Ring Chalcogen In The Additional Hetero Ring (e.g., Oxazole, Etc.) Patents (Class 514/236.8)
  • Patent number: 11142507
    Abstract: The present invention provides novel compounds of Formulae (I?), (I), (II?), and (II), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing proliferative diseases (e.g., cancers (e.g., leukemia, acute lymphoblastic leukemia, lymphoma, Burkitt's lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, ovarian cancer, neuroblastoma, lung cancer, colorectal cancer), benign neoplasms, diseases associated with angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g.
    Type: Grant
    Filed: September 9, 2016
    Date of Patent: October 12, 2021
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Nathanael S. Gray, Tinghu Zhang, Nicholas Paul Kwiatkowski, Mingfeng Hao
  • Patent number: 11036132
    Abstract: A resist composition which generates an acid upon exposure and whose solubility in a developing solution is changed due to an action of the acid, the resist composition including a base material component whose solubility in a developing solution is changed due to the action of an acid; and a compound represented by Formula (d1) in which Rb1 and Rb2 each independently represents —COO?, —COOH, or a hydroxyl group, where at least one of Rb1 and Rb2 represents —COO?, Rb3, Rb4, and Rb5 each independently represents a hydroxyl group or a halogen atom, Rb6 to Rb8 each independently represents an alkyl group, nb3 represents an integer of 0 to 4, nb4 and nb5 each independently represents an integer of 0 to 2, nb6 to nb8 each independently represents an integer of 0 to 5, m represents 1 or 2, and q represents an integer of 0 to 3.
    Type: Grant
    Filed: December 19, 2018
    Date of Patent: June 15, 2021
    Assignee: Tokyo Ohka Kogyo Co., Ltd.
    Inventors: Takashi Nagamine, Kazuishi Tanno, Tsuyoshi Nakamura, Masafumi Fujisaki
  • Patent number: 11033534
    Abstract: The present invention relates to a combination product and its use in therapy.
    Type: Grant
    Filed: January 29, 2018
    Date of Patent: June 15, 2021
    Assignee: GENFIT
    Inventors: Corinne Foucart, Robert Walczak, Carole Belanger, Benoït Noel
  • Patent number: 10889579
    Abstract: The present disclosure provides a class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables R1, R1?, R2, R2?, R3, R4, R5, R6, R7, and b of Formula I are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to A? plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, and other central nervous system conditions.
    Type: Grant
    Filed: December 13, 2017
    Date of Patent: January 12, 2021
    Assignee: Amgen Inc.
    Inventors: Matthew P. Bourbeau, Paul E. Harrington, Qingyian Liu
  • Patent number: 10738040
    Abstract: The present disclosure features disclosed compounds which can increase cystic fibrosis transmembrane conductance regulator (CFTR) activity as measured in human bronchial epithelial (hBE) cells. The present disclosure also features methods of treating a condition associated with decreased CFTR activity or a condition associated with a dysfunction of proteostasis comprising administering to a subject an effective amount of a disclosed compound.
    Type: Grant
    Filed: November 14, 2018
    Date of Patent: August 11, 2020
    Assignee: Proteostasis Therapeutics, Inc.
    Inventors: Cecilia M. Bastos, Benito Munoz, Bradley Tait
  • Patent number: 10351556
    Abstract: The present invention relates to novel processes for the preparation 1,3-Thiazol-5-ylmethyl[(2R,5R)-5-{[(2S)-2-[(methyl{[2-(propan-2-yl)-1,3-thiazol-4-yl]methyl} carbamoyl)amino]-4-(morpholin-4-yl)butanoyl]amino}-1,6-diphenylhexan-2-yl] carbamate having the following structural formula-1 and it's intermediates thereof.
    Type: Grant
    Filed: February 17, 2016
    Date of Patent: July 16, 2019
    Assignee: MSN LABORATORIES PRIVATE LIMITED
    Inventors: Srinivasan Thirumalai Rajan, Sajja Eswaraiah, Gutta Madhusudhan, Komati Satyanarayana, Jakku Malleswara Reddy
  • Patent number: 10149836
    Abstract: The subject matter described here relates to the use of compounds and methods for the increase of progranulin expression. The methods may take place in vitro, ex vivo such as in isolates from adult mammalian tissue, or in vivo. Compounds and methods described herein may find use in the treatment of frontotemporal dementia.
