Plural Ring Nitrogens In The Additional Hetero Ring (e.g., Imidazole, Pyrazine, Etc.) Patents (Class 514/235.8)
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Publication number: 20140178360Abstract: The present invention relates to pyrimidine compounds of formula (I): which are useful in treating mTOR kinase- or PI3K kinase-related diseases.Type: ApplicationFiled: February 27, 2014Publication date: June 26, 2014Applicants: DCB-USA LLC, DEVELOPMENT CENTER FOR BIOTECHNOLOGYInventors: Mann-Yan KUO, Ying-Shuan Lee, Paonien Chen, Li Jung Chen, Yann Yu Lu, Yi-Ting Huang, Hung-Yi Hsu, Ping-Kuei Tsai
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Publication number: 20140178470Abstract: The present invention relates to a tablet comprising Nimorazole. In particular, the invention concerns a pharmaceutical composition or a tablet comprising Nimorazole or a pharmaceutically acceptable salt, for dispersion in water and administration via a tube to a patient with swallowing difficulties.Type: ApplicationFiled: February 28, 2014Publication date: June 26, 2014Applicant: Azanta A/SInventors: Nilesh Tanhaji Dumbre, Mahesh Mohanrao Bhadgale, Vardhaman Chandrakant Bafna
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Publication number: 20140179664Abstract: The present invention relates to compounds of formula (I) wherein X1 to X5, Z1 to Z3, Y0, RY1, RY2 and R have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.Type: ApplicationFiled: July 24, 2012Publication date: June 26, 2014Applicant: Cellzome LimitedInventors: Jay Freeman, Valerie Reader, Glynn Addison, Nigel Ramsden, Jane Elizabeth Scanlon, Richard John Harrison
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Patent number: 8759365Abstract: The present invention provides a compound of formula (I): wherein the variants R1, R2, R3, R4, R6, R7 are as defined herein, and wherein said compound is an inhibitor of CETP, and thus can be employed for the treatment of a disorder or disease mediated by CETP or responsive to the inhibition of CETP.Type: GrantFiled: December 1, 2008Date of Patent: June 24, 2014Assignee: Novartis AGInventors: Muneto Mogi, Toshio Kawanami, Ken Yamada, Kayo Yasoshima, Hidetomo Imase, Takahiro Miyake, Osamu Ohmori
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Publication number: 20140171421Abstract: A compound of Formula I in free or salt or solvate form, where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: ApplicationFiled: February 21, 2014Publication date: June 19, 2014Applicant: NOVARTIS AGInventors: Gurdip Bhalay, Emma Budd, Graham Charles Bloomfield, Stephen Paul Collingwood, Andrew Dunstan, Lee Edwards, Peter Gedeck, Catherine Howsham, Peter Hunt, Thomas Anthony Hunt, Paul Oakley, Nichola Smith
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Publication number: 20140171433Abstract: A method of treating a subject presenting with multiple myeloma at a stage characterized by an increase in the prevalence of MM cells that (1) are IL-6 non-responsive and/or (2) have a CD45? phenotype, comprising administering to the subject an amount of a compound of formula Ib.Type: ApplicationFiled: May 1, 2012Publication date: June 19, 2014Applicant: YM Biosciences Australia Pty LtdInventors: Christopher John Burns, Andrew Spencen, Katherine Anne Monaghan
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Publication number: 20140162983Abstract: The present invention provides novel pyrimidine and pyridine compounds according to Formula (I), Formula (II), Formula (III), Formula (IV) and Formula (V) their manufacture and use for the treatment of hyperproliferative diseases including, but not limited to, cancer, lupus, allergic disorders, Sjogren's disease and rheumatoid arthritis. In preferred embodiments, the present invention describes irreversible kinase inhibitors including, but not limited to, inhibitors of Bruton's tyrosine kinase.Type: ApplicationFiled: June 10, 2012Publication date: June 12, 2014Applicant: Merck Patent GmbHInventors: Brian L. Hodous, Lesley Liu-Bujalski, Reinaldo Jones, Donald Bankston, Theresa L. Johnson, Igor Mochalkin, Ngan Nguyen, Hui Qiu, Andreas Goutopoulos, Nadia Brugger
