforniaInventor: Pradipta Ghosh
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Patent number: 11324740Abstract: A method is provided for using of type-2 dopaminergic receptor agonists, for example, cabergoline, in treatment of eye diseases caused by an elevated level of vascular endothelial growth factor (VEGF), particularly in treatment or prevention of diseases of an eye retina resulting from an increase in permeability of blood vessels and their angiogenesis using cabergoline, a dopaminergic D2 receptor agonist.Type: GrantFiled: March 31, 2020Date of Patent: May 10, 2022Inventor: Maciej Oseka
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Patent number: 11318122Abstract: The present invention describes the combination of a 6-propylamino-4,5,6,7-tetrahydro-1,3-benzothiazole-2-amine or of a pharmaceutically acceptable salt or solvate thereof with fluoxetine or a pharmaceutically acceptable salt or solvate thereof, for use for treating a synucleinopathy such as Parkinson's disease, Lewy body disease, mutations in the glucocerebrosidase gene, or multiple system atrophy.Type: GrantFiled: April 11, 2018Date of Patent: May 3, 2022Assignee: CHASE THERAPEUTICS CORPORATIONInventors: Thomas N. Chase, Kathleen E. Clarence-Smith
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Patent number: 11234961Abstract: In various embodiments, provided herein are pamoate salts of monoamine Anti-Parkinsons disease agents including rotigotine, ropinirole, pramipexole, selegiline, rasagiline, and safinamide, pharmaceutical composition comprising the same, methods of preparing the same, and methods of using the same. For example, the pamoate salt herein can be characterized by a molar ratio of rotigotine, ropinirole, pramipexole, selegiline, rasagiline, or safinamide to pamoic acid of about 1:1 or about 2:1. The pamoate salt herein can also be crystalline including anhydrous, hydrate or solvate forms, or their polymorphs, or amorphous. The pamoate salts described herein can provide a long acting and/or extended release profile of the monoamine agents for the treatment of Parkinsons disease (PD). Thus, also provided herein are methods of preparing a long acting and/or extended release injectable formulation of the monoamine agents using their respective pamoate salts.Type: GrantFiled: August 17, 2018Date of Patent: February 1, 2022Inventor: Zi-Qiang Gu
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Patent number: 10851114Abstract: A compound of formula (I?) wherein R6 is H, C1-6alkyl, —(CH2)pCOOH, —(CH2)pCOOC1-6alkyl, —(CH2)pCONH2, —(CH2)pCONHC1-6alkyl, —(CH2)pCON(C1-6alkyl)2, R7 is as defined for R6; or and R7 taken together with the atoms joining them can form a 6-membered aromatic or non aromatic, saturated or unsaturated, carbocyclic or heteroatom containing (e.g.Type: GrantFiled: December 10, 2018Date of Patent: December 1, 2020Assignee: Avexxin ASInventors: Berit Johansen, Marcel Sandberg, Inger-Reidun Aukrust, George Kokotos, Johan Evenäs, Thomas Brimert, Kildahl-Andersen Geir
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Patent number: 10844026Abstract: Pharmaceutical compositions of the invention include substituted riluzole prodrugs useful for the treatment of cancers including melanoma, breast cancer, brain cancer, and prostate cancer through the release of riluzole. Prodrugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process.Type: GrantFiled: January 21, 2020Date of Patent: November 24, 2020Assignees: Biohaven Pharmaceutical Holding Company Ltd., Rutgers, The State University of New JerseyInventors: Garry Robert Smith, Allen B. Reitz, Mark McDonnell, Suzie Chen, Matthew D. Vera, Benjamin E. Blass, Jeffrey Claude Pelletier, Venkata N. Velvadapu, Jay Edward Wrobel
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Patent number: 10799484Abstract: The present invention describes the use of a 5HT3-antagonist, in combination with a 6-propylamino-4,5,6,7-tetrahydro-1,3-benzothiazole-2-amine, to reduce adverse effects and to facilitate the neuroprotective treatment of a patient suffering from a synucleinopathic disorder to enable a therapeutically effective 6-propylamino-4,5,6,7-tetrahydro-1,3-benzothiazole-2-amine daily dose without the dose-limiting adverse effects caused by pramipexole when administered alone.Type: GrantFiled: March 26, 2018Date of Patent: October 13, 2020Assignee: CHASE THERAPEUTICS CORPORATIONInventors: Thomas N. Chase, Kathleen E. Clarence-Smith