    Type: Grant
    Filed: March 20, 2015
    Date of Patent: December 11, 2018
    Assignee: The Board of Regents of the University of Texas System
    Inventors: Joachim Herz, Gang Yu, Bruce Posner, Basar Cenik
  • Patent number: 10130634
    Abstract: The present invention provides a therapeutic agent or prophylactic agent for an ophthalmic disease caused by ocular angiogenesis, which contains a morpholine compound represented by the formula (1) wherein ring A is aryl optionally having substituent(s) and the like; ring B is arylene optionally having substituent(s) and the like; m=0-2; n=1-5; X is a bond and the like; Y is a bond and the like; and Z is a hydrogen atom and the like, or a pharmaceutically acceptable salt thereof as an active ingredient.
    Type: Grant
    Filed: July 24, 2014
    Date of Patent: November 20, 2018
    Assignee: MITSUBISHI TANABE PHARMA CORPORATION
    Inventor: Hidemitsu Higashi
  • Patent number: 10030034
    Abstract: Compounds and methods in the fields of chemistry and medicine are disclosed. Some of the disclosed embodiments include compounds, compositions and methods of using heterocycle amines. Some of the disclosed embodiments include heterocycle amines useful to treat inflammatory disorders.
    Type: Grant
    Filed: January 26, 2016
    Date of Patent: July 24, 2018
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventors: Koc-Kan Ho, David Diller, Jeffrey J. Letourneau, Brian F. McGuinness, Andrew G. Cole, David Rosen, Cornelis A. van Oeveren, Jason C. Pickens, Lin Zhi, Yixing Shen, Bijan Pedram
  • Patent number: 10017463
    Abstract: Disclosed are small molecule inhibitors of deubiquitinating enzymes (DUBs), and methods of using them. Certain compounds are selective for particular ubiquitin-specific proteases (USPs).
    Type: Grant
    Filed: July 21, 2015
    Date of Patent: July 10, 2018
    Assignee: Brandeis University
    Inventors: Lizbeth K. Hedstrom, Marcus J. Long, Ann Parrinello Lawson
  • Patent number: 10000511
    Abstract: This invention relates to compounds which selectively bind to the survival protein MCL-1 with high affinity and selectivity, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for modulating MCL-1 activity and for treating hyperproliferative disorders, angiogenesis disorders, cell cycle regulation disorders, autophagy regulation disorders, inflammatory disorders, and/or infectious disorders and/or for enhancing cellular engraftment and/or wound repair, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: May 6, 2015
    Date of Patent: June 19, 2018
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Loren D. Walensky, Michelle L. Stewart, Nicole Cohen
  • Patent number: 9994536
    Abstract: Embodiments of the present disclosure provide for compositions including a compound, pharmaceutical compositions including the compound, methods of treatment of a disease or related condition (e.g., neurological disease on condition), methods of treatment using compositions or pharmaceutical compositions, and the like.
    Type: Grant
    Filed: May 1, 2015
    Date of Patent: June 12, 2018
    Assignee: Torrey Pines Institute for Molecular Studies
    Inventors: Madepalli K. Lakshmana, Adel Nefzi, Richard Houghten, Dmitriy Minond
  • Patent number: 9884842
    Abstract: The present invention relates novel heterocyclic analogs of combretastatin, their synthesis, and their use as anti-cancer compounds. In particular, compounds of Formula (I), Formula (II), and Formula (V) are provided.
    Type: Grant
    Filed: April 15, 2014
    Date of Patent: February 6, 2018
    Assignee: BIOVENTURES, LLC
    Inventors: Narsimha Reddy Penthala, Peter Crooks, Vijayakumar Sonar
  • Patent number: 9856246
    Abstract: The invention relates to compounds acting as selective antagonists of Transient Receptor Potential cation channel subfamily M member 8 (TRPM8), and having formula: Said compounds are useful in the treatment of diseases associated with activity of TRPM8 such as pain, inflammation, ischaemia, neurodegeneration, stroke, psychiatric disorders, itch, irritable bowel diseases, cold induced and/or exacerbated respiratory disorders and urological disorders.
