The Additional Hetero Ring Contains Ring Nitrogen Patents (Class 514/210.2)
-
Publication number: 20140235608Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.Type: ApplicationFiled: September 26, 2012Publication date: August 21, 2014Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: John Lloyd, Jeniffer X. Qiao, Heather Finlay, James Neels, Zulan Pi, Carol Hui Hu, Tammy C. Wang
-
Patent number: 8809317Abstract: Compounds and methods for preventing and treating viral infections are provided. In some embodiments, novel compounds broad-spectrum antiviral activity are provided. In more specific embodiments, the compounds and methods are effective against viruses such as Venezuelan Equine Encephalitis, West Nile Virus, and Hepatitis C.Type: GrantFiled: March 29, 2012Date of Patent: August 19, 2014Assignee: Prosetta Antiviral Inc.Inventors: Clarence R. Hurt, Vishwanath Lingappa, Beverly Freeman, Andy Atuegbu, Anatoliy Kitaygorodskyy
-
Publication number: 20140228339Abstract: There is provided a compound which is (a) a pyrimidine sulfonamide of formula (I) or (b) a pharmaceutically acceptable salt thereof, crystalline forms of the compound, processes for obtaining the compound, pharmaceutical intermediates used in the manufacture of the compound, and pharmaceutical compositions containing the compound. The compound is useful in the treatment of a disease/condition in which modulation of chemokine receptor activity is beneficial.Type: ApplicationFiled: April 15, 2014Publication date: August 14, 2014Applicant: AstraZeneca ABInventors: Stephen Connolly, Mark Richard Ebden, Iain Alastair Stewart Walters, Thomas Langer, Alan Robert Steven, Craig Robert Stewart, Paula Margaret Tomlin, Andrew John Williams
-
Publication number: 20140228338Abstract: The topical ophthalmic use of certain 2,4-diamino-substituted 1,3-triazines for preventing or alleviating ocular pain in patients is disclosed. Topcial ocular pharmaceutical composition are also disclosed.Type: ApplicationFiled: February 13, 2014Publication date: August 14, 2014Applicant: Novartis AGInventors: Martha E. Gadd, Peter G. Klimko, Karen C. David, Kenneth C. Appell, Mark R. Hellberg
-
Publication number: 20140228340Abstract: Compounds of the formula I, in which R1, R2, X and Y 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 diseases.Type: ApplicationFiled: August 13, 2012Publication date: August 14, 2014Applicant: MERCK PATENT GMBHInventors: Guenter Hoelzemann, Dieter Dorsch, Hans-Michael Eggenweiler
-
Publication number: 20140228322Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.Type: ApplicationFiled: February 7, 2014Publication date: August 14, 2014Applicant: Celgene Avilomics Research, Inc.Inventors: Nadia Haq, Deqiang Niu, Russell C. Petter, Lixin Qiao, Juswinder Singh, Zhendong Zhu
-
Publication number: 20140228348Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.Type: ApplicationFiled: September 21, 2012Publication date: August 14, 2014Inventors: Jason Brubaker, Matthew Lloyd Childers, Matthew Christopher, Joshua T. Close, Jason David Katz, Joon Jung, Scott Peterson, Phieng Siliphaivanh, Tony Siu, Graham Frank Smith, Luis E. Torres, Hyun Chong Woo, Jonathan R. Young, Hongjun Zhang
-
Patent number: 8802657Abstract: The present invention provides compounds useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.Type: GrantFiled: October 22, 2012Date of Patent: August 12, 2014Assignees: Millennium Pharmaceuticals, Inc., Sunesis Pharmaceuticals, Inc.Inventors: Jennifer Cossrow, Bing Guan, John Howard Jones, Gnanasambandam Kumaravel, Alexey Lugovskoy, Hairuo Peng, Noel Powell, Brian C. Raimundo, Hiroko Tanaka, Jeffrey Vessels, Thomas Wynn, Zhili Xin
-
Publication number: 20140221334Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: ApplicationFiled: April 10, 2014Publication date: August 7, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Juan-Miguel Jimenez, Guy William Bemis, Francois Maltais, Tiansheng Wang, Ronald Marcellus Alphonsus Knegtel, Christopher John Davis, Damien Fraysse, Dean Boyall, Luca Settimo, Stephen Young, Michael Paul Mortimore
-
Publication number: 20140221332Abstract: Compounds that modulate GluR5 activity and methods of using the same are disclosed.Type: ApplicationFiled: May 25, 2012Publication date: August 7, 2014Applicant: SUNOVION PHARMACEUTICALS INC.Inventors: Michele L. R. Heffernan, Larry Wendell Hardy, Frank Xinhe Wu, Lakshmi D. Saraswat
-
Publication number: 20140221311Abstract: The present invention relates to compounds of Formula (I), or a form thereof, wherein ring A, R1, R2, R3, R3?, L, W, and V are as defined herein, useful as FLAP modulators. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I).Type: ApplicationFiled: January 31, 2014Publication date: August 7, 2014Applicant: JANSSEN PHARMACEUTICA NVInventors: Genesis M. Bacani, Wendy Eccles, Anne E. Fitzgerald, Steven D. Goldberg, Michael D. Hack, Natalie A. Hawryluk, William M. Jones, John M. Keith, Paul Krawczuk, Alec D. Lebsack, Alice Lee-Dutra, Jing Liu, Kelly J. McClure, Steven P. Meduna, Daniel J. Pippel, Mark D. Rosen, Zachary S. Sales
-
Publication number: 20140221310Abstract: The present invention relates to compounds of Formula (I), or a form thereof, wherein ring A, R1, L and R2 are as defined herein, useful as FLAP modulators. 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: ApplicationFiled: January 31, 2014Publication date: August 7, 2014Applicant: JANSSEN PHARMACEUTICA NVInventors: Wendy Eccles, Anne E. Fitzgerald, Michael D. Hack, Natalie A. Hawryluk, William M. Jones, John M. Keith, Paul Krawczuk, Alec D. Lebsack, Jing Liu, Neelakandha S. Mani, Kelly J. McClure, Steven P. Meduna, Mark D. Rosen
-
Patent number: 8796255Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: GrantFiled: November 8, 2011Date of Patent: August 5, 2014Assignee: Celgene Avilomics Research, IncInventors: Kwangho Lee, Deqiang Niu, Matthew F. Baevsky
-
Patent number: 8796253Abstract: This invention relates to novel heteroaryl substituted pyrazole compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients or therapeutic measures.Type: GrantFiled: May 8, 2008Date of Patent: August 5, 2014Assignee: Bayer Intellectual Property GmbHInventors: Stephen Boyer, Michael Härter, Philip Wickens, Manoj Patel, Ellalahewage Sathyajith Kumarasinghe, Ajay Kumar Bhargava, Karl-Heinz Thierauch, Hartmut Beck, Susanne Greschat, Peter Ellinghaus, Patrick Paulus, Holger Hess-Stumpp
-
Patent number: 8796254Abstract: Disclosed are uses of carboxamide, sulfonamide and amine compounds for the treatment and amelioration of disorders and conditions related to oxidative stress, mitochondrial dysfunction, free radical damage and metabolic inefficiency, among others. Also described are methods for increasing exercise endurance, exercise efficiency and aerobic workload using the compounds described herein.Type: GrantFiled: March 31, 2011Date of Patent: August 5, 2014Assignee: Rigel Pharmaceuticals, Inc.Inventors: Donald Payan, Yasumichi Hitoshi, Todd Kinsella
-
Publication number: 20140213568Abstract: The invention relates to new pyrrolidine derivatives of the formula to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: January 22, 2014Publication date: July 31, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Martin FLECK, Niklas HEINE, Bernd NOSSE, Gerald Juergen ROTH
-
Publication number: 20140213574Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: ApplicationFiled: April 16, 2014Publication date: July 31, 2014Applicant: Celgene Avilomics Research, Inc.Inventors: Juswinder Singh, Russell Petter, Richland Wayne Tester, Arthur F. Kluge, Hormoz Mazdiyasni, William Frederick Westlin, III, Deqiang Niu, Lixin Qiao
-
Publication number: 20140213569Abstract: Substituted 6-amino-nicotinamides, pharmaceutical compositions containing these compounds and also use of these compounds in the treatment and/or prophylaxis of pain and further diseases and/or disorders.Type: ApplicationFiled: March 31, 2014Publication date: July 31, 2014Applicant: GRUNENTHAL GMBHInventors: Sven KÜHNERT, Gregor BAHRENBERG, Achim KLESS, Wolfgang SCHRÖDER, Simon LUCAS
-
Publication number: 20140213572Abstract: Unsaturated nitrogen heterocyclic compounds of formula (I): as defined in the specification, compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, Huntington's Disease, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.Type: ApplicationFiled: April 1, 2014Publication date: July 31, 2014Applicant: AMGEN INC.Inventors: Jennifer R. Allen, Jian J. Chen, Michael J. Frohn, Essa Hu Harrington, Qingyian Liu, Alexander J. Pickrell, Shannon Rumfelt, Robert M. Rzasa, Wenge Zhong
-
Publication number: 20140213570Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: April 1, 2014Publication date: July 31, 2014Applicant: NOVARTIS AGInventors: Atwood Kim CHEUNG, Donovan Noel CHIN, Natalie DALES, Aleem FAZAL, Timothy HURLEY, John KERRIGAN, Gary O'BRIEN, Lei SHU, Robert SUN, Moo Je SUNG
-
Publication number: 20140206660Abstract: The present invention provides phenyl-heteroaryl derivatives of Formula (I) and pharmaceutically acceptable salts thereof These compounds are useful in the treatment of RAGE-mediated diseases. The present invention further relates to methods for the preparation of compounds of Formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising such compounds, and the use of such compounds and/or pharmaceutical compositions in treating RAGE-mediated diseases.Type: ApplicationFiled: March 26, 2014Publication date: July 24, 2014Applicant: TransTech Pharma, LLCInventors: Devi R. Gohimukkula, David Jones, Ghassan Qabaja, Jeff J. Zhu, Jeremy T. Cooper, William K. Banner, Kurt Sundermann, Muralidhar Bondlela, Mohan Rao, Pingzhen Wang, Raju B. Gowda, Robert C. Andrews, Suparna Gupta, Anitha Hari, Rongyuan Xie
-
Patent number: 8778925Abstract: The present invention relates to pyridine and pyrimidine based compounds, pharmaceutical compositions comprising these compounds and their potential use as therapeutic agents for the treatment and/or prevention of cancer.Type: GrantFiled: October 6, 2009Date of Patent: July 15, 2014Assignee: Cancer Research Technology Ltd.Inventors: Edward McDonald, Julian Blagg, Mark Pichowicz, Simon Ross Crumpler
-
Patent number: 8778926Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, LP, LQ, X1, X2, X3, A, n and m are as defined in the application. The compounds of formula I have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.Type: GrantFiled: January 20, 2012Date of Patent: July 15, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Frank Himmelsbach, Elke Langkopf, Bernd Nosse
-
Publication number: 20140194402Abstract: Described herein are methods for using compounds that activate pyruvate kinase.Type: ApplicationFiled: May 3, 2012Publication date: July 10, 2014Applicant: AGIOS PHARMACEUTICALS, INCInventor: Shin-San M. Su
-
Patent number: 8772277Abstract: The present invention provides a novel compound having a superior activity as an ERR-? modulator and useful as an agent for the prophylaxis or treatment of ERR-? associated diseases. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.Type: GrantFiled: August 3, 2012Date of Patent: July 8, 2014Assignee: Takeda Pharmaceutical Company LimitedInventors: Shigemitsu Matsumoto, Koji Ono, Yusuke Tominari, Taisuke Katoh, Kazuhiro Miwa, Atsushi Hasuoka, Shinichi Imamura
-
Publication number: 20140187533Abstract: The invention relates to compounds useful in treating conditions associated with voltage-gated ion channel function, particularly conditions associated with sodium channel activity. More specifically, the invention concerns compounds (e.g., compounds according to any of Formulas (I)-(XIII) or Compounds (1)-(236) of Table 1) that are useful in treatment of a variety of diseases and conditions.Type: ApplicationFiled: March 2, 2012Publication date: July 3, 2014Applicant: Zalicus Pharmaceuticals Ltd.Inventors: Hassan Pajouhesh, Richard Holland, Lingyun Zhang, Hossein Pajouhesh, Jason Lamontagne, Brendan Whelan
-
Publication number: 20140187531Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.Type: ApplicationFiled: March 3, 2014Publication date: July 3, 2014Applicant: AbbVie Inc.Inventors: Milan Bruncko, Hong Ding, Steven W. Elmore, Aaron R. Kunzer, Christopher L. Lynch, William J. McClellan, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Xilu Wang, Noah P. Tu, Michael D. Wendt, Alexander R. Shoemaker, Michael J. Mitten
-
Publication number: 20140187529Abstract: A compound of formula (I): wherein all symbols have the same meanings as defined in the specification; a salt thereof, a solvate thereof, an N-oxide thereof, or a prodrug thereof, has an Itk inhibitory activity, and is useful as a method for preventing and/or treating atopic dermatitis, and the like.Type: ApplicationFiled: February 29, 2012Publication date: July 3, 2014Applicant: LOCUS PHARMACEUTICALS, INC.Inventors: Rupa S. Shetty, Martha J. Kelly, Bin Liu, Jinming Zou, Kristopher K. Moffett, Younghee Lee
-
Publication number: 20140187530Abstract: The present invention provides a compound of Formula I or Formula II: enantiomer, diastereomer, prodrug, solvate, metabolite, or pharmaceutically acceptable salt thereof, wherein constituent variables are provided herein. The compounds of Formula I and II are modulators of metalloproteases and are useful in treating diseases associated with metalloprotease activity such as arthritis, cancer, cardiovascular disorders, skin disorders, inflammation and allergic conditions.Type: ApplicationFiled: November 27, 2013Publication date: July 3, 2014Applicant: INCYTE CORPORATIONInventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Fenglei Zhang, Brian W. Metcalf
-
Patent number: 8765733Abstract: The invention relates to amine substituted methanesulfonamide derivatives as vanilloid receptor ligands, 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: GrantFiled: September 25, 2012Date of Patent: July 1, 2014Assignee: Gruenenthal GmbHInventors: Robert Frank, Gregor Bahrenberg, Thomas Christoph, Bernhard Lesch, Jeewoo Lee
-
Patent number: 8765730Abstract: This invention relates to novel 1-hydroxyimino-3-phenyl-propanes of the formula wherein R1 to R10 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and may be used as medicaments for the treatment of diseases such as type II diabetes.Type: GrantFiled: July 12, 2011Date of Patent: July 1, 2014Assignee: Hoffmann-La Roche IncInventors: Caterina Bissantz, Henrietta Dehmlow, Shawn David Erickson, Kyungjin Kim, Rainer E. Martin, Patrizio Mattei, Ulrike Obst Sander, Sherrie Lynn Pietranico-Cole, Hans Richter, Christoph Ullmer
-
Publication number: 20140179670Abstract: The present invention provides: an uracil derivative represented by general formula (I) or a physiologically acceptable salt thereof (in the formula, R1 represents a hydrogen atom, a C1-10 alkyl group, a C2-6 alkene group or a 3- to 6-membered saturated or 4- to 6-membered unsaturated aliphatic ring group which may contain 1 to 2 hetero atoms independently selected from the group consisting of N, O and S; R2 represents a hydrogen atom, a halogen atom, a cyano group, —NRcRd, —N?CHN(CH3)2, or an C1-3 alkyl group; Ar1 and Ar2 independently represent a 5- to 6-membered aromatic ring group which may contain 1 to 3 hetero atoms independently selected from the group consisting of N, O and S; and L represents a 6-membered aromatic ring group which may contain 1 to 4 nitrogen atoms, a pyrazole group, a triazole group, or an imidazole group); and a therapeutic agent or prophylactic agent for various inflammatory diseases associated with elastase, comprises the compound or the like as an active ingredient.Type: ApplicationFiled: July 31, 2012Publication date: June 26, 2014Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.Inventors: Tomoya Shiro, Masanori Tobe, Katsumi Kubota, Yosuke Takanashi, Tomoaki Nakamura, Toshihiko Sone
-
Publication number: 20140179663Abstract: The present invention relates to compounds of Formula (I): Wherein variables are as defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases, diabetes, diabetic nephropathy, cardio-renal diseases, including kidney disease, fibrotic diseases, respiratory diseases, COPD, idiopathic pulmonary fibrosis, acute lung injury, acute and chronic liver diseases, and neurodegenerative diseases.Type: ApplicationFiled: December 20, 2013Publication date: June 26, 2014Applicant: Gilead Sciences, Inc.Inventor: Gregory Notte
-
Publication number: 20140179648Abstract: The present disclosure relates to compounds, which are useful for inhibition of BET protein function by binding to bromodomains, and their use in therapy.Type: ApplicationFiled: December 19, 2013Publication date: June 26, 2014Applicant: RVX Therapeutics Inc.Inventors: Shuang Liu, Bryan Cordell Duffy, John Frederick Quinn, May Xiaowu Jiang, Ruifang Wang, Gregory Scott Martin, He Zhao, Bruce Francis Molino, Peter Ronald Young
-
Publication number: 20140179662Abstract: The present invention relates to disubstituted triazine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said disubstituted triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said disubstituted triazine derivatives as inhibitors for a protein kinase.Type: ApplicationFiled: March 1, 2012Publication date: June 26, 2014Applicants: LEAD DISCOVERY CENTER GMBH, BAYER INTELLECTUAL PROPERTY GMBHInventors: Gerd Rühter, Uwe Koch, Peter Nussbaumer, Carsten Schulz-Fademrecht, Jan Eickhoff
-
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
-
Patent number: 8759336Abstract: Novel compounds, methods, and compositions for treating various viral infections are described. In some embodiments the novel compounds of the invention are 3-oxo-phenothiazine derivatives; more specific embodiments include 3-oxo-phenothiazine derivatives having substituents at the 1-, 7-, and 9-positions of the phenothiazine parent ring. In other embodiments, the invention provides compositions and methods for treating viral infections, especially HIV.Type: GrantFiled: March 16, 2012Date of Patent: June 24, 2014Assignee: Prosetta Antiviral Inc.Inventors: Clarence R. Hurt, Vishwanath Lingappa, Beverly Freeman, Andy Atuegbu, Anatoliy Kitaygorodorskyy
-
Patent number: 8759335Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: GrantFiled: January 31, 2005Date of Patent: June 24, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara Hadida Ruah, Peter Grootenhuis, Mark Miller, Matthew Hamilton
-
Publication number: 20140171402Abstract: The present invention relates to an azetidine derivative or a pharmaceutically acceptable salt thereof, and an antidepressant agent or a composition for the prevention or treatment of psychiatric disorders including the same. The azetidine derivative is useful as a triple reuptake inhibitor capable of inhibiting reuptake of the neurotransmitters, dopamine, serotonin, and norepinephrine at the same time.Type: ApplicationFiled: September 4, 2012Publication date: June 19, 2014Inventors: Hoh-Gyu Hahn, Kee-Dal Nam, Min-soo Han, Young-Hue Han, Chi-Man Song, Dong-Yun Shin
-
Publication number: 20140162998Abstract: A Pim kinase inhibitor compound having the structure represented by Formula I, and isomers, diastereomers, enantiomers, tautomers, and pharmaceutically acceptable salts thereof. The compounds significantly inhibit Pim kinase activity and can be used to prepare drugs for treating 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
-
Publication number: 20140162997Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, R2, ring A, and G are defined herein.Type: ApplicationFiled: August 16, 2013Publication date: June 12, 2014Applicant: Janssen Pharmaceutica NVInventors: Mark Wall, Nalin Subasinghe, Zhihua Sui, Christopher Flores
-
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
-
Publication number: 20140162981Abstract: The present application relates to novel substituted aryloxazole derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular and metabolic disorders.Type: ApplicationFiled: May 14, 2013Publication date: June 12, 2014Applicant: BAYER INTELLECTUAL PROPERTY GmbHInventors: Peter NELL, Walter HÜBSCH, Barbara ALBRECHT-KÜPPER, Jorg KELDENICH, Alexandros VAKALOPOULOS, Frank SÜSSMEIER, Katja ZIMMERMANN, Dieter LANG, Daniel MEIBOM
-
Publication number: 20140163008Abstract: A dibenzoxepin derivative represented by the following general formula (I) wherein Y is a hydrogen atom and the like, RA is a hydrogen atom and the like, X is the formula (b3) wherein RB is a hydrogen atom and the like, and the like, A is the formula (a18) wherein R1 is a hydrogen atom and the like, and RC and RD are the same or different and each is a hydrogen atom and the like, and the like, which has a PPAR? agonist activity and the like, and useful as a therapeutic agent and/or prophylaxis agent and the like for type 2 diabetes and the like, or a pharmaceutically acceptable salt thereof and the like is provided.Type: ApplicationFiled: August 3, 2011Publication date: June 12, 2014Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Keisuke Yamamoto, Tomohiro Tamura, Rina Nakamura, Kimihisa Ueno, Shintaro Hosoe
-
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
-
Publication number: 20140155370Abstract: The invention generally relates to the field of nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to new substituted-heterocyclic azole compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity such as in treating cancer and other neoplastic disorders, inflammatory diseases, disorders of abnormal tissue growth and fibrosis including cardiomyopathy, pulmonary fibrosis, hepatic fibrosis, glomerulonephritis, and other renal disorders, and for the treatment of viral infections (both acute and chronic).Type: ApplicationFiled: June 28, 2013Publication date: June 5, 2014Inventors: Sharon Shacham, Michael Kauffman, Vincent P. Sandanayaka, Sharon Shechter
-
Publication number: 20140148430Abstract: Certain imidazopyridines (I) and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.Type: ApplicationFiled: November 26, 2012Publication date: May 29, 2014Applicant: Gilead Connecticut, Inc.Inventors: Peter A. Blomgren, Kevin S. Currie, Jeffrey E. Kropf, Seung H. Lee, Scott A. Mitchell, Aaron C. Schmitt, Jianjun Xu, Zhongdong Zhao
-
Publication number: 20140148431Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infection is disclosed.Type: ApplicationFiled: August 24, 2012Publication date: May 29, 2014Inventors: Mahesh Vithalbhai Patel, Prasad Keshav Deshpande, Satish Bhawsar, Sachin Bhagwat, Mohammed Alam Jafri, Amit Mishra, Laxmikant Pavase, Sunil Gupta, Rajesh Kale, Sanjeev Joshi
-
Patent number: 8735385Abstract: The present disclosure relates to a series of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and formula (Ib). wherein R1, R2, R3, R4, X, m, l, n, p and s are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure relates to methods of preparation of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and (Ib), and intermediates therefor.Type: GrantFiled: November 6, 2012Date of Patent: May 27, 2014Assignee: SanofiInventor: Zhongli Gao
-
Publication number: 20140142082Abstract: The invention provides modulators for the orphan nuclear receptor RORy and methods for treating RORy mediated diseases by administrating these novel RORy modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo sulfonamide compounds of Formula (1) and the enantiomers, diastereomers, tautomers, solvates and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: April 13, 2012Publication date: May 22, 2014Applicant: PHENEX PHARMACEUTICALS AGInventors: Christoph Steeneck, Olaf Kinzel, Christian Gege, Gerald Kleymann, Thomas Hoffmann