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Patent number: 10774046Abstract: Some embodiments of the invention include inventive compounds. Other embodiments include compositions (e.g., pharmaceutical compositions) comprising the inventive compound. Still other embodiments of the invention include compositions (e.g., pharmaceutical compositions) for treating, for example, certain diseases using the compounds. Some embodiments include methods of using the inventive compound (e.g., in compositions or in pharmaceutical compositions) for administering and treating (e.g., diseases such as cancer). Further embodiments include methods for making the inventive compounds. Other embodiments include PFKFB4 inhibitors and methods of using the same that can target neoplastic cells, including, such as, mechanisms within those cells that relate to the use of the glycolytic pathway. In other embodiments, small molecule PFKFB4 inhibitors are used to disrupt the kinase domain of PFKFB4 and, in some instances, decrease the glucose metabolism and growth of human cancers.Type: GrantFiled: October 25, 2018Date of Patent: September 15, 2020Assignee: UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC.Inventors: Sucheta Telang, Jason Chesney, John O. Trent, Joseph A. Burlison, Nagaraju Miriyala
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Patent number: 10724070Abstract: Stable, constitutively expressed, chromosomal fluorescent transcriptional fusions in bacterial pathogens and methods of using the same to screen candidate compounds for anti-bacterial efficacy.Type: GrantFiled: November 14, 2013Date of Patent: July 28, 2020Assignees: University of Cincinnati, Government of the United States as Represented by the Secretary of the Air ForceInventors: Daniel J. Hassett, Shengchang Su, Thomas J. Lamkin, Roland Saldanha
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Patent number: 10640476Abstract: The present invention relates compounds of Formula (A), as well as their preparation and uses, and further relates pharmaceutical compositions comprising these compounds and their uses as modulators of dysfunctional glutamate transmission. The present invention also relates to uses of the compounds or pharmaceutical compositions in treating or preventing certain neurological and psychiatric disorders and diseases as well as cancer in humans.Type: GrantFiled: September 30, 2019Date of Patent: May 5, 2020Assignee: XW LABORATORIES INC.Inventors: Jia-Ning Xiang, Xuesong Xu, Wei Zhou
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Patent number: 10611730Abstract: Provided herein are compounds of Formula (I), and pharmaceutically acceptable salts, N-oxides, or solvates thereof, Also provided herein are pharmaceutical compositions comprising compounds of Formula (I) and methods of using compounds of Formula (I).Type: GrantFiled: April 28, 2016Date of Patent: April 7, 2020Assignee: Janssen Pharmaceutica NVInventors: Michael K. Ameriks, Suchitra Ravula, Devin M. Swanson, Bradley M. Savall
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Patent number: 10562870Abstract: Pharmaceutical compositions of the invention include substituted riluzole prodrugs useful for the treatment of cancers including melanoma, breast cancer, brain cancer, and prostate cancer through the release of riluzole. Prodrugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process.Type: GrantFiled: August 4, 2017Date of Patent: February 18, 2020Assignee: Biohaven Pharmaceutical Holding Company Ltd.Inventors: Garry Robert Smith, Allen B. Reitz, Mark Mcdonnell, Suzie Chen, Matthew D. Vera, Benjamin E. Blass, Jeffery Claude Pelletier, Venkata N. Velvadapu, Jay Edward Wrobel
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Patent number: 10414760Abstract: The present invention provides compounds having the general structural formula (I) and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving fibrosis and proliferation, and where anti-fibrotic or anti-proliferative activity is beneficial.Type: GrantFiled: November 29, 2016Date of Patent: September 17, 2019Assignee: ANGION BIOMEDICA CORP.Inventors: Bijoy Panicker, Dong Sung Lim, Rama K. Mishra, Lambertus J. W. M. Oehlen, James G. Tarrant, Xiaokang Zhu, Dawoon Jung
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Patent number: 10407600Abstract: The invention relates to a yeast protein extract with adhesive properties, comprising extracts of Rhodotorula rubra, Pichia pastoris and Sacharomyces cerevisiae, which have been deposited. The invention also relates to an adhesive composition for wood panels, comprising the yeast protein extract in equal quantities. The invention further relates to a method for preparing the yeast protein extract. The composition can be used in wood panels.Type: GrantFiled: October 25, 2016Date of Patent: September 10, 2019Assignee: UNIVERSIDAD DEL BIO BIOInventors: Mario A. Núñez, Julio E. Alarcón, Aldo A. Ballerini
