Isoquinolines (including Hydrogenated) Patents (Class 514/307)
  • Patent number: 10889588
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R9, Y, W, m, n, p and q are as defined herein, compositions including the compounds and methods of using the compounds.
    Type: Grant
    Filed: June 1, 2020
    Date of Patent: January 12, 2021
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jerome Hert, Daniel Hunziker, Patrizio Mattei, Markus Rudolph, Petra Schmitz, Christoph Ullmer
  • Patent number: 10875845
    Abstract: Described herein are compositions and methods for the treatment of ocular surface disorders including meibomian gland dysfunction, blepharitis, dry eye disease and other inflammatory and/or infectious disease of the anterior surface of the eye. Said compositions and methods comprise keratolytic conjugates which demonstrate keratolytic activity, and anti-inflammatory or other desirable activities. Topical administration of said compositions to the eyelid margin or surrounding areas provides therapeutic benefit to patients suffering from ocular surface disorders.
    Type: Grant
    Filed: June 17, 2020
    Date of Patent: December 29, 2020
    Assignee: AZURA OPHTHALMICS LTD.
    Inventors: Ian Holmes, Yair Alster, Hila Barash, Charles Bosworth, Omer Rafaeli, Marc Gleeson, Mark Richard Stewart, Robert M. Burk, Jonathan Dunn, Nicholas Chapman
  • Patent number: 10835513
    Abstract: Disclosed herein are methods and compositions for treating learning and memory deficits associated with Noonan Syndrome.
    Type: Grant
    Filed: June 27, 2014
    Date of Patent: November 17, 2020
    Assignee: The Regents of the University of California
    Inventors: Alcino Silva, Yong-Seok Lee, Dan Ehninger
  • Patent number: 10787410
    Abstract: Described are methods of treating or preventing a disease in a subject treatable by modulating cell mechanics.
    Type: Grant
    Filed: April 6, 2018
    Date of Patent: September 29, 2020
    Assignee: The Johns Hopkins University
    Inventors: Douglas Robinson, Alexandra Surcel, Win Pin Ng, Caren L. Freel Meyers
  • Patent number: 10738053
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R9, Y, W, m, n, p and q are as defined herein, compositions including the compounds and methods of using the compounds.
    Type: Grant
    Filed: March 23, 2018
    Date of Patent: August 11, 2020
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jerome Hert, Daniel Hunziker, Patrizio Mattei, Markus Rudolph, Petra Schmitz, Christoph Ullmer
  • Patent number: 10723721
    Abstract: The invention relates to a process for the preparation of lifitegrast (I) comprising a) reacting benzofuran-6-carboxylic acid (II) with a non-chlorinated carboxyl activating agent; and b) reacting the activated compound obtained in step a) with compound (III) or a salt thereof to give lifitegrast. It also relates to a process for the purification of lifitegrast (I) by i) reacting lifitegrast with dicyclohexylamine to give the dicyclohexylamine salt of lifitegrast (Ia); ii) isolating the salt from the reaction medium; iii) converting the isolated salt into lifitegrast by treatment with an acid; and iv) isolating lifitegrast from the reaction medium. It also relates to the dicyclohexylamine salt of lifitegrast (Ia) and to a process for its preparation.
    Type: Grant
    Filed: July 23, 2018
    Date of Patent: July 28, 2020
    Assignee: INTERQUIM, S.A.
