Additional Hetero Ring Attached Directly Or Indirectly To The 1,4-thiazine By Nonionic Bonding Patents (Class 514/227.8)
  • Patent number: 10376598
    Abstract: The present invention provides pharmacological compounds including an effector moiety conjugated to a binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.
    Type: Grant
    Filed: April 26, 2016
    Date of Patent: August 13, 2019
    Assignee: MADRIGAL PHARMACEUTICALS, INC.
    Inventors: Dinesh U. Chimmanamada, Weiwen Ying
  • Patent number: 10351549
    Abstract: The present invention relates to amide derivatives having dual pharmacological activity towards both the sigma (?) receptor, and the ?-opioid receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
    Type: Grant
    Filed: July 28, 2016
    Date of Patent: July 16, 2019
    Assignee: LABORATORIOS DEL DR. ESTEVE S.A.
    Inventors: Monica Garcia-Lopez, Carmen Almansa-Rosales
  • Patent number: 10299475
    Abstract: To provide a compound highly active against pests, a pesticide using the compound, and a method for controlling pests by applying the compound. A phenoxyalkylbenzamide compound represented by the formula (I) or its salt; a pesticide containing it as an active ingredient, and a controlling method, which comprises applying an effective amount of the compound: wherein R1, Y and R3 are a hydrogen atom or the like, and Ar is as follows: wherein R4 and R7 are halogen or the like, R5 and R6 are a hydrogen atom or the like, m is from 0 to 5, and n is from 0 to 3.
    Type: Grant
    Filed: August 22, 2014
    Date of Patent: May 28, 2019
    Assignee: ISHIHARA SANGYO KAISHA, LTD.
    Inventors: Koji Higuchi, DamdinSuren Boldbaatar, Yuta Tazawa, Michiko Kanuma
  • Patent number: 10280146
    Abstract: The present invention relates to pyrimidone compounds used as Lp-PLA2 inhibitors and pharmaceutical compositions thereof. The structure of the pyrimidone compounds is represented by general formula (I), wherein R1, R2, R3, X, Ar, Y and n are defined as in the specification and claims. The compounds of general formula (I) in the present invention, stereoisomers and pharmaceutically acceptable salts thereof can be used as Lp-PLA2 inhibitors for preventing, treating and/or ameliorating diseases associated with the activity of Lp-PLA2 enzyme.
    Type: Grant
    Filed: December 28, 2015
    Date of Patent: May 7, 2019
    Assignee: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Jianhua Shen, Yiping Wang, Xinde Chen, Wenwei Xu, Kai Wang
  • Patent number: 10245255
    Abstract: Provided herein are compositions and methods for the treatment of obesity and related disorders, including, but not limited to insulin resistance, diabetes, and hepatic steatosis. For example, in some embodiments, pharmaceutically acceptable compositions and methods are provided employing amlexanox, a derivative thereof, or a pharmaceutically acceptable salt thereof, alone or in combination with other agents and/or medical interventions, for the treatment, prevention, and management of such diseases and conditions.
    Type: Grant
    Filed: February 14, 2012
    Date of Patent: April 2, 2019
    Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Alan R. Saltiel, Stuart Decker
  • Patent number: 10183009
    Abstract: The present invention relates to compounds of formula (I): and to salts thereof, wherein R1, R2, and Q have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of bromodomains. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various bromodomain-mediated disorders.
    Type: Grant
    Filed: May 10, 2017
    Date of Patent: January 22, 2019
    Assignees: GENENTECH, INC., CONSTELLATION PHARMACEUTICALS, INC.
    Inventors: Brian K. Albrecht, Steven F. Bellon, Daniel J. Burdick, Alexandre Cote, Terry Crawford, Les A. Dakin, Vickie Hsiao-Wei Tsui, Michael Charles Hewitt, Yves LeBlanc, Steven R. Magnuson, Christopher G. Nasveschuk, F. Anthony Romero, Yong Tang, Alexander M. Taylor, Shumei Wang
  • Patent number: 10137132
    Abstract: This invention relates to stable pharmaceutical compositions for parenteral administration comprising dopamine agonists and peripheral acting agents useful for treatment of metabolic disorders or key elements thereof. The parenteral dosage forms exhibit long stable shelf life and distinct pharmacokinetics.
