Polycylo Ring System Having A Ring Nitrogen In The System Patents (Class 514/80)
  • Patent number: 11453689
    Abstract: The present application relates to 3-cyclic amine-indole derivatives of general Formula (I), to processes for their preparation, to compositions comprising them and to their use in activation of a serotonin receptor in a cell, as well as to treating diseases, disorders or conditions by activation of a serotonin receptor in a cell. The diseases, disorders or conditions include, for example, psychosis, mental illnesses, and other neurological diseases, disorders and conditions.
    Type: Grant
    Filed: July 28, 2021
    Date of Patent: September 27, 2022
    Assignee: MINDSET PHARMA INC.
    Inventors: Abdelmalik Slassi, Joseph Araujo
  • Patent number: 11426406
    Abstract: Provided herein are methods of treating a lysosomal storage disorder (LSD) in a subject and methods of promoting lysosomal clearance in one or more cells of a subject.
    Type: Grant
    Filed: February 9, 2018
    Date of Patent: August 30, 2022
    Assignee: GEORGETOWN UNIVERSITY
    Inventor: Charbel Moussa
  • Patent number: 11414393
    Abstract: Aminoalcohol lipidoids are prepared by reacting an amine with an epoxide-terminated compound are described. Methods of preparing aminoalcohol lipidoids from commercially available starting materials are also provided. Aminoalcohol lipidoids may be prepared from racemic or stereochemically pure epoxides. Aminoalcohol lipidoids or salts forms thereof are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the amino moiety of these aminoalcohol lipidoid compounds, they are particularly suited for the delivery of polynucleotides. Complexes, micelles, liposomes or particles containing the inventive lipidoids and polynucleotide have been prepared. The inventive lipidoids may also be used in preparing microparticles for drug delivery. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.
    Type: Grant
    Filed: October 14, 2020
    Date of Patent: August 16, 2022
    Assignee: Massachusetts Institute of Technology
    Inventors: Kerry Peter Mahon, Kevin Thomas Love, Christopher G. Levins, Kathryn Ann Whitehead, Robert S. Langer, Daniel Griffith Anderson
  • Patent number: 11390609
    Abstract: The present invention relates to a Rho-associated protein kinase inhibitor of formula (I), a pharmaceutical composition comprising the same, a preparation method thereof, and a use of the same in preventing or treating a disease mediated by Rho-associated protein kinase (ROCK).
    Type: Grant
    Filed: June 29, 2018
    Date of Patent: July 19, 2022
    Assignee: BEIJING TIDE PHARMACEUTICAL CO., LTD.
    Inventors: Yanping Zhao, Hongjun Wang, Gong Li, Yuanyuan Jiang, Xiang Li, Bin Liu, Weiting Zhong, Kai Liu, Fajie Li, Liying Zhou, Yanan Liu
  • Patent number: 11376239
    Abstract: Provided herein are pharmaceutical combinations comprising (a) a B-Raf inhibitor, or a pharmaceutically acceptable salt thereof, (b) at least one mitogen activated protein kinase (MEK) inhibitor, or a pharmaceutically acceptable salt thereof, and (c) an epidermal growth factor receptor (EGFR) inhibitor or a pharmaceutically acceptable salt thereof; and optionally at least one pharmaceutically acceptable carrier; methods for preparing the pharmaceutical combinations, and the uses of the pharmaceutical combinations in the treatment of proliferative diseases, such as cancer.
    Type: Grant
    Filed: September 24, 2019
    Date of Patent: July 5, 2022
    Assignee: ARRAY BIOPHARMA INC
    Inventors: Giordano Caponigro, Zhu Alexander Cao
  • Patent number: 11332441
    Abstract: Crystalline N-methyl tryptamine derivatives, compositions containing those crystalline forms and their methods of use are disclosed. The crystalline N-methyl tryptamine derivatives according to the invention include crystalline N-methyl-N-propyltryptamine (MPT), crystalline N-methyl-N-isopropyltryptammonium fumarate (MiPT fumarate) and crystalline 4-hydroxy-N-methyl-N-isopropyltryptammonium fumarate monohydrate (HO-MiPT fumarate monohydrate).
