Three Or More Ring Hetero Atoms In The Tricyclo Ring System Patents (Class 546/82)
  • Patent number: 11858933
    Abstract: The invention provides a novel class of therapeutics that are safe and effective inhibitors of Janus kinase 1 and pharmaceutical composition and methods of preparation and use thereof in the treatment of various diseases and disorders (e.g., inflammatory diseases, immune-mediated diseases or cancer).
    Type: Grant
    Filed: June 30, 2023
    Date of Patent: January 2, 2024
    Assignee: LYNK PHARMACEUTICALS CO. LTD.
    Inventors: Zhaokui Wan, Michael Lawrence Vazquez
  • Patent number: 11851431
    Abstract: The invention provides a novel class of therapeutics that are safe and effective inhibitors of Janus kinase 1 and pharmaceutical composition and methods of preparation and use thereof in the treatment of various diseases and disorders (e.g., inflammatory diseases, immune-mediated diseases or cancer).
    Type: Grant
    Filed: June 30, 2023
    Date of Patent: December 26, 2023
    Assignee: LYNK PHARMACEUTICALS CO. LTD.
    Inventors: Zhaokui Wan, Michael Lawrence Vazquez
  • Patent number: 11767323
    Abstract: The present application provides tricyclic pyridone compounds that modulate the activity of the V617F variant of JAK2, which are useful in the treatment of various diseases, including cancer.
    Type: Grant
    Filed: July 1, 2021
    Date of Patent: September 26, 2023
    Assignee: Incyte Corporation
    Inventors: Kai Liu, Onur Atasoylu, Yu Bai, Andrew W. Buesking, Leah C. Konkol, Cheng-Tsung Lai, Song Mei, Jun Pan, Liangxing Wu, Wenqing Yao
  • Patent number: 11753408
    Abstract: Disclosed are compounds of formula (I) and formula (II): wherein R1, R2, A, and B are as defined herein. Also disclosed is a method of blocking transmission of a Plasmodium parasite and a method of treating or preventing malaria comprising administering to an animal an effective amount of a first compound of formula (I) or (II) either alone or in combination with a second compound selected from elesclomol, NSC174938, NVP-AUY922, Maduramicin, Narasin, Alvespimycin, Omacetaxine, Thiram, Zinc pyrithione, Phanquinone, Bortezomib, Salinomycin sodium, Monensin sodium, Dipyrithione, Dicyclopentamethylene-thiuram disulfide, YM155, Withaferin A, Adriamycin, Romidepsin, AZD-1152-HQPA, CAY10581, Plicamycin, CUDC-101, Auranofin, Trametinib, GSK-458, Afatinib, and Panobinostat.
    Type: Grant
    Filed: April 22, 2021
    Date of Patent: September 12, 2023
    Assignees: The United States of America, as represented by the Secretary, Department of Health and Human Services, Loyola University of Chicago
    Inventors: Wenwei Huang, Hao Li, Wei Sun, Xiuli Huang, Paresma R. Patel, Hangmao Sun, Wei Zheng, Xiao Lu, Philip E. Sanderson, Myunghoon Kim, Meghan J. Orr, Gregory J. Tawa, Kim C. Williamson
  • Patent number: 11648245
    Abstract: The present invention provides heteroaryl ketone fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators, including their use for treating amyotrophic lateral sclerosis (ALS).
    Type: Grant
    Filed: July 28, 2021
    Date of Patent: May 16, 2023
    Assignee: Corcept Therapeutics, Inc.
    Inventors: Hazel Hunt, Tony Johnson, Nicholas Ray, Iain Walters
  • Patent number: 11590113
    Abstract: Methods and compositions are disclosed for diagnosing a patient suspected of suffering from, and for treating a patient suffering from, a disorder such as hypercortisolemia, metabolic syndrome, pre-diabetes, diabetes, Cushing's syndrome, Cushing's Disease, hyperglycemia secondary to hypercortisolemia, a liver disease, a cardiac disorder, high blood pressure, a blood clotting disorder, a cancer, a psychological disorder, weight gain, a disorder of glucose control, a bone disorder (e.g., osteoporosis), hypogonadism, pseudoacromegaly, pituitary tumors, functional hypercortisolism, ACTH secreting tumors, peripheral neuropathy, dyslipidemia and other disorders. The methods and compositions include administration of a heteroaryl-ketone fused azadecalin glucocorticoid receptor modulator (GRM).