    Inventors: Xavier Berzosa Rodríguez, Francisco Marquillas Olondriz
  • Patent number: 10696638
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof is provided. In formula (I), Ar is indazole, 5-isoquinoline, 6-isoquinoline, or their N-oxide. X is —C(?Z)—, wherein Z is N—CN, NH, NR4, NCOR4, NCONR4R5, NCO-aryl, S, or O. Y and J are independently H, alkyl, aryl, aminoalkyl, —NH2, —CN, —OH, —O-alkyl, —O-aryl, —COOH, —COOR4, —CONHR4, —CONHCH2-aryl, —CONR4CH2-aryl, —NHCOR4, halogen, halogened alkyl, -alkyl-OR4, -alkyl-ONO2, alkyl-ONO2, —OCOOR4, —O(C?O)-aryl, —CHR4OH, —CH2OH, —CH2O(C?O)-aryl, —CH2O(C?O)—R4, —CHR4O(C?O)-aryl, —CHR4O(C?O)—R4, unsaturated carboxylic ester, substituted alkynyl, —NHSO2R4, —SO2R4, —SO2NHR4, or —SO2NR4R5, or Y and J bond together to form a carbocylic or aromatic ring, wherein R4 and R5 are independently H, substituted C1-C6 alkyl, substituted aryl, cycloalkyl, alkylaryl, -alkyl-NR6R7, —S(O)0-2-(alkyl-NR6R7).
    Type: Grant
    Filed: November 30, 2018
    Date of Patent: June 30, 2020
    Assignee: INDUSTRIAL TECHNOLOGY RESEARCH INSTITUTE
    Inventors: Chih-Hung Chen, Yi-Hsun Chen, Jui-Wen Huang, Kuo-Kuei Huang, Chih-Peng Liu, Chrong-Shiong Hwang
  • Patent number: 10676429
    Abstract: Inhibitors of HBV replication of Formula (I) including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein B, R1, R2 and R4 have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HBV inhibitors, in HBV therapy.
    Type: Grant
    Filed: August 28, 2013
    Date of Patent: June 9, 2020
    Assignee: Janssen Sciences Ireland UC
    Inventors: Koen Vandyck, Stefaan Julien Last, Geert Rombouts, Wim Gaston Verschueren, Pierre Jean-Marie Bernard Raboisson
  • Patent number: 10654844
    Abstract: Provided are compounds that are inhibitors of both rho kinase and of a monoamine transporter (MAT) act to improve the disease state or condition. Further provided are compositions comprising the compounds. Further provided are methods for treating diseases or conditions, the methods comprising administering compounds according to the invention. One such disease may be glaucoma for which, among other beneficial effects, a marked reduction in intraocular pressure (IOP) may be achieved.
    Type: Grant
    Filed: June 7, 2019
    Date of Patent: May 19, 2020
    Assignee: Aerie Pharmaceuticals, Inc.
    Inventors: Mitchell A. deLong, Jill Marie Sturdivant, Susan M. Royalty
  • Patent number: 10655130
    Abstract: Described herein is a previously unknown function of XBP1 in triple-negative breast cancer (TNBC). It is shown that XBP1 is preferentially spliced and activated in TNBC, and that deletion of XBP1 significantly blocks triple negative breast tumor growth. Strikingly, XBP1 is required for the self-renewal of breast tumor initiating cells (TICs). Genome-wide mapping of the XBP1 transcriptional regulatory network identified a fundamental role for XBP1 in regulating the response to hypoxia via the transcription factor hypoxia-inducible factor 1? (HIF1?). Importantly, activation of this pathway appears to carry prognostic implications, as expression of the XBP1-dependent signature is associated with shorter survival times in human TNBC.
    Type: Grant
    Filed: February 23, 2017
    Date of Patent: May 19, 2020
    Assignee: Cornell University
    Inventors: Laurie H. Glimcher, Xi Chen
  • Patent number: 10640466
    Abstract: A compound of the general formula (A) or a pharmaceutically acceptable salt, solvate, hydrate, polymorph, prodrug, codrug, cocrystal, tautomer, racemate, stereoisomer or mixture thereof, in which: X is independently NO2 or H; and Y is selected from H, amino, amide, ester, carboxy and its esters and amides, alkyl, alkenyl, alkynyl, cycloalkyl, alkaryl, aryl, heterocyclic or heteroaryl groups, all of which can be substituted with heteroatoms and/or side groups, and wherein any chains can be straight or branched is disclosed.
