The Other Cyclo In The Bicyclo Ring System Is A Benzene Ring (e.g., Quinazoline, Etc.) Patents (Class 544/283)
  • Patent number: 10143692
    Abstract: Polymorphs of N4-(4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)-3-methylphenyl)-N6-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine are provided herein. Processes for preparing the polymorphs and pharmaceutical composition comprising the polymorphs are also disclosed.
    Type: Grant
    Filed: January 3, 2018
    Date of Patent: December 4, 2018
    Assignee: Array BioPharma Inc.
    Inventors: Donald T. Corson, Christopher M. Lindemann, Daniel J. Watson
  • Patent number: 9822190
    Abstract: A nano-composition that includes nanoparticles, a method of forming the nano-composition, and a method of using the composition. The nanoparticles include a polycationic polymer ionically bonded to one or more polyanionic Glycosaminoglycans (GAGs), wherein the polycationic polymer is chitosan, methylated chitosan, poly L-Lysine, or poly L-Arginine.
    Type: Grant
    Filed: January 28, 2016
    Date of Patent: November 21, 2017
    Inventor: Shaker A. Mousa
  • Patent number: 9771333
    Abstract: Disclosed are compounds, compositions and methods for treating diseases, syndromes, conditions and disorders that are affected by the modulation of the activity of, e.g., the inhibition of, one or more members of the TAM family kinases.
    Type: Grant
    Filed: November 19, 2014
    Date of Patent: September 26, 2017
    Assignee: SignalChem Lifesciences Corp.
    Inventor: Zaihui Zhang
  • Patent number: 9695165
    Abstract: Described herein are inhibitors of FGFR-4, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of FGFR-4.
    Type: Grant
    Filed: January 14, 2015
    Date of Patent: July 4, 2017
    Assignee: BLUEPRINT MEDICINES CORPORATION
    Inventors: Neil Bifulco, Jr., Lucian V. DiPietro, Chandrasekhar V. Miduturu
  • Patent number: 9695184
    Abstract: Described herein are compounds of Formula (I) pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Methods of using the compounds or pharmaceutical compositions thereof for treating diseases are also provided.
    Type: Grant
    Filed: February 18, 2014
    Date of Patent: July 4, 2017
    Assignee: Kala Pharmaceuticals, Inc.
    Inventors: Winston Zapanta Ong, Pawel Wojciech Nowak, Ben C Askew
  • Patent number: 9181202
    Abstract: Provided is a crystal of a salt of the compound represented by formula (I), which is excellent in its solubility in water. In particular, also provided is a crystal of hydrochloride, hydrobromate, sulfate, nitrate, p-toluenesulfonate or methanesulfonate of the compound represented by formula (I).
    Type: Grant
    Filed: October 1, 2012
    Date of Patent: November 10, 2015
    Assignee: AJINOMOTO CO., INC.
    Inventors: Noriyasu Kataoka, Riho Kodama, Akinori Tatara
  • Patent number: 9108929
    Abstract: The present invention relates to quinazoline containing zinc-binding moiety based derivatives of formula I that have enhanced and unexpected properties as inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and their use in the treatment of EGFR-TK related diseases and disorders such as cancer.
    Type: Grant
    Filed: December 6, 2012
    Date of Patent: August 18, 2015
    Assignee: Curis, Inc.
    Inventors: Changgeng Qian, Xiong Cai
  • Patent number: 9102630
    Abstract: Provided is a crystal of a salt of the compound represented by formula (I), which is excellent in its solubility in water. In particular, also provided is a crystal of hydrochloride, hydrobromate, sulfate, nitrate, p-toluenesulfonate or methanesulfonate of the compound represented by formula (I).
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: August 11, 2015
    Assignee: AJINOMOTO CO., INC.
