Carbocyclic Ring Containing Patents (Class 544/321)
  • Patent number: 10738032
    Abstract: There is provided a compound of formula (I) which is an inhibitor of the family of p38 mitogen-activated protein kinase enzymes, and to its use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as asthma and COPD.
    Type: Grant
    Filed: February 26, 2019
    Date of Patent: August 11, 2020
    Assignee: Respivert Limited
    Inventors: Kazuhiro Ito, Catherine Elisabeth Charron, John King-Underwood, Stuart Thomas Onions, Alistair Ian Longshaw, Rudy Broeckx, Walter Filliers, Alex Copmans
  • Patent number: 10336768
    Abstract: The present invention relates to 2-amino-4-arylpyrimidine and 2-amino-4-aryltriazine compounds as inhibitors of heat shock protein 90 family of chaperone proteins. The invention also features pharmaceutical compositions and kits that include the compounds and compositions of the invention. The invention further relates to the medical use of these compounds and compositions for the treatment of a disorder in a subject. For example, the disorder is a neurodegenerative disease.
    Type: Grant
    Filed: June 15, 2015
    Date of Patent: July 2, 2019
    Assignees: Yuma Therapeutics, Inc., The Brigham and Women's Hospital, Inc.
    Inventors: Gregory D. Cuny, Marcie A. Glicksman, Kevin J. Hodgetts, Steven L. Mathieu, Yukari Y. Perrella, Vincent Darmency, Hrvoje Lusic
  • Patent number: 10266519
    Abstract: There is provided a compound of formula (I) which is an inhibitor of the family of p38 mitogen-activated protein kinase enzymes, and to its use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as asthma and COPD.
    Type: Grant
    Filed: November 14, 2017
    Date of Patent: April 23, 2019
    Assignee: RESPIVERT LIMITED
    Inventors: Kazuhiro Ito, Catherine Elisabeth Charron, John King-Underwood, Stuart Thomas Onions, Alistair Ian Longshaw, Rudy Broeckx, Walter Filliers, Alex Copmans
  • Patent number: 10227333
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of Olig2. Also described herein are methods of using such Olig2 inhibitors, alone and in combination with other compounds, for treating cancer and other diseases. In particular the Olig2 inhibitors may be used to treat glioblastoma.
    Type: Grant
    Filed: February 10, 2016
    Date of Patent: March 12, 2019
    Assignee: CURTANA PHARMACEUTICALS, INC.
    Inventors: Graham Beaton, Fabio Tucci, Satheesh B. Ravula, Hua-Yu Wang
  • Patent number: 9850231
    Abstract: There is provided a compound of formula (I) which is an inhibitor of the family of p38 mitogen-activated protein kinase enzymes, and to its use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as asthma and COPD.
    Type: Grant
    Filed: July 10, 2015
    Date of Patent: December 26, 2017
    Assignee: Respivert Limited
    Inventors: Kazuhiro Ito, Catherine Elisabeth Charron, John King-Underwood, Stuart Thomas Onions, Alistair Ian Longshaw, Rudy Broeckx, Walter Filliers, Alex Copmans
  • Patent number: 9850233
    Abstract: There are provided compounds of formula I, wherein: Y represents NR2R3; one of R2 and R3 represents —[C2-4 alkylene-O]1-12—[C2-4 alkylene]-R2a and the other of R2 and R3 has a meaning given in the description; and R, R1, R2a, Ra, Rb, Q, X and Y have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
    Type: Grant
    Filed: July 12, 2016
    Date of Patent: December 26, 2017
    Assignees: Respivert Limited, Topivert Pharma Limited
    Inventor: Matthew Colin Thor Fyfe
  • Patent number: 9446995
    Abstract: Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds.
    Type: Grant
    Filed: May 17, 2013
    Date of Patent: September 20, 2016
    Assignee: Illinois Institute of Technology
    Inventor: Hyun-Soon Chong
  • Patent number: 9108950
    Abstract: There is provided a compound of formula (I) which is an inhibitor of the family of p38 mitogen-activated protein kinase enzymes, and to its use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as asthma and COPD.
    Type: Grant
    Filed: October 3, 2012
    Date of Patent: August 18, 2015
    Assignee: Respivert, Ltd.
    Inventors: Kazuhiro Ito, Catherine Elisabeth Charron, John King-Underwood, Stuart Thomas Onions, Alistair Ian Longshaw, Rudy Broeckx, Walter Filliers, Alex Copmans
  • Publication number: 20150148327
    Abstract: The invention provides certain substituted pyridines of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, Cy, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
    Type: Application
    Filed: June 17, 2013
    Publication date: May 28, 2015
    Applicant: Merck Canada Inc.
    Inventors: Andrew M. Haidle, Sandra Lee Knowles, Solomon D. Kattar, Denis Deschenes, Jason Burch, Joel Robichaud, Matthew Christopher, Michael D. Altman, James P. Jewell, Alan B. Northrup, Marc Blouin, John Michael Ellis, Hua Zhou, Christian Fischer, Adam J. Schell, Michael H. Reutershan, Brandon M. Taoka, Anthony Donofrio, Joel Robichaud
  • Publication number: 20150141446
    Abstract: Pyrimidine compounds and their use in controlling pests such as insects and other invertebrates are provided. Further embodiments, forms, objects, features, advantages, aspects and benefits shall become apparent from the description.
    Type: Application
    Filed: November 19, 2014
    Publication date: May 21, 2015
    Inventors: Tony K. Trullinger, Timothy C. Johnson, Ricky Jim Hunter
  • Publication number: 20150133457
    Abstract: The present invention relates to pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment and/or prevention of a proliferation disorder, a cancer, a tumor, an inflammatory disease, an autoimmune disease, psoriasis, dry eye or an immunologically related disease, and in some embodiments diseases or disorders related to the dysregulation of kinase such as, but not limited to, EGFR (including HER), Alk, PDGFR, BLK, BMX/ETK, FLT3(D835Y), ITK, TEC, TXK, BTK, or JAK, and the respective pathways.
    Type: Application
    Filed: July 11, 2014
    Publication date: May 14, 2015
    Inventors: Xiao XU, Xiaobo WANG, Long MAO, Li ZHAO, Biao XI
  • Patent number: 9018218
    Abstract: The invention relates to substituted pyrimidine ammonia compounds. The structure of the compounds is represented as the general formula (I): The groups are as defined as specification. The compound represented by formula (I) can be used in the prevention of plants diseases caused by a plurality of pathogenic bacteria such as oomycota, basidiomycota, ascomycota, and fungi imperfecti, and due to these compounds have good bioactivity, which make them have very good effects at very low doses, especially more effective to powdery mildew of wheat. Therefore, the present invention relates to the use of the compounds having general formula I as fungicides, both in agriculture and other fields.
    Type: Grant
    Filed: November 18, 2011
    Date of Patent: April 28, 2015
    Assignees: Sinochem Corporation, Shenyang Research Institute of Chemical Industry Co., Ltd.
    Inventors: Changling Liu, Baoshan Chai, Zhinian Li, Xufeng Sun, Zhonggang Shan
  • Patent number: 9006433
    Abstract: The present invention relates to substituted pyrimidines useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
    Type: Grant
    Filed: April 18, 2011
    Date of Patent: April 14, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Changyou Zhou, Wuxin Zou, Yuxia Hua, Qun Dang
  • Patent number: 8969341
    Abstract: The invention relates to compounds of formula (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.
    Type: Grant
    Filed: November 28, 2012
    Date of Patent: March 3, 2015
    Assignee: Novartis AG
    Inventors: Pascal Furet, Vito Guagnano, Philipp Holzer, Robert Mah, Keiichi Masuya, Achim Schlapbach, Stefan Stutz, Andrea Vaupel
  • Patent number: 8962641
    Abstract: The invention relates to new pyrrolidine derivatives of the formula wherein R1 to R3, Ar, L T and n are as defined in the description and claims, to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: April 7, 2014
    Date of Patent: February 24, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Martin Fleck, Annekatrin Heimann, Niklas Heine, Bernd Nosse, Gerald Juergen Roth
  • Patent number: 8946249
    Abstract: Compound of Formula A and pharmaceutically acceptable salts thereof and crystalline Forms I and II of Compound of Formula A! Also, methods for the preparation of such compounds, pharmaceutical compositions comprising such compounds, and methods for their uses.
    Type: Grant
    Filed: December 12, 2013
    Date of Patent: February 3, 2015
    Assignee: Hutchison Medipharma Limited
    Inventors: Wei-Guo Su, Weihan Zhang, Hong Jia, Yumin Cui, Yongxin Ren, Yang Sai, Zhenping Wu, Wenji Li, Jiangyong Shao, Zhenping Tian
  • Patent number: 8946248
    Abstract: HIV replication inhibitors of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein A is —CH2—CH2—, —CH?CH—, —C?C—; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, R2 hydroxy, halo, C1-6alkyl, carboxyl, cyano, —C(?O)R6, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl; X1 is —NR1—, —O—, —S—, —S(?O)p—; R3 is H, C1-6alkyl, halo; R4 is H, C1-6alkyl, halo; R5 is nitro, amino, mono- and diC1-4alkylamino, aryl, halo, —CHO, —CO—R6, —COOR7, —NH—C(?O)H, —NH—C(?O)R6, —CH?N—O—R8; R6 is C1-4alkyl, amino, mono- or di(C1-4alkyl)amino or polyhaloC1-4alkyl; R7 is hydrogen, C1-6alkyl, arylC1-6alkyl; R8 is hydrogen, C1-6alkyl, aryl; p is 1 or 2; aryl is optionally substituted phenyl; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compounds and compositions.
    Type: Grant
    Filed: September 29, 2005
    Date of Patent: February 3, 2015
    Assignee: Janssen R&D Ireland
    Inventors: Jerôme Emile Georges Guillemont, Jan Heeres, Paulus Joannes Lewi
  • Patent number: 8940748
    Abstract: In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (I): and include stereoisomers thereof, and pharmaceutically acceptable salts of said compounds stereoisomers, wherein each of R1, R2, R3, R4, R5, R9, ring A, ring B, m, n, p, -L1-, -L2-, and -L3- is selected independently and as defined herein. The novel iminothiadiazine dioxide compounds of the invention have surprisingly been found to exhibit properties which are expected to render them advantageous as BACE inhibitors and/or for the treatment and prevention of various pathologies related to ?-amyloid (“A?”) production. 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 in treating pathologies associated with amyloid beta (A?) protein, including Alzheimer's disease, are also disclosed.
    Type: Grant
    Filed: March 21, 2014
    Date of Patent: January 27, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jack D. Scott, Andrew W. Stamford, Eric J. Gilbert, Jared N. Cumming, Ulrich Iserloh
  • Publication number: 20150011574
    Abstract: The present invention provides a compound which enhances the production of erythropoietin. The present invention provides a compound represented by the formula (1) wherein R1: an aromatic hydrocarbon ring group or an aromatic heterocyclic group; R2: a hydrogen atom, an alkyl group, or a heterocycloalkyl group; R3: a hydrogen atom or an alkyl group; A: a hydrogen atom or a hydroxy group; L: —NHCO— or —OCH2—; and X: a nitrogen atom or ?CH—.
    Type: Application
    Filed: September 24, 2014
    Publication date: January 8, 2015
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Tatsuya NISHI, Naoki TANAKA, Ryoko KITAZAWA, Riki GOTO, Takashi ISHIYAMA
  • Patent number: 8927563
    Abstract: There is provided a compound of formula I, which compound has antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases, e.g., Src and Lck) and has use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
    Type: Grant
    Filed: April 1, 2014
    Date of Patent: January 6, 2015
    Assignees: Respivert Limited, Topivert Pharma Limited
    Inventor: Matthew Colin Thor Fyfe
  • Patent number: 8927534
    Abstract: The present invention is related to a compound of formula (I), wherein A is a nonaromatic heterocyclic ring, Ar is either absent or phenylene; ? is a radical of formula (II), R2 is a hydrophobic moiety; and G is a radical containing one or more moieties selected from the group consisting of NH, OH and a basic moiety. The compounds are inhibitors of integrins, especially antagonists of the fibronectin receptor alpha5beta1, useful as anti-angiogenic agents.
    Type: Grant
    Filed: January 31, 2007
    Date of Patent: January 6, 2015
    Assignee: Shire Orphan Therapies GmbH
    Inventors: Gunther Zischinsky, Roland Stragies, Frank Osterkamp, Dirk Scharn, Gerd Hummel, Holger Kalkhof, Grit Zahn, Doerte Vossmeyer, Claudia Christner-Albrecht, Ulrich Reineke
  • Publication number: 20140363588
    Abstract: Provided is a polymer film containing at least one of a compound represented by formula (1) of hydrates, solvates, or salts thereof. Y is a methine group or nitrogen atom. Qa, Qb, and Qc are a single bond or a divalent linking group. Ra, Rb, and Rc, are hydrogen atom, alkyl group, alkenyl group, alkynyl group, aryl group, cyano group, halogen group, or heterocyclic group. X2 is a single bond or a divalent linking group. X1 is a single bond or a predetermined divalent linking group.
    Type: Application
    Filed: August 27, 2014
    Publication date: December 11, 2014
    Applicant: FUJIFILM Corporation
    Inventors: Aiko YAMAMOTO, Satoshi TANAKA, Teruki NIORI, Masato NAGURA, Masaki NORO, Aiko YOSHIDA, Nobutaka FUKAGAWA, Yasukazu KUWAYAMA
  • Publication number: 20140357616
    Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1a, R1b, R1c, X, and Y are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as Cdc7 and methods of treating diseases such as cancer.
    Type: Application
    Filed: July 28, 2014
    Publication date: December 4, 2014
    Inventors: Thomas D. Penning, Keith W. Woods, Chunqiu Lai, Alan S. Florjancic, Yunsong Tong
  • Patent number: 8901120
    Abstract: In one aspect, the invention relates to substituted N-phenylpyrimidin-2-amine analogs, derivatives thereof, and related compounds, which are useful as inhibitors of Axl kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions for treating disorders associated with dysfunction of the Axl kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: March 31, 2012
    Date of Patent: December 2, 2014
    Assignee: University of Utah Research Foundation
    Inventors: David J. Bearss, Hariprasad Vankayalapati, Alexis Mollard, Steven L. Warner, Sunil Sharma
  • Publication number: 20140350010
    Abstract: The invention relates to compounds of formula (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.
    Type: Application
    Filed: November 28, 2012
    Publication date: November 27, 2014
    Applicant: NOVARTIS AG
    Inventors: Pascal Furet, Vito Guagnano, Philipp Holzer, Robert Mah, Keiichi Masuya, Achim Schlapbach, Stefan Stutz, Andrea Vaupel
  • Publication number: 20140343006
    Abstract: This invention concerns HIV replication inhibitors of formula the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing -a1=a2-a3=a4- and -b1=b2-b3=b4- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; substituted C1-6alkyl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyloxy; substituted C1-6alkyloxyC1-6alkylcarbonyl; R2 is hydroxy, halo, optionally substituted C1-6alkyl, C3-7cycloalkyl, optionally substituted C2-6alkenyl, optionally substituted C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(?O)pR6, —NH—S(?O)pR6, —C(?O)R6, —NHC(?O)H, —C(?O)NHNH2, —NHC(?O)R6, —C(?NH)R6 or a 5-membered heterocycle; X1 is —NR5—, —NH—NH—, —N?N—, —O—, —C(?O)—, C1-4alkanediyl,
    Type: Application
    Filed: August 5, 2014
    Publication date: November 20, 2014
    Inventors: Jerome Emile Georges Guillemont, Patrice Palandijian, Marc Rene DeJonge, Lucien Maria Henricus Koymans, Hendrik Maarten Vinkers, Frederik Frans Desire Daeyaert, Jan Heeres, Koen Jeanne Alfons Van Aken, Paulus Joannes Lewi, Frank Xavier Jozef Herwig Arts
  • Publication number: 20140343015
    Abstract: A morphinan derivative represented by the following general formula (I) (in the formula, R1 represents hydrogen, C1-6 alkyl, cycloalkylalkyl (the cycloalkyl moiety has 3 to 6 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms), aralkyl (the aryl moiety has 6 to 10 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms) and the like, R2 represents hydrogen, C1-6 alkyl, C3-6 cycloalkyl, C6-10 aryl, aralkyl (the aryl moiety has 6 to 10 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms) and the like, R3, R4 and R5 represent hydrogen, hydroxy, carbamoyl, C1-6 alkoxy, C6-10 aryloxy and the like, R6a, R6b, R7, R8, R9, and R10 represent hydrogen and the like, X represents O or CH2, and Y represents C?O, SO2, an atomic bond and the like), or an acid addition salt thereof is used as an analgesic.
    Type: Application
    Filed: September 7, 2012
    Publication date: November 20, 2014
    Applicants: NIPPON CHEMIPHAR CO., LTD., THE KITASATO INSTITUTE
    Inventors: Hiroshi Nagase, Hideaki Fujii, Eriko Nakata, Yoshikazu Watanabe, Toshihiro Takahashi
  • Publication number: 20140336208
    Abstract: This invention relates to compounds of the formula wherein R1 to R9 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the therapeutic and/or prophylactic treatment of diseases such as diabetes, particularly type 2 diabetes, and other metabolic disorders.
    Type: Application
    Filed: July 9, 2014
    Publication date: November 13, 2014
    Inventors: David Banner, Emanuele Gabellieri, Wolfgang Guba, Hans Hilpert, Benoit Hornsperger, Roland Humm, Harald Mauser, Alexander V. Mayweg, Robert Narquizian, Emmanuel Pinard, Mark Rogers-Evans, Thomas Woltering, Wolfgang Wostl
  • Publication number: 20140329799
    Abstract: This invention relates to aminopyrimidinone compounds of Formula (I) that are inhibitors of Interleukin receptor-associated kinases, in particular IRAK-4, and are useful in the treatment or prevention of inflammatory diseases, including rheumatoid arthritis and inflammatory bowel disease.
    Type: Application
    Filed: October 26, 2012
    Publication date: November 6, 2014
    Inventors: W. Michael Seganish, Stephanie Nicole Brumfield, Jongwon Lim, Julius J. Matasi, William T. Mcelroy, Deen B. Tulshian, Brian J. Lavey, Michael D. Altman, Criag R. Gibeau, John William Lampe, Joey Methot, Liang Zhu
  • Patent number: 8871314
    Abstract: Provided is a polymer film containing at least one of a compound represented by formula (1) of hydrates, solvates, or salts thereof. Y is a methine group or nitrogen atom. Qa, Qb, and Qc are a single bond or a divalent linking group. Ra, Rb, and Rc, are hydrogen atom, alkyl group, alkenyl group, alkynyl group, aryl group, cyano group, halogen group, or heterocyclic group. X2 is a single bond or a divalent linking group. X1 is a single bond or a predetermined divalent linking group. R1 and R2 are a hydrogen atom, alkyl group, alkenyl group, alkynyl group, aryl group, or heterocyclic group.
    Type: Grant
    Filed: May 31, 2013
    Date of Patent: October 28, 2014
    Assignee: FUJIFILM Corporation
    Inventors: Aiko Yamamoto, Satoshi Tanaka, Teruki Niori, Masato Nagura, Masaki Noro, Aiko Yoshida, Nobutaka Fukagawa, Yasukazu Kuwayama
  • Patent number: 8859529
    Abstract: This invention relates to compounds of the Formula (I) as described herein, or a pharmaceutically acceptable salt, solvate or ester thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.
    Type: Grant
    Filed: September 22, 2009
    Date of Patent: October 14, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Bandarpalle B. Shankar, Seong Heon Kim, Wensheng Yu, Ling Tong, Michael K. C. Wong, Brian J. Lavey, Joseph A. Kozlowski, Lei Chen, Razia K. Rizvi, Aneta Maria Kosinski, De-Yi Yang, Guowei Zhou, Kristen E. Rosner, Luke Fire, Judson E. Richard, Dansu Li
  • Patent number: 8853228
    Abstract: The compositions and methods described herein disclose the design, synthesis and testing of compounds that act as inhibitors of DHFR. The basic scaffold of these inhibitors includes a 2,4-diaminopyrimidine ring with a propargyl linker to another substituted aryl, bicyclo or heteroaryl ring. These DHFR inhibitors are potent and selective for many different pathogenic organisms, including the DHFR enzyme from bacteria such as Bacillus anthracis and methicillin-resistant Staphylococcus aureus, fungi such as Candida glabrata, Candida albicans and Cryptococcus neoformans and protozoa such as Cryptosporidium hominis and Toxoplasma gondii. These compounds and other similar compounds are also potent against the mammalian enzyme and may be useful as anti-cancer therapeutics.
    Type: Grant
    Filed: November 7, 2011
    Date of Patent: October 7, 2014
    Assignee: University of Connecticut
    Inventors: Amy C. Anderson, Dennis L. Wright, Kathleen Mary Frey, Janet Leigh Paulsen, Eric William Scocchera, Kishore Viswanathan
  • Publication number: 20140296208
    Abstract: There are provided compounds of formula I, wherein R1A to R1E, R2 to R5, L and X1 to X3 have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
    Type: Application
    Filed: April 1, 2014
    Publication date: October 2, 2014
    Applicants: Topivert Pharma Limited, Respivert Limited
    Inventors: Thomas Matthew BAKER, Matthew Colin Thor FYFE, Gareth William HARBOTTLE, Vedran HASIMBEGOVIC, Premji MEGHANI, Aaron RIGBY, Colin SAMBROOK-SMITH, Stephen Malcolm THOM
  • Publication number: 20140296236
    Abstract: The invention relates to new quinoline derivative compounds of formula (I), to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 2, 2014
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventors: Valerio Berdini, Patrick Rene Angibaud, Steven John Woodhead, Gordon Saxty
  • Publication number: 20140296271
    Abstract: There is provided a compound of formula I, which compound has antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases, e.g., Src and Lck) and has use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
    Type: Application
    Filed: April 1, 2014
    Publication date: October 2, 2014
    Applicants: Topivert Pharma Limited, Respivert Limited
    Inventor: Matthew Colin Thor FYFE
  • Publication number: 20140288063
    Abstract: The present invention pertains to the field of medical technology, and particularly relates to a heterocyclic substituted pyrimidine compound represented by General Formula (I) and its pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4 and R5 are as defined in the description, the present invention also relates to a preparation method of the compound, a pharmaceutical composition containing the compound, and a use of the compound and the pharmaceutical composition in preparation of a medicine for enhancing a cGMP signal transduction function or a medicine for treating or preventing sexual dysfunction and diseases with lower urinary tract symptoms.
    Type: Application
    Filed: July 19, 2012
    Publication date: September 25, 2014
    Applicant: Xuanzhu Pharma Co., Ltd.
    Inventors: Yongqian Wu, Aichen Wang
  • Publication number: 20140275085
    Abstract: Described are compounds of Formula I which find utility in the treatment of cancer, autoimmune diseases and metabolic bone disorders through inhibition of c-FMS (CSF-1R), c-KIT, and/or PDGFR kinases. These compounds also find utility in the treatment of other mammalian diseases mediated by c-FMS, c-KIT, or PDGFR kinases.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: Deciphera Pharmaceuticals, LLC
    Inventors: Michael D. Kaufman, Daniel L. Flynn, YuMi Ahn, Lakshminarayana Vogeti, Timothy Malcolm Caldwell
  • Publication number: 20140249169
    Abstract: There is provided a compound of formula (I) which is an inhibitor of the family of p38 mitogen-activated protein kinase enzymes, and to its use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as asthma and COPD.
    Type: Application
    Filed: October 3, 2012
    Publication date: September 4, 2014
    Inventors: Kazuhiro Ito, Catherine Elisabeth Charron, John King-Underwood, Stuart Thomas Onions, Alistair Ian Longshaw, Rudy Broeckx, Walter Filliers, Alex Copmans
  • Patent number: 8822446
    Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1a, R1b, R1c, X, and Y are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as Cdc7 and methods of treating diseases such as cancer.
    Type: Grant
    Filed: April 14, 2011
    Date of Patent: September 2, 2014
    Assignee: AbbVie Inc.
    Inventors: Thomas D. Penning, Keith W. Woods, Chunqiu Lai, Yunsong Tong, Alan S. Florjancic
  • Patent number: 8815883
    Abstract: Compounds having the structures below that are TPH1 inhibitors are provided: The compounds are useful of, e.g., to increase bone mass. In preferred embodiments, the patient is known to have, or to be at risk for, a low bone mass disease such as osteoporosis.
    Type: Grant
    Filed: November 2, 2010
    Date of Patent: August 26, 2014
    Assignee: The Trustees of Columbia Unviersity in the City of New York
    Inventors: Donald Landry, Shi-Xian Deng
  • Patent number: 8815881
    Abstract: This invention relates to compounds of the formula wherein R1 to R9 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the therapeutic and/or prophylactic treatment of diseases such as diabetes, particularly type 2 diabetes, and other metabolic disorders.
    Type: Grant
    Filed: August 3, 2011
    Date of Patent: August 26, 2014
    Assignees: Hoffmann-La Roche Inc., Siena Biotech S.p.A.
    Inventors: David Banner, Emanuele Gabellieri, Wolfgang Guba, Hans Hilpert, Benoit Hornsperger, Roland Humm, Harald Mauser, Alexander V. Mayweg, Robert Narquizian, Emmanuel Pinard, Mark Rogers-Evans, Thomas Woltering, Wolfgang Wostl
  • Publication number: 20140221408
    Abstract: Pyrimidine compounds and their use in controlling pests such as insects and other invertebrates are provided. Further embodiments, forms, objects, features, advantages, aspects and benefits shall become apparent from the description.
    Type: Application
    Filed: April 3, 2014
    Publication date: August 7, 2014
    Applicant: Dow AgroSciences, LLC
    Inventors: Tony K. Trullinger, Timothy C. Johnson, Ricky Jim Hunter
  • Patent number: 8796296
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R3 and R4 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.
    Type: Grant
    Filed: November 28, 2012
    Date of Patent: August 5, 2014
    Assignee: Genentech, Inc.
    Inventors: Charles Baker-Glenn, Mark Chambers, Bryan K. Chan, Anthony Estrada, Zachary Kevin Sweeney
  • Publication number: 20140213574
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Application
    Filed: April 16, 2014
    Publication date: July 31, 2014
    Applicant: Celgene Avilomics Research, Inc.
    Inventors: Juswinder Singh, Russell Petter, Richland Wayne Tester, Arthur F. Kluge, Hormoz Mazdiyasni, William Frederick Westlin, III, Deqiang Niu, Lixin Qiao
  • Publication number: 20140213787
    Abstract: The present invention relates to a method of making 2,4-differentiated 5-trifluoromethylpyrimidines, which are useful as intermediates in the manufacture of active pharmaceutical substances.
    Type: Application
    Filed: April 3, 2014
    Publication date: July 31, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Guenter LINZ, Gerd KRAEMER
  • Publication number: 20140213598
    Abstract: Disclosed is a substituted cyanoaniline compound or a salt thereof, wherein the compound has a structure represented by General Formula I. The compound of General Formula I has broad-spectrum fungicidal activity in the field of agriculture and effectively prevents against a variety of pathogens such as cucumber downy mildew, wheat powdery mildew, maize rust disease, rice blast and cucumber gray mold. In particular, even at a low dose, the compound effectively prevents and treats rice blast, cucumber gray mold, maize rust disease and cucumber downy mildew. Moreover, the raw materials for preparing the compounds are widely available and the synthesis method therefor is simple and convenient.
    Type: Application
    Filed: June 15, 2012
    Publication date: July 31, 2014
    Applicants: SHENYANG RESEARCH INSTITUTE OF CHEMICAL INDUSTRY CO., LTD., SINOCHEM CORPORATION
    Inventors: Changling Liu, Guang Huang, Jie Lan, Shulin Hao, Zhinian Li, Huichao Li, Aiying Guan, Airu Jiang, Ying Xu
  • Patent number: 8791130
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n. X, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.
    Type: Grant
    Filed: November 28, 2012
    Date of Patent: July 29, 2014
    Assignee: Genentech, Inc.
    Inventors: Charles Baker-Glenn, Mark Chambers, Bryan K. Chan, Anthony Estrada, Zachary Kevin Sweeney
  • Patent number: 8785464
    Abstract: The present invention includes compounds of general formula (1) wherein A, X, R1 and R2 are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.
    Type: Grant
    Filed: October 9, 2013
    Date of Patent: July 22, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Heinz Stadtmueller, Bodo Betzemeier, Ioannis Sapountzis
  • Publication number: 20140194405
    Abstract: The disclosed compounds are useful in the treatment of mammalian cancers and especially human cancers. Compounds, pharmaceutical compositions, and methods of Formula I are disclosed: or a pharmaceutically acceptable salt, hydrate, solvate, enantiomer, stereoisomer, or tautomer thereof.
    Type: Application
    Filed: December 20, 2013
    Publication date: July 10, 2014
    Applicant: Deciphera Pharmaceuticals, LLC
    Inventors: Daniel L. Flynn, Michael D. Kaufman
  • Patent number: 8772302
    Abstract: The present invention relates to novel GPR 119 agonists of the general Formula (I), their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, stereoisomers, and polymorphs. The invention also relates to processes for the preparation of the compounds of the invention, pharmaceutical compositions containing the compounds and to methods for treating one or both of diabetes and obesity using the compounds of the invention. The present invention is directed to G-protein coupled receptor (GPCR) agonists that are useful for the treatment of obesity, diabetes and related metabolic disorders.
    Type: Grant
    Filed: June 17, 2010
    Date of Patent: July 8, 2014
    Assignee: Cadila Healthcare Limited
    Inventors: Harikishore Pingali, Pandurang Zaware, Mukul Jain