Tricyclo Ring System Having The Five-membered Hetero Ring As One Of The Cyclos Patents (Class 514/411)
  • Patent number: 11458121
    Abstract: Disclosed herein are compounds of formula I: or a salt thereof and compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods for treating or preventing a bacterial infection in an animal comprising administering to the animal a compound of formula I or a pharmaceutically acceptable salt thereof, alone or in combination with a bacterial efflux pump inhibitor.
    Type: Grant
    Filed: June 26, 2018
    Date of Patent: October 4, 2022
    Assignee: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY
    Inventors: Edmond J. LaVoie, Ajit Parhi, Hye Yeon Sagong
  • Patent number: 11414422
    Abstract: 1-(3,4-Dihydro-1H-pyrido[4, 3-b]indol-2(5H)-yl)-2-hydroxyethanones are disclosed. The compounds are inhibitors of human cGAS in interferon-producing cell types. They are thus useful as therapeutic agents for treating cGAS-related autoimmune diseases in humans.
    Type: Grant
    Filed: February 5, 2019
    Date of Patent: August 16, 2022
    Assignee: The Rockefeller University
    Inventors: Lodoe Lama, Thomas Tuschl, Daisuke Tomita, Dinshaw Patel, J. Fraser Glickman, Taku Kamei, Michael Miller, Yasutomi Asano, Rei Okamoto, Shogo Hashizume, Jumpei Aida, Toshihiro Imaeda, Mayako Michino, Takanobu Kuroita
  • Patent number: 11414423
    Abstract: The present invention provides substituted 1,2,3,4,5,6-hexahydroazepino[4,5-b]indoles and methods of using the compounds for treating brain disorders.
    Type: Grant
    Filed: June 11, 2021
    Date of Patent: August 16, 2022
    Assignee: The Regents of the University of California
    Inventors: David E. Olson, Florence Wagner
  • Patent number: 11400075
    Abstract: The invention includes an amount of (3aR)-1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indol-5-yl phenylcarbamate for administering to a subject and also a method of preventing or treating neurotoxicity or neurodegenerative processes in a subject in need thereof using the amount thereof.
    Type: Grant
    Filed: August 17, 2020
    Date of Patent: August 2, 2022
    Assignee: ANNOVIS BIO, INC.
    Inventor: Maria Maccecchini
  • Patent number: 11382893
    Abstract: The invention includes an amount of (3aR)-1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indol-5-yl phenylcarbamate for administering to a subject and also a method of preventing or treating neurotoxicity or neurodegenerative processes in a subject in need thereof using the amount thereof.
    Type: Grant
    Filed: August 17, 2020
    Date of Patent: July 12, 2022
    Assignee: ANNOVIS BIO, INC.
    Inventor: Maria Maccecchini
  • Patent number: 11376238
    Abstract: The invention includes an amount of (3aR)-1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indol-5-yl phenylcarbamate for administering to a subject and also a method of preventing or treating neurotoxicity or neurodegenerative processes in a subject in need thereof using the amount thereof.
    Type: Grant
    Filed: August 17, 2020
    Date of Patent: July 5, 2022
    Assignee: ANNOVIS BIO, INC.
    Inventor: Maria Maccecchini
  • Patent number: 11325888
    Abstract: The present invention relates to a method for the synthesis of compounds useful in the preparation of antibody drug conjugates (ADC), namely, monoprotected dimeric bifunctional prodrugs based on duocarmycin analogs. In a further aspect, compounds obtained by the method according to the present invention are provided. The monoprotected bifunctional prodrug is used for preparing antibody drug conjugates composed of an antibody moiety and the monoprotected bifunctional prodrug. The antibody compound conjugates thus obtained are provided. Further, a method of preparing an antibody drug conjugate composed of two identical or two different antibody moieties is provided as well as the antibody compound conjugate containing two different antibody moieties accordingly. These conjugates can be used in pharmaceutical compositions, in particular, for use in treatment of tumors, e.g. for use in ADC therapy.