    Type: Grant
    Filed: May 7, 2014
    Date of Patent: November 27, 2018
    Assignee: VeroScience, LLC
    Inventor: Anthony H. Cincotta
  • Patent number: 10112898
    Abstract: The present invention relates to an improved process for the preparation of pyrroles derivatives having hypolipidemic and hypocholesteremic activities. In particular, the invention relates to an improved process for the preparation of 2-ethoxy-3-(4-(2-(2-methyl-5-(4-(methylthio)phenyl)-1H-pyrrol-1-yl)ethoxy)phenyl)propanoate and its pharmaceutically acceptable salts, hydrates, solvates, polymorphs or intermediates thereof. The invention also relates to an improved process for the preparation of mesylate compound (A1).
    Type: Grant
    Filed: September 5, 2014
    Date of Patent: October 30, 2018
    Assignee: Cadila Healthcare Limited
    Inventors: Shri Prakash Dhar Dwivedi, Ramesh Chandra Singh, Jagdish Maganlal Patel, Vikas Patel, Vishwadeepak Rama Pati Tripathi, Pranav Jitendra Gangwar, Jigar Mukundbhai Raval
  • Patent number: 10080725
    Abstract: Synthetically-derived S,S-heterodisubstituted disulfides that exhibit potent in vitro antibacterial activity against a variety of bacteria, including Staphylococcus aureus, methicillin-resistant Staphylococcus aureus and Francisella tularensis. The present invention provides compounds, methods and compositions effective to treat microbial/bacterial infections, and, especially, infections arising from bacteria which have developed resistance to conventional antibiotics.
    Type: Grant
    Filed: November 11, 2016
    Date of Patent: September 25, 2018
    Assignee: University of South Florida
    Inventors: Edward Turos, Praveen Ramaraju
  • Patent number: 10053455
    Abstract: The present invention is concerned with substituted oxazole derivatives that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant protein kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, autoimmune, allergic, and degenerative disorders. In particular, the presently disclosed compounds are Syk inhibitors.
    Type: Grant
    Filed: March 23, 2015
    Date of Patent: August 21, 2018
    Assignee: AB SCIENCE
    Inventors: Abdellah Benjahad, Jason Martin, Claire Schalon, Didier Pez, Emmanuel Chevenier, Franck Sandrinelli, Willy Picoul, Alain Moussy
  • Patent number: 10040785
    Abstract: The present invention concerns compounds of formula (I) or an N-oxide or salt thereof and their use for controlling parasites in and on warm-blooded animals or fish.
    Type: Grant
    Filed: February 5, 2018
    Date of Patent: August 7, 2018
    Assignee: Elanco Tiergesundheit AG
    Inventors: Noëlle Gauvry, Thomas Goebel, Steve Nanchen, Jean-Luc Perret, Ulrich Roos, Sandra Schorderet Weber
  • Patent number: 10017470
    Abstract: The present invention provides a therapeutic compound of formula (I) and their pharmaceutically acceptable salts for the prevention and treatment of lipodystrophy caused because of HIV infection or combination therapy of HIV-1 protease inhibitors (Pis) and/or reverse transcriptase inhibitors (nRTIs) by neutralizing lipohypertrophy, lipoatrophy and metabolic abnormalities in HIV patient.
    Type: Grant
    Filed: January 30, 2012
    Date of Patent: July 10, 2018
    Assignee: Cadila Healthcare Limited
    Inventors: Dhiraj Gambhire, Rajendrakumar Hariprasad Jani, Bipin Pandey, Kaushik Sata, Himanshu Kothari, Pankaj Ramanbhai Patel
  • Patent number: 10006913
    Abstract: Heteroaryldihydropyrimidine (HAP)-based fluorescent stains (compounds), as well as uses of such stains as diagnostic reagents, viral-tracking agents, and/or tools for drug discovery are described. The present invention relates to heteroaryldihydropyrimidine (HAP)-based fluorescent stains (compounds), as well as uses of such stains as diagnostic reagents, viral-tracking agents, and/or tools for drug discovery.
