Three Or More Hetero Atoms In The Tricyclo Ring System Patents (Class 514/293)
  • Patent number: 11311530
    Abstract: Provided is a therapeutic agent for Lewy body disease comprising (S)-7-(2-methoxy-3,5-dimethylpyridin-4-yl)-1-(tetrahydrofuran-3-yl)-1H-pyrazolo[4,3-c]quinolin-4(5H)-one represented by formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 30, 2018
    Date of Patent: April 26, 2022
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Mai Miyamoto, Yukio Ishikawa
  • Patent number: 11274099
    Abstract: A deuterated compound having structural formula I or a pharmaceutically acceptable salt thereof: Values and example values of the variable in formula (I) are disclosed herein. Also disclosed are the use of compounds of formula (I) in the methods of treating a disease selected from cancer, an autoimmune disease, and an infectious disease, and methods of enhancing an immune response to an antigen.
    Type: Grant
    Filed: May 18, 2018
    Date of Patent: March 15, 2022
    Assignee: Superb Wisdom Limited
    Inventor: Lihu Yang
  • Patent number: 11234971
    Abstract: Novel methods for treating cancer include: measuring the expression level of a gene; administering a glucocorticoid receptor modulator (GRM) to a patient; again measuring the expression level of a gene; identifying a patient in whom the expression level of the gene is decreased following GRM administration (compared to the baseline gene expression level) as likely to benefit from treatment by combined cancer chemotherapy plus GRM administration; and administering to the identified patient a combination of the GRM and cancer chemotherapy, whereby the cancer is treated in the patient. The GRM may be selected from relacorilant, CORT125281, CORT122928, and CORT113176. The cancer chemotherapy agent may be a taxane. The genes whose expression level is measured may be selected from COX2, DUSP1, GSK3b, MCL-1, PIK3CG, RGS-2, SGK1, and STAT3, and may be selected from FCGRT, C5, MAP3K7, TP53, BBC3, THBD, PRR5, RICTOR, and EIF2B4.
    Type: Grant
    Filed: January 17, 2020
    Date of Patent: February 1, 2022
    Assignee: Corcept Therapeutics Incorporated
    Inventors: Andrew Greenstein, Stacie Shepherd, Andreas G. Moraitis
  • Patent number: 11213526
    Abstract: Applicant discloses methods for treating a glucocorticoid receptor positive (GR+) neuroepithelial tumor in a subject, comprising administering a selective glucocorticoid receptor modulator (SGRM) in an amount effective to reduce the tumor load in a subject. The GR+ neuroepithelial tumor may be a neurofibromatosis type 2 (NF 2) tumor; the GR+ neuroepithelial tumor may be a schwannoma, meningioma, or ependymoma. In embodiments, the GR+ neuroepithelial tumor is not an adrenocorticotropic hormone (ACTH)-secreting tumor. In embodiments, the SGRM comprises a steroidal backbone. In embodiments, the SGRM is mifepristone. In embodiments, the SGRM comprises a non-steroidal backbone, such as, e.g., a cyclohexyl pyrimidine, a fused azadecalin, a heteroaryl ketone fused azadecalin, or an octahydro fused azadecalin backbone. The SGRM may be administered orally. The SGRM may be administered alone. In embodiments, the SGRM is administered with at least one non-SGRM therapy, e.g.
    Type: Grant
    Filed: June 18, 2018
    Date of Patent: January 4, 2022
    Assignee: Corcept Therapeutics, Inc.
    Inventor: Andreas G. Moraitis
  • Patent number: 11202752
    Abstract: Pharmaceutical formulations and methods for the topical and/or transdermal delivery of imiquimod, including creams, ointments and pressure-sensitive adhesive compositions to treat dermatological disorders, namely, viral infections, such as Type I or Type II Herpes simplex infections and genital warts, actinic keratosis and superficial basal cell carcinoma, and to induce interferon biosynthesis, with shorter durations of therapy, than currently approved for imiquimod by the Food & Drug Administration (“FDA”).