    Type: Grant
    Filed: June 9, 2021
    Date of Patent: February 28, 2023
    Assignee: Corcept Therapeutics Incorporated
    Inventor: Andreas Moraitis
  • Patent number: 11498919
    Abstract: The invention provides novel azaindolylpyridone and diazaindolylpyridone compounds of formula (I), pharmaceutical compositions containing such compounds, and methods for using such compounds in treatment of diseases including cancer, type II diabetes, inflammatory diseases, autoimmune diseases, neurodegenerative disorders, cardiovascular disorders and viral infections; wherein R2, R3 and X are as defined in the specification.
    Type: Grant
    Filed: August 23, 2018
    Date of Patent: November 15, 2022
    Assignee: Sprint Bioscience AB
    Inventors: Johan Lindström, Rickard Forsblom, Fredrik Rahm, Jenny Viklund
  • Patent number: 11484502
    Abstract: The present invention provides a pharmaceutical composition comprising a PDE9 inhibitor. Specifically, the PDE9 inhibitor is (S)-7-(2-methoxy-3,5-dimethylpyridin-4-yl)-1-(tetrahydrofuran-3-yl)-1H-pyrazolo[4,3-c]quin olin-4(5H)-one or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: May 30, 2018
    Date of Patent: November 1, 2022
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Edgar Schuck, Robert Lai, Ishani Savant Landry, Bhaskar Rege, Mai Miyamoto, Sadaharu Kotani, Kanta Horie
  • Patent number: 11466005
    Abstract: Disclosed are tricyclic compounds as bromodomain and extra-terminal (BET) inhibitors which are shown as formula I, their synthesis and their use for treating diseases. More particularly, disclosed are fused heterocyclic derivatives useful as inhibitors of BET, methods for producing such compounds and methods for treating diseases and conditions wherein inhibition of one or more BET bromodomains provides a benefit.
    Type: Grant
    Filed: December 23, 2021
    Date of Patent: October 11, 2022
    Assignee: JACOBIO PHARMACEUTICALS CO., LTD.
    Inventors: Haiquan Fang, Mingming Chen, Guiqun Yang, Yuelei Du, Yanping Wang, Tong Wu, Qinglong Li, Lei Zhang, Shaojing Hu
  • Patent number: 11439625
    Abstract: A combination product comprising: (A) a compound of formula (I) (I) wherein X is O or S, preferably O; R6 is H, C1-6alkyl, —(CH2)pCOOH, —(CH2)pCOOC1-6alkyl, —(CH2)pCONH2, (CH2)pCONHC1-6alkyl, and —(CH2)pCON(C1-6alkyl)2; R11 is H or C1-6 alkyl; each R5 is —OC1-10alkyl, —SC1-10alkyl, —C1-12alkyl, or OAr2; wherein Ar2 is phenyl, optionally substituted with one or more halo; each p is 0 to 3; each z is 1 to 2; or a salt thereof; and (B) a compound of formula (X) (X) where R1 is phenyl wherein said phenyl is substituted by lower alkyl unsubstituted or substituted by cyano; R3 is lower alkyl, such as methyl; and R4 is quinolinyl unsubstituted or substituted by halogen; or a tautomer thereof, or a pharmaceutically acceptable salt, or a hydrate or solvate thereof.
    Type: Grant
    Filed: March 14, 2017
    Date of Patent: September 13, 2022
    Assignee: Avexxin AS
    Inventors: Berit Johansen, Astrid Jullumstrø Feuerherm
  • Patent number: 11370788
    Abstract: Imidazo[4,5-c]quinoline compounds having a substituent that is attached at the N?1 position by a branched group, single enantiomers of the compounds, pharmaceutical compositions containing the compounds, and methods of making the compounds are disclosed. Methods of use of the compounds as immune response modifiers, for inducing cytokine biosynthesis in humans and animals, and in the treatment of diseases including infectious and neoplastic diseases are also disclosed.
    Type: Grant
    Filed: February 25, 2019
    Date of Patent: June 28, 2022
    Assignee: 3M Innovative Properties Company
    Inventors: George W. Griesgraber, Kevin J. Bechtold
  • Patent number: 11312716
    Abstract: The invention relates to 9H-pyrrolo-dipyridine derivatives of formula I, processes for preparing them, pharmaceutical compositions containing them and their use as radiopharmaceuticals in particular as imaging agents for the detection of Tau aggregates.