    Type: Grant
    Filed: March 23, 2020
    Date of Patent: May 17, 2022
    Assignee: CAAMTECH, INC.
    Inventor: Andrew R. Chadeayne
  • Patent number: 11130749
    Abstract: The present invention relates to a Rho-associated protein kinase inhibitor of formula (I), a pharmaceutical composition comprising the same, a preparation method thereof, and a use of the same in preventing or treating a disease mediated by Rho-associated protein kinase (ROCK).
    Type: Grant
    Filed: June 29, 2018
    Date of Patent: September 28, 2021
    Assignee: BEIJING TIDE PHARMACEUTICAL CO., LTD.
    Inventors: Yanping Zhao, Hongjun Wang, Gong Li, Yuanyuan Jiang, Xiang Li, Bin Liu, Weiting Zhong, Kai Liu, Fajie Li, Liying Zhou, Yanan Liu
  • Patent number: 11078221
    Abstract: Compounds of general formula (I): (Formula I)) wherein R1, Q, R3, R4, R5, R6, R7 and Ar1 are as defined herein are inhibitors of class I histone deacetylases and are of use in the treatment of lysosomal storage disorders, especially Niemann-Pick type C disease, as well as other lysosomal storage disorders, defective autophagy, accumulation of free cholesterol and mycobacterial diseases.
    Type: Grant
    Filed: September 28, 2018
    Date of Patent: August 3, 2021
    Assignee: UNIVERSITY COLLEGE CARDIFF CONSULTANTS LTD
    Inventors: Emyr Lloyd-Evans, Fabrizio Pertusati, Edward James, Emily Maguire, Christopher McGuigan
  • Patent number: 11072618
    Abstract: The present disclosure relates generally to methods and compositions for preventing or arresting cell death and/or inflammation.
    Type: Grant
    Filed: June 7, 2019
    Date of Patent: July 27, 2021
    Assignee: DENALI THERAPEUTICS INC.
    Inventors: Anthony A. Estrada, Jianwen A. Feng, Brian Fox, Cheng Hu, Maksim Osipov, Zachary K. Sweeney, Javier de Vicente Fidalgo, Arun Thottumkara
  • Patent number: 11065250
    Abstract: The present invention relates to solid dosage forms of palbociclib comprising a water-soluble acid. The dosage forms described herein have desirable pharmacokinetic characteristics.
    Type: Grant
    Filed: May 24, 2016
    Date of Patent: July 20, 2021
    Assignee: Pfizer Inc.
    Inventors: Fady Makram Louiz Ibrahim, Matthew Patrick Mullarney, Ravi M. Shanker, Barbara Rodriguez Spong, Jian Wang
  • Patent number: 11034691
    Abstract: The invention provides compounds effective as sphingosine-1-phosphate receptor modulators for treatment of cardiopulmonary diseases, such as hypertension (including malignant hypertension), angina, myocardial infarction, cardiac arrhythmias, congestive heart failure, coronary heart disease, atherosclerosis, angina pectoris, dysrhythmias, cardiomyothopy (including hypertropic cardiomyothopy), heart failure, cardiac arrest, bronchitis, asthma, chronic obstructive pulmonary disease, cystic fibrosis, croup, emphysema, pleurisy, pulmonary fibrosis, pneumonia, pulmonary embolus, pulmonary hypertension, mesothelioma, ventricular conduction abnormalities, complete heart block, adult respiratory distress syndrome, sepsis syndrome, idiopathic pulmonary fibrosis, scleroderma, systemic sclerosis, retroperitoneal fibrosis, prevention of keloid formation, or cirrhosis.
    Type: Grant
    Filed: June 11, 2019
    Date of Patent: June 15, 2021
    Assignee: THE SCRIPPS RESEARCH INSTITUTE
    Inventors: Edward Roberts, Hugh Rosen, Mariangela Urbano, Miguel Guerrero
  • Patent number: 11002524
    Abstract: The present invention discloses a cyclic compound of formula (I) and a process of preparation thereof. The present invention further discloses a process for the preparation of compound of formula (II) preferably Hunanamycin A from compound of formula (I).