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Publication number: 20140162999Abstract: PIM kinase inhibitor compound having a structure as represented by Formula I, and isomers, diastereomers, enantiomers, tautomers, and pharmaceutically acceptable salts of the compounds as represented by Formula I. The compounds significantly inhibit the Pim kinase activity and are used to prepare drugs to treat PIM kinase mediated diseases, such as cancers, autoimmune diseases, allergic reactions, or organ transplant rejection. Also provided are methods for preparing the compounds represented by Formula I.Type: ApplicationFiled: February 10, 2014Publication date: June 12, 2014Applicant: Jikai Biosciences, Inc.Inventor: Yu GE
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Patent number: 8748423Abstract: The invention relates to compositions and methods for the treatment and prevention of cancer and other cell proliferative disorders.Type: GrantFiled: March 11, 2011Date of Patent: June 10, 2014Assignee: Kinex Pharmaceuticals, LLCInventors: David G. Hangauer, Jr., Michael J. Ciesielski, Robert Alan Fenstermaker
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Publication number: 20140155382Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.Type: ApplicationFiled: November 22, 2013Publication date: June 5, 2014Applicant: ABBVIE INC.Inventors: David A. DEGOEY, Allan C. KRUEGER, Charles W. HUTCHINS, Warren M. KATI, William A. CARROLL
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Publication number: 20140155402Abstract: The present invention includes novel methods of treating a disease or disorder characterized by hyperactivity of Vps34, and compound as Vps34 inhibitors; particularly compounds of Formula I: or a pharmaceutically acceptable salt thereof, as well as methods of treating a disease, disorder, or syndrome associated with Vps34 inhibition, particularly hyperproliferative diseases. The present invention also includes pharmaceutical compositions including compounds of formula I and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: February 5, 2014Publication date: June 5, 2014Applicant: Novartis AGInventors: Ivan Cornella Taracido, Edmund Harrington, Ayako Honda, Erin Keaney
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Patent number: 8742099Abstract: Compounds of formula (I) wherein R1 is 2-indanyl, R2 is 1-methylpropyl, R3 is a group selected from 2,6-dimethyl-3-pyridyl or 4,6-dimethyl-3-pyridyl, R4 represents methyl and R5 represents hydrogen or methyl or, R4 and R5 together with the nitrogen atom to which they are attached represent morpholino and pharmaceutically acceptable derivatives thereof are described, as are processes for their preparation, pharmaceutical compositions containing them and their use in medicine, particularly their use as oxytocin antagonists.Type: GrantFiled: May 20, 2013Date of Patent: June 3, 2014Assignee: Glaxo Group LimitedInventors: Alan David Borthwick, Deirdre Mary Bernadette Hickey, John Liddle, Andrew McMurtrie Mason
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Patent number: 8741344Abstract: The present invention relates to a tablet comprising Nimorazole. In particular, the invention concerns a pharmaceutical composition or a tablet comprising Nimorazole or a pharmaceutically acceptable salt, for dispersion in water and administration via a tube to a patient with swallowing difficulties.Type: GrantFiled: February 28, 2014Date of Patent: June 3, 2014Assignee: Azanta A/SInventors: Nilesh Tanhaji Dumbre, Mahesh Mohanrao Bhadgale, Vardhaman Chandrakant Bafna
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Publication number: 20140148454Abstract: The invention relates to amino-arylcarboxamides, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.Type: ApplicationFiled: November 27, 2013Publication date: May 29, 2014Applicant: GRÜNENTHAL GMBHInventors: Simon LUCAS, Sven Kühnert, Gregor Bahrenberg, Wolfgang Schröder
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Publication number: 20140148448Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, colon cancer, stomach cancer, hairy cell leukemia and non-small lung carcinoma; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including arthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.Type: ApplicationFiled: January 30, 2014Publication date: May 29, 2014Applicant: Janssen Pharmaceutica NVInventors: Carl R. ILLIG, Shelley K. BALLENTINE, Jinsheng CHEN, Renee Louise DESJARLAIS, Sanath K. MEEGALLA, Mark WALL, Kenneth WILSON