    Type: Grant
    Filed: January 22, 2020
    Date of Patent: April 26, 2022
    Inventors: Joel Mercier, Laurent Provins, Celine Vermeiren, Yogesh Anil Sabnis
  • Patent number: 11267813
    Abstract: The invention relates to imidazoquinoline derivatives and to pharmaceutical compositions containing the imidazoquinoline derivatives. The imidazoquinoline derivatives of the invention are useful as toll-like receptor agonists, in particular agonists of TLR7, and promote induction of certain cytokines.
    Type: Grant
    Filed: August 31, 2018
    Date of Patent: March 8, 2022
    Inventor: Christophe Henry
  • Patent number: 11254674
    Abstract: The present disclosure is directed to inhibitors of the CBP/p300 family of bromodomains. The compounds can be useful in the treatment of disease or disorders associated with the inhibition of the CBP/p300 family of bromodomains. For instance, the disclosure is concerned with compounds and compositions for inhibition of the CBP/p300 family of bromodomains, methods of treating, preventing, or ameliorating diseases or disorders associated with the inhibition of CBP/p300 family of bromodomains, and methods of synthesis of these compounds.
    Type: Grant
    Filed: June 8, 2020
    Date of Patent: February 22, 2022
    Assignee: FORMA Therapeutics, Inc.
    Inventors: Shawn E. R. Schiller, Torsten Herbertz, Hongbin Li, Bradford Graves, Steven Mischke, Angela West, Jennifer R. Downing, Anna Ericsson
  • Patent number: 11161844
    Abstract: The present invention provides novel cyclic substituted imidazo[4,5-c]quinoline derivatives of Formula (I), and the pharmaceutically acceptable salts thereof; wherein R1, R2, R4, R5, R6, X and Z are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of Formula I and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.
    Type: Grant
    Filed: March 1, 2018
    Date of Patent: November 2, 2021
    Assignee: PFIZER INC.
    Inventors: Thomas Allen Chappie, Paul Galatsis, Michelle Renee Garnsey, Christopher John Helal, Jaclyn Louise Henderson, Bethany Lyn Kormos, Ravi G. Kurumbail, Luis Angel Martinez-Alsina, Martin Youngjin Pettersson, Antonia Friederike Stepan, Travis T. Wager
  • Patent number: 11059823
    Abstract: 2-((1r,4r)-4-(imidazo[4,5-d]pyrrolo[2,3-b]pyridin-1(6H)-yl)cyclohexyl)acetonitrile compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions mediated by JAK, such as inflammatory bowel disease.
    Type: Grant
    Filed: February 12, 2019
    Date of Patent: July 13, 2021
    Assignee: Janssen Pharmaceutica NV
    Inventors: Tatiana Koudriakova, Kevin D. Kreutter, Kristi Leonard, Michele C. Rizzolio, Russell C. Smith, Mark S. Tichenor, Aihua Wang
  • Patent number: 11058670
    Abstract: Methods and compositions are disclosed for diagnosing a patient suspected of suffering from, and for treating a patient suffering from, a disorder such as hypercortisolemia, metabolic syndrome, pre-diabetes, diabetes, Cushing's syndrome, Cushing's Disease, hyperglycemia secondary to hypercortisolemia, a liver disease, a cardiac disorder, high blood pressure, a blood clotting disorder, a cancer, a psychological disorder, weight gain, a disorder of glucose control, a bone disorder (e.g., osteoporosis), hypogonadism, pseudoacromegaly, pituitary tumors, functional hypercortisolism, ACTH secreting tumors, peripheral neuropathy, dyslipidemia and other disorders. The methods and compositions include administration of a heteroaryl-ketone fused azadecalin glucocorticoid receptor modulator (GRM).