    Inventors: Noriyasu Kataoka, Riho Kodama, Akinori Tatara
  • Patent number: 9090588
    Abstract: The invention provides alkyne substituted quinazoline compounds, such as compounds of the formula (I), which are irreversible ErbB kinase inhibitors. The compounds are useful in the treatment of diseases and disorders where ErbB kinase activity is implicated such as a hyperproliferative disorder (e.g., cancer).
    Type: Grant
    Filed: March 2, 2012
    Date of Patent: July 28, 2015
    Assignee: NewGen Therapeutics, Inc.
    Inventors: Wang Shen, Aimin Zhang, Jack Maung, Xiaoling Zheng
  • Publication number: 20150148535
    Abstract: The present invention relates to a method for preparing nitrogen compounds using carbon dioxide, and to the use of the method in the production of vitamins, pharmaceutical products, adhesives, acrylic fibres, synthetic leathers, pesticides, herbicides, antifungal agents and fertilisers. The invention also relates to a method for producing vitamins, pharmaceutical products, adhesives, acrylic fibres, synthetic leathers, pesticides, herbicides, antifungal agents and fertilisers, which includes a step of preparing nitrogen compounds using the method of the invention. The invention further relates to a method for preparing labelled nitrogen compounds using carbon dioxide and to the uses thereof.
    Type: Application
    Filed: June 4, 2013
    Publication date: May 28, 2015
    Applicant: Commissariat A L'Energie Atomique Et Aux Energies Alternatives
    Inventors: Thibault Cantat, Christophe Gomes, Olivier Jacquet
  • Patent number: 9040548
    Abstract: The invention relates to quinazoline derivatives of formula (I), wherein m is an integer from 1 to 3; R1 represents halogeno or C1-3alkyl; X1 represents —O—; R2 is selected from one of the following three groups: 1) C1-5alkylR3, wherein R3 is piperidinyl-4-yl which may bear one or two substituents selected from hydroxy, halogeno, C1-4alkyl, C1-4hydroxyalkyl and C1-4alkoxy; 2) C2-5alkenylR3, wherein R3 is as defined herein; 3) C2-5alkynylR3, wherein R3 is as defined herein; and wherein any alkyl, alkenyl or alkynyl group may bear one or more substituents selected from hydroxy, halogeno and amino; and salts thereof; processes for their preparation; pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.
    Type: Grant
    Filed: January 3, 2014
    Date of Patent: May 26, 2015
    Assignee: AstraZeneca AB
    Inventors: Andrew Peter Thomas, Elaine Sophie Elizabeth Stokes, Laurent Francois Andre Hennequin
  • Patent number: 9034886
    Abstract: The present invention provides a 4-aminoquinazoline derivative having the chemical structure of the following formula, and the use thereof. It is demonstrated by the pharmacological experiment that, the compound or a salt thereof according to the present invention not only has distinct inhibitory effect on histone deacetylases, but also has stronger differentiation induction and anti-proliferative activities for certain tumor cells. It can be used in the treatment of cancers and diseases related to cell differentiation and proliferation. Excellent efficacy is observed especially for leukemia and a solid tumor. As demonstrated by the animal test, the compound or a salt thereof according to the present invention is less toxic.
    Type: Grant
    Filed: May 10, 2012
    Date of Patent: May 19, 2015
    Assignees: Shanghai Institute of Pharmaceutical Industry, Jiangsu Hengyi Pharmaceutical Co., Ltd.
    Inventors: Jianqi Li, Qingwei Zhang, Wangping Cai
  • Patent number: 9034655
    Abstract: Luminescent labels based on aromatic and heterocyclic compounds, including reactive intermediates used to synthesize these compounds, and methods of synthesizing and using these reporter compounds. These labels combine high photostabilities, large Stokes' shifts and contain a pyrimidinium moiety as a water-soluble group. These luminescent compounds relate generally to the following structure: The methods relate generally to the synthesis and/or use of reporter compounds for fluorescence lifetime or fluorescence polarization based applications.