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Publication number: 20140148443Abstract: Disclosed are compounds of Formula I or pharmaceutically acceptable salts thereof, wherein X1, X2, X3, R1, R2 and R3 are as described in this application, and methods of using the compounds in the treatment of cancer.Type: ApplicationFiled: November 20, 2013Publication date: May 29, 2014Applicant: Hoffmann-La Roche Inc.Inventors: Xin-Jie Chu, Allen John Lovey, Binh Thanh Vu, Chunlin Zhao
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Publication number: 20140148453Abstract: Disclosed are sulfonamide compounds of Formula (I): or stereoisomers, N-oxides, prodrugs, or pharmaceutically acceptable salts thereof, wherein ring A, R1, R2, R3, R4 and R5 are defined herein. Also disclosed are methods of using such compounds in the treatment of conditions related to CYP17 enzyme, such as cancer, and pharmaceutical compositions comprising such compounds.Type: ApplicationFiled: July 25, 2011Publication date: May 29, 2014Inventors: Joel Francis Austin, Lisa S. Sharma, James Aaron Balog, Audris Huang, Upender Velaparthi, Chetan Padmakar Darne, Mark George Saulnier
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Publication number: 20140142104Abstract: The present invention relates to novel pyrimidine hydroxy amide compounds, and the use of such compounds in the inhibition of HDAC6 and in the treatment of various diseases, disorders or conditions related to HDAC6.Type: ApplicationFiled: November 18, 2013Publication date: May 22, 2014Inventors: John H. van Duzer, Ralph Mazitschek, Yanbing Ding, Nan Yu, Yun Cao, Yong Liu
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Publication number: 20140142097Abstract: Compounds of the formula (I) in which R, R1 and X have the meanings indicated in claim 1, are inhibitors of TBK1 and IKK? and can be employed, inter alia, for the treatment of cancer and inflammatory diseasesType: ApplicationFiled: April 11, 2012Publication date: May 22, 2014Applicant: Merck Patent GmbHInventors: Guenter Hoelzemann, Hans-Michael Eggenweiler, Srinivasa R. Karra
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Publication number: 20140142084Abstract: Provided is a compound useful as a prophylactic and/or therapeutic agent for bladder cancer. As a result of studies on compounds having FGFR inhibitory action, the present inventors have found that the nitrogen-containing aromatic heterocyclic compounds of the present invention have inhibitory action on FGFR1, FGFR2, and/or FGFR3, particularly, mutant FGFR3, and thus, the present invention has been accomplished. The nitrogen-containing aromatic heterocyclic compound of the present invention can be used as a therapeutic agent for various cancers related to FGFR1, FGFR2, and/or FGFR3, such as lung cancer and hormone therapy-resistant breast cancer, stomach cancer, triple negative breast cancer, endometrial cancer, bladder cancer, and glioblastoma, particularly as a prophylactic and/or therapeutic agent for mutant FGFR3-positive bladder cancer.Type: ApplicationFiled: February 26, 2013Publication date: May 22, 2014Applicants: KOTOBUKI PHARMACEUTICAL CO., LTD., Astellas Pharma Inc.Inventors: Minoru Kameda, Ikumi Kuriwaki, Kazuhiko Iikubo, Hiroyuki Hisamichi, Yuichiro Kawamoto, Hiroyuki Moritomo, Tomoyuki Suzuki, Takashi Futami, Atsushi Suzuki, Kazuhisa Tsunoyama, Makoto Asaumi, Hiroshi Tomiyama, Atsushi Noda, Yoshinori Iwai, Kazuo Tokuzaki, Haruki Okada, Kozo Miyasaka
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Patent number: 8729077Abstract: Disclosed are compounds, stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, their preparation, use, and compositions thereof for treating an infection mediated at least in part by a virus in the Flaviviridae family of viruses.Type: GrantFiled: November 19, 2009Date of Patent: May 20, 2014Assignee: GlaxoSmithKline LLCInventors: Frank Ulrich Schmitz, Roopa Rai, Christopher Don Roberts, Wieslaw Kazmierski, Richard Grimes
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Publication number: 20140135298Abstract: This invention is in the fields of cancer therapy. More particularly it concerns compounds which are useful agents for treating cell proliferative disorders, especially those disorders characterized by over activity and/or inappropriate activity of a EGFR, including EGFR-related cancers, particularly for expanding the efficacy of drugs previously developed for this purpose, and for methods of treatments using the compounds for this purpose.Type: ApplicationFiled: March 16, 2012Publication date: May 15, 2014Applicant: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIAInventors: Alan Berezov, Mark I. Greene, Natalie Minkovsky, Zheng Cai, Hongtao Zhang