    Type: Grant
    Filed: February 21, 2020
    Date of Patent: July 13, 2021
    Assignee: Corcept Therapeutics Incorporated
    Inventor: Andreas Moraitis
  • Patent number: 10953004
    Abstract: A combination product comprising: (A) a compound of formula (I) R-L-CO—X (I) wherein R is a C10-24 unsaturated hydrocarbon group optionally interrupted by one or more heteroatoms or groups of heteroatoms selected from S, O, N, SO, SO2, said hydrocarbon group comprising at least 4 non-conjugated double bonds; L is a linking group forming a bridge of 1 to 5 atoms between the R group and the carbonyl CO wherein L comprises at least one heteroatom in the backbone of the linking group; and X is an electron withdrawing group; or a salt thereof; and (B) a compound of formula (X) where R1 is phenyl wherein said phenyl is substituted by lower alkyl unsubstituted or substituted by cyano; R3 is lower alkyl, such as methyl; and R4 is quinolinyl unsubstituted or substituted by halogen; or a tautomer thereof, or a pharmaceutically acceptable salt, or a hydrate or solvate thereof.
    Type: Grant
    Filed: March 14, 2017
    Date of Patent: March 23, 2021
    Assignee: Avexxin AS
    Inventors: Berit Johansen, Astrid Jullumstrø Feuerherm
  • Patent number: 10874670
    Abstract: The disclosure relates to substituted fused heteroaromatic compounds and the use thereof. Specifically, the disclosure provides compounds of the following Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein A1-A4, B1-B3, D1-D4 and R1-R3 are defined herein. Compounds having Formula I are kinalse inhibitors. Therefore, compounds of the disclosure may be used to treat clinical conditions caused by DDR functional defects, such as cancer.
    Type: Grant
    Filed: January 9, 2018
    Date of Patent: December 29, 2020
    Assignee: IMPACT THERAPEUTICS, INC.
    Inventors: Suixiong Cai, Ye Edward Tian
  • Patent number: 10870648
    Abstract: The present disclosure is directed to inhibitors of the CBP/p300 family of bromodomains. The compounds can be useful in the treatment of disease or disorders associated with the inhibition of the CBP/p300 family of bromodomains. For instance, the disclosure is concerned with compounds and compositions for inhibition of the CBP/p300 family of bromodomains, methods of treating, preventing, or ameliorating diseases or disorders associated with the inhibition of CBP/p300 family of bromodomains, and methods of synthesis of these compounds.
    Type: Grant
    Filed: June 28, 2019
    Date of Patent: December 22, 2020
    Assignee: Forma Therapeutics, Inc.
    Inventors: Shawn E. R. Schiller, Torsten Herbertz, Hongbin Li, Bradford Graves, Steven Mischke, Angela West, Jennifer R. Downing, Anna Ericsson
  • Patent number: 10745399
    Abstract: A compound of formula (IV) or a pharmaceutically acceptable salt, solvate, tautomer or stereoisomer thereof These imidazolonylquinoline compounds are useful in the inhibition, regulation and/or modulation of signal transduction by kinases, in particular ATM kinase, furthermore in pharmaceutical compositions, and in their use for the treatment of diseases which relate to ATM kinase, in particular cancer.
    Type: Grant
    Filed: March 14, 2019
    Date of Patent: August 18, 2020
    Assignee: Merck Patent GmbH
    Inventors: Thomas Fuchss, Kai Schiemann
  • Patent number: 10662193
    Abstract: The present invention relates to novel compounds that can be employed in the diagnosis, treatment, alleviation or prevention of a group of disorders and abnormalities associated with amyloid proteins and amyloid-like proteins, such as Alzheimer's disease. Precursors for the preparation of the compounds according to the present invention are also provided.
    Type: Grant
    Filed: January 21, 2015
    Date of Patent: May 26, 2020
    Assignees: AC IMMUNE SA, LIFE MOLECULAR IMAGING SA
    Inventors: Heiko Kroth, Sreenivasachary Nampally, Jér{hacek over (o)}me Molette, Emanuele Gabellieri, Pascal André René Benderitter, Wolfgang Froestl, Hanno Schieferstein, Andre Mueller, Heribert Schmitt-Willich, Mathias Berndt
  • Patent number: 10556903
    Abstract: This disclosure features compounds of Formula I, or a pharmaceutically acceptable salt thereof: in which R1, R2, R3, and R4 are as defined herein. These compounds are modulators of NLRP3, which are useful, e.g., for treating a condition, disease or disorder in which a decrease in NLRP3 activity (e.g., a condition, disease or disorder associated with repressed or impaired NLRP3 signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions as well as other methods of using and making the same.
    Type: Grant
    Filed: April 19, 2017
    Date of Patent: February 11, 2020
    Assignee: Innate Tumor Immunity, Inc.
