Ring Chalcogen In The Bicyclo Ring System Patents (Class 514/260.1)
  • Patent number: 10449191
    Abstract: Methods for treating prostate cancer, including advanced prostate cancer, in a subject in need thereof, include administering once-daily to the subject, at least 80 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4- tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N?-methoxyurea, or a corresponding amount of a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 29, 2019
    Date of Patent: October 22, 2019
    Assignees: Myovant Sciences GmbH, Takeda Pharmaceutical Company Limited
    Inventors: Vijaykumar Reddy Rajasekhar, Brendan Mark Johnson, David B. MacLean, Lynn Seely, Paul N. Mudd, Jr.
  • Patent number: 10450326
    Abstract: The present invention provides structural details of a thiazolopyrimidinone compound, a preparation method thereof, and use thereof in the manufacture of a medicament for the treatment of central nervous system diseases.
    Type: Grant
    Filed: June 3, 2016
    Date of Patent: October 22, 2019
    Assignee: PEKING UNIVERSITY
    Inventors: Kewei Wang, Qi Sun, Wenxuan Jiao, Jingshu Tang
  • Patent number: 10377767
    Abstract: The disclosure relates to inhibitors of USP7 inhibitors useful in the treatment of cancers, neurodegenerative diseases, immunological disorders, inflammatory disorders, cardiovascular diseases, ischemic diseases, viral infections and diseases, and bacterial infections and diseases, having the Formula: where R1, R2, R3, R5, R5?, X1, X2, n, and m are described herein.
    Type: Grant
    Filed: March 1, 2018
    Date of Patent: August 13, 2019
    Assignee: FORMA Therapeutics, Inc.
    Inventors: Stephanos Ioannidis, Adam Charles Talbot, Bruce Follows, Alexandre Joseph Buckmelter, Minghua Wang, Ann-Marie Campbell, David R. Lancia, Jr.
  • Patent number: 10323041
    Abstract: Compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R8, R14, W, A and n are as defined in the description. Medicinal products containing the same which are useful in treating conditions requiring a pro-apoptotic agent.
    Type: Grant
    Filed: June 22, 2016
    Date of Patent: June 18, 2019
    Assignees: LES LABORATOIRES SERVIER, VERNALIS (R&D) LTD
    Inventors: Balazs Balint, Márton Csékei, Zoltán Szabó, Zoltan Szlavik, András Kotschy, Maïa Chanrion, Olivier Geneste, I-Jen Chen, James Edward Paul Davidson, James Brooke Murray, Szabolcs Sipos, Levente Ondi, Ágnes Proszenyák
  • Patent number: 10316043
    Abstract: This invention relates to thieno[3,2-d]pyrimidines derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.
    Type: Grant
    Filed: January 30, 2017
    Date of Patent: June 11, 2019
    Assignee: Janssen Sciences Ireland Unlimited Company
    Inventors: David Craig McGowan, Pierre Jean-Marie Bernard Raboisson
  • Patent number: 10273242
    Abstract: The present invention relates to a compound inhibiting the activities of Bruton's tyrosine kinase (BTK) and/or Janus kinase 3 (JAK3), a pharmaceutical composition of the compound, pharmaceutical applications of same, a method for using the compound in inhibiting the activities of BTK and/or JAK3, and a method for using the compound in treatment and/or prevention of BTK- and/or JAK3-mediated diseases or disorders in mammals (especially human). The compound is as represented by structural formula (I).
    Type: Grant
    Filed: October 31, 2017
    Date of Patent: April 30, 2019
    Assignee: BEIJING HANMI PHARMACEUTICAL CO., LTD.
    Inventors: Jinming Liu, Mi Young Cha, Gong Li, Zhanmei Li, Hongjuan Qiu, Maengsup Kim
  • Patent number: 10233194
    Abstract: The present invention discloses a compound comprising the formula: wherein R is hydrogen or an alkyl group having from one to ten carbon atoms, or a compound of the formula wherein the S is replaced by CH2, and optionally comprising a pharmaceutically acceptable salt, hydrate, or solvate thereof. A method of treating a patient having cancer or a disease comprising administering to a patient an effective amount of the compound or pharmaceutically acceptable salt, hydrate, or solvate thereof.
    Type: Grant
    Filed: April 5, 2017
    Date of Patent: March 19, 2019
    Assignee: Duquesne Unversity of the Holy Spirit
    Inventor: Aleem Gangjee
  • Patent number: 10220044
    Abstract: The present invention relates to compounds of formula (I): wherein R6 is —CONH2 or a —C(R?)(R?)(OH) group; R is a substituted phenyl or heteroaryl group; R7 is an optionally substituted aryl or heteroaryl group. Process for the preparation thereof and therapeutic use thereof.
    Type: Grant
    Filed: July 26, 2017
    Date of Patent: March 5, 2019
    Assignee: SANOFI
    Inventors: Jean-Christophe Carry, Fabienne Chatreaux, Stephanie Deprets, Olivier Duclos, Vincent Leroy, Sergio Mallart, Dominique Melon-Manguer, Maria Mendez-Perez, Fabrice Vergne
  • Patent number: 10160769
    Abstract: The present disclosure relates generally to thienopyrimidine and thienopyridine compounds and methods of use thereof. In particular embodiments, the present disclosure provides compositions comprising thienopyrimidine and thienopyridine compounds of Formula 3: and methods of use to inhibit the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins.
    Type: Grant
    Filed: October 18, 2016
    Date of Patent: December 25, 2018
    Assignee: The Regents of the University of Michigan
    Inventors: Jolanta Grembecka, Tomasz Cierpicki, Dmitry Borkin, Jay L. Hess, Duxin Sun, Xiaoqin Li, Kevin Greenman, Mohamed Ibrahim, Artem Plekhov
  • Patent number: 10150778
    Abstract: The present invention provides a production method of a thienopyrimidine derivative or a salt thereof which has a gonadotropin releasing hormone (GnRH) antagonistic action with high quality in high yield. The present invention provides a method of producing a thienopyrimidine derivative, which comprises reacting 6-(4-aminophenyl)-1-(2,6-difluorobenzyl)-5-dimethylaminomethyl-3-(6-methoxypyridazin-3-yl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione or salt thereof, 1,1?-carbonyldiimidazole or a salt thereof and methoxyamine or a salt thereof, and the like.
    Type: Grant
    Filed: April 7, 2017
    Date of Patent: December 11, 2018
    Assignee: Takeda Pharmaceutical Company Limited
    Inventor: Kazuhiro Miwa
  • Patent number: 10077277
    Abstract: This application relates to derivatives of Formula I: and pharmaceutically acceptable salts thereof, which are inhibitors of PI3K, and compositions and methods of treatment related thereto.
    Type: Grant
    Filed: June 10, 2015
    Date of Patent: September 18, 2018
    Assignee: Incyte Corporation
    Inventors: Yun-Long Li, Andrew P. Combs
  • Patent number: 10047098
    Abstract: In its many embodiments, the present invention provides certain C5-C6-oxacyclic fused iminopyrimidinone compounds, including compounds Formula (I): or a tautomer thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein RN, R1, RA, ring A, m, n, -L1-, ring B, RB, and p are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.
    Type: Grant
    Filed: November 20, 2015
    Date of Patent: August 14, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Xing Dai, Jared N. Cumming, Hong Liu, Jack D. Scott
  • Patent number: 9921161
    Abstract: Methods and systems are provided for estimating locations of sub-wavelength-sized emitters, which may be sparsely arrayed among inactive emitters, in one or more dimensions to synthesize a super-resolved image. The emitter emits light in response to structured illumination, which may be acousto-optically generated. The structured illumination is translated, and a detector, such as a camera pixel, senses the emitted linear or nonlinear response, producing a periodic signal. A processor computes a phase of the signal using phase shifting interferometry and uses it to estimate the emitter location with resolution finer than a quarter of the illumination wavelength. Modulation depth and/or amplitude of the signal may be used to estimate emitter size and/or evaluate location fidelity. Optical sectioning or extended depth of field may be provided by controlling spatial coherence of the illumination. Encoding and decoding emitter locations with non-periodic patterns is also described.
    Type: Grant
    Filed: January 8, 2016
    Date of Patent: March 20, 2018
    Inventor: Daniel Feldkhun
  • Patent number: 9782411
    Abstract: {4-[5-(3-chloro-phenoxy)-oxazolo[5,4-d]pyrimidin-2-yl]-2,6-dimethyl-phenoxy}-acetic acid or a pharmaceutically acceptable salt thereof for use in the prevention or treatment of AKI (acute kidney injury). Medicament and pharmaceutical composition thereof.
    Type: Grant
    Filed: October 15, 2014
    Date of Patent: October 10, 2017
    Assignee: SANOFI
    Inventors: Véronique Briand, Sabine Gratzer, Thomas Huebschle, Philip Janiak, Dieter Kadereit, Ashfaq Parkar, Bruno Poirier, Matthias Schaefer, Paulus Wohlfart
  • Patent number: 9777012
    Abstract: Compounds of Formula I: and compounds of Formula II: are provided. Pharmaceutical compositions comprising either the compound of Formula I or Formula II are disclosed. Methods of treating patients having cancer are provided by administering to the patient a therapeutically effective amount of one or more compounds having Formula I or Formula II to treat the patient. The compounds of Formula I or II are preferably conformationally restricted furo[2,3-d]pyrimidines having dual inhibition of microtubule assembly and receptor tyrosine kinases.
    Type: Grant
    Filed: December 16, 2015
    Date of Patent: October 3, 2017
    Assignee: Duquesne University of the Holy Spirit
    Inventor: Aleem Gangjee
  • Patent number: 9745320
    Abstract: A five-and-six-membered heterocyclic compound as represented by general formula I, pharmaceutically acceptable salt, metabolite, metabolic precursors or drug precursors thereof, preparation method, pharmaceutical composition, and use thereof; the five-and-six-membered heterocyclic compound has activity as a Janus kinase (JAK) inhibitor, and can be used to prepare drugs for treating diseases caused by the abnormal activity of kinase, such as cell proliferation diseases like cancer.
    Type: Grant
    Filed: January 17, 2014
    Date of Patent: August 29, 2017
    Assignee: GUANGZHOU MAXINOVEL PHARMACEUTICALS CO., LTD.
    Inventors: Zusheng Xu, Nong Zhang, Qingrui Sun, Tinghan Wang
  • Patent number: 9604996
    Abstract: The present application relates to novel 2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidine-6-carboxamide derivatives (“thienouracil”-carboxamides), to processes for their preparation, to their use alone or in combinations for the treatment and/or prevention of diseases and to their use for the preparation of medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of pulmonary and cardiovascular disorders.
    Type: Grant
    Filed: October 2, 2014
    Date of Patent: March 28, 2017
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Michael Härter, Martina Delbeck, Bernd Kalthof, Klemens Lustig, Niels Lindner, Raimund Kast, Pierre Wasnaire, Frank Süβmeier
  • Patent number: 9527832
    Abstract: The invention relates to novel substituted condensed pyrimidine compounds of general formula (I) in which the chemical groupings, substituents and indices are as defined in the description, and to their use as medicaments, in particular as medicaments for the treatment of conditions and diseases that can be treated by inhibition of the PDE4 enzyme.
    Type: Grant
    Filed: October 15, 2015
    Date of Patent: December 27, 2016
    Assignee: GRÜNENTHAL GMBH
    Inventors: Ingo Konetzki, Florian Jakob, Tobias Craan, Christian Hesslinger, Paul Ratcliffe, Antonio Nardi
  • Patent number: 9486455
    Abstract: The present application relates to compounds and methods for treating pain and other conditions related to TRPV3.
    Type: Grant
    Filed: March 4, 2011
    Date of Patent: November 8, 2016
    Assignee: HYDRA BIOSCIENCES, INC.
    Inventors: Jayhong A. Chong, Christopher Fanger, Glenn R. Larsen, Magdalene M. Moran, Howard Ng, Amy Ripka, Dennis John Underwood, Manfred Weigele, Xiaoguang Zhen
  • Patent number: 9440992
    Abstract: There are disclosed novel 5-substituted 7-amino-[1,3]thiazolo[4,5-d]pyrimidine derivatives of formula (I) wherein R1, R2, R3, R4 and R5 are as defined in the specification, and pharmaceutically acceptable salts thereof, together with processes for their preparation, pharmaceutical compositions comprising them and their use in therapy. The compounds of formula (I) are CX3CR1 receptor antagonists and are thereby particularly useful in the treatment or prophylaxis of neurodegenerative disorders, demyelinating disease, cardio- and cerebrovascular atherosclerotic disorders, peripheral artery disease, rheumatoid arthritis, pulmonary diseases such as COPD, asthma or pain.
    Type: Grant
    Filed: December 28, 2010
    Date of Patent: September 13, 2016
    Assignee: Acturum Life Science AB
    Inventors: Gunnar Nordvall, Colin Ray, Tobias Rein, Daniel Sohn
  • Patent number: 9309402
    Abstract: Disclosed are a biodegradable resin composition comprising a copolymer (A) with a weight average molecular weight of 1,000 to 30,000, which comprises a constituent unit (a-1) derived from a multivalent carboxylic acid except for an amino acid and a constituent unit (a-2) derived from a hydroxycarboxylic acid, and a biodegradable resin (B), which has excellent hydrolyzability and excellent transparency; and a biodegradable molded article composed of this biodegradable resin composition.
    Type: Grant
    Filed: March 30, 2012
    Date of Patent: April 12, 2016
    Assignee: MITSUI CHEMICALS, INC.
    Inventors: Shintaro Maekawa, Shinichi Usugi, Hitoshi Onishi
  • Patent number: 9290511
    Abstract: The present invention provides compounds of formula (I): (Formula (I); wherein A, R1, R2, R3I, V, X, and Z are defined herein, which are potassium channel inhibitors. The invention further provides pharmaceutical compositions comprising the compounds of formula (I) and their use in therapy, in particular in treatment of diseases or conditions that are mediated by Kir3.1 and/or Kir3.4 or any heteromultimers thereof, or that require inhibition of Kir3.1 and/or Kir3.4 or any heteromultimers thereof.
    Type: Grant
    Filed: November 15, 2012
    Date of Patent: March 22, 2016
    Assignee: Xention Limited
    Inventors: David Madge, Fiona Chan, Derek Edward John, Simon D. Edwards, Richard Blunt, Basil Hartzoulakis, Lindsay Brown
  • Patent number: 9271980
    Abstract: The present invention is concerned with deuterium-enriched pyrimidine compounds of formula I, their derivatives and pharmaceutically acceptable salts and methods of use thereof, The compounds of formula I are useful for the prevention and treatment of liver fibrosis and cirrhosis, hepatocellular carcinoma, neuroendrcrine neoplasia including metastasis and fibrosis fibrotic processes associated with neuroendocrine cell dysregulation for example Crohn's disease, pulmonary arterial hypertension, pulmonary hypertension associated with chronic obstructive pulmonary disease (COPD), right ventricular hypertrophy, pulmonary vascular remodeling, asthma, cystic fibrosis, hypertension, ischemic stroke, angina pectoris, congestive heart failure, arrhythmia, arterial fibrillation, gastrointestinal disorders, anxiety, depression, stress disorders, post-traumatic stress disorder, obsessive compulsive disorders, demyelinating diseases, acute or chronic cerebrovascular damage, cerebral infarction, subarachanoid hemorrhage
    Type: Grant
    Filed: October 12, 2012
    Date of Patent: March 1, 2016
    Inventor: Daljit Singh Dhanoa
  • Patent number: 9198909
    Abstract: The current study reports novel inhibitors of s-nitrosoglutathione reductase (GSNOR) identified that specifically inhibit GSNOR among the alcohol dehydrogenases. These inhibitors may bind into the GSNO binding site and inhibit GSNOR at multiple places in its kinetic pathway. These molecules inhibit GSNOR in a dose dependent manner and demonstrate that GSNOR actively regulates the s-nitrosylation of proteins against incoming low molecular weight nitrosothiols. These compounds are useful in method of treatment of diseases such as asthma, chronic obstructive pulmonary disease, heart disease, heart failure, heart attack, hypertension, atherosclerosis, restenosis, impotence, Parkinson's disease, Alzheimer's disease, amyotrophic lateral sclerosis, stroke, septic shock, cardiogenic shock, endotoxic shock, toxic shock syndrome, systemic inflammatory response syndrome, and other inflammatory diseases.
    Type: Grant
    Filed: June 11, 2010
    Date of Patent: December 1, 2015
    Assignee: Indiana University Research and Technology Corporation
    Inventor: Paresh Sanghani
  • Patent number: 9150578
    Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R1 to R6, A, B, C, n, p, q and r are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, pharmaceutical preparations which contain compounds of this kind and their use as medicaments.
    Type: Grant
    Filed: January 22, 2013
    Date of Patent: October 6, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventor: Matthias Treu
  • Patent number: 9120807
    Abstract: Compounds of formula (I) are A2B receptor antagonists, wherein R1 is optionally substituted aryl or an optionally substituted 5- or 6-membered heteroaryl ring; R2 and R3 are independently selected from hydrogen, C1-C6 alkyl, C3-C8 cycloalkyl, C3-C8 cycloalkyl-(C1-C6)-alkyl, aryl-(C1-C6)-alkyl optionally substituted in the ring part thereof, a 5- or 6-membered monocyclic heterocyclic group optionally linked via a C1-C6 alkylene chain and optionally substituted in the ring part thereof, benzimidazol-2-yl-methyl, pyrid-3-yl-carbonyl, or (1-methyl-piperidin-4-yl)-carbonyl-methyl; or R2 and R3 taken together with the nitrogen atom to which they are attached form an optionally substituted 5- or 6-membered ring; R4 is C1-C3 alkyl, C2-C3 alkenyl, —N(—R5)—R6, or optionally substituted heteroarylmethylamino; and R5 and R6 are independently selected from hydrogen or C1-C3 alkyl; or R5 and R6 taken together with the nitrogen atom to which they are attached form an optionally substituted 4- to 6-membered saturated ring.
    Type: Grant
    Filed: September 19, 2008
    Date of Patent: September 1, 2015
    Assignee: Vernalis (R&D) Ltd.
    Inventors: Allan Jordan, Simon Bedford, Klenke Burkhard, Ian Yule, Karine Poullennec
  • Patent number: 9096613
    Abstract: The present invention provides methods and compositions comprising compounds useful for stimulating neurogenesis. The methods and compositions comprising compounds are also useful for inhibiting neuronal degeneration. Thus, the present invention can be used in the treatment of diseases and conditions characterized by neuronal loss and reduced neurogenesis including Alzheimer's disease, stroke, traumatic brain injury, traumatic nerve injury, and depression. This invention is useful for research products including single agents or mixtures of agents to promote, proliferate, differentiate, or maintain neurons from stem or progenitor cells.
    Type: Grant
    Filed: November 13, 2013
    Date of Patent: August 4, 2015
    Assignee: Neuronascent, Inc.
    Inventor: Judith Kelleher-Andersson
  • Patent number: 9096614
    Abstract: A series of thiazolo[5,4-d]pyrimidine derivatives of formula (I) or an N-oxide thereof, or a pharmaceutically acceptable salt or solvate thereof: (I) Q represents a group of formula (Qa), (Qb), (Qc), (Qd) or (Qe) are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases; and organ and cell transplant rejection.
    Type: Grant
    Filed: November 8, 2012
    Date of Patent: August 4, 2015
    Inventors: Daniel Christopher Brookings, Daniel James Ford, Richard Jeremy Franklin, Anant Ramrao Ghawalkar, Claire Louise Kulisa, Judi Charlotte Neuss, James Thomas Reuberson
  • Publication number: 20150148322
    Abstract: The invention relates to novel piperidino-dihydrothienopyrimidine sulfoxides of formula I, wherein Ring A is a 6-membered aromatic ring which may optionally comprise one or two nitrogen atoms and wherein R is Cl and wherein R may be located either in the para-, meta- or ortho-position of Ring A, wherein S* is a sulphur atom that represents a chiral center, and all pharmaceutically acceptable salts, enantiomers and racemates, hydrates and solvates thereof and the use of these compounds for the treatment of inflammatory or allergic diseases of the respiratory tract such as COPD or asthma.
    Type: Application
    Filed: March 15, 2012
    Publication date: May 28, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Pascale A.J. Pouzet, Peter Nickolaus, Ulrike Werthmann, Rogelio P. Frutos, Bing-Shiou Yang, Soojin Kim, Jason Alan Mulder, Nitinchandra Patel, Chris H. Senanayake, Thomas G. Tampone, Xudong Wei
  • Patent number: 9040544
    Abstract: The invention relates to oxazolopyrimidine compounds of formula I, where A, R1 and R2 are defined as stated in the claims. The compounds of formula I are suitable, for example, for wound healing.
    Type: Grant
    Filed: January 14, 2011
    Date of Patent: May 26, 2015
    Assignee: Sanofi
    Inventors: Dieter Kadereit, Matthias Schaefer, Stephanie Hachtel, Axel Dietrich, Thomas Huebschle, Katrin Hiss
  • Publication number: 20150126513
    Abstract: The present invention provides for compounds of formula (I): wherein R1-R4 and n are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.
    Type: Application
    Filed: July 13, 2012
    Publication date: May 7, 2015
    Applicant: Novartis AG
    Inventors: Christine Hiu-Tung Chen, Donovan Noel Chin, Lucian V. DiPietro, Jianmei Fan, Mark G. Palermo, Michael David Shultz, Bakary-Barry Toure
  • Patent number: 9018209
    Abstract: The present invention relates to compounds according to the formula I: Where Ra is H or an optionally OH-substituted C1-C3 alkyl; R1 is OR1, an optionally substituted C4-12 carbocyclic group which may be saturated or unsaturated (including aromatic) or an optionally substituted heterocyclic group; R1 is an optionally substituted C1-C14 hydrocarbyl group or an optionally substituted heterocyclic group; R2, R3 and R4 are each independently H, an optionally substituted C1-C4 alkyl group (preferably CH3, CH2CH3 or CF3), halogen (preferably F, Cl, Br), OR, CN, NO2, a C1-C6 thioether, a C1-C6 thioester group, an optionally substituted CO2R group, an optionally substituted COR group or an optionally substituted OCOR group (preferably R4 is H); R is H or an optionally substituted C1-C6 alkyl group; RHET is an optionally substituted heterocyclic group; and pharmaceutically acceptable salts, solvates or polymorphs thereof.
    Type: Grant
    Filed: September 25, 2006
    Date of Patent: April 28, 2015
    Assignee: Yale University
    Inventors: William L. Jorgensen, Juliana Ruiz-Caro, Andrew D. Hamilton
  • Publication number: 20150111876
    Abstract: A sulfur-containing bicyclic compound having a PAM action of GABAB, and it use for preventing and/or treating schizophrenia, CIAS, cognitive impairment, fragile X syndrome, autism spectrum disorder, spasticity, anxiety disorder, substance addiction, pain, fibromyalgia, or Charcot-Marie-Tooth disease. A pharmaceutical composition for preventing and/or treating schizophrenia, cognitive impairment associated with schizophrenia (CIAS), cognitive impairment, fragile X syndrome, autism spectrum disorder, spasticity, anxiety disorder, substance addiction, pain, fibromyalgia, Charcot-Marie-Tooth disease, or the like, which has a positive allosteric modulator (PAM action) of GABAB.
    Type: Application
    Filed: October 17, 2014
    Publication date: April 23, 2015
    Applicant: Astellas Pharma Inc.
    Inventors: Nobuyuki Shiraishi, Hiroaki Hoshii, Wataru Hamaguchi, Eriko Honjo, Tomofumi Takuwa, Yuji Kondo, Takayuki Goto
  • Publication number: 20150111894
    Abstract: The present invention provides an aromatic ring compound having a melanin-concentrating hormone receptor antagonistic action and useful as an agent for the prophylaxis or treatment of obesity and the like. The present invention relates to a compound represented by the formula wherein each symbol as defined in the specification, or a salt thereof.
    Type: Application
    Filed: May 9, 2013
    Publication date: April 23, 2015
    Inventors: Shizuo Kasai, Hideyuki Igawa, Masashi Takahashi, Asato Kina
  • Publication number: 20150105407
    Abstract: The present invention provides substituted pyrrolo-, furano-, and cyclopentylpyrimidine bicyclic compounds of Formula III, and Formula IV, and pharmaceutically acceptable salts, solvates, and hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, such as for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds and pharmaceutical compositions for treating tumor cells and inhibiting mitosis of cancerous cells.
    Type: Application
    Filed: December 17, 2014
    Publication date: April 16, 2015
    Inventor: Aleem Gangjee
  • Publication number: 20150105406
    Abstract: The present patent application relates to a pharmaceutical composition comprising a TRPA1 antagonist and an analgesic agent. Particularly, the present patent application provides a pharmaceutical composition comprising a thienopyrimidinedione compound as a TRPA1 antagonist and an analgesic agent; and use of such composition for treating pain in a subject.
    Type: Application
    Filed: October 14, 2014
    Publication date: April 16, 2015
    Inventors: Srinivas GULLAPALLI, Praveen Kumar GUPTA, Maulik Nitinkumar GANDHI, Sravan MANDADI
  • Patent number: 9006253
    Abstract: The invention provides a crystal of 2-(3,4-dichlorobenzyl)-5-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidine-6-carboxylic acid (which has the chemical structure shown below) and a mixed crystal comprising such a crystal. The invention also provides methods of producing such crystals, pharmaceutical compositions comprising such crystals, and methods of modulating phosphodiesterase-9 activity and treating disorders such as overactive bladder syndrome by administration of an effective amount of the crystals.
    Type: Grant
    Filed: March 26, 2014
    Date of Patent: April 14, 2015
    Assignee: ASKA Pharmaceutical Co., Ltd.
    Inventors: Hiroyuki Hayashi, Takayoshi Nakagawa, Koichi Miyazaki
  • Patent number: 9006252
    Abstract: Fused multicyclic compounds of formula (I): wherein R?, R?, X, Y, Z, A, B, C, D, and n are defined herein. Also disclosed are a method for inhibiting protein kinase (e.g., Aurora kinase) activity and a method for treating a protein kinase mediated disorder (e.g., cancer) with these compounds.
    Type: Grant
    Filed: September 22, 2009
    Date of Patent: April 14, 2015
    Assignee: National Health Research Institutes
    Inventors: Hsing-Pang Hsieh, Selvaraj Mohane Coumar, Yu-Sheng Chao
  • Patent number: 8999973
    Abstract: The present invention relates to a thieno[3,2-d]pyrimidine derivative of formula (I), or a pharmaceutically acceptable salt, hydrate or solvate thereof, which has an excellent inhibitory activity on protein kinases, and a pharmaceutical composition comprising the same is effective in preventing or treating abnormal cell growth diseases.
    Type: Grant
    Filed: January 31, 2011
    Date of Patent: April 7, 2015
    Assignees: Hanmi Science Co., Ltd, Korea Institute of Science and Technology, Catholic University Industry Academic Cooperation Foundation
    Inventors: Jung Beom Son, Seung Hyun Jung, Wha II Choi, Young Hee Jung, Jae Yul Choi, Ji Yeon Song, Kyu Hang Lee, Jae Chul Lee, Eun Young Kim, Young Gil Ahn, Maeng Sup Kim, Hwan Geun Choi, Tae Bo Sim, Young Jin Ham, Dong-sik Park, Hwan Kim, Dong-Wook Kim
  • Publication number: 20150094305
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.
    Type: Application
    Filed: September 25, 2014
    Publication date: April 2, 2015
    Inventors: Donna ROMERO, Craig E. MASSE, Shaughnessy ROBINSON, Jeremy Robert GREENWOOD, Geraldine C. HARRIMAN
  • Publication number: 20150094275
    Abstract: The present invention provides novel heteroaryl compounds having a pyrimidine-containing core that is linked to a 4-trifluoromethoxyphenyl group via an amine linker. Such compounds are useful for the treatment of cancers.
    Type: Application
    Filed: November 13, 2014
    Publication date: April 2, 2015
    Applicants: THE SCRIPPS RESEARCH INSTITUTE, DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Nathanael S. GRAY, Jianming ZHANG, Barun OKRAM, Xianming DENG, Jae Won CHANG, Amy WOJCIECHOWSKI
  • Patent number: 8987278
    Abstract: The present invention is related to novel thienopyrimidinedione derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.
    Type: Grant
    Filed: June 25, 2013
    Date of Patent: March 24, 2015
    Assignee: Glenmark Pharmaceuticals S.A.
    Inventors: Sukeerthi Kumar, Abraham Thomas, Nayan Taterao Waghmare, Sanjay Margal, Neelima Khairatkar-Joshi, Indranil Mukhopadhyay
  • Publication number: 20150080416
    Abstract: This invention provides thieno[2,3-d]pyrimidine derivatives containing isoxazole heterocycle represented by formula (I), or pharmaceutically acceptable salts thereof Wherein: R1 and R2 may be the same or different and is independently to each other selected from H, C1-6 alkyl, C1-6 alkoxy, halo-C1-6 alkyl or halo-C1-6 alkoxy, aryl group optionally substituted by R7 or heteroaryl group optionally substituted by R8; or R1 and R2 together with the carbon atoms to which they are attached, may form a 4- to 6-membered carbocyclic ring or heterocyclic ring; said carbocyclic ring or heterocyclic ring is optionally substituted by H, C1-6 alkyl, halogen, nitro, or amino; said heterocyclic ring contains at least one heteroatom selected from N, O or S; Z is —NR6—, C(R6)2, —S— or —O—, in which R5 is H or C1-6 alkyl, and R6 is the same or different, selected from H, C1-6 alkyl or hydroxyl substituted C1-6 alkyl; R3 is selected from H, halogen, C1-6 alkyl, C1-6 alkoxy, halo-C1-6 alkyl or halo-C1-6 alkoxy; n is an inte
    Type: Application
    Filed: September 19, 2012
    Publication date: March 19, 2015
    Applicant: FUJIAN INSTITUTE OF RESEARCH ON THE STRUCTURE OF MATTER, CHINESE ACADEMY OF SCIENCES
    Inventors: Canzhong Lu, Jianping Yong
  • Publication number: 20150071930
    Abstract: A method of preventing and/or treating a cancer including co-administering a c-Met inhibitor and a beta-catenin inhibitor to a subject in need thereof, a pharmaceutical composition comprising a c-Met inhibitor and a beta-catenin inhibitor, and a kit comprising a pharmaceutical composition comprising a c-Met inhibitor, and a pharmaceutical composition comprising a beta-catenin inhibitor packaged together.
    Type: Application
    Filed: September 8, 2014
    Publication date: March 12, 2015
    Inventors: Ji Min Lee, Kyung Ah Kim
  • Publication number: 20150072998
    Abstract: Compounds and methods of modulating 15-PGDH activity, modulating tissue prostaglandin levels, treating disease, diseases disorders, or conditions in which it is desired to modulate 15-PGDH activity and/or prostaglandin levels include 15-PGDH inhibitors and 15-PGDH activators described herein.
    Type: Application
    Filed: April 16, 2013
    Publication date: March 12, 2015
    Inventors: Sanford Markowitz, James K.V. Willson, Bruce A. Posner, Joseph Ready, Yongyou Zhang, Hsin-Hsiung Tai, Melissa Moss, Monika Antczak, Stanton Gerson, KiBeom Bae, Sung Yeun Yang, Amar Desai
  • Publication number: 20150072959
    Abstract: Substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
    Type: Application
    Filed: November 13, 2014
    Publication date: March 12, 2015
    Inventors: Dane Goff, Jing Zhang, Catherine Sylvain, Rajinder Singh, Sacha Holland, Jiaxin Yu, Thilo J. Heckrodt, Pingyu Ding
  • Publication number: 20150065501
    Abstract: The invention relates to N-substituted hetero-bicyclic furanone compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to methods and uses of these N-substituted hetero-bicyclic furanone compounds, and of compositions comprising thereof, for combating and controlling animal pests. Furthermore the invention relates also to pesticidal methods of applying such N-substituted hetero-bicyclic furanone compounds. The N-substituted hetero-bicyclic furanone compounds of the present invention are defined by the following formula I: wherein A, X, Het, W1, W2, W3, R1, R2 and R4 are defined as in the description.
    Type: Application
    Filed: March 27, 2013
    Publication date: March 5, 2015
    Inventors: Nina Gertrud Bandur, Ralph Paulini, Florian Kaiser, Arun Narine, Joachim Dickhaut, Karsten Körber
  • Patent number: 8969557
    Abstract: The present invention provides compounds useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: March 3, 2015
    Assignee: Nimbus Apollo, Inc.
    Inventors: Geraldine C. Harriman, Craig E. Masse, James Harwood, Sathesh Bhat, Jeremy Robert Greenwood
  • Publication number: 20150057286
    Abstract: This invention relates to bis-amido pyridines of general formula (I) their use as SMAC mimetics, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The groups R1 to R4 have the meanings given in the claims and in the specification.
    Type: Application
    Filed: August 20, 2014
    Publication date: February 26, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventor: Ulrich REISER
  • 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