    Type: Grant
    Filed: January 25, 2017
    Date of Patent: January 2, 2018
    Assignee: Dompé farmaceutici S.p.A.
    Inventors: Alessio Moriconi, Gianluca Bianchini, Sandro Colagioia, Laura Brandolini, Andrea Aramini, Chiara Liberati, Silvia Bovolenta
  • Patent number: 9585875
    Abstract: The invention relates to compounds acting as selective antagonists of Transient Receptor Potential cation channel subfamily M member 8 (TRPM8), and having formula (I). Said compounds are useful in the treatment of diseases associated with activity of TRPM8 such as pain, inflammation, ischaemia, neurodegeneration, stroke, psychiatric disorders, itch, irritable bowel diseases, cold induced and/or exhacerbated respiratory disorders and urological disorders.
    Type: Grant
    Filed: December 19, 2012
    Date of Patent: March 7, 2017
    Assignee: DOMPÉ FARMACEUTICI S.P.A.
    Inventors: Alessio Moriconi, Gianluca Bianchini, Sandro Colagioia, Laura Brandolini, Andrea Aramini, Chiara Liberati, Silvia Bovolenta
  • Patent number: 9562040
    Abstract: Processes and intermediates for preparing rivaroxaban, and analogs and derivatives thereof, and pharmaceutically acceptable salts of each of the foregoing, are described herein.
    Type: Grant
    Filed: April 4, 2013
    Date of Patent: February 7, 2017
    Assignee: Indiana University Research and Technology Corporation
    Inventor: James R. McCarthy
  • Patent number: 9546155
    Abstract: The compound represented by the general formula: wherein ring A is benzene which may be substituted and the like; ring B is benzene which may be substituted and the like; X is a single bond and the like; Y is alkyl which may be substituted and the like; Z is CR1 or nitrogen atom; R1 is hydrogen and the like; R2 is alkyl which may be substituted and the like or a pharmaceutically acceptable salt thereof is useful as a prevention/treatment agent of obesity, diabetes, and the like.
    Type: Grant
    Filed: June 14, 2013
    Date of Patent: January 17, 2017
    Assignee: MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Kunio Saruta, Norimitsu Hayashi, Osamu Sakurai, Hiroaki Sawamoto, Eri Ooboki
  • Patent number: 9512143
    Abstract: The compounds provided herein are phenyl analine amides and are useful for inhibiting histone deacteylase (“HDAC”) enzymes, such as HDAC1, HDAC2, and HDAC3.
    Type: Grant
    Filed: January 16, 2015
    Date of Patent: December 6, 2016
    Assignee: BIOMARIN PHARMACEUTICAL INC.
    Inventors: Vincent Jacques, James R. Rusche, Norton P. Peet, Jasbir Singh
  • Patent number: 9493481
    Abstract: In one aspect, the invention relates to substituted 5-aminothieno[2,3-c]pyridazine-6 -carboxamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: February 23, 2013
    Date of Patent: November 15, 2016
    Assignee: Vanderbilt University
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, James C. Tarr, James M. Salovich, Michael S. Poslusney
  • Patent number: 9481659
    Abstract: Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds is provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.
    Type: Grant
    Filed: May 11, 2012
    Date of Patent: November 1, 2016
    Assignee: Celgene International II SÀRL
    Inventors: Marcus F. Boehm, Esther Martinborough, Enugurthi Brahmachary, Manisha Moorjani, Junko Tamiya, Liming Huang, Adam Richard Yeager
  • Patent number: 9453009
    Abstract: The present invention is directed to a process for preparing a 2,26,6-d4-morpholine derivative represented by Structural Formula (I): or a salt thereof.
    Type: Grant
    Filed: December 10, 2014
    Date of Patent: September 27, 2016
    Assignee: Concert Pharmaceuticals, Inc.