    Inventors: Gary D. Glick, Shomir Ghosh, William R. Roush, Edward James Olhava
  • Patent number: 10487083
    Abstract: 2-((1r,4r)-4-(imidazo[4,5-d]pyrrolo[2,3-b]pyridin-1(6H)-yl)cyclohexyl)acetonitrile compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions mediated by JAK, such as inflammatory bowel disease.
    Type: Grant
    Filed: February 13, 2019
    Date of Patent: November 26, 2019
    Assignee: Janssen Pharmaceutica NV
    Inventors: Kevin D. Kreutter, Kristi Leonard, Michele C. Rizzolio, Russell C. Smith, Mark S. Tichenor, Aihua Wang
  • Patent number: 10364246
    Abstract: 2-((1r,4r)-4-(imidazo[4,5-d]pyrrolo[2,3-b]pyridin-1(6H)-yl)cyclohexyl)acetonitrile compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions mediated by JAK, such as inflammatory bowel disease.
    Type: Grant
    Filed: January 9, 2019
    Date of Patent: July 30, 2019
    Assignee: Janssen Pharmaceutica NV
    Inventors: Tatiana Koudriakova, Kevin D. Kreutter, Kristi Leonard, Michele C. Rizzolio, Russell C. Smith, Mark S. Tichenor, Aihua Wang
  • Patent number: 10294226
    Abstract: 2-((1r,4r)-4-(imidazo[4,5-d]pyrrolo[2,3-b]pyridin-1(6H)-yl)cyclohexyl)acetonitrile compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions mediated by JAK, such as inflammatory bowel disease.
    Type: Grant
    Filed: December 15, 2017
    Date of Patent: May 21, 2019
    Assignee: Janssen Pharmaceutica NV
    Inventors: Tatiana Koudriakova, Kevin D. Kreutter, Kristi Leonard, Michele C. Rizzolio, Russell C. Smith, Mark S. Tichenor, Aihua Wang
  • Patent number: 10130622
    Abstract: A corrector agent capable of stabilizing a newly synthesized cystic fibrosis transmembrane conductance regulator (CFTR) protein, useful in the treatment of cystic fibrosis.
    Type: Grant
    Filed: October 7, 2016
    Date of Patent: November 20, 2018
    Assignees: AbbVie S.á.r.l., Galapagos NV
    Inventors: Rhalid Akkari, Luke Jonathan Alvey, Xavier Marie Bock, Brian S. Brown, Pieter Isabelle Roger Claes, Marlon D. Cowart, Katja E. Conrath, Douglas Cyr, Elsa De Lemos, Gert Jules Hector De Wilde, Nicolas Desroy, Béranger Duthion, Gregory A. Gfesser, Romain Luc Marie Gosmini, Christopher Gaëtan Housseman, Koen Karel Jansen, Jianguo Ji, Philip R. Kym, Jean-Michel Lefrancois, Oscar Mammoliti, Christel Jeanne Marie Menet, Nuria Merayo Merayo, Gregory John Robert Newsome, Adeline Marie Elise Palisse, Sachin V. Patel, Mathieu Rafaël Pizzonero, Anurupa Shrestha, Elizabeth C. Swift, Chris Tse, Steven Emiel Van der Plas, Xueqing Wang
  • Patent number: 10118925
    Abstract: Imidazo[4,5-c] ring compounds, (particularly imidzao[4,5-c]quinolines, 6,7,8,9-tetrahydroimidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and 6,7,8,9-tetrahydroimidazo[4,5-c]naphthyridine compounds) having a substituted guanidine substituent at the 1-position, pharmaceutical compositions containing the compounds, and methods of making the compounds are disclosed. Methods of use of the compounds as immune response modifiers, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are also disclosed.
    Type: Grant
    Filed: August 26, 2016
    Date of Patent: November 6, 2018
    Assignee: 3M Innovative Properties Company
    Inventor: George W. Griesgraber
  • Patent number: 10105349
    Abstract: The present invention relates to certain PDE2 inhibitory compounds, in free or salt form, pharmaceutical compositions containing such compounds and methods for the treatment of PDE2 mediated disorders.