    Type: Grant
    Filed: March 30, 2017
    Date of Patent: May 11, 2021
    Assignee: Council of Scientific & Industrial Research
    Inventors: Dumbala Srinivasa Reddy, Rahul Dilip Shingare
  • Patent number: 10987356
    Abstract: The present disclosure provides pharmaceutical compositions including a CDK inhibitor and an HSP90 inhibitor, as well as methods of treating cancer or a tumor in a subject by administering a CDK inhibitor and an HSP90 inhibitor to the subject.
    Type: Grant
    Filed: November 12, 2019
    Date of Patent: April 27, 2021
    Assignee: Institute For Cancer Research
    Inventors: Shuai Zhao, Wafik S. El-Deiry
  • Patent number: 10729706
    Abstract: One or more cannabinoids and/or terpenes in combination with psilocybin and/or psilocin may be used in the prevention or treatment of psychological or brain disorders. The one or more cannabinoids may be taken from the group of cannabidiol (CBD); cannabidiolic acid (CBDA); tetrahydrocannbidivarin (THCV); tetrahydrocannbidivarinin acid (THCVA); cannabichromene (CBC); cannabichromenic acid (CBCA); cannabigerol (CBG) and cannabigerolic acid (CBGA).
    Type: Grant
    Filed: January 18, 2018
    Date of Patent: August 4, 2020
    Assignee: Procare Beheer B.V.
    Inventors: Murat Küçüksen, Ali Neset Küçüksen
  • Patent number: 10730833
    Abstract: Described is a method to make diindolylmethanes and indolyl/pyrrolylmethanes, The method includes the steps of contacting an ether comprising an arylpropargyl moiety and an amine-protected, substituted or unsubstituted aniline moiety with a substituted or unsubstituted indol or a substituted or unsubstituted pyrrole, in the presence of a metal-containing catalyst, for a time and at a temperature to cause an annulation/arylation cascade reaction that yields a diindolylmethane or a indolyl/pyrrolylmethane. The resulting compounds are effective to modulate activity of arylhydrocarbon receptors, to inhibit activity of PCSK9, and to stimulate secretion of glucagon-like peptide 1 in mammals.
    Type: Grant
    Filed: April 5, 2018
    Date of Patent: August 4, 2020
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Weiping Tang, Xiaoxun Li, Dongxu Shu, Gabrielle N. Winston-McPherson
  • Patent number: 10550128
    Abstract: A hydrogenated Diels-Alder adduct of the formula (III) a hydrogenated Diels-Alder adduct of the formula (IV) and a lactone compound of formula (V) are disclosed and described.
    Type: Grant
    Filed: March 4, 2019
    Date of Patent: February 4, 2020
    Assignees: Avantium Knowledge Centre B.V., Stichting Wageningen Research
    Inventors: Jan Cornelis Van Der Waal, Edserd De Jong, Jacco Van Haveren, Shanmugam Thiyagarajan
  • Patent number: 10517883
    Abstract: A method of treating an acute myocardial infarction by administering to an individual an effective amount of a formulation which inhibits and/or depletes phagocytic cells with high specificity, thereby suppressing the inflammatory response that occurs during and following acute myocardial infarction. The formulation comprises an agent which is an intra-cellular inhibitor that is released within the targeted phagocytic cells, specifically macrophage/monocytes, and inhibits and/or destroys the macrophages and/or monocytes, thereby reducing the final zone of infarct and improving cardiac repair and myocardial remodeling. Since macrophages and monocytes possess the unique ability to phagocytose large bodies, the agent is formulated into a specific size such that it can enter cells primarily via phagocytosis. Thus, the specifically sized formulation selectively targets monocytes/macrophages.
    Type: Grant
    Filed: June 27, 2003
    Date of Patent: December 31, 2019
    Assignee: ZULI HOLDINGS LTD.
    Inventors: Haim D. Danenberg, Gershon Golomb, Elazer R. Edelman
  • Patent number: 10512751
    Abstract: Methods of modifying the luminal profile of a body vessel are described. An example method comprises advancing a cannula out of the distal end of a catheter disposed within the lumen of a body vessel of an animal and toward a target site on the wall of the body vessel; passing contrast dye through the cannula toward the target site; simultaneously continuing the advancing and passing until the distal end of the cannula punctures the inner layer of the wall of the body vessel at the target site; and passing a bulking agent through the cannula and into a space between connective tissue layers surrounding the vessel wall at the target site. Medical devices, medical device assemblies, and kits are also described.