    Type: Grant
    Filed: May 9, 2016
    Date of Patent: May 5, 2020
    Assignee: UNIVERSITY OF HERTFORDSHIRE HIGHER EDUCATION CORPORATION
    Inventors: Sharon Rossiter, Stewart Brian Kirton, Ramatoulie Camara
  • Patent number: 10596168
    Abstract: Chemical compounds are useful in the treatment of a subject afflicted by a thyroid disease. The compounds exhibit activity as thyroid-stimulating hormone receptor (TSHR) antagonists and can be used in the treatment of hyperthyroidism, Graves' disease, Graves' Ophthalmopathy and thyroid cancer.
    Type: Grant
    Filed: April 26, 2017
    Date of Patent: March 24, 2020
    Assignee: Forschungsverbund Berlin e.V.
    Inventors: Gerd Krause, Inna Hoyer, Edgar Specker, Jens Furkert, Patrick Marcinkowski, Jens-Peter Von Kries, Martin Neuenschwander, Marc Nazare
  • Patent number: 10543207
    Abstract: The present disclosure is directed to compounds and methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist-induced fluid retention. The present disclosure is also directed to compounds and methods for the treatment of hypertension. The present disclosure is also directed to compounds and methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders. The methods generally comprise administering to a mammal in need thereof a pharmaceutically effective amount of a compound, or a pharmaceutical composition comprising such a compound, that is designed to be substantially active in the gastrointestinal (GI) tract to inhibit NHE-mediated antiport of sodium ions and hydrogen ions therein.
    Type: Grant
    Filed: January 9, 2017
    Date of Patent: January 28, 2020
    Assignee: ARDELYX, INC.
    Inventors: Dominique Charmot, Marc Navre, Christopher Carreras, Noah Bell, Michael Robert Leadbetter, Jeffrey W. Jacobs
  • Patent number: 10532977
    Abstract: Small molecule compounds derived from ?-sulfophenylacetic amide (SPAA) are provided as novel sulfonic acid based pTyr mimetics. These compounds effectively inhibit a variety of protein tyrosine phosphatases (PTPs), such as mPTPA, mPTPB, LMWPTP, and Laforin. Use of these compounds as pharmaceutical agents for treating diseases associated with abnormal protein tyrosine phosphatase activity is also provided.
    Type: Grant
    Filed: June 1, 2016
    Date of Patent: January 14, 2020
    Assignee: Indiana University Research and Technology Corporation
    Inventors: Zhong-Yin Zhang, Rongjun He
  • Patent number: 10525050
    Abstract: Derivatives of 1,2,3,4-tetrahydroisoquinoline (THIQ) having the general formula A-(CH2)n—B are provided, wherein A is THIQ or a substituted derivative thereof and B is an aryl, cycloalkylaryl, or cycloalkyl group, wherein A and B are linked to each other by an alkyl or substituted alkyl chain. The compounds are useful as selective ligands (agonists or antagonists) of central nervous system receptors, and in particular of the seratonin receptors. The compounds or their salts can be formulated into pharmaceutical in need thereof by any route of administration suitable for a desired treatment protocol and especially for the treatment of psychiatric disorders.
    Type: Grant
    Filed: January 4, 2018
    Date of Patent: January 7, 2020
    Assignee: Florida A&M University
    Inventor: Seth Y. Ablordeppey
  • Patent number: 10493070
    Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, azadecaline derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formula I: These compounds are useful for the treatment of HIV and AIDS.
    Type: Grant
    Filed: June 28, 2017
    Date of Patent: December 3, 2019
    Assignee: ViiV HEALTHCARE UK (NO. 5) LIMITED
    Inventors: Jie Chen, Nicholas A. Meanwell, Alicia Regueiro-Ren, Sing-Yuen Sit, Jacob Swidorski, Yan Chen
  • Patent number: 10450293
    Abstract: The disclosure relates to chemokine receptor modulators and uses related thereto. In certain embodiments, the disclosure relates to pharmaceutical compositions comprising compounds disclosed herein or pharmaceutically acceptable salts or prodrugs thereof. In certain embodiments, the compositions disclosed herein are used for managing chemokine related conditions, typically prevention or treatment of viral infections such as HIV or for managing cancer.