    Type: Grant
    Filed: March 20, 2014
    Date of Patent: June 26, 2018
    Assignee: Indiana University Research and Technology Corporation
    Inventors: Adam Zlotnick, Lichun Li, Michael S. Van Nieuwenhze, William W. Turner
  • Patent number: 9951087
    Abstract: The present invention relates to arylcarbonyl and heteroarylcarbonyl anthranilate compounds that may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment disorders.
    Type: Grant
    Filed: June 4, 2015
    Date of Patent: April 24, 2018
    Assignee: Fibrotech Therapeutics PTY LTD
    Inventors: Spencer John Williams, Steven Zammit, Darren James Kelly
  • Patent number: 9908884
    Abstract: The present invention relates to novel pyrimidine, pyrrolo-pyrimidine, pyrrolo-pyridine, pyridine, purine and triazine compounds which are able to modulate epidermal growth factor receptor (EGFR), including Her-kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.
    Type: Grant
    Filed: May 5, 2010
    Date of Patent: March 6, 2018
    Assignee: DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Nathanael S. Gray, Pasi Janne, Michael J. Eck, Wenjun Zhou
  • Patent number: 9902709
    Abstract: The present invention provides a polysubstituted pyridine compound of Formula I, a preparation method, a use and a pharmaceutical composition thereof. The polysubstituted pyridine compound of Formula I according to the present invention has an excellent anti-tumor effect, can inhibit various cell kinases simultaneously, has significantly excellent pharmacokinetic characteristics, and is very suitable for oral and intravenous administration. The pharmaceutical composition according to the present invention can be useful for treating tumors and cancers.
    Type: Grant
    Filed: December 30, 2014
    Date of Patent: February 27, 2018
    Assignees: PEKING UNIVERSITY FOUNDER GROUP CO., LTD., PKUCARE PHARMACEUTICAL R & D CENTER, PKU HEALTHCARE INDUSTRY GROUP CO., LTD.
    Inventors: Chongqin Yi, Heng Xu, Jing Tao, Songwen Lin, Fangbin Han
  • Patent number: 9856247
    Abstract: The invention provides novel compounds having the general formula: wherein R1, R2, R3, R4, R5, M and X are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Grant
    Filed: August 28, 2015
    Date of Patent: January 2, 2018
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Lei Guo, Xianfeng Lin, Haixia Liu, Zongxing Qiu, Hong Sheng, Guozhi Tang, Guolong Wu, Weixing Zhang, Wei Zhu
  • Patent number: 9776988
    Abstract: A compound represented by the general Formula (I), wherein hydrogen atoms shown as attached to pyrazole and benzimidazole rings are attached to one of nitrogen atoms of the pyrazole or benzimidazole ring, respectively; R1 represents —X-Q-P, wherein X is absent or represents —CH2—, —C(O)—, or —C(O)NH—(CH2)k—, wherein k is 0, 1 or 2; Q is selected from the group consisting of Q1, Q2, Q3, Q4 and Q5; P is absent or represents straight- or branched-chain C1-C3 alkyl, —(CH2)l—NR2R3, or —(CH2)m—C(O)—NR2R3, wherein l and m independently of each other represent 0, 1 or 2, with the proviso that when B in Q1 represents oxygen atom, then P is absent; and R2 and R3 independently represent C1 or C2 alkyl, or R2 and R3 together with nitrogen atom to which they are both attached form a 6-membered saturated heterocyclic ring, wherein one of carbon atoms can be replaced with oxygen, —NH— or —N(C1-C2)alkyl-; and acid addition salts thereof. The compound can be useful in the treatment of cancer diseases.
    Type: Grant
    Filed: March 7, 2014
    Date of Patent: October 3, 2017
    Assignee: Celon Pharma S.A.
    Inventors: Daria Zdzalik, Joanna Lipner, Maciej Wieczorek, Karolina Dzwonek, Abdellah Yamani, Krzysztof Dubiel, Monika Lamparska-Przybysz, Paulina Grygielewicz, Aleksandra Stanczak
  • Patent number: 9725465
    Abstract: Biaryl acetamide compounds and compositions and their methods of use are provided for modulating the activity of class III receptor tyrosine kinases and for the treatment, prevention or amelioration of one or more symptoms of disease of disorder mediated by class III receptor tyrosine kinases.