    Type: Grant
    Filed: November 21, 2018
    Date of Patent: December 24, 2019
    Assignee: Cook Medical Technologies LLC
    Inventors: John C. Sigmon, Jr., Vihar Surti
  • Patent number: 10478494
    Abstract: Provided herein are combination therapies for the treatment of cancer. In particular, the disclosed methods are directed to treatment of cancer in a patient comprising administering an antibody that blocks the interaction between PD-1 and PD-L1 and an FGFR inhibitor, wherein the antibody that blocks the interaction between PD-1 and PD-L1 and the FGFR inhibitor are administered if one or more FGFR variants are present in a biological sample from the patient.
    Type: Grant
    Filed: March 24, 2016
    Date of Patent: November 19, 2019
    Assignee: ASTEX THERAPEUTICS LTD
    Inventors: Jayaprakash Karkera, Suso Jesus Platero, Raluca Verona, Matthew V. Lorenzi
  • Patent number: 10239869
    Abstract: The present invention relates to sulfonamide compounds Formula (I) wherein the substituents are as described herein, and their use in a medicine for the treatment of diseases, disorders associated with the inhibition of Voltage-gated sodium channels (VGSC) particularly NaV1.7. It further relates to the compounds herein and their pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof useful in treating diseases, disorders, syndromes and/or conditions associated with the inhibition of Voltage-gated sodium channels (VGSC) particularly NaV1.7. The invention also relates to process for the preparation of the compounds of the invention.
    Type: Grant
    Filed: September 3, 2016
    Date of Patent: March 26, 2019
    Assignee: LUPIN LIMITED
    Inventors: Vidya Ramdas, Rajeshkumar Maganlal Loriya, Moloy Banerjee, Pradeep Rangrao Patil, Advait Arun Joshi, Laxmikant Shamlal Datrange, Deepak Sahebrao Walke, Talha Hussain Khan, Amit Kumar Das, Ganesh Navinchandra Gote, Vaibhav Madhukar Kalhapure, Venkata P. Palle, Rajender Kumar Kamboj
  • Patent number: 10189802
    Abstract: Aminoalcohol lipidoids are prepared by reacting an amine with an epoxide-terminated compound are described. Methods of preparing aminoalcohol lipidoids from commercially available starting materials are also provided. Aminoalcohol lipidoids may be prepared from racemic or stereochemically pure epoxides. Aminoalcohol lipidoids or salts forms thereof are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the amino moiety of these aminoalcohol lipidoid compounds, they are particularly suited for the delivery of polynucleotides. Complexes, micelles, liposomes or particles containing the inventive lipidoids and polynucleotide have been prepared. The inventive lipidoids may also be used in preparing microparticles for drug delivery. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.
    Type: Grant
    Filed: January 27, 2017
    Date of Patent: January 29, 2019
    Assignee: Massachusetts Institute of Technology
    Inventors: Kerry Peter Mahon, Kevin Thomas Love, Christopher G. Levins, Kathryn Ann Whitehead, Robert S. Langer, Daniel Griffith Anderson
  • Patent number: 10173027
    Abstract: Methods of modifying the luminal profile of a body vessel are described. An example method comprises advancing a cannula out of the distal end of a catheter disposed within the lumen of a body vessel of an animal and toward a target site on the wall of the body vessel; passing contrast dye through the cannula toward the target site; simultaneously continuing the advancing and passing until the distal end of the cannula punctures the inner layer of the wall of the body vessel at the target site; and passing a bulking agent through the cannula and into a space between connective tissue layers surrounding the vessel wall at the target site. Medical devices, medical device assemblies, and kits are also described.
    Type: Grant
    Filed: October 7, 2016
    Date of Patent: January 8, 2019
    Assignee: Cook Medical Technologies LLC
    Inventors: John C. Sigmon, Jr., Vihar Surti
  • Patent number: 10155749
    Abstract: The present invention relates to compounds of formula (I), or the tautomers or pharmacologically acceptable acid addition salts thereof, characterized by a topological polar surface area value (TPSA) of at least 145, wherein R1, R2, R3, R4, X, and Z? have one of the meanings as defined in the specification, to the use of compounds of formula (I) as a medicament, to pharmaceutical composition comprising at least one compound of formula (I), as well as to medicament combinations containing one or more compounds of formula (I).