    Inventors: Julie F. Liu, Xuejun Tang, Scott L. Harbeson, Craig E. Masse
  • Patent number: 9422275
    Abstract: Certain embodiments of the present invention provide selected compounds having a molecular structure according to Formula 1: In Formula 1, Z is —CO—, —SO—, or —SO2—; Ar is phenyl, heteroaryl, or heterocycloalkyl; Het is heteroaryl; R is R?, X, or NR1R2; R? is R3, or OR3; R? is R4, or OR4; R1 and R2 are each independently H, alkyl, or acyl; R3 is H, heteroaryl, or alkyl; R4 is H, heteroaryl, or CnH2n+1 (n>2); and X is F, Br, I, CN, or NO2. In some embodiments, compounds having a molecular structure according to Formula 1 have the property of inhibiting a growth of a cell line selected from HeLa and MB468 with a sub-micromolar IC50.
    Type: Grant
    Filed: July 19, 2014
    Date of Patent: August 23, 2016
    Assignee: The Regents of the University of California
    Inventors: Wen-Hwa Lee, Jiewen Zhu, Chun-Mei Hu
  • Patent number: 9388174
    Abstract: The present invention provides: a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, which has an excellent inhibitory activity on xanthine oxidase and is useful as a therapeutic agent or a prophylactic agent for diseases associated with xanthine oxidase, such as gout, hyperuricemia, tumor lysis syndrome, urinary tract stone, hypertension, dyslipidemia, diabetes, cardiovascular diseases including arteriosclerosis and heart failure, renal diseases including diabetic nephropathy, respiratory diseases including chronic obstructive pulmonary disease, inflammatory bowel disease or autoimmune diseases; and a medicine or a pharmaceutical composition comprising the compound or the salt as an active ingredient.
    Type: Grant
    Filed: January 30, 2014
    Date of Patent: July 12, 2016
    Assignee: Teijin Pharma Limited
    Inventors: Asahi Kawana, Chikashi Kanazawa, Yoshimasa Takahashi, Takashi Shirakura
  • Patent number: 9376427
    Abstract: The present inventors have surprisingly found that rivaroxaban of formula I can be prepared in a one-pot process, in high purity and with high yield, by reacting 5-chlorothiophene-2-carboxylic acid or a salt thereof with a sulfonylating agent to produce a sulfonyl ester intermediate, which is then condensed with 4-[4-[(SS)-5-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl]morpholine-3-one or an acid addition salt thereof to produce rivaroxaban.
    Type: Grant
    Filed: May 2, 2012
    Date of Patent: June 28, 2016
    Assignee: Symed Labs Limited
    Inventors: Mohan Rao Dodda, Venkat Reddy Buthukuri
  • Patent number: 9247740
    Abstract: The present invention provides compounds of formula (I), wherein G1 is oxygen; R1 is hydrogen; R2 is group P (P) L is a bond, methylene or ethylene; one of A1 and A2 is S, SO or SO2 and the other is —C(R4)R4—R3 is hydrogen or methyl; each R4 is independently hydrogen or methyl; Y1 is C—R6, CH or nitrogen; Y2 and Y3 are independently CH or nitrogen; wherein no more than two of Y1, Y2 and Y3 are nitrogen and wherein Y2 and Y3 are not both nitrogen; R5 is hydrogen, halogen, cyano, nitro, NH2, C1-C2alkyl, C1-C2haloalkyl, C3-C5cycloalkyl, C3-C5halocycloalkyl, C1-C2alkoxy, C1-C2haloalkoxy; R6 together with R5 forms a —CH?CH—CH?CH— bridge; X2 is C—X6 or nitrogen; X1, X3 and X6 are independently hydrogen, halogen or trihalomethyl, wherein at least two of X1, X3 and X6 are not hydrogen; X4 is trifluoromethyl, difluoromethyl or chlorodifluoromethyl.
    Type: Grant
    Filed: August 24, 2012
    Date of Patent: February 2, 2016
    Assignee: Syngenta Participations AG
    Inventors: Jerome Yves Cassayre, Peter Renold, Thomas Pitterna, Myriem El Qacemi
  • Patent number: 9187506
    Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the NR2B NMDA receptor and may be useful for the treatment of various disorders of the central nervous system.
    Type: Grant
    Filed: January 7, 2015
    Date of Patent: November 17, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Lorin A. Thompson, III, John E. Macor
  • Patent number: 9073881
    Abstract: There are disclosed are compounds of the formula: wherein R1 and R2 are as disclosed herein, which are eIF4E inhibitors useful in the treatment of cancers. Also disclosed are compositions comprising the compounds, as well as methods of treating cancer using the compounds.