    Type: Grant
    Filed: August 10, 2018
    Date of Patent: May 10, 2022
    Assignee: Georg-August-Universitaet Goettingen Stiftung Oeffentlichen Rechts
    Inventor: Lutz F. Tietze
  • Patent number: 11252953
    Abstract: The combination of a repellent agent or an attractant agent with a wavelength-specific visual cue agent has been found to produce an unexpected and synergistic effect of increased repellency or attraction in dichromatic animals who are not maximally sensitive to the wavelength of the repellent or attractant agent. The method of the invention may be used to repel dichromatic-animal pests; or to prevent or minimize monetary damage, particularly to agricultural products, natural resources or private property. The method of the invention may also be used to attract dichromatic animals for the purpose of agricultural production, recreational opportunities (e.g., wild-rodent feeders), or the effective administration of target-animal pharmaceuticals or mitigation techniques.
    Type: Grant
    Filed: March 30, 2020
    Date of Patent: February 22, 2022
    Assignees: Arkion Life Sciences, LLC, United States of America, as Represented by the Secretary of Agriculture
    Inventors: Scott J. Werner, Kenneth E. Ballinger, Jr.
  • Patent number: 11234944
    Abstract: The invention relates to pharmaceutical compositions comprising a statin and a cannabinoid, and their use for the treatment of hypercholesterolemia and atherosclerosis. It has been found that compositions combining a statin and a cannabinoid are improved over existing statin formulations. The compositions of the invention for example allow for a lower effective dose of statin and a reduction of the adverse effects seen with statins taken alone. Dosing ranges and formulations suitable for oral, buccal, and sublingual administration are disclosed. Various specific cannabinoids such as cannabidiol and synthetic cannabidiols selected for their anti-inflammatory, antioxidant, and anti-atherosclerotic effect are shown to be particularly advantageous.
    Type: Grant
    Filed: October 20, 2020
    Date of Patent: February 1, 2022
    Assignee: Indication BioScience LLC
    Inventors: James Smeeding, Mathew Sherwood
  • Patent number: 11149003
    Abstract: It is described an industrially viable and advantageous process for the preparation of (S)-beta-aminosulfone (1) starting from the corresponding racemic compound, said (S)-beta-aminosulfone being a useful intermediate for the preparation of N-(2-((1S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl)acetamide, also known as Apremilast, the latter being suitable for use in methods of treating, preventing and/or managing psoriasis or psoriatic arthritis.
    Type: Grant
    Filed: March 28, 2018
    Date of Patent: October 19, 2021
    Assignee: Quimica Sintetica, S.A.
    Inventors: Giuseppe Barreca, Giovanni Marras, Bruno Romanò
  • Patent number: 11104646
    Abstract: Small molecule carbazole compounds for use as androgen receptor inhibitors are provided herein. Also provided herein are methods for using the carbazole compounds in treating prostate cancer, including castration-resistant prostate cancer and enzalutamide-resistant prostate cancer. The methods include administering to a subject an effective amount of a compound or composition as described herein.
    Type: Grant
    Filed: October 23, 2019
    Date of Patent: August 31, 2021
    Assignee: GEORGETOWN UNIVERSITY
    Inventors: Milton L. Brown, Shujie Hou, Partha Banerjee, Karishma Amin
  • Patent number: 11046689
    Abstract: The specification relates to compounds of Formula (I): and to pharmaceutically acceptable salts thereof, to processes and intermediates used for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of cell proliferative disorders.
    Type: Grant
    Filed: January 29, 2020
    Date of Patent: June 29, 2021
    Assignee: AstraZeneca AB
    Inventors: Johannes Wilhelmus Maria Nissink, James Stewart Scott, Thomas Andrew Moss, Samantha Jayne Hughes, Bernard Christophe Barlaam, Bin Yang
  • Patent number: 11007178
    Abstract: Described herein are methods and uses of Nampt activators for treatment of cardiovascular diseases and disorders, and/or diabetes, symptoms thereof, and complications associated with diabetes.
    Type: Grant
    Filed: March 17, 2017
    Date of Patent: May 18, 2021
    Assignee: University of South Florida
    Inventors: Srinivas M. Tipparaju, Sachin L. Badole, Kalyan C. Chapalamadugu, Jared Tur
  • Patent number: 10933050
    Abstract: Polymorph forms of 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide are disclosed as well as their methods of synthesis and pharmaceutical compositions.
    Type: Grant
    Filed: July 24, 2019
    Date of Patent: March 2, 2021
    Assignee: SIGA TECHNOLOGIES INC.