    Type: Grant
    Filed: January 7, 2016
    Date of Patent: December 18, 2018
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Armin Heckel, Dieter Hamprecht, Joerg Kley
  • Patent number: 10138213
    Abstract: Provided, in part, is a composition comprising one or more chemical entities of formula I, each of which is a compound of formula I: a pharmaceutically acceptable salt thereof, a solvate thereof, or a solvate of a pharmaceutically acceptable salt thereof, the composition characterized in that greater than a first threshold amount of the total amount of chemical entities of formula I in the composition: are chemical entities of formula I.a, wherein the first threshold amount is 50%; or are chemical entities of formula I.b.1, wherein the first threshold amount is 25%; or are chemical entities of formula I.b.2, wherein the first threshold amount is 25%, wherein the chemical entities of formula I.a, I.b.1, and I.b.2, are described herein, and methods of using such compositions, for example, for the delivery of a polynucleotide in vivo.
    Type: Grant
    Filed: June 24, 2015
    Date of Patent: November 27, 2018
    Assignee: Translate Bio, Inc.
    Inventors: Frank DeRosa, Shrirang Karve, Michael Heartlein
  • Patent number: 10131679
    Abstract: Provided is a compound represented by formula (I) or a pharmacologically acceptable salt thereof: wherein L1 is an optionally substituted C1-6 alkylene group or the like, L2 is a single bond or the like, L3 is a single bond or the like, R1, R2, and R3 are each independently an optionally substituted C1-4 alkyl group or the like, R4 is a hydrogen atom or the like, and R5 is a hydrogen atom or the like.
    Type: Grant
    Filed: October 30, 2015
    Date of Patent: November 20, 2018
    Assignee: UBE INDUSTRIES, LTD.
    Inventors: Yasuhiro Aga, Shigeru Ushiyama, Noriaki Iwase, Shigeyuki Kono, Hidetoshi Sunamoto, Takashi Matsushita, Sayaka Ogi, Masayuki Tanaka, Masaaki Matoyama, Satoshi Umezaki, Yusuke Shiraishi, Kazuhiro Onuma, Masahiro Kojima, Hayato Nishiyama, Tomio Kimura
  • Patent number: 9993492
    Abstract: The present invention refers to a compound selected from the group consisting of a lysophospholipid and a lysophospholipid analog for use in the treatment or prophylaxis of honeybee brood diseases, in particular American foulbrood and European foulbrood. The invention also refers to a diet composition, a sprayable composition, a dipping solution for brood combs, a beeswax composition and liposomal and microsphere- or nanosphere-based compositions, comprising a compound according to the invention, for use in the treatment or prophylaxis of bee brood diseases.
    Type: Grant
    Filed: May 22, 2014
    Date of Patent: June 12, 2018
    Assignee: University of Graz
    Inventors: Wolfgang Schühly, Ulrike Riessberger-Gallé, Javier Hernández-López, Karl Crailsheim
  • Patent number: 9987237
    Abstract: The present invention provides for a method of treating a disease such as cancer, comprising the step of administering to a patient a therapeutically effective amount of an isomer or analog of monoterpene or sesquiterpene (or its derivative), such as an isoperillyl alcohol. The present invention also provides for a method of treating a disease comprising the step of administering to a patient a therapeutically effective amount of a derivative of an isomer or analog of monoterpene or sesquiterpene, such as an isoperillyl alcohol carbamate. The derivative may be an isoperillyl alcohol conjugated with a therapeutic agent such as a chemotherapeutic agent. The route of administration may vary, including inhalation, intranasal, oral, transdermal, intravenous, subcutaneous or intramuscular injection.
    Type: Grant
    Filed: August 24, 2015
    Date of Patent: June 5, 2018
    Assignee: NeOnc Technologies, Inc.