    Type: Grant
    Filed: May 15, 2015
    Date of Patent: October 22, 2019
    Assignee: Emory University
    Inventors: Bryan D. Cox, Lawrence J. Wilson, Anthony Prosser, Dennis C. Liotta, James P. Snyder
  • Patent number: 10406199
    Abstract: Provided herein are stable lisinopril oral liquid formulations. Also provided herein are methods of using lisinopril oral liquid formulations for the treatment of certain diseases including hypertension, heart failure and acute myocardial infarction.
    Type: Grant
    Filed: March 7, 2019
    Date of Patent: September 10, 2019
    Assignee: SILVERGATE PHARMACEUTICALS, INC.
    Inventors: Gerold L. Mosher, David W. Miles
  • Patent number: 10385060
    Abstract: The present invention relates to a piperidine derivative and the preparation method and a pharmaceutical use thereof. In particular, the present invention relates to the piperidine derivative as shown by general formula (I) and the preparation method thereof and a pharmaceutical composition containing the same, and the use thereof as an estrogen receptor modulator in the treatment of estrogen receptor mediated or dependent diseases or conditions, the diseases preferably being breast cancer. In the abstract, the definition of each substituent of the general formula (I) is the same as that in the description.
    Type: Grant
    Filed: June 20, 2018
    Date of Patent: August 20, 2019
    Assignees: Jiangsu Hengrui Medicine Co., Ltd., Shanghai Hangrui Pharmaceutical Co., Ltd.
    Inventors: Shanghai Yu, Fanglong Yang, Lei Chen, Jingjing Yan, Xiqian Zhang, Zhichao Xie, Lingxiang Chen, Mingxun He
  • Patent number: 10385024
    Abstract: The present disclosure is directed to compounds and methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist-induced fluid retention. The present disclosure is also directed to compounds and methods for the treatment of hypertension. The present disclosure is also directed to compounds and methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders.
    Type: Grant
    Filed: June 13, 2018
    Date of Patent: August 20, 2019
    Assignee: ARDELYX, INC.
    Inventors: Noah Bell, Christopher Carreras, Dominique Charmot, Tao Chen, Michael Leadbetter, Jeffrey Jacobs, Jason Lewis
  • Patent number: 10385399
    Abstract: The present invention provides a method for determining the oxygen status of a cancer of an individual. The method comprise determining the transcriptional expression level of ADM (SEQ ID No:1), and/or at least one gene selected from ANKRD37 (SEQ ID NO.: 3), P4HA2 (SEQ ID NO.: 12), NDRG1 (SEQ ID NO: 10), SLC2A1 (SEQ ID NO:15), P4HA1 (SEQ ID NO.: 11), LOX (SEQ ID NO.: 9), C3orf28 (SEQ ID NO.: 6), BNIP3L (SEQ ID NO.: 5), BNIP3 (SEQ ID NO.:4), EGLN3 (SEQ ID NO.: 7), PDK1 (SEQ ID NO.: 13), PFKFB3 (SEQ ID NO.: 14), KCTD11 (SEQ ID NO.: 8), and/or ALDOA (SEQ ID NO.: 2), in a cancer sample. The transcriptional level is then correlated to the transcriptional level to at least one reference gene, and oxygen status 10 is then evaluated by comparing the correlated transcription level with a predetermined reference sample comprising cancer cells characterized by a high oxygen level.
    Type: Grant
    Filed: April 30, 2012
    Date of Patent: August 20, 2019
    Assignee: AARHUS UNIVERSITET
    Inventors: Jens Overgaard, Brita Singers Sorensen, Jan Alsner, Carsten Wiuf, Marianne Nordsmark, Kasper Toustrup
  • Patent number: 10376481
    Abstract: The present disclosure is directed to compounds and methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist-induced fluid retention. The present disclosure is also directed to compounds and methods for the treatment of hypertension. The present disclosure is also directed to compounds and methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders.
    Type: Grant
    Filed: January 9, 2017
    Date of Patent: August 13, 2019
    Assignee: ARDELYX, INC.