    Type: Grant
    Filed: December 7, 2015
    Date of Patent: October 23, 2018
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Peng Li, Hailin Zheng, Gretchen Snyder, Lawrence P. Wennogle, Joseph Hendrick
  • Patent number: 9938275
    Abstract: Imidazo-quinoline, -pyridine, and -naphthyridine ring systems (particularly quinolines, tetrahydroquinolines, pyridines, [1,5]naphthyridines, [1,5]tetrahydronaphthyridines) substituted at the 1-position with a cyclic substituent, pharmaceutical compositions containing the compounds, methods of making these compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
    Type: Grant
    Filed: January 23, 2017
    Date of Patent: April 10, 2018
    Assignee: 3M Innovative Properties Company
    Inventors: Doris Stoermer, Joseph F. Dellaria, Jr., David T. Amos, Bernhard M. Zimmermann, Luke T. Dressel, Jason D. Bonk, Matthew R. Radmer
  • Patent number: 9913844
    Abstract: Reversing resistance to a B-Raf inhibitor for the treatment of a proliferative disease by obtaining a tumor sample from the patient and testing it for genetic alterations in a panel of genes comprising BRAF, CRAF, CCND1, CDK4, HER2, IGF-1R, cMET, FGFR1, FGFR2, FGFR3 EGFR, MAP2K1, MAP2K2, NRAS, KRAS HRAS, PTEN, PIK3CA, and P16 and administering a drug combination therapy comprising the B-Raf inhibitor and a second inhibitor which overcomes resistance to the B-Raf inhibitor, which second inhibitor is selected based on genetic alterations discovered in the tumor sample.
    Type: Grant
    Filed: March 19, 2014
    Date of Patent: March 13, 2018
    Assignee: NOVARTIS AG
    Inventors: Giordano Caponigro, Darrin Stuart, Laure De Parseval
  • Patent number: 9873694
    Abstract: The present invention relates to a compound of Formula I: or an enantiomer, diastereomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same; and a method for treating or preventing autoimmunity disease using the same.
    Type: Grant
    Filed: October 3, 2012
    Date of Patent: January 23, 2018
    Assignee: JANUS BIOTHERAPEUTICS, INC.
    Inventors: Grayson B. Lipford, Charles M. Zepp
  • Patent number: 9598413
    Abstract: Crystalline form, Form T2H1.5-4, of N,Ndicyclopropyl-4-(1,5-dimethyl-1 Hpyrazol-3-ylamino)-6-ethyl-1-methyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridine-7-carboxamide, (Compound (I)) is provided. Also provided is a pharmaceutical composition and an oral dosage form comprising Form T2H1.5-4 of Compound (I) as well as a method of using the Form T2H1.5-4 of Compound (I) in the treatment of myeloproliferative disorders, which include polycythaemia vera, thrombocythaemia and primary myelofibrosis.
    Type: Grant
    Filed: May 28, 2014
    Date of Patent: March 21, 2017
    Assignee: Bristol-Myers Squibb Company
    Inventor: Shella Tameze
  • Patent number: 9593116
    Abstract: Crystalline form, Form T1H1.5-4, of N,N-dicyclopropyl-4-(1,5-dimethyl-1H-pyrazol-3-ylamino)-6-ethyl-1-methyl -1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridine-7-carboxamide (Compound (I)) is provided. Also provided is a pharmaceutical composition and an oral dosage form comprising Form T1H1.5-4 of Compound (I) as well as a method of using the Form T1H1.5-4 of Compound for the treatment of myeloproliferative disorders, which include polycythaemia vera, thrombocythaemia and primary myelofibrosis.
    Type: Grant
    Filed: May 28, 2014
    Date of Patent: March 14, 2017
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ashok Vinayak Purandare, Honghe Wan
  • Patent number: 9593117
    Abstract: Crystalline form, Form HI.5-4, of N,N-di-cyclopropyl-4-(1,5-dimethyl-1H-pyrazol-3-ylamino)-6-ethyl-1-methyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridine-7-carboxamide, (Compound I) is provided. Also provided are a pharmaceutical composition and an oral dosage form comprising Form HI.5-4 of Compound I as well as a method of using the Form HI.5-4 of Compound I in the treatment of myeloproliferative disorders, which include polycythaemia vera, thrombocythaemia and primary myelofibrosis.
    Type: Grant
    Filed: May 28, 2014
    Date of Patent: March 14, 2017
    Assignee: Bristol-Myers Squibb Company
    Inventor: Shella Tameze
  • Patent number: 9533997
    Abstract: The present invention relates to tricyclic heterocycles of Formula (I), which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.