    Inventors: Thomas Chen, Daniel Levin, Satish Pupalli, Daniel Anthony Dickman
  • Patent number: 9981954
    Abstract: The present invention relates to compounds of formula (I) or the tautomers or pharmacologically acceptable acid addition salts thereof, characterized by a topological polar surface area value (TPSA) of at least 145, wherein R1, R2, R3, R4, X, and Z? have one of the meanings as defined in the specification, to the use of compounds of formula (I) as medicaments, to pharmaceutical compositions comprising at least one compound of formula (I), as well as to medicament combinations containing one or more compounds of formula (I). The compounds are ENaC inhibitors useful for the treatment of respiratory diseases and allergic diseases of the airways.
    Type: Grant
    Filed: January 7, 2016
    Date of Patent: May 29, 2018
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Armin Heckel, Sara Frattini, Joerg Kley
  • Patent number: 9867825
    Abstract: A combination of a CDK4/6 inhibitor and a MEK inhibitor for the treatment of diseases such as cancer.
    Type: Grant
    Filed: December 16, 2013
    Date of Patent: January 16, 2018
    Assignee: Novartis AG
    Inventors: Giordano Caponigro, Scott Delach, Shivang Doshi, Thomas Horn-Spirohn, Sunkyu Kim
  • Patent number: 9809609
    Abstract: The present invention provides a benzoazepine compound represented by following general formula (1): or a salt thereof, wherein R represents a hydrogen atom, a hydroxy group optionally protected with a protecting group, etc., R1 represents a hydrogen atom or hydroxy-protecting group, and X represents an oxygen atom or a sulfur atom. The benzoazepine compound of the present invention and salts thereof have high solubility in water, and can be suitably used for injections.
    Type: Grant
    Filed: May 1, 2012
    Date of Patent: November 7, 2017
    Assignee: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Makoto Komatsu, Fumitaka Goto, Yasuhiro Menjo, Keigo Yamada, Takakuni Matsuda, Yusuke Kato
  • Patent number: 9777018
    Abstract: The present invention relates to novel compounds of formula (A) and (B) as modulators of GPR-119, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of GPR-119 mediated diseases or disorders with them.
    Type: Grant
    Filed: August 21, 2015
    Date of Patent: October 3, 2017
    Assignee: RHIZEN PHARMACEUTICALS SA
    Inventors: Dhanapalan Nagarathnam, Swaroop K. Vakkalanka, Srikant Viswanadha, Gayatri S. Merikapudi
  • Patent number: 9732035
    Abstract: Presently provided are indoximod prodrug and salt compounds and pharmaceutical compositions comprising salts and prodrugs of indoximod, that produce enhanced plasma concentration and exposure to indoximod compared to direct administration of indoximod, in patients in need of treatment of immunosuppression mediated by the indoleamine-2,3-dioxygenase pathway, such as patients with cancer or chronic infectious diseases.
    Type: Grant
    Filed: June 2, 2016
    Date of Patent: August 15, 2017
    Assignee: NEWLINK GENETICS CORPORATION
    Inventors: Mario Mautino, Sanjeev Kumar, Firoz Jaipuri, Jesse Waldo, Hima Potturi, Hong Zhuang
  • Patent number: 9730904
    Abstract: A pharmaceutical composition which is different from an existing therapeutic agent of an adult disease, of a biochemical reaction-inhibiting type, and which action mechanism is to improve the basal metabolism, wherein the composition has no side effects, and does not generate drug resistance against adult disease; and a method for preventing/treating an adult disease by using the same.
    Type: Grant
    Filed: May 8, 2015
    Date of Patent: August 15, 2017
    Assignee: SBI Pharmaceuticals Co., Ltd.
    Inventor: Tohru Tanaka
  • Patent number: 9556110
    Abstract: Aminoalcohol lipidoids are prepared by reacting an amine with an epoxide-terminated compound are described. Methods of preparing aminoalcohol lipidoids from commercially available starting materials are also provided. Aminoalcohol lipidoids may be prepared from racemic or stereochemically pure epoxides. Aminoalcohol lipidoids or salts forms thereof are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the amino moiety of these aminoalcohol lipidoid compounds, they are particularly suited for the delivery of polynucleotides. Complexes, micelles, liposomes or particles containing the inventive lipidoids and polynucleotide have been prepared. The inventive lipidoids may also be used in preparing microparticles for drug delivery. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.