    Type: Grant
    Filed: September 5, 2012
    Date of Patent: July 7, 2015
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventor: Paul Gillespie
  • Publication number: 20150125527
    Abstract: The present invention relates to solid orally administrable pharmaceutical administration forms comprising 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}-methyl)-2-thiophenecarboxamide (rivaroxaban, active compound (I)), characterized in that a partial amount of the active compound (I) is released rapidly and a partial amount is released in a controlled manner (modified, retarded, delayed), and to processes for their preparation, their use as medicaments and their use for the prophylaxis, secondary prophylaxis or treatment of disorders.
    Type: Application
    Filed: June 28, 2013
    Publication date: May 7, 2015
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Klaus Benke, Heike Neumann, Wolfgang Mück
  • Publication number: 20150119376
    Abstract: The present invention relates to cycloalkenyl aryl derivatives, isomers thereof, pharmaceutically acceptable salts thereof, hydrates thereof, or solvates thereof; a method for preparing the derivatives; and pharmaceutical compositions containing the same. The compounds of the present invention show the effect of CETP activity inhibition. It means that the compounds can increase HDL-cholesterol and decrease LDL-cholesterol.
    Type: Application
    Filed: April 12, 2012
    Publication date: April 30, 2015
    Applicant: CHONG KUN DANG PHARMACEUTICAL CORP.
    Inventors: SeoHee LEE, JungTaek OH, JaeKwang LEE, JaeWon LEE, Suyeal BAE, Nina HA, Sera LEE
  • Publication number: 20150111866
    Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol and reducing LDL-cholesterol in human patients and for treating or preventing atherosclerosis.
    Type: Application
    Filed: April 26, 2013
    Publication date: April 23, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: John J. Acton, III, Feng Ye, Petr Vachal, Deyou Sha, James F. Dropinski, Lin Chu, Debra Ondeyka, Alexander J. Kim, Vincent J. Colandrea, Yi Zang, Fengqi Zhang, Guizhen Dong
  • Publication number: 20150105392
    Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Paul R. Fatheree, Robert Murray McKinnell
  • Publication number: 20150105391
    Abstract: Certain embodiments of the present invention provide selected compounds having a molecular structure according to Formula 1: In Formula 1, Z is —CO—, —SO—, or —SO2—; Ar is phenyl, heteroaryl, or heterocycloalkyl; Het is heteroaryl; R is R?, X, or NR1R2; R? is R3, or OR3; R? is R4, or OR4; R1 and R2 are each independently H, alkyl, or acyl; R3 is H, heteroaryl, or alkyl; R4 is H, heteroaryl, or CnH2n+1 (n>2); and X is F, Br, I, CN, or NO2. In some embodiments, compounds having a molecular structure according to Formula 1 have the property of inhibiting a growth of a cell line selected from HeLa and MB468 with a sub-micromolar IC50.
    Type: Application
    Filed: July 19, 2014
    Publication date: April 16, 2015
    Inventors: Wen-Hwa Lee, Jiewen Zhu, Chun-Mei Hu
  • Publication number: 20150099719
    Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
    Type: Application
    Filed: October 6, 2014
    Publication date: April 9, 2015
    Inventors: Shawn Stachel, Daniel V. Paone, Jing Li, Kausik Nanda
  • Publication number: 20150099714
    Abstract: The present invention is directed to a process for preparing a 2,26,6-d4-morpholine derivative represented by Structural Formula (I): or a salt thereof.
    Type: Application
    Filed: December 10, 2014
    Publication date: April 9, 2015
    Inventors: Julie F. Liu, Xuejun Tang, Scott L. Harbeson, Craig E. Masse
  • Patent number: 9000010
    Abstract: The invention relates to compounds corresponding to the general formula (I): in which R2 represents a hydrogen, fluorine, hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy or —NR8R9; n and m represent, independently of one another, an integer equal to 1, 2 or 3, it being understood that the sum m+n is at most equal to 5; A represents a covalent bond, an oxygen, a C1-6-alkylene or —O—C1-6-alkylene; R1 represents a phenyl or a heterocycle which is optionally substituted; R3 represents a hydrogen, fluorine, C1-6-alkyl or trifluoromethyl; R4 represents an optionally substituted 5-membered heterocycle; in the form of the base or of an addition salt with an acid; with the exclusion of 5-methylisoxazol-3-ylmethyl 4-hydroxy-4-(4-chlorophenyl)piperidine-1-carboxylate. The invention also relates to a process for the preparation of the compounds of formula (I), to compositions comprising them and to their therapeutic application.