    Inventors: Noah Bell, Christopher Carreras, Michael Robert Leadbetter, Jason Gustaf Lewis, Jeffrey W. Jacobs, Irina Dotsenko, Dean Dragoli, Ying He, Andrew King, Matthew Siegel
  • Patent number: 10329516
    Abstract: The present invention relates to novel compounds and their use as fragrance materials.
    Type: Grant
    Filed: December 1, 2017
    Date of Patent: June 25, 2019
    Assignee: International Flavors & Fragrances Inc.
    Inventors: Benjamin Amorelli, Iyare Amegor, Michael G. Monteleone, Vincent Colandrea
  • Patent number: 10316029
    Abstract: Provided are compounds that are inhibitors of both rho kinase and of a monoamine transporter (MAT) act to improve the disease state or condition. Further provided are compositions comprising the compounds. Further provided are methods for treating diseases or conditions, the methods comprising administering compounds according to the invention. One such disease may be glaucoma for which, among other beneficial effects, a marked reduction in intraocular pressure (IOP) may be achieved.
    Type: Grant
    Filed: March 30, 2018
    Date of Patent: June 11, 2019
    Assignee: Aerie Pharmaceuticals, Inc.
    Inventors: Mitchell A. deLong, Jill M. Sturdivant, Susan M. Royalty
  • Patent number: 10292980
    Abstract: In DN-DISC1 mice, a mouse model for major mental illnesses, the model that expresses pathological phenotypes relevant to schizophrenia, mood disorders, and addiction simultaneously, the inventors of the present invention found pronounced levels of oxidative stress in the prefrontal cortex, but not in the striatum. These mice also displayed greater amounts of GAPDH-Siah1 binding, a protein-protein interaction that is activated under exposure to oxidative stress. The present inventors investigated the role of oxidative stress in other organ systems. As detailed herein, the inventors found that GAPDH-Siah1 binding was increased in mouse models of cardiac failure. It was also found, that certain novel analogs of deprenyl, significantly inhibited GAPDH-Siah1 binding in cardiac tissue.
    Type: Grant
    Filed: December 12, 2016
    Date of Patent: May 21, 2019
    Assignee: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Akira Sawa, Elki Takimoto, Neelam Shahani, David Kass, Toshiaki Saito
  • Patent number: 10247737
    Abstract: A method of classifying a subject having idiopathic scoliosis (IS) or at risk of developing IS comprising: determining the cellular response to Gi stimulation in a cell sample from the subject in the presence of OPN; determining the cellular response to Gi stimulation in a cell sample from the subject in the absence of OPN; and comparing the cellular response obtained in the presence of OPN with the cellular response obtained in the absence of OPN, whereby the comparing step enables the classification of the subject into one IS functional group. Also provided is the use of the foregoing method to classify borderline subjects and kits for applying the methods.
    Type: Grant
    Filed: September 9, 2014
    Date of Patent: April 2, 2019
    Assignee: Chu Sainte-Justine
    Inventors: Alain Moreau, Marie-Yvonne Akoume Ndong
  • Patent number: 10195192
    Abstract: A method for the treatment and/or prevention of pain which comprises administering to a subject in need of such treatment a therapeutically effective amount of 1-(3-4(((1R,3S,5S)-adamantan-1-yl)(phenyl)methyl)propyl)-4-methylpiperazine and pharmaceutically acceptable salts thereof (“AV1066”), with reference to visceral and neuropathic pain.
    Type: Grant
    Filed: November 1, 2016
    Date of Patent: February 5, 2019
    Assignee: ANAVEX LIFE SCIENCES CORP.
    Inventor: Christopher U. Missling
  • Patent number: 10174017
    Abstract: Provided are compounds that are inhibitors of both rho kinase and of a monoamine transporter (MAT) act to improve the disease state or condition. Further provided are compositions comprising the compounds. Further provided are methods for treating diseases or conditions, the methods comprising administering compounds according to the invention. One such disease may be glaucoma for which, among other beneficial effects, a marked reduction in intraocular pressure (IOP) may be achieved.
    Type: Grant
    Filed: March 16, 2018
    Date of Patent: January 8, 2019
    Assignee: Aerie Pharmaceuticals, Inc.