    Type: Grant
    Filed: August 29, 2014
    Date of Patent: August 8, 2017
    Assignee: Ambit Biosciences Corporation
    Inventors: Mark W. Holladay, Gang Liu, Martin W. Rowbottom
  • Patent number: 9688688
    Abstract: Described herein are certain crystalline forms of 4-((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-6-methoxyquinazolin-7-yl)oxy)-1-(2-oxa-7-azaspiro[3.5]nonan-7-yl)butan-1-one, as well as pharmaceutical compositions employing the crystalline forms. Also provided are particles (e.g., nanoparticles) comprising such crystalline forms or pharmaceutical compositions. In certain examples, the particles are mucus penetrating particles (MPPs). Also described are methods of treating and/or preventing diseases using the crystalline forms or pharmaceutical compositions described herein.
    Type: Grant
    Filed: November 3, 2014
    Date of Patent: June 27, 2017
    Assignee: Kala Pharmaceuticals, Inc.
    Inventors: Elizabeth Enlow, Minh Ngoc Nguyen, Winston Z. Ong
  • Patent number: 9630928
    Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, X is CH or N; Y is C(O) or S(O)2; provided that when Y is S(O)2, then X is CH; A is a radical selected from the group consisting of and B1, B2, B3, T, R1, R2 R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and R13 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: September 30, 2015
    Date of Patent: April 25, 2017
    Assignee: E. I. DU PONT DE NEMOURS AND COMPANY
    Inventors: Thomas Paul Selby, Brenton Todd Smith, Andrew Edmund Taggi
  • Patent number: 9567310
    Abstract: The present invention relates to compound of general formula (1) wherein R1 represents C6-C10 aryl comprising one or two fused rings, wherein from 2 to 5 carbon atoms may be replaced with a heteroatom selected from O, S and NR6, and eventually substituted with from 5 to 11 substituents selected from R6, halo, CN, NO2, CF3, OCF3, COOR6, OCOR6, SO2NR6R7, CONR6R7, NR6R7, NR6COR7, (CH2)p—NR6R7, (CH2)p—OR6 and (CH2)pSR6, as well as, if appropriate, their pharmaceutically acceptable salts and/or isomers, tautomers, solvates or isotopic variations thereof. The compounds are useful for the treatment of cancers.
    Type: Grant
    Filed: November 8, 2013
    Date of Patent: February 14, 2017
    Assignees: INSERM (INSTITUT NATIONAL DE LA SANTE ET DE LA RECHARCHE MEDICALE), UNIVERSITE NICE SOPHIA ANTIPOLIS, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS)
    Inventors: Stephane Rocchi, Robert Ballotti, Rachid Benhida, Michael Cerezo, Maria Duca, Jean-Patrick Joly
  • Patent number: 9527829
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic diseases. Provided herein are substituted imidazole-pyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase enzymes. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: December 27, 2016
    Assignee: Celgene Quanticel Research, Inc.
    Inventors: Toufike Kanouni, Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal
  • Patent number: 9428462
    Abstract: The present invention relates to solid forms having a low degree of crystallinity or substantially amorphous of the hydrochloride salt of 4-[2-[[5-methyl-1-(2-naphthalenyl)-1H-pyrazol-3-yl]oxy]ethyl]morpholine (P027) and processes for their preparation.
    Type: Grant
    Filed: August 8, 2011
    Date of Patent: August 30, 2016
    Assignee: LABORATORIOS DEL DR. ESTEVE, S.A.
    Inventors: Jordi Benet Buchholz, Laura Puig Fernandez
  • Patent number: 9428589
    Abstract: Described herein are compounds and methods for tethering proteins. For example, dimers of proteins, including SOD1 and DJ-1, are described, where the dimers are formed by the covalent bonding of a cysteine on the first monomer to a cysteine on the second monomer via a cyclic disulfide linker. The covalently attached dimers exhibit increased stabilization.