    Type: Grant
    Filed: January 16, 2015
    Date of Patent: January 31, 2017
    Assignee: Massachusetts Institute of Technology
    Inventors: Kerry Peter Mahon, Kevin Thomas Love, Christopher G. Levins, Kathryn Ann Whitehead, Robert S. Langer, Daniel Griffith Anderson
  • Patent number: 9481698
    Abstract: The present invention relates to a novel process for preparing ceftaroline fosamil as well as to intermediates of this process.
    Type: Grant
    Filed: September 27, 2013
    Date of Patent: November 1, 2016
    Assignee: Sandoz AG
    Inventors: Hubert Sturm, Josef Wieser
  • Patent number: 9452197
    Abstract: In certain aspects, the present disclosure relates to the insight that a polypeptide comprising a ligand-binding portion of the extracellular domain of activin-like kinase I (ALK1) polypeptide may be used to inhibit angiogenesis in vivo, particularly in mammals suffering angiogenesis-related disorders. In certain aspects, the disclosure demonstrates that antagonists of BMP9 and/or BMP10, ligands for ALK1, may also be used to inhibit angiogenesis in vivo.
    Type: Grant
    Filed: December 27, 2013
    Date of Patent: September 27, 2016
    Assignee: Acceleron Pharma, Inc.
    Inventors: Jasbir Seehra, John Knopf, Robert S. Pearsall, Asya Grinberg, Ravindra Kumar
  • Patent number: 9339029
    Abstract: The present disclosure is directed to hydrazinyl lipidoids, formulations thereof further comprising at least one active agent, as well as methods of delivering the at least one active agent to a target organism.
    Type: Grant
    Filed: September 3, 2015
    Date of Patent: May 17, 2016
    Assignee: Preceres Inc.
    Inventors: Richard Wayne Heidebrecht, Jr., Cheng Zhong
  • Patent number: 9303052
    Abstract: The present invention provides a benzoazepine compound represented by following general formula (1): or a salt thereof, wherein R represents a hydrogen atom, a hydroxy group optionally protected with a protecting group, etc., R1 represents a hydrogen atom or hydroxy-protecting group, and X represents an oxygen atom or a sulfur atom. The benzoazepine compound of the present invention and salts thereof have high solubility in water, and can be suitably used for injections.
    Type: Grant
    Filed: August 12, 2013
    Date of Patent: April 5, 2016
    Assignee: I. OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Makoto Komatsu, Fumitaka Goto, Yasuhiro Menjo, Keigo Yamada, Takakuni Matsuda, Yusuke Kato
  • Patent number: 9238627
    Abstract: The present invention relates to processes for preparing 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxyethyoxy)-amide, processes for preparing crystallized 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxyethyoxy)-amide, and intermediates useful therefore. Also provided herein are pharmaceutical compositions comprising this crystallized compound.
    Type: Grant
    Filed: October 18, 2013
    Date of Patent: January 19, 2016
    Assignees: Array BioPharma, Inc., Novartis AG
    Inventors: Christoph Max Krell, Marian Misun, Daniel Andreas Niederer, Werner Heinz Pachinger, Marie-Christine Wolf, Daniel Zimmermann, Weidong Liu, Peter J. Stengel, Paul Nichols
  • Patent number: 9181286
    Abstract: The present disclosure relates to pantothenate derivatives for the treatment of neurologic disorders (such as pantothenate kinase-associated neurodegeneration), pharmaceutical compositions containing such compounds, and their use in treatment of neurologic disorders.
    Type: Grant
    Filed: January 16, 2014
    Date of Patent: November 10, 2015
    Assignee: Retrophin, Inc.
    Inventors: Andrew Vaino, Marek Biestek, Martin Shkreli
  • Patent number: 9095165
    Abstract: It is to provide a pharmaceutical composition which is different from an existing therapeutic agent of an adult disease, of a biochemical reaction-inhibiting type, and which action mechanism is to improve the basal metabolism, wherein the composition has no side effects, and does not generate drug resistance against adult disease; and a method for preventing/treating an adult disease by using the same.