    Inventors: Mitchell A. deLong, Jill M. Sturdivant, Susan M. Royalty
  • Patent number: 10159634
    Abstract: A method for inhibiting hair growth in mammals using compositions containing FP receptor antagonists (e.g., prostaglandin F analogs that are block activation of the FP receptor). The compositions can be applied topically to the skin and/or hair. The compositions can arrest hirsutism or hypertrichosis, reverse hirsutism and hypertrichosis, and further prevent hair growth. These compositions can also be used to protect hair from chemical or radiation-induced alopecia or hair loss. These compositions can also be used to inhibit pigmentation of the hair or skin.
    Type: Grant
    Filed: April 12, 2017
    Date of Patent: December 25, 2018
    Inventors: Mitchell A. deLong, Elise A. Olsen
  • Patent number: 10123997
    Abstract: A method of treating hepatitis B virus includes inhibiting the activities of AKT and/or mTOR, inhibiting the synthesis of 5-phosphate ribose, and inhibiting HBV DNA and HBV cccDNA.
    Type: Grant
    Filed: June 15, 2015
    Date of Patent: November 13, 2018
    Inventor: Yong Liao
  • Patent number: 10081607
    Abstract: Embodiments of the present disclosure, in one aspect, relate to a 2,4-diaminoquinazoline compound, pharmaceutical compositions including a 2,4-diaminoquinazoline compound, methods of treatment of a condition (e.g., infection) or disease, methods of treatment using compositions or pharmaceutical compositions, and the like.
    Type: Grant
    Filed: October 31, 2014
    Date of Patent: September 25, 2018
    Assignee: University of South Florida
    Inventors: Roman Manetsch, Lindsey Neil Shaw, Kurt Steven Van Horn, Whittney Nicole Burda
  • Patent number: 10077261
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including those mediated by inhibition of fatty acid synthase (FASN) enzyme, such as, cancer, obesity or related discorders, and liver related disorders. Such compounds are represented by formula (I) as follows: wherein L1, a, b, m, n, R1, R2, R3, R4, and R5 are defined herein.
    Type: Grant
    Filed: September 11, 2015
    Date of Patent: September 18, 2018
    Assignee: Janssen Pharmaceutica NV
    Inventors: Peter J. Connolly, Gilles C. Bignan, Tianbao Lu, Michael H. Parker, Donald W. Ludovici, Christophe Meyer, Lieven Meerpoel, Karine Smans, Christian Rocaboy
  • Patent number: 10047087
    Abstract: The present application relates to a series of substituted pyrazolo[1,5-a]pyridine compounds, their use as tropomyosin receptor kinase (Trk) family protein kinase inhibitors, method of making and pharmaceutical compositions comprising such compounds.
    Type: Grant
    Filed: June 1, 2017
    Date of Patent: August 14, 2018
    Assignee: Dr. Reddy's Laboratories Ltd.
    Inventors: Pradip Kumar Sasmal, Shahadat Ahmed, Ashok Tehim, Vidyadhar Paradkar, Prasanna M. Dattatreya, Nanjegowda Jagadeesh Mavinahalli
  • Patent number: 9993470
    Abstract: Described herein are compounds and compositions for treating glaucoma and/or reducing intraocular pressure. Compositions may comprise an isoquinoline compound and a prostaglandin or a prostaglandin analog. Compounds described herein include those in which an isoquinoline compound is covalently linked to a prostaglandin or a prostaglandin analog, and those in which an isoquinoline compound and a prostaglandin free acid together form a salt.
    Type: Grant
    Filed: June 19, 2017
    Date of Patent: June 12, 2018
    Assignee: Aerie Pharmaceuticals, Inc.
    Inventors: Casey Kopczynski, Cheng-Wen Lin, Jill Marie Sturdivant, Mitchell A. deLong
  • Patent number: 9963432
    Abstract: Disclosed are alpha-aryl-beta-amino isoquinoline amide compounds and substituted benzamide compounds. In particular, the invention provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents. The compounds of the invention are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, cardiovascular diseases, and diseases characterized by abnormal growth, such as cancers. The invention further provides compositions containing isoquinoline amide compounds.