    Type: Grant
    Filed: November 15, 2013
    Date of Patent: August 30, 2016
    Assignee: Brandeis University
    Inventors: Jeffrey N. Agar, Joseph Salisbury
  • Patent number: 9365567
    Abstract: Imidazoquinoline compounds with an alkoxy substituent at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, methods of making, and methods of use of these compounds as immunomodulators, for inducing or inhibiting cytokine biosynthesis in animals and in the treatment of diseases including viral, and neoplastic, are disclosed.
    Type: Grant
    Filed: September 30, 2014
    Date of Patent: June 14, 2016
    Assignee: 3M Innovative Properties Company
    Inventors: Kyle J. Lindstrom, Bryon A. Merrill, Chad A. Haraldson, Michael J. Rice, Tushar A. Kshirsagar, Philip D. Heppner, Joshua R. Wurst, Shri Niwas, Sarah J. Slania
  • Patent number: 9340549
    Abstract: Compounds of Formula (I) and Formula (II) are useful inhibitors of tankyrase. Compounds of Formula (I) and Formula (II) have the following structure: where the definitions of the variables are provided herein.
    Type: Grant
    Filed: March 1, 2013
    Date of Patent: May 17, 2016
    Assignee: AMGEN INC.
    Inventors: Howard Bregman, John L. Buchanan, Nagasree Chakka, Erin F. Dimauro, Hakan Gunaydin, Angel Guzman-Perez, Zihao Hua, Hongbing Huang, Xin Huang, Matthew W. Martin, Vinod F. Patel
  • Patent number: 9326976
    Abstract: Compounds of formula (I) defined herein are both phosphodiesterase 4 (PDE4) enzyme inhibitors and muscarinic M3 receptor antagonists and are useful for the prevention and/or treatment of diseases of the respiratory tract.
    Type: Grant
    Filed: May 28, 2015
    Date of Patent: May 3, 2016
    Assignee: CHIESI FARMACEUTICI S.p.A.
    Inventors: Elisabetta Armani, Gabriele Amari, Carmelida Capaldi, Charles Baker-Glenn
  • Patent number: 9242969
    Abstract: The present invention provides compounds of Formula (I) as described herein, and salts thereof, and therapeutic uses of these compounds for treatment of disorders associated with Raf kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent.
    Type: Grant
    Filed: March 11, 2014
    Date of Patent: January 26, 2016
    Assignee: Novartis AG
    Inventors: Paul A. Barsanti, Matthew Burger, Yan Lou, Gisele Nishiguchi, Valery Polyakov, Savithri Ramurthy, Alice Rico, Lina Setti, Aaron Smith, Benjamin Taft, Huw Tanner, Alan DiPesa, Naeem Yusuff
  • Patent number: 9233956
    Abstract: The present invention provides thiazole sulfonamide and oxazole sulfonamide compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.
    Type: Grant
    Filed: November 25, 2013
    Date of Patent: January 12, 2016
    Assignee: Novartis AG
    Inventor: Tara Renae Rheault
  • Patent number: 9200076
    Abstract: The present invention relates to diagnostic imaging and in particular to the diagnostic imaging and therapy of cancer by means of compositions which specifically target the FSH Receptor expressed by tumor endothelial cells and circulating blood cells.
    Type: Grant
    Filed: July 17, 2014
    Date of Patent: December 1, 2015
    Assignees: INSERM (INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE), ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI
    Inventors: Nicolae Ghinea, Aurelian Radu
  • Patent number: 9192681
    Abstract: The invention relates to (among other things) oligomer-amino acid conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over un-conjugated amino acid compounds.
    Type: Grant
    Filed: February 24, 2010
    Date of Patent: November 24, 2015
    Assignee: NEKTAR THERAPEUTICS
    Inventors: Xuyuan Gu, Jennifer Riggs-Sauthier
  • Patent number: 9193697
    Abstract: The present invention is directed to certain Oxazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease.