    Type: Grant
    Filed: February 10, 2016
    Date of Patent: January 3, 2017
    Assignees: Incyte Holdings Corporation, Incyte Corporation
    Inventors: Andrew P. Combs, Thomas P. Maduskuie, Jr.
  • Patent number: 9518058
    Abstract: The invention relates to an improved process for synthesizing N,N-dicyclopropyl-4-(1,5-dimethyl-1H-pyrazol-3-ylamino)-6-ethyl-1-methyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridine-7-carboxamide of the formula: (I) Compound (I) is currently in clinical trials for the treatment of myeloproliferative disorders, such as polycythaemia vera, thrombocythaemia and primary myelofibrosis.
    Type: Grant
    Filed: August 28, 2014
    Date of Patent: December 13, 2016
    Assignee: Bristol-Myers Squibb Company
    Inventors: Martin D. Eastgate, Gregory L. Beutner, Benjamin Cohen, Nicolas Cuniere, Lopa V. Desai, Monica Fitzgerald, Qi Gao, Michael Bryan Hay, Michael Joseph Lawler, Paul C. Lobben, Christopher S. Regens, Thorsten Rosner, Neil Strotman, Carolyn S. Wei, Yi Xiao, Bin Zheng, Keming Zhu
  • Patent number: 9475812
    Abstract: The present invention relates to a pyridonaphthyridine compound as represented by general formula (I), which has a dual PI3K and mTOR inhibition effect, and its pharmaceutically acceptable salt, stereoisomer and deuteride thereof, wherein R1, R2, R3, R4, R5, R6, R7 and X are as defined in the specification; the present invention also relates to a method for preparing said compound, a pharmaceutical composition and a pharmaceutical formulation containing said compound, and uses of said compound in treating and/or preventing a proliferative disease and in the manufacture of a medicament for treating and/or preventing a proliferative disease.
    Type: Grant
    Filed: June 4, 2012
    Date of Patent: October 25, 2016
    Assignee: Xuanzhu Pharma Co., Ltd.
    Inventors: Frank Wu, Yan Zhang
  • Patent number: 9376392
    Abstract: The invention provides compounds and salts thereof as d herein. The invention also provides pharmaceutical compositions comprising a compound disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection, treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds disclosed herein.
    Type: Grant
    Filed: January 3, 2013
    Date of Patent: June 28, 2016
    Assignee: Gilead Sciences, Inc.
    Inventors: Kerim Babaoglu, Kyla L. Bjornson, Paul Hrvatin, Eric Lansdon, John O. Link, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu
  • Patent number: 9353113
    Abstract: An object of the present invention is to provide a drug having the inhibitory activity on ENPP2 which is a different target from that of the existing drug, as a medicament useful in a urinary excretion disorder patient for whom the existing drug has the insufficient effect. The present invention provides a compound represented by the general formula (I): (wherein definition of each group is as defined in the description) having the ENPP2 inhibitory activity, a salt thereof or a solvate thereof or a prodrug thereof, and an agent for preventing or treating urinary excretion disorder and/or improving symptoms thereof, containing them as an active ingredient.
    Type: Grant
    Filed: January 5, 2012
    Date of Patent: May 31, 2016
    Assignee: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Akira Ohata, Shingo Nakatani, Tetsuya Sugiyama, Takashi Morimoto
  • Patent number: 9326978
    Abstract: The claimed subject matter relates to allosteric modulation of A3 adenosine receptor (A3AR) and provides for the use of an A3 adenosine receptor modulator (A3RM), for the preparation of pharmaceutical compositions for modulating the A3AR in a subject, as well as pharmaceutical compositions including the same and therapeutic methods including administering to a subject an amount of an A3RM, the amount being effective to modulate A3AR activity. The A3RM according to claimed subject matter are 1H-Imidazo-[4,5-c]quinolin-4-amine derivatives. Also provided are 1H-Imidazo-[4,5-c]quinolin-4-amine derivatives.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: May 3, 2016
    Assignees: The United States of America, Represented by the Secretary, Dept. of Health and Human Services, Universiteit Leiden
    Inventors: Anikó Göblyös, Johannes Brussee, Adriaan P. Ijzerman, Zhan-Guo Gao, Kenneth Jacobson
  • Patent number: 9328110
    Abstract: Imidazo ring systems substituted at the 1-position, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
    Type: Grant
    Filed: March 11, 2014
    Date of Patent: May 3, 2016
    Assignee: 3M INNOVATIVE PROPERTIES COMPANY
    Inventors: Larry R. Krepski, Joseph F. Dellaria, Jr., Daniel E. Duffy, Matthew R. Radmer, David T. Amos
  • Patent number: 9324955
    Abstract: Provided herein are organic compounds useful in a variety of OLED applications.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: April 26, 2016
    Assignee: The Trustees of Dartmouth College
    Inventors: Ivan Abrahamian, Xin Su
  • Patent number: 9284330
    Abstract: Disclosed are 1,4-dihydro-naphthyridine derivatives and pharmaceutical composition and uses thereof. The 1,4-dihydro-naphthyridine derivatives are a compound capable of inhibiting acetylcholinesterase activity and preventing extracellular calcium from flowing into a cell via a calcium channel, i.e., having a dual-activity, which are of potential importance as a pharmaceutical and can be used to prepare the drugs for treating cardiovascular diseases, cerebrovascular diseases and dementia.