    Type: Grant
    Filed: March 31, 2017
    Date of Patent: May 8, 2018
    Assignee: Aerie Pharmaceuticals, Inc.
    Inventors: Jill M. Sturdivant, Mitchell A. deLong, Susan M. Royalty
  • Patent number: 9951059
    Abstract: Provided are compounds that are inhibitors of both rho kinase and of a monoamine transporter (MAT) act to improve the disease state or condition. Further provided are compositions comprising the compounds. Further provided are methods for treating diseases or conditions, the methods comprising administering compounds according to the invention. One such disease may be glaucoma for which, among other beneficial effects, a marked reduction in intraocular pressure (IOP) may be achieved.
    Type: Grant
    Filed: February 28, 2017
    Date of Patent: April 24, 2018
    Assignee: Aerie Pharmaceuticals, Inc.
    Inventors: Mitchell A. deLong, Jill Marie Sturdivant, Susan M. Royalty
  • Patent number: 9856239
    Abstract: The present invention relates to the technical field of medicine, and specifically relates to the carboxylic acid compound represented by the chemical formula I or chemical formula II, and a pharmaceutically acceptable salt, a prodrug, and a solvate thereof, and a method for preparation thereof, as well as a pharmaceutical composition containing the described substances, and a use thereof.
    Type: Grant
    Filed: October 3, 2017
    Date of Patent: January 2, 2018
    Assignee: InventisBio Shanghai Ltd.
    Inventor: Yueheng Jiang
  • Patent number: 9856478
    Abstract: The present invention features methods for preventing and treating three related diseases, diet-induced obesity, metabolic syndrome, and atherosclerosis, alone or in combination by inhibiting Acyl-CoA:Cholesterol Acyltransferase 1 (ACATI) activity or expression in myeloid cells.
    Type: Grant
    Filed: September 10, 2014
    Date of Patent: January 2, 2018
    Assignee: TRUSTEES OF DARTMOUTH COLLEGE
    Inventors: Ta-Yuan Chang, Catherine C. Y. Chang, Li-Hao Huang, Elaina Melton, Paul Sohn
  • Patent number: 9814751
    Abstract: Provided herein are stable lisinopril oral liquid formulations. Also provided herein are methods of using lisinopril oral liquid formulations for the treatment of certain diseases including hypertension, heart failure and acute myocardial infarction.
    Type: Grant
    Filed: April 10, 2017
    Date of Patent: November 14, 2017
    Assignee: SILVERGATE PHARMACEUTICALS, INC.
    Inventors: Gerold L. Mosher, David W. Miles
  • Patent number: 9815797
    Abstract: A series of substituted heteroaromatic compounds containing two fused six-membered rings, tivity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
    Type: Grant
    Filed: December 8, 2014
    Date of Patent: November 14, 2017
    Assignee: UCB Biopharma SPRL
    Inventors: Rikki Peter Alexander, Gregory Foulkes, Martin Clive Hutchings, Victoria Elizabeth Jackson, Boris Kroeplien, James Thomas Reuberson, Sarah Margaret Rook, Zhaoning Zhu
  • Patent number: 9809858
    Abstract: Biomarkers, methods, assays, and kits are provided for determining the prognosis of and treating a patient with ovarian cancer. Also disclosed are biomarkers, methods, assays, and kits for predicting the sensitivity of ovarian cancer cells to chemotherapy.
    Type: Grant
    Filed: April 5, 2013
    Date of Patent: November 7, 2017
    Assignee: H. Lee Moffitt Cancer Center and Research Institute, Inc.
    Inventors: Johnathan M. Lancaster, Douglas C. Marchion, Yin Xiong
  • Patent number: 9791452
    Abstract: This disclosure relates to methods of diagnosing and predicting renal disease, using one, two, or more biomarkers, including sTNFR1, sTNFR2, sFAS, TNF, and IL-6.
    Type: Grant
    Filed: December 9, 2009
    Date of Patent: October 17, 2017
    Assignee: Joslin Diabetes Center, Inc.