    Type: Grant
    Filed: October 18, 2010
    Date of Patent: May 19, 2015
    Assignee: SETA BioMedicals, LLC
    Inventors: Leonid D. Patsenker, Inna G. Yermolenko, Iryna A. Fedyunyaeva, Yelena N. Obukhova, Olga N. Semenova, Ewald A. Terpetschnig
  • Patent number: 9024023
    Abstract: The present invention refers to a new efficient process for the synthesis of the active pharmaceutical ingredient Lapatinib and salts thereof. In particular, the present synthesis is carried out employing new intermediates in which the amine function is protected by a group cleavable in basic milieu that provides a higher overall yield of the synthesis process.
    Type: Grant
    Filed: September 3, 2013
    Date of Patent: May 5, 2015
    Assignee: F.I.S.—Fabbrica Italiana Sintetici S.p.A.
    Inventors: Francesco Fontana, Alfredo Paio
  • Patent number: 9006257
    Abstract: The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.
    Type: Grant
    Filed: February 7, 2013
    Date of Patent: April 14, 2015
    Assignee: Glenmark Pharmaceuticals S.A.
    Inventors: Laxmikant Atmaram Gharat, Abhisek Banerjee, Neelima Khairatkar-Joshi, Vidya Ganapati Kattige
  • Patent number: 8999988
    Abstract: Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following structure: including steroisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein A is a ring moiety selected from: and wherein R1, R2, R3, X, Z, L1, Cycl1, L2 and Cycl2 are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.
    Type: Grant
    Filed: July 22, 2013
    Date of Patent: April 7, 2015
    Assignees: Arizona Board of Regents on behalf of the University of Arizona, Astex Pharmaceuticals, Inc.
    Inventors: Laurence H. Hurley, Daruka Mahadevan, David J. Bearss, Hariprasad Vankayalapati, Steven L. Warner, James Welsh, Sridevi Bashyam
  • Patent number: 8987284
    Abstract: Disclosed are novel quinazoline derivatives containing phosphorus substitutions and methods for the treatment of hyperproliferative diseases (e.g. cancer) using the compounds. These compounds are type I receptor protein kinase inhibitors useful in treating disorders related to abnormal protein kinase activities such as cancer and inflammation in mammals. Also disclosed are pharmaceutical compositions containing the compounds, methods for the preparation of the compounds and their pharmaceutically acceptable salts.
    Type: Grant
    Filed: July 2, 2010
    Date of Patent: March 24, 2015
    Assignee: Newgen Therapeutics, Inc.
    Inventors: Wang Shen, Aimin Zhang, Junfa Fan, Xiaoling Zheng
  • Patent number: 8987285
    Abstract: The present invention relates to a novel crystalline anhydrous form of [(5-chlorothiophene-2-ylsulfonylcarbamoyl)-(4-(6-fluoro-7-(methylamino)-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)phenyl)amide, potassium salt, and its use in the treatment or prevention of a condition or a disorder with platelet ADP receptor inhibition, in particular, P2Y12 inhibition, in animals, particularly humans. It also relates processes for making such a novel crystalline form. The present invention also relates to a solid, oral formulation of this novel crystalline form, its preparation and use thereof.
    Type: Grant
    Filed: December 5, 2011
    Date of Patent: March 24, 2015
    Assignee: Portola Pharmaceuticals, Inc.
    Inventors: Ulrich Meier, Nicole Bieri, Dieter Becker, Julien Taillemite, Marie-Pierre Filliot, Tanja Meister
  • Patent number: 8987715
    Abstract: An organic electroluminescence device (1) includes: an anode (3); a cathode (4); and an emitting layer (5) provided between the anode (3) and the cathode (4). The emitting layer contains a first host, a second host and a phosphorescent dopant. A triplet energy of each of the first host and the second host is 2.8 eV or more. An ionization potential of the first host is 5.5 eV or less. An affinity Af1 of the first host is smaller than an affinity Af2 of the second host.