    Type: Grant
    Filed: January 19, 2011
    Date of Patent: April 7, 2015
    Assignee: Sanofi
    Inventors: Ahmed Abouabdellah, Antoine Ravet
  • Patent number: 8999983
    Abstract: Compounds, compositions, and methods for modulation of Hec1/Nek2 interaction are provided. Such compounds disrupt Nek2/Hec1 binding and may be useful as chemotherapeutic agents for neoplastic diseases.
    Type: Grant
    Filed: November 29, 2012
    Date of Patent: April 7, 2015
    Assignees: Taivex Therapeutics Corporation, Development Center of Biotechnology
    Inventors: Jiann-Jyh Huang, Shih-Hsien Chuang, Ying-Shuan Eda Lee, Yu-Ling Huang, Johnson Lau
  • Publication number: 20150093437
    Abstract: The present invention relates to a novel pharmaceutical composition of Linezolid. The present invention relates to a novel pharmaceutical composition comprising Linezolid Form III along with pharmaceutically acceptable excipients and a process to prepare the said composition. The present invention relates to an oral dosage forms for the treatment of severe infections caused by Gram-positive bacteria.
    Type: Application
    Filed: August 2, 2013
    Publication date: April 2, 2015
    Inventors: Aditi Panandikar, Sundeep Bambolkar, Kavita Inamdar, Sapna Ramesh, Amol Burkul, Nasir Shaikh
  • Patent number: 8993567
    Abstract: Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders.
    Type: Grant
    Filed: March 27, 2014
    Date of Patent: March 31, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jagabandhu Das, Ramesh Padmanabha, Ping Chen, Derek Norris, Arthur M. P. Doweyko, Joel C. Barrish, John Wityak
  • Patent number: 8993573
    Abstract: Novel compounds selected from 2-(3-aminoaryl)amino-4-aryl-thiazoles of formula (I) that selectively modulate, regulate, and/or inhibit signal transductions mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferative metabolic, allergic and degenerative disorders. More particularly, these compounds are potent and selective c-kit inhibitors.
    Type: Grant
    Filed: November 26, 2013
    Date of Patent: March 31, 2015
    Assignee: AB Science
    Inventors: Marco Ciufolini, Camille Wermuth, Bruno Giethlen, Alain Moussy
  • Patent number: 8993556
    Abstract: The present invention relates to substituted resorcinol derivatives which inhibit the activity of Heat Shock Protein HSP90. The compounds of the invention are therefore useful in treating proliferative diseases such as cancer and neurodegenerative diseases. The present invention also provides processes for preparing these compounds, pharmaceutical compositions comprising them, methods of treating diseases and the pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: April 16, 2010
    Date of Patent: March 31, 2015
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Maria Gabriella Brasca, Elena Casale, Ron Ferguson, Paolo Polucci, Fabio Zuccotto
  • Publication number: 20150087648
    Abstract: The present invention relates to substituted 2-(chroman-6-yloxy)-thiazoles of the formula I, in which Ar, R2, R3 and R4 are as defined in the claims. The compounds of the formula I are inhibitors of the sodium-calcium exchanger (NCX), especially of the sodium-calcium exchanger of subtype 1 (NCX1), and are suitable for the treatment of diverse disorders in which intracellular calcium homeostasis is disturbed, such as arrhythmias, heart failure and stroke. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Application
    Filed: November 10, 2014
    Publication date: March 26, 2015
    Inventors: Werngard CZECHTIZKY, John WESTON, Nils RACKELMANN, Michael PODESCHWA, Petra ARNDT, Klaus WIRTH, Heinz GOEGELEIN, Olaf RITZELER, Volker KRAFT, Patrice BELLEVERGUE, Gary McCORT
  • Patent number: 8987313
    Abstract: The present application provides for a compound of formula I, or a salt thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods that include the administration of such compounds with at least one additional therapeutic agent.