    Inventors: Monika A. Niewczas, Andrzej S. Krolewski
  • Patent number: 9783573
    Abstract: There are disclosed compounds of formula (I) that modulate the activity of inhibitors of apoptosis (IAPs), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.
    Type: Grant
    Filed: September 17, 2013
    Date of Patent: October 10, 2017
    Assignee: Bristol-Myers Squibb Company
    Inventors: Robert M. Borzilleri, Kyoung S. Kim, Heidi L. Perez, Erik M. Stang, David K. Williams, Liping Zhang
  • Patent number: 9783544
    Abstract: Compounds having formula I, or pharmaceutically acceptable salts, hydrates or N-oxides thereof are provided and are useful for binding to CXCR7, and treating diseases that are dependent, at least in part, on CXCR7 activity. Accordingly, the present invention provides in further aspects, compositions containing one or more of the above-noted compounds in admixture with a pharmaceutically acceptable excipient.
    Type: Grant
    Filed: August 26, 2015
    Date of Patent: October 10, 2017
    Assignee: CHEMOCENTRYX, INC.
    Inventors: Junfa Fan, Antoni Krasinski, Christopher W. Lange, Rebecca M. Lui, Jeffrey P. McMahon, Jay P. Powers, Yibin Zeng, Penglie Zhang
  • Patent number: 9775902
    Abstract: The present invention relates to methods and agents useful for the treatment of stroke, including ischemic stroke and hemorrhagic stroke. In particular, methods and agents for treating stroke in a subject are provided, wherein the agent is administered prior to diagnosis of the stroke as an ischemic stroke or a hemorrhagic stroke.
    Type: Grant
    Filed: July 11, 2011
    Date of Patent: October 3, 2017
    Assignee: FIBROGEN, INC
    Inventors: Stephen J. Klaus, Ingrid Langsetmo Parobok, Christopher T. Jacob
  • Patent number: 9751850
    Abstract: Compounds of formula (I) wherein R1, R2, R3, and Y are defined in the description are TRPA1 antagonists. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
    Type: Grant
    Filed: November 4, 2014
    Date of Patent: September 5, 2017
    Assignee: ABBVIE INC.
    Inventors: Richard J. Perner, Michael E. Kort, Stanley DiDomenico, Jun Chen, Anil Vasudevan
  • Patent number: 9707222
    Abstract: The present invention provides a method for activating the AMP-dependent protein kinase (AMPK) in a subject comprising administering the subject with a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound having the general Formula I, preferably salsolinol or reticuline. The pharmaceutical composition is able to activate AMPK, and thus is effective in the regulation of cell growth and metabolism, and the treatment of AMPK associated diseases.
    Type: Grant
    Filed: September 22, 2014
    Date of Patent: July 18, 2017
    Assignee: ZIH YUAN TANG BIOTECHNOLOGY CO., LTD.
    Inventors: Shoei-Sheng Lee, Ming-Jai Su, Chi-Huan Yeh, Sheng-Fa Tsai, Cheng-Yen Tsai, Chi-Tun Ruan, Chao-Min Hsu
  • Patent number: 9688635
    Abstract: Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of treatment of cancer are described.
    Type: Grant
    Filed: September 24, 2013
    Date of Patent: June 27, 2017
    Assignee: NEUPHARMA, INC.
    Inventors: Xiangping Qian, Yong-liang Zhu
  • Patent number: 9682950
    Abstract: Selective neuronal nitric oxide synthase (nNOS) inhibitor compounds designed with one or more thiophene-2-carboximidamide substituents for improved bioavailability.
    Type: Grant
    Filed: January 25, 2016
    Date of Patent: June 20, 2017
    Assignee: Northwestern University
    Inventors: Richard B. Silverman, He Huang, Qing Jing
  • Patent number: RE46886
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: October 31, 2016
    Date of Patent: June 5, 2018
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Jehrod Burnett Brenneman, John Ginn, Michael D. Lowe, Christopher Ronald Sarko, Edward S. Tasber, Zhonghua Zhang