    Type: Grant
    Filed: June 8, 2011
    Date of Patent: March 24, 2015
    Assignee: Idemitsu Kosan Co., Ltd.
    Inventors: Kazuki Nishimura, Hitoshi Kuma, Chishio Hosokawa, Hideaki Nagashima, Masaki Numata
  • Publication number: 20150057260
    Abstract: The invention relates to compounds of Formula (0): wherein A1-A8, R4 and R5 each has the meaning as described herein. Compounds of Formula (0) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over-activation of NF-kB signaling is observed.
    Type: Application
    Filed: August 22, 2014
    Publication date: February 26, 2015
    Applicant: Genentech, Inc.
    Inventors: Nicole Blaquiere, Georgette Castanedo, Jianwen A. Feng, Baihua Hu, Steven Staben, Po-wai Yuen, Guosheng Wu, Xingyu Lin, Jason Burch
  • Patent number: 8952022
    Abstract: The present invention relates to processes for the preparation of erlotinib and salts and polymorphs thereof, preferably of high purity. The present invention also relates to erlotinib and salts and polymorphs thereof preparable by said processes, to medical uses of said erlotinib, salts and polymorphs, and to pharmaceutical compositions comprising the same.
    Type: Grant
    Filed: July 22, 2011
    Date of Patent: February 10, 2015
    Assignee: Generics [UK] Limited
    Inventors: Vinayak Govind Gore, Anilkumar Tripathi, Madhav Jadhav
  • Publication number: 20150034938
    Abstract: A compound for an organic optoelectronic device, an organic light emitting diode including the same, and a display device including the organic light emitting diode are disclosed and the compound for an organic optoelectronic device represented by the following Chemical Formula 1 or 2 provides an organic light emitting diode having life-span characteristics due to excellent electrochemical and thermal stability, and high luminous efficiency at a low driving voltage.
    Type: Application
    Filed: September 12, 2014
    Publication date: February 5, 2015
    Inventors: Dong-Min KANG, Hyun-Jung KIM, Chang-Ju SHIN, Jong-Woo WON, Nam-Heon LEE, Soo-Young JEONG, Ho-Kuk JUNG, Mi-Young CHAE
  • Publication number: 20150038514
    Abstract: The invention relates to sodium and calcium salts of {8-fluoro-2-[4-(3-methoxyphenyl)piperazine-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-3,4-dihydroquinazoline-4-yl}acetic acid and solvates thereof, to the use thereof in a method of treatment and/or prophylaxis of virus infections and to the use thereof for producing drugs for use in methods of treatment and/or prophylaxis of diseases, more particularly the use thereof as antiviral agents, more particularly against cytomegaloviruses.
    Type: Application
    Filed: February 28, 2013
    Publication date: February 5, 2015
    Inventors: Alfons Grunenberg, Mathias Berwe, Birgit Keil, Edwin Aret, Kerstin Paulus, Wilfried Schwab
  • Patent number: 8946247
    Abstract: The invention provides novel quinazoline carboxamide azetidine compounds according to Formula (I) and use for the treatment of hyperproliferative diseases, such as cancer.
    Type: Grant
    Filed: November 11, 2011
    Date of Patent: February 3, 2015
    Assignee: Merck Patent GmbH
    Inventors: Bayard R. Huck, Reinaldo Jones, Yufang Xiao, Constantin Neagu, Donald Bankston, Andreas Goutopoulos
  • Publication number: 20150031709
    Abstract: Provided herein are thiophene compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.
    Type: Application
    Filed: February 8, 2013
    Publication date: January 29, 2015
    Applicant: SUNOVION PHARMACEUTICALS, INC.
    Inventors: John Emmerson Campbell, Una Campbell, Taleen G. Hanania, Liming Shao
  • Patent number: 8927559
    Abstract: This application provides for compounds of the formula Formula I or a pharmaceutically acceptable salt thereof, wherein the individual variables are defined herein, as well as processes to prepare these compounds, pharmaceutical compositions comprising the same and their use in treating disease state associated with the CRTH2 receptor.
