Patents Issued in June 22, 2017
  • Publication number: 20170174647
    Abstract: A compound of formula (I) is provided wherein R represents a linear or branched C5 alkyl group, as well as the use of such compounds in a fragrant and/or flavoring composition, or as a masking agent for odors and/or flavors.
    Type: Application
    Filed: March 2, 2017
    Publication date: June 22, 2017
    Inventors: Jean MANE, Caroline PLESSIS, Jean-Jacques CHANOT
  • Publication number: 20170174648
    Abstract: This disclosure is related to methods for producing anhydroryanodol, ryanodol, or analogues thereof and novel compounds prepared thereby.
    Type: Application
    Filed: December 16, 2016
    Publication date: June 22, 2017
    Inventors: Sarah Reisman, Kangway V. Chuang, Chen Xu
  • Publication number: 20170174649
    Abstract: Esters of acetals of chemical structure: are provided which have excellent solubility power in sunscreens, excellent properties of emollience, spreadability and ease of preparing stable aqueous formulas, are completely non-toxic, have no characteristics that generate ocular or cutaneous irritation, and these properties enable their use as solubilizers and emollients in cosmetic formulations for body use, facial sunscreens, makeup removers and component for use in roll-on deodorants.
    Type: Application
    Filed: December 15, 2016
    Publication date: June 22, 2017
    Inventors: Setsuo SATO, Marcelo Eiji Borges Sato
  • Publication number: 20170174650
    Abstract: The present invention is directed to novel organoleptic compounds, a process of augmenting, enhancing or imparting taste to a material selected from the group consisting of a foodstuff, a chewing gum, a dental product, an oral hygiene product and a medicinal product comprising the step of incorporating an olfactory acceptable amount of such novel organoleptic compounds, and a process of improving, enhancing or modifying a fragrance composition through the addition of an olfactory acceptable amount of such novel organoleptic compounds.
    Type: Application
    Filed: April 6, 2015
    Publication date: June 22, 2017
    Inventors: David O. AGYEMANG, Anja VAN KIPPERSLUIS BRAIN, Tingwei CAI, Robert J. CANNON, Zhen CHEN, Nicole L. CURTO, Adam Jan JANCZUK, Paul D. JONES, Arkadiusz KAZIMIERSKI, Jing LI, David RODRIGUEZ
  • Publication number: 20170174651
    Abstract: A method of reducing cellular damage to a plant by treating the plant with a compound containing an NO-releasing moiety and an H2S-releasing moiety covalently bonded to an aspirin derived core or a NOSH compound is claimed. The compounds may also be used in a method of priming a plant against abiotic stress factors and a method of promoting plant growth.
    Type: Application
    Filed: February 11, 2015
    Publication date: June 22, 2017
    Inventors: Khosrow Kashfi, Vasileios Fotopoulos
  • Publication number: 20170174652
    Abstract: Described herein are inhibitors of FGFR-4, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.
    Type: Application
    Filed: July 28, 2016
    Publication date: June 22, 2017
    Inventors: Neil Bifulco, JR., Lucian V. DiPietro, Brian L. Hodous, Chandrasekhar V. Miduturu
  • Publication number: 20170174653
    Abstract: The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as TLR7/8 antagonists.
    Type: Application
    Filed: December 16, 2016
    Publication date: June 22, 2017
    Inventors: Brian A. SHERER, Nadia BRUGGER
  • Publication number: 20170174654
    Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    Type: Application
    Filed: February 28, 2017
    Publication date: June 22, 2017
    Inventors: Brian W. METCALF, Chihyuan Chuang
  • Publication number: 20170174655
    Abstract: Described herein are compounds, pharmaceutical compositions and methods for inhibiting the expression of a vitamin D receptor target gene, inhibiting interactions between the vitamin D receptor and at least one vitamin D receptor coactivator, for treating cancer in a subject, and for inhibiting angiogenesis in a subject.
    Type: Application
    Filed: August 16, 2016
    Publication date: June 22, 2017
    Inventors: Alexander E. Arnold, Preetpal Singh Sidhu, Premchendar Nandhikonda, Rakesh K. Singh
  • Publication number: 20170174656
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted 3-aminopyridine derivative compounds, substituted 3-aminopyridazine derivative compounds, and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition 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: Application
    Filed: March 1, 2017
    Publication date: June 22, 2017
    Inventors: Toufike Kanouni, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennan Wallace
  • Publication number: 20170174657
    Abstract: The present invention relates to the 1H-indazole-3-carboxamide compounds as glycogen synthase kinase 3 beta (GSK-3?) inhibitors and to their use in the treatment of GSK-3?-related disorders such as, for example, (i) insulin-resistance disorders; (ii) neurodegenerative diseases; (iii) mood disorders; (iv) schizophrenic disorders; (v) cancerous disorders; (vi) inflammation, (vii) substance abuse disorders; (viii) epilepsies; and (ix) neuropathic pain.
    Type: Application
    Filed: March 7, 2017
    Publication date: June 22, 2017
    Applicant: AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R. A.F. S.P.A.
    Inventors: Maria Alessandra ALISI, Nicola CAZZOLLA, Patrizia DRAGONE, Guido FURLOTTI, Caterina MAUGERI, Rosella OMBRATO, Francesca MANCINI
  • Publication number: 20170174658
    Abstract: The invention relates to inhibitors of mutant isocitrate dehydrogenase (mt-IDH) proteins with neomorphic activity useful in the treatment of cell-proliferation disorders and cancers, having the Formula: where A, U, W1, W2, W3, R1-R6, and R9 are described herein.
    Type: Application
    Filed: March 7, 2017
    Publication date: June 22, 2017
    Inventors: Jian LIN, Anna ERICSSON, Ann-Marie CAMPBELL, Gary R. GUSTAFSON, Zhongguo WANG, R. Bruce DIEBOLD, Susan ASHWELL, David LANCIA, JR., Justin Andrew CARAVELLA, Wei LU
  • Publication number: 20170174659
    Abstract: The present invention provides compounds of formula I: which are useful as modulators of GPR6, pharmaceutical compositions thereof, methods for treatment of conditions associated with GPR6, processes for making the compounds and intermediates thereof.
    Type: Application
    Filed: February 13, 2015
    Publication date: June 22, 2017
    Inventors: Mark E. Adams, Jason W. Brown, Stephen Hitchcock, Maria Hopkins, Shota Kikuchi, Betty Lam, Holger Monenschein, Holly Reichard, Huikai Sun
  • Publication number: 20170174660
    Abstract: Inducible HSP70 is overexpressed in a wide spectrum of human tumors and its expression correlates with metastasis and poor outcomes to radiation and chemotherapy in patients. Identification of small molecule inhibitors of HSP70 pose a new therapy to cancer treatment. HS72, a benzimidazole piperidinyl carboxamide has been identified as an allosteric inhibitor for HSP70 and has demonstrated good tumor growth inhibition in vivo.
    Type: Application
    Filed: March 25, 2015
    Publication date: June 22, 2017
    Inventors: Timothy A. J. HAYSTEAD, Khaldon BOODOOR, Philip F. HUGHES
  • Publication number: 20170174661
    Abstract: Disclosed herein is the compound (R)-1-(4-(6-(2-(4-(3,3-difluorocyclobutoxy)-6-methylpyridin-2-yl)acetamido)pyridazin-3-yl)-2-fluorobutyl)-N-methyl-1H-1,2,3-triazole-4-carboxamide, and salt forms and polymorphs thereof demonstrating improved exposure after oral dosing. Methods of inhibition GLS1 activity in a human or animal subject are also provided.
    Type: Application
    Filed: December 21, 2016
    Publication date: June 22, 2017
    Inventors: Philip JONES, Michael J. SOTH, Jason B. BURKE, Kang LE, Gang LIU
  • Publication number: 20170174662
    Abstract: Disclosed are a novel crystalline form and an amorphous form of Olaparib, and the process for their preparation.
    Type: Application
    Filed: December 19, 2016
    Publication date: June 22, 2017
    Inventors: Barbara Novo, Jacopo Bonanomi, Stella Defiore, Francesco Calogero
  • Publication number: 20170174663
    Abstract: The present invention encompasses compounds of the formula (I) wherein the groups R1, Cy and Y are defined herein, which are suitable for the treatment of diseases related to BTK, and processes for making these compounds, pharmaceutical preparations containing these compounds, and their methods of use.
    Type: Application
    Filed: December 15, 2016
    Publication date: June 22, 2017
    Inventors: Todd BOSANAC, Joerg BENTZIEN, Michael Jason BURKE, Ryan Michael FRYER, Eric Thomas LARSON, Wang MAO, Bryan Patrick MCKIBBEN, Yue SHEN, Fariba SOLEYMANZADEH, Matt Aaron TSCHANTZ
  • Publication number: 20170174664
    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: Application
    Filed: March 6, 2017
    Publication date: June 22, 2017
    Inventors: Xialing Guo, Zhen Zhu, Thomas C. Malone, Julie Wurster
  • Publication number: 20170174665
    Abstract: The invention discloses a new series of inhibitors of soluble epoxide hydrolase (sEH) with improved physical properties that enhance their druglikeness to treat sEH associated diseases such as chronic diabetic neuropathic pain.
    Type: Application
    Filed: March 27, 2015
    Publication date: June 22, 2017
    Inventors: Bruce D. Hammock, Kin Sing Stephen Lee, Ahmet Bora Inceoglu
  • Publication number: 20170174666
    Abstract: The invention disclosed herein is directed to compounds of Formula I [Formula should be entered here] and pharmaceutically acceptable salts thereof, which are useful in the treatment of prostate, breast, colon, pancreatic, human chronic lymphocytic leukemia, acute or chronic myeloid leukemia, melanoma, and other cancers. The invention also includes pharmaceutical compositions comprising a therapeutically effective amount of compound of Formula I, or a pharmaceutically acceptable salt thereof. The invention disclosed herein is also directed to methods of treating prostate, breast, ovarian, liver, kidney, colon, pancreatic, human chronic lymphocytic leukemia, acute or chronic myeloid leukemia, melanoma and other cancers.
    Type: Application
    Filed: February 9, 2015
    Publication date: June 22, 2017
    Inventors: Nicholas Simon Stock, Austin Chih-Yu Chen, Yalda Mostofi Bravo, Jason Duarte Jacintho, Yen Truong
  • Publication number: 20170174667
    Abstract: Compounds of Formula (I), including their salts, as well as compositions and methods of using the compounds are set forth.
    Type: Application
    Filed: March 20, 2015
    Publication date: June 22, 2017
    Inventors: Tao Wang, Zhiwei Yin, John F. Kadow
  • Publication number: 20170174668
    Abstract: This invention relates to novel sulfoximine substituted quinazoline derivatives of formula (I), wherein Ar, R1 and R2 are as defined in the description and claims, and their use as MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) kinase inhibitors, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment or amelioration of MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) mediated disorders.
    Type: Application
    Filed: November 28, 2014
    Publication date: June 22, 2017
    Inventors: Joerg Kley, Andreas Blum, Dirk Gottschling, Joerg P. Hehn, Dieter Wiedenmayer
  • Publication number: 20170174669
    Abstract: The present invention includes novel derivatives, analogs, and intermediates of the natural products radicicol, pochonins, pochoximes, and their syntheses. The present invention also provides a pharmaceutical composition comprising the present compound and the use of the compound as inhibitors of kinases and of the enzyme family known as heat shock protein 90 (HSP90).
    Type: Application
    Filed: August 29, 2016
    Publication date: June 22, 2017
    Inventors: Nicolas WINSSINGER, Sofia BARLUENGA
  • Publication number: 20170174670
    Abstract: Compounds, and compositions, methods, and uses thereof, are described herein for treating neurodegenerative diseases and disorders. In particular, vasopressin receptor modulators, and compositions, methods and uses thereof, are described herein for treating neuropsychiatric aspects of neurodegenerative diseases such as Huntington's Disease, Parkinson's Disease, and Alzheimer's Disease.
    Type: Application
    Filed: March 27, 2015
    Publication date: June 22, 2017
    Applicant: Azevan Pharmaceuticals, Inc.
    Inventor: Michael J. BROWNSTEIN
  • Publication number: 20170174671
    Abstract: Disclosed are compounds of Formula (I?), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
    Type: Application
    Filed: December 16, 2016
    Publication date: June 22, 2017
    Inventors: Liangxing Wu, Zhiyong Yu, Fenglei Zhang, Wenqing Yao
  • Publication number: 20170174672
    Abstract: The invention relates to (hetero)cyclic compounds as S1P modulators, pharmaceutical compositions comprising such compounds, and uses thereof in the treatment, alleviation or prevention of diseases or disorders mediated by an S1P receptor.
    Type: Application
    Filed: December 22, 2016
    Publication date: June 22, 2017
    Inventors: Wilhelm Amberg, Udo Lange, Herve Geneste, Michael Ochse, Ralf Biesinger, Frank Oellien
  • Publication number: 20170174673
    Abstract: In one aspect, the invention provides a compound according to formula I, as well as tautomers, pharmaceutically acceptable salts, and hydrates thereof. Pharmaceutical compositions, methods of inhibiting Janus kinases (JAKs), and methods for treating a condition or disorder mediated at least in part by JAK kinase activity are also described.
    Type: Application
    Filed: February 12, 2015
    Publication date: June 22, 2017
    Inventors: Qing XU, Yonghong SONG, Anjali PANDEY
  • Publication number: 20170174674
    Abstract: Disclosed are compounds of Formula A, or a salt thereof: wherein R1, R2, and E are defined herein, which compounds have properties for inhibiting Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating pain disorders, cough, and itch using the same.
    Type: Application
    Filed: December 14, 2016
    Publication date: June 22, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Thomas J. Greshock, James Mulhearn, Junying Zheng, Ronald M. Kim, Ting Zhang, Anthony J. Roecker, Walter Won, Philippe Nantermet, Rajan Anand, Gang Zhou, Deping Wang, Liangqin Guo
  • Publication number: 20170174675
    Abstract: The present invention relates to modulators of cystic fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating CFTR mediated diseases using such modulators.
    Type: Application
    Filed: April 22, 2016
    Publication date: June 22, 2017
    Inventors: Sara Hadida-Ruah, Fredrick Van Goor, Mark Miller, Jason McCartney, Jinglan Zhou, Vijayalaksmi Arumugam
  • Publication number: 20170174676
    Abstract: The present invention relates to chlorinated naphthalenetetracarboxylic acid derivatives, preparation thereof and use thereof as charge transport materials, exciton transport materials or emitter materials.
    Type: Application
    Filed: October 26, 2016
    Publication date: June 22, 2017
    Applicant: BASF SE
    Inventors: Martin KOENEMANN, Gabriele MATTERN, Frank WUERTHNER, Cornelia ROEGER, Ruediger SCHMIDT
  • Publication number: 20170174677
    Abstract: The present invention provides compounds of formula I: which are useful as modulators of GPR6, pharmaceutical compositions thereof, methods for treatment of conditions associated with GPR6, processes for making the compounds and intermediates thereof.
    Type: Application
    Filed: February 13, 2015
    Publication date: June 22, 2017
    Inventors: Stephen Hitchcock, Maria Hopkins, Shota Kikuchi, Holger Monenschein, Holly Reichard, Huikai Sun, Todd Macklin
  • Publication number: 20170174678
    Abstract: The present invention includes bicyclic compounds that are useful in preventing or treating viral infections, such as viral infections caused by a filovirus, arenavirus, rhabdovirus, paramyxovirus, and/or retrovirus. The present invention further includes compositions comprising such compounds, and methods of treating a viral infection in a subject using such compounds.
    Type: Application
    Filed: March 31, 2015
    Publication date: June 22, 2017
    Inventors: Ronald N. HARTY, Bruce D. FREEDMAN, Jay E. WROBEL, Allen B. REITZ, H. Marie LOUGHRAN
  • Publication number: 20170174679
    Abstract: Disclosed are compounds of Formula (I?), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
    Type: Application
    Filed: December 21, 2016
    Publication date: June 22, 2017
    Inventors: Neil Lajkiewicz, Liangxing Wu, Wenqing Yao
  • Publication number: 20170174680
    Abstract: The present invention is directed to a compound of Formula (I) or (Ia) The invention also relates to pharmaceutical compositions comprising compounds of Formula (I) or (Ia). Methods of making and using the compounds of Formula (I) or (Ia) are also within the scope of the invention.
    Type: Application
    Filed: March 2, 2017
    Publication date: June 22, 2017
    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: 20170174681
    Abstract: The invention relates to FGF-inhibiting pyrazolopyrimidine derivatives of general formula (I) to a process for preparing them and to the therapeutic use thereof.
    Type: Application
    Filed: March 7, 2017
    Publication date: June 22, 2017
    Inventors: Chantal ALCOUFFE, Kirsten BJEGARDE, Jacques MAUGER
  • Publication number: 20170174682
    Abstract: Provided is a compound or a salt thereof, which has an excellent JAK inhibitory action, and is useful as a prophylactic or therapeutic agent for autoimmune diseases (rheumatoid arthritis, psoriasis, inflammatory bowel disease, Sjogren's syndrome, Behcet's syndrome, multiple sclerosis, systemic lupus erythematosus, etc.), cancer (leukemia, uterine leiomyosarcoma, prostate cancer, multiple myeloma, cachexia, myelofibrosis, etc.) and the like. The present invention relates to a compound represented by the formula (I) wherein each symbol is as defined in the present specification, or a salt thereof.
    Type: Application
    Filed: March 7, 2017
    Publication date: June 22, 2017
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Masato YOSHIDA, Hiroyuki NAGAMIYA, Yusuke OHBA, Masaki SETO, Takatoshi YOGO, Satoshi SASAKI, Norihito TOKUNAGA, Kazuyoshi ASO
  • Publication number: 20170174683
    Abstract: The present invention is related to novel compounds of formula (I) that inhibit the activity of the FabI enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.
    Type: Application
    Filed: March 9, 2017
    Publication date: June 22, 2017
    Inventors: Jerôme Emile Georges Guillemont, David Francis Alain Lançois, Magali Madeleine Simone Motte, Anil Koul, Wendy Mia Albert Balemans, Eric Pierre Alexandre Arnoult
  • Publication number: 20170174684
    Abstract: Provided herein are ergoline compounds and pharmaceutical compositions thereof. In some embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and pharmaceutical compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT1A, 5-HT1B and 5-HT1D receptors without agonizing the 5-HT2B receptor using the compounds and pharmaceutical compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing the 5-HT2B adrenergic alpha2A and/or the alpha2B receptors using the compounds and pharmaceutical compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing the D2 and D3 receptor using the compounds and pharmaceutical compositions disclosed herein.
    Type: Application
    Filed: March 3, 2017
    Publication date: June 22, 2017
    Applicant: Xoc Pharmaceuticals, Inc.
    Inventors: Thomas Armer, Geoff McKinley, Scott Borland, Miguel Guzman, Ármin Szabolcs, János Gerencser
  • Publication number: 20170174685
    Abstract: Provided herein are ergoline compounds and pharmaceutical compositions thereof. In some embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and pharmaceutical compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT1A, 5-HT1B and 5-HT1D receptors without agonizing the 5-HT2B receptor using the compounds and pharmaceutical compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing the 5-HT2B adrenergic alpha2A and/or the alpha2B receptors using the compounds and pharmaceutical compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing the D2 and D3 receptor using the compounds and pharmaceutical compositions disclosed herein.
    Type: Application
    Filed: March 3, 2017
    Publication date: June 22, 2017
    Applicant: Xoc Pharmaceuticals, Inc.
    Inventors: Thomas Armer, Geoff McKinley, Scott Borland, Miguel Guzman, Armin Szabolcs, János Gerencser
  • Publication number: 20170174686
    Abstract: A process for preparation of a compound of Formula (I) is disclosed.
    Type: Application
    Filed: March 12, 2015
    Publication date: June 22, 2017
    Applicant: WOCKHARDT LIMITED
    Inventors: Vijaykumar Jagdishwar PATIL, Ravikumar TADIPARTHI, Satish BIRAJDAR, Mohammad Usman SHAIKH, Mahesh Vithalbhai PATEL
  • Publication number: 20170174687
    Abstract: (Formula I), The present invention relates to the compounds of formula I, processes for their preparation, pharmaceutical compositions containing them as active ingredient, methods for the treatment of disease states associated with cancers associated with protein kinases, to their use as medicaments for use in the production of inhibition of mTor, pi3k reducing effects in warm-blooded animals such as humans.
    Type: Application
    Filed: July 11, 2015
    Publication date: June 22, 2017
    Inventors: Paul Guoqing Chen, Changren Yan, Michael Reale, Monica Chen
  • Publication number: 20170174688
    Abstract: The invention provides for compounds of formula (I) wherein R1, R2, R3, R4, R5, and R6 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions mediated and modulated by SUV420H1. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).
    Type: Application
    Filed: December 17, 2015
    Publication date: June 22, 2017
    Applicant: AbbVie Inc.
    Inventors: Yujia Dai, William McClellan, Mike Michaelides, Ramzi Sweis, Noel Wilson, Justin Dietrich
  • Publication number: 20170174689
    Abstract: The present invention provides for compounds that inhibit the activity of an anti-apoptotic Bcl-2 family member Myeloid cell leukemia-1 (Mcl-1) protein. The present invention also provides for pharmaceutical compositions as well as methods for using compounds for treatment of diseases and conditions (e.g., cancer) characterized by the over-expression or dysregulation of Mcl-1 protein.
    Type: Application
    Filed: March 26, 2015
    Publication date: June 22, 2017
    Inventors: Taekyu Lee, Zhiguo Bian, Johannes Belmar, Plamen P. Christov, Nicholas F. Pelz, Subrata Shaw, Kwangho Kim, James C. Tarr, Edward T. Olejniczak, Bin Zhao, Stephen W. Fesik
  • Publication number: 20170174690
    Abstract: The present invention relates to substituted 4,5,6,7-tetrahydro-pyrazolo[1,5-a]pyrazine derivatives and 5,6,7,8-tetrahydro-4H-pyrazolo[1,5-a][1,4]diazepine derivatives of formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as ROS1 inhibitors. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Application
    Filed: March 26, 2015
    Publication date: June 22, 2017
    Applicant: Janssen Pharmaceutica NV
    Inventors: Laurence Anne Mevellec, Elisabeth Therese Jeanne Pasquier, Sophie Descamps, Guillaume Jean Maurice Mercey, Berthold Wroblowski, Jorge Eduardo Vialard, Lieven Mrrtpoel, Matthieu Ludovic Jeanty, Thierry Francois Alain Jean Jousseaume
  • Publication number: 20170174691
    Abstract: The invention relates to protein conjugates that contain a protein kinase containing a cysteine residue in the ATP binding site and an inhibitor that is covalently and irreversibly bonded to said cysteine residue, such that the activity of the protein kinase is irreversibly inhibited. The invention also relates to compounds that irreversibly inhibit protein kinases.
    Type: Application
    Filed: July 18, 2016
    Publication date: June 22, 2017
    Inventors: Juswinder Singh, Russell Colyn Petter, Deqiang Niu, Lixin Qiao, Arthur Kluge, Roy Lobb, Shomir Ghosh, Zhendong Zhu
  • Publication number: 20170174692
    Abstract: The present invention provides novel compounds described herein, such as of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of cyclin-dependent kinase 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.
    Type: Application
    Filed: April 3, 2015
    Publication date: June 22, 2017
    Inventors: Jason J. Marineau, Kevin Sprott, Darby Schmidt
  • Publication number: 20170174693
    Abstract: The invention provides compounds of the Formula (I) or a pharmaceutically acceptable salts thereof, wherein X, Y, Z, R1, R2, R4, Ra, and the subscripts m, p, and q are as described herein. The compounds or their pharmaceutically acceptable salts can modulate the body's production of cyclic guanosine monophosphate (“cGMP”), and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The invention also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose.
    Type: Application
    Filed: December 20, 2016
    Publication date: June 22, 2017
    Inventors: Raphaelle Berger, Yi-Heng Chen, Guoqing Li, Joie Garfunkle, Hong-Dong Li, Shouwu Miao, Subharekha Raghavan, Cameron J. Smith, John Stelmach, Alan Whitehead, Rui Zhang, Yong Zhang, Jianmin Fu, Gang Ji, Falong Jiang
  • Publication number: 20170174694
    Abstract: The present disclosure is concerned with certain pyrrolopyrimidine compounds that are capable of inhibiting certain protein kinases, and especially the leucine-rich repeat kinase 2 (LRRK2) protein. Compounds of the present disclosure can be used to treat a number of disorders caused by or associated with abnormal LRRK2 kinase activity. Compounds of the present disclosure can be used to treat disorders including neurodegenerative diseases such as Parkinson's disease; precancerous conditions and cancer; autoimmune disorders such as Crohn's disease, rheumatoid arthritis and psoriasis; and leprosy (Hansen's disease). 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: Application
    Filed: December 16, 2016
    Publication date: June 22, 2017
    Inventors: Corinne E. Augelli-Szafran, Mark Suto, Robert Galemmo, Omar Moukha-Chafiq, Vandana Gupta, Subramaniam Ananthan
  • Publication number: 20170174695
    Abstract: The present invention encompasses compounds of formula (I) wherein the groups R1 to R4, R7, A, D, E, F, V, W, X, Y, n, r and q are defined in claim 1, their use as inhibitors of MDM2-p53 interaction, pharmaceutical compositions which contain compounds of this kind, their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases, and synthetic intermediates.
    Type: Application
    Filed: October 7, 2016
    Publication date: June 22, 2017
    Inventors: Andreas GOLLNER, Joachim BROEKER, Nina KERRES, Christiane KOFINK, Juergen RAMHARTER, Harald WEINSTABL, Annika GILLE, Stefan GOEPPER, Manuel HENRY, Guenther HUCHLER
  • Publication number: 20170174696
    Abstract: Compounds of Formula I, including their salts, as well as compositions and methods of using the compounds are set forth. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
    Type: Application
    Filed: March 20, 2015
    Publication date: June 22, 2017
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Tao Wang, Zhongxing Zhang, John F. Kadow