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Patent number: 10383858Abstract: The invention relates to the use of a pan-PPAR agonist, or of a pharmaceutical composition containing said agonist, for the treatment of a fibrotic condition.Type: GrantFiled: July 24, 2018Date of Patent: August 20, 2019Assignee: INVENTIVAInventors: Irena Konstantinova, Jean-Michel Luccarini, Jean-Louis Junien, Pierre Broqua
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Patent number: 10357497Abstract: Pharmaceutical compositions of the invention include substituted riluzole pro drugs useful for the treatment of amyotrophic lateral sclerosis (ALS) and related disorders through the release of riluzole, especially to avoid patient to patient variability in first pass, hepatic metabolism promoted by Cyp 1A2. Pro-drugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process. The invention further includes pro-drugs of riluzole useful for the treatment of disease states that can be treated with riluzole through the release of riluzole from a pro-drug agent.Type: GrantFiled: June 24, 2013Date of Patent: July 23, 2019Assignee: Biohaven Pharmaceutical Holding Company LimitedInventors: Allen B. Reitz, Garry R. Smith
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Patent number: 10285981Abstract: A method for treating amyotrophic lateral sclerosis (ALS) in a subject in need thereof comprising administering to said subject an effective amount of (6R)-2-amino-4,5,6,7-tetrahydro-6-(propylamino)benzothiazole or pharmaceutically acceptable salt thereof, wherein said subject is a treatment responder. In certain embodiments, said subject is a subject with definite amyotrophic lateral sclerosis, a subject with amyotrophic lateral sclerosis symptom onset duration of less than about 18 months, a subject with a high level of serum creatinine, a subject with concomitant riluzole administration and combinations thereof.Type: GrantFiled: March 20, 2018Date of Patent: May 14, 2019Assignee: Knopp Biosciences LLCInventors: Michael E. Bozik, Thomas Petzinger, Jr., James L. Mather, Donald Archibald
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Patent number: 10231954Abstract: The present invention provides a compound of formula (I) wherein: Y represents a C or N atom which may be substituted or form a cyclic group with R?? but may not be a quaternary C atom; R? is —OR1, —CONH2, —CF3, F, —OH, —NO2, —CN or —OCOR1 in which R1, is C1-3 alkyl and each may be in the beta or gamma position; R? is C1-3 alkyl or H; and R?? is H or a group consisting of 1-12 non-hydrogen atoms and may be linear, branched and/or incorporate one or more cyclic groups, cyclic groups may be aromatic and/or heterocyclic and 2 or more cyclic groups may be linked or fused and each may be substituted; or a salt, hydrate or solvate of a compound of formula (I) for use in the treatment or prevention of a neurodegenerative disorder by inhibiting formation of neurofibrillary (tau) tangles and/or by inhibiting Dyrk 1A. The invention further relates to non-therapeutic uses of these compounds.Type: GrantFiled: February 4, 2015Date of Patent: March 19, 2019Assignee: LYTIX BIOPHARMA ASInventors: John S. Svendsen, Wenche Stensen, Frederick A. Leeson
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Patent number: 10195213Abstract: Disclosed herein are compounds that are effective for treatment of various disease states associated with senescence. The disclosed compounds can be used to eliminate senescent cells for disease treatment. The dosing of the compounds includes both single administration and regimens of cycling dosages.Type: GrantFiled: March 14, 2016Date of Patent: February 5, 2019Assignee: UNITY BIOTECHNOLOGY, INC.Inventor: Nathaniel David
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Patent number: 10195183Abstract: Disclosed herein are methods of treating conditions, which may be associated with elevated levels of mast cells, basophils, eosinophils, or a combination thereof, with a therapeutically effective amount of dexpramipexole or pharmaceutical acceptable salt thereof.Type: GrantFiled: August 14, 2017Date of Patent: February 5, 2019Assignee: Knopp Biosciences LLCInventors: Michael E Bozik, Steven Dworetzky
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Patent number: 10076528Abstract: This invention relates the use of cortisol blockers (glucocorticoid receptor [GR] antagonists) for the treating or preventing treatment resistant prostate cancer, treating or preventing neoplasia, and treating or preventing infection related to acute or chronic injury or disease.Type: GrantFiled: December 26, 2017Date of Patent: September 18, 2018Assignee: Pop Test Oncology Limited Liability CompanyInventors: Randice Lisa Altschul, Neil David Theise, Myron Rapkin, Rebecca O'Brien