    Type: Grant
    Filed: October 6, 2011
    Date of Patent: January 6, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Robert G. Aslanian, Christopher W. Boyce, Robert D. Mazzola, Jr., Brian A. McKittrick, Kevin D. McCormick, Anandan Palani, Jun Qin, Haiqun Tang, Dong Xiao, Younong Yu, John P. Caldwell, Elizabeth Helen Kelley, Hongjun Zhang, Phieng Siliphaivanh, Rachel N. MacCoss, Joey L. Methot, Jolicia Polivina Gauuan, Qin Jiang, Andrew J. Leyhane, Purakkattle Johny Biju, Li Dong, Xianhai Huang, Ning Shao, Wei Zhou, Pawan K. Dhondi, Ashwin U. Rao
  • Patent number: 8916575
    Abstract: This invention relates to quinazoline derivatives, processes for their preparation, pharmaceutical compositions, and their use in therapy of disorders in which the modulation of toll-like-receptors is involved.
    Type: Grant
    Filed: May 18, 2012
    Date of Patent: December 23, 2014
    Assignee: Janssen R&D Ireland
    Inventors: David McGowan, Pierre Jean-Marie Bernard Raboisson, Tim Hugo Maria Jonckers, Stefaan Julien Last, Werner Embrechts, Serge Maria Aloysius Pieters
  • Patent number: 8916573
    Abstract: The invention relates to antibacterial compounds of formula (I), wherein R1 is H, halogen, (C1-C3)alkyl or (C1-C3)alkoxy; R2 is H, halogen, (C1-C3)alkyl, (C1-C3)alkoxy or pyrrolidin-1-yl; R3 is H, halogen, (C1-C3)alkyl, (C1-C3)alkoxy, vinyl or 2-methoxycarbonyvinyl or R2 and R3 together with the two carbon atoms which bear them form a phenyl ring; R4 is H, halogen, (C1-C3)alkyl or (C1-C3)alkoxy; and R5 is H, (C1-C3)alkyl or cyclopropyl, or R4 and R5form together a —CH2CH2CH2— group; A is the divalent group —CH2—, —CH2CH2—, #—CH(OH)CH2—*, #—CH2N(R6)—* and —CH2NHCH2—, wherein # indicates the point of attachment to the optionally substituted (quinazoline-2,4-dione-3-yl)methyl residue and * represents the point of attachment to the substituted (oxazolidinon-4-yl)methyl residue; R6 is H or acetyl; Y is CH or N; and Q is O or S; and salts of such compounds.
    Type: Grant
    Filed: August 10, 2012
    Date of Patent: December 23, 2014
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn Acklin
  • Patent number: 8916572
    Abstract: Novel bis-quinazoline derivatives as tyrosine kinase inhibitors, synthesis of these compounds, and novel methods for treating tyrosine kinase mediated diseases or disorders using these compounds are disclosed. In particular, the present invention provides tethered quinazoline derivative dimers as inhibitors to the epidermal growth factor receptor (EGFR) tyrosine kinase, pharmaceutical compositions thereof, and their therapeutic uses for treating EGFR kinase-mediated diseases or disorders, such as various cancers, as well as synthetic methods for preparing these novel compounds.
    Type: Grant
    Filed: May 6, 2013
    Date of Patent: December 23, 2014
    Assignee: Tetranov International Inc.
    Inventors: Yusheng Wu, Chengshan Niu, Dapeng Zou, Jingya Li, Ruiyun Guo
  • Patent number: 8916574
    Abstract: The present invention relates to 4-(substituted anilino)-quinazoline derivatives as tyrosine kinase inhibitors. Specifically, compounds of formula I, or pharmaceutically acceptable salts or solvates thereof are disclosed, in which each substitutent in formula I is defined in the description. Preparation method of the compounds of formula I, pharmaceutical compositions and pharmaceutical uses thereof are also disclosed. The compounds of formula I are effective tyrosine kinase inhibitors.