    Inventors: Shanthakumar R. Tyavanagimatt, Melialani A. C. L. S. Anderson, William C. Weimers, Dylan Nelson, Tove′ C. Bolken, Dennis E. Hruby, Michael H. O'Neill, Gary Sweetapple, Kelley A. McCloughan
  • Patent number: 10919855
    Abstract: An alternative and improved process for the preparation of Apremilast (Formula I) and Apremilast form B or a pharmaceutically acceptable salt thereof is provided. The novel process includes hydrogenation in acetone, Cyclization and acetylation followed by condensation in methyl isobutyl ketone (MIBK) and acetic acid mixture in specific volume ratios.
    Type: Grant
    Filed: April 27, 2018
    Date of Patent: February 16, 2021
    Assignee: UNICHEM LABORATORIES LTD
    Inventors: Dhananjay G. Sathe, Arijit Das, Bhavesh B. Patel, Dipak Subhash Patil, Ashok Govind Matale, Eknath Kamalakar Kshirsagar
  • Patent number: 10849881
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, Y and R2 are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Grant
    Filed: June 4, 2018
    Date of Patent: December 1, 2020
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Patrizio Mattei, Daniel Hunziker, Patrick Di Giorgio, Jerome Hert, Markus Rudolph, Lisha Wang
  • Patent number: 10835501
    Abstract: The invention relates to pharmaceutical compositions comprising a statin and a cannabinoid, and their use for the treatment of hypercholesterolemia and atherosclerosis. It has been found that compositions combining a statin and a cannabinoid are improved over existing statin formulations. The compositions of the invention for example allow for a lower effective dose of statin and a reduction of the adverse effects seen with statins taken alone. Dosing ranges and formulations suitable for oral, buccal, and sublingual administration are disclosed. Various specific cannabinoids such as cannabidiol and synthetic cannabidiols selected for their anti-inflammatory, antioxidant, and anti-atherosclerotic effect are shown to be particularly advantageous.
    Type: Grant
    Filed: October 1, 2017
    Date of Patent: November 17, 2020
    Assignee: Indication BioScience LLC
    Inventors: James Smeeding, Mathew Sherwood
  • Patent number: 10799478
    Abstract: The present invention provides a method of treating symptoms associated with Androgen Deprivation Therapy comprising administering to a patient in need of such treatment an effective amount of a compound of Formula I: or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 11, 2018
    Date of Patent: October 13, 2020
    Assignee: Eli Lilly and Company
    Inventors: Rachel Nicole Richey, Hannah Yu
  • Patent number: 10786466
    Abstract: The present invention includes a low dose and sustained release formulation of 2,4-dinitrophenol (DNP). The compositions of the invention are useful for preventing or treating a disease or disorder, such as non-alcoholic fatty liver disease, non-alcoholic steatohepatitis, insulin resistance and/or diabetes, in a subject in need thereof.
    Type: Grant
    Filed: August 29, 2014
    Date of Patent: September 29, 2020
    Assignee: Yale University
    Inventors: Gerald I. Shulman, Rachel Jamison Perry
  • Patent number: 10758515
    Abstract: The present invention provides a method of treating symptoms associated with Androgen Deprivation Therapy comprising administering to a patient in need of such treatment an effective amount of a compound of Formula I or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: September 8, 2015
    Date of Patent: September 1, 2020
    Assignee: Eli Lilly and Company
    Inventor: Charles Thomas Benson
  • Patent number: 10676435
    Abstract: The present invention relates to, inter alia, a novel crystalline free-plate habit or morphology, processes for preparing the crystalline free-plate habit, and uses of the crystalline free-plate habit of the L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl)acetic acid (Compound 1) in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in the vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development, and atherosclerosis).
    Type: Grant
    Filed: April 9, 2019
    Date of Patent: June 9, 2020
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Anthony C. Blackburn, Ryan O. Castro, Mark Allen Hadd, You-An Ma, Antonio Garrido Montalban, Jaimie Karyn Rueter, Lee Alani Selvey, Sagar Raj Shakya, Marlon Carlos
  • Patent number: 10493169
    Abstract: The present invention relates to a method for detecting renal disease and for assessing the efficacy of dialysis treatment using imaging agents having desirable in vivo properties.
    Type: Grant
    Filed: June 26, 2017
    Date of Patent: December 3, 2019
    Assignees: Beth Israel Deaconess Medical Center, Georgia State University Research Foundation Inc.
    Inventor: John V. Frangioni
  • Patent number: 10487056
    Abstract: Small molecule carbazole compounds for use as androgen receptor inhibitors are provided herein. Also provided herein are methods for using the carbazole compounds in treating prostate cancer, including castration-resistant prostate cancer and enzalutamide-resistant prostate cancer. The methods include administering to a subject an effective amount of a compound or composition as described herein.