    Type: Grant
    Filed: May 15, 2013
    Date of Patent: December 21, 2021
    Assignee: Medicis Pharmaceutical Corporation
    Inventors: Jefferson J. Gregory, Michael T. Nordsiek
  • Patent number: 11179387
    Abstract: There is provided a therapeutic agent for Alzheimer's disease and Lewy body dementia for combined use of (S)-7-(2-methoxy-3,5-dimethylpyridin-4-yl)-1-(tetrahydrofuran-3-yl)-1H-pyrazolo[4,3-c]quinoline-4(5H)-one represented by formula (1): or a pharmaceutically acceptable salt thereof, and donepezil represented by formula (II): or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 30, 2018
    Date of Patent: November 23, 2021
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Mai Miyamoto, Sadaharu Kotani
  • Patent number: 11147803
    Abstract: There is provided a therapeutic agent for Alzheimer's disease for combined use of (S)-7-(2-methoxy-3,5-dimethylpyridin-4-yl)-1-(tetrahydrofuran-3-yl)-1H-pyrazolo[4,3-c]quinoline-4(5H)-one represented by formula (I): or a pharmaceutically acceptable salt thereof, and memantine represented by formula (II): or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 30, 2018
    Date of Patent: October 19, 2021
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Mai Miyamoto, Sadaharu Kotani
  • Patent number: 11059834
    Abstract: Compounds are provided that are useful as immunomodulators. The compounds have the following Formula (I) or (II): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R, R1, R2a, R2b, R2c, R3, R4, R5, R6a, R6b, R6c, m and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Grant
    Filed: July 8, 2019
    Date of Patent: July 13, 2021
    Assignee: ChemoCentryx, Inc.
    Inventors: Viengkham Malathong, Jeffrey McMahon, Darren J. McMurtrie, Sreenivas Punna, Howard S. Roth, Rajinder Singh, Penglie Zhang
  • Patent number: 10989719
    Abstract: To provide a compound which enables treatment or prevention of spinocerebellar ataxia, analyses were carried out based on a screening using a spinocerebellar ataxia type 1 (SCA1) fly model and on the like. As a result, the following proteins ameliorating the pathology of spinocerebellar ataxia were identified: RPA1, PNKP, XRCC3, XRCC4, CCNH, POLE, POLH, and PER1. On the other hand, the following proteins aggravating the pathology were identified: CHK1, LIG3, FEN1, LIG1, ERCC5, XAB2, ERCC2, DMC1, RECQL5, MUS81, EME1, SPO11, and BLM. In addition, it has been revealed that ATXN1, which is a cause of SCA1, binds to RPA1, BRCA1, and BRCA2, and suppresses the activities of these proteins, so that the above-described pathology is caused.
    Type: Grant
    Filed: October 10, 2014
    Date of Patent: April 27, 2021
    Assignee: National University Corporation Tokyo Medical and Dental University
    Inventor: Hitoshi Okazawa
  • Patent number: 10968225
    Abstract: The present invention relates to compounds of Formula (I) or pharmaceutically acceptable salts or solvates thereof: It further discloses a pharmaceutical composition comprising the compounds of Formula (I) and their uses, in particular to modulate CFTR protein or ABC protein activities.
    Type: Grant
    Filed: August 14, 2020
    Date of Patent: April 6, 2021
    Inventors: Tiziano Bandiera, Fabio Bertozzi, Paolo Di Fruscia, Federico Sorana, Francesco Berti, Alejandra Rodriguez Gimeno, Emanuela Caci, Loretta Ferrera, Nicoletta Pedemonte, Luis Juan Vicente Galietta
  • Patent number: 10947576
    Abstract: A method for rapid antibiotic susceptibility testing by tracking sub-micron scale motion of single bacterial cells including obtaining a biological sample from a subject including live bacteria. Different doses of antibiotic are added to a multi-well glass slide and adding portions of the biological sample to the wells. Bacterial cells are tethered onto the surface. The tethered bacterial cells are imaged and tracked. Bacterial sub-micron motion of tethered cells is measured at the different doses. A processor performs statistical analysis on a population of cells for each antibiotic dose to generate an antibiotic dose curve proportional to the motion changes, where the antibiotic dose curve plots data including a decrease in movement over time indicating a proportional effectiveness of an antibiotic applied to a well.
    Type: Grant
    Filed: July 25, 2018
    Date of Patent: March 16, 2021
    Assignee: ARIZONA BOARD OF REGENTS ON BEHALF OF ARIZONA STATE UNIVERSITY
    Inventors: Nongjian Tao, Karan Syal
  • Patent number: 10889575
    Abstract: The invention belongs to the field of medicine and chemical industry and relates to a 4,4-diphenylpiperidine compound or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same and uses thereof. In particular, the invention relates to a compound of Formula I or a pharmaceutically acceptable salt thereof, and to a pharmaceutical composition comprising the compound or a pharmaceutically acceptable salt thereof. In the present invention, the compound or pharmaceutically acceptable salt thereof and the pharmaceutical composition have significant activity in blocking an N-type calcium channel, and have good pharmacokinetic properties, can effectively relieve pain, and have a potential as a new medicament for prevention or treatment of pain, stroke, cerebral ischemia, alcohol addiction, alcoholism, kidney disease, addictive disorder caused by analgesic or tolerance disorder caused by analgesic.
    Type: Grant
    Filed: January 12, 2018
    Date of Patent: January 12, 2021
    Assignee: Academy of Military Medical Sciences
    Inventors: Cheng Zhang, Haoshan Wang, Guoxing Dong, Ning Wu, Shuzhuo Zhang, Xiaomei Zhuang, Chong Pang, Juan Wang, Rifang Yang, Jianquan Zheng, Jin Li, Liuhong Yun
  • Patent number: 10865203
    Abstract: Provided herein are novel pyrazolo-quinolinone compounds and method of using such compounds to treat disorders such as neuropsychiatric disorders with sensorimotor gating deficits, such as schizophrenia, tic disorders, attention deficit hyperactivity disorder, obsessive compulsive disorder, panic disorder, Huntington's disease and nocturnal enuresis; depression; temporomandibular myofascial pain; disorders of trigeminal nerve, such as trigeminal neuralgia and trigeminal neuropathy; migraine; and tinnitus.
    Type: Grant
    Filed: June 3, 2016
    Date of Patent: December 15, 2020
    Assignees: UWM Research Foundation, Inc., Medical University of Vienna
    Inventors: James Cook, Daniel Knutson, Marko Mihovilovic, Laurin Wimmer
  • Patent number: 10766896
    Abstract: Imidazo[4,5-c] ring compounds of formula I, (particularly imidazo4,5-c]quinolines, 6,7,8,9-tetrahydroimidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and 6,7,8,9-tetrahydroimidazo[4,5-c]naphthyridine compounds) having a guanidine substituted benzamide that is attached at the N?1 position by a linking group, pharmaceutical compositions containing the compounds, and methods of making the compounds are disclosed. Methods of use of the compounds as immune response modifiers, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are also disclosed.
    Type: Grant
    Filed: February 27, 2018
    Date of Patent: September 8, 2020
    Assignee: 3M INNOVATIVE PROPERTIES COMPANY
    Inventors: Bryon A. Merrill, George W. Griesgraber, Chad A. Haraldson, Kevin J. Bechtold
  • Patent number: 10745407
    Abstract: The present invention relates to compounds of Formula (I) or pharmaceutically acceptable salts or solvates thereof: It further discloses a pharmaceutical composition comprising the compounds of Formula (I) and their uses, in particular to modulate CFTR protein or ABC protein activities.
    Type: Grant
    Filed: March 14, 2018
    Date of Patent: August 18, 2020
    Assignee: Fondazione Istituto Italiano Di Tecnologia
    Inventors: Tiziano Bandiera, Fabio Bertozzi, Paolo Di Fruscia, Federico Sorana, Francesco Berti, Alejandra Rodriguez Gimeno, Emanuela Caci, Loretta Ferrera, Nicoletta Pedemonte, Luis Juan Vicente Galietta
  • Patent number: 10722591
    Abstract: The present disclosure relates to cleavable conjugates (for example, particle-based or antibody-based conjugates) of TLR7/8 agonists (for example, 1H-imidazo[4,5-c]quinoline derivatives) containing a conjugation linker, a cleavable linker, and a self-eliminating linker. The present disclosure also related to methods for preparation of the cleavable conjugates, uses thereof for stimulating an effective immune response, and uses thereof for the treatment of cancer.
    Type: Grant
    Filed: November 13, 2018
    Date of Patent: July 28, 2020
    Assignee: Dynavax Technologies Corporation
    Inventors: Robert L. Coffman, Stewart D. Chipman, Radwan Kiwan, Samuel Zalipsky, Gary S. Ott
  • Patent number: 10533007
    Abstract: This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that modulate (e.g., agonize or partially agonize) NLRP3 and TLR7 and/or TLR8 that are useful, e.g., for treating a condition, disease or disorder in which a decrease in NLRP3 and TLR7 and/or TLR8 activities (e.g., a condition, disease or disorder associated with repressed or impaired NLRP3 and TLR7 and/or TLR8 signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions as well as other methods of using and making the same.
    Type: Grant
    Filed: April 19, 2017
    Date of Patent: January 14, 2020
    Assignee: Innate Tumor Immunity, Inc.
    Inventors: Gary D. Glick, Shomir Ghosh, William R. Roush
  • Patent number: 10428064
    Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I):(I) or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein A is a heterocyclic or heteroaryl ring, and R1, R2a, R2b, R2c, R3a, R3b, R4a, R4b, A, G1, G2, L1, L2, m1, m2, and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.
    Type: Grant
    Filed: April 15, 2016
    Date of Patent: October 1, 2019
    Assignee: Araxes Pharma LLC
    Inventors: Liansheng Li, Jun Feng, Yun Oliver Long, Yuan Liu, Tao Wu, Pingda Ren, Yi Liu
  • Patent number: 10392405
    Abstract: Compounds are provided that are useful as immunomodulators. The compounds have the following Formula (I) or (II): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R, R1, R2a, R2b, R2c, R3, R4, R5, R6a, R6b, R6c, m and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Grant
    Filed: August 7, 2018
    Date of Patent: August 27, 2019
    Assignee: ChemoCentryx, Inc.
    Inventors: Viengkham Malathong, Jeffrey McMahon, Darren J. McMurtrie, Sreenivas Punna, Howard S. Roth, Rajinder Singh, Penglie Zhang
  • Patent number: 10206930
    Abstract: The present invention is directed to methods of treating T-ALL that involve administering an inhibitor of jumonji D3 (JMJD3) demethylase. Another embodiment of the invention relates to methods inhibiting T-ALL cell proliferation and/or survival that involves administering an inhibitor of jumonji D3 (JMJD3) demethylase to a population of T-ALL cells.
    Type: Grant
    Filed: August 15, 2016
    Date of Patent: February 19, 2019
    Assignee: New York University
    Inventors: Iannis Aifantis, Panagiotis Ntziachristos
  • Patent number: 10208032
    Abstract: The present disclosure provides benzamide and nicotinamide compounds and pharmaceutical uses of the compounds. The compounds can be used to treat, for example, cancers such hematopoietic cancers (e.g., leukemia). The preferred compounds of the invention contain a phenylethynyl moiety as well as an amine-based heterocyclyl or heteroaryl moiety attached to the benzamide or nicotinamide compound.
    Type: Grant
    Filed: December 23, 2014
    Date of Patent: February 19, 2019
    Assignee: ONCOTARTIS INC.
    Inventors: Alexander Polinsky, Lioubov Korotchkina, Slavoljub Vujcic, Olga Chernova
  • Patent number: 10201536
    Abstract: The present invention relates to methods and pharmaceutical compositions for the treatment of bacterial infections in patients suffering from cirrhosis. In particular, the present invention relates to a method of treating bacterial infection in a patient suffering from cirrhosis comprising administering to the patient a therapeutically effective amount of a TLR7 and/or TLR8 agonist.
    Type: Grant
    Filed: May 12, 2016
    Date of Patent: February 12, 2019
    Assignees: INSERM (INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE), UNIVERISTE PARIS DIDEROT—PARIS 7, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS)
    Inventors: Axel Joseph Perianin, Loiec Rolas
  • Patent number: 10137122
    Abstract: The present invention provides compounds of formula I, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting kinase (e.g., GSK3 (e.g., GSK3? or GSK3?) or CK1) activity. The present invention further provides methods of using the compounds described herein for treating kinase-mediated disorders, such as neurological diseases, psychiatric disorders, metabolic disorders, and cancer.
    Type: Grant
    Filed: July 14, 2015
    Date of Patent: November 27, 2018
    Assignees: The Broad Institute, Inc., Dana-Farber Cancer Institute, Inc., The General Hospital Corporation
    Inventors: Florence Fevrier Wagner, Jennifer Q. Pan, Sivaraman Dandapani, Andrew Germain, Edward Holson, Benito Munoz, Partha P. Nag, Michael C. Lewis, Stephen J. Haggarty, Joshua A. Bishop, Kimberly Stegmaier, Michel Weiwer, Versha Banerji
  • Patent number: 9908880
    Abstract: Imidazoquinolines of formula I that contain substituted amine or amide functionality at 1-position and that are effective as Toll like Receptor 7 activators are disclosed. These compounds are useful as anticancer agents.
    Type: Grant
    Filed: September 19, 2016
    Date of Patent: March 6, 2018
    Assignee: 4SC AG
    Inventors: Volker Gekeler, Thomas Maier, Astrid Zimmermann, Hans-Peter Hofmann, Sanjeev A. Kulkarni, Anil P. Jagtap, Ganesh S. Chaure
  • Patent number: 9908895
    Abstract: The present invention provides tricyclic fused thiophene derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
    Type: Grant
    Filed: October 1, 2015
    Date of Patent: March 6, 2018
    Assignee: Incyte Corporation
    Inventors: Yun-Long Li, Wenyu Zhu, Song Mei, Joseph Glenn
  • Patent number: 9893299
    Abstract: The invention concerns heterocyclic compounds and electronic devices, in particular organic electroluminescent devices, containing these compounds.
    Type: Grant
    Filed: August 13, 2014
    Date of Patent: February 13, 2018
    Assignee: Merck Patent GmbH
    Inventors: Philipp Stoessel, Nils Koenen
  • Patent number: 9777017
    Abstract: The present invention provides tricyclic fused thiophene derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
    Type: Grant
    Filed: October 1, 2015
    Date of Patent: October 3, 2017
    Assignees: Incyte Holdings Corporation, Incyte Corporation
    Inventors: Yun-Long Li, Wenyu Zhu, Song Mei
  • Patent number: 9550776
    Abstract: A compound represented by formula (I), or a pharmaceutically acceptable salt thereof: wherein R1 represents a group represented by the formula: a group represented by the formula: or a group represented by the formula: and R2 represents a 3-methyltetrahydro-2H-pyran-4-yl group or 4-methoxycyclohexyl group.
    Type: Grant
    Filed: April 3, 2014
    Date of Patent: January 24, 2017
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Yoshihiko Norimine, Nobuaki Sato, Yuki Ishihara, Kunitoshi Takeda
  • Patent number: 9499564
    Abstract: Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.
    Type: Grant
    Filed: May 14, 2015
    Date of Patent: November 22, 2016
    Assignee: G1 Therapeutics, Inc.
    Inventors: Francis X. Tavares, Jay C. Strum
  • Patent number: 9265769
    Abstract: The present invention relates to substituted thiazolyl- and oxazolyl-isoquinolinones that act, for example, as modulators of poly(ADP-ribose) polymerase (PARP). The present invention also relates to processes for the preparation of substituted thiazolyl- and oxazolyl-isoquinolinones and to their use in treating various diseases and disorders.
    Type: Grant
    Filed: November 7, 2014
    Date of Patent: February 23, 2016
    Inventors: Roberto Pellicciari, Flavio Moroni
  • Patent number: 9216999
    Abstract: Novel tricyclic pyrimidine compounds and tricyclic pyridine compounds having JAK inhibitory activities are provided. A tricyclic heterocyclic compound represented by the formula (Ia): wherein the rings Aa and Ba, Xa, Ya, R1a, R2a, R3a, L1a L2a, L3a and na are as defined in the description.
    Type: Grant
    Filed: August 10, 2012
    Date of Patent: December 22, 2015
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Keishi Hayashi, Tsuneo Watanabe, Koji Toyama, Junji Kamon, Masataka Minami, Miyuki Uni, Mariko Nasu
  • Patent number: 9216980
    Abstract: Methods of use of compounds of formula (I) for treating cancer: wherein X, Y, X, R3, R5 and R6 are as defined herein.
    Type: Grant
    Filed: April 17, 2014
    Date of Patent: December 22, 2015
    Assignee: Genentech, Inc.
    Inventors: Huifen Chen, Hazel Joan Dyke, Charles Ellwood, Emanuela Gancia, Lewis J. Gazzard, Simon Goodacre, Samuel Kintz, Joseph Lyssikatos, Calum MacLeod, Karen Williams
  • Patent number: 9127015
    Abstract: Compounds which are tricyclopyrazole derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.
    Type: Grant
    Filed: November 24, 2010
    Date of Patent: September 8, 2015
    Assignee: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Teresa Disingrini, Sergio Mantegani, Mario Varasi
  • Patent number: 9072876
    Abstract: The present invention is directed to airless storage and dispensing systems that include a pump or dispensing package pre-filled with a topical semi-solid imiquimod pharmaceutical formulation (“pump systems”) and methods for storing and dispensing from the pump systems a plurality of precisely measured and uniform unit doses of a topical semi-solid imiquimod pharmaceutical formulation, and more particularly to pump systems, pre-filled with a topical imiquimod pharmaceutical cream and methods for delivering multiple precisely measured unit doses of a topical imiquimod pharmaceutical cream, and methods for using a controlled delivery pump system to store and dispense a plurality of consistent and precisely measured unit doses of a topical imiquimod pharmaceutical cream for use in topically treating a dermal and mucosal-associated condition, such as, external genital warts and/or perianal warts (EGWs), actinic keratosis or actinic keratoses (AK or AKs) and superficial basal cell carcinoma (sBCC).
    Type: Grant
    Filed: September 3, 2010
    Date of Patent: July 7, 2015
    Assignee: MEDICIS PHARMACEUTICAL CORPORATION
    Inventors: Michael T. Nordsiek, Kodumudi S. Balaji
  • Publication number: 20150148341
    Abstract: The present invention provides octahydro fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.
    Type: Application
    Filed: November 21, 2014
    Publication date: May 28, 2015
    Inventors: Hazel Hunt, Iain Walters, Benoit Gourdet
  • Publication number: 20150141410
    Abstract: Chemical compounds are provided which act on GPR17 receptors and are useful in the treatment or amelioration of chronic and/or acute neurodegenerative diseases, such as multiple sclerosis, inflammatory diseases, pathologies involving the immune system, cardiovascular diseases, and renal diseases.
    Type: Application
    Filed: May 9, 2012
    Publication date: May 21, 2015
    Applicants: UNIVERSITA' DEGLI STUDI DI MILANO, FONDAZIONE ITALIANA SCLEROSI MULTIPLA - FISH ONLUS
    Inventors: Maria Pia Abbracchio, Mario Alberto Battaglia, Ivano Eberini, Marta Fumagalli, Chiara Parravicini, Cristina Sensi, Paola Zaratin
  • Patent number: 9034336
    Abstract: The invention provides compounds of formula I: wherein R1-R3, Ra, and Rb have any of the values defined herein, and salts thereof. The compounds have immunomodulatory properties.
    Type: Grant
    Filed: August 30, 2012
    Date of Patent: May 19, 2015
    Assignee: Regents of the University of Minnesota
    Inventors: David M. Ferguson, John Ohlfest, Courtney Aldrich
  • Publication number: 20150133436
    Abstract: The use of compounds in the treatment of autoimmune and inflammatory diseases or conditions, pharmaceutical compositions containing such compounds and to methods for identifying compounds for use in the treatment of such diseases or conditions.
    Type: Application
    Filed: January 23, 2015
    Publication date: May 14, 2015
    Inventors: Chun-Wa CHUNG, Edwige NICODEME
  • Publication number: 20150133443
    Abstract: The present invention relates to substituted thiazolyl- and oxazolyl-isoquinolinones that act, for example, as modulators of poly(ADP-ribose) polymerase (PARP). The present invention also relates to processes for the preparation of substituted thiazolyl- and oxazolyl-isoquinolinones and to their use in treating various diseases and disorders.
    Type: Application
    Filed: November 7, 2014
    Publication date: May 14, 2015
    Inventors: Roberto Pellicciari, Flavio Moroni
  • Publication number: 20150133434
    Abstract: The present disclosure provides compositions and methods for reactivating latent immunodeficiency vims. The methods generally involve contacting an HIV-infected cell in which HIV is latent with an agent that binds a bromodomain (BRD) in the cell. Latently infected cells contain replication-competent integrated HIV-1 genomes that are blocked at the transcriptional level, resulting in the absence of viral protein expression. The present disclosure provides methods for reducing the reservoir of latent immunodeficiency virus in an individual.
    Type: Application
    Filed: March 13, 2013
    Publication date: May 14, 2015
    Inventors: Melanie Ott, Eric M. Verdin, Ming-Ming Zhou
  • Patent number: 9029388
    Abstract: The present invention provides a compound having a superior PDE10A inhibitory action and use thereof. The compound is a compound represented by the following formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.
    Type: Grant
    Filed: March 15, 2012
    Date of Patent: May 12, 2015
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Takahiko Taniguchi, Jun Kunitomo, Masato Yoshikawa, Tomoaki Hasui, Eiji Honda, Keisuke Imamura, Haruhi Kamisaki, Shinkichi Suzuki, Kasei Miura
  • Publication number: 20150126501
    Abstract: The present invention belongs to the technical field of medicine, relating in particular to: a fused ring compound as represented by Formula (I) for use as a mineralocorticoid receptor antagonist, a pharmaceutically acceptable salt thereof, and an isomer thereof; a preparation method for these compounds; a pharmaceutical preparation containing these compounds; and an application of these compounds, the pharmaceutically acceptable salt thereof, or the isomers thereof in the preparation of medicants for the treatment and/or prevention of kidney injury, cardiovascular diseases such as hypertension, and/or endocrine disease. The definitions of X, Y1, Y2, Y3, R1, R2a, R2b, R3a, R3b, R4, Cy and n are as presented in the description.
    Type: Application
    Filed: January 7, 2015
    Publication date: May 7, 2015
    Inventors: Zhenhua Huang, Jinyuan Wang, Dedong Zhang
  • Patent number: 9023863
    Abstract: The present invention provides a foamable composition comprising water and an organic solvent, wherein the organic solvent comprises a fatty acid. The composition may further comprise a pharmaceutically active agent. The composition of the invention is also useful for the treatment of a dermatological disorder in a mammal by the topical administration of the composition.
    Type: Grant
    Filed: July 12, 2007
    Date of Patent: May 5, 2015
    Assignee: Stiefel Research Australia Pty Ltd
    Inventors: Albert Zorko Abram, Iulian Goldstein
  • Publication number: 20150110784
    Abstract: The present invention provides therapeutic combinations that include an immune response modifier (IRM) component and an anti-inflammatory component. The inventions further provide methods of treating a condition by administering to one having the condition a therapeutic combination that includes an IRM component and an anti-inflammatory component.
    Type: Application
    Filed: December 23, 2014
    Publication date: April 23, 2015
    Inventors: Mark A. Tomai, Gary W. Gullikson, David M. Hammerbeck, Elaine A. Egging, Michael J. Reiter, Christopher D. Gram, John P. Vasilakos
  • Patent number: 9012470
    Abstract: The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and negatively modulating the ?5 subtype of GABAA, and use of the compound of formula I in the manufacture of a medicament for the treatment of GABAA receptor associated disorders. The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).
    Type: Grant
    Filed: October 11, 2011
    Date of Patent: April 21, 2015
    Assignee: Dart NeuroScience (Cayman) Ltd.
    Inventors: Varsha Gupta, Joel Renick, Graeme Freestone, Alan P. Kaplan
  • Publication number: 20150105415
    Abstract: The present invention relates to the compound represented by formula (I): (wherein, all the symbols have the same meaning as that of the specification), a salt thereof, a solvate thereof or a prodrug thereof. Since the compound of the present invention has an anti stress action, it is useful for preventive and/or therapeutic agent for a disease caused by stress, especially a digestive system disease caused by stress and is superior to oral absorption.
    Type: Application
    Filed: December 17, 2014
    Publication date: April 16, 2015
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Kazuyuki OHMOTO, Masashi KATO, Yoshifumi KAGAMIISHI, Junichiro MANAKO
  • Publication number: 20150105417
    Abstract: The invention relates to a pharmaceutical combination which comprises (a) a phosphoinositide 3-kinase inhibitor compound and (b) a compound which modulates the Ras/Raf/Mek pathway for the treatment of a proliferative disease, especially a solid tumor disease; a pharmaceutical composition comprising such a combination; the use of such a combination for the preparation of a medicament for the treatment of a proliferative disease; a commercial package or product comprising such a combination as a combined preparation for simultaneous, separate or sequential use; and to a method of treatment of a warm-blooded animal, especially a human.
    Type: Application
    Filed: December 19, 2014
    Publication date: April 16, 2015
    Inventors: Carlos Garcia-Echeverria, Sauveur-Michel Maira, Darrin Stuart, Susan Wee, Christine Fritsch, Tobi Nagel
  • Patent number: 9006246
    Abstract: An object of the present invention is to provide a drug having the inhibitory activity on ENPP2 which is a different target from that of the existing drug, as a medicament useful in a urinary excretion disorder patient for whom the existing drug has the insufficient effect. The present invention provides a compound represented by the general formula (I): (wherein definition of each group is as defined in the description) having the ENPP2 inhibitory activity, a salt thereof or a solvate thereof or a prodrug thereof, and an agent for preventing or treating urinary excretion disorder and/or improving symptoms thereof, containing them as an active ingredient.
    Type: Grant
    Filed: July 5, 2011
    Date of Patent: April 14, 2015
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Akira Ohata, Shingo Nakatani, Tetsuya Sugiyama, Takashi Morimoto
  • Patent number: 9006264
    Abstract: Imidazo-quinoline, -pyridine, and -naphthyridine ring systems (particularly quinolines, tetrahydroquinolines, pyridines, [1,5]naphthyridines, [1,5]tetrahydronaphthyridines) substituted at the 1-position with a cyclic substituent, pharmaceutical compositions containing the compounds, methods of making these compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
    Type: Grant
    Filed: September 9, 2013
    Date of Patent: April 14, 2015
    Assignee: 3M Innovative Properties Company
    Inventors: Doris Stoermer, Joseph F. Dellaria, Jr., David T. Amos, Bernhard M. Zimmermann, Luke T. Dressel, Jason D. Bonk
  • Patent number: 9000153
    Abstract: The invention relates to compounds of the formulae (I) and (II) in which R1, R2, R3, R4, R5, R8, X and m have the meaning indicated in the claims, and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitization of cancer cells to anticancer agents and/or ionizing radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumors, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I).
    Type: Grant
    Filed: July 26, 2011
    Date of Patent: April 7, 2015
    Assignee: Merck Patent GmbH
    Inventors: Thomas Fuchss, Werner Mederski, Frank Zenke