    Type: Grant
    Filed: September 20, 2010
    Date of Patent: December 23, 2014
    Assignee: Qilu Pharmaceutical Co., Ltd.
    Inventors: Jingyi Wang, Chuanwen Fan, Long Zhang, Zhongru Guo, Ying Li, Shaobo Yang, Shousheng Yan, Jianrong Zhu, Qingmin Yang, Minghui Zhang
  • Publication number: 20140371209
    Abstract: Compounds of formula (I) or (II) can modulate the activity of SIP receptors.
    Type: Application
    Filed: February 3, 2012
    Publication date: December 18, 2014
    Inventors: Jermaine Thomas, Sha Mi, Edward Yin-Shiang Lin, Guo Zhu Zheng, Bin Ma, Kevin Guckian, Gnanasambandam Kumaravel
  • Publication number: 20140371233
    Abstract: The present invention provides compositions and methods for treating and preventing an A?-modulated disease. In certain embodiments, the invention provides an inhibitor of Fyn tyrosine kinase, and methods of using the same. In certain embodiments, the inhibitor of the invention inhibits A? oligomer induced signaling and reduces or halts the progression of Alzheimer's Disease.
    Type: Application
    Filed: May 8, 2014
    Publication date: December 18, 2014
    Applicant: Yale University
    Inventor: Stephen M. Strittmatter
  • Patent number: 8912186
    Abstract: The invention provides specific small molecule compounds that allosterically regulate the activity or modulate protein-protein interactions of AGC protein kinases and the Aurora family of protein kinases, methods for their production, pharmaceutical compositions comprising same, and their use for preparing medicaments for the treatment and prevention of diseases related to abnormal activities of AGC protein kinases or of protein kinases of the Aurora family.
    Type: Grant
    Filed: October 16, 2009
    Date of Patent: December 16, 2014
    Assignee: Universitaet des Saarlandes
    Inventors: Matthias Engel, Wolfgang Fröhner, Adriane Stroba, Ricardo M. Biondi
  • Patent number: 8912205
    Abstract: A pharmaceutical formulation comprising the compound of formula
    Type: Grant
    Filed: July 16, 2013
    Date of Patent: December 16, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Malcolm Clive Carter, George Stuart Cockerill, Karen Elizabeth Lackey
  • Patent number: 8906930
    Abstract: Novel quinazolinamide derivatives of the formula (I), in which R1-R4 and X have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.
    Type: Grant
    Filed: October 26, 2010
    Date of Patent: December 9, 2014
    Assignee: Merck Patent GmbH
    Inventors: Hans Michael Eggenweiler, Christian Sirrenberg, Hans Peter Buchstaller
  • Patent number: 8906931
    Abstract: The present invention relates to a compound of formula (I), which has valuable pharmacological properties, particularly an inhibiting effect on signal transduction mediated by tyrosine kinases, processes for stereoselectively preparing these compounds, particularly pharmaceutical formulations suitable for inhalation and their use for the treatment of diseases, particularly tumoral diseases, benign prostatic hyperplasia and diseases of the lungs and airways.
    Type: Grant
    Filed: August 28, 2014
    Date of Patent: December 9, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Waldemar Pfrengle, Guenther Huchler, Markus Ostermeier, Peter Sieger
  • Patent number: 8901138
    Abstract: This invention relates to novel sulfoximine substituted quinazoline derivatives of formula I wherein Ar, R1 and R2 are as defined herein, and their use as MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) kinase inhibitors, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment or amelioration of MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) mediated disorders.
    Type: Grant
    Filed: November 7, 2013
    Date of Patent: December 2, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Andreas Blum, Dirk Gottschling, Armin Heckel, Joerg Hehn, Thorsten Lehmann-Lintz, Dieter Wiedenmayer
  • Patent number: 8889698
    Abstract: The present disclosure relates to compounds, which are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis.