    Type: Grant
    Filed: October 27, 2009
    Date of Patent: August 4, 2015
    Assignee: SBI Pharmaceuticals Co., Ltd.
    Inventor: Tohru Tanaka
  • Patent number: 9062053
    Abstract: The present invention relates to novel crystalline forms of sodium salt of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide (e.g., NXL-104) thereof. The present invention relates to compositions comprising a crystalline form of sodium salt of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide (e.g., NXL-104) alone or in combination with an antibacterial agent (e.g., ceftaroline fosamil). Processes for the preparation of the crystalline forms and methods of treating bacterial infections by administering the crystalline forms alone or in combination with an antibacterial agent (e.g., ceftaroline fosamil) are also described.
    Type: Grant
    Filed: August 7, 2014
    Date of Patent: June 23, 2015
    Inventors: Mahendra G. Dedhiya, Sisir Bhattacharya, Véronique Ducandas, Alexandre Giuliani, Valérie Ravaux, Alain Bonnet, Alain Priour, Peter Spargo
  • Patent number: 9051317
    Abstract: Azaindoles having inhibitory activity on RSV replication and having the formula I compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.
    Type: Grant
    Filed: December 16, 2011
    Date of Patent: June 9, 2015
    Assignee: JANSSEN SCIENCES IRELAND UC
    Inventors: Ludwig Paul Cooymans, Samuël Dominique Demin, Lili Hu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri, Sandrine Marie Helene Vendeville
  • Publication number: 20150148312
    Abstract: Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, can be used to treat or alleviate pain or related conditions.
    Type: Application
    Filed: January 23, 2015
    Publication date: May 28, 2015
    Inventors: Herriot Tabuteau, Graeme Jones
  • Publication number: 20150148311
    Abstract: Compounds having the following structure (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or prodrug thereof, wherein R1, R2, R3, R4, R8, R9, R10, R11, R12, A1, A2, X, Y and Z are as defined herein. Uses of such compounds as TGR5 antagonists and for treatment of various indications, including Type II diabetes meletus are also provided.
    Type: Application
    Filed: June 20, 2014
    Publication date: May 28, 2015
    Inventors: Jason G. Lewis, Nicholas Reich, Tao Chen, Jeffrey W. Jacobs, Dominique Charmot, Marc Navre, Patricia Finn, Christopher Carreras, Andrew Spencer
  • Publication number: 20150141374
    Abstract: Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, can be used to treat or alleviate pain or related conditions.
    Type: Application
    Filed: January 28, 2015
    Publication date: May 21, 2015
    Inventors: Herriot Tabuteau, Graeme Jones
  • Publication number: 20150141373
    Abstract: Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, can be used to treat or alleviate pain or related conditions.
    Type: Application
    Filed: January 28, 2015
    Publication date: May 21, 2015
    Inventors: Herriot Tabuteau, Graeme Jones
  • Publication number: 20150133403
    Abstract: Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, can be used to treat or alleviate pain or related conditions.
    Type: Application
    Filed: January 26, 2015
    Publication date: May 14, 2015
    Inventors: Herriot Tabuteau, Graeme Jones
  • Publication number: 20150126477
    Abstract: Provided are certain methods useful in the treatment of cancer comprising administering a compound of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor;
    Type: Application
    Filed: February 24, 2012
    Publication date: May 7, 2015
    Inventors: Jayant Thatte, Anthony C. Blackburn, Sangdon Han, Robert M. Jones, Jae-Kyu Jung, Antonio Garrido Montalban, Biman B. Pal, Jaimie Karyn Rueter, Sonja Strah-Pleynet, Lars Thoresen, Yifeng Xiong, Dawei Yue, Xiuwen Zhu
  • Patent number: 9018191
    Abstract: Quinazoline derivatives of formula (I): wherein A is 5-membered heteroaryl containing a nitrogen atom and one or two further nitrogen atoms; compositions containing them, processes for their preparation and their use in therapy.
    Type: Grant
    Filed: August 21, 2012
    Date of Patent: April 28, 2015
    Assignee: AstraZeneca AB
    Inventors: Nicola Murdoch Heron, Andrew Austen Mortlock, Frederic Henri Jung, Georges Rene Pasquet