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Patent number: 10052311Abstract: The invention relates to the use of a pan-PPAR agonist, or of a pharmaceutical composition containing said agonist, for the treatment of a fibrotic condition.Type: GrantFiled: June 12, 2015Date of Patent: August 21, 2018Assignee: INVENTIVAInventors: Irena Konstantinova, Jean-Michel Luccarini, Jean-Louis Junien, Pierre Broqua
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Patent number: 9968579Abstract: The present disclosure describes how all-retinoic acid (ATRA) binds and inhibits Pin1 activity and induces degradation of the activated Pin1 monomer selectively in cancer cells. Identification of the binding mechanism of ATRA with Pin1 confirm ATRA binding specificity to Pin1 residues in the PPIase active site, thus demonstrating that drug-induced Pin1 ablation has potent anticancer activity, such as in acute promyelocytic leukemia (APL), by inducing PML-RARa degradation, as well as against other types of cancer and diseases that are associated with Pin1 overexpression, such as aggressive triple negative breast cancer, lupus, asthma, cocaine addiction, among others, due to their unique ability to simultaneously block numerous cancer-driving pathways, with relatively lower toxicity. The present disclosure also provides a rationale for developing sustained released ATRA-containing formulations.Type: GrantFiled: July 16, 2015Date of Patent: May 15, 2018Assignee: Beth Isreal Deaconess Medical Center, Inc.Inventors: Kun Ping Lu, Xiao Zhen Zhou, Shuo Wei
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Patent number: 9956206Abstract: A method for treating amyotrophic lateral sclerosis (ALS) in a subject in need thereof comprising administering to said subject an effective amount of (6R)-2-amino-4,5,6,7-tetrahydro-6-(propylamino)benzothiazole or pharmaceutically acceptable salt thereof, wherein said subject is a treatment responder. In certain embodiments, said subject is a subject with definite amyotrophic lateral sclerosis, a subject with amyotrophic lateral sclerosis symptom onset duration of less than about 18 months, a subject with a high level of serum creatinine, a subject with concomitant riluzole administration and combinations thereof.Type: GrantFiled: April 20, 2017Date of Patent: May 1, 2018Assignee: Knopp Biosciences LLCInventors: Michael E. Bozik, Thomas Petzinger, Jr., James L. Mather, Donald Archibald
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Patent number: 9856252Abstract: Substituted benzimidazole and 3H-imidazo[4,5-b]pyridines or formula I: where X and Y respectively are selected from: (i) N and N; and (ii) N and CR4; A2 is selected from: a C5 heteroarylene group, containing 2 or 3 ring heteroatoms, where the bonds to L1 and the core are ? to one another; L1 is selected from: (i) A1—O—CH2—A2; (ii) A1—CH2—O—A2; (iii) A1—C(?O)—NH—A2; (iv) A1—CH(OH)—A2; (v) A1—CH2—NH—C(?O)—A2; (vi) A1—S—CH2—A2; (vii) A1—CH2—S—A2; (viii) A1—CH2—A2; and (ix) A1—CH(CH3)—O—A2; A1 is phenyl, optionally substituted by F or CF3; their use as pharmaceuticals, and in particular, in treating cancer and hemoglobinopathies.Type: GrantFiled: February 20, 2014Date of Patent: January 2, 2018Assignee: Cancer Therapeutics CRC Pty LtdInventors: Paul Anthony Stupple, Scott Raymond Walker, Jo-Anne Pinson, Helen Rachel Lagiakos, Gillian Elizabeth Lunniss, Ian Peter Holmes, Alexandra Elizabeth Stupple, Ylva Elisabet Bergman, Richard Charles Foitzik, Wilhelmus Johannes Antonius Kersten, Michelle Ang Camerino
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Patent number: 9801893Abstract: Methods are directed to the treatment of subjects with prostate cancer, in particular those with castration resistant prostate cancer, with glucocorticoid receptor antagonists. The prostate cancer may be one that has become resistant to androgen deprivation therapy, for example, by increase in glucocorticoid receptor expression and/or activity.Type: GrantFiled: February 2, 2016Date of Patent: October 31, 2017Assignee: The University of ChicagoInventors: Russell Z. Szmulewitz, Suzanne D. Conzen
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Patent number: 9763918Abstract: Disclosed herein are methods of treating conditions, which may be associated with elevated levels of mast cells, basophils, eosinophils, or a combination thereof, with a therapeutically effective amount of dexpramipexole or pharmaceutical acceptable salt thereof.Type: GrantFiled: August 13, 2014Date of Patent: September 19, 2017Assignee: Knopp Biosciences LLCInventors: Michael E. Bozik, Steven Dworetzky