    Type: Grant
    Filed: December 7, 2012
    Date of Patent: March 15, 2016
    Assignee: Jiangsu Simovay Pharmaceutical Co., Ltd.
    Inventors: Rong Chen, Lin Feng, Zhengping Zhang, Fang Fang, Qingli Dong, Fulong Li, Lei Wang, Yao Hua, Shibao Yang, Peng Wang
  • Patent number: 9273047
    Abstract: The present invention provides heteroaryl ketone fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.
    Type: Grant
    Filed: September 16, 2014
    Date of Patent: March 1, 2016
    Assignee: Corcept Therapeutics, Inc.
    Inventors: Hazel Hunt, Tony Johnson, Nicholas Ray, Iain Walters
  • Patent number: 9127007
    Abstract: The invention relates to FSH receptor antagonist according to general formula (I) or a pharmaceutically acceptable salt thereof and to a pharmaceutical composition containing the same. The compounds can be used for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, and for the treatment of uterine fibroids and other menstrual-related disorders.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: September 8, 2015
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Wesley Peter Blackaby, Martin De Kort, Mark Enthoven, Paul Stuart Hinchliffe, Christian Bernard Matthijs Poulie, Cornelis Marius Timmers, Saskia Verkaik
  • Patent number: 9096594
    Abstract: The present invention provides compounds of formula I, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting kinase (e.g., GSK3 (e.g., GSK3? or GSK3?) or CK1) activity. The present invention further provides methods of using the compounds described herein for treating kinase-mediated disorders, such as neurological diseases, psychiatric disorders, metabolic disorders, and cancer.
    Type: Grant
    Filed: October 11, 2013
    Date of Patent: August 4, 2015
    Assignees: The Broad Institute, Inc., The General Hospital Corporation, Dana-Farber Cancer Institute, Inc.
    Inventors: Florence Fevrier Wagner, Jennifer Q. Pan, Sivaraman Dandapani, Andrew Germain, Edward Holson, Benito Munoz, Partha P. Nag, Michel Weiwer, Michael C. Lewis, Stephen J. Haggarty, Joshua A. Bishop, Kimberly Stegmaier, Versha Banerji
  • Patent number: 9045472
    Abstract: Disclosed herein are a compound of formula (I) and pharmaceutically acceptable salts thereof, processes for preparing the same, pharmaceutical compositions containing the same, and methods of using the same.
    Type: Grant
    Filed: December 16, 2011
    Date of Patent: June 2, 2015
    Assignees: ASTRAZENECA AB, SUMITOMO DAINIPPON PHARMA CO., LTD.
    Inventors: Thomas McInally, Austen Pimm
  • Publication number: 20150148341
    Abstract: The present invention provides octahydro fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.
    Type: Application
    Filed: November 21, 2014
    Publication date: May 28, 2015
    Inventors: Hazel Hunt, Iain Walters, Benoit Gourdet
  • Patent number: 9040706
    Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, Q, X1, X2, Y, R1, R2, R3, R4, R4?, R5, R6 and R6? are as described herein.
    Type: Grant
    Filed: November 22, 2013
    Date of Patent: May 26, 2015
    Assignee: GENENTECH, INC.
    Inventors: Frederick Cohen, Vickie Hsiao-Wei Tsui, Cuong Ly, John A. Flygare