    Type: Grant
    Filed: December 20, 2011
    Date of Patent: March 24, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Manoj C. Desai, Hon Chung Hui, Hongtao Liu, Jianyu Sun, Lianhong Xu
  • Publication number: 20150080382
    Abstract: This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.
    Type: Application
    Filed: June 24, 2014
    Publication date: March 19, 2015
    Inventors: Damian O. Arnaiz, Greg Brown, Emmanuel Claret, Arwed Cleve, David Davey, William Guilford, Seock-Kyu Khim, Thomas Kirkland, Monica J. Kochanny, Amy Liang, David Light, John Parkinson, Guo Ping Wei, Bin Ye
  • Publication number: 20150080399
    Abstract: Disclosed are compressed tablets containing atazanavir sulfate and an acidifying agent, optionally with another active agent, e.g., anti-HIV agents, and optionally with precipitation retardant agents. Also disclosed are processes for making the tablets, and methods of treating HIV.
    Type: Application
    Filed: November 25, 2014
    Publication date: March 19, 2015
    Inventors: FARANAK NIKFAR, Munir Alwan Hussain, Feng Qian
  • Patent number: 8980892
    Abstract: A compound of formula (I): wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5a, R5b and R6 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.
    Type: Grant
    Filed: February 18, 2010
    Date of Patent: March 17, 2015
    Assignees: Syngenta Crop Protection LLC, Syngenta Limited
    Inventors: Peter Renold, Thomas Pitterna, Jerome Yves Cassayre, Myriem El Qacemi
  • Publication number: 20150072976
    Abstract: Provided herein are Substituted Benzamides, compositions, and method of their manufacture and use.
    Type: Application
    Filed: April 11, 2013
    Publication date: March 12, 2015
    Inventors: Amato Giaccia, Edwin Lai, Olga Razorenova, Denise Chan, Michael Patrick Hay, Muriel Bonnet, Connie Sun, Ray Tabibiazar, Po-wai Yuen
  • Publication number: 20150065507
    Abstract: The present invention is directed to novel retinoid-related orphan receptor gamma (ROR?) modulators, processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by ROR?.
    Type: Application
    Filed: April 25, 2013
    Publication date: March 5, 2015
    Applicant: Glaxo Group Limited
    Inventors: Veronique Birault, Amanda Jennifer Campbell, Stephen Harrison, Joelle Le, Lena Shukla
  • Publication number: 20150057280
    Abstract: The invention relates to pyridylidene compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to methods and uses of these N-substituted pyridylidene compounds, and of compositions comprising thereof, for combating and controlling animal pests. Furthermore the invention relates also to pesticidal methods of applying such N-substituted pyridylidene compounds. The N-substituted pyridylidene compounds of the present invention are defined by the following formula I: wherein X, Het, R1, R2, R3, R4 and R6 are defined as in the description.
    Type: Application
    Filed: March 27, 2013
    Publication date: February 26, 2015
    Applicant: BASF SE
    Inventors: Nina Gertrud Bandur, Ralph Paulini, Florian Kaiser, Arun Narine, Joachim Dickhaut, Karsten Korber
  • Publication number: 20150057281
    Abstract: Compounds, compositions, and methods for modulation of Hec1/Nek2 interaction are provided. Especially preferred compounds disrupt Nek2/Hec1 binding and are therefore useful as chemotherapeutic agent for neoplastic diseases.
    Type: Application
    Filed: October 29, 2014
    Publication date: February 26, 2015
    Inventors: Johnson LAU, Jiann-Jyh HUANG
  • Publication number: 20150057282
    Abstract: The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2 are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.
    Type: Application
    Filed: October 31, 2014
    Publication date: February 26, 2015
    Applicant: SAREUM LIMITED
    Inventors: John Charles READER, John Mark ELLARD, Helen BOFFEY, Susanne TAYLOR, Andrew David CARR, Michael CHERRY, Michelle WILSON, Richard Boakye OWOARE