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Patent number: 9725427Abstract: Pharmaceutical compositions of the invention include substituted riluzole prodrugs useful for the treatment of cancers including melanoma, breast cancer, brain cancer, and prostate cancer through the release of riluzole. Prodrugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process.Type: GrantFiled: March 15, 2013Date of Patent: August 8, 2017Assignees: Biohaven Pharmaceutical Holding Company Limited, Rutgers, The State University of New JerseyInventors: Garry R. Smith, Allen B. Reitz, Mark McDonnell, Suzie Chen, Matthew D. Vera, Benjamin E. Blass, Jeffery C. Pelletier, Venkata N. Velvadapu, Jay E. Wrobel
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Patent number: 9675591Abstract: The present invention provides methods for treating seizure disorders. The method includes administering to a subject in need thereof 2-amino-6-trifluoromethylthio-benzothiazole, or a pharmaceutically acceptable salt thereof. Methods for the treatment of pain are also described.Type: GrantFiled: April 15, 2016Date of Patent: June 13, 2017Assignee: The Regents of the University of CaliforniaInventors: Heike Wulff, Nichole Coleman, David Paul Jenkins
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Patent number: 9662313Abstract: A method for treating amyotrophic lateral sclerosis (ALS) in a subject in need thereof comprising administering to said subject an effective amount of (6R)-2-amino-4,5,6,7-tetrahydro-6-(propylamino)benzothiazole or pharmaceutically acceptable salt thereof, wherein said subject is a treatment responder. In certain embodiments, said subject is a subject with definite amyotrophic lateral sclerosis, a subject with amyotrophic lateral sclerosis symptom onset duration of less than about 18 months, a subject with a high level of serum creatinine, a subject with concomitant riluzole administration and combinations thereof.Type: GrantFiled: February 28, 2014Date of Patent: May 30, 2017Assignee: Knopp Biosciences LLCInventors: Michael E. Bozik, Thomas Petzinger, Jr., James L. Mather, Donald Archibald
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Patent number: 9648877Abstract: The present invention provides a method for increasing tolerance to abiotic stress and/or reducing the consequence of abiotic stress in a plant or part thereof comprising contacting a plant or part thereof with a composition comprising an effective amount of dicarboxylic acid or derivative thereof.Type: GrantFiled: August 25, 2014Date of Patent: May 16, 2017Assignee: Crop Microclimate Management Inc.Inventor: Charles Christian Kupatt
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Patent number: 9642840Abstract: Disclosed herein are methods of treating conditions, which may be associated with elevated levels of plasma cells and/or B-cells, with a therapeutically effective amount of dexpramipexole or pharmaceutical acceptable salt thereof.Type: GrantFiled: August 13, 2014Date of Patent: May 9, 2017Assignee: Knopp Biosciences, LLCInventors: Michael E. Bozik, Steven Dworetzky
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Patent number: 9623012Abstract: The present invention relates to a pharmaceutical composition in solid oral dosage form comprising (R)-7-(2-(1-(4-butoxyphenyl)-2-methylpropan-2-ylamino)-1-hydroxyethyl)-5-hydroxybenzo[d]thiazol-2(3H)-one acetate salt.Type: GrantFiled: February 26, 2014Date of Patent: April 18, 2017Assignee: NOVARTIS AGInventors: Miloud Achour, Robin Alec Fairhurst, Arnaud Grandeury, Shinji Hatakeyama, Magdalena Koziczak-Holbro, Nicola Tufilli, Thomas Ullrich
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Patent number: 9512096Abstract: The present invention is related to an improved process for the preparation of amino-substituted 4,5,6,7-tetrahydrobenzothiazole compounds of formula I, such as the compound 2-amino-4,5,6,7-tetrahydro-6-(n-propylamino)benzothiazole. The invention further relates to an improved synthesis of (R)-2-amino-4,5,6,7-tetrahydro-6-(n-propylamino)benzothiazole. The invention also relates to the methods and intermediates associated with the synthetic process.Type: GrantFiled: December 21, 2012Date of Patent: December 6, 2016Assignee: Knopp Biosciences, LLPInventors: Weirong Chen, Michael Humora, Daw-long Albert Kwok, William F. Kiesman, Erwin Ayandra Irdam
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Patent number: RE47404Abstract: The present disclosure relates to methods for treating viral hepatitis, compounds useful in the treatment of viral hepatitis, and pharmaceutical compositions comprising such compounds. In one embodiment, pharmaceutical compositions comprising nitazoxanide, tizoxanide, or derivatives and/or mixtures thereof are provided, as well as methods of treating hepatitis C using such compositions.Type: GrantFiled: July 7, 2017Date of Patent: May 28, 2019Assignee: ROMARK LABORATORIES, L.C.Inventor: Jean-Francois Rossignol