Three Ring Nitrogens In The Bicyclo Ring System Patents (Class 544/279)
  • Patent number: 10160759
    Abstract: Provided are a hydroxyethyl sulfonate of a cyclin-dependent protein kinase inhibitor, a crystalline form thereof and a preparation method therefor. Specifically, 6-acetyl-8-cyclopentyl-5-methyl-2-((5-(piperidin-4-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one hydroxyethyl sulfonate (compound of formula (I)), a crystal form I thereof and a preparation method therefor are provided. Crystal form I of the compound of formula (I) has good chemical and crystalline stability, low toxicity, and low residual crystallization solvent. The compound of formula (I) and crystal form I thereof can be used in improved clinical therapy.
    Type: Grant
    Filed: April 13, 2018
    Date of Patent: December 25, 2018
    Assignee: Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Guaili Wu, Xiaohui Gao, Junlei Jia
  • Patent number: 10065966
    Abstract: The present invention provides compounds of formula I-h: useful as inhibitors of protein kinases, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Grant
    Filed: May 25, 2017
    Date of Patent: September 4, 2018
    Assignees: Celgene CAR LLC, Sanofi
    Inventors: Laura Akullian D'Agostino, Robert Tjin Tham Sjin, Deqiang Niu, Joseph John McDonald, Zhendong Zhu, Haibo Liu, Hormoz Mazdiyasni, Russell C. Petter, Juswinder Singh, Matthieu Barrague, Alexandre Gross, Mark Munson, Darren Harvey, Andrew Scholte, Sachin Maniar
  • Patent number: 10030018
    Abstract: Provided are a hydroxyethyl sulfonate of a cyclin-dependent protein kinase inhibitor, a crystalline form thereof and a preparation method therefor. Specifically, 6-acetyl-8-cyclopentyl-5-methyl-2-((5-(piperidin-4-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one hydroxyethyl sulfonate (compound of formula (I)), a crystal form I thereof and a preparation method therefor are provided. Crystal form I of the compound of formula (I) has good chemical and crystalline stability, low toxicity, and low residual crystallization solvent. Therefore, the crystal form I can be used in improved clinical therapy.
    Type: Grant
    Filed: January 12, 2016
    Date of Patent: July 24, 2018
    Assignee: Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Guaili Wu, Xiaohui Gao, Junlei Jia
  • Patent number: 9850244
    Abstract: The invention discloses a method for preparing Palbociclib (I). The preparation method comprises the steps of: causing a ring-closing reaction of 2-acetyl-2-butenoic acid methyl ester and malononitrile to occur in an alkaline condition to generate 1,4,5,6-tetrahydro-2-methoxyl-4-methyl-5-acetyl-6-oxy-3-pyridine carbonitrile (II); causing a substitution reaction of the intermediate(II) and halogenated cyclopentane(III) to occur under the effect of acid binding agent to generate N-cyclopentyl-1,4,5,6-tetrahydro-2-methoxyl-4-methyl-5-acetyl-6-oxy-3-pyridinecarbonitrile (IV); causing a condensation reaction of the intermediate(IV) and N-[5-(1-piperazinyl)-2-pyridinyl]guanidine (V) to occur to generate 6-acetyl-8-cyclopentyl-5,8-dihydro-5-methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]-pyrido[2,3-d]pyrimidin-7(6H)-one (VI); and causing a dehydrogenation reaction of the intermediate(VI) and sodium selenate to occur to prepare Palbociclib(I).
    Type: Grant
    Filed: May 15, 2017
    Date of Patent: December 26, 2017
    Assignee: SUZHOU MIRACPHARMA TECHNOLOGY CO., LTD.
    Inventor: Xuenong Xu
  • Patent number: 9643965
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrido[3,4-d]pyrimidin-4-one derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
    Type: Grant
    Filed: September 16, 2015
    Date of Patent: May 9, 2017
    Assignee: Celgene Quantical Research, Inc.