    Type: Grant
    Filed: November 7, 2018
    Date of Patent: November 26, 2019
    Assignee: Georgetown University
    Inventors: Milton L. Brown, Shujie Hou, Partha Banerjee, Karishma Amin
  • Patent number: 10485806
    Abstract: The present invention relates to aryl analogs, pharmaceutical compositions containing them and their use as NRF2 regulators.
    Type: Grant
    Filed: April 4, 2019
    Date of Patent: November 26, 2019
    Assignees: GlaxoSmithKline Intellectual Property Development Limited, Astex Therapeutics Limited
    Inventors: Jeffrey K. Kerns, James Francis Callahan, Hongxing Yan, Thomas Daniel Heightman, Jeffrey Charles Boehm, Alison Jo-Anne Woolford
  • Patent number: 10406137
    Abstract: Polymorph forms of 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide are disclosed as well as their methods of synthesis and pharmaceutical compositions.
    Type: Grant
    Filed: July 2, 2018
    Date of Patent: September 10, 2019
    Assignee: Siga Technologies Inc.
    Inventors: Shanthakumar R. Tyavanagimatt, Melialani A.C.L.S. Anderson, William C. Weimers, Dylan Nelson, Tove′ C. Bolken, Dennis E. Hruby, Michael H. O'Neill, Gary Sweetapple, Kelley A. McCloughan
  • Patent number: 10383851
    Abstract: The invention includes an amount of (3aR)-1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indol-5-yl phenylcarbamate for administering to a subject and also a method of preventing or treating neurotoxicity or neurodegenerative processes in a subject in need thereof using the amount thereof.
    Type: Grant
    Filed: March 6, 2017
    Date of Patent: August 20, 2019
    Assignee: QR PHARMA, INC.
    Inventor: Maria Maccecchini
  • Patent number: 10370329
    Abstract: A process for the resolution of racemic 2-(3-ethoxy-4-methoxyphenyl)-1-(methylsulphonyl)-eth-2-ylamine using novel chiral salts is disclosed. An L-phenylalanine p-toluene-sulfonamide salt of (S)-2-(3-ethoxy-4-methoxyphenyl)-1-(methylsulphonyl)-eth-2-ylamine and a di-p-toluoyl-L-tartaric acid salt of (S)-2-(3-ethoxy-4-methoxyphenyl)-1-(methylsulphonyl)-eth-2-ylamine are also provided.
    Type: Grant
    Filed: April 22, 2016
    Date of Patent: August 6, 2019
    Inventors: Ramesh Dandala, Sureshbabu Jayachandra, Vipin Kumar Kaushik, Nageshwara Rao Achanta, Sivaprasad Dorasala
  • Patent number: 10370385
    Abstract: Compounds that inhibit digestion in blood-ingesting pests are described herein. In one embodiment, the compounds described herein block entry of blood into the midgut and thereby inhibit digestion and nutrient processing. In another embodiment, the compounds described herein prevent pathogens contained in the blood meal from entering the midgut where they could cross the epithelial cell layer and infect the mosquito. The compounds can be administered to a population of blood-ingesting pests, such as mosquitos, directly or indirectly in an effective amount to prevent mosquitoes from transmitting diseases such as malaria, dengue fever, West Nile virus and lymphatic filariasis. Preferably, the compounds are lethal to blood-ingesting pests. The compounds can be combined with one or more excipients to prepare compositions.
    Type: Grant
    Filed: July 10, 2015
    Date of Patent: August 6, 2019
    Assignee: Arizona Board of Regents on Behalf of the University of Arizona
    Inventors: Jon Njardarson, Jun Isoe, Roger Miesfeld
  • Patent number: 10328052
    Abstract: The present invention relates to the compound ((2R,2?R)-bis(((tetrahydro-2H-pyran-4-carbonyl)oxy)methyl) 1,1?-adipoylbis(pyrrolidine-2-carboxylate), pharmaceutical compositions comprising the same and the use of the same for treatment of diseases or disorders wherein depletion of serum amyloid P component (SAP) would be beneficial, including amyloidosis, Alzheimer's disease, type 2 diabetes mellitus and osteoarthritis.