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Publication number: 20140135329Abstract: The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.Type: ApplicationFiled: June 20, 2013Publication date: May 15, 2014Inventors: Urs BAETTIG, Kamlesh BALA, Emma BUDD, Lee EDWARDS, Catherine HOWSHAM, Glyn Alan HUGHES, Darren Mark LEGRAND, Katrin SPIEGEL
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Publication number: 20140135330Abstract: The present invention relates to oxazolidin-2-one substituted pyrimidine compounds that act as PI3K (phosphatidylinositol-3-kinase) inhibitors, as well as pharmaceutical compositions thereof, methods for their manufacture and uses for the treatment of conditions, diseases and disorders dependent on PI3K.Type: ApplicationFiled: November 1, 2013Publication date: May 15, 2014Applicant: NOVARTIS AGInventors: Robin Alec Fairhurst, Pascal Furet, Frank Stephan Kalthoff, Andreas Lerchner, Heinrich Rueeger
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Publication number: 20140134262Abstract: The present invention provides a compound of Formula I: for use in the treatment, amelioration and/or prevention of diseases and conditions associated with CETP activity, such as atherosclerosis and dyslipidemia, in a subject with high triglyceride level; wherein R1, X1, R7, R5, C, L and p are defined herein. The present invention further provides a combination of pharmacologically active agents for use in the treatment, amelioration and/or prevention of diseases and conditions associated with CETP activity, such as atherosclerosis and dyslipidemia, in a subject with high triglyceride levels.Type: ApplicationFiled: July 6, 2012Publication date: May 15, 2014Inventors: Yoshie Arai, Margaret Elizabeth Brousseau, Jessie Gu, Tomoko Hayashi, Hironobu Mitani, Muneto Mogi, Kazuhiko Nonomura, Ken Yamada
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Publication number: 20140128394Abstract: This invention relates to a piperazine compound represented by Formula (I), wherein R1 is c1-6 alkyl; R2 is hydroxy, c1-6 alkyl that may have one or more substituents, —(C=0)-N(R2)(R4), or —(C=0)-0R5; R3 and R4 are the same or different, and each represents hydrogen or c1-6 alkyl that may have one or more substituents, or R3 and R4, taken together with a nitrogen atom to which R3 and R4 are attached, may form a saturated heterocyclic group; R5 is hydrogen or c1-6 alkyl that may have one or more 15 substituents; and n is 1 or 2; or a salt thereof.Type: ApplicationFiled: January 8, 2014Publication date: May 8, 2014Applicant: TAIHO PHARMACEUTICAL CO., LTD.Inventors: Yoshihiro URADE, Makoto KITADE, Kazuhiko SHIGENO, Keiko YAMANE, Katsunao TANAKA
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Publication number: 20140128385Abstract: The present invention relates to the use of BACE-2 inhibitors and pharmaceutical compositions comprising BACE-2 inhibitors for treating metabolic disorders related to decreased ? cell mass and/or function.Type: ApplicationFiled: January 13, 2012Publication date: May 8, 2014Inventor: Heinrich Ruegger
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Patent number: 8716285Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt, ester or stereoisomer thereof, wherein R1 to R3 and X have the significances given herein. The present invention is also directed to processes for making said compounds and uses of said compounds, in particular their use as medicaments, more particularly their use as medicaments in the treatment of cancer.Type: GrantFiled: September 7, 2011Date of Patent: May 6, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Lei Guo, Guozhi Tang, Zhanguo Wang, Jason Christopher Wong, Weixing Zhang
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Patent number: 8716286Abstract: The present invention relates to crystalline forms of (3R,6R)-3-(2,3-dihydro-1H-inden-2-yl)-1-[(1R)-1-(2,6-dimethyl-3-pyridinyl)-2-(4-morpholinyl)-2-oxoethyl]-6-[(1S)-1-methylpropyl]-2,5-piperazinedione benzenesulfonate salt and pharmaceutical compositions thereof. Also disclosed are processes for the preparation the above compounds and methods for use thereof.Type: GrantFiled: October 28, 2010Date of Patent: May 6, 2014Assignee: Glaxo Group LimitedInventors: Richard Bellingham, Andrew Mark Buswell, Victoria Ironmonger, Michael Urquhart
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Patent number: 8716281Abstract: The present invention describes pyrimidine compounds of Formula I that are useful as anaplastic lymphoma kinase inhibitors, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: GrantFiled: May 4, 2011Date of Patent: May 6, 2014Assignee: Amgen Inc.Inventors: Marian C. Bryan, Alan C. Cheng, Elizabeth M. Doherty, James R. Falsey, Ingrid M. Fellows, Joseph L. Kim, Richard T. Lewis, Michele H. Potashman, Douglas A. Whittington
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Patent number: 8716287Abstract: A compound of the formula (I):Type: GrantFiled: May 12, 2011Date of Patent: May 6, 2014Assignee: Sentinel Oncology LimitedInventors: Robert George Boyle, David Winter Walker, Richard Justin Boyce
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Patent number: 8716470Abstract: [Problem] The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases. [Means for Solution] The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that the compound or a salt thereof of the present invention exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. In addition, the present invention relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound or a salt thereof of the present invention, and an excipient.Type: GrantFiled: January 31, 2013Date of Patent: May 6, 2014Assignee: Astellas Pharma Inc.Inventors: Kousei Yoshihara, Daisuke Suzuki, Susumu Yamaki, Hiroyoshi Yamada, Hisashi Mihara, Norio Seki
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Publication number: 20140121208Abstract: The present invention relates to pharmaceutical compositions comprising an inhibitor of epithelial sodium channel activity in combination with at least one ABC Transporter modulator compound of Formula A, Formula B, Formula C, or Formula D. The invention also relates to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis using the pharmaceutical combination compositions.Type: ApplicationFiled: December 16, 2013Publication date: May 1, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Fredrick F. Van Goor, William Lawrence Burton
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Publication number: 20140121193Abstract: The invention provides methods for treating or ameliorating cognitive dysfunction, fatigue, energy, concentration, mood, and pain associated with fibromyalgia using compositions containing methylphenidate or pharmaceutically equivalents thereof.Type: ApplicationFiled: November 1, 2013Publication date: May 1, 2014Inventors: Robert S. KATZ, Frank LEAVITT
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Patent number: 8703188Abstract: The present invention relates to a tablet comprising Nimorazole. In particular, the invention concerns a pharmaceutical composition or a tablet comprising Nimorazole or a pharmaceutically acceptable salt, for dispersion in water and administration via a tube to a patient with swallowing difficulties.Type: GrantFiled: November 19, 2012Date of Patent: April 22, 2014Assignee: Azanta A/SInventors: Nilesh Tanhaji Dumbre, Mahesh Mohanrao Bhadgale, Vardhaman Chandrakant Bafna
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Patent number: 8703767Abstract: In one aspect, the invention relates to substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the BTK kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the BTK 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: GrantFiled: April 1, 2012Date of Patent: April 22, 2014Assignee: University of Utah Research FoundationInventors: David J. Bearss, Hariprasad Vankayalapati, Venkataswamy Sorna, Steven L. Warner, Sunil Sharma
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Publication number: 20140107123Abstract: The invention relates to the treatment and prevention of type I diabetes. More specifically, the invention relates to compounds that treat or prevent the body's immune system from destroying ?-cells (i.e., insulin-producing cells in the pancreatic islets of Langerhans) by inhibition of JNK2, selective inhibition of JNK2, or inhibition of the expression of the MAPK9 gene or gene product. In one embodiment, the present invention contemplates the diagnosis, identification, production, and use of compounds which modulate MAPK9 gene expression or the activity of the MAPK9 gene product including but not limited to, JNK2, the nucleic acid encoding MAPK9 and homologues, analogues, and deletions thereof, as well as antisense, ribozyme, triple helix, antibody, and polypeptide molecules as well as small inorganic molecules. The present invention contemplates a variety of pharmaceutical formulations and routes of administration for such compounds.Type: ApplicationFiled: August 5, 2013Publication date: April 17, 2014Applicant: University of MassachusettsInventors: Roger J. Davis, Anja Jaeschke
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Publication number: 20140107118Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of Alzheimer's Disease or diabetes via inhibition of BACE-1 or BACE-2.Type: ApplicationFiled: December 20, 2013Publication date: April 17, 2014Applicant: NOVARTIS AGInventors: Sangamesh BADIGER, Murali CHEBROLU, Konstanze HURTH, Sebastien JACQUIER, Rainer Martin LUEOEND, Rainer MACHAUER, Heinrich RUEEGER, Marina TINTELNOT-BLOMLEY, Siem Jacob VEENSTRA, Markus VOEGTLE
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Publication number: 20140107119Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.Type: ApplicationFiled: November 15, 2013Publication date: April 17, 2014Applicant: AbbVie Inc.Inventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura A. Hexamer, Aaron R. Kunzer, Robert A. Mantei, William J. McClellan, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt, Todd M. Hansen
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Patent number: 8697694Abstract: The present invention provides compounds of Formula (I): and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and prodrugs of said compounds, wherein each of R, R1, X, Y, Z, R2, R3, R4, R5, R6, R7, R8, R9, R18, R19 and n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing diseases or disorders such as viral infections and virus-related disorders.Type: GrantFiled: August 19, 2009Date of Patent: April 15, 2014Assignees: Merck Sharp & Dohme Corp., Southern Research InstituteInventors: Ashok Arasappan, F. George Njoroge, Cecil D. Kwong, Subramaniam Ananthan, Frank Bennett, Jeremy Clark, Hollis S. Kezar, III, Vinay M. Girijavallabhan, Yuhua Huang, Regina Huelgas, Joseph A. Maddry, John J. Piwinski, Robert C. Reynolds, Abhijit Roychowdhury, Anita T. Fowler, Feng Geng, John A. Secrist, III, Neng-Yang Shih, Vishal Verma, Francisco Velazquez, Srikanth Venkatraman
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Patent number: 8697687Abstract: A compound of Formula I in free or salt or solvate form, where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: GrantFiled: September 13, 2012Date of Patent: April 15, 2014Assignee: Novartis AGInventors: Gurdip Bhalay, Emma Budd, Graham Charles Bloomfield, Stephen Paul Collingwood, Andrew Dunstan, Lee Edwards, Peter Gedeck, Catherine Howsham, Peter Hunt, Thomas Anthony Hunt, Paul Oakley, Nichola Smith
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Patent number: 8697695Abstract: The present invention provides a pest control composition comprising, as active ingredients, (A) an amide compound of the formula (I), wherein R1 is an ethyl group, R2 is a hydrogen atom or an ethyl group, R3 is a methyl group, R4 is a chlorine atom, a bromine atom or a methyl group, R5 is a chlorine atom, a bromine atom or a cyano group, R6 is a chlorine atom, a bromine atom or a trifluoromethyl group and R7 is a chlorine atom; and (B) pyriproxyfen.Type: GrantFiled: October 19, 2010Date of Patent: April 15, 2014Assignee: Sumitomo Chemical Company, LimitedInventors: Norihisa Sakamoto, Shinya Nishimura
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Publication number: 20140100210Abstract: [Problem] The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases. [Means for Solution] The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that the compound or a salt thereof of the present invention exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. In addition, the present invention relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound or a salt thereof of the present invention, and an excipient.Type: ApplicationFiled: December 6, 2013Publication date: April 10, 2014Applicant: Astellas Pharma Inc.Inventors: Kousei YOSHIHARA, Daisuke SUZUKI, Susumu YAMAKI, Hiroyoshi YAMADA, Hisashi MIHARA, Norio SEKI
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Publication number: 20140100224Abstract: The present application is related to compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders associated with p75 expression, such as degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such compounds.Type: ApplicationFiled: June 26, 2013Publication date: April 10, 2014Applicants: The University of North Carolina at Chapel Hill, U.S. Government represented by the Department of Veterans Affairs, The Regents of the University of CaliforniaInventors: Frank M. Longo, Stephen M. Massa
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Publication number: 20140100225Abstract: Novel compounds and their synthesis are described. Methods for using these compounds in the prevention or treatment of cancer, a bacterial infection or a viral infection in a subject are also described.Type: ApplicationFiled: October 4, 2013Publication date: April 10, 2014Applicants: Inhibikase Therapeutics, Inc., Sphaera Pharma Pvt. Ltd., Sphaera Pharma Pte. Ltd.Inventors: Rhushikesh Chandrabhan Deokar, Sundeep Dugar, Dinesh Mahajan, Milton Henry Werner
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Patent number: 8691817Abstract: The present application relates to novel sulfonamide- or sulfoximine-substituted 1,4-diaryldihydropyrimidin-2-one derivatives, to processes for their preparation, to their use alone or in combination for the treatment and/or prevention of diseases and also to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of disorders of the lung and the cardiovascular system.Type: GrantFiled: March 30, 2010Date of Patent: April 8, 2014Assignee: Bayer Intellectual Property GmbHInventors: Franz Von Nussbaum, Dagmar Karthaus, Sonja Anlauf, Martina Delbeck, Volkhart Min-Jian Li, Daniel Meibom, Klemens Lustig, Dirk Schneider
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Patent number: 8691777Abstract: The disclosure relates to methods of treating tuberous sclerosis in a subject, comprising administering a composition comprising an mTOR inhibitor and a tyrosine kinase inhibitor to a subject that is diagnosed with, suspected of, or exhibiting symptoms of cancer. In some embodiments, the cancer is tuberous sclerosis. In some embodiments, the mTOR inhibitor is sirolimus and the tyrosine kinase inhibitor is imatinib. In some embodiments, the disclosure relates to a composition comprising an mTOR inhibitor and a tyrosine kinase inhibitor. In some embodiments, the disclosure relates to a composition comprising sirolimus and imatinib.Type: GrantFiled: January 25, 2012Date of Patent: April 8, 2014Assignee: Emory UniversityInventor: Jack L. Arbiser
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Publication number: 20140094436Abstract: Compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I) and methods of inhibiting Hsp90 in a cell, treating or preventing a proliferation disorder in a mammal and treating cancer in a mammal comprising administering a compound of formula (I) to a patient or a cell. Variable R5 is an optionally substituted heteroaryl; an optionally substituted 6 to 14-membered aryl; a bicyclic 9-member heterocycle optionally substituted at any substitutable nitrogen or carbon atoms; or a substituent R18, defined herein. Ring A is an aryl or a heteroaryl optionally further substituted with one or more substituents in addition to R3. Substituent R3 is defined herein.Type: ApplicationFiled: December 11, 2013Publication date: April 3, 2014Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: Weiwen Ying, Zhenjian Du, Kevin Foley
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Patent number: 8685972Abstract: The invention encompasses pyrimidine derivatives as gamma secretase modulators, useful for treating diseases associated with the deposition of beta-amyloid peptide in the brain, such as Alzheimer's disease, or of preventing or delaying the onset of dementia associated with such diseases. Pharmaceutical compositions and methods of use are included.Type: GrantFiled: July 31, 2009Date of Patent: April 1, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Alexey A. Rivkin, Sean P. Ahearn, Stephanie M. Chichetti
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Patent number: 8685973Abstract: The present invention provides a class of pyrimidinedione cyclohexyl compounds and methods of using these compounds as glucocorticoid receptor modulators.Type: GrantFiled: March 16, 2012Date of Patent: April 1, 2014Assignee: Corcept Therapeutics, Inc.Inventors: Robin Clark, George Hynd, Nicholas Ray, Mohammad Sajad