    Type: Grant
    Filed: September 23, 2011
    Date of Patent: November 18, 2014
    Assignee: Resverlogix Corp.
    Inventor: Henrik C. Hansen
  • Patent number: 8883808
    Abstract: Patients suffering from serotonin-mediated diseases or conditions, such as depression, may be treated by administering an effective combined amount of a 5-HT7 receptor antagonist and a serotonin reuptake inhibitor.
    Type: Grant
    Filed: October 18, 2006
    Date of Patent: November 11, 2014
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Pascal Bonaventure, Christine Dugovic, Curt A. Dvorak, Dale A. Rudolph, Jonathan Edward Shelton
  • Patent number: 8877352
    Abstract: A biscarbazole derivative of the invention is represented by a formula (1A) or (1B) below. In the formula (1A) or (1B): A1 represents a substituted or unsubstituted nitrogen-containing heterocyclic group having 1 to 30 ring carbon atoms; A2 represents a substituted or unsubstituted aromatic hydrocarbon group having 6 to 30 ring carbon atoms, or substituted or unsubstituted nitrogen-containing heterocyclic group having 1 to 30 ring carbon atoms; X1 and X2 each are a linking group; Y1 to Y4 each represent a substituent; p and q represent an integer of 1 to 4; and r and s represent an integer of 1 to 3.
    Type: Grant
    Filed: April 20, 2011
    Date of Patent: November 4, 2014
    Assignee: Idemitsu Kosan Co., Ltd.
    Inventors: Tetsuya Inoue, Mitsunori Ito, Kei Yoshida, Kumiko Hibino, Kazuki Nishimura, Toshinari Ogiwara, Kiyoshi Ikeda
  • Publication number: 20140309245
    Abstract: The invention provides novel heterocyclic carboxamide compounds compounds according to Formula (I) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
    Type: Application
    Filed: December 17, 2012
    Publication date: October 16, 2014
    Inventors: Bayard R. Huck, Xiaoling Chen, Yufang Xiao, Ruoxi Lan, Lizbeth Celeste De Selm, Constantin Neagu, Justin Potnick, Srinivasa R. Karra, Theresa L. Johnson
  • Patent number: 8859571
    Abstract: Disclosed are compounds having the formula: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein, and methods of making and using the same.
    Type: Grant
    Filed: November 1, 2010
    Date of Patent: October 14, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Lara S. Kallander, Brian Griffin Lawhorn, Joanne Philp
  • Patent number: 8859570
    Abstract: The present invention relates to AZD2171 maleate salt, to particular crystalline forms of AZD2171 maleate salt, to processes for their preparation, to pharmaceutical compositions containing them as active ingredient, to their use in the manufacture of medicaments for use in the production of antiangiogenic and/or vascular permeability reducing effects in warm-blooded animals such as humans, and to their use in methods for the treatment of disease states associated with angiogenesis and/or increased vascular permeability.
    Type: Grant
    Filed: December 23, 2009
    Date of Patent: October 14, 2014
    Assignee: AstraZeneca AB
    Inventor: James McCabe
  • Patent number: 8853225
    Abstract: The present invention relates to a compound of formula (I), which has valuable pharmacological properties, particularly an inhibiting effect on signal transduction mediated by tyrosine kinases, processes for stereoselectively preparing these compounds, particularly pharmaceutical formulations suitable for inhalation and their use for the treatment of diseases, particularly tumoral diseases, benign prostatic hyperplasia and diseases of the lungs and airways.
    Type: Grant
    Filed: January 27, 2012
    Date of Patent: October 7, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Waldermar Pfrengle, Guenther Huchler, Markus Ostermeier, Peter Sieger
  • Patent number: 8846654
    Abstract: A subject-matter of the present invention is the use of compounds of formula (I) in the base, hydrate or solvate form or in the form of their mixtures, as medicaments or for the preparation of medicaments intended for the treatment of at least one cardiovascular disease and/or to prevent the appearance of at least one cardiovascular disease.