    Type: Grant
    Filed: October 25, 2016
    Date of Patent: June 25, 2019
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Alexis Denis, Olivier Mirguet, Jérôme Toum
  • Patent number: 10301262
    Abstract: The present invention relates to, inter alia, a novel crystalline free-plate habit or morphology, processes for preparing the crystalline free-plate habit, and uses of the crystalline free-plate habit of the L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl)acetic acid (Compound 1) in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in the vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development, and atherosclerosis).
    Type: Grant
    Filed: June 21, 2016
    Date of Patent: May 28, 2019
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Anthony C. Blackburn, Ryan O. Castro, Mark Allen Hadd, You-An Ma, Antonio Garrido Montalban, Jaimie Karyn Rueter, Lee Alani Selvey, Sagar Raj Shakya, Marlon Carlos
  • Patent number: 10272095
    Abstract: The present invention relates to aryl analogs, pharmaceutical compositions containing them and their use as NRF2 regulators.
    Type: Grant
    Filed: June 15, 2016
    Date of Patent: April 30, 2019
    Assignees: GlaxoSmithKline Intellectual Propert Development Limited, Astex Therapeutics, Limited
    Inventors: Jeffrey K. Kerns, James Francis Callahan, Hongxing Yan, Thomas Daniel Heightman, Jeffrey Charles Boehm, Alison Jo-Anne Woolford
  • Patent number: 10183970
    Abstract: The present invention provides one or more compounds of formula (I) for conjugation to small molecules, polymers, peptides, proteins, antibodies, antibody fragments etc.
    Type: Grant
    Filed: January 28, 2015
    Date of Patent: January 22, 2019
    Assignee: Tube Pharmaceuticals GmbH
    Inventor: Wolfgang Richter
  • Patent number: 10173978
    Abstract: Small molecule carbazole compounds for use as androgen receptor inhibitors are provided herein. Also provided herein are methods for using the carbazole compounds in treating prostate cancer, including castration-resistant prostate cancer and enzalutamide-resistant prostate cancer. The methods include administering to a subject an effective amount of a compound or composition as described herein.
    Type: Grant
    Filed: August 2, 2016
    Date of Patent: January 8, 2019
    Assignee: Georgetown University
    Inventors: Milton L. Brown, Shujie Hou, Partha Banerjee, Karishma Amin
  • Patent number: 10111850
    Abstract: Pharmaceutical compositions comprising an ester anesthetic and a cholinesterase inhibitor have been found to exhibit surprising and beneficial results in achieving a long-acting nerve block for example when administered to an interfascial plane or a peri-neural location in a subject. Such pharmaceutical compositions may also contain an amide anesthetic. Pharmaceutical compositions and methods of using such compositions as described herein provide a surprising and unexpected duration of pain control and a reduced need for the use of narcotics.
    Type: Grant
    Filed: December 1, 2015
    Date of Patent: October 30, 2018
    Inventor: Samuel Wilson
  • Patent number: 10100331
    Abstract: The present invention relates to a composition for transfecting a cell with a genetic material comprising a first agent capable of directing the genetic material away from the acidic compartments in the cell and a second agent capable of stabilizing the microtubule or a network thereof. The invention also relates to the use of the composition in the manufacture of a medicament for treating a disease, a method for delivering a genetic material into a cell and a kit.
    Type: Grant
    Filed: October 29, 2013
    Date of Patent: October 16, 2018
    Assignee: Agency for Science, Technology and Research
    Inventors: Heng-Phon Too, Yoon Khei Ho, Lihan Zhou
  • Patent number: 10092510
    Abstract: The invention relates to a method of inducing emesis in animals, particularly companion animals such as dogs and cats, in situations where vomiting is desired. The method comprises administering an eye drop composition comprising a selective D2 family dopamine agonist as an active ingredient to the eye of the animal to induce emesis. The method and the composition are useful in situations involving ingestion of a potentially toxic substance or foreign body by the animal.
    Type: Grant
    Filed: September 29, 2014
    Date of Patent: October 9, 2018
    Assignee: ORION CORPORATION
    Inventors: Jouko Levijoki, Lasse Saloranta, Johanna Kokkonen
  • Patent number: 10045964
    Abstract: Polymorph forms of 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide are disclosed as well as their methods of synthesis and pharmaceutical compositions.
    Type: Grant
    Filed: July 27, 2017
    Date of Patent: August 14, 2018
    Assignee: Siga Technologies Inc.
    Inventors: Shanthakumar R. Tyavanagimatt, Melialani A. C. L. S. Anderson, William C. Weimers, Dylan Nelson, Tove' C. Bolken, Dennis E. Hruby, Michael H. O'Neill, Gary Sweetapple, Kelley A. McCloughan
  • Patent number: 10005759
    Abstract: The subject matter herein is directed to carbazole-containing amide, carbamate, and urea derivatives and pharmaceutically acceptable salts or hydrates thereof of structural formula I wherein the variable R1, R2, R3, R4, R5, R6, R7, A, D, E, G, J, L, M, Q, a, and b are accordingly described. Also provided are pharmaceutical compositions containing the compounds of formula I to treat a Cry-mediated disease or disorder, such as diabetes, complications associated with diabetes, Cushing's syndrome, NASH, NAFLD, asthma, and COPD.
    Type: Grant
    Filed: April 6, 2015
    Date of Patent: June 26, 2018
    Assignee: Reset Therapeutics, Inc.
    Inventors: Ross Bersot, Paul Humphries
  • Patent number: 9994524
    Abstract: The T cells specific to human collagen type II, one of the possible autoantigens, have a crucial role in the development of rheumatoid arthritis in the context of HLA-DR4. The protein-protein interactions between the T cell receptor (TCR) and the type II collagen linked to the allele MHC of class II HLA-DR4 may thus represent the target for the development of new drugs against rheumatoid arthritis. Using computational virtual screening techniques, families of pharmacologically active molecules have been identified that interfere with the TCR/collagen II-MHCII interaction. The compounds identified here open up new possibilities in the treatment of rheumatoid arthritis.
    Type: Grant
    Filed: March 24, 2017
    Date of Patent: June 12, 2018
    Assignees: CONSIGLIO NAZIONALE DELLE RICERCHE, UNIVERSITÀ CATTOLICA DEL SACRO CUORE
    Inventors: Maria Cristina De Rosa, Francesco Ria, Bruno Giardina, Gianfranco Ferraccioli, Davide Pirolli, Chiara Nicolo′
  • Patent number: 9834563
    Abstract: The present invention relates to a compound represented by formula (I): and pharmaceutically acceptable salts thereof. The compounds of formula I are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
    Type: Grant
    Filed: December 17, 2014
    Date of Patent: December 5, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: William K. Hagmann, Bing Li, Jason W. Szewczyk, Bowei Wang, Dann Parker, Timothy Blizzard, Hubert Josien, Purakkattle Biju, Harry Chobanian, Candido Gude, Ravi P. Nargund, Barbara Pio, Qun Dang, Linus S. Lin, Bin Hu, Mingxiang Cui, Zhengxia Chen, Meibi Dai, Zaihong Zhang, Ying Lv, Lili Tian
  • Patent number: 9822060
    Abstract: A compound having a group represented by the formula (Ia): wherein R1 represents a C1 to C8 fluorinated alkyl group, R2 represents a group having an optionally substituted C5 to C18 alicyclic hydrocarbon group, and * represents a binding site.
    Type: Grant
    Filed: August 25, 2015
    Date of Patent: November 21, 2017
    Assignee: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Tatsuro Masuyama, Satoshi Yamamoto, Koji Ichikawa
  • Patent number: 9775845
    Abstract: The subject matter herein is directed to carbazole-containing sulfonamide derivatives and pharmaceutically acceptable salts or hydrates thereof of structural formula I wherein the variable R1, R2, R3, R4, R5, R6, R7, A, B, C?, D, E, F, G, H?, a, and b are accordingly described. Also provided are pharmaceutical compositions comprising the compounds of formula I to treat a Cry-mediated disease or disorder, such as diabetes, obesity, metabolic syndrome, Cushing's syndrome, and glaucoma.
    Type: Grant
    Filed: January 12, 2016
    Date of Patent: October 3, 2017
    Assignee: Reset Therapeutics, Inc.
    Inventors: Ross Bersot, Paul Humphries
  • Patent number: 9775830
    Abstract: Novel dihydropyrazole derivatives of formula (I) wherein L, R, R3, R4, R5, R6, R7, X1, X2, X3, X4, Y, m and n have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.
    Type: Grant
    Filed: November 3, 2016
    Date of Patent: October 3, 2017
    Assignee: Merck Patent GmbH
    Inventors: Henry Yu, Thomas E. Richardson, Robert James Foglesong, Lizbeth Celeste Deselm, Andreas Goutopoulos
  • Patent number: 9744154
    Abstract: Polymorph forms of 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide are disclosed as well as their methods of synthesis and pharmaceutical compositions.
    Type: Grant
    Filed: December 4, 2015
    Date of Patent: August 29, 2017
    Assignee: SIGA TECHNOLOGIES, INC.
    Inventors: Shanthakumar R. Tyavanagimatt, Melialani A.C.L.S. Anderson, William C. Weimers, Dylan Nelson, Tove′ C. Bolken, Dennis E. Hruby, Michael H. O'Neill, Gary Sweetapple, Kelley A. McCloughan
  • Patent number: 9701676
    Abstract: Compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like.
    Type: Grant
    Filed: August 23, 2013
    Date of Patent: July 11, 2017
    Assignee: Board of Regents of the University of Texas System
    Inventors: Steven L. McKnight, Andrew A. Pieper, Joseph M. Ready, Enrique Fernandez
  • Patent number: 9642841
    Abstract: The present invention features compositions and methods for treatment of snoring. We describe compositions comprising an antihistamine or a pharmaceutically acceptable salt thereof and one or more dietary supplements or pharmaceutically acceptable salts thereof. The compositions can be administered to a subject suffering from snoring.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: May 9, 2017
    Inventors: James M. Hand, Linda M. Hand
  • Patent number: 9629825
    Abstract: The invention relates to a pharmaceutical composition comprising a first pharmacologically active ingredient selected from (1r,4r)-6?-fluoro-N,N-dimethyl-4-phenyl-4?,9?-dihydro-3?H-spiro[cyclohexane-1,1?-pyrano[3,4,b]indol]-4-amine and the physiologically acceptable salts thereof, and a second pharmacologically active ingredient selected from gabapentinoids and the physiologically acceptable salts thereof.
    Type: Grant
    Filed: March 15, 2016
    Date of Patent: April 25, 2017
    Assignee: Gruenenthal GmbH
    Inventors: Stefanie Frosch, Klaus Linz, Thomas Christoph
  • Patent number: 9462455
    Abstract: Disclosed is a method, performed in a Body Area Network (BAN) enabled media experience device for enabling transmission of a media experience according to a stored, predefined user configuration associated with an identification data, userID, of a BAN enabled communication device, the method comprising: establishing a connection between the BAN enabled media experience device and the BAN enabled communication device by using BAN; retrieving the identification data, userID, of the BAN enabled communication device; retrieving the stored, predefined user configuration associated with the userID of the BAN enabled communication device; and initiating transmission of the media experience by the BAN enabled media experience device according to the stored, predefined user configuration.
    Type: Grant
    Filed: November 11, 2014
    Date of Patent: October 4, 2016
    Assignees: SONY CORPORATION, SONY MOBILE COMMUNICATIONS INC.
    Inventors: Aleksandar Rodzevski, Thomas Bolin, Henrik Bengtsson, Erik Bengtsson, Kristian Tärnhed, Malin Larsson, Ola Thörn
  • Patent number: 9447041
    Abstract: The present invention relates to processes and intermediates useful in the preparation of (R)-2-(7-(4-cyclopentyl-3-(trifluromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid of Formula (I) and salts thereof, an S1P1 receptor modulator that is useful in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development and atherosclerosis).
    Type: Grant
    Filed: September 30, 2015
    Date of Patent: September 20, 2016
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Antonio Garrido Montalban, Daniel J. Buzard, John A. DeMattei, Tawfik Gharbaoui, Stephen R. Johannsen, Ashwin M. Krishnan, Young Mi Kuhlman, You-An Ma, Michael John Martinelli, Suzanne Michiko Sato, Dipanjan Sengupta
  • Patent number: 9393232
    Abstract: Disclosed are substituted 5-(3,5-dimethylisoxazol-4-yl)indoline-2-one compounds, pharmaceutical compositions comprising at least one such 4 substituted 5-(3,5-dimethylisoxazol-4-yl)indoline-2-one compound processes for the preparation thereof, and the use thereof for inhibiting BET family of bromodomains and for treating disorders mediated thereby, such as certain cancers.
    Type: Grant
    Filed: April 14, 2014
    Date of Patent: July 19, 2016
    Assignee: BeiGene, Ltd.
    Inventors: Bo Ren, Changyou Zhou, Hexiang Wang