    Type: Grant
    Filed: April 4, 2011
    Date of Patent: November 24, 2015
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: ZhiQiang Yang, Philippe G. Nantermet, Constantine Kreatsoulas, Keith P. Moore, Evan Foster Shalen
  • Patent number: 9187455
    Abstract: The present invention is concerned with novel pyridazinone derivatives of formula (I) wherein R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as pharmaceuticals.
    Type: Grant
    Filed: February 16, 2010
    Date of Patent: November 17, 2015
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Daniela Alberati, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Rosa Maria Rodriguez Sarmiento, Mark Rogers-Evans, Markus Rudolph
  • Patent number: 9051275
    Abstract: The present invention relates to polymorphs and solvates of the hydrochloride salt of 4-[2-[[5-methyl-1-(2-naphthalenyl)-1H-pyrazol-3-yl]oxy]ethyl]morpholine (P027), processes for their preparation, and to pharmaceutical compositions comprising them.
    Type: Grant
    Filed: February 4, 2011
    Date of Patent: June 9, 2015
    Assignee: Laboratories Del Dr. Esteve, S.A.
    Inventors: Ramón Berenguer Maimó, Jorge Medrano Rupérez, Jordi Benet Buchholz, Laura Puig Fernandez, Laia Pellejà Puxeu
  • Patent number: 9045445
    Abstract: The compounds of the present invention are represented by the following formula (I): wherein the substituents R1, R2, R3, R4, (R5)m, R6, A, X, and Y are as defined herein. The compounds are useful in methods of treating a disorder which is created by or is dependent upon inhibiting GlyT-1.
    Type: Grant
    Filed: June 2, 2011
    Date of Patent: June 2, 2015
    Assignee: Albany Molecular Research, Inc.
    Inventors: Christopher L. Cioffi, Mark A. Wolf, Peter R. Guzzo, Shuang Liu, Kashinath Sadalapure
  • Patent number: 9040516
    Abstract: The present invention provides: an uracil derivative represented by general formula (I) or a physiologically acceptable salt thereof (in the formula, R1 represents a hydrogen atom, a C1-10 alkyl group, a C2-6 alkene group or a 3- to 6-membered saturated or 4- to 6-membered unsaturated aliphatic ring group which may contain 1 to 2 hetero atoms independently selected from the group consisting of N, O and S; R2 represents a hydrogen atom, a halogen atom, a cyano group, —NRcRd, —N?CHN(CH3)2, or an C1-3 alkyl group; Ar1 and Ar2 independently represent a 5- to 6-membered aromatic ring group which may contain 1 to 3 hetero atoms independently selected from the group consisting of N, O and S; and L represents a 6-membered aromatic ring group which may contain 1 to 4 nitrogen atoms, a pyrazole group, a triazole group, or an imidazole group); and a therapeutic agent or prophylactic agent for various inflammatory diseases associated with elastase, comprises the compound or the like as an active ingredient.
    Type: Grant
    Filed: July 31, 2012
    Date of Patent: May 26, 2015
    Assignee: SUMITOMO DAINIPPON PHARMA CO., LTD.
    Inventors: Tomoya Shiro, Masanori Tobe, Katsumi Kubota, Yosuke Takanashi, Tomoaki Nakamura, Toshihiko Sone
  • Publication number: 20150140089
    Abstract: The present invention relates to a novel formulation of sustained-release Nifurtimox with enhanced activity while having low toxicity. The formulation can improve patient compliance by reducing the frequency of administering the drug.
    Type: Application
    Filed: May 8, 2013
    Publication date: May 21, 2015
    Inventors: Danong Chen, Glenn Rice
  • Publication number: 20150141413
    Abstract: The present invention provides a compound of formula I having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.
    Type: Application
    Filed: May 21, 2013
    Publication date: May 21, 2015
    Inventors: Hans Hilpert, Thomas Woltering
  • Patent number: 9034869
    Abstract: This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic[4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Grant
    Filed: March 7, 2013
    Date of Patent: May 19, 2015
    Assignee: Medivation Technologies, Inc.
    Inventors: David T. Hung, Andrew Asher Protter, Sarvajit Chakravarty, Rajendra Parasmal Jain
  • Patent number: 9029364
    Abstract: The present invention is directed to 2,5-disubstituted thiomorpholine amide compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2,5-disubstituted thiomorpholine amide compounds described herein in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: October 16, 2012
    Date of Patent: May 12, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Christina Di Marco
  • Publication number: 20150126499
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound.
    Type: Application
    Filed: January 7, 2015
    Publication date: May 7, 2015
    Inventors: Joseph Burlison, Shijie Zhang, Weiwen Ying, Dinesh U. Chimmanamada, Minghu Song, Junghyun Chae, Stefan M. Schweizer
  • Publication number: 20150126500
    Abstract: Provided are piperazinyl pyrimidine derivatives of formula I having CCR4 antagonism, and the preparation method, pharmaceutical composition and use thereof in the preparation of a medicament. The medicament is useful for the treatment and prevention of CCR4-related diseases.
    Type: Application
    Filed: January 15, 2013
    Publication date: May 7, 2015
    Inventors: Song Li, Ying Wang, Junhai Xiao, Dalong Ma, Hongwei Gong, Hui Qi, Lili Wang, Xiaomei Ling, Zhibing Zheng, Yang Zhang, Wu Zhong, Meina Li, Yunde Xie, Enquan Xu, Xingzhou Li, Jing Ma, Guoming Zhao, Xinbo Zhou, Xiaokui Wang, Hongying Liu
  • Publication number: 20150111879
    Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.
    Type: Application
    Filed: December 24, 2014
    Publication date: April 23, 2015
    Applicants: CURIS, INC., GENENTECH, INC.
    Inventors: Janet L. GUNZNER, Daniel P. SUTHERLIN, Mark S. STANLEY, Liang BAO, Georgette M. CASTANEDO, Rebecca L. LALONDE, Shumei WANG, Mark E. REYNOLDS, Scott J. SAVAGE, Kimberly MALESKY, Michael S. DINA, Michael F.T. KOEHLER
  • Publication number: 20150105378
    Abstract: The present invention provides compounds of Formula (I) or Formula (III): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Inventors: Lynn Abell, Leonard Adam, Cullen L. Cavallaro, Heather Finlay, Todd J. Friends, Jon J. Hangeland, Ji Jiang, R. Michael Lawrence, John Lloyd, Zulan Pi, George O. Tora, Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
  • Patent number: 9006234
    Abstract: This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic[4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Grant
    Filed: July 2, 2012
    Date of Patent: April 14, 2015
    Assignee: Medivation Technologies, Inc.
    Inventors: Rajendra Parasmal Jain, Sarvajit Chakravarty
  • 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
  • Patent number: 8999977
    Abstract: This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic [4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Grant
    Filed: March 8, 2013
    Date of Patent: April 7, 2015
    Assignee: Medivation Technologies, Inc.
    Inventors: David T. Hung, Andrew Asher Protter, Sarvajit Chakravarty, Rajendra Parasmal Jain
  • Patent number: 8999971
    Abstract: Disclosed herein are methods for controlling the activity of hypoxia-inducible transcription factor 1-alpha (HIF-1?) and diseases, conditions, or syndromes related thereto, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia. Further disclosed are pharmaceutical compositions comprising HIF-1? prolyl hydroxylase inhibitors useful in treating diseases, conditions, and/or syndromes related thereto the activity of HIF-1?.
    Type: Grant
    Filed: August 21, 2014
    Date of Patent: April 7, 2015
    Assignee: Aerpio Therapeutics Inc.
    Inventors: Robert Shalwitz, Joseph H. Gardner
  • Patent number: RE47214
    Abstract: The present invention relates to polymorphs and solvates of the hydrochloride salt of 4-[2-[[5-methyl-1-(2-naphthalenyl)-1H-pyrazol-3-yl]oxy]ethyl]morpholine (P027), processes for their preparation, and to pharmaceutical compositions comprising them.
    Type: Grant
    Filed: June 7, 2017
    Date of Patent: January 29, 2019
    Assignee: LABORATORIOS DEL DR. ESTEVE, S.A.
    Inventors: Ramón Berenguer Maimó, Jorge Medrano Rupérez, Jordi Benet Buchholz, Laura Puig Fernandez, Laia Pellejà Puxeu