    Type: Grant
    Filed: October 7, 2011
    Date of Patent: September 30, 2014
    Assignee: Sanofi
    Inventors: Philip Janiak, Gilbert Marciniak, Jean-Francois Nave, Fabrice Viviani
  • Patent number: 8835445
    Abstract: The present disclosure provides compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R5, R6 and Z are as described herein. The disclosure also provides pharmaceutical compositions thereof; and methods for inhibiting DHFR activity; and methods for treating cell proliferative diseases, autoimmune disease, inflammatory disease or bacterial, fungal or parasitic infection by administering a compound of Formula I.
    Type: Grant
    Filed: June 2, 2011
    Date of Patent: September 16, 2014
    Assignee: Trius Therapeutics, Inc.
    Inventors: Zhiyong Chen, Christopher J. Creighton, Mark Cunningham, John Finn, Mark Hilgers, Michael Jung, Lucy Aguirre Kohnen, Thanh Lam, Xiaoming Li, Mark Stidham, Les Tari, Michael Trzoss, Junhu Zhang
  • Patent number: 8815878
    Abstract: Substituted spiro hemiaminals and methods for their use in the treatment of viral diseases, including hepatitis C viral infections, are described herein.
    Type: Grant
    Filed: July 27, 2011
    Date of Patent: August 26, 2014
    Assignee: NovaDrug, LLC
    Inventor: Eliezer Huberman
  • Patent number: 8809326
    Abstract: Disclosed are novel substituted 2H-isoquinolin-1-one and 3H-quinazolin-4-one derivatives useful as inhibitors of Rho kinase and for treating a variety of diseases and disorders that are mediated or sustained through the activity of Rho kinase, including cardiovascular diseases, pharmaceutical compositions comprising such compounds, methods for using such compounds and processes for making such compounds.
    Type: Grant
    Filed: September 18, 2007
    Date of Patent: August 19, 2014
    Assignee: Aerie Pharmaceuticals, Inc.
    Inventors: Todd Bosanac, John David Ginn, Eugene Richard Hickey, Thomas Martin Kirrane, Jr., Weimin Liu, Anthony S. Prokopowicz, Sabine K. Schlyer, Cheng-Kon Shih, Roger John Snow, Michael Robert Turner, Frank Wu, Erick Richard Young
  • Patent number: 8809354
    Abstract: Surprising antiviral activity of 3-amino-2-(4-nitrophenyl)-4-(3H)-quinazolinone (Compound 1) was reported in the treatment or prevention of viral infections, particularly in combination with other antiviral agents such as interferon and/or ribavarin.
    Type: Grant
    Filed: December 31, 2011
    Date of Patent: August 19, 2014
    Inventors: Sheikh Riazuddin, Osman Ali, Usman Ashfaq, Shaheen N. Khan, Javed Akram, Atta-ur Rahman, M. Iqbal Choudhary, Khalid M. Khan, Zulfiqar Ali Khan
  • Patent number: RE46791
    Abstract: The invention relates to substituted dihydroquinazolines and to processes for their preparation and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for use as antiviral agents, in particular against cytomegalo viruses.
    Type: Grant
    Filed: April 9, 2015
    Date of Patent: April 17, 2018
    Assignee: AICURIS ANTI-INFECTIVE CURES GMBH
    Inventors: Tobias Wunberg, Judith Baumeister, Ulrich Betz, Mario Jeske, Thomas Lampe, Susanne Nikolic, Jurgen Reefschlager, Rudolf Schohe-Loop, Frank Sussmeier, Holger Zimmermann, Rolf Grosser, Kerstin Henninger, Guy Hewlett, Jorg Keldenich, Dieter Lang, Peter Nell