    Inventors: Amogh Boloor, Toufike Kanouni, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennan Wallace
  • Patent number: 9365571
    Abstract: This invention relates to piperidino-pyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.
    Type: Grant
    Filed: August 4, 2015
    Date of Patent: June 14, 2016
    Assignee: Janssen Sciences Ireland UC
    Inventors: David Craig McGowan, Pierre Jean-Marie Bernard Raboisson, Tim Hugo Maria Jonckers, Mourad Daoubi Khamlichi
  • Patent number: 9326984
    Abstract: Alkyl-piperazine-phenyl 4 (3H)-quinazolinones compounds of general formula (I) below are provided that are pharmacologically active and able to act on the 5-HT1A and 5-HT2A serotonin receptors in a manner that promotes the control, relief or cure of disorders associated with these receptors, and pharmaceutical compositions containing the compounds for the treatment of disorders associated with these receptors. These compounds and their pharmaceutical compositions are useful in the treatment of conditions such as depression, anxiety, phobias, addictions, aggressiveness, impulsiveness, panic, psychotic, eating and sleep disorders, obsessive-compulsive disorder and female sexual dysfunctions, including loss of sexual desire, inhibition of sexual desire and absence of sexual desire, among other disorders associated with these receptors.
    Type: Grant
    Filed: September 23, 2015
    Date of Patent: May 3, 2016
    Assignees: ACHE LABORATORIOS FARMACEUTICOS S.A., ACHE INTERNATIONAL (BVI) LTD.
    Inventors: Valter Freire Torres Russo, Elisa Mannochio De Souza Russo
  • Patent number: 9321725
    Abstract: The present invention relates to a process of providing the 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid in substantially free form (Compound 1).
    Type: Grant
    Filed: October 23, 2013
    Date of Patent: April 26, 2016
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Mark Thomas Miller, Jason McCartney, Sara Sabina Hadida-Ruah, Jinglan Zhou
  • Patent number: 9321766
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
    Type: Grant
    Filed: October 6, 2014
    Date of Patent: April 26, 2016
    Assignee: Allergan, Inc.
    Inventors: Julie Wurster, Richard Yee, Clarence Eugene Hull, III, Thomas C. Malone
  • Patent number: 9227955
    Abstract: Disclosed are an anti-angiogenic compound, represented by Chemical Formula I, or a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutically acceptable composition including the same. Because the compound of Chemical Formula I potently suppresses the angiogenesis, the compound of Chemical Formula I is applicable to the prevention and treatment of diseases caused by aberrant activity of vascular endothelial growth factor, and available as an anti-angiogenic agent.
    Type: Grant
    Filed: July 27, 2012
    Date of Patent: January 5, 2016
    Assignee: Boryung Pharmaceutical Co., Ltd.
    Inventors: Ji Han Kim, Je Hak Kim, Joon Kwang Lee, Hahn-Sun Jung, Nam Seok Han, Yong Park, Seung-Hoon Kang, Hee Jin Jeong, Kyung-Tae Lee, Hye Eun Choi, Yong Ha Chi, Joo Han Lee, Soo Heui Paik
  • Patent number: 9181201
    Abstract: The present invention relates to a method for treating comorbid anxiety disorders and depression disorders, as well as for preventing depression disorders in individuals affected by anxiety disorders, by administering a therapeutically effective amount of the compound of general formula (I): wherein R1 is —OCH3 or —CN or suitable pharmaceutical salts, hydrates or anhydrates thereof.
    Type: Grant
    Filed: April 14, 2014
    Date of Patent: November 10, 2015
    Assignees: ACHE LABORATORIOS FARMACEUTICOS S.A., ACHE INTERNATIONAL (BVI) LTD.
    Inventors: Valter Freire Torres Russo, Elisa Mannochio De Souza Russo
  • Patent number: 9181239
    Abstract: Compounds of formula (I), and pharmaceutical acceptable salts thereof, which inhibit the activity of kinases such as Wee-1 kinase are described. Also described are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
    Type: Grant
    Filed: October 18, 2012
    Date of Patent: November 10, 2015
    Assignee: AbbVie Inc.
    Inventors: Anthony Mastracchio, Chunqiu Lai, Thomas D. Penning
  • Patent number: 9108968
    Abstract: Methods for producing 1,5,7-triazabicyclo[4.4.0]dec-5-ene using a disubstituted carbodiimide, dipropylene triamine and optionally an ethereal solvent and/or an alcohol are disclosed. Use of 1,5,7-triazabicyclo[4.4.0]dec-5-ene produced by this method in an electrodepositable coating composition, and electrophoretic deposition of such coating onto a substrate to form a coated substrate, are also disclosed.
    Type: Grant
    Filed: April 25, 2012
    Date of Patent: August 18, 2015
    Assignee: PPG Industries Ohio, Inc.
    Inventors: Christopher Dacko, Richard F. Karabin, Craig Wilson, Steven R. Zawacky
  • Patent number: 9096596
    Abstract: The present invention is directed to a compound of Formula (I) The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: August 4, 2015
    Assignee: JANSSEN PHARMACEUTICA NV
    Inventors: Manuel Jesus Alcazar Vaca, Jose Ignacio Andres Gil, Michael A. Letavic, Dale A. Rudolph, Brock T. Shireman, Brice M. Stenne, Jeannie M. Ziff
  • Publication number: 20150148356
    Abstract: The present invention relates to the cosmetic use, as agent for preventing and/or treating an aesthetic defect in the skin and/or its appendages that is associated with an imbalance in the differentiation and/or proliferation of the cells of an epidermis, of an effective amount of at least one compound represented by one of the general formulae, (Ia) or (Ib)
    Type: Application
    Filed: June 5, 2013
    Publication date: May 28, 2015
    Inventors: Xavier Marat, Benoit Muller, Agnès Thomas-Collignon, Dominique Bernard
  • Publication number: 20150133424
    Abstract: The present disclosure is related to heteroaryl compounds as MEK inhibitors. These compounds include heteroaryl compounds of formula I, their pharmaceutically acceptable salts, combinations with suitable medicament and pharmaceutical compositions thereof. The present disclosure also includes processes of preparation of the compounds and their use in methods of treatment.
    Type: Application
    Filed: March 11, 2013
    Publication date: May 14, 2015
    Inventors: Bhavesh Dave, Rakesh Kumar Banerjee, Samiron Phukan, Abhijit Datta Khoje, Rajkumar Hangarge, Jitendra Sambhaji Jadhav, Venkata P. Palle, Rajender Kumar Kamboj
  • Patent number: 9029392
    Abstract: Disclosed are a series of quinoline and quinoxaline derivatives comprising a fluorinated ethyl side-chain, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
    Type: Grant
    Filed: September 2, 2011
    Date of Patent: May 12, 2015
    Assignee: UCB Pharma S.A.
    Inventors: Andrew Harry Parton, Mezher Hussein Ali, Daniel Christopher Brookings, Julien Alistair Brown, Daniel James Ford, Richard Jeremy Franklin, Judi Charlotte Neuss, Joanna Rachel Quincey, Jackalyn Hinkins
  • Publication number: 20150126534
    Abstract: Covalent conjugation of an alpha amino acid ester to a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by one or more intracellular carboxylesterase enzymes to the corresponding acid, leads to accumulation of the carboxylic acid hydrolysis product in the cell and enables improved or more prolonged enzyme or receptor modulation relative to the unconjugated modulator.
    Type: Application
    Filed: October 7, 2014
    Publication date: May 7, 2015
    Inventors: Alan Hornsby Davidson, Alan Hastings Drummond, Lindsey Ann Needham
  • Publication number: 20150126500
    Abstract: Provided are piperazinyl pyrimidine derivatives of formula I having CCR4 antagonism, and the preparation method, pharmaceutical composition and use thereof in the preparation of a medicament. The medicament is useful for the treatment and prevention of CCR4-related diseases.
    Type: Application
    Filed: January 15, 2013
    Publication date: May 7, 2015
    Inventors: Song Li, Ying Wang, Junhai Xiao, Dalong Ma, Hongwei Gong, Hui Qi, Lili Wang, Xiaomei Ling, Zhibing Zheng, Yang Zhang, Wu Zhong, Meina Li, Yunde Xie, Enquan Xu, Xingzhou Li, Jing Ma, Guoming Zhao, Xinbo Zhou, Xiaokui Wang, Hongying Liu
  • Publication number: 20150126519
    Abstract: Disclosed herein are compounds and methods for inhibiting bacterial DNA repair enzymes, including AddAB and RecBCD helicase-nucleases. Pharmaceutical compositions and methods for treating a subject with an antibacterial agent are also disclosed herein.
    Type: Application
    Filed: March 20, 2013
    Publication date: May 7, 2015
    Inventors: Gerald R. Smith, Susan K. Amundsen, Ahmet C. Karabulut, Thomas D. Bannister, Reji Narayanan Nair
  • Publication number: 20150126506
    Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
    Type: Application
    Filed: January 8, 2015
    Publication date: May 7, 2015
    Inventors: Alfredo C. CASTRO, Catherine A. EVANS, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Tao LIU, Daniel A. SNYDER, Martin R. TREMBLAY, Pingda REN, Yi LIU, Liansheng LI, Katrina CHAN
  • Publication number: 20150119405
    Abstract: Described herein are inhibitors of FGFR-4, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.
    Type: Application
    Filed: October 23, 2014
    Publication date: April 30, 2015
    Applicant: BLUEPRINT MEDICINES CORPORATION
    Inventors: Neil Bifulco, Jr., Lucian V. DiPietro, Brian L. Hodous, Chandrasekhar V. Miduturu
  • Publication number: 20150119392
    Abstract: This invention provides compounds of Formula I: (Formula I should be inserted here) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising a compound of Formula I; and use of a compound of Formula I for treating specified cancers.
    Type: Application
    Filed: March 5, 2013
    Publication date: April 30, 2015
    Inventors: Daniel L. Flynn, Michael D. Kaufman, Lakshminarayana Vogeti, Scott Wise, Wei-Ping Lu, Bryan Smith, James R. Henry, Philip A. Hipskind, Sheng-Bin Peng
  • Publication number: 20150111747
    Abstract: 6-Pyridone-2-carbamoylazoles of the general formula (I) are described as herbicides. In this formula (I), W, X and Z represent radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. Q represents a 5-membered radical such as oxadiazyl.
    Type: Application
    Filed: April 30, 2013
    Publication date: April 23, 2015
    Inventors: Ralf Braun, Stefan Lehr, Arnim Koehn, Hansjoerg Dietrich, Elmar Gatzweiler, Christopher Hugh Rosinger, Dirk Schmutzler
  • Publication number: 20150105549
    Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, X is CH or N; Y is C(O) or S(O)2; provided that when Y is S(O)2, then X is CH; A is a radical selected from the group consisting of and B1, B2, B3, T, R1, R2R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and R13 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: December 17, 2014
    Publication date: April 16, 2015
    Inventors: KANU MAGANBHAI PATEL, Thomas Paul Selby, Brenton Todd Smith, Andrew Edmund Taggi, Patrick Ryan Kovacs
  • Patent number: 9006265
    Abstract: The use of substituted fused pyrimidinones and dihydropyrimidinones of the formula (I) or salts thereof where the radicals of the formula (I) are each as defined in the description, for enhancing stress tolerance in plants to abiotic stress, and for invigorating plant growth and/or for increasing plant yield.
    Type: Grant
    Filed: September 2, 2011
    Date of Patent: April 14, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Jens Frackenpohl, Hans-Joachim Zeiβ, Ines Heinemann, Lothar Willms, Thomas Müller, Marco Busch, Pascal Von Koskull-Döring, Isolde Häuser-Hahn, Christopher Hugh Rosinger, Jan Dittgen, Martin Jeffrey Hills, Monika H. Schmitt
  • Patent number: 9006255
    Abstract: Compounds of the formula I in which R, X, L2 and A1-A6 have the meanings indicated in Claim 1, are PI3K inhibitors and can be employed, inter alia, for the treatment of autoimmune diseases, inflammation, cardiovascular diseases, neurodegenerative diseases and tumors.
    Type: Grant
    Filed: September 22, 2011
    Date of Patent: April 14, 2015
    Assignee: Merck Patent GmbH
    Inventor: Markus Klein
  • Patent number: 8987267
    Abstract: Compounds according to Formula (I), as well salts thereof: wherein R1 and R2 are as defined herein, are useful as antiproliferative agents and kinase inhibitors. Synthetic methods for preparing the compounds of Formula (I) are also provided.
    Type: Grant
    Filed: July 21, 2011
    Date of Patent: March 24, 2015
    Assignee: Temple University—of the Commonwealth System of Higher Education
    Inventors: E. Premkumar Reddy, M. V. Ramana Reddy
  • Publication number: 20150072974
    Abstract: Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and neurological disorders, including, but not limited to, e.g., psychosis, schizophrenia, depression, movement disorders, and Parkinson's disease.
    Type: Application
    Filed: May 9, 2013
    Publication date: March 12, 2015
    Inventors: Phillip G. Jones, Robert Lew, Kerry L. Spear, Linghong Xie
  • Patent number: 8975250
    Abstract: The present invention relates to 5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine derivatives having Formula (I) as defined herein, their preparation and their therapeutic use.
    Type: Grant
    Filed: July 9, 2012
    Date of Patent: March 10, 2015
    Assignee: SANOFI
    Inventors: Philippe Beauverger, Guillaume Begis, Sandrine Biscarrat, Olivier Duclos, Gary McCort
  • Patent number: 8969590
    Abstract: Classes of compounds that exhibit effective inhibition of autotaxin enzymes are provided. Such classes include thioureas, diphenyldiazerenes, xanthenes, and isoindoles and exhibit reactivity with autotaxin to ultimately reduce the size of the reactive sites thereon to prevent conversion of lysophosphatidyl choline to lysophophatidic acid. Furthermore, such compounds can be incorporated within delivery forms for human ingestion. As such, these compounds accord an excellent manner of potentially reducing generation of certain cancers attributable to the presence of naturally occurring autotaxin within the human body. Methods of inactivating autotaxin to certain degrees therewith such compounds are encompassed within invention as well.
    Type: Grant
    Filed: September 18, 2012
    Date of Patent: March 3, 2015
    Inventors: Abby Louise Parrill-Baker, Daniel Lee Baker
  • Patent number: 8969363
    Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
    Type: Grant
    Filed: July 18, 2012
    Date of Patent: March 3, 2015
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Alfredo C. Castro, Catherine A. Evans, Somarajannair Janardanannair, Andre Lescarbeau, Tao Liu, Daniel A. Snyder, Martin R. Tremblay, Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan
  • Publication number: 20150057283
    Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.
    Type: Application
    Filed: March 28, 2014
    Publication date: February 26, 2015
    Applicant: CHOONGWAE PHARMA CORPORATION
    Inventors: Sung Hwan Moon, Jae Uk Chung, Sung Chan Lee, Masakatsu Eguchi, Michael Kahn, Kwang Won Jeong, Cu Nguyen
  • Patent number: 8962637
    Abstract: The present invention relates to substituted aromatic bicyclic compounds containing pyrimidine and pyridine rings of formula (I) having the structure as well as pharmaceutically acceptable salts thereof. The compounds of the present invention are useful as tyrosine kinase inhibitors, preferably SRC family kinases (SFKs) inhibitors, in particular as multi SFK/JAK. kinases inhibitors and even preferably as dual c-SRC/JAK kinases inhibitors, thereby inhibiting the STAT3 activation and therefore abnormal growth of particular cell types. Notably, the compounds of the present invention are useful for the treatment or inhibition of certain diseases that are the result of deregulation of STAT3.
    Type: Grant
    Filed: January 14, 2013
    Date of Patent: February 24, 2015
    Assignees: Debiopharm S.A., Aurigene Discovery Technologies Ltd.
    Inventors: Andrès Mc Allister, Maximilien Murone, Saumitra Sengupta, Shankar Jayaram Shetty
  • Publication number: 20150051395
    Abstract: Provided are sulfonamide derivatives of a specific chemical structure in which a sulfonamide group having, as a substituent, a phenyl group or a heterocyclic group having a hetero atom(s) as a constituent element(s) is present at its terminal, and pharmaceutically acceptable salts thereof. These compounds are novel compounds having excellent ?4 integrin-inhibitory action.
    Type: Application
    Filed: April 24, 2013
    Publication date: February 19, 2015
    Applicant: AJINOMOTO CO., LTD.
    Inventors: Hirokazu Ueno, Takashi Yamamoto, Ryuta Takashita, Ryohei Yokoyama, Toshihiko Sugiura, Shunsuke Kageyama, Ayatoshi Ando, Hiroyuki Eda, Agung Eviryanti, Tomoko Miyazawa, Aya Kirihara, Itsuya Tanabe, Tarou Nakamura, Misato Noguchi, Manami Shuto, Masayuki Sugiki, Mizuki Dohi
  • Patent number: 8957062
    Abstract: Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: April 5, 2012
    Date of Patent: February 17, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott Edmondson, Zhiqiang Guo, Harold B. Wood, Andrew W. Stamford, Michael W. Miller, Duane E. DeMong, Gregori J. Morriello, Rajan Anand, Vincent J. Colandrea, Megan Macala, Milana Maletic, Cheng Zhu, Yuping Zhu, Wanying Sun, Kake Zhao, Yong Huang, Joel M. Harris, Lehua Chang, Nam Fung Kar, Zhiyong Hu, Liping Wang, Bowei Wang, Ping Liu, Jason W. Szewczyk, William B. Geiss
  • Patent number: 8952018
    Abstract: A novel combination comprising the MEK inhibitor N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimethyl; -2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, with a B-Raf inhibitor, particularly N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of MEK and/or B-Raf is beneficial, eg. cancer.
    Type: Grant
    Filed: March 5, 2014
    Date of Patent: February 10, 2015
    Assignee: GlaxosmithKline LLC
    Inventors: Melissa Dumble, Rakesh Kumar, Sylvie Laquerre, Peter Lebowitz
  • Publication number: 20150031693
    Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of Fragile X syndrome.
    Type: Application
    Filed: November 2, 2012
    Publication date: January 29, 2015
    Applicant: AFRAXIS HOLDINGS, INC.
    Inventors: John C. Mckew, Wenwei Huang, David Campbell, Sergio G. Durön, Mark Behnke, Min Shen
  • Publication number: 20150031882
    Abstract: Methods of treating patients with cancer are provided, wherein the methods comprise administering to the patient an effective amount of a MEK inhibitor and an effective amount of a PI3K inhibitor. Compositions in which the MEK and PI3K inhibitors are combined also are described.
    Type: Application
    Filed: October 2, 2014
    Publication date: January 29, 2015
    Inventors: Karl HSU, Joanne LAGER, Janet OGDEN
  • Publication number: 20150031672
    Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
    Type: Application
    Filed: October 10, 2014
    Publication date: January 29, 2015
    Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson, Alfredo C. Castro, Catherine A. Evans, Daniel A. Snyder
  • Publication number: 20150031674
    Abstract: Compounds having the formula I wherein R1, R2, R3, R4, R5, Ra, Rb, Rc, Rd, Re, n, r, s and t are as defined herein and which compounds are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders.
    Type: Application
    Filed: July 25, 2014
    Publication date: January 29, 2015
    Applicant: GENENTECH, INC.
    Inventors: Joachim Rudolph, Lewis J. Gazzard, James J. Crawford, Chudi Ndubaku, Joy Drobnick, Wendy Lee
  • Patent number: 8940752
    Abstract: The present invention provides pyrimidinones that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
    Type: Grant
    Filed: June 28, 2010
    Date of Patent: January 27, 2015
    Assignee: Incyte Corporation
    Inventors: Yun-Long Li, Brian W. Metcalf
  • Publication number: 20150025058
    Abstract: Compounds of the formula I in which R1, R2 and R4 have the meanings indicated in Claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment of cancer, rheumatoid arthritis and/or systemic lupus
    Type: Application
    Filed: January 22, 2013
    Publication date: January 22, 2015
    Applicant: MERCK PATENT GMBH
    Inventors: Carl Deutsch, Daniel Kuhn, Tatjana Ross, Lars Burgdorf
  • Publication number: 20150025090
    Abstract: The present application relates to novel substituted azabicycles, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Application
    Filed: March 5, 2013
    Publication date: January 22, 2015
    Inventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Alexandros Vakalopoulos, Dieter Lang, Frank Wunder, Walter Hübsch, Michael Hahn
  • Publication number: 20150018546
    Abstract: A heterocyclic compound represented by the general formula (In the formula, R1, R2 and R3 may be the same or different, and each represents a hydrogen atom, a halogen atom, or this general formula (X1—Y1—R4) (in the formula: X1 represents this general formula (NR5) (in the formula, R5 represents a hydrogen atom, etc.) or the like; Y1 represents an optionally substituted C1-6 alkylene group or the like; and R4 represents an optionally substituted aryl group or the like), and Z represents a nitrogen atom or this general formula (CR6) (in the formula, R6 represents a hydrogen atom, a halogen atom, or an optionally substituted C1-12 alkyl group or the like)), or a salt thereof, exhibits excellent anti-HIV activity and is useful as an anti-HIV agent.
    Type: Application
    Filed: January 30, 2013
    Publication date: January 15, 2015
    Applicant: TOYAMA CHEMICAL CO., LTD.
    Inventors: Hyouei Kawai, Daigo Murata, Yuko Suzumura
  • Publication number: 20150018352
    Abstract: The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.
    Type: Application
    Filed: March 7, 2013
    Publication date: January 15, 2015
    Inventors: Thomas Dineen, Charles Kreiman, Matthew Weiss, Stephanie Geuns-Meyer
  • Publication number: 20150011761
    Abstract: Among other things, the present invention encompasses methods of synthesizing salicylaldehyde derivatives comprising the steps of: a) providing salicylaldehyde or a derivative thereof, b) forming an anhydro dimer of the provided salicylaldehyde compound, c) performing one or more chemical transformations on the anhydro dimer and d) hydrolyzing the anhydro dimer to provide a salicylaldehyde derivative different from that provided in step (a).
    Type: Application
    Filed: September 25, 2014
    Publication date: January 8, 2015
    Inventors: Jay J. Farmer, Gabriel E. Job
  • Patent number: 8912203
    Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders such as neuropsychiatric disorders.
    Type: Grant
    Filed: June 9, 2011
    Date of Patent: December 16, 2014
    Assignee: Afraxis Holdings, Inc.
    Inventors: David Campbell, Sergio G. Duron, Benedikt Vollrath, Warren Wade
  • Patent number: 8912205
    Abstract: A pharmaceutical formulation comprising the compound of formula
    Type: Grant
    Filed: July 16, 2013
    Date of Patent: December 16, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Malcolm Clive Carter, George Stuart Cockerill, Karen Elizabeth Lackey
  • Publication number: 20140364430
    Abstract: Provided herein are PAK inhibitors.
    Type: Application
    Filed: August 14, 2014
    Publication date: December 11, 2014
    Inventors: Jay LICHTER, David CAMPBELL, Benedikt VOLLRATH